Patents Examined by Jane T. Fan
  • Patent number: 5254571
    Abstract: This invention relates to phenylpyridone derivatives which have bronchodilator and anti-allergic activities. A compound of the invention is 6-(2-propoxyphenyl)-1,2-dihydro-2-oxopyridine-3-carboxamide.
    Type: Grant
    Filed: September 25, 1992
    Date of Patent: October 19, 1993
    Assignee: Smith Kline & French Laboratories Ltd.
    Inventors: William J. Coates, Sean T. Flynn
  • Patent number: 5252590
    Abstract: A novel pyridylimidazole derivative having the formula; ##STR1## wherein R.sup.1 is a halogen atom, a nitro group or a trifluoromethyl group; R.sup.2 is a C.sub.1 -C.sub.3 haloalkyl group or a C.sub.1 -C.sub.3 haloalkoxy group; R.sup.3 is a C.sub.1 -C.sub.3 alkyl group; R.sup.4 is a tert-butyl group or a C.sub.1 -C.sub.4 haloalkyl group, a process for producing the same and insecticides containing the same as an active ingredient, are disclosed.
    Type: Grant
    Filed: June 24, 1992
    Date of Patent: October 12, 1993
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hiroki Tomioka, Noriyasu Sakamoto, Kimitoshi Umeda, Hiroaki Fujimoto, Takao Ishiwatari, Hirosi Kisida
  • Patent number: 5250547
    Abstract: Compounds of the Formula: ##STR1## wherein: R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl, or when taken together with the carbon to which they are attached are cycloalkyl of 3 to 8 carbon atoms;R.sup.3 is fluoro lower alkyl; cyano; or nitro;R.sup.4 is ##STR2## R.sup.5 and R.sup.6 are independently hydrogen or lower alkyl; and R.sup.7 is --NR.sup.8 R.sup.9 ; wherein:R.sup.8 is hydrogen; lower alkyl; lower alkoxy; hydroxy; or hydroxy lower alkyl; andR.sup.9 is hydrogen; lower alkyl; hydroxy lower alkyl; --SO.sub.2 R.sup.10 ; --CO.sub.2 R.sup.10 ; --C(O)NR.sup.11 R.sup.12 ; --C(S)NR.sup.11 R.sup.12 ; or --C(O)R.sup.12 ;whereinR.sup.10 is lower alkyl;R.sup.11 is hydrogen or lower alkyl; andR.sup.12 is hydrogen, lower alkyl, or fluoro lower alkyl;with the proviso that R.sup.8 and R.sup.9 cannot both be hydrogen; and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 29, 1991
    Date of Patent: October 5, 1993
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Alistair W. Lochead, Michel J. Navet, Peter E. Hicks
  • Patent number: 5250501
    Abstract: A compound of formula (I): ##STR1## or a salt, enamine or the like, acylate, sulphonate, carbamate or ether derivative thereof; wherein X, X.sup.1 and X.sup.2 are independently oxygen or sulphur, R.sup.1 is an optionally substituted heterocyclic or cycloalkyl group, and Y is an optionally substituted C.sub.2 -C.sub.4 alkylene group which is optionally interposed by an oxygen atom, a group ##STR2## or an optionally mono-substituted nitrogen atom, wherein p is 0, 1 or 2, s is 0 or 1 and R.sup.b is alkyl or alkoxy; provided that when X, X.sup.1 and X.sup.2 are oxygen R.sup.1 is not pyridyl or pyrimidinyl. Processes for the preparation of these compounds and herbicidal compositions containing them are also described and claimed.
    Type: Grant
    Filed: January 10, 1992
    Date of Patent: October 5, 1993
    Assignees: Imperial Chemical Industries PLC, ICI Americas, Inc.
    Inventors: John E. D. Barton, David Cartwright, John M. Cox, Glynn Mitchell, Charles G. Carter, David L. Lee, Francis H. Walker, Frank X. Woolard
  • Patent number: 5250700
    Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkyl;R.sup.2 is C.sub.3-7 alkyl or C.sub.3-7 cycloalkyl;R.sup.3 is hydrogen, lower alkyl, carboxyloweralkyl, lower alkoxycarbonyl, lower alkoxycarbonyl loweralkyl, aryl or aralkyl;R.sup.4 is hydrogen, C.sub.1-8 alkyl, ##STR2## B is a bond, NH or O; Y is O or S;A is a bond or --C.dbd.C--;n is 0-5R.sup.5 may be hydrogen when B is NH, orR.sup.5 is lower alkyl, C.sub.3-8 cycloalkyl, aryl, substituted aryl, aralkyl, substituted aralkyl, aralkenyl, aralkenylalkyl, ##STR3## --(CH.sub.2).sub.n NR.sup.1 R.sup.1 or --(CH.sub.2).sub.n het, where het is a 5- or 6-membered, saturated or unsaturated, nitrogen- or sulfur- or oxygen-containing monoheterocycle, optionally substituted with lower alkyl or oxo;R.sup.
