Sulfur In Substituent Q Patents (Class 564/162)
  • Publication number: 20150141513
    Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of neurological degenerative disorders and neurological diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of narcolepsy, shift work sleep disorder, and as an adjunct treatment for obstructive sleep apnea/hypopnea, hypersomnias, like idiopathic hypersomnia, Psychiatric/neurodegenerative disorders, ADHD, Psychiatric/neurodegenerative disorders, Depersonalization disorder, Cognitive enhancement, Fatigue, Post-chemotherapy cognitive impairment and weight loss.
    Type: Application
    Filed: April 19, 2013
    Publication date: May 21, 2015
    Inventor: Mahesh Kandula
  • Patent number: 9005598
    Abstract: Novel compounds of the general formula (I): in which X represents a polymer; Q represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; each of R1 and R2 independently represents a hydrogen atom or a C1-4alkyl group; and either Z1 represents a protein or a peptide linked to CR2 via a nucleophilic moiety, and Z2 represents a molecule linked to CR2 via a nucleophilic moiety, or Z1 and Z2 together represent a single group derived from a protein or peptide linked to CR via two nucleophilic moieties.
    Type: Grant
    Filed: March 4, 2010
    Date of Patent: April 14, 2015
    Assignee: Polytherics Limited
    Inventors: Antony Robert Godwin, Stephen James Brocchini
  • Publication number: 20150094276
    Abstract: This invention relates to novel substituted styryl benzylsulfones that are multikinase inhibitors and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by an agent that inhibits kinases, such as phosphatidylinositol 3-kinase (PI3-K) and polo-like kinase (PLK-1).
    Type: Application
    Filed: April 19, 2013
    Publication date: April 2, 2015
    Inventor: Roger D. Tung
  • Patent number: 8975442
    Abstract: The invention relates to a polymorphic form of (?)-modafinil that produces a powder X-ray diffraction spectrum comprising intensity peaks corresponding to interplanar spacings of about 14.14, 10.66, 7.80 and 4.02 ?, and a process for the preparation thereof.
    Type: Grant
    Filed: August 28, 2013
    Date of Patent: March 10, 2015
    Assignee: Teva Sante
    Inventors: Pierre Leproust, Olivier Neckebrock
  • Publication number: 20150045367
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.
    Type: Application
    Filed: December 19, 2012
    Publication date: February 12, 2015
    Inventors: Erik Verner, Wei Chen, Sriram Balasubramanian
  • Patent number: 8937083
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.
    Type: Grant
    Filed: October 24, 2012
    Date of Patent: January 20, 2015
    Assignee: DowAgroSciences, LLC
    Inventors: Noormohamed M. Niyaz, Negar Garizi, Yu Zhang, Tony K. Trullinger, Ricky Hunter, Ann M. Buysse, Asako Kubota, Paul Renee LePlae, Jr., Daniel Knueppel, Christian T. Lowe, Dan Pernich, David A. Demeter, Timothy C. Johnson
  • Patent number: 8895772
    Abstract: The present invention provide processes for the preparation of N-[4-Cyano-3-(trifluoro methyl)phenyl]-3-[(4-fluorophenyl)sulphonyl]-2-hydroxy-2-methyl propanamide (I). The present application also provides a method of purification of N-[4-Cyano-3-(trifluoro methyl)phenyl]-3-[(4-fluorophenyl)sulphonyl]-2-hydroxy-2-methyl propanamide (I) using ethyl acetate solvent resulting in the product, substantially free from process related impurities A, B, C and D. The crystalline product of the process according to the present invention having an XRDP pattern as per FIG. 1, is useful as an active pharmaceutical and has anti-androgenic activity.
    Type: Grant
    Filed: August 29, 2011
    Date of Patent: November 25, 2014
    Assignee: Shilpa Medicare Limited
    Inventors: Vimal Kumar Shrawat, Karri Papa Rao, Rafiuddin, Prashant Purohit
  • Patent number: 8871208
    Abstract: A method for treating a patient suffering from inflammation, chronic inflammation, pain, rheumatoid arthritis (RA), osteoarthritis and osteoporosis, comprising administering an effective amount of a selective inhibitor of the 11-?-hydroxysteroid dehydrogenase Type 1 enzyme.
