Chalcogen Attached Indirectly To The Thiazole Ring By Nonionic Bonding Patents (Class 548/193)
-
Patent number: 5185450Abstract: Novel tetrazolium salts, which are biologically reducible to blue water-soluble formazan compounds by living cells, are utilized in cell culture viability assays.Type: GrantFiled: June 12, 1992Date of Patent: February 9, 1993Assignee: University of South FloridaInventor: Terence C. Owen
-
Patent number: 5183827Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where X is S, O or NR'; where R' is hydrogen or lower alkyl; R.sub.1, R.sub.2 and R.sub.3 are hydrogen or lower alkyl; R.sub.4 and R.sub.5 are hydrogen or lower alkyl with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen, A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl or oxazolyl; n is 0-5, and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR.sub.1 or a ketal derivative where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 18, 1991Date of Patent: February 2, 1993Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna
-
Patent number: 5182402Abstract: A method of killing or controlling unwanted plants by applying to the plant on to a locus thereof an effective amount of a compound of formula (I) ##STR1## or a salt thereof: wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are independently selected from hydrogen, hydroxy, alkyl, alkoxy, alkylcarbonyl, halogen, cyans, nitro, haloalkyl and haloalkoxy; R.sup.6 is hydrogen, hydroxy, amino, lower alkyl, halogen, cyano, haloalkyl, nitro, aryl, or a group C(O).sub.m R.sup.10, wherein R.sup.10 is hydrogen, alkyl, alkenyl, alkynyl or phenyl any of which may be optionally substituted and m is 1 or 2; R.sup.7 is hydrogen, lower alkyl, haloalkyl, C(O).sub.m R.sup.10 or halogen; or R.sup.6 and R.sup.7 together form an optionally substituted alkylene chain of 2 or 3 carbon atoms; R.sup.8 is hydrogen, lower alkyl or halogen or the group R.sup.7 or R.sup.8 together form an oxo group; and the group CZR.sup.9 is carboxy or an ester thereof, or R.sup.9 is a group SR.sup.10 or NR.sup.11 R.sup.12 wherein R.sup.Type: GrantFiled: September 19, 1991Date of Patent: January 26, 1993Assignee: Imperial Chemical Industries PLCInventors: Terence Lewis, Harjinder S. Bansal, Raymond L. Sundley, Michael R. Bartley, Walter Hepworth, David J. Gilman, Ian T. Kay, David J. Collins
-
Patent number: 5179207Abstract: Provided are certain substituted 2-aminothiazoles and 2-aminothiophenes which are useful as red colorants and as intermediates in the synthesis of bathochromic azo dyes. These compounds are prepared by reacting 2-aminothiophenes or 2-aminothiazoles, which contain a primary amino group, with 2-chloro-3-negatively-substituted maleimides. These compounds can be diazotized and coupled with azo components, for example, anilines, 1,2,3,4-tetrahydroquinolines, 2,3-dihydroindoles, and 3,4-dihydro-2H-1,4-benzoxazines to form bathochromic blue-cyan azo dyes.Type: GrantFiled: August 19, 1991Date of Patent: January 12, 1993Assignee: Eastman Kodak CompanyInventors: James J. Krutak, Max A. Weaver
-
Patent number: 5177095Abstract: Substituted triazoles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I, are useful as angiotensin II antagonists.Type: GrantFiled: August 13, 1991Date of Patent: January 5, 1993Assignee: Merck & Co., Inc.Inventors: William J. Greenlee, Arthur A. Patchett, David Hangauer, Wallace Ashton, Kenneth J. Fitch, Thomas F. Walsh, Ralph A. Rivero, Daljit S. Dhanoa
-
Patent number: 5132412Abstract: Thiazoleazo dyes of the formula ##STR1## where X is nitrogen or a radical C--R.sup.5, R.sup.5 being cyano, halogen, alkoxycarbonyl or thiocyanato, R.sup.1 is cyano, chlorine, unsubstituted or substituted C.sub.1 -C.sub.6 -alkyl, unsubstituted or substituted phenyl, unsubstituted or substituted thienyl, unsubstituted or substituted pyridyl or unsubstituted or substituted alkylthio, alkylsulfinyl or alkylsulfonyl, R.sup.2 is unsubstituted or substituted alkyl, cycloalkyl, unsubstituted or substituted phenyl, furyl, unsubstituted or substituted thienyl or pyridyl and R.sup.3 and R.sup.4 independently of one another are each unsubstituted or substituted alkyl, or R.sup.3 and R.sup.4, together with the nitrogen atom which links them, form a heterocyclic radical, are used for dyeing textile fibers having good wet fastness and color build-up.Type: GrantFiled: September 15, 1989Date of Patent: July 21, 1992Assignee: BASF AktiengesellschaftInventors: Guenter Hansen, Gunther Lamm, Helmut Reichelt, Ernst Schefczik
