CA2585490A1 - Composes heteroaromatiques de l'azote qui se lient au site actif d'enzymes de type proteines kinases - Google Patents

Composes heteroaromatiques de l'azote qui se lient au site actif d'enzymes de type proteines kinases Download PDF

Info

Publication number
CA2585490A1
CA2585490A1 CA002585490A CA2585490A CA2585490A1 CA 2585490 A1 CA2585490 A1 CA 2585490A1 CA 002585490 A CA002585490 A CA 002585490A CA 2585490 A CA2585490 A CA 2585490A CA 2585490 A1 CA2585490 A1 CA 2585490A1
Authority
CA
Canada
Prior art keywords
alkyl
aryl
heteroaryl
alkoxy
nr4r5
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
CA002585490A
Other languages
English (en)
Inventor
Veronique Birault
Jose Antonio Bravo
Roger Crossley
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.)
Galapagos NV
Original Assignee
Galapagos Nv
Veronique Birault
Jose Antonio Bravo
Roger Crossley
Biofocus Discovery Limited
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 GB0425026A external-priority patent/GB0425026D0/en
Application filed by Galapagos Nv, Veronique Birault, Jose Antonio Bravo, Roger Crossley, Biofocus Discovery Limited filed Critical Galapagos Nv
Publication of CA2585490A1 publication Critical patent/CA2585490A1/fr
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • 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
    • C07D401/14—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
    • 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
    • C07D405/14—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 three or more hetero rings
CA002585490A 2004-11-12 2005-11-11 Composes heteroaromatiques de l'azote qui se lient au site actif d'enzymes de type proteines kinases Abandoned CA2585490A1 (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GB0425026.2 2004-11-12
GB0425026A GB0425026D0 (en) 2004-11-12 2004-11-12 Compounds which bind to the active site of protein kinase enzymes
GB0500245.6 2005-01-07
GBGB0500245.6A GB0500245D0 (en) 2004-11-12 2005-01-07 Compounds which bind to the active site of protein kinase enzymes
PCT/GB2005/004358 WO2006051311A1 (fr) 2004-11-12 2005-11-11 Composés hétéroaromatiques de l'azote qui se lient au site actif d'enzymes de type protéines kinases

Publications (1)

Publication Number Publication Date
CA2585490A1 true CA2585490A1 (fr) 2006-05-18

Family

ID=35788166

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002585490A Abandoned CA2585490A1 (fr) 2004-11-12 2005-11-11 Composes heteroaromatiques de l'azote qui se lient au site actif d'enzymes de type proteines kinases

Country Status (4)

Country Link
EP (1) EP1814856A1 (fr)
JP (1) JP2008519814A (fr)
CA (1) CA2585490A1 (fr)
WO (1) WO2006051311A1 (fr)

