JP2010526105A5 - - Google Patents
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- JP2010526105A5 JP2010526105A5 JP2010506707A JP2010506707A JP2010526105A5 JP 2010526105 A5 JP2010526105 A5 JP 2010526105A5 JP 2010506707 A JP2010506707 A JP 2010506707A JP 2010506707 A JP2010506707 A JP 2010506707A JP 2010526105 A5 JP2010526105 A5 JP 2010526105A5
- Authority
- JP
- Japan
- Prior art keywords
- salt
- pharmaceutical composition
- solid form
- crystalline solid
- diffraction pattern
- 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.)
- Withdrawn
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- 150000003839 salts Chemical class 0.000 claims description 42
- 239000003814 drug Substances 0.000 claims description 13
- 229940079593 drug Drugs 0.000 claims description 3
- 239000007787 solid Substances 0.000 claims 20
- 239000008194 pharmaceutical composition Substances 0.000 claims 16
- 238000000634 powder X-ray diffraction Methods 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 13
- 150000002500 ions Chemical class 0.000 claims 9
- 239000000203 mixture Substances 0.000 claims 9
- 208000007536 Thrombosis Diseases 0.000 claims 8
- 238000000034 method Methods 0.000 claims 7
- 229940124597 therapeutic agent Drugs 0.000 claims 7
- 241000124008 Mammalia Species 0.000 claims 6
- 208000007814 Unstable Angina Diseases 0.000 claims 6
- 206010002388 Angina unstable Diseases 0.000 claims 5
- 208000018262 Peripheral vascular disease Diseases 0.000 claims 5
- 206010000891 acute myocardial infarction Diseases 0.000 claims 5
- 201000004332 intermediate coronary syndrome Diseases 0.000 claims 5
- 208000007718 Stable Angina Diseases 0.000 claims 4
- 208000006011 Stroke Diseases 0.000 claims 4
- 239000003146 anticoagulant agent Substances 0.000 claims 4
- 238000013172 carotid endarterectomy Methods 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 208000037803 restenosis Diseases 0.000 claims 4
- 230000002792 vascular Effects 0.000 claims 4
- 206010051055 Deep vein thrombosis Diseases 0.000 claims 3
- 208000005189 Embolism Diseases 0.000 claims 3
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000007023 Thrombotic Thrombocytopenic Purpura Diseases 0.000 claims 3
- 208000032109 Transient ischaemic attack Diseases 0.000 claims 3
- 206010047249 Venous thrombosis Diseases 0.000 claims 3
- 230000033115 angiogenesis Effects 0.000 claims 3
- 239000002775 capsule Substances 0.000 claims 3
- 230000015271 coagulation Effects 0.000 claims 3
- 238000005345 coagulation Methods 0.000 claims 3
- 210000004351 coronary vessel Anatomy 0.000 claims 3
- 239000003112 inhibitor Substances 0.000 claims 3
- 238000003780 insertion Methods 0.000 claims 3
- 230000037431 insertion Effects 0.000 claims 3
- 230000000302 ischemic effect Effects 0.000 claims 3
- 239000007937 lozenge Substances 0.000 claims 3
- 238000013146 percutaneous coronary intervention Methods 0.000 claims 3
- 201000011461 pre-eclampsia Diseases 0.000 claims 3
- 208000010110 spontaneous platelet aggregation Diseases 0.000 claims 3
- 208000011580 syndromic disease Diseases 0.000 claims 3
- 239000003826 tablet Substances 0.000 claims 3
- 201000005665 thrombophilia Diseases 0.000 claims 3
- 201000010875 transient cerebral ischemia Diseases 0.000 claims 3
- IKXCHOUDIPZROZ-LXGUWJNJSA-N (2r,3r,4r,5s)-6-(ethylamino)hexane-1,2,3,4,5-pentol Chemical compound CCNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO IKXCHOUDIPZROZ-LXGUWJNJSA-N 0.000 claims 2
- QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 claims 2
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- ODKSFYDXXFIFQN-BYPYZUCNSA-N L-arginine Chemical compound OC(=O)[C@@H](N)CCCN=C(N)N ODKSFYDXXFIFQN-BYPYZUCNSA-N 0.000 claims 2
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims 2
