Patents Examined by Kurt G. Briscoe
  • Patent number: 4778897
    Abstract: Novel 6H-dibenz[b,e][1,4]oxathiepin derivatives of the formulae I and Ia are employed in the treatment and control of allergic conditions such as allergic asthma.
    Type: Grant
    Filed: May 28, 1987
    Date of Patent: October 18, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Clarence S. Rooney, Joshua Rokach
  • Patent number: 4777182
    Abstract: Amidine compounds of formula (I) ##STR1## and the pharmaceutically acceptable acid addition salts thereof are novel and are of use as anti-trypsin, anti-plasmin, anti-kallikrein, anti-thrombin and anti-complement agents which may be administered orally. These amidine compounds can be produced by the reaction between a carboxylic acid compound of formula (II) ##STR2## or a reactive intermediate thereof and 6-amidino-2-naphthol of formula (III) ##STR3## or preferably an acid addition salt thereof.
    Type: Grant
    Filed: February 24, 1986
    Date of Patent: October 11, 1988
    Assignee: Torii & Co., Ltd.
    Inventors: Setsurou Fujii, Toshiyuki Okutome, Toyoo Nakayama, Shigeki Nunomura, Kimio Sudo, Shinichi Watanabe, Masateru Kurumi, Takuo Aoyama
  • Patent number: 4775406
    Abstract: The salts of 1-phenylimidazole-5-carboxylic acids substituted in the phenyl ring, of the general formula (I) ##STR1## exhibit a good plant growth-regulating activity. In the general formula the symbols have the following meaning:Y is an ammonium ion substituted up to fourfold by (substituted) alkyl, (substituted) alkenyl, alkynyl, (substituted) cycloalkyl, cycloalkenyl, and (substituted) phenyl, wherein the charged N may be part of a heterocyclic radial (NH.sub.4.sup.+ is excepted); phosphonium ion substituted fourfold by alkyl, (substituted) phenyl or (substituted) benzyl; sulfonium- or sulfoxonium ion substituted threefold by alkyl, (substituted) phenyl or (substituted) benzyl; the guanidinium ion or an O-alkylisourea cation;R.sup.1, R.sup.2 independently of each other are alkyl;R.sup.3 is alkyl, alkoxy or halogen; andn is 0, 1, 2 or 3.
    Type: Grant
    Filed: November 21, 1985
    Date of Patent: October 4, 1988
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Roland Schmierer, Ernst-Friedrich Schulze, Helmut Bustell, Erwin Hacker
  • Patent number: 4775409
    Abstract: Pollen formation in cereal grain plants is inhibited by application of a 4-carboxy(or derivative)-1-aryl-5-pyrazolecarboxamide. Production of hybrid seed is facilitated by use of the compounds.
    Type: Grant
    Filed: February 2, 1987
    Date of Patent: October 4, 1988
    Assignee: Eli Lilly and Company
    Inventors: James R. Beck, Carole W. Price
  • Patent number: 4774254
    Abstract: A method of combating insects and acarids which comprises applying to such insects, acarids or a habitat thereof, an insecticidally or acaricidally effective amount of a 5-amino-1-aryl-pyrazole of the formula ##STR1## in which R.sup.1 represents hydrogen, alkyl or halogenoalkyl,R.sup.2 represents trifluoromethyl,R.sup.3 represents hydrogen, alkyl or alkenyl,R.sup.4 represents hydrogen, alkyl, alkenyl, alkinyl or a ##STR2## radical, and Ar represents in each case optionally substituted phenyl or pyridyl, where X represents oxygen or sulphur, and R.sup.5 denotes alkyl or halogenoalkyl.Some of the compounds are new.
    Type: Grant
    Filed: March 19, 1987
    Date of Patent: September 27, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Jorg Stetter, Otto Schallner, Markus Lindig, Uta Jensen-Korte, Bernd Baasner, Benedikt Becker, Bernhard Homeyer, Wolfgang Behrenz, Wilhelm Stendel
  • Patent number: 4772721
    Abstract: A process is disclosed for the preparation of new N.sup..tau. -substituted histidine derivatives of the general formula ##STR1## According to the process, a histidine derivative of the general formula ##STR2## is reacted with phosgene, and the resultant product is then alkylated and thereafter hydrolyzed with an acid.The products obtained by the process are highly useful for preparation of histidine-analogous proteins and enzymes.
