JP2013514981A5 - - Google Patents
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- Publication number
- JP2013514981A5 JP2013514981A5 JP2012544856A JP2012544856A JP2013514981A5 JP 2013514981 A5 JP2013514981 A5 JP 2013514981A5 JP 2012544856 A JP2012544856 A JP 2012544856A JP 2012544856 A JP2012544856 A JP 2012544856A JP 2013514981 A5 JP2013514981 A5 JP 2013514981A5
- Authority
- JP
- Japan
- Prior art keywords
- diffraction pattern
- salt
- ray powder
- powder diffraction
- crystalline form
- 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
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- 238000000634 powder X-ray diffraction Methods 0.000 claims description 28
- 150000003839 salts Chemical class 0.000 claims description 28
- 239000013078 crystal Substances 0.000 claims description 22
- 150000001875 compounds Chemical class 0.000 claims description 17
- 238000000034 method Methods 0.000 claims description 13
- ZWEHNKRNPOVVGH-UHFFFAOYSA-N 2-Butanone Chemical compound CCC(C)=O ZWEHNKRNPOVVGH-UHFFFAOYSA-N 0.000 claims description 12
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical class CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims description 12
- 238000000113 differential scanning calorimetry Methods 0.000 claims description 12
- 239000000203 mixture Substances 0.000 claims description 9
- -1 4- (2-oxopyridin-1 (2H) -yl) phenyl Chemical group 0.000 claims description 8
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims description 8
- 239000000843 powder Substances 0.000 claims description 8
- 230000002265 prevention Effects 0.000 claims description 8
- 229910019142 PO4 Inorganic materials 0.000 claims description 6
- 208000007536 Thrombosis Diseases 0.000 claims description 6
- 239000010452 phosphate Substances 0.000 claims description 6
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 4
- JUJNQUIRRLHBSX-UHFFFAOYSA-N CS(=O)(=O)O.S1C=CC=C1C(=O)N Chemical compound CS(=O)(=O)O.S1C=CC=C1C(=O)N JUJNQUIRRLHBSX-UHFFFAOYSA-N 0.000 claims description 4
- 241000124008 Mammalia Species 0.000 claims description 4
- 208000006011 Stroke Diseases 0.000 claims description 4
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims description 4
- 238000004458 analytical method Methods 0.000 claims description 4
- 239000002904 solvent Substances 0.000 claims description 4
- 229930192474 thiophene Natural products 0.000 claims description 4
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims description 2
- 206010003178 Arterial thrombosis Diseases 0.000 claims description 2
- 206010003658 Atrial Fibrillation Diseases 0.000 claims description 2
- 206010051055 Deep vein thrombosis Diseases 0.000 claims description 2
- AVRWEULSKHQETA-UHFFFAOYSA-N Thiophene-2 Chemical compound S1C=2CCCCCC=2C(C(=O)OC)=C1NC(=O)C1=C(F)C(F)=C(F)C(F)=C1F AVRWEULSKHQETA-UHFFFAOYSA-N 0.000 claims description 2
- 206010047249 Venous thrombosis Diseases 0.000 claims description 2
- 239000008280 blood Substances 0.000 claims description 2
- 210000004369 blood Anatomy 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 239000012458 free base Substances 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 229940098779 methanesulfonic acid Drugs 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 208000010125 myocardial infarction Diseases 0.000 claims description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 2
- 230000009863 secondary prevention Effects 0.000 claims description 2
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims description 2
