Chalcogen Bonded Directly To Ring Carbon Of The Oxadiazole Ring Patents (Class 548/144)
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Patent number: 6384215Abstract: The present invention provides new thioester derivatives of 4-halogeno-2-methoxyimino-3-oxo-butyric acid of the general formula (I), also, the invention provides a method by which the said thioester derivatives can be prepared by reacting 4-halogeno-2-methoxyimino-3-oxo-butyric acid of the general formula (II) with 2-mercapto-5-substituted-1,3,4-oxadiazoles of the general formula (III) in a solvent, in the presence of DMF/POCl3 and in presence of an organic base and if desired the so obtained thioester derivatives so obtained are reacted with 7-amino-cephem carboxylic acids of the general formula (V) to produce condensed products which are insitu reacted with thiourea to get cephalosporin antibiotic compounds having the general formula (VI).Type: GrantFiled: June 7, 2001Date of Patent: May 7, 2002Assignee: Orchid Chemicals & Pharmaceuticals Ltd.Inventors: Pandurang Balwant Deshpande, Parven Kumar Luthra
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Patent number: 6369088Abstract: Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones of the formula 1 are described, in which R1 is substituted C1-C6-alkyl and C3-C9-cycloalkyl, R2, R3, R4 and R5 are hydrogen, halogen, nitro, C1-C4-alkyl, C1-C9-alkyloxy, substituted C6-C10-aryl-C1-C4-alkyloxy, C6-C10-aryloxy, C6-C10-aryl, C3-C8-cycloalkyl or O—C3—C8-cycloalkyl, or 2-oxopyrrolidin-1-yl, 2,5-dimethylpyrrol-1-yl or NR6-A-R7, with the proviso that R2, R3, R4 and R5 are not simultaneously hydrogen, and at least one of the radicals R2, R3, R4 or R5 is the radical 2-oxopyrrolidin-1-yl, 2,5-dimethylpyrrol-1-yl or NR6-A-R7, wherein R6=hydrogen, C1-C4-alkyl or substituted C6-C10-aryl-C1-C4-alkyl, A=a single bond, COn, SOn or CONH, n=1 or 2, R7=hydrogen, substituted C1-C18-alkyl, C2-C18-alkenyl, C6-C10-aryl-C1-C4-alkyl, C5-C8-cycloalkyl-C1-C4-alkyl, C5-C8-cycloalkyl, C6-C10-aryl-C2-C6-alkenyl, C6-C10-aryl, biphenylyl, biphenylyl-C1-C4-alkyl, indanyl, or the group Het-(CH2)r—, wherein r&eqType: GrantFiled: March 6, 2001Date of Patent: April 9, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Karl Schoenafinger, Stefan Petry, Guenter Mueller, Karl-Heinz Baringhaus
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Patent number: 6342245Abstract: The present invention is concerned with novel pharmaceutical compositions of lipid lowering agents which can be administered to a mammal suffering from hyperlipidemia, obesitas or atherosclerosis, whereby a single such dosage form can be administered once daily, and in addition at any time of the day independently of the food taken in by said mammal. These novel compositions comprise particles obtainable by melt-extruding a mixture comprising a lipid lowering agent and an appropriate water-soluble polymer and subsequently milling said melt-extruded mixture.Type: GrantFiled: April 24, 2000Date of Patent: January 29, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Baert, Geert Verreck
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Patent number: 6306852Abstract: Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R1 and R2 are optional substituents and independently represent C1-6 alkyl, C2-6 alkenyl, optionally substituted by CO2H or CO2(C1-6 alkyl), C2-6 alkynyl, halogen, C1-3 perfluoroalkyl, (CH2)mAr1, (CH2)mHet1, (CH2)mCONR7R8, (CH2)mCO2R8, O(CH2)qCO2R8, (CH2)mCOR8, (CH2)mOR8, O(CH2)pOR8, (CH2)mNR7R8, CO2(CH2)qNR7R8, (CH2)mCN, S(O)nR8, SO2NR7R8, CONH(CH2)mAr1 or CONH(CH2)mHet1; R3 represents H, C1-6 alkyl, (CH2)pNR9R10, SO2R10, SO2NR9R10, (CH2)mCO2R10, C2-6 alkenyl, C2-6 alkynyl, (CH2)mCONR9R10, (CH2)mCO2R10, (CH2)pCN, (CH2)pR10 or (CH2)pOR10; R4 represents H or C1-6 alkyl; R5 represents H or OH; R6 represents phenyl optionally fused to a herterocyclic ring, the group as a whole being optionally substituted; R7-10 are fully defined herein and may independently represent Ar2 or Het2; Z represents CO2H, CONH(tetrazol-5-yl), CONHSO2O(C1-4 alkyl), CO2Ar3, CO2(C1-6 alkyl), tetrazol-5-yl, CONHSO2Ar3, CONHSO2(CH2)qAr3 oType: GrantFiled: April 24, 2000Date of Patent: October 23, 2001Assignee: Pfizer Inc.Inventors: David James Rawson, Kevin Neil Dack, Roger Peter Dickinson, Kim James
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Publication number: 20010031772Abstract: Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones of the formula 1 are described, 1Type: ApplicationFiled: March 6, 2001Publication date: October 18, 2001Inventors: Karl Schoenafinger, Stefan Petry, Guenter Mueller, Karl-Heinz Baringhaus
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Patent number: 6297261Abstract: A compound having the formula (I) or a pharmaceutically acceptable salt thereof where the variables are defined in the specification are useful in the treatment of sickle-cell anemia.Type: GrantFiled: September 30, 1999Date of Patent: October 2, 2001Assignee: Neurosearch A/SInventors: Palle Christophersen, Ove Pedersen
