Patents Examined by Nicholas S. Rizzo
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Patent number: 5389626Abstract: Compounds of formula (I): ##STR1## in which: R.sup.1 is hydrogen or acyl; R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkoxy; and Ar is phenyl or substituted phenyl and pharmaceutically acceptable salts and esters thereof have valuable antibiotic activity, including against Methicillin-resistant strains of Staphylococcus. The invention also provides a process for preparing the compounds and methods and compositions using them.Type: GrantFiled: May 5, 1992Date of Patent: February 14, 1995Assignee: Sankyo Company, LimitedInventors: Koichi Kojima, Kazuo Koyama, Shigeo Amemiya, Masayuki Iwata
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Patent number: 5387748Abstract: Antimicrobial dithiocarbamoyl quinolone compounds of the general formula: ##STR1## wherein (1) A.sup.1, A.sup.2, A.sup.3, R.sup.1, R.sup.3, R.sup.4, and R.sup.6 form any of a variety of quinolone and related heterocyclic structures similar to those known in the art to have antimicrobial activity; and(2)(1) R.sup.1 is X, R.sup.3 is X, or both R.sup.1 and R.sup.3 are X; and(2) X is --R.sup.15 --N(R.sup.16)(R.sup.17) or --R.sup.15 --R.sup.18 --N(R.sup.19)(R.sup.17), where(a)(1) R.sup.15 is nil, alkyl, a carbocyclic ring, or a heterocyclic ring; and(2) R.sup.16 is hydrogen; alkyl; alkenyl; a carbocyclic ring; a heterocyclic ring; or(3) when X is R.sup.15 --N(R.sup.16)(R.sup.17), R.sup.16 and R.sup.15 may together comprise a heterocyclic ring including the nitrogen atom to which R.sup.15 and R.sup.16 are bonded;(b) R.sup.17 is C(.dbd.S)--S--M, where M is a pharmaceutically-acceptable salt or biohydrolyzable ester; and(c)(1) R.sup.18 is alkyl, a carbocyclic ring, or a heterocyclic ring; and(2) R.sup.Type: GrantFiled: May 2, 1991Date of Patent: February 7, 1995Assignee: Procter & Gamble Pharmaceuticals, Inc.Inventors: Thomas P. Demuth, Jr., Ronald E. White
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Patent number: 5385897Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R is selected from the group consisting of ##STR2## and R.sub.b --NH--, Ra is an organic radical, Ri and Rj are individually selected from the group consisting of hydrogen, aliphatic hydrocarbon, aromatic hydrocarbon and heterocycle or taken together with the nitrogen atom to which they are attached form an optionally substituted ring, Rb is selected from the group consisting of carbocyclic aryl and heterocyclic aryl, both optionally substituted, R.sub.1A is selected from the group consisting of ##STR3## R.sub.A ' and R.sub.B ' are individually selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, Z.sub.A is selected from the group consisting of a simple bond, --O-- and optionally oxidize sulfur, R.sub.Type: GrantFiled: March 20, 1992Date of Patent: January 31, 1995Assignee: Roussel-UclafInventors: Jean-Georges Teutsch, Alain Bonnet, Jozsef Aszodi, Solange Gouin d'Ambrieres
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Patent number: 5374739Abstract: The present invention provides novel mitomycin analogs containing a cyclic acetal or thioacetal group. These compounds are mitomycin C analogs in which the 7-amino group bears a 5-membered heterocyclic substituent. Mitomycin C is an antitumor agent of established utility, and the 7-N-substituted mitosane analogs thereof have similar utility.Type: GrantFiled: May 28, 1993Date of Patent: December 20, 1994Assignee: Bristol-Myers Squibb CompanyInventors: Takushi Kaneko, Henry S. L. Wong, Terrence W. Doyle
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Patent number: 5373001Abstract: A compound selected from the group consisting of a syn isomer of a compound of the formula ##STR1## in the R or S form or in the form of a R, S mixture wherein the various substituents are defined as in the specification and their non-toxic, pharmaceutically acceptable acid addition salts having anti-bacterial activity.Type: GrantFiled: July 22, 1993Date of Patent: December 13, 1994Assignee: Roussel UclafInventors: Jozsef Aszodi, Jean-Francois Chantot, Solange G. D'Ambrieres
