Carbocyclic Ring Bonded Directly To The Piperazine Ring Patents (Class 514/255.03)
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Patent number: 8710059Abstract: The present invention relates to N-Phenyl-(homo)piperazinyl-benzenesulfonyl or benzenesulfonamide compounds of formula I wherein the variables have the meanings given in the claims and the description, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.Type: GrantFiled: November 1, 2011Date of Patent: April 29, 2014Assignees: Abbott Laboratories, AbbVie Deutschland GmbH & Co. KGInventors: Andreas Haupt, Frauke Pohlki, Liliane Unger, Ana Lucia Relo, Karsten Wicke, Min Zhang
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Publication number: 20140113913Abstract: Some embodiments are based on the discovery that proliferative diseases (e.g., neoplastic diseases, for example, tumors or cancers) having an FBW7 mutation or other FBW7 deficiency are sensitive to Mcl1 inhibiting agents, but resistant to pro-apoptotic drugs that do not inhibit Mcl1. Some embodiments provide methods of treating a proliferative disease based on an assessment of FBW7 expression level or mutation status. Some embodiments provide methods of classifying a hyperproliferative cell or cell population, for example, a malignant cell or cell population based on an assessment of FBW7 expression level or mutation status. Some embodiments provide methods of selecting a treatment regimen for treating a proliferative disease, for example, a malignant disorder, based on an assessment of FBW7 expression level or mutation status.Type: ApplicationFiled: March 2, 2012Publication date: April 24, 2014Applicant: Beth Israel Deaconess Medical Center, Inc.Inventor: Wenyi Wei
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Publication number: 20140107027Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.Type: ApplicationFiled: December 18, 2013Publication date: April 17, 2014Applicant: BHI LIMITED PARTNERSHIPInventors: Xianqi Kong, David Migneault, Isabelle Valade, Xinfu Wu, Francine Gervais
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Publication number: 20140086834Abstract: The invention relates to a new class of compounds able to inhibit with high affinity and selectivity the 5-HT7 receptor. The invention also relates to the utilization of such compounds as medicaments useful in the treatment and prevention of 5-HT7 receptor relating disorders of the central nervous system. The invention also relates to the isotopically labeled compounds for use in vivo diagnosis or imaging of a 5-HT7 condition.Type: ApplicationFiled: May 24, 2011Publication date: March 27, 2014Applicant: UNIVERSITA' DEGLI STUDI DI BARI ''ALDO MORO''Inventors: Marcello Leopoldo, Enza Lacivita, Nicola Colabufo, Paola De Giorgio, Francesco Berardi, Roberto Perrone
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Patent number: 8680105Abstract: The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT1A receptor subtype, comprising as an active ingredient a carbostyril derivative or a salt thereof represented by the formula (1): wherein the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or a double bond.Type: GrantFiled: December 15, 2011Date of Patent: March 25, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Shaun Jordan, Tetsuro Kikuchi, Katsura Tottori, Tsuyoshi Hirose, Yasufumi Uwahodo
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Patent number: 8669247Abstract: Provided herein are 2,5-disubstituted arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: GrantFiled: March 18, 2013Date of Patent: March 11, 2014Assignee: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Marie Chantal Siu-Ying Tran, Erik Dean Raaum
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Patent number: 8664225Abstract: The use of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine in the treatment of pain and residual symptoms in depression is provided.Type: GrantFiled: March 14, 2008Date of Patent: March 4, 2014Assignee: H. Lundbeck A/SInventors: Nicholas Moore, Tine Bryan Stensbol
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Publication number: 20140057890Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: October 18, 2013Publication date: February 27, 2014Applicant: AbbVie Inc.Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
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Publication number: 20140057889Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: October 18, 2013Publication date: February 27, 2014Applicant: AbbVie Inc.Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
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Publication number: 20140051710Abstract: The present invention relates to novel crystalline forms of carbarmoyl-cyclohexane derivatives and, more particularly, to novel co-crystalline forms of trans-1{4-[2-[4-(2,3-dichlorophenyl-piperazin-1-yl]-ethyl]-cyclohexyl}-3,3-dimethly urea hydrochloride and an acid such as fumaric acid. Processes for preparing these forms, compositions containing these forms, and methods of use thereof are also described.Type: ApplicationFiled: March 14, 2013Publication date: February 20, 2014Inventors: Xiangmin Liao, Hiajian (Jim) Zhu, Andreas Grill