- DENPQNAWGQXKCU-UHFFFAOYSA-N thiophene-2-carboxamide Chemical compound NC(=O)C1=CC=CS1 DENPQNAWGQXKCU-UHFFFAOYSA-N 0.000 claims description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 2
- CHXZRHMQQRUVHF-UHFFFAOYSA-N 2-hex-5-en-1,3-diynyl-5-prop-1-ynylthiophene Chemical compound CC#CC1=CC=C(C#CC#CC=C)S1 CHXZRHMQQRUVHF-UHFFFAOYSA-N 0.000 claims 2
- 229940126062 Compound A Drugs 0.000 claims 1
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims 1
- 150000003857 carboxamides Chemical class 0.000 claims 1
- 230000015271 coagulation Effects 0.000 claims 1
- 238000005345 coagulation Methods 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 206010053567 Coagulopathies Diseases 0.000 description 1
- 230000035602 clotting Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US28768309P | 2009-12-17 | 2009-12-17 | |
| US61/287,683 | 2009-12-17 | ||
| PCT/US2010/060885 WO2011084652A2 (en) | 2009-12-17 | 2010-12-16 | Salts and crystalline forms of a factor xa inhibitor |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013514981A JP2013514981A (ja) | 2013-05-02 |
| JP2013514981A5 true JP2013514981A5 (https=) | 2014-01-30 |
| JP5796872B2 JP5796872B2 (ja) | 2015-10-21 |
Family
ID=43618959
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012544856A Expired - Fee Related JP5796872B2 (ja) | 2009-12-17 | 2010-12-16 | 第Ｘａ因子阻害剤の結晶性塩 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8530501B2 (https=) |
| EP (1) | EP2513094B1 (https=) |
| JP (1) | JP5796872B2 (https=) |
| CN (1) | CN102762550B (https=) |
| CA (1) | CA2784921A1 (https=) |
| WO (1) | WO2011084652A2 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8742120B2 (en) * | 2009-12-17 | 2014-06-03 | Millennium Pharmaceuticals, Inc. | Methods of preparing factor xa inhibitors and salts thereof |
| 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. |
| CN120633248B (zh) * | 2025-08-08 | 2025-10-17 | 成都理工大学 | 超临界地热流体体系KCl-H2O的电导率计算方法 |
Family Cites Families (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9226238D0 (en) | 1992-12-16 | 1993-02-10 | Scherer Ltd R P | Encapsulation apparatus and process |
| US6514977B1 (en) | 1997-05-22 | 2003-02-04 | G.D. Searle & Company | Substituted pyrazoles as p38 kinase inhibitors |
| CA2295620A1 (en) | 1997-08-11 | 1999-02-18 | Boehringer Ingelheim Pharmaceuticals, Inc. | 5,6-heteroaryl-dipyrido¬2,3-b:3',2'-f|azepines and their use in the prevention or treatment of hiv infection |
| GB9725244D0 (en) | 1997-11-29 | 1998-01-28 | Zeneca Ltd | Chemical compounds |
| JP2000178243A (ja) | 1998-12-14 | 2000-06-27 | Teijin Ltd | ビフェニルアミジン誘導体 |
| ES2316383T3 (es) | 1999-09-17 | 2009-04-16 | Millennium Pharmaceuticals, Inc. | Benzamidas e inhibidores relacionados del factor xa. |
| US6844367B1 (en) | 1999-09-17 | 2005-01-18 | Millennium Pharmaceuticals, Inc. | Benzamides and related inhibitors of factor Xa |
| WO2001021160A2 (en) | 1999-09-23 | 2001-03-29 | Axxima Pharmaceuticals Aktiengesellschaft | Carboxymide and aniline derivatives as selective inhibitors of pathogens |
| DE19962924A1 (de) | 1999-12-24 | 2001-07-05 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
| US6906063B2 (en) | 2000-02-04 | 2005-06-14 | Portola Pharmaceuticals, Inc. | Platelet ADP receptor inhibitors |
| WO2001064642A2 (en) | 2000-02-29 | 2001-09-07 | Cor Therapeutics, Inc. | Benzamides and related inhibitors of factor xa |
| DE10027151A1 (de) | 2000-05-31 | 2001-12-06 | Bayer Ag | Herbizide Mittel auf Basis von substituierten Carbonsäureamiden |
| AU2001273040A1 (en) | 2000-06-27 | 2002-01-08 | Du Pont Pharmaceuticals Company | Factor xa inhibitors |
| ATE368643T1 (de) | 2001-03-30 | 2007-08-15 | Millennium Pharm Inc | Faktor xa benzamidin inhibitoren |
