Tricyclo Ring System Having 1,3-diazine As One Of The Cyclos Patents (Class 514/267)
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Patent number: 8858911Abstract: Tracers targeting phosphodiesterase 1 for use in gamma radiation detection-based diagnostic techniques, particularly gamma-emitter labeled tracers for SPECT and positron emitter-labeled compositions for PET are disclosed. Radio-labeled multiple novel scaffolds as PDE1 inhibitors such as substituted pyrazolo-pyrimidin-4-one derivatives, biomarkers for phosphodiesterase 1 [PDE1) in vivo, methods for developing novel therapies for PDE1-implicated conditions such as pulmonary arterial hypertension (PAH), Central Nervous System (CNS) and Cardiovascular (CV) disorders, and methods of detection and treatment are also disclosed.Type: GrantFiled: October 7, 2010Date of Patent: October 14, 2014Assignee: Intra-Cellular Therapies, Inc.Inventors: Peng Li, Lawrence P. Wennogle, Jun Zhao, Hailin Zheng
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Patent number: 8853226Abstract: The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-? or by PDE4, including but not limited to rheumatoid arthritis.Type: GrantFiled: March 4, 2011Date of Patent: October 7, 2014Assignee: High Point Pharmaceuticals, LLCInventors: Adnan M. M. Mjalli, Bapu Gaddam, Dharma Rao Polisetti, Matthew J. Kostura, Mustafa Guzel
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Patent number: 8853227Abstract: Methods are provided for using methotrexate (MTX) active agents in which reduced host toxicity is observed. Aspects of the methods include administering to a subject an effective amount of an MTX active agent in conjunction with a MTX toxicity-reducing adjuvant, such as a 2,2?-anhydropyrimidine, a derivative thereof or a uridine phosphorylase inhibitor. Also provided are compositions and kits that find use in practicing embodiments of the invention. The methods and compositions find use in a variety of applications, including the treatment of a variety of different disease conditions.Type: GrantFiled: June 20, 2011Date of Patent: October 7, 2014Assignee: Tosk, IncorporatedInventors: William A. Garland, Brian D. Frenzel, Travis Karg
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Patent number: 8853220Abstract: The present invention relates to methods for synthesizing energetic compounds and intermediates thereof. Specifically, the present invention relates to methods for synthesizing adamantanes and intermediates that are useful in such synthesis. Synthesized intermediates are useful in the synthesis of bicyclic and tricyclic substituted adamantanes. Examples of various intermediates are: acyclic 2-nitromalonaldehyde intermediates, 2,6,9-tri-substituted-4,8-dinitro-2,6,9-triazabicyclo[3.3.1]nona-3,7-dienes and 2,6-dinitro-4,8,9,10-tetra-aza-4,8,9,10-tetra-substituted adamantanes. Intermediates synthesized according to the methods of the present invention are useful toward the synthesis of tetraaza-adamantanes, which can serve as precursors to potentially superior new high-energy-density compounds (HEDCs). The tricyclic intermediate compound has a structure of Formula III: where R is one of a benzyl, 4-methoxybenzyl, acetyl, nitro, formyl, allyl, and a carboethoxyl group.Type: GrantFiled: February 25, 2011Date of Patent: October 7, 2014Assignee: The United States of America as Represented by the Secretary of the NavyInventors: Alfred G. Stern, Craig J. Diamond
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Patent number: 8846701Abstract: The present invention relates to pyrazolo-quinazolines, characterized by an ortho-substituted-arylamino, heterocyclylamino- or C3-C7 cycloalkylamino residue at 8 position and an aryl, heterocyclyl or C3-C7 cycloalkyl as substituent of a carboxamide at 3 position of the molecule framework. The compounds of this invention modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular MPS1/TTK. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.Type: GrantFiled: June 17, 2009Date of Patent: September 30, 2014Assignee: Nerviano Medical Sciences S.R.L.Inventors: Marina Caldarelli, Mauro Angiolini, Riccardo Colombo, Teresa Disingrini, Stefano Nuvoloni, Helena Posteri, Matteo Salsa, Marco Silvagni
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Patent number: 8846702Abstract: The present invention is directed to pyranyl aryl methyl benzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: August 26, 2010Date of Patent: September 30, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Ronald K. Chang, Thomas J. Greshock
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Patent number: 8846703Abstract: To provide a crystal of a tricyclic pyrazolopyrimidine compound inhibiting the effect of HSP90. The present invention provides a crystal of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2,7-dihydro-6-thia-1,2,3,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide which inhibits the ATPase activity of HSP90 and which has antitumor activity, a medicament comprising the same, an anticancer agent comprising the same, and the like.Type: GrantFiled: February 21, 2013Date of Patent: September 30, 2014Assignee: Daiichi Sankyo Company, LimitedInventors: Yasusi Ueda, Nobuyuki Suzuki, Hitoshi Ohki
