Double Bonded Divalent Chalcogen Containing Patents (Class 544/54)
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Patent number: 5654294Abstract: Compounds of the formula ##STR1## are disclosed as possessing inhibotory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular agents. Processes for preparing these compounds are also disclosed.Type: GrantFiled: June 19, 1996Date of Patent: August 5, 1997Assignee: Bristol-Myers SquibbInventor: Jeffrey A. Robl
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Patent number: 5646276Abstract: Compounds of the formula ##STR1## wherein X.sub.1 is ##STR2## are disclosed as possessing inhibotory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular agents.Type: GrantFiled: June 19, 1996Date of Patent: July 8, 1997Assignee: Bristol-Myers Squibb Co.Inventor: Jeffrey A. Robl
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Patent number: 5641776Abstract: The present invention relates to novel substituted thiosemicarbazone derivatives of formula (I) wherein R.sub.1 is lower alkyl, lower alk-2-en-1-yl, lower alk-2-yn-1-yl, or aryl-lower alkyl, R.sub.2 is hydrogen, lower alkyl, aryl, aryl-lower alkyl, lower alk-2-en-1-yl, lower alk-2-yn-1-yl, unsaturated or saturated heterocyclyl-lower alkyl, lower alkoxycarbonyl-lower alkyl or the group --C(.dbd.O)--R.sub.3, wherein R.sub.3 is lower alkyl, aryl, aryl-lower alkyl, aryl-lower alkenyl, heteroaryl (betaryl), aryloxy, aryl-lower alkoxy or lower alk-2-en-1-yloxy, and the salts thereof, to a process for the preparation of said compounds, to pharmaceutical compositions containing them, and to the use thereof as medicaments.Type: GrantFiled: July 25, 1995Date of Patent: June 24, 1997Assignee: Ciba-Geigy CorporationInventor: Martin Missbach
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Patent number: 5633253Abstract: The present invention relates to novel substituted thiosemicarbazonic acid esters of formula I ##STR1## wherein R.sub.1 is lower alkyl, lower alk-2-en-1-yl, lower alk-2-yn-1-yl, or aryl-lower alkyl, R.sub.2 is hydrogen, lower alkyl, aryl, aryl-lower alkyl, lower alk-2-en-1-yl, lower alk-2-yn-1-yl, unsaturated or saturated heterocyclyl-lower alkyl, lower alkoxycarbonyl-lower alkyl or the group --C(.dbd.O)-R.sub.3, wherein R.sub.3 is lower alkyl, aryl, aryl-lower alkyl, aryl-lower alkenyl, heteroaryl (hetaryl), aryloxy, aryl-lower alkoxy or lower alk-2-en-1-yloxy, and R.sub.4 is lower alkyl, lower alkoxy, lower alk-2-en-1-yl, lower alk-2-yn-1-yl, aryl-lower alkyl, aryl-lower alkenyl, or also lower alkoxycarbonyl-lower alkyl, and the salts thereof, to a process for the preparation of said compounds, to pharmaceutical compositions containing them, and to the use thereof as medicaments.Type: GrantFiled: July 25, 1995Date of Patent: May 27, 1997Assignee: Ciby-Geigy CorporationInventor: Martin Missbach
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Patent number: 5629335Abstract: 1-(Substituted phenyl)-3-(thioimidate)pyrazoles having systemic activity, arthropodicidal (especially insecticidal) and nematocidal compositions comprising same and methods for controlling arthropods (especially insects) and nematodes.Type: GrantFiled: January 30, 1996Date of Patent: May 13, 1997Assignee: Rhone-Poulenc Inc.Inventors: David T. Manning, Tai-Teh Wu, Michael T. Pilato
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Patent number: 5627180Abstract: The present invention relates to novel substituted thiosemicarbazonethiones containing 6-ring members of formula I ##STR1## wherein R.sub.1 is lower alkyl, lower alk-2-en-1-yl, lower alk-2-yn-1-yl, or aryl-lower alkyl, R.sub.2 is hydrogen, lower alkyl, lower alk-2-en-1-yl, lower alk-2-yn-1-yl, aryl, aryl-lower alkyl, unsaturated or saturated heterocyclyl-lower alkyl, lower alkoxycarbonyl-lower alkyl or a group --C(.dbd.O)-R.sub.3 or --C(.dbd.S)-R.sub.3, wherein R.sub.3 is lower alkyl, aryl, aryl-lower alkyl, aryl-lower alkenyl, heteroaryl (hetaryl), aryloxy, aryl-lower alkoxy or lower alk-2-en-1-yloxy, and the salts thereof, to a process for the preparation of said compounds, to pharmaceutical compositions containing them, and to the use thereof as medicaments.Type: GrantFiled: July 25, 1995Date of Patent: May 6, 1997Assignee: Ciba-Geigy CorporationInventor: Martin Missbach
