JP2011518219A - タンパク質キナーゼの阻害剤 - Google Patents

タンパク質キナーゼの阻害剤 Download PDF

Info

Publication number
JP2011518219A
JP2011518219A JP2011506293A JP2011506293A JP2011518219A JP 2011518219 A JP2011518219 A JP 2011518219A JP 2011506293 A JP2011506293 A JP 2011506293A JP 2011506293 A JP2011506293 A JP 2011506293A JP 2011518219 A JP2011518219 A JP 2011518219A
Authority
JP
Japan
Prior art keywords
alkylene
ylamino
pyrrolo
pyrimidin
amino
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Withdrawn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
JP2011506293A
Other languages
English (en)
Japanese (ja)
Other versions
JP2011518219A5 (OSRAM
Inventor
ヨンホン・ソン
スー・キン
ショーン・エム・バウアー
チャオチョン・ジェイ・ジア
ムクンド・メーロトラ
アンジャリ・パンディ
Original Assignee
ポートラ ファーマシューティカルズ， インコーポレイテッド
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 ポートラ ファーマシューティカルズ， インコーポレイテッド filed Critical ポートラ ファーマシューティカルズ， インコーポレイテッド
Publication of JP2011518219A publication Critical patent/JP2011518219A/ja
Publication of JP2011518219A5 publication Critical patent/JP2011518219A5/ja
Withdrawn legal-status Critical Current

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/16—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2011506293A 2008-04-22 2009-04-22 タンパク質キナーゼの阻害剤 Withdrawn JP2011518219A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US4707708P 2008-04-22 2008-04-22
US61/047,077 2008-04-22
PCT/US2009/002512 WO2009131687A2 (en) 2008-04-22 2009-04-22 Inhibitors of protein kinases

Publications (2)

Publication Number Publication Date
JP2011518219A true JP2011518219A (ja) 2011-06-23
JP2011518219A5 JP2011518219A5 (OSRAM) 2012-06-14

Family

ID=40910850

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2011506293A Withdrawn JP2011518219A (ja) 2008-04-22 2009-04-22 タンパク質キナーゼの阻害剤

Country Status (10)

Country Link
US (2) US8258144B2 (OSRAM)
EP (1) EP2271631B1 (OSRAM)
JP (1) JP2011518219A (OSRAM)
CN (2) CN102066338A (OSRAM)
AU (1) AU2009238590A1 (OSRAM)
BR (1) BRPI0910668A2 (OSRAM)
CA (1) CA2723185A1 (OSRAM)
IL (1) IL208719A0 (OSRAM)
NZ (1) NZ588830A (OSRAM)
WO (1) WO2009131687A2 (OSRAM)

Cited By (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011525193A (ja) * 2008-06-20 2011-09-15 ジェネンテック， インコーポレイテッド トリアゾロピリジンｊａｋ阻害剤化合物と方法
JP2011525192A (ja) * 2008-06-20 2011-09-15 ジェネンテック， インコーポレイテッド トリアゾロピリジンｊａｋ阻害剤化合物と方法
JP2015524828A (ja) * 2012-08-14 2015-08-27 シュエンジュウ・ファーマ・カンパニー・リミテッド 二環性基置換ピリミジン化合物
JP2015534959A (ja) * 2012-10-19 2015-12-07 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Ｓｙｋの阻害剤
JP2016505041A (ja) * 2013-01-16 2016-02-18 シグナル ファーマシューティカルズ，エルエルシー 置換型ピロロピリミジン化合物、その組成物、およびこれらを用いた治療方法
JP2016530335A (ja) * 2013-09-18 2016-09-29 北京韓美薬品有限公司 Ｂｔｋ及び／又はｊａｋ３キナーゼの活性を抑制する化合物
JP2016534056A (ja) * 2013-10-21 2016-11-04 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ Ｂｔｋ阻害剤としてのヘテロアリール化合物及びその使用
WO2016208595A1 (ja) * 2015-06-22 2016-12-29 小野薬品工業株式会社 Ｂｒｋ阻害化合物
JP2018514559A (ja) * 2015-04-29 2018-06-07 シアメン ユニヴァーシティー ピリミドピロール類化合物、その調製方法、医薬用組成物及びその応用
WO2018117177A1 (ja) * 2016-12-21 2018-06-28 小野薬品工業株式会社 Ｂｒｋ阻害化合物
JP2018523672A (ja) * 2015-08-13 2018-08-23 北京韓美薬品有限公司 Ｉｒａｋ４阻害剤、及びその応用
JP2018524356A (ja) * 2015-07-09 2018-08-30 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ Ｂｔｋ阻害剤としてのピリミジン誘導体及びその使用
JP2018525394A (ja) * 2015-08-13 2018-09-06 北京韓美薬品有限公司 Ｉｒａｋ４阻害剤、及びその応用
JP2019518796A (ja) * 2016-06-27 2019-07-04 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−ジアミノ−ピリミジン化合物ならびに該化合物の作製法および使用法
JP2019532092A (ja) * 2016-10-28 2019-11-07 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｉｌ−１２、ｉｌ−２３および／またはｉｆｎアルファ応答の調節剤として有用なヘテロ二環化合物
JP2019536820A (ja) * 2016-12-01 2019-12-19 アプトセ バイオサイエンシーズ インコーポレイテッド Ｂｒａｄ４およびｊａｋ２の二重阻害剤としての縮合環式ピリミジン化合物、ならびにその使用に関する方法
JP2022518723A (ja) * 2019-01-18 2022-03-16 ボロノイ・カンパニー・リミテッド ピロロピリジン誘導体およびタンパク質キナーゼ関連疾患の予防または治療での使用のためのその用途
JP2022523477A (ja) * 2019-01-18 2022-04-25 ボロノイ・カンパニー・リミテッド ピロロピリミジン誘導体及びこれを有効成分として含有するタンパク質キナーゼ関連疾患の予防又は治療用薬学的組成物
US12194048B2 (en) 2020-12-09 2025-01-14 Voronoi Co., Ltd. Use of pyrrolopyridine derivatives for preventing or treating inflammatory diseases

