Additional Hetero Ring Which Is Not Part Of The Bicyclo Ring System Patents (Class 514/414)
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Publication number: 20150111940Abstract: The present invention relates to an ascorbic acid salt of sunitinib and a process for its preparation. The present invention further provides a crystalline Form I of an L-ascorbic acid salt of sunitinib.Type: ApplicationFiled: January 6, 2014Publication date: April 23, 2015Applicant: RANBAXY LABORATORIES LIMITEDInventors: Hari Babu MATTA, Mahavir Singh KHANNA, Mohan PRASAD
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Publication number: 20150111890Abstract: The present invention provides for compounds of formula (I) wherein A, Y, J, R1, R2, and R3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof,that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).Type: ApplicationFiled: April 19, 2013Publication date: April 23, 2015Inventors: Lisa A. Hasvold, Dachun Liu, Chang Hoon Park, John K. Pratt, George S. Sheppard, Le Wang
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Publication number: 20150110713Abstract: A method for treating cancer, preventing cancer or delaying the progression of a cancer in an animal or human comprising the step of: administering to the animal or the human having a cancer a composition in an amount effective to treat cancer, prevent cancer or delay the progression of cancer in the animal or the human. The composition comprises a pharmaceutically acceptable excipient, and ascorbate which is joined to a carrier structure containing an anti-cancer active agent, said carrier structure being capable of releasing the anti-cancer agent in the presence of a reactive oxygen species.Type: ApplicationFiled: December 22, 2014Publication date: April 23, 2015Inventors: Anthony Manganaro, Karen Rockwell
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Patent number: 9012659Abstract: The present invention relates to a compound of formula (I) wherein R1, R2 and R3 are as defined in the description and the physiologically acceptable salts thereof as well as the physiologically acceptable solvates of the compounds of formula I and of the salts thereof. The compounds of formula I are suitable for treating tumors.Type: GrantFiled: December 10, 2010Date of Patent: April 21, 2015Assignee: Johannes Gutenberg—Universitat MainzInventors: Gerd Dannhardt, Jan-Peter Kramb, Stanislav Plutizki
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Publication number: 20150105375Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.Type: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Inventors: Ralf ANDERSKEWITZ, Florian BINDER, Matthias GRAUERT, Marc GRUNDL, Peter Wilhelm HAEBEL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS, Viktor VINTONYAK
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Publication number: 20150104387Abstract: Prostate-specific membrane antigen (PSMA) targeting compounds are described. Uses of the compounds for imaging, therapy, cell sorting, and tumor mapping are also described.Type: ApplicationFiled: April 2, 2014Publication date: April 16, 2015Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: MARTIN G. POMPER, RONNIE C. MEASE, YING CHEN, Sangeeta Ray
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Patent number: 9006256Abstract: The present invention provides pharmaceutical compositions and therapeutic methods for treating diseases such as multiple endocrine neoplasia type IIA, multiple endocrine neoplasia type IIB, familial medullary thyroid carcinoma, thyroid carcinoma, papillary thyroid carcinoma, sporadic medullary thyroid carcinoma, Hirschsprung disease, pheochromocytoma, parathyroid hyperplasia and mucosal neuromas of the gastrointestinal tract. The therapeutic methods and pharmaceutical compositions use a RET kinase inhibiting substance, such as 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide and pharmacologically acceptable salts thereof, and involve a step of administering the RET kinase inhibiting substance to a patient.Type: GrantFiled: April 8, 2011Date of Patent: April 14, 2015Assignee: Eisai R&D Management Co., Ltd.Inventor: Junji Matsui
