Plural Chalcogens Bonded Directly To Ring Carbons Of The Diazole Ring Patents (Class 548/317.1)
  • Patent number: 11739080
    Abstract: Hydantoin based compounds useful as inhibitors of matrix metalloproteinases (MMPs), particularly macrophage elastase (MMP-12) are described. Also described are related compositions and methods of using the compounds to inhibit MMP-12 and treat diseases mediated by MMP-12, such as asthma, chronic obstructive pulmonary disease (COPD), emphysema, acute lung injury, idiopathic pulmonary fibrosis (IPF), sarcoidosis, systemic sclerosis, liver fibrosis, nonalcoholic steatohepatitis (NASH), arthritis, cancer, heart disease, inflammatory bowel disease (IBD), acute kidney injury (AKI), chronic kidney disease (CKD), Alport syndrome, and nephritis.
    Type: Grant
    Filed: May 14, 2019
    Date of Patent: August 29, 2023
    Assignee: Foresee Pharmaceuticals USA, Inc.
    Inventors: Wenjin Yang, Kai-Wei Chang, Suying Liu, Cheng-Han Tsai
  • Patent number: 9023879
    Abstract: Compositions, such as pharmaceutical compositions, comprising specific diarylhydantoin and diarylthiohydantoin compounds, or salts or solvates thereof, are provided. Isolated and purified forms of the compounds are also described, as are unit dosage forms, compositions of substantially pure compound and kits comprising the compounds. The compounds and pharmaceutical compositions thereof may find use in the prevention and/or treatment of a variety of conditions, including prostate cancer, Parkinson's disease, Alzheimer's disease, and others.
    Type: Grant
    Filed: June 24, 2013
    Date of Patent: May 5, 2015
    Assignee: Medivation Prostate Therapeutics, Inc.
    Inventors: Rajendra Parasmal Jain, Jacqueline A. Gibbons
  • Patent number: 8907106
    Abstract: A process for the resolution of two enantiomers which involves inducing the preferential crystallization of one enantiomer by adjusting the composition of a suspension or solution including a racemic mixture of the two enantiomers and a solvent, by evaporation of the latter.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: December 9, 2014
    Assignee: Universite de Rouen
    Inventors: Gerard Coquerel, Guillaume Levilain
  • Publication number: 20140221591
    Abstract: There is provided a copolymer having the general structure below, wherein a, b, and d are molar ratios varying between about 0.01 and about 0.90 and c is a molar ratio varying between about 0.01 and about 0.90; A1 represents monomer units comprising a cyano-containing pendant group in which the cyano is not directly attached to the backbone of the copolymer; A2 represents monomer units comprising two or more hydrogen bonding sites; A3 represents monomer units that increase solubility in organic solvents; and A4 represents monomer units that increase solubility in aqueous alkaline solutions. There is also provided a near-infrared radiation-sensitive coating composition comprising this copolymer as well as a positive-working thermal lithographic printing plate comprising a near-infrared radiation-sensitive coating comprising this copolymer, a method of producing such a printing plate, and finally a method of printing using such a printing plate. Formula (I).
    Type: Application
    Filed: September 14, 2010
    Publication date: August 7, 2014
    Applicant: MYLAN GROUP
    Inventors: My T. Nguyen, Akha Phan, Viet-Thu Nguyen-Truong, Marc-André Locas
  • Patent number: 8648105
    Abstract: The present invention relates to diarylthiohydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: February 11, 2014
    Assignee: The Regents of the University of California
    Inventors: Michael E. Jung, Dongwon Yoo, Charles L. Sawyers, Chris Tran, John Wongvipat
  • Publication number: 20130266895
    Abstract: The present invention provides a charge control agent containing, as an active substance(s), one or two or more hydantoin derivatives represented by the following formula (1): wherein R1 and R2, which may be identical to or different from each other, represent a hydrogen atom, etc.; R3 represents a hydrogen atom, etc.; R4, to R8, which may be identical to or different from each other, represent a hydrogen atom, a chlorine atom, a linear or branched alkyl group having 1 to 8 carbon atoms which may have a substituent, etc.; R3, to R8 may be joined to each other to form a ring; and V, W, X, Y and Z represent a carbon atom or a nitrogen atom, and 0 to 3 of V, W, X, Y and Z are nitrogen atoms which have no substituent of R4 to R8.
