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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 antagonist

Info

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
Application number
IL161165A
Original Assignee
Boehringer Ingelheim Pharma
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=7704331&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=IL161165(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Pharma filed Critical Boehringer Ingelheim Pharma
Publication of IL161165A publication Critical patent/IL161165A/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/20Two benzimidazolyl-2 radicals linked together directly or via a hydrocarbon or substituted hydrocarbon radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

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)

Patent Claims
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:
IL161165A 2001-10-31 2004-03-30 Crystalline sodium salt of telmisartan and the use of the same as an angiotensin antagonist IL161165A (en)

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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

Also Published As

Publication number Publication date
MY129741A (en) 2007-04-30
WO2003037876A1 (en) 2003-05-08
EP1442023A1 (en) 2004-08-04
EA200400479A1 (en) 2004-10-28
NO326465B1 (en) 2008-12-08
CA2463146C (en) 2011-01-25
ATE370125T1 (en) 2007-09-15
TWI333419B (en) 2010-11-21
AU2002338886B2 (en) 2008-04-17
ECSP045089A (en) 2004-06-28
TW200300082A (en) 2003-05-16
HRP20040372A2 (en) 2004-10-31
KR100929502B1 (en) 2009-12-03
DE10153737A1 (en) 2003-05-28
DK1442023T3 (en) 2007-11-05
JP2005536445A (en) 2005-12-02
HUP0402391A3 (en) 2010-03-29
UA82833C2 (en) 2008-05-26
IL161165A0 (en) 2004-08-31
EP1442023B1 (en) 2007-08-15
MEP43608A (en) 2011-02-10
UY27520A1 (en) 2003-05-30
CY1107504T1 (en) 2013-03-13
HRPK20040372B4 (en) 2025-09-12
PT1442023E (en) 2007-09-17
HK1073841A1 (en) 2005-10-21
TW201034664A (en) 2010-10-01
KR20050035172A (en) 2005-04-15
CN1578772A (en) 2005-02-09
PL367477A1 (en) 2005-02-21
TWI341200B (en) 2011-05-01
SA02230419B1 (en) 2007-07-31
CO5580785A2 (en) 2005-11-30
BR0213568A (en) 2004-09-08
CA2463146A1 (en) 2003-05-08
EA007596B1 (en) 2006-12-29
DE50210719D1 (en) 2007-09-27
MXPA04004013A (en) 2004-06-18
HUP0402391A2 (en) 2005-03-29
AR037148A1 (en) 2004-10-27
JP5124076B2 (en) 2013-01-23
PE20030629A1 (en) 2003-07-14
HRP20040372A8 (en) 2025-09-12
NO20041758L (en) 2004-04-29
RS50879B (en) 2010-08-31
CN100509789C (en) 2009-07-08
SI1442023T1 (en) 2007-12-31
PL211462B1 (en) 2012-05-31
ES2291505T3 (en) 2008-03-01
NZ532716A (en) 2007-06-29
HRPK20040372B3 (en) 2006-02-28
YU36304A (en) 2006-08-17

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