Polycyclo Heterocyclic Ring System Containing Ring Nitrogen Patents (Class 548/181)
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Publication number: 20110028451Abstract: The invention relates to benzoindazole derivatives according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: ApplicationFiled: July 29, 2010Publication date: February 3, 2011Applicant: N.V. OrganonInventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen
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Patent number: 7879850Abstract: The present invention provides compounds of the following structure; A-Q-B—C-D that are useful for treating conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: GrantFiled: September 26, 2008Date of Patent: February 1, 2011Assignee: Novartis AGInventors: Young-Shin Kwak, Gary Mark Coppola
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Publication number: 20110012075Abstract: A fine particle which contains a compound represented by formula (1): wherein R1a and R1b may be the same or different, and each independently represent an alkyl group, an aryl group, or a heteroaryl group; R2 and R3 each independently represent a hydrogen atom or a substituent, and at least one of R2 and R3 is an electron withdrawing group; R2 may be bonded to R3 to form a ring; R4 represents a hydrogen atom, an alkyl group, an aryl group, a heteroaryl group, a substituted boron, or a metal atom; and R4 may be covalently bonded or coordinately bonded to at least one among R1a, R1b and R3.Type: ApplicationFiled: March 27, 2009Publication date: January 20, 2011Applicant: FUJIFILM CorporationInventors: Kazumi Nii, Shunya Kato, Yoshihiro Jimbo
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Publication number: 20110015234Abstract: The invention is concerned with novel indazole derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used in the prevention or treatment of diseases which are modulated by L-CPT1 inhibitors.Type: ApplicationFiled: September 8, 2010Publication date: January 20, 2011Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei
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Publication number: 20110009461Abstract: The invention relates to 2-aza-bicyclo[3.3.0]octane derivatives of Formula (I) wherein A, B, and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.Type: ApplicationFiled: July 25, 2008Publication date: January 13, 2011Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen, Daniel Trachsel
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Publication number: 20100331346Abstract: Novel heterocyclic compounds of the formula I in which R1, R2, R2?, R2?, R3, R4, R5, R6, R7 and R8 have the meanings indicated in Claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Typ 1 and 2, obesity, neuropathy and/or nephropathy.Type: ApplicationFiled: December 23, 2008Publication date: December 30, 2010Applicant: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Stefan Bender, Lars Thore Burgdorf, Ulrich Emde, Norbert Beier, Johannes Gleitz, Christine Charon
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Publication number: 20100324302Abstract: The present invention relates to processes for making epothilone compounds and analogs thereof, such as epi-epothilone A or epi-epothilone B, and aziridinyl-epothilone analogs.Type: ApplicationFiled: May 23, 2008Publication date: December 23, 2010Inventors: Luca Parlanti, Jurong Yu
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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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Publication number: 20100317674Abstract: Compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the description, processes for the preparing the compounds, new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and uses of the compounds in therapy.Type: ApplicationFiled: August 23, 2010Publication date: December 16, 2010Inventors: Bradford Van Wagenen, Radhakrishnan Ukkiramapandian, Joshua Clayton, Ian Egle, James R. Empfield, Methvin Isaac, Fupeng Ma, Abdelmalik Slassi, Gary Steelman, Rebecca Urbanek, Sally Walsh
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Publication number: 20100311741Abstract: This invention pertains generally to the field of therapeutic compounds, and more particularly, to certain bicyclosulfonyl acid (BCSA) compounds which act as inhibitors of Tumour Necrosis Factor-? Converting Enzyme (TACE). The compounds are useful in the treatment of conditions mediated by TNF-?, such as rheumatoid arthritis; inflammation; psoriasis; septic shock; graft rejection; cachexia; anorexia; congestive heart failure; post ischaemic reperfusion injury; inflammatory disease of the central nervous system; inflammatory bowel disease; insulin resistance; HIV infection; cancer; chronic obstructive pulmonary disease (COPD); and asthma. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in the inhibition of TACE, and in the treatment of conditions that are ameliorated by the inhibition of TACE.Type: ApplicationFiled: May 16, 2008Publication date: December 9, 2010Applicant: INHIBOX LTD.Inventors: Aigars Jirgensons, Gundars Leitis, Ivars Kalvinsh, Daniel Robinson, Paul Finn, Nagma Khan
