EA032458B1 - Гетероарилы и их применение - Google Patents

Гетероарилы и их применение Download PDF

Info

Publication number
EA032458B1
EA032458B1 EA201691421A EA201691421A EA032458B1 EA 032458 B1 EA032458 B1 EA 032458B1 EA 201691421 A EA201691421 A EA 201691421A EA 201691421 A EA201691421 A EA 201691421A EA 032458 B1 EA032458 B1 EA 032458B1
Authority
EA
Eurasian Patent Office
Prior art keywords
mmol
pharmaceutically acceptable
compound
acceptable salt
methyl
Prior art date
Application number
EA201691421A
Other languages
English (en)
Russian (ru)
Other versions
EA201691421A1 (ru
Inventor
Инду Т. Бхаратхан
Крис Блэкберн
Джеффри П. Кьяварри
Джоухара Чуитар
Кортни А. Каллис
Натали Д'Амор
Пол Э. Флеминг
Кеннет М. Гигстад
Криста Э. Гипсон
Марио Жирар
Юнбо Ху
Дженис Ли
Ган Ли
Мансурех Резаеи
Майкл Д. Синтчак
Франсуа Суси
Стефен Г. Страуд
Трисия Дж. Вос
Тцзу-Тшинь Вонг
Хе Сюй
Тяньлинь Сюй
Инчунь Е
Original Assignee
Милленниум Фармасьютикалз, Инк.
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=53543363&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA032458(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Милленниум Фармасьютикалз, Инк. filed Critical Милленниум Фармасьютикалз, Инк.
Publication of EA201691421A1 publication Critical patent/EA201691421A1/ru
Publication of EA032458B1 publication Critical patent/EA032458B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/33—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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/549—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
EA201691421A 2014-01-14 2015-01-13 Гетероарилы и их применение EA032458B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461927055P 2014-01-14 2014-01-14
US201462054742P 2014-09-24 2014-09-24
PCT/US2015/011191 WO2015108861A1 (en) 2014-01-14 2015-01-13 Heteroaryls and uses thereof

Publications (2)

Publication Number Publication Date
EA201691421A1 EA201691421A1 (ru) 2017-05-31
EA032458B1 true EA032458B1 (ru) 2019-05-31

Family

ID=53543363

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201691421A EA032458B1 (ru) 2014-01-14 2015-01-13 Гетероарилы и их применение

Country Status (26)