    Type: Application
    Filed: January 17, 2012
    Publication date: October 10, 2013
    Applicant: HODOGAYA CHEMICAL CO., LTD.
    Inventors: Ikuo Kimura, Motonori Tsuji, Masaya Tojo, Masafumi Asakai
  • Patent number: 8551191
    Abstract: Dicationic azo dyes of the formula (I), which are suitable for coloring keratin fibers, in particular human hair, and are in part themselves still not described in the prior art are provided. In colorations, particularly brilliant and luminous red shades are obtained. Agents for dyeing and optionally simultaneously lightening keratin fibers and methods for dyeing and optionally simultaneously lightening keratinic fibers also are provided.
    Type: Grant
    Filed: March 4, 2013
    Date of Patent: October 8, 2013
    Assignee: Henkel AG & Co. KGaA
    Inventors: Wibke Gross, Helmut Giesa, Astrid Kroos
  • Patent number: 8524755
    Abstract: Compositions, such as pharmaceutical compositions, comprising specific diarylhydantoin and diarylthiohydantoin compounds, or salts or solvates thereof, are provided. Isolated and purified forms of the compounds are also described, as are unit dosage forms, compositions of substantially pure compound and kits comprising the compounds. The compounds and pharmaceutical compositions thereof may find use in the prevention and/or treatment of a variety of conditions, including prostate cancer, Parkinson's disease, Alzheimer's disease, and others.
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: September 3, 2013
    Assignee: Medivation Prostate Therapeutics, Inc.
    Inventors: Rajendra Parasmal Jain, Jacqueline A. Gibbons
  • Patent number: 8507692
    Abstract: An ester compound represented by formula (1): wherein R1 represents C1-C4 alkyl, has an excellent pest control effect and is therefore useful as an active ingredient of a pest control agent.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: August 13, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Noritada Matsuo
  • Patent number: 8420683
    Abstract: The present invention relates to 5-substituted hydantoins, a process for the preparation of 5-substituted hydantoins and the use of 5-substituted hydantoins in the preparation of enantiomerically enriched ?-amino acids. Furthermore, the present invention relates to the preparation of pharmaceutically active products such as perindopril and ramipril using the novel 5-substituted hydantoins.
    Type: Grant
    Filed: June 3, 2008
    Date of Patent: April 16, 2013
    Assignee: DSM Sinochem Pharmaceuticals Netherlands B.V.
    Inventors: Georgios Sarakinos, Wilhelmus Hubertus Joseph Boesten, Dennis Heemskerk, Ben De Lange
  • Publication number: 20120227545
    Abstract: This invention relates to a process for the recovery of precious metal/s from a precious metal-containing material in an aqueous leach slurry or solution. The process includes the step of contacting the precious metal/s in the leach slurry or solution with a ligand selected from dithiooxamide (rubeanic acid), or a substituted dithiooxamide. The leaching of PGMs, gold and silver from their ores using the ligand of the present invention may take place under aqueous alkaline conditions, avoiding both corrosive acidic conditions and the use of cyanide.
    Type: Application
    Filed: July 21, 2010
    Publication date: September 13, 2012
    Applicant: ANGLO OPERATIONS LIMITED
    Inventors: Diandree Padayachee, Makhosazane Chucky Kunene, Marga Retha Burger, Noko Simon Phala
  • Patent number: 8217068
    Abstract: The present invention is related to a new series of chemical compounds, namely 3-benzyl-imidazolidine-2,4-dione substituted in the position 2 and/or 6 of benzyl ring by halogens as presented to the molecule named LPSF-PT-31, GIRSUPAN and its therapeutic use as drug with analgesic, sedative and adjuvant of anesthetics activities. The invention is also related to a process for production of said compounds as well as pharmaceutical compositions comprising them.