-
Patent number: 5104889Abstract: This invention provides thiazole derivative of the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A are as defined above, and salts thereof. These compounds have particularly potent angiogenesis inhibiting activity.Type: GrantFiled: May 29, 1990Date of Patent: April 14, 1992Assignee: Otsuka Pharmaceutical Factory, Inc.Inventors: Kenichi Kanai, Kiyoto Goto, Kinji Hashimoto, Yoshiaki Tsuda
-
Patent number: 5104890Abstract: Benzopyrene derivatives effective for the treatment of hypertension have been prepared.Type: GrantFiled: March 8, 1990Date of Patent: April 14, 1992Assignee: Fujisawa Pharmaceutical Company, Ltd.Inventors: Youichi Shiokawa, Koichi Takimoto, Kohei Takenaka, Takeshi Kato
-
Patent number: 5096914Abstract: Benzopyran derivatives of the general formula I ##STR1## wherein the substituents are as defined herein are provided. The compounds show vasodilating and vascular spasmolytic activity and are useful in treating hypertension.Type: GrantFiled: November 30, 1990Date of Patent: March 17, 1992Assignee: Beiersdorf AktiengesellschaftInventors: Wolfgang Stenzel, Theo Schotten, Ben Armah
-
Patent number: 5089512Abstract: The invention provides thiazole derivatives of the general formula I: ##STR1## or acid-addition salts or metal salt complexes thereof, in which R represents an optionally substituted phenyl group; A represents a group ##STR2## R.sup.1 represents a hydrogen atom or an optionally substituted alkyl, alkenyl or aralkyl group; and R.sup.2 represents a hydrogen or halogen atom or an alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, hydroxyl, cyano, nitro, amino, alkylamino or dialkylamino group; processes for their preparation; compositions containing such compounds and their use as fungicides.Type: GrantFiled: April 23, 1990Date of Patent: February 18, 1992Assignee: Shell Research LimitedInventors: John R. H. Wilson, Indu Sawhney
-
Patent number: 5071864Abstract: Aminoalkyl-substituted 2-aminothiazole derivatives of the general formula I ##STR1## where R.sup.1 and R.sup.2, which may be identical or different, are each hydrogen, C.sub.1 -C.sub.5 -alkyl, phenyl or C.sub.1 -C.sub.5 -alkanoyl, R.sup.3 is C.sub.1 -C.sub.5 -alkyl, phenyl which is unsubstituted or monosubstituted by halogen, C.sub.1 -C.sub.5 -alkyl or C.sub.1 -C.sub.5 -alkoxy, or thienyl,n is an integer of from 2 to 6, andNR.sup.4 R.sup.5 is one of the groups a, b, c or d ##STR2## where Ar is a phenyl ring which is unsubstituted or monosubstituted by C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -alkoxy, halogen, hydroxyl, nitro or trifluoromethyl, or is pyridyl, pyrimidinyl or thienyl, R.sup.5 is H or C.sub.1 -C.sub.5 -alkyl and R.sup.7 is phenyl which is unsubstituted or monosubstituted by C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -alkoxy, halogen, hydroxyl or trifluoromethyl, or R.sup.7 is thienyl, with the proviso that R.sup.3 is C.sub.1 -C.sub.5 alkyl only when either R.sup.1 and R.sup.Type: GrantFiled: June 28, 1990Date of Patent: December 10, 1991Assignee: BASF AktiengesellschaftInventors: Beatrice Rendenbach-Mueller, Liliane Unger, Hans-Juergen Teschendorf
-
Patent number: 5028715Abstract: A radioprotective agent consisting essentially of 3-(3"-aminoalkyl)-2-arylthiazolidine or a pharmacologically acceptable salt thereof having the formula: ##STR1## wherein R is a NH.sub.2 R' or XNHR' radical in which R' is a C.sub.2 to C.sub.4 alkyl group and X is a C.sub.1 to C.sub.3 alkyl group and Ar is an aromatic aldehyde moiety; or a pharmacologically acceptable salt thereof.Type: GrantFiled: February 6, 1989Date of Patent: July 2, 1991Assignee: Southwest Research InstituteInventors: Robert E. Lyle, William A. McMahon, Donald J. Mangold, Nollie F. Swynnerton
-
Patent number: 5028711Abstract: Benzopyran derivatives of the general formula I ##STR1## are disclosed. The compounds are therapeutic active compounds.Type: GrantFiled: July 6, 1989Date of Patent: July 2, 1991Assignee: Beiersdorf AktiengesellschaftInventors: Wolfgang Stenzel, Theo Schotten, Ben Armah
-
