ATE376543T1 - Indazol-verbindungen und pharmazeutische zusammensetzungen zur hemmung von proteinkinasen und verfahren zu ihrer verwendung - Google Patents

Indazol-verbindungen und pharmazeutische zusammensetzungen zur hemmung von proteinkinasen und verfahren zu ihrer verwendung

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Publication number
ATE376543T1
ATE376543T1 AT00943375T AT00943375T ATE376543T1 AT E376543 T1 ATE376543 T1 AT E376543T1 AT 00943375 T AT00943375 T AT 00943375T AT 00943375 T AT00943375 T AT 00943375T AT E376543 T1 ATE376543 T1 AT E376543T1
Authority
AT
Austria
Prior art keywords
methods
pharmaceutical compositions
protein kinases
inhibiting protein
indazole compounds
Prior art date
Application number
AT00943375T
Other languages
German (de)
English (en)
Inventor
Robert Kania
Steven Bender
Allen Borchardt
John Braganza
Stephan Cripps
Ye Hua
Michael Johnson
Theodore Johnson
Hiep Luu
Cynthia Palmer
Siegfried Reich
Anna Tempczyk-Russell
Min Teng
Christine Thomas
Michael Varney
Michael Wallace
Michael Collins
Original Assignee
Agouron Pharma
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22498654&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ATE376543(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Agouron Pharma filed Critical Agouron Pharma
Application granted granted Critical
Publication of ATE376543T1 publication Critical patent/ATE376543T1/de

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    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
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    • A61P17/06—Antipsoriatics
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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    • 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
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    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
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    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
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    • C07D405/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D405/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AT00943375T 1999-07-02 2000-06-30 Indazol-verbindungen und pharmazeutische zusammensetzungen zur hemmung von proteinkinasen und verfahren zu ihrer verwendung ATE376543T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US14213099P 1999-07-02 1999-07-02

Publications (1)

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ATE376543T1 true ATE376543T1 (de) 2007-11-15

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AT00943375T ATE376543T1 (de) 1999-07-02 2000-06-30 Indazol-verbindungen und pharmazeutische zusammensetzungen zur hemmung von proteinkinasen und verfahren zu ihrer verwendung

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EP (2) EP1614683B1 (enExample)
JP (2) JP3878849B2 (enExample)
KR (1) KR100529639B1 (enExample)
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AT (1) ATE376543T1 (enExample)
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Families Citing this family (367)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL199802B1 (pl) 1999-02-10 2008-10-31 Astrazeneca Ab Pochodne chinazoliny, sposoby ich wytwarzania, ich kompozycje farmaceutyczne i ich zastosowania
PE20010306A1 (es) * 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
WO2001047922A2 (en) 1999-12-24 2001-07-05 Aventis Pharma Limited Azaindoles
AU2001229727B2 (en) 2000-02-07 2004-10-14 Bristol-Myers Squibb Co. 3-aminopyrazole inhibitors of cyclin dependent kinases
EP1264820A4 (en) * 2000-03-14 2004-09-15 Fujisawa Pharmaceutical Co amide compounds
ATE287886T1 (de) 2000-04-25 2005-02-15 Bristol Myers Squibb Co Verwendung von 5-thio, sulfinyl- und sulfonylpyrazolo 3,4-b) pyridinen als cyclin- abhängige kinase-hemmer
AU7652101A (en) 2000-08-09 2002-02-18 Astrazeneca Ab Cinnoline compounds
BR0113056A (pt) 2000-08-09 2003-07-08 Astrazeneca Ab Composto, processo papa a preparação do mesmo, composição farmacêutica, e, método para produzir um efeito antiangiogênico e/ou redutor da permeabilidade vascular em um animal de sangue quente, e, uso de um composto
ES2334641T3 (es) 2000-09-01 2010-03-15 Novartis Vaccines And Diagnostics, Inc. Derivados aza heterociclicos y su uso terapeutico.
NZ524717A (en) 2000-09-11 2004-09-24 Chiron Corp Quinolinone derivatives
HU230302B1 (hu) 2000-10-20 2015-12-28 Eisai R&D Management Co., Ltd. Nitrogéntartalmú aromás származékok és ezeket tartalmazó gyógyászati készítmények
TWI243164B (en) 2001-02-13 2005-11-11 Aventis Pharma Gmbh Acylated indanyl amines and their use as pharmaceuticals
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
JP2004536113A (ja) * 2001-07-03 2004-12-02 カイロン コーポレイション チロシンキナーゼおよびセリン／スレオニンキナーゼのインヒビターとしてのインダゾールベンズイミダゾール化合物
US7642278B2 (en) 2001-07-03 2010-01-05 Novartis Vaccines And Diagnostics, Inc. Indazole benzimidazole compounds
WO2003024969A1 (en) 2001-09-14 2003-03-27 Merck & Co., Inc. Tyrosine kinase inhibitors
EP1441725A1 (en) * 2001-10-26 2004-08-04 Aventis Pharmaceuticals Inc. Benzimidazoles and analogues and their use as protein kinases inhibitors
US6897208B2 (en) * 2001-10-26 2005-05-24 Aventis Pharmaceuticals Inc. Benzimidazoles
FR2831537B1 (fr) * 2001-10-26 2008-02-29 Aventis Pharma Sa Nouveaux derives de benzimidazoles, leur procede de preparation, leur application a titre de medicament, compositions pharmaceutiques et nouvelle utilisation
