JP2013544271A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2013544271A5 JP2013544271A5 JP2013541384A JP2013541384A JP2013544271A5 JP 2013544271 A5 JP2013544271 A5 JP 2013544271A5 JP 2013541384 A JP2013541384 A JP 2013541384A JP 2013541384 A JP2013541384 A JP 2013541384A JP 2013544271 A5 JP2013544271 A5 JP 2013544271A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- compound
- solid pharmaceutical
- solid
- formula
- 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.)
- Pending
Links
- 239000008194 pharmaceutical composition Substances 0.000 claims description 80
- 239000007787 solid Substances 0.000 claims description 57
- 150000001875 compounds Chemical class 0.000 claims description 38
- 150000003839 salts Chemical class 0.000 claims description 17
- 239000000203 mixture Substances 0.000 claims description 16
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 claims description 16
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 14
- 238000002425 crystallisation Methods 0.000 claims description 13
- 230000008025 crystallization Effects 0.000 claims description 13
- 239000003112 inhibitor Substances 0.000 claims description 13
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 12
- 239000003795 chemical substances by application Substances 0.000 claims description 11
- 239000007884 disintegrant Substances 0.000 claims description 11
- 239000003937 drug carrier Substances 0.000 claims description 11
- 230000005764 inhibitory process Effects 0.000 claims description 10
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims description 8
- 238000000034 method Methods 0.000 claims description 8
- 239000000243 solution Substances 0.000 claims description 8
- 238000011282 treatment Methods 0.000 claims description 8
- 230000002265 prevention Effects 0.000 claims description 7
- 238000005079 FT-Raman Methods 0.000 claims description 6
- HSHXDCVZWHOWCS-UHFFFAOYSA-N N'-hexadecylthiophene-2-carbohydrazide Chemical compound CCCCCCCCCCCCCCCCNNC(=O)c1cccs1 HSHXDCVZWHOWCS-UHFFFAOYSA-N 0.000 claims description 6
- 102000007466 Purinergic P2 Receptors Human genes 0.000 claims description 6
- 108010085249 Purinergic P2 Receptors Proteins 0.000 claims description 6
- 239000013543 active substance Substances 0.000 claims description 6
- 230000003113 alkalizing effect Effects 0.000 claims description 6
- 229960000913 crospovidone Drugs 0.000 claims description 6
- 238000000113 differential scanning calorimetry Methods 0.000 claims description 6
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 6
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 6
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 6
- 238000004519 manufacturing process Methods 0.000 claims description 6
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 6
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 6
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 6
- 239000007909 solid dosage form Substances 0.000 claims description 6
- 238000001228 spectrum Methods 0.000 claims description 6
- 239000000725 suspension Substances 0.000 claims description 6
- 238000004922 13C solid-state nuclear magnetic resonance spectroscopy Methods 0.000 claims description 5
- 229920002785 Croscarmellose sodium Polymers 0.000 claims description 4
- 238000001157 Fourier transform infrared spectrum Methods 0.000 claims description 4
- 239000002253 acid Substances 0.000 claims description 4
- 229910000019 calcium carbonate Inorganic materials 0.000 claims description 4
- 239000001506 calcium phosphate Substances 0.000 claims description 4
- 229910000389 calcium phosphate Inorganic materials 0.000 claims description 4
- 235000011010 calcium phosphates Nutrition 0.000 claims description 4
- 239000013078 crystal Substances 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 239000000314 lubricant Substances 0.000 claims description 4
- 239000000395 magnesium oxide Substances 0.000 claims description 4
- CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Inorganic materials [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 claims description 4
- AXZKOIWUVFPNLO-UHFFFAOYSA-N magnesium;oxygen(2-) Chemical compound [O-2].[Mg+2] AXZKOIWUVFPNLO-UHFFFAOYSA-N 0.000 claims description 4
- 239000006186 oral dosage form Substances 0.000 claims description 4
