EE05585B1 - Indasoolihendid ja farmatseutilised kompositsioonid proteiini kinaaside inhibeerimiseks ning nende kasutamine - Google Patents

Indasoolihendid ja farmatseutilised kompositsioonid proteiini kinaaside inhibeerimiseks ning nende kasutamine

Info

Publication number
EE05585B1
EE05585B1 EEP200100717A EEP200100717A EE05585B1 EE 05585 B1 EE05585 B1 EE 05585B1 EE P200100717 A EEP200100717 A EE P200100717A EE P200100717 A EEP200100717 A EE P200100717A EE 05585 B1 EE05585 B1 EE 05585B1
Authority
EE
Estonia
Prior art keywords
inhibition
pharmaceutical compositions
protein kinases
indazole compounds
indazole
Prior art date
Application number
EEP200100717A
Other languages
English (en)
Estonian (et)
Inventor
Steven Kania Robert
Lee Bender Steven
J. Borchardt Allen
F. Braganza John
James Cripps Stephan
Hua Ye
David Johnson Michael
Otto Johnson Theodore Jr.
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, Inc.
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=EE05585(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Agouron Pharmaceuticals, Inc. filed Critical Agouron Pharmaceuticals, Inc.
Publication of EE200100717A publication Critical patent/EE200100717A/xx
Publication of EE05585B1 publication Critical patent/EE05585B1/xx

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
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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
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
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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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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D405/02—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
    • 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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    • C07D405/02—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
    • 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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    • C07D405/14—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 three or more hetero rings
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    • C07D417/06—Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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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    • C07D417/14—Heterocyclic 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 three or more hetero rings
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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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
    • C07D491/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Ophthalmology & Optometry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (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)
EEP200100717A 1999-07-02 2000-06-30 Indasoolihendid ja farmatseutilised kompositsioonid proteiini kinaaside inhibeerimiseks ning nende kasutamine EE05585B1 (et)

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
EE200100717A EE200100717A (et) 2003-02-17
EE05585B1 true EE05585B1 (et) 2012-10-15

Family

ID=22498654

Family Applications (1)

Application Number Title Priority Date Filing Date
EEP200100717A EE05585B1 (et) 1999-07-02 2000-06-30 Indasoolihendid ja farmatseutilised kompositsioonid proteiini kinaaside inhibeerimiseks ning nende kasutamine

Country Status (51)

Country Link
EP (2) EP1218348B1 (en:Method)
JP (2) JP3878849B2 (en:Method)
KR (1) KR100529639B1 (en:Method)
CN (2) CN1234693C (en:Method)
AP (1) AP1486A (en:Method)
AR (2) AR035554A1 (en:Method)
AT (1) ATE376543T1 (en:Method)
AU (1) AU777701B2 (en:Method)
BE (1) BE2013C015I2 (en:Method)
BG (1) BG66070B1 (en:Method)
BR (1) BRPI0012352B8 (en:Method)
CA (1) CA2383630C (en:Method)
CO (1) CO5190686A1 (en:Method)
CR (2) CR6517A (en:Method)
CY (3) CY1107148T1 (en:Method)
CZ (1) CZ301667B6 (en:Method)
DE (2) DE60037211T2 (en:Method)
DK (2) DK1614683T3 (en:Method)
DZ (1) DZ3191A1 (en:Method)
EA (1) EA004460B1 (en:Method)
EE (1) EE05585B1 (en:Method)
ES (2) ES2296014T3 (en:Method)
FR (1) FR13C0010I2 (en:Method)
GE (1) GEP20063885B (en:Method)
GT (1) GT200000107A (en:Method)
HR (1) HRP20020109B1 (en:Method)
HU (1) HU228502B1 (en:Method)
IL (1) IL146710A0 (en:Method)
IS (1) IS2791B (en:Method)
JO (1) JO2319B1 (en:Method)
LU (1) LU92154I2 (en:Method)
MA (1) MA26803A1 (en:Method)
ME (1) ME00385B (en:Method)
MX (1) MXPA01012795A (en:Method)
MY (2) MY139999A (en:Method)
NO (3) NO322507B1 (en:Method)
NZ (1) NZ516676A (en:Method)
OA (1) OA11980A (en:Method)
PA (1) PA8498001A1 (en:Method)
PE (1) PE20010306A1 (en:Method)
PL (1) PL212108B1 (en:Method)
PT (2) PT1218348E (en:Method)
RS (1) RS50339B (en:Method)
SI (2) SI1218348T1 (en:Method)
SK (1) SK286936B6 (en:Method)
SV (1) SV2002000121A (en:Method)
TN (1) TNSN00146A1 (en:Method)
UA (1) UA66933C2 (en:Method)
UY (1) UY26231A1 (en:Method)
WO (1) WO2001002369A2 (en:Method)
ZA (1) ZA200110061B (en:Method)

Families Citing this family (361)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA01008182A (es) 1999-02-10 2003-08-20 Astrazeneca Ab Derivados de quinazolina como inhibidores de angiotensina.
