JP2022543155A - Ｈｐｋ１阻害剤の固体形態 - Google Patents

Ｈｐｋ１阻害剤の固体形態 Download PDF

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JP2022543155A
JP2022543155A JP2022507441A JP2022507441A JP2022543155A JP 2022543155 A JP2022543155 A JP 2022543155A JP 2022507441 A JP2022507441 A JP 2022507441A JP 2022507441 A JP2022507441 A JP 2022507441A JP 2022543155 A JP2022543155 A JP 2022543155A
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salt
compound
theta
degrees
cancer
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JP2022543155A5 (https=
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ジア，ジョンジアン
フリーツェ，ウィリアム
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Incyte Corp
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Incyte Corp
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/702—Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/19—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton containing rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/255—Tartaric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/265—Citric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40—Unsaturated compounds
    • C07C59/42—Unsaturated compounds containing hydroxy or O-metal groups
    • C07C59/48—Unsaturated compounds containing hydroxy or O-metal groups containing six-membered aromatic rings
    • C07C59/50—Mandelic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/36—Systems containing two condensed rings the rings having more than two atoms in common
    • C07C2602/42—Systems containing two condensed rings the rings having more than two atoms in common the bicyclo ring system containing seven carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2022507441A 2019-08-06 2020-08-05 Ｈｐｋ１阻害剤の固体形態 Pending JP2022543155A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201962883350P 2019-08-06 2019-08-06
US62/883,350 2019-08-06
US201962889848P 2019-08-21 2019-08-21
US62/889,848 2019-08-21
PCT/US2020/044919 WO2021026180A1 (en) 2019-08-06 2020-08-05 Solid forms of an hpk1 inhibitor

Publications (2)

Publication Number Publication Date
JP2022543155A true JP2022543155A (ja) 2022-10-07
JP2022543155A5 JP2022543155A5 (https=) 2023-08-15

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JP2022507441A Pending JP2022543155A (ja) 2019-08-06 2020-08-05 Ｈｐｋ１阻害剤の固体形態

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US (2) US11066394B2 (https=)
EP (1) EP4010338A1 (https=)
JP (1) JP2022543155A (https=)
KR (1) KR20220059480A (https=)
CN (1) CN114450276A (https=)
AU (1) AU2020326703A1 (https=)
BR (1) BR112022002059A2 (https=)
CA (1) CA3147918A1 (https=)
CL (1) CL2022000267A1 (https=)
CO (1) CO2022002563A2 (https=)
CR (1) CR20220097A (https=)
EC (1) ECSP22015801A (https=)
IL (1) IL289879A (https=)
MX (1) MX2022001562A (https=)
PE (1) PE20221419A1 (https=)
PH (1) PH12022550271A1 (https=)
TW (1) TWI865579B (https=)
WO (1) WO2021026180A1 (https=)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018049214A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer
US20180072741A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyrimidine compounds and uses thereof
CN115819417A (zh) 2016-09-09 2023-03-21 因赛特公司 作为hpk1调节剂的吡唑并吡啶衍生物及其用于治疗癌症的用途
US10752635B2 (en) 2018-02-20 2020-08-25 Incyte Corporation Indazole compounds and uses thereof
EP3755703B1 (en) 2018-02-20 2022-05-04 Incyte Corporation N-(phenyl)-2-(phenyl)pyrimidine-4-carboxamide derivatives and related compounds as hpk1 inhibitors for treating cancer
US11299473B2 (en) 2018-04-13 2022-04-12 Incyte Corporation Benzimidazole and indole compounds and uses thereof
US10899755B2 (en) 2018-08-08 2021-01-26 Incyte Corporation Benzothiazole compounds and uses thereof
WO2020092528A1 (en) 2018-10-31 2020-05-07 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity
US11203591B2 (en) 2018-10-31 2021-12-21 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds
EP3972695A1 (en) 2019-05-23 2022-03-30 Gilead Sciences, Inc. Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors
BR112022002059A2 (pt) 2019-08-06 2022-06-07 Incyte Corp Formas sólidas de um inibidor de hpk1
TW202321239A (zh) 2021-07-20 2023-06-01 瑞典商阿斯特捷利康公司 作為ｈｐｋ１抑制劑用於治療癌症之經取代的吡𠯤—２—甲醯胺

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009058348A1 (en) * 2007-11-01 2009-05-07 Sirtris Pharmaceuticals, Inc. Amide derivatives as sirtuin modulators
WO2016205942A1 (en) * 2015-06-25 2016-12-29 University Health Network Hpk1 inhibitors and methods of using same

Family Cites Families (240)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE8800613D0 (sv) 1988-02-23 1988-02-23 Wallac Oy A novel spectrofluorometric method and compounds that are of value for the method
