Bicyclo Ring System Which Is Indole (including Hydrogenated) Patents (Class 546/201)
  • NOVEL INDOLES ARE CANNABINOID RECEPTOR LIGANDS
    Publication number: 20110065685
    Abstract: The present invention provides novel compounds of Formula (I) which are CB2 selective ligands useful for the treatment of pain.
    Type: Application
    Filed: June 14, 2010
    Publication date: March 17, 2011
    Applicant: Abbott Laboratories
    Inventors: Jennifer M. Frost, Karin Tietje, Michael J. Dart, Michael D. Meyer
  • DERIVATIVES OF 4-AMINOPIPERIDINE AND THEIR USE AS A MEDICAMENT
    Publication number: 20110059971
    Abstract: A subject of the present application is new derivatives of 4-aminopiperidines of formula in which R1, R2 and R3 represent various radical, and their preparation processes by synthetic methods in parallel in liquid and solid phase. These products having a good affinity with certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) somatostatin receptors are involved.
    Type: Application
    Filed: November 15, 2010
    Publication date: March 10, 2011
    Applicant: IPSEN S.A.S.
    Inventors: Christophe THURIEAU, Jérôme Gonzalez, Christophe Moinet
  • NOVEL 3-AMINOALKYL-1,3-DIHYDRO-2H-INDOL-2-ONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
    Publication number: 20110059955
    Abstract: The present invention relates to novel 3-aminoalkyl-1,3-dihydro-2H-indol-2-one derivatives, to their preparation and to their therapeutic application. The compounds of the present invention correspond to the formula (I): in which the variables are as set forth in the specification. These compounds exhibit a strong affinity and a high selectivity for human arginine-vasopressin (AVP) V1a receptors and some compounds additionally exhibit a strong affinity for AVP V1b receptors.
    Type: Application
    Filed: August 18, 2010
    Publication date: March 10, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Loic FOULON, Laurent GOULLIEUX, Brigitte POUZET, Claudine SERRADEIL-LE GAL, Gerard VALETTE
  • INDOLE DERIVATIVES AS HISTAMINE 3 RECEPTOR INHIBITORS FOR THE TREATMENT OF COGNITIVE AND SLEEP DISORDERS, OBESITY AND OTHER CNS DISORDERS
    Publication number: 20110059966
    Abstract: This invention relates to compounds having pharmacological activity, to compositions containing these compounds, and to a method of treatment employing the compounds and compositions. More particularly, this invention concerns certain indole derivatives and their salts and solvates. These compounds have H3 histamine receptor antagonist activity. This invention also relates to pharmaceutical compositions containing these compounds and to a method of treating disorders in which histamine H3 receptor blockade is beneficial.
    Type: Application
    Filed: November 10, 2010
    Publication date: March 10, 2011
    Inventors: Youssef L. Bennani, Michael G. Campbell, David Dastrup, Emilie Porter Huck
  • Hydroxamate-Based Inhibitors of Deacetylases
    Publication number: 20110053925
    Abstract: The present teachings relate to compounds of Formula I: and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R1, R2, R3, ring A, and are as defined herein. The present teachings also provide methods of preparing compounds of Formula I and methods of using compounds of Formula I in treating, inhibiting, or preventing pathologic conditions or disorders mediated wholly or in part by deacetylases.
    Type: Application
    Filed: August 27, 2010
    Publication date: March 3, 2011
    Inventors: Young Shin CHO, Lei JIANG, Michael SHULTZ, Christine Hiu-Tung CHEN, Gang LIU, Jianke LI
  • ANTI-CYTOKINE HETEROCYCLIC COMPOUNDS
    Publication number: 20110053955
    Abstract: Heterocyclic compounds which are inhibitors of Mitrogen-Activated Protein Kinase-Activated Protein Kinase-2 (MAPKAP-K2) as described, in addition to their use in the treatment of cytokine mediated diseases.
    Type: Application
    Filed: February 7, 2008
    Publication date: March 3, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Asitha Abeywardane, Denise Andersen, Tina Marie Morwick, Roger John Snow, Yancey David Ward
  • Cannabinoid receptor modulators
    Patent number: 7897601
    Abstract: A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, is useful in treating diseases, disorders, or conditions such as obesity, metabolic disorders, addiction, diseases of the central nervous system, cardiovascular disorders, respiratory disorders, and gastrointestinal disorders.
