Patents Examined by Cecilia Shen
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Patent number: 5120845Abstract: The present invention relates to novel positive inotropic and lusitropic 3,5-dihydroimidazo[2,1-b]quinazolin-2(1H)-one derivatives having positive inotropic and lusitropic properties which are useful in the treatment of warm-blooded animals suffering from Congestive Heart Failure. Pharmaceutical compositions containing said compounds as an active ingredient. Methods of preparing said compounds and pharmaceutical compositions.Type: GrantFiled: July 24, 1991Date of Patent: June 9, 1992Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers
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Patent number: 5120736Abstract: The present invention relates to novel 4-methyl-5-[2-(4-phenylpiperazin-1-yl)ethyl]thiazole derivatives of the general formula ##STR1## in which R is selected from a hydrogen atom, an alkyl radical having from 2 to 7 carbon atoms and an aralkyl radical of which the aryl moiety preferably consists of phenyl and of which the alkyl moiety has from 1 to 4 carbon atoms, and to the pharmaceutically acceptable salts of these derivatives.It further relates to a method of preparing these products and to pharmaceutical compositions in which they are incorporated.These derivatives are applied especially in the preparation of drugs intended for the treatment of functional dysuria associated with hyperactivity of the .alpha.-adrenergic sympathetic nervous system.Type: GrantFiled: April 11, 1991Date of Patent: June 9, 1992Assignee: Institut de Recherches Chimiques et Biologiques AppliqueesInventors: Patrick Houziaux, Jean-Pierre Riffaud, Jean-Yves LaColle, Bernard Danree
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Patent number: 5120723Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.Type: GrantFiled: May 10, 1990Date of Patent: June 9, 1992Assignee: University of Southern CaliforniaInventors: Kelvin W. Gee, Michael B. Bolger
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Patent number: 5120860Abstract: .beta.-Hydroxyamines can be converted to the corresponding aziridines by contacting the amines with a molecular sieve, which has incorporated therein at least one alkali metal or alkaline metal, the preferred metal being cesium. Molecular sieves useful in the reaction include aluminosilicates, aluminophosphates and silicoaluminophosphates. The process is especially useful for the conversion of monoethanolamine to ethylenimine.Type: GrantFiled: December 18, 1987Date of Patent: June 9, 1992Assignee: Union Carbide Chemicals & Plastics Technology CorporationInventors: Kurt D. Olson, Steven W. Kaiser
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Patent number: 5120738Abstract: Compounds represented by general formula (I) below ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, each represent a hydrogen atom or a protective group for a hydroxyl group;R.sup.3 represents a saturated or unsaturated, linear, branched or cyclic, monovalent C.sub.5 .about.C.sub.25 -aliphatic hydrocarbon group which may be substituted with an aromatic group, or a group of formula ##STR2## where R.sup.4 represents a saturated or unsaturated, linear, branched or cyclic, monovalent C.sub.5 .about.C.sub.25 -aliphatic hydrocarbon group which may be substituted with an aromatic group, andR.sup.5 represents a hydrogen atom, or a saturated or unsaturated, linear, branched or cyclic, monovalent hydrovarbon group which may be substituted with an aromatic group;Q represents(a) a group of formula --X.sup.1 --A--Y.sup.1 --, where A represents a saturated or unsaturated, linear, branched or cyclic divalent C.sub.2 .about.C.sub.Type: GrantFiled: October 5, 1990Date of Patent: June 9, 1992Assignee: Fujirebio Inc.Inventors: Hiroshi Ikawa, Hajime Matsumoto, Nobuo Kobayashi, Jun Kusunoki