Patent number: 4996218Abstract: Compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, which have .beta..sub.2 -adrenoreceptor stimulant activity. They may be used in the treatment of diseases associated with reversible airways obstruction, such as asthma and chronic bronchitis.In preferred embodiments, Q represents a chlorine atom or a trifluoromethyl group, X represents a C.sub.3-4 alkylene chain, Y a C.sub.1-5 alkylene chain, R, R.sup.1 and R.sup.2 are each preferably a hydrogen atom or a methyl group and Het represents a pyrimidinyl pyrazinyl, triazinyl, thiazolyl, quinolinyl, benzimidazolyl, benzothiazolyl, benzoxazolyl or pyridyl group.Type: GrantFiled: August 10, 1988Date of Patent: February 26, 1991Assignee: Glaxo Group LimitedInventor: Lawrence H. C. Lunts
-
Patent number: 4988723Abstract: Benzopyran derivatives of formula (I) wherein the substituents are as defined herein are provided. The compounds possess vasodilating activity and are useful in the treatment of hypertension. Pharmaceutical compositions and methods of treating hypertension are also provided.Type: GrantFiled: May 17, 1989Date of Patent: January 29, 1991Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Youichi Shiokawa, Koichi Takimoto, Kohei Takenaka, Takeshi Kato
-
Patent number: 4987146Abstract: N-hetaryl imidazole derivatives of general Formula I ##STR1##are disclosed in whichHet represents an optionally substituted monocyclic or bicyclic heteroaromate,R.sup.3 represents hydrogen, a straight or branched C.sub.1-6 -alkyl group, or a C.sub.1-6 -alkoxy-alkyl group, andR.sup.4 represents --COOR.sup.5 --CONR.sup.6 R.sup.7 --CN, ##STR2##with R.sup.5 meaning hydrogen, a straight or branched C.sub.1-6 -alkyl group, R.sup.6 and R.sup.7 are the same of different and represent hydrogen or a straight, branched, or cyclic alkyl group with up to 7 carbon atoms or, together with the nitrogen atom, form a saturated five or six ring optionally containing another heteroatom and R.sup.8 means hydrogen or a straight, branched or cyclic alkyl group with up to 7 carbon atoms.Type: GrantFiled: July 14, 1989Date of Patent: January 22, 1991Assignee: Schering AktiengesellschaftInventors: Ralph Rohde, Helmut Biere, Ralph Schmiechen, John S. Andrews, David N. Stephens
-
Patent number: 4942243Abstract: A process for preparing N"-[4-[[(2-cyanoethyl)thiol]methyl]-2-thiazolyl]guanidine which comprises reacting a dihaloacetone with an .beta.-cyanoethylthiol in a two phase solvent system at a pH of 4.5-6.0 to produce a 1-halo-3-(2-cyanoethylthio)propanone and reacting the 1-halo-3-(2-cyanoethylthio) with an amidinothiourea.Type: GrantFiled: April 8, 1988Date of Patent: July 17, 1990Assignee: Hanil Pharmaceutical Ind., Co., Ltd.Inventors: Moon G. Koh, Jai M. Shin, Dong S. Kim, Choon S. Lee
-
Patent number: 4935049Abstract: New substituted azolylmethylcarbinols of the formula ##STR1## in which Ar stands for optionally substituted aryl,Z stands for nitrogen or an CH group andR stands for alkyl, dialkylaminoalkyl, alkenyl, alkinyl, alkoxyalkyl, optionally substituted aralkyl, optionally substituted aryloxyalkyl, optionally substituted aryl or a radical of the formula ##STR2##whereinR.sup.1 stands for hydrogen, alkyl, alkenyl, alkinyl or cycloalkyl andR.sup.2 stands for hydrogen, alkyl, alkoxyalkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, for optionally substituted aryl or for optionally substituted aralkyl, orR.sup.1 and R.sup.2 together with the nitrogen atom to which they are bonded stand for an optionally substituted heterocyclic ring which cna optionally contain further heteroatoms,and acid addition salts and metal salt complexes thereof, and the use of the novel compounds as fungicides and plant growth regulators.Type: GrantFiled: October 7, 1988Date of Patent: June 19, 1990Assignee: Bayer AktiengesellschaftInventors: Wolfgang Kramer, Erik Regel, Karl H. Buchel, Stefan Dutzmann, Wilhelm Brandes, Klaus Lurssen
-
Patent number: 4913722Abstract: A 2-iminophenyl thiazolidine having the formula ##STR1## wherein R is hydrogen or methyl; R.sub.1 is halo, nitro, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, perhalomethyl, difluoromethyl, pentafluoroethyl, trifluoromethylthhio, difluoromethoxy, trifluoromethoxy, tetrafluoroethoxy, methylsulfonyl, C.sub.1 -C.sub.4 alkyloxyiminomethyl, benzyloxyiminomethyl, 1-(C.sub.1 -C.sub.4 alkyl)-oxyiminoethyl or 1-benzyloxyiminoethyl; R.sub.2 is hydrogen or halo; R.sub.3 and R.sub.4 are independently hydrogen, halo, nitro, cyano, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 fluoroalkoxy, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio; and X is hydrogen or halogen.Also disclosed is a process for making the compounds and a method of use which comprises applying the compound or composition to the locus where control is desired.Type: GrantFiled: November 15, 1988Date of Patent: April 3, 1990Assignee: ICI Americas Inc.Inventors: Raymond A. Felix, Jeffery T. Springer, Eugene G. Teach, Frank X. Woolard