Country Link
US (3) US9802960B2 (enExample)
EP (1) EP3094325B1 (enExample)
JP (1) JP6609258B2 (enExample)
KR (1) KR20160122736A (enExample)
CN (1) CN105916503B (enExample)
AP (1) AP2016009368A0 (enExample)
AU (1) AU2015206652A1 (enExample)
BR (1) BR112016016289B1 (enExample)
CA (1) CA2935867C (enExample)
CL (1) CL2016001805A1 (enExample)
CR (1) CR20160363A (enExample)
DO (1) DOP2016000173A (enExample)
EA (1) EA032458B1 (enExample)
EC (1) ECSP16067303A (enExample)
ES (1) ES2908042T3 (enExample)
GE (2) GEP20196983B (enExample)
IL (1) IL246755A0 (enExample)
MX (1) MX2016009135A (enExample)
MY (1) MY182908A (enExample)
PE (1) PE20161313A1 (enExample)
PH (1) PH12016501388A1 (enExample)
SG (1) SG11201604820XA (enExample)
TN (1) TN2016000270A1 (enExample)
TW (1) TWI662024B (enExample)
UY (1) UY35951A (enExample)
WO (1) WO2015108861A1 (enExample)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104230922B (zh) 2013-06-19 2016-12-28 中国科学院上海药物研究所 一类五元杂环并吡啶类化合物及其制备方法和用途
TN2016000270A1 (en) 2014-01-14 2017-10-06 Millennium Pharm Inc Heteroaryls and uses thereof.
WO2015108881A1 (en) 2014-01-14 2015-07-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
WO2017068412A1 (en) * 2015-10-21 2017-04-27 Otsuka Pharmaceutical Co., Ltd. Benzolactam compounds as protein kinase inhibitors
PL3416945T3 (pl) 2016-02-19 2020-12-28 Sprint Bioscience Ab Związki 6-arylo-4-(morfolin-4-ylo)-1h-pirydyn-2-onu przydatne w leczeniu nowotworu i cukrzycy
PT3416957T (pt) 2016-02-19 2020-09-25 Sprint Bioscience Ab Compostos 6-heterociclil-4-morfolin-4-ilpiridin-2-ona úteis para o tratamento do cancro e da diabetes
WO2018144791A1 (en) * 2017-02-03 2018-08-09 Millennium Pharmaceuticals, Inc. Combination of vps34 inhibitors and mtor inhibitors
GB201706327D0 (en) * 2017-04-20 2017-06-07 Otsuka Pharma Co Ltd A pharmaceutical compound
BR102018007822A2 (pt) 2017-04-20 2018-11-06 Gilead Sciences, Inc. composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição
HRP20220497T1 (hr) 2017-08-23 2022-05-27 Sprint Bioscience Ab Spoj morfolinilpiridona
IL302356A (en) * 2017-08-23 2023-06-01 Sprint Bioscience Ab Pyridylpyridone compounds
PL3672948T3 (pl) * 2017-08-23 2022-12-05 Sprint Bioscience Ab Związki pirydynoamino-pirydonu i pirymidynoamino-pirydonu
IL302355A (en) 2017-08-23 2023-06-01 Sprint Bioscience Ab Azaindolylpyridone and diazaindolylpyridone compounds
EP3684761A1 (en) 2017-09-18 2020-07-29 Basf Se Substituted trifluoromethyloxadiazoles for combating phytopathogenic fungi
WO2019160882A1 (en) 2018-02-13 2019-08-22 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
PE20210642A1 (es) 2018-07-13 2021-03-23 Gilead Sciences Inc Inhibidores de pd-1/pd-l1
WO2020045941A1 (ko) * 2018-08-27 2020-03-05 주식회사 대웅제약 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물
KR102328682B1 (ko) * 2018-08-27 2021-11-18 주식회사 대웅제약 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물
CN109608444B (zh) * 2018-11-27 2022-02-11 中国药科大学 含异吲哚啉酮的erk抑制剂及其制备方法与用途
AU2020345950A1 (en) * 2019-09-11 2022-03-31 Prelude Therapeutics Incorporated CDK inhibitors and their use as pharmaceuticals
CN112574207B (zh) * 2019-09-30 2023-04-11 南京药石科技股份有限公司 Erk1/2蛋白激酶抑制剂及其用途
CN115135648B (zh) * 2020-02-13 2024-02-09 劲方医药科技(上海)有限公司 二氢萘啶酮类化合物，其制法与医药上的用途
CN117083064A (zh) 2020-11-25 2023-11-17 德西费拉制药有限责任公司 作为vps34抑制剂用于治疗病毒感染的吡啶基吡啶酮衍生物
TWI824626B (zh) * 2021-08-02 2023-12-01 大陸商勁方醫藥科技(上海)有限公司 Ripk1抑制劑的晶型及其酸式鹽和其酸式鹽的晶型
US12319655B2 (en) 2021-12-09 2025-06-03 Deciphera Pharmaceuticals, Llc RAF kinase inhibitors and methods of use thereof
EP4604955A1 (en) 2022-10-18 2025-08-27 Pfizer Inc. Use of patatin-like phospholipase domain-containing protein 3 compounds
IL319392A (en) 2022-10-18 2025-05-01 Pfizer Pectin-like phospholipase domain-containing protein 3 (PNPLA3) modification preparations
GB202216324D0 (en) * 2022-11-02 2022-12-14 Cerevance Ltd Novel compounds
WO2025184010A1 (en) * 2024-03-01 2025-09-04 Merck Sharp & Dohme Llc N-biaryl sulfonamides as modulators of the hippo pathway

