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WO2003066604A3 - Nouvelles aryl- et heteroarylpiperazines - Google Patents

Nouvelles aryl- et heteroarylpiperazines Download PDF

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Publication number
WO2003066604A3
WO2003066604A3 PCT/DK2003/000071 DK0300071W WO03066604A3 WO 2003066604 A3 WO2003066604 A3 WO 2003066604A3 DK 0300071 W DK0300071 W DK 0300071W WO 03066604 A3 WO03066604 A3 WO 03066604A3
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WO
WIPO (PCT)
Prior art keywords
compounds
heteroarylpiperazines
histamine
receptor
novel aryl
Prior art date
Application number
PCT/DK2003/000071
Other languages
English (en)
Other versions
WO2003066604A2 (fr
Inventor
Rolf Hohlweg
Florencio Zaragoza Doerwald
Henrik Stephensen
Ingrid Pettersson
Bernd Peschke
Original Assignee
Novo Nordisk As
Boehringer Ingelheim Int
Rolf Hohlweg
Florencio Zaragoza Doerwald
Henrik Stephensen
Ingrid Pettersson
Bernd Peschke
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to IL16285903A priority Critical patent/IL162859A0/xx
Priority to JP2003565978A priority patent/JP4607458B2/ja
Priority to KR10-2004-7011995A priority patent/KR20040081177A/ko
Priority to BR0307429-3A priority patent/BR0307429A/pt
Priority to UA20040705946A priority patent/UA83187C2/ru
Priority to AU2003203148A priority patent/AU2003203148A1/en
Priority to EP03701482A priority patent/EP1474401A2/fr
Priority to CA002474214A priority patent/CA2474214A1/fr
Priority to MXPA04007612A priority patent/MXPA04007612A/es
Application filed by Novo Nordisk As, Boehringer Ingelheim Int, Rolf Hohlweg, Florencio Zaragoza Doerwald, Henrik Stephensen, Ingrid Pettersson, Bernd Peschke filed Critical Novo Nordisk As
Priority to US10/383,310 priority patent/US20030236259A1/en
Publication of WO2003066604A2 publication Critical patent/WO2003066604A2/fr
Publication of WO2003066604A3 publication Critical patent/WO2003066604A3/fr
Priority to ZA2004/05694A priority patent/ZA200405694B/en
Priority to NO20043709A priority patent/NO328714B1/no
Priority to US12/367,952 priority patent/US20090264435A1/en
Priority to AU2010200135A priority patent/AU2010200135A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D237/20—Nitrogen atoms
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    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
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    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/44—Benzopyrazines with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/02—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements
    • C07D295/027—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring
    • C07D295/03—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring with the ring nitrogen atoms directly attached to acyclic carbon atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/02—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements
    • C07D295/027—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring
    • C07D295/033—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring with the ring nitrogen atoms directly attached to carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/06—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals
    • C07D295/073—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals with the ring nitrogen atoms and the substituents separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/096—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/10—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms
    • C07D295/112—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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  • Nitrogen Condensed Heterocyclic Rings (AREA)
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Abstract

L'invention concerne de nouvelles aryl- et hétéroarylpiperazines, l'utilisation de ces composés comme compositions pharmaceutiques, les compositions pharmaceutiques comprenant les composés ainsi qu'une méthode thérapeutique utilisant ces composés et compositions. Les composés font preuve d'une forte affinité de liaison sélective avec le récepteur de l'histamine H3 indiquant une activité antagoniste du récepteur H3, agoniste inverse ou agoniste. Par conséquent, les composés sont utilisés dans le traitement de maladies et de troubles associés au récepteur de l'histamine H3.
PCT/DK2003/000071 2002-02-05 2003-02-05 Nouvelles aryl- et heteroarylpiperazines WO2003066604A2 (fr)

Priority Applications (14)

Application Number Priority Date Filing Date Title
MXPA04007612A MXPA04007612A (es) 2002-02-05 2003-02-05 Aril- y heteroarilpiperazinas novedosas.
