The Nitrogen Bonded Directly To The Hetero Ring Patents (Class 514/472)
  • Patent number: 5506263
    Abstract: Benzyl derivatives of the formula I ##STR1## where A is CH.sub.2, CHCl, CH-alkyl, CH-alkoxy, CH-alkylthio or N-alkoxy,B is OH, alkylthio, alkoxy or alkylamino,U, V, W are hydrogen, halogen, alkyl or alkoxy,D is ##STR2## where R' is hydrogen or alkyl andR is hydrogen, alkyl, cycloalkyl, haloalkyl, halocycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkylthioalkyl, arylthioalkyl, aryloxyalkyl, aryl, arylalkyl, hetaryl, hetaryl-alkyl, hetaryloxyalkyl or heterocyclyl, and fungicides containing these compounds.
    Type: Grant
    Filed: December 14, 1994
    Date of Patent: April 9, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Horst Wingert, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5472956
    Abstract: Cyclophosphamide analogs are provided of the general formula: ##STR1## wherein R.sup.1 and R.sup.2 are each (C.sub.2 -C.sub.6)alkyl, substituted with a leaving group such as halo or alkylsulfonyl, R.sup.3 and R.sup.4 are the same as R.sup.1 and R.sup.2 or are H and Ar is a heteroaromatic ring and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: January 21, 1994
    Date of Patent: December 5, 1995
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Richard F. Borch, James P. Schmidt
  • Patent number: 5434151
    Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: August 24, 1992
    Date of Patent: July 18, 1995
    Assignee: CytoMed, Inc.
    Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
  • Patent number: 5416110
    Abstract: Benzyl derivatives of the formula I ##STR1## where A isCH.sub.2, CHCl, CH-alkyl, CH-alkoxy, CH-alkylthio or N-alkoxy,B isOH, alkylthio, alkoxy or alkylamino,U, V, W arehydrogen, halogen, alkyl or alkoxy,D is ##STR2## where R' ishydrogen or alkyl andR ishydrogen, alkyl, cycloalkyl, haloalkyl, halocycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkylthioalkyl, arylthioalkyl, aryloxyalkyl, aryl, arylalkyl, hetaryl, hetaryl-alkyl, hetaryloxyalkyl or heterocyclyl, and fungicides containing these compounds.
    Type: Grant
    Filed: July 30, 1993
    Date of Patent: May 16, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Horst Wingert, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5387594
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: August 4, 1992
    Date of Patent: February 7, 1995
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, William R. Pilgrim
  • Patent number: 5344843
    Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.2 ' X, Y, Z, A, B, Q and n are as described herein. Their pharmaceutically acceptable salts, and when appropriate, enantiomers, racemates, diastereomers or mixtures thereof or geometric isomer or mixtures thereof, and pharmaceutically acceptable salts thereof. The compounds of formula I inhibit enzyme carnitine acyltransferase 1 (CAT-1) and are therefore useful in the prevention of injury to ischemic tissue, and can limit infarct size, improve cardiac function and prevent arrhythmias during and following a myocardial infarction.
    Type: Grant
    Filed: March 13, 1992
    Date of Patent: September 6, 1994
    Assignee: Hoffman-La Roche Inc.
    Inventors: Robert W. Guthrie, John G. Mullin, Jr., David F. Kachensky, Richard W. Kierstead, Jefferson W. Tilley, Guy P. Heathers, Alan J. Higgins, Ronald A. LeMahieu
  • Patent number: 5334614
    Abstract: The invention concerns hydroxylamine derivatives of the formula I ##STR1## wherein R.sup.4 is hydrogen, carbamoyl, (1-4C)alkyl, cyclopentyl, cyclohexyl, tetrahydrofuran-3-yl, tetrahydropyran-4-yl, piperidin-4-yl, N-(1-4C)alkylpiperidin-4-yl, (2-5C)alkanoyl, (1-4C)alkylsulphonyl, N-(1-4C)alkylcarbamoyl, N,N-di-(1-4C)alkylcarbamoyl, phenyl, phenyl-(1-4C)alkyl, di-phenyl-(1-4C)alkyl, benzoyl, phenylsulphonyl or a heteroarylmethyl group;R.sup.5 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, cyano-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl;A.sup.4 is (1-4C)alkylene;Ar.sup.1 is phenylene, pyridinediyl or pyrimidinediyl;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene, pyridinediyl, pyrimidinediyl, thiophenediyl, furandiyl or thiazolediyl;R.sup.1 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula -A.sup.2 -X.sup.2 -A.sup.3 -wherein each of A.sup.2 and A.sup.
