Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 546/118)
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Patent number: 7816369Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.Type: GrantFiled: November 3, 2005Date of Patent: October 19, 2010Assignees: Curis, Inc., Genentech, Inc.Inventors: Oivin M. Guicherit, Edward Andrew Boyd, Judith Boyd, legal representative, Shirley Ann Brunton, Stephen Price, John Harry Alexander Stibbard, Colin H. MacKinnon
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Publication number: 20100260715Abstract: 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: March 1, 2010Publication date: October 14, 2010Inventors: Yat Sun Or, Ce Wang, Lu Ying, Xiaowen Peng, Yao-Ling Qiu
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Publication number: 20100261909Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct copper catalyzed regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.Type: ApplicationFiled: December 22, 2009Publication date: October 14, 2010Applicant: sanofi-aventisInventors: Jorge ALONSO, Andreas LINDENSCHMIDT, Marc NAZARÉ, Matthias URMANN, Nis HALLAND, Omar RKYEK
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Patent number: 7807684Abstract: Compounds having the structure: are HIV reverse transcriptase inhibitors, wherein A, X, Y, Z, R1 and R2 are defined herein. The compounds 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: GrantFiled: July 17, 2006Date of Patent: October 5, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Sandeep A. Saggar, John T. Sisko, Thomas J. Tucker, Robert M. Tynebor, Dai-Shi Su, Neville J. Anthony
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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: 20100249181Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: ApplicationFiled: June 10, 2010Publication date: September 30, 2010Applicant: ABBOTT LABORATORIESInventors: David A. DeGoey, Charles A. Flentge, William J. Flosi, David J. Grampovnik, Dale J. Kempf, Larry L. Klein, Ming C. Yeung, John T. Randolph, Xiu C. Wang, Su Yu
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Patent number: 7799801Abstract: Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I wherein R1, R1?, R2, R3, R4, Xa, Y, Z and n are as described herein. The compounds provided herein are useful in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.Type: GrantFiled: July 22, 2009Date of Patent: September 21, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Guixue Yu, Jun Li, William R. Ewing, Richard B. Sulsky, James J. Li, Joseph Anthony Tino
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Patent number: 7799806Abstract: This invention relates to compounds of the formula wherein A, R1 to R3 are as defined in the claims and G is benzoimidazole, quinoxaline, benzotriazole, dihydro-imidazo[4,5-c]pyridinone and dihydro-isoindolone group as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5 such as diabetes mellitus.Type: GrantFiled: March 24, 2008Date of Patent: September 21, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Konrad Bleicher, Andreas D. Christ, Rainer E. Martin, Peter Mohr
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Patent number: 7799800Abstract: Lipid-modified immune response modifier compounds, pharmaceutical compositions containing the compounds and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: GrantFiled: August 12, 2004Date of Patent: September 21, 2010Assignee: 3M Innovative Properties CompanyInventor: Paul D. Wightman
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Publication number: 20100234593Abstract: The present invention relates to new compounds of formula (I) as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.Type: ApplicationFiled: March 28, 2008Publication date: September 16, 2010Applicant: ASTRAZENECA ABInventors: Per Arvidsson, Jeremy Burrows, Peter Soderman, Ulrika Yngve
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Publication number: 20100234601Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional 2H-indazoles or 2H-azaindazoles of the formula (I) from 2-halo-phenylacetylenes or (2-sulfonato)phenylacetylenes and monosubstituted hydrazines.Type: ApplicationFiled: December 22, 2009Publication date: September 16, 2010Applicant: SANOFI-AVENTISInventors: Nis HALLAND, Marc NAZARE, Andreas LINDENSCHMIDT, Jorge ALONSO, Omar RKYEK, Matthias URMANN
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Patent number: 7795276Abstract: The compound 5-((3-(2,4-trifluoromethyphenyl)isoxazol-5-yl)methyl)-2 -(2-fluorophenyl)-5H-imidazo[4,5-c]pyridine, together with the salts and solvates thereof. Also provided are compositions comprising this compound and pharmaceutically acceptable carriers, as well as the use of such compositions in the treatment or prophylaxis of viral infections.Type: GrantFiled: January 30, 2008Date of Patent: September 14, 2010Assignees: Gilead Sciences, Inc., K.U. Leuven Research & DevelopmentInventors: Steven S. Bondy, David A. Oare, Winston C. Tse