- 229940079832 sodium starch glycolate Drugs 0.000 claims description 4
- 239000008109 sodium starch glycolate Substances 0.000 claims description 4
- 229920003109 sodium starch glycolate Polymers 0.000 claims description 4
- 230000001732 thrombotic effect Effects 0.000 claims description 4
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 3
- 241000124008 Mammalia Species 0.000 claims description 2
- 229920003081 Povidone K 30 Polymers 0.000 claims description 2
- UYAFFHXGCSJRIB-UHFFFAOYSA-N [K].FC=1C=C2C(NC(NC2=CC1NC)=O)=O Chemical compound [K].FC=1C=C2C(NC(NC2=CC1NC)=O)=O UYAFFHXGCSJRIB-UHFFFAOYSA-N 0.000 claims description 2
- VJHCJDRQFCCTHL-UHFFFAOYSA-N acetic acid 2,3,4,5,6-pentahydroxyhexanal Chemical compound CC(O)=O.OCC(O)C(O)C(O)C(O)C=O VJHCJDRQFCCTHL-UHFFFAOYSA-N 0.000 claims description 2
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 2
- 239000003929 acidic solution Substances 0.000 claims description 2
- 150000001408 amides Chemical class 0.000 claims description 2
- 239000007864 aqueous solution Substances 0.000 claims description 2
- 239000002775 capsule Substances 0.000 claims description 2
- 238000001816 cooling Methods 0.000 claims description 2
- 229960005168 croscarmellose Drugs 0.000 claims description 2
- 229960001681 croscarmellose sodium Drugs 0.000 claims description 2
- 239000001767 crosslinked sodium carboxy methyl cellulose Substances 0.000 claims description 2
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims description 2
- 238000000354 decomposition reaction Methods 0.000 claims description 2
- 238000001035 drying Methods 0.000 claims description 2
- 239000000945 filler Substances 0.000 claims description 2
- 238000001914 filtration Methods 0.000 claims description 2
- 238000010438 heat treatment Methods 0.000 claims description 2
- 238000002844 melting Methods 0.000 claims description 2
- 230000008018 melting Effects 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 229920000642 polymer Polymers 0.000 claims description 2
- 239000002904 solvent Substances 0.000 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- 238000001757 thermogravimetry curve Methods 0.000 claims description 2
- 238000005406 washing Methods 0.000 claims description 2
- 239000008177 pharmaceutical agent Substances 0.000 claims 1
- 239000002831 pharmacologic agent Substances 0.000 claims 1
- 238000000371 solid-state nuclear magnetic resonance spectroscopy Methods 0.000 claims 1
- 0 CNc(cc(c(C(N1c(cc2)ccc2NC(NSc([s]2)ccc2Cl)=O)=*)c2)NC1=O)c2F Chemical compound CNc(cc(c(C(N1c(cc2)ccc2NC(NSc([s]2)ccc2Cl)=O)=*)c2)NC1=O)c2F 0.000 description 2
- 238000011321 prophylaxis Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41956710P | 2010-12-03 | 2010-12-03 | |
| US61/419,567 | 2010-12-03 | ||
| PCT/EP2011/071821 WO2012072824A1 (en) | 2010-12-03 | 2011-12-05 | Pharmaceutical compositions, dosage forms and new forms of the compound of formula (i), and methods of use thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015222649A Division JP2016026231A (ja) | 2010-12-03 | 2015-11-13 | 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013544271A JP2013544271A (ja) | 2013-12-12 |
| JP2013544271A5 true JP2013544271A5 (enExample) | 2015-01-22 |
Family
ID=45315756
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013541384A Pending JP2013544271A (ja) | 2010-12-03 | 2011-12-05 | 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 |
| JP2015222649A Pending JP2016026231A (ja) | 2010-12-03 | 2015-11-13 | 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 |
| JP2017242767A Pending JP2018039854A (ja) | 2010-12-03 | 2017-12-19 | 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 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015222649A Pending JP2016026231A (ja) | 2010-12-03 | 2015-11-13 | 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 |
| JP2017242767A Pending JP2018039854A (ja) | 2010-12-03 | 2017-12-19 | 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 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8987285B2 (enExample) |
| EP (1) | EP2646434B1 (enExample) |
| JP (3) | JP2013544271A (enExample) |
| CN (1) | CN103339126B (enExample) |
| WO (1) | WO2012072824A1 (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA202091385A3 (ru) * | 2014-08-20 | 2021-06-30 | Портола Фармасьютикалз, Инк. | Лиофилизированные составы для антидота фактора ха |
