Ring Chalcogen In The Additional Hetero Ring (e.g., Oxazole, Etc.) Patents (Class 514/236.8)
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Patent number: 7723333Abstract: The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) ? (NR1H3) and/or ? (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: GrantFiled: January 9, 2006Date of Patent: May 25, 2010Assignee: AstraZeneca ABInventors: Anders Broo, Robert Judkins, Lanna Li, Eva-Lotte Lindstedt-Alstermark, Pernilla Sandberg, Marianne Swanson, Lars Weidolf, Kay Brickmann, Patrik Holm
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Publication number: 20100120770Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I thiazolyl compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's disease.Type: ApplicationFiled: April 9, 2008Publication date: May 13, 2010Inventors: Anne Marinier, Marco Dodier, Stephan Roy, Kurt Zimmermann, Xiaopeng Sang, Mark D. Wittman, David R. Langley, Ramkumar Rajamani
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Publication number: 20100120718Abstract: The present invention relates to combinations of A) oxazolidinones of the formula (I) with B) acetylsalicylic acid (aspirin) and C) an ADP receptor antagonist, in particular P2Y12 purinoreceptor blocker, to a process for producing these combinations and to the use thereof as medicaments, in particular for the prophylaxis and/or treatment of thromboembolic disorders.Type: ApplicationFiled: October 19, 2007Publication date: May 13, 2010Applicant: Bayer Schering Pharma AktiengesellschaftInventor: Elisabeth Perzborn
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Publication number: 20100113435Abstract: The present invention relates to compounds with the formula (II) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.Type: ApplicationFiled: November 16, 2009Publication date: May 6, 2010Inventors: Tjeerd BARF, Rikard Emond, Guido Kurz, Jerk Vallgarda, Marianne Nilsson
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Publication number: 20100113448Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycle or optionally substituted heterocyclealkyl, X is —O—, —NR3—, —NR3C(?O)— or —NR3S(?O)2—, R2 is optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, R3 is hydrogen or optionally substituted alkyl.Type: ApplicationFiled: March 27, 2008Publication date: May 6, 2010Applicants: INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC., SHIONOGI & CO., LTD.Inventors: Akiko Itai, Susumu Muto, Ryuko Tokuyama, Hiroshi Fukasawa, Takeshi Yanase
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Publication number: 20100105663Abstract: The invention relates to substituted indazoles and methods for production thereof and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases, especially of cardiovascular diseases, preferably of thromboembolic diseases.Type: ApplicationFiled: July 2, 2007Publication date: April 29, 2010Applicant: BAYER HEALTHCARE AGInventors: Stephan Siegel, Dirk Schneider, Anja Buchmüller, Elke Dittrich-Wengenroth, Chrisstoph Gerdes, Mark Jean Gnoth, Stefan Heitmeier, Martin Hendrix, Ulrich Rester, Uwe Saatmann
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Publication number: 20100099662Abstract: A hydrazone derivative of formula [I]: wherein Ring A is aryl or heteroaryl, Ring T is heteroaryl or heterocycle, R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl, etc., R3 and R4 combine each other together with the adjacent nitrogen atom to form substituted or unsubstituted heterocycle, R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl, etc., and R6 is hydrogen atom, etc.; or a pharmaceutically acceptable salt thereof is useful as a glucokinase activation agent.Type: ApplicationFiled: January 9, 2008Publication date: April 22, 2010Inventors: Iwao Takamuro, Kazutoshi Sugawara, Hiroshi Sugama
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Publication number: 20100099677Abstract: The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-V) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.Type: ApplicationFiled: April 20, 2009Publication date: April 22, 2010Inventor: Kevin James Doyle
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Publication number: 20100093732Abstract: The present invention relates to new salt forms of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide, in particular the mesylate, hydrochloride, tartrate, phosphate and hemi fumarate salt thereof; to crystalline forms of such salts; to polymorphs of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide; to hydrates and polymorphs of the new salt forms mentioned above; to the use of the new salt forms mentioned above for the manufacture of a medicament for the treatment of a disorder mediated by Hsp90; to a method for treating a disorder mediated by Hsp90 using the new salt forms; to formulations comprising such salt forms, in particular aqueous solutions suitable for intravenous administration; and to amber glass containers being filled with such formulations.Type: ApplicationFiled: February 28, 2008Publication date: April 15, 2010Inventors: Martin James Drysdale, Brian William Dymock, Christoph Krell, Michael Mutz, Holger Petersen, Weijia Zheng
