CA2293706C - Nouveaux composes d'uree n-substitues inhibiteurs de la farnesyl transferase - Google Patents

Nouveaux composes d'uree n-substitues inhibiteurs de la farnesyl transferase Download PDF

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Publication number
CA2293706C
CA2293706C CA002293706A CA2293706A CA2293706C CA 2293706 C CA2293706 C CA 2293706C CA 002293706 A CA002293706 A CA 002293706A CA 2293706 A CA2293706 A CA 2293706A CA 2293706 C CA2293706 C CA 2293706C
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CA
Canada
Prior art keywords
aryl
compound
alkyl
heterocycloalkyl
hydrogen
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Expired - Fee Related
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CA002293706A
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CA2293706A1 (fr
Inventor
Stacy Remiszewski
Alan K. Mallams
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Merck Sharp and Dohme Corp
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Schering Corp
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Publication of CA2293706C publication Critical patent/CA2293706C/fr
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    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D401/14—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 three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Abstract

La présente invention concerne de nouveaux composés d'urée halogéno N-substitués et des compositions pharmaceutiquement acceptables de formules (1.0) ainsi que leurs sels ou solvates pharmaceutiquement acceptables, qui sont des inhibiteurs de l'enzyme farnésyl transférase. La présente invention concerne également une méthode d'inhibition de la fonction Ras et donc de la croissance anormale des cellules. Cete méthode, qui consiste à administrer le nouveau composé d'urée halogéno N-substitué à un système biologique permet notamment d'inhiber la croissance anormale des cellules chez des mammifères tel que l'homme.
CA002293706A 1997-06-17 1998-06-15 Nouveaux composes d'uree n-substitues inhibiteurs de la farnesyl transferase Expired - Fee Related CA2293706C (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US87704997A 1997-06-17 1997-06-17
US08/877,049 1997-06-17
PCT/US1998/011507 WO1998057948A1 (fr) 1997-06-17 1998-06-15 Nouveaux composes d'uree n-substitues inhibiteurs de la farnesyl transferase

Publications (2)

Publication Number Publication Date
CA2293706A1 CA2293706A1 (fr) 1998-12-23
CA2293706C true CA2293706C (fr) 2008-11-18

Family

ID=25369144

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002293706A Expired - Fee Related CA2293706C (fr) 1997-06-17 1998-06-15 Nouveaux composes d'uree n-substitues inhibiteurs de la farnesyl transferase

Country Status (14)

