Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Piperazine Ring Patents (Class 514/255.01)
  • NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE
    Publication number: 20120004213
    Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
    Type: Application
    Filed: September 15, 2011
    Publication date: January 5, 2012
    Applicant: FOREST LABORATORIES HOLDINGS LIMITED
    Inventors: Kumar SUNDARESAN, Sandeep N. RAIKAR, Srinivasa Raju SAMMETA, Ganesh PRABHU, Hosahalli SUBRAMANYA, Alexander BISCHOFF
  • Cyclohexyl-1, 4-diamine compounds
    Patent number: 8088763
    Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I, processes for the production thereof, pharmaceutical compositions containing these compounds, methods of producing pharmaceutical compositions including these compounds and related methods of treating or inhibiting certain diseases or conditions.
    Type: Grant
    Filed: November 9, 2006
    Date of Patent: January 3, 2012
    Assignee: Gruenenthal GmbH
    Inventors: Corinna Sundermann, Bernd Sundermann
  • METHOD OF TREATMENT OR PROPHYLAXIS
    Publication number: 20110318329
    Abstract: The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT2 receptor) antagonists for the treatment, prophylaxis, reversal and/or symptomatic relief of neuropathic pain, including mechanical hyperalgesia, thermal or mechanical allodynia, diabetic pain and entrapment pain, in vertebrate animals and particularly in human subjects. The AT2 receptor antagonists may be provided alone or in combination with other compounds such as those that are useful in the control of neuropathic conditions.
    Type: Application
    Filed: August 3, 2010
    Publication date: December 29, 2011
    Inventors: MAREE THERESE SMITH, BRUCE DOUGLAS WYSE
  • RETINOID DERIVATIVES ENDOWED WITH CYTOTOXIC AND/OR ANTIANGIOGENIC PROPERTIES
    Publication number: 20110312965
    Abstract: The present invention relates to new retinoid derivatives of formula I and to pharmaceutical compositions containing them for the treatment of patients affected by pathologies such as arthritic conditions, tumours, metastatic cancer, diabetic retinopathy, psoriasis, chronic inflammatory diseases or atherosclerosis.
    Type: Application
    Filed: December 21, 2009
    Publication date: December 22, 2011
    Inventors: Walter Cabri, Giuseppe Giannini, Gianfranco Battistuzzi, Domenico Alloatti, Claudio Pisano, Sabrina Dallavalle, Tiziana Brunetti
  • Thio-substituted arylmethanesulfinyl derivatives
    Patent number: 8071604
    Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, X, Y, R1, R2, R3, and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.
    Type: Grant
    Filed: November 8, 2007
    Date of Patent: December 6, 2011
    Assignees: Cephalon France, Cephalon, Inc.
    Inventors: Brigitte Lesur, Philippe Louvet, Rabindranath Tripathy
  • Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
    Patent number: 8071603
    Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where x, y, J, K, W, V, R3, R4, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
    Type: Grant
    Filed: September 20, 2005
    Date of Patent: December 6, 2011
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Rajender Kamboj, Zaihui Zhang, Serguei Sviridov, Vandna Raina, Duanjie Hou, Vishnumurthy Kodumuru, Mehran Seid Bagherzadeh
  • COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS
    Publication number: 20110294814
    Abstract: Disclosed are compounds of Formula (I) and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: February 20, 2009
    Publication date: December 1, 2011
    Inventors: Teresa Kowalczyk-Prezewloka, Lijun Sun
  • NOVEL COMPOUNDS
    Publication number: 20110294775
    Abstract: Novel compounds which are useful for treating acute pain, visceral pain, neuropathic pain, inflammatory/pain receptor-mediated pain, tumour pain and headache diseases.
    Type: Application
    Filed: August 12, 2008
    Publication date: December 1, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
  • HYDROXYPHENYL SULFONAMIDES AS ANTIAPOPTOTIC BCL INHIBITORS
    Publication number: 20110294793
    Abstract: The present invention provides compound of Formula (I): or a stereoisomer, tautomer, salt or solvate thereof, wherein the variables are defined herein. The compounds of formula (I) are inhibitors of Bcl-2 family antiapoptotic proteins, compositions containing the compounds and methods of treating diseases using the compounds.