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Patent number: 6297241Abstract: The present invention provides novel carbamate oxadiazolone derivatives having the general formula wherein R1 and R2 are as defined herein, or a nontoxic pharmaceutically acceptable salt or solvate thereof and are useful in the treatment of disorders which are responsive to the opening of the large conductance calcium-activated potassium channels.Type: GrantFiled: November 6, 2000Date of Patent: October 2, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Piyasena Hewawasam, Xi Chen, John E. Starrett
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Patent number: 6288236Abstract: Benzimidazole compounds represented by the formula set out below and analogs thereof, wherein Y represents a single bond or sulfur atom; Z represents oxygen atom, sulfur atom, or N—R4; R1 and R2 independently represent hydrogen, a halogen atom, alkyl group or other; R3 and R4 independently represent hydrogen, alkyl group, acyl group or other; n and m independently represent an integer of 1, 2, or 3; and L represents a linking group such as C2-12 alkylene group or an alkylene group containing one or more phenylene groups or ether groups. The compounds are useful as an active ingredient of a medicament such as a preventive and therapeutic medicament for hyperlipemia or arterial sclerosis.Type: GrantFiled: October 16, 2000Date of Patent: September 11, 2001Assignee: Fuji Photo Film Co., Ltd.Inventors: Kozo Aoki, Kazuhiro Aikawa
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Patent number: 6258751Abstract: The present invention relates to novel heterocyclic compounds and their agronomically suitable salts, methods for the use of these compounds in controlling unwanted plant species, and the use of herbicidal compositions containing these compounds. In particular, the present invention pertains to substituted and unsubstituted triazoles, imidazoles and pyrazoles linked to a heterocyclic substituted benzene group. Such compounds are useful as pre-emergent and post-emergent herbicides.Type: GrantFiled: June 13, 2000Date of Patent: July 10, 2001Assignee: Rohm and Haas CompanyInventors: Richard Martin Jacobson, Mark Joseph Mulvihill, Changling Liu, Xiaonan Liu
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Patent number: 6255327Abstract: The invention relates to new diphenyl-substituted 5-ring heterocycles of general formula (I) wherein A, X and the groups R1, R2, R3, R4 and R5 are defined as in the claims, processes for preparing them and their use as pharmaceutical compositions.Type: GrantFiled: April 13, 1999Date of Patent: July 3, 2001Assignee: Boehringer Ingelheim Pharma KGInventors: Michael Brenner, Wolf-Dietrich Bechtel, Rainer Palluk, Marion Wienrich, Thomas Weiser, Enzo Cereda, Maura Bignotti, Carlo Maria Pellegrini
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Patent number: 6251829Abstract: This invention relates to herbicidal alpha-(2,4,5-trisubstituted)- and alpha-(2,5-disubstituted)-benzoyloxy-alpha-beta-, and/or beta-gamma-unsaturated-carboxylates and their derivatives, to compositions which contain these compounds, and to methods of use of these compounds.Type: GrantFiled: April 18, 2000Date of Patent: June 26, 2001Assignee: Rohm and Haas CompanyInventors: Bin Li, Ying Man, Zongjian Zhang, Longhe Xu, Adam Chi-Tung Hsu
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Patent number: 6248757Abstract: Compounds corresponding to the general formula (I) in which R1 represents hydrogen or an alkyl or cycloalkylmethyl group, X1 represents hydrogen or a halogen or an alkoxy group, or alternatively OR1 and X1 together represent a group of formula —OCH2O—, —O(CH2)2—, —O(CH2)3—, —O(CH2)2O— or —O(CH2)3O—, X2 represents hydrogen, an amino group or a group of general formula —NHCO2R in which R represents an alkyl or phenylalkyl group, X3 represents hydrogen or a halogen, and R2 represents hydrogen or an alkyl, phenylalkyl or [(4-dimethylamino)piperid-1-ylcarbonyl]alkyl group. Therapeutic application.Type: GrantFiled: November 4, 1999Date of Patent: June 19, 2001Assignee: Sanofi-SynthelaboInventors: Alistair Lochead, Samir Jegham, Jean Jeunesse
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Patent number: 6197770Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where X, W, Z, A, G, R1, R2, R3, R4, R5, R5′ and k have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof Also described are pharmaceutical compositions comprising these compounds, and methods of treating or preventing metalloprotease-related maladies using the compounds or the pharmaceutical compositions.Type: GrantFiled: March 1, 2000Date of Patent: March 6, 2001Assignee: The Procter & Gamble Co.Inventors: Michael George Natchus, Roger Gunnard Bookland, Neil Gregory Almstead, Stanislaw Pikul, Biswanath De, Menyan Cheng
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Patent number: 6184383Abstract: There is disclosed a method of producing acetals, which comprises reacting a compound of formula (I), at least one compound selected from a group consisting of a compound of formula (II), paraformaldehyde, and trioxane; and a compound of formula (III), to synthesize an acetal of formula (IV), wherein the reaction is carried out in the presence of an oxidizing agent and an acid: wherein R1 is an alkyl group etc., R2 is an alkyl or aryl group, R3 and R4 each independently are a hydrogen atom, an alkyl group or an aryl group, X1 and X2 each are a group of nonmetal atoms necessary to form a 5- or 6-membered N-containing heteroring, and M is a hydrogen atom or a cation. This method can give acetal compounds with good efficiency and a high yield.Type: GrantFiled: November 18, 1999Date of Patent: February 6, 2001Assignee: Fuji Photo Film Co., Ltd.Inventors: Atsuo Kondoh, Fumio Iwamoto