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20110130380A1 (en) * 2009-09-04 2011-06-02 Barsanti Paul A Heteroaryl Kinase Inhibitors
US20130102608A1 (en) * 2010-07-05 2013-04-25 Merck Patent Gesellschaft Mit Beschrankter Haftung Bipyridyl derivatives

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1562911B1 (en) 2002-11-01 2010-01-06 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of jak and other protein kinases
FR2850652B1 (fr) 2003-01-31 2008-05-30 Aventis Pharma Sa Nouveaux derives d'uree cyclique, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de kinases
SE0402735D0 (sv) 2004-11-09 2004-11-09 Astrazeneca Ab Novel compounds
GB0425026D0 (en) * 2004-11-12 2004-12-15 Biofocus Discovery Ltd Compounds which bind to the active site of protein kinase enzymes
EP1814856A1 (en) 2004-11-12 2007-08-08 Galapagos N.V. Nitrogen heteroaromatic compounds which bind to the active site of protein kinase enzymes
CN101111479A (zh) * 2004-12-16 2008-01-23 沃泰克斯药物股份有限公司 可用作激酶抑制剂的吡啶酮
MX2007007330A (es) * 2004-12-16 2007-10-04 Vertex Pharma Piridonas de utilidad como inhibidores de quinasas .
US7601716B2 (en) 2006-05-01 2009-10-13 Cephalon, Inc. Pyridopyrazines and derivatives thereof as ALK and c-Met inhibitors
WO2007135398A1 (en) 2006-05-22 2007-11-29 Astrazeneca Ab Indole derivatives
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
JP5336375B2 (ja) 2006-08-30 2013-11-06 セルゾーム リミテッド キナーゼ阻害剤としてのトリアゾール誘導体
UA96964C2 (ru) 2006-12-04 2011-12-26 Астразенека Аб Соединения полициклической мочевины с антибактериальными свойствами
EP2094682A2 (en) 2006-12-22 2009-09-02 Novartis AG Heteroaryl-heteroaryl compounds as cdk inhibitors for the treatment of cancer, inflammation and viral infections
UY31137A1 (es) 2007-06-14 2009-01-05 Smithkline Beecham Corp Derivados de quinazolina como inhibidores de la pi3 quinasa
MX2010001020A (es) 2007-07-26 2010-03-01 Novartis Ag Derivados de pirimidina utiles para el tratamiento de condiciones inflamatorias o alergicas.
US7928140B2 (en) 2007-08-02 2011-04-19 Amgen Inc. Benzothiazole PI3 kinase modulators for cancer treatment
JP2010539239A (ja) 2007-09-17 2010-12-16 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Ｐｉ３キナーゼ阻害剤としてのピリドピリミジン誘導体
JP2011500823A (ja) * 2007-10-22 2011-01-06 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Ｐｉ３キナーゼ阻害物質としてのピリドスルホンアミド誘導体
US7820665B2 (en) 2007-12-19 2010-10-26 Amgen Inc. Imidazopyridazine inhibitors of PI3 kinase for cancer treatment
US8343966B2 (en) 2008-01-11 2013-01-01 Novartis Ag Organic compounds
US8268834B2 (en) 2008-03-19 2012-09-18 Novartis Ag Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme
US8309577B2 (en) 2008-04-23 2012-11-13 Bristol-Myers Squibb Company Quinuclidine compounds as α-7 nicotinic acetylcholine receptor ligands
JP5599783B2 (ja) 2008-05-30 2014-10-01 アムジエン・インコーポレーテツド Ｐｉ３キナーゼの阻害薬
EP2280946B1 (en) 2008-06-05 2016-02-10 Glaxo Group Limited 4-carboxamide indazole derivatives useful as inhibitors of p13-kinases
EP2311842A3 (en) 2008-06-24 2011-07-13 Takeda Pharmaceutical Company Limited PI3K/M TOR inhibitors
WO2010007100A1 (en) 2008-07-15 2010-01-21 Cellzome Ltd 7-substituted amino triazoles as pi3k inhibitors
BRPI0916576A2 (pt) 2008-08-04 2017-06-27 Chdi Inc pelo menos uma entidade química, composição farmacêutica, e, método para tratar uma condição ou distúrbio.
CA2743242A1 (en) 2008-11-11 2010-05-20 Eli Lilly And Company P70 s6 kinase inhibitor and mtor inhibitor combination therapy
WO2010057877A1 (en) * 2008-11-18 2010-05-27 Cellzome Limited 7-pyridinyl- or phenyl- substituted triazolo [1, 5 -a] pyridines as pi3k inhibitors
US8071605B2 (en) 2008-12-12 2011-12-06 Astrazeneca Ab Piperidine compounds for use in the treatment of bacterial infections
WO2010135524A1 (en) 2009-05-22 2010-11-25 Exelixis, Inc. Benzoxazepines based p13k/mt0r inhibitors against proliferative diseases
US8435980B2 (en) 2009-07-15 2013-05-07 Abbvie Inc. Pyrrolopyridine inhibitors of kinases
JP2011033670A (ja) * 2009-07-30 2011-02-17 Sony Corp 光学ファインダユニットおよび撮像装置
EP2531500B1 (en) * 2010-02-05 2018-01-24 Merck Patent GmbH Hetaryl-[1,8]naphthyridine derivatives
ES2550939T3 (es) 2010-07-16 2015-11-13 Nivalis Therapeutics, Inc. Nuevos compuestos de dihidropiridin-2-(1H)-ona como inhibidores de la S-nitrosoglutatión reductasa y antagonistas del receptor de la neurocinina-3
CN103209960A (zh) 2010-07-26 2013-07-17 百时美施贵宝公司 用作cyp17抑制剂的磺酰胺化合物
EP2603214A4 (en) 2010-08-11 2013-12-18 Millennium Pharm Inc HETEROARYLE AND USES THEREOF
US8478700B2 (en) 2010-08-11 2013-07-02 Brightedge Technologies, Inc. Opportunity identification and forecasting for search engine optimization
US8859768B2 (en) 2010-08-11 2014-10-14 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
WO2012037108A1 (en) 2010-09-13 2012-03-22 Glaxosmithkline Llc Aminoquinoline derivatives as antiviral agents
WO2012066065A1 (en) 2010-11-17 2012-05-24 Novartis Ag Phenyl-heteroaryl amine compounds and their uses
CA2816679A1 (en) 2010-11-17 2012-05-24 Novartis Ag 3-(aminoaryl)-pyridine compounds
EA201390917A1 (ru) * 2010-12-21 2013-12-30 Новартис Аг Дигетероарильные соединения в качестве ингибиторов vps34
PT2655375E (pt) 2010-12-23 2015-03-02 Sanofi Sa Derivados de pirimidinona, sua preparação e sua utilização farmacêutica