    Type: Application
    Filed: June 8, 2009
    Publication date: December 1, 2011
    Inventors: kyoung S Kim, Robert M. Borzilleri, Zhen-Wei Cai, Kap-Sun Yeung
  • Piperazines as antimalarial agents
    Patent number: 8067419
    Abstract: The invention relates to novel piperazine derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, especially malaria.
    Type: Grant
    Filed: October 20, 2006
    Date of Patent: November 29, 2011
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Christoph Binkert, Christoph Boss, Olivier Corminboeuf, Corinna Grisostomi, Solange Meyer
  • AZA SPIRO ALKANE DERIVATIVES AS INHIBITORS OF METALLOPROTEASES
    Publication number: 20110288068
    Abstract: The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.
    Type: Application
    Filed: July 18, 2011
    Publication date: November 24, 2011
    Inventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian Metcalf
  • Sphingosine kinase inhibitors
    Patent number: 8063248
    Abstract: The invention relates to substituted adamantane compounds, pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.
    Type: Grant
    Filed: December 23, 2007
    Date of Patent: November 22, 2011
    Assignee: Apogee Biotechnology Corporation
    Inventors: Charles D. Smith, Kevin J. French, Yan Zhuang
  • Pharmaceutical Compositions with Attenuated Release of Phenolic Opioids
    Publication number: 20110281886
    Abstract: Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise a phenolic opioid prodrug that provides enzymatically-controlled release of a phenolic opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the phenolic opioid from the prodrug so as to attenuate enzymatic cleavage of the prodrug.
    Type: Application
    Filed: October 16, 2009
    Publication date: November 17, 2011
    Inventors: Thomas E. Jenkins, Julie D. Seroogy, Jonathan W. Wray
  • N-HYDROXYAMIDE DERIVATIVES AND USE THEREOF
    Publication number: 20110281891
    Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
    Type: Application
    Filed: July 28, 2011
    Publication date: November 17, 2011
    Applicant: MERCK SERONO SA
    Inventors: Dominique SWINNEN, Jerome GONZALEZ
  • Prostaglandin derivatives
    Patent number: 8058467
    Abstract: Prostaglandin nitroderivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.
    Type: Grant
    Filed: February 11, 2011
    Date of Patent: November 15, 2011
    Assignee: Nicox S.A.
    Inventors: Ennio Ongini, Valerio Chiroli, Francesca Benedini, Piero Del Soldato
  • METHODS AND COMPOSITIONS RELATED TO TARGETING MONOACYLGLYCEROL LIPASE
    Publication number: 20110275650
    Abstract: This invention provides compounds that selectively inhibit monoacylglycerol lipase (MAGL). The invention also provides methods of using the MAGL selective inhibitors to stimulate 2-Arachidonoylglycerol (2-AG) mediated endocannabinoid signaling in vivo, and to treat conditions that are associated with or linked to endocannabinoid signaling. The invention additionally provides methods of treating cancer or inhibiting tumor growth by targeting MAGL with MAGL specific inhibitors. The invention further provides methods of screening for MAGL inhibitors with improved biochemical and pharmaceutical properties.
    Type: Application
    Filed: November 10, 2009
    Publication date: November 10, 2011
    Applicant: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Benjamin F. Cravatt, Jonathan Z. Long, Weiwei Li, Daniel K. Nomura
  • TREATMENT OF OXIDATIVE STRESS DISORDERS INCLUDING CONTRAST NEPHROPATHY, RADIATION DAMAGE AND DISRUPTIONS IN THE FUNCTION OF RED CELLS
    Publication number: 20110269776
    Abstract: Methods of treating or suppressing oxidative stress diseases and symptoms related to oxidative stress affecting normal electron flow in the cells or caused by reactive oxygen species with redox-active therapeutics. Use of redox-active therapeutics for the reduction, suppression or treatment of oxidative stress induced by chemical agents such as contrast agents and other nephrotoxic agents, by radiation exposure, and by disruptions in the transport of oxygen to tissues, is disclosed.