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Publication number: 20150099012Abstract: The present invention relates to a method for increasing retrovirus transcription in an infected eukaryotic cell, comprising increasing Wnt pathway signaling in said cell such that transcription of said retrovirus is increased. Also, the present invention relates to a method of treating a subject infected with a retrovirus, said method comprising administering to said subject an activator of the Wnt pathway in an amount that increased Wnt pathway signaling in resting memory CD4+ T cells of said subject such that the retroviral long terminal repeat (LTR) in said cells is activated or de-repressed.Type: ApplicationFiled: March 1, 2013Publication date: April 9, 2015Inventor: Tokameh Mahmoudi
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Publication number: 20150099746Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: October 16, 2014Publication date: April 9, 2015Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone
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Publication number: 20150093391Abstract: A method of treating cancer or metastasis is provided involving administering at least one oncostatin M (OSM) antagonist to a subject, wherein the subject has been diagnosed with cancer. Administration of an OSM antagonist such as a small molecule pharmaceutical is provided as well as an anti-OSM antibody, an anti-OSM aptamer, and an OSM mRNA antagonist. The OSM antagonists were found to inhibit or prevent tumor cell detachment, proliferation and metastasis in several cancer types.Type: ApplicationFiled: September 5, 2014Publication date: April 2, 2015Applicant: BOISE STATE UNIVERSITYInventors: Cheryl Jorcyk, Dong Xu
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Publication number: 20150094330Abstract: The invention provides compositions and methods for wound healing and scar reduction. The compositions and methods of the invention include at least one EP4 agonist set forth herein. Wounds and or scars that can be treated by the compositions and methods of the invention can arise from events such as surgery, trauma, disease, mechanical injury, burn, radiation, poisoning, and the like.Type: ApplicationFiled: September 26, 2014Publication date: April 2, 2015Inventors: Yariv Donde, Jeremiah H. Nguyen
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Publication number: 20150094304Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: December 11, 2014Publication date: April 2, 2015Inventors: SARA SABINA HADIDA RUAH, PETER DIEDERIK JAN GROOTENHUIS, FREDRICK F. VAN GOOR, JINGLAN ZHOU, BRIAN RICHARD BEAR, MARK THOMAS MILLER, JASON MC CARTNEY, MEHDI MICHEL DJAMEL NUMA
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Patent number: 8993615Abstract: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.Type: GrantFiled: August 8, 2009Date of Patent: March 31, 2015Assignee: The Johns Hopkins UniversityInventors: Donald J. Zack, Zhiyong Yang, Cynthia Berlinicke, Harry Quigley
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Publication number: 20150087687Abstract: The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutically active agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to therapeutically active agents selected from the group consisting of: (i) indirubin; (ii) an analog of indirubin; (iii) a derivative of indirubin or of an analog of indirubin; and (iv) a pharmaceutical composition comprising indirubin, an analog of indirubin, or a derivative of indirubin or of an analog of indirubin, especially meisoindigo.Type: ApplicationFiled: March 22, 2013Publication date: March 26, 2015Inventor: Dennis BROWN
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Patent number: 8987320Abstract: The present invention relates to solid salt forms of the 3-pyrrole substituted 2-indolinone compound 5-[5-fluoro-2-oxo-1, 2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-pirrolidin-1-yl-ethyl)-amide. It also relates to polymorphs of the phosphate salt of the amide. The invention further relates to the use of the salts and polymorphs in the treatment of protein kinase related disorders.Type: GrantFiled: February 6, 2012Date of Patent: March 24, 2015Assignee: Zoetis LLCInventors: Changquan C. Sun, Michael Hawley
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Patent number: 8986993Abstract: A SMAC mimetic and pharmaceutical compositions thereof and methods of use.Type: GrantFiled: November 8, 2013Date of Patent: March 24, 2015Assignee: TetraLogic Pharmaceuticals CorporationInventors: Stephen M. Condon, Yijun Deng, Matthew G. LaPorte, Susan R. Rippin