JPH03287584A (ja) 1990-04-05 1991-12-18 Banyu Pharmaceut Co Ltd 置換アリルアミン誘導体
US5250534A (en) 1990-06-20 1993-10-05 Pfizer Inc. Pyrazolopyrimidinone antianginal agents
US6200980B1 (en) 1995-06-07 2001-03-13 Cell Pathways, Inc. Method of treating a patient having precancerous lesions with phenyl purinone derivatives
US6723719B1 (en) 1997-04-25 2004-04-20 Pfizer Inc Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3′,5′—monophosphate phosphodiesterase (cGMP PDE5) for the treatment of sexual dysfunction
RS50011B (sr) 1998-04-20 2008-09-29 Pfizer Inc., Derivati piridin-3-karboksilne kiseline i njihova upotreba kao intermedijera
JP2000038350A (ja) 1998-05-18 2000-02-08 Yoshitomi Pharmaceut Ind Ltd 糖尿病治療薬
GB9823102D0 (en) 1998-10-23 1998-12-16 Pfizer Ltd Pharmaceutically active compounds
GB9823101D0 (en) 1998-10-23 1998-12-16 Pfizer Ltd Pharmaceutically active compounds
WO2001046124A1 (en) 1999-12-22 2001-06-28 Nihon Nohyaku Co., Ltd. Aromatic diamide derivatives, chemicals for agricultural or horticultural use and usage thereof
CZ27399A3 (cs) 1999-01-26 2000-08-16 Ústav Experimentální Botaniky Av Čr Substituované dusíkaté heterocyklické deriváty, způsob jejich přípravy, tyto deriváty pro použití jako léčiva, farmaceutická kompozice a kombinovaný farmaceutický přípravek tyto deriváty obsahující a použití těchto derivátů pro výrobu léčiv
IN187433B (https=) 1999-09-10 2002-04-27 Cipla Ltd
WO2001019827A1 (en) 1999-09-13 2001-03-22 Cipla Ltd. A novel process for the synthesis of sildenafil citrate
MXPA02002938A (es) 1999-09-17 2004-12-06 Abbott Gmbh & Co Kg Inhibidores de cinasa como agentes agentes terapeuticos.
ES2239035T3 (es) 1999-09-24 2005-09-16 Nihon Nohyaku Co., Ltd. Derivados de diamida aromatica o sales de estos derivados, productos quimicos para la agricultura/horticultura y procedimiento de utilizacion de estos productos.
TWI265925B (en) 1999-10-11 2006-11-11 Pfizer Pyrazolo[4,3-d]pyrimidin-7-ones useful in inhibiting type 5 cyclic guanosine 3',5'-monophosphate phosphodiesterases(cGMP PDE5), process and intermediates for their preparation, their uses and composition comprising them
HK1049834A1 (zh) 1999-10-11 2003-05-30 辉瑞大药厂 用作磷酸二酯酶抑制剂的5-(2-取代的-5-杂环基磺酰基吡啶-3-基)-二氢吡唑并[4，3-d]嘧啶-7-酮类化合物
IL139073A0 (en) 1999-10-21 2001-11-25 Pfizer Treatment of neuropathy
CO5271697A1 (es) 2000-01-12 2003-04-30 Pfizer Prod Inc Composiciones y procedimientos para el tratamiento de afecciones que responden a un aumento de testosterona
US20020013327A1 (en) 2000-04-18 2002-01-31 Lee Andrew G. Compositions and methods for treating female sexual dysfunction
KR100786927B1 (ko) 2000-06-28 2007-12-17 스미스클라인비이참피이엘시이 습식 분쇄방법
AU2001277621A1 (en) 2000-08-09 2002-03-04 Astrazeneca Ab Antiangiogenic bicyclic derivatives
AU2001284417A1 (en) 2000-09-05 2002-03-22 Taisho Pharmaceutical Co. Ltd. Hair growth stimulants
US6548508B2 (en) 2000-10-20 2003-04-15 Pfizer, Inc. Use of PDE V inhibitors for improved fecundity in mammals
EP1343506A1 (de) 2000-12-19 2003-09-17 MERCK PATENT GmbH Pharmazeutische formulierung enthaltend pyrazolo 4,3-d]pyrimidine und antithrombotica, calcium-antagonisten, prostaglandine oder prostaglandinderivate
AU2002222293A1 (en) 2000-12-19 2002-07-01 Smithkline Beecham P.L.C. Pyrazolo(3,4-c)pyridines as gsk-3 inhibitors
US6784185B2 (en) 2001-03-16 2004-08-31 Pfizer Inc. Pharmaceutically active compounds
US6770645B2 (en) 2001-03-16 2004-08-03 Pfizer Inc. Pharmaceutically active compounds
US7902179B2 (en) 2001-04-26 2011-03-08 Ajinomoto Co., Inc. Heterocyclic compounds
US20040157866A1 (en) 2001-04-30 2004-08-12 Hisashi Takasugi Amide compounds
FR2825706B1 (fr) 2001-06-06 2003-12-12 Pf Medicament Nouveaux derives de benzothienyle ou d'indole, leur preparation et leur utilisation comme inhibiteurs de proteines prenyl transferase
JP2005508978A (ja) 2001-11-02 2005-04-07 ファイザー・プロダクツ・インク Ｐｄｅ９阻害薬によるインスリン抵抗性症候群及び２型糖尿病の治療
TW200303201A (en) 2001-12-10 2003-09-01 Bristol Myers Squibb Co Synthesis of 4,5-dihydro-pyrazolo [3,4-c] pyrid-2-ones
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
US7429609B2 (en) 2002-05-31 2008-09-30 Eisai R & D Management Co., Ltd. Pyrazole compound and medicinal composition containing the same
EP1606289B1 (en) 2003-02-14 2009-12-02 Glaxo Group Limited Carboxamide derivatives
WO2004074286A1 (en) 2003-02-14 2004-09-02 Wyeth Heterocyclyl-3-sulfonylazaindole or -azaindazole derivatives as 5-hydroxytryptamine-6 ligands
EP1613747A1 (en) 2003-03-31 2006-01-11 Pfizer Products Inc. Crystal structure of 3 ,5 -cyclic nucleotide phosphodiesterase 1b (pde1b) and uses thereof
OA13050A (en) 2003-04-29 2006-11-10 Pfizer Ltd 5,7-diaminopyrazolo [4,3-D] pyrimidines useful in the treatment of hypertension.