    Type: Grant
    Filed: May 5, 2008
    Date of Patent: July 10, 2012
    Assignees: Universidade Federal de Pernambuco—UFPE, Universidade Federal do Rio de Janeiro—UFRJ
    Inventors: Ivan Da Rocha Pitta, Maria Do Carmo Alves De Lima, Teresinha Gonçalves da Silva, Gisele Zapata Sudo, Suely Lins Galdino, Roberto Takashi Sudo
  • Patent number: 8168667
    Abstract: Compounds of formula (I): wherein X is O or S, R1 is acyl, aldehyde, cycloalkyl, an optionally substituted alkyl, alkenyl or alkynyl, R2 is H, alkyl, hydroxyalkyl, haloalkyl, alkenyl, or alkynyl; substituted alkyl; alkylcarbonyl; R3 and R4 are H, halogen, alkyl, alkenyl, alkynyl, alkoxyl, alkylthio, hydroxyalkyl, haloalkyl, haloalkenyl, or haloalkynyl; or R3 and R4 form an, optionally aromatic or heterocyclic, optionally substituted ring, R5 is H, halogen, trifluoromethyl, —CN, or —NO2; not all of R3, R4, and R5 being H, R6 and R9 are H, halogen, OH; alkyl, hydroxyalkyl, alkoxyl, thioalkyl, haloalkyl, alkenyl, or alkynyl; R7 and R8 are H, halogen, OH, SH; alkoxyl or alkylthio optionally substituted by OH and/or halogen; one of R7 and R8 not being H or halogen; or one of R7 and R8 is a pharmaceutically acceptable ester or thioester grouping, or R6 is C1-3-alkyl or, together with either R1 or R2, represents C1-3 alkylene or alkenylene linking group, optionally substituted by methyl, trifluoromethyl, OH, or
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: May 1, 2012
    Assignee: Galapagos NV
    Inventors: Francois Nique, Catherine Jagerschmidt, Philippe Clement-Lacroix
  • Patent number: 8067458
    Abstract: The invention relates to new alkoxyalkyl-substituted cyclic ketoenols of the formula (I) in which A, B, D, G, W, X and Y have the definitions indicated above, to processes and intermediates for their preparation, and to their use as pesticides and/or microbicides and/or herbicides. The invention further provides selectively herbicidal compositions which comprise alkoxyalkyl-substituted cyclic ketoenols on the one hand and a crop plant tolerance promoter compound on the other. The invention further relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the additions of ammonium salts or phosphonium salts and optionally penetration promoters.
    Type: Grant
    Filed: April 12, 2007
    Date of Patent: November 29, 2011
    Assignee: Bayer Cropscience AG
    Inventors: Reiner Fischer, Stefan Lehr, Dieter Feucht, Ulrich Görgens, Olga Malsam, Jan Dittgen, Martin Jeffrey Hills, Heinz Kehne, Christopher Hugh Rosinger
  • Patent number: 8039499
    Abstract: An ester compound represented by the formula (I): (wherein, R1 represents a C1-C3 alkyl group, a 2-propenyl group or a 2-propynyl group.) has excellent pest controlling activity and is useful as an active ingredient for a pest controlling agent.