    Type: Grant
    Filed: December 9, 1992
    Date of Patent: October 5, 1993
    Assignee: American Home Products Corporation
    Inventors: Jehan F. Bagli, Louis J. Lombardo, Jerauld S. Skotnicki
  • Patent number: 5246947
    Abstract: This invention relates to substituted pyridinylamino-1H-indoles, 1H-indazoles, 2H-indazoles, benzo[b]thiophenes and 1,2-benzisothiazoles of the formula ##STR1## wherein Q is S, N or NR.sub.2 ;Y is CH, N or NR.sub.2 ;R.sub.1 is hydrogen, loweralkyl, loweralkynyl, loweralkenyl, arylloweralkyl, loweralkoxycarbonylaminoloweralkylcarbonyl, arylloweralkoxycarbonylaminoloweralkylcarbonyl, aminoloweralkylcarbonyl, loweralkoxycarbonyl or acyl;R.sub.2 is hydrogen or loweralkyl;R.sub.3 is hydrogen or loweralkyl;X is hydrogen, loweralkyl, halogen; andn is 0 or 1; or a pharmaceutically acceptable acid addition salt thereof.The compounds of this invention are useful in the treatment of memory dysfunctions characterized by a cholinergic deficit such as the type associated with Alzheimer's disease and other memory disorders.
    Type: Grant
    Filed: August 7, 1992
    Date of Patent: September 21, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Effland, Joseph T. Klein, Lawrence L. Martin
  • Patent number: 5245039
    Abstract: A process for the optical resolution of racemic 1,4-dihydropyridines, containing isothioureido groups. Salification of racemic isothioureas with optically active acids produces diasteroisomeric mixtures of isothiouronium salts, that, using conventional techniques, are separated in the individual components to give optically pure isothioureides of 1,4-dihydropyridines and salts thereof with conventional acids. Said optically pure 1,4-dihydropyridines can then be subjected to desulphuration and to different transformations to give to other enantiomerically pure and therapeutically useful 1,4-dihydropyridines.
    Type: Grant
    Filed: August 14, 1991
    Date of Patent: September 14, 1993
    Assignee: Boehringer Mannheim Italia
    Inventors: Carmelo A. Gandolfi, Marco Frigerio, Carlo Riva, Andrea Zaliani, Giorgio Long, Roberto D. Domenico
  • Patent number: 5242940
    Abstract: N-1 and C-5 heterocyclic pyrazoles, a method of their preparation, compositions containing the same and methods of their use are disclosed. The pyrazoles are useful in alleviating inflammatory and cardiovascular disorders in mammals.
    Type: Grant
    Filed: December 17, 1991
    Date of Patent: September 7, 1993
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Michael P. Wachter, William V. Murray
  • Patent number: 5243051
    Abstract: The present invention relates to tetrahydropyridine derivatives which have high affinity and specificity to .sigma. receptors, whereby these compounds are thought to be effective for treatment of some psychoses.
    Type: Grant
    Filed: June 26, 1992
    Date of Patent: September 7, 1993
    Assignee: Shionigi & Co., Ltd.
    Inventors: Hiromu Matsumura, Toshisada Yano, Hiroshi Hashizume, Akira Matsushita, Masami Eigyo
  • Patent number: 5239079
    Abstract: A pyridinium salt is useful as an antiulcer and is defined by the following formula. It includes a sulphenamide compound and a pyridinium compound. J is benzoimidazole, K is --S-- or --SSR, Z is hydroxy or oxyalkyl.
    Type: Grant
    Filed: August 13, 1992
    Date of Patent: August 24, 1993
    Assignee: Eisai Co., Ltd.