| US7312235B2 (en) | 2001-03-30 | 2007-12-25 | Millennium Pharmaceuticals, Inc. | Benzamide inhibitors of factor Xa |
| DE10129725A1 (de) * | 2001-06-20 | 2003-01-02 | Bayer Ag | Kombinationstherapie substituierter Oxazolidinone |
| US6627646B2 (en) * | 2001-07-17 | 2003-09-30 | Sepracor Inc. | Norastemizole polymorphs |
| ES2180456B1 (es) | 2001-07-20 | 2004-05-01 | Laboratorios S.A.L.V.A.T., S.A. | Isoxazoles sustituidos y su utilizacion como antibioticos. |
| US6914058B2 (en) | 2002-01-18 | 2005-07-05 | Dr. Reddy's Laboratories, Limited | Antibacterial compounds: process for their preparation and pharmaceutical compositions containing them |
| JP4471262B2 (ja) | 2002-03-07 | 2010-06-02 | 株式会社エス・ディー・エス バイオテック | 置換イソキサゾールアルキルアミン誘導体及び農園芸用殺菌剤 |
| US20070043079A1 (en) | 2003-04-18 | 2007-02-22 | Hiromu Habashita | Heterocyclic compound containing nitrogen atom and use thereof |
| WO2004101531A1 (en) | 2003-04-29 | 2004-11-25 | Dr. Reddy's Laboratories Ltd. | Antiinfective 1,2,3-triazole derivatives, process for their preparation and pharmaceutical compositions containing them |
| DE10322469A1 (de) | 2003-05-19 | 2004-12-16 | Bayer Healthcare Ag | Heterocyclische Verbindungen |
| WO2004106329A2 (en) | 2003-06-03 | 2004-12-09 | Dr. Reddy's Laboratories Ltd. | Novel antiinfective compounds and their pharmaceutical compositions |
| US7199149B2 (en) | 2003-10-01 | 2007-04-03 | Bristol Myers Squibb Company | Monocyclic and bicyclic lactams as factor Xa inhibitors |
| US7022695B2 (en) | 2003-10-09 | 2006-04-04 | Millennium Pharmaceuticals, Inc. | Thioether-substituted benzamides as inhibitors of Factor Xa |
| WO2005035528A2 (en) | 2003-10-14 | 2005-04-21 | Dr. Reddy's Laboratories Ltd. | Triazole derivatives as antibacterial agents |
| WO2005082892A2 (en) | 2004-02-17 | 2005-09-09 | Dr. Reddy's Laboratories Ltd. | Triazole compounds as antibacterial agents and pharmaceutical compositions containing them |
| 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 |
| WO2007007588A1 (ja) | 2005-07-08 | 2007-01-18 | Ono Pharmaceutical Co., Ltd. | 平面性を有する環状基を母核とする化合物 |
| AR057976A1 (es) * | 2005-08-29 | 2008-01-09 | Boehringer Ingelheim Int | Biarilos sustituidos y su uso como medicamentos. |
| PT1951254E (pt) | 2005-11-03 | 2012-04-12 | Portola Pharm Inc | [4-(6-halo-7-substituído-2,4-dioxo-1,4-di-hidro-2hquinazolin- 3-il)-fenil]-5-cloro-tiofen-2-il-sulfonilureias e formas e métodos relacionados com as mesmas |
| 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 |
| DE102006025314A1 (de) | 2006-05-31 | 2007-12-06 | Bayer Healthcare Ag | Arylsubstituierte Heterozyklen und ihre Verwendung |
| US20080051578A1 (en) | 2006-08-24 | 2008-02-28 | Georg Dahmann | Substituted biaryls, process for their manufacture and use thereof as medicaments |
| 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 |
| WO2008121721A2 (en) | 2007-03-28 | 2008-10-09 | Portola Pharmaceuticals, Inc. | Targeted delivery and expression of procoagulant hemostatic activity |
| 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 |
| 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 |
-
2010
- 2010-12-16 CN CN201080064120.8A patent/CN102762550B/zh not_active Expired - Fee Related
- 2010-12-16 EP EP10801041.4A patent/EP2513094B1/en not_active Not-in-force
- 2010-12-16 JP JP2012544856A patent/JP5796872B2/ja not_active Expired - Fee Related
- 2010-12-16 US US12/970,785 patent/US8530501B2/en not_active Expired - Fee Related
- 2010-12-16 CA CA2784921A patent/CA2784921A1/en not_active Abandoned
- 2010-12-16 WO PCT/US2010/060885 patent/WO2011084652A2/en not_active Ceased
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