- MBBZMMPHUWSWHV-BDVNFPICSA-N N-methylglucamine Chemical compound CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO MBBZMMPHUWSWHV-BDVNFPICSA-N 0.000 claims 2
- 238000002399 angioplasty Methods 0.000 claims 2
- 230000003110 anti-inflammatory effect Effects 0.000 claims 2
- 230000000702 anti-platelet effect Effects 0.000 claims 2
- 229940127219 anticoagulant drug Drugs 0.000 claims 2
- 239000008280 blood Substances 0.000 claims 2
- 210000004369 blood Anatomy 0.000 claims 2
- 229910052791 calcium Inorganic materials 0.000 claims 2
- 239000011575 calcium Substances 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 208000029078 coronary artery disease Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 229910052749 magnesium Inorganic materials 0.000 claims 2
- 239000011777 magnesium Substances 0.000 claims 2
- 239000000843 powder Substances 0.000 claims 2
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 claims 2
- 230000001052 transient effect Effects 0.000 claims 2
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 claims 2
- 229960000281 trometamol Drugs 0.000 claims 2
- 239000003981 vehicle Substances 0.000 claims 2
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 claims 1
- 208000034826 Genetic Predisposition to Disease 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
- 206010022562 Intermittent claudication Diseases 0.000 claims 1
- 208000033463 Ischaemic neuropathy Diseases 0.000 claims 1
- 208000032382 Ischaemic stroke Diseases 0.000 claims 1
- 235000019766 L-Lysine Nutrition 0.000 claims 1
- 229930064664 L-arginine Natural products 0.000 claims 1
- 235000014852 L-arginine Nutrition 0.000 claims 1
- 239000004472 Lysine Substances 0.000 claims 1
- 229910002651 NO3 Inorganic materials 0.000 claims 1
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 claims 1
- SNIOPGDIGTZGOP-UHFFFAOYSA-N Nitroglycerin Chemical compound [O-][N+](=O)OCC(O[N+]([O-])=O)CO[N+]([O-])=O SNIOPGDIGTZGOP-UHFFFAOYSA-N 0.000 claims 1
- 239000000006 Nitroglycerin Substances 0.000 claims 1
- 102100037600 P2Y purinoceptor 1 Human genes 0.000 claims 1
- 108010085249 Purinergic P2 Receptors Proteins 0.000 claims 1
- 206010038563 Reocclusion Diseases 0.000 claims 1
- 101000712605 Theromyzon tessulatum Theromin Proteins 0.000 claims 1
- 229940122388 Thrombin inhibitor Drugs 0.000 claims 1
- 206010043647 Thrombotic Stroke Diseases 0.000 claims 1
- 229940123987 Thromboxane A2 receptor antagonist Drugs 0.000 claims 1
- WLMZTKAZJUWXCB-KQYNXXCUSA-N [(2r,3s,4r,5r)-5-(6-amino-2-methylsulfanylpurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl phosphono hydrogen phosphate Chemical compound C12=NC(SC)=NC(N)=C2N=CN1[C@@H]1O[C@H](COP(O)(=O)OP(O)(O)=O)[C@@H](O)[C@H]1O WLMZTKAZJUWXCB-KQYNXXCUSA-N 0.000 claims 1
- 229960001138 acetylsalicylic acid Drugs 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 239000000443 aerosol Substances 0.000 claims 1
- 238000004220 aggregation Methods 0.000 claims 1
- 230000002776 aggregation Effects 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 239000003529 anticholesteremic agent Substances 0.000 claims 1
- 229940127226 anticholesterol agent Drugs 0.000 claims 1
- 239000002220 antihypertensive agent Substances 0.000 claims 1
- 229940030600 antihypertensive agent Drugs 0.000 claims 1
- 210000001367 artery Anatomy 0.000 claims 1
- 230000002490 cerebral effect Effects 0.000 claims 1
- 229940072645 coumadin Drugs 0.000 claims 1
- 239000003255 cyclooxygenase 2 inhibitor Substances 0.000 claims 1
- 230000001419 dependent effect Effects 0.000 claims 1
- 208000009190 disseminated intravascular coagulation Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000003527 fibrinolytic agent Substances 0.000 claims 1
- 229960003711 glyceryl trinitrate Drugs 0.000 claims 1
- 229960002897 heparin Drugs 0.000 claims 1
- 229920000669 heparin Polymers 0.000 claims 1
