Abstract: Compounds of the formula ##STR1## where R and A have the meanings given in the description, and their use in the treatment of disorders are described.
Abstract: Fungicidally active substituted pyrazolin-5-ones of the formula ##STR1## in which R.sup.1 and R.sup.2 independently of one another each represents hydrogen, alkyl, alkenyl, alkinyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxycarbonyl, hydroxycarbonylalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, alkylaminocarbonylalkyl or dialkylaminocarbonylalkyl, or represents in each case optionally substituted oxiranylalkyl, aralkyl, heterocyclyl or aryl, andR.sup.3 represents halogenoalkyl, halogenoalkenyl or halogenoalkinyl, or represents substituted cycloalkyl, or represents substituted cycloalkylalkyl.
Type:
Grant
Filed:
October 31, 1986
Date of Patent:
May 10, 1988
Assignee:
Bayer Aktiengesellschaft
Inventors:
Klaus Jelich, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
Abstract: This is a continuation in part application derived from our copending application Ser. No. 837,977 (filing date Mar. 10, 1986). This continuation in part is directed to novel pyridine compounds of formula I below have good selective herbicidal properties pre- and postemergence and also influence or inhibit plant growth. The compounds are of formula I ##STR1## wherein each of X, Y and Z independently of one another is hydrogen or a C.sub.1 -C.sub.4 alkyl group, or two adjacent substituents together also form a saturated or unsaturated 3- or 4-membered alkylene chain or alkenyl chain, each of which chains may in turn by substituted by one to four C.sub.1 -C.sub.4 alkyl groups, R is a C.sub.1 -C.sub.4 nitroalkyl group, a substituted C.sub.1 -C.sub.4 alkylthio group or C.sub.1 -C.sub.4 alkoxy group, an unsubstituted or substituted C.sub.3 -C.sub.4 alkenylthio or C.sub.3 -C.sub.4 alkynylthio group, the hydroxyamino group, a C.sub.1 -C.sub.4 alkoxyamino, C.sub.3 -C.sub.4 alkenyloxyamino or C.sub.3 -C.sub.
Type:
Grant
Filed:
December 1, 1986
Date of Patent:
May 10, 1988
Assignee:
Ciba-Geigy Corporation
Inventors:
Dieter Durr, Hans-Georg Brunner, Henry Szczepanski
Abstract: Compounds having the formula: ##STR1## which are ester prodrugs of potent dopamine-.beta.-hydroxylase inhibitors and thus are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmeceutical compositions including these compounds, and methods of using these compounds to inhibit dopamine-.beta.-hydroxylase activity in mammals.
Type:
Grant
Filed:
April 8, 1986
Date of Patent:
May 10, 1988
Assignee:
SmithKline Beckman Corporation
Inventors:
James S. Frazee, Carl Kaiser, Lawrence I. Kruse, Stephen T. Ross
Abstract: The present invention provides a process for the preparation of crystalline torasemide in the pure modification I (monoclinic, space group P2.sub.1 /c, melting point 162.degree. C.) from torasemide of modification II (monoclinic, space group P2/n, melting point 169.degree. C.), wherein a suspension of torasemide of modification II is stirred in water with the addition of a catalytic amount of modification I until the rearrangement is complete.The present invention also provides a pharmaceutical compositions containing torasemide of modification I.
Abstract: New derivatives of 2-(3-pyridyl)-2-phenylaminoacetic acid, of the formula: ##STR1## with: R.sub.0 : --CN, --COOH, CONH.sub.2, COOR.sub.4,R.sub.1 : H, lower alkyl, cycloalkyl, phenyl, if appropriate substituted, aralkyl if appropriate substituted,R.sub.2 : H, lower alkyl, if appropriate substituted,Ar: phenyl if appropriate substituted,Z: halogen, lower alkyl, lower alkoxy, lower alkylthio.They can be employed in agriculture for combating phytopathogenic fungi such as the sclerotiniaceae.