KR10-2004-7011995A KR20040081177A (ko) 2002-02-05 2003-02-05 신규 아릴- 및 헤테로아릴피페라진
BR0307429-3A BR0307429A (pt) 2002-02-05 2003-02-05 Composto, uso do mesmo, composição farmacêutica, e, método para o tratamento de distúrbios ou doenças relacionadas com receptor de histamina h3
UA20040705946A UA83187C2 (en) 2002-02-05 2003-02-05 Aryl- and heteroarylpiperazines
AU2003203148A AU2003203148A1 (en) 2002-02-05 2003-02-05 Novel aryl- and heteroarylpiperazines
EP03701482A EP1474401A2 (fr) 2002-02-05 2003-02-05 Nouvelles aryl- et heteroarylpiperazines
CA002474214A CA2474214A1 (fr) 2002-02-05 2003-02-05 Nouvelles aryl- et heteroarylpiperazines
IL16285903A IL162859A0 (en) 2002-02-05 2003-02-05 Novel aryl-and heteroarylpiperazines
JP2003565978A JP4607458B2 (ja) 2002-02-05 2003-02-05 新規なアリールおよびへテロアリールピペラジン
US10/383,310 US20030236259A1 (en) 2002-02-05 2003-03-07 Novel aryl- and heteroarylpiperazines
ZA2004/05694A ZA200405694B (en) 2002-02-05 2004-07-16 Novel aryl-and heteroarylpiperazines
NO20043709A NO328714B1 (no) 2002-02-05 2004-09-03 Aryl- og heteroarylpiperaziner, farmasoytiske preparater som omfatter minst en slik forbindelse, samt anvendelser av slike forbindelser til fremstilling av farmasoytiske preparater
US12/367,952 US20090264435A1 (en) 2002-02-05 2009-02-09 Novel Aryl- and Heteroarylpiperazines
AU2010200135A AU2010200135A1 (en) 2002-02-05 2010-01-13 Novel aryl-and heteroarylpiperazines

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
DKPA200200168 2002-02-05
DKPA200200168 2002-02-05
US35663002P 2002-02-08 2002-02-08
US60/356,630 2002-02-08
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Families Citing this family (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7390813B1 (en) 2001-12-21 2008-06-24 Xenon Pharmaceuticals Inc. Pyridylpiperazines and aminonicotinamides and their use as therapeutic agents
GB0224084D0 (en) * 2002-10-16 2002-11-27 Glaxo Group Ltd Novel compounds
AU2003287206A1 (en) 2002-10-23 2004-05-13 Janssen Pharmaceutica, N.V. Phenylpiperidines and phenylpyrrolidines as histamine h3 receptor modulators
KR20060054392A (ko) * 2003-07-29 2006-05-22 노보 노르디스크 에이/에스 피리다지닐-피페라진 및 히스타민 ｈ３ 수용체 리간드로서그들의 사용
US7754711B2 (en) * 2003-07-30 2010-07-13 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
DK1648874T3 (da) 2003-07-30 2012-01-23 Xenon Pharmaceuticals Inc Piperazinderivater samt deres anvendelse som terapeutisk aktive stoffer
ATE555789T1 (de) * 2003-07-30 2012-05-15 Xenon Pharmaceuticals Inc Pyridazinderivate und deren verwendung als therapeutische mittel
SG145700A1 (en) 2003-07-30 2008-09-29 Xenon Pharmaceuticals Inc Pyridyl derivatives and their use as therapeutic agents
WO2005035521A1 (fr) * 2003-10-09 2005-04-21 Argenta Discovery Ltd. Quinoleines substituees, utilisees comme modulateurs de la mch
GB0324159D0 (en) 2003-10-15 2003-11-19 Glaxo Group Ltd Novel compounds
JP4596792B2 (ja) * 2004-02-24 2010-12-15 あすか製薬株式会社 ５−ｈｔ１ａ作動作用と５−ｈｔ３拮抗作用を併有する薬剤
WO2005097751A2 (fr) * 2004-03-31 2005-10-20 Janssen Pharmaceutica, N.V. Composes heterocycliques non-imidazole
WO2005097127A2 (fr) 2004-04-02 2005-10-20 Merck & Co., Inc. Methode destinee a traiter des hommes presentant des troubles metaboliques et anthropometriques
US20050256309A1 (en) * 2004-05-12 2005-11-17 Altenbach Robert J Tri-and bi-cyclic heteroaryl histamine-3 receptor ligands
MXPA06015267A (es) * 2004-06-22 2007-03-15 Pfizer Prod Inc Antagonistas diazabiciclicos del receptor histamina-3.
AU2005286846A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as therapeutic agents
MX2007003318A (es) 2004-09-20 2007-05-18 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como agentes terapeuticos.
