Patents Examined by Nicholas S. Rizzo
  • Patent number: 5389626
    Abstract: 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: Grant
    Filed: May 5, 1992
    Date of Patent: February 14, 1995
    Assignee: Sankyo Company, Limited
    Inventors: Koichi Kojima, Kazuo Koyama, Shigeo Amemiya, Masayuki Iwata
  • Patent number: 5387748
    Abstract: 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: Grant
    Filed: May 2, 1991
    Date of Patent: February 7, 1995
    Assignee: Procter & Gamble Pharmaceuticals, Inc.
    Inventors: Thomas P. Demuth, Jr., Ronald E. White
  • Patent number: 5385897
    Abstract: 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: Grant
    Filed: March 20, 1992
    Date of Patent: January 31, 1995
    Assignee: Roussel-Uclaf
    Inventors: Jean-Georges Teutsch, Alain Bonnet, Jozsef Aszodi, Solange Gouin d'Ambrieres
  • Patent number: 5374739
    Abstract: 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: Grant
    Filed: May 28, 1993
    Date of Patent: December 20, 1994
    Assignee: Bristol-Myers Squibb Company
    Inventors: Takushi Kaneko, Henry S. L. Wong, Terrence W. Doyle
  • Patent number: 5373001
    Abstract: 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: Grant
    Filed: July 22, 1993
    Date of Patent: December 13, 1994
    Assignee: Roussel Uclaf
    Inventors: Jozsef Aszodi, Jean-Francois Chantot, Solange G. D'Ambrieres
  • Patent number: 5371220
    Abstract: 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: Grant
    Filed: May 21, 1992
    Date of Patent: December 6, 1994
    Assignees: Imperial Chemical Industries PLC, ICI Pharma
    Inventors: Dominique Boucherot, Frederick H. Jung, Colin J. Strawson
  • Patent number: 5366970
    Abstract: The invention relates to a compound of the formula: ##STR1## of antimicrobial activity.
    Type: Grant
    Filed: September 2, 1992
    Date of Patent: November 22, 1994
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Kazuo Sakane, Kohji Kawabata, Yoshiko Inamoto
  • Patent number: 5362722
    Abstract: 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: Grant
    Filed: December 23, 1992
    Date of Patent: November 8, 1994
    Assignee: Eli Lilly and Company
    Inventor: Robert J. Ternansky
  • Patent number: 5360798
    Abstract: 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: Grant
    Filed: June 10, 1992
    Date of Patent: November 1, 1994
    Assignee: Shionogi Seiyaku Kabushiki Kaisha
    Inventors: Yuji Sendo, Kii Makoto
  • Patent number: 5359057
    Abstract: 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: Grant
    Filed: January 16, 1992
    Date of Patent: October 25, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andre Furlenmeier, Urs Weiss
  • Patent number: 5356924
    Abstract: 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: Grant
    Filed: February 22, 1993
    Date of Patent: October 18, 1994
    Assignee: Shell Research Limited
    Inventors: Martin Anderson, Antony G. Brinnand, Roger E. Woodall
  • Patent number: 5354884
    Abstract: .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: Grant
    Filed: October 1, 1992
    Date of Patent: October 11, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rolf Grosser, Walter Lange, Bruno Bomer, Dieter Arlt, Dietmar Bielefeldt
  • Patent number: 5350845
    Abstract: 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: Grant
    Filed: November 13, 1992
    Date of Patent: September 27, 1994
    Assignee: Eli Lilly and Company
    Inventor: Frank Brown, Jr.
  • Patent number: 5348952
    Abstract: 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: Grant
    Filed: June 12, 1992
    Date of Patent: September 20, 1994
    Assignee: Farmitalia Carlo Erba S.R.L.
    Inventors: Pierluigi Bissolino, Marco Alpegiani, Ettore Perrone, Piergiuseppe Orezzi, Giuseppe Cassinelli, Giovanni Franceschi
  • Patent number: 5348951
    Abstract: 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: Grant
    Filed: September 5, 1991
    Date of Patent: September 20, 1994
    Assignee: ICI Pharma
    Inventor: Frederic H. Jung
  • Patent number: 5346691
    Abstract: S-triazine derivatives of formula (I): ##STR1## a process for the preparation thereof and the use thereof as light stabilisers.
    Type: Grant
    Filed: May 20, 1993
    Date of Patent: September 13, 1994
    Assignee: 3V Inc.
    Inventor: Giuseppe Raspanti
  • Patent number: 5336768
    Abstract: 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: Grant
    Filed: May 24, 1988
    Date of Patent: August 9, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Harry A. Albrecht, Dennis D. Keith, Frederick M. Konzelmann, Pamela L. Rossman, Manfred Weigele
  • Patent number: 5336673
    Abstract: 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: Grant
    Filed: February 26, 1992
    Date of Patent: August 9, 1994
    Assignee: 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
  • Patent number: 5332847
    Abstract: A process is disclosed for the preparation of 21-bromo-4-pregnene-3,20-dione derivatives of general Formula I ##STR1## wherein R.sub.1 is a hydrogen atom, a hydroxy group or an alkanoyl group of up to 6 carbon atoms,R.sub.2 symbolizes a hydrogen atom or a methyl group, or whereinR.sub.1 and R.sub.2 jointly mean an isopropylidenedioxy group,whereinR.sub.3 is a hydrogen atom, a fluorine atom or a methyl group,V is a methylene group or ethylene group,X is a hydrogen atom, a fluorine atom or a chlorine atom, andY is a methylene group, a hydroxymethylene group or a carbonyl group.
    Type: Grant
    Filed: June 15, 1992
    Date of Patent: July 26, 1994
    Assignee: Schering Aktiengesellschaft
    Inventor: Gerhard Hempel, deceased
  • Patent number: RE34960
    Abstract: 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: Grant
    Filed: May 20, 1987
    Date of Patent: May 30, 1995
    Assignee: Sankyo Company, Limited
    Inventors: Tetsuo Miyadera, Yukio Sugimura, Toshihiko Hashimoto, Teruo Tanaka, Kimio Iino, Tomoyuki Shibata, Shinichi Sugawara