+

WO1993014084A3 - Piperidine derivatives - Google Patents

Piperidine derivatives Download PDF

Info

Publication number
WO1993014084A3
WO1993014084A3 PCT/EP1993/000101 EP9300101W WO9314084A3 WO 1993014084 A3 WO1993014084 A3 WO 1993014084A3 EP 9300101 W EP9300101 W EP 9300101W WO 9314084 A3 WO9314084 A3 WO 9314084A3
Authority
WO
WIPO (PCT)
Prior art keywords
alkyl
represents hydrogen
4alkoxy
piperidine derivatives
relates
Prior art date
Application number
PCT/EP1993/000101
Other languages
French (fr)
Other versions
WO1993014084A2 (en
Inventor
Anthony William James Cooper
Russell Michael Hagan
Original Assignee
Glaxo Group Ltd
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
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of WO1993014084A2 publication Critical patent/WO1993014084A2/en
Publication of WO1993014084A3 publication Critical patent/WO1993014084A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C07D401/06—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 linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

The present invention relates to the novel piperidine derivatives of formula (I) wherein R1 represents phenyl optionally substituted by one or two C¿1-4?alkyl, C1-4alkoxy, trifluoromethyl groups or halogen atoms; R?2¿ represents hydrogen, hydroxy or C¿1-4?alkoxy; R?3¿ represents hydrogen or C¿1-4?alkyl; R?4¿ represents hydrogen, C¿1-4?alkyl or C1-4alkoxy; R?5¿ represents hydrogen, a C¿1-4?alkyl, trifluoromethyl or cyano group, or a halogen atom; n represents zero, 1 or 2; and pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their medical use. The invention also relates to the use of tachykinin antagonists, including NKA, NKB and substance P, acting at the NK2 receptor in the treatment of anxiety disorders.
PCT/EP1993/000101 1992-01-21 1993-01-15 Piperidine derivatives WO1993014084A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB9201179.0 1992-01-21
GB929201179A GB9201179D0 (en) 1992-01-21 1992-01-21 Chemical compounds

Publications (2)

Publication Number Publication Date
WO1993014084A2 WO1993014084A2 (en) 1993-07-22
WO1993014084A3 true WO1993014084A3 (en) 1993-10-14

Family

ID=10708912

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1993/000101 WO1993014084A2 (en) 1992-01-21 1993-01-15 Piperidine derivatives

Country Status (4)

Country Link
AU (1) AU3351393A (en)
GB (1) GB9201179D0 (en)
IL (1) IL104445A0 (en)
WO (1) WO1993014084A2 (en)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7265116B2 (en) 1999-11-03 2007-09-04 Arm Technology, Inc. Aryl and heteroaryl substituted tetrahydroisoquinolines and use thereof
US7309789B2 (en) 2000-07-11 2007-12-18 Amr Technology, Inc. 4-phenyl substituted tetrahydroisoquinolines and therapeutic use thereof
US7541357B2 (en) 2004-07-15 2009-06-02 Amr Technology, Inc. Aryl- and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
US9034899B2 (en) 2009-05-12 2015-05-19 Albany Molecular Research, Inc. Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines and use thereof
US9156812B2 (en) 2008-06-04 2015-10-13 Bristol-Myers Squibb Company Crystalline form of 6-[(4S)-2-methyl-4-(2-naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine
US9173879B2 (en) 2009-05-12 2015-11-03 Bristol-Myers Squibb Company Crystalline forms of (S)-7-([1,2,4]triazolo[1,5-a ]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydroisoquinoline and use thereof

