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WO1993014084A3 - Piperidine derivatives - Google Patents

Piperidine derivatives Download PDF

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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
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/EP1993/000101
Other languages
French (fr)
Other versions
WO1993014084A2 (en
Inventor
Anthony William James Cooper
Russell Michael Hagan
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Glaxo Group Ltd
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
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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

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  • 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 Ceased WO1993014084A2 (en)

Applications Claiming Priority (2)

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

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 Ceased 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 (7)

* 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
US9403776B2 (en) 2005-07-15 2016-08-02 Albany Molecular Research, Inc. Aryl- and heteroaryl-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin

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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
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
FR2719476B1 (en) * 1994-05-05 1997-05-23 Oreal Use of a substance P antagonist in a cosmetic composition and composition 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
FR2740341B1 (en) * 1995-10-26 1997-12-19 Oreal USE OF LANTHANIDE SALT, TIN, ZINC, MANGANESE, YTTRIUM, COBALT, BARIUM, STRONTIUM IN A SKIN COMPOSITION
FR2740335B1 (en) * 1995-10-26 1997-12-19 Oreal USE OF LANTHANIDE, LITHIUM, TIN, ZINC, MANGANESE OR YTTRIUM SALT AS A SUBSTANCE P ANTAGONIST
WO1997045119A1 (en) * 1996-05-24 1997-12-04 Novartis Ag Use of substance p antagonists for treating social phobia
JP2001504848A (en) * 1996-12-02 2001-04-10 メルク シヤープ エンド ドーム リミテツド Use of an NK-1 receptor antagonist for the treatment of severe anxiety disorder
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
EP1182193A4 (en) * 1999-04-09 2002-09-11 Mochida Pharm Co Ltd Remedies for neuropathic pain
US7163949B1 (en) 1999-11-03 2007-01-16 Amr Technology, Inc. 4-phenyl substituted tetrahydroisoquinolines and use thereof
ES2382814T3 (en) 2005-05-17 2012-06-13 Merck Sharp & Dohme Ltd. Cis-4 - [(4-chlorophenyl) sulfonyl] -4- (2,5-difluorophenyl) cyclohexanopropanoic acid for cancer treatment
CN101277960A (en) 2005-09-29 2008-10-01 默克公司 Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
WO2008039327A2 (en) 2006-09-22 2008-04-03 Merck & Co., Inc. Method of treatment using fatty acid synthesis inhibitors
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
CA2682727C (en) 2007-04-02 2016-03-22 Banyu Pharmaceutical Co., Ltd. Indoledione derivative
WO2009002495A1 (en) 2007-06-27 2008-12-31 Merck & Co., Inc. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
CN102014631A (en) 2008-03-03 2011-04-13 泰格尔医药科技公司 Tyrosine kinase inhibitors
UA105182C2 (en) 2008-07-03 2014-04-25 Ньюрексон, Інк. Benzoxazines, benzothiazines, and related compounds having nos inhibitory activity
EP2413932A4 (en) 2009-04-01 2012-09-19 Merck Sharp & Dohme INHIBITORS OF AKT ACTIVITY
AU2010247763B2 (en) 2009-05-12 2015-12-24 Albany Molecular Research, Inc. 7-([1,2,4,]triazolo[1,5,-a]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4- tetrahydroisoquinoline and use thereof
US8859776B2 (en) 2009-10-14 2014-10-14 Merck Sharp & Dohme Corp. 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
EP3330377A1 (en) 2010-08-02 2018-06-06 Sirna Therapeutics, Inc. Rna interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (ctnnb1) gene expression using short interfering nucleic acid (sina)
EP4079856A1 (en) 2010-08-17 2022-10-26 Sirna Therapeutics, Inc. Rna interference mediated inhibition of hepatitis b virus (hbv) gene expression using short interfering nucleic acid (sina)
EP2608669B1 (en) 2010-08-23 2016-06-22 Merck Sharp & Dohme Corp. NOVEL PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
WO2012030685A2 (en) 2010-09-01 2012-03-08 Schering Corporation 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
EP3766975A1 (en) 2010-10-29 2021-01-20 Sirna Therapeutics, Inc. Rna interference mediated inhibition of gene expression using short interfering nucleic acid (sina)
US9351965B2 (en) 2010-12-21 2016-05-31 Merck Sharp & Dohme Corp. Indazole derivatives useful as ERK inhibitors
CA2831730A1 (en) 2011-04-21 2012-10-26 Piramal Enterprises Limited A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation
US9023865B2 (en) 2011-10-27 2015-05-05 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
EP3919620A1 (en) 2012-05-02 2021-12-08 Sirna Therapeutics, Inc. Short interfering nucleic acid (sina) compositions
CA2882950A1 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
ME02925B (en) 2012-11-28 2018-04-20 Merck Sharp & Dohme COMPOSITIONS AND METHOD FOR THE TREATMENT OF CANCER
AU2013361694B2 (en) 2012-12-20 2017-10-26 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
WO2018071283A1 (en) 2016-10-12 2018-04-19 Merck Sharp & Dohme Corp. Kdm5 inhibitors
WO2019094312A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2019094311A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
EP3833667B1 (en) 2018-08-07 2024-03-13 Merck Sharp & Dohme LLC Prmt5 inhibitors
EP3833668B1 (en) 2018-08-07 2025-03-19 Merck Sharp & Dohme LLC Prmt5 inhibitors
US12173026B2 (en) 2018-08-07 2024-12-24 Merck Sharp & Dohme Llc 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 (11)

* 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
US9403776B2 (en) 2005-07-15 2016-08-02 Albany Molecular Research, Inc. Aryl- and heteroaryl-substituted tetrahydrobenzazepines 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
WO1993014084A2 (en) 1993-07-22
IL104445A0 (en) 1993-05-13
AU3351393A (en) 1993-08-03
GB9201179D0 (en) 1992-03-11

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