Plural Chalcogens Bonded Directly To Ring Carbons Of The Piperidine Ring Patents (Class 514/328)
  • Publication number: 20030191098
    Abstract: The present invention comprises a group of compounds that effectively inhibit angiogenesis. More specifically, thalidomide and various related compounds such as thalidomide precursors, analogs, metabolites and hydrolysis products have been shown to inhibit angiogenesis and to treat disease states resulting from angiogenesis. Additionally, antiinflammatory drugs, such as steroids and NSAIDs can inhibit angiogenesis dependent diseases either alone or in combination with thalidomide and related compounds. Importantly, these compounds can be administered orally.
    Type: Application
    Filed: January 10, 2003
    Publication date: October 9, 2003
    Inventor: Robert J. D'Amato
  • Patent number: 6610709
    Abstract: This invention relates to (2R,3S,4R,5R)-2-amino-5-methylpiperidine-3,4-diol or a (2S,3S,4R,5R)-2-N-substituted-2-amino-5-methylpiperidine-3,4-diol represented by the general formula (I): wherein R1 and R2 each are a hydrogen atom, or R1 is a hydrogen atom and R2 is a lower alkanoyl group or a lower &ohgr;-trihaloalkanoyl group, or R1 and R2 together denote phthaloyl group, and a pharmaceutically acceptable salt thereof. Said compound can be prepared from a (2S,3S,4R)-5-N-protected-2,3,4-O-tri-protected-5-aminopentane-1,2,3,4-tetraol by multi-steps of reactions.
    Type: Grant
    Filed: August 1, 2001
    Date of Patent: August 26, 2003
    Assignees: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai, Meiji Seika Kaisha, Ltd.
    Inventors: Yoshio Nishimura, Eiki Shitara, Tomio Takeuchi
  • Publication number: 20030130317
    Abstract: Methods for treating lipid storage diseases using compounds that inhibit glucosyltransferase enzymes are disclosed herein. The invention relates to the treatment of lipid storage disease with compounds that inhibit glucosyltransferase activity in the affected cells. It relates particularly to the use of 1,5-dideoxy-1,5-imino-D-glucitol and derivatives thereof.
    Type: Application
    Filed: September 17, 2002
    Publication date: July 10, 2003
    Inventors: Terry D. Butters, Frances M. Platt, Raymond A. Dwek
  • Publication number: 20030119874
    Abstract: Method for enhancing in a mammalian cell the activity of an enzyme associated with Gaucher Disease by administering a competitive inhibitor of glucocerebrosidase in an amount effective to enhance the activity of the enzyme. Preferred compounds for use in the method are imino sugars and related compounds. In particular, C8-12-alkyl derivatives of N-alkyl-deoxynojirimycin, isofagomine compounds, and calystegine compoiunds are effective to enhance glucocerebrosidase activity.
    Type: Application
    Filed: November 26, 2002
    Publication date: June 26, 2003
    Applicant: Mount Sinai School of Medicine
    Inventors: Jian-Qiang Fan, Satoshi Ishii, Naoki Asano, Robert J. Desnick
  • Publication number: 20030119789
    Abstract: Methods and compositions are described for treating and diagnosing autoimmune diseases, and in particular for treating and detecting rheumatoid arthritis. Treatment is described with a new class of anti-RA drug, namely compounds that inhibit proliferation and induce apoptosis.
    Type: Application
    Filed: October 31, 2002
    Publication date: June 26, 2003
    Applicant: The Regents of the University of Michigan
    Inventors: Joseph Holoshitz, James A. Shayman, Shi-Yu Tan
  • Publication number: 20030100532
    Abstract: Provided are methods and compositions for treating hepatitis virus infections in mammals, especially humans. The methods comprise (1) administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds in combination with nucleoside antiviral agents, nucleotide antiviral agents, mixtures thereof, or immunomodulating/immunostimulating agents, or (2) administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds in combination with nucleoside antiviral agents, nucleotide antiviral agents, or mixtures thereof, and immunomodulating/immunostimulating agents.