    Type: Grant
    Filed: June 20, 1984
    Date of Patent: September 20, 1988
    Assignee: Diamalt AG
    Inventor: Wolfgang Voelter
  • Patent number: 4772633
    Abstract: This invention relates to a novel compound represented by the following general formula (I), its production, and an insecticidal and acaricidal composition containing it as an active ingredient: ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, are a hydrogen atom, a halogen atom, a lower alkyl group, a trifluoromethyl group, a lower alkoxyl group, a lower alkenyloxy group or a halogenated lower alkoxyl group or are, taken together, a methylenedioxy group; R.sub.3 is a vinyl group or a ethynyl group; R.sub.4 is a hydrogen atom or a lower alkyl group; R.sub.5 is a hydrogen atom or a fluorine atom; R.sub.6 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxyl group or a trifluoromethyl group; Z is a nitrogen atom or a group represented by the formula --CH.dbd.; when Z is a nitrogen atom, Y is an oxygen atom; and when Z is a group of the formula --CH.dbd., Y is an oxygen atom, a sulfur atom, a methylene group or a group represented by the formula --NH--.
    Type: Grant
    Filed: February 20, 1986
    Date of Patent: September 20, 1988
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Noritada Matsuo, Kazunori Tsushima, Sumio Nishida, Toshihiko Yano, Masachika Hirano
  • Patent number: 4772312
    Abstract: Herbicidally active novel 5-amino-1-pyridyl-pyrazoles of the formula ##STR1## in which R.sup.1 represents hydrogen or represents alkyl with 1 to 12 carbon atoms,R.sup.2 represents hydrogen, nitro, nitroso or halogen, or represents a radical ##STR2## wherein R.sup.5 represents hydrogen, hydroxyl, alkyl, alkenyl, alkinyl, halogenoalkyl, alkoxyalkyl or alkylthioalkyl, or represents optionally substituted cycloalkyl, or represents optionally substituted aryl, or represents alkoxy or alkylthio, or represents optionally substituted aryloxy, or represents optionally substituted arylthio, or represents alkylamino or dialkylamino, or represents optionally substituted arylamino,R.sup.3 represents hydrogen, or represents a radical ##STR3## or represents a radical --S(O).sub.n --R.sup.7, R.sup.4 represents hydrogen, or represents alkyl, or represents a radical ##STR4## or represents a radical --S(O).sub.n --R.sup.7, and, in the case where R.sup.3 represents an --SO.sub.2 --R.sup.
    Type: Grant
    Filed: May 22, 1986
    Date of Patent: September 20, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Otto Schallner, Reinhold Gehring, Jorg Stetter, Hans-Joachim Santel, Robert R. Schmidt
  • Patent number: 4772602
    Abstract: A N-substituted 3,4-dihydropyrimidine derivative of the formula (1): ##STR1## Wherein R.sup.1 is --(CH.sub.2).sub.n --X; X is substituted aminoethyl, substituted sulfideethyl, substituted or nonsubstituted heterocyclo-ethyl wherein the ethylene group is directly bonded to a hetero atom in the heterocyclic ring, or substituted or nonsubstituted heterocyclo-methyl wherein the methylene group is directly bonded to a carbon atom in the heterocyclic ring; n is an integer from 0 to 8; R.sup.2 is straight, branched cyclic or cyclo-straight alkyl having from one to thirteen carbon atoms, or aralkyl having from seven to thirteen carbon atoms and pharmacologically acceptable acid additional salts thereof have substantially strong and long lasting effects. Therefore the compounds are useful as agents for treating disorders of the cardiovascular system, and are useful, for example, as antihypertensive agents, circulation improvers and antianginal agents.