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Patent number: 5583135Abstract: wherein R.sup.1 is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, halogen, nitro, amino or protected amino,R.sup.2 is hydroxy, protected hydroxy, halogen, amino or protected amino,R.sup.3 is hydrogen or an organic group,R.sup.4 R is hydrogen or lower alkyl,R.sup.8 is hydrogen or lower alkyl, and--Z-- is --O-- or a group of the formula: ##STR2## (in which n is 0, 1 or 2), and pharmaceutically acceptable salts thereof which are useful as a medicament.Type: GrantFiled: July 26, 1994Date of Patent: December 10, 1996Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaaki Matsuo, Kiyoshi Tsuji, Katsuya Nakamura, Glen W. Spears
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Patent number: 5567700Abstract: Compounds of formula I ##STR1## wherein G, J, L, M, m and D have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.Type: GrantFiled: August 15, 1994Date of Patent: October 22, 1996Assignee: Zeneca LimitedInventor: Scott C. Miller
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Patent number: 5565450Abstract: The present invention relates to the new substituted 5-aryl-1,3-thiazine derivatives of general formula (I) ##STR1## in which A, G, X, Y and Z are defined in the specification and their use as pesticides, preferably as arthropodicides, nematicides and herbicides, as well as ecto- and endoparasiticides.Type: GrantFiled: June 6, 1995Date of Patent: October 15, 1996Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Folker Lieb, Michael Ruther, J org Stetter, Christoph Erdelen, Ulrike Wachendorff-Neumann, Markus Dollinger, Klaus L urssen, Hans-Joachim Santel
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Patent number: 5549974Abstract: The invention provides an efficient and versatile method for the combinatorial synthesis and screening of libraries of 4-thiazolidinones, metathiazanones, and derivatives thereof. In order to expediently synthesize a combinatorial library of derivatives based upon these core structures, a general methodology for the solid phase synthesis of these derivatives is also provided. Arrays of thiazolidinones, metathiazanones, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antihistaminic, or antimicrobial activity or use in the treatment of inflammation, hypertension, renal failure, congestive heart failure, uremia and other conditions can be prepared using this method.Type: GrantFiled: June 23, 1994Date of Patent: August 27, 1996Assignee: AFFYMAX Technologies NVInventor: Christopher P. Holmes
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Patent number: 5550229Abstract: Novel process for preparing azetidinone compound of the formula [III]: ##STR1## wherein R.sup.1 is H or lower alkyl, R.sup.2 and R.sup.3 combine together with the adjacent nitrogen to form heterocyclic group, and R.sup.4 is protected or unprotected hydroxy-substituted lower alkyl, which comprises reacting an alkanamide compound of the formula [I]: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are the same as defined above, with a compound of the formula [II]: ##STR3## wherein L.sup.1 is a leaving group and R.sup.4 is the same as defined above, in the presence of a base, said compound [III] being useful as synthetic intermediate for 1-methylcarbapenem derivative having excellent antibacterial activity.Type: GrantFiled: June 21, 1994Date of Patent: August 27, 1996Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Tameo Iwasaki, Kazuhiko Kondo, Hiroshi Ohmizu
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Patent number: 5538967Abstract: Substituted oxazines and thiazines, arthropodicidal compositions containing them and methods of controlling arthropods are provided. The oxazines and thiazines having the formula ##STR1## wherein Z is O or S; Q is phenyl or pyridyl substituted with alkenyl, alkynyl or substituted phenyl; andA, E, q, R.sup.1 and R.sup.2 are as described.Type: GrantFiled: January 18, 1995Date of Patent: July 23, 1996Assignee: E. I. Du Pont de Nemours and CompanyInventors: Jeffrey K. Long, Thomas M. Stevenson
