JP2013542258A5 - - Google Patents
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- Publication number
- JP2013542258A5 JP2013542258A5 JP2013538839A JP2013538839A JP2013542258A5 JP 2013542258 A5 JP2013542258 A5 JP 2013542258A5 JP 2013538839 A JP2013538839 A JP 2013538839A JP 2013538839 A JP2013538839 A JP 2013538839A JP 2013542258 A5 JP2013542258 A5 JP 2013542258A5
- Authority
- JP
- Japan
- Prior art keywords
- crystalline
- salt
- powder
- differential scanning
- scanning calorimetry
- 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
- 150000003839 salts Chemical class 0.000 claims description 18
- 238000000113 differential scanning calorimetry Methods 0.000 claims description 16
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 16
- 238000001757 thermogravimetry curve Methods 0.000 claims description 16
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 12
- 239000007787 solid Substances 0.000 claims description 12
- 238000004519 manufacturing process Methods 0.000 claims description 11
- 238000000034 method Methods 0.000 claims description 11
- -1 (S) -2-mercapto-4-methylpentanoylamino Chemical group 0.000 claims description 10
- 150000001875 compounds Chemical class 0.000 claims description 9
- 239000003814 drug Substances 0.000 claims description 9
- 238000002844 melting Methods 0.000 claims description 8
- 230000008018 melting Effects 0.000 claims description 8
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims description 6
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims description 6
- 238000004090 dissolution Methods 0.000 claims description 6
- 238000010438 heat treatment Methods 0.000 claims description 6
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims description 6
- 238000003756 stirring Methods 0.000 claims description 6
- 206010019280 Heart failures Diseases 0.000 claims description 5
- 206010020772 Hypertension Diseases 0.000 claims description 5
- 239000002253 acid Substances 0.000 claims description 5
- BSJZYWSFNCKCDR-VWLOTQADSA-N 2-[4-[[2-ethoxy-4-ethyl-5-[[[(2s)-4-methyl-2-sulfanylpentanoyl]amino]methyl]imidazol-1-yl]methyl]-3-fluorophenyl]benzoic acid Chemical compound CCOC1=NC(CC)=C(CNC(=O)[C@@H](S)CC(C)C)N1CC1=CC=C(C=2C(=CC=CC=2)C(O)=O)C=C1F BSJZYWSFNCKCDR-VWLOTQADSA-N 0.000 claims description 4
- 239000005541 ACE inhibitor Substances 0.000 claims description 4
- 239000003795 chemical substances by application Substances 0.000 claims description 4
- 239000002792 enkephalinase inhibitor Substances 0.000 claims description 4
- XTEGVFVZDVNBPF-UHFFFAOYSA-N naphthalene-1,5-disulfonic acid Chemical compound C1=CC=C2C(S(=O)(=O)O)=CC=CC2=C1S(O)(=O)=O XTEGVFVZDVNBPF-UHFFFAOYSA-N 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- UUUHXMGGBIUAPW-UHFFFAOYSA-N 1-[1-[2-[[5-amino-2-[[1-[5-(diaminomethylideneamino)-2-[[1-[3-(1h-indol-3-yl)-2-[(5-oxopyrrolidine-2-carbonyl)amino]propanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbon Chemical compound C1CCC(C(=O)N2C(CCC2)C(O)=O)N1C(=O)C(C(C)CC)NC(=O)C(CCC(N)=O)NC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C1CCCN1C(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C1CCC(=O)N1 UUUHXMGGBIUAPW-UHFFFAOYSA-N 0.000 claims description 2
- 101710129690 Angiotensin-converting enzyme inhibitor Proteins 0.000 claims description 2
- 101710086378 Bradykinin-potentiating and C-type natriuretic peptides Proteins 0.000 claims description 2
- 229940127291 Calcium channel antagonist Drugs 0.000 claims description 2
- 229940118365 Endothelin receptor antagonist Drugs 0.000 claims description 2