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Publication number: 20140288103Abstract: Since each of the site I sodium channel blockers have a unique activity and cannot be used to extrapolate the same effective dosage for another site I sodium channel blocker, studies were conducted to identify dosages of neosaxitoxin (“NeoSTX”) and bupivacaine, alone or in combination with epinephrine, to provide two to three days of pain relief in humans. Bupivacaine-NeoSTX combinations produce more reliable blockade and longer duration blockade compared to NeoSTX alone. The three-way combination of NeoSTX-bupivacaine-epinephrine produces more prolonged local anesthesia than the two-way combination of NeoSTX-bupivacaine. Addition of epinephrine to this NeoSTX-bupivacaine combination dramatically prolongs the duration of complete blockade to a mechanical stimulus. These results led to development of specific combination dosage formulations.Type: ApplicationFiled: March 17, 2014Publication date: September 25, 2014Applicant: The Children's Medical Center CorporationInventors: Charles Berde, Daniel S. Kohane
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Patent number: 8841312Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.Type: GrantFiled: December 18, 2008Date of Patent: September 23, 2014Assignee: Amgen Inc.Inventors: Richard V. Connors, Dai Kang, John Eksterowicz, Pingchen Fan, Benjamin Fisher, Jiasheng Fu, Kexue Li, Zhihong Li, Lawrence R. McGee, Rajiv Sharma, Xiaodong Wang, Dustin L. McMinn, Jeffrey T. Mihalic, Jeffrey Deignan
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Publication number: 20140275130Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have the formula I: Additionally, the compounds of this invention have the formula I-A: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.Type: ApplicationFiled: December 6, 2013Publication date: September 18, 2014Inventors: Jean-Damien Charrier, Chris Davis, Steven Durrant, Gorka Etxebarria I Jardi, Damien Fraysse, David Kay, Ronald Knegtel, Francoise Pierard, Joanne Pinder, Pierre-Henri Storck
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Publication number: 20140271540Abstract: This disclosure relates, at least in part, to a method of treatment. In one embodiment, the method of treatment comprises administering to a subject in need of such treatment a first therapeutic agent including compound (1): or a pharmaceutically acceptable salt thereof in combination with a second therapeutic agent, wherein the first therapeutic agent and the second therapeutic agent are administered either simultaneously or sequentially.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: ONCOCEUTICS, INC.Inventors: Martin STOGNIEW, Joshua E. ALLEN
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Publication number: 20140275131Abstract: Provided are PDE1 inhibitors of Formula I, processes for their production, their use as pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventors: Peng LI, Hailin ZHENG, Jun ZHAO, Lawrence P. WENNOGLE
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Publication number: 20140275064Abstract: The present invention relates to novel thiazolo[5,4-f]quinazoline compounds and methods that are useful in the amelioration, treatment or control of Down's syndrome or early Alzheimer's disease or in the amelioration, treatment or control of cancers, especially solid tumors. More specifically, the invention relates to DYRK1A and/or DYRK1B inhibitors and to methods for preparing such compounds.Type: ApplicationFiled: August 17, 2012Publication date: September 18, 2014Applicant: DIAXONHITInventors: Bertrand Leblond, Anne-Sophie Casagrande, Laurent Desire, Alicia Foucourt, Thierry Besson
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Publication number: 20140275023Abstract: The present invention relates to substituted tricyclic pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tricyclic pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: March 11, 2014Publication date: September 18, 2014Inventors: Nivedita Namdev, Jianqiang Wang
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Publication number: 20140275092Abstract: The present invention relates to compounds useful as inhibitors of one or more histone demethylses. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: Constellation Pharmaceuticals, Inc.Inventors: Brian K. Albrecht, Steven F. Bellon, Victor S. Gehling, Jean-Christophe Harmange
