1,2,5-thiadiazoles (including Hydrogenated) Patents (Class 514/362)
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Publication number: 20020028799Abstract: The present invention relates to the use of neutral endopeptidase inhibitors (NEPi) and a combination of NEPi and phosphodiesterase type 5 (PDE5) inhibitor for the treatment of male sexual dysfunction, in particular MED.Type: ApplicationFiled: June 29, 2001Publication date: March 7, 2002Inventors: Alasdair Mark Naylor, Pieter Hadewijn Van Der Graaf, Christopher peter Wayman
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Publication number: 20020025973Abstract: This invention provides compounds of Formula I having the structure 1Type: ApplicationFiled: July 12, 2001Publication date: February 28, 2002Applicant: American Home Products CorporationInventors: William F. Fobare, Jill Freymuller
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Patent number: 6344454Abstract: This invention describes the new, nonsteroidal gestagens of general formula I in which A, B, Ar, R1, R2 and R3 have the meanings that are indicated in more detail in the description. The new compounds show a very great affinity to the gestagen receptor. They can be used alone or in combination with estrogens in contraceptive preparations. In addition, they can be used for treating endometriosis. Together with estrogens, they can also be used in preparations for treating gynecological disorders, for treating premenstrual symptoms and for substitution therapy. Based on the androgenic action, they can also be used for male birth control, male HRT and hormone therapy and for treating andrological disease agents.Type: GrantFiled: September 14, 2000Date of Patent: February 5, 2002Assignee: Schering AktiengesellschaftInventors: Manfred Lehmann, Klaus Schoellkopf, Peter Strehlke, Nikolaus Heinrich, Karl-Heinrich Fritzemeier, Rolf Krattenmacher, Hans-Peter Muhn
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Patent number: 6340697Abstract: Various oxime derivatives are provided, which do not cause any chemical damage to plants and which exhibit sufficient effectiveness against various plant diseases. The oxime derivatives are expressed by two general chemical formulas (1) and (2), as follows. Agricultural chemicals and plant disease control chemicals are also provided which contain the above mentioned oxime derivatives as active ingredients. Test results of these agricultural chemicals and the plant disease control chemicals are proved to be very effective for downey mildews and late blights or Phytophthora rot etc.Type: GrantFiled: June 12, 2000Date of Patent: January 22, 2002Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Takeo Kobori, Tomoko Goto, Hitoshi Kondo, Hiroyuki Tsuboi, Mika Iiyama, Toru Asada, Takashi Goto
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Patent number: 6329366Abstract: A pharmaceutical compound of the formula in which R1 and R2 are each hydrogen, halo, cyano or methyl, the dotted line represents an optional double bond, where R4 and R5 are each hydrogen, C1-6 alkyl, cyclopropyl or cyclopropyl-C1-6 alkyl, n is 0 or 1, and R3 is —SR6, —SOR6, —SO2R6, —COR6, —CH2OH or —CONHR7, where R6 is C1-6 alkyl and R7 is hydrogen or C1-6 alkyl; provided that when one of R1 and R2 is hydrogen and the other is fluoro, R4 and R5 are each hydrogen or C1-6 alkyl, and n is 0, then R3 is not —COR6 or —CONHR7; and salts thereof.Type: GrantFiled: November 18, 1999Date of Patent: December 11, 2001Assignee: Eli Lilly and Company LimitedInventors: John Fairhurst, Peter Thaddeus Gallagher, Martin Victor Miles
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Patent number: 6329372Abstract: Phenylalanine derivatives of formula (1) are described: wherein R is a carboxylic acid or a derivative thereof; L1 is a linker atom or group; Het is an optionally substituted heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of alpha4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.Type: GrantFiled: January 26, 1999Date of Patent: December 11, 2001Assignee: Celltech Therapeutics LimitedInventors: John Clifford Head, Sarah Catherine Archibald, Graham John Warrellow, John Robert Porter
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Patent number: 6329373Abstract: A compound of formula (I) wherein X is a —CONHOH group and the R groups are defined in the claims. The compounds are inhibitors of matrix metalloproteinases involved in tissue degradation and inhibitors of the release of tumour necrosis factor from cells.Type: GrantFiled: January 7, 2000Date of Patent: December 11, 2001Assignee: British Biotech Pharmaceuticals, Ltd.Inventors: Fionna Mitchell Martin, Christopher Norman Lewis, Mark Whittaker
