JP2015533168A5 - - Google Patents
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- Publication number
- JP2015533168A5 JP2015533168A5 JP2015536906A JP2015536906A JP2015533168A5 JP 2015533168 A5 JP2015533168 A5 JP 2015533168A5 JP 2015536906 A JP2015536906 A JP 2015536906A JP 2015536906 A JP2015536906 A JP 2015536906A JP 2015533168 A5 JP2015533168 A5 JP 2015533168A5
- Authority
- JP
- Japan
- Prior art keywords
- oxopiperazin
- tetrahydroisoquinoline
- tetrazol
- acryloyl
- carboxamide
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 208000035475 disorder Diseases 0.000 claims 6
- 238000000634 powder X-ray diffraction Methods 0.000 claims 6
- 230000009424 thromboembolic effect Effects 0.000 claims 6
- 239000005711 Benzoic acid Substances 0.000 claims 5
- 235000010233 benzoic acid Nutrition 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- WLYWXDYDKXCXKT-UHFFFAOYSA-N 2-[3-[3-chloro-2-fluoro-6-(tetrazol-1-yl)phenyl]prop-2-enoyl]-5-(4-methyl-2-oxopiperazin-1-yl)-3,4-dihydro-1H-isoquinoline-1-carboxamide Chemical group ClC=1C(=C(C(=CC=1)N1N=NN=C1)C=CC(=O)N1C(C2=CC=CC(=C2CC1)N1C(CN(CC1)C)=O)C(=O)N)F WLYWXDYDKXCXKT-UHFFFAOYSA-N 0.000 claims 4
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- 239000013078 crystal Substances 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- -1 3- (3-chloro-2-fluoro-6- (1H-tetrazol-1-yl) phenyl) acryloyl Chemical group 0.000 claims 2
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 2
- 208000007536 Thrombosis Diseases 0.000 claims 2
- 206010047249 Venous thrombosis Diseases 0.000 claims 2
- 230000002526 effect on cardiovascular system Effects 0.000 claims 2
- 208000010125 myocardial infarction Diseases 0.000 claims 2
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 206010002388 Angina unstable Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010003658 Atrial Fibrillation Diseases 0.000 claims 1
- 206010008088 Cerebral artery embolism Diseases 0.000 claims 1
- 206010008092 Cerebral artery thrombosis Diseases 0.000 claims 1
- 206010011091 Coronary artery thrombosis Diseases 0.000 claims 1
- 206010051055 Deep vein thrombosis Diseases 0.000 claims 1
- 206010014513 Embolism arterial Diseases 0.000 claims 1
- 208000032382 Ischaemic stroke Diseases 0.000 claims 1
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims 1
- 208000010378 Pulmonary Embolism Diseases 0.000 claims 1
- 206010063544 Renal embolism Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000007814 Unstable Angina Diseases 0.000 claims 1
- 239000002473 artificial blood Substances 0.000 claims 1
- DKPFZGUDAPQIHT-UHFFFAOYSA-N butyl acetate Chemical compound CCCCOC(C)=O DKPFZGUDAPQIHT-UHFFFAOYSA-N 0.000 claims 1
- 230000002612 cardiopulmonary effect Effects 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 208000002528 coronary thrombosis Diseases 0.000 claims 1
- 235000019439 ethyl acetate Nutrition 0.000 claims 1
- 238000001631 haemodialysis Methods 0.000 claims 1
- 230000000322 hemodialysis Effects 0.000 claims 1
- 239000007943 implant Substances 0.000 claims 1
- 201000004332 intermediate coronary syndrome Diseases 0.000 claims 1
- 201000010849 intracranial embolism Diseases 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- 230000000306 recurrent effect Effects 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 201000005060 thrombophlebitis Diseases 0.000 claims 1
- 230000001052 transient effect Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261712850P | 2012-10-12 | 2012-10-12 | |
| US61/712,850 | 2012-10-12 | ||
| PCT/US2013/064423 WO2014059203A1 (en) | 2012-10-12 | 2013-10-11 | Crystalline forms of a factor xia inhibitor |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015533168A JP2015533168A (ja) | 2015-11-19 |
| JP2015533168A5 true JP2015533168A5 (enExample) | 2016-07-07 |
| JP6154473B2 JP6154473B2 (ja) | 2017-06-28 |
Family
ID=49474724
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015536906A Expired - Fee Related JP6154473B2 (ja) | 2012-10-12 | 2013-10-11 | 第ＸＩａ因子阻害剤の結晶形 |
Country Status (34)
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| HRP20170784T8 (hr) | 2011-10-14 | 2018-05-18 | Bristol-Myers Squibb Company | Supstituirani spojevi tetrahidroizohinolina kao inhbitori xia faktora |
