Additional Hetero Ring Which Is Not Part Of The Bicyclo Ring System Patents (Class 514/414)
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Patent number: 8895602Abstract: The present invention relates to a 6-pyrazolylamido-3-substituted azabicyclo[3.1.0]hexane derivatives useful as calcium channel blockers, pharmaceutically acceptable salts thereof and medical use of the calcium channel inhibiting effect of the compounds for treatment of diseases.Type: GrantFiled: August 29, 2013Date of Patent: November 25, 2014Assignee: Korea Institute of Science and TechnologyInventors: Ghil Soo Nam, Kyung Il Choi, Ae Nim Pae, Seon Hee Seo, Hyun Ah Choo, Gyo Chang Keum, Jung Hyun Kim
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Publication number: 20140343065Abstract: 3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4.Type: ApplicationFiled: May 12, 2014Publication date: November 20, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Riccardo GIOVANNINI, Yunhai CUI, Henri DOODS, Marco FERRARA, Stefan JUST, Raimund KUELZER, Iain LINGARD, Rocco MAZZAFERRO, Klaus RUDOLF
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Publication number: 20140343037Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.Type: ApplicationFiled: August 4, 2014Publication date: November 20, 2014Inventors: Kenneth He Huang, Jeron Eaves, Gunnar Hanson, James Veal, Thomas Barta, Lifeng Geng, Lindsay Hinkley
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Publication number: 20140336234Abstract: Degranulation suppressors are provided that are effective against allergic disease and osteoarthritis. The degranulation suppressors contain chlorophyll c.Type: ApplicationFiled: December 28, 2012Publication date: November 13, 2014Inventors: Hisashi Yoshioka, Akira Kamata, Tatsuya Konishi, Hiroshi Oda, Tadakazu Tamai
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Patent number: 8883824Abstract: Disclosed is a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is 1: a C3-8 cycloalkyl C1-4 alkyl group, 2: a C7-14 aralkyl group, in which the aryl moiety thereof is optionally substituted with the same or different 1 to 3 groups selected from the group consisting of: (a) halogen, (b) C1-4 alkyl, which is optionally substituted with 1 to 3 fluorine atoms, (c) C1-4 alkoxy, which is optionally substituted with 1 to 3 fluorine atoms, and (d) C1-4 alkylcarbonyl, which is optionally substituted with C1-4 alkoxy, 3: a five-to ten-membered heteroaryl-C1-4 alkyl group, in which the heteroaryl moiety thereof is optionally substituted with the same or different 1 to 3 groups selected from the group consisting of: (a) halogen, and (b) C1-4 alkyl, or 4: a C6-10 aryl C2-6 alkenyl group; and R2 is a cyano group or a nitro group.Type: GrantFiled: May 12, 2010Date of Patent: November 11, 2014Assignee: Sumitomo Dainippon Pharma Co., Ltd.Inventors: Akihito Fujii, Kazumi Niidome, Chiaki Migihashi, Toshiyuki Kamei, Takafumi Matsumoto, Tomoyuki Hirata
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Publication number: 20140329836Abstract: This invention provides compounds of formula (I): wherein R1, R2, G, n, p and q have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: December 5, 2013Publication date: November 6, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
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Publication number: 20140329823Abstract: Molecular mimics of Smac are capable of modulating apoptosis through their interaction with cellular IAPs (inhibitor of apoptosis proteins). The mimetics are based on a monomer or dimer of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac/DIABLO, Hid, Grim and Reaper, which interact with a specific surface groove of IAP. Also disclosed are methods of using these peptidomimetics for therapeutic purposes.Type: ApplicationFiled: July 21, 2014Publication date: November 6, 2014Applicant: TETRALOGIC PHARMACEUTICALS CORPORATIONInventors: Stephen M. Condon, Matthew G. Laporte, Yijun DENG, Susan R. Rippin
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Publication number: 20140323475Abstract: The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.Type: ApplicationFiled: September 14, 2012Publication date: October 30, 2014Inventors: Antoni Torrens Jover, Ramon Mercé Vidal, Francesc Xavier Caldentey Frontera, Antonio David Rodríguez Garrido, Elena Carceller González, Jordi Salas Solana
