1,3-diazole Ring (including Hydrogenated) Patents (Class 544/370)
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Publication number: 20100317100Abstract: The present invention embraces compositions and methods for establishing and maintaining stem cells and inhibiting stem cell differentiation using a selective Protein Kinase C (PKC) inhibitor.Type: ApplicationFiled: June 11, 2010Publication date: December 16, 2010Inventors: Soumen Paul, Debasree Dutta, Soma Ray, Jeffrey Aube, Frank John Schoenen
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Publication number: 20100316607Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: June 15, 2010Publication date: December 16, 2010Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
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Patent number: 7851626Abstract: There is provided a compound of formula I and the pharmaceutically acceptable salts and esters thereof wherein X1, X2, R1, R2, R3, R4, R5 and R6 are herein described. The compounds exhibit activity as anticancer agents.Type: GrantFiled: November 27, 2006Date of Patent: December 14, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Qingjie Ding, Bradford James Graves, Norman Kong, Jin-Jun Liu, Allen John Lovey, Giacomo Pizzolato, John Lawson Roberts, Sung-Sau So, Binh Thanh Vu, Peter Michael Wovkulich
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Publication number: 20100310512Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: May 12, 2010Publication date: December 9, 2010Inventors: Hongyan Guo, Darryl Kato, Thorsten A. Kirschberg, Hongtao Liu, John O. Link, Michael L. Mitchell, Jay P. Parrish, Jianyu Sun, James Taylor, Elizabeth M. Bacon, Eda Canales, Aesop Cho, Choung U. Kim, Jeromy J. Cottell, Manoj C. Desai, Randall L. Halcomb, Michael Graupe, Evan S. Krygowski, Scott E. Lazerwith, Qi Liu, Richard L. Mackman, Hyung-Jun Pyun, Joseph H. Saugier, James D. Trenkle, Winston C. Tse, Randall W. Vivian, Scott D. Schroeder, William J. Watkins, Lianhong Xu
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Publication number: 20100305140Abstract: Compounds of formula I or pharmaceutically acceptable salts thereof: wherein X, A, R1, R2, R3 and R4 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.Type: ApplicationFiled: June 11, 2007Publication date: December 2, 2010Applicant: AstraZeneca ABInventors: William Brown, Daniel Page, Sanjay Srivastava, Christopher Walpole, Zhong-Yong Wei, Hua Yang
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Patent number: 7842693Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: December 9, 2003Date of Patent: November 30, 2010Assignee: ChemoCentryx, Inc.Inventors: Andrew M. K. Pennell, James B. Aggen, J. J. Kim Wright, Subhabrata Sen, Brian E. McMaster, Daniel Joseph Dairaghi, Valeri V. Martichonok
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Publication number: 20100298321Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: June 3, 2010Publication date: November 25, 2010Applicant: ABBOTT LABORATORIESInventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Todd M. Hansen
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Publication number: 20100297035Abstract: Thiazole amides, imidazole amides and related analogues of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).Type: ApplicationFiled: April 12, 2010Publication date: November 25, 2010Applicant: LIGAND PHARMACEUTICALS, INC.Inventors: Wallace C. Pringle, John M. Peterson, Linghong Xie, Ping Ge, Yang Gao, Joseph W. Ochterski, Jiong Lan
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Patent number: 7834017Abstract: There is provided compounds having the formula of structure I: wherein the groups —C(R8)(CH2)vCH(R9)(CH2)y-Q and —C(R8)(CH2)vCH(R9)(CH2)y-J are the same, and R1a, R1b, R2a, R2b, R8, R9, J, Q, W, X, L2, v and y have meanings given in the description. The use of such compounds in the treatment of a condition responsive to changes in melanocortin receptor function in a human or non-human mammal (e.g. male sexual dysfunction, female sexual dysfunction, an eating disorder, above optimal body weight, obesity, below-optimal body weight or cachexia) is also described.Type: GrantFiled: August 10, 2007Date of Patent: November 16, 2010Assignee: Palatin Technologies, Inc.Inventors: Kevin Burris, Yi-Qun Shi, Shubh D. Sharma, Yadi Reddy Bonuga, Papireddy Purma
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Publication number: 20100286160Abstract: Compounds of Formula (I): or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.Type: ApplicationFiled: June 25, 2008Publication date: November 11, 2010Inventors: Eric J. Gilbert, William J. Greenlee, Sarah Wei Li, Michael W. Miller, Jack D. Scott, Adrew Stamford, Chander Shekher Celly
