Patents Examined by Dominic Keating
  • Patent number: 6372778
    Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: April 16, 2002
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: Roger D. Tung, Mark A. Murcko, Govinda R. Bhisetti
  • Patent number: 6258815
    Abstract: The novel specific immunophilin ligands of the general formula I have an antiasthmatic and immunosuppressive action and are suitable for the preparation of drugs.
    Type: Grant
    Filed: April 25, 1997
    Date of Patent: July 10, 2001
    Assignee: ASTA Medica Aktiengesellschaft
    Inventors: Dietmar Reichert, Bernhard Kutscher, Holger Bang, Kay Brune, Gerhard Quinkert, Hans-G√ľnter Schaible
  • Patent number: 6153662
    Abstract: Aromatic maleimides and methods using the same are disclosed. Polymerization of compositions which include the compounds of the invention may be activated by irradiating the composition with radiation.
    Type: Grant
    Filed: May 26, 1998
    Date of Patent: November 28, 2000
    Assignees: University of Southern Mississippi, First Chemical Corp.
    Inventors: Christopher W. Miller, Charles E. Hoyle, E. Sonny Jonsson
  • Patent number: 6147208
    Abstract: Caprolactam and hexamethylenediamine are prepared simultaneously starting from adiponitrile.
    Type: Grant
    Filed: June 16, 1998
    Date of Patent: November 14, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Gunther Achhammer, Peter Bassler, Rolf Fischer, Eberhard Fuchs, Hermann Luyken, Werner Schnurr, Guido Voit, Lutz Hilprecht
  • Patent number: 6133308
    Abstract: The present invention is directed to an improved synthesis of clasto-lactacystin-.beta.-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-.beta.-lactones, and analogs thereof and their use as proteosome inhibitors.
    Type: Grant
    Filed: August 14, 1998
    Date of Patent: October 17, 2000
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Fran.cedilla.ois Soucy, Louis Plamondon, Mark Behnke, William Roush
  • Patent number: 6130338
    Abstract: A method for producing pyrrolidine derivatives such as 3,4-epoxypyrrolodines, 3-pyrrolidols and the like, by oxidizing 3-pyrrolines with at least one peroxide in the presence of at least one acid is disclosed. The 3-pyrrolines are produced by deriving cis-2-butene compounds from cis-2-butene-1,4-diols and performing a cyclization between the cis-2-butene derivatives and at least one primary amine. The method may be performed as a one-pot synthesis and may be performed as a continuous reaction.
    Type: Grant
    Filed: September 3, 1999
    Date of Patent: October 10, 2000
    Assignee: Toray Industries, Inc.
    Inventors: Hideo Muraoka, Haruyo Sato
  • Patent number: 6124473
    Abstract: The present invention relates to a process for preparing (S)- and (R)-.alpha.-ethyl-2-oxo-1-pyrrolidineacetamide and (R)-.alpha.-ethyl-2-oxo-1-pyrrolidineacetamide. According to this process, the enantiomeric resolution of the racemic mixture of .alpha.-ethyl-2-oxo-1-pyrrolidineacetamide is carried out by simulated mobile bed chromatography, using at least three columns filled with chiral stationary phase.This process makes it possible to achieve good production efficiency on the industrial scale.
    Type: Grant
    Filed: May 7, 1999
    Date of Patent: September 26, 2000
    Assignee: UCB, S.A.
    Inventors: Emile Cavoy, Michel Hamende, Michel Deleers, Jean-Pierre Canvat, Vincent Zimmermann
  • Patent number: 6124465
    Abstract: Novel products of formula (I), their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments. ##STR1## In the formula (I), the following substituents are among the preferred: Ar represents a substituted or condensed phenyl radical or a polycyclic or heterocyclic aromatic radical, R represents a radical of general formula --(CH.sub.2).sub.m --X.sub.1 --(CH.sub.2).sub.n --Z in which X.sub.1 =single bond, O, S; m=0, 1; n=0, 1, 2; it being possible for the CH.sub.2 radicals to be substituted; Z represents carboxyl, COOR.sub.6 (R.sub.6 =alkyl), CON(R.sub.7)(R.sub.8) (R.sub.7 =hydrogen or alkyl and R.sub.8 =hydrogen, hydroxyl, arylsulphonyl, heterocyclyl, optionally substituted amino, optionally substituted alkyloxy or optionally substituted alkyl), PO(OR.sub.9).sub.2 (R.sub.9 =hydrogen or alkyl), an --NH--CO--T (T=hydrogen or optionally substituted alkyl) radical, or else--a ##STR2## radical, R.sub.1 and R.sub.
