Patents Examined by Philip I. Datlow
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Patent number: 5635505Abstract: A 1,4-benzoxazine-2-acetic acid compound of the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, a method for production thereof, and a pharmaceutical composition, an aldose reductase inhibitor and an agent for the prevention and/or treatment of the complications of diabetes, which contain the same. The compound (I) of the present invention and pharmaceutically acceptable salts thereof have aldose reductase inhibitory action and are superior in safety. Accordingly, they are useful as an agent for the prevention and/or treatment of the complications of diabetes such as faulty union of corneal injury, cataract, neurosis, retinopathy and nephropathy, in particular, cataract and neurosis.Type: GrantFiled: July 3, 1996Date of Patent: June 3, 1997Assignees: Senju Pharmaceutical Co., Ltd., The Green Cross CorporationInventors: Takahiro Kumonaka, Takema Hase, Tomoji Aotsuka, Toshio Kurihara, Yoshiyuki Nakamura, Tetsuo Matsui, Hiromichi Ishikawa, Fujio Kobayashi
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Patent number: 5635506Abstract: This invention relates to a compound useful for the treatment of tumors having the formula: ##STR1##Type: GrantFiled: November 18, 1993Date of Patent: June 3, 1997Assignee: Research Corporation Technologies, Inc.Inventors: David S. Alberts, Robert T. Dorr, William A. Remers, Salah M. Sami
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Patent number: 5635503Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of piperazine and homopiperazine derivatives of 4-phenyl-1,4-dihydropyridines of Formula (I). ##STR1## As antagonists of NPY-induced feeding behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.Type: GrantFiled: June 7, 1995Date of Patent: June 3, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Graham S. Poindexter, Marc Bruce, Graham Johnson, Michael Kozlowski, Karen LeBoulluec, Ivo Monkovic, Ramakrishna Seethala, Charles P. Sloan
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Patent number: 5631386Abstract: The residual level of alkylene oxide in the reaction mixture resulting from reaction of alkylene oxide with carbon dioxide to form alkylene carbonate is reduced by stripping with an inert gas such as carbon dioxide.Type: GrantFiled: August 2, 1996Date of Patent: May 20, 1997Assignee: ARCO Chemical Technology, L.P.Inventor: Vijai P. Gupta
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Patent number: 5629421Abstract: There are provided a hydrazone compound represented by formula (I), an electrophotographic photoreceptor which has a photosensitive layer containing the compound on an electrically conductive support, and an organic electroluminescent element containing the compound as a charge transporting material: ##STR1## wherein Ar.sub.1 represents a substituted or unsubstituted phenylene group, a substitued or unsubstituted naphthylene group, a substitued or unsubstituted biphenylene group, or a substituted or unsubstituted anthrylene group, Ar.sub.2 represents a substituted or unsubstituted aryl group, R.sub.1 and R.sub.2 each independently represents a hydrogen atom, a halogen atom, an unsubstituted alkyl group, or an unsubstituted alkoxy group, R.sub.3 represents an unsubstituted alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group, Z represents an ethylene group or a vinylene group, and n is 0 or 1.Type: GrantFiled: January 18, 1996Date of Patent: May 13, 1997Assignee: Hodagaya Chemical Co., Ltd.Inventors: Atsushi Takesue, Yasuo Murakami, Takanobu Watanabe, Mitsutoshi Anzai
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Patent number: 5627178Abstract: 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-[2,3-b][1,5]benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders of the central nervous system.Type: GrantFiled: February 13, 1995Date of Patent: May 6, 1997Assignee: Lilly Industries LimitedInventors: Jiban K. Chakrabarti, Terrence M. Hotten, David E. Tupper
