RU2573569C2 - Ингибиторы фосфатидилинозитол-3-киназы на основе изоиндолинона - Google Patents

Ингибиторы фосфатидилинозитол-3-киназы на основе изоиндолинона Download PDF

Info

Publication number
RU2573569C2
RU2573569C2 RU2012131416/04A RU2012131416A RU2573569C2 RU 2573569 C2 RU2573569 C2 RU 2573569C2 RU 2012131416/04 A RU2012131416/04 A RU 2012131416/04A RU 2012131416 A RU2012131416 A RU 2012131416A RU 2573569 C2 RU2573569 C2 RU 2573569C2
Authority
RU
Russia
Prior art keywords
compound
alkyl
mmol
aliphatic group
group
Prior art date
Application number
RU2012131416/04A
Other languages
English (en)
Russian (ru)
Other versions
RU2012131416A (ru
Inventor
Алекс АРОНОВ
Джон Х. КАМ
Роберт Дж. ДЭВИС
Альберт К. ПИРС
Цзянь ВАН
Сугантини НАНТАКУМАР
Дзингронг КАО
Упул К. БАНДАРАГЕ
Элейн КРЮГЕР
Амауд Ле ТИРАН
Юшенг ЛИАО
Дэвид МЕССЕРСМИТ
Филип Н. КОЛЛИЕР
Рональд ГРЕЙ
Хардвин О'Доуд
Джеймс А. ХЕНДЕРСОН
Анн-Лор Грийо
Original Assignee
Вертекс Фармасьютикалз Инкорпорейтед
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=43859800&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=RU2573569(C2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Вертекс Фармасьютикалз Инкорпорейтед filed Critical Вертекс Фармасьютикалз Инкорпорейтед
Publication of RU2012131416A publication Critical patent/RU2012131416A/ru
Application granted granted Critical
Publication of RU2573569C2 publication Critical patent/RU2573569C2/ru

Links

Classifications

    • 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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (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)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Psychology (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (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)
RU2012131416/04A 2009-12-22 2010-12-21 Ингибиторы фосфатидилинозитол-3-киназы на основе изоиндолинона RU2573569C2 (ru)

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

Publications (2)

Publication Number Publication Date
RU2012131416A RU2012131416A (ru) 2014-01-27
RU2573569C2 true RU2573569C2 (ru) 2016-01-20

Family

ID=43859800

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2012131416/04A RU2573569C2 (ru) 2009-12-22 2010-12-21 Ингибиторы фосфатидилинозитол-3-киназы на основе изоиндолинона

Country Status (16)

Country Link
US (4) US20120040950A1 (enExample)
EP (3) EP2516417B1 (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) ES2655391T3 (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
RU2833422C1 (ru) * 2020-11-20 2025-01-21 Тарапьютикс Сайенс Инк. Производные дигидроизохинолинона и изоиндолинона и их применение

Families Citing this family (117)

