The Cyano Is Bonded Directly To A Benzene Ring Patents (Class 514/522)
  • Patent number: 5677333
    Abstract: A method for controlling phytopathogenic fungi comprises applying a selected fungicidally active N-acetonylbenzamide compound and a second fungicidally active compound selected from the group consisting of manganese-zinc ethylenebis(dithiocarbamate), manganese ethylenebis(dithiocarbamate), zinc ammoniate ethylenebis(dithiocarbamate), zinc ethylenebis(dithiocarbamate), 2-cyano-N-((ethylamino)carbonyl)-2-(methoxyimino)acetamide, and (E,Z) 4-(3-(4-chlorophenyl)-3-(3,4-dimethoxyphenyl)acryloyl)morpholine to plant seed, to plant foliage or to a plant growth medium and provides higher fungicidal activity than separate use of the same compounds.
    Type: Grant
    Filed: July 8, 1996
    Date of Patent: October 14, 1997
    Assignee: Rohm and Haas Company
    Inventors: Daniel Louis Loughner, Enrique Luis Michelotti, Willie Joe Wilson, David Hamilton Young
  • Patent number: 5654321
    Abstract: The present invention relates to a novel 2-chloro-3-arylamino-1,4-naphthoquinone derivative represented by the following formula (I), which has a potent inhibitory activity against platelet aggregation: ##STR1## in which X represents nitrogen (N) or carbon (C) atom andR represents cyano, orR can further represent alkyl, carboxyl or acyl when X represents nitrogen (N) atom,and to a process for preparing thereof and to a pharmaceutical composition for inhibiting blood coagulation which comprises the compound of formula (I) as an active ingredient.
    Type: Grant
    Filed: January 30, 1996
    Date of Patent: August 5, 1997
    Assignee: Dong Kook Pharmaceutical Co. Ltd.
    Inventors: Chang-Kiu Moon, Chung-Kyu Ryu
  • Patent number: 5643894
    Abstract: Ingestible compounds which are substantially tasteless and which have been found to be effective reducers or eliminators of undesirable tastes for eatables.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: July 1, 1997
    Assignee: Bioresearch, Inc.
    Inventors: Robert J. Kurtz, William D. Fuller
  • Patent number: 5629347
    Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is R.sup.9 CR.sup.10 R.sup.11 or CH.sub.2 R.sup.9 CR.sup.10 R.sup.11 where R.sup.9 is H or OH and R.sup.10 and R.sup.11 are optionally substituted phenyl, optionally substituted benzyl, C.sub.5-7 cycoalkyl or (C.sub.5-7 cycloalkyl)methyl; R.sup.1 and R.sup.2 are H, optionally substituted C.sub.1-6 alkyl, optionally substituted phenyl(C.sub.1-4 alkyl), C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, COR.sup.a, COOR.sup.a, COC.sub.1-6 alkylhalo, COC.sub.1-6 alkylNR.sup.a R.sup.b, CONR.sup.12 C.sub.1-6 alkylCONR.sup.a R.sup.b, CONR.sup.a R.sup.b, or SO.sub.2 R.sup.a, or R.sup.1 and R.sup.2 together form a chain (CH.sub.2).sub.q optionally substituted by oxo where one methylene group may optionally be replaced by O or NR.sup.x ; R.sup.3 is H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; R.sup.4 is optionally substituted phenyl(C.sub.1-3 alkyl); X and Y are H, or X and Y together are .dbd.O; and Z is O, S, or NR.sup.7 ; are tachykinin antagonists.
    Type: Grant
    Filed: December 22, 1993
    Date of Patent: May 13, 1997
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Christopher J. Swain, Martin R. Teall, Brian J. Williams
  • Patent number: 5629346
    Abstract: Certain N-acetonylbenzamides exhibit low toxicity to plants are particularly useful for control of fungi, especially Phycomycetes.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: May 13, 1997
    Assignee: Rohm and Haas Company
    Inventors: H. Edwin Carley, Ashok K. Sharma, Colin Swithenbank
  • Patent number: 5612373
    Abstract: The invention concerns acid derivatives of formula IR.sup.1 --CON(R.sup.2)--N(R.sup.3)CO--X.sup.1 --Q--X.sup.2 --GIand pharmaceutically acceptable metabolically labile esters or amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.1, R.sup.2, R.sup.3, X.sup.1, Q, X.sup.2 and G have the meanings given in the specification. The invention also concerns processes for the preparation of the acid derivatives of formula I, pharmaceutical compositions containing them and their use as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa.
