CY1119281T1 - Καινοφανεις μακροκυκλοι ως αναστολεις τελεστη xiα - Google Patents
Καινοφανεις μακροκυκλοι ως αναστολεις τελεστη xiαInfo
- Publication number
- CY1119281T1 CY1119281T1 CY20171100930T CY171100930T CY1119281T1 CY 1119281 T1 CY1119281 T1 CY 1119281T1 CY 20171100930 T CY20171100930 T CY 20171100930T CY 171100930 T CY171100930 T CY 171100930T CY 1119281 T1 CY1119281 T1 CY 1119281T1
- Authority
- CY
- Cyprus
- Prior art keywords
- xia
- open circuits
- new macro
- compounds
- macro cycles
- 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
- C07D471/02—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
- C07D471/08—Bridged systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
- 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
- C07D471/06—Peri-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
- C07D487/06—Peri-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
- C07D487/08—Bridged systems
-
- 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
- C07D498/02—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 two hetero rings
- C07D498/06—Peri-condensed systems
-
- 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
- C07D498/02—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 two hetero rings
- C07D498/08—Bridged systems
-
- 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
Abstract
Η παρούσα εφεύρεση παρέχει ενώσεις του Χημικού Τύπου (la): ή ένα στερεοϊσομερές, ταυτομερές, ή φαρμακευτικώς αποδεκτό άλας εξ' αυτών, όπου όλες οι μεταβλητές καθορίζονται ως εις το παρόν. Αυτές οι ενώσεις είναι επιλεκτικοί αναστολείς τελεστή XIa ή διπλοί αναστολείς του FXIa και της καλλικρεΐνης πλάσματος. Αυτή η εφεύρεση σχετίζεται επίσης με φαρμακευτικές συνθέσεις που περιλαμβάνουν αυτές τις ενώσεις και μεθόδους αγωγής θρομβοεμβολικών και/ή φλεγμονωδών διαταραχών χρησιμοποιώντας τις ίδιες.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201161515401P | 2011-08-05 | 2011-08-05 | |
PCT/US2012/049706 WO2013022818A1 (en) | 2011-08-05 | 2012-08-06 | Novel macrocycles as factor xia inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
CY1119281T1 true CY1119281T1 (el) | 2018-02-14 |
Family
ID=46889416
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CY20171100930T CY1119281T1 (el) | 2011-08-05 | 2017-09-04 | Καινοφανεις μακροκυκλοι ως αναστολεις τελεστη xiα |
Country Status (21)
Country | Link |
---|---|
US (4) | US9221818B2 (el) |
EP (1) | EP2739628B1 (el) |
JP (1) | JP6158181B2 (el) |
CN (1) | CN103857681B (el) |
AR (1) | AR088748A1 (el) |
BR (1) | BR112014002202A2 (el) |
CA (1) | CA2844254A1 (el) |
CY (1) | CY1119281T1 (el) |
DK (1) | DK2739628T3 (el) |
EA (1) | EA024791B1 (el) |
ES (1) | ES2635088T3 (el) |
HR (1) | HRP20171122T1 (el) |
HU (1) | HUE034487T2 (el) |
LT (1) | LT2739628T (el) |
MX (1) | MX345763B (el) |
PL (1) | PL2739628T3 (el) |
PT (1) | PT2739628T (el) |
RS (1) | RS56244B1 (el) |
SI (1) | SI2739628T1 (el) |
TW (1) | TW201311689A (el) |
WO (1) | WO2013022818A1 (el) |
Families Citing this family (47)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU2011215898B2 (en) | 2010-02-11 | 2016-08-11 | Bristol-Myers Squibb Company | Macrocycles as Factor XIa inhibitors |
TW201311689A (zh) | 2011-08-05 | 2013-03-16 | 必治妥美雅史谷比公司 | 作為因子xia抑制劑之新穎巨環化合物 |
TW201319068A (zh) | 2011-08-05 | 2013-05-16 | 必治妥美雅史谷比公司 | 作為xia因子抑制劑之環狀p1接合劑 |
SG11201401384UA (en) | 2011-10-14 | 2014-09-26 | Bristol Myers Squibb Co | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
ES2579832T3 (es) | 2011-10-14 | 2016-08-17 | Bristol-Myers Squibb Company | Compuestos de tetrahidroisoquinolina sustituida como inhibidores del factor XIa |
CN103987697B (zh) | 2011-10-14 | 2017-04-26 | 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 |
BR112015002293A2 (pt) | 2012-08-03 | 2017-07-04 | Bristol Myers Squibb Co | di-hidropiridona pi como inibidores do fator xia |