* 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
AU2009204483B2 (en) 2008-01-04 2014-03-13 Intellikine, Llc Certain chemical entities, compositions and methods
WO2010036380A1 (en) 2008-09-26 2010-04-01 Intellikine, Inc. Heterocyclic kinase inhibitors
WO2010129816A2 (en) 2009-05-07 2010-11-11 Intellikine, Inc. Heterocyclic compounds and uses thereof
NZ600954A (en) 2009-12-22 2013-11-29 Isoindolinone inhibitors of phosphatidylinositol 3-kinase
JP5951600B2 (ja) 2010-05-21 2016-07-13 インフィニティー ファーマシューティカルズ， インコーポレイテッド キナーゼ調節のための、化合物、組成物および方法
US8901133B2 (en) 2010-11-10 2014-12-02 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
KR20180080358A (ko) 2011-01-10 2018-07-11 인피니티 파마슈티칼스, 인코포레이티드 이소퀴놀린온 및 이의 고체 형태의 제조 방법
EP2734530A1 (en) 2011-07-19 2014-05-28 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
CN103930422A (zh) 2011-07-19 2014-07-16 无限药品股份有限公司 杂环化合物及其用途
CN103998442B (zh) 2011-08-29 2016-09-14 无限药品股份有限公司 杂环化合物及其用途
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
WO2013161312A1 (en) * 2012-04-25 2013-10-31 Raqualia Pharma Inc. Pyrrolopyridinone derivatives as ttx-s blockers
US9611267B2 (en) 2012-06-13 2017-04-04 Incyte Holdings Corporation Substituted tricyclic compounds as FGFR inhibitors
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
UA110688C2 (uk) * 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
IL291945B2 (en) 2012-11-01 2025-11-01 Infinity Pharmaceuticals Inc Treatment of cancers using pi3 kinase isoform modulators
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
TWI649318B (zh) 2013-04-19 2019-02-01 英塞特控股公司 作為ｆｇｆｒ抑制劑之雙環雜環
RU2018142605A (ru) 2013-09-25 2019-02-04 Вертекс Фармасьютикалз Инкорпорейтед Селективный ингибитор фосфатидилинозитол-3-киназы-гамма
MX389256B (es) 2013-10-04 2025-03-20 Infinity Pharmaceuticals Inc Compuestos heterociclicos y usos de los mismos.
WO2015051241A1 (en) 2013-10-04 2015-04-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
EP4066834A1 (en) 2014-03-19 2022-10-05 Infinity Pharmaceuticals, Inc. Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders
US20150320755A1 (en) 2014-04-16 2015-11-12 Infinity Pharmaceuticals, Inc. Combination therapies
WO2015160307A1 (en) * 2014-04-16 2015-10-22 Nanyang Technological University Allenamide as an orthogonal handle for selective modification of cysteine in peptides and proteins
MX373274B (es) 2014-04-23 2020-04-16 Takeda Pharmaceuticals Co Derivados de isoindolin-1-ona con actividad de modulador alostérico positivo del receptor colinérgico muscarínico m1 para el tratamiento de la enfermedad de alzheimer.
CA2952018A1 (en) 2014-06-13 2015-12-17 Gilead Sciences, Inc. Quinazolinone derivatives as phosphatidylinositol 3-kinase inhibitors
CA2952025A1 (en) 2014-06-13 2015-12-17 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
CA2952037A1 (en) 2014-06-13 2015-12-17 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
US9499523B2 (en) * 2014-06-13 2016-11-22 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
WO2016054491A1 (en) 2014-10-03 2016-04-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
AU2016219822B2 (en) 2015-02-20 2020-07-09 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
ES2898765T3 (es) 2015-04-10 2022-03-08 Araxes Pharma Llc Compuestos de quinazolina sustituidos y métodos de uso de los mismos
ES2856880T3 (es) 2015-04-15 2021-09-28 Araxes Pharma Llc Inhibidores tricíclicos condensados de KRAS y métodos de uso de los mismos
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
CN108349985A (zh) 2015-09-14 2018-07-31 无限药品股份有限公司 异喹啉酮的固体形式、其制备方法、包含其的组合物及其使用方法
WO2017045955A1 (en) * 2015-09-14 2017-03-23 Basf Se Heterobicyclic compounds
EP3356353A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10975071B2 (en) 2015-09-28 2021-04-13 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10730867B2 (en) 2015-09-28 2020-08-04 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
US10689356B2 (en) 2015-09-28 2020-06-23 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10647703B2 (en) 2015-09-28 2020-05-12 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058792A1 (en) 2015-09-28 2017-04-06 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