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Publication number: 20150079111Abstract: Mechanisms for complications of renal failure and processes for treating the same are disclosed. They include contacting a biological fluid (e.g. blood) with a filter body, the filter body having immobilized thereon either a CD36 receptor or a CD36 receptor fragment or a SCARB1 receptor or a SCARB1 receptor fragment, the blood having a reduced quantity of oxidatively modified proteins after contacting the filter body. They also include administering an antagonist drug to a patient that blocks the binding activity of the RAGE receptor or the CD36 receptor or the SCARB1 receptor. Diagnostic methods are also provided.Type: ApplicationFiled: June 5, 2013Publication date: March 19, 2015Inventor: Jonas AXELSSON
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Publication number: 20150080381Abstract: Method of treating alopecia and acne with are disclosed.Type: ApplicationFiled: April 12, 2013Publication date: March 19, 2015Inventors: Mark G. Currie, Yueh-tyng Chien
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Publication number: 20150080349Abstract: The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect. In another embodiment, the compounds of the present invention are able to act in a manner which disturbs or inhibits the naturally occurring ligand-protein binding system in quorum sensing bacteria; that is, they produce an antagonistic effect. The compounds of the present invention comprise N-acylated-homoserine lactones (AHLs) comprised of a wide range of acyl groups.Type: ApplicationFiled: July 10, 2014Publication date: March 19, 2015Inventors: Helen E. BLACKWELL, Grant D. GESKE, Jennifer C. CAMPBELL
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Publication number: 20150057267Abstract: The invention provides a method for treating viral infections and coinfections through the use of inhibitory agents that prevent a unique viral structural protein motifs from binding to host proteins from the clathrin adaptor proteins family and subsequently preventing viral replication.Type: ApplicationFiled: December 6, 2012Publication date: February 26, 2015Applicant: The Board of Trustees of the Leland Stanford Junior universityInventors: Shirit Einav, Rina Barouch-Bentov, Gregory Neveu, Amotz Zivav
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Patent number: 8957093Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), inhibit kinase-mediated, e.g., cdk5-mediated, phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. In methods of treatment of these conditions using a compound of the invention, the compound can avoid producing side effects of significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, in the patient receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.Type: GrantFiled: June 6, 2012Date of Patent: February 17, 2015Assignee: The Scripps Research InstituteInventors: Theodore Mark Kamenecka, Patrick R. Griffin, Marcel Koenig, Alice Asteian, Anne-Laure Blayo, Yuanjun He, Youseung Shin
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Patent number: 8957103Abstract: The present invention relates to 3-(Indolyl)- and 3-(azaindolyl)-4-phenylmaleimide compounds of formula (I) wherein R1, R2 and R3 are as defined in the description, and the physiologically acceptable salts, solvates and solvates of the salts of the compounds of formula (I). The compounds of formula (I) are suitable for treating tumors.Type: GrantFiled: December 15, 2011Date of Patent: February 17, 2015Assignee: Johannes Gutenberg—Universitat MainzInventors: Gerd Dannhardt, Stanislav Plutizki, Christopher Ganser, Eva Lauermann
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Publication number: 20150045404Abstract: The invention provides a compound of formula (I): wherein R1-R5 have any of the values defined in the specification. The compounds are useful for the treatment of cancer and other diseases.Type: ApplicationFiled: March 25, 2013Publication date: February 12, 2015Inventors: John Kodet, Jeffrey D. Neighbors, David F. Wiemer
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Publication number: 20150044293Abstract: Radioprotector compounds including 3,3?-diindolylmethane (DIM) analogs, are provided. Further provided are methods for their use in reducing or preventing radiation damage, killing a tumor cell and protecting a non-tumor cell, and treating cancer.Type: ApplicationFiled: March 14, 2013Publication date: February 12, 2015Applicant: Georgetown UniversityInventors: Eliot M. Rosen, Milton Brown, Saijun Fan, Thomas Walls, Kathryn E. Ditmer