EP1628661A2 (en) 2003-06-05 2006-03-01 Vertex Pharmaceuticals Incorporated Modulators of vr1 receptor
CA2528587A1 (en) 2003-06-10 2005-01-20 Fulcrum Pharmaceuticals, Inc. .beta.-lactamase inhibitors and methods of use thereof
ZA200305330B (en) 2003-07-10 2004-05-26 Jb Chemicals & Pharmaceuticals An improved process for the preparation of 5-[2-ethoxy-5-(4-methylpiperazin-1-ylsulphonyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazole[4,3-D]P yrimidin-7-one.
JP2007500700A (ja) 2003-07-29 2007-01-18 スミスクライン ビーチャム コーポレーション 化合物
TWI339206B (en) 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
CN1905873A (zh) 2003-11-19 2007-01-31 阵列生物制药公司 Mek的杂环抑制剂及其使用方法
US7241773B2 (en) 2003-12-22 2007-07-10 Abbott Laboratories 3-quinuclidinyl heteroatom bridged biaryl derivatives
US20050137398A1 (en) 2003-12-22 2005-06-23 Jianguo Ji 3-Quinuclidinyl heteroatom bridged biaryl derivatives
GB0402137D0 (en) 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
DE102004005172A1 (de) 2004-02-02 2005-08-18 Aventis Pharma Deutschland Gmbh Indazolderivate als Inhibitoren der Hormon Sensitiven Lipase
WO2005085249A1 (en) 2004-02-27 2005-09-15 F. Hoffmann-La Roche Ag Fused derivatives of pyrazole
CN1934111A (zh) 2004-02-27 2007-03-21 霍夫曼-拉罗奇有限公司 杂芳基稠合的吡唑并衍生物
JP2007526324A (ja) 2004-03-02 2007-09-13 スミスクライン・ビーチャム・コーポレイション Ａｋｔ活性のある阻害剤
TW200618800A (en) 2004-08-03 2006-06-16 Uriach Y Compania S A J Heterocyclic compounds
ES2377430T3 (es) 2004-09-02 2012-03-27 Genentech, Inc. Inhibidores piridílicos de la señalización de hedgehog
WO2006038001A1 (en) 2004-10-06 2006-04-13 Celltech R & D Limited Aminopyrimidine derivatives as jnk inhibitors
WO2006045010A2 (en) 2004-10-20 2006-04-27 Resverlogix Corp. Stilbenes and chalcones for the prevention and treatment of cardiovascular diseases
AR051596A1 (es) 2004-10-26 2007-01-24 Irm Llc Compuestos heterociclicos condensados nitrogenados como inhibidores de la actividad del receptor canabinoide 1; composiciones farmaceuticas que los contienen y su empleo en la preparacion de medicamentos para el tratamiento de trastornos alimentarios
EP1805136A1 (en) 2004-10-28 2007-07-11 The Institutes for Pharmaceutical Discovery, LLC Substituted phenylalkanoic acids
TW200628463A (en) 2004-11-10 2006-08-16 Synta Pharmaceuticals Corp Heteroaryl compounds
AU2005304473A1 (en) 2004-11-10 2006-05-18 Cgi Pharmaceuticals, Inc. Imidazo[1 , 2-a] pyrazin-8-ylamines useful as modulators of kinase activity
WO2006053227A2 (en) 2004-11-10 2006-05-18 Synta Pharmaceuticals Corp. Il-12 modulatory compounds
DE102004054666A1 (de) 2004-11-12 2006-05-18 Bayer Cropscience Gmbh Substituierte Pyrazol-3-carboxamide, Verfahren zur Herstellung und Verwendung als Herbizide und Pflanzenwachstumsregulatoren
CN100516049C (zh) 2004-11-16 2009-07-22 永信药品工业股份有限公司 抗血管生成药n2-(取代的芳基甲基)-3-(取代的苯基)吲唑的合成
EP1838320B1 (en) 2005-01-07 2014-07-16 Emory University Cxcr4 antagonists for the treatment of medical disorders
JP5023054B2 (ja) 2005-03-31 2012-09-12 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 抗バクテリア剤としての二環式ピラゾール化合物
US20070032493A1 (en) 2005-05-26 2007-02-08 Synta Pharmaceuticals Corp. Method for treating B cell regulated autoimmune disorders
EP1910369A1 (en) 2005-07-29 2008-04-16 Astellas Pharma Inc. Fused heterocycles as lck inhibitors
DK1910384T3 (da) 2005-08-04 2012-12-17 Sirtris Pharmaceuticals Inc Imidazo [2,1-b] thiazol-derivater som sirtuinmodulerende forbindelser
GB0516703D0 (en) 2005-08-15 2005-09-21 Syngenta Participations Ag Novel insecticides
JP2007055940A (ja) 2005-08-24 2007-03-08 Astellas Pharma Inc ピラゾロピリミジン誘導体
KR101011956B1 (ko) 2005-08-25 2011-01-31 에프. 호프만-라 로슈 아게 Ｐ３８ ｍαｐ 키나아제 저해제 및 이의 사용 방법
CN101243051A (zh) 2005-08-25 2008-08-13 霍夫曼-拉罗奇有限公司 p38 MAP激酶抑制剂及使用它的方法
BRPI0614884A2 (pt) 2005-08-25 2011-04-19 Hoffmann La Roche inibidores de p38 map cinase e métodos para uso dos mesmos
CN101277939A (zh) 2005-09-09 2008-10-01 布里斯托尔-迈尔斯斯奎布公司 无环ikur抑制剂
US20070087988A1 (en) 2005-09-30 2007-04-19 New York University Hematopoietic progenitor kinase 1 for modulation of an immune response
EP1940296A2 (en) 2005-10-25 2008-07-09 SmithKline Beecham Corporation Chemical compounds
AU2006311766A1 (en) 2005-11-03 2007-05-18 Ilypsa, Inc. Indole compounds having C4-acidic substituents and use thereof as phospholipase-A2 inhibitors
CA2629964A1 (en) 2005-11-30 2007-06-07 Astellas Pharma Inc. 2-aminobenzamide derivative
GB0525143D0 (en) 2005-12-09 2006-01-18 Novartis Ag Organic compounds
EP1979325A1 (en) 2006-01-11 2008-10-15 AstraZeneca AB Morpholino pyrimidine derivatives and their use in therapy
US8658801B2 (en) 2006-02-16 2014-02-25 Syngenta Crop Protection, Llc Pesticides containing a bicyclic bisamide structure
AU2007230911A1 (en) 2006-03-23 2007-10-04 Synta Pharmaceuticals Corp. Benzimidazolyl-pyridine compounds for inflammation and immune-related uses
WO2007120454A1 (en) 2006-03-30 2007-10-25 Irm Llc Azolopyrimidines as inhibitors of cannabinoid 1 activity
PL2018380T3 (pl) 2006-05-19 2012-05-31 Abbvie Bahamas Ltd Skondensowane azabicykliczne pochodne alkanowe podstawione bicykloheterocyklem o aktywności wobec OUN
US20080280891A1 (en) 2006-06-27 2008-11-13 Locus Pharmaceuticals, Inc. Anti-cancer agents and uses thereof
WO2008008059A1 (en) 2006-07-12 2008-01-17 Locus Pharmaceuticals, Inc. Anti-cancer agents ans uses thereof
PE20080403A1 (es) 2006-07-14 2008-04-25 Amgen Inc Derivados heterociclicos fusionados y metodos de uso
GB0614691D0 (en) 2006-07-24 2006-08-30 Syngenta Participations Ag Insecticidal compounds
JP2010505859A (ja) 2006-10-06 2010-02-25 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤およびそれを使用するための方法
WO2008070313A2 (en) 2006-10-20 2008-06-12 Concert Pharmaceuticals Inc. 3-(dihydro-1h-pyrazolo [4,3-d] pyrimidin-5-yl)-4-propoxybenzenesulfonamide derivatives and methods of use
US20080194557A1 (en) 2007-01-18 2008-08-14 Joseph Barbosa Methods and compositions for the treatment of pain, inflammation and cancer
WO2008089310A2 (en) 2007-01-18 2008-07-24 Lexicon Pharmaceuticals, Inc. Delta 5 desaturase inhibitors for the treatment of obesity
CA2679659C (en) 2007-03-01 2016-01-19 Novartis Ag Pim kinase inhibitors and methods of their use
US20140249135A1 (en) * 2007-03-01 2014-09-04 Novartis Ag Pim kinase inhibitors and methods of their use
EP2002835A1 (en) 2007-06-04 2008-12-17 GenKyo Tex Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
CL2008001822A1 (es) 2007-06-20 2009-03-13 Sirtris Pharmaceuticals Inc Compuestos derivados de tiazolo[5,4-b]piridina; composicion farmaceutica que comprende a dichos compuestos; y uso del compuesto en el tratamiento de la resistencia a la insulina, sindrome metabolico, diabetes, entre otras.
MY150032A (en) 2007-07-19 2013-11-29 Merck Sharp & Dohme Heterocyclic amide compounds as protein kinase inhibitors
MY146643A (en) 2007-07-30 2012-09-14 Dae Woong Pharma Novel benzoimidazole derivatives and pharmaceutical composition comprising the same
CN101790519B (zh) 2007-08-08 2013-10-16 默克雪兰诺有限公司 用于治疗多发性硬化症的结合于鞘氨醇1-磷酸(s1p)的6-氨基-嘧啶-4-羧酰胺衍生物及相关化合物
GB0716414D0 (en) 2007-08-22 2007-10-03 Syngenta Participations Ag Novel insecticides
WO2009032651A1 (en) 2007-08-31 2009-03-12 Smithkline Beecham Corporation Inhibitors of akt activity
WO2009038784A1 (en) 2007-09-21 2009-03-26 Amgen Inc. Triazole fused heteroaryl compounds as p38 kinase inhibitors
KR100963644B1 (ko) 2007-11-23 2010-06-15 한국과학기술연구원 피라졸로피리미딘온 유도체 및 그의 제조방법
CA2714181C (en) 2008-02-04 2013-12-24 Mercury Therapeutics, Inc. Ampk modulators
CN102098918A (zh) 2008-05-13 2011-06-15 帕纳德制药公司 用于治疗癌症和神经退行性疾病的生物活性化合物
CN102089278A (zh) 2008-06-11 2011-06-08 Irm责任有限公司 用于治疗疟疾的化合物和组合物
NZ603525A (en) 2008-06-27 2015-02-27 Celgene Avilomics Res Inc Pyrimidine based compound and uses thereof
WO2010029300A1 (en) 2008-09-12 2010-03-18 Biolipox Ab Bis aromatic compounds for use in the treatment of inflammation
EP2166008A1 (en) 2008-09-23 2010-03-24 Genkyo Tex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
EP2166010A1 (en) 2008-09-23 2010-03-24 Genkyo Tex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
EP2165707A1 (en) 2008-09-23 2010-03-24 Genkyo Tex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
WO2010046780A2 (en) 2008-10-22 2010-04-29 Institut Pasteur Korea Anti viral compounds
JP2010111624A (ja) 2008-11-06 2010-05-20 Shionogi & Co Ltd Ｔｔｋ阻害作用を有するインダゾール誘導体
WO2010080503A1 (en) 2008-12-19 2010-07-15 Genentech, Inc. Heterocyclic compounds and methods of use
KR20100101055A (ko) 2009-03-07 2010-09-16 주식회사 메디젠텍 세포핵에서 세포질로의 ｇｓｋ３의 이동을 억제하는 화합물을 함유하는 세포핵에서 세포질로의 ｇｓｋ３ 이동 관련 질환의 치료 또는 예방용 약학적 조성물
WO2010107768A1 (en) 2009-03-18 2010-09-23 Schering Corporation Bicyclic compounds as inhibitors of diacylglycerol acyltransferase
EP2411328B1 (en) 2009-03-26 2019-07-24 Northeastern University Carbon nanostructures from pyrolysis of organic materials
WO2010118367A2 (en) 2009-04-10 2010-10-14 Progenics Pharmaceuticals, Inc. Antiviral pyrimidines
US8846673B2 (en) 2009-08-11 2014-09-30 Bristol-Myers Squibb Company Azaindazoles as kinase inhibitors and use thereof
EP2477498A4 (en) 2009-09-14 2013-02-27 Merck Sharp & Dohme INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE
WO2011050245A1 (en) 2009-10-23 2011-04-28 Yangbo Feng Bicyclic heteroaryls as kinase inhibitors
ES2360333B1 (es) 2009-10-29 2012-05-04 Consejo Superior De Investigaciones Cientificas (Csic) (70%) Derivados de bis (aralquil) amino y sistemas (hetero) aromaticos de seis miembros y su uso en el tratamiento de patologias neurodegenerativas, incluida la enfermedad de alzheimer
JP2013032290A (ja) 2009-11-20 2013-02-14 Dainippon Sumitomo Pharma Co Ltd 新規縮合ピリミジン誘導体
WO2011078143A1 (ja) 2009-12-22 2011-06-30 塩野義製薬株式会社 ピリミジン誘導体およびそれらを含有する医薬組成物
WO2011090738A2 (en) 2009-12-29 2011-07-28 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
WO2011082400A2 (en) 2010-01-04 2011-07-07 President And Fellows Of Harvard College Modulators of immunoinhibitory receptor pd-1, and methods of use thereof
US20130109758A1 (en) 2010-01-06 2013-05-02 The University Of British Columbia Bisphenol derivative therapeutics and methods for their use
DE102010009903A1 (de) 2010-03-02 2011-09-08 Merck Patent Gmbh Verbindungen für elektronische Vorrichtungen
CN102206172B (zh) 2010-03-30 2015-02-25 中国医学科学院医药生物技术研究所 一组取代双芳基化合物及其制备方法和抗病毒应用
US9133123B2 (en) 2010-04-23 2015-09-15 Cytokinetics, Inc. Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use
JP6112486B2 (ja) 2010-04-27 2017-04-12 カルシメディカ，インク． 細胞内カルシウムを調節する化合物
GB201008134D0 (en) 2010-05-14 2010-06-30 Medical Res Council Technology Compounds
JP2011246389A (ja) 2010-05-26 2011-12-08 Oncotherapy Science Ltd Ｔｔｋ阻害作用を有する縮環ピラゾール誘導体
JP2013528169A (ja) 2010-05-27 2013-07-08 バイエル・クロップサイエンス・アーゲー 殺菌剤としてのピリジニルカルボン酸誘導体
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
CN103068814B (zh) 2010-06-15 2015-11-25 拜耳知识产权有限责任公司 邻氨基苯甲酸衍生物
EP2582666B1 (en) 2010-06-16 2014-08-13 Purdue Pharma L.P. Aryl substituted indoles and their use as blockers of sodium channels
CA2806655A1 (en) 2010-07-28 2012-02-02 Bayer Intellectual Property Gmbh Substituted imidazo[1,2-b]pyridazines
US10005750B2 (en) 2010-10-06 2018-06-26 J-Pharma Co., Ltd. Developing potent urate transporter inhibitors: compounds designed for their uricosuric action
GB201017345D0 (en) 2010-10-14 2010-11-24 Proximagen Ltd Receptor antagonists
CA2819373A1 (en) 2010-12-09 2012-06-14 Amgen Inc. Bicyclic compounds as pim inhibitors
CN103261188A (zh) 2010-12-17 2013-08-21 先正达参股股份有限公司 杀虫化合物
PT2661433T (pt) 2011-01-04 2017-10-24 Novartis Ag Compostos de indole ou seus análogos úteis para o tratamento da degeneração macular relacionada com a idade (amd)
EP2672820B1 (en) 2011-02-07 2019-04-17 The Washington University Mannoside compounds and methods of use thereof
EP2691399B1 (en) 2011-03-28 2016-07-13 F.Hoffmann-La Roche Ag Thiazolopyrimidine compounds
HRP20170422T1 (hr) 2011-04-12 2017-06-16 Chong Kun Dang Pharmaceutical Corp. 3-(2-aril-cikloalkenilmetil)-oksazolidin-2-on derivati kao inhibitori transportnog proteina estera kolesterola (cetp)
AP2013007253A0 (en) 2011-04-21 2013-11-30 Origenis Gmbh Pyrazolo [4,3-D] pyrimidines useful as kinase inhibitors
US9328075B2 (en) 2011-05-05 2016-05-03 St. Jude Children's Research Hospital Pyrimidinone compounds and methods for treating influenza
US20140107151A1 (en) 2011-05-17 2014-04-17 Principia Biophama Inc. Tyrosine kinase inhibitors
US20140288069A1 (en) 2011-05-17 2014-09-25 Bayer Intellectual Property Gmbh Amino-substituted imidazopyridazines as mknk1 kinase inhibitors
TW201311677A (zh) 2011-05-31 2013-03-16 Syngenta Participations Ag 殺蟲化合物
WO2012163942A1 (en) 2011-06-01 2012-12-06 Bayer Intellectual Property Gmbh Substituted aminoimidazopyridazines
WO2012175591A1 (en) 2011-06-22 2012-12-27 Bayer Intellectual Property Gmbh Heterocyclyl aminoimidazopyridazines
EP3111937B1 (en) 2011-07-08 2020-06-17 Helmholtz-Zentrum für Infektionsforschung GmbH Medicament for treatment of liver cancer
EP2543372A1 (en) 2011-07-08 2013-01-09 Helmholtz-Zentrum für Infektionsforschung GmbH Medicament for the treatment of liver cancer
AU2012293417A1 (en) 2011-08-10 2013-05-02 Purdue Pharma L.P. TRPV1 antagonists including dihydroxy substituent and uses thereof
KR20140047160A (ko) 2011-08-12 2014-04-21 에프. 호프만-라 로슈 아게 인다졸 화합물, 조성물 및 사용 방법
EP2742046A1 (en) 2011-08-12 2014-06-18 F.Hoffmann-La Roche Ag PYRAZOLO[3,4-c]PYRIDINE COMPOUNDS AND METHODS OF USE
WO2013042137A1 (en) 2011-09-19 2013-03-28 Aurigene Discovery Technologies Limited Bicyclic heterocycles as irak4 inhibitors
CA2849345A1 (en) 2011-09-23 2013-03-28 Bayer Intellectual Property Gmbh Substituted imidazopyridazines
CN102516263B (zh) 2011-10-25 2015-04-08 南方医科大学 一种螺三环类化合物及其制备方法、以及含该类化合物的药物组合物及其应用
CN102503959B (zh) 2011-10-25 2015-04-08 南方医科大学 一种稠三环类化合物及其制备方法、以及含该类化合物的药物组合物及其应用
KR20140095513A (ko) 2011-11-01 2014-08-01 에프. 호프만-라 로슈 아게 이미다조피리다진 화합물
AP3675A (en) 2012-02-17 2016-04-15 Kineta Four Llc Antiviral drugs for treatment of arenavirus infection
TW201348231A (zh) 2012-02-29 2013-12-01 Amgen Inc 雜雙環化合物
KR20140131955A (ko) 2012-03-09 2014-11-14 카나 바이오사이언스 인코포레이션 신규 트리아진 유도체
JP6101248B2 (ja) 2012-03-28 2017-03-22 出光興産株式会社 新規化合物、有機エレクトロルミネッセンス素子用材料および有機エレクトロルミネッセンス素子
UY34750A (es) 2012-04-20 2013-11-29 Gilead Sciences Inc ?compuestos para el tratamiento del hiv, composiciones,métodos de preparación, intermediarios y métodos terapéuticos?.
