DK151018C - METHOD OF ANALOGUE FOR THE PREPARATION OF BENZOXAZOLYL OR BENZTHIAZOLYL-4,5-DIHYDRO-3 (2H) -PYRIDAZINONES OR THEIR OPTICALLY ACTIVE ANTIPODES OR THEIR ADDITIONAL SALTS WITH ACIDS - Google Patents

METHOD OF ANALOGUE FOR THE PREPARATION OF BENZOXAZOLYL OR BENZTHIAZOLYL-4,5-DIHYDRO-3 (2H) -PYRIDAZINONES OR THEIR OPTICALLY ACTIVE ANTIPODES OR THEIR ADDITIONAL SALTS WITH ACIDS

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Publication number
DK151018C
DK151018C DK073781A DK73781A DK151018C DK 151018 C DK151018 C DK 151018C DK 073781 A DK073781 A DK 073781A DK 73781 A DK73781 A DK 73781A DK 151018 C DK151018 C DK 151018C
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Prior art keywords
carbon atoms
substituted
group
general formula
hydrogen atom
Prior art date
Application number
DK073781A
Other languages
Danish (da)
Other versions
DK73781A (en
DK151018B (en
Inventor
Norbert Hauel
Herbert Stein
Joachim Heider
Volkhard Austel
Manfred Reiffen
Willi Diederen
Walter Haarmann
Original Assignee
Thomae Gmbh Dr K
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.)
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Publication date
Application filed by Thomae Gmbh Dr K filed Critical Thomae Gmbh Dr K
Publication of DK73781A publication Critical patent/DK73781A/en
Publication of DK151018B publication Critical patent/DK151018B/en
Application granted granted Critical
Publication of DK151018C publication Critical patent/DK151018C/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58Benzoxazoles; Hydrogenated benzoxazoles 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 in position 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C205/00Compounds containing nitro groups bound to a carbon skeleton
    • C07C205/49Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups
    • C07C205/56Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups bound to carbon atoms of six-membered aromatic rings and carboxyl groups bound to acyclic carbon atoms of the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40Unsaturated compounds
    • C07C59/76Unsaturated compounds containing keto groups
    • C07C59/84Unsaturated compounds containing keto groups containing six membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/04Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having less than three double bonds between ring members or between ring members and non-ring members

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Polymerisation Methods In General (AREA)
  • Eyeglasses (AREA)
  • Macromonomer-Based Addition Polymer (AREA)

