1,3,4-oxadiazoles (including Hydrogenated) Patents (Class 548/143)
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Patent number: 6156772Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.Type: GrantFiled: May 14, 1999Date of Patent: December 5, 2000Assignee: Merck & Co., Inc.Inventors: Mark Goulet, Thomas F. Walsh, Feroze Ujjainwalla, Matthew J. Wyvratt, Jr.
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Patent number: 6156702Abstract: 4-Benzoylpyrazoles of the formula I ##STR1## useful for controlling harmful plants, are disclosed.Type: GrantFiled: February 7, 2000Date of Patent: December 5, 2000Assignee: BASF AktiengesellschaftInventors: Stefan Engel, Joachim Rheinheimer, Ernst Baumann, Wolfgang von Deyn, Regina Luise Hill, Guido Mayer, Ulf Misslitz, Oliver Wagner, Matthias Witschel, Martina Otten, Helmut Walter, Karl-Otto Westphalen
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Patent number: 6150386Abstract: Compounds of formula (I) and their possible isomers and isomer mixtures, in which (Z) is a group (a), (b), (c) or (d) and in which the other substituents are as defined herein.Type: GrantFiled: December 22, 1997Date of Patent: November 21, 2000Assignee: Novartis Crop Protection, Inc.Inventors: Stephan Trah, Rene Zurfluh
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Patent number: 6133259Abstract: Amyloid binding compounds which are non-azo derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down's Syndrome are described. Pharmaceutical compositions containing non-azo derivatives of Chrysamine G and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using non-azo Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using non-azo Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.Type: GrantFiled: November 9, 1998Date of Patent: October 17, 2000Assignee: University of PittsburghInventors: William E. Klunk, Jay W. Pettegrew, Chester A. Mathis, Jr.
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Patent number: 6107311Abstract: A compound having the structure: ##STR1## wherein (a) n is from 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) W is O or S; and(f) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: April 9, 1998Date of Patent: August 22, 2000Assignee: The Procter & Gamble CompanyInventors: Laurence Ichih Wu, John Michael Janusz
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Patent number: 6100238Abstract: The present invention relates to certain substituted oxadiazole nonpeptides, which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.Type: GrantFiled: June 3, 1998Date of Patent: August 8, 2000Assignee: Cortech Inc.Inventors: Albert C. Gyorkos, Lyle W. Spruce
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Patent number: 6066766Abstract: 4-Chlorobiphenyls are prepared by reacting a haloaromatic with an aryl Grignard compound, where halogen is chlorine, bromine or iodine, in the presence of a palladium catalyst of the formula (IV) ##STR1##Type: GrantFiled: August 3, 1999Date of Patent: May 23, 2000Assignee: Clariant GmbHInventors: Steffen Haber, Stefan Scherer, Andreas Meudt, Antje Noerenberg
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Patent number: 6051572Abstract: A class of azetidine, pyrrolidine and piperidine derivatives, substituted by inter alia a phenylmorpholinyl, phenylpiperidinyl or benzimidazolone moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.Type: GrantFiled: April 28, 1998Date of Patent: April 18, 2000Assignee: Merck Sharp & Dohme Ltd.Inventor: Jose Luis Castro Pineiro
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Patent number: 6036890Abstract: Photochromic diaryl-2H-naphthopyran structures, which dye photochromically well at room temperature, lighten up quickly when incorporated into ophthalmic lenses, possess longevity, and due to their spacial structures, have a reduced tendency of the molecules to migrate in plastics.Type: GrantFiled: July 31, 1998Date of Patent: March 14, 2000Assignee: Optische Werke G. RodenstockInventors: Manfred Melzig, Herbert Zinner