    Type: Application
    Filed: February 12, 1998
    Publication date: May 29, 2003
    Inventors: GARY S. JACOB, TIMOTHY M BLOCK, RAYMOND A DWEK
  • Publication number: 20030087934
    Abstract: The present invention relates to certain substituted polyketides of formula I, 1
    Type: Application
    Filed: August 5, 2002
    Publication date: May 8, 2003
    Inventors: Frederick R. Kinder, Kenneth W. Bair, Timothy M. Ramsey, Michael L. Sabio
  • Publication number: 20030069200
    Abstract: Treatments for brain cancer are provided, based on administration of inhibitors of glycophospholipids synthesis.
    Type: Application
    Filed: September 13, 2002
    Publication date: April 10, 2003
    Inventors: Frances Mary Platt, Thomas Neil Seyfried, Paul David Smith
  • Patent number: 6545021
    Abstract: N-Substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds of Formula I are effective in treatment of hepatitis infections, including hepatitis B and hepatitis C. In treating hepatitis infections, the compounds of Formula I may be used alone, or in combination with another antiviral agent selected from among nucleosides, nucleotides, immunomodulators, immunostimulats or various combinations of such other agents.
    Type: Grant
    Filed: February 14, 2000
    Date of Patent: April 8, 2003
    Assignee: G.D. Searle & Co.
    Inventors: Richard A. Mueller, Martin L. Bryant, Richard A. Partis
  • Patent number: 6495570
    Abstract: A novel combination drug therapy is disclosed for the treatment of a patient affected with Gaucher's disease or other such glycolipid storage diseases. The method comprises administering to said patient a therapeutically effective amount of both a N-alkyl derivative of deoxynojirimycin (DNJ) and a glucocerebrosidase enzyme to alleviate or inhibit the glycolipid storage disease. The alkyl group has from about two to about 20 carbon atoms and preferably is butyl, nonyl or decyl.
    Type: Grant
    Filed: May 17, 2001
    Date of Patent: December 17, 2002
    Assignee: G. D. Searle & Co.
    Inventors: Gary S. Jacob, Raymond A. Dwek
  • Patent number: 6476053
    Abstract: The invention provides the use of certain succinimide compounds in the treatment of mycobacterial diseases.
    Type: Grant
    Filed: July 22, 1999
    Date of Patent: November 5, 2002
    Assignee: AstraZeneca AB
    Inventors: Meenakshi Balganesh, Kantharaj Ethirajulu, Babita Singh Ganguly, Ramachandran Janakiraman, Parvinder Kaur, Rangarao Kajipalya, Santosh Nandan, Ramanujulu Pondi Murugappan, Narayanan Ramamurthy, Balasubramanian Venkataraman
  • Patent number: 6465487
    Abstract: Methods for inhibiting morphogenesis of host cell membrane-budding viruses and infections caused thereby using compounds that inhibit host cell glucosidase or glucosyltransferase enzymes. Methods for treating lipid storage diseases using compounds that inhibit glucosyl transferance enzymes.
    Type: Grant
    Filed: December 10, 1998
    Date of Patent: October 15, 2002
    Assignees: Synergy Pharmaceuticals, Inc., Thomas Jefferson University, The Chancellor, Masters and Scholars of the University of Oxford
    Inventors: Timothy M. Block, Raymond A. Dwek, Baruch S. Blumberg, Anand Mehta, Frances Platt, Terry D. Butters, Nicole Zitzmann
  • Publication number: 20020142985
    Abstract: A method for treating a glycolipid storage-related disorder, comprising administering a therapeutically effective amount of an inhibitor of glycolipid synthesis in combination with an agent capable of increasing the rate of glycolipid degradation or in combination with bone marrow transplantation. Inhibitors of glycolipid synthesis include N-butyldeoxynojirimycin (NB-DNJ), N-butyldeoxygalactonojirimycin (NB-DGJ) or N-nonyldeoxynojirimycin (NN-DNJ). Glycolipid storage-related disorders include Gaucher disease, Sandhoff's disease, Fabry's disease, Tay-Sach's disease, Niemann-Pick C storage disease, GM1 gangliosidosis, genetic disorders in which neuronal glycolipid accumulation contributes to disease pathology.