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Patent number: 5532259Abstract: Isoxazole-4-carboxamides and hydroxyalkylidenecyanoacetamides, pharmaceuticals containing these compounds and their useIsoxazole-4-carboxamide derivatives and hydroxyalkylidene-cyanoacetamide derivatives are suitable for the treatment of carcinoses. These compounds can be prepared by known processes. Some of the compounds are novel and are additionally suitable for the treatment of rheumatic disorders.Type: GrantFiled: June 7, 1995Date of Patent: July 2, 1996Assignee: Hoechst AktiengesellschaftInventors: Robert R. Bartlett, Friedrich-Johannes Kammerer
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Patent number: 5510353Abstract: Compounds of formulaA--X--Y--NH--Bwherein A is derived from optionally substituted benzothiophene, indole, 4-aza-and 7-aza-benzothiophene or-indole, A bearing in position 5 hydrogen, halogen, optionally substituted alkyl, hydroxy, nitro, amino, alkylamino, acylamino, alkoxycarbonyl, sulfamoyl, cyano, trimethylsilyl, carboxy, carbamoyl, phosphate, oxycarbamoyl, heterocyclic radical or ether or ester group, X-Y is --CR.sub.8 .dbd.N-- or CH(R.sub.8)--NH-- wherein R.sub.8 is -H or alkyl and attached at position 3 of A, and B is a heterocyclic radical or a residue ##STR1## wherein R.sub.10 is H, optionally substituted alkyl, cycloalkyl, aryl, adamantyl, acyl or carbamoyl and X.sub.2 is alkylthio or NR.sub.3 R.sub.10 wherein R.sub.3 is H or alkyl or R.sub.3 and R.sub.10 together with the nitrogen atom to which they are attached form a heterocyclic radical, in free form or in salt form, have pharmacological activity, e.g. for treating gastrointestinal disorders.Type: GrantFiled: January 9, 1995Date of Patent: April 23, 1996Assignee: Sandoz Ltd.Inventors: Rudolf K. A. Giger, Henri Mattes
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Patent number: 5494911Abstract: Isoxazole-4-carboxamide derivatives and hydroxyalkylidene-cyanoacetamide derivatives are suitable for the treatment of carcinoses. These compounds can be prepared by known processes. Some of the compounds are novel and are additionally suitable for the treatment of rheumatic disorders.Type: GrantFiled: November 16, 1992Date of Patent: February 27, 1996Assignee: Hoechst AktiengesellschaftInventors: Robert R. Bartlett, Friedrich-Johannes Kammerer
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Patent number: 5466687Abstract: The invention relates to arylidene-1-azacycloalkanes and arylalkyl-1-azacycloalkanes of the general formula ##STR1## (wherein n, m, p, A, W.sup.1, W.sup.2, X, Y, and R.sup.1 to R.sup.11 are as defined in claim 1) and the isomers, isomer mixtures and salts thereof, which have useful properties, in particular an inhibitory effect on cholesterol biosynthesis.Type: GrantFiled: March 25, 1994Date of Patent: November 14, 1995Assignee: Dr. Karl Thomae GmbHInventors: Roland Maier, Peter Muller, Eberhard Woitun, Rudolf Hurnaus, Michael Mark, Bernhard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
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Patent number: 5430156Abstract: There are disclosed color-providing compounds comprising two or more cyclic 1,3 sulfur-nitrogen groups and two or more color-providing moieties, i.e., complete dyes or dye intermediates, capable of releasing the color-forming moieties upon cleavage in the presence of silver ions or a soluble silver complex. The color-providing compounds are useful as image-forming materials in color photographic processes.Type: GrantFiled: February 4, 1994Date of Patent: July 4, 1995Assignee: Polaroid CorporationInventors: Michael J. Arnost, Efthimios Chinoporos, Donald A. McGowan, David P. Waller
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Patent number: 5428032Abstract: Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.Type: GrantFiled: December 20, 1993Date of Patent: June 27, 1995Assignee: Nihon Bayer Agrochem K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
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Patent number: 5424307Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a 1,3-thiomorpholino-type group or a 1,4-thiomorpholino-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: December 16, 1993Date of Patent: June 13, 1995Assignee: C. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5420099Abstract: A compound having the formula ##STR1## wherein A is CR.sub.7 ; and R.sup.1 through R.sup.7 are substituents such as hydrogen, halogen, branched and straight chain hydrocarbons, cyclic hydrocarbons, aromatics, and sulfur and nitrogen containing functional groups. Further, R.sup.5 and R.sup.6 may be taken together with the atom to which they are attached to form a group ##STR2## in which R.sup.9 and R.sup.10 are further functional groups. The compounds are useful in herbicidal compositions, particularly in combination with carriers and surfactants. A process for making this compound is also presented.Type: GrantFiled: December 21, 1992Date of Patent: May 30, 1995Assignee: Shell Research LimitedInventor: Trevor W. Newton
