Nitrogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 548/245)
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Patent number: 5962490Abstract: Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)-furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.Type: GrantFiled: September 27, 1996Date of Patent: October 5, 1999Assignee: Texas Biotechnology CorporationInventors: Ming Fai Chan, Chengde Wu, Bore Gowda Raju, Timothy Kogan, Adam Kois, Erik Joel Verner, Rosario Silvestre Castillo, Venkatachalapathi Yalamorri, Vitukudi Narayanaiyengar Balaji
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Patent number: 5955607Abstract: Compounds of the formula I ##STR1## having the meanings of the substituents indicated in the claims are outstandingly efficacious substances for producing medicaments for the prophylaxis and for the therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal disorders.Type: GrantFiled: September 25, 1998Date of Patent: September 21, 1999Assignee: Hoechst Marion Roussel DeutschlandInventors: Joachim Brendel, Uwe Gerlach, Hans Jochen Lang, Klaus Weidmann
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Patent number: 5945408Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: August 8, 1996Date of Patent: August 31, 1999Assignee: G.D. Searle & Co.Inventors: R. Keith Webber, Foe S. Tjoeng, Robert E. Manning
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Patent number: 5939418Abstract: Isoxazolines, isothiazolines and pyrazolines which are inhibitors of Factor Xa, pharmaceutical compositions containing these compounds, and methods of using these compounds as anticoagulant agents for treatment and prevention of thromboembolic disorders. The compounds can be represented by the formula: ##STR1## where X is O, S or NR.sup.15.Type: GrantFiled: December 17, 1996Date of Patent: August 17, 1999Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Mimi Lifen Quan, John Wityak, Robert Anthony Galemmo, Jr., Petrus F. W. Stouten, James Russell Pruitt, Donald J. P. Pinto
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Patent number: 5935973Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R.sub.1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO.HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.Type: GrantFiled: January 5, 1998Date of Patent: August 10, 1999Assignee: Knoll AktiengesellschaftInventors: Alan Martin Birch, David John Heal, Frank Kerrigan, Keith Frank Martin, Patricia Lesley Needham, Bruce Jeremy Sargent
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Patent number: 5908931Abstract: The present invention relates particularly to novel preorganized hexadentate ligands that are suitable for completing with a radionuclide, and are useful as general imaging agents for diagnostic purposes.Type: GrantFiled: December 14, 1990Date of Patent: June 1, 1999Assignee: Mallinckrodt Inc.Inventors: Raghavan Rajagopalan, William L. Neumann, Dennis L. Nosco
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Patent number: 5859257Abstract: A class of substituted isoxazolyl compounds is described for use in treating cyclooxygenase-2 related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3, are described in the specification.Type: GrantFiled: August 14, 1996Date of Patent: January 12, 1999Assignee: G. D. Searle & Co.Inventor: John J Talley
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Patent number: 5856507Abstract: Methods for the preparation of biphenyl isoxazole sulfonamides and intermediates thereof. The present invention also relates to the novel intermediates prepared by these methods. The biphenyl isoxazole sulfonamides prepared by the present methods are endothelin antagonists useful, inter alia, for the treatment of hypertension.Type: GrantFiled: January 21, 1997Date of Patent: January 5, 1999Assignee: Bristol-Myers Squibb Co.Inventors: Richard P. Polniaszek, Xuebao Wang, Jeffrey S. DePue, Chennagiri R. Pandit, Kumar G. Gadamasetti, Yadagiri Pendri, Eduardo J. Martinez