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Publication number: 20140256706Abstract: Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed.Type: ApplicationFiled: March 11, 2014Publication date: September 11, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Xu Ran, Yujun Zhao, Chao-Yie Yang, Liu Liu, Longchuan Bai, Donna McEachern, Jeanne Stuckey, Jennifer Lynn Meagher, Duxin Sun, Xiaoqin Li, Bing Zhou, Hacer Karatas, Ruijuan Luo, Arul Chinnaiyan, Irfan A. Asangani
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Publication number: 20140249143Abstract: Provided are certain compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections.Type: ApplicationFiled: October 19, 2012Publication date: September 4, 2014Applicant: GlaxoSmithKline LLCInventors: Anna Lindsey Banka, Janos Botyanszki, Eric Gregory Burroughs, John George Catalano, Wendy Huang Chern, Hamilton D. Dickson, Margaret J. Gartland, Robert Hamatake, Hans Hofland, Jesse Daniel Keicher, Christopher Brooks Moore, John Bradford Shotwell, Matthew David Tallant, Jean-Philippe Therrien, Shihyun You
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Publication number: 20140249137Abstract: The present invention relates to compounds useful as inhibitors of treating tuberculosis.Type: ApplicationFiled: October 31, 2013Publication date: September 4, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Tiansheng Wang, Brian Hanzelka, Ute Muh, Guy Bemis, Harmon J. Zuccola
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Publication number: 20140249145Abstract: Substituted pyrazolopyrimidines and dihydropyrazolopyrimidines and related compounds, their methods of manufacture, compositions containing these compounds, and methods of use of these compounds in treating lysosomal storage disorders such as Gaucher disease are described herein. The compounds are of general Formula (I) in which variables R1-R7 and X are described in the application.Type: ApplicationFiled: December 8, 2011Publication date: September 4, 2014Applicant: THE UNITED STATES OF AMERICA, as represented by the Secretary, Department of Health and Human ServInventors: Juan Jose Marugan, Noel Southall, Ehud Goldin, Wei Zheng, Samarjit Patnaik, Ellen Sidransky, Omid Motabar, Wendy Westbroek
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Publication number: 20140248264Abstract: Methods and compositions relating to TIC10 are described according to aspects of the present invention. The compositions and methods have utility in treating disease, particularly cancer in a subject in need thereof, including a human subject as well as subjects of other species. The compositions have utility in treating brain cancer in a subject in need thereof.Type: ApplicationFiled: February 27, 2014Publication date: September 4, 2014Applicant: The Penn State Research FoundationInventors: Wafik S. El-Deiry, Joshua E. Allen, Gen Sheng Wu
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Publication number: 20140249129Abstract: This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.Type: ApplicationFiled: February 20, 2014Publication date: September 4, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Christian GNAMM, Thorsten OOST, Stefan PETERS, Klaus RUDOLF
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Patent number: 8822483Abstract: The present invention provides a catalyst complex or ligand, and compositions thereof, for use in a variety of organic reactions having high reactivity and enantioselectivity. The catalyst is a N-heterocyclic carbene having three fused rings with first and second rings being six-membered rings and the third being a five-membered ring. The first ring is fused to the second and has four substituents. The second ring has two nitrogens flanking a carbene atom with one nitrogen bound to a substituent. The carbene atom may optionally be bonded to a metal. The third ring is fused to the second ring and contains two nitrogens. The third ring of the catalyst has a double bond and two substituents on adjacent non-fused carbons. A non-fused nitrogen of the third ring is partially bonded to another substituent. Methods for the synthesis and use of the catalyst embodiments of the present invention are also provided.Type: GrantFiled: May 22, 2012Date of Patent: September 2, 2014Assignee: Florida State University Research FoundationInventors: D. Tyler McQuade, Jin Kyoon Park, Matthew D. Rexford, Hershel H. Lackey
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Patent number: 8822484Abstract: The present invention relates to novel compounds, their pharmaceutically acceptable salts, and their isomers, steroisomers, conformers, tautomers, polymorphs, hydrates and solvates. The present invention also encompasses pharmaceutically acceptable compositions of said compounds and process for preparing novel compounds. The invention further relates to the use of the above-mentioned compounds for the preparation of medicament for use as pharmaceuticals.Type: GrantFiled: August 9, 2013Date of Patent: September 2, 2014Assignee: Torrent Pharmaceuticals LimitedInventors: Sanjay Srivastava, Laxmikant Chhipa, Ramesh Chandra Gupta, Shailesh Deshpande, Anita Chaudhari, Anookh Mohanan, Chaitanya Dutt, Vijay Chauthaiwale, Murali Badanthadka, Prashant G. Jamadarkhana