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Publication number: 20100093690Abstract: Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: December 17, 2009Publication date: April 15, 2010Inventors: Ian Bruce, Peter Finan, Catherine LeBlanc, Clive McCarthy, Lewis Whitehead, Nicola Press, Graham Charles Bloomfield, Judy Hayler, Louise Kirman, Mrinalini Sachin Oza, Lena Shukla
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Patent number: 7691889Abstract: Novel compounds belonging to the class of oxazolidinones possessing potent antimycobacterial properties especially useful in the treatment of acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai. The compound and its pharmaceutically acceptable salts act as antibacterial agents. Also mentioned is a method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial conditions such as Mycobacterium tuberculosis, drug resistant Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai., including administering an antimycobacterially effective amount of the compound and/or pharmaceutically acceptable salts. There is also mentioned a process for the manufacture of the compound or its pharmaceutically acceptable salts.Type: GrantFiled: March 18, 2005Date of Patent: April 6, 2010Assignee: Lupin LimitedInventors: Sudershan Kumar Arora, Vijaykumar Jagdishwar Patil, Prathap Sreedharan Nair, Prasad Purushottam Dixit, Shankar Ajay, Rakesh Kumar Sinha
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Publication number: 20100075931Abstract: Certain oxazole ketone compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).Type: ApplicationFiled: September 7, 2007Publication date: March 25, 2010Applicant: THE SCRIPPS RESEARCH INSTITUTEInventor: Dale L. Boger
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Publication number: 20100069363Abstract: The present application relates to novel substituted 4-amino-3,5-dicyano-2-thiopyridine 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, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.Type: ApplicationFiled: November 17, 2007Publication date: March 18, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Peter Nell, Nicole Diedrichs, Barbara Albrecht-Küpper, Alexandros Vakalopoulos, Frank Süssmeier, Joerg Keldenich
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Patent number: 7678789Abstract: The present invention relates to 5-imino-5H-[1,2,4]-dithiazol-3-yl-amine and [1,2,4]-dithiazolidine-3,5-diylidene-diamine derivatives as inducers of gluthathione-S-transferase (GST) and NADPH quinone oxidoreductase (NQO), to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said [1,2,4]-dithiazoli(di)ne derivatives. The invention also relates to the use of a compound disclosed herein for the treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular. The invention relates to compounds of the general formula (I): wherein wherein the symbols have the meanings given in the specification.Type: GrantFiled: February 9, 2006Date of Patent: March 16, 2010Assignee: Solvay Pharmaceuticals B.V.Inventors: Roelof W. Feenstra, Hiskias G. Keizer, Maria L. Pras-Raves, Bernard J Van Vliet, Gustaaf J. M. Van Scharrenburg
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Publication number: 20100061960Abstract: Disclosed are compounds, stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses.Type: ApplicationFiled: July 16, 2009Publication date: March 11, 2010Inventors: Franz Ulrich Schmitz, Roopa Rai, Ronald Griffith, Christopher Don Roberts
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Publication number: 20100063022Abstract: The present application relates to cannabinoid receptor ligands of formula (I) wherein X1, A1, Rx, R2, R3, R4, and z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: September 4, 2009Publication date: March 11, 2010Applicant: ABBOTT LABORATORIESInventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Teodozyj Kolasa, Tongmei Li, Bo Liu, Arturo Perez-Medrano, Meena Patel, Xueqing Wang, Sridhar Peddi
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Patent number: 7671051Abstract: The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.Type: GrantFiled: July 13, 2005Date of Patent: March 2, 2010Assignee: Biovitrum ABInventors: Tjeerd Barf, Rikard Emond, Jerk Vallgarda, Guido Kurz, Marianne Nilsson, Lian Zhang