Families Citing this family (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1922306A2 (fr) * 2005-09-02 2008-05-21 Astellas Pharma Inc. Dérivés d'amides comme inhibiteurs rock
WO2008022164A2 (fr) * 2006-08-16 2008-02-21 Boehringer Ingelheim International Gmbh Composés de pyrazine, leur utilisation et procédés de préparation
US8071779B2 (en) * 2006-12-18 2011-12-06 Inspire Pharmaceuticals, Inc. Cytoskeletal active rho kinase inhibitor compounds, composition and use
BRPI0810202A2 (pt) 2007-05-03 2014-10-21 Pfizer Ltd Derivados de piridina
PL2190825T3 (pl) 2007-08-22 2014-09-30 Novartis Ag Związki 5-(4-(chlorowcoalkoksy)-fenylo)-pirymidyno-2-aminowe i kompozycje jako inhibitory kinazy
TWI504395B (zh) 2009-03-10 2015-10-21 Substituted 3-amino-2-mercaptoquinoline as a KCNQ2 / 3 modifier
TWI461197B (zh) 2009-03-12 2014-11-21 2-mercaptoquinoline-3-carboxamide as a KCNQ2 / 3 modifier
TWI475020B (zh) 2009-03-12 2015-03-01 The substituted nicotine amide as a KCNQ2 / 3 modifier
TW201038565A (en) 2009-03-12 2010-11-01 Gruenenthal Gmbh Substituted 2-mercapto-3-aminopyridines as KCNQ2/3 modulators
ES2459468T3 (es) * 2009-05-15 2014-05-09 Novartis Ag Arilpiridinas como inhibidores de aldosterona sintasa
US10253020B2 (en) 2009-06-12 2019-04-09 Abivax Compounds for preventing, inhibiting, or treating cancer, AIDS and/or premature aging
BR122019013687B1 (pt) * 2009-06-12 2020-04-14 Abivax composto de fórmula (i)
CN102822150B (zh) 2010-02-05 2014-12-03 赫普泰雅治疗有限公司 1,2,4-三嗪-4-胺衍生物
JP5605727B2 (ja) * 2010-04-06 2014-10-15 Ｊｎｃ株式会社 セレンテラジン類縁体及びセレンテラミド類縁体
US8653101B2 (en) 2010-08-27 2014-02-18 Gruenenthal Gmbh Substituted 2-oxy-quinoline-3-carboxamides as KCNQ2/3 modulators
BR112013004690A2 (pt) 2010-08-27 2016-05-10 Gruenenthal Gmbh 2-oxo-e 2-tioxo-di-hidroquinolina-3-carboxamidas substituídas como moduladores kcnq2/3
US8470852B2 (en) 2010-08-27 2013-06-25 Gruenenthal Gmbh Substituted 2-amino-quinoline-3-carboxamides as KCNQ2/3 modulators
CA2807886A1 (fr) 2010-09-01 2012-03-08 Gruenenthal Gmbh 1-oxo-dihydroisoquinoline-3-carboxamides substitues en tant que modulateurs des kcnq2/3
CA2816679A1 (fr) * 2010-11-17 2012-05-24 Novartis Ag Composes 3-(aminoaryl)-pyridine
US9458147B2 (en) 2012-02-22 2016-10-04 Sanford-Burnham Medical Research Institute Sulfonamide compounds and uses as TNAP inhibitors
EP2757161A1 (fr) 2013-01-17 2014-07-23 Splicos miRNA-124 comme biomarqueur de l'infection virale
KR102177199B1 (ko) 2013-04-24 2020-11-10 고쿠리쓰다이가쿠호진 규슈다이가쿠 안저질환 치료제
MY182908A (en) 2014-01-14 2021-02-05 Millennium Pharm Inc Heteroaryls and uses thereof
EP3094326A4 (fr) 2014-01-14 2017-07-26 Millennium Pharmaceuticals, Inc. Hétéroaryles et utilisations de ceux-ci
EP2974729A1 (fr) 2014-07-17 2016-01-20 Abivax Dérivés de quinoléine utilisés dans le traitement de maladies inflammatoires
US10421756B2 (en) 2015-07-06 2019-09-24 Rodin Therapeutics, Inc. Heterobicyclic N-aminophenyl-amides as inhibitors of histone deacetylase
SI3319959T1 (sl) 2015-07-06 2022-02-28 Alkermes, Inc. Hetero-halo inhibitorji histonske deacetilaze
EP4088719A1 (fr) 2015-10-13 2022-11-16 Institut National de la Santé et de la Recherche Médicale (INSERM) Procédés et compositions pharmaceutiques pour le traitement de non-perfusion capillaire rétinienne
US20180296474A1 (en) 2015-10-13 2018-10-18 INSERM (Institut National de la Santé et de la Recherche Médicale Methods and pharmaceutical compositions for the treatment of retinal capillary non-perfusion
JP6946412B2 (ja) 2016-07-18 2021-10-06 ヤンセン ファーマシューティカ エヌ．ベー． タウｐｅｔ画像化リガンド
MD3570834T2 (ro) 2017-01-11 2022-04-30 Alkermes Inc Inhibitori biciclici ai histon deacetilazei
MA49839B1 (fr) 2017-08-07 2022-05-31 Alkermes Inc Inhibiteurs bicycliques de la histone déacétylase
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
SG11202107615TA (en) 2019-01-18 2021-08-30 Astrazeneca Ab Pcsk9 inhibitors and methods of use thereof
US11384083B2 (en) 2019-02-15 2022-07-12 Incyte Corporation Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
US11472791B2 (en) 2019-03-05 2022-10-18 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as CDK2 inhibitors
US11919904B2 (en) 2019-03-29 2024-03-05 Incyte Corporation Sulfonylamide compounds as CDK2 inhibitors
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
KR20220064369A (ko) 2019-08-14 2022-05-18 인사이트 코포레이션 Cdk2 저해제로서의 이미다졸릴 피리디미딘일아민 화합물
CA3157681A1 (fr) 2019-10-11 2021-04-15 Incyte Corporation Amines bicycliques utilisees en tant qu'inhibiteurs de cdk2

