JP6026525B2 - 置換6−アザ−イソインドリン−1−オン誘導体 - Google Patents

置換6−アザ−イソインドリン−1−オン誘導体 Download PDF

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JP6026525B2
JP6026525B2 JP2014517111A JP2014517111A JP6026525B2 JP 6026525 B2 JP6026525 B2 JP 6026525B2 JP 2014517111 A JP2014517111 A JP 2014517111A JP 2014517111 A JP2014517111 A JP 2014517111A JP 6026525 B2 JP6026525 B2 JP 6026525B2
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pyrrolo
fluoro
pyridin
amino
pyran
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JP2014520153A5 (enExample
JP2014520153A (ja
Inventor
ニエ、ジャ
チェン、ロンリャン
光功 ▲高▼野
光功 ▲高▼野
ラム、ベティ
ラルディ、マシュウ
ナタラ、スリニヴァサ、レディ
ジェームス ウィルケンズ、スティーヴン
ジェームス ウィルケンズ、スティーヴン
アダムス、マーク、イー.
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Takeda Pharmaceutical Co Ltd
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    • C07ORGANIC CHEMISTRY
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    • 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
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    • A61K31/4365Heterocyclic 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 having sulfur as a ring hetero atom, e.g. ticlopidine
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    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/5365Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2014517111A 2011-06-22 2012-06-20 置換6−アザ−イソインドリン−1−オン誘導体 Expired - Fee Related JP6026525B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161500094P 2011-06-22 2011-06-22
US61/500,094 2011-06-22
PCT/US2012/043276 WO2012177714A1 (en) 2011-06-22 2012-06-20 Substituted 6-aza-isoindolin-1-one derivatives

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JP2014520153A JP2014520153A (ja) 2014-08-21
JP2014520153A5 JP2014520153A5 (enExample) 2015-08-06
JP6026525B2 true JP6026525B2 (ja) 2016-11-16

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US (3) US9056873B2 (enExample)
EP (1) EP2723739B1 (enExample)
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WO (1) WO2012177714A1 (enExample)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG181857A1 (en) 2009-12-23 2012-07-30 Takeda Pharmaceutical Fused heteroaromatic pyrrolidinones as syk inhibitors
CN103833665B (zh) * 2014-02-24 2015-09-23 杰达维(上海)医药科技发展有限公司 一种新的合成异噻唑的方法
PL3233857T3 (pl) * 2014-12-18 2020-07-27 Takeda Pharmaceutical Company Limited Stałe postacie skondensowanych heteroaromatycznych pirolidynonów
US11174254B2 (en) 2017-09-28 2021-11-16 Yangtze River Pharmaceutical Group Co., Ltd. Aniline-substituted 1,2-dihydropyrrol[3,4-C]pyridin/pyrimidin-3-one derivative and use thereof
SG11202002475TA (en) * 2017-10-19 2020-04-29 Bayer Animal Health Gmbh Use of fused heteroaromatic pyrrolidones for treatment and prevention of diseases in animals
ES3030701T3 (en) 2018-05-10 2025-07-01 Zoetis Services Llc Endoparasitic depsipeptides
CN111004211B (zh) * 2019-12-29 2021-04-02 苏州诚和医药化学有限公司 一种依匹哌唑中间体4-溴苯并[b]噻吩的合成方法
CN111393349A (zh) * 2020-05-15 2020-07-10 上海毕得医药科技有限公司 一种4-碘-1h-吡咯-2-甲醛的合成方法
CN117510431A (zh) * 2023-11-08 2024-02-06 浙江雅辰药物科技股份有限公司 一种异噻唑-3-酮及其衍生物、合成方法

Family Cites Families (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS63107966A (ja) 1986-05-22 1988-05-12 Fujisawa Pharmaceut Co Ltd ピリミジン誘導体
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
US5272158A (en) 1991-10-29 1993-12-21 Merck & Co., Inc. Fibrinogen receptor antagonists
US5238950A (en) 1991-12-17 1993-08-24 Schering Corporation Inhibitors of platelet-derived growth factor
GB9518953D0 (en) 1995-09-15 1995-11-15 Pfizer Ltd Pharmaceutical formulations
GB9711643D0 (en) 1997-06-05 1997-07-30 Janssen Pharmaceutica Nv Glass thermoplastic systems
EP1054004B1 (en) 1997-12-15 2008-07-16 Astellas Pharma Inc. Novel pyrimidine-5-carboxamide derivatives
WO1999032479A1 (en) 1997-12-23 1999-07-01 Alcon Laboratories, Inc. Phthalimide-piperidine, -pyrrolidine and -azepine derivatives, their preparation and their use as muscarinic receptor (ant-)agonists
EP1184376B1 (en) 1999-06-09 2005-02-02 Yamanouchi Pharmaceutical Co. Ltd. Novel heterocyclic carboxamide derivatives
GB9918035D0 (en) 1999-07-30 1999-09-29 Novartis Ag Organic compounds
EP1250128A2 (en) 1999-12-16 2002-10-23 Alcon, Inc. Inhibitors of adenosine kinase for the treatment of optic nerve and retinal damage
EP1244668B1 (en) 2000-01-07 2006-04-05 Universitaire Instelling Antwerpen Purine derivatives, process for their preparation and use thereof
AU2001232271A1 (en) 2000-02-14 2001-08-20 Japan Tobacco Inc. Preventives/remedies for postoperative stress
JP2001302667A (ja) 2000-04-28 2001-10-31 Bayer Ag イミダゾピリミジン誘導体およびトリアゾロピリミジン誘導体
WO2002088079A2 (en) 2001-05-01 2002-11-07 Bristol-Myers Squibb Company Dual inhibitors of pde 7 and pde 4
US7105667B2 (en) 2001-05-01 2006-09-12 Bristol-Myers Squibb Co. Fused heterocyclic compounds and use thereof
PE20030008A1 (es) 2001-06-19 2003-01-22 Bristol Myers Squibb Co Inhibidores duales de pde 7 y pde 4
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
WO2003009852A1 (en) 2001-07-24 2003-02-06 Merck & Co., Inc. Tyrosine kinase inhibitors
US20030158195A1 (en) 2001-12-21 2003-08-21 Cywin Charles L. 1,6 naphthyridines useful as inhibitors of SYK kinase
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
MXPA05001804A (es) 2002-08-14 2005-05-27 Vertex Pharma Inhibidores de proteinas cinasas y usos de los mismos.
AU2003286711A1 (en) 2002-10-25 2004-05-13 Vertex Pharmaceuticals Incorporated Indazolinone compositions useful as kinase inhibitors
AU2003286895A1 (en) 2002-11-05 2004-06-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of jak and other protein kinases
EP1610793A2 (en) 2003-03-25 2006-01-04 Vertex Pharmaceuticals Incorporated Thiazoles useful as inhibitors of protein kinases
CA2523126A1 (en) 2003-03-25 2004-10-14 Vertex Pharmaceuticals Incorporated Thiazoles useful as inhibitors of protein kinases
KR20050122220A (ko) 2003-03-25 2005-12-28 다케다 샌디에고, 인코포레이티드 디펩티딜 펩티다제 억제제
US8178671B2 (en) 2003-07-30 2012-05-15 Rigel Pharmaceuticals, Inc. Methods of treating or preventing autoimmune diseases with 2, 4-pyrimidinediamine compounds
US7320992B2 (en) 2003-08-25 2008-01-22 Amgen Inc. Substituted 2,3-dihydro-1h-isoindol-1-one derivatives and methods of use
US20050182061A1 (en) 2003-10-02 2005-08-18 Jeremy Green Phthalimide compounds useful as protein kinase inhibitors
WO2005056524A2 (en) 2003-12-09 2005-06-23 Euro-Celtique S.A. Therapeutic agents useful for treating pain
US8057815B2 (en) 2004-04-19 2011-11-15 Portola Pharmaceuticals, Inc. Methods of treatment with Syk inhibitors
JP2008511659A (ja) 2004-09-01 2008-04-17 ライジェル ファーマシューティカルズ, インコーポレイテッド 2,4−ピリミジンジアミン化合物の合成
EP1814878B1 (en) 2004-11-24 2012-01-04 Rigel Pharmaceuticals, Inc. Spiro-2, 4-pyrimidinediamine compounds and their uses
US20060128710A1 (en) 2004-12-09 2006-06-15 Chih-Hung Lee Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof
KR100926399B1 (ko) 2005-04-06 2009-11-12 아이알엠 엘엘씨 디아릴아민―함유 화합물 및 조성물, 및 스테로이드 호르몬핵 수용체의 조절제로서의 그들의 용도
US7745641B2 (en) 2005-04-19 2010-06-29 Kyowa Hakko Kirin Co., Ltd. Nitrogen-containing heterocyclic compound
WO2006129100A1 (en) 2005-06-03 2006-12-07 Glaxo Group Limited Novel compounds
CA2608476A1 (en) 2005-06-28 2007-01-04 Bausch & Lomb Incorporated Preparations comprising arylazine substituted with a carbonylic moiety to increase the activity of gelatinase a in ocular cells
