Patents Represented by Attorney Michael D. Alexander
  • Patent number: 5994350
    Abstract: The subject of the invention is indolin-2-one derivatives of formula: ##STR1## in which: W represents a --CH.sub.2 -- or --SO.sub.2 -- group;Cy forms, with the carbon to which it is bonded, a non-aromatic, saturated or unsaturated C.sub.3 -C.sub.12 hydrocarbon ring which is optionally condensed or substituted by one or a number of (C.sub.1 -C.sub.7)alkyl groups, it being possible for the said groups to substitute the same carbon atom one or a number of times, or by a C.sub.3 -C.sub.6 spirocycloalkyl;T represents a (C.sub.1 -C.sub.4)alkylene which is optionally interrupted by a (C.sub.3 -C.sub.6)cycloalkylene, the said alkylenes optionally being substituted one or a number of times on the same carbon atom by a (C.sub.1 -C.sub.3)alkyl; or alternatively T represents a direct bond;Z represents in particular an amino group;R.sub.1 and R.sub.2, as well as R.sub.3 and R.sub.4, are either hydrogen or substituents, such as, for example, a halogen, an alkyl, and the like.
    Type: Grant
    Filed: April 17, 1998
    Date of Patent: November 30, 1999
    Assignee: Sanofi-Synthelabo
    Inventors: Loic Foulon, Georges Garcia, Claudine Serradeil-Le Gal, Gerard Valette
  • Patent number: 5989578
    Abstract: The invention relates to a pharmaceutical composition containing an association of active principles, wherein the active principles are clopidogrel and aspirin, each constituent being present in a free form or in the form of a pharmaceutically acceptable salt.
    Type: Grant
    Filed: August 12, 1998
    Date of Patent: November 23, 1999
    Assignee: Sanofi
    Inventors: Andre Bernat, Jean Marc Herbert, Pierre Savi
  • Patent number: 5977118
    Abstract: 6-Substituted pyrazolo[3,4-d]pyrimidin-4-one derivatives, pharmaceutical compositions containing them and methods for effecting c-GMP-phosphodiesterase inhibition and for treating heart failure and/or hypertension.
    Type: Grant
    Filed: March 26, 1997
    Date of Patent: November 2, 1999
    Assignee: Sanofi
    Inventors: Edward R. Bacon, Sol J. Daum, Baldev Singh
  • Patent number: 5965122
    Abstract: Mammalian Interleukin-7 proteins (IL-7s)g DNAs and expression vectors encoding mammalian IL-7s, end processes for producing mammalian IL-7s as products of cell culture, including recombinant systems, are disclosed.
    Type: Grant
    Filed: June 9, 1997
    Date of Patent: October 12, 1999
    Assignee: SANOFI
    Inventors: Anthony E. Namen, Raymond G. Goodwin, Stephen D. Lupton, Diane Y. Mochizuki
  • Patent number: 5958929
    Abstract: 6-Aryl pyrazolo?3,4-d!pyrimidin-4-one derivatives, pharmaceutical compositions containing them and methods for effecting c-GMP-phosphodiesterase inhibition and for treating heart failure and/or hypertension.
    Type: Grant
    Filed: January 30, 1998
    Date of Patent: September 28, 1999
    Assignee: Sanofi
    Inventors: Edward R. Bacon, Baldev Singh
  • Patent number: 5955456
    Abstract: Injectable aqueous composition comprising ursodeoxycholic acid or tauroursodeoxycholic acid, a strong base compatible with intravenous injection and trometamol.
