Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Piperidine Ring Patents (Class 546/225)
  • Publication number: 20150087674
    Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of severe pain may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of postoperative pain, cancer pain, kidney stones pain, fractures, local pain, chronic pain, chemotherapy induced pain, neuropathic pain, post herpetic neuralgia, neuralgia, motor neurone disease, diabetic neuropathy, postherpetic neuralgia, injury, post-operative pain, osteoarthritis, rheumatoid arthritis, multiple sclerosis, spinal cord injury, migraine, HIV related neuropathic pain, cancer pain and lower back pain.
    Type: Application
    Filed: February 23, 2013
    Publication date: March 26, 2015
    Inventor: Mahesh KANDULA
  • Patent number: 8962659
    Abstract: The present invention provides a compound of the Formula II: wherein X is: R1 is H, —CN, or F; R2 is H or methyl; R3 is H; and R4 is H, methyl, or ethyl; or R3 and R4 joined together form a cyclopropyl ring; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 20, 2013
    Date of Patent: February 24, 2015
    Assignee: Eli Lilly and Company
    Inventors: Matthew Allen Schiffler, Jeremy Schulenburg York
  • Publication number: 20150051194
    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: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. WENTLAND
  • Publication number: 20140349368
    Abstract: The present invention relates to compounds that exhibit vasodilatory and anti-inflammatory effects by inhibiting the activity of soluble epoxide hydrolase (sEH). The present invention is also directed to methods of identifying such compounds, and use of such compounds for the treatment of diseases related to dysfunction of vasodilation, inflammation, and/or endothelial cells. In particular non-limiting embodiments, components of the invention may be used to treat hypertension.
    Type: Application
    Filed: February 17, 2014
    Publication date: November 27, 2014
    Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Donald W. Landry, Yuli Xie, Yidong Lu, Gangli Gong, Shi-Xian Deng, Kirsten Alison Rinderspacher
  • Publication number: 20140329746
    Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
    Type: Application
    Filed: July 16, 2014
    Publication date: November 6, 2014
    Inventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
  • Publication number: 20140309228
    Abstract: The present disclosure provides substituted pyridine and pyrimidine compounds of Formula (I): A1-X-A2-Z-R1 (I) and the pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein A, X, A, Z, and R are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.
    Type: Application
    Filed: October 30, 2012
    Publication date: October 16, 2014
    Applicant: Purdue Pharma L.P.
    Inventor: John J. Engel
  • Publication number: 20140243373
    Abstract: There is described a group of novel cyclic amine derivative compounds having an EP4 receptor agonistic activity. Specifically, the compounds according to the invention are provided with analgesic, antinflammatory, antiglaucoma activity, and also with anti-osteoporosis and antiulcerative activity. The present invention therefore relates to novel cyclic amine derivative compounds, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as pain, glaucoma, ulcerative colitis and osteoporosis.
    Type: Application
    Filed: July 4, 2011
    Publication date: August 28, 2014
    Applicant: Rottapharm S.P.A.
    Inventors: Manuela Borriello, Sabrina Pucci, Luigi Piero Stasi, Lucio Rovati
  • 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
  • Publication number: 20140163024
    Abstract: Compounds of the formula Ia or Ib: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: December 10, 2013
    Publication date: June 12, 2014
    Applicant: GENENTECH, INC.
    Inventors: Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Simon Gaines, Jonathan Killen, Stuart Ward
  • Publication number: 20140121217
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein A, Y, L, R1, W1 and W2 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: January 2, 2014
    Publication date: May 1, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Lijun Sun, Jun Jiang, Yu Xie
  • Patent number: 8653273
    Abstract: The present invention relates to compounds that exhibit vasodilatory and anti-inflammatory effects by inhibiting the activity of soluble epoxide hydrolase (sEH). The present invention is also directed to methods of identifying such compounds, and use of such compounds for the treatment of diseases related to dysfunction of vasodilation, inflammation, and/or endothelial cells. In particular non-limiting embodiments, components of the invention may be used to treat hypertension.
