Nitrogen In Substituent Q Patents (Class 564/163)
  • Patent number: 10155772
    Abstract: The present invention relates to compounds of formula I and a process for the synthesis: The invention further relates to a process for the synthesis of 3-carboxamide substituted morphinans where a 3-cyano substituted 6-oxo substituted morphinan is reacted with a 1,3-diol.
    Type: Grant
    Filed: May 24, 2018
    Date of Patent: December 18, 2018
    Assignee: Alkermes Pharma Ireland Limited
    Inventor: Scott Duncan
  • Patent number: 9199923
    Abstract: In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.
    Type: Grant
    Filed: March 6, 2014
    Date of Patent: December 1, 2015
    Assignees: President and Fellows of Harvard College, Dana-Farber Cancer Institute, Inc.
    Inventors: James Elliot Bradner, Ralph Mazitschek
  • Publication number: 20140350263
    Abstract: Reagents comprising MS active, fluorescent molecules with an activated functionality for reaction with amines useful in tagging biomolecules such as N-glycans and uses thereof are taught and described.
    Type: Application
    Filed: August 13, 2014
    Publication date: November 27, 2014
    Applicant: WATERS TECHNOLOGIES CORPORATION
    Inventors: Darryl W. Brousmiche, Ying-Qing Yu, Matthew Lauber
  • Publication number: 20140343322
    Abstract: The invention relates to one-pot process for preparing (1S,2R)-1-phenyl-1-(N,N-diethylaminocarbonyl)-2-aminomethylcyclopropane of formula (I) comprising the step of reacting (1S,2R)-N,N-diethyl-2-(hydroxymethyl)-1-phenylcyclopropanecarboxamide successively with the following reactants 1) triethyl orthoformate and methanesulfonic acid or triethylamine and methanesulfonyl chloride, 2) a phthalimidating agent, 3) aqueous EtNH2, wherein the reaction is carried out in toluene. In another aspect the invention concerns a process for preparing (1S,2R)-N,N-diethyl-2-(hydroxymethyl)-1-phenylcyclopropanecarboxamide trough a step of crystallization of (1S,5R)-1-phenyl-3-oxabicyclo[3.1.0]hexan-2-one.
    Type: Application
    Filed: May 20, 2014
    Publication date: November 20, 2014
    Applicant: COSMA S.P.A.
    Inventors: Paolo CELESTINI, Sergio BARETTI, Enrica PIZZATTI
  • Publication number: 20140323487
    Abstract: Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.
    Type: Application
    Filed: July 8, 2014
    Publication date: October 30, 2014
    Inventors: David John Cowan, Andrew Lamont Larkin, Cunyu Zhang, David Lee Musso, Gary Martin Green, Rodolfo Cadilla, Paul Kenneth Spearing, Michael Joseph Bishop, Jason Daniel Speake
  • Patent number: 8853393
    Abstract: The invention discloses a novel intermediate for preparing tapentadol and analogues thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogues thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: October 7, 2014
    Assignee: Anhui New Star Pharmaceutical Development Co., Ltd.
    Inventors: Ziao Xu, Yuanhai Zhao, Degang Li, Xiaoxiang Li
  • Patent number: 8815485
    Abstract: A compound that can improve azo pigment dispersibility in a non-water-soluble solvent. The compound is represented by formula (1): wherein R1 to R4 represent hydrogen or halogen; R5 to R9 represent hydrogen, COOR17 or CONR18R19, and at least one of R5 to R9 represents COOR17 or CONR18R19, where R17 to R19 represent hydrogen or an alkyl group having 1 to 3 carbons; R10 represents an alkyl group having 1 to 6 carbons or a phenyl group; R11 to R15 represent a hydrogen, L1R20 or L2R21R22, and at least one of R11 to R15 represents L1R20 or L2R21R22, where L1 represents a divalent linking group, L2 represents a trivalent linking group, and R20 to R22 represent an alkyl group having 8 or more carbons or an alkenyl group having 8 or more carbons; and R16 represents an alkyl group having 1 to 6 carbons or a phenyl group.
    Type: Grant
    Filed: August 11, 2011
    Date of Patent: August 26, 2014
    Assignee: Canon Kabushiki Kaisha
    Inventors: Masatake Tanaka, Masashi Kawamura, Yuki Hasegawa, Takayuki Toyoda, Yasuaki Murai, Masashi Hirose, Takeshi Miyazaki
  • Patent number: 8791135
    Abstract: Novel compounds and compositions for treating patients in need of relief from HIV, AIDS, and AIDS-related diseases are described. Methods for treating HIV, AIDS, and AIDS-related diseases using the compounds described herein are also described.
