Patents Examined by Matthew V. Grumbling
  • Patent number: 5792863
    Abstract: An acridine derivative metal complex of formula 1 or formula 2 having a large absorption in the near-infrared range and a reduced absorption in the visible range, which acridine derivative metal complex is used in a transparent recording medium: ##STR1## where M is a metal atom, and X is a negative ion.
    Type: Grant
    Filed: April 15, 1996
    Date of Patent: August 11, 1998
    Assignee: Nippon Paper Industries Co., Ltd.
    Inventors: Reiji Ohashi, Yukiko Ryu, Tomoaki Nagai, Hidetoshi Yoshioka
  • Patent number: 5792771
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction and particularly KDR/FLK-1 receptor signal transduction in order to regulate and/or modulate vasculogenesis and angiogenesis. The invention is based, in part, on the demonstration that KDR/FLK-1 tyrosine kinase receptor expression is associated with endothelial cells and the identification of vascular endothelial growth factor (VEGF) as the high affinity ligand of FLK-1. These results indicate a major role for KDR/FLK-1 in the signaling system during vasculogenesis and angiogenesis. Engineering of host cells that express FLK-1 and the uses of expressed FLK-1 to evaluate and screen for drugs and analogs of VEGF involved in FLK-1 modulation by either agonist or antagonist activities is also described.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: August 11, 1998
    Assignees: Sugen, Inc., Yissum Research Development Co. of the Hebrew University of Jerusalem
    Inventors: Harald App, Gerald M. McMahon, Peng Cho Tang, Aviv Gazit, Alexander Levitzki
  • Patent number: 5789415
    Abstract: Compounds of the formula ##STR1## wherein: Q is naphthyl, heterocyclic or heterobicyclic; R.sup.1 and R.sup.2, when taken separately, are hydrogen, hydroxy, alkyl, alkylthio, alkylsulfinyl, alkylsulfonyl, phenyl, heterocyclic or heterobicyclic; R.sup.1 and R.sup.2, when taken together, form a carbocyclic, carbobicyclic, heterocyclic or heterobicyclic group; R.sup.3 is --(CH.sub.2).sub.n COR.sup.4, tetrazolyl, alkyltetrazolyl, triazolyl, alkyltriazolyl, --(CH.sub.2).sub.n CH.sub.2 OH, --SO.sub.2 R.sup.4, --SO.sub.2 NR.sup.5 R.sup.6 or --NHSO.sub.2 R.sup.7 ; R.sup.4 is hydrogen, hydroxy, --NR.sup.5 R.sup.6, --NHSO.sub.2 R.sup.7, alkoxy, alkylthio, --NR.sup.5 R.sup.6, --NHSO.sub.2 R.sup.7 or --OY; n is 0 to 5; Y is a pharmaceutically acceptable cation or a group hydrolyzable under physiological conditions; R.sup.5 and R.sup.6, when taken separately, are hydrogen, alkyl, --CONRR, --COOR or --CO(C.sub.6 H.sub.5); R.sup.5 and R.sup.6, when taken together, form an azacyclic ring; R.sup.
    Type: Grant
    Filed: January 11, 1996
    Date of Patent: August 4, 1998
    Assignee: Pfizer Inc.
    Inventors: Philip A. Carpino, Eric R. Larson, Banavara L. Mylari
  • Patent number: 5789410
    Abstract: Disclosed are compounds encompassed by the following general formula: ##STR1## wherein, A represents ethenylene, or A represents --X--CH.sub.2 --; where X is carbon or oxygen, provided that when X is oxygen, the oxygen is adjacent the 6-membered ring;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are inorganic or organic substituents; andR.sub.5 and R.sub.6 is are optionally substituted organic substituents; orNR.sub.5 R.sub.6 represents a carbocyclic or heterocyclic six membered ring optionally substituted with various orgainic or inorganic groups, which compounds can be used in the treatment of neuropsychological disorders.
    Type: Grant
    Filed: January 22, 1997
    Date of Patent: August 4, 1998
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Andrew Thurkauf
  • Patent number: 5786479
    Abstract: A process for producing a 6-substituted 2(1H)-quinoxalinone of the formula (I): ##STR1## wherein X is a halogen atom, a trihalogeno-substituted C.sub.1-5 alkyl group or a nitro group, which comprises reacting a 6-substituted 2(1H)-quinoxalinone-N-oxide of the formula (II): ##STR2## wherein X is as defined above, with an alkali metal hydrosulfide and/or an alkali metal sulfide in the presence of from 1 to 20 mol times of an alkali.