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: October 28, 2014
    Assignee: AbbVie Inc.
    Inventors: Peer B. Jacobson, Lisa M. Olson, Sreeinvasarao Vepachedu
  • Publication number: 20140296333
    Abstract: The present invention relates to modafinil or derivatives thereof as a medicine for the treatment of vascular diseases or KCa3.1 channel (Ca activated K channel) mediated diseases and a novel use of the same. More specifically, the present invention relates to a pharmaceutical composition for the prevention or treatment of vascular diseases or KCa3.1 channel-mediated diseases comprising modafinil or a derivative of modafinil, or pharmaceutically acceptable salts thereof which relax blood vessels and inhibit KCa3.1 channel currents by increasing intracellular cAMP, a method for treating vascular diseases or KCa3.1 channel-mediated diseases using the composition and a health functional food composition for the prevention or improvement of vascular diseases or the KCa3.1 channel-mediated diseases comprising modafinil or a modafinil derivative compound, or sitologically acceptable salts thereof.
    Type: Application
    Filed: October 24, 2012
    Publication date: October 2, 2014
    Applicant: EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATION
    Inventors: Suk Hyo Suh, Jae Chul Jung, Sei Kwan Oh
  • Publication number: 20140256743
    Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Application
    Filed: May 20, 2014
    Publication date: September 11, 2014
    Applicants: Merck Frosst Canada Ltd., Axys Pharmaceuticals, Inc.
    Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien, Michael J. Green, Bernard L. Hirschbein, James William Janc, James T. Palmer, Chitra I. Baskaran
  • Publication number: 20140235702
    Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having sulfonamido-1-hydroxynaphthalene structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.
    Type: Application
    Filed: October 8, 2012
    Publication date: August 21, 2014
    Inventors: Zaneta Nikolovska-Coleska, Hollis D. Showalter, Chenzhong Liao, Ramzi Mohammad, Fardokht Abulwerdi
  • Patent number: 8809586
    Abstract: Polymorphs and solvates of racemic, enantiomerically pure, and enantiomerically mixed modafinil are formed and discussed. In addition, said forms are described as useful for the treatment of many conditions including, but not limited to, narcolepsy.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: August 19, 2014
    Assignee: Cephalon, Inc.
    Inventors: Magali Bourghol Hickey, Matthew Peterson, Orn Almarsson, Mark Oliveira
  • Patent number: 8759583
    Abstract: The invention relates to a method for preparing a sulphoxide compound of formula (I) either as a single enantiomer or in an enantiomerically enriched form, comprising the steps of: a) contacting a pro-chiral sulphide of formula (II) with a metal chiral complex, a base and an oxidizing agent in an organic solvent; and optionally b) isolating the obtained sulphoxide of formula (I). wherein n, Y, R1, R1a, R2 and R2a are as defined in claim 1.
    Type: Grant
    Filed: November 1, 2012
    Date of Patent: June 24, 2014
    Assignee: Teva Sante
    Inventors: Laurent Courvoisier, Gerard Duret, Stephanie Graf, Laurence Prat-Lacondemine, Francois Rebiere, Nicolas Sabourault
  • Publication number: 20140148468
    Abstract: The invention relates to specific carboxamides, to processes for their preparation, to medicaments comprising these compounds and to the use of these compounds in the preparation of medicaments.
    Type: Application
    Filed: November 27, 2013
    Publication date: May 29, 2014
    Applicant: GRÜNENTHAL GMBH
    Inventors: Simon LUCAS, Sven Kühnert, Gregor Bahrenberg, Wolfgang Schröder
  • Patent number: 8729305
    Abstract: The invention relates to a polymorphic form of (?)-modafinil that produces a powder X-ray diffraction spectrum comprising intensity peaks corresponding to interplanar spacings of about 14.14, 10.66, 7.80 and 4.02 ?, and a process for the preparation thereof.
    Type: Grant
    Filed: April 8, 2013
    Date of Patent: May 20, 2014
    Assignee: Teva Sante
    Inventors: Pierre Leproust, Olivier Neckebrock
  • Publication number: 20140113898
    Abstract: The invention relates to bisarylsulfone and dialkylarylsulfone compounds (e.g., compounds according to any of Formulas (I)-(IX) or compounds (1)-(227) of Tables 4 and 5) useful in treating conditions associated with calcium channel function, and particularly conditions associated with N-type calcium channel activity. The invention also relates to pharmaceutical compositions that include these bisarylsulfone compounds, as well methods for the treatment of conditions such as cardiovascular disease, epilepsy, cancer and pain.