| US9315519B2 (en) | 2012-10-12 | 2016-04-19 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors |
| EP2906541B1 (en) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| 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 |
| UY35971A (es) | 2014-01-31 | 2015-07-31 | Bristol Myers Squibb Company Una Corporación Del Estado De Delaware | Macrociclos con grupos p2? aromáticos como inhibidores del factor xia |
| NO2760821T3 (enExample) | 2014-01-31 | 2018-03-10 | ||
| 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 |
| ES2762987T3 (es) | 2015-06-19 | 2020-05-26 | Bristol Myers Squibb Co | Macrociclos de diamida como inhibidores del factor XIA |
| CN114874222B (zh) | 2015-07-29 | 2025-06-06 | 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 |
| 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 |
| TW201808908A (zh) | 2016-08-22 | 2018-03-16 | 美商默沙東藥廠 | 因子XIa抑制劑 |
| CN109867660A (zh) * | 2017-12-01 | 2019-06-11 | 四川科伦博泰生物医药股份有限公司 | 含季铵离子的四氢异喹啉酰胺化合物及其药物用途 |
| EP3778597B1 (en) | 2018-03-28 | 2025-05-28 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | Tetrahydroisoquinoline derivative, preparation method therefor and uses thereof |
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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 |
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| CN104507924B (zh) | 2012-08-03 | 2018-01-23 | 百时美施贵宝公司 | 二氢吡啶酮p1作为凝血因子xia抑制剂 |
| EP2906541B1 (en) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| US9315519B2 (en) | 2012-10-12 | 2016-04-19 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors |
| US9708308B2 (en) | 2012-12-19 | 2017-07-18 | Merck Sharp Dohme Corp. | Factor IXa inhibitors |
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| 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 |
-
2013
- 2013-10-11 HR HRP20180465TT patent/HRP20180465T1/hr unknown
- 2013-10-11 PT PT137802872T patent/PT2906551T/pt unknown
- 2013-10-11 PE PE2015000477A patent/PE20150639A1/es not_active Application Discontinuation
- 2013-10-11 TR TR2018/07316T patent/TR201807316T4/tr unknown
- 2013-10-11 ES ES13780287.2T patent/ES2668318T3/es active Active
- 2013-10-11 SG SG11201502605PA patent/SG11201502605PA/en unknown
- 2013-10-11 LT LTEP13780287.2T patent/LT2906551T/lt unknown
- 2013-10-11 NZ NZ707990A patent/NZ707990A/en not_active IP Right Cessation
- 2013-10-11 EA EA201590548A patent/EA032092B1/ru not_active IP Right Cessation
- 2013-10-11 AU AU2013329125A patent/AU2013329125B2/en not_active Ceased
- 2013-10-11 EP EP13780287.2A patent/EP2906551B1/en active Active
- 2013-10-11 MY MYPI2015701150A patent/MY173058A/en unknown
- 2013-10-11 PL PL13780287T patent/PL2906551T3/pl unknown
- 2013-10-11 HU HUE13780287A patent/HUE038272T2/hu unknown
- 2013-10-11 MX MX2015004328A patent/MX351848B/es active IP Right Grant
- 2013-10-11 BR BR112015007937A patent/BR112015007937A2/pt not_active Application Discontinuation
- 2013-10-11 SI SI201330987T patent/SI2906551T1/en unknown
- 2013-10-11 WO PCT/US2013/064423 patent/WO2014059203A1/en not_active Ceased
- 2013-10-11 CN CN201380064797.5A patent/CN104837833B/zh not_active Expired - Fee Related
- 2013-10-11 DK DK13780287.2T patent/DK2906551T3/en active
- 2013-10-11 US US14/434,507 patent/US9920034B2/en active Active
- 2013-10-11 CA CA2888100A patent/CA2888100A1/en not_active Abandoned
- 2013-10-11 JP JP2015536906A patent/JP6154473B2/ja not_active Expired - Fee Related
- 2013-10-11 RS RS20180328A patent/RS57039B1/sr unknown
- 2013-10-11 SM SM20180262T patent/SMT201800262T1/it unknown
- 2013-10-11 KR KR1020157011941A patent/KR102143257B1/ko not_active Expired - Fee Related
-
2014
- 2014-05-21 NO NO14169333A patent/NO2819265T3/no unknown
-
2015
- 2015-03-26 PH PH12015500678A patent/PH12015500678A1/en unknown
- 2015-04-01 IL IL238089A patent/IL238089B/en active IP Right Grant
- 2015-04-10 CL CL2015000916A patent/CL2015000916A1/es unknown
- 2015-05-07 CO CO15104857A patent/CO7350621A2/es unknown
- 2015-05-07 MA MA38071A patent/MA38071B1/fr unknown
- 2015-05-11 ZA ZA2015/03238A patent/ZA201503238B/en unknown
-
2018
- 2018-05-18 CY CY20181100522T patent/CY1120238T1/el unknown
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