    Type: Grant
    Filed: August 13, 1996
    Date of Patent: July 28, 1998
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Isao Hashiba, Masataka Hatanaka
  • Patent number: 5783698
    Abstract: The present invention relates to a method for the synthesis of 1,3-disubstituted quinazolinedione derivatives which comprises:(a) reacting a haloformate functionalized polystyrene resin with a substituted anthranilic acid derivative under conditions effective to form a urethane-linkage;(b) reacting the product of step (a) with a primary amine under conditions effective to form an anthranilamide derivative;(c) heating the anthranilamide to effect intramolecular cyclization thereby liberating the 1,3-disubstituted quinazolinedione derivative from the resin into solution; and(d) isolating the 1,3-disubstituted quinazolinedione by filtration and solvent removal.
    Type: Grant
    Filed: January 7, 1997
    Date of Patent: July 21, 1998
    Assignee: Merck Sharp & Dohme Limited
    Inventor: Adrian Leonard Smith
  • Patent number: 5780628
    Abstract: A process for producing an dioxoquinazoline of following formula (II): ##STR1## wherein R.sub.1 and R.sub.2 independently represent a hydrogen atom, a halogen atom, a nitro group, a lower alkyl group, an aralkyl group, an alkoxy group, an alkoxylcarbonyl group or a group represented by YNR.sub.3 R.sub.4, wherein Y represents a direct bond, a lower alkylene group or a carbonyl group, and R.sub.3 and R.sub.4 independently represent a lower alkyl group or N, R.sub.3 and R.sub.4 may bond together to form a five- or six-membered heterocycle which comprises reacting an anthranylamide of formula (I): ##STR2## wherein X, R.sub.1 and R.sub.2 are as defined above.
    Type: Grant
    Filed: January 31, 1997
    Date of Patent: July 14, 1998
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Masashi Komatsu, Shinji Nishii, Hiroshi Ueda
  • Patent number: 5780634
    Abstract: Quinolin-2-yl benzoic acid compounds which are useful as intermediates of quinoline compounds having angiotensin II antagonist activity prepared by decarboxylating 2-(carboxyphenyl)-4-quinolinecarboxylic acid compounds in which a carboxyl group bonded to a phenyl group may be esterified, while a carboxyl group bonded to a quinoline ring is not esterified, and both rings may have one or more substituents inert to the decarboxylation reaction.
    Type: Grant
    Filed: October 27, 1995
    Date of Patent: July 14, 1998
    Assignees: The Green Cross Corporation, Asahi Glass Co., Ltd.
    Inventors: Yoshihisa Inoue, Hajime Ebisu, Naomichi Ishida, Norifumi Nakamura, Jun Sasaki, Takashi Okazoe, Yoshitomi Morizawa, Arata Yasuda, Shuzhong Wang, Tomoko Ito
  • Patent number: 5780482
    Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which one of A or B represents N and the other represents N or C--R.sub.3 ; R.sub.1 represents hydrogen, halo, alkyl, hydroxy, carboxyalkenyl, alkoxycarbonylalkenyl, hydroxyalkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxy, halogenated alkyl, carboxy, alkoxycarbonyl, alkanoylamino or carbamoylalkenyl; R.sub.2 represents hydrogen, alkyl, halo, alkoxy, hydroxy, alkanoyloxy, or phenoxy; R.sub.3 represents hydrogen or alkyl; R.sub.4 represents hydrogen, halo, alkoxycarbonyl, cyano, benzyloxycarbonyl, alkanoyl, benzoyl, alkyl, carboxy, alkylthio or carbamoyl; R.sub.5 represents hydrogen or alkyl; R.sub.9 represents hydrogen or alkyl; R.sub.10 represents phenyl, pyridyl or pyrimidinyl substituted by OR.sub.6 and optionally further substituted wherein R.sub.6 represents hydrogen, alkyl, alkoxycarbonyl or carbamoyl, alicyclic hydrocarbon, phenyl, cycloalkylalkyl, arylalkyl or pyridyl; or when R.sub.10 represents phenyl, OR.sub.
