CA2249607A1 - Inhibiteurs de transferase de farnesyl-proteine - Google Patents

Inhibiteurs de transferase de farnesyl-proteine Download PDF

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Publication number
CA2249607A1
CA2249607A1 CA002249607A CA2249607A CA2249607A1 CA 2249607 A1 CA2249607 A1 CA 2249607A1 CA 002249607 A CA002249607 A CA 002249607A CA 2249607 A CA2249607 A CA 2249607A CA 2249607 A1 CA2249607 A1 CA 2249607A1
Authority
CA
Canada
Prior art keywords
substituted
alkyl
unsubstituted
aryl
hydrogen
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.)
Abandoned
Application number
CA002249607A
Other languages
English (en)
Inventor
Neville J. Anthony
Robert P. Gomez
Samuel L. Graham
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.)
Merck and Co Inc
Original Assignee
Individual
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 GBGB9613462.2A external-priority patent/GB9613462D0/en
Priority claimed from GBGB9617277.0A external-priority patent/GB9617277D0/en
Application filed by Individual filed Critical Individual
Publication of CA2249607A1 publication Critical patent/CA2249607A1/fr
Abandoned legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring 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
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/70—One oxygen atom
    • 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
    • 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
    • C07D403/10—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 aromatic rings
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/06—Heterocyclic 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 only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical 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)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Cette invention concerne des composés permettant d'inhiber la transférase de farnésyl-protéine (FTase), ainsi que la farnésylation de la protéine oncogène Ras. Cette invention concerne également des compositions chimiothérapeutiques contenant les composés susmentionnés, ainsi que des procédés permettant d'inhiber la transférase de farnésyl-protéine et la farnésylation de la protéine oncogène Ras.
CA002249607A 1996-04-03 1997-04-01 Inhibiteurs de transferase de farnesyl-proteine Abandoned CA2249607A1 (fr)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US1459296P 1996-04-03 1996-04-03
US60/014,592 1996-04-03
GBGB9613462.2A GB9613462D0 (en) 1996-06-27 1996-06-27 Inhibitors of farnesyl-protein transferase
GB9613462.2 1996-06-27
US2264796P 1996-07-24 1996-07-24
US60/022,647 1996-07-24
GB9617277.0 1996-08-16
GBGB9617277.0A GB9617277D0 (en) 1996-08-16 1996-08-16 Inhibitors of farnesyl-protein transferase

Publications (1)

Publication Number Publication Date
CA2249607A1 true CA2249607A1 (fr) 1997-10-09

Family

ID=27451473

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002249607A Abandoned CA2249607A1 (fr) 1996-04-03 1997-04-01 Inhibiteurs de transferase de farnesyl-proteine

Country Status (5)

Country Link
EP (1) EP0891361A1 (fr)
JP (1) JP2000507590A (fr)
AU (1) AU706150B2 (fr)
CA (1) CA2249607A1 (fr)
WO (1) WO1997036901A1 (fr)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6015817A (en) * 1996-12-05 2000-01-18 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5939439A (en) * 1996-12-30 1999-08-17 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US6093737A (en) * 1996-12-30 2000-07-25 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US6127390A (en) * 1997-10-02 2000-10-03 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
PL340729A1 (en) 1997-11-28 2001-02-26 Lg Chemical Ltd Imidazolic derivatives exhibiting inhibitive activity in respect to pharnesil transferase and method of obtaining them
EP1045843A4 (fr) * 1997-12-04 2001-10-24 Merck & Co Inc Inhibiteurs de la farnesyl-proteine transferase
US6420555B1 (en) 1998-06-16 2002-07-16 Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. Imidazolyl derivatives
ES2216535T3 (es) * 1998-06-16 2004-10-16 Societe De Conseils De Recherches Et D'applications Scientifiques S.A.S. Derivados de imidazolilo.
US6511978B1 (en) * 1999-04-13 2003-01-28 Lg Life Sciences, Ltd. Pyrrole derivatives useful for farnesyl transferase inhibitors and their preparations
EP1420015A1 (fr) * 1999-06-11 2004-05-19 Societe De Conseils De Recherches Et D'applications Scientifiques S.A.S. Dérivés de l'imidazole
CA2413245A1 (fr) 2000-06-30 2002-01-10 Bristol-Myers Squibb Pharma Company N-ureidoheterocycloaklyl-piperidines utilises comme modulateurs de l'activite du recepteur de la chimiokine
US7211595B2 (en) 2000-11-30 2007-05-01 Abbott Laboratories Farnesyltransferase inhibitors
US20020115640A1 (en) * 2000-11-30 2002-08-22 Claiborne Akiyo K. Farnesyltransferase inhibitors
JP2006502107A (ja) 2002-07-02 2006-01-19 エフ．ホフマン−ラ　ロシュ　アーゲー Ｃｃｒ−３レセプターアンタゴニストｉｘとしての２，５−置換ピリミジン誘導体
MX2007000885A (es) 2004-07-23 2007-03-12 Pfizer Derivados de piridina.
EP2129660A2 (fr) 2006-12-19 2009-12-09 Pfizer Products Inc. Dérivés de nicotinamide en tant qu'inhibiteurs de h-pgds et leur utilisation pour le traitement de maladies liées aux prostaglandines d2
UY30892A1 (es) 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
JP2010519328A (ja) 2007-02-26 2010-06-03 ファイザー・プロダクツ・インク Ｈ−ｐｇｄｓの阻害剤としてのニコチンアミド誘導体およびプロスタグランジンｄ２が媒介する疾患の治療のためのそれらの使用
JP2010532381A (ja) 2007-06-29 2010-10-07 サネシス ファーマシューティカルズ， インコーポレイテッド Ｒａｆキナーゼ阻害剤として有用な複素環式化合物
CL2008001933A1 (es) 2007-06-29 2009-09-25 Millennium Pharm Inc Compuestos derivados de pirimidina, inhibidores de la raf quinasa; compuestos intermediarios; procedimiento de preparacion; composicion farmaceutica; y su uso para tratar trastornos proliferativos, cardiacos, neurodegenerativos, inflamatorios, oseos, inmunologicos enfermedad viral, entre otros.
PE20110843A1 (es) 2008-09-22 2011-12-08 Cayman Chem Co Derivados de 5-(1h-imidazol-5-il)-2-fenilpirimidina, como inhibidores de prostaglandina d sintasa hematopoyetica
EP2414344A1 (fr) 2009-03-31 2012-02-08 ArQule, Inc. Composés indolo-pyridinone substitués
EP2730561B1 (fr) * 2010-04-06 2015-10-14 Nippon Soda Co., Ltd. Méthodes de préparation de composés hétérocycliques haloalkylés contenant de l'azote
AU2014201038B2 (en) * 2010-04-06 2015-08-06 Nippon Soda Co., Ltd. Nitrogen-containing heterocyclic compound and method for producing same
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
BR112016007467B1 (pt) 2013-10-04 2022-09-20 Infinity Pharmaceuticals, Inc Compostos heterocíclicos e usos dos mesmos
WO2015051241A1 (fr) 2013-10-04 2015-04-09 Infinity Pharmaceuticals, Inc. Composés hétérocycliques et leurs utilisations
JP6701088B2 (ja) 2014-03-19 2020-05-27 インフィニティー ファーマシューティカルズ， インコーポレイテッド Ｐｉ３ｋ−ガンマ媒介障害の治療で使用するための複素環式化合物
US9975874B2 (en) 2014-07-28 2018-05-22 Merck Sharp & Dohme Corp. Factor XIa inhibitors
WO2016054491A1 (fr) 2014-10-03 2016-04-07 Infinity Pharmaceuticals, Inc. Composés hétérocycliques et leurs utilisations
EP3319968A1 (fr) 2015-07-06 2018-05-16 Rodin Therapeutics, Inc. N-aminophényl-amides hétérocycliques en tant qu'inhibiteurs de l'histone désacétylase
RS62639B1 (sr) 2015-07-06 2021-12-31 Alkermes Inc Hetero-halo inhibitori histonskih deacetilaza
EP3350183A1 (fr) 2015-09-14 2018-07-25 Infinity Pharmaceuticals, Inc. Formes solides de dérivés d'isoquinolinone, leur procédé de fabrication, compositions les comprenant et méthodes d'utilisation de celles-ci
WO2017161116A1 (fr) 2016-03-17 2017-09-21 Infinity Pharmaceuticals, Inc. Isotopologues de composés isoquinolinone et quinazolinone et leurs utilisations comme inhibiteurs de la kinase pi3k
US10919914B2 (en) 2016-06-08 2021-02-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
MA47305A (fr) 2017-01-11 2019-11-27 Rodin Therapeutics Inc Inhibiteurs bicycliques d'histone désacétylase
EP3664802B1 (fr) 2017-08-07 2022-02-23 Alkermes, Inc. Inhibiteurs bicycliques de la histone déacétylase

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GB2162513B (en) * 1984-06-25 1988-01-20 Toyama Chemical Co Ltd Dihydropyridine derivatives
US5633376A (en) * 1990-12-28 1997-05-27 Neurogen Corporation Certain aminomethyl phenylimidazole derivatives; and 4-aryl substituted piperazinyl and piperidinylmethyl phenylimidazole derivatives; a new class of dopamine receptor subtype ligands
US5159083A (en) * 1990-12-28 1992-10-27 Neurogen Corporation Certain aminomethyl phenylimidazole derivatives; a class of dopamine receptor subtype specific ligands
IT1255802B (it) * 1992-08-07 1995-11-16 Luso Farmaco Inst Derivati imidazolici ad attivita' a ii antagonista

Also Published As

Publication number Publication date
EP0891361A1 (fr) 1999-01-20
JP2000507590A (ja) 2000-06-20
AU706150B2 (en) 1999-06-10
AU2430197A (en) 1997-10-22
WO1997036901A1 (fr) 1997-10-09

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