Families Citing this family (152)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20140097446A (ko) 2006-11-20 2014-08-06 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 통증 및 소양증 치료용 방법, 조성물 및 키트
JP2010518083A (ja) * 2007-02-12 2010-05-27 メルク・シャープ・エンド・ドーム・コーポレイション ピペリジン誘導体
US8063058B2 (en) 2008-04-16 2011-11-22 Portola Pharmaceuticals, Inc. Inhibitors of syk and JAK protein kinases
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
AU2009248923B2 (en) 2008-05-21 2015-01-29 Takeda Pharmaceutical Company Limited Phosphorous derivatives as kinase inhibitors
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
WO2010038081A2 (en) * 2008-10-03 2010-04-08 Astrazeneca Ab Heterocyclic derivatives and methods of use thereof
US8242248B2 (en) * 2009-03-23 2012-08-14 Nodality, Inc. Kits for multiparametric phospho analysis
CA2767646C (en) 2009-07-10 2019-01-29 President And Fellows Of Harvard College Permanently charged sodium and calcium channel blockers as anti-inflammatory agents
EP2536689A1 (en) * 2010-02-17 2012-12-26 Amgen Inc. Aryl carboxamide derivatives as sodium channel inhibitors for treatment of pain
TWI513694B (zh) 2010-05-11 2015-12-21 Amgen Inc 抑制間變性淋巴瘤激酶的嘧啶化合物
PL2589592T3 (pl) 2010-06-30 2019-03-29 Fujifilm Corporation Nowe pochodne nikotynamidu lub ich sole
US9586961B2 (en) 2010-07-09 2017-03-07 Leo Pharma A/S Homopiperazine derivatives as protein tyrosine kinase inhibitors and pharmaceutical use thereof
CN102372717B (zh) * 2010-08-20 2014-06-18 和记黄埔医药（上海）有限公司 吡咯并嘧啶类化合物及其用途
AU2011323484B2 (en) * 2010-11-01 2016-10-06 Portola Pharmaceuticals, Inc. Benzamides and nicotinamides as Syk modulators
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
CN102093364B (zh) 2011-01-07 2015-01-28 北京赛林泰医药技术有限公司 作为FAK/Pyk2抑制剂的2,4-二氨基-6,7-二氢-5H-吡咯并[2,3]嘧啶衍生物
CN103476776B (zh) * 2011-01-07 2016-09-28 北京赛林泰医药技术有限公司 作为FAK/Pyk2抑制剂的2,4-二氨基-6,7-二氢-5H-吡咯并[2,3]嘧啶衍生物
EP2489663A1 (en) 2011-02-16 2012-08-22 Almirall, S.A. Compounds as syk kinase inhibitors
WO2012123312A1 (en) * 2011-03-11 2012-09-20 Glaxo Group Limited Pyrido[3,4-b]pyrazine derivatives as syk inhibitors
PH12013501940A1 (en) * 2011-03-23 2015-12-04 Amgen Inc Fused tricyclic dual inhibitors of cdk 4/6 and flt3
UA120740C2 (uk) 2011-04-22 2020-02-10 Сігнал Фармасьютікалз, Елелсі Заміщені діамінокарбоксамідні і діамінокарбонітрильні похідні піримідинів, їх композиції і способи лікування з їх допомогою
US9834518B2 (en) 2011-05-04 2017-12-05 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in EGFR-driven cancers
JP2014513687A (ja) 2011-05-10 2014-06-05 メルク・シャープ・アンド・ドーム・コーポレーション Ｓｙｋ阻害薬としてのピリジルアミノピリジン
EP2706852B1 (en) 2011-05-10 2018-08-22 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as syk inhibitors
MX2013013090A (es) 2011-05-10 2013-12-16 Merck Sharp & Dohme Aminopirimidinas como inhibidores de tirosina cinaza del bazo.
EP2554544A1 (en) 2011-08-01 2013-02-06 Almirall, S.A. Pyridin-2(1h)-one derivatives as jak inhibitors
EP2763976B1 (en) 2011-10-05 2016-05-18 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
EP2763974B1 (en) 2011-10-05 2016-09-14 Merck Sharp & Dohme Corp. Phenyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
WO2013052393A1 (en) 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. 3-PYRIDYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
CA2856301C (en) 2011-11-23 2020-10-06 Portola Pharmaceuticals, Inc. Pyrazine kinase inhibitors
ES2661444T3 (es) 2011-12-28 2018-04-02 Fujifilm Corporation Nuevo derivado de nicotinamida o sal del mismo
US9586965B2 (en) 2012-01-13 2017-03-07 Acea Biosciences Inc. Pyrrolo[2,3-d]pyrimidine compounds as inhibitors of protein kinases
US9034885B2 (en) 2012-01-13 2015-05-19 Acea Biosciences Inc. EGFR modulators and uses thereof
CN110194748A (zh) 2012-01-13 2019-09-03 艾森生物科学公司 杂环化合物及其作为抗癌药的用途
US9464089B2 (en) 2012-01-13 2016-10-11 Acea Biosciences Inc. Heterocyclic compounds and uses thereof
JP6469567B2 (ja) 2012-05-05 2019-02-13 アリアド・ファーマシューティカルズ・インコーポレイテッド Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物
SI2861595T1 (sl) 2012-06-13 2017-04-26 Incyte Holdings Corporation Substituirane triciklične spojine kot inhibitorji fgfr
WO2013192128A1 (en) 2012-06-20 2013-12-27 Merck Sharp & Dohme Corp. Imidazolyl analogs as syk inhibitors
WO2013192125A1 (en) 2012-06-20 2013-12-27 Merck Sharp & Dohme Corp. Pyrazolyl derivatives as syk inhibitors
US9416111B2 (en) 2012-06-22 2016-08-16 Merck Sharp & Dohme Corp. Substituted diazine and triazine spleen tyrosine kinease (Syk) inhibitors
EP2863916B1 (en) 2012-06-22 2018-07-18 Merck Sharp & Dohme Corp. Substituted pyridine spleen tyrosine kinase (syk) inhibitors
CA2878054C (en) 2012-06-29 2018-09-11 Pfizer Inc. Novel 4-(substituted-amino)-7h-pyrrolo[2,3-d]pyrimidines as lrrk2 inhibitors
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
WO2014031438A2 (en) 2012-08-20 2014-02-27 Merck Sharp & Dohme Corp. SUBSTITUTED PHENYL SPLEEN TYROSINE KINASE (Syk) INHIBITORS
EP2900665B1 (en) 2012-09-28 2018-01-03 Merck Sharp & Dohme Corp. Triazolyl derivatives as syk inhibitors