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Patent number: 6162817Abstract: The present invention provides novel carbamate oxadiazolone derivatives having the general formula ##STR1## wherein R.sup.1 and R.sup.2 are as defined herein, or a nontoxic pharmaceutically acceptable salt or solvate thereof and are useful in the treatment of disorders which are responsive to the opening of the large conductance calcium-activated potassium channels.Type: GrantFiled: January 20, 2000Date of Patent: December 19, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Piyasena Hewawasam, Xi Chen, John E. Starrett, Jr.
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Patent number: 6100252Type: GrantFiled: December 8, 1998Date of Patent: August 8, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Takehiko Naka, Yoshiyuki Inada
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Patent number: 6034113Abstract: The present invention provides novel oxadiazolone derivatives having the general formula ##STR1## wherein A, B, D and R are as defined herein, or a nontoxic pharmaceutically acceptable salt or solvate thereof and are useful in the treatment of disorders which are responsive to the opening of the large conductance calcium-activated potassium channels.Type: GrantFiled: January 15, 1999Date of Patent: March 7, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Piyasena Hewawasam, Min Ding, John E. Starrett, Jr.
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Patent number: 6022868Abstract: Disclosed are compounds of formula (I) selected from the following ##STR1## wherein Y is ##STR2## and wherein A, B, C, D, R, k, m, n, o, p, s, t and u are as defined in the specification. These compounds are useful in treating diseases in the central nervous system related to malfunctioning of the nicotinic cholinergic system.Type: GrantFiled: December 19, 1997Date of Patent: February 8, 2000Assignee: Novo Nordisk AlsInventors: Preben Houlberg Olesen, John Bondo Hansen
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Patent number: 6013804Abstract: The present invention relates to 1,3,4-oxadiazolin-2-ones of the formula (I) ##STR1## in which Ar.sup.1 represents optionally substituted phenyl andAr.sup.2 represents optionally substituted biphenyl,to processes for their preparation and to their use for controlling animal pests.Type: GrantFiled: February 20, 1998Date of Patent: January 11, 2000Assignee: Bayer AktiengesellschaftInventors: Gerd Kleefeld, Ulrike Wachendorff-Neumann
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Patent number: 5998456Abstract: Benzimidazole compounds represented by the formula set out below and analogs thereof, wherein Y represents a single bond or sulfur atom; Z represents oxygen atom, sulfur atom, or N--R.sup.4 ; R.sup.1 and R.sup.2 independently represent hydrogen, a halogen atom, alkyl group or other; R.sup.1 and R.sup.4 independently represent hydrogen, alkyl group, acyl group or other; n and m independently represent an integer of 1, 2, or 3; and L represents a linking group such as C.sub.2-12 alkylene group or an alkylene group containing one or more phenylene groups or ether groups. The compounds are useful as an active ingredient of a medicament such as a preventive and therapeutic medicament for hyperlipemia or arterial sclerosis.Type: GrantFiled: January 16, 1998Date of Patent: December 7, 1999Assignee: Fuji Photo Film Co., Ltd.Inventors: Kozo Aoki, Kazuhiro Aikawa
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Patent number: 5977149Abstract: Cyclic amides of Formula (I) which are useful as fungicides wherein: A is O; S; N; NR.sup.5 ;or CR.sup.14--, G is C or N; W is O or S; X is OR.sup.1, S(O).sub.m R.sup.1 or halogen; R.sup.1, R.sup.2, and R.sup.5 are independently, in part, C.sub.1 -C.sub.6 alkyl; Y is, in part, --O--; --S(O).sub.n --,--CHR.sup.6 O--; or --CHR.sup.6 O--N.dbd.C(R.sup.7)--; Z is, in part, optionally substituted cycloalkyl, phenyl, pyridinyl, pyrimidinyl, or naphthyl; and R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.14, m, and n are defined in the disclosure, are disclosed.Type: GrantFiled: January 14, 1998Date of Patent: November 2, 1999Assignee: E. I. du Pont de Nemours and CompanyInventors: Richard James Brown, King-Mo Sun, Deborah Ann Frasier
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Patent number: 5977150Abstract: The present invention provides novel amino acid derivatives having the general formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined herein, or a nontoxic pharmaceutically acceptable salt or solvate thereof and are useful in the treatment of disorders which are responsive to the opening of potassium channels.Type: GrantFiled: January 26, 1999Date of Patent: November 2, 1999Assignee: Bristol-Myers Squibb CompanyInventors: Piyasena Hewawasam, Xi Chen, John E. Starrett, Jr.