    Type: Grant
    Filed: June 27, 1994
    Date of Patent: March 18, 1997
    Assignee: Zeneca Limited
    Inventors: Andrew G. Brewster, Peter W. R. Caulkett, Alan W. Faull, Robert J. Pearce, Richard E. Shute
  • Patent number: 5610191
    Abstract: Thioamides of the formula I ##STR1## where A, B, R' are hydrogen, cyano, alkyl, alkoxy or halogen,X is .dbd.CHCH.sub.3 or .dbd.N--OCH.sub.3,R.sup.1, R.sup.2 are hydrogen or alky1,Y is a group ##STR2## R is hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted hetaryl,and pesticides containing these compounds.
    Type: Grant
    Filed: November 22, 1995
    Date of Patent: March 11, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Horst Wingert, Hubert Sauter, Herbert Bayer, Klaus Oberdorf, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5604261
    Abstract: A compound which is selected from those of formula (I) : ##STR1## in which A, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined in the description, its optical isomers, and its addition salts thereof with a pharmaceutically-acceptable acid or base,and medicinal products containing the same which are useful for treating a disorder of the melatoninergic system.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: February 18, 1997
    Assignee: Adir Et Compagnie
    Inventors: Michel Langlois, Pierre Renard, G erard Adam
  • Patent number: 5602174
    Abstract: A method of treatment or prophylaxis of angina in mammals, such as humans, which comprises the administration to the sufferer of an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, or a solvate of any of the foregoing: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, A and B are herein defined.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: February 11, 1997
    Assignee: Beecham Wuefling GmbH & Co.
    Inventor: Harald Maschler
  • Patent number: 5599840
    Abstract: A nutritional composition, adapted for consumption by mammals, contains (1) an orally ingestible diluent or carrier, except an oily carrier or diluent which comprises C.sub.8-18 saturated fatty acids, oleic acid and derivatives of these acids, and (2) a composition of matter which consists of (a) from about 13.0 to about 27.5% by weight of at least one compound selected from linolenic acid and its salts, esters and amides, calculated as the free acid, and (b) about 87.0 to about 72.5% by weight of at least one compound selected from linoleic acid and its salts, esters and amides thereof, calculated as the free acid, the salts, esters and amides of linolenic and linoleic acid being both physiologically hydrolyzable and pharmacologically acceptable. The invention also relates to a method for treating a mammal for the purpose of inducing therein at least one physiological effect selected from memory enhancement and analgesia, by administration of an effective amount of the nutritional composition.
    Type: Grant
    Filed: November 13, 1995
    Date of Patent: February 4, 1997
    Assignee: Bar Ilan University
    Inventor: Shlomo Yehuda
  • Patent number: 5578639
    Abstract: Certain compounds have been synthesized and found to be effective inhibitors of phospholipase A.sub.2 (PLA.sub.2), and thereby useful in the treatment of intestinal cholesterol absorption and the disease states arising therefrom, such as hypercholesterolemia and coronary artery disease.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: November 26, 1996
    Assignee: Warner-Lambert Company
    Inventor: Reynold Homan
  • Patent number: 5571842
    Abstract: Perfluoroalkyl-substituted benzoylguanidines, a process for their preparation, their use as a medicament or diagnostic agent, and a medicament containing themA description is given of perfluoroalkyl-substituted benzoylguanidines of the formula I ##STR1## where R(1) is (C.sub.1 -C.sub.6)-perfluoroalkyl-SO.sub.m ; R(2) and R(3) are H, halogen, alk(yl)(oxy), phenoxy; R(4) and R(5) are H, alkyl, Hal, CN, OR(7), NR(8)R(9), --(CH.sub.2).sub.n --(CF.sub.2).sub.o --CF.sub.3 and of the pharmacologically acceptable salts thereof; the compounds I are obtained by reacting a compound II ##STR2## with guanidine, L being a leaving group which is able readily to undergo nucleophilic substitution.
    Type: Grant
    Filed: May 11, 1995
    Date of Patent: November 5, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: 5569673
    Abstract: N-Acylated catecholmethylamines are used to inhibit cancer cell proliferation. Specifically, capsaicin is found to inhibit growth at low concentration, but not normal cells.
    Type: Grant
    Filed: May 24, 1994
    Date of Patent: October 29, 1996
    Assignee: Purdue Research Foundation
    Inventors: D. James Morre, Dorothy M. Morre
  • Patent number: 5567734
    Abstract: Phenyl-substituted alkylcarboguanidides carrying perfluoroalkyl groups, of the formula I ##STR1## are described where R(A) and R(B) are H, Hal, CN, OR(6), alkyl, O.sub.r -perfluoroalkyl or NR(7)R(8); R(6) is hydrogen, (cyclo)alk(en)yl, perfluoroalkyl, phenyl or benzyl; R(7) and R(8) are defined as R(6); X is 1-3; R(1) is H, alkyl or --O.sub.0-1 (CH.sub.2)O.sub.0-1 perfluoroalkyl; R(2), R(3), R(4) and R(5) are defined as R(1), with the condition, however, that R(1), R(2), R(3), R(4) and R(5) are not simultaneously hydrogen and that R(1), R(2), R(3), R(4) and R(5) can only be alkyl when at least one of the substituents R(A) or R(B) contains a O.sub.r (CH.sub.2).sub.a C.sub.b F.sub.2b+1 group; as are the pharmaceutically acceptable salts thereof. Methods of preparation of compounds of formula I are also described.
