The Chalcogen, X, Is Part Of A -c(=x)x- Group, Wherein The X's Are The Same Or Diverse Chalcogens Patents (Class 546/335)
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Patent number: 8389553Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: GrantFiled: June 24, 2008Date of Patent: March 5, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Paul Harrington, Solomon Kattar, Thomas A. Miller, Matthew G. Stanton, Paul Tempest, David J. Witter
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Patent number: 8378107Abstract: Described herein are heteroaryl compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the heteroaryl compounds described. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: GrantFiled: October 1, 2009Date of Patent: February 19, 2013Assignee: Panmira Pharmaceuticals, LLCInventors: John Howard Hutchinson, Nicholas Simon Stock, Jeffrey Roger Roppe, Deborah Volkots
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Publication number: 20130040993Abstract: The present invention relates to hydroximoyl-heterocycle derivatives, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: December 28, 2010Publication date: February 14, 2013Inventors: Christian Beier, Jurgen Benting, David Bernier, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Stephanie Gary, Pierre Genix, Daniela Portz, Ulrike Wachendorff-Neumann
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ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
Publication number: 20130030008Abstract: 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: October 1, 2012Publication date: January 31, 2013Applicant: SANOFIInventor: Sanofi -
Patent number: 8362017Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Even more specifically, the invention provides compounds for modulating c-Kit kinase activity and methods of treating diseases mediated by c-Kit activity utilizing the compounds and pharmaceutical compositions thereof.Type: GrantFiled: August 27, 2004Date of Patent: January 29, 2013Assignee: Exelixis, Inc.Inventors: Wei Cheng, Erick Wang Co, Moon Hwan Kim, Rhett Ronald Klein, Donna T. Le, Amy Lew, John M. Nuss, Wei Xu, William Bajjalieh
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Patent number: 8362045Abstract: The invention relates to compounds corresponding to formula (I): In which Ar1, Ar2, Q, Y, Z, Alk?, k and m are as defined herein. The invention further relates to their preparations, intermediates therefor and their therapeutic uses.Type: GrantFiled: April 7, 2010Date of Patent: January 29, 2013Assignee: SanofiInventors: Lionel Barre, Christian Congy, Philippe Pointeau, Murielle Rinaldi-Carmona
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Publication number: 20120329711Abstract: The invention relates to GLP-1 receptor agonist compounds with a modified N-terminus. The compounds are of the formula Chem. 1: Y—Z—P, wherein P represents a fragment of a GLP-1 receptor agonist peptide lacking the two N-terminal amino acid residues; and Y—Z represents novel His-Ala mimetics. Examples of GLP-1 receptor agonist compounds are derived from human GLP-1 (7-37), exendin-4(1-39), or GLP-1 A (1-37). The invention also relates to derivatives of these compounds, in particular compounds with one or more albumin binding side chains capable of protracting the duration of action in vivo of these compounds. The peptides and derivatives of the invention have a good potency, a protracted pharmacokinetic profile, are stable against degradation by gastro intestinal enzymes, and/or have a high oral bioavailability. These properties are of importance in the development of GLP-1 receptor agonist compounds for subcutaneous, intravenous, and/or in particular oral administration.Type: ApplicationFiled: December 16, 2010Publication date: December 27, 2012Applicant: Nordisk A/SInventors: Janos Tibor Kodra, Johnny Madsen, Patrick William Garibay
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Publication number: 20120309796Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, asthma and COPD.Type: ApplicationFiled: May 11, 2012Publication date: December 6, 2012Inventors: Fariborz Firooznia, Paul Gillespie, Tai-An Lin, Sung-Sau So
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Publication number: 20120295923Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: ApplicationFiled: January 19, 2011Publication date: November 22, 2012Inventors: Christopher William Am Ende, Benjamin Adam Fish, Douglas Scott Johnson, Ricardo Lira, Christopher John O'Donnell, Martin Youngjin Pettersson, Corey Michael Stiff
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Publication number: 20120289554Abstract: This invention relates to novel 4-dimethylaminobutyric acid derivatives of the formula wherein A1, A2, R1, m and n are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit carnitine palmitoyl transferase (CPT) activity, in particular CPT2 activity, and can be used as medicaments in methods for the treatment of diseases modulated by CPT2 inhibitors.Type: ApplicationFiled: July 24, 2012Publication date: November 15, 2012Inventors: Mirjana Andjelkovic, Simona M. Ceccarelli, Odile Chomienne, Gerald Lewis Kaplan, Patrizio Mattei, Jefferson Wright Tilley