-
Patent number: 4908454Abstract: A process is provided for producing a guanidinothiazole compound represented by the formula: ##STR1## wherein, R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen or an alkyl group having 1 to 3 carbon atoms; m represents 1 or 2; and n represents 2, 3 or 4. The process comprises reacting an aminothiazole compound of the formula: ##STR2## with a cyanamide or an amidinopyrazole, the compounds are useful as intermediates in the preparation of a gastric acid secretion inhibitor.Type: GrantFiled: January 23, 1989Date of Patent: March 13, 1990Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Yoshio Ishii, Isao Yanagisawa
-
Patent number: 4892871Abstract: The invention is directed to azido-substituted octopamine agonists and the radiolabeled derivatives thereof. The invention also relates to past controlling compositions comprising the azido-substituted octopamine agonists of the invention.The invention also relates to methods of controlling invertebrate pests by bringing the pest into contact with an invertebrate pest-controlling composition of the invention and to an apparatus for controlling invertebrate pests utilizing the pest-controlling compositions of the invention. The pest-controlling compositions may be used alone or in conjunction with ultraviolet light.The invention also relates to methods for the isolation of octopamine receptor proteins utilizing the radiolabeled azido-substituted octopamine agonists of the invention.Type: GrantFiled: April 12, 1988Date of Patent: January 9, 1990Assignee: The General Hospital CorporationInventor: James A. Nathanson
-
Patent number: 4876261Abstract: A compound of the formula (I) or its salt and a process for producing the compounds; The compounds have the effect to dilate neophrovascular tracts; ##STR1## wherein ##STR2## represents the formula ##STR3## (wherein R.sup.4 is a hydrogen atom or lower alkylsulfonyl); R.sup.1 is hydrogen, lower alkyl, hydroxyl, halogen, amino, or lower acylamino;R.sup.2 is hydrogen, lower alkyl, hydroxyl, amino, or lower alkylsulfonylamino;R.sup.3 is hydrogen, lower, alkyl or hydroxyl;R is hydrogen or halogen;with the proviso that when R.sup.1 is hydroxyl, there is no case that all of R.sup.2, R.sup.3 and R are hydrogens, and further with the proviso that when R is hydrogen, A excludes ##STR4## or a salt thereof.Type: GrantFiled: March 25, 1988Date of Patent: October 24, 1989Inventors: Akihiro Tanaka, Takashi Fujikura, Ryuji Tsuzuki, Masaki Yokota, Takeyuki Yatsu
-
Patent number: 4863947Abstract: This invention relates to novel N-aryl-3-aryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.Type: GrantFiled: August 11, 1986Date of Patent: September 5, 1989Assignee: Rohm and HaasInventor: Richard M. Jacobson
-
Patent number: 4861789Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable acid addition salt and/or a pharmaceutically acceptable solvate thereof, wherein A represents a residue of a benzene ring optionally having up to four substituents selected from the group consisting of halogen, C.sub.1-6 alkyl aNd C.sub.1-6 alkoxy; R.sup.1 and R.sup.2 each independently represent a hydrogen atom or a C.sub.1-6 alkyl group; X represents a bond or a moiety CHR.sup.1 wherein R.sup.1 is as defined above; and Z represents O, NH or S.Type: GrantFiled: May 4, 1987Date of Patent: August 29, 1989Assignee: Beecham Group plcInventors: John Berge, Lee J. Beeley
-
Patent number: 4849432Abstract: Novel heterocyclic compounds of the formula ##STR1## wherein, R.sup.1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by alkyl, X represents an oxygen or sulfur atom or the group ##STR2## in which R.sup.2 represents a hydrogen atom of an optionally substituted alkyl, an alkenyl, an alkynyl or an acyl group, and R.sup.3 represents a hydrogen atom or an alkyl group, and Z represents an optionally sibstituted 5- or 6-membered heterocyclic group which contains at least two hetero atoms selected from oxygen, sulfur and nitrogen atoms, or an optionally substituted 3- or 4-pyridyl group.The above defined novel heterocyclic compounds of formula (I) exhibit powerful insecticidal properties.Type: GrantFiled: February 24, 1987Date of Patent: July 18, 1989Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Shoko Sasaki, Koichi Moriya, Yumi Hattori
