Having -c(=x)-, Wherein X Is Chalcogen, Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/494)
  • Patent number: 9259412
    Abstract: The present invention relates to modafinil or derivatives thereof as a medicine for the treatment of vascular diseases or KCa3.1 channel (Ca activated K channel) mediated diseases and a novel use of the same. More specifically, the present invention relates to a pharmaceutical composition for the prevention or treatment of vascular diseases or KCa3.1 channel-mediated diseases comprising modafinil or a derivative of modafinil, or pharmaceutically acceptable salts thereof which relax blood vessels and inhibit KCa3.1 channel currents by increasing intracellular cAMP, a method for treating vascular diseases or KCa3.1 channel-mediated diseases using the composition and a health functional food composition for the prevention or improvement of vascular diseases or the KCa3.1 channel-mediated diseases comprising modafinil or a modafinil derivative compound, or sitologically acceptable salts thereof.
    Type: Grant
    Filed: October 24, 2012
    Date of Patent: February 16, 2016
    Assignee: EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATION
    Inventors: Suk Hyo Suh, Jae Chul Jung, Sei Kwan Oh
  • Publication number: 20140296254
    Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are described that correspond to general formula (I). Also described, are pharmaceutical compositions that include these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated diseases.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 2, 2014
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Branislav Musicki, Jerôme Aubert, Jean-Guy Boiteaux, Laurence Clary, Patricia Rossio, Marlène Schuppli-Nollet
  • Patent number: 8835491
    Abstract: Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.
    Type: Grant
    Filed: August 19, 2013
    Date of Patent: September 16, 2014
    Assignee: Arizona Board of Regents on Behalf of the University of Arizona
    Inventors: Gary A Flynn, Andrea J Yool, Elton Rodrigues Migliati, Leslie S Ritter
  • Publication number: 20140155357
    Abstract: The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds such as blocking tetracycline efflux and modulation of gene expression.
    Type: Application
    Filed: June 14, 2013
    Publication date: June 5, 2014
    Inventors: Paul Abato, Haregewein Assefa, Joel Berniac, Beena Bhatia, Todd Bowser, Jackson Chen, Mark Grier, Laura Honeyman, Mohamed Y. Ismail, Mark L. Nelson, Kwasi Ohemeng, Jingwen Pan
  • Publication number: 20140094455
    Abstract: Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.
    Type: Application
    Filed: August 19, 2013
    Publication date: April 3, 2014
    Applicant: ARIZONA BOARD OF REAGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA
    Inventors: Gary A. Flynn, Andrea J. Yool, Elton Rodrigues Migliati, Leslie S. Ritter
  • Patent number: 8685947
    Abstract: Diuretic bioactivity profiles of phase inversion micronized furosemide and furosemide co-precipitated with Eudragit L100, and mixtures of those formulations with stock furosemide, reduced or eliminated the rapid spike in diuresis associated with immediate release formulations and maintained cumulative urine output. Of the formulations tested, each of a mixture of micronized furosemide with stock furosemide, and Eudragit L100 polymer with stock furosemide demonstrated optimal diuretic bioactivity profiles in subjects.
    Type: Grant
    Filed: August 25, 2011
    Date of Patent: April 1, 2014
    Assignee: Brown University
    Inventors: Edith Mathiowitz, Bryan Laulicht
  • Patent number: 8519168
    Abstract: This application discloses a novel process for the preparation of 1,2-substituted 3,4-dioxo-1-cyclobutene compounds, which have utility, for example, in the treatment of CXC chemokine-mediated diseases, and intermediates useful in the synthesis thereof.
    Type: Grant
    Filed: July 1, 2008
    Date of Patent: August 27, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Xiaoyong Fu, Frank Bruno Guenter, Agnes S. Kim-Meade, Kenneth Stanley Matthews, Mathew Thomas Maust, Gerald Werne, Jason L. Winters, Jianguo Yin, Shuyi Zhang, David J. Moloznik
  • Publication number: 20130217889
    Abstract: Compounds of formula (I): wherein R1 to R8, and X? are defined herein. Also disclosed are methods of making and using these compounds.
