1,2-thiazoles (including Hydrogenated) Patents (Class 514/372)
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Publication number: 20130310428Abstract: A thermo-stable, arsenic-free synergistic biocide concentrate composition to afford enhanced antimicrobial properties to a polymer matrix comprising (i) a mixture of trihalomethyl-thio-phthalimide analogue and a second biocide; (ii) an antioxidant; (iii) a carrier; and (iv) optionally, one or more additives. The composition is capable of withstanding high processing temperatures up to about 250° C., substantially without thermal degradation of biocides and discoloration of the polymer matrix employed.Type: ApplicationFiled: August 5, 2011Publication date: November 21, 2013Applicant: ISP INVESTMENTS INC.Inventors: Bartko Joseph, Karen Winkowski
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Publication number: 20130303524Abstract: The subject matter herein is directed to carbazole-containing sulfonamide derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, B, C, D, E, F, G, H, a, and b are accordingly described. Also provided are pharmaceutical compositions comprising the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, obesity, metabolic syndrome, Cushing's syndrome, and glaucoma.Type: ApplicationFiled: May 10, 2013Publication date: November 14, 2013Inventors: Ross Bersot, Paul Humphries
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Publication number: 20130296369Abstract: The present invention relates to cyanoenamine derivatives, their process of preparation, intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants and in material protection, using these compounds or compositions.Type: ApplicationFiled: November 11, 2011Publication date: November 7, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Jürgen Benting, Ulrike Wachendorff-Neumann, Philippe Desbordes, Christophe Dubost, Pierre Genix, Shinichi Narabu, Jean-Pierre Vors
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Publication number: 20130296310Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.Type: ApplicationFiled: July 1, 2013Publication date: November 7, 2013Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Patent number: 8563714Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.Type: GrantFiled: May 17, 2010Date of Patent: October 22, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
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Publication number: 20130267570Abstract: An aqueous, stable, highly-concentrated preservative composition comprising (i) about 5 to 50 wt % of a dehydroacetic acid (DHA) or a salt thereof; (ii) about 1 to 20 wt % of a 2-methyl-4-isothiazolin-3-one (MIT); (iii) about 0.1 to 10 wt % of at least one block copolymer; (iv) optionally, about 0.01 to 5.0 wt % of at least one sulfosuccinate surfactant; (v) optionally, about 0.01 to 5.0 wt % of at least one sequestering agent; and (vi) optionally, about 0.01 to 5.0 wt % of one or more additives. Also disclosed is a process for preparing said preservative composition.Type: ApplicationFiled: November 18, 2011Publication date: October 10, 2013Applicant: ISP Investments Inc.Inventors: Raman Premachandran, Najeeb H. Najehakimi, Karen Winkowski, Andrea Wingenfeld
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Patent number: 8546588Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: GrantFiled: February 25, 2011Date of Patent: October 1, 2013Assignee: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
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Patent number: 8546563Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: October 30, 2008Date of Patent: October 1, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Angela Berry, Doris Riether, Renee M. Zindell, Nigel James Blumire
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Patent number: 8546305Abstract: The invention relates to active compound combinations, in particular a fungicidal and/or insecticidal composition, comprising Isotianil (3,4-dichloro-N-(2-cyanophenyl)-5-isothiazolecarboxamide) and at least one further insecticide of the anthranilamide group and optionally one further insecticide of the neonicotinoids. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi and/or microorganisms and/or pests of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.Type: GrantFiled: November 28, 2008Date of Patent: October 1, 2013Assignee: Bayer CropScience AGInventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Heike Hungenberg, Wolfgang Thielert
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Publication number: 20130252937Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: March 14, 2013Publication date: September 26, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Matthias ECKHARDT, Sara FRATTINI, Dieter HAMPRECHT, Frank HIMMELSBACH, Elke LANGKOPF, Iain LINGARD, Stefan PETERS, Holger WAGNER
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Publication number: 20130236434Abstract: A method of enhancing binding of cells to an integrin-binding ligand comprises treating integrin-expressing cells in vitro with an agonist of integrin, wherein the integrin is selected from the group consisting of ?4?1, ?5?1, ?4?7, ?v?3 and ?L?2, and contacting the treated cells with an integrin-binding ligand; integrin agonist compounds having the general formula I; methods of treating integrin-expressing cells with such agonists to enhance binding; and therapeutic methods comprising administering agonist-treated cells or agonist compounds to a mammal.Type: ApplicationFiled: November 16, 2011Publication date: September 12, 2013Applicant: TEXAS HEART INSTITUTEInventors: Ronald J. Biediger, William C. Gundlach, IV, Robert V. Market, Michael M. Savage, Peter Vanderslice
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Publication number: 20130225617Abstract: Compounds of the invention are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions.Type: ApplicationFiled: January 31, 2013Publication date: August 29, 2013Applicant: PULMAGEN THERAPEUTICS (ASTHMA) LIMITEDInventor: PULMAGEN THERAPEUTICS (ASTHMA) LIMITED
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Publication number: 20130217690Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is O or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.Type: ApplicationFiled: March 15, 2013Publication date: August 22, 2013Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventor: Mochida Pharmaceutical Co., Ltd.