    Type: Grant
    Filed: January 23, 1995
    Date of Patent: October 22, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jan-Robert Schwark, Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: 5567735
    Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the aides and pharmaceutical compositions containing them.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 22, 1996
    Assignee: Imperial Chemical Industries PLC
    Inventors: Keith Russell, Cyrus J. Ohnmacht, Keith H. Gibson
  • Patent number: 5559150
    Abstract: The present invention is directed to novel compounds that are non-peptidic thrombin inhibitors. The compounds have the structure: ##STR1## and pharmaceutically acceptable salts thereof; wherein R.sup.1 is one of alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl; and n is from zero to five. The compounds of the invention are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 24, 1996
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventor: Richard M. Soll
  • Patent number: 5556884
    Abstract: Substituted oxime ethers of the general formula I ##STR1## where R.sup.1 is alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, cyanoalkyl, alkoxycarbonylalkyl, arylalkyl, heteroarylalkyl, arylalkenyl or aryloxyalkyl, the aromatic or heteroaromatic ring being substituted or unsubstituted,R.sup.2 and R.sup.3 are hydrogen, alkyl, haloalkyl, alkoxy, haloalkoxy, halogen, cyano or nitro,R.sup.4 is hydrogen, alkyl, cycloalkyl, haloalkyl or aryl, the aromatic ring being substituted or unsubstituted, andR.sup.5 and R.sup.6 are identical or different and each is hydrogen or alkyl, andX is CH or N, and fungicides and pesticides containing these compounds.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: September 17, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Oberdorf, Hubert Sauter, Wassilios Grammenos, Reinhard Kirstgen, Volker Harries, Gisela Lorenz, Eberhard Ammermann, Randall E. Gold, Wolfgang Siegel, Albrecht Harreus
  • Patent number: 5545664
    Abstract: Substituted phenoxymethylphenyl derivatives I ##STR1## X is .dbd.CH--OCH.sub.3, .dbd.C--CH.sub.3 or .dbd.N--OCH.sub.3 ; R.sup.1 is, inter alia,R.sup.2 and R.sup.3 are, inter alia,H, halogen, CN, NO.sub.2, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.2 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 --C.sub.2 -haloalkoxy;R.sup.4 is, inter alia,CN, Cl, Dr, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio or C.sub.1 -C.sub.4 -haloalkoxy;R.sup.5 is, inter alia,NO.sub.2, CN, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -haloalkoxy;n is 0-4; Y is --O--, --NH--, --N(CH.sub.3)--; R.sup.6 is H, C.sub.1 -C.sub.4 -alkyl.The compounds are useful for controlling pests and fungi.
    Type: Grant
    Filed: March 23, 1995
    Date of Patent: August 13, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Kirstgen, Klaus Oberdorf, Hubert Sauter, Herbert Bayer, Wassilios Grammenos, Harald Rang, Volker Harries, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5530025
    Abstract: The compounds of formula I: ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen, alkyl or cyclic or bicyclic alkyl; R.sub.3 is formyl, alkanoyl, alkenoyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl arylalkanoyl or arylalkylsulfonyl; A is a substituted phenyl group of the following formula: ##STR2## wherein R.sub.5 is cyano and R.sub.6 is alkyl, chloro, bromo, fluoro or iodo and pharmaceutically acceptable salts thereof, are smooth muscle relaxants.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: June 25, 1996
    Assignee: American Home Products Corporation
    Inventors: Madelene M. Antane, John A. Butera, Bradford H. Hirth, Schuyler A. Antane
  • Patent number: 5514711
    Abstract: Styrene derivatives of the following general formula (I): ##STR1## or pharmaceutically acceptable salts thereof. A pharmaceutical composition useful as anticancer agent, which comprises the above compound as an essential component, is also provided.
    Type: Grant
    Filed: January 5, 1995
    Date of Patent: May 7, 1996
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Yasunori Kitano, Hisao Takayanagi, Koichi Sugawara, Hiroto Hara, Hideo Nakamura, Toshiko Oshino
  • Patent number: 5506252
    Abstract: The compounds of the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are, independently, hydrogen, straight or branched chain alkyl or mono- or bi-cyclic alkyl; A is a substituted phenyl group containing one cyano substituent and one substituent selected from cyano, nitro, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, alkylcarboxamido, arylcarboxamido, alkylsulfonyl, perfluoroalkylsulfonyl, arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl or carboxyl; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.
