Patents Examined by Tamthom T. Ngo
  • Patent number: 5714487
    Abstract: This invention relates to compounds of formula I ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, X, m and n are defined as in the specification, their pharmaceutically acceptable salts and pharmaceutical compositions containing such compounds or their salts.
    Type: Grant
    Filed: December 23, 1996
    Date of Patent: February 3, 1998
    Assignee: Pfizer Inc.
    Inventor: Mark A. Sanner
  • Patent number: 5710156
    Abstract: The invention is concerned with the compounds having the formula ##STR1## the pharmaceutically acceptable acid addition salts and the stereochemically isomeric form thereof, wherein X and Y are CH or N; R.sup.1, R.sup.2 and R.sup.3 are hydrogen or C.sub.1-4 alkyl; R.sup.4 and R.sup.5 are hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, hydroxy, trifluoromethyl, trifluoromethyloxy or difluoromethyloxy; R.sup.6 is C.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.1-4 alkyloxyC.sub.1-6 alkyl, phenyl or phenylC.sub.1-4 alkyl; Z is C.dbd.O or CHOH; and ##STR2## compositions comprising said compounds, processes for preparing the same and the use of these compounds for treating Helicobacter related diseases.
    Type: Grant
    Filed: September 20, 1996
    Date of Patent: January 20, 1998
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jan Heeres, Joseph Hector Mostmans, Robert Jozef Maria Hendrickx, Louis Jozef Elisabeth Van der Veken, Raymond Antoine Stokbroekx, Marcel Jozef Maria Van de Aa
  • Patent number: 5710336
    Abstract: A process, and variations thereof, for the preparation of 5,6-dihydroxy-2-amino-1,2,3,4-tetrahydronaphthalene derivatives of formula (I), wherein R.sub.1, R.sub.2, R.sub.3 can independently be hydrogen or lower alkyl.
    Type: Grant
    Filed: October 24, 1996
    Date of Patent: January 20, 1998
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Paolo Chiesi, Paolo Ventura, Vittorino Servadio, Maurizio Del Canale, Renato De Fanti, Gabriele Amari
  • Patent number: 5708170
    Abstract: Arthropodicidal carboxanilides of Formula I or II: ##STR1## wherein: Q is selected from the group ##STR2## A, E, G, X, X.sup.1, Y, Z, Z.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and n are as defined in the text, arthropodicidal compositions containing said compounds and a method for using the compounds to control arthropods.
    Type: Grant
    Filed: May 23, 1995
    Date of Patent: January 13, 1998
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Gary David Annis, William Eldo Barnette, Stephen Frederick McCann, Keith Dumont Wing
  • Patent number: 5700809
    Abstract: Compounds of formula I are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia.
    Type: Grant
    Filed: August 29, 1995
    Date of Patent: December 23, 1997
    Assignee: Merck Sharp & Dohme, Ltd.
    Inventors: Paul David Leeson, Adrian Leonard Smith, Mark Peter Ridgill, Raymond Baker, Neil Roy Curtis, Janusz Jozef Kulagowski
  • Patent number: 5698564
    Abstract: Diphenyl disulfide compounds having an inhibiting activity against the production of Interleukin-1.beta. (IL-1.beta.) or the release of Tumor Necrosis Factor.alpha. (TNF.alpha.), which are useful in the treatment or prophylaxis of the diseases such as chronic rheumatism and sepsis are described.
    Type: Grant
    Filed: December 21, 1995
    Date of Patent: December 16, 1997
    Assignee: Nisshin Flour Milling Co., Ltd.
    Inventors: Koichi Katsuyama, Masato Ariga, Yukio Saito, Shigeo Hatanaka, Toshihiro Takahashi
  • Patent number: 5698741
    Abstract: An improved synthesis of a highly potent HIV reverse transcription inhibitor is disclosed, involving an acetylide and a trifluoromethyl ketone which produces a chiral product in the presence of a chiral amino alcohol.
    Type: Grant
    Filed: July 15, 1996
    Date of Patent: December 16, 1997
    Assignee: Merck & Co. Inc.
    Inventors: Andrew S. Thompson, Edward G. Corley, Edward J. J. Grabowski, Nobuyoshi Yasuda
  • Patent number: 5691344
    Abstract: The present invention is concerned with compounds of formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, the N-oxides thereof and the stereochemically isomeric forms thereof, wherein .dbd.a.sub.1 --a.sub.2 .dbd.a.sub.3 --a.sub.4 .dbd. is a bivalent radical of formula:.dbd.N--CH.dbd.CH--CH.dbd. (a),.dbd.CH--N.dbd.CH--CH.dbd. (b),.dbd.CH--CH.dbd.N--CH.dbd. (c),.dbd.CH--CH.dbd.CH--N.dbd. (d),wherein in said bivalent radicals one or two hydrogen atoms can be substituted by halo, hydroxy, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is C.sub.1-5 alkanediyl; Alk.sup.2 is C.sub.2-15 alkanediyl; Q is a five- or six-membered heterocyclic ring containing at least one nitrogen atom or a radical of formula ##STR2## wherein R.sup.4 is hydrogen, cyano, aminocarbonyl or C.sub.1-6 alkyl; R.sup.5 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.
    Type: Grant
    Filed: January 24, 1996
    Date of Patent: November 25, 1997
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Guy Rosalia Eugene Van Lommen, Francisco Javier Fernandez-Gadea, Jose Ignacio Andres-Gil, Maria Encarnacion Matesanz-Ballesteros
  • Patent number: 5688818
    Abstract: Provision of a succinamic acid compound of the formula (1) ##STR1## wherein R.sup.1 is an alkyl or a lower alkenyl and R.sup.2 is an optionally esterified carboxyl, a pharmaceutically acceptable salt thereof, an agent for the prophylaxis and/or treatment of the complications of diabetes, comprising, as an active ingredient, the succinamic acid compound or a pharmaceutically acceptable salt thereof, an aldose reductase inhibitor comprising, as an active ingredient, the succinamic acid compound or a pharmaceutically acceptable salt thereof, and a method for producing the succinamic acid compound or a pharmaceutically acceptable salt thereof. The novel succinamic acid compounds of the formula (1) of the present invention and pharmaceutically acceptable salts thereof have a strong aldose reductase activity-inhibitory in mammals such as human, and show superior safety.
    Type: Grant
    Filed: March 14, 1996
    Date of Patent: November 18, 1997
    Assignees: Senju Pharmaceutical Co., Ltd., The Green Cross Corporation
    Inventors: Hiroshi Hosono, Toshiyuki Nishio, Hiromichi Ishikawa, Yoshiyuki Nakamura, Tetsuo Matsui
  • Patent number: 5686466
    Abstract: A novel compound of the formula: ##STR1## wherein Ar represents an optionally substituted tricyclic condensed benzene ring group which includes at least one heterocyclic ring as a component ring; n represents an integer from 2 to 10; R.sup.1 represents H or an optionally substituted hydrocarbon group, which may be different from one another in the repetition of n; and Y represents an optionally substituted 4-piperidinyl, 1-piperazinyl or 4-benzyl-1-piperidinyl group, or a salt thereof, inhibiting excellent cholinesterase inhibitory activity and monoamine reuptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.
    Type: Grant
    Filed: March 20, 1996
    Date of Patent: November 11, 1997
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Giichi Goto, Yuji Ishihara, Keisuke Hirai
  • Patent number: 5679794
    Abstract: Compounds possessing both a hindered amine moiety, such as a derivative of 2,2,6,6-tetramethylpiperidine, and a hydroxylamine moiety where the N-hydroxy group is not attached to a nitrogen atom in a piperidine ring are valuable stabilizers for protecting polymer compositions against the deleterious effects of actinic light and from the adverse effects of high temperature polymer processing environments.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: October 21, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Joseph Suhadolnik, Ramanathan Ravichandran, Valerio Borzatta, Graziano Vignali
  • Patent number: 5677309
    Abstract: The present invention encompasses structures of the Formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: X is oxygen, H.sub.2, or sulfur;Y is oxygen or sulfur;W is alkyl, arylalkyl, or heteroarylalkyl, each of which is optionally substituted; orW is aryl or heteroaryl; ##STR2## wherein: Z.sub.1, Z.sub.2, Z.sub.3, and Z.sub.4 independently represent nitrogen or C--R.sub.a, whereeach R.sub.a independently is hydrogen, an inorganic substitutent or an optionally substituted aromatic group;n is 1, 2 or 3; andR.sub.b is hydrogen, alkyl, or an optionally substituted aromatic group,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.