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Patent number: 8822482Abstract: The invention relates to 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, its therapeutic usage for treatment of diseases mediated by EGFR kinase and its combinatory therapeutic usage together with other therapeutic agents. The invention also provides synthetic methods for preparation of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, and the relevant synthetic intermediates for synthesis of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride.Type: GrantFiled: July 7, 2009Date of Patent: September 2, 2014Assignee: Beta Pharma, Inc.Inventors: Yinxiang Wang, Guojian Xie, Lieming Ding, Fenlai Tan, Yunyan Hu, Wei He, Bin Han, Wei Long, Yong Liu, Haima Ai, Charles Davis, Don Zhang
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Publication number: 20140243320Abstract: A compound represented by the following general formula (1) or a salt thereof. R1 represents a halogen atom and so on; R2 and R3 each represent a hydrogen atom and so on; R4 and R5 each represent a hydrogen atom and so on, or R4 and R5 may form an oxo group; Ra and Rb each represent a lower alkyl group optionally having a substituent and so on, or they may bind to each other to form a nitrogen-containing heterocyclic ring which may be substituted by one or plural Rc; Rc represents an aryl group optionally having a substituent and so on; ring A represents a benzene ring and so on; and m represents 0, 1 or 2.Type: ApplicationFiled: July 12, 2012Publication date: August 28, 2014Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Takahiro Honda, Hiroshi Enomoto, Kenji Kawashima, Shinji Takaoka, Yasutaka Fujioka, Mamoru Matsuda, Koji Ohashi, Yukie Fujita, Shin-ichiro Hirai, Hiroaki Kurashima
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Patent number: 8815880Abstract: To provide a hydrochloride of a tricyclic pyrazolopyrimidine compound inhibiting the effect of HSP90 and a crystal thereof. The present invention provides a hydrochloride of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2,7-dihydro-6-thia-1,2,3,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide which inhibits the ATPase activity of HSP90 and which has antitumor activity, a crystal thereof, a medicament comprising the same, an anticancer agent comprising the same, and the like.Type: GrantFiled: February 21, 2013Date of Patent: August 26, 2014Assignee: Daiichi Sankyo Company, LimitedInventors: Shinji Matuura, Hisaki Kajino, Tomoyuki Nagai, Keijiro Kobayashi
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Patent number: 8809355Abstract: The present invention relates to novel compounds of the general formula (I) having anxiolytic, anticonvulsant, sedative-hypnotic and myorelaxant conditions as well as anxiogenic, somnolytic and convulsant conditions in mammals, including humans, as GABAA receptor modulator.Type: GrantFiled: April 2, 2009Date of Patent: August 19, 2014Assignee: Innovationspatent Sverige ABInventors: Mogens Peter Cherly Nielsen, Tommy Liljefors, Jakob Alexander Nilsson, Olov A Sterner
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Publication number: 20140228320Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):Type: ApplicationFiled: April 15, 2014Publication date: August 14, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Takahiko TANIGUCHI, Masato YOSHIKAWA, Kasei MIURA, Tomoaki HASUI, Eiji HONDA, Keisuke IMAMURA, Makoto KAMATA, Haruhi KAMISAKI, John F. QUINN, Joseph RAKER, Fatoumata CAMARA, Yi WANG
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Patent number: 8802849Abstract: The invention relates to novel tricyclic benzo[4,5]thieno-[2,3-d]pyrimidine-4-yl-amin derivatives, as well as their pharmaceutically acceptable salts. The subject of the invention too the process for producing the compounds and their use as a pharmaceutically active agent and as pharmaceutical compositions for prophylaxis and/or treatment of proliferative diseases such as cancer.Type: GrantFiled: February 19, 2008Date of Patent: August 12, 2014Assignee: Vichem Chemie Kutató Kft.Inventors: Péter Bánhegyi, György Kéri, Lászlö Örfi, Zsolt Szekélyhidi, Frigyes Wáczek
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Publication number: 20140221405Abstract: Novel compounds of formulae (I) to (VII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylfulfonamide derivatives which are effective platelet ADF receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: July 31, 2013Publication date: August 7, 2014Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles K. Marlowe, Kim A. Kane-MaGuire
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Publication number: 20140221407Abstract: Pharmaceutical compositions comprising tricyclic 3,4-propinoperhydropurines and uses thereof for the treatment of facial wrinkling are provided.Type: ApplicationFiled: April 10, 2014Publication date: August 7, 2014Applicant: Phytotox LimitedInventor: Nestor Antonio Lagos Wilson