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Publication number: 20140038945Abstract: The invention includes a compound of formula I: wherein R1, X, Z, n, and m have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds ate inhibitors of PDE4function and are useful for improving cognitive function in animals.Type: ApplicationFiled: July 31, 2013Publication date: February 6, 2014Applicant: DART NEUROSCIENCE (CAYMAN) LTDInventors: Terence P. Keenan, Alan P. Kaplan
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Publication number: 20140038979Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: October 14, 2013Publication date: February 6, 2014Applicant: Janssen Pharmaceutica NVInventors: Kristof VAN EMELEN, Janine Arts, Leo-Jacobus Jozef Backx, Hans Louis Jos De Winter, Sven Franciscus Anna Van Brandt, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Isabelle Noelle Constance Pilatte, Virginie Sophie Poncelet, Alexey Borisovich Dyatkin, Jimmy Arnold Viviene Van Heusden
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Publication number: 20140031363Abstract: Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: wherein: each (L)k-Ar1 is a substituted or unsubstituted, mono or bicyclic aryl or heteroaryl; W is a bond, alkyl, or alkenyl; X is a bond, NR1 or O and each R1 and R2 is independently H, alkyl, alkenyl or aralkyl or R1 and R2 taken together form a 5-8 membered ring; R3-R6 are selected from certain specific substituents or a carbonyl; Y is a bond, O, S, SO, SO2, CH2, NH, N(alkyl), or NHC(?O); and Z is OH, NR6R7, NR8SO2(alkyl), NR8C(O)NR6R7, NR8C(O)O(alkyl), NR8-dihydrothiazole, or NR8-dihydroimidazole or wherein Z can fuse with Ar2 to form selected heterocycles.Type: ApplicationFiled: April 15, 2013Publication date: January 30, 2014Inventors: Dennis C. Liotta, James P. Snyder, Stephen F. Traynelis, Lawrence Wilson, Cara Mosley, Raymond J. Dingledine, Scott Myers, Yesim Altas Tahirovic
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Patent number: 8633197Abstract: The invention relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof, and methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.Type: GrantFiled: June 5, 2008Date of Patent: January 21, 2014Assignee: Janssen Pharmaceutica N.V.Inventors: Jean-Pierre André Marc Bongartz, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Christophe Francis Robert Nestor Buyck
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Patent number: 8624027Abstract: The present disclosure relates to a combination of therapeutic agents for use in treating a patient a subject suffering from cancer. In addition, the present disclosure also relates to diagnostic assays useful in classification of patients for treatment with one or more therapeutic agents.Type: GrantFiled: December 4, 2009Date of Patent: January 7, 2014Assignee: AbbVie Inc.Inventors: Omar Jameel Shah, Yu Shen, Xiaoyu Lin, Mark Anderson, Xiaoli Huang, Junling Li, Leiming Li
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Patent number: 8618135Abstract: The present invention provides methods and compositions for treating hyperlipidemia and/or hypercholesterolemia comprising administering to the subject an effective amount of an MTP inhibitor to inhibit hyperlipidemia and/or hypercholesterolemia in said subject, wherein said administration comprises an escalating series of doses of the MTP inhibitor. In some embodiments the method comprises administering at least three step-wise, increasing dosages of the MTP inhibitor to the subject. In some embodiments, the method further comprises the administration of one or more other lipid modifying compounds.Type: GrantFiled: March 11, 2011Date of Patent: December 31, 2013Assignee: The Trustees of the University of PennsylvaniaInventor: Daniel J. Rader
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Patent number: 8609665Abstract: The present invention relates to novel solvate and crystalline forms of carbamoyl-cyclohexane derivatives and, more particularly, to novel solvate and crystalline forms of trans-1{4-[2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl]-cyclohexyl}-3,3-dimethyl-urea hydrochloride. Processes for the preparation of these forms, compositions containing these forms, and methods of use thereof are also described.Type: GrantFiled: October 5, 2010Date of Patent: December 17, 2013Inventors: Xiangmin Liao, Haijian Zhu, Andreas Grill
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Patent number: 8604021Abstract: The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.Type: GrantFiled: May 10, 2011Date of Patent: December 10, 2013Inventors: Oren Becker, Rosa Melendez, Yael Marantz, Anurag Sharadendu, Merav Fichman, Mercedes Lobera, Hanoch Senderowitz, Srinivasa Rao Cheruku, Sharon Shacham, Laurence Wu, Ashis Saha, Pini Orbach, Dale S. Dhanoa
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Publication number: 20130324507Abstract: The present invention concerns novel (aza)benzhydryl ether derivatives which exhibit H4-receptor binding activity. The present invention also concerns their process of preparation and their therapeutical uses.Type: ApplicationFiled: June 5, 2013Publication date: December 5, 2013Applicant: BIOPROJETInventors: Isabelle BERREBI-BERTRAND, Xavier BILLOT, Thierry CALMELS, Marc CAPET, Stéphane KRIEF, Olivier LABEEUW, Jeanne-Marie LECOMTE, Nicolas LEVOIN, Xavier LIGNEAU
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Publication number: 20130317043Abstract: The invention relates to a compound of Formula I:Type: ApplicationFiled: May 6, 2013Publication date: November 28, 2013Applicants: President and Fellows of Harvard College, The Broad Institute, Inc.Inventors: The Broad Institute, Inc., President and Fellows of Harvard College
