EA201100426A1 - Бициклические ингибиторы киназы - Google Patents

Бициклические ингибиторы киназы

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Publication number
EA201100426A1
EA201100426A1 EA201100426A EA201100426A EA201100426A1 EA 201100426 A1 EA201100426 A1 EA 201100426A1 EA 201100426 A EA201100426 A EA 201100426A EA 201100426 A EA201100426 A EA 201100426A EA 201100426 A1 EA201100426 A1 EA 201100426A1
Authority
EA
Eurasian Patent Office
Prior art keywords
kinase
compositions
kinase inhibitors
inhibiting
activity
Prior art date
Application number
EA201100426A
Other languages
English (en)
Inventor
Маттью Бергер
Мика Линдвалль
Original Assignee
Новартис Аг
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 Новартис Аг filed Critical Новартис Аг
Publication of EA201100426A1 publication Critical patent/EA201100426A1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Abstract

Описаны новые соединения, композиции и способы ингибирования активности провирусной интеграции киназы Maloney (киназы PIM), связанной с опухолегенезом у человека или животного. В некоторых вариантах осуществления соединения и композиции эффективны для ингибирования активности по крайней мере одной киназы PIM. Новые соединения и композиции могут использоваться отдельно или в комбинации по крайней мере с одним дополнительным агентом для лечения нарушений, опосредованных серин/треонинкиназой или рецепторной тирозинкиназой, таких как рак.
EA201100426A 2008-09-02 2009-08-31 Бициклические ингибиторы киназы EA201100426A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US9366908P 2008-09-02 2008-09-02
PCT/EP2009/061182 WO2010026121A1 (en) 2008-09-02 2009-08-31 Bicyclic kinase inhibitors

Publications (1)

Publication Number Publication Date
EA201100426A1 true EA201100426A1 (ru) 2011-10-31

Family

ID=41211220

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201100426A EA201100426A1 (ru) 2008-09-02 2009-08-31 Бициклические ингибиторы киназы

Country Status (11)

Country Link
US (1) US8735424B2 (ru)
EP (1) EP2342190A1 (ru)
JP (1) JP5564045B2 (ru)
KR (1) KR20110058866A (ru)
CN (1) CN102203075B (ru)
AU (1) AU2009289316A1 (ru)
BR (1) BRPI0918496A2 (ru)
CA (1) CA2735779A1 (ru)
EA (1) EA201100426A1 (ru)
MX (1) MX2011002367A (ru)
WO (1) WO2010026121A1 (ru)

Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007070514A1 (en) 2005-12-13 2007-06-21 Incyte Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
RS58449B1 (sr) 2007-06-13 2019-04-30 Incyte Holdings Corp Upotreba soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h- pirazol-1-il)-3-ciklopentilpropionitrila
AU2010249380B2 (en) 2009-05-22 2015-08-20 Incyte Holdings Corporation N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as Janus kinase inhibitors
EP3643312A1 (en) 2009-05-22 2020-04-29 Incyte Holdings Corporation 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
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
CN102985417B (zh) 2010-03-10 2015-01-28 因塞特公司 作为jak1抑制剂的哌啶-4-基氮杂环丁烷衍生物
EA035981B1 (ru) 2010-05-21 2020-09-09 Инсайт Холдингс Корпорейшн Композиция ингибитора jak для местного применения
TW201249845A (en) 2010-11-19 2012-12-16 Incyte Corp Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
EP2640725B1 (en) 2010-11-19 2015-01-07 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
WO2012177606A1 (en) 2011-06-20 2012-12-27 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
PL3409278T3 (pl) 2011-07-21 2021-02-22 Sumitomo Pharma Oncology, Inc. Heterocykliczne inhibitory kinazy białkowej
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
CN113384545A (zh) 2012-11-15 2021-09-14 因赛特公司 鲁索利替尼的缓释剂型
CA2897200C (en) 2013-01-14 2021-07-06 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors
US9200004B2 (en) 2013-01-15 2015-12-01 Incyte Holdings Corporation Thiazolecarboxamides and pyridinecarboxamide compounds useful as Pim kinase inhibitors
JP6307096B2 (ja) 2013-01-23 2018-04-04 アストラゼネカ アクチボラグ 化合物
SI3489239T1 (sl) 2013-03-06 2022-04-29 Incyte Holdings Corporation Postopki in intermediati za pripravo zaviralca JAK
EA201690357A1 (ru) 2013-08-07 2016-07-29 Инсайт Корпорейшн Лекарственные формы с замедленным высвобождением для ингибитора jak1
SG11201601259YA (en) 2013-08-23 2016-03-30 Incyte Corp Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors
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
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
US9822124B2 (en) 2014-07-14 2017-11-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors
TWI700283B (zh) * 2014-08-04 2020-08-01 德商拜耳製藥公司 2-(嗎啉-4-基)-1,7-萘啶
USD816841S1 (en) 2014-12-15 2018-05-01 Jjgc Industria E Comercio De Materiais Dentarios S/A Bone implant
WO2016196244A1 (en) 2015-05-29 2016-12-08 Incyte Corporation Pyridineamine compounds useful as pim kinase inhibitors
WO2017019723A1 (en) 2015-07-29 2017-02-02 Merck Sharp & Dohme Corp. Aza-cyanoquinolinone pde9 inhibitors
US10370336B2 (en) 2015-07-29 2019-08-06 Merck Sharp & Dohme Corp. Phenyl-cyanoquinolinone PDE9 inhibitors
US10370337B2 (en) 2015-07-29 2019-08-06 Merck, Sharp & Dohme Corp. Oxy-cyanoquinolinone PDE9 inhibitors
TWI734699B (zh) 2015-09-09 2021-08-01 美商英塞特公司 Pim激酶抑制劑之鹽
US9920032B2 (en) 2015-10-02 2018-03-20 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
NZ742476A (en) * 2015-12-17 2022-09-30 Merck Patent Gmbh Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders
KR20210134838A (ko) 2016-07-14 2021-11-10 크리네틱스 파마슈티칼스, 인크. 소마토스타틴 조절제 및 그의 용도
CN105974036A (zh) * 2016-07-31 2016-09-28 合肥远志医药科技开发有限公司 一种氨基吡啶异构体的检测方法
BR112019000696A2 (pt) 2016-08-08 2019-04-24 Merck Patent Gmbh antagonistas de tlr7/8 e uso dos mesmos
US10596161B2 (en) 2017-12-08 2020-03-24 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
SI3746429T1 (sl) 2018-01-30 2023-01-31 Incyte Corporation Postopki za pripravo (1-(3-fluoro-2-(trifluorometil)izonikotinil) piperidin-4-ona)
WO2019191684A1 (en) 2018-03-30 2019-10-03 Incyte Corporation Treatment of hidradenitis suppurativa using jak inhibitors
CA3095580A1 (en) 2018-04-13 2019-10-17 Sumitomo Dainippon Pharma Oncology, Inc. Pim kinase inhibitors for treatment of myeloproliferative neoplasms and fibrosis associated with cancer
MX2021002132A (es) 2018-08-24 2021-04-28 Bayer Ag Metodo para preparar 2-[(3r)-3--metilmofolin--4-il]-4-(1-metil-1h- pirazol-5-il)-8-(1h-pirazol-5-il)-1,7-naftiridina.
WO2020167990A1 (en) 2019-02-12 2020-08-20 Tolero Pharmaceuticals, Inc. Formulations comprising heterocyclic protein kinase inhibitors
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
WO2022090101A1 (en) 2020-10-26 2022-05-05 Boehringer Ingelheim International Gmbh Process for synthesis of 2,4-dichloro-5-aminopyrimidine
CN113648294B (zh) * 2021-08-26 2024-01-23 山东领海生物科技有限公司 β-双磺酰亚胺取代酮类化合物在治疗癌症中的应用