WO2014003405A1 (ko) 2012-06-26 2014-01-03 주식회사 제이앤드제이 캐미칼 신규한 화합물 및 이를 포함하는 발광소자
MX2014015738A (es) 2012-06-28 2015-08-06 Novartis Ag Derivados de pirrolidina y su uso como moduladores de la senda del complemento.
KR101936851B1 (ko) 2012-07-16 2019-01-11 한국과학기술연구원 단백질 키나아제 저해제인 신규 피라졸로피리딘 유도체 또는 인다졸 유도체
WO2014024125A1 (en) 2012-08-08 2014-02-13 Celon Pharma S.A. Pyrazolo[4,3-d]pyrimidin-7(6h)-one derivatives as pde9 inhibitors
TW201412744A (zh) 2012-08-23 2014-04-01 Mitsubishi Tanabe Pharma Corp 吡唑并嘧啶化合物
US9882150B2 (en) 2012-09-24 2018-01-30 Arizona Board Of Regents For And On Behalf Of Arizona State University Metal compounds, methods, and uses thereof
WO2014055955A1 (en) 2012-10-05 2014-04-10 Rigel Pharmaceuticals, Inc. Gdf-8 inhibitors
KR102137472B1 (ko) 2013-02-08 2020-07-27 삼성디스플레이 주식회사 유기 발광 소자
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
EP3495357B1 (en) 2013-03-14 2021-05-05 The Trustees of Columbia University in the City of New York 4-phenylpiperidines, their preparation and use
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
US9034927B2 (en) 2013-05-22 2015-05-19 Curza Global, Llc Methods of use for compositions comprising a biocidal polyamine
CN104232076B (zh) 2013-06-10 2019-01-15 代表亚利桑那大学的亚利桑那校董会 具有改进的发射光谱的磷光四齿金属络合物
US9718818B2 (en) 2013-08-22 2017-08-01 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
TWI652014B (zh) 2013-09-13 2019-03-01 美商艾佛艾姆希公司 雜環取代之雙環唑殺蟲劑
WO2015037965A1 (en) 2013-09-16 2015-03-19 Rohm And Haas Electronic Materials Korea Ltd. Novel organic electroluminescent compounds and organic electroluminescent device comprising the same
CA2927924A1 (en) 2013-10-18 2015-04-23 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
BR112016008632A8 (pt) 2013-10-21 2020-03-17 Merck Patent Gmbh compostos de heteroarila como inibidores de btk, seus usos, e composição farmacêutica
EP3444251B1 (en) 2013-12-11 2023-06-07 Biogen MA Inc. Biaryl compounds useful for the treatment of human diseases in oncology, neurology and immunology
EP3079683A4 (en) 2013-12-13 2017-12-20 Dana-Farber Cancer Institute, Inc. Methods to treat lymphoplasmacytic lymphoma
TWI667233B (zh) 2013-12-19 2019-08-01 德商拜耳製藥公司 新穎吲唑羧醯胺，其製備方法、含彼等之醫藥製劑及其製造醫藥之用途
EP3083589B1 (en) 2013-12-20 2019-12-18 Sunshine Lake Pharma Co., Ltd. Substituted piperazine compounds and methods of use thereof
EP3092226B1 (en) 2014-01-10 2019-03-13 Aurigene Discovery Technologies Limited Indazole compounds as irak4 inhibitors
JP6640098B2 (ja) 2014-02-05 2020-02-05 メルク、パテント、ゲゼルシャフト、ミット、ベシュレンクテル、ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ ＧｍｂＨ 金属錯体
US9732103B2 (en) 2014-02-25 2017-08-15 Achillion Pharmaceuticals, Inc. Carbamate, ester, and ketone compounds for treatment of complement mediated disorders
US9871208B2 (en) 2014-02-26 2018-01-16 Samsung Display Co., Ltd. Condensed cyclic compound and organic light-emitting device including the same
WO2015164956A1 (en) 2014-04-29 2015-11-05 The University Of British Columbia Benzisothiazole derivative compounds as therapeutics and methods for their use
US20150328188A1 (en) 2014-05-19 2015-11-19 Everardus O. Orlemans Combination Therapies for the Treatment of Proliferative Disorders
KR102402729B1 (ko) 2014-06-18 2022-05-26 메르크 파텐트 게엠베하 유기 전계발광 소자용 재료
WO2015193506A1 (en) 2014-06-20 2015-12-23 Institut Pasteur Korea Anti-infective compounds
AU2015275730A1 (en) 2014-06-20 2016-12-15 Aurigene Discovery Technologies Limited Substituted indazole compounds as IRAK4 inhibitors
WO2015200682A1 (en) 2014-06-25 2015-12-30 Vanderbilt University Substituted 4-alkoxypicolinamide analogs ds mglur5 negative allosteric modulators
KR20160007967A (ko) 2014-07-10 2016-01-21 삼성디스플레이 주식회사 유기 발광 소자
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
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
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