| US20190022013A1 (en) | 2015-12-19 | 2019-01-24 | First Time Us Generics Llc | Soft-chew tablet pharmaceutical formulations |
| EP3389628A4 (en) * | 2015-12-19 | 2019-08-07 | Dixit, Manesh A. | PHARMACEUTICAL FORMULATIONS OF MOUSE CHEESE TABLETS |
| CN108883160B (zh) | 2016-02-24 | 2022-06-28 | 博尔托拉制药公司 | 因子xa解毒剂的冻干制剂 |
| CN110296911B (zh) * | 2019-07-25 | 2021-09-24 | 天津科技大学 | 一种快速检测加工过程中淀粉-脂质复合物含量的方法 |
| KR102759429B1 (ko) | 2019-07-29 | 2025-01-22 | 마더슨 이노베이션스 컴퍼니 리미티드 | 회로기판이 장착된 차량용 리어뷰 디바이스 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SK9742002A3 (en) * | 2000-01-07 | 2003-02-04 | Transform Pharmaceuticals Inc | High-throughput formation, identification, and analysis of diverse solid-forms |
| US6264987B1 (en) | 2000-05-19 | 2001-07-24 | Alkermes Controlled Therapeutics Inc. Ii | Method for preparing microparticles having a selected polymer molecular weight |
| EP1425577A4 (en) * | 2001-08-10 | 2004-12-29 | Symyx Technologies Inc | APPARATUSES AND METHODS FOR PREPARING AND TESTING PRE-FORMULATIONS AND CORRESPONDING SYSTEMS |
| CN1923835A (zh) * | 2001-12-18 | 2007-03-07 | 特瓦制药工业有限公司 | 氯吡格雷硫酸氢盐的多晶型 |
| US8058284B2 (en) * | 2005-11-03 | 2011-11-15 | 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 |
| EA200901474A1 (ru) * | 2007-05-02 | 2010-04-30 | Портола Фармасьютиклз, Инк. | Соли [4-(6-фтор-7-метиламино-2,4-диоксо-1,4-дигидро-2н-хиназолин-3-ил)фенил]-5-хлортиофен-2-илсульфонилмочевины в различных кристаллических формах и фармацевтические композиции на их основе |
| 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 |
| WO2008137753A2 (en) * | 2007-05-02 | 2008-11-13 | Portola Pharmaceuticals, Inc. | Intravenous and oral dosing of a direct-acting and reversible p2y12 inhibitor |
| RU2011123377A (ru) * | 2008-11-14 | 2012-12-20 | Портола Фармасьютиклз, Инк. | ТВЕРДАЯ КОМПОЗИЦИЯ ДЛЯ КОНТРОЛИРУЕМОГО ВЫСВОБОЖДЕНИЯ АКТИВНЫХ ИОНИЗИРУЕМЫХ АГЕНТОВ, ХАРАКТЕРИЗУЮЩИХСЯ НИЗКОЙ РАСТВОРИМОСТЬЮ В ВОДЕ ПРИ НИЗКИХ ЗНАЧЕНИЯХ pН, И СПОСОБЫ ЕЕ ПРИМЕНЕНИЯ |
| WO2011088152A1 (en) | 2010-01-12 | 2011-07-21 | Portola Pharmaceuticals, Inc. | Pharmaceutical composition and dosage forms of elinogrel and methods of use thereof |
-
2011
- 2011-12-05 CN CN201180066359.3A patent/CN103339126B/zh not_active Expired - Fee Related
- 2011-12-05 JP JP2013541384A patent/JP2013544271A/ja active Pending
- 2011-12-05 US US13/990,632 patent/US8987285B2/en active Active
- 2011-12-05 EP EP11794108.8A patent/EP2646434B1/en not_active Not-in-force
- 2011-12-05 WO PCT/EP2011/071821 patent/WO2012072824A1/en not_active Ceased
-
2015
- 2015-11-13 JP JP2015222649A patent/JP2016026231A/ja active Pending
-
2017
- 2017-12-19 JP JP2017242767A patent/JP2018039854A/ja active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2022176961A (ja) | ｛［５－（３－クロロフェニル）－３－ヒドロキシピリジン－２－カルボニル］アミノ｝酢酸の固体形態、組成物、及びその使用 | |
| KR101612642B1 (ko) | 테노포비어 알라펜아미드 헤미푸마레이트 | |
| JP2019515024A (ja) | ボルチオキセチンのパモ酸塩及びその結晶形 | |
| JP2015518885A5 (enExample) | ||
| JP2013526482A5 (enExample) | ||
| JP2016512531A5 (enExample) | ||
| JP2010514806A5 (enExample) | ||
| JP2010077141A5 (enExample) | ||
| JP2014074067A (ja) | メシル酸イマチニブのｆ、ｇ、ｈ、ｉおよびｋ結晶形 | |
| JP2025131661A (ja) | ２－（５－（４－（２－モルホリノエトキシ）フェニル）ピリジン－２－イル）－ｎ－ベンジルアセトアミドの固体形態 | |
| JP2020073513A (ja) | α，ω‐二置換ジヒドロキシシクロペンチル化合物の固体形態、並びにその製造及び使用方法 | |
| RU2014138619A (ru) | Новые соли тримебутина на основе сульфонатов | |
| KR100878698B1 (ko) | 결정형의 베포타스틴 금속염 수화물, 이의 제조방법 및이를 포함하는 약학 조성물 | |
| RU2013125756A (ru) | Твердые формы (s)-2-амино-3-(4-(2-амино-6-((r)-1-(4-хлор-2-(3-метил-1н-пиразол-1-ил)фенил)-2,2,2-трифторэтокси)пиримидин-4-ил)фенил)пропановой кислоты | |
| JP2013541589A5 (enExample) | ||
| KR20100082359A (ko) | 신경병성 통증에 활성이 있는 약물 | |
| JP2018521055A (ja) | サクビトリルカルシウム塩 | |
| JP7139116B2 (ja) | フェニルアミノピリミジン化合物またはその塩の多形物 | |
| JP2008007507A (ja) | 結晶形アトルバスタチン | |
| RU2005105688A (ru) | Полиморфизм додекагидроциклопента (а) фенантренилового эфира тиофенкарбоновой кислоты | |
| CN103068392A (zh) | 苯甲酸阿格列汀的多晶形物 | |
| JP2026511788A (ja) | ピトリサント塩酸塩の多形形態 | |
| WO2015116782A1 (en) | Nucleobase analogue derivatives and their applications | |
| JP7809725B2 (ja) | 三環式誘導体化合物の結晶形及びその製造方法並びにそれを含む薬学的組成物 | |
| JP6421873B2 (ja) | テノホビルジソプロキシルの新規塩 |