Plural Chalcogens Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/155)
  • Patent number: 5607945
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: March 4, 1997
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5605913
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: February 25, 1997
    Assignee: Hoechst Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Yulin Chiang, Edward J. Glamkowski, Kenneth J. Bordeau, Grover C. Helsley
  • Patent number: 5602158
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: February 11, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5602159
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: February 11, 1997
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5599821
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: February 4, 1997
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5597833
    Abstract: Substituted quinol-2-yl-methoxy-phenylacetic acid derivatives are prepared by reacting correspondingly substituted phenols with quinolylmethyl halides or by reacting unsubstituted phenols with quinolylmethyl halides and subsequent alkylation. The substituted quinol-2-yl-methoxy-phenylacetic acid derivatives may be employed as active substances in medicaments.
    Type: Grant
    Filed: August 4, 1993
    Date of Patent: January 28, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Michael Matzke, Klaus-Helmut Mohrs, Siegfried Raddatz, Romanis Fruchtmann, Reiner M uller-Peddinghaus, Armin Hatzelmann
  • Patent number: 5597842
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: January 28, 1997
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5596001
    Abstract: Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, m, X and Q are as defined below, and novel intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and natiatherosclerosis agents.
    Type: Grant
    Filed: October 25, 1993
    Date of Patent: January 21, 1997
    Assignee: Pfizer Inc.
    Inventor: Ernest S. Hamanaka
  • Patent number: 5594021
    Abstract: Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: January 14, 1997
    Assignee: Texas Biotechnology Corporation
    Inventors: Ming F. Chan, Bore G. Raju, Adam Kois, Erik J. Verner, Chengde Wu, Rosario S. Castillo, Venkatachalapathi Yalamoori, Vitukudi N. Balaji
  • Patent number: 5593995
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: January 14, 1997
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5594006
    Abstract: This invention provides a carbostyril derivative of the formula (1): ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and n are as defined, or its salt. This carbostyril derivative or its salt possess an excellent matrix metalloproteinases inhibitory action.
    Type: Grant
    Filed: February 16, 1995
    Date of Patent: January 14, 1997
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Makoto Sakamoto, Takeshi Imaoka, Masaaki Motoyama, Yoshihito Yamamoto, Hideki Takasu
  • Patent number: 5591745
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: January 7, 1997
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5591761
    Abstract: Thiophenyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, isoxazolyl-thiophenyl-sulfonamides, isoxazolyl-furyl-sulfonamides and isoxazolyl-pyrrolyl-sulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.
    Type: Grant
    Filed: April 5, 1994
    Date of Patent: January 7, 1997
    Assignee: Texas Biotechnology Corporation
    Inventors: Ming F. Chan, Bore G. Raju, Adam Kois, Erik J. Verner, Chengde Wu, Rosario S. Castillo, Venkatachalapathi Yalamoori, Vitukudi N. Balaji
  • Patent number: 5589494
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: December 31, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5580879
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: December 3, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5580890
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: December 3, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5578624
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 26, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau
  • Patent number: 5571821
    Abstract: Sulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided. The sulfonamides have formula I: ##STR1## in which Ar.sup.1 is a 3- or 5-isoxazolyl and Ar.sup.2 is selected from among alkyl, including straight and branched chains, aromatic rings, fused aromatic rings and heterocyclic rings, including 5-membered heterocycles with one, two or more heteroatoms and fused ring analogs thereof and 6-membered rings with one, two or more heteroatoms and fused ring analogs thereof. Ar.sup.2 is preferably thiophenyl, furyl, pyrrolyl, naphthyl, and phenyl. Compounds in which Ar.sup.
    Type: Grant
    Filed: May 20, 1994
    Date of Patent: November 5, 1996
    Assignee: Texas Biotechnology Corporation
    Inventors: Ming Fai Chan, Bore G. Raju, Adam Kois, Erik J. Verner, Chengde Wu, Rosario S. Castillo, Venkatachalapathi Yalamoori, Vitukudi N. Balaji, Kalyanaraman Ramnarayan
  • Patent number: 5571828
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 5, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5571803
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: December 22, 1995
    Date of Patent: November 5, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5563154
    Abstract: Compounds characterized generally as tetrahydro-quinolinyl or tetrahydro-isoquinolinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein G is a tetrahydro-quinolinyl or tetrahydro-isoquinolinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from--(CH.sub.2).sbsb.q--C.tbd.C-Vwherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: October 8, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, Robert E. Manning
  • Patent number: 5559125
    Abstract: A class of 4-hydroxy-2-(1H)-quinolone derivatives, substituted at the 3-position by an optionally substituted aryl substituent, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA receptor antagonist.