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Patent number: 7790729Abstract: The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: May 19, 2006Date of Patent: September 7, 2010Assignee: Methylgene Inc.Inventors: Oscar Mario Saavedra, Stephen William Claridge, Lijie Zhan, Franck Raeppel, Arkadii Vaisburg, Stephane Raeppel, Robert Deziel, Michael Mannion, Nancy Z. Zhou, Ljubomir Isakovic
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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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Patent number: 7790710Abstract: The compounds of formula (I) in which R1, R11 and A have the meanings as given in the description are novel effective iNOS inhibitors.Type: GrantFiled: March 29, 2006Date of Patent: September 7, 2010Assignee: NYCOMED GmbHInventors: Thomas Fuchss, Andreas Strub, Wolf-Rüdiger Ulrich, Christian Hesslinger, Martin Lehner, Raimund Külzer, Rainer Boer, Manfrid Eltze
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Patent number: 7790740Abstract: The present invention provides compounds of formula (I) wherein R1 and R2 are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.Type: GrantFiled: August 27, 2007Date of Patent: September 7, 2010Assignee: Pfizer IncInventor: Paul Anthony Stupple
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Patent number: 7790891Abstract: A process for the preparation of a compound of formula (I), or a salt thereof, wherein Q is ?CR8— or ?N—; and R1-R8 are as herein defined; comprising the reaction of a compound of formula (II), or a salt thereof, wherein Q, R1-R7 are as herein defined; with a reducing agent selected from a trivalent phosphorous compound, an oxidizable solvent and a sulfonic acid chloride; and, if desired, the conversion of a compound of formula (I) to another compound of formula (I) or a salt thereof.Type: GrantFiled: October 29, 2007Date of Patent: September 7, 2010Assignee: Dipharma Francis S.R.L.Inventors: Pietro Allegrini, Marcello Rasparini, Gabriele Razzetti, Simone Mantegazza, Vittorio Lucchini, Alberto Bologna
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Publication number: 20100222345Abstract: This invention relates to novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy.Type: ApplicationFiled: August 8, 2007Publication date: September 2, 2010Inventors: Caroline Jean Diaz, Curt Dale Haffner, Jason Daniel Speake, Cunyu Zhang, Wendy Yoon Mills, Paul Kenneth Spearing, David John Cowan, Gary Martin Green
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Patent number: 7786120Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: August 25, 2006Date of Patent: August 31, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Sharn Ramaya, Steven Durrant, Juan-Miguel Jimenez, Julian M. C. Golec, Michael Mortimore
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Patent number: 7786113Abstract: Objects of the present invention are the compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.Type: GrantFiled: December 22, 2005Date of Patent: August 31, 2010Assignee: Hoffman-La Roche Inc.Inventors: Konrad Honold, Klaus Kaluza, Birgit Masjost, Wolfgang Schaefer, Stefan Scheiblich
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Publication number: 20100216760Abstract: Disclosed herein are cannabinoid receptor ligands of formula (I) wherein L1, A1, R1g, z, R2, R3, and R4 are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.Type: ApplicationFiled: December 16, 2009Publication date: August 26, 2010Applicant: ABBOTT LABORATORIESInventors: Jennifer M. Frost, Steven P. Latshaw, Michael J. Dart, William A. Carroll, Arturo Perez-Medrano, Teodozyj Kolasa, Meena V. Patel, Derek W. Nelson, Tongmei Li, Sridhar Peddi, Xueqing Wang, Bo Liu
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Publication number: 20100217000Abstract: A method for the preparation of a compound of formula (1) or a pharmaceutically acceptable salt or solvate thereof; from a compound of the formula: (IV); wherein L represents a leaving group.Type: ApplicationFiled: December 15, 2009Publication date: August 26, 2010Inventors: Michael Butters, Richard Wisedale, Matthew James Welham, Colin Thomson, Andrew Watts
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Patent number: 7781452Abstract: A compound represented by the following general formula (1), or a salt or hydrate thereof: [Formula 1] wherein R1 represents a C1-C6 alkyl group or C2-C6 alkynyl group which may be substituted, or a phenyl group which may be substituted, R2 represents a hydrogen atom or a C1-C6 alkyl group, R3 represents methyl or ethyl group, R4 represents a C1-C6 alkyl group, R5 represents a hydrogen atom, provided that a compound wherein R1 is a C1-C6 alkyl group unsubstituted or substituted with a halogen atom and R2 is a hydrogen atom is excluded.Type: GrantFiled: March 22, 2006Date of Patent: August 24, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Shuhei Miyazawa, Hitoshi Harada, Hideaki Fujisaki, Atsuhiko Kubota, Kotaro Kodama, Junichi Nagakawa, Kiyoshi Oketani, Nobuhisa Watanabe