    Inventors: Shigeru Souda, Shuhei Miyazawa, Norihiro Ueda, Katsuya Tagami, Seiichiro Nomoto, Makoto Okita, Naoyuki Shimomura, Toshihiko Kaneko, Masatoshi Fujimoto, Manabu Murakami, Kiyoshi Oketani, Hideaki Fujisaki, Hisashi Shibata, Tsuneo Wakabayashi
  • Patent number: 5237075
    Abstract: A process for producing a 3,4-dihydrocoumarin compound represented by formula (II): ##STR1## wherein R.sub.1 to R.sub.4 are as defined in the specification, comprising the steps of:(1) heating a 3-(2-cyclohexanoyl)propionic acid ester compound represented by formula (I): ##STR2## wherein R.sub.1 R.sub.5 are as defined in the specification, in the presence of at least one solid metal catalyst, thereby to allow said compound of formula (I) to undergo ring formation and dehydrogenation to yield said 3,4-dihydrocoumarin compound of formula (II) and, as a by-product, a coumarin compound represented by formula (III): ##STR3## wherein R.sub.1 to R.sub.
    Type: Grant
    Filed: February 24, 1992
    Date of Patent: August 17, 1993
    Assignee: Sumitomo Chemical Co., Ltd.
    Inventors: Tamio Shirafuji, Kiyomi Sakai, Kensen Okusako, Itaru Kawata, Yasumoto Simazu, Tetuya Suzuta
  • Patent number: 5236945
    Abstract: Abstract Certain 1H-indazole-3-acetic acid derivatives, and their pharmaceutically-acceptable esters and salts, are inhibitors of the aldose reductase enzyme, and so are useful in the treatment of diabetic complications.
    Type: Grant
    Filed: October 11, 1991
    Date of Patent: August 17, 1993
    Assignee: Pfizer Inc.
    Inventors: Banavara L. Mylari, William J. Zembrowski
  • Patent number: 5234935
    Abstract: Improving circulation, with minimal effect on blood pressure, using N-alkylated 1,4-dihydropyridines of the formula ##STR1## in which R.sup.1 represents hydrogen, nitro, cyano, trifluoromethyl, trifluoromethoxy, halogen or methyl,R.sup.2 represents hydrogen, halogen, nitro, hydroxyl, trifluoromethyl or methyl,R.sup.3 represents hydrogen or cyano, orR.sup.2 and R.sup.3 together form a fused benzo ring,R.sup.4 and R.sup.5 are identical or different and represent straight-chain or branched alkyl having up to 8 carbon atoms, which is optionally substituted by alkoxy having up to 4 carbon atoms, andR.sup.6 represents straight-chain or branched alkyl having up to 10 carbon atoms or represents cycloalkyl having 3 to 7 carbon atoms.Many of the compounds are new.
    Type: Grant
    Filed: April 4, 1991
    Date of Patent: August 10, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Otto Behner, Hartmut Wollweber, Bruno Rosen, Siegfried Zaiss, Siegfried Goldmann
  • Patent number: 5232899
    Abstract: A herbicidal substituted benzoxazolinones of the formula ##STR1## in which: R is hydrogen, alkyl, alkoxy, alkenyloxy, alkynyloxy, carboxyalkoxy, alkoxycarbonylalkoxy, alkoxyalkoxy, cyanoalkoxy, haloalkysulphonylamino, alkysulphonylamino, alkoxycarbonyl, haloalkyl, halogen, nitro, carboxy, carboxyalkyl, hydroxy, benzyloxy and cyano;n is 0, 1, 2, or 3;R.sup.1 is hydrogen, nitro, halogen, cyano, haloalkyl, alkyl, alkyoxy, and alkythio;R.sup.2 is hydrogen, halogen, haloalkyl, haloalkyoxy, nitro and cyano; andZ is N or C--R.sub.3, wherein R.sub.3 is hydrogen, halogen, nitro, cyano, alkythio, alkoxy and haloalkyl. Also disclosed is an herbicidal composition and method of treating weeds.
    Type: Grant
    Filed: June 8, 1992
    Date of Patent: August 3, 1993
    Assignee: Imperial Chemical Industries plc
    Inventor: Ferenc M. Pallos
  • Patent number: 5228897
    Abstract: Disclosed herein are herbicidal pyridine compounds substituted at the 2- or 6-position with an OR.sub.2 moiety where R.sub.2 is hydrogen, lower alkyl, halomethyl, lower cyanoalkyl, alkenyl or alkynyl, as well as herbicidal compositions and herbicidal use of these compounds.