-
Patent number: 4847274Abstract: The present invention relates to 4-phenylthiazole derivatives, namely 2-(2-hydroxyethylamino)-4-phenylthiazole and its addition salts.These derivatives act on the CNS and are useful as sedatives.Type: GrantFiled: September 22, 1987Date of Patent: July 11, 1989Assignee: Laboratoire L. LafonInventor: Louis Lafon
-
Patent number: 4845219Abstract: A compound of the general formula [I]: ##STR1## wherein R.sub.1 represents a higher alkyl group or an N-(higher alkyl)carbamoyl group, R.sub.2 represents a lower alkyl group, an acyl group having at least three carbon atoms, an N-(lower alkyl)carbamoyl group, an N-(lower alkyl)thiocarbamoyl group or a benzyl group, R represents a primary, secondary or tertiary amino group or a quaternary ammonium group, x is 1 or 2, y is a number of 0, 1 or 2, and z is an integer of 2-10, or a pharmaceutically acceptable salt thereof. The novel substances have both anti-tumor activity and platelet activating factor-inhibiting property, and they are effective as an anti-tumor agent without circulatory trouble.Type: GrantFiled: July 23, 1987Date of Patent: July 4, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Keizo Inoue, Hiroaki Nomura, Tetsuya Aono
-
Patent number: 4826990Abstract: There are disclosed compounds of the formula ##STR1## wherein X is ##STR2## Y is ##STR3## Z is ##STR4## R.sup.1 is ##STR5## n is 0-5; R.sup.2 is hydrogen, loweralkyl, loweralkoxy, lower alkoxycarbonyl, trifluoromethyl, nitro, cyano or halo;R.sup.3 is ##STR6## W represents a bond or ##STR7## m is 1-15; R.sup.4 is hydrogen or loweralkyl;R.sup.5 is lower alkyl, monofluoroloweralkyl, difluoroloweralkyl, polyfluoroloweralkyl, perfluoroloweralkyl or ##STR8## R.sup.6 is hydrogen, lower alkyl, ##STR9## and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, and as antiinflammatory agents.Type: GrantFiled: September 30, 1987Date of Patent: May 2, 1989Assignee: American Home Products CorporationInventors: John H. Musser, Reinhold H. W. Bender, Anthony F. Kreft, III
-
Patent number: 4826861Abstract: This invention relates to 2-aminothiazoles and to their process of manufacture. These compounds are endowed with potent antimicrobial and antifungic properties. They are useful in antibacterial and antifungal therapy.Type: GrantFiled: January 7, 1987Date of Patent: May 2, 1989Assignee: Albert Roland, S.A.Inventors: Moinet Gerard, Schaefer Michel
-
Patent number: 4814341Abstract: A series of novel thiazole compounds, having a guanidino or substituted guanidino group at the 2-position and a 5-(N,N-disubstituted aminomethyl)-2-furyl group at the 4-position. The compounds of the invention are useful for administration to mammals for prophylactic or curative treatment of peptic ulcers.Type: GrantFiled: April 19, 1988Date of Patent: March 21, 1989Inventor: Lawrence A. Reiter
-
Patent number: 4803277Abstract: Novel insecticidally active heterocyclic compounds of the formula ##STR1## wherein W represents a substituted pyridyl group, or a 5- or 6-membered optionally substituted heterocyclic group containing at least two hetero atoms selected from oxygen, sulfur and nitrogen atoms,R represents a hydrogen atom or an alkyl group,Y represents .dbd.N--or ##STR2## R' represents a hydrogen atom, an alkyl group, an aryl group, an acyl group, an alkoxycarbonyl group or a cyano group,Z represents a nitro group or a cyano group, andT represents 3 or 4 optionally substituted ring members of a 5- or 6-membered unsaturated heterocyclic ring which it forms together with the adjoining carbon atom and nitrogen atom, said 5- or 6-membered unsaturated heterocyclic ring containing 1 to 3 hetero atoms which are selected from oxygen, sulfur and nitrogen atoms and at least one of which is a nitrogen atom.Type: GrantFiled: August 24, 1987Date of Patent: February 7, 1989Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shoko Sasaki, Koichi Moriya, Yumi Hattori, Katsuhiko Shibuya
-
Patent number: 4791200Abstract: The present invention relates to novel 2-substituted-4-aryloxyalkylamine thiazoles as described herein. The thiazoles are useful as antisecretory agents.Type: GrantFiled: June 22, 1987Date of Patent: December 13, 1988Assignee: Ortho Pharmaceutical CorporationInventors: Jeffery B. Press, Pauline Sanfilippo, Maud Urbanski
-
Patent number: 4785008Abstract: The subject of the invention is N-substituted 2-aminothiazoles of formula ##STR1## in which: X is a C--H group or a nitrogen atom,R.sub.1 and R.sub.2 are, independently of each other, a hydrogen atom, a halogen atom or an alkyl, alkoxy, alkylthio, alkenyloxy, cycloalkyl, trifluoromethyl, nitro, amino, (C.sub.1 -C.sub.6 alkyl)amino or di(C.sub.1 -C.sub.6 alkyl)-amino radical, andR.sub.3 is a hydrogen atom, a --CH.sub.2 --OH group or a --COOR.sub.4 group, R.sub.4 being a hydrogen atom or an alkyl group,and also the pharmaceutically acceptable salts thereof.These compounds have an anti-inflammatory and antiallergic activity and can be used in therapy, especially in the ocular field.Type: GrantFiled: April 24, 1986Date of Patent: November 15, 1988Assignee: Laboratoires Chauvin-BlacheInventors: Claude Coquelet, Daniel Sincholle, Claude Bonne, Alain Alazet
-
Patent number: 4771062Abstract: A diaryl sulphide derivative of the formula ##STR1## in which R.sup.1 represents a thiazolamino radical of the formulae ##STR2## wherein R.sup.5 represents hydrogen, alkyl, aralkyl or acyl,R.sup.6 and R.sup.6 ' are identical or different and represent hydrogen, alkyl, aralkyl or aryl,R.sup.7 represents alkyl, cycloalkyl, aralkyl, acyl or aryl andn represents the number 1 or 2,R.sup.2 and R.sup.3 are identical or different and represent hydrogen, alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, aryl, aralkyl, aryloxy, aralkoxy, aralkylthio, acyl, carboxyl, alkoxycarbonyl, carboxyalkyl, alkoxycarbonylalkyl, nitro, cyano or halogen, or represent a group of the formula ##STR3## wherein R.sup.8 and R.sup.9 are identical or different and represent hydrogen, alkyl, aryl, aralkyl, acyl, trifluoroacetyl, alkylsulphonyl, arylsulphonyl, trifluoromethylphenylsulphonyl or tolylsulphonyl andR.sup.4 has one of the abovementioned meanings or R.sup.Type: GrantFiled: February 20, 1987Date of Patent: September 13, 1988Assignee: Bayer AktiengesellschaftInventors: Siegfried Raddatz, Hans Plumpe, Romanis Fruchtmann, Christian Kohlsdorfer, Bernhard Pelster
-
Patent number: 4762932Abstract: Compounds useful for inhibiting gastric acid secretion and for the treatment of peptic ulcers caused or exacerbated by gastric acidity having the following formula (I): ##STR1## in which R.sup.1 and R.sup.2, are H, C.sub.1-10 alkyl, C.sub.3-8 cycloalkyl or cycloalkylalkyl in which the alkyl part is C.sub.1-6 and the cycloalkyl part is C.sub.3-8, each of the alkyl, cycloalkyl and cycloalkylalkyls being optionally substituted by one or more halogens selected from F, Cl and Br, provided that at least one of R.sup.1 and R.sup.2 is a halogen substituted alkyl, cycloalkyl or cycloalkylalkyl and provided that there is no halogen substituent on the carbon directly attached to the nitrogen; and X, m, Y, n and R.sup.3 are as described in the specification; and the pharmaceutically-acceptable acid-addition salts thereof.Type: GrantFiled: June 2, 1986Date of Patent: August 9, 1988Assignees: Imperial Chemical Industries, Ltd., ICI Americas, Inc.Inventors: Tobias O. Yellin, Philip N. Edwards, Michael S. Large
-
Patent number: 4761422Abstract: This invention relates to a series of thiazole derivatives having the general formula ##STR1## The compounds of the invention have an interesting diuretic activity and low toxicity.Type: GrantFiled: November 19, 1986Date of Patent: August 2, 1988Assignee: Lusofarmaco Istituto Lusofarmaco d'Italia SpAInventors: Elso Manghisi, Aldo Salimbeni
-
Patent number: 4742060Abstract: 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: January 21, 1986Date of Patent: May 3, 1988Assignee: Nihon Tokushu Noyaku Seizo K. K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
-
Patent number: 4740231Abstract: 1-Aryl-5-alkoximinoalkylamino-pyrazoles of the formula ##STR1## in which R represents cyano or nitro, or represents an optionally substituted heterocyclic radical,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen or alkyl, or represents optionally substituted aryl,R.sup.3 represents hydrogen, alkyl or alkenyl, or represents in each case optionally substituted aralkyl or aryl andAr represents optionally substituted phenyl or pyridyl,are active as herbicides and plant growth regulants. Compounds of the formula ##STR2## in which R" has the same definition as R other than cyano, are also active and useful as intermediates as well.Type: GrantFiled: May 22, 1986Date of Patent: April 26, 1988Assignee: Bayer AktiengesellschaftInventors: Reinhold Gehring, Otto Schallner, Jorg Stetter, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
