Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Piperazine Ring Patents (Class 514/255.01)
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Publication number: 20140094464Abstract: The invention described herein pertains to compounds and compositions for treating Ape1 mediated diseases. In particular, the invention described herein pertains to quinone compounds and pharmaceutical compositions containing them for treating Ape1 mediated diseases.Type: ApplicationFiled: May 25, 2012Publication date: April 3, 2014Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATIONInventors: Mark R. Kelley, James H. Wikel
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Publication number: 20140094455Abstract: Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.Type: ApplicationFiled: August 19, 2013Publication date: April 3, 2014Applicant: ARIZONA BOARD OF REAGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONAInventors: Gary A. Flynn, Andrea J. Yool, Elton Rodrigues Migliati, Leslie S. Ritter
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Publication number: 20140086936Abstract: The present invention provides matriptase inhibitors and compositions for treating and preventing orthomyxovirus infections such as flu infections. The present invention also provides novel compounds, compositions, methods of use, uses and kits thereof for inhibiting matriptase. Such compounds are useful for treating and preventing orthomyxovirus infections, such as flu infections, and for inhibiting tumor growth, progression and/or metastasis.Type: ApplicationFiled: May 28, 2012Publication date: March 27, 2014Applicant: SOCPRA SCIENCES SANTE ET HUMAINES S.E.C.Inventors: Martin Richter, Richard Leduc, Eloic Colombo, Eric Marsault
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Publication number: 20140088095Abstract: There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof.Type: ApplicationFiled: September 16, 2013Publication date: March 27, 2014Applicant: SK Biopharmaceuticals Co., Ltd.Inventors: Byong Sung KWAK, Hong Sik MOON, Han-Ju YI, Young Soon KANG, Dae Joong IM, Eun Hee CHAE, Sang Mi CHAE, Ki Ho LEE
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Publication number: 20140088074Abstract: Fluorinated arylalkylaminocarboxamide derivatives of formula (I) are described wherein W, J, n, R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification and pharmaceutically salts thereof, pharmaceutical compositions containing them as active ingredients and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urological, and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.Type: ApplicationFiled: May 29, 2012Publication date: March 27, 2014Applicant: NEWRON PHARMACEUTICALS S.P.A.Inventor: Paolo Pevarello
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Patent number: 8669261Abstract: Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R?, R?, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.Type: GrantFiled: April 30, 2013Date of Patent: March 11, 2014Assignee: Congenia SLRInventors: Daniele Fancelli, Mario Varasi, Simon Plyte, Marco Ballarini, Anna Cappa, Giacomo Carenzi, Saverio Minucci, Gilles Pain, Manuela Villa
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Publication number: 20140066446Abstract: Provided herein are 2,5-disubstituted arylsulfonamide CCR3 antagonists, e.g., compounds of Formula I, and pharmaceutical compositions thereof: Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: ApplicationFiled: August 30, 2013Publication date: March 6, 2014Applicant: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Garrett Thomas Potter
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Publication number: 20140066369Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as single pharmaceutical agents or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.Type: ApplicationFiled: April 18, 2012Publication date: March 6, 2014Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Robert M. Jones, Daniel J. Buzard, Sangdon Han, Sun Hee Kim, Juerg Lehmann, Dawei Yue, Xiuwen Zhu
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Patent number: 8658642Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: GrantFiled: March 15, 2013Date of Patent: February 25, 2014Assignee: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Jared Andrew Forrester
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Patent number: 8653080Abstract: The disclosure provides methods and compositions useful for screening inhibitors of aggregation mediated proteotoxicity. The disclosure provides transgenic animals and cell useful for such screening. Also provided are compounds useful for inhibiting aggregation mediated proteotoxicity in a subject.Type: GrantFiled: January 14, 2010Date of Patent: February 18, 2014Assignee: Salk Institute for Biological StudiesInventors: Andrew Dillin, Thomas J. Baiga, Erik Kapernick, Joseph P. Noel
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Patent number: 8648083Abstract: A method of treating diabetic hyperlipidemia or lipidemia with carbamoyloxy arylalkanoyl arylpiperazine compounds including:Type: GrantFiled: July 8, 2011Date of Patent: February 11, 2014Assignee: SK Biopharmaceuticals Co., Ltd.Inventors: Hong Sik Moon, Han Ju Yi, Eun Hee Chae, Sang Mi Chae, Hye Won Shin