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Publication number: 20100305073Abstract: The present invention relates to compounds that have CYP450 inhibiting properties and are therefore useful as boosters of certain drugs, i.e. they are able to increase at least one of the pharmacokinetic variables of certain drugs when co-administered. The invention further provides the use of said compounds as improvers of the bioavailability of certain drugs. Methods for the preparation of the compounds of the invention and pharmaceutical compositions are also provided.Type: ApplicationFiled: December 5, 2008Publication date: December 2, 2010Inventors: Tim Hugo Maria Jonckers, Wim Bert Griet Schepens, Geerwin Yvonne Paul Haché, Beate Sabine Hallenberger, Jennifer Chiyomi Sasaki, Judith Eva Baumeister, Gerben Albert Van 'T Klooster
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Publication number: 20100298340Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.Type: ApplicationFiled: April 12, 2007Publication date: November 25, 2010Applicants: AstraZeneca AB, Astex Therapeutics Ltd.Inventors: Stefan Berg, Karin Kolmodin
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Publication number: 20100286210Abstract: An object of the present invention is to provide novel carbazole derivatives, solvates thereof, or pharmaceutically acceptable salts thereof having an excellent adipose tissue weight reducing effect, hypoglycemic effect, and hypolipidemic effect, which are useful as a preventive and/or therapeutic agent for fatty liver, obesity, lipid metabolism abnormality, visceral adiposity, diabetes, hyperlipemia, impaired glucose tolerance, hypertension, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, and the like.Type: ApplicationFiled: October 28, 2005Publication date: November 11, 2010Applicant: Zeria Pharmaceutical Co., Ltd.Inventors: Masakazu Murata, Yoshihiko Itokazu, Ryu Nakao
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Publication number: 20100267714Abstract: The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.Type: ApplicationFiled: May 4, 2010Publication date: October 21, 2010Inventors: William L. Jorgensen, Richard J. Bucala
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Publication number: 20100267708Abstract: The present invention relates to new compounds of formula (1) exhibiting excellent activity for glucokinase, and pharmaceutical compositions comprising the same as an active ingredient.Type: ApplicationFiled: December 22, 2008Publication date: October 21, 2010Applicant: LG Life Sciences Ltd.Inventors: Soon Ha Kim, Sung Bae Lee, Seung Hyun Yoon, Mi Kyoung Cho, Kyoung Hee Kim, Heui Sul Park, Hyoung Jin Kim
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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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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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Patent number: 7812043Abstract: This invention relates to compounds that are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial. The compounds are of the general formula (I) wherein A and B are further defined in the application.Type: GrantFiled: May 24, 2006Date of Patent: October 12, 2010Assignee: TransTech Pharma, Inc.Inventors: Jesper F Lau, Per Vedsø, János Tibor Kodra, Anthony Murray, Lone Jeppesen, Michael Ankersen, Govindan Subramanian, Adnan M. M. Mjalli, Robert Carl Andrews, Dharma Rao Polisetti, Daniel Peter Christen
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Patent number: 7807690Abstract: A compound represented by the following general formula (1), or a salt thereof has serine protease inhibiting activity, and particularly excellent inhibiting activity against clotting factor VIIa. This compound or a salt thereof is useful as therapeutic and/or prophylactic agents for diseases associated with thrombus formation. [wherein R1 represents hydrogen, R2 represents optionally substituted phenyl, etc., R3 represents optionally substituted C6-10 aryl, etc.].Type: GrantFiled: September 19, 2008Date of Patent: October 5, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Richard Clark, Atsushi Takemura, Nobuhisa Watanabe, Osamu Asano, Tadashi Nagakura, Kimiyo Tabata
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Publication number: 20100233116Abstract: The present invention provides heterocyclic derivatives hat modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: August 13, 2007Publication date: September 16, 2010Inventors: Natalie Dales, Julia Fonarev, Jianmin Fu, Rajender Kamboj, Vishnumurthy Kodumuru, Shifeng Liu, Natalia Pokrovskaia, Vandna Raina, Shaoyi Sun, Zaihui Zhang
