Polycyclo Ring System Having The Thiazole Ring As One Of The Cyclos Patents (Class 514/366)
  • Patent number: 4929623
    Abstract: A benzothiazol compound having the formula is disclosed and is effective to inhibit the production of leukotriene. It is useful against allergy, asthma, affections of the skin, allergic rhinitis and affection of a cardiovascular system. ##STR1## in which R20 is ester or amide and --NR5R6 is amino in variety.
    Type: Grant
    Filed: June 16, 1988
    Date of Patent: May 29, 1990
    Assignee: Eisai Co., Ltd.
    Inventors: Shinya Abe, Mitsuaki Miyamoto, Masayuki Tanaka, Kozo Akasaka, Kenji Hayashi, Tetsuya Kawahara, Satoshi Katayama, Yoshinori Sakuma, Takeshi Suzuki, Isao Yamatsu
  • Patent number: 4929636
    Abstract: The invention relates to compounds of the general formula I ##STR1## wherein R.sub.1 represents one up to and including four, the same or different substituents selected from alkyl(1-6 C), alkoxy(1-6 C), hydroxy, halogen, NO.sub.2, CF.sub.3 or the group --NR.sub.5 R.sub.6, whereby two substituents taken together may also represent a methylene-dioxy group,X represents nitrogen or the group ##STR2## n has the value 0, 1 or 2, R.sub.3 represents one of the moieties: ##STR3## the latter meaning of R.sub.3 (amide) only under the condition that for X is nitrogen the meaning of R.sub.1 is limited to substituents selected from hydroxy, alkoxy(1-6 C) and methylenedioxy, and R.sub.4, R.sub.5 and R.sub.6 represent hydrogen or alkyl(1-6 C), and pharmaceutically acceptable salts thereof, suitable in the treatment of heart failure.
    Type: Grant
    Filed: April 6, 1989
    Date of Patent: May 29, 1990
    Assignee: Akzo N.V.
    Inventors: James Redpath, Robert T. Logan, David B. McFadzen, Robert G. Roy
  • Patent number: 4895863
    Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of ##STR2## R.sub.4, R.sub.5, R.sub.7 and R.sub.8 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, R.sub.6 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, phenyl, halogen, alkoxycarbonyl of 2 to 5 carbon atoms, cyano, ##STR3## R' and R" are individually alkyl of 1 to 5 carbon atoms, R.sub.2 and R.sub.3 together form a member of the group consisting of ##STR4## m is 1, 2 or 3, X.sub.1 and X.sub.2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, alkenyl of 2 to 5 carbon atoms, alkoxy of 1 to 5 carbon atoms, aralkoxy, aryloxy, halogen, azido and nitro or taken together form methylenedioxy and their non-toxic, pharmaceutically acceptable acid additon salts capable of treating memory disorders.
    Type: Grant
    Filed: October 18, 1988
    Date of Patent: January 23, 1990
    Assignee: Roussel Uclaf
    Inventors: Charles J. R. Hedgecock, David P. Kay
  • Patent number: 4880824
    Abstract: Heterocyclic compounds of formulae (I) and (II): ##STR1## where R.sup.1 and R.sup.2 are alkyl, R.sup.3 is H or alkyl, m is 2-5 and Het is a hetercycle such as thiazole, benzothiazole, substituted benzothiazole, pyrazine, triazine, thiadiazole, substituted thiadiazole, pyrimidine or substituted pyrimidine. The compounds are calcium channel blockers useful in the treatment of cardiovascular conditions such as hypertension or angina.
    Type: Grant
    Filed: September 21, 1987
    Date of Patent: November 14, 1989
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffery B. Press, Maud Urbanski
  • Patent number: 4873237
    Abstract: The invention relates to a method of treatment of ulcers or hypersecretion in a mammal which comprises administering a compound of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein --B--B.sup.1 -- represents a chain of formula--(CHR.sup.5).sub.n --CHR.sup.6 -- (Ia)R represents an optionally substituted aryl or heteroaryl radical,R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, or a defined substituent or any adjacent pair of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached complete a five or six membered saturated or unsaturated carbocyclic or heterocyclic ring, said ring being optionally substituted by a defined substituent and said heterocyclic ring having at least one heteroatom selected from oxygen, nitrogen and sulphur;R.sup.5 and R.sup.