    Type: Grant
    Filed: July 1, 2009
    Date of Patent: July 29, 2014
    Assignee: Purdue Research Foundation
    Inventor: Arun K. Ghosh
  • Patent number: 8785637
    Abstract: The present invention relates to carboxamide-substituted dyes, the production and use of such dyes as labeling groups in analytics.
    Type: Grant
    Filed: August 8, 2013
    Date of Patent: July 22, 2014
    Assignee: Atto-Tec GmbH
    Inventors: Jutta Arden-Jacob, Karl-Heinz Drexhage, Monika Hamers-Schneider, Norbert Kemnitzer, Alexander Zilles
  • Patent number: 8785627
    Abstract: This invention relates to polymerizable ultraviolet light absorbers and yellow colorants and their use in ophthalmic lenses. In particular, this invention relates to polymerizable ultraviolet light absorbing methane compounds and yellow compounds of the methine and anthraquinone classes that block ultraviolet light and/or violet-blue light transmission through ophthalmic lenses.
    Type: Grant
    Filed: August 5, 2013
    Date of Patent: July 22, 2014
    Assignee: Abbott Medical Optics Inc.
    Inventors: Jason Clay Pearson, Max Allen Weaver, Jean Carroll Fleischer, Gregory Allan King
  • Patent number: 8778838
    Abstract: The present invention relates to aqueous concentrate formulations for plant protection comprising: 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]sulfonyl]benzamide in the form of its anhydrate; N-(phosphonomethyl)glycine in the form of its free acid, in the form of the ammonium salt or a substituted ammonium salt or a mixture thereof; at least two different non-ionic surfactants with at least one of them comprising an ethylene oxide polymer moiety or an ethylene oxide/C3-C4-alkylene oxide block copolymer moiety, and water; wherein the pH-value of the formulation is below 6.
    Type: Grant
    Filed: August 26, 2010
    Date of Patent: July 15, 2014
    Assignee: BASF SE
    Inventors: Michael Krapp, Wolfgang Gregori, Sven Adam, Klaus Kolb, Juergen Jakob, Bernd Sievernich, Joerg Steuerwald, Steven Bowe, Joseph Zawierucha, Rex Liebl
  • Publication number: 20140135496
    Abstract: An isoxazoline-substituted benzamide compound of formula (1) or a salt thereof: wherein A1, A2 and A3 independently of one another are carbon atom or nitrogen atom, G is benzene ring, etc., W is oxygen atom or sulfur atom, etc., X is halogen atom, C1-C6haloalkyl, etc., Y ia halogen atm, C1-C6alkyl, etc., R1 is —CH?NOR1a, —C(O)OR1c, —C(O)NHR1d, phenyl substituted with (Z)p1, D-14, D-52, D-53, D-55 to D-59, etc., R1a is C1-C6alkyl, etc., R1c is C1-C6alkyl, etc., R1d is hydrogen atom, —C(O)R15, —C(O)OR15, etc., R2 is C1-C6alkyl, —CH2R14a, C1-C6alkynyl, —C(O)R15, —C(O)OR15, etc., further when R1 is —CH?NOR1a, —C(O)OR1c or —C(O)N(R1e)R1d, R2 may be hydrogen atom, R3 is C1-C6haloalkyl, etc., R14a is cyano, —OR25, etc., R15 is C1-C6alkyl, C1-C6haloalkyl, C1-C4alkoxy C1-C4alkyl, C1-C4alkylthio C1-C4alkyl, C3-C6cycloalkyl, C2-C6alkenyl, etc., R25 is C1-C4alkyl, C1-C4haloalkyl, —C(O)R32 or —C(O)OR32, etc., R32 is C1-C6alkyl or C3-C6cycloalkyl, etc., Z is halogen atom, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, etc.
    Type: Application
    Filed: January 16, 2014
    Publication date: May 15, 2014
    Applicant: Nissan Chemical Industries, Ltd.