    Type: Grant
    Filed: July 2, 1999
    Date of Patent: September 26, 2000
    Assignee: Rhone-Poulenc S.A.
    Inventors: Jean-Dominique Bourzat, Alain Commer.cedilla.on, Norbert Dereu, Patrick Mailliet, Fabienne Sounigo-Thompson, Jean-Paul Martin, Marc Capet, Michel Cheve
  • Patent number: 6121479
    Abstract: A compound of the formula ##STR1## where R.sup.1 is the radical of the formula II or III ##STR2## is suitable for the production of a pharmaceutical for the treatment of inflammations, carcinomatous diseases, or autoimmune diseases. A compound of the formula IV ##STR3## is suitable for the production of specific antibodies against a compound of the formula I for the discovery of specific-binding proteins from cell extracts, serum, blood, or synovial fluids, for the purification of proteins, for the modification of microtiter plates, or for the preparation of chromatography material, in particular of affinity chromatography material, and for use in diagnostics.
    Type: Grant
    Filed: April 22, 1999
    Date of Patent: September 19, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Stefan Mullner, Bernd Kirschbaum, Wilfried Schwab
  • Patent number: 6118001
    Abstract: Disclosed are hydroxamic and carboxylic acid derivatives which are useful inhibitors of matrix metalloproteinase and/or TNF.alpha.-mediated diseases, including degenerative diseases and certain cancers.
    Type: Grant
    Filed: August 7, 1997
    Date of Patent: September 12, 2000
    Assignee: Darwin Discovery, Ltd.
    Inventors: David Alan Owen, John Gary Montana, John Fraser Keily, Robert John Watson, Andrew Douglas Baxter
  • Patent number: 6117822
    Abstract: Substituted phthalimidocinnamic acid derivatives I ##STR1## where R.sup.1 is H or C.sub.1 -C.sub.4 -alkyl;R.sup.2 is H or halogen;R.sup.3 is CN, NO.sub.2, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.1 -C.sub.6 -alkoxy or C.sub.1 -C.sub.6 -haloalkoxy;R.sup.4 is H, CN, NO.sub.2, halogen or C.sub.1 -C.sub.6 -alkyl;R.sup.5 is H, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.1 -C.sub.6 -cyanoalkyl, C.sub.1 -C.sub.6 -hydroxyalkyl, C.sub.1 -C.sub.6 -mercaptoalkyl, C.sub.1 -C.sub.6 -alkoxy-C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -alkylthio-C.sub.1 -C.sub.6 -alkyl;R.sup.6 is one of the radicals stated under R.sup.5 or CN, NO.sub.2, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -haloalkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -haloalkylthio, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -cycloalkyl-C.sub.1 -C.sub.6 -alkyl, (C.sub.1 -C.sub.6 -alkoxy) carbonyl-C.sub.1 -C.sub.6 -alkyl, hydroxycarbonyl-C.sub.1 -C.sub.
    Type: Grant
    Filed: June 22, 1998
    Date of Patent: September 12, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Elisabeth Heistracher, Peter Plath, Christoph-Sweder von dem Bussche-Hunnefeld, Gerhard Hamprecht, Ralf Klintz, Peter Schafer, Karl-Otto Westphalen, Helmut Walter, Matthias Gerber, Ulf Misslitz
  • Patent number: 6114371
    Abstract: The present invention relates to novel 3-(cyclohexano-heteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.
    Type: Grant
    Filed: November 12, 1998
    Date of Patent: September 5, 2000
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Li Sun, Gerald McMahon, Robert A. Blake
  • Patent number: 6114375
    Abstract: Compounds with fungicidal properties are presented having the formula ##STR1## wherein m and n are 0 or 1; X is hydrogen, halo, (C.sub.1 -C.sub.4)alkyl or alkoxy; Z is (C.sub.1 -C.sub.12) alkyl or haloalkyl; R, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are independently hydrogen, a halogen, lower alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, aryl, arylcycloalkyl, or heterocyclyl, optionally substituted with one or more halogen atoms.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: September 5, 2000
    Assignee: Rohm and Haas Company
    Inventors: Ronald Ross, Ted Tsutomo Fujimoto, Steven Howard Shaber
  • Patent number: 6114541
    Abstract: The invention is concerned with a new process for the preparation of compounds of formula ##STR1## wherein R is hydrogen, lower alkyl, lower alkoxy, cycloalkyl, cycloalkenyl, cycloalkyl-lower alkyl, lower alkenyl, lower alkynyl, aryl, aryl-lower alkyl, heterocyclyl or heterocyclyl-lower alkyl; the lower alkyl, cycloalkyl, lower alkenyl, cycloalkenyl, lower alkynyl, aryl-lower alkyl, aryl and the heterocyclyl moieties being unsubstituted or substituted with at least one group selected from carboxy, amino, carbamoyl, nitro, cyano, lower alkyl, lower alkoxy, hydroxy, halogen, aminomethyl, mercapto, trifluoromethyl and trichloroethyl.The compounds prepared according to above mentioned process are useful in the preparation of cephem, isoxacephem and carbacephem derivatives.