    Type: Grant
    Filed: May 11, 1993
    Date of Patent: August 2, 1994
    Assignees: Zeneca Ltd., Zeneca Pharma SA
    Inventors: Philip N. Edwards, Michael S. Large
  • Patent number: 5332757
    Abstract: The invention concerns oxime derivatives of the formula I ##STR1## wherein R.sup.4 includes hydrogen, carboxy, carbamoyl, amino, cyano, trifluoromethyl, (1-4C)alkylamino, di-(1-4C)alkylamino and (1-4C)alkyl;R.sup.5 includes hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, (2-5C)alkanoyl, halogeno-(2-4C)alkyl and hydroxy-(2-4C)alkyl;Ar.sup.1 is phenylene or a heteroaryl diradical;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene or a heteroaryl diradical;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula -A.sup.2 -X.sup.2 -A.sup.3 - which together with the carbon atom to which A.sup.2 and A.sup.3 are attached define a ring having 5 or 6 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.
    Type: Grant
    Filed: February 8, 1993
    Date of Patent: July 26, 1994
    Assignees: Zeneca Limited, Zeneca PHARMA S A
    Inventors: Thomas G. C. Bird, Patrick Ple
  • Patent number: 5317021
    Abstract: Amino acid compounds of the formula: ##STR1## wherein the various symbols are as hereinafter described, which have inhibiting effect on enkephalinase.
    Type: Grant
    Filed: November 4, 1992
    Date of Patent: May 31, 1994
    Assignee: ONO Pharmaceutical Co., Ltd.
    Inventors: Masanori Kawamura, Yoshinobu Arai, Hideki Aishita
  • Patent number: 5306727
    Abstract: Cyclophosphamide analogs are provided of the general formula: ##STR1## wherein R.sup.1 and R.sup.2 are each (C.sub.2 -C.sub.6)alkyl, substituted with a leaving group such as halo or alkylsulfonyl, R.sup.3 and R.sup.4 are the same as R.sup.1 and R.sup.2 or are H and Ar is a heteroaromatic ring and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: April 30, 1993
    Date of Patent: April 26, 1994
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Richard F. Borch, James P. Schmidt
  • Patent number: 5292771
    Abstract: Compound of formula ##STR1## wherein n is 0 or 1, R.sub.1 and R.sub.2 are independently methyl, ethyl or cyclopropyl and R is an optionally substituted phenyl or heteroaryl group or salt or ester thereof are useful in the treatment of inflammatory bowel disease.
    Type: Grant
    Filed: October 8, 1992
    Date of Patent: March 8, 1994
    Assignee: Orion-yhtyma Oy
    Inventors: Reijo J. Backstrom, Erkki J. Honkanen, Jarmo J. Pystynen, Anne M. Luiro, Paivi A. Aho, Inge-Britt Y. Linden, Erkki A. O. Nissinen, Pentti Pohto
  • Patent number: 5288750
    Type: Grant
    Filed: January 31, 1991
    Date of Patent: February 22, 1994
    Assignee: Orion-yhtyma Oy
    Inventors: Pentti Pohto, Paivi A. Aho, Reijo J. Backstrom, Erkki J. Honkanen, Inge-Britt Y. Linden, Erkki A. O. Nissinen
  • Patent number: 5270301
    Abstract: The present invention relates to certain fluoro-amide derivatives, as described herein, which are human leukocyte elastase (HLE) inhibitors making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated, including treatment of tissue degenerative diseases such as pulmonary emphysema. The invention also includes intermediates useful in the synthesis of these fluoro-amide derivatives, processes for preparing them, pharmaceutical compositions containing such peptide derivatives and methods for their use.
    Type: Grant
    Filed: May 7, 1990
    Date of Patent: December 14, 1993
    Assignee: ICI Americas Inc.
    Inventor: Donald J. Wolanin
  • Patent number: 5219884
    Abstract: The present invention relates to an immunosuppressive agent which comprises at least one compound selected from the compounds of formula ##STR1## wherein R represents a hydrogen atom or an acyl, Y represents carbonyl or hydroxymethylene and represents a single bond or a double bond and their lactones, in an effective amount and a pharmaceutically acceptable carrier; a method of prophylaxis and therapy for suppressing rejection or autoimmune diseases which comprises administering the above-mentioned compound or its lactone in an effective amount; and a novel compound of formula ##STR2## or its lactone.
