HRP20020109B1 - Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use - Google Patents

Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use

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Publication number
HRP20020109B1
HRP20020109B1 HR20020109A HRP20020109A HRP20020109B1 HR P20020109 B1 HRP20020109 B1 HR P20020109B1 HR 20020109 A HR20020109 A HR 20020109A HR P20020109 A HRP20020109 A HR P20020109A HR P20020109 B1 HRP20020109 B1 HR P20020109B1
Authority
HR
Croatia
Prior art keywords
aryl
heteroaryl
substituted
definition
refers
Prior art date
Application number
HR20020109A
Other languages
English (en)
Croatian (hr)
Inventor
Steve Kania Robert
Lee Bender Steven
J. Borchardt Allen
F. Braganza John
James Cripps Stephan
Hua Ye
David Johnson Michael
Otto Theodore
The Luu Hiep
Louise Palmer Cynthia
Heinz Reich Siegfried
Maria Tempczyk-Russell Anna
Teng Min
Thomas Christine
David Varney Michael
Brennan Wallace Michael
Raymond Collins Michael
Original Assignee
Agouron Pharmaceuticals
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=HRP20020109(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Agouron Pharmaceuticals filed Critical Agouron Pharmaceuticals
Publication of HRP20020109A2 publication Critical patent/HRP20020109A2/hr
Publication of HRP20020109B1 publication Critical patent/HRP20020109B1/xx

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    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
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    • A61P19/00Drugs for skeletal disorders
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
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    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • A61P9/00Drugs for disorders of the cardiovascular system
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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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    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
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    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/12Heterocyclic 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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    • C07D405/04Heterocyclic 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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    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems

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  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Ophthalmology & Optometry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Obesity (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Emergency Medicine (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)
HR20020109A 1999-07-02 2000-06-30 Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use HRP20020109B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US14213099P 1999-07-02 1999-07-02
PCT/US2000/018263 WO2001002369A2 (en) 1999-07-02 2000-06-30 Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use

Publications (2)

Publication Number Publication Date
HRP20020109A2 HRP20020109A2 (en) 2003-12-31
HRP20020109B1 true HRP20020109B1 (en) 2008-07-31

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ID=22498654

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Application Number Title Priority Date Filing Date
HR20020109A HRP20020109B1 (en) 1999-07-02 2000-06-30 Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use

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JP (2) JP3878849B2 (enExample)
KR (1) KR100529639B1 (enExample)
CN (2) CN1234693C (enExample)
AP (1) AP1486A (enExample)
AR (2) AR035554A1 (enExample)
AT (1) ATE376543T1 (enExample)
AU (1) AU777701B2 (enExample)
BE (1) BE2013C015I2 (enExample)
BG (1) BG66070B1 (enExample)
BR (1) BRPI0012352B8 (enExample)
CA (1) CA2383630C (enExample)
CO (1) CO5190686A1 (enExample)
CR (2) CR6517A (enExample)
CY (3) CY1107148T1 (enExample)
CZ (1) CZ301667B6 (enExample)
DE (2) DE60037211T2 (enExample)
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EA (1) EA004460B1 (enExample)
EE (1) EE05585B1 (enExample)
ES (2) ES2296014T3 (enExample)
FR (1) FR13C0010I2 (enExample)
GE (1) GEP20063885B (enExample)
GT (1) GT200000107A (enExample)
HR (1) HRP20020109B1 (enExample)
HU (1) HU228502B1 (enExample)
IL (1) IL146710A0 (enExample)
IS (1) IS2791B (enExample)
JO (1) JO2319B1 (enExample)
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SI (2) SI1614683T1 (enExample)
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UA (1) UA66933C2 (enExample)
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Families Citing this family (368)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2674803C (en) 1999-02-10 2012-10-09 Astrazeneca Ab Quinazoline derivatives as angiogenesis inhibitors
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
AP1917A (en) 1999-12-24 2008-11-12 Aventis Pharma Ltd Azaindoles
AU2972701A (en) 2000-02-07 2001-08-14 Bristol Myers Squibb Co 3-aminopyrazole inhibitors of cyclin dependent kinases
AU2001241128A1 (en) * 2000-03-14 2001-09-24 Fujisawa Pharmaceutical Co. Ltd. Novel amide compounds
EP1278749B1 (en) 2000-04-25 2005-01-26 Bristol-Myers Squibb Company USE OF 5-THIO-, SULFINYL- AND SULFONYLPYRAZOLO 3,4-b]-PYRIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS
IL153947A0 (en) 2000-08-09 2003-07-31 Astrazeneca Ab Quinoline derivatives having vegf inhibiting activity
AU2001276521B2 (en) 2000-08-09 2006-05-25 Astrazeneca Ab Cinnoline compounds
ES2334641T3 (es) 2000-09-01 2010-03-15 Novartis Vaccines And Diagnostics, Inc. Derivados aza heterociclicos y su uso terapeutico.
