JP2010526105A5 - - Google Patents
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- Publication number
- 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- Withdrawn
Links
- 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 (enExample) | 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 (enExample) |
| EP (1) | EP2076510A2 (enExample) |
| JP (1) | JP2010526105A (enExample) |
| KR (1) | KR20100020455A (enExample) |
| CN (1) | CN101720324A (enExample) |
| AU (1) | AU2008247457A1 (enExample) |
| BR (1) | BRPI0810800A2 (enExample) |
| CA (1) | CA2686221A1 (enExample) |
| CO (1) | CO6241155A2 (enExample) |
| EA (1) | EA200901474A1 (enExample) |
| EC (1) | ECSP099779A (enExample) |
| GT (1) | GT200900282A (enExample) |
| IL (1) | IL201829A0 (enExample) |
| MA (1) | MA31397B1 (enExample) |
| MX (1) | MX2009011836A (enExample) |
| TN (1) | TN2009000452A1 (enExample) |
| WO (1) | WO2008137809A2 (enExample) |
| ZA (1) | ZA200907493B (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2627719C (en) * | 2005-11-03 | 2016-07-12 | Portola Pharmaceuticals, Inc. | [4-(6-halo-7-substituted-2,4-dioxo-1,4-dihydro-2h-quinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylureas and forms and methods related thereto |
| 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 |
| WO2011088152A1 (en) | 2010-01-12 | 2011-07-21 | Portola Pharmaceuticals, Inc. | 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 |
| DE60144284D1 (de) * | 2000-11-01 | 2011-05-05 | Millennium Pharm Inc | Stickstoffhaltige heterozyklische verbindungen und verfahren zu deren herstellung |
| US6824790B2 (en) * | 2002-01-09 | 2004-11-30 | Enzrel Inc. | Liposome drug delivery of polycyclic, aromatic, antioxidant or anti-inflammatory compounds |
| US20040242658A1 (en) * | 2003-01-08 | 2004-12-02 | Dr. Reddy's Laboratories Limited | Amorphous form of rosiglitazone maleate and process for preparation thereof |
| PL1668002T3 (pl) * | 2003-10-03 | 2010-02-26 | Portola Pharm Inc | 2,4-diokso-3-chinazolinyloarylowe pochodne sulfonylomocznika |
| CA2627719C (en) * | 2005-11-03 | 2016-07-12 | Portola Pharmaceuticals, Inc. | [4-(6-halo-7-substituted-2,4-dioxo-1,4-dihydro-2h-quinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylureas and forms and methods related thereto |
| 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 |
| US20090048216A1 (en) * | 2007-05-02 | 2009-02-19 | Portola Pharmaceuticals, Inc. | Intravenous and oral dosing of a direct-acting and reversible p2y12 inhibitor |
-
2008
- 2008-05-02 CA CA002686221A patent/CA2686221A1/en not_active Abandoned
- 2008-05-02 EP EP08747609A patent/EP2076510A2/en not_active Withdrawn
- 2008-05-02 AU AU2008247457A patent/AU2008247457A1/en not_active Abandoned
- 2008-05-02 CN CN200880022604A patent/CN101720324A/zh active Pending
- 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 WO PCT/US2008/062584 patent/WO2008137809A2/en not_active Ceased
- 2008-05-02 KR KR1020097025052A patent/KR20100020455A/ko not_active Withdrawn
- 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
-
2009
- 2009-10-26 ZA ZA200907493A patent/ZA200907493B/xx unknown
- 2009-10-29 IL IL201829A patent/IL201829A0/en unknown
- 2009-10-30 GT GT200900282A patent/GT200900282A/es unknown
- 2009-10-30 TN TNP2009000452A patent/TN2009000452A1/fr 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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