EA201491967A1 - Производные имидазотиадиазола в качестве ингибиторов активируемых протеазой рецепторов 4 (par4) для лечения агрегации тромбоцитов - Google Patents
Производные имидазотиадиазола в качестве ингибиторов активируемых протеазой рецепторов 4 (par4) для лечения агрегации тромбоцитовInfo
- Publication number
- EA201491967A1 EA201491967A1 EA201491967A EA201491967A EA201491967A1 EA 201491967 A1 EA201491967 A1 EA 201491967A1 EA 201491967 A EA201491967 A EA 201491967A EA 201491967 A EA201491967 A EA 201491967A EA 201491967 A1 EA201491967 A1 EA 201491967A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- imidazotia
- par4
- diazole
- derivatives
- treatment
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- 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
- A61K31/433—Thidiazoles
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4355—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
- A61K31/535—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
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261638591P | 2012-04-26 | 2012-04-26 | |
| PCT/US2013/037892 WO2013163244A1 (en) | 2012-04-26 | 2013-04-24 | Imidazothiadiazole derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EA201491967A1 true EA201491967A1 (ru) | 2015-03-31 |
Family
ID=48225152
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201491967A EA201491967A1 (ru) | 2012-04-26 | 2013-04-24 | Производные имидазотиадиазола в качестве ингибиторов активируемых протеазой рецепторов 4 (par4) для лечения агрегации тромбоцитов |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US9862730B2 (enExample) |
| EP (1) | EP2847200B1 (enExample) |
| JP (1) | JP6181744B2 (enExample) |
| KR (1) | KR20150003767A (enExample) |
| CN (1) | CN104540835B (enExample) |
| AU (1) | AU2013251683A1 (enExample) |
| BR (1) | BR112014026493A2 (enExample) |
| CA (1) | CA2871637A1 (enExample) |
| EA (1) | EA201491967A1 (enExample) |
| ES (1) | ES2625029T3 (enExample) |
| IL (1) | IL235140A0 (enExample) |
| MX (1) | MX2014012454A (enExample) |
| SG (1) | SG11201406759YA (enExample) |
| WO (1) | WO2013163244A1 (enExample) |
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| EP2855489B1 (en) | 2012-04-26 | 2017-01-04 | Bristol-Myers Squibb Company | Imidazothiadiazole and imidazopyridazine derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation |
| JP6073464B2 (ja) | 2012-04-26 | 2017-02-01 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | 血小板凝集を治療するためのプロテアーゼ活性化受容体4(par4)阻害剤としてのイミダゾチアジアゾールおよびイミダゾピラジン誘導体 |
| US9598419B1 (en) | 2014-06-24 | 2017-03-21 | Universite De Montreal | Imidazotriazine and imidazodiazine compounds |
| US9617279B1 (en) | 2014-06-24 | 2017-04-11 | Bristol-Myers Squibb Company | Imidazooxadiazole compounds |
| HRP20211778T1 (hr) | 2014-08-29 | 2022-03-18 | Chdi Foundation, Inc. | Kontrastna sredstva za slikovnu dijagnostiku huntingtin proteina |
| WO2016125621A1 (ja) * | 2015-02-03 | 2016-08-11 | 住友化学株式会社 | ベンゾイミダゾール化合物及びその有害節足動物防除用途 |
| WO2016125622A1 (ja) * | 2015-02-03 | 2016-08-11 | 住友化学株式会社 | ベンゾオキサゾール化合物及びその有害節足動物防除用途 |
