Patents Examined by Ba K. Trinh
  • Patent number: 5412107
    Abstract: N-Phenylsulfonyl-N'-pyrimidinyl-, -N'-triazinyl- and -N'-triazolylureas and -thioureas of formula I ##STR1## in which X is oxygen, sulfur, SO or SO.sub.2 ; W is oxygen or sulfur; R.sub.1 is hydrogen or methyl; R.sub.2 is hydrogen, fluorine, chlorine, bromine, iodine, (X).sub.n R.sub.3, NO.sub.2, NR.sub.4 R.sub.5, --C.tbd.CR.sub.6, ##STR2## or cyano; n is the number 0 or 1; R.sub.3 is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkyl which is substituted by 1-4 halogen atoms, C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.3 alkylthio; or C.sub.2 -C.sub.4 alkenyl or C.sub.2 -C.sub.4 alkenyl which is substituted by 1-4 halogen atoms; R.sub.4 is hydrogen, CH.sub.3 O, CH.sub.3 CH.sub.2 O or C.sub.1 -C.sub.3 alkyl; R.sub.5 is hydrogen or C.sub.1 -C.sub.3 alkyl; R.sub.6 is hydrogen, methyl or ethyl; R.sub.7 is hydrogen or methyl; Z is ##STR3## E is methine or nitrogen; R.sub.8 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 haloalkylthio, C.sub.
    Type: Grant
    Filed: November 19, 1993
    Date of Patent: May 2, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Willy Meyer
  • Patent number: 5411984
    Abstract: Substituted 2'-benzoyl and 2', 7-dibenzoyl taxol derivatives are synthesized which have improved water solubility and stability while maintaining bioactivity. In a preferred embodiment, taxol 2',7-di(sodium 1,2-benzenedicarboxylate) is synthesized by reacting taxol with phthalic anhydride, and subsequently neutralizing the resulting acid by an ion exchange resin. Taxol 2'-(sodium 1,4-benzenedicarboxylate) is prepared by reacting the monobenzyl ester of 1,4-benzene dicarboxylic acid with taxol in the presence of dicyclohexyl carbodiimide and dimethylaminopyridine, hydrogenolysing the resulting ester to remove the benzyl group, and neutralizing with ion exchange resin. Other taxol prodrugs are prepared by modifications of these routes. In a preferred embodiment, the compounds prepared have improved water-solubility as compared with taxol and demonstrate activity in the M109 mouse bioassay system.
    Type: Grant
    Filed: October 16, 1992
    Date of Patent: May 2, 1995
    Assignee: Virginia Tech Intellectual Properties, Inc.
    Inventors: David G. I. Kingston, Jingyu Liang
  • Patent number: 5412113
    Abstract: The present invention relates to a proces for manufacturing L-(-)-carnitine from D-(+)-carnitine or a derivative thereof. D-(+)-carnitine is esterified in order to protect the carboxyl group and subsequently converted to an acyl derivative. The acyl derivative is then converted to a lactone of L-(-)-carnitine. Finally, the lactone is reopened to obtain L-(-)-carnitine.
    Type: Grant
    Filed: December 21, 1993
    Date of Patent: May 2, 1995
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Fabio Giannessi, Maria L. Bolognesi, Maria O. Tinti, Francesco De Angelis
  • Patent number: 5405972
    Abstract: Process for the synthesis of taxol and other tricyclic and tetracyclic taxanes.
    Type: Grant
    Filed: January 27, 1994
    Date of Patent: April 11, 1995
    Assignee: Florida State University
    Inventors: Robert A. Holton, Carmen Somoza, Hyeong B. Kim, Mitsuru Shindo, Ronald J. Biediger, P. Douglas Boatman, Chase Smith, Feng Liang, Krishna Murthi
  • Patent number: 5399726
    Abstract: Process for the preparation of a derivative or analog of baccatin III or 10-desacetyl baccatin III having a C2 substituent other than benzoate and/or a C4 substituent other than acetate in which the C2 benzoate substituent and/or the C4 acetate substituent of a derivative of baccatin III or 10-desacetyl baccatin III is/are selectively reduced to the corresponding hydroxy group(s) and converted to R.sub.7 COO- and/or R.sub.8 COO-, respectively, wherein R.sub.7 and R.sub.8 are independently H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, moncyclic aryl, or monocyclic heteroaryl.