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Publication number: 20010031774Abstract: A composition and method for protecting and immunizing plants against attack by insects, acarina and nematodes, comprising at least two active ingredient components in amounts having synergistic action, together with a suitable carrier, wherein component I is a compound of formula 1Type: ApplicationFiled: January 27, 2001Publication date: October 18, 2001Inventors: Michael Oostendorp, Wilhelm Ruess
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Patent number: 6281233Abstract: The present invention relates to a novel method for treating a mammal suffering from gastrointestinal motility disorders.Type: GrantFiled: June 7, 1995Date of Patent: August 28, 2001Assignee: Novo Nordisk A/SInventor: Beverley Greenwood
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Patent number: 6281232Abstract: The present invention relates to a novel method for treating a mammal suffering from gastrointestinal motility disorders.Type: GrantFiled: June 7, 1995Date of Patent: August 28, 2001Assignee: Novo Nordisk A/SInventor: Beverley Greenwood
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Patent number: 6262089Abstract: New compounds have the formula: wherein R, R1, X and Y have the meanings described herein. Methods are set forth for synthesizing these compounds and using these compounds to treat diseases associated with amyloidosis, such as Alzheimer's disease, maturity onset diabetes mellitus, familial amyloid polyneuropathy, scrapie, and Kreuzfeld-Jacob disease.Type: GrantFiled: February 16, 2000Date of Patent: July 17, 2001Assignee: Hoffman-La Roche Inc.Inventors: Cornelia Hertel, Torsten Hoffmann, Roland Jakob-Roetne, Roger David Norcross
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Patent number: 6258851Abstract: Compounds of formula (I), wherein A, B, X, R1, R2, R3, R4, R5, R6 are as defined in the specification, are matrix metalloproteinase inhibitors.Type: GrantFiled: October 8, 1999Date of Patent: July 10, 2001Assignee: British Biotech Pharmaceuticals LimitedInventors: Christopher David Floyd, Sanjay Ratilal Patel, Mark Whittaker
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Patent number: 6248755Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6, R14 and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.Type: GrantFiled: April 4, 2000Date of Patent: June 19, 2001Assignee: Merck & Co., Inc.Inventors: Kevin Chapman, Jeffrey Hale, Dooseop Kim, Christopher Lynch, Shrenik Shah, Kothandaraman Shankaran, Dong-Ming Shen, Christopher Willoughby, Malcolm MacCoss, Sander G. Mills, Jennifer L. Loebach, Ravindra N. Guthikonda
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Patent number: 6225329Abstract: The present invention provides novel compounds of Formula 1, compositions containing these compounds, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTP&agr;, LAR and HePTP or the like, wherein A, R1, R2, R3, R4, R16 and R17 are as defined in the specification.Type: GrantFiled: March 9, 1999Date of Patent: May 1, 2001Assignee: Novo Nordisk A/SInventors: Lutz Stefan Richter, Henrik Sune Andersen, Josef Vagner, Claus Bekker Jeppesen, Niels Peter Hundahl Møller, Sven Branner, Jing Su, Farid Bakir, Luke Milburn Judge
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Patent number: 6197800Abstract: Novel compounds of the formula I in which R is X is O or S, and R1, R2, R3, R4, R5 and R6 have the meaning indicated in patent claim 1, or a tautomeric ring-closed form, and the (E) isomers and their salts exhibit endothelin receptor-antagonistic properties.Type: GrantFiled: March 27, 2000Date of Patent: March 6, 2001Assignee: Merck Patent Gesellschaft mi beschraenkter HaftungInventors: Dieter Dorsch, Mathias Osswald, Werner Mederski, Claudia Wilm, Maria Christadler, Claus Jochen Schmitges
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Patent number: 6191159Abstract: The present application describes disubstituted pyrazolines and triazolines of formulae I and II: or pharmaceutically acceptable salt forms thereof, wherein one of M1 and M2 maybe N and D may be a variety of N-containing groups, which are useful as inhibitors of factor Xa.Type: GrantFiled: March 26, 1999Date of Patent: February 20, 2001Assignee: Dupont Pharmaceuticals CompanyInventor: Donald J. P. Pinto