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Patent number: 5118694Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, halogen, trifluoromethyl, nitro, cyano, lower alkyl, lower alkoxycarbonyl, lower alkylthio, lower alkylsulphonyl, lower alkanoyl, aroyl, carbamoyl, mono(lower alkyl)carbamoyl or di(lower alkyl)carbamoyl, R.sup.2 is hydrogen, lower alkyl or phenyl, R.sup.3 is hydrogen or lower alkyl, R.sup.4 and R.sup.5 each is hydrogen or R.sup.4 is hydroxy and R.sup.5 is hydrogen or R.sup.4 and R.sup.5 together are a carbon-carbon bond and R.sup.6 is an aryl or N-heteroaryl group carrying a hydroxy group in the 2-position or, in the case of a N-heteroaryl group, also a N-oxide group in the 2-position,and pharmaceutically acceptable acid addition salts of these compounds of formula I which are basic, possess pronounced potassium channel activating activity and can be used as medicaments, particularly in the control or prevention of hypertension, congestive heart failure, angina pectoris, peripheral and cerebral vascular disease and smooth muscle disorders.Type: GrantFiled: September 11, 1990Date of Patent: June 2, 1992Assignee: Hoffmann-La Roche Inc.Inventors: Michael R. Attwood, Philip S. Jones, Sally Redshaw
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Patent number: 5118808Abstract: The synthesis and application of N(1)-n-alkyl-pyrimidinium-salts are described. These surfactants have a very small critical micelle concentration (CMC) in the order of 10.sup.-5 -10.sup.-7 Mol/Liter. These N(1)-n-alkyl-pyrimidinium components have pharmacological activities and can act as antimetabolites.Type: GrantFiled: May 24, 1990Date of Patent: June 2, 1992Assignee: Medice Chem.-Pharm. Fabrik Putter GmbH & Co. KGInventor: Henrich H. Paradies
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Patent number: 5118818Abstract: Organic carbonates: ##STR1## and cyclic organic carbonates: ##STR2## are prepared by reacting an alcohol (R--OH), or respectively a diol (HO--R'--OH), with carbon monoxide, in the presence of:a halogen, ora halogen and/or a halide ion and an oxidizing agent.Type: GrantFiled: March 6, 1991Date of Patent: June 2, 1992Assignee: Enichem Synthesis S.p.A.Inventors: Daniele Delledonne, Franco Rivetti, Ugo Romano
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Patent number: 5116404Abstract: The present invention provides novel uracil derivatives and pesticides which contain the novel uracil derivatives as an active ingredient, and exhibit preventing and controlling effects against harmful living things, especially agricultural insect pests, sanitary insect pests, stored product insect pests, house insect pests and veterinary insect pests at a very low drug-concentration.Type: GrantFiled: January 8, 1991Date of Patent: May 26, 1992Assignee: Nissan Chemical Industries Ltd.Inventors: Shigeru Ishii, Kazunari Nakayama, Kazuo Yagi, Jun Satow, Kenzou Fukuda, Kaoru Itoh, Toshiyuki Umehara, Masaki Kudo, Yoichi Inoue, Tsutomu Nawamaki, Shigeomi Watanabe
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Patent number: 5116867Abstract: Chemicals are disclosed which are useful for inhibiting the actions of adenosine in mammals, comprising: L-propranolol, or D-propranolol, or alprenolol and derivatives thereof for parenteral or topical administration are disclosed for purposes of achieving desired circulating concentrations in the range of 10 nanogram to 10 milligrams per kilogram.D-Propranolol is of special interest because it is relatively inactive as a .beta.-adrenergic blocking agent. Specific uses of D-propranolol include the treatment of asthma, chronic obstructive pulmonary disease, A-V node conduction disturbances; apnea of preterm infants, pulmonary hypertension, headaches, migraine, and in attention-deficit disorder. D-Propranolol might also be used as a substitute for xanthines in beverages to produce a feeling of well being, awakeness, awareness and increased performance.Type: GrantFiled: June 30, 1989Date of Patent: May 26, 1992Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: David C. Klein, Olga Nikodijevic
