CN109069504A - 氨基噻唑化合物及其用途 - Google Patents
氨基噻唑化合物及其用途 Download PDFInfo
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- CN109069504A CN109069504A CN201780010118.4A CN201780010118A CN109069504A CN 109069504 A CN109069504 A CN 109069504A CN 201780010118 A CN201780010118 A CN 201780010118A CN 109069504 A CN109069504 A CN 109069504A
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Classifications
-
- 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
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Description
GI<sub>50</sub>(nM) | AC220 | 1 | 2 | 4 |
ITD-D835Y | 19 | 1.1 | 1.8 | 1.0 |
ITD-D835V | 103 | 0.76 | 1.5 | 0.87 |
ITD-D835F | 57 | 3.2 | 5.8 | 5.5 |
ITD-F691L | 101 | 8.5 | 14 | 12 |
ITD-F691I | >300 | 45 | 158 | 19 |
Mia-paca2肿瘤模型 | 第18天的TGI |
5 | 65% |
6 | 68% |
MOLM-13异种移植的裸鼠 | 第25天肿瘤大小 |
2 | 53mm<sup>3</sup>(50mpk),270mm<sup>3</sup>(25mpk) |
4 | 193mm<sup>3</sup>(150mpk) |
MOLM-13异种移植的裸鼠 | 第12天的肿瘤退化 |
2 | 34% |
5 | 22% |
Claims (32)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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US201662291667P | 2016-02-05 | 2016-02-05 | |
US62/291,667 | 2016-02-05 | ||
PCT/US2017/015765 WO2017136315A1 (en) | 2016-02-05 | 2017-01-31 | Aminothiazole compounds and use thereof |
Publications (2)
Publication Number | Publication Date |
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CN109069504A true CN109069504A (zh) | 2018-12-21 |
CN109069504B CN109069504B (zh) | 2022-06-28 |
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CN201780010118.4A Active CN109069504B (zh) | 2016-02-05 | 2017-01-31 | 氨基噻唑化合物及其用途 |
Country Status (9)
Country | Link |
---|---|
US (1) | US10047078B2 (zh) |
EP (1) | EP3411035B1 (zh) |
JP (1) | JP6883049B2 (zh) |
KR (1) | KR102449712B1 (zh) |
CN (1) | CN109069504B (zh) |
ES (1) | ES2909612T3 (zh) |
HK (1) | HK1258689A1 (zh) |
TW (1) | TWI620748B (zh) |
WO (1) | WO2017136315A1 (zh) |
Families Citing this family (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP3205654B1 (en) | 2010-05-20 | 2019-01-02 | Array Biopharma, Inc. | Macrocyclic compounds as trk kinase inhibitors |
PL3322706T4 (pl) | 2015-07-16 | 2021-07-19 | Array Biopharma, Inc. | Podstawione związki pirazolo[1,5-a]pirydynowe jako inhibitory kinazy ret |
JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
CN110267960B (zh) | 2017-01-18 | 2022-04-26 | 阿雷生物药品公司 | 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡嗪化合物 |
JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
TW202410896A (zh) | 2017-10-10 | 2024-03-16 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
EP3740491A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
CA3087972C (en) | 2018-01-18 | 2023-01-10 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
TW201938169A (zh) | 2018-01-18 | 2019-10-01 | 美商亞雷生物製藥股份有限公司 | 作為RET激酶抑制劑之經取代吡唑并[3,4-d]嘧啶化合物 |
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CA2503715A1 (en) * | 2002-10-30 | 2004-05-21 | Merck & Co., Inc. | Kinase inhibitors |
JP2008528585A (ja) * | 2005-01-26 | 2008-07-31 | アイアールエム・リミテッド・ライアビリティ・カンパニー | タンパク質キナーゼ阻害剤としての化合物および組成物 |
EP2268635B1 (en) | 2008-04-21 | 2015-06-10 | Taigen Biotechnology Co., Ltd. | Heterocyclic compounds |
WO2010046780A2 (en) | 2008-10-22 | 2010-04-29 | Institut Pasteur Korea | Anti viral compounds |
CA2849995A1 (en) | 2011-09-27 | 2013-04-04 | Novartis Ag | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh |
WO2013143466A1 (zh) * | 2012-03-27 | 2013-10-03 | 广东东阳光药业有限公司 | 作为欧若拉激酶抑制剂的取代嘧啶衍生物 |
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US20130150364A1 (en) * | 2010-08-10 | 2013-06-13 | Astellas Pharma Inc. | Heterocyclic compound |
US20120225880A1 (en) * | 2011-03-04 | 2012-09-06 | National Health Research Institutes | Pyrazole compounds and thiazole compounds as protein kinases inhibitors |
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EP3411035A4 (en) | 2019-08-14 |
KR102449712B1 (ko) | 2022-09-30 |
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JP6883049B2 (ja) | 2021-06-02 |
TWI620748B (zh) | 2018-04-11 |
CN109069504B (zh) | 2022-06-28 |
US20170226100A1 (en) | 2017-08-10 |
TW201728583A (zh) | 2017-08-16 |
JP2019511564A (ja) | 2019-04-25 |
HK1258689A1 (zh) | 2019-11-15 |
ES2909612T3 (es) | 2022-05-09 |
EP3411035B1 (en) | 2022-03-02 |
US10047078B2 (en) | 2018-08-14 |
WO2017136315A1 (en) | 2017-08-10 |
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