    Type: Application
    Filed: November 4, 2011
    Publication date: April 24, 2014
    Applicant: Zalicus Pharmaceuticals Ltd.
    Inventors: Hassan A. Pajouhesh, Richard Holland, Yuanxi Zhou, Yongbao Zhu, Michael Edward Grimwood, Navjot Chahal
  • Publication number: 20140107368
    Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(=G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.
    Type: Application
    Filed: December 11, 2013
    Publication date: April 17, 2014
    Applicant: Mitsui Chemicals Agro, Inc.
    Inventors: Yumi Kobayashi, Hiroyuki Katsuta, Michikazu Nomura, Hidetaka Tsukada, Atsushi Hirabayashi, Hidenori Daido, Yusuke Takahashi, Shinichi Banba
  • Publication number: 20140088157
    Abstract: Provided are an endoparasite control agent comprising a carboxamide derivative represented by the general formula (I): or a salt thereof as an active ingredient, and a method for controlling endoparasites, comprising orally or parenterally administering the endoparasite control agent.
    Type: Application
    Filed: March 1, 2012
    Publication date: March 27, 2014
    Applicants: NIHON NOHYAKU CO., LTD., THE UNIVERSITY OF TOKYO
    Inventors: Kiyoshi Kita, Akiyuki Suwa
  • Patent number: 8653134
    Abstract: Compounds of the formula (I): in which A, R1, R2, X, Y and Z are defined in the description, the processes for the preparation of these compounds, the uses thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, and the pharmaceutical compositions comprising them.
    Type: Grant
    Filed: December 22, 2005
    Date of Patent: February 18, 2014
    Assignee: Merck Patent GmbH
    Inventors: Catherine Vidal, Nathalie Adje, Stéphane Yvon, Jean Jacques Zeiller
  • Patent number: 8642799
    Abstract: Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition or decreasing function of these proteases can be useful in the treatment and/or prevention of these parasitic diseases including; toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, schistosomiasis, amebiasis, giardiasis, clonorchiasis, opisthorchiasis, paragonimiasis, fasciolopsiasis, lymphatic filariasis, onchocerciasis, dracunculiasis, ascariasis, trichuriasis, stronglyoidiasis, trichostrongyliasis, trichomoniasis or cestodiasis.
    Type: Grant
    Filed: April 11, 2013
    Date of Patent: February 4, 2014
    Assignee: Merck Canada Inc.
    Inventors: Elise Isabel, Christopher Mellon, Christian Beaulieu
  • Publication number: 20140031589
    Abstract: The invention relates to a polymorphic form of (?)-modafinil that produces a powder X-ray diffraction spectrum comprising intensity peaks corresponding to interplanar spacings of about 14.14, 10.66, 7.80 and 4.02 ?, and a process for the preparation thereof.
    Type: Application
    Filed: August 28, 2013
    Publication date: January 30, 2014
    Applicant: Teva Sante
    Inventors: Pierre Leproust, Olivier Neckebrock
  • Publication number: 20140024679
    Abstract: The present invention provides novel phenylcycloalkylmethylamine derivatives, and methods of preparing phenylcycloalkylmethylamine derivatives. The present invention also provides methods of using phenylcycloalkylmethylamine derivatives and compositions of phenylcycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.
    Type: Application
    Filed: December 31, 2012
    Publication date: January 23, 2014
    Applicant: Reviva Pharmaceuticals, Inc.
    Inventor: Reviva Pharmaceuticals, Inc.
  • Publication number: 20130338231
    Abstract: The invention provides compound of the general formula: in which each X independently represents a polymer chain; n represents an integer greater than 1; Q represents a linker; Y represents an amide group; and Z represents either —CH.(CH2L)2 or —C(CH2L)(?CH2), in which each L independently represents a leaving group. The compounds are useful reagents for the conjugation of polymers to proteins, the resulting conjugates being novel and also forming part of the invention.