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
BR0017038A (pt) 1999-12-24 2003-01-07 Aventis Pharma Ltd Azaindóis
ES2228905T3 (es) 2000-02-07 2005-04-16 Bristol-Myers Squibb Co. Inhibidores 3-aminopirazoles de quinasa dependientes de ciclinas.
AU2001241128A1 (en) * 2000-03-14 2001-09-24 Fujisawa Pharmaceutical Co. Ltd. Novel amide compounds
AU2001253540A1 (en) 2000-04-25 2001-11-07 Bristol-Myers Squibb Company Use of 5-thio-, sulfinyl- and sulfonylpyrazolo(3,4-b)-pyridines as cyclin dependent kinase inhibitors
JP2004505964A (ja) 2000-08-09 2004-02-26 アストラゼネカ　アクチボラグ Ｖｅｇｆ阻害活性を有するキノリン誘導体
DE60137234D1 (de) 2000-08-09 2009-02-12 Astrazeneca Ab Cinnoline verbindungen
US6756383B2 (en) 2000-09-01 2004-06-29 Chiron Corporation Heterocyclic derivatives of quinolinone benimidazoles
AP1666A (en) 2000-09-11 2006-09-29 Chiron Corp Quinolinone derivatives as tyrosine kinase inhibitors.
DE60126997T2 (de) 2000-10-20 2007-10-25 Eisai R&D Management Co., Ltd. Stickstoff-enthaltende aromatische ringverbindungen zur behandlung von tumorerkrankungen
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
EP1401831A1 (en) * 2001-07-03 2004-03-31 Chiron Corporation Indazole benzimidazole compounds as tyrosine and serine/threonine kinase inhibitors
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
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
WO2003035065A1 (en) * 2001-10-26 2003-05-01 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
PT1474420E (pt) 2002-02-01 2012-05-10 Astrazeneca Ab Compostos 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
US7186716B2 (en) 2002-08-12 2007-03-06 Sugen, Inc. 3-Pyrrol-pyridopyrazoles and 3-pyrrolyl-indazoles as novel kinase inhibitors
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
PL377713A1 (pl) 2002-12-19 2006-02-06 Pfizer Inc. Związki 2-(1H-indazol-6-iloamino)benzamidowe jako inhibitory kinaz białkowych użyteczne w leczeniu chorób oczu
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
PL214032B1 (pl) 2003-03-03 2013-06-28 Array Biopharma Zwiazki bedace inhibitorami kinazy p38, kompozycja farmaceutyczna je zawierajaca oraz ich zastosowanie do wytwarzania leku do leczenia stanu, w którym posredniczy kinaza p38
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
EP1651612B9 (en) 2003-07-22 2012-09-05 Astex Therapeutics Limited 3,4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3) modulators
US7872014B2 (en) 2003-07-23 2011-01-18 Exelixis, Inc. Anaplastic lymphoma kinase modulators and methods of use
WO2005012257A1 (ja) 2003-07-30 2005-02-10 Kyowa Hakko Kogyo Co., Ltd. インダゾール誘導体
AU2004260759B2 (en) * 2003-07-30 2010-04-22 Kyowa Hakko Kirin Co., Ltd. Protein kinase inhibitors
US7494983B2 (en) * 2003-09-04 2009-02-24 Merck & Co. Inc. Ophthalmic compositions for treating ocular hypertension
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
KR20060111520A (ko) 2003-11-07 2006-10-27 카이론 코포레이션 Ｆｇｆｒ3의 억제 및 다발성 골수종의 치료
CN100450998C (zh) 2003-11-11 2009-01-14 卫材R&D管理有限公司 脲衍生物的制备方法
AU2004293443A1 (en) * 2003-11-19 2005-06-09 Signal Pharmaceuticals, Llc. Indazole Compounds and methods of use thereof as protein kinase inhibitors
GB0330002D0 (en) 2003-12-24 2004-01-28 Astrazeneca Ab Quinazoline derivatives
CN1922150A (zh) * 2004-02-27 2007-02-28 霍夫曼-拉罗奇有限公司 吲唑衍生物以及含有它们的药物组合物
EP1720855A4 (en) * 2004-03-02 2008-12-17 Smithkline Beecham Corp HEMMER OF ACT ACTIVITY