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Patent number: 5849736Abstract: This invention relates to novel isoxazolines and isoxazoles which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex or the vitronectin receptor, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.Type: GrantFiled: May 31, 1995Date of Patent: December 15, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: John Wityak, Chu-Biao Xue, Thais Motria Sielecki-Dzurdz, Richard Eric Olson, William Frank Degrado, Gary Avonn Cain, Douglas Guy Batt, Donald Pinto, Munir Alwan Hussain, Shaker Ahmed Mousa
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Patent number: 5846985Abstract: Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols R.sup.1, R.sup.2, Q, K, J, .alpha., .beta., p, R.sup.11, R.sup.12, R.sup.13 R.sup.14, X, Y, R.sup.3 and R.sup.4 are defined herein.Type: GrantFiled: March 5, 1997Date of Patent: December 8, 1998Assignee: Bristol-Myers Squibb Co.Inventor: Natesan Murugesan
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Patent number: 5846990Abstract: Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each directly bonded to a ring carbon and are each independently(a) hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z.sup.1, Z.sup.2 and Z.sup.3 ;(c) halo;(d) hydroxyl;(e) cyano;(f) nitro;(g) --C(O)H or --C(O)R.sup.5 ;(h) --CO.sub.2 H or --CO.sub.2 R.sup.5 ;(i) --Z.sup.4 --NR.sup.6 R.sup.7 ;(j) --Z.sup.4 --N(R.sup.10)--Z.sup.5 --NR.sup.8 R.sup.9 ; or(k) R.sup.3 and R.sup.4 together may also be alkylene or alkenylene, either of which may be substituted with Z.sup.1, Z.sup.2 and Z.sup.3, completing a 4- to 8-membered saturated, unsaturated or aromatic ring together with the carbon atoms to which they are attached;and the remaining symbols are as defined in the specification.Type: GrantFiled: February 13, 1997Date of Patent: December 8, 1998Assignee: Bristol-Myers Squibb Co.Inventors: Natesan Murugesan, Joel C. Barrish, Steven H. Spergel
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Patent number: 5843937Abstract: The present invention relates to novel DNA alkylating agents and the prodrugs of these agents which are useful as antitumor agents and DNA labelling agents. The compounds are hydroxy dihydrobenzindole oligopeptides and prodrugs thereof wherein the monomeric constituents are derived from monocyclic or bicyclic heterocyclic aromatic residues.Type: GrantFiled: May 23, 1996Date of Patent: December 1, 1998Assignee: Panorama Research, Inc.Inventors: Yuqiang Wang, Susan C. Wright, James W. Larrick
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Patent number: 5834468Abstract: This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.Type: GrantFiled: July 2, 1996Date of Patent: November 10, 1998Assignee: Zeneca LimitedInventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
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Patent number: 5834494Abstract: Compounds of formula (I), processes for their preparation and their use in medicine are disclosed: ##STR1## wherein: P represents phenyl, a quinoline or isoquinoline residue, or a 5-membered or 6-membered aromatic heterocyclic ring containing up to three heteroatoms selected from nitrogen, oxygen or sulphur;R.sup.1 is hydrogen, C.sub.1-6 alkyl, halogen, CF.sub.3, NR.sup.7 R.sup.8 or OR.sup.9 where R.sup.7, R.sup.8 and R.sup.9 are independently hydrogen, C.sub.1-6 alkyl or arylC.sub.1-6 alkyl;R.sup.2 is hydrogen or C.sub.1-6 alkyl;R.sup.3 is C.sub.1-6 alkyl;n is 0 to 3;m is 0 to 4; andR.sup.4 groups are independently C.sub.1-6 alkyl optionally substituted by one or more halogen atoms, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl-C.sub.1-6 alkyl, C.sub.1-6 alkylthio, C.sub.3-6 cycloalkylthio, C.sub.3-6 cycloalkylC.sub.1 C.sub.6 alkylthio, halogen, nitro, CF.sub.3, OCF.sub.3, SCF.sub.3, SO.sub.2 CF.sub.3, SO.sub.2 F, formyl, C.sub.Type: GrantFiled: September 23, 1996Date of Patent: November 10, 1998Assignee: SmithKline Beecham p.l.c.Inventors: Peter Ham, Graham Elgin Jones, Ian Thomson Forbes
