EA201691561A1 - Макроциклические ингибиторы фактора xia, конденсированные с гетероциклами - Google Patents
Макроциклические ингибиторы фактора xia, конденсированные с гетероцикламиInfo
- Publication number
- EA201691561A1 EA201691561A1 EA201691561A EA201691561A EA201691561A1 EA 201691561 A1 EA201691561 A1 EA 201691561A1 EA 201691561 A EA201691561 A EA 201691561A EA 201691561 A EA201691561 A EA 201691561A EA 201691561 A1 EA201691561 A1 EA 201691561A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- heterocycles
- condensed
- compounds
- present
- macrocyclic inhibitors
- Prior art date
Links
Classifications
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- 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
- C07D471/12—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 three hetero rings
- C07D471/18—Bridged systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
-
- 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
- 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
- C07D487/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Настоящее изобретение относится к соединениям формулы (Ia)или их стереоизомерам, таутомерам или фармацевтически приемлемым солям, где все переменные определены в настоящем описании. Эти соединения представляют собой селективные ингибиторы фактора XIa или двойные ингибиторы FXIa и калликреина плазмы. Настоящее изобретение также относится к фармацевтическим композициям, содержащим указанные соединения, и к способам лечения тромбоэмболических и/или воспалительных заболеваний с их использованием.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201461933948P | 2014-01-31 | 2014-01-31 | |
PCT/US2015/013647 WO2015116882A1 (en) | 2014-01-31 | 2015-01-30 | Macrocyclic factor xia inhibitors condensed with heterocycles |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201691561A1 true EA201691561A1 (ru) | 2017-01-30 |
EA032650B1 EA032650B1 (ru) | 2019-06-28 |
Family
ID=52484569
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201691561A EA032650B1 (ru) | 2014-01-31 | 2015-01-30 | Макроциклические ингибиторы фактора xia, конденсированные с гетероциклами |
Country Status (23)
Country | Link |
---|---|
US (3) | US20170057961A1 (ru) |
EP (1) | EP3099688B1 (ru) |
JP (1) | JP6419836B2 (ru) |
CN (1) | CN106459051B (ru) |
AR (1) | AR099228A1 (ru) |
BR (1) | BR112016016741B1 (ru) |
CA (1) | CA2937738C (ru) |
CY (1) | CY1120534T1 (ru) |
DK (1) | DK3099688T3 (ru) |
EA (1) | EA032650B1 (ru) |
ES (1) | ES2655540T3 (ru) |
HR (1) | HRP20172002T1 (ru) |
HU (1) | HUE038060T2 (ru) |
LT (1) | LT3099688T (ru) |
MX (1) | MX2016009385A (ru) |
NO (1) | NO2760821T3 (ru) |
PL (1) | PL3099688T3 (ru) |
PT (1) | PT3099688T (ru) |
RS (1) | RS56785B1 (ru) |
SI (1) | SI3099688T1 (ru) |
TW (1) | TWI703144B (ru) |
UY (1) | UY35972A (ru) |
WO (1) | WO2015116882A1 (ru) |
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TWI586651B (zh) | 2011-10-14 | 2017-06-11 | 必治妥美雅史谷比公司 | 作為因子xia抑制劑之經取代四氫異喹啉化合物 |
US9738655B2 (en) | 2013-03-25 | 2017-08-22 | Bristol-Myers Squibb Company | Tetrahydroisoquinolines containing substituted azoles as factor XIa inhibitors |
CN110845498B (zh) | 2014-01-31 | 2023-02-17 | 百时美施贵宝公司 | 作为因子xia抑制剂的具有杂环p2′基团的大环化合物 |
NO2760821T3 (ru) | 2014-01-31 | 2018-03-10 | ||
