Additional Hetero Atom In The Polycyclo Ring System Patents (Class 514/215)
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Publication number: 20140357622Abstract: The present invention is directed to a compound of formula (I): or a crystalline form thereof, or a solvate thereof; to a solid pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula (I), or a crystalline form thereof, or a solvate thereof, and at least one pharmaceutically acceptable carrier or diluent, and to the use of a compound of formula (I), or a crystalline form thereof, or a solvate thereof, for treating a patient suffering from, or subject to, a disease, disorder, or condition mediated by Aurora kinase, and methods related thereto.Type: ApplicationFiled: January 9, 2014Publication date: December 4, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Ian Armitage, Martin I. Cooper, Mark D. Eddleston, Neil C. Faiber, Quentin J. McCubbin, Stephen W. Watt
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Publication number: 20140349994Abstract: The present invention relates to novel compounds of Formula (I), wherein M and R1 are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: January 18, 2013Publication date: November 27, 2014Inventors: Christelle Bolea, Cedric Boudou, Sylvain Celanire, Vincent Darmency, Celine Mordant, Vincent Pericolle, Yannick Regereau, Jean-Philippe Rocher, Radouane Souissi, Lam Tang
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Patent number: 8895544Abstract: A method of treating a disease or condition for which a JAK inhibitor is indicated in a subject in need of such treatment, comprising administering to the subject a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, and particularly, a method for the treatment of various inflammatory diseases, particularly psoriasis, asthma and COPD.Type: GrantFiled: September 30, 2013Date of Patent: November 25, 2014Assignee: Pfizer LimitedInventors: Jotham Wadsworth Coe, Christoph Martin Dehnhardt, Peter Jones, Steven Wade Korturn, Yogesh Anil Sabnis, Florian Michel Wakenhut, Gavin Alistair Whitlock
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Patent number: 8889667Abstract: Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.Type: GrantFiled: December 29, 2011Date of Patent: November 18, 2014Assignee: Agios Pharmaceuticals, IncInventors: Francesco G. Salituro, Jeffrey Saunders, Shunqi Yan
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Publication number: 20140336180Abstract: The present invention relates to methods for the treatment of proliferative disorders. In particular, the invention provides methods for treatment of proliferative disorders by administering a MEK inhibitor in combination with a selective inhibitor of Aurora A kinase.Type: ApplicationFiled: June 4, 2012Publication date: November 13, 2014Applicants: TAKEDA PHARMACEUTICAL COMPANY LIMITED, Millennium Pharmaceuticals, Inc.Inventors: Arijit Chakravarty, Patrick Vincent
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Publication number: 20140323423Abstract: Systems and methods for longevity, anti-aging, fatigue management, obesity, weight loss, weight management, delivery of nutraceuticals, and treating hyperglycemia, Alzheimer's disease, sleep disorders, Parkinson's disease, Attention Deficit Disorder and nicotine addiction involve synchronizing and tailoring the administration of nutraceuticals, medications and other substances (for example, stimulants) in accordance with the body's natural circadian rhythms, meal times and other factors. Improved control of blood glucose levels, extended alertness, and weight control, and counteracting of disease symptoms when they are at their worst are possible.Type: ApplicationFiled: May 2, 2014Publication date: October 30, 2014Applicant: Chrono Therapeutics, Inc.Inventors: Guy DiPierro, Steven A. Giannos
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Publication number: 20140315892Abstract: The present invention relates to (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane and pharmaceutically acceptable salts thereof, compositions comprising (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and methods for treating or preventing an alcohol-related or addictive disorder. The (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.Type: ApplicationFiled: January 31, 2014Publication date: October 23, 2014Inventors: Anthony Alexander McKinney, Franklin Porter Bymaster
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Patent number: 8865641Abstract: A method of treating a fatty liver disease in a subject. The method comprises administering to the subject an effective amount of a cholinergic pathway stimulating agent, wherein the fatty liver disease is selected from non-alcoholic fatty liver (NAFL), alcoholic fatty liver (AFL), non-alcoholic steatohepatitis (NASH), alcoholic steatohepatitis (ASH), NASH-associated liver fibrosis, ASH-associated liver fibrosis, non-alcoholic cirrhosis, and alcoholic cirrhosis.Type: GrantFiled: June 14, 2012Date of Patent: October 21, 2014Assignee: The Feinstein Institute for Medical ResearchInventors: Valentin A. Pavlov, Kevin J. Tracey
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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: 20140303144Abstract: 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 adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?2B. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.Type: ApplicationFiled: February 17, 2012Publication date: October 9, 2014Applicant: Medivation Technologies, Inc.Inventors: Andrew Asher Protter, Sarvajit Chakravarty