-
Patent number: 4735957Abstract: New thiazole derivatives of the formula: ##STR1## wherein R.sup.1 is lower alkyl, carboxy, a drivative of carboxy, hydroxymethyl, halomethyl, lower alkylthiomethyl, hydroxyiminomethyl or alkenyl which may be substituted with lower alkoxycarbonyl, pyridyl or cyano,R.sup.2 is hydrogen, hydroxy, lower alkyl, pyridyl, amino, lower alkylamino, pyridylamino, arylamino, acylamino, N-(lower)alkylN-acylamino, guanidino optionally substituted with dimethylaminomethylene, or ar(lower)alkylamino optionally substituted with lower alkoxy,R.sup.3 is lower alkyl, halo(lower)alkyl or N-containing unsaturated heterocyclic group which may be substituted with halogen, lower alkyl, lower alkoxy, carboxy, a derivative of carboxy, hydroxy, pyridyl, amino, lower alkylamino, pyridylamino, arylamino, acylamino, N-(lower)alkyl-N-acylamino, guanidino, N-oxide or ar(lower)alkylamino optionally substituted with lower alkoxy,Q is --CO--, andn is an integer of 0 or 1,provided that when both of R.sup.1 and R.sup.Type: GrantFiled: November 18, 1986Date of Patent: April 5, 1988Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Hisashi Takasugi
-
Patent number: 4728655Abstract: Sulfonamidine is disclosed of the general formula (I):R--NH--CH.dbd.N--SO.sub.2 --R.sub.1 (I)wherein R is a group selected from 2-[[(5-methyl-1H-imidazole-4-yl)methyl]thio]ethyl], 2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethyl, 2-[[[2-[(aminoiminomethyl)amino]-4-thiazolyl]methyl]thio]ethyl] or 3-[3-(1-piperidinylmethyl)phenoxy] propyl and R.sub.1 is alkyl; or a phenyl group optionally substituted by alkyl, halogen, nitro, alkoxy, alkanoylamino, carboxylic acid, alkoxycarbonyl, dialkylamino, alkylsulphonyl, alkylsulphonylamino or alkylthio; or 1,3,4-thiadiazole-2-yl substituted by alkanoylamino, and the pharmaceutically acceptable salts thereof, as well as a process for preparing these compounds and pharmaceutical compositions containing the same. These compounds have antiulcer activity and can be used in the treatment of peptic ulcers and other pathologies caused or stimulated by gastric acidity.Type: GrantFiled: April 18, 1985Date of Patent: March 1, 1988Assignee: Ferrer Internacional S.A.Inventors: Rafael Foguet, Luis Anglada, Josep Castello, Aurelio Sacristan, Jose Ortiz
-
Patent number: 4720493Abstract: Thienylthiazole compounds of the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, wherein: R is amino, guanidino, alkylamino, alkenylamino, unsubstituted or optionally substituted phenylamino or acylamino;A is amino, alkylamino, cyclic amino, alkanoylamino, a group of the formula: ##STR2## wherein each symbol is as defined in claim 1; Z is hydrogen or halogen; andm is 0 or 1 to 4,are useful in the treatment of peptic ulcer, acute or chronic gastritis, acute damage of gastric mucous membrane, dimentia and anxiety.Type: GrantFiled: November 20, 1985Date of Patent: January 19, 1988Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Takeshi Kawakita, Mitsuharu Sano, Mitsuyoshi Yasumoto, Kunio Ohsuga, Kei-ichiro Haga
-
Patent number: 4704157Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: A, B and D are selected from CH and N;E is selected from oxygen and sulfur;X are selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, alkenyl, alkenyloxy, alkynyl, alkynyloxy, acyloxy, alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, sulfamoyl, substituted sulfamoyl, alkanoyloxy, benzyloxy, substituted benzyloxy, phenyl, substituted phenyl, amino, substituted amino, and the groups formyl and alkanoyl and the oxime, imine and Schiff base derivatives thereof;R.sup.1 is selected from hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl, alkylsulfonyl, arylsulfonyl, acyl and an inorglanic or organic cation;R.sup.2 is selected from alkyl substituted alkyl, alkenyl, haloalkenyl, alkynyl and haloalkynyl;R.sup.3 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl, and phenyl;R.sup.Type: GrantFiled: May 8, 1986Date of Patent: November 3, 1987Assignee: CI Australia Ltd.Inventors: Richard J. Conway, Keith G. Watson, Graeme J. Farquharson
-