| ES2929208T3 (es) | 2015-02-26 | 2022-11-25 | Univ Montreal | Compuestos de imidazotiadiazol como inhibidores de PAR4 |
| EP3262052A1 (en) | 2015-02-26 | 2018-01-03 | Bristol-Myers Squibb Company | Benzothiazole and benzothiophne compounds |
| US9789087B2 (en) | 2015-08-03 | 2017-10-17 | Thomas Jefferson University | PAR4 inhibitor therapy for patients with PAR4 polymorphism |
| US10457627B2 (en) | 2015-09-23 | 2019-10-29 | Xw Laboratories Inc. | Prodrugs of gamma-hydroxybutyric acid, compositions and uses thereof |
| WO2017066863A1 (en) | 2015-10-19 | 2017-04-27 | Universite De Montreal | Heterocyclic compounds as inhibitors of platelet aggregation |
| US20190119300A1 (en) * | 2016-04-18 | 2019-04-25 | Vanderbilt University | Substituted and fused 6-membered protease activated receptor 4 (par-4) antagonists |
| JP7058256B2 (ja) | 2016-07-14 | 2022-04-21 | ブリストル-マイヤーズ スクイブ カンパニー | 二環式ヘテロアリール置換化合物 |
| CN109689649B (zh) | 2016-07-14 | 2022-07-19 | 百时美施贵宝公司 | 经二环杂芳基取代的化合物 |
| CN109689642B (zh) | 2016-07-14 | 2022-04-12 | 百时美施贵宝公司 | 经单环杂芳基取代的化合物 |
| ES2823127T3 (es) | 2016-07-14 | 2021-05-06 | Bristol Myers Squibb Co | Compuestos tricíclicos de quinolina y azaquinolina sustituidos con heteroarilo como inhibidores de PAR4 |
| AU2017406159B2 (en) | 2017-03-30 | 2020-05-21 | XWPharma Ltd. | Bicyclic heteroaryl derivatives and preparation and uses thereof |
| KR102755742B1 (ko) | 2017-09-11 | 2025-01-15 | 모나쉬 유니버시티 | 인간 트롬빈 수용체 par4 결합 단백질 |
| WO2019149205A1 (zh) * | 2018-01-31 | 2019-08-08 | 江苏恒瑞医药股份有限公司 | 苯并杂芳基类衍生物、其制备方法及其在医药上的应用 |
| CN110218218B (zh) * | 2018-03-01 | 2022-04-08 | 江苏恒瑞医药股份有限公司 | 苯并呋喃类衍生物、其制备方法及其在医药上的应用 |
| WO2019218955A1 (zh) * | 2018-05-16 | 2019-11-21 | 深圳信立泰药业股份有限公司 | 作为用于治疗血小板聚集的蛋白酶激活受体4(par4)抑制剂的化合物 |
| CN112074521B (zh) * | 2018-05-16 | 2022-08-09 | 深圳信立泰药业股份有限公司 | 作为用于治疗血小板聚集的蛋白酶激活受体4(par4)抑制剂的化合物 |
| WO2019218957A1 (zh) * | 2018-05-16 | 2019-11-21 | 深圳信立泰药业股份有限公司 | 作为用于治疗血小板聚集的蛋白酶激活受体4(par4)抑制剂的化合物 |
| CN110627817B (zh) * | 2018-06-25 | 2022-03-29 | 中国药科大学 | 咪唑并环类par4拮抗剂及其医药用途 |
| CN112004802B (zh) | 2018-09-30 | 2021-12-28 | 凯瑞康宁生物工程(武汉)有限公司 | 作为神经元组胺受体-3拮抗剂的化合物及其用途 |
| CN113874015B (zh) | 2018-12-21 | 2024-05-24 | 细胞基因公司 | Ripk2的噻吩并吡啶抑制剂 |
| CN111349105B (zh) * | 2018-12-24 | 2023-04-07 | 江苏恒瑞医药股份有限公司 | 苯并呋喃类衍生物、其制备方法及其在医药上的应用 |
| CN111362970A (zh) * | 2018-12-25 | 2020-07-03 | 天津药物研究院有限公司 | 苯并呋喃类衍生物及其制备方法和用途 |
| CN110407697A (zh) * | 2019-08-28 | 2019-11-05 | 上海毕得医药科技有限公司 | 一种4-甲酰基-3-羟基苯甲酸甲酯的合成方法 |
| JP7483890B2 (ja) | 2019-12-20 | 2024-05-15 | エックスダブリューファーマ リミテッド | 4-バリルオキシ酪酸の合成方法 |
| EP4167966A1 (en) | 2020-06-18 | 2023-04-26 | XWPharma Ltd. | Pharmaceutical granulations of water-soluble active pharmaceutical ingredients |
| CN115038432B (zh) | 2020-06-18 | 2023-12-26 | 凯瑞康宁生物工程(武汉)有限公司 | 水溶性活性药物成分的控制释放制粒 |
| WO2022020621A1 (en) | 2020-07-24 | 2022-01-27 | XWPharma Ltd. | Pharmaceutical compositions and pharmacokinetics of a gamma-hydroxybutyric acid derivative |
| KR20230058151A (ko) | 2020-10-05 | 2023-05-02 | 엑스더블유파마 리미티드 | 감마-하이드록시부티르산 유도체의 변형된 방출 조성물 |