Abstract

1. Claims for the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL Benzoxazoles of general formula see diagramm : EP0034743,P9,F2 in which R1 represents a hydrogen atom ; a straight or branched alkyl group with 1 to 7 carbon atoms which can be substituted by an alkoxy group with 1 to 3 carbon atoms ; a cycloalkyl group with 3 to 7 carbon atoms ; an alkyl group with 1 to 3 carbon atoms substituted by a phenyl group which can be substituted by one or two alkoxy groups with 1 to 3 carbon atoms ; or a phenyl group which can be substituted by an alkyl or alkoxy group each with 1 to 3 carbon atoms, by a trifluormethyl, nitro or cyano group or by a fluorine, chlorine or bromine atom ; and in addition one of the mono-substituted phenyl groups mentioned above can be substituted by one or two alkyl groups with 1 to 3 carbon atoms or by an alkoxy group with 1 to 3 carbon atoms or by a fluorine, chlorine or bromine atom ; and R2 represents a hydrogen atom or an alkyl group with 1 to 3 carbon atoms ; and their optically active antipodes as well as their physiologically compatible acid addition salts with inorganic or organic acids. 1. Claims for the Contracting State : AT Process for producing benzoxazoles of general formula see diagramm : EP0034743,P10,F4 in which R1 represents a hydrogen atom ; a straight or branched alkyl group with 1 to 7 carbon atoms which can be substituted by an alkoxy group with 1 to 3 carbon atoms ; a cycloalkyl group with 3 to 7 carbon atoms ; an alkyl group with 1 to 3 carbon atoms substituted by a phenyl group which can be substituted by one or two alkoxy groups with 1 to 3 carbon atoms ; or a phenyl group which can be substituted by an alkyl or alkoxy group each with 1 to 3 carbon atoms, by a trifluormethyl, nitro or cyano group or by a fluorine, chlorine or bromine atom ; and additionally one of the mono-substituted phenyl groups mentioned above can be substituted by one or two alkyl groups with 1 to 3 carbon atoms or by an alkoxy group with 1 to 3 carbon atoms or by a fluorine, chlorine or bromine atom ; and R2 represents a hydrogen atom or an alkyl group with 1 to 3 carbon atoms ; and their optically active antipodes as well as their physiologically compatible acid addition salts with inorganic or organic acids characterised in that see diagramm : EP0034743,P11,F1 in which R1 and R2 are as defined in the introduction, X represents a mercapto, alkylmercapto, arylmercapto or aralkylmercapto group, and Y represents a hydrogen atom or an acyl radical, is cyclised ; or b) a carboxylic acid of general formula see diagramm : EP0034743,P11,F3 in which R1 and R2 are as defined in the introduction, or its amides, esters, thioester or halides, is reacted with hydrazine ; and if desired a compound of general formula I, in which R1 represents a hydrogen atom, obtained according to processes a) or b) is subsequently converted by means of alkylation into a corresponding compound of general formula I, in which R1 is defined as in the introduction with the exception of the hydrogen atom and the phenyl radicals mentioned in the introduction, and/or a racemate obtained, of general formula I, is separated by means of racemate separation into its optically active antipodes, and/or a compound obtained, of general formula I, is converted into its physiologically compatible acid addition salts with inorganic or organic acids.
DK073781A 1980-02-22 1981-02-19 METHOD OF ANALOGUE FOR THE PREPARATION OF BENZOXAZOLYL OR BENZTHIAZOLYL-4,5-DIHYDRO-3 (2H) -PYRIDAZINONES OR THEIR OPTICALLY ACTIVE ANTIPODES OR THEIR ADDITIONAL SALTS WITH ACIDS DK151018C (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19803006671 DE3006671A1 (en) 1980-02-22 1980-02-22 NEW BENZOXAZOLES, THEIR PRODUCTION AND THEIR USE AS MEDICINAL PRODUCTS
DE3006671 1980-02-22

Publications (3)

Publication Number Publication Date
DK73781A DK73781A (en) 1981-08-23
DK151018B DK151018B (en) 1987-10-12
DK151018C true DK151018C (en) 1988-06-20

Family

ID=6095308

Family Applications (1)

Application Number Title Priority Date Filing Date
DK073781A DK151018C (en) 1980-02-22 1981-02-19 METHOD OF ANALOGUE FOR THE PREPARATION OF BENZOXAZOLYL OR BENZTHIAZOLYL-4,5-DIHYDRO-3 (2H) -PYRIDAZINONES OR THEIR OPTICALLY ACTIVE ANTIPODES OR THEIR ADDITIONAL SALTS WITH ACIDS

Country Status (19)