AR085013A1 (es) * 2011-01-26 2013-08-07 Sanofi Aventis Derivados de acido 3-heteroaroilamino-propionico sustituidos y su uso como sustancias farmaceuticas
WO2012101066A1 (en) 2011-01-28 2012-08-02 Novartis Ag Pyridine biaryl amine compounds and their uses
WO2012101062A1 (en) 2011-01-28 2012-08-02 Novartis Ag Substituted bi-heteroaryl compounds as cdk9 inhibitors and their uses
WO2012101064A1 (en) 2011-01-28 2012-08-02 Novartis Ag N-acyl pyrimidine biaryl compounds as protein kinase inhibitors
DE102011077104A1 (de) 2011-06-07 2012-12-13 Siemens Aktiengesellschaft Verfahren zur Gewinnung von metallhaltigen Wertstoffen aus einem metallhaltige Wertstoffe enthaltenden suspensionsartigen Massestrom
KR101502500B1 (ko) 2011-07-01 2015-03-16 주식회사 엘지화학 비수 전해액 및 이를 이용한 리튬 이차전지
UA111382C2 (uk) * 2011-10-10 2016-04-25 Оріон Корпорейшн Інгібітори протеїнкінази
TW201331194A (zh) 2011-12-23 2013-08-01 Millennium Pharm Inc 雜芳基化合物及其用途
AU2013222345B2 (en) 2012-02-22 2017-09-07 Sanford-Burnham Medical Research Institute Sulfonamide compounds and uses as TNAP inhibitors
CA2873861C (en) * 2012-04-05 2021-01-19 Boehringer Ingelheim International Gmbh Naphthyridinone derivatives as inhibitors of cytomegalovirus dna polymerase
FR2992314B1 (fr) 2012-06-22 2015-10-16 Sanofi Sa Nouveaux derives de 2,3-dihydro-1h-imidazo{1,2-a}pyrimidin-5-one et 1,2,3,4-tetrahydro-pyrimido{1,2-a}pyrimidin-6-one comportant une morpholine substituee, leur preparation et leur utilisation pharmaceutique
WO2014053533A1 (en) * 2012-10-05 2014-04-10 Sanofi Use of substituted 3-heteroaroylamino-propionic acid derivatives as pharmaceuticals for prevention/treatment of atrial fibrillation
WO2014058691A1 (en) 2012-10-08 2014-04-17 Merck Sharp & Dohme Corp. Inhibitors of irak4 activity
WO2014083327A1 (en) 2012-11-27 2014-06-05 Md Pharma Ab Adenine derivatives suitable for the treatment of (inter alia) muscular dystrophy
GB201223265D0 (en) 2012-12-21 2013-02-06 Selvita Sa Novel benzimidazole derivatives as kinase inhibitors
BR112015016580A2 (pt) * 2013-01-11 2017-07-11 Fujifilm Corp composto heterocíclico contendo nitrogênio ou sal deste
TW201444820A (zh) 2013-03-13 2014-12-01 Abbvie Inc 吡啶ｃｄｋ９激酶抑制劑
US9242969B2 (en) * 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
TN2016000270A1 (en) * 2014-01-14 2017-10-06 Millennium Pharm Inc Heteroaryls and uses thereof.
WO2015108881A1 (en) 2014-01-14 2015-07-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
UY36294A (es) * 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
JP6636014B2 (ja) * 2014-09-12 2020-01-29 ノバルティス アーゲー Ｒａｆキナーゼ阻害剤としての化合物および組成物