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Patent number: 5624948Abstract: 1-(2-benzimidazolyl)-1,5-diazacyclooctane compounds represented by the formula: ##STR1## wherein X represents a hydrogen atom or a halogen atom; Y represents a covalent bond, a straight- or branched-chain alkylene group having 1 to 6 carbon atoms, or a straight- or branched-chain alkenylene group having 2 to 6 carbon atoms; R represents a hydrogen atom, or a straight- or branched-chain alkyl group having 1 to 6 carbon atoms; and pharmaceutically acceptable salts thereof. The compounds represented above are novel potent and long-lasting histamine HI-receptor antagonist with less-topical irritation, and can be topically administered by inhalation for the treatment of bronchial asthma.Type: GrantFiled: November 14, 1995Date of Patent: April 29, 1997Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hidetoshi Isawa, Nobuko Yanagi, Yasuo Takehana, Den-ichi Momose, Masaaki Satoh, Yoshinori Nonaka
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Patent number: 5624923Abstract: Tricyclic diazepines of the formula: ##STR1## wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.Type: GrantFiled: June 6, 1995Date of Patent: April 29, 1997Assignee: American Cyanamid CompanyInventors: Jay D. Albright, Marvin F. Reich, Fuk-Wah Sum, Efren G. Delos Santos
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Patent number: 5620973Abstract: A novel compound of the formula ##STR1## wherein Ar represents a tetracyclic fused heterocyclic group which may be substituted; R.sup.1 represents H or a hydrocarbon group which may be substituted; Y represents an amino or nitrogen-containing saturated heterocyclic group which may be substituted, its salt, inhibiting excellent cholinesterase inhibitory activity and monoamine uptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.Type: GrantFiled: October 25, 1994Date of Patent: April 15, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Yuji Ishihara, Masaomi Miyamoto
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Patent number: 5620976Abstract: The cyclic amide derivative is defined by the formula (I) or a salt thereof: R.sup.1 --(CH2)n--Z in which R.sup.1 is a group derived from a cyclic amide compound, substituted or unsubstituted, n is zero or an integer of 1 to 10 and Z is ##STR1## R.sup.2 being an aryl, a substituted aryl, a cycloalkyl or a heterocyclic group, m being an integer of 1 to 6, R.sup.3 being hydrogen or a lower alkyl, R.sup.4 being an aryl or a substituted aryl, a cycloalkyl or a heterocyclic group, p being an integer of 1 to 6, provided that the cyclic amide compound is quinazoline-on or quinazoline-dion, R2 and R4 are neither aryl nor substituted aryl. The cyclic amide compound is pharmacologically effective to prevent and treat diseases due to insufficiency of the central choline functions.Type: GrantFiled: May 25, 1995Date of Patent: April 15, 1997Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Masahiro Yonaga, Norio Karibe, Youichi Iimura, Satoshi Nagato, Atsushi Sasaki, Yoshiharu Yamanishi, Hiroo Ogura, Takashi Kosasa, Kumi Uchikoshi, Kiyomi Yamatsu
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Patent number: 5618812Abstract: Compounds of Formula (I), and salts and prodrugs thereof, wherein R.sup.1 represents H, optionally substituted C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; R.sup.2 is NHR.sup.12 or (CH.sub.2).sub.s R.sup.13 where 5 is 0, 1 or 2; R.sup.3 represents C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; R.sup.4 and R.sup.5 are H, C.sub.1-12 alkyl optionally substituted by NR.sup.9 R.sup.9' or an azacyclic or azabicyclic group, optionally substituted C.sub.4-9 cycloalkyl, C.sub.4-9 cycloalkyl C.sub.1-4 alkyl, aryl, arylC.sub.1-6 alkyl or azacyclic or azabicyclic groups, or R.sup.4 and R.sup.5 together form the residue of an optionally substituted azacyclic or azabicyclic ring system; x is 0, 1, 2 or 3; R.sup.12 is optionally substituted phenyl or pyridyl; R.sup.13 represents a group (A) wherein R.sup.14 is H or C.sub.1-6 alkyl; R.sup.15 is H, C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; and the dotted line is an optional covalent bond; are CCK and/or gastrin antagonists useful in therapy.Type: GrantFiled: January 26, 1995Date of Patent: April 8, 1997Assignee: Merck Sharp & Dohme, Ltd.Inventors: Jose L. Castro Pineiro, William R. Carling, Mark S. Chambers, Stephen R. Fletcher, Sarah C. Hobbs, Victor G. Matassa, Kevin W. Moore, Graham A. Showell, Michael G. Russell
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Patent number: 5612334Abstract: Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.Type: GrantFiled: June 2, 1995Date of Patent: March 18, 1997Assignee: American Cyanamid CompanyInventors: Jay D. Albright, John P. Dusza