FR2831536A1 (fr) * 2001-10-26 2003-05-02 Aventis Pharma Sa Nouveaux derives de benzimidazoles, leur procede de preparation, leur application a titre de medicament, compositions pharmaceutiques et nouvelle utilisation notamment comme inhibiteurs de kdr
NZ534171A (en) 2002-02-01 2007-06-29 Astrazeneca Ab Quinazoline compounds for the treatment of diseases associated with angiogenesis and/or increased vascular permeability
US7166293B2 (en) * 2002-03-29 2007-01-23 Carlsbad Technology, Inc. Angiogenesis inhibitors
US20050119278A1 (en) * 2002-05-16 2005-06-02 Che-Ming Teng Anti-angiogenesis methods
WO2004014368A1 (en) 2002-08-12 2004-02-19 Sugen, Inc. 3-pyrrolyl-pyridopyrazoles and 3-pyrrolyl-indazoles as novel kinase inhibitors
CA2496164C (en) 2002-08-23 2010-11-09 Chiron Corporation Benzimidazole quinolinones and uses thereof
US20060058366A1 (en) * 2002-12-03 2006-03-16 Kyowa Hakko Kogyo Co., Ltd. Jnk inhibitor
DK1585743T3 (da) * 2002-12-19 2007-09-17 Pfizer 2-(H-indazol-6-ylamino)-benzamid forbindelser som protein kinase inhibitorer, nyttige til behandling opthalmiske sygdomme
US7192976B2 (en) 2002-12-21 2007-03-20 Angion Biomedica Corporation Small molecule modulators of hepatocyte growth factor (scatter factor) activity
US7135575B2 (en) 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
EP1606283B1 (en) 2003-03-03 2008-10-08 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
EP1613320A1 (en) * 2003-04-03 2006-01-11 Pfizer Inc. Dosage forms comprising ag013736
EP1618133A1 (en) * 2003-04-17 2006-01-25 Pfizer Inc. Crystal structure of vegfrkd: ligand complexes and methods of use thereof
FR2854159B1 (fr) * 2003-04-25 2008-01-11 Aventis Pharma Sa Nouveaux derives de l'indole, leur preparation a titre de medicaments, compositions pharmaceutiques et notamment comme inhibiteurs de kdr
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
NZ544756A (en) 2003-07-22 2009-09-25 Astex Therapeutics Ltd 3,4-Disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinases (CDK) and glycogen synthase kinase-3 (GSK-3) modulators
AU2004259012C1 (en) * 2003-07-23 2012-08-02 Exelixis, Inc. Anaplastic lymphoma kinase modulators and methods of use
CA2518951A1 (en) * 2003-07-30 2005-02-10 Kyowa Hakko Kogyo Co., Ltd. Protein kinase inhibitors
ES2384568T3 (es) * 2003-07-30 2012-07-09 Kyowa Hakko Kirin Co., Ltd. Derivados de indazol
AU2004271978B2 (en) * 2003-09-04 2009-02-05 Merck & Co., Inc. Ophthalmic compositions for treating ocular hypertension
WO2005028624A2 (en) * 2003-09-15 2005-03-31 Plexxikon, Inc. Molecular scaffolds for kinase ligand development
US20050182061A1 (en) * 2003-10-02 2005-08-18 Jeremy Green Phthalimide compounds useful as protein kinase inhibitors
KR101224410B1 (ko) 2003-11-07 2013-01-23 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 퀴놀리논 화합물을 합성하는 방법
CN101337930B (zh) 2003-11-11 2010-09-08 卫材R&D管理有限公司 脲衍生物的制备方法
US20060004043A1 (en) * 2003-11-19 2006-01-05 Bhagwat Shripad S Indazole compounds and methods of use thereof
GB0330002D0 (en) 2003-12-24 2004-01-28 Astrazeneca Ab Quinazoline derivatives
AU2005219518A1 (en) * 2004-02-27 2005-09-15 F. Hoffmann-La Roche Ag Indazole derivatives and pharmaceutical compositions containing them
US20070185152A1 (en) * 2004-03-02 2007-08-09 Smithkline Beecham Corporation Inhibitors of akt activity
WO2005094823A1 (ja) * 2004-03-30 2005-10-13 Kyowa Hakko Kogyo Co., Ltd. Ｆｌｔ－３阻害剤
WO2005108370A1 (ja) * 2004-04-16 2005-11-17 Ajinomoto Co., Inc. ベンゼン化合物
CA2565965A1 (en) 2004-05-06 2006-07-27 Plexxikon, Inc. Pde4b inhibitors and uses therefor
WO2006009736A1 (en) 2004-06-17 2006-01-26 Wyeth Processes for preparing gonadotropin releasing hormone receptor antagonists
BRPI0512261A (pt) 2004-06-17 2008-02-26 Wyeth Corp antagonistas de receptor de hormÈnio liberador de gonadotropina
EP1786777A1 (en) * 2004-08-26 2007-05-23 Pfizer, Inc. Aminoheteroaryl compounds as protein tyrosine kinase inhibitors
US7605168B2 (en) 2004-09-03 2009-10-20 Plexxikon, Inc. PDE4B inhibitors
EP1797881B1 (en) 2004-09-17 2009-04-15 Eisai R&D Management Co., Ltd. Medicinal composition with improved stability and reduced gelation properties
EP1647549A1 (en) * 2004-10-14 2006-04-19 Laboratoire Theramex Indazoles, benzisoxazoles and benzisothiazoles as estrogenic agents
RU2007116150A (ru) * 2004-11-02 2008-11-10 Пфайзер Инк. (US) Полиморфные формы 6-[2-(метилкарбамоил)фенилсульфанил]-3-е-[2-[пиридин-2-ил)этенил]индазола
WO2006048745A1 (en) * 2004-11-02 2006-05-11 Pfizer Inc. Methods for preparing indazole compounds
RU2007120635A (ru) * 2004-11-02 2008-12-10 Пфайзер Инк. (US) Способы получения индазольных соединений
EP1831225A2 (en) 2004-11-19 2007-09-12 The Regents of the University of California Anti-inflammatory pyrazolopyrimidines
FR2878442B1 (fr) * 2004-11-29 2008-10-24 Aventis Pharma Sa THIENO(2,3-c)PYRAZOLES SUBSTITUES, PROCEDE DE PREPARATION, COMPOSITIONS LES CONTENANT ET UTILISATION
US20060142247A1 (en) * 2004-12-17 2006-06-29 Guy Georges Tricyclic heterocycles
JP5507049B2 (ja) 2004-12-30 2014-05-28 アステックス、セラピューティックス、リミテッド 医薬品
US7622583B2 (en) 2005-01-14 2009-11-24 Chemocentryx, Inc. Heteroaryl sulfonamides and CCR2
WO2006077424A1 (en) 2005-01-21 2006-07-27 Astex Therapeutics Limited Pharmaceutical compounds
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
WO2006077428A1 (en) 2005-01-21 2006-07-27 Astex Therapeutics Limited Pharmaceutical compounds
ES2336243T3 (es) * 2005-01-26 2010-04-09 Schering Corporation Derivados de 3-(indazol-5-il)-(1,2,4)triazina y composiciones similares como inhibidores de proteina quinasa para el tratamiento del cancer.