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Publication number: 20140296209Abstract: 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 adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?1B—The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.Type: ApplicationFiled: February 17, 2012Publication date: October 2, 2014Applicant: MEDIVATION TECHNOLOGIES, INC.Inventors: Andrew Asher Protter, Sarvajit Chakravarty
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Publication number: 20140296206Abstract: Compounds and compositions useful for treating disorders related to Kit are described herein.Type: ApplicationFiled: March 14, 2014Publication date: October 2, 2014Applicant: BLUEPRINT MEDICINES CORPORATIONInventors: Lucian V. DiPietro, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Steven Mark Wenglowsky, Douglas Wilson, Yulian Zhang
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Publication number: 20140296211Abstract: This invention concerns a dosage form comprising a therapeutically neuroprotective amount of A2-73 and a neuroprotective amount of at least one cooperating acetylcholinesterase inhibitor selected from the group consisting of donepezil, galantamine, rivastigmine, or memantine and method of use.Type: ApplicationFiled: July 12, 2013Publication date: October 2, 2014Applicant: ANAVEX LIFE SCIENCES CORP.Inventors: Alexandre Vamvakides, Tangui Maurice
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Patent number: 8846951Abstract: The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) wherein R1, R2, R3, R4, R5, A, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.Type: GrantFiled: November 19, 2010Date of Patent: September 30, 2014Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KGInventors: Irini Akritopoulou-Zanze, Wilfried Braje, Stevan W. Djuric, Noel S. Wilson, Sean C. Turner, Albert W. Kruger, Ana-Lucia Relo, Shashank Shekhar, Dennie S. Welch, Hongyu Zhao, Jorge Gandarilla, Alan F. Gasiecki, Huanqiu Li, Christina M. Thompson, Min Zhang
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Publication number: 20140288057Abstract: There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetylcholinesterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-anticholinergic antiemetic agent, whereby an enhanced acetylcholinesterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-anticholinergic antiemetic agent for the preparation of a pharmaceutical composition for the treatment of Alzheimer type dementia in combination with an acetylcholinesterase inhibitor (AChEI) and pharmaceutical compositions comprising (a) a 5HT3 receptor antagonist, a dopamine antagonist, a H1-receptor antagonist, a cannabinoid agonist, aprepitant or casopitant as an antiemetic agent and (b) an acetylcholinesterase inhibitor are also described.Type: ApplicationFiled: March 18, 2014Publication date: September 25, 2014Applicant: CHASE PHARMACEUTICALS CORPORATIONInventors: Thomas N. CHASE, Kathleen E. CLARENCE-SMITH
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Publication number: 20140286899Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.Type: ApplicationFiled: November 18, 2013Publication date: September 25, 2014Applicant: Presidio Pharmaceuticals, Inc.Inventors: Min Zhong, Leping Li
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Publication number: 20140275036Abstract: There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-selective, peripheral anticholinergic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent.Type: ApplicationFiled: May 29, 2014Publication date: September 18, 2014Applicant: Chase Pharmaceuticals CorporationInventors: Thomas N. CHASE, Kathleen E. CLARENCE-SMITH
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Publication number: 20140275035Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are thienylindole azepines. These compounds are serotonin receptor (5-HT2c) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT2c) is desired (e.g. addiction, anxiety, depression, obesity, and others).Type: ApplicationFiled: March 7, 2014Publication date: September 18, 2014Applicant: ABT Holding CompanyInventors: Michael Robarge, Michelle Zawadski, John Harrington
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Patent number: 8835423Abstract: The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: GrantFiled: September 20, 2013Date of Patent: September 16, 2014Assignee: Incyte CorporationInventors: Argyrios G. Arvanitis, James D. Rodgers, Andrew P. Combs, Richard B. Sparks, Darius J. Robinson
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Publication number: 20140249125Abstract: A polyacrylate formulation suitable for delivery of drug to through a body surface of an individual. By loading the drug and permeation enhancers at a high concentration into a polyacrylate proadhesive that has inadequate adhesive properties for typical adhesive application on the skin, a formulation with desirable adhesive characteristics and effective therapeutic properties can be made. The proadhesive has higher glass transition temperature than typical pressure sensitive adhesives.Type: ApplicationFiled: May 9, 2014Publication date: September 4, 2014Applicant: ALZA CorporationInventors: Jay Audett, Jianye Wen, Eli J. Goldman, Robert M. Gale, Allison Luciano, Paul B. Foreman, Eric N. Silverberg