ES2250480T3 (es) 2000-09-11 2006-04-16 Chiron Corporation Derivados de quinolinona como inhibidores de tirosina quinasa.
MX242553B (es) 2000-10-20 2006-12-06 Eisai Co Ltd Derivados aromaticos que contienen nitrogeno.
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
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
IL161576A0 (en) * 2001-10-26 2004-09-27 Aventis Pharma Inc Benzimidazoles and analogues and their use as protein kinases inhibitors
MXPA04007459A (es) 2002-02-01 2005-09-08 Astrazeneca Ab Compuestos de quinazolina.
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
MXPA05001688A (es) 2002-08-12 2005-04-19 Sugen Inc 3-pirrolil-piridopirazoles y 3-pirrolil-indazoles como inhibidores de cinasa novedosos.
BR0313743A (pt) 2002-08-23 2005-07-05 Chiron Corp Benzimidazol quinolinonas e usos destas
JPWO2004050088A1 (ja) * 2002-12-03 2006-03-30 協和醗酵工業株式会社 Jnk阻害剤
HRP20050559A2 (en) * 2002-12-19 2006-02-28 Pfizer Inc. 2-(1h-indazole-6-ylamino)-benzamide compounds as protein kinases inhibitors useful for the treatment of ophthalmic diseases
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
JP4617299B2 (ja) 2003-03-03 2011-01-19 アレイ バイオファーマ、インコーポレイテッド p38阻害剤及びその使用法
WO2004087152A1 (en) * 2003-04-03 2004-10-14 Pfizer Inc. Dosage forms comprising ag013736
WO2004092217A1 (en) * 2003-04-17 2004-10-28 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
PL1651612T3 (pl) 2003-07-22 2012-09-28 Astex Therapeutics Ltd Związki 3,4-pochodne 1h-pirazolu i ich zastosowanie jako kinazy zależne od cyklin (cdk) i modulatory kinazy syntazy glikogenu-3 (gsk-3)
US7872014B2 (en) 2003-07-23 2011-01-18 Exelixis, Inc. Anaplastic lymphoma kinase modulators and methods of use
MXPA05011420A (es) 2003-07-30 2005-12-12 Kyowa Hakko Kogyo Kk Derivados de indazol.
US20060281789A1 (en) * 2003-07-30 2006-12-14 Kyowa Hakko Kogyo Co., Ltd Protein kinase inhibitors
JP2007504236A (ja) * 2003-09-04 2007-03-01 メルク エンド カムパニー インコーポレーテッド 高眼圧症を治療するための眼用組成物
US20050164300A1 (en) * 2003-09-15 2005-07-28 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
CA2544186A1 (en) 2003-11-07 2005-05-26 Chiron Corporation Inhibition of fgfr3 and treatment of multiple myeloma with benzimidazole quinolinones
WO2005044788A1 (ja) 2003-11-11 2005-05-19 Eisai Co., Ltd. ウレア誘導体およびその製造方法
JP2007511618A (ja) * 2003-11-19 2007-05-10 シグナル ファーマシューティカルズ,エルエルシー インダゾール化合物およびタンパク質キナーゼ阻害剤としてのその使用方法
GB0330002D0 (en) 2003-12-24 2004-01-28 Astrazeneca Ab Quinazoline derivatives
RU2006134022A (ru) * 2004-02-27 2008-04-10 Ф.Хоффманн-Ля Рош Аг (Ch) Производные индазола и содержащие их фармацевтические композиции
EP1720855A4 (en) * 2004-03-02 2008-12-17 Smithkline Beecham Corp HEMMER OF ACT 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
WO2006078287A2 (en) 2004-05-06 2006-07-27 Plexxikon, Inc. Pde4b inhibitors and uses therefor
NZ552093A (en) 2004-06-17 2009-06-26 Wyeth Corp Processes for preparing gonadotropin releasing hormone receptor antagonists
AU2005264996A1 (en) * 2004-06-17 2006-01-26 Wyeth Gonadotropin releasing hormone receptor antagonists
CA2578075A1 (en) * 2004-08-26 2006-03-02 Pfizer Inc. Aminoheteroaryl compounds as protein tyrosine kinase inhibitors
AU2005279795A1 (en) 2004-09-03 2006-03-09 Plexxikon, Inc. Bicyclic heteroaryl PDE4B inhibitors
JP4834553B2 (ja) 2004-09-17 2011-12-14 エーザイ・アール・アンド・ディー・マネジメント株式会社 医薬組成物
EP1647549A1 (en) * 2004-10-14 2006-04-19 Laboratoire Theramex Indazoles, benzisoxazoles and benzisothiazoles as estrogenic agents
WO2006048745A1 (en) * 2004-11-02 2006-05-11 Pfizer Inc. Methods for preparing indazole compounds
EP1814859A2 (en) * 2004-11-02 2007-08-08 Pfizer, Inc. Methods for preparing indazole compounds
JP2008518904A (ja) * 2004-11-02 2008-06-05 ファイザー・インク 6−[2−(メチルカルバモイル)フェニルスルファニル]−3−e−[2−(ピリジン−2−イル)エテニル]インダゾールの多形体形態
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
CA2593993C (en) 2004-12-30 2014-07-29 Astex Therapeutics Limited Pyrazole compounds that modulate the activity of cdk, gsk and aurora kinases
US7622583B2 (en) 2005-01-14 2009-11-24 Chemocentryx, Inc. Heteroaryl sulfonamides and CCR2
US20090036435A1 (en) 2005-01-21 2009-02-05 Astex Therapeutics Limited Pharmaceutical Compounds
EP1845974A1 (en) 2005-01-21 2007-10-24 Astex Therapeutics Limited Pharmaceutical compounds
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
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.