    Type: Grant
    Filed: July 11, 1994
    Date of Patent: September 24, 1996
    Assignee: Merck, Sharp & Dohme Limited
    Inventors: Janusz J. Kulagowski, Paul D. Leeson, Ian M. Mawer, Michael Rowley
  • Patent number: 5552551
    Abstract: Proton-transfer, low self-absorbing chromophores of the formula: ##STR1## wherein R.sub.2 and R.sub.3 are independently hydrogen, alkyl, aryl, cyano, nitro, halo or an ether group, R.sub.4 is O or N--H, and R.sub.5 is thienyl, naphthyl, furanyl, pyrrolyl, phenyl vinyl, diphenyl vinyl, phenyl ethynyl, hydroxy chromonyl phenyl, didecyloxy hydroxy chromonyl phenyl, phenyl or ##STR2## wherein R.sub.1 is vinyl, vinyl phenyl, vinyl benzyl, alkyl ethenyl, or alkyl phenyl ethenyl, provided that when R.sub.5 is phenyl and R.sub.2 and R.sub.3 are hydrogen, R.sub.4 is N--H.
    Type: Grant
    Filed: July 26, 1995
    Date of Patent: September 3, 1996
    Assignee: Florida State University
    Inventors: Joseph B. Schlenoff, Kurtis F. Johnson, Jayesh Dharia, Feng Gao
  • Patent number: 5550244
    Abstract: Substituted (herbicidally active) sulphonylaminocarbonyltriazolinones of the formula (I) ##STR1## in which R.sup.1 represents hydrogen, hydroxyl or amino, or represents an optionally substituted radical from the group comprising alkyl, alkenyl, alkinyl, alkoxy, alkenyloxy, alkylamino, dialkylamino, cycloalkyl, cycloalkyloxy, cycloalkylamino, cycloalkylalkyl, aryl or arylalkyl,R.sup.2 represents hydrogen, hydroxyl, mercapto, amino or halogen, or represents an optionally substituted radical from the group comprising alkyl, alkenyl, alkinyl, alkoxy, alkenyloxy, alkinyloxy, alkylthio, alkenylthio, alkinylthio, alkylsulphinyl, alkylsulphonyl, alkylamino, dialkylamino, cycloalkyl, cycloalkenyl, cycloalkyloxy, cycloalkenyloxy, cycloalkylthio, cycloalkenylthio, cycloalkylamino, cycloalkenylamino, cycloalkylalkyl, cycloalkenylalkyl, aryl, aryloxy, arylthio, arylamino, arylalkyl, arylalkyloxy, arylalkylthio or arylalkylamino, andR.sup.
    Type: Grant
    Filed: December 14, 1994
    Date of Patent: August 27, 1996
    Assignee: Bayer Aktiengesellschaft
    Inventors: Joachim Kluth, Klaus-Helmut M uller
  • Patent number: 5550241
    Abstract: The present invention relates to novel adducts of cyclic carbonyl monomers with substituted olefins, which also are useful as solution viscosifiers.
    Type: Grant
    Filed: March 18, 1993
    Date of Patent: August 27, 1996
    Assignee: Exxon Research and Engineering Company
    Inventor: Stanley J. Brois
  • Patent number: 5543533
    Abstract: Photochromic products belonging to the group of chromenes having general formula (I): ##STR1##
    Type: Grant
    Filed: June 2, 1994
    Date of Patent: August 6, 1996
    Assignee: Great Lakes Chemical Italia S.r.l.
    Inventors: Pietro Allegrini, Nereo Nodari, Luciana Crisci, Vincenzo Malatesta
  • Patent number: 5541196
    Abstract: Substituted quinolines having formula (1), wherein R.sub.1, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 each independently represent a hydrogen atom, a linear or branched C.sub.1-7 alkyl, alkenyl, epoxy-alkyl or mono/polyalcohol group; an amine group or an amide group, an OR group in which R is hydrogen or a C.sub.1-7 alkyl or alkenyl group or a phenyl group; and R.sub.2 is an OR group in which R is as defined above, or a C.sub.1-7 alkyl alkenyl or epoxyalkyl group, a phenyl, phenol, methylenedioxyphenyl, or dimethoxyphenyl group, or a C.sub.1-7 alkyl, alkenyl or epoxyalkyl group, a phenyl, phenol, methylenedioxyphenyl, or dimethoxphenyl group or a C.sub.1-7 alkyl, alkenyl or epoxy-alklyl group comprising at least one of the following substituents: a C.sub.1-4 alkyl or alkenyl group; a phenyl, phenol, dimethylphenyl, dimethoxyphenyl or methylenedioxphenyl group; or an OR group in which R is hydrogen or a C.sub.1-4 alkyl or alkenyl group; or an NHR group in which R is hydrogen or a C.sub.
    Type: Grant
    Filed: June 9, 1994
    Date of Patent: July 30, 1996
    Assignee: Institut Francais de Recherche Scientifique Pour le Developpment en Cooperation (ORSTOM)
    Inventors: Alain Fournet, Alcira Angelo Barrios, Victoria Munoz, Reynald Hocquemiller, Fran.cedilla.ois Roblot, Jean Bruneton, Pascal Richomme, Jean Charles Gantier
  • Patent number: 5541323
    Abstract: Anhydride compounds which contain at least one rodlike mesogenic moiety and at least two anhydride groups per molecule, wherein each of said aromatic anhydride groups is linked to the mesogen via an ester linkage are prepared. These anhydride compounds are useful in curing epoxy resins to provide the cured products with one or more improved properties.
    Type: Grant
    Filed: January 18, 1995
    Date of Patent: July 30, 1996
    Assignee: The Dow Chemical Company
    Inventors: Robert E. Hefner, Jr., Jimmy D. Earls
  • Patent number: 5529978
    Abstract: Certain N-acetonyl-substituted-amides of the formula: ##STR1## wherein A is a heterocycle, a phenylalkyl, a phenylalkoxy, naphthyl, cycloalkyl, alkoxyalkyl, alkyl, haloalkyl or alkenyl group; X, Y and Z are selected from the group consisting of hydrogen, halo, cyano, thiocyano, isothiocyano, methylsulfonyloxy, thio(C.sub.1 -C.sub.2)alkyl, (C.sub.1 -C.sub.2)alkoxy, carbamoyl, dithiocarbamoyl, hydroxy, azide, trifluoromethylcarboxy, (C.sub.1 -C.sub.4)alkylcarbonyloxy, phenylcarbonyloxy, phenoxy, thiophenyl, imidazolyl or triazolyl group as described herein; R.sup.1 and R.sup.2 are each independently a hydrogen atom or a (C.sub.1 -C.sub.6)alkyl group; and compositions containing these amides are fungicidally active, particularly against phytopathogenic fungi.
    Type: Grant
    Filed: May 3, 1994
    Date of Patent: June 25, 1996
    Assignee: Rohm and Haas Company
    Inventor: Ashok K. Sharma
  • Patent number: 5523312
    Abstract: Disclosed herein are compounds and pharmaceutical compositions useful for combating picornaviruses and preventing or treating picornaviral infections. The compounds have the formula: ##STR1## wherein Het.sub.1 is chosen from the group consisting of oxazolyl, isoxazolyl, oxadiazolyl;Y is an alkylene bridge of 3 to 9 carbon atoms;Het.sub.2 is benzofuranyl or indolyl;R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, acetyl, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluromethyl, or cyano; andR.sub.3 is oxazolyl, oxadiazolyl, isoxazolyl or any of these substituted with alkyl, halo, alkoxyalkyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, thienyl, or fluoroalkyl;the N-oxide thereof or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: September 27, 1994
    Date of Patent: June 4, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Gee-Hong Kuo, Theodore J. Nitz, Michael Reuman
  • Patent number: 5519022
    Abstract: The invention concerns .alpha.,.alpha.-dialkylbenzyl derivatives of the formula I ##STR1## wherein Ar.sup.1 is phenyl or naphthyl, or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;A.sup.1 is a direct link to X.sup.1 or is (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;the phenylene group may optionally bear one or two substituents R.sup.3 ;each of R.sup.1 and R.sup.2, which may be the same or different is (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, fluoro-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl, provided that both of R.sup.1 and R.sup.2 are not methyl or fluoromethyl; andQ is cyano, amino, nitro, formyl, (1-4C)alkoxy, thiazolyl or (2-4C)alkanoyl;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
    Type: Grant
    Filed: November 10, 1993
    Date of Patent: May 21, 1996
    Assignees: Imperial Chemical Industries Plc, ICI Pharma
    Inventors: Philip N. Edwards, David Waterson
  • Patent number: 5514692
    Abstract: The invention discloses compounds of the formula ##STR1## wherein, Het.sub.1 is chosen from the group consisting of substituted or unsubstituted furyl, oxazolyl, isoxazolyl, oxadiazolyl, tetrazolyl, thiadiazolylY is an alkylene bridge of 3 to 9 carbon atoms.Het.sub.2 is quinolyl quinolyl substituted by R.sub.1 and R.sub.2 ;R.sub.1 and R.sub.2 are each individually chosen from hydrogen, halo, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl or cyano;R.sub.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: May 7, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Gee-Hong Kuo, Theodore J. Nitz, Michael Reuman
  • Patent number: 5514691
    Abstract: N-(4-halo-isoxazolyl)sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(4-halo-3-isoxazolyl)sulfonamides and N-(4-halo-5-isoxazolyl)benzenesulfonamides and methods for inhibiting the binding of an endothelin peptide to an endothelin receptor or increasing the activity of endothelin peptides by contacting the receptor with a sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.
    Type: Grant
    Filed: October 21, 1993
    Date of Patent: May 7, 1996
    Assignee: Immunopharmaceutics, Inc.
    Inventors: Ming F. Chan, Bore G. Raju, Rosario S. Castillo, Adam Kois, Chengde Wu, Yalamoori Venkatachalapathi, Erik J. Verner, Vitukudi N. Balaji
  • Patent number: 5506360
    Abstract: There is provided a process for the manufacture of 2-alkoxymethylacrolein compounds via the reaction of an appropriate alcohol and acrolein in the presence of an acid and a trisubstituted amine to form an intermediate and the subsequent reaction of the intermediate with formaldehyde in the presence of an acid and a disubstituted amine. There is also provided a process for the manufacture of 3-alkoxymethylquinolines from 2-alkoxymethylacrolein.
    Type: Grant
    Filed: November 5, 1993
    Date of Patent: April 9, 1996
    Assignee: American CYanamid Company
    Inventors: Henry L. Strong, David A. Cortes, Zareen Ahmed
  • Patent number: 5506240
    Abstract: The invention relates to N-acyl-N-heterocyclylalkylamino acids of the formula ##STR1## The compounds and their pharmaceutically acceptable salts can be used as antihypertensives, agents for the treatment of glaucoma, or for increasing the flow of the retinal ocular fluid.
    Type: Grant
    Filed: July 27, 1993
    Date of Patent: April 9, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Tibur Schmidlin, Paul Zbinden, Peter Buhlmayer
  • Patent number: 5502196
    Abstract: The invention relates to pyrrolo 3,4-c!pyrroles of formula ##STR1## wherein A and B are each independently of the other a group of formula ##STR2## or Q, wherein Q is a 5- or 6-membered heterocyclic aromatic amine oxide radical which is unsubstituted or substituted by one, two or three C.sub.1 -C.sub.18 alkyl, C.sub.1 -C.sub.18 alkoxy or ##STR3## and which may contain one or two fused benzene rings, R.sub.1 and R.sub.2 are each independently of the other hydrogen, halogen, C.sub.1 -C.sub.18 alkyl, C.sub.1 -C.sub.18 alkoxy, C.sub.1 -C.sub.18 alkylmercapto, --CN, --NO.sub.2 or trifiuoromethyl, D and E are each independently of the other hydrogen, C.sub.1 -C.sub.18 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.7 -C.sub.10 aralkyl, unsubstituted phenyl or phenyl which is substituted by chloro, bromo, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.4 alkoxy, trifiuoromethyl or nitro, with the proviso that at least one of the sustituents A and B is an amine oxide radical Q.
    Type: Grant
    Filed: March 14, 1995
    Date of Patent: March 26, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Zhimin Hao, Abul Iqbal, Rudolf Kirchmayr
  • Patent number: 5492915
    Abstract: This invention relates to compounds having selective LTB.sub.4 antagonist properties. Therapeutic compositions comprising said compounds and methods for the treatment of disorders involving LTB.sub.4 agonist-mediated activity utilizing said compositions wherein the compounds are described by the formula ##STR1## wherein R.sub.4, X, R, Y, R', Q, m and n are herein defined, and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: October 6, 1994
    Date of Patent: February 20, 1996
    Assignee: Rhone-Poulenc Rorer S.A.