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Patent number: 8815843Abstract: 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 ?2A. 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 ?2B 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: GrantFiled: February 17, 2012Date of Patent: August 26, 2014Assignee: Medivation Technologies, Inc.Inventors: Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain, Michael John Green
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Patent number: 8815842Abstract: Disclosed is an anti-foot-and-mouth disease virus agent for an animal belonging to the Family Suidae, which comprises 3-oxo-3,4-dihyro-2-pyrazincarboxamide or a salt thereof. The agent is extremely useful for the prevention or treatment of food-and-mouth disease in an animal belonging to the Family Suidae. Also disclosed is an anti-foot-and-mouth disease virus agent for sheep, which comprises 3-oxo-3,4-dihyro-2-pyrazincarboxamide or a salt thereof. The agent is extremely useful for the prevention, therapy or the like of food-and-mouth disease in sheep.Type: GrantFiled: May 29, 2007Date of Patent: August 26, 2014Assignee: Toyama Chemical Co., Ltd.Inventor: Yousuke Furuta
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Publication number: 20140228353Abstract: 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 ?2A. 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 ?2B 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: August 14, 2014Applicant: Medivation Technologies, Inc.Inventors: Andrew Asher Protter, Sarvvajit Chakravarty
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Patent number: 8796262Abstract: This invention relates to new fused heterocyclic derivatives having affinity to S1P receptors, a pharmaceutical composition containing said compounds, as well as the use of said compounds for the preparation of a medicament for treating, alleviating or preventing diseases and conditions in which any S1P receptor is involved or in which modulation of the endogenous S1P signaling system via any S1P receptor is involved.Type: GrantFiled: July 8, 2011Date of Patent: August 5, 2014Assignees: AbbVie B.V., AbbVie Inc.Inventors: Pieter Smid, Wouter I. Iwema Bakker, Hein K. A. C. Coolen, Leonardus A. J. M. Sliedregt, Maria J. P. van Dongen, Jacobus A. J. den Hartog, Adrian Hobson
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Patent number: 8796261Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. 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: GrantFiled: December 2, 2011Date of Patent: August 5, 2014Assignee: Constellation Pharmaceuticals, Inc.Inventors: Brian K. Albrecht, James E. Audia, Alexandre Côté, Victor S. Gehling, Jean-Christophe Harmange, Michael C. Hewitt, Yves Leblanc, Christopher G. Nasveschuk, Alexander M. Taylor, Rishi G. Vaswani
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Publication number: 20140213577Abstract: This disclosure relates to new azepino[4,5-b]indole compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new 1,2,3,4,5,6-tetrahydroazepino[4,5-b]indoles. Pharmaceutical compositions are also provided.Type: ApplicationFiled: October 8, 2013Publication date: July 31, 2014Applicant: MEDIVATION TECHNOLOGIES, INC.Inventors: David T. HUNG, Andrew Asher PROTTER, Rajendra Parasmal JAIN, Sarvajit CHAKRAVARTY
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Publication number: 20140206671Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: January 27, 2014Publication date: July 24, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Youssef Bennani, Tianseng Wang, Francesco Salituro, John P. Duffy
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Publication number: 20140206664Abstract: Heterocycle amino alkyloxy substituted quinazoline derivatives as represented by the structural Formula (I) and pharmaceutically acceptable salts thereof, capable of inhibiting the activity of receptor tyrosine kinase EGFR, and being used to treat cancers related to the expression of the receptor tyrosine kinase of the ErbB family are provided.Type: ApplicationFiled: December 13, 2012Publication date: July 24, 2014Inventor: Wei Qian
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Publication number: 20140206672Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are thiophenyl and pyrrolyl azepine compounds. These compounds are serotonin receptor (5-HT2c) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT2c) is desired (e.g. addiction, anxiety, depression, obesity, and others).Type: ApplicationFiled: March 19, 2014Publication date: July 24, 2014Applicant: ABT Holding CompanyInventors: L. Nathan Tumey, David C. Bom, Youssef L. Bennani, Michael J. Robarge
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Publication number: 20140194411Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are benzazepine compounds. These compounds are serotonin receptor (5-HT2c) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT2c) is desired (e.g. addiction, anxiety, depression, obesity, and others).Type: ApplicationFiled: December 23, 2013Publication date: July 10, 2014Applicant: ABT Holding CompanyInventors: Mike Robarge, John Harrington, David Gerrish, John Mecom