    Type: Grant
    Filed: August 24, 2007
    Date of Patent: October 18, 2011
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Jun Ohshita, Toru Uekawa
  • Patent number: 7932400
    Abstract: An object of the present invention is to provide an industrially suitable process for preparing an imidazolidin-2,4-dione compound which is safe, simple and easy to prepare the imidazolidin-2,4-dione compound with high yield, which is a useful compound, for example, as a material for decomposing a harmful halogenated aromatic hydrocarbon compound such as dioxin, etc., an electroless silver plating solution for electronic parts, or a diazo copying material, etc. This object can be solved by a process for preparing an imidazolidin-2,4-dione compound which comprises subjecting a 4,5-dihydroxy-2-imidazolidinone compound, (1) to dehydration reaction in the presence of an acid catalyst(s); or (2) to reaction at 100 to 300° C. Or, it can be solved by a process for preparing an imidazolidin-2,4-dione compound which comprises reacting a mixed solution of a urea compound, glyoxal, and a base at 20 to 300° C.
    Type: Grant
    Filed: July 13, 2007
    Date of Patent: April 26, 2011
    Assignee: Ube Industries, Ltd.
    Inventors: Shigeyoshi Nishino, Hidetaka Shima, Tetsuro Shimano, Kimihiko Yoshimura
  • Publication number: 20110053947
    Abstract: The invention relates to compounds of formula (I) wherein the groups R and R?, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.
    Type: Application
    Filed: August 6, 2010
    Publication date: March 3, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Gerhard JAEHNE, Siegfried STENGELIN, Matthias GOSSEL, Thomas KLABUNDE, Irvin WINKLER
  • Patent number: 7803826
    Abstract: The present invention provides a compound represented by formula (I): wherein n is an integer selected from 1 to 20, Q is A is cyano or the like; B is hydrogen, halogen, or the like; X1 and X2 are each independently selected from O and S; E is a C1-4 alkyl group; and R1, R2, R3 and R4 are each independently selected from a hydrogen atom and a C1-C6 alkyl group, and a drug, a pharmaceutical composition containing the compound, and the like.
    Type: Grant
    Filed: August 3, 2005
    Date of Patent: September 28, 2010
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Kazutaka Tachibana, Haruhiko Sato, Masateru Ohta, Mitsuaki Nakamura, Takuya Shiraishi, Ikuhiro Imaoka, Hitoshi Yoshino, Masahiro Nagamuta, Hiromitsu Kawata
  • Publication number: 20100216855
    Abstract: Imidazolone derivatives, as medicaments, of formula wherein: R1?H, C1 to C5 alkyl, aryl or a 5- or 6-membered heterocyclic group; Ar1=optionally substituted aryl or an aromatic heterocycle; R?R2—S—, R3—HN—, R4COHN or Ar2, with R2=a C1-C5 alkyl, vinyl or vinyl(C1-C5)alkyl, nitrile or nitrile(C1-C5)alkyl, aryl or benzyl radical, which are optionally substituted; R3=the meanings given above and H; Ar2=substituted or unsubstituted aryl.
    Type: Application
    Filed: August 1, 2008
    Publication date: August 26, 2010
    Inventors: Francois Carreaux, Jean-Pierre Bazureau, Steven Renault, Laurent Meijer, Olivier Lozach
  • Patent number: 7772403
    Abstract: A novel process for the preparation of hydantoin sulfonyl chlorides of general formula (I) wherein R and n are as specified in the description, and certain novel intermediates thereto, are disclosed.
    Type: Grant
    Filed: March 15, 2007
    Date of Patent: August 10, 2010
    Assignee: AstraZeneca AB
    Inventors: Philip Cornwall, Daniel Horner
  • Patent number: 7767811
    Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.
    Type: Grant
    Filed: June 5, 2006
    Date of Patent: August 3, 2010
    Assignee: Brandeis University
    Inventors: Li Deng, Jianfeng Hang, Liang Tang
  • Patent number: 7759493
    Abstract: Bicyclic compounds containing a phenyl or pyridyl ring fused to a cycloalkyl or heterocyclic ring, to which is attached a 5-membered heterocyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
    Type: Grant
    Filed: January 30, 2006
    Date of Patent: July 20, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Min Ge, Lihu Yang, Changyou Zhou, Songnian Lin, Haifeng Tang, Eric Dean Cline, Sunita Malkani
  • Publication number: 20100174092
    Abstract: The present invention relates to 5-substituted hydantoins, a process for the preparation of 5-substituted hydantoins and the use of 5-substituted hydantoins in the preparation of enantiomerically enriched ?-amino acids. Furthermore, the present invention relates to the preparation of pharmaceutically active products such as perindopril and ramipril using the novel 5-substituted hydantoins.
