ATE543811T1 - Pyridazinderivate als faktor-xia-inhibitoren - Google Patents
Pyridazinderivate als faktor-xia-inhibitorenInfo
- Publication number
- ATE543811T1 ATE543811T1 AT09720875T AT09720875T ATE543811T1 AT E543811 T1 ATE543811 T1 AT E543811T1 AT 09720875 T AT09720875 T AT 09720875T AT 09720875 T AT09720875 T AT 09720875T AT E543811 T1 ATE543811 T1 AT E543811T1
- Authority
- AT
- Austria
- Prior art keywords
- factor xia
- xia inhibitors
- compounds
- pyridazine derivatives
- inhibitors
- Prior art date
Links
Classifications
-
- 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
- C07D403/02—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 two hetero rings
- C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61P9/10—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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D498/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US3612708P | 2008-03-13 | 2008-03-13 | |
US14520309P | 2009-01-16 | 2009-01-16 | |
PCT/US2009/036934 WO2009114677A1 (en) | 2008-03-13 | 2009-03-12 | Pyridazine derivatives as factor xia inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
ATE543811T1 true ATE543811T1 (de) | 2012-02-15 |
Family
ID=40640383
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
AT09720875T ATE543811T1 (de) | 2008-03-13 | 2009-03-12 | Pyridazinderivate als faktor-xia-inhibitoren |
Country Status (8)
Country | Link |
---|---|
US (1) | US8324199B2 (de) |
EP (1) | EP2265601B1 (de) |
JP (1) | JP5537442B2 (de) |
CN (1) | CN102026996B (de) |
AT (1) | ATE543811T1 (de) |
ES (1) | ES2380648T3 (de) |
TW (1) | TW200942527A (de) |
WO (1) | WO2009114677A1 (de) |
Families Citing this family (72)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8791792B2 (en) * | 2010-01-15 | 2014-07-29 | Idex Asa | Electronic imager using an impedance sensor grid array mounted on or about a switch and method of making |
JP5841547B2 (ja) | 2010-02-11 | 2016-01-13 | 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マクロ環 |
LV14606B (lv) | 2011-05-17 | 2013-01-20 | Tetra, Sia | Jauns XII faktora inhibitors |
JP6205354B2 (ja) * | 2011-07-06 | 2017-09-27 | ギリアード サイエンシーズ, インコーポレイテッド | Hivの処置のための化合物 |
GB2494851A (en) | 2011-07-07 | 2013-03-27 | Kalvista Pharmaceuticals Ltd | Plasma kallikrein 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 |
PT2766346T (pt) | 2011-10-14 | 2017-05-26 | Bristol Myers Squibb Co | Compostos de tetrahidroisoquinolina substituídos como inibidores do fator xia |
EP2766345B1 (de) | 2011-10-14 | 2016-03-16 | Bristol-Myers Squibb Company | Substituierte tetrahydroisochinolinverbindungen als faktor-xia-hemmer |
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 |
RU2630677C2 (ru) * | 2011-12-21 | 2017-09-12 | Оно Фармасьютикал Ко., Лтд. | Соединения |
CN104203935A (zh) | 2012-04-04 | 2014-12-10 | 霍夫曼-拉罗奇有限公司 | 作为gpbar1调节剂的1,2-哒嗪,1,6-哒嗪或嘧啶-苯甲酰胺衍生物 |
KR102245293B1 (ko) | 2012-04-10 | 2021-04-28 | 이덱스 바이오메트릭스 아사 | 생체정보의 감지 |
GB201209138D0 (en) * | 2012-05-24 | 2012-07-04 | Ono Pharmaceutical Co | Compounds |
MX361370B (es) | 2012-08-03 | 2018-12-05 | Bristol Myers Squibb Co | Dihidropiridona p1 como inhibidores del factor xia. |
WO2014022767A1 (en) | 2012-08-03 | 2014-02-06 | Bristol-Myers Squibb Company | Dihydropyridone p1 as factor xia inhibitors |
WO2014059202A1 (en) | 2012-10-12 | 2014-04-17 | 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 |
BR112015007937A2 (pt) * | 2012-10-12 | 2017-07-04 | Bristol Myers Squibb Co | formas cristalinas de um inibidor de fator xia |
IL239682B (en) | 2013-01-08 | 2018-10-31 | Kalvista Pharmaceuticals Ltd | History of benzylamine and 2-(aminomethyl)pyridine |
GB201300304D0 (en) * | 2013-01-08 | 2013-02-20 | Kalvista Pharmaceuticals Ltd | Benzylamine derivatives |