JPWO2005094823A1 (ja) * 2004-03-30 2007-08-16 協和醗酵工業株式会社 Ｆｌｔ−３阻害剤
JPWO2005108370A1 (ja) * 2004-04-16 2008-03-21 味の素株式会社 ベンゼン化合物
AU2005325271A1 (en) 2004-05-06 2006-07-27 Plexxikon, Inc. PDE4B inhibitors and uses therefor
JP2008503470A (ja) * 2004-06-17 2008-02-07 ワイス ゴナドトロピン放出ホルモン受容体アンタゴニストの製造法
AU2005264996A1 (en) * 2004-06-17 2006-01-26 Wyeth Gonadotropin releasing hormone receptor antagonists
BRPI0514687A (pt) * 2004-08-26 2008-06-17 Pfizer compostos amino heteroarila como inibidores de proteìna tirosina cinase
CN101048407A (zh) * 2004-09-03 2007-10-03 普莱希科公司 双环杂芳基pde4b抑制剂
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
RU2007114112A (ru) * 2004-11-02 2008-12-10 Пфайзер Инк. (US) Способ получения индазольных соединений
KR20070085727A (ko) * 2004-11-02 2007-08-27 화이자 인코포레이티드 인다졸 화합물의 제조 방법
WO2006048751A1 (en) * 2004-11-02 2006-05-11 Pfizer Inc. Polymorphic forms of 6-[2-(methylcarbamoyl)phenylsulfanyl]-3-e-[2-(pyridin-2-yl)ethenyl]indazole
US9512125B2 (en) 2004-11-19 2016-12-06 The Regents Of The University Of California Substituted pyrazolo[3.4-D] pyrimidines as anti-inflammatory agents
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
NZ555982A (en) 2004-12-30 2011-01-28 Astex Therapeutics Ltd 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
ES2552338T3 (es) 2005-01-21 2015-11-27 Astex Therapeutics Limited Compuestos farmacéuticos
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
AU2006207321B2 (en) 2005-01-21 2012-09-06 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.
JP4804480B2 (ja) * 2005-01-26 2011-11-02 シェーリング コーポレイション 癌の処置のためのプロテインキナーゼインヒビターとしての、３−（インダゾール−５−イル）−（１，２，４）トリアジン誘導体、および関連する化合物
AU2006209712B2 (en) 2005-01-27 2011-06-09 Kyowa Hakko Kirin Co., Ltd. IGF-1R inhibitor
US7534796B2 (en) 2005-02-18 2009-05-19 Wyeth Imidazo[4,5-b]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
US7582634B2 (en) 2005-02-18 2009-09-01 Wyeth 7-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor
ES2376347T3 (es) 2005-05-17 2012-03-13 Novartis Ag Métodos para sintetizar compuestos heteroc�?clicos.
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
WO2006127587A1 (en) * 2005-05-20 2006-11-30 Vertex Pharmaceuticals Incorporated 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
US7541367B2 (en) 2005-05-31 2009-06-02 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
JP2009517481A (ja) 2005-11-29 2009-04-30 ノバルティス アクチエンゲゼルシャフト キノリノンの製剤
TW200732305A (en) * 2005-12-23 2007-09-01 Yung Shin Pharmaceutical Ind Cancer chemotherapy
SI1981851T1 (sl) 2006-01-31 2012-05-31 Array Biopharma Inc Kinazni inhibitorji in postopki za njihovo uporabo
AU2007228940A1 (en) * 2006-03-23 2007-09-27 F. Hoffmann-La Roche Ag Substituted indazole derivatives, their manufacture and use as pharmaceutical agents
EP2004654B1 (en) 2006-04-04 2013-05-22 The Regents of the University of California Pyrazolopyrimidine derivatives for use as kinase antagonists
CN101443009A (zh) 2006-05-18 2009-05-27 卫材R&D管理有限公司 针对甲状腺癌的抗肿瘤剂
EP2036893A4 (en) 2006-06-30 2011-04-13 Kyowa Hakko Kirin Co Ltd ABL Kinase Inhibitor
EP2036894A4 (en) 2006-06-30 2011-01-12 Kyowa Hakko Kirin Co Ltd AURORA INHIBITOR
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
US8865737B2 (en) 2006-08-28 2014-10-21 Eisai R&D Management Co., Ltd. Antitumor agent for undifferentiated gastric cancer
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.