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Patent number: 6037367Abstract: Compounds of formula (I) wherein: R.sub.1 is --(CR.sub.4 R.sub.5).sub.n C(O)O(CR.sub.4 R.sub.5).sub.m R.sub.6, --(CR.sub.4 R.sub.5).sub.n C(O)NR.sub.4 (CR.sub.4 R.sub.5).sub.m R.sub.6, (CR.sub.4 R.sub.5).sub.n O(CR.sub.4 R.sub.5).sub.m R.sub.6, or --(CR.sub.4 R.sub.5).sub.r R.sub.6 : W is alkynyl or 2 carbon atoms; R.sub.3 is H or R.sub.7 ; Z is C(O)R.sub.13, (CH.sub.2).sub.0-1 C(O)OR.sub.13, (CH.sub.2).sub.0-1 C(O)NR.sub.10 R.sub.13, (CH.sub.2).sub.0-1 C(R.sub.8 R.sub.8)OR.sub.8, --NHC(O)R.sub.7, (CH.sub.2).sub.0-1 NR.sub.10 R.sub.13, NH[C(O)C(O)OR.sub.8 ], CH.sub.2 NH[C(O)CNR.sub.10 R.sub.13 ], CH.sub.2 S(O).sub.q R.sub.7, CH[S(O).sub.q R.sub.7 ].sub.2, dithiolane, (tetrazol-5-yl), thiazol-2-yl, [1,2,4]thiadiazol-5-yl, [1,3,4]oxadiazol-2-yl, imidazol-2-yl, oxazol-2-yl, or (3- or 5-oxadiazolyl[1,2,4]; R.sub.7 is --(CR.sub.4 R.sub.5).sub.q R.sub.11 or C.sub.1-6 alkyl wherein the R.sub.11 or C.sub.Type: GrantFiled: September 14, 1998Date of Patent: March 14, 2000Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski, James S. Frazee
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Patent number: 6030970Abstract: Novel to isooxazoles, oxazoles, thiazoles, isothiazoles and imidazoles, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.Type: GrantFiled: February 2, 1998Date of Patent: February 29, 2000Assignee: Smithkline Beecham CorporationInventors: John Duncan Elliott, Juan Ignacio Luengo, Jia-Ning Xiang
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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: 6008219Abstract: This invention relates to compounds of formula (I) ##STR1## which are useful as modulators of D.sub.3 receptors, in particular as antipsychotic agents.Type: GrantFiled: October 29, 1997Date of Patent: December 28, 1999Assignee: SmithKline Beech p.l.c.Inventors: Geoffrey Stemp, Christopher Norbert Johnson
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Patent number: 6001811Abstract: The present invention relates to oxadiazole, thiadiazole, and triazole peptoids that are inhibitors of serine protease, specifically human neutrophil elastase; which proteases are useful in treatment of adult respiratory distress syndrome, septic shock, and multiple organ failure.Type: GrantFiled: December 4, 1997Date of Patent: December 14, 1999Assignee: Cortech Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 5998379Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole, and triazole peptoids that are useful as inhibitors of serine proteases, in particular human neutrophil elastase. Serine protease inhibitors of the invention are useful in the treatment of, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.Type: GrantFiled: December 4, 1997Date of Patent: December 7, 1999Assignee: Cortech Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 5985903Abstract: Novel benzotriazoles of the formula ##STR1## in which R, X.sup.1, X.sup.2, X.sup.3, X.sup.4 and Y have the meanings given in the description,and their acid addition salts and metal salt complexes,a process for the preparation of these substances and their use as microbicides in crop protection and in material protection.Type: GrantFiled: December 19, 1997Date of Patent: November 16, 1999Assignee: Bayer AktiengesellschaftInventors: Lutz Assmann, Ralf Tiemann, Martin Kugler, Heinrich Schrage, Klaus Stenzel
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Patent number: 5985901Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.Type: GrantFiled: May 22, 1998Date of Patent: November 16, 1999Assignee: Merck & Co., Inc.Inventors: Mark Goulet, Feroze Ujjainwalla, Thomas F. Walsh, Matthew J. Wyvratt, Jr., Jonathan R. Young, Lin Chu
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Patent number: 5977373Abstract: The present invention provides thiadiazolyl and oxadiazolyl phenyl oxzolidinone compounds of formula I ##STR1## wherein Q is thiadiazolyl or oxadiazolyl; wherein X.sup.1 and X.sup.2 are independently hydrogen, fluorine or chlorine; andwherein R.sup.1 is, for example, --COCH.sub.3 or --COCH.sub.2 CH.sub.3.These compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive and gram-negative aerobic bacteria.Type: GrantFiled: July 8, 1998Date of Patent: November 2, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Robert C. Gadwood, Lisa Marie Thomasco, David John Anderson
