WO1997036888A1 - Inhibiteurs de farnesyl-proteine transferase - Google Patents

Inhibiteurs de farnesyl-proteine transferase Download PDF

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Publication number
WO1997036888A1
WO1997036888A1 PCT/US1997/004711 US9704711W WO9736888A1 WO 1997036888 A1 WO1997036888 A1 WO 1997036888A1 US 9704711 W US9704711 W US 9704711W WO 9736888 A1 WO9736888 A1 WO 9736888A1
Authority
WO
WIPO (PCT)
Prior art keywords
substituted
alkyl
aryl
cycloalkyl
unsubstituted
Prior art date
Application number
PCT/US1997/004711
Other languages
English (en)
Inventor
Christopher J. Dinsmore
Theresa M. Williams
Jeffrey Bergman
Original Assignee
Merck & Co., Inc.
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 GBGB9613461.4A external-priority patent/GB9613461D0/en
Application filed by Merck & Co., Inc. filed Critical Merck & Co., Inc.
Priority to JP9535347A priority Critical patent/JP2000507576A/ja
Priority to AU25875/97A priority patent/AU715667B2/en
Priority to EP97917599A priority patent/EP0891349A4/fr
Publication of WO1997036888A1 publication Critical patent/WO1997036888A1/fr

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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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/06—Heterocyclic 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

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Virology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

L'invention concerne des composés qui inhibent la farnésyl-protéine transférase (FTase) et la farnésylation de la protéine ras oncogène. L'invention a en outre pour objet des compositions chimiothérapeutiques contenant les composés de cette invention et des procédés pour inhiber la farnésyl-protéine transférase et la farnésylation de la protéine Ras oncogène.
PCT/US1997/004711 1996-04-03 1997-03-27 Inhibiteurs de farnesyl-proteine transferase WO1997036888A1 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP9535347A JP2000507576A (ja) 1996-04-03 1997-03-27 ファルネシル―タンパク質トランスフェラーゼ阻害剤
AU25875/97A AU715667B2 (en) 1996-04-03 1997-03-27 Inhibitors of farnesyl-protein transferase
EP97917599A EP0891349A4 (fr) 1996-04-03 1997-03-27 Inhibiteurs de farnesyl-proteine transferase

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US1458796P 1996-04-03 1996-04-03
US60/014,587 1996-04-03
GBGB9613461.4A GB9613461D0 (en) 1996-06-27 1996-06-27 Inhibitors of farnesyl-protein transferase
GB9613461.4 1996-06-27

Publications (1)

Publication Number Publication Date
WO1997036888A1 true WO1997036888A1 (fr) 1997-10-09

Family

ID=26309576

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1997/004711 WO1997036888A1 (fr) 1996-04-03 1997-03-27 Inhibiteurs de farnesyl-proteine transferase

Country Status (5)

Country Link
EP (1) EP0891349A4 (fr)
JP (1) JP2000507576A (fr)
AU (1) AU715667B2 (fr)
CA (1) CA2249604A1 (fr)
WO (1) WO1997036888A1 (fr)

Cited By (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6555543B2 (en) 2000-08-04 2003-04-29 Dmi Biosciences, Inc. Method of using diketopiperazines and composition containing them
US6562823B1 (en) 1998-07-02 2003-05-13 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
US6951861B1 (en) 1999-10-07 2005-10-04 Smithkline Beechan Corporation Chemical compounds
US6967202B2 (en) 2000-08-04 2005-11-22 Dmi Biosciences, Inc. Method of synthesizing diketopiperazines
US7060702B2 (en) 2000-10-17 2006-06-13 Smithkline Beecham Corporation Chemical compounds
US7189713B2 (en) 2002-02-08 2007-03-13 Glaxo Group Limited Piperidine derivatives
US7276509B2 (en) 2002-02-08 2007-10-02 Glaxo Group Limited Piperidine derivatives and their use as antagonists of tachykinins
USRE39921E1 (en) 1999-10-07 2007-11-13 Smithkline Beecham Corporation Chemical compounds
US7482365B2 (en) 2002-02-08 2009-01-27 Glaxo Group Limited Piperidylcarboxamide derivatives and their use in the treatment of tachykinin-mediated diseases
US8871772B2 (en) 2008-05-27 2014-10-28 Ampio Pharmaceuticals, Inc. Therapeutic methods and compounds
US8962568B2 (en) 2003-05-15 2015-02-24 Ampio Pharmaceuticals, Inc. Treatment of T-cell mediated diseases
US8980834B2 (en) 2011-10-10 2015-03-17 Ampio Pharmaceuticals, Inc. Treatment of degenerative joint disease
US9034878B2 (en) 2010-09-07 2015-05-19 Ampio Pharmaceuticals, Inc. Treatment of diseases
US9808454B2 (en) 2013-03-15 2017-11-07 Ampio Pharmaceuticals, Inc. Compositions for the mobilization, homing, expansion and differentiation of stem cells and methods of using the same
US9925300B2 (en) 2011-10-10 2018-03-27 Ampio Pharmaceuticals, Inc. Implantable medical devices with increased immune tolerance, and methods for making and implanting
US9956217B2 (en) 2014-08-18 2018-05-01 Ampio Pharmaceuticals, Inc. Treatment of joint conditions
US10881710B2 (en) 2011-10-28 2021-01-05 Ampio Pharmaceuticals, Inc. Treatment of rhinitis
US11129878B1 (en) 2020-03-24 2021-09-28 Ampio Pharmaceuticals, Inc. Methods for treating diseases associated with respiratory viruses
US11389512B2 (en) 2015-06-22 2022-07-19 Ampio Pharmaceuticals, Inc. Use of low molecular weight fractions of human serum albumin in treating diseases