CA2595514C (en) * 2005-01-26 2012-06-12 Schering Corporation Kinase inhibitors
ES2426482T3 (es) * 2005-01-27 2013-10-23 Kyowa Hakko Kirin Co., Ltd. Inhibidor de IGF-1R
US7538113B2 (en) 2005-02-18 2009-05-26 Wyeth 4-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor
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
US8222413B2 (en) 2005-05-17 2012-07-17 Novartis Ag Methods for synthesizing heterocyclic compounds
US7531542B2 (en) 2005-05-18 2009-05-12 Wyeth Benzooxazole and benzothiazole antagonists of gonadotropin releasing hormone receptor
EP1885338A1 (en) * 2005-05-19 2008-02-13 Pfizer, Inc. Pharmaceutical compostions comprising an amorphous form of a vegf-r inhibitor
ZA200710379B (en) * 2005-05-20 2009-05-27 Vertex Pharma Pyrrolopyridines useful as inhibitors of protein kinase
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
JP4989476B2 (ja) 2005-08-02 2012-08-01 エーザイ・アール・アンド・ディー・マネジメント株式会社 血管新生阻害物質の効果を検定する方法
EP1957074B1 (en) 2005-11-29 2014-03-19 Novartis AG Formulations of quinolinones
TW200732305A (en) * 2005-12-23 2007-09-01 Yung Shin Pharmaceutical Ind Cancer chemotherapy
AU2007210073B2 (en) 2006-01-31 2011-10-06 Array Biopharma Inc. Kinase inhibitors and methods of use thereof
EP2001882A1 (en) * 2006-03-23 2008-12-17 F. Hoffmann-La Roche AG Substituted indazole derivatives, their manufacture and use as pharmaceutical agents
DK2004654T3 (da) 2006-04-04 2013-07-22 Univ California Pyrazolopyrimidin derivater til anvendelse som kinase antagonister
EP2036557B1 (en) 2006-05-18 2015-10-21 Eisai R&D Management Co., Ltd. Antitumor agent for thyroid cancer
JPWO2008001885A1 (ja) 2006-06-30 2009-11-26 協和発酵キリン株式会社 Ablキナーゼ阻害剤
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.
WO2008093855A1 (ja) 2007-01-29 2008-08-07 Eisai R & D Management Co., Ltd. 未分化型胃癌治療用組成物
EP2133095A4 (en) 2007-03-05 2012-09-26 Kyowa Hakko Kirin Co Ltd PHARMACEUTICAL COMPOSITION
CN101730703B (zh) * 2007-03-16 2012-12-26 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
SG156088A1 (en) * 2007-04-05 2009-11-26 Pfizer Prod 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
CA2692761C (en) 2007-07-12 2013-04-30 Chemocentryx, Inc. Fused heteroaryl pyridyl and phenyl benzenesulfonamides as ccr2 modulators for the treament of inflammation
US20110160232A1 (en) 2007-10-04 2011-06-30 Pingda Ren Certain chemical entities and therapeutic uses thereof
AU2008310663A1 (en) * 2007-10-11 2009-04-16 Vertex Pharmaceuticals Incorporated Aryl amides useful as inhibitors of voltage-gated sodium channels
TW200924762A (en) 2007-11-02 2009-06-16 Vertex Pharma Kinase inhibitors
EP2218712B1 (en) 2007-11-09 2015-07-01 Eisai R&D Management Co., Ltd. Combination of anti-angiogenic substance and anti-tumor platinum complex
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
CN101965335B (zh) 2008-01-04 2015-01-14 英特利凯恩有限责任公司 某些化学实体、组合物和方法
US8637542B2 (en) 2008-03-14 2014-01-28 Intellikine, Inc. Kinase inhibitors and methods of use
US8993580B2 (en) 2008-03-14 2015-03-31 Intellikine Llc Benzothiazole kinase inhibitors and methods of use
MX2010011221A (es) 2008-04-28 2010-11-01 Asahi Kasei Pharma Corp Derivado del acido fenilpropionico y uso del mismo.