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Patent number: 8637497Abstract: The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.Type: GrantFiled: July 18, 2011Date of Patent: January 28, 2014Assignee: Incyte CorporationInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian Metcalf
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Patent number: 8629149Abstract: Compounds of formula (I) which are useful in ameliorating conditions characterized by unwanted sodium and/or calcium channel actrvrh, particularly Nav 1, 7, Nav 1, 8, or Cav 3, 2 channel activity are disclosed. More specifically, compounds for use in the treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's disease, depression, schizophrenia, psychosis, and tinnitus are disclosed.Type: GrantFiled: September 3, 2010Date of Patent: January 14, 2014Assignee: Zalicus Pharmaceuticals Ltd.Inventors: Hassan Pajouhesh, Yanbing Ding
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Patent number: 8623857Abstract: The present invention provide Imidazole Carboxamide Compounds of Formula (I): wherein D, T, R1, R2, R3, and R6 are as defined herein, and pharmaceutically acceptable salts of such Imidazole Carboxamide Compounds. The Imidazole Carboxamide Compounds are useful in the treatment of cancer and other aberrant conditions that result from overstimulation of the PDK-1 signaling pathway.Type: GrantFiled: May 24, 2011Date of Patent: January 7, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Hon-Chung Tsui, Sunil Paliwal, Hyunjin M. Kim, Angela D. Kerekes, Mary Ann Caplen, Sara J. Esposite, Brian A. McKittrick, Thierry Olivier Fischmann, Ronald J. Doll, Matthew Paul Rainka, Ang Li
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Patent number: 8623865Abstract: The invention relates to novel acylpiperazinone compounds, to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.Type: GrantFiled: January 15, 2013Date of Patent: January 7, 2014Assignee: Fab Pharma S.A.S.Inventors: Vincent Gerusz, Sonia Escaich, Mayalen Oxoby, Francois Moreau
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Patent number: 8609664Abstract: The present application describes modulators of MIP-1? of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, T, W, R1, R4, R5, R5a and R5b are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using said modulators are disclosed.Type: GrantFiled: August 5, 2009Date of Patent: December 17, 2013Assignee: Bristol-Myers Squibb Co.Inventors: Percy H. Carter, Cullen L. Cavallaro, George V. De Lucca
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Publication number: 20130324556Abstract: A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrate thereof Wherein Y, Z, R3, U, R4, m and n are as defined in the claims.Type: ApplicationFiled: January 27, 2012Publication date: December 5, 2013Inventors: Joe William Boyd, Paul Meo, Michael Higginbottom, Iain Simpson, David Mark Mountford, Edward Daniel Savory
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Publication number: 20130324555Abstract: The present invention is directed to the method of use of effective pharmaceutical formulations for the treatment of diseases caused by apicomplexan parasites, said formulation comprised of a salicylanilide or salicylanilide derivative, disclosed herein, alone or in combination with one or more other active or excipient pharmaceutical substances. The present invention is further directed to the method of use of effective pharmaceutical formulations for the treatment of diseases caused by apicomplexan parasites, said formulation comprised of a combination of salicylanilides or salicylanilide derivatives, disclosed herein. The present invention is further directed to the method of use of effective pharmaceutical formulations for the treatment of diseases caused by apicomplexan parasites, said formulation comprised of a combination of salicylanilides or salicylanilide derivatives, disclosed herein, further comprised of one or more active or excipient pharmaceutical substances.Type: ApplicationFiled: May 29, 2013Publication date: December 5, 2013Inventors: Richard Delarey Wood, Rima McLeod, Ernest Mui, Alina Fomovska, William Welsh
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Publication number: 20130315981Abstract: The present invention is a method of increasing lipolysis in an adipose tissue of a mammal comprising delivering to macrophages at the adipose tissue of the mammal an effective amount of an agent which reduces the concentration of macrophages at the adipose tissue of the mammal, thereby increasing lipolysis in the adipose tissue of the mammal.Type: ApplicationFiled: June 22, 2011Publication date: November 28, 2013Applicant: The Trustees of Columbia University in the City of New YorkInventors: Anthony W. Ferrante, JR., Aliki Kosteli
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Patent number: 8586589Abstract: The present invention relates to piperidine and piperazine phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain.Type: GrantFiled: October 2, 2012Date of Patent: November 19, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Esther Martinborough, Lev T. D. Fanning, Urvi Sheth, Dean Wilson, Andreas P. Termin, Timothy D. Neubert, Nicole Hilgraf, Tara Leanne Hampton, Tara Whitney, Aarti Sameer Kawatkar, Danielle Lehsten, Dean Stamos, Jinglan Zhou, Vijayalaksmi Arumugam, Corey Anderson