    Type: Grant
    Filed: March 1, 1990
    Date of Patent: June 15, 1993
    Assignees: Taito Co., Ltd., Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Tetsuro Fujita, Takeshi Ikumoto, Shigeo Sasaki, Takeki Okumoto, Kenji Chiba
  • Patent number: 5190961
    Abstract: Thiourea derivatives represented by the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents a lower alkyl group, or R.sub.1 or R.sub.2 taken together represent a group having the formula --(CH.sub.2).sub.m --in which m is 4 or 5, R.sub.3 represents a lower alkyl group or a cycloalkyl group or a group having the formula--(CH.sub.2).sub.l --R.sub.4 in which R.sub.4 is a phenyl, naphthyl, pyridyl, furyl or thienyl group optionally having 1-3 substituents selected from the group consisting of lower alkyl, lower alkoxy, phenoxy, lower alkylthio, hydroxy, halogen, nitro, cyano and trifluoromethyl, and l represents an integer of 0 to 2 and n represents an integer of 1 to 5 or a physiologically acceptable salt thereof.The compounds of the invention are useful as a therapeutic agent for peptic ulcers which is also effective on prevention of the recurrence after discontinuation of the administration due to the antimicrobial activity against Helicobacter pyroli.
    Type: Grant
    Filed: August 2, 1991
    Date of Patent: March 2, 1993
    Assignee: Terumo Kabushiki Kaisha
    Inventors: Hirokazu Hasegawa, Isamu Endo, Shingo Koyama, Masashi Isozaki, Yukari Yoshiyama, Shigenori Nozawa, Norio Arakawa
  • Patent number: 5182277
    Abstract: A synergistic plant fungicide is disclosed which comprises:(A) a morpholine compound selected from the group consisting of:(a) N-tridecyl-2,6-dimethylmorpholine;(b) N-cyclododecyl-2,6-dimethylmorpholine;(c) N-alkyl(C.sub.12)-2,6-dimethylmorpholine; and(d) 4-(3-p-tert.-butylphenyl)-2-methylpropyl-6-cis-dimethylmorpholine; or an agriculturally acceptable salt thereof; in combination with(B) a second compound selected from the group consisting of:(e) 2-chloro-N-(2,6-dimethylphenyl)-N-(tetrahydro-2- -oxo-3-furanyl)-acetamide;(f) 2-methoxy-N-(2-oxo-1,3-oxazolidin-3-yl)-N-(2,6-dimethylphenyl)-acetamide; wherein the weight ratio of Compound (A) to Compound (B) is 20:1 to 1:2.
    Type: Grant
    Filed: March 9, 1990
    Date of Patent: January 26, 1993
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara R.T.
    Inventors: Thomas Strumpf, Horst Lyr, Dieter Zanke, Gerlinde Zollfrank, Gyula Oros, Ferenc Viranyi, Tibor Ersek
  • Patent number: 5162364
    Abstract: A compound of formula (I): ##STR1## in which R, R.sub.1 and R.sub.2 are as defined in the description. Medicinal product, which is useful in treating disorders related to a dysfunction of GABA.sub.B receptors.
    Type: Grant
    Filed: June 11, 1991
    Date of Patent: November 10, 1992
    Assignee: Adir et Compagnie
    Inventors: Michel Debaert, Pascal Berthelot, Claude Vaccher
  • Patent number: 5128371
    Abstract: There are described novel acylated naphthylamines of the formula I defined herein ##STR1## which have valuable fungicidal properties. They can be used in practice on their own or in the form of compositions for the protection of cultivated plants against fungus infection.
    Type: Grant
    Filed: July 15, 1991
    Date of Patent: July 7, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans Moser, Wolfgang Eckhardt, Walter Kunz, Adolf Hubele
  • Patent number: 5118704
    Abstract: Optically active or racemic compounds are provided having the formula ##STR1## where R.sub.2, R.sub.3, R.sub.4 and R.sub.6 are defined in the specification; R.sub.1 is selected from the group consisting of ##STR2## wherein Y is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido, halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12, preferably 1 to 6, carbon atoms, and a is an integer of from zero to 3, for instance zero to 2; and pharmaceutically acceptable salts thereof; as dopaminergics.