AU2005286648A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
EP2269610A3 (fr) 2004-09-20 2011-03-09 Xenon Pharmaceuticals Inc. Dérivés hétérocycliques et leur utilisation en tant qu'inhibiteurs de la stearoyl-coa desaturase
EP1807085B1 (fr) 2004-09-20 2013-08-21 Xenon Pharmaceuticals Inc. Dérivés hétérocycliques et leur utilisation en tant qu'agents thérapeutiques
ES2359840T5 (es) * 2004-09-20 2015-03-25 Xenon Pharmaceuticals Inc. Derivados de piridina para inhibición de estearoil-CoA-desaturasa humana
CA2580781A1 (fr) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Derives heterocycliques bicycliques et leur utilisation comme inhibiteurs de stearoyl-coa desaturase (scd)
TW200626155A (en) 2004-09-20 2006-08-01 Xenon Pharmaceuticals Inc Heterocyclic derivatives and their use as therapeutic agents
MX2007003327A (es) 2004-09-20 2007-06-05 Xenon Pharmaceuticals Inc Derivados heterociclicos, y su uso como mediadores de estearoil-coa desaturasa.
US8367672B2 (en) * 2004-11-02 2013-02-05 Universite De Strasbourg Pyridazine compounds, compositions and methods
RU2007131400A (ru) 2005-03-01 2009-04-10 Вайет (Us) Соединения циннолина и их применение в качестве модуляторов х-рецепторов печени
JP2009513563A (ja) 2005-06-03 2009-04-02 ゼノン・ファーマシューティカルズ・インコーポレイテッド ヒトのステアロイル−ＣｏＡデサチュラーゼ阻害剤としてのアミノチアゾール誘導体
BRPI0613564A2 (pt) 2005-07-04 2011-01-18 Novo Nordisk As compostos, seus usos na preparação de composições farmacêuticas e composições farmacêuticas compreendendo os mesmos
RS51994B (en) * 2005-07-05 2012-04-30 F. Hoffmann-La Roche Ag DERIVATI PIRIDAZINA
EP1917245A1 (fr) * 2005-08-21 2008-05-07 Abbott GmbH & Co. KG Composes heterocycliques et leur utilisation en tant que partenaires de liaison des recepteurs 5-ht5
GB0517184D0 (en) * 2005-08-22 2005-09-28 Glaxo Group Ltd Compounds
JP5185120B2 (ja) 2005-09-16 2013-04-17 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ヒスタミンｈ３受容体のモジュレーターとしてのシクロプロピルアミン
JO2769B1 (en) 2005-10-26 2014-03-15 جانسين فارماسوتيكا ان. في Rapid decomposition of physiologically antagonistic agents of the 2-dopamine receptor
MX2008011123A (es) * 2006-03-28 2008-09-30 High Point Pharmaceuticals Llc Benzotiazoles que tienen actividad de receptor h3 de histamina.
CN101754762A (zh) * 2006-04-28 2010-06-23 西北大学 用于治疗神经炎症性疾病的包含哒嗪化合物的制剂
US8318927B2 (en) 2006-05-23 2012-11-27 High Point Pharmaceuticals, Llc 6-(4-cyclopropylpiperazin-1-yl)-2′-methyl-[3, 4′]-bipyridine and its uses as a medicament
BRPI0711370A2 (pt) * 2006-05-29 2011-11-01 High Point Pharmaceuticals Llc 3-(1,3-benzodioxol-5-il)-6-(4-ciclopropilpiperazin-1-il)pi ridazina e seus sais e solvatos e seu uso como antagonista receptor h3 de histamina
JP5285603B2 (ja) * 2006-05-30 2013-09-11 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ヒスタミンｈ３受容体のモジュレーターとしての置換ピリジルアミド化合物
AU2007267184A1 (en) * 2006-05-30 2007-12-06 F. Hoffmann-La Roche Ag Piperidinyl pyrimidine derivatives
US9108948B2 (en) 2006-06-23 2015-08-18 Abbvie Inc. Cyclopropyl amine derivatives
NZ611323A (en) 2006-06-23 2014-10-31 Abbvie Bahamas Ltd Cyclopropyl amine derivatives as histamin h3 receptor modulators
JP2009541460A (ja) * 2006-07-03 2009-11-26 ベレナギング ヴォー クリスタラク ホガー オンダーヴェイル ヴェーテンザパーリク オンダージーク エン パシェンテンゾーク ヒスタミンｈ４受容体と相互作用する縮合二環式化合物
