JP5721187B2 - ホスファチジルイノシトール３−キナーゼのイソインドリノンインヒビター - Google Patents

ホスファチジルイノシトール３−キナーゼのイソインドリノンインヒビター Download PDF

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Publication number
JP5721187B2
JP5721187B2 JP2012546137A JP2012546137A JP5721187B2 JP 5721187 B2 JP5721187 B2 JP 5721187B2 JP 2012546137 A JP2012546137 A JP 2012546137A JP 2012546137 A JP2012546137 A JP 2012546137A JP 5721187 B2 JP5721187 B2 JP 5721187B2
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Japan
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aliphatic
alkyl
hydrogen
compound
pharmaceutically acceptable
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JP2012546137A
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JP2013515074A (ja
JP2013515074A5 (enExample
Inventor
アレックス アロノフ，
アレックス アロノフ，
ジョン エイチ． カム，
ジョン エイチ． カム，
ロバート ジェイ． デイビーズ，
ロバート ジェイ． デイビーズ，
アルバート シー． ピアス，
アルバート シー． ピアス，
ジアン ワン，
ジアン ワン，
スギャンティニ ナンタクマール，
スギャンティニ ナンタクマール，
カオ，　ジンロン
ジンロン カオ，
ウプル ケー． バンダラージ，
ウプル ケー． バンダラージ，
エレイン クルーガー，
エレイン クルーガー，
アモー ル ティラン，
アモー ル ティラン，
ユーシェン リャオ，
ユーシェン リャオ，
デイビッド メサースミス，
デイビッド メサースミス，
フィリップ エヌ． コリアー，
フィリップ エヌ． コリアー，
ロナルド ジュニア グレイ，
ロナルド ジュニア グレイ，
ハードウィン オダウト，
ハードウィン オダウト，
ジェイムズ エー． ヘンダーソン，
ジェイムズ エー． ヘンダーソン，
アンーロール グリロット，
アンーロール グリロット，
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43859800&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=JP5721187(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
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Publication of JP2013515074A5 publication Critical patent/JP2013515074A5/ja
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    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D417/14—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—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 three hetero rings
    • C07D471/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—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
    • C07D491/12—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 three hetero rings
    • C07D491/20—Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2012546137A 2009-12-22 2010-12-21 ホスファチジルイノシトール３−キナーゼのイソインドリノンインヒビター Expired - Fee Related JP5721187B2 (ja)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US28900309P 2009-12-22 2009-12-22
US61/289,003 2009-12-22
US35063110P 2010-06-02 2010-06-02
US61/350,631 2010-06-02
US36920110P 2010-07-30 2010-07-30
US61/369,201 2010-07-30
US38758210P 2010-09-29 2010-09-29
US61/387,582 2010-09-29
PCT/US2010/061484 WO2011087776A1 (en) 2009-12-22 2010-12-21 Isoindolinone inhibitors of phosphatidylinositol 3-kinase

Related Child Applications (1)

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JP2015034849A Division JP6132410B2 (ja) 2009-12-22 2015-02-25 ホスファチジルイノシトール３−キナーゼのイソインドリノンインヒビター

Publications (3)

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JP2013515074A JP2013515074A (ja) 2013-05-02
JP2013515074A5 JP2013515074A5 (enExample) 2014-02-13
JP5721187B2 true JP5721187B2 (ja) 2015-05-20

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ID=43859800

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JP2012546137A Expired - Fee Related JP5721187B2 (ja) 2009-12-22 2010-12-21 ホスファチジルイノシトール３−キナーゼのイソインドリノンインヒビター
JP2015034849A Expired - Fee Related JP6132410B2 (ja) 2009-12-22 2015-02-25 ホスファチジルイノシトール３−キナーゼのイソインドリノンインヒビター
JP2017067536A Expired - Fee Related JP6510580B2 (ja) 2009-12-22 2017-03-30 ホスファチジルイノシトール３−キナーゼのイソインドリノンインヒビター
JP2018079069A Withdrawn JP2018131449A (ja) 2009-12-22 2018-04-17 ホスファチジルイノシトール３−キナーゼのイソインドリノンインヒビター