TWI623531B (zh) 2012-11-21 2018-05-11 Ｐｔｃ治療公司 經取代反向嘧啶ｂｍｉ－１抑制劑
WO2014085154A1 (en) 2012-11-27 2014-06-05 Beth Israel Deaconess Medical Center, Inc. Methods for treating renal disease
WO2014093191A1 (en) 2012-12-12 2014-06-19 Merck Sharp & Dohme Corp. AMINO-PYRIMIDINE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
WO2014130693A1 (en) * 2013-02-25 2014-08-28 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
US10130609B2 (en) 2013-03-13 2018-11-20 University Health Network Pyrazole derivatives and their uses thereof
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
LT2986610T (lt) 2013-04-19 2018-04-10 Incyte Holdings Corporation Bicikliniai heterociklai, kaip fgfr inhibitoriai
WO2014176210A1 (en) 2013-04-26 2014-10-30 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
EP2988749B1 (en) 2013-04-26 2019-08-14 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyrimidines as spleen tyrosine kinase inhibitors
CN104177363B (zh) * 2013-05-24 2018-06-05 江苏先声药业有限公司 双环杂环胺类Hedgehog信号通路抑制剂
KR101657616B1 (ko) * 2013-05-24 2016-09-19 주식회사유한양행 피리미딘 고리를 포함하는 바이사이클릭 유도체 및 그의 제조방법
EP3019496B1 (en) 2013-07-11 2019-09-11 ACEA Therapeutics, Inc. Pyrimidine derivatives as kinase inhibitors
JP6524094B2 (ja) 2013-08-30 2019-06-05 ピーティーシー セラピューティクス， インコーポレイテッド 置換ピリミジンＢｍｉ−１阻害剤
US10584115B2 (en) 2013-11-21 2020-03-10 Ptc Therapeutics, Inc. Substituted pyridine and pyrazine BMI-1 inhibitors
JP6345786B2 (ja) 2013-12-05 2018-06-20 ファーマサイクリックス エルエルシー ブルトン型チロシンキナーゼの阻害剤
JP6487921B2 (ja) 2013-12-17 2019-03-20 ファイザー・インク ＬＲＲＫ２阻害薬としての新規の３，４−二置換−１Ｈ−ピロロ［２，３−ｂ］ピリジンおよび４，５−二置換−７Ｈ−ピロロ［２，３−ｃ］ピリダジン
EP3083559B1 (en) 2013-12-20 2021-03-10 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
US9783531B2 (en) 2013-12-20 2017-10-10 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
EP3083560B1 (en) 2013-12-20 2021-10-27 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
US10093646B2 (en) 2014-01-17 2018-10-09 Novartis Ag 1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and compositions thereof for inhibiting the activity of SHP2
JP6473457B2 (ja) 2014-01-17 2019-02-20 ノバルティス アーゲー Ｓｈｐ２の活性を阻害するための１−（トリアジン−３−イル／ピリダジン−３−イル）−ピペリジン／ピペラジン誘導体およびその組成物
GB201401086D0 (en) * 2014-01-23 2014-03-12 Galapagos Nv Novel compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders
NZ715903A (en) 2014-01-30 2017-06-30 Signal Pharm Llc Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use
EP3116506B1 (en) 2014-03-13 2019-04-17 Merck Sharp & Dohme Corp. 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors
MX2016012574A (es) 2014-03-28 2017-09-26 Calitor Sciences Llc Compuestos heteroarilo sustituidos y metodos de uso.
JP2017518737A (ja) 2014-04-21 2017-07-13 ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． ＳＹＫ標的治療薬のための抗ｐＳＹＫ抗体分子及びその使用
CN104086551B (zh) * 2014-06-06 2016-09-21 人福医药集团股份公司 化合物及其制备方法和用途
CA2955009A1 (en) * 2014-07-14 2016-01-21 Signal Pharmaceuticals, Llc Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof
NZ629796A (en) * 2014-07-14 2015-12-24 Signal Pharm Llc Amorphous form of 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d]oxazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
JP6903577B2 (ja) 2014-12-16 2021-07-14 シグナル ファーマシューティカルズ，エルエルシー 皮膚におけるｃ−Ｊｕｎ Ｎ末端キナーゼの阻害の測定方法
CA3210612A1 (en) 2014-12-16 2016-06-23 Signal Pharmaceuticals, Llc Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide
TWI727939B (zh) 2015-01-16 2021-05-21 美商通用醫院公司 改善ｍＲＮＡ剪接之化合物
WO2016123291A1 (en) 2015-01-29 2016-08-04 Signal Pharmaceuticals, Llc Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide
CN105837577B (zh) * 2015-02-02 2019-01-25 四川大学 1-(嘧啶-4-基)3-胺基哌啶衍生物及其制备方法和用途
EP3256475A4 (en) * 2015-02-13 2019-02-13 Dana-Farber Cancer Institute, Inc. LRRK2 INHIBITORS AND METHOD FOR THE PRODUCTION AND USE THEREOF
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
SG10201913036RA (en) 2015-02-20 2020-02-27 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
ES2824576T3 (es) 2015-06-19 2021-05-12 Novartis Ag Compuestos y composiciones para inhibir la actividad de SHP2
EP3310779B1 (en) 2015-06-19 2019-05-08 Novartis AG Compounds and compositions for inhibiting the activity of shp2
CN107922388B (zh) 2015-06-19 2020-12-29 诺华股份有限公司 用于抑制shp2活性的化合物和组合物
WO2017011720A1 (en) * 2015-07-16 2017-01-19 Signal Pharmaceuticals, Llc Solod forms 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d] oxazol-6-yl)17h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use
CA2993173C (en) 2015-07-24 2023-10-03 Celgene Corporation Methods of synthesis of (1r,2r,5r)-5-amino-2-methylcyclohexanol hydrochloride and intermediates useful therein
CN108348774A (zh) 2015-08-03 2018-07-31 哈佛大学校长及研究员协会 带电离子通道阻断剂及其应用
WO2017046675A1 (en) 2015-09-14 2017-03-23 Pfizer Inc. Novel imidazo [4,5-c] quinoline and imidazo [4,5-c][1,5] naphthyridine derivatives as lrrk2 inhibitors
US10526309B2 (en) 2015-10-02 2020-01-07 The University Of North Carolina At Chapel Hill Pan-TAM inhibitors and Mer/Axl dual inhibitors
US10533011B2 (en) 2015-10-09 2020-01-14 ACEA Therapeutics, Inc. Pharmaceutical salts, physical forms, and compositions of pyrrolopyrimidine kinase inhibitors, and methods of making same