    Type: Application
    Filed: June 3, 2008
    Publication date: July 8, 2010
    Inventors: Georgios Sarakinos, Wilhelmus Hubertus Joseph Boesten, Dennis Heemskerk, Ben De Lange
  • Publication number: 20100143981
    Abstract: The present invention relates to a whole cell catalytic system for the preparation of an enantiomerically enriched ?-amino acid from a corresponding hydantoin wherein hydantoinase, L-carbamoylase and hydantoin racemase are coexpressed in a recombinant micro-organism wherein the genes coding for these three enzymes are located on a single replicon. The present invention further relates to the use of such a whole cell catalytic system according in the preparation of an enantiomerically enriched L-?-amino acid from a corresponding hydantoin.
    Type: Application
    Filed: December 4, 2007
    Publication date: June 10, 2010
    Inventors: Monika Rusnak-Müller, Oliver May, Petrus Johannes Hermsen, Henricus Martinus Maria Gerardus Straatman, Wolfgang Skranc, Wilhelmus Hubertus Joseph Boesten, Dannis Heemskerk, Ben De Lange, Georgios Sarakinos
  • Publication number: 20100130575
    Abstract: The present invention is related to a new series of chemical compounds, namely 3-benzyl-imidazolidine-2,4-dione substituted in the position 2 and/or 6 of benzyl ring by halogens as presented to the molecule named LPSF-PT-31, GIRSUPAN and its therapeutic use as drug with analgesic, sedative and adjuvant of anesthetics activities. The invention is also related to a process for production of said compounds as well as pharmaceutical compositions comprising them.
    Type: Application
    Filed: May 5, 2008
    Publication date: May 27, 2010
    Inventors: Ivan Da Rocha Pitta, Maria Do Carmo Alves De Lima, Teresinha Goncalves Da Silva, Gisele Zapata Sudo, Suely Lins Galdino, Roberto Takashi Sudo
  • Patent number: 7713967
    Abstract: Compounds comprising a structure or a pharmaceutically acceptable salt thereof, or a prodrug thereof; wherein a dashed line represents the presence or absence of a bond are disclosed, wherein Y, A, B, and J are as described. Methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: May 1, 2009
    Date of Patent: May 11, 2010
    Assignee: Allergan, Inc.
    Inventor: David W. Old
  • Patent number: 7709517
    Abstract: The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.
    Type: Grant
    Filed: May 15, 2006
    Date of Patent: May 4, 2010
    Assignee: The Regents of the University of California
    Inventors: Charles L. Sawyers, Michael E. Jung, Charlie D. Chen, Samedy Ouk, Derek Welsbie, Chris Tran, John Wongvipat, Dongwon Yoo
  • Patent number: 7683088
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.
    Type: Grant
    Filed: January 16, 2007
    Date of Patent: March 23, 2010
    Assignee: Schering Corporation
    Inventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Bandarpalle B. Shankar, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Aneta M. Micula, Seong-Heon Kim, De-Yi Yang, Razia Rizvi
  • Publication number: 20100063118
    Abstract: The present invention relates to hydantoin derivatives having RNase H, polymerase and/or HIV reverse transcriptase modulatory, and particularly, inhibitory activity. Included in the invention are the hydantoin derivatives, compositions containing the derivatives, methods of synthesis of the derivatives, screening methods to identify the derivatives, and methods of treatment using the hydantoin derivatives, including the treatment of HIV, AIDS and retrovirus-associated cancer.