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Publication number: 20140206536Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein X is O or S; Y is O or S; A is O, S, NR3e or C(R3c)?C(R3d); Z is a direct bond, O, S(O)n, NR6, C(R7)2O, OC(R7)2, C(?X1), C(?X1)E, EC(?X1), C(?NOR8) or C(?NN(R6)2); a is 1, 2 or 3; and R1, R2, R3a-R3e, R4, R5, R6, R7, R8, X1 and E are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: March 19, 2014Publication date: July 24, 2014Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: WENMING ZHANG, CALEB WILLIAM HOLYOKE, JR., KENNETH ANDREW HUGHES, GEORGE PHILIP LAHM, THOMAS FRANCIS PAHUTSKI, JR., MY-HANH THI TONG, MING XU
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Patent number: 8785460Abstract: There is provided a compound of the formula (I?): wherein x is a nitrogen or CRx, Rx is a hydrogen, etc., R1 is an optionally substituted hydrocarbon group, etc., R2 is an optionally substituted hydrocarbon group, etc., ring A is 5- to 8-membered heterocyclic ring, etc., and each of Y1, Y2 and Y3 is an optionally substituted carbon or a nitrogen, etc.; or a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof.Type: GrantFiled: January 21, 2009Date of Patent: July 22, 2014Assignee: Takeda Pharmaceutical Company LimitedInventors: Kazuyoshi Aso, Katsumi Kobayashi, Takafumi Takai, Takuto Kojima, Kazuyuki Tokumaru, Michiyo Mochizuki, Yasutaka Hoashi
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Patent number: 8779154Abstract: The invention relates to certain fused ring compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: GrantFiled: September 25, 2007Date of Patent: July 15, 2014Inventors: Qinglin Che, Nha Huu Vo, Shoujun Chen
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Publication number: 20140194396Abstract: The present invention relates to PDEI inhibitory compounds of Formula I as described herein, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.Type: ApplicationFiled: June 11, 2012Publication date: July 10, 2014Applicant: INTRA-CELLULAR THERAPIES, INC.Inventors: Peng Li, Hlilin Zheng, Jun Zhao, Lawrence P. Wennogle
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Publication number: 20140194414Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic[4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: March 8, 2013Publication date: July 10, 2014Applicant: MEDIVATION TECHNOLOGIES, INC.Inventor: MEDIVATION TECHNOLOGIES, INC.
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Publication number: 20140194417Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: January 8, 2014Publication date: July 10, 2014Applicant: Nimbus Iris, Inc.Inventors: Jeremy Robert Greenwood, Geraldine C. Harriman, Rosana Kapeller-Libermann, Craig E. Masse, Shaughnessy Robinson, Donna L. Romero, Mee Shelley, Ronald T. Wester
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Patent number: 8772301Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.Type: GrantFiled: December 17, 2010Date of Patent: July 8, 2014Assignee: Sunovion Pharmaceuticals, Inc.Inventors: Larry Wendell Hardy, Michele L. R. Heffernan, Frank Xinhe Wu, Kerry L. Spear, Lakshmi D. Saraswat
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Publication number: 20140187550Abstract: A compound of formula (I): in free or salt form, wherein R1, R3, Qa, Qb and Q are as defined herein, for the treatment of a disease mediated by the S1P2 or S1P3 receptor, such as inflammatory or obstructive airways disease.Type: ApplicationFiled: December 16, 2013Publication date: July 3, 2014Applicant: Novartis AGInventor: Roger John Taylor
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Patent number: 8765775Abstract: The invention relates to compounds of formula 1, tautomers and salts thereof, wherein R1, R2, R3, R4, and R5 have the meanings indicated in the specification. These compounds are receptor tyrosine kinase EphB4 inhibitors useful for the treatment of angiogenesis dependent cancers and intraocular neovascular syndromes. The invention further relates to a method termed ALTA (anchor-based library tailoring) of selecting compounds from a large compound library for screening as EphB4 inhibitors by computational procedures.Type: GrantFiled: January 23, 2009Date of Patent: July 1, 2014Assignee: Universitaet ZuerichInventors: Danzhi Huang, Peter Kolb, Karine Lafleur, Cristina Nevado, Amedeo Caflisch
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Patent number: 8765757Abstract: The present invention relates to 3-Heterocyclic Substituted Indole Derivatives, compositions comprising at least one 3-Heterocyclic Substituted Indole Derivative, and methods of using the 3-Heterocyclic Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: GrantFiled: November 13, 2008Date of Patent: July 1, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Tin-Yau Chan, Jose S. Duca, Liwu Hong, Charles A. Lesburg, Brian A. McKittrick, Haiyan Pu, Li Wang, Henry M. Vaccaro
