Double Bonded Divalent Chalcogen Containing Patents (Class 544/130)
  • N-ACYLOXYSULFONAMIDE AND N-HYDROXY-N-ACYLSULFONAMIDE DERIVATIVES
    Publication number: 20140235636
    Abstract: The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
    Type: Application
    Filed: April 25, 2014
    Publication date: August 21, 2014
    Applicants: Cardioxyl Pharmaceuticals, Inc., The Johns Hopkins University
    Inventors: John P. Toscano, Art Sutton, Vincent Jacob Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
  • CYANOMETHYLPYRAZOLE CARBOXAMIDES AS JANUS KINASE INHIBITORS
    Publication number: 20140228348
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Application
    Filed: September 21, 2012
    Publication date: August 14, 2014
    Inventors: Jason Brubaker, Matthew Lloyd Childers, Matthew Christopher, Joshua T. Close, Jason David Katz, Joon Jung, Scott Peterson, Phieng Siliphaivanh, Tony Siu, Graham Frank Smith, Luis E. Torres, Hyun Chong Woo, Jonathan R. Young, Hongjun Zhang
  • SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS
    Publication number: 20140228351
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Application
    Filed: March 14, 2014
    Publication date: August 14, 2014
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • NO- AND H2S- RELEASING COMPOUNDS
    Publication number: 20140221316
    Abstract: This disclosure relates to novel compounds containing an H2S releasing moiety and a nitric oxide (NO) releasing moiety covalently linked with a core (e.g., a salicylic acid moiety) and the use of such compounds in treating inflammatory diseases, including cancers. Therapeutic potency of these compounds is significantly higher than NSAIDs containing a H2S-releasing moiety alone (HS-NSAIDs) and NSAID containing a NO-releasing moiety alone (NO-NSAIDs). The compounds, in addition, exhibit reduced side effect, e.g., reduced stomach ulcers, upon administration.
    Type: Application
    Filed: August 15, 2012
    Publication date: August 7, 2014
    Applicant: RESEARCH FOUNDATION OF THE CITY UNIVERSITY OF NEW YORK
    Inventors: Khosrow Kashfi, Ravinder Kodela
  • Substituted heteroaryl inhibitors of B-RAF
    Patent number: 8778929
    Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.
    Type: Grant
    Filed: September 28, 2009
    Date of Patent: July 15, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
  • NOVEL BENZAMIDES, PRODUCTION THEREOF, AND USE THEREOF AS MEDICAMENTS
    Publication number: 20140187539
    Abstract: Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the mixtures and the salts thereof. The compounds according to the invention are suitable for the treatment of respiratory complaints, particularly COPD and asthma.
    Type: Application
    Filed: March 4, 2014
    Publication date: July 3, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Holger WAGNER, Elke LANGKOPF, Frank HIMMELSBACH, Rolf GOEGGEL, Birgit JUNG
  • Indazole derivatives or pharmaceutically acceptable salts thereof as protein kinase inhibitors for proliferative diseases treatment, and a pharmaceutical composition containing the same as an active ingredient
    Patent number: 8754209
    Abstract: Disclosed are novel indazole derivatives represented by the following Chemical Formula 1 or pharmaceutically acceptable salts, hydrates or solvates thereof, and pharmaceutical compositions for the prevention or treatment of proliferative diseases, containing the same as an active ingredient. Having potent inhibitory effect against protein kinase, such as b-raf, KDR, Fms, Tie2, SAPK2a and Ret, inducing diseases caused by abnormal cell proliferation, the novel indazole derivatives can be used for the prevention or treatment of diseases caused by abnormal cell proliferation.