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Patent number: 6187798Abstract: The present invention provides aza-bicyclo[2.2.1]heptane compounds which are useful for modulating a muscarinic receptor.Type: GrantFiled: June 1, 1999Date of Patent: February 13, 2001Assignee: Eli Lilly and CompanyInventors: Leander Merritt, Lone Jeppesen, John S. Ward
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Patent number: 6159938Abstract: Provided are methods of inhibiting the activity of a serine protease using protease inhibitors that include an alpha-keto heterocycle in their structure. The methods are useful in the treatment of ischemic heart or treatment of symptoms associated with blood coagulation disorders. Also provided are methods for detecting or quantifying the activity of a serine protease in a pure sample.Type: GrantFiled: May 20, 1997Date of Patent: December 12, 2000Assignee: Cortech, Inc.Inventors: Albert C. Gyorkos, Lyle W. Spruce, Axel H. Leimer, John C. Cheronis
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Patent number: 6159994Abstract: Compounds of formula (I) and pharmaceutically acceptable salt thereof are useful as histamine H.sub.3 receptor ligands. R.sup.1 is an optional substituent such as C.sub.1 to C.sub.6 alkyl. The moiety (1) replaces any available hydrogen atom on a carbon or nitrogen atom in the ring which includes X. R.sup.2 is C.sub.1 to C.sub.8 hydrocarbylene (in which one or more hydrogen atoms may be replaced by halogen atoms, and up to 2 carbon atoms may be replaced by oxygen, nitrogen or sulfur atoms); R.sup.3 replaces any available hydrogen atom on a carbon or nitrogen atom in the ring which includes X, and is hydrogen or C.sub.1 to C.sub.15 hydrocarbyl (in which one or more hydrogen atoms may be replaced by halogen atoms, and up to 3 carbon atoms may be replaced by oxygen, nitrogen or sulfur atoms); the (or each) R.sup.4 group is independently selected from H, non-aromatic C.sub.1 to C.sub.6 hydrocarbyl, and aryl (C.sub.1 to C.sub.3 alkyl); X is --SO-- or --SO.sub.2 --; Y and Z are each hydrogen, or together represent .Type: GrantFiled: March 13, 2000Date of Patent: December 12, 2000Assignee: James Black FoundationInventors: Iain Mair McDonald, David John Dunstone, Matthew John Tozer
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Patent number: 6124312Abstract: The present invention provides heterocyclic 2-aza-bicyclo[2.2.1]heptane compounds which are useful for modulating a muscarinic ptor.Type: GrantFiled: June 1, 1999Date of Patent: September 26, 2000Assignee: Eli Lilly and CompanyInventors: Charles H Mitch, Steven J Quimby, Jon K Reel, Celia A Whitesitt
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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: 6096769Abstract: The invention relates a concentrated liquid fungicidal composition comprising a fungicidally acceptable carrier and/or surface active agent and(a) at least one compound of formula I, ##STR1## (b) one or more additional fungicidal active ingredients, which exist as a suspension of fire particles;(c) a solubilizing agent; and(d) a dispersing agent, which has the capability to adsorb irreversibly on the surfaces of hydrophobic particles suspended in water or polar organic solvents.Type: GrantFiled: April 20, 1998Date of Patent: August 1, 2000Assignee: American Cyanamid CompanyInventors: Michael Perlitz, Friedrich Schmidt, Annerose Edith Elise Rehnig, Ewald Gerhard Sieverding, Christopher William Horsler
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Patent number: 6075040Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity.Type: GrantFiled: May 2, 1997Date of Patent: June 13, 2000Assignee: Eli Lilly and CompanyInventors: Michael Gregory Bell, Thomas Alan Crowell, Cynthia Darshini Jesudason, Donald Paul Matthews, John Hampton McDonald, III, David Andrew Neel, Christopher John Rito, Anthony John Shuker, Mark Alan Winter
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Patent number: 6069159Abstract: The present invention provides heterocyclic compounds which are useful for modulating a muscarinic receptor.Type: GrantFiled: May 10, 1999Date of Patent: May 30, 2000Assignee: Eli Lilly and CompanyInventors: Leander Merritt, Lone Jeppesen, John S Ward