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Publication number: 20140323465Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: July 14, 2014Publication date: October 30, 2014Inventors: Deqiang Niu, Russell C. Petter, Juswinder Singh, Arthur F. Kluge, Lixin Qiao
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Publication number: 20140322136Abstract: The present invention provides methods to reduce or inhibit weight gain by administering inhibitors of the SirT1 protein to a subject. Methods to identify such inhibitors are also disclosed.Type: ApplicationFiled: May 6, 2014Publication date: October 30, 2014Inventors: Yansong GU, Hongzhe LI
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Patent number: 8865682Abstract: 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: GrantFiled: November 15, 2012Date of Patent: October 21, 2014Assignee: Allergan, Inc.Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone, Julie Wurster
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Publication number: 20140309213Abstract: This invention relates to compounds of Formula I-VI having the following general structure: Z1—Y1—(CH2)n1—R—(CH2)n2—Y2—Z2 wherein R is a 6-8 membered saturated heterocyclic ring having 2 Nitrogen atoms connected with —(CH2)n1— and —(CH2)n2—, respectively, and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: October 25, 2012Publication date: October 16, 2014Inventors: Shawn P. Walsh, Alexander Pasternak, Reynalda K. DeJesus, Haifeng Tang, Barbara Pio, Aurash Shahripour, Kevin M. Belyk, Harry R. Chobanian, Yan Guo, Jessica L. Frie, Zhi-Cai Shi, Helen Chen, Timothy A. Blizzard, Brian Cato
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Publication number: 20140309272Abstract: Novel bis-indolic derivatives, processes for their preparation, and their potential use as new antibacterial drugs.Type: ApplicationFiled: July 20, 2012Publication date: October 16, 2014Applicant: UNIVERSITE JOSEPH FOURIERInventors: Jean-Noël Denis, Marcelle Claude Jolivalt, Max Maruin Louis Mauring, Matthieu Jeanty
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Publication number: 20140309263Abstract: The present invention relates to methods of diagnosing a kidney disorder in a patient, as well as methods of monitoring the progression of a kidney disorder and/or methods of monitoring a treatment protocol of a therapeutic agent or a therapeutic regimen. The invention also relates to assay methods used in connection with the diagnostic methods described herein.Type: ApplicationFiled: January 31, 2014Publication date: October 16, 2014Applicant: MESO SCALE TECHNOLOGIES, LLCInventors: Simone Barbero, Eli N. Glezer, Anu Mathew, Mingyue Wang
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Publication number: 20140309208Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are disclosed that are represented by general formula (I). Also disclosed, are pharmaceutical compositions including these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated pathologies.Type: ApplicationFiled: October 26, 2012Publication date: October 16, 2014Inventors: Branislav Musicki, Jerôme Aubert, Jean-Guy Boiteaux, Laurence Clary, Patricia Rossio, Marlène Schuppli-Nollet
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Patent number: 8859609Abstract: 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: January 3, 2012Date of Patent: October 14, 2014Assignee: Targacept, Inc.Inventors: Anatoly Mazurov, Lan Miao, Yunde Xiao
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Publication number: 20140303207Abstract: The invention provides novel 1-heteroaryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including but not limited to depression and anxiety.Type: ApplicationFiled: April 3, 2013Publication date: October 9, 2014Applicant: NEUROVANCE, Inc.Inventors: Phil SKOLNICK, Zhengming Chen
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Publication number: 20140303225Abstract: Block copolymer pharmaceutical compositions containing 3,3?-diindolylmethane (DIM). The pharmaceutical composition for peroral administration comprises 3,3?-diindolylmethane as an active component and a target additive, the target additive being a block copolymer of oxyethylene and oxypropylene, in which the content of the hydrophobic oxypropylene block is less than 50 mass % and the molecular mass of the hydrophilic oxyethylene block is equal to 2,250 Da or more, at a ratio of the active component to the selected block copolymer varying between 1:2 and 1:10. The composition improves absorption of the active compound by the bloodstream upon peroral delivery.Type: ApplicationFiled: June 20, 2014Publication date: October 9, 2014Inventors: Vsevolod Ivanovich KISELEV, Irina Gennadievna VASSILIEVA