EP2119707B1 (en) 2007-01-29 2015-01-14 Eisai R&D Management Co., Ltd. Composition for treatment of undifferentiated-type of gastric cancer
TW200901975A (en) 2007-03-05 2009-01-16 Kyowa Hakko Kogyo Kk Pharmaceutical composition
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
CA2682859C (en) * 2007-04-05 2013-10-08 Pfizer Products Inc. Crystalline forms of 6-[2-(methylcarbamoyl)phenylsulfanyl]-3-e-[2-(pyridin-2-yl)ethenyl)indazole for treatment of abnormal cell growth in mammals
EP2002836B1 (en) 2007-05-31 2010-10-20 Nerviano Medical Sciences S.r.l. Cyclocondensed azaindoles active as kinase inhibitors
PT2175859E (pt) 2007-07-12 2012-06-06 Chemocentryx Inc Heteroarilpiridil- e fenil-benzenossulfonamidas condensadas como moduladores de ccr2 para o tratamento de inflamação
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
MX2010004819A (es) 2007-11-02 2010-07-05 Vertex Pharma Derivados de [1h-pirazolo[3,4-b]piridin-4-il]-fenilo o piridin-2-ilo como proteina cinasa c-theta.
AU2008325608B2 (en) 2007-11-09 2013-03-14 Eisai R & D Management Co., Ltd. Combination of anti-angiogenic substance and anti-tumor platinum complex
WO2009088990A1 (en) 2008-01-04 2009-07-16 Intellikine, Inc. Certain chemical entities, compositions and methods
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
WO2009114874A2 (en) 2008-03-14 2009-09-17 Intellikine, Inc. Benzothiazole kinase inhibitors and methods of use
JP5547099B2 (ja) 2008-03-14 2014-07-09 インテリカイン， エルエルシー キナーゼ阻害剤および使用方法
RU2479579C2 (ru) 2008-04-28 2013-04-20 Асахи Касеи Фарма Корпорейшн Производное фенилпропионовой кислоты и его применение
US20110224223A1 (en) 2008-07-08 2011-09-15 The Regents Of The University Of California, A California Corporation MTOR Modulators and Uses Thereof
BRPI0915231A2 (pt) 2008-07-08 2018-06-12 Intellikine Inc compostos inibidores de quinase e métodos de uso
CA2767331A1 (en) 2008-07-10 2010-01-14 Angion Biomedica Corp. Methods and compositions of small molecule modulators of hepatocyte growth factor (scatter factor) activity
US8703778B2 (en) 2008-09-26 2014-04-22 Intellikine Llc Heterocyclic kinase inhibitors
WO2010045542A2 (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
ES2882797T3 (es) 2009-04-02 2021-12-02 Merck Serono Sa Inhibidores de dihidroorotato deshidrogenasa
JP5789252B2 (ja) 2009-05-07 2015-10-07 インテリカイン， エルエルシー 複素環式化合物およびその使用
PT2464232E (pt) 2009-08-10 2016-02-01 Samumed Llc Inibidores de indazol da via de sinalização wnt e usos terapêuticos dos mesmos
WO2011047384A2 (en) 2009-10-16 2011-04-21 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
DK3001903T3 (en) 2009-12-21 2017-12-18 Samumed Llc 1H-PYRAZOLO [3,4 -?] PYRIDINES AND THERAPEUTIC APPLICATIONS THEREOF
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
CN103080093A (zh) * 2010-03-16 2013-05-01 达纳－法伯癌症研究所公司 吲唑化合物及其应用
EP2571357B1 (en) 2010-05-21 2016-07-06 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulation
CN102958523B (zh) 2010-06-25 2014-11-19 卫材R&D管理有限公司 使用具有激酶抑制作用的组合的抗肿瘤剂
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
US20130266590A1 (en) 2010-12-13 2013-10-10 Novartis Ag Dimeric iap inhibitors
UY33794A (es) 2010-12-13 2012-07-31 Novartis Ag Inhibidores diméricos de las iap
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
TWI659956B (zh) 2011-01-10 2019-05-21 美商英菲尼提製藥股份有限公司 製備異喹啉酮之方法及異喹啉酮之固體形式
US9295673B2 (en) 2011-02-23 2016-03-29 Intellikine Llc Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
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
MX2013009931A (es) 2011-04-18 2013-10-01 Eisai R&D Man Co Ltd Agentes terapeuticos contra tumores.