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Patent number: 7786137Abstract: Bicyclic derivatives having formula (I) and a composition thereof are useful as ion channel antagonists:Type: GrantFiled: May 8, 2006Date of Patent: August 31, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Aarti S. Kawatkar, Tara M. Whitney, Timothy D. Neubert, Nicole Zimmermann, Andreas Termin, Esther Martinborough
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Patent number: 7786153Abstract: Novel compounds of formula 1 or a pharmaceutically acceptable salt thereof inhibit cytochrome P450 monooxygenase.Type: GrantFiled: March 2, 2006Date of Patent: August 31, 2010Assignee: Abbott Laboratories Inc.Inventors: Dale J. Kempf, Charles A. Flentge, John T. Randolph, Peggy Huang, Larry L. Klein
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Publication number: 20100210647Abstract: The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole compounds as an active ingredient.Type: ApplicationFiled: August 18, 2008Publication date: August 19, 2010Applicant: LG Life Sciences Ltd.Inventors: Soon Ha Kim, Hyoung Jin Kim, Sun Young Koo, Sung Bae Lee, Heui Sul Park, Seung Hyun Yoon, Seung Yup Paek, Hyo Shin Kwak, Dong Ook Seo, Eok Park
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Publication number: 20100197630Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are potent CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In formula I, A-B is an arylamide moiety.Type: ApplicationFiled: June 16, 2008Publication date: August 5, 2010Inventors: Julianne A. Hunt, Rogelio L. Martinez, Peter J. Sinclair, Ramzi F. Sweis
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Patent number: 7767432Abstract: The present invention relates to improved methods for the production, isolation and purification of epothilone B. These methods include, for example, a fermentation process for the production of epothilone B, isolation via adsorption onto a resin, and subsequent purification.Type: GrantFiled: January 31, 2007Date of Patent: August 3, 2010Assignee: Bristol-Myers Squibb CompanyInventor: Brian L. Davis
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Publication number: 20100184808Abstract: The invention relates to 3-aza-bicyclo[3.3.0]octane derivatives of the formula (I) wherein R1, R2, R3, and A are as described in the description and their use as orexin receptor antagonists.Type: ApplicationFiled: July 2, 2008Publication date: July 22, 2010Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
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Patent number: 7759372Abstract: A compound of the formula (I): wherein Z4, Z5 and Z9 each is independently carbon atom or nitrogen atom; Y is hydroxy, mercapto or amino; RA is a group of the formula: (wherein C ring is nitrogen-containing heteroaryl) has an inhibitory activity against integrase.Type: GrantFiled: August 8, 2006Date of Patent: July 20, 2010Assignee: Shionogi & Co., Ltd.Inventors: Masahiro Fuji, Hidenori Mikamiyama, Hitoshi Murai
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Patent number: 7758861Abstract: The present invention discloses dye-sulfenate derivatives and their bioconjugates for dual phototherapy of tumors and other lesions. The compounds of the present invention may contain either a mixture of Type 1 and Type 2 agents or a single entity that integrates both units in the same molecules. The compounds are designed to produce both Type 1 and Type 2 phototherapeutic effect at once using dual wavelength light source that will produce singlet oxygen and free radicals at the lesion of interest.Type: GrantFiled: March 21, 2006Date of Patent: July 20, 2010Assignee: Mallinckrodt Inc.Inventors: Raghavan Rajagopalan, Samuel I. Achilefu, Joseph E. Bugaj, Richard D. Dorshow
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Publication number: 20100179122Abstract: Compounds of Formula (I): are HIV reverse transcriptase inhibitors, wherein R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula (I) and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: June 23, 2006Publication date: July 15, 2010Inventors: Craig W. Lindsley, William H. Leister, Scott E. Wolkenberg
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Publication number: 20100168182Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly TrkA, TrkB, TrkC, PDGFR and c-kit.Type: ApplicationFiled: December 11, 2007Publication date: July 1, 2010Applicant: IRM LLCInventors: Yuan Mi, Pamela Albaugh, Yi Fan, Ha-Soon Choi, Zuosheng Liu, Shenlin Huang