    Inventors: Takeshi MITA, Yuki FURUKAWA, Ken-ichi TOYAMA, Manabu YAOSAKA, Eitatsu IKEDA, Yoshihide MASUZAWA, Mitsuaki KOMODA
  • Publication number: 20140088153
    Abstract: The invention relates to compounds of the general formula (I) in which the radicals A1, A2, A3, A4, L, Q, R1, T and W have the meaning given in the description and to the use of the compounds for controlling animal pests. The invention furthermore relates to processes and intermediates for preparing the compounds of formula (I).
    Type: Application
    Filed: March 12, 2012
    Publication date: March 27, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Michael Maue, Isabelle Adelt, Markus Heil, Peter Jeschke, Tobias Kapferer, Friedrich August Muehlthau, Alexander Sudau, Olga Malsam, Peter Loesel, Arnd Voerste, Ulrich Goergens
  • Patent number: 8653129
    Abstract: The present invention provides a novel therapeutic combination comprising one or more anti-androgen agents and one or more antibiotic/anti-inflammatory agents or pharmaceutically acceptable salts or hydrates thereof, useful for the treatment of a dermatological disorder.
    Type: Grant
    Filed: April 11, 2011
    Date of Patent: February 18, 2014
    Assignee: M. Alphabet 1, LLC
    Inventors: Howard Fein, Mindy B. Berlin
  • Patent number: 8653002
    Abstract: The present invention relates to aqueous suspension concentrate formulation for plant protection comprising: 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]sulfonyl]benzamide in the form of its crystalline anhydrate; at least one non-ionic surfactant selected from polyoxyethylene-polyoxy-C3-C4-alkylene block copolymers; at least one anionic surfactant comprising at least one arylsulfonate group; and water; wherein the pH value of the formulation is in the range of 3 to 7.
    Type: Grant
    Filed: August 26, 2010
    Date of Patent: February 18, 2014
    Assignee: BASF SE
    Inventors: Michael Krapp, Wolfgang Gregori, Klaus Kolb, Bernd Sievernich, Heidi Emilia Saxell, Joerg Steuerwald, Steven Bowe, Rex Liebl, Terrance M. Cannan
  • 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: 20140018422
    Abstract: Disclosed herein are derivatives of tetracaine that, among other things, block cyclic nucleotide gated (CNG) channels and are useful in the treatment of diseases characterized by overactive CNG channels such as retinal degeneration diseases.
    Type: Application
    Filed: December 14, 2012
    Publication date: January 16, 2014
    Inventors: Jeffrey Karpen, Sarah Kirk, Adriana Andrade, Michelle Schaffer, Kenneth Melich
  • Publication number: 20130310567
    Abstract: A method for preparing a compound of Formula 1 comprising contacting a compound of Formulae 2 and 3 in the presence of a palladium source, a ligand, a base and carbon monoxide wherein R1, R2, X and R3 are as defined in the disclosure. A method for preparing a compound of Formula 5 wherein R1, R2, R3, R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 characterized by preparing a compound of Formula 1 by the method disclosed above or using a compound of Formula 1 prepared by the method above.
    Type: Application
    Filed: January 27, 2012
    Publication date: November 21, 2013
    Applicant: EI DU PONT DE NEMOURS AND COMPANY
    Inventors: Sigridur Soley Kristjansdottir, Rafael Shapiro, Matthew Richard Oberholzer
  • Publication number: 20130289076
    Abstract: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I) as described and defined herein, and their use in therapy, including, e.g., the treatment or prevention of cancer.
    Type: Application
    Filed: October 7, 2011
    Publication date: October 31, 2013
    Inventors: Julio Castro-Palomino Laria, Matthew Colin Thor Fyfe, Marc Murtinell Pedemonte, Alberto Ortega Muñoz, Núrla Valls Vidal
  • Publication number: 20130253142
    Abstract: A novel separating agent for protein purification which not only can adsorb proteins in a sufficient amount for protein purification from a low concentration buffer but also can desorb the adsorbed protein easily just by altering the pH of the buffer and a simple and economical method for its production and a method for protein purification using it. One or two ligands selected from the group consisting of a ligand represented by the following formula (1): (wherein m is an integer of from 2 to 6) and a ligand represented by the following formula (2): (wherein each of R1 and R2 is independently a hydrogen atom or a C1-4 alkyl group, and n is an integer of from 1 to 6) are immobilized on a support via a urethane bond without intervention of a spacer arm.