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Patent number: 5117015Abstract: A process for producing a 1.alpha.,3.beta.,24-trihydroxy-.DELTA..sup.5 -steroid represented by the formula (II): ##STR1## wherein R.sub.1 and R.sub.2, independently, represent a hyrogen atom, or R.sub.1 and R.sub.2 together form a single bond, R.sub.3 represents an unsubstituted or halogen-substituted lower alkyl, and R.sub.4 represents a hydrogen atom, hydroxy or a protected hydroxy, comprising reducing a 1.alpha.,2.alpha.-epoxy-.DELTA..sup.4,6 -3,24-dioxosteroid represented by the formula (I) ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the same meanings as defined in formula (II), using an alkaline metal or alkaline earth metal and a proton donor in a solvent comprising ammonia or amine characterized in that at an early stage of the reaction, the 1.alpha.,2.alpha.-epoxy-.DELTA..sup.Type: GrantFiled: April 30, 1991Date of Patent: May 26, 1992Assignee: Teijin LimitedInventors: Tatuo Yarino, Takao Fujii
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Patent number: 5116842Abstract: Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents --COR.sub.4, --CO.sub.2 R.sub.4, --COCO.sub.2 R.sub.4 or --CONR.sub.4 R.sub.5 (where R.sub.4 and R.sub.5 may be the same or different and represent a hydrogen atom or a C.sub.1-3 alkyl group);R.sub.2 represents a hydrogen atom or a hydroxy or oxo group, with the proviso that when R.sub.1 is --COR.sub.4, --CO.sub.2 R.sub.4 or --COCO.sub.2 R.sub.4, R.sub.2 is not a hydrogen atom;R.sub.3 represents a hydrogen atom or a hydroxy group;X represents a direct bond, --CH.sub.2 -- or --CH.sub.2 O--;Ar represents a substituted phenyl moiety; and physiologically acceptable salts thereof.The compounds are indicated as useful in the treatment of pain.Processes for their preparation and pharmaceutical compositions containing them are also disclosed.Type: GrantFiled: May 17, 1990Date of Patent: May 26, 1992Assignee: Glaxo Group LimitedInventors: Alan Naylor, Duncan B. Judd
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Patent number: 5116836Abstract: Novel 3-aryl-pyrrolidine 2,4-dione derivatives of the formula ##STR1## having pesticidal activity.Type: GrantFiled: August 15, 1990Date of Patent: May 26, 1992Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Hermann Hagemann, Andreas Krebs, Albrecht Marhold, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen, Benedikt Becker, Wilhelm Stendel, Christoph Erdelen
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Patent number: 5114941Abstract: A pyrimidinedione derivative compound has a basic backbone in which a 4-oxobenzopyran ring group part and a pyrimidinedione part are linked by a structure comprising an alkyl chain containing at least two nitrogen atoms and one oxygen. The pyrimidinedione derivative is useful for a medical treatment of cardiac arrhythmias.Type: GrantFiled: November 27, 1990Date of Patent: May 19, 1992Assignee: Mitsui Toatsu Chemicals, IncorporatedInventors: Tsutomu Katakami, Tatsuro Yokoyama, Haruki Mori, Nobuya Kawauchi, Joji Kamiya, Masaaki Ishii
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Patent number: 5114960Abstract: Compounds of the formula ##STR1## wherein A taken together with the two carbon atoms denoted as .alpha. and .beta. is a group of the formula ##STR2## and the dotted line is the double bond present in formulas (i) and (iii); and wherein n is zero, 1, 2 or 3, one of R.sup.1 and R.sup.2 is carboxy or alkoxycarbonyl and the other is hydrogen, R.sup.3 is hydrogen, alkyl, alkoxy, aryloxy, azido, cyano or alkylthio, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each, independently, is hydrogen or alkyl or, when R.sup.1 is carboxy or alkoxycarbonyl and n stands for 1, R.sup.4 and R.sup.6 taken together can be a carbon-carbon bond or, when R.sup.2 is carboxy or alkoxycarbonyl, R.sup.5 and R.sup.7 taken together can be a carbon-carbon bond, R.sup.8 is halogen, alkyl, haloalkyl or alkoxy and R.sup.9 is hydrogen, halogen, alkyl or alkoxy, and pharmaceutically acceptable salts of the compounds of formula I in which one of R.sup.1 and R.sup.Type: GrantFiled: June 26, 1990Date of Patent: May 19, 1992Assignee: Hoffmann-La Roche Inc.Inventors: Geoffrey Lawton, John M. Osbond, Christopher R. Self