    Type: Application
    Filed: October 19, 2001
    Publication date: October 3, 2002
    Inventors: Raymond A. Dwek, Terence D. Butters
  • Patent number: 6432985
    Abstract: The invention relates to a compound of the formula its R,R-, S,S-enantiomers and racemic mixtures thereof and to their pharmaceutically acceptable acid addition salts. The compound of formula I and its R,R- and S,S-enantiomers may be used as medicaments for the treatment of diseases, wherein the therapeutic indications include acute forms of neurodegeneration caused by stroke or brain trauma; chronic forms of neurodegeneration such as Alzheimer's disease, Parkinson's disease, Huntington's disease or ALS (amyotrophic lateral sclerosis); neurodegeneration associated with bacterial or viral infections, and, diseases such as schizophrenia, anxiety, depression and chronic/acute pain.
    Type: Grant
    Filed: March 19, 2001
    Date of Patent: August 13, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Alanine, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Georg Jaeschke, Emmanuel Pinard, Rene Wyler
  • Publication number: 20020091117
    Abstract: The present invention relates to compounds of the formula 1
    Type: Application
    Filed: November 6, 2001
    Publication date: July 11, 2002
    Applicant: Pfizer Inc.
    Inventor: Harry Ralph Howard
  • Publication number: 20010044453
    Abstract: A novel combination drug therapy is disclosed for the treatment of a patient affected with Gaucher's disease or other such glycolipid storage diseases. The method comprises administering to said patient a therapeutically effective amount of both a N-alkyl derivative of deoxynojirimycin (DNJ) and a glucocerebrosidase enzyme to alleviate or inhibit the glycolipid storage disease. The alkyl group has from about two to about 20 carbon atoms and preferably is butyl, nonyl or decyl.
    Type: Application
    Filed: May 17, 2001
    Publication date: November 22, 2001
    Inventors: Gary S. Jacob, Raymond A. Dwek
  • Publication number: 20010014688
    Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.
    Type: Application
    Filed: November 13, 1998
    Publication date: August 16, 2001
    Inventors: THOMAS E. BARTA, DANIEL P. BECKER, TERRI L. BOEHM, GARY A. DECRESCENZO, CLARA I. WILLAMIL, JOSEPH J. MCDONALD, JOHN N. FRESKOS, DANIEL P. GETMAN, GUNNAR J. HANSON
  • Patent number: 6242466
    Abstract: Phenylamidines of the formula (I) wherein: R6 is a C5-12-alkyloxycarbonyl group, and R7 is a hydrogen atom, or a C1-8-alkyl, C4-7-cycloalkyl, phenyl-C1-4-alkyl, or R8—CO—OCHR9— group, wherein R8 is a C1-4-alkyl, C1-4-alkoxy, C3-7-cycloalkyl, or C4-7-cycloalkoxy group, and R9 is a hydrogen atom or a C1-4-alkyl group, or a tautomer or pharmaceutically acceptable salt thereof. These compounds inhibit cell aggregation and are useful for the treatment or prevention of thrombosis, inflammation, bone degradation, tumors and tumor metastasis.
    Type: Grant
    Filed: July 14, 1999
    Date of Patent: June 5, 2001
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Frank Himmelsbach, Brian Guth, Hans-Dieter Schubert
  • Patent number: 6232325
    Abstract: This invention is directed to benzamidine derivatives substituted by cyclic amino acid and cyclic hydroxy acid derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
    Type: Grant
    Filed: November 12, 1999
    Date of Patent: May 15, 2001
    Assignee: Berlex Laboratories, Inc.
    Inventors: Monica Kochanny, Michael M. Morrissey, Howard P. Ng
  • Patent number: 6225325
    Abstract: Methods and compositions for preventing, reducing, or reversing multidrug resistance (MDR) during cancer chemotherapy in patients undergoing treatment with therapeutically effective amounts of chemotherapeutic agents are provided. The methods comprise administering an anti-MDR effective amount of an N-substituted-1,5-dideoxy-1,5-imino-D-glucitol or galactitol iminosugar to a patient.