| EP4588471A3 (en) | 2021-03-19 | 2025-09-24 | XWPharma Ltd. | Pharmacokinetics of combined release formulations of a gamma-hydroxybutyric acid derivative |
| CN113150005B (zh) * | 2021-04-09 | 2022-08-30 | 中国药科大学 | 喹喔啉类化合物、制备方法及其在医药上的应用 |
| CN115521282B (zh) * | 2022-08-23 | 2023-10-27 | 大理大学 | 一种香豆素化合物E-Suberenol的合成工艺 |
| CN115636742B (zh) * | 2022-11-11 | 2024-04-09 | 江西亚太科技发展有限公司 | 一种重结晶的方法 |
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| EP2518066B1 (en) * | 2009-12-18 | 2016-05-18 | Mitsubishi Tanabe Pharma Corporation | Novel anti-platelet agent |
| CN102372701A (zh) | 2010-08-10 | 2012-03-14 | 江苏恒瑞医药股份有限公司 | 氮杂双环己烷类衍生物、其制备方法及其在医药上的应用 |
| SG10201506238SA (en) | 2010-08-11 | 2015-09-29 | Millennium Pharm Inc | Heteroaryls And Uses Thereof |
| KR20140054295A (ko) | 2011-08-22 | 2014-05-08 | 머크 샤프 앤드 돔 코포레이션 | Bace 억제제로서의 2-스피로-치환된 이미노티아진 및 그의 모노- 및 디옥시드, 조성물 및 그의 용도 |
| EP2855489B1 (en) | 2012-04-26 | 2017-01-04 | Bristol-Myers Squibb Company | Imidazothiadiazole and imidazopyridazine derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation |
| JP6073464B2 (ja) * | 2012-04-26 | 2017-02-01 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | 血小板凝集を治療するためのプロテアーゼ活性化受容体4(par4)阻害剤としてのイミダゾチアジアゾールおよびイミダゾピラジン誘導体 |
| CA2879460C (en) | 2012-07-18 | 2021-10-19 | Garrett MORASKI | 5,5-heteroaromatic anti-infective compounds |
-
2013
- 2013-04-24 EP EP13719361.1A patent/EP2847200B1/en active Active
- 2013-04-24 EA EA201491967A patent/EA201491967A1/ru unknown
- 2013-04-24 KR KR20147030173A patent/KR20150003767A/ko not_active Withdrawn
- 2013-04-24 BR BR112014026493A patent/BR112014026493A2/pt not_active IP Right Cessation
- 2013-04-24 SG SG11201406759YA patent/SG11201406759YA/en unknown
- 2013-04-24 CA CA2871637A patent/CA2871637A1/en not_active Abandoned
- 2013-04-24 AU AU2013251683A patent/AU2013251683A1/en not_active Abandoned
- 2013-04-24 CN CN201380033512.1A patent/CN104540835B/zh active Active
- 2013-04-24 ES ES13719361.1T patent/ES2625029T3/es active Active
- 2013-04-24 US US14/396,807 patent/US9862730B2/en active Active
- 2013-04-24 JP JP2015509094A patent/JP6181744B2/ja active Active
- 2013-04-24 WO PCT/US2013/037892 patent/WO2013163244A1/en not_active Ceased
- 2013-04-24 MX MX2014012454A patent/MX2014012454A/es unknown
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2014
- 2014-10-19 IL IL235140A patent/IL235140A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2015518004A (ja) | 2015-06-25 |
| AU2013251683A1 (en) | 2014-12-18 |
| BR112014026493A2 (pt) | 2017-06-27 |
| JP6181744B2 (ja) | 2017-08-16 |
| EP2847200B1 (en) | 2017-03-29 |
| EP2847200A1 (en) | 2015-03-18 |
| CN104540835A (zh) | 2015-04-22 |
| US20150133446A1 (en) | 2015-05-14 |
| WO2013163244A8 (en) | 2014-04-03 |
| WO2013163244A1 (en) | 2013-10-31 |
| ES2625029T3 (es) | 2017-07-18 |
| KR20150003767A (ko) | 2015-01-09 |
| CA2871637A1 (en) | 2013-10-31 |
| US9862730B2 (en) | 2018-01-09 |
| CN104540835B (zh) | 2017-08-08 |
| IL235140A0 (en) | 2014-12-31 |
| SG11201406759YA (en) | 2014-11-27 |
| MX2014012454A (es) | 2015-03-13 |
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