    Type: Grant
    Filed: April 20, 1992
    Date of Patent: July 20, 1993
    Assignee: Monsanto Company
    Inventors: Donald E. Korte, Len F. Lee
  • Patent number: 5221682
    Abstract: There are described compounds of the formula ##STR1## where n is 0 or 1;X is O or NR.sub.2, R.sub.2 being hydrogen, loweralkyl or loweralkylcarbonyl;R is hydrogen, loweralkyl, arylloweralkyl or loweralkylcarbonyl; andR.sub.1 is ##STR2## wherein R.sub.3 is hydrogen, loweralkyl or loweralkylcarbonyl; m is 1 or 2; each R.sub.4 is independently hydrogen or loweralkyl; and Y is hydrogen, halogen, loweralkyl, loweralkoxy or trifluoromethyl;which compounds are useful as topical antiinflammatory agents for the treatment of various dematoses.
    Type: Grant
    Filed: May 3, 1991
    Date of Patent: June 22, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Effland, Joseph T. Klein, Gordon E. Olsen, Larry Davis, Russell R. L. Hamer, Brian S. Freed
  • Patent number: 5216169
    Abstract: A 3-hydroxypyridineazomethine dye represented by general formula (I) ##STR1## wherein R.sub.1 represents an aliphatic group, an aromatic group, or a heterocyclic group; R.sub.2 represents an aliphatic group, an aromatic group, a heterocyclic group, an alkoxy group, an aryloxy group, an alkenyloxy group, an amino group, an acyl group, an ester group, an amido group, a carbamoylamino group, a sulfamoylamino group, a sulfamido group, an imido group, a ureido group, an aliphatic or an aromatic sulfonyl group, an aliphatic or an aromatic thio group, a hydroxyl group, a cyano group, a carboxy group, or a halogen atom; R.sub.3 represents an aryl group; Y represents a bivalent linking group containing at least one of amide bond and ester bond; n represents 0, 1 or 2; where n is 2, the two R.sub.2 groups may be the same group or atom or may be mutually different groups or atoms, or the two R.sub.2 groups may form a ring; where n is 1 or more, R.sub.1 and R.sub.2 may form a ring; and at least one of R.sub.1 and R.sub.
    Type: Grant
    Filed: September 18, 1990
    Date of Patent: June 1, 1993
    Assignee: Fuji Photo Film Co., Ltd.
    Inventor: Shigeru Yamazaki
  • Patent number: 5214058
    Abstract: This invention relates to compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, loweralkenyl or loweralkynyl;R.sub.2 is hydrogen, loweralkyl, loweralkenyl, formyl or cyano;X is hydrogen, halogen, nitro, amino, loweralkyl, loweralkoxy or hydroxy;Y is hydrogen, loweralkyl, loweralkoxy, arylloweralkoxy, hydroxy, halogen, nitro or amino, with the proviso that when Y is hydrogen or loweralkyl, R.sub.1 is not hydrogen and R.sub.2 is not formyl; a pharmaceutically acceptable acid addition salt thereof, or where applicable, a geometric or optical isomer or racemic mixture thereof. The compounds of the invention are useful for the treatment of various memory dysfunctions characterized by a decreased cholinergic function, such as found in Alzheimer's disease and other senile dementia.
    Type: Grant
    Filed: June 27, 1991
    Date of Patent: May 25, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Larry Davis, Gordon E. Olsen
  • Patent number: 5210097
    Abstract: A xanthocillin X monomethyl ether derivative represented by the formula (I) ##STR1## wherein R represents an alkyl group, an alkenyl group, an alkoxycarbonyl group, an aralkyl group, an alkyl group substituted with a pyridyl group or a halogen atom, an aralkyl group substituted with an alkyl group or a halogen atom, or an aroyl group, which exerts an intense effect of inhibiting the proliferation of a tumor, in particular, a solid tumor.
    Type: Grant
    Filed: May 18, 1990
    Date of Patent: May 11, 1993
    Assignee: Meiji Seika Kaisha Ltd.
    Inventors: Hiroshi Kurihara, Hiromi Watanabe, Masao Koyama, Masaji Sezaki, Tsutomu Tsuruoka, Harumi Fukuyasu, Haruo Yamamoto
  • Patent number: 5208245
    Abstract: The present invention provides dihydropyridine derivatives represented by the following formula (I) ##STR1## and salts thereof. They have extremely strong, slow and long-acting vasodilating action and antihypertensive action with less adverse effects so that they are useful as therapeutic agents for cardiovascular diseases.
    Type: Grant
    Filed: May 7, 1991
    Date of Patent: May 4, 1993
    Assignee: Wakunaga Seiyaku Kabushiki Kaisha
    Inventors: Terukage Hirata, Yasushi Yoshimura, Masanori Kakimoto, Koichi Tamura, Harunobu Amagase