    Type: Application
    Filed: June 17, 2013
    Publication date: December 19, 2013
    Inventors: Antony GODWIN, Stephen Brocchini
  • Publication number: 20130295196
    Abstract: The invention relates to the molecule having formula (I), as well as the enantiomers thereof, and to the use of same in the treatment of ADHD, narcolepsy or idiopathic hypersomnia.
    Type: Application
    Filed: January 20, 2012
    Publication date: November 7, 2013
    Applicant: ASSISTANCE PUBLIQUE-HOPITAUX DE PARIS
    Inventor: Eric Konofal
  • Publication number: 20130289122
    Abstract: Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing them are useful as sodium and/or calcium channel modulators for preventing, alleviating and curing pathologies wherein the above mechanisms play a pathological role. The compounds may be particularly useful for the prevention, alleviation, and curing of, for example, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases.
    Type: Application
    Filed: March 11, 2013
    Publication date: October 31, 2013
    Inventor: Newron Pharmaceuticals S.P.A.
  • Publication number: 20130274521
    Abstract: The invention relates to a polymorphic form of (?)-modafinil that produces a powder X-ray diffraction spectrum comprising intensity peaks corresponding to interplanar spacings of about 14.14, 10.66, 7.80 and 4.02 ?, and a process for the preparation thereof.
    Type: Application
    Filed: April 8, 2013
    Publication date: October 17, 2013
    Inventors: Pierre Leproust, Olivier Neckebrock
  • Patent number: 8557812
    Abstract: The invention relates to small molecules which function as inhibitors of anti-apoptotic Bcl-2 family member proteins (e.g., Bcl-2 and Bcl-xL). The invention also relates to the use of these compounds for inducing apoptotic cell death and sensitizing cells to the induction of apoptotic cell death.
    Type: Grant
    Filed: August 22, 2005
    Date of Patent: October 15, 2013
    Assignee: The Regents of the University of Michigan
    Inventors: Shaomeng Wang, Guoping Wang, Guozhi Tang, Renxiao Wang, Zaneta Nikolovska-Coleska, Dajun Yang, Liang Xu
  • Patent number: 8476306
    Abstract: The invention relates to novel inhibitors of urokinase and to their preparation and use for the therapy, prophylaxis and diagnosis of a tumor, in particular for reducing the formation of tumor metastases.
    Type: Grant
    Filed: November 22, 2010
    Date of Patent: July 2, 2013
    Assignee: The Medicines Company (Leipzig) GmbH
    Inventors: Joerg Stuerzebecher, Torsten Steinmetzer, Andrea Schweinitz
  • Publication number: 20130121919
    Abstract: The invention provides for a method for screening compounds that bind to and modulate a histone acetyltransferase protein. The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a HAT-activating compound to a subject.
    Type: Application
    Filed: June 11, 2012
    Publication date: May 16, 2013
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: Yan FENG, Mauro Fa, Ottavio Arancio, Shi Xian Deng, Donald W. Landry, Yitshak Francis
  • Publication number: 20130096345
    Abstract: Polymorphs and solvates of racemic, enantiomerically pure, and enantiomerically mixed modafinil are formed and discussed. In addition, said forms are described as useful for the treatment of many conditions including, but not limited to, narcolepsy.
    Type: Application
    Filed: December 6, 2012
    Publication date: April 18, 2013
    Applicant: CEPHALON, INC.
    Inventor: CEPHALON, INC.
  • Patent number: 8420823
    Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].
    Type: Grant
    Filed: April 17, 2009
    Date of Patent: April 16, 2013
    Assignee: MSD K.K.
    Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
  • Publication number: 20130066111
    Abstract: The invention relates to a method for preparing a sulphoxide compound of formula (I) either as a single enantiomer or in an enantiomerically enriched form, comprising the steps of: a) contacting a pro-chiral sulphide of formula (II) with a metal chiral complex, a base and an oxidizing agent in an organic solvent; and optionally b) isolating the obtained sulphoxide of formula (I). wherein n, Y, R1, R1a, R2 and R2a are as defined in claim 1.
    Type: Application
    Filed: November 1, 2012
    Publication date: March 14, 2013
    Applicant: CEPHALON FRANCE
    Inventors: Cephalon France, Veronique Courvoisier
  • Publication number: 20130030029
    Abstract: Provided herein are compounds, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof which have glucagon receptor antagonist or inverse agonist activity. Further, provided herein are pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. Moreover, provided herein are methods of making or manufacturing compounds disclosed herein, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or Co-crystals and prodrugs thereof.