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Publication number: 20130303545Abstract: The invention relates to methods and compositions for the treatment or prevention of protein conformation disorders. In particular, the invention relates to an LSD1 inhibitor for use in treating or preventing a protein conformation disorder, such as, e.g., Huntington Disease.Type: ApplicationFiled: September 20, 2011Publication date: November 14, 2013Inventors: Tamara Maes, Carlos Buesa Arjol
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Publication number: 20130289034Abstract: Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.Type: ApplicationFiled: June 21, 2013Publication date: October 31, 2013Inventors: Orion D. JANKOWSKI, Kieron E. WESSON, Paul MOLLARD, William D. SHRADER
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Patent number: 8569495Abstract: This invention is directed to compounds and salts that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the compounds and salts, pharmaceutical compositions and kits comprising the compounds and salts, uses of the compounds and salts to make medicaments, and treatments comprising the administration of the compounds and salts to animals in need of the treatments.Type: GrantFiled: December 16, 2008Date of Patent: October 29, 2013Assignee: Intervet International B.V.Inventors: Christophe Pierre Alain Chassaing, Jörg Schröder, Thomas Simon Ilg, Manfred Uphoff, Thorsten Meyer
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Patent number: 8557800Abstract: The invention relates to substituted adamantane compounds, pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.Type: GrantFiled: October 19, 2011Date of Patent: October 15, 2013Assignee: Apogee Biotechnology CorporationInventors: Charles D. Smith, Kevin J. French, Yan Zhuang
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Publication number: 20130267516Abstract: Compounds of general formula I, (formula [I)], their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.Type: ApplicationFiled: November 21, 2011Publication date: October 10, 2013Applicant: LEO PHARMA A/SInventors: Kristoffer Månsson, Lars Kristian Albert Blæhr
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Publication number: 20130267537Abstract: Certain substituted sulfonamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: ApplicationFiled: February 5, 2013Publication date: October 10, 2013Applicant: Cytokinetics, Inc.Inventors: Bradley Paul MORGAN, Fady MALIK, Erica Anne KRAYNACK, Alexander Ramon MUCI, Xiangping QIAN, David J. MORGANS, JR.
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Publication number: 20130261132Abstract: Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.Type: ApplicationFiled: November 21, 2011Publication date: October 3, 2013Applicant: LEO PHARMA A/SInventors: Per Vedso, Lars Kristian Albert BlÆher
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Publication number: 20130251673Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.Type: ApplicationFiled: December 21, 2012Publication date: September 26, 2013Applicant: Novira Therapeutics, INC.Inventors: George D. HARTMAN, Osvaldo A. FLORES
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Publication number: 20130244995Abstract: Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.Type: ApplicationFiled: November 21, 2011Publication date: September 19, 2013Applicant: LEO PHARMA A/SInventors: Per Vedsø, Lars Kristian Albert Blæhr
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Patent number: 8536184Abstract: The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof and a process for making thereof. The compounds have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention also provides intermediate compounds useful in the process, as well as final products produced by the process, and salts or prodrugs thereof. The invention further provides a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases comprising administering an effective amount of a compound according to the invention to a patient in need thereof.Type: GrantFiled: November 19, 2009Date of Patent: September 17, 2013Assignee: Millennium Pharmaceuticals, Inc.Inventors: James Kanter, James Robinson, Anjali Pandey, Robert M. Scarborough
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Patent number: 8524717Abstract: The invention relates to phenylcyclopropylamine acetamide derivatives and their use in treating diseases.Type: GrantFiled: April 18, 2011Date of Patent: September 3, 2013Assignee: Oryzon Genomics, S.A.Inventors: Nathalie Guibourt, Alberto Ortega Munoz, Julio Castro-Palomino Laria
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ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
Publication number: 20130225605Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: April 22, 2013Publication date: August 29, 2013Applicant: SANOFIInventor: SANOFI -
Patent number: 8518950Abstract: The invention relates to compounds of structural formula (I) and structural formula (VI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein R, R1, R2, Z, L, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: GrantFiled: January 25, 2006Date of Patent: August 27, 2013Assignee: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Shoujun Chen, Jun Jiang, Yu Xie, Chih-Yi Yu
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Patent number: 8518951Abstract: Described herein are 4-methyl-piperazine-1-carbothioic acid amide derivatives and analogs, as well as compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by hemorrhagic fever viruses, such as Arenaviruses.Type: GrantFiled: December 28, 2011Date of Patent: August 27, 2013Assignee: Siga Technologies, Inc.Inventors: Dennis E. Hruby, Tove C. Bolken, Dongcheng Dai