ES2841809T3 (es) 2011-06-03 2021-07-09 Eisai R&D Man Co Ltd Biomarcadores para pronosticar y evaluar el grado de respuesta de sujetos con cáncer de tiroides y de riñón a compuestos de lenvatinib
JP6027610B2 (ja) 2011-07-19 2016-11-16 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 複素環式化合物及びその使用
AR088218A1 (es) 2011-07-19 2014-05-21 Infinity Pharmaceuticals Inc Compuestos heterociclicos utiles como inhibidores de pi3k
US8575336B2 (en) 2011-07-27 2013-11-05 Pfizer Limited Indazoles
MX2014002542A (es) 2011-08-29 2014-07-09 Infinity Pharmaceuticals Inc Compuestos heterociclicos y usos de los mismos.
WO2013077921A2 (en) 2011-09-02 2013-05-30 The Regents Of The University Of California Substituted pyrazolo[3,4-d]pyrimidines and uses thereof
PE20141678A1 (es) 2011-09-14 2014-11-21 Samumed Llc Indazol-3-carboxamidas y su uso como inhibidores de la ruta de senalizacion de wnt/b-catenina
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
EP2771337B1 (en) 2011-09-27 2017-08-02 Novartis AG 3-(pyrimidin-4-yl)-oxazolidin-2-ones as inhibitors of mutant idh
EP2822935B1 (en) 2011-11-17 2019-05-15 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
CA2856824A1 (en) 2011-12-05 2013-06-13 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
HK1205758A1 (en) 2012-01-09 2015-12-24 Novartis Ag Rnai agents to treat beta-catenin related diseases
UY34591A (es) 2012-01-26 2013-09-02 Novartis Ag Compuestos de imidazopirrolidinona
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
RU2689141C2 (ru) 2012-05-04 2019-05-24 СЭМЬЮМЕД, ЭлЭлСи 1н-пиразоло[3,4-b]пиридины и их терапевтические применения
PT3495367T (pt) 2012-06-13 2020-11-12 Incyte Holdings Corp Compostos tricíclicos substituídos como inibidores de 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
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
JP2015532287A (ja) 2012-09-26 2015-11-09 ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア Ｉｒｅ１の調節
EP2909194A1 (en) 2012-10-18 2015-08-26 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
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
JP6584952B2 (ja) 2012-11-01 2019-10-02 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 Ｐｉ３キナーゼアイソフォームモジュレーターを用いる癌の治療
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
JPWO2014098176A1 (ja) 2012-12-21 2017-01-12 エーザイ・アール・アンド・ディー・マネジメント株式会社 キノリン誘導体のアモルファス及びその製造方法
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
EP3360870A1 (en) 2013-02-19 2018-08-15 Novartis AG Benzothiophene derivatives and compositions thereof as selective estrogen receptor degraders
MX355945B (es) 2013-03-14 2018-05-07 Novartis Ag 3-pirimidin-4-il-oxazolidin-2-onas como inhibidoras de idh mutante.
AU2014229283B2 (en) 2013-03-14 2016-07-28 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
US9533984B2 (en) 2013-04-19 2017-01-03 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
NZ714049A (en) 2013-05-14 2020-05-29 Eisai R&D Man 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
HUE057734T2 (hu) 2013-10-04 2022-06-28 Infinity Pharmaceuticals Inc Heterociklusos vegyületek és alkalmazásuk
WO2015051241A1 (en) 2013-10-04 2015-04-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
CN105849099B (zh) 2013-10-18 2020-01-17 达纳-法伯癌症研究所股份有限公司 周期蛋白依赖性激酶7(cdk7)的多环抑制剂
EP3057955B1 (en) 2013-10-18 2018-04-11 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
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
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
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
CA2943075C (en) 2014-03-19 2023-02-28 Infinity Pharmaceuticals, Inc. Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders
RU2667486C2 (ru) * 2014-03-31 2018-09-20 Сэндзю Фармацевтикал Ко., Лтд. Производное алкинилиндазола и его применение
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
US9862688B2 (en) 2014-04-23 2018-01-09 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
RS63559B1 (sr) 2014-08-28 2022-10-31 Eisai R&D Man Co Ltd Derivat hinolina velike čistoće i postupak za njegovu proizvodnju
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
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
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
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
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
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
