Additional Hetero Ring Which Is Not Part Of The Bicyclo Ring System Patents (Class 514/414)
  • Publication number: 20140039030
    Abstract: The invention relates to (among other things) polymer-des-ethyl sunitinib conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over des-ethyl sunitinib in unconjugated form.
    Type: Application
    Filed: December 23, 2011
    Publication date: February 6, 2014
    Applicant: NEKTAR THERAPEUTICS
    Inventors: Antoni Kozlowski, Sean M. Culbertson, Xiaoming Shen, Samuel P. Mcmanus, Mark A. Wilson
  • Publication number: 20140037622
    Abstract: Methods of treating a head and neck cancer are disclosed.
    Type: Application
    Filed: August 2, 2013
    Publication date: February 6, 2014
    Applicants: UCL BUSINESS PLC, FOUNDATION MEDICINE, INC.
    Inventors: Chris Hendrik Boshoff, Timothy Robert Fenton, Matthias Alexander Lechner, Philip James Stephens, Matthew J. Hawryluk, Roman Yelensky, Garrett Michael Frampton
  • Patent number: 8642624
    Abstract: Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like.
    Type: Grant
    Filed: November 15, 2011
    Date of Patent: February 4, 2014
    Assignee: Amgen Inc.
    Inventors: Guoqing Chen, Jeffrey A. Adams, Jean E. Bemis, Shon Booker, Guolin Cai, Lucian V. DiPietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Stephanie Geuns-Meyer, Michael K. Handley, Qi Huang, Joseph L. Kim, Tae-Seong Kim, Alexander S. Kiselyov, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Markian M. Stec, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael D. Croghan
  • Patent number: 8642770
    Abstract: The present invention provides an indole derivative having a melanin-concentrating hormone receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Grant
    Filed: January 5, 2011
    Date of Patent: February 4, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Shinichi Masada, Yoshito Terao, Toshiki Murata
  • Publication number: 20140031408
    Abstract: Biocompatible intraocular implants include a tyrosine kinase inhibitor and a biodegradable polymer that is effective to facilitate release of the tyrosine kinase inhibitor into the vitreous of an eye for an extended period of time. The therapeutic agents of the implants may be associated with a biodegradable polymer matrix, such as a matrix that is substantially free of a polyvinyl alcohol. The implants can be placed in an eye to treat or reduce the occurrence of one or more ocular conditions.
    Type: Application
    Filed: August 19, 2013
    Publication date: January 30, 2014
    Applicant: Allergan, Inc.
    Inventors: Jeffrey L. Edelman, Patrick M. Hughes, Thomas C. Malone, Gerald W. DeVries, Joan-En Chang-Lin, Jane-Guo Shiah, Thierry Nivaggioli, Lon T. Spada, Wendy M. Blanda
  • Publication number: 20140030224
    Abstract: The present invention relates to methods and pharmaceutical compositions for inhibiting influenza virus replication. More particularly, the present invention relates to a compound selected from the group consisting of Gemcitabine, Obatoclax Mesylate, Docetaxel, HA-14, Alsterpaullone, GSK3B inhibitor VIII, GSK3B inhibitor XV, Indirubin 3?- monoxime, L glutathione reduced, Fluocinolone acetonide, Tirofiban, Topotecan hydrochloride, Clofarabine, Vinblastine, Menadione Crystalline and derivatives or analogues thereof for use in the treatment of an influenza infection in a subject in need thereof.
    Type: Application
    Filed: April 10, 2012
    Publication date: January 30, 2014
    Applicant: UNIVERSITÉ CLAUDE BERNARD - LYON 1
    Inventors: Vincent Lotteau, Benoit De Chassey, Patrice Andre, Laurene Meyniel-Schicklin, Anne Aublin-Gex
  • Patent number: 8637567
    Abstract: This invention provides compounds, compositions and methods for treating a cognitive disorder or memory disorder in animals that result from aging or other neurodegenerative condition. In particular, compounds of this invention can stimulate neural cell growth, increased amounts of cells containing a key enzyme needed for production of the cholinergic neurotransmitter, and can improve memory and cognitive function in animals who have experienced a loss of memory or cognitive function.
