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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English (en)
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CA2293706A1 (fr
Inventor
Stacy Remiszewski
Alan K. Mallams
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Merck Sharp and Dohme LLC
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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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material 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)
  • Plural Heterocyclic 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 (38)

* 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
EP1322334A2 (fr) * 2000-10-05 2003-07-02 George Q. Daley Methodes d'induction de l'apoptose de cellules cancereuses et de la regression de tumeurs
US20020077301A1 (en) * 2000-10-05 2002-06-20 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
CA2904393A1 (fr) * 2013-03-15 2014-09-25 Araxes Pharma Llc Inhibiteurs covalents de k-ras g12c
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
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
ES2898765T3 (es) 2015-04-10 2022-03-08 Araxes Pharma Llc Compuestos de quinazolina sustituidos y métodos de uso de los mismos
US10428064B2 (en) 2015-04-15 2019-10-01 Araxes Pharma Llc Fused-tricyclic inhibitors of KRAS and methods of use thereof
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
EP3356351A1 (fr) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibiteurs de protéines kras portant la mutation g12c
WO2017058728A1 (fr) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibiteurs de protéines kras portant la mutation g12c
WO2017058805A1 (fr) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibiteurs de protéines kras portant la mutation g12c
WO2017058902A1 (fr) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibiteurs de protéines mutantes kras g12c
EP3356359B1 (fr) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibiteurs de protéines kras portant la mutation g12c
EP3356347A1 (fr) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibiteurs de protéines kras portant la mutation g12c
WO2017070256A2 (fr) 2015-10-19 2017-04-27 Araxes Pharma Llc Méthode de criblage d'inhibiteurs de ras
KR20180081596A (ko) 2015-11-16 2018-07-16 아락세스 파마 엘엘씨 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법
US9988357B2 (en) 2015-12-09 2018-06-05 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
WO2017172979A1 (fr) 2016-03-30 2017-10-05 Araxes Pharma Llc Composés quinazoline substitués et procédés d'utilisation
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
WO2018064510A1 (fr) 2016-09-29 2018-04-05 Araxes Pharma Llc Inhibiteurs de protéines mutantes kras g12c
EP3523289A1 (fr) 2016-10-07 2019-08-14 Araxes Pharma LLC Composés hétérocycliques en tant qu'inhibiteurs de ras et leurs procédés d'utilisation
WO2018140513A1 (fr) 2017-01-26 2018-08-02 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
JP7327802B2 (ja) 2017-01-26 2023-08-16 アラクセス ファーマ エルエルシー 縮合ヘテロ－ヘテロ二環式化合物およびその使用方法
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
WO2018140599A1 (fr) 2017-01-26 2018-08-02 Araxes Pharma Llc Composés à base de benzothiophène et de benzothiazole et leurs procédés d'utilisation
EP3573954A1 (fr) 2017-01-26 2019-12-04 Araxes Pharma LLC Composés benzohétéroaromatiques bicycliques fusionnés et leurs procédés d'utilisation
CN110869357A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 化合物及其用于治疗癌症的使用方法
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
US10745385B2 (en) 2017-05-25 2020-08-18 Araxes Pharma Llc Covalent inhibitors of KRAS
MX2021000887A (es) 2018-08-01 2021-03-31 Araxes Pharma Llc Compuestos espiroheterociclicos y metodos de uso de los mismos para el tratamiento de cancer.
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
JP2001500508A (ja) * 1996-09-13 2001-01-16 シェーリング コーポレイション ファルネシルタンパク質トランスフェラーゼの阻害に有用な置換ベンゾシクロヘプタピリジン誘導体
ES2234036T3 (es) * 1996-09-13 2005-06-16 Schering Corporation Compuestos utiles para inhibir la farnesil-protein-transferasa.

Also Published As

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

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