    Type: Grant
    Filed: January 16, 2007
    Date of Patent: March 1, 2011
    Assignees: Intervet, Inc., Intervet International B.V.
    Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Martin C. Clasby, Keith A. Eagen, Jack D. Scott, Yuguang Wang, Yan Xia, William J. Greenlee
  • Indolinone compounds as kinase inhibitors
    Patent number: 7897602
    Abstract: Indolinone compounds of formula (I) or (II): wherein A, R1, R2, R3, R4, R5, R6, R7, and n are defined herein. Also disclosed are methods for decreasing the activity of a protein kinase and for treating a protein kinase-related disease, such as cancer, with these compounds.
    Type: Grant
    Filed: June 26, 2009
    Date of Patent: March 1, 2011
    Assignee: Development Center for Biotechnology
    Inventors: Jiann-Jyh Huang, Chao-Cheng Chiang, Chiawei Liu, Chun-Liang Lai, Shu Fu Lin, Yu-Hsiang Lin, Ru-Wen Wang, Sheng-Chuan Yang, Jia-Ming Chang, Shih-Hsien Chuang, Paonien Chen
  • 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
  • PROTEIN KINASE AND PHOSPHATASE INHIBITORS
    Publication number: 20110028474
    Abstract: The present invention provides a method for identifying inhibitors of protein kinases and/or protein phosphatases. Methods are also provided for inhibiting protein kinase and/or protein phosphatase activity. Specific non-peptide protein tyrosine kinase and/or protein phosphatase inhibitors are provided. The protein kinase or protein phosphatase inhibitors of the present invention may be used to treat a number of conditions in patients, including cancer, psoriasis, arthrosclerosis, immune system activity, Type II diabetes, and obesity.
    Type: Application
    Filed: August 10, 2010
    Publication date: February 3, 2011
    Applicant: THE RESEARCH FOUNDATION OF STATE UNIVERSITY OF NEW YORK
    Inventors: David G. Hangauer, JR., Moustafa E. El-Araby, Karen L. Milkiewicz
  • LXR receptor modulators
    Patent number: 7872021
    Abstract: Benzenesulfonamide derivative compounds corresponding to the general formula (I): and their pharmaceutically acceptable addition salts; a process for preparation of such compounds; pharmaceutical compositions containing such compounds, and the use of such compounds as a pharmacologically active substance, in particular in the treatment of neurodegenerative diseases, cardiovascular diseases, inflammatory diseases; hypercholesterolemia, and diabetes.
    Type: Grant
    Filed: November 7, 2006
    Date of Patent: January 18, 2011
    Assignee: Laboratories Fournier S.A.
    Inventors: Luc Lebreton, Christine Massardier, Christine Dumas, Pierre Dodey, Philippe Masson
  • FUSED RING COMPOUNDS AS PARTIAL AGONISTS OF PPAR-GAMMA
    Publication number: 20110009384
    Abstract: The present invention provides an agent for the prophylaxis or treatment of diabetes, which has a superior hypoglycemic action, and is associated with a fewer side effects such as body weight gain and the like. The resent invention relates an agent for the prophylaxis or treatment of diabetes, which comprises a compound represented by wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof.
    Type: Application
    Filed: February 5, 2008
    Publication date: January 13, 2011
    Inventors: Taisuke Tawaraishi, Hiroshi Imoto, Nobuo Cho
  • Substituted isoindolones and their use as metabotropic glutamate receptor potentiators
    Patent number: 7868008
    Abstract: The present invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.
    Type: Grant
    Filed: February 15, 2006
    Date of Patent: January 11, 2011
    Assignee: AstraZeneca AB
    Inventors: Bradford Van Wagenen, Radhakrishnan Ukkiramapandian, Joshua Clayton, Ian Egle, James Empfield, Methvin Isaac, Fupeng Ma, Abdelmalik Slassi, Gary Steelman, Rebecca Urbanek, Sally Walsh
  • CYCLOALKANE DERIVATIVE
    Publication number: 20110003994
    Abstract: The present invention relates to a novel cycloalkane derivative which exhibits an excellent psychotropic action and has less side effect.