    Type: Grant
    Filed: November 10, 1998
    Date of Patent: May 1, 2001
    Assignee: G.D. Searle & Company
    Inventor: Gary S. Jacob
  • Patent number: 6191156
    Abstract: A method for treating patients having bladder dysfunction is described. The method involves the step of treating a patient with a renin-angiotensin system inhibitor. Preferably the inhibitor is an Angiotensin II antagonist, an ACE inhibitor, or a renin inhibitor. Compositions of a combination of an AT1 specific Angiotensin II antagonist and an Angiotensin II agonist are also described. The compositions are useful for treating bladder dysfunction.
    Type: Grant
    Filed: March 25, 1998
    Date of Patent: February 20, 2001
    Assignee: The Brigham and Women's Hospital, Inc.
    Inventors: Imre Kifor, Gordon Williams, Maryrose P. Sullivan
  • Patent number: 6110935
    Abstract: Compounds of the general structural formula ##STR1## are shown to have AMPA receptor enhancing properties. The compounds are useful for such therapeutic purposes as facilitating the learning of behaviors dependent upon AMPA receptors, and in treating conditions, such as memory impairment, in which AMPA receptors, or synapses utilizing these receptors, are reduced in numbers or efficiency. They may also be used to enhance excitatory synaptic activity in order to restore an imbalance between brain subregions, as in treatment of schizophrenia or schizophreniform behavior.
    Type: Grant
    Filed: February 13, 1997
    Date of Patent: August 29, 2000
    Assignee: The Regents of the University of California
    Inventors: Gary A. Rogers, Christopher M. Marrs
  • Patent number: 6080742
    Abstract: Substituted benzamides corresponding to the formula I ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 have the meanings given herein, and their use in pharmaceutical compositions. The compounds are particularly useful as immunomodulators.
    Type: Grant
    Filed: September 24, 1999
    Date of Patent: June 27, 2000
    Assignee: Gruenenthal GmbH
    Inventors: Tieno Germann, Stefanie Frosch, Oswald Zimmer
  • Patent number: 6048849
    Abstract: This invention provides for pharmaceutical formulations of compounds which are useful as protective agents when administered to patients also receiving antineoplastic drugs. The invention also includes methods of reducing the toxicity of various antineoplastic agents by administering an effective amount of the protective agent to a patient receiving one or more antineoplastic agents. The compounds useful as protective agents have either a sulfhydryl moiety or are reducible disulfides.
    Type: Grant
    Filed: January 6, 1999
    Date of Patent: April 11, 2000
    Assignee: BioNumerik Pharmaceuticals, Inc.
    Inventors: Frederick H. Hausheer, Thomas J. Dodd
  • Patent number: 6046214
    Abstract: Novel piperidine compounds are provided, and those compounds are useful in the treatment and/or prevention of diabetes, and especially non-insulin dependent diabetes (NIDDM or type 2 diabetes) including overnight or meal treatment and treatment or prevention of longterm complications, such as retinopathy, neuropathy, nephropathy, and micro- and macroangiopathy; treatment of hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis or myocardial ischemia.
    Type: Grant
    Filed: November 4, 1998
    Date of Patent: April 4, 2000
    Assignee: Novo Nordisk A/S
    Inventors: Marit Kristiansen, Palle Jakobsen, Jane Marie Lundbeck, Birgitte S.o slashed.kilde, Karsten Lundgren
  • Patent number: 6020327
    Abstract: A method for treating hair loss is disclosed by topically adminstering an aromatase inhibitor to a mammal, including humans, on the area to be treated.
    Type: Grant
    Filed: March 14, 1997
    Date of Patent: February 1, 2000
    Assignees: The Central Sheffield University Hospitals NHS Trust, Bio-Scientific Ltd
    Inventor: Andrew Guy Messenger
  • Patent number: 6008234
    Abstract: This invention is directed to benzamidine derivatives substituted by cyclic amino acid and cyclic hydroxy acid derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
    Type: Grant
    Filed: August 27, 1997
    Date of Patent: December 28, 1999
    Assignee: Berlex Laboratories, Inc.