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Patent number: 5371220Abstract: Cephalosporins derivatives having a 3-position substituent of the formula I are described: ##STR1## wherein R.sup.1 is hydrogen, alkenyl or optionally substituted alkyl, Het is a 5- or 6-membered heterocyclic ring bonded via a carbon atom to the amide linkage, wherein Het is selected from a group of the formulae II-III: ##STR2## wherein A is CH or a nitrogen atom; B is oxygen, sulphur or a group NR.sup.4 ; one or two of D, E, F and G are nitrogen atoms and the remainder are CH groups: or Het is a pyrazinone, pyridinone, pyridazinone or pyrimidinone ring, or is a thione equivalent of such a ring, said rings having a substituent R.sup.4 on one nitrogen atom, or is pyranone, or pyranthione; the ring Het being fused by any two adjacent carbon atoms to the benzene ring; and Het being attached to the --CH.sub.2 NR.sup.1 CO-- group via a carbon atomR.sup.2 is hydroxy or an in vivo hydrolysable ester thereof;R.sup.3 is ortho to R.sup.2 and is hydroxy or an in vivo hydrolysable ester thereof; and R.sup.Type: GrantFiled: May 21, 1992Date of Patent: December 6, 1994Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Dominique Boucherot, Frederick H. Jung, Colin J. Strawson
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Patent number: 5366970Abstract: The invention relates to a compound of the formula: ##STR1## of antimicrobial activity.Type: GrantFiled: September 2, 1992Date of Patent: November 22, 1994Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kazuo Sakane, Kohji Kawabata, Yoshiko Inamoto
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Patent number: 5362722Abstract: The present invention provides compounds of the formula ##STR1## wherein R is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 cycloalkyl, or C.sub.1 -C.sub.6 haloalkyl;A and A' are independently hydrogen, C.sub.1 -C.sub.6 alkyl, nitro, amino, a 5-6 membered organic heterocycle containing 1, 2, or 3 hetero atoms selected from nitrogen or sulfur, C.sub.1 -C.sub.6 alkoxy, or phenyl; or A and A' taken together form a group of the formulae ##STR2## wherein X is hydrogen, halo, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkoxycarbonyl, amino, nitro, or carboxy; and Y is nitrogen or carbon; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions and methods of treatment using the above compounds.Type: GrantFiled: December 23, 1992Date of Patent: November 8, 1994Assignee: Eli Lilly and CompanyInventor: Robert J. Ternansky
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Patent number: 5360798Abstract: An antibacterial aminooxypyrrolidinylthiocarbapenem I, its production from the corresponding carbapenem V and thiol VI, its pharmaceutical formulation, and its use or combating bacteria are presented. ##STR1## (wherein R is optionally substituted amino; R.sup.1 is hydrogen or 1C to 5C alkyl; R.sup.2 is hydrogen or a conventional hydroxy protective group; R.sup.3 is hydrogen or an imino protective group or imino substituent; R.sup.4 is 1C to 5C alkylene; and R.sup.5 is hydrogen or a conventional carboxy protective group; X is a leaving group; R.sup.6 is hydrogen or a thiol protective group; and wavy lines each shows a bond in R or S configuration).Type: GrantFiled: June 10, 1992Date of Patent: November 1, 1994Assignee: Shionogi Seiyaku Kabushiki KaishaInventors: Yuji Sendo, Kii Makoto
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Patent number: 5359057Abstract: There is described a process for the manufacture of carboxylic acid amides by acylating amines with 2-benzothiazolyl thioesters of carboxylic acids, which process comprises reacting the amine in the form of an acid addition salt. This process is especially of great advantage when the amine is not particularly stable in the form of the free base, which is frequently the case especially with 7-aminocephalosporin derivatives. 7-Acylamino-cephalosporin derivatives can be manufactured in good yield and in high purity with the novel process.Type: GrantFiled: January 16, 1992Date of Patent: October 25, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Andre Furlenmeier, Urs Weiss
