Patents Examined by Nicholas Rizzo
  • Patent number: 5389627
    Abstract: The present invention relates to novel cephem compounds having the formula: ##STR1## wherein, Q is a carbon or nitrogen atom; X is an oxygen atom, or a nitroalkyl or cyanoimine group, with the proviso that X cannot be an oxygen atom when Q is a carbon atom; R.sub.1 is a hydrogen atom, or a lower alkyl group, or a lower alkyl group which may be substituted by fluoro, or by a carboxylic group or an inorganic cation salt thereof; and R.sub.2 and R.sub.3 independently are a hydrogen atom or a lower alkyl group; or pharmaceutically acceptable salts thereof.The compounds of the present invention have potent antibacterial activities against gram-negative bacteria, especially Pseudomonas, and a longer half-life than conventional cephem compounds.
    Type: Grant
    Filed: November 3, 1993
    Date of Patent: February 14, 1995
    Assignee: Cheil Foods & Chemicals
    Inventors: Choong S. Kim, Yang S. Ahn, Kang Y. Jung, Nam H. Lee, Rok L. Yun, Seong Y. Park, Yeo H. Yoon, Keon H. Lee, Chun S. Lyu, Kwang H. Lee
  • Patent number: 5389625
    Abstract: Cephalosporin compounds of the formula (I) ##STR1## wherein R.sup.1 is hydrogen atom or lower alkyl, and R.sup.2 is 1-alkanoyloxyalkyl or 1-alkoxycarbonyloxyalkyl, their pharmaceutically acceptable salts, methods for producing them, and pharmaceutical use thereof.The cephalosporin compounds and their salts are superior in absorption from digestive tract, and upon absorption from the digestive tract, show a wide range of antimicrobial activities in the body as hydrolysis products, and in addition, they have 10-400 times greater sweetness than sucrose. Thus, said compounds are useful as agents to be administered orally for the prophylaxis and treatment of bacterial infectious diseases.
    Type: Grant
    Filed: June 8, 1992
    Date of Patent: February 14, 1995
    Assignee: Kyoto Pharmaceutical Industries, Ltd.
    Inventors: Hiroyuki Muro, Masayasu Kasai, Satoru Hatano, Ken-ichi Nishimura, Susumu Nishizawa, Nobuharu Kakeya
  • Patent number: 5387679
    Abstract: The present invention relates to a process for preparing a compound of formula (I) ##STR1## wherein R is an heterocyclic group which contains at least one nitrogen atom with or without oxygen or sulphur and R.sup.1 and R.sup.2 are both hydrogen atoms or one of them is an hydrogen atom and the other is an acyl group; the process comprising reacting a compound of formula (II) ##STR2## wherein R.sup.1 and R.sup.2 are each as defined above, and wherein, if necessary, any reactive group is protected by a suitable protective group, or a salt thereof, with a compound of formula (III)R--SH (III)wherein R is as defined above, or a salt thereof, in the presence of an acid and of a compound of formula (IV) ##STR3## wherein each of R.sup.3 and R.sup.4 is a C.sub.1 -C.sub.4 alkyl group or R.sup.3 and R.sup.4 taken together are a C.sub.2 or C.sub.3 alkylene chain and, if necessary, removing the protective groups possibly present.
    Type: Grant
    Filed: March 15, 1993
    Date of Patent: February 7, 1995
    Assignee: Antibioticos S.p.A.
    Inventors: Loris Sogli, Daniele Terrassan, Giuseppe Ribaldone
  • Patent number: 5385938
    Abstract: Preventive as well as therapeutic treatment to alleviate cosmetic conditions and symptoms of dermatologic disorders with amphoteric compositions containing alpha hydroxyacids, alpha ketoacids, related compounds or polymeric forms of hydroxyacids is disclosed. The cosmetic conditions and the dermatologic disorders in which the amphoteric compositions and the polymeric compounds may be useful include dry skin, dandruff, acne, keratoses, psoriasis, eczema, pruritus, age spots, lentigines, melasmas, wrinkles, warts, blemished skin, hyperpigmented skin, kyperkeratotic skin, inflammatory dermatoses, skin changes associated with aging, and skin requiring cleansers.