    Type: Application
    Filed: October 27, 2011
    Publication date: August 22, 2013
    Applicant: National University of Singapore
    Inventors: Choon Hong Tan, Kuo Wei Huang, Ting Ma, Xiao Fu
  • Publication number: 20130183252
    Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.
    Type: Application
    Filed: February 10, 2012
    Publication date: July 18, 2013
    Applicant: Senomyx, Inc.
    Inventors: Xiaodong LI, Andrew Patron, Catherine Tachdjian, Hong Xu, Qing Li, Alexey Pronin, Guy Servant, Lan Zhang, Thomas Brady, Vincent Darmohusodo, Melissa Arellano, Victor Selchau, Brett Weylan Ching, Donald S. Karanewsky, Paul Brust, Jing Ling, Wen Zhao, Chad Priest
  • Publication number: 20130072677
    Abstract: Provided is a novel compound which is useful as a pharmaceutical composition by inhibiting an LpxC activity, thereby exhibiting potent antimicrobial activity against gram-negative bacteria including Pseudomonas aeruginosa and its drug resistant bacteria.
    Type: Application
    Filed: April 20, 2011
    Publication date: March 21, 2013
    Applicants: TOYAMA CHEMICAL CO., LTD., TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Hajime Takashima, Risa Tsuruta, Tetsuya Yabuuchi, Yusuke Oka, Hiroki Urabe, Yoichiro Suga, Masato Takahashi, Fumito Uneuchi, Hironori Kotsubo, Muneo Shoji, Yasuko Kawaguchi
  • Publication number: 20130005735
    Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Application
    Filed: September 12, 2012
    Publication date: January 3, 2013
    Inventors: Urs Baettig, Anne-Marie D'souza, Peter Hunt, Neil John Press, Simon James Watson
  • Publication number: 20120271049
    Abstract: A process for preparing phenyl iso(thio)cyanates of the formula I in which a compound of the formula II or its HCl adduct is reacted with a phosgenating agent where W is oxygen or sulfur and Ar and A are as defined in claim 1 is described. Moreover, the invention relates to the use of the phenyl iso(thio)cyanates for preparing crop protection agents.
    Type: Application
    Filed: June 28, 2012
    Publication date: October 25, 2012
    Applicant: BASF AKTIENGESELLSCHAFT
    Inventors: Gerhard Hamprecht, Michael Puhl, Bernd Wolf, Norbert Götz, Michael Keil, Robert Reinhard, Ingo Sagasser, Werner Seitz
  • Patent number: 8283376
    Abstract: The invention relates to the use of substituted 2-aminotetralins of general formula (I) as a medicament for the preventive treatment of Parkinson's disease.
    Type: Grant
    Filed: December 23, 2004
    Date of Patent: October 9, 2012
    Assignee: UCB Pharma GmbH
    Inventors: Dieter Scheller, Frank Dressen
  • Publication number: 20120234721
    Abstract: The present invention provides compounds that are effective in treating central nervous system disorders and maintaining normal brain function. Methods of making and using the compounds are also provided.
    Type: Application
    Filed: September 9, 2011
    Publication date: September 20, 2012
    Applicant: Neurotherapeutics Pharma, Inc.
    Inventors: Daryl W. HOCHMAN, John J. Partridge
  • Publication number: 20120208876
    Abstract: The invention relates to compounds, to compositions comprising the same and uses thereof for the prevention or treatment of pain, e.g neuropathic pain while having neutral or beneficial effect on metabolic parameters.
    Type: Application
    Filed: November 4, 2011
    Publication date: August 16, 2012
    Inventors: Xianqi KONG, Nigel LEVENS, Serge LAMOTHE, Mohamed ATFANI, Stephane CIBLAT, Lucie JETTE
  • Publication number: 20120196819
    Abstract: Compositions and methods for the treatment and control of various conditions in an animal which comprises administering to said animal an effective amount of a immediate release composition of about 0.5% to 50% wt/wt of active ingredient together with excipients to a total of about 100%, wherein said compositon dissolves in a relatively short period of time, e.g., 75 seconds or less, 5 seconds or less, or 3 seconds or less, upon administration to said animal.