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Patent number: 5356924Abstract: Compounds of the general formula: ##STR1## wherein R.sub.1 and R.sub.2 each independently represents a halogen atom or an alkyl, alkoxy, haloalkyl, haloalkoxy, alkoxycarbonyl, alkenoxy, cyano or nitro group; R.sub.3 and R.sub.4 each independently represents a hydrogen atom or an alkyl group; R.sub.5 represents a hydrogen atom, or an alkyl, alkoxy or alkoxycarbonylalkyl group; X and Y each independently represents an oxygen or sulphur atom or a group N--R, in which R is a hydrogen atom or an alkyl group; n is 0-3; r is 0 or 1; m is 0-4; and A or B represents a group of the general formula: ##STR2## wherein R.sub.6 represents a hydrogen or halogen atom, or an alkyl group; and R.sub.7 represents a halogen atom or an alkyl group; the other of A and B being a hydrogen atom or as for R.sub.1 or R.sub.2, have useful pesticidal activity.Type: GrantFiled: February 22, 1993Date of Patent: October 18, 1994Assignee: Shell Research LimitedInventors: Martin Anderson, Antony G. Brinnand, Roger E. Woodall
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Patent number: 5354884Abstract: .alpha.-Fluoro-substituted N-acryloylamino acid derivatives of the formula ##STR1## are used to make polymers optionally for chromatographic resolution of racemates into their enantiomers. The fluorine atom improves performance in many instances.Type: GrantFiled: October 1, 1992Date of Patent: October 11, 1994Assignee: Bayer AktiengesellschaftInventors: Rolf Grosser, Walter Lange, Bruno Bomer, Dieter Arlt, Dietmar Bielefeldt
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Patent number: 5350845Abstract: A process for the conversion of a 4-chlorosulfonyl azetidinone (a) to a 3-hydroxy-3-cephem-sulfoxide ester (d) by subjecting an intermediate comprising a tin containing Lewis acid-type Fiedel-Crafts catalyst and 3-exomethylene cepham to ozonolysis.Type: GrantFiled: November 13, 1992Date of Patent: September 27, 1994Assignee: Eli Lilly and CompanyInventor: Frank Brown, Jr.
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Patent number: 5348951Abstract: Cephalosporin compounds having a 3-position substituent of the formula (I) are described,--CH.sub.2 --Y--Q (I)wherein Y is a bond or a linking group --NR.sup.4 --Y'--, --O--Y'--, --S--Y'-- wherein R.sup.4 is hydrogen, various optionally substituted alkyl groups, alkenyl, alkanoyl or alkanesulphonyl, and Y' is a bond or various optionally substituted alkylene groups; and Q is a benzene ring (optionally fused to a further benzene ring so forming a naphthyl group or optionally fused to a 5 or 6 membered heterocyclic aromatic group containing 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur), said benzene ring being substituted by groups R.sup.1 and R.sup.2 which are ortho with respect to one another, wherein R.sup.1 is hydroxy or an in vivo hydrolysable ester thereof and R.sup.2 is hydroxy, an in vivo hydrolysable ester thereof, carboxy, sulpho, hydroxymethyl, methanesulphonamido or ureido; or Q is a group of the formula (II) or (III): ##STR1## wherein M is oxygen or a group NR.sup.3 wherein R.Type: GrantFiled: September 5, 1991Date of Patent: September 20, 1994Assignee: ICI PharmaInventor: Frederic H. Jung
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Patent number: 5348952Abstract: Cephalosporins of the formula (I): ##STR1## wherein m is one or two; n is zero, one or two; A and B are organic residues; and R.sub.1 and R.sub.2 are halogen or hydrogen atoms or organic groups are endowed with elastase inhibitory activity. Two processes for their preparation starting from the corresponding 4-acyl cephem are also provided.Type: GrantFiled: June 12, 1992Date of Patent: September 20, 1994Assignee: Farmitalia Carlo Erba S.R.L.Inventors: Pierluigi Bissolino, Marco Alpegiani, Ettore Perrone, Piergiuseppe Orezzi, Giuseppe Cassinelli, Giovanni Franceschi
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Patent number: 5346691Abstract: S-triazine derivatives of formula (I): ##STR1## a process for the preparation thereof and the use thereof as light stabilisers.Type: GrantFiled: May 20, 1993Date of Patent: September 13, 1994Assignee: 3V Inc.Inventor: Giuseppe Raspanti
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Patent number: 5336673Abstract: The present invention relates to novel cephalosporins of the formula (I); ##STR1## wherein, R.sub.1 represents a C.sub.1 .about.C.sub.4 alkyl group or ##STR2## wherein, R.sub.2 and R.sub.3, independently, represent hydrogen or a C.sub.1 .about.C.sub.3 alkyl group and R.sub.4 represents hydrogen or a C.sub.1 .about.C.sub.4 alkyl group;R.sub.1a represents hydrogen or an amino-protecting group;Q represents CH or N; andthe formula ##STR3## represents a saturated or unsaturated heterocyclic group which contains 1 to 4 nitrogen atoms of which one is substituted with an amino group to form quaternary ammonium, and oxygen or sulfur, or a fused heterocyclic group thereof formed together with a substituted or unsubstituted benzene or an optional heterocyclic group, or a pharmaceutically acceptable salt thereof, to processes for preparing the same and to a pharmaceutical composition containing the same as an active ingredient.Type: GrantFiled: February 26, 1992Date of Patent: August 9, 1994Assignee: Dae Woong Pharmaceutical Co., Ltd.Inventors: Chi J. Moon, Sae C. Park, Myoung G. Kim, Sea H. Oh, Seong S. Yim, Nam J. Park, Young K. Choi, Moo J. Sung
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Patent number: 5336768Abstract: There are presented antibacterial cephalosporine having broad antimicrobial activity, having the formula ##STR1## wherein R is hydrogen or a carboxylic acid-protecting group: R.sub.1 represents a substituted piperazinyl group of formula ##STR2## or a substituted pyrrolidinylamino group of formula ##STR3## or a substituted pyrrolidinylmethylamino group of formula ##STR4## where the piperazinyl or pyrrolidinyl group may be optionally substituted with one or more lower alkyl groups, and where Q represents a substituted quinolinyl or naphthyridinyl group: R.sub.2 is selected from the group consisting of hydrogen, lower alkoxy, lower alkylthio and amido; R.sub.3 is hydrogen or an acyl group: and m is 0, 1 or 2, but preferably 0; as well as the corresponding readily hydrolyzable esters. pharmaceutically acceptable salts and hydrates of these compounds.Type: GrantFiled: May 24, 1988Date of Patent: August 9, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Harry A. Albrecht, Dennis D. Keith, Frederick M. Konzelmann, Pamela L. Rossman, Manfred Weigele
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Patent number: 5332735Abstract: Compounds of the general formula (I): ##STR1## where A, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are defined in the description.Medicinal products.Type: GrantFiled: November 14, 1991Date of Patent: July 26, 1994Assignee: Adir et CompagnieInventors: Sylvain Rault, Marie P. Foloppe, Max Robba, Michel Boulouard, Pierre Renard, Michelle Devissaguet, Gerard Adam
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Patent number: RE34960Abstract: Compounds of formula (I): ##STR1## .[.[.]. wherein: R.sup.1 .[.represents a hydrogen atom, an alkyl group, an alkoxy group or various substituted alkyl groups.]. .Iadd.is hydroxyethyl; .Iaddend.R.sup.2 represents a group of formula ##STR2## in which ##STR3## .[.represents an alicyclic amine group having from 4 to 8 ring atoms, optionally having a single double bond, optionally containing an additional hetero-atom and optionally having an oxo group on the ring;.]. .Iadd.is a 3-pyrrolidinyl group; .Iaddend.X represents a hydrogen atom.[.; an alkyl group, an alkoxy group, an alkylthio group, an alkylsulphinyl group, an alkylsulphonyl group, a hydroxy group, a halogen atom or various substituted alkyl groups.].;Y represents .[.a hydrogen atom, an alkyl group, an aliphatic acyl group or an acylimidoyl.]. .Iadd.an acetylimidoyl .Iaddend.group; andR.sup.3 represents a carboxy group or a protected carboxy group.[.].].Type: GrantFiled: May 20, 1987Date of Patent: May 30, 1995Assignee: Sankyo Company, LimitedInventors: Tetsuo Miyadera, Yukio Sugimura, Toshihiko Hashimoto, Teruo Tanaka, Kimio Iino, Tomoyuki Shibata, Shinichi Sugawara