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Publication number: 20120282180Abstract: The present invention relates to the field of therapeutic and diagnostic agents and more specifically to compounds of formula (I) that are inhibitors of matrix-metalloproteinases (MMPs) and are useful in the treatment of diseases related thereto such as cardiovascular diseases, inflammatory diseases and malignant diseases. One embodiment of the invention is a compound of formula (I) labeled with a 18-fluorine atom having matrix metalloproteinase inhibitory activity suitable for diagnostic imaging. Also disclosed in the present invention is a pharmaceutical composition comprising the inhibitors of matrix-metalloproteinases (MMPs) of the invention or the corresponding labeled compounds useful as diagnostic imaging agents of the invention in a form suitable for mammalian administration.Type: ApplicationFiled: June 8, 2011Publication date: November 8, 2012Inventors: Hartmuth C. Kolb, Guenter Haufe, Malte Behrends, Klaus Kopka, Stefan Wagner, Verena Hugenberg, Hans-Joerg Breyholz, Sven Hermann, Michael Schaefers
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Patent number: 8283367Abstract: The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly or indirectly with proteasome activity.Type: GrantFiled: November 6, 2008Date of Patent: October 9, 2012Assignee: Cephalon, Inc.Inventors: Raffaella Bernardini, Alberto Bernareggi, Paolo G. Cassara, Germano D'Arasmo, Ernesto Menta, Ambrogio Oliva
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Publication number: 20120252810Abstract: The invention relates to fatty non-flushing acid niacin derivatives; compositions comprising an effective amount of a fatty acid non-flushing niacin derivative; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid non-flushing niacin derivative.Type: ApplicationFiled: April 4, 2012Publication date: October 4, 2012Applicant: CATABASIS PHARMACEUTICALS, INC.Inventors: Chi B. Vu, Jean E. Bemis, Michael R. Jirousek, Jill C. Milne, Amal Ting
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Patent number: 8278338Abstract: Saturated and unsaturated 3-pyridyl-benzocycloalkylmethyl-amines=compounds corresponding to formula (I), wherein the various substituents have the meaning provided in the description, and pharmaceutical formulations containing these compounds and methods for producing these compounds and related pharmaceutical formulation, and to methods for treating or inhibiting pain, depression and/or anxiety states.Type: GrantFiled: December 22, 2006Date of Patent: October 2, 2012Assignee: Gruenenthal GmbHInventors: Bernd Sundermann, Hagen-Heinrich Hennies, Klaus Schiene, Petra Bloms-Funke, Werner Englberger, Sven Frormann, Derek Saunders
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Publication number: 20120184745Abstract: The present invention is an improved method for the preparation of 4-fluoro-3-piperidin-4-yl-benzyl)-carbamic acid tert-butyl ester, compound of formula I. The invention is directed to a method of synthesis for the compound of formula I in three steps, comprising formation of 5-((tert-butoxycarbonyl)aminomethyl)-2-fluorobenzeneboronic acid (compound 11), reaction of compound 11 under Suzuki coupling conditions to yield (4-fluoro-2-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester and selective hydrogenation of the aforementioned product under hydrogenation conditions yields compound I. The invention is also directed to the intermediates 5-((tert-butoxycarbonyl)amino-methyl)-2-fluorobenzeneboronic acid (compound 11), and (4-fluoro-2-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester (compound 13).Type: ApplicationFiled: March 22, 2012Publication date: July 19, 2012Applicant: SANOFI-AVENTIS U.S. LLCInventors: Nakyen CHOY, John J. SHAY, JR., Adam W. SLEDESKI
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Patent number: 8211401Abstract: A compound of Formula I, a pharmaceutically acceptable salt, or solvate thereof: complexes with metals such as rhenium, technetium, and others to provide a complex for imaging tissues or treating disease, particularly where the metal is radioactive. Such complexes are specific to PSMA protein and can therefore be used in imaging or treating cancer of the prostate and other tissue where the protein is expressed.Type: GrantFiled: December 4, 2009Date of Patent: July 3, 2012Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig Zimmerman, John Joyal, Kevin P. Maresca, Genliang Lu, Shawn Hillier
