Patents Examined by Nicholas S. Rizzo
  • Patent number: 5246937
    Abstract: The present invention provides antiviral compounds of Formula (I): ##STR1## pharmaceutical compositions prepared therefrom, and methods of treatment of viral infections therewith.
    Type: Grant
    Filed: January 22, 1992
    Date of Patent: September 21, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: Michael R. Harnden, Richard L. Jarvest
  • Patent number: 5247073
    Abstract: The present invention provides compounds of the formula ##STR1## wherein R.sup.0 is amino or protected amino; A and A' are 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, carboxy; and Y is nitrogen; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 2, 1992
    Date of Patent: September 21, 1993
    Assignee: Eli Lilly and Company
    Inventor: Robert J. Ternansky
  • Patent number: 5246926
    Abstract: .beta.-Lactam compounds of the formula (Ia) including pharmaceutically acceptable salts and in vivo hydrolysable esters, processes for their preparation and their use as antibiotics: ##STR1## wherein R.sup.1 is hydrogen, methoxy or formamido;R.sup.2 is an acyl group, in particular that of an antibacterially active cephalosporin;CO.sub.2 R.sup.6 is a carboxy group or a carboxylate anion;R.sup.3 is a Y-lactone ring optionally containing an endocyclic double bond, which ring is optionally substituted at any carbon atom by alkyl, dialkylamino, alkoxy, hydroxy, halogen or aryl, which in the case of more than one substituent may be the same or different, or is optionally di-substituted at two adjacent carbon atoms, which are available for substitution, to form an aromatic fused bicyclic system; and X is S, SO, SO.sub.2, O or CH.sub.2.
    Type: Grant
    Filed: March 28, 1990
    Date of Patent: September 21, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: John H. Bateson, George Burton, Stephen C. M. Fell
  • Patent number: 5244890
    Abstract: Cephem compounds having the following formula are disclosed: ##STR1## R.sup.1 =amino or protected amino R.sup.2 =an organic group ##STR2## R.sup.6 =lower alkyl R.sup.7, R.sup.8 .dbd.OH or protected OHY.dbd.N or CHThe compounds are useful as antimicrobial agents.
    Type: Grant
    Filed: May 20, 1992
    Date of Patent: September 14, 1993
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Hideaki Yamanaka, Yoshiki Yoshida, Jiro Goto, Takeshi Terasawa, Shinya Okuda, Kazuo Sakane
  • Patent number: 5244892
    Abstract: Novel cephem compounds represented by a formula [I] and pharmacologically admissible salts or capable of physiologically hydrolyzable nontoxic esters thereof are disclosed. ##STR1## [wherein R.sup.1 indicates a straight-chain or branched lower alkyl group, which may be substituted by carboxyl group which may be protected, trityl group, hydrogen atom or fluorine-substituted lower alkyl group, R.sup.2 indicates a hydrogen atom, metal atom, protective group for carboxyl group or ester residue producible hydrolyzable ester in vivo, R.sup.3, R.sup.4, R.sup.5 and R.sup.6, which may be identical or different, indicate hydrogen atoms, halogen atoms, straight-chain or branched lower alkyl groups, which may be substituted, mercapto groups, which may be substituted, lower alkylamino groups, hydroxyl groups, which may be protected, lower alkoxy groups, lower alkanoyl groups, lower alkoxycarbonyl groups, or lower alkylenedioxy groups, which may be substituted, being maybe formed with R.sup.3 and R.sup.4, R.sup.
    Type: Grant
    Filed: October 11, 1991
    Date of Patent: September 14, 1993
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Seigo Suzue, Kikoh Obi, Tatsuhiro Saito, Keiji Hirai, Hideyuki Fukuda
  • Patent number: 5245027
    Abstract: 3-Fluorosulfonyloxyceph-3-ems having a protected amino or acylamino group in the 7-position are subject to carbon-carbon bond formation at the 3-position by means of a palladium catalyzed coupling reaction with substituted organostannanes. A process for preparing cefprozil is disclosed.
    Type: Grant
    Filed: October 31, 1990
    Date of Patent: September 14, 1993
    Assignee: Bristol-Myers Squibb Company
    Inventors: Stephen R. Baker, Chester Sapino, Jr., Gregory P. Roth
  • Patent number: 5243043
    Abstract: Novel syn isomers of 3-alkoxymethyl or 3-alkylthio-methyl-7-[2-(2-amino-4-thiazolyl)-2-oximino-acetamido]-cephalo sporanic acid compounds of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl and alkynyl of 2 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, acyl of an organic carboxylic acid of 1 to 18 carbon atoms and alkoxy carbonyl of 2 to 6 carbon atoms, A is selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, --NH.sub.
    Type: Grant
    Filed: October 31, 1990
    Date of Patent: September 7, 1993
    Assignee: Roussel Uclaf
    Inventor: Rene Heymes
  • Patent number: 5242913
    Abstract: Certain 7-beta-[2-(2-amino-4-thiazolyl)-(Z)-2-(chloromethylene)acetamido]-3-[(subs tituted)methyl]-ceph-3-em-4-carboxylic acids, pharmaceutically-acceptable salts thereof and conventional in vivo hydrolyzable esters thereof are valuable as broad spectrum antibacterial agents, particularly useful for the treatment of bacterial infections in man and other mammals.
    Type: Grant
    Filed: October 11, 1991
    Date of Patent: September 7, 1993
    Assignee: Pfizer Inc.
    Inventor: Susumu Nakanishi
  • Patent number: 5239068
    Abstract: A method for preparing 2-amino-.beta.-lactams which are substituted by readily-removed protecting groups is provided. According to this invention, an acyl-2-amino-.beta.-lactam is further acylated with a different acyl group and is subsequently treated with base to provide a protected 2-amino .beta.-lactam with a more desirable protecting group.
    Type: Grant
    Filed: April 20, 1992
    Date of Patent: August 24, 1993
    Assignee: Eli Lilly and Company
    Inventors: Larry C. Blaszczak, John E. Munroe, Douglas O. Spry
  • Patent number: 5238942
    Abstract: Novel substituted quinazolinones of the formula (I) are useful as angiotensin II antagonists.
    Type: Grant
    Filed: April 16, 1992
    Date of Patent: August 24, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, William J. Greenlee, Nathan B. Mantlo, Arthur A. Patchett, Dooseop Kim, Stephen E. de Laszlo, Tomasz W. Glinka
  • Patent number: 5238906
    Abstract: Pyridone derivatives of the formula: ##STR1## wherein R is an alkyl group, an alkenyl group, an alkynyl group, a haloalkyl group, a haloalkenyl group or an alkoxyalkyl group, X is a hydrogen atom, a halogen atom, a methyl group optionally substituted with mono or poly halogen atoms or an ethyl group optionally substituted with mono or poly halogen atoms and Y is a hydrogen atom or a methyl group. Said compounds show a high herbicidal potency against undesired weeds.
    Type: Grant
    Filed: November 25, 1991
    Date of Patent: August 24, 1993
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Toru Uekawa, Susumu Takemura, Masayuki Enomoto, Masaharu Sakai, Ryo Sato, Eiki Nagano
  • Patent number: 5236922
    Abstract: The present invention relates to the preparation of new 1-(aminophenyl)-2-aminopropanone derivatives of the general formula: ##STR1## in which X is NH.sub.2, Y is H or a halogen atom, Z is H or a halogen atom, R.sub.1 is C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.6 cycloalkyl and R.sub.2 is H or C.sub.1 -C.sub.4 alkyl, or R.sub.1 and R.sub.2, taken together, can form, with the nitrogen atom to which they are bonded, a heterocyclic group selected from the group consisting of the pyrrolidino, morpholino, thiomorpholino, piperidino, hexamethyleneimino, piperazino, 4-methyl-piperazino, 4-(.beta.-hydroxyethyl)piperazino, 4-phenyl-piperazino and 4-(p-chlorophenyl)piperazino groups, and addition salts thereof.These new derivatives are useful as pharmaceuticals. They are obtained by deacetylation of the corresponding acetylated products.
    Type: Grant
    Filed: May 2, 1990
    Date of Patent: August 17, 1993
    Assignee: Laboratoire L. Lafon
    Inventor: Louis Lafon
  • Patent number: 5236950
    Abstract: This invention relates to a hair-restorer comprising, as an active ingredient, (a) an acyclic branched higher aliphatic hydrocarbon of 20 carbon atoms which may be substituted with hydroxyl group or acyloxy group, or (b) an acyclic branched carboxylic acid of 20 carbon atoms or its derivative and to a process for hair growth.
    Type: Grant
    Filed: February 17, 1989
    Date of Patent: August 17, 1993
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Hajime Aoyama, Satoshi Ono, Osamu Oohashi, Hirokazu Narita, Shuntaro Takano
  • Patent number: 5234920
    Abstract: The present invention relates to new cephalosporins of the formula ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or carboxy, with the proviso that both cannot be the same;R.sup.3 is hydrogen or acetyl; andR.sup.4 is a radical selected from the group consisting of ##STR2## in which n is 1 or 2, R.sup.5 is hydrogen or acetyl, and R.sup.6 is hydrogen, a lower C.sub.1-3 alkyl, or a radical selected from the group consisting of ##STR3## in which n and R.sup.5 are as defined above. In another aspect, this invention relates to processes for the preparation of the compounds of Formula I, to pharmaceutical compositions containing at least one compound of Formula I, and to intermediates in their preparation.
    Type: Grant
    Filed: January 6, 1992
    Date of Patent: August 10, 1993
    Assignee: Bristol-Myers Squibb Company
    Inventors: Takaaki Okita, Hajime Kamachi, Shinji Masuyoshi, Kiyoto Imae
  • Patent number: 5233038
    Abstract: The invention relates to novel photochromic compounds of the family of indolino-spiro-oxazines, these compounds being distinguished by the fact that they correspond to the formula of an indolino-spiro-benzo-cyclodiazene.
    Type: Grant
    Filed: December 5, 1991
    Date of Patent: August 3, 1993
    Assignee: Essilor International (Compagnie Generale d'Optique)
    Inventors: Robert Guglielmetti, Pascale Tardieu
  • Patent number: 5233035
    Abstract: A cephalosporin compound represented by the general formula: ##STR1## This compound exhibits a high antimicrobial activity.
    Type: Grant
    Filed: March 27, 1992
    Date of Patent: August 3, 1993
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Ryuichiro Hara, Noriaki Nagano, Hideki Anan, Tokuo Koide, Ei-ichi Nakai, Masaki Yokota, Katsuhiko Hamaguchi, Masato Sato, Toru Yoden, Tetsuya Maeda
  • Patent number: 5232918
    Abstract: Cephalosporin derivatives having a 3-position substituent of 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 atom;R.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: February 11, 1991
    Date of Patent: August 3, 1993
    Assignees: Imperial Chemical Industries PLC, ICI Pharma
    Inventors: Jean C. Arnould, Dominique Boucherot, David H. Davies, Frederick H. Jung, Colin J. Strawson
  • Patent number: 5229395
    Abstract: The compounds of the subject invention can be represented as follows: ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, are the same or different and are hydrogen (H), or a lower alkyl group of from about 1-4 carbon atoms, or a lower alkoxy group of from about 1-4 carbon atoms.R is a substituted aniline ##STR2## wherein one of R.sup.5, R.sup.6, R.sup.7 is an alkanol having the formula --(CH.sub.2).sub.n OH, n=1-4, or its carbamate ester having the formula --(CH.sub.2).sub.n OCONR'R", n=1-4, and wherein R' and R" the same or different lower alkyl groups of from about 1 to 4 carbon atoms, one of R' and R" may be hydrogen (H), and the remaining groups are hydrogen.Additionally, the subject invention provides methods for synthesizing the above-identified compounds, physiologically acceptable compositions containing these compounds and methods for using these compounds to inhibit the growth of tumor cells.
    Type: Grant
    Filed: August 30, 1991
    Date of Patent: July 20, 1993
    Assignee: Sloan-Kettering Institute For Cancer Research
    Inventors: Kyoichi A. Watanabe, Kiyobumi Takahashi
  • Patent number: 5227153
    Abstract: Use of 4-(2-oxo-3-bornylidenemethyl)benzenesulphonic acid or its salts for the protection of hair against environmental attacking agents, and in particular against light and process for the protection of hair using this compound.Use of 4-(2-oxo-3-bornylidenemethyl)benzenesulphonic acid or of its salts to preserve the mechanical properties of hair for degradation by environmental attacking agents, and in particular by light.The compound is used in proportions of at least 0.3% by weight of free acid, in a cosmetically acceptable, aqueous, alcoholic or aqueous-alcoholic support, and particularly in proportions of 0.4 to 9% by weight.
    Type: Grant
    Filed: October 1, 1991
    Date of Patent: July 13, 1993
    Assignee: L'Oreal
    Inventors: Jean F. Grollier, Claude Dubief, Chantal Fourcadier
  • Patent number: 5225406
    Abstract: The present invention relates to a compound having the formula: ##STR1## wherein R is a hydrogen atom, a carboxyl-protecting group or a negative charge and Q is a hydrogen atom, a halogen atom, a hydroxyl group, an acetoxy group, a carbamoyloxy group, an azide group, a substituted or unsubstituted quarternary ammonio group or a substituted or unsubstituted heterocyclic thio group having at least one hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom, and a sulfur atom, or a non-toxic salt or physiologically hydrolyzable non-toxic ester thereof; a process for producing it; and an antibacterial agent comprising it as an active ingredient.Further, the present invention also relates to a compound having the formula: ##STR2## wherein R.sup.3 is a hydrogen atom or an amino-protecting group, and each of R.sup.4 and R.sup.5 which may be the same or different is a hydrogen atom or a carboxyl-protecting group, or a salt thereof; and a process for producing it.
    Type: Grant
    Filed: September 3, 1991
    Date of Patent: July 6, 1993
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Susumu Nakagawa, Ryuji Mitomo, Koji Yamada, Norikazu Otake, Fumio Nakano, Akira Asai, Satoru Kuroyanagi, Yoshiharu Tanaka, Moriaki Ishikawa, Ryosuke Ushijima