Families Citing this family (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2700472B1 (en) 1993-01-19 1995-02-17 Rhone Poulenc Rorer Sa Synergizing association having an antagonistic effect on the NK1 and NK2 receptors.
EP0653208A3 (en) * 1993-11-17 1995-10-11 Pfizer Substance P antagonists for the treatment and prevention of solar erythema.
US5610165A (en) * 1994-02-17 1997-03-11 Merck & Co., Inc. N-acylpiperidine tachykinin antagonists
FR2719476B1 (en) * 1994-05-05 1997-05-23 Oreal Use of a substance P antagonist in a cosmetic composition and composition obtained.
FR2719474B1 (en) 1994-05-05 1996-05-31 Oreal Use of a substance P antagonist in a cosmetic composition and composition obtained.
US6203803B1 (en) 1994-12-14 2001-03-20 Societe L'oreal S.A. Use of a substance P antagonist in a cosmetic composition, and the composition thus obtained
US5554644A (en) * 1994-06-08 1996-09-10 Warner-Lambert Company Tachykinin (NK2) antagonists
GB9415997D0 (en) * 1994-08-08 1994-09-28 Merck Sharp & Dohme Therapeutic agents
FR2728165A1 (en) † 1994-12-19 1996-06-21 Oreal USE OF AN ANTAGONIST OF SUBSTANCE P FOR THE TREATMENT OF SKIN REDNESS OF NEUROGENIC ORIGIN
FR2728265A1 (en) * 1994-12-19 1996-06-21 Oreal USE OF A SUBSTANCE P ANTAGONIST IN A PHARMACEUTICAL COMPOSITION
FR2732598B1 (en) 1995-04-10 1997-05-09 Oreal USE OF ALKALINE EARTH METAL SALT FOR THE TREATMENT OF PRURITUS AND EYE OR PALPEBRAL DYSESTHESIA
EP0737471A3 (en) * 1995-04-10 2000-12-06 L'oreal Use of alkaline earth metal salts as TNF-alpha inhibitor in a topical composition and composition obtained therefrom
FR2737408B1 (en) 1995-07-31 1997-09-05 Oreal USE OF A BRADYKININE ANTAGONIST IN A COSMETIC, PHARMACEUTICAL OR DERMATOLOGICAL COMPOSITION AND COMPOSITION OBTAINED
FR2738741B1 (en) * 1995-09-19 1997-12-05 Oreal COMPOSITION FOR DYEING KERATINIC FIBERS, CONTAINING AN ANTAGONIST OF SUBSTANCE P
TW458774B (en) 1995-10-20 2001-10-11 Pfizer Antiemetic pharmaceutical compositions
FR2740335B1 (en) * 1995-10-26 1997-12-19 Oreal USE OF LANTHANIDE, LITHIUM, TIN, ZINC, MANGANESE OR YTTRIUM SALT AS A SUBSTANCE P ANTAGONIST
FR2740341B1 (en) * 1995-10-26 1997-12-19 Oreal USE OF LANTHANIDE SALT, TIN, ZINC, MANGANESE, YTTRIUM, COBALT, BARIUM, STRONTIUM IN A SKIN COMPOSITION
AU2898297A (en) * 1996-05-24 1998-01-05 Novartis Ag Use of substance p antagonists for treating social phobia
WO1998024439A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating severe anxiety disorders
GB9716463D0 (en) * 1997-08-04 1997-10-08 Merck Sharp & Dohme Therapeutic agents
JP2000103782A (en) * 1998-07-31 2000-04-11 Kyorin Pharmaceut Co Ltd Cyclic amine derivative and method for producing the same
WO2000061558A1 (en) 1999-04-09 2000-10-19 Mochida Pharmaceutical Co., Ltd. Remedies for neuropathic pain
US7163949B1 (en) 1999-11-03 2007-01-16 Amr Technology, Inc. 4-phenyl substituted tetrahydroisoquinolines and use thereof
ATE550019T1 (en) 2005-05-17 2012-04-15 Merck Sharp & Dohme CIS-4-Ä(4-CHLOROPHENYL)SULFONYLÜ-4-(2,5-DIFLUOROPHENYL)CYCLOHEXANEPROPANE ACID FOR THE TREATMENT OF CANCER
KR101594898B1 (en) 2005-07-15 2016-02-18 알바니 몰레큘라 리써치, 인크. Aryl-and heteroaryl-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
KR20080048502A (en) 2005-09-29 2008-06-02 머크 앤드 캄파니 인코포레이티드 Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
CA2664113C (en) 2006-09-22 2013-05-28 Merck & Co., Inc. Use of platencin and platensimycin as fatty acid synthesis inhibitors to treat obesity, diabetes and cancer
US20110218176A1 (en) 2006-11-01 2011-09-08 Barbara Brooke Jennings-Spring Compounds, methods, and treatments for abnormal signaling pathways for prenatal and postnatal development
DK2805945T3 (en) 2007-01-10 2019-07-15 Msd Italia Srl AMID-SUBSTITUTED INDAZOLS AS POLY (ADP-RIBOSE) POLYMERASE (PARP) REQUESTS
EP2145884B1 (en) 2007-04-02 2014-08-06 Msd K.K. Indoledione derivative