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Publication number: 20140187537Abstract: This disclosure relates to diagnostic and therapeutic methods and systems related thereto. In certain embodiments, the disclosure contemplates methods of improving chemotherapy treatments by administering chemotherapy agents, analyzing CHFR gene expression, methylation, or both, and determining an appropriate therapeutic strategy. Analysis of data herein revealed that reduced CHFR expression levels was a predictor of improved overall survival of subject with non-small cell lung cancer.Type: ApplicationFiled: January 2, 2014Publication date: July 3, 2014Applicant: EMORY UNIVERSITYInventor: Johann C. Brandes
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Publication number: 20140179676Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: December 20, 2013Publication date: June 26, 2014Applicant: ABBVIE INC.Inventors: Kevin P. Cusack, Thomas D. Gordon, Michael Z. Hoemann, David C. Ihle, Bin Li, Gloria Y. Lo Schiavo, Gagandeep K. Somal, Michael Friedman, Martin E. Hayes, Wouter Iwema Bakker
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Publication number: 20140161731Abstract: Described are a compound of formula (II) or (III): The compounds are effective in the treatment of disease, including a tauopathy condition or a disease of tau protein aggregation.Type: ApplicationFiled: February 14, 2014Publication date: June 12, 2014Applicant: WisTa Laboratories Ltd.Inventors: Scott Clunas, John Mervyn David Storey, Janet Elizabeth Rickard, David Horsley, Charles Robert Harrington, Claude Michel Wischik
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Publication number: 20140163012Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described.Type: ApplicationFiled: October 31, 2013Publication date: June 12, 2014Applicant: Albany Molecular Research, Inc.Inventors: Matthew D. SURMAN, Emily E. FREEMAN, Peter R. GUZZO, Alan J. HENDERSON, Mark HADDEN
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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
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Publication number: 20140155369Abstract: An agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that activates a serotonin 5-HT2C receptor, an agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that stimulates an androgen binding site, and a method of screening for a drug for the prophylaxis or treatment of abdominal pressure incontinence, which includes electrostimulating the abdominal muscles or a nerve controlling them of an animal to increase the abdominal pressure, and measuring the leak point pressure at that time.Type: ApplicationFiled: January 16, 2014Publication date: June 5, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Izumi KAMO, Tadatoshi HASHIMOTO
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Publication number: 20140148440Abstract: The present invention relates to heterocyclyl compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to Histamine H3 receptors, for example cognitive disorders, sleep disorders, obesity and pain.Type: ApplicationFiled: November 15, 2010Publication date: May 29, 2014Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Ramasastri Kambhampati, Rambabu Namala, Adi Reddy Dwarampudi, Laxman Kota, Murlimohan Gampa, Padmavathi Kodru, Taraka Naga Vinaykumar Tiriveedhi, Vishwottam Nagaraj Kandikere, Nageshwara Rao Muddana, Ramanatha Shrikantha Saralaya, Pradeep Jayarajan, Dhanalakshmi Shanmuganathan, Ishtiyaque Ahmad, Venkateswarlu Jasti
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Publication number: 20140135311Abstract: Certain tetrahydro-pyrimidoazepine compounds are described, which are useful as TRPV1 modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by TRPV1. Thus, the compounds may be administered to treat, e.g., pain, itch, cough, asthma, or inflammatory bowel disease.Type: ApplicationFiled: January 17, 2014Publication date: May 15, 2014Applicant: Janssen Pharmaceutica NVInventors: Brett D. Allison, Bryan James Branstetter, J. Guy Breitenbucher, Michael D. Hack, Natalie A. Hawryluk, Alec D. Lebsack, Kelly J. McClure, Jeffrey E. Merit
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Patent number: 8716277Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: GrantFiled: December 10, 2012Date of Patent: May 6, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Klaus Rudolf, Daniel Bischoff, Georg Dahmann, Matthias Grauert, Raimund Kuelzer, Bernd Wellenzohn
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Patent number: 8716276Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are thiophenyl and pyrrolyl azepine compounds. These compounds are serotonin receptor (5-HT2c) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT2c) is desired (e.g. addiction, anxiety, depression, obesity, and others).Type: GrantFiled: January 12, 2011Date of Patent: May 6, 2014Assignee: Athersys, Inc.Inventors: L. Nathan Tumey, David C. Bom, Youssef L. Bennani, Michael J. Robarge
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Patent number: 8703762Abstract: A method for treating organophosphorous poisoning (OP) comprising administering to a mammal at risk for OP poisoning an OP poisoning-inhibiting amount of galantamine.Type: GrantFiled: February 14, 2011Date of Patent: April 22, 2014Assignees: University of Maryland Baltimore, The United States of America as repr. by the Sec. of the Army, U.S. Army Med. Resr. Inst. of Chem. DefenseInventors: Edson X. Albuquerque, Michael Adler, Edna F.R. Pereira