    Type: Grant
    Filed: August 7, 1992
    Date of Patent: January 31, 1995
    Inventors: Ruey J. Yu, Eugene J. Van Scott
  • Patent number: 5380842
    Abstract: Phthalocyanine compounds represented by the below-described formula are suitable for use in the fabrication of color filters. ##STR1## wherein R.sup.1, R.sup.4, R.sup.5, R.sup.8, R.sup.9, R.sup.12, R.sup.13 and R.sup.16 represent a group represented by the below-described formula, H or a halogen atom, R.sup.2, R.sup.3, R.sup.6, R.sup.7, R.sup.10, R.sup.11, R.sup.14 and R.sup.15 represent an alkyl, alkoxyl, alkylthio, alkylamino, dialkylamino or aryloxyl, arylthio group or --COOR.sup.17, R.sup.17 being a particular monovalent group, H or a halogen atom; and Met represents a metal atom. ##STR2## wherein X and Z represent O or S, R.sup.18, R.sup.19 and R.sup.20 represent H or an alkyl group, A, B and D represent a connecting group, n and l is an integer of 0-10, m, q, t, u, r and w are an integer of 0-2, and p is 0 or 1.
    Type: Grant
    Filed: June 22, 1992
    Date of Patent: January 10, 1995
    Assignees: Mitsui Toatsu Chemicals, Incorporated, Yamamoto Chemicals, Incorporated
    Inventors: Hisato Itoh, Akio Karasawa, Kenichi Sugimoto, Takahisa Oguchi, Shin Aihara
  • Patent number: 5380714
    Abstract: Compounds of the formula I: ##STR1## wherein: X is O, S or NH;n is O or an integer of from 1 to 3;R.sup.1 is hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl;R.sup.2 is CH.sub.2 R.sup.3, NHR.sup.4, SO.sub.2 NR.sup.5 YNR.sup.6 R.sup.7 or R.sup.8, in which R.sup.3 is hydroxy, (1-4C)alkoxy or (1-4C)alkylsulphonyl; R.sup.4 is (1-4C)alkylsulphonyl, (1-4C)haloalkylsulphonyl, formyl, carbamoyl or 2,6-dichloro-4-(2-(1,1-dimethylethyl)amino-1-hydroxyethyl)phenyl; R.sup.5 is hydrogen or (1-4C)alkyl; Y is CO or (1-6C)alkylene; R.sup.6 and R.sup.7 are independently (1-4C)alkyl, or R.sup.6 is hydrogen and R.sup.7 is (1-4C)alkyl, (1-4C)haloalkyl, phenyl(1-4C)alkyl or, when Y is (1-6C)alkylene, is (1-4C)alkylaminocarbonyl or (5-6C)cycloalkylaminocarbonyl; and R.sup.8 is a sugar residue of formula II in which R.sup.
    Type: Grant
    Filed: November 20, 1992
    Date of Patent: January 10, 1995
    Assignee: Imperial Chemical Industries PLC
    Inventors: Geraint Jones, Roger James, Rodney B. Hargreaves
  • Patent number: 5378838
    Abstract: Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).
    Type: Grant
    Filed: January 13, 1993
    Date of Patent: January 3, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Jeffrey M. Bergman, Roger M. Freidinger, Mark G. Bock
  • Patent number: 5378697
    Abstract: The syn isomer of a compound of the formula ##STR1## in the R or S form or a mixture of R and S forms and their non-toxic, pharmaceutically acceptable acid addition salts wherein the substituents are defined as in the specification having antibacterial activity and their preparation.
    Type: Grant
    Filed: June 24, 1992
    Date of Patent: January 3, 1995
    Assignee: Roussel-UCLAF
    Inventors: Jean-Francois Chantot, Solange Gouin D'Ambrieres, Daniel Humbert, Jean-Georges Teutsch
  • Patent number: 5374723
    Abstract: A spiro-oxazine compound represented by the following general formula (A) or (A') is a photochromic compound having an excellent fatigue resistance to repetition of coloration and decoloration and an abundance of hues: ##STR1## wherein the .alpha. ring is a ring selected from a 5-membered ring having one N atom, which may be connected to a benzene ring or naphthalene ring, and a 6-membered ring having one N atom, with the proviso that the N atom in the .alpha.ring is bonded to a C.sub.1-20 alkyl or another organic group, X is selected from O, S, Se and N--R.sup.1 (in which R.sup.1 is selected from H, and C.sub.1-20 alkyl and other organic groups), R.sup.2 and R.sup.3 are selected from --OH, amino, C.sub.1-20 alkoxy, halogen, and other groups, and k is an integer of 0 to 2.