    Type: Grant
    Filed: January 29, 1993
    Date of Patent: March 21, 1995
    Assignee: Florida State University
    Inventors: Robert A. Holton, Seokchan Kim
  • Patent number: 5391770
    Abstract: Process for preparing pure ascorbic acid from 2-keto-L-gulonic acid or its sodium salt, by carrying out the following successive steps:esterification of 2-keto-L-gulonic acid or its sodium saltlactonization to sodium ascorbateoptional separation of the sodium ascorbatedisplacement of the ascorbic acid from its saltseparation of the sodium sulphateseparation and purification of the ascorbic acid from its methanolic or aqueous-methanolic solution.
    Type: Grant
    Filed: December 23, 1993
    Date of Patent: February 21, 1995
    Assignee: Rhone Poulenc Rorer S.A.
    Inventors: Isidore Le Fur, Jean-Paul Richard, Gerard Wolff
  • Patent number: 5389673
    Abstract: The present invention relates to novel 4- or 5-(substituted sulfonyl) methyl-3(2H)-furanones having the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are independently alkyl containing 1 to 6 branched or straight chain carbon atoms, phenyl, or halogen substituted phenyl; or R.sup.1 and R.sup.2 are joined by 5 to 7 carbon atoms;R.sup.3 and R.sup.4 are independently hydrogen, alkyl containing 1 to 6 branched or straight chain carbon atoms or R.sup.3 and R.sup.4 are joined by 4 to 6 carbon atoms;R.sup.
    Type: Grant
    Filed: February 16, 1994
    Date of Patent: February 14, 1995
    Assignee: American Home Products Corporation
    Inventors: Steven W. Felman, Ivo L. Jirkovsky, Kevin A. Memoli
  • Patent number: 5389671
    Abstract: The present invention relates to novel 4- or 5-(substituted sulfonyl) methyl-3(2H)-furanones having the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are independently alkyl containing 1 to 6 branched or straight chain carbon atoms, phenyl, or halogen substituted phenyl; or R.sup.1 and R.sup.2 are joined by 5 to 7 carbon atoms;R.sup.3 and R.sup.4 are independently hydrogen, alkyl containing 1 to 6 branched or straight chain carbon atoms or R.sup.3 and R.sup.4 are joined by 4 to 6 carbon atoms;R.sup.
    Type: Grant
    Filed: February 16, 1994
    Date of Patent: February 14, 1995
    Assignee: American Home Products Corporation
    Inventors: Steven W. Felman, Ivo L. Jirkovsky, Kevin A. Memoli
  • Patent number: 5389672
    Abstract: The present invention relates to novel 4- or 5-(substituted sulfonyl) methyl-3(2H)-furanones having the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are independently alkyl containing 1 to 6 branched or straight chain carbon atoms, phenyl, or halogen substituted phenyl; or R.sup.1 and R.sup.2 are joined by 5 to 7 carbon atoms;R.sup.3 and R.sup.4 are independently hydrogen, alkyl containing 1 to 6 branched or straight chain carbon atoms or R.sup.3 and R.sup.4 are joined by 4 to 6 carbon atoms;R.sup.
    Type: Grant
    Filed: February 16, 1994
    Date of Patent: February 14, 1995
    Assignee: American Home Products Corporation
    Inventors: Steven W. Felman, Ivo L. Jirkovsky, Kevin A. Memoli
  • Patent number: 5387751
    Abstract: Olefine oxides are produced by contacting an olefine with oxygen in the presence of a silver containing catalyst and a chlorine-containing reaction modifier; the performance of the catalyst is improved by contacting it with a nitrate or nitrite forming substance for example nitric oxide.