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Patent number: 6060492Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity. The invention provides compounds and method of treating type II diabetes, comprising administering to a mammal in need thereof compounds of the Formula II: ##STR1## The variables in Formula II are defined herein.Type: GrantFiled: June 25, 1997Date of Patent: May 9, 2000Assignee: Eli Lilly and CompanyInventors: Michael Gregory Bell, Thomas Alan Crowell, Donald Paul Matthews, John Hampton McDonald, III, David Andrew Neel, Anthony John Shuker, Mark Alan Winter
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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: 6048859Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: February 16, 1999Date of Patent: April 11, 2000Assignee: Merck & Co., Inc.Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
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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: 6022875Abstract: Disclosed in this invention is a method of analgesic treatment comprising administering an effective analgesic amount of a substituted 2,4-imidazolidinedione compound.Type: GrantFiled: July 31, 1998Date of Patent: February 8, 2000Assignee: Gruenenthal GmbHInventors: Oswald Zimmer, Norma Selve
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Patent number: 6017939Abstract: The invention concerns compounds of formula (I),in which R is (i), (ii) or (iii); n is 0, 1 or 2; X means O or S; and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have different meanings, or a cyclized tautomeric shape. The invention also concerns the (E) isomers and salts of these compounds which display endothelin receptor antagonistic properties.Type: GrantFiled: November 12, 1998Date of Patent: January 25, 2000Assignee: Merck Patent GesellschaftInventors: Dieter Dorsch, Mathias Osswald, Werner Mederski, Claudia Wilm, Claus Schmitges, Maria Christadler, Soheila Anzali
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Patent number: 6015813Abstract: The present invention relates to therapeutically active azabicyclic compounds of formula I ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3, Ar, m and n are defined in the description, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a disease in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: April 8, 1998Date of Patent: January 18, 2000Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Per Sauerberg
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Patent number: 6013644Abstract: The present invention is directed spiro-substituted azacycles of formula I: (wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, k, l and m are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.Type: GrantFiled: December 12, 1997Date of Patent: January 11, 2000Assignee: Merck & Co., Inc.Inventors: Sander G. Mills, Malcolm Maccoss, Martin S. Springer
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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: 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: 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: 5977129Abstract: The present invention relates to compounds of formula I: whereinone or both G is an azacyclic ring of formula II: ##STR1## and Z is oxygen or sulfur and the remaining variables are as defined in the specification. The compounds are useful as stimulants of the cognitive function of the forebrain and hippocampus of mammals and especially in the treatment of Alzheimer's disease, severe painful conditions and glaucoma.Type: GrantFiled: May 3, 1995Date of Patent: November 2, 1999Assignee: Novo Nordisk A/SInventors: Preben H. Olesen, Per Sauerberg
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Patent number: 5972978Abstract: 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: February 19, 1999Date of Patent: October 26, 1999Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Niels Peter Hundahl Moller, Peter Madsen
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Patent number: 5972937Abstract: The invention relates to heterocyclic families of compounds having pharmacological activity, in particular possessing 5HT.sub.2C receptor antagonist activity processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders.Type: GrantFiled: September 16, 1997Date of Patent: October 26, 1999Assignee: SmithKline Beecham p.l.c.Inventors: Laramie Mary Gaster, Paul Adrian Wyman, Keith Raymond Mulholland, David Thomas Davies
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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: 5945413Abstract: This invention relates to a novel class of compounds that are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.Type: GrantFiled: September 30, 1996Date of Patent: August 31, 1999Assignee: Vertex Pharmaceuticals IncorporatedInventors: Roger Dennis Tung, Francesco Gerald Salituro, David D. Deininger, Govinda Rao Bhisetti, Christopher Todd Baker, Andrew Spaltenstein
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Patent number: 5942546Abstract: A compound of the formula: ##STR1## wherein X is arylene, heteroarylene, fused arylene, fused heteroarylene, or deleted; Y is sulfonyl, --O--, or deleted; R.sub.1 is aryl, heteroaryl, fused aryl, or fused heteroaryl; R.sub.2 is H, lower alkyl, lower alkoxy, halo, nitro, cyano, haloalkyl, hydroxyl, carboxyl, amido, amino, or aminoalkyl; or a salt thereof are disclosed. Also disclosed are a pharmaceutical composition which contains an excipient and an effective amount of a compound of the above formula and a method of treating cancer which involves the administration of an effective amount of such a compound to a patient in need thereof.Type: GrantFiled: November 20, 1997Date of Patent: August 24, 1999Assignee: Development Center for BiotechnologyInventors: Ji-Wang Chern, Yu-Ling Leu, Shan-Shue Wang, Chin-Fen Lee, Shih-Chung Hsu
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Patent number: 5942535Abstract: The present invention relates to heterocyclic compounds of the formula ##STR1## in which R.sup.1 -R.sup.7, B, a and X have the meanings recited in the specification. These compounds are usable in the treatment of diseases of the rheumatoid group and for the prevention of allergically induced diseases.Type: GrantFiled: March 28, 1997Date of Patent: August 24, 1999Assignee: Merckle GmbHInventors: Stefan Laufer, Hans Gunther Striegel, Gerd Dannhardt
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Patent number: 5939443Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity. The invention provides compounds and method of treating type II diabetes, comprising administering to a mammal in need thereof compounds of the Formula II: ##STR1## The variables in Formula II are defined herein.Type: GrantFiled: June 25, 1997Date of Patent: August 17, 1999Assignee: Eli Lilly and CompanyInventors: Michael Gregory Bell, Thomas Alan Crowell, Christine Ann Droste, Donald Paul Matthews, John Hampton McDonald, III, Christopher John Rito, Anthony John Shuker, Mark Alan Winter
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Patent number: 5919809Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives of the formula ##STR1## and the pharmaceutically-acceptable salts thereof which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.Type: GrantFiled: November 4, 1993Date of Patent: July 6, 1999Assignee: Pfizer Inc.Inventors: Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte
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Patent number: 5914338Abstract: The present invention relates to therapeutically active azatricyclic compounds of formula I ##STR1## a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a disease in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: April 1, 1997Date of Patent: June 22, 1999Assignee: Novo NordiskInventors: Lone Jeppesen, Preben H. Olesen, Per Sauerberg
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Patent number: 5914351Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.Type: GrantFiled: December 12, 1997Date of Patent: June 22, 1999Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.Inventors: Walter Gerhard Brouwer, Ewa Maria Osika
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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: 5872116Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: October 28, 1997Date of Patent: February 16, 1999Assignee: Merck & Co., Inc.Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
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Patent number: RE36375Abstract: The present invention relates to therapeutically active azacyclic compounds. The novel compounds are useful as stimulants of the cognitive function of the forebrain and hippocampus of mammals and especially in the treatment of Alzheimer's disease, severe painful conditions and glaucoma.Type: GrantFiled: February 18, 1998Date of Patent: November 2, 1999Assignee: Novo Nordisk A/SInventors: Per Sauerberg, Preben H. Olesen, Charles H. Mitch