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Patent number: 5962656Abstract: A photographic element comprising a support having situated thereon at least one silver halide emulsion layer, the layer containing a photographic coupler represented by the formulaCOUP--T.sup.1 --T.sup.2 --(T.sup.3).sub.b --PUGwhereinCOUP is a coupler moiety having a coupling site to which T.sup.1 is attached;T.sup.1 and T3 are timing or linking groups;T.sup.2 is an indazole timing or linking group which, after release from T.sup.1, functions by electron transfer down a conjugated chain to release T.sup.3 or PUG, and which is represented by the formula: ##STR1## wherein ** denotes the point of attachment to T.sup.1 and *** denotes the point of attachment to T.sup.3 or PUG;R.sup.1 and R.sup.2 are independently selected from hydrogen, or an aliphatic, carbocyclic, or heterocyclic group, or may be bonded together to form a 5, 6, or 7 membered ring;V is independently a substituent group as further defined;q is 0, 1, 2, 3 or 4;b is 0 or 1; andPUG is a photographically useful group.Type: GrantFiled: June 10, 1997Date of Patent: October 5, 1999Assignee: Eastman Kodak CompanyInventors: William James Begley, Teh Hsuan Chen, Donald Singleton, Jr., Frank Dino Coms
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Patent number: 5958957Abstract: The present invention relates to novel organic compounds, to methods for their preparation, to compositions containing them, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings. The novel organic compounds are compounds of formula (I)(L).sub.n --Ar.sub.1 --R.sub.1 --A (I)wherein(L).sub.n, n, Ar.sub.1, R.sub.1 and A are as defined in the application.Type: GrantFiled: April 16, 1997Date of Patent: September 28, 1999Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Niels Peter Hundahl Moller, Peter Madsen
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Patent number: 5948802Abstract: The present invention provides novel benzoate derivatives having the general formula ##STR1## wherein R is as defined herein, or a nontoxic pharmaceutically acceptable salt or solvate thereof and are useful in the treatment of disorders which are responsive to the opening of potassium channels.Type: GrantFiled: January 15, 1999Date of Patent: September 7, 1999Assignee: Bristol-Myers Squibb CompanyInventors: Piyasena Hewawasam, Xi Chen, Min Ding, John E. Starrett, Jr.