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Publication number: 20120149736Abstract: Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ?CH— or ?N—; W is —CH?CH— Or —CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intra-cellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-nat-ural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(?O)—, —S(?O)2—, —C(?O)O—, —C(?O)NR?—, —C(?5)—NR?, —C(?NH)NR? or —S(?O)2NR — wherein R? is hydrogen or optionally substituted C1—C6 alkyl; L1 is a divalent radical of formula —(Alk1)m,(Q)n(Alk2)p— wherein m, n, p, Q, Alk1 and Alk2 are as defined in the claims; X1 represents a bond; —C(?O); or —S(?O)2—; —NR4C(?O)—, —C(?O)NR4—,— NR4C(?O)NR5—, —NR4S(?O)2—, or —S(?O)2NR4— wherein R4 and R5 are independently hydrogen or optionally substituted C1Type: ApplicationFiled: February 25, 2010Publication date: June 14, 2012Applicant: Chroma Therapeutics Ltd.Inventors: Alastair David Graham Donald, David Festus Charles Moffat, Andrew James Belfield, Carl Leslie North, Stewart Andrew Wayne Jones
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Publication number: 20120149737Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-amido-aryl compounds of the following formula (for convenience, collectively referred to herein as “AAA compounds”), which, inter alia, are (selective) retinoic acid receptor ? (RAR?) agonists. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to (selectively) activate RAR?, and in the treatment of diseases and conditions that are mediated by RAR?, that are ameliorated by the activation of RAR?, etc., including cognitive disorders, memory impairment, memory deficit, senile dementia, Alzheimer's disease, early stage Alzheimer's disease, intermediate stage Alzheimer's disease, late stage Alzheimer's disease, cognitive impairment, and mild cognitive impairment.Type: ApplicationFiled: September 1, 2010Publication date: June 14, 2012Applicant: KING'S COLLEGE LONDONInventors: Jonathan Patrick Thomas Corcoran, Sarkis Barret Kalindjian, Alan David Borthwick, David Reginald Adams, Jane Theresa Brown, David Michel Adrien Taddei, Jason John Shiers
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Publication number: 20120122764Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, B, X, m and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of compounds of the invention, and a combination of pharmacologically active agents and a compound of the invention.Type: ApplicationFiled: November 10, 2011Publication date: May 17, 2012Applicant: NOVARTIS AGInventors: Rajeshri Ganesh KARKI, Toshio KAWANAMI, Gary Michael KSANDER, Qian LIU, Muneto MOGI, Nikolaus SCHIERING, Robert SUN
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Publication number: 20120095234Abstract: This invention relates to processes and intermediates for manufacturing fused heterocyclic-type kinase inhibitor compounds, such as thienopyridine-based compounds, and to processes and intermediates for preparing intermediates that are useful in the manufacture of fused heterocyclic-type kinase inhibitor compounds, such as thienopyridine-based compounds, particularly at an industrial level.Type: ApplicationFiled: December 20, 2011Publication date: April 19, 2012Inventors: Franck Raeppel, Ljubomir Isakovic, Stephen William Claridge, Michael Mannion, Lijie Zhan, Marie-Claude Granger, Arkadii Vaisburg, Miguel Nantel
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Publication number: 20120083471Abstract: The present invention relates to novel pharmaceutical compositions containing the same, and methods of use for a variety of therapeutically valuable uses including, but not limited to, treating obesity by inhibiting the activity of Glycerol 3-phosphate acyltransferase (GPAT).Type: ApplicationFiled: October 14, 2011Publication date: April 5, 2012Inventors: Craig A. Townsend, Edward Wydysh, Francis Kuhajda, Gabriele Valeria Ronnett
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Publication number: 20120065204Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, ester or stereoisomer thereof, wherein R1 to R3 and X have the significances given herein. The present invention is also directed to processes for making said compounds and uses of said compounds, in particular their use as medicaments, more particularly their use as medicaments in the treatment of cancer.Type: ApplicationFiled: September 7, 2011Publication date: March 15, 2012Inventors: Lei Guo, Guozhi Tang, Zhanguo Wang, Jason Christopher Wong, Weixing Zhang
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Publication number: 20120035139Abstract: Gamma-amino-butyric acid derivatives that are GABAB receptor ligands, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives and pharmaceutical compositions thereof for treating diseases are disclosed.Type: ApplicationFiled: April 16, 2010Publication date: February 9, 2012Inventors: Feng Xu, Mark A. Gallop, Ge Peng, Thu Phan, Usha Dilip, David J. Wustrow
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Publication number: 20120022080Abstract: The present invention provides a novel compound having plasminogen activator inhibitor-1 inhibitory activity, and an inhibitor of PAI-1 comprising the compound as an active ingredient. The present invention also provides a pharmaceutical composition having an inhibitory action on PAI-1 activity and being efficacious in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity.Type: ApplicationFiled: March 31, 2010Publication date: January 26, 2012Applicant: RENASCIENCE CO., LTD.Inventors: Toshio Miyata, Kenji Murano, Nagahisa Yamaoka, Akihisa Maeda