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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: 5972935Abstract: The invention relates to novel heterocyclic compounds of formula (I) or a salt or N-oxide thereof, in which R is a group of formulae (i), (ii) or (iii), where R.sup.1 is hydrogen, halogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, COC.sub.1-6 akyl, C.sub.1-6 alkoxy, hydroxy, hydroxyC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkoxy, C.sub.1-6 alkoxyC.sub.1-6 alkoxy, acyle, nitro, trifluoromethyl, cyano, SR.sup.9, SOR.sup.9, SO.sub.2 R.sup.9, NR.sup.9 CONR.sup.10 R.sup.11, NR.sup.10 SO.sub.2 R.sup.11, SO.sub.2 NR.sup.11 r.sup.11, SO.sub.2 NR.sup.10 R.sup.11, CO.sub.2 R.sup.10, CONR.sup.10 R.sup.11, CO.sub.2 NR.sup.10 R.sup.11, CONR.sup.10 (CH.sub.2).sub.a CO.sub.2 R.sup.11, (CH.sub.2).sub.a NR.sup.10 R.sup.11, ##STR1## (CH.sub.2).sub.a CONR.sup.10 R.sup.11, (CH.sub.2).sub.a COR.sup.11, (CH.sub.2).sub.a CO.sub.2 C.sub.1-6 alkyl, CO.sub.2 (CH.sub.2).sub.a OR.sup.10, NR.sup.10 R.sup.11, N.dbd.CNR.sup.9 NR.sup.10 R.sup.11, NR.sup.10 CO(CH.sub.2).sub.a NR.sup.10 R.sup.11, NR.sup.10 CO.sub.2 R.sup.11, CONHNR.sup.10 R.sup.11, CR.Type: GrantFiled: April 24, 1998Date of Patent: October 26, 1999Assignee: SmithKline Beecham p.l.c.Inventor: Laramie Mary Gaster
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Patent number: 5965565Abstract: The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R.sup.1, R.sup.1a, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.5, D, X, Y, n, x and y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: December 11, 1997Date of Patent: October 12, 1999Assignee: Merck & Co., Inc.Inventors: Meng H. Chen, Zhijian Lu, Ravi Nargund, Arthur A. Patchett, James R. Tata, Lihu Yang, Mu Tsu Wu
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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: 5955491Abstract: The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which may be substituted; R.sup.2 and R.sup.3 independently are a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.4 is an alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl group which may be substituted; X is formula: --CHO or --CH.sub.2 OB (wherein B is a hydrogen atom or a protecting group of hydroxyl group); m and n independently are an integer of 0 or 1; provided that R.sup.4 is an alkanoyl group substituted by aryl, a sulfonyl group substituted by aryl having more than 9 carbon atoms or by lower alkyl, or a carbamoyl or thiocarbamoyl group which may be substituted when R.sup.1 is an unsubstituted lower alkyl, arylalkyl on methylthioethyl group, R.sup.2 and R.sup.3 independently are a lower alkyl or arylalkyl, X is --CHO, m is 1 and n is 0 or 1, or a salt thereof.Type: GrantFiled: June 27, 1995Date of Patent: September 21, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Yukio Fujisawa, Tsuneo Yasuma, Junji Mizoguchi, Masakuni Kori, Masayuki Takizawa
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Patent number: 5932363Abstract: A luminescent composition containing a mixture of a fluorescent material and a metal chelate compound of the formulaL.sub.n --M.sup.+n (I)wherein M represents a metal; n is a number of from 1 to 3, and L is a ligand of the formula ##STR1## wherein Ar is an aryl; X is selected from the group consisting of oxygen, sulfur, and selenium; N is nitrogen; O is oxygen, and Z is a suitable aromatic component.Type: GrantFiled: October 2, 1997Date of Patent: August 3, 1999Assignee: Xerox CorporationInventors: Nan-Xing Hu, Shuang Xie, Zoran D. Popovic, Beng S. Ong, Ah-Mee Hor
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Patent number: 5925472Abstract: A metal chelate compound of the formulaL.sub.n --M.sup.+n (I)wherein M represents a metal; n is an integer, or number of from 1 to 3; and L is a ligand of ##STR1## wherein Ar is aryl; X is selected from the group consisting of oxygen, sulfur, and selenium; N is nitrogen; O is oxygen; and Z is a suitable aromatic component.Type: GrantFiled: March 31, 1997Date of Patent: July 20, 1999Assignee: Xerox CorporationInventors: Nan-Xing Hu, Shuang Xie, Zoran D. Popovic, Beng S. Ong, Ah-Mee Hor