    Type: Grant
    Filed: March 29, 1993
    Date of Patent: December 20, 1994
    Assignee: Toray Industries, Inc.
    Inventors: Shinichi Yamamoto, Takashi Taniguchi
  • Patent number: 5374720
    Abstract: A compound of the formula: ##STR1## wherein R is a hydrogen atom or a methyl group, R.sup.1 is a hydrogen atom or a negative charge, each of R.sup.2 and R.sup.3 which may be the same or different, is a hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group, a formimidoyl group, an acetoimidoyl group, --COOR.sup.4, --CON(R.sup.5)R.sup.6, --N(R.sup.5)R.sup.6, --CH.sub.2 COOR.sup.4, --CH.sub.2 N(R.sup.5)R.sup.6 or --CH.sub.2 CON(R.sup.5)R.sup.6 (wherein R.sup.4 is a hydrogen atom or a lower alkyl group, each of R.sup.5 and R.sup.6 which may be the same or different, is a hydrogen atom or a lower alkyl group, or R.sup.5 and R.sup.6 form together with the adjacent nitrogen atom a heterocyclic group selected from the group consisting of an aziridinyl group, an azetidinyl group, a pyrrolidinyl group and a piperidyl group), A is .dbd.NR.sup.7, .dbd.N.sup.+ (R.sup.7)R.sup.8, wherein each of R.sup.7 and R.sup.
    Type: Grant
    Filed: October 21, 1991
    Date of Patent: December 20, 1994
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Susumu Nakagawa, Norikazu Ohtake, Fumio Nakano, Koji Yamada, Ryosuke Ushijima, Satoshi Murase, Hiroshi Fukatsu
  • Patent number: 5374719
    Abstract: A process for the preparation of the crystalline monohydrate form of the compound of formula (I) ##STR1## which includes exposing the crystalline dihydrate form of the compound of formula (I) to a temperature of between about 50.degree. and 65.degree. C. and a relative humidity of between about 60 to about 100%.
    Type: Grant
    Filed: June 4, 1993
    Date of Patent: December 20, 1994
    Assignee: Eli Lilly and Company
    Inventors: Edward F. Plocharczyk, Erin E. Strouse
  • Patent number: 5371221
    Abstract: The invention relates to a process for recovering caffeine from caffeine-loaded activated carbon using a circulated inert gas sweeping stream held at a temperature of 250.degree. to 460.degree. C., in which process the activated carbon is preheated prior to the desorption of the caffeine with heat sources other than the sweeping gas and held during the desorption step at a uniform temperature or at a temperature increasing from the inlet to the outlet of the inert gas sweeping stream within the range of 250.degree. to 460.degree. C. and the caffeine is subsequently separated from the inert gas sweeping stream by conventional means.
    Type: Grant
    Filed: July 15, 1993
    Date of Patent: December 6, 1994
    Assignee: Jacobs Suchard AG
    Inventors: Stefan Sipos, Gary Jones
  • Patent number: 5364848
    Abstract: New substituted cephalosporin sulfones are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.
    Type: Grant
    Filed: May 1, 1992
    Date of Patent: November 15, 1994
    Assignee: Merck & Co., Inc.
    Inventors: James B. Doherty, Raymond A. Firestone, Paul E. Finke, William K. Hagmann, Shrenik K. Shah, Kevan R. Thompson
  • Patent number: 5362872
    Abstract: The invention relates to chromogenic lactams, to their preparation and to the use thereof in pressure-sensitive or heat-sensitive recording materials.The novel lactams have the general formula I ##STR1## wherein the ring A is an aromatic or heteroaromatic radical containing 6 ring atoms;the ring B is an unsubstituted or substituted benzene nucleus; andZ is ##STR2## R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, X.sub.1 and X.sub.2 are as defined in the description.
    Type: Grant
    Filed: March 10, 1993
    Date of Patent: November 8, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans Baumann, Rox Phaff
  • Patent number: 5362724
    Abstract: A compound of the formula I: ##STR1## wherein Acyl is C.sub.1 -C.sub.12 acyl; Het is an 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.sup.2 is a straight or branched C.sub.1 -C.sub.4 alkylene; and Y is a hydrogen atom or methoxy group, or a pharmaceutically acceptable salt or an amino-, carboxy- and/or hydroxy-protected derivative thereof, which have a potent antibiotic activity.
