The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Tricyclo Ring System Patents (Class 544/126)
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Publication number: 20090264399Abstract: The invention relates to compound of the formula (I) or its salt, wherein —R1, —R2, —R3, —R4, —R5, -M-, —X— and —Y? are as defined in the description, their use of as, medicament, the process for their preparation and use for the treatment of JAK3 mediated diseases.Type: ApplicationFiled: July 13, 2006Publication date: October 22, 2009Applicant: Astellas Pharma Inc.Inventors: Takayuki Inoue, Takashi Tojo, Masataka Morita, Yutaka Nakajima, Keiko Hatanaka, Shohei Shirakami, Hiroshi Sasaki, Akira Tanaka, Fumie Takahashi, Koichiro Mukoyoshi, Yasuyuki Higashi, Akira Okimoto, Takeshi Hondo, Hitoshi Sawada
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Publication number: 20090258852Abstract: The instant invention provides for compounds which comprise benzoisoquinolinones and aza derivatives that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: June 30, 2006Publication date: October 15, 2009Inventors: Kenneth L. Arrington, Vadim Y. Dudkin, Mark E. Fraley, Robert M. Garbaccio, George D. Hartman, Shaei Y. Huang, Constantine Kreatsoulas, Edward S. Tasber
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Publication number: 20090253695Abstract: Certain imidazonaphthyridines with a hydroxymethyl or hydroxyethyl substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for preferentially inducing IFN-? biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: ApplicationFiled: February 22, 2006Publication date: October 8, 2009Applicant: Coley Pharmaceutical Group, Inc,Inventors: Tushar A. Kshirsagar, Scott E. Langer, Shri Niwas, George W. Griesgraber, Philip D. Heppner, Kyle J. Lindstrom
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Publication number: 20090239859Abstract: The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate Pim kinase activity and/or FMS-like tyrosine kinase (Flt) activity. The invention also relates in part to methods for using such molecules.Type: ApplicationFiled: March 2, 2009Publication date: September 24, 2009Inventors: Peter C. CHUA, Mustapha Haddach, Johnny Y. Nagasawa, Fabrice Pierre, Jeffrey P. Whitten
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Publication number: 20090227571Abstract: Provided herein are compounds that bind to androgen receptors and modulate the activity and/or the amount of androgen receptors and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.Type: ApplicationFiled: June 30, 2006Publication date: September 10, 2009Inventors: Jon C. Loren, Todd Miller, Bijan Pedram, Charlene V. Rowley, Yixing Shen, Cornelis Arjan Van Oeveren, Lin Zhi
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Publication number: 20090227561Abstract: The present invention provides a compound having a superior Smo inhibitory activity and lower toxicity, which is sufficiently satisfactory as a pharmaceutical product. The present invention provides a compound represented by the formula wherein ring A is 5- to 7-membered ring optionally having substituent(s), where substituents are optionally bonded to each other to form a ring; X is O, S or NR1 (R1 is a hydrogen atom or a hydrocarbon group optionally having substituent(s)); R2 is carbamoyl optionally having substituent(s); and R3 is hydroxy optionally having substituent(s), or a salt thereof.Type: ApplicationFiled: February 25, 2009Publication date: September 10, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Nobuhiro FUJII, Yuya OGURO, Satoshi SASAKI, Shigeru KONDO
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Publication number: 20090221556Abstract: 1H-Imidazo[4,