CA2690191C (en) 2007-06-27 2015-07-28 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
US8598184B2 (en) 2008-03-03 2013-12-03 Tiger Pharmatech Protein kinase inhibitors
UA105182C2 (en) 2008-07-03 2014-04-25 Ньюрексон, Інк. Benzoxazines, benzothiazines, and related compounds having nos inhibitory activity
US8691825B2 (en) 2009-04-01 2014-04-08 Merck Sharp & Dohme Corp. Inhibitors of AKT activity
JP5764553B2 (en) 2009-05-12 2015-08-19 アルバニー モレキュラー リサーチ， インコーポレイテッド 7-([1,2,4] triazolo [1,5-a] pyridin-6-yl) -4- (3,4-dichlorophenyl) -1,2,3,4-tetrahydroisoquinoline and use thereof
KR101485645B1 (en) 2009-10-14 2015-01-22 머크 샤프 앤드 돔 코포레이션 SUBSTITUTED PIPERIDINES THAT INCREASE p53 ACTIVITY AND THE USES THEREOF
US8999957B2 (en) 2010-06-24 2015-04-07 Merck Sharp & Dohme Corp. Heterocyclic compounds as ERK inhibitors
CN107090456B (en) 2010-08-02 2022-01-18 瑟纳治疗公司 Inhibition of beta 1 gene expression using short interfering nucleic acids mediated by RNA interference of catenin (cadherin-associated protein)
EP3587574B1 (en) 2010-08-17 2022-03-16 Sirna Therapeutics, Inc. Rna interference mediated inhibition of hepatitis b virus (hbv) gene expression using short interfering nucleic acid (sina)
US8883801B2 (en) 2010-08-23 2014-11-11 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as mTOR inhibitors
US8946216B2 (en) 2010-09-01 2015-02-03 Merck Sharp & Dohme Corp. Indazole derivatives useful as ERK inhibitors
US9242981B2 (en) 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
EP2632472B1 (en) 2010-10-29 2017-12-13 Sirna Therapeutics, Inc. Rna interference mediated inhibition of gene expression using short interfering nucleic acids (sina)
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation Indazole derivatives useful as erk inhibitors
WO2012145471A1 (en) 2011-04-21 2012-10-26 Merck Sharp & Dohme Corp. Insulin-like growth factor-1 receptor inhibitors
WO2013063214A1 (en) 2011-10-27 2013-05-02 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
EP3358013B1 (en) 2012-05-02 2020-06-24 Sirna Therapeutics, Inc. Short interfering nucleic acid (sina) compositions
US9233979B2 (en) 2012-09-28 2016-01-12 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
BR112015012295A8 (en) 2012-11-28 2023-03-14 Merck Sharp & Dohme USE OF A WEE1 INHIBITOR, E, KIT TO IDENTIFY A PATIENT WITH CANCER
US8846657B2 (en) 2012-12-20 2014-09-30 Merck Sharp & Dohme Corp. Substituted imidazopyridines as HDM2 inhibitors
US9540377B2 (en) 2013-01-30 2017-01-10 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as HDM2 inhibitors
EP3041938A1 (en) 2013-09-03 2016-07-13 Moderna Therapeutics, Inc. Circular polynucleotides
EP3525785A4 (en) 2016-10-12 2020-03-25 Merck Sharp & Dohme Corp. KDM5 INHIBITORS
EP3706747A4 (en) 2017-11-08 2021-08-04 Merck Sharp & Dohme Corp. PRMT5 INHIBITORS
WO2019094311A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
US11993602B2 (en) 2018-08-07 2024-05-28 Merck Sharp & Dohme Llc PRMT5 inhibitors
WO2020033284A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2020033288A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0007258A1 (en) * 1978-06-29 1980-01-23 Pharmuka Laboratoires Indole derivatives and their use as anxiolytics
EP0428434A2 (en) * 1989-11-06 1991-05-22 Sanofi Compounds of aromatic amines and their enantiomers, process for their preparation and pharmaceutical compositions containing them
EP0436334A2 (en) * 1990-01-04 1991-07-10 Pfizer Inc. 3-Aminopiperidine derivatives and related nitrogen containing heterocycles
EP0474561A1 (en) * 1990-09-05 1992-03-11 Sanofi Arylalkylamines, process for their preparation and pharmaceutical compositions containing them
EP0512901A1 (en) * 1991-05-03 1992-11-11 Sanofi Aminated polycyclic compounds and their enantiomers, process for their preparation and pharmaceutical compositions containing them