    Type: Application
    Filed: July 10, 2009
    Publication date: March 11, 2010
    Applicant: Wyeth
    Inventors: Matthew W. Olson, Martin Di Grandi, Amarnauth Prashad
  • Patent number: 7666892
    Abstract: Compounds of the formula (I) wherein Z is SO2(N6) or N(R7)SO2 or N(R7)SO2N(R6) useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.
    Type: Grant
    Filed: May 5, 2008
    Date of Patent: February 23, 2010
    Assignee: AstraZeneca AB
    Inventors: Anders Eriksson, Matti Lepistö, Michael Lundkvist, Magnus Munck Af Rosenschöld, Pavol Zlatoidsky
  • Patent number: 7652143
    Abstract: The present invention relates to a novel compound of the formula I: and/or all stereoisomeric forms of the compound of the formula I and/or mixtures of these forms in any ratio, and/or a physiologically tolerated salt of the compound of the formula I, in which R1 to R5 and V1, V2 have the meanings stated in the claims and specification. The inventive compounds are suitable as inhibitors of metalloproteases, especially of ADAMTS proteases and TNF-? converting enzyme (TACE), and for the treatment of disorders such as but not limited to osteoarthrosis and rheumatoid arthritis.
    Type: Grant
    Filed: June 15, 2007
    Date of Patent: January 26, 2010
    Assignee: sanofi-aventis Deutschland GmbH
    Inventors: Andreas Lindenschmidt, Holger Wagner, Jochen Beninga, Sven Grueneberg, Klaus-ulrich Weithmann
  • Publication number: 20100010233
    Abstract: An object of the present invention is to provide an industrially suitable process for preparing an imidazolidin-2,4-dione compound which is safe, simple and easy to prepare the imidazolidin-2,4-dione compound with high yield, which is a useful compound, for example, as a material for decomposing a harmful halogenated aromatic hydrocarbon compound such as dioxin, etc., an electroless silver plating solution for electronic parts, or a diazo copying material, etc. This object can be solved by a process for preparing an imidazolidin-2,4-dione compound which comprises subjecting a 4,5-dihydroxy-2-imidazolidinone compound, (1) to dehydration reaction in the presence of an acid catalyst(s); or (2) to reaction at 100 to 300° C. Or, it can be solved by a process for preparing an imidazolidin-2,4-dione compound which comprises reacting a mixed solution of a urea compound, glyoxal, and a base at 20 to 300° C.
    Type: Application
    Filed: July 13, 2007
    Publication date: January 14, 2010
    Inventors: Shigeyoshi Nishino, Hidetaka Shima, Tetsuro Shimano, Kimihiko Yoshimura
  • Publication number: 20100010049
    Abstract: Compounds corresponding to the following general formula (I): are formulated into pharmaceutical compositions useful in human or veterinary medicine or else into cosmetic compositions; novel compounds of formula (II) are also thus useful:
    Type: Application
    Filed: January 12, 2009
    Publication date: January 14, 2010
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Itaru Suzuki, Irène Erdelmeier, Jean-Claude Yadan, Isabelle Pelisson
  • Patent number: 7612212
    Abstract: The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.
    Type: Grant
    Filed: January 25, 2007
    Date of Patent: November 3, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Shaoqing Chen, Nicholas J. S. Huby, Norman Kong, Steven Gregory Mischke, John Anthony Moliterni, Hong Wang, Zhuming Zhang
  • Patent number: 7572816
    Abstract: The present invention is directed to compounds having the structure wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells.
    Type: Grant
    Filed: July 21, 2004
    Date of Patent: August 11, 2009
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Bruno Tse, Sepehr Sarshar
  • Patent number: 7521465
    Abstract: Novel diphenyl ether derivatives are provided that exhibit activity useful for reducing glucose, cholesterol, and/or triglyceride levels in plasma, and for treatment of obesity, inflammation, immunological diseases, autoimmune diseases, diabetes and disorders associated with insulin resistance.
    Type: Grant
    Filed: March 31, 2005
    Date of Patent: April 21, 2009
    Assignee: Bexel Pharmaceuticals, Inc.
    Inventors: Bishwajit Nag, Abhijeet Nag, Debendranath Dey, Shiv Kumar Agarwal, Partha Neogi, Gaddam Om Reddy, Sangamesh Badiger, Gajendra Singh, Surendra Kumar Pandey, Santhanagopalan Chithra
  • Patent number: 7514462
    Abstract: The invention relates to the use of derivatives of E-type prostaglandins as EP2 agonists, in general, and, in particular as ocular hypotensives. The PGE derivatives used in accordance with the invention are represented by the following formula I: wherein the hatched segment represents an ? bonds, the solid triangle represents a ? bond, the wavy segments represent ? or ? bond, dashed lines represent a double bond or a single bond, X is selected from the group consisting of hydrogen and halogen radicals, R3 is heteroaryl or a substituted heteroaryl radical, R1 and R2 are independently selected from the group consisting of hydrogen or a lower alkyl radical having up to six carbon atoms, or a lower acyl radical having up to six carbon atoms, R is selected from the group consisting of CO2R4, CONR42, CH2OR4, CONR4SO2R4, P(O)(OR4) and wherein R4 is selected from the group consisting of H, phenyl and lower alkyl having from one to six carbon atoms and n is 0 or an integer of from 1 to 4.
    Type: Grant
    Filed: June 6, 2007
    Date of Patent: April 7, 2009
    Assignee: Allergan, Inc.
    Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner
  • Patent number: 7511149
    Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.
    Type: Grant
    Filed: February 9, 2007
    Date of Patent: March 31, 2009
    Assignee: Dow AgroSciences LLC
    Inventors: Kim E. Arndt, Douglas C. Bland, David E. Podhorez, James R. McConnell
  • Publication number: 20080241896
    Abstract: The present invention provides a production method of optically active hydroxymethyl-substituted phenylalanine, which includes reducing cyano-substituted benzylidene hydantoin (1) to give aminomethyl-substituted benzyl hydantoin (2) or a salt thereof, converting an amino group of the aminomethyl-substituted benzyl hydantoin (2) or a salt thereof to a hydroxyl group to give hydroxymethyl-substituted benzyl hydantoin (3), treating the hydroxymethyl-substituted benzyl hydantoin (3) with an enzyme to give D-hydroxymethyl-substituted phenylalanine (4a) or a salt thereof, or L-hydroxymethyl-substituted phenylalanine (4b) or a salt thereof. According to the present invention, a production method capable of conveniently producing optically active hydroxymethyl-substituted phenylalanine on an industrial scale can be provided.
    Type: Application
    Filed: September 24, 2007
    Publication date: October 2, 2008
    Applicant: Ajinomoto Co., Inc.
    Inventors: Masakazu NAKAZAWA, Atsuko Hashimoto, Hiroyuki Nozaki
  • Patent number: 7427631
    Abstract: Compounds of the formula (I) wherein z is SO2 or SO, useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.
    Type: Grant
    Filed: March 13, 2002
    Date of Patent: September 23, 2008
    Assignee: AstraZeneca AB
    Inventors: Anders Eriksson, Matti Lepistö, Michael Lundkvist, Magnus Munck Af Rosenschöld, Pavol Zlatoidsky
  • Publication number: 20070197617
    Abstract: The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.
    Type: Application
    Filed: January 25, 2007
    Publication date: August 23, 2007
    Inventors: Shaoqing Chen, Nicholas J. S. Huby, Norman Kong, Steven Gregory Mischke, John Anthony Moliterni, Hong Wang, Zhuming Zhang
  • Patent number: 7226940
    Abstract: The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel Disease
    Type: Grant
    Filed: August 24, 2005
    Date of Patent: June 5, 2007
    Assignees: Incyte San Diego, Inc., Ortho McNeil Pharmaceutical Inc.
