ES2567721T3 - Formas cristalinas de un ácido alcoxi-imidazol-1-ilmetil bifenil carboxílico - Google Patents
Formas cristalinas de un ácido alcoxi-imidazol-1-ilmetil bifenil carboxílico Download PDFInfo
- Publication number
- ES2567721T3 ES2567721T3 ES11785872.0T ES11785872T ES2567721T3 ES 2567721 T3 ES2567721 T3 ES 2567721T3 ES 11785872 T ES11785872 T ES 11785872T ES 2567721 T3 ES2567721 T3 ES 2567721T3
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- Spain
- Prior art keywords
- acid
- imidazol
- carboxylic acid
- crystalline form
- ylmethyl
- 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.)
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- -1 (S) -2-mercapto-4-methylpentanoylamino Chemical group 0.000 abstract description 20
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract description 11
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- 238000012360 testing method Methods 0.000 description 13
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- VYMDGNCVAMGZFE-UHFFFAOYSA-N phenylbutazonum Chemical compound O=C1C(CCCC)C(=O)N(C=2C=CC=CC=2)N1C1=CC=CC=C1 VYMDGNCVAMGZFE-UHFFFAOYSA-N 0.000 description 1
- BWSDNRQVTFZQQD-AYVHNPTNSA-N phosphoramidon Chemical compound O([P@@](O)(=O)N[C@H](CC(C)C)C(=O)N[C@H](CC=1[C]2C=CC=CC2=NC=1)C(O)=O)[C@H]1O[C@@H](C)[C@H](O)[C@@H](O)[C@@H]1O BWSDNRQVTFZQQD-AYVHNPTNSA-N 0.000 description 1
- 108010072906 phosphoramidon Proteins 0.000 description 1
- 229960005095 pioglitazone Drugs 0.000 description 1
- 229960002702 piroxicam Drugs 0.000 description 1
- QYSPLQLAKJAUJT-UHFFFAOYSA-N piroxicam Chemical compound OC=1C2=CC=CC=C2S(=O)(=O)N(C)C=1C(=O)NC1=CC=CC=N1 QYSPLQLAKJAUJT-UHFFFAOYSA-N 0.000 description 1
- 239000000106 platelet aggregation inhibitor Substances 0.000 description 1
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 229960002965 pravastatin Drugs 0.000 description 1
- TUZYXOIXSAXUGO-PZAWKZKUSA-N pravastatin Chemical compound C1=C[C@H](C)[C@H](CC[C@@H](O)C[C@@H](O)CC(O)=O)[C@H]2[C@@H](OC(=O)[C@@H](C)CC)C[C@H](O)C=C21 TUZYXOIXSAXUGO-PZAWKZKUSA-N 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 1
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
- 229960003415 propylparaben Drugs 0.000 description 1
- 238000000159 protein binding assay Methods 0.000 description 1
- 230000001698 pyrogenic effect Effects 0.000 description 1
- 238000004451 qualitative analysis Methods 0.000 description 1
- 238000004445 quantitative analysis Methods 0.000 description 1
- 239000010453 quartz Substances 0.000 description 1
- 230000005855 radiation Effects 0.000 description 1
- 238000003653 radioligand binding assay Methods 0.000 description 1
- 238000001525 receptor binding assay Methods 0.000 description 1
- 229960004702 remikiren Drugs 0.000 description 1
- ZHIQVOYGQFSRBZ-VQXQMPIVSA-N remikiren Chemical compound C([C@H](CS(=O)(=O)C(C)(C)C)C(=O)N[C@@H](CC=1[N]C=NC=1)C(=O)N[C@@H](CC1CCCCC1)[C@@H](O)[C@@H](O)C1CC1)C1=CC=CC=C1 ZHIQVOYGQFSRBZ-VQXQMPIVSA-N 0.000 description 1
- 239000002461 renin inhibitor Substances 0.000 description 1
- 229940086526 renin-inhibitors Drugs 0.000 description 1
- 229960002354 repaglinide Drugs 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 229960004586 rosiglitazone Drugs 0.000 description 1
