IN2014CN04676A - - Google Patents
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- Publication number
- IN2014CN04676A IN2014CN04676A IN4676CHN2014A IN2014CN04676A IN 2014CN04676 A IN2014CN04676 A IN 2014CN04676A IN 4676CHN2014 A IN4676CHN2014 A IN 4676CHN2014A IN 2014CN04676 A IN2014CN04676 A IN 2014CN04676A
- Authority
- IN
- India
- Prior art keywords
- general formula
- compounds
- prodrugs
- solvates
- inhibitors
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 abstract 2
- 108010080805 Factor XIa Proteins 0.000 abstract 1
- 208000001435 Thromboembolism Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
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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
- A61K31/435—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
- A61K31/437—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 nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
-
- 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
-
- 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
-
- 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
- A61P9/06—Antiarrhythmics
-
- 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
-
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1122139.7A GB2497806A (en) | 2011-12-21 | 2011-12-21 | Pyridinone and pyrimidinone derivatives as factor XIa inhibitors |
| GB201217290A GB201217290D0 (en) | 2012-09-27 | 2012-09-27 | Compounds |
| PCT/GB2012/053217 WO2013093484A1 (en) | 2011-12-21 | 2012-12-20 | Pyridinone and pyrimidinone derivatives as factor xia inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IN2014CN04676A true IN2014CN04676A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) | 2015-09-18 |
Family
ID=47553259
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IN4676CHN2014 IN2014CN04676A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) | 2011-12-21 | 2012-12-20 |
Country Status (22)
Families Citing this family (68)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101901545B1 (ko) | 2010-02-11 | 2018-09-21 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 ＸＩａ 억제제로서의 마크로사이클 |
| US9062061B2 (en) * | 2011-07-13 | 2015-06-23 | Santen Pharmaceutical Co., Ltd. | Compound having PARP inhibitory activity |
| EP2899183B1 (en) | 2011-10-14 | 2018-09-19 | Bristol-Myers Squibb Company | Substituted Tetrahydroisoquinoline Compounds as Factor Xia Inhibitors |
| EP2766346B1 (en) | 2011-10-14 | 2017-03-29 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| CN103987696B (zh) | 2011-10-14 | 2016-12-21 | 百时美施贵宝公司 | 作为因子xia抑制剂的取代的四氢异喹啉化合物 |
| IN2014CN04676A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) * | 2011-12-21 | 2015-09-18 | Ono Pharmaceutical Co | |
| TW201332989A (zh) * | 2011-12-23 | 2013-08-16 | Millennium Pharm Inc | 雜芳基化合物及其用途 |
| AU2013291098A1 (en) | 2012-07-19 | 2015-02-05 | Sumitomo Dainippon Pharma Co., Ltd. | 1-(cycloalkyl-carbonyl)proline derivative |
| SMT201700240T1 (it) | 2012-08-03 | 2017-07-18 | Bristol Myers Squibb Co | Diidropiridone-p1 come inibitore del fattore xia |
| SG11201500270RA (en) | 2012-08-03 | 2015-03-30 | Bristol Myers Squibb Co | Dihydropyridone p1 as factor xia inhibitors |
| EP2906552B1 (en) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| WO2014059214A1 (en) | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| EA032092B1 (ru) | 2012-10-12 | 2019-04-30 | Бристол-Майерс Сквибб Компани | Кристаллические формы ингибитора фактора xia |
| JP6479763B2 (ja) | 2013-03-25 | 2019-03-06 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | 第ｘｉａ因子阻害剤としての置換アゾール含有のテトラヒドロイソキノリン |
| EP2978425B1 (en) * | 2013-03-27 | 2017-09-27 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| TWI633089B (zh) * | 2013-03-28 | 2018-08-21 | 拜耳製藥股份有限公司 | 經取代的酮基吡啶衍生物 |
