Having -c(=x)-, Wherein X Is Chalcogen, Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/494)
-
Patent number: 9259412Abstract: 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: GrantFiled: October 24, 2012Date of Patent: February 16, 2016Assignee: EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATIONInventors: Suk Hyo Suh, Jae Chul Jung, Sei Kwan Oh
-
Publication number: 20140296254Abstract: 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: ApplicationFiled: October 26, 2012Publication date: October 2, 2014Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Branislav Musicki, Jerôme Aubert, Jean-Guy Boiteaux, Laurence Clary, Patricia Rossio, Marlène Schuppli-Nollet
-
Patent number: 8835491Abstract: 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: GrantFiled: August 19, 2013Date of Patent: September 16, 2014Assignee: Arizona Board of Regents on Behalf of the University of ArizonaInventors: Gary A Flynn, Andrea J Yool, Elton Rodrigues Migliati, Leslie S Ritter
-
Publication number: 20140155357Abstract: 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: ApplicationFiled: June 14, 2013Publication date: June 5, 2014Inventors: 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: 20140094455Abstract: 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: ApplicationFiled: August 19, 2013Publication date: April 3, 2014Applicant: ARIZONA BOARD OF REAGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONAInventors: Gary A. Flynn, Andrea J. Yool, Elton Rodrigues Migliati, Leslie S. Ritter
-
Patent number: 8685947Abstract: 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: GrantFiled: August 25, 2011Date of Patent: April 1, 2014Assignee: Brown UniversityInventors: Edith Mathiowitz, Bryan Laulicht
-
Patent number: 8519168Abstract: 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: GrantFiled: July 1, 2008Date of Patent: August 27, 2013Assignee: 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: 20130217889Abstract: Compounds of formula (I): wherein R1 to R8, and X? are defined herein. Also disclosed are methods of making and using these compounds.Type: ApplicationFiled: October 27, 2011Publication date: August 22, 2013Applicant: National University of SingaporeInventors: Choon Hong Tan, Kuo Wei Huang, Ting Ma, Xiao Fu
-
Publication number: 20130183252Abstract: 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: ApplicationFiled: February 10, 2012Publication date: July 18, 2013Applicant: 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: 20130072677Abstract: 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: ApplicationFiled: April 20, 2011Publication date: March 21, 2013Applicants: TOYAMA CHEMICAL CO., LTD., TAISHO PHARMACEUTICAL CO., LTDInventors: Hajime Takashima, Risa Tsuruta, Tetsuya Yabuuchi, Yusuke Oka, Hiroki Urabe, Yoichiro Suga, Masato Takahashi, Fumito Uneuchi, Hironori Kotsubo, Muneo Shoji, Yasuko Kawaguchi
-
Publication number: 20130005735Abstract: 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: ApplicationFiled: September 12, 2012Publication date: January 3, 2013Inventors: Urs Baettig, Anne-Marie D'souza, Peter Hunt, Neil John Press, Simon James Watson
-
Publication number: 20120271049Abstract: 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: ApplicationFiled: June 28, 2012Publication date: October 25, 2012Applicant: BASF AKTIENGESELLSCHAFTInventors: Gerhard Hamprecht, Michael Puhl, Bernd Wolf, Norbert Götz, Michael Keil, Robert Reinhard, Ingo Sagasser, Werner Seitz
-
Patent number: 8283376Abstract: 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: GrantFiled: December 23, 2004Date of Patent: October 9, 2012Assignee: UCB Pharma GmbHInventors: Dieter Scheller, Frank Dressen
-
Publication number: 20120234721Abstract: 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: ApplicationFiled: September 9, 2011Publication date: September 20, 2012Applicant: Neurotherapeutics Pharma, Inc.Inventors: Daryl W. HOCHMAN, John J. Partridge
-
Publication number: 20120208876Abstract: 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: ApplicationFiled: November 4, 2011Publication date: August 16, 2012Inventors: Xianqi KONG, Nigel LEVENS, Serge LAMOTHE, Mohamed ATFANI, Stephane CIBLAT, Lucie JETTE
-
Publication number: 20120196819Abstract: 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: ApplicationFiled: January 4, 2012Publication date: August 2, 2012Applicant: NEWMARKET PHARMACEUTICALS LLCInventors: David ROCK, Mark RIDALL
-
Patent number: 8207221Abstract: 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: GrantFiled: July 16, 2008Date of Patent: June 26, 2012Assignee: Schering CorporationInventors: 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: 20120135968Abstract: 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: ApplicationFiled: May 7, 2010Publication date: May 31, 2012Inventors: Chi-Li Chen, Roger B. Clark, Yonghong Deng, Minsheng He, Louis Plamondon, Cuixiang Sun, Xiao-Yi Xiao, Magnus Rönn
-
Publication number: 20120053156Abstract: 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: ApplicationFiled: August 25, 2011Publication date: March 1, 2012Applicant: BROWN UNIVERSITYInventors: Edith Mathiowitz, Bryan Laulicht
-
Publication number: 20120022039Abstract: 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: ApplicationFiled: February 12, 2010Publication date: January 26, 2012Applicant: SANOFIInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Klaus Wirth
-
Patent number: 8063046Abstract: Compounds having high angiogenesis inhibiting activity useful as agents for effective treatment and prevention of diseases involving pathologic angiogenesis, e.g.Type: GrantFiled: March 23, 2010Date of Patent: November 22, 2011Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Hiroshi Koyano, Atsushi Suda, Kousuke Aso, Kihito Hada, Miyuki Asai, Masami Hasegawa, Yasuko Sato
-
Publication number: 20110275635Abstract: 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: ApplicationFiled: January 8, 2010Publication date: November 10, 2011Applicant: THE UAB RESEARCH FOUNDATIONInventors: Wayne J. Brouillette, Christie G. Brouillette, Whitney B. Moro
-
Publication number: 20110251206Abstract: 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: ApplicationFiled: June 21, 2011Publication date: October 13, 2011Inventors: Urs Baettig, Anne-Marie D'Souza, Peter Hunt, Neil John Press, Simon James Watson
-
Publication number: 20110212943Abstract: 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: ApplicationFiled: October 14, 2009Publication date: September 1, 2011Applicant: ORCHID RESEARCH LABORATORIES LIMITEDInventors: Gopalan Balasubramanian, Ponpandian Thanasekaran, Sridharan Rajagopal, Bharathimohan Kuppusamy, Virendra Kachhadia, Vignesh Radhakrishnan, Sivasudar Velaiah, Shridhar Narayanan, Mandar Bhonde, Praveen Rajendran, Sriram Rajagopal
-
Publication number: 20110160469Abstract: 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: ApplicationFiled: July 1, 2008Publication date: June 30, 2011Inventor: Xiaoyong Fu
-
Publication number: 20110054017Abstract: 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: ApplicationFiled: January 29, 2009Publication date: March 3, 2011Inventors: Thomas Lampe, Raimund Kast, Friederike Stoll, Joachim Schuhmacher
-
Publication number: 20110004007Abstract: 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: ApplicationFiled: August 25, 2010Publication date: January 6, 2011Applicant: LONZA AGInventor: Dominique Michel
-
Publication number: 20100311727Abstract: 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: ApplicationFiled: June 8, 2010Publication date: December 9, 2010Applicant: ALGEBRA, INC.Inventors: Philip F. MORGAN, James L. KELLEY
-
Publication number: 20100298559Abstract: 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: ApplicationFiled: December 10, 2008Publication date: November 25, 2010Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Masakatsu Shibasaki, Shigeki Matsunaga, Zhihua Chen
-
Publication number: 20100249439Abstract: 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: ApplicationFiled: July 1, 2008Publication date: September 30, 2010Inventors: Vincenzo Liotta, Xu Yanke
-
Patent number: 7795315Abstract: 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: GrantFiled: January 23, 2009Date of Patent: September 14, 2010Assignee: Hoffman-La Roche Inc.Inventors: Li Chen, Yun He, Jason Christopher Wong
-
Patent number: 7763612Abstract: 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: GrantFiled: January 3, 2007Date of Patent: July 27, 2010Assignee: Algebra, Inc.Inventors: Philip F. Morgan, James L. Kelley
-
Publication number: 20100179326Abstract: Compounds having high angiogenesis inhibiting activity useful as agents for effective treatment and prevention of diseases involving pathologic angiogenesis, e.g.Type: ApplicationFiled: March 23, 2010Publication date: July 15, 2010Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Hiroshi KOYANO, Atsushi Suda, Kousuke Aso, Kihito Hada, Miyuki Asai, Masami Hasegawa, Yasuko Sato
-
Patent number: 7737288Abstract: 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: GrantFiled: May 26, 2006Date of Patent: June 15, 2010Assignees: Shanghai Institute of Materia Medica Chinese Academy of Sciences, Sichuan UniversityInventors: Mingwei Wang, Caihong Zhou, Xin Hui, Haoran Su, Jie Gao, Yong Deng, Dacheng Yang
-
Publication number: 20100125071Abstract: The present invention relates to compounds of formula (I) with the substituents as defined herein, and uses thereof.Type: ApplicationFiled: June 4, 2008Publication date: May 20, 2010Inventors: Neil John Press, Simon James Watson
-
Patent number: 7528157Abstract: 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: GrantFiled: December 22, 2006Date of Patent: May 5, 2009Assignee: Asterand UK LimitedInventors: 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: 7495023Abstract: 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: GrantFiled: March 18, 2005Date of Patent: February 24, 2009Assignee: The Regents of the University of CaliforniaInventors: Fred E. Cohen, Xiaohui Du, Chun Guo, James H. McKerrow
-
Publication number: 20080319057Abstract: 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: ApplicationFiled: November 29, 2006Publication date: December 25, 2008Inventors: Florian Thaler, Mauro Napoletano, Cibele Sabido-David, Ermanno Moriggi, Carla Caccia, Laura Faravelli, Alessandra Restivo, Patricia Salvati
-
Publication number: 20080293808Abstract: 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: ApplicationFiled: May 26, 2006Publication date: November 27, 2008Inventors: Mingwei Wang, Caihong Zhou, Xin Hui, Haoran Su, Jie Gao, Yong Deng, Dacheng Yang
-
Publication number: 20080287442Abstract: 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: ApplicationFiled: January 11, 2007Publication date: November 20, 2008Applicant: Nabriva Therapeutics Forschungs GmbHInventors: Klaus Thirring, Gerd Ascher, Susanne Paukner, Werner Heilmayer, Rodger Novak
-
Publication number: 20080279822Abstract: 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: ApplicationFiled: July 16, 2008Publication date: November 13, 2008Inventors: Mengwei Hu, Younong Yu, Michael Dwyer, Arthur Taveras, Agnes Kim-Meade, Jianguo Yin, Xiaoyong Fu, Timothy McAllister, Shuyi Zhang, Kevin Klopfer
-
Patent number: 7259166Abstract: 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: GrantFiled: April 10, 2006Date of Patent: August 21, 2007Assignee: 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: 7132445Abstract: 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: GrantFiled: July 30, 2003Date of Patent: November 7, 2006Assignees: 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: 7071342Abstract: 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: GrantFiled: April 16, 2004Date of Patent: July 4, 2006Assignee: Schering CorporationInventors: Jianguo Yin, Xiaoyong Fu, Shuyi Zhang, Timothy L. McAllister, Agnes S. Kim-Meade, Jason L. Winters, Anantha Sudhakar, Doris P. Schumacher
-
Patent number: 7049308Abstract: 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: GrantFiled: September 27, 2001Date of Patent: May 23, 2006Assignee: Duke UniversityInventors: Jonathan S. Stamler, Eric J. Toone
-
Patent number: 7030239Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) useful in treating Alzheimer's disease and other similar diseases.Type: GrantFiled: May 18, 2004Date of Patent: April 18, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Roy Hom, Shumeye S. Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Y. Fang
-
Publication number: 20040110768Abstract: Bombesin receptor antagonists are provided which are compounds of formula (I) or pharmaceutically acceptable salts thereof: 1Type: ApplicationFiled: December 4, 2003Publication date: June 10, 2004Inventors: Michael Higginbottom, Martyn Clive Pritchard, Herman Thijs Stock
-
Patent number: 6743564Abstract: 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: GrantFiled: December 6, 2001Date of Patent: June 1, 2004Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Jun Hatakeyama, Tomohiro Kobayashi, Takeru Watanabe
-
Patent number: 6710071Abstract: 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: GrantFiled: August 15, 2002Date of Patent: March 23, 2004Assignee: Pfizer IncInventor: John Adams Lowe, III
-
Patent number: 6710190Abstract: 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: GrantFiled: November 21, 2001Date of Patent: March 23, 2004Assignee: Warner-Lambert CompanyInventor: Po-Wai Yuen