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Publication number: 20100048570Abstract: The present invention relates to novel 2-carbonyl-3-acyl-1,3-thiazolidines having a ?-amino group on the acyl chain, in free, prodrug form or pharmaceutically acceptable salt thereof, including their enantiomers, diastereomers and racemates, as efficient inhibitors against DPP-IV. The invention further relates to the pharmaceutical compositions comprising the disclosed compounds. The present invention also relates to methods for preparing the disclosed compounds and for treating DPP-IV-mediated diseases.Type: ApplicationFiled: January 16, 2008Publication date: February 25, 2010Applicants: Kainos Medicine, Inc, Korea Research Institute of Chemical Technology, Yungjin Pharmaceutical Company, LtdInventors: Sung Soo Kim, Jin Hee Ahn, Hyae Gyeong Cheon, Sang Dal Rhee, Nam Sook Kang, Ki Young Kim, Seung Kyu Kang, Won Hoon Jung, Sung Gyu Kim, Sun Young Kim, Jae Hong Kweon, Sang Kwon Sohn, Min Ki Shin, Ni Na Ha
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Publication number: 20100022545Abstract: Compounds in accord with Formula I: wherein R1, R2, R3 and R4 are as defined in the specification, pharmaceutically acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.Type: ApplicationFiled: October 8, 2009Publication date: January 28, 2010Inventors: Joseph Cacciola, James Empfield, James Folmer, Angela M. Hunter, Scott Throner
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Publication number: 20100022542Abstract: Pharmaceutical compositions containing as an active ingredient compounds of the general formula (I), prodrugs of the same, pharmaceutically acceptable salts of both, or solvates of them and exhibiting thrombopoietin receptor agonism: X1—Y1-Z1-W1??(I) wherein X1 is optionally substituted aryl, optionally substituted heteroaryl or the like; Y1 is —NRACO—(CH2)0-2— or the like (wherein RA is a hydrogen or the like); Z1 is optionally substituted phenylene or the like; and W1 is a group represented by the below formula: wherein R1, R2, R3, and R4 are each independently a hydrogen atom, optionally substituted lower alkyl or the like, a broken line (---) represents the presence or absence of bond.Type: ApplicationFiled: July 16, 2009Publication date: January 28, 2010Inventors: Hiroshi TAKEMOTO, Takeshi SHIOTA, Masami TAKAYAMA
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Publication number: 20100022544Abstract: The present application relates to novel 4-cycloalkyl- and 4-heterocycloalkyl-3,5-dicyano-2-thio-pyridine 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, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.Type: ApplicationFiled: November 17, 2007Publication date: January 28, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Peter Nell, Walter Hübsch, Barbara Albrecht-Küpper, Alexandros Vakalopoulos, Frank Süssmeier, Jörg Keldenich, Joachim Telser
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Publication number: 20100022541Abstract: The invention relates to new compounds having heptose synthesis inhibitory properties, of formula (I) or a pharmaceutically acceptable salt, or prodrug thereof, wherein A is an aryl or heterocycle, optionally substituted by one or several identical or different R such as H, C1-C10 alkyl, C1-C10 alkyl-OR1, C1-C10 alkyl-NR1R1, alkoxy, hydroxy, thioalkyl, aryl, heterocycle, halogen, nitro, cyano, CO2R1, NR1R1, NR1C(O)R1, C(O)NR1R1, NR1C(S)R1, C(S)NR1R1, SO2NR1R1, SO2R1, NR1SO2R1, NR1C(O)NR1R1, NR1C(O)OR1, NR1C(S)NR1R1, NR1C(S)OR1, R1C?NOR1, C(O)R1, aryloxy, thioaryl, alkenyl, alkynyl R1 identical or different is H or C1-C10 alkyl B1, B2, B3 identical or not represent C, N, O, S to form a five-membered aromatic ring wherein from one to three carbon atoms are replaced by a heteroatom selected from S, O, N optionally substituted by one or several identical or different R such as defined above B4 is C or N Y is H, C1-C10 alkyl, alkoxy, thio-alkyl, optionally substituted by one or several identical or different R sucType: ApplicationFiled: September 25, 2007Publication date: January 28, 2010Inventors: Sonia Escaich, Alexis Denis, Francois Moreau, Vincent Gerusz, Nicolas Desroy
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Publication number: 20100022543Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: ApplicationFiled: July 28, 2009Publication date: January 28, 2010Inventors: Lawrence S. Melvin, JR., Michael Graupe, Chandrasekar Venkataramani
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Patent number: 7652047Abstract: The invention concerns compounds which inhibit MEK and which have activity as anti-neoplastic agents. These compounds include N-substituted-3-hydroxy-5-arylamino-isothiazole-4-carboxamidines. Also included are the tautomeric isothiazol-3(2H)-ones.Type: GrantFiled: July 11, 2008Date of Patent: January 26, 2010Assignee: Ardea Biosciences, Inc.Inventors: Hassan El Abdellaoui, Robert Tam, Huanming Chen, Varaprasad Chamakura, Dinesh Barawkar, Andreas Maderna, Zhi Hong, Stanley Lang
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Publication number: 20100016321Abstract: The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) ? (NR1H3) and/or ? (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: July 23, 2009Publication date: January 21, 2010Applicant: ASTRAZENECA ABInventors: Jonas Bostrom, Kay Brickmann, Anders Broo, Robert Judkins, Lanna Li, Pernilla Sandberg, Marianne Swanson, Christer Westerlund, Patrik Holm
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Publication number: 20100009989Abstract: This application relates to novel urea glucokinase activators and use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes. Further encompassed is a pharmaceutical composition comprising a compound according to the invention and a process for preparing such.Type: ApplicationFiled: January 8, 2008Publication date: January 14, 2010Applicant: Novo Nordisk A/SInventors: Anthony Murray, Jesper Lau, Per Vedsø
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Publication number: 20100004219Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity, including metabolic and inflammatory or immune associated diseases or disorders having the structure of formula I or an enantiomer, diastereomer, tautomer, or a pharmaceutically-acceptable salt, thereof, wherein: A is a 5-, 6-, or 7-membered heterocyclo or heteroaryl, each containing 1, 2, or 3 heteroatoms selected from N, O, and S and substituted with one to four groups, R1, R2, R3, and/or R4, provided that (i) A is not tetrazole or (ii) if A is thienyl or furanyl then Z is selected from a group other than succinimido or thalimido; M is selected from alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl; Ma is a linker between C and M and is selected from a bond and C1-C3alkylene; Q is selected from (i) hydrogen, halogen, nitro, cyano, hydroxy, C1-4alkyl, and substituted C1-4 alkyl; or (ii) Q is combined with R6 and with the carbon atoms to whType: ApplicationFiled: October 31, 2007Publication date: January 7, 2010Inventors: Bingwei Vera Yang, Lidia M. Doweyko
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Publication number: 20090324729Abstract: The invention provides a composition comprising, a compound of formula (I): or a pharmaceutically acceptable salt thereof and a plurality of solid carrier particles, as well as methods for using the composition to inhibit the activity of cytochrome P-450.Type: ApplicationFiled: May 1, 2009Publication date: December 31, 2009Applicant: GILEAD SCIENCES, INC.Inventors: Joanna M. Koziara, Mark M. Menning, Reza Oliyai, Robert G. Strickley, Richard Yu, Brian P. Kearney, Anita A. Mathias
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Publication number: 20090325961Abstract: Novel non-steroidal compounds are provided that are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases having the structure of formula (I): or enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, where X is A1QA2-; Q is a bond, —C(?O)—, —OC(O)—, —C(?O)NR5—, —SOp—, —SOpNR5—, —C(O)O—, —NR5C(O)—, —OC(O)NR5—, —NR5C(O)O—, —S(O)pNR5C(O)—, —C(O)NR5S(O)p— —NR5S(O)p—, or —NR5C(?O)NR6—. Y is selected from hydrogen, C1-6alkyl, OR16, substituted C1-6alkyl, cycloalkyl, aryl, heterocyclo and heteroaryl. A1 and A2 are independently selected from a bond, C1-3alkylene, or C1-3alkenylene, and R1-R11 are defined herein. Also provided are pharmaceutical compositions, combinations, and methods of treating obesity, diabetes and inflammatory- or immune-associated diseases comprising said compounds.Type: ApplicationFiled: August 18, 2009Publication date: December 31, 2009Inventors: Jingwu Duan, Bin Jiang
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Publication number: 20090325925Abstract: This invention provides thiophene compounds of formula I: wherein R1, R2, R3, R4, n, p, and m are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: January 26, 2009Publication date: December 31, 2009Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christelle C. Renou, Tricia J. Vos, Matthew O. Duffey, Robert Downham
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Publication number: 20090318409Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, Q, X1, X2, Y, R1, R2, R3, R4, R4?, R5, R6 and R6? are as described herein.Type: ApplicationFiled: August 10, 2009Publication date: December 24, 2009Applicant: Genentech, Inc.Inventors: Frederick Cohen, Vickie Hsiao-Wei Tsui, Cuong Ly, John A. Flygare
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Publication number: 20090318403Abstract: The present invention provides antimicrobial compositions comprising an antibiotic and a sensitizer that enhances the effectiveness or activity of the antibiotic, wherein the sensitizer is preferably a primary amine containing a long alkyl chain. Such compositions are particularly useful for the treatment of infections by drug resistant bacteria.Type: ApplicationFiled: August 2, 2007Publication date: December 24, 2009Applicant: Prosensa Technologies B.V.Inventors: Peter Christian De Visser, Gerard Johannes Platenburg, Jaap Tamino Van Dissel
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Publication number: 20090298833Abstract: The present application describes substituted piperidinyl modulators of MIP-1? or CCR-1 or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using said modulators are disclosed.Type: ApplicationFiled: July 20, 2009Publication date: December 3, 2009Inventors: Percy H. Carter, Cullen L. Cavallaro, John V. Duncia, Daniel S. Gardner, John Hynes, Rui-Qin Liu, Joseph B. Santella, Dharmpal S. Dodd
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Publication number: 20090298832Abstract: The present invention relates to 2,4,5-trisubstituted thiazole compounds of formula (I) or all possible isomers, prodrugs, pharmaceutically acceptable salts, solvates or hydrates thereof for the inhibition of plasma PLTP activity and/or plasma CETP activity, wherein the substituents are as defined in the specification; a process for the preparation of the compounds of formula (I); a pharmaceutical composition comprising the compound of formula (I) and its use for the preparation of a medicament for treatment and/or prevention of diseases associated with the increased plasma PLTP activity and/or the increased plasma CETP activity in a mammal, such as atherosclerosis, cardiovascular diseases and peripheral vascular diseases, etc.Type: ApplicationFiled: August 15, 2006Publication date: December 3, 2009Inventors: Song Li, Changbin Guo, Xiancheng Jiang, Junhai Xiao, Zhong Wu
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Publication number: 20090298806Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: ApplicationFiled: January 5, 2009Publication date: December 3, 2009Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough
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Publication number: 20090298822Abstract: The present invention relates to the use of compounds for manufacturing a pharmaceutical product/medicament for the prophylaxis and/or treatment of reperfusion damage.Type: ApplicationFiled: July 6, 2006Publication date: December 3, 2009Applicant: Bayer Health CareInventors: Thomas Krahn, Johannes-peter Stasch, Gerrit Weimann, Wolfgang Thielemann
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Publication number: 20090291952Abstract: The present application provides for a compound of Formula I, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.Type: ApplicationFiled: July 6, 2007Publication date: November 26, 2009Applicant: GILEAD SCIENCES, INC.Inventors: Manoj C. Desai, Allen Y. Hong, Hongtao Liu, Randall W. Vivian, Lianhong Xu
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Publication number: 20090286766Abstract: Provided is an agent for treating or preventing urinary frequency, urinary urgency and urinary, incontinence which are associated with overactive bladder, a lower urinary tract disease such as interstitial cystitis and chronic prostatitis accompanied by lower urinary tract pain, and various diseases accompanied by pain. A novel azolecarboxamide derivative in which an azole ring such as thioazole or oxazole is bonded to a benzene ring, pyridine ring or pyrimidine ring through carboxamide was confirmed to have a potent trkA receptor-inhibitory activity and found to be an agent for treating or preventing lower urinary tract disease and various diseases accompanied by pain, which is excellent in efficacy and safety, and thus the present invention was accomplished.Type: ApplicationFiled: April 19, 2007Publication date: November 19, 2009Applicant: ASTELLAS PHARMA INC.Inventors: Keizo Sugasawa, Kenichi Kawaguchi, Takaho Matsuzawa, Ryushi Seo, Hironori Harada, Akira Suga, Tomoaki Abe, Hidenori Azami, Shunichiro Matsumoto, Takashi Shin, Masayuki Tanahashi, Toru Watanabe
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Publication number: 20090286793Abstract: Compounds active on phosphodiesterase PDE4B are provided. Also provided herewith are compositions useful for treatment of PDE4B-mediated diseases or conditions, and methods for the use thereof.Type: ApplicationFiled: July 20, 2009Publication date: November 19, 2009Inventors: Prabha N. Ibrahim, Hanna Cho, Bruce England, Sam Gillette, Dean R. Artis, Rebecca Zuckerman, Chao Zhang
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Publication number: 20090286792Abstract: The present invention relates to 3-cycloalkylaminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, X, Y and Z are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as modulators of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: ApplicationFiled: November 19, 2008Publication date: November 19, 2009Inventors: Chu-Biao Xue, Brian W. Metcalf, Amy Qi Han, Darius J. Robinson, Changsheng Zheng, Anlai Wang, Yingxin Zhang
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Patent number: 7618961Abstract: The present invention relates to compounds with the formula (II) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.Type: GrantFiled: May 22, 2001Date of Patent: November 17, 2009Assignee: Biovitrum ABInventors: Tjeerd Barf, Rikard Emond, Guido Kurz, Jerk Vallgårda, Marianne Nilsson
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Patent number: 7608619Abstract: Substituted oxazole derivatives corresponding to formula I: a method for producing such compounds, pharmaceutical compositions containing such compounds, and the use of such compounds to treat pain, depression, urinary incontinence, diarrhoea, pruritus, alcohol and drug misuse, drug dependency, lethargy and/or anxiety.Type: GrantFiled: June 20, 2008Date of Patent: October 27, 2009Assignee: Gruenenthal GmbHInventors: Beatrix Merla, Stefan Oberboersch, Bernd Sundermann, Werner Englberger, Hagen-Heinrich Hennies, Heinz Graubaum
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Publication number: 20090264430Abstract: (2S)-[4-(Carboxymethyl)thiazol-2-ylthio]-N-{[4-(3,4-dichlorobenzyl)morpholin-2-yl]methyl}acetamide hydrobromide and a crystal thereof, which resist easy weight change caused by vapor sorption as compared to a free form, and are superior as drug substances of pharmaceutical products, and a production intermediate therefor are provided.Type: ApplicationFiled: July 11, 2007Publication date: October 22, 2009Inventors: Katsuhiko Masuda, Shuzo Takeda, Yoshihito Tanaka
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Publication number: 20090258875Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I) wherein T represent a tetrazolyl substituents, A represents a carbo- or heterocycle, L1 and L2 represent various linking groups and Q represents a carbocycle, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: July 12, 2007Publication date: October 15, 2009Inventors: Isabelle Christian, Marie-Claire Grosjean-Cournoyer, Pierre Hutin, Philippe Rinolfi, Arounarith Tuch, Jacky Vidal
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Publication number: 20090258851Abstract: The instant invention provides compounds of Formula II which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula II are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: ApplicationFiled: April 6, 2007Publication date: October 15, 2009Inventors: LIN Chu, Bing Li, Anthony K. Ogawa, Hyun O. Ok, Debra L Ondeyka, Minal Patel, Rosemary Sisco, Feroze Ujjainwalla, Jinyou Xu
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Publication number: 20090247516Abstract: The present invention concerns novel azolidine compounds of Formula (I) wherein X denotes S, NH, CH2 or O, Y and W denotes each independently S or O, Q denotes CH or N, n and m are an integer from 0 to 2, and R1 and R2 denote independently from each other hydrogen, optionally substituted aryl, optionally substituted heterocyclyl, or an optionally substituted (C1-10) aliphatic group, R3 denotes hydrogen, lower alkyl, halogen, lower alkoxy, nitro, and R4 and R5 denote independently from each other hydrogen, halogen or alkyl, with the proviso that if one of R1 and R2 is hydrogen then the respective other one of R1 and R2 does not denote substituted or unsubstituted 2-furyland their salts, that are useful as pharmaceutical agents, e.g. as antibacterial agents, and to pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: October 8, 2007Publication date: October 1, 2009Inventors: Miha Kotnik, Marko Oblak, Petra Stefanic Anderluh, Andrej Prezelj, Jan Humljan, Ivan Plantan, Uros Urleb, Tomaz Solmajer
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Publication number: 20090247526Abstract: Provided are compounds of formula I wherein R2, L, Z, Y, G and R1 are as defined herein, that are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.Type: ApplicationFiled: January 24, 2007Publication date: October 1, 2009Applicant: ARRAY BIOPHARMA INC.Inventors: Thomas D. Aicher, Steven Armen Boyd, Mark Joseph Chicarelli, Kevin Ronald Condroski, Rustam Ferdinand Garrey, Ronald Jay Hinklin, Ajay Singh, Timothy M. Turner
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Publication number: 20090247527Abstract: A compound having the formula or a pharmaceutically acceptable salt or a prodrug thereof is disclosed herein. Y, A, U, and B are as described herein. Methods, compositions, and medicaments related to these compounds are also disclosed.Type: ApplicationFiled: March 20, 2009Publication date: October 1, 2009Applicant: ALLERGAN, INC.Inventor: David W. Old
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Patent number: 7592339Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.Type: GrantFiled: July 27, 2006Date of Patent: September 22, 2009Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Alexander Straub, Thomas Lampe, Jens Pohlmann, Susanne Rohrig, Elisabeth Perzborn, Karl-Heinz Schlemmer, Joseph Pernerstorfer
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Publication number: 20090233931Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein J1, J2, B, Y, A and D are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: March 12, 2009Publication date: September 17, 2009Inventors: David W. Old, Robert M. Burk