WO2010006072A2 (en) 2008-07-08 2010-01-14 The Regents Of The University Of California Mtor modulators and uses 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
US8772326B2 (en) 2008-07-10 2014-07-08 Anigion Biomedica Corp. Methods and compositions of small molecule modulators of hepatocyte growth factor (scatter factor) activity
EP2346508B1 (en) 2008-09-26 2016-08-24 Intellikine, LLC Heterocyclic kinase inhibitors
AU2009305669A1 (en) 2008-10-16 2010-04-22 The Regents Of The University Of California Fused ring heteroaryl kinase inhibitors
US8476431B2 (en) 2008-11-03 2013-07-02 Itellikine LLC Benzoxazole kinase inhibitors and methods of use
US9006454B2 (en) * 2009-04-02 2015-04-14 Merck Serono S.A. Dihydroorotate dehydrogenase inhibitors
WO2010129816A2 (en) 2009-05-07 2010-11-11 Intellikine, Inc. Heterocyclic compounds and uses thereof
PL2464232T3 (pl) 2009-08-10 2016-04-29 Samumed Llc Indazolowe inhibitory szlaku sygnałowego Wnt i ich zastosowania terapeutyczne
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
CA2986631C (en) 2009-12-21 2020-06-02 Samumed, Llc 1h-pyrazolo[3,4-.beta.]pyridines and thereapeutic uses thereof
WO2011090738A2 (en) 2009-12-29 2011-07-28 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
US8987275B2 (en) * 2010-03-16 2015-03-24 Dana-Farber Cancer Institute, Inc. Indazole compounds and their uses
ES2593256T3 (es) 2010-05-21 2016-12-07 Infinity Pharmaceuticals, Inc. Compuestos químicos, composiciones y métodos para las modulaciones de cinasas
RU2560683C2 (ru) 2010-06-25 2015-08-20 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Противоопухолевое средство, задействующее соединения с ингибирующим эффектом к киназам в комбинации
JP2013538191A (ja) 2010-07-23 2013-10-10 トラスティーズ オブ ボストン ユニバーシティ 病的血管新生および腫瘍細胞侵襲性の阻害のための治療法としてならびに分子イメージングおよび標的化送達のための抗DEsupR阻害剤
AU2011326427B2 (en) 2010-11-10 2016-01-07 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
JP2014501235A (ja) 2010-12-13 2014-01-20 ノバルティス アーゲー 二量体iap阻害剤
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
EP2663309B1 (en) 2011-01-10 2017-03-15 Infinity Pharmaceuticals, Inc. Processes for preparing isoquinolinones and solid forms of isoquinolinones
JP6130305B2 (ja) 2011-02-23 2017-05-17 インテリカイン, エルエルシー キナーゼ阻害剤の組み合わせおよびそれらの使用
EP2694060A4 (en) * 2011-04-01 2014-09-10 Univ Utah Res Found SUBSTITUTED 3- (1H-BENZO- {D} -IMIDAZOL-2-YL-) 1H-INDAZOL ANALOGUE AS PDK1 KINASE INHIBITOR
US8962650B2 (en) 2011-04-18 2015-02-24 Eisai R&D Management Co., Ltd. Therapeutic agent for tumor
JP6038128B2 (ja) 2011-06-03 2016-12-07 エーザイ・アール・アンド・ディー・マネジメント株式会社 レンバチニブ化合物に対する甲状腺癌対象及び腎臓癌対象の反応性を予測及び評価するためのバイオマーカー
EP2734520B1 (en) 2011-07-19 2016-09-14 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
HK1198475A1 (en) 2011-07-19 2015-05-08 无限药品股份有限公司 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
AU2012341028C1 (en) 2011-09-02 2017-10-19 Mount Sinai School Of Medicine 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
DK2755483T3 (en) 2011-09-14 2019-03-11 Samumed Llc INDAZOL-3-CARBOXAMIDES AND ITS USE AS WNT / B-CATENIN SIGNAL INHIBITORS
CU24269B1 (es) 2011-09-27 2017-08-08 Novartis Ag 3- pirimidin- 4-il- oxazolidin- 2- onas inhibidores de la idh mutante
EP3569598A1 (en) 2011-11-17 2019-11-20 Dana Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
US20140329858A1 (en) 2011-12-05 2014-11-06 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
JP6158833B2 (ja) 2012-01-09 2017-07-05 アローヘッド ファーマシューティカルズ インコーポレイテッド ベータ−カテニン関連疾患を処置するための有機組成物
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
JP6209593B2 (ja) 2012-05-04 2017-10-04 サミュメッド リミテッド ライアビリティ カンパニー 1H−ピラゾロ[3,4−b]ピリジンおよびそれらの治療的使用
SMT201700146T1 (it) 2012-06-13 2017-05-08 Incyte Holdings Corp Composti triciclici sostituiti come inibitori di fgfr
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
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
KR20150061651A (ko) 2012-09-26 2015-06-04 더 리젠츠 오브 더 유니버시티 오브 캘리포니아 Ire1의 조절
WO2014063068A1 (en) 2012-10-18 2014-04-24 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2014063061A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
