Plural Carbocyclic Rings Containing Patents (Class 546/234)
  • Publication number: 20150141397
    Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Application
    Filed: August 5, 2014
    Publication date: May 21, 2015
    Inventors: Trevor T. Charvat, Junfa Fan, Christopher W. Lange, Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jeffrey P. McMahon, Jay Powers, Sreenivas Punna, Ju Yang
  • Patent number: 9034922
    Abstract: A composition for maintaining a function of platelets, the composition comprising, as an active ingredient, a compound represented by the following general formula (I) or a salt thereof, or a solvate thereof: wherein X represents a phenylene group; Y represents any one of a hydrogen atom and —(CH2)mR1; wherein m represents an integer of any one of 0 to 4; and R1 is any one of —NR5COR2, —NR5SO2R2, and —NR3R4; wherein R2 represents any one of a C1 to C6 alkyl group, an aryl group, a C1 to C6 alkoxy group, and the like; R3 and R4 represent a C1 to C6 alkyl group or the like; and R5 represents any one of a hydrogen atom, a C1 to C6 alkyl group, and the like; and Z represents any one of a hydrogen atom and a C1 to C6 alkyl group.
    Type: Grant
    Filed: September 16, 2011
    Date of Patent: May 19, 2015
    Assignees: THE UNIVERSITY OF TOKYO, KAKEN PHARMACEUTICAL CO., LTD.
    Inventors: Koji Eto, Ryoko Ohnishi, Hiromitsu Nakauchi, Takahiko Murata
  • Publication number: 20150126493
    Abstract: The invention provides bicyclic sulfone compounds, pharmaceutical compositions, methods of inhibiting RORy activity, reducing the amount of iL-17 in a subject, and treating immune disorders and inflammatory disorders using such bicyclic sulfone compounds. Another aspect of the invention provides a method of treating a subject suffering from a medical disorder. The method comprises administering to the subject a therapeutically effective amount of one or more bicyclic sulfone compounds described herein. In certain other embodiments, the disorder is rheumatoid arthritis.
    Type: Application
    Filed: May 3, 2013
    Publication date: May 7, 2015
    Inventors: Thomas D. Aicher, Kenneth J. Barr, Vladimir Simov, Willam D. Thomas, Peter L. Toogood, Chad A. Van Huis
  • Patent number: 9018200
    Abstract: Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: April 28, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Milana Maletic, Harold B. Wood, Wanying Sun
  • Patent number: 8951999
    Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: February 10, 2015
    Assignee: Orexo AB
    Inventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Robert Roenn, Benjamin Pelcman
  • Publication number: 20150038708
    Abstract: In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: August 5, 2014
    Publication date: February 5, 2015
    Inventors: James Turkson, Patrick Gunning
  • Publication number: 20150038515
    Abstract: Pharmaceutical compositions of the invention comprise covalently closed circular DNA formation inhibitors having a disease-modifying action in the treatment of diseases associated with the formation of covalently closed circular DNA that include hepatitis B infection, and any disease involving formation of covalently closed circular DNA.
    Type: Application
    Filed: February 28, 2013
    Publication date: February 5, 2015
    Inventors: Andrea Cuconati, Haitao Guo, Timothy M. Block, Ju-Tao Guo, Xiaodong Xu, Huagang Lu, Dawei Cai
  • Publication number: 20140377219
    Abstract: Chemical compounds that inhibit retroviruses are presented herein. More particularly, this disclosure provides small molecule compounds that inhibit infection with, or treat infection caused by, human immunodeficiency viruses.
    Type: Application
    Filed: September 6, 2012
    Publication date: December 25, 2014
    Applicant: New York Blood CEnter, Inc.
    Inventors: Asim Kumar Debnath, Francesca Curreli, Peter D. Kwong, Young Do Kwon
  • Patent number: 8895551
    Abstract: The invention relates to acrylamide compounds of Formula I mentioned below. The invention is also directed to the use compounds of Formula I to treat or prevent a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: April 2, 2010
    Date of Patent: November 25, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hidenori Mikamiyama, Akira Matsumura, Moriyasu Masui, Kosuke Anan, Kayoko Hata
  • Publication number: 20140296202
    Abstract: Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
    Type: Application
    Filed: October 18, 2012
    Publication date: October 2, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Milana Maletic, Harold B. Wood, Wanying Sun
  • Patent number: 8835419
    Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: September 16, 2014
    Assignee: ChemoCentryx, Inc.