ES2426482T3 (es) * 2005-01-27 2013-10-23 Kyowa Hakko Kirin Co., Ltd. Inhibidor de IGF-1R
US7534796B2 (en) 2005-02-18 2009-05-19 Wyeth Imidazo[4,5-b]pyridine antagonists of gonadotropin releasing hormone receptor
US7582634B2 (en) 2005-02-18 2009-09-01 Wyeth 7-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor
US7538113B2 (en) 2005-02-18 2009-05-26 Wyeth 4-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor
PL1888556T3 (pl) 2005-05-17 2012-03-30 Novartis Ag Metody syntetyzowania związków heterocyklicznych
US7531542B2 (en) 2005-05-18 2009-05-12 Wyeth Benzooxazole and benzothiazole antagonists of gonadotropin releasing hormone receptor
US20080274192A1 (en) * 2005-05-19 2008-11-06 Pfizer Inc. Pharmaceutical Compositions Comprising an Amorphous Form of a Vegf-R-Inhibitor
ES2380795T3 (es) * 2005-05-20 2012-05-18 Vertex Pharmaceuticals, Inc. Pirrolopiridinas útiles como inhibidores de proteínas quinasas
US7582636B2 (en) 2005-05-26 2009-09-01 Wyeth Piperazinylimidazopyridine and piperazinyltriazolopyridine antagonists of Gonadotropin Releasing Hormone receptor
WO2006130673A1 (en) 2005-05-31 2006-12-07 Janssen Pharmaceutica, N.V. 3-benzoimidazolyl-pyrazolopyridines useful in treating kinase disorders
US7888381B2 (en) 2005-06-14 2011-02-15 Bristol-Myers Squibb Company Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity, and use thereof
WO2007015578A1 (ja) 2005-08-02 2007-02-08 Eisai R & D Management Co., Ltd. 血管新生阻害物質の効果を検定する方法
AR062545A1 (es) 2005-11-29 2008-11-19 Novartis Ag Formulaciones estables de quinolinonas
TW200732305A (en) * 2005-12-23 2007-09-01 Yung Shin Pharmaceutical Ind Cancer chemotherapy
CA2635813C (en) 2006-01-31 2014-01-07 Array Biopharma, Inc. Urea derivatives as kinase inhibitors and methods of use thereof
WO2007107346A1 (en) * 2006-03-23 2007-09-27 F. Hoffmann-La Roche Ag Substituted indazole derivatives, their manufacture and use as pharmaceutical agents
KR20150038395A (ko) 2006-04-04 2015-04-08 더 리젠트스 오브 더 유니이버시티 오브 캘리포니아 키나제 길항물질
ES2556173T3 (es) 2006-05-18 2016-01-13 Eisai R&D Management Co., Ltd. Agente antitumoral para un cáncer de tiroides
EP2036893A4 (en) 2006-06-30 2011-04-13 Kyowa Hakko Kirin Co Ltd ABL Kinase Inhibitor
US20090209537A1 (en) 2006-06-30 2009-08-20 Kyowa Hakko Kirin Co., Ltd. Aurora inhibitors
US8519135B2 (en) 2006-07-14 2013-08-27 Chemocentryx, Inc. Heteroaryl sulfonamides and CCR2/CCR9
JPWO2008020606A1 (ja) * 2006-08-16 2010-01-07 協和発酵キリン株式会社 血管新生阻害剤
CN101511793B (zh) * 2006-08-28 2011-08-03 卫材R&D管理有限公司 针对未分化型胃癌的抗肿瘤剂
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.
KR101445892B1 (ko) 2007-01-29 2014-09-29 에자이 알앤드디 매니지먼트 가부시키가이샤 미분화형 위암 치료용 조성물
JPWO2008111441A1 (ja) 2007-03-05 2010-06-24 協和発酵キリン株式会社 医薬組成物
CN103087043A (zh) * 2007-03-16 2013-05-08 中国人民解放军军事医学科学院放射与辐射医学研究所 具有抗增殖活性的苯甲酰胺类衍生物及其药用制剂
EP3252047B1 (en) * 2007-04-05 2022-05-11 Pfizer Products Inc. Crystalline forms of 6-[2-(methylcarbamoyl)phenylsulfanyl]-3-e-[2-(pyridin-2-yl)ethenyl]indazole suitable for the treatment of abnormal cell growth in mammals
DE602008003055D1 (de) 2007-05-31 2010-12-02 Nerviano Medical Sciences Srl Zyklokondensierte Azaindole, die als Kinase-Hemmer wirken
JP5306344B2 (ja) 2007-07-12 2013-10-02 ケモセントリックス， インコーポレイテッド 炎症の治療のためのｃｃｒ２モジュレーターとしての縮合ヘテロアリールピリジルおよびフェニルベンゼンスルホンアミド
WO2009046448A1 (en) 2007-10-04 2009-04-09 Intellikine, Inc. Chemical entities and therapeutic uses thereof
US8779197B2 (en) * 2007-10-11 2014-07-15 Vertex Pharmaceuticals Incorporated Aryl amides useful as inhibitors of voltage-gated sodium channels
KR20100093552A (ko) 2007-11-02 2010-08-25 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제 ｃ-세타로서의 [1ｈ-피라졸로[3,4-ｂ]피리딘-4-일]-페닐 또는 -피리딘-2-일 유도체
CN101848895B (zh) 2007-11-09 2013-10-23 卫材R&D管理有限公司 血管新生抑制物质和抗肿瘤性铂络合物的组合使用
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
KR101653842B1 (ko) 2008-01-04 2016-09-02 인텔리카인, 엘엘씨 특정 화학 물질, 조성물 및 방법
WO2009114870A2 (en) 2008-03-14 2009-09-17 Intellikine, Inc. Kinase inhibitors and methods of use
WO2009114874A2 (en) 2008-03-14 2009-09-17 Intellikine, Inc. Benzothiazole kinase inhibitors and methods of use
AU2009241038B2 (en) 2008-04-28 2011-12-22 Asahi Kasei Pharma Corporation Phenylpropionic acid derivative and use thereof
JP5788316B2 (ja) 2008-07-08 2015-09-30 インテリカイン， エルエルシー キナーゼインヒビターおよび使用方法
US20110224223A1 (en) 2008-07-08 2011-09-15 The Regents Of The University Of California, A California Corporation MTOR Modulators and Uses Thereof
EP2313093A4 (en) 2008-07-10 2012-03-28 Angion Biomedica Corp METHOD AND COMPOSITIONS FOR LOW-MOLECULAR MODULATORS OF THE HEPATOCYTE GROWTH FACTOR (SCATTER FACTOR) ACTIVITY
CA2738429C (en) 2008-09-26 2016-10-25 Intellikine, Inc. Heterocyclic kinase inhibitors
WO2010045542A2 (en) 2008-10-16 2010-04-22 The Regents Of The University Of California Fused ring heteroaryl kinase inhibitors
US8476282B2 (en) 2008-11-03 2013-07-02 Intellikine Llc Benzoxazole kinase inhibitors and methods of use
CN102574786A (zh) * 2009-04-02 2012-07-11 默克雪兰诺有限公司 二氢乳清酸脱氢酶抑制剂
CA2760791C (en) 2009-05-07 2017-06-20 Intellikine, Inc. Heterocyclic compounds and uses thereof
ES2835553T3 (es) 2009-08-10 2021-06-22 Biosplice Therapeutics Inc Inhibidores de indazol de la vía de señalización de Wnt y sus usos terapéuticos
US8980899B2 (en) 2009-10-16 2015-03-17 The Regents Of The University Of California Methods of inhibiting Ire1
WO2011073521A1 (en) 2009-12-15 2011-06-23 Petri Salven Methods for enriching adult-derived endothelial progenitor cells and uses thereof
CN102821607B (zh) 2009-12-21 2014-12-17 萨穆梅德有限公司 1H-吡唑并[3，4-b]吡啶及其治疗应用
AU2010343102B2 (en) 2009-12-29 2016-03-24 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
UY33236A (es) 2010-02-25 2011-09-30 Novartis Ag Inhibidores dimericos de las iap
MX2012010617A (es) * 2010-03-16 2012-10-05 Dana Farber Cancer Inst Inc Compuestos de imidazol y sus usos.
JP5951600B2 (ja) 2010-05-21 2016-07-13 インフィニティー ファーマシューティカルズ， インコーポレイテッド キナーゼ調節のための、化合物、組成物および方法
CA2802644C (en) 2010-06-25 2017-02-21 Eisai R & D Management Co., Ltd. Antitumor agent using compounds having kinase inhibitory effect in combination
WO2012012750A1 (en) 2010-07-23 2012-01-26 Trustees Of Boston University ANTI-DEsupR INHIBITORS AS THERAPEUTICS FOR INHIBITION OF PATHOLOGICAL ANGIOGENESIS AND TUMOR CELL INVASIVENESS AND FOR MOLECULAR IMAGING AND TARGETED DELIVERY
CN103298474B (zh) 2010-11-10 2016-06-29 无限药品股份有限公司 杂环化合物及其用途
WO2012080260A1 (en) 2010-12-13 2012-06-21 Novartis Ag Dimeric iap inhibitors
UY33794A (es) 2010-12-13 2012-07-31 Novartis Ag Inhibidores diméricos de las iap
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
AR084824A1 (es) 2011-01-10 2013-06-26 Intellikine Inc Procesos para preparar isoquinolinonas y formas solidas de isoquinolinonas
TWI592411B (zh) 2011-02-23 2017-07-21 英特爾立秦有限責任公司 激酶抑制劑之組合及其用途
JP2014509660A (ja) * 2011-04-01 2014-04-21 ユニバーシティ・オブ・ユタ・リサーチ・ファウンデイション ＰＤＫ１キナーゼの阻害剤としての置換３−（１Ｈ−ベンゾ｛ｄ｝イミダゾール−２−イル）−１Ｈ−インダゾール類似体
RU2580609C2 (ru) 2011-04-18 2016-04-10 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Противоопухолевое терапевтическое средство
EP3444363B1 (en) 2011-06-03 2020-11-25 Eisai R&D Management Co., Ltd. Biomarkers for prediciting and assessing responsiveness of thyroid and kidney cancer subjects to lenvatinib compounds
MX2014000648A (es) 2011-07-19 2014-09-25 Infinity Pharmaceuticals Inc Compuestos heterociclicos y sus usos.
AU2012284088B2 (en) 2011-07-19 2015-10-08 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
US8575336B2 (en) 2011-07-27 2013-11-05 Pfizer Limited Indazoles
US8785470B2 (en) 2011-08-29 2014-07-22 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
CA2846496C (en) 2011-09-02 2020-07-14 The Regents Of The University Of California Substituted pyrazolo[3,4-d]pyrimidines and uses thereof
CN102432595B (zh) * 2011-09-14 2013-09-25 湖南有色凯铂生物药业有限公司 N-吲哚-1-酰胺类化合物及作为抗癌药物的应用
HRP20190281T1 (hr) 2011-09-14 2019-05-31 Samumed, Llc Indazol-3-karboksamidi i njihova uporaba kao inhibitora signalizacijskog puta wnt/b-katenin
JP6026544B2 (ja) 2011-09-27 2016-11-16 ノバルティス アーゲー 変異体ｉｄｈの阻害剤としての３−ピリミジン−４−イル−オキサゾリジン−２−オン類
JP6106685B2 (ja) 2011-11-17 2017-04-05 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド Ｃ−ｊｕｎ−ｎ−末端キナーゼ（ｊｎｋ）の阻害剤
EP2788330A1 (en) 2011-12-05 2014-10-15 Novartis AG Cyclic urea derivatives as androgen receptor antagonists
FR2985257B1 (fr) * 2011-12-28 2014-02-14 Sanofi Sa Composes dimeres agonistes des recepteurs des fgfs (fgfrs), leur procede de preparation et leur application en therapeutique
EP2802658A2 (en) 2012-01-09 2014-11-19 Novartis AG Rnai agents to treat beta-catenin related diseases
US8815926B2 (en) 2012-01-26 2014-08-26 Novartis Ag Substituted pyrrolo[3,4-D]imidazoles for the treatment of MDM2/4 mediated diseases
PH12017500997A1 (en) 2012-04-04 2018-02-19 Samumed Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
PL2770994T3 (pl) 2012-05-04 2020-03-31 Samumed, Llc 1H-Pirazolo[3,4-b]pirydyny i ich zastosowania terapeutyczne
HUE042374T2 (hu) 2012-06-13 2019-06-28 Incyte Holdings Corp Szubsztituált triciklusos vegyületek mint FGFR inhibitorok
JP6231262B2 (ja) * 2012-06-20 2017-11-15 大日本印刷株式会社 ピタバスタチンカルシウムの前駆体の製造法
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
MX2015003874A (es) 2012-09-26 2015-12-16 Univ California Modulacion de ire1.
US10112927B2 (en) 2012-10-18 2018-10-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
WO2014063054A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
WO2014063061A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
WO2014071109A1 (en) 2012-11-01 2014-05-08 Infinity Pharmaceuticals, Inc. Treatment of cancers using pi3 kinase isoform modulators
CN103804349A (zh) * 2012-11-01 2014-05-21 杨子娇 一类治疗青光眼的化合物及其用途
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
AU2013364953A1 (en) 2012-12-21 2015-04-30 Eisai R&D Management Co., Ltd. Amorphous form of quinoline derivative, and method for producing same
EP2943198B1 (en) 2013-01-08 2019-07-17 Samumed, LLC 3-(benzoimidazol-2-yl)-indazole inhibitors of the wnt signaling pathway and therapeutic uses thereof
CN104370889A (zh) * 2013-01-24 2015-02-25 韩冰 一类降低眼压的化合物及其制备方法和用途
ES2716617T3 (es) * 2013-02-02 2019-06-13 Chia Tai Tianqing Pharmaceutical Group Co Ltd Inhibidor de proteína quinasa de 2-aminopiridina sustituida
PE20151428A1 (es) 2013-02-19 2015-09-24 Novartis Ag Derivados de benzotiofeno y composiciones de los mismos como degradantes selectivos de los receptores de estrogeno
MX2015012822A (es) 2013-03-14 2016-05-31 Novartis Ag 3-pirimidin-4-il-oxazolidin-2-onas- como inhibidores del idh mutante.
GEP201706699B (en) 2013-03-14 2017-07-10 Novartis Ag 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh
US9481667B2 (en) 2013-03-15 2016-11-01 Infinity Pharmaceuticals, Inc. Salts and solid forms of isoquinolinones and composition comprising and methods of using the same
WO2014147586A1 (en) 2013-03-22 2014-09-25 Novartis Ag 1-(2-(ethylamino)pyrimidin-4-yl)pyrrolidin-2-ones as inhibitors of mutant idh
KR102469849B1 (ko) 2013-04-19 2022-11-23 인사이트 홀딩스 코포레이션 Fgfr 저해제로서 이환식 헤테로사이클
WO2014185540A1 (en) 2013-05-14 2014-11-20 Eisai R&D Management Co., Ltd. Biomarkers for predicting and assessing responsiveness of endometrial cancer subjects to lenvatinib compounds
US20150018376A1 (en) * 2013-05-17 2015-01-15 Novartis Ag Pyrimidin-4-yl)oxy)-1h-indole-1-carboxamide derivatives and use thereof
CN103387565B (zh) * 2013-07-29 2014-10-29 苏州明锐医药科技有限公司 阿西替尼的制备方法
WO2015051241A1 (en) 2013-10-04 2015-04-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
PE20160685A1 (es) 2013-10-04 2016-07-23 Infinity Pharmaceuticals Inc Compuestos heterociclicos y usos de los mismos
EP3057955B1 (en) 2013-10-18 2018-04-11 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
EP3057956B1 (en) 2013-10-18 2021-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
CN103570696B (zh) * 2013-11-06 2016-02-24 湖南欧亚生物有限公司 一种阿西替尼中间体的制备方法以及在制备阿西替尼中的应用
WO2015067224A1 (en) 2013-11-08 2015-05-14 Zentiva, K.S. Salts of 6-[2-(methylcarbamoyl)phenylsulfanyl]-3-e-[2-(pyridin-2-yl)ethanyl] indazole
WO2015092634A1 (en) 2013-12-16 2015-06-25 Novartis Ag 1,2,3,4-tetrahydroisoquinoline compounds and compositions as selective estrogen receptor antagonists and degraders
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
WO2015107493A1 (en) 2014-01-17 2015-07-23 Novartis Ag 1 -pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2
ES2699354T3 (es) 2014-01-17 2019-02-08 Novartis Ag Derivados de 1-(triazin-3-il/piridazin-3-il)-piper(-azin)idina y composiciones de las mismas para inhibir la actividad de SHP2
CN113620958A (zh) 2014-03-19 2021-11-09 无限药品股份有限公司 用于治疗PI3K-γ介导的障碍的杂环化合物
EP3127900B1 (en) * 2014-03-31 2017-10-18 Senju Pharmaceutical Co., Ltd. Alkynyl indazole derivative and use thereof
WO2015160975A2 (en) 2014-04-16 2015-10-22 Infinity Pharmaceuticals, Inc. Combination therapies
US9862688B2 (en) 2014-04-23 2018-01-09 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
WO2015164614A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
WO2015181624A2 (en) 2014-05-28 2015-12-03 Idenix Pharmaceuticals, Inc Nucleoside derivatives for the treatment of cancer
CN104072484B (zh) * 2014-07-07 2016-07-06 渤海大学 氮-(4-(芳巯基)-1氢-吲唑-3-基)-1-(芳杂环取代)甲基亚胺类化合物及其药学上可接受的盐及其制备方法和应用
AR101198A1 (es) 2014-07-16 2016-11-30 Gruenenthal Gmbh Pirimidinas 2,5-sustituidas como inhibidores de pde4b
AR101196A1 (es) 2014-07-16 2016-11-30 Gruenenthal Gmbh Compuestos de pirimidina sustituidos
KR102329681B1 (ko) 2014-08-28 2021-11-23 에자이 알앤드디 매니지먼트 가부시키가이샤 고순도의 퀴놀린 유도체 및 이를 제조하는 방법
WO2016040188A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040182A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 2-(1h-indazol-3-yl)-1h-imidazo[4,5-c]pyridine and therapeutic uses thereof
WO2016040193A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof
WO2016040180A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040181A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040184A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040190A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof
WO2016040185A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 2-(1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine and therapeutic uses thereof
US9758517B2 (en) 2014-09-17 2017-09-12 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
US9708348B2 (en) 2014-10-03 2017-07-18 Infinity Pharmaceuticals, Inc. Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US10086000B2 (en) 2014-12-05 2018-10-02 Merck Sharp & Dohme Corp. Tricyclic compounds as inhibitors of mutant IDH enzymes
WO2016089797A1 (en) 2014-12-05 2016-06-09 Merck Sharp & Dohme Corp. Novel tricyclic compounds as inhibitors of mutant idh enzymes
US10508108B2 (en) 2014-12-05 2019-12-17 Merck Sharp & Dohme Corp. Tricyclic compounds as inhibitors of mutant IDH enzymes
MA41140A (fr) 2014-12-12 2017-10-17 Cancer Research Tech Ltd Dérivés de 2,4-dioxo-quinazoline-6-sulfonamide en tant qu'inhibiteurs de la parg
MA41179A (fr) * 2014-12-19 2017-10-24 Cancer Research Tech Ltd Composés inhibiteurs de parg
CA2972239A1 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
JP6852848B2 (ja) 2015-01-13 2021-03-31 国立大学法人京都大学 筋萎縮性側索硬化症の予防及び／又は治療剤
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
AU2016219822B2 (en) 2015-02-20 2020-07-09 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
KR20250024102A (ko) 2015-02-25 2025-02-18 에자이 알앤드디 매니지먼트 가부시키가이샤 퀴놀린 유도체의 고미 억제 방법
AU2015384801B2 (en) 2015-03-04 2022-01-06 Eisai R&D Management Co., Ltd. Combination of a PD-1 antagonist and a VEGFR/FGFR/RET tyrosine kinase inhibitor for treating cancer
CN107427521B (zh) 2015-03-27 2021-08-03 达纳-法伯癌症研究所股份有限公司 细胞周期蛋白依赖性激酶的抑制剂
US9580406B2 (en) 2015-04-28 2017-02-28 Signa S.A. De C.V. Processes for the preparation of axitinib
HK1252245A1 (zh) 2015-05-27 2019-05-24 Idenix Pharmaceuticals Llc 用於治疗癌症的核苷酸
KR20240034866A (ko) 2015-06-06 2024-03-14 클라우드브레이크 테라퓨틱스, 엘엘씨 익상편을 치료하기 위한 조성물 및 방법
WO2016201370A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
ES2886107T3 (es) 2015-06-16 2021-12-16 Prism Biolab Co Ltd Antineoplásico
CN112625028B (zh) 2015-06-19 2024-10-29 诺华股份有限公司 用于抑制shp2活性的化合物和组合物
WO2016203404A1 (en) 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
JP6878316B2 (ja) 2015-06-19 2021-05-26 ノバルティス アーゲー Ｓｈｐ２の活性を阻害するための化合物および組成物
GB201511382D0 (en) 2015-06-29 2015-08-12 Imp Innovations Ltd Novel compounds and their use in therapy
GB201511790D0 (en) 2015-07-06 2015-08-19 Iomet Pharma Ltd Pharmaceutical compound
US10206909B2 (en) 2015-08-03 2019-02-19 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
WO2017023984A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof
US10188634B2 (en) 2015-08-03 2019-01-29 Samumed, Llc 3-(3H-imidazo[4,5-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
US10350199B2 (en) 2015-08-03 2019-07-16 Samumed, Llc 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof
WO2017024015A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
US10285982B2 (en) 2015-08-03 2019-05-14 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
WO2017024010A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof
US10231956B2 (en) 2015-08-03 2019-03-19 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
US10166218B2 (en) 2015-08-03 2019-01-01 Samumed, Llc 3-(1H-indol-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
WO2017023975A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof
US10392383B2 (en) 2015-08-03 2019-08-27 Samumed, Llc 3-(1H-benzo[d]imidazol-2-yl)-1H-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017023972A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017023993A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-indol-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017023987A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof
WO2017023986A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-indol-2-yl)-1h-indazoles and therapeutic uses thereof
US10285983B2 (en) 2015-08-03 2019-05-14 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-B] pyridines and therapeutic uses thereof
US10519169B2 (en) 2015-08-03 2019-12-31 Samumed, Llc 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
US11453697B1 (en) 2015-08-13 2022-09-27 Merck Sharp & Dohme Llc Cyclic di-nucleotide compounds as sting agonists
BR112018002757A8 (pt) 2015-08-13 2023-04-11 Merck Sharp & Dohme Composto, composição farmacêutica, e, métodos para induzir uma resposta imune, para induzir uma produção de interferon tipo i e para tratamento de um distúrbio
SG11201801083UA (en) 2015-08-20 2018-03-28 Eisai R&D Man Co Ltd Tumor therapeutic agent
EP4019515A1 (en) 2015-09-09 2022-06-29 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
PH12018500554B1 (en) 2015-09-14 2024-01-24 Infinity Pharmaceuticals Inc Solid forms of isoquinolinone derivatives, process of making, compositions comprising, and methods of using the same
AU2016335675B2 (en) * 2015-10-07 2022-04-28 Aiviva Biopharma, Inc. Compositions and methods of treating skin fibrotic disorders
KR20180073629A (ko) * 2015-10-22 2018-07-02 셀비타 에스에이 피리돈 유도체 및 키나제 억제제로서의 그의 용도
KR20180080262A (ko) 2015-11-06 2018-07-11 사뮤메드, 엘엘씨 골관절염의 치료
EP3389783B1 (en) 2015-12-15 2024-07-03 Merck Sharp & Dohme LLC Novel compounds as indoleamine 2,3-dioxygenase inhibitors
WO2017161116A1 (en) 2016-03-17 2017-09-21 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as pi3k kinase inhibitors
AR108325A1 (es) 2016-04-27 2018-08-08 Samumed Llc Isoquinolin-3-il carboxamidas y preparación y uso de las mismas
JP6969800B2 (ja) 2016-05-04 2021-11-24 ジェノシアンス ファルマ 増殖性疾患の治療に使用される置換２，４−ジアミノ−キノリン誘導体
ES2933109T3 (es) 2016-06-01 2023-02-02 Biosplice Therapeutics Inc Proceso para preparar N-(5-(3-(7-(3-fluorofenil)-3h-imidazo[4,5-c]piridin-2-il)-1h-indazol-5-il)piridin-3-il)-3-metilbutanamida
WO2017214269A1 (en) 2016-06-08 2017-12-14 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
RU2744988C2 (ru) 2016-06-14 2021-03-17 Новартис Аг Соединения и композиции для подавления активности shp2
RU2754507C2 (ru) 2016-06-24 2021-09-02 Инфинити Фармасьютикалз, Инк. Комбинированная терапия
EP3523287B1 (en) 2016-10-04 2021-09-01 Merck Sharp & Dohme Corp. Benzo[b]thiophene compounds as sting agonists
CN110709082A (zh) 2016-10-21 2020-01-17 萨穆梅德有限公司 吲唑-3-甲酰胺的使用方法及其作为Wnt/β-连环蛋白信号传导途径抑制剂的用途
KR102558716B1 (ko) 2016-11-07 2023-07-21 사뮤메드, 엘엘씨 단일-투여량, 즉시-사용가능한 주사용 제제
US20190365788A1 (en) 2016-11-21 2019-12-05 Idenix Pharmaceuticals Llc Cyclic phosphate substituted nucleoside derivatives for the treatment of liver diseases
US10973809B2 (en) 2016-11-23 2021-04-13 Chemocentryx, Inc. Method of treating focal segmental glomerulosclerosis
CN110234403A (zh) 2017-01-27 2019-09-13 詹森生物科技公司 作为sting激动剂的环状二核苷酸
WO2018138684A1 (en) 2017-01-27 2018-08-02 Janssen Biotech, Inc. Cyclic dinucleotides as sting agonists
US12303505B2 (en) 2017-02-08 2025-05-20 Eisai R&D Management Co., Ltd. Tumor-treating pharmaceutical composition
US20190388407A1 (en) 2017-02-12 2019-12-26 Aiviva Biopharma, Inc. Multikinase inhibitors of vegf and tfg beta and uses thereof
WO2018151126A1 (ja) * 2017-02-14 2018-08-23 富士フイルム株式会社 インダゾール化合物の製造方法およびインダゾール化合物
EP3621624B1 (en) 2017-05-12 2023-08-30 Merck Sharp & Dohme LLC Cyclic di-nucleotide compounds as sting agonists
US20200197384A1 (en) 2017-05-16 2020-06-25 Eisai R&D Management Co., Ltd. Treatment of hepatocellular carcinoma
CN108947970B (zh) * 2017-05-18 2022-04-05 四川大学 吲唑类衍生物及其制备方法和用途
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
EP3661498A4 (en) 2017-08-04 2021-04-21 Merck Sharp & Dohme Corp. BENZO [B] THIOPHEN STING ANTAGONISTS FOR CANCER TREATMENT
RU2020109328A (ru) 2017-08-04 2021-09-06 Мерк Шарп И Доум Корп. Комбинации антагонистов pd-1 и бензо[b]тиофеновых агонистов sting для лечения рака
CN118903386A (zh) 2017-08-24 2024-11-08 诺和诺德股份有限公司 Glp-1组合物及其用途
US10435389B2 (en) 2017-09-11 2019-10-08 Krouzon Pharmaccuticals, Inc. Octahydrocyclopenta[c]pyrrole allosteric inhibitors of SHP2
WO2019067332A1 (en) 2017-09-27 2019-04-04 Merck Sharp & Dohme Corp. COMPOSITIONS AND METHODS FOR TREATING CANCER THROUGH A COMBINATION OF PROGRAMMED DEATH ANTIBODY ANTIBODIES (PD-1) AND A CXCR2 ANTAGONIST
MX386699B (es) 2017-10-11 2025-03-19 Chemocentryx Inc Tratamiento de glomerulosclerosis segmentaria focal con antagonistas ccr2
WO2019089412A1 (en) 2017-11-01 2019-05-09 Merck Sharp & Dohme Corp. Novel substituted tetrahydroquinolin compounds as indoleamine 2,3-dioxygenase (ido) inhibitors
AR113878A1 (es) 2017-11-14 2020-06-24 Merck Sharp & Dohme Compuestos de biarilo sustituido como inhibidores de indolamina 2,3-dioxigenasa (ido)
EP3709986B1 (en) 2017-11-14 2023-11-01 Merck Sharp & Dohme LLC Novel substituted biaryl compounds as indoleamine 2,3-dioxygenase (ido) inhibitors
US20210009630A1 (en) 2017-12-15 2021-01-14 Janssen Biotech, Inc. Cyclic dinucleotides as sting agonists
US11685761B2 (en) 2017-12-20 2023-06-27 Merck Sharp & Dohme Llc Cyclic di-nucleotide compounds as sting agonists
WO2019177873A1 (en) 2018-03-13 2019-09-19 Merck Sharp & Dohme Corp. Arginase inhibitors and methods of use
US11702430B2 (en) 2018-04-03 2023-07-18 Merck Sharp & Dohme Llc Aza-benzothiophene compounds as STING agonists
EP3774764A1 (en) 2018-04-03 2021-02-17 Merck Sharp&Dohme Corp. Benzothiophenes and related compounds as sting agonists
EP3781687A4 (en) 2018-04-20 2022-02-09 Merck Sharp & Dohme Corp. NEW RIG-I SUBSTITUTED AGONISTS: COMPOSITIONS AND METHODS THEREOF
EP4309737A3 (en) 2018-05-04 2024-03-27 Incyte Corporation Solid forms of an fgfr inhibitor and processes for preparing the same
EP3788046B1 (en) 2018-05-04 2025-12-10 Incyte Corporation Salts of an fgfr inhibitor
CN110452176A (zh) * 2018-05-07 2019-11-15 四川大学 吲唑类衍生物及其制备方法和用途
WO2019231870A1 (en) 2018-05-31 2019-12-05 Merck Sharp & Dohme Corp. Novel substituted [1.1.1] bicyclo compounds as indoleamine 2,3-dioxygenase inhibitors
US11274111B2 (en) 2018-06-20 2022-03-15 Merck Sharp & Dohme Corp. Arginase inhibitors and methods of use
JP7590185B2 (ja) 2018-06-25 2024-11-26 ダナ－ファーバー キャンサー インスティテュート， インコーポレイテッド Ｔａｉｒｅファミリーキナーゼインヒビターおよびそれらの使用
WO2020061103A1 (en) 2018-09-18 2020-03-26 Nikang Therapeutics, Inc. Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors
EP3856726A1 (en) 2018-09-25 2021-08-04 Black Diamond Therapeutics, Inc. Quinazoline derivatives as tyrosine kinase inhibitor, compositions, methods of making them and their use
CN113164776A (zh) 2018-09-25 2021-07-23 黑钻治疗公司 酪氨酸激酶抑制剂组合物、其制备方法和使用方法
MX2021003459A (es) 2018-09-29 2021-06-18 Novartis Ag Proceso de fabricacion de un compuesto para la inhibicion de la actividad de shp2.
US12091405B2 (en) 2018-11-01 2024-09-17 Merck Sharp & Dohme Llc Substituted pyrazole compounds as indoleamine 2,3-dioxygenase inhibitors
WO2020096871A1 (en) 2018-11-06 2020-05-14 Merck Sharp & Dohme Corp. Novel substituted tricyclic compounds as indoleamine 2,3-dioxygenase inhibitors
CN111205227A (zh) * 2018-11-22 2020-05-29 四川大学 3-乙烯基吲唑类衍生物及其制备方法和用途
WO2020112581A1 (en) 2018-11-28 2020-06-04 Merck Sharp & Dohme Corp. Novel substituted piperazine amide compounds as indoleamine 2, 3-dioxygenase (ido) inhibitors
US12240867B2 (en) 2018-12-18 2025-03-04 Merck Sharp & Dohme Llc Arginase inhibitors and methods of use
EP3902542A4 (en) 2018-12-28 2022-09-07 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
US12304897B2 (en) 2019-01-31 2025-05-20 Kyorin Pharmaceutical Co., Ltd. 15-PGDH inhibitors
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
WO2020205688A1 (en) 2019-04-04 2020-10-08 Merck Sharp & Dohme Corp. Inhibitors of histone deacetylase-3 useful for the treatment of cancer, inflammation, neurodegeneration diseases and diabetes
CN114026085A (zh) 2019-04-11 2022-02-08 安吉昂生物医药公司 (e)-3-[2-(2-噻吩基)乙烯基]-1h-吡唑的固体形式
EA202192731A1 (ru) 2019-04-18 2022-02-04 Синтон Б.В. СПОСОБ ПОЛУЧЕНИЯ АКСИТИНИБА, СПОСОБ ОЧИСТКИ ПРОМЕЖУТОЧНОГО СОЕДИНЕНИЯ 2-((3-ЙОД-1H-ИНДАЗОЛ-6-ИЛ)ТИО)-N-МЕТИЛБЕНЗАМИДА, СПОСОБ ОЧИСТКИ АКСИТИНИБА ЧЕРЕЗ HCl СОЛЬ АКСИТИНИБА, ТВЕРДАЯ ФОРМА HCl СОЛИ АКСИТИНИБА
US12290601B2 (en) 2019-05-09 2025-05-06 Synthon B.V. Pharmaceutical composition comprising axitinib
WO2020260547A1 (en) 2019-06-27 2020-12-30 Rigontec Gmbh Design method for optimized rig-i ligands
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
TW202120500A (zh) 2019-08-02 2021-06-01 美商梅爾莎納醫療公司 干擾素基因刺激蛋白（ｓｔｉｎｇ）激動劑化合物及用途
US12435046B2 (en) 2019-08-15 2025-10-07 Black Diamond Therapeutics, Inc. Alkynyl quinazoline compounds
WO2021035360A1 (en) * 2019-08-30 2021-03-04 Risen (Suzhou) Pharma Tech Co., Ltd. Prodrugs of the tyrosine kinase inhibitor for treating cancer
CN112442010B (zh) * 2019-08-30 2023-10-03 润佳（苏州）医药科技有限公司 一类前药化合物及其在治疗癌症方面的应用
CN112442011B (zh) * 2019-08-30 2023-11-14 润佳（苏州）医药科技有限公司 一种前药化合物及其在治疗癌症方面的应用
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021076602A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN112694474B (zh) * 2019-10-23 2022-03-18 四川大学 吲唑类衍生物及其制备方法和用途
KR20220131900A (ko) 2019-12-04 2022-09-29 인사이트 코포레이션 Fgfr 억제제의 유도체
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
EP4069683A1 (en) 2019-12-06 2022-10-12 Mersana Therapeutics, Inc. Dimeric compounds as sting agonists
US20220396577A1 (en) 2019-12-17 2022-12-15 Merck Sharp & Dohme Llc Novel substituted 1,3-8-triazaspiro[4,5] decane-2,4-dione compounds as indoleamine 2,3-dioxygenase (ido) and/or tryptophan 2,3-dioxygenase (tdo) inhibitors
WO2021141751A1 (en) 2020-01-07 2021-07-15 Merck Sharp & Dohme Corp. Arginase inhibitors and methods of use
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CN111829859B (zh) * 2020-01-20 2024-01-05 北京林业大学 一种高效杨树种子透明染色及其三维成像的方法
PL4097097T3 (pl) 2020-01-29 2025-05-12 Gilead Sciences, Inc. Związki modulujące glp-1r
KR20220143036A (ko) 2020-02-18 2022-10-24 노보 노르디스크 에이/에스 약학적 제형
BR102020005423A2 (pt) * 2020-03-18 2021-09-28 Faculdades Catolicas Compostos n-acil-hidrazônicos, uso no tratamento de agregopatias degenerativas amiloides e não-amiloides, e composição farmacêutica
WO2021195206A1 (en) 2020-03-24 2021-09-30 Black Diamond Therapeutics, Inc. Polymorphic forms and related uses
BR122022020762A2 (pt) 2020-04-02 2023-04-11 Mersana Therapeutics, Inc Conjugados de anticorpo-fármaco compreendendo agonistas de sting, seu uso e composição
PE20230680A1 (es) 2020-05-06 2023-04-21 Merck Sharp And Dohme Llc Inhibidores de il4i1 y metodos de uso
WO2021232367A1 (zh) * 2020-05-21 2021-11-25 四川大学 3-乙烯基吲唑类衍生物及其制备方法和用途
CN113943271B (zh) * 2020-07-15 2023-11-14 鲁南制药集团股份有限公司 一种阿昔替尼晶型及其制备方法
CN112028831A (zh) * 2020-09-24 2020-12-04 山东大学 一种苯并吡唑类化合物、其制备方法及作为抗肿瘤药物的应用
EP4247804A1 (en) 2020-11-20 2023-09-27 Gilead Sciences, Inc. Polyheterocyclic glp-1 r modulating compounds
JP7746384B2 (ja) * 2020-12-08 2025-09-30 ディスアーム セラピューティクス， インコーポレイテッド Ｓａｒｍ１のベンゾピラゾール阻害剤
AU2021409561A1 (en) 2020-12-22 2023-07-06 Nikang Therapeutics, Inc. Compounds for degrading cyclin-dependent kinase 2 via ubiquitin proteosome pathway
EP4277901A1 (en) 2021-01-13 2023-11-22 Monte Rosa Therapeutics, Inc. Isoindolinone compounds
WO2022170052A1 (en) 2021-02-05 2022-08-11 Black Diamond Therapeutics, Inc. Quinazoline derivatives, pyridopyrimidine derivatives, pyrimidopyrimidine derivatives, and uses thereof
CA3215903A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
WO2022219407A1 (en) 2021-04-14 2022-10-20 Monte Rosa Therapeutics Ag Isoindolinone compounds
EP4323349A1 (en) 2021-04-14 2024-02-21 Monte Rosa Therapeutics AG Isoindolinone amide compounds useful to treat diseases associated with gspt1
WO2022227015A1 (en) 2021-04-30 2022-11-03 Merck Sharp & Dohme Corp. Il4i1 inhibitors and methods of use
EP4352059A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2022261159A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CN117980310A (zh) 2021-07-14 2024-05-03 尼坎治疗公司 作为kras抑制剂的亚烷基衍生物
CN115701423B (zh) * 2021-08-02 2025-03-25 沈阳化工大学 三氟乙基硫醚（亚砜）取代苯类化合物的制备方法及其中间体
AU2023239344A1 (en) 2022-03-23 2024-10-10 Ideaya Biosciences, Inc. Piperazine substituted indazole compounds as inhibitors of parg
US12331026B2 (en) 2022-03-28 2025-06-17 Nikang Therapeutics, Inc. Sulfonamido derivatives as cyclin-dependent kinase 2 inhibitors
EP4282415A1 (en) 2022-05-26 2023-11-29 Genepharm S.A. A stable tablet composition of axitinib
CN119790053A (zh) 2022-06-08 2025-04-08 霖康疗法公司 作为细胞周期蛋白依赖性激酶2抑制剂的磺酰胺衍生物
WO2024032584A1 (zh) * 2022-08-08 2024-02-15 苏州必扬医药科技有限公司 一种蛋白酪氨酸激酶抑制剂及其医疗用途
IL320316A (en) 2022-11-11 2025-06-01 Nikang Therapeutics Inc Bifunctional compounds containing pyrimidine derivatives with substitutions at positions 2 and 5, for degradation of cyclin-dependent kinase 2 (CDK2) via the ubiquitin-proteasome pathway
TW202502311A (zh) 2023-03-29 2025-01-16 美商默沙東有限責任公司 Il4i1抑制劑及其使用方法
WO2025072462A1 (en) 2023-09-27 2025-04-03 Nikang Therapeutics, Inc. Sulfonamide derivatives as cyclin-dependent kinase 2 inhibitors
WO2025082316A1 (zh) * 2023-10-17 2025-04-24 苏州必扬医药科技有限公司 一种眼用制剂及其制备方法和应用
WO2025117616A1 (en) 2023-11-27 2025-06-05 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and cyclin-dependent kinase 4 via ubiquitin proteasome pathway
WO2025117981A1 (en) 2023-12-02 2025-06-05 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway
WO2025212828A1 (en) 2024-04-03 2025-10-09 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and cyclin-dependent kinase 4 via ubiquitin proteasome pathway
WO2025240536A1 (en) 2024-05-15 2025-11-20 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and/or cyclin-dependent kinase 4 via ubiquitin proteasome pathway
CN118994101B (zh) * 2024-08-08 2025-10-31 安徽医科大学 一种芳基吲唑环类化合物、制备方法、药物组合物及用途

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5625031A (en) * 1994-02-08 1997-04-29 Bristol-Myers Squibb Company Peptide inhibitors of the p33cdk2 and p34cdc2 cell cycle regulatory kinases and human papillomavirus E7 oncoprotein
US5631156A (en) * 1994-06-21 1997-05-20 The University Of Michigan DNA encoding and 18 KD CDK6 inhibiting protein
JPH10509708A (ja) * 1994-11-10 1998-09-22 コア セラピューティクス，インコーポレイティド プロテイン・キナーゼのインヒビターとして有用な医薬ピラゾール組成物
ZA951822B (en) * 1994-12-23 1996-09-26 Glaxo Group Ltd Chemical compounds
US5710173A (en) * 1995-06-07 1998-01-20 Sugen, Inc. Thienyl compounds for inhibition of cell proliferative disorders
US5733920A (en) * 1995-10-31 1998-03-31 Mitotix, Inc. Inhibitors of cyclin dependent kinases
US5760028A (en) * 1995-12-22 1998-06-02 The Dupont Merck Pharmaceutical Company Integrin receptor antagonists
WO1997034876A1 (en) * 1996-03-15 1997-09-25 Zeneca Limited Cinnoline derivatives and use as medicine
WO1997048697A1 (en) * 1996-06-19 1997-12-24 Rhone-Poulenc Rorer Limited Substituted azabicylic compounds and their use as inhibitors of the production of tnf and cyclic amp phosphodiesterase
CN1234031A (zh) * 1996-09-04 1999-11-03 辉瑞大药厂 吲唑衍生物及其作为磷酸二酯酶(pde)iv型和肿瘤坏死因子(tnf)产生的抑制剂的应用
SI20324A (sl) * 1997-10-27 2001-02-28 Agouron Pharmaceuticals, Inc. Substituirane 4-amino-tiazol-2-il spojine kot cdk inhibitorji
EP1040100A1 (en) * 1997-11-04 2000-10-04 Pfizer Products Inc. Therapeutically active compounds based on indazole bioisostere replacement of catechol in pde4 inhibitors
EA200000488A1 (ru) * 1997-11-04 2000-10-30 Пфайзер Продактс Инк. Замена катехина на биоизостеру индазола в терапевтически активных соединениях
PE20010306A1 (es) * 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa

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