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Publication number: 20130217687Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: ApplicationFiled: March 15, 2013Publication date: August 22, 2013Applicant: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei LY, Jared Andrew FORRESTER
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Publication number: 20130217686Abstract: A novel methylcyclohexane derivative, and a pharmaceutical composition including the same that is effective for the prevention or treatment of pain.Type: ApplicationFiled: September 28, 2011Publication date: August 22, 2013Applicant: SK BIOPHARMACEUTICALS CO., LTD.Inventors: Sung Jin Bae, Han Ju Yi, Sun Gwan Hwang, Mo Ses Jeong, Yeo Jin Yoon, Sang Mi Chae, Joo Young Park, Eun Ju Ryu
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Patent number: 8513258Abstract: The present invention relates to compounds of general formula (I): wherein: R1 represents: halogen, CN or NO2; R2 represents: hydrogen or halogen; n represents: 1 or 2; R3 represents: phenyl substituted by one or more halogens or C1-C6 alkyls; or a cyclohexyl; as well as the therapeutically-acceptable salts or solvates thereof. These compounds are useful as protease-activated receptor-1 (PAR-1) antagonists, particularly in the treatment of thrombosis.Type: GrantFiled: May 21, 2012Date of Patent: August 20, 2013Assignee: Pierre Fabre MedicamentInventors: Michel Perez, Marie Lamothe, Bruno Le Grand, Robert Letienne
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Patent number: 8513235Abstract: The invention provides a homocysteine synthase inhibitor useful for the prophylaxis or treatment of diseases involving homocysteine synthase. The homocysteine synthase inhibitor is a compound of the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof.Type: GrantFiled: April 10, 2009Date of Patent: August 20, 2013Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Akira Nakao, Hiroko Suzuki, Ryo Tatsumi, Maki Seki, Minoru Tanaka, Tomofumi Setsuta, Hiroshi Iwasaki
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Patent number: 8497373Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.Type: GrantFiled: May 15, 2012Date of Patent: July 30, 2013Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Michael N. Greco, Harold R. Almond, Jr., Lawrence de Garavilla, Michael J. Hawkins, Michael J. Humora, Yun Qian, Donald Gilmore Walker, Sergio Cesco-Cancian, Christopher Norman Nilsen, Mitul N. Patel, Kirk Leonard Sorgi, Eugene Powell
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Publication number: 20130190288Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, A, X1, X2, X3, X4, R1, R2, R3a, R3b, R4a and R4b are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: ApplicationFiled: December 18, 2012Publication date: July 25, 2013Applicant: GENENTECH, INC.Inventor: Genentech, Inc.
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Publication number: 20130190327Abstract: The invention relates to bis-fatty acid conjugates; compositions comprising an effective amount of a bis-fatty acid conjugate; and methods for treating or preventing cancer, a metabolic disease or a neurodegenerative disease comprising the administration of an effective amount of a bis-fatty acid conjugate.Type: ApplicationFiled: February 25, 2011Publication date: July 25, 2013Applicant: CATABASIS PHARMACEUTICALS INCInventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Patent number: 8492385Abstract: The present invention relates to novel crystalline modifications of N-?-(2,4,6-triisopropylphenyl-sulfonyl)-3-hydroxyamidino-(L)-phenylalanine 4-ethoxy-carbonylpiperazide and/or salts thereof, which can be used as pharmaceutical agents, and to pharmaceutical compositions and pharmaceutical uses comprising these novel crystalline modifications.Type: GrantFiled: March 29, 2010Date of Patent: July 23, 2013Assignee: Wilex AGInventors: Alfons Grunenberg, Jana Lenz
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Patent number: 8492382Abstract: The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT2 receptor) antagonists for the treatment, prophylaxis, reversal and/or symptomatic relief of neuropathic pain, including mechanical hyperalgesia, thermal or mechanical allodynia, diabetic pain and entrapment pain, in vertebrate animals and particularly in human subjects. The AT2 receptor antagonists may be provided alone or in combination with other compounds such as those that are useful in the control of neuropathic conditions.Type: GrantFiled: August 3, 2010Date of Patent: July 23, 2013Assignee: Spinifex Pharmaceuticals Pty LtdInventors: Maree Therese Smith, Bruce Douglas Wyse
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Publication number: 20130184290Abstract: The present invention relates to formulations and methods for increasing the bioavailability of 1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one, diphenylpropanoyl)piperazine, or a salt thereof. In particular, the formulation can include one or more self-emulsifying carriers.Type: ApplicationFiled: October 26, 2012Publication date: July 18, 2013Applicants: CAPSUGEL, Inc., Zalicus Pharmaceuticals Ltd.Inventors: Zalicus Pharmaceuticals Ltd., CAPSUGEL, Inc.