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Patent number: 5420125Abstract: Nitromethylene compounds of general formula ##STR1## wherein R represents a hydrogen atom or an alkyl group, R.sup.1 represents a hydrogen atom or an alkyl group, n is 0 or 1, and Het represents an optionally substituted 3-pyridyl, 4-pyridyl or 5-isoxazolyl group, processes for their preparation, and their use as insecticides, are described.Type: GrantFiled: March 24, 1994Date of Patent: May 30, 1995Assignee: Shell Research LimitedInventors: David Munro, Bipin Patel
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Patent number: 5393754Abstract: Insecticidal, acaricidal or nematocidal compositions which comprise a series of organophosphorus compounds represented by the following representative structural formulae: ##STR1## show excellent effect for controlling harmful insects, mites and nematodes, do not give off a bad or irritating smell and exhibit very low toxicity to warm-blooded animals.Type: GrantFiled: September 9, 1993Date of Patent: February 28, 1995Assignee: Agro-Kanesho Co., Ltd.Inventors: Katsumi Nanjo, Akinori Kariya, Shinya Henmi, Hideyo Fujii, Syuichi Usui
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Patent number: 5378839Abstract: There are provided 1-(substituted)thioalkylpyrrole compounds of formula I ##STR1## the use thereof for the control of insect, acarid and mollusk pests and methods and compositions for the protection of crops from the ravages of said pests.Type: GrantFiled: January 26, 1994Date of Patent: January 3, 1995Assignee: American Cyanamid CompanyInventors: David G. Kuhn, Venkataraman Kameswaran
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Patent number: 5362872Abstract: The invention relates to chromogenic lactams, to their preparation and to the use thereof in pressure-sensitive or heat-sensitive recording materials.The novel lactams have the general formula I ##STR1## wherein the ring A is an aromatic or heteroaromatic radical containing 6 ring atoms;the ring B is an unsubstituted or substituted benzene nucleus; andZ is ##STR2## R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, X.sub.1 and X.sub.2 are as defined in the description.Type: GrantFiled: March 10, 1993Date of Patent: November 8, 1994Assignee: Ciba-Geigy CorporationInventors: Hans Baumann, Rox Phaff
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Patent number: 5356893Abstract: The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt or solvate thereof wherein R.sup.1 represents a halogen or hydrogen atom or a C.sub.1-6 alkyl or C.sub.1-6 alkoxy group;R.sup.2 represents a phenyl group optionally substituted by one or two substituents;R.sup.3 represents the group ##STR2## R.sup.4 and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a halogen atom, or a group selected from hydroxy, C.sub.1-6 alkoxy or C.sub.1-6 alkyl.The compounds may be used in the treatment or prophylaxis of depression and other CNS disorders.Type: GrantFiled: September 17, 1992Date of Patent: October 18, 1994Assignee: Glaxo Group LimitedInventors: John Bradshaw, John W. Clitherow, Ian B. Campbell
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Patent number: 5342937Abstract: A solvent soluble heterocyclic o-hydroxy thione carrying a lipophilic group and the process for the selective extraction of gallium, and certain other related metals, especially from solutions containing excess aluminium.Type: GrantFiled: October 7, 1991Date of Patent: August 30, 1994Assignees: Zeneca, Limited, Nerco, Inc.Inventors: Peter W. Austin, Peter M. Quan, Peter A. Tasker, Derek Thorp
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Patent number: 5334715Abstract: Novel 1-piperazinyl-2-butenes and -2-butynes, intermediates and processes for the preparation thereof, and methods of treating psychoses utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: February 1, 1993Date of Patent: August 2, 1994Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Helen H. Ong, Nicholas J. Hrib, Joseph Perez, John G. Jurcak
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Patent number: 5322847Abstract: A series of imidazo[4,5-c]pyridines which inhibit platelet activating factor (PAF) and also block leukotriene D4 receptors are useful in treating asthma, arthritis, psoriasis, gastrointestinal distress, myocardial infarction, stroke and shock.Type: GrantFiled: November 5, 1992Date of Patent: June 21, 1994Assignee: Pfizer Inc.Inventors: Anthony Marfat, James F. Eggler, Michael J. Fray, Kelvin Cooper
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Patent number: 5312799Abstract: This invention described in this patent application relates to novel amides of the formula (I) ##STR1## wherein the substituents are as defined in the disclosure, intermediates for such amides, synthesis thereof and their use for the control of weeds.Type: GrantFiled: May 8, 1992Date of Patent: May 17, 1994Assignee: Sandoz Ltd.Inventors: Karl Seckinger, Karlheinz Milzner, Fred Kuhnen, Sasank S. Mohanty
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Patent number: 5300640Abstract: A novel herbicidal pyrimidine derivative represented by the formula ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y.sup.1, Y.sup.2, Y.sup.3, X and Z are as defined herein.Type: GrantFiled: December 19, 1991Date of Patent: April 5, 1994Assignee: Sumitomo Chemical Company, LimitedInventors: Mitsumori Hiratsuka, Naonori Hirata, Kazuo Saito, Hideyuki Shibata
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Patent number: 5276037Abstract: The invention concerns an aryl derivative of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl, naphthyl or a heterocyclic moiety, and X.sup.1 is oxy, thio, sulphinyl, sulphonyl, difluoromethylene, imino, (1-4C)alkylimino or optionally substituted (1-4C)alkylene, or X.sup.1 is a group of the formula--X.sup.4 --CR.sub.2 -- or --CR.sub.2 --X.sup.4 --whereinX.sup.4 is oxy, thio, sulphinyl, sulphonyl or carbonyl and each R is hydrogen, methyl or ethyl;each of Ar.sup.2 and Ar.sup.3 is optionally substituted phenylene;X.sup.2 is oxy, thio, sulphinyl or sulphonyl;R.sup.1 is (1-4C)alkyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.1 --X.sup.3 --A.sup.2 -- which together with the carbon atom to which A.sup.1 and A.sup.2 are attached define a ring having 5 to 7 ring atoms, wherein each of A.sup.1 and A.sup.2 is (1-3C)alkylene and X.sup.Type: GrantFiled: April 14, 1993Date of Patent: January 4, 1994Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Robert I. Dowell, Philip N. Edwards, Keith Oldham
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Patent number: 5264440Abstract: Compounds having the formula (I): ##STR1## in which any two of K, L and M are nitrogen and the other is CE; X and Y are independently hydrogen, halogen, C.sub.1-4 alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, C.sub.2-4 alkynyloxy, phenyl, benzyloxy, cyano, isocyano, isothiocyanato, nitro, NR.sup.1 R.sup.2, NR.sup.1 OR.sup.2,N.sub.3, NHCOR.sup.1, NR.sup.1 CO.sub.2 R.sup.2, NHCONR.sup.1 R.sup.2, N.dbd.CHNR.sup.1 R.sup.2, NHSO.sub.2 R.sup.1, OR.sup.1, OCOR.sup.1, OSO.sub.2 R.sup.1, SR.sup.1, SOR.sup.1, SO.sub.2 R.sup.1, SO.sub.2 OR.sup.1, SO.sub.2 NR.sup.1 R.sup.2, COR.sup.1, CR.sup.1 .dbd.NOR.sup.2, CHR.sup.1 CO.sub.2 R.sup.2, CO.sub.2 R.sup.1, CONR.sup.1 R.sup.2, CSNR.sup.1 R.sup.2, CH.sub.3 O.sub.2 C.C:CH.OCH.sub.Type: GrantFiled: July 20, 1992Date of Patent: November 23, 1993Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Ian T. Streeting, Rex Cheetham
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Patent number: 5248683Abstract: Compounds of the formula ##STR1## in which A.sub.1 and A.sub.2 independently of one another are CO--C.sub.1 -C.sub.4 alkyl, COO--C.sub.1 -C.sub.4 alkyl, CO--CF.sub.3, CO--N(R).sub.2 or cyano;A.sub.1 and A.sub.2 together are CO(X).sub.n --C.sub.1 -C.sub.3 alkylene-(X).sub.n CO, CO(X).sub.n --C.sub.1 -C.sub.3 alkylene-(X).sub.n CO which is substituted by C.sub.1 -C.sub.4 alkyl, COOR, CON(R).sub.2, cyano or phenyl, it being possible for the phenyl ring, in turn, to be substituted by halogen, methyl, trifluoromethyl, methoxy, nitro or cyano; CO--N(R)--CO--N(R)--CO;R is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl or C.sub.3 -C.sub.6 alkynyl;X is oxygen, sulfur or N(CH.sub.3);X.sub.1, X.sub.2 and X.sub.3 independently of one another are hydrogen, halogen, methyl, methylthio, methoxy or nitro;n is 0 or 1;including the salts of the compounds of the formula I with agriculturally acceptable organic or inorganic bases, and including the metal complexes; have valuable microbicidal properties.Type: GrantFiled: June 4, 1992Date of Patent: September 28, 1993Assignee: Ciba-Geigy CorporationInventors: Hans-Georg Brunner, Walter Kunz, Rolf Schurter
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Patent number: 5245040Abstract: A process for the preparation of 1,3-disubstituted 2-nitroguanidines of the formula I ##STR1## in which R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or a radical --CH.sub.2 B; A is an unsubstituted or mono- to tetrasubstituted aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical, which may contain one or two substituents from the group comprising C.sub.1 -C.sub.3 haloalkyl having 1 to 7 halogen atoms, cyclopropyl, halocyclopropyl having 1 to 3 halogen atoms, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.3 alkynyl, C.sub.2 -C.sub.3 haloalkenyl and C.sub.2 -C.sub.3 haloalkynyl having 1 to 4 halogen atoms, C.sub.1 -C.sub.3 haloalkoxy having 1 to 7 halogen atoms, C.sub.1 -C.sub.3 alkylthio, C.sub.1 -C.sub.3 haloalkylthio having 1 to 7 halogen atoms, allyloxy, propargyloxy, allylthio, propargylthio, haloallyloxy, haloallylthio, cyano and nitro and one to four substituents from the group comprising C.sub.1 -C.sub.3 alkyl, C.sub.Type: GrantFiled: October 16, 1991Date of Patent: September 14, 1993Assignee: Ciba-Geigy CorporationInventors: Peter Maienfisch, Odd Kristiansen, Laurenz Gsell
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Patent number: 5239070Abstract: There are provided alkyl esters of 5-heterocyclic-pyridine-2,3-dicarboxylic acids useful as intermediates for the preparation of highly effective 5-heterocyclic-2-(2-imidazolin-2-yl)pyridine herbicidal agents and methods for the preparation thereof.Type: GrantFiled: June 11, 1991Date of Patent: August 24, 1993Assignee: American Cyanamid CompanyInventor: John M. Finn
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Patent number: 5190955Abstract: Antibacterial 8-cyano-1-cyclopropyl-1,4-dihydro-4-oxo-3-quinolinecarboxlyic acid derivatives of the formula ##STR1## in which Y represents a carboxyl group, a nitrile group, an ester group --COOR.sup.1 or an acid amide group --CONR.sup.2 R.sup.3,X.sup.1 represents hydrogen nitro, alkyl or halogenX.sup.4 can be hydrogen or halogen, or alkyl,R.sup.4 and R.sup.5, together with the nitrogen atom to which they are bonded, form a 5- or 6-membered heterocyclic ring which can additionally contain the atoms or groups --O--, --S--, --SO--, --SO.sub.2 --, ##STR2## as ring members or the group ##STR3## can also represent a ring system of the structure ##STR4## which can optionally be substituted on the ring carbons by methyl and pharmaceutically usable hydrates, salts or esters thereof.These compounds have a high antibacterial activity and are therefore suitable as active compounds for human and veterinary medicine.Type: GrantFiled: January 25, 1991Date of Patent: March 2, 1993Assignee: Bayer AktiengesellschaftInventors: Michael Schriewer, Klaus Grohe, Uwe Petersen, Ingo Haller, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler
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Patent number: 5179091Abstract: Compounds of general formula (I): in which: ##STR1## R.sub.1, X, Y, Z, T, R.sub.2, R.sub.3 and R.sub.4 are defined in the description. Medicinal products.Type: GrantFiled: June 3, 1991Date of Patent: January 12, 1993Assignee: Adir et CompagnieInventors: Daniel Lesieur, Daniel H. Caignard, Isabelle Lesieur, Michelle Devissaguet, Beatrice Guardiola
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Patent number: 5162325Abstract: Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists.Type: GrantFiled: May 7, 1991Date of Patent: November 10, 1992Assignee: Merck & Co., Inc.Inventors: Prasun K. Chakravarty, Malcolm MacCoss, Nathan Mantlo, Thomas F. Walsh