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Patent number: 5922744Abstract: The present invention provides a compound of formula: ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6a and R.sup.6b are defined herein or a pharmaceutically acceptable salt thereof, a process for its preparation, intermediates and its use as a tachykinin antagonist.Type: GrantFiled: January 12, 1998Date of Patent: July 13, 1999Assignee: Merck Sharp & Dohme LimitedInventors: Timothy Harrison, Andrew Pate Owens
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Patent number: 5916847Abstract: Arylheterocycles having the general formula (I): ##STR1## and process for preparing them. The arylheterocycles having the general formula (I) display high herbicidal activity.Type: GrantFiled: March 17, 1997Date of Patent: June 29, 1999Assignee: Isagro Ricerca S.r.l.Inventors: Franco Bettarini, Piero La Porta, Giovanni Meazza, Giampaolo Zanardi, Ernesto Signorini, Domenico Portoso
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Patent number: 5891852Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.Type: GrantFiled: December 6, 1996Date of Patent: April 6, 1999Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 5888941Abstract: Compounds of general formula I and their salts and solvates are antifungal agents and as such are useful in the treatment of various fungal infections. Pharmaceutical compositions including these compounds and processes for their preparation are also provided.Type: GrantFiled: March 31, 1997Date of Patent: March 30, 1999Assignee: J. Uriach & Cia. S.A.Inventors: Javier Bartroli, Enric Turmo, Manuel Anguita
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Patent number: 5886187Abstract: Benzene derivatives of the formula ##STR1## wheren is 0, 1 or 2,x is nitro or amino,Z is a direct bond or unsubstituted or substituted C.sub.1 -C.sub.6 -alkylene,Y is vinyl or a radical of the formula C.sub.2 H.sub.4 --Q, where Q is hydroxyl or a group which can be removed under alkaline reaction conditions,R.sup.1 and R.sup.2 are hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, halogen, nitro, amino, hydroxysulfonyl or a radical of the formula Z--S(O).sub.n --Y, where n, Z and Y have the abovementioned meanings, andHet is the radical of a heterocyclic ring, are described.Type: GrantFiled: January 26, 1998Date of Patent: March 23, 1999Assignee: BASF AktiengesellschaftInventors: Helmut Hagen, Manfred Patsch, Bernd-Peter Walther, Andrea Zamponi
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Patent number: 5885984Abstract: Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the blockade of ion channels and the treatment of arrhythmias.Type: GrantFiled: February 27, 1997Date of Patent: March 23, 1999Assignee: University of British ColumbiaInventors: Bernard A. MacLeod, Michael J. A. Walker, Richard A. Wall
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Patent number: 5886242Abstract: The invention relates to chiral compounds containing at least one divalent or polyvalent chiral group, at least one polymerizable group, at least one spacer and at least one mesogenic group, and to their use as polymerizable, chiral dopes for the preparation of cholesteric networks.The novel compounds are suitable for use in electro-optical displays or as chiral dopes for nematic or cholesteric liquid crystals in order to produce layers which reflect in colors.Type: GrantFiled: January 12, 1998Date of Patent: March 23, 1999Assignee: BASF AktiengesellschaftInventors: Karl-Heinz Etzbach, Paul Delavier, Karl Siemensmeyer, Gerhard Wagenblast, Lothar Laupichler, Volkmar Vill
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Patent number: 5874585Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of serine proteases including human neutrophil elastase, equivalently known as human leukocyte elastase.Type: GrantFiled: August 15, 1996Date of Patent: February 23, 1999Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 5869455Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.Type: GrantFiled: December 6, 1996Date of Patent: February 9, 1999Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 5863926Abstract: The present invention relates to novel 4,4-(disubstituted)cyclohexan-1-carboxylate monomers and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).Type: GrantFiled: October 6, 1997Date of Patent: January 26, 1999Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski, M. Dominic Ryan, Paul E. Bender