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Publication number: 20130210873Abstract: The present invention provides a wood preservative formulation comprising an isothiazolone, an organic fungicidal timber decay preservative and an unsaturated carboxylic or sulphonic acid, salt or precursor thereof. The formulations of the invention are surprisingly effective at protecting wood and other cellulosic substrates, in particular at providing prolonged protection against in-service surface staining. The invention also provides methods for treating wood and other cellulosic substrates with said formulations.Type: ApplicationFiled: April 13, 2011Publication date: August 15, 2013Applicant: Arch Timber Protection LimitedInventors: Paul Stuart Warburton, Lee Mason, Andrew Stewart Hughes
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Publication number: 20130210721Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is O or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.Type: ApplicationFiled: March 15, 2013Publication date: August 15, 2013Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventor: MOCHIDA PHARMACEUTICAL CO., LTD.
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Publication number: 20130209823Abstract: The present invention provides a method of protecting wood or other celiulosic material from decay by copper-tolerant fungi, and wood preservative formulations for use in the same. The wood preservative formulations comprise a biocidal metal compound, a 1,2,4-triazole and a didecyl quaternary ammonium cation. Didecyldimethyl quaternary ammonium compounds are particularly preferred.Type: ApplicationFiled: June 21, 2011Publication date: August 15, 2013Applicant: ARCH TIMBER PROTECTION LIMITEDInventors: Craig Andrew Mars, David Grindon Cantrell, Kevin Hughes, Andrew Stewart Hughes
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Publication number: 20130203739Abstract: [Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogues and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of solving the problem] A compound of Formula (1): (where n is 0 to 2; p is 0 to 4; h is 0 to 3; j is 0 to 3; k is 0 to 2; a ring B is an aryl group or a heteroaryl group; X is O, S, or —NR7—; J1 is —CR11aR11b— or —NR11c—; J2 is —CR12aR12b— or —NR12c—; and R1 to R12c are specific groups), a salt of the compound, or a solvate of the salt or the compound.Type: ApplicationFiled: October 11, 2011Publication date: August 8, 2013Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventors: Akihiro Okano, Munetaka Ohkouchi, Muneyoshi Makabe
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Publication number: 20130203825Abstract: A phosphate-free, highly-concentrated aqueous dispersion composition comprising at least one biocide, sulfosuccinate based surfactant, block copolymer, suspending agent, and optionally an antifoaming agent and desired additives if any. The composition of the present application is significantly stable against heat, cold, transit, storage and dilution for at least 18 months. The preferred biocides of the dispersion composition are 2-meth-4-isothiazolin-3-one (MIT), 1,2-Benzisothiazolin-3-one (BIT), 5-Chloro-2-methyl-4-isothiazolin-3-one (CMIT), 2-Octyl-4-isothiazolin-3-one (Off) 3-Iodo-2-propynylbutyl carbamate (IPBC), oxyfluorfen, thiabendazole, terbutryn, zinc pyrithione (ZnPy), bronopol, folpet, diiiron, dehydroacetic acid (DHA), dazomet and carbendazim alone or in combination. Also disclosed is a process for preparing the dispersion composition and appropriate applications thereof.Type: ApplicationFiled: May 26, 2011Publication date: August 8, 2013Applicant: ISP Investments Inc.Inventors: Raman Premachandran, Karen Winkowski
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Publication number: 20130203824Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.Type: ApplicationFiled: March 5, 2013Publication date: August 8, 2013Inventors: Lijun Sun, Jun Jiang, Christopher Borella, Shoujun Chen, Keizo Koya