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Patent number: 5804585Abstract: Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds that include those of the formula: ##STR1## where X is selected from groups that include O, S, and NH; Y is selected from O.sup.+ and N, and R.sup.1 and R.sup.2 are each selected independently from among alkyl, lower alkenyl, lower alkynyl, lower haloalkyl, halide, pseudohalide or H, except that R.sup.2 is not halide. R.sup.3, R.sup.4 and R.sup.5 are selected from among groups that include hydrogen, halide, alkoxy, alkyl, haloalkyl; and R.sup.7 is selected from groups that include (CH.sub.2).sub.r R.sup.18, in which r is 0 to 6 and R.sup.18 is selected from groups that include aryl, particularly pyrmidinyl and phenyl.Type: GrantFiled: April 15, 1996Date of Patent: September 8, 1998Assignee: Texas Biotechnology CorporationInventor: Erik Joel Verner
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Patent number: 5783705Abstract: A process of preparing an alkali metal salt of a hydrophobic sulfonamide is provided. The process includes the step of dissolving a free sulfonamide in an organic solvent in the presence of a saturated alkali metal salt solution and recovering the formed sulfonamide salt from the organic phase.Type: GrantFiled: April 28, 1997Date of Patent: July 21, 1998Assignee: Texas Biotechnology CorporationInventors: Natalie Blok, Chengde Wu, Karin Keller, Timothy P. Kogan
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Patent number: 5747424Abstract: The invention relates to 4-substituted isoxazole derivatives of formula I: ##STR1## wherein R, R.sup.1, R.sup.2, Q and n have the meanings defined in the description, which possess valuable herbicidal properties.Type: GrantFiled: May 1, 1997Date of Patent: May 5, 1998Assignee: Rhone-Poulenc Agriculture Ltd.Inventors: David Alan Roberts, Susan Mary Cramp, Derek Ian Wallis, Jean-Paul Bulot
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Patent number: 5716967Abstract: This invention relates to isoxazoline compounds which are selective inhibitors of phosphodiesterase type IV (PDE.sub.IV). The isoxazoline compounds are useful in inhibiting PDE.sub.IV and in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease, psoriasis, allergic rhinitis, dermatitis, shock, atopic dermatitis, rheumatoid arthritis and osteoarthritis. This invention also relates to pharmaceutical compositions useful therefor.Type: GrantFiled: May 15, 1996Date of Patent: February 10, 1998Assignee: Pfizer Inc.Inventor: Edward Fox Kleinman
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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: 5686434Abstract: This invention relates to 3-aryl-2-isoxazoline compounds which are selective inhibitors of phosphodiesterase type IV (PDE.sub.IV). The 3-aryl-2-isoxazolines are useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease, psoriasis, allergic rhinitis, dermatitis, shock, atopic dermatitis, rheumatoid arthritis and osteoarthritis. This invention also relates to pharmaceutical compositions useful therefor.Type: GrantFiled: May 15, 1996Date of Patent: November 11, 1997Assignee: Pfizer Inc.Inventor: Edward Fox Kleinman
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Patent number: 5674894Abstract: The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound.Type: GrantFiled: May 15, 1995Date of Patent: October 7, 1997Assignee: G.D. Searle & Co.Inventors: Mark G. Currie, Foe S. Tjoeng, Mark E. Zupec
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Patent number: 5656573Abstract: The invention relates to 4-substituted isoxazole derivatives of formula I: ##STR1## wherein R, R.sup.1, R.sup.2, Q and n have the meanings defined in the description, which possess valuable herbicidal properties.Type: GrantFiled: June 2, 1995Date of Patent: August 12, 1997Assignee: Rhone-Poulenc Agriculture Ltd.Inventors: David Alan Roberts, Susan Mary Cramp, Paul Alfred Cain, Derek Ian Wallis, Jean-Paul Bulot, Gillian Mary Little, Brian Malcolm Luscombe