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
JP6723663B2 (ja) 2014-09-17 2020-07-15 セルジーン クオンティセル リサーチ，インク． ヒストンデメチラーゼ阻害剤
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
EP3226689B1 (en) 2014-12-05 2020-01-15 Merck Sharp & Dohme Corp. Novel tricyclic compounds as inhibitors of mutant idh enzymes
EP3226688B1 (en) 2014-12-05 2020-07-01 Merck Sharp & Dohme Corp. Tricyclic compounds as inhibitors of mutant idh enzymes
US10086000B2 (en) 2014-12-05 2018-10-02 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
US10870651B2 (en) 2014-12-23 2020-12-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
EP4599890A2 (en) 2015-01-13 2025-08-13 Kyoto University Sunitinib for preventing and/or treating amyotrophic lateral sclerosis
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
TWI712601B (zh) 2015-02-20 2020-12-11 美商英塞特公司 作為fgfr抑制劑之雙環雜環
SG11201706630UA (en) 2015-02-25 2017-09-28 Eisai R&D Man Co Ltd Method for suppressing bitterness of quinoline derivative
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
US10550121B2 (en) 2015-03-27 2020-02-04 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
US9580406B2 (en) 2015-04-28 2017-02-28 Signa S.A. De C.V. Processes for the preparation of axitinib
EP3303361A1 (en) 2015-05-27 2018-04-11 Idenix Pharmaceuticals LLC Nucleotides for the treatment of cancer
WO2016200688A1 (en) 2015-06-06 2016-12-15 Cloudbreak Therapeutics, Llc Compositions and methods for treating pterygium
WO2016201370A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
SG11201710198YA (en) 2015-06-16 2018-01-30 Eisai R&D Man Co Ltd Anticancer agent
US10308660B2 (en) 2015-06-19 2019-06-04 Novartis Ag Compounds and compositions for inhibiting the activity of SHP2
CN107922388B (zh) 2015-06-19 2020-12-29 诺华股份有限公司 用于抑制shp2活性的化合物和组合物
US10975080B2 (en) 2015-06-19 2021-04-13 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
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
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
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
WO2017024021A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles 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
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
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
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
US10383861B2 (en) 2015-08-03 2019-08-20 Sammumed, 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
US10329309B2 (en) 2015-08-03 2019-06-25 Samumed, Llc 3-(3H-imidazo[4,5-B]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines 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
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
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
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
WO2017023988A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-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
TN2018000023A1 (en) 2015-08-13 2019-07-08 Merck Sharp & Dohme Cyclic di-nucleotide compounds as sting agonists.
ES2887426T3 (es) 2015-08-20 2021-12-22 Eisai R&D Man Co Ltd Lenvatinib combinado con etopósido e ifosfamida para su uso en el tratamiento de un tumor
EP3347018B1 (en) 2015-09-09 2021-09-01 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
WO2017048702A1 (en) 2015-09-14 2017-03-23 Infinity Pharmaceuticals, Inc. Solid forms of isoquinolinone derivatives, process of making, compositions comprising, and methods of using the same
WO2017062694A1 (en) * 2015-10-07 2017-04-13 Diane Tang-Liu Compositions and methods of treating skin fibrotic disorders
CA3002875A1 (en) * 2015-10-22 2017-04-27 Selvita S.A. Pyridone derivatives and their use as kinase inhibitors
US10899757B2 (en) 2015-11-06 2021-01-26 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
US10759806B2 (en) 2016-03-17 2020-09-01 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
EP3452465B1 (en) 2016-05-04 2020-11-04 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
US10919914B2 (en) 2016-06-08 2021-02-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
EP3468972B1 (en) 2016-06-14 2020-05-20 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
IL263680B1 (en) 2016-06-24 2025-06-01 Infinity Pharmaceuticals Inc Pi3k inhibitors for use in combination with a second therapeutic agent in treating, managing, or preventing cancer