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0007258A1 (en) * 1978-06-29 1980-01-23 Pharmuka Laboratoires Indole derivatives and their use as anxiolytics
EP0428434A2 (en) * 1989-11-06 1991-05-22 Sanofi Compounds of aromatic amines and their enantiomers, process for their preparation and pharmaceutical compositions containing them
EP0436334A2 (en) * 1990-01-04 1991-07-10 Pfizer Inc. 3-Aminopiperidine derivatives and related nitrogen containing heterocycles
EP0474561A1 (en) * 1990-09-05 1992-03-11 Sanofi Arylalkylamines, process for their preparation and pharmaceutical compositions containing them
EP0512901A1 (en) * 1991-05-03 1992-11-11 Sanofi Aminated polycyclic compounds and their enantiomers, process for their preparation and pharmaceutical compositions containing them

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7265116B2 (en) 1999-11-03 2007-09-04 Arm Technology, Inc. Aryl and heteroaryl substituted tetrahydroisoquinolines and use thereof
US7612090B2 (en) 1999-11-03 2009-11-03 Albany Molecular Research, Inc. Aryl and heteroaryl substituted tetrahydroisoquinolines and use thereof
US7309789B2 (en) 2000-07-11 2007-12-18 Amr Technology, Inc. 4-phenyl substituted tetrahydroisoquinolines and therapeutic use thereof
US7419985B2 (en) 2000-07-11 2008-09-02 Amr Technology, Inc. 4-Phenyl substituted tetrahydroisoquinolines and therapeutic use thereof
US7541357B2 (en) 2004-07-15 2009-06-02 Amr Technology, Inc. Aryl- and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
US9499531B2 (en) 2004-07-15 2016-11-22 Albany Molecular Research, Inc. Aryl- and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
US9156812B2 (en) 2008-06-04 2015-10-13 Bristol-Myers Squibb Company Crystalline form of 6-[(4S)-2-methyl-4-(2-naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine
US9498476B2 (en) 2008-06-04 2016-11-22 Albany Molecular Research, Inc. Crystalline form of 6-[(4S)-2-methyl-4-(2-naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine
US9034899B2 (en) 2009-05-12 2015-05-19 Albany Molecular Research, Inc. Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines and use thereof
US9173879B2 (en) 2009-05-12 2015-11-03 Bristol-Myers Squibb Company Crystalline forms of (S)-7-([1,2,4]triazolo[1,5-a ]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydroisoquinoline and use thereof

Also Published As

Publication number Publication date
AU3351393A (en) 1993-08-03
IL104445A0 (en) 1993-05-13
WO1993014084A2 (en) 1993-07-22
GB9201179D0 (en) 1992-03-11