    Type: Application
    Filed: August 13, 2009
    Publication date: January 31, 2013
    Applicant: METABASIS THERAPEUTICS, INC.
    Inventors: Jorge E. Gomez-Galeno, Scott J. Hecker, Qun Dang, Mali Venkat Reddy, Zhili Sun, Matthew P. Grote, Thanh Huu Nguyen, Robert Huerta Lemus, Haiqing Li
  • Patent number: 8344181
    Abstract: the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents O, S, NR6, SO or SO2; R1 represents hydrogen, cyano, hydroxy, or C1-4alkyl optionally substituted with halo, R2 represents hydrogen, C1-4alkyl, or C1-4alkyloxy-; R3 represents hydrogen, C1-4alkyl, C1-4alkyloxy- or R3 combined with R2 form together a divalent radical selected from the group consisting of —O—CH2— (a), —NR7—CH2— (b), —(CR8R9)m- (c) and —CR10? (d) wherein m represents 1 or 2 and R7, R8, R9 and R10 are each independently selected from hydrogen or C1-4alkyl; R4 represents hydrogen, halo, hydroxy, cyano, amino, NR11R12, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy and halo or R4 represents C1-4alkyl optionally substituted with one or where possible two or three substituents selected from hydroxy and halo; R5 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C1-4alkyloxycarbonyl, hydrox
    Type: Grant
    Filed: August 26, 2005
    Date of Patent: January 1, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Libuse Jaroskova, Joannes Theodorus Maria Linders, Louis Jozef Elisabeth Van Der Veken, Gustaaf Henri Maria Willemsens, François Paul Bischoff
  • Patent number: 8338646
    Abstract: Polymorphs and solvates of racemic, enantiomerically pure, and enantiomerically mixed modafinil are formed and discussed. In addition, said forms are described as useful for the treatment of many conditions including, but not limited to, narcolepsy.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: December 25, 2012
    Assignee: Cephalon, Inc
    Inventors: Magali Bourghol Hickey, Matthew Peterson, Orn Almarsson, Mark Oliveira
  • Publication number: 20120323040
    Abstract: Methods for producing a compound of formula k1 or k2 by reducing a dihydronapthalene amide compound of formula i with hydrogen gas in the presence of a ruthenium catalyst of formula j1 or j2 Ru(Z)2(L)??j1; Ru(E)(E?)(L)(D)??j2; wherein m, n, Ar, Y, R1E, E?, D, Z and L are as defined herein.
    Type: Application
    Filed: January 26, 2012
    Publication date: December 20, 2012
    Inventors: Kieran Durkin, Lawrence Emerson Fisher, Arthur MEILI, Michaelangelo Scalone, Xianqing Shi, Justin Vitale
  • Publication number: 20120316173
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: January 11, 2011
    Publication date: December 13, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Alessandra Bartolozzi, Angela Berry, Doris Riether, Monika Ermann, James Edward Jenkins, Innocent Mushi
  • Patent number: 8318979
    Abstract: The invention relates to a method for preparing a sulphoxide compound of formula (I) either as a single enantiomer or in an enantiomerically enriched form, comprising the steps of: a) contacting a pro-chiral sulphide of formula (II) with a metal chiral complex, a base and an oxidizing agent in an organic solvent; and optionally b) isolating the obtained sulphoxide of formula (I). wherein n, Y, R1, R1a, R2 and R2a are as defined in claim 1.
    Type: Grant
    Filed: March 24, 2011
    Date of Patent: November 27, 2012
    Assignee: Cephalon France
    Inventors: Laurent Courvoisier, Veronique Courvoisier, legal representative, Gerard Duret, Stephanie Graf, Laurence Prat-Lacondemine, Francois Rebiere, Nicolas Sabourault
  • Patent number: 8314270
    Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.