    Type: Grant
    Filed: May 22, 1986
    Date of Patent: October 10, 1989
    Assignee: John Wyeth & Brother Limited
    Inventor: Roger Crossley
  • Patent number: 4863930
    Abstract: 5H-pyrido[2',1':2,3]imidazo[4,5-b]indoles of the formulae ##STR1## their pharmaceutically acceptable acid addition salts and the corresponding compounds bearing one or more halogens and/or lower-alkyl groups on the available ring carbon atoms are administered in cholinomimetic amounts to mammals with low acetylcholine or cholinergic activity to ameliorate the symptoms associated with that condition.
    Type: Grant
    Filed: December 19, 1986
    Date of Patent: September 5, 1989
    Inventor: Parimal K. Adhikary
  • Patent number: 4835167
    Abstract: The present invention provides new tricyclic benzotriazoles of the general formula: ##STR1## wherein Z is a hydrogen atom or an acyl radical, Y is an oxygen or sulphur atom or two hydrogen atoms and X is an oxygen or sulphur atom or a >CR.sub.1 R.sub.2 or >NR.sub.3 group, R.sub.1 is a hydrogen atom or an alkyl, alkenyl or cycloalkyl radical, R.sub.2 is a hydrogen atom or an alkyl, alkenyl or cyano group or a carbonyl group substituted by a hydroxyl, alkyl, alkoxy, amino, alkylamino, dialkylamino or hydrazino group or R.sub.2, together with R.sub.1, represents a cycloalkylene radical or R.sub.1 and R.sub.2 together form an alkylidene or cycloalkylidene radical and R.sub.3 is a hydrogen atom or an alkyl radical; the tautomers thereof and the physiologically acceptable acid-addition salts thereof with inorganic and organic acids.
    Type: Grant
    Filed: August 3, 1987
    Date of Patent: May 30, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Wolfgang Von Der Saal, Walter-Gunar Friebe, Alfred Mertens, Bernd Muller-Beckmann, Gisbert Sponer
  • Patent number: 4831032
    Abstract: The present invention provides benzimidazoles of the general formula: ##STR1## wherein R.sub.1, X, A, and R.sub.2 are as defined in the specification. The present invention also provides processes for the preparation of these new benzimidazoles and pharmaceutical compositions containing them, as well as intermediates for the preparation thereof.The new benzimidazoles are useful to treat heart or circulatory diseases which respond to a lowering of blood pressure, a positive inotropic action and/or an improvement in microcirculation.
    Type: Grant
    Filed: July 3, 1986
    Date of Patent: May 16, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Wolfgang von der Saal, Alfred Mertens, Herbert Berger, Bernd Muller-Beckmann, Klaus Strein
  • Patent number: 4829077
    Abstract: Compounds of formula ##STR1## (wherein R and R.sub.1 have the meanings reported in the specification) and their preparation are described.The compounds of formula I have anti-allergic, anti-anaphylactic and anti-arthritic activity and are useful in pharmaceutical field.Compositions for pharmaceutical use containing a compound of formula I as active ingredient are described too.
    Type: Grant
    Filed: March 23, 1988
    Date of Patent: May 9, 1989
    Assignee: Zambon Group S.p.A.
    Inventors: Dario Chiarino, Gian C. Grancini, Viviana Frigeni, Angelo Carenzi
  • Patent number: 4814329
    Abstract: The invention relates to novel, sulfur-containing 5-substituted benzimidazole derivatives of formula I ##STR1## and acid-addition salts thereof antihyperlipoproteinemic action, a process for preparing the same, pharmaceutical formulations comprising the novel compound as active ingredient and a method for inhibiting atherosclerosis, trombus formation and treating hyperlipoproteinemic diseases.
    Type: Grant
    Filed: March 17, 1986
    Date of Patent: March 21, 1989
    Assignee: Richter Gedeon Vegyeszeti Gyar R.T.
    Inventors: Kalmen Harsanyi, Andrea Maderspach, Andres Javor, Gyorgy Hajos, Gyorgy Fekete, Laslo Szporny, Peter Tetenyi, Katalin Csomor, Egon Karpati, Bela Hegedus, Marta Kapolnas nee Pap, Marta Szollosy, Anna Kallay nee Sohonyai
  • Patent number: 4794123
    Abstract: This invention relates to a method of treating ulcers or hypersecretion in a mammal which comprises administering a compound of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein --B--B.sup.1 -- represents a chain of formula--CR.sup.5 .dbd.CR.sup.6 -- (Ib)or--(CHR.sup.5).sub.n --CR.sup.6 .dbd. (Ic);R represents an optionally substituted aryl or heteroaryl radical; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, or a defined substituent or any adjacent pair of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached complete a five or six membered saturated or unsaturated carbocyclic or heterocyclic ring, said ring being optionally substituted by a defined substituent said heterocyclic ring having at least one heteroatom selected from oxygen, nitrogen and sulphur. Novel compositions and compounds of formula I are also disclosed.