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 |
TWI636047B (zh) | 2013-08-14 | 2018-09-21 | 英商卡爾維斯塔製藥有限公司 | 雜環衍生物 |
EP3054944B1 (de) * | 2013-10-07 | 2019-12-04 | Merck Sharp & Dohme Corp. | Faktor-xia-hemmer |
NO2760821T3 (de) | 2014-01-31 | 2018-03-10 | ||
IL298983B2 (en) | 2014-01-31 | 2024-03-01 | Bristol Myers Squibb Co | Macrocyclines with P2' heterocyclic groups as factor XIA inhibitors |
CN106029064B (zh) * | 2014-02-07 | 2018-08-14 | 艾克赛特赫拉制药有限责任公司 | 治疗化合物和组合物 |
WO2015123091A1 (en) | 2014-02-11 | 2015-08-20 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
US9944643B2 (en) | 2014-02-11 | 2018-04-17 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
EP3134408B1 (de) | 2014-04-22 | 2020-08-12 | Merck Sharp & Dohme Corp. | Faktor-xia-hemmer |
US9868727B2 (en) | 2014-07-28 | 2018-01-16 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
US9988443B2 (en) | 2014-08-07 | 2018-06-05 | Novartis Ag | Angiopoetin-like 4 (ANGPTL4) antibodies and methods of use |
NZ728425A (en) | 2014-08-07 | 2022-05-27 | Novartis Ag | Angiopoietin-like 4 antibodies and methods of use |
CN107074821B (zh) | 2014-09-04 | 2020-05-22 | 百时美施贵宝公司 | 为fxia抑制剂的二酰胺大环化合物 |
US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
CN104387376B (zh) * | 2014-10-30 | 2017-01-18 | 广东东阳光药业有限公司 | 吡啶酮类化合物及其组合物和用途 |
GB201421085D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | New enzyme inhibitors |
GB201421083D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | Enzyme inhibitors |
EP3310777B1 (de) | 2015-06-19 | 2019-10-09 | Bristol-Myers Squibb Company | Diamid makrocyclen als faktor xia inhibitoren |
JOP20200312A1 (ar) | 2015-06-26 | 2017-06-16 | Novartis Ag | الأجسام المضادة للعامل xi وطرق الاستخدام |
EP3328852B1 (de) | 2015-07-29 | 2021-04-28 | Bristol-Myers Squibb Company | Makrozyklische faktor-xia-hemmer mit einer nichtaromatischen p2'-gruppe |
EP3328851B1 (de) | 2015-07-29 | 2020-04-22 | Bristol-Myers Squibb Company | Makrocyclische inhibitoren von xia-faktor mit alkyl- oder cycloalkyl-p2'-gruppen |
CN108430471B (zh) | 2015-10-29 | 2021-07-09 | 默沙东公司 | 因子XIa抑制剂 |
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 |
CN105400143B (zh) * | 2015-12-11 | 2017-10-03 | 广州欣凯化工科技有限公司 | 一种木制品缝隙的修补组合物 |
TW201802121A (zh) | 2016-05-25 | 2018-01-16 | 諾華公司 | 抗因子XI/XIa抗體之逆轉結合劑及其用途 |
HUE049918T2 (hu) | 2016-05-31 | 2020-11-30 | Kalvista Pharmaceuticals Ltd | Pirazol-származékok mint plazma kallikrein inhibitorok |
GB201609603D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide |
GB201609607D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts |
BR122020001791B1 (pt) | 2016-08-19 | 2022-01-25 | Gilead Sciences, Inc | Usos de compostos terapêuticos no tratamento profilático ou terapêutico de uma infecção por vírus hiv |
TW201808908A (zh) | 2016-08-22 | 2018-03-16 | 美商默沙東藥廠 | 因子XIa抑制劑 |
AU2017383232A1 (en) | 2016-12-23 | 2019-06-27 | Novartis Ag | Factor XI antibodies and methods of use |
TW202024061A (zh) | 2017-08-17 | 2020-07-01 | 美商基利科學股份有限公司 | Hiv蛋白質膜抑制劑之固體形式 |
AR112412A1 (es) | 2017-08-17 | 2019-10-23 | Gilead Sciences Inc | Formas de sal de colina de un inhibidor de la cápside del vih |
LT3716952T (lt) | 2017-11-29 | 2022-04-11 | Kalvista Pharmaceuticals Limited | Vaisto formos, apimančios plazmos kalikreino inhibitorių |
GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
EP3752495B1 (de) | 2018-02-15 | 2023-07-19 | Gilead Sciences, Inc. | Pyridinderivate und ihre verwendung zur behandlung von hiv-infektionen |
EP3752496B1 (de) | 2018-02-16 | 2023-07-05 | Gilead Sciences, Inc. | Verfahren und zwischenprodukte zur herstellung einer therapeutischen verbindung zur behandlung von retroviridae-vireninfektionen |
JP2021530523A (ja) | 2018-07-16 | 2021-11-11 | ギリアード サイエンシーズ, インコーポレイテッド | Hivの処置のためのカプシド阻害剤 |