    Type: Grant
    Filed: July 7, 2011
    Date of Patent: February 18, 2014
    Assignee: The Trustees of Columbia University in the city of New York
    Inventors: Kirsten Alison Rinderspacher, Donald W. Landry, Yuli Xie, Yidong Liu, Gangli Gong, Shi-Xian Deng
  • Publication number: 20140005226
    Abstract: The present invention provides a compound of the Formula II: wherein X is: R1 is H, —CN, or F; R2 is H or methyl; R3 is H; and R4 is H, methyl, or ethyl; or R3 and R4 joined together form a cyclopropyl ring; or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: June 20, 2013
    Publication date: January 2, 2014
    Inventors: Matthew Allen SCHIFFLER, Jeremy Schulenburg YORK
  • Publication number: 20130345199
    Abstract: The present invention relates to 1-[m-Carboxamido(hetero)aryl-methyl]-piperidine-4-carboxamide derivatives of formula (I) wherein X, Ar1, R1, R2, R3, R4, R5 and p 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 CXCR7 receptor modulators.
    Type: Application
    Filed: June 21, 2013
    Publication date: December 26, 2013
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Heinz FRETZ, Markus Gude, Philippe Guerry, Thierry Kimmerlin, Francois Lehembre, Thomas Pfeifer, Anja Valdenaire
  • Publication number: 20130324556
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrate thereof Wherein Y, Z, R3, U, R4, m and n are as defined in the claims.
    Type: Application
    Filed: January 27, 2012
    Publication date: December 5, 2013
    Inventors: Joe William Boyd, Paul Meo, Michael Higginbottom, Iain Simpson, David Mark Mountford, Edward Daniel Savory
  • 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
  • Publication number: 20130296245
    Abstract: Provided are a compound of formula (I), pharmaceutically acceptable salts thereof, preparation methods and applications thereof for inhibiting thrombin, and applications in the treatment and prevention of thrombin-mediated and thrombin-related diseases.
    Type: Application
    Filed: November 14, 2011
    Publication date: November 7, 2013
    Inventors: Min Li, Hanbin Shan, Yu Huang, Zhedong Yuan, Xiong Yu
  • Patent number: 8541572
    Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF—or combinations thereof.
    Type: Grant
    Filed: November 9, 2009
    Date of Patent: September 24, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joseph A. Kozlowski, Wensheng Yu, Michael K. C. Wong, Seong Heon Kim, Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, De-Yi Yang, Robert Feltz, Aneta Maria Kosinski, Guowei Zhou, Razia K. Rizvi, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristin E. Rosner, M. Arshad Siddiqui, Liping Yang
  • Patent number: 8513425
    Abstract: Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, Ar, R1, R2, Ra and Rb are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
    Type: Grant
    Filed: November 21, 2011
    Date of Patent: August 20, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Pravin Iyer, Clara Jeou Jen Lin, Stephen M. Lynch, Matthew C. Lucas, Ann Marie Madera, Kerem Erol Ozboya, Robert James Weikert, Ryan Craig Schoenfeld
  • Publication number: 20130096151
    Abstract: The present invention relates to the use of an anesthetic agent for killing clinically latent microorganisms associated with microbial infections and to novel combinations comprising an anesthetic agent and an antimicrobial agent for the treatment of microbial infections.
    Type: Application
    Filed: March 29, 2011
    Publication date: April 18, 2013
    Applicant: HELPERBY THERAPEUTICS LIMITED
    Inventors: Yanmin Hu, Anthony M.R. Coates
  • 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
  • Patent number: 8389730
    Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.
    Type: Grant
    Filed: May 25, 2011
    Date of Patent: March 5, 2013
    Assignee: Dendreon Corporation
    Inventors: Sateesh K. Natarajan, Ofir Moreno, Thomas J. Graddis, David F. Duncan, Reiner Laus, Feng Chen
  • Publication number: 20130023565
    Abstract: The present invention relates to polypeptide fragments comprising an amino-terminal fragment of the PA subunit of a viral RNA-dependent RNA polymerase possessing endonuclease activity, wherein said PA subunit is from Influenza A 2009 pan-demic H1N1 virus or is a variant thereof. This invention also relates to (i) crystals of the polypeptide fragments which are suitable for structure determination of said polypeptide fragments using X-ray crystallography and (ii) computational methods using the structural coordinates of said polypeptide to screen for and design compounds that modulate, preferably inhibit the endonucleolytically active site within the polypeptide fragment. In addition, this invention relates to methods identifying compounds that bind to the PA polypeptide fragments possessing endonuclease activity and preferably inhibit said endonucleolytic activity, preferably in a high throughput setting.
    Type: Application
    Filed: March 15, 2011
    Publication date: January 24, 2013
    Applicant: European Molecular Biology Laboratory
    Inventors: Stephen Cusack, Eva Kowalinski, Chloe Zubieta
  • Patent number: 8268828
    Abstract: This invention is directed to a 3-(amido or sulphamido)-4-(4-substituted-azinyl)benzamide or benzsulphonamide compound as defined herein. The 3-(amido or sulphamido)-(4-substituted-azinyl)benzamide or benzsulphonamide compound is useful as a inhibitor of the chemokine receptor CxCR3, and for preventing or treating a CxCR3 chemokine receptor mediated disease or condition related thereto in a patient in need of such.
    Type: Grant
    Filed: August 6, 2010
    Date of Patent: September 18, 2012
    Assignee: Sanofi
    Inventors: David Squire Thorpe, Martin Smrcina, Dagmar Dasha Cabel
  • Patent number: 8262945
    Abstract: Photochromic compositions are disclosed comprising a polymeric material, a photochromic dye, a hydroxyphenyl triazine UV absorber and, optionally, a further light stabilizer selected from the sterically hindered amines. These systems provide a reversible photochromic effect and show improved light stabilization and color fastness.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: September 11, 2012
    Assignee: BASF SE
    Inventors: Mara Destro, Dario Lazzari, Dirk Simon, Manuele Vitali
  • Patent number: 8258305
    Abstract: The invention provides a class of dopamine transporter inhibitors of formula (I) (DAT inhibitors), packaged pharmaceuticals comprising such inhibitors, and their uses in treating, or manufacturing medicaments for treating disease conditions including Parkinson's disease, when assessed by one or more of Hoehn and Yahr Staging of Parkinson's Disease, Unified Parkinson Disease Rating Scale (UPDRS), and Schwab and England Activities of Daily Living Scale. Related business methods such as marketing the inhibitors to healthcare providers are also provided.
    Type: Grant
    Filed: February 21, 2006
    Date of Patent: September 4, 2012
    Assignee: Prexa Pharmaceuticals, Inc.
    Inventor: James R. Hauske
  • Patent number: 8258304
    Abstract: N-aryl piperidine substituted biphenylcarboxamides compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.
    Type: Grant
    Filed: January 9, 2009
    Date of Patent: September 4, 2012
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx, Peter Walter Maria Roevens
  • Patent number: 8178559
    Abstract: 3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification.
    Type: Grant
    Filed: July 6, 2011
    Date of Patent: May 15, 2012
    Assignee: Novartis AG
    Inventors: Werner Breitenstein, Takeru Ehara, Claus Ehrhardt, Philipp Grosche, Yuko Hitomi, Yuki Iwaki, Takanori Kanazawa, Kazuhide Konishi, Juergen Klaus Maibaum, Keiichi Masuya, Atsuko Iwasaki, Nils Ostermann, Masaki Suzuki, Atsushi Toyao, Fumiaki Yokokawa
  • Patent number: 8153657
    Abstract: One aspect of the invention relates to piperidine compounds that are useful as inhibitors of monoamine transporters. The invention also relates to pharmaceutical compositions, comprising a piperidine compound of the invention. Another aspect of the present invention relates to the use of the aforementioned compounds in a method of treating a disorder of the central nervous system in a mammal.
    Type: Grant
    Filed: October 22, 2004
    Date of Patent: April 10, 2012
    Assignee: Georgetown University
    Inventors: Alan P. Kozikowski, Jia Zhou
  • Publication number: 20120053208
    Abstract: Curcumin analogues and methods of making and using the same are disclosed.
    Type: Application
    Filed: April 15, 2010
    Publication date: March 1, 2012
    Applicant: THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION
    Inventors: Pui-Kai Li, Chenglong Li, Jiayuh Lin, James R. Fuchs
  • Publication number: 20120046272
    Abstract: The present invention describes a series of therapeutically active compounds of formula I, X—Y—Z??(I) that are useful for treating a disorder in a mammal. In the formula I, X and Z, which may be same or different, are independently selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted heterocyclic group or substituted or unsubstituted heterocyclylalkyl; and Y is a linker selected from —O—, —S—, —NH—, —(CH2)n—, —CO—, —CONRa—, —NRaCO—, —NRaCOO—, —COO—, —CONRaCO—, —CONRaCOO— and —COOCOO—.
    Type: Application
    Filed: August 19, 2011
    Publication date: February 23, 2012
    Applicant: GRUNENTHAL GMBH
    Inventor: Ramesh SESHA
  • Publication number: 20120040964
    Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
    Type: Application
    Filed: October 24, 2011
    Publication date: February 16, 2012
    Applicant: INCYTE CORPORATION
    Inventors: Wenqing Yao, Meizhong Xu, Colin Zhang, Yanlong Li, Jincong Zhuo, Brian W. Metcalf
  • Publication number: 20120029022
    Abstract: The present invention relates to compounds that exhibit vasodilatory and anti-inflammatory effects by inhibiting the activity of soluble epoxide hydrolase (sEH). The present invention is also directed to methods of identifying such compounds, and use of such compounds for the treatment of diseases related to dysfunction of vasodilation, inflammation, and/or endothelial cells. In particular non-limiting embodiments, components of the invention may be used to treat hypertension.
    Type: Application
    Filed: July 7, 2011
    Publication date: February 2, 2012
    Applicant: The Trustees Of Columbia Univesity In The City Of New York
    Inventors: Donald W. Landry, Yuli Xie, Yidong Liu, Gangli Gong, Shi-Xian Deng, Kirsten Alison Rinderspacher
  • Publication number: 20120020881
    Abstract: This invention relates to novel compounds suitable for labeling by positron emitting isotopes, such as 18F, 11C, 13N and 15O, through appropriate labeling reagents, such as 18F reagents and methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).
    Type: Application
    Filed: December 4, 2009
    Publication date: January 26, 2012
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Lutz Lehmann, Timo Stellfeld, Keith Graham, Jessica Becaud, Linjing Mu
  • Patent number: 8097637
    Abstract: The present invention relates to compounds of formula (I) wherein R1 and A are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use as medicaments. Compounds of general formula (I) have high affinity for the dopamine D3 and serotonin (5-Hydroxytryptamine; 5-HT) 5-HT2A receptors and are effective in the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.
    Type: Grant
    Filed: August 1, 2008
    Date of Patent: January 17, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luca Gobbi, Georg Jaeschke, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
  • Patent number: 8080541
    Abstract: The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.
    Type: Grant
    Filed: August 19, 2010
    Date of Patent: December 20, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Patent number: 8076359
    Abstract: The present invention relates to disubstituted piperidinyl renin inhibitor compounds having the structure (Formula I) and their use in treating cardiovascular events and renal insufficiency.
    Type: Grant
    Filed: November 14, 2007
    Date of Patent: December 13, 2011
    Assignee: Merck Canada Inc.
    Inventors: Daniel Dube, Michel Gallant, Erich L. Grimm, Helene Juteau, Sebastien Laliberte, Tom Yao-Hsiang Wu
  • Publication number: 20110301031
    Abstract: A compound of the formula (I), wherein the substituents are as defined in claim 1, are useful as a pesticides.
    Type: Application
    Filed: December 9, 2009
    Publication date: December 8, 2011
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Michel Muehlebach, Thomas Pitterna, Jérôme Yves Cassayre, Andrew Edmunds, Camilla Corsi, Myriem El Qacemi, Roger Graham Hall, André Jeanguenat, André Stoller, Christopher Richard Ayles Godfrey, Jürgen Harry Schaetzer, Olivier Loiseleur, Peter Maienfisch, Neil Brian Carter
  • 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
  • Publication number: 20110275639
    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: March 25, 2011
    Publication date: November 10, 2011
    Applicant: ChemoCentryx, Inc.
    Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay P. Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
  • Publication number: 20110263560
    Abstract: 3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification.
    Type: Application
    Filed: July 6, 2011
    Publication date: October 27, 2011
    Applicant: NOVARTIS AG
    Inventors: Werner BREITENSTEIN, Takeru EHARA, Claus EHRHARDT, Philipp GROSCHE, Yuko HITOMI, Yuki IWAKI, Takanori KANAZAWA, Kazuhide KONISHI, Juergen Klaus MAIBAUM, Keiichi MASUYA, Atsuko Nihonyanagi, Nils OSTERMANN, Masaki SUZUKI, Atsushi TOYAO, Fumiaki YOKOKAWA
  • Patent number: 8039490
    Abstract: The present invention relates to compounds of the general formula as dual modulators of the 5-HT2a and D3 receptors useful against CNS disorders, wherein A, R1, R2, n, p, q and r are as defined in the specification.
    Type: Grant
    Filed: February 13, 2007
    Date of Patent: October 18, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luca Gobbi, Georg Jaeschke, Thomas Luebbers, Olivier Roche, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
  • Publication number: 20110201581
    Abstract: The present invention provides compounds of formula (I) in which n, y, X1, X2, A, B, R1, R2, R3, R4 and R5 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: February 11, 2011
    Publication date: August 18, 2011
    Inventors: Mark Furber, Christopher Andrew Luckhurst, Hitesh Jayantilal Sanganee, Linda Anne Stein, Peter Alan Cage
  • Publication number: 20110144107
    Abstract: The invention provides a class of compounds of formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria.
    Type: Application
    Filed: June 11, 2009
    Publication date: June 16, 2011
    Applicants: IRM LLC, DANA-FARBER CANCER INSTITUTE INC.
    Inventors: Arnab K. Chatterjee, Advait Nagle, Tao Wu, Nathanael S. Gray
  • Patent number: 7939552
    Abstract: Disclosed is a novel benzyloxypropylamine derivative having an excellent tachykinin receptor antagonistic effect. This compound shows a good transfer into the blood and a long blood half-life in the blood kinetic test using a guinea pig orally administered with the compound and is stable in an animal plasma. The compound also shows a high transfer to the central nervous system when it is orally administered to a guinea pig at a certain dose. Accordingly, the benzyloxypropylamine derivative is quite useful as a novel anti-tachykinin agent.
    Type: Grant
    Filed: March 29, 2006
    Date of Patent: May 10, 2011
    Assignee: Nippon Zoki Pharmaceutical Co., Ltd.
    Inventors: Kunihiko Higashiura, Takashi Ogino, Kazuhito Furukawa
  • Publication number: 20110086818
    Abstract: The invention features methods, compositions, and kits for selective inhibition of pain-and itch sensing neurons (nociceptors and pruriceptors) by drug molecules of small molecule weight, while minimizing effects on non-pain-sensing neurons or other types of cells.
    Type: Application
    Filed: March 11, 2009
    Publication date: April 14, 2011
    Applicants: Presidents and Fellows of Harvard College, The General Hospital Corporation
    Inventors: Bruce P. Bean, Clifford J. Woolf
  • Publication number: 20110065707
    Abstract: The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts thereof, wherein A1, A2, R1, R2, R3, R4, R5 and R6 have the significance given herein.
    Type: Application
    Filed: September 3, 2010
    Publication date: March 17, 2011
    Inventors: Jean Ackermann, Aurelia Conte, Werner Neidhart, Matthias Nettekoven, Stanley Wertheimer
  • Publication number: 20110053985
    Abstract: This invention relates to novel piperidine-4-carboxylic acid phenyl-alkyl-amide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Application
    Filed: January 14, 2009
    Publication date: March 3, 2011
    Applicant: NEUROSEARCH A/S
    Inventors: Dan Peters, John Paul Redrobe, Elsebet Ostergaard
  • Publication number: 20110053904
    Abstract: The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.
    Type: Application
    Filed: August 19, 2010
    Publication date: March 3, 2011
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Patent number: 7893261
    Abstract: A serotonin reuptake inhibitor which can be used in the treatment of depression and which has a decreased occurrence of unwanted side effects. The serotonin reuptake inhibitors are bi-functional organic molecules which combine serotonin transporter reuptake inhibition with serotonin (5-HT, such as 5-HT2A) receptor antagonism in one molecular entity. The serotonin-selective reuptake inhibitor (SSRI) homologue portion of the molecule shows an affinity to the serotonin reuptake transporter (SERT) and has antidepressant properties. The piperazine or piperidine portion of the molecule demonstrates an affinity to 5-HT receptors and restores the undesired side effects of SSRIs.
    Type: Grant
    Filed: March 28, 2005
    Date of Patent: February 22, 2011
    Assignee: Baylor University
    Inventors: Kevin G. Pinney, Maria Graciela Miranda, James Michael Dorsey
  • Patent number: RE43390
    Abstract: The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.
    Type: Grant
    Filed: October 27, 1998
    Date of Patent: May 15, 2012
    Assignees: GlaxoSmithKline LLC, SmithKline Beecham Limited
    Inventors: Valerie Joan Berry, Steven Dabbs, Colin Henry Frydrych, Eric Hunt, Francis Dominic Sanderson, Gary Woodnutt