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Patent number: 8853212Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: February 17, 2011Date of Patent: October 7, 2014Assignee: Merck Sharp & Dohme CorpInventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
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Publication number: 20140294767Abstract: A method of treating an Hepatitis C Virus infection in a patient, comprising providing a therapeutically effective amount, to a patient in need thereof, of a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein: G1 is a group of the formula or where n is 0, 1, 2, 3, or 4 and Het is a 5- or 6-membered heteroaryl group containing 1 to 4 heteroatoms independently chosen from N, O, and S, which Het is optionally substituted.Type: ApplicationFiled: October 26, 2012Publication date: October 2, 2014Inventors: David Waugh, Christopher Self, Guangtao Zhang, Yves Pommier, Robert H. Shoemaker, Michael Currens, John Cardellina, Andrew Jobson, George Lountos, Dominic Scudiero
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Publication number: 20140296292Abstract: Some embodiments include compositions and methods of using or identifying compounds that modulate the activity of the granulocyte colony-stimulating factor receptor (GCFR). Some embodiments include use of compounds to treat certain disorders, such as hematopoietic or neurological disorders.Type: ApplicationFiled: November 12, 2012Publication date: October 2, 2014Inventors: Lin Zhi, Keith Marschke, Virginia H. Grant, Steven L. Roach, Yixing Shen, Jason C. Pickens, Bijan Pedram, C. Arjan van Oeveren, Lino J. Valdez, Andrew R. Hudson
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Patent number: 8846674Abstract: The invention provides methods for treating ophthalmic disorders comprising at least one nitric oxide enhancing prostaglandin compound or a pharmaceutically acceptable salt thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The nitric oxide enhancing prostaglandin compounds comprise at least one heterocyclic nitric oxide donor group and/or at least one nitroxide group.Type: GrantFiled: October 18, 2011Date of Patent: September 30, 2014Assignee: Nicox, S.A.Inventor: David S. Garvey
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Publication number: 20140288127Abstract: The present invention provides compounds of formula (I), as well as pharmaceutically acceptable salt thereof, wherein R1 to R7 have the significance given herein. The compounds are useful in the treatment of prophylaxis of diseases that are related to AMPK regulation.Type: ApplicationFiled: June 3, 2014Publication date: September 25, 2014Inventors: Li Chen, Lichun Feng, Mengwei Huang, Jia Li, Fajun Nan, Tao Pang, Lifang Yu, Mei Zhang
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Publication number: 20140288042Abstract: This invention relates to compounds of Formula I having the following general structure: Z1—Y1—(CH2)n1—R—(CH2)n2—Y2—Z2 wherein R represents a fused bicyclic or spirocyclic aliphatic diamine and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: October 25, 2012Publication date: September 25, 2014Inventors: Shawn P. Walsh, Alexander Pasternak, Zhi-Cai Shi, Brian Cato, Esther Y. Kim
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Publication number: 20140288065Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.Type: ApplicationFiled: June 10, 2014Publication date: September 25, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Muneaki KURIMURA, Shinichi TAIRA, Takahiro TOMOYASU, Nobuaki ITO, Kuninori TAI, Noriaki TAKEMURA, Takayuki MATSUZAKI, Yasuhiro MENJO, Shin MIYAMURA, Yohji SAKURAI, Akihito WATANABE, Yasuyo SAKATA, Takumi MASUMOTO, Kohei AKAZAWA, Haruhiko SUGINO, Naoki AMADA, Satoshi OHASHI, Tomoichi SHINOHARA, Hirofumi SASAKI, Chisako MORITA, Junko YAMASHITA, Satoko NAKAJIMA
