IL161165A - Crystalline sodium salt of telmisartan and the use of the same as an angiotensin antagonist - Google Patents
Crystalline sodium salt of telmisartan and the use of the same as an angiotensin antagonistInfo
- Publication number
- IL161165A IL161165A IL161165A IL16116504A IL161165A IL 161165 A IL161165 A IL 161165A IL 161165 A IL161165 A IL 161165A IL 16116504 A IL16116504 A IL 16116504A IL 161165 A IL161165 A IL 161165A
- Authority
- IL
- Israel
- Prior art keywords
- sodium salt
- telmisartan
- acid
- crystalline
- crystalline telmisartan
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/20—Two benzimidazolyl-2 radicals linked together directly or via a hydrocarbon or substituted hydrocarbon radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Ophthalmology & Optometry (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Vascular Medicine (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
The invention relates to a crystalline sodium salt of 4'-[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)benzimidazol-1-ylmethyl]biphenyl-2-carboxylic acid (INN: Telmisartan), to a method for the production thereof, and to the use of the same for producing a pharmaceutical having an angiotensin II antagonistic action.
Claims (10)
1. ) Crystalline telmisartan-sodium salt of formula 1 characterised by
2. ) Crystalline telmisartan-sodium salt according to claim 1 , characterised in that in the X-ray powder diagram it has, inter alia, the characteristic values d= 20.95 A, 17.72 A, 13.97 A and 13.63 A.
3. ) Crystalline telmisartan-sodium salt according to one of claims 1 or 2, , characterised in that it is present in the form of the solvates or hydrates thereof, preferably in the form of the hydrates thereof.
4. ) Process for preparing crystalline telmisartan-sodium salt A, characterised in that the free acid of telmisartan is taken up in a suitable solvent, this solution is then combined with a suitable sodium salt, while at least 1 mol of sodium salt is added per mol of telmisartan, then the reaction mixture is heated for a period of from 15 minutes to 2 hours, then the solution obtained is filtered and the resulting filtrate is slowly added to an organic solvent heated to a temperature of >40°C, some of the solvent is optionally distilled off while the abovementioned filtrate is being added, the resulting concentrated solution is then cooled and the telmisartan- sodium salt which crystallises out is isolated and dried, optionally after washing with the organic solvent mentioned hereinbefore. 15 161165/2
5. ) Process for preparing crystalline telmisartan-sodium salt 1, characterised in that, an acid addition salt of formula 2 wherein H-X denotes an acid selected from among hydrochloric acid, hydrobromic acid, toluenesuiphonic acid or methanesulphonic acid, is taken up in a suitable solvent and reacted with a suitable sodium salt, using at least 2 mol of sodium salt per mol of the compound 2 used.
6. ) Crystalline telmisartan-sodium salt which may be obtained according to claim 4 or 5.
7. ) Use of crystalline telmisartan-sodium salt according to one of claims 1-3 or 6 for the preparation of a pharmaceutical composition.
8. ) Pharmaceutical formulations, characterised in that they contain crystalline telmisartan-sodium salt according to one of claims 1-3 or 6.
9. ) Compounds of formula 2 where H-X denotes toluenesuiphonic acid or methanesulphonic acid. 16 161165/2
10. ) Compound according to claim 9, characterized in that it is present in crystalline form. For the Applicants, REINHOLD COHN AND PARTNERS By:
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10153737A DE10153737A1 (en) | 2001-10-31 | 2001-10-31 | Crystalline sodium salt of telmisartan, process for its preparation and its use for the manufacture of a medicament |
| PCT/EP2002/011394 WO2003037876A1 (en) | 2001-10-31 | 2002-10-11 | Crystalline sodium salt of telmisartan and the use of the same as an angiotensin antagonist |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IL161165A true IL161165A (en) | 2009-12-24 |
Family
ID=7704331