JO2642B1 (en) 2006-12-08 2012-06-17 جانسين فارماسوتيكا ان. في Dopamine 2 receptor antagonists are rapidly hydrolyzed
JO2849B1 (en) * 2007-02-13 2015-03-15 جانسين فارماسوتيكا ان. في Dopamine 2 receptor antagonists are rapidly hydrolyzed
DK2148873T3 (da) 2007-04-23 2012-11-26 Janssen Pharmaceutica Nv 4-alkoxypyridazinderivater som hurtigt dissocierende dopamin 2- receptorantagonister
CA2682671C (fr) 2007-04-23 2015-11-17 Janssen Pharmaceutica N.V. Thia(dia)zoles en tant qu'antagonistes du recepteur de la dopamine a dissociation rapide
CA2687931C (fr) * 2007-05-31 2016-05-24 Boehringer Ingelheim International Gmbh Antagonistes des recepteurs ccr2 et utilisations de ceux-ci
EP2014656A3 (fr) 2007-06-11 2011-08-24 High Point Pharmaceuticals, LLC Nouveaux antagonistes d'hétéocycliques h3
CA2695071A1 (fr) * 2007-08-02 2009-02-05 F. Hoffmann-La Roche Ag Utilisation de derives de benzamide pour le traitement de troubles du snc
AR068370A1 (es) 2007-09-06 2009-11-11 Glaxo Group Ltd 1-(1-metiletil)-4-{[4-(tetrahidro-2h-piran-4-iloxi)fenil]carbonil}piperazina y su sal de hidrocloruro, composiciones farmaceuticas que la contienen, su uso en el tratamiento o profilaxis de enfermedades neurologicas y proceso para su preparacion.
US8883776B2 (en) 2007-11-20 2014-11-11 Janssen Pharmaceutica N.V. Cycloalkyloxy- and heterocycloalkyloxypyridine compounds as modulators of the histamine H3 receptor
US20120129870A1 (en) * 2007-12-17 2012-05-24 Wenying Chai Piperazinyl derivatives useful as modulators of the neuropeptide y2 receptor
US20120015957A1 (en) * 2007-12-17 2012-01-19 Wenying Chai Piperazinyl derivatives useful as modulators of the neuropeptide y2 receptor
US8530474B2 (en) 2008-07-03 2013-09-10 Janssen Pharmaceutica Nv Substituted 6-(1-piperazinyl)-pyridazines as 5-HT6 receptor antagonists
ES2622161T3 (es) 2008-07-31 2017-07-05 Janssen Pharmaceutica, N.V. Piridinas sustituidas con piperazin-1-il-trifluorometilo como antagonistas del receptor de la dopamina 2 de disociación rápida
PL2379525T3 (pl) 2008-12-19 2016-01-29 Centrexion Therapeutics Corp Cykliczne pirymidyno-4-karboksamidy jako antagoniści receptora CCR2 do leczenia stanów zapalnych, astmy oraz COPD
US9186353B2 (en) 2009-04-27 2015-11-17 Abbvie Inc. Treatment of osteoarthritis pain
SI2513093T1 (sl) 2009-12-17 2014-11-28 Boehringer Ingelheim International Gmbh Novi CCR2 receptorski antagonisti in njihove uporabe
WO2011103091A1 (fr) 2010-02-18 2011-08-25 Transtech Pharma, Inc. Dérivés de phényl-hétéroaryle et procédés d'utilisation de ceux-ci
EP2569295B1 (fr) 2010-05-12 2014-11-19 Boehringer Ingelheim International GmbH Nouveaux antagonistes du récepteur ccr2, son procédé de production et utilisation associée en tant que médicaments
JP2013526507A (ja) 2010-05-12 2013-06-24 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規ｃｃｒ２受容体アンタゴニスト、その製造方法及び薬物としてのその使用
US8841313B2 (en) 2010-05-17 2014-09-23 Boehringer Ingelheim International Gmbh CCR2 antagonists and uses thereof
EP2576542B1 (fr) 2010-05-25 2015-04-22 Boehringer Ingelheim International GmbH Dérivés d'amide cycliques d'acides pyridazine-3-carboxyliques utiles dans le traitement de maladies respiratoires, liées à des douleurs, liées au système immunitaire et cardiovasculaires
WO2011151251A1 (fr) 2010-06-01 2011-12-08 Boehringer Ingelheim International Gmbh Nouveaux antagonistes du ccr2