Patent number: 4698357Abstract: The compound 2,4-dichloro-5-nitro-thiazole of the formula ##STR1## is microbicidally active.Type: GrantFiled: May 15, 1986Date of Patent: October 6, 1987Assignee: Bayer AktiengesellschaftInventors: Gunther Beck, Paul Reinecke, Wilfried Paulus, Hans-Georg Schmitt
-
Patent number: 4692531Abstract: Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.Type: GrantFiled: September 25, 1986Date of Patent: September 8, 1987Assignee: Bristol-Myers CompanyInventors: Aldo A. Algieri, Ronnie R. Crenshaw
-
Patent number: 4684658Abstract: The invention provides novel pyrrole derivatives of formula: ##STR1## in which R'=H, alkyl or phenyl optionally substituted by halogen, alkyl, alkyloxy or alkylthio, Z=0 or S, p=0 or 1, andeither A is a heterocyclic ring such that it forms, with pyrrole, a 1H,3H-pyrrolo[1,2-c]thiazole, 2,3-dihydro-1H-pyrrolizine optionally substituted by OH, 5,6,7,8-tetrahydroindolizine, 1,2-dihydro-4H-pyrrolo[1,2-c]-1,3-thiazine, 2,3-dihydropyrrolo[2,1-b]thiazole, 1H,3H-pyrrolo[1,2-c]oxazole, 1,2-dihydro-4H-pyrrolo]1,2-c]-1,3-oxazine or 2,3-dihydropyrrolo[2,1-b]oxazole ring system, n=0 or 1, Het=3-pyridyl or 5-thiazolyl, and(1) either R=H, halogen, alkyl or phenyl optionally substituted by halogen, alkyloxy or alkylthio and Y=alkyl or phenyl optionally substituted by halogen, alkyl, alkyloxy or alkylthio, or Y=--NR.sub.1 R.sub.2 with:either R.sub.1 =H and R.sub.2 =unsubstituted alkyl, cycloalkyl (C.sub.3 -C.sub.6), alkenyl (C.sub.2 -C.sub.4), alkynyl (C.sub.3 -C.sub.Type: GrantFiled: December 20, 1984Date of Patent: August 4, 1987Assignee: Rhone-Poulenc SanteInventors: Jean-Louis Fabre, Daniel Farge, Claude James, Daniel Lave
-
Patent number: 4680300Abstract: A compound having the formula ##STR1## where Ar=naphthyl, biphenyl, or quinolinyl;X=oxygen or NH;Y=2 to 8;R.sub.1 =phenyl, substituted phenyl, hydrogen, lower alkyl; andR.sub.2 is the same or different from R.sub.3 and is alkyl, cycloalkyl, phenyl, substituted phenyl, thiazolyl; andthe pharmaceutically acceptable salts thereof.Compounds of this general formula are useful as anti-inflammatories, and as anti-psoriatic agents.Type: GrantFiled: January 10, 1985Date of Patent: July 14, 1987Assignee: Syntex (U.S.A.) Inc.Inventors: Peter Nelson, Stefan H. Unger
-
Patent number: 4665083Abstract: The invention relates to novel iminothiazolidine derivatives of the formula (I), ##STR1## wherein R.sup.1 and R.sup.3 represent, independently from each other, hydrogen or lower alkyl group,R.sup.3 is nitro or amino group,R stands for halo, lower alkyl, haloalkyl, nitro, amino, hydroxy, lower alkoxy, carboxy or lower alkoxycarbonyl group, andn is 0, 1 or 2,and pharmaceutically acceptable acid addition salts thereof.The iminothiazolidine derivatives of the formula (I) possess valuable antidepressant, antiparkinsonic, antiepileptic and spasmolytic activities.Type: GrantFiled: April 25, 1985Date of Patent: May 12, 1987Assignee: Egis GyogyszergyarInventors: Karoly Lempert, Gyula Hornyak, Ferenc Bartha, Gabor Doleschall, Jozsef Fetter, Jozsef Nyitrai, Gyula Simig, Karoly Zauer, Peter Huszthy, Antal Feller, Lujza Petocz, Eniko Szirt, Katalin Grasser, Edit Berenyi, Zsuzsanna Orr, Etelka Pjeczka
-
Patent number: 4663341Abstract: This invention relates to N-aryl-3-aryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.Type: GrantFiled: January 11, 1985Date of Patent: May 5, 1987Assignee: Rohm and Haas CompanyInventor: Richard M. Jacobson
-
Patent number: 4656184Abstract: This invention relates to therapeutic compositions comprising, as active ingredient, N-substituted hydrazones having the formula: ##STR1## in which Z is a 2-thienyl or phenyl radical. Said compositions have an anti-inflammatory activity, particularly in the ocular field.Type: GrantFiled: February 7, 1984Date of Patent: April 7, 1987Inventors: Claude Coquelet, Chantal Bertez, Claude Bonne, Daniel Sincholles
-
2-(ethylene-thio methyl furanyl)amino thiazole derivatives having acid secretion inhibiting activity
Patent number: 4652575Abstract: Compound of formula (I) ##STR1## wherein R is an alkyl or an aromatic group, having pharmaceutical utility as an agent for treating a condition mediated through gastric acid secretion for reducing the volume and the acidity of gastric juice.Type: GrantFiled: September 12, 1985Date of Patent: March 24, 1987Assignee: Medosan Industrie Biochimiche Riunite S.p.A.Inventor: Alessandro Baglioni