Polycyclo Ring System Having The Oxazole Ring As One Of The Cyclos Patents (Class 514/375)
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Publication number: 20130203818Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: April 27, 2011Publication date: August 8, 2013Applicant: CALCIMEDICA, INC.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Patent number: 8497283Abstract: The present invention relates to compounds according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.Type: GrantFiled: September 14, 2012Date of Patent: July 30, 2013Assignee: Merck Patent GmbHInventors: Melanie Schultz, Kai Schiemann, Jr., Wolfgang Staehle
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Publication number: 20130190350Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.Type: ApplicationFiled: December 12, 2012Publication date: July 25, 2013Applicant: CURIS, INC.Inventor: Curis, Inc.
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Publication number: 20130178466Abstract: The invention provides compositions, medicaments and methods of treating microbial infections, and especially respiratory disorders caused by microbial infections. In particular, the invention relates to the treatment of respiratory diseases caused by pathogenic infections using certain either alkyl substituted or un-substituted 2-aryl acetic acid, or 2-aryl, N-hydroxyacetamide derivatives, or pentoxifylline, and to the use of these compounds in methods of treatment.Type: ApplicationFiled: November 9, 2010Publication date: July 11, 2013Applicant: BIOCOPEA LIMITEDInventors: Robin Mark Bannister, Wilson Caparros Wanderlay, John Brew
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Patent number: 8481532Abstract: Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.Type: GrantFiled: July 9, 2009Date of Patent: July 9, 2013Assignee: EnVivo Pharmaceuticals, Inc.Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Patent number: 8481547Abstract: The present invention is directed to substituted benzothiazole and benzoxazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.Type: GrantFiled: December 16, 2010Date of Patent: July 9, 2013Assignee: Janssen Pharmaceutica NVInventors: Alfonzo D. Jordan, Renee L. DesJarlais, Dennis J. Hlasta, Michael H. Parker, Carsten Schubert, Kimberly White
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Publication number: 20130172333Abstract: Provided is a pharmaceutical composition comprising a pharmaceutically acceptable organic solvent, a pharmaceutically acceptable surfactant, and a compound according to the following formula: wherein the variables are defined herein. Optionally, the pharmaceutical composition further comprises a co-solvent. Also provided is a method of using the pharmaceutical composition disclosed herein for the treatment of a patient in need thereof.Type: ApplicationFiled: May 20, 2011Publication date: July 4, 2013Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Neera Jain, Suresh R. Babu, Shweta Kotecha, Hong Yang
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Publication number: 20130172351Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.Type: ApplicationFiled: June 26, 2012Publication date: July 4, 2013Applicant: MERCK PATENT GMBHInventors: Henry Yu, Thomas E. Richardson, Robert James Foglesong, Lizbeth Celeste DeSelm, Andreas Goutopoulos
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Publication number: 20130172335Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: February 22, 2013Publication date: July 4, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8476274Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: GrantFiled: October 18, 2012Date of Patent: July 2, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Kevin D. McCormick, Li Dong, Christopher W. Boyce, Manuel de Lera Ruiz, Salem Fevrier, Jie Wu, Junying Zheng, Younong Yu, Jianhua Chao, Walter S. Won, Ashwin U. Rao, Rongze Kuang, Pauline C. Ting, Xianhai Huang, Ning Shao, Anandan Palani, Michael Y. Berlin, Robert G. Aslanian
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Publication number: 20130165454Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.Type: ApplicationFiled: October 18, 2012Publication date: June 27, 2013Applicant: HYDRA BIOSCIENCES, INC.Inventor: HYDRA BIOSCIENCES, INC.
