RU2013126403A - Кристаллические формы алкоксиимидазол-1-илметилбифенилкарбоновых кислот - Google Patents
Кристаллические формы алкоксиимидазол-1-илметилбифенилкарбоновых кислот Download PDFInfo
- Publication number
- RU2013126403A RU2013126403A RU2013126403/04A RU2013126403A RU2013126403A RU 2013126403 A RU2013126403 A RU 2013126403A RU 2013126403/04 A RU2013126403/04 A RU 2013126403/04A RU 2013126403 A RU2013126403 A RU 2013126403A RU 2013126403 A RU2013126403 A RU 2013126403A
- Authority
- RU
- Russia
- Prior art keywords
- crystalline
- hemidisilate
- salt
- salt according
- powder
- Prior art date
Links
- 150000001735 carboxylic acids Chemical class 0.000 title 1
- 239000013078 crystal Substances 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims abstract 26
- 238000001757 thermogravimetry curve Methods 0.000 claims abstract 14
- 238000000113 differential scanning calorimetry Methods 0.000 claims abstract 10
- -1 (S) -2-mercapto-4-methylpentanoylamino Chemical group 0.000 claims abstract 6
- 238000000634 powder X-ray diffraction Methods 0.000 claims abstract 6
- 238000002844 melting Methods 0.000 claims abstract 5
- 230000008018 melting Effects 0.000 claims abstract 5
- 238000010438 heat treatment Methods 0.000 claims abstract 4
- 238000003756 stirring Methods 0.000 claims abstract 4
- 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 abstract 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract 3
- 238000004519 manufacturing process Methods 0.000 claims abstract 2
- 239000007787 solid Substances 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 5
- 239000000843 powder Substances 0.000 claims 5
- 238000000034 method Methods 0.000 claims 4
- 238000004090 dissolution Methods 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 239000005541 ACE inhibitor Substances 0.000 claims 2
- 206010019280 Heart failures Diseases 0.000 claims 2
- 206010020772 Hypertension Diseases 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 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 1
- 108060003345 Adrenergic Receptor Proteins 0.000 claims 1
- 102000017910 Adrenergic receptor Human genes 0.000 claims 1
- 229940127291 Calcium channel antagonist Drugs 0.000 claims 1
- 229940118365 Endothelin receptor antagonist Drugs 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- 102000004270 Peptidyl-Dipeptidase A Human genes 0.000 claims 1
- 108090000882 Peptidyl-Dipeptidase A Proteins 0.000 claims 1
- 239000002170 aldosterone antagonist Substances 0.000 claims 1
- 229940083712 aldosterone antagonist Drugs 0.000 claims 1
- 239000002333 angiotensin II receptor antagonist Substances 0.000 claims 1
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims 1
- 239000003146 anticoagulant agent Substances 0.000 claims 1
- 239000003472 antidiabetic agent Substances 0.000 claims 1
- 229940125708 antidiabetic agent Drugs 0.000 claims 1
- 229960004676 antithrombotic agent Drugs 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 239000000480 calcium channel blocker Substances 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000002934 diuretic Substances 0.000 claims 1
- 229940030606 diuretics Drugs 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000003511 endothelial effect Effects 0.000 claims 1
- 239000002308 endothelin receptor antagonist Substances 0.000 claims 1
- 239000002792 enkephalinase inhibitor Substances 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
- 229940094443 oxytocics prostaglandins Drugs 0.000 claims 1
- 150000003180 prostaglandins Chemical class 0.000 claims 1
- 238000000746 purification Methods 0.000 claims 1
- 239000002461 renin inhibitor Substances 0.000 claims 1
- 229940086526 renin-inhibitors Drugs 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- AFAXGSQYZLGZPG-UHFFFAOYSA-N ethanedisulfonic acid Chemical compound OS(=O)(=O)CCS(O)(=O)=O AFAXGSQYZLGZPG-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D233/70—One oxygen atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4174—Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
- A61P5/42—Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of mineralocorticosteroids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2013126403A true RU2013126403A (ru) | 2014-12-20 |
Family
ID=45003086
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2013126403/04A RU2013126403A (ru) | 2010-11-10 | 2011-11-09 | Кристаллические формы алкоксиимидазол-1-илметилбифенилкарбоновых кислот |
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
Also Published As
| Publication number | Publication date |
|---|---|
| AR083828A1 (es) | 2013-03-27 |
| BR112013011715A2 (pt) | 2017-10-31 |
| CO6741224A2 (es) | 2013-08-30 |
| PH12013500945A1 (en) | 2013-07-08 |
| TW201300366A (zh) | 2013-01-01 |
| AU2011326622B2 (en) | 2014-12-18 |
| HK1187919A1 (zh) | 2014-04-17 |
| EP2638017B1 (en) | 2016-01-27 |
| US20120115920A1 (en) | 2012-05-10 |
| JP2016028061A (ja) | 2016-02-25 |
| MX2013005165A (es) | 2013-07-05 |
| US9249105B2 (en) | 2016-02-02 |
| US8362060B2 (en) | 2013-01-29 |
| US20130267573A1 (en) | 2013-10-10 |
| KR20130130730A (ko) | 2013-12-02 |
| ES2567721T3 (es) | 2016-04-26 |
| JP2013542258A (ja) | 2013-11-21 |
| CN103189362A (zh) | 2013-07-03 |
| NZ609804A (en) | 2015-02-27 |
| CA2812598A1 (en) | 2012-05-18 |
| AU2011326622A1 (en) | 2013-04-04 |
| US20150133518A1 (en) | 2015-05-14 |
| IL225303A0 (en) | 2013-06-27 |
| WO2012064807A1 (en) | 2012-05-18 |
| US8802709B2 (en) | 2014-08-12 |
| CN103189362B (zh) | 2015-03-11 |
| EP2638017A1 (en) | 2013-09-18 |
| SG189448A1 (en) | 2013-05-31 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20151215 |