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PE20010641A1 - Derivados de piperazina como antagonistas del receptor de serotonina 5-ht1b - Google Patents

Derivados de piperazina como antagonistas del receptor de serotonina 5-ht1b

Info

Publication number
PE20010641A1
PE20010641A1 PE2000000989A PE0009892000A PE20010641A1 PE 20010641 A1 PE20010641 A1 PE 20010641A1 PE 2000000989 A PE2000000989 A PE 2000000989A PE 0009892000 A PE0009892000 A PE 0009892000A PE 20010641 A1 PE20010641 A1 PE 20010641A1
Authority
PE
Peru
Prior art keywords
alkyl
halogen
heteroaryl
serotonin
phenyl
Prior art date
Application number
PE2000000989A
Other languages
English (en)
Inventor
Paul Adrian Wyman
Mervyn Thompson
Howard Marshall
Original Assignee
Smithkline Beecham Plc
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 claimed from GBGB9922831.4A external-priority patent/GB9922831D0/en
Priority claimed from GB0001936A external-priority patent/GB0001936D0/en
Priority claimed from GB0013873A external-priority patent/GB0013873D0/en
Application filed by Smithkline Beecham Plc filed Critical Smithkline Beecham Plc
Publication of PE20010641A1 publication Critical patent/PE20010641A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/10Heterocyclic 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 linked by a carbon chain containing aromatic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/08Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A DERIVADOS DE PIPERAZINA DE FORMULA I, DONDE: Ra ES UN GRUPO i, P1 ES FENILO, NAFTILO, HETEROARILO; R1 Y R2 SON HALOGENO, ALQUILO C1-C6, CICLOALQUILO C3-C6, CO-ALQUILO C1-C6, SR6, SO2NR6R7, NR6CONR7R8, ENTRE OTROS; R6, R7 Y R8 SON H, ALQUILO C1-C6; a ES 0-3; Ra ES UN GRUPO ii; P2 ES FENILO, HETEROARILO, ANILLO HETEROCICLICO DE 5-7 MIEMBROS; P3 ES FENILO, NAFTILO, HETEROARILO; A ES UN ENLACE, O, CARBONILO, CH2, NR4; R4 ES H, ALQUILO C1-C6; O R2 ES UN HETEROARILO OPCIONALMENTE SUSTITUIDO CON ALQUILO C1-C6, HALOGENO, CO-ALQUILO C1-C6, ENTRE OTROS; R3 ES HALOGENO, ALQUILO C1-C6, CICLOALQUILO C3-C6, ENTRE OTROS; b Y c SON 0-3; Y ES UN ENLACE, CH2, O, NR5; R5 ES H, ALQUILO C1-C6; W ES -(CR9R10)t-, -HC=CH-, t ES 2-4; R9 Y R10 SON H, ALQUILO C1-C6; Rb ES H, HALOGENO, HIDROXI, ALQUILO C1-C6, CF3, CO-ALQUILO C1-C6, ENTRE OTROS; Ro ES H, ALQUILO C1-C6, Rd Y Re SON ALQUILO C1-C4. SON COMPUESTOS PREFERIDOS CIS-1-[(2-CLORO-3-TRIFLUOROMETILFENIL)ACETIL]-6-(3,4,5-TRIMETILPIPERAZIN-1-IL)INDOL; CIS-1-[(2-FLUORO-3-TRIFLUOROMETILFENIL)ACETIL]-5-METOXI-6-(3,4,5-TRIMETILPIPERAZIN-1-IL)INDOLINA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. EL COMPUESTO I ES UN ANTAGONISTA DEL RECEPTOR DE SEROTONINA 5-HT1B Y PUEDE SER UTIL PARA EL TRATAMIENTO DE LA DEPRESION
PE2000000989A 1999-09-25 2000-09-22 Derivados de piperazina como antagonistas del receptor de serotonina 5-ht1b PE20010641A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB9922831.4A GB9922831D0 (en) 1999-09-25 1999-09-25 Novel compounds
GB0001936A GB0001936D0 (en) 2000-01-27 2000-01-27 Novel compounds
GB0013873A GB0013873D0 (en) 2000-06-07 2000-06-07 Novel compounds

Publications (1)

Publication Number Publication Date
PE20010641A1 true PE20010641A1 (es) 2001-07-14