SG10202008647TA (en) 2016-10-04 2020-10-29 Merck Sharp & Dohme BENZO[b]THIOPHENE COMPOUNDS AS STING AGONISTS
JP2019535672A (ja) 2016-10-21 2019-12-12 サミュメッド リミテッド ライアビリティ カンパニー インダゾール−３−カルボキサミドの使用方法およびｗｎｔ／β−カテニンシグナル伝達経路阻害剤としてのそれらの使用
WO2018085865A1 (en) 2016-11-07 2018-05-11 Samumed, Llc Single-dose, ready-to-use injectable formulations
EP3541825A1 (en) 2016-11-21 2019-09-25 Idenix Pharmaceuticals LLC. Cyclic phosphate substituted nucleoside derivatives for the treatment of liver diseases
KR102754341B1 (ko) 2016-11-23 2025-01-13 케모센트릭스, 인크. 국소 분절 사구체경화증의 치료 방법
AU2018212788A1 (en) 2017-01-27 2019-07-25 Janssen Biotech, Inc. Cyclic dinucleotides as STING agonists
CN110234404A (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
CA3044658A1 (en) 2017-02-08 2018-08-16 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
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
RU2019134940A (ru) 2017-05-16 2021-06-16 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Лечение гепатоцеллюлярной карциномы
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
WO2019027858A1 (en) 2017-08-04 2019-02-07 Merck Sharp & Dohme Corp. BENZO [B] STING THIOPHEN AGONISTS FOR THE TREATMENT OF CANCER
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
CN111050750B (zh) 2017-08-24 2024-09-24 诺和诺德股份有限公司 Glp-1组合物及其用途
EP3681879A1 (en) 2017-09-11 2020-07-22 Krouzon Pharmaceuticals, Inc. Octahydrocyclopenta[c]pyrrole allosteric inhibitors of shp2
US11052065B2 (en) 2017-09-27 2021-07-06 Merck Sharp & Dohme Corp. Compositions and methods for treating cancer with a combination of programmed death receptor (PD-1) antibodies and a CXCR2 antagonist
SG11202002975YA (en) 2017-10-11 2020-04-29 Chemocentryx Inc Treatment of focal segmental glomerulosclerosis with ccr2 antagonists
WO2019089412A1 (en) 2017-11-01 2019-05-09 Merck Sharp & Dohme Corp. Novel substituted tetrahydroquinolin 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
MX2020004930A (es) 2017-11-14 2020-08-27 Merck Sharp & Dohme Compuestos de biarilo sustituido novedosos como inhibidores de indolamina 2,3-dioxigenasa (ido).
BR112020010941A2 (pt) 2017-12-15 2020-11-17 Janssen Biotech, Inc. dinucleotídeos cíclicos como agonistas de sting
US11685761B2 (en) 2017-12-20 2023-06-27 Merck Sharp & Dohme Llc Cyclic di-nucleotide compounds as sting agonists
US12215116B2 (en) 2018-03-13 2025-02-04 Merck Sharp & Dohme Llc Arginase inhibitors and methods of use
CN111971277B (zh) 2018-04-03 2023-06-06 默沙东有限责任公司 作为sting激动剂的苯并噻吩及相关化合物
EP3774765A4 (en) 2018-04-03 2021-12-29 Merck Sharp & Dohme Corp. Aza-benzothiophene compounds as sting agonists
AU2019262579B2 (en) 2018-05-04 2024-09-12 Incyte Corporation Salts of an FGFR inhibitor
SI3788047T1 (sl) 2018-05-04 2024-11-29 Incyte Corporation Trdne oblike inhibitorja fgfr in postopki priprave le-teh
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
EP3810116B1 (en) 2018-05-31 2023-11-15 Merck Sharp & Dohme LLC 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
EP3810132A4 (en) 2018-06-25 2022-06-22 Dana-Farber Cancer Institute, Inc. TAIRE FAMILY KINASE INHIBITORS AND RELATED USES
TWI827677B (zh) 2018-09-18 2024-01-01 美商尼坎醫療公司 作為src同源-2磷酸酶抑制劑之稠合三環衍生物
EP3856349A1 (en) 2018-09-25 2021-08-04 Black Diamond Therapeutics, Inc. Tyrosine kinase inhibitor compositions, methods of making and methods of use
CA3113241A1 (en) 2018-09-25 2020-04-02 Black Diamond Therapeutics, Inc. Quinazoline derivatives as tyrosine kinase inhibitor, compositions, methods of making them and their use
EP4282416A3 (en) 2018-09-29 2024-03-06 Novartis AG Process of manufacture of a compound for inhibiting the activity of shp2
WO2020092183A1 (en) 2018-11-01 2020-05-07 Merck Sharp & Dohme Corp. Novel substituted pyrazole compounds as indoleamine 2,3-dioxygenase inhibitors
US12065438B2 (en) 2018-11-06 2024-08-20 Merck Sharp & Dohme Llc 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
EP3886845B1 (en) 2018-11-28 2024-09-04 Merck Sharp & Dohme LLC 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
WO2020140098A1 (en) 2018-12-28 2020-07-02 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
US12281109B2 (en) 2019-04-04 2025-04-22 Merck Sharp & Dohme Llc Inhibitors of histone deacetylase-3 useful for the treatment of cancer, inflammation, neurodegeneration diseases and diabetes
CA3133803A1 (en) 2019-04-11 2020-10-15 Angion Biomedica Corp. Solid forms of (e)-3-[2-(2-thienyl)vinyl]-1h-pyrazole