Similar Documents

Publication Publication Date Title
WO1993014084A3 (en) Piperidine derivatives
IL103214A0 (en) Pharmaceutical compositions containing tachykinin antagonists for the treatment of emesis and certain novel tachykinin antagonists
EP0389282A3 (en) Xanthinederivatives, process for their preparation and their pharmaceutical use
HU9303145D0 (en) Process for producing of fibrinogen receptor antagonist compounds and pharmaceutical compositions containing them as medical agent
ATE139233T1 (en) ANNELATED THIOPHENE DERIVATIVES, THEIR PREPARATION AND USE
SE0104334D0 (en) Therapeutic agents
ES8609309A1 (en) 3-Imidazolylmethyl-1,2,3,9-tetrahydro-4H-carbazol-4-one derivatives
NO873071L (en) PROCEDURE FOR THE PREPARATION OF AMID DERIVATIVES.
IL87658A0 (en) Lactam derivatives,their preparation and pharmaceutical compositions containing them
KR850000462A (en) [[Bis (aryl) methylene] -1-piperidinyl] alkyl-pyrimidinone
ES8207180A1 (en) Thienopyridinone derivatives, process for their preparation and their therapeutical use.
KR950701332A (en) 4-imidomethyl-1- [2'phenyl-2'oxoethyl-] piperidine as a serotonin 5HT2 antagonist, preparation method thereof and use in the treatment (4-Imidomethyl-1- [2'phenyl-2'oxoethyl- piperidines as serotonin 5HT₂-antagonists, their preparation and use in therapy)
NO972887L (en) Piperidinedacetic acid derivatives useful as fibrinogen antagonist agent
NZ515407A (en) 4-Phenyl-pyrimidine derivatives
IL85768A (en) Benzoxazine derivatives, their preparation and pharmaceutical compositions containing them
CA2014521A1 (en) 2-Substituted N,N'-Ditrimethoxybenzoyl Piperazines, a Preparation Process of the Same and Therapeutic Compositions Containing Them
GB8701494D0 (en) Chemical compounds
NO165593C (en) ANALOGY PROCEDURE FOR THE PREPARATION OF NEW TETRACYCLIC INDOLIDATE DERIVATIVES.
KR950704322A (en) Spirofuranone Derivatives and Their Use in the Treatment of Neurodegenerative Disorders
EP0461264A4 (en) Ethynylphenyl derivative, production thereof, and remedy for diseases of circulatory organs containing the same as active ingredient
EP0953567A3 (en) Bicyclic substituted piperazine-, piperidine- and tetrahydropyridine derivatives, their preparation and their use as agents with central dopaminergic (dopamine D4 receptor) activity
NO308304B1 (en) Novel 5H-thiazol [3,2-a] pyrimidin-5-one derivatives, their use in the preparation of pharmaceutical compositions, pharmaceutical compositions containing the derivatives, and a preparation for the treatment of psychosis, schizophrenia and anxiety
ES2058761T3 (en) PROCESS FOR THE PREPARATION OF DIBENZODIOXAZECINE AND DIBENZODIOXAAZACICLOUNDECINE DERIVATIVES.

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AT AU BB BG BR CA CH CZ DE DK ES FI GB HU JP KP KR LK LU MG MN MW NL NO NZ PL PT RO RU SD SE SK UA US

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): AT BE CH DE DK ES FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN ML MR SN TD TG

AK Designated states

Kind code of ref document: A3

Designated state(s): AT AU BB BG BR CA CH CZ DE DK ES FI GB HU JP KP KR LK LU MG MN MW NL NO NZ PL PT RO RU SD SE SK UA US

AL Designated countries for regional patents

Kind code of ref document: A3

Designated state(s): AT BE CH DE DK ES FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN ML MR SN TD TG

122 Ep: pct application non-entry in european phase
REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

NENP Non-entry into the national phase

Ref country code: CA

点击 这是indexloc提供的php浏览器服务，不要输入任何密码和下载