    Type: Grant
    Filed: September 9, 2010
    Date of Patent: November 20, 2012
    Assignee: Abbott Laboratories
    Inventors: James T. Link, Qi Shuai, Martin Winn, Hong Yong
  • Patent number: 8278484
    Abstract: Disclosed is a process for preparing anti-inflammatory compound nepafenac comprising preparing a compound of formula (V) wherein a N-halosuccinimide is used as the halogenating agent, followed by desulfurization using Raney Nickel. Also disclosed is a polymorphic form B of 2-amino-3-benzoyl-?-(methylthio)-benzeneacetamide (i.e.
    Type: Grant
    Filed: June 12, 2009
    Date of Patent: October 2, 2012
    Assignee: Medichem, S.A.
    Inventors: Gabriel Tojo Suárez, Ana Gavaldá Escudé
  • Publication number: 20120245341
    Abstract: The present invention provides an oligonucleotide derivative that enables to easily synthesize an oligonucleotide derivative chemically modified at the 3?-end with two moieties each having a benzene or pyridine structure with a few steps, an aromatic compound serving as a precursor for preparing the modification carrier for synthesizing oligonucleotide derivative, and the oligonucleotide derivative and the oligonucleotide construct using the same, that is chemically modified at the 3?-end with two moieties each having a benzene or pyridine structure, and has good permeability through a cell membrane and excellent nuclease resistance. The modification carrier for synthesizing oligonucleotide derivative, comprising a unit and a carrier carrying the unit directly or via a linker, wherein the unit is represented by the formula (a): wherein, R1 to R6 each independently represent hydrogen or a substituent other than hydrogen; Z1 and Z2 each independently represent CH or nitrogen; and X represents oxygen or sulfur.
    Type: Application
    Filed: December 8, 2009
    Publication date: September 27, 2012
    Inventors: Yukio Kitade, Yoshiaki Kitamura
  • Publication number: 20120204763
    Abstract: An object of the present invention is to provide a recording material that is excellent in color-developing properties and background and image stabilities, and a compound used therein. The present invention relates to a compound represented by the formula (I) [wherein R11 to R14 each independently represent a halogen atom or the like; n, p, q, and r each independently represent 0 or any integer of 1 to 4; m represents 0 or any integer of 1 to 2; a represents any integer of 1 to 10; R2 represents a hydrogen atom or the like; R3 represents an OR51 group or the like; and R41 and R42 each independently represent a hydrogen atom or the like], a composition containing the compound, a method for producing the compound, a recording material containing at least one compound represented by the formula (I), and a recording sheet having the recording material.
    Type: Application
    Filed: September 28, 2010
    Publication date: August 16, 2012
    Inventors: Toshio Aihara, Hiroshi Sakai, Shuntaro Kinoshita, Satoshi Kodama, Tadahiro Kondo, Kazumi Jyujyo
  • Publication number: 20120189614
    Abstract: Organic compounds showing the ability to inhibit viral glycoprotein (GP)-mediated entry of a filovirus into a host cell are disclosed. The disclosed filovirus entry inhibitor compounds are useful for treating, preventing, or reducing the spread of infections by filovirus including the type species Marburg virus (MARV) and Ebola virus (EBOV). Preferred inhibitors of the invention provide therapeutic agents for combating the Ivory Coast, Sudan, Zaire, Bundibugyo, and Reston Ebola virus strains.
    Type: Application
    Filed: July 10, 2010
    Publication date: July 26, 2012
    Applicant: Crobiotix, Inc.
    Inventors: Arnab Basu, Debra M. Mills, Norton P. Peet, John D. Williams
  • Patent number: 8216974
    Abstract: There is provided a fluorine-containing organosulfur compound having an excellent controlling effect on arthropod pests represented by the formula (I): wherein G represents an oxygen atom or a sulfur atom; R2 represents a C1-C4 chain hydrocarbon group which is optionally substituted with a halogen atom, etc.; R3 and R4 independently represent a C1-C4 chain hydrocarbon group or a hydrogen atom; R5 represents a C1-C5 haloalkyl group containing at least one fluorine atom, or a fluorine atom; R6 represents a halogen atom, a cyano group, a nitro group or a -(G1)q-R8 group; R7 represents an amino group etc.; R8 represents a C1-C4 chain hydrocarbon group which is optionally substituted with a halogen atom; m represents an integer of 0 to 5; n represents an integer of 0 to 2; p represents 0 or 1; q represents 0 or 1; and G1 represents an oxygen atom etc.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: July 10, 2012
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Koji Kumamoto, Hiroyuki Miyazaki
  • Publication number: 20120142771
    Abstract: The present invention provides a compound of formula (I) or a salt thereof, wherein R1, R2 and R3 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, bromine atom, C1-6 alkyl, C1-6 alkoxy substituted with fluorine atom, and others; R4 and R5 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, C1-6 alkyl, C1-6 alkoxy substituted with fluorine atom, and others; R6 and R7 are independently selected from the group consisting of hydrogen atom, fluorine atom, methyl, ethyl, hydroxy group, and others; and R8 and R9 are independently selected from the group consisting of hydrogen atom, C1-6 alkyl, and others, which is useful as an agent for treating or preventing various types of epilepsy including partial seizures and/or generalized seizures.