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Publication number: 20100168101Abstract: The present invention is related to the use of oxindole hydrazide derivatives of formula (I) for the treatment and/or prevention of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, obesity, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of oxindole hydrazide derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs, in particular of PTP1B, TC-PTP, SHP and GLEPP-1. The present invention is furthermore related to novel oxindole hydrazide derivatives and method of preparation thereof.Type: ApplicationFiled: December 23, 2009Publication date: July 1, 2010Applicant: APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.Inventors: Agnes BOMBRUN, Patrick Gerber, Dennis Church
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Publication number: 20100166881Abstract: Novel indoleamine 2,3-dioxygenase (IDO) inhibitors, compositions comprising the same, and methods of use thereof are disclosed.Type: ApplicationFiled: March 11, 2010Publication date: July 1, 2010Inventors: George C. Prendergast, William P. Malachowski, Alexander J. Muller, James B. DuHadaway
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Publication number: 20100152191Abstract: The present invention is directed to cyclopropyl proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: ApplicationFiled: May 19, 2008Publication date: June 17, 2010Inventors: Paul J. Coleman, Swati P. Mercer, Anthony J. Roecker
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Publication number: 20100144594Abstract: The invention relates to heterocyclic derivatives of formula I wherein R, R1, A, B, D, M, L and n are as defined herein, or their physiologically compatible salts, their pharmaceutical compositions and their uses as SCD1 inhibitors.Type: ApplicationFiled: October 26, 2009Publication date: June 10, 2010Applicant: SANOFI-AVENTISInventors: Gerhard ZOLLER, Marc Dietrich VOSS, Stefanie KEIL, Andreas HERLING, Hans MATTER
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Patent number: 7700621Abstract: This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula (I) in which R1a, R1b, R2a, R3a, R3b, R4, R5, R6, R7, A, Y, D, E, G, Y and Z have the meanings that are indicated in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and thus find use in treating diseases or conditions associated with the need for cell growth, division and/or proliferation. Thus the compounds are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanoma, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (such as psoriasis, arthritis). Methods of use and preparation of the compounds are also described.Type: GrantFiled: August 31, 2005Date of Patent: April 20, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Ulrich Klar, Wolfgang Schwede, Werner Skuballa, Bernd Buchmann, Jens Hoffmann, Rosemarie Lichtner
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Publication number: 20100076014Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, wherein (Ia) is heterocycle or heteroaryl; J, Ja, E, F, G, Ma, M, Q, Za and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases and obesity and diabetes employing said compounds.Type: ApplicationFiled: October 31, 2007Publication date: March 25, 2010Inventors: James E. Sheppeck, John l. Gilmore, T.G. Murali Dhar, Hai-Yun Xiao
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Publication number: 20100069404Abstract: The present invention provides a compound of the formula: Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly reduced bones mass, osteoporosis, osteopenia, or reduced muscle mass or strength, comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt thereof. X-17142.Type: ApplicationFiled: November 6, 2007Publication date: March 18, 2010Inventors: Konstantinos Gavardinas, Jonathan Edward Green, Prabhakar Kondaji Jadhav, Donald Paul Matthews
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Patent number: 7672217Abstract: The present invention provides an optical recording medium that includes a recording layer composed mainly of an organic compound and can utilize blue-violet semiconductor laser light (390 to 420 nm in wavelength) as recording/reproducing laser light. The present invention also provides an optical recording/reproducing method using the optical recording medium. The optical recording medium 1 comprises at least a supporting substrate 2; a recording layer 3 on the supporting substrate 2, the recording layer 3 containing an organic compound as a major component; and a light-transmitting layer 5 on the recording layer 3, the light-transmitting layer 5 being capable of transmitting laser light with a wavelength of 390 to 420 nm for recording and reproducing information.Type: GrantFiled: September 9, 2003Date of Patent: March 2, 2010Assignee: TDK CorporationInventor: Narutoshi Fukuzawa
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Publication number: 20100016371Abstract: The present application relates to compounds of formula (I) or a pharmaceutically acceptable derivative thereof; wherein X, R1, R2, and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.Type: ApplicationFiled: July 9, 2007Publication date: January 21, 2010Applicant: Glaxo Group LimitedInventors: Gerard Martin Paul Giblin, Adrian Hall, David Nigel Hurst, Tiziana Scoccitti, Pamela Joan Theobald
