Chalcogens Bonded Directly To At Least Two Ring Carbons Of The Six-membered Hetero Ring Patents (Class 514/348)
  • Patent number: 6503948
    Abstract: A method for treating an organ donor prior to harvesting organ to reduce graft rejection in a recipient. An amount effective to reduce graft rejection of at least one compound selected from the group consisting of compounds having formulas I, II, III, IV, V, VI, and VII is administered to the organ donor: wherein Y is X is F or Cl; and the remaining groups are as defined in the specification.
    Type: Grant
    Filed: April 17, 2002
    Date of Patent: January 7, 2003
    Assignee: Southern Research Institute
    Inventors: Herbert M. Blatter, Donald R. Kahn, James R. Piper, John A. Secrist, III, Robert F. Struck, Carroll Temple
  • Patent number: 6503932
    Abstract: Fungicidal mixtures, comprising A) an amide compound of the formula I in which R1, R2 are identical or different and are halogen, nitro, cyano, C1-C8-alkyl, C2-C8-alkenyl, C2-C8-alkynyl, C1-C8-haloalkyl, C2-C8-haloalkenyl, C2-C8-haloalkynyl, C1-C8-alkoxy, C1-C8-haloalkoxy, C1-C8-haloalkylthio, C1-C8-alkylsulfinyl or C1-C8-alkylsulfonyl; x is 1, 2, 3 or 4; y is 1, 2, 3, 4 or 5; and B) the amino compound of the formula II in a synergistically effective amount, methods for controlling harmful fungi using mixtures of the compounds I and II and the use of the compounds I and II for preparing such mixtures are described.
    Type: Grant
    Filed: December 12, 2001
    Date of Patent: January 7, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Karl Eicken, Eberhard Ammermann, Reinhard Stierl, Gisela Lorenz, Siegfried Strathmann, Maria Scherer, Klaus Schelberger, Manfred Hampel
  • Patent number: 6495580
    Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infections.
    Type: Grant
    Filed: October 18, 1999
    Date of Patent: December 17, 2002
    Assignee: ViroPharma Incorporated
    Inventors: Theodore J. Nitz, Daniel C. Pevear
  • Patent number: 6495571
    Abstract: New pyridine compounds are provided along with their method of preparation. The compounds are useful as intermediates in preparing new anticancer agents. A few of the pyridine compounds are also useful for treating cancer.
    Type: Grant
    Filed: March 25, 2002
    Date of Patent: December 17, 2002
    Assignee: Southern Research Institute
    Inventors: Robert F. Struck, Herbert M. Blatter, Anita Tiwari
  • Patent number: 6492405
    Abstract: The present invention provides a compound containing at least one sulfhydryl group and at least one NO donor group, wherein said compound is a) a compound containing one or more sulfhydryl groups linked to at least one aromatic ring or a heteroaromatic ring with a nitrogen in the ring structure, which ring is substituted by one or more substituents bearing a terminal —ONO2 group; b) a 5-membered ring heterocyclic compound containing a sulfur atom and a nitrogen atom, which ring is substituted by one or more substituents bearing a terminal —ONO2 group; c) a 5-membered ring compound containing two conjugate S-atoms, which ring is linked to one or more substituents bearing a terminal —ONO2 group; or d) a compound containing an acyclic —S—S group, linked to at least one aromatic ring or a heteroaromatic ring with a nitrogen in the ring structure, which ring is substituted by one or more substituents bearing a terminal —ONO2 group.
    Type: Grant
    Filed: January 9, 2002
    Date of Patent: December 10, 2002
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem
    Inventor: Abdullah Haj-Yehia
  • Patent number: 6489348
    Abstract: Fungicidal mixtures comprise as active components a) an amide compound of the formula I A—CO—NR1R2  I  in which A, R1 and R2 are as defined in the description, and b) compounds of the formula II, their N-oxide or one of their salts  where the substituents R12 to R18 are as defined in the description, and/or c) compounds of the formula III  where the substituents X1 to X5 and R19 to R22 are as defined in the description, in a synergistically effective amount.
    Type: Grant
    Filed: September 24, 2001
    Date of Patent: December 3, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Schelberger, Maria Scherer, Karl Eicken, Manfred Hampel, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
  • Patent number: 6472412
    Abstract: This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.
