The Additional Hetero Ring Is 1,3-diazine (including Hydrogenated) Patents (Class 540/601)
  • Patent number: 4871387
    Abstract: New pyri(mi)dyl-oxy- or -thio-benzoic acid derivatives of the formula ##STR1## are taught which have herbicidal and plant growth regulating activity. In the formula Z can be Ch or N, X is oxygen or sulphur, A is oxygen, sulphur, a radical R.sup.5 --N.dbd.or a radical R.sup.6 O--N.dbd.and B is oxygen, sulphur, a radical ##STR2## with the proviso that at least one of the radicals R.sup.1, R.sup.2 or R.sup.3 represents alkyl or a part of a 3- to 6-membered fused carbocyclic ring.
    Type: Grant
    Filed: December 4, 1986
    Date of Patent: October 3, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Sasse, Reiner Fischer, Hermann Hagemann, Hans-Joachim Santel, Robert R. Schmidt, Kalus Lurssen
  • Patent number: 4868181
    Abstract: 1,4-Dihydropyridine derivatives which combine both calcium agonist and alpha.sub.1 -antagonist activity are useful in treating congestive heart failure. These derivatives are compounds having the formula: ##STR1## wherein Ar, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are defined in the specification.
    Type: Grant
    Filed: June 30, 1987
    Date of Patent: September 19, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Alexander L. Johnson, Philip Ma, Petrus B. M. W. M. Timmermans, Ruth R. Wexler
  • Patent number: 4855301
    Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is oxygen or sulfur;R is hydrogen, alkyl, cycloalkyl, aryl, or arylalkyl and R.sub.1 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, ##STR2## or halo substituted alkyl, or R and R.sub.1 taken together with the nitrogen atom to which they are attached are 1-pyrrolidinyl, 1-piperidinyl, 1-azepinyl, 4-morpholinyl, 4-thiamorpholinyl, 1-piperazinyl, 4-alkyl-1-piperazinyl, 4-arylalkyl-1-piperazinyl, 4-diarylalkyl-1-piperazinyl or 1-pyrrolidinyl, 1-piperidinyl, or 1-azeipinyl substituted with alkyl, alkoxy, alkylthio, halo, trifluoromethyl or hydroxy;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, ##STR3## or halo substituted alkyl; R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, ##STR4## or halo substituted alkyl; R.sub.4 is aryl or heterocyclo;R.sub.5 and R.sub.6 are each independently hydrogen, alkyl, --(CH.sub.2).sub.q --aryl or --(CH.sub.2).sub.
    Type: Grant
    Filed: February 9, 1987
    Date of Patent: August 8, 1989
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Karnail Atwal, George C. Rovnyak
  • Patent number: 4851406
    Abstract: The present invention provides indole derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl, cycloalkyl, cycloalkenyl, carboxyl, cyano, alkylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl or aryl radical, R.sub.2 is a hydrogen atom or an alkyl, trihalogenomethyl, hydroxyl, cycloalkyl, cyano, carboxyl, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl, alkylaminocarbonyl or dialkylaminocarbonyl radical; R.sub.2 is a heterocyclic five-membered ring containing 1 to 4 heteroatoms or a heterocyclic six-membered ring containing 1 to 5 heteroatoms, the heteroatoms of the five- and six-membered rings being the same or different and being nitrogen, oxygen or sulphur and one or more of the nitrogen atoms optionally carrying an oxygen atom, the said five- and six-membered rings optionally being substituted by one or more alkyl, alkoxy, alkylthio, oxo, hydroxyl, nitro, amino, halogen or cyano groups; or R.sub.
    Type: Grant
    Filed: September 4, 1986
    Date of Patent: July 25, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Alfred Mertens, Wolfgang von der Saal, Walter-Gunar Friebe, Bernd Muller-Beckmann, Gisbert Sponer
  • Patent number: 4849422
    Abstract: New alkylol derivatives are described, which belong to the class having the structure formula ##STR1## where R represents a 5 or 6 membered heterocyclic ring selected among pyridine, pyrimidine, pyrazine, pyridazine, thiophene, furan, thiazole which optionally may be substituted with one or more groups selected among alkyl, alkoxy, halogen, amide, hydroxy, methylthio, trifluoromethyl, cyano, carboxy and the corresponding alkyl esters and salts with alkali metalsn is 2X and X' represent each a hydrogen atom or hydroxy group with the exception of both being hydrogen atom, and X' may be hydroxyethoxy moietym is 0 or 1and the corresponding non-toxic pharmaceutically acceptable acid addition salts. The compounds of the formula I are endowed with an interesting antitussive activity and, at their active dose, practically they are free of undesired side effects.