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Publication number: 20090324544Abstract: 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. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: June 11, 2009Publication date: December 31, 2009Inventors: Yao-Ling Qiu, Ce Wang, Jiang Long, Lu Ying, Yat Sun Or
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Publication number: 20090326019Abstract: 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. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: June 11, 2009Publication date: December 31, 2009Inventors: Yat Sun Or, Jiang Long, Ce Wang, Lu Ying, Yao-Ling Qiu
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Publication number: 20090318440Abstract: Carbonylamino Pyrrolopyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4.Type: ApplicationFiled: December 12, 2006Publication date: December 24, 2009Inventors: Junhu Zhang, Anle Yang, Susan Elizabeth Kephart, Liming Dong, Chuangxing Guo, Yufeng Hong, Mary Catherine Johnson, Indrawan James Mc Alpine, Jayashree Tikhe, Haitao Li
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Publication number: 20090291970Abstract: The invention provides compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: ApplicationFiled: July 27, 2009Publication date: November 26, 2009Inventors: James P. Beck, Matthew Drowns, Martha A. Warpehoski
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Patent number: 7622592Abstract: Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient.Type: GrantFiled: October 28, 2003Date of Patent: November 24, 2009Assignee: Merck & Co., Inc.Inventors: Yuntae Kim, Barbara Hanney, Mark E. Duggan, Keith L. Spencer
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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: 20090286775Abstract: New bicyclic derivatives of formula (I), wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors.Type: ApplicationFiled: June 28, 2006Publication date: November 19, 2009Applicant: PALAU PHARMA, S.A.Inventors: Carmen Almansa Rosales, Marina Virgili Bernadó
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Patent number: 7605174Abstract: The present invention relates to indane derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: June 9, 2006Date of Patent: October 20, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Timothy Neubert, Aarti S. Kawatkar, Esther Martinborough, Andreas Termin
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Publication number: 20090247746Abstract: The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof. According to the present invention, a glucokinase activator useful as a pharmaceutical agent such as agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like can be provided.Type: ApplicationFiled: April 20, 2006Publication date: October 1, 2009Inventors: Tsuneo Yasuma, Osamu Ujikawa, Hidehisa Iwata
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Patent number: 7576079Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein; ?represents either a single or a double bond; R2 is selected from 6 or 10-membered aryl and Het, each optionally substituted with R20; provided that Het is not a 5- or 6-membered monocyclic heterocycle having 1 or 2 nitrogen heteroatoms; B is NR3 or CR3, with the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein; K is N or CR4, wherein R4 is defined herein; L is N or CR5, wherein R5 has the same definition as R4; M is N or CR7, wherein R7 has the same definition as R4; Y1 is O or S; Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; and R6 is H, alkyl, cycloalkyl, alkenyl, Het, alkyl-aryl, alkyl-Het; or R6 is wherein R7 and R8 and Q are as defined herein; Y2 is O or S; R9 is H, (C1-6 alkyl), (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl, aryl, Het, (C1-6)alkyl-arylType: GrantFiled: January 17, 2006Date of Patent: August 18, 2009Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Pierre Louis Beaulieu, Gulrez Fazal, Sylvie Goulet, George Kukolj, Martin Poirier, Youla S. Tsantrizos, James Gillard, Marc-Andre Poupart
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Publication number: 20090202920Abstract: The present invention provides an optical recording composition comprising at least one optical recording compound selected from the group consisting of cyanine compounds having specific structures and a holographic recording medium comprising a recording layer, wherein the recording layer comprises at least one optical recording compound selected from the group consisting of cyanine compounds having specific structures.Type: ApplicationFiled: February 10, 2009Publication date: August 13, 2009Applicant: FUJIFILM CorporationInventor: Hiroyuki SUZUKI