US8853390B2 (en) 2010-09-16 2014-10-07 Abbvie Inc. Processes for preparing 1,2-substituted cyclopropyl derivatives
JP5786258B2 (ja) 2011-07-15 2015-09-30 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規かつ選択的なｃｃｒ２拮抗薬
WO2013151982A1 (fr) 2012-04-03 2013-10-10 Arena Pharmaceuticals, Inc. Méthodes et composés utiles pour traiter le prurit, et procédés d'identification desdits composés
RU2719422C2 (ru) 2014-08-04 2020-04-17 Нуэволюшон А/С Необязательно конденсированные гетероциклил-замещенные производные пиримидина, пригодные для лечения воспалительных, метаболических, онкологических и аутоиммунных заболеваний
MX383744B (es) 2015-07-02 2025-03-14 Centrexion Therapeutics Corp Citrato de (4-((3r,4r)-3-metoxitetrahidro-piran-4-ilamino)piperidin-1-il) (5-metil-6-(((2r, 6s)-6-(p-tolil)tetrahidro-2h-piran-2-il) metilamino) pirimidin-4-il) metanona.
JP2021098692A (ja) 2019-12-20 2021-07-01 ヌエヴォリューション・アクティーゼルスカブＮｕｅｖｏｌｕｔｉｏｎ Ａ／Ｓ 核内受容体に対して活性の化合物
WO2021198955A1 (fr) 2020-03-31 2021-10-07 Nuevolution A/S Composés actifs vis-à-vis des récepteurs nucléaires
EP4126875A1 (fr) 2020-03-31 2023-02-08 Nuevolution A/S Composés actifs vis-à-vis des récepteurs nucléaires

Citations (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB753166A (en) * 1953-05-22 1956-07-18 Miles Lab Improvements in or relating to substituted piperazines
US2993899A (en) * 1958-03-31 1961-07-25 Miles Lab Acetylenically unsaturated piperazine derivatives
US3309370A (en) * 1964-07-16 1967-03-14 Miles Lab Bicycloalkyl piperazine derivatives and process
DE2609746A1 (de) * 1975-04-07 1976-10-14 Parcor Piperazinverbindungen sowie arzneimittel, die diese verbindungen enthalten
EP0177392A1 (fr) * 1984-09-14 1986-04-09 Innothera Nouvelles (pyridyl-2)-1 pipérazines, leur procédé de préparation et leur application en thérapeutique
EP0236140A2 (fr) * 1986-03-05 1987-09-09 Otsuka Pharmaceutical Co., Ltd. Dérivés de carbostyrile et leurs sels et agents arythmiques les contenant
DE3803860A1 (de) * 1988-02-09 1989-08-17 Basf Ag N,n'-disubstituierte piperazine
EP0385237A2 (fr) * 1989-03-03 1990-09-05 Dainippon Pharmaceutical Co., Ltd. Dérivés de 2-(1-pipérazinyl)-4-phénylcycloalkynopyridines, procédés de préparation et compositions pharmaceutiques les contenant
AU639529B2 (en) * 1987-03-04 1993-07-29 Higuchi, Yoshinari Carbostyril derivatives and salts thereof and anti-arrhythmic agents containing the carbostyril derivatives
WO1997002245A1 (fr) * 1995-07-06 1997-01-23 Japan Tobacco Inc. Derives de benzamidoxime et leur utilisation a des fins medicinales
WO1998027081A1 (fr) * 1996-12-19 1998-06-25 Smithkline Beecham Plc Derives de sulfamide, procede de preparation de ces derives et utilisation de ces derniers en tant que medicaments
EP1020445A1 (fr) * 1997-10-02 2000-07-19 Eisai Co., Ltd. Derives de pyridine condenses
WO2000066578A1 (fr) * 1999-04-30 2000-11-09 Pfizer Products Inc. Composes pour le traitement de l'obesite
WO2001044201A1 (fr) * 1999-12-16 2001-06-21 Schering Corporation Antagonistes du recepteur y5 au neuropeptide y a imidazoles substituees
WO2001064645A2 (fr) * 2000-03-01 2001-09-07 Orion Corporation Derives de quinoline utilises comme antagonistes alpha2