    Inventors: Norbert Dereu, Wolfram Hendel, Richard Labaudiniere
  • Patent number: 5488057
    Abstract: The present invention provides novel aryl- and heteroarylethenylene derivatives which are useful as tyrosine kinase activity inhibitors.
    Type: Grant
    Filed: August 23, 1994
    Date of Patent: January 30, 1996
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Franco Buzzetti, Antonio Longo, Maristella Colombo
  • Patent number: 5478843
    Abstract: The invention concerns a thiazole derivative of the formula I ##STR1## wherein Q is 2-oxo-1,2,3,4-tetrahydroquinolin-6-yl or 2-oxo-1,2-dihydroquinolin-6-yl which bears on the nitrogen atom at the 1-position a (1-4C)alkyl substituent;X.sup.1 is thio, sulphinyl or sulphonyl;Ar is thiazolediyl;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which together with the carbon atom to which A.sup.2 and A.sup.3 are attached define a ring having 5 or 6 ring atoms, wherein A.sup.2 and A.sup.3, which may be the same or different, each is (1-3C)alkylene and X.sup.2 is oxy, and which ring may bear one or two (1-4C)alkyl substituents;or a pharmaceutically-acceptable salt thereof;processes for their preparation; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
    Type: Grant
    Filed: July 20, 1994
    Date of Patent: December 26, 1995
    Assignees: Zeneca Limited, Zeneca Pharma S.A.
    Inventor: Thomas G. C. Bird
  • Patent number: 5475007
    Abstract: Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions and inducing anesthesia are disclosed by administering to an animal in need of such treatment a substituted or unsubstituted 1,2,3,4-tetrahydroquinoline-2,3,4-trione-3 or 4-oxime or pharmaceutically acceptable salts thereof which have high binding to the glycine receptor.
    Type: Grant
    Filed: May 28, 1993
    Date of Patent: December 12, 1995
    Assignees: The Regents of the University of California, State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and the University of Oregon
    Inventors: Sui X. Cai, John F. W. Keana, Eckard Weber
  • Patent number: 5466701
    Abstract: Compounds having the structural formula ##STR1## which inhibit the enzymatic activity of proteolytic enzymes, and processes for preparation thereof, method of use thereof in treatment of degenerative diseases and pharmaceutical compositions thereof are disclosed.
    Type: Grant
    Filed: June 22, 1994
    Date of Patent: November 14, 1995
    Assignee: Sterling Winthrop Inc.
    Inventors: Dennis J. Hlasta, James H. Ackerman, Albert J. Mura, Ranjit C. Desai
  • Patent number: 5464853
    Abstract: N-(5-isoxazolyl)biphenylsulfonamides and N-(3-isoxazolyl)biphenylsulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(5-isoxazolyl)biphenylsulfonamides and N-(3-isoxazolyl)biphenylsulfonamides and methods for inhibiting the binding of an endothelin peptide to an endothelin receptor or increasing the activity of endothelin peptides by contacting the receptor with a sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.
    Type: Grant
    Filed: October 21, 1993
    Date of Patent: November 7, 1995
    Assignee: ImmunoPharmaceutics, Inc.
    Inventors: Ming F. Chan, Bore G. Raju, Rosario S. Castillo, Adam Kois, Chengde Wu, Vitukudi Balaji
  • Patent number: 5461055
    Abstract: Compounds of the formula ##STR1## wherein R.sub.3, R.sub.4, J, K, Z, and Het are as set forth herein are described.The compounds of formula I are useful as agents in the treatment of fungal infections.
    Type: Grant
    Filed: June 3, 1994
    Date of Patent: October 24, 1995
    Assignee: Schering Corporation
    Inventors: Alan B. Cooper, Anil K. Saksena, Raymond Lovey, Viyyoor Girijavallabhan, Ashit Ganguly
  • Patent number: 5444071
    Abstract: The invention concerns pharmaceutically useful novel compounds of the formula I, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, Ra, A, X and Z have the various meanings defined herein, and their non-toxic salts, and pharmaceutical compositions containing them. The novel compounds are of value in treating conditions such as hypertension and congestive heart failure. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.