Family

ID=27255501

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000000989A PE20010641A1 (es) 1999-09-25 2000-09-22 Derivados de piperazina como antagonistas del receptor de serotonina 5-ht1b

Country Status (27)

Country Link
US (2) US6747030B1 (es)
EP (1) EP1216239B1 (es)
JP (1) JP2003510317A (es)
KR (1) KR20020030126A (es)
CN (1) CN1190432C (es)
AR (1) AR029454A1 (es)
AT (1) ATE259363T1 (es)
AU (1) AU765020B2 (es)
BR (1) BR0014279A (es)
CA (1) CA2385737A1 (es)
CO (1) CO5200839A1 (es)
CZ (1) CZ20021038A3 (es)
DE (1) DE60008262T2 (es)
DK (1) DK1216239T3 (es)
ES (1) ES2211624T3 (es)
HK (1) HK1046909B (es)
HU (1) HUP0202787A3 (es)
IL (1) IL148818A0 (es)
MX (1) MXPA02003175A (es)
MY (1) MY122391A (es)
NO (1) NO20021459D0 (es)
NZ (1) NZ517865A (es)
PE (1) PE20010641A1 (es)
PL (1) PL362900A1 (es)
PT (1) PT1216239E (es)
TR (1) TR200200795T2 (es)
WO (1) WO2001023374A1 (es)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1216239B1 (en) * 1999-09-25 2004-02-11 SmithKline Beecham plc Piperazine derivatives as 5-ht1b antagonists
US6906192B2 (en) 2000-11-07 2005-06-14 Bristol Myers Squibb Company Processes for the preparation of acid derivatives useful as serine protease inhibitors
JP2004514669A (ja) 2000-11-07 2004-05-20 ブリストル−マイヤーズ スクイブ カンパニー セリンプロテアーゼ阻害剤として有用な酸誘導体
GB0106419D0 (en) * 2001-03-15 2001-05-02 Smithkline Beecham Plc Novel compounds
GB0106586D0 (en) * 2001-03-16 2001-05-09 Smithkline Beecham Plc Novel compounds
GB0224557D0 (en) 2002-10-22 2002-11-27 Glaxo Group Ltd Novel compounds
CA2528644A1 (en) 2003-06-18 2004-12-23 Pfizer Products Inc. Novel piperazinyl-aryloxy and piperazinyl-heteroaryloxy-n-aryl lactams
AR053407A1 (es) 2004-07-28 2007-05-09 Glaxo Group Ltd Derivados de piperazina, proceso para la preparacion de dicho compuesto y composicion farmaceutica que lo comprende.
EP2006289B1 (en) 2006-03-31 2011-11-30 Wako Pure Chemical Industries, Ltd. Pyrazole-type cyanine dye
WO2007113202A1 (en) 2006-03-31 2007-10-11 Glaxo Group Limited Piperazine derivatives as growth hormone secretagogue (ghs) receptor agonists
EP3412676B1 (en) 2010-08-10 2020-02-12 Rempex Pharmaceuticals, Inc. Cyclic boronic acid ester derivatives, method for the preparation and therapeutic uses thereof
US9012491B2 (en) 2011-08-31 2015-04-21 Rempex Pharmaceuticals, Inc. Heterocyclic boronic acid ester derivatives and therapeutic uses thereof
US9156858B2 (en) 2012-05-23 2015-10-13 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
US10561675B2 (en) 2012-06-06 2020-02-18 Rempex Pharmaceuticals, Inc. Cyclic boronic acid ester derivatives and therapeutic uses thereof
CN102766139B (zh) * 2012-08-14 2014-09-17 江苏先声药物研究有限公司 阿齐沙坦的多晶型物及其制备方法
US9241947B2 (en) 2013-01-04 2016-01-26 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
EA201591003A1 (ru) 2013-01-04 2015-12-30 Ремпекс Фармасьютикалз, Инк. Производные бороновой кислоты и их терапевтическое применение
US9101638B2 (en) 2013-01-04 2015-08-11 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
US9132140B2 (en) 2013-01-04 2015-09-15 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
EP3604316B1 (en) 2014-05-05 2023-12-06 Melinta Therapeutics, Inc. Synthesis of boronate salts
US9687497B1 (en) 2014-05-05 2017-06-27 Rempex Pharmaceuticals, Inc. Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof
JP6672176B2 (ja) 2014-05-19 2020-03-25 レンペックス・ファーマシューティカルズ・インコーポレイテッド ボロン酸誘導体およびその治療的使用
WO2016003929A1 (en) 2014-07-01 2016-01-07 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
US10662205B2 (en) 2014-11-18 2020-05-26 Qpex Biopharma, Inc. Cyclic boronic acid ester derivatives and therapeutic uses thereof
GB2532990A (en) 2014-12-05 2016-06-08 Schlumberger Holdings Corrosion inhibition
US20180051041A1 (en) 2015-03-17 2018-02-22 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
GB2543498A (en) 2015-10-19 2017-04-26 Schlumberger Holdings Corrosion inhibition
WO2018005662A1 (en) 2016-06-30 2018-01-04 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
IL273551B2 (en) 2017-10-11 2024-02-01 Qpex Biopharma Inc Boronic acid derivatives and their synthesis
CA3097127A1 (en) 2018-04-20 2019-10-24 Qpex Biopharma, Inc. Boronic acid derivatives and therapeutic uses thereof
WO2020183011A1 (en) 2019-03-14 2020-09-17 Institut Curie Htr1d inhibitors and uses thereof in the treatment of cancer

Family Cites Families (7)

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Publication number Priority date Publication date Assignee Title
DE69232003T2 (de) * 1991-09-18 2002-04-25 Glaxo Group Ltd., Greenford Benzanilidderivate als 5-HT1D-Antagonisten
US5696122A (en) * 1993-09-03 1997-12-09 Smithkline Beecham P.L.C. Indole and indoline derivatives as 5HT1D receptor antagonists
CA2274055A1 (en) 1996-12-19 1998-06-25 Smithkline Beecham P.L.C. N-piperazin-1-ylphenyl-benzamide derivatives
EP0975614A1 (en) * 1997-04-18 2000-02-02 Smithkline Beecham Plc A bicyclic aryl or a bicyclic heterocyclic ring containing compounds having a combined 5ht1a, 5ht1b and 5ht1d receptor antagonistic activity
WO1998050358A1 (en) 1997-04-18 1998-11-12 Smithkline Beecham Plc Indole derivatives having combined 5ht1a, 5ht1b and 5ht1d receptor antagonist activity
GB9725931D0 (en) * 1997-12-05 1998-02-04 Smithkline Beecham Plc Novel compounds
EP1216239B1 (en) * 1999-09-25 2004-02-11 SmithKline Beecham plc Piperazine derivatives as 5-ht1b antagonists

Also Published As

Publication number Publication date
US20040176388A1 (en) 2004-09-09
HK1046909B (zh) 2004-12-03
HK1046909A1 (en) 2003-01-30
DE60008262D1 (de) 2004-03-18
PL362900A1 (en) 2004-11-02
KR20020030126A (ko) 2002-04-22
WO2001023374A1 (en) 2001-04-05
CA2385737A1 (en) 2001-04-05
HUP0202787A3 (en) 2003-12-29
PT1216239E (pt) 2004-05-31
DK1216239T3 (da) 2004-06-14
NO20021459L (no) 2002-03-22
EP1216239B1 (en) 2004-02-11
NZ517865A (en) 2003-11-28
MY122391A (en) 2006-04-29
CN1399635A (zh) 2003-02-26
AR029454A1 (es) 2003-07-02
MXPA02003175A (es) 2002-09-30
AU7783600A (en) 2001-04-30
ATE259363T1 (de) 2004-02-15
CN1190432C (zh) 2005-02-23
TR200200795T2 (tr) 2002-07-22
CO5200839A1 (es) 2002-09-27
AU765020B2 (en) 2003-09-04
HUP0202787A2 (hu) 2002-12-28
IL148818A0 (en) 2002-09-12
BR0014279A (pt) 2002-05-21
DE60008262T2 (de) 2004-12-16
US6747030B1 (en) 2004-06-08
JP2003510317A (ja) 2003-03-18
ES2211624T3 (es) 2004-07-16
EP1216239A1 (en) 2002-06-26
CZ20021038A3 (cs) 2002-08-14
NO20021459D0 (no) 2002-03-22

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