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Patent number: 8501933Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.Type: GrantFiled: July 26, 2010Date of Patent: August 6, 2013Assignee: Roche Palo Alto LLCInventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Patent number: 8501794Abstract: The present application relates to isothiazolylidene containing compounds of Formula (I) wherein R1, R2, R3, R4, and L are as defined in the specification, compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions.Type: GrantFiled: November 4, 2009Date of Patent: August 6, 2013Assignee: AbbVie Inc.Inventors: William A. Carroll, Michael J. Dart, Teodozyj Kolasa, Tongmei Li, Derek W. Nelson, Meena V. Patel, Sridhar Peddi, Arturo Perez-Medrano, Xueqing Wang
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Publication number: 20130196994Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.Type: ApplicationFiled: November 16, 2012Publication date: August 1, 2013Applicant: OMEROS CORPORATIONInventor: Omeros Corporation
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Publication number: 20130184319Abstract: The invention relates to novel fungicidally active compound combinations of 2?-cyano-3,4-dichloroisothiazole-5-carboxanilide and active compounds listed in the disclosure.Type: ApplicationFiled: March 5, 2013Publication date: July 18, 2013Applicant: BAYER CROPSCIENCE AGInventor: Bayer CropScience AG
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Publication number: 20130172353Abstract: This invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R, R1, R2, R3, n, X1, X2, L1, and L2 are as defined herein. The compounds of Formula I are useful as receptor tyrosine kinase (RTK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders and metabolic diseases.Type: ApplicationFiled: December 27, 2012Publication date: July 4, 2013Applicant: Allergan, Inc.Inventor: Allergan, Inc.
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Patent number: 8476287Abstract: [Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of solving the problem] A compound of Formula (I): (where n is 0 to 2; p is 0 to 4; j is 0 to 3; k is 0 to 2; a ring A is an aryl group which is optionally substituted with L or a heterocyclic group which is optionally substituted with L; a ring B is a benzene ring, a pyridine ring, or a pyrimidine ring; X is O, S, —NR7—; and R1 to R7 are specific groups), a salt of the compound, or a solvate of the salt or the compound.Type: GrantFiled: December 24, 2010Date of Patent: July 2, 2013Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Akihiro Okano, Naoto Kosuga, Munetaka Ohkouchi, Daido Hotta, Muneyoshi Makabe
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Publication number: 20130165489Abstract: The present invention includes a method of inhibiting, suppressing or preventing a viral infection in a subject, comprising administering to the subject a pharmaceutical composition comprising one or more of the compounds useful within the invention.Type: ApplicationFiled: April 25, 2011Publication date: June 27, 2013Applicants: The Trustees of the University of Pennsylvania, Philadelphia Health & Education Corporation d/b/a Drexel University College of MedicineInventors: Simon Cocklin, Sandhya Kortagere, Amos B. Smith, III
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Publication number: 20130158018Abstract: Disclosed are Cathepsin-S reversible inhibitor compounds of the formula (I) which are useful in the treatment of autoimmune and other diseases. Also disclosed are pharmaceutical compositions containing the same, and methods of making and using the same.Type: ApplicationFiled: March 2, 2011Publication date: June 20, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Michael J. Burke, Derek Cogan, Donghong Amy Gao, Alexander Heim-Riether, Eugene Richard Hickey, Matthew Russell Netherton, Philip Dean Ramsden, David Charles Thompson, Zhaoming Xiong