    Type: Grant
    Filed: September 11, 1991
    Date of Patent: June 2, 1992
    Assignee: Whitby Research, Inc.
    Inventors: Gevork Minaskanian, James V. Peck
  • Patent number: 5112868
    Abstract: The present invention is novel selected hydroxamic acid derivatives of acyl residues of selected NSAIDS, i.e. having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by the inhibition and methods for treating these conditions in mammals, including humans suffering therefor.
    Type: Grant
    Filed: May 2, 1990
    Date of Patent: May 12, 1992
    Assignee: Warner-Lambert Company
    Inventors: Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Jagadish C. Sircar
  • Patent number: 5064827
    Abstract: Compounds of the present invention, are represented by the general formula ##STR1## wherein R.sub.1 group which may be alkyl of from 1 to about 6 carbon atoms, alkenyl of from 2 to about 6 carbon atoms, alkynyl of from 2 to about 10 carbon atoms, alkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms, halogen, acetamido, amino, nitro, alkylamino of from 1 to about 6 carbon atoms, hydroxy, hydroxyalkyl of from 1 to about 6 carbon atoms, cyano or arylalkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms R.sub.2, R.sub.3 and R.sub.4 are hydrogen or hydroxyl groups or the combination of either hydrogen or hydroxyl groups; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NHCOR.sub.5, --NHCONR.sub.5 R.sub.6, or --NHCOOR.sub.5 wherein R.sub.5 and R.sub.
    Type: Grant
    Filed: August 23, 1990
    Date of Patent: November 12, 1991
    Assignee: Du Pont Merck Pharmaceutical Company
    Inventors: Ghanshyam Patil, William L. Matier, Khuong H. X. Mai
  • Patent number: 5059620
    Abstract: The present invention relates to new compounds of the formula ##STR1## wherein X is ##STR2## wherein R.sub.1 is hydrogen, lower alkyl, phenyl, benzyl, cinnamoyl, thiophene, furan, pyrrole, imidazole, pyrazole oxazole or thiazole; W is hydrogen or hydroxy; (Y).sub.A is positioned ortho to W and is an aminoloweralkyl having the formula --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 are the same or different and may be lower alkyl or R.sub.2 and R.sub.3 may together with N form a pyrrolidine, piperidine or azepine ring, and A is 2; n and m are independently from 0 to 5; and R is straight or branched C.sub.1 -C.sub.10 alkyl, straight or branched C.sub.3 -C.sub.10 cycloalkyl, straight or branched C.sub.2 -C.sub.4 alkenyl or straight or branched C.sub.2 -C.sub.4 alkynyl, or a pharmaceutically acceptable salt thereof.These compounds are useful in the treatment of various cardiac arrhythmias.
    Type: Grant
    Filed: April 7, 1988
    Date of Patent: October 22, 1991
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventors: David M. Stout, William L. Matier, Lawrence A. Black
  • Patent number: 5055471
    Abstract: This invention relates to derivatives of propanoic acid of the formula ##STR1## Useful as fungicides, insecticides and miticides, to processes for preparing them, to compositions containing them, and to methods of using them to combat fungi, especially fungal infections of plants, and to kill or control insects and mites.
    Type: Grant
    Filed: November 15, 1989
    Date of Patent: October 8, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventors: Paul J. de Fraine, Anne Martin
  • Patent number: 5053430
    Abstract: Novel compounds having the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. These compounds are useful in the treatment of schizophrenia.
    Type: Grant
    Filed: September 22, 1989
    Date of Patent: October 1, 1991
    Assignee: Boehringer Ingelheim KG
    Inventors: Matthias Grauert, Herbert Merz, Joachim Mierau, Gunter Schingnitz, Claus Schneider
  • Patent number: 5010104
    Abstract: Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formul (I): ##STR1## which strongly antagonize an action of thromboxane A.sub.2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.
    Type: Grant
    Filed: June 29, 1989
    Date of Patent: April 23, 1991
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
  • Patent number: 4997847
    Abstract: The invention relates to phenylsulphonamidolkanoic acids which have thromboxane A.sub.2 receptor antagonist activity.