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL16116502A IL161165A0 (en) | 2001-10-31 | 2002-10-11 | Crystalline sodium salt of telmisartan and the use of the same as an angiotensin antagonist |
| IL161165A IL161165A (en) | 2001-10-31 | 2004-03-30 | Crystalline sodium salt of telmisartan and the use of the same as an angiotensin antagonist |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL16116502A IL161165A0 (en) | 2001-10-31 | 2002-10-11 | Crystalline sodium salt of telmisartan and the use of the same as an angiotensin antagonist |
Country Status (34)
| Country | Link |
|---|---|
| EP (1) | EP1442023B1 (en) |
| JP (1) | JP5124076B2 (en) |
| KR (1) | KR100929502B1 (en) |
| CN (1) | CN100509789C (en) |
| AR (1) | AR037148A1 (en) |
| AT (1) | ATE370125T1 (en) |
| AU (1) | AU2002338886B2 (en) |
| BR (1) | BR0213568A (en) |
| CA (1) | CA2463146C (en) |
| CO (1) | CO5580785A2 (en) |
| CY (1) | CY1107504T1 (en) |
| DE (2) | DE10153737A1 (en) |
| DK (1) | DK1442023T3 (en) |
| EA (1) | EA007596B1 (en) |
| EC (1) | ECSP045089A (en) |
| ES (1) | ES2291505T3 (en) |
| HR (1) | HRP20040372A8 (en) |
| HU (1) | HUP0402391A3 (en) |
| IL (2) | IL161165A0 (en) |
| ME (1) | MEP43608A (en) |
| MX (1) | MXPA04004013A (en) |
| MY (1) | MY129741A (en) |
| NO (1) | NO326465B1 (en) |
| NZ (1) | NZ532716A (en) |
| PE (1) | PE20030629A1 (en) |
| PL (1) | PL211462B1 (en) |
| PT (1) | PT1442023E (en) |
| RS (1) | RS50879B (en) |
| SA (1) | SA02230419B1 (en) |
| SI (1) | SI1442023T1 (en) |
| TW (2) | TWI333419B (en) |
| UA (1) | UA82833C2 (en) |
| UY (1) | UY27520A1 (en) |
| WO (1) | WO2003037876A1 (en) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10319450A1 (en) * | 2003-04-30 | 2004-11-18 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Pharmaceutical formulation of telmisartan sodium salt |
| US9029363B2 (en) | 2003-04-30 | 2015-05-12 | Boehringer Ingelheim International Gmbh | Telmisartan sodium salt pharmaceutical formulation |
| CA2555294A1 (en) | 2004-02-11 | 2005-08-25 | Marina Yu Etinger | Candesartan cilexetil polymorphs |
| KR20090029310A (en) * | 2004-05-05 | 2009-03-20 | 테바 파마슈티컬 인더스트리즈 리미티드 | Preparation of high purity candesartan cilexetil |
| WO2006044754A2 (en) | 2004-10-18 | 2006-04-27 | Dr. Reddy's Laboratories Ltd. | Process for preparing telmisartan |
| JP2008516001A (en) * | 2004-11-03 | 2008-05-15 | テバ ファーマシューティカル インダストリーズ リミティド | Amorphous and polymorphic forms of telmisartan sodium |
| EP1908469A1 (en) | 2006-10-06 | 2008-04-09 | Boehringer Ingelheim Vetmedica Gmbh | Angiotensin II receptor antagonist for the treatment of systemic diseases in cats |
| EP2151450A1 (en) * | 2008-07-29 | 2010-02-10 | Sandoz AG | Method for processing microbiologically produced cyclic oligopeptides |
| CA2761576C (en) | 2009-05-20 | 2017-08-22 | Boehringer Ingelheim Vetmedica Gmbh | Oral suspension comprising telmisartan |
| EP2448576A2 (en) | 2009-07-02 | 2012-05-09 | Mahmut Bilgic | Solubility enhancing pharmaceutical composition |
| WO2011002425A2 (en) | 2009-07-02 | 2011-01-06 | Bilgig Mahmut | Pharmaceutical composition increasing solubility and stability |
| EA025946B1 (en) | 2010-10-27 | 2017-02-28 | Крка, Товарна Здравил, Д. Д., Ново Место | Multilayer pharmaceutical composition comprising telmisartan and amlodipine |
| EA031602B1 (en) | 2011-11-25 | 2019-01-31 | Адверио Фарма Гмбх | Processes for preraring aldehydes |
| CN111888368B (en) | 2014-10-21 | 2024-02-02 | 武田药品工业株式会社 | Crystalline forms of 5-chloro-N4- [2- (dimethylphosphoryl) phenyl ] -N2- { 2-methoxy-4- [4- (4-methylpiperazin-1-yl) piperidin-1-yl ] phenyl } pyrimidine-2, 4-diamine |
| KR101872726B1 (en) * | 2016-07-28 | 2018-06-29 | 주식회사 씨트리 | Telmisartan methanesulfonate and pharmaceutical composition comprising the same |
| NZ759782A (en) | 2017-07-07 | 2023-06-30 | Boehringer Ingelheim Vetmedica Gmbh | Angiotensin ii receptor antagonist for the prevention or treatment of systemic diseases in cats |
| US20220098197A1 (en) * | 2019-01-10 | 2022-03-31 | Cspc Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd | Salts of heterocyclic compound and use thereof |
| WO2024240632A1 (en) | 2023-05-24 | 2024-11-28 | Boehringer Ingelheim Vetmedica Gmbh | Combination treatment and/or prevention of cardiac diseases in non-human mammals comprising one or more sglt-2 inhibitors and pimobendan and/or telmisartan |
