JP2009514976A5 - - Google Patents
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- JP2009514976A5 JP2009514976A5 JP2008540190A JP2008540190A JP2009514976A5 JP 2009514976 A5 JP2009514976 A5 JP 2009514976A5 JP 2008540190 A JP2008540190 A JP 2008540190A JP 2008540190 A JP2008540190 A JP 2008540190A JP 2009514976 A5 JP2009514976 A5 JP 2009514976A5
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- JP
- Japan
- Prior art keywords
- acid
- salt
- formula
- compound
- pharmaceutical composition
- 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.)
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- 150000003839 salts Chemical class 0.000 claims 17
- 238000000034 method Methods 0.000 claims 10
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims 8
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 6
- 239000002253 acid Substances 0.000 claims 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 6
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- LCPDWSOZIOUXRV-UHFFFAOYSA-N phenoxyacetic acid Chemical compound OC(=O)COC1=CC=CC=C1 LCPDWSOZIOUXRV-UHFFFAOYSA-N 0.000 claims 6
- 208000007536 Thrombosis Diseases 0.000 claims 5
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 5
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims 4
- RGHNJXZEOKUKBD-SQOUGZDYSA-N D-gluconic acid Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-SQOUGZDYSA-N 0.000 claims 4
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 4
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 4
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims 4
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims 4
- WNLRTRBMVRJNCN-UHFFFAOYSA-N adipic acid Chemical compound OC(=O)CCCCC(O)=O WNLRTRBMVRJNCN-UHFFFAOYSA-N 0.000 claims 4
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims 4
- 239000011976 maleic acid Substances 0.000 claims 4
- 238000000634 powder X-ray diffraction Methods 0.000 claims 4
- 235000019260 propionic acid Nutrition 0.000 claims 4
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 claims 4
- 230000001732 thrombotic effect Effects 0.000 claims 4
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 3
- 239000004310 lactic acid Substances 0.000 claims 3
- 235000014655 lactic acid Nutrition 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 claims 3
- WXTMDXOMEHJXQO-UHFFFAOYSA-N 2,5-dihydroxybenzoic acid Chemical compound OC(=O)C1=CC(O)=CC=C1O WXTMDXOMEHJXQO-UHFFFAOYSA-N 0.000 claims 2
- LSPHULWDVZXLIL-UHFFFAOYSA-N Camphoric acid Natural products CC1(C)C(C(O)=O)CCC1(C)C(O)=O LSPHULWDVZXLIL-UHFFFAOYSA-N 0.000 claims 2
- 206010053567 Coagulopathies Diseases 0.000 claims 2
- RGHNJXZEOKUKBD-UHFFFAOYSA-N D-gluconic acid Natural products OCC(O)C(O)C(O)C(O)C(O)=O RGHNJXZEOKUKBD-UHFFFAOYSA-N 0.000 claims 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims 2
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 claims 2
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 2
- 206010047249 Venous thrombosis Diseases 0.000 claims 2
- 239000001361 adipic acid Substances 0.000 claims 2
- 235000011037 adipic acid Nutrition 0.000 claims 2
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims 2
- 235000010323 ascorbic acid Nutrition 0.000 claims 2
- 239000011668 ascorbic acid Substances 0.000 claims 2
- 229960005070 ascorbic acid Drugs 0.000 claims 2
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 claims 2