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JP2015034849A Expired - Fee Related JP6132410B2 (ja) 2009-12-22 2015-02-25 ホスファチジルイノシトール３−キナーゼのイソインドリノンインヒビター
JP2017067536A Expired - Fee Related JP6510580B2 (ja) 2009-12-22 2017-03-30 ホスファチジルイノシトール３−キナーゼのイソインドリノンインヒビター
JP2018079069A Withdrawn JP2018131449A (ja) 2009-12-22 2018-04-17 ホスファチジルイノシトール３−キナーゼのイソインドリノンインヒビター

Country Status (16)

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US (4) US20120040950A1 (enExample)
EP (3) EP3309152B1 (enExample)
JP (4) JP5721187B2 (enExample)
KR (1) KR101758046B1 (enExample)
CN (1) CN102762548B (enExample)
AU (1) AU2010341573B2 (enExample)
BR (1) BR112012018386A8 (enExample)
CA (1) CA2785499C (enExample)
CL (1) CL2012001714A1 (enExample)
ES (2) ES2842399T3 (enExample)
IL (1) IL220625A (enExample)
MX (2) MX350761B (enExample)
NZ (1) NZ600954A (enExample)
RU (1) RU2573569C2 (enExample)
SG (2) SG10201502073PA (enExample)
WO (1) WO2011087776A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017114916A (ja) * 2009-12-22 2017-06-29 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ ホスファチジルイノシトール３−キナーゼのイソインドリノンインヒビター