    Type: Application
    Filed: June 30, 2010
    Publication date: January 6, 2011
    Inventor: Megumi MARUYAMA
  • Crystal Forms of (3R)-1-(2-Methylalanyl-D-Tryptophyl)-3-(Phenylmethyl)-3-Piperidinecarboxylic Acid 1,2,2-Trimethylhydrazide
    Publication number: 20110003996
    Abstract: Crystalline polymorphs of (3R)-1-(2-methylalanyl-D-tryptophyl)-3-(phenylmethyl)-3-piperidinecarboxylic acid 1,2,2-trimethylhydrazide which are useful as pharmaceutical agents are disclosed. Methods of production and isolation of these polymorphs and pharmaceutical compositions which include these polymorphs and pharmaceutical methods of treatment are also disclosed. The crystalline polymorphs of the present invention are useful as they act directly on the pituitary gland cells to release growth hormone.
    Type: Application
    Filed: July 6, 2010
    Publication date: January 6, 2011
    Applicant: Helsinn Therapeutics (U.S.), Inc.
    Inventors: Keith Lorimer, Seemon H. Pines, Bernhard Paul, Benjamin Littler
  • Processes for the preparation of substituted 2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolines
    Patent number: 7863451
    Abstract: The present invention concerns new processes for the preparation of substituted 2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolines which are useful for preventing or treating diseases or conditions related to an abnormally high level or activity of TNF?. The invention provides processes for the commercial production of substituted 2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolines including, but not limited to, the therapeutically active 3-(4-amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione.
    Type: Grant
    Filed: September 1, 2005
    Date of Patent: January 4, 2011
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Roger Chen, Manohar Tukaram Saindane, Chuansheng Ge
  • Chemical compounds
    Patent number: 7858796
    Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: where R1, R2, R3, U and V are defined below and to pharmaceutically acceptable salts thereof. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). 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 IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Grant
    Filed: September 21, 2005
    Date of Patent: December 28, 2010
    Assignee: Glaxo Group Limited
    Inventors: Jeffrey K. Kerns, Michael Lindenmuth, Xichen Lin, Hong Nie, Sonia M. Thomas
  • NOVEL SUBSTITUTED PIPERIDYL-PROPANE-THIOLS
    Publication number: 20100317669
    Abstract: One object of the present invention are novel substituted piperidyl-propane-thiols of the formula (1), wherein R1, R2, R3 and D are defined as below. Another object of the present invention is to provide agonists or antagonists of CCR-3, or pharmaceutically acceptable salts thereof, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 25, 2007
    Publication date: December 16, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Domnic Martyres, Matthias Hoffmann, Peter Seither, Thierry Bouyssou
  • PIPERIDYL-PROPANE-THIOL CCR3 MODULATORS
    Publication number: 20100317634
    Abstract: One object of the present invention are novel substituted piperidyl-propane-thiols of the formula (1), wherein R1, R2, R3 and R4 are defined as below. Another object of the present invention is to provide agonists or antagonists of CCR-3, or pharmaceutically acceptable salts thereof, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 25, 2007
    Publication date: December 16, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Domnic Martyres, Matthias Hoffmann, Peter Seither, Thierry Bouyssou
  • META-SUBSTITUTED PHENYL SULFONYL AMIDES OF SECONDARY AMINO ACID AMIDES, THE PRODUCTION THEREOF, AND USE THEREOF AS MATRIPTASE INHIBITORS
    Publication number: 20100305090
    Abstract: The invention relates to meta-substituted phenyl sulfonyl amides of secondary amino acid amides according to the general formula (I), (II), or (III), the production thereof, and the use thereof as matriptase inhibitors, in particular the use thereof as drugs for inhibiting tumor growth and/or metastasization.
    Type: Application
    Filed: March 5, 2008
    Publication date: December 2, 2010
    Inventors: Torsten Steinmetzer, Andrea Schweinitz, Daniel Donnecke
  • Anti-migraine spirocycles
    Patent number: 7842808
    Abstract: The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.
    Type: Grant
    Filed: January 5, 2007
    Date of Patent: November 30, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Prasad V. Chaturvedula, Ling Chen, Rita Civiello, Andrew P. Degnan, Gene M. Dubowchik, Xiaojun Han, Xiang Jun J. Jiang, Guanglin Luo, John E. Macor, Graham S. Poindexter, George O. Tora
  • Compounds having ?adrenergic receptor agonist and muscarinic receptor antagonist activity
    Patent number: 7842704
    Abstract: The invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7a, R7b, W, G1, G2, a, b, c, d and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: December 11, 2007
    Date of Patent: November 30, 2010
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Sarah Dunham
  • METHODS FOR TREATING HEPATITIS C
    Publication number: 20100292187
    Abstract: The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.
    Type: Application
    Filed: June 14, 2010
    Publication date: November 18, 2010
    Applicant: PTC THERAPEUTICS, INC.
    Inventors: Gary M. Karp, Peter Seongwoo Hwang, James J. Takasugi, Hongyu Ren, Richard Gerald Wilde, Anthony A. Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey A. Campbell, Chunshi Li, Steven Paget, Nanjing Zhang, Xiaoyan Zhang, Jin Zhu
  • Oxazolyl Piperidine Modulators of Fatty Acid Amide Hydrolase
    Publication number: 20100292266
    Abstract: Certain oxazolyl piperidine 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. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).
    Type: Application
    Filed: May 25, 2007
    Publication date: November 18, 2010
    Inventors: Richard Apodaca, James Guy Breitenbucher, Alison L. Chambers, Mark Seierstad, Wei Xiao
  • Methods for treating cancer using 3-[1,3dioxo-4-benzamidoisoindolin-2-yl]-2,6-dioxo-5-hydroxypiperidine
    Patent number: 7834033
    Abstract: Isoindolin-1-one and Isoindoline-1,3-dione substituted in the 2-position with a 2,6-dioxo-3-hydroxypiperidin-5-yl group, which may be further substituted in the 5-position with alkyl or halogeno, and in the 4-position with alkyl or a nitrogen-containing group are inhibitors of, and thus useful in the treatment of disease states mediated by, TNF?. A typical embodiment is 2-(2,6-dioxo-3-hydroxy-5-fluoro-piperidin-5-yl)4-aminoisoindolin-1-one.
    Type: Grant
    Filed: November 4, 2005
    Date of Patent: November 16, 2010
    Assignee: Celgene Corporation
    Inventors: George Muller, Hon-Wah Man, David I. Stirling
  • Piperidine derivatives
    Patent number: 7834032
    Abstract: Compounds of the formula (I), in which R1, R2, Q, X, Y, m and n have the meanings indicated in Claim (1), are potent 5-HT2A antagonists and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders, such as bulimia, anorexia nervosa, of premenstrual syndrome and/or for positively influencing obsessive-compulsive disorder (OCD).
    Type: Grant
    Filed: February 14, 2005
    Date of Patent: November 16, 2010
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Timo Heinrich, Henning Boettcher, Joachim Leibrock
  • Cyclic amine derivative having heteroaryl ring
    Patent number: 7829580
    Abstract: A compound having the general formula (I) wherein R1 represents C1-C6 alkyl, etc., R2 represents hydrogen, C2-C7 alkanoyl, C7-C11 arylcarbonyl, the formula R4—(CH2)l—, etc., R3 represents C6-C10 aryl, etc., X1, X2, X3, X4 and X5 each independently represents hydrogen, halogen, etc., and n represents an integer of 0 to 2, pharmacologically acceptable salts thereof or prodrugs thereof. They have excellent inhibition of platelet activation, etc. and are useful as a prophylactic or therapeutic agents for diseases related to thrombus or embolus formation.
    Type: Grant
    Filed: May 26, 2006
    Date of Patent: November 9, 2010
    Assignee: Sankyo Company, Ltd.
    Inventors: Tomio Kimura, Naoki Tanaka, Atsuhiro Sugidachi, Toshiyuki Konosu
  • Oxindole derivative as feeding control agent
    Patent number: 7825155
    Abstract: Disclosed is a compound represented by the formula (1) below, a prodrug thereof or a pharmaceutically acceptable salt of either, which is useful as a therapeutic, preventive or ameliorating agent for diabetes and the like. (In the formula, R3 represents an optionally substituted carbamoyl group or the like; X represents a hydroxyl group or the like; W1 and W2 independently represent a single bond or methylene; R7 and R8 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; and Ar represents an optionally substituted aryl group or the like.
    Type: Grant
    Filed: September 13, 2006
    Date of Patent: November 2, 2010
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Teruhisa Tokunaga, Tsuyoshi Takasaki, Kozo Yoshida, Ryu Nagata
  • Crystal forms of (3R)-1-(2-methylalanyl-D-tryptophyl)-3-(phenylmethyl)-3-piperidinecarboxylic acid 1,2,2-trimethylhydrazide
    Patent number: 7825138
    Abstract: Crystalline polymorphs of (3R)-1-(2-methylalanyl-D-tryptophyl)-3-(phenylmethyl)-3-piperidinecarboxylic acid 1,2,2-trimethylhydrazide which are useful as pharmaceutical agents are disclosed. Methods of production and isolation of these polymorphs and pharmaceutical compositions which include these polymorphs and pharmaceutical methods of treatment are also disclosed. The crystalline polymorphs of the present invention are useful as they act directly on the pituitary gland cells to release growth hormone.
    Type: Grant
    Filed: June 22, 2005
    Date of Patent: November 2, 2010
    Assignee: Helsinn Therapeutics (U.S.), Inc.
    Inventors: Keith Lorimer, Seemon H. Pines, Bernhard Paul, Benjamin Littler
  • SUBSTITUTED OXINDOL DERIVATIVES, MEDICAMENTS CONTAINING SAID DERIVATIVES AND USE THEREOF
    Publication number: 20100273766
    Abstract: The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.
    Type: Application
    Filed: December 1, 2006
    Publication date: October 28, 2010
    Applicant: Abbott GmbH & Co. KG
    Inventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Herve Geneste, Astrid Netz
  • Apoptosis inhibitors
    Patent number: 7816352
    Abstract: The present invention provides compounds that act as selective agents to protect against unintentional cell death or tissue damage and can relieve side effects of cancer treatment such as, for example, oral mucositis, hair loss, diarrhea due to damage to the gastrointestinal epithelium, and myelosuppression. In addition, these compounds can be used to prevent premature cell death when the cell death is caused by signals from damaged cells, for example, signals generated as the result of a traumatic incident or an ischemic episode.
    Type: Grant
    Filed: March 10, 2006
    Date of Patent: October 19, 2010
    Assignee: The Regents of The University of California
    Inventors: Dennis A. Carson, Howard B. Cottam, Sylvie Barchéchath, Mary Patricia Corr
  • Cyclic amides
    Patent number: 7816376
    Abstract: The invention relates to compounds of the formula (I) and pharmaceutically usable derivatives, salts, solvates and stereoisomers and mixtures thereof, in which X, Y, Z, R1, R3, R4, R8, p, k, E, G, Z and Q are as defined in claim 1, which are employed as excitatory amino acid antagonists for combating neurodegenerative diseases, including cerebrovascular diseases, epilepsy, schizophrenia, Alzheimer's, Parkinson's or Huntington's disease, cerebral ischaemia, infarction or psychoses.
    Type: Grant
    Filed: March 5, 2003
    Date of Patent: October 19, 2010
    Assignee: Merck Patent GmbH
    Inventors: Oliver Schadt, Joachim Leibrock, Helmut Pruecher, Christoph Seyfried
  • Kinase inhibitor compounds
    Publication number: 20100261665
    Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.
    Type: Application
    Filed: January 28, 2010
    Publication date: October 14, 2010
    Applicant: Xcovery, Inc.
    Inventors: Congxin Liang, Ming Qi, Shu Gao, Zhigang Li
  • Method of synthesis of 4-amino-thalidomide enantiomers
    Patent number: 7812169
    Abstract: The invention provides new and useful analogs of 4-amino-thalidomide. These analogs include S(?)-4-amino-thalidomide and R(+)-4-amino-thalidomide. The invention also provides processes for making these analogs. Further, the invention provides methods for inhibiting angiogenesis and treating angiogenesis-associated diseases, including cancer and macular degeneration, by administering these compounds.
    Type: Grant
    Filed: November 30, 2001
    Date of Patent: October 12, 2010
    Assignee: The Children's Medical Center Corporation
    Inventors: Anthony Treston, Jamshed H. Shah, Robert J. D'Amato, Kimberly A. Hunsucker, John Rougas, Barry P. Conner, Victor Pribdula, Glenn M. Swartz
  • PIPERIDINE DERIVATIVE
    Publication number: 20100256189
    Abstract: As a result of studies on compounds having a selective inhibitory activity against 17?HSD type 5, the present inventors have confirmed that a {1-[(indol-2-yl)carbonyl]piperidyl}alkanol derivative has a potent selective inhibitory activity against 17?HSD type 5. The invention has been completed based on these findings. The compound of the present invention can be used as an agent for treating and/or an agent for preventing diseases associated with 17?HSD type 5, such as benign prostatic hyperplasia and prostate cancer, without accompanying adverse effects due to a decrease in testosterone.
    Type: Application
    Filed: August 28, 2008
    Publication date: October 7, 2010
    Inventor: Akio KAKEFUDA
  • 4-Phenylpiperidine Derivatives as Renin Inhibitors
    Publication number: 20100240679
    Abstract: Compounds of the present invention having the formula exhibit inhibitory activity on the natural enzyme renin. Thus, compounds of formula (I) may be employed for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.
    Type: Application
    Filed: May 28, 2010
    Publication date: September 23, 2010
    Inventors: Richard Sedrani, Juergen Klaus Maibaum, Werner Breitenstein, Holger Sellner, Claus Ehrhardt, Nils Ostermann
  • DERIVATIVES OF N-PHENYL(PIPERIDINE-2-YL) METHYL BENZAMIDE PREPARATION METHOD THEREOF AND APPLICATIONS OF SAME IN THERAPEUTICS
    Publication number: 20100234424
    Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.
    Type: Application
    Filed: May 20, 2010
    Publication date: September 16, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Gihad DARGAZANLI, Genevieve ESTENNE-BOUHTOU, Pascale MAGAT
  • Indole derivatives as antiviral agents
    Patent number: 7795250
    Abstract: The present invention relates to indole compounds of the formula (I): wherein R1, R2, R3, R4, A, E and X are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.
    Type: Grant
    Filed: June 8, 2005
    Date of Patent: September 14, 2010
    Assignee: Istituto di Ricerche di Biologia Molecolare P Angeletti SpA
    Inventors: Stefania Colarusso, Immacolata Conte, Joerg Habermann, Frank Narjes, Simona Ponzi
  • Ether derivatives
    Patent number: 7795437
    Abstract: The present invention relates to ether derivatives according to general formula I, and to their pharmaceutically-acceptable salts, which may be used in treating or preventing cognitive disorders, drug addiction, depression, anxiety, drug dependence, dementias, memory impairment, psychotic disorders comprising schizophrenia, schizoaffective disorders, bipolar disease, mania, psychotic depression, or psychoses comprising paranoia and delusions.
    Type: Grant
    Filed: October 22, 2007
    Date of Patent: September 14, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luca Claudio Gobbi, Georg Jaeschke, Olivier Roche, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
  • Monocyclic and bicyclic compounds and methods of use
    Patent number: 7790726
    Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
    Type: Grant
    Filed: August 14, 2006
    Date of Patent: September 7, 2010
    Assignee: Chemocentryx, Inc.
    Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Lianfa Li, Edward J. Sullivan, Wei Chen, Kevin Lloyd Greenman
  • Azinyl-3-sulfonylindazole derivatives as 5-hydroxytryptamine-6 ligands
    Patent number: 7790751
    Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
    Type: Grant
    Filed: August 14, 2006
    Date of Patent: September 7, 2010
    Assignee: Wyeth LLC
    Inventors: Hassan Mahmoud Elokdah, Alexander Alexei Greenfield, Kevin Liu, Geraldine Ruth McFarlane, Cristina Grosanu, Jennifer Rebecca Lo, Albert Jean Robichaud
  • Derivatives of N-[phenyl(alkylpiperidine-2-yl)methyl]benzamide, preparation method thereof and application of same in therapeutics
    Patent number: 7790753
    Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.
    Type: Grant
    Filed: April 17, 2006
    Date of Patent: September 7, 2010
    Assignee: sanofi-aventis
    Inventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Corinne Veronique
  • Indol-3-yl-carbonyl-azaspiro derivatives
    Patent number: 7790752
    Abstract: This invention relates to indol-3-yl-carbonyl-azaspiro derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the azaspiro-head group A and the residues R1, R2 and R3 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, their use for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders, and methods of preparation thereof.
    Type: Grant
    Filed: September 21, 2006
    Date of Patent: September 7, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
  • Bicyclic Derivatives as P38 Inhibitors
    Publication number: 20100222363
    Abstract: New bicyclic derivatives of formula (I); wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors.
    Type: Application
    Filed: June 28, 2006
    Publication date: September 2, 2010
    Applicant: PALAU PHARMA, S.A.
    Inventors: Carmen Almansa Rosales, Marina Virgili Bernadó
  • Non-Nucleoside Reverse Transcriptase Inhibitors
    Publication number: 20100222322
    Abstract: Indole compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula (I) and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: June 23, 2006
    Publication date: September 2, 2010
    Applicant: MERCK & CO., INC.
    Inventors: Scott E. Wolkenberg, Zhijian Zhao, Craig W. Lindsley
  • INDOL-3-Y-CARBONYL-PIPERIDIN AND PIPERAZIN-DERIVATIVES
    Publication number: 20100222357
    Abstract: The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.
    Type: Application
    Filed: May 13, 2010
    Publication date: September 2, 2010
    Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
  • NOVEL NITROREDUCTASE ENZYMATIC SUBSTRATES
    Publication number: 20100221764
    Abstract: The present invention relates to an enzyme substrate for detecting nitroreductase activity of formula (I) below: in which X is S, NX1, O or NX1-CO; R1 is nothing or a substituent selected from Cl, CH3, Br, F, I, alkyl, aryl and carboxyl; R2 is nothing or a substituent selected from Cl, O—CH2—O, O—CH3, F, diethylenediamine-CH3, NR3R4, Br, I, alkyl, aryl, carboxyl, NO2 and R3 and R4 are independently H or an alkyl group containing from 1 to 4 carbon atoms; and X1 is selected from H, CH3, C2H4Ph, OH, alkyl and aryl.
    Type: Application
    Filed: May 29, 2008
    Publication date: September 2, 2010
    Applicant: BIOMERIEUX
    Inventors: Olivier Fabrega, Arthur James, Vindhya Lakshika Salwatura, Sylvain Orenga, Stephen Stanforth
  • Substituted Indole Compounds
    Publication number: 20100222324
    Abstract: Substituted indole compounds corresponding to the formula I: In which R8, R9a, R9b, R10, R11, R200, R210, A, D, T, q, s and t have defined meanings, processes for the preparation thereof, pharmaceutical compositions containing such compounds and the use of substituted indole compounds for the treatment or inhibition of pain and other conditions which are at least partly mediated by Bradykinin 1 receptors (B1R).
    Type: Application
    Filed: February 3, 2010
    Publication date: September 2, 2010
    Applicant: Gruenenthal GmbH
    Inventors: Stefan Schunk, Melanie Reich, Michael Engels, Tieno Germann, Ruth Jostock, Sabine Hees
  • Indol-3-y-carbonyl-piperidin and piperazin-derivatives
    Patent number: 7781436
    Abstract: The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.
    Type: Grant
    Filed: July 25, 2006
    Date of Patent: August 24, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
  • Cyclic derivatives as modulators of chemokine receptors activity
    Patent number: 7776884
    Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis, asthma, restinosis, organ transplantation, and cancer.
    Type: Grant
    Filed: February 10, 2006
    Date of Patent: August 17, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventor: Robert J. Cherney