The Cyano Is Bonded Directly To A Benzene Ring Patents (Class 514/522)
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Patent number: 5677333Abstract: 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: GrantFiled: July 8, 1996Date of Patent: October 14, 1997Assignee: Rohm and Haas CompanyInventors: Daniel Louis Loughner, Enrique Luis Michelotti, Willie Joe Wilson, David Hamilton Young
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Patent number: 5654321Abstract: 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: GrantFiled: January 30, 1996Date of Patent: August 5, 1997Assignee: Dong Kook Pharmaceutical Co. Ltd.Inventors: Chang-Kiu Moon, Chung-Kyu Ryu
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Patent number: 5643894Abstract: Ingestible compounds which are substantially tasteless and which have been found to be effective reducers or eliminators of undesirable tastes for eatables.Type: GrantFiled: June 2, 1995Date of Patent: July 1, 1997Assignee: Bioresearch, Inc.Inventors: Robert J. Kurtz, William D. Fuller
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Patent number: 5629347Abstract: 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: GrantFiled: December 22, 1993Date of Patent: May 13, 1997Assignee: Merck Sharp & Dohme Ltd.Inventors: Christopher J. Swain, Martin R. Teall, Brian J. Williams
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Patent number: 5629346Abstract: Certain N-acetonylbenzamides exhibit low toxicity to plants are particularly useful for control of fungi, especially Phycomycetes.Type: GrantFiled: June 6, 1995Date of Patent: May 13, 1997Assignee: Rohm and Haas CompanyInventors: H. Edwin Carley, Ashok K. Sharma, Colin Swithenbank
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Patent number: 5612373Abstract: 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: GrantFiled: June 27, 1994Date of Patent: March 18, 1997Assignee: Zeneca LimitedInventors: Andrew G. Brewster, Peter W. R. Caulkett, Alan W. Faull, Robert J. Pearce, Richard E. Shute
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Patent number: 5610191Abstract: 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: GrantFiled: November 22, 1995Date of Patent: March 11, 1997Assignee: BASF AktiengesellschaftInventors: Horst Wingert, Hubert Sauter, Herbert Bayer, Klaus Oberdorf, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5604261Abstract: 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: GrantFiled: May 22, 1995Date of Patent: February 18, 1997Assignee: Adir Et CompagnieInventors: Michel Langlois, Pierre Renard, G erard Adam
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Patent number: 5602174Abstract: 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: GrantFiled: June 1, 1995Date of Patent: February 11, 1997Assignee: Beecham Wuefling GmbH & Co.Inventor: Harald Maschler
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Patent number: 5599840Abstract: 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: GrantFiled: November 13, 1995Date of Patent: February 4, 1997Assignee: Bar Ilan UniversityInventor: Shlomo Yehuda
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Patent number: 5578639Abstract: 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: GrantFiled: May 30, 1995Date of Patent: November 26, 1996Assignee: Warner-Lambert CompanyInventor: Reynold Homan
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Patent number: 5571842Abstract: 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: GrantFiled: May 11, 1995Date of Patent: November 5, 1996Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
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Patent number: 5569673Abstract: 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: GrantFiled: May 24, 1994Date of Patent: October 29, 1996Assignee: Purdue Research FoundationInventors: D. James Morre, Dorothy M. Morre
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Patent number: 5567734Abstract: 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: GrantFiled: January 23, 1995Date of Patent: October 22, 1996Assignee: Hoechst AktiengesellschaftInventors: Jan-Robert Schwark, Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Wolfgang Scholz, Udo Albus
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Patent number: 5567735Abstract: 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: GrantFiled: June 7, 1995Date of Patent: October 22, 1996Assignee: Imperial Chemical Industries PLCInventors: Keith Russell, Cyrus J. Ohnmacht, Keith H. Gibson
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Patent number: 5559150Abstract: 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: GrantFiled: June 6, 1995Date of Patent: September 24, 1996Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventor: Richard M. Soll
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Patent number: 5556884Abstract: 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: GrantFiled: May 24, 1995Date of Patent: September 17, 1996Assignee: BASF AktiengesellschaftInventors: Klaus Oberdorf, Hubert Sauter, Wassilios Grammenos, Reinhard Kirstgen, Volker Harries, Gisela Lorenz, Eberhard Ammermann, Randall E. Gold, Wolfgang Siegel, Albrecht Harreus