    Type: Grant
    Filed: December 4, 2009
    Date of Patent: June 17, 2014
    Assignees: Korea Institute of Science and Technology, Korea Research Institute of Chemical Technology, Korea Research Institute of Bioscience and Biotechnology
    Inventors: Tae Bo Sim, Jung Beom Son, Hwan Kim, Dong Sik Park, Hwan Geun Choi, Young Jin Ham, Jung Mi Hah, Kyung Ho Yoo, Chang Hyun Oh, So Ha Lee, Jae Du Ha, Sung Yun Cho, Byoung Mog Kwon, Dong Cho Han
  • Aminopyrrolidines as chemokine receptor antagonists
    Patent number: 8754107
    Abstract: The present invention is directed to novel aminopyrrolidines of formula I pharmaceutically acceptable salts thereof, metabolites thereof, isomers thereof, stereoisomers thereof or pro-drugs 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, cancers.
    Type: Grant
    Filed: November 16, 2007
    Date of Patent: June 17, 2014
    Assignee: AbbVie Inc.
    Inventors: Dawn M. George, Richard W. Dixon, Michael Friedman, Adrian D. Hobson, Biqin Li, Lu Wang, Xiaoyun Wu, Neil Wishart
  • Arylsulfonamide CCR3 antagonists
    Patent number: 8741894
    Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: June 3, 2014
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Garrett Thomas Potter, Jared Andrew Forrester
  • Benzothiazole derivatives
    Patent number: 8735576
    Abstract: Provided are compounds and their pharmaceutically acceptable salts that are useful for the treatment of diseases related to the adenosine receptor. Also included are methods of treating patients suffering from or susceptible to at least one symptom of abuse of, dependence on, or withdrawal from at least one substance.
    Type: Grant
    Filed: August 5, 2013
    Date of Patent: May 27, 2014
    Assignee: Biotie Therapies, Inc.
    Inventors: Thomas R. Malefyt, Lesley Pickford
  • CO-CRYSTALS AND SALTS OF CCR3-INHIBITORS
    Publication number: 20140135307
    Abstract: This invention relates to co-crystals and salts of CCR3 inhibitors of formula 1, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases related with the CCR3-receptor.
    Type: Application
    Filed: January 22, 2014
    Publication date: May 15, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Markus FRANK, Hans HAEBERLE, Manuel HENRY, Thorsten PACHUR, Marco SANTAGOSTINO, Uwe STERTZ, Thomas TREBING, Ulrike WERTHMANN
  • NOVEL COMPOUNDS AS HISTAMINE H3 RECEPTOR LIGANDS
    Publication number: 20140135304
    Abstract: The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to Histamine H3 receptors.
    Type: Application
    Filed: June 7, 2011
    Publication date: May 15, 2014
    Applicant: SUVEN LIFE SCIENCES LIMITED
    Inventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Ramasastri Kambhampati, Amol Dinakar Deshpande, Adi Reddy Dwarampudi, Narasimhareddy Gangadasari, Sangram Keshari Saraf, Vishwottam Nagaraj Kandikere, Pradeep Jayarajan, Ishtiyaque Ahmad, Mohmadsadik Abdulhamid Mulla, Venkateswarlu Jasti
  • SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND METHODS OF TREATMENT
    Publication number: 20140128368
    Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.
    Type: Application
    Filed: June 11, 2012
    Publication date: May 8, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael Miller, Andrew Stamford, Kallol Basu, Harold B. Wood, Duane DeMong, Wanying Sun, Joie Garfunkle, Christopher Moyes, Zhiyong Hu, Ping Liu, Scott D. Edmondson, Xing Dai, Byron Gabriel DuBois
  • Heterocyclic compound and use thereof
    Patent number: 8664380
    Abstract: Compounds represented by the formulas wherein each symbol is as defined in the specification, and a prodrug thereof have a superior renin inhibitory activity, and are useful as agents for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.
    Type: Grant
    Filed: June 17, 2009
    Date of Patent: March 4, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takanobu Kuroita, Yasuhiro Imaeda, Kouichi Iwanaga, Naohiro Taya, Hidekazu Tokuhara
  • SUBSTITUTED CYCLOPROPLY COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
    Publication number: 20140057893
    Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119.
    Type: Application
    Filed: April 5, 2012
    Publication date: February 27, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Scott Edmondson, Zhiqiang Guo, Harold B. Wood, Andrew W. Stamford, Michael W. Miller, Duane E. DeMong, Gregori J. Morriello, Rajan Anand, Vincent J. Colandrea, Megan Macala, Milana Maletic, Cheng Zhu, Yuping Zhu, Wanying Sun, Kake Zhao, Yong Huang, Joel M. Harris, Lehua Chang, Nam Fung Kar, Zhiyong Hu, Liping Wang, Bowei Wang, Ping Liu, Jason W. Szewczyk, William B. Geiss
  • AMPK-Activating Heterocycloalkyloxy(Hetero)Aryl Carboxamide, Sulfonamide And Amine Compounds And Methods For Using The Same
    Publication number: 20140051673
    Abstract: Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, E, T, n and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Application
    Filed: October 14, 2013
    Publication date: February 20, 2014
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventors: Hui Hong, Xiang Xu, Jiaxin Yu, Rajinder Singh, Ihab S. Darwish, Sambaiah Thota
  • HETEROAROMATIC COMPOUNDS AS BTK INHIBITORS
    Publication number: 20140045813
    Abstract: The present invention encompasses compounds of the formula (I) wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.
    Type: Application
    Filed: August 8, 2013
    Publication date: February 13, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Joerg Martin BENTZIEN, Angela Kay BERRY, Todd BOSANAC, Michael Jason BURKE, Darren Todd DISALVO, Joshua Courtney HORAN, Shuang LIANG, Can MAO, Wang MAO, Yue SHEN, Fariba SOLEYMANZADEH, Renee M. ZINDELL
  • SALTS AND SOLID FORMS OF (S)-3-(4-((4-(MORPHOLINOMETHYL)BENZYL)OXY)-1-OXOISOINDOLIN-2-YL)PIPERIDINE-2,6-DIONE AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME
    Publication number: 20140046057
    Abstract: Salts and solid forms of 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a stereoisomer thereof, are disclosed. Compositions comprising and methos of using the salts and solid forms are also disclosed.
    Type: Application
    Filed: August 8, 2013
    Publication date: February 13, 2014
    Applicant: Celgene Corporation
    Inventors: Benjamin M. Cohen, John M. Traverse, Jean Xu, Ying Li
  • PROCESS FOR THE PREPARATION OF MORPHOLINO SULFONYL INDOLE DERIVATIVES
    Publication number: 20140046059
    Abstract: The present invention relates to a process for the preparation of the compounds of formula (I) which are morpholino sulphonyl indole derivatives. The compounds of formula (I) are capable of inhibiting, modulating or regulating Insulin-Like-Growth Factor I Receptors or Insulin Receptors. The present invention also relates to the processes for preparation of the pharmaceutically acceptable salts of the compounds of formula (I).
    Type: Application
    Filed: April 19, 2012
    Publication date: February 13, 2014
    Applicant: PIRAMAL ENTERPRISES LIMITED
    Inventors: Malcolm Mascarenhas, Shashikant Patil, Ravindra Ashok Janrao, Abhijit Roychowdhury
  • Insulin-Like Growth Factor-1 Receptor Inhibitors
    Publication number: 20140045832
    Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating Insulin-Like-Growth Factor I Receptor and Insulin Receptor. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
    Type: Application
    Filed: April 19, 2012
    Publication date: February 13, 2014
    Applicants: PIRAMAL ENTERPRISES LIMITED, MERCK SHARP & DOHME CORP.
    Inventors: Sarala Balachandran, Christopher J. Dinsmore, Abhijit Roychowdhury, Rajiv Sharma, Ram Asrey Vishwakarma
  • CRYSTALLINE FORM OF A SALT OF A MORPHOLINO SULFONYL INDOLE DERIVATIVE AND A PROCESS FOR ITS PREPARATION
    Publication number: 20140045847
    Abstract: The present invention relates to a crystalline form of a pharmaceutically acceptable salt of a morpholino sulphonyl indole derivative, that is capable of inhibiting, modulating and/or regulating Insulin-Like-Growth Factor I Receptor and Insulin Receptor. The present invention also relates to a process for the preparation of the crystalline form of said compound.
    Type: Application
    Filed: April 19, 2012
    Publication date: February 13, 2014
    Applicant: PIRAMAL ENTERPRISES LIMITED
    Inventors: Suneel Manohar Babu Chennamsetty, Kishor Joshi, Yogesh Chinchwade, Yogesh Hulawale, Selvam Paramasivan, Meenakshi Sivakumar, Sivaramakrishnan Hariharan
  • PROCESSES FOR THE PREPARATION OF (S)-3-(4-((4-(MORPHOLINOMETHYL)BENZYL)OXY)-1-OXOISOINDOLIN-2-YL)PIPERIDINE-2,6-DIONE AND PHARMACEUTICALLY ACCEPTABLE FORMS THEREOF
    Publication number: 20140046058
    Abstract: Provided are processes for the preparation of enantiomerically enriched or enantiomerically pure 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a pharmaceutically acceptable form thereof.
    Type: Application
    Filed: August 8, 2013
    Publication date: February 13, 2014
    Applicant: Celgene Corporation
    Inventors: John F. Traverse, Chengmin Zhang, Gregg B. Feigelson, Benjamin M. Cohen, William W. Leong
  • Substituted phenoxypropylcycloamine derivatives as histamine-3 (H) receptor ligands
    Patent number: 8648067
    Abstract: The present invention provides compounds of formula I: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: February 11, 2014
    Assignees: Cephalon, Inc., Teva Sante
    Inventors: Edward R. Bacon, Thomas R. Bailey, Sankar Chatterjee, Derek D. Dunn, Greg A. Hostetler, Robert L. Hudkins, Brigitte Lesur, Babu G. Sundar, Allison L. Zulli, Christophe Yue
  • Chromenone Derivatives
    Publication number: 20140038937
    Abstract: The invention concerns chromenone compounds of Formula I; or pharmaceutically-acceptable salts thereof, wherein each of R1, R2, R3, R4, R5, n and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
    Type: Application
    Filed: August 6, 2013
    Publication date: February 6, 2014
    Applicant: Astrazeneca AB
    Inventors: Bernard Christophe BARLAAM, Sebastien Louis DEGORCE, Christine Marie Paul LAMBERT-VAN DER BREMPT, Jean-Jacques Marcel LOHMANN, Patrick PLE
  • COMPOUNDS AND METHODS FOR INHIBITING PHOSPHATE TRANSPORT
    Publication number: 20140023611
    Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: January 4, 2013
    Publication date: January 23, 2014
    Inventor: ARDELYX, INC.
  • N-PIPERIDINYL ACETAMIDE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS
    Publication number: 20140011996
    Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing N-piperidinyl acetamide derivatives as shown in formula (1).
    Type: Application
    Filed: August 29, 2013
    Publication date: January 9, 2014
    Applicant: Zalicus Pharmaceuticals Ltd.
    Inventors: Hassan Pajouhesh, Ramesh Kaul, Yanbing Ding, Yongbao Zhu, Lingyun Zhang, Nagasree Chakka, MIchael Edward Grimwood, Jason Tan, Yuanxi Zhou
  • BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHIBITORS
    Publication number: 20140010892
    Abstract: The invention provides compounds of the formula (I): The compounds have activity against cyclin dependent kinases, glycogen synthase kinase and Aurora kinases and are therefore useful to treat cancer and viral diseases.
    Type: Application
    Filed: May 24, 2013
    Publication date: January 9, 2014
    Applicant: Astex Therapeutics Limited
    Inventors: Valerio BERDINI, Michael Alistair O'BRIEN, Maria Grazia CARR, Theresa Rachel EARLY, Eva Figueroa NAVARRO, Adrian Liam GILL, Steven HOWARD, Gary TREWARTHA, Alison Jo-Anne WOOLFORD, Andrew James WOODHEAD, Paul Graham WYATT
  • PIPERIDINONE DERIVATIVES AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER
    Publication number: 20140011796
    Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
    Type: Application
    Filed: September 12, 2013
    Publication date: January 9, 2014
    Applicant: AMGEN INC.
    Inventors: Michael David BARTBERGER, Ana Gonzalez Buenrostro, Hilary Plake Beck, Xiaoqi Chen, Richard Victor Connors, Jeffrey Deignan, Jason Duquette, John Eksterwicz, Benjamin Fisher, Brian Matthew Fox, Jiasheng Fu, Zice Fu, Felix Gonzalez Lopez De Turiso, Michael William Gribble, Dann James Gustin, Julie Anne Heath, Xin Huang, Xianyun Jiao, Michael Johnson, Frank Kayser, David John Kopecky, Sujen Lai, Yihong Li, Zhihong Li, Jiwen Liu, Jonathan Dante Low, Brian Stuart Lucas, Zhihua Ma, Lawrence R. McGee, Joel McIntosh, Dustin McMinn, Julio Cesar Medina, Jeffrey Thomas Mihalic, Steven Howard Olson, Yosup Rew, Philip Marley Roveto, Daqing Sun, Xiaodong Wang, Yingcai Wang, Xuelei Yan, Ming Yu, Jiang Zhu
  • N-phenyl imidazole carboxamide inhibitors of 3-phosphoinositide-dependent protein kinase-1
    Patent number: 8623857
    Abstract: The present invention provide Imidazole Carboxamide Compounds of Formula (I): wherein D, T, R1, R2, R3, and R6 are as defined herein, and pharmaceutically acceptable salts of such Imidazole Carboxamide Compounds. The Imidazole Carboxamide Compounds are useful in the treatment of cancer and other aberrant conditions that result from overstimulation of the PDK-1 signaling pathway.
    Type: Grant
    Filed: May 24, 2011
    Date of Patent: January 7, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Hon-Chung Tsui, Sunil Paliwal, Hyunjin M. Kim, Angela D. Kerekes, Mary Ann Caplen, Sara J. Esposite, Brian A. McKittrick, Thierry Olivier Fischmann, Ronald J. Doll, Matthew Paul Rainka, Ang Li
  • Cyclic amine BACE-1 inhibitors having a benzamide substituent
    Patent number: 8623867
    Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: January 7, 2014
    Assignees: Merck Sharp & Dohme Corp., Pharmacopeia Drug Discovery, Inc.
    Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voight, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X. H. Le, Jeffrey H. Lowrie, Kurt W. Saionz, Suresh D. Babu
  • SULFONAMIDE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG
    Publication number: 20140005103
    Abstract: The present invention relates to Sulfonamide Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, W, X, R1, R2, R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Sulfonamide Derivative, and methods of using the Sulfonamide Derivatives for improving the pharmacokinetics of a drug.
    Type: Application
    Filed: June 25, 2013
    Publication date: January 2, 2014
    Inventors: Craig A. Coburn, Milana Maletic, Richard Soll, Chunsing Li, Yunfu Luo, Zhiqi Qi
  • COMPOUNDS AND METHODS FOR INHIBITING PHOSPHATE TRANSPORT
    Publication number: 20130336920
    Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y, A, R1 and R2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: January 4, 2013
    Publication date: December 19, 2013
    Applicant: ARDELYX, INC.
    Inventor: Ardelyx, Inc.
  • COMPOUNDS AND METHODS FOR INHIBITING PHOSPHATE TRANSPORT
    Publication number: 20130336921
    Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: January 4, 2013
    Publication date: December 19, 2013
    Applicant: ARDELYX, INC.
    Inventors: Jason G. Lewis, Jeffrey W. Jacobs, Nicholas Reich, Michael R. Leadbetter, Noah Bell, Han-Ting Chang, Tao Chen, Marc Navre, Dominique Charmot, Christopher Carreras, Eric Labonte
  • Benzothiazole Derivatives
    Publication number: 20130317219
    Abstract: Provided are compounds and their pharmaceutically acceptable salts that are useful for the treatment of diseases related to the adenosine receptor. Also included are methods of treating patients suffering from or susceptible to at least one symptom of abuse of, dependence on, or withdrawal from at least one substance.
    Type: Application
    Filed: August 5, 2013
    Publication date: November 28, 2013
    Applicant: Biotie Therapies, Inc.
    Inventors: Thomas R. Malefyt, Lesley Pickford
  • C5aR ANTAGONISTS
    Publication number: 20130317028
    Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.
    Type: Application
    Filed: May 14, 2013
    Publication date: November 28, 2013
    Applicant: ChemoCentryx, Inc.
    Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay Powers, Horoko Tanaka, Ju Yang, Yibin Zeng
  • N-ACYLSULFONAMIDE APOPTOSIS PROMOTERS
    Publication number: 20130310344
    Abstract: The present invention relates to compounds of Formula (I): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit Bcl-2 and/or Bcl-XL activities and may be used for the treatment of cancer.
    Type: Application
    Filed: August 5, 2011
    Publication date: November 21, 2013
    Applicant: ASTRAZENECA AB
    Inventors: Robert Bruce Diebold, Thomas Gero, Paul Grover, Shan Huang, Stephanos Ioannidis, Claude Afona Ogoe, Jamal Carlos Saeh, Jeffrey Gilbert Varnes
  • MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
    Publication number: 20130310379
    Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
    Type: Application
    Filed: November 21, 2011
    Publication date: November 21, 2013
    Applicant: CONSTELLATION PHARMACEUTICALS
    Inventors: Brian K. Albrecht, James Edmund Audia, Alexandre Gagnon, Jean-Christophe Harmange, Christopher G. Naveschuk
  • Triazole Compounds that Modulate HSP90 Activity
    Publication number: 20130303493
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Application
    Filed: July 12, 2013
    Publication date: November 14, 2013
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Joseph Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
  • NAMPT INHIBITORS
    Publication number: 20130303509
    Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
    Type: Application
    Filed: May 10, 2013
    Publication date: November 14, 2013
    Applicant: ABBVIE INC.
    Inventors: Todd M. Hansen, Kenton Longenecker, Howard R. Heyman, Michael L. Curtin, Richard F. Clark, Bryan Sorensen, Zhiqin Ji, Kevin Woller, George Doherty, Robin Frey
  • NAMPT INHIBITORS
    Publication number: 20130303510
    Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
    Type: Application
    Filed: May 10, 2013
    Publication date: November 14, 2013
    Applicant: ABBVIE INC.
    Inventors: Todd M. Hansen, Kenton Longenecker, Howard R. Heyman, Michael L. Curtin, Richard F. Clark, Bryan Sorensen, Zhiqin Ji, Kevin Woller, George Doherty, Robin Frey
  • Prolylcarboxypeptidase inhibitors
    Patent number: 8569299
    Abstract: Compounds of structural formulas I-1 and I-2 are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Grant
    Filed: June 3, 2011
    Date of Patent: October 29, 2013
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Thomas H. Graham, Wensheng Liu, Iyassu K. Sebhat, Dong-Ming Shen, Zhi-Cai Shi
  • INHIBITORS OF CYTOCHROME P450 (CYP3A4)
    Publication number: 20130274254
    Abstract: The present application provides for a compound of formula I, and related compounds, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional therapeutic agent.
    Type: Application
    Filed: December 20, 2011
    Publication date: October 17, 2013
    Applicant: Gilead Sciences, Inc.
    Inventors: Carina Cannizzaro, Manoj C. Desai, Hon Chung Hui, Melody S. Lee, Hongtao Liu, Jianyu Sun, Lianhong Xu
  • NOVEL COMPOUNDS AND COMPOSITIONS FOR THE INHIBITION OF NAMPT
    Publication number: 20130273034
    Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.
    Type: Application
    Filed: September 2, 2011
    Publication date: October 17, 2013
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Bingsong Han, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng, Po-Wai Yuen
  • CRYSTAL OF AMIDE COMPOUND
    Publication number: 20130252954
    Abstract: Provision of crystal of 1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride which has a superior rennin inhibitory activity and is useful as a prophylactic or therapeutic agent for hypertension and various organ disorders caused by hypertension, and the like. Crystal of 1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride having an X-ray powder diffraction pattern showing characteristic peaks at interplanar spacings (d) of around 26.43±0.2, 7.62±0.2 and 4.32±0.2 angstroms.
    Type: Application
    Filed: June 15, 2011
    Publication date: September 26, 2013
    Inventor: Masato KITAYAMA
  • BICYCLIC GPR119 MODULATORS
    Publication number: 20130245000
    Abstract: The present invention relates to compounds of Formula (I) that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of GPR119 receptor activity. The invention also relates to the process for preparation of the compounds, pharmaceutical compositions thereof. The invention further relates to methods of treating, preventing and/or managing diseases, disorders syndromes or conditions associated with the modulation of GPR119 receptor by using either alone or in combinations of Formula (I).
    Type: Application
    Filed: November 24, 2011
    Publication date: September 19, 2013
    Applicant: LUPIN LIMITED
    Inventors: Rajesh Thotapally, Onkar Gangaram Kachi, Atish Harishchandra Rodge, Ashok Bhau Pathak, Bhavana Shrirang Kardile, Milind Dattatraya Sindkhedkar, Venkata P. Palle, Rajender Kumar Kamboj
  • HETEROCYCLIC MODULATORS OF CANNABINOID RECEPTORS
    Publication number: 20130237536
    Abstract: Heterocyclic compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.
    Type: Application
    Filed: April 26, 2013
    Publication date: September 12, 2013
    Applicant: The Cleveland Clinic Foundation
    Inventors: Mohamed Naguib Attala, Philippe Diaz
  • LACTAM DERIVATIVES USEFUL AS OREXIN RECEPTOR ANTAGONISTS
    Publication number: 20130237525
    Abstract: The present invention relates to lactam derivatives of formula (I) wherein Y, R1, R2 and R3 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.
    Type: Application
    Filed: November 9, 2011
    Publication date: September 12, 2013
    Applicant: ACTELION PHARMACEUTICALS LTD.
    Inventors: Hamed Aissaoui, Christoph Boss, Christine Brotschi, Bibia Heidmann, Thierry Sifferlen, Jodi T. Williams
  • Kinase inhibitor compounds
    Patent number: 8524709
    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: Grant
    Filed: January 12, 2012
    Date of Patent: September 3, 2013
    Assignee: Tyrogenex, Inc.
    Inventors: Congxin Liang, Ming Qi, Shu Gao, Zhigang Li
  • Heterocyclic derivatives as M-GLU5 antagonists
    Patent number: 8518916
    Abstract: This invention relates to novel heterocyclic compounds having selective affinity for the mGlu5 subtype of metabotropic receptors, pharmaceutical compositions thereof and uses for such compounds and compositions in the treatment of lower urinary tract disorders, such as neuromuscular dysfunction of the lower urinary tract, and in the treatment of migraine and gastroesophagael reflux disease (GERD).
    Type: Grant
    Filed: August 4, 2008
    Date of Patent: August 27, 2013
    Assignee: Recordati Ireland Limited
    Inventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Elena Poggesi, Davide Graziani, Matteo Longhi
  • PYRIDINE-2-DERIVATIVES AS SMOOTHENED RECEPTOR MODULATORS
    Publication number: 20130210800
    Abstract: The present application relates to compounds of Formula (I), and Formula (II), or pharmaceutically acceptable salt thereof, wherein A, X, Y, Z, e, f, R1, R2, R3, R4, R5, R5b, R6, R7, R8, R9, R10, R11, R20, R21, R22 and R23 are defined herein. These novel pyridine derivatives that are useful in therapy, in particular for treating diseases or conditions mediated by Smo, including the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to methods of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: October 19, 2011
    Publication date: August 15, 2013
    Applicant: PFIZER INC.
    Inventors: Sajiv Krishnan Nair, Simon Paul Planken