    Type: Grant
    Filed: January 26, 1996
    Date of Patent: October 29, 2002
    Assignee: Aventis Pharma Limited
    Inventors: Garry Fenton, Tahir Nadeem Majid, Malcolm Norman Palfreyman
  • Patent number: 6436969
    Abstract: The present invention provides improved dialysis compositions and methods for dialysis comprising utilizing the disclosed AGE inhibitors, together with methods to reduce dialysis-related complications and disorders.
    Type: Grant
    Filed: April 6, 2000
    Date of Patent: August 20, 2002
    Assignee: Kansas University Medical Center Research Institute Inc.
    Inventors: Raja Gabriel Khalifah, Billy G. Hudson
  • Patent number: 6436934
    Abstract: Fungicidal mixtures comprise as active components a) an amide compound of the formula I A—CO—NR1R2  I in which A, R1 and R2 are as defined in the description, and b) dimethomorph or flumetover, and/or c) a valinamide of the formula III  in which R13 is C3-C4-alkyl and R14 is naphthyl or phenyl, where the phenyl radical is substituted in the 4-position by a halogen atom, a C1-C4-alkyl or C1-C4-alkoxy group, and/or d) benalaxyl, ofurace, metalaxyl, furalaxyl or oxydixyl, and/or e) 1-(2-cyano-2-methoxyiminoacetyl)-3-ethylurea in a synergistically effective amount.
    Type: Grant
    Filed: June 19, 2000
    Date of Patent: August 20, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Schelberger, Maria Scherer, Karl Eicken, Manfred Hampel, Eberhard Ammermann, Gisela Lorenz, Siegfreid Strathmann
  • Patent number: 6432989
    Abstract: A corticotropin releasing factor (CRF) antagonist is administered to treat disorders that can be treated by altering circadian rhythm.
    Type: Grant
    Filed: June 5, 2000
    Date of Patent: August 13, 2002
    Assignee: Pfizer Inc
    Inventor: Yuhpyng L. Chen
  • Patent number: 6432990
    Abstract: The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds with polyether substituents on the pyridine ring, their use as fungicidal compounds, and their use in fungicidal compositions comprising at least one of the 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds as the active ingredient.
    Type: Grant
    Filed: January 30, 2002
    Date of Patent: August 13, 2002
    Assignee: Dow AgroSciences LLC
    Inventors: Emily J. Canada, Carl P. Denny, Christopher S. Galka, Neil V. Kirby, Marc McKennon, Mary E. Pieczko, Rebecca L. Rezac, Brent J. Rieder, John K. Swayze, Chrislyn M. Carson, David D. Johnson, Gregory M. Kemmitt
  • Publication number: 20020068758
    Abstract: A novel 3-hydroxypyridinone compound of formula I is provided 1
    Type: Application
    Filed: September 4, 2001
    Publication date: June 6, 2002
    Applicant: BTG International Limited.
    Inventors: Robert Charles Hider, Gary Stuart Tilbrook, Zudong Liu
  • Patent number: 6391893
    Abstract: New pyridine compounds are provided along with their method of preparation. The compounds are useful as intermediates in preparing new anticancer agents. A few of the pyridine compounds are also useful for treating cancer.
    Type: Grant
    Filed: January 21, 2000
    Date of Patent: May 21, 2002
    Assignee: Southern Research Institute
    Inventors: Robert F. Struck, Herbert M. Blatter, Anita Tiwari
  • Patent number: 6376518
    Abstract: Acyl derivatives of 4-demethylpenclomedine are provided along with pharmaceutical compositions containing them and use for treating cancer. A method for preparing the derivatives is also provided.
    Type: Grant
    Filed: January 21, 2000
    Date of Patent: April 23, 2002
    Assignee: Southern Research Institute
    Inventor: Robert F. Struck
  • Patent number: 6372748
    Abstract: Fungicidal mixtures comprise as active components a) an amide compound of the formula I A—CO—NR1R2  I  in which A is an aryl group or an aromatic or non-aromatic, 5- or 6-membered heterocycle which has from 1 to 3 hetero atoms selected from O, N and S; where the aryl group or the heterocycle may or may not have 1, 2 or 3 substituents which are selected, independently of one another, from alkyl, halogen, CHF2, CF3, alkoxy, haloalkoxy, alkylthio, alkylsulfynyl and alkylsulfonyl; R1 is a hydrogen atom; R2 is a phenyl or cycloalkyl group which may or may not have 1, 2 or 3 substituents which are selected, independently of one another, from alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, cycloalkyl, cycloalkenyl, cycloalkyloxy, cycloalkenyloxy, phenyl and halogen, where the aliphatic and cycloaliphatic radicals may be partially or fully halogenated and/or the cycloaliphatic radicals may be substituted by from 1 to 3 alkyl groups and where the phenyl group may have from 1
    Type: Grant
    Filed: June 13, 2000
    Date of Patent: April 16, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Schelberger, Maria Scherer, Karl Eicken, Manfred Hampel, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
  • Patent number: 6369083
    Abstract: The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl) phenyl acetamide compounds with polyether substituents on the pyridine ring, their use as fungicidal compounds, and their use in fungicidal compositions comprising at least one of the 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds as the active ingredient.