    Type: Grant
    Filed: January 16, 1987
    Date of Patent: July 18, 1989
    Assignee: Dompe' Farmaceutici S.p.A.
    Inventors: Roberto P. Giani, Salvatore Malandrino, Giancarlo Tonon
  • Patent number: 4847379
    Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein X is oxygen or nitrogen and R.sub.4 is aryl, are disclosed. These novel compounds are useful, for example, as cardiovascular agents.
    Type: Grant
    Filed: November 30, 1987
    Date of Patent: July 11, 1989
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4769371
    Abstract: Pyridine compounds of the formula ##STR1## wherein R.sub.4 is aryl or heterocyclo are disclosed. These compounds are useful as cardiovascular agents due to their calcium entry blocking vasodilator activity.
    Type: Grant
    Filed: May 1, 1987
    Date of Patent: September 6, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4760074
    Abstract: Novel N-(bicyclic heterocyclyl)-4-piperidinamines having antihistaminic and serotonin-antagonistic properties which are useful in the treatment of allergic diseases.
    Type: Grant
    Filed: November 21, 1985
    Date of Patent: July 26, 1988
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans E. Janssens, Jozeph L. G. Torremans, Jozef F. Hens, Theophilus T. J. M. Van Offenwert
  • Patent number: 4753946
    Abstract: Pyridine compounds of the formula ##STR1## wherein R.sub.4 is aryl or heterocyclo are disclosed. These compounds are useful as cardiovascular agents due to their calcium entry blocking vasodilator activity.
    Type: Grant
    Filed: April 8, 1987
    Date of Patent: June 28, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Karnail Atwal, George C. Rovnyak
  • Patent number: 4745110
    Abstract: A class of bicyclic benzenoid aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.
    Type: Grant
    Filed: July 27, 1987
    Date of Patent: May 17, 1988
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
  • Patent number: 4738960
    Abstract: 1,3,4-Thiadiazole derivatives corresponding to the general formula I ##STR1## which constitute highly effective inhibitors for histamine-H.sub.2 receptors are described. These compounds in addition have a cytoprotective action.
    Type: Grant
    Filed: November 19, 1985
    Date of Patent: April 19, 1988
    Assignee: Ludwig Heumann & Co. GmbH
    Inventors: Helmut Schickaneder, Rolf Herter, Kurt Wegner, Walter Schunack, Istvan Szelenyi, Stefan Postius, Kurt H. Ahrens
  • Patent number: 4729995
    Abstract: Novel pyrimidine compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.1 ' are each hydrogen atom, a lower alkyl, benzyl, an alkali metal, or ammonium; R.sub.2 is hydrogen atom, a halogen atom, a lower alkyl, a lower alkoxy, an aryl, a group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are each hydrogen atom, a lower alkyl, or an aryl), or a group of the formula: ##STR3## [wherein R.sub.5 and R.sub.6 are each an alkylene having 1 to 3 carbon atoms, and X is oxygen atom, methylene, or a group of the formula: >N-Y (wherein Y is hydrogen atom, a lower alkyl, benzyl, or an aryl)], which have excellent antiallergic activities and are useful for the prophylaxis and treatment of various allergic diseases, and a pharmaceutical composition containing said pyrimidine compound as an active ingredient.
    Type: Grant
    Filed: April 3, 1987
    Date of Patent: March 8, 1988
    Assignee: Toyo Boseki Kabushiki Kaisha
    Inventors: Hiroaki Taguchi, Takeo Katsushima, Masakazu Ban, Shoichi Aoki, Akihiko Watanabe
  • Patent number: 4728652
    Abstract: 1,4-Dihydropyrimidines of the formula ##STR1## wherein X is sulfur or oxygen and R.sub.4 is aryl or heterocyclo and disclosed. These compounds are useful as cardiovacular agents, particularly anti-hypertensive agents, due to their vasodilator activity.
    Type: Grant
    Filed: April 21, 1986
    Date of Patent: March 1, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4725303
    Abstract: Herbicidally active guanidine derivatives of the formula ##STR1## in which m represents the numbers zero, 1 or 2,R.sup.5 represents an optionally substituted radical from the series comprising alkyl, aralkyl, aryl and heteroaryl,R.sup.2 represents a pyrimidin-2-yl radical which is substituted by halogen, amino, cyano or formyl and/or by optionally substituted radicals from the series comprising alkyl, alkoxy, alkylamino, dialkylamino, alkylcarbonyl and alkoxycarbonyl,R.sup.3 represents hydrogen, an optionally substituted radical from series comprising alkyl, cycloalkyl, alkenyl, alkinyl and aralkyl,R.sup.9 represents hydrogen or optionally substituted alkyl andR.sup.10 represents an optionally substituted radical from the series comprising alkyl, alkenyl, alkinyl, cycloalkyl, aralkyl, aryl, heteroaryl, alkyl- or alkoxycarbonyl and alkyl- or arylsulphonyl, or R.sup.9 and R.sup.
