Nitrogen Double Bonded Directly At 2-position Of The Diazole Ring, Or Tautomeric Equivalent Patents (Class 514/388)
  • Patent number: 6630503
    Abstract: A cell adhesion inhibitor of the general formula: R3—L—L′—R1 is disclosed. An inhibitor of the present invention interacts with VLA-4 molecules and inhibits VLA-4 dependent cell adhesion. Also disclosed are methods for preparing and using such a cell adhesion inhibitor, as well as pharmaceutical compositions containing the same.
    Type: Grant
    Filed: August 14, 2000
    Date of Patent: October 7, 2003
    Assignee: Biogen, Inc.
    Inventors: Daniel Scott, Wen-Cherng Lee, Russell C. Petter, Mark Cornebise
  • Patent number: 6608096
    Abstract: Benzimidazole derivatives and salts and prodrugs thereof are disclosed, together with methods for the treatment of cancers or viral infections in warm-blooded animals by administration of these compounds. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.
    Type: Grant
    Filed: September 26, 2000
    Date of Patent: August 19, 2003
    Assignee: University of Arizona Foundation
    Inventors: James Berger Camden, James C. Quada, Jr., Joseph K. Agyin
  • Patent number: 6569880
    Abstract: This invention relates to novel potassium channel blocking agents, and their use in the preparation of pharmaceutical compositions.
    Type: Grant
    Filed: February 28, 2002
    Date of Patent: May 27, 2003
    Assignee: Neurosearch A/S
    Inventors: Bo Skaaning Jensen, Søren Peter Olesen, Lene Teuber, Dan Peters, Dorte Strøbæk
  • Patent number: 6569875
    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 nonaromatic, 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 to
    Type: Grant
    Filed: June 13, 2000
    Date of Patent: May 27, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Schelberger, Maria Scherer, Karl Eicken, Manfred Hampel, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
  • Patent number: 6552059
    Abstract: Method of treating leukemia, inhibiting the growth or proliferation of leukemic cells or extending the life span of a animal having leukemia are disclosed. The methods comprise the step of treating the leukemia with an effective amount of a compound of the Formula I or a pharmaceutically acceptable salt or prodrug form thereof, wherein: X is hydrogen, halogen or alkyl of less than 7 carbon atoms; n is a positive integer of less than 4; Y is hydrogen, chlorine, nitro, methyl or ethyl; R is hydrogen or an alkyl group of from 1 to 8 carbon atoms, alkylcarbamyl; R2 is 4-thiazolyl or NHCOOR1; and R1 is an aliphatic hydrocarbon of less than 7 carbon atoms. A chemotherapeutic agent and/or potentiator can be used in conjunction with the compound of the Formula I.
    Type: Grant
    Filed: February 23, 2001
    Date of Patent: April 22, 2003
    Assignee: University of Arizona Foundation
    Inventor: James Berger Camden
  • Patent number: 6518291
    Abstract: The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.
    Type: Grant
    Filed: September 14, 1999
    Date of Patent: February 11, 2003
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: Jeffrey O. Saunders, David M. Armistead, Michael C. Badia, Randy S. Bethiel, Catherine A. Frank, Doug Naegele, Perry M. Novak, David A. Pearlman, Steven M. Ronkin
  • Publication number: 20030022926
    Abstract: The present invention relates to a method for a sustained treatment and/or prophylaxis of neuropathic pain in mammal comprising administering by peripheral nerve injection a neuropathic pain relieving composition comprising an alpha-2-adrenergic agonist.
    Type: Application
    Filed: May 7, 2002
    Publication date: January 30, 2003
    Inventor: Patricia Lavand'Homme
  • Patent number: 6506783
    Abstract: A pharmaceutical composition that inhibits the growth of tumors and cancers in mammals and can be used to treat viral infections that comprises a fungicide is disclosed. The particular fungicide used is a benzimidazole derivative having the formula: wherein R is selected from the group consisting of H, carboxyl (—CO2H), hydroxyl, amino or esters (—CO2R′) wherein R′ is selected from the group consisting of alkoxy, haloalkyl, alkenyl, and cycloalkyl wherein the alkyl groups have from 1-8 carbons or CH3CH2(OCH2CH2)n—or CH3CH2CH2(OCH2CH2CH2)n—or (CH3)2CH—(OCH(CH3)CH2)n—wherein n is from 1-3, the pharmaceutically acceptable salts thereof, or mixtures thereof.