- 102000004270 Peptidyl-Dipeptidase A Human genes 0.000 claims description 2
- 108090000882 Peptidyl-Dipeptidase A Proteins 0.000 claims description 2
- 239000000332 adrenergic beta-1 receptor antagonist Substances 0.000 claims description 2
- 239000002170 aldosterone antagonist Substances 0.000 claims description 2
- 229940083712 aldosterone antagonist Drugs 0.000 claims description 2
- 239000002333 angiotensin II receptor antagonist Substances 0.000 claims description 2
- 239000000400 angiotensin II type 1 receptor blocker Substances 0.000 claims description 2
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims description 2
- 230000003178 anti-diabetic effect Effects 0.000 claims description 2
- 239000003146 anticoagulant agent Substances 0.000 claims description 2
- 239000003472 antidiabetic agent Substances 0.000 claims description 2
- 229960004676 antithrombotic agent Drugs 0.000 claims description 2
- 239000000480 calcium channel blocker Substances 0.000 claims description 2
- KNHUKKLJHYUCFP-UHFFFAOYSA-N clofibrate Chemical compound CCOC(=O)C(C)(C)OC1=CC=C(Cl)C=C1 KNHUKKLJHYUCFP-UHFFFAOYSA-N 0.000 claims description 2
- 239000002934 diuretic Substances 0.000 claims description 2
- 230000001882 diuretic effect Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 239000002857 endothelin converting enzyme inhibitor Substances 0.000 claims description 2
- 239000002308 endothelin receptor antagonist Substances 0.000 claims description 2
- AFAXGSQYZLGZPG-UHFFFAOYSA-N ethanedisulfonic acid Chemical compound OS(=O)(=O)CCS(O)(=O)=O AFAXGSQYZLGZPG-UHFFFAOYSA-N 0.000 claims description 2
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims description 2
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims description 2
- 235000006408 oxalic acid Nutrition 0.000 claims description 2
- 150000003180 prostaglandins Chemical class 0.000 claims description 2
- 239000002461 renin inhibitor Substances 0.000 claims description 2
- 229940086526 renin-inhibitors Drugs 0.000 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- 238000002560 therapeutic procedure Methods 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 3
- 229940122783 Endothelin converting-enzyme inhibitor Drugs 0.000 claims 1
- 239000013078 crystal Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41201110P | 2010-11-10 | 2010-11-10 | |
| US61/412,011 | 2010-11-10 | ||
| PCT/US2011/059895 WO2012064807A1 (en) | 2010-11-10 | 2011-11-09 | Crystalline forms of an alkoxyimidazol-1-ylmethyl biphenyl carboxylic acid |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015174397A Division JP2016028061A (ja) | 2010-11-10 | 2015-09-04 | アルコキシイミダゾール−１−イルメチルビフェニルカルボン酸の結晶性形態 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013542258A JP2013542258A (ja) | 2013-11-21 |
| JP2013542258A5 true JP2013542258A5 (https=) | 2014-11-06 |
Family
ID=45003086
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013538839A Pending JP2013542258A (ja) | 2010-11-10 | 2011-11-09 | アルコキシイミダゾール−１−イルメチルビフェニルカルボン酸の結晶性形態 |
| JP2015174397A Pending JP2016028061A (ja) | 2010-11-10 | 2015-09-04 | アルコキシイミダゾール−１−イルメチルビフェニルカルボン酸の結晶性形態 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015174397A Pending JP2016028061A (ja) | 2010-11-10 | 2015-09-04 | アルコキシイミダゾール−１−イルメチルビフェニルカルボン酸の結晶性形態 |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US8362060B2 (https=) |
| EP (1) | EP2638017B1 (https=) |
| JP (2) | JP2013542258A (https=) |
| KR (1) | KR20130130730A (https=) |
| CN (1) | CN103189362B (https=) |
| AR (1) | AR083828A1 (https=) |