    Type: Application
    Filed: May 17, 2013
    Publication date: September 26, 2013
    Applicant: TOSOH CORPORATION
    Inventors: Seiji MASUMOTO, Katsuo KOMIYA, Koji NAKAMURA
  • Publication number: 20130231478
    Abstract: The invention discloses a novel intermediate for preparing tapentadol and analogues thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogues thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production.
    Type: Application
    Filed: July 29, 2011
    Publication date: September 5, 2013
    Inventors: Ziao Xu, Yuanhai Zhao, Degang Li, Xiaoxiang Li
  • Publication number: 20130210899
    Abstract: A methodology and pharmaceutical and gene therapies for the treatment and regulation of memory function are provided. The invention identifies specific HDAC, and in particular, HDAC3 and HDAC4 as negative regulators of memory formation and specifically targets one or both HDAC3 and HDAC4 for down-regulation. By specifically targeting HDAC3 and HDAC4 with small molecule inhibitors and gene therapies it is possible to provide a powerful therapeutic approach to facilitate gene expression during memory formation that can lead to the regulation and treatment of memory disorders.
    Type: Application
    Filed: July 28, 2011
    Publication date: August 15, 2013
    Applicant: The Regents of the University of California
    Inventor: Marcelo Andres Wood
  • Publication number: 20130178457
    Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I).
    Type: Application
    Filed: July 5, 2012
    Publication date: July 11, 2013
    Applicant: LUPIN LIMITED
    Inventors: Sanjeev Anant KULKARNI, Sachin MADAN, Nirmal Kumar JANA, Prashant Vitthalrao TALE, Narasimha Murthy CHEEMALA, Sachin Jaysing MAHANGARE, Prashant Popatrao VIDHATE, Chaitanya Prabhakar KULKARNI, Sapana Suresh PATEL, Amolsing Dattu PATIL, Seema Prabhakar ZADE, Rohan Mahadev SHINDE, Venkata P. PALLE, Rajender Kumar KAMBOJ
  • Patent number: 8466318
    Abstract: The present invention encompasses a process for preparing compounds of formula (1), wherein a compound of formula (2) is reacted in the presence of a catalyst and a solvent under hydrogen pressure to form a compound of formula (1) and wherein A and R1—R4 are defined herein.
    Type: Grant
    Filed: May 15, 2007
    Date of Patent: June 18, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Guenter Linz, Gerd Kraemer, Zeno A. Leuter, Markus Ostermeier, Werner Rall, Claudia Ochs, Rolf Schmid
  • Patent number: 8455550
    Abstract: The present invention concerns compounds of general formula (1), where in:—-a- is a single or double bond, Ar is an aromatic group, substituted or unsubstituted, R1 and R2 each independently or together are: a hydrogen atom or C1-C6 alkyl group, branched or unbranched, saturated or unsaturated, substituted or unsubstituted; the groups R1 and R2 may also form a heterocycle, R3 and R3? each independently or together are a hydrogen atom or C1-C6 alkyl group, X is an oxygen atom or a sulphur atom, and the addition salts of the compounds of general formula (1) with pharmaceutically acceptable mineral acids or organic acids.
    Type: Grant
    Filed: April 2, 2010
    Date of Patent: June 4, 2013
    Assignee: Pierre Fabre Medicament
    Inventors: Stéphane Cuisiat, Adrian Newman-Tancredi, Olivier Vitton, Bernard Vacher
  • Patent number: 8431514
    Abstract: The present invention relates to bis-amide derivatives of formula (I), to processes and intermediates for preparing them, to methods of using them to control insect, acarine, nematode and mollusc pests, and to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them.
    Type: Grant
    Filed: April 14, 2010
    Date of Patent: April 30, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Pierre Joseph Marcel Jung, Christopher Richard Ayles Godfrey, Ottmar Franz Hueter, Peter Maienfisch
  • Publication number: 20130079514
    Abstract: (R)-2-Arylpropionamide compounds of formula (I), pharmaceutical preparations of the compounds and a process for making the compounds are described. The 2-Arylpropionamides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonuclear leukocytes and monocytes at inflammatory sites. In particular, the invention relates to the R enantiomers of omega-aminoalkylamides of 2-aryl propionic acids, of formula (I), for use as inhibitors of chemotaxis of neutrophils and monocytes induced by the C5a fraction of complement and by other chemotactic proteins whose biological activity is associated with activation of a 7-TD receptor. Selected compounds of formula (I) are dual inhibitors of both the C5a-induced chemotaxis of neutrophils and monocytes and the IL-8-induced chemotaxis of polymorphonuclear leukocytes.
