Chalcogens Bonded Directly To At Least Two Ring Carbons Of The Six-membered Hetero Ring Patents (Class 514/348)
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Patent number: 6503948Abstract: 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: GrantFiled: April 17, 2002Date of Patent: January 7, 2003Assignee: Southern Research InstituteInventors: Herbert M. Blatter, Donald R. Kahn, James R. Piper, John A. Secrist, III, Robert F. Struck, Carroll Temple
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Patent number: 6503932Abstract: 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: GrantFiled: December 12, 2001Date of Patent: January 7, 2003Assignee: BASF AktiengesellschaftInventors: Karl Eicken, Eberhard Ammermann, Reinhard Stierl, Gisela Lorenz, Siegfried Strathmann, Maria Scherer, Klaus Schelberger, Manfred Hampel
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Patent number: 6495580Abstract: 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: GrantFiled: October 18, 1999Date of Patent: December 17, 2002Assignee: ViroPharma IncorporatedInventors: Theodore J. Nitz, Daniel C. Pevear
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Patent number: 6495571Abstract: 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: GrantFiled: March 25, 2002Date of Patent: December 17, 2002Assignee: Southern Research InstituteInventors: Robert F. Struck, Herbert M. Blatter, Anita Tiwari
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Patent number: 6492405Abstract: 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: GrantFiled: January 9, 2002Date of Patent: December 10, 2002Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventor: Abdullah Haj-Yehia
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Patent number: 6489348Abstract: 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: GrantFiled: September 24, 2001Date of Patent: December 3, 2002Assignee: BASF AktiengesellschaftInventors: Klaus Schelberger, Maria Scherer, Karl Eicken, Manfred Hampel, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6472412Abstract: 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: GrantFiled: January 26, 1996Date of Patent: October 29, 2002Assignee: Aventis Pharma LimitedInventors: Garry Fenton, Tahir Nadeem Majid, Malcolm Norman Palfreyman
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Patent number: 6436969Abstract: 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: GrantFiled: April 6, 2000Date of Patent: August 20, 2002Assignee: Kansas University Medical Center Research Institute Inc.Inventors: Raja Gabriel Khalifah, Billy G. Hudson
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Patent number: 6436934Abstract: 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: GrantFiled: June 19, 2000Date of Patent: August 20, 2002Assignee: BASF AktiengesellschaftInventors: Klaus Schelberger, Maria Scherer, Karl Eicken, Manfred Hampel, Eberhard Ammermann, Gisela Lorenz, Siegfreid Strathmann
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Patent number: 6432989Abstract: A corticotropin releasing factor (CRF) antagonist is administered to treat disorders that can be treated by altering circadian rhythm.Type: GrantFiled: June 5, 2000Date of Patent: August 13, 2002Assignee: Pfizer IncInventor: Yuhpyng L. Chen
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Patent number: 6432990Abstract: 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: GrantFiled: January 30, 2002Date of Patent: August 13, 2002Assignee: Dow AgroSciences LLCInventors: 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
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Publication number: 20020068758Abstract: A novel 3-hydroxypyridinone compound of formula I is provided 1Type: ApplicationFiled: September 4, 2001Publication date: June 6, 2002Applicant: BTG International Limited.Inventors: Robert Charles Hider, Gary Stuart Tilbrook, Zudong Liu
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Patent number: 6391893Abstract: 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: GrantFiled: January 21, 2000Date of Patent: May 21, 2002Assignee: Southern Research InstituteInventors: Robert F. Struck, Herbert M. Blatter, Anita Tiwari
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Patent number: 6376518Abstract: 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: GrantFiled: January 21, 2000Date of Patent: April 23, 2002Assignee: Southern Research InstituteInventor: Robert F. Struck
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Patent number: 6372748Abstract: 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 1Type: GrantFiled: June 13, 2000Date of Patent: April 16, 2002Assignee: BASF AktiengesellschaftInventors: Klaus Schelberger, Maria Scherer, Karl Eicken, Manfred Hampel, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6369083Abstract: 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: GrantFiled: September 16, 1999Date of Patent: April 9, 2002Assignee: Dow AgroSciences LLCInventors: 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
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Patent number: 6335353Abstract: 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: GrantFiled: November 10, 1999Date of Patent: January 1, 2002Assignee: BTG International LimitedInventors: Robert Charles Hider, Gary Stuart Tilbrook, Zudong Liu
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Patent number: 6300346Abstract: Indenyl hydroxamic acids, (hydroxy) ureas and urethanes are useful in the treatment of precancerous lesions and neoplasms.Type: GrantFiled: March 7, 2000Date of Patent: October 9, 2001Assignee: Cell Pathways, Inc.Inventors: Gerhard Sperl, Paul Gross, Klaus Brendel, Rifat Pamukcu, Gary A. Piazza
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Patent number: 6235761Abstract: 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: GrantFiled: February 22, 1999Date of Patent: May 22, 2001Inventors: Neil Hartman, Robert F. Struck, Seamus O'Reilly, John M. Strong, Eric K. Rowinsky, Jerry M. Collins
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Patent number: 6221886Abstract: 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: GrantFiled: January 11, 2000Date of Patent: April 24, 2001Assignee: Berlex Laboratories, Inc.Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
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Patent number: 6200996Abstract: 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: GrantFiled: January 27, 2000Date of Patent: March 13, 2001Assignee: American Cyanamid CompanyInventors: Jeremy I. Levin, James M. Chen, Frances C. Nelson
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Patent number: 6187924Abstract: Compounds of formula (I) are useful as therapeutic agents, by virtue of having MMP and TNF inhibitory activity.Type: GrantFiled: November 12, 1998Date of Patent: February 13, 2001Assignee: Darwin Discovery, Ltd.Inventors: Andrew Douglas Baxter, David Alan Owen, John Gary Montana, Robert John Watson
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Patent number: 6162815Abstract: 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: GrantFiled: September 10, 1998Date of Patent: December 19, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 6150382Abstract: 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: GrantFiled: May 21, 1999Date of Patent: November 21, 2000Assignee: Berlex Laboratories, Inc.Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
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Patent number: 6114363Abstract: 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: GrantFiled: August 4, 1998Date of Patent: September 5, 2000Assignee: BASF AktiengesellschaftInventors: 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
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Patent number: 6103732Abstract: 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: GrantFiled: October 8, 1998Date of Patent: August 15, 2000Assignee: BASF AktiengesellschaftInventors: Wilhelm Amberg, Andreas Kling, Dagmar Klinge, Hartmut Riechers, Ernst Baumann, Liliane Unger, Manfred Raschack, Stefan Hergenroder, Sabine Schult
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Patent number: 6080766Abstract: 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: GrantFiled: December 16, 1997Date of Patent: June 27, 2000Assignee: Cornell Research Foundation, Inc.Inventors: Hartmut M. Hanauske-Abel, Timothy A. McCaffrey, Robert Walter Grady
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Patent number: 6075023Abstract: 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: GrantFiled: February 17, 1998Date of Patent: June 13, 2000Assignee: BASF AktiengesellschaftInventors: Gerhard Peter Dohmen, Christoph Kunast, Reinhart Munk, Gerhard Rothhaas
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Patent number: 6066642Abstract: 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: GrantFiled: December 7, 1998Date of Patent: May 23, 2000Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Ji-Long Jiang, Yong-Chul Kim, Yishai Karton, Albert M. Van Rhee
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Patent number: 6057342Abstract: 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: GrantFiled: July 7, 1997Date of Patent: May 2, 2000Assignee: Dupont Pharmaceutical Co.Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
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Patent number: 6046219Abstract: 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: GrantFiled: December 16, 1997Date of Patent: April 4, 2000Assignee: Cornell Research Foundation, Inc.Inventors: Hartmut M. Hanauske-Abel, Timothy A. McCaffrey, Robert W. Grady
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Patent number: 6046221Abstract: 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: GrantFiled: August 25, 1998Date of Patent: April 4, 2000Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire, David I. Stirling
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Patent number: 6046218Abstract: 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: GrantFiled: November 17, 1997Date of Patent: April 4, 2000Assignee: 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