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Publication number: 20140288143Abstract: Therapeutic compositions comprising an indoloquinone compound and various bladder cancer treatments and methods are disclosed. More specifically, bladder cancer treatments include the intravesical administration of apaziquone immediately following transurethral resection. Also disclosed are therapeutic compositions comprising an indoloquinone compound and a formulation vehicle. The formulation vehicle improves the solubility and stability of the indoloquinone compound. Additionally, the coating compositions can include coating agents that provide better adhesion of the coating composition to the bladder wall during intravesical delivery of the coating composition.Type: ApplicationFiled: February 5, 2014Publication date: September 25, 2014Applicant: Spectrum Pharmaceuticals, Inc.Inventors: Bastiaan Nuijen, Ernie Pfadenhauer, Jos H. Beijnen, Luigi Lenaz, Shanta Chawla, Mario Beer
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Patent number: 8841324Abstract: Compounds of the formula (I), in which Het, R, X, Y, R1 and p have the meanings indicated in claim 1, are autotaxin inhibitors and can be employed for the treatment of tumors.Type: GrantFiled: March 3, 2010Date of Patent: September 23, 2014Assignee: Merck Patent GmbHInventors: Wolfgang Staehle, Kai Schiemann, Melanie Schultz
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Patent number: 8841319Abstract: The present invention relates to the use of a compound of formula (I) wherein R1 is H, C1-C6-alkyl, phenyl-C1-C4-alkyl or phenyl, R2 is a phenyl group which is substituted with 2 or 3 C1-C6-alkoxy groups and R3 is indolyl or azaindolyl which may carry one or two substituents independently selected from C1-C6-alkyl, C1-C6-alkoxy, phenyl, OH, halogen, NH2, C1-C6-alkylamino, di-C1-C6-alkylamino, heteroaryl with 5 or 6 ring atoms containing 1 or 2 heteroatoms which are independently selected from O, N, and S, or heterocyclyl with 5 or 6 ring atoms containing 1 or 2 heteroatoms which are independently selected from O, N, and S, a physiologically acceptable salt thereof, or a solvate of the compound of formula (I) or of the salt thereof, for the prevention or treatment of leukemia.Type: GrantFiled: December 4, 2008Date of Patent: September 23, 2014Assignee: Johannes Gutenberg-Universitat MainzInventors: Gerd Dannhardt, Thomas Fischer, Florian Heidel
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Patent number: 8841463Abstract: 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: GrantFiled: February 9, 2012Date of Patent: September 23, 2014Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Christopher E Neipp, Michael R. Palovich
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Publication number: 20140275114Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (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: March 12, 2014Publication date: September 18, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ralf ANDERSKEWITZ, Marc GRUNDL, Gerd MORSCHHAEUSER, Thorsten OOST, Alexander PAUTSCH
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Publication number: 20140275025Abstract: 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: March 12, 2014Publication date: September 18, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: 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: 20140275201Abstract: The present invention provides biomarkers of cancer stem cells, as well as cells that have undergone EMT. In addition, the present invention provides methods of treating patients determined to comprise cancer stem cells with PDGFR-? inhibitors to eliminate the cancer stem cells. Methods of predicting sensitivity to PDGFR-? inhibitors, monitoring efficacy of treatment, and determining a prognosis are also provided.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEMInventors: Sendurai A. MANI, Brett G. HOLLIER, Kurt W. EVANS, Steven J. WERDEN, Tapasree Roy SARKAR, Agata TINNIRELLO
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Publication number: 20140275010Abstract: The present invention provides quaternary salts, such as those of Formula I: as well as the use thereof in methods of treatment for cancer.Type: ApplicationFiled: March 11, 2014Publication date: September 18, 2014Inventors: Guo Zhu Zheng, Yuan Wang, Gregg F. Keany, Kenzo Arai, Kazunobu Kira, Xiang Liu, Nick Gearhart, Baudouin Gerard
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Publication number: 20140275033Abstract: The invention provides novel inhibitors of cancer stem cells as well as cancer stem cell pathway kinase and other related kinases, pharmaceutical compositions and uses thereof in the treatment of cancer or a related disorder in a mammal, and methods of making such compounds and compositions.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventors: Chiang Jia Li, Ji-Feng Liu, Wei Li, Amanda Gibeau, Harry Rogoff