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Patent number: 7776878Abstract: Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.Type: GrantFiled: July 28, 2006Date of Patent: August 17, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Edward Boyd, Frederick Brookfield, Jonathan Gridley, Konrad Honold, Raymond Lau, Stefan Scheiblich
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Publication number: 20100204246Abstract: The present invention relates to compounds of Formula (I) and to their pharmaceutical compositions, and to their methods of use. These novel compounds provide a treatment for myeloproliferative disorders and cancer.Type: ApplicationFiled: April 17, 2008Publication date: August 12, 2010Applicant: AstraZeneca ABInventors: Audrey Davies, Stephanos Ioannidis, Michelle Lamb, Tao Wang, Hai-Jun Zhang
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Patent number: 7772226Abstract: The present invention is related to compounds represented by the following formula, or salts or hydrates thereof wherein, T1 represents a 4- to 12-membered heterocyclic group containing one or two nitrogen atoms in the ring, which is a monocyclic or bicyclic structure that may have one or more substituents; X represents a C1-6 alkyl group which may have one or more substituents, or such; Z1 and Z2 each independently represent a nitrogen atom or a group represented by the formula —CR2—; R1 and R2 independently represent a hydrogen atom, a C1-6 alkyl group which may have one or more substituents, or a C1-6 alkoxy group which may have one or more substituents, or such. These are novel compounds that exhibit an excellent DPPIV-inhibiting activity.Type: GrantFiled: August 28, 2008Date of Patent: August 10, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Seiji Yoshikawa, Eita Emori, Fumiyoshi Matsuura, Richard Clark, Hironori Ikuta, Kazunobu Kira, Nobuyuki Yasuda, Tadashi Nagakura, Kazuto Yamazaki
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Patent number: 7767673Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-Oxide thereof, are useful in the treatment of cancer.Type: GrantFiled: September 12, 2008Date of Patent: August 3, 2010Assignee: OSI Pharmaceuticals, Inc.Inventors: Arlindo L. Castelhano, Andrew P. Crew, Han-Qing Dong, Radoslaw Laufer, An-Hu Li, Li Qiu, Colin Peter Sambrook Smith, Tao Zhang
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Publication number: 20100190777Abstract: Compounds of formula I active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. Formula (I) wherein Ar is optionally substituted heteroaryl; R2 is hydrogen, lower alkyl or halogen; U is selected from the group consisting of —S(O)2—, —C(X)—, —C(X)—N(R10)—, and —S(O)2—N(R10)—; R3 is optionally substituted lower alkyl, optionally substituted C3.6 cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl or optionally substituted heteroaryl; and wherein R1, R3, R4, m, L1, X R10 are as described herein.Type: ApplicationFiled: July 16, 2008Publication date: July 29, 2010Applicant: PLEXXIKON INC.Inventors: Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
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Publication number: 20100190780Abstract: The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.Type: ApplicationFiled: February 9, 2010Publication date: July 29, 2010Inventors: Christian Laggner, Maria Rosa Cuberes-Altisent, Joerg Holenz, Juana Maria Berrocal-Romero, Maria Montserrat Contijoch-LLobet
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Publication number: 20100190820Abstract: 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 the group X is O or (Rx)(Ry); is heterocyclo or heteroaryl; E is —N—, —NR1—, —O—, —C(?O), —S—, —SO2—, or —CR2—; F is —N—, —NR1a, —O—, —C(?O), —S—, —SO2—, or —CR2a—; G is independently N, —NR1b—, —O—, —C(?O), —S—, —SO2— or —CR2b— provided that the heterocyclic ring formed does not contain a S—S or S—O bond and at least one of E, F and G is a hetero atom; and Ma, Rx, Ry, R1, R1a, R1b, R2, R2a, R2b, R4, R5a, R6, R7, X, Za and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases employing said compounds.Type: ApplicationFiled: October 31, 2007Publication date: July 29, 2010Inventors: T. G. Murali Dhar, Hai-Yun Xiao, James E. Sheppeck
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Publication number: 20100183552Abstract: Inhibitors of RSV replication of formula (I) which can be represented by formula (I) the salts and stereochemically isomeric forms thereof, wherein R is a radical of formula Q is hydrogen or C1-6alkyl optionally substituted with a heterocycle or Q is C1-6alkyl substituted with both a radical —OR4 and a heterocycle; Alk is C1-6alkanediyl; X is O or S; -a1=a2-a3=a4- is —N?CH—CH?CH—, —CH?N—CH?CH—, —CH?CH—N?CH— or —CH?CH—CH?N—; R1 is Ar or a heterocycle; R2 is hydrogen, C1-6alkyl, substituted C1-6alkyl, C3-7cycloalkyl; R3 is hydrogen, C1-6alkyl, cyano, aminocarbonyl, polyhaloC1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4 is hydrogen or C1-6alkyl; Ar is phenyl or substituted phenyl; Het is a heterocycle; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).Type: ApplicationFiled: June 20, 2006Publication date: July 22, 2010Inventors: Jean-François Bonfanti, Philippe Muller, Jérôme Michel Claude Fortin, Frédéric Marc Maurice Doublet
