RS59059B1 - Diaril makrociklična jedinjenja kao modulatori protein kinaza - Google Patents
Diaril makrociklična jedinjenja kao modulatori protein kinazaInfo
- Publication number
- RS59059B1 RS59059B1 RS20190900A RSP20190900A RS59059B1 RS 59059 B1 RS59059 B1 RS 59059B1 RS 20190900 A RS20190900 A RS 20190900A RS P20190900 A RSP20190900 A RS P20190900A RS 59059 B1 RS59059 B1 RS 59059B1
- Authority
- RS
- Serbia
- Prior art keywords
- fluoro
- 4alkyl
- ethenopyrazolo
- methyl
- tetrahydro
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- 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
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
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- 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
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- 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
- 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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- 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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Communicable Diseases (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Vascular Medicine (AREA)
- Transplantation (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pulmonology (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461931506P | 2014-01-24 | 2014-01-24 | |
| US201462049326P | 2014-09-11 | 2014-09-11 | |
| US201562106301P | 2015-01-22 | 2015-01-22 | |
| PCT/US2015/012597 WO2015112806A2 (en) | 2014-01-24 | 2015-01-23 | Diaryl macrocycles as modulators of protein kinases |
| EP15740510.1A EP3097107B1 (en) | 2014-01-24 | 2015-01-23 | Diaryl macrocycles as modulators of protein kinases |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RS59059B1 true RS59059B1 (sr) | 2019-08-30 |
Family
ID=53682127
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RS20190900A RS59059B1 (sr) | 2014-01-24 | 2015-01-23 | Diaril makrociklična jedinjenja kao modulatori protein kinaza |
| RS20240447A RS65417B1 (sr) | 2014-01-24 | 2015-01-23 | Diaril makrocikli kao modulatori protein kinaza |
| RS20221161A RS63829B1 (sr) | 2014-01-24 | 2015-01-23 | Diaril makrociklična jedinjenja kao modulatori protein kinaza |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RS20240447A RS65417B1 (sr) | 2014-01-24 | 2015-01-23 | Diaril makrocikli kao modulatori protein kinaza |
| RS20221161A RS63829B1 (sr) | 2014-01-24 | 2015-01-23 | Diaril makrociklična jedinjenja kao modulatori protein kinaza |
Country Status (35)
Families Citing this family (94)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2350075T3 (da) | 2008-09-22 | 2014-05-26 | Array Biopharma Inc | Substituerede imidazo[1,2b]pyridazinforbindelser som trk-kinase-inhibitorer |
| EP2350071B1 (en) | 2008-10-22 | 2014-01-08 | Array Biopharma, Inc. | SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| DK2918588T3 (en) | 2010-05-20 | 2017-08-28 | Array Biopharma Inc | Macrocyclic compounds as TRK kinase inhibitors |
| DK3636649T3 (da) * | 2014-01-24 | 2024-05-21 | Turning Point Therapeutics Inc | Diarylmakrocykler som modulatorer af proteinkinaser |
| TWI767858B (zh) | 2014-11-16 | 2022-06-11 | 美商亞雷生物製藥股份有限公司 | (S)-N-(5-((R)-2-(2,5-二氟苯基)-吡咯啶-1-基)-吡唑并[1,5-a]嘧啶-3-基)-3-羥基吡咯啶-1-甲醯胺硫酸氫鹽結晶型 |
| US10758525B2 (en) | 2015-01-22 | 2020-09-01 | MyoKardia, Inc. | 4-methylsulfonyl-substituted piperidine urea compounds |
| AU2016270803A1 (en) | 2015-06-01 | 2018-01-04 | Loxo Oncology, Inc. | Methods of diagnosing and treating cancer |
| CA2989327A1 (en) | 2015-07-02 | 2017-01-05 | Tp Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
| HRP20240780T1 (hr) | 2015-07-06 | 2024-09-13 | Turning Point Therapeutics, Inc. | Polimorf diaril makrocikla |
| PT3322706T (pt) | 2015-07-16 | 2021-03-08 | Array Biopharma Inc | Compostos de pirazolo[1,5-a]piridina substituídos como inibidores da quinase do ret |
| EP3733187B1 (en) * | 2015-07-21 | 2024-10-16 | Turning Point Therapeutics, Inc. | Chiral diaryl macrocycle and use thereof in the treatment of cancer |
| SG11201803438XA (en) | 2015-10-26 | 2018-05-30 | Univ Colorado Regents | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| US11278521B2 (en) | 2015-12-15 | 2022-03-22 | University Of South Florida | GAS5 binding compounds, formulations, and uses thereof |