- 238000000338 in vitro Methods 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
- 208000021156 intermittent vascular claudication Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims 1
- 238000007911 parenteral administration Methods 0.000 claims 1
- 230000007170 pathology Effects 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- 239000002570 phosphodiesterase III inhibitor Substances 0.000 claims 1
- 229940126409 proton pump inhibitor Drugs 0.000 claims 1
- 239000000612 proton pump inhibitor Substances 0.000 claims 1
- 230000002441 reversible effect Effects 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 229940076279 serotonin Drugs 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- 239000003868 thrombin inhibitor Substances 0.000 claims 1
- 239000003769 thromboxane A2 receptor blocking agent Substances 0.000 claims 1
- 238000011200 topical administration Methods 0.000 claims 1
- 230000037317 transdermal delivery Effects 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
- PJVWKTKQMONHTI-UHFFFAOYSA-N warfarin Chemical compound OC=1C2=CC=CC=C2OC(=O)C=1C(CC(=O)C)C1=CC=CC=C1 PJVWKTKQMONHTI-UHFFFAOYSA-N 0.000 claims 1
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical group [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 3
- 159000000000 sodium salts Chemical class 0.000 description 2
- QHFUNOSLYOQGKO-UHFFFAOYSA-N 1-(5-chlorothiophen-2-yl)sulfonyl-1-[4-[6-fluoro-7-(methylamino)-2,4-dioxo-1h-quinazolin-3-yl]phenyl]urea;potassium Chemical compound [K].O=C1C=2C=C(F)C(NC)=CC=2NC(=O)N1C(C=C1)=CC=C1N(C(N)=O)S(=O)(=O)C1=CC=C(Cl)S1 QHFUNOSLYOQGKO-UHFFFAOYSA-N 0.000 description 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 238000013112 stability test Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US92732807P | 2007-05-02 | 2007-05-02 | |
| PCT/US2008/062584 WO2008137809A2 (en) | 2007-05-02 | 2008-05-02 | [4-(6-fluoro-7-methylamino-2,4-dioxo-1,4-dihydro-2h-quinazolin-3-yl)-phenyl] -5-chloro-thiophen-2-yl-sulfonylurea salts, in different crystalline forms, pharmaceutical compositions thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010526105A JP2010526105A (ja) | 2010-07-29 |
| JP2010526105A5 true JP2010526105A5 (https=) | 2011-07-14 |
Family
ID=39651344
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010506707A Withdrawn JP2010526105A (ja) | 2007-05-02 | 2008-05-02 | ［４−（６−フルオロ−７−メチルアミノ−２，４−ジオキソ−１，４−ジヒドロ−２ｈ−キナゾリン−３−イル）−フェニル］−５−クロロ−チオフェン−２−イル−スルホニルウレア塩、異なる結晶形態、その医薬組成物 |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US20090042916A1 (https=) |
| EP (1) | EP2076510A2 (https=) |
| JP (1) | JP2010526105A (https=) |
| KR (1) | KR20100020455A (https=) |
| CN (1) | CN101720324A (https=) |
| AU (1) | AU2008247457A1 (https=) |
| BR (1) | BRPI0810800A2 (https=) |
| CA (1) | CA2686221A1 (https=) |
| CO (1) | CO6241155A2 (https=) |
| EA (1) | EA200901474A1 (https=) |
| EC (1) | ECSP099779A (https=) |
| GT (1) | GT200900282A (https=) |
| IL (1) | IL201829A0 (https=) |
| MA (1) | MA31397B1 (https=) |
| MX (1) | MX2009011836A (https=) |
| TN (1) | TN2009000452A1 (https=) |
| WO (1) | WO2008137809A2 (https=) |
| ZA (1) | ZA200907493B (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US20090156620A1 (en) * | 2007-05-02 | 2009-06-18 | Portola Pharmaceuticals, Inc. | [4-(6-fluoro-7-methylamino-2,4-dioxo-1,4-dihydro-2h-quinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylurea salts, forms and methods related thereto |
| WO2011006169A1 (en) | 2009-07-10 | 2011-01-13 | Portola Pharmaceuticals, Inc. | Methods for diagnosis and treatment of thrombotic disorders mediated by cyp2c19*2 |
| US20130165459A1 (en) * | 2010-01-12 | 2013-06-27 | Norvartis Pharma Ag | Pharmaceutical composition and dosage forms of elinogrel and methods of use thereof |
| WO2011137459A1 (en) | 2010-04-30 | 2011-11-03 | Portola Pharmaceuticals, Inc. | Dosage forms of elinogrel and methods of injectable administration thereof |