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Publication number: 20140275076Abstract: Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, R1 is optionally substituted heteroaryl etc.; R2 is hydrogen etc.; R3 and R4 are each independently hydrogen etc., R5 is the following group: (wherein Y is optionally substituted five membered heteroaryl etc., R9a is optionally substituted aryl etc., R9b and R9c are each dependently hydrogen etc., and m is the integral 0 etc.) etc.; R6 is hydrogen etc.; and R7 is hydrogen etc.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventors: Katsunori Tsuboi, Yosuke Takanashi, Shingo Tojo, Tomohiro Kodama, Katsumi Kubota, Toshio Kanai
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Publication number: 20140275075Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.Type: ApplicationFiled: March 13, 2013Publication date: September 18, 2014Applicant: MUSC FOUNDATION FOR RESEARCH DEVELOPMENTInventors: Craig C. BEESON, Christopher C. LINDSEY, Yuri K. PETERSON, Baerbel ROHRER
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Publication number: 20140271480Abstract: The present invention provides a method of using indole-ketone or indolidone to treat or prevent a neurodegenerative disease or disorder. In one embodiment, the neurodegenerative disease is Parkinson's disease. In another embodiment, the neurodegenerative disease or disorder is associated with excessive neuronal Nitric Oxide Synthase (nNOS) activity. Examples of indole-ketone include, but are not limited to, SU4312, SU5416, SU11248 (Sunitinib), and indirubin-3-oxime.Type: ApplicationFiled: October 25, 2012Publication date: September 18, 2014Inventors: Ming Yuen Lee, Yifan Han, Chung Lit Choi, Zaijun Zhang, Wei Cui
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Publication number: 20140275168Abstract: Indirubin is the major active anti-tumor component of a traditional Chinese herbal medicine used for treatment of chronic myelogenous leukemia (CML). Indirubin derivatives (IRDs) potently reduce the viabilities of various cancer cells and affect kinase activities. IRDs disclosed herein provide new therapeutics for cancer and conditions regulated by the kinase activities.Type: ApplicationFiled: March 14, 2013Publication date: September 18, 2014Inventors: Sangkil NAM, Richard JOVE, Leandros SKALTSOUNIS
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Publication number: 20140275155Abstract: This invention relates to bicyclic 1-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: March 12, 2014Publication date: September 18, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias GRAUERT, Ralf ANDERSKEWITZ, Marc GRUNDL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS
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Publication number: 20140256768Abstract: The present document describes novel compounds which may inhibit the activity of anti-apoptotic proteins such as Bcl-2 family protein members, compositions containing the compounds and methods of treating diseases involving a defect in apoptosis, such as, for example, in the treatment of cancer.Type: ApplicationFiled: October 11, 2012Publication date: September 11, 2014Inventor: Zhaoyin Wang
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Publication number: 20140256725Abstract: The invention relates to FSH receptor antagonist according to general formula I or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders.Type: ApplicationFiled: September 14, 2012Publication date: September 11, 2014Inventors: Wesley Peter Blackaby, Martin De Kort, Mark Enthoven, Paul Stuart Hinchliffe, Christian Matthijs Poulie, Cornelis Marius Timmers, Saskia Vertaik
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Patent number: 8829039Abstract: Disclosed are dihydroindolone compounds which can modulate the activity of protein tyrosine kinases, a method for preparing the same, and pharmaceutical compositions comprising the same. Also disclosed are use of such compounds and pharmaceutical compositions thereof in the treatment and/or prophylaxis of protein tyrosine kinase associated diseases in an organism, particularly in the treatment and/or prophylaxis of tumors and fibroblast proliferation associated diseases.Type: GrantFiled: May 25, 2009Date of Patent: September 9, 2014Assignees: Shanghai Institute of Pharmaceutical Industry, Jiangsu Chiatai Tianqing Pharmaceutical Co., Ltd.Inventors: Zhedong Yuan, Xiaomin Zhang, Hubo Wang, Xueyan Zhu, Hongjiang Xu, Hui Fu, Wei Song