ES2982700T3 (es) 2019-04-18 2024-10-17 Synthon Bv Proceso para preparar axitinib, proceso para purificar el producto intermedio 2-((3-yodo-1H-indazol-6-il)tio)-n-metilbenzamida, proceso para purificar axitinib a través de la sal HCI de axitinib, forma sólida de la sal HCI de axitinib
US12290601B2 (en) 2019-05-09 2025-05-06 Synthon B.V. Pharmaceutical composition comprising axitinib
EP3990635A1 (en) 2019-06-27 2022-05-04 Rigontec GmbH Design method for optimized rig-i ligands
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11155567B2 (en) 2019-08-02 2021-10-26 Mersana Therapeutics, Inc. Sting agonist compounds and methods of use
CA3150701A1 (en) 2019-08-15 2021-02-18 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
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
WO2021035360A1 (en) * 2019-08-30 2021-03-04 Risen (Suzhou) Pharma Tech Co., Ltd. Prodrugs of the tyrosine kinase inhibitor for treating cancer
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
KR20220100879A (ko) 2019-10-14 2022-07-18 인사이트 코포레이션 Fgfr 저해제로서의 이환식 헤테로사이클
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
PE20221504A1 (es) 2019-12-04 2022-09-30 Incyte Corp Derivados de un inhibidor de fgfr
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
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
EP4087583A4 (en) 2020-01-07 2024-01-24 Merck Sharp & Dohme LLC ARGINASE INHIBITORS AND METHODS OF USE
WO2021146424A1 (en) 2020-01-15 2021-07-22 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
CA3168543A1 (en) 2020-01-29 2021-08-05 Gilead Sciences, Inc. Glp-1r modulating compounds
US20230082544A1 (en) 2020-02-18 2023-03-16 Novo Nordisk A/S Pharmaceutical formulations
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
PH12022552639A1 (en) 2020-04-02 2024-02-19 Mersana Therapeutics Inc Antibody drug conjugates comprising sting agonists
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
US20240051939A1 (en) * 2020-12-08 2024-02-15 Disarm Therapeutics, Inc. Benzopyrazole inhibitors of sarm1
IL303661A (en) 2020-12-22 2023-08-01 Nikang Therapeutics Inc Compounds for degrading cyclin-dependent kinase 2 via ubiquitin proteosome pathway
WO2022152821A1 (en) 2021-01-13 2022-07-21 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
EP4323350A1 (en) 2021-04-14 2024-02-21 Monte Rosa Therapeutics AG Isoindolinone compounds
WO2022219412A1 (en) 2021-04-14 2022-10-20 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
CA3220274A1 (en) 2021-06-09 2022-12-15 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
MX2024011545A (es) 2022-03-23 2024-09-26 Ideaya Biosciences Inc Compuestos de indazol sustituidos con piperazina como inhibidores de 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
EP4536363A1 (en) 2022-06-08 2025-04-16 Nikang Therapeutics, Inc. Sulfamide derivatives as cyclin-dependent kinase 2 inhibitors
EP4556466A1 (en) * 2022-08-08 2025-05-21 Beyang Therapeutics Co., Ltd. Protein tyrosine kinase inhibitor and medical use thereof
AU2023375457A1 (en) 2022-11-11 2025-05-01 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway
US20240336608A1 (en) 2023-03-29 2024-10-10 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
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

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
WO1996014843A2 (en) * 1994-11-10 1996-05-23 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
CA2258728C (en) * 1996-06-19 2011-09-27 Rhone Poulenc Rorer Limited Substituted azabicylic compounds and their use as inhibitors of the production of tnf and cyclic amp phosphodiesterase
SK27299A3 (en) * 1996-09-04 2000-10-09 Pfizer Indazole derivatives and their use as inhibitors of phosphodiesterase (pde) type iv and the production of tumor necrosis factor (tnf)
UA66810C2 (uk) * 1997-10-27 2004-06-15 Агорон Фармацевтикалз Інк. Похідні 4-амінотіазолу та композиції на їх основі як інгібітори циклінозалежних кіназ
SK6262000A3 (en) * 1997-11-04 2002-03-05 Pfizer Prod Inc Therapeutically active compounds based on indazole bioisostere replacement of catechol in pde4 inhibitors
CA2309150A1 (en) * 1997-11-04 1999-05-14 Pfizer Products Inc. Indazole bioisostere replacement of catechol in therapeutically active compounds
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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