    Type: Application
    Filed: January 4, 2012
    Publication date: August 2, 2012
    Applicant: NEWMARKET PHARMACEUTICALS LLC
    Inventors: David ROCK, Mark RIDALL
  • Patent number: 8207221
    Abstract: The present invention relates to four distinct crystalline polymorphs of a monohydrate of Compound A having the following chemical structure: These four polymorphic forms, herein referred to as Forms I, II, III and IV are active as a CXC-chemokine receptor ligands. The invention is further directed to formulations, methods of treatment, and processes of synthesis of these polymorphic forms.
    Type: Grant
    Filed: July 16, 2008
    Date of Patent: June 26, 2012
    Assignee: Schering Corporation
    Inventors: Mengwei Hu, Younong Yu, Michael P. Dwyer, Arthur G. Taveras, Agnes Kim-Meade, Jianguo Yin, Xiaoyong Fu, Timothy L. McAllister, Shuyi Zhang, Kevin Klopfer
  • Publication number: 20120135968
    Abstract: The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.
    Type: Application
    Filed: May 7, 2010
    Publication date: May 31, 2012
    Inventors: Chi-Li Chen, Roger B. Clark, Yonghong Deng, Minsheng He, Louis Plamondon, Cuixiang Sun, Xiao-Yi Xiao, Magnus Rönn
  • Publication number: 20120053156
    Abstract: Diuretic bioactivity profiles of phase inversion micronized furosemide and furosemide co-precipitated with Eudragit L100, and mixtures of those formulations with stock furosemide, reduced or eliminated the rapid spike in diuresis associated with immediate release formulations and maintained cumulative urine output. Of the formulations tested, each of a mixture of micronized furosemide with stock furosemide, and Eudragit L100 polymer with stock furosemide demonstrated optimal diuretic bioactivity profiles in subjects.
    Type: Application
    Filed: August 25, 2011
    Publication date: March 1, 2012
    Applicant: BROWN UNIVERSITY
    Inventors: Edith Mathiowitz, Bryan Laulicht
  • Publication number: 20120022039
    Abstract: The invention relates to substituted indanes and derivatives thereof, to physiologically acceptable salts and physiologically functional derivatives thereof, to the production thereof, to drugs containing at least one substituted indane according to the invention or derivative thereof, and to the use of the substituted indanes according to the invention and to derivatives thereof as MCH antagonists.
    Type: Application
    Filed: February 12, 2010
    Publication date: January 26, 2012
    Applicant: SANOFI
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Klaus Wirth
  • Patent number: 8063046
    Abstract: Compounds having high angiogenesis inhibiting activity useful as agents for effective treatment and prevention of diseases involving pathologic angiogenesis, e.g.
    Type: Grant
    Filed: March 23, 2010
    Date of Patent: November 22, 2011
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Hiroshi Koyano, Atsushi Suda, Kousuke Aso, Kihito Hada, Miyuki Asai, Masami Hasegawa, Yasuko Sato
  • Publication number: 20110275635
    Abstract: Small molecule inhibitors of bacterial nicotinamide adenine dinucleotide synthetase (NADs), bacterial nicotinic acid mononucleotide adenylyltransferase (NaMNAT), and human nicotinamide mononucleotide adenylyltransferase (NMNAT) are provided, as well as methods of making and using the inhibitors.
    Type: Application
    Filed: January 8, 2010
    Publication date: November 10, 2011
    Applicant: THE UAB RESEARCH FOUNDATION
    Inventors: Wayne J. Brouillette, Christie G. Brouillette, Whitney B. Moro
  • Publication number: 20110251206
    Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Application
    Filed: June 21, 2011
    Publication date: October 13, 2011
    Inventors: Urs Baettig, Anne-Marie D'Souza, Peter Hunt, Neil John Press, Simon James Watson
  • Publication number: 20110212943
    Abstract: Provided herein are novel bridged cyclic derivatives of the general formula (I), their analogs, tautomeric forms, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds can inhibit HDACs and are useful as therapeutic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, autoimmune diseases, skin diseases, infections, inflammation, neurode-generative disorders etc.
    Type: Application
    Filed: October 14, 2009
    Publication date: September 1, 2011
    Applicant: ORCHID RESEARCH LABORATORIES LIMITED
    Inventors: Gopalan Balasubramanian, Ponpandian Thanasekaran, Sridharan Rajagopal, Bharathimohan Kuppusamy, Virendra Kachhadia, Vignesh Radhakrishnan, Sivasudar Velaiah, Shridhar Narayanan, Mandar Bhonde, Praveen Rajendran, Sriram Rajagopal
  • Publication number: 20110160469
    Abstract: This application discloses a novel process for the preparation of 1,2-substituted 3,4-dioxo-1-cyclobutene compounds, which have utility, for example, in the treatment of CXC chemokine-mediated diseases, and intermediates useful in the synthesis thereof.
    Type: Application
    Filed: July 1, 2008
    Publication date: June 30, 2011
    Inventor: Xiaoyong Fu
  • Publication number: 20110054017
    Abstract: The present application relates to novel substituted furan derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases.
    Type: Application
    Filed: January 29, 2009
    Publication date: March 3, 2011
    Inventors: Thomas Lampe, Raimund Kast, Friederike Stoll, Joachim Schuhmacher
  • Publication number: 20110004007
    Abstract: A process is disclosed for the preparation of a compound of formula and/or an addition salt of a proton acid, wherein R1 and R2 independently represent alkyl, cycloalkyl, aryl or aralkyl, each aryl or aralkyl being optionally further substituted with alkyl, alkoxy and/or halogen. The process involves reacting a mixture comprising a methyl ketone of formula and a compound of formula H2N—R2 (V) and/or an addition salt of proton acid, and formaldehyde in the presence of a solvent selected from the group consisting of water, aliphatic alcohols, cycloaliphatic alcohols and mixtures thereof, and optionally a proton acid to afford a ?-amino ketone of formula and/or an addition salt of a proton acid, and reducing the carbonyl group of said ?-amino ketone to afford a compound of formula I, and/or an addition salt of a proton acid wherein the first step is carried out at a pressure above 1.5 bar.
    Type: Application
    Filed: August 25, 2010
    Publication date: January 6, 2011
    Applicant: LONZA AG
    Inventor: Dominique Michel
  • Publication number: 20100311727
    Abstract: Therapeutic amine-arylsulfonamide conjugate compounds, of the general formula: wherein R? is [D-W-], hydroxyl, or alkoxyl; R? is independently [D-W?-], hydrogen, alkoxy, alkyl, cycloalkyl, alkenyl, alkynyl or aryl, or R? and R? together with the nitrogen atom to which they are attached form a 4-, 5-, 6-, 7- or 8-membered ring optionally containing one or two further heteroatoms independently selected from nitrogen, oxygen and sulfur; D is independently a therapeutic amine radical comprising at least one nitrogen atom and optionally at least one oxygen atom coupled to W or W? by a nitrogen or oxygen atom; W and W? are a chemical bond or linker; wherein either R? is [D-W-] or at least one R? is [D-W?-], and pharmaceutically acceptable esters, amides, salts or solvates thereof, pharmaceutical compositions containing same, methods for their preparation, and their use in treating psychiatric, neurologic and metabolic disorders are disclosed.
    Type: Application
    Filed: June 8, 2010
    Publication date: December 9, 2010
    Applicant: ALGEBRA, INC.
    Inventors: Philip F. MORGAN, James L. KELLEY
  • Publication number: 20100298559
    Abstract: There is provided a novel optically active dinickel complex and/or a production method of an optically active amine by an asymmetric Mannich reaction using the dinickel complex as a catalyst. An optically active dinickel complex of Formula (I) or Formula (I?): [where R0, R1, R2, R3, R4, R5, R6, and R7 are each independently a hydrogen atom, a halogen atom, a C1-10 alkyl group or a C1-10 alkoxy group, etc., R2 and R3 together form, together with a benzene ring bonded to them, a naphthalene ring, etc. A novel production method of an optically active amine by an asymmetric Mannich reaction using the dinickel complex as a catalyst.
    Type: Application
    Filed: December 10, 2008
    Publication date: November 25, 2010
    Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Masakatsu Shibasaki, Shigeki Matsunaga, Zhihua Chen
  • Publication number: 20100249439
    Abstract: This application discloses a novel process for the preparation of 2-Hydroxy-N,N-dimethyl-3-[[2-[[1(R)-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]benzamide, which has utility, for example, in the treatment of CXC chemokine-mediated diseases.
    Type: Application
    Filed: July 1, 2008
    Publication date: September 30, 2010
    Inventors: Vincenzo Liotta, Xu Yanke
  • Patent number: 7795315
    Abstract: The present invention provides novel compounds of the general formula (I) and pharmaceutically acceptable salts thereof, processes for the manufacture of these novel compounds and medicaments containing such compounds. The compounds of the present invention show anti-proliferative and differentiation-inducing activity, which results in inhibition of tumor cell proliferation, induction of apoptosis and inhibition of invasion. The invention also covers the use of such compounds for the treatment of diseases such as cancer and for the manufacture of corresponding medicaments.
    Type: Grant
    Filed: January 23, 2009
    Date of Patent: September 14, 2010
    Assignee: Hoffman-La Roche Inc.
    Inventors: Li Chen, Yun He, Jason Christopher Wong
  • Patent number: 7763612
    Abstract: Therapeutic amine-arylsulfonamide conjugate compounds, of the general formula: wherein R? is [D-W-], hydroxyl, or alkoxyl; R? is independently [D-W?-], hydrogen, alkoxy, alkyl, cycloalkyl, alkenyl, alkynyl or aryl, or R? and R? together with the nitrogen atom to which they are attached form a 4-, 5-, 6-, 7- or 8-membered ring optionally containing one or two further heteroatoms independently selected from nitrogen, oxygen and sulfur; D is independently a therapeutic amine radical comprising at least one nitrogen atom and optionally at least one oxygen atom coupled to W or W? by a nitrogen or oxygen atom; W and W? are a chemical bond or linker; wherein either R? is [D-W-] or at least one R? is [D-W?-], and pharmaceutically acceptable esters, amides, salts or solvates thereof, pharmaceutical compositions containing same, methods for their preparation, and their use in treating psychiatric, neurologic and metabolic disorders are disclosed.
    Type: Grant
    Filed: January 3, 2007
    Date of Patent: July 27, 2010
    Assignee: Algebra, Inc.
    Inventors: Philip F. Morgan, James L. Kelley
  • Publication number: 20100179326
    Abstract: Compounds having high angiogenesis inhibiting activity useful as agents for effective treatment and prevention of diseases involving pathologic angiogenesis, e.g.
    Type: Application
    Filed: March 23, 2010
    Publication date: July 15, 2010
    Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHA
    Inventors: Hiroshi KOYANO, Atsushi Suda, Kousuke Aso, Kihito Hada, Miyuki Asai, Masami Hasegawa, Yasuko Sato
  • Patent number: 7737288
    Abstract: Non-steroidal androgen receptor modulating compounds of the general formula (I), their pharmaceutically acceptable salts, preparation process and pharmaceutically compositions containing the said compounds are disclosed. Such compounds of the general formula (I) or their pharmaceutically acceptable salts can be used for preparing non-steroidal medicines to treat and/or prevent conditions or diseases such as prostatic hyperplasia, prostate cancer, hirsutism, severe hormone-dependent alopecia or acne, etc. as a result of androgen receptor antagonistic activities.
    Type: Grant
    Filed: May 26, 2006
    Date of Patent: June 15, 2010
    Assignees: Shanghai Institute of Materia Medica Chinese Academy of Sciences, Sichuan University
    Inventors: Mingwei Wang, Caihong Zhou, Xin Hui, Haoran Su, Jie Gao, Yong Deng, Dacheng Yang
  • Publication number: 20100125071
    Abstract: The present invention relates to compounds of formula (I) with the substituents as defined herein, and uses thereof.
    Type: Application
    Filed: June 4, 2008
    Publication date: May 20, 2010
    Inventors: Neil John Press, Simon James Watson
  • Patent number: 7528157
    Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.
    Type: Grant
    Filed: December 22, 2006
    Date of Patent: May 5, 2009
    Assignee: Asterand UK Limited
    Inventors: Alexander W. Oxford, Richard J. Davis, Robert A. Coleman, Kenneth L. Clark, David E. Clark, Neil V. Harris, Garry Fenton, George Hynd, Keith A. J. Stuttle, Jonathan M. Sutton, Christopher G. Newton
  • Patent number: 7495023
    Abstract: The present invention relates to thio semicarbazone and semicarbazone inhibitors of cysteine proteases and methods of using such compounds to prevent and treat protozoan infections such as trypanosomiasis, malaria and leishmaniasis. The compounds also find use in inhibiting cysteine proteases associated with carcinogenesis, including cathepsins B and L.
    Type: Grant
    Filed: March 18, 2005
    Date of Patent: February 24, 2009
    Assignee: The Regents of the University of California
    Inventors: Fred E. Cohen, Xiaohui Du, Chun Guo, James H. McKerrow
  • Publication number: 20080319057
    Abstract: 2-Phenylethylamino substituted carboxamide derivatives of formula (I); wherein J, W, R0, R1, R2, R3, and R4 have the meanings as defined in the specification and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and their use as sodium and/or calcium channel modulators useful in preventing alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urology, and gastrointestinal diseases where the above mechanisms have been described as playing a pathological role, are described.
    Type: Application
    Filed: November 29, 2006
    Publication date: December 25, 2008
    Inventors: Florian Thaler, Mauro Napoletano, Cibele Sabido-David, Ermanno Moriggi, Carla Caccia, Laura Faravelli, Alessandra Restivo, Patricia Salvati
  • Publication number: 20080293808
    Abstract: Non-steroidal androgen receptor modulating compounds of the general formula (I), their pharmaceutically acceptable salts, preparation process and pharmaceutically compositions containing the said compounds are disclosed. Such compounds of the general formula (I) or their pharmaceutically acceptable salts can be used for preparing non-steroidal medicines to treat and/or prevent conditions or diseases such as prostatic hyperplasia, prostate cancer, hirsutism, severe hormone-dependent alopecia or acne, etc. as a result of androgen receptor antagonistic activities.
    Type: Application
    Filed: May 26, 2006
    Publication date: November 27, 2008
    Inventors: Mingwei Wang, Caihong Zhou, Xin Hui, Haoran Su, Jie Gao, Yong Deng, Dacheng Yang
  • Publication number: 20080287442
    Abstract: 14-O—[(((C1-6)Alkoxy-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O—[(((C1-6)Mono- or dialkylamino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Hydroxy-(C1-8)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Formyl-(C0-5)-alkyl)-phenylsulfanyl)-acetyl]-mutilins 14-O-[((Guanidino-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Ureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Thioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Isothioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins and their use as pharmaceuticals.
    Type: Application
    Filed: January 11, 2007
    Publication date: November 20, 2008
    Applicant: Nabriva Therapeutics Forschungs GmbH
    Inventors: Klaus Thirring, Gerd Ascher, Susanne Paukner, Werner Heilmayer, Rodger Novak
  • Publication number: 20080279822
    Abstract: The present invention relates to four distinct crystalline polymorphs of a monohydrate of Compound A having the following chemical structure: Compound A. These four polymorphic forms, herein referred to as Forms I, II III and IV are active as a CXC-chemokine receptor ligands. The invention is further directed to formulations, methods of treatment, and processes of synthesis of these polymorphic forms.
    Type: Application
    Filed: July 16, 2008
    Publication date: November 13, 2008
    Inventors: Mengwei Hu, Younong Yu, Michael Dwyer, Arthur Taveras, Agnes Kim-Meade, Jianguo Yin, Xiaoyong Fu, Timothy McAllister, Shuyi Zhang, Kevin Klopfer
  • Patent number: 7259166
    Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a polar ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.
    Type: Grant
    Filed: April 10, 2006
    Date of Patent: August 21, 2007
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Wendy Lea Corbett, Joseph Samuel Grimsby, Nancy-Ellen Haynes, Robert Francis Kester, Paige Erin Mahaney, Jagdish Kumar Racha, Ramakanth Sarabu, Ka Wang
  • Patent number: 7132445
    Abstract: There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
    Type: Grant
    Filed: July 30, 2003
    Date of Patent: November 7, 2006
    Assignees: Schering Corporation, Pharmacopeia Drug Discovery, Inc.
    Inventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jianhua Chao, Younong Yu, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Purakkattle J. Biju, Kingsley H. Nelson, Jr., Laura L. Rokosz, James P. Jakway, Gaifa Lai, Minglang Wu, Evan A. Hecker, Daniel Lundell, Jay S. Fine
  • Patent number: 7071342
    Abstract: Disclosed is a process for making the compound of formula I: using the compounds of formulas II, Q, and XI or XII: wherein A is selected from the group consisting of Br, Cl and I (with Br being preferred); and R represents (C1–C10)alkyl. Also disclosed are intermediate compounds that are made in the disclosed process.
    Type: Grant
    Filed: April 16, 2004
    Date of Patent: July 4, 2006
    Assignee: Schering Corporation
    Inventors: Jianguo Yin, Xiaoyong Fu, Shuyi Zhang, Timothy L. McAllister, Agnes S. Kim-Meade, Jason L. Winters, Anantha Sudhakar, Doris P. Schumacher
  • Patent number: 7049308
    Abstract: A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. In another embodiment, a biocompatible polymer incorporates a C-nitroso moiety.
    Type: Grant
    Filed: September 27, 2001
    Date of Patent: May 23, 2006
    Assignee: Duke University
    Inventors: Jonathan S. Stamler, Eric J. Toone
  • Patent number: 7030239
    Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) useful in treating Alzheimer's disease and other similar diseases.
    Type: Grant
    Filed: May 18, 2004
    Date of Patent: April 18, 2006
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Roy Hom, Shumeye S. Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Y. Fang
  • Publication number: 20040110768
    Abstract: Bombesin receptor antagonists are provided which are compounds of formula (I) or pharmaceutically acceptable salts thereof: 1
    Type: Application
    Filed: December 4, 2003
    Publication date: June 10, 2004
    Inventors: Michael Higginbottom, Martyn Clive Pritchard, Herman Thijs Stock
  • Patent number: 6743564
    Abstract: Amine compounds having a cyano group are useful in resist compositions for preventing a resist film from thinning and also for enhancing the resolution and focus margin of resist.
    Type: Grant
    Filed: December 6, 2001
    Date of Patent: June 1, 2004
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Jun Hatakeyama, Tomohiro Kobayashi, Takeru Watanabe
  • Patent number: 6710071
    Abstract: This invention relates to a series of difluoromethylene aromatic ethers of the formula wherein ring A and X and Y are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.
    Type: Grant
    Filed: August 15, 2002
    Date of Patent: March 23, 2004
    Assignee: Pfizer Inc
    Inventor: John Adams Lowe, III
  • Patent number: 6710190
    Abstract: The invention is a novel series of compounds which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.
    Type: Grant
    Filed: November 21, 2001
    Date of Patent: March 23, 2004
    Assignee: Warner-Lambert Company
    Inventor: Po-Wai Yuen