Country Link
EP (1) EP0989979A1 (fr)
JP (1) JP2002506444A (fr)
KR (1) KR20010013881A (fr)
CN (1) CN1267291A (fr)
AR (1) AR013094A1 (fr)
AU (1) AU8253598A (fr)
CA (1) CA2293706C (fr)
CO (1) CO4940458A1 (fr)
HU (1) HUP0002954A3 (fr)
IL (1) IL133389A0 (fr)
NZ (1) NZ501571A (fr)
PE (1) PE82799A1 (fr)
WO (1) WO1998057948A1 (fr)
ZA (1) ZA985205B (fr)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7342016B2 (en) 2000-08-30 2008-03-11 Schering Corporation Farnesyl protein transferase inhibitors as antitumor agents
HUP0302913A3 (en) * 2000-10-05 2005-05-30 Daley George Q Weston Methods of inducing cancer cell death and tumor regression and preparation of pharmaceutical compositions suitable for treating the same
AU2002211427A1 (en) * 2000-10-05 2002-04-15 Whitehead Institute For Biomedical Research Effects of combined administration of farnesyl transferase inhibitors and signal transduction inhibitors
EP1695961A4 (fr) * 2003-12-17 2007-10-24 Takeda Pharmaceutical Derives d'uree, processus de production correspondant et utilisation
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
TW201524952A (zh) * 2013-03-15 2015-07-01 Araxes Pharma Llc Ｋｒａｓ ｇ１２ｃ之共價抑制劑
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Ｋｒａｓ ｇ１２ｃ之抑制劑
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
JP2017528498A (ja) 2014-09-25 2017-09-28 アラクセス ファーマ エルエルシー Ｋｒａｓ ｇ１２ｃ変異体タンパク質のインヒビター
WO2016049568A1 (fr) 2014-09-25 2016-03-31 Araxes Pharma Llc Méthodes et compositions permettant l'inhibition de la ras
US10246424B2 (en) 2015-04-10 2019-04-02 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
ES2856880T3 (es) 2015-04-15 2021-09-28 Araxes Pharma Llc Inhibidores tricíclicos condensados de KRAS y métodos de uso de los mismos
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
EP3356349A1 (fr) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibiteurs de protéines mutantes kras g12c
US10689356B2 (en) 2015-09-28 2020-06-23 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10647703B2 (en) 2015-09-28 2020-05-12 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10858343B2 (en) 2015-09-28 2020-12-08 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10875842B2 (en) 2015-09-28 2020-12-29 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3356359B1 (fr) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibiteurs de protéines kras portant la mutation g12c
US10730867B2 (en) 2015-09-28 2020-08-04 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3364977A4 (fr) 2015-10-19 2019-09-04 Araxes Pharma LLC Méthode de criblage d'inhibiteurs de ras
US10414757B2 (en) 2015-11-16 2019-09-17 Araxes Pharma Llc 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
US9988357B2 (en) 2015-12-09 2018-06-05 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
US10822312B2 (en) 2016-03-30 2020-11-03 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
EP3519402A1 (fr) 2016-09-29 2019-08-07 Araxes Pharma LLC Inhibiteurs de protéines mutantes kras g12c
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
EP3573964A1 (fr) 2017-01-26 2019-12-04 Araxes Pharma LLC Composés à base de benzothiophène et de benzothiazole et leurs procédés d'utilisation
WO2018140512A1 (fr) 2017-01-26 2018-08-02 Araxes Pharma Llc Composés benzohétéroaromatiques bicycliques fusionnés et leurs procédés d'utilisation
EP3573970A1 (fr) 2017-01-26 2019-12-04 Araxes Pharma LLC Dérivés de 1-(6-(3-hydroxynaphtalen-1-yl)quinazolin-2-yl)azétidin-1-yl)prop-2-en-1-one et composés similaires utilisés en tant qu'inhibiteurs de kras g12c pour le traitement du cancer
EP3573971A1 (fr) 2017-01-26 2019-12-04 Araxes Pharma LLC Dérivés de 1-(3-(6-(3-hydroxynaphtalen-1-yl)benzofuran-2-yl)azétidin-1yl)prop-2-en-1-one et composés similaires utilisés en tant que modulateurs de kras g12c pour le traitement du cancer
EP3573967A1 (fr) 2017-01-26 2019-12-04 Araxes Pharma LLC Composés hétéro-hétéro-bicycliques fusionnés et leurs procédés d'utilisation
JP2020521741A (ja) 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー がんの処置のための化合物およびその使用の方法
WO2018218069A1 (fr) 2017-05-25 2018-11-29 Araxes Pharma Llc Dérivés de quinazoline utilisés en tant que modulateurs de kras, hras ou nras mutants
CA3063440A1 (fr) 2017-05-25 2018-11-29 Araxes Pharma Llc Inhibiteurs covalents de kras
CN111960990A (zh) * 2020-07-23 2020-11-20 宿迁联盛科技股份有限公司 一种助剂及其制备方法

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL111235A (en) * 1993-10-15 2001-03-19 Schering Plough Corp Medicinal preparations for inhibiting protein G activity and for the treatment of malignant diseases, containing tricyclic compounds, some such new compounds and a process for the preparation of some of them
US5719148A (en) * 1993-10-15 1998-02-17 Schering Corporation Tricyclic amide and urea compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
IL117798A (en) * 1995-04-07 2001-11-25 Schering Plough Corp Tricyclic compounds useful for inhibiting the function of protein - G and for the treatment of malignant diseases, and pharmaceutical preparations containing them
IL125062A (en) * 1995-12-22 2003-11-23 Schering Corp Tricyclic amides and pharmaceutical compositions containing them for inhibition of g-protein function and for treatment of proliferative diseases
ES2234036T3 (es) * 1996-09-13 2005-06-16 Schering Corporation Compuestos utiles para inhibir la farnesil-protein-transferasa.
CZ87499A3 (cs) * 1996-09-13 1999-08-11 Schering Corporation Substituované deriváty benzocykloheptapyridinu použitelné při léčbě nádorových onemocnění tím, že inhibují farnesylprotein transferázu

Also Published As

Publication number Publication date
AU8253598A (en) 1999-01-04
IL133389A0 (en) 2001-04-30
JP2002506444A (ja) 2002-02-26
WO1998057948A1 (fr) 1998-12-23
CO4940458A1 (es) 2000-07-24
CA2293706A1 (fr) 1998-12-23
PE82799A1 (es) 1999-08-26
HUP0002954A2 (hu) 2001-06-28
CN1267291A (zh) 2000-09-20
NZ501571A (en) 2002-02-01
ZA985205B (en) 1998-12-15
KR20010013881A (ko) 2001-02-26
EP0989979A1 (fr) 2000-04-05
AR013094A1 (es) 2000-12-13
HUP0002954A3 (en) 2002-11-28

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