Plural Chalcogens Bonded Directly To Ring Carbons Of The Thiazole Ring Patents (Class 548/183)
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Publication number: 20110224207Abstract: Methods of treating, preventing, and/or ameliorating a Flavivirus infection in a subject are disclosed. The methods comprise administering to the subject a therapeutically effective amount of a Flavivirus inhibitor, e.g., a Flavivirus serine protease inhibitor. These methods are useful in treating, preventing, and/or ameliorating Flavivurs infections such as, for example, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus.Type: ApplicationFiled: September 23, 2009Publication date: September 15, 2011Applicant: GEORGETOWN UNIVERSITYInventors: Radhakrishnan Padmanabhan, Nagarajan Pattabiraman, Niklaus Mueller, Kuppuswamy Nagarajan
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Publication number: 20110218182Abstract: The invention relates to chemical compounds of formula (I), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of PIM-1 and/or PIM-2, and/or PIM-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of PIM kinase related conditions and diseases, preferably cancer.Type: ApplicationFiled: July 2, 2009Publication date: September 8, 2011Applicant: ASTRAZENECA ABInventors: Leslie Dakin, James Edward Dowling, Michelle Lamb, Jon Read, Qibin Su, Xiaolan Zheng
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Publication number: 20110178102Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: ApplicationFiled: June 30, 2004Publication date: July 21, 2011Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITYInventors: Vern L Schramm, Anthony A. Suave
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Publication number: 20110172414Abstract: A pesticide, particularly an insecticide or an acaricide, including a substituted isoxazoline compound of formula (1) or a salt thereof: wherein A1, A2 and A3 independently of one another are carbon atom or nitrogen atom, G is benzene ring, etc., L is —N(R2c)—, or —CH(R2a)N(R2c)—, etc., X is halogen atom, C1-C6 haloalkyl, etc., Y is halogen atom, C1-C6alkyl, etc., R1 is —C(O)R1a, —C(O)OR1a, —C(O)NHR1a, etc., R2 is hydrogen atom, C1-C6haloalkyl, —C1-C4alkoxy C1-C4alkyl, cyano C1-C6alkyl, C3-C6alkenyl, C3-C6alkynyl, —C(O)R15, —C(O)OR15, etc., R3 is C1-C6haloalkyl, etc., m is an integer of 0 to 5, n is an integer of 0 to 4. The pesticide containing these compounds.Type: ApplicationFiled: March 28, 2011Publication date: July 14, 2011Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Takeshi MITA, Kazushige MAEDA, Mitsuaki KOMODA, Eitatsu IKEDA, Ken-ichi TOYAMA, Motoyoshi IWASA
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Publication number: 20110166191Abstract: 3-(2-amino-ethyl)-5-(3-cyclohexyl-propylidene)-thiazolidine-2,4-dione and derivatives thereof are provided for use as dual inhibitors of the Raf/MEK/ERK and PI3K/Akt pathways and for use in the treatment of cancer.Type: ApplicationFiled: January 5, 2011Publication date: July 7, 2011Inventors: Shijun Zhang, Tai Liang Guo
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Patent number: 7973062Abstract: Compounds of the thiazolidinedione family are provided and shown to be effective androgen receptor ablative agents that can be used in methods of treating or preventing cancer or precancer, including prostate cancer. Also provided are methods of treating or preventing cancer by administering a therapeutically effective amount of one of the androgen receptor ablative agents to a subject in need of such treatment.Type: GrantFiled: February 20, 2009Date of Patent: July 5, 2011Assignee: The Ohio State University Research FoundationInventors: Ching-Shih Chen, Dasheng Wang, Jian Yang
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Publication number: 20110160462Abstract: Thiazolidinedione compound crystalline forms useful as a bulk material for the manufacture of a peroxisome proliferator-activated receptor (PPAR) ? activator or an anticancer pharmaceutical composition are provided, which are hydrate crystalline forms of 5-(4-{[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H-benzimi dazol-2-yl]methoxy}benzyl)-1,3-thiazolidine-2,4-dione represented by Formula (I) below and of its dihydrochloride.Type: ApplicationFiled: July 30, 2009Publication date: June 30, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Hisaki Kajino, Eiji Numagami, Satoru Nihei
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Patent number: 7947717Abstract: The invention provides compounds that can efficiently and specifically inhibit bacterial toxins, such as inhibit the lethal factor (LF) protease activity of anthrax toxin and/or botulinum neurotoxin type A. The invention also provides methods for inhibiting proteases, such as lethal factor protease, as well as methods for treating bacterial infections, such as anthrax and botulinum.Type: GrantFiled: July 18, 2008Date of Patent: May 24, 2011Assignee: Burnham Institute for Medical ResearchInventor: Maurizio Pellecchia
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Publication number: 20110112098Abstract: The present invention relates to the C-13 molecule (methyl 2-{5-[(3-benzyl-4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]-2-furyl}-benzoate) and to organic molecules functionally equivalent to the C-13 molecule, capable of inhibiting the binding of an antibody or antibody fragment with the human Syk protein tyrosine kinase, to the use of these molecules for the production of medicaments for the prevention or treatment of diseases dependent on metabolic pathways involving Syk, and also to a method for identifying such molecules.Type: ApplicationFiled: April 8, 2009Publication date: May 12, 2011Inventors: Piona Dariavach, Pierre Emile Ulysse Martineau, Bruno Villoutreix
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Publication number: 20110105565Abstract: Provided herein are highly water soluble, thiazolidinone derivative compounds and glycine hydrazide derivative compounds that inhibit the ion transport activity of the cystic fibrosis transmembrane conductance regulator (CFTR). The compounds, and compositions comprising the compounds, described herein are useful for treating diseases, disorders, and sequelae of diseases, disorders, and conditions that are associated with aberrantly increased CFTR activity, for example, secretory diarrhea. The compounds may also be used for inhibiting expansion or preventing formation of cysts in persons who have polycystic kidney disease.Type: ApplicationFiled: March 25, 2009Publication date: May 5, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Alan S. Verkman, Nitin D. Sonawane
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Publication number: 20110092555Abstract: A compound which is 5-{4-[(6-methoxy-1-methyl-1H-benzimidazol-2-yl)methoxy]benzyl}thiazolidine-2,4-dione hydrochloride, in crystal form wherein a powder x-ray diffraction pattern obtained by irradiation with a Cu K? line shows main peaks at interplanar spacings d=14.29, 7.12, 5.34, 4.97, 4.74, 3.95, 3.85, 3.75, 3.55, 3.51, 3.15, 2.84, 2.76, 2.52 and 2.37.Type: ApplicationFiled: December 14, 2010Publication date: April 21, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Yoshitaka Nakamura, Chiharu Satoh, Hiroshi Miyamoto, Hisaki Kajino
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Publication number: 20110092524Abstract: The invention relates to a pharmacological action of a compound which functions as a PPAR? agonist on the barrier function of the corneal epithelium. A PPAR? agonist such as rivoglitazone, DRF-2593, GW-544 or BMS-298585 exhibits an excellent effect of enhancing the corneal epithelial barrier function in a test for enhancement of corneal epithelial barrier function, and therefore is useful as a preventive agent or a therapeutic agent for ocular infection or ocular unidentified complaint caused by a decrease in the corneal epithelial barrier function. Further, the PPAR? agonist can enhance the corneal epithelial barrier function of diabetic patients, patients with decreased corneal epithelial barrier function due to aging and patients who underwent refractive surgery such as PRK (photorefractive keratectomy) or LASIK (laser in situ keratomileusis) or cataract surgery.Type: ApplicationFiled: February 25, 2009Publication date: April 21, 2011Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Shin-ichiro Hirai, Atsushi Yoshida
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Publication number: 20110076721Abstract: 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 thiazolidine-diones inhibitors of Pmt-mediated O-linked glycosylation.Type: ApplicationFiled: May 18, 2009Publication date: March 31, 2011Applicant: Merck Sharp & Dohme Corp.Inventors: Ranjit Desai, Lihu Yang
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Publication number: 20110014250Abstract: Inhibitors of 15-hydroxyprostaglandin dehydrogenase (15-PGDH), for example tetrazole, styrylpyrazole, phenylfuran, phenylthiophene, phenylpyrrazole, pyrazolecarboxamide, 2-thioacetamide and azo compounds, are useful for promoting or stimulating pigmentation of the skin and/or skin appendages and/or for preventing and/or for limiting depigmentation and/or whitening of the skin and/or skin appendages, notably for preventing and/or limiting canities.Type: ApplicationFiled: February 17, 2010Publication date: January 20, 2011Applicant: L'OREALInventors: JEAN-FRANCOIS MICHELET, STEPHANE COMMO
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Patent number: 7872027Abstract: Compounds and compositions for interfering with the association of Myc and Max are described herein. These compounds and compositions are useful in methods inhibiting growth or proliferation of a cell. Methods of inhibiting growth or proliferation of a cell are provided, comprising contacting the cell with an amount of a compound that interferes with Myc and Max association effective to inhibit growth or proliferation of the cell.Type: GrantFiled: February 16, 2007Date of Patent: January 18, 2011Assignees: University of Pittsburgh - Of the Commonwealth System of Higher Education, Georgetown UniversityInventors: Steven J. Metallo, Edward V. Prochownik
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Publication number: 20110009384Abstract: The present invention provides an agent for the prophylaxis or treatment of diabetes, which has a superior hypoglycemic action, and is associated with a fewer side effects such as body weight gain and the like. The resent invention relates an agent for the prophylaxis or treatment of diabetes, which comprises a compound represented by wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof.Type: ApplicationFiled: February 5, 2008Publication date: January 13, 2011Inventors: Taisuke Tawaraishi, Hiroshi Imoto, Nobuo Cho
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Publication number: 20110003828Abstract: The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.Type: ApplicationFiled: June 24, 2010Publication date: January 6, 2011Inventors: Laura Cook Blumberg, Julius F. Remenar, Örn Almarsson, Tarek A. Zeidan
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Publication number: 20100331315Abstract: The invention provides compounds that inhibit PIM kinases and/or CK2, and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, vascular disorders, pathogenic infections and certain immunological disorders.Type: ApplicationFiled: June 18, 2010Publication date: December 30, 2010Inventors: Mustapha HADDACH, David M. RYCKMAN
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Patent number: 7846953Abstract: 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: December 7, 2010Assignee: Janssen Pharmaceutica, NVInventors: Michael Gaul, Alexander Kim, Lily Lee Searle, Raymond Patch, Dionisois Rentzeperis, Guozhang Xu, Xizhen Zhu
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Patent number: 7846925Abstract: The present invention is related to azolidinedione-vinyl fused-benzene derivatives of formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, graft rejection or lung injuries. Formula (I), wherein A, X, Y, Z, R1, R2 and n are as described in the description.Type: GrantFiled: July 10, 2003Date of Patent: December 7, 2010Assignee: Merck Serono SAInventors: Thomas Rueckle, Xuliang Jiang, Pascale Gaillard, Dennis Church, Tania Grippi Vallotton
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Publication number: 20100305174Abstract: The present invention relates to novel heterocyclic derivatives of formula (I) and their pharmaceutically acceptable salts, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts, their pharmaceutical compositions, and their prodrugs thereof. The present invention more particularly provides novel compounds of the general formula (1).Type: ApplicationFiled: April 12, 2006Publication date: December 2, 2010Applicant: ORCHID RESEARCH LABORATORIES LIMITEDInventors: Surendrakumar Satyanarayan Pandey, Gadam Om Reddy, Shiv Kumar Agarwal, Gajendra Singh, Santhanagopalan Chithra, Debendranath Dey, Abhijeet Nag, Kadnur Venkatachalapathi Sanjay
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Patent number: 7842706Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: March 20, 2009Date of Patent: November 30, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Publication number: 20100298390Abstract: The present invention provides compounds that efficiently and specifically inhibit lethal factor (LF) protease activity of anthrax toxin.Type: ApplicationFiled: February 3, 2010Publication date: November 25, 2010Applicant: Burnham Institute for Medical ResearchInventors: Maurizio Pellecchia, Alex Strongin
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Publication number: 20100298168Abstract: Capture compounds and collections thereof and methods using the compounds for the analysis of biomolecules are provided. In particular, collections, compounds and methods are provided for analyzing complex protein mixtures, such as the proteome. The compounds are multifunctional reagents that provide for the separation and isolation of complex protein mixtures. Automated systems for performing the methods also are provided.Type: ApplicationFiled: April 7, 2010Publication date: November 25, 2010Inventors: Hubert Köster, Daniel Paul Little, Suhaib Mahmood Siddiqi, Matthew Peter Grealish, Subramanian Marappan, Chester Frederick Hassman, III
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Publication number: 20100286212Abstract: 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: ApplicationFiled: October 31, 2008Publication date: November 11, 2010Applicant: THE UAB RESEARCH FOUNDATIONInventors: Ming Luo, Zhen Yang
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Publication number: 20100247468Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.Type: ApplicationFiled: September 21, 2009Publication date: September 30, 2010Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Laurence Clary, Etienne Thoreau, Michel Rivier, Jerome Aubert, Laurent Chantalat, Johannes Voegel
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Publication number: 20100234612Abstract: 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: ApplicationFiled: May 19, 2010Publication date: September 16, 2010Applicant: SANKYO COMPANY, LIMITEDInventors: Hisaki Kajino, Hiroshi Miyamoto, Yutaka Ikeuchi
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Publication number: 20100222596Abstract: A kind of organic compound and organic dye used in dye-sensitized solar cell thereof. In the present invention, we synthesize a series of novel organic compounds with the structure of donor-conjugated chain-acceptor (D-?-A). The electron donor and acceptor groups, for example, are arylamine and cyanoacrylic acid, respectively. These novel organic compounds can be applied to the material of dye layer in the dye-sensitized solar cell (DSSC).Type: ApplicationFiled: February 9, 2010Publication date: September 2, 2010Applicant: National Taipei University of TechnologyInventors: Shu-Mei Chang, Yu-Cheng Chang, Chi-Ming Lan
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Publication number: 20100222399Abstract: 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: ApplicationFiled: September 15, 2008Publication date: September 2, 2010Inventors: Gerard R. Colca, Robert C. Gadwood, Tim Parker
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Publication number: 20100216853Abstract: The present invention relates to a method for identifying compounds that modulate the activity of p300/CBP. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the newly identified lysine-CoA inhibitor binding site, L1 loop, electronegative pocket, or electronegative groove of the HAT domain of p300/CBP and testing the compound for its ability to modulate the activity of p300/CBP. Compositions and methods for preventing or treating diseases or disorders associated with p300/CBP are also provided as is a method for producing a semi-synthetic HAT domain.Type: ApplicationFiled: June 19, 2008Publication date: August 26, 2010Inventors: Ronen Marmorstein, Xin Liu, Philip A. Cole, Ling Wang, Erin M. Bowers, David J. Meyers, Chandrani Mukherjee
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Patent number: 7781464Abstract: The present invention relates to novel heterocyclic diphenyl ether and diphenyl amine compounds, derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and pharmaceutically acceptable solvates thereof and pharmaceutically acceptable compositions containing these singly or in combination. The compounds of the present invention are effective in lowering blood glucose, serum insulin, free fatty acids, cholesterol and triglyceride levels and are useful in the treatment and/or prophylaxis of diabetes. The compounds of the present invention are effective in treatment of obesity, inflammation, autoimmune diseases such as multiple sclerosis and rheumatoid arthritis and immunological diseases, including the treatment of cancer. Furthermore, the compounds are useful for the treatment of disorders associated with insulin resistance.Type: GrantFiled: February 21, 2006Date of Patent: August 24, 2010Assignee: Bexel Pharmaceuticals, Inc.Inventors: Partha Neogi, Bishwajit Nag, Debendranath Dey, Abhijeet Nag, Birendra Kumar Bhattacharya, Vinod Kumar Singh, Surendradoss Jayakumar
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Publication number: 20100210577Abstract: 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: ApplicationFiled: June 8, 2007Publication date: August 19, 2010Inventors: Jasbir Singh, Carl F. Nathan, Ruslana Bryk, Raghu Samy, Krzysztof Pupek, Mark Gurney
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Patent number: 7759493Abstract: Bicyclic compounds containing a phenyl or pyridyl ring fused to a cycloalkyl or heterocyclic ring, to which is attached a 5-membered heterocyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.Type: GrantFiled: January 30, 2006Date of Patent: July 20, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Min Ge, Lihu Yang, Changyou Zhou, Songnian Lin, Haifeng Tang, Eric Dean Cline, Sunita Malkani
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Patent number: 7732470Abstract: Derivative compounds of 11-nonyloxy-undec-8(Z)-eonic acid that mimic epoxide metabolites are provided. Also provided are compositions comprising a therapeutically effective amount of the derivative compounds. The present invention further provides methods for the use of such compositions for the treatment of renal or cardiovascular disease and/or related conditions.Type: GrantFiled: February 29, 2008Date of Patent: June 8, 2010Assignees: Medical College of Georgia Research Institute, Board of Regents, The University of Texas SystemInventors: John D. Imig, John R. Falck
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Patent number: 7718681Abstract: The present invention relates to a 5-(1,3-diaryl-1H-pyrazol-4-ylmethylene)-thiazolidine-2,4-dione derivative or its pharmaceutically acceptable salts thereof, a method for preparing the same and an anticancer agent composition comprising the same as an active ingredient.Type: GrantFiled: February 3, 2006Date of Patent: May 18, 2010Assignee: Korea Research Institute of Chemical TechnologyInventors: Hyoung Rae Kim, Jaesung No, Min Jung Seo, Bo Gan Song, Bum Suk Son, Jung Ki Kim, Kwang-Rok Kim, Hyae Gyeong Cheon, Ge Hyeong Lee
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Publication number: 20100056503Abstract: 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. 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: ApplicationFiled: June 19, 2009Publication date: March 4, 2010Applicant: The General Hospital CorporationInventors: Vineet Gupta, M. Amin Arnaout
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Publication number: 20100016292Abstract: The invention provides compounds that can efficiently and specifically inhibit bacterial toxins, such as inhibit the lethal factor (LF) protease activity of anthrax toxin and/or botulinum neurotoxin type A. The invention also provides methods for inhibiting proteases, such as lethal factor protease, as well as methods for treating bacterial infections, such as anthrax and botulinum.Type: ApplicationFiled: July 18, 2008Publication date: January 21, 2010Applicant: The Burnham InstituteInventor: Maurizio Pellecchia
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Publication number: 20090312352Abstract: The invention generally relates to compositions and methods for treatment of disease caused by Yersinia spp. infection. More specifically, the invention relates to protein tyrosine phosphatase inhibitors and derivatives and analogs thereof, pharmaceutical compositions containing the protein tyrosine phosphatase inhibitors and analogs, methods of making the protein tyrosine phosphatase inhibitors and analogs and methods of use thereof.Type: ApplicationFiled: October 19, 2005Publication date: December 17, 2009Inventors: Tomas Mikael Mustelin, Maurizio Pellecchia, Lutz Tautz
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Publication number: 20090312303Abstract: Bicyclic compounds containing a phenyl or pyridyl ring fused to a cycloalkyl or heterocyclic ring, to which is attached a 5-membered heterocyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.Type: ApplicationFiled: January 30, 2006Publication date: December 17, 2009Applicant: MERCK & CO., INC.Inventors: Min Ge, Lihu Yang, Changyou Zhou, Songnian Lin, Haifeng Tang, Eric Dean Cline, Sunita Malkani
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Publication number: 20090291992Abstract: Compounds of the thiazolidinedione family are provided and shown to be effective androgen receptor ablative agents that can be used in methods of treating or preventing cancer or precancer, including prostate cancer. Also provided are methods of treating or preventing cancer by administering a therapeutically effective amount of one of the androgen receptor ablative agents to a subject in need of such treatment.Type: ApplicationFiled: February 20, 2009Publication date: November 26, 2009Applicant: THE OHIO STATE UNIVERSITY RESEARCH FOUNDATIONInventors: Ching-Shih Chen, Dasheng Wang, Jian Yang
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Publication number: 20090258914Abstract: A compound having the structure A is described as well as the use of such compounds to inhibit at least one BCL-2 protein family member.Type: ApplicationFiled: April 15, 2009Publication date: October 15, 2009Applicant: Burnham Institute for Medical ResearchInventor: Maurizio Pellecchia
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Publication number: 20090247587Abstract: The object is to provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. The solving means is a 1,3-dihydroisobenzofuran derivative represented by the following general formula (1) or salt thereof, or their solvate.Type: ApplicationFiled: March 30, 2009Publication date: October 1, 2009Applicant: KOWA COMPANY, LTD.Inventors: Ayumu OKUDA, Takayuki MATSUDA, Toru MIURA, Koichi YAMAZAKI, Yuki YAMAGUCHI, Minoru KOURA, Sayaka KUROBUCHI, Yuuichiro WATANABE, Kimiyuki SHIBUYA
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Publication number: 20090227790Abstract: The present application is directed to therapeutic compounds, compositions, and methods for culturing neuronal cells and for preventing and the treatment of neurodegenerative diseases, such as Parkinson's disease and amyotrophic lateral sclerosis (ALS).Type: ApplicationFiled: April 7, 2009Publication date: September 10, 2009Inventor: Leu-Fen H. Lin
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Patent number: 7572816Abstract: The present invention is directed to compounds having the structure wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells.Type: GrantFiled: July 21, 2004Date of Patent: August 11, 2009Assignee: Auspex Pharmaceuticals, Inc.Inventors: Bruno Tse, Sepehr Sarshar
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Publication number: 20090197870Abstract: Compounds for use in compositions and methods for modulating the activity of nuclear receptors are provided. In particular, compounds for use in compositions and methods for modulating the estrogen related receptors are provided. In one embodiment, the compounds provided herein are ERR modulators. In another embodiment, the compounds provided herein are agonists, partial agonists, antagonists, or inverse agonists of ERR or ERR?. In certain embodiments, the compounds of the invention, as described above in the Summary of the Invention, are compounds of formula (I).Type: ApplicationFiled: October 21, 2005Publication date: August 6, 2009Applicant: EXELIXIS, INC.Inventors: Richard Martin, Raju Mohan, Brett B. Busch, Michael Charles Nyman, William C. Stevens, JR.
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Publication number: 20090170908Abstract: The Spiro compound represented by the following general formula [Ia], its pharmaceutically acceptable salt or a solvate thereofType: ApplicationFiled: October 24, 2008Publication date: July 2, 2009Applicant: Japan Tobacco Inc.Inventors: Takashi Shimada, Hiroshi Ueno, Kazuhiro Tsutsumi, Kouichi Aoyagi, Tomoyuki Manabe, Shin-Ya Sasaki, Susumu Katoh
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Publication number: 20090124675Abstract: Various compounds comprising a thiazolidine ring are described as well as the use of such compounds to inhibit at least one BCL-2 protein family member. One of the compounds described has the structure the structure A, wherein each of R1, and R2 comprises hydrogen, a substituted or unsubstituted straight-chained aliphatic group, a halogen, an alkoxyl, a halogen-substituted alkyl, a halogen-substituted alkoxyl, hydroxyl, carboxyl, cyano group, an amido group, a substituted or unsubstituted cycloaliphatic group, a substituted or unsubstituted aromatic group, or a substituted or unsubstituted heterocyclic group; X comprises oxygen, sulfur, or imino group; and Z comprises a moiety such as naphthaline or dehydronaphthaline, among others.Type: ApplicationFiled: October 17, 2008Publication date: May 14, 2009Applicant: Burnham Institute for Medical ResearchInventor: Maurizio Pellecchia
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Publication number: 20090111855Abstract: 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: ApplicationFiled: March 6, 2008Publication date: April 30, 2009Inventors: Michael Gaul, Alexander Kim, Lily Lee Searle, Raymond J. Patch, Dionisios Rentzeperis, Guozhang Xu, Xizhen Zhu
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Publication number: 20090105254Abstract: Disclosed herein are Vaccinia H1-related (VHR) protein tyrosine phosphatase (PTP) inhibitors that provide a method for treating cancer.Type: ApplicationFiled: October 17, 2008Publication date: April 23, 2009Applicant: BURNHAM INSTITUTE FOR MEDICAL RESEARCHInventors: Tomas Mustelin, Lutz Tautz
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Patent number: RE42700Abstract: The present invention provides compounds that are inducers or inhibitors of apoptosis of apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.Type: GrantFiled: July 25, 2008Date of Patent: September 13, 2011Assignees: Sanford-Burnham Medical Research Institute, Oregon State University, SRI International, Molecular Medicine Research Institute, Department of Veterans Affairs, Wayne State UniversityInventors: Marcia Dawson, Joseph A. Fontana, Xiao-Kun Zhang, Mark Leid, Ling Jong, Peter D. Hobbs