WO2016041618A1 (en) 2014-09-15 2016-03-24 Merck Patent Gmbh Substituted indazoles and related heterocycles
US10253023B2 (en) 2014-10-06 2019-04-09 Merck Patent Gmbh Heteroaryl compounds as BTK inhibitors and uses thereof
JO3705B1 (ar) 2014-11-26 2021-01-31 Bayer Pharma AG إندازولات مستبدلة جديدة، عمليات لتحضيرها، مستحضرات دوائية تحتوي عليها واستخدامها في إنتاج أدوية
CN107206088A (zh) 2014-12-05 2017-09-26 豪夫迈·罗氏有限公司 使用pd‑1轴拮抗剂和hpk1拮抗剂用于治疗癌症的方法和组合物
WO2016124304A1 (de) 2015-02-03 2016-08-11 Merck Patent Gmbh Metallkomplexe
EP3265445B1 (en) 2015-03-06 2021-05-05 Pharmakea, Inc. Lysyl oxidase-like 2 inhibitors and uses thereof
CN112679467B (zh) 2015-03-11 2024-11-01 Fmc公司 杂环取代的二环唑杀有害生物剂
WO2016161571A1 (en) 2015-04-08 2016-10-13 Merck Sharp & Dohme Corp. Indazole and azaindazole btk inhibitors
TW201701879A (zh) 2015-04-30 2017-01-16 拜耳製藥公司 Ｉｒａｋ４抑制劑組合
CN108024971A (zh) 2015-07-15 2018-05-11 奥列基因发现技术有限公司 作为irak-4抑制剂的取代的氮杂化合物
JP2018524372A (ja) 2015-07-15 2018-08-30 アウリジーン ディスカバリー テクノロジーズ リミテッド Ｉｒａｋ−４阻害剤としてのインダゾール及びアザインダゾール化合物
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
WO2017023894A1 (en) 2015-08-03 2017-02-09 Raze Therapeutics, Inc. Mthfd2 inhibitors and uses thereof
CA2995094A1 (en) 2015-08-07 2017-02-16 Calcimedica, Inc. Use of crac channel inhibitors for the treatment of stroke and traumatic brain injury
WO2017045955A1 (en) 2015-09-14 2017-03-23 Basf Se Heterobicyclic compounds
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017108744A1 (de) 2015-12-22 2017-06-29 Bayer Pharma Aktiengesellschaft Neue substituierte indazole, verfahren zu ihrer herstellung, pharmazeutische präparate die diese enthalten, sowie deren verwendung zur herstellung von arzneimitteln
TWI726968B (zh) 2016-01-07 2021-05-11 開曼群島商Ｃｓ醫藥技術公司 Egfr酪胺酸激酶之臨床重要突變體之選擇性抑制劑
EP3492462B1 (en) 2016-07-26 2023-08-30 Shenzhen TargetRx, Inc. Amino pyrimidine compound for inhibiting protein tyrosine kinase activity
US10280164B2 (en) 2016-09-09 2019-05-07 Incyte Corporation Pyrazolopyridone compounds and uses thereof
CN115819417A (zh) 2016-09-09 2023-03-21 因赛特公司 作为hpk1调节剂的吡唑并吡啶衍生物及其用于治疗癌症的用途
US20180072741A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyrimidine compounds and uses thereof
WO2018049214A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer
WO2018152220A1 (en) 2017-02-15 2018-08-23 Incyte Corporation Pyrazolopyridine compounds and uses thereof
US10722495B2 (en) 2017-09-08 2020-07-28 Incyte Corporation Cyanoindazole compounds and uses thereof
EP3755703B1 (en) * 2018-02-20 2022-05-04 Incyte Corporation N-(phenyl)-2-(phenyl)pyrimidine-4-carboxamide derivatives and related compounds as hpk1 inhibitors for treating cancer
US10752635B2 (en) 2018-02-20 2020-08-25 Incyte Corporation Indazole compounds and uses thereof
US10745388B2 (en) 2018-02-20 2020-08-18 Incyte Corporation Indazole compounds and uses thereof
US11299473B2 (en) 2018-04-13 2022-04-12 Incyte Corporation Benzimidazole and indole compounds and uses thereof
GEP20227433B (en) 2018-04-26 2022-10-25 Pfizer 2-amino-pyridine or 2-amino-pyrimidine derivatives as cyclin dependent kinase inhibitors
US11633459B2 (en) 2018-05-04 2023-04-25 Novo Nordisk A/S GIP derivatives and uses thereof
EP3793559A1 (en) 2018-05-17 2021-03-24 Bayer Aktiengesellschaft Substituted dihydropyrazolo pyrazine carboxamide derivatives
US10899755B2 (en) 2018-08-08 2021-01-26 Incyte Corporation Benzothiazole compounds and uses thereof
BR112022002059A2 (pt) 2019-08-06 2022-06-07 Incyte Corp Formas sólidas de um inibidor de hpk1

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009058348A1 (en) * 2007-11-01 2009-05-07 Sirtris Pharmaceuticals, Inc. Amide derivatives as sirtuin modulators
WO2016205942A1 (en) * 2015-06-25 2016-12-29 University Health Network Hpk1 inhibitors and methods of using same

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