    Type: Grant
    Filed: February 6, 1998
    Date of Patent: September 5, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Stefan Abrecht
  • Patent number: 6114542
    Abstract: Ethers of polyalkyl or polyalkenyl N-hydroxyalkyl succinimides having the formula: ##STR1## or a fuel soluble salt thereof. The compounds of formula I are useful as fuel additives for the prevention and control of engine deposits.
    Type: Grant
    Filed: August 28, 1998
    Date of Patent: September 5, 2000
    Assignee: Chevron Chemical Company LLC
    Inventor: Richard E. Cherpeck
  • Patent number: 6114528
    Abstract: The invention is directed at novel fluorinated amide compounds of formula (1): ##STR1## wherein Rf is a divalent perfluoroalkylene or perfluoropolyether group, X is a group of formula (2), (3) or (4), and m is an integer inclusive of 0. ##STR2## R.sup.1 is a monovalent hydrocarbon group, and R.sup.2 is a divalent hydrocarbon group. These compounds can be used to obtain elastomers or cured resins having a high fluorine content and a low surface energy, making them effective as starting materials in the production of chemical and solvent-resistant elastomeric materials, parting agents, and water repellents.
    Type: Grant
    Filed: December 8, 1999
    Date of Patent: September 5, 2000
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Kouichi Yamaguchi, Noriyuki Koike, Hirofumi Kishita, Masatoshi Arai
  • Patent number: 6107491
    Abstract: Diketopyrrolopyrroles of formula I ##STR1## wherein R.sub.1 is a radical of formula II--Y--X--Z--Q (II),whereinY is --CR.sub.3 R.sub.4, --SO.sub.2 --, --CO--, --Si(Hal).sub.2 --, --POHal--, wherein R.sub.3 and R.sub.4 are each independently of the other hydrogen or C.sub.1 -C.sub.4 alkyl, and Hal is halogen,X is an unsubstituted or substituted carbocylic or heterocyclic arylene group,Z is a single bond, uninterrupted linear or branched C.sub.1 -C.sub.30 alkylene, or linear or branched C.sub.2 -C.sub.30 alkylene which is interrupted once or more than once by a hetero atom, --CH.dbd.CH--,--C.tbd.C--, --N.dbd.CH--, --CH.dbd.N-- or --NH--, or is C.sub.5 -C.sub.12 cycloalkylene,Q is a polyreactive functional group, andR.sub.2 is C.sub.1 -C.sub.6 alkyl, ##STR2## or R.sub.1, and R.sub.7 is hydrogen or C.sub.1 -C.sub.
    Type: Grant
    Filed: January 26, 1999
    Date of Patent: August 22, 2000
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Sameer Eldin
  • Patent number: 6107519
    Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)X.sub.2 --CH.sub.2 --C*H(OH)--CH.sub.2 --NH--CO--R.sub.N (VIIIA)and processes for production of pharmacologically useful oxazolidinones.
    Type: Grant
    Filed: October 13, 1998
    Date of Patent: August 22, 2000
    Assignee: Pharmacia & Upjohn Company
    Inventor: Bruce Allen Pearlman
  • Patent number: 6100275
    Abstract: A compound having the formula, ##STR1## or any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof;whereinR is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or 2-hydroxyethyl; andR.sup.4 isphenyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF.sub.3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl;3,4-methylenedioxyphenyl;benzyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF.sub.3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl;heteroaryl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF.sub.
    Type: Grant
    Filed: May 18, 1998
    Date of Patent: August 8, 2000
    Assignee: Neurosearch A/S
    Inventors: Peter Moldt, J.o slashed.rgen Scheel-Kruger, Gunnar M. Olsen, Elsebet .O slashed.stergaard Nielsen
  • Patent number: 6096778
    Abstract: This invention relates to .alpha.-ketoamide inhibitors of multicatalytic protease (MCP), to compositions including such inhibitors, and to methods for the use of MCP inhibitors. The MCP inhibitors of the present invention are useful, for example, to retard loss of muscle mass incident to various physiological states.
    Type: Grant
    Filed: October 6, 1998
    Date of Patent: August 1, 2000
    Assignee: Cephalon, Inc.
    Inventors: Sankar Chatterjee, John P. Mallamo