    Type: Grant
    Filed: October 13, 2010
    Date of Patent: January 28, 2014
    Assignee: Neuren Pharmaceuticals Ltd.
    Inventors: Peter David Gluckman, Jian Guan, Mary-Anne Woodnorth, Margaret Anne Brimble
  • Patent number: 8637681
    Abstract: Provided are pyrrolyl substituted dihydroindol-2-one derivatives represented by formula (I), pharmaceutically acceptable salts or solvates of said derivatives, or solvates of said salts, which are effective tyrosine kinase inhibitors. Also provided are the preparation methods of the above compounds, pharmaceutical compositions containing these compounds, and the use of these compounds in manufacturing drugs useful for the treatment or adjunctive treatment of tumors medicated by tyrosine kinases or proliferation or migration of tumor cells driven by tyrosine kinases in mammals (including human).
    Type: Grant
    Filed: March 31, 2011
    Date of Patent: January 28, 2014
    Assignee: Qilu Pharmaceutical Co., Ltd.
    Inventors: Jingyi Wang, Chuanwen Fan, Long Zhang, Boyan Xu, Shousheng Yan, Zongru Guo, Minghui Zhang, Dong Lin, Zhantao Zhang, Haojie Zhou
  • Publication number: 20140024657
    Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 23, 2014
    Applicant: President and Fellows of Harvard College
    Inventors: Junying YUAN, Emily S. Hsu
  • Publication number: 20140024641
    Abstract: A method of treating exposure to organophosphate agents and preventing morbidity due to such exposure through the administration of a triptan compound to a subject.
    Type: Application
    Filed: January 7, 2013
    Publication date: January 23, 2014
    Inventors: David Reed HELTON, David Brian FICK, Ernest H. PFADENHAUER, James LUCOT
  • Publication number: 20140024646
    Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, R4, R5, Z1 and Z2 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
    Type: Application
    Filed: July 16, 2013
    Publication date: January 23, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Chaozhong Cai, David F. MCCOMSEY, Zhihua Sui, Fu-An Kang
  • Patent number: 8633239
    Abstract: The present invention relates to a novel process for the preparation of (R)-3-((1-methylpyrrolidin-2-yl)methyl)-5-(2-(phenylsulfonyl)ethyl)-1H-indole and its intermediates thereof.
    Type: Grant
    Filed: October 29, 2009
    Date of Patent: January 21, 2014
    Assignee: Biophore India Pharmaceuticals Private Limited
    Inventors: Manik Reddy Pullagurla, Jagadeesh Babu Rangisetty, Neelam Naidu, Nagaraju Maddela, Radha Nagarapu, Pulla Rao Polagani
  • Publication number: 20140011856
    Abstract: Provided are acid addition salts of (Z)—N-[2-(diethylamino)ethyl]-2-methyl-7-(1,2-dihydro-5-fluoro-2-oxo-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indol-3-carboxamide, wherein the salt comprising at least one of a number of salts including L-malate, hydrochloride, phosphate, L-tartrate, benzenesulfonate, sulfate, methanesulfonate, succinate, citrate, fumarate, p-toluenesulfonate, hydrobromate, L-mandelate, lactate, acetate or maleate salt. Also provided is a pharmaceutical composition comprising the salt compounds, and a method of treatment by administering a therapeutically effective amount of the salt compounds as preparation of medicaments.
    Type: Application
    Filed: September 11, 2013
    Publication date: January 9, 2014
    Applicant: JIANGSU SIMCERE PHARMACEUTICAL R&D Co., Ltd
    Inventors: Feng TANG, Qiu JIN, Wei LI, Tian ZHU, Yang HU, Feng SHAO
  • Publication number: 20140010760
    Abstract: The present invention provides a composition and method for targeting hypoxic tumor areas for detection or treatment or a treatment adjuvant for cancer. Specifically, a hypoxia targeting moiety is conjugated to a polymeric micelle containing imaging agents, therapeutic agents, or therapeutic adjuvants.