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4144346A (en) * 1977-01-31 1979-03-13 Janssen Pharmaceutica N.V. Novel 1-(1,3-dioxolan-2-ylmethyl)-1H-imidazoles
US4163849A (en) * 1978-03-17 1979-08-07 Merck & Co., Inc. Piperazinylpyrazines
JPS56118074A (en) * 1980-02-22 1981-09-16 Tanabe Seiyaku Co Ltd Propane derivative and its preparation
US4339579A (en) * 1980-12-29 1982-07-13 American Home Products Corporation 2,6-Bis-(pyrrolopyrazinyl)pyrazines
US5001125A (en) * 1984-03-26 1991-03-19 Janssen Pharmaceutica N.V. Anti-virally active pyridazinamines
JP2576862B2 (ja) * 1986-03-05 1997-01-29 大塚製薬 株式会社 カルボスチリル誘導体
GB9012316D0 (en) * 1990-06-01 1990-07-18 Wellcome Found Pharmacologically active cns compounds
JPH0971564A (ja) * 1995-07-06 1997-03-18 Japan Tobacco Inc ベンズアミドオキシム誘導体及びその医薬用途
JP3989102B2 (ja) * 1997-10-02 2007-10-10 エーザイ・アール・アンド・ディー・マネジメント株式会社 縮合ピリジン誘導体
GB9926303D0 (en) * 1999-11-05 2000-01-12 Smithkline Beecham Plc Novel compounds
GB9926302D0 (en) * 1999-11-05 2000-01-12 Smithkline Beecham Plc Novel compounds
JP4739650B2 (ja) * 2001-01-31 2011-08-03 ハー・ルンドベック・アクティーゼルスカブ うつ病および／又は不安症を治療するためのｇａｌ３受容体アンタゴニストの使用、およびこのような方法において有用な化合物
WO2003104235A1 (fr) * 2002-06-06 2003-12-18 Novo Nordisk A/S Azepines et pyrazines substituees

Patent Citations (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB753166A (en) * 1953-05-22 1956-07-18 Miles Lab Improvements in or relating to substituted piperazines
US2993899A (en) * 1958-03-31 1961-07-25 Miles Lab Acetylenically unsaturated piperazine derivatives
US3309370A (en) * 1964-07-16 1967-03-14 Miles Lab Bicycloalkyl piperazine derivatives and process
DE2609746A1 (de) * 1975-04-07 1976-10-14 Parcor Piperazinverbindungen sowie arzneimittel, die diese verbindungen enthalten
EP0177392A1 (fr) * 1984-09-14 1986-04-09 Innothera Nouvelles (pyridyl-2)-1 pipérazines, leur procédé de préparation et leur application en thérapeutique
EP0236140A2 (fr) * 1986-03-05 1987-09-09 Otsuka Pharmaceutical Co., Ltd. Dérivés de carbostyrile et leurs sels et agents arythmiques les contenant
AU639529B2 (en) * 1987-03-04 1993-07-29 Higuchi, Yoshinari Carbostyril derivatives and salts thereof and anti-arrhythmic agents containing the carbostyril derivatives
DE3803860A1 (de) * 1988-02-09 1989-08-17 Basf Ag N,n'-disubstituierte piperazine
EP0385237A2 (fr) * 1989-03-03 1990-09-05 Dainippon Pharmaceutical Co., Ltd. Dérivés de 2-(1-pipérazinyl)-4-phénylcycloalkynopyridines, procédés de préparation et compositions pharmaceutiques les contenant
WO1997002245A1 (fr) * 1995-07-06 1997-01-23 Japan Tobacco Inc. Derives de benzamidoxime et leur utilisation a des fins medicinales
WO1998027081A1 (fr) * 1996-12-19 1998-06-25 Smithkline Beecham Plc Derives de sulfamide, procede de preparation de ces derives et utilisation de ces derniers en tant que medicaments
EP1020445A1 (fr) * 1997-10-02 2000-07-19 Eisai Co., Ltd. Derives de pyridine condenses
WO2000066578A1 (fr) * 1999-04-30 2000-11-09 Pfizer Products Inc. Composes pour le traitement de l'obesite
WO2001044201A1 (fr) * 1999-12-16 2001-06-21 Schering Corporation Antagonistes du recepteur y5 au neuropeptide y a imidazoles substituees
WO2001064645A2 (fr) * 2000-03-01 2001-09-07 Orion Corporation Derives de quinoline utilises comme antagonistes alpha2

Non-Patent Citations (26)

* Cited by examiner, † Cited by third party
