JP2009521504A - Akt活性阻害剤 - Google Patents

Akt活性阻害剤 Download PDF

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Publication number
JP2009521504A
JP2009521504A JP2008547763A JP2008547763A JP2009521504A JP 2009521504 A JP2009521504 A JP 2009521504A JP 2008547763 A JP2008547763 A JP 2008547763A JP 2008547763 A JP2008547763 A JP 2008547763A JP 2009521504 A JP2009521504 A JP 2009521504A
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JP
Japan
Prior art keywords
pyrrolo
pyridin
amino
thiophenecarboxamide
ethyl
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.)
Withdrawn
Application number
JP2008547763A
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English (en)
Japanese (ja)
Inventor
マーク・アンドリュー・シーフェルド
俊裕 濱嶋
デイビッド・ケンドール・ジュング
裕子 中村
ポール・アール・レイド
マイケル・ジョン・レノ
ミーガン・ビー・ラウズ
ディルク・アー・ヘールディング
タン・ジュン
ワン・ジチョウ
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.)
SmithKline Beecham Corp
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SmithKline Beecham Corp
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Filing date
Publication date
Application filed by SmithKline Beecham Corp filed Critical SmithKline Beecham Corp
Publication of JP2009521504A publication Critical patent/JP2009521504A/ja
Withdrawn legal-status Critical Current

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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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2008547763A 2005-12-22 2006-12-21 Akt活性阻害剤 Withdrawn JP2009521504A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US75303305P 2005-12-22 2005-12-22
US79319806P 2006-04-19 2006-04-19
PCT/US2006/062453 WO2007076423A2 (fr) 2005-12-22 2006-12-21 INHIBITEURS D’ACTIVITE Akt

Publications (1)

Publication Number Publication Date
JP2009521504A true JP2009521504A (ja) 2009-06-04

Family

ID=38218824

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2008547763A Withdrawn JP2009521504A (ja) 2005-12-22 2006-12-21 Akt活性阻害剤

Country Status (3)

Country Link
EP (1) EP1968568A4 (fr)
JP (1) JP2009521504A (fr)
WO (1) WO2007076423A2 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015530980A (ja) * 2012-08-02 2015-10-29 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤として活性な置換ピロール類
JP2021500339A (ja) * 2017-10-18 2021-01-07 エイチケー イノ.エヌ コーポレーション タンパク質キナーゼ阻害剤としての複素環化合物
JP2021520415A (ja) * 2018-04-04 2021-08-19 エピオダイン,インク. オピオイド受容体モジュレーター、およびそれに関連する生成物ならびに方法