    Type: Application
    Filed: March 14, 2013
    Publication date: January 9, 2014
    Inventors: Brij P. Giri, Kristina Gregg, Pritam Singh, Dinesh J. Dagli, Anshu Giri
  • Publication number: 20140011850
    Abstract: A method of improving cognitive function or treating cognitive dysfunction is provided. The method is based on activating a kainate receptor or a glutamate GluR6 receptor by kainate or a glutamate GluR6 receptor activator such as an agonist. Additionally, a method of enhancing a learning ability by activating a kainate receptor such as the glutamate GluR6 receptor via kainate or a glutamate GluR6 receptor activator such as an agonist is provided.
    Type: Application
    Filed: June 26, 2013
    Publication date: January 9, 2014
    Inventors: Edi Barkai, Dietmar Schmitz
  • Publication number: 20140010866
    Abstract: 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: Application
    Filed: December 29, 2011
    Publication date: January 9, 2014
    Applicant: Strategic Science & Technologies, LLC
    Inventor: Eric T. Fossel
  • Publication number: 20140011822
    Abstract: This document provides methods and materials for reducing venous stenosis formation of an arteriovenous fistula or graft. For example, methods and materials for using VEGF inhibitors to reduce venous stenosis formation of arteriovenous fistulas or grafts are provided.
    Type: Application
    Filed: March 16, 2012
    Publication date: January 9, 2014
    Inventor: Sanjay Misra
  • Publication number: 20140011855
    Abstract: The invention relates to (among other things) polymer-semaxanib moiety conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over the semaxanib moiety in unconjugated form.
    Type: Application
    Filed: December 23, 2011
    Publication date: January 9, 2014
    Applicant: NEKTAR THERAPEUTICS
    Inventors: Jennifer Riggs-Sauthier, Stephanie Allums-Donald, Sean M. Culbertson
  • Patent number: 8623905
    Abstract: 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 (“CFFR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: April 26, 2010
    Date of Patent: January 7, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick F. van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Djamel Numa
  • Publication number: 20140005221
    Abstract: The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below.
    Type: Application
    Filed: January 30, 2012
    Publication date: January 2, 2014
    Applicant: SATO PHARMACEUTICAL CO., LTD.
    Inventors: Keita Nagai, Koh Nagasawa, Hirobumi Takahashi, Motoaki Baba, Shinichi Fujioka, Eri Kondoh, Kenichi Tanaka, Yoshiki Itoh
  • Publication number: 20140005181
    Abstract: The present disclosure relates to compounds and methods for treating a disease mediated by apelin.
    Type: Application
    Filed: June 20, 2013
    Publication date: January 2, 2014
    Applicant: Sanford-Burnham Medical Research Institute
    Inventors: Layton Smith, Anthony B. Pinkerton
  • Publication number: 20140005165
    Abstract: Disclosed are CCR2 antagonists of Formula (I) or pharmaceutically acceptable thereof, wherein R1, L1 and A are defined herein. Also disclosed are pharmaceutical compositions containing the compounds, methods of treatment using the compounds, and compositions to treat diseases or disorders associated with CCR2 activity.
    Type: Application
    Filed: March 14, 2012
    Publication date: January 2, 2014
    Inventors: Anilkumar G. Nair, Jose S. Duca, Michael P. Dwyer, Joseph A. Kozlowski, Stuart B. Rosenblum
  • Publication number: 20130345281
    Abstract: 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: Application
    Filed: December 15, 2011
    Publication date: December 26, 2013
    Applicant: JOHANNES GUTENBERG-UNIVERSITAT MAINZ
    Inventors: Gerd Dannhardt, Stanislav Plutizki, Christopher Ganser, Eva Lauermann
  • Publication number: 20130344165
    Abstract: This disclosure relates to compounds and compositions for forming bone and methods related thereto. In certain embodiments, the disclosure relates to methods of forming bone comprising implanting a bone graft composition comprising a growth factor such as BMP in a subject at a site of desired bone growth or enhancement in combination with a JAB1 blocker.
    Type: Application
    Filed: February 23, 2012
    Publication date: December 26, 2013
    Applicant: EMORY UNIVERSITY
    Inventors: Scott D. Boden, Sreedhara Sangadala
  • Publication number: 20130345236
    Abstract: A drug in a solubility-improved form is combined with a concentration-enhancing polymer in a sufficient amount so that the combination provides substantially enhanced drug concentration in a use environment relative to a control comprising the same amount of the same solubility-improved form of drug without the concentration-enhancing polymer.
