Patents Examined by Nicholas S. Rizzo
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Patent number: 5223504Abstract: Xanthines of the general formula: ##STR1## wherein R.sup.1 represents a straight or branched chain alkyl, alkenyl or alkynyl group of 3-6 carbon atoms, and R.sup.2 and R.sup.3, which may be the same or different, each represent hydrogen or halogen or a methyl, methoxy, nitro or trifluoromethyl group or R.sup.2 and R.sup.3 together form a methylenedioxy or ethylenedioxy group; with the proviso that R.sup.2 and R.sup.3 are not both hydrogen; and pharmacologically acceptable salts thereof with an alkali metal base or a nitrogen base containing organic base, are bronchodilators making them of value in treating asthma and vasodilators making them of interest in treating angina, hypertension, congestive heart failure and multi-infarct dementia. The compounds are also of use in combatting other conditions where inhibition of PDE type IV is thought to be beneficial.Type: GrantFiled: August 16, 1991Date of Patent: June 29, 1993Assignee: Laboratorios Almirall SAInventors: Armando V. Noverola, Jose M. P. Soto, Jacinto M. Mauri, Robert W. Gristwood
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Patent number: 5223496Abstract: Cephalosporin compounds of Formulas II ##STR1## where R is hydrogen or a pharmaceutical cation, in which case R.sub.1 is not present, orR is hydrogen or a chemical bond when R.sub.1 is an acid addition salt anion, and R.sub.2 is (a) hydrogen, (b) a duplicate of the formula I compound to form a dimer, (c) an aminocarbonylmethyl, or (d) an --SR.sub.3 group where R.sub.3 is alkyl, cyclohexyl, phenyl, chloro-substituted phenyl, nitro-substituted phenyl, benzyl or furfuryl, have been found to be valuable as antibiotics for treating warm-blooded animals to combat pathogenic bacterial infections which cause diseases such as the commonly known "shipping fever".Type: GrantFiled: April 23, 1992Date of Patent: June 29, 1993Assignee: The Upjohn CompanyInventors: Alexander R. Cazers, K. Thomas Koshy, Prem S. Jaglan, Robert J. Yancey, Jr., Terry J. Gilbertson, Thomas S. Arnold, David B. Johnson, Catherine L. Gatchell
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Patent number: 5223619Abstract: A process for the preparation of 9-substituted quanine derivatives of general formula (I), in which R is C.sub.1 -C.sub.4 -alkyl optionally substituted with one or more hydroxy groups, or R is (.alpha.), benzyl, ribosyl, 2'-deoxyribosyl or (CH.sub.2).sub.n -OR.sup.1 where n is 1 or 2, and R.sup.1 is CH.sub.2 CH.sub.2 OH or (.beta.) or salts thereof, in which a 1-substituted5-(thiocarbamoyl)amino-1H-imidazole-4-carboxamide of general formula (III), where R has the same meaning as in formula (I), is cyclized: a) by treatment with a heavy metal salt of the group of Cu-, Ag-, Pb- and Hg-salts in an aqueous alkaline medium containing at least for equivalents of OH-ions at a temperature form about 0.degree. C. to the reflux temperature, or b) by treatment with a peroxy compound in an aqueous alkaline medium at a temperature of about 0.degree.-30.degree. C., whereafter (I) is isolated by treatment with a acid and, if desired, is converted into a salt.Type: GrantFiled: September 20, 1991Date of Patent: June 29, 1993Assignee: A/S Gea Farmaceutisk FabrikInventors: Borge Alhede, Finn P. Clausen, Jorgen Juhl-Christensen, Klaus K. McCluskey, Herbert Preikschat
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Patent number: 5223625Abstract: The invention relates to a group of new annelated indolo [3,2-c] lactam derivatives of the formula ##STR1## having an antagonistic activity on 5-HT receptors. The compounds can be used for the treatment of symptoms which are caused by excessive stimulation of said receptors in the gastrointestinal system, the central nervous system, the cardiovascular system, the respiratory system, and for alleviating or preventing withdrawal symptoms which are induced by abuse of drugs.Type: GrantFiled: July 16, 1992Date of Patent: June 29, 1993Assignee: Duphar International Research B.V.Inventors: Ineke Van Wijngaarden, Hans H. Haeck, Derk Hamminga, Wouter Wouters