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Publication number: 20130165485Abstract: A compound of formula (I): where A, B, C, G, m, n, o, p, R1, R2, R3, R4, R5, R6, X, R7, R8, R9, R10 and R11 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: February 20, 2013Publication date: June 27, 2013Applicant: Syngenta Crop Protection LLCInventors: Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik, Myriem El Qacemi, Anne Jacqueline Dalencon, Werner Zambach, Christopher Richard Godfrey, Thomas Pitterna, Pierre Joseph Jung, Jagadish Pabba
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Patent number: 8470776Abstract: The present invention provides conjugates of disorazoles and their derivatives with cell-binding molecules, such as peptides, proteins, hormones, blood proteins and antibodies. The present invention further provides novel disorazole derivatives and processes of manufacturing such conjugates and disorazole derivatives. These compounds can be used as medicaments for the treatment of physiological and/or pathophysiological conditions in mammals, in particular for the treatment of various tumors.Type: GrantFiled: March 19, 2010Date of Patent: June 25, 2013Assignee: Aeterna Zentaris GmbHInventors: Eckhard Guenther, Olaf Schaefer, Michael Teifel, Klaus Paulini
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Publication number: 20130157997Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B?, X, Y, R1, R1?, R2, R2?, R3, R3?, R5, R5?, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: November 16, 2012Publication date: June 20, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
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Patent number: 8466294Abstract: 1-aza-3,7-dioxabicyclo[3.3.0]octane compounds, process for their preparation, their use as pro-fragrances, and washing and cleaning compositions, fabric softeners and cosmetics comprising them, and a process for prolonging the odor perception of such compositions.Type: GrantFiled: July 17, 2008Date of Patent: June 18, 2013Assignee: Henkel AG & Co. KGaAInventors: Ursula Huchel, Silvia Sauf, Thomas Gerke
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Publication number: 20130150321Abstract: A pharmaceutical dosage form is provided comprising a non-steroidal anti-inflammatory agent and acetaminophen, and methods for their use. In one embodiment, the dosage form is comprised of ibuprofen and acetaminophen as the sole pharmaceutically effective agents, wherein the ibuprofen and acetaminophen are in a weight ratio of about 12 parts:about 88 parts.Type: ApplicationFiled: February 6, 2013Publication date: June 13, 2013Applicant: MCNEIL-PPC, INC.Inventor: McNeil-PPC, Inc.
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Publication number: 20130150347Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: December 7, 2012Publication date: June 13, 2013Inventors: Klaus RUDOLF, Daniel BISCHOFF, Georg DAHMANN, Matthias GRAUERT, Raimund KUELZER, Bernd WELLENZOHN
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Publication number: 20130143841Abstract: Embodiments herein provide compounds and methods of making and using such compounds for prevention and treatment of multidrug resistant bacteria. In particular, embodiments are directed to anti-bacterial agents from benzo[d]heterocyclic scaffolds for prevention and treatment of multidrug resistant bacteria.Type: ApplicationFiled: January 29, 2013Publication date: June 6, 2013Applicant: UNIVERSITY OF NOTRE DAME DU LACInventor: UNIVERSITY OF NOTRE DAME DU LAC
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Publication number: 20130137687Abstract: The invention relates to a compound of formula (I) wherein A and R1 to R7 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: November 20, 2012Publication date: May 30, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8450304Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, and R4 are as defined in the specification. The invention also comprises pharmaceutical compositions comprising the compounds of formula (I) and methods of preventing, treating or ameliorating a CCR2 mediated syndrome, disorder or disease, for example, type II diabetes, obesity or asthma, by administering the compounds of formula (I).Type: GrantFiled: December 9, 2009Date of Patent: May 28, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Xuqing Zhang, Heather Rae Hufnagel, Cuifen Hou, Dana L. Johnson, Zhihua Sui, Barry Fegely, David Breslin
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Patent number: 8450313Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: GrantFiled: May 22, 2012Date of Patent: May 28, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Publication number: 20130131044Abstract: The invention provides compounds of Formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.Type: ApplicationFiled: May 10, 2011Publication date: May 23, 2013Inventors: Tong-Shuang Li, Ernest J. Mceachern, David J. Vocadlo, Yuanxi Zhou, Yongbao Zhu
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Patent number: 8445522Abstract: Disclosed is a harmful arthropod control composition comprising, as an active ingredient, a fused heterocyclic compound represented by formula (1) [wherein A1 and A2 independently represent a nitrogen atom or the like; R1 and R4 independently represent a halogen atom or the like; R2 and R3 independently represent a halogen atom or the like; R5 and R6 independently represent a linear C1-C6 hydrocarbon group which may be substituted, or the like (provided that both R5 and R6 cannot represent a hydrogen atom simultaneously); and n represents 0 or 1]. The harmful arthropod control composition has an excellent efficacy to control harmful arthropods.Type: GrantFiled: April 17, 2012Date of Patent: May 21, 2013Assignee: Sumitomo Chemical Company, LimitedInventors: Mitsuhiko Iwakoshi, Ippei Uemura
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Patent number: 8445480Abstract: Compounds having the structure of Formula I1 including pharmaceutically acceptable salts of the compounds, are potent CETP (cholesterol ester transfer protein) inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis Atherosclerosis and its clinical consequences, coronary heart disease (CHD), stroke and penpheral vascular disease, represent a truly enormous burden to the health care systems of the industrialized world In formula I, A-B is an arylamide moiety.Type: GrantFiled: June 16, 2008Date of Patent: May 21, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Julianne A. Hunt, Ramzi F. Sweis, Dooseop Kim, Florida Kallashi, Peter J. Sinclair
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Patent number: 8436028Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are potent CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In formula I, A-B is an arylamide moiety.Type: GrantFiled: June 16, 2008Date of Patent: May 7, 2013Assignee: Merck Sharp & Dohme CorpInventors: Julianne A. Hunt, Rogelio L. Martinez, Peter J. Sinclair, Ramzi F. Sweis
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Publication number: 20130109649Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.Type: ApplicationFiled: October 25, 2012Publication date: May 2, 2013Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha
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Patent number: 8431572Abstract: Described are compounds which inhibit, regulate and/or modulate kinase signal transduction, for example of Met kinase. The compounds are of the formulae A1 to A148 and B1 described herein, including 2-oxobenzoxazol-3-ylmethyl]phenyl}carbamate and 2-oxooxazolo[4,5-b]pyridin-3-ylmethyl)phenyl]carbamate compounds, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. Also described are compositions containing these compounds. Also described are methods for the treatment of diseases in which the inhibition, regulation and/or modulation of kinase signal transduction plays a role by administering these compounds.Type: GrantFiled: July 6, 2011Date of Patent: April 30, 2013Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
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Publication number: 20130102629Abstract: Compounds represented by formula (I) or pharmaceutically acceptable salts thereof, wherein A, B, B?, X, Y, R1, R2, R2?, R3, R3?, R4, R4?, R5, R5?, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: September 24, 2012Publication date: April 25, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
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Patent number: 8426455Abstract: The present invention provides a therapeutic agent for hyperlipidemia having an excellent effect of lowering the cholesterol and triglyceride level in blood plasma. The present invention relates to a prophylactic and/or therapeutic agent for hyperlipidemia, a prophylactic and/or therapeutic agent for obesity or diabetes mellitus, and a prophylactic and/or therapeutic agent for metabolic syndrome, each agent including a compound represented by the formula (1), or a salt thereof, and a statin, particularly pitavastatin, in combination.Type: GrantFiled: March 28, 2008Date of Patent: April 23, 2013Assignee: Kowa Company, Ltd.Inventors: Toshiaki Takizawa, Noriyuki Inoue, Katsutoshi Miyosawa
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Publication number: 20130096113Abstract: Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFR? kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: October 12, 2012Publication date: April 18, 2013Applicant: Ambit Biosciences CorporationInventor: Ambit Biosciences Corporation
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Publication number: 20130085150Abstract: Compounds represented by formula I or pharmaceutically acceptable salts thereof, wherein A, B, B?, X, Y, R1, R2, R2?, R3, R3?, R4, R4?, R5, R5?m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: September 24, 2012Publication date: April 4, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventors: Oswy Z. Pereira, John Maxwell, Youssef L. Bennani, Sanjoy Kumar Das, Laval Chan Chun Kong, Jagadeeswar T. Reddy, Simon Giroux, Kevin M. Cottrell, Mark A. Morris
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Publication number: 20130079374Abstract: The present invention provides a compound represented by the formula which is useful as an agent for the prophylaxis or treatment of diseases related to the action of melatonin, or a salt thereof and the like.Type: ApplicationFiled: October 23, 2012Publication date: March 28, 2013Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventor: TAKEDA PHARMACEUTICAL COMPANY LIMITE
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Publication number: 20130079339Abstract: The invention discloses compounds of formula I wherein Y is a group of formula A, B, C, D, or E: and W, Q, n, R1, R2, R3, U1-U5, J and K have the meanings given in the description. The compounds of formula I are TRPV1 antagonists and are useful as active ingredients of pharmaceutical compositions for the treatment of pain and other conditions ameliorated by the inhibition of the vanilloid receptor TRPV1.Type: ApplicationFiled: December 22, 2010Publication date: March 28, 2013Applicant: PHARMESTE S.R.L.Inventors: Mauro Napoletano, Marcello Trevisani, Maria Giovanna Pavani, Francesca Fruttarolo
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Publication number: 20130065902Abstract: The present invention relates to 3-(heteroaryl-amino)-1,2,3,4-tetrahydro-9H-carbazole derivatives of the formula (I), wherein R1, R2 and R3 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.Type: ApplicationFiled: March 21, 2011Publication date: March 14, 2013Applicant: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Heinz Fretz, Julien Hazemann, Sylvia Richard-Bildstein, Romain Siegrist
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Patent number: 8394816Abstract: Disclosed are methods of treating Waldenstrom's Macroglobulinemia comprising administering to the animal, a therapeutically effective amount of a heterocyclic compound of Formula I.Type: GrantFiled: December 5, 2008Date of Patent: March 12, 2013Inventors: Irene Ghobrial, Aldo Roccaro, Dharminder Chauhan, Kenneth Anderson, Michael Palladino
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Patent number: 8394794Abstract: The invention provides compounds of Formula (I) and (IV): as described herein, as well as salts thereof. The compounds have anti-cancer properties and/or chemosensitization properties.Type: GrantFiled: March 21, 2008Date of Patent: March 12, 2013Assignee: Regents of The University of MinnesotaInventors: Chengguo Xing, Jignesh Doshi
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Patent number: 8394799Abstract: Disclosed herein are an HIF-1 inhibitor, a method for the preparation thereof, and a pharmaceutical composition comprising the same as an active ingredient. The HIF-1 inhibitor shows anticancer activity thanks to the inhibition activity against HIF-1, a transcription factor which plays an important role in the growth and metastasis of cancer, but not to general cytotoxicity. Thus, the HIF-inhibitor and a pharmaceutically acceptable salt thereof can be used as a therapeutic for various cancers such as liver cancer; stomach cancer and breast cancer. Also, the compound having inhibition activity against HIF-1 is useful in the treatment of diabetic retinopathy and arthritis, which are aggravated by HIF-1-mediated VEGF expression.Type: GrantFiled: July 3, 2007Date of Patent: March 12, 2013Assignee: Korea Research Institute of Bioscience and BiotechnologyInventors: Jung Joon Lee, Jeong-Hyung Lee, Kyeong Lee, Young-Soo Hong, B. K. Shanthaveerappa, Yinlan Jin, Jin Hwan Kim, Xuejun Jin
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Publication number: 20130059845Abstract: The present disclosure relates to compounds that act as agonists of, or otherwise modulate the activity of, GPR131 and to their use in the treatment of various diseases. In particular embodiments, the structure of the compounds is given by Formula I: wherein the variables are as described herein. Related compositions, formulations and methods for the preparation of compounds of formula I are also described.Type: ApplicationFiled: August 24, 2012Publication date: March 7, 2013Inventors: Jiangao SONG, Phuongly Pham, Jingyuan Ma, Aaron Robert Novack, Imad Nashashibi, David W. G. Wone, Dong-Fang Shi, Xin Chen
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Publication number: 20130053412Abstract: The invention relates to cyclopentanecarboxamide derivatives of formula 1, to their use as Fatty Acid Synthase inhibitors, to methods for their therapeutic use and to pharmaceutical compositions containing them, wherein R1, R2, R3, LO, W, AR1, n are as defined in claim 1.Type: ApplicationFiled: October 15, 2010Publication date: February 28, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Joerg Kley, Bradford S. Hamilton, Juergen Mack, Norbert Redemann, Corinna Schoelch
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Patent number: 8377981Abstract: A unique class of N-acyl O-amino phenol prodrugs of CBI-TMI and CBI-indole2 were synthesized and shown to be prodrugs, subject to reductive activation by nucleophilic cleavage of a weak N—O bond, effectively releasing the free drug in functional cellular assays for cytotoxic activity approaching or matching the activity of the free drug, yet remain essentially stable to ex vivo DNA alkylation conditions. Most impressively, assessment of the in vivo antitumor activity of a representative O-(acylamino) prodrug, 8, indicate that they approach the potency and exceed the efficacy of the free drug itself (CBI-indole2), indicating that the inactive prodrugs not only effectively release the free drug in vivo, but that they offer additional advantages related to a controlled or targeted release in vivo.Type: GrantFiled: November 13, 2008Date of Patent: February 19, 2013Assignee: The Scripps Research InstituteInventor: Dale Boger
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Publication number: 20130035324Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the heterocyclic entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.Type: ApplicationFiled: August 17, 2010Publication date: February 7, 2013Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Simon Fraser Campbell
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Publication number: 20130030029Abstract: Provided herein are compounds, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof which have glucagon receptor antagonist or inverse agonist activity. Further, provided herein are pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. Moreover, provided herein are methods of making or manufacturing compounds disclosed herein, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or Co-crystals and prodrugs thereof.Type: ApplicationFiled: August 13, 2009Publication date: January 31, 2013Applicant: METABASIS THERAPEUTICS, INC.Inventors: Jorge E. Gomez-Galeno, Scott J. Hecker, Qun Dang, Mali Venkat Reddy, Zhili Sun, Matthew P. Grote, Thanh Huu Nguyen, Robert Huerta Lemus, Haiqing Li
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Publication number: 20130030027Abstract: The present invention is directed to hemi phorboxazole A: and its stereoisomers, as well as derivatives of hemi phorboxazole A of formula I: wherein ring A is aryl or a 5- or 6-membered heteroaryl optionally substituted with one or more of halogen, —OH, or —C1-6alkyl; and R is —CN, a 5- or 6-membered heteroaryl, or halogen; and the pharmaceutically acceptable salt forms thereof, in addition to methods of using these compounds.Type: ApplicationFiled: July 23, 2010Publication date: January 31, 2013Applicants: The Regents of the University of California, The Trustes of The University of PennsylvaniaInventors: Amos B. Smith, III, Zhuqing Liu, Anne-Marie L. Hogan, Doralyn S. Dalisay, Tadeusz F. Molinski
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Publication number: 20130023556Abstract: The present invention relates to compounds according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.Type: ApplicationFiled: September 14, 2012Publication date: January 24, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Melanie SCHULTZ, Kai Schiemann, JR., Wolfgang Staehle
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Patent number: 8354397Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.Type: GrantFiled: July 29, 2002Date of Patent: January 15, 2013Assignee: Curis, Inc.Inventors: Lee L. Rubin, Oivin Guicherit, Stephen Price, Edward Andrew Boyd
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Patent number: 8354400Abstract: The present invention provides benzoxazole compounds and pharmaceutically acceptable salts thereof and pharmaceutical compositions including the same. The present invention further provides methods of use as described herein.Type: GrantFiled: September 25, 2009Date of Patent: January 15, 2013Assignee: Eisai R&D Co., Ltd.Inventors: Wanjun Zheng, Mark Spyvee, Fabian Gusovsky, Sally T. Ishizaka
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Publication number: 20130005666Abstract: The NF-E2-related factor 2 (Nrf2) is a key transcriptional regulator of antioxidant defense and detoxification. To directly monitor stabilization of Nrf2 we fused its Neh2 domain, responsible for the interaction with its nucleocytoplasmic regulator, Keap1, to firefly luciferase (Neh2-luciferase). It is shown herein that Neh2 domain is sufficient for recognition, ubiquitination and proteasomal degradation of Neh2-luciferase fusion protein. The novel Neh2-luc reporter system allows direct monitoring of the adaptive response to redox stress and classification of drugs based on the time-course of reporter activation. The novel reporter was used to screen a library of compounds to identify activators of Nrf2. The most robust and yet non toxic Nrf2 activators found—nordihydroguaiaretic acid, fisetin, and gedunin-induced astrocyte-dependent neuroprotection from oxidative stress via an Nrf2-dependent mechanism.Type: ApplicationFiled: June 29, 2012Publication date: January 3, 2013Applicant: CORNELL UNIVERSITYInventors: Rajiv RATAN, Irina GAZARYAN, Natalya A. SMIRNOVA
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Publication number: 20120329775Abstract: The present invention provides compounds of formula (I) in which y, m, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: June 4, 2012Publication date: December 27, 2012Inventors: Rhonan Ford, Andrew Mather, Antonio Mete, Ian Millichip
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Patent number: 8338469Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for, using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.Type: GrantFiled: April 19, 2011Date of Patent: December 25, 2012Assignee: IRM LLCInventors: David C. Tully, Amab K. Chatterjee, Agnes Vidal, Hank Michael James Petrassi, Zhiwei Wang, Badry Bursulaya, Glen Spraggon
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Patent number: 8338477Abstract: The present disclosure is directed to compositions and methods which utilize the tetracycline scaffold, preferably the scaffold of tetracycline or minocycline, and which significantly lack antibiotic activity. The compounds have neuroprotective attributes without interfering with the drugs capacity to pass through the blood brain barrier. These compounds have neuroprotective activity because of their inhibition of neuronal cell cycle progression. The compounds are characterized in part by a fifth ring joining positions 9 and 10.Type: GrantFiled: July 10, 2009Date of Patent: December 25, 2012Assignee: NeuMedicsInventors: Iain W. Duncan, Edward A. Kesicki, Carl G. Osborne, William D. Schwieterman, Irina Jacobson