    Type: Grant
    Filed: September 16, 1999
    Date of Patent: April 9, 2002
    Assignee: Dow AgroSciences LLC
    Inventors: Emily J. Canada, Carl P. Denny, Christopher S. Galka, Neil V. Kirby, Marc McKennon, Mary E. Pieczko, Rebecca L. Rezac, Brent J. Rieder, John K. Swayze, Chrislyn M. Carson, David D. Johnson, Gregory M. Kemmitt
  • Patent number: 6335353
    Abstract: A novel 3-hydroxypyridin-4-one compound of formula I is provided wherein R is hydrogen or a group that is removed by metabolism in vivo to provide the free hydroxy compound, R1 is an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by a hydroxy group or a carboxylic acid ester, sulpho acid ester or a C1-6 alkoxy, C6-aryloxy or C7-10aralkoxy ether thereof, R3 is selected from hydrogen and C1-6alkyl; and R4 is selected from hydrogen, C1-6alkyl and a group as described for R2; characterised in that R2 is selected from groups —CONH—R5  (i) —CH2NHCO—R5  (ii) —SO2NH—R5  (iii) —CH2NHSO2—R5  (iv) —CR6R6OR7  (v) —CONHCOR5  (viii)  wherein R5 is selected from hydrogen and optionally hydroxy, alkoxy, or aralkoxy substituted C1-13 alkyl, aryl and C71-13 aralkyl, R6 is independently selected from hydrogen, C1-13 alkyl, aryl and C7-13 aralkyl,
    Type: Grant
    Filed: November 10, 1999
    Date of Patent: January 1, 2002
    Assignee: BTG International Limited
    Inventors: Robert Charles Hider, Gary Stuart Tilbrook, Zudong Liu
  • Patent number: 6300346
    Abstract: Indenyl hydroxamic acids, (hydroxy) ureas and urethanes are useful in the treatment of precancerous lesions and neoplasms.
    Type: Grant
    Filed: March 7, 2000
    Date of Patent: October 9, 2001
    Assignee: Cell Pathways, Inc.
    Inventors: Gerhard Sperl, Paul Gross, Klaus Brendel, Rifat Pamukcu, Gary A. Piazza
  • Patent number: 6235761
    Abstract: Substantially pure 3,5-dichloro-2-nethoxy-4-hydroxy-6-(trichloromethyl)pyridine or 4-demethylpenclomedine (formula I), acid addition salts thereof, pharmaceutical compositions containing the aforesaid compound, and a method of using the compound in the treatment of cancer in a mammal are disclosed.
    Type: Grant
    Filed: February 22, 1999
    Date of Patent: May 22, 2001
    Inventors: Neil Hartman, Robert F. Struck, Seamus O'Reilly, John M. Strong, Eric K. Rowinsky, Jerry M. Collins
  • Patent number: 6221886
    Abstract: This invention is directed to monocyclic N-heterocyclics which are substituted by acyclic or cyclic thio 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: January 11, 2000
    Date of Patent: April 24, 2001
    Assignee: Berlex Laboratories, Inc.
    Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
  • Patent number: 6200996
    Abstract: Compounds of the formula: are useful in treating disease conditions mediated by TNF-&agr; such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: March 13, 2001
    Assignee: American Cyanamid Company
    Inventors: Jeremy I. Levin, James M. Chen, Frances C. Nelson
  • Patent number: 6187924
    Abstract: Compounds of formula (I) are useful as therapeutic agents, by virtue of having MMP and TNF inhibitory activity.
    Type: Grant
    Filed: November 12, 1998
    Date of Patent: February 13, 2001
    Assignee: Darwin Discovery, Ltd.
    Inventors: Andrew Douglas Baxter, David Alan Owen, John Gary Montana, Robert John Watson
  • Patent number: 6162815
    Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds having the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## which are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders are provided. In particular, based on their RXR-agonist activity, these compounds may be used to treat noninsulin-dependent diabetes mellitus (NIDDM) and obesity.
    Type: Grant
    Filed: September 10, 1998
    Date of Patent: December 19, 2000
    Assignee: Centre International de Recherches Dermatologiques Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 6150382
    Abstract: This invention is directed to monocyclic N-heterocyclics which are substituted by acyclic or cyclic thio 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: May 21, 1999
    Date of Patent: November 21, 2000
    Assignee: Berlex Laboratories, Inc.
    Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
  • Patent number: 6114363
    Abstract: Pyridyl phenyl and pyridyl benzyl ethers of the formula I ##STR1## and their salts and N-oxides where the substituent and indices have the following meanings:Q is C(CO.sub.2 CH.sub.3).dbd.CHCl.sub.3, C(CO.sub.2 CH.sub.3).dbd.CHOCH.sub.3, C(CONH.sub.2).dbd.NOCH.sub.3, C(CO.sub.2 CH.sub.3).dbd.NOCH.sub.3, C(CONHCH.sub.3).dbd.NOCH.sub.3 or N(OCH.sub.3)--CO.sub.2 CH.sub.3 ;n is 0 or 1;R.sup.1 is hydrogen or an organic radical linked via a carbon atom;R.sup.2 is hydrogen, cyano, halogen or an organic radical linked via a carbon, oxygen, sulfur or nitrogen atom;R.sup.3 is hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.2 -haloalkyl;x is 0, 1 or 2;R.sup.4 is cyano, nitro, halogen or an organic radical linked via a carbon, oxygen, sulfur or nitrogen atom;y is 0, 1, 2 or 3;R.sup.5 is cyano, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl or C.sub.1 -C.sub.4 -alkoxy,processes and intermediates for their preparation and their use.
    Type: Grant
    Filed: August 4, 1998
    Date of Patent: September 5, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Oberdorf, Wassilios Grammenos, Hubert Sauter, Thomas Grote, Bernd Muller, Reinhard Kirstgen, Ruth Muller, Herbert Bayer, Arne Ptock, Michael Rack, Albrecht Harreus, Franz Rohl, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann, Volker Harries
  • Patent number: 6103732
    Abstract: Carboxylic acid derivatives of the formula I ##STR1## where the radicals have the meanings stated in the description, and the preparation of these agreements [sic] and their use as drugs are described.
    Type: Grant
    Filed: October 8, 1998
    Date of Patent: August 15, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Wilhelm Amberg, Andreas Kling, Dagmar Klinge, Hartmut Riechers, Ernst Baumann, Liliane Unger, Manfred Raschack, Stefan Hergenroder, Sabine Schult
  • Patent number: 6080766
    Abstract: The present invention relates to a method of treating a patient with a fibrotic or fibroproliferative disorder and a method of suppressing formation of collagen and collagen-like substances or biosynthesis of procollagen in living systems by administering to a patient or living system, respectively, an effective amount of a compound of Formulae (I) or (II) and derivatives thereof: ##STR1## R.sub.1, R.sub.2, R.sub.3, and R.sub.4 each individually represent a hydrogen, an alkyl, alkenyl, or alkoxy group containing 1 to about 8 carbon atoms, an aryl, aralkyl, or cycloalkyl group containing about 5 to 12 carbon atoms, or a carboalkoxy or carbamyl group containing up to 8 carbon atoms, or a peptide or peptidomimetic moiety containing 10 to about 30 carbon atoms.
    Type: Grant
    Filed: December 16, 1997
    Date of Patent: June 27, 2000
    Assignee: Cornell Research Foundation, Inc.
    Inventors: Hartmut M. Hanauske-Abel, Timothy A. McCaffrey, Robert Walter Grady
  • Patent number: 6075023
    Abstract: Fish mycoses and single-cell ectoparasites on fish are controlled using an active compound suitable for inhibiting the mitochondrial respiratory chain at the stage of the b/c.sub.1 complex.
    Type: Grant
    Filed: February 17, 1998
    Date of Patent: June 13, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerhard Peter Dohmen, Christoph Kunast, Reinhart Munk, Gerhard Rothhaas
  • Patent number: 6066642
    Abstract: The present invention provides certain novel compounds, compositions, and a method of treating a mammal by blocking its adenosine receptors comprising administering at least one compound of the present invention. Examples of the present inventive compounds include certain flavonoids of formulae (I) and (II), wherein R.sub.1 to R.sub.4 are as defined in the description, and M is --CH(OH)--CH(R.sub.2)-- or --C(OH).dbd.C(R.sub.2)-- and R.sub.1, R.sub.2 are as defined in the description; or dihydropyridines of formula (III), wherein R.sub.2 to R.sub.6 are as defined in the description; or pyridines of formula (IV), wherein R.sub.2 to R.sub.6 are as defined in the description, or triazoloquinazolines of formula (V), wherein R.sub.1 and R.sub.2 are as defined in the description; and their derivatives, or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: December 7, 1998
    Date of Patent: May 23, 2000
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Kenneth A. Jacobson, Ji-Long Jiang, Yong-Chul Kim, Yishai Karton, Albert M. Van Rhee
  • Patent number: 6057342
    Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.
    Type: Grant
    Filed: July 7, 1997
    Date of Patent: May 2, 2000
    Assignee: Dupont Pharmaceutical Co.
    Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
  • Patent number: 6046219
    Abstract: The present invention relates to a method of treating conditions mediated by collagen formation together with cell proliferation by administering to a patient or living system an effective amount of a compound of Formulae (I) or (II) and derivatives thereof: ##STR1## R.sub.1, R.sub.2, R.sub.3, and R.sub.4 each individually represent a hydrogen, an alkyl, alkenyl, or alkoxy group containing 1 to about 8 carbon atoms, an aryl, aralkyl, or cycloalkyl group containing about 5 to 12 carbon atoms, or a carboalkoxy or carbamyl group containing up to 8 carbon atoms, or a peptide or peptidomimetic moiety containing 10 to about 30 carbon atoms.
    Type: Grant
    Filed: December 16, 1997
    Date of Patent: April 4, 2000
    Assignee: Cornell Research Foundation, Inc.
    Inventors: Hartmut M. Hanauske-Abel, Timothy A. McCaffrey, Robert W. Grady
  • Patent number: 6046221
    Abstract: Novel aryl amides are inhibitors of tumor necrosis factor .alpha. and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is N-benzoyl-3-amino-3-(3',4'-dimethoxyphenyl)propanamide.
    Type: Grant
    Filed: August 25, 1998
    Date of Patent: April 4, 2000
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Mary Shire, David I. Stirling
  • Patent number: 6046218
    Abstract: Described is a pyridine derivative represented by the following formula (1): ##STR1## wherein R.sup.1 and R.sup.2 individually represent H, an alkyl group, a cycloalkyl group, a hydroxyalkyl group, an alkoxyalkyl group which may have a substituent, a carboxyalkyl group, an alkoxycarbonylalkyl group, an aralkyl group which may have a substituent, a phenacyl group or an acyl group, R.sup.3 represents an alkyl group, a phenyl group which may have a substituent, a heteroaryl group or a cyclic amino group, X represents O or combination of OH and H, or a salt thereof; and a medicament, such as cytokine production suppressant, comprising the derivative or salt thereof as an effective ingredient. The invention compound has potential, highly specific and highly safe immunoregulating capacity so that it can suppress the excessive production of a specific cytokine in various diseases related to the immune system.
    Type: Grant
    Filed: November 17, 1997
    Date of Patent: April 4, 2000
    Assignee: SS Pharmaceutical Co., Ltd.
    Inventors: Hiroshi Hasegawa, Tadashi Mikami, Koichi Tachibana, Kazuo Yamazaki, Noriyuki Kawamoto, Noriaki Shioiri, Koji Kusano, Susumu Sato, Hideaki Matsuda, Toshio Yokoyama
  • Patent number: 6043260
    Abstract: This invention relates to method for treating a mammal which presents with heart failure comprising administering to a mammal a therapeutically effective amount of wherein 4-(1-ethyl-propoxy)-3,6-dimethyl-2-(2,4,6-trimethyl-phenoxy)-pyridine and (3,6-dimethyl-2-(2,4,6-trimethyl-phenoxy)-pyridin-4-yl)-(1-ethyl-propyl)-a mine or a pharmaceutically acceptable salt thereof. This invention is also directed to methods of using combinations of those two agents with other congestive heart failure treating compounds to treat congestive heart failure.
    Type: Grant
    Filed: February 10, 1999
    Date of Patent: March 28, 2000
    Assignee: Pfizer Inc
    Inventors: Yuhpyng L. Chen, Anthony A. Fossa
  • Patent number: 6015569
    Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: November 17, 1997
    Date of Patent: January 18, 2000
    Assignee: Centre International de Recherches Dermatologiques Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 6015820
    Abstract: Compounds of formula (3) in which:R.sub.1 and R.sub.2 independently represent an atom of hydrogen, an aliphatic group or an alkyloxyalkyl group in which the alkyl chains are from C.sub.1 to C.sub.4 or together form an aromatic ring;R.sub.3 represents:an atom of hydrogen, oran NHR.sub.5 group in which R.sub.5 represents an atom of hydrogen or a COR.sub.6 group in which R.sub.6 is an aliphatic or aromatic group, oran NO.sub.2 group ora COOR.sub.7 group in which R.sub.7 is an aliphatic group,R.sub.4 represents a phenyl or heterocyclic group.These compounds can be used in the treatment of illnesses linked to the HIV virus.
    Type: Grant
    Filed: April 15, 1998
    Date of Patent: January 18, 2000
    Assignee: Centre National de la Recherche Scientifique (CNRS)
    Inventors: Emile Bisagni, Valerie Dolle, Chi Hung Nguyen, Michel Legraverend, Anne-Marie Aubertin, Andre Kirn, Marie-Line Andreola, Laura Tarrago-Litvak, Michel Ventura
  • Patent number: 6004985
    Abstract: This invention is directed to monocyclic N-heterocyclics which are substituted by acyclic or cyclic thio 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: October 9, 1996
    Date of Patent: December 21, 1999
    Assignee: Berlex Laboratories, Inc.
    Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
  • Patent number: 6005009
    Abstract: Methods of inhibiting fibrosis comprising administering certain pyridoxal benzoyl hydrazones or analogs thereof are disclosed. Preferred hydrazones are pyridoxal benzoyl hydrazone, 3-hydroxyisonicotinaldehyde benzoyl hydrazone and salicylaldehyde benzoyl hydrazone. The methods are useful in treating fibrosing disorders, including dermal fibrosing disorders, fibrosis of internal organs and fibrotic conditions of the eye.
    Type: Grant
    Filed: March 20, 1997
    Date of Patent: December 21, 1999
    Assignee: Duke University
    Inventors: Saood Murad, Sheldon R. Pinnell, Huanshu Yang
  • Patent number: 6004986
    Abstract: The invention relates to methods for treating cerebral vasospasm induced by hemorrhage or cerebral ischemia, by treating patients with a therapeutically effective amount of a lipophilic iron chelator.
    Type: Grant
    Filed: May 8, 1998
    Date of Patent: December 21, 1999
    Assignee: The University of Virginia Patent Foundation
    Inventors: Adam S. Arthur, Giuseppe Lanzino
  • Patent number: 5965586
    Abstract: The present invention relates to a method of treating a patient with a fibrotic or fibroproliferative disorder and a method of suppressing formation of collagen and collagen-like substances or biosynthesis of procollagen in living systems by administering to a patient or living system, respectively, an effective amount of a compound of Formulae (I) or (II) and derivatives thereof: ##STR1## R.sub.1, R.sub.2, R.sub.3, and R.sub.4 each individually represent a hydrogen, an alkyl, alkenyl, or alkoxy group containing 1 to about 8 carbon atoms, an aryl, aralkyl, or cycloalkyl group containing about 5 to 12 carbon atoms, or a carboalkoxy or carbamyl group containing up to 8 carbon atoms, or a peptide or peptidomimetic moiety containing 10 to about 30 carbon atoms.
    Type: Grant
    Filed: December 16, 1997
    Date of Patent: October 12, 1999
    Assignee: Cornell Research Foundation, Inc.