    Type: Grant
    Filed: March 14, 1986
    Date of Patent: September 20, 1988
    Assignee: Suntory Limited
    Inventors: Hidetsura Cho, Akira Mizuno, Keiyu Shima
  • Patent number: 4772309
    Abstract: A 5-Acylamino-pyrazole derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen or nitro,R.sup.2 represents hydrogen, alkyl, alkenyl, alkinyl or optionally substituted cycloalkyl,R.sup.3 represents hydrogen or alkyl,R.sup.4 represents hydrogen or alkyl,X represents oxygen or sulphur,n represents the integer 0, 1 or 2,Ar represents in each case optionally substituted phenyl or pyridyl andHet represents an optionally substituted 5- or 6- membered heterocyclic radical linked via a carbon atom,which exhibit herbicidal and plant growth regulating activity.
    Type: Grant
    Filed: March 19, 1987
    Date of Patent: September 20, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Jorg Stetter, Reinhold Gehring, Otto Schallner, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
  • Patent number: 4772310
    Abstract: Herbicidal and plant growth-regulating novel 5-acylamino-pyrazoles of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen or nitro,R.sup.2 represents hydrogen, alkyl, alkenyl, alkinyl or optionally substituted cycloalkyl,Ar represents in each case optionally substituted phenyl or pyridyl,X represents oxygen or sulphur,A represents a straight-chain or branched optionally substituted alkylene bridge,n represents the numbers 0 or 1 andY represents cyano or the grouping ##STR2## wherein X.sup.1 represents oxygen or sulphur andR.sup.3 represents hydroxyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, amino, alkylamino, dialkylamino, alkenylamino, dialkenylamino, alkyl-alkenylamino or a --OM radical,wherein M represents one equivalent of the cation of an inorganic or organic base.Intermediates therefor of the formula ##STR3## are also new.
    Type: Grant
    Filed: May 19, 1987
    Date of Patent: September 20, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Jorg Stetter, Otto Schallner, Reinhold Gehring, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
  • Patent number: 4771066
    Abstract: Insecticidally and acarididally active 1-arylpyrazoles of the formula ##STR1## in which R.sup.1 represents hydrogen, alkyl or halogen alkyl,R.sup.2 represents alkyl, alkenyl, alkinyl, cycloalkyl, halogenoalkyl, halogenoalkenyl, alkoxyalkyl, alkylthioalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl, optionally substituted aralkyl or optionally substituted aryl,R.sup.3 represents alkyl, alkenyl, alkinyl, halogenoalkyl, halogenoalkenyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl or optionally substituted aralkyl,R.sup.4 represents alkyl, alkenyl, alkinyl, halogenoalkyl, halogenoalkenyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl or optionally substituted aralkyl, and, in addition, also represents hydrogen in the case where R.sup.3 does not simultaneously represent unsubstituted alkyl, orR.sup.3 and R.sup.
    Type: Grant
    Filed: February 12, 1987
    Date of Patent: September 13, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhold Gehring, Uta Jensen-Korte, Otto Schallner, Jorg Stetter, Heinz-Jurgen Wroblowsky, Benedikt Becker, Wolfgang Behrenz, Bernhard Homeyer, Wilhelm Stendel
  • Patent number: 4770692
    Abstract: Novel herbicidal and plant-growth regulating pyrazoles of the formula ##STR1## in which R.sup.1 represents hydrogen, alkyl or halogenoalkyl,R.sup.2 represents nitro or cyano,R.sup.3 represents optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkinyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl or optionally substituted aryl,Ar represents phenyl which is substituted twice or more, or optionally substituted pyridyl, andY represents O, S, SO or SO.sub.2.Several intermediates therefor are also new.
    Type: Grant
    Filed: July 14, 1987
    Date of Patent: September 13, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Jorg Stetter, Reinhold Gehring, Otto Schallner, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
  • Patent number: 4770693
    Abstract: Herbicidally active novel substituted 5-acylamino-1-phenylpyrazoles of the formula ##STR1## in which R.sup.1 represents cyano, alkoxycarbonyl, alkenyloxycarbonyl, alkinyloxycarbonyl, aminocarbonyl, alkylaminocarbonyl, alkenylaminocarbonyl or alkinylaminocarbonyl,R.sup.2 represents hydrogen, alkyl, alkenyl, alkinyl, optionally substituted cycloalkyl, alkoxyalkyl, alkylthioalkyl, halogenoalkyl or optionally substituted aryl andR.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7, which are identical or different, represent hydrogen, halogen, cyano, nitro, alkyl, alkoxy, alkylsulphonyl, alkoxycarbonyl or a radical --R.sup.8,whereinR.sup.8 represents halogenoalkyl, with the proviso that at least one of the radicals R.sup.3, R.sup.4, R.sup.5, R.sup.6 or R.sup.7 represents a radical --R.sup.8, but R.sup.1 does not represent cyano if R.sup.5 represents trifluoromethyl. Many of the intermediates are also novel.