| JP2013544271A (ja) * | 2010-12-03 | 2013-12-12 | ポートラ ファーマシューティカルズ， インコーポレイテッド | 式（ｉ）の化合物の薬学的組成物、投薬形態、および新規の形態、ならびにその使用方法 |
| CN106777526B (zh) * | 2016-11-25 | 2020-05-01 | 江苏大学 | 基于遗传算法的高温高压离心式叶轮多学科优化方法 |
| WO2019126557A1 (en) | 2017-12-22 | 2019-06-27 | Aesthetics Biomedical, Inc. | Biologic preserving composition and methods of use |
| US10933096B2 (en) | 2017-12-22 | 2021-03-02 | Aesthetics Biomedical, Inc. | Biologic preserving composition and methods of use |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3847925A (en) * | 1971-07-15 | 1974-11-12 | En Nom Collectif Science Et Ci | Benzenesulfonyl semicarbazides |
| DE3134780A1 (de) * | 1981-09-02 | 1983-03-10 | Hoechst Ag, 6000 Frankfurt | "sulfonylharnstoffe, verfahren zu ihrer herstellung, pharmazeutische praeparate auf basis dieser verbindungen und ihre verwendung" |
| US4720450A (en) * | 1985-06-03 | 1988-01-19 | Polaroid Corporation | Thermal imaging method |
| US5314902A (en) * | 1993-01-27 | 1994-05-24 | Monsanto Company | Urea derivatives useful as platelet aggregation inhibitors |
| US6160000A (en) * | 1996-12-23 | 2000-12-12 | Merck & Co., Inc. | Antidiabetic agents based on aryl and heteroarylacetic acids |
| US6906063B2 (en) * | 2000-02-04 | 2005-06-14 | Portola Pharmaceuticals, Inc. | Platelet ADP receptor inhibitors |
| WO2001057037A1 (en) * | 2000-02-04 | 2001-08-09 | Cor Therapeutics, Inc. | Platelet adp receptor inhibitors |
| JP4564713B2 (ja) * | 2000-11-01 | 2010-10-20 | ミレニアム・ファーマシューティカルズ・インコーポレイテッド | 窒素性複素環式化合物、ならびに窒素性複素環式化合物およびその中間体を作製するための方法 |
| JP2005523249A (ja) * | 2002-01-09 | 2005-08-04 | エンズレル インコーポレイテッド | 多環式芳香族抗酸化剤または抗炎症化合物のリポソーム薬物配達 |
| US20040242658A1 (en) * | 2003-01-08 | 2004-12-02 | Dr. Reddy's Laboratories Limited | Amorphous form of rosiglitazone maleate and process for preparation thereof |
| ES2334795T3 (es) * | 2003-10-03 | 2010-03-16 | Portola Pharmaceuticals, Inc. | Sulfonilureas 2,4-dioxo-3-quinazolinilarilo. |
| 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 |
| CA2686203A1 (en) * | 2007-05-02 | 2008-11-13 | Portola Pharmaceuticals, Inc. | Intravenous and oral dosing of a direct-acting and reversible p2y12 inhibitor |
| US20090156620A1 (en) * | 2007-05-02 | 2009-06-18 | Portola Pharmaceuticals, Inc. | [4-(6-fluoro-7-methylamino-2,4-dioxo-1,4-dihydro-2h-quinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylurea salts, forms and methods related thereto |
-
2008
- 2008-05-02 WO PCT/US2008/062584 patent/WO2008137809A2/en not_active Ceased
- 2008-05-02 BR BRPI0810800-5A2A patent/BRPI0810800A2/pt not_active IP Right Cessation
- 2008-05-02 JP JP2010506707A patent/JP2010526105A/ja not_active Withdrawn
- 2008-05-02 AU AU2008247457A patent/AU2008247457A1/en not_active Abandoned
- 2008-05-02 KR KR1020097025052A patent/KR20100020455A/ko not_active Withdrawn
- 2008-05-02 CA CA002686221A patent/CA2686221A1/en not_active Abandoned
- 2008-05-02 EA EA200901474A patent/EA200901474A1/ru unknown
- 2008-05-02 MX MX2009011836A patent/MX2009011836A/es not_active Application Discontinuation
- 2008-05-02 US US12/114,742 patent/US20090042916A1/en not_active Abandoned
- 2008-05-02 EP EP08747609A patent/EP2076510A2/en not_active Withdrawn
- 2008-05-02 CN CN200880022604A patent/CN101720324A/zh active Pending
-
2009
- 2009-10-26 ZA ZA200907493A patent/ZA200907493B/xx unknown
- 2009-10-29 IL IL201829A patent/IL201829A0/en unknown
- 2009-10-30 TN TNP2009000452A patent/TN2009000452A1/fr unknown
- 2009-10-30 GT GT200900282A patent/GT200900282A/es unknown
- 2009-11-20 CO CO09132279A patent/CO6241155A2/es not_active Application Discontinuation
- 2009-11-26 MA MA32376A patent/MA31397B1/fr unknown
- 2009-12-02 EC EC2009009779A patent/ECSP099779A/es unknown
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