    Type: Application
    Filed: October 15, 2012
    Publication date: March 28, 2013
    Applicant: Dompé S.p.A.
    Inventor: Dompé S.p.A.
  • Publication number: 20130071773
    Abstract: Disclosed herein are novel amidic nitrone and a method of manufacturing a data storage media comprising mixing the amidic nitrone, as a photochromic dye, with an organic material or an inorganic material to form a holographic composition and molding the holographic composition into holographic data storage media. Disclosed herein too is an article comprising a photochromic dye and an organic material, wherein the article is used as a data storage media. Disclosed herein too is a method for recording information comprising irradiating an article that comprises a photochromic dye, wherein the irradiation is conducted with electromagnetic energy having a wavelength of about 350 to about 1,100 nanometers; and reacting the photochromic dye.
    Type: Application
    Filed: September 16, 2011
    Publication date: March 21, 2013
    Applicant: SABIC INNOVATIVE PLASTICS IP B.V.
    Inventors: Gary Davis, Shantaram Narayan Naik, Kiran Arunkumar Puthamane, George Kuriakose, Sumeet Jain, Vinodkumar Vasudevan, Prashant Patil
  • Publication number: 20130035328
    Abstract: The invention relates to compounds having antiviral activity and methods utilizing the compounds to treat viral infections.
    Type: Application
    Filed: July 19, 2012
    Publication date: February 7, 2013
    Inventors: Peter William Gage, Gary Dinneen Ewart, Lauren Elizabeth Wilson, Wayne Best, Anita Premkumar
  • Publication number: 20130012611
    Abstract: Compounds of formula (I): wherein Ar represents an, optionally substituted, aryl or heteroaryl group, R represents an, optionally substituted, aryl or heteroaryl group, an optionally substituted straight or branched chain C1.10-alkyl, R1 is H or methyl, X is an extender group, n is 0 or an integer between 1 and 12 inclusive, A is a polyol residue wherein the unsubstituted polyol from which the residue is derived has at least y OH groups, and y is an integer>1, can easily be prepared, and are useful as synergists in radiation curing.
    Type: Application
    Filed: March 25, 2011
    Publication date: January 10, 2013
    Inventors: Robert Stephen Davidson, Shaun Lawrence Herlihy
  • Publication number: 20120283101
    Abstract: The present invention pertains to plant additives containing a molecule selected in a family of compounds, wherein said molecule can modulate some molecular markers and physiological modifications observed in cases of phosphate deficiency. The family of compounds comprises the molecule MC2 of formula (I) as well as analogues thereof.
    Type: Application
    Filed: September 17, 2010
    Publication date: November 8, 2012
    Inventors: Mathilde Clement, Thierry Desnos, Laurent Nussaume
  • Publication number: 20120264823
    Abstract: The invention relates to compounds of Formula (I): (A?)x-(A)-(B)—(Z)-(L)-C(?O)NH2 or pharmaceutically acceptable salts or solvates thereof, wherein: (A) is heteroaryl or aryl; each (A?), if present, is indepedently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A?) is substituted with 0, 1, 2 or 3 substituents independently chosen from halo, haloalkyl, aryl, arylalkoxy, alkyl, alkoxy, cyano, sulfonyl, sulfinyl, and carboxamide; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; and (L) is —(CH2)mCR1,R2—, wherein m is 0, 1, 2, 3, 4, 5, or 6, and wherein R1 and R2 are each independently hydrogen or C1-C6 alkyl; provided that, if (L) is —CH2— or —CH(CH3)—, then X is not 0. The compounds of the invention are useful in the treatment of diseases such as cancer and neurodegenerative diseases.
    Type: Application
    Filed: April 19, 2010
    Publication date: October 18, 2012
    Inventors: Alberto Ortega Muñoz, Julio Castro-Palomino Laria, Matthew Colin Thor Fyfe
  • 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
  • Patent number: 8263807
    Abstract: Compounds of formulas: are disclosed. The compounds are useful for ameliorating the side effects of therapeutic opiates.
    Type: Grant
    Filed: August 8, 2008
    Date of Patent: September 11, 2012
    Assignee: Rensselaer Polytechnic Institute
    Inventor: Mark P. Wentland
  • Patent number: 8232411
    Abstract: The invention discloses compounds of formula II: and methods of making the compounds, which are VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.