    Type: Application
    Filed: June 11, 2013
    Publication date: December 26, 2013
    Inventors: William J. Curatolo, Ravi M. Shanker, Walter C. Babcock, Dwayne T. Friesen, James A. S. Nightingale, Douglas A. Lorenz
  • Publication number: 20130338158
    Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y, R4, n, o, A, A1, A2, X, Z, R1, R3, R2, p, q and r are as defined in the specification.
    Type: Application
    Filed: July 19, 2013
    Publication date: December 19, 2013
    Applicant: Allergan, Inc.
    Inventors: Richard L. Beard, John E. Donello, Tien T. Duong, Xiaoxia Liu, Haiging Yuan
  • Publication number: 20130338112
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
    Type: Application
    Filed: August 1, 2013
    Publication date: December 19, 2013
    Inventors: Zachary Demko, Christopher Borella, Shoujun Chen, Lijun Sun
  • Publication number: 20130338208
    Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are fulvene and/or fulvalene analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, as well as numerous inflammatory, degenerative and vascular diseases, including various ocular diseases. Representative fulvene and/or fulvalene analogs include fulvene and fulvalene analogues of various dyes, hormones, sugars, peptides, oligonucleotides, amino acids, nucleotides, nucleosides, and polyols. The compounds are believed to function, at least, by inhibiting Nox or ROS. In some embodiments, the Nox is one that is selectively expressed in cancer cells over normal cells, or one that is expressed in higher amounts in cancer cells over normal cells. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.
    Type: Application
    Filed: August 20, 2013
    Publication date: December 19, 2013
    Applicants: U.S. GOVERNMANET AS REPRESENTED BY UNITED STATES DEPARTMENT OF VETERANS AFFAIRS, EMORY UNIVERSITY
    Inventor: Jack L. Arbiser
  • Publication number: 20130336962
    Abstract: Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R, R1, R2, R3, R4, M1, M2, X, L1, L2, J1, J2, a1, a2, b1 and b2 are as defined herein, and wherein at least one of M2 or L2 is a moiety comprising an aziridine, acrylamide or sulfonate functional group, are provided. Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provided.
    Type: Application
    Filed: April 16, 2013
    Publication date: December 19, 2013
    Applicants: The University of Biritish Columbia, British Columbia Cancer Agency Branch
    Inventors: British Columbia Cancer Agency Branch, The University of British Columbia
  • Publication number: 20130338116
    Abstract: The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.
    Type: Application
    Filed: August 16, 2013
    Publication date: December 19, 2013
    Inventor: Irving Sucholeiki
  • Patent number: 8609712
    Abstract: Methods for purifying a compound of formula I are provided, wherein A, B, X, Q, and R1 are defined herein. The methods include mixing the compound of formula I and a solvent; adding a base to the solvent; and precipitating purified compound of formula I.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: December 17, 2013
    Assignee: Wyeth LLC
    Inventors: Bogdan Kazimierz Wilk, Arkadiy Zinoviy Rubezhov, Anthony Francis Hadfield, Jean Louise Helom
  • Publication number: 20130331413
    Abstract: Disclosed are compositions and methods for treating and/or preventing infections in mammals, by administering to a mammal a therapeutically effective amount of at least one defensin-like molecule, e.g., in a composition that includes such molecule. Also disclosed are kits that include such molecules, or compositions that include such molecules, as well as instructions for using such molecules to treat a mammal.
    Type: Application
    Filed: June 6, 2013
    Publication date: December 12, 2013
    Inventors: Erik DE LEEUW, Alexander D. MACKERELL, JR.
  • Publication number: 20130331425
    Abstract: The invention relates to (among other things) polymer-sunitinib conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over sunitinib in unconjugated form.
    Type: Application
    Filed: December 23, 2011
    Publication date: December 12, 2013
    Applicant: NEKTAR THERAPEUTICS
    Inventors: Sean M. Culbertson, Antoni Kozlowski, Tony Drew Vinson
  • Publication number: 20130331387
    Abstract: Disclosed is a compound of formula (I), wherein Z, m and R1-R6 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the ?7 subtype, in a subject in need thereof, as well as analogues, prodrugs, isotopically substituted analogs, metabolites, pharmaceutically acceptable salts, polymorphs, solvates, isomers, clathrates, and co-crystal thereof, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds and analogues. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.