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CA2621261C (fr) 2005-09-22 2014-05-20 Incyte Corporation Inhibiteurs tetracycliques de janus kinases
US7625890B2 (en) 2005-11-10 2009-12-01 Smithkline Beecham Corp. Substituted imidazo[4,5-c]pyridine compounds as Akt inhibitors
PT3184526T (pt) 2005-12-13 2018-12-19 Incyte Holdings Corp Derivados de pirrolo[2,3-d]pirimidina como inibidores da cinase janus
CN101389324A (zh) 2005-12-23 2009-03-18 史密丝克莱恩比彻姆公司 Aurora激酶的氮杂吲哚抑制剂
GB0617161D0 (en) * 2006-08-31 2006-10-11 Vernalis R&D Ltd Enzyme inhibitors
EP2121692B1 (fr) 2006-12-22 2013-04-10 Incyte Corporation Hétérocycles substitués servant d'inhibiteurs de janus kinases
UY30892A1 (es) * 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
ES2543325T3 (es) * 2007-02-07 2015-08-18 Glaxosmithkline Llc Inhibidores de la actividad de Akt
US20080312259A1 (en) 2007-06-13 2008-12-18 Incyte Corporation SALTS OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE
CL2008001709A1 (es) 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
ES2389992T3 (es) 2007-11-02 2012-11-05 Vertex Pharmaceuticals Incorporated Derivados de [1H-pirazolo[3,4-b]piridin-4-il]-fenilo o -piridin-2-ilo como proteína cinasa c-theta
EA201070700A1 (ru) * 2007-12-07 2011-06-30 Вертекс Фармасьютикалз Инкорпорейтед Способы получения циклоалкилкарбоксамидопиридинбензойных кислот
US8329709B2 (en) * 2008-01-09 2012-12-11 Genentech, Inc. 5H-cyclopenta[D]pyrimidines as AKT protein kinase inhibitors
TWI444382B (zh) 2008-03-11 2014-07-11 Incyte Corp 作為jak抑制劑之氮雜環丁烷及環丁烷衍生物
JP2011525929A (ja) * 2008-06-26 2011-09-29 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Akt活性の阻害剤
US20110288142A1 (en) 2009-01-30 2011-11-24 Chen Pingyun Y CRYSTALLINE N--5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride
WO2010093885A1 (fr) * 2009-02-12 2010-08-19 Glaxosmithkline Llc Inhibiteurs de l'activité d'akt
EP2426117A4 (fr) * 2009-04-30 2012-09-19 Sumitomo Chemical Co Dérivé de thiophène
ES2487542T3 (es) 2009-05-22 2014-08-21 Incyte Corporation Derivados de N-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como inhibidores de cinasas Janus
CN106967070A (zh) 2009-05-22 2017-07-21 因塞特控股公司 作为jak抑制剂的化合物
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
BR112012008267B1 (pt) 2009-10-09 2022-10-04 Incyte Holdings Corporation Derivados hidroxila, ceto e glucuronida de 3-(4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1- il)-3-ciclopentilpropanonitrila
TWI766281B (zh) 2010-03-10 2022-06-01 美商英塞特控股公司 作為jak1抑制劑之哌啶-4-基三亞甲亞胺衍生物
PE20130216A1 (es) 2010-05-21 2013-02-27 Incyte Corp Formulacion topica para un inhibidor de jak
AR083933A1 (es) 2010-11-19 2013-04-10 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
JP5917544B2 (ja) 2010-11-19 2016-05-18 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Jak阻害剤としての複素環置換ピロロピリジンおよびピロロピリミジン
US9993480B2 (en) 2011-02-18 2018-06-12 Novartis Pharma Ag mTOR/JAK inhibitor combination therapy
EA201490042A1 (ru) 2011-06-20 2014-10-30 Инсайт Корпорейшн Азетидинил-фенил-, пиридил- или пиразинилкарбоксамидные производные как ингибиторы jak
WO2013023119A1 (fr) 2011-08-10 2013-02-14 Novartis Pharma Ag Polythérapie par jak p13k/mtor
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
CN105732639A (zh) 2012-06-29 2016-07-06 辉瑞大药厂 作为LRRK2抑制剂的4-(取代的氨基)-7H-吡咯并〔2,3-d〕嘧啶类
DE102012019369A1 (de) 2012-10-02 2014-04-03 Merck Patent Gmbh 7-Azaindolderivat
SG11201503695XA (en) 2012-11-15 2015-06-29 Incyte Corp Sustained-release dosage forms of ruxolitinib
HUE057262T2 (hu) 2013-03-06 2022-04-28 Incyte Holdings Corp Eljárás és köztitermékek JAK inhibitor elõállítására
TW201533043A (zh) 2013-04-18 2015-09-01 Lundbeck & Co As H 作爲lrrk2抑制劑的芳基吡咯并吡啶衍生化合物
US9655854B2 (en) 2013-08-07 2017-05-23 Incyte Corporation Sustained release dosage forms for a JAK1 inhibitor
EP3083618B1 (fr) 2013-12-17 2018-02-21 Pfizer Inc Nouvelles 1h-pyrrolo[2,3- b]pyridines 3,4-disubstituées et 7h-pyrrolo[2,3-c]pyridazines 4,5-disubstituées en tant qu'inhibiteurs de la lrrk2
CN103833725B (zh) * 2014-03-03 2016-06-08 上海北卡医药技术有限公司 一种合成5-n-叔丁氧羰基-5-n-甲基氨基-2-噻吩甲酸的方法
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
TW201613919A (en) 2014-07-02 2016-04-16 Pharmacyclics Llc Inhibitors of Bruton's tyrosine kinase
JP6873980B2 (ja) 2015-09-14 2021-05-19 ファイザー・インク LRRK2阻害薬としての新規のイミダゾ[4,5−c]キノリンおよびイミダゾ[4,5−c][1,5]ナフチリジン誘導体
EP3426674A4 (fr) 2016-03-09 2019-08-14 Blade Therapeutics, Inc. Composés céto-amides cycliques utilisés en tant que modulateurs de la calpaïne, et leurs procédés de production et d'utilisation
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CN108948002A (zh) 2017-05-19 2018-12-07 厦门大学 五元并六元氮杂芳环类化合物、其制备方法、药用组合物及其应用
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CN112266349B (zh) * 2020-11-17 2022-02-15 上海凌凯医药科技有限公司 一种制备2-氨基-4-甲基-1-丙基-1h-吡咯-3-甲腈的方法
CN115073469B (zh) * 2021-03-15 2023-12-22 药雅科技(上海)有限公司 吡咯并嘧啶类化合物作为激酶抑制剂的制备及其应用
WO2022216717A1 (fr) * 2021-04-05 2022-10-13 The Cleveland Clinic Foundation Inhibiteurs de citron kinase

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KR101223914B1 (ko) * 2003-11-21 2013-01-18 어레이 바이오파마 인크. Akt 단백질 키나제 억제제
AU2005236002A1 (en) * 2004-04-02 2005-11-03 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of rock and other protein kinases
EP1765819B1 (fr) * 2004-06-30 2014-03-12 Vertex Pharmaceuticals Inc. Azaindoles utilises comme inhibiteurs de proteine kinases
WO2006058120A1 (fr) * 2004-11-22 2006-06-01 Vertex Pharmaceuticals Incorporated Inhibiteurs bicycliques de rho kinase
CN101228161B (zh) * 2005-05-20 2012-10-10 沃泰克斯药物股份有限公司 适用作蛋白激酶抑制剂的吡咯并吡啶类

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015530980A (ja) * 2012-08-02 2015-10-29 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤として活性な置換ピロール類
JP2021500339A (ja) * 2017-10-18 2021-01-07 エイチケー イノ.エヌ コーポレーション タンパク質キナーゼ阻害剤としての複素環化合物
JP7112488B2 (ja) 2017-10-18 2022-08-03 エイチケー イノ.エヌ コーポレーション タンパク質キナーゼ阻害剤としての複素環化合物
US11524968B2 (en) 2017-10-18 2022-12-13 Hk Inno.N Corporation Heterocyclic compound as a protein kinase inhibitor
JP2021520415A (ja) * 2018-04-04 2021-08-19 エピオダイン,インク. オピオイド受容体モジュレーター、およびそれに関連する生成物ならびに方法
JP7402857B2 (ja) 2018-04-04 2023-12-21 エピオダイン,インク. オピオイド受容体モジュレーター、およびそれに関連する生成物ならびに方法

Also Published As

Publication number Publication date
EP1968568A2 (fr) 2008-09-17
WO2007076423A2 (fr) 2007-07-05
WO2007076423A3 (fr) 2007-11-29
EP1968568A4 (fr) 2011-04-13

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