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Patent number: 5654301Abstract: The present invention relates to compounds of the formula ##STR1##Type: GrantFiled: January 12, 1993Date of Patent: August 5, 1997Assignee: Research Corporation Technologies, Inc.Inventors: Harold L. Kohn, Darrell Watson
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Patent number: 5643933Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: GrantFiled: June 2, 1995Date of Patent: July 1, 1997Assignee: G. D. Searle & Co.Inventors: John J. Talley, James A. Sikorski, Bryan H. Norman, Roland S. Rogers, deceased, Balekudru Devadas, Matthew J. Graneto, Jeffery S. Carter
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Patent number: 5633272Abstract: A class of substituted isoxazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II ##STR1## wherein R.sup.1 is selected from hydroxyl, lower alkyl, carboxyl, lower carboxyalkyl, lower aminocarbonylalkyl, lower alkoxycarbonylalkyl, lower aralkyl, lower alkoxyalkyl, lower aralkoxyalkyl, lower alkylthioalkyl, lower aralkylthioalkyl, lower alkylaminoalkyl, lower aryloxyalkyl, lower arylthioalkyl, lower haloalkyl, lower hydroxylalkyl, cycloalkyl, cycloalkylalkyl, and aralkyl; wherein R.sup.3 is selected from cycloalkyl, cycloalkenyl, aryl, and heteroaryl; wherein R.sup.Type: GrantFiled: June 7, 1995Date of Patent: May 27, 1997Inventors: John J. Talley, David L. Brown, Srinivasan Nagarajan, Jeffery S. Carter, Richard M. Weier, Michael A. Stealey, Paul W. Collins, Roland S. Rogers, deceased, Karen Seibert
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Patent number: 5621109Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed wherein the terms R.sub.1, R.sub.2, R.sub.5, R.sub.6, Y, Y', m and n are herein defined.Type: GrantFiled: May 31, 1995Date of Patent: April 15, 1997Assignee: Abbott LaboratoriesInventors: Daniel W. Norbeck, Hing L. Sham, Dale J. Kempf, Chen Zhao
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Patent number: 5612359Abstract: Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each directly bonded to a ring carbon and are each independently(a) hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z.sup.1, Z.sup.2 and Z.sup.3 ;(c) halo;(d) hydroxyl;(e) cyano;(f) nitro;(g) --C(O)H or --C(O)R.sup.5 ;(h) --CO.sub.2 H or --CO.sub.2 R.sup.5 ;(i) --Z.sup.4 --NR.sup.6 R.sup.7 ;--Z.sup.4 --N(R.sup.10)--Z.sup.5 --NR.sup.8 R.sup.9 ; or(k) R.sup.3 and R.sup.4 together may also be alkylene or alkenylene, either of which may be substituted with Z.sup.1, Z.sup.2 and z.sup.3, completing a 4- to 8-membered saturated, unsaturated or aromatic ring together with the carbon atoms to which they are attached; and the remaining symbols are as defined in the specification.Type: GrantFiled: June 7, 1995Date of Patent: March 18, 1997Assignee: Bristol-Myers Squibb CompanyInventor: Natesan Murugesan
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Patent number: 5594021Abstract: Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.Type: GrantFiled: June 6, 1995Date of Patent: January 14, 1997Assignee: Texas Biotechnology CorporationInventors: Ming F. Chan, Bore G. Raju, Adam Kois, Erik J. Verner, Chengde Wu, Rosario S. Castillo, Venkatachalapathi Yalamoori, Vitukudi N. Balaji
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Patent number: 5591761Abstract: Thiophenyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, isoxazolyl-thiophenyl-sulfonamides, isoxazolyl-furyl-sulfonamides and isoxazolyl-pyrrolyl-sulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.Type: GrantFiled: April 5, 1994Date of Patent: January 7, 1997Assignee: Texas Biotechnology CorporationInventors: Ming F. Chan, Bore G. Raju, Adam Kois, Erik J. Verner, Chengde Wu, Rosario S. Castillo, Venkatachalapathi Yalamoori, Vitukudi N. Balaji