    Type: Grant
    Filed: October 2, 1994
    Date of Patent: April 9, 1996
    Assignee: American Home Products Corporation
    Inventors: John A. Butera, Schuyler A. Antane
  • Patent number: 5492687
    Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising iodophenoxy alkylene ethers and pharmaceutically acceptable clays in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.
    Type: Grant
    Filed: May 3, 1994
    Date of Patent: February 20, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: Stephen B. Ruddy, Gregory L. McIntire, Mary E. Roberts, Edward R. Bacon
  • Patent number: 5482942
    Abstract: This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to their use in the treatment of hypertension as well as for treatment of peripheral vascular disease, congestive heart failure, disorders involving excessive smooth muscle contraction of the urinary tract such as incontinence or of the gastrointestinal tract such as irritable bowel syndrome, asthma, and hair loss and to pharmaceutical compositions containing an invention compound. The present invention discloses compounds represented by the formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, independent from each other, are selected from the following: C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.1-6 alkoxycarbonyl, nitro, cyano, halogen, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.1-6 acylamino, C.sub.
    Type: Grant
    Filed: June 28, 1994
    Date of Patent: January 9, 1996
    Assignee: American Home Products Corporation
    Inventors: Richard M. Soll, Paul J. Dollings
  • Patent number: 5482969
    Abstract: Compounds of formula I: ##STR1## wherein, ring C, A-B, R.sup.1, n, R.sup.2, and R.sup.3 have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinary incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
    Type: Grant
    Filed: March 11, 1994
    Date of Patent: January 9, 1996
    Assignee: Zeneca Limited
    Inventors: James R. Empfield, Cyrus J. Ohnmacht, Keith Russell, Diane A. Trainor, Paul J. Warwick, Jr.
  • Patent number: 5466435
    Abstract: Disclosed are contrast agents of the formula ##STR1## wherein Z is H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, alkoxycarbonyl, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R is C.sub.1 -C.sub.25 alkyl, cycloalkyl, ##STR2## or halo-lower-alkyl; each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy;(CR.sub.1 R.sub.2).sub.p --(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently H or lower-alkyl, optionally substituted with halo;x is 1-4;n is 1-4;m is 1-15;p is 1-20; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl;in an aqueous, pharmaceutically acceptable carrier comprising a cellulose derivative.
    Type: Grant
    Filed: April 4, 1994
    Date of Patent: November 14, 1995
    Assignee: Sterling Winthrop Inc.
    Inventors: Edward J. Baker, Edward R Bacon, Carl R. Illig, Thomas J. Caulfield, Brent D. Douty, Kurt A. Josef, John L. Toner, Robert W. Lee
  • Patent number: 5459149
    Abstract: The present Application discloses pesticidally active compounds of formula (I):Q(CH.sub.2).sub.a (O).sub.b Q.sup.1 CR.sup.2 =CR.sup.3 CR.sup.4 =CR.sup.5 CXNR.sup.1 R.sup.xor a salt or propesticide thereof, wherein Q is an optionally substituted aromatic monocyclic or fused bicyclic ring system in which at least one ring is aromatic, or Q is a dihalovinyl group or a group R.sup.6 --C=C--where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halo or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, C.sub.2-3 alkynyl, or cyano; or Q.sup.1 is (CH.sub.2).sub.7 ; a=0 or 1; b=0 or 1; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; X is oxygen or sulphur;R.sup.1 is phenyl optionally substituted by 1-5 substituents chosen from: a) C.sub.1-4 alkyl, C.sub.
    Type: Grant
    Filed: September 20, 1994
    Date of Patent: October 17, 1995
    Assignee: Roussel Uclaf
    Inventors: John E. Robinson, George S. Cockerill
  • Patent number: 5457126
    Abstract: Disclosed are methods of using certain defined phenylene dioxamic acids in treating allergic ocular responses, such as, hayfever, conjunctivitis, atopic and keratoconjunctivitis, vernal conjunctivitis, giant capillary conjunctivitis and other diseases where mast cell degranulation are important in the etiology, by topical administration of said active to the affected eye; also disclosed are pharmaceutical compositions comprising said actives.
    Type: Grant
    Filed: March 21, 1994
    Date of Patent: October 10, 1995
    Assignee: Alcon Laboratories, Inc.
    Inventors: K. Roger Aoki, Louis M. DeSantis
  • Patent number: 5436267
    Abstract: A novel N-phenylcarbamate compound or its salt where possible, which is useful as the active ingredient of a biocidal composition for control of harmful organisms, is represented by the following general formula (I): ##STR1## wherein R.sup.1 is unsubstituted or substituted alkyl; R.sup.2 is H, unsubstituted or substituted alkyl, alkenyl, alkynyl or cycloalkyl, or --COX.sup.1 wherein X.sup.1 is unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl or alkoxy; Z is --CH.sub.2 S--, --SCH.sub.2 --, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 SO--, --CH.sub.2 SO.sub.2 --, --CH.sub.2 SCH.sub.2 --, or --CH.sub.2 O--N.dbd.C(R.sup.4)--; R.sup.
    Type: Grant
    Filed: July 11, 1994
    Date of Patent: July 25, 1995
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Terumasa Komyoji, Itaru Shigehara, Norifusa Matsuo, Hiroshi Shimoharada, Takeshi Ohshima, Toshio Akagi, Shigeru Mitani
  • Patent number: 5434186
    Abstract: Compounds of the formula ##STR1## wherein X is O or CH.sub.2 ; Y is O, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, or --OCH.sub.2 C.sub.6 H.sub.4 --;Z is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or --C.tbd.C--;f, h, k, m and t, independently, are 0 or 1;n is an integer from 1 to 12;R.sup.1 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl, or aralkyl; and A is B or --O--B, wherein B is a mono-, di- or tricyclic aromatic or heteroaromatic moiety substituted by the group --COR.sup.2, --(O).sub.t --(W).sub.s --COR.sup.2 or --(CH.dbd.CH).sub.p COR.sup.2 and which may also contain up to 4 additional substituents selected, independently, from the group consisting of halogen, cyano, lower alkyl, lower alkoxy, sulfonamido, alkanoyl, aroyl, --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, provided that no more than one of said substituents is --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, and wherein E is COR.sup.
    Type: Grant
    Filed: September 28, 1993
    Date of Patent: July 18, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Noal Cohen, Ferdinand K. Lee, Keith A. Yagaloff
  • Patent number: 5420165
    Abstract: There are provided substituted acid amide, arylhydrazone compounds (amidrazones) of formula I ##STR1## the use thereof for the control of insect and acarid pests and methods and compositions for the protection of crops from the damage and loss caused by said pests.
    Type: Grant
    Filed: December 29, 1992
    Date of Patent: May 30, 1995
    Assignee: American Cyanamid Company
    Inventors: Joseph A. Furch, David G. Kuhn, David A. Hunt
  • Patent number: 5416112
    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 alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms and alkenyl and alkynyl of 2 to 6 carbon atoms, R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms, Y is selected from the group consisting of ##STR2## Z.sub.1 and Z.sub.2 are individually selected from the group consisting of hydrogen, halogen, --NO.sub.2, --CN and alkyl of 1 to 3 carbon atoms, R.sub.3 is hydrogen or alkyl of 1 to 3 carbon atoms, m is an integer from 0 to 6, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are individually selected from the group consisting of hydrogen, halogen, --CN, --NO.sub.2, alkyl, alkylthio and alkoxy of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, --COR.sub.10, --(CH.sub.2).sub.n --CX.sub.3, --O--(CH.sub.2).sub.n CX.sub.3 and --S--(CH.sub.2).sub.n --CX.sub.3, R.sub.
    Type: Grant
    Filed: June 6, 1994
    Date of Patent: May 16, 1995
    Assignee: Roussel Uclaf
    Inventor: Elizabeth A. Kuo
  • Patent number: 5416111
    Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols containing a cyano group and having an N-phenyl-amino-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.
    Type: Grant
    Filed: December 16, 1993
    Date of Patent: May 16, 1995
    Assignee: G.D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5409954
    Abstract: .alpha.-arylacrylic acid derivatives of the general formula I ##STR1## where X is ethylene or ethenylene; Y is a direct bond or oxygen;R.sup.1 is a mononuclear or dinuclear aromatic system substituted by C.sub.1 -C.sub.4 -alkyl, their preparation, insecticides and fungicides containing them and methods for their use.
    Type: Grant
    Filed: October 29, 1993
    Date of Patent: April 25, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Kirstgen, Albrecht Harreus, Uwe Kardorff, Thomas Kuekenhoehner, Harald Rang, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast
  • Patent number: 5407951
    Abstract: The present invention provides sulphonamides of the general formula: ##STR1## wherein R.sup.1 and R.sup.2, which can be the same or different, are hydrogen or halogen atoms or C.sub.1 -C.sub.6 -alkyl, trifluoro-methyl, cyano, carboxyl, alkoxycarbonyl, aminocarbonyl, N-alkylaminocarbonyl or N,N-dialkylaminocarbonyl radicals or, when R.sup.1 and R.sup.2 are alkyl radicals ortho to one another, R.sup.1 and R.sup.2 together with the carbon atoms to which they are attached, form a saturated or unsaturated C.sub.5-C.sub.7 -alkylene ring, R.sup.3 is a hydrogen atom, an alkyl radical containing up to 6 carbon atoms, an acyl radical, a phenylalkyl or phenylalkenyl radical, the phenyl moiety of which can be substituted by halogen, alkyl or trifluoromethyl, C is a --(CH.sub.2).sub.m --radical, in which m is 0, 1, 2 or 3, or a branched C.sub.2 -C.sub.5 -alkylene radical, whereby a methylene radical --CH.sub.