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Patent number: 5545664Abstract: 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: GrantFiled: March 23, 1995Date of Patent: August 13, 1996Assignee: BASF AktiengesellschaftInventors: Reinhard Kirstgen, Klaus Oberdorf, Hubert Sauter, Herbert Bayer, Wassilios Grammenos, Harald Rang, Volker Harries, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5530025Abstract: 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: GrantFiled: June 2, 1995Date of Patent: June 25, 1996Assignee: American Home Products CorporationInventors: Madelene M. Antane, John A. Butera, Bradford H. Hirth, Schuyler A. Antane
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Patent number: 5514711Abstract: 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: GrantFiled: January 5, 1995Date of Patent: May 7, 1996Assignee: Mitsubishi Chemical CorporationInventors: Yasunori Kitano, Hisao Takayanagi, Koichi Sugawara, Hiroto Hara, Hideo Nakamura, Toshiko Oshino
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Patent number: 5506252Abstract: 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: GrantFiled: October 2, 1994Date of Patent: April 9, 1996Assignee: American Home Products CorporationInventors: John A. Butera, Schuyler A. Antane
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Patent number: 5492687Abstract: 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: GrantFiled: May 3, 1994Date of Patent: February 20, 1996Assignee: Sterling Winthrop Inc.Inventors: Stephen B. Ruddy, Gregory L. McIntire, Mary E. Roberts, Edward R. Bacon
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Patent number: 5482942Abstract: 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: GrantFiled: June 28, 1994Date of Patent: January 9, 1996Assignee: American Home Products CorporationInventors: Richard M. Soll, Paul J. Dollings
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Patent number: 5482969Abstract: 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: GrantFiled: March 11, 1994Date of Patent: January 9, 1996Assignee: Zeneca LimitedInventors: James R. Empfield, Cyrus J. Ohnmacht, Keith Russell, Diane A. Trainor, Paul J. Warwick, Jr.
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Patent number: 5466435Abstract: 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: GrantFiled: April 4, 1994Date of Patent: November 14, 1995Assignee: 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
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Patent number: 5459149Abstract: 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: GrantFiled: September 20, 1994Date of Patent: October 17, 1995Assignee: Roussel UclafInventors: John E. Robinson, George S. Cockerill
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Patent number: 5457126Abstract: 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: GrantFiled: March 21, 1994Date of Patent: October 10, 1995Assignee: Alcon Laboratories, Inc.Inventors: K. Roger Aoki, Louis M. DeSantis
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Patent number: 5436267Abstract: 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: GrantFiled: July 11, 1994Date of Patent: July 25, 1995Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Terumasa Komyoji, Itaru Shigehara, Norifusa Matsuo, Hiroshi Shimoharada, Takeshi Ohshima, Toshio Akagi, Shigeru Mitani
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Patent number: 5434186Abstract: 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: GrantFiled: September 28, 1993Date of Patent: July 18, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Noal Cohen, Ferdinand K. Lee, Keith A. Yagaloff
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Patent number: 5420165Abstract: 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: GrantFiled: December 29, 1992Date of Patent: May 30, 1995Assignee: American Cyanamid CompanyInventors: Joseph A. Furch, David G. Kuhn, David A. Hunt
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Patent number: 5416112Abstract: 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: GrantFiled: June 6, 1994Date of Patent: May 16, 1995Assignee: Roussel UclafInventor: Elizabeth A. Kuo
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Patent number: 5416111Abstract: 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: GrantFiled: December 16, 1993Date of Patent: May 16, 1995Assignee: G.D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5409954Abstract: .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: GrantFiled: October 29, 1993Date of Patent: April 25, 1995Assignee: BASF AktiengesellschaftInventors: Reinhard Kirstgen, Albrecht Harreus, Uwe Kardorff, Thomas Kuekenhoehner, Harald Rang, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast
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Patent number: 5407951Abstract: 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: GrantFiled: June 30, 1992Date of Patent: April 18, 1995Assignee: Boehringer Mannheim GmbHInventors: Ernst-Christian Witte, Karlheinz Stegmeier, Liesel Doerge
