Quinoline Or Isoquinoline (including Hydrogenated) Patents (Class 544/363)
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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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Patent number: 8551999Abstract: The present invention provides a heterocyclic compound represented by General Formula (1): wherein R1 is a group R5—Z1—, etc., Z1 is a lower alkylene group, etc., and R5 is a group represented by General Formula; wherein R13 is a hydrogen atom, etc., m is an integer from 1 to 5; R2 is a hydrogen atom: Y is CH or N: A1 is a heterocyclic ring selected from the group consisting of indolediyl groups, wherein the heterocyclic ring may have at least one substituent: T is a group —CO—, etc.: R3 is a hydrogen atom, etc.: R4 is a lower alkyl group optionally substituted by one or more hydroxy groups, etc.: R3 and R4, together with the nitrogen atom to which they bind, may bind to each other and form a 5- to 10-membered saturated heterocyclic ring, wherein the heterocyclic ring may have at least one substituent. The heterocyclic compound of the present invention has excellent effects of suppressing the production of collagen and/or treating tumors.Type: GrantFiled: October 29, 2008Date of Patent: October 8, 2013Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Takumi Sumida, Fujio Tabusa, Kazuo Sekiguchi, Takeshi Kodama, Koichi Yasumura, Yutaka Kojima, Masaaki Motoyama, Keisuke Miyajima, Kenji Yoshida, Keizo Kan, Makoto Sakamoto, Hideki Takasu, Takashi Nakagawa, Naoto Ohi, Yasuo Harada, Norikazu Hashimoto, Hironori Matsuyama, Masatoshi Iida, Shigekazu Fujita, Tae Fukushima
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Publication number: 20130261116Abstract: The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.Type: ApplicationFiled: May 10, 2013Publication date: October 3, 2013Applicants: Rhizen Pharmaceuticals SA, Incozen Therapeutics Pvt. Ltd.Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant VISWANADHA, Govindarajulu BABU, Swaroop Kumar V.S. VAKKALANKA
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Patent number: 8546368Abstract: Compounds of Formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of treatment comprising compounds of Formula (I), and methods of inhibiting the PARP enzyme comprising compounds of Formula (I).Type: GrantFiled: February 15, 2007Date of Patent: October 1, 2013Assignee: AbbVie Inc.Inventors: Thomas D. Penning, Gui-Dong Zhu, Virajkumar B. Gandhi, Jianchun Gong, Vincent L. Giranda
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Patent number: 8541573Abstract: Substituted sulfonamide compounds corresponding to the formula I processes for the preparation thereof, pharmaceutical compositions containing these compounds and the use of substituted sulfonamide compounds for the preparation of pharmaceutical compositions for treating pain and other conditions at least partly mediated via the bradykinin 1 receptor.Type: GrantFiled: March 4, 2009Date of Patent: September 24, 2013Assignee: Gruenenthal GmbHInventors: Stefan Oberboersch, Ruth Jostock, Klaus Schiene, Jean De Vry, Tieno Germann, Sabine Hees, Stefan Schunk, Melanie Reich
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Publication number: 20130244997Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: ApplicationFiled: May 1, 2013Publication date: September 19, 2013Applicant: Janssen Pharmaceutica NVInventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Peter J. Connolly, Christopher M. Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark J. Macielag, Mark E. McDonnell, Philip M. Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
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Publication number: 20130245022Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).Type: ApplicationFiled: May 3, 2013Publication date: September 19, 2013Applicant: Janssen Pharmaceutica NVInventors: J. GUY BREITENBUCHER, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Sierestad
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Publication number: 20130244262Abstract: The present invention provides a cardiomyocyte- and/or cardiac progenitor cell-proliferating agent comprising at least one compound selected from the group consisting of: a GSK3? inhibitor, ERK dephosphorylation inhibitor, Raf activator, CaMK2 inhibitor and p38 inhibitor; and a method for proliferating cardiomyocytes and/or cardiac progenitor cells using the agent.Type: ApplicationFiled: November 17, 2011Publication date: September 19, 2013Applicant: KYOTO UNIVERSITYInventors: Jun Yamashita, Hideki Uosaki
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Publication number: 20130245036Abstract: A crystalline form of (S)-1-(4-Chloro-phenyl)-7-isopropoxy-6-methoxy-2-(4-{methyl-[4-(4-methyl-3-oxo-piperazin-1-yl)-trans-cyclohexylmethyl]-amino}-phenyl)-1,4-dihydro-2H-isoquinolin-3-one, which is useful in the treatment of a disease or disorder associated with the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively.Type: ApplicationFiled: November 17, 2011Publication date: September 19, 2013Applicant: NOVARTIS AGInventors: Joerg Berghausen, Haixia Ren
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Patent number: 8535655Abstract: The invention relates to a biodegradable polymer comprising a plurality of releasable bioactive moieties, the releasable bioactive moieties being pendant from and covalently bonded to the biodegradable polymer backbone, wherein the biodegradable polymer backbone is formed from monomeric units that are each coupled via a biodegradable moiety, and wherein the bioactive moieties are capable of being released at a rate equal to or faster than the rate of biodegradation of the polymer backbone.Type: GrantFiled: April 8, 2011Date of Patent: September 17, 2013Assignee: Polyactiva Pty Ltd.Inventors: Michael Shane O'Shea, Florian Hans Maximilian Graichen, Russell John Tait, Heng Chy Taing, Justine Leigh Jeffery
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Publication number: 20130236395Abstract: Heterocyclic compounds of formula (I) useful as imaging probes of Tau pathology in Alzheimer's disease are described. Compositions and methods of making such compounds are also described.Type: ApplicationFiled: November 7, 2011Publication date: September 12, 2013Applicant: GE HEALTHCARE LIMITEDInventors: Clare Jones, Amanda Ewan, Duncan Wynn, Alessandra Gaeta, James Nairne
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Patent number: 8524894Abstract: The compounds of formula (I) are derived from perhydroquinoline and perhydroisoquinoline and are useful as active pharmaceutical ingredients for the prophylaxis or treatment of diseases caused by 11-beta-hydroxysteroid dehydrogenase type 1 (11-beta-HSD1) enzyme-associated disorders, such as glaucoma, elevated ocular pressure, metabolic disorders, obesity, metabolic syndrome, dyslipidemia, hypertension, diabetes, atherosclerosis, Cushing's syndrome, psoriasis, rheumatoid arthritis, cognitive disorders, Alzheimer's disease or neurodegeneration.Type: GrantFiled: June 4, 2010Date of Patent: September 3, 2013Assignee: Laboratorios Salvat, S.A.Inventors: Juan Lorenzo Catena Ruiz, Carme Serra Comas, Oscar Rey Puiggros, Albert Antolin Hernandez, Esther Monlleo Mas
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Patent number: 8524700Abstract: The disclosure relates to tetrahydroisoquinoline sulfonamide compounds of formula I: wherein R1, R2, n and B are as defined in the disclosure, their preparation and their use in therapies for the treatment of central nervous system diseases such as vigilance and sleep disorders, narcolepsy, Alzheimer's disease and other dementias, Parkinson's disease, attention disorders in hyperkinetic children, memory and learning disorders, epilepsy, schizophrenia, moderate cognitive disorders, depression, anxiety, sexual dysfunction, dizziness and travel sickness.Type: GrantFiled: August 24, 2012Date of Patent: September 3, 2013Assignee: SanofiInventors: Juan Antonio Diaz Martin, Maria Dolores Jimenez Bargueno
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Publication number: 20130225548Abstract: A main object of the present invention is to provide a novel pyridine derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof. In formula [1], R represents an aryl group or a heteroaryl group, which may be substituted by an optionally substituted alkyl group, a hydroxy group, a halogen atom or a group represented by general formula [2]. In formula [2], -L1-L2-L3-RA ??[2] L1 and L3 independently represent a single bond, an alkylene group or a cycloalkylene group; L2 represents a single bond, O, or NRB; RB represents H or an optionally substituted alkyl group; and RA represents B, an amino group, a cyano group, a hydroxy group, an alkoxy group, an aryl group, a monoalkylamino group, a dialkylamino group, a carbamoyl group, an alkyloxycarbonyl group, a monoalkylaminocarbonyl group, a dialkylaminocarbonyl group, an alkylcarbonylamino group, and a saturated heterocyclic group, among other groups.Type: ApplicationFiled: October 27, 2011Publication date: August 29, 2013Applicant: NIPPON SHINYAKU CO., LTD.Inventors: Hidetaka Fujihara, Hiroyuki Sugiyama, Takashi Tsuji, Takara Ino, Yoshinari Haruta
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Publication number: 20130224735Abstract: Chemical compounds having a high selectivity for double stranded DNA over RNA and single stranded DNA are disclosed. The chemical compounds are stains that become fluorescent upon illumination and interaction with double stranded DNA, but exhibit reduced or no fluorescence in the absence of double stranded DNA. The compounds can be used in a variety of biological applications to qualitatively or quantitatively assay DNA, even in the presence of RNA.Type: ApplicationFiled: April 11, 2013Publication date: August 29, 2013Applicant: Life Technologies CorporationInventor: Life Technologies Corporation
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Publication number: 20130225524Abstract: The invention is directed to substituted quinoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, R4, and R5 are defined herein. The compounds of the invention are inhibitors of lactate dehydrogenase A and can be useful in the treatment of cancer and diseases associated with tumor cell metabolism, such as cancer, and more specifically cancers of the breast, colon, prostate and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting lactate dehydrogenase A activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: November 3, 2011Publication date: August 29, 2013Inventors: Deping Chai, Mariela Colon, Christopher Dodson, Kevin J. Duffy, Antony Nicholas Shaw
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Patent number: 8518970Abstract: In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.Type: GrantFiled: January 10, 2012Date of Patent: August 27, 2013Assignees: AbbVie Inc., Genentech, Inc., The Walter and Eliza Hall Institute of Medical ResearchInventors: Jonathan Bayldon Baell, Chinh Thien Bui, Peter Colman, Danette A. Dudley, Wayne J. Fairbrother, John A. Flygare, Guillaume Laurent Lessene, Chudi Ndubaku, George Nikolakopoulos, Carl Steven Rye, Brad Edmund Sleebs, Brian John Smith, Keith Geoffrey Watson, Steven W. Elmore, Andrew M. Petros, Andrew J. Souers, Peter Czabotar
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Publication number: 20130217669Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: ApplicationFiled: March 18, 2013Publication date: August 22, 2013Applicant: Janssen Pharmaceutica, NVInventor: Janssen Pharmaceutica, NV
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Publication number: 20130217671Abstract: The present invention directs a compound represented by formula (I).Type: ApplicationFiled: July 28, 2011Publication date: August 22, 2013Inventors: Yo Matsuo, Shoji Hisada, Yusuke Nakamura, Feryan Ahmed, Raymond Huntley, Joel R. Walker, Helene Decomez
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Publication number: 20130210705Abstract: It is an object of the present invention to provide antimicrobial metallodrugs comprising an antimicrobial peptide (“AMP”) and/or an antibiotic covalently bound to a metal binding moiety. These metallodrugs combine a metal binding domain which typically catalyzes oxido-reductase chemistry or acts as a Lewis-Acid catalyst, with a member of a diverse class of antimicrobial agents currently validated in preclinical and clinical settings for the treatment of a broad spectrum of pathogenic organisms.Type: ApplicationFiled: January 18, 2013Publication date: August 15, 2013Applicant: METALLOPHARM LLCInventor: Metallopharm LLC
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Publication number: 20130203733Abstract: The present invention is based, in part, on assays we conducted that revealed compounds that may be used to treat or prevent diseases characterized by an abnormal or undesirable association of one protein with another.Type: ApplicationFiled: December 20, 2012Publication date: August 8, 2013Applicants: Massachusetts Institute of Technology, The General Hospital CorporationInventors: The General Hospital Corporation, Massachusetts Institute of Technology
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Publication number: 20130203749Abstract: The present invention relates to tetrahydroisoquinoline of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetrahydroisoquinolines, and the use of such tetrahydroisoquinolines for therapeutic purposes. The tetrahydroisoquinolines are GlyT1 inhibitors.Type: ApplicationFiled: March 10, 2013Publication date: August 8, 2013Applicants: ABBVIE INC., ABBVIE DEUTSCHLAND GMBH & CO. KGInventors: Wilhelm Amberg, Michael Ochse, Udo Lange, Wilfried Braje, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles Hutchins
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Publication number: 20130203768Abstract: This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to the preparation of the N-heteroaryl compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.Type: ApplicationFiled: September 28, 2011Publication date: August 8, 2013Inventors: Michael Berger, Christopher Kern, Marko Eck, Jörg Schröder
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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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Patent number: 8501736Abstract: The invention relates to 6-piperidinyl-substituted isoquinoline derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.Type: GrantFiled: December 20, 2007Date of Patent: August 6, 2013Assignee: SanofiInventors: Oliver Plettenburg, Armin Hofmeister, Dieter Kadereit, Stefan Peukert, Sven Ruf, Kurt Ritter, Matthias Loehn, Yuri Ivashchenko, Peter Monecke, Matthias Dreyer, Aimo Kannt
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Publication number: 20130190324Abstract: The present invention provides compositions and methods for increasing the delivery (i.e., bioavailability) of a compound to an ocular cell. Such compositions and methods can be used to treat an ocular clinical condition. Typically, increased bioavailability or delivery of the compound to ocular cells is achieved by utilizing a membrane transporter.Type: ApplicationFiled: December 22, 2012Publication date: July 25, 2013Applicant: The Regents of the University of Colorado, a body corporateInventor: The Regents of the University of Colorado, a body corporate
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Publication number: 20130190489Abstract: The present invention provides compounds of general formulae A, useful as potential anti-tubercular agents against Mycobacterium tuberculosis H37Rv, and drug-resistant Mycobacterium tuberculosis and a process for the preparation thereof. Formula (A).Type: ApplicationFiled: May 6, 2011Publication date: July 25, 2013Inventors: Ahmed Kamal, Azeeza Shaik, Ahmad Ali Shaik, Mohammed Shaheer Malik, Inshad Ali Khan, Sheikh Tasdug Abdullah, Sandeep Sharma, Anshu Beulah Ram
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Publication number: 20130184251Abstract: Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, r, R2 and Z are defined herein.Type: ApplicationFiled: March 4, 2013Publication date: July 18, 2013Applicant: Janssen Pharmaceutica, NVInventor: Janssen Pharmaceutica, NV
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Publication number: 20130184248Abstract: 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, Ar, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: January 11, 2013Publication date: July 18, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF
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Patent number: 8486931Abstract: The present invention relates to compounds of the general formula (I) in which A, B, R1, R2 and Het have the meaning given in claim 1; Y is a bivalent group of the formula in which D is C1-C3-alkylene, where D may have a substituent R5; R3 is hydrogen, C1-C8-alkyl or together with R4 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, and R4 is hydrogen, C1-C8-alkyl or together with R3 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, where R5 together with R5a, where present, are a bond or C1-C3-alkylene; and where one of the following conditions is satisfied: R3 together with R4 is C1-C3-alkylene which may have a radical R5a; or R3 together with R5 is C1-C3-alkylene; or R4 together with R5 is C1-C3-alkylene where the radical A is different from phenyl when the radical B is phenyl or naphthyl; and medicaments which comprise such compounds and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent and/oType: GrantFiled: February 29, 2008Date of Patent: July 16, 2013Assignee: Abbott GmbH & Co. KGInventors: Herve Genesle, Thorsten Oost, Charles W. Hutchins, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch, Astrid Netz, Alfred Hahn
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Publication number: 20130178457Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I).Type: ApplicationFiled: July 5, 2012Publication date: July 11, 2013Applicant: LUPIN LIMITEDInventors: Sanjeev Anant KULKARNI, Sachin MADAN, Nirmal Kumar JANA, Prashant Vitthalrao TALE, Narasimha Murthy CHEEMALA, Sachin Jaysing MAHANGARE, Prashant Popatrao VIDHATE, Chaitanya Prabhakar KULKARNI, Sapana Suresh PATEL, Amolsing Dattu PATIL, Seema Prabhakar ZADE, Rohan Mahadev SHINDE, Venkata P. PALLE, Rajender Kumar KAMBOJ
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Publication number: 20130178458Abstract: In one aspect, the invention relates to substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs, derivatives thereof, and related compounds, which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: December 3, 2012Publication date: July 11, 2013Applicant: Vanderbilt UniversityInventor: Vanderbilt University
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Patent number: 8481546Abstract: The disclosure generally relates to the compound of formula I, (R)—N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)piperazin-1-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide, including pharmaceutically acceptable salts, which is a CGRP-receptor antagonist. The disclosure also relates to pharmaceutical compositions and methods for using the compound in the treatment of CGRP related disorders including migraine headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, chronic obstructive pulmonary disease (COPD), and cancer.Type: GrantFiled: March 2, 2011Date of Patent: July 9, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Prasad V. Chaturvedula, Gene M. Dubowchik, John E. Macor
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Patent number: 8481532Abstract: Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.Type: GrantFiled: July 9, 2009Date of Patent: July 9, 2013Assignee: EnVivo Pharmaceuticals, Inc.Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Publication number: 20130172330Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts, solvates, tautomers, stereoisomers, and/or esters thereof.Type: ApplicationFiled: November 15, 2012Publication date: July 4, 2013Applicant: ALTIRIS THERAPEUTICS, INC.Inventor: Altiris Therapeutics, Inc
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Publication number: 20130172363Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.Type: ApplicationFiled: February 22, 2013Publication date: July 4, 2013Applicant: GALDERMA RESEARCH & DEVELOPMENTInventor: Galderma Research & Development
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Patent number: 8476276Abstract: Disclosed are pharmaceutical compositions containing, as active ingredients, a mixture of a corticosteroid and a kinin B2 receptor antagonist. Said compositions have proved particularly effective, especially in the treatment of inflammatory disorders such as asthma, ophthalmic or dermatological disorders and, above all, as regards the joints, arthritis.Type: GrantFiled: July 3, 2009Date of Patent: July 2, 2013Assignee: Istituto Luso Farmaco d'Italia S.p.A.Inventors: Sandro Giuliani, Carlo Alberto Maggi
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Publication number: 20130165442Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: November 30, 2012Publication date: June 27, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130158042Abstract: 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. R1, R2, R3, R4, Q have meanings given in the description.Type: ApplicationFiled: December 10, 2012Publication date: June 20, 2013Inventors: Annekatrin HEIMANN, Georg DAHMANN, Marc GRUNDL, Stephan Georg MUELLER, Bernd WELLENZOHN
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Publication number: 20130158044Abstract: The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: ApplicationFiled: November 28, 2012Publication date: June 20, 2013Applicant: Otsuka Pharmaceutical Co., Ltd.Inventor: Otsuka Pharmaceutical Co., Ltd.
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Publication number: 20130158015Abstract: Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.Type: ApplicationFiled: February 15, 2013Publication date: June 20, 2013Applicant: AERIE PHARMACEUTICALS, INC.Inventor: Aerie Pharmaceuticals, Inc.
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Publication number: 20130144056Abstract: The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role.Type: ApplicationFiled: July 3, 2012Publication date: June 6, 2013Applicant: SYMPHONY EVOLUTION, INC.Inventors: Lynne Canne Bannen, Erick W. Co, Vasu Jammalamadaka, John M. Nuss, Moon Hwan Kim, Donna Tra Le, Amy Lew Tsuhako, Morrison B. Mac, Shumeye Mamo, Zhaoyang Wen, Wei Xu, Richard George Khoury
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Patent number: 8455476Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: GrantFiled: April 22, 2010Date of Patent: June 4, 2013Assignee: Janssen Pharmaceutica, NVInventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
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Publication number: 20130137674Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: ApplicationFiled: January 25, 2013Publication date: May 30, 2013Applicant: Janssen Pharmaceutica, NVInventor: Janssen Pharmaceutica, NV
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Publication number: 20130137688Abstract: 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, Ar, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: November 26, 2012Publication date: May 30, 2013Inventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF
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Patent number: 8450317Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R5, A, B, D and X are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: April 27, 2010Date of Patent: May 28, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Jennifer A. Kowalski, Daniel Richard Marshall, Anthony S. Prokopowicz, III, Sabine Schlyer, Robert Sibley, Ronald John Sorcek, Di Wu, Frank Wu, Erick Richard Roush Young
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Patent number: 8445495Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: June 11, 2009Date of Patent: May 21, 2013Assignee: Cytokinetics, Inc.Inventors: Bradley P. Morgan, David J. Morgans, Jr., Alex Muci, Pu-Ping Lu, Erica A. Kraynack, Todd Tochimoto
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Patent number: 8445496Abstract: This invention is directed to a crystalline 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile monohydrate having an x-ray diffraction pattern wherein 2? angles (°) of significant peaks are at about: 9.19, 11.48, 14.32, 19.16, 19.45, 20.46, 21.29, 22.33, 23.96, 24.95, 25.29, 25.84, 26.55, 27.61, and 29.51, and a transition temperature of about 109° C. to about 115° C.Type: GrantFiled: June 22, 2010Date of Patent: May 21, 2013Assignee: Wyeth LLCInventors: Marc Sadler Tesconi, Gregg Feigelson, Henry Strong, Hong Wen
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Patent number: 8445477Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: GrantFiled: April 22, 2010Date of Patent: May 21, 2013Assignee: Janssen Pharmaceutica, NVInventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
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Publication number: 20130123258Abstract: Provided are 4(1H)-quinolone derivatives effective in inhibiting or eliminating the viability of at least one of the stages in the life-cycle of the malarial parasite, and to show a reduced propensity to induce resistance to the compound by the target parasite. In particular, the compounds can be derivatives of phenoxyethoxy-quinolones, and including, but not only, 7-(2-phenoxyethoxy)quinolin derivatives. These compounds may be administered by themselves, with at least one other derivative compound, or with other antimalarial compounds, to an animal or human subject. The therapeutic compositions can be and formulated to reduce the extent of a Plasmodium infection in the recipient subject, or to reduce the likelihood of the onset or establishment of a Plasmodium infection if administered prior to the parasite contacting the subject. The therapeutic compositions can be formulated to provide an effective single dose amount of an antimalarial compound or multiple doses for administering over a period of time.Type: ApplicationFiled: October 26, 2012Publication date: May 16, 2013Inventors: Roman Manetsch, Richard Matthew Cross, Niranjan Kumar Namelikonda, Dennis Edward Kyle, Tina Susanna Mutka, Alexis Nichole LaCrue, Jordany Richarlson Maignan, Fabian Ernesto Saenz