- 229960000672 rosuvastatin Drugs 0.000 description 1
- BPRHUIZQVSMCRT-VEUZHWNKSA-N rosuvastatin Chemical compound CC(C)C1=NC(N(C)S(C)(=O)=O)=NC(C=2C=CC(F)=CC=2)=C1\C=C\[C@@H](O)C[C@@H](O)CC(O)=O BPRHUIZQVSMCRT-VEUZHWNKSA-N 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 229960002855 simvastatin Drugs 0.000 description 1
- RYMZZMVNJRMUDD-HGQWONQESA-N simvastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)C(C)(C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 RYMZZMVNJRMUDD-HGQWONQESA-N 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 239000012798 spherical particle Substances 0.000 description 1
- 229960002256 spironolactone Drugs 0.000 description 1
- LXMSZDCAJNLERA-ZHYRCANASA-N spironolactone Chemical compound C([C@@H]1[C@]2(C)CC[C@@H]3[C@@]4(C)CCC(=O)C=C4C[C@H]([C@@H]13)SC(=O)C)C[C@@]21CCC(=O)O1 LXMSZDCAJNLERA-ZHYRCANASA-N 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000008223 sterile water Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000007916 tablet composition Substances 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 229960002871 tenoxicam Drugs 0.000 description 1
- WZWYJBNHTWCXIM-UHFFFAOYSA-N tenoxicam Chemical compound O=C1C=2SC=CC=2S(=O)(=O)N(C)C1=C(O)NC1=CC=CC=N1 WZWYJBNHTWCXIM-UHFFFAOYSA-N 0.000 description 1
- 229950000584 tezosentan Drugs 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 150000001467 thiazolidinediones Chemical class 0.000 description 1
- OUDSBRTVNLOZBN-UHFFFAOYSA-N tolazamide Chemical compound C1=CC(C)=CC=C1S(=O)(=O)NC(=O)NN1CCCCCC1 OUDSBRTVNLOZBN-UHFFFAOYSA-N 0.000 description 1
- 229960002277 tolazamide Drugs 0.000 description 1
- 229960002905 tolfenamic acid Drugs 0.000 description 1
- YEZNLOUZAIOMLT-UHFFFAOYSA-N tolfenamic acid Chemical compound CC1=C(Cl)C=CC=C1NC1=CC=CC=C1C(O)=O YEZNLOUZAIOMLT-UHFFFAOYSA-N 0.000 description 1
- 229960001017 tolmetin Drugs 0.000 description 1
- UPSPUYADGBWSHF-UHFFFAOYSA-N tolmetin Chemical compound C1=CC(C)=CC=C1C(=O)C1=CC=C(CC(O)=O)N1C UPSPUYADGBWSHF-UHFFFAOYSA-N 0.000 description 1
- GYHCTFXIZSNGJT-UHFFFAOYSA-N tolvaptan Chemical compound CC1=CC=CC=C1C(=O)NC(C=C1C)=CC=C1C(=O)N1C2=CC=C(Cl)C=C2C(O)CCC1 GYHCTFXIZSNGJT-UHFFFAOYSA-N 0.000 description 1
- 229960001256 tolvaptan Drugs 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 229950000451 triflumidate Drugs 0.000 description 1
- 229960004799 tryptophan Drugs 0.000 description 1
- 229940032178 vaseretic Drugs 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 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 | |
| US412011P | 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 |
|---|---|
| ES2567721T3 true ES2567721T3 (es) | 2016-04-26 |
Family
ID=45003086
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES11785872.0T Active ES2567721T3 (es) | 2010-11-10 | 2011-11-09 | Formas cristalinas de un ácido alcoxi-imidazol-1-ilmetil bifenil carboxílico |
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 |
| RU2013126403A (ru) | 2014-12-20 |
| 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 |
| 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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