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Patent number: 8466182Abstract: The present invention relates to compounds of Formula I below and their tautomers or pharmaceutically acceptable salts, compositions and methods of uses thereof.Type: GrantFiled: November 2, 2011Date of Patent: June 18, 2013Assignees: The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone, University of Maryland, BaltimoreInventors: Paul J. Muchowski, Joseph M. Muchowski, Robert Schwarcz, Paolo Guidetti
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Publication number: 20130150326Abstract: Described herein are compounds that are inhibitors of autotaxin. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such inhibitors, alone and in combination with other compounds, for treating autotaxin-dependent or autotaxin-mediated conditions or diseases.Type: ApplicationFiled: August 19, 2011Publication date: June 13, 2013Applicant: Amira Pharmaceuticals, Inc.Inventors: Jeffrey Roger Roppe, Timothy Andrew Parr, Nicholas Simon Stock, Deborah Volkots, John Howard Hutchinson
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Publication number: 20130150367Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: ApplicationFiled: September 12, 2012Publication date: June 13, 2013Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
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Patent number: 8450304Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, and R4 are as defined in the specification. The invention also comprises pharmaceutical compositions comprising the compounds of formula (I) and methods of preventing, treating or ameliorating a CCR2 mediated syndrome, disorder or disease, for example, type II diabetes, obesity or asthma, by administering the compounds of formula (I).Type: GrantFiled: December 9, 2009Date of Patent: May 28, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Xuqing Zhang, Heather Rae Hufnagel, Cuifen Hou, Dana L. Johnson, Zhihua Sui, Barry Fegely, David Breslin
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Patent number: 8445527Abstract: The present invention provides a method of treating a HCV infection in a subject in need thereof by administering a compound of Formula I: or pharmaceutically acceptable salts thereof or stereoisomers thereof.Type: GrantFiled: May 22, 2012Date of Patent: May 21, 2013Assignee: Novartis AGInventors: Michael Patane, Prakash Raman, David Thomas Parker, Jiping Fu, Branko Radetich, Mohindra Seepersaud, Aregahegn Yifru, Rui Zheng, Trixi Brandl, Francois Lenoir, Pascal Rigollier, Oliver Simic
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Publication number: 20130116240Abstract: Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.Type: ApplicationFiled: September 26, 2012Publication date: May 9, 2013Applicant: JAPAN TOBACCO INC.Inventor: Japan Tobacco Inc.
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Patent number: 8435996Abstract: The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: GrantFiled: July 31, 2008Date of Patent: May 7, 2013Assignee: Synta Pharmaceuticals Corp.Inventor: Shoujun Chen
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Publication number: 20130102646Abstract: The invention relates to a microbicidal composition which comprises a mixture of at least two components, the first component being 2-methyl-3-isothiazolone (MIT) and the second component being at least one active compound selected from the following groups of active compounds: a) compound having activated methylol groups b) quats or polyquats c) carbamates d) organic acids e) aromatic alcohols.Type: ApplicationFiled: December 14, 2012Publication date: April 25, 2013Applicant: ISP Investment Inc.Inventor: ISP Investment Inc.