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Patent number: 5589439Abstract: Herbicidal novel tetrazolinone derivatives of the formula: ##STR1## wherein R.sup.1 is alkyl, haloalkyl, cycloalkyl, alkenyl, haloalkenyl, alkynyl, alkoxy or phenyl which is optionally substituted, andR.sup.2 is alkyl, haloalkyl, cycloalkyl, alkenyl, haloalkenyl, alkynyl, alkoxy or phenyl which is optionally substituted, orR.sup.1 and R.sup.2 form, together with the nitrogen atom to which R.sup.1 and R.sup.2 are bonded, a 5- or 6-membered heterocyclic ring, optionally fused to a carbocyclic ring optionally and independently substituted by C.sub.1-4 alkyl, andR.sup.3 is a 5-membered heterocyclic radical containing at least one hereto atom selected from the group consisting of nitrogen, oxygen, and sulfur, optionally substituted by at least one substitutent selected from the group consisting of halogen, benzyl, phenyl, halogen-substituted phenyl, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylthio, C.sub.1-4 alkyl-sulfonyl and C.sub.Type: GrantFiled: July 28, 1995Date of Patent: December 31, 1996Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Koichi Moriya, Fritz Maurer, Seishi Ito, Katsuaki Wada, Kazuhiro Ukawa, Ryo Watanabe, Asami Ito, Natsuko Minegishi
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Patent number: 5571821Abstract: Sulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided. The sulfonamides have formula I: ##STR1## in which Ar.sup.1 is a 3- or 5-isoxazolyl and Ar.sup.2 is selected from among alkyl, including straight and branched chains, aromatic rings, fused aromatic rings and heterocyclic rings, including 5-membered heterocycles with one, two or more heteroatoms and fused ring analogs thereof and 6-membered rings with one, two or more heteroatoms and fused ring analogs thereof. Ar.sup.2 is preferably thiophenyl, furyl, pyrrolyl, naphthyl, and phenyl. Compounds in which Ar.sup.Type: GrantFiled: May 20, 1994Date of Patent: November 5, 1996Assignee: Texas Biotechnology CorporationInventors: Ming Fai Chan, Bore G. Raju, Adam Kois, Erik J. Verner, Chengde Wu, Rosario S. Castillo, Venkatachalapathi Yalamoori, Vitukudi N. Balaji, Kalyanaraman Ramnarayan
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Patent number: 5571810Abstract: This invention relates to new thiophene derivatives having antiinflammatory and analgesic activities and represented by the general formula [I]: ##STR1## wherein R.sup.1 is hydrogen, halogen, cyano, substituted lower alkyl, substituted or unsubstituted lower alkenyl, acyl, nitro, substituted or unsubstituted amino, sulfo, substituted or unsubstituted sulfamoyl, N-containing heterocyclicsulfonyl, hydoxy, substituted or unsubstituted heterocyclic group,R.sup.2 is substituted or unsubstituted aryl, andR.sup.3 is substituted or unsubstituted aryl, provided that R.sup.3 is aryl substituted with substituent(s) selected from the group consisting of amino, mono(lower)-alkylamino, acylamino, lower alkyl(acyl)amino and sulfamoyl when R.sup.1 is hydrogen, halogen or cyano, and pharmaceutically acceptable salts thereof, to processes for the preparation thereof and to a pharmaceutical composition comprising the same.Type: GrantFiled: April 13, 1995Date of Patent: November 5, 1996Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaaki Matsuo, Kiyoshi Tsuji, Nobukiyo Konishi, Katsuya Nakamura
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Patent number: 5554633Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; X and Y are each H or together form a group=O; Z is O, S or NR.sup.9, where R.sup.9 is H or C.sub.1-6 alkyl; R.sup.1 represents H or C.sub.1-6 alkyl; R.sup.2 represents C.sub.1-6 alkyl substituted by CONR.sup.7 (CH.sub.2).sub.p R.sup.8 (where R.sup.7 is H or C.sub.1-6 alkyl, R.sup.8 is optionally substituted heteroaryl and p is 0, 1, 2, 3, 4, 5 or 6); R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkynyl; R.sup.4 represents H, C.sub.1-6 alkyl or optionally substitute phenyl; R.sup.5 represents optionally substituted phenyl; R.sup.6 is H or C.sub.1-6 alkyl; and q is 0, 1, 2 or 3; are tachykinin antagonists useful in therapy.Type: GrantFiled: January 27, 1995Date of Patent: September 10, 1996Assignee: Merck, Sharp & Dohme, Ltd.Inventor: Martin R. Teall
