Enzyme Inactivation By Chemical Treatment Patents (Class 435/184)
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Publication number: 20140296207Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the isoquinolone entities, and methods of using these chemical entities for treating diseases and conditions associated with P13 kinase activity are described herein.Type: ApplicationFiled: June 11, 2014Publication date: October 2, 2014Inventors: Pingda REN, Yi LIU, Liansheng LI, Troy Edward WILSON
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Publication number: 20140296288Abstract: The present disclosure relates to iminosugar derivatives and processes for the preparation thereof. The disclosed compounds have glycosidase inhibiting properties, and are useful in the treatment of various diseases, such as type 2 diabetes, neurodegenerative diseases or lysosomal storage disorders. The present disclosure also relates to pharmaceutical compositions containing the disclosed compounds and to their use as biochemical tools.Type: ApplicationFiled: July 19, 2012Publication date: October 2, 2014Applicants: UNIVERSITE PIERRE ET MARIE CURIE (PARIS 6), DORPHAN S.A., CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Matthieu Sollogoub, Yves Bleriot, Giuseppe Prencipe, Nicolas Auberger
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Publication number: 20140294763Abstract: The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.Type: ApplicationFiled: June 17, 2014Publication date: October 2, 2014Inventors: Robert Edward Babine, Shu Hui Chen, Ivan Collado-Cano, Maria Cristina Garcia Paredes, John Irvin Glass, Ling Jin, Jason Eric Lamar, Raymond Samuel Parker, III, Nancy June Snyder, Xicheng David Sun, Deqi Guo, Yvonne Yee Mai Yip, May Q. Wang, Victor Frantz, Mark Joseph Tebbe, Robert B. Perni, Luc J. Farmer
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Patent number: 8846932Abstract: Disclosed are methods and compositions for modulating the function of transcription factors, especially transcription factors that recruit epigenetic regulators (histone modifying enzymes) to specific DNA promoters. The targeted transcription factors include but are not limited to the myocyte enhancing factor (MEF2), the forkhead/winged helix transcription factor FOXP3 and the transcription factor GATA3. Also disclosed are small molecule modulators of MEF2 and its associated factors that include but not limited to histone deacetylases (HDACs), p300/CBP and Cabin1 and the therapeutic applications thereof.Type: GrantFiled: March 13, 2013Date of Patent: September 30, 2014Assignee: University of Southern CaliforniaInventors: Lin Chen, Nimanthi Jayathilaka, Aidong Han, Nicos A. Petasis
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Publication number: 20140288119Abstract: This invention provides a compound having the structure: wherein R1 is H, halogen, —NR5R6, —NR5—C(?O)—R6, —NH—C(?O)—OR7, —OR7, —NO2, —CN, —SR7, —SO2R7, —CO2R7, CF3, —SOR7, —POR7, —C(?S)R7, —C(?O)—NR5R6, —CH2—C(?O)—NR5R6, —C(?NR5)R6, —P(?O)(OR5)(OR6), —P(OR5)(OR6), —C(?S)R7, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, aryl, heteroaryl, or heterocyclyl, wherein R5, R6, and R7 and are each, independently, H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; m is an integer from 0 to 2; R2 and R3 are each, independently, H, halogen, —NH2, —CX3, —C(?O)OR8, C(?O)R8, —C(?O)NR9R10, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, heteroalkyl, aryl, heteroaryl, or heterocyclyl; wherein X is Cl, Br, or F; R8, R9 and R10 are each, independently, H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; Q is —Ar1—Z— or —Z—Ar1—Z—, wherein Ar1 is aryl or heteroaryl; and each occurrence of Z is independently present orType: ApplicationFiled: October 3, 2012Publication date: September 25, 2014Applicants: The Trustees of Columbia University in the City of New York, SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCHInventors: Ronald Breslow, Paul A. Marks
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Publication number: 20140288000Abstract: Compositions and methods are disclosed that relate to novel plasmin-inhibiting polypeptides that are structural variants of a human TFPI-2 Kunitz-type proteinase first inhibitor domain (KD1). The polypeptides are potent plasmin inhibitors and in certain embodiments have anti-fibrinolytic activity and/or decreased anti-coagulation activity relative to wild-type TFPI-2 KD1 and are not highly immunogenic. The plasmin-inhibiting polypeptides will find uses as anti-cancer agents, as antifibrinolytic agents, as protease inhibitors, and in other contexts.Type: ApplicationFiled: March 14, 2014Publication date: September 25, 2014Applicant: The Regents of the University of CaliforniaInventor: S. Paul Bajaj