WO2014063054A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
LT2914296T (lt) 2012-11-01 2018-09-25 Infinity Pharmaceuticals, Inc. Vėžio gydymas, panaudojant p13 kinazės izoformos moduliatorius
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
US9334239B2 (en) 2012-12-21 2016-05-10 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
CA2899968C (en) * 2013-02-02 2016-12-20 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Substituted 2-aminopyridine protein kinase inhibitor
RS57106B1 (sr) 2013-02-19 2018-06-29 Novartis Ag Derivati benzotiofena i njihove kompozicije kao selektivni degraderi estrogenskog receptora
CA2903979A1 (en) 2013-03-14 2014-09-18 Novartis Ag 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh
KR20150127197A (ko) 2013-03-14 2015-11-16 노파르티스 아게 돌연변이 idh의 억제제로서의 3-피리미딘-4-일-옥사졸리딘-2-온
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
CA2909207C (en) 2013-04-19 2021-11-02 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
MX368099B (es) 2013-05-14 2019-09-19 Eisai R&D Man Co Ltd Biomarcadores para predecir y evaluar el grado de respuesta de sujetos con cancer de endometrio a compuestos de tipo lenvatinib.
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
PH12016500582B1 (en) 2013-10-04 2023-06-30 Infinity Pharmaceuticals Inc Heterocyclic compounds and uses thereof
WO2015051241A1 (en) 2013-10-04 2015-04-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
EP3057955B1 (en) 2013-10-18 2018-04-11 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
AU2014337044A1 (en) 2013-10-18 2016-05-05 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
WO2015107494A1 (en) 2014-01-17 2015-07-23 Novartis Ag 1 -(triazin-3-yi_/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions thereof for inhibiting the activity of shp2
CN105899491B (zh) 2014-01-17 2019-04-02 诺华股份有限公司 用于抑制shp2活性的1-哒嗪-/三嗪-3-基-哌(-嗪)/啶/吡咯烷衍生物及其组合物
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
JP6701088B2 (ja) 2014-03-19 2020-05-27 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 Pi3k−ガンマ媒介障害の治療で使用するための複素環式化合物
CN106458920B (zh) * 2014-03-31 2019-02-15 千寿制药株式会社 炔基吲唑衍生物及其用途
WO2015160975A2 (en) 2014-04-16 2015-10-22 Infinity Pharmaceuticals, Inc. Combination therapies
WO2015164614A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
WO2015164604A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
AU2015265607A1 (en) 2014-05-28 2016-11-17 Idenix Pharmaceuticals Llc 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
AR101196A1 (es) 2014-07-16 2016-11-30 Gruenenthal Gmbh Compuestos de pirimidina sustituidos
AR101198A1 (es) 2014-07-16 2016-11-30 Gruenenthal Gmbh Pirimidinas 2,5-sustituidas como inhibidores de pde4b
JP6659554B2 (ja) 2014-08-28 2020-03-04 エーザイ・アール・アンド・ディー・マネジメント株式会社 高純度キノリン誘導体およびその製造方法
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
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
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
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
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
SG11201702119PA (en) 2014-09-17 2017-04-27 Quanticel Pharmaceuticals Inc Histone demethylase inhibitors
WO2016054491A1 (en) 2014-10-03 2016-04-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
EP3226690B1 (en) 2014-12-05 2020-05-20 Merck Sharp & Dohme Corp. Novel tricyclic compounds as inhibitors of mutant idh enzymes
US10442819B2 (en) 2014-12-05 2019-10-15 Merck Sharp & Dohme Corp. Tricyclic compounds as inhibitors of mutant IDH enzymes
WO2016089830A1 (en) 2014-12-05 2016-06-09 Merck Sharp & Dohme Corp. Novel 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
AU2015371251B2 (en) 2014-12-23 2020-06-11 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
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
UA121669C2 (uk) 2015-02-20 2020-07-10 Інсайт Корпорейшн Біциклічні гетероцикли як інгібітори fgfr
HUE064614T2 (hu) 2015-02-25 2024-04-28 Eisai R&D Man Co Ltd Eljárás egy kinolin-származék keserû ízének elnyomására
KR20240064733A (ko) 2015-03-04 2024-05-13 머크 샤프 앤드 돔 코포레이션 암을 치료하기 위한 pd-1 길항제 및 vegfr/fgfr/ret 티로신 키나제 억제제의 조합