| CA2918814C (en) | 2013-07-23 | 2021-10-12 | Bayer Pharma Aktiengesellschaft | Substituted oxopyridine derivatives and use thereof as factor xia/plasma |
| EP3063150B1 (de) * | 2013-10-30 | 2017-11-22 | Bayer Pharma Aktiengesellschaft | Substituierte oxopyridin-derivate |
| NO2760821T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) | 2014-01-31 | 2018-03-10 | ||
| EP3099686B1 (en) * | 2014-01-31 | 2020-03-11 | Bristol-Myers Squibb Company | Macrocycles with aromatic p2' groups as factor xia inhibitors |
| US9676723B2 (en) | 2014-02-11 | 2017-06-13 | Merck Sharp & Dohme Corp | Factor XIa inhibitors |
| WO2015123093A1 (en) | 2014-02-11 | 2015-08-20 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| CN105829298B (zh) | 2014-02-14 | 2019-02-01 | 四川海思科制药有限公司 | 一种吡啶酮或嘧啶酮衍生物、及其制备方法和应用 |
| WO2015164308A1 (en) | 2014-04-22 | 2015-10-29 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| CN105658641B (zh) * | 2014-07-25 | 2018-04-17 | 江苏恒瑞医药股份有限公司 | 氮茚‑酰胺类衍生物、其制备方法及其在医药上的应用 |
| WO2016015593A1 (en) | 2014-07-28 | 2016-02-04 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| EP3189047B1 (en) | 2014-09-04 | 2018-12-26 | Bristol-Myers Squibb Company | Diamide macrocycles that are fxia inhibitors |
| CN104311537B (zh) * | 2014-09-19 | 2016-08-24 | 广东东阳光药业有限公司 | 含有嘧啶酮乙酰基取代基吡唑类化合物及其组合物及用途 |
| WO2016046164A1 (de) * | 2014-09-24 | 2016-03-31 | Bayer Pharma Aktiengesellschaft | Substituierte oxopyridin-derivate |
| ES2722423T3 (es) * | 2014-09-24 | 2019-08-12 | Bayer Pharma AG | Derivados de oxopiridina sustituidos |
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| NO2721243T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) * | 2014-10-01 | 2018-10-20 | ||
| PT3231803T (pt) | 2014-12-10 | 2020-09-03 | Ono Pharmaceutical Co | Derivado de di-hidroindolizinona |
| GB201506660D0 (en) | 2015-04-20 | 2015-06-03 | Cellcentric Ltd | Pharmaceutical compounds |
| RU2649141C2 (ru) * | 2015-04-20 | 2018-03-30 | государственное бюджетное образовательное учреждение высшего профессионального образования "Пермская государственная фармацевтическая академия" Министерства здравоохранения Российской Федерации (ГБОУ ВПО ПГФА Минздрава России) | 3,4-диметил-6-(3-пиридил)-N-фенил-2-оксо-1,2,3,6-тетрагидропиримидин-5-карбоксамид, проявляющий противогрибковое действие в отношении штамма Candida albicans |
| GB201506658D0 (en) | 2015-04-20 | 2015-06-03 | Cellcentric Ltd | Pharmaceutical compounds |
| JO3703B1 (ar) | 2015-07-09 | 2021-01-31 | Bayer Pharma AG | مشتقات أوكسوبيريدين مستبدلة |
| RU2653511C2 (ru) * | 2015-07-29 | 2018-05-10 | государственное бюджетное образовательное учреждение высшего профессионального образования "Пермская государственная фармацевтическая академия" Министерства здравоохранения Российской Федерации (ГБОУ ВПО ПГФА Минздрава России) | 4-метил-n-2,4-диметилфенил-6-(3-фторфенил)-2-тиоксо-1,2,3,6-тетрагидропиримидин-5-карбоксамид, проявляющий анальгетическое действие |
| US10336730B2 (en) | 2015-08-05 | 2019-07-02 | Bristol-Myers Squibb Company | Substituted glycine derived FXIA inhibitors |
| CN106496249B (zh) * | 2015-09-07 | 2019-12-13 | 江苏恒瑞医药股份有限公司 | 噁唑并吲哚类衍生物、其制备方法及其在医药上的应用 |
| US10344039B2 (en) * | 2015-10-29 | 2019-07-09 | Merck Sharp & Dohme Corp. | Macrocyclic spirocarbamate derivatives as factor XIa inhibitors, pharmaceutically acceptable compositions and their use |
| CA2998902C (en) | 2015-10-29 | 2024-03-26 | Merck Sharp & Dohme Corp. | Macrocyclic compounds as factor xia inhibitors |
| JP6992284B2 (ja) * | 2016-06-06 | 2022-01-13 | 小野薬品工業株式会社 | ジヒドロインドリジノン誘導体を含有する医薬組成物 |
| EP3500556B1 (en) | 2016-08-22 | 2023-08-02 | Merck Sharp & Dohme LLC | Pyridine-1-oxide derivatives and their use as factor xia inhibitors |
