Nitrogen Attached Directly To The Thiazole Ring By Nonionic Bonding Patents (Class 548/161)
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Patent number: 5391565Abstract: Compounds of the formula: ##STR1## or tautomeric forms and a pharmaceutically acceptable salt, and pharmaceutically acceptable solvates thereof, wherein:A.sup.1 is a substituted or unsubstituted oxazole substituted by up to 4 substituents selected from the group consisting of C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, phenyl, and halogen or any two substituents on adjacent carbon atoms, together with the carbon atoms to which they are attached, form a benzene ring, and wherein the carbon atoms of the benzene ring represented by the said two substituents are unsubstituted or substituted with up to three groups selected from halogen, C.sub.1-6 -alkyl, phenyl, C.sub.1-6 -alkoxy, halo-C.sub.1-6 -alkyl, hydroxy, amino, nitro, carboxy, C.sub.1-6 -alkoxycarbonyl, C.sub.1-6 -alkoxycarbonyl-C.sub.1-6 -alkyl, C.sub.1-6 -alkylcarbonyloxy, and C.sub.1-5 -alkylcarbonyl;R.sup.l is a hydrogen atom, a C.sub.1-6 -alkyl group, a C.sub.1-6 -alkylcarbonyloxy group, a phenyl-C.sub.Type: GrantFiled: February 3, 1993Date of Patent: February 21, 1995Assignee: Beechan Group p.l.c.Inventor: Richard M. Hindley
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Patent number: 5380735Abstract: The present invention relates to a novel benzothiazole derivative of the following general formula (I) or its (E) , (Z)isomer, and processes for preparation thereof, ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 independently of one another represent hydrogen, halogen, straight and branched (C.sub.1 -C.sub.8)alkyl, (C.sub.1 -C.sub.8)halogenoalkyl or (C.sub.1 -C.sub.8)alkoxy,X represents N or CH,Y represents a group -OR.sup.4, SR.sup.5 or ##STR2## R.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently of one another represent hydrogen, straight and branched (C.sub.1 -C.sub.16)alkyl, (C.sub.3 -C.sub.8)alkenyl, (C.sub.3 -C.sub.8)alkynyl, (C.sub.3 -C.sub.8)cycloalkyl, alkyl substituted with (C.sub.1 -C.sub.6)alkoxy or (C.sub.1 -C.sub.6)halogenoalkyl, or represent a substituted phenyl, phenylacyl or benzyl group wherein the possible substituent on the phenyl, phenylacyl or benzyl group includes halogen, straight and branched (C.sub.1 -C.sub.8)alkyl, (C.sub.1 -C.sub.8)alkoxy, (C.sub.3 -C.sub.8)alkenyl, (C.sub.3 -C.Type: GrantFiled: September 27, 1993Date of Patent: January 10, 1995Assignee: Lucky, Ltd.Inventors: Bon Y. Jung, Choon S. Ra, Yo S. Rew, Young H. Rhee, Ho S. Yeo, Man Y. Yoon, Woo B. Choi
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Patent number: 5328994Abstract: New azinoneutromethines of the formula ##STR1## in which the symbols used have the meaning given in the description, a process for their preparation and their use in thermal and photochromic recording materials, as nonlinear optical materials, as photoconductors in electrophotography and for dyeing fibres and woven fabrics of polyester and plastics.Type: GrantFiled: February 19, 1993Date of Patent: July 12, 1994Assignee: Bayer AktiengesellschaftInventors: Horst Berneth, Karin Hassenruck
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Patent number: 5302718Abstract: A compound of the formula Het--NR--SO.sub.2 --Ph.sup.2 --A--Ph.sup.1 (COOH)(OH) and tautomeric form, salts, solvates, C.sub.1-6 alkyl esters and pharmaceutical compositions of the compound. Ph.sup.1 and Ph.sup.2 are benzene rings with the proviso that carboxy and hydroxy are ortho to one another. Het includes an optionally substituted heterocyclic ring which includes conjugated double bonds and binds to nitrogen in NR. The compound is characterized in that A is a bridge which is stable against reduction because it is not azo, and in that R is hydrogen or lower alkyl.The invention also includes the preparation of the compound and its use as a drug, particularly for treating autoimmune diseases.Type: GrantFiled: November 9, 1992Date of Patent: April 12, 1994Assignee: Kabi Pharmacia ABInventors: Hubert Agback, Leif Ahrgren, Thomas Berglindh, Martin Haraldsson, Goran Smedegard, Lars-Inge Olsson
