HUP0203132A2 - Eljárás N-[4,5-bisz(metánszulfonil)-2-metil-benzoil]-guanidin-hidroklorid és hidrátja előálítására - Google Patents

Eljárás N-[4,5-bisz(metánszulfonil)-2-metil-benzoil]-guanidin-hidroklorid és hidrátja előálítására

Info

Publication number
HUP0203132A2
HUP0203132A2 HU0203132A HUP0203132A HUP0203132A2 HU P0203132 A2 HUP0203132 A2 HU P0203132A2 HU 0203132 A HU0203132 A HU 0203132A HU P0203132 A HUP0203132 A HU P0203132A HU P0203132 A2 HUP0203132 A2 HU P0203132A2
Authority
HU
Hungary
Prior art keywords
guanidine
bis
methyl
methanesulfonyl
benzoyl
Prior art date
Application number
HU0203132A
Other languages
English (en)
Inventor
Manfred Baumgarth
Hans Markus Bender
Rolf Gericke
Bernhard Ladstetter
Original Assignee
Merck Patent Gmbh
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
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of HUP0203132A2 publication Critical patent/HUP0203132A2/hu
Publication of HUP0203132A3 publication Critical patent/HUP0203132A3/hu
Publication of HU228634B1 publication Critical patent/HU228634B1/hu

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00Sulfones; Sulfoxides
    • C07C317/44Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C315/00Preparation of sulfones; Preparation of sulfoxides
    • C07C315/04Preparation of sulfones; Preparation of sulfoxides by reactions not involving the formation of sulfone or sulfoxide groups
    • 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
    • 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
    • A61P9/06Antiarrhythmics
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C315/00Preparation of sulfones; Preparation of sulfoxides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (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)
  • Cardiology (AREA)
  • Public Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

A találmány szerinti NHE-1 szelektív Na+/H+-antiporter inhibitorhatású N-[4,5-bisz(metánszulfonil)-2-metil- benzoil]-guanidin-hidroklorid és -hidroklorid-hidrát előállítására 2-metil-4-halogén-5-metilszulfonil-benzoesavat - ahol halogén jelentése fluor- vagybrómatom- metánszulfináttal reagáltatva 2-metil-4,5-bisz(metilszulfonil)-benzoesavvá, majd ezt savkloriddá alakítják ésguanidinnel reagáltatják N-[4,5-bisz(metánszulfonil)-2-metilbenzoil]-guanidin előállítására, majd az így kapott vegyületet vizes sósavvalreagáltatva nyerik a célterméke(ke)t. Ó
HU0203132A 1999-10-26 2000-10-11 Method of producing n-[4,5-bis-methanesulfonyl-2-methyl-benzoyl)-guanidine, hydrochloride HU228634B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19951418A DE19951418A1 (de) 1999-10-26 1999-10-26 Verfahren zur Herstellung von N-(4,5-Bismethansulfonyl-2-methyl-benzoyl) -guanidin, Hydrochlorid
PCT/EP2000/009977 WO2001030750A1 (de) 1999-10-26 2000-10-11 Verfahren zur herstellung von n-(4,5-bis-methansulfonyl-2-methyl-benzoyl)-guanidin, hydrochlorid

Publications (3)

Publication Number Publication Date
HUP0203132A2 true HUP0203132A2 (hu) 2003-01-28
HUP0203132A3 HUP0203132A3 (en) 2004-12-28
HU228634B1 HU228634B1 (en) 2013-04-29

Family

ID=7926842

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0203132A HU228634B1 (en) 1999-10-26 2000-10-11 Method of producing n-[4,5-bis-methanesulfonyl-2-methyl-benzoyl)-guanidine, hydrochloride

Country Status (26)

Country Link
US (1) US6673968B1 (hu)
EP (1) EP1224166B1 (hu)
JP (1) JP4969750B2 (hu)
KR (1) KR100699571B1 (hu)
CN (1) CN1202078C (hu)
AT (1) ATE250026T1 (hu)
AU (1) AU782471B2 (hu)
BR (1) BR0015022A (hu)
CA (1) CA2388915C (hu)
CZ (1) CZ299201B6 (hu)
DE (2) DE19951418A1 (hu)
DK (1) DK1224166T3 (hu)
ES (1) ES2204712T3 (hu)
HK (1) HK1051358A1 (hu)
HU (1) HU228634B1 (hu)
MX (1) MXPA02004144A (hu)
MY (1) MY122651A (hu)
NO (1) NO328250B1 (hu)
PL (1) PL199010B1 (hu)
PT (1) PT1224166E (hu)
RU (1) RU2276134C2 (hu)
SI (1) SI1224166T1 (hu)
SK (1) SK286603B6 (hu)
UA (1) UA73329C2 (hu)
WO (1) WO2001030750A1 (hu)
ZA (1) ZA200204119B (hu)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10023405A1 (de) * 2000-05-12 2001-11-15 Merck Patent Gmbh Verfahren zur Herstellung von Sulfonyl-benzoylguanidinum-Salzen
US7629493B2 (en) * 2003-05-06 2009-12-08 Merck Patent Gmbh Process for the crystallisation of guandinium salts
AU2009243749B2 (en) 2008-05-09 2013-11-21 Merck Patent Gmbh Pharmaceutical composition comprising rimeporide for treating diseases associated with insulin resistance and beta-cell dysfunction
JOP20200296A1 (ar) * 2013-06-10 2017-06-16 Amgen Inc عمليات صنع وأشكال بلورية من mdm2 مثبط
JP6562221B2 (ja) * 2014-06-23 2019-08-21 日産化学株式会社 スルホニル結合を有するシラン化合物の製造方法
MX2018009558A (es) * 2016-02-08 2018-09-06 Merck Patent Gmbh Modificaciones cristalinas de clorhidrato de n-(4,5-bismetansulfon il-2-metilbenzoil)guanidina y sales de n-(4,5-bismetansulfonil-2-m etilbenzoil)guanidina.
EP3960165A1 (en) * 2020-08-25 2022-03-02 Fondation EspeRare Nhe-1 inhibitors for the treatment of coronavirus infections