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Publication number: 20140107103Abstract: Dihydrothienopyrimidinesulphoxides of formula 1 wherein X is SO or SO2, R1 is H or C1-6-alkyl, R2 is H or an organic group as disclosed herein, and R3 is an optionally substituted, mono- or bicyclic, unsaturated, partially saturated or saturated heterocycle or an optionally substituted, mono- or bicyclic heteroaryl, and the pharmacologically acceptable salts thereof, as well as pharmaceutical compositions which contain these compounds. These dihydrothienopyrimidinesulphoxides 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: ApplicationFiled: December 19, 2013Publication date: April 17, 2014Applicant: 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: 20140100218Abstract: The present invention relates to methods of treatment using [3-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-propyl]-diethyl amine (“COMPOUND I”) or a pharmaceutically acceptable salt thereof. In various embodiments, the methods of treatment include treatment of mild-to-moderate dementia of Alzheimer's type, diabetes, insomnia, and other indications. The present invention also relates to pharmaceutical compositions comprising COMPOUND I or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 22, 2013Publication date: April 10, 2014Applicant: TransTech Pharma, LLCInventors: Cesare Orlandi, David J. Clark, Imogene M. Grimes, Maria Carmen Valcarce Lopez, Matthew J. Kostura
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Publication number: 20140088087Abstract: This disclosure relates to new azepino[4,5-b]indole compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new 1,2,3,4,5,6-tetrahydroazepino[4,5-b]indoles. Pharmaceutical compositions are also provided.Type: ApplicationFiled: March 8, 2013Publication date: March 27, 2014Applicant: MEDIVATION TECHNOLOGIES, INC.Inventor: MEDIVATION TECHNOLOGIES, INC.
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Publication number: 20140086910Abstract: The present invention provides indane acetic acid and their derivatives and methods for the treating and/or preventing of Alzheimer's diseases.Type: ApplicationFiled: August 29, 2013Publication date: March 27, 2014Applicant: DARA BIOSCIENCES, INC.Inventor: Mary Katherine Delmedico
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Publication number: 20140088081Abstract: The invention provides PDE9-inhibiting compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, A, and n are as defined herein. Pharmaceutical compositions containing the compounds of Formula I, and uses thereof in treating neurodegenerative and cognitive disorders, such as Alzheimer's disease and schizophrenia, are also provided.Type: ApplicationFiled: November 27, 2013Publication date: March 27, 2014Applicant: Pfizer Inc.Inventors: Michelle Marie Claffey, Christopher John Helal, Patrick Robert Verhoest
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Publication number: 20140088086Abstract: 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 adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?1B. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.Type: ApplicationFiled: March 7, 2013Publication date: March 27, 2014Applicant: MEDIVATION TECHNOLOGIES, INC.Inventor: Medivation Technologies, Inc.
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Publication number: 20140080801Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: November 18, 2013Publication date: March 20, 2014Applicant: Genentech, Inc.Inventors: Alastair James Hodges, Mizio Matteucci, Andrew Sharpe, Minghua Sun, Xiaojing Wang, Vickie H. Tsui
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Publication number: 20140080811Abstract: NSC antagonists are disclosed as useful in the treatment of dementia, in delaying the onset of dementia, and in the prevention of dementia. Dementia so treated may be, for example, Alzheimer's Disease (AD). NSC antagonists for treating dementia such as AD may be administered alone, a) in combination with other drugs used for treating dementia, b) in combination with drugs that stabilize or increase blood plasma glucose levels, or with both a) and b). Pharmaceutical compositions, dosage forms, and methods for using the same are disclosed, which include NSC antagonists, NSC antagonists combined with dementia drugs, NSC antagonists combined with glucose-level stabilizing or enhancing drugs, or combinations of these. Dosage forms may be designed to provide stable plasma levels for extended periods of time.Type: ApplicationFiled: February 27, 2013Publication date: March 20, 2014Applicant: Remedy Pharmaceuticals, Inc.Inventor: Remedy Pharmaceuticals, Inc.
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Patent number: 8673895Abstract: Certain tetrahydro-pyrimidoazepine compounds are described, which are useful as TRPV1 modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by TRPV1. Thus, the compounds may be administered to treat, e.g., pain, itch, cough, asthma, or inflammatory bowel disease.Type: GrantFiled: March 21, 2007Date of Patent: March 18, 2014Assignee: Janssen Pharmaceutica NVInventors: Bryan James Branstetter, James Guy Breitenbucher, Natalie A. Hawryluk, Alec D. Lebsack, Jeffrey E. Merit