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Publication number: 20140249158Abstract: The present disclosure generally relates to nanoparticles comprising a substantially hydrophobic acid, a basic therapeutic agent having a protonatable nitrogen, and a polymer. Other aspects include methods of making and using such nanoparticles.Type: ApplicationFiled: May 13, 2014Publication date: September 4, 2014Applicant: BIND Therapeutics, Inc.Inventors: Maria Figueiredo, Erick Peeke, David Dewitt, Christina Van Geen Hoven, Greg Troiano, James Wright, Young-Ho Song, Hong Wang
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Publication number: 20140249197Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: ApplicationFiled: May 14, 2014Publication date: September 4, 2014Applicant: Janssen Pharmaceutica, NVInventors: James C. Lanter, Zhihua Sui, James J. Fiordeliso, Weiqin Jiang, Xuqing Zhang
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Publication number: 20140248358Abstract: The present disclosure generally relates to nanoparticles comprising a substantially hydrophobic acid, a basic therapeutic agent having a protonatable nitrogen, and a polymer. Other aspects include methods of making and using such nanoparticles.Type: ApplicationFiled: May 13, 2014Publication date: September 4, 2014Applicant: BIND Therapeutics, Inc.Inventors: Maria Figueiredo, Erick Peeke, David Dewitt, Christina Van Geen Hoven, Greg Troiano, James Wright, Young-Ho Song, Hong Wang
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Publication number: 20140243390Abstract: Novel RET fusion molecules and uses are disclosed.Type: ApplicationFiled: February 23, 2014Publication date: August 28, 2014Applicant: FOUNDATION MEDICINE, INC.Inventors: Sean R. Downing, Matthew J. Hawryluk, Doron Lipson, Alexander N. Parker, Philip James Stephens
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Publication number: 20140243324Abstract: The present invention relates to uses of small molecule mimetics of hematopoietic growth factors. In particular the present invention relates to uses of small molecule mimetics of erythropoietin.Type: ApplicationFiled: November 17, 2011Publication date: August 28, 2014Applicant: LIGAND PHARMACEUTICALS INCORPORATEDInventors: Reid P. Bissonnette, Andrew R. Hudson, Keith B. Marschke, Deepa Rungta, Lin Zhi
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Patent number: 8815903Abstract: 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: GrantFiled: January 24, 2012Date of Patent: August 26, 2014Assignees: Kissei Pharmaceutical Co., Ltd., Kyorin Pharmaceutical Co., Ltd.Inventors: Kazuya Tatani, Atsushi Kondo, Tatsuhiro Kondo, Naohiro Kawamura, Shigeki Seto, Yasushi Kohno
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Publication number: 20140235654Abstract: The present invention relates to the use of derivatives of indoles having a general formula (I) as follow: for the manufacture of a pharmaceutical composition intended for the treatment of cancer.Type: ApplicationFiled: February 12, 2014Publication date: August 21, 2014Applicants: COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Catherine GUILLOU, Frank KOZIELSKI, Christophe LABRIERE, Francoise GUERITTE, Sergey TCHERNIUK, Dimitrios SKOUFIAS, Claude THAL, Henri-Philippe HUSSON
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Publication number: 20140235533Abstract: The present invention provides compounds of formula I wherein Q is Q1 or Q2; A1, A2, A3 and A4 are independently of each other C—H, C—R7, or nitrogen; R1 is C1-C8haloalkyl; R2 is aryl or aryl substituted by one to five R11, or heteroaryl or heteroaryl substituted by one to five R11; and R3, R4, R5, R6 and R7 are as defined in the claims. The invention also provides methods of controlling insects, acarines, nematodes or molluscs which methods comprise applying to a pest, to a locus of a pest, or to a plant susceptible to attack by a pest an insecticidally, acaricidally, nematicidally or molluscicidally effective amount of a compound of formula (I).Type: ApplicationFiled: August 10, 2012Publication date: August 21, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Tomas Smejkai, Sebastian Volker Wendeborn, Jerome Yves Cassayre, Myriem El Qacemi, Bernhard Breit, Lisa Diab, Regis Jean Georges Mondiere