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Publication number: 20110319445Abstract: Described herein are heteroaryl compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the heteroaryl compounds described. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: October 1, 2009Publication date: December 29, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Nicholas Simon Stock, Jeffrey Roger Roppe, Deborah Volkots
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Publication number: 20110312974Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: September 28, 2009Publication date: December 22, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Brian Andrew Stearns, Nicholas Simone Stock, Yen Pham Truong, Jeffrey Roger Roppe, Deborah Volkots, Jill Melissa Scott, Timothy Andrew Parr, Bowei Wang, Thomas Jon Seiders, Ryan Clark, Heather Renee Coate
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Publication number: 20110301196Abstract: The invention provides compounds that are effective as inhibitors of human plasmin and plasma kallikrein, and that are useful for the prevention of blood loss and as components of fibrin adhesives. The invention further provides methods of making and using the compounds.Type: ApplicationFiled: January 28, 2011Publication date: December 8, 2011Applicant: The Medicines Company (Leipzig) GmbHInventors: Peter HEROLD, Mohammed DAGHISH, Stjepan JELAKOVIC, Friedrich-Alexander LUDWIG, Claudia REICHELT, Alexander SCHULZE, Andrea SCHWEINITZ
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Publication number: 20110281872Abstract: The invention relates to compositions and methods for the treatment and prevention of cancer and other cell proliferative disorders.Type: ApplicationFiled: March 11, 2011Publication date: November 17, 2011Applicant: Kinex Pharmaceuticals, LLCInventors: David G. Hangauer, JR., Michael J. Ciesielski, Robert A. Fenstermaker
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Publication number: 20110275678Abstract: The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.Type: ApplicationFiled: June 4, 2009Publication date: November 10, 2011Inventors: Michael Higginbottom, Anne Viet-Anh Horgan (nee Nguyen), James Horton, Iain Simpson, Charles Tyzack
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Publication number: 20110275650Abstract: This invention provides compounds that selectively inhibit monoacylglycerol lipase (MAGL). The invention also provides methods of using the MAGL selective inhibitors to stimulate 2-Arachidonoylglycerol (2-AG) mediated endocannabinoid signaling in vivo, and to treat conditions that are associated with or linked to endocannabinoid signaling. The invention additionally provides methods of treating cancer or inhibiting tumor growth by targeting MAGL with MAGL specific inhibitors. The invention further provides methods of screening for MAGL inhibitors with improved biochemical and pharmaceutical properties.Type: ApplicationFiled: November 10, 2009Publication date: November 10, 2011Applicant: THE SCRIPPS RESEARCH INSTITUTEInventors: Benjamin F. Cravatt, Jonathan Z. Long, Weiwei Li, Daniel K. Nomura
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Publication number: 20110275638Abstract: The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.Type: ApplicationFiled: June 4, 2009Publication date: November 10, 2011Inventors: Emma Chapman, Michael Higginbottom, Anne Viet-Anh Horgan (nee Nguyen), Iain Simpson
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Publication number: 20110269761Abstract: The invention relates to substituted aryl-sulphonylglycine derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as in the specification and claims, which are suitable for preparing a pharmaceutical composition for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.Type: ApplicationFiled: April 17, 2009Publication date: November 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Elke Langkopf, Frank Himmelsbach, Juergen Mack, Alexander Pautsch, Corinna Schoelch, Annette Schuler-Metz, Ruediger Streicher, Holger Wagner
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Publication number: 20110224213Abstract: The invention relates to the use of glutaric acid derivatives of general formula (I), which are disclosed in the invention description, as anti-arrhythmic agents.Type: ApplicationFiled: March 18, 2009Publication date: September 15, 2011Inventors: Vladimir Evgenievich Nebolsin, Dmitry Sergeevich Blinov, Vladimir Pavlovich Balashov, Tatyana Alexandrovna Kromova, Galina Alexandrovna Zheltukhina
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Publication number: 20110178305Abstract: The present invention relates to a process for the preparation of threo-3,4-epoxy-2-amino-1-substituted butane derivatives represented by general Formula I which comprises reacting compound of Formula III or salt thereof with an active ester of acid of Formula IV and treating the product thereof with base. The carbon atom bonded to the radical R3 in Formula I and IV is in the (R)-, (S)- or (R,S)-configuration. The compounds of Formula I and III, particularly in their (2S,3R) configuration are useful intermediates for the preparation of atazanavir bisulfate.Type: ApplicationFiled: May 5, 2009Publication date: July 21, 2011Applicant: RANBAXY LABORATORIES LIMITEDInventors: Rakesh Singh, Prasad Yeragorla, Mahavir Singh Khanna, Mohan Prasad
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Publication number: 20110160252Abstract: First, the present inventors assessed the effect of the compound represented by formula (III) below on Huh-7 cells infected with HBV, and demonstrated that the compound alone had an anti-HBV effect in vitro. Formula (III) Then, the present inventors revealed that the HBV replication-suppressing effect of PEG-IFN is enhanced in chimeric mice having a human liver infected with genotype C or A HBV when PEG-IFN is used in combination with the compound represented by formula (III) above. The present inventors also revealed that the HBV replication-suppressing effect of Entecavir is enhanced in chimeric mice having a human liver infected with genotype C HBV (wild-type and Entecavir-resistant strains) when Entecavir is used in combination with the compound represented by formula (III) above.Type: ApplicationFiled: June 18, 2009Publication date: June 30, 2011Inventors: Masashi Mizokami, Yasuhito Tanaka, Masaya Sugiyama, Masayuki Sudoh
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Publication number: 20110112140Abstract: The present invention relates to a novel compound having plasminogen activator inhibitor-1 (PAI-1) inhibitory activity, and a PAI-1 inhibitor comprising the compound as an active ingredient. The present invention further relates to a pharmaceutical composition that has an inhibitory action on PAI-1 activity and is useful in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity. The novel compound is represented by the following general formula. Each symbol is defined as those in the specification.Type: ApplicationFiled: March 31, 2009Publication date: May 12, 2011Applicant: RENASCIENCE CO., LTD.Inventors: Toshio Miyata, Nagahisa Yamaoka, Hidehiko Kodama, Kenji Murano
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Publication number: 20110105482Abstract: A dual thyrointegrin antagonist and a method for treating an angiogenesis-mediated disorder and/or a hyperthyroidism disorders by introducing the dual thyrointegrin antagonist into animals (e.g., mammals, human beings). The dual thyrointegrin antagonist includes a chemical structure having a thyroid hormone antagonist and ?v?3 integrin antagonist in the same molecule.Type: ApplicationFiled: November 1, 2010Publication date: May 5, 2011Applicant: VASCULAR VISION PHARMACEUTICAL COMPANYInventor: Shaker A. Mousa
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Publication number: 20110098477Abstract: There is provided a convenient and inexpensive method of producing a compound which has a high activity of inhibiting replication of hepatitis C virus (HCV) and is useful for preventing and treating a liver disease caused by HCV infection.Type: ApplicationFiled: June 27, 2006Publication date: April 28, 2011Inventors: Masahiro Aoki, Yoshie Nagahashi, Hideyuki Kato, Tatsuya Ito, Miyako Masubuchi, Toru Okuda
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Patent number: 7928264Abstract: The present invention relates to a compound of the formula [I]: wherein (a), in which —Y—, R4, R5 and R6 are4 R5 each as defined in the description, etc., R1 is hydrogen, halogen, lower alkyl, hydroxy, etc., R2 is hydrogen, lower alkyl or hydroxy(lower)alkyl, R3 is hydrogen or an amino protective group, 20R7 is hydrogen, lower alkyl, cyclo(lower)alkyl, lower R9 alkenyl, —Z—R9 or (b), in which —Z— is —0—, —S—, R9 —SO— or —SO2—, and each R9 is independently hydrogen, lower alkyl, cyclo(lower)alkyl, etc., and R8 is -D-E-R10, in which -D- is —CONHSO2— or —S02NHCO—, E is bond or lower alkylene, and R10 is halogen, cyano, carboxy, etc., or a prodrug thereof or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of ulcer, overactive bladder, and the like.Type: GrantFiled: September 20, 2005Date of Patent: April 19, 2011Assignee: Astellas Pharma Inc.Inventors: Kouji Hattori, Susumu Toda, Kenichi Washizuka, Shinji Ito, Daisuke Tanabe, Takanobu Araki, Minoru Sakurai
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Publication number: 20110061723Abstract: The present invention pertains to an electrode layer comprising a porous film made of oxide semiconductor fine particles sensitized with certain methin dyes. Moreover the present invention pertains to a photoelectric conversion device comprising said electrode layer, a dye sensitized solar cell comprising said photoelectric conversion device and to novel methin dyes.Type: ApplicationFiled: February 26, 2009Publication date: March 17, 2011Applicant: BASF SEInventors: Kazuhiko Kunimoto, Hiroshi Yamamoto, Shinji Nakamichi, Ryuichi Takahashi, Junichi Tanabe
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Publication number: 20110053858Abstract: A novel class of peptide ?-ketoamides useful for selectively inhibiting calpains, selectively inhibiting cysteine proteases, and generally inhibiting all cysteine proteases, having the formula M-AA2-AA1-CO—NH—(CH2)n—R3. Processes for the synthesis of peptidyl ?-ketoamide derivatives.Type: ApplicationFiled: July 16, 2008Publication date: March 3, 2011Inventors: James C. Powers, Jonathan D. Glass, Asli Ovat, Zhaozhao Li
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Patent number: 7893094Abstract: The present invention is directed to the amphiphilic pyridinium compounds, such as for suppressing IL-8 secretion and production. The present invention further provides methods of making and using such compounds for the treatment of the IL-8 related diseases, such as cystic fibrosis.Type: GrantFiled: June 28, 2004Date of Patent: February 22, 2011Assignees: The Henry M. Jackson Foundation for the Advancement of Military Medicine, Inc., National Institutes of Health (NIH)Inventors: Harvey B. Pollard, Kenneth Jacobson
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Publication number: 20110039851Abstract: The invention relates to a compound of formula (I): or a tautomer thereof or a pharmaceutically acceptable salt thereof, wherein R1 to R11, W, X, Y, Z, and n are as defined herein. The invention also relates to methods of using the compounds of formula (I) and compositions thereof to treat various diseases and disorders in a patient. The invention also relates to processes for preparing the compounds of formula (I) and intermediates useful in these processes.Type: ApplicationFiled: October 14, 2008Publication date: February 17, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Kaka Dey, Donghong Amy Gao, Daniel R. Goldberg, Alexander Heim-Riether, John Edward Mangette, Ingo Andreas Mugge, Roger John Snow, Alan David Swinamer, Jiang-Ping Wu, Zhaoming Xiong, Yu Yang
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Publication number: 20110039874Abstract: Disclosed are compounds and compositions that inhibit the action of monoacylglycerol lipase (MGL) and fatty acid amide hydrolase (FAAH), methods of inhibiting MGL and FAAH, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors.Type: ApplicationFiled: April 16, 2010Publication date: February 17, 2011Applicant: Northeastern UniversityInventors: Alexandros Makriyannis, Spyridon P. Nikas, Shakiru O. Alapafuja, Vidyanand G. Shukla
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Publication number: 20100324046Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 24, 2008Publication date: December 23, 2010Inventors: Paul Harrington, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Paul Tempest, Kevin J. Wilson, David J. Witter
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Publication number: 20100324103Abstract: The present application relates to substituted enaminocarbonyl compounds of the formula (I) in which A, B, D, R1 to R3 are each as defined in the description, to processes for preparation thereof and to the use thereof for controlling animal pests.Type: ApplicationFiled: June 17, 2010Publication date: December 23, 2010Applicant: Bayer CropScience AGInventors: Peter Jeschke, Thomas Schenke, Robert Velten, Peter Lümmen, Olga Malsam, Ulrich Görgens, Arnd Voerste
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Publication number: 20100317854Abstract: The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, wherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.Type: ApplicationFiled: August 23, 2010Publication date: December 16, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Cristina Alonso-Alija, Markus Heil, Dietmar Flubacher, Paul Naab, Josef Pernerstorfer, Johannes-Peter Stasch, Frank Wunder, Klaus Dembowsky, Elizabeth Perzborn, Elke Stahl
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Patent number: 7846949Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).Type: GrantFiled: February 11, 2005Date of Patent: December 7, 2010Assignee: IRM LLCInventors: Valentina Molteni, Xiaolin Li, Fang Liang, Juliet Nabakka, Enrique Saez, John Wityak
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Patent number: RE42889Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: April 23, 2007Date of Patent: November 1, 2011Assignee: G.D. Searle LLCInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
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Patent number: RE43372Abstract: Compounds having the general structure: which are useful for the treatment of a variety of diseases and conditions, such as bone disorders.Type: GrantFiled: June 5, 2009Date of Patent: May 8, 2012Assignee: Duke UniversityInventors: Mitchell Anthony deLong, David Lindsey Soper, John August Wos, Biswanath De