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Patent number: 5861421Abstract: This invention relates to derivatives of 4,4-(disubstituted)cyclohexan-1-ones and related compounds which are useful for treating allergic and inflammatory diseases.Type: GrantFiled: June 23, 1997Date of Patent: January 19, 1999Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski, M. Dominic Ryan, Paul E. Bender
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Patent number: 5861380Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.Type: GrantFiled: December 6, 1996Date of Patent: January 19, 1999Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 5849923Abstract: This invention relates to a compound of formula I ##STR1## in which T is --CONH-- or --CH=CH--;R.sup.a and R.sup.b are independently C.sub.1-6 alkyl;R.sup.C is C.sub.1-6 alkyl or hydrogen; andR is heteroaryl.Type: GrantFiled: June 4, 1996Date of Patent: December 15, 1998Assignee: Bristol-Myers Squibb CompanyInventors: John E. Starrett, Jr., David R. Tortolani, Muzammil M. Mansuri, Nicholas A. Meanwell
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Patent number: 5846906Abstract: Herbicidally active phenyldiketone compounds of the formula I ##STR1## in which the substituents have the following meanings: L and M are hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, C.sub.1 -C.sub.4 -alkoxy, it being possible for these groups to be unsubstituted or substituted by one to five halogen atoms or C.sub.1 -C.sub.4 -alkoxy, or halogen, cyano, nitro, a group --(Y).sub.n --S(O).sub.m R.sup.7 or a group --(Y).sub.n --CO--R.sup.8,Z is a 5- or 6-membered heterocyclic saturated or unsaturated radical which has one to three hetero atoms selected from the group consisting of oxygen, sulfur or nitrogen and which is unsubstituted or substituted by halogen, cyano, nitro, a group --CO--R.sup.8, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkylthio, di-C.sub.1 -C.sub.Type: GrantFiled: July 30, 1997Date of Patent: December 8, 1998Assignee: BASF AktiengesellschaftInventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Stefan Engel, Martina Otten, Marcus Vossen, Peter Plath, Harald Rang, Albrecht Harreus, Hartmann Konig, Helmut Walter, Karl-Otto Westphalen, Ulf Misslitz
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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: 5846907Abstract: Pyrazol-4-ylbenzoyl compounds of the formula I ##STR1## where Z is a 5- or 6-membered heterocyclic saturated or unsaturated radical, Q is a pyrazole ring and L and M are as defined in the specification, their use as herbicidal compounds and to processes for preparing the compounds.Type: GrantFiled: July 30, 1997Date of Patent: December 8, 1998Assignee: BASF AktiengesellschaftInventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Stefan Engel, Martina Otten, Marcus Vossen, Peter Plath, Harald Rang, Albrecht Harreus, Hartmann Konig, Helmut Walter, Karl-Otto Westphalen, Ulf Misslizt
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Patent number: 5840980Abstract: A diamine compound of the following formula (1): ##STR1## wherein R.sub.1 is a hydrogen atom, a lower alkyl group or a lower alkoxy group, each of A.sub.1, A.sub.2 and A.sub.3 which are independent of one another, is a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, or a group of the following formula (2): ##STR2## wherein R.sub.1 is as defined above, and X is a substituted or unsubstituted arylene group or a substituted or unsubstituted heterocyclic bivalent group.Type: GrantFiled: July 24, 1997Date of Patent: November 24, 1998Assignee: Hodogaya Chemical Co., Ltd.Inventors: Mitsutoshi Anzai, Atsushi Takesue, Takanobu Watanabe, Chieko Inayoshi