WO2017148995A1 (en) 2016-03-04 2017-09-08 Bayer Pharma Aktiengesellschaft 1-(pyrimidin-2-yl)-1h-indazoles having bub1 kinase inhibiting activity
US10711002B2 (en) 2016-04-21 2020-07-14 The Royal Institution For The Advancement Of Learning/Mcgill University Purine compounds and method for the treatment of cancer
PT3468972T (pt) 2016-06-14 2020-08-21 Novartis Ag Compostos e composições para inibir a atividade da shp2
CN106187899B (zh) * 2016-06-28 2019-07-16 绍兴文理学院 一种氟代氮杂芳烃的合成方法
WO2018004306A1 (en) * 2016-06-30 2018-01-04 Daewoong Pharmaceutical Co., Ltd. Pyrazolopyrimidine derivatives as kinase inhibitor
CN106349224A (zh) * 2016-08-03 2017-01-25 山东大学 一种含有4‑氨基‑(1h)‑吡唑结构的jak激酶抑制剂及其制备方法和应用
JP7503380B2 (ja) 2017-01-10 2024-06-20 ノバルティス アーゲー Ａｌｋ阻害剤およびｓｈｐ２阻害剤を含む組合せ医薬
EP3587422A4 (en) 2017-02-22 2020-05-06 Daegu-Gyeongbuk Medical Innovation Foundation PYRROLO-PYRIMIDINE DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME AS ACTIVE INGREDIENT FOR THE PREVENTION OR TREATMENT OF A PROTEIN KINASE-RELATED DISEASE
JP2020516682A (ja) 2017-04-07 2020-06-11 エイシア セラピューティクス， インコーポレイテッド ピロロピリミジンキナーゼの薬学的な塩、物理的形態および組成物、ならびにその作製方法
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
WO2019043208A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROQUINOLINONES
JOP20180094A1 (ar) * 2017-10-18 2019-04-18 Hk Inno N Corp مركب حلقي غير متجانس كمثبط بروتين كيناز
PE20201146A1 (es) 2017-12-28 2020-10-26 Dae Woong Pharma Derivado de oxi-fluoropiperidina como inhibidor de quinasa
PL3788047T3 (pl) 2018-05-04 2025-04-14 Incyte Corporation Stałe postacie inhibitora fgfr i sposoby ich otrzymywania
KR20210018264A (ko) 2018-05-04 2021-02-17 인사이트 코포레이션 Fgfr 억제제의 염
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
CA3129131A1 (en) 2019-03-11 2020-09-17 Bridget Mccarthy Cole Charged ion channel blockers and methods for use
US10786485B1 (en) 2019-03-11 2020-09-29 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
US10780083B1 (en) 2019-03-11 2020-09-22 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
JP7678757B2 (ja) 2019-03-11 2025-05-16 ノシオン セラピューティクス，インコーポレイテッド 荷電したイオンチャンネル遮断薬および使用方法
CN113924094A (zh) 2019-03-11 2022-01-11 诺西恩医疗公司 酯取代的离子通道阻滞剂及其使用方法
KR20210142154A (ko) 2019-03-21 2021-11-24 옹쎄오 암 치료를 위한 키나제 억제제와 조합된 dbait 분자
KR20200133188A (ko) * 2019-05-17 2020-11-26 보로노이바이오 주식회사 헤테로고리 융합 피리미딘 유도체 및 이의 용도
CN110317176A (zh) * 2019-07-04 2019-10-11 沈阳药科大学 2-氨基嘧啶类化合物及其用途
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
KR20220088699A (ko) 2019-09-27 2022-06-28 디스크 메디슨, 인크. 골수섬유증 및 관련 상태의 치료 방법
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CR20220169A (es) 2019-10-14 2022-10-27 Incyte Corp Heterociclos bicíclicos como inhibidores de fgfr
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
EP4054586A4 (en) 2019-11-06 2023-11-22 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
US10842798B1 (en) 2019-11-06 2020-11-24 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
JP2023500906A (ja) 2019-11-08 2023-01-11 インサーム（インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル） キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
JP7720840B2 (ja) 2019-12-04 2025-08-08 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式複素環
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
US12162851B2 (en) 2020-03-11 2024-12-10 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
JP7708777B2 (ja) 2020-03-11 2025-07-15 ノシオン セラピューティクス，インコーポレイテッド 荷電したイオンチャンネル遮断薬および使用方法
JP2023528223A (ja) 2020-05-13 2023-07-04 ディスク・メディシン・インコーポレイテッド 骨髄線維症を処置するための抗ヘモジュベリン（ｈｊｖ）抗体
CN115667228A (zh) * 2020-05-25 2023-01-31 上海翰森生物医药科技有限公司 杂芳类衍生物的盐、晶型及其制备方法
CN113717194A (zh) * 2020-05-25 2021-11-30 上海翰森生物医药科技有限公司 杂芳类衍生物的盐及其制备方法
CN113717202B (zh) * 2020-05-25 2025-10-17 上海翰森生物医药科技有限公司 杂芳类衍生物的自由碱晶型及其制备方法
CN112107580A (zh) * 2020-09-29 2020-12-22 北京鑫开元医药科技有限公司 一种脾酪氨酸激酶抑制剂的制剂组合物及其制备方法
CN111892580B (zh) * 2020-09-29 2021-02-05 北京鑫开元医药科技有限公司 一种2-氨基-4-(异吲哚啉-2-基)嘧啶-5-甲酰胺衍生物、制备方法及应用
WO2022203466A1 (ko) * 2021-03-26 2022-09-29 주식회사 스탠다임 Lrrk2에 대해 저해 활성을 갖는 신규한 페닐아미노피리미딘 화합물 및 이의 용도
TW202304459A (zh) 2021-04-12 2023-02-01 美商英塞特公司 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法
KR20240004539A (ko) * 2021-04-30 2024-01-11 위겐 바이오메더슨 테크널러지 (상하이) 컴퍼니 리미티드 Wee-1 억제제로서의 축합 고리 화합물, 그를 위한 제조 방법 및 그의 용도
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
EP4352060A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US20250122202A1 (en) * 2021-09-18 2025-04-17 Shandong New Time Pharmaceutical Co., Ltd. Egfr inhibitor, preparation method therefor and use thereof
WO2023055731A1 (en) * 2021-09-28 2023-04-06 Sanford Burnham Prebys Medical Discovery Institute Inhibitors of serine/threonine protein kinase stk3 or stk4 and uses thereof
WO2023107705A1 (en) 2021-12-10 2023-06-15 Incyte Corporation Bicyclic amines as cdk12 inhibitors
CN116813550A (zh) * 2022-03-28 2023-09-29 上海医药工业研究院有限公司 吲唑类衍生物、其制备方法、药物组合物及应用
CN118005609B (zh) * 2022-11-09 2025-06-17 沈阳药科大学 2-氨基嘧啶类化合物及其用途
US20250320206A1 (en) * 2024-03-27 2025-10-16 Gilead Sciences, Inc. Stat6 degraders

Family Cites Families (81)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5728536A (en) * 1993-07-29 1998-03-17 St. Jude Children's Research Hospital Jak kinases and regulation of Cytokine signal transduction
DE59610282D1 (de) * 1995-05-19 2003-04-30 Siemens Ag Verfahren zum rechnergestützten austausch kryptographischer schlüssel zwischen einer ersten computereinheit und einer zweiten computereinheit
US6316635B1 (en) * 1995-06-07 2001-11-13 Sugen, Inc. 2-indolinone derivatives as modulators of protein kinase activity
US6696448B2 (en) * 1996-06-05 2004-02-24 Sugen, Inc. 3-(piperazinylbenzylidenyl)-2-indolinone compounds and derivatives as protein tyrosine kinase inhibitors
US6316429B1 (en) * 1997-05-07 2001-11-13 Sugen, Inc. Bicyclic protein kinase inhibitors
US6486185B1 (en) * 1997-05-07 2002-11-26 Sugen, Inc. 3-heteroarylidene-2-indolinone protein kinase inhibitors
GB9718913D0 (en) 1997-09-05 1997-11-12 Glaxo Group Ltd Substituted oxindole derivatives
US6133305A (en) * 1997-09-26 2000-10-17 Sugen, Inc. 3-(substituted)-2-indolinones compounds and use thereof as inhibitors of protein kinase activity
WO2000000202A1 (en) 1998-06-30 2000-01-06 Parker Hughes Institute Method for inhibiting c-jun expression using jak-3 inhibitors
EP1105378B1 (en) 1998-08-21 2005-03-30 Parker Hughes Institute Quinazoline derivatives
GB9828511D0 (en) 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
US6841567B1 (en) 1999-02-12 2005-01-11 Cephalon, Inc. Cyclic substituted fused pyrrolocarbazoles and isoindolones
GB9904995D0 (en) 1999-03-04 1999-04-28 Glaxo Group Ltd Substituted aza-oxindole derivatives
US6624171B1 (en) * 1999-03-04 2003-09-23 Smithkline Beecham Corporation Substituted aza-oxindole derivatives
US6080747A (en) * 1999-03-05 2000-06-27 Hughes Institute JAK-3 inhibitors for treating allergic disorders
GB9905075D0 (en) * 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
US7125875B2 (en) 1999-04-15 2006-10-24 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
US7655423B2 (en) 1999-06-14 2010-02-02 Henry Ford Health System Nitric oxide donors for inducing neurogenesis
GB9918035D0 (en) * 1999-07-30 1999-09-29 Novartis Ag Organic compounds
AU4903201A (en) * 1999-11-30 2001-07-03 Parker Hughes Institute Inhibitors of thrombin induced platelet aggregation
CN1195755C (zh) 1999-12-10 2005-04-06 辉瑞产品公司 吡咯并[2,3－d]嘧啶化合物
US6610688B2 (en) * 1999-12-21 2003-08-26 Sugen, Inc. 4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors
US20020065270A1 (en) 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
ATE369844T1 (de) 2000-01-24 2007-09-15 Genzyme Corp Inhibitoren des jak/stat-weges und deren verwendung zur behandlung von allgemeiner primärer osteoarthritis
AU782878B2 (en) * 2000-02-05 2005-09-08 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of erk
AU782775B2 (en) 2000-02-05 2005-08-25 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of ERK
GB0004888D0 (en) * 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US6608048B2 (en) * 2000-03-28 2003-08-19 Wyeth Holdings Tricyclic protein kinase inhibitors
AR028261A1 (es) 2000-03-28 2003-04-30 Wyeth Corp Inhibidores triciclicos de la proteina quinasa
SK17342002A3 (sk) 2000-06-26 2004-06-08 Pfizer Products Inc. Derivát pyrolo[2,3-d]pyrimidínu ako činidlo potlačujúce imunitu
WO2002043735A1 (en) 2000-11-29 2002-06-06 Parker Hughes Institute Inhibitors of thrombin induced platelet aggregation
US20020115173A1 (en) 2000-12-11 2002-08-22 Children's Medical Center Corporation Short peptides from the 'A-region' of protein kinases which selectively modulate protein kinase activity
CA2432114A1 (en) * 2000-12-20 2002-07-18 Sugen, Inc. 4-(hetero)aryl substituted indolinones
DK1343782T3 (da) 2000-12-21 2009-08-24 Smithkline Beecham Corp Pyrimidinaminer som angiogenesemodulatorer
FR2818642B1 (fr) 2000-12-26 2005-07-15 Hoechst Marion Roussel Inc Nouveaux derives de la purine, leur procede de preparation, leur application a titre de medicaments, compositions pharmaceutiques et nouvelle utilistion
US20040102455A1 (en) * 2001-01-30 2004-05-27 Burns Christopher John Method of inhibiting kinases
AUPR279101A0 (en) * 2001-01-30 2001-02-22 Cytopia Pty Ltd Protein kinase signalling
PL367130A1 (en) * 2001-05-29 2005-02-21 Schering Aktiengesellschaft Cdk inhibiting pyrimidines, production thereof and their use as medicaments
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
EP1399440B1 (en) * 2001-06-15 2009-06-03 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl)benzisoxazoles as protein kinase inhibitors
US6433018B1 (en) * 2001-08-31 2002-08-13 The Research Foundation Of State University Of New York Method for reducing hypertrophy and ischemia
AU2002334355A1 (en) 2001-09-06 2003-03-18 Prochon Biotech Ltd. Protein tyrosine kinase inhibitors
MXPA04002242A (es) * 2001-09-10 2005-03-07 Sugen Inc Derivados de 3-(4,5,6,7,-tetrahidroindol-2-ilmetiliden)-2-indolinona como inhibidores de cinasa.
WO2003030909A1 (en) 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
GT200200234A (es) 2001-12-06 2003-06-27 Compuestos cristalinos novedosos
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
US6998391B2 (en) * 2002-02-07 2006-02-14 Supergen.Inc. Method for treating diseases associated with abnormal kinase activity
EP1472233A1 (en) 2002-02-08 2004-11-03 SmithKline Beecham Corporation Pyrimidine compounds
CA2477505A1 (en) 2002-03-01 2003-09-12 Smithkline Beecham Corporation Diamino-pyrimidines and their use as angiogenesis inhibitors
ATE489384T1 (de) 2002-05-06 2010-12-15 Vertex Pharma Thiadiazole oder oxadiazole und ihre verwendung als jak proteinkinaseinhibitoren
WO2003095448A1 (en) 2002-05-06 2003-11-20 Bayer Pharmaceuticals Corporation Pyridinyl amino pyrimidine derivatives useful for treating hyper-proliferative disorders
KR20050013562A (ko) * 2002-05-30 2005-02-04 버텍스 파마슈티칼스 인코포레이티드 Ｊａｋ 및 ｃｄｋ2 프로테인 키나아제의 억제제
JP2005529954A (ja) 2002-06-17 2005-10-06 スミスクライン ビーチャム コーポレーション 化学プロセス
IL166241A0 (en) 2002-07-29 2006-01-15 Rigel Pharmaceuticals Inc Method of treating or preventing autoimmune diseases with 2,4-pyrimidinedinediamine compounds
US7304071B2 (en) 2002-08-14 2007-12-04 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
EP1562911B1 (en) * 2002-11-01 2010-01-06 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of jak and other protein kinases
ES2289349T3 (es) 2002-11-04 2008-02-01 Vertex Pharmaceuticals Incorporated Derivados de heteroaril-pirimidina como inhibidores de jak.
WO2004041810A1 (en) 2002-11-05 2004-05-21 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of jak and other protein kinases
CL2003002353A1 (es) 2002-11-15 2005-02-04 Vertex Pharma Compuestos derivados de diaminotriazoles, inhibidores d ela proteina quinasa; composicion farmaceutica; procedimiento de preparacion; y su uso del compuesto en el tratamiento de enfermedades de desordenes alergicos, proliferacion, autoinmunes, condic
RS20050380A (sr) 2002-11-21 2007-11-15 Pfizer Products Inc., Derivati 3-aminopiperidina i postupci njihove proizvodnje
NZ539901A (en) 2002-11-26 2007-09-28 Pfizer Prod Inc Method of treatment of transplant rejection
DE60326646D1 (de) 2002-12-18 2009-04-23 Vertex Pharma Benzisoxazolderivate, die sich als inhibitoren von proteinkinasen eigen
JP2006522124A (ja) 2003-04-03 2006-09-28 バーテックス　ファーマシューティカルズ　インコーポレイテッド プロテインキナーゼのインヒビターとして有用な組成物
JP2006528629A (ja) 2003-07-24 2006-12-21 メルク　エンド　カムパニー　インコーポレーテッド チロシンキナーゼ阻害薬
RS53109B (sr) * 2003-07-30 2014-06-30 Rigel Pharmaceuticals Inc. Jedinjenja 2,4 pirimidindiamina za upotrebu u tretmanu ili prevenciji autoimunih bolesti
WO2005016344A1 (en) 2003-08-14 2005-02-24 Pfizer Limited Piperazine derivatives for the treatment of hiv infections
PL2287156T3 (pl) 2003-08-15 2013-11-29 Novartis Ag 2,4-Di(fenyloamino)-pirymidyny stosowane w leczeniu chorób nowotworowych, chorób zapalnych i zaburzeń układu immunologicznego
TWI339206B (en) 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
EA009941B1 (ru) 2003-10-03 2008-04-28 Пфайзер Инк. Имидазопиридинзамещённые тропановые производные, обладающие активностью антагониста ccr5 рецептора, для лечения вируса иммунодефицита человека (вич) и воспаления
DE10349423A1 (de) 2003-10-16 2005-06-16 Schering Ag Sulfoximinsubstituierte Parimidine als CDK- und/oder VEGF-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
GB2432834A (en) 2004-01-12 2007-06-06 Cytopia Res Pty Ltd Selective Kinase Inhibitors
GB0407723D0 (en) * 2004-04-05 2004-05-12 Novartis Ag Organic compounds
WO2005122294A1 (ja) 2004-06-14 2005-12-22 Nec Corporation フィルム外装電気デバイス
ES2380550T3 (es) 2004-11-24 2012-05-16 Rigel Pharmaceuticals, Inc. Compuestos de espiro-2,4-pirimidindiamina y sus usos
NZ555947A (en) 2005-01-19 2010-11-26 Rigel Pharmaceuticals Inc Prodrugs of 2,4-pyrimidinediamine compounds and their uses
CA2604551A1 (en) * 2005-05-03 2007-03-08 Rigel Pharmaceuticals, Inc. Jak kinase inhibitors and their uses
BRPI0617241A2 (pt) * 2005-10-13 2016-11-08 Glaxo Group Ltd composto ou um sal ou solvato do mesmo, composição farmacêutica, método para tratar uma doença ou condição mediada por atividade syk inadequada em um mamífero, e, uso de um composto ou um sal ou solvato farmaceuticamente aceitável do mesmo
EP1960372B1 (en) * 2005-12-15 2015-12-09 Rigel Pharmaceuticals, Inc. Kinase inhibitors and their uses
GB0526246D0 (en) * 2005-12-22 2006-02-01 Novartis Ag Organic compounds
JP2009544592A (ja) 2006-07-21 2009-12-17 ノバルティス アクチエンゲゼルシャフト Ｊａｋキナーゼ阻害剤としての２，４−ジ（アリールアミノ）−ピリミジン−５−カルボキサミド化合物
US20110160185A9 (en) * 2007-04-02 2011-06-30 Jorge Salas Solana Pyrrolopyrimidine derivatives as jak3 inhibitors

