Patents Examined by Mukund J. Shah
  • Patent number: 6657067
    Abstract: A method for the manufacture of chlorophthalic acid by liquid phase oxidation of chloro-ortho-xylene is disclosed. The chlorophthalic acid may be dehydrated to form chlorophthalic anhydride which is useful in the synthesis of polyetherimide.
    Type: Grant
    Filed: March 22, 2002
    Date of Patent: December 2, 2003
    Assignee: General Electric Company
    Inventors: Robert Edgar Colborn, David Bruce Hall, Peter Koch, Gerald Oeckel
  • Patent number: 6657058
    Abstract: The present invention provides a process of synthesizing a compound of Formula I by treating, in an inert medium and in the presence of an organic base, a compound of formula A with an organo metallic agent capable of acting as an outer sphere oxidant to form a compound of Formula I.
    Type: Grant
    Filed: October 18, 2002
    Date of Patent: December 2, 2003
    Assignees: Pharmacyclics, Inc., Board of Regents, University of Texas System
    Inventors: Darren Magda, Jonathan L. Sessler, Sharon Hannah
  • Patent number: 6656946
    Abstract: Compounds of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases and their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.
    Type: Grant
    Filed: August 22, 2001
    Date of Patent: December 2, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
  • Patent number: 6653472
    Abstract: New intermediates of the formula (II)B described below for the synthesis of amidine derivatives of (−)-6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid, such as for example (S)-N-{4-[4-[(3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-yl)-carbonyl]-1-piperazinyl]phenyl}-2-thiophenecarboximidamide wherein A′ is X is —Z1—CO; &rgr; is a bond or a heterocycle selected from the group consisting of piperidine, piperazine, homopiperazine, 2-methylpiperazine, 2,5-dimethyl-piperazine and 4-aminopiperidine; Y is —Z2— or —NR3—Z2, R3 is hydrogen, alkyl of 1 to 6 carbon atoms or —COR4, R4 is alkyl of 1 to 6 carbon atoms; Z1 and Z2 independently are a single bond or alkylene of 1 to 6 carbon atoms; and R6 is hydrogen or OH.
    Type: Grant
    Filed: April 26, 2002
    Date of Patent: November 25, 2003
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Christine Le Breton, Eric Manginot, Jean-Bernard Cazaux
  • Patent number: 6653316
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyrimidinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
    Type: Grant
    Filed: November 20, 2000
    Date of Patent: November 25, 2003
    Assignee: Pharmacia Corporation
    Inventors: Michael S. South, Ashton T. Hamme, II, William L. Neumann, Darin E. Jones, Melvin L. Rueppel
  • Patent number: 6653301
    Abstract: This invention describes novel pyrazole compounds of formula IIa: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-7 membered ring having 0-3 heteroatoms; and R2 and R2 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
    Type: Grant
    Filed: December 19, 2001
    Date of Patent: November 25, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Bebbington, Jean-Damien Charrier, Robert Davies, Julian M. C. Golec, David Kay, Ronald Knegtel, Sanjay Patel
  • Patent number: 6653315
    Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl or heteroaryl, cycloalkenyl, —C(═CH2)CH3, —C≡C—CH3, —CH═C(CH3)2, X is alkylene, —C(O)CH2— or —C(O)N(R2)CH2—; Y is —N(R2)CH2CH2N(R3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—N(R2)—, or optionally substituted divalent heteroaryl, piperidinyl or piperazinyl; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl or R6—C(O)—; or when Y is Z is also R6—SO2—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)— or R6OC(O)—; or when Y is 4-piperidinyl, Z can be phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl, substituted pyrrolidinyl or substituted phenyl; R14 is H, halogen or optionall
    Type: Grant
    Filed: October 11, 2002
    Date of Patent: November 25, 2003
    Assignee: Schering Corporation
    Inventors: Deen Tulshian, Lisa S. Silverman, Julius J. Matasi, Eugenia Y. Kiselgof, John P. Caldwell
  • Patent number: 6653300
    Abstract: This invention describes novel pyrazole compounds of formula I′: wherein Q′ is —O—, —C(R6′)2—, 1,2-cyclopropanediyl, 1,2-cyclobutanediyl, or 1,3-cyclopropanediyl, and R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T—R3 or L—Z—R3, or Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-7 membered ring having 0-3 heteroatoms; and R2 and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
    Type: Grant
    Filed: December 19, 2001
    Date of Patent: November 25, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Jeremy Green, David Kay, Ronald Knegtel, Andrew Miller, Ronald Tomlison, Pan Li
  • Patent number: 6653484
    Abstract: Triazine, benzotriazole and benzophenone derivatives which are substituted or bridged with polyoxyalkylene groups, according to claim 1, and their use as UV absorbers, especially in photographic materials, in inks, including inkjet inks and printing inks, in transfer prints, in paints and varnishes, organic polymeric materials, plastics, rubber, glass, packaging materials, in sunscreens of cosmetic preparations and in skin protection compositions.
    Type: Grant
    Filed: November 8, 2001
    Date of Patent: November 25, 2003
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Vien Van Toan, Andreas Valet, Pascal Hayoz
  • Patent number: 6653295
    Abstract: The present invention relates generally to a novel class of pyrimidinones of Formula (I): that are useful as serine protease inhibitors, and more particularly as Hepatitis C virus NS3 protease inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.
    Type: Grant
    Filed: December 12, 2001
    Date of Patent: November 25, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter William Glunz, Brent Dale Douty, Wei Han
  • Patent number: 6653309
    Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.
    Type: Grant
    Filed: October 30, 2000
    Date of Patent: November 25, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jeffrey O. Saunders, Daniel Elbaum, Perry M. Novak, Douglas Naegele, Randy S. Bethiel, Steven M. Ronkin, Michael C. Badia, Catharine Frank, Dean P. Stamos, William Walters, David Pearlman
  • Patent number: 6653305
    Abstract: A compound of formula (I) wherein: Ra is a benzyl or 1-phenylethyl group or a phenyl group substituted by the groups R1 and R2, wherein: R1 is a hydrogen, fluorine, chlorine, or bromine atom, or a methyl, trifluoromethyl, cyano, or ethynyl group, and R2 is a hydrogen or fluorine atom; Rb is an R3O—CO—CH2—N—CH2—CH2—OH group optionally substituted at the methylene groups by 1 or 2 methyl or ethyl groups, wherein R3 is a hydrogen atom or a C1-4-alkyl group, a 2-oxomorpholin-4-yl group optionally substituted by 1 or 2 methyl or ethyl groups, or a N-[(1,3-dioxolan-2-yl)methyl]methylamino group; Rc is a hydrogen atom, or a methoxy, ethoxy, 2-methoxyethoxy, 2-ethoxyethoxy, cyclobutyloxy, cyclopentyloxy, cyclohexyloxy, cyclopropylmethoxy, cyclobutylmethoxy, cyclopentylmethoxy, cyclohexylmethoxy, tetrahydrofuran-3-yloxy, tetrahydropyran-3-yloxy, tetrahydropyran-4-yloxy, tetrahydrofuranylmethoxy, or tetrahydropyranylmethoxy group; and n is 1, 2, or 3
    Type: Grant
    Filed: August 15, 2001
    Date of Patent: November 25, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
  • Patent number: 6652921
    Abstract: The present invention relates to wood which contains a sorbic acid store and to processes for producing the sorbic acid store in the wood or on the surface of the wood. The present invention also relates to a process for using sorbic acid and its salts for protecting wood from microbially induced degradation.
    Type: Grant
    Filed: November 8, 2001
    Date of Patent: November 25, 2003
    Assignee: Nutrinova Nutrition Specialties & Food Ingredients GmbH
    Inventors: Nico N. Raczek, Katrin Saelzer
  • Patent number: 6649787
    Abstract: An improvement is provided in a method for preparing an (meth)acrylic acid ester comprising an esterification step for forming the (meth)acrylic acid ester by esterification reaction between (meth)acrylic acid and the corresponding aliphatic alcohol having 1 to 4 carbon atoms in the presence of an acidic catalyst, and a separation-purification step comprising an acid-separating column, a low boiling matter-separating column and a rectification column for separating and purifying the (meth)acrylic acid ester from the (meth)acrylic acid ester-containing mixture obtained in the esterification step. This improvement lies in that by circulating the bottom residue of the rectification column into the esterification step and/or the separation-purification step, the remaining polymerization inhibitor in the bottom residue is effectively reused and the remaining (meth)acrylic acid ester in the bottom residue is efficiently recovered.
    Type: Grant
    Filed: October 10, 2000
    Date of Patent: November 18, 2003
    Assignee: Nippon Shokubai Co., Ltd.
    Inventors: Sei Nakahara, Masatoshi Ueoka
  • Patent number: 6649622
    Abstract: aP2 inhibiting compounds are provided having the formula wherein A, B, X, and Y are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such aP2 inhibitor or a combination of such aP2 inhibitor and another antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.
    Type: Grant
    Filed: January 26, 2001
    Date of Patent: November 18, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Richard Sulsky, Jeffrey A. Robl
  • Patent number: 6649613
    Abstract: Diacylhydrazine derivatives of general formula (I) wherein X, Y, Z, R1, 2 and R3 are as defined herein, and their physiologically acceptable salts or solvates thereof, are integrin inhibitors and can be used to combat thromboses, myocardial infarcts, coronary cardiac diseases, arteriosclerosis, inflammations, tumors, osteoporosis, infections, and restenosis following angioplasty or during pathological processes that are maintained or propagated by angiogenesis.
    Type: Grant
    Filed: January 14, 2002
    Date of Patent: November 18, 2003
    Assignee: Merck Patent GmbH
    Inventors: Günter Hölzemann, Simon Goodman, Horst Kessler, Christoph Gibson, Gabór Sulyok
  • Patent number: 6649773
    Abstract: A method for the manufacture of halophthalic acid by liquid phase oxidation of halo-ortho-xylene is disclosed. The halophthalic acid may be dehydrated to form halophthalic anhydride which is useful in the synthesis of polyetherimide.
    Type: Grant
    Filed: March 22, 2002
    Date of Patent: November 18, 2003
    Assignee: General Electric Company
    Inventors: Robert Edgar Colborn, David Bruce Hall, Peter Koch, Gerald Oeckel
  • Patent number: 6645259
    Abstract: Cationic aminoanthraquinones in which at least one cationic charge is delocalized on a 5-membered unsaturated polynitrogen-containing heterocycle, their use as a direct dye in dyeing compositions for keratinous materials, in particular for human keratinous fibers such as hair, dyeing compositions containing them, and dyeing methods using these compositions.
    Type: Grant
    Filed: July 9, 2002
    Date of Patent: November 11, 2003
    Assignee: L'Oreal S.A.
    Inventors: Alain Genet, Alain Lagrange
  • Patent number: 6645971
    Abstract: A compound given by general formula (1): [wherein T represents oxygen or sulfur atom, Y represents alkyl, cycloalkyl group, etc., ring W represents benzene ring, etc., R1 and R2 represent independently hydrogen atom, lower alkyl group, etc., and R3 represents hydrogen atom, alkyl group, etc. Z represents a group given by formula: {wherein A1 and A2 represent independently hydrogen atom, alkyl group, etc. and G represents straight chain alkylene having 1-6 of the carbon number, etc.} or a group given by formula: {wherein n represents 0, 1 or 2, ring E represents 4-8 membered saturated heterocyclic ring containing nitrogen atom(s), and A3 represents hydrogen atom, alkyl group, etc.}], its prodrug or pharmaceutically acceptable salt thereof is an antagonist against muscarinic receptor that is useful as anticholinergic medicaments, and therefore it is useful as pollakiuria or urinary incontinence remedy.
    Type: Grant
    Filed: April 10, 2001
    Date of Patent: November 11, 2003
    Assignee: Sumitomo Pharmaceuticals Company Limited
    Inventors: Masami Muraoka, Kazuki Matsui, Koji Morishita, Naohito Ohashi
  • Patent number: 6645904
    Abstract: The present invention relates to compounds of the formula in which one, two or three of the radicals R1, R2, R3 and R4 are where m and n are an integer from 1 to 10, R5, R6, R7 and R8 are, independently of one another, identical or different and are a straight-chain or branched alkyl radical having 1 to 10 carbon atoms, and the remaining radical(s) R1 to R4 are or —NR9R10, where R9 and R10 are identical or different and are a straight-chain or branched alkyl radical having 1 to 10 carbon atoms, and X− is an inorganic or organic anion or an equivalent of a multiply charged inorganic or organic anion. The invention further relates to mixtures of substances comprising compounds of the formula (1), to a process for preparing the compounds of the formula (1) and to the use thereof.
    Type: Grant
    Filed: April 30, 2002
    Date of Patent: November 11, 2003
    Assignee: Clariant GmbH
    Inventors: Berthold Schiemenz, Thomas Wessel, Ralf Pfirmann