- LSPHULWDVZXLIL-QUBYGPBYSA-N camphoric acid Chemical compound CC1(C)[C@H](C(O)=O)CC[C@]1(C)C(O)=O LSPHULWDVZXLIL-QUBYGPBYSA-N 0.000 claims 2
- 235000015165 citric acid Nutrition 0.000 claims 2
- 238000000113 differential scanning calorimetry Methods 0.000 claims 2
- 239000000174 gluconic acid Substances 0.000 claims 2
- 235000012208 gluconic acid Nutrition 0.000 claims 2
- 229940098779 methanesulfonic acid Drugs 0.000 claims 2
- 235000011007 phosphoric acid Nutrition 0.000 claims 2
- 239000011975 tartaric acid Substances 0.000 claims 2
- 235000002906 tartaric acid Nutrition 0.000 claims 2
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 claims 1
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 206010002383 Angina Pectoris Diseases 0.000 claims 1
- 206010002388 Angina unstable Diseases 0.000 claims 1
- XDTMQSROBMDMFD-UHFFFAOYSA-N Cyclohexane Chemical compound C1CCCCC1 XDTMQSROBMDMFD-UHFFFAOYSA-N 0.000 claims 1
- 206010051055 Deep vein thrombosis Diseases 0.000 claims 1
- 206010014498 Embolic stroke Diseases 0.000 claims 1
- HTTJABKRGRZYRN-UHFFFAOYSA-N Heparin Chemical compound OC1C(NC(=O)C)C(O)OC(COS(O)(=O)=O)C1OC1C(OS(O)(=O)=O)C(O)C(OC2C(C(OS(O)(=O)=O)C(OC3C(C(O)C(O)C(O3)C(O)=O)OS(O)(=O)=O)C(CO)O2)NS(O)(=O)=O)C(C(O)=O)O1 HTTJABKRGRZYRN-UHFFFAOYSA-N 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
- 206010043647 Thrombotic Stroke Diseases 0.000 claims 1
- 201000007023 Thrombotic Thrombocytopenic Purpura Diseases 0.000 claims 1
- 208000032109 Transient ischaemic attack Diseases 0.000 claims 1
- 208000007814 Unstable Angina Diseases 0.000 claims 1
- 206010047115 Vasculitis Diseases 0.000 claims 1
- 239000003146 anticoagulant agent Substances 0.000 claims 1
- 239000000010 aprotic solvent Substances 0.000 claims 1
- SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 claims 1
- 229940092714 benzenesulfonic acid Drugs 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 208000015294 blood coagulation disease Diseases 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 230000035602 clotting Effects 0.000 claims 1
- 238000007887 coronary angioplasty Methods 0.000 claims 1
- NKDDWNXOKDWJAK-UHFFFAOYSA-N dimethoxymethane Chemical compound COCOC NKDDWNXOKDWJAK-UHFFFAOYSA-N 0.000 claims 1
- 208000009190 disseminated intravascular coagulation Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000001530 fumaric acid Substances 0.000 claims 1
- 229960005219 gentisic acid Drugs 0.000 claims 1
- 229960002897 heparin Drugs 0.000 claims 1
- 229920000669 heparin Polymers 0.000 claims 1
- 150000003840 hydrochlorides Chemical class 0.000 claims 1
- 230000006698 induction Effects 0.000 claims 1
- 238000001802 infusion Methods 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 238000009434 installation Methods 0.000 claims 1
- 201000004332 intermediate coronary syndrome Diseases 0.000 claims 1
- 239000007937 lozenge Substances 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 230000000414 obstructive effect Effects 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 239000001384 succinic acid Substances 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 206010043554 thrombocytopenia Diseases 0.000 claims 1
- 230000002537 thrombolytic effect Effects 0.000 claims 1
- 230000037317 transdermal delivery Effects 0.000 claims 1
- 201000010875 transient cerebral ischemia Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US73522405P | 2005-11-08 | 2005-11-08 | |