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Publication number: 20140288045Abstract: Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.Type: ApplicationFiled: March 14, 2014Publication date: September 25, 2014Inventors: Pingda Ren, Yi Liu, Liansheng Li, Jun Feng, Tao Wu
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Publication number: 20140286937Abstract: We provide an antibody capable of binding to an intracellular PRL-I or PRL-3 polypeptide, in which the antibody is capable of binding to an epitope bound by antibody 269, antibody 223 or antibody 318. Such anti-PRL antibodies may be capable of binding to intracellular PRL-I or PRL-3. They may be suitable for use as therapies against cancer or metastasis thereof, or in clinical diagnosis to identify PRL-3 or PRL-I positive patients.Type: ApplicationFiled: March 18, 2014Publication date: September 25, 2014Applicant: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCHInventor: Qi Zeng
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Publication number: 20140286859Abstract: The invention includes stable multimeric, particularly dimeric, forms of PSMA protein, compositions and kits containing dimeric PSMA protein as well as methods of producing, purifying and using these compositions. Such methods include methods for eliciting or enhancing an immune response to cells expressing PSMA, including methods of producing antibodies to dimeric PSMA, as well as methods of treating cancer, such as prostate cancer.Type: ApplicationFiled: September 10, 2012Publication date: September 25, 2014Applicants: PSMA Development Company, LLC, Amgen Fremont Inc.Inventors: Paul J. Maddon, Gerald P. Donovan, William C. Olson, Norbert Schuelke, Jason Gardner, Dangshe Ma, Jaspal S. Kang, Larry Green
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Publication number: 20140275224Abstract: Compounds and methods are provided for enhancing or boosting the transfection rate or efficiency of mammalian cells by foreign DNA, such as bacterial plasmid DNA. Compounds, including natural products and inventive synthetic compounds can increase the effectiveness of uptake and incorporation of foreign DNA by mammalian cells, such as human cells, by suppression of DNA cytosine deamination, which is believed to be a mechanism by which these cells eliminate foreign DNA. Inhibition of the cytosine deaminase enzymes by compounds as described herein serves to provide more effective transfection of eukaryotic cells by plasmids including engineered gene sequences. Transfection can be used to study cellular processes, or to cure genetic diseases in human patients. The inventive materials and methods increase the efficiency and effectiveness of such transfection techniques.Type: ApplicationFiled: November 3, 2011Publication date: September 18, 2014Applicant: Regents of the University of MinnesotaInventors: Reuben S. Harris, Daniel A. Harki, Angela L. Perkins-Harki, Michael A. Carpenter, Ming Li
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Publication number: 20140275055Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventors: Rajinder Singh, Matthew Duncton, Jing Zhang, Salvador Alvarez, Kin Tso, Sacha Holland, Rose Yen, Rao Kolluri, Thilo Heckrodt, Yan Chen, Esteban Masuda, Hui Li, Donald G. Payan
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Publication number: 20140275031Abstract: The present invention provides piperidin-4-yl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase 1 (JAK1) and are useful in the treatment of diseases related to the activity of JAK1 including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: ApplicationFiled: May 28, 2014Publication date: September 18, 2014Applicant: INCYTE CORPORATIONInventors: Taisheng Huang, Chu-Biao Xue, Hui-Yin Li, Qun Li, Anlai Wang, Lingquan Kong, Hai Fen Ye, Wenqing Yao, James D. Rodgers, Stacey Shepard, Haisheng Wang, Lixin Shao
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Publication number: 20140275165Abstract: The present invention relates to compounds with activity as BACE1 and NF?B modulators, and methods for treating, preventing, or ameliorating neurodegenerative diseases, such as Alzheimer's disease. The present invention is also directed to the treatment of diseases related to dysfunction of cell proliferation, the immune system and/or inflammation using such compounds or pharmaceutical compositions containing such candidate compounds.Type: ApplicationFiled: March 24, 2014Publication date: September 18, 2014Applicant: The Trustees of Columbia University in the City of New YorkInventors: Donald W. Landry, Tae-Wan Kim, Shi-Xian Deng, Gangli Gong, Jeremy C. Hwang, Yuli Xie, Yidong Liu, Kirsten Alison Rinderspacher