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4287195A (en) * 1978-07-14 1981-09-01 Janssen Pharmaceutica, N.V. Heterocyclic derivatives of [4-(piperazin-1-yl-phenyloxymethyl)-1,3-dioxolan-2-ylmethyl]-1H-imidazoles and 1H-1,2,4-triazoles
US4456605A (en) * 1981-05-07 1984-06-26 Janssen Pharmaceutica N.V. Heterocyclic derivatives of [4-(piperazin-1-yl-phenyloxymethyl)-1,3-dioxolan-2-ylmethyl]-1H-imidazoles and 1H-1,2,4-triazoles
US5478934A (en) * 1994-11-23 1995-12-26 Yuan; Jun Certain 1-substituted aminomethyl imidazole and pyrrole derivatives: novel dopamine receptor subtype specific ligands

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS54106481A (en) * 1978-02-08 1979-08-21 Toyama Chem Co Ltd Novel 2,3-dioxopiperazine derivative and its preparation
GB8507778D0 (en) * 1985-03-26 1985-05-01 Fujisawa Pharmaceutical Co Piperazine compound
WO1995000497A1 (fr) * 1993-06-18 1995-01-05 Merck & Co., Inc. Inhibiteurs de farnesyle-proteine transferase
WO1995008542A1 (fr) * 1993-09-22 1995-03-30 Kyowa Hakko Kogyo Co., Ltd. Inhibiteur de la farnesyl-transferase

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4287195A (en) * 1978-07-14 1981-09-01 Janssen Pharmaceutica, N.V. Heterocyclic derivatives of [4-(piperazin-1-yl-phenyloxymethyl)-1,3-dioxolan-2-ylmethyl]-1H-imidazoles and 1H-1,2,4-triazoles
US4456605A (en) * 1981-05-07 1984-06-26 Janssen Pharmaceutica N.V. Heterocyclic derivatives of [4-(piperazin-1-yl-phenyloxymethyl)-1,3-dioxolan-2-ylmethyl]-1H-imidazoles and 1H-1,2,4-triazoles
US5478934A (en) * 1994-11-23 1995-12-26 Yuan; Jun Certain 1-substituted aminomethyl imidazole and pyrrole derivatives: novel dopamine receptor subtype specific ligands