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Patent number: 5523302Abstract: This invention relates to novel compounds containing basic and acidic termini, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.Type: GrantFiled: November 24, 1993Date of Patent: June 4, 1996Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Gary A. Cain, Charles J. Eyermann
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Patent number: 5514691Abstract: N-(4-halo-isoxazolyl)sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(4-halo-3-isoxazolyl)sulfonamides and N-(4-halo-5-isoxazolyl)benzenesulfonamides and methods for inhibiting the binding of an endothelin peptide to an endothelin receptor or increasing the activity of endothelin peptides by contacting the receptor with a sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.Type: GrantFiled: October 21, 1993Date of Patent: May 7, 1996Assignee: Immunopharmaceutics, Inc.Inventors: Ming F. Chan, Bore G. Raju, Rosario S. Castillo, Adam Kois, Chengde Wu, Yalamoori Venkatachalapathi, Erik J. Verner, Vitukudi N. Balaji
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Patent number: 5514696Abstract: Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: R.sup.1, R.sup.2 and R.sup.3 are each independently(a) hydrogen, except that R.sup.1 is other than hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z.sup.1, Z.sup.2 and Z.sup.3 ;(c) halo;(d) hydroxyl;(e) cyano;(f) nitro;(g) --C(O)H or --C(O)R.sup.6 ;(h) --CO.sub.2 H or --CO.sub.2 R.sup.6 ;(i) --SH, --S(O).sub.n R.sup.6, --S(O).sub.m --OH, --S(O).sub.m --OR.sup.6, --O--S(O).sub.m --R.sup.6, --O--S(O).sub.m OH or --O--S(O).sub.m --OR.sup.6 ;(j) --Z.sup.4 --NR.sup.7 R.sup.8 ; or(k) --Z.sup.4 --N(R.sup.11 --Z.sup.5 --NR.sup.9 R.sup.10 ;and the remaining symbols are as defined in the specification.Type: GrantFiled: October 29, 1993Date of Patent: May 7, 1996Assignee: Bristol-Myers Squibb Co.Inventors: Natesan Murugesan, John T. Hunt, Philip D. Stein
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Patent number: 5510477Abstract: High quality acyl lactam imides are prepared by reacting an acyl lactam of the formula ##STR1## where 5 carbon atoms and an acylating acid of the formula R'CO.sub.2 H or by reacting a lactam, an anhydride of the formula (RCO).sub.2 O where R is 1 to 5 carbon atoms and an acylating acid, preferably in the presence of a base catalyst. The process affords acyl lactam imides in high yield and at lower reaction temperatures by providing for the removal of volatile carboxylic acid by-products under vacuum or by the use of a stripping gas. The acyl lactam imides are particularly suited for use as bleach activators in detergent compositions.Type: GrantFiled: March 1, 1994Date of Patent: April 23, 1996Assignee: The Procter & Gamble CompanyInventors: Alan D. Willey, Larry E. Miller
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Patent number: 5508450Abstract: Benzopyran derivatives which have an inhibitory effect on the Maillard reaction as well as an antioxidizing effect are described herein. These derivatives may be utilized in the treatment and/or prevention of diabetic complications such as, for example, coronary heart disease, peripheral circulatory insufficiency or failure, cerebrovascular hindrance, neurogenous diabetes, nephropathy, arteriosclerosis, arthrosclerosis, cataracts and retinopathy. Further, the derivatives may also be used in the treatment and/or prevention of diseases induced by aging and in the treatment and/or prevention of diseases caused by the formation of peroxidized fat.Type: GrantFiled: September 30, 1994Date of Patent: April 16, 1996Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Masaaki Toda, Tsumoru Miyamoto
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Patent number: 5506254Abstract: Pyrazolyl derivatives of the general formula I ##STR1## where the indices and the substituents have the following meanings: n is is 0, 1, 2, 3 or 4, it being possible for the radicals R.sup.1 to be different if n is greater than 1;m is 0, 1 or 2, it being possible for the radicals R.sup.3 to be different if m is greater than 1;R.sup.1 is nitro, cyano, halogen,alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio,unsubstituted or substituted phenyl or phenoxy;R.sup.2 is hydrogen,unsubstituted or substituted alkyl, alkenyl or alkynyl,an unsubstituted or substituted, saturated or mono- or diunsaturated ring,an unsubstituted or substituted, mono- or binuclear aromatic radical;R.sup.3 is nitro, cyano, halogen, alkyl, haloalkyl, alkoxy or haloalkoxy;R.sup.4 is hydrogen, cyano, halogen, alkyl or haloalkyl,processes for their preparation and their use are described.Type: GrantFiled: July 6, 1995Date of Patent: April 9, 1996Inventors: Reinhard Kirstgen, Hartmann Konig, Hubert Sauter, Volker Harries, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5484780Abstract: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their methods of use for antagonizing angiotensin II receptors in mammals.Type: GrantFiled: December 14, 1994Date of Patent: January 16, 1996Assignee: Eli Lilly and CompanyInventors: Donald B. Boyd, Kenneth L. Hauser, Sherryl L. Lifer, Winston S. Marshall, Alan D. Palkowitz, William Pfeifer, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, Kumiko Takeuchi, K. Jeff Thrasher, Celia A. Whitesitt
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Patent number: 5478856Abstract: A styrene derivative represented by the formula (1) or a salt thereof: ##STR1##Type: GrantFiled: June 27, 1994Date of Patent: December 26, 1995Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Masahiro Suzuki, Kenzi Nozaki, Toshiyuki Hosoya, Takashi Suzuki, Yuzi Basaki, Mitiyo Kozima, Naosuke Matsuura
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Patent number: 5478934Abstract: Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof; useful for treating disorders of the central nervous system.Type: GrantFiled: November 23, 1994Date of Patent: December 26, 1995Inventors: Jun Yuan, Jan W. F. Wasley
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Patent number: 5464853Abstract: N-(5-isoxazolyl)biphenylsulfonamides and N-(3-isoxazolyl)biphenylsulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(5-isoxazolyl)biphenylsulfonamides and N-(3-isoxazolyl)biphenylsulfonamides and methods for inhibiting the binding of an endothelin peptide to an endothelin receptor or increasing the activity of endothelin peptides by contacting the receptor with a sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.Type: GrantFiled: October 21, 1993Date of Patent: November 7, 1995Assignee: ImmunoPharmaceutics, Inc.Inventors: Ming F. Chan, Bore G. Raju, Rosario S. Castillo, Adam Kois, Chengde Wu, Vitukudi Balaji
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Patent number: 5461067Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed wherein R.sub.1, R.sub.2, R.sub.5, R.sub.6, Y.sub.m and Y'.sub.n are herein defined.Type: GrantFiled: February 1, 1994Date of Patent: October 24, 1995Assignee: Abbott LaboratoriesInventors: Daniel W. Norbeck, Hing L. Sham, Dale J. Kempf, Chen Zhao
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Patent number: 5434267Abstract: Process for the preparation of compounds of the formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, X and n have the meaning given in the description, by reacting acetates with carbon monoxide in the presence of a basic auxiliary, followed by alkylation. The products are intermediates for fungicidal acrylates.Type: GrantFiled: March 14, 1994Date of Patent: July 18, 1995Assignee: Bayer AktiengesellschaftInventors: Helmut Kraus, Alexander Klausener, Hans-Joachim Diehr