    Type: Grant
    Filed: August 22, 1988
    Date of Patent: March 5, 1991
    Assignees: Smith Kline & French Laboratories Limited, Boehringer Mannheim GmbH
    Inventors: Robert J. Ife, David G. Cooper, Robert A. Slater, Karlheinz Stegmeier, Ernst-Christian Witte
  • Patent number: 4983207
    Abstract: The invention relates to synergistic antifungal and plant-growth regulating compositions and to their application in plant-protection.The fungicides according to the invention contain the mixture of fungicide from the group of morpholines and acylalanines as active ingredients.
    Type: Grant
    Filed: March 3, 1986
    Date of Patent: January 8, 1991
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara R.T.
    Inventors: Thomas Strumpf, Horst Lyr, Dieter Zanke, Gerlinde Zollfrank nee Baumann, Gyula Oros, Ferenc Viranyi, Tibor Ersek
  • Patent number: 4983619
    Abstract: Compounds of the following formula have pharmaceutical properties: ##STR1## in which X is R'(HO)C.dbd.C(CN)--, R.sup.1 (CO)--CH(CN)-- or ##STR2## R.sup.1 and R.sup.2 are each hydrogen or C.sub.1-6 alkyl, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each hydrogen, hydroxy, halogen, nitro, cyano, carboxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halo-substituted C.sub.1-4 alkyl, halo-substituted C.sub.1-4 alkoxy, halo-substituted C.sub.1-4 alkylthio, C.sub.2-5 alkoxycarbonyl, optionally substituted phenyl, optionally substituted phenoxy, R'R"N-- where R' and R" are each hydrogen or C.sub.1-4 alkyl or R'"CONH-- where R'" is C.sub.1-4 alkyl, or a group of the formula --CR.sup.7 R.sup.8 R.sup.9 in which R.sup.7, R.sup.8 and R.sup.9 are each C.sub.1-6 alkyl, halo-substituted C.sub.1-6 alkyl or optionally substituted phenyl, or R.sup.7 and R.sup.8, together with the carbon atom to which they are attached, form a cycloalkyl group containing 3 to 7 carbon atoms, or R.sup.7, R.sup.8 and R.sup.
    Type: Grant
    Filed: January 11, 1990
    Date of Patent: January 8, 1991
    Assignee: Lilly Industries Limited
    Inventors: Peter T. Gallagher, Terence A. Hicks
  • Patent number: 4977153
    Abstract: Compounds of formula (I), ##STR1## characterized in that R signifies optionally substituted heteroaryl-, heteroarylakyl or heteroarylalkenyl, R.sub.1 signifies hydrogen or a substituent, R.sub.2 is hydroxy or a group --z--(CH.sub.2).sub.n --Y--R.sub.3 wherein R.sub.3 is hydrogen, alkyl, hydroxyalkyl, alkenyl, cycloalkyl, cycloalkylalkylene, hydroxy substituted cycloalkyl or cycloalkylalkylene, or optionally substituted aryl or aralkyl or aralkenyl moiety, and Y signifies oxygen or sulfur, and either Z is an oxygen atom and n is 2 or 3, or Z is a bond and n is 1, 2 or 3, A signifies alkylene or branched alkylene of 2 to 5 carbon atoms, W signifies a bond or imino, and X signifies a bond or imino, and their physiologically hydrolyzable derivatives, in which at least one hydroxy group is in esterified form. The compounds exhibit beta adrenoceptor blocking activity. Processes for the preparation of the compounds are also disclosed.
    Type: Grant
    Filed: January 14, 1987
    Date of Patent: December 11, 1990
    Assignee: William J. Louis
    Inventors: William J. Louis, Richard Berthold, Max-Peter Seiler, Andre Stoll
  • Patent number: 4952580
    Abstract: Polyhaloalkene compounds of the formula: ##STR1## wherein X is sulfur, oxygen, or nitrogen, Y.sup.1 and Y.sup.2 are fluorine, Z is hydrogen or the same as Y.sup.1 and Y.sup.2, and n is 1-4; provided that:(A) when X is sulfur, Z is fluorine and R is thienyl or substituted thienyl, thianaphthyl or substituted thianaphthyl, thiazolinyl or substituted thiazolinyl, oxadiazolyl or substituted oxadiazolyl, 3,4,4-trifluoro-3-butenyloxycarbonylmethyl, thiadiazolyl substituted by halogen or R.sup.2 S, wherein R.sup.2 is 3,4,4-trifluoro-3-butenyl or R.sup.2 is phenylmethyl or phenylthiomethyl each optionally substituted by halogen or nitro; or R is thiadiazolyl substituted by R.sup.3, wherein R.sup.3 is substituted aryl, arylalkyl, aryloxyalkyl, alkylthio, haloalkylthio, haloarylthio, cyanoalkylthio, arylalkylthio, aryloxyalkylthio, arylthioalkylthio, heterocycloalkylthio, alkenylthio, haloalkenylthio, halocycloalkylalkenylthio, wherein said aryl or heterocyclic groups of R.sup.