    Type: Grant
    Filed: March 22, 1996
    Date of Patent: October 14, 1997
    Assignee: Neurogen Corporation
    Inventors: Paul Chen, Alan Hutchison
  • Patent number: 5670503
    Abstract: New heterocyclic derivatives of the formula: ##STR1## wherein R.sup.1 is aryl which may have suitable substituent(s) or heterocyclic group which may have suitable substituent(s),R.sup.2 is aryl which may have suitable substituent(s) or heterocyclic group which may have suitable substituent(s),R.sup.3 is hydrogen or acyl,R.sup.4 is hydrogen, lower alkyl, cyclo(lower)alkyl, cyclo(lower)alkyl-(lower)alkyl, carboxy(lower)alkyl, protected carboxy(lower)alkyl, ar(lower)alkyl which may have suitable substituent(s), ar(lower)alkenyl, bridged tricyclicalkyl, heterocyclic group which may have suitable substituent(s), acyl, or a group of the formula ##STR2## (in which A is lower alkylene), and R.sup.5 is hydrogen or lower alkyl,and a pharmaceutically acceptable salt thereof which are useful as a medicament.
    Type: Grant
    Filed: August 21, 1995
    Date of Patent: September 23, 1997
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Yoshio Kawai, Hitoshi Yamazaki, Hirokazu Tanaka, Teruo Oku
  • Patent number: 5668127
    Abstract: Methods, compounds and compositions are provided for inhibiting the growth of pathogenic mycobacteria in vitro and of treatment of pathogenic bacterial infections, such as mycobacterial and clostridium infections, in vivo using bicyclic nitroimidazole compounds of the formula (II): ##STR1## wherein R.sub.1 is hydrogen, halogen, loweralkyl, haloloweralkyl, cycloalkyl, heterocycle, substituted heterocycle and heterocyclicalkyl; X is oxygen, sulfur or NK.sub.2, where R.sub.2 is hydrogen, loweralkyl, aryl, cycloalkyl, heterocycle, substituted heterocycle, heterocyclicalkyl, COR.sub.3 or SO.sub.2 R.sub.4 CONR.sub.4 R.sub.5, where R.sub.4 and R.sub.5 are independently selected from hydrogen, loweralkyl, aryl, alkylaryl, alkoxyalkyl, alkoxyaryl, alkoxyalkoxyaryl, alkylheterocycle, and alkoxyheterocycle; n is 1, 2 or 3; Y and Z are independently selected CH.sub.2, CO, CR.sub.4 R.sub.5 or NR.sub.4, where R.sub.4 and R.sub.
    Type: Grant
    Filed: June 26, 1995
    Date of Patent: September 16, 1997
    Assignee: PathoGenesis Corporation
    Inventors: William R. Baker, Cai Shaopei, Eric L. Keeler
  • Patent number: 5656627
    Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.
    Type: Grant
    Filed: March 17, 1995
    Date of Patent: August 12, 1997
    Assignee: Vertex Pharmaceuticals, Inc.
    Inventors: Guy W. Bemis, Julian M. C. Golec, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, David J. Livingston
  • Patent number: 5652363
    Abstract: The present invention relates to compounds of the formula ##STR1## and pharmaceutical compositions containing a therapeutically effective amount of the compounds in combination with a pharmaceutically acceptable carrier and a method for treating diseases mediated by platelet activating factor.
    Type: Grant
    Filed: October 2, 1996
    Date of Patent: July 29, 1997
    Assignee: C.D. Searle & Co.
    Inventors: Ish Kumar Khanna, Michael Allan Stealey, Richard Mathias Weier