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Patent number: 5158959Abstract: What are disclosed are aminoacid compounds of the formula ##STR1## wherein n is 0 or 1, and salts thereof, said compounds and salts having hypotensive properties; methods for making the compounds; pharmaceutical compositions containing the compounds or salts; and use of the compounds and salts for treating hypertension.Type: GrantFiled: December 27, 1983Date of Patent: October 27, 1992Assignee: Hoechst AktiengesellschaftInventors: Rolf Geiger, Volker Teetz, Hansjorg Urbach, Bernward Scholkens, Rainer Henning
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Patent number: 5149872Abstract: A new process for preparing oxalyl- and oxamyl-hydrazides which comprises contacting oxamide or diacetyloxamide with the corresponding hydrazine derivative of formulaR.sub.1 R.sub.2 N--NHR.sub.3wherein R.sub.1 represents a hydrogen atom or an optionally substituted alkyl, cycloalkyl, aryl, or aryl-alkyl group, R.sub.2 is a hydrogen atom or an optionally substituted alkyl group, or R.sub.1 and R.sub.2 taken together with the adjacent nitrogen atom represent a saturated heterocyclic ring, and R.sub.3 is a hydrogen atom or an optionally substituted alkyl group.Type: GrantFiled: February 14, 1991Date of Patent: September 22, 1992Assignee: Enichem Anic S.p.A.Inventors: Giuseppe Messina, Loreno Lorenzoni, Paolo Calaresu, Giovanni M. Sechi
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Patent number: 5135563Abstract: The present invention relates to a pyrimidine derivative having the formula ##STR1## (wherein the variables are defined in the full text of the patent), a method for producing the same, and its use as a herbicide.Type: GrantFiled: July 5, 1991Date of Patent: August 4, 1992Assignee: Sumitomo Chemical Company, LimitedInventors: Mitsunori Hiratsuka, Naonori Hirata, Kazuo Saitoh, Hideyuki Shibata
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Patent number: 5136034Abstract: Thioacids, thiols, an acid, and an aldehyde are used to produce chiral thioacetals of the general formula. ##STR1## The compounds are leukotriene antagonists.Type: GrantFiled: October 5, 1990Date of Patent: August 4, 1992Assignee: Merck Frosst Canada, Inc.Inventors: Robert N. Young, Michel Therien, Jacques-Yves Gauthier, Robert Zamboni, Michel L. Belley
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Patent number: 5135926Abstract: New soft .beta.-adrenergic blocking agents, useful in the treatment or prevention of cardiovascular disorders and in the treatment of glaucoma, have the formula ##STR1## wherein n is an integer from 0 to 10; R is C.sub.6 -C.sub.12 cycloalkyl-C.sub.p H.sub.2p -, C.sub.6 -C.sub.18 polycycloalkyl-C.sub.p H.sub.2p -, C.sub.6 -C.sub.18 polycycloalkenyl-C.sub.p H.sub.2p - or C.sub.6 -C.sub.12 cycloalkenyl-C.sub.p H.sub.2p - (wherein p is 0, 1, 2 or 3), or together with the adjacent ##STR2## group represents a variety of other complex ester groupings; R.sub.1 is C.sub.1 -C.sub.7 alkyl; and Ar is a divalent radical containing at least one aromatic nucleus. The corresponding pharmaceutically acceptable acid addition salts are also described.Type: GrantFiled: April 26, 1991Date of Patent: August 4, 1992Inventor: Nicholas S. Bodor
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Patent number: 5130315Abstract: Novel 1-piperazinyl-2-butenes and -2-butynes, intermediates and processes for the preparation thereof, and methods of treating psychoses utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: January 10, 1991Date of Patent: July 14, 1992Assignee: Raymond R. WittekindInventors: Helen H. Ong, Nicholas J. Hrib, Joseph Perez, John G. Jurcak
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Patent number: 5125957Abstract: A pyrimidine derivative represented by the formula ##STR1## wherein the variables are defined below in the specification, and their production and herbicidal activities are described.Type: GrantFiled: October 24, 1990Date of Patent: June 30, 1992Assignee: Sumitomo Chemical Company, LimitedInventors: Mitsunori Hiratsuka, Naonori Hirata, Kazuo Saito, Hideyuki Shibata
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Patent number: 5124322Abstract: Novel compounds of formula (I), salts, solvates and hydrates thereof: ##STR1## in which: R.sub.1 and R.sub.2 are independently hydrogen; alkyl; alkoxy; halogen; or CF.sub.3 ;R.sub.3 is hydrogen; acyl, such as ##STR2## where Z is optionally substituted aryl; or a group R--S-- where R is an organic residue such that the group R--S-- provides an in vivo-cleavable disulphide bond;R.sub.4 is C.sub.3-6 alkyl;R.sub.5 is hydrogen; alkyl; --CH.sub.2 --R.sub.10 where R.sub.10 is optionally substituted phenyl or heteroaryl; or a group ##STR3## where R.sub.11 is hydrogen; alkyl; or --CH.sub.2 --Ph is optionally substituted phenyl; and R.sub.12 is hydrogen or alkyl; andR.sub.6 is hydrogen; alkyl; or a group ##STR4## where R.sub.13 is hydrogen; or alkyl; and R.sub.14 is hydroxy; alkoxy; or --NR.sub.7a R.sub.8 where each of R.sub.7a and R.sub.8 is hydrogen or alkyl, or R.sub.7a and R.sub.Type: GrantFiled: June 19, 1989Date of Patent: June 23, 1992Assignee: Beecham Group p.l.c.Inventor: Ian Hughes
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Patent number: 5120843Abstract: The aromatic amines (I), alkyl amines (II), bicyclic amines (III). ##STR1## cycloalkyl amines (IV), aromatic bicyclic amines (V), hydroquinone amines (VI), quinone amines (VII), amino-ethers (VIII) and bicyclic amino ethers (IX) are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc. Also disclosed is a method of treatment using the 3,4-dihydrobenzopyrans (XI).Type: GrantFiled: October 23, 1989Date of Patent: June 9, 1992Assignee: UpjohnInventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer
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Patent number: 5098466Abstract: Substituted semicarbazones, thiosemicarbazones and isothiosemicarbazones and salts thereof, intermediates therefor, synthesis thereof, and the use of said compounds for the control of weeds.Type: GrantFiled: August 21, 1990Date of Patent: March 24, 1992Assignee: Sandoz Ltd.Inventors: Richard J. Anderson, Michael M. Leippe, Joe T. Bamberg
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Patent number: 5096902Abstract: The invention relates to novel nitrogen- and sulfur-containing heterocyclic compounds of the formula (I), acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the formula (I) ##STR1## Ar stands for an optionally mono- or polysubstituted aryl or heteroaryl group;R.sup.1 means a carbonyl or (C.sub.2-6 alkenyl)carbonyl group;R.sup.2 stands for hydrogen C.sub.1-6 alkyl, phenyl or phenyl (C.sub.1-4 alkyl) group;R.sup.3 means hydrogen or (C.sub.1-6 alkoxy)carbonyl group;R.sup.4 and R.sup.5 stand, independently from each other, for hydrogen or C.sub.1-6 alkyl group;R.sub.6 ogen, C.sub.1-6 alkyl group or halophenyl group;m is 0 or 1; andn is 1 or 2,with the proviso that R.sup.2 means hydrogen when m is 0.The compounds of formula (I) show a significant cerebral antihypoxic action and thus, they can be used for the treatment of diseases caused by hypoxic brain damages such as e.g.Type: GrantFiled: April 12, 1990Date of Patent: March 17, 1992Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Karoly Nador, Pal Scheiber, nee Szelecsenyi Andrasi, Bela Molnar, Laszlo Szporny, Bela Kiss, Egon Karpati, Eva Palosi, Dora Groo, Istvan Laszlovszky, Zsolt Szombathelyi, Adam Sarkadi, Aniko Gere, Mihaly Bodo, Katalin Csomor, Judit Laszy, Zsolt Szentirmay
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Patent number: RE34299Abstract: The present invention relates to novel indole derivatives which have interesting pharmacodynamic effects indicating pronounced activity in the treatment of psychic disorders, especially psychoses and, at the same time, a low degree of undesired side effects.Moreover, the invention relates to methods for the preparation of said indole derivatives, pharmaceutical compositions containing same, and methods for the treatment of psychic disorders, especially psychoses, by administering a therapeutically active amount of one of said derivatives to a living animal body, including human beings.The novel indole derivatives of the present invention are represented by the following formula; ##STR1## wherein R is phenyl, optionally substituted with halogen.[., lower alkyl or trifluoromethyl,.]. or a hetero aromatic group, such as 2-thienyl, 3-thienyl, .[.2-furoyl, 3-furoyl, 2-thiazol, 2-oxazol, 2-imidazole, 2-pyridyl, 3-pyridyl.]. .Iadd.2-oxazolyl, 2-imidazolyl, 2-pyridyl 3-pyridyl.Iaddend.or 4-pyridyl; R.sup.Type: GrantFiled: September 13, 1991Date of Patent: June 29, 1993Assignee: H. Lundbeck A/SInventor: Jens K. Perregaard