    Type: Grant
    Filed: November 9, 1988
    Date of Patent: August 28, 1990
    Assignee: FMC Corporation
    Inventors: Anthony J. Martinez, Thomas G. Cullen
  • Patent number: 4931471
    Abstract: Derivatives with amide function obtained by reaction between derivatives of linear, branched or cyclic amines having an amino acid or peptidic structure and paramethoxycinnamic acid or urocanic acid. Application of said compounds as specific solar filter, absorbing about 310 nm and avoiding erythematous phenomena during exposures to the sun and as active principles of dermo-pharmaceutical and cosmetological preparations.
    Type: Grant
    Filed: October 3, 1988
    Date of Patent: June 5, 1990
    Assignee: Universite Louis Pasteur
    Inventors: Louis Jung, Dominique Robert
  • Patent number: 4927823
    Abstract: The invention relates to synergistic mixtures comprising as active ingredients(a) a compound of formula I ##STR1## wherein R.sub.1 and R.sub.2 are both H or together form a covalent bond,R.sub.3 is H, Cl or BrX is CH or N andY is CH.sub.2 OCH.sub.3, 2-furyl, benzyl or CH.sub.2 Cl in association with(b) the compound of formula II ##STR2## in a fungicidally effective aggregate amount, and the use of such mixtures.
    Type: Grant
    Filed: November 30, 1988
    Date of Patent: May 22, 1990
    Assignee: Sandoz Ltd.
    Inventor: Ulrich Gisi
  • Patent number: 4925831
    Abstract: Disclosed are specific aminoalkyl naphthalenediol derivatives that enhance natural human host resistance to viral infectious organisms and particularly AIDS-related viruses. Such agents are also administered prophylactically to individuals whose resistance to infection has been specifically immunocompromised by an AIDs-related (HIV) virus.
    Type: Grant
    Filed: June 11, 1987
    Date of Patent: May 15, 1990
    Assignee: Merck & Co., Inc.
    Inventor: Philippe L. Durette
  • Patent number: 4923852
    Abstract: Disclosed are specific aminoalkyl naphthalenediol derivatives that enhance natural human host resistance to viral infectious organisms and particularly AIDS-related viruses. Such agents are also administered prophylactically to individuals whose resistance to infection has been specifically immunocompromised by an AIDS-related (HIV) virus.
    Type: Grant
    Filed: June 11, 1987
    Date of Patent: May 8, 1990
    Assignee: Merck & Co., Inc.
    Inventor: Philippe L. Durette
  • Patent number: 4917826
    Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.
    Type: Grant
    Filed: June 16, 1987
    Date of Patent: April 17, 1990
    Assignee: The Upjohn Company
    Inventors: Roy A. Johnson, Gordon L. Bundy, Gilbert A. Youngdale, Douglas R. Morton, Donald P. Wallach, deceased
  • Patent number: 4904681
    Abstract: The compound D-4-amino-3-isoxazolidone, its pharmaceutically-acceptable salts and its prodrug compounds are described as having cognitive-enhancing activity.
    Type: Grant
    Filed: December 1, 1987
    Date of Patent: February 27, 1990
    Assignee: G. D. Searle & Co.
    Inventors: Alex A. Cordi, Gail E. Handelmann, Joseph B. Monahan
  • Patent number: 4897397
    Abstract: Certain aryl-alkynoic, alkenoic and alkanoic acids and derivatives and their use in treating inflammation, allergy and hyperproliferative skin disease are disclosed.
    Type: Grant
    Filed: December 16, 1988
    Date of Patent: January 30, 1990
    Assignee: Schering Corporation
    Inventors: Neng Y. Shih, David J. Blythin
  • Patent number: 4894392
    Abstract: Disclosed are specific aminoalkyl naphthalenediol derivatives that enhance host resistance to infectious organisms. Such agents are administered prophylactically to individuals whose resistance to infection is comprised by chemotherapy, surgery, burns or other forms of severe stress.