WO2016036893A1 (en) | 2014-09-04 | 2016-03-10 | Bristol-Myers Squibb Company | Diamide macrocycles that are fxia inhibitors |
NO2721243T3 (ru) * | 2014-10-01 | 2018-10-20 | ||
US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
JP6742348B2 (ja) | 2015-06-19 | 2020-08-19 | 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ジアミド大員環 |
ES2871111T3 (es) | 2015-07-29 | 2021-10-28 | Bristol Myers Squibb Co | Inhibidores macrocíclicos del factor XIa que contienen un grupo P2' no aromático |
CN107849026B (zh) * | 2015-07-29 | 2021-01-01 | 百时美施贵宝公司 | 携带烷基或环烷基p2′部分的因子xia大环抑制剂 |
EP3368036B1 (en) * | 2015-10-29 | 2022-07-20 | Merck Sharp & Dohme LLC | Macrocyclic pyridine-n-oxide derivatives as factor xia inhibitors |
WO2017074833A1 (en) | 2015-10-29 | 2017-05-04 | Merck Sharp & Dohme Corp. | Macrocyclic spirocarbamate derivatives as factor xia inhibitors, pharmaceutically acceptable compositions and their use |
US10752641B2 (en) | 2016-03-02 | 2020-08-25 | Bristol-Myers Squibb Company | Diamide macrocycles having factor XIa inhibiting activity |
TW201808908A (zh) | 2016-08-22 | 2018-03-16 | 美商默沙東藥廠 | 因子XIa抑制劑 |
WO2018095953A1 (de) | 2016-11-23 | 2018-05-31 | Bayer Cropscience Aktiengesellschaft | 2-[3-(alkylsulfonyl)-2h-indazol-2-yl]-3h-imidazo[4,5-b]pyridin-derivate und ähnliche verbindungen als schädlingsbekämpfungsmittel |
EP3568392B1 (de) | 2017-01-10 | 2021-02-24 | Bayer Aktiengesellschaft | Imidazol-derivate als schädlingsbekämpfungsmittel |
KR20230020566A (ko) | 2017-01-10 | 2023-02-10 | 바이엘 악티엔게젤샤프트 | 해충 방제제로서의 헤테로사이클 유도체 |
CN110062757B (zh) * | 2017-01-18 | 2022-03-04 | 广东东阳光药业有限公司 | 凝血因子XIa抑制剂及其用途 |
CN110922412A (zh) * | 2018-09-20 | 2020-03-27 | 复旦大学 | 具有抗精神病作用药物化合物的不对称合成方法 |
KR102709654B1 (ko) * | 2019-04-16 | 2024-09-26 | 차이나 리소어시즈 바이오파마슈티컬 컴퍼니 리미티드 | XIa 인자 억제제로서의 거대고리 유도체 |
EP3997492A4 (en) * | 2019-07-08 | 2023-11-15 | Meta Platforms Technologies, Llc | HIGH CONTRAST COLLIMATORS BASED ON COMPACT POLARIZATION |
JP7286001B2 (ja) * | 2019-07-23 | 2023-06-02 | メッドシャイン ディスカバリー インコーポレイテッド | 第XIa因子阻害剤としての大環状誘導体 |
TW202246268A (zh) * | 2021-04-21 | 2022-12-01 | 大陸商上海美悦生物科技發展有限公司 | FXIa抑制劑及其藥物組合物、製備方法和用途 |
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US20180222907A1 (en) | 2018-08-09 |
CA2937738C (en) | 2023-01-17 |
SI3099688T1 (sl) | 2017-12-29 |
JP2017504640A (ja) | 2017-02-09 |
AR099228A1 (es) | 2016-07-06 |
US20170342071A1 (en) | 2017-11-30 |
TW201615640A (zh) | 2016-05-01 |
RS56785B1 (sr) | 2018-04-30 |
LT3099688T (lt) | 2017-12-27 |
MX2016009385A (es) | 2016-09-16 |
TWI703144B (zh) | 2020-09-01 |
CN106459051B (zh) | 2018-10-16 |
US20170057961A1 (en) | 2017-03-02 |
BR112016016741A2 (ru) | 2017-08-08 |
UY35972A (es) | 2015-07-31 |
EP3099688A1 (en) | 2016-12-07 |
PL3099688T3 (pl) | 2018-03-30 |
HUE038060T2 (hu) | 2018-09-28 |
JP6419836B2 (ja) | 2018-11-07 |
CA2937738A1 (en) | 2015-08-06 |
PT3099688T (pt) | 2018-01-15 |
WO2015116882A1 (en) | 2015-08-06 |
BR112016016741B1 (pt) | 2023-01-17 |
DK3099688T3 (en) | 2018-01-15 |
EP3099688B1 (en) | 2017-10-18 |
US10273236B2 (en) | 2019-04-30 |
CY1120534T1 (el) | 2019-07-10 |
NO2760821T3 (ru) | 2018-03-10 |
CN106459051A (zh) | 2017-02-22 |
HRP20172002T1 (hr) | 2018-02-09 |
EA032650B1 (ru) | 2019-06-28 |
ES2655540T3 (es) | 2018-02-20 |
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