AR056191A1 (es) 2005-08-23 2007-09-26 Idenix Phatmaceuticals Inc Anillo de nucleosidos de siete miembros como inhibidores de la replica viral, metodos para su sintesis, composiciones farmaceuticas que los contienen y su uso en el tratamiento de infecciones con virus de la familia flaviviridae
WO2007023382A2 (en) 2005-08-25 2007-03-01 Pfizer Inc. Pyrimidine amino pyrazole compounds, potent kinase inhibitors
US20070117775A1 (en) 2005-10-31 2007-05-24 Rigel Pharmaceuticals, Inc. Compositions and Methods For Treating Inflammatory Disorders
WO2007070872A1 (en) 2005-12-15 2007-06-21 Rigel Pharmaceuticals, Inc. Kinase inhibitors and their uses
EP2537849A3 (en) 2006-01-17 2013-04-03 Vertex Pharmaceuticals, Inc. Azaindoles useful as inhibitors of janus kinases
CL2007002617A1 (es) 2006-09-11 2008-05-16 Sanofi Aventis Compuestos derivados de pirrolo[2,3-b]pirazin-6-ilo; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar inflamacion de las articulaciones, artritis reumatoide, tumores, linfoma de las celulas del manto.
EP2108642A1 (en) 2006-10-17 2009-10-14 Kyowa Hakko Kirin Co., Ltd. Jak inhibitor
MX2009004077A (es) 2006-10-19 2009-05-05 Signal Pharm Llc Compuestos de heteroarilo, composiciones de los mismos, y su uso como inhibidores de proteina cinasas.
WO2008057402A2 (en) 2006-11-02 2008-05-15 Cytovia, Inc. N-aryl-isoxazolopyrimidin-4-amines and related compounds as activators of caspases and inducers of apoptosis and the use thereof
JP5264759B2 (ja) 2006-11-21 2013-08-14 ライジェル ファーマシューティカルズ, インコーポレイテッド 2,4−ピリミジンジアミン化合物のプロドラッグ塩およびそれらの使用
JPWO2008081928A1 (ja) 2006-12-28 2010-04-30 大正製薬株式会社 ピラゾロピリミジン化合物
JP2010522174A (ja) 2007-03-23 2010-07-01 シェーリング コーポレイション Hcvns3−プロテアーゼ阻害剤としてのヒドラジド−ペプチド
EP2162136A4 (en) 2007-06-03 2012-02-15 Univ Vanderbilt GLUTAMATE METABOTROPIC POSITIVE RECEPTOR-BASED ALLOSTERIC-MODULATOR BENZAMIDE DERIVATIVES (MGLUR5) AND METHODS OF MAKING AND USING THEM
WO2009026107A1 (en) 2007-08-17 2009-02-26 Portola Pharmaceuticals, Inc. Protein kinase inhibitors
JP2009067729A (ja) 2007-09-14 2009-04-02 Kyowa Hakko Kirin Co Ltd Hsp90ファミリー蛋白質阻害剤
CA2705303A1 (en) 2007-11-07 2009-05-14 Foldrx Pharmaceuticals, Inc. Modulation of protein trafficking
WO2009080638A2 (en) 2007-12-20 2009-07-02 Cellzome Limited Sulfamides as zap-70 inhibitors
JP5496915B2 (ja) 2008-02-13 2014-05-21 シージーアイ ファーマシューティカルズ,インコーポレーテッド 6−アリール−イミダゾ[1,2−a]ピラジン誘導体、その製造方法、及びその使用方法
AU2009215430B2 (en) 2008-02-22 2015-02-12 Rigel Pharmaceuticals, Inc. Use of 2,4-pyrimidinediamines for the treatment of atherosclerosis
US8436005B2 (en) 2008-04-03 2013-05-07 Abbott Laboratories Macrocyclic pyrimidine derivatives
WO2009145856A1 (en) 2008-04-16 2009-12-03 Portola Pharmaceuticals, Inc. 2, 6-diamino-pyrimidin- 5-yl-carboxamides as syk or jak kinases inhibitors
KR101773313B1 (ko) 2008-04-16 2017-08-31 포톨라 파마슈티컬스, 인코포레이티드 syk 또는 JAK 키나제 억제제로서의 2,6-디아미노-피리미딘-5-일-카르복스아미드
EP2310381A1 (en) 2008-06-13 2011-04-20 Novartis AG 2,4'-bipyridinyl compounds as protein kinase d inhibitors useful for the treatment of ia heart failure and cancer
WO2010015518A2 (de) 2008-08-05 2010-02-11 Boehringer Ingelheim Interntional Gmbh 4-dimethylamino-phenyl-substituierte naphthyridine und ihre verwendung als arzneimittel
WO2010015520A1 (de) 2008-08-05 2010-02-11 Boehringer Ingelheim International Gmbh Substituierte naphthyridine und ihre verwendung als arzneimittel
TWI453207B (zh) 2008-09-08 2014-09-21 Signal Pharm Llc 胺基三唑并吡啶,其組合物及使用其之治療方法
EP3552607A3 (en) 2008-12-08 2020-01-15 Gilead Connecticut, Inc. Imidazopyrazine syk inhibitors
EP2443106A1 (en) 2009-06-18 2012-04-25 Cellzome Limited Heterocyclylaminopyrimidines as kinase inhibitors
MX2012007154A (es) 2009-12-17 2012-08-01 Merck Sharp & Dohme Aminopirimidinas como inhibidores de syk.
EP2512246B1 (en) 2009-12-17 2015-09-30 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
SG181857A1 (en) 2009-12-23 2012-07-30 Takeda Pharmaceutical Fused heteroaromatic pyrrolidinones as syk inhibitors
GB201007203D0 (en) 2010-04-29 2010-06-16 Glaxo Group Ltd Novel compounds

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