    Type: Grant
    Filed: October 13, 1987
    Date of Patent: December 27, 1988
    Assignee: John Wyeth & Brother Limited
    Inventors: Roger Crossley, Peter J. Meade
  • Patent number: 4767775
    Abstract: Microbicidal substituted pyrazolin-5-ones of the formula ##STR1## in which R.sup.1 and R.sup.2 independently of one another each represent hydrogen, alkyl, alkenyl, alkinyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxycarbonyl, hydroxycarbonylalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, alkylaminocarbonylalkyl or dialkylaminocarbonylalkyl, or represent in each case optionally substituted oxiranylalkyl, aralkyl, heterocyclyl or aryl andHet represents an optionally substituted heterocyclic radical.Intermediates therefor of the formula ##STR2## in which R is alkyl, are also disclosed.
    Type: Grant
    Filed: July 24, 1986
    Date of Patent: August 30, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Jelich, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
  • Patent number: 4730003
    Abstract: The present invention provides compounds of the general formula: ##STR1## wherein the various substituents are defined hereinbelow. The compounds are used for the treatment and/or prophylaxis of heart and circulatory diseases.
    Type: Grant
    Filed: September 4, 1986
    Date of Patent: March 8, 1988
    Assignee: Boehringer Mannheim GmbH
    Inventors: Wolfgang von der Saal, Alfred Mertens, Herbert Berger, Bernd Muller-Beckmann
  • Patent number: 4725605
    Abstract: This invention relates to a method of treating ulcers or hypersecretion in a mammal which comprises administering a compound of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein --B--B.sup.1 -- represents a chain of formula--CR.sup.5 .dbd.CR.sup.6 -- (Ib)or--(CHR.sup.5).sub.n --CR.sup.6 .dbd. (Ic);R represents an optionally substituted aryl or heteroaryl radical; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, or a defined substituent or any adjacent pair of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached complete a five or six membered saturated or unsaturated carbocyclic or heterocyclic ring, said ring being optionally substituted by a defined substituent said heterocyclic ring having at least one heteroatom selected from oxygen, nitrogen and sulphur. Novel compositions and compounds of formula I are also disclosed.
    Type: Grant
    Filed: May 22, 1986
    Date of Patent: February 16, 1988
    Assignee: John Wyeth & Brother Limited
    Inventors: Roger Crossley, Peter J. Meade
  • Patent number: 4695571
    Abstract: Tricyclic oxindole carboxamides, prepared by (a) reaction of an isocyanate with the basic ring system or (b) ammonolysis of a corresponding alkyl ester, are non-steroidal antiinflammatory agents useful in the treatment of rheumatoid arthritis.
    Type: Grant
    Filed: April 2, 1986
    Date of Patent: September 22, 1987
    Assignee: Pfizer Inc.
    Inventor: Lawrence S. Melvin
  • Patent number: 4666913
    Abstract: A method for increasing cardiotonic contractility in humans or other animals using a class of hydroxy and aminothiazolyl-benzodiazinone compounds and pharmaceutical compositions including the same.
    Type: Grant
    Filed: November 22, 1985
    Date of Patent: May 19, 1987
    Assignee: William H. Rorer, Inc.
    Inventors: Donald E. Kubla, Henry F. Campbell, William L. Studt, Bruce F. Molino, Thomas J. Tucker
  • Patent number: 4537892
    Abstract: Disclosed are substituted or unsubstituted planar tricyclic fluorene or nuclear analogs thereof, spiro-coupled to a five-membered ring containing a secondary amide, and the pharmaceutically acceptable salts thereof. These compounds are useful, inter alia, in the treatment of diabetes. Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when indicated for, inter alia, long term, prophylactic treatment of the diabetes syndrome.
    Type: Grant
    Filed: September 14, 1983
    Date of Patent: August 27, 1985
    Assignee: Alcon Laboratories, Inc.
    Inventor: Billie M. York, Jr.