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Patent number: 8426372Abstract: The invention relates to novel fungicidally active compound combinations of 2?-cyano-3,4-dichloroisothiazole-5-carboxanilide of the formula and active compounds listed in the disclosure.Type: GrantFiled: May 13, 2010Date of Patent: April 23, 2013Assignee: Bayer Cropscience AGInventors: Peter Dahmen, Ulrike Wachendorff-Neumann, Rolf Pontzen, Lutz Assmann, Haruko Sawada
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Patent number: 8410150Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 6, 2008Date of Patent: April 2, 2013Assignee: University Health NetworkInventors: Heinz W. Pauls, Peter Brent Sampson, Bryan T. Forrest, Radoslaw Laufer, Yong Liu, Miklos Feher, Yi Yao, Guohua Pan
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Patent number: 8404727Abstract: The present patent application relates to a pharmaceutical composition for oral administration that includes a certain pyrrolidine derivative as DPP-IV inhibitor, and a pharmaceutically acceptable excipient. More particularly, the present invention contemplates pharmaceutical compositions that include melogliptin and a pharmaceutically acceptable excipient as well as to processes for preparing the pharmaceutical composition and the use of the composition in reducing glucose level in a subject. The present invention also contemplates an impurity associated with melogliptin.Type: GrantFiled: January 7, 2010Date of Patent: March 26, 2013Assignee: Glenmark Pharmaceuticals S.A.Inventors: Ulhas Dhuppad, Vaijnath Aravat, Someshwar Navhat, Abraham Thomas, Suresh Kadam
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Patent number: 8404728Abstract: This disclosure relates to materials and methods for inhibiting Botulinum neurotoxin, and more particularly to materials and methods for inhibiting the zinc endopeptidase of Botulinum neurotoxin serotypes A, D and/or E (BoNTA, BoNTD and/or BoNTE).Type: GrantFiled: July 29, 2010Date of Patent: March 26, 2013Assignees: Mayo Foundation for Medical Education and Research, U.S. Army Medical Research and Material CommandInventors: Yuan-Ping Pang, Jewn Giew Park, Shaohua Wang, Anuradha Vummenthala, Rajesh K Mishra, Jon Davis, Charles B. Millard, James J. Schmidt
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Patent number: 8398759Abstract: An ecologically compatible anti-microbial-adhesion agent is described, which is particularly suitable for use in anti-fouling paints, preferably for boats, characterized in that it comprises a compound selected from eugenol, vanillin, benzaldehyde substituted with one or two substituents selected from the groups —OH (hydroxy) and —OCH3 (methoxy), or any combination thereof. An anti-fouling paint is also described, particularly for boats, comprising the anti-microbial-adhesion agent mentioned above and other components selected from conventional biocides, solvents, resins, pigments, charges and fillings, and combinations thereof.Type: GrantFiled: May 12, 2009Date of Patent: March 19, 2013Assignee: Biopaint S.R.L.Inventors: Cecilia Calisti, Giulio Zanaroli, Fabio Fava, Alessandra Bontempi Di Roccaspada, Maurizio Ruzzi
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Patent number: 8399435Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.Type: GrantFiled: October 7, 2011Date of Patent: March 19, 2013Assignee: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Jun Jiang, Christopher Borella, Shoujun Chen, Keizo Koya
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Publication number: 20130065897Abstract: The present invention provides novel compounds of the Formula I, pharmaceutical compositions comprising such compounds and methods for using such compounds as agents or drugs for inhibiting perforin activity and for treating a subject at risk of or susceptible to a disease or disorder, or having a disease or disorder associated with undesirable perforin activity.Type: ApplicationFiled: December 22, 2010Publication date: March 14, 2013Applicant: PETER MACCALLUM CANCER INSTITUTEInventors: Julie Ann Spicer, Kristiina Maria Huttunen, Dani Michelle Lyons, Joseph Albert Trapani, Mark John Smyth, William Alexander Denny
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Publication number: 20130053364Abstract: The invention provides sulphone compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various sulphone compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.Type: ApplicationFiled: April 23, 2012Publication date: February 28, 2013Inventors: Hazel J. Dyke, Susan M. Cramp, Thomas D. Pallin, Janusz J. Kulagowski, John G. Montana, Robert Zahler