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Patent number: 8952049Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: February 28, 2013Date of Patent: February 10, 2015Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Sabina Hadida Ruah, Peter Diederik Jan Grootenhuis, Fredrick F. Van Goor, Jinglan Zhou, Brian Richard Bear, Mark Thomas Miller, Jason McCartney, Mehdi Michel Djamel Numa
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Patent number: 8952050Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: September 25, 2013Date of Patent: February 10, 2015Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Sabina Hadida Ruah, Peter Diederik Jan Grootenhuis, Fredrick F. Van Goor, Jinglan Zhou, Brian Richard Bear, Mark Thomas Miller, Jason McCartney, Mehdi Numa, Xiaoqing Yang
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Patent number: 8946282Abstract: A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer.Type: GrantFiled: April 3, 2013Date of Patent: February 3, 2015Assignee: Annji Pharmaceutical Co., Ltd.Inventors: Ji-Wang Chern, Ajit Dhananjay Jagtap, Hsiao-Chun Wang, Grace Shiahuy Chen
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Patent number: 8946283Abstract: Disclosed is a composition for preventing or treating obesity, dyslipidemia, fatty liver or diabetes, containing an indole-3-carbinol derivative as an active ingredient. The indole-3-carbinol derivative of the present disclosure can be usefully used as a pharmaceutical or functional food composition for preventing or treating obesity, dyslipidemia, fatty liver or diabetes by inhibiting differentiation of preadipocytes and reducing accumulation of triglyceride in cells.Type: GrantFiled: December 27, 2011Date of Patent: February 3, 2015Assignees: Industry-Academic Cooperation Foundation, Yonsei University, Korea Health Industry Development Institute (KHIDI)Inventors: Tae Sun Park, Gyoon Hee Han
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Publication number: 20150031685Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, and R6 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.Type: ApplicationFiled: March 5, 2013Publication date: January 29, 2015Applicant: Dr. Reeddy's Laboratories Ltd.Inventors: Pradip Kumar Sasmal, Chintakunta Vamseekrishna, Vijay Potluri, Ashok Tehim, Yonghua Gai, Hang Zhang
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Publication number: 20150031670Abstract: Compounds of the formula (I), in which R1, R3, R5, R6, R7, R, X and Y have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.Type: ApplicationFiled: March 21, 2013Publication date: January 29, 2015Applicant: MERCK PATENT GmbHInventors: Timo Heinrich, Frank Zenke, Mireille Krier, Manja Friese-Hamim, Jeyaprakashnarayanan Seenisamy
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Publication number: 20150018301Abstract: Leucine-rich repeat kinase-2 (LRRK2) mutations are a common cause of Parkinson's disease. Inhibitors of LRRK2 kinase that are protective in in vitro and in vivo models of LRRK2-induced neurodegeneration were identified. The presently disclosed subject matter establishes that LRRK2-induced degeneration of neurons in vivo is kinase dependent and that LRRK2 kinase inhibition provides a potential new neuroprotective paradigm for treating Parkinson's disease.Type: ApplicationFiled: November 8, 2010Publication date: January 15, 2015Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Byoung Dae Lee, Ted M. Dawson, Valina L. Dawson, Andrew B. West, Howard Federoff
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Publication number: 20150018310Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: September 29, 2014Publication date: January 15, 2015Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone, Julie Wurster
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Publication number: 20150018380Abstract: The present invention provides methods for obtaining specific and non-toxic inhibitors of AID nuclear import. The methods comprise a primary screen and a counter screen to identify a pool of AID specific nuclear import inhibitors that do not have off-target of toxic effects. AID specific nuclear import inhibitors identified by the screens of the invention prevent nuclear entry, limit the access of AID to genomic DNA, and inhibit AID mutagenic activity. Preparations, including pharmaceutical preparations, comprising specific nuclear import inhibitors, used for example, to inhibit cancer progression, are also encompassed in the invention.Type: ApplicationFiled: February 7, 2013Publication date: January 15, 2015Applicant: University of RochesterInventor: Harold C. Smith