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Patent number: 5221739Abstract: Provided is a process for 3' acetylation of 3-hydroxymethylcephalosporins under aqueous conditions.Type: GrantFiled: January 9, 1992Date of Patent: June 22, 1993Assignee: Eli Lilly and CompanyInventor: Marvin E. Wildfeuer
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Patent number: 5221688Abstract: The invention relates to salts formed between basic H.sub.2 -receptor antagonists and a complex of zinc with a carboxylic acid selected from tartaric acid, citric acid and alkyl citric acids, and to solvates of such salts, excluding salts in which the basic H.sub.2 -receptor antagonist is ranitidine. Examples of basic H.sub.2 -receptor antagonists are cimetidine, famotidine, nizatidine and roxatidine.The salts are useful in the treatment of gastrointestinal disorders, such as peptic ulcer disease and non-ulcer dyspepsia.Type: GrantFiled: April 24, 1991Date of Patent: June 22, 1993Assignee: Glaxo Group LimitedInventors: John W. Clitherow, Eric W. Collington
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Patent number: 5220030Abstract: A photographic silver halide material is chemically sensitized with a soluble gold(I) compound of the formula:AuL.sub.2.sup.+ X.sup.-orAuL(L.sup.1).sup.+ X.sup.-wherein L is a mesoionic compound; X is an anion; and L.sup.1 is Lewis donor ligand. The novel gold(I) compounds possess properties which are advantageous compared to the properties of previously known gold compounds.Type: GrantFiled: May 13, 1991Date of Patent: June 15, 1993Assignee: Eastman Kodak CompanyInventor: Joseph C. Deaton
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Patent number: 5219848Abstract: Cephalosporin antibiotics having a 3-position substituent of the formula: ##STR1## are described, wherein X is --CO--, --SO.sub.2 -- or --COCH.sub.2 --; Y is --CO--, --SO.sub.2 -- or --CH.sub.2 --; Q is a benzene, pyridine or naphthalene ring, R.sup.1 and R.sup.2 are ortho with respect to each other and are independently hydroxy or of the formula O--M wherein M is a moiety and the O--M bond is cleavable in vivo and ring Q may be further substituted by a variety of atoms and groups. Processes for their preparation and use are described.Type: GrantFiled: August 10, 1990Date of Patent: June 15, 1993Assignees: ICI Pharma, Imperial Chemical Industries PLCInventors: Laurent F. A. Hennequin, David M. Hollinshead
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Patent number: 5216134Abstract: A chelate formed between Eu.sup.3+, Tb.sup.3+, Dy.sup.3+ and Sm.sup.3+ and a compound having the formula ##STR1## where A.sub.1-6 are single carbon or nitrogen atoms; n=1 or 2; R.sub.1-6 is nothing when A is a nitrogen, and hydrogen or an organic group when A is a carbon; Z and Z' are selected among --N(CH.sub.2 CH.sub.2 COO.sup.-).sub.2, --N(CH.sub.2 COO.sup.-).sub.2, --N(CH.sub.2 OPO.sub.3.sup.2-).sub.2 and --N(CH.sub.2 PO.sub.3.sup.2-).sub.2 ;--species that --X--Y is a substituent replacing a hydrogen anywhere in the parent compound; and --X--Y represents an organic group containing no chelating heteroatom closer than four atoms from a chelating heteroatom in the parent compound and X is a stable bridge containing certain groups and Y is selected from (a) specified relative groups allowing coupling to other compounds and (b) residues of compounds participating in biospecific affinity reactions.Type: GrantFiled: March 6, 1991Date of Patent: June 1, 1993Assignee: Wallac OyInventors: Veli-Matti Mukkala, Christian Sund, Marek Kwiatkowski