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Patent number: 5403930Abstract: A compound of the formula Het--NR--SO.sub.2 --Ph.sup.2 --A--Ph.sup.1 (COOH)(OH) and tautomic 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: October 7, 1993Date of Patent: April 4, 1995Assignee: Pharmacia ABInventors: Hubert Agback, Leif Ahrgren, Thomas Berglindh, Martin Haraldsson, Goran Smedeg.ang.rd, Lars-Inge Olsson
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Patent number: 5378729Abstract: The present invention relates to compounds exhibiting central nervous system (CNS) activity which are useful in the treatment of epilepsy and other CNS disorders. The compounds of this invention have the following general formula: ##STR1## and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 4, 1991Date of Patent: January 3, 1995Assignee: Research Corporation Technologies, Inc.Inventors: Harold L. Kohn, Darrell Watson
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Patent number: 5378715Abstract: Compounds of the formula ##STR1## inhibit endothelin, wherein: one of X and Y is N and the other is O; R is naphthyl or naphthyl substituted with R.sup.1, R.sup.2 and R.sup.3 ;R.sup.1, R.sup.2 and R.sup.3 are each independently hydrogen; alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, or aralkyl, any of which may be substituted with Z.sup.1, Z.sup.2 and Z.sup.3 ; halo; hydroxyl; cyano; nitro; --C(O)H; --C(O)R.sup.6 ; CO.sub.2 H; --CO.sub.2 R.sup.6 ; --SH; --S(O).sub.n R.sup.6 ; --S(O).sub.m --OH; --S(O).sub.m --OR.sup.6 ; --O--S(O).sub.m --R.sup.6 ; --O--S(O).sub.m OH; --O--S(O).sub.m --OR.sup.6 ; --Z.sup.4 --NR.sup.7 R.sup.8 ; or --Z.sup.4 --N(R.sup.11)--Z.sup.5 --NR.sup.9 R.sup.10 ;R.sup.4 and R.sup.5 are each independently hydrogen; alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, or aralkyl, any of which may be substituted with Z.sup.1, Z.sup.2 and Z.sup.Type: GrantFiled: July 15, 1993Date of Patent: January 3, 1995Assignee: Bristol-Myers Squibb Co.Inventors: Philip D. Stein, John T. Hunt, Natesan Murugesan
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Patent number: 5340832Abstract: A novel prolinal derivative of the general formula: ##STR1## [wherein A represents alkylene or alkenylene group of from 1 to 8 carbon atom(s) or a saturated hydrocarbon ring of from 3 to 7 carbon atoms, R represents hydrogen atom, phenyl group, benzyl group, alkyl group of from 1 to 8 carbon atom(s) or cycloalkyl group of from 3 to 7 carbon atoms,B represents alkylene group of from 1 to 8 atom(s) unsubstituted or substituted by phenyl group or benzyl group, or a single bond,D represents carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three of halogen atom, alkyl or alkoxy group of from 1 to 4 carbon atom(s), nitro group or trifluoromethyl group.]possess inhibitory activity on prolyl endopeptidase, and therefore are useful for treating and/or preventing agent as a amnesia.Type: GrantFiled: August 17, 1993Date of Patent: August 23, 1994Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaaki Toda, Shuichi Ohuchida, Hiroyuki Ohno
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Patent number: 5326911Abstract: Ortho-amides of the formula ##STR1## can be prepared by reacting salts of the formula ##STR2## with alcoholates of the formulaM.sup.1 OR.sup.1 (III)where the radicals R.sup.1 to R.sup.4, M.sup.1 and X.sup..crclbar. have the meaning given in the description. The alcoholates are employed in highly active form with an effective content of 98-100% M.sup.1 OR.sup.1.Type: GrantFiled: July 20, 1992Date of Patent: July 5, 1994Assignee: Bayer AktiengesellschaftInventors: Heinz-Ulrich Blank, Helmut Kraus, Gerhard Marzolph, Nikolaus Muller