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Publication number: 20150010619Abstract: The present invention generally relates to the transdermal delivery of various compounds. In some aspects, transdermal delivery may be facilitated by the use of a hostile biophysical environment. One set of embodiments provides a composition for topical delivery comprising ergopeptines, triptans, and other compounds, including salts and derivatives of these, and optionally, a hostile biophysical environment and/or a nitric oxide donor. In some cases, the composition may be stabilized using a combination of a stabilization polymer (such as xanthan gum, KELTROL® BT and/or KELTROL® RD), propylene glycol, and a polysorbate surfactant such as Polysorbate 20, which combination unexpectedly provides temperature stability to the composition, e.g., at elevated temperatures such as at least 40° C. (at least about 104° F.), as compared to compositions lacking one or more of these.Type: ApplicationFiled: September 26, 2014Publication date: January 8, 2015Applicant: Strategic Science & Technologies, LLCInventor: Eric T. Fossel
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Publication number: 20150005275Abstract: The present invention discloses compounds according to Formula I: wherein R1, R2, R3, L, and the subscript m are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions, and methods of treatment using the same, for the treatment of cystic fibrosis by administering a compound of the invention.Type: ApplicationFiled: May 6, 2014Publication date: January 1, 2015Inventors: Steven Emiel Van der Plas, Oscar Mammoliti, Christel Jeanne Marie Menet, Giovanni Alessandro Tricarico, Ann De De Blieck, Caroline Martine Andrée Marie Joannesse, Hans Kelgtermans, Tom Roger Lisette De Munck
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Publication number: 20150005344Abstract: The present invention relates to solid forms of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1) in substantially crystalline form (Form A) or amorphous form, pharmaceutical compositions thereof, and methods of treatment therewith.Type: ApplicationFiled: June 27, 2014Publication date: January 1, 2015Inventors: Ali Keshavarz-Shokri, Beili Zhang, Tim Edward Alcacio, Elaine Chungmin Lee, Yuegang Zhang, Mariusz Krawiec
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Publication number: 20150004626Abstract: The present invention relates to a method for labeling or targeting cells whose plasma membrane has lost integrity, such as dead cells, such as for discriminating between live cells and cells whose plasma membrane has lost integrity; to an embodiment of the method for determining one or more values of one or more parameters of cells of a biological sample; to use of the method in an assay for screening drugs for therapy such as cancer therapy; to use of the method to monitor and/or determine the effectiveness of a therapy; to an assay kit; to a complex; to the complex for use as a medicament; to the complex for use in treatment of cancer(s) and/or plaque(s) and/or regeneration and/or supporting the immune system; and, to a dead cell.Type: ApplicationFiled: February 6, 2013Publication date: January 1, 2015Inventors: Markwin Hendrik Maring, Clemens Waltherus Gerardus Löwik, Ermond Reijer Van Beek
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Patent number: 8921410Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the ?4?2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).Type: GrantFiled: July 23, 2012Date of Patent: December 30, 2014Assignee: Targacept, Inc.Inventors: Anatoly Mazurov, Lan Miao, Yunde Xiao
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Patent number: 8921560Abstract: Indoles having inhibitory activity on RSV replication and having the formula I the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.Type: GrantFiled: December 16, 2011Date of Patent: December 30, 2014Assignee: Janssen R&D IrelandInventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
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Publication number: 20140371274Abstract: The present invention relates to novel compounds, their use in the prevention or treatment of symptoms and disorders associated with the bradykinin B1 pathway and pharmaceutical compositions containing them.Type: ApplicationFiled: June 13, 2014Publication date: December 18, 2014Inventors: Andrea Rosario BECCARI, Gianluca BIANCHINI, Chiara LIBERATI, Michela FANI', Mara ZIPPOLI