    Type: Grant
    Filed: June 23, 1998
    Date of Patent: September 21, 1999
    Assignee: Sanofi
    Inventors: Tiziano Prato, Anna Giulia Rusticali
  • Patent number: 5925768
    Abstract: The present invention relates to compounds of the formula ##STR1## in which: X.sub.1 is a group --NR.sub.1 R.sub.2 or a group --OR.sub.2 ;g.sub.2, g.sub.3, g.sub.4, g.sub.5, g.sub.6 and w.sub.2, w.sub.3, w.sub.4, w.sub.5, w.sub.6 are identical or different and are each independently hydrogen, a halogen atom, a (C.sub.1 -C.sub.4)alkyl, a (C.sub.1 -C.sub.4)alkoxy, a trifluoromethyl, a nitro or a (C.sub.1 -C.sub.4)alkylthio, with the proviso that at least one of the substituents g.sub.2, g.sub.3, g.sub.4, g.sub.5, g.sub.6 and at least one of the substituents w.sub.2, w.sub.3, w.sub.4, w.sub.5, w.sub.6 are other than hydrogen;R.sub.1 is hydrogen or a (C.sub.1 -C.sub.4)alkyl;R.sub.2 is a non-aromatic (C.sub.3 -C.sub.15)carbocyclic radical which is unsubstituted or monosubstituted or polysubstituted by a substituent selected from a halogen atom, a (C.sub.1 -C.sub.4)alkyl and a (C.sub.1 -C.sub.4)alkoxy;R.sub.3 is hydrogen or a group --CH.sub.2 R.sub.6 ; andR.sub.4 and R.sub.5 are each independently a hydrogen, a (C.
    Type: Grant
    Filed: June 3, 1998
    Date of Patent: July 20, 1999
    Assignee: Sanofi
    Inventors: Francis Barth, Pierre Casellas, Joseph Millan, Didier Oustric, Murielle Rinaldi, Martine Sarran
  • Patent number: 5892024
    Abstract: Disclosed are novel bifunctional nucleoside analogs and oligonucleosides of 3-4 bases (trimers and tetramers) and longer containing at least two consecutive internucleoside linkages of two carbon-one nitrogen atom or two carbon-one oxygen atom (3'-NCC-5', 3'-CNC-5', 3'-OCC-5') internucleoside linkages. The bifunctional nucleosides are useful for preparing the trimers and tetramers, which, in turn, are useful, together with the nucleosides, in preparing oligonucleosides as well as chimeric oligonucleotide analogs, preferably antisense oligonucleosides and oligonucleotide analogs, of 6 to about 60 bases having at least two consecutive internucleoside linkages of two carbon atoms and one nitrogen atom or 2 carbon atoms and one oxygen atom in the oligonucleoside backbone.
    Type: Grant
    Filed: March 13, 1997
    Date of Patent: April 6, 1999
    Assignee: Sanofi
    Inventors: Prasad Venkata Chala Chaturvedula, Ashis Kumar Saha
  • Patent number: 5874432
    Abstract: Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula ##STR1## wherein: L is --O--, --S--, --SO-- or --SO.sub.2 --;m and n are each independently 0 or 1;R.sub.1 is halo, lower-alkanoyl, 1-oxophenalenyl, phenyl or substituted phenyl, heterocyclyl or substitued heterocyclyl or, when L is --O-- and n is 1, cycloheptatrienon-2-yl or, when L is --S-- and n is 1, cyano or lower-alkoxythiocarbonyl or, when L is --SO.sub.2 -- and n is 1, lower-alkyl or trifluoromethyl;R.sub.2 is hydrogen, lower-alkoxycarbonyl, phenyl or phenylthio; andR.sub.3 and R.sub.4 are each hydrogen or various substituents and processes for preparation and pharmaceutical compositions and method of use thereof are disclosed.
    Type: Grant
    Filed: February 20, 1997
    Date of Patent: February 23, 1999
    Assignee: Sanofi
    Inventors: Richard Paul Dunlap, Neil Warren Boaz, Albert Joseph Mura, Dennis John Hlasta, Ranjit Chimanlal Desai, Chakrapani Subramanyam, Lee Hamilton Latimer, Eric Piatt Lodge
  • Patent number: 5872207
    Abstract: Peptides or peptides having an amino acid-like moiety in place of an amino acid moiety thereof immobilized on glass beads, especially controlled-pore glass beads, by a C-terminal .alpha.-carboxyl-.omega.-amino linker and .alpha.-silyl-.omega.-amino anchor, especially wherein the anchor has the structural formula--NH(CH.sub.2).sub.n Si(OR).sub.2 O--wherein n is 3 and R is hydrogen or the glass bead and the linker has the structural formula--?NH(CH.sub.2).sub.r CO!.sub.
    Type: Grant
    Filed: August 29, 1995
    Date of Patent: February 16, 1999
    Assignee: Sanofi Pharmaceuticals, Inc.
    Inventors: Barry Arnold Morgan, Mark Alan Ator, James Arthur Gainor, Thomas Douglas Gordon, Lawrence Ivan Kruse, Teruna Jaya Siahaan
  • Patent number: 5856349
    Abstract: 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl heterocyclic carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with either a heterocyclic carboxylic acid in the presence of an acid-acceptor or the alkali metal salt of a heterocyclic carboxylic acid.
    Type: Grant
    Filed: June 6, 1997
    Date of Patent: January 5, 1999
    Assignee: Sanofi
    Inventors: Richard Paul Dunlap, Dennis John Hlasta, Ranjit Chimanlal Desai, Lee Hamilton Latimer, Chakrapani Subramanyam, John Joseph Court, Malcolm Rice Bell, Virendra Kumar
  • Patent number: 5849738
    Abstract: A method of using 1,2,4-benzotriazine oxides, some of which are novel compounds, as radiosensitizers and selective cytotoxic agents is disclosed. These compounds are shown to specifically radiosensitize hypoxic tumor cells. Some are additionally disclosed to be useful as specific cytotoxic agents for these cells. They also show an unexpected ability to radiosensitize aerobic cells following or preceding a hypoxic incubation of the cells with the drug. This provides a basis for selective radiosensitization of tumors compared to normal cells. A novel method for preparing the 1,2,4-benzotriazine oxides is also disclosed.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: December 15, 1998
    Assignee: SRI International
    Inventors: William W. Lee, J. Martin Brown, Edward W. Grange, Abelardo P. Martinez, Michael Tracy, Daniel J. Pollart
  • Patent number: 5846986
    Abstract: Compounds of the formula ##STR1## wherein Azo is alkyltetrazolyl or is chosen from the group consisting of oxadiazolyl, imidazolyl, pyrazolyl, triazolyl, oxazolyl, triazinyl, thiazolyl, isothiazolyl or any of these substituted with a member of the group consisting of alkyl, alkylthio, alkoxy, hydroxy, halo, cyano, nitro, hydroxyalkyl, alkoxyalkyl, alkoxycarbonyl, alkanoyl, fluoroalkyl or the N-oxide of any of the preceding;Y is an alkylene bridge of 3-9 carbon atoms;R.sub.1 and R.sub.2 are each individually chosen from hydrogen, halo, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl or cyano;R.sub.
    Type: Grant
    Filed: November 25, 1997
    Date of Patent: December 8, 1998
    Assignee: Sanofi
    Inventors: David J. Aldous, Thomas R. Bailey, Guy Dominic Diana, Theodore J. Nitz, Gee-Hong Kuo
  • Patent number: 5843956
    Abstract: Substituted N-arylmethyl and heterocyclylmethyl-1H-pyrazolo?3,4-b!quinolin-4-amines, pharmaceutical compositions containing them and methods for a) effecting c-GMP-phosphodiesterase inhibition, b) treating heart failure and/or hypertension, c) reversing or reducing nitrate-induced tolerance and d) treating angina pectoris, congestive heart disease and myocardial infarction utilizing them.
    Type: Grant
    Filed: February 18, 1997
    Date of Patent: December 1, 1998
    Assignee: Sanofi
    Inventors: Virendra Kumar, John Alan Dority, Jr.
  • Patent number: 5844000
    Abstract: This invention relates to novel propenone oxime ethers, methods of preparing them and pharmaceutical compositions containing them. The compounds have the formula: ##STR1## wherein R.sup.1 is H, or glucuronide;R.sup.2 and R.sup.3 are independently H or methyl;R.sup.4 is 0, or glucuronide, andn is 0 or 1, provided that when R.sup.1 is H, n is 1.
    Type: Grant
    Filed: June 12, 1997
    Date of Patent: December 1, 1998
    Assignee: Sanofi
    Inventors: William Brian, Brian Folk, Juan Shi, Gerard Fabre, Claude Tronquet
  • Patent number: 5837714
    Abstract: This invention provides solid pharmaceutical dispersions comprising a poorly soluble drug substance, as SR48692 or naproxen, xylitol and Transcutol, and a method of preparing such dispersions comprising the steps of dissolving the poorly soluble drug substance in Transcutol and adding the solution to xylitol. The dispersions exhibit good pharmaceutical properties and reduced levels of impurities and degradation products.