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU779908B2 (en) * 1999-09-10 2005-02-17 Merck & Co., Inc. Tyrosine kinase inhibitors
DE60136731D1 (de) * 2000-09-20 2009-01-08 Ortho Mcneil Pharm Inc Pyrazine derivate als tyrosin kinase modulatoren
GB2392154B (en) * 2002-05-23 2005-01-19 Cytopia Pty Ltd Protein Kinase Inhibitors
WO2005003101A2 (fr) * 2003-07-02 2005-01-13 Biofocus Discovery Limited Composes se liant au site actif d'enzymes proteine kinases

Also Published As

Publication number Publication date
JP2008519814A (ja) 2008-06-12
EP1814856A1 (fr) 2007-08-08
WO2006051311A1 (fr) 2006-05-18

Similar Documents

Publication Publication Date Title
CA2585490A1 (fr) Composes heteroaromatiques de l'azote qui se lient au site actif d'enzymes de type proteines kinases
US20080194584A1 (en) Nitrogen Heteroaromatic Compounds Which Bind To The Active Site Of Protein Kinase Enzymes
WO2005003101A2 (fr) Composes se liant au site actif d'enzymes proteine kinases
TWI377198B (en) Novel pyridine derivatives and pyrimidine derivatives (3)
TWI338684B (en) Tetrahydroquinoline derivatives and a process for preparing the same
US20060199821A1 (en) Heterocyclic amides and sulfonamides
TW201704237A (zh) 適用於治療與ｋｉｔ及ｐｄｆｇｒ相關之病症的組合物
TW200526635A (en) Hydroxypyrimidinone derivative having HIV integrase inhibitory activity
KR20070026357A (ko) 인돌 유도체, 및 키나제 억제제, 특히 ｉｋｋ2억제제로서의 그의 용도
KR20130109943A (ko) 항암 및 항증식 활성을 나타내는 시클로프로필 디카르복사미드 및 유사체
JP7195436B2 (ja) バニン阻害剤としての複素芳香族化合物
JP5412430B2 (ja) ｍＧｌｕ５拮抗薬としての新規複素環系化合物
WO2018121650A1 (fr) Inhibiteur de fgfr
Hobson et al. Identification of selective dual ROCK1 and ROCK2 inhibitors using structure-based drug design
CN111620878A (zh) 吡咯并嘧啶类衍生物作为蛋白激酶抑制剂及其应用
AU758246B2 (en) N,N-substituted cyclic amine derivatives
WO2006072792A2 (fr) Composes se liant au site actif des proteines kinases
SK6862003A3 (en) Guanidine and amidine derivatives as factor XA inhibitors, process for the preparation thereof, pharmaceutical composition and use thereof
EP2733144B1 (fr) Nouveau composé ayant une activité d'inhibition de parp
US20090163515A1 (en) Compounds Which Bind to the Active Site of Protein Kinase Enzymes
KR100791693B1 (ko) 항혈전제 및 항응고제로서의 ｎ-(헤테로시클릴)벤젠 또는피리딘 술폰아미드
TW201619134A (zh) 取代苯基化合物
US11078161B2 (en) Rock-inhibiting compound and uses thereof
AU2004218180B2 (en) Novel aminopyridine derivatives as mGluR5 antagonists
WO2003082263A1 (fr) Acides sulfamiques utilises comme inhibiteurs de proteines tyrosines phosphatases cytoplasmiques humaines

Legal Events

Date Code Title Description
FZDE Dead