    Inventors: Hartmut M. Hanauske-Abel, Timothy A. McCaffrey, Robert Walter Grady
  • Patent number: 5965585
    Abstract: The present invention relates to a method of treating a patient with a fibrotic or fibroproliferative disorder and a method of suppressing formation of collagen and collagen-like substances or biosynthesis of procollagen in living systems by administering to a patient or living system, respectively, an effective amount of a compound of Formulae (I) or (II) and derivatives thereof: ##STR1## R.sub.1, R.sub.2, R.sub.3, and R.sub.4 each individually represent a hydrogen, an alkyl, alkenyl, or alkoxy group containing 1 to about 8 carbon atoms, an aryl, aralkyl, or cycloalkyl group containing about 5 to 12 carbon atoms, or a carboalkoxy or carbamyl group containing up to 8 carbon atoms, or a peptide or peptidomimetic moiety containing 10 to about 30 carbon atoms.
    Type: Grant
    Filed: May 30, 1997
    Date of Patent: October 12, 1999
    Assignee: Cornell Research Foundation, Inc.
    Inventors: Hartmut M. Hanauske-Abel, Timothy A. McCaffrey, Robert Walter Grady
  • Patent number: 5962479
    Abstract: Corticotropin-releasing factor (CRF) antagonists having formulae (I), (II) or (III) wherein the dashed lines, A, B, Y, Z, G, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.16 and R.sub.17 are as defined in the description, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment of CNS and stress-related disorders.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: October 5, 1999
    Assignee: Pfizer Inc.
    Inventor: Yuhpyng Liang Chen
  • Patent number: 5935977
    Abstract: The present invention relates to a substituted vinylpyridine derivative represented by the following formula (1): ##STR1## (wherein R.sup.1 represents a hydrogen atom, an alkyl group, etc., R.sup.2 represents an alkyl group; one of R.sup.3 and R.sup.4, which are different from each other, represents a hydrogen atom and the other represents a nitrile group, R.sup.5 represents an aryl group or a heteroaryl group, X represents an oxygen atom, etc., and one of Q.sup.1, Q.sup.2, and Q.sup.3 represents a nitrogen atom and the other two represent CH); a salt of the derivative; and a drug containing the derivative or salt as the active ingredient. Due to strong PDE inhibitory action and TNF-.alpha. production inhibitory action, the derivative, salt, and drug are useful for the prevention and treatment of a wide variety of inflammatory diseases and autoimmune diseases.
    Type: Grant
    Filed: May 26, 1998
    Date of Patent: August 10, 1999
    Assignee: SS Pharmaceutical Co., Ltd.
    Inventors: Kazuo Yamazaki, Yoichiro Ogawa, Hidehiko Kohya, Tadashi Mikami, Noriyuki Kawamoto, Noriaki Shioiri, Hiroshi Hasegawa, Susumu Sato
  • Patent number: 5919816
    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: October 17, 1997
    Date of Patent: July 6, 1999
    Assignee: BioNumerik Pharmaceuticals, Inc.
    Inventors: Frederick H. Hausheer, Thomas J. Dodd
  • Patent number: 5891895
    Abstract: Hydroxypyridine derivatives of the formula ##STR1## wherein R.sup.1 is a branched C.sub.3-8 alkyl group or a C.sub.3-8 cycloalkyl group, each of which may be substituted;R.sup.2 is a halogen atom, a C.sub.1-4 alkyl group or a C.sub.1-4 alkoxy group;X is an oxygen atom or NR.sup.3 in which R.sup.3 is a hydrogen atom or a C.sub.1-4 alkyl group;R.sup.4, R.sup.5 and R.sup.6 are independently (1) a hydrogen atom, (2) a halogen atom, (3) a cyano group, (4) a nitro group, (5) a C.sub.1-4 acyl group, (6) a C.sub.1-4 alkoxy group which may be substituted with halogen, (7) a C.sub.1-4 alkyl group which may be substituted with halogen or (8) a mercapto group which may be substituted with a C.sub.1-4 alkyl group;m is 0 to 3; andn is 0 or 1;provided that all of R.sup.4, R.sup.5 and R.sup.6 are not hydrogen atom, or a salt thereof, which have potassium channel opening activity and are useful as therapeutic agents of cardiovascular diseases such as angina pectoris, hypertension, etc.