    Type: Grant
    Filed: June 30, 1992
    Date of Patent: April 18, 1995
    Assignee: Boehringer Mannheim GmbH
    Inventors: Ernst-Christian Witte, Karlheinz Stegmeier, Liesel Doerge
  • Patent number: 5393774
    Abstract: The invention relates to phenylethanolamines of general formula ##STR1## wherein R.sub.1 and R.sub.2 are defined as in claim 1, the enantiomers and the acid addition salts thereof, which have valuable pharmacological properties, not only analgesic, antiphlogistic, broncholytic, uterus-spasmolytic, lipolytic effects and an antispastic effect on the cross-striped muscle, but also .beta..sub.2 -mimetic and/or .beta..sub.1 -blocking effects, the use thereof as pharmaceuticals and as performance enhancers and processes for preparing them.
    Type: Grant
    Filed: January 27, 1994
    Date of Patent: February 28, 1995
    Inventors: Helmut Pieper, Gunther Engelhardt
  • Patent number: 5389682
    Abstract: The invention concerns a series of novel bis-urea derivatives, nonpeptides, which show good binding affinity for the CCK-B receptor. The compounds, compositions containing them, methods of preparation, and utilities including anxiety, gastric acid secretion inhibition, and psychoses are included.
    Type: Grant
    Filed: September 13, 1993
    Date of Patent: February 14, 1995
    Assignee: Warner-Lambert Company
    Inventors: Bradley D. Tait, Michael W. Wilson
  • Patent number: 5382598
    Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolyzable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the amides and pharmaceutical compositions containing them.
    Type: Grant
    Filed: September 24, 1993
    Date of Patent: January 17, 1995
    Assignees: Imperial Chemical Industries PLC, Imperial Chemical House
    Inventors: Russell Keith, Cyrus J. Ohnmacht, Keith H. Gibson
  • Patent number: 5380755
    Abstract: The present invention provides alkyl and alkylbenzyl ethers of substituted hydroquinones and pharmaceutical compositions containing them. The present invention further provides methods of using these compounds and compositions to inhibit monoamine oxidase, particularly monoamine oxidase B. The present invention further provides methods for the treatment of diseases involving monoamine oxidase.
    Type: Grant
    Filed: July 24, 1992
    Date of Patent: January 10, 1995
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventors: Argyrios G. Arvanitis, Everett L. Scholfield
  • Patent number: 5373023
    Abstract: The invention provides compounds which are tetrahydronaphthalene derivatives of the formula (I) ##STR1## wherein R.sub.1 represents a halogen atom, a cyano group, a nitro group, an unbranched (C.sub.1 -C.sub.6) alkoxy group, a (C.sub.1 -C.sub.6 cycloalkyl) (C.sub.1 -C.sub.2 alkoxy) group or an aryl (C.sub.1 -C.sub.2 alkoxy) group,R.sub.2 represents a (C.sub.1 -C.sub.4) alkyl group, an aryl group optionally substituted with at least one methoxy group, a pyridyl group or a benzodioxanyl group,R.sub.3 represents a hydrogen atom or a (C.sub.1 -C.sub.2) alkyl group, and n=0 to 3, or are addition salts with pharmaceutically acceptable acids. The compounds of the invention have anti-ischaemic activity.
    Type: Grant
    Filed: August 4, 1993
    Date of Patent: December 13, 1994
    Assignee: SYNTHELABO
    Inventors: Paul Howard Williams, Christian Hoornaert, Jean Claude Muller
  • Patent number: 5373024
    Abstract: Benzoylguanidines of the formula I ##STR1## are described where R(1) is R(4)--SO.sub.m or R(5)R(6)N--SO.sub.z --, where R(4) and R(5) are alk(en)yl or --C.sub.n H.sub.2n --R(7), and where R(7) is a cycloalkyl or phenyl, where R(5) also has the meaning of H, and R(6) is H or C.sub.1 -C.sub.4 -alkyl, R(2) is hydrogen, halogen, alkyl, O--(CH.sub.2).sub.m C.sub.p F.sub.2p+1, --X--R(10), where X is O, S or NR(11), R(10) is H, (cyclo)alkyl(methyl) or --C.sub.n H.sub.2n --R(12) where R(12) is phenyl, and R(3) is defined, inter alia, as R(1), and their pharmaceutically tolerable salts.The compounds I are obtained by reaction of compounds of the formula II ##STR2## with guanidine, in which L is a leaving group which can be easily nucleophilically substituted.