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Patent number: 6043260Abstract: 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: GrantFiled: February 10, 1999Date of Patent: March 28, 2000Assignee: Pfizer IncInventors: Yuhpyng L. Chen, Anthony A. Fossa
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Patent number: 6015569Abstract: 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: GrantFiled: November 17, 1997Date of Patent: January 18, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 6015820Abstract: 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: GrantFiled: April 15, 1998Date of Patent: January 18, 2000Assignee: 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
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Patent number: 6004985Abstract: 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: GrantFiled: October 9, 1996Date of Patent: December 21, 1999Assignee: Berlex Laboratories, Inc.Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
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Patent number: 6005009Abstract: 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: GrantFiled: March 20, 1997Date of Patent: December 21, 1999Assignee: Duke UniversityInventors: Saood Murad, Sheldon R. Pinnell, Huanshu Yang
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Patent number: 6004986Abstract: 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: GrantFiled: May 8, 1998Date of Patent: December 21, 1999Assignee: The University of Virginia Patent FoundationInventors: Adam S. Arthur, Giuseppe Lanzino
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Patent number: 5965586Abstract: 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: GrantFiled: December 16, 1997Date of Patent: October 12, 1999Assignee: Cornell Research Foundation, Inc.Inventors: Hartmut M. Hanauske-Abel, Timothy A. McCaffrey, Robert Walter Grady
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Patent number: 5965585Abstract: 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: GrantFiled: May 30, 1997Date of Patent: October 12, 1999Assignee: Cornell Research Foundation, Inc.Inventors: Hartmut M. Hanauske-Abel, Timothy A. McCaffrey, Robert Walter Grady
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Patent number: 5962479Abstract: 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: GrantFiled: December 6, 1996Date of Patent: October 5, 1999Assignee: Pfizer Inc.Inventor: Yuhpyng Liang Chen
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Patent number: 5935977Abstract: 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: GrantFiled: May 26, 1998Date of Patent: August 10, 1999Assignee: SS Pharmaceutical Co., Ltd.Inventors: Kazuo Yamazaki, Yoichiro Ogawa, Hidehiko Kohya, Tadashi Mikami, Noriyuki Kawamoto, Noriaki Shioiri, Hiroshi Hasegawa, Susumu Sato
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Patent number: 5919816Abstract: 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: GrantFiled: October 17, 1997Date of Patent: July 6, 1999Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Frederick H. Hausheer, Thomas J. Dodd
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Patent number: 5891895Abstract: 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: GrantFiled: April 14, 1997Date of Patent: April 6, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Tsuyoshi Maekawa, Toshifumi Watanabe
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Patent number: 5852042Abstract: 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: GrantFiled: September 26, 1995Date of Patent: December 22, 1998Assignee: Hoechst Schering AgrEvo GmbHInventors: Harald Jakobi, Werner Knauf, Ulrich Sanft, Manfred Kern, Dieter Bernd Reuschling, Adolf Heinz Linkies, Werner Bonin
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Patent number: 5837703Abstract: 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: GrantFiled: November 12, 1993Date of Patent: November 17, 1998Assignee: Cell Therapeutics, Inc.Inventors: Anil M. Kumar, John Michnick, Gail E. Underiner, J. Peter Klein, Glenn C. Rice
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Patent number: 5789426Abstract: 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: GrantFiled: January 20, 1995Date of Patent: August 4, 1998Assignee: Cornell Research Foundation, Inc.Inventors: Hartmut M. Hanauske-Abel, Timothy A. McCaffrey, Robert Walter Grady
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Patent number: RE37087Abstract: 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: GrantFiled: June 20, 1991Date of Patent: March 6, 2001Assignee: Schering AktiengesellschaftInventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles
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Patent number: RE35948Abstract: 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, fType: GrantFiled: February 17, 1995Date of Patent: November 3, 1998Assignee: British Technology Group Ltd.Inventors: Robert C. Hider, George Kontoghiorghes, Jack Silver