Cited By (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011525192A (ja) * 2008-06-20 2011-09-15 ジェネンテック， インコーポレイテッド トリアゾロピリジンｊａｋ阻害剤化合物と方法
JP2011525193A (ja) * 2008-06-20 2011-09-15 ジェネンテック， インコーポレイテッド トリアゾロピリジンｊａｋ阻害剤化合物と方法
JP2015524828A (ja) * 2012-08-14 2015-08-27 シュエンジュウ・ファーマ・カンパニー・リミテッド 二環性基置換ピリミジン化合物
US9359371B2 (en) 2012-08-14 2016-06-07 Xuanzhu Pharma Co., Ltd. Bicyclic substituted pyrimidine compounds
JP2015534959A (ja) * 2012-10-19 2015-12-07 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Ｓｙｋの阻害剤
JP2016505041A (ja) * 2013-01-16 2016-02-18 シグナル ファーマシューティカルズ，エルエルシー 置換型ピロロピリミジン化合物、その組成物、およびこれらを用いた治療方法
JP2016530335A (ja) * 2013-09-18 2016-09-29 北京韓美薬品有限公司 Ｂｔｋ及び／又はｊａｋ３キナーゼの活性を抑制する化合物
US9840517B2 (en) 2013-09-18 2017-12-12 Beijing Hanmi Pharmaceutical Co., Ltd. Compound inhibiting activities of BTK and/or JAK3 kinases
US10273242B2 (en) 2013-09-18 2019-04-30 Beijing Hanmi Pharmaceutical Co., Ltd. Compound inhibiting activities of BTK and/or JAK3 kinases
JP2016534056A (ja) * 2013-10-21 2016-11-04 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ Ｂｔｋ阻害剤としてのヘテロアリール化合物及びその使用
JP2018514559A (ja) * 2015-04-29 2018-06-07 シアメン ユニヴァーシティー ピリミドピロール類化合物、その調製方法、医薬用組成物及びその応用
WO2016208595A1 (ja) * 2015-06-22 2016-12-29 小野薬品工業株式会社 Ｂｒｋ阻害化合物
JPWO2016208595A1 (ja) * 2015-06-22 2018-04-05 小野薬品工業株式会社 Ｂｒｋ阻害化合物
US11512087B2 (en) 2015-06-22 2022-11-29 Ono Pharmaceutical Co., Ltd. BRK inhibitory compound
US10377759B2 (en) 2015-06-22 2019-08-13 Ono Pharmaceutical Co., Ltd. Brk inhibitory compound
RU2719477C2 (ru) * 2015-06-22 2020-04-17 Оно Фармасьютикал Ко., Лтд. Соединение, ингибирующее brk
JP2018524356A (ja) * 2015-07-09 2018-08-30 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ Ｂｔｋ阻害剤としてのピリミジン誘導体及びその使用
US10562902B2 (en) 2015-08-13 2020-02-18 Beijing Hanmi Pharmaceutical Co., Ltd. IRAK4 inhibitor and use thereof
JP2018523672A (ja) * 2015-08-13 2018-08-23 北京韓美薬品有限公司 Ｉｒａｋ４阻害剤、及びその応用
JP2018525394A (ja) * 2015-08-13 2018-09-06 北京韓美薬品有限公司 Ｉｒａｋ４阻害剤、及びその応用
US10988482B2 (en) 2015-08-13 2021-04-27 Beijing Hanmi Pharmaceutical Co., Ltd. IRAK4 inhibitor and use thereof
JP2019518796A (ja) * 2016-06-27 2019-07-04 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−ジアミノ−ピリミジン化合物ならびに該化合物の作製法および使用法
US11524955B2 (en) 2016-06-27 2022-12-13 Rigel Pharmaceuticals, Inc. 2,4-diamino-pyrimidine compounds and method for making and using the compounds
JP7065840B2 (ja) 2016-06-27 2022-05-12 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－ジアミノ－ピリミジン化合物ならびに該化合物の作製法および使用法
JP2019532092A (ja) * 2016-10-28 2019-11-07 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｉｌ−１２、ｉｌ−２３および／またはｉｆｎアルファ応答の調節剤として有用なヘテロ二環化合物
JP7145850B2 (ja) 2016-10-28 2022-10-03 ブリストル－マイヤーズ スクイブ カンパニー Ｉｌ－１２、ｉｌ－２３および／またはｉｆｎアルファ応答の調節剤として有用なヘテロ二環化合物
JP2019536820A (ja) * 2016-12-01 2019-12-19 アプトセ バイオサイエンシーズ インコーポレイテッド Ｂｒａｄ４およびｊａｋ２の二重阻害剤としての縮合環式ピリミジン化合物、ならびにその使用に関する方法
JPWO2018117177A1 (ja) * 2016-12-21 2019-10-31 小野薬品工業株式会社 Ｂｒｋ阻害化合物
JP7047772B2 (ja) 2016-12-21 2022-04-05 小野薬品工業株式会社 Ｂｒｋ阻害化合物
WO2018117177A1 (ja) * 2016-12-21 2018-06-28 小野薬品工業株式会社 Ｂｒｋ阻害化合物
JP2022518723A (ja) * 2019-01-18 2022-03-16 ボロノイ・カンパニー・リミテッド ピロロピリジン誘導体およびタンパク質キナーゼ関連疾患の予防または治療での使用のためのその用途
JP2022523477A (ja) * 2019-01-18 2022-04-25 ボロノイ・カンパニー・リミテッド ピロロピリミジン誘導体及びこれを有効成分として含有するタンパク質キナーゼ関連疾患の予防又は治療用薬学的組成物
JP7564983B2 (ja) 2019-01-18 2024-10-10 ボロノイ インコーポレイテッド ピロロピリジン誘導体およびタンパク質キナーゼ関連疾患の予防または治療での使用のためのその用途
US12240844B2 (en) 2019-01-18 2025-03-04 Voronoi, Inc. Pyrrolopyridine derivative and use thereof in prevention and treatment of protein kinase-related disease
US12194048B2 (en) 2020-12-09 2025-01-14 Voronoi Co., Ltd. Use of pyrrolopyridine derivatives for preventing or treating inflammatory diseases