    Type: Grant
    Filed: March 20, 2009
    Date of Patent: July 31, 2012
    Assignee: Abbott Laboratories
    Inventors: Kirill A. Lukin, Brian J. Kotecki, Su Yu, Lei Wang, Anthony R. Haight
  • Patent number: 8222453
    Abstract: The present invention provides novel benzamide derivatives of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables A, W, Y, Z, R8, and R9 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
    Type: Grant
    Filed: June 7, 2007
    Date of Patent: July 17, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Eldon Scott Priestley, Xiaojun Zhang
  • Publication number: 20120142671
    Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.
    Type: Application
    Filed: November 1, 2011
    Publication date: June 7, 2012
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey
  • Patent number: 8188306
    Abstract: Novel compounds useful for inhibiting the 90kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.
    Type: Grant
    Filed: September 30, 2009
    Date of Patent: May 29, 2012
    Assignee: University of Kansas
    Inventors: Brian S. J. Blagg, Gang Shen
  • Patent number: 8188307
    Abstract: Disclosed is an industrially advantageous production method of optically active ?-amino acid of formula (5a), which includes subjecting an enaminoester of formula (4a) to an asymmetric hydrogenation: wherein * shows an asymmetric carbon atom.
    Type: Grant
    Filed: August 31, 2009
    Date of Patent: May 29, 2012
    Assignee: Takasago International Corporation
    Inventors: Takashi Moroi, Tsukasa Sotoguchi, Kazuhiko Matsumura, Motonobu Takenaka, Wataru Kuriyama, Toshiyuki Murayama, Hideki Nara, Tohru Yokozawa, Kenji Yagi
  • Patent number: 8153844
    Abstract: Disclosed is a method for preparing a compound of Formula 1 by contacting compound of Formula 2 with R1—NH2 in the presence of a carboxylic acid and a method for preparing a compound of Formula 2 by contacting a compound of Formula 4 with phosphorus tribromide. wherein R1 is H, C1-C4 alkyl, cyclopropyl, cyclopropylmethyl or methylcyclopropyl; R2 is CH3 or Cl; R3 is C1-C6 alkyl or C3-C6 alkenyl, each optionally substituted with up to 3 halogen and up to 1 phenyl; and X is Cl or Br. Also disclosed is a method for preparing a compound of Formula 5 wherein R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 that is characterized by preparing the compound of Formula 1 by the method above.
    Type: Grant
    Filed: June 27, 2007
    Date of Patent: April 10, 2012
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Richard F. Davis, Rafael Shapiro, Eric G. Taylor
  • Patent number: 8110703
    Abstract: The invention relates to a retinoid derivative and pharmaceutical composition and use thereof. The compound of the invention is capable of preventing or treating hematological tumors, such as acute leukemia, chronic leukemia, multiple myeloma and lymphoma, solid tumors, such as liver cancer, rectal cancer, mammary cancer and esophagus cancer, and skin disorders, such as psoriasis and acne.
    Type: Grant
    Filed: May 31, 2009
    Date of Patent: February 7, 2012
    Assignees: Anhui Medical University, Anhui New Star Pharmaceutical Development Co., Ltd.
    Inventors: Feihu Chen, Jingbo Shi, Yuan Wang, Jun Li, Juan Shen, Jingjing Ruan, Fanrong Wu
  • Publication number: 20110306600
    Abstract: The invention discloses a number of therapeutic compounds and a method of treating a disorder in mammal.
    Type: Application
    Filed: June 10, 2011
    Publication date: December 15, 2011
    Applicant: Grunenthal GmbH
    Inventor: Ramesh SESHA
  • Publication number: 20110301365
    Abstract: This invention relates to novel alpha-substituted ?,?-unsaturated E- or Z-aldehydes, or isomer mixture thereof, of the formula in which R1 and R2 may be identical or different and are each H or a hydrocarbon, in which the hydrocarbon may have one or more heteroatoms and R3 and R4 may be identical or different and are each a hydrocarbon, in which the hydrocarbon may have one or more heteroatoms, and R5 may be identical or different and is H or a hydrocarbon, in which the hydrocarbon may have one or more heteroatoms, to the use thereof, and to processes for their preparation. The invention further relates to the preparation of further intermediates for pharmaceuticals and to the preparation of the pharmaceuticals.
