Isoquinolines (including Hydrogenated) Patents (Class 514/307)
Plural isoquinoline ring systems attached directly or indirectly to each other by nonionic bonding (Class 514/308)
Chalcogen attached directly to the six-membered hetero ring by nonionic bonding (Class 514/309)
Nitrogen, other than as nitro or nitroso, attached directly to the isoquinoline ring system by nonionic bonding (Class 514/310)
  • THERAPEUTIC COMPOUNDS
    Publication number: 20110059939
    Abstract: Compounds comprising formula (I) or a pharmaceutically acceptable salt thereof, a dashed line represent the presence or absence of a double bond, are disclosed, wherein J1, J2, U1, B, Y, and A are as described in claims 1-12. Methods, compositions, and medicaments related thereto are also disclosed, for treating glaucoma, inflammatory bowel disease and baldness.
    Type: Application
    Filed: May 4, 2009
    Publication date: March 10, 2011
    Applicant: ALLERGAN ,INC
    Inventors: David W. Old, Vinh X. Ngo
  • ANILINE DERIVATIVE HAVING ANTI-RNA VIRAL ACTIVITY
    Publication number: 20110059950
    Abstract: Viruses, and particularly RNA viruses, have high mutation rates. Hence, antiviral agents that have been developed to date targeting protease or reverse transcriptase of viruses have quickly lost their effectiveness and resistant viruses have emerged. Also, in recent years, viral diseases caused by various new viruses such as SARS, avian influenza, and the hepatitis C have become social menaces. Therefore, the development of a novel antiviral agent that can cope with a virus resistant to an existing drug or a new virus and has a wide range of applications has been demanded. The present invention provides a novel anti-RNA viral agent and a method for use thereof. The present invention further provides an anti-RNA viral agent that is also effective against a new virus or a drug-resistant virus, and a method for use thereof.
    Type: Application
    Filed: February 4, 2009
    Publication date: March 10, 2011
    Applicant: KinoPharma, Inc.
    Inventors: Hiroshi Onogi, Masatoshi Hagiwara, Masaaki Suzuki, Hiroko Koyama, Takamitsu Hosoya, Toshiyuki Hiramatsu
  • Piperidine/Cyclohexane Carboxamide Derivatives For Use as Vanilloid Receptor Modulators
    Publication number: 20110059979
    Abstract: Certain compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, P, P?, X, m and n are as defined in the specification, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds in medicine.
    Type: Application
    Filed: August 12, 2004
    Publication date: March 10, 2011
    Applicant: GLAXO GROUP LIMITED
    Inventors: Craig Jamieson, David Drysdale Miller, Harshad Kantilal Rami, Mervyn Thompson
  • S1P Receptor Modulating Compounds and Use Thereof
    Publication number: 20110059945
    Abstract: The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.
    Type: Application
    Filed: November 12, 2010
    Publication date: March 10, 2011
    Applicant: EPIX PHARMACEUTICALS, INC.
    Inventors: Ashis K. Saha, Nili Schutz, Xiang Yu, Dilara McCauley, Mercedes Lobera, Yael Marantz, Jian Lin, Srinivasa Cheruku, Pini Orbach, Anurag Sharadendu, Robert Christian Penland, Kimberley Gannon, Sharon Shacham, Silvia Noiman, Oren Becker
  • BICYCLIC DERIVATIVES AS MODULATORS OF ION CHANNELS
    Publication number: 20110059965
    Abstract: Bicyclic derivatives having formula (I) and a composition thereof are useful as ion channel antagonists:
    Type: Application
    Filed: July 6, 2010
    Publication date: March 10, 2011
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Aarti Sameer Kawatkar, Tara Whitney, Timothy D. Neubert, Nicole Hilgraf, Andreas P. Termin, Esther Martinborough
  • NANOSCALE BOUND BILAYERS, METHODS OF USE AND PRODUCTION
    Publication number: 20110059159
    Abstract: Methods for rapidly obtaining a nanoscale apolipoprotein bound phospholipid bilayer (NABB) associated with at least one membrane protein are provided. Also disclosed are methods for rapidly obtaining a NABB not associated with membrane proteins. Immunogenic compositions comprising NABBs with native conformational epitopes are also provided along with their methods of use.
    Type: Application
    Filed: January 30, 2009
    Publication date: March 10, 2011
    Applicant: THE ROCKEFELLER UNIVERSITY
    Inventors: Thomas P. Sakmar, Thomas Huber, Sourabh Banerjee
  • COMPOUNDS FOR THE TREATMENT OF PROLIFERATIVE DISORDERS
    Publication number: 20110059893
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
    Type: Application
    Filed: September 16, 2010
    Publication date: March 10, 2011
    Inventors: Lijun Sun, Christopher Borella, Hao Li, Jun Jiang, Shoujun Chen, Keizo Koya, Takayo Inoue, Zhenjian Du, Kevin Foley, Yaming Wu, Mei Zhang, Weiwen Ying
  • Substituted tetrahydroisoquinolines as ?-secretase inhibitors
    Patent number: 7902218
    Abstract: There is provided a series of tetrahydroisoquinoline diaminopropane compounds of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R8 and R9 are as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
    Type: Grant
    Filed: December 6, 2007
    Date of Patent: March 8, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lorin A. Thompson, III, Kenneth M. Boy, Jianliang Shi, John E. Macor, Andrew C. Good, Lawrence R. Marcin
  • 3,4-SUBSTITUTED PIPERIDINE DERIVATIVES AS RENIN INHIBITORS
    Publication number: 20110053940
    Abstract: The present invention relates to 3,4-substituted piperidinyl-based renin inhibitor compounds bearing at 4-position oxopyridine and having the formula (I). The invention further relates to pharmaceutical compositions containing said compounds, as well as their use in treating cardiovascular events and renal insufficiency.
    Type: Application
    Filed: May 4, 2009
    Publication date: March 3, 2011
    Inventors: Austin Chih-Yu Chen, Daniel Dube, Pierre-Andre Fournier, Erich L. Grimm, Patrick Lacombe, Sebastien Laliberte, Dwight MacDonald, D. Bruce MacKay, Daniel James McKay, Tom Yao-Hsiang Wu, Louis-Charles Campeau, Jeremy Peter Scott, Nadine Bremeyer
  • N-aroyl cyclic amine derivatives as orexin receptor antagonists
    Patent number: 7897618
    Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.
    Type: Grant
    Filed: October 29, 2007
    Date of Patent: March 1, 2011
    Assignee: SmithKline Beecham Limited
    Inventors: Clive Leslie Branch, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Alan Porter, Rachel Elizabeth Anne Stead, Geoffrey Stemp
  • MODULATION OF NEUROGENESIS WITH GABA AGENTS AND GABA ANALOGS
    Publication number: 20110046090
    Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use of a GABA agent or GABA analog, in combination with one or more other neurogenic agents, to stimulate or activate the formation of new nerve cells.
    Type: Application
    Filed: August 20, 2010
    Publication date: February 24, 2011
    Applicant: BrainCells Inc.
    Inventors: Carrolee BARLOW, Todd Carter, Andrew Morse, Kai Treuner, Kym Lorrain, Jammieson Pires
  • Benzazole derivatives, compositions, and methods of use as ?-secretase inhibitors
    Patent number: 7893267
    Abstract: The present invention is directed to benzazole compounds that inhibit ?-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment or prevention of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which BACE is involved.
    Type: Grant
    Filed: March 14, 2006
    Date of Patent: February 22, 2011
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Adnan M. M. Mjalli, David Jones, Devi Reddy Gohimmukkula, Guoxiang Huang, Jeff Zhu, Mohan Rao, Robert C. Andrews, Tan Ren
  • Thiazolyl-dihydro-indazole
    Patent number: 7893049
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R6 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Grant
    Filed: April 5, 2007
    Date of Patent: February 22, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Darryl McConnell, Bodo Betzemeier, Thomas Gerstberger, Maria Impagnatiello, Steffen Steurer, Lars van der Veen, Ulrike Weyer-Czernilofsky
  • PIPERIDINE AND PYROOLIDINE COMPOUNDS
    Publication number: 20110039857
    Abstract: The invention relates to piperidine and pyrrolidine compounds of formula (I) wherein A, B, n and X are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds use as medicaments, especially as orexin receptor antagonists.
    Type: Application
    Filed: April 29, 2009
    Publication date: February 17, 2011
    Inventors: Hamed Aissaoui, Christoph Boss, Ralf Koberstein, Thierry Sifferlen, Daniel Trachsel
  • 5-SUBSTITUTED-2-IMINO-THIAZOLIDINONE COMPOUNDS AND THEIR USE AS INHIBITORS OF BACTERIAL INFECTION
    Publication number: 20110039849
    Abstract: A method for inhibiting Gram-negative bacterial pathogenesis, a method of screening for compounds that inhibit type III secretion in Gram-negative bacteria, and compounds that inhibit type III secretion in Gram-negative bacteria.
    Type: Application
    Filed: August 16, 2010
    Publication date: February 17, 2011
    Applicant: UNIVERSITY OF WASHINGTON
    Inventors: Heather B. Felise, Samuel I. Miller, Toni Kline
  • METHODS FOR INCREASING ENDOTHELIAL PROGENITOR CELLS
    Publication number: 20110039885
    Abstract: The present invention relates to methods and compounds useful for increasing endothelial progenitor cell levels in blood and bone marrow. Methods and compounds for increasing endothelial progenitor cell mobilization are also provided.
    Type: Application
    Filed: December 8, 2008
    Publication date: February 17, 2011
    Applicant: FibroGen, Inc.
    Inventors: Stephen J. Klaus, Ingrid Langsetmo Parobok, Oksana Sirenko
  • ELEVATION OF THE PLASMA HDL-CHOLESTEROL LEVEL
    Publication number: 20110038827
    Abstract: The present invention relates to the use of isosteviol, steviol, and related compounds for elevating the plasma HDL-cholesterol level. The invention furthermore relates to the use of these compounds for reducing the body weight of a subject and/or lowering the plasma triglyceride level of a subject, including a concomitant elevation of the plasma HDL-cholesterol level. Preferably the compounds used are isosteviol and/or steviol, or pharmaceutically acceptable salts, solvates or prodrugs thereof. The compounds may furthermore be administered in combination with one or more further active compounds, such as e.g. LDL-cholesterol lowering agents. The invention furthermore relates to a method for elevating the plasma HDL-cholesterol level in a subject by administering to a subject in need of such treatment a plasma HDL-cholesterol level elevating amount of the compounds, described herein.
    Type: Application
    Filed: December 5, 2008
    Publication date: February 17, 2011
    Inventors: Kjeld Hermansen, Per Bendix Jeppesen
  • ANILIDES AND ANALOGS AS RHO KINASE INHIBITORS
    Publication number: 20110038835
    Abstract: Compounds useful as Rho kinase inhibitors of formula (I): wherein variable are as defined herein are provided. Methods of treatment of malconditions mediated by Rho kinase, and methods of preparation of the compounds, are also provided.
    Type: Application
    Filed: December 18, 2008
    Publication date: February 17, 2011
    Applicant: The Scripps Research Institute
    Inventors: Yangbo Feng, Philip LoGrasso, Thomas Bannister, Thomas Schroeter, Xingang Fang, Yen ting Chen, Yan Yin, Michael P. Smolinski, Lei Yao, Bo Wang, Hampton Sessions
  • Substituted hydroxamic acids and uses thereof
    Publication number: 20110039827
    Abstract: This invention provides compounds of formula (I): wherein R1, R2, G, m, n, p and q have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: June 21, 2010
    Publication date: February 17, 2011
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Jeffrey P. Ciavarri, Kenneth M. Gigstad, He Xu
  • Use of triazolopyrimidine derivatives as microbicides
    Patent number: 7888371
    Abstract: Use of compounds of the formula (I) in which R1, R2, R3 and R4 are as defined in the description for protecting engineered materials.
    Type: Grant
    Filed: May 16, 2002
    Date of Patent: February 15, 2011
    Assignee: LANXESS Deutschland GmbH
    Inventors: Rainer Bruns, Martin Kugler, Thomas Jaetsch, Hans-Ludwig Elbe, Dietmar Kuhnt, Olaf Gebauer, Heiko Rieck
  • SUBSTITUTED PIPERIDINE COMPOUNDS AND METHODS OF THEIR USE
    Publication number: 20110034417
    Abstract: Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.
    Type: Application
    Filed: October 5, 2010
    Publication date: February 10, 2011
    Applicant: Adolor Corporation
    Inventors: Bertrand Le Bourdonnec, Roland E. Dolle
  • Pharmaceutical Combinations Comprising Specified Age Breaker and Further Drugs, I.A. Antihypertensive Drugs, Antidiabetic Drugs Etc.
    Publication number: 20110034378
    Abstract: The present invention relates to a combination, such as a combined preparation or pharmaceutical composition comprising: (a) compound of formula (I), and/or (II) or a pharmaceutically acceptable salt thereof; (b) at least one therapeutic agent selected from the group consisting of: an antihypertensive agent; an antidiabetics agent; a hypolipidemic agent; an antiplatelet agent; an antiobesity agent; an antithrombotic agent; an agent for diabetic vascular complications; and an agent for treatment of heart failure; or a pharmaceutically acceptable salts thereof, optionally in presence of a pharmaceutically acceptable carrier for separate, simultaneous or sequential use. The present invention also relates to a use of such combination for the treatment of mammal including human being. R1, R2, R3, R1, R2, R3, R4, R5, X, Y, A and B and m are as defined in the specification.
    Type: Application
    Filed: January 21, 2009
    Publication date: February 10, 2011
    Inventors: Chaitanya Dutt, Deepa Joshi, Ram Gupta, Kumarprafull Chandra
  • Sulfonamides
    Publication number: 20110028509
    Abstract: The invention relates to compounds of formula I wherein R1, R2, R4, Ra, Rb, Rc, Re, A*, W1, W2 and W3 are as defined in claim 16, for the treatment of CXCR3 related diseases.
    Type: Application
    Filed: April 8, 2009
    Publication date: February 3, 2011
    Applicant: MERCK SERONO SA
    Inventors: Stefano Crosignani, Christophe Cleva, Christos Tsaklakidis, Lars Burgdorf
  • Niacin Receptor Agonists, compositions Containing Such Compounds and Methods of Treatment
    Publication number: 20110028462
    Abstract: A method of treating atherosclerosis and related conditions using compounds of formula I: as well as pharmaceutically acceptable salts and solvates is disclosed. The compounds are useful for treating dyslipidemias, and in particular, reducing serum LDL, VLDL and triglycerides, and raising HDL levels.
    Type: Application
    Filed: September 15, 2006
    Publication date: February 3, 2011
    Inventors: Steven L. Colletti, Jason E. Imbriglio, Richard Thomas Beresis, Jessica Leslie Frie
  • TETRAHYDROISOQUINOLINE SULFONAMIDE DERIVATIVES, THE PREPARATION THEREOF, AND THE USE OF THE SAME IN THERAPEUTICS
    Publication number: 20110028475
    Abstract: 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: Application
    Filed: October 8, 2010
    Publication date: February 3, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Juan Antonio DIAZ MARTIN, Maria Dolores JIMENEZ BARGUENO
  • Diaminothiazoles useful as Axl inhibitors
    Patent number: 7879856
    Abstract: Diaminothiazoles and pharmaceutical compositions containing them are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the diaminothiazoles in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: February 1, 2011
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland
  • NOVEL HYDROXAMATES AS THERAPEUTIC AGENTS
    Publication number: 20110021528
    Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
    Type: Application
    Filed: October 1, 2010
    Publication date: January 27, 2011
    Applicant: PHARMACYCLICS, INC.
    Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
  • INDAZOLECARBOXAMIDE DERIVATIVES FOR THE TREATMENT AND PREVENTION OF MALARIA
    Publication number: 20110021467
    Abstract: The invention relates to methods of treating or preventing malaria which comprises administering to a patient in need thereof, an effective amount of a 1H-indazole-3-carboxamide derivative of general formula (I), in the form of a base or of an addition salt with an acid, or in the form of a hydrate or of a solvate of said base or acid addition salt.
    Type: Application
    Filed: October 1, 2010
    Publication date: January 27, 2011
    Applicant: Sanofi-Aventis
    Inventors: Hugues D'ORCHYMONT, Laurent Fraisse, André Zimmermann
  • SUBSTITUTED PYRAZOLE SIGMA RECEPTOR ANTAGONISTS
    Publication number: 20110015183
    Abstract: The invention relates to compounds having pharmacological activity towards the sigma receptor, and more particularly to pyrazole derivatives of formula I and to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use therapy and prophylaxis, in particular for the treatment of psychosis or pain.
    Type: Application
    Filed: September 29, 2010
    Publication date: January 20, 2011
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Jordi CORBERA ARJONA, Maria Rosa CUBERES-ALTISENT, Joerg HOLENZ, Daniel MARTÍNEZ-OLMO, David VAÑO-DOMENECH
  • (+)-Morphinans as Antagonists of Toll-Like Receptor 9 and Therapeutic Uses Thereof
    Publication number: 20110015219
    Abstract: The present invention provides (+)-morphinans comprising Toll-like receptor 9 (TLR9) antagonist activity, as well as a method for identifying (+)-morphinans that may be therapeutically effective by determining whether the (+)-morphinan inhibits the activation of TLR9. Also provided are methods of using the (+)-morphinans comprising TLR9 antagonist activity to treat conditions such as traumatic pain, neuropathic pain, inflammatory disorders, acetaminophen toxicity, autoimmune disorders, neurodegenerative disorders, and cancer.
    Type: Application
    Filed: July 16, 2010
    Publication date: January 20, 2011
    Applicant: Mallinckrodt Inc.
    Inventors: Bobby N. Trawick, David W. Berberich
  • OLIGOMER-GUANIDINE CLASS CONJUGATES
    Publication number: 20110009446
    Abstract: The invention relates to (among other things) oligomer-guanidine class conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.
    Type: Application
    Filed: January 9, 2009
    Publication date: January 13, 2011
    Applicant: Nektar Therapeutics
    Inventors: Wen Zhang, Stephanie Allums, Jennifer Riggs-Sauthier
  • Azapeptide Derivatives
    Publication number: 20110009355
    Abstract: This invention relates to novel compounds that are azapeptides, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel azapeptide compounds that are derivatives of the HIV protease inhibitor atazanavir sulfate. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administering HIV protease inhibitors. The invention also relates to the use of one or more of the disclosed compounds as reagents in analytical studies involving atazanavir.
    Type: Application
    Filed: April 6, 2010
    Publication date: January 13, 2011
    Inventors: Scott L. Harbeson, Roger D. Tung
  • Dermatitis treating agent
    Patent number: 7868019
    Abstract: The present invention is to provide a topical dermatitis treating agent which comprises a pyridine compound represented by the following formula [I]: wherein R1 and R2 each represent a lower alkoxy group, ?X— represents a group represented by the formula: or a group represented by the formula: ?N—, Ring A represents a saturated or unsaturated bicyclic nitrogen-containing heterocyclic group having 1 to 4 substituents selected from hydroxyl group, oxo group, a lower alkoxy group, a di-lower alkylaminophenyl group, a pyperidino-lower alkoxy group, a morpholino-lower alkoxy group, a cyclo-lower alkylamino-lower alkylamino group, pyridyl group and morpholino group, and represents a single bond or a double bond, or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: October 5, 2006
    Date of Patent: January 11, 2011
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Atsuko Naotsuka, Matsuo Kikuchi
  • Substituted 4-phenyltetrahydroisoquinolines, pharmaceutical compositions comprising them and therapeutic methods for their use
    Patent number: 7868003
    Abstract: The invention relates to substituted 4-phenyltetrahydroisoquinolines of formula I wherein R1-R8, N, W, X and Z are defined herein. These compounds and pharmaceutical compositions comprising them are useful in the treatment of respiratory disorders, sleep apnea, kidney disorders, high blood pressure, hypertension, disorders of the central nervous system and the like.
    Type: Grant
    Filed: July 11, 2007
    Date of Patent: January 11, 2011
    Assignee: Sanofi-Aventis
    Inventors: Uwe Heinelt, Hans-Jochen Lang, Klaus Wirth, Thomas Licher, Armin Hofmeister
  • Methods for Treatment of HIV or Malaria Using Combinations of Chloroquine and Protease Inhibitors
    Publication number: 20110003764
    Abstract: The present invention relates to a drug combination capable of conferring therapeutic benefits in the treatment of both AIDS and malaria. In particular, it relates to a drug combination including at least one quinolinic antimalarial compound such as chloroquine or hydroxychloroquine, and at least one inhibitor of the Human Immunodeficiency Virus (HIV) protease enzyme. This drug combination is capable of inhibiting the replication of both HIV and Plasmodium sp. It also relates to the direct antimalarial effects of the HIV PIs.
    Type: Application
    Filed: May 26, 2009
    Publication date: January 6, 2011
    Inventor: Andrea Savarino
  • Substituted Aromatic Carboxamide and Urea Derivatives as Vanilloid Receptor Ligands
    Publication number: 20110003795
    Abstract: The invention relates to substituted aromatic carboxamide and urea derivatives, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.
    Type: Application
    Filed: May 6, 2010
    Publication date: January 6, 2011
    Applicant: Gruenenthal GmbH
    Inventors: Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Nils DAMANN, Sven FRORMANN, Bernhard LESCH, Jeewoo LEE, Yong-Soo KIM, Myeong-Seop KIM
  • Heteroaryls and uses thereof
    Publication number: 20110003806
    Abstract: This invention provides compounds of formula IA or IB: wherein R1, R2, G1 and HY are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: January 28, 2010
    Publication date: January 6, 2011
    Applicants: Millennium Pharmaceuticals, Inc., Takeda Pharmaceutical Company Limited
    Inventors: Masaaki Hirose, Steven P. Langston, Hirotake Mizutani, Stepan Vyskocil
  • DERIVATIVES OF 4-(N-AZACYCLOALKYL) ANILIDES AS POTASSIUM CHANNEL MODULATORS
    Publication number: 20110003850
    Abstract: This invention provides a compound of formula IA where X=0 or S; Y is 0 or S; q=1 or 0; and other substituents are defined herein. Such compounds can affect the opening of, or otherwise modulate, voltage-gated potassium channels. Such compounds useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.
    Type: Application
    Filed: February 1, 2010
    Publication date: January 6, 2011
    Applicant: Valeant Pharmaceuticals International, Inc.
    Inventors: Jean-Michel Vernier, Martha Alicia De La Rosa, Huanming Chen, Jim Zhen Wu, Gary Lee Larson, Ian Wayne Cheney
  • HIGHLY SELECTIVE SIGMA RECEPTOR LIGANDS
    Publication number: 20100329978
    Abstract: Compounds having the general formula II, III, or IV wherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.
    Type: Application
    Filed: May 21, 2010
    Publication date: December 30, 2010
    Applicants: University of Mississippi, I'Universite catholique de Louvain
    Inventors: Christopher R. McCurdy, Christophe Mesangeau, Rae Reiko Matsumoto, Jacques Henri Poupaert, Bonnie Ann Avery, Ahmed Hassan Amin Abdelazeem
  • PROLYL HYDROXYLASE INHIBITORS AND METHODS OF USE
    Publication number: 20100331303
    Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.
    Type: Application
    Filed: August 20, 2010
    Publication date: December 30, 2010
    Inventors: Richard Masaru Kawamoto, Shengde Wu, Namal C. Warshakoon, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer
  • Inhibitors of Jun N-Terminal Kinase
    Publication number: 20100331335
    Abstract: The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.
    Type: Application
    Filed: February 5, 2010
    Publication date: December 30, 2010
    Inventors: Hing L. Sham, Roy K. Hom, Andrei W. Konradi, Gary D. Probst, Simeon Bowers, Anh Truong, R. Jeffrey Neitz, Jennifer Sealy, Gergely Toth
  • MODULATORS OF THE HISTAMINE H3 RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
    Publication number: 20100331312
    Abstract: Amide derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the histamine H3 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as excessive daytime sleepiness, narcolepsy, shift-work sleep disorder, drowsiness as a side effect from a medication, maintenance of vigilance to aid in the completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease, pain and the like.
    Type: Application
    Filed: February 18, 2009
    Publication date: December 30, 2010
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: Vincent J. Santora, Brian J. Hofilena, Michelle Pulley, Graeme Semple, Yun Shan, Brian M. Smith
  • Biphenyl compounds useful as muscarinic receptor antagonists
    Patent number: 7858792
    Abstract: This invention provides compounds of formula I: wherein a, b, c, m, p, r, R1, R2, R3, R4, R5, R6, W and X1 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: March 12, 2009
    Date of Patent: December 28, 2010
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu, Viengkham Malathong
  • Antibacterial Agents
    Publication number: 20100324025
    Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
    Type: Application
    Filed: September 21, 2009
    Publication date: December 23, 2010
    Applicant: University of Washington
    Inventors: Niels H. Andersen, Jason Bowman, Alice L. Erwin, Eric A. Harwood, Toni Kline, Khisimuzi E. Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
  • 4-CARBOXYBENZYLAMINO DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
    Publication number: 20100324046
    Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: June 24, 2008
    Publication date: December 23, 2010
    Inventors: Paul Harrington, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Paul Tempest, Kevin J. Wilson, David J. Witter
  • Indazolyl-substituted pyrroline compounds as kinase inhibitors
    Patent number: 7855203
    Abstract: The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: December 21, 2010
    Assignee: Ortho-McNeil-Janssen Pharmaceuticals, Inc.
    Inventors: Han-Cheng Zhang, Bruce Maryanoff, Kimberly White, Hong Ye, Leonard R. Hecker, David F. McComsey
  • NOVEL ANABASEINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF
    Publication number: 20100311773
    Abstract: Disclosed are novel anabaseine derivatives that act as agonists of the ?7 nAChR. Also disclosed are pharmaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds.
    Type: Application
    Filed: December 30, 2009
    Publication date: December 9, 2010
    Applicant: Cornerstone Therapeutic, Inc.
    Inventors: Gregory J. Habgood, Daniel Elbaum
  • 3-Substituted Propanamine Compounds
    Publication number: 20100311789
    Abstract: Racemic or enantiomerically enriched 3-substituted propanamine compounds represented by the following structural formula (I): or a pharmaceutically acceptable salt thereof are disclosed. Pharmaceutical compositions containing the subject compounds are also disclosed. The subject compounds are useful for the treatment of diseases of the central nervous system, such as depression, anxiety and pain disorders.
    Type: Application
    Filed: June 3, 2009
    Publication date: December 9, 2010
    Inventors: Chun-Eung Park, Kyung-Hyun Min, Yong-Je Shin, Yu-Jin Shin, Hae-Jeong Yoon, Won Kim, Eun-Ju Ryu, Coo-Min Chung, Hui-Ho Kim
  • PHARMACEUTICAL FORMULATIONS
    Publication number: 20100310607
    Abstract: The present invention relates to oral formulations comprising an active agent comprising at least one of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid, salts of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid or buffered 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid.
    Type: Application
    Filed: March 19, 2010
    Publication date: December 9, 2010
    Applicant: Abbott Laboratories
    Inventors: Tzuchi R. Ju, Claudia M. Davila, Yi Gao, Linda E. Gustavson, David LeBlond, Tong Zhu
  • METHODS FOR TREATING AND PREVENTING MUCOSITIS
    Publication number: 20100310684
    Abstract: Methods for treating and preventing mucositis, in particular mucositis following the administration of chemotherapy drugs or a combination of said drugs with radiotherapy, are disclosed herein. More specifically, disclosed herein is the administration of a therapeutically effective amount of at least one of an anthocyanoside, a proanthocyanidin, or an extract containing at least one of an anthocyanoside or a proanthocyanidin for the treatment or prevention of mucositis. The therapeutically effective amount of the anthocyanoside, proanthocyanidin or extract can be administered alone or in combination with a therapeutically effective amount of at least one of an anti-inflammatory agent, immunomodulating agent, analgesic, antimicrobial agent or antifungal agent. Also disclosed herein are pharmaceutical compositions for treating and preventing mucositis.
    Type: Application
    Filed: August 16, 2010
    Publication date: December 9, 2010
    Inventors: Ezio Bombardelli, Paolo Morazzoni