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS59216865A (ja) * 1983-05-26 1984-12-06 Mitsui Toatsu Chem Inc システイン塩酸塩水和物の乾燥方法
DE3929582A1 (de) * 1989-09-06 1991-03-07 Hoechst Ag Benzoylguanidine, verfahren zu ihrer herstellung, ihre verwendung als medikament sowie sie enthaltendes medikament
EP0589336B1 (de) * 1992-09-22 1997-01-08 Hoechst Aktiengesellschaft Benzoylguanidine, Verfahren zu ihrer Herstellung, sowie ihre Verwendung als Antiarrhythmika
EP0604852A1 (de) * 1992-12-28 1994-07-06 Hoechst Aktiengesellschaft 2,4-Substituierte 5-(N-substituierte-Sulfamoyl)-Benzoylguanidine, als Antiarrythmika, Inhibitoren der Proliferationen von Zellen, und Inhibitoren des Natrium-Protonen-Antiporters
JPH07206857A (ja) * 1993-12-28 1995-08-08 Synthelabo Sa アルフゾシン塩酸塩の二水和物
JP3755908B2 (ja) * 1994-08-17 2006-03-15 塩野義製薬株式会社 セファロスポリン化合物の晶析法
ATE185557T1 (de) * 1995-01-30 1999-10-15 Hoechst Ag Basisch-substituierte benzoylguanidine, verfahren zu ihrer herstellung, ihre verwendung als medikament oder diagnostikum sowie sie enthaltendes medikament
DE19502895A1 (de) * 1995-01-31 1996-08-01 Merck Patent Gmbh 4-Mercapto-benzoylguanidin-Derivate
DE19529612A1 (de) * 1995-08-11 1997-02-13 Merck Patent Gmbh Sulfonyl- oder Sulfinyl-benzoylguanidin-Derivate

Also Published As

Publication number Publication date
NO20021950L (no) 2002-04-25
ATE250026T1 (de) 2003-10-15
ES2204712T3 (es) 2004-05-01
SI1224166T1 (en) 2004-04-30
WO2001030750A1 (de) 2001-05-03
JP4969750B2 (ja) 2012-07-04
US6673968B1 (en) 2004-01-06
HU228634B1 (en) 2013-04-29
PL199010B1 (pl) 2008-08-29
CZ299201B6 (cs) 2008-05-14
HUP0203132A3 (en) 2004-12-28
CA2388915A1 (en) 2001-05-03
UA73329C2 (uk) 2005-07-15
AU1136101A (en) 2001-05-08
AU782471B2 (en) 2005-08-04
DE19951418A1 (de) 2001-05-03
HK1051358A1 (en) 2003-08-01
JP2003512451A (ja) 2003-04-02
MY122651A (en) 2006-04-29
PL355149A1 (en) 2004-04-05
BR0015022A (pt) 2002-06-18
DK1224166T3 (da) 2004-01-05
SK5462002A3 (en) 2002-10-08
NO328250B1 (no) 2010-01-18
RU2276134C2 (ru) 2006-05-10
PT1224166E (pt) 2004-02-27
MXPA02004144A (es) 2006-01-12
KR100699571B1 (ko) 2007-03-23
SK286603B6 (sk) 2009-02-05
ZA200204119B (en) 2003-10-29
CN1382120A (zh) 2002-11-27
DE50003759D1 (de) 2003-10-23
CZ20021354A3 (cs) 2002-09-11
EP1224166A1 (de) 2002-07-24
EP1224166B1 (de) 2003-09-17
CA2388915C (en) 2009-12-15
CN1202078C (zh) 2005-05-18
KR20020044572A (ko) 2002-06-15
NO20021950D0 (no) 2002-04-25

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MM4A Lapse of definitive patent protection due to non-payment of fees