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Publication number: 20140275072Abstract: The invention relates to compounds of the formula (I) in which R1, L and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formulae (II) and (III) and optionally conversion of a base or acid of the compounds of the formula (I) into a salt thereof.Type: ApplicationFiled: October 30, 2012Publication date: September 18, 2014Applicant: Merck Patent GmbHInventors: Werner Mederski, Thomas Fuchss, Ulrich Emde, Hans-Peter Buchstaller
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Patent number: 8835423Abstract: The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: GrantFiled: September 20, 2013Date of Patent: September 16, 2014Assignee: Incyte CorporationInventors: Argyrios G. Arvanitis, James D. Rodgers, Andrew P. Combs, Richard B. Sparks, Darius J. Robinson
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Publication number: 20140256016Abstract: Aminopyridine compounds, as can be used in conjunction with methods for modulation of nitric oxide synthase activity.Type: ApplicationFiled: March 6, 2014Publication date: September 11, 2014Applicant: Northwestern UniversityInventors: Richard B. Silverman, Qing Jing
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Publication number: 20140256754Abstract: Quinazoline derivatives 1-25, (2-[3,4-bis(methyloxy)phenyl]quinazolin-4-(3H)-one) and 2-[2-(ethyloxy)phenyl]quinazoline-4-(3H)-one) are reported as ?-glucuronidase inhibitors useful in the treatment of ?-glucuronidase hyperactivity disorders.Type: ApplicationFiled: March 7, 2013Publication date: September 11, 2014Inventors: Muhammad Iqbal Choudhary, Kahalid Mohammed KHAN, Nimra Naveed SHAIKH, Syed Muhammad SAAD, Sammer YOUSUF, Atta-ur Rahman
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Publication number: 20140249176Abstract: The present invention provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to stimulate the synthesis of proteins sufficient to consolidate long-term memory. The present invention also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to downregulate PKC.Type: ApplicationFiled: March 4, 2014Publication date: September 4, 2014Applicant: Blanchette Rockefeller Neurosciences InstituteInventor: Daniel L. Alkon
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Publication number: 20140249157Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables are as defined herein. Moreover, The compounds of this invention have formula I-A: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.Type: ApplicationFiled: March 7, 2014Publication date: September 4, 2014Inventors: Nadia Ahmad, Dean Boyall, Jean-Damien Charrier, Chris Davis, Rebecca Davis, Steven Durrant, Gorka Etxebarria I Jardi, Damien Fraysse, Juan-Miguel Jimenez, David Kay, Ronald Knegtel, Donald Middleton, Michael O'Donnell, Maninder Panesar, Francoise Pierard, Joanne Pinder, David Shaw, Pierre-Henri Storck, John Studley, Heather Twin
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Publication number: 20140249146Abstract: The present invention relates to 4-alkyl substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.Type: ApplicationFiled: October 4, 2012Publication date: September 4, 2014Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Francesco Casuscelli, Alessandra Badari, Sten Christian Orrenius, Claudia Piutti, Teresa Disingrini
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Publication number: 20140243348Abstract: Compositions and methods that are useful for the treatment of herpesvirus infection (including herpes simplex virii) are disclosed. Methods for identifying compounds useful for the treatment of herpesvirus infection are also disclosed.Type: ApplicationFiled: January 22, 2014Publication date: August 28, 2014Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventors: David M. Knipe, Kevin Bryant, David H. Dreyfus
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Publication number: 20140243347Abstract: The present invention relates to substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.Type: ApplicationFiled: October 4, 2012Publication date: August 28, 2014Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Francesco Casuscelli, Elena Casale, Marisa Montemartini, Claudia Piutti