    Type: Grant
    Filed: September 17, 1993
    Date of Patent: November 8, 1994
    Assignee: Shionogi & Co., Ltd.
    Inventors: Tadatoshi Kubota, Masaharu Kume
  • Patent number: 5360904
    Abstract: A process for preparing penem esters by reacting ##STR1## wherein R.sub.1 is a hydroxy protecting group and X is a C.sub.1 -C.sub.10 alkyl or aryl group, with ##STR2## wherein R.sub.2 is hydrogen or a C.sub.1 -C.sub.6 alkyl group in the presence of an anhydrous organic solvent, condensing the product with ##STR3## wherein X is a halogen atom or a --OCOOR.sub.3 group and then cyclizing.
    Type: Grant
    Filed: September 21, 1992
    Date of Patent: November 1, 1994
    Assignee: Farmitalia Carlo Erba S r l
    Inventors: Angelo Bedeschi, Walter Cabri, Marcello Marchi, Ettore Perrone
  • Patent number: 5358951
    Abstract: This disclosure describes novel 2,3,6, substituted quinazolinones of the formula: ##STR1## wherein R.sub.1, R.sup.6 and X are described in the specification which have activity as angiotensin II (AII) antagonistis.
    Type: Grant
    Filed: April 23, 1993
    Date of Patent: October 25, 1994
    Assignee: American Cyanamid Company
    Inventors: Jeremy I. Levin, Aranapakam M. Venkatesan
  • Patent number: 5359058
    Abstract: A cephalosporin compound substituted in the 7-position with a (cyclo)alkylideneammonio group of formula (II) ##STR1## wherein X' is an anion from an acid HX, R.sub.1 and R.sub.2 are individually a C.sub.1 -C.sub.16 alkyl group, or R.sub.1 and R.sub.2 together with the carbon atom to which they are attached form a cycloalkylidene ring with up to 8 carbon atoms and a process for the preparation which compounds are useful intermediates.
    Type: Grant
    Filed: April 27, 1992
    Date of Patent: October 25, 1994
    Assignee: Gist-Brocades, N.V.
    Inventors: Jan Verweij, Henri G. J. Hirs, Hendrik A. Witkamp, Everardus J. A. M. Leenderts, Jan J. Dekoning, Herman H. Grootveld
  • Patent number: 5356888
    Abstract: There are provided compounds I ##STR1## wherein A is a hydrogen atom or an organic group,R.sub.1 is hydrogen or halogen atom or an organic group,R.sub.2 is hydrogen or halogen atom, C.sub.1 -C.sub.4 alkyl or acyloxy group,R.sub.3 is hydrogen atom, C.sub.1 -C.sub.4 alkyl or alkoxy, benzyl group or a methylene andR.sub.4 is chloro, fluoro, hydrogen atom or an organic group.The compounds I are elastase inhibitors. A process for their preparation is also provided, as are pharmaceutical compositions containing them.
    Type: Grant
    Filed: October 22, 1991
    Date of Patent: October 18, 1994
    Assignee: Farmitalia Carlo Erba
    Inventors: Marco Alpegiani, Pierluigi Bissolino, Ettore Perrone, Francesco Di Matteo, Piergiuseppe Orezzi, Giuseppe Cassinelli
  • Patent number: 5352782
    Abstract: The invention provides a process for the preparation of the crystalline monohydrate form of the compound of the formula (I) ##STR1## which comprises the step of mixing a form of loracarbef, other than the crystalline monohydrate, such as the ethanol crystal, acetone crystal, crystalline dihydrate, acetonitrile crystal, methanol crystal, propanol crystal, ethyl acetate crystal, methylene chloride crystal, crystalline bis(DMF) and crystalline mono(DMF) form, in water at a temperature between about 30.degree. C. to about 60.degree. C., and preferably at a temperature between 40.degree. C. and 50.degree. C. Conversion may also be accomplished by exposing the loracarbef form to saturated steam at a temperature of between about 90.degree. to about 100.degree. C. Another aspect of the invention is the preparation of the above mentioned crystal forms by slurrying the bis(DMF) solvate form of the compound of formula (I) with the respective solvent.
    Type: Grant
    Filed: June 4, 1993
    Date of Patent: October 4, 1994
    Assignee: Eli Lilly and Company
    Inventors: Robert L. Nist, Marvin E. Wildfeuer