    Type: Grant
    Filed: February 10, 1993
    Date of Patent: December 13, 1994
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Florian Lang, Hans-Jochen Lang, Dieter Mania, Andreas Weichert, Wolfgang Scholz, Udo Albus, Heinrich Englert
  • Patent number: 5371084
    Abstract: Compounds having the formula (I): ##STR1## and stereoisomers thereof, wherein A is hydrogen, halo, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclylalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl, optionally substituted heteroarylalkyl, optionally substituted aryloxyalkyl, optionally substituted heteroaryloxyalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aryloxy, optionally substituted heteroaryloxy, nitro, halo, cyano, --NR.sup.3 R.sup.4, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --S(O).sub.n R.sup.3 wherein n is 0, 1 or 2, (CH.sub.2).sub.m PO(OR.
    Type: Grant
    Filed: October 28, 1993
    Date of Patent: December 6, 1994
    Assignee: Zeneca Limited
    Inventors: Paul J. de Fraine, Anne Martin
  • Patent number: 5362747
    Abstract: 2-Nitroaryl or 2-cyanoaryl compounds of the formula ##STR1## pharmaceutical compositions thereof, intermediates useful in the preparation of these compounds, and methods for treating disorders of vascular smooth muscles or diseases of the cartilage, macrophages, neurons, platelets, bronchial smooth muscles, optic muscles and gastrointestinal smooth muscles, in addition to sickle cell anemia, diabetes, synovitis, chondroarthritis and osteoarthritis by employing these compounds.
    Type: Grant
    Filed: November 3, 1993
    Date of Patent: November 8, 1994
    Assignee: Abbott Laboratories
    Inventors: Marlon Cowart, James F. Kerwin
  • Patent number: 5358965
    Abstract: The present invention relates to a hydrazone derivative represented by the general formula (I) shown below: ##STR1## wherein the substituents are as defined in the specification, processes for preparing the derivative, and uses of the derivative as an insecticide.The hydrazone derivative has a marked insecticidal effect on insect pests, especially against LEPIDOPTERA and COLEOPTERA.
    Type: Grant
    Filed: May 28, 1993
    Date of Patent: October 25, 1994
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Tomokazu Hino, Nobuharu Andoh, Hiroshi Hamaguchi, Atsushi Kanaoka
  • Patent number: 5358968
    Abstract: Substituted oxime ethers of the general formula I ##STR1## where R.sup.1 is alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, cyanoalkyl, alkoxycarbonylalkyl, arylalkyl, heteroarylalkyl, arylalkenyl or aryloxyalkyl, the aromatic or heteroaromatic ring being substituted or unsubstituted,R.sup.2 and R.sup.3 are hydrogen, alkyl, haloalkyl, alkoxy, haloalkoxy, halogen, cyano or nitro,R.sup.4 is hydrogen, alkyl, cycloalkyl, haloalkyl or aryl, the aromatic ring being substituted or unsubstituted, andR.sup.5 and R.sup.6 are identical or different and each is hydrogen or alkyl, andX is CH or N, and fungicides and pesticides containing these compounds.
    Type: Grant
    Filed: July 15, 1993
    Date of Patent: October 25, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Oberdorf, Hubert Sauter, Wassilios Grammenos, Reinhard Kirstgen, Volker Harries, Gisela Lorenz, Eberhard Ammermann, Randall E. Gold, Wolfgang Siegel, Albrecht Harreus
  • Patent number: 5356931
    Abstract: Alpha-Arylacrylic acid derivatives of the general formula I ##STR1## where X is ethylene or ethenylene; n is 0 or 1;m is 0, 1, 2, 3 or 4;R.sup.1 is cyano, cyanato, thiocyanato, nitro, hydroxyl, carboxyl, haloalkyl, haloalkoxy, unsubstituted or substituted cycloalkyl, cycloalkenyl, cycloalkadienyl, alkenyl, alkynyl or amino, alkylcarbonyl, alkoxycarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, unsubstituted or substituted benzyloxycarbonyl, benzoyl, phenylalkyl, phenylalkoxy or phenoxyalkyl,or R.sup.1 together with one of the radicals R.sup.2 forms an unsubstituted or substituted 1,3-butadiene-1,4-diyl group or an unsubstituted or substituted chain consisting of carbon members and an oxygen member, andR.sup.2 is halogen, unsubstituted or substituted alkyl, alkoxy, alkenyloxy, alkynyloxy, alkadienyloxy, benzyloxy or benzylthio, are used for controlling pests.