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Patent number: 5112835Abstract: 6-substitutted acyclopyrimidine nucleoside derivatives represented by the following general formula I: ##STR1## wherein R.sup.1 represents a hydrogen or halogen atom or a group of alkyl, alkenyl, alkynyl, alkylcarbonyl, arylcarbonyl, arylcarbonylalkyl, arylthio or aralkyl; R.sup.2 represents a group of arylthio, alkylthio, cycloalkylthio, aryl sulfoxide, alkyl sulfoxide, cycloalkyl sulfoxide, alkenyl, alkynyl, aralkyl, arylcarbonyl, arylcarbonylalkyl or aryloxy; R.sup.3 represents a hydroxyalkyl group of which alkyl portion may contain an oxygen atom; X represents an oxygen or sulfur atom or amino group; Y represents an oxygen or sulfur atom; and A represents .dbd.N-- or --NH-- or pharmaceutically acceptable salts thereof, processes for their preparation and antiviral agents containing them as active ingredients.Type: GrantFiled: November 21, 1989Date of Patent: May 12, 1992Assignee: Mitsubishi Kasei CorporationInventors: Tadashi Miyasaka, Hiromichi Tanaka, Erik D. A. De Clercq, Masanori Baba, Richard T. Walker, Masaru Ubasawa
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Patent number: 5112999Abstract: Compounds of general formula I or Ia ##STR1## or mixtures thereof, wherein the groups P-L-P are a ligand from the group comprising diphosphine and diphosphinite, in which the secondary phosphine groups or phosphinite groups P are coupled via 2 to 4 C atoms, and which form a 5-, 6- or 7-membered ring with the Ir atoms, X, X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5 and X.sup.6 independently of the others are Cl, Br or I, or X.sup.1 and X.sup.6 and H and X.sup.2, X.sup.3, X.sup.4 and X.sup.5 independently of the others are Cl, Br or I, or X.sup.1 and X.sup.5 and H and X.sup.2, X.sup.3, X.sup.4 and X.sup.6 independently of the others are Cl, Br or I, and M.sup..sym. is an alkali metal cation or quaternary ammonium. The compounds are suitable as homogeneous catalysts for the (preferably) asymmetric hydrogenation of N-substituted imines to secondary amines.Type: GrantFiled: September 11, 1990Date of Patent: May 12, 1992Assignee: Ciba-Geigy CorporationInventors: John A. Osborn, You P. N. C. Chan, Hans-Ulrich Blaser, Felix Spindler
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Patent number: 5112974Abstract: This invention concerns a coordination complex or salt thereof which is spectroscopically or photoactively determinable when bound to DNA having the formula ##STR1## wherein M is a suitable transition metal and each of R.sub.1, R.sub.2 and R.sub.3 is ethylenediamine, bipyridine, phenanthroline, diazafluorene-9-one or phenanthrenequinonediimine. In the complex, R.sub.1, R.sub.2 and R.sub.3 are bound to M by coordination bonds and R.sub.1 and R.sub.2 may be the same or different and both are different from R.sub.3. In the preferred embodiments, the invention concerns complexes of ruthenium(Ru) or rhodium(Rh) wherein R.sub.1 and R.sub.2 are the same. The invention also concerns the complex ##STR2## wherein M is Ru or Rh and R is 9-10-phenanthrenequinonediimine or 5-nitrophenanthroline.Type: GrantFiled: November 7, 1988Date of Patent: May 12, 1992Assignee: The Trustees of Columbia University in the City of New YorkInventor: Jacqueline K. Barton
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Patent number: 5112826Abstract: The dihydrodibenzocycloheptyliden-ethylpiperazine derivative has the formula: ##STR1## wherein R represents a substituent selected from the group consisting of --CH.dbd.CH.sub.2 ; --CO.sub.2 C.sub.2 H.sub.5 ; --CH.dbd.CH--CO.sub.2 CH.sub.Type: GrantFiled: April 12, 1989Date of Patent: May 12, 1992Inventors: Xavier D. Cirera, Romeo R. Andreoli, Pedro P. Lloveras, Leonida Bruseghini, Jose P. Irurre
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Patent number: 5112991Abstract: A process is provided herein for preparing an organo-substituted sodium aluminum hydride by reacting sodium, aluminum, an organic compound of specific structure containing a hydroxyl group and hydrogen.In such process, an aluminum alloy is used as the aluminum.Type: GrantFiled: February 16, 1990Date of Patent: May 12, 1992Assignee: Mitsui Toatsu Chemicals IncorporatedInventors: Tetsuya Iwao, Shuichi Osaka, Takao Sakaki, Tadao Nishida, Kiyoshi Yamamura, Seijiro Koga, Reiji Hirai, Haruo Nakagawa