WO2020042622A1 - 化合物、组合物及其在药物制备中的用途 - Google Patents
化合物、组合物及其在药物制备中的用途 Download PDFInfo
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- WO2020042622A1 WO2020042622A1 PCT/CN2019/082441 CN2019082441W WO2020042622A1 WO 2020042622 A1 WO2020042622 A1 WO 2020042622A1 CN 2019082441 W CN2019082441 W CN 2019082441W WO 2020042622 A1 WO2020042622 A1 WO 2020042622A1
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- compound
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- pharmaceutically acceptable
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- VZTVJUDKBKYHBN-UHFFFAOYSA-N CC(C)(C(N(C1=S)c(cc2)cc(C(F)(F)F)c2C#N)=O)N1c(cc1)cc(F)c1C(NO)=O Chemical compound CC(C)(C(N(C1=S)c(cc2)cc(C(F)(F)F)c2C#N)=O)N1c(cc1)cc(F)c1C(NO)=O VZTVJUDKBKYHBN-UHFFFAOYSA-N 0.000 description 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- 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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D233/86—Oxygen and sulfur atoms, e.g. thiohydantoin
-
- 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Description
Claims (13)
- 权利要求1所述的化合物,其中,R1为氢或氟。
- 权利要求1所述的化合物,其中,R2和R3独立地为C1-C3的烷基,或者合起来形成一个C3-C6环烷基。
- 权利要求1所述的化合物,其中,R4为氰基。
- 权利要求1所述的化合物,其中,R5为三卤甲烷基,优选为三氟甲基。
- 药物组合物,包含治疗有效量的权利要求1的化合物或其可药用盐,以及可药用载体。
- 药物组合物,包含治疗有效量的权利要求1的化合物或其可药用盐,以及可药用稀释剂。
- 药物组合物,包含治疗有效量的权利要求1的化合物或其可药用盐,以及可药用助剂。
- 权利要求6-8任一项的药物组合物,其中该药物组合物为通过静脉注射给药、通过注射到组织给药、腹膜内给药、口服给药、或鼻内给药的形式。
- 权利要求1的化合物或其可药用盐在制造用于治疗前列腺癌的药物组合物中的用途
- 权利要求12的用途,其中该前列腺癌是激素敏感的前列腺癌或激素难治的前列腺癌。
Priority Applications (6)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP19853453.9A EP3825308B1 (en) | 2018-08-27 | 2019-04-12 | Thiohydantoin compound, composition, and use thereof as androgen receptor antagonists |
AU2019330575A AU2019330575B2 (en) | 2018-08-27 | 2019-04-12 | Compound, composition, and use thereof in preparation of drug |
CA3104188A CA3104188A1 (en) | 2018-08-27 | 2019-04-12 | Compound, composition and use thereof in pharmaceutical preparation |
JP2020573431A JP7148650B2 (ja) | 2018-08-27 | 2019-04-12 | 化合物、組成物及びその薬物製造における用途 |
KR1020207037607A KR20210014146A (ko) | 2018-08-27 | 2019-04-12 | 화합물, 조성물 및 의약물 제조에서의 사용 |
US17/136,176 US20210115014A1 (en) | 2018-08-27 | 2020-12-29 | Compound, composition, and use thereof in preparation of drug |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN201810982835.X | 2018-08-27 | ||
CN201810982835.XA CN108976171B (zh) | 2018-08-27 | 2018-08-27 | 化合物、组合物及其在药物制备中的用途 |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
US17/136,176 Continuation-In-Part US20210115014A1 (en) | 2018-08-27 | 2020-12-29 | Compound, composition, and use thereof in preparation of drug |
Publications (1)
Publication Number | Publication Date |
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WO2020042622A1 true WO2020042622A1 (zh) | 2020-03-05 |
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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PCT/CN2019/082441 WO2020042622A1 (zh) | 2018-08-27 | 2019-04-12 | 化合物、组合物及其在药物制备中的用途 |
Country Status (8)
Country | Link |
---|---|
US (1) | US20210115014A1 (zh) |
EP (1) | EP3825308B1 (zh) |
JP (1) | JP7148650B2 (zh) |
KR (1) | KR20210014146A (zh) |
CN (1) | CN108976171B (zh) |
AU (1) | AU2019330575B2 (zh) |
CA (1) | CA3104188A1 (zh) |