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Patent number: 5929075Abstract: The present invention provides novel compounds of formula ##STR1## the N-oxides, the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts thereof, wherein A and B taken together form a bivalent radical of formula:--N.dbd.CH-- (a), --CH.dbd.N-- (b), --CH.sub.2 --CH.sub.2 -- (c), --CH.dbd.CH-- (d), --C(.dbd.O)--CH.sub.2 -- (e), --CH.sub.2 --C(.dbd.O)-- (f); R.sup.1 is hydrogen, C.sub.1-6 alkyl, or halo; R.sup.2 is hydrogen or halo; R.sup.3 is hydrogen; C.sub.1-8 alkyl; C.sub.3-6 cycloalkyl or C.sub.1-8 alkyl substituted with hydroxy, oxo, C.sub.3-6 cycloalkyl or aryl. Het is five- or six-membered optionally substituted heterocyclic ring. The use as a medicine, especially as a lipid lowering agent is disclosed as well as pharmaceutical compositions and processes for preparing compounds and compositions.Type: GrantFiled: April 9, 1997Date of Patent: July 27, 1999Assignee: Janssen Pharmaceutica, N.V.Inventors: Jan Heeres, Leo Jacobus Jozef Backx, Robert Jozef Maria Hendrickx, Luc Alfons Leo Van der Eycken, Didier Robert Guy Gabriel de Chaffoy de Courcelles
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Patent number: 5889032Abstract: The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel azolidinedione derivatives of the general formula (I), and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them.Type: GrantFiled: May 5, 1997Date of Patent: March 30, 1999Assignees: Dr. Reddy's Research Foundation, Reddy-Cheminor, Inc.Inventors: Vidya Bhushan Lohray, Braj Bhushan Lohray, Ashok Channaveerappa Bajji, Sekar Reddy Alla, Rajagopalan Ramanujam, Ranjan Chakrabarti
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Patent number: 5889025Abstract: Novel antidiabetic compounds, their tautomeric forms, their derivatives, their steroisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical acceptable compositions containing them: Methods for preparing the antidiabetic compounds and their uses.Type: GrantFiled: May 5, 1997Date of Patent: March 30, 1999Assignees: Reddy's Research Foundation, Reddy-Cheminor, Inc.Inventors: Vidya Bhushan Lohray, Braj Bhushan Lohray, Sekar Reddy Alla, Rajagopalan Ramanujam, Ranjan Chakrabarti
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Patent number: 5874382Abstract: Compounds of Formula I and II, and their agriculturally-suitable salts, are disclosed which are useful for controlling undesired vegetation ##STR1## wherein X is a direct bond; O; S; NH; N(C.sub.1 -C.sub.3 alkyl); N(C.sub.1 -C.sub.3 haloalkyl); or N(allyl);R.sup.1 is H; F; Cl; or Br;R.sup.2 is H; F; Cl; Br; CF.sub.3 ; nitro; or cyano;R.sup.4 is H; C.sub.1 -C.sub.3 alkyl; or halogen;R.sup.5 is H; C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 haloalkyl; halogen; S(O).sub.2 (C.sub.1 -C.sub.6 alkyl); or C(.dbd.O)R.sup.8 ; orR.sup.4 and R.sup.5 are taken together along with the carbon to which they are attached to form a spiro-cyclopropane ring;and R.sup.3, R.sup.8, and J are as defined in the disclosure.Also disclosed are compositions containing the compounds of Formulae I and II and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula I or II.Type: GrantFiled: January 23, 1998Date of Patent: February 23, 1999Assignee: E. I. du Pont de Nemours and CompanyInventors: Balreddy Kamireddy, William Mark Murray
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Patent number: 5834604Abstract: A photographic element comprising a support having situated thereon at least one silver halide emulsion layer, the element further comprising a photographic coupler represented by the formulaCOUP--(T.sup.1).sub.b --T.sup.2 --(T.sup.3).sub.c --PUGwherein the substituents are as defined in the specification.Type: GrantFiled: September 4, 1997Date of Patent: November 10, 1998Assignee: Eastman Kodak CompanyInventors: William James Begley, Frank Dino Coms, Teh-Hsuan Chen, Donald Singleton, Jr.
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Patent number: 5817809Abstract: A photographic element comprising a support having situated thereon at least one silver halide emulsion layer, the element further comprising a photographic coupler represented by the formulaCOUP--(T.sup.1).sub.b --T.sup.2 --(T.sup.3).sub.c --PUGwhereinCOUP is a coupler moiety having a coupling site to which T.sup.1 is attached;T.sup.1 is a timing or linking group which releases from COUP during processing and which functions by electron transfer down a conjugated or unconjugated chain, or by a nucleophilic displacement reaction, to release T.sup.2 ;T.sup.2 is a triazole timing or linking group which, after release from T.sup.1, functions by a nucleophilic displacement reaction to release T.sup.3 or PUG and is represented by the formula: ##STR1## wherein ** denotes the point of attachment to T.sup.1 and *** denotes the point of attachment to T.sup.3 or PUG;R.sup.Type: GrantFiled: September 4, 1997Date of Patent: October 6, 1998Assignee: Eastman Kodak CompanyInventors: William James Begley, Frank D. Coms, Teh-Hsuan Chen