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Publication number: 20140243320Abstract: A compound represented by the following general formula (1) or a salt thereof. R1 represents a halogen atom and so on; R2 and R3 each represent a hydrogen atom and so on; R4 and R5 each represent a hydrogen atom and so on, or R4 and R5 may form an oxo group; Ra and Rb each represent a lower alkyl group optionally having a substituent and so on, or they may bind to each other to form a nitrogen-containing heterocyclic ring which may be substituted by one or plural Rc; Rc represents an aryl group optionally having a substituent and so on; ring A represents a benzene ring and so on; and m represents 0, 1 or 2.Type: ApplicationFiled: July 12, 2012Publication date: August 28, 2014Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Takahiro Honda, Hiroshi Enomoto, Kenji Kawashima, Shinji Takaoka, Yasutaka Fujioka, Mamoru Matsuda, Koji Ohashi, Yukie Fujita, Shin-ichiro Hirai, Hiroaki Kurashima
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Publication number: 20140243338Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.Type: ApplicationFiled: February 28, 2014Publication date: August 28, 2014Inventors: Mimi L. Quan, Zilun Hu, Cailan Wang
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Publication number: 20140243382Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: May 12, 2014Publication date: August 28, 2014Applicant: Janssen Pharmaceutica NVInventors: Carl R. ILLIG, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth J. Wilson
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Publication number: 20140235675Abstract: There are provided 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: July 18, 2012Publication date: August 21, 2014Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Gianluca Mariano Enrico Papeo, Daniela Borghi, Michele Caruso, Helena Posteri, Mikhail Yurievitch Krasavin
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Publication number: 20140235705Abstract: A pharmaceutical composition comprises: a) polymorphic form M or tromethamine salt of Compound (1) represented by the following structural formula: and b) a filler. A method of preparing a pharmaceutical composition comprises: providing a mixture of Compound (1) and a filler to form the composition of Compound (1). A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of the pharmaceutical composition.Type: ApplicationFiled: January 24, 2014Publication date: August 21, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Nicholas Cardoso, Chong-Hui Gu, Peter A. Ojakovo, Tapan Sanghvi, Eric A. Simone, Marinus J. Verwijs
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Publication number: 20140235549Abstract: The present invention provides inventive polypeptides comprising a C terminal RAB binding domain (RabBD) of RAB family interacting proteins (FIPs) stabilized by peptide stapling, and pharmaceutical compositions thereof. Also provided are methods for modulating RAB function comprising contacting an inventive stapled polypeptide with a RAB protein, and methods of treatment associated with modulation of RAB activity. The present invention also provides methods of making the inventive stapled polypeptides by ring closing metathesis of unstapled polypeptide precursors.Type: ApplicationFiled: June 15, 2012Publication date: August 21, 2014Applicant: President and Fellows of Harvard CollegeInventors: Raymond E. Moellering, Gregory L. Verdine
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Publication number: 20140235703Abstract: Polymorph Forms M, H, P, X, and ZA of Compound (1) represented by the following structural formula: are described. A method of preparing polymorph Form M of Compound (1) includes stirring a mixture of Compound (1) and a solvent system that includes isopropanol, ethyl acetate, n-butyl acetate, methyl acetate, acetone, 2-butanone (methylethylketone (MEK)), or heptane, or a combination thereof at a temperature in a range of 10° C. to 47° C. to form From M of Compound (1). A method of preparing polymorph Form H of Compound (1) includes stirring a solution of Compound (1) at a temperature in a range of 48° C. to 70° C. to form Form H of Compound (1). A method of preparing polymorph Form P of Compound (1) includes stirring a mixture of Compound (1) and a solvent system that includes a solvent selected from the group consisting of dichloromethane and tetrahydrofuran (THF), and a mixture thereof at room temperature to form Form P of Compound (1).Type: ApplicationFiled: January 24, 2014Publication date: August 21, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Brian Luisi, David Willcox, Stefanie Roeper, Kan-Nian Hu, Hoa Q. Luong
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Publication number: 20140235704Abstract: A co-crystal of Compound (1) includes Compound (1) and a co-crystal former selected from the group consisting of urea, nicotinamide, and isonicotinamide, wherein Compound (1) is characterized by the following structural formula: A pharmaceutical composition includes such a co-crystal of Compound (1) and at least one pharmaceutically acceptable carrier or excipient.Type: ApplicationFiled: January 24, 2014Publication date: August 21, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventor: Brian Luisi
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Publication number: 20140234254Abstract: The present invention provides heteroaromatic derivatives and pharmaceutical acceptable salts and formulations thereof useful in modulating the protein kinase activity, especially phosphatidylinositol 3-kinases (PI3 kinases) and mTOR, and in modulating inter- and/or intra-cellular signaling activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: ApplicationFiled: February 15, 2014Publication date: August 21, 2014Applicants: SUNSHINE LAKE PHARMA CO., LTD., CALITOR SCIENCES, LLCInventor: Ning Xi
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Publication number: 20140234939Abstract: Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.Type: ApplicationFiled: December 23, 2013Publication date: August 21, 2014Applicant: Northwestern UniversityInventors: Richard B. Silverman, Hua Wang, Mohammad Khanfar
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Publication number: 20140235551Abstract: Novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies and have the general formula I: wherein R1, R2, R3, R4, R5 and R6 are as described herein.Type: ApplicationFiled: May 5, 2014Publication date: August 21, 2014Applicant: GENENTECH, INC.Inventors: Frederick COHEN, Lewis J. GAZZARD, Vickie Hsiao-Wei TSUI, John A. FLYGARE
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Publication number: 20140234333Abstract: The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases are therapeutically useful.Type: ApplicationFiled: April 8, 2014Publication date: August 21, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Ankush Argade, Sambaiah Thota, David Carroll, Arvinder Sran, Robin Cooper, Rajinder Singh, Kin Tso, Somasekhar Bhamidipati
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Publication number: 20140227225Abstract: The present invention discloses thioflavine S and primuline derivatives which inhibit hepatitis C virus helicase and protease activity. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are useful as antiviral agents. The present invention further relates to pharmaceutical compositions containing the aforementioned compounds and methods of treating an HCV infection.Type: ApplicationFiled: September 7, 2012Publication date: August 14, 2014Applicants: UWM RESEARCH FOUNDATION, INC., UNIVERSITY OF KANSASInventors: Jeffrey Aube, Brian Scott Jonathan Blagg, Kevin John Frankowski, David Norman Frick, Kelin Li, Frank John Schoenen
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Publication number: 20140228322Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: February 7, 2014Publication date: August 14, 2014Applicant: Celgene Avilomics Research, Inc.Inventors: Nadia Haq, Deqiang Niu, Russell C. Petter, Lixin Qiao, Juswinder Singh, Zhendong Zhu
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Publication number: 20140228361Abstract: The present invention relates to the field of medicine. Provided herein are aminoquinazoline derivatives, their salts and pharmaceutical formulations useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. Also provided herein are pharmaceutically acceptable compositions comprising the aminoquinazoline compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: ApplicationFiled: November 14, 2012Publication date: August 14, 2014Applicant: SUNSHINE LAKE PHARMA CO., LTD.Inventors: Jiancun Zhang, Yingjun Zhang, Weihong Zhang, Bing Liu, Jiquan Zhang, Jinlei Liu, Lu Zhang
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Publication number: 20140221374Abstract: Described herein are compounds, pharmaceutical compositions and methods for the inhibition of RAF kinase mediated signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human disease and disorders.Type: ApplicationFiled: March 16, 2012Publication date: August 7, 2014Applicant: Ruga CorporationInventors: Jean-Michel Vernier, Stephanie Hopkins, Pierre-Yves Bounaud, Patrick O'Connor, David Matthews, Steve Bender
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Publication number: 20140221336Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: February 5, 2014Publication date: August 7, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Marion W. Wannamaker, Francesco Salituro, Albert Pierce, Alex Aronov, Gabriel Martinez-Botella, Jian Wang, Luc Farmer, Mark Ledeboer, Tiansheng Wang, Randy Bethiel, Brian Ledford, Emilie Porter Huck
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Publication number: 20140220027Abstract: Antagonists of human proprotein convertase subtilisin-kexin type 9 (“PCSK9”) are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.Type: ApplicationFiled: April 14, 2014Publication date: August 7, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Jon H. Condra, Rose M. Cubbon, Holly A. Hammond, Laura Orsatti, Shilpa Pandit, Laurence B. Peterson, Joseph C. Santoro, Ayesha Sitlani, Dana D. Wood, Henryk Mach, Heidi Yoder Pixley, Sonia M. Gregory, Jeffrey T. Blue, Kevin Wang, Peizhi (Peter) Luo, Denise K. Nawrocki, Pingyu Zhong, Feng Dong, Yan Li
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Publication number: 20140221352Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: ApplicationFiled: April 10, 2014Publication date: August 7, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
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Patent number: 8796001Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: GrantFiled: June 19, 2012Date of Patent: August 5, 2014Assignee: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Zachary A. Buchan, Michael T. Sullenberger
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Publication number: 20140213620Abstract: In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.Type: ApplicationFiled: July 17, 2013Publication date: July 31, 2014Inventors: James Elliot Bradner, Ralph Mazitschek
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Publication number: 20140213574Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: April 16, 2014Publication date: July 31, 2014Applicant: Celgene Avilomics Research, Inc.Inventors: Juswinder Singh, Russell Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
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Publication number: 20140212431Abstract: The invention provides PCSK9-binding polypeptides and methods of using the same.Type: ApplicationFiled: December 19, 2013Publication date: July 31, 2014Applicant: GENENTECH, INC.Inventors: Daniel K. Kirchhofer, Yingnan Zhang, Andrew Scott Peterson, Wei Li, Monica Kong-Beltran, Lijuan Zhou
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Publication number: 20140213515Abstract: Macrocyclic compounds that specifically inhibit insulin degrading enzyme (IDE) are provided. Pharmaceutically acceptable salts, solvates, hydrates, stereoisomers, polymorphs, tautomers, isotopically enriched forms, and prodrugs of the macrocyclic IDE inhibitors are also described. Pharmaceutical compositions are also provided. In vivo and in vitro methods of using the IDE inhibitor, and pharmaceutical compositions comprising the IDE inhibitor, for example, for the inhibition of IDE in a subject exhibiting aberrant IDE activity, impaired insulin signaling, or insulin resistance, for example, a subject having diabetes, are also provided.Type: ApplicationFiled: June 29, 2012Publication date: July 31, 2014Applicant: President and Fellows of Harvard CollegeInventors: David R. Liu, Juan Pablo Maianti, Alan Saghatelian, Ralph E. Kleiner
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Publication number: 20140213591Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.Type: ApplicationFiled: December 23, 2013Publication date: July 31, 2014Applicant: Quanticel Pharmaceuticals, Inc.Inventors: Young K. Chen, Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
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Publication number: 20140206671Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: January 27, 2014Publication date: July 24, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Youssef Bennani, Tianseng Wang, Francesco Salituro, John P. Duffy
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Publication number: 20140205537Abstract: Provided herein are compounds that inhibit or partially inhibit the activity of leucine rich repeat kinases. Also provided herein are methods of treatment of CNS disorders comprising administration of inhibitors of leucine rich repeat kinases.Type: ApplicationFiled: June 22, 2012Publication date: July 24, 2014Applicant: ZENOBIA THERAPEUTICS, INC.Inventors: Pierre-Yves Bounaud, Vicki Nienaber, Ruo W. Steensma, John A. Lowe, III
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Publication number: 20140206686Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.Type: ApplicationFiled: January 17, 2014Publication date: July 24, 2014Inventors: Peter W. Glunz, Yan Zou, Mimi L. Quan