Patents Examined by Philip I. Datlow
  • Patent number: 5635505
    Abstract: 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: Grant
    Filed: July 3, 1996
    Date of Patent: June 3, 1997
    Assignees: Senju Pharmaceutical Co., Ltd., The Green Cross Corporation
    Inventors: Takahiro Kumonaka, Takema Hase, Tomoji Aotsuka, Toshio Kurihara, Yoshiyuki Nakamura, Tetsuo Matsui, Hiromichi Ishikawa, Fujio Kobayashi
  • Patent number: 5635506
    Abstract: This invention relates to a compound useful for the treatment of tumors having the formula: ##STR1##
    Type: Grant
    Filed: November 18, 1993
    Date of Patent: June 3, 1997
    Assignee: Research Corporation Technologies, Inc.
    Inventors: David S. Alberts, Robert T. Dorr, William A. Remers, Salah M. Sami
  • Patent number: 5635503
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: June 3, 1997
    Assignee: Bristol-Myers Squibb Company
    Inventors: Graham S. Poindexter, Marc Bruce, Graham Johnson, Michael Kozlowski, Karen LeBoulluec, Ivo Monkovic, Ramakrishna Seethala, Charles P. Sloan
  • Patent number: 5631386
    Abstract: 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: Grant
    Filed: August 2, 1996
    Date of Patent: May 20, 1997
    Assignee: ARCO Chemical Technology, L.P.
    Inventor: Vijai P. Gupta
  • Patent number: 5629421
    Abstract: 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: Grant
    Filed: January 18, 1996
    Date of Patent: May 13, 1997
    Assignee: Hodagaya Chemical Co., Ltd.
    Inventors: Atsushi Takesue, Yasuo Murakami, Takanobu Watanabe, Mitsutoshi Anzai
  • Patent number: 5627178
    Abstract: 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: Grant
    Filed: February 13, 1995
    Date of Patent: May 6, 1997
    Assignee: Lilly Industries Limited
    Inventors: Jiban K. Chakrabarti, Terrence M. Hotten, David E. Tupper
  • Patent number: 5624948
    Abstract: 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: Grant
    Filed: November 14, 1995
    Date of Patent: April 29, 1997
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Hidetoshi Isawa, Nobuko Yanagi, Yasuo Takehana, Den-ichi Momose, Masaaki Satoh, Yoshinori Nonaka
  • Patent number: 5624923
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: April 29, 1997
    Assignee: American Cyanamid Company
    Inventors: Jay D. Albright, Marvin F. Reich, Fuk-Wah Sum, Efren G. Delos Santos
  • Patent number: 5620973
    Abstract: 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: Grant
    Filed: October 25, 1994
    Date of Patent: April 15, 1997
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Giichi Goto, Yuji Ishihara, Masaomi Miyamoto
  • Patent number: 5620976
    Abstract: 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: Grant
    Filed: May 25, 1995
    Date of Patent: April 15, 1997
    Assignee: 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
  • Patent number: 5618812
    Abstract: 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: Grant
    Filed: January 26, 1995
    Date of Patent: April 8, 1997
    Assignee: 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
  • Patent number: 5612334
    Abstract: 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: Grant
    Filed: June 2, 1995
    Date of Patent: March 18, 1997
    Assignee: American Cyanamid Company
    Inventors: Jay D. Albright, John P. Dusza
  • Patent number: 5612376
    Abstract: A method for visibly reducing a facial wrinkle by topically applying to the wrinkle 3-phenyllactic acid or a topically effective salt thereof.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: March 18, 1997
    Assignee: Tristrata Technology, Inc.
    Inventors: Ruey J. Yu, Eugene J. Van Scott
  • Patent number: 5610299
    Abstract: 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: Grant
    Filed: December 21, 1995
    Date of Patent: March 11, 1997
    Assignee: Neurogen Corporation
    Inventors: Charles Blum, Alan Hutchison
  • Patent number: 5610156
    Abstract: 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: Grant
    Filed: June 2, 1995
    Date of Patent: March 11, 1997
    Assignee: American Cyanamid Company
    Inventors: Jay D. Albright, Aranapakam M. Venkatesan
  • Patent number: 5610163
    Abstract: 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: Grant
    Filed: March 16, 1995
    Date of Patent: March 11, 1997
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Rolf Banholzer, Rudolf Bauer, Richard Reichl
  • Patent number: 5610158
    Abstract: 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: Grant
    Filed: August 3, 1994
    Date of Patent: March 11, 1997
    Assignee: The Upjohn Company
    Inventors: Sharon N. Bisaha, Ronald B. Gammill
  • Patent number: 5607926
    Abstract: 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: Grant
    Filed: March 29, 1995
    Date of Patent: March 4, 1997
    Assignee: Microcide Pharmaceuticals, Inc.
    Inventors: Scott J. Hecker, In-Seop Cho, Burton G. Christensen, Tomasz W. Glinka
  • Patent number: 5608054
    Abstract: 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: Grant
    Filed: March 17, 1995
    Date of Patent: March 4, 1997
    Assignee: Sun Company, Inc. (R&M)
    Inventors: Tilak Wijesekera, James E. Lyons, Paul E. Ellis, Jr., Manoj V. Bhinde
  • Patent number: 5605897
    Abstract: 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: Grant
    Filed: February 13, 1995
    Date of Patent: February 25, 1997
    Assignees: Eli Lilly and Company, Lilly Industries Limited
    Inventors: Charles M. Beasley, Jr., Jiban K. Chakrabarti, Terrence M. Hotten, David E. Tupper