| US60/735,224 | 2005-11-08 | ||
| PCT/US2006/043635 WO2007056517A2 (en) | 2005-11-08 | 2006-11-07 | Pharmaceutical salts and polymorphs of n- (5-chl0r0-2-pyridinyl) -2- [ [4- [ (dimethylamino) iminomethyl] benzoyl] amino] -5-meth oxy-benzamide, a factor xa inhibitor |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012204757A Division JP5662980B2 (ja) | 2005-11-08 | 2012-09-18 | Ｎ−（５−クロロ−２−ピリジニル）−２−［［４−［（ジメチルアミノ）イミノメチル］ベンゾイル］アミノ］−５−メトキシ−ベンズアミド、第Ｘａ因子阻害剤の薬学的な塩および多形体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009514976A JP2009514976A (ja) | 2009-04-09 |
| JP2009514976A5 true JP2009514976A5 (https=) | 2009-11-05 |
| JP5227178B2 JP5227178B2 (ja) | 2013-07-03 |
Family
ID=38023988
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008540190A Expired - Fee Related JP5227178B2 (ja) | 2005-11-08 | 2006-11-07 | Ｎ−（５−クロロ−２−ピリジニル）−２−［［４−［（ジメチルアミノ）イミノメチル］ベンゾイル］アミノ］−５−メトキシ−ベンズアミド、第Ｘａ因子阻害剤の薬学的な塩および多形体 |
| JP2012204757A Active JP5662980B2 (ja) | 2005-11-08 | 2012-09-18 | Ｎ−（５−クロロ−２−ピリジニル）−２−［［４−［（ジメチルアミノ）イミノメチル］ベンゾイル］アミノ］−５−メトキシ−ベンズアミド、第Ｘａ因子阻害剤の薬学的な塩および多形体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012204757A Active JP5662980B2 (ja) | 2005-11-08 | 2012-09-18 | Ｎ−（５−クロロ−２−ピリジニル）−２−［［４−［（ジメチルアミノ）イミノメチル］ベンゾイル］アミノ］−５−メトキシ−ベンズアミド、第Ｘａ因子阻害剤の薬学的な塩および多形体 |
Country Status (20)
| Country | Link |
|---|---|
| US (7) | US7598276B2 (https=) |
| EP (2) | EP1948608B1 (https=) |
| JP (2) | JP5227178B2 (https=) |
| KR (1) | KR101358574B1 (https=) |
| CN (2) | CN101304971B (https=) |
| AR (2) | AR056787A1 (https=) |
| AT (1) | ATE549317T1 (https=) |
| AU (1) | AU2006311544B2 (https=) |
| BR (1) | BRPI0618362A2 (https=) |
| CA (1) | CA2627086C (https=) |
| DK (1) | DK1948608T3 (https=) |
| ES (1) | ES2384116T3 (https=) |
| IL (2) | IL190524A (https=) |
| NZ (2) | NZ592533A (https=) |
| PE (2) | PE20070717A1 (https=) |
| PT (1) | PT1948608E (https=) |
| RU (1) | RU2440986C2 (https=) |
| TW (1) | TWI443088B (https=) |
| WO (1) | WO2007056517A2 (https=) |
| ZA (1) | ZA200803820B (https=) |
Families Citing this family (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001064642A2 (en) * | 2000-02-29 | 2001-09-07 | Cor Therapeutics, Inc. | Benzamides and related inhibitors of factor xa |
| KR101195801B1 (ko) | 2004-06-18 | 2012-11-05 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | Ｘａ 인자 억제제 |
| US7696352B2 (en) * | 2004-06-18 | 2010-04-13 | Millennium Pharmaceuticals, Inc. | Factor Xa inhibitors |
| PE20070717A1 (es) * | 2005-11-08 | 2007-08-17 | Millennium Pharm Inc | Sal de maleato y polimorfo de [2-({4-[(dimetilamino)iminometil]fenil}carbonilamino)-5-metoxifenil]-n-(5-cloro-(2-piridil))carboxamida |
| US20090186810A1 (en) * | 2006-03-27 | 2009-07-23 | Portola Pharmaceuticals, Inc. | Potassium channel modulators and platelet procoagulant activity |
| NZ572418A (en) * | 2006-05-05 | 2011-08-26 | Millennium Pharm Inc | Factor xa inhibitors |
| CN101595092B (zh) | 2006-11-02 | 2012-02-01 | 米伦纽姆医药公司 | 合成因子xa抑制剂的医药盐的方法 |
| KR101472765B1 (ko) * | 2006-12-08 | 2014-12-15 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | 경구용 Ｘａ 인자 억제제를 포함하는 단위 용량 제형 및 경구용 Ｘａ 인자 억제제를 사용하는 혈전증의 치료 방법 |
| WO2008086226A2 (en) * | 2007-01-05 | 2008-07-17 | Millennium Pharmaceuticals, Inc. | Factor xa inhibitors |