    Type: Grant
    Filed: December 30, 1986
    Date of Patent: September 13, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhold Gehring, Erich Klauke, Otto Schallner, Jorg Stetter, Hans-Joachim Santel, Robert R. Schmidt
  • Patent number: 4770688
    Abstract: A 1-aryl-pyrazole of the formula ##STR1## in which R represents cyano or nitro,Ar represents in each case optionally substituted phenyl or pyridyl,X represents an azido group, or represents the radical ##STR2## and R.sup.1, R.sup.2 and R.sup.3 each independently represents alkyl, alkenyl, alkinyl, halogenoalkyl, alkoxy, alkoxyalkyl, cycloalkyl or cycloalkyloxy, or represents in each case optionally substituted aryl, aryloxy, aralkyl or aralkyloxy,but wherein, in the case where R represents cyano and X simultaneously represents an azido group, Ar does not represent unsubstituted phenyl and does not represent 5-nitro-2-pyridyl. The compounds exhibit herbicidal and plant growth-regulating activity.
    Type: Grant
    Filed: December 16, 1986
    Date of Patent: September 13, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhold Gehring, Markus Lindig, Otto Schallner, Jorg Stetter, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
  • Patent number: 4769472
    Abstract: There are described compounds of the formula ##STR1## where X is O or NR, R being hydrogen or loweralkyl; R.sub.1 is hydrogen; and R.sub.2 is loweralkyl, arylloweralkyl, aryloxyloweralkyl or loweralkyl substituted with ##STR2## or alternatively--NR.sub.1 R.sub.2 taken together is ##STR3## R.sub.3 being arylloweralkyl or a pharmaceutically acceptable acid addition salt thereof, which are useful as ocular or systemic antihypertensive agents.There are also described intermediate compounds having the formula ##STR4## where X is oxygen or NR, R being hydrogen or loweralkyl; and Y is --OCH.sub.3, --OH or ##STR5## as well as intermediate compounds of the formula ##STR6## where Z is oxygen, NOH or NNHR.sub.4, R.sub.4 being hydrogen or loweralkyl.
    Type: Grant
    Filed: November 25, 1987
    Date of Patent: September 6, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Helen H. Ong, Christine M. Yasenchak
  • Patent number: 4769473
    Abstract: 1-Hydroxypyrazole-4-carboxylic acid is prepared by heating an alkali metal of alkaline earth metal salt of 1-hydroxypyrazole, or a mixture of 1-hydroxypyrazole with an alkali metal or alkaline earth metal carbonate or bicarbonate, at from 120.degree. to 250.degree. C. for from 1 to 40 hours under a CO.sub.2 pressure of 20-300 bar, and is used for the preparation of pharmacologically useful compounds.
    Type: Grant
    Filed: August 29, 1986
    Date of Patent: September 6, 1988
    Assignee: BASF Aktiengesellschaft
    Inventors: Heinrich Boehm, Norbert Rieber
  • Patent number: 4769386
    Abstract: The imidazolylthio substituted alkanoic acids represented by the formula (I) or (IA) as defined herein have been found to be leukotriene antagonists and useful in the treatment of diseases in which leukotrienes are a factor, such as asthma.
    Type: Grant
    Filed: October 24, 1986
    Date of Patent: September 6, 1988
    Assignee: Smithkline Beckman Corporation
    Inventors: William E. Bondinell, David T. Hill, Barry M. Weichman
  • Patent number: 4767871
    Abstract: 4-(Protected amino)-3-oxo-1-(substituted and unsubstituted methylene)-1,2-pyrazolidinium ylides are intermediates to 7-substituted bicyclic pyrazolidione antimicrobials.
    Type: Grant
    Filed: April 30, 1987
    Date of Patent: August 30, 1988
    Assignee: Eli Lilly and Company
    Inventors: Richard E. Holmes, Louis N. Jungheim
  • 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