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Patent number: 5292669Abstract: A method of detecting hydrolase activity using as substrates the compounds of the formula ##STR1## wherein each of R.sup.1, R.sup.2 and R.sup.3 is C.sub.1 -C.sub.4 alkyl, or phenyl optionally substituted in the meta- or para- position by C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or mono- or di-(C.sub.1 -C.sub.6)-alkylamino, or optionally substituted by an O-X group in which X is a glycosyl, phosphate or acyl moiety of a natural substrate of the corresponding glycosidase, phosphatase or esterase.Type: GrantFiled: August 10, 1992Date of Patent: March 8, 1994Assignee: Boehringer Mannheim GmbHInventors: Hans-Joachim Guder, Werner Guthlein, Wolfgang Weckerle, Johann Berger, Harvey Buck, Rupert Herrmann
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Patent number: 5278177Abstract: The invention concerns a bicyclic heterocyclic derivative of the formula I ##STR1## wherein Q is an optionally substituted 9-membered bicyclic heterocyclic moiety containing 1 or 2 N's and optionally a further N, O or S heteroatom;A.sup.1 is a direct link to X.sup.1 or 1- 3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar is optionally substituted phenylene or pyridylene;R.sup.1 is (1- 4C)alkyl, (3- 4C)alkenyl or (3- 4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1- 3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl; or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: September 24, 1992Date of Patent: January 11, 1994Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Pierre A. R. Bruneau, Graham C. Crawley, Keith Oldham
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Patent number: 5243047Abstract: A compound contains a ligand group and at least one group of the general formula --XR.sub.n where X is a linking group which contains at least one hetero-atom, R is a saturated hydrocarbyl group containing at least six carbon atoms or is an unsaturated hydrocarbyl group containing at least three carbon atoms. The ligand group can be a polyhydroxyhydrocarbyl, a triazole, an imidazole, an indazole, a thiazole, an oxazole, a carbamate, an xanthate or a phthalazine. The compounds can be used to improve bonding between a metal and a coating material in contact with the metal surface. The metal may be a tire cord and the coating material rubber or a rubber composition.Type: GrantFiled: November 16, 1990Date of Patent: September 7, 1993Assignee: Imperial Chemical Industries PLCInventor: John R. Lawson
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Patent number: 5240950Abstract: There are provided carbazate derivatives of the formula:R.sup.1 --N.dbd.CH--NHNH--R.sup.2wherein R.sup.1 is a heterocyclic group; and R.sup.2 is an esterified carboxyl group, and their salts, which are useful as AGE-formation inhibitory agents.The derivatives or the salts can be produced by reacting compounds of the formula: R.sup.1 --N.dbd.CH--OR.sup.3 wherein R.sup.1 is a heterocyclic group; and R.sup.3 is a lower alkyl group, with a carbazic acid ester or its salt.Type: GrantFiled: September 7, 1989Date of Patent: August 31, 1993Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Hitoshi Ikeda, Yu Momose
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Patent number: 5220029Abstract: A reagent for proteolytic enzyme assays has the general formula ##STR1## where RCO-- is an enzyme reactive acyl, such as an amino acid, peptide or substituted amino acid or peptide. The reagent may by hydrolyzed by proteolytic enzymes and developed to form a distinctive color. The reagent may be formed by reacting RCOOH with N-hydroxysuccinimide to form the acyl N-hydroxysuccinimide ester. The ester may then be reacted to form the reagent.Type: GrantFiled: March 13, 1990Date of Patent: June 15, 1993Assignee: Vitek Systems, Inc.Inventors: Michael S. Matta, Raymond E. O'Bear
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Patent number: 5131946Abstract: The invention relates to new anilino iminoazoles and iminoazines of general formula I ##STR1## in which A, B, D, E, W, X, Y, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Rr.sup.5 have the meanings given in the description, processes for their preparation and their use as herbicides.Type: GrantFiled: July 6, 1988Date of Patent: July 21, 1992Assignee: Schering AktiengesellschaftInventors: Wilfried Franke, Friedhelm Blume, Friedrich Arndt, Richard Rees
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Patent number: 5103007Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.Type: GrantFiled: October 27, 1989Date of Patent: April 7, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Keizo Inoue