    Type: Grant
    Filed: April 14, 1997
    Date of Patent: April 6, 1999
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuru Shiraishi, Tsuyoshi Maekawa, Toshifumi Watanabe
  • Patent number: 5852042
    Abstract: The invention relates to novel substituted N-(4-pyridyl)carboxamides of the formula ##STR1## in which Q is substituted 4-pyridyl, A is hydrogen, alkyl, acyl or aralkyl and Y-Z is an optionally modified hydrocarbon radical or Y is a bond or a bivalent radical and Z is aryl, O-aryl, cycloalkyl, cycloalkenyl or heterocyclyl, all of which are optionally substituted, to processes for their preparation, to intermediates during their preparation, and to their use as pesticides, in particular as insecticides, acaricides and nematicides, and also as fungicides.
    Type: Grant
    Filed: September 26, 1995
    Date of Patent: December 22, 1998
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Harald Jakobi, Werner Knauf, Ulrich Sanft, Manfred Kern, Dieter Bernd Reuschling, Adolf Heinz Linkies, Werner Bonin
  • Patent number: 5837703
    Abstract: Therapeutic compounds have the formula:(X)j-(core moiety),j being an integer from one to three, the core moiety comprising a core moiety, the core moiety being a heterocycle having one ring or two-fused rings, each ring having five or six ring atoms, A being a carbon atom of the core moiety and attached to a terminal carbon atom of (CH.sub.2).sub.m, and X has a structure and X being a racemic mixture, R or S enantiomer, solvate, hydrate, or salt of: ##STR1## *C is a chiral carbon atom, n is an integer from one to four (preferably from one to three), one or more carbon atoms of (CH.sub.2).sub.n may be substituted by a keto or hydroxy group, and m is an integer from one to fourteen. Independently, R.sub.1 and R.sub.2 may be a hydrogen, a straight or branched chain alkyl or alkenyl of up to twelve carbon atoms in length, or --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.
    Type: Grant
    Filed: November 12, 1993
    Date of Patent: November 17, 1998
    Assignee: Cell Therapeutics, Inc.
    Inventors: Anil M. Kumar, John Michnick, Gail E. Underiner, J. Peter Klein, Glenn C. Rice
  • Patent number: 5789426
    Abstract: The present invention relates to a method of treating a patient with a fibrotic or fibroproliferative disorder and a method of suppressing formation of collagen and collagen-like substances or biosynthesis of procollagen in living systems by administering to a patient or living system, respectively, an effective amount of a compound of Formulae (I) or (II) and derivatives thereof: ##STR1## R.sub.1, R.sub.2, R.sub.3, and R.sub.4 each individually represent a hydrogen, an alkyl, alkenyl, or alkoxy group containing 1 to about 8 carbon atoms, an aryl, aralkyl, or cycloalkyl group containing about 5 to 12 carbon atoms, or a carboalkoxy or carbamyl group containing up to 8 carbon atoms, or a peptide or peptidomimetic moiety containing 10 to about 30 carbon atoms.
    Type: Grant
    Filed: January 20, 1995
    Date of Patent: August 4, 1998
    Assignee: Cornell Research Foundation, Inc.
    Inventors: Hartmut M. Hanauske-Abel, Timothy A. McCaffrey, Robert Walter Grady
  • Patent number: RE37087
    Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.
    Type: Grant
    Filed: June 20, 1991
    Date of Patent: March 6, 2001
    Assignee: Schering Aktiengesellschaft
    Inventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles
  • Patent number: RE35948
    Abstract: Pharmaceutical compositions containing a 3-hydroxypyrid-2-one or 3-hydroxypyrid one in which the hydrogen atom attached to the nitrogen atom is replaced by an aliphatic acyl group, by an aliphatic hydrocarbon group, or by an aliphatic hydrocarbon group substituted by one or, except in the case of ionizable groups, more than one substituent selected from aliphatic acyl, alkoxy, aliphatic amine, aliphatic amide, carboxy, aliphatic ester, halogen, hydroxy and sulpho groups and, optionally, in which one or more of the hydrogen atoms attached to ring carbon atoms are replaced by one of said substituents, by an aliphatic hydrocarbon group, or by an aliphatic hydrocarbon group substituted by an alkoxy, aliphatic ester, halogen or hydroxy group, but excluding compounds in which said replacement of hydrogen atoms in the compound is effected only by aliphatic hydrocarbon groups, or a salt thereof containing a physiologically acceptable ion or ions, are of value for removing toxic amounts of metals, particularly iron, f
    Type: Grant
    Filed: February 17, 1995
    Date of Patent: November 3, 1998
    Assignee: British Technology Group Ltd.
    Inventors: Robert C. Hider, George Kontoghiorghes, Jack Silver