    Type: Grant
    Filed: December 21, 1995
    Date of Patent: July 14, 1998
    Assignee: Knoll Aktiengesellschaft
    Inventors: Bernard John Armitage, Bruce William Leslie, Thomas Kerr Miller, Christopher Morley
  • Patent number: 5776942
    Abstract: A rapid-acting remedy for asthma having a bronchodilating action contains at least one pyrido?2,3-d!pyrimidine derivative represented by the general formula (A) or pharmaceutically acceptable salts or metal complexes thereof as an effective component: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each of R.sup.1 and R.sup.2 is hydrogen, alkyl or benzyl; R.sup.3 is hydrogen, hydroxyl, dialkylaminomethyleneamino or --NH--X; X is hydrogen, alkyl, alkenyl, hydroxyl, amino, hydroxyalkyl, benzyl or acyl; R.sup.4 is hydrogen, alkyl, halogen, nitro, amino, hydroxyl, benzyloxy, cyano, carboxyl, alkoxycarbonyl, alkoxysulfonyl, aminosulfonyl, dialkylaminosulfonyl or sulfo; and R.sup.5 is hydrogen, alkyl or amino. The rapid-acting remedy for bronchial asthma is capable of relieving the symptom of laboring breath at the onset of asthma due to its excellent bronchodilating action.
    Type: Grant
    Filed: June 14, 1995
    Date of Patent: July 7, 1998
    Assignee: Nippon Zoki Pharmaceutical Co., Ltd.
    Inventors: Kazuhito Furukawa, Taisuke Hasegawa
  • Patent number: 5773616
    Abstract: Disclosed are compounds encompassed by the following general formula: ##STR1## wherein, A represents ethenylene, or A represents --X--CH.sub.2 --; where X is carbon or oxygen, provided that when X is oxygen, the oxygen is adjacent the 6-membered ring;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are inorganic or organic substituents; andR.sub.5 and R.sub.6 is are optionally substituted organic substituents; orNR.sub.5 R.sub.6 represents a carbocyclic or heterocyclic six membered ring optionally substituted with various orgainic or inorganic groups,which compounds can be used in the treatment of neuropsychological disorders.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: June 30, 1998
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Andrew Thurkauf
  • Patent number: 5773439
    Abstract: Novel amido-quinoxalinediones of the formula ##STR1## where R.sup.1 -R.sup.5, n and m have the meanings stated in the description, and the preparation thereof are described. The compounds are suitable for controlling diseases.
    Type: Grant
    Filed: December 20, 1996
    Date of Patent: June 30, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Wilfried Lubisch, Berthold Behl, Hans Peter Hofmann
  • Patent number: 5770599
    Abstract: The invention concerns quinazoline derivatives of the formula I ##STR1## wherein n is 1, 2 or 3 and each R.sup.2 is independently halogeno, trifluoromethyl or (1-4C)alkyl;R.sup.3 is (1-4C)alkoxy; andR.sup.1 is di-?(1-4C)alkyl!amino-(2-4C)alkoxy, pyrrolidin-1-yl-(2-4C)alkoxy, piperidino-(2-4C)alkoxy, morpholino-(2-4C)alkoxy, piperazin-1-yl-(2-4C)alkoxy, 4-(1-4C)alkylpiperazin-1-yl-(2-4C)alkoxy, imidazol-1-yl-(2-4C)alkoxy, di-?(1-4C)alkoxy-(2-4C)alkyl!amino-(2-4C)alkoxy, thiamorpholino-(2-4C)alkoxy, 1-oxothiamorpholino-(2-4C)alkoxy or 1,1-dioxothiamorpholino-(2-4C)alkoxy, and wherein any of the above-mentioned R.sup.1 substituents comprising a CH.sub.2 (methylene) group which is not attached to a N or O atom optionally bears on said CH.sub.
    Type: Grant
    Filed: April 26, 1996
    Date of Patent: June 23, 1998
    Assignee: Zeneca Limited
    Inventor: Kieth Hopkinson Gibson
  • Patent number: 5770603
    Abstract: The invention concerns quinazoline derivatives of the formula I ##STR1## wherein n is 1,2 or 3 and each R.sup.2 is independently halogeno, trifluoromethyl or (1-4C)alkyl;R.sup.1 is (1-4C)alkoxy;A is (1-4C)alkylene; andQ is a saturated, monocyclic 4-, 5-, 6- or 7-membered heterocyclic ring containing one or two oxygen heteroatoms, which ring optionally bears up to four (1-4C)alkyl substituents; or a pharmaceutically-acceptable salt thereof;processes for their preparation, pharmaceutical compositions containing them and the use of their receptor tyrosine kinase inhibitory properties in the treatment of proliferative disease such as cancer.