    Inventors: Monica Kochanny, Michael M. Morrissey, Howard P. Ng
  • Patent number: 5981539
    Abstract: The present invention discloses compounds of the formula ##STR1## any of its enantiomers or any mixture thereof, or a pharmaceutically-acceptable addition salt thereof, wherein X, Ar, R, R.sup.1, R.sup.2, n are as defined herein.
    Type: Grant
    Filed: May 29, 1998
    Date of Patent: November 9, 1999
    Assignee: Neurosearch A/S
    Inventors: Oskar Axelsson, Dan Peters, Nielsen Elsebet stergaard, Palle Christophersen
  • Patent number: 5958952
    Abstract: The present invention relates to phenyl amidines of general formula (I), ##STR1## in which R.sup.1 to R.sup.5 are as defined in claim 1, their tautomers, their stereoisomers and their mixtures and their salts, especially their physiologically acceptable salts with inorganic or organic acids or bases also having valuable pharmacological properties, preferably aggregation-limiting effects, producing them.
    Type: Grant
    Filed: December 17, 1997
    Date of Patent: September 28, 1999
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Frank Himmelsbach, Volkhard Austel, Gunther Linz, Helmut Pieper, Brian Guth, Johannes Weisenberger
  • Patent number: 5952354
    Abstract: Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in the inhibition of the esterification of cholesterol and are therefore implicated in the inhibition of absorption of cholesterol and thus can lower serum cholesterol levels. Compounds of the formula: ##STR1## where Z is ##STR2## or --Ar.sup.1 --(CR.dbd.CR).sub.1-3 --Ar.sup.2, --AR.sup.1 --NR.sup.7 --AR.sup.2 and A is a linking group inhibit the enzymes CEH and/or ACAT (in vitro) and inhibit absorption of cholesterol.
    Type: Grant
    Filed: July 21, 1993
    Date of Patent: September 14, 1999
    Assignee: American Home Products Corporation
    Inventors: Thomas Joseph Commons, Donald Peter Strike, Christa Marie LaClair
  • Patent number: 5952376
    Abstract: Triene-containing compounds which mimic the chemical and/or biological activity of the spongistatins are provided, as are methods and intermediates useful in their preparation.
    Type: Grant
    Filed: November 7, 1997
    Date of Patent: September 14, 1999
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Amos B. Smith, III, Qiyan Lin
  • Patent number: 5844102
    Abstract: A compound of the formula ##STR1## wherein n, m, and p, which may be the same or different, are a number between 0 and 5; q is a number between 0 and 10; R.sub.1, R.sub.2 R.sub.3 R.sub.4 and R.sub.5, which may be the same or different, are a hydrogen, a hydroxyl, a halogen, a hydrocarbon or an O-hydrocarbon group having between 1 and 6 carbons which is aliphatic, alicyclic or aromatic, or a glycosyl group; and R.sub.4 is a glycosyl group, is disclosed. Nitrogen oxides of such compounds are also included. These novel compounds have been found to be potent glycohydrolase inhibitors. Processes for preparing these novel compounds and methods for their use in the treatment of diabetes mellitus are also provided.
    Type: Grant
    Filed: September 7, 1994
    Date of Patent: December 1, 1998
    Assignee: University of Maryland Baltimore County
    Inventors: Michael R. Sierks, Mikael Bols, Troels Skrydstrup
  • Patent number: 5776951
    Abstract: The present invention is concerned with diaryl compounds of formula (l) and their use in medical therapy, particularly in the prophylaxis or treatment of a clinical condition for which an ACAT inhibitor is indicated, such as hyperlipidaema or atherosclerosis. The invention also relates to pharmaceutical compositions and processes for the preparation of compounds according to the invention.
    Type: Grant
    Filed: April 11, 1996
    Date of Patent: July 7, 1998
    Assignee: Glaxo Wellcome Inc.
    Inventors: Richard James Arrowsmith, John Gordon Dann, Karl Witold Franzmann, Simon Teanby Hodgson, Peter John Wates
  • Patent number: 5693630
    Abstract: Compounds of the general formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Z is a saturated or unsaturated 3 to 6 carbon chain,m is 2 or 3,R.sub.1 is a hydrogen atom, or a straight or branched C.sub.1-4 alkyl group,R.sub.2, R.sub.3 and R.sub.13 are situated in the ortho, meta, or para position of the phenyl ring and are the same or different and selected from the following groups: H, OH, OR.sub.14, halogen, CO.sub.2 R.sub.9, CN, CF.sub.3, NO.sub.2, NH.sub.2, COCH.sub.3,OSO.sub.2 CF.sub.3,OSO.sub.2 CH.sub.3,CONR.sub.10 R.sub.11, OCOR.sub.12, whereinR.sub.9, R.sub.12 and R.sub.14 is a straight or branched C.sub.1-4 alkyl group,R.sub.10 and R.sub.11 are the same or different and represents hydrogen or a straight or branched C.sub.1-6 alkyl group,R is 1) ##STR2## processes for their preparation, pharmaceutical preparations containing them and the use of the compounds in the treatment psychiatric disorders.
    Type: Grant
    Filed: October 26, 1994
    Date of Patent: December 2, 1997
    Assignee: Astra Aktiebolag
    Inventors: Stefan Bengtsson, Sven Hellberg, Nina Mohell, Lian Zhang, Gerd Hallnemo, David Jackson, Bengt Ulff
  • Patent number: 5635537
    Abstract: A compound of the formula ##STR1## Z is hydrogen or halogen, Q is COR.sup.1 or 5-or 6-membered aryl which may contain 1 or 2 heteroatoms selected from N, 0 or S and may be substituted or fused wherein R is hydrogen or C.sub.1 -methyl (cis-configuration), R.sup.1 is C.sub.1 -C.sub.6 alkyl or an aromatic ring which may contain heteroatoms selected from O and S and may be substituted or fused to an optionally substituted benzene ring, R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sup.3 may be different groups defined in claim 1, and enantiomers/salts thereof, processes for preparation of said compounds, pharmaceutical preparations containing said compounds, use of and method of treatment of disorders in CNS by using said compounds.
    Type: Grant
    Filed: March 18, 1993
    Date of Patent: June 3, 1997
    Assignee: Astra Aktiebolag
    Inventors: Nils-Erik Anden, Berit C. E. Backlund Hook, Anna L. Bjork, Uli A. Hacksell, Sven-Erik Hillver, Ye Liu, Eva C. Mellin, Eva M. Persson, Karl J. Vallg.ang.rda, Hong Yu
  • Patent number: 5622972
    Abstract: A method is provided for treating a mammal infected with respiratory syncytial virus (RSV) comprising administering to the mammal an RSV inhibitory effective amount of a compound or its pharmaceutically acceptable salt of the formula ##STR1## wherein R.sup.1 is alkyl, aralkyl, aroyl or acyl and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are H or acyl.
    Type: Grant
    Filed: January 26, 1996
    Date of Patent: April 22, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Martin L. Bryant, Francis J. Koszyk, Richard A. Mueller, Richard A. Partis
  • Patent number: 5620993
    Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral fining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: April 15, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Michael A. Patane, Mark G. Bock, Roger M. Friedinger
  • Patent number: 5620989
    Abstract: The present invention is directed to compounds of the formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.
    Type: Grant
    Filed: April 13, 1995
    Date of Patent: April 15, 1997
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Timothy Harrison, Angus M. MacLeod, Graeme I. Stevenson, Brian J. Williams
  • Patent number: 5616593
    Abstract: A pharmaceutical composition having increased bioavailability characterized by piperine of the formula ##STR1## and a drug for treating a disease or condition of the human cardiovascular system, central nervous system, gastrointestinal tract, respiratory tract, endocrine system, genito urinary tract or haemopoietic system.
    Type: Grant
    Filed: October 18, 1994
    Date of Patent: April 1, 1997
    Assignee: Cadila Laboratories Limited
    Inventors: Ramanbhai B. Patel, Indravadan A. Modi
  • Patent number: 5607931
    Abstract: Amides of the formula ##STR1## wherein: R.sup.1 is A and R.sup.2 is B; R.sup.1 is B and R.sup.2 is A; or R.sup.1 and R.sup.2 are independently selected from the group B;A is phenyl, substituted phenyl, heteroaryl, or substituted heteroaryl;B is cycloalkyl, substituted cycloalkyl, heterocycloalkyl, or substituted heterocycloalkyl;R.sup.3 is an alkyl chain of 1 to 25 carbon atoms, branched or straight; an alkenyl chain of 2 to 25 carbon atoms, branched or straight; a substituted alkyl chain; a substituted alkenyl chain; an interrupted alkyl chain; an interrupted alkenyl chain; a substituted interrupted alkyl chain; or a substituted interrupted alkenyl chain;R.sup.4 is hydrogen, lower alkyl, phenyl, Q-substituted phenyl, heteroaryl or Q-substituted heteroaryl;R.sup.6 and R.sup.7 are both H, or R.sup.6 and R.sup.7 together represent .dbd.
    Type: Grant
    Filed: March 20, 1995
    Date of Patent: March 4, 1997
    Assignee: Schering Corporation
    Inventor: Sundeep Dugar
  • Patent number: 5605917
    Abstract: A method is provided for treating dysmenorrhea (menstrual cramps) employing an interphenylene 7-oxabicycloheptyl substituted heterocyclic amide prostaglandin analog thromboxane A.sub.2 receptor antagonist such as ifetroban, alone or in combination with a non-steroidal anti-inflammatory drug (NSAID).
    Type: Grant
    Filed: December 22, 1994
    Date of Patent: February 25, 1997
    Assignee: Bristol-Myers Squibb Company
    Inventor: Martin L. Ogletree
  • Patent number: 5550107
    Abstract: A method of treatment of breast and endometrial cancer in susceptible warm-blooded animals may include inhibition of ovarian hormonal secretion by surgical (ovariectomy) or chemical (use of an LHRH agonist, e.g. [D-Trp.sup.6, des-Gly-NH.sub.2.sup.10 ]LHRH ethylamide or antagonist) as part of a combination therapy comprising administering an antiestrogen together with at least one compound selected from the group consisting of an androgen, a progestin, at least one inhibitor of sex steroid formation, especially 17.beta.-hydroxysteroid dehydrogenase and aromatase activity, at least one inhibitor of prolactin secretion, one inhibitor of growth hormone secretion and one inhibitor of ACTH secretion. Pharmaceutical compositions useful for such treatment and pharmaceutical kits containing such composition are disclosed.
    Type: Grant
    Filed: November 4, 1991
    Date of Patent: August 27, 1996
    Assignee: Endorecherche Inc.
    Inventor: Fernand Labrie
  • Patent number: 5498779
    Abstract: This invention relates to novel polyfluorinated alkyl derivatives of certain tripeptides, to the methods for their preparation, the intermediates therefore, to their use in inhibiting thrombin and lung tryptase and in their end-use application as anti-coagulants useful in treating thrombophlebitis and coronary thrombosis and in the treatment of asthma.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: March 12, 1996
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Bernhard Neises, Axel Ganzhorn, Celine Tarnus, Robert J. Broersma, Jr.
  • Patent number: 5489600
    Abstract: The present invention relates to piperidyl amides which are useful as inhibitors of cholesterol biosynthesis and as agents which lower total serum cholesterol in patients in need thereof.
    Type: Grant
    Filed: May 25, 1994
    Date of Patent: February 6, 1996
    Inventors: Marion W. Wannamaker, William A. VanSickle, William R. Moore
  • Patent number: 5476859
    Abstract: A method of inhibiting lentivirus is disclosed which comprises mammalian host susceptible to said lentivirus with a virally inhibitory effective amount of an O-acylated derivative of 1,5-dideoxy-1,5-imino-D-glucitol and their N-alkyl, N-acyl and N-aroyl derivatives in which from one to four of the free hydroxyl groups are O-acylated with carboxylic alkanoyl radicals selected from the group consisting of .omega.,.omega.,.omega.-trifluoroalkanoyl having from three to eight carbon atoms, carboxylic cycloalkanoyl groups having from four to eight carbon atoms and carboxylic acyclic alkanoyl groups having from two to ten carbon atoms, wherein the N-aroyl groups contain from 7 to 14 carbon atoms, the N-acyl groups contain from 4 to 8 carbon atoms and the N-alkyl groups contain from 1 to 14 carbon atoms.