Also Published As

Publication number Publication date
US20130029944A1 (en) 2013-01-31
NZ588830A (en) 2012-11-30
IL208719A0 (en) 2010-12-30
US8258144B2 (en) 2012-09-04
US9139581B2 (en) 2015-09-22
WO2009131687A2 (en) 2009-10-29
AU2009238590A1 (en) 2009-10-29
US20090298823A1 (en) 2009-12-03
BRPI0910668A2 (pt) 2019-09-24
EP2271631A2 (en) 2011-01-12
CA2723185A1 (en) 2009-10-29
CN102066338A (zh) 2011-05-18
CN103224497A (zh) 2013-07-31
WO2009131687A3 (en) 2010-01-07
EP2271631B1 (en) 2018-07-04

Similar Documents

Publication Publication Date Title
US11414410B2 (en) Inhibitors of protein kinases
US9139581B2 (en) Inhibitors of protein kinases
JP5705720B2 (ja) Ｓｙｋまたはｊａｋキナーゼ阻害剤としての２，６−ジアミノ−ピリミジン−５−イル−カルボキサミド
KR101773313B1 (ko) ｓｙｋ 또는 ＪＡＫ 키나제 억제제로서의 ２,６－디아미노-피리미딘－５－일－카르복스아미드
US8318755B2 (en) Inhibitors of SYK and JAK protein kinases
US9102625B2 (en) Nicotinamides as JAK kinase modulators
AU2009251863B2 (en) 2, 6-diamino-pyrimidin- 5-yl-carboxamides as syk or JAK kinases inhibitors
HK1153192B (en) Inhibitors of protein kinases
HK1153192A (en) Inhibitors of protein kinases

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20120423

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20120423

A761 Written withdrawal of application

Free format text: JAPANESE INTERMEDIATE CODE: A761

Effective date: 20130426