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Patent number: 8481527Abstract: The present invention relates to new phenylsulfamoyl benzamide derivatives of formula (I) wherein R1-R5 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, to pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.Type: GrantFiled: October 27, 2007Date of Patent: July 9, 2013Assignee: Richter Gedeon Nyrt.Inventors: Istvan Vago, Gyula Beke, Eva Bozo, Sandor Farkas, Katalin Hornok, Gyorgy Keseru, Eva Schmidt, Eva Szentirmay, Monika Vastag
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Patent number: 8470831Abstract: Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R?, R?, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.Type: GrantFiled: September 23, 2009Date of Patent: June 25, 2013Assignee: Cogenia SRLInventors: Daniele Fancelli, Mario Varasi, Simon Plyte, Marco Ballarini, Anna Cappa, Giacomo Carenzi, Saverio Minucci, Gilles Pain, Manuela Villa
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Publication number: 20130137669Abstract: The invention relates to a method for determining the responsiveness of a Dirofilaria spp. nematode to a macrocyclic lactone, by determining the genotype of the nematode at a position in a P-glycoprotein gene of the nematode corresponding to position 1 1, and optionally to position 618, in SEQ ID NO: 1, wherein the genotype GG at a position corresponding to position 1 1, or at positions corresponding to positions 1 1 and 618, in SEQ ID NO: 1 indicates that the nematode is likely resistant to the macrocyclic lactone. The invention also relates to methods for selecting a treatment to treat an animal infected with macrocyclic lactone resistant Dirofilaria spp nematode, and treating the animal; or for selecting a prophylactic to prevent an animal from becoming infected with a macrocyclic lactone resistant Dirofilaria spp nematode, and providing the prophylactic to the animal. The invention further relates to an isolated nucleic acid having at least 80% sequence identity to SEQ ID NO: 1.Type: ApplicationFiled: March 30, 2011Publication date: May 30, 2013Inventors: Roger Prichard, Catherine Bourguinat, Timothy Geary, Rudolf Schenker
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Publication number: 20130137689Abstract: The invention relates to novel acylpiperazinone compounds, to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.Type: ApplicationFiled: January 15, 2013Publication date: May 30, 2013Applicant: FAB PHARMA S.A.S.Inventor: FAB PHARMA S.A.S.
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Publication number: 20130131081Abstract: A pharmaceutical composition that includes a carbamoyloxy arylalkanoyl arylpiperazine compound SERUM CHOLESTEROL and effectively prevents or treats diabetic nephropathy, diabetic neuropathy, diabetic vascular complications, hyperlipidemia, coronary artery disease, or inflammation.Type: ApplicationFiled: July 8, 2011Publication date: May 23, 2013Applicant: SK BIOPHARMACEUTICALS CO., LTD.Inventors: Hong Sik Moon, Han Ju Yi, Eun Hee Chae, Sang Mi Chae, Hye Won Shin
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Publication number: 20130123266Abstract: A benzene sulphonamide compound of formula I or one of its addition salts with pharmaceutically acceptable acids, for its use in a method for treating a pathology linked to an excessive effect of TNF-alpha and for its use in a method for treating the human or animal body as a direct inhibitor of TNF-alpha.Type: ApplicationFiled: July 19, 2011Publication date: May 16, 2013Applicant: VAX-CONSULTINGInventors: Jean-François Zagury, Matthieu Montes, Hadley Mouhsine, Hélène Guillemain