HK1246645A1 (zh) 2015-03-27 2018-09-14 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
US10815264B2 (en) 2015-05-27 2020-10-27 Southern Research Institute Nucleotides for the treatment of cancer
CA2988293A1 (en) 2015-06-06 2016-12-15 Cloudbreak Therapeutics, Llc Compositions and methods for treating pterygium
US10702527B2 (en) 2015-06-12 2020-07-07 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
BR112017027227B1 (pt) 2015-06-16 2023-12-12 Eisai R&D Management Co., Ltd Agente anti-câncer
EP3310779B1 (en) 2015-06-19 2019-05-08 Novartis AG Compounds and compositions for inhibiting the activity of shp2
WO2016203406A1 (en) 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
EP3310771B1 (en) 2015-06-19 2020-07-22 Novartis AG Compounds and compositions for inhibiting the activity of shp2
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
US10463651B2 (en) 2015-08-03 2019-11-05 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-indazoles and therapeutic uses thereof
WO2017024026A1 (en) 2015-08-03 2017-02-09 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
WO2017023986A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-indol-2-yl)-1h-indazoles and therapeutic uses thereof
WO2017024025A1 (en) 2015-08-03 2017-02-09 Sunil Kumar Kc 3-(1h-pyrrolo[2,3-c]pyridin-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
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
WO2017024003A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-pyrrolo[3,2-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
WO2017024004A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]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
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
WO2017023996A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof
WO2017023980A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-b]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
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
US11453697B1 (en) 2015-08-13 2022-09-27 Merck Sharp & Dohme Llc Cyclic di-nucleotide compounds as sting agonists
EA034786B1 (ru) 2015-08-13 2020-03-20 Мерк Шарп И Доум Корп. Циклические динуклеотидные соединения в качестве агонистов sting
JP6553726B2 (ja) 2015-08-20 2019-07-31 エーザイ・アール・アンド・ディー・マネジメント株式会社 腫瘍治療剤
US11142507B2 (en) 2015-09-09 2021-10-12 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
AU2016322552B2 (en) 2015-09-14 2021-03-25 Infinity Pharmaceuticals, Inc. Solid forms of isoquinolinone derivatives, process of making, compositions comprising, and methods of using the same
EP3359258A4 (en) * 2015-10-07 2019-08-21 AiViva Biopharma, Inc. COMPOSITIONS AND METHOD FOR THE TREATMENT OF FIBROTIC SKIN DISEASES
WO2017068064A1 (en) * 2015-10-22 2017-04-27 Selvita S.A. Pyridone derivatives and their use as kinase inhibitors
CA3004297A1 (en) 2015-11-06 2017-05-11 Samumed, Llc 2-(1h-indazol-3-yl)-3h-imidazo[4,5-c]pyridines and their anti-inflammatory uses thereof
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
CA3023032A1 (en) 2016-05-04 2017-11-09 Genoscience Pharma Substituted 2,4-diamino-quinoline derivatives for use in the treatment of proliferative diseases
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
CN109561985B (zh) 2016-06-02 2022-03-04 拨云生物医药科技(广州)有限公司 使用尼达尼布改善青光眼手术成功情况的组合物和方法
WO2017214269A1 (en) 2016-06-08 2017-12-14 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
KR102457146B1 (ko) 2016-06-14 2022-10-19 노파르티스 아게 Shp2의 활성을 억제하기 위한 화합물 및 조성물
BR112018077021A2 (pt) 2016-06-24 2019-04-02 Infinity Pharmaceuticals, Inc. terapias de combinação
SI3523287T1 (sl) 2016-10-04 2021-11-30 Merck Sharp & Dohme Corp. Benzo(b)tiofenske spojine kot agonisti STING
EP3528808B1 (en) 2016-10-21 2021-10-06 BioSplice Therapeutics, Inc. Methods of using indazole-3-carboxamides and their use as wnt/b-catenin signaling pathway inhibitors
JP7630905B2 (ja) 2016-11-07 2025-02-18 バイオスプライス セラピューティクス インコーポレイテッド 単回用量の調整済み注射用製剤
EP3541825A1 (en) 2016-11-21 2019-09-25 Idenix Pharmaceuticals LLC. Cyclic phosphate substituted nucleoside derivatives for the treatment of liver diseases
IL294410B2 (en) 2016-11-23 2024-02-01 Chemocentryx Inc Method of treating focal segmental glomerulosclerosis
EP3573718B1 (en) 2017-01-27 2022-06-01 Janssen Biotech, Inc. Cyclic dinucleotides as sting agonists
EP3573717B1 (en) 2017-01-27 2021-07-28 Janssen Biotech, Inc. Cyclic dinucleotides as sting agonists
KR102539920B1 (ko) 2017-02-08 2023-06-05 에자이 알앤드디 매니지먼트 가부시키가이샤 종양-치료용 약제학적 조성물
US20190388407A1 (en) 2017-02-12 2019-12-26 Aiviva Biopharma, Inc. Multikinase inhibitors of vegf and tfg beta and uses thereof
JP6803410B2 (ja) 2017-02-14 2020-12-23 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
US11466047B2 (en) 2017-05-12 2022-10-11 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
CN108947961B (zh) * 2017-05-18 2021-06-04 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
JP2020529421A (ja) 2017-08-04 2020-10-08 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. がんの処置のためのPD−1アンタゴニストおよびベンゾ[b]チオフェンSTINGアゴニストの組み合わせ
EP3661498A4 (en) 2017-08-04 2021-04-21 Merck Sharp & Dohme Corp. BENZO [B] THIOPHEN STING ANTAGONISTS FOR CANCER TREATMENT
RS65380B1 (sr) 2017-08-24 2024-04-30 Novo Nordisk As Glp-1 kompozicije i njihova upotreba
TW202517628A (zh) 2017-09-11 2025-05-01 美商克魯松藥物公司 Shp2之八氫環戊烷并[c]吡咯別構抑制劑
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
SG11202002975YA (en) 2017-10-11 2020-04-29 Chemocentryx Inc Treatment of focal segmental glomerulosclerosis with ccr2 antagonists
US12275729B2 (en) 2017-11-01 2025-04-15 Merck Sharp & Dohme Llc Substituted tetrahydroquinolin compounds as indoleamine 2,3-dioxygenase (IDO) inhibitors
US10647705B2 (en) 2017-11-14 2020-05-12 Merck Sharp & Dohme Corp. Substituted biaryl compounds as indoleamine 2,3-dioxygenase (IDO) inhibitors
WO2019099294A1 (en) 2017-11-14 2019-05-23 Merck Sharp & Dohme Corp. Novel substituted biaryl compounds as indoleamine 2,3-dioxygenase (ido) inhibitors
AU2018386222B2 (en) 2017-12-15 2023-04-20 Janssen Biotech, Inc. Cyclic dinucleotides as sting agonists
EP3727401A4 (en) 2017-12-20 2022-04-06 Merck Sharp & Dohme Corp. 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
AU2019248545B2 (en) 2018-04-03 2022-08-11 Merck Sharp & Dohme Llc Benzothiophenes and related compounds as sting agonists
US11702430B2 (en) 2018-04-03 2023-07-18 Merck Sharp & Dohme Llc Aza-benzothiophene compounds as STING agonists
WO2019204179A1 (en) 2018-04-20 2019-10-24 Merck Sharp & Dohme Corp. Novel substituted rig-i agonists: compositions and methods thereof
SMT202400507T1 (it) 2018-05-04 2025-01-14 Incyte Corp Forme solide di un inibitore di fgfr e procedimenti per preparare le stesse
SG11202010882XA (en) 2018-05-04 2020-11-27 Incyte Corp 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
WO2019245890A1 (en) 2018-06-20 2019-12-26 Merck Sharp & Dohme Corp. Arginase inhibitors and methods of use
CN112367991A (zh) 2018-06-25 2021-02-12 达纳-法伯癌症研究所股份有限公司 Taire家族激酶抑制剂及其用途
BR112021005082A2 (pt) 2018-09-18 2021-06-08 Nikang Therapeutics, Inc. derivados de anel tricíclico fundido como inibidores de src homologia-2 fosfatase
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
KR20210137422A (ko) 2018-09-25 2021-11-17 블랙 다이아몬드 테라퓨틱스, 인코포레이티드 티로신 키나아제 억제제로서의 퀴나졸린 유도체, 조성물, 이들의 제조 방법 및 이들의 용도
EP3856345A1 (en) 2018-09-29 2021-08-04 Novartis AG Process of manufacture of a compound for inhibiting the activity of 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
US12264134B2 (en) 2018-11-28 2025-04-01 Merck Sharp & Dohme Llc Substituted piperazine amide compounds as indoleamine 2,3-dioxygenase (IDO) inhibitors
WO2020131598A1 (en) 2018-12-18 2020-06-25 Merck Sharp & Dohme Corp. 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
JP7532385B2 (ja) * 2019-01-31 2024-08-13 杏林製薬株式会社 15-pgdh阻害薬
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
WO2020210657A1 (en) 2019-04-11 2020-10-15 Angion Biomedica Corp. Solid forms of (e)-3-[2-(2-thienyl)vinyl]-1h-pyrazole
US20220194921A1 (en) 2019-04-18 2022-06-23 Synthon B.V. Process for preparation of axitinib
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