| CL2008000070A1 (es) * | 2007-01-17 | 2008-07-25 | Lg Life Sciences Ltd | Monosal del acido maleico (3-[({1-[(2-amino-9h-purin-9-il)metil]ciclopropil}oxi)metil]-8,8-dimetil-3,7-dioxo-2,4,6-trioxa-3 lambda 5-fosfanon-1-il-pivalato; composicion farmaceutica que comprende a dicha monosal; y uso para el tratamiento del virus h |
| EA020531B1 (ru) | 2007-04-13 | 2014-11-28 | Милленниум Фармасьютикалз, Инк. | КОМБИНИРОВАННАЯ ТЕРАПИЯ АНТИКОАГУЛИРУЮЩЕГО СРЕДСТВА С СОЕДИНЕНИЕМ, КОТОРОЕ ДЕЙСТВУЕТ КАК ИНГИБИТОР ФАКТОРА Ха |
| KR101509829B1 (ko) | 2007-05-02 | 2015-04-06 | 포톨라 파마슈티컬스, 인코포레이티드 | 혈소판 ａｄｐ 수용체 억제제로 작용하는 화합물을 이용한 병용요법 |
| EP2915564B1 (en) | 2007-09-28 | 2020-11-04 | Portola Pharmaceuticals, Inc. | Antidotes for factor XA inhibitors and methods of using the same |
| PE20091156A1 (es) * | 2007-12-17 | 2009-09-03 | Astrazeneca Ab | Sales de (3-{[[3-(6-amino-2-butoxi-8-oxo-7,8-dihidro-9h-purin-9-il)propil](3-morfolin-4-ilpropil)amino]metil}fenil)acetato de metilo |
| MX2011004907A (es) | 2008-11-14 | 2011-07-29 | Portola Pharm Inc | Antidotos para inhibidores del factor xa y metodos para el uso de los mismos en combinacion con agentes de coagulacion de sangre. |
| EP3121271B1 (en) | 2009-03-30 | 2019-07-24 | Portola Pharmaceuticals, Inc. | Antidotes for factor xa inhibitors and methods of using the same |
| ES2605801T3 (es) * | 2009-07-15 | 2017-03-16 | Portola Pharmaceuticals, Inc. | Formulación de dosis unitaria de antídoto para inhibidores del factor Xa para su uso en la prevención de la hemorragia |
| CN102762550B (zh) * | 2009-12-17 | 2015-04-01 | 米伦纽姆医药公司 | Xa因子抑制剂的盐和结晶形式 |
| AR079491A1 (es) * | 2009-12-17 | 2012-02-01 | Millennium Pharm Inc | Metodos de sintesis de inhibidores del factor xa tal como el betrixaban y composiciones farmaceuticas que contienen la base libre de betrixaban o su sal sustancialmente pura. |
| US8742120B2 (en) * | 2009-12-17 | 2014-06-03 | Millennium Pharmaceuticals, Inc. | Methods of preparing factor xa inhibitors and salts thereof |
| EA015918B1 (ru) * | 2010-03-03 | 2011-12-30 | Дмитрий Геннадьевич ТОВБИН | УРЕТАНЫ, МОЧЕВИНЫ, АМИДЫ И РОДСТВЕННЫЕ ИНГИБИТОРЫ ФАКТОРА Xa |
| AR082803A1 (es) | 2010-09-01 | 2013-01-09 | Portola Pharm Inc | Metodos y formulaciones para el tratamiento de la trombosis con betrixaban y un inhibidor de la glicoproteina p |
| AR082804A1 (es) * | 2010-09-01 | 2013-01-09 | Portola Pharm Inc | Formas cristalinas de un inhibidor del factor xa |
| CN102952138B (zh) * | 2011-08-17 | 2016-07-06 | 上海特化医药科技有限公司 | 一种吡唑并嘧啶酮化合物的盐、多晶型物及其药物组合物、制备方法和应用 |
| US20150224091A1 (en) | 2011-08-31 | 2015-08-13 | Portola Pharmaceuticals, Inc. | Prevention and treatment of thrombosis in medically ill patients |
| US20140346397A1 (en) | 2012-12-27 | 2014-11-27 | Portola Pharmaceuticals, Inc. | Compounds and methods for purification of serine proteases |
| US9200268B2 (en) | 2012-12-27 | 2015-12-01 | Portola Pharmaceuticals, Inc. | Compounds and methods for purification of serine proteases |
| CN104341343B (zh) * | 2013-07-24 | 2018-09-28 | 四川海思科制药有限公司 | 贝曲西班的晶型及其制备方法和用途 |
| CN105085387A (zh) * | 2014-05-20 | 2015-11-25 | 四川海思科制药有限公司 | 贝曲西班盐及其制备方法和用途 |
| EP3750556A1 (en) | 2014-08-20 | 2020-12-16 | Portola Pharmaceuticals, Inc. | Lyophilized formulations for factor xa antidote |
| WO2017091757A1 (en) | 2015-11-24 | 2017-06-01 | Portola Pharmaceuticals, Inc. | Isotopically enriched betrixaban |
| CN106995405A (zh) * | 2016-01-25 | 2017-08-01 | 重庆医药工业研究院有限责任公司 | 一种贝曲西班马来酸盐无定型物及其制备方法 |