    Type: Application
    Filed: February 22, 2012
    Publication date: December 12, 2013
    Applicant: Lupin Limited
    Inventors: Neelima Sinha, Gourhari Jana, Sachchidanand Sachchidanand, Sanjay Pralhad Kurhade, Navnath Popat Karche, Anil Kashiram Hajare, Ajay Ramchandra Tilekar, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 8603816
    Abstract: A SMAC mimetic and pharmaceutical compositions thereof and methods of use.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: December 10, 2013
    Assignee: TetraLogic Pharmaceuticals Corp.
    Inventors: Stephen M. Condon, Yijun Deng, Matthew G. LaPorte, Susan R. Rippin
  • Patent number: 8603531
    Abstract: The present invention describes nanoprodrugs of non-steroidal anti-inflammatory drug (NSAIDs) and nanoprodrugs of ?-lipoic acid-containing and NSAIDs. These nanoprodrugs have antioxidant properties and stimuli-responsiveness, which can be used to treat various disease conditions.
    Type: Grant
    Filed: April 8, 2009
    Date of Patent: December 10, 2013
    Assignee: Cedars-Sinai Medical Center
    Inventors: John S. Yu, Bong Seop Lee
  • Publication number: 20130324584
    Abstract: 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: Application
    Filed: February 9, 2012
    Publication date: December 5, 2013
    Inventors: Christopher E. Neipp, Michael R. Palovich
  • Publication number: 20130324583
    Abstract: Neurological disorders and diseases, such as Alzheimer's disease, Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis (ALS) and Down's syndrome, can be ameliorated or beneficially treated by administration of a formulation comprising an effective amount of a pyrone-indole derivative of formula (I) Ar—B—Ar???(I) wherein AR represents an indole nucleus ring system: Ar? represents an alpha-, beta- or gamma-pyrone nucleus ring system: and each of B, R1, R2, R3, R4, R1? and R2? are as defined herein.
    Type: Application
    Filed: August 12, 2013
    Publication date: December 5, 2013
    Applicant: Neurim Pharmaceuticals (1991) Ltd.
    Inventors: Moshe Laudon, Tal Peleg-Shulman
  • Publication number: 20130324548
    Abstract: The invention relates to chemoembolization composition for anti-angiogenic agent delivery. The invention further relates to a method of preparing chemoembolization composition and to the use of chemoembolization composition in the method for treating solid tumour cancers.
    Type: Application
    Filed: November 29, 2011
    Publication date: December 5, 2013
    Applicant: CENTRE HOSPITALIER UNIVERSITAIRE VAUDOIS
    Inventors: Alban Denys, Pierre Bize, Olivier Jordan, Eric Doelker, Nathalie Boulens
  • Patent number: 8598181
    Abstract: 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: Grant
    Filed: July 2, 2010
    Date of Patent: December 3, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: 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
  • Publication number: 20130317065
    Abstract: The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism: wherein A represents a benzene ring, a pyridine ring, or the like; Y1 represents a C1-6 alkylene group or the like; Y2 represents a single bond or the like; Z represents —C(?O)—NHSO2R6, an acidic 5-membered hetero ring group, or the like; R1 represents a hydrogen atom or the like; R2 represents a phenyl group, a 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], or a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.
    Type: Application
    Filed: January 24, 2012
    Publication date: November 28, 2013
    Inventors: Kazuya Tatani, Atsushi Kondo, Tatsuhiro Kondo, Naohiro Kawamura, Shigeki Seto, Yasushi Kohno
  • Publication number: 20130317077
    Abstract: 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: Application
    Filed: December 27, 2011
    Publication date: November 28, 2013
    Inventors: Tae Sun Park, Gyoon Hee Han
  • Publication number: 20130317024
    Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
    Type: Application
    Filed: May 22, 2013
    Publication date: November 28, 2013
    Applicant: NOVARTIS AG
    Inventors: Simona Cotesta, Pascal Furet, Vito Guagnano, Philipp Holzer, Joerg Kallen, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
  • Publication number: 20130317043
    Abstract: The invention relates to a compound of Formula I:
    Type: Application
    Filed: May 6, 2013
    Publication date: November 28, 2013
    Applicants: President and Fellows of Harvard College, The Broad Institute, Inc.