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Patent number: 5215983Abstract: Novel carbapenem compounds of the formula: ##STR1## in which R.sup.1 is carboxy or protected carboxy,R.sup.2 is hydroxy(lower)alkyl or protected hydroxy(lower)alkyl,R.sup.3 is hydrogen or lower alkyl,R.sup.4 is unsaturated bicyclic heterocyclic group which may be substituted by suitable substituent(s),R.sup.5 is hydrogen or imino-protective group, andA is lower alkylene,or pharmaceutically acceptable salts thereof.Processes for their preparation and pharmaceutical compositions for the treatment of infectious diseases are also disclosed.Type: GrantFiled: October 10, 1990Date of Patent: June 1, 1993Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masayoshi Murata, Hideo Tsutsumi, Keiji Matsuda
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Patent number: 5215997Abstract: The invention relates to an improved process for the preparation of compounds of formula ##STR1## or salts thereof, starting from compounds of formulae ##STR2## via compounds of formulae ##STR3## in which compounds R.sub.1 is hydrogen or lower alkyl, R.sub.2 is an organic radical which may carry a functional group which may be protected by a customary protective group R.sub.2.sup.o, R.sub.3 is hydrogen or a customary carboxyl protective group R.sub.3.sup.o, W is a group which can be replaced by a thiocarboxylic acid radical of formula III, and Z is oxygen or sulfur.Type: GrantFiled: July 1, 1992Date of Patent: June 1, 1993Assignee: Ciba-Geigy CorporationInventors: Ernst Hungerbuhler, Jaroslav Kalvoda
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Patent number: 5215982Abstract: Cephem compounds of the following formula are disclosed: ##STR1## wherein R.sup.1 is amino or protected amino group. R.sup.2 is H or an organic group,R.sup.3 is H or an organic group,R.sup.4 is H, lower alkyl, carboxy, protected carboxy, amino, protected amino or carbamoyl, Z=N or CH. The compounds are useful as antimicrobial agents.Type: GrantFiled: October 26, 1990Date of Patent: June 1, 1993Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kazuo Sakane, Kohji Kawabata, Yoshiko Inamoto
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Patent number: 5214037Abstract: A novel thioalkylthio cephalosporin antibiotic compound of formula I: ##STR1## wherein Acyl is C.sub.1 -C.sub.12 acyl; Het is optionally substituted monocyclic heteroaromatic group containing one or more hetero atoms; R.sup.1 is a single bond or C.sub.1 -C.sub.4 alkylene; R.sub.2 is a straight or branched C.sub.1 -C.sub.4 alkylene; X is a sulfur atom or sulioxide group; and Y is a hydrogen atom or methoxy group, or a pharmaceutically acceptable salt or an amino-, carboxy- and/or hydroxy-protected derivative thereof, a formulation containing the same and a method for treating bacterial infections.Type: GrantFiled: July 12, 1991Date of Patent: May 25, 1993Assignee: Shionogi & Co., Ltd.Inventors: Tadatoshi Kubota, Masaharu Kume
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Patent number: 5211738Abstract: A denine derivatives represented by the following formula: ##STR1## (wherein n is 1 or 2 and R and R' represent hydrogen or a methyl, ethyl, allyl, or propargyl group) and agriculturally acceptable acid addition salts thereof, which have cytokinin activity and besides, excellent rooting action, is applied to as plant growth regulators.Type: GrantFiled: April 2, 1992Date of Patent: May 18, 1993Assignee: Mitsubishi Gas Chemical Co., Inc.Inventors: Yoshinori Sasaki, Takashi Oritani, Akinori Tanaka, Taketo Maruyama, Mitsunori Oda, Takashi Suzuki, Yoshiaki Suzuki, Masakazu Furushima
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Patent number: 5210080Abstract: The invention relates to compounds of antimicrobial activity, of the formula ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is lower alkyl or lower alkenyl,R.sup.3 is lower alkyl, hydroxy(lower)alkyl or protected hydroxy(lower)alkyl,R.sup.4 is amino, protected amino, lower alkylamino, protected lower alkylamino, carboxy(lower)alkylamino, N-[protected carboxy(lower)alkyl]amino andR.sup.7 is hydrogen or lower alkyl, ora pharmaceutically acceptable salt thereof.Type: GrantFiled: April 9, 1991Date of Patent: May 11, 1993Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Kazuo Sakane, Kenzi Miyai, Kohji Kawabata
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Patent number: 5210192Abstract: The invention is directed to a process for preparing 3,7-dialkylxanthines of the formula I ##STR1## (R.sup.1 and R.sup.2 denote C.sub.1 -C.sub.4 -alkyl) by the reaction of 4-amino-imidazolecarboxamide-(5) of the formula II ##STR2## with an alkali cyanate in aqueous solution at a pH of from 3 to 5 followed by cyclization of the resulting urea derivative at a pH of from 8 to 14.Type: GrantFiled: March 2, 1992Date of Patent: May 11, 1993Assignee: BASF AktiengesellschaftInventors: Marius Bugglin, Herbert Gropp, Lothar Janitschke, Ulrich Karl, Hans-Heinrich Lenz
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Patent number: 5208240Abstract: The present invention relates to certain novel 8-substituted purines as selective A.sub.1 -adenosine receptor antagonists which are useful in the treatment of patients suffering from Alzheimer's disease, congestive heart failure or pulmonary bronchoconstriction.Type: GrantFiled: March 12, 1991Date of Patent: May 4, 1993Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Norton P. Peet, Nelsen L. Lentz, Mark W. Dudley
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Patent number: 5206361Abstract: The present invention provides a thiazolinoazetidinone derivative represented by the formula ##STR1## wherein R.sup.1 is phenyl having or not having substituent(s), methyl having or not having substituent(s) or ##STR2## group, R.sup.3 being phenyl having or not having substituent(s), and R.sup.2 is a hydrogen atom or carboxylic acid protective group, and a process for preparing the same.The present invention further provides a process for preparing a 2-exo-methylenepenam derivative characterized by hydrolyzing the thiazoline ring of a thiazolinoazetidinone derivative of the above formula (1) to effect recyclization and obtain a 2-exo-methylenepenam derivative represented by the formula ##STR3## wherein R.sup.1 and R.sup.2 are as defined above.Type: GrantFiled: March 7, 1991Date of Patent: April 27, 1993Assignee: Otsuka Kagaku Kabushiki KaishaInventors: Sigeru Torii, Hideo Tanaka, Masatoshi Taniguchi, Michio Sasaoka, Takashi Shiroi, Yutaka Kameyama
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Patent number: 5206365Abstract: A series of psychotropic heterobicycloalkylpiperazine derivatives having the structure ##STR1## wherein V is a 3- or 4-membered unsaturated chain, containing all carbon atoms when 4-membered, or when a 3-membered chain, V contains an oxygen or sulfur atom as one of the members; R is H or C.sub.1-4 alkyl; W is CH, N, CH.sub.2, or a chemical bond; X is CH, N, SO.sub.2, or CO, with the proviso that both W and X cannot simultaneously be N; and Z is a heteroaromatic ring system. These compounds are useful antipsychotic and/or anxiolytic agents.Type: GrantFiled: March 2, 1992Date of Patent: April 27, 1993Inventors: James S. New, William L. Christopher
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Patent number: 5206360Abstract: A compound of formula I ##STR1## wherein X is sulfur or CH.sub.2 ;R.sup.1 is hydrogen, hydroxy, amino, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, phenyl optionally substituted with one to three C.sub.1-6 alkyl, C.sub.1-6 alkyloxy or hydroxy, C.sub.1-6 alkylthio, phenylthio optionally substituted with one to three C.sub.1-6 alkyl or C.sub.1-6 alkyloxy on the phenyl ring, phenylmethyloxy optionally substituted with one to three C.sub.1-6 alkyl or C.sub.1-6 alkyloxy on the phenyl ring, 1-morpholino, C.sub.1-6 alkyloxy, C.sub.2-6 alkenylmethyloxy, C.sub.3-6 alkynylmethyloxy, C.sub.1-6 alkylamino, C.sub.1-6 dialkylamino or a radical selected from the group consisting of ##STR2## in which n is 0 to 3, R.sup.5 is C.sub.1-6 alkyl or hydrogen, and R.sup.3 and R.sup.4 are independently C.sub.1-6 alkyl;R.sup.2 is hydrogen, a conventional amino protecting group or an acyl group;R.sup.0 is hydrogen or a conventional carboxy protecting group, or --CO.sub.2 R.sup.Type: GrantFiled: April 17, 1992Date of Patent: April 27, 1993Assignee: Bristol-Myers Squibb CompanyInventors: Thomas W. Hudyma, Richard A. Partyka