| AU2017317988B2 (en) | 2016-08-31 | 2020-12-24 | Jiangsu Hengrui Medicine Co., Ltd. | Oxopicolinamide derivative, preparation method therefor and pharmaceutical use thereof |
| EP3305538A1 (de) | 2016-10-07 | 2018-04-11 | Mitsubishi HiTec Paper Europe GmbH | Wärmeempfindliches aufzeichnungsmaterial |
| EP3523134A1 (de) | 2016-10-07 | 2019-08-14 | Mitsubishi HiTec Paper Europe GmbH | Wärmeempfindliches aufzeichnungsmaterial |
| CN106950319B (zh) * | 2017-04-20 | 2019-08-30 | 西安科技大学 | 一种检测特鲁曲班光学异构体含量的方法 |
| CN109507345B (zh) * | 2017-09-15 | 2022-08-05 | 万特制药(海南)有限公司 | 重酒石酸卡巴拉汀中间体及其杂质的分离测定方法 |
| CA3091528A1 (en) | 2018-02-27 | 2019-09-06 | Jiangsu Hengrui Medicine Co., Ltd. | Crystal form of oxopicolinamide derivative and preparation method therefor |
| KR20210028232A (ko) | 2018-07-02 | 2021-03-11 | 지앙수 헨그루이 메디슨 컴퍼니 리미티드 | 옥시피리딘 아미드 유도체의 결정 형태 및 이를 위한 제조 방법 |
| TWI825144B (zh) * | 2018-08-10 | 2023-12-11 | 美商思達利醫藥公司 | 第二型轉麩醯胺酸酶(tg2)抑制劑 |
| WO2020094156A1 (zh) * | 2018-11-11 | 2020-05-14 | 上海海雁医药科技有限公司 | 双杂环取代的吡啶-2(1h)-酮衍生物、其制法与医药上的用途 |
| JP7196931B2 (ja) * | 2018-11-30 | 2022-12-27 | 小野薬品工業株式会社 | （３ｓ）－３－［２－（６－アミノ－２－フルオロピリジン－３－イル）－４－フルオロ－１ｈ－イミダゾール－５－イル］－７－［５－クロロ－２－（１ｈ－テトラゾール－１－イル）フェニル］－２，３－ジヒドロインドリジン－５（１ｈ）－オンの新規結晶 |
| CN109836360B (zh) * | 2019-03-19 | 2021-08-13 | 南京恩泰医药科技有限公司 | 一种甲苯磺酸依度沙班中间体的制备方法及中间体化合物 |
| CN112028877B (zh) * | 2019-06-04 | 2021-11-26 | 江西济民可信集团有限公司 | 烷氧吡啶酮化合物及其制备方法和用途 |
| JP7222123B2 (ja) * | 2019-06-28 | 2023-02-14 | シャンハイ ジェミンケア ファーマシューティカルズ カンパニー、リミテッド | 三環式化合物及びその製造方法と使用 |
| BR112022005660A2 (pt) * | 2019-09-27 | 2022-07-12 | Shenzhen Salubris Pharm Co Ltd | Inibidores de fxia e método de preparação dos mesmos e uso farmacêutico dos mesmos. |
| CN112778277B (zh) * | 2019-11-11 | 2024-04-02 | 江西济民可信集团有限公司 | 环酮并吡啶酮联杂芳环化合物及其制备方法和用途 |
| CN116133660B (zh) * | 2020-07-22 | 2025-05-02 | 詹森药业有限公司 | 可用作因子XIa抑制剂的化合物 |
| JP2024125436A (ja) * | 2021-07-20 | 2024-09-19 | 小野薬品工業株式会社 | イミダゾール化合物の製造方法 |
| US20230097157A1 (en) * | 2021-07-22 | 2023-03-30 | Janssen Pharmaceutica Nv | Bicyclic Pyridin-2-one and pyrimidin-4-one Derivatives Useful As a Factor XIa Inhibitors |
| US11958856B2 (en) | 2021-07-22 | 2024-04-16 | Janssen Pharmaceutica Nv | Substituted 1,2,3,8,9,9a-hexahydro-5H-pyrrolo[1,2-a]azepin-5-ones as factor XIa inhibitors |
| CN113735770B (zh) * | 2021-09-30 | 2023-06-06 | 四川大学 | 一种铑催化的4-苯基噁二唑酮与碳酸亚乙烯酯合成1-氨基异喹啉骨架的方法 |
| CN118974045A (zh) * | 2022-03-21 | 2024-11-15 | 上海济煜医药科技有限公司 | 三并环类化合物制备方法及其中间体 |
| CN116283908A (zh) * | 2023-03-10 | 2023-06-23 | 合肥工业大学 | 一种n-芳香甲基吡啶酮类衍生物及其制备方法与应用 |
| CN118406037B (zh) * | 2024-06-25 | 2025-02-25 | 四川师范大学 | 一种三氮唑类衍生物及其制备方法和用途 |
| CN118894814B (zh) * | 2024-07-15 | 2025-09-12 | 上海康鹏科技股份有限公司 | 1-(2-溴-4-氯苯基)-4-(三氟甲基)-1h-1，2，3-三唑的制备方法 |
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| BRPI0518126A (pt) | 2004-10-15 | 2008-10-28 | Astrazeneca Ab | composto, processo para preparar o mesmo, composição farmacêutica, uso de um composto, e, métodos para produzir um efeito inibitório de b-raf e um efeito anti-cáncer em um animal de sangue quente, e para tratar uma doença ou condição |
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| EP2102189B1 (en) * | 2006-12-15 | 2015-07-29 | Bristol-Myers Squibb Company | Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors |
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| US8324199B2 (en) * | 2008-03-13 | 2012-12-04 | Bristol-Myers Squibb Company | Pyridazine derivatives as factor xia inhibitors |
| CN102325765B (zh) | 2009-02-06 | 2014-12-24 | 杨森制药公司 | 作为γ-分泌酶调节剂的取代的双环杂环化合物 |
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2012
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