    Type: Application
    Filed: February 7, 2012
    Publication date: June 7, 2012
    Applicant: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Seiji IWAMA, Tomoyuki Tanaka, Nana Yajima
  • Patent number: 8183294
    Abstract: The invention relates to a method for preparing a sulphoxide compound of formula (I) either as a single enantiomer or in an enantiomerically enriched form, comprising the steps of: a) contacting a pro-chiral sulphide of formula (II) with a metal chiral complex, a base and an oxidizing agent in an organic solvent; and optionally b) isolating the obtained sulphoxide of formula (I). wherein Ar, Y, R1 are as defined in claim 1.
    Type: Grant
    Filed: January 4, 2011
    Date of Patent: May 22, 2012
    Assignee: Cephelon France
    Inventors: Philippe Louvet, Dominique Schweizer
  • Publication number: 20120123161
    Abstract: The invention relates to a method for preparing a sulphoxide compound of formula (I) either as a single enantiomer or in an enantiomerically enriched form, comprising the steps of: a) contacting a pro-chiral sulphide of formula (II) with a metal chiral complex, a base and an oxidizing agent in an organic solvent; and optionally b) isolating the obtained sulphoxide of formula (I). wherein n, Y, R1, R1a, R2 and R2a are as defined in claim 1.
    Type: Application
    Filed: March 24, 2011
    Publication date: May 17, 2012
    Applicant: CEPHALON FRANCE
    Inventors: Laurent Courvoisier, Veronique Courvoisier, Gerard Duret, Stephanie Graf, Laurence Prat-Lacondemine, Francois Rebiere, Nicolas Sabourault
  • Publication number: 20120108515
    Abstract: Novel compounds which may be for treatment, prevention or alleviation of a condition associated with bone loss or low bone density or to inhibit osteoclast differentiation and stimulation, bone resorption, or loosening of a prosthetic device.
    Type: Application
    Filed: June 17, 2010
    Publication date: May 3, 2012
    Applicant: NEOBIOTICS AB
    Inventors: Anders Grubb, Franciszek Kasprzykowski, Ulf Lerner, Beata Zolnowska, Regina Kasprzykowska
  • Publication number: 20120101053
    Abstract: The present invention relates to compounds capable of inhibiting and/or decreasing the activity of one or more cathepsins, thereby treating and/or preventing various disease states associated with one or more cysteine proteases including, but not limited to, cathepsins and papain-like cysteine proteases. Disease states treated and/or prevented by the compounds of the invention include, but are not limited to, mammalian parasitic diseases in which the parasite utilizes a critical cysteine protease from the papain family. Examples of parasitic diseases to be treated or prevented by the compounds of the invention include, but are not limited to, toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, coccidiosis, giardiosis, cryptosporidiosis or schistosomiasis.
    Type: Application
    Filed: June 16, 2010
    Publication date: April 26, 2012
    Inventors: Cameron Black, Christian Beaulieu
  • Patent number: 8143447
    Abstract: The present invention provides compositions of matter, kits and methods for their use in the treatment of cancer. In particular, the invention provides compositions and methods for treating cancer in a subject by inhibiting a poly-ADP-ribose polymerase, as well as providing formulations and modes of administering such compositions.
    Type: Grant
    Filed: September 5, 2007
    Date of Patent: March 27, 2012
    Assignee: BiPar Sciences, Inc.
    Inventors: Jerome Moore, Bruce Keyt, John Burnier, Barry M. Sherman, Max Totrov, Valeria S. Ossovskaya