    Type: Grant
    Filed: May 4, 1993
    Date of Patent: August 22, 1995
    Assignee: Imperial Chemical Industries PLC
    Inventors: David A. Roberts, Simon T. Russell, Robert J. Pearce
  • Patent number: 5434162
    Abstract: Compounds characterized as quinolinyl- or isoquinolinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension and are of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; X is selected from oxygen atom and methylene; G is a quinolinyl or isoquinolinyl group; R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; R.sub.2 is phenylmethyl; each of R.sub.3 and R.sub.5 is hydrido; R.sub.4 is--(CH.sub.2).sub.q --C--V;V is selected from hydrido and methyl; R.sub.6 is cyclohexylmethyl; R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; q is a number selected from zero through three, inclusive; and n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: September 13, 1993
    Date of Patent: July 18, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, Robert E. Manning
  • Patent number: 5430153
    Abstract: The present invention relates to novel 2-quinolinone derivanves of the following general formula(I) useful in agriculture, especially as fungicides but also as insecticides and miticides. ##STR1## wherein, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen, halogen, C.sub.1 -C.sub.10 alkyl, branched C.sub.c -C.sub.4 alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 haloalkoxy, C.sub.1 -C.sub.3 alkylthio, C.sub.1 -C.sub.3 haloallcylthio, NO.sub.2, CN, alkoxy carbonyl, phenyl, substituted phenyl, phenoxy, substituted phenoxy, benzenesulfonyl, benzyi, substituted benzyl or morpholine;R.sub.5 is C.sub.1 -C.sub.6 alkyl, branched C.sub.3 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, phenyl, substituted phenyl, benzyl or phenylthio methyl: andX is S(O)nR.sub.6, OR.sub.9 or NAB:wherein.n is 0 or 1;R.sub.6, R.sub.9, A and B are defined within the description.
    Type: Grant
    Filed: February 3, 1993
    Date of Patent: July 4, 1995
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Chwang S. Pak, Eun B. Choi, Heui C. Yang, Gyu H. Yon, Ge H. Lee, Hyeon K. Lee, Sung K. Kim, Yeon S. Lee, Kwang W. Lee, Young R. Chung, Heung T. Kim
  • Patent number: 5412104
    Abstract: Compounds useful as antihypertensive agents and useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Methods of treating a viral infection using compounds represented by Formula 1.0 are disclosed.Also disclosed are methods of treating hypertension using compounds of Formula 1.0 wherein R is selected from the group consisting of H, halogen and --C(O)OR.sup.6 ; and R.sup.1 is selected from the group consisting of --OR.sup.14, --O(CH.sub.2).sub.a C(H).sub.3-i Z.sub.i and --O(CH.sub.2).sub.h N(R.sup.15).sub.2.
    Type: Grant
    Filed: March 1, 1993
    Date of Patent: May 2, 1995
    Assignee: Schering Corporation
    Inventors: Adriano Afonso, Jay Weinstein, Margaret J. Gentles
  • Patent number: 5410054
    Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.
    Type: Grant
    Filed: July 20, 1993
    Date of Patent: April 25, 1995
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Rick Friesen, Robert N. Young, Yves Girard, Marc Blouin, Daniel Dube
  • Patent number: 5401848
    Abstract: Novel indane and quinoline derivatives, useful, for example, as antiischemic agents, having the formula ##STR1## where A, X, R.sub.1 -R.sub.7 are as defined herein, are disclosed.
    Type: Grant
    Filed: October 15, 1991
    Date of Patent: March 28, 1995
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: RE35177
    Abstract: A pyridine-compound is reacted with fluorine together with a .[.Bronsted.]. .Iadd.Bronsted .Iaddend.acid-compound or Lewis acid to form a N-fluoropyridinium salt which is very active to other compounds but is very selective for the preparation of a desired product and this product is very useful for a fluorine-introducing agent which makes it useful for the preparation of fluoro-compounds such as thyroid inhibitor.
    Type: Grant
    Filed: February 17, 1994
    Date of Patent: March 12, 1996
    Assignees: Sagami Chemical Research Center, Chichibu Onoda Cement Corporation
    Inventors: Teruo Umemoto, Kyoichi Tomita, Kosuke Kawada, Ginjiro Tomizawa