CA2362495A1 - Inhibiteurs de prenyl-proteine transferases - Google Patents

Inhibiteurs de prenyl-proteine transferases Download PDF

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Publication number
CA2362495A1
CA2362495A1 CA002362495A CA2362495A CA2362495A1 CA 2362495 A1 CA2362495 A1 CA 2362495A1 CA 002362495 A CA002362495 A CA 002362495A CA 2362495 A CA2362495 A CA 2362495A CA 2362495 A1 CA2362495 A1 CA 2362495A1
Authority
CA
Canada
Prior art keywords
alkyl
substituted
aryl
unsubstituted
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
CA002362495A
Other languages
English (en)
Inventor
Theresa M. Williams
Craig A. Stump
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
Application filed by Individual filed Critical Individual
Publication of CA2362495A1 publication Critical patent/CA2362495A1/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
    • C07D233/64—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
    • 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
    • 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
    • A61P31/12—Antivirals
    • 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
    • A61P31/14—Antivirals for RNA viruses
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

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

Abstract

La présente invention concerne des composés contenant de la pipérazine et inhibant des prényl-protéine transférases. L'invention concerne en particulier des inhibiteurs de prényl-protéine transférases efficaces in vivo comme inhibiteurs de géranylgéranyl-protéine transférases de type I (GGTase-I) et inhibant le traitement cellulaire de la protéine H-Ras et de la protéine K4B-Ras. Ces composés thérapeutiques s'utilisent pour le traitement du cancer.
CA002362495A 1999-03-03 2000-03-01 Inhibiteurs de prenyl-proteine transferases Abandoned CA2362495A1 (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US12297199P 1999-03-03 1999-03-03
US60/122,971 1999-03-03
US12725299P 1999-03-31 1999-03-31
US60/127,252 1999-03-31
PCT/US2000/005354 WO2000051614A1 (fr) 1999-03-03 2000-03-01 Inhibiteurs de prenyl-proteine transferases

Publications (1)

Publication Number Publication Date
CA2362495A1 true CA2362495A1 (fr) 2000-09-08

Family

ID=26821069

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002362495A Abandoned CA2362495A1 (fr) 1999-03-03 2000-03-01 Inhibiteurs de prenyl-proteine transferases

Country Status (5)

Country Link
EP (1) EP1165084A4 (fr)
JP (1) JP2002538121A (fr)
AU (1) AU3248600A (fr)
CA (1) CA2362495A1 (fr)
WO (1) WO2000051614A1 (fr)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10035927A1 (de) 2000-07-21 2002-03-07 Asta Medica Ag Neue Heteroaryl-Derivate und deren Verwendung als Arzneimittel
DE10035928A1 (de) 2000-07-21 2002-03-07 Asta Medica Ag Neue Heteroaryl-Derivate und deren Verwendung als Arzneimittel
UA79286C2 (en) * 2002-06-29 2007-06-11 Zentaris Gmbh Arylcarbonylpipererazines and heteroarylcarbonylpiperazines and their use in the treatment of benign and malignant tumors
SG10202003901UA (en) 2005-12-13 2020-05-28 Incyte Holdings Corp Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
JP2010502664A (ja) 2006-09-11 2010-01-28 ノバルティス アクチエンゲゼルシャフト 代謝型グルタミン酸受容体の調節剤としてのニコチン酸誘導体
KR20150036210A (ko) 2007-06-13 2015-04-07 인사이트 코포레이션 야누스 키나제 억제제（Ｒ）―３―（４―（７Ｈ―피롤로［２，３－ｄ］피리미딘―4―일）―1Ｈ―피라졸―1―일）―３―사이클로펜틸프로판니트릴의 염
AR076794A1 (es) 2009-05-22 2011-07-06 Incyte Corp Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen
SI2432472T1 (sl) 2009-05-22 2019-11-29 Incyte Holdings Corp 3-(4-(7H-pirolo(2,3-d)pirimidin-4-il)-1H-pirazol-1-il)oktan- ali heptan-nitril kot inhibitorji JAK
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
WO2011103091A1 (fr) 2010-02-18 2011-08-25 Transtech Pharma, Inc. Dérivés de phényl-hétéroaryle et procédés d'utilisation de ceux-ci
EP3354652B1 (fr) 2010-03-10 2020-05-06 Incyte Holdings Corporation Dérivés de pipéridine-4-yl azétidine utilisés en tant qu'inhibiteurs de jak1
PE20130216A1 (es) 2010-05-21 2013-02-27 Incyte Corp Formulacion topica para un inhibidor de jak
WO2011153359A1 (fr) 2010-06-04 2011-12-08 Albany Molecular Research, Inc. Inhibiteurs du transporteur 1 de la glycine, procédés de fabrication associés, et utilisations associées
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
PE20140146A1 (es) 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
CN103797010B (zh) 2011-06-20 2016-02-24 因塞特控股公司 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物
US8921533B2 (en) 2011-07-25 2014-12-30 Chromatin Technologies Glycosylated valproic acid analogs and uses thereof
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
PH12020551186B1 (en) 2012-11-15 2024-03-20 Incyte Holdings Corp Sustained-release dosage forms of ruxolitinib
RS62867B1 (sr) 2013-03-06 2022-02-28 Incyte Holdings Corp Postupci i intermedijeri za dobijanje inhibitora jak
SMT202000315T1 (it) 2013-08-07 2020-07-08 Incyte Corp Forme di dosaggio a rilascio prolungato per un inibitore di jak1
WO2015070367A1 (fr) * 2013-11-12 2015-05-21 Merck Sharp & Dohme Corp. Dérivés d'imidazole et de triazole liés à la pipéridine ou la pipérazine et leurs procédés d'utilisation pour améliorer la pharmacocinétique d'un médicament
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
US10196383B2 (en) 2015-07-17 2019-02-05 Sunshine Lake Pharma Co., Ltd. Substituted quinazoline compounds and preparation and uses thereof
KR20200066690A (ko) 2017-10-16 2020-06-10 칭화대학교 메발로네이트 경로 억제제 및 이의 약제학적 조성물
WO2019113487A1 (fr) 2017-12-08 2019-06-13 Incyte Corporation Polythérapie à faible dose pour le traitement de néoplasmes myéloprolifératifs
SG11202007164UA (en) 2018-01-30 2020-08-28 Incyte Corp Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
SMT202400306T1 (it) 2018-03-30 2024-09-16 Incyte Corp Trattamento dell'idrosadenite suppurativa utilizzando inibitori di jak.
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4093726A (en) * 1976-12-02 1978-06-06 Abbott Laboratories N-(2-benzimidazolyl)-piperazines
US4159331A (en) * 1978-05-05 1979-06-26 The Upjohn Company Antihypertensive 4-aminoquinolines
JPS57106663A (en) * 1980-12-23 1982-07-02 Kyorin Pharmaceut Co Ltd 1,4-disubstituted piperazine derivative and its preparation
IT1176613B (it) * 1984-08-14 1987-08-18 Ravizza Spa Derivati piperazinici farmacologicamente attivi e processo per la loro preparazione
JPH0696555B2 (ja) * 1986-07-31 1994-11-30 大塚製薬株式会社 カルボスチリル誘導体
JPS63183565A (ja) * 1986-09-24 1988-07-28 Ss Pharmaceut Co Ltd イミダゾ−ル誘導体
JPH01132579A (ja) * 1987-11-19 1989-05-25 Ss Pharmaceut Co Ltd インドール誘導体
GB9013750D0 (en) * 1990-06-20 1990-08-08 Pfizer Ltd Therapeutic agents
US5856326A (en) * 1995-03-29 1999-01-05 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase

Also Published As

Publication number Publication date
EP1165084A1 (fr) 2002-01-02
JP2002538121A (ja) 2002-11-12
EP1165084A4 (fr) 2002-05-15
WO2000051614A1 (fr) 2000-09-08
AU3248600A (en) 2000-09-21

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Legal Events

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