US9409908B2 (en) | 2012-08-03 | 2016-08-09 | Bristol-Myers Squibb Company | Dihydropyridone p1 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 |
CN104837833B (zh) | 2012-10-12 | 2017-07-14 | 百时美施贵宝公司 | Xia因子抑制剂的晶型 |
EP2906552B1 (en) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
ES2712699T3 (es) | 2013-03-25 | 2019-05-14 | Bristol Myers Squibb Co | Tetrahidroisoquinolinas que contienen azoles sustituidos como inhibidores del factor XIa |
WO2014160592A2 (en) | 2013-03-27 | 2014-10-02 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
FR3010076B1 (fr) * | 2013-09-02 | 2016-12-23 | Centre Nat De La Rech Scient - Cnrs - | Inhibiteurs de metalloproteases, leurs procedes de preparation et leurs utilisations therapeutiques |
NO2760821T3 (el) | 2014-01-31 | 2018-03-10 | ||
CN116987080A (zh) * | 2014-01-31 | 2023-11-03 | 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 |
EP3104703B1 (en) * | 2014-02-11 | 2020-11-18 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
EP3104702B1 (en) | 2014-02-11 | 2022-08-10 | Merck Sharp & Dohme LLC | Factor xia inhibitors |
WO2015164308A1 (en) | 2014-04-22 | 2015-10-29 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
EP3180317B1 (en) | 2014-07-28 | 2021-04-14 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
JP6526796B2 (ja) * | 2014-09-04 | 2019-06-05 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | Fxia阻害剤であるジアミドマクロ環 |
NO2721243T3 (el) * | 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 |
CN114874222A (zh) | 2015-07-29 | 2022-08-09 | 百时美施贵宝公司 | 携带非芳族p2,基团的因子xia新大环 |
EP3328851B1 (en) | 2015-07-29 | 2020-04-22 | Bristol-Myers Squibb Company | Factor xia macrocyclic inhibitors bearing alkyl or cycloalkyl p2' moieties |
EA202191548A1 (ru) | 2015-10-01 | 2021-09-02 | Байокрист Фармасьютикалз, Инк. | Ингибиторы плазменного калликреина человека |
EP3371162B1 (en) | 2015-10-29 | 2022-01-26 | Merck Sharp & Dohme Corp. | Macrocyclic spirocarbamate derivatives as factor xia inhibitors, pharmaceutically acceptable compositions and their use |
BR112018008506B8 (pt) * | 2015-10-29 | 2023-12-05 | Merck Sharp & Dohme | Compostos inibidores do fator xia, composição farmacêutica e usos dos mesmos |
EP3423458A1 (en) | 2016-03-02 | 2019-01-09 | Bristol-Myers Squibb Company | Diamide macrocycles having factor xia inhibiting activity |
US20190135761A1 (en) * | 2016-05-10 | 2019-05-09 | Solvay Sa | Composition comprising 3-(haloalkyl or formyl)-1h-pyrazole-4-carboxylic acids or esters, its manufacture and its use for the preparation of carboxamides |
TW201808908A (zh) | 2016-08-22 | 2018-03-16 | 美商默沙東藥廠 | 因子XIa抑制劑 |
EP3309143A1 (en) * | 2016-10-17 | 2018-04-18 | Solvay SA | Method for producing fluoroformate compounds |
TW201822637A (zh) | 2016-11-07 | 2018-07-01 | 德商拜耳廠股份有限公司 | 用於控制動物害蟲的經取代磺醯胺類 |
CN107011275A (zh) * | 2017-03-31 | 2017-08-04 | 深圳市众康动保科技有限公司 | 一种1,4,5‑三取代‑1,2,3‑三氮唑类化合物的合成方法 |
WO2019011166A1 (zh) * | 2017-07-14 | 2019-01-17 | 四川科伦博泰生物医药股份有限公司 | 大环酰胺化合物及其药物组合物和用途 |
US20220204508A1 (en) | 2019-04-16 | 2022-06-30 | Medshine Discovery Inc. | Macrocyclic derivatives acting as xia factor inhibitor |
CN114008047B (zh) | 2019-07-23 | 2023-03-21 | 南京明德新药研发有限公司 | 作为XIa因子抑制剂的大环衍生物 |
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CA3159559A1 (en) | 2019-11-04 | 2021-05-14 | Revolution Medicines, Inc. | Ras inhibitors |
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KR20230067635A (ko) | 2020-09-15 | 2023-05-16 | 레볼루션 메디슨즈, 인크. | 암의 치료에서 ras 억제제로서 인돌 유도체 |
CN112920005B (zh) * | 2021-01-31 | 2022-06-14 | 上海李氏化学科技有限公司 | 一种(r)-3-(3-氯-2-氟苯)-4,5-二氢异噁唑-5-羧酸的制备方法 |
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CN113336715B (zh) * | 2021-08-04 | 2021-11-23 | 山东海利尔化工有限公司 | 一种含二氧戊环的三唑类化合物及其中间体的制备方法 |
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PE20071132A1 (es) * | 2005-12-23 | 2007-12-14 | Bristol Myers Squibb Co | Compuestos macrociclicos como inhibidores del factor viia |