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Patent number: 5084571Abstract: There are disclosed substituted thiazole dye compounds represented by the following Formula (I):Formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom or a group capable of substitution onto a benzene ring, n is an integer of 1 to 4, x represents a substitutent capable of forming a hydrogen bond with the hydrogen of --CONH--, R.sub.2 represents an electron-attractive substituent, R.sub.3 represents a group capable of substitution onto a thiazole ring, and R.sub.4 represents an aromatic group or an unsaturated heterocyclic group that bonds to the nitrogen atom at a carbon atom having an unsaturated linkage.The dye compounds provide a cyan color which is good in hues and possesses fastness to light and heat.Type: GrantFiled: October 18, 1989Date of Patent: January 28, 1992Assignee: Fuji Photo Film Co., Ltd.Inventor: Yasuhiro Shimada
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Patent number: 5081245Abstract: A compound represented by the formula: ##STR1## wherein R represents a hydrogen atom or a lower alkyl group;R.sup.1 represents a higher alkyl group which may be substituted;R.sup.2 represents a hydrogen atom or a lower alkyl group, a lower alkanoyl group or a nitrogen-containing 5- to 7-membered heterocyclic group each of which may be substituted; X represents a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --wherein p represents an integer of 1 to 5, a divalent group represented by the formula:--O(CH.sub.2).sub.q --wherein q represents an integer of 3 to 8, or a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --J--(CH.sub.2).sub.q --wherein J represents an oxygen atom or a group represented by the formula: --S(O).sub.Type: GrantFiled: August 18, 1989Date of Patent: January 14, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Eiko Imamiya, Keizo Inoue
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Patent number: 5077309Abstract: Novel compounds have the formula (I) ##STR1## where ##STR2## represents one of the divalent cyclic groups ##STR3## the letters a and b indicating in each case the points of attachment of the substituents R.sup.1 and CV(R.sup.2)-NV'R, respectively; R.sup.1 is a group --(CH.sub.2).sub.b --(A).sub.a --(CH.sub.2).sub.c --B--CH.sub.2 --CO.sub.2 R' in which A and B are each separately oxygen or sulphur, a is 0, b is 0 and c is an integer from 3 to 10, or a is 1, b is 0 or an integer from 1 to 7 and c is an integer from 2 to 9 with the sum of b and c being from 2 to 9, and CO.sub.2 R' is a carboxy group or an amide, ester or salt derivative thereof; V and V' either each separately is hydrogen or together are the second bond of a carbon-nitrogen double bond; R.sup.2 is hydrogen, an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by an aromatic group directly or through an oxygen or sulphur atom; and R is a group --OR.sup.3, --OR.sup.4, --D--R.sup.3, --N.dbd. R.sup.5 or --NW.G.Type: GrantFiled: March 28, 1990Date of Patent: December 31, 1991Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 5068238Abstract: Compounds of formula: ##STR1## R.sub.1 represents a polyfluoroalkoxy radical, R.sub.2 represents an alkylthioalkyl, alkylsulphinylalkyl or alkylsulphonylalkyl radical, andR.sub.3 represents an alkyl radical,as well as the salts of these compounds with an inorganic or organic acid, processes for preparing them and medicinal products containing them.Type: GrantFiled: June 29, 1990Date of Patent: November 26, 1991Assignee: Rhone-Poulenc SanteInventors: Patrick Jimonet, Conception Nemecek
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Patent number: 5064846Abstract: Insecticides of the general formula ##STR1## wherein R.sub.1 is an optionally substituted 5- to 10-member heterocyclic moiety; R.sub.2 is an optionally substituted alkyl, cycloalkyl or alkenyl moiety; X is oxygen, sulfur or --NH--; and R.sub.3 is: (a) an optionally substituted 3-phenoxyphenalkyl, 3-phenoxypyridylalkyl, 3-(pyridyloxy)phenalkyl, 3-phenylaminophenalkyl, 3-benzylphenalkyl or 3-benzyloxyphenalkyl moiety; (b) a benzylfuranylmethyl moiety; (c) a 3- or 4-substituted benzyl or tetrafluorobenzyl moiety; (d) 4-phenoxy-2-butyn-2-yl; or (e) 2-methyl-3-phenylbenzyl.Type: GrantFiled: August 24, 1990Date of Patent: November 12, 1991Assignee: ICI Americas Inc.Inventor: Michael D. Broadhurst