| TW202508455A (en) | 2023-05-24 | 2025-03-01 | 德商百靈佳殷格翰維美迪加股份有限公司 | Combination treatment and/or prevention of renal diseases and/or hypertension in non-human mammals comprising one or more sglt-2 inhibitors and telmisartan |
| US20250195525A1 (en) | 2023-12-15 | 2025-06-19 | Boehringer Ingelheim Vetmedica Gmbh | Angiotensin ii receptor antagonist for the prevention of systemic diseases in cats |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI9210098B (en) * | 1991-02-06 | 2000-06-30 | Dr. Karl Thomae | Benzimidazoles, drugs with this compounds, and process for their preparation |
| US5594003A (en) * | 1991-02-06 | 1997-01-14 | Dr. Karl Thomae Gmbh | Tetrahydroimidazo[1,2-a]pyridin-2-yl-(benzimidazol-1-yl)-methyl-biphenyls useful as angiotensin-II antagonists |
| US5591762A (en) * | 1991-02-06 | 1997-01-07 | Dr. Karl Thomae Gmbh | Benzimidazoles useful as angiotensin-11 antagonists |
| US6174910B1 (en) * | 1996-02-29 | 2001-01-16 | Novartis Ag | AT1 receptor antagonist for the stimulation of apoptosis |
| DE19901921C2 (en) * | 1999-01-19 | 2001-01-04 | Boehringer Ingelheim Pharma | Polymorphs of telmisartan, process for their preparation and their use in the manufacture of a medicament |
-
2001
- 2001-10-31 DE DE10153737A patent/DE10153737A1/en not_active Ceased
-
2002
- 2002-10-11 HU HU0402391A patent/HUP0402391A3/en not_active Application Discontinuation
- 2002-10-11 CA CA2463146A patent/CA2463146C/en not_active Expired - Fee Related
- 2002-10-11 ES ES02777305T patent/ES2291505T3/en not_active Expired - Lifetime
- 2002-10-11 CN CNB028216202A patent/CN100509789C/en not_active Expired - Fee Related
- 2002-10-11 EA EA200400479A patent/EA007596B1/en not_active IP Right Cessation
- 2002-10-11 PL PL367477A patent/PL211462B1/en unknown
- 2002-10-11 MX MXPA04004013A patent/MXPA04004013A/en active IP Right Grant
- 2002-10-11 ME MEP-436/08A patent/MEP43608A/en unknown
- 2002-10-11 NZ NZ532716A patent/NZ532716A/en not_active IP Right Cessation
- 2002-10-11 IL IL16116502A patent/IL161165A0/en unknown
- 2002-10-11 DE DE50210719T patent/DE50210719D1/en not_active Expired - Lifetime
- 2002-10-11 SI SI200230594T patent/SI1442023T1/en unknown
- 2002-10-11 PT PT02777305T patent/PT1442023E/en unknown
- 2002-10-11 JP JP2003540158A patent/JP5124076B2/en not_active Expired - Lifetime
- 2002-10-11 KR KR1020047006317A patent/KR100929502B1/en not_active Expired - Fee Related
- 2002-10-11 DK DK02777305T patent/DK1442023T3/en active
- 2002-10-11 EP EP02777305A patent/EP1442023B1/en not_active Expired - Lifetime
- 2002-10-11 AU AU2002338886A patent/AU2002338886B2/en not_active Ceased
- 2002-10-11 HR HRP20040372AA patent/HRP20040372A8/en not_active IP Right Cessation
- 2002-10-11 AT AT02777305T patent/ATE370125T1/en active
- 2002-10-11 BR BR0213568-0A patent/BR0213568A/en active Search and Examination
- 2002-10-11 WO PCT/EP2002/011394 patent/WO2003037876A1/en not_active Ceased
- 2002-10-11 RS YUP-363/04A patent/RS50879B/en unknown
- 2002-10-28 PE PE2002001061A patent/PE20030629A1/en not_active Application Discontinuation
- 2002-10-28 UY UY27520A patent/UY27520A1/en not_active Application Discontinuation
- 2002-10-29 TW TW091132070A patent/TWI333419B/en not_active IP Right Cessation
- 2002-10-29 TW TW099114822A patent/TWI341200B/en not_active IP Right Cessation
- 2002-10-29 MY MYPI20024051A patent/MY129741A/en unknown
- 2002-10-30 AR ARP020104113A patent/AR037148A1/en active IP Right Grant
- 2002-11-05 SA SA02230419A patent/SA02230419B1/en unknown
- 2002-11-10 UA UA20040503959A patent/UA82833C2/en unknown
-
2004
- 2004-03-30 IL IL161165A patent/IL161165A/en not_active IP Right Cessation
- 2004-04-27 EC EC2004005089A patent/ECSP045089A/en unknown
- 2004-04-29 NO NO20041758A patent/NO326465B1/en not_active IP Right Cessation
- 2004-05-07 CO CO04042445A patent/CO5580785A2/en not_active Application Discontinuation
-
2007
- 2007-10-15 CY CY20071101332T patent/CY1107504T1/en unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FF | Patent granted | ||
| KB | Patent renewed | ||
| KB | Patent renewed | ||
| MM9K | Patent not in force due to non-payment of renewal fees |