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Patent number: 5801170Abstract: A compound of formula (I) or a salt thereof: ##STR1## wherein P is a 5 to 7 membered heterocyclic ring selected from the group consisting of thienyl, furyl, pyrrolyl, triazolyl, diazolyl, tetrazolyl, imidazolyl, oxadiazolyl, isothiazolyl, isoxazolyl, thiadiazolyl, pyridyl, pyrimdyl and pyrazinyl;R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen, halogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkenyl, C.sub.1-6 alkoxy, hydroxyC.sub.1-6 alkyl, C.sub.1-6 alkylOC.sub.1-6 alkyl, alkanoyl, optionally substituted phenyl, alkanoyloxy, hydroxy, nitro, trifluoromethyl, cyano, CO.sub.2 R.sup.9,CONR.sup.10 R.sup.11 where R.sup.9, R.sup.10 and R.sup.11 are independently hydrogen or C.sub.1-6 alkyl;R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1-6 alkyl;R.sup.6 is hydrogen, halogen, hydroxy, C.sub.1-6 alkyl or C.sub.1-6 alkoxyR.sup.7 and R.sup.8 are independently hydrogen, C.sub.Type: GrantFiled: June 7, 1996Date of Patent: September 1, 1998Assignee: SmithKline Beecham plcInventors: Laramie Mary Gaster, Francis David King, Paul Adrian Wyman
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Patent number: 5780490Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen or alkyl; R.sup.2 is alkylene; R.sup.3 is hydrogen, alkyl, alkoxy, alkylthio, halogen, nitro group, amino group, monoalkylamino, dialkylamino, aryl, or aralkyl; X is aryl, or aromatic heterocyclic; Y is oxygen, sulfur or a group of formula >N--R.sup.4, in which R.sup.4 is hydrogen, alkyl or acyl; and Z is a group of formula (Za), (Zb), (Zc) or (Zd): ##STR2## and salts thereof can be used to treat or prevent are included those arising from hyperlipidemia, hyperglycemia, obesity, impaired glucose tolerance (IGT), insulin resistant non-IGT (NGT), non-diagnostic glucose tolerance, insulin resistance, diabetic complications, fatty liver, polycystic ovary syndrome (PCOS) and gestational diabetes mellitus (GDM); in addition the compounds of the present invention have aldose reductase inhibitory activity.Type: GrantFiled: June 18, 1997Date of Patent: July 14, 1998Assignee: Sankyo Company, LimitedInventors: Hiroaki Yanagisawa, Takashi Fujita, Koichi Fujimoto, Takao Yoshioka, Kunio Wada, Minoru Oguchi, Toshihiko Fujiwara, Hiroyoshi Horikoshi
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Patent number: 5767041Abstract: The invention relates to new substituted aryliminoheterocycles of the general formula (I) ##STR1## in which A represents oxygen, sulphur or the group N--R.sup.1 whereR.sup.1 represents hydrogen or in each case optionally substituted alkyl, alkenyl or akinyl,E represents one of the following groups ##STR2## where Q represents oxygen, sulphur or the group N--R.sup.1 (where R.sup.1 has the abovementioned meaning) andR.sup.2 represents hydrogen, cyano or in each case optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl or cycloalkenyl,R represents hydrogen or in each case optionally substituted alkyl, alkenyl or alkinyl, andAr represents in each case optionally substituted monocyclic or bicyclic aryl or heteroaryl,to processes for their preparation and to their use as herbicides.Type: GrantFiled: January 7, 1997Date of Patent: June 16, 1998Assignee: Bayer AktiengesellschaftInventors: Otto Schallner, Andreas Lender, Hans-Joachim Santel, Markus Dollinger
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Patent number: 5763618Abstract: A method of manufacturing a sulfide comprises the steps of (a) dissolving a thiol in a solvent to form a solution; (b) oxidizing the thiol to a disulfide in the presence of a first oxidizing agent in the solution; (c) reacting the disulfide with a coupler in the presence of a base and a second oxidizing agent, without isolation of said disulfide from the solution, to form a reaction mixture in which the sulfide is produced; and (d) obtaining said sulfide.Type: GrantFiled: April 29, 1996Date of Patent: June 9, 1998Assignee: Konica CorporationInventors: Ryuzou Watanabe, Shinri Tanaka, Katsuji Ota, Michiko Nagato, Tomio Horiuchi
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Patent number: 5760246Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure ##STR1## including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2;R.sup.x is H, alkyl, aryl or halogen;A is(1) a bond;(2) --O--; or(3) ##STR2## B is: ##STR3## and wherein L.sup.2, L.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.3', R.sup.3a, R.sup.3b, R.sup.4, R.sup.4', R.sup.5, X, ##STR4## are as defined herein.Type: GrantFiled: December 17, 1996Date of Patent: June 2, 1998Inventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, William A. Slusarchyk, Richard B. Sulsky, Joseph A. Tino