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Patent number: 5055582Abstract: This invention relates to a process for preparing useful thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)thioxomethyl]hydrazono]ethyl]-1.alpha. ,4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha.,7a.alpha.-4.alpha.,7.alpha.-meth ano-2H-inden-2-ones.Type: GrantFiled: December 13, 1988Date of Patent: October 8, 1991Assignee: National Research Development CorporationInventors: Robert B. Garland, Masateru Miyano
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Patent number: 5037840Abstract: Compounds having the formula: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful an anti-asthmatic, antiallergic, anti-inflammatory, and cytoprotective agents.Type: GrantFiled: March 5, 1990Date of Patent: August 6, 1991Assignee: Merck Frosst Canada, Inc.Inventors: Robert N. Young, Robert Zamboni
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Patent number: 5026720Abstract: Compounds of the general formula I ##STR1## where X is alkyl, aryl, aryloxy or alkoxy, Y is hydrogen, alkyl, alkoxy, halogen, aryl or aryloxy, n is 0 to 5, and Z is CH or N, and fungicides containing these compounds.Type: GrantFiled: March 30, 1990Date of Patent: June 25, 1991Assignee: BASF AktiengesellschaftInventors: Ulf Baus, Wolfgang Reuther, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5010198Abstract: Benzoxazol- and benzothiazolamine derivatives having anti-anoxic properties which compounds are useful in the treatment of anoxia. These compounds are produced from certain benzoxazol- and benzothizolamine intermediates.Type: GrantFiled: August 24, 1989Date of Patent: April 23, 1991Assignee: Janssen Pharmaceutica N.V.Inventors: Raymond A. Stokbroekx, Marcel G. M. Luyckx, Frans E. Janssens
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Patent number: 5008280Abstract: Compounds of the formula: ##STR1## in which - R.sub.1 denotes a polyfluoroalkoxy or polyfluoroalkyl radical, and - R.sub.2 denoteseither a chain --CH.sub.2 --(CH(R.sub.4)).sub.n --R.sub.3, in which R.sub.3 denotes a dialkylamino, piperidino, 1-pyrrolidinyl, mercapto, acylthio, alkylthio, alkylsulphinyl or alkylsulphonyl radical, R.sub.4 denotes a hydrogen atom or an alkyl radical and n is equal to 0 or 1,or a residue of formula: ##STR2## the said alkyl and alkoxy radicals and portions containing 1 to 4 carbon atoms each in a straight or branched chain and said the acyl portions containing 2 to 4 carbon atoms each, and the salts of these compounds, are useful in the treatment of diseases in which glutamate is implicated.Type: GrantFiled: December 13, 1989Date of Patent: April 16, 1991Assignee: Rhone-Poulenc SanteInventors: Claude Gueremy, Patrick Jimonet, Serge Mignani
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Patent number: 5002953Abstract: Compounds of formula (I): ##STR1## or a tautomeric form thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein:A.sup.1 represents a substituted or unsubstituted aromatic heterocyclyl group;R.sup.1 represents a hydrogen atom, an alkyl group, an acyl group, an aralkyl group, wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group;R.sup.2 and R.sup.3 each represent hydrogen, or R.sup.2 and R.sup.3 together represent a bond;A.sup.2 represents a benzene ring having in total up to five substituents; andn represents an integer in the range of from 2 to 6; pharmaceutical compositions containing such compounds and the use of such compounds and compositions in medicine.Type: GrantFiled: December 27, 1989Date of Patent: March 26, 1991Assignee: Beecham Group p.l.c.Inventor: Richard M. Hindley
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Patent number: 4996316Abstract: A process for the preparation of tertiary N,N-dimethylamines by the reaction of primary amines, formaldehyde, and hydrogen under pressure and at elevated temperature in the presence of a nickel-containing hydrogenation catalyst in the liquid phase. The hydrogenation catalyst is suspended in a solvent, the nickel concentration is 0.1 to 10% by weight, based on the primary amine. The starting materials are separate from each other, brought to 80.degree. to 150.degree. C. and 1 to 15 MPa and fed into the catalyst suspension simultaneously with stirring and reacted in one step to form the tertiary N,N-dimethylamines.Type: GrantFiled: December 24, 1988Date of Patent: February 26, 1991Assignee: Hoechst AktiengesellschaftInventors: Jurgen Weber, Detlef Kampmann, Claus Kniep