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Patent number: 8912199Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: October 21, 2013Date of Patent: December 16, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
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Patent number: 8912141Abstract: A combined therapy which utilizes hydroxychloroquine and GNS-227: for the treatment of an HCV-related disease, including HCV chronic infection, is disclosed. Further disclosed is pharmaceutical composition (e.g., as a unit dosage form) comprising hydroxychloroquine and GNS-227.Type: GrantFiled: June 21, 2012Date of Patent: December 16, 2014Assignee: Panmed Ltd.Inventor: Philippe Halfon
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Publication number: 20140364476Abstract: Disclosed are 4-amino-2-butenamides of Formula (I) having pharmacological activity, pharmaceutical compositions containing them, and methods for the treatment of diseases mediated by the cathepsin C enzyme such as chronic obstructive pulmonary disease.Type: ApplicationFiled: August 21, 2014Publication date: December 11, 2014Inventors: Christopher E. NEIPP, Michael R. PALOVICH
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Patent number: 8906913Abstract: The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.Type: GrantFiled: June 22, 2010Date of Patent: December 9, 2014Assignee: Panacea Biotec LimitedInventors: Rajesh Jain, Sanjay Trehan, Jagattaran Das, Gurmeet Kaur, Sandeep Kanwar, Nishan Singh, Gurmeet Kaur Nanda, Sitaram Kumar Magadi, Sudhir Kumar Sharma
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Patent number: 8906911Abstract: Disclosed herein are chemokine receptor antagonists of formula (I) wherein R1, R2, and R3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.Type: GrantFiled: March 29, 2013Date of Patent: December 9, 2014Assignee: AbbVie Inc.Inventors: Michael D. Meyer, Xueqing Wang, Tao Guo, Robert Guo Ping Wei, Lijuan Jane Wang
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Publication number: 20140357634Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.Type: ApplicationFiled: August 14, 2014Publication date: December 4, 2014Applicant: GRÜNENTHAL GMBHInventors: BERT NOLTE, WOLFGANG SCHRÖDER, KLAUS LINZ, WERNER ENGLBERGER, HANS SCHICK, HEINZ GRAUBAUM, BIRGIT ROLOFF, SIGRID OZEGOWSKI, JÓZSEF BÁLINT, HELMUT SONNENSCHEIN
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Patent number: 8900565Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.Type: GrantFiled: November 21, 2012Date of Patent: December 2, 2014Assignee: Pharmacyclics, Inc.Inventors: Joseph J. Buggy, Sriram Balasubramanian, Erik Verner, Vincent W. F. Tai, Chang-Sun Lee
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Publication number: 20140348746Abstract: The invention relates to a family of compounds that comprise fluorescent cyanine dyes. The compounds are near infrared absorbing heptamethine cyanine dyes with a 4,4-disubstituted cyclohexyl ring as part of the polymethine chromophore. The compounds are generally hydrophilic and can be chemically linked to biomolecules, such as proteins, nucleic acids, and therapeutic small molecules. The compounds can be used for imaging in a variety of medical, biological and diagnostic applications.Type: ApplicationFiled: March 17, 2014Publication date: November 27, 2014Applicant: VisEn Medical, Inc.Inventor: Narasimhachari Narayanan
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Publication number: 20140349918Abstract: The present invention relates to xanthone analogs. Such compounds may be used in the treatment of bacterial infections.Type: ApplicationFiled: September 10, 2012Publication date: November 27, 2014Applicants: Singapore Health Services Pte Ltd., Agency for Science, Technology and ResearchInventors: Hanxun Zou, Lakshminiarayan Rajanmani, Lei Zhou, Chang Chui Charles Tang, Jun Jie Koh, Tiang Hwee Donald Tan, Chandra Verma, Roger W. Beuerman, Shouping Liu, Saraswathi Padmanabhan
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Publication number: 20140349987Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo carboxamide compounds of Formula (1) and the enantiomers, diastereomers, N-oxides, tautomers, solvates and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: December 3, 2012Publication date: November 27, 2014Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann