Patents Examined by Tamthom T. Ngo
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Patent number: 5714487Abstract: 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: GrantFiled: December 23, 1996Date of Patent: February 3, 1998Assignee: Pfizer Inc.Inventor: Mark A. Sanner
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Patent number: 5710156Abstract: 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: GrantFiled: September 20, 1996Date of Patent: January 20, 1998Assignee: 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
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Patent number: 5710336Abstract: 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: GrantFiled: October 24, 1996Date of Patent: January 20, 1998Assignee: Chiesi Farmaceutici S.p.A.Inventors: Paolo Chiesi, Paolo Ventura, Vittorino Servadio, Maurizio Del Canale, Renato De Fanti, Gabriele Amari
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Patent number: 5708170Abstract: 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: GrantFiled: May 23, 1995Date of Patent: January 13, 1998Assignee: E. I. du Pont de Nemours and CompanyInventors: Gary David Annis, William Eldo Barnette, Stephen Frederick McCann, Keith Dumont Wing
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Patent number: 5700809Abstract: 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: GrantFiled: August 29, 1995Date of Patent: December 23, 1997Assignee: Merck Sharp & Dohme, Ltd.Inventors: Paul David Leeson, Adrian Leonard Smith, Mark Peter Ridgill, Raymond Baker, Neil Roy Curtis, Janusz Jozef Kulagowski
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Patent number: 5698564Abstract: 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: GrantFiled: December 21, 1995Date of Patent: December 16, 1997Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Koichi Katsuyama, Masato Ariga, Yukio Saito, Shigeo Hatanaka, Toshihiro Takahashi
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Patent number: 5698741Abstract: 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: GrantFiled: July 15, 1996Date of Patent: December 16, 1997Assignee: Merck & Co. Inc.Inventors: Andrew S. Thompson, Edward G. Corley, Edward J. J. Grabowski, Nobuyoshi Yasuda
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Patent number: 5691344Abstract: 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: GrantFiled: January 24, 1996Date of Patent: November 25, 1997Assignee: Janssen Pharmaceutica, N.V.Inventors: Guy Rosalia Eugene Van Lommen, Francisco Javier Fernandez-Gadea, Jose Ignacio Andres-Gil, Maria Encarnacion Matesanz-Ballesteros
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Patent number: 5688818Abstract: 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: GrantFiled: March 14, 1996Date of Patent: November 18, 1997Assignees: Senju Pharmaceutical Co., Ltd., The Green Cross CorporationInventors: Hiroshi Hosono, Toshiyuki Nishio, Hiromichi Ishikawa, Yoshiyuki Nakamura, Tetsuo Matsui
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Patent number: 5686466Abstract: 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: GrantFiled: March 20, 1996Date of Patent: November 11, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Yuji Ishihara, Keisuke Hirai
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Patent number: 5679794Abstract: 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: GrantFiled: June 6, 1995Date of Patent: October 21, 1997Assignee: Ciba-Geigy CorporationInventors: Joseph Suhadolnik, Ramanathan Ravichandran, Valerio Borzatta, Graziano Vignali
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Patent number: 5677309Abstract: 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: GrantFiled: March 22, 1996Date of Patent: October 14, 1997Assignee: Neurogen CorporationInventors: Paul Chen, Alan Hutchison
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Patent number: 5670503Abstract: 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: GrantFiled: August 21, 1995Date of Patent: September 23, 1997Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Yoshio Kawai, Hitoshi Yamazaki, Hirokazu Tanaka, Teruo Oku
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Patent number: 5668127Abstract: 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: GrantFiled: June 26, 1995Date of Patent: September 16, 1997Assignee: PathoGenesis CorporationInventors: William R. Baker, Cai Shaopei, Eric L. Keeler
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Patent number: 5656627Abstract: 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: GrantFiled: March 17, 1995Date of Patent: August 12, 1997Assignee: Vertex Pharmaceuticals, Inc.Inventors: Guy W. Bemis, Julian M. C. Golec, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, David J. Livingston
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Patent number: 5652363Abstract: 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: GrantFiled: October 2, 1996Date of Patent: July 29, 1997Assignee: C.D. Searle & Co.Inventors: Ish Kumar Khanna, Michael Allan Stealey, Richard Mathias Weier