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Patent number: 8575174Abstract: The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D1 and D2 as well as the 5HT2 receptors in the central nervous system, to medicaments comprising such compounds as active ingredients, to the use of such compounds in the treatment of diseases in the central nervous system, and to methods of treatment comprising administration of such compounds.Type: GrantFiled: June 19, 2012Date of Patent: November 5, 2013Assignee: H. Lundbeck A/SInventors: Morten Jorgensen, Peter Hongaard Andersen, Klaus Gjervig Jensen, Mette Graulund Hvenegaard, Lassina Badolo, Mikkel Fog Jacobsen
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Publication number: 20130289049Abstract: The present invention relates to the new acid addition salts AB of the following free base of formula A or the enantiomer thereof with a physiologically acceptable acid B which is selected from among hydrochloric acid, fumaric acid and tartaric acid, as well as the polymorphs, hydrates and solvates thereof.Type: ApplicationFiled: August 4, 2011Publication date: October 31, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Thorsten Pachur, Waldemar Pfrengle, Manfred Birk, Juergen Schnaubelt, Ulrike Werthmann
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Publication number: 20130281436Abstract: The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D1 and D2 as well as the 5HT2 receptors in the central nervous system, to medicaments comprising such compounds as active ingredients, to the use of such compounds in the treatment of diseases in the central nervous system, and to methods of treatment comprising administration of such compounds.Type: ApplicationFiled: June 24, 2013Publication date: October 24, 2013Inventors: Morten JORGENSEN, Peter Hongaard ANDERSEN, Klaus Gjervig JENSEN, Mette Graulund HVENEGAARD, Lassina BADOLO, Mikkel Fog JACOBSEN
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Publication number: 20130281462Abstract: Disclosed herein are compounds (for example, diamidine derivatives and prodrugs) and methods of use thereof, for example in treating muscular dystrophy (DM) or disease caused by a toxic RNA in a subject. In some embodiments, the methods include administering an effective amount of one of more of the disclosed compounds to a subject to treat or inhibit DM or a disease caused by or associated with toxic RNA, such as DM1, DM2, spinocerebellar ataxia type 8 (SCA8), fragile X tremor ataxia syndrome (FXTAS), or Huntington disease-like 2 (HLD2). In some examples, the methods include selecting a subject for treatment, for example selecting a subject with DM1, DM2, SCA8, FXTAS, or HLD2.Type: ApplicationFiled: April 19, 2013Publication date: October 24, 2013Applicants: University of OregonInventor: State of Oregon, acting by and through the State Board of Higher Education, on behalf of the University of Oregon
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Publication number: 20130274270Abstract: Polymorphs of 3-chloro-4[(2R)-2-(4-chlorophenyl)-4-[(1R)-1-(4-cyanophenyl)ethyl]-1-piperazinyl]-benzonitrile are disclosed, as well as pharmaceutical compositions comprising said polymorphs, methods of using the polymorphs, and a process for preparing them.Type: ApplicationFiled: December 21, 2011Publication date: October 17, 2013Inventors: Monika Brink, Hans-Peter Niedermann, Marcus Knell, Tao Feng, Scott T. Trzaska, Arthur J. Cooper, Shaileshkumar Ramanial Desai, Vinayak Keshav Gore
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Publication number: 20130267536Abstract: The present invention relates to novel substituted methyl-amines, serotonin 5-HT6 receptor antagonists, to active components, pharmaceutical compositions, method for prophylaxis and treatment of CNS diseases and “molecular tools”, in which novel substituted methyl-amines represent compounds of the general formula 1 and their crystalline forms and pharmaceutically acceptable salts, wherein: W represents benzene, naphthalene, indolizine, quinoline or oxazole cycle; R1=H, F, Cl; R2 represents hydrogen, fluoro, methyl, phenyl, thienyl, furan-2-yl, pyridyl, piperazin-1-yl or 4-methylpiperazin-1-yl; R3 represents cyclopropyl or optionally substituted methyl; with the exception of the compounds in which W simultaneously represents oxazole cycle and R2=phenyl or pyridyl.Type: ApplicationFiled: December 13, 2011Publication date: October 10, 2013Applicant: ALLA CHEM, LLCInventors: Alexandre Vasilievich Ivachtchenko, Oleg Dmitrievich Mitkin, Madina Georgievna Kadieva
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Publication number: 20130252970Abstract: Disclosed herein are new methods of treatment of non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and other fibrotic diseases of the liver in a subject by modulating PPAR? with sulfonyl-substituted bicyclic compounds and compositions as pharmaceuticals.Type: ApplicationFiled: May 14, 2013Publication date: September 26, 2013Applicant: KALYPSYS, INC.Inventors: Mausumee Guha, Paul Grint
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Patent number: 8541409Abstract: There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof.Type: GrantFiled: April 30, 2008Date of Patent: September 24, 2013Assignee: SK Biopharmaceuticals Co., Ltd.Inventors: Byong Sung Kwak, Hong Sik Moon, Han Ju Yi, Young Soon Kang, Dae Joong Im, Eun Hee Chae, Sang Mi Chae, Ki Ho Lee