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Publication number: 20130053422Abstract: Environmentally beneficial antimicrobial compositions are described that include a cationic surfactant and certain antimicrobial agents or preservatives. Useful cationic surfactants include lauric arginate (LAE). Advantageously, the pH of the composition may be adjusted to reduce irritancy.Type: ApplicationFiled: March 22, 2011Publication date: February 28, 2013Inventors: Sarah L. Edmonds, James Bingham, Mitchell Cohen, Helen Burk
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Publication number: 20130045264Abstract: There is provided an antifouling coating composition capable of forming an antifouling coating film which has stable coating film consumption degree on ships, underwater structures and the like and which exhibits excellent antifouling property over a long term. The antifouling coating composition includes a hydrolyzable copolymer (A) and an antifouling agent (B), wherein the hydrolyzable copolymer (A) is, e.g., a metal salt bond-containing copolymer having a component unit derived from a monomer (a21) represented by the general formula (II): CH2?C(R2)—COO-M-O—CO—C(R2)?CH2??(II) [In the formula (II), M is zinc or copper, and R2 is a hydrogen atom or a methyl group], and a component unit derived from other unsaturated monomer (a22) copolymerizable with the monomer (a21), and wherein the antifouling agent (B) includes at least medetomidine.Type: ApplicationFiled: March 18, 2011Publication date: February 21, 2013Applicant: CHUGOKU MARINE PAINTS, LTD.Inventors: Satoshi Masuda, Yusuke Hayashi, Yukio Kozono
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Patent number: 8362051Abstract: Wallboard and facing paper that provides increased mold resistance at lower biocide loadings. The biocide is: (a) an n-alkyl isothiazolinone such as octylisothiazolinone (OIT), a monohalo and dihalo substituted n-alkylisothiazolinone such as chloromethylisothiazolinone (CMIT) or dichlorooctylisothiazolinone (DCOIT), 3-iodo-2-propynyl-butylcarbamate (IPBC), chlorothalonil, methylene-bis-thiocyanate, or mixtures of two or more thereof; or (b) carbendazim and a second biocide selected from 3-iodo-2-propynyl-butylcarbamate (IPBC), diiodomethyltolylsulfone (DIMTS), sodium pyrithione, octylisothiazolinone (OIT), dichlorooctylisothiazolinone (DCOIT), and chlorothalonil.Type: GrantFiled: January 18, 2008Date of Patent: January 29, 2013Assignee: Rohm and Haas CompanyInventors: Sheila M. Tinetti, Paul Foley, Li Wang, Michael V. Enzien, Sanjay B. Bishnoi
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Patent number: 8362003Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: GrantFiled: June 16, 2011Date of Patent: January 29, 2013Assignee: Incyte CorporationInventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taisheng Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han
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Patent number: 8362052Abstract: The present invention relates to a compound represented by formula (I): (wherein R, R2, R3 and R4 each independently represent a hydrogen or halogen atom; R5 and R6 each independently represent a hydrogen atom or lower alkyl or together represent oxo; X represents C(O) or the like; Y represents an oxygen atom or the like; Z represents a hydrogen atom or the like; R represents 5- or 6-membered heteroaryl having 1-3 hetero atoms selected from the group consisting of nitrogen, sulfur and oxygen atoms, contained within a ring, or the like) or to a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 9, 2010Date of Patent: January 29, 2013Assignee: MSD K.K.Inventors: Keisuke Arakawa, Teruyuki Nishimura, Yuichi Sugimoto, Hiroyuki Takahashi, Tadashi Shimamura
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Patent number: 8354412Abstract: The present invention relates to new compounds, ligands of the beta-3 adrenergic receptor, their preparation and their use in therapy or as research tools for said receptor; the invention also relates to a process for the preparation of the compounds of the invention and the use of inverse agonists of the beta-3 adrenergic receptor as medicaments.Type: GrantFiled: August 3, 2011Date of Patent: January 15, 2013Assignee: Universita' Degli Studi di BariInventors: Antonio Scilimati, Maria Grazia Perrone, Ernesto Santandrea
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Publication number: 20130005655Abstract: A composition comprising doxepin, or a pharmaceutically acceptable salt, or prodrug thereof, and a compound that enhances sleep onset, sleep maintenance or reduces early morning awakenings. These compositions are useful for treating multiple manifestations of insomnia.Type: ApplicationFiled: September 12, 2012Publication date: January 3, 2013Applicant: Somaxon Pharmaceuticals, Inc.Inventors: Philip Jochelson, Robert Mansbach, Michael Skinner, Neil B. Kavey