Families Citing this family (116)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
CA2711558C (en) 2008-01-04 2016-12-13 Intellikine, Inc. Phosphatidyl inositol-3 kinase inhibiting compounds
JP5731978B2 (ja) 2008-09-26 2015-06-10 インテリカイン， エルエルシー 複素環キナーゼ阻害剤
EP2427195B1 (en) 2009-05-07 2019-05-01 Intellikine, LLC Heterocyclic compounds and uses thereof
AU2011255218B2 (en) 2010-05-21 2015-03-12 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulation
JP2013545749A (ja) 2010-11-10 2013-12-26 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 複素環化合物及びその使用
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
AU2012205669B2 (en) 2011-01-10 2015-08-20 Infinity Pharmaceuticals Inc. Processes for preparing isoquinolinones and solid forms of isoquinolinones
US9056877B2 (en) 2011-07-19 2015-06-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
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
EP2751093A1 (en) 2011-08-29 2014-07-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
MX360323B (es) * 2012-04-25 2018-10-29 Raqualia Pharma Inc Derivados de pirrolopiridinona como bloqueadores de ttx-s.
LT3495367T (lt) 2012-06-13 2021-02-25 Incyte Holdings Corporation Pakeistieji tricikliniai junginiai, kaip fgfr inhibitoriai
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
UA110688C2 (uk) * 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
KR102229478B1 (ko) 2012-11-01 2021-03-18 인피니티 파마슈티칼스, 인코포레이티드 Pi3 키나아제 동형단백질 조절인자를 사용하는 암의 치료
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
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
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
LT2986610T (lt) 2013-04-19 2018-04-10 Incyte Holdings Corporation Bicikliniai heterociklai, kaip fgfr inhibitoriai
AU2014324873B2 (en) 2013-09-25 2018-11-08 Vertex Pharmaceuticals Incorporated A selective inhibitor of phosphatidylinositol 3-kinase-gamma
US9751888B2 (en) 2013-10-04 2017-09-05 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
PE20160685A1 (es) 2013-10-04 2016-07-23 Infinity Pharmaceuticals Inc Compuestos heterociclicos y usos de los mismos
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
SG10201808053XA (en) 2014-03-19 2018-10-30 Infinity Pharmaceuticals Inc Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders
US10294205B2 (en) 2014-04-16 2019-05-21 Nanyang Technological University Allenamide as an orthogonal handle for selective modification of cysteine in peptides and proteins
US20150320755A1 (en) 2014-04-16 2015-11-12 Infinity Pharmaceuticals, Inc. Combination therapies
TWI664165B (zh) 2014-04-23 2019-07-01 日商武田藥品工業股份有限公司 含氮雜環化合物
US10308639B2 (en) 2014-06-13 2019-06-04 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
CA2952044C (en) * 2014-06-13 2019-01-29 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
JP6455995B2 (ja) 2014-06-13 2019-01-23 ギリアード サイエンシーズ， インコーポレイテッド ホスファチジルイノシトール３−キナーゼ阻害剤
NZ726052A (en) 2014-06-13 2018-04-27 Gilead Sciences Inc Phosphatidylinositol 3-kinase inhibitors
AU2015274635B2 (en) 2014-06-13 2018-04-19 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
US9708348B2 (en) 2014-10-03 2017-07-18 Infinity Pharmaceuticals, Inc. Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
SG11201706287PA (en) 2015-02-20 2017-09-28 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MX382355B (es) 2015-04-10 2025-03-13 Araxes Pharma Llc Compuestos de quinazolina sustituidos y métodos de uso de los mismos.
EP3283462B1 (en) 2015-04-15 2020-12-02 Araxes Pharma LLC Fused-tricyclic inhibitors of kras and methods of use thereof
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
US10160761B2 (en) 2015-09-14 2018-12-25 Infinity Pharmaceuticals, Inc. Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same
WO2017045955A1 (en) * 2015-09-14 2017-03-23 Basf Se Heterobicyclic compounds
WO2017058792A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356347A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10689356B2 (en) 2015-09-28 2020-06-23 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356351A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10514986B2 (en) 2015-09-30 2019-12-24 Commvault Systems, Inc. Dynamic triggering of block-level backups based on block change thresholds and corresponding file identities in a data storage management system
US10457669B2 (en) 2015-10-21 2019-10-29 Otsuka Pharmaceutical Co., Ltd. Benzolactam compounds as protein kinase inhibitors
WO2017068064A1 (en) * 2015-10-22 2017-04-27 Selvita S.A. Pyridone derivatives and their use as kinase inhibitors
EP3377481A1 (en) 2015-11-16 2018-09-26 Araxes Pharma LLC 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
WO2017107089A1 (en) * 2015-12-23 2017-06-29 Merck Sharp & Dohme Corp. 3- (1h-pyrazol-4-yl) pyridineallosteric modulators of the m4 muscarinic acetylcholine receptor
WO2017107087A1 (en) * 2015-12-23 2017-06-29 Merck Sharp & Dohme Corp. 6, 7-dihydro-5h-pyrrolo [3, 4-b] pyridin-5-oneallosteric modulators of the m4 muscarinic acetylcholine receptor
ES2789756T3 (es) 2015-12-23 2020-10-26 Merck Sharp & Dohme Moduladores alostéricos de 6,7-dihidro-5H-pirrolo[3,4-b]piridin-5-ona del receptor de acetilcolina muscarínico M4
EA036388B1 (ru) * 2016-03-10 2020-11-03 Астразенека Аб Ингибиторы фосфатидилинозитол-3-киназы гамма
WO2017161116A1 (en) 2016-03-17 2017-09-21 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as pi3k kinase inhibitors
MY195528A (en) 2016-03-17 2023-01-30 Hoffmann La Roche 5-Ethyl-4-Methyl-Pyrazole-3-Carboxamide Derivative Having Activity as Agonist of Taar
GB201604970D0 (en) 2016-03-23 2016-05-04 Syngenta Participations Ag Improvements in or relating to organic compounds
US10919914B2 (en) 2016-06-08 2021-02-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
MX391135B (es) 2016-06-24 2025-03-21 Infinity Pharmaceuticals Inc Terapias de combinacion.
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
EP3519402A1 (en) 2016-09-29 2019-08-07 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10377743B2 (en) * 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
WO2018112842A1 (en) 2016-12-22 2018-06-28 Merck Sharp & Dohme Corp. 6,6-fused heteroaryl piperidine ether allosteric modulators of m4 muscarinic acetylcholine receptor
WO2018112843A1 (en) 2016-12-22 2018-06-28 Merck Sharp & Dohme Corp. Heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor
US11358959B2 (en) 2017-01-26 2022-06-14 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
CN110382482A (zh) 2017-01-26 2019-10-25 亚瑞克西斯制药公司 稠合的杂-杂二环化合物及其使用方法
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
WO2018140513A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
GB201706327D0 (en) 2017-04-20 2017-06-07 Otsuka Pharma Co Ltd A pharmaceutical compound
CN110831933A (zh) 2017-05-25 2020-02-21 亚瑞克西斯制药公司 喹唑啉衍生物作为突变kras、hras或nras的调节剂
JP2020521741A (ja) 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー がんの処置のための化合物およびその使用の方法
CN110869358A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 Kras的共价抑制剂
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
WO2018226545A1 (en) * 2017-06-09 2018-12-13 Merck Sharp & Dohme Corp. Azabicyclo[4.1.0]heptane allosteric modulators of the m4 muscarinic acetylcholine receptor
JP6647738B2 (ja) 2017-06-12 2020-02-14 矢崎総業株式会社 電池パック
WO2019000237A1 (en) * 2017-06-27 2019-01-03 Merck Sharp & Dohme Corp. ALLOSTERIC MODULATORS OF 3- (1H-PYRAZOL-4-YL) PYRIDINE FROM THE M4 ACETYLCHOLINE MUSCARINIC RECEPTOR
WO2019000236A1 (en) 2017-06-27 2019-01-03 Merck Sharp & Dohme Corp. ALLOSTERIC MODULATORS OF 3- (1H-PYRAZOL-4-YL) PYRIDINE FROM THE M4 ACETYLCHOLINE MUSCARINIC RECEPTOR
WO2019000238A1 (en) 2017-06-27 2019-01-03 Merck Sharp & Dohme Corp. 5- (PYRIDIN-3-YL) OXAZOLE ALLOSTERIC MODULATORS OF M4 ACETYLCHOLINE MUSCARINIC RECEPTOR
EP3774782A2 (en) * 2018-04-06 2021-02-17 Black Belt TX Ltd Atf6 inhibitors and uses thereof
MX2020011718A (es) 2018-05-04 2021-02-15 Incyte Corp Formas solidas de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr) y procesos para prepararlas.
ES3061844T3 (en) 2018-05-04 2026-04-07 Incyte Corp Salts of an fgfr inhibitor
BR112021001709A2 (pt) 2018-08-01 2021-05-04 Araxes Pharma Llc compostos espiro heterocíclicos e métodos de uso dos mesmos para o tratamento de câncer
WO2020102216A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Substituted heterocyclic derivatives as pi3k inhibitors
US11161838B2 (en) 2018-11-13 2021-11-02 Incyte Corporation Heterocyclic derivatives as PI3K inhibitors
US11078204B2 (en) 2018-11-13 2021-08-03 Incyte Corporation Heterocyclic derivatives as PI3K inhibitors
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
JP7644023B2 (ja) * 2019-04-10 2025-03-11 ナンジン ゼンシャイン ファーマシューティカルズ カンパニー リミテッド ホスファチジルイノシトール３－キナーゼ阻害剤
CN114206332B (zh) 2019-06-04 2024-08-23 艾库斯生物科学有限公司 2,3,5-三取代吡唑并[1,5-a]嘧啶化合物
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
TWI891666B (zh) 2019-10-14 2025-08-01 美商英塞特公司 作為ｆｇｆｒ抑制劑之雙環雜環
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2021113462A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Derivatives of an fgfr inhibitor
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
IL297625B2 (en) 2020-04-29 2026-05-01 Relay Therapeutics Inc PI3K-alpha inhibitors and methods of using them
CN114516856B (zh) * 2020-11-20 2025-05-23 安徽中科拓苒药物科学研究有限公司 二氢异喹啉酮和异吲哚啉酮衍生物及其用途
WO2022197577A1 (en) * 2021-03-17 2022-09-22 Merck Sharp & Dohme Llc Heteroaroyl amides as lrrk2 inhibitors, pharmaceutical compositions, and uses thereof
TW202304459A (zh) 2021-04-12 2023-02-01 美商英塞特公司 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法
EP4352060A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
JP2024522189A (ja) 2021-06-09 2024-06-11 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式ヘテロ環
WO2023081759A1 (en) * 2021-11-03 2023-05-11 Relay Therapeutics, Inc. Bifunctional pi3k-alpha inhibitors and uses thereof
CN118302427A (zh) * 2021-12-02 2024-07-05 上海翰森生物医药科技有限公司 稠环类衍生物调节剂、其制备方法和应用
KR102670554B1 (ko) * 2022-01-04 2024-05-30 주식회사 이노보테라퓨틱스 캐스파제 저해제로서의 신규한 이소인돌리논 유도체 화합물
US20250171444A1 (en) * 2022-03-04 2025-05-29 Synnovation Therapeutics, Inc. PI3Ka INHIBITORS
CN117683036A (zh) * 2022-09-09 2024-03-12 上海璎黎药业有限公司 一种含氮杂环化合物、其药物组合物及应用
WO2024153238A1 (zh) * 2023-01-20 2024-07-25 南京再明医药有限公司 四环化合物及其应用
WO2024251212A1 (en) * 2023-06-06 2024-12-12 Revir Therapeutics, Inc. Isoindolinone and dihydropyrrolopridinone compounds and uses thereof
WO2025179441A1 (zh) * 2024-02-27 2025-09-04 上海璎黎药业有限公司 一种三并环结构化合物、其药物组合物及应用