| WO2017147522A1 (en) | 2016-02-24 | 2017-08-31 | Portola Pharmaceuticals, Inc. | Lyophilized formulations for factor xa antidote |
| US20190300483A1 (en) * | 2016-06-02 | 2019-10-03 | Dr. Reddy's Laboratories Limited | POLYMORPHS OF BETRlXABAN & ITS MALEATE SALT |
| EP3254674A1 (en) | 2016-06-08 | 2017-12-13 | Sandoz Ag | Pharmaceutical compositions of betrixaban maleate |
| PT3472314T (pt) | 2016-06-17 | 2021-06-18 | Alexion Pharma Inc | Preparação de derivados do fator xa |
| WO2018042320A1 (en) * | 2016-08-30 | 2018-03-08 | Dr. Reddy’S Laboratories Limited | Salts of betrixaban and processes for preparation thereof |
| EP3293174A1 (en) * | 2016-09-09 | 2018-03-14 | Sandoz Ag | Crystalline salts of betrixaban |
| WO2018069936A1 (en) | 2016-10-13 | 2018-04-19 | Mylan Laboratories Limited | Polymorphs and solid dispersion of betrixaban and methods for the preparation thereof |
| CN108017576B (zh) * | 2016-11-01 | 2022-06-21 | 石药集团中奇制药技术（石家庄）有限公司 | 一种贝曲西班及其盐酸盐的制备方法，以及它们的晶型 |
| CN108586325A (zh) * | 2017-03-16 | 2018-09-28 | 上海度德医药科技有限公司 | 一种Betrixaban中间体的制备方法 |
| WO2018229796A2 (en) * | 2017-06-14 | 2018-12-20 | Mylan Laboratories Limited | A process for betrixaban hydrochloride and betrixaban maleate salt |
| CN107868039A (zh) * | 2017-11-27 | 2018-04-03 | 中国药科大学 | 一种贝曲沙班中间体n－（5－氯－2－吡啶基）－2－［（4－氰基苯甲酰基）氨基］－5－甲氧基苯甲酰胺的制备方法 |
| WO2022211680A1 (ru) * | 2021-03-30 | 2022-10-06 | Общество С Ограниченной Ответственностью "Фармадиол" | Способ получения антикоагулянта n-(5-хлорпиридин-2-ил)-2-({4-[этан-имидоил(метил)амино]бензоил}амино)-5-метилбензамид гидрохлорида |
| CN115057854A (zh) * | 2022-04-19 | 2022-09-16 | 河北常山生化药业股份有限公司 | 马来酸阿伐曲泊帕中间体的制备方法 |
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| JPH08504769A (ja) | 1992-12-15 | 1996-05-21 | コルバス・インターナショナル、インコーポレイテッド | 因子Ｘａの新規インヒビター |
| GB9226238D0 (en) | 1992-12-16 | 1993-02-10 | Scherer Ltd R P | Encapsulation apparatus and process |
| ES2193202T3 (es) | 1994-12-02 | 2003-11-01 | Yamanouchi Pharma Co Ltd | Nuevo derivado de amidinonaftilo o sal de este. |
| US5849759A (en) | 1995-12-08 | 1998-12-15 | Berlex Laboratories, Inc. | Naphthyl-substituted benzimidazole derivatives as anti-coagulants |
| AU730224B2 (en) | 1996-12-23 | 2001-03-01 | Du Pont Pharmaceuticals Company | Nitrogen containing heteroaromatics as factor Xa inhibitors |
| KR20010023364A (ko) | 1997-08-27 | 2001-03-26 | 간자와 무츠와 | 3-아미디노아닐린 유도체, 활성화 혈액응고 제 ｘ 인자저해제 및 그것의 제조중간체 |
| US6140351A (en) * | 1997-12-19 | 2000-10-31 | Berlex Laboratories, Inc. | Ortho-anthranilamide derivatives as anti-coagulants |
| US6844367B1 (en) | 1999-09-17 | 2005-01-18 | Millennium Pharmaceuticals, Inc. | Benzamides and related inhibitors of factor Xa |
| ES2316383T3 (es) * | 1999-09-17 | 2009-04-16 | Millennium Pharmaceuticals, Inc. | Benzamidas e inhibidores relacionados del factor xa. |
| WO2001064642A2 (en) * | 2000-02-29 | 2001-09-07 | Cor Therapeutics, Inc. | Benzamides and related inhibitors of factor xa |
| US6627646B2 (en) * | 2001-07-17 | 2003-09-30 | Sepracor Inc. | Norastemizole polymorphs |
| PE20070717A1 (es) | 2005-11-08 | 2007-08-17 | Millennium Pharm Inc | Sal de maleato y polimorfo de [2-({4-[(dimetilamino)iminometil]fenil}carbonilamino)-5-metoxifenil]-n-(5-cloro-(2-piridil))carboxamida |
| CN101595092B (zh) | 2006-11-02 | 2012-02-01 | 米伦纽姆医药公司 | 合成因子xa抑制剂的医药盐的方法 |
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