CN104039798B - 具有蛋白激酶抑制活性的噻吩并[3，2-d]嘧啶衍生物 - Google Patents
具有蛋白激酶抑制活性的噻吩并[3，2-d]嘧啶衍生物 Download PDFInfo
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- CN104039798B CN104039798B CN201280064739.8A CN201280064739A CN104039798B CN 104039798 B CN104039798 B CN 104039798B CN 201280064739 A CN201280064739 A CN 201280064739A CN 104039798 B CN104039798 B CN 104039798B
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- pyrimidine
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- methylisoquinolin
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
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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
- A61K31/495—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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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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
- A61K31/535—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
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Biomedical Technology (AREA)
- Pulmonology (AREA)
- Oncology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Rheumatology (AREA)
- Vascular Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Ophthalmology & Optometry (AREA)
- Communicable Diseases (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Psychiatry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR10-2011-0146818 | 2011-12-30 | ||
| KR20110146818 | 2011-12-30 | ||
| PCT/KR2012/011571 WO2013100632A1 (en) | 2011-12-30 | 2012-12-27 | THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASES |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104039798A CN104039798A (zh) | 2014-09-10 |
| CN104039798B true CN104039798B (zh) | 2016-08-24 |
Family
ID=48697978
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280064739.8A Active CN104039798B (zh) | 2011-12-30 | 2012-12-27 | 具有蛋白激酶抑制活性的噻吩并[3，2-d]嘧啶衍生物 |
Country Status (32)
Families Citing this family (48)
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| KR102015402B1 (ko) | 2010-05-20 | 2019-08-28 | 어레이 바이오파마 인크. | Trk 키나제 저해제로서의 매크로시클릭 화합물 |
| TWI713455B (zh) | 2014-06-25 | 2020-12-21 | 美商伊凡克特治療公司 | ＭｎＫ抑制劑及其相關方法 |
| KR20220051422A (ko) | 2014-10-14 | 2022-04-26 | 신젠타 파티서페이션즈 아게 | 1-(3,5-디클로로페닐)-2,2,2-트리플루오로에타논 및 그의 유도체의 제조 방법 |
| HUE053067T2 (hu) | 2015-07-16 | 2021-06-28 | Array Biopharma Inc | Helyettesített pirazolo[1,5-A]piridin vegyületek, mint RET kináz inhibitorok |
| WO2017075394A1 (en) | 2015-10-29 | 2017-05-04 | Effector Therapeutics, Inc. | Isoindoline, azaisoindoline, dihydroindenone and dihydroazaindenone inhibitors of mnk1 and mnk2 |
| CA3002558A1 (en) | 2015-10-29 | 2017-05-04 | Effector Therapeutics, Inc. | Pyrrolo-, pyrazolo-, imidazo-pyrimidine and pyridine compounds that inhibit mnk1 and mnk2 |
| WO2017087808A1 (en) | 2015-11-20 | 2017-05-26 | Effector Therapeutics, Inc. | Heterocyclic compounds that inhibit the kinase activity of mnk useful for treating various cancers |
| WO2017114275A1 (zh) * | 2015-12-31 | 2017-07-06 | 成都先导药物开发有限公司 | 一种抑制rock的化合物及其制备方法与应用 |
| EP3414247B1 (en) | 2016-02-08 | 2021-04-21 | F. Hoffmann-La Roche AG | Spiroindolinones as ddr1 inhibitors |
| EP3443114A1 (en) | 2016-04-15 | 2019-02-20 | H. Hoffnabb-La Roche Ag | Diagnostic and therapeutic methods for cancer |
| CN106153920B (zh) * | 2016-07-25 | 2018-04-27 | 四川大学华西医院 | 一种肺癌筛查试剂盒 |
| TWI752098B (zh) | 2016-10-10 | 2022-01-11 | 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 |
| 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 |
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| 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 |
| 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 |
| KR102777989B1 (ko) * | 2017-11-30 | 2025-03-12 | 한미약품 주식회사 | 4-아미노-N-(1-((3-클로로-2-플루오로페닐)아미노)-6-메틸이소퀴놀린-5-일)티에노[3,2-d]피리미딘-7-카르복사미드의 염, 및 그의 결정질 형태 |
| US11492357B2 (en) * | 2017-11-30 | 2022-11-08 | Hanmi Pharm. Co., Ltd. | Thieno[3,2-d]pyrimidine derivative compound having inhibitory activity for protein kinase |
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| EP3740490A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| WO2019158579A1 (en) | 2018-02-13 | 2019-08-22 | Vib Vzw | Targeting minimal residual disease in cancer with rxr antagonists |
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| CN116472041B (zh) * | 2020-11-24 | 2024-12-06 | 正大天晴药业集团股份有限公司 | 氘修饰的噻吩并吡啶酮化合物 |
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| CN114213430B (zh) * | 2021-12-28 | 2022-12-02 | 深圳湾实验室 | 4-氨基噻吩[3,2-d]嘧啶-7-羧酸的制备方法、蛋白激酶抑制剂中间体 |
| CN114524826A (zh) * | 2022-02-18 | 2022-05-24 | 郑州猫眼农业科技有限公司 | 7-溴-4-氯噻吩并[3,2-d]嘧啶的制备工艺 |
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