| AU (1) | AU2011326622B2 (https=) |
| BR (1) | BR112013011715A2 (https=) |
| CA (1) | CA2812598A1 (https=) |
| CO (1) | CO6741224A2 (https=) |
| ES (1) | ES2567721T3 (https=) |
| IL (1) | IL225303A0 (https=) |
| MX (1) | MX2013005165A (https=) |
| NZ (1) | NZ609804A (https=) |
| PH (1) | PH12013500945A1 (https=) |
| RU (1) | RU2013126403A (https=) |
| SG (1) | SG189448A1 (https=) |
| TW (1) | TW201300366A (https=) |
| WO (1) | WO2012064807A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI448284B (zh) | 2007-04-24 | 2014-08-11 | Theravance Inc | 雙效抗高血壓劑 |
| CN106810542B (zh) * | 2015-11-30 | 2021-03-09 | 苏州开拓药业股份有限公司 | 一种硫代咪唑烷酮化合物的晶型、盐型及其制备方法 |
| EP4337638A1 (en) * | 2021-05-11 | 2024-03-20 | Astex Pharmaceuticals, Inc. | Solid forms of salts of 4-[5-[(3s)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-ethylpropyl)phenyl]phenyl]-2-fluoro-benzonitrile |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006027680A1 (en) | 2004-09-10 | 2006-03-16 | Pfizer Limited | 3-(1-carbamoylcyclohexyl) propionic acid derivatives as inhibitors of neutral endopeptidase enzyme |
| AR057882A1 (es) | 2005-11-09 | 2007-12-26 | Novartis Ag | Compuestos de accion doble de bloqueadores del receptor de angiotensina e inhibidores de endopeptidasa neutra |
| WO2007106708A2 (en) | 2006-03-10 | 2007-09-20 | Novartis Ag | Combinations of the angiotensin ii antagonist valsartan and the nep inhibitor daglutril |
| TWI448284B (zh) * | 2007-04-24 | 2014-08-11 | Theravance Inc | 雙效抗高血壓劑 |
| TW201014830A (en) * | 2008-09-30 | 2010-04-16 | Theravance Inc | Crystalline form of an alkoxyimidazol-1-ylmethyl biphenyl carboxylic acid |
| TWI545114B (zh) * | 2009-09-29 | 2016-08-11 | 施萬生物製藥研發Ｉｐ有限責任公司 | 製備聯苯基咪唑化合物之方法 |
| US8399501B2 (en) | 2010-03-04 | 2013-03-19 | Theravance, Inc. | Crystalline alkoxyimidazol-1-ylmethyl biphenyl carboxylic acid and methods for preparing thereof |
-
2011
- 2011-11-09 BR BR112013011715A patent/BR112013011715A2/pt not_active IP Right Cessation
- 2011-11-09 AU AU2011326622A patent/AU2011326622B2/en not_active Ceased
- 2011-11-09 EP EP11785872.0A patent/EP2638017B1/en active Active
- 2011-11-09 CA CA2812598A patent/CA2812598A1/en not_active Abandoned
- 2011-11-09 CN CN201180053069.5A patent/CN103189362B/zh not_active Expired - Fee Related
- 2011-11-09 PH PH1/2013/500945A patent/PH12013500945A1/en unknown
- 2011-11-09 JP JP2013538839A patent/JP2013542258A/ja active Pending
- 2011-11-09 ES ES11785872.0T patent/ES2567721T3/es active Active
- 2011-11-09 NZ NZ609804A patent/NZ609804A/en not_active IP Right Cessation
- 2011-11-09 KR KR1020137014134A patent/KR20130130730A/ko not_active Withdrawn
- 2011-11-09 RU RU2013126403/04A patent/RU2013126403A/ru not_active Application Discontinuation
- 2011-11-09 WO PCT/US2011/059895 patent/WO2012064807A1/en not_active Ceased
- 2011-11-09 US US13/292,370 patent/US8362060B2/en not_active Expired - Fee Related
- 2011-11-09 MX MX2013005165A patent/MX2013005165A/es unknown
- 2011-11-09 SG SG2013029178A patent/SG189448A1/en unknown
- 2011-11-10 TW TW100141108A patent/TW201300366A/zh unknown
- 2011-11-10 AR ARP110104201A patent/AR083828A1/es unknown
-
2012
- 2012-12-19 US US13/720,395 patent/US8802709B2/en not_active Expired - Fee Related
-
2013
- 2013-03-18 IL IL225303A patent/IL225303A0/en unknown
- 2013-05-03 CO CO13111802A patent/CO6741224A2/es unknown
-
2014
- 2014-06-27 US US14/317,060 patent/US9249105B2/en not_active Expired - Fee Related
-
2015
- 2015-09-04 JP JP2015174397A patent/JP2016028061A/ja active Pending
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