ES2989326T3 (es) 2015-10-21 2024-11-26 Otsuka Pharma Co Ltd Compuestos de benzolactama como inhibidores de la proteína cinasa
MX2018004879A (es) * 2015-10-22 2019-02-28 Selvita S A Nuevos derivados de piridona y su uso como inhibidores de quinasas.
US10414757B2 (en) 2015-11-16 2019-09-17 Araxes Pharma Llc 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
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
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
CA3015893C (en) * 2016-03-10 2021-11-09 Astrazeneca Ab Novel inhibitors of phosphatidylinositol 3-kinase gamma
US10759806B2 (en) 2016-03-17 2020-09-01 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as PI3K kinase inhibitors
JP6814814B2 (ja) 2016-03-17 2021-01-20 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｔａａｒのアゴニストとしての活性を有する５−エチル−４−メチル−ピラゾール−３−カルボキサミド誘導体
GB201604970D0 (en) 2016-03-23 2016-05-04 Syngenta Participations Ag Improvements in or relating to organic compounds
WO2017214269A1 (en) 2016-06-08 2017-12-14 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
CA3028718A1 (en) 2016-06-24 2017-12-28 Infinity Pharmaceuticals, Inc. Combination therapies
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
WO2018064510A1 (en) 2016-09-29 2018-04-05 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
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
EP3573971A1 (en) 2017-01-26 2019-12-04 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
WO2018140600A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused hetero-hetero bicyclic compounds and methods of use thereof
GB201706327D0 (en) 2017-04-20 2017-06-07 Otsuka Pharma Co Ltd A pharmaceutical compound
CN110869357A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 化合物及其用于治疗癌症的使用方法
WO2018218069A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant kras, hras or nras
KR20200010306A (ko) 2017-05-25 2020-01-30 아락세스 파마 엘엘씨 Kras의 공유적 억제제
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
US10945771B2 (en) 2017-06-09 2021-03-16 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
WO2019000238A1 (en) * 2017-06-27 2019-01-03 Merck Sharp & Dohme Corp. 5- (PYRIDIN-3-YL) OXAZOLE ALLOSTERIC MODULATORS OF M4 ACETYLCHOLINE MUSCARINIC RECEPTOR
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
KR20210028144A (ko) * 2018-04-06 2021-03-11 블랙 벨트 티엑스 리미티드 Atf6 저해제 및 그의 용도
TW201946630A (zh) 2018-05-04 2019-12-16 美商英塞特公司 Fgfr抑制劑之鹽
ES2991427T3 (es) 2018-05-04 2024-12-03 Incyte Corp Formas sólidas de un inhibidor de FGFR y procedimientos para preparar las mismas
CA3107168A1 (en) 2018-08-01 2020-02-06 Araxes Pharma Llc Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer
WO2020102150A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Heterocyclic derivatives as pi3k inhibitors
WO2020102216A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Substituted heterocyclic derivatives as pi3k inhibitors
WO2020102198A1 (en) 2018-11-13 2020-05-22 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
AU2020288610A1 (en) 2019-06-04 2022-01-27 Arcus Biosciences, Inc. 2,3,5-trisubstituted pyrazolo[1,5-a]pyrimidine compounds
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
GEAP202415945A (en) 2019-10-14 2024-04-25 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
KR20250057919A (ko) * 2020-04-29 2025-04-29 릴레이 테라퓨틱스, 인크. PI3Kα 억제제 및 이의 사용 방법
EP4249481A4 (en) * 2020-11-20 2024-10-30 Hefei Institutes of Physical Science, Chinese Academy of Sciences DIHYDROISOQUINOLINONE AND ISOINDOLINONE DERIVATIVES AND USES THEREOF
WO2022197577A1 (en) * 2021-03-17 2022-09-22 Merck Sharp & Dohme Llc Heteroaroyl amides as lrrk2 inhibitors, pharmaceutical compositions, and uses thereof
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
AR126101A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
EP4426286A4 (en) * 2021-11-03 2025-12-24 Relay Therapeutics Inc Bifunctional PI3K-Alpha Inhibitors and Their Uses
WO2023098880A1 (zh) * 2021-12-02 2023-06-08 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
EP4585596A4 (en) * 2022-09-09 2025-12-10 Shanghai Yingli Pharm Co Ltd Nitrogen-containing heterocyclic compound, pharmaceutical composition thereof and uses thereof
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