    Type: Grant
    Filed: November 14, 1986
    Date of Patent: February 16, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Koichi Moriya, Theodor Pfister, Hans-Jochem Riebel, Ludwig Eue, Robert R. Schmidt, Klaus Lurssen, Hans-Joachim Diehr, Christa Fest, Rolf Kirsten, Joachim Kluth, Klaus-Helmut Muller, Uwe Priesnitz, Wolfgang Roy, Hans-Joachim Santel
  • Patent number: 4710498
    Abstract: Pyridyloxy derivatives represented by the general formula: ##STR1## wherein the substituted group Z is either one of the following groups: ##STR2## were prepared. These derivatives exert antagonism against Histamine H2-receptors and hence are efficacious for the treatments of digestive ulcers.
    Type: Grant
    Filed: September 30, 1985
    Date of Patent: December 1, 1987
    Assignee: Ikeda Mohando Co., Ltd.
    Inventors: Fujio Nohara, Tomoaki Fujinawa
  • Patent number: 4703119
    Type: Grant
    Filed: June 4, 1985
    Date of Patent: October 27, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Egbert Wehinger, Horst Meyer
  • Patent number: 4687507
    Abstract: N-(heterocyclicaminocarbonyl)arylsulfonamides in which the aryl radical is substituted in the 2-position by a carboxy radical, ester, thioester, or amide thereof; e.g. N-[(4,6-dimethylpyrimidin-2-yl)-aminocarbonyl]-2-methoxycarbonylbenzenesul fonamide or N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-2-methoxycarbonylbenze nesulfonamide; are useful for the regulation of plant growth and as pre-emergence and post-emergence herbicides.
    Type: Grant
    Filed: August 9, 1985
    Date of Patent: August 18, 1987
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: George Levitt
  • Patent number: 4686220
    Abstract: This disclosure describes certain substituted piperazine-1,4-naphthalenediones useful as anti-asthmatic agents.
    Type: Grant
    Filed: December 19, 1985
    Date of Patent: August 11, 1987
    Assignee: American Cyanamid Company
    Inventors: Jeffrey B. Medwid, Lawrence W. Torley, Andrew S. Tomcufcik
  • Patent number: 4683228
    Abstract: A guanidine derivative of the formula I: ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, ring X and D are a variety of radicals defined in the specification and A is a 3-8C alkylene chain which is substituted by a hydroxy radical and into which is optionally inserted, as part of the backbone of the chain, one or two groups selected from oxygen and sulphur atoms and NH and 1-6C N-alkyl radicals; and the pharmaceutically-acceptable acid additions salts thereof. Pharmaceutical compositions and methods of manufacture are also described. The compound of the formula I is a histamine H-2 antagonist and is therefore useful in ulcer therapy.
    Type: Grant
    Filed: January 22, 1985
    Date of Patent: July 28, 1987
    Assignees: ICI Americas Inc., Imperial Chemical Industries PLC
    Inventors: Karin M. Kirkland, Derrick M. Mant
  • Patent number: 4675045
    Abstract: Thiocarbonylsulfonylureas, useful as herbicides and plant growth regulants, herbicidal compositions employing these compounds and methods of applying them to soil or directly to plants have been discovered.
    Type: Grant
    Filed: May 2, 1986
    Date of Patent: June 23, 1987
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Wallace C. Petersen
  • Patent number: 4639264
    Abstract: N-Arylsulfonyl-N'-(4-mercaptomethyl-pyrimidinyl- and -triazinyl)-ureas of the formula ##STR1## (symbols in this formula defined below) and the salts of these compounds with amines, alkali metal bases or alkaline-earth metal bases or with ammonium bases, have good pre- and post-emergence-selective, herbicidal and growth-regulating properties.
    Type: Grant
    Filed: August 15, 1984
    Date of Patent: January 27, 1987
    Assignee: Ciga-Geigy Corporation
    Inventor: Werner Topfl
  • Patent number: 4612309
    Abstract: A class of bicyclic benzo-oxy heterocyclic ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastro-intestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.
    Type: Grant
    Filed: October 23, 1984
    Date of Patent: September 16, 1986
    Assignee: William H. Rorer, Inc.
    Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, Kent W. Neuenschwander