MA55381A (fr) * | 2019-03-20 | 2022-01-26 | Goldfinch Bio Inc | Pyridazinones et leurs procédés d'utilisation |
WO2021028645A1 (en) | 2019-08-09 | 2021-02-18 | Kalvista Pharmaceuticals Limited | Plasma kallikrein inhibitors |
TWI749881B (zh) * | 2019-11-21 | 2021-12-11 | 大陸商深圳信立泰藥業股份有限公司 | 二氧代哌類衍生物、其製備方法及其在醫藥上的應用 |
WO2021108544A1 (en) | 2019-11-26 | 2021-06-03 | Gilead Sciences, Inc. | Capsid inhibitors for the prevention of hiv |
WO2021136390A1 (zh) * | 2019-12-31 | 2021-07-08 | 上海京新生物医药有限公司 | 凝血因子XIa抑制剂 |
WO2021262990A1 (en) | 2020-06-25 | 2021-12-30 | Gilead Sciences, Inc. | Capsid inhibitors for the treatment of hiv |
TW202227079A (zh) * | 2020-10-23 | 2022-07-16 | 大陸商深圳信立泰藥業股份有限公司 | FXIa抑制劑化合物或其鹽的醫藥用途及含有其的藥物組合物 |
CN112679446A (zh) * | 2020-10-26 | 2021-04-20 | 都创(上海)医药科技有限公司 | 一种合成反式-3-(3-氯-2-氟-6-(1h-四氮唑-1-基)苯基)丙烯酸的方法 |
CN117480164A (zh) * | 2020-12-11 | 2024-01-30 | 上海领泰生物医药科技有限公司 | 凝血因子XIa抑制剂及其制备方法和应用 |
CN112675173B (zh) * | 2020-12-25 | 2022-04-05 | 华南理工大学 | FXIa抑制剂化合物或其盐的医药用途 |
CN112608303B (zh) * | 2020-12-25 | 2021-10-26 | 华南理工大学 | 一种哌嗪类中间体及其制备方法与应用 |
TW202337439A (zh) | 2021-12-03 | 2023-10-01 | 美商基利科學股份有限公司 | 用於hiv病毒感染之治療性化合物 |
CN114315623B (zh) * | 2022-01-13 | 2024-02-09 | 上海彤颜实业有限公司 | 一锅合成花椒素wgx-50及其衍生物的方法 |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20040180855A1 (en) * | 2003-02-19 | 2004-09-16 | Schumacher William A. | Methods of treating thrombosis with reduced risk of increased bleeding times |
US7429604B2 (en) * | 2004-06-15 | 2008-09-30 | Bristol Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
US7453002B2 (en) * | 2004-06-15 | 2008-11-18 | Bristol-Myers Squibb Company | Five-membered heterocycles useful as serine protease inhibitors |
JP4478157B2 (ja) * | 2004-10-13 | 2010-06-09 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ヒドラジド誘導体 |
US7459564B2 (en) * | 2005-01-13 | 2008-12-02 | Bristol-Myers Squibb Company | Substituted biaryl compounds as factor XIa inhibitors |
AR056764A1 (es) * | 2005-11-03 | 2007-10-24 | Vertex Pharma | Aminopirimidinas utiles como inhibidores de quinasa |
WO2007070818A1 (en) * | 2005-12-14 | 2007-06-21 | Bristol-Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
EP1981854B1 (de) | 2005-12-14 | 2011-06-01 | Bristol-Myers Squibb Company | Arylpropionamid-, arylacrylamid-, arylpropinamid- oder arylmethylharnstoffanaloge als faktor-xia-inhibitoren |
US8466295B2 (en) * | 2005-12-14 | 2013-06-18 | Bristol-Myers Squibb Company | Thiophene derivatives as factor XIa inhibitors |
CN101605779B (zh) * | 2006-12-15 | 2013-11-20 | 百时美施贵宝公司 | 作为凝血因子xia抑制剂的芳基丙酰胺、芳基丙烯酰胺、芳基丙炔酰胺或芳基甲基脲类似物 |
AU2008266228A1 (en) * | 2007-06-13 | 2008-12-24 | Bristol-Myers Squibb Company | Dipeptide analogs as coagulation factor inhibitors |
-
2009
- 2009-03-12 JP JP2010550858A patent/JP5537442B2/ja not_active Expired - Fee Related
- 2009-03-12 EP EP09720875A patent/EP2265601B1/de not_active Not-in-force
- 2009-03-12 CN CN200980117506.8A patent/CN102026996B/zh not_active Expired - Fee Related
- 2009-03-12 AT AT09720875T patent/ATE543811T1/de active
- 2009-03-12 WO PCT/US2009/036934 patent/WO2009114677A1/en active Application Filing
- 2009-03-12 ES ES09720875T patent/ES2380648T3/es active Active
- 2009-03-12 US US12/921,177 patent/US8324199B2/en active Active
- 2009-03-13 TW TW098108304A patent/TW200942527A/zh unknown
Also Published As
Publication number | Publication date |
---|---|
WO2009114677A1 (en) | 2009-09-17 |
CN102026996A (zh) | 2011-04-20 |
CN102026996B (zh) | 2015-01-07 |
JP5537442B2 (ja) | 2014-07-02 |
ES2380648T3 (es) | 2012-05-17 |
US8324199B2 (en) | 2012-12-04 |
EP2265601B1 (de) | 2012-02-01 |
US20110021492A1 (en) | 2011-01-27 |
TW200942527A (en) | 2009-10-16 |
EP2265601A1 (de) | 2010-12-29 |
JP2011514910A (ja) | 2011-05-12 |
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