    Type: Grant
    Filed: August 2, 1993
    Date of Patent: February 7, 1995
    Assignee: Imperial Chemical Industries PLC
    Inventors: Percy Hayden, Richard W. Clayton, John R. Ramforth, Alan F. G. Cope
  • Patent number: 5387698
    Abstract: The invention provides a method for making a curable epoxysilicone composition through the hydrosilation reaction between an ethylenically unsaturated epoxide and an SiH-containing silicone to produce an epoxysilicone product, and catalyzed by a rhodium containing selective catalyst which does not promote the oxirane ring-opening reaction of either the ethylenically unsaturated epoxide starting material or the epoxysilicone product. The invention also provides for a curable epoxysilicone composition made by the above method for the catalyst, and two methods of making the catalyst.
    Type: Grant
    Filed: June 11, 1992
    Date of Patent: February 7, 1995
    Assignee: General Electric Company
    Inventors: James V. Crivello, Mingxin Fan
  • Patent number: 5380887
    Abstract: A diphenylsulfone derivative of the formula (I) ##STR1## which is highly safe and used for imparting storage stability to a colored image of thermal or heat sensitive recording material, wherein R.sup.1 represents lower alkenyl or aralkyl optionally substituted with halogen or lower alkyl, and R.sup.2 represents hydrogen or methyl, provided that R.sup.2 represents methyl when R.sup.1 represents unsubstituted benzyl.
    Type: Grant
    Filed: February 4, 1994
    Date of Patent: January 10, 1995
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Takafumi Tohyama, Takehiro Sato, Kousaku Morita, Masaaki Uchikawa, Nobuyuki Hirai
  • Patent number: 5374745
    Abstract: The invention relates to a process for the production of prostaglandin precursors of formula I ##STR1## as well as their enantiomers in which X is A--W or W--A,A is a --C.tbd.C-- group,W is a hydroxymethylene group, in which the OH group can be functionally modified by etherification or esterification,D is a straight-chain or branched-chain alkylene group with 2-5 C atoms each or a ##STR2## group, n i s 1 to 3,E is a --C.tbd.C-- group or a --CR.sub.3 .dbd.CR.sub.4 group with R.sub.3 and R.sub.4 each meaning a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group,R.sub.1 is a hydrogen atom or a hydroxy group, which can be functionally modified as in W,R.sub.2 is a straight-chain or branched-chain alkyl group with 1-7 C atoms, characterized in that vinyl bromides of formula II ##STR3## in which Z means the group ##STR4## and R.sub.1, W, D, E and R.sub.2 have the above-indicated meanings and hydroxy groups unprotected in R.sub.1 and W or represented by an optionally substituted benzoyl radical, a C.sub.1 -C.sub.
    Type: Grant
    Filed: September 29, 1992
    Date of Patent: December 20, 1994
    Assignee: Schering Aktiengesellschaft
    Inventor: Ulrich Klar
  • Patent number: 5374746
    Abstract: The present invention relates to a L-talopyranoside derivative of the formula (I): ##STR1## wherein, A is hydrogen atom, a lower alkyl group having 1 to 5 carbon atoms, or a hydroxyl-protecting group;B.sub.1 and B.sub.2, the same or different from each other, are independently hydrogen atom or a hydroxyl-protecting group;R.sub.1 and R.sub.2 may form a alkylene group with a carbon atom of 5-position of the sugar skeleton, or one of them is hydrogen atom and the other is CH.sub.2 X wherein, X is hydrogen, or a protected or un-protected hydroxyl group.Provided that, the following compounds are excepted: ##STR2## wherein, B.sub.1 and B.sub.2 are independently hydrogen atom or acetyl. L-talopyronoside derivatives of the present invention is a very useful intermediate for the synthesis of anthracycline antibiotics having an antitumor activity.