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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
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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
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Patent number: 4980356Abstract: Compounds of formula: ##STR1## and their salts, in which R.sub.1 represents polyfluoroalkoxy, and R.sub.2 represents alkyl, alkenyl (3-6 C), [cycloalkyl (3-6 C)]-alkyl, carbamoylalkyl, dialkylcarbamoylalkyl, acylaminoalkyl, phenylthioalkyl, hydroxyalkyl, cyanoalkyl, sulphamoylethyl, N-alkylsulphamoylethyl, pyridylthioalkyl, pyridiylalkylthioalkyl, pyridylsulphinylalkyl, alkynyl (3-6 C), phenylsulphinylalkyl, halophenylthioalkyl, (2,2,2-trifluoroethylthio)alkyl, 2-dialkylaminopropyl, pyrimidinylsulphinylalkyl, pyridylalkylsulphinylalkyl, halophenylsulphinylalkyl or (2,2,2-trifluoroethylsulphinyl)alkyl are useful in the treatment of medical conditions associated with the effects of glutamate.Type: GrantFiled: December 13, 1989Date of Patent: December 25, 1990Assignee: Rhone-Poulenc SanteInventors: Francois Audiau, Claude Gueremy, Patrick Jimonet, Serge Mignani
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Patent number: 4962040Abstract: 2-Hydrazono-4,6-dinitrobenzthiazolones of the formula ##STR1## in which X.sub.1 represents hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -hydroxyalkyl, C.sub.1 -C.sub.4 -sulphoalkyl or C.sub.1 -C.sub.4 -sulphatoalkyl, andX.sub.2 represents hydrogen or --SO.sub.2 X.sub.3, whereX.sub.3 may represent hydrogen, C.sub.1 -C.sub.8 -alkyl or optionally substituted aryl andX.sub.1 also represents a double bond between the cyclic nitrogen atom and the carbon atom 2 according to the formula II below: ##STR2## where X.sub.2 has the meaning specified under the above formula. These hydrazones may be employed in the preparation of azo dyestuffs and as color formers for detecting of biological substances, and in the determination of H.sub.2 O.sub.2.Type: GrantFiled: August 10, 1989Date of Patent: October 9, 1990Assignee: Bayer AktiengesellschaftInventors: Herbert Hugl, Aloysius Engel, Klaus Wehling
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Patent number: 4950593Abstract: A reagent for proteolytic enzyme assays has the general formula ##STR1## where RCO-- is an enzyme reactive acyl, such as an amino acid, peptide or substituted amino acid or peptide. The reagent may be hydrolysed by proteolytic enzymes and developed to form a distinctive color. The reagent may be formed by reacting RCOOH with N-hydroxysuccinimide to form the acyl N-hydroxysuccinimide ester. The ester may then be reacted to form the reagent.Type: GrantFiled: August 15, 1986Date of Patent: August 21, 1990Assignee: Vitek Systems, Inc.Inventors: Michael S. Matta, Raymond E. O'Bear
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Patent number: 4945106Abstract: Prostaglandin analogues exhibiting activity at thromboxane receptor sites have been prepared.Type: GrantFiled: July 6, 1989Date of Patent: July 31, 1990Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 4929623Abstract: A benzothiazol compound having the formula is disclosed and is effective to inhibit the production of leukotriene. It is useful against allergy, asthma, affections of the skin, allergic rhinitis and affection of a cardiovascular system. ##STR1## in which R20 is ester or amide and --NR5R6 is amino in variety.Type: GrantFiled: June 16, 1988Date of Patent: May 29, 1990Assignee: Eisai Co., Ltd.Inventors: Shinya Abe, Mitsuaki Miyamoto, Masayuki Tanaka, Kozo Akasaka, Kenji Hayashi, Tetsuya Kawahara, Satoshi Katayama, Yoshinori Sakuma, Takeshi Suzuki, Isao Yamatsu
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Patent number: 4886812Abstract: This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nucleic may each be substituted by 1 or 2 halogen atoms,R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by fluorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.Type: GrantFiled: October 12, 1988Date of Patent: December 12, 1989Assignee: Dr. Karl Thomae GmbHInventors: Gerhart Griss, deceased, Claus Schneider, Rudolf Hurnaus, Walter Kobinger, Ludwig Pichler, Rudolf Bauer, Joachim Mierau, Dieter Hinzen, Gunter Schingnitz
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Patent number: 4873346Abstract: The present invention provides certain novel substituted benzothiazoles, benzimidazoles and benzoxazoles which are useful as inhibitors of leukotriene biosynthesis and/or as inhibitors of the action of lipoxygenase and/or as inhibitors of mucus secretion in mammalian metabolism. They are thus employed wherever it is medically necessary or desirable to inhibit these systems.Type: GrantFiled: September 20, 1985Date of Patent: October 10, 1989Assignee: The Upjohn CompanyInventor: David J. Anderson
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Patent number: 4861785Abstract: Benzoxazol-and benzothiazolamine derivatives having anti-anoxic properties which compounds are useful in the treatment of anoxia.Type: GrantFiled: October 11, 1985Date of Patent: August 29, 1989Assignee: Janssen Pharmaceutica N.V.Inventors: Raymond A. Stokbroekx, Marcel G. M. Luyckx, Frans E. Janssens
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Patent number: 4814459Abstract: Compounds of the formula ##STR1## in which X denotes O or S; R and R.sup.1 denote H, halogen, alkyl, alkoxy, CN, NO.sub.2 or CF.sub.3 ; R.sup.2 denotes H or alkyl; Y denotes an optionally substituted alkylene or phenylene group and Z denotes a carboxyl, carboxylate, carboxylic acid ester, carboxamide, nitrile or thioamide group, are suitable for reducing the phytotoxicity of herbicides in useful plants.Type: GrantFiled: May 28, 1985Date of Patent: March 21, 1989Assignee: Hoechst AktiengesellschaftInventors: Heinz Boesenberg, Hilmar Mildenberger, Klaus Bauer, Hermann Bieringer
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Patent number: 4808605Abstract: Compounds of the formula ##STR1## wherein R is lower-alkyl, R.sup.1 is halogen, R.sup.2 is C.sub.1 -C.sub.12 -alkyl, R.sup.3 is hydroxy, lower-alkoxy, lower-alkyl-carbonyloxy, lower-alkoxy-lower-alkylcarbonoyloxy, lower-alkylaminocarbonyloxy, arylaminocarbonyloxy or aryl-lower alkylaminocarbonyloxy, X is C.sub.1 -C.sub.18 -alkylene which optionally can be interrupted by 1,4-phenylene or interrupted or lengthened by 1,4-cyclohexylene, A is di- or tri-substituted 2-imidazolyl attached via an ethylene group or a substituted or unsubstituted heterocycle selected from the group consisting of benzimidazolyl, benzimidazolonyl, imidazo[4,5-c]pyridinyl, imidazo[4,5-c]pyridinonyl, benzthiazolyl, benzodiazepine-2,5-dion-1-yl and pyrrolo[2,1-c]-[1,4]benzodiazepine-5,11-dion-10-yl and n is the number 0 or 1, in the form of racemates and optical antipodes, as well as N-oxides and pharmaceutically usable acid addition salts thereof.Type: GrantFiled: November 10, 1987Date of Patent: February 28, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Quirico Branca, Roland Jaunin, Hans P. Maki, Franzi Marti, Henri Ramuz
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Patent number: 4771061Abstract: This disclosure describes certain substituted piperazine-1,4-naphthalenediones useful as anti-asthmatic agents.Type: GrantFiled: May 6, 1987Date of Patent: September 13, 1988Assignee: American Cyanamid CompanyInventors: Jeffrey B. Medwid, Lawrence W. Torley, Andrew S. Tomcufcik
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Patent number: 4762848Abstract: Heterocyclic sulfides of the general formula heterocycle-S-R, a process for their preparation and, in particular, their use for immunostimulation, immunorestoration and cytostatic treatment, and pharmaceutical agents, which contain a sulfide of this type, for these indications.Type: GrantFiled: March 10, 1986Date of Patent: August 9, 1988Assignee: Hoechst AktiengesellschaftInventors: Karl-Heinz Scheunemann, Walter Durckheimer, Jurgen Blumbach, Michael Limbert, Hans-Ulrich Schorlemmer, Gerhard Dickneite, Hans-Harald Sedlacek
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Patent number: 4732986Abstract: Benzothiazole derivatives corresponding to the general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent, independently of one another, a hydrogen atom, a halogen atom, a linear C.sub.1 -C.sub.3 -alkyl group or a linear C.sub.1 -C.sub.3 -alkoxy group, R.sup.5 represents a hydrogen atom or a linear C.sub.1 -C.sub.3 -alkyl group, R.sup.6 represents a hydrogen atom, and R.sup.7 represents a formyl group, a carbalkoxy group of the formula ##STR2## wherein R.sup.8 denotes a linear or branch chained C.sub.1 -C.sub.4 -alkyl group, or it represents an acyl group of the formula ##STR3## wherein R.sup.9 denotes a linear C.sub.1 -C.sub.3 -alkyl group, or R.sup.6 and R.sup.7 together represent the group ##STR4## wherein R.sup.10 and R.sup.11 represent, independently of one another, a hydrogen atom or a linear C.sub.1 -C.sub.6 -alkyl group or R.sup.6 and R.sup.7 represent the group ##STR5## wherein R.sup.12 and R.sup.13 represent, independently of one another, a linear C.sub.1 -C.sub.Type: GrantFiled: May 12, 1987Date of Patent: March 22, 1988Assignee: Ludwig Heumann & Co. GmbHInventors: Kay Brune, Heidrun Engler, Istvan Szelenyi, Peter Morsdorf, Helmut Schickaneder, Kurt H. Ahrens
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Patent number: 4731374Abstract: This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynylk group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nuclei may each be substituted by 1 or 2 halogen atoms,R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by flurorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.Type: GrantFiled: December 19, 1985Date of Patent: March 15, 1988Assignee: Dr. Karl Thomae GmbHInventors: Gerhart Griss, deceased, Rudolf Hurnaus, Walter Kobinger, Ludwig Pichler, Rudolf Bauer, Joachim Mierau, Dieter Hinzen, Gunter Schingnitz
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Patent number: 4720297Abstract: A compound of the formula: ##STR1## wherein R is a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, a C.sub.3 -C.sub.4 alkenyl group, a C.sub.3 -C.sub.4 alkynyl group, a halo(C.sub.1 -C.sub.4)alkyl group, a halo(C.sub.3 -C.sub.4)alkenyl group, a halo(C.sub.3 -C.sub.4)alkynyl group, a C.sub.1 -C.sub.2 alkoxy(C.sub.1 -C.sub.2)alkyl group, a C.sub.1 -C.sub.2 alkoxy(C.sub.1 -C.sub.2)alkoxy(C.sub.1 -C.sub.2)alkyl group, a cinnamyl group, a cyano(C.sub.1 -C.sub.3)alkyl group, a carboxy(C.sub.1 -C.sub.3)alkyl group, a C.sub.1 -C.sub.5 alkoxycarbonyl(C.sub.1 -C.sub.3)alkyl group, a halo(C.sub.1 -C.sub.5)alkoxycarbonyl(C.sub.1 -C.sub.3)alkyl group, a C.sub.1 -C.sub.2 alkoxy(C.sub.1 -C.sub.2)alkoxycarbonyl(C.sub.1 -C.sub.3)alkyl group, a C.sub.1 -C.sub.5 alkoxycarbonyl(C.sub.1 -C.sub.2)alkoxycarbonyl(C.sub.1 -C.sub.3)alkyl group, a cyclo(C.sub.3 -C.sub.6)alkoxycarbonyl(C.sub.1 -C.sub.3)alkyl group, a C.sub.1 -C.sub.5 alkylaminocarbonyl(C.sub.1 -C.sub. 3)alkyl group or a di(C.sub.1 -C.sub.5)alkylaminocarbonyl(C.sub.1 -C.Type: GrantFiled: September 25, 1986Date of Patent: January 19, 1988Assignee: Sumitomo Chemical Company, LimitedInventors: Toru Haga, Eiki Nagano, Ryo Sato, Kouichi Morita
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Patent number: 4686220Abstract: This disclosure describes certain substituted piperazine-1,4-naphthalenediones useful as anti-asthmatic agents.Type: GrantFiled: December 19, 1985Date of Patent: August 11, 1987Assignee: American Cyanamid CompanyInventors: Jeffrey B. Medwid, Lawrence W. Torley, Andrew S. Tomcufcik
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Patent number: 4681883Abstract: This invention relates to aminoalkylphenoxyalkyl substituted heterocycles. These compounds antagonize the action of histamine on histamine H.sub.2 -receptors in the brain. A compound of the invention is 2-[3-[3-(piperidinomethyl)phenoxy]propylamino]benzthiazole.Type: GrantFiled: October 17, 1985Date of Patent: July 21, 1987Assignee: Smith Kline & French Laboratories LimitedInventors: Thomas H. Brown, Robert C. Mitchell, Ian R. Smith, Rodney C. Young
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Patent number: 4670448Abstract: The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in which the substituents are defined in the detailed description.The compounds show pharmaceutical activity as selective histamine H.sub.2 -antagonists.Type: GrantFiled: February 10, 1983Date of Patent: June 2, 1987Assignee: Glaxo Group LimitedInventors: John W. Clitherow, John Bradshaw, John W. M. Mackinnon, Duncan B. Judd, David E. Bays, Roger Hayes, Andrew Pearce
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Patent number: 4665206Abstract: The invention relates to compounds of the general formula I ##STR1## wherein R.sub.1 represents one up to and including four, the same or different substituents selected from alkyl(1-6 C), alkoxy(1-6 C), hydroxy, halogen, NO.sub.2 CF.sub.3 or the group --NR.sub.5 R.sub.6, whereby two substituents taken together may also represent a methylene-dioxy group,X represents nitrogen or the group ##STR2## n has the value 0, 1 or 2, R.sub.3 represents one of the moieties: ##STR3## the latter meaning of R.sub.3 (amide) only under the condition that for X is nitrogen the meaning of R.sub.1 is limited to substituents selected from hydroxy, alkoxy(1-6 C) and methylenedioxy, and R.sub.4, R.sub.5 and R.sub.6 represent hydrogen or alkyl(1-6 C), and pharmaceutically acceptable salts thereof, suitable in the treatment of heart failure.Type: GrantFiled: March 7, 1985Date of Patent: May 12, 1987Assignee: Akzo N.V.Inventors: James Redpath, Robert T. Logan, David B. McFadzen, Robert G. Roy