    Type: Grant
    Filed: May 16, 1997
    Date of Patent: January 14, 2003
    Assignee: The Procter & Gamble Company
    Inventor: James Berger Camden
  • Patent number: 6498194
    Abstract: The invention relates to a novel fungicidal composition comprising a fungicidally acceptable carrier and/or surface active agent together with, and synergistically effective amounts of (a) at least one benzophenone of formula I  wherein R1, R2, R3, R4, R5, R6, R7, m and n have the meaning given; at least one fungicidal active ingredient selected from the following groups (A), (B), (C), (D) and (E): (A) an ergosterol biosynthesis inhibitor; (B) a strobilurine derivative, (C) a melanin biosynthesis inhibitor; (D) a compound selected from the group consisting of acibenzolar, benomyl, captan, carboxin, chlorothalonil, copper, cyprodinil, dinocap, dithianon, dimethomorph, dodine, ethirimol, famoxadone, fenpiclonil, fluazinam, mancozeb, metalaxyl, pyrifenox, sulfur, vinclozolin and (E) an azolopyrimidine of formula II  in which R8, R9, R10, R11, A, L and p have the meaning given; and to a method of controlling the growth of phytopathogenic fungi at a locus which
    Type: Grant
    Filed: January 16, 2002
    Date of Patent: December 24, 2002
    Assignee: BASF Aktiengsellschaft
    Inventors: Henry Van Tuyl Cotter, Gunther Reichert, Ewald Sieverding, Petrus Martinus Franciscus Emanuel Jegerings
  • Patent number: 6495698
    Abstract: Novel, binder-free compacted forms of 1,3-dihalo-5,5-dimethylhydantoins in which one halogen atom is chlorine and the other is a bromine or chlorine atom are produced and used for microbiological control in aqueous media and water.
    Type: Grant
    Filed: January 18, 2000
    Date of Patent: December 17, 2002
    Assignee: Albemarle Corporation
    Inventor: Jonathan N. Howarth
  • Patent number: 6482843
    Abstract: Benzimidazole derivatives and salts and prodrugs thereof are disclosed, together with methods for the treatment of cancers or viral infections in warm blooded animals by administration of these compounds. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.
    Type: Grant
    Filed: September 29, 2000
    Date of Patent: November 19, 2002
    Assignee: The Procter & Gamble Company
    Inventors: James C. Quada, Jr., Joseph K. Agyin, James Berger Camden
  • Patent number: 6479526
    Abstract: This invention is a method of treating cancer, both carcinomas and sarcomas, and viral infections, in particular HIV through the administration of a pharmaceutical composition containing a benzimidazole derivative. The composition is also claimed. The benzimidazole derivative is selected from the group consisting of: wherein X is hydrogen, halogen, alkyl of less than 7 carbon atoms or alkoxy of less than 7 carbon atoms; n is a positive integer of less than 4; Y is hydrogen, chlorine, nitro, methyl, ethyl or oxychloro; R is hydrogen, alkylaminocarbonyl wherein the alkyl group has from 3 to 6 carbon atoms, or an alkyl group of from 1 to 8 carbon atoms and R2 is 4-thiazolyl, NHCOOR1 wherein R1 is aliphatic hydrocarbon of less than 7 carbon atoms, prodrugs, pharmaceutically acceptable salts and mixtures thereof and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: March 26, 2002
    Date of Patent: November 12, 2002
    Assignee: The Procter & Gamble Company
    Inventor: James Berger Camden
  • Patent number: 6462062
    Abstract: Benzimidazole derivatives and salts and prodrugs thereof are disclosed, together with methods for the treatment of cancers or viral infections in warm blooded animals by administration of these compounds. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.
    Type: Grant
    Filed: September 26, 2000
    Date of Patent: October 8, 2002
    Assignee: The Procter & Gamble Company
    Inventors: James Berger Camden, James C. Quada, Jr., Joseph K. Agyin
  • Patent number: 6423734
    Abstract: Methods of treating and inhibiting cancerin animals by administering a therapeutically effective amount of a pharmaceutical composition having benzimidazole of the general formula: wherein X is hydrogen, halogen, alkyl of less than 7 carbon atoms or alkoxy of less than 7 carbon atoms; n is a positive integer of less than 4; Y is hydrogen, chlorine, oxychloro, nitro, methyl or ethyl; and R is hydrogen, or an alkyl group of from 1 to 8 carbon atoms and R2 is NHCOOR1 wherein R1 is aliphatic hydrocarbon of less than 7 carbon atoms, and preferably an alkyl group of less than 7 carbon atoms and pharmaceutically acceptable derivatives alone, or in combination, or in conduction with other therapeutic agents such as other cancer inhibiting compounds, and operative combinations thereof.
