TWI620748B - 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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- TWI620748B TWI620748B TW106103165A TW106103165A TWI620748B TW I620748 B TWI620748 B TW I620748B TW 106103165 A TW106103165 A TW 106103165A TW 106103165 A TW106103165 A TW 106103165A TW I620748 B TWI620748 B TW I620748B
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- 150000003384 small molecules Chemical class 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 238000005507 spraying Methods 0.000 description 1
- 230000000087 stabilizing effect Effects 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 238000010189 synthetic method Methods 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 125000004213 tert-butoxy group Chemical group [H]C([H])([H])C(O*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 239000012085 test solution Substances 0.000 description 1
- 125000006169 tetracyclic group Chemical group 0.000 description 1
- QEMXHQIAXOOASZ-UHFFFAOYSA-N tetramethylammonium Chemical compound C[N+](C)(C)C QEMXHQIAXOOASZ-UHFFFAOYSA-N 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 125000004055 thiomethyl group Chemical group [H]SC([H])([H])* 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- 238000000844 transformation Methods 0.000 description 1
- ODLHGICHYURWBS-LKONHMLTSA-N trappsol cyclo Chemical compound CC(O)COC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)COCC(O)C)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1COCC(C)O ODLHGICHYURWBS-LKONHMLTSA-N 0.000 description 1
- 125000006168 tricyclic group Chemical group 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
- 239000003643 water by type Substances 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
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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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Thiazole And Isothizaole Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662291667P | 2016-02-05 | 2016-02-05 | |
| US62/291,667 | 2016-02-05 |
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| TW201728583A TW201728583A (zh) | 2017-08-16 |
| TWI620748B true TWI620748B (zh) | 2018-04-11 |
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| WO (1) | WO2017136315A1 (enExample) |
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| HUE044025T2 (hu) | 2010-05-20 | 2019-09-30 | Array Biopharma Inc | Makrociklusos vegyületek mint TRK-kináz inhibitorok |
| ES2857081T3 (es) | 2015-07-16 | 2021-09-28 | Array Biopharma Inc | Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa 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 |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| ES2948194T3 (es) | 2017-01-18 | 2023-09-01 | Array Biopharma Inc | Compuestos de pirazolo[1,5-a]pirazina sustituida como inhibidores de la cinasa RET |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| 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 |
| TWI812649B (zh) | 2017-10-10 | 2023-08-21 | 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 |
| CA3087578C (en) | 2018-01-18 | 2023-08-08 | Array Biopharma Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| TW201932464A (zh) | 2018-01-18 | 2019-08-16 | 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基[4,3-c]吡啶化合物 |
| US11603374B2 (en) | 2018-01-18 | 2023-03-14 | Array Biopharma Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| KR102797697B1 (ko) | 2018-05-25 | 2025-04-22 | 에이2에이 파마수티칼스, 잉크. | 신종 항암제 후보로서, 매우 강력한 tacc3 억제제 |
| EP3849986B1 (en) | 2018-09-10 | 2022-06-08 | Array Biopharma, Inc. | Fused heterocyclic compounds as ret kinase inhibitors |
| EP4323351A4 (en) * | 2021-04-12 | 2025-07-30 | A2A Pharmaceuticals Inc | COMPOSITIONS AND METHODS FOR THE TREATMENT OF CANCER |
| AU2023241042A1 (en) | 2022-03-24 | 2024-10-10 | A2A Pharmaceuticals, Inc. | Compositions and methods for treating cancer |
Citations (1)
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| 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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| CN101481359A (zh) * | 1999-04-15 | 2009-07-15 | 布里斯托尔-迈尔斯斯奎布公司 | 环状蛋白酪氨酸激酶抑制剂 |
| AU2002231139B2 (en) * | 2000-12-21 | 2007-03-22 | Bristol-Myers Squibb Company | Thiazolyl inhibitors of tec family tyrosine kinases |
| EP1558609A4 (en) * | 2002-10-30 | 2008-05-28 | Merck & Co Inc | KINASE INHIBITORS |
| CN101106990B (zh) * | 2005-01-26 | 2010-12-08 | Irm责任有限公司 | 用作蛋白激酶抑制剂的化合物和组合物 |
| HRP20150932T2 (hr) | 2008-04-21 | 2017-10-20 | Taigen Biotechnology Co., Ltd. | Heterociklički spojevi |
| WO2010046780A2 (en) | 2008-10-22 | 2010-04-29 | Institut Pasteur Korea | Anti viral compounds |
| MX346042B (es) | 2010-08-10 | 2017-03-03 | Astellas Pharma Inc | Compuesto heterociclico. |
| CU24269B1 (es) | 2011-09-27 | 2017-08-08 | Novartis Ag | 3- pirimidin- 4-il- oxazolidin- 2- onas inhibidores de la idh mutante |
| 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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2017
- 2017-01-26 TW TW106103165A patent/TWI620748B/zh active
- 2017-01-30 US US15/419,183 patent/US10047078B2/en active Active
- 2017-01-31 JP JP2018560435A patent/JP6883049B2/ja active Active
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- 2017-01-31 WO PCT/US2017/015765 patent/WO2017136315A1/en not_active Ceased
- 2017-01-31 KR KR1020187024997A patent/KR102449712B1/ko active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20120225880A1 (en) * | 2011-03-04 | 2012-09-06 | National Health Research Institutes | Pyrazole compounds and thiazole compounds as protein kinases inhibitors |
Non-Patent Citations (3)
| Title |
|---|
| CT Chen,et al."Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations",European Journal of Medicinal Chemistry, 100 (2015) 151~161,Available online 9 May 2015. |
| CT Chen,et al."Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations",European Journal of Medicinal Chemistry, 100 (2015) 151~161,Available online 9 May 2015. George A. Patani and Edmond J. LaVoie,"Bioisosterism: A Rational Approach in Drug Design",Chem. Rev. 1996, 96, 3147-3176.、 * |
| George A. Patani and Edmond J. LaVoie,"Bioisosterism: A Rational Approach in Drug Design",Chem. Rev. 1996, 96, 3147-3176.、 |
Also Published As
| Publication number | Publication date |
|---|---|
| TW201728583A (zh) | 2017-08-16 |
| KR102449712B1 (ko) | 2022-09-30 |
| US10047078B2 (en) | 2018-08-14 |
| HK1258689A1 (zh) | 2019-11-15 |
| EP3411035B1 (en) | 2022-03-02 |
| US20170226100A1 (en) | 2017-08-10 |
| CN109069504A (zh) | 2018-12-21 |
| JP2019511564A (ja) | 2019-04-25 |
| KR20180132618A (ko) | 2018-12-12 |
| WO2017136315A1 (en) | 2017-08-10 |
| CN109069504B (zh) | 2022-06-28 |
| EP3411035A4 (en) | 2019-08-14 |
| EP3411035A1 (en) | 2018-12-12 |
| ES2909612T3 (es) | 2022-05-09 |
| JP6883049B2 (ja) | 2021-06-02 |
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