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TW201319068A (zh) | 2011-08-05 | 2013-05-16 | 必治妥美雅史谷比公司 | 作為xia因子抑制劑之環狀p1接合劑 |
TW201311689A (zh) | 2011-08-05 | 2013-03-16 | 必治妥美雅史谷比公司 | 作為因子xia抑制劑之新穎巨環化合物 |
CN103987697B (zh) | 2011-10-14 | 2017-04-26 | 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 |
ES2579832T3 (es) | 2011-10-14 | 2016-08-17 | Bristol-Myers Squibb Company | Compuestos de tetrahidroisoquinolina sustituida como inhibidores del factor XIa |
SG11201401384UA (en) | 2011-10-14 | 2014-09-26 | Bristol Myers Squibb Co | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
US9409908B2 (en) | 2012-08-03 | 2016-08-09 | Bristol-Myers Squibb Company | Dihydropyridone p1 as factor XIa inhibitors |
BR112015002293A2 (pt) | 2012-08-03 | 2017-07-04 | Bristol Myers Squibb Co | di-hidropiridona pi como inibidores do fator xia |
EP2906552B1 (en) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
CN104837833B (zh) | 2012-10-12 | 2017-07-14 | 百时美施贵宝公司 | Xia因子抑制剂的晶型 |
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2012
- 2012-08-03 TW TW101128173A patent/TW201311689A/zh unknown
- 2012-08-06 CA CA2844254A patent/CA2844254A1/en not_active Abandoned
- 2012-08-06 EA EA201490418A patent/EA024791B1/ru not_active IP Right Cessation
- 2012-08-06 WO PCT/US2012/049706 patent/WO2013022818A1/en active Application Filing
- 2012-08-06 PT PT127624278T patent/PT2739628T/pt unknown
- 2012-08-06 US US14/236,973 patent/US9221818B2/en active Active
- 2012-08-06 EP EP12762427.8A patent/EP2739628B1/en active Active
- 2012-08-06 MX MX2014000831A patent/MX345763B/es active IP Right Grant
- 2012-08-06 PL PL12762427T patent/PL2739628T3/pl unknown
- 2012-08-06 SI SI201231004T patent/SI2739628T1/sl unknown
- 2012-08-06 RS RS20170852A patent/RS56244B1/sr unknown
- 2012-08-06 JP JP2014524152A patent/JP6158181B2/ja active Active
- 2012-08-06 ES ES12762427.8T patent/ES2635088T3/es active Active
- 2012-08-06 BR BR112014002202A patent/BR112014002202A2/pt not_active Application Discontinuation
- 2012-08-06 LT LTEP12762427.8T patent/LT2739628T/lt unknown
- 2012-08-06 HU HUE12762427A patent/HUE034487T2/en unknown
- 2012-08-06 CN CN201280049108.9A patent/CN103857681B/zh active Active
- 2012-08-06 DK DK12762427.8T patent/DK2739628T3/en active
- 2012-08-07 AR ARP120102878A patent/AR088748A1/es unknown
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2015
- 2015-11-16 US US14/942,013 patent/US9611274B2/en active Active
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2017
- 2017-02-21 US US15/437,605 patent/US9902742B2/en active Active
- 2017-07-21 HR HRP20171122TT patent/HRP20171122T1/hr unknown
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US20160068544A1 (en) | 2016-03-10 |
LT2739628T (lt) | 2017-08-25 |
JP2014521701A (ja) | 2014-08-28 |
PT2739628T (pt) | 2017-08-02 |
DK2739628T3 (en) | 2017-09-11 |
SI2739628T1 (sl) | 2017-08-31 |
US9611274B2 (en) | 2017-04-04 |
US20140221338A1 (en) | 2014-08-07 |
WO2013022818A1 (en) | 2013-02-14 |
HRP20171122T1 (hr) | 2017-10-06 |
EP2739628B1 (en) | 2017-06-07 |
AR088748A1 (es) | 2014-07-02 |
TW201311689A (zh) | 2013-03-16 |
EA024791B1 (ru) | 2016-10-31 |
JP6158181B2 (ja) | 2017-07-05 |
US9221818B2 (en) | 2015-12-29 |
EA201490418A1 (ru) | 2014-05-30 |
US20180148461A1 (en) | 2018-05-31 |
ES2635088T3 (es) | 2017-10-02 |
EP2739628A1 (en) | 2014-06-11 |
CN103857681B (zh) | 2017-07-14 |
CA2844254A1 (en) | 2013-02-14 |
US9902742B2 (en) | 2018-02-27 |
HUE034487T2 (en) | 2018-02-28 |
BR112014002202A2 (pt) | 2017-03-07 |
US20170158712A1 (en) | 2017-06-08 |
CN103857681A (zh) | 2014-06-11 |
US10208068B2 (en) | 2019-02-19 |
MX345763B (es) | 2017-02-15 |
RS56244B1 (sr) | 2017-11-30 |
PL2739628T3 (pl) | 2017-11-30 |
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