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Patent number: 5612376Abstract: A method for visibly reducing a facial wrinkle by topically applying to the wrinkle 3-phenyllactic acid or a topically effective salt thereof.Type: GrantFiled: June 6, 1995Date of Patent: March 18, 1997Assignee: Tristrata Technology, Inc.Inventors: Ruey J. Yu, Eugene J. Van Scott
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Patent number: 5610299Abstract: This invention encompasses compounds of formula I: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## represents: ##STR3## where n is 0, 1, or 2; R.sub.1 and R.sub.2 are hydrogen or straight or branched chain alkyl groups;Y represents various organic and inorganic substituents;W represents an aromatic group substituted with various organic and inorganic substituents;A is CH or N;B is a substituted or unsubstituted carbon or N; andE is hydrogen or straight or branched alkyl groups.These 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 type drugs, and enhancement of alertness.Type: GrantFiled: December 21, 1995Date of Patent: March 11, 1997Assignee: Neurogen CorporationInventors: Charles Blum, Alan Hutchison
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Patent number: 5610156Abstract: Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.Type: GrantFiled: June 2, 1995Date of Patent: March 11, 1997Assignee: American Cyanamid CompanyInventors: Jay D. Albright, Aranapakam M. Venkatesan
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Patent number: 5610163Abstract: Compounds of the formula ##STR1## of which, in exemplary compounds, the thienyl group is attached via the 2-position and:(a) A is 3.alpha.-(6.beta., 7.beta.-epoxy)-tropanyl methobromide and R.sub.1 is 2-thienyl;(b) A is 3.alpha.-(6, 7dehydro)-tropanyl methobromide and R.sub.1 is 2-thienyl;(c) A is 3.beta.-tropanyl methobromide and R.sub.1 is 2-thienyl; and,(d) A is 3.alpha.-(N-isopropyl)-nortropanyl methobromide and R.sub.1 is cyclopentyl.These are anticholinergics. Administered by inhalation, they are useful for the treatment of chronic obstructive bronchitis or slight to moderately severe asthma. Administered by the intravenous or oral routes, they are useful for the treatment of vagally induced sinus bradycardia.Type: GrantFiled: March 16, 1995Date of Patent: March 11, 1997Assignee: Boehringer Ingelheim GmbHInventors: Rolf Banholzer, Rudolf Bauer, Richard Reichl
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Patent number: 5610158Abstract: Imidazo-benzoxazines of Formula (I) and pharmaceutically acceptable salts thereof. ##STR1## where Q is selected from (A) through (H) ##STR2## or pharmaceutically acceptable salts thereof wherein the R groups are as defined herein. The imidazo-benzoxazines, Formula (I), of the present invention are useful as anxiolytics and sedatives.Type: GrantFiled: August 3, 1994Date of Patent: March 11, 1997Assignee: The Upjohn CompanyInventors: Sharon N. Bisaha, Ronald B. Gammill
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Patent number: 5607926Abstract: The present invention includes novel (7R)-7-(acylamino)-3-(arylthio)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to .beta.-lactam antibiotics and are useful as antibacterial agents. The invention also relates to novel intermediates useful for making the novel compounds of the present invention and to novel methods for producing the novel compounds and intermediate compounds.Type: GrantFiled: March 29, 1995Date of Patent: March 4, 1997Assignee: Microcide Pharmaceuticals, Inc.Inventors: Scott J. Hecker, In-Seop Cho, Burton G. Christensen, Tomasz W. Glinka
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Patent number: 5608054Abstract: Transition metal complexes of meso-haloalkylporphyrins, wherein the haloalkyl groups contain 2 to 8 carbon atoms have been found to be highly effective catalysts for oxidation of alkanes and for the decomposition of hydroperoxides.Type: GrantFiled: March 17, 1995Date of Patent: March 4, 1997Assignee: Sun Company, Inc. (R&M)Inventors: Tilak Wijesekera, James E. Lyons, Paul E. Ellis, Jr., Manoj V. Bhinde
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Patent number: 5605897Abstract: Olanzapine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders of the central nervous system.Type: GrantFiled: February 13, 1995Date of Patent: February 25, 1997Assignees: Eli Lilly and Company, Lilly Industries LimitedInventors: Charles M. Beasley, Jr., Jiban K. Chakrabarti, Terrence M. Hotten, David E. Tupper