    Type: Grant
    Filed: May 12, 1988
    Date of Patent: January 16, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, Timothy F. Gallagher
  • Patent number: 4882341
    Abstract: The invention relates to amino substituted propenoates and their use against fungi.
    Type: Grant
    Filed: September 9, 1988
    Date of Patent: November 21, 1989
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Ian T. Kay
  • Patent number: 4879274
    Abstract: Novel external medications comprise, as essential components, the following three components (A) to (C):(A) an .alpha.-monoglyceryl ether represented by the following formula (I): ##STR1## wherein R means an alkyl or alkenyl group having 10 - 24 carbon atoms; (B) a physiologically active material; and(C) an oily material.The external medications have extremely high skin occlusive properties and significantly-improved absorptivity of phosiologically active materials. Therefore, a smaller amount of the medications compared with the conventional ones can give sufficient pharmacological effects and thus side effects can be reduced. The external medications may contain physiologically active materials such as drugs, growth hormones and the like, which are expected to show pharmacological effects upon their percutaneous absorption.
    Type: Grant
    Filed: September 12, 1986
    Date of Patent: November 7, 1989
    Assignee: Kao Corporation
    Inventors: Tetsuro Kamiya, Shuichi Tsuchiya, Kenji Hara
  • Patent number: 4849219
    Abstract: A microbicidal composition comprising at least one microbicidal acylaniline derivative such as metalaxyl, furalaxyl and the like, and H.sub.3 PO.sub.3 or a salt thereof, exerts a synergistically potentiated activity against plant diseases, especially also against acylaniline-resistant pathogens. The composition may optionally comprise a third protective fungicidal component. The three active components may be applied in succession in any order or simultaneously.
    Type: Grant
    Filed: April 27, 1988
    Date of Patent: July 18, 1989
    Assignee: Ciba-Geigy Corporation
    Inventors: Theodor Staub, Robert J. Williams, Paul Margot
  • Patent number: 4845122
    Abstract: As an anti-allergic treatment for warm-blooded animals, therapeutic amounts of a compound having the formula I (including acid salts thereof) or II are administered: ##STR1## where; R is OR.sup.4 or NHR.sup.5 in which R.sup.4 is hydrogen or lower alkyl, R.sup.5 is selected from phenyl and phenyl monosubstituted with halogen, lower alkyl, lower alkoxy, R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl, andR.sup.3 is selected from lower alkyl, arylcyclopropyl, naphthyl, phenyl, and phenyl monosubstituted with lower alkyl, lower alkoxy, trifluoromethyl, halogen, nitro, carboxyl, or ethyl carboxylate; ##STR2## R.sup.6 is lower alkyl, R.sup.7 is selected from phenyl and phenyl monosubstituted with lower alkyl, lower alkoxy, halogen or acetyl, and M is an alkali or alkaline earth metal.
    Type: Grant
    Filed: December 5, 1986
    Date of Patent: July 4, 1989
    Inventors: Vassil S. Georgiev, Clyde R. Kinsolving, Robert A. Mack
  • Patent number: 4835177
    Abstract: Disclosed are specific aminoalkyl naphthalenediol derivatives that enhance natural human host resistance to viral infectious organisms and particularly AIDS-related viruses. Such agents are also administered prophylactically to individuals whose resistance to infection has been specifically immunocompromised by an AIDS-related (HIV) virus.
    Type: Grant
    Filed: June 11, 1987
    Date of Patent: May 30, 1989
    Assignee: Merck & Co., Inc.
    Inventor: Philipe L. Durette
  • Patent number: 4829078
    Abstract: This invention relates to compounds presented by the general formula: ##STR1## [wherein R.sup.1 and R.sup.2 are: (i) R.sup.1, R.sup.2 and carbon atoms to which R.sup.1 and R.sup.2 are linked, together represent the group of the general formula: ##STR2## (wherein R.sup.5 and R.sup.6 represent hydrogen, alkyl, cycloalkyl, cycloalkyl-alkyl or phenyl, independently, with the proviso that R.sup.5 and R.sup.6 is not hydrogen atoms at the same time), or(ii) R.sup.1 represents hydrogen and R.sup.2 represents the group of the formula: --COR.sup.7 (wherein R.sup.7 represents the group of the formula: ##STR3## (wherein Y represents a single-bond, alkylene, alkenylene, W represents oxygen or sulfur, m represents 1 to 3, R.sup.8 represents hydrogen, halogen, nitro, hydroxy, alkyl or alkoxy, with the proviso that when m represents two or more, plural R.sup.8 s may be different each, and R.sup.9 represents hydrogen, alkyl or phenyl group, with the proviso that two of R.sup.9 may be different each)), R.sup.