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Publication number: 20100286166Abstract: The present invention relates to the use of specific types of compounds acting as pharmacological chaperones having a stabilizing activity on the phenylalanine hydroxylase (PAH) enzyme for the prophylaxis and/or treatment of hyperphenylalaninemia (HPA) and phenylketonuria PKU) and diseases, disorders and conditions related thereto. Further, the present invention relates to pharmaceutical compositions containing the compounds according to the present invention as well as to methods of treatment of HPA, in particular, PKU and diseases, disorders and conditions related thereto.Type: ApplicationFiled: June 27, 2008Publication date: November 11, 2010Applicant: UNIVERSIDAD DE ZARAGOZAInventors: Ángel Pey Rodríguez, Aurora Martínez Ruiz, Javier Sancho Sanz, Nunilo Cremades Casasín, Adrián Velázquez Campoy, Ming Ying
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Publication number: 20100286114Abstract: Heterocyclic compounds that modulate the hedgehog signaling pathway, pharmaceutical composition thereof and their therapeutic applications.Type: ApplicationFiled: December 10, 2008Publication date: November 11, 2010Applicant: SIENA BIOTECH S.P.A.Inventors: Russell John Thomas, Gal.la Pericot Mohr, Giacomo Minetto, Annette Cornelia Bakker, Pietro Ferruzzi
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Patent number: 7829713Abstract: The invention includes a compound of formula I: wherein R1, X, Z, n, and m have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function in animals.Type: GrantFiled: February 27, 2007Date of Patent: November 9, 2010Assignee: Helicon Therapeutics, Inc.Inventors: Terrence P. Keenan, Alan P. Kaplan
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Publication number: 20100280013Abstract: [Object] It is to provide a novel LXR? agonist useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate: (wherein, each V and W independently show N or C—R7; each X and Y independently show CH2, C?O, SO2, etc; Z shows CH or N; each R1, R2 and R7 independently show a hydrogen atom, C1-8 alkyl group, etc.; R3 shows C1-8 alkyl group; R4 shows an optionally substituted C6-10 aryl group or an optionally substituted 5- to 11-membered heterocyclic group; R5 and R6 show a hydrogen atom, etc.; L shows a C1-8 alkyl chain optionally substituted with an oxo group, etc.; and n shows any integer of 0 to 2.Type: ApplicationFiled: April 28, 2010Publication date: November 4, 2010Applicant: KOWA COMPANY, LTD.Inventors: Minoru Koura, Hisashi Sumida, Sayaka Kurobuchi, Takayuki Matsuda, Yuichiro Watanabe, Takashi Enomoto, Kimiyuki Shibuya, Sumiko Kurobuchi
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Publication number: 20100280028Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R5, A, B, D and X are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: April 27, 2010Publication date: November 4, 2010Applicant: Boehringer Ingelheim International GmbHInventors: Jennifer A. KOWALSKI, Daniel Richard MARSHALL, Anthony S. PROKOPOWICZ, III, Sabine SCHLYER, Robert SIBLEY, Ronald John SORCEK, Di WU, Frank WU, Erick Richard Roush YOUNG
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Patent number: 7820821Abstract: The present invention relates to compounds and methods from the treatment of cancer. The invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising compounds that inhibit Aurora kinase, and methods for the treatment of cancer using the compounds of the presentation invention or pharmaceutical compositions comprising compounds of the present invention.Type: GrantFiled: February 9, 2007Date of Patent: October 26, 2010Assignee: TransTech Pharma, Inc.Inventors: Adnan M. M. Mjalli, Brian S. Grella, Govindan Subramanian, Murty N. Arimilli, Ramesh Gopalaswamy, Robert C. Andrews, Stephen Davis, Xiaochuan Guo, Jeff Zhu
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Patent number: 7820646Abstract: The present invention relates to new substituted imidazole compounds have the following Formula (I) and to the pharmaceutically acceptable salts, esters, or prodrugs thereof, to compositions of the compounds together with pharmaceutically acceptable carriers, and to uses of the compounds:Type: GrantFiled: January 3, 2008Date of Patent: October 26, 2010Assignee: Novartis Vaccines and Diagnostics, Inc.Inventors: Rustum Boyce, Eric Martin, Weibo Wang, Hong Yang, Paul A. Barsanti
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Patent number: 7820673Abstract: The present invention provides a urea derivative or a salt thereof, which is useful as a therapeutic agent for thrombosis.Type: GrantFiled: December 15, 2004Date of Patent: October 26, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Keiji Kubo, Yasuhiro Imaeda
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Publication number: 20100266543Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: February 9, 2010Publication date: October 21, 2010Inventors: Yao-Ling Qiu, Ce Wang, Lu Ying, Xiaowen Peng, Yat Sun Or
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Publication number: 20100267710Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 28, 2010Publication date: October 21, 2010Applicant: ARRAY BIOPHARMA INC.Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