    Type: Grant
    Filed: June 18, 1993
    Date of Patent: December 20, 1994
    Assignee: Dong-A Pharmaceutical Co., Ltd.
    Inventors: Kwang D. Ok, Moon S. Kim, Dong Y. Jung
  • Patent number: 5374650
    Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: March 25, 1993
    Date of Patent: December 20, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill, Gerard O'Malley
  • Patent number: 5371069
    Abstract: The present invention provides organoleptic compositions which upon thermolyis, hydrolysis or both, release an odorant molecule. They find utility, for example, in tobacco, in tobacco paper, and as additives to food, beverages or gum. The compositions contain one or more dicarboalkoxy dioxolane derivatives having the following formula: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, --CO.sub.2 R.sup.3 wherein R.sup.3 is --H.sub.3 or lower alkyl, provided that in at least one of R.sup.1 and R.sup.2, R.sup.3 is lower alkyl; wherein Z is a direct bond, or --CH.dbd.C(R.sup.4)--; where R.sup.4 is --H or alkyl group; and Y is ##STR2## where R.sup.5 and R.sup.6 are independently --H, lower alkyl or --OR.sup.7 where R.sup.7 is --H or lower alkyl.
    Type: Grant
    Filed: April 17, 1992
    Date of Patent: December 6, 1994
    Assignee: Giuaudan-Roure Corporation
    Inventors: Philip A. Christenson, Paul J. Riker, Denise A. Anderson, John M. Yurecko, Jr.
  • Patent number: 5369123
    Abstract: Novel nitrogen-substituted mevinic acid derivatives which inhibit the activity of HMG-CoA reductase. Pharmaceutical compositions, and methods of use for the treatment or prevention of hypercholesterolemia, atherosclerosis, hyperlipoproteinaemia and hyperlipidemia are provided, as are novel methods for preparation and intermediate compounds.
    Type: Grant
    Filed: October 9, 1992
    Date of Patent: November 29, 1994
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Dinos P. Santafianos, Kathleen M. Poss, Eric M. Gordon, Peggy J. McCann
  • Patent number: 5367086
    Abstract: Taxol, 10-deacetyltaxol and other taxane derivatives are prepared from naturally occurring taxane-7-xylosides by the oxidative cleavage of the 7-xyloside moieties.
    Type: Grant
    Filed: March 10, 1993
    Date of Patent: November 22, 1994
    Assignee: University of Florida
    Inventor: Koppaka V. Rao
  • Patent number: 5364880
    Abstract: Described is a novel compound and method, useful for treatment of cardiac arrhythmias, especially useful in patients with congestive heart failure (CHF). A process for synthesizing the novel compound is also described.
    Type: Grant
    Filed: June 16, 1993
    Date of Patent: November 15, 1994
    Assignee: Advanced Therapies, Inc.
    Inventor: Pascal Druzgala
  • Patent number: 5362888
    Abstract: A process for the preparation of a polycyclic dye of Formula (1): ##STR1## by reacting a compound of Formula (2): ##STR2## with a benzofuranone of Formula (3): ##STR3## wherein: R.sup.1 and R.sup.2 each independently is --H or alkyl;R.sup.3 is alkyl;R.sup.4 is --H or alkyl;R.sup.5 and R.sup.6 each independently is alkyl; orR.sup.5 and R.sup.6 together with the N atom to which they are attached form a heteroalicyclic ring; andRing A is unsubstituted or is substituted by from one to three substituentsprovided that at least one of R.sup.1, R.sup.2 and R.sup.4 is --H.The polycyclic dyes of Formula (1) are useful for the coloration of synthetic textiles such as polyester to which they impart blue to navy shades.
    Type: Grant
    Filed: June 14, 1993
    Date of Patent: November 8, 1994
    Assignee: Zeneca Limited
    Inventors: Nigel Hall, Michael C. H. Standen