    Inventors: Trevor T. Charvat, Junfa Fan, Christopher W. Lange, Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jeffrey P. MacMahon, Jay Powers, Sreenivas Punna, Ju Yang
  • Publication number: 20140256698
    Abstract: The present invention is directed to inhibitors of cathepsins and the methods for using and making such inhibitors.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 11, 2014
    Inventors: Robert Booth, Jeff Dener, Michael Green
  • Publication number: 20140194383
    Abstract: Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer, (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.
    Type: Application
    Filed: April 9, 2012
    Publication date: July 10, 2014
    Applicants: Cornell University, Coferon, Inc., Purdue Research Foundation
    Inventors: Francis Barany, Maneesh Pingle, Donald E. Bergstrom, Sarah F. Giardina, Lee Daniel Arnold
  • Publication number: 20140179665
    Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
    Type: Application
    Filed: December 9, 2013
    Publication date: June 26, 2014
    Inventors: George D. Hartman, Osvaldo A. Flores
  • Patent number: 8759528
    Abstract: The invention relates to new piperidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: December 3, 2012
    Date of Patent: June 24, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Gerald Juergen Roth, Martin Fleck, Thorsten Lehmann-Lintz, Bernd Nosse
  • Publication number: 20140171467
    Abstract: Methods and compositions are provided that are utilized for treatment and/or prevention of intraventricular hemorrhage or progressive hemorrhagic necrosis (PHN), particularly following spinal cord injury. In particular, the methods and compositions are inhibitors of a particular NCca-ATP channel and include, for example, inhibitors of SURI and/or inhibitors of TRPM4. Kits for treatment and/or prevention of intraventricular hemorrhage or progressive hemorrhagic necrosis (PHN), particularly following spinal cord injury, are also provided. The present invention also concerns treatment and/or prevention of intraventricular hemorrhage in infants, including premature infants utilizing one or more inhibitors of the channel is provided to the infant, for example to brain cells of the infant.
    Type: Application
    Filed: September 27, 2013
    Publication date: June 19, 2014
    Inventor: J. Marc Simard
  • Publication number: 20140171403
    Abstract: The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin.
    Type: Application
    Filed: March 15, 2013
    Publication date: June 19, 2014
    Applicant: Novartis AG
    Inventors: Darren Mark Legrand, Vikki Furminger, Christopher Thomson, Owen Rhys Hughes, Emily Stanley
  • Publication number: 20140107340
    Abstract: The present invention is directed to benzamide containing compounds which inhibit the P2X7 receptor
    Type: Application
    Filed: October 10, 2013
    Publication date: April 17, 2014
    Applicant: H. Lundbeck A/S
    Inventors: John Paul Kilburn, Lars Kyhn Rasmussen, Mikkel Jessing, Eman Mohammed Eldemenky, Bin Chen, Yu Jiang, Allen T. Hopper
  • Publication number: 20140107335
    Abstract: The present invention is directed to novel cyclic amines which inhibit the P2X7 receptor.
    Type: Application
    Filed: October 10, 2013
    Publication date: April 17, 2014
    Applicant: H. Lundbeck A/S
    Inventors: John Paul Kilburn, Lars Kyhn Rasmussen, Mikkel Jessing, Eman Mohammed Eldemenky, Bin Chen, Yu Jiang
  • Publication number: 20140094493
    Abstract: A compound of Formula (I), and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein R1 is independently selected from F, Cl, Br, CN, NH2, OH, CHO, COOH, oxo, C1-4alkyl, C1-4alkoxy, CONH2 (optionally mono- or di-substituted by C1-4alkyl) and SO2NH2, R2 is independently selected from C1-6allkyl substituted by R3 wherein the C1-6alkyl chain optionally comprises one or two heteroatoms select from O; R3 is selected from aryl, C3-6cycloalkyl, C3-6heterocyclyl and C3-6heteroaryl, wherein the heterocyclyl and heteroaryl rings are nitrogen containing; and wherein R3 is optonally substituted by one or more groups selected from R1; n1 is zero or an integer from 1 to 2; n2 is an integer from 1 to 2; and the sum of n1 and 2 is less than or equal to 2; R5 is selected from any group defined for R1 and R2; R6a and R6b are independently selected from H or C1-4alkyl; R7 is independently selected from F, Cl, Br, CN, NH2, OH, CHO, COOH, oxo, C1-4al
    Type: Application
    Filed: February 6, 2012
    Publication date: April 3, 2014
    Inventors: Jillian G. Baker, Peter M. Fischer, Christophe Fromont, Sheila M. Gardiner, Stephen J. Hill, Gopal Jadhav, Barrie Kellam, Shailesh Mistry, Jeanette Woolard
  • Patent number: 8642772
    Abstract: Piperidine compounds and pharmaceutically useful salts thereof, a pharmaceutical composition including an effective amount of the racemic or enantiomerically enriched piperidine compounds to treat gastrointestinal diseases, and a method of treating gastrointestinal diseases in a mammal are provided.
    Type: Grant
    Filed: October 9, 2009
    Date of Patent: February 4, 2014
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Coo-Min Chung, Hyung-Jin Jun, Jin-Sung Kim, Hui-Ho Kim, Hye-Kyung Min, Yong-Gil Kim, Jong-Gil Choi, Hongwook Kim
  • Publication number: 20140024679
    Abstract: The present invention provides novel phenylcycloalkylmethylamine derivatives, and methods of preparing phenylcycloalkylmethylamine derivatives. The present invention also provides methods of using phenylcycloalkylmethylamine derivatives and compositions of phenylcycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.
    Type: Application
    Filed: December 31, 2012
    Publication date: January 23, 2014
    Applicant: Reviva Pharmaceuticals, Inc.
    Inventor: Reviva Pharmaceuticals, Inc.
  • 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
  • Publication number: 20140005222
    Abstract: The present invention provides a compound of the Formula II: wherein A is: R1 is CH3, CF3, or F; R2 is H, CH3, or F; R3 is CH3, OCH3, OH, F; R4 is OH or CH2OH; and X is CH or N; or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: June 20, 2013
    Publication date: January 2, 2014
    Inventors: Maria-Jesus BLANCO-PILLADO, Matthew Joseph FISHER, Steven Lee KUKLISH, Tatiana Natali VETMAN
  • Patent number: 8598206
    Abstract: The invention provides compounds that are effective as inhibitors of human plasmin and plasma kallikrein, and that are useful for the prevention of blood loss and as components of fibrin adhesives. The invention further provides methods of making and using the compounds.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: December 3, 2013
    Assignee: The Medicines Company (Leipzig) GmbH
    Inventors: Peter Herold, Mohammed Daghish, Stjepan Jelakovic, Friedrich-Alexander Ludwig, Claudia Reichelt, Alexander Schulze, Andrea Schweinitz
  • 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
  • Publication number: 20130310347
    Abstract: High throughput methods for identifying novel inhibitors of Hsp90 chaperone protein folding are disclosed. The inhibitors so identified disrupt the binding of p23 to either Hsp90? or Hsp90? and have selective activity against the proliferation of cancer cells. In particular are provided embodiments of therapeutic compositions that comprise at least one inhibitor of an Hsp90 chaperone activity, the inhibitor being any of the compounds designated as CP1-CP19 as shown in FIGS. 1A-1D or a 2-(trifluoromethyl)pyrimidin-2-yl)thio)acetamide derivatives.
    Type: Application
    Filed: May 21, 2013
    Publication date: November 21, 2013
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Carmel Chan, Sanjiv S. Gambhir, David E. Solow-Cordero, Aileen Hoehne, Ramasamy Paulmurugan
  • Publication number: 20130310399
    Abstract: An insecticidal acaricidal and nematicidal composition of formula I Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; the ring is a 6 membered aromatic ring or is a 5 or 6 membered heteroaromatic ring; Z and provided that both are not N; R1, R2, R3, R3a, R4, R8 and Ra are specified organic groups and n and p are independently 0, 1, 2, 3 or 4; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.
    Type: Application
    Filed: July 24, 2013
    Publication date: November 21, 2013
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Peter Maienfisch, Louis-Pierre Molleyres, Jerome Cassayre, Fredik Cederbaum, Camilla Corsi, Thomas Pitterna
  • Patent number: 8580821
    Abstract: The present invention relates to trans-derivatives of formula wherein R1, R2, R3, and the dotted line are as defined herein and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I are good inhibitors of the serotonin transporter (SERT inhibitors) and simultaneously, they have good activity on the NK-1 receptor (dual effect). By virtue of their efficacy as SERT inhibitors, the compounds in the present invention are particularly useful for the treatment of CNS disorders and psychotic disorders, in particular in the treatment or prevention of depressive states and/or in the treatment of anxiety.
    Type: Grant
    Filed: January 10, 2011
    Date of Patent: November 12, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christophe Grundschober, Patrick Schnider
  • Patent number: 8575170
    Abstract: Flurbiprofen analog compounds having an amino acid derivatized at the flurbiprofen alkanoic acid carboxyl group and terminating at an ester or amide group are effective in inhibiting cancer cells in vitro and inhibiting the growth of cancers in viva. The compounds and pharmaceutical compositions containing them are particularly useful for the treatment of lung, pancreatic and head and neck cancers.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: November 5, 2013
    Assignee: The Regents of the Unversity of Colorado, a body corporate
    Inventors: Lajos Gera, Daniel C. Chan, Robert S. Hodges, Paul A. Bunn
  • Publication number: 20130281452
    Abstract: Substituted 4-aminobenzamides, pharmaceutical compositions containing these compounds and also methods of using these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Application
    Filed: April 18, 2013
    Publication date: October 24, 2013
    Inventors: Gregor BAHRENBERG, Sven KUEHNERT, Simon LUCAS, Wolfgang SCHROEDER
  • Publication number: 20130251673
    Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
    Type: Application
    Filed: December 21, 2012
    Publication date: September 26, 2013
    Applicant: Novira Therapeutics, INC.
    Inventors: George D. HARTMAN, Osvaldo A. FLORES
  • Patent number: 8541586
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Grant
    Filed: August 23, 2011
    Date of Patent: September 24, 2013
    Assignee: Rensselaer Polytechnic Institute
    Inventor: Mark P. Wentland
  • Publication number: 20130225621
    Abstract: In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: August 2, 2011
    Publication date: August 29, 2013
    Applicants: University of Toronto Mississauga, University of Central Florida Research Foundation, Inc.
    Inventors: James Turkson, Patrick Gunning
  • Publication number: 20130217660
    Abstract: Compounds of structural formula I 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: Application
    Filed: May 12, 2011
    Publication date: August 22, 2013
    Inventors: Dong-Ming Shen, John S. Debenham, Thomas H. Graham, Matthew J. Clements, Yong Zhang
  • Patent number: 8501937
    Abstract: The invention is directed to compounds and methods of synthesizing hydroxyethlamino amides and their use in treatment of aspartyl protease mediated diseases and conditions.
    Type: Grant
    Filed: March 28, 2012
    Date of Patent: August 6, 2013
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Steven J. Coats, Dennis J. Hlasta, Mark J. Schulz
  • Patent number: 8492550
    Abstract: The application describes modulators of MIP-1? or CCR-1 of the formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein ring A, T, V, R1, R2 and R5, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
    Type: Grant
    Filed: March 5, 2009
    Date of Patent: July 23, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Percy H. Carter, Lyndon A. M. Cornelius
  • Publication number: 20130177900
    Abstract: A composition for maintaining a function of platelets, the composition comprising, as an active ingredient, a compound represented by the following general formula (I) or a salt thereof, or a solvate thereof: wherein X represents a phenylene group; Y represents any one of a hydrogen atom and —(CH2)mR1; wherein m represents an integer of any one of 0 to 4; and R1 is any one of —NR5COR2, —NR5SO2R2, and —NR3R4; wherein R2 represents any one of a C1 to C6 alkyl group, an aryl group, a C1 to C6 alkoxy group, and the like; R3 and R4 represent a C1 to C6 alkyl group or the like; and R5 represents any one of a hydrogen atom, a C1 to C6 alkyl group, and the like; and Z represents any one of a hydrogen atom and a C1 to C6 alkyl group.
    Type: Application
    Filed: September 16, 2011
    Publication date: July 11, 2013
    Applicants: KAKEN PHARMACEUTICAL CO., LTD., THE UNIVERSITY OF TOKYO
    Inventors: Koji Eto, Ryoko Ohnishi, Hiromitsu Nakauchi, Takahiko Murata
  • Publication number: 20130172315
    Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Application
    Filed: November 30, 2012
    Publication date: July 4, 2013
    Applicant: ChemoCentryx, Inc.
    Inventor: ChemoCentryx, Inc.
  • Publication number: 20130165444
    Abstract: Piperidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.
    Type: Application
    Filed: December 14, 2012
    Publication date: June 27, 2013
    Inventors: Gerald Juergen ROTH, Martin FLECK, Bernd NOSSE, Thorsten LEHMANN-LINTZ
  • Patent number: 8470831
    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: Grant
    Filed: September 23, 2009
    Date of Patent: June 25, 2013
    Assignee: Cogenia SRL
    Inventors: Daniele Fancelli, Mario Varasi, Simon Plyte, Marco Ballarini, Anna Cappa, Giacomo Carenzi, Saverio Minucci, Gilles Pain, Manuela Villa
  • Patent number: 8461341
    Abstract: The present invention relates to a resolution process of (±)-methyl phenyl[4-[4-[[[4?-(trifluoromethyl)-2-biphenylyl]carbonyl]amino]phenyl]-1-piperidinyl]acetate to isolate the MTP (microsomal triglyceride transfer protein) inhibitor methyl (2S)-phenyl[4-[4-[[[4?-(trifluoromethyl)-2-biphenylyl]carbonyl]amino]phenyl]-1-piperidinyl]acetate and an epimerisation procedure for racemizing methyl (2R)-phenyl[4-[4-[[[4?-(trifluoromethyl)-2-biphenylyl]carbonyl]amino]phenyl]-1-piperidinyl]acetate.
    Type: Grant
    Filed: May 27, 2010
    Date of Patent: June 11, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Alex Herman Copmans, Jérôme Albert Joseph Hoet, Albert Louis Anna Willemsens, Wouter Louis J Couck, Joannes Petrus Van Dun
  • Publication number: 20130109701
    Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfon-amide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein X, Ar1, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
    Type: Application
    Filed: July 4, 2011
    Publication date: May 2, 2013
    Applicant: Pfizer Limited
    Inventors: Alan Daniel Brown, David James Rawson, Robert Ian Storer, Nigel Alan Swain
  • Patent number: 8420823
    Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].
    Type: Grant
    Filed: April 17, 2009
    Date of Patent: April 16, 2013
    Assignee: MSD K.K.
    Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
  • Publication number: 20130085160
    Abstract: The present invention provides a novel benzamide derivative or a pharmaceutically acceptable salt thereof, a method for preparing the same, and a 5-HT4 receptor agonist containing the same as an active ingredient. Benzamide derivatives of the present invention have a superior affinity for 5-HT4 receptors, a capability to reduce a gastric emptying time and a low toxicity, and consequently are therapeutically effective for the treatment of a variety of diseases associated with 5-HT4 receptors.
    Type: Application
    Filed: April 18, 2011
    Publication date: April 4, 2013
    Inventors: Soon-Hoe Kim, Weon-Bin Im, Sung-Hak Choi, Sun-Ho Choi, Ju-Hee Sohn, Hyun-Jung Sung, Mi-Yeon Kim, Kang-Hun Cho, Tae-Kyoung Sohn
  • Patent number: 8410138
    Abstract: Compositions and methods for treatment and prevention of disorders and conditions characterized by reduced TGF-? signaling are described.
    Type: Grant
    Filed: December 12, 2011
    Date of Patent: April 2, 2013
    Assignees: The Board of Trustees of the Leland Stanford Junior University, SRI International
    Inventors: Anton Wyss-Coray, Mary J. Tanga
  • Publication number: 20130079320
    Abstract: The invention relates to amine substituted methanesulfonamide derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Application
    Filed: September 25, 2012
    Publication date: March 28, 2013
    Applicant: Gruenenthal GmbH
    Inventor: Gruenenthal GmbH
  • Publication number: 20130045165
    Abstract: 4-Fluoro-4-phenylpiperidin-1-yl ? antagonists of general structure as well as pharmaceutical compositions comprising compounds of formula I, are disclosed. These compounds and compositions are useful as treatments of conditions or diseases associated with binding opioid receptors including pain, obesity, hyperalgesia, inflammation, osteoarthritis, drug addiction, and cancer. These compounds and compositions are also useful as treatments for tardive dyskinesia.
    Type: Application
    Filed: April 29, 2011
    Publication date: February 21, 2013
    Applicant: KINENTIA BIOSCIENCES, LLC
    Inventor: David J. Fairfax
  • Patent number: 8367698
    Abstract: [Problem] There is provided a compound useful as a preventive or remedy for cardiovascular disease, neurologic disease, metabolic disease, reproductive disease, and digestive disease. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I) wherein Z represents wherein n1, n2, and n3 are 0, 1, or 2, respectively; R1 represents C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 represents aryl or heteroaryl; R3 represents a hydrogen atom, C1-6 alkyl, or the like; and M1, M2, M3, and M4 independently represent a hydrogen atom, C1-6 alkyl, or the like, or M1, together with M2, M3, or M4, forms —CH2— or the like.
    Type: Grant
    Filed: May 23, 2012
    Date of Patent: February 5, 2013
    Assignee: MSD K.K.
    Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
  • Publication number: 20130029991
    Abstract: The present invention relates to new sulfonamide derivatives of formula (I) wherein R1-R8 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these same compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
    Type: Application
    Filed: August 1, 2012
    Publication date: January 31, 2013
    Inventors: Gyula Beke, Eva Bozo, Sandor Farkas, Katalin Hornok, Gyorgy Keseru, Eva Schmidt, Eva Szentirmay, Istvan Vago, Monika Vastag