Abstract: N-[.omega.(3-pyridinyl)alkyl]benzamides which are useful as inhibitors of thromboxane synthetase enzyme and/or as cardioprotective agents in the prevention of myocardial infarction.
Type:
Grant
Filed:
March 16, 1987
Date of Patent:
May 10, 1988
Assignee:
American Cyanamid Company
Inventors:
William B. Wright, Jr., Andrew S. Tomcufcik
Abstract: This invention relates to pyridone-pyridyl-imidazolyl and triazolyl compounds, including methods for increasing cardiac contractility, pharmaceutical compositions including the same and methods for the preparation thereof.
Type:
Grant
Filed:
July 15, 1986
Date of Patent:
May 10, 1988
Assignee:
Rorer Pharmaceutical Corporation
Inventors:
William C. Faith, Henry F. Campbell, Donald E. Kuhla
Abstract: Orally active prodrug derivatives of the cardiotonic agent 4-ethyl-1,3-dihydro-5-[4-(2-methyl-1H-imidazol-1-yl)benzoyl]-2H-imidazol-2 -one are disclosed. Pharmaceutical formulations containing such compounds are also provided.
Type:
Grant
Filed:
October 17, 1986
Date of Patent:
May 10, 1988
Assignee:
Berlex Laboratories, Inc.
Inventors:
Paul W. Erhardt, Alfred A. Hagedorn, III
Abstract: Arylsulphonyl-pyridinealdoxime derivatives of the formula (I) ##STR1## in which R, R.sup.1, R.sup.2, n and m have the meanings stated in the description, and their use as agents for combating pests.The new arysulphonyl-pyridinealdoxime derivatives of the formula (I) can be prepared from suitable arylsulphonyl-pyridinealdoximes and suitable carbonyl compounds.
Type:
Grant
Filed:
March 12, 1987
Date of Patent:
May 3, 1988
Assignee:
Bayer Aktiengesellschaft
Inventors:
Christa Fest, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
Abstract: A propionic acid thiol ester derivative having the formula: ##STR1## wherein R.sub.1 is a cyano group, a trifluoromethyl group, a halogen atom or a nitro group, R.sub.2 is a hydrogen atom, a halogen atom or a cyano group, R.sub.3 is a thiazolin-2-yl group or a benzothiazol-2-yl group, and A is a methine group or a nitrogen atom.
Type:
Grant
Filed:
May 12, 1987
Date of Patent:
May 3, 1988
Assignees:
Toyo Soda Mfg. Co., Agro-Kenesho Co., Ltd.
Abstract: A pyrazolecarboxamide derivative represented by the formula hereinbelow is useful since it has preventively, curatively or systematically controlling effects against various plant diseases and fungicides containing said compound as an active ingredient have excellent controlling activities: ##STR1## wherein R.sup.1 and R.sup.2 which are identical or different and represent each a hydrogen atom, a halogen atom, a methyl group, an ethyl group or a trifluoromethyl group, R.sup.3 represents a hydrogen atom or a methyl group and n represents 0 or 1.
Abstract: The present invention provides a process for preparing alkylsulfinyl 2-phenylimidazo[4,5-c]pyridines comprising reacting an N-(3-amino-4-pyridinyl)alkylthiobenzamide with an oxidizing agent in a lower alkanoic acid solvent.
Abstract: Herbicidally active 5-amino-1-phenylpyrazoles of the formula ##STR1## in which R is CN, or an ester or amido group,R.sup.1 is an organic radical,R.sup.2 is an organic radical, hydrogen or an acyl or thioacyl radical,R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 can be hydrogen or various organic radicals but at least one is a haloalkyl, haloalkoxy, haloalkylthio, haloalkylsulphinyl or haloalkylsulphonyl radical, but R is not CN at the same time as R.sup.5 is CF.sub.3. The compounds ##STR2## are intermediates therefor and are also herbicidal.
Type:
Grant
Filed:
July 11, 1985
Date of Patent:
April 26, 1988
Assignee:
Bayer Aktiengesellschaft
Inventors:
Reinhold Gehring, Jorg Stetter, Otto Schallner, Ludwig Eue, Hans-Joachim Santel, Robert R. Schmidt
Abstract: 1-Aryl-5-alkoximinoalkylamino-pyrazoles of the formula ##STR1## in which R represents cyano or nitro, or represents an optionally substituted heterocyclic radical,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen or alkyl, or represents optionally substituted aryl,R.sup.3 represents hydrogen, alkyl or alkenyl, or represents in each case optionally substituted aralkyl or aryl andAr represents optionally substituted phenyl or pyridyl,are active as herbicides and plant growth regulants. Compounds of the formula ##STR2## in which R" has the same definition as R other than cyano, are also active and useful as intermediates as well.
Type:
Grant
Filed:
May 22, 1986
Date of Patent:
April 26, 1988
Assignee:
Bayer Aktiengesellschaft
Inventors:
Reinhold Gehring, Otto Schallner, Jorg Stetter, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
Abstract: The present invention relates to novel derivatives of alpha-(2-oxo 2,4,5,6,7,7a-hexahydro thieno [3,2-c] 5-pyridyl) phenyl acetic acid corresponding to the following general formula: ##STR1## their addition salts with pharmaceutically-acceptable inorganic or organic acids as well as isomers and their mixtures.The invention also relates to their process of preparation and to medicaments containing these compounds which are of therapeutic use as inhibitors of platelet- and thrombotic-aggregation.
Type:
Grant
Filed:
January 31, 1986
Date of Patent:
April 26, 1988
Assignee:
Sanofi (S.A.)
Inventors:
Alain Badorc, Daniel Frehel, Jean-Pierre Maffrand, Eric Vallee
Abstract: An imidazole derivative having antimicrobial activities against bacteria, fungi, yeast, pathogenic plant fungi and the like represented by the following general formula (I): ##STR1## wherein R.sub.1 means a hydrogen or halogen atom or a lower alkyl group, R.sub.2 denotes a hydrogen atom or an alkyl, alkenyl, haloalkyl or substituted or unsubstituted benzyl group, R.sub.3 stands for a hydrogen or halogen atom, and R.sub.4 is a substituted or unsubstituted benzylthio group, a phenylthio, alkylthio, alkenylthio, furfurylthio, alkoxy or phenoxy group or a halogen atom; or an acid addition salt thereof.
Abstract: This invention relates to various 2-acetyl- and 2-propionylpyridine thiosemicarbazones which are substituted on the 4-nitrogen atom. These compounds are useful in the treatment of gonorrhea and, in addition, many are useful either in the treatment of malaria or bacterial infection. Also disclosed are several synthetic procedures used to prepare the thiosemicarbazones.
Type:
Grant
Filed:
December 7, 1984
Date of Patent:
April 19, 1988
Assignee:
The United States of America as represented by the Secretary of the Army
Inventors:
Daniel L. Klayman, John P. Scovill, Joseph F. Bartosevich, Carl J. Mason, T. Scott Griffin
Abstract: The invention relates to a process for the preparation of a compound of general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-(C.sub.1-4)alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-(C.sub.1-3)alkyl group, and one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl or phenyl-(C.sub.1-3)alkyl group and each of the other two groups, which may be the same or different, represent a hydrogen atom or a C.sub.1-6 alkyl group;or a salt or protected derivative thereof, by cyclization of a compound of general formula (II) ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined above, or a salt or a protected derivative thereof.The compounds of formula (I) are potent and selective antagonists at "neuronal" 5-hydroxytryptamine receptors.
Type:
Grant
Filed:
July 23, 1986
Date of Patent:
April 19, 1988
Assignee:
Sanofi
Inventors:
Alexander W. Oxford, Colin D. Eldred, Ian H. Coates, James A. Bell, David C. Humber, George B. Ewan
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