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Publication number: 20100184761Abstract: The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.Type: ApplicationFiled: January 13, 2010Publication date: July 22, 2010Inventors: John Stephen Robinson, Philip Stephen Jones, Jiaqiang Cai, David Jonathan Bennett
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Publication number: 20100168093Abstract: The present invention relates to substituted pyrrolidine compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animal.Type: ApplicationFiled: April 30, 2007Publication date: July 1, 2010Inventors: Miguel Angel Pericas-Brondo, Antoni Torrens-Jover, Susana Yenes-Minguez, Félix Cuevas Cordobés, Carmen Garcia Granda
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Publication number: 20100168088Abstract: The present invention relates to a compound of formula I wherein Ar1, Ar2, R1, R2, R3, n, o, and p are as described herein or to a pharmaceutically active salt, to all stereoisomeric forms, including individual diastereoisomers and enantiomers as well as to racemic and non-racemic mixtures thereof. Compounds of the invention 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: ApplicationFiled: October 2, 2009Publication date: July 1, 2010Inventors: Caterina Bissantz, Philippe Jablonski, Henner Knust, Matthias Nettekoven, Angélique Patiny-Adam, Hasane Ratni, Claus Riemer
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Publication number: 20100168159Abstract: [Problems] To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 agonist activity.Type: ApplicationFiled: January 29, 2010Publication date: July 1, 2010Applicant: ASTELLAS PHARMA INC.Inventors: Hironori Harada, Kazuyuki Hattori, Kazuya Fujita, Masataka Morita, Sunao Imada, Yoshito Abe, Hiromichi Itani, Tatsuaki Morokata, Hideo Tsutsumi
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Publication number: 20100168100Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.Type: ApplicationFiled: May 16, 2008Publication date: July 1, 2010Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Nicholas D. Adams, Amita M. Chaudhari
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Publication number: 20100152230Abstract: Hydroxy substituted 1H-imidazo[4,5-c]pyridin-4-amines, with a hydroxy substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: September 1, 2006Publication date: June 17, 2010Inventors: Joseph F. Dellaria, JR., William H. Moser, Matthew R. Radmer, George W. Gries-Graber
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Publication number: 20100145054Abstract: The present invention is directed to a novel imidazole derivative having an aryl piperidine substituent of formula (I) and a method for preparation thereof, and a pharmaceutical composition containing said imidazole derivative as an active ingredient for preventing or treating a MCH (melanine-concentrating hormone)-related disease.Type: ApplicationFiled: May 13, 2008Publication date: June 10, 2010Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Jee Hee Suh, Kyu Yang YI, Nack Jeong KIM, Sung Eun Yoo, Kwang-Seok Oh, Hyae Gyeong Cheon, Mija Ahn, Byung Ho Lee, Won Hoon Jung, Sang Dal Rhee
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Publication number: 20100125062Abstract: Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: November 16, 2009Publication date: May 20, 2010Applicant: AMEN INC.Inventors: Jennifer R. Allen, Kaustav Biswas, Frank Chavez, Jr., Ning Chen, Frenel Fils Demorin, James R. Falsey, Mike Frohn, Paul Harrington, Dan Horne, Essa Hu, Matthew R. Kaller, Roxanne Kunz, Holger Monenschein, Tom Nguyen, Alex Pickrell, Andreas Reichelt, Shannon Rumfelt, Rob Rzasa, Kelvin Sham, Guomin Yao
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Publication number: 20100120841Abstract: Provided is an ORL-1 receptor agonist having improved bioavailability based on superior metabolic stability and strong and high selectivity, as compared to conventional compounds. A compound represented by the formula (I) wherein each symbol is as defined in the claims.Type: ApplicationFiled: February 28, 2008Publication date: May 13, 2010Inventors: Masakazu Nakano, Masanori Minoguchi, Tokushi Hanano, Shin-ichiro Ono, Hideki Horiuchi, Koji Teshima
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Publication number: 20100120840Abstract: Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.Type: ApplicationFiled: July 28, 2006Publication date: May 13, 2010Inventors: Edward Boyd, Frederick Brookfield, Jonathan Gridley, Konrad Honold, Raymond Lau, Stefan Scheiblich