    Type: Grant
    Filed: April 10, 1997
    Date of Patent: June 23, 1998
    Assignee: Zeneca Limited
    Inventor: Keith Hopkinson Gibson
  • Patent number: 5770602
    Abstract: A compound represented by the general formula: ##STR1## wherein Y represents a nitrogen atom or C--G (G represents a carboxyl group which may be esterified); ring R is a nitrogen-containing unsaturated heterocyclic group which may be substituted for; each of rings A and B may have a substituent; n represents an integer from 1 to 4; k represents the integer 0 or 1, or a salt thereof, which serves well as an anti-inflammatory agent, particularly a therapeutic agent for arthritis.
    Type: Grant
    Filed: May 8, 1995
    Date of Patent: June 23, 1998
    Assignee: Takeda Chemical Industries
    Inventors: Takashi Sohda, Haruhiko Makino, Atsuo Baba
  • Patent number: 5770554
    Abstract: All purpose cleaning or microemulsion compositions more environmentally friendly, which is especially effective in the removal of a mixture of oil and kaolin soil, contains an analephotropic negatively charged complex, a hydrocarbon ingredient, a cosurfactant, and water.
    Type: Grant
    Filed: July 9, 1996
    Date of Patent: June 23, 1998
    Assignee: Colgate-Palmolive Co.
    Inventors: Anne-Marie Misselyn, Patrick Durbut, Guy Broze
  • Patent number: 5767116
    Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or --O--; B is methylene or --O--; and g is 0, 1, 2, 3 or 4;R.sub.1, R.sub.2, R.sub.3, R.sub.4, U, Q and T are defined in claim 1.The compounds have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behaviour, panic attacks, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.
    Type: Grant
    Filed: June 5, 1996
    Date of Patent: June 16, 1998
    Assignee: Knoll Atkiengesellschaft
    Inventors: Frank Kerrigan, David John Heal, Keith Frank Martin
  • Patent number: 5767127
    Abstract: N.sub.1 -(1,2-cis-2-halogenocydopropyl)-substituted pyridonecarboxylic acid derivatives represented by formula (I) and the salts thereof are disclosed. These compounds have patent antibacterial activities against a wide variety of infectious bacteria, and are useful as antibacterial agents by oral or parenteral administration.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 16, 1998
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Isao Hayakawa, Youichi Kimura
  • Patent number: 5767142
    Abstract: The present invention provides anti-neoplastic topoisomerase I inhibitors of the formula: ##STR1## wherein Ar is (C.sub.6 -C.sub.12)aryl or (5- to 12-membered) heteroaryl comprising 1-3 N, S or non-peroxide O, wherein N is unsubstituted or is substituted with (C.sub.1 -C.sub.4)alkyl; X is H, CN, CHO, OH, acetyl, CF.sub.3, O(C.sub.1 -C.sub.4)alkyl, NO.sub.2, NH.sub.2, halogen or halo-(C.sub.1 -C.sub.4)alkyl; each Y is individually H, (C.sub.1 -C.sub.4)alkyl or aralkyl; Y' is H or (C.sub.1 -C.sub.4)alkyl; n is 0 or 1; and each Z is individually H, (C.sub.1 -C.sub.4)alkyl, halogen or halo(C.sub.1 -C.sub.4)alkyl; or a pharmaceutically acceptable salt therein.
    Type: Grant
    Filed: March 20, 1996
    Date of Patent: June 16, 1998
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Leroy Fong Liu, Qun Sun
  • Patent number: 5763444
    Abstract: Novel compound of formula I and pharmaceutically acceptable salts thereof are useful CNS agents: ##STR1## wherein X is CH or N;X' is CH or a direct covalent link;Y is CH, CH.sub.2 or N;Y' is N, NH, O or S;R.sup.1 is H, Br, Cl, F, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxycarbonyl, CN, CONH.sub.2 or CH.sub.3 SO.sub.2 NH;n is 2 or 3;R.sup.2 is H or C.sub.1-4 alkyl;R.sup.3 is C.sub.1-4 alkoxy;R.sup.4 is H, Br, Cl, or F; andZ is CH or N.
    Type: Grant
    Filed: August 13, 1996
    Date of Patent: June 9, 1998
    Assignee: Bristol-Myers Squibb Company
    Inventors: David W. Smith, Joseph P. Yevich