Country Link
EP (1) EP0034743B1 (en)
JP (1) JPS56131581A (en)
AT (1) ATE7696T1 (en)
AU (1) AU543524B2 (en)
CA (1) CA1166252A (en)
DE (2) DE3006671A1 (en)
DK (1) DK151018C (en)
ES (3) ES8206519A1 (en)
FI (1) FI73426C (en)
GR (1) GR74154B (en)
HK (1) HK50785A (en)
IE (1) IE51012B1 (en)
IL (1) IL62181A (en)
NO (1) NO157895C (en)
NZ (1) NZ196313A (en)
PH (1) PH21232A (en)
PT (1) PT72546B (en)
SG (1) SG885G (en)
ZA (1) ZA811130B (en)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1199027A (en) * 1981-11-12 1986-01-07 Stuart D. Mills Heterocyclic derivatives of pyridazinone, thiadiazinone, oxadiazinone and triazinone
WO1996025157A1 (en) 1995-02-17 1996-08-22 Smithkline Beecham Corporation Il-8 receptor antagonists
US6262113B1 (en) 1996-03-20 2001-07-17 Smithkline Beecham Corporation IL-8 receptor antagonists
US6211373B1 (en) 1996-03-20 2001-04-03 Smithkline Beecham Corporation Phenyl urea antagonists of the IL-8 receptor
TR199802694T2 (en) * 1996-06-27 1999-03-22 Smithkline Beecham Corporation IL-8 resept�r kar��tlar�
TR199802695T2 (en) 1996-06-27 1999-04-21 Smithkline Beecham Corporation IL-8 Resett�r kar��tlar�
UY32138A (en) 2008-09-25 2010-04-30 Boehringer Ingelheim Int SUBSTITUTED AMIDES 2- (2,6-DICLORO-PHENYLAMINE) -6-FLUORO-1-METHYL-1H-BENCIMIDAZOL-5-CARBOXYL AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS
UY32470A (en) 2009-03-05 2010-10-29 Boehringer Ingelheim Int DERIVATIVES OF 2- {2-CHLORINE-5 - [(REPLACED) METHYL] PHENYLAMINE} -1-METHYL] PHENYLAMINE} -1-METHYLBENCIMIDAZOL-5-CARBOXAMIDES-N- (SUBSTITUTED) AND ITS PHYSIOLOGICALLY ACCEPTABLE SALTS, COMPOSITIONS AND APPLIANCE
US8586604B2 (en) 2010-08-20 2013-11-19 Boehringer Ingelheim International Gmbh Inhibitors of the microsomal prostaglandin E2 synthase-1
US8759537B2 (en) 2010-08-20 2014-06-24 Boehringer Ingelheim International Gmbh 3H-imidazo [4, 5-C] pyridine-6-carboxamides as anti-inflammatory agents
US8486968B2 (en) 2010-12-10 2013-07-16 Boehringer Ingelheim International Gmbh Compounds
US8466186B2 (en) 2010-12-10 2013-06-18 Boehringer Ingelheim International Gmbh Compounds
UY33779A (en) 2010-12-10 2012-07-31 Boehringer Ingelheim Int ? 2- (Phenylamino) -1H-benzimidazol-5-carboxamides novel?

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2516040C2 (en) * 1974-06-10 1984-12-20 Dr. Karl Thomae Gmbh, 7950 Biberach Benzimidazoles, processes for their preparation and pharmaceuticals containing them
DE2436279A1 (en) * 1974-07-27 1976-02-12 Henkel & Cie Gmbh Imidazoline and tetrahydropyrimidine derivs - prepd e.g. by reacting 2-cyano-benzoxazoles with alkylene diamines

Also Published As

Publication number Publication date
NO810586L (en) 1981-08-24
AU543524B2 (en) 1985-04-26
IL62181A0 (en) 1981-03-31
EP0034743B1 (en) 1984-05-30
SG885G (en) 1985-11-15
IL62181A (en) 1984-10-31
PT72546A (en) 1981-03-01
EP0034743A1 (en) 1981-09-02
IE810343L (en) 1981-08-22
ES8302699A1 (en) 1983-01-16
ES509532A0 (en) 1983-01-16
NO157895C (en) 1988-06-08
JPS6334154B2 (en) 1988-07-08
DE3163797D1 (en) 1984-07-05
NZ196313A (en) 1984-07-06
GR74154B (en) 1984-06-06
DE3006671A1 (en) 1981-08-27
ES509533A0 (en) 1983-01-16
PT72546B (en) 1982-10-21
JPS56131581A (en) 1981-10-15
DK73781A (en) 1981-08-23
ES499378A0 (en) 1982-08-16
HK50785A (en) 1985-07-12
IE51012B1 (en) 1986-09-03
ATE7696T1 (en) 1984-06-15
CA1166252A (en) 1984-04-24
NO157895B (en) 1988-02-29
ES8206519A1 (en) 1982-08-16
AU6751981A (en) 1981-08-27
FI73426B (en) 1987-06-30
DK151018B (en) 1987-10-12
ZA811130B (en) 1982-10-27
ES8302700A1 (en) 1983-01-16
FI73426C (en) 1987-10-09
FI810535L (en) 1981-08-23
PH21232A (en) 1987-08-21

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