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Publication number: 20100112090Abstract: [Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. [Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, —OW1, —SW1, —COW2, —NW3W4, —SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, —CO—Y, —SO2—Y, —S-(alkylene)-Y, —O-(alkylene)-Y, —SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.Type: ApplicationFiled: April 16, 2008Publication date: May 6, 2010Applicant: KISSEI PHARMACEUTICAL CO., LTDInventors: Shigeru Yonekubo, Takashi Miyagi, Kohsuke Ohno, Mikie Kambara, Nobuhiko Fushimi
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Patent number: 7709488Abstract: The compounds of formula (I) in which R1, R2, R3, R4, R5 and A have the meanings as given in the description are novel effective iNOS inhibitors.Type: GrantFiled: September 27, 2007Date of Patent: May 4, 2010Assignee: Altana Pharma AGInventor: Wolf-Ruediger Ulrich
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Publication number: 20100105723Abstract: The present disclosure relates to compounds of formula (I): or a pharmaceutically acceptable salt or N-oxide thereof. The present disclosure also relates to pharmaceutical compositions comprising the compounds of formula (I), and to their methods of treatment.Type: ApplicationFiled: November 23, 2007Publication date: April 29, 2010Inventors: Jose Aiguade Bosch, Ines Carranco Moruno, Bernat Vidal Juan
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Publication number: 20100105719Abstract: The present invention relates to imidazolidinecarboxamide derivatives of the general formula I, wherein R, R1, R2, X and Y are as defined herein, or pharmaceutically usable salts thereof and the use thereof as medicinal substances.Type: ApplicationFiled: October 2, 2009Publication date: April 29, 2010Applicant: SANOFI-AVENTISInventors: Gerhard ZOLLER, Stefan PETRY, Gunter MÜLLER, Norbert TENNAGELS
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Patent number: 7700616Abstract: The present invention provides compounds and amyloid probes thereof that allow for an antemortem method of diagnosing AD and quantitating the extent or progression of amyloid deposits (plaques) by in vivo imaging of amyloid and/or amyloid deposits in the regions of the brain. Preferably, an amyloid probe of the invention can cross the blood-brain barrier and distinguish AD brain from normal brain. An amyloid probe can be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits. Amyloid probes of the invention can also be used to detect and quantitate amyloid deposits in diseases including, without limitation, Down's syndrome, familial AD and homozygotes for the apolipoprotein E4 allele. In one aspect, the compounds may be used in the treatment or prophylaxis of diseases that include, without limitation, AD and type 2 diabetes mellitus.Type: GrantFiled: May 8, 2007Date of Patent: April 20, 2010Assignee: Molecular Neuroimaging, LLC.Inventors: Gilles D. Tamagnan, David Alagille, Herve Da Costa
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Patent number: 7700618Abstract: This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein A, R1, R2, R3, R4, R5, m and n are each as described herein, and compositions containing such compounds, and the use of such compounds in the treatment of a condition mediated by CB2 receptor activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asType: GrantFiled: February 23, 2007Date of Patent: April 20, 2010Assignee: Pfizer IncInventors: Tomoki Kato, Kana Kon-I, Yohei Yuki, Kazuo Ando
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Publication number: 20100093767Abstract: The invention relates to inhibitors of enzymes that disrupt the assembly and function of the mitotic spindle, compositions comprising the inhibitors of Formula (I), kits and articles of manufacture comprising the inhibitors and inhibitor compositions, and methods of using the inhibitors and inhibitor compositions. The inhibitors and inhibitor compositions are useful for treating, preventing or modulating diseases in which mitotic kinesins, including kinesin-like spindle protein (KSP), may be involved; symptoms of such diseases; or the effect of other physiological events mediated by mitotic kinesins, including KSP.Type: ApplicationFiled: December 2, 2005Publication date: April 15, 2010Applicant: TAKEDA SAN DIEGO, INC.Inventors: Jerome C. Bressi, Andrew John Jennings, Stephen W. Kaldor, Lily Kwok, Clifford D. Mol, Jeffrey A. Stafford
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Publication number: 20100093788Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein W1, W2, W3, R1, R1a, R2, R2a, R3, V, Q, and X are defined herein.Type: ApplicationFiled: October 9, 2009Publication date: April 15, 2010Inventors: Mark R. Player, Daniel J. Parks, William Parsons, Senath K. Meegalla, Carl R. Illig, Shelley K. Ballentine
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Patent number: 7696224Abstract: Compounds of the formula (I), in which R1a—R1e, R2a, R2b, R3 and X have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours.Type: GrantFiled: September 16, 2005Date of Patent: April 13, 2010Assignee: Merck Patent GmbHInventors: Wolfgang Staehle, Guenter Hoelzemann, Wilfried Rautenberg