    Type: Grant
    Filed: February 22, 1988
    Date of Patent: May 9, 1989
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Katsuhiro Imaki, Tadao Okegawa, Yoshinobu Arai
  • Patent number: 4781920
    Abstract: The invention provides physically stable anthelmintic paste compositions containing resinates of d1-6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole and other anthelmintic compounds in combination with a wide variety of therapeutic agents such as antibiotics, vitamins, vaccines, or mineral supplements.
    Type: Grant
    Filed: September 3, 1985
    Date of Patent: November 1, 1988
    Assignee: American Cyanamid Company
    Inventor: James M. Quinlan
  • Patent number: 4758561
    Abstract: The present invention to pharmaceutical composition comprising an effective amount of products having the structural formula ##STR1## where R.sub.1 is a hydrogen atom or a lower alkyl group such as methyl or ethyl,R.sub.2 is a straight or branched cyclopropylmethyl, 2-furyl methyl, benzyl, phenyl or lower alkyl group from C.sub.1 to C.sub.4 such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tertiary butyl; the NR.sub.1 R.sub.2 group can also represent a nitrogenous heterocyclic compound N(CH.sub.2).sub.n in which n can be any value between 4 and 6.The products are useful in human and veterinary therapy because of their anti-inflammatory, diuretic, bronchodilating, anticholinergic, antispasmodic and antidepressant properties.
    Type: Grant
    Filed: July 22, 1985
    Date of Patent: July 19, 1988
    Assignee: Societe Cortial, S.A.
    Inventors: Guillaume Le Baut, Louis Sparfel, Marie-Helene Creuzet, Claude Feniou, Henri Pontagnier, Gisele Prat
  • Patent number: 4757067
    Abstract: The present invention to pharmaceutical composition comprising an effective amount of products having the structural formula ##STR1## where R.sub.1 is a hydrogen atom or a lower alkyl group such as methyl or ethyl,R.sub.2 is a straight or branched cyclopropylmethyl, 2-furyl methyl, benzyl, phenyl or lower alkyl group from C.sub.1 to C.sub.4 such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tertiary butyl; the NR.sub.1 R.sub.2 group can also represent a nitrogenous heterocyclic compound N(CH.sub.2).sub.n in which n can be any value between 4 and 6.The products are useful in human and veterinary therapy because of their anti-inflammatory, diuretic, bronchodilating, anticholinergic, antispasmodic and antidepressant properties.
    Type: Grant
    Filed: January 21, 1987
    Date of Patent: July 12, 1988
    Assignee: Societe Cortial, S.A.
    Inventors: Guillaume Le Baut, Louis Sparfel, Marie-Helene Creuzet, Claude Feniou, Henri Pontagnier, Gisele Prat
  • Patent number: 4728669
    Abstract: 3-(N-acyl-N-arylamino)-gamma-butyrolactones and thiobutyrolactones have fungicidal activity.
    Type: Grant
    Filed: February 22, 1979
    Date of Patent: March 1, 1988
    Assignee: Chevron Research Company
    Inventor: David C. K. Chan
  • Patent number: 4707499
    Abstract: This invention relates to 3-alkyl-5-[(substituted amino) methyl]dihydro-3-phenyl-2(3H)-furanones and imino analogs thereof, and to the pharmaceutical compositions containing such compounds, that are useful as inhibitors of cardiac arrhythmias and are therefore useful in the treatment of irregular heartbeat. This invention also relates to the use of such compounds and pharmaceutical compositions in the treatment of irregular heartbeat.
    Type: Grant
    Filed: December 1, 1986
    Date of Patent: November 17, 1987
    Assignee: G. D. Searle & Co.
    Inventors: John S. Baran, Harman S. Lowrie
  • Patent number: 4701457
    Abstract: Amidinoureas are disclosed as useful for the treatment of irritable bowel syndrome.
    Type: Grant
    Filed: January 13, 1984
    Date of Patent: October 20, 1987
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: John Yelnosky, Ghulam N. Mir