| PE20181888A1 (es) | 2016-04-04 | 2018-12-11 | Loxo Oncology Inc | Formulaciones liquidas de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida |
| JP7057343B2 (ja) | 2016-04-04 | 2022-04-19 | ロクソ オンコロジー， インコーポレイテッド | 小児癌の処置方法 |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| HUE053643T2 (hu) | 2016-05-18 | 2021-07-28 | Loxo Oncology Inc | (S)-N-(5 -((R)-2-(2,5-difluor-fenil)-pirrolidin-1-il)-pirazolo[1,5-A] pirimidin-3-il)-3-hidroxi-pirrolidin-1-karboxamid elõkészítése |
| BR112019001607A2 (pt) * | 2016-07-28 | 2019-04-30 | Tp Therapeutics, Inc. | inibidores macrocíclicos de quinases |
| 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 |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| WO2018136661A1 (en) | 2017-01-18 | 2018-07-26 | Andrews Steven W | SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| TWI808958B (zh) * | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| CN107586796B (zh) * | 2017-07-20 | 2021-08-06 | 暨明医药科技（苏州）有限公司 | (r)-2-(1-氨基乙基)-4-氟苯酚的合成方法 |
| PT3658148T (pt) | 2017-07-28 | 2024-08-26 | Turning Point Therapeutics Inc | Compostos macrocíclicos e utilizações dos mesmos |
| 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 |
| CA3080157A1 (en) | 2017-10-26 | 2019-05-02 | Array Biopharma Inc. | Formulations of a macrocyclic trk kinase inhibitor |
| CN109516999B (zh) * | 2017-11-01 | 2021-08-17 | 郑州泰基鸿诺医药股份有限公司 | 用作蛋白质激酶调节剂的化合物及其应用 |
| CA3081790C (en) | 2017-11-10 | 2023-03-07 | Angex Pharmaceutical, Inc. | Macrocyclic compounds as trk kinase inhibitors and uses thereof |
| EP3728270A4 (en) | 2017-12-19 | 2021-06-23 | Turning Point Therapeutics, Inc. | MACROCYCLIC KINASE INHIBITORS AND THEIR USES |
| KR102814342B1 (ko) | 2017-12-19 | 2025-05-29 | 터닝 포인트 테라퓨틱스, 인크. | 질병 치료용 대환식 화합물 |
| US11453672B2 (en) | 2017-12-22 | 2022-09-27 | Shenzhen Targetrx, Inc. | Substituted pyrazolo[1,5-a]pyrimidines as tropomyosin receptor kinase inhibitors |
| CN111630054B (zh) | 2018-01-18 | 2023-05-09 | 奥瑞生物药品公司 | 作为RET激酶抑制剂的取代的吡唑并[3,4-d]嘧啶化合物 |
| WO2019143994A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| TWI802635B (zh) | 2018-01-18 | 2023-05-21 | 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咯并[2,3-d]嘧啶化合物 |
| CN109575025B (zh) * | 2018-01-23 | 2020-09-11 | 深圳市塔吉瑞生物医药有限公司 | 取代的吡唑并[1,5-a]嘧啶类的大环化合物 |
| CN111511749B (zh) * | 2018-01-30 | 2022-02-08 | 上海吉倍生物技术有限公司 | 具有大环分子结构的化合物及其用途 |
| CN110156813B (zh) * | 2018-02-13 | 2023-07-25 | 北京诺诚健华医药科技有限公司 | 作为trk抑制剂的杂环化合物 |
| US11555042B2 (en) * | 2018-03-28 | 2023-01-17 | Fochon Biosciences, Ltd. | Macrocyclic compounds as TRK kinases inhibitors |
| US20210023086A1 (en) | 2018-03-29 | 2021-01-28 | Loxo Oncology, Inc. | Treatment of trk-associated cancers |
| CN110386944B (zh) * | 2018-04-16 | 2021-10-29 | 深圳市塔吉瑞生物医药有限公司 | 用于抑制蛋白激酶活性的二(杂)芳基大环化合物 |
| WO2019206069A1 (zh) * | 2018-04-25 | 2019-10-31 | 北京普祺医药科技有限公司 | 一种二芳基巨环化合物、药物组合物以及其用途 |
| CN111918868B (zh) * | 2018-05-04 | 2022-12-30 | 正大天晴药业集团股份有限公司 | 作为蛋白激酶调节剂的二芳基大环化合物 |
| CN110627812B (zh) | 2018-06-25 | 2022-10-11 | 北京诺诚健华医药科技有限公司 | 作为trk抑制剂的杂环化合物 |
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| US12180207B2 (en) | 2018-12-19 | 2024-12-31 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of FGFR tyrosine kinases |
| CN111592541B (zh) * | 2019-02-21 | 2021-09-10 | 山东轩竹医药科技有限公司 | 大环类激酶抑制剂及其用途 |
| WO2020185755A1 (en) * | 2019-03-11 | 2020-09-17 | Fronthera U.S. Pharmaceuticals Llc | Tyk2 inhibitors and uses thereof |
| MX2021011723A (es) * | 2019-03-26 | 2021-10-22 | Ventyx Biosciences Inc | Ligandos de pseudocinasa tyk2. |
| CN113727984B (zh) * | 2019-05-21 | 2024-03-15 | 浙江海正药业股份有限公司 | 大环类衍生物、及其制备方法和用途 |
| WO2020257165A1 (en) * | 2019-06-19 | 2020-12-24 | Turning Point Therapeutics, Inc. | Macrocycles for use in treating disease |
| WO2020257189A1 (en) * | 2019-06-19 | 2020-12-24 | Turning Point Therapeutics, Inc. | Macrocycles for treating disease |
| PE20220135A1 (es) * | 2019-06-19 | 2022-01-27 | Turning Point Therapeutics Inc | Polimorfos de un inhibidor de cinasas macrociclicas |
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