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    Spiro-thiazoloquinazoline derivs - with bactericidal, fungicidal ,anti-inflammatory, analgesic and sedative activity
    1.
    发明专利
    Spiro-thiazoloquinazoline derivs - with bactericidal, fungicidal ,anti-inflammatory, analgesic and sedative activity 未知

    公开(公告)号：DE2212371A1

    公开(公告)日：1973-09-20

    申请号：DE2212371

    申请日：1972-03-15

    Applicant: BASF AG

    Inventor： THIEME PETER DR ,  KOENIG HORST DR ,  AMANN AUGUST DR

    IPC: C07D277/60 ,  C07D513/04 ,  C07D91/42

    Abstract: Thiazoloquinazoline derivs. of formula (I): (where n is 4, 5, 6 or 7; and R' and R2 are H, halogen, lower alkyl, OH, alkoxy, NO2, NH2 or SO3H). Bactericides and fungicides. Also anti-inflammatories, analgesics and sedatives. EXAMPLE A mixture of o-isothiocyanatobenzoic acid methyl ester (5.8 g), 1-ethynyl-cyclohexylamine (3.7 g) and n-PrOH (50 ml) is stirred 1 hr. at room temp., refluxed 2 hrs., cooled, treated with KOH (0.3 g) in H2O (1 ml), refluxed 2 hrs., and evapd. The residue is taken up in CH2Cl2 and the soln. is washed with dilute HCl and water, dried (Na2SO4) and evapd. The residue (8.5 g) is recrystallized from EtOH (charcoal) to give 2-methylene-3-spirocyclohexan-2,3-dihydro-5-oxo-5H-thiazolo- 2,3-- b quinazoline (6.4 g), m.pt. 119-120 degrees.

    Quinazoline derivs prepn - from isocyanatobenzoic acid and propargylamine
    2.
    发明专利
    Quinazoline derivs prepn - from isocyanatobenzoic acid and propargylamine 未知

    公开(公告)号：DE2228259A1

    公开(公告)日：1973-12-20

    申请号：DE2228259

    申请日：1972-06-09

    Applicant: BASF AG

    Inventor： THIEME PETER DR ,  KOENIG HORST DR ,  AMANN AUGUST DR

    IPC: C07D277/42 ,  C07D513/04 ,  C07D91/42

    Abstract: Process comprises reacting a cpd. (I) with a cpd. (II) and cyclising the resulting cpd. (III) to give the 2-methylene-2,3-dihydro-5-oxo- 5H-thiazolo-[21,31-b]quinazoline (IV): (where R1, R2, R3 are H or aliphatic gp., or R3 may be halogen, OH, CF3, alkoxy, alkylthio, NO2, CN, carboxyamido, sulphonic acid gp. or -NR4R4 where each R4 is H or aliphatic gp.). Cpds. (IV) are inflammation preventing agents, analgesics and sedatives, fungicides, bactericides and inters. for pharmaceuticals, dyes and pesticides.

    7.
    发明专利
    未知

    公开(公告)号：CH615430A5

    公开(公告)日：1980-01-31

    申请号：CH211975

    申请日：1975-02-20

    Applicant: BASF AG

    Inventor： AMANN AUGUST DR ,  KOENIG HORST DR ,  THIEME PETER DR ,  GIERTZ HUBERT PROF DR ,  KRETZSCHMAR ROLF DR

    IPC: C07D285/12 ,  A61K31/41 ,  A61K31/433 ,  A61P25/08 ,  C07D285/125

    Abstract: 1494757 1,3,4-Thiadiazolium compounds BASF AG 20 Feb 1975 [21 Feb 1974] 7106/75 Heading C2C The invention comprises novel compounds (I) in which (a) R 2 , R 3 , R 4 , R 5 and R 6 are identical or different and are hydrogen, fluorine, chlorine, bromine, iodine, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms in the alkyl moiety, trifluoromethyl or NO 2 , at least one of the substituents R 2 to R 6 being different from hydrogen, and R 1 is alkyl or 2 to 6 carbon atoms which is optionally substituted by OH, CN, phenyl or cycloalkyl of 3 to 6 carbon atoms in the ring, or (b) R 1 is methyl optionally substituted by phenyl or cycloalkyl of 3 to 6 carbon atoms in the ring when at least two of R 2 to R 6 are different from hydrogen, or, when R 2 , R 3 , R 5 and R 6 have the above meanings, R 4 is hydrogen, fluorine, bromine, iodine, alkyl of 2 to 4 carbon atoms, alkoxy of 2 to 4 carbon atoms in the alkyl moiety, trifluoromethyl or NO 2 and at least one of R 2 , R 3 , R 4 , R 6 and R 6 is different from H, or (c) R 2 , R 3 , R 4 , R 5 and R 6 are each hydrogen when R 1 is alkyl of 3 to 6 carbon atoms which is optionally substituted by OH, CN, phenyl or cycloalkyl of 3 to 6 carbon atoms in the ring or when R 1 is ethyl which is #-substituted by OH, CN, phenyl or cycloalkyl of 3 to 6 carbon atoms in the ring, or (d) R 1 is methyl substituted by cycloalkyl of 3 to 6 carbon atoms in the ring when R 2 , R 3 , R 4 , R 5 and R 6 are each hydrogen or R 2 , R 3 , R 5 and R 6 are hydrogen and R 4 is chlorine. They are made by reacting compounds (II) (obtained by reacting compounds III with R 1 NHNH 2 ; the free acids corresponding to III are also prepared as are compounds IV) with carbon disulphide or thiophosgene. Pharmaceutical preparations having anticonvulsive action contain (I) as active ingredient. Administration is preferably orally.

    8.
    发明专利
    未知

    公开(公告)号：DE2818999A1

    公开(公告)日：1979-11-15

    申请号：DE2818999

    申请日：1978-04-29

    Applicant: BASF AG

    Inventor： THIEME PETER DR ,  FRICKEL FRITZ-FRIEDER DR ,  THEOBALD HANS DR ,  FRANKE ALBRECHT DR ,  LENKE HANS-DIETER PROF DR ,  GRIES JOSEF DR

    IPC: A61K31/41 ,  A61K31/42 ,  A61P9/00 ,  A61P9/06 ,  A61P9/12 ,  A61P25/02 ,  C07D261/08

    Abstract: Alkylamino-propanol derivatives of 3-alkyl-5-(2-hydroxystyryl)-isoxazole, of the general formula where R is hydrogen, alkyl of 1 to 8 carbon atoms, which is unsubstituted or substituted by hydroxyl, alkoxy of 1 to 3 carbon atoms or cycloalkyl with 3 to 8 carbon atoms in the ring, alkenyl or alkynyl of 2 to 8 carbon atoms, or cycloalkyl with 3 to 8 carbon atoms in the ring, the cycloalkyl rings being unsubstituted or mono- or di-substituted by alkyl of 1 to 3 carbon atoms, and R' is alkyl of 1 to 4 carbon atoms, and their addition salts with physiologically acceptable acids, their preparation, and pharmaceutical formulations which contain these compounds and which can be used as valuable drugs in the treatment of hypertonia, coronary diseases of the heart and cardiac arrhythmias.

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