    Type: Application
    Filed: October 13, 2009
    Publication date: November 3, 2011
    Applicant: Edison Pharmaceuticals, Inc.
    Inventor: Guy M. Miller
  • ARYLSULPHONYLGLYCINE DERIVATIVES, THE PREPARATION THEREOF AND THEIR USE AS MEDICAMENTS
    Publication number: 20110269761
    Abstract: The invention relates to substituted aryl-sulphonylglycine derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as in the specification and claims, which are suitable for preparing a pharmaceutical composition for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.
    Type: Application
    Filed: April 17, 2009
    Publication date: November 3, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Elke Langkopf, Frank Himmelsbach, Juergen Mack, Alexander Pautsch, Corinna Schoelch, Annette Schuler-Metz, Ruediger Streicher, Holger Wagner
  • 1,1'-Diadamantyl carboxylic acids, medicaments containing such compounds and their use
    Publication number: 20110269736
    Abstract: The present invention relates to compounds defined by formula (I) wherein the group R is defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 ?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases.
    Type: Application
    Filed: July 24, 2009
    Publication date: November 3, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias Eckhardt, Bradford S. Hamilton, Frank Himmelsbach
  • Oxidase inhibitors and their use
    Publication number: 20110263604
    Abstract: The invention relates to phenylcyclopropylamine acetamide derivatives and their use in treating diseases.
    Type: Application
    Filed: April 18, 2011
    Publication date: October 27, 2011
    Applicant: Oryzon Genomics, S.A.
    Inventors: Nathalie Guibourt, Alberto Ortega Munoz, Julio Castro-Palomino Laria
  • Piperazine derivatives as inhibitors of stearoyl-CoA desaturase
    Patent number: 8039463
    Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
    Type: Grant
    Filed: March 20, 2009
    Date of Patent: October 18, 2011
    Assignee: Forest Laboratories Holdings Limited
    Inventors: Kumar Sundaresan, Sandeep N. Raikar, Srinivasa Raju Sammeta, Ganesh Prabhu, Hosahalli Subramanya, Alexander Bischoff
  • Piperazine Derivatives for Binding and Imaging Amyloid Plaques and Their Use
    Publication number: 20110250135
    Abstract: The invention relates to compounds of formula I, their synthesis and their use, in particular for detecting amyloid deposits in a patient.
    Type: Application
    Filed: September 4, 2009
    Publication date: October 13, 2011
    Applicant: Bayer Schering Pharma Aktiengesellschaft
    Inventors: Heribert Schmitt-Willich, Ulrike Röhn, Matthias Friebe, Lutz Lehmann, Ansgar Fitzner, Sabine Krause, Damian Brockschnieder, Thomas Dyrks, Andrea Thiele, Ulf Bömer, Ursula Mönning, Tobias Heinrich
  • Composition for Prevention or Treatment of Heart Failure
    Publication number: 20110245179
    Abstract: Provided are a composition for preventing or treating heart failure and a method for screening an agent for treating heart failure. The present disclosure demonstrates for the first time that administration of PKC? inhibitor provides inotropic effect by increasing myocardial contractility. Thus, the present disclosure will contribute greatly to the prevention or treatment of heart failure. Also, since the present disclosure is based on the change in calcium sensitivity in cardiac myocytes unlike the existing inotropic agents, it can enhance the myocardial contractility without increasing oxygen demand or the risk of arrhythmia.
    Type: Application
    Filed: September 17, 2009
    Publication date: October 6, 2011
    Inventors: Woo Jin Park, Jae Gyun Oh
  • DPP-IV inhibitor including beta-amino group, preparation method thereof and pharmaceutical composition containing the same for preventing and treating diabetes or obesity
    Patent number: 8030315
    Abstract: The present invention provides a novel heterocyclic compound containing a beta-amino group, a method for preparing the same, and a pharmaceutical composition comprising the same heterocyclic compound or a pharmaceutically acceptable salt thereof as an active ingredient. The heterocyclic compound of the present invention exhibits excellent DPP-IV inhibitory activity and bioavailability and therefore can be useful for the prophylaxis or treatment of DPP-IV-related diseases such as diabetes or obesity.
    Type: Grant
    Filed: April 18, 2008
    Date of Patent: October 4, 2011
    Assignee: Dong-A Pharm. Co., Ltd.
    Inventors: Heung Jae Kim, Woo Young Kwak, Chang Yell Shin, Hadong Kim, Jong Pil Min, Kyung Jin Park, Jae Young Lee, Song-Hyen Choi, Tae Hyun Yoon, Hae-Sun Kim, Ji Myun Jang, Mi-Kyung Kim, Moon-Ho Son, Soon Hoe Kim, Moohi Yoo
  • Phenylpentadienoyl derivatives and their use as PAR 1 antagonists
    Patent number: 8022064
    Abstract: The present invention relates to compounds of general formula (I): wherein: R1 and R2, identical or different, represent: an atom of hydrogen or halogen, CN or NO2, with R1 and R2 not representing hydrogen simultaneously, m represents: 1 or 2 n represents: 0, 1 or 2 R3 represents: phenyl substituted or not by one or more residues chosen among halogen, hydroxyl or C1-C6 alkyl; C2-C6 alkyl substituted or not by one or more residues chosen among halogen or hydroxyl; cycloalkyl; pyridine; thiophene; pyrrole substituted or not by C1-C6 alkyl; thiazole or furan; or the therapeutically-acceptable salts or solvates thereof.
    Type: Grant
    Filed: June 19, 2007
    Date of Patent: September 20, 2011
    Assignee: Pierre Fabre Medicament
    Inventors: Michel Perez, Marie Lamothe, Bruno Le Grand, Robert Letienne
  • Cyclohexyl sulfonamide derivatives
    Patent number: 8017773
    Abstract: The present invention relates to compounds of formula I wherein R1 to R3 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
    Type: Grant
    Filed: January 18, 2010
    Date of Patent: September 13, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Matthias Nettekoven, Olivier Roche
  • METHODS OF TREATING AMYLOID DISEASE USING ANALOGS OF 1-(4-NITROPHENYL) PIPERAZINE
    Publication number: 20110218200
    Abstract: The present invention is directed to compounds that inhibit amyloid aggregation and methods of treatment there-with.
    Type: Application
    Filed: August 28, 2009
    Publication date: September 8, 2011
    Inventors: Christopher J. Barden, Michael D. Carter, Mark A. Reed, Donald F. Weaver, Arun Yadav, Shengguo Sun
  • Modulators of HCV replication
    Patent number: 8012982
    Abstract: The present invention is directed to compounds of formula (I): where X, Y, R1, R2 and R3 are defined therein, which can act as modulators of viral replication and/or virus production, especially of the hepatitis C virus (HCV).
    Type: Grant
    Filed: September 29, 2005
    Date of Patent: September 6, 2011
    Assignee: Istituto di Ricerche Biologia Molecolare P. Angeletti SpA
    Inventors: Immacolata Conte, Caterina Ercolani, Claudio Giuliano, Giovanni Migliaccio, Gessica Filocamo, legal representative, Veronica Suriano, legal representative, Ian Stansfield
  • DIKETO FUSED AZOLOPIPERIDINES AND AZOLOPIPERAZINES AS ANTI-HIV AGENTS
    Publication number: 20110212971
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, diketo fused azolopiperidine and azolopiperazine derivatives that possess unique antiviral activity are provided. These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: May 5, 2011
    Publication date: September 1, 2011
    Inventors: Tao Wang, Yasutsugu Ueda, Lawrence G. Hamann, Zhongxing Zhang, Zhiwei Yin, Alicia Regueiro-Ren, David J. Carini, Jacob Swidorski, Zheng Liu, Nicolas A. Meanwell, John F. Kadow, Barry L. Johnson
  • UREA DERIVATIVES AS ANTIBACTERIAL AGENTS
    Publication number: 20110212080
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC.
    Type: Application
    Filed: July 28, 2009
    Publication date: September 1, 2011
    Inventors: Umar Faruk Mansoor, Panduranga Adulla Reddy, M. Arshad Siddiqui
  • METHOD FOR IDENTIFYING COMPOUNDS USEFUL FOR TREATING AND/OR PREVENTING DISEASE-ASSOCIATED BONE LOSS
    Publication number: 20110212974
    Abstract: The present invention concerns a method for identifying a compound which inhibits the activation of RAC GTPase by DOCK5 protein comprising the steps of (i) coexpressing the DOCK5 and the RAC proteins in a cell, wherein said DOCK5 protein induces the conversion of inactive RAC, which inactive RAC is bound to GDP, to active RAC, which active RAC is bound to GTP, (ii) contacting or not said cell with said compound, (iii) determining the conversion of inactive RAC to active RAC in the presence or absence of said compound, and (iv) selecting the compound inhibiting the conversion of inactive RAC to active RAC. Said compound is useful for treating disease-associated bone loss.
    Type: Application
    Filed: August 18, 2009
    Publication date: September 1, 2011
    Inventor: Anne Blangy
  • N-hydroxyamide derivatives and use thereof
    Patent number: 8008302
    Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof, in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
    Type: Grant
    Filed: July 25, 2005
    Date of Patent: August 30, 2011
    Assignee: Merck Serono SA
    Inventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
  • ION CHANNEL MODULATING COMPOUNDS AND USES THEREOF
    Publication number: 20110207730
    Abstract: Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of analgesia and local anesthesia.
    Type: Application
    Filed: December 16, 2010
    Publication date: August 25, 2011
    Applicant: Cardiome Pharma Corp.
    Inventors: Allen I. Bain, Gregory N. Beatch, Cindy J. Longley, Bertrand M.C. Plouvier, Tao Sheng, Michael J.A. Walker, Richard A. Wall, Sandro L. Yong, Jeff Jiqun Zhu, Alexander B. Zolotoy
  • Activation of the Renin-Angiotensin System (RAS) and Sudden Cardiac Death
    Publication number: 20110207741
    Abstract: Provided herein are methods of treating a medical condition in which RAS activation is increased. The method comprises the step of administering to a subject a c-Src inhibitor in an amount effective to treat the medical condition. The invention also provides a method of treating or preventing a cardiac arrhythmia. The method comprises the step of administering to the subject a c-Src inhibitor in an amount effective to treat or prevent the cardiac arrhythmia. The invention additionally provides a method of delaying the onset of sudden cardiac death. The method comprises the step of administering to the subject a c-Src inhibitor in an amount effective to delay the onset of SCD. Methods of augmenting gap junction function and methods of increasing Connexin 43 levels in a subject in need thereof are further provided.
    Type: Application
    Filed: February 22, 2011
    Publication date: August 25, 2011
    Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventor: Samuel Dudley
  • Integrin antagonists useful as anticancer agents
    Patent number: 8003806
    Abstract: The invention relates to compounds of the Formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein A, X2, X4, X5 and X1 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of Formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of Formula 1.
    Type: Grant
    Filed: November 9, 2005
    Date of Patent: August 23, 2011
    Assignee: OSI Pharmaceuticals, LLC
    Inventors: Jason Bloxham, Gary V. Borzillo, Eric William Collington, Shazia Sadiq, Colin Peter Sambrook Smith, Chris L. Waller, Graham M. Wynne
  • Crystalline Form Of A Cyclopropyl Benzamide Derivative
    Publication number: 20110201623
    Abstract: The present invention relates to a crystalline form of compound (I), 4-{(1S,2S)-2-[(4-cyclobutylpiperazin-1-yl)carbonyl]-cyclopropyl}-benzamide, pharmaceutical formulations containing said compound and to the use of said active compound in therapy.
    Type: Application
    Filed: February 17, 2011
    Publication date: August 18, 2011
    Inventor: Michael A. UCZYNSKI
  • Pharmaceutical Composition for Prevention and Treatment of Diabetes or Obesity Comprising a Compound that Inhibits Activity of Dipeptidyl Peptidase-IV, and other Antidiabetic or Antiobesity Agents as Active Ingredients
    Publication number: 20110201624
    Abstract: The present invention relates to a pharmaceutical composition for the prevention and treatment of diabetes or obesity comprising as active ingredients a compound which inhibits the activity of dipeptidyl peptidase-IV (DPP-IV), a pharmaceutically acceptable salt thereof, a hydrate thereof, or a solvate thereof, and one or more other antidiabetic or antiobesity agents. The pharmaceutical composition exhibits excellent glucose tolerance and may be useful in the prevention and treatment of diabetes, obesity, and the like by effectively inhibiting blood glucose levels and reducing fat mass.
    Type: Application
    Filed: October 16, 2009
    Publication date: August 18, 2011
    Applicant: DONG-A PHARMACEUTICAL. CO., LTD
    Inventors: Chang Yell Shin, Song-Hyen Choi, Yu Na Chae, Eun Kyoung Yang, Gook Jun Ahn, Moon-Ho Son, Heung Jae Kim, Woo Young Kwak, Jong Pil Min, Tae Hyun Yoon, Soon Hoe Kim, Moohi Yoo
  • Solid Forms Comprising A Cyclopropyl Amide Derivative
    Publication number: 20110201622
    Abstract: This disclosure relates to at least one solid form of 4-{(1S, 2S)-2-[((R)-4-cyclobutyl-2-methylpiperazin-1-yl)carbonyl]-cyclopropyl}-benzamide. This disclosure also relates to at least one pharmaceutical composition comprising at least one solid form described herein, methods of using the solid forms and pharmaceutical compositions comprised thereof, and processes of manufacturing the solid forms.
    Type: Application
    Filed: February 17, 2011
    Publication date: August 18, 2011
    Inventor: Craig D. COLLINS
  • N-hydroxyamide derivatives and use thereof
    Patent number: 7998964
    Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
    Type: Grant
    Filed: November 16, 2006
    Date of Patent: August 16, 2011
    Assignee: Merck Serono S.A.
    Inventors: Dominique Swinnen, Jerome Gonzalez
  • ACRYLAMIDO DERIVATIVES USEFUL AS INHIBITORS OF THE MITOCHONDRIAL PERMEABILITY TRANSITION
    Publication number: 20110195977
    Abstract: Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R?, R?, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.
    Type: Application
    Filed: September 23, 2009
    Publication date: August 11, 2011
    Inventors: Daniele Fancelli, Varasi Mario, Simon Plyte, Marco Ballarini, Anna Cappa, Giacomo Carenzi, Saverio Minucci, Gilles Pain, Manuela Villa
  • NOVEL CARBAMOYLOXY ARYLALKANOYL ARYLPIPERAZINE COMPOUND, PHARMACEUTICAL COMPOSITIONS COMPRISING THE COMPOUND AND METHOD FOR TREATING PAIN, ANXIETY AND DEPRESSION BY ADMINISTERING THE COMPOUND
    Publication number: 20110195963
    Abstract: There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof.
    Type: Application
    Filed: April 30, 2008
    Publication date: August 11, 2011
    Inventors: Byong Sung Kwak, Hong Sik Moon, Han Ju Yi, Young Soon Kang, Dae Joong Im, Eun Hee Chae, Sang Mi Chae, Ki Ho Lee
  • Anti-infective compounds
    Publication number: 20110178077
    Abstract: The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.
    Type: Application
    Filed: June 17, 2009
    Publication date: July 21, 2011
    Inventors: Priscille Brodin, Thierry Christophe, Zaesung No, Jaeseung Kim, Auguste Genovesio, Denis Philippe Cedric Fenistein, Heekyoung Jeon, Fanny Anne Ewann, Sunhee Kang, Saeyeon Lee, Min Jung Seo, Eunjung Park, Monica Contreras Dominguez, Ji Youn Nam, Eun Hye Kim
  • OCTAHYDROPENTALENE COMPOUNDS AS CHEMOKINE RECEPTOR ANTAGONISTS
    Publication number: 20110178096
    Abstract: The present invention is directed to novel compounds of Formula (I) pharmaceutically acceptable salts thereof, pro-drugs thereof, biologically active metabolites thereof, isomers thereof or stereoisomers thereof wherein the variables are as defined herein. The compounds of Formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, rheumatoid arthritis, osteoarthritis, multiple sclerosis and asthma.
    Type: Application
    Filed: March 29, 2011
    Publication date: July 21, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Dawn M. George, Lu X. Wang, Biqin Li, Anna M. Ericsson, Graham K. Ansell
  • Carbamic acid compounds comprising a piperazine linkage as HDAC inhibitors
    Patent number: 7981895
    Abstract: This invention pertains to certain carbamic acid compounds which inhibit HDAC (histone deacetylase) activity of the following formula: The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.
    Type: Grant
    Filed: July 1, 2008
    Date of Patent: July 19, 2011
    Assignee: Topotarget UK Limited
    Inventors: Clare J. Watkins, Maria-Rosario Romero-Martin, James Ritchie, Paul W. Finn, Ivars Kalvinsh, Einars Loza, Klara Dikovska, Igor Starchenkov, Daina Lolya, Vija Gailite
  • NOVEL CATECHOL DERIVATIVE, PHARMACEUTICAL COMPOSITION CONTAINING THE SAME, USE OF THE CATECHOL DERIVATIVE, AND USE OF THE PHARMACEUTICAL COMPOSITION
    Publication number: 20110172208
    Abstract: The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or the like; R4 is cyano, lower alkoxycarbonyl, carboxy or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.
    Type: Application
    Filed: June 26, 2009
    Publication date: July 14, 2011
    Applicant: Kissei Pharmaceutical Co., Ltd.
    Inventors: Takehiro Ishikawa, Satoko Kobayashi, Hitoshi Inoue, Yasunori Ueno, Masako Yoshida, Nobuyuki Tanaka
  • Substituted cyclic hydroxamates as inhibitors of matrix metalloproteinases
    Patent number: 7973041
    Abstract: The present invention provides compounds of the formula: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.
    Type: Grant
    Filed: February 15, 2008
    Date of Patent: July 5, 2011
    Assignee: Incyte Corporation
    Inventors: Yun-Long Li, Jincong Zhuo, David M. Burns, Wenqing Yao, Ravi Kumar Jalluri
  • Derivatives of alkylpiperazine- and alkylhomopiperazine-carboxylates, preparation method thereof and use of same as fatty acid amido hydrolase enzyme inhibitors
    Patent number: 7973042
    Abstract: The present invention comprises alkylpiperazine- and alkylhomopiperazine carboxylates and their derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of disease and other pathological conditions are not generated and the incidence of the disease is greatly reduced.
    Type: Grant
    Filed: December 15, 2008
    Date of Patent: July 5, 2011
    Assignee: Sanofi-Aventis
    Inventors: Ahmed Abouabdellah, Antonio Almario Garcia, Christian Hoornaert, Tak Adrien Li
  • HETEROCYCLIC AMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS
    Publication number: 20110160207
    Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.
    Type: Application
    Filed: March 2, 2011
    Publication date: June 30, 2011
    Inventors: Stephen T. Wrobleski, Jagabandhu Das, T.G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
  • 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 (11BETA-HSD1) INHIBITORS AND USES THEREOF
    Publication number: 20110159005
    Abstract: A method for treating a patient suffering from inflammation, chronic inflammation, pain, rheumatoid arthritis (RA), osteoarthritis and osteoporosis, comprising administering an effective amount of a selective inhibitor of the 11-?-hydroxysteroid dehydrogenase Type 1 enzyme.
    Type: Application
    Filed: December 2, 2010
    Publication date: June 30, 2011
    Applicant: Abbott Laboratories
    Inventors: Peer B. Jacobson, Lisa M. Olson, Sreeinvasarao Vepachedu
  • Thiophene compounds and thrombopoietin receptor activators
    Patent number: 7968542
    Abstract: A compound represented by the formula (I) (wherein R1, R2, R3 and R4 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Grant
    Filed: July 13, 2006
    Date of Patent: June 28, 2011
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Katsuaki Miyaji, Kazufumi Yanagihara, Yukihiro Shigeta, Shunsuke Iwamoto, Masato Horikawa, Yutaka Hirokawa, Shingo Owada, Satoshi Nakano, Hirofumi Ota, Norihisa Ishiwata