    Type: Grant
    Filed: January 4, 1993
    Date of Patent: October 18, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Kirstgen, Rainer Otter, Christoph Kuenast, Uwe Kardorff, Wolfgang Steglich, Gunda Bertram
  • Patent number: 5348727
    Abstract: A compound of the formula: ##STR1## wherein Z.dbd.H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, alkoxycarbonyl, cyano, wherein thealkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R.dbd.C.sub.1 -C.sub.25 alkyl, cycloalkyl, ##STR2## or halo-lower-alkyl; each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy, (CR.sub.1 R.sub.2).sub.p -(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C-Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently H, or lower-alkyl, optionally substituted with halo;x is 1-4;n is [1-5]1-4;m is 1-15;p is 1-20; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, these compounds are useful as X-ray contrast agents or aryl-lower alkyl.
    Type: Grant
    Filed: March 11, 1993
    Date of Patent: September 20, 1994
    Assignee: Sterling Winthrop Inc.
    Inventors: Edward R. Bacon, Carl R. Illig, Thomas J. Caulfield, Brent D. Douty, Kurt A. Josef
  • Patent number: 5334607
    Abstract: Antimycotics containing a compound of the formula ##STR1## where .dbd.Y is .dbd.CH--OCH.sub.3, .dbd.CH--CH.sub.3, .dbd.CH--CH.sub.2 --CH.sub.3, .dbd.CH--SCH.sub.3 or .dbd.N--OCH.sub.3, and X is oxygen, or X may also be NH if Y is .dbd.N--OCH.sub.3,Z is halogen, nitro, cyano, unsubstituted or substituted organic radicals, OR.sup.12, SR.sup.13, SOR.sup.14, SO.sub.2 R.sup.15, --COOR.sup.16, --CONR.sup.17 R.sup.18, --COR.sup.19, --CR.sup.20 .dbd.NR.sup.21, --N.dbd.CR.sup.22 R.sup.23, --CR.sup.24 .dbd.N--OR.sup.25, --CR.sup.25 R.sup.26 --O--N.dbd.CR.sup.27 R.sup.28 andU, V, W can be hydrogen or one of the meanings given for Z, or where two of Z, U, V and W in adjacent positions on the phenyl ring can form an unsubstituted or substituted five- or six-membered, aromatic or aliphatic ring which may contain one to three hetero atoms (N, S, O), and R.sup.12 to R.sup.26 are identical or different and are hydrogen, unsubstituted or substituted organic radicals,are used for controlling mycoses.
    Type: Grant
    Filed: May 28, 1992
    Date of Patent: August 2, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Hubert Sauter, Gisela Lorenz, Gerd Steiner, Bernd Janssen, Timm Anke, Wolfgang Steglich
  • Patent number: 5331007
    Abstract: There is provided a method of treatment of neurological disorders, such as epilepsy, stroke and cerebral ischaemia, which comprises the administration of a compound of Formula I: ##STR1## wherein, Ar.sub.1 and Ar.sub.2, which may be the same or different, independently represent phenyl or phenyl substituted by one or more of amino, nitro, halogen, hydroxy, C1 to 6 alkoxy, C1 to 6 alkyl or cyano;R.sub.1 represents hydrogen, C1 to 6 alkyl, C1 to 6 alkoxycarbonyl;R.sub.2 represents hydrogen or COCH.sub.2 NH.sub.2 ;R.sub.3 represents hydrogen or C1 to 6 alkyl;in addition, when R.sub.2 represents hydrogen either one or both of Ar.sub.1 and Ar.sub.2 may also represent 2-, 3- or 4-pyridinyl and R.sub.1 may also represent trihalomethyl;or a pharmaceutically acceptable salt thereof.Some of the compounds of formula I are novel, and these are also provided, together with pharmaceutical compositions containing the novel compounds.
    Type: Grant
    Filed: July 20, 1992
    Date of Patent: July 19, 1994
    Assignee: Fisons Corporation
    Inventors: Ronald C. Griffith, James J. Napier
  • Patent number: 5321046
    Abstract: Disclosed herein are novel unsymmetrical dithiol ketals which are useful in the treatment or prevention of hypercholesterolemia, hyperlipoproteinemia, and atherosclerosis.
    Type: Grant
    Filed: October 27, 1992
    Date of Patent: June 14, 1994
    Assignee: Bristol-Myers Squibb Company
    Inventors: Sing-Yuen Sit, John J. Wright, Jeff A. Field
  • Patent number: H1595
    Abstract: The invention relates to diketontrile derivatives which have been discovered useful against arthropods, plant nematodes, helminth protozoan pests or as intermediates for such useful compounds which have a general formula: ##STR1##
    Type: Grant
    Filed: June 13, 1994
    Date of Patent: September 3, 1996
    Assignee: Rhone-Poulene Inc.
    Inventors: Paul A. Cain, David T.-W. Chou, Themistocles D. J. D'Silva, Daniel B. Grant, Nancy D. Herman