WO (1) | WO2020042622A1 (zh) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN116082246A (zh) * | 2022-12-31 | 2023-05-09 | 长沙泽达医药科技有限公司 | 一种乙撑硫脲衍生物的合成方法 |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN108976171B (zh) * | 2018-08-27 | 2020-06-16 | 长沙泽达医药科技有限公司 | 化合物、组合物及其在药物制备中的用途 |
CN109503416A (zh) * | 2018-12-24 | 2019-03-22 | 常州智超化学有限公司 | 一种恩杂鲁胺中间体合成方法 |
CN111848607B (zh) * | 2020-07-22 | 2023-03-17 | 长沙创新药物工业技术研究院有限公司 | 一种新型bcl-2/bcl-xl抑制剂、药物组合物及用途 |
CN114621109B (zh) * | 2020-12-14 | 2024-04-26 | 成都苑东生物制药股份有限公司 | 一种阿帕他胺的合成方法及其中间体 |
CN113698310B (zh) * | 2021-08-20 | 2023-03-17 | 江西金丰药业有限公司 | 一种恩杂鲁胺双酯中间体的制备方法 |
CN115850186B (zh) * | 2023-02-07 | 2024-04-09 | 长沙泽达医药科技有限公司 | 一种乙撑硫脲衍生物的晶型及用途 |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101048381A (zh) * | 2004-09-09 | 2007-10-03 | 中外制药株式会社 | 新型四氢咪唑衍生物及其用途 |
CN101222922A (zh) * | 2005-05-13 | 2008-07-16 | 加利福尼亚大学董事会 | 二芳基乙内酰脲化合物 |
CN101454002A (zh) * | 2006-03-27 | 2009-06-10 | 加利福尼亚大学董事会 | 用于治疗前列腺癌和与雄激素受体相关的疾病的雄激素受体调节剂 |
CN108976171A (zh) * | 2018-08-27 | 2018-12-11 | 长沙泽达医药科技有限公司 | 化合物、组合物及其在药物制备中的用途 |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
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BR112015004637B1 (pt) * | 2012-09-04 | 2022-04-05 | Shanghai Hengrui Pharmaceutical Co., Ltd. | Derivados de imidazolina, seus usos e seus processos de preparação, e composição farmacêutica |
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2018
- 2018-08-27 CN CN201810982835.XA patent/CN108976171B/zh active Active
-
2019
- 2019-04-12 CA CA3104188A patent/CA3104188A1/en active Pending
- 2019-04-12 JP JP2020573431A patent/JP7148650B2/ja active Active
- 2019-04-12 KR KR1020207037607A patent/KR20210014146A/ko not_active Application Discontinuation
- 2019-04-12 WO PCT/CN2019/082441 patent/WO2020042622A1/zh unknown
- 2019-04-12 EP EP19853453.9A patent/EP3825308B1/en active Active
- 2019-04-12 AU AU2019330575A patent/AU2019330575B2/en active Active
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2020
- 2020-12-29 US US17/136,176 patent/US20210115014A1/en active Pending
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101048381A (zh) * | 2004-09-09 | 2007-10-03 | 中外制药株式会社 | 新型四氢咪唑衍生物及其用途 |
CN101222922A (zh) * | 2005-05-13 | 2008-07-16 | 加利福尼亚大学董事会 | 二芳基乙内酰脲化合物 |
CN101454002A (zh) * | 2006-03-27 | 2009-06-10 | 加利福尼亚大学董事会 | 用于治疗前列腺癌和与雄激素受体相关的疾病的雄激素受体调节剂 |
CN108976171A (zh) * | 2018-08-27 | 2018-12-11 | 长沙泽达医药科技有限公司 | 化合物、组合物及其在药物制备中的用途 |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN116082246A (zh) * | 2022-12-31 | 2023-05-09 | 长沙泽达医药科技有限公司 | 一种乙撑硫脲衍生物的合成方法 |
CN116082246B (zh) * | 2022-12-31 | 2023-11-21 | 长沙泽达医药科技有限公司 | 一种乙撑硫脲衍生物的合成方法 |
Also Published As
Publication number | Publication date |
---|---|
JP2021529204A (ja) | 2021-10-28 |
EP3825308A4 (en) | 2022-05-11 |
AU2019330575B2 (en) | 2022-03-03 |
EP3825308B1 (en) | 2023-10-11 |
KR20210014146A (ko) | 2021-02-08 |
EP3825308A1 (en) | 2021-05-26 |
US20210115014A1 (en) | 2021-04-22 |
CA3104188A1 (en) | 2020-03-05 |
CN108976171A (zh) | 2018-12-11 |
JP7148650B2 (ja) | 2022-10-05 |
EP3825308C0 (en) | 2023-10-11 |
CN108976171B (zh) | 2020-06-16 |
AU2019330575A1 (en) | 2021-02-04 |
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