    Type: Grant
    Filed: January 20, 1995
    Date of Patent: December 19, 1995
    Inventors: Richard A. Partis, Francis J. Koszyk, Richard A. Mueller
  • Patent number: 5466691
    Abstract: Thiophene compounds of the formula ##STR1## wherein each symbol is as defined in the specification, their pharmaceutically acceptable salts, pharmaceutical compositions containing said compound and additives for pharmaceuticals, and antipsychotics containing said compound as an active ingredient.The compound of the present invention has pharmacological actions required of antipsychotic, such as motility suppressing action, anti-apomorphine action, mothamphetamine antagonistic action, tetrabenazine-induced blepharoptosis enhancing action, and the like. The compound of the present invention is useful as an antipsychotic having less extrapyramidal side-effects or a non-benzodiazepine type antianxiety agent.
    Type: Grant
    Filed: March 30, 1993
    Date of Patent: November 14, 1995
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Tohru Nakao, Yuji Ono, Hiroshi Tanaka, Minoru Obata, Yasuto Morimoto
  • Patent number: 5455276
    Abstract: Pharmaceutical compositions for treating psychiatric disorders are provided. The compositions include 2-phenylethylamine ("PEA") and at least one inhibitor of monoamine oxidase B. Methods for the treatment of psychiatric disorders, including depression, using the disclosed pharmaceutical compositions are also provided.
    Type: Grant
    Filed: May 20, 1993
    Date of Patent: October 3, 1995
    Inventor: Hector C. Sabelli
  • Patent number: 5451564
    Abstract: A composition comprising (a) a metal salt or complex with an organic compound of the general formula ##STR1## and (b) an oxy-phosphorus compound where W may be --SH or an optionally substituted hydrocarbyl group, Q is --OH, hydrogen or optionally substituted hydrocarbyl and Z is hydrogen or optionally substituted hydrocarbyl and Q and Z or Z and W may complete a ring. The compounds are typically metal complexes of thiohydroxamic acids or dithiocarbamates. The metal is typically zinc. The compositions exhibit improved aqueous solubility compared with the metal complexes alone, and can be used as industrial biocides, especially fungicides and particularly in paint films and latices.
    Type: Grant
    Filed: March 29, 1994
    Date of Patent: September 19, 1995
    Assignee: Zeneca Limited
    Inventors: Peter W. Austin, Fraser F. Morpeth
  • Patent number: 5424319
    Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a piperidinyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.
    Type: Grant
    Filed: December 16, 1993
    Date of Patent: June 13, 1995
    Assignee: G.D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5411970
    Abstract: A method of inhibiting lentivirus is disclosed which comprises mammalian host susceptible to said lentivirus with a virally inhibitory effective amount of an O-acylated derivative of 1,5-dideoxy-1,5-imino-D-glucitol and their N-alkyl, N-acyl and N-aroyl derivatives in which from one to four of the free hydroxyl groups are O-acylated with carboxylic alkanoyl radicals selected from the group consisting of .omega.,.omega.,.omega.-trifluoroalkanoyl having from three to eight carbon atoms, carboxylic cycloalkanoyl groups having from four to eight carbon atoms and carboxylic acyclic alkanoyl groups having from two to ten carbon atoms, wherein the N-aroyl groups contain from 7 to 14 carbon atoms, the N-acyl groups contain from 4 to 8 carbon atoms and the N-alkyl groups contain from 1 to 14 carbon atoms.
    Type: Grant
    Filed: December 21, 1993
    Date of Patent: May 2, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Partis, Francis J. Koszyk, Richard A. Mueller