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Publication number: 20130245019Abstract: Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R?, R?, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.Type: ApplicationFiled: April 30, 2013Publication date: September 19, 2013Applicant: CONGENIA SRLInventors: Daniele Fancelli, Mario Varasi, Simon Plyte, Marco Ballarini, Anna Cappa, Giacomo Carenzi, Saverio Minucci, Gilles Pain, Manuela Villa
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Publication number: 20130245034Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: May 6, 2013Publication date: September 19, 2013Applicant: Janssen Pharmaceutica, N.V.Inventors: Kristof VAN EMELEN, Marc Gustaaf Celine VERDONCK, Sven Franciscus Anna VAN BRANDT, Patrick Rene ANGIBAUD, Lieven MEERPOEL, Alexey Borisovich DYATKIN
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Patent number: 8530479Abstract: The present invention is concerned with deuterium-enriched isobutyl and cyclohexylmethyl sulfonamides of formula I and II, and pharmaceutically acceptable salts and methods of use thereof for the treatment of general anxiety disorders, major depressive disorders, attention deficit disorders, attention deficit hyperactivity disorder, Alzheimer's disease, frontotemporal dementia, cognitive impairment associated with age-related dementia, schizophrenia, migraine, sleep disorders, neurodegenerative diseases and obesity.Type: GrantFiled: August 9, 2010Date of Patent: September 10, 2013Inventor: Daljit Singh Dhanoa
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Patent number: 8530670Abstract: Novel heterocyclic derivatives of formula (I): or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein Ra, n, R1 and R2 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).Type: GrantFiled: March 16, 2012Date of Patent: September 10, 2013Assignee: Probiodrug AGInventors: Ulrich Heiser, Daniel Ramsbeck
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Publication number: 20130231350Abstract: The present invention relates to formulations and methods for increasing the bioavailability of 1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one, 1-(3,3-diphenylpropanoyl)piperazine, or a salt thereof. In particular, the formulation can include one or more pharmaceutically acceptable matrix polymers to form a solid dispersion, e.g., a spray dried dispersion or a hot melt extrusion.Type: ApplicationFiled: April 1, 2013Publication date: September 5, 2013Applicant: Zalicus Pharmaceuticals Ltd.Inventors: Mahesh V. Padval, Jeff T. Gautschi, Daniel T. Smithey, Marshall D. Crew, Abizer Harianawala
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Publication number: 20130225565Abstract: Provided herein are 2,5-disubstituted arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: ApplicationFiled: March 18, 2013Publication date: August 29, 2013Applicant: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei LY, Marie Chantal Siu-Ying TRAN, Erik Dean RAAUM
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Publication number: 20130225561Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I 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 21, 2011Publication date: August 29, 2013Inventors: Haifeng Tang, Alexander Pasternak, Lihu Yang, Shawn P. Walsh, Barbara Pio, Aurash Shahripour, Nardos Teumelsan
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APPLICATION OF 5-HT6 RECEPTOR ANTAGONISTS FOR THE ALLEVIATION OF COGNITIVE DEFICITS OF DOWN SYNDROME
Publication number: 20130210829Abstract: Methods for treating Down syndrome and improving cognitive function of a patient with an intellectual disability are disclosed. 5-hydroxytryptamine sub-receptor six (5-HT6) receptor antagonists are provided for improving the cognition of a Down syndrome patient.Type: ApplicationFiled: March 15, 2013Publication date: August 15, 2013Inventor: THE UNIVERSITY OF UTAH RESEARCH FOUNDATION -
Publication number: 20130209483Abstract: The disclosure relates to cannabinoid derivative compounds, pharmaceutical compositions made thereof, and methods for treating various diseases and disorders including cancer.Type: ApplicationFiled: November 30, 2012Publication date: August 15, 2013Applicant: SUTTER WEST BAY HOSPITALSInventor: SUTTER WEST BAY HOSPITALS
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Patent number: 8501763Abstract: The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions.Type: GrantFiled: March 10, 2008Date of Patent: August 6, 2013Assignee: The Scripps Research InstituteInventors: Congxin Liang, Marcel Koenig, Yuanjun He, Par Holmberg
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Patent number: 8501745Abstract: The invention includes a compound of formula I: wherein R1, X, Z, n, and m have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function in animals.Type: GrantFiled: September 1, 2010Date of Patent: August 6, 2013Assignee: Dart Neuroscience (Cayman) Ltd.Inventors: Terence P. Keenan, Alan P. Kaplan
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Publication number: 20130190288Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, A, X1, X2, X3, X4, R1, R2, R3a, R3b, R4a and R4b are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: ApplicationFiled: December 18, 2012Publication date: July 25, 2013Applicant: GENENTECH, INC.Inventor: Genentech, Inc.
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Publication number: 20130184291Abstract: The invention provides new therapeutic uses of 1-[2-(2,4-dimethyl-phenylsulfanyl)phenyl]-piperazine and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: August 22, 2011Publication date: July 18, 2013Applicant: H. LUNDBECK A/SInventors: Marianne Dragheim, Ioana Florea
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Publication number: 20130171158Abstract: A method of treating or preventing an abnormality of glucose metabolism in a subject, the method comprising administering an antagonist of Inhibitor of Differentiation 1 (Id1) to the subject.Type: ApplicationFiled: June 29, 2011Publication date: July 4, 2013Applicant: GARVAN INSTITUTE OF MEDICAL RESEARCHInventors: Mia Akerfeldt, Ross Laybutt
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Publication number: 20130172315Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.Type: ApplicationFiled: November 30, 2012Publication date: July 4, 2013Applicant: ChemoCentryx, Inc.Inventor: ChemoCentryx, Inc.
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Patent number: 8476279Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.Type: GrantFiled: February 6, 2012Date of Patent: July 2, 2013Assignee: H. Lundbeck A/SInventor: Benny Bang-Andersen
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Publication number: 20130158035Abstract: Screening methods for identifying compounds and compounds and pharmaceutical compositions for treating and preventing cancer are disclosed. The compounds affect signal transduction downstream of the MET receptor.Type: ApplicationFiled: August 23, 2011Publication date: June 20, 2013Applicant: Brigham Young UniversityInventor: Marc Hansen
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Patent number: 8455498Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: September 16, 2009Date of Patent: June 4, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Kristof Van Emelen, Marc Gustaaf Celine Verdonck, Sven Franciscus Anna Van Brandt, Patrick René Angibaud, Lieven Meerpoel, Alexey Borisovich Dyatkin
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Publication number: 20130137679Abstract: The present invention relates to novel functionally selective ligands of dopamine D2 receptors, FIG. 1 including agonists, antagonists, and inverse agonists. The invention further relates to the use of these compounds for treating central nervous system disorders related to D2 receptors.Type: ApplicationFiled: July 1, 2011Publication date: May 30, 2013Inventors: Jian Jin, Bryan Roth, Stephen Frye
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Patent number: 8450324Abstract: Crystalline base of compound trans-1-((1R,3S)-6-chloro-3-phenylindan-1-yl)-3,3-dimethylpiperazine, processes for the preparation of purified free base or salts of this compound, pharmaceutical compositions comprising the base and medical use thereof, including for treatment of schizophrenia and other psychotic disorders.Type: GrantFiled: December 1, 2009Date of Patent: May 28, 2013Assignee: H. Lunbeck A/SInventors: Benny Bang-Andersen, Heidi Lopez de Diego
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Patent number: 8450306Abstract: Novel compounds which are useful for treating acute pain, visceral pain, neuropathic pain, inflammatory/pain receptor-mediated pain, tumor pain and headache diseases.Type: GrantFiled: August 12, 2008Date of Patent: May 28, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
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Publication number: 20130121923Abstract: A composition comprising a selective oxytocin antagonist for use in the treatment and/or prevention of a male ejaculatory disorder; which selective oxytocin antagonist is optionally admixed with a pharmaceutically acceptable carrier, diluent or excipient.Type: ApplicationFiled: January 16, 2013Publication date: May 16, 2013Applicant: PFIZER INC.Inventor: PFIZER INC.