WO2021007269A1 (en) 2019-07-09 2021-01-14 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
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
EP4021912A4 (en) 2019-08-30 2023-08-23 Risen (Suzhou) Pharma Tech Co., Ltd. TYROSINE KINASE INHIBITOR PRODRUGS FOR THE TREATMENT OF CANCER
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
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3157361A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 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
WO2021113462A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Derivatives of an fgfr inhibitor
US11897891B2 (en) 2019-12-04 2024-02-13 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
EP4069683A1 (en) 2019-12-06 2022-10-12 Mersana Therapeutics, Inc. Dimeric compounds as sting agonists
WO2021126725A1 (en) 2019-12-17 2021-06-24 Merck Sharp & Dohme Corp. 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
CN115135304A (zh) 2020-02-18 2022-09-30 诺和诺德股份有限公司 Glp-1组合物及其用途
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
JP2023520513A (ja) 2020-04-02 2023-05-17 メルサナ セラピューティクス インコーポレイテッド Stingアゴニストを含む抗体薬物コンジュゲート
WO2021226003A1 (en) 2020-05-06 2021-11-11 Merck Sharp & Dohme Corp. Il4i1 inhibitors and methods of use
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
US11851419B2 (en) 2020-11-20 2023-12-26 Gilead Sciences, Inc. GLP-1R modulating compounds
US20240051939A1 (en) * 2020-12-08 2024-02-15 Disarm Therapeutics, Inc. Benzopyrazole inhibitors of sarm1
EP4267575A1 (en) 2020-12-22 2023-11-01 Nikang Therapeutics, Inc. Compounds for degrading cyclin-dependent kinase 2 via ubiquitin proteosome pathway
AU2022207648A1 (en) 2021-01-13 2023-07-27 Monte Rosa Therapeutics Ag 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
EP4323349A1 (en) 2021-04-14 2024-02-21 Monte Rosa Therapeutics AG Isoindolinone amide compounds useful to treat diseases associated with gspt1
WO2022219407A1 (en) 2021-04-14 2022-10-20 Monte Rosa Therapeutics Ag Isoindolinone compounds
WO2022227015A1 (en) 2021-04-30 2022-11-03 Merck Sharp & Dohme Corp. Il4i1 inhibitors and methods of use
WO2022261160A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
EP4352060A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
EP4370522A1 (en) 2021-07-14 2024-05-22 Nikang Therapeutics, Inc. Alkylidene derivatives as kras inhibitors
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
CN119255994A (zh) 2022-03-23 2025-01-03 艾迪亚生物科学公司 哌嗪取代的吲唑化合物作为parg抑制剂
WO2023192801A1 (en) 2022-03-28 2023-10-05 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
WO2023240024A1 (en) 2022-06-08 2023-12-14 Nikang Therapeutics, Inc. Sulfamide derivatives as cyclin-dependent kinase 2 inhibitors
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
TW202434563A (zh) 2022-11-11 2024-09-01 美商尼坎醫療公司 用於經由泛素蛋白酶體途徑降解週期蛋白依賴性激酶2的含有2,5-取代的嘧啶衍生物之雙功能化合物
WO2024206357A1 (en) 2023-03-29 2024-10-03 Merck Sharp & Dohme Llc Il4i1 inhibitors and methods of use
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
TW202527955A (zh) 2023-11-27 2025-07-16 美商尼坎醫療公司 用於經由泛素蛋白酶體途徑降解週期蛋白依賴性激酶2和週期蛋白依賴性激酶4的含有2,5-取代的嘧啶衍生物的雙功能化合物
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
AU700964B2 (en) * 1994-11-10 1999-01-14 Cor Therapeutics, Inc. Pharmaceutical pyrazole compositions useful as inhibitors of protein kinases
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
JP2000506880A (ja) * 1996-03-15 2000-06-06 ゼネカ・リミテッド シンノリン誘導体及びその使用
JP4373497B2 (ja) * 1996-06-19 2009-11-25 ローン−プーラン・ロレ・リミテツド 置換されたアザビシクロ化合物、ならびにtnfおよびサイクリックampホスホジエステラーゼ産生の阻害剤としてのそれらの使用
US6262040B1 (en) * 1996-09-04 2001-07-17 Pfizer Inc Indazole derivatives and their use as inhibitors of phosphodiesterase (PDE) type IV and the production of tumor necrosis factor (TNF)
EE200000289A (et) * 1997-10-27 2001-06-15 Agouron Pharmaceuticals, Inc. Asendatud 4-amino-tiasool-2-üüli ühendid kui tsükliinisõltuvusega kinaaside inhibiitorid
KR20010031783A (ko) * 1997-11-04 2001-04-16 데이비드 존 우드 Pde4 억제제 중 인다졸에 의한 카테콜의 생등입체성치환을 기재로 하는 치료상 활성인 화합물
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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