    Type: Grant
    Filed: August 13, 1999
    Date of Patent: July 23, 2002
    Assignee: The Procter & Gamble Company
    Inventor: James Berger Camden
  • Patent number: 6407105
    Abstract: Benzimidazole derivatives and salts and prodrugs thereof are disclosed, together with methods for the treatment of cancers or viral infections in warm blooded animals by administration of these compounds. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.
    Type: Grant
    Filed: September 26, 2000
    Date of Patent: June 18, 2002
    Assignee: The Procter & Gamble Company
    Inventors: James C. Quada, Jr., Joseph K. Agyin, James Berger Camden
  • Patent number: 6380232
    Abstract: Benzimidazole derivatives and salts and prodrugs thereof are disclosed, together with methods for the treatment of cancers or viral infections in warm blooded animals by administration of these compounds. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.
    Type: Grant
    Filed: September 26, 2000
    Date of Patent: April 30, 2002
    Assignee: The Procter & Gamble Company
    Inventors: James C. Quada, Jr., Joseph K. Agyin, James Berger Camden
  • Publication number: 20020049246
    Abstract: This invention relates to novel potassium channel blocking agents, and their use in the preparation of pharmaceutical compositions.
    Type: Application
    Filed: December 29, 2000
    Publication date: April 25, 2002
    Applicant: NeuroSearch A/S
    Inventors: Bo Skaaning Jensen, Soren Peter Olesen, Lene Teuber, Dan Peters, Dorte Strobaek
  • Patent number: 6365734
    Abstract: Cucurbituril derivatives, their preparation methods and uses.
    Type: Grant
    Filed: June 28, 2000
    Date of Patent: April 2, 2002
    Assignee: Pohang University of Science and Technology Foundation
    Inventors: Kimoon Kim, Jaheon Kim, In-Sun Jung, Soo-Young Kim, Eunsung Lee, Jin-Koo Kang
  • Patent number: 6365613
    Abstract: A fungicidal mixture comprises a.1)a phenyl benzyl ether derivative of the formula I.a, I.b or I.c, or a.2) a carbamate of the formula I.d, where X is CH and N, n is 0, 1 or 2 and R is halogen, C1-C4-alkyl and C1-C4-haloalkyl, it being possible for the radicals R to be different if n is 2, or a salt or adduct thereof, and b) a fungicidally active compound from the class of the benzimidazoles or benzimidazole-releasing precursors (II), in a synergistically effective amount.
    Type: Grant
    Filed: November 17, 1999
    Date of Patent: April 2, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Schelberger, Maria Scherer, Hubert Sauter, Bernd Müller, Erich Birner, Joachim Leyendecker, Manfred Hampel, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
  • Patent number: 6348464
    Abstract: The present invention relates to pharmaceutical compositions and methods of using pyrrolecarbonylimino derivatives to inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, thereby effecting neuronal activities, inhibiting angiogenesis, and treating glutamate abnormalities, compulsive disorders, prostate diseases and cancers.
    Type: Grant
    Filed: November 12, 1999
    Date of Patent: February 19, 2002
    Assignee: Guilford Pharmaceuticals, Inc.
    Inventors: Paul F. Jackson, Barbara S. Slusher
  • Publication number: 20020010201
    Abstract: The invention relates to an active substance combination consisting of clonidine and pramipexole for treating Restless Leg Syndrome.
    Type: Application
    Filed: October 4, 2001
    Publication date: January 24, 2002
    Inventor: Hans Michael Brecht
  • Publication number: 20010053387
    Abstract: A pharmaceutical composition which is a solid pellet comprising an inert core, a benzimidazole in or on the core, a moisture resistant coating around the core, the moisture resistant coating comprising at least one hydrophobic material, and an enteric coating around the moisture resistant coating.
    Type: Application
    Filed: July 9, 2001
    Publication date: December 20, 2001
    Inventors: Yusuf Khwaja Hamied, Vinay G. Nayak, Geena Malhotra
  • Patent number: 6329355
    Abstract: A method for inhibiting the growth of tumors and cancers in mammals comprising administering a chemotherapeutic agent to significantly reduce the tumor in mass and then administering a benzimidazole derivative. Potentiators can also be included in the benzimidazole composition.
    Type: Grant
    Filed: April 19, 2000
    Date of Patent: December 11, 2001
    Assignee: The Procter & Gamble Company
    Inventor: James Berger Camden
  • Patent number: 6319949
    Abstract: A method for preventing fungal diseases in crops which comprises the steps of: (a) applying to a crop an aqueous or a non-aqueous spray composition which includes a pesticide and a spray adjuvant including a solvent and an emulsifier, wherein the solvent is a mixture of aliphatic hydrocarbons having a distillation range of about 520 to 600° F. and an aromatic content of about 1% or less, or the solvent is a single or combination of C6-C18 fatty alcohol(s); and (b) applying chlorothalonil to the crop previously to, simultaneously with, or subsequently to the application of the aqueous spray composition, wherein phytotoxicity associated with the application of chlorothalonil is reduced or eliminated.
    Type: Grant
    Filed: November 4, 1996
    Date of Patent: November 20, 2001
    Assignee: Syngenta Limited
    Inventors: Jeffrey R. Schussler, Robert E. Moser, Kevin E. Crosby, John R. Washington
  • Publication number: 20010027205
    Abstract: Method of treating leukemia, inhibiting the growth or proliferation of leukemic cells or extending the life span of a animal having leukemia are disclosed.
    Type: Application
    Filed: February 23, 2001
    Publication date: October 4, 2001
    Applicant: The Procter & Gamble Company
    Inventor: James Berger Camden
  • Patent number: 6271217
    Abstract: A method for inhibiting the growth of tumors and cancers in mammals comprising administering a chemotherapeutic agent to significantly reduce the tumor in mass and then administering a benzimidazole derivative. Potentiators can also be included in the benzimidazole composition.
    Type: Grant
    Filed: December 22, 1998
    Date of Patent: August 7, 2001
    Assignee: The Procter & Gamble Company
    Inventor: James Berger Camden
  • Patent number: 6265427
    Abstract: Method of treating leukemia, inhibiting the growth or proliferation of leukemic cells or extending the life span of a animal having leukemia are disclosed. The methods comprise the step of treating the leukemia with an effective amount of a compound of the Formula I or a pharmaceutically acceptable salt or prodrug form thereof, wherein: X is hydrogen, halogen or alkyl of less than 7 carbon atoms; n is a positive integer of less than 4; Y is hydrogen, chlorine, nitro, methyl or ethyl; R is hydrogen or an alkyl group of from 1 to 8 carbon atoms, alkylcarbamyl; R2 is 4-thiazolyl or NHCOOR1; and R1 is an aliphatic hydrocarbon of less than 7 carbon atoms. A chemotherapeutic agent and/or potentiator can be used in conjunction with the compound of the Formula I.
    Type: Grant
    Filed: August 16, 1999
    Date of Patent: July 24, 2001
    Assignee: The Proctor & Gamble Company
    Inventor: James Berger Camden
  • Patent number: 6262093
    Abstract: This invention is a method of treating cancer, both carcinomas and sarcomas, and viral infections, in particular HIV through the administration of a pharmaceutical composition containing a benzimidazole derivative. The composition is also claimed.
    Type: Grant
    Filed: March 9, 1999
    Date of Patent: July 17, 2001
    Assignee: The Proctor & Gamble Company
    Inventor: James Berger Camden
  • Patent number: 6242445
    Abstract: A novel benzimidazole derivative [specifically, for example, 2-ethoxy-1-[{4′-(2″-N,N-dimethylaminoethoxycarbonyl)phenyl}methyl]-1H-benzimidazole-6-carboxylic acid morpholide] represented by formula (I) and a salt thereof. The compound exhibits satisfactory curative effects for cardiac and nephric diseases, although having little action on blood-pressure.
    Type: Grant
    Filed: August 23, 2000
    Date of Patent: June 5, 2001
    Assignee: Kureha Chemical Industry Co., Ltd.
    Inventors: Mikiro Yanaka, Shigeru Suzuki, Fuyuhiko Nishijima, Hiroshi Takahashi, Mikio Sugano, Hiroshi Maruoka, Toru Yamazaki, Toshikazu Dewa, Hiroyuki Enari, Michihito Ise
  • Patent number: 6211200
    Abstract: Invented are zinc chelated G-CSF receptor ligands, pharmaceutical compositions containing these compounds, and methods of using these compounds as agonist of the G-CSF receptor. Also invented are novel processes used in preparing these compounds. Also invented are novel G-CSF receptor binding moieties of the invented zinc chelated G-CSF receptor ligands.
    Type: Grant
    Filed: October 30, 1998
    Date of Patent: April 3, 2001
    Assignees: SmithKline Beecham Corporation, Ligand Pharmaceuticals
    Inventors: Juan I. Luengo, Stephen G. Miller
  • Patent number: 6204278
    Abstract: The invention provides novel anilide compounds and pharmaceutical compositions comprising them. The invention relates to compounds of a formula: where Ar is an optionally-substituted aryl group; R4 and R5 are the same or different, and each is a hydrogen atom, a lower alkyl group, or a lower alkoxy group; and R4 and R5 may together form a lower alkylene group of which one or more methylene moieties may optionally be substituted by oxygen and/or sulfur atoms; X is —NH—, or oxygen or sulfur atom; Y is —NH—, an oxygen or sulfur atom, or a sulfoxide or sulfone group; Z is a single bond, or —NH6—; R6 represents a hydrogen atom or a lower alkylene group; and n is an integer of from 0 to 15; and their salts and solvates. The compounds of the invention are useful as pharmaceutical compositions, especially as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitors.
    Type: Grant
    Filed: May 19, 1997
    Date of Patent: March 20, 2001
    Assignee: Kowa Company, Ltd.
    Inventors: Kimiyuki Shibuya, Katsumi Kawamine, Yukihiro Sato, Toshiyuki Edano, Souhei Tanabe, Masami Shiratsuchi
  • Patent number: 6197804
    Abstract: Disclosed are novel 4,5-azolo-oxindoles having the formula These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. Thus, these compounds and their pharmaceutically acceptable salts, and *prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing these compounds, and methods for the treatment and/or prevention of cancer, particularly in the treatment or control of solid tumors using these compounds, as well as intermediates useful in the preparation of compounds of formula I.
    Type: Grant
    Filed: May 16, 2000
    Date of Patent: March 6, 2001
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kin-Chun Luk, Steven Gregory Mischke
  • Patent number: 6197805
    Abstract: This invention is directed to a broad spectrum antimicrobial composition which comprises a mixture of an iodopropynyl compound in combination with 2-(methoxycarbonylamino)benzimidazole and, where desirable, an algicide said mixture provided in an amount sufficient to protect a substrate from attack by one or more organisms. The composition can be used broadly in industrial systems and more particularly with substrates such as paints, coatings, stucco, concrete, stone, cementaceous surfaces, wood, caulking, sealants, textiles, leather, wood, preservatives, metal working fluids, drilling muds, clay slurries, glazes, optical brightness, carpet backing, pigments and as a preservative for other aqueous and wet state products, and the like.
    Type: Grant
    Filed: May 27, 1999
    Date of Patent: March 6, 2001
    Assignee: Troy Technology Corporation, Inc.
    Inventor: Roger Errol Smith
  • Patent number: 6194396
    Abstract: This invention relates to a heterocyclic compound of the formula wherein a group of the formula: is a group of the formula X is O, S or N-R5, R1 is lower alkyl, etc., R5 is hydrogen, lower alkyl, etc., R2 is hydrogen, halogen, lower alkyl, etc., R3 is halogen, lower alkyl, etc., R4 is amino optionally having suitable substituent(s), and A is lower alkylene, and a salt thereof, to processes for preparation thereof, and to a pharmaceutical composition comprising the same for the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.
    Type: Grant
    Filed: October 22, 1999
    Date of Patent: February 27, 2001
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Teruo Oku, Hiroshi Kayakiri, Shigeki Satoh, Yoshito Abe, Yuki Sawada, Takayuki Inoue, Hirokazu Tanaka
  • Patent number: 6194447
    Abstract: This invention relates to novel potassium channel blocking agents, and their use in the preparation of pharmaceutical compositions.
    Type: Grant
    Filed: July 2, 1999
    Date of Patent: February 27, 2001
    Assignee: Neurosearch A/S
    Inventors: Bo Skaaning Jensen, Søren Peter Olesen, Lene Teuber, Dan Peters, Dorte Strøbæk
  • Patent number: 6153634
    Abstract: Disclosed are novel 4,5-azolo-oxindoles having the formula ##STR1## These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. Thus, these compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing these compounds, and methods for the treatment and/or prevention of cancer, particularly in the treatment or control of solid tumors using these compounds, as well as intermediates useful in the preparation of compounds of formula I.
    Type: Grant
    Filed: December 15, 1999
    Date of Patent: November 28, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kin-Chun Luk, Christophe Michoud, Steven Gregory Mischke
  • Patent number: 6143747
    Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: ##STR1## or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.
    Type: Grant
    Filed: February 26, 1998
    Date of Patent: November 7, 2000
    Assignee: G. D. Searle & Co.
    Inventors: John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
  • Patent number: 6127422
    Abstract: A method of inhibiting an envelope virus selected from the group consisting of influenza bovine diarrheal, hepatitis C and tick borne encephalitis virus that udergoes hemagglutinin-mediated fusion with a host cell is disclosed which comprises administering to a virus-infected cell, a cell susceptible of infection or a mammal in need thereof, an effective amount of a compound as defined by Formula I in the specification.
    Type: Grant
    Filed: January 6, 1999
    Date of Patent: October 3, 2000
    Assignee: Eli Lilly and Company
    Inventors: Joseph M. Colacino, William J. Hornback, Scott C. Mauldin, John E. Munroe, Joseph C. Tang
  • Patent number: 6114327
    Abstract: The present application provides a series of benzimidazole compounds of formula I: ##STR1## which inhibit the growth of picornaviruses, such as rhinoviruses (bovine and human), enteroviruses such as polioviruses, coxsackieviruses of the A and B groups, or echo virus, cardioviruses such as encephalomyocarditis (EMC), apthoviruses such as foot and mouth disease virus, and flaviviruses such as hepatitis C virus and bovine viral diarrhea virus.Such compounds are also useful as intermediates for preparing additional benzimidazole antiviral compounds.
    Type: Grant
    Filed: October 22, 1999
    Date of Patent: September 5, 2000
    Assignee: Eli Lilly and Company
    Inventors: Steven Eugene Dunlap, Louis Nickolaus Jungheim, Mark Joseph Tebbe, Gilbert Thomas Voy, John Arnold Werner
  • Patent number: 6083961
    Abstract: This invention relates to a heterocyclic compound of the formula: ##STR1## wherein a group of the formula: ##STR2## is a group of the formula: ##STR3## etc., X is O, S or N--R.sup.5,R.sup.1 is lower alkyl, etc.,R.sup.5 is hydrogen, lower alkyl, etc.,R.sup.2 is hydrogen, halogen, lower alkyl, etc.,R.sup.3 is halogen, lower alkyl, etc.,R.sup.4 is amino optionally having suitable substituent(s), andA is lower alkylene,and a salt thereof, to processes for preparation thereof, and to a pharmaceutical composition comprising the same for the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.
    Type: Grant
    Filed: February 3, 1997
    Date of Patent: July 4, 2000
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Teruo Oku, Hiroshi Kayakiri, Shigeki Satoh, Yoshito Abe, Yuki Sawada, Takayuki Inoue, Hirokazu Tanaka
  • Patent number: 6077862
    Abstract: A pharmaceutical composition that inhibits the growth of tumors and cancers in mammals and can be used to treat viral infections that comprises a fungicide is disclosed. The particular fungicide used is a benzimidazole derivative having the formula: ##STR1## wherein R is selected from the group consisting of H, carboxyl (--CO.sub.2 H), hydroxyl, amino or esters (--CO.sub.2 R') wherein R' is selected from the group consisting of alkoxy, haloalkyl, alkenyl, and cycloalkyl wherein the alkyl groups have from 1-8 carbons or CH.sub.3 CH.sub.2 (OCH.sub.2 CH.sub.2).sub.n --or CH.sub.3 CH.sub.2 CH.sub.2 (OCH.sub.2 CH.sub.2 CH.sub.2).sub.n --or (CH.sub.3).sub.2 CH--(OCH(CH.sub.3)CH.sub.2).sub.n -- wherein n is from 1-3, the pharmaceutically acceptable salts thereof, or mixtures thereof.
    Type: Grant
    Filed: March 1, 1999
    Date of Patent: June 20, 2000
    Assignee: The Procter & Gamble Company
    Inventor: James Berger Camden
  • Patent number: 6071941
    Abstract: A method for the protection of trees of the families Musaceae or Plantanginaceae from destructive pests whereby the trees to be protected share a common root system.
    Type: Grant
    Filed: October 6, 1999
    Date of Patent: June 6, 2000
    Assignee: Rhone-Poulenc Agro
    Inventors: Jorge Cepeda, Juan Bocanegra
  • Patent number: 6063795
    Abstract: Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: May 16, 2000
    Assignee: G.D. Searle & Company
    Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L Brown, Joseph J McDonald
  • Patent number: 6011045
    Abstract: The present invention relates to compounds of the formula IA--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.
    Type: Grant
    Filed: December 22, 1997
    Date of Patent: January 4, 2000
    Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.
    Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Jochen Knolle, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
  • Patent number: 5990145
    Abstract: The present invention relates to compounds of the formula I,A--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.
    Type: Grant
    Filed: December 22, 1997
    Date of Patent: November 23, 1999
    Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.
    Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Karlheinz Scheunemann, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
  • Patent number: 5981551
    Abstract: Described herein are substituted 2,5-Diimino-3a,6a-diaryl-1,2,3,3a,4,5,6,6a-octahydroimidazo[4,5-d]imidazol es of formula (I), wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are defined therein, pharmaceutical compositions containing these compounds, methods of using these compounds as G-CSF Mimetics, and processes used in preparing these compounds.
    Type: Grant
    Filed: November 20, 1998
    Date of Patent: November 9, 1999
    Assignee: SmithKline Beecham Corporation
    Inventors: Juan I. Luengo, James A. Chan, Ann L. Breen
  • Patent number: 5958933
    Abstract: A method for treating a mammal having a damaged central nervous system, as the result of trauma or disease, for reestablishing previously destroyed neurological functions in a traumatized or diseased mammal, or for controlling spasticity and for providing protection from such injury to the central nervous system. The method comprises administering to the mammal at least one neurologically active compound comprising two groups, one group providing alpha-adrenergic agonist activity, specifically a guanidino group, and the second group providing agonist activity selected from the group consisting of beta-adrenergic agonist activity, serotinergic agonist activity, and GABA-ergic agonist activity (for example a methylated xanthine group, having beta-adrenergic agonist activity) as the primary therapeutic agent. The neurologically active compound is administered in a dosage amount and at a dosage rate sufficient to at least partially restore the lost neurological function or to control spasticity.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 28, 1999
    Inventor: N. Eric Naftchi
  • Patent number: 5939357
    Abstract: This invention provides a novel fungicide composition which has a bicarbonate-containing inorganic salt ingredient which enhances the efficacy of a fungicide ingredient for the treatment of cultivated crops. An invention fungicide composition also contains a surfactant ingredient, and a water-soluble organic compound which functions as a compatibility enhancing ingredient in aqueous formulations, and the ingredients improve the spreadability and adhesiveness of the composition when applied to foliage. An invention fungicide composition also contains a fertilizer-effective ratio of nitrogen, phosphorus and potassium.
    Type: Grant
    Filed: June 7, 1993
    Date of Patent: August 17, 1999
    Assignee: Church & Dwight Co., Inc.
    Inventors: Keith A. Jones, Anthony E. Winston, M. Stephen Lajoie, Amy L. Joseph
  • Patent number: 5932600
    Abstract: The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.
    Type: Grant
    Filed: March 14, 1997
    Date of Patent: August 3, 1999
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jeffrey O. Saunders, David M. Armistead, Michael C. Badia, Randy S. Bethiel, Catharine A. Frank, Doug Naegele, Perry M. Novak, David A. Pearlman, Steven M. Ronkin
  • Patent number: 5929099
    Abstract: A pharmaceutical composition that inhibits the growth of tumors and cancers in mammals and can be used to treat viral infections that comprises a fungicide in combination with chemotherapeutic agents is disclosed. The particular fungicide used is a benzimidazole derivative. Potentiators can also be included in the composition.
    Type: Grant
    Filed: July 15, 1996
    Date of Patent: July 27, 1999
    Assignee: Procter & Gamble Co.
    Inventor: James Berger Camden