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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

Links

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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (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
US12725299P 1999-03-31 1999-03-31
US60/122,971 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
WO2004002965A1 (fr) * 2002-06-29 2004-01-08 Zentaris Gmbh Aryl- et heteroarylcarbonylpiperazines et leur utilisation dans le traitement de maladies tumorales benignes et malignes
PL2455382T3 (pl) 2005-12-13 2017-04-28 Incyte Holdings Corporation Podstawione heteroarylem pirolo[2,3-b]pirydyny i pirolo[2,3-b]pirymidyny jako inhibitory kinazy Janusowej
US20100041641A1 (en) 2006-09-11 2010-02-18 Glatthar Ralf Uses of metabotropic glutamate receptors
DK3070090T3 (en) 2007-06-13 2019-03-18 Incyte Holdings Corp USE OF SALTS OF THE JANUS-KINASE INHIBITOR (R) -3- (4- (7H-PYRROLO [2,3-D] PYRIMIDIN-4-YL) -1H-PYRAZOL-1-YL) -3- CYCLOPENTYL PROPANNITRIL
EA025520B1 (ru) 2009-05-22 2017-01-30 Инсайт Холдингс Корпорейшн N-(ГЕТЕРО)АРИЛПИРРОЛИДИНОВЫЕ ПРОИЗВОДНЫЕ ПИРАЗОЛ-4-ИЛ-ПИРРОЛО[2,3-d]ПИРИМИДИНОВ И ПИРРОЛ-3-ИЛ-ПИРРОЛО[2,3-d]ПИРИМИДИНОВ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ
UA106078C2 (uk) 2009-05-22 2014-07-25 Інсайт Корпорейшн 3-[4-(7H-ПІРОЛО[2,3-d]ПІРИМІДИН-4-ІЛ)-1H-ПІРАЗОЛ-1-ІЛ]ОКТАН- АБО ГЕПТАННІТРИЛ ЯК JAK-ІНГІБІТОРИ
AR078012A1 (es) 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
TWI510241B (zh) 2010-02-18 2015-12-01 Vtv Therapeutice Llc 苯基－雜芳基衍生物及其使用方法
KR20180117206A (ko) 2010-03-10 2018-10-26 인사이트 홀딩스 코포레이션 Ｊａｋ１ 저해제로서의 피페리딘­４­일 아제티딘 유도체
EA202091303A3 (ru) 2010-05-21 2021-05-31 Инсайт Холдингс Корпорейшн Композиция ингибитора jak для местного применения
AU2011261375B2 (en) 2010-06-04 2016-09-22 Albany Molecular Research, Inc. Glycine transporter-1 inhibitors, methods of making them, and uses thereof
WO2012068440A1 (fr) 2010-11-19 2012-05-24 Incyte Corporation Pyrrolopyridines et pyrrolopyrimidines à substitution hétérocyclique utilisées en tant qu'inhibiteurs des jak
UA113156C2 (xx) 2010-11-19 2016-12-26 Циклобутилзаміщені похідні піролопіридину й піролопіримідину як інгібітори jak
EA201490042A1 (ru) 2011-06-20 2014-10-30 Инсайт Корпорейшн Азетидинил-фенил-, пиридил- или пиразинилкарбоксамидные производные как ингибиторы jak
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
AR091079A1 (es) 2012-05-18 2014-12-30 Incyte Corp Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak
LT2919766T (lt) 2012-11-15 2021-09-27 Incyte Holdings Corporation Ruksolitinibo pailginto atpalaidavimo vaisto formos
UA120162C2 (uk) 2013-03-06 2019-10-25 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки при отриманні інгібітора jak
IL277554B2 (en) 2013-08-07 2024-03-01 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
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
WO2017012502A1 (fr) 2015-07-17 2017-01-26 Sunshine Lake Pharma Co., Ltd. Composés de quinazoline substitués, ainsi que préparation et utilisations de ceux-ci
CN111225672B (zh) 2017-10-16 2023-09-29 清华大学 甲羟戊酸通路抑制剂及其药物组合物
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
CA3089832A1 (fr) 2018-01-30 2019-08-08 Incyte Corporation Procedes de preparation de (1-(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
SI3773593T1 (sl) 2018-03-30 2024-08-30 Incyte Corporation Zdravljenje hidradenitisa suppurative z zaviralci 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
WO2000051614A1 (fr) 2000-09-08
JP2002538121A (ja) 2002-11-12
AU3248600A (en) 2000-09-21
EP1165084A4 (fr) 2002-05-15
EP1165084A1 (fr) 2002-01-02

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