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Patent number: 5840217Abstract: Use of spiro compounds of the formula (I) ##STR1## where K.sup.1 and K.sup.2 are, independently of one another, conjugated systems, in electroluminescence devices.Preferred compounds of the formula (I) are 9,9'-spirobifluorene derivatives of the formula (II) ##STR2## where the benzo groups can be substituted independently of one another. Compounds of the formula (I) have a good solubility in customary organic solvents, improved film-forming properties and a significantly reduced tendency to crystallize. The production of electroluminescence devices is thereby made easier and their service life is increased.Type: GrantFiled: April 5, 1995Date of Patent: November 24, 1998Assignee: Hoechst AktiengesellschaftInventors: Donald Lupo, Josef Salbeck, Hermann Schenk, Thomas Stehlin, Roland Stern, Arno Wolf
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Patent number: 5837720Abstract: A compound of formula (I): ##STR1## and its pharmaceutically acceptable salt, wherein R is hydrogen or hydroxy; Ar is unsubstituted or substituted phenyl; X is unsubstituted or substituted phenyl or heterocyclic, mono-, di- or trihalomethyl, cyano, or the like; and X.sup.2 is phenyl, naphthyl, furyl, thienyl, pyridyl, thiazolyl, benzofuryl or benzothienyl, each of which may either be unsubstituted or substituted. These compounds have agonist activity toward opioid kappa receptors and are thus useful as analgesic, anti-inflammatory, diuretic and neuroprotective agents.Type: GrantFiled: April 17, 1997Date of Patent: November 17, 1998Assignee: Pfizer Inc.Inventor: Fumitaka Ito
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Patent number: 5824691Abstract: Guanidine derivatives of the formula: ##STR1## wherein Y is C--R.sup.1(in which R.sup.1 is hydrogen, lower alkyl, hydroxy, protected hydroxy, etc.,)R.sup.2 is pyrrolyl, tetrazolyl, pyrazolyl, etc.,R.sup.3 is hydrogen, lower alkoxy, hydroxy, protected hydroxy, etc.,Z is C--R.sup.4(in which R.sup.4 is hydrogen, carboxy, protected carboxy, nitro, halogen, hydroxy(lower)alkyl, etc.,), andW is R.sup.12(in which R.sup.12 is hydrogen, lower alkoxy, nitro, hydroxy or protected hydroxy)and pharmaceutically acceptable salts thereof which are useful as a medicament which are useful in inhibiting Na.sup.+ /H.sup.+ exchange in cells and in the prevention of cardiovascular diseases, cerebrovascular diseases, renal diseases, arteriosclerosis and shock.Type: GrantFiled: November 9, 1995Date of Patent: October 20, 1998Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Atsushi Kuno, Yoshikazu Inoue, Hisashi Takasugi, Hiroaki Mizuno, Kumi Yamasaki
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Patent number: 5824677Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.13. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.Type: GrantFiled: June 7, 1995Date of Patent: October 20, 1998Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
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Patent number: 5821250Abstract: A compound having the structure: ##STR1## wherein (a) n is from about 1 to about 3;(b) X is selected from the group consisiting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen; and(e) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: February 1, 1996Date of Patent: October 13, 1998Assignee: The Procter & Gamble CompanyInventors: Laurence Ichih Wu, John Michael Janusz
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Patent number: 5817679Abstract: 7-Aza-bicyclo?2.2.1!-heptane and -heptene derivatives are disclosed that can be administered to a mammal, including a human, to treat disorders associated with a decrease or increase in cholinergic activity.Type: GrantFiled: August 25, 1994Date of Patent: October 6, 1998Assignee: University of VirginiaInventors: T. Y. Shen, W. Dean Harman, Dao Fei Huang, Javier Gonzalez
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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: 5801148Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.Type: GrantFiled: December 6, 1996Date of Patent: September 1, 1998Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce