Plural Chalcogens Bonded Directly To Ring Carbons Of The Thiazole Ring Patents (Class 548/183)
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Publication number: 20130231604Abstract: Halo-organic heterocyclic compounds are described, in which at least two halogen atoms are bound to a nitrogen-containing heterocyclic terminal moiety of the compound, with at least one of such halogen atoms being iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.Type: ApplicationFiled: March 3, 2012Publication date: September 5, 2013Applicant: NANOQUANTUM SCIENCES, INC.Inventors: Gary W. Jones, Anatoliy L. Tatarets, Leonid D. Patsenker
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Publication number: 20130211095Abstract: The present invention provides novel methods for synthesizing PPAR? sparing compounds, e.g., thiazolidinediones, that are useful for preventing and/or treating metabolic disorders such as diabetes, obesity, hypertension, and inflammatory diseases.Type: ApplicationFiled: April 18, 2011Publication date: August 15, 2013Applicant: Metabolic Solutions Development Company, LLCInventors: Timothy Parker, Robert C. Gadwood, Steven P. Tanis, Scott D. Larsen, James R. Zeller
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Publication number: 20130204008Abstract: The present invention provides novel methods for synthesizing PPAR? sparing compounds, e.g., thiazolidinediones, that are useful for preventing and/or treating metabolic disorders such as diabetes, obesity, hypertension, and inflammatory diseases.Type: ApplicationFiled: August 9, 2011Publication date: August 8, 2013Applicant: Metabolic Solutions Development Company, LLCInventors: Steven P. Tanis, Timothy Parker, Robert C. Gadwood, Gerald D. Artman, III, James R. Zeller
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Publication number: 20130204004Abstract: The present invention provides novel methods for synthesizing PPAR? sparing compounds, e.g., thiazolidinediones, that are useful for preventing and/or treating metabolic disorders such as diabetes, obesity, hypertension, and inflammatory diseases.Type: ApplicationFiled: April 18, 2011Publication date: August 8, 2013Applicant: Metabolic Solutions Development Company, LLCInventors: James R. Zeller, Steven P. Tanis, Scott D. Larsen, Timothy Parker
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Patent number: 8501438Abstract: A method is described for producing protein compositions having reduced amounts of O-linked glycosylation. The method includes producing the protein in cells cultured in the presence of an inhibitor of Pmt-mediated O-linked glycosylation and/or in the presence of one or more ?-1,2-mannosidases.Type: GrantFiled: May 31, 2012Date of Patent: August 6, 2013Assignee: GlycoFi, Inc.Inventors: Piotr Bobrowicz, W. James Cook, Warren Kett
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Publication number: 20130184258Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium 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.Type: ApplicationFiled: October 26, 2012Publication date: July 18, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130177843Abstract: The present invention provides a charge control agent containing, as an active substance(s), one or two or more thiazolidinedione derivatives represented by the following formula (1), where R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, a linear or branched alkyl group having 1 to 8 carbon atoms which may have a substituent, etc.; R3 to R7, which may be identical to or different from each other, represent a hydrogen atom, a chlorine atom, a linear or branched alkyl group having 1 to 8 carbon atoms which may have a substituent, etc., and may be joined to each other to form a ring; and V, W, X, Y and Z represent a carbon atom or a nitrogen atom, and 0 to 3 of any of V, W, X, Y and Z are nitrogen atoms which do not have the substituents of R3 to R7.Type: ApplicationFiled: September 1, 2011Publication date: July 11, 2013Applicant: HODOGAYA CHEMICAL CO., LTD.Inventors: Ikuo Kimura, Motonori Tsuji, Masami Ito, Masaya Tojo, Kanae Hiraishi
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Publication number: 20130177844Abstract: The present invention provides a positive-charge control agent containing, as an active substance(s), one or two or more rhodanine compounds represented by the following formula (1). wherein R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, etc.; and R3 to R7, which may be identical to or different from each other, represent a hydrogen atom, a cyano group, a trifluoromethyl group, a nitro group, etc. R2 to R7 may be joined to each other to form a ring. V, W, X, Y and Z represent a carbon atom or a nitrogen atom and 0 to 3 of V, W, X, Y and Z are nitrogen atoms, with the proviso that at least one of R3 to R7 is a linear or branched alkyl group having 1 to 4 carbon atoms substituted with three or more fluorine atoms etc.Type: ApplicationFiled: November 22, 2011Publication date: July 11, 2013Applicant: HODOGAYA CHEMICAL CO., LTD.Inventors: Masateru Yasumura, Masami Ito, Ikuo Kimura, Masaya Tojo, Kanae Hiraishi, Masaki Okubo
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Patent number: 8476449Abstract: The present invention is a compound represented by the following formula (1) or a salt thereof. Furthermore, the present invention is an imaging agent used for imaging a tau protein, the imaging agent containing a compound represented by the formula (1) below or a salt thereof. In the formula (1), R3 is a radioactive iodine.Type: GrantFiled: February 24, 2011Date of Patent: July 2, 2013Assignees: Nihon Medi-Physics Co., Ltd., Kyoto UniversityInventors: Hideo Saji, Masahiro Ono, Ikuya Seki
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Patent number: 8466177Abstract: Compounds that are useful in treating or preventing viral infections, such as influenza, are described herein. Further described are compositions made from these compounds and methods for using the compounds and their compositions in treating or preventing viral infections.Type: GrantFiled: October 31, 2008Date of Patent: June 18, 2013Assignee: The UAB Research FoundationInventors: Ming Luo, Zhen Yang
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Publication number: 20130096125Abstract: Disclosed are novel rhodanine derivatives which are inhibitory of HIV activity. Also provided are a method for preparing the novel rhodanine derivatives, and a pharmaceutical composition for the prevention or treatment of AIDS containing the rhodanine derivatives as active ingredients. Having high inhibitory activity against HIV, the rhodanine derivatives can be effectively used in the prophylaxis or therapy of AIDS.Type: ApplicationFiled: June 17, 2011Publication date: April 18, 2013Applicant: AVIXGEN INC.Inventors: Ji Chang You, Gyoon Hee Han, Chul Ho Lee, Doo Na Song, Koo Hwan Chung
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Publication number: 20130090339Abstract: Novel 3-N-cycloalkyl-5-substituted-2-thioxothiazolidin-4-one derivatives that are effective for use in treating viral infections are described. Also described are pharmaceutical compositions comprising the 3-N-cycloalkyl-5-substituted-2-thioxothiazolidin-4-one derivatives and methods for using the compounds or compositions.Type: ApplicationFiled: June 17, 2011Publication date: April 11, 2013Applicants: THE UAB RESEARCH FOUNDATION, FUZIANS BIOMEDICALS, INC.Inventors: Guoxin Wang, Ming Luo, Zhen Yang
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Patent number: 8383656Abstract: A method of inhibiting glycolysis in a subject by administering a pharmaceutical composition including a thiazolidinedione derivative to the subject is described. The thiazolidinedione derivatives are effective energy restriction mimetic agents, and can therefore be used to treat or prevent cancer in a subject, treat metabolic disorder, or increase the longevity of a subject. Various thiazolidinedione derivatives are also suitable for activating adenosine phosphate-activated protein kinase or inhibiting IL-6 expression.Type: GrantFiled: October 11, 2010Date of Patent: February 26, 2013Assignee: The Ohio State University Research FoundationInventors: Ching-Shih Chen, Jih-Hwa Guh
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Publication number: 20130028966Abstract: The invention provides compounds represented by the formulae: (I) and (II) where the compounds are useful in treating, for example, viral and/or parasitic infections. Also provided are pharmaceutical compositions comprising the compounds and methods of treatment using the compounds.Type: ApplicationFiled: April 13, 2011Publication date: January 31, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Benhur Lee, Michael E. Jung, Jihye Lee, Frederic Vigant, Peter J. Bradley, Michael C. Wolf, Bettina E. Hajagos
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Patent number: 8357709Abstract: The present invention is directed to 2,4-disubstituted pyrrolidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: GrantFiled: October 15, 2009Date of Patent: January 22, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Paul J. Coleman, Christopher D. Cox, John D. Schreier
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Patent number: 8344009Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: GrantFiled: October 7, 2010Date of Patent: January 1, 2013Assignee: Janssen Pharmaceutica, NVInventors: Michael Gaul, Alexander Kim, Lily Lee Searle, Raymond Patch, Dionisois Rentzeperis, Guozhang Xu, Xizhen Zhu
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Publication number: 20120330024Abstract: The present invention is a compound represented by the following formula (1) or a salt thereof. Furthermore, the present invention is an imaging agent used for imaging a tau protein, the imaging agent containing a compound represented by the formula (1) below or a salt thereof. In the formula (1), R3 is a radioactive iodine.Type: ApplicationFiled: February 24, 2011Publication date: December 27, 2012Applicants: Kyoto University, Nihon Medi-Physics Co., Ltd.Inventors: Hideo Saji, Masahiro Ono, Ikuya Seki
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Patent number: 8338465Abstract: Disclosed are methods for the prevention or treatment of tuberculosis in a subject infected with Mycobacterium tuberculosis by administering rhodanine derivatives of formula (I), as well as some novel such compounds. Other embodiments are also disclosed.Type: GrantFiled: June 8, 2007Date of Patent: December 25, 2012Assignee: Cornell Research Foundation, Inc.Inventors: Jasbir Singh, Carl F. Nathan, Ruslana Bryk, Raghu Samy, Krzysztof Pupek, Mark Gurney
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Patent number: 8338466Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: GrantFiled: January 18, 2010Date of Patent: December 25, 2012Assignee: Abbott LaboratoriesInventors: Aaron R. Kunzer, Steven W. Elmore, Laura A. Hexamer, Cheol-Min Park, Andrew J. Souers, Gerard M. Sullivan, Gary T. Wang, Xilu Wang, Michael D. Wendt
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Publication number: 20120315576Abstract: The present invention provides a charge control agent containing, as an active substance(s), one or two or more rhodanine compounds represented by the following formula (1). where R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, a linear or branched alkyl group having 1 to 8 carbon atoms which may have a substituent, a substituted or unsubstituted heterocyclic group, etc.; R3 to R7, which may be identical to or different from each other, represent a hydrogen atom, a linear or branched alkyl group having 1 to 10 carbon atoms which may have a substituent, a linear or branched alkyloxy group having 1 to 20 carbon atoms which may have a substituent, etc., and may be joined to each other to form a ring; and V, W, X, Y and Z represent a carbon atom or a nitrogen atom, and 0 to 3 of any of V, W, X, Y and Z are nitrogen atoms which do not have the substituents of R3 to R7.Type: ApplicationFiled: February 21, 2011Publication date: December 13, 2012Applicant: HODOGAYA CHEMICAL CO., LTD.Inventors: Masateru Yasumura, Masami Ito, Masaya Tojo, Kanae Hiraishi, Masaki Okubo, Hideyuki Otsuka
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Publication number: 20120309975Abstract: The present invention relates to novel salts of thiazolidinediones and other pharmaceutical agents that are useful for treating and/or preventing metabolic diseases (e.g., diabetes, or neurodegenerative diseases (e.g., Alzheimer's Disease).Type: ApplicationFiled: December 15, 2010Publication date: December 6, 2012Applicant: Metabolic Solutions Development Company LLCInventors: Gerard R. Colca, Steven P. Tanis, Scott D. Larsen
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Patent number: 8309325Abstract: Compounds and methods are described for producing protein compositions having reduced amounts of O-linked glycosylation. The method includes producing the protein in cells cultured in the presence of certain benzylidene thiazolidinediones inhibitors of Pmt-mediated O-linked glycosylation.Type: GrantFiled: May 18, 2009Date of Patent: November 13, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Ranjit Desai, Lihu Yang
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Patent number: 8304441Abstract: The present invention relates to thiazolidinedione analogues that are useful for treating hypertension, diabetes, and inflammatory diseases.Type: GrantFiled: November 16, 2011Date of Patent: November 6, 2012Assignee: Metabolic Solutions Development Company, LLCInventors: Gerard R. Colca, Robert C. Gadwood, Tim Parker
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Publication number: 20120238759Abstract: A method for manufacturing a 6-substituted 1-methyl-1H-benzimidazole derivative represented by the formula (IV) wherein R3 represents a hydrogen atom or a C1-C4 alkyl group. A 4-substituted N2-methylbenzene-1,2-diamine derivative is prepared from a particular 5-substituted N-methyl-2-nitroaniline derivative, subsequently reacting the resulting compound with {4-[(2,4-dioxo-1,3-thiazolidin-5-yl)methyl]phenoxy}acetic acid or an acid chloride or a mixed acid anhydride thereof, and subsequently subjecting the resulting compound to intramolecular dehydration condensation. A compound of the formula (II) wherein R1 represents a hydrogen atom, a C1-C4 alkyl group, or a protective group for the nitrogen atom, and R2 represents a hydrogen atom or a protective group for the nitrogen atom is prepared and used as an intermediate.Type: ApplicationFiled: November 25, 2010Publication date: September 20, 2012Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Yutaka Ikeuchi, Chiharu Satoh, Eiji Numagami, Satoru Nihei, Hisaki Kajino
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Patent number: 8268816Abstract: The application describes an assay for the identification of small molecule modulators of integrin CD11b/CD18 and small molecules capable of modulating activity of this receptor. For example, one such compound useful as an agonist of integrin CD11b/CD18 is the compound of Formula (I): Such compounds may be used in certain embodiments for treating a disease or condition selected from inflammation, immune-related disorders, cancer, ischemia-reperfusion injury, stroke, neointimal thickening associated with vascular injury, bullous pemphigoid, neonatal obstructive nephropathy, and cardiovascular disease, or in other embodiments for the treatment of a disease or condition selected from immune deficiency, acquired immune deficiency syndrome (AIDS), myeloperoxidase deficiency, Wiskott-Aldrich syndrome, chronic granulomatous disease, hyper-IgM syndromes, leukocyte adhesion deficiency, Chediak-Higashi syndrome, and severe combined immunodeficiency.Type: GrantFiled: June 19, 2009Date of Patent: September 18, 2012Inventors: Vineet Gupta, M. Amin Arnaout
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Publication number: 20120219613Abstract: Provided herein are a series of arylmethylidene rhodanine derivatives having broad-spectrum antiviral activity against enveloped viruses, including but not limited to filoviruses, poxviruses, arenaviruses, bunyaviruses, paramyxoviruses, flaviviruses, influenza A, and HIV-1. The compounds act via a novel mechanism to disrupt viral membranes and inhibit viral attachment, fusion, and/or entry into host cells. The membrane disrupting activity of the compounds is selective for viral membranes relative to other biological membranes, making the compounds non-toxic to cells and host subjects.Type: ApplicationFiled: June 18, 2009Publication date: August 30, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Benhur Lee, Michael E. Jung, Michael C. Wolf, Tinghu Zhang
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Publication number: 20120202814Abstract: The present invention relates to the medical use of the compound of formula 1, 2, 3 or 4:Type: ApplicationFiled: October 4, 2010Publication date: August 9, 2012Applicants: UNIVERSITร DEGLI STUDI DI SIENA, CONSIGLIO NAZIONALE DELLE RICERCHEInventors: Marco Radi, Maurizio Botta, Federico Falchi, Giovanni Maga, Fausto Baldanti, Stefania Paolucci
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Patent number: 8236834Abstract: It is an object of the present invention to provide the crystalline form of a thiazolidinedione compound, which is effective as a pharmaceutical ingredient for manufacturing a peroxisome proliferator-activated receptor (PPAR) activator and an anticancer pharmaceutical composition. The present invention relates to a crystalline form of a hydrate of 5-(4-{[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H-benzimidazol-2-yl]methoxy}benzyl)-1,3-thiazolidine-2,4-dione dihydrochloride represented by the following formula (I).Type: GrantFiled: February 8, 2008Date of Patent: August 7, 2012Assignee: Daiichi Sankyo Company, LimitedInventors: Hisaki Kajino, Yutaka Ikeuchi, Eiji Numagami
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Patent number: 8206949Abstract: A method is described for producing protein compositions having reduced amounts of O-linked glycosylation. The method includes producing the protein in cells cultured in the presence of an inhibitor of Pmt-mediated O-linked glycosylation and/or in the presence of one or more ?-1,2-mannosidases.Type: GrantFiled: November 10, 2006Date of Patent: June 26, 2012Assignee: GlycoFi, Inc.Inventors: Piotr Bobrowicz, W. James Cook, Warren Kett
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Publication number: 20120149710Abstract: Bacterial infections, including Methicillin resistant Staphylococcus aureus (MRSA) infections are a major health problem that has created a pressing need for new antibiotics. Pyridazinone, rhodanine, and pyrazolethione compounds effective inhibit the enzymatic activity of sortase A (srtA) found in gram positive bacteria are disclosed. A structure activity relationship (SAR) analysis led to the identification of several pyridazinone and pyrazolethione analogs that inhibit SrtA with IC50 values in the sub-micromolar range. Compounds that inhibit the S. aureus SrtA sortase may function as potent anti-infective agents as this enzyme attaches virulence factors to the cell wall. Many of these molecules also inhibit the sortase enzyme from B. anthracis suggesting that they may be generalized sortase inhibitors. The novel compounds, compositions, uses, formulations, medicaments, articles of manufacture provide improved materials, uses, and treatments useful in combating infectious disorders.Type: ApplicationFiled: August 23, 2010Publication date: June 14, 2012Inventors: Michael E. Jung, Robert T. Clubb, Sung Wook Yi, Nutee Suree, Jeremy Justin Clemens
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Patent number: 8188080Abstract: Disclosed herein are Vaccinia H1-related (VHR) protein tyrosine phosphatase (PTP) inhibitors that provide a method for treating cancer.Type: GrantFiled: October 17, 2008Date of Patent: May 29, 2012Assignee: Sanford-Burnham Medical Research InstituteInventors: Tomas Mustelin, Lutz Tautz
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Publication number: 20120088783Abstract: The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I wherein the substituents are as defined in the specification. They are useful in the treatment of disorders mediated by lipoxygenase, such as immune diseases, respiratory diseases and cardiovascular diseases, as well as in the treatment of neurodegenerative disorders and/or mitochondria) disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.Type: ApplicationFiled: September 26, 2011Publication date: April 12, 2012Applicant: Ampere Life Sciences, Inc.Inventors: Bing WANG, Gail Walkinshaw, Donald R. James
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Publication number: 20120088759Abstract: The present invention relates to thiazolidin-4-one and [1,3]-thiazinan-4-one compounds of formula (I) wherein X, Y, R3 and R4 are as described in the description, or pharmaceutically acceptable salts thereof, for the prevention or treatment of diseases related to the orexin system. The present invention also relates to novel thiazolidin-4-one compounds of formula (II) and their use as pharmaceuticals, pharmaceutical compositions containing one or more compounds of formula (II), and especially their use as orexin receptor antagonists.Type: ApplicationFiled: May 11, 2010Publication date: April 12, 2012Inventors: Hamed Aissaoui, Christoph Boss, Christine Brotschi, Markus Gude, John Gatfield, Romain Siegrist, Thierry Sifferlen, Jodi T. Williams
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Patent number: 8148541Abstract: Disclosed herein are rhodanine derivatives, a method for the preparation thereof, and a pharmaceutical composition containing the same. The rhodanine derivatives have inhibitory activity against protein phosphatases (PPase) such as PTP1B, Prl-3, LAR, CD45, Cdc25A, Cdc25B, Cdc25C, Yop, PP1 and VHR, and can be applied for the prevention and treatment of PPase-caused diseases, including autoimmune diseases, diabetes, impaired glucose intolerance, insulin resistance, obesity, cancers, etc. when the inhibitory activity thereof is modulated.Type: GrantFiled: December 8, 2006Date of Patent: April 3, 2012Assignee: Korea Research Institute of Bioscience and BiotechnologyInventors: Seong Eon Ryu, Seung Jun Kim, Dae Gwin Jeong, Sang Hyeup Lee, Suk Kyeong Jung, Hwan Mook Kim, Song Kyu Park, Ki Ho Lee, Chang Woo Lee, Joong-Kwon Choi, Jin Hee Ahn
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Publication number: 20120070511Abstract: Compositions which modulate mitochondrial functions treat diseases associated with cells that are hyperactively using their endoplasmic reticulum. Screening assays identify agents which modulate mitochondrial functions.Type: ApplicationFiled: September 21, 2011Publication date: March 22, 2012Applicant: UNIVERSITY OF MIAMIInventors: Theodore Lampidis, Metin Kurtoglu
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Patent number: 8119669Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: GrantFiled: March 6, 2008Date of Patent: February 21, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Michael Gaul, Lily Lee Searle, Dionisios Rentzeperis
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Patent number: 8106079Abstract: A compound having the following formula (III) wherein R2 is hydrogen, alkyl, cycloalkyl, phenyl or a 5- or 6-membered heterocyclic, and X is oxygen, sulfur or nitrogen, and a method for preparing said compound.Type: GrantFiled: May 19, 2010Date of Patent: January 31, 2012Assignee: Sankyo Company, LimitedInventors: Hisaki Kajino, Hiroshi Miyamoto, Yutaka Ikeuchi
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Publication number: 20120022086Abstract: Novel compounds, compositions, and methods related to the activation of the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing a catecholamine backbone and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods, compositions, and compounds for the treatment of disorders including neurological disorders, neuropsychiatric disorders, and metabolic disorders are provided. For example, a first method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes administering to the subject a therapeutically effective amount of the described compounds. A further method of promoting neuroprotection in a subject also is provided, which includes administering to the subject a therapeutically effective amount of the described compounds.Type: ApplicationFiled: March 17, 2010Publication date: January 26, 2012Applicant: EMORY UNIVERSITYInventor: Keqiang Ye
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Publication number: 20120010255Abstract: The application describes small molecules capable of modulating activity of beta2 family of integrins, such as integrin CD11b/CD18 (also known as Mac-1, CR3 and ?M?2). Such compounds may be used in certain embodiments for treating a disease or condition, such as inflammation, immune-related disorders, cancer, ischemia-reperfusion injury, stroke, neointimal thickening associated with vascular injury, wound-healing, organ transplantation and cardiovascular disease, among others.Type: ApplicationFiled: October 14, 2010Publication date: January 12, 2012Inventor: Vineet Gupta
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Publication number: 20120004271Abstract: Use of vaginal insulin sensitising agents for the prevention and/or treatment of hyperandrogenism and/or polycystic ovary syndrome and/or related disorders.Type: ApplicationFiled: February 16, 2010Publication date: January 5, 2012Inventors: Jaime Moscoso Del Prado, Beatriz Bandi Tosi
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Publication number: 20110319455Abstract: A method of treating or preventing fungal infection, which includes identifying a plant or animal having a fungal infection and administering an effective amount of an anti-fungal composition to the plant or animal to reduce the fungal infection. In a preferred form of the present invention, the antifungal composition is compound 13 or 33 and is combined with an azole compound, such as fluconazole.Type: ApplicationFiled: April 19, 2011Publication date: December 29, 2011Inventors: Bruce Steven Klein, Brad Mark Tebbets
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Publication number: 20110312967Abstract: This invention provides for certain bridged and fused compounds of the formula G-L-A I or a pharmaceutically acceptable salt, ester of solvate thereof wherein: A is: (I) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.Type: ApplicationFiled: January 21, 2010Publication date: December 22, 2011Applicant: Schering CorporationInventors: Hubert B. Josien, John W. Clader, William J. Greenlee, Michael John Mayer, Jason L. Davis, Shuangyi Wan
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Publication number: 20110313008Abstract: This invention provides for certain pentafluorosulpholane-containing compounds of the formula or a pharmaceutically acceptable salt, ester, solvate or prodrug thereof, wherein the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.Type: ApplicationFiled: January 21, 2010Publication date: December 22, 2011Applicant: Schering CorporationInventors: Hubert B. Josien, John W. Clader, Andrew Stamford, William J. Greenlee, Michael John Mayer, Jason L. Davis, Ming Min Hsia, Shuangyi Wan
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Patent number: 8067450Abstract: The present invention relates to thiazolidinedione analogues that are useful for treating hypertension, diabetes, and inflammatory diseases. Formula (I), wherein: each of R1 and R4 is independently selected from H, halo, aliphatic, and alkoxy, wherein the aliphatic and alkoxy are optionally substituted with 1-3 of halo; R2 is halo, hydroxy, or optionally substituted aliphatic, and R?2 is H, or R2 and R?2 together form oxo; R3 is H; and Ring A is a phenyl.Type: GrantFiled: September 15, 2008Date of Patent: November 29, 2011Assignee: Metabolic Solutions Development CompanyInventors: Gerard R. Colca, Robert C. Gadwood, Tim Parker
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Publication number: 20110281921Abstract: Novel agents exhibiting anti-biofilm formation activity while being non-cytotoxic are provided, as well as methods of using the same, either per se or conjugated to a polymer, for preventing and/or reducing the formation of microbial biofilms and/or for disrupting microbial biofilms. The novel agents described herein include thiazolidine-2,4-diones (TZDs), pyrrolidine-2,5-diones (PYDs), imidazolidine-2,4-diones or oxazolidine-2,4-diones, substituted by an alkyl having 7-20 carbon atoms in its backbone chain.Type: ApplicationFiled: November 19, 2009Publication date: November 17, 2011Applicants: Hadasit Medical Research Services and Development Ltd., Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.Inventors: Morris Srebnik, Itzhack Polacheck, Doron Steinberg, Adel Jabbour, Edward Sionov
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Patent number: 8058295Abstract: The invention provides compositions, pharmaceutical preparations and methods for inhibition of cystic fibrosis transmembrane conductance regulator protein (CFTR) that are useful for the study and treatment of CFTR-mediated diseases and conditions. The compositions and pharmaceutical preparations of the invention may comprise one or more thiazolidinone compounds, and may additionally comprise one or more pharmaceutically acceptable carriers, excipients and/or adjuvants. The methods of the invention comprise, in certain embodiments, administering to a patient suffering from a CFTR-mediated disease or condition, an efficacious amount of a thiazolidinone compound. In other embodiments the invention provides methods of inhibiting CFTR that comprise contacting cells in a subject with an effective amount of a thiazolidinone compound.Type: GrantFiled: November 19, 2009Date of Patent: November 15, 2011Assignee: The Regents of the University of CaliforniaInventors: Alan Verkman, Tonghui Ma
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Publication number: 20110275681Abstract: The invention relates to novel crystalline salts of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid and a novel betaine cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel crystalline salts and cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel crystalline salts and cocrystal and the therapeutic use of the novel crystalline salts and cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, inhibiting aldose reductase, and affording cardioprotection in patients who may be non-diabetic.Type: ApplicationFiled: January 25, 2011Publication date: November 10, 2011Inventors: Isabel Kalofonos, G. Patrick Stahly, William Martin-Doyle, Dimitris Kalofonos, Jeffrey S. Stults, Travis L. Houston
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Publication number: 20110275682Abstract: The invention relates to a novel choline cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel choline cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel choline cocrystal and the therapeutic use of the novel choline cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, treating and/or preventing homocystinuria reducing levels of homocysteine in blood serum, inhibiting aldose reductase, and affording cardioprotection in non-diabetic patients.Type: ApplicationFiled: September 3, 2009Publication date: November 10, 2011Applicant: BioNevia PhArmaceuticals, Inc.Inventors: Isabel Kalofonos, Patrick G. Stahly, William Martin-Doyle, Dimitris Kalofonos, Travis L. Houston, Jeffrey S. Stults
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Publication number: 20110269954Abstract: The present invention relates to novel thiazolidinedione derivatives expressed by the following formula (I) and the uses thereof. More specifically, the present invention relates to novel thiazolidinedione derivatives expressed by the following formula (I) and a pharmaceutical composition comprising the same. The novel thiazolidinedione derivatives of formula (I) according to the present invention can be effectively used for the prevention or treatment of cardiovascular disease, gastrointestinal disease and renal disease by inhibiting the activity of 15-hydroxyprostaglandin dehydrogenase (15-PGDH) that decomposes prostaglandins as well as useful for the prevention of hair loss and the stimulation of hair growth, and osteogenic stimulation and wound healing.Type: ApplicationFiled: December 30, 2009Publication date: November 3, 2011Inventors: Hoon Cho, Ying Wu, Cheol-Hee Choi
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Publication number: 20110263664Abstract: The disclosure relates to inhibitors of Pim-1 and/or Pim-2 protein kinase, to compositions comprising one or more inhibitors of Pim-1 and/or Pim-2 protein kinase, and to methods for treating cancer.Type: ApplicationFiled: November 14, 2008Publication date: October 27, 2011Applicant: MUSC FOUNDATION FOR RESEARCH DEVELOPMENTInventors: Charles D. Smith, Andrews S. Kraft