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Publication number: 20140179682Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.Type: ApplicationFiled: June 8, 2012Publication date: June 26, 2014Applicant: SUNOVION PHARMACEUTICALS INC.Inventors: Michele L. R. Heffernan, Larry Wendell Hardy, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
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Publication number: 20140179717Abstract: A method of treating a movement abnormality associated with the pathology of a neurological movement disorder, such as Parkinson's disease or Restless Leg(s) Syndrome by administering a therapeutically effective amount of a PDE7 inhibitory agent. An aspect of the invention provides for the administration of a PDE& inhibitory agent in conjunction with a dopamine agonist or precursor, such as levodopa. In another aspect of the invention, the PDE7 inhibitory agent may be selective for PDE7 relative to other molecular targets (i) known to be involved with the pathology of Parkinson's disease or (ii) at which other drug(s) that are therapeutically effective to treat Parkinson's disease act.Type: ApplicationFiled: December 13, 2013Publication date: June 26, 2014Applicant: OMEROS CORPORATIONInventors: John E. Bergmann, Neil S. Cutshall, Gregory A. Demopulos, Vincent A. Florio, George A. Gaitanaris, Patrick Gray, John Hohmann, Rene Onrust, Hongkui Zeng
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Publication number: 20140171456Abstract: The present invention relates to certain pyrazolo[1,5-a]pyrrolo[3,2-e]pyrimidine and dipyrazolopyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrrolo[3,2-e]pyrimidine or dipyrazolopyrimidine compounds.Type: ApplicationFiled: July 20, 2012Publication date: June 19, 2014Applicant: MERCK SHARP & DOHME CORP.Inventors: Zhaoyang Meng, Arshad Siddiqui, Panduranga Abdulla P. Reddy, Mehul F. Patel, Yang Nan
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Publication number: 20140171417Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: December 17, 2013Publication date: June 19, 2014Applicant: NOVARTIS AGInventors: Mahbub AHMED, Alexander ASHALL-KELLY, Louisa GUERITZ, Jeffrey MCKENNA, Joseph MCKENNA, Simon MUTTON, Rakesh PARMAR, Jon SHEPHERD, Paul WRIGHT
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Patent number: 8754073Abstract: Piperidinodihydrothienopyrimidines of formula 1 wherein X is SO or SO2 (preferably SO), and R1, R2, R3, and R4 may have the meanings given in the disclosure and claims, pharmacologically acceptable salts thereof, and pharmaceutical compositions containing these compounds. These piperidinodihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system, or cancers.Type: GrantFiled: October 16, 2008Date of Patent: June 17, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Pascale Pouzet, Ralf Anderskewitz, Horst Dollinger, Dennis Fiegen, Thomas Fox, Rolf Goeggel, Christoph Hoenke, Domnic Martyres, Peter Nickolaus, Klaus Klinder
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Publication number: 20140163052Abstract: Compounds of Formula I are useful inhibitors of CDK 4, CDK6, and FLT3. Such compounds are useful in treating cancer and various other disease conditions. Compounds of Formula I have the following structure: where R1 is a group of Formula IA, Formula IB, Formula IC, or Formula ID and the definitions of the other variables are provided herein.Type: ApplicationFiled: November 25, 2013Publication date: June 12, 2014Applicant: AMGEN INC.Inventors: Xiaoqi Chen, Kang Dai, Jason Duquette, Michael W. Gribble, JR., Justin N. Huard, Kathleen S. Keegan, Zhihong Li, Sarah E. Lively, Lawrence R. McGee, Mark L. Ragains, Xianghong Wang, Margaret F. Weidner, Jian Zhang
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Publication number: 20140163051Abstract: Pharmaceutical compositions comprising tricyclic 3,4-propinoperhydropurines and uses thereof for the treatment of facial wrinkling are provided.Type: ApplicationFiled: October 1, 2013Publication date: June 12, 2014Applicant: Phytotox LimitedInventor: Nestor Antonio Lagos Wilson
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BRIDGED BICYCLIC ARYL AND BRIDGED BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS
Publication number: 20140155386Abstract: Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: December 2, 2013Publication date: June 5, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak -
Publication number: 20140155384Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor a2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2? and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.Type: ApplicationFiled: February 17, 2012Publication date: June 5, 2014Applicant: Medivation Technologies, Inc.Inventors: Andrew Asher Protter, Sarvajit Chakravarty