    Inventors: The Broad Institute, Inc., President and Fellows of Harvard College
  • Patent number: 8586621
    Abstract: The present invention includes methods and compositions for the treatment and prevention of protozoal parasitic infections utilizing Diindolylmethane-related indoles. Additive and synergistic interaction of Diindolylmethane-related indoles with other known anti-parasitic and pro-apoptotic agents is believed to permit more effective therapy and prevention of protozoal parasitic infections. The methods and compositions described provide new treatment of protozoal parasitic diseases of mammals and birds including malaria, leishmaniasis, trypanosomiasis, trichomoniasis, neosporosis and coccidiosis.
    Type: Grant
    Filed: October 26, 2007
    Date of Patent: November 19, 2013
    Inventor: Michael A. Zeligs
  • Patent number: 8586620
    Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.
    Type: Grant
    Filed: May 6, 2011
    Date of Patent: November 19, 2013
    Assignee: NeurAxon, Inc.
    Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
  • Publication number: 20130303518
    Abstract: The invention provides a method of inhibiting the catalytic activity of a protein kinase comprising contacting said protein kinase with a compound of formula (I), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing the same, and also provides a method of treating a protein kinase related disorder comprising a step of administering to a patient in need thereof a therapeutically effective amount of the compound of formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing the same, wherein each substituent in formula (I) is same as defined in the description.
    Type: Application
    Filed: September 27, 2012
    Publication date: November 14, 2013
    Applicants: Shanghai Hengrui Pharmaceutical Co., Ltd., Jiangsu Hansoh Pharmaceutical Co., Ltd.
    Inventors: Peng Cho Tang, Yidong Su, Yali Li, Lei Zhang, Fuqiang Zhao, Jialiang Yang, Ying Zhou, Pingyan Bie, Guangtao Qian, Minggang Ju
  • Publication number: 20130303525
    Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts. (I) Wherein A, m, R1s, R2, R3, R4 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: Application
    Filed: July 19, 2011
    Publication date: November 14, 2013
    Applicants: DR. REDDY'S LABORATORIES, INC., DR. REDDY;S LABORATORIES LTD.
    Inventors: Pradip Kumar Sasmal, Vamsee Krishna Chintakunta, Vijay Potluri, Ish Kumar Khanna, Ashok Tehim, Mahaboobi Jaleel, Thomas Hogberg, Oystein Rist, Lisbeth Elster, Thomas Michael Frimurer, Lars-Ole Gerlach
  • Publication number: 20130303461
    Abstract: The technology described herein is directed to methods of determining oligonucleotide sequences, e.g. by enriching target sequences prior to sequencing the sequences.
    Type: Application
    Filed: March 11, 2013
    Publication date: November 14, 2013
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventors: Anthony John Iafrate, Long Phi Le, Zongli Zheng
  • Publication number: 20130303582
    Abstract: The present invention, in one or more embodiments, comprises water-soluble derivatives of 3-n-pentadecylcatechol (poison ivy urushiol saturated congener) and/or 3-n-heptadecylcatechol (poison oak urushiol saturated congener) as compositions for the prevention and/or prophylactic treatment of contact dermatitis caused by poison ivy and poison oak. The present invention is also directed towards processes for making such compounds. Disclosed are compounds which are effective for tolerizing and desensitizing a subject against allergens contained in plants of the Anacardiaceae and Ginkgoaceae families comprising water soluble urushiol esters of general formula (I) Tolerizing and desensitizing mammals, including humans, to allergens contained in plants of the Anacardiaceae and Ginkgoaceae families is attained by administering a composition containing at least one water soluble urushiol ester compound.
    Type: Application
    Filed: April 11, 2013
    Publication date: November 14, 2013
    Inventors: Mahmoud A. Elsohly, Waseem Gul, Mohammad Khalid Ashfaq, Susan P. Manly