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Publication number: 20100267698Abstract: This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.Type: ApplicationFiled: January 5, 2010Publication date: October 21, 2010Inventors: Guiying Li, Pamela Albaugh, Kevin S. Currie, Guolin Cai, Linda M. Gustavson, Kyungae Lee, Alan Hutchison, George D. Maynard, Jun Yuan, Ling Hong Xie, Manuka Ghosh, Nian Liu, George P. Luke, Scott Mitchell, Martin Patrick Allen, Spiros Liras
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Publication number: 20100261717Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 28, 2010Publication date: October 14, 2010Applicant: ARRAY BIOPHARMA INC.Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
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Publication number: 20100261899Abstract: Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor expression, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.Type: ApplicationFiled: June 9, 2010Publication date: October 14, 2010Inventors: Daniel J. Buzard, James P. Edwards, David E. Kindrachuk, Jennifer D. Venable
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Publication number: 20100261898Abstract: Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor expression, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.Type: ApplicationFiled: June 4, 2010Publication date: October 14, 2010Inventors: Daniel J. BUZARD, James P. Edwards, David E. Kindrachuk, Jennifer D. Venable
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Publication number: 20100261718Abstract: Disclosed are compounds of the Formula and pharmaceutically acceptable salts and prodrugs thereof, wherein A, R1, R2, R7, R8, and R9 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 28, 2010Publication date: October 14, 2010Applicant: ARRAY BIOPHARMA INC.Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
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Patent number: 7812021Abstract: The invention relates to a compound of general formula wherein Ar, R1, R2, R3, R4, n, o, p, s, X and are as defined herein or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. The compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: GrantFiled: August 21, 2008Date of Patent: October 12, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Philippe Jablonski, Kenichi Kawasaki, Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Xihan Wu
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Publication number: 20100256376Abstract: A process for preparing benzimidazole thiophenes including 5-{6-[(4-methylpiperazin-1-yl)methyl]-1H-benzimidazol-1-yl}-3-{(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy}thiophene-2-carboxamide.Type: ApplicationFiled: June 23, 2008Publication date: October 7, 2010Inventors: Amanda Caroline Lucas, Robert M. Harris, Christopher James Nichols, Andrew Jonathan Whitehead
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Publication number: 20100249085Abstract: This invention relates to novel heteroaryl substituted pyrazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients or therapeutic measures.Type: ApplicationFiled: May 8, 2008Publication date: September 30, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Stephen Boyer, Michael Härter, Philip L. Wickens, Manoj Patel, Ellalahewage Sathyajith Kumarasinghe, Ajay Kumar Bhargava, Karl-Heinz Thierauch, Hartmut Beck, Susanne Greschat, Peter Ellinghaus, Patrick Paulus, Holger Hess-Stumpp
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Publication number: 20100240639Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: April 13, 2010Publication date: September 23, 2010Inventors: Kristof Van Emelen, Janine Arts, Leo-Jacobus Jozef Backx, Hans Louis Jos De Winter, Sven Franciscus Anna Van Brandt, Mac Gustaaf Celine Verdonck, Lieven Meerpoel, Isabelle Noëlle Constance Pilatte, Virginie Sophie Poncelet, Alexey Borisovich Dyatkin, Jimmy Arnold Viviane Van heusden
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Publication number: 20100234374Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts and tautomers thereof. Compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. They are also useful for treating neurodegenerative diseases, mental retardation, schizophrenia, inflammatory diseases, restenosis, immune disorders, diabetes, cardiovascular disorders and asthma.Type: ApplicationFiled: December 21, 2006Publication date: September 16, 2010Inventors: Philip Jones, Jesus Maria Ontoria Ontoria, Rita Scarpelli, Raffaele Ingenito, Carsten Schultz-Fademrecht
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Patent number: 7795255Abstract: Disclosed are novel rigidified compounds having a rhodanine-like residue and at least one aryl or heteroaryl residue linked to the rhodanine-like residue, whereby a core structure of these compounds, as defined in the specification, is characterized as having one or zero free-to-rotate bonds. Also disclosed are pharmaceutical compositions containing these rigidified compounds and uses thereof for modulating the activity of heparanase and hence in the treatment of heparanase-associated diseases and disorders, and uses thereof for modulating the activity of heparin-binding proteins and hence in the treatment of heparin-binding proteins-associated diseases and disorders as well as in the treatment of medical conditions that are at least partially treatable by rhodanine or a rhodanine analog.Type: GrantFiled: January 5, 2006Date of Patent: September 14, 2010Assignee: InSight Biopharmaceuticals Ltd.Inventors: Joel M. Van Gelder, Joseph Y. Klein, Yochai Basel, Anat Reizelman, Susanna Tchilibon, Orly Mouallem
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Patent number: 7795265Abstract: Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R, such as obesity, and diabetes.Type: GrantFiled: April 10, 2007Date of Patent: September 14, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Scott Edmondson, Alexa Hansen, Cheng Zhu
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Publication number: 20100226969Abstract: The invention provides compositions comprising protein aggregation inhibitors, and pharmaceutical compositions comprising them, and methods for making and using them, including methods for preventing, reversing, slowing or inhibiting protein aggregation, e.g., for treating diseases that are characterized by protein aggregation—including some degenerative neurological diseases such as Parkinson's disease. In one aspect, the compositions of the invention specifically target synuclein, beta-amyloid and/or tau protein aggregates, and the methods of the invention can be used to specifically prevent, reverse, slow or inhibit synuclein, beta-amyloid and/or tau protein aggregation. In alternative embodiments, the compositions and methods of the invention, are used to treat, prevent or ameliorate (including slowing the progression of) degenerative neurological diseases related to or caused by protein aggregation, e.g., synuclein, beta-amyloid and/or tau protein aggregation.Type: ApplicationFiled: June 13, 2008Publication date: September 9, 2010Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Eliezer Masliah, Igor Tsigelny, Wolfgang Wrasidlo, Edward Rockenstein
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Patent number: 7790726Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: August 14, 2006Date of Patent: September 7, 2010Assignee: Chemocentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Lianfa Li, Edward J. Sullivan, Wei Chen, Kevin Lloyd Greenman
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Publication number: 20100221215Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: February 9, 2010Publication date: September 2, 2010Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Publication number: 20100222588Abstract: There is provided a method for manufacture of 2-oxoimidazolidines of Formula I comprising one or more of the steps of converting an amine to an acylation agent, condensation of the acylation agent with a bi-functional compound of structure L-C(R4)(R5)—C(R2)(R3)—NHR1, wherein L is a leaving group, and ring closure of the resulting urea. In this manner, certain 2-oxoimidazolidines may be manufactured that are useful intermediates for the production of Pramiconazole and structurally related compounds.Type: ApplicationFiled: March 1, 2010Publication date: September 2, 2010Applicant: Thesis Chemistry, LLCInventors: John R. Peterson, Christopher M. Yost
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Patent number: 7786127Abstract: The present invention provides benzimidazole thiophene compounds, pharmaceutical compositions containing the same, and their use as pharmaceutical agents.Type: GrantFiled: August 28, 2006Date of Patent: August 31, 2010Assignee: Glaxo SmithKline LLCInventors: Mui Cheung, Kyle Allen Emmitte, James Michael Salovich
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Publication number: 20100215618Abstract: The invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, R6 and L are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are useful in the treatment of hepatitis C virus.Type: ApplicationFiled: February 23, 2010Publication date: August 26, 2010Applicant: Arrow Therapeutics LimitedInventors: Malcolm Clive Carter, Neil Mathews
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Publication number: 20100216809Abstract: The invention further relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —S(?O)p-; C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —O—C(?O)—; —C(?O)—C(?O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5-or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxlyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzo-dioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-mType: ApplicationFiled: June 5, 2008Publication date: August 26, 2010Applicant: Janssen Pharmaceutica N.V.Inventors: Jean-Pierre André Marc Bongartz, Lieven Meerpoel, Gustaaf Maria Boeckx, Guy Rosalia Eugeen Van Lommen, Christophe Francis Robert Buyck, Daniel Obrecht, Philipp Ermert, Anatol Luther
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Patent number: 7781596Abstract: The invention relates to novel 2-phenylbenzimidazoles of general formula (I) or (II), wherein the radicals have the meanings cited in the description, and to their tautomeric forms, possible enantiomeric and diastereomeric forms, to their prodrugs, and to possible physiologically compatible salts. The invention also relates to the production of said compounds and to their use.Type: GrantFiled: October 28, 1999Date of Patent: August 24, 2010Assignee: Abbott LaboratoriesInventors: Wilfried Lubisch, Michael Kock, Thomas Höger
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Patent number: 7776855Abstract: This invention includes oxazolidinone prodrug compounds of Formula (I) and Formula (II) as defined herein. The prodrugs are convertible by natural biological processes into an active ingredient possessed of antimicrobial properties useful in treating bacterial infections in mammals.Type: GrantFiled: July 9, 2007Date of Patent: August 17, 2010Assignee: Janssen Pharmaceutica N.V.Inventors: Mark J. Macielag, Manomi A. Tennakoon
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Patent number: 7772230Abstract: The present invention provides a chroman compound of formula (I) and its pharmaceutical salt, methods of its preparation and its pharmaceutical applications. Wherein: X is O or S; n is for 2, 3 or 4; R1 is 6-substituted or 7-substituted halogen, C1-4alkyl, C1-4alkoxyl, benzyloxy, carbamoyl; R2 is nitrogen-containing five-membered or six-membered substituted heterocyclic ring selected from piperidinyl, morpholinyl, N-methyl-piperazinyl, N-(2-ethoxyl)piperazinyl, pyrrolyl, pyrazolyl or imidazolyl. The compounds are useful to prepare medicaments for treating cardiovascular diseases, their preparation employs mild reaction conditions, the raw material are plenty and easy to be obtained, and the operation and post-treatment in the preparation are simple.Type: GrantFiled: October 25, 2007Date of Patent: August 10, 2010Assignee: China Pharmaceutical UniversityInventors: Qidong You, Lvpei Du, Minyong Li, Lin Xia
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Patent number: 7767674Abstract: The present invention provides kinase inhibitors of Formula I:Type: GrantFiled: June 15, 2005Date of Patent: August 3, 2010Assignee: Eli Lilly and CompanyInventors: Tiechao Li, Mark Andrew Pobanz, Chuan Shih, Yong Wang, Boyu Zhong, Jesus Andres Blas, Alfonso De Dios, Beatriz Lopez De Uralde-Garmendia, Luisa Maria Martin Cabrejas
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Publication number: 20100191475Abstract: Materials, methods and a computer system are provided which facilitate the identification and characterization of modulators of potassium ion channels, particularly the HERG channel.Type: ApplicationFiled: March 4, 2010Publication date: July 29, 2010Inventors: Scott Perschke, Ming Liu
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Publication number: 20100190183Abstract: Subject of the present invention are new isotopic and isobaric tagged molecules, kits comprising them and methods of using them in mass spectrometry.Type: ApplicationFiled: July 8, 2008Publication date: July 29, 2010Applicant: KONINKLIJKE PHILIPS ELECTRONICS N.V.Inventors: Ralf Hoffmann, Edwin Peter Romijn, Eef Hubert Cecil Dirksen
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Patent number: 7763726Abstract: The present invention relates to compounds and methods from the treatment of cancer. The invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising compounds that inhibit Aurora kinase, and methods for the treatment of cancer using the compounds of the presentation invention or pharmaceutical compositions comprising compounds of the present invention.Type: GrantFiled: February 9, 2007Date of Patent: July 27, 2010Assignee: TransTech Pharma, Inc.Inventors: Adnan M. M. Mjalli, Brian S. Grella, Govindan Subramanian, Murty N. Arimilli, Ramesh Gopalaswamy, Robert C. Andrews, Stephen Davis, Xiaochuan Guo, Jeff Zhu
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Publication number: 20100184747Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: June 9, 2008Publication date: July 22, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Treu, Ulrich Guertler, Thomas Karner, Oliver Kraemer, Jens Juergen Quant, Stephan Karl Zahn
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Publication number: 20100184750Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: January 18, 2010Publication date: July 22, 2010Applicant: ABBOTT LABORATORIESInventors: Laura A. Hexamer, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Michael D. Wendt
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Patent number: 7759352Abstract: Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R, such as obesity, and diabetes.Type: GrantFiled: April 10, 2007Date of Patent: July 20, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Joseph L. Duffy, Scott Edmondson, Hansen Alexa, Cheng Zhu
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Publication number: 20100179147Abstract: Benzimidazole compounds of formula (I): wherein R1, R2, R3, R4, R5, X, Y, Z1, and Z2 are defined herein. Also disclosed is a method for treating cancer with benzimidazole compounds.Type: ApplicationFiled: December 10, 2009Publication date: July 15, 2010Inventors: Chih-Shiang Chang, Jih-Hwa Guh, Che-Ming Teng, Shiow-Lin Pan, Wei-Ling Chang, Ju-Fang Liu, Kai-Wei Chang, Sheng-Chu Kuo