    Inventors: Magnus Pfahl, Catherine Tachdjian, Hussien A. Al-Shamma, Andrea Fanjul, David P. M. Pleynet, Lyle W. Spruce
  • Patent number: 7179831
    Abstract: 5-[3-(4-benzyloxyphenylthio)-fur-2-yl]-imidazolidin-2,4-dione and analogues useful as inhibitors of macrophage elastase are disclosed.
    Type: Grant
    Filed: August 17, 2005
    Date of Patent: February 20, 2007
    Assignee: Quest Pharmaceutical Services
    Inventor: Fude Yang
  • Patent number: 7138526
    Abstract: A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide.
    Type: Grant
    Filed: June 13, 2000
    Date of Patent: November 21, 2006
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Timothy F. Herpin, George C. Morton, Joseph M Salvino
  • Patent number: 7125871
    Abstract: Compounds of the formula (I) in which R1, R2 and X1 have the meanings given in the specification, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous system
    Type: Grant
    Filed: May 24, 2001
    Date of Patent: October 24, 2006
    Assignee: Eli Lilly and Company
    Inventors: Ivan Collado Cano, Jesus Ezquerra-Carrera, Alicia Marcos Liorente, Luisa Maria Martin-Cabrejas, James Allen Monn
  • Patent number: 7102013
    Abstract: Method of making an alpha-amino acid compound having the structure of Formula 32: comprising treating under hydrolyzing conditions a hydantoin compound having the structure of Formula 33: where the substituents are described herein.
    Type: Grant
    Filed: December 17, 2002
    Date of Patent: September 5, 2006
    Assignee: Pharmacia Corporation
    Inventors: Ronald Keith Webber, Richard C. Durley, Alok K. Awasthi, Arija A. Bergmanis, Kam F. Fok, Scott S. Ganser, Timothy J. Hagen, E. Ann Hallinan, Donald W. Hansen, Jr., Brian S. Hickory, Pamela T. Manning, Michael Mao, Alan E. Moormann, Barnett S. Pitzele, Michelle A. Promo, Richard R. Schartman, Jeffrey A. Scholten, Jeffrey S. Snyder, Mihaly V. Toth, Mahima Trivedi, Sofya Tsymbalov, Foe Siong Tjoeng
  • Patent number: 7084208
    Abstract: The present invention provides heterocyclic vinylic compounds that can be used to form biocidal polymers. The polymers thus generated can used alone or can be grafted onto textiles, fabrics and polymers. The polymers are readily converted to N-halamine structures on exposure to a halogen source such as commercially available chlorine bleach. The N-halamine derivatives exhibit potent antibacterial properties against microorganisms and these properties are durable and regenerable.
    Type: Grant
    Filed: May 6, 2003
    Date of Patent: August 1, 2006
    Assignee: Regents of the University of California
    Inventors: Gang Sun, Yuyu Sun
  • Patent number: 7071218
    Abstract: The present invention relates to certain compounds of Formula (I) which can be useful in the treatment of diseases, such as, cancer, metabolic disorders, Type 2 Diabetes, dyslipidemia and/or hyperchloesterolemia:
    Type: Grant
    Filed: November 15, 2002
    Date of Patent: July 4, 2006
    Assignees: Incyte San Diego Incorporated, Ortho McNeil Pharmaceutical Inc.
    Inventors: Magnus Pfahl, Catherine Tachdjian, Lyle W. Spruce, Hussien A. Al-Shamma, Mohamed Boudjelal, Andrea N. Fanjul, Torsten R. Wiemann, David P. M. Pleynet
  • Patent number: 7057038
    Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.
    Type: Grant
    Filed: May 26, 2004
    Date of Patent: June 6, 2006
    Assignee: Brandeis University
    Inventors: Li Deng, Jianfeng Hang, Liang Tang
  • Patent number: 7034015
    Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.
    Type: Grant
    Filed: August 28, 2002
    Date of Patent: April 25, 2006
    Assignee: Leo Pharma A/S
    Inventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang