Bicyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 514/233.5)
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Publication number: 20120238562Abstract: The invention relates to the treatment of prostate cancer. In various embodiments, the invention teaches a method of administering one or more compounds that inhibit a molecule that antagonizes the activity of tumor suppressor Mst1 and Mst2 pathway signaling. In certain embodiments, one or more of the compounds include an mTOR and PI3K inhibitor.Type: ApplicationFiled: March 8, 2012Publication date: September 20, 2012Applicant: CEDARS-SINAI MEDICAL CENTERInventors: Bekir Cinar, Filiz Kisaayak Collak
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Publication number: 20120238541Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: September 17, 2010Publication date: September 20, 2012Applicant: Almac Discovery LimitedInventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
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Publication number: 20120238567Abstract: The present invention relates to compounds having pharmacological activity towards the sigma (?) receptor, and more particularly to some 4, 5, 6, 7 tetrahydrobenzo[b]thiophene derivatives, wherein n is selected from 0, 1, 2, 3 or 4; m is selected from 0, 1 or 2; the dotted line represents either a single or a double bond; to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis.Type: ApplicationFiled: May 30, 2012Publication date: September 20, 2012Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Jordi CORBERA-ARJONA, Daniel MARTINEZ-OLMO, David VANO-DOMENECH
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Publication number: 20120238566Abstract: Use of cell autophagy (type II cell apoptosis) inhibitors for preventing and/or treating avian influenza, injury of lungs caused by avian influenza virus or nanometer materials. The cell autophagy (type II cell apoptosis) inhibitors are selected from 3-methyladenine, SB203580, LY294002, and or wortmannin. The injury of lungs includes acute respiratory distress syndrome. The avian influenza virus is H5N1, H5N2 or H9N2 avian influenza virus. The nanometer materials include PAMAM G3, G4, G5, G5.5, G6, G7, or G8.Type: ApplicationFiled: April 27, 2010Publication date: September 20, 2012Inventors: Chengyu Jiang, Shuan Rao, Haolin Liu, Feng Guo, Hongliang Wang, Yang Sun, Chenggang Li
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Publication number: 20120222142Abstract: The present application relates to a composition including gut flora-derived extracellular vesicles, and to an animal disease model using same. In addition, the present application relates to a method for using the gut flora-derived extracellular vesicles to efficiently search for a candidate drug which may prevent or treat diseases that occur due to gut flora-derived extracellular vesicles, and to a vaccine which can efficiently prevent or treat infections caused by gut flora or diseases that occur due to gut flora-derived extracellular vesicles. Further, the development of diagnostic technology to discover, using the gut flora-derived extracellular vesicles of the present application, the etiology of diseases that occur due to gut flora-derived extracellular vesicles, can be achieved.Type: ApplicationFiled: July 20, 2010Publication date: August 30, 2012Applicant: AEON MEDIX INC.Inventors: Yoon Keun Kim, Yong Song Gho, Kyoung Su Park, Bok Sil Hong, Ji Hyun Kim, You Sun Kim, Won Hee Lee, Jung Wook Kim, Dae-Kyum Kim
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Publication number: 20120214794Abstract: This invention provides compounds of formula I-A or I-B: wherein HY, G1, G2, R2, R12, W1, W2, n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: October 13, 2011Publication date: August 23, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu
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Patent number: 8242115Abstract: Compounds that inhibit DNA-dependent protein kinase, compositions comprising the compounds, methods to inhibit the DNA-PK biological activity, methods to sensitize cells the agents that cause DNA lesions, and methods to potentiate cancer treatment are disclosed.Type: GrantFiled: February 16, 2007Date of Patent: August 14, 2012Assignee: Luitpold Pharmaceuticals, Inc.Inventors: James Halbrook, Edward A. Kesicki, Laurence E. Burgess, Stephen T. Schlachter, Charles T. Eary, Justin G. Schiro, Hongmei Huang, Michael Evans, Yongxin Han
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Publication number: 20120201749Abstract: Compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein: W is arylene, heteroarylene or formula (a) each L is independently alkylene, alkenylene, alkynylene, a direct bond, arylene, cycloalkylene, alkylene-arylene, alkylene-C?O or —C?O; each X is independently an N-containing heteroarylene, N-containing cycloalkylene or NR; Y is N-containing heteroaryl, N-containing cycloalkyl, NR2, OR1, CN or CO2R; Z1 is formula (b); are useful in therapy, particularly in the therapy of neurodegeneration and cancer.Type: ApplicationFiled: August 25, 2010Publication date: August 9, 2012Inventors: Melanie Jayne Crawshaw, Philip Spencer Fallon, Ashley Nicholas Jarvis, Jonathan Raymond Powell, Natalie Louise Winfield, David Selwood, Ian Charles Zachary, Haiyan Jia
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Publication number: 20120190674Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.Type: ApplicationFiled: February 28, 2012Publication date: July 26, 2012Inventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Reaney, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
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Publication number: 20120183553Abstract: Disclosed are composition and methods for treating immune disorders. Also disclosed are diagnosis methods and prognosis methods.Type: ApplicationFiled: July 15, 2010Publication date: July 19, 2012Inventors: Zhenglun Zhu, Hong Gao
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Publication number: 20120178735Abstract: Provided is a 2H-chromene compound or a derivative thereof which has an excellent S1P1 agonist action. The 2H-chromene compound or derivative is particularly useful for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells.Type: ApplicationFiled: February 15, 2012Publication date: July 12, 2012Applicant: ASTELLAS PHARMA INC.Inventors: Hironori Harada, Kazuyuki Hattori, Kazuya Fujita, Sunao Imada, Tatsuaki Morokata
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Publication number: 20120172351Abstract: A compound represented by the formula (I): wherein each symbol is as defined in the specification, and a salt thereof have a GPR40 receptor activation action and is useful as an insulin secretagogue or a prophylactic or therapeutic drug for diabetes and the like.Type: ApplicationFiled: June 8, 2010Publication date: July 5, 2012Inventors: Nobuyuki Negoro, Yoshito Terao, Satoshi Mikami, Tomoya Yukawa
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Publication number: 20120157449Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, x, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.Type: ApplicationFiled: December 7, 2011Publication date: June 21, 2012Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Patent number: 8198271Abstract: A compound having the following formula (1) or a salt thereof: wherein R1 and R2 represent hydrogen, a lower alkyl, a lower alkenyl, a lower alkynyl or a group having the following formula (2): (R6)n—{circle around (A)}—Z—??(2), R3 represents hydroxy, a lower alkoxy, a lower cycloalkyloxy, an aryloxy, carboxy, a lower alkoxycarbonyl, or —NRaRb having the following formula (3): (R7)o—{circle around (B)}—??(3), R4 and R5 represent halogen, a lower alkyl, hydroxy, or a lower alkoxy; R6 represents halogen, a lower alkyl, an aryl group, a heterocyclic, a hydroxy, a lower alkoxy, mercapto, a lower alkylthio, a lower alkylcarbonyl, amino, nitro or cyano; R7 represents a lower alkyl, hydroxy or a lower alkoxy; Ra and Rb represent hydrogen or a lower alkyl; the ring A represents a cyclic hydrocarbon or a heterocyclic ring; the ring B represents a heterocyclic ring having one or more heteroatoms selected from the group consisting of nitrogen and oxygen; X represents a lower alkylene; Y represents a lower alkyleType: GrantFiled: May 25, 2009Date of Patent: June 12, 2012Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Hiroyuki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
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Publication number: 20120142682Abstract: Compounds that inhibit bacterial virulence factors from the mono-ADP-ribosyltransferase (mART) family of toxins have been identified that are not toxic to cells or the producing bacterial pathogen. These compounds have great potential as antivirulence agents for treating many bacterial infections and disease states.Type: ApplicationFiled: December 2, 2011Publication date: June 7, 2012Applicant: UNIVERSITY OF GUELPHInventor: Allen Rod Merrill
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Publication number: 20120114637Abstract: Diseases and conditions associated with tissues of the body, including but not limited to tissues in the eye, can be effectively treated, prevented, inhibited, onset delayed, or regression caused by administering therapeutic agents to those tissues. Described herein are ophthalmic formulations that deliver a variety of therapeutic agents, including but not limited to rapamycin (sirolimus), analogs thereof (rapalogs) or other mTOR inhibitors, to a subject for an extended period of time. The ophthalmic formulations may be placed in an aqueous medium of a subject, including but not limited to intraocular or periocular administration, or placement proximate to a site of a disease or condition to be treated in a subject. A method may be used to administer a therapeutic agent to treat or prevent age-related macular degeneration, macular edema, diabetic retinopathy, uveitis, dry eye, or a hyperpermeability disease in a subject.Type: ApplicationFiled: May 4, 2010Publication date: May 10, 2012Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Thierry Nivaggioli, David A. Weber, Philippe JM Dor, Philip Reilly
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Patent number: 8153682Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.Type: GrantFiled: July 18, 2008Date of Patent: April 10, 2012Assignee: Janssen Pharmaceutica, NVInventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Reaney, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
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Patent number: 8148422Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.Type: GrantFiled: December 15, 2009Date of Patent: April 3, 2012Assignee: Janssen Pharmaceutica, NVInventors: Mark J. Macielag, James J. McNally
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Publication number: 20120077775Abstract: Disclosed are macrocyclic compounds of formulae I-V, which are analogs of the pochonin resorcylic acid lactones, and processes for the preparation of the compounds. The compounds disclosed are useful as inhibitors of kinases and Heat Shock Protein 90 (HSP 90). Also disclosed are pharmaceutical compositions comprising an effective kinase-inhibiting amount or an effective HSP90-inhibiting amount of the compounds and methods for the treatment of disorders that are mediated by kinases and HSP90.Type: ApplicationFiled: September 23, 2011Publication date: March 29, 2012Applicants: LE CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE STRASBOURGInventors: Nicolas WINSSINGER, Sofia BARLUENGA, Martin KARPLUS
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Publication number: 20120059001Abstract: The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.Type: ApplicationFiled: November 9, 2011Publication date: March 8, 2012Applicants: Incozen Therapeutics Pvt. Ltd., Rhizen Pharmaceuticals SAInventors: Meyyappan MUTHUPPALANIAPPAN, Srikant Viswanadha, Govindarajulu Babu, Swaroop Kumar V.S. Vakkalanka
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Publication number: 20120053164Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. Formula (I), wherein A is selected from among a single bond, ?CH—, —CH2—, —O—, —S—, and —NH—; wherein n is 1, 2 or 3; wherein Z is C or N, the other variables are as defined in the claims, as well as in form of their acid addition salts with pharmacologically acceptable acids.Type: ApplicationFiled: December 17, 2009Publication date: March 1, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Thomas Trieselmann, Patrick Tielmann, Stefan Scheuerer, Silke Hobbie, Frank Buettner
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Publication number: 20120053173Abstract: Provision of a prophylactic or therapeutic agent for diabetes, which has superior efficacy. A compound represented by the formula: wherein each symbol is as described in the specification, or a salt thereof.Type: ApplicationFiled: March 4, 2009Publication date: March 1, 2012Inventors: Yoshihiro Banno, Ryoma Hara, Ryosuke Tokunoh
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Publication number: 20120046277Abstract: The present invention provides a compound represented by the following formula (I): wherein: Ring A represents an optionally substituted piperazine ring, an optionally substituted morpholine ring, or an optionally substituted bromopiperazine ring; R1 and R2 are the same or different from each other, and represent a hydrogen atom or optionally substituted lower alkyl; R3 and R4 are the same or different from each other, and represent a hydrogen atom or halogenated or non-halogenated lower alkyl; R3 to R7 are the same or different from each other, and represent a hydrogen atom, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted cycloakyl, optionally substituted aryl, an optionally substituted aromatic heterocyclic ring, optionally substituted amino, or acyl; and represents a single bond or double bond, wherein R2 and R3 do not exist when carbon atoms respectively adjacent to R2: and R3 form a double bond, and there is noType: ApplicationFiled: March 9, 2010Publication date: February 23, 2012Inventors: Tetsuya Tsukamoto, Takeshi Wakabayashi, Taiichi Ohra
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Publication number: 20120039839Abstract: We found that FIZZ1/RELM? is inducible by hypoxia in lung. The hypoxia-upregulated expression of FIZZ1/RELM? was located in the pulmonary vasculature, bronchial epithelial cells, and type II pneumocytes. Recombinant FIZZ1/RELM? protein stimulates rat pulmonary microvascular smooth muscle cell (RPSM) proliferation dose-dependently. Therefore, we renamed this gene as hypoxia-induced mitogenic factor (HIMF). HIMF strongly activated Akt phosphorylation. The phosphatidylinositol 3-kinase (PI3K) inhibitor LY294002 inhibits HIMF-activated Akt phosphorylation. It also inhibits HIMF-stimulated RPSM proliferation. Thus, the PI3K/Akt pathway, at least in part, mediates the proliferative effect of HIMF. HIMF also has angiogenic and vasoconstrictive activity. Notably, HIMF increases pulmonary arterial pressure and vascular resistance more potently than either endothelin-1 or angiotensin II.Type: ApplicationFiled: August 17, 2011Publication date: February 16, 2012Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Roger Johns, Xingwu Teng, Dechun LI
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Patent number: 8106045Abstract: A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein X represents CH or N; represents a C1-C12 alkyl; R2 represents a hydrogen atom, or the like; R? represents a C1-C6 alkyl or the like; q represents 0 or an integer of 1 to 7; Y represents a C1-C6 alkyl or the like; p represents 0 or an integer of 1 to 5; R represents a 2,3-dihydroindolyl or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).Type: GrantFiled: September 9, 2005Date of Patent: January 31, 2012Assignees: Mitsubishi Tanabe Pharma Corporation, Sanofi-AventisInventors: Kazutoshi Watanabe, Fumiaki Uehara, Shinsuke Hiki, Toshiyuki Kohara, Kenji Fukunaga, Satoshi Yokoshima
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Publication number: 20120022062Abstract: The present invention relates to flavanoid compounds of general formula (X1) wherein: R1 is selected from a group consisting of morpholinyl, N-methyl piperizinyl, piperidinyl and N,N?-dimethylamino groups, and n ranges from 3 to 6, and process for preparation thereof. The present invention relates to the demonstration of anti Helicobacter pylori activity and gastric antisecretory activity of semisynthetically designed flavonoid compounds, to be used for the prevention and treatment of gastroduodenal disorders in general and peptic ulcer diseases in particular. The present invention also relates to a hetero-dimeric bi-functional molecule that can be used as monotherapy substituting/replacing/overcoming currently used triple/quadruple therapy, thereby implicating/anticipating/envisaging its commercial applicability.Type: ApplicationFiled: February 26, 2010Publication date: January 26, 2012Inventors: Pratap Kumar Dab, Suchandra Goswami, Annalaskhmi Chinniah, Janaswamy Madusudana Rao, Suresh Babu Katragadda
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Patent number: 8101606Abstract: The present invention encompasses methods for treating neurofibromatosis.Type: GrantFiled: November 12, 2008Date of Patent: January 24, 2012Assignee: Washington UniversityInventors: David Gutmann, Jason Weber
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Publication number: 20120015928Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Applicant: INCYTE CORPORATIONInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Brian W. Metcalf, Chunhong He, Ding-Quan Qian, Colin Zhang
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Publication number: 20120015925Abstract: A pharmaceutical useful as a therapeutic agent and a preventive agent for hyperlipemia, and a pharmaceutical useful as a therapeutic agent and a preventive agent for hepatic disorders associated with cholestasis, particularly, primary biliary cirrhosis and primary sclerosing cholangitis, and a pharmaceutical useful as a therapeutic agent and a preventive agent for obesity, fatty liver and steatohepatitis are provided.Type: ApplicationFiled: May 16, 2011Publication date: January 19, 2012Applicant: ASAHI KASEI PHARMA CORPORATIONInventors: Takehiko SASAHARA, Mitsunobu MOHRI, Ken-ichi KASAHARA
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Publication number: 20110306608Abstract: The disclosure provides methods and compositions for the treatment of vascular, autoimmune and inflammatory diseases using a combination of an inosine monophosphate dehydrogenase (IMPDH) inhibitor and a HMG CoA reductase inhibitor.Type: ApplicationFiled: April 5, 2011Publication date: December 15, 2011Inventors: Michael R. Hayden, Noel Hall
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Publication number: 20110294787Abstract: The present invention relates to morpholine and thiomorpholine derivatives of the general formula I or pharmaceutically acceptable salts thereof and their use.Type: ApplicationFiled: July 28, 2011Publication date: December 1, 2011Applicant: H. Lundbeck A/SInventors: Christian Wenzel Tornøe, Mario Rottländer, Nikolay Khanzhin, Andreas Ritzèn, William Patrick Watson
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Patent number: 8067412Abstract: Disclosed are macrocyclic compounds of formulae I-V, which are analogs of the pochonin resorcylic acid lactones, and processes for the preparation of the compounds. The compounds disclosed are useful as inhibitors of kinases and Heat Shock Protein 90 (HSP 90). Also disclosed are pharmaceutical compositions comprising an effective kinase-inhibiting amount or an effective HSP90-inhibiting amount of the compounds and methods for the treatment of disorders that are mediated by kinases and HSP90.Type: GrantFiled: August 10, 2007Date of Patent: November 29, 2011Assignees: Universite de Strasbourg, Le Centre National de la Recherche ScientifiqueInventors: Nicolas Winssinger, Sofia Barluenga, Martin Karplus
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Patent number: 8063035Abstract: The present invention provides triazolyl aminopyrimidine compounds useful in the treatment of cancer.Type: GrantFiled: May 7, 2008Date of Patent: November 22, 2011Assignee: Eli Lilly and CompanyInventors: Joyce Z. Crich, James Robert Henry, Hong Hu, Delu Jiang, Hong-Yu Li, William Thomas McMillen, Jason Scott Sawyer, Melissa Kate Slater, Yan Wang
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Publication number: 20110269755Abstract: The disclosure provides compositions and methods for the treatment of vascular, autoimmune, and inflammatory diseases using a combination of an inosine monophosphate dehydrogenase (IMPDH) inhibitor and a HMG CoA reductase inhibitor.Type: ApplicationFiled: December 9, 2010Publication date: November 3, 2011Applicant: Aspreva International Ltd.Inventors: Michael HAYDEN, Noel Hall
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Publication number: 20110262437Abstract: It is disclosed herein that members of the protein tyrosine kinase (PTK) family are highly mutated in patients with melanoma. Described herein are novel somatic mutations in the ERBB4 gene that result in increased kinase activity, transformation ability and anchorage-independent growth. These ERBB4 mutations contribute to the tumorogenicity of melanoma. Thus, provided herein is a method of predicting the prognosis of a patient with melanoma by detecting the presence or absence of a mutation in the ERBB4 gene. In some examples, the ERBB4 mutation is selected from G949A, G1354A, G1624A, C1630T, G1687A, G2506A and G2614A (numbering based on SEQ ID NO: 1). Also provided are methods of selecting a patient as a candidate for treatment with an ERBB4 and/or PI3K/AKT pathway inhibitor, and a method of identifying a therapeutic agent for the treatment of a subject diagnosed with melanoma.Type: ApplicationFiled: August 6, 2009Publication date: October 27, 2011Inventors: Yardena R. Samuels, Todd D. Prickett
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Publication number: 20110257174Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: September 29, 2009Publication date: October 20, 2011Applicant: Sirtris Pharmaceuticals, Inc.Inventors: Christopher Oalmann, Robert B. Perni, Chi B. Vu
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Publication number: 20110251182Abstract: This invention relates to methods of screening for modulators of mammalian cell injury cause by TRPM7 gene and protein activity, compounds that modulate TRPM7 gene and protein activity and methods of treatment of mammalian cell injury using modulators of TRPM7 gene and protein activity.Type: ApplicationFiled: December 13, 2010Publication date: October 13, 2011Applicant: NoNO, Inc.Inventors: Xiujun Sun, Michael Tymianski, Jonathan David Garman
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Publication number: 20110244043Abstract: A controlled releasing composition comprising a plurality of microparticles and a matrix as well as the preparation method thereof is disclosed. The plurality of microparticles comprise a first material and the matrix comprises a second material. The melting temperature of the first material is higher than the melting temperature of the second material.Type: ApplicationFiled: December 10, 2009Publication date: October 6, 2011Inventors: Jianjian Xu, Shiliang Wang, Manzhi Ding
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Publication number: 20110245244Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR? and should be useful for treating conditions mediated by the same.Type: ApplicationFiled: April 4, 2011Publication date: October 6, 2011Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Per Sauerberg, Pavel Pihera, Zdenek Polivka, Miroslav Havranek, Ingrid Pettersson, John Patrick Mogensen
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Publication number: 20110224206Abstract: The present invention relates to substituted pyrrole compounds of formula I and compositions comprising substituted tri-substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a tri-substituted’ triazole compound of the invention, or a pharmaceutical composition comprising such a compound.Type: ApplicationFiled: August 7, 2009Publication date: September 15, 2011Inventors: Weiwen Ying, Dinesh U. Chimmanamada, Joseph A. Burlison, Shijie Zhang, Minghu Song, Junghyun Chae
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Publication number: 20110218179Abstract: This invention provides a method of treating a subject afflicted with active lupus nephritis comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the subject. This invention also provides laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with active lupus nephritis. This invention further provides a pharmaceutical composition comprising an amount of laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with active lupus nephritis.Type: ApplicationFiled: March 2, 2011Publication date: September 8, 2011Inventors: Asi Haviv, Nora Tarcic
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Publication number: 20110217335Abstract: Disclosed are macrocyclic compounds of formulae I, I?, II, II?, III, III?, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.Type: ApplicationFiled: January 15, 2009Publication date: September 8, 2011Applicant: UNIVERSITE DE STRASBOURGInventors: Nicolas Winssinger, Sofia Barluenga, Martin Karplus
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Publication number: 20110212940Abstract: The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.Type: ApplicationFiled: February 25, 2011Publication date: September 1, 2011Applicant: EPIX PHARMACEUTICALS, INC.Inventors: Roland Burli, Victor J. Cee, Jennifer Golden, Brian Alan Lanman, Susana Neira, Ashis Saha, Nili Schutz, Xiang Yu, Dilara McCauley, Mercedes Lobera, Yael Marantz, Jian Lin, Srinivasa R. Cheruku, Pini Orbach, Anurag Sharadendu, Robert C. Penland, Kimberley Gannon, Sharon Shacham, Silvia Noiman, Oren Becker, Zhaoda Zhang
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Publication number: 20110212958Abstract: The invention relates to fatty acid raloxifene derivatives; compositions comprising an effective amount of a fatty acid raloxifene derivative; and methods for treating osteoporosis or preventing invasive breast cancer in postmenopausal women comprising the administration of an effective amount of a fatty acid raloxifene derivative.Type: ApplicationFiled: February 25, 2011Publication date: September 1, 2011Applicant: CATABASIS PHARMACEUTICALS, INC.Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Publication number: 20110207729Abstract: An object of the present invention is to provide a novel and excellent agent for treating or preventing dementia, schizophrenia, and the like, based on the serotonin 5-HT5A receptor modulating action. It was confirmed that a bicyclic acylguanidine derivative which has a characteristic structure that guanidine is bonded to one ring of a bicyclic structure such as chromene and dihydronaphthalene through a carbonyl group and a cyclic group is bonded on the other ring, has a potent 5-HT5A receptor modulating action and an excellent pharmacological action based on this mechanism. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder.Type: ApplicationFiled: August 7, 2008Publication date: August 25, 2011Applicant: ASTELLAS PHARMA INC.Inventors: Isao Kinoyama, Satoshi Miyamoto, Takehiro Miyazaki, Yohei Koganemaru, Yuichiro Kawamoto, Nobuyuki Shiraishi, Hiroaki Hoshii, Akio Kuroda, Mayako Yamazaki, Minoru Yasuda, Hiroaki Mizuno
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Publication number: 20110207730Abstract: Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of analgesia and local anesthesia.Type: ApplicationFiled: December 16, 2010Publication date: August 25, 2011Applicant: Cardiome Pharma Corp.Inventors: Allen I. Bain, Gregory N. Beatch, Cindy J. Longley, Bertrand M.C. Plouvier, Tao Sheng, Michael J.A. Walker, Richard A. Wall, Sandro L. Yong, Jeff Jiqun Zhu, Alexander B. Zolotoy
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Publication number: 20110190291Abstract: Methods and compositions for treating disease caused by increased iron levels are disclosed Fluoregenic compounds and methods of using the same are also described.Type: ApplicationFiled: July 21, 2009Publication date: August 4, 2011Applicant: Regents of the University of California, a California corporationInventors: Adam Renslo, Sumit Mahajan
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Publication number: 20110178061Abstract: Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.Type: ApplicationFiled: December 17, 2010Publication date: July 21, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Andreas P. Termin, Esther Ann Martinborough, Nicole Hilgraf, Charles J. Cohen, Corey Anderson
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Patent number: 7973030Abstract: A pharmaceutical useful as a therapeutic agent and a preventive agent for hyperlipemia, and a pharmaceutical useful as a therapeutic agent and a preventive agent for hepatic disorders associated with cholestasis, particularly, primary biliary cirrhosis and primary sclerosing cholangitis, and a pharmaceutical useful as a therapeutic agent and a preventive agent for obesity, fatty liver and steatohepatitis are provided.Type: GrantFiled: February 25, 2005Date of Patent: July 5, 2011Assignee: Asahi Kasei Pharma CorporationInventors: Takehiko Sasahara, Mitsunobu Mohri, Ken-Ichi Kasahara
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Publication number: 20110152250Abstract: Compounds that are antagonists of the VR1 receptor, having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A1, A2, A3, A4, R7, R8, R9, X, Y, Z, L, n, and m, are as defined herein, and are useful in disorders prevented or ameliorated by inhibiting the VR1 receptor.Type: ApplicationFiled: September 3, 2010Publication date: June 23, 2011Applicant: ABBOTT LABORATORIESInventors: Arthur Gomtsyan, Erol K. Bayburt, Robert G. Schmidt, JR., Chih-Hung Lee, Brian S. Brown, Tammie K. Jinkerson, John R. Koenig, Jerome F. Daanen, Steven P. Latshaw