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4017500A (en) * 1973-07-16 1977-04-12 Schering Corporation Certain 8-amino-1,7-naphthyridines
DE3815617A1 (de) * 1988-05-07 1989-11-16 Bayer Ag 4-aza-1,10-phenanthrolin-derivate, verfahren zu ihrer herstellung sowie ihre verwendung in schaedlingsbekaempfungsmitteln
DE4011105A1 (de) * 1990-04-06 1991-10-10 Bayer Ag Neue 4-chinolyl-dihydropyridine, verfahren zu ihrer herstellung und ihre verwendung in arzneimitteln
US5204472A (en) * 1990-04-06 1993-04-20 Bayer Aktiengesellschaft Quinoline and isoquinoline intermediates
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
ATE227283T1 (de) * 1996-07-13 2002-11-15 Glaxo Group Ltd Kondensierte heterozyklische verbindungen als protein kinase inhibitoren
EP0837063A1 (en) * 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
GB9708917D0 (en) * 1997-05-01 1997-06-25 Pfizer Ltd Compounds useful in therapy
US7470709B2 (en) * 2002-08-23 2008-12-30 Novartis Vaccines And Diagnostics, Inc. Benzimidazole quinolinones and uses thereof
EP2210892A3 (en) * 2002-10-04 2010-10-27 Prana Biotechnology Limited Neurologically-active compounds
JP4794446B2 (ja) * 2003-09-23 2011-10-19 メルク・シャープ・エンド・ドーム・コーポレイション イソキノリン系カリウムチャンネル阻害薬
WO2005120509A1 (en) 2004-06-04 2005-12-22 Amphora Discovery Corporation Quinoline- and isoquinoline-based compounds exhibiting atp-utilizing enzyme inhibitory activity, and compositions, and uses thereof
JP2006219453A (ja) 2005-02-14 2006-08-24 Tokyo Univ Of Pharmacy & Life Science キノリン環を母核とする金属識別型二波長性蛍光分子
US8232278B2 (en) * 2005-06-24 2012-07-31 Gilead Sciences, Inc. Pyrido(3,2-D)pyrimidines and pharmaceutical compositions useful for treating hepatitis C
US9259426B2 (en) 2006-07-20 2016-02-16 Gilead Sciences, Inc. 4,6-di- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections
PE20090717A1 (es) * 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa
AR066660A1 (es) * 2007-05-23 2009-09-02 Genentech Inc Prevencion y tratamiento de condiciones del ojo asociadas con su complemento
GEP20135849B (en) * 2008-09-02 2013-06-10 Novartis Ag Picolinamide derivatives as kinase inhibitors

Also Published As

Publication number Publication date
AU2009289316A1 (en) 2010-03-11
BRPI0918496A2 (pt) 2019-09-24
JP5564045B2 (ja) 2014-07-30
KR20110058866A (ko) 2011-06-01
CA2735779A1 (en) 2010-03-11
CN102203075B (zh) 2014-09-10
MX2011002367A (es) 2011-04-04
US8735424B2 (en) 2014-05-27
US20110195980A1 (en) 2011-08-11
CN102203075A (zh) 2011-09-28
JP2012501312A (ja) 2012-01-19
EP2342190A1 (en) 2011-07-13
WO2010026121A1 (en) 2010-03-11

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