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Patent number: 5731441Abstract: The invention provides hydroxamic acid derivatives of the general formula ##STR1## wherein R.sup.1 represents cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; R.sup.2 represents a saturated 5- to 8-membered monocyclic or bridged N-heterocyclic ring, which N-heterocyclic ring is attached via the N atom and when it is monocyclic, optionally contains NR.sup.4, O, S, SO or SO.sub.2 as a ring member and/or is optionally substituted on one or more C atoms by hydroxy, lower alkyl, lower alkoxy, oxo, ketalized oxo, amino, mono(lower alkyl)amino, di(lower alkyl)amino,carboxy, lower alkoxycarbonyl, hydroxy-methyl, lower alkoxymethyl, carbamoyl, mono(lower alkyl)-carbamoyl, di(lower alkyl)carbamoyl or hydroxyimino; R.sup.3 represents a 5- or 6-membered N-heterocyclic ring which (a) is attached via the N atom, (b) optionally contains N, O and/or S, SO or SO.sub.Type: GrantFiled: October 29, 1996Date of Patent: March 24, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Michael John Broadhurst, Paul Anthony Brown, William Henry Johnson
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Patent number: 5714437Abstract: Novel compounds of the formula ?1! are disclosed, wherein X is hydrogen, fluorine or chlorine; Y is fluorine, chlorine or bromine; R.sup.1 is hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sup.2 and Q are various groups. Also disclosed are herbicidal compositions containing these compounds as active ingredients and methods for controlling unfavorable weeds by application of these compounds.Type: GrantFiled: August 30, 1995Date of Patent: February 3, 1998Assignee: Sumitomo Chemical Company, LimitedInventors: Minoru Takano, Masayuki Enomoto, Kazuo Saito, Satoru Kizawa
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Patent number: 5703065Abstract: The invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof, wherein A, W, P, R.sup.3, Q and R.sup.1 are as defined herein. The compounds of formula I, and pharmaceutically acceptable salts thereof, are substance P antagonists and as such are useful in the treament of various inflammatory and central nervous system disorders.Type: GrantFiled: May 7, 1996Date of Patent: December 30, 1997Assignee: Pfizer Inc.Inventor: Harry R. Howard, Jr.
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Patent number: 5677282Abstract: Amino acid amides of 5-amino-1,3,4-thiadiazole-2-thione are disclosed. These compounds inhibit matrix metalloproteinase enzymes and cartilage degradation. Methods of treating diseases caused by over-activity of matrix metalloproteinases, such as osteoarthritis and rheumatoid arthritis, are also disclosed.Type: GrantFiled: June 7, 1995Date of Patent: October 14, 1997Assignee: Proscript, Inc.Inventors: Jozef Oleksyszyn, Alan R. Jacobson
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Patent number: 5670526Abstract: 1,3,4-oxadiazole compounds are disclosed. The subject compounds suppress immune function and have hepatoprotection activity.Type: GrantFiled: December 21, 1995Date of Patent: September 23, 1997Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Dharmpal S. Dodd, Takao Nishi
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Patent number: 5668159Type: GrantFiled: May 8, 1996Date of Patent: September 16, 1997Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Fuqiang Jin, Pasquale Nicholas Confalone
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Patent number: 5639770Abstract: A thiazole derivative of the general formula: ##STR1## The thiazole derivatives have an excellent inhibitory activity for superoxide radical.Type: GrantFiled: December 11, 1995Date of Patent: June 17, 1997Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Masatoshi Chihiro, Hajime Komatsu, Michiaki Tominaga, Yoichi Yabuuchi
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Patent number: 5602181Abstract: Naphthyl ethers of the general formula I ##STR1## where the index and the substituents have the meanings defined in the specification.Type: GrantFiled: October 12, 1994Date of Patent: February 11, 1997Assignee: BASF AktiengesellschaftInventors: Wassilios Grammenos, Reinhard Kirstgen, Hartmann K onig, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5573999Abstract: .beta.