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS57134467A (en) * 1981-02-13 1982-08-19 Dai Ichi Seiyaku Co Ltd Pyridine derivative and its preparation
CA2527814A1 (en) * 2003-06-02 2004-12-16 Abbott Laboratories Isoindolin-1-one compounds as kinase inhibitors
EP1726585A4 (en) 2004-03-05 2009-07-15 Banyu Pharma Co Ltd DIARYLSUBSTITUTED FIVE-GLOSS HETEROCYCLUS DERIVAT
SE0400970D0 (sv) * 2004-04-14 2004-04-14 Astrazeneca Ab Nicotinic acetylcholine receptor ligands
TW200613272A (en) * 2004-08-13 2006-05-01 Astrazeneca Ab Isoindolone compounds and their use as metabotropic glutamate receptor potentiators
GB0504753D0 (en) 2005-03-08 2005-04-13 Astrazeneca Ab Chemical compounds
TW200728277A (en) * 2005-06-29 2007-08-01 Palau Pharma Sa Bicyclic derivatives as P38 inhibitors
TW200804281A (en) * 2006-02-16 2008-01-16 Astrazeneca Ab New metabotropic glutamate receptor-potentiating isoindolones
CN101421237A (zh) * 2006-02-16 2009-04-29 阿斯利康(瑞典)有限公司 增效亲代谢性谷氨酸受体的异吲哚酮
US8110681B2 (en) * 2006-03-17 2012-02-07 The United States Of America As Represented By The Secretary, Department Of Health And Human Services Compounds for the treatment of spinal muscular atrophy and other uses
WO2008127712A1 (en) * 2007-04-11 2008-10-23 Exelixis, Inc. Pyrido [2, 3-d] pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer
EP3309152B1 (en) 2009-12-22 2020-09-09 Vertex Pharmaceuticals Incorporated Isoindolinone inhibitors of phosphatidylinositol 3-kinase

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017114916A (ja) * 2009-12-22 2017-06-29 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ ホスファチジルイノシトール３−キナーゼのイソインドリノンインヒビター

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