Title
BULLETIN DE LA SOCIETE CHIMIQUE DE FRANCE, vol. 1, 1969, pages 319 - 324, ISSN: 0037-8968 *
CHEMICAL & PHARMACEUTICAL BULLETIN, vol. 38, no. 5, 1990, pages 1286 - 1291, ISSN: 0009-2363 *
CHEMICAL & PHARMACEUTICAL BULLETIN, vol. 39, no. 2, 1991, pages 367 - 371, ISSN: 0009-2363 *
COMPTES RENDUS DES SEANCES DE L'ACADEMIE DES SCIENCES, SERIE C: SCIENCES CHIMIQUE, vol. 267, no. 12, 1968, pages 724 - 727, ISSN: 0567-6541 *
DATABASE ZCAPLUS [online] BALLABEN E ET AL: "Reactivity of cyclopentanone enamines towards non-symmetric electrophilic diazenes.", XP002902956, retrieved from STN Database accession no. 1994:191665 *
DATABASE ZCAPLUS [online] HORI MANABU ET AL: "Novel 4-substituted 2-piperazinylquinazolines as potent anticonvulsive and antihypoxic agents.", XP002902958, retrieved from STN Database accession no. 1990:552359 *
DATABASE ZCAPLUS [online] HORI MANABU ET AL: "Potential nootropic agents, 4-alkoxy-2-(1-piperazinyl)quinazoline derivatives.", XP002902957, retrieved from STN Database accession no. 1991:400232 *
DATABASE ZCAPLUS [online] MAZARGUIL H ET AL: "Enamines of N-methyl- and N- phenylpiperazine. I. Synthesis and physicochemical study.", XP002902959, retrieved from STN Database accession no. 1969:106472 *
DATABASE ZCAPLUS [online] MAZARGUIL H ET AL: "Enamines of N-methyl and N- phenylpiperazines. Synthesis of unsymmetrical N,N'-disubstituted and N-monosubstituted piperazines.", XP002902960, retrieved from STN Database accession no. 1969:20015 *
DATABASE ZCAPLUS [online] WU QIUYE ET AL: "Synthesis and platelet aggregation activity of 6-[4-substituted- piperazinyl)phenyl]-4,5-dihydro-3(2H)-pyridazinones.", XP002902955, retrieved from STN Database accession no. 1999:729780 *
DATABASE ZCAPLUS [online] XP002902943, retrieved from STN Database accession no. 2001:661394 *
DATABASE ZCAPLUS [online] XP002902944, retrieved from STN Database accession no. 2001:453029 *
DATABASE ZCAPLUS [online] XP002902945, retrieved from STN Database accession no. 2000:790496 *
DATABASE ZCAPLUS [online] XP002902946, retrieved from STN Database accession no. 1997:140310 *
DATABASE ZCAPLUS [online] XP002902947, retrieved from STN Database accession no. 1994:298482 *
DATABASE ZCAPLUS [online] XP002902948, retrieved from STN Database accession no. 1991:143438 *
DATABASE ZCAPLUS [online] XP002902949, retrieved from STN Database accession no. 1986:491334 *
DATABASE ZCAPLUS [online] XP002902950, retrieved from STN Database accession no. 1977:43741 *
DATABASE ZCAPLUS [online] XP002902951, retrieved from STN Database accession no. 1990:35892 *
DATABASE ZCAPLUS [online] XP002902952, retrieved from STN Database accession no. 1968:2915 *
DATABASE ZCAPLUS [online] XP002902953, retrieved from STN Database accession no. 1957:39516 *
DATABASE ZCAPLUS [online] XP002902954, retrieved from STN Database accession no. 1999:244638 *
DATABASE ZCAPLUS [online] XP002902961, retrieved from STN Database accession no. 1998:424243 *
DATABASE ZCAPLUS [online] XP002902965, retrieved from STN Database accession no. 1988:406428 *
GAZZETTA CHIMICA ITALIANA, vol. 123, no. 7, 1993, pages 387 - 391, ISSN: 0016-5603 *
ZHONGGUO YAOWU HUAXUE ZAZHI, vol. 9, no. 3, 1999, pages 172 - 175, 185, ISSN: 1005-0108 *

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