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Patent number: 4656180Abstract: Diamine derivatives corresponding to the general formula IR.sup.1 R.sup.2 N--(CH.sub.2).sub.m --Q--A--NH--R--NH--B--Q'--(CH.sub.2).sub.n NR.sup.3 R.sup.4 (I)which have a highly selective action on histamine-H.sub.2 receptors and are therefore suitable for use as anti-ulcerative agents are described. Processes for the preparation of these compounds and pharmaceutical preparations containing these compounds are also described.Type: GrantFiled: March 5, 1985Date of Patent: April 7, 1987Assignee: Ludwig Heumann & Co., GmbHInventors: Stefan Postius, Rolf Herter, Peter Morsdorf, Helmut Schickaneder, Istvan Szelenyi, Kurt H. Ahrens
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Patent number: 4599410Abstract: Methine dyes are disclosed which contain a 2-halo or pseudohalo substituted 1,2,5-oxatellurazole ring fused with an aromatic nucleus, the aromatic nucleus being substituted with a methine linkage terminating in an auxochrome providing a conjugated resonance chromophore. The dyes can be formed by condensing a methine linkage precursor with a compound containing an oxatellurazole ring fused with an aromatic nucleus. The dyes are useful in optical recording elements and in photographic elements.Type: GrantFiled: February 19, 1985Date of Patent: July 8, 1986Assignee: Eastman Kodak CompanyInventor: Wolfgang H. H. Gunther
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Patent number: 4596823Abstract: Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo[2,2,1]hept-2Z-ene, bicyclo[2,2,1]heptane, 7-oxabicyclo[2,2,1]hept-2Z-ene, 7-oxabicyclo[2,2,1]heptane, bicyclo[2,2,2]oct-2Z-ene or bicyclo[2,2,2]octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group C(R.sup.2).dbd.NR, a 6,6-dimethyl-bicyclo[3,1,1]heptane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group C(R.sup.2).dbd.NR or at the 5-position by the group C(R.sup.2).dbd.NR and at the 6-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group C(R.sup.2).dbd.NR, or a 1-hydroxycyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group C(R.sup.2).dbd.NR, R.sup.1 is a 6-caboxyhex-2-enyl group or a modification thereof as defined herein, R.sup.Type: GrantFiled: February 12, 1982Date of Patent: June 24, 1986Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 4594425Abstract: There are disclosed compounds of the formula ##STR1## n is 0-6; A is O or S;B is OR.sup.2, SR.sup.2 or N(R.sup.2).sub.2 ;R.sup.1 is hydrogen, loweralkyl, loweralkoxy or halo;R.sup.2 is hydrogen or loweralkyl;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.Type: GrantFiled: February 9, 1984Date of Patent: June 10, 1986Assignee: American Home Products CorporationInventors: John H. Musser, Dennis M. Kubrak
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Patent number: 4581457Abstract: There are disclosed compounds of the formula ##STR1## wherein X is ##STR2## W is ##STR3## Y is ##STR4## n is 0-8; R.sup.1 is hydrogen, loweralkyl, loweralkoxy, lower alkanoyl, halo, trifluoromethyl, cyano or nitro;R.sup.2 is hydrogen or loweralkyl;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 in antithrombotic therapy.Type: GrantFiled: September 21, 1984Date of Patent: April 8, 1986Assignee: American Home Products CorporationInventors: John H. Musser, Dennis M. Kubrak
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Patent number: RE34284Abstract: A reagent for proteolytic enzyme assays has the general formula ##STR1## where RCO-- is an enzyme reactive acyl, such as an amino acid, peptide or substituted amino acid or peptide. The reagent may be hydrolysed by proteolytic enzymes and developed to form a distinctive color. The reagent may be formed by reacting RCOOH with N-hydroxysuccinimide to form the acyl N-hydroxysuccinimide ester. The ester may then be reacted to form the reagent.Type: GrantFiled: March 9, 1992Date of Patent: June 15, 1993Assignee: bioMerieux Vitek, Inc.Inventors: Michael S. Matta, Raymond E. O'Bear