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20110130380A1 (en) * 2009-09-04 2011-06-02 Barsanti Paul A Heteroaryl Kinase Inhibitors
US20130102608A1 (en) * 2010-07-05 2013-04-25 Merck Patent Gesellschaft Mit Beschrankter Haftung Bipyridyl derivatives

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
PubChem Substance summary for CID 10468190 Deposit date 25 October 2006 (25.10.2006), p. 1 *
PubChem Substance summary for CID 13066345 Deposit date 08 February 2007 (08.02.2007), p. 2 *
PubChem Substance summary for CID 4636058 Deposit date 21 July 2010 (21.07.2010), p. 2 *
PubChem Substance summary for CID11566395 Deposit date 26 October 2006 (26.10.2006), p. 2 *
PubChem Substance summary for CID46315357 Deposit date 21 July 2010 (21.07.2010), p. 2 *

Also Published As

Publication number Publication date
US9751854B2 (en) 2017-09-05
US20170073326A1 (en) 2017-03-16
IL246755A0 (en) 2016-08-31
ES2908042T3 (es) 2022-04-27
WO2015108861A1 (en) 2015-07-23
MY182908A (en) 2021-02-05
DOP2016000173A (es) 2016-12-15
US9802960B2 (en) 2017-10-31
UY35951A (es) 2015-07-31
CA2935867A1 (en) 2015-07-23
JP6609258B2 (ja) 2019-11-20
CR20160363A (es) 2016-10-12
EP3094325A4 (en) 2017-08-09
KR20160122736A (ko) 2016-10-24
EP3094325B1 (en) 2021-10-13
GEP20196983B (en) 2019-06-25
CA2935867C (en) 2023-04-04
US20150225422A1 (en) 2015-08-13
EP3094325A1 (en) 2016-11-23
US10538533B2 (en) 2020-01-21
AU2015206652A1 (en) 2016-08-04
GEAP201914237A (en) 2019-02-25
AP2016009368A0 (en) 2016-08-31
BR112016016289B1 (pt) 2023-02-07
CL2016001805A1 (es) 2017-07-07
BR112016016289A2 (en) 2018-05-08
TN2016000270A1 (en) 2017-10-06
SG11201604820XA (en) 2016-07-28
US20180118762A1 (en) 2018-05-03
CN105916503B (zh) 2020-04-14
PE20161313A1 (es) 2016-12-17
TW201613865A (en) 2016-04-16
TWI662024B (zh) 2019-06-11
JP2017503813A (ja) 2017-02-02
PH12016501388A1 (en) 2016-08-15
ECSP16067303A (es) 2017-02-24
CN105916503A (zh) 2016-08-31
EA201691421A1 (ru) 2017-05-31
MX2016009135A (es) 2016-10-05

Similar Documents

Publication Publication Date Title
CA2935867C (en) Heteroaryls and uses thereof
JP7508584B2 (ja) ＰＩ３Ｋα阻害剤およびそれらの使用
AU2014348191B2 (en) Tetrahydroquinoline compositions as BET bromodomain inhibitors
AU2009281822B2 (en) cMET inhibitors
EP2454257B1 (en) Pyrrolopyridine inhibitors of kinases
JP6898914B2 (ja) コロニー刺激因子−１受容体（ｃｓｆ−１ｒ）阻害剤
ES2413808T3 (es) Derivados de piridina y pirimidina como inhibidores de fosfodiesterasa 10
IL282103B2 (en) Purinones as ubiquitin-specific protease 1 inhibitors
TW202110834A (zh) 作為ＤＮＡ聚合酶θ抑制劑之噻二唑基衍生物
AU2019201532A1 (en) Imidazopyridazines useful as inhibitors of the PAR-2 signaling pathway
CA2824871A1 (en) Bicyclic inhibitors of alk
JP2016516710A (ja) ピリジン系ｃｄｋ９キナーゼ阻害薬
AU2011329233A1 (en) NAMPT and ROCK inhibitors
WO2015161142A1 (en) Quinoxaline compounds and uses thereof
TW201124416A (en) Heterocyclic compounds useful as PDK1 inhibitors
SG181917A1 (en) Isoindolinone inhibitors of phosphatidylinositol 3-kinase
EA019700B1 (ru) Ингибиторы pi3 киназы или mtor
AU2004322641A1 (en) Gyrase inhibitors and uses thereof
US20160176871A1 (en) Tgf beta r antagonists
MX2014013734A (es) Inhibidores de nampt.
CA3185649A1 (en) Indole compounds as androgen receptor modulators
WO2016180537A1 (en) Substituted quinoxaline derivatives
US8673922B2 (en) Azaindazole compounds
EP4587434A1 (en) N-((isoquinolin-6-yl)methyl)-1h-pyrazole-4-carboxamid derivatives as plasma kallikrein inhibitors for the treatment of hereditary angioedema

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM

PC4A Registration of transfer of a eurasian patent by assignment