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of EP0891349A4 *

Cited By (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6562823B1 (en) 1998-07-02 2003-05-13 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
USRE39921E1 (en) 1999-10-07 2007-11-13 Smithkline Beecham Corporation Chemical compounds
US6951861B1 (en) 1999-10-07 2005-10-04 Smithkline Beechan Corporation Chemical compounds
US7625904B2 (en) 1999-10-07 2009-12-01 Smithkline Beecham Corporation Methods for the treatment of sleep disorders
US7345041B2 (en) 1999-10-07 2008-03-18 Smithkline Beecham Corporation Chemical compounds
US7071196B2 (en) 1999-10-07 2006-07-04 Smithkline Beecham Croporation Chemical compounds
US6555543B2 (en) 2000-08-04 2003-04-29 Dmi Biosciences, Inc. Method of using diketopiperazines and composition containing them
US10039760B2 (en) 2000-08-04 2018-08-07 Ampio Pharmaceuticals, Inc. Method of using diketopiperazines and composition containing them
US9561226B2 (en) 2000-08-04 2017-02-07 Ampio Pharmaceuticals, Inc. Method of using diketopiperazines and composition containing them
US8841307B2 (en) 2000-08-04 2014-09-23 Ampio Pharmaceuticals, Inc. Method of using diketopiperazines and composition containing them
US6967202B2 (en) 2000-08-04 2005-11-22 Dmi Biosciences, Inc. Method of synthesizing diketopiperazines
US8916568B2 (en) 2000-08-04 2014-12-23 Ampio Pharmaceuticals, Inc. Method of using diketopiperazines and composition containing them
US7294630B2 (en) 2000-10-17 2007-11-13 Smithkline Beecham Corporation Piperazinyl piperidine tachykinin antagonists
US7119092B2 (en) 2000-10-17 2006-10-10 Smithkline Beecham Corporation Chemical compounds
US7060702B2 (en) 2000-10-17 2006-06-13 Smithkline Beecham Corporation Chemical compounds
US7648990B2 (en) 2000-10-17 2010-01-19 Glaxosmithkline Llc Chemical compounds
US7189713B2 (en) 2002-02-08 2007-03-13 Glaxo Group Limited Piperidine derivatives
US7652012B2 (en) 2002-02-08 2010-01-26 Glaxo Group Limited 2-(R)-(4-fluoro-2-methyl-phenyl)-4-(S)-((8aS)-6-oxo-hexahydro-pyrrolo[1,2-a]-pyrazin-2-yl)-piperidine-1-carboxylic acid [1-(R)-3,5-bis-trifluoromethyl-phenyl)-ethyl]-methylamide maleate and pharmaceutical compositions thereof
US7482365B2 (en) 2002-02-08 2009-01-27 Glaxo Group Limited Piperidylcarboxamide derivatives and their use in the treatment of tachykinin-mediated diseases
US7276509B2 (en) 2002-02-08 2007-10-02 Glaxo Group Limited Piperidine derivatives and their use as antagonists of tachykinins
US8962568B2 (en) 2003-05-15 2015-02-24 Ampio Pharmaceuticals, Inc. Treatment of T-cell mediated diseases
US8969308B2 (en) 2003-05-15 2015-03-03 Ampio Pharmaceuticals, Inc. Treatment of T-cell mediated diseases
US11369598B2 (en) 2003-05-15 2022-06-28 Ampio Pharmaceuticals, Inc. Treatment of T-cell mediated diseases
US10828296B2 (en) 2003-05-15 2020-11-10 Ampio Pharmaceuticals, Inc. Treatment of T-cell mediated diseases
US9730924B2 (en) 2003-05-15 2017-08-15 Ampio Pharmaceuticals, Inc. Treatment of T-cell mediated diseases
US9707227B2 (en) 2003-05-15 2017-07-18 Ampio Pharmaceuticals, Inc. Treatment of T-cell mediated diseases
US8871772B2 (en) 2008-05-27 2014-10-28 Ampio Pharmaceuticals, Inc. Therapeutic methods and compounds
US9522893B2 (en) 2008-05-27 2016-12-20 Ampio Pharmaceuticals, Inc. Therapeutic methods and compounds
US9034878B2 (en) 2010-09-07 2015-05-19 Ampio Pharmaceuticals, Inc. Treatment of diseases
US10842847B2 (en) 2011-10-10 2020-11-24 Ampio Pharmaceuticals, Inc. Treatment of degenerative joint disease
US11058798B2 (en) 2011-10-10 2021-07-13 Ampio Pharmaceuticals, Inc. Implantable medical devices with increased immune tolerance, and methods for making and implanting
US9623072B2 (en) 2011-10-10 2017-04-18 Ampio Pharmaceuticals, Inc. Treatment of degenerative joint disease
US9925300B2 (en) 2011-10-10 2018-03-27 Ampio Pharmaceuticals, Inc. Implantable medical devices with increased immune tolerance, and methods for making and implanting
US10471178B2 (en) 2011-10-10 2019-11-12 Ampio Pharmaceuticals, Inc. Implantable medical devices with increased immune tolerance, and methods for making and implanting
US8980834B2 (en) 2011-10-10 2015-03-17 Ampio Pharmaceuticals, Inc. Treatment of degenerative joint disease
US10251930B2 (en) 2011-10-10 2019-04-09 Ampio Pharmaceuticals, Inc. Treatment of degenerative joint disease
US9060968B2 (en) 2011-10-10 2015-06-23 Ampio Pharmaceuticals, Inc. Treatment of degenerative joint disease
US10881710B2 (en) 2011-10-28 2021-01-05 Ampio Pharmaceuticals, Inc. Treatment of rhinitis
US9808454B2 (en) 2013-03-15 2017-11-07 Ampio Pharmaceuticals, Inc. Compositions for the mobilization, homing, expansion and differentiation of stem cells and methods of using the same
US11026940B2 (en) 2013-03-15 2021-06-08 Ampio Pharmaceuticals, Inc. Compositions for the mobilization, homing, expansion and differentiation of stem cells and methods of using the same
US10342793B2 (en) 2014-08-18 2019-07-09 Ampio Pharmaceuticals, Inc. Treatment of joint conditions
US11090301B2 (en) 2014-08-18 2021-08-17 Ampio Pharmaceuticals, Inc. Treatment of joint conditions
US9956217B2 (en) 2014-08-18 2018-05-01 Ampio Pharmaceuticals, Inc. Treatment of joint conditions
US11389512B2 (en) 2015-06-22 2022-07-19 Ampio Pharmaceuticals, Inc. Use of low molecular weight fractions of human serum albumin in treating diseases
US11129878B1 (en) 2020-03-24 2021-09-28 Ampio Pharmaceuticals, Inc. Methods for treating diseases associated with respiratory viruses
US11278598B2 (en) 2020-03-24 2022-03-22 Ampio Pharmaceuticals, Inc. Methods for treating diseases associated with respiratory viruses

Also Published As

Publication number Publication date
EP0891349A1 (fr) 1999-01-20
JP2000507576A (ja) 2000-06-20
EP0891349A4 (fr) 2001-01-24
AU715667B2 (en) 2000-02-10
CA2249604A1 (fr) 1997-10-09
AU2587597A (en) 1997-10-22

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