-Substituted cinnamic acid derivatives of the formula 1, ##STR1## where R.sup.1 is alkyl, chlorine or bromine, --X-- is --O--, --S--, ##STR2## m is 0 or 1, --Y is --OR.sup.4, --O--N.dbd.CR.sup.5 R.sup.6, --NR.sup.7 R.sup.8, --N(OR.sup.9)R.sup.10 or --SR.sup.11, where the above-mentioned substituents R.sup.2 to R.sup.11 are alkyl, and R.sup.2, and R.sup.3 and R.sup.5 to R.sup.11 can also be hydrogen,Z is halogen, nitro, cyano, alkyl, cycloalkyl, aralkyl, aryloxyalkyl, arylthioalkyl, hetarylalkyl, hetaryloxyalkyl, hetarylthioalkyl, alkenyl, aralkenyl, aryloxyalkenyl, arylthioalkenyl, hetarylalkenyl, hetaryloxyalkenyl, hetarylthioalkenyl, alkynyl, arylalkynyl, hetarylalkynyl, aryl, hetaryl, arylazo, acylamino, --OR.sup.12, --SR.sup.13, --SOR.sup.14, --SO.sub.2 R.sup.15, --COOR.sup.16, --CONR.sup.17 R.sup.18, --COR.sup.19, --CR.sup.20 .dbd.NR.sup.21, --N.dbd.CR.sup.22, R.sup.23, --CR.sup.24 .dbd.N--OR.sup.25, --CR.sup.25 R.sup.26 --O--, N.dbd.CR.sup.27 R.sup.28, --CH.sub.2 --OCOR.sup.39 or --NR.sup.37 R.Type: GrantFiled: May 15, 1995Date of Patent: November 12, 1996Assignee: BASF AktiengesellschaftInventors: Hubert Sauter, Herbert Bayer, Klaus Oberdorf, Horst Wingert, Wolfgang von Deyn, Wassilios Grammenos, Hartmann Koenig, Harald Rang, Franz Roehl, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5552409Abstract: This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula ##STR1## wherein A, Q, D and R.sup.1 are as defined within, compositions containing these compounds and methods of controlling agricultural and mammalian fungal diseases.Type: GrantFiled: March 31, 1994Date of Patent: September 3, 1996Assignee: Rohm and Haas CompanyInventors: Enrique L. Michelotti, Anne R. Egan, Ronald Ross, Jr., Willie J. Wilson
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Patent number: 5525619Abstract: 1,3,4-Oxadiazol-2(3H)-one derivatives, of formula ##STR1## in which R.sub.1 represents either a hydrogen atom or a linear or branched (C.sub.1-4)alkyl group which is substituted with a hydroxyl group, a phenoxy group, a (C.sub.1-4)alkoxy group, a (C.sub.1-4)alkylthio group, a mercapto group, a (C.sub.1-4)alkoxy-(C.sub.1-4)alkoxy group, a di(C.sub.1-4)alkylamino group or an N-(C.sub.1-4)alkyl-N-propynylamino group, or represents a (C.sub.3-4)alkynyl group, andR.sub.2 either represents a linear or branched (C.sub.1-8)alkyl group which is substituted with one or more halogen atoms and/or a hydroxyl group, a 1-imidazolyl group or a 3-tetrahydropyranyl group, or represents a trifluoro(C.sub.3-5)alkenyl group,in the form of pure enantiomers or mixtures of enantiomers, including racemic mixtures, as well as the addition salts thereof with pharmaceutically acceptable acids, are useful as inhibitors of monoamine oxidase B.Type: GrantFiled: November 23, 1994Date of Patent: June 11, 1996Assignee: SynthelaboInventors: Jean-Jacques Koenig, Samir Jegham, Frederic Puech, Philippe Burnier
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Patent number: 5523278Abstract: There are provided substituted benzisoxazole and benzisothiazole compounds having the structural formula I ##STR1## Further provided are compositions and methods comprising those compounds for the control of undesirable plant species.Type: GrantFiled: September 12, 1995Date of Patent: June 4, 1996Assignee: American Cyanamid CompanyInventor: Peter J. Wepplo
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Patent number: 5523312Abstract: Disclosed herein are compounds and pharmaceutical compositions useful for combating picornaviruses and preventing or treating picornaviral infections. The compounds have the formula: ##STR1## wherein Het.sub.1 is chosen from the group consisting of oxazolyl, isoxazolyl, oxadiazolyl;Y is an alkylene bridge of 3 to 9 carbon atoms;Het.sub.2 is benzofuranyl or indolyl;R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, acetyl, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluromethyl, or cyano; andR.sub.3 is oxazolyl, oxadiazolyl, isoxazolyl or any of these substituted with alkyl, halo, alkoxyalkyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, thienyl, or fluoroalkyl;the N-oxide thereof or a pharmaceutically acceptable acid addition salt thereof.Type: GrantFiled: September 27, 1994Date of Patent: June 4, 1996Assignee: Sterling Winthrop Inc.Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Gee-Hong Kuo, Theodore J. Nitz, Michael Reuman
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Patent number: 5514679Abstract: Compounds of the formula ##STR1## wherein: R.sub.1 and R.sub.2 are independently hydrogen, halo, alkyl, alkenyl, alkoxy, hydroxy, hydroxyalkyl, hydroxyhaloalkyl, alkoxyalkyl, alkylthioalkynyl, hydroxyalkoxy, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonyl, carboxy or cyanomethyl, nitro, difluoromethyl, trifluoromethyl or cyano;Y is alkylene of 3 to 9 carbon atoms;R.sub.3 and R.sub.4 are independently hydrogen, alkyl, alkoxy, hydroxy, cycloalkyl, hydroxyalkyl, hydroxyhaloalkyl, alkoxyalkyl, hydroxyalkoxy, alkylthioalkyl, alkanoyl, alkanoyloxy, alkylsulfinylalkyl, alkylsulfonylalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonyl, carboxy, cyanomethyl, fluoroalkyl, cyano, phenyl, alkynyl, alkene, or halo;R.sub.5 is alkoxycarbonyl, alkyltetrazolyl, phenyl or a heterocycle;or a pharmaceutically acceptable acid addition salts thereof; N-oxides thereof, are useful as antipirconaviral agents.Type: GrantFiled: May 13, 1994Date of Patent: May 7, 1996Assignee: Sterling Winthrop Inc.Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Theodore J. Nitz