    Type: Application
    Filed: August 8, 2011
    Publication date: December 8, 2011
    Applicant: DSM IP Assets B.V.
    Inventors: Gerhard STEINBAUER, Martina Kotthaus, Klaus Edegger, Stefaan Marie Andre De Wildeman, Henricus Martinus Maria Gerardus Straatman, Anna Maria Cornelia Francisca Castelijns, Andreas Hendrikus Maria De Vries
  • Patent number: 8063247
    Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, are opioid receptor modulators, e.g. mu-opioid receptor antagonists, neutral antagonists or inverse agonists, and are useful inter alia for the treatment of obesity.
    Type: Grant
    Filed: September 8, 2008
    Date of Patent: November 22, 2011
    Assignee: Prosidion Limited
    Inventors: Jason Bloxham, Stuart Edward Bradley, Thomas Martin Krulle, Martin James Procter, Colin Peter Sambrook-Smith, Karen Lesley Schofield, Donald Smyth
  • Publication number: 20110269689
    Abstract: High penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas HPCs of NSAIA, for example, have demonstrated indications such as treating hair loss. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
    Type: Application
    Filed: December 4, 2009
    Publication date: November 3, 2011
    Inventor: Chongxi Yu
  • Publication number: 20110269706
    Abstract: The disclosure includes hydroxamic compounds of Formula I: (I) wherein P, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.
    Type: Application
    Filed: January 7, 2010
    Publication date: November 3, 2011
    Applicant: Northlake Biosciences LLC
    Inventors: Yu Chen, Yi Chen
  • Publication number: 20110263604
    Abstract: The invention relates to phenylcyclopropylamine acetamide derivatives and their use in treating diseases.
    Type: Application
    Filed: April 18, 2011
    Publication date: October 27, 2011
    Applicant: Oryzon Genomics, S.A.
    Inventors: Nathalie Guibourt, Alberto Ortega Munoz, Julio Castro-Palomino Laria
  • Publication number: 20110263457
    Abstract: We describe herein a cell-based multiplexing technique called detectable cell barcoding (DCB). In DCB, each individual sample is labeled with a different DCB signature that distinguishes each sample by one or both of detected intensity or type of detection characteristic. The samples are then combined and analyzed for a detectable characteristic of interest (e.g., presence of an analyte). By employing multiple distinct DCB labels at varying concentrations, one can perform multiplex analyses on up to hundreds or thousands (or more) of cell samples in a single reaction tube. DCB reduces reagent consumption by factors of 100-fold or more, significantly reduces data acquisition times and allows for stringent control sample analysis.
    Type: Application
    Filed: July 1, 2011
    Publication date: October 27, 2011
    Inventors: Peter O. Krutzik, Garry Nolan
  • Publication number: 20110251393
    Abstract: The invention provides a helicene derivative, axially chiral amino acid, amine or amino alcohol derivative, and azaperylene, such as compounds represented by Formulae (I), (I?), (II), (II?), and (III): and a method for producing the same.
    Type: Application
    Filed: October 20, 2009
    Publication date: October 13, 2011
    Applicant: KYOTO UNIVERSITY
    Inventors: Takumi Furuta, Takeo Kawabata
  • Publication number: 20110245250
    Abstract: Compounds of formula (I) and pharmacologically acceptable salts and pro-drugs thereof wherein: Ar1 and Ar2 are aryl or heteroaryl; a is 0 to 5; R1 is alkyl, halogen, haloalkyl, alkoxy, haloalkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monoalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino or cyano and, where a is greater than 1, each substituent R1 may be the same or different; b is 0 to 5; R2 is alkyl, halogen, haloalkyl, haloalkoxy, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monoalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino or cyano and where b is greater than 1, each substituent R2 may be the same or different; V is selected from the group consisting of (CR3aR3b)pCON(R3b)X and (CR3aR3b)pN(R3b)CO(X), wherein said groups are in the 3- (meta) or 4- (para) position with respect to the substituent Z; W is selected from the group consisting of NR4a, O, S, S?O, SO2 and C(R4aR4b)2; X is hydroge
    Type: Application
    Filed: July 20, 2009
    Publication date: October 6, 2011
    Applicant: Ramot at tel-Aviv University Ltd.
    Inventors: Simon David Edwards, Meriel Ruth Kimberley, Richard Edward Armer, Nawaz Mohammed Khan