    Type: Grant
    Filed: March 3, 1997
    Date of Patent: November 17, 1998
    Assignee: Sanofi
    Inventors: William Rocco, Sharon Laughlin
  • Patent number: 5837705
    Abstract: The invention relates to alpha-substituted pyridazino-quinoline compounds of the formula I: ##STR1## wherein Ring A is chosen from an ortho fused aromatic or heteroaromatic five- or six-membered ring; R.sup.1 is selected from a variety of substituents including halogen, (1-4C)alkyl and nitro; R.sup.2 is selected from a group of the formula R2', R2" or R2"' wherein R2' is --CHR.sup.3 (CH.sub.2).sub.n C(O)NR.sup.5 R.sup.6 ; R2" is --CHR.sup.3 (CH.sub.2).sub.n R.sup.4 and R2"' is --CHR.sup.3 (CH.sub.2).sub.n L wherein n is 0-6; R.sup.5 is aryl or substituted aryl; R.sup.6 is (1-6C)alkyl or hydrogen; R.sup.3 is (1-6C)alkyl, (0-6C)alkylCF.sub.3 or (0-6C)alkylCOOR'; R.sup.4 is (1-6C)alkyl, (2-6C)alkyl containing a double or triple bond, or (0-6C)alkylaryl; L is a variety of substituents including phenyl, heteroaryl and CO.sub.2 R'; R' is hydrogen or (1-4C)alkyl; Z is selected from oxo, --OH, H,H--, H, (1-6C)alkyl or (1-6C)alkylaryl; and R.sup.7 is hydrogen or --(CO)R.sup.8 wherein R.sup.
    Type: Grant
    Filed: April 1, 1996
    Date of Patent: November 17, 1998
    Assignee: Zeneca Limited
    Inventors: Thomas Michael Bare, James Roy Empfield, Janet Marie Forst, Keith John Herzog, Richard Bruce Sparks
  • Patent number: 5827850
    Abstract: Disclosed are: aqueous parenteral formulations for the treatment of cancer tumors comprising 1,2,4-benzotriazine 1,4-dioxides in a citrate buffer; and method of cancer tumor treatment.
    Type: Grant
    Filed: April 21, 1997
    Date of Patent: October 27, 1998
    Assignee: Sanofi Pharmaceuticals, Inc.
    Inventors: Stephen Brown, Edward Baker
  • Patent number: 5821257
    Abstract: Compounds of the formula; ##STR1## wherein: Thi is thiadiazolyl or substituted thiadiazolyl alkoxy, fluoromethyl, difluoromethyl, trifluoromethyl, 1,1-difluoroethyl, halo, alkyl, cycloalkyl, hydroxyalkyl, orY is alkylene bridge of 3-9 carbon atoms;R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl, or cyano;R.sub.3 is a heterocyclyl chosen from benzoxazolyl, benzathiazolyl, thiadiazolyl, oxazolyl, thiazolyl, oxadiazolyl, isoxazolyl, isothiazolyl, or substituted heterocyclyl wherein the substitution is with alkyl, alkoxyalkyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, thienyl, or fluoroalkyl;or a pharmaceutically acceptable salt thereof are effective antipicornaviral agents.
    Type: Grant
    Filed: March 31, 1998
    Date of Patent: October 13, 1998
    Assignee: Sanofi
    Inventors: David J. Aldous, Thomas R. Bailey, Guy Dominic Diana, Theodore J. Nitz
  • Patent number: 5817651
    Abstract: 2-R.sub.2 --R.sub.4 -substituted-3-R.sub.3 --CO-1-?(C-attached-N-heteryl)-(Alk) .sub.n !-1H-indoles useful as analgesic, anti-rheumatic, anti-inflammatory or anti-glaucoma agents.
    Type: Grant
    Filed: January 14, 1997
    Date of Patent: October 6, 1998
    Assignee: Sanofi
    Inventors: Thomas Edward D'Ambra, Edward Richard Bacon, Malcolm Rice Bell, Philip Michael Carabateas, Michael Allen Eissenstat, Virendra Kumar, John Peter Mallamo, Susan Jean Ward