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Patent number: 5393774Abstract: 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: GrantFiled: January 27, 1994Date of Patent: February 28, 1995Inventors: Helmut Pieper, Gunther Engelhardt
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Patent number: 5389682Abstract: 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: GrantFiled: September 13, 1993Date of Patent: February 14, 1995Assignee: Warner-Lambert CompanyInventors: Bradley D. Tait, Michael W. Wilson
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Patent number: 5382598Abstract: 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: GrantFiled: September 24, 1993Date of Patent: January 17, 1995Assignees: Imperial Chemical Industries PLC, Imperial Chemical HouseInventors: Russell Keith, Cyrus J. Ohnmacht, Keith H. Gibson
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Patent number: 5380755Abstract: 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: GrantFiled: July 24, 1992Date of Patent: January 10, 1995Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Argyrios G. Arvanitis, Everett L. Scholfield
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Patent number: 5373023Abstract: 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: GrantFiled: August 4, 1993Date of Patent: December 13, 1994Assignee: SYNTHELABOInventors: Paul Howard Williams, Christian Hoornaert, Jean Claude Muller
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Patent number: 5373024Abstract: 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: GrantFiled: February 10, 1993Date of Patent: December 13, 1994Assignee: Hoechst AktiengesellschaftInventors: Florian Lang, Hans-Jochen Lang, Dieter Mania, Andreas Weichert, Wolfgang Scholz, Udo Albus, Heinrich Englert
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Patent number: 5371084Abstract: 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: GrantFiled: October 28, 1993Date of Patent: December 6, 1994Assignee: Zeneca LimitedInventors: Paul J. de Fraine, Anne Martin
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Patent number: 5362747Abstract: 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: GrantFiled: November 3, 1993Date of Patent: November 8, 1994Assignee: Abbott LaboratoriesInventors: Marlon Cowart, James F. Kerwin
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Patent number: 5358965Abstract: 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: GrantFiled: May 28, 1993Date of Patent: October 25, 1994Assignee: Nihon Nohyaku Co., Ltd.Inventors: Tomokazu Hino, Nobuharu Andoh, Hiroshi Hamaguchi, Atsushi Kanaoka
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Patent number: 5358968Abstract: 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: GrantFiled: July 15, 1993Date of Patent: October 25, 1994Assignee: BASF AktiengesellschaftInventors: Klaus Oberdorf, Hubert Sauter, Wassilios Grammenos, Reinhard Kirstgen, Volker Harries, Gisela Lorenz, Eberhard Ammermann, Randall E. Gold, Wolfgang Siegel, Albrecht Harreus
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Patent number: 5356931Abstract: 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: GrantFiled: January 4, 1993Date of Patent: October 18, 1994Assignee: BASF AktiengesellschaftInventors: Reinhard Kirstgen, Rainer Otter, Christoph Kuenast, Uwe Kardorff, Wolfgang Steglich, Gunda Bertram
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Patent number: 5348727Abstract: 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: GrantFiled: March 11, 1993Date of Patent: September 20, 1994Assignee: Sterling Winthrop Inc.Inventors: Edward R. Bacon, Carl R. Illig, Thomas J. Caulfield, Brent D. Douty, Kurt A. Josef
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Patent number: 5334607Abstract: 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: GrantFiled: May 28, 1992Date of Patent: August 2, 1994Assignee: BASF AktiengesellschaftInventors: Hubert Sauter, Gisela Lorenz, Gerd Steiner, Bernd Janssen, Timm Anke, Wolfgang Steglich
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Patent number: 5331007Abstract: 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: GrantFiled: July 20, 1992Date of Patent: July 19, 1994Assignee: Fisons CorporationInventors: Ronald C. Griffith, James J. Napier
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Patent number: 5321046Abstract: Disclosed herein are novel unsymmetrical dithiol ketals which are useful in the treatment or prevention of hypercholesterolemia, hyperlipoproteinemia, and atherosclerosis.Type: GrantFiled: October 27, 1992Date of Patent: June 14, 1994Assignee: Bristol-Myers Squibb CompanyInventors: Sing-Yuen Sit, John J. Wright, Jeff A. Field
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Patent number: H1595Abstract: 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: GrantFiled: June 13, 1994Date of Patent: September 3, 1996Assignee: Rhone-Poulene Inc.Inventors: Paul A. Cain, David T.-W. Chou, Themistocles D. J. D'Silva, Daniel B. Grant, Nancy D. Herman