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004108672A1 (en) * 2003-06-02 2004-12-16 Abbott Laboratories Isoindolin-1-one compounds as kinase inhibitors
WO2007000339A1 (en) * 2005-06-29 2007-01-04 Palau Pharma, S.A. Bicyclic derivatives as p38 kinase inhibitors
WO2007095024A1 (en) * 2006-02-16 2007-08-23 Astrazeneca Ab Metabotropic glutamate receptor-potentiating γsoindolones
WO2007109211A2 (en) * 2006-03-17 2007-09-27 Government Of The United States Of America, Represented By The Secretary, Department Of Health And Human Services 1-oxo-isoindoline compounds for the treatment of spinal muscular atrophy and other uses
EA200970936A1 (ru) * 2007-04-11 2010-02-26 Экселиксис, Инк. СОЕДИНЕНИЯ ПИРИДО[2,3-d]ПИРИМИДИН-7-ОНА В КАЧЕСТВЕ ИНГИБИТОРОВ PI3K-АЛЬФА ДЛЯ ЛЕЧЕНИЯ РАКА

Family Cites Families (7)

* 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
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
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
NZ600954A (en) 2009-12-22 2013-11-29 Isoindolinone inhibitors of phosphatidylinositol 3-kinase

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004108672A1 (en) * 2003-06-02 2004-12-16 Abbott Laboratories Isoindolin-1-one compounds as kinase inhibitors
WO2007000339A1 (en) * 2005-06-29 2007-01-04 Palau Pharma, S.A. Bicyclic derivatives as p38 kinase inhibitors
WO2007095024A1 (en) * 2006-02-16 2007-08-23 Astrazeneca Ab Metabotropic glutamate receptor-potentiating γsoindolones
WO2007109211A2 (en) * 2006-03-17 2007-09-27 Government Of The United States Of America, Represented By The Secretary, Department Of Health And Human Services 1-oxo-isoindoline compounds for the treatment of spinal muscular atrophy and other uses
EA200970936A1 (ru) * 2007-04-11 2010-02-26 Экселиксис, Инк. СОЕДИНЕНИЯ ПИРИДО[2,3-d]ПИРИМИДИН-7-ОНА В КАЧЕСТВЕ ИНГИБИТОРОВ PI3K-АЛЬФА ДЛЯ ЛЕЧЕНИЯ РАКА

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
J. HURS, D. G. WIBBERLEY: "22. 2-Bromomethylnicotinates: reaction with nucleophilic reagents", J. CHEM. SOC., 1962, pages 119-122. *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2833422C1 (ru) * 2020-11-20 2025-01-21 Тарапьютикс Сайенс Инк. Производные дигидроизохинолинона и изоиндолинона и их применение

Also Published As

Publication number Publication date
NZ600954A (en) 2013-11-29
EP3309152B1 (en) 2020-09-09
IL220625A (en) 2017-05-29
EP3309152A1 (en) 2018-04-18
ES2655391T3 (es) 2018-02-19
EP2516417A1 (en) 2012-10-31
ES2842399T3 (es) 2021-07-14
AU2010341573B2 (en) 2016-10-13
KR20120097406A (ko) 2012-09-03
RU2012131416A (ru) 2014-01-27
KR101758046B1 (ko) 2017-07-14
MX350761B (es) 2017-09-18
US20120040950A1 (en) 2012-02-16
US20120202784A1 (en) 2012-08-09
JP5721187B2 (ja) 2015-05-20
EP3808739A1 (en) 2021-04-21
CA2785499A1 (en) 2011-07-21
JP2015101589A (ja) 2015-06-04
HK1253412A1 (en) 2019-06-14
AU2010341573A1 (en) 2012-07-19
CN102762548B (zh) 2014-11-26
SG10201502073PA (en) 2015-05-28
CA2785499C (en) 2017-05-02
CN102762548A (zh) 2012-10-31
BR112012018386A8 (pt) 2017-12-19
JP2017114916A (ja) 2017-06-29
BR112012018386A2 (pt) 2017-06-20
JP6132410B2 (ja) 2017-05-24
US20170260175A1 (en) 2017-09-14
US10183933B2 (en) 2019-01-22
WO2011087776A1 (en) 2011-07-21
US9676759B2 (en) 2017-06-13
EP2516417B1 (en) 2017-10-11
US20140038936A1 (en) 2014-02-06
CL2012001714A1 (es) 2013-04-12
SG181917A1 (en) 2012-08-30
JP6510580B2 (ja) 2019-05-08
US8466288B2 (en) 2013-06-18
MX2012007403A (es) 2012-09-12
JP2018131449A (ja) 2018-08-23
JP2013515074A (ja) 2013-05-02

Similar Documents

Publication Publication Date Title
RU2573569C2 (ru) Ингибиторы фосфатидилинозитол-3-киназы на основе изоиндолинона
EP3652164B1 (en) Phenylacetamides as inhibitors of rock
AU2009281822B2 (en) cMET inhibitors
AU2019382504B2 (en) Cyclic ureas
AU2013251804A1 (en) DNA-PK inhibitors
AU2013276519B2 (en) 1,3-dihydro-2H-benzimidazol-2-one derivatives substituted with heterocycles as respiratory syncytial virus antiviral agents
CA2930414A1 (en) Tetrahydroquinoline compositions as bet bromodomain inhibitors
CA2963607A1 (en) Heparan sulfate biosynthesis inhibitors for the treatment of diseases
EP3741752A1 (en) Tam family kinase /and csf1r kinase inhibitor and use thereof
AU2010250055A1 (en) Tri-cyclic pyrazolopyridine kinase inhibitors
CN105073751A (zh) 作为酪蛋白激酶1δ/ε抑制剂的新的取代的咪唑
JP2010519174A (ja) ｃ−Ｍｅｔの複素環阻害薬およびその使用方法
CN120225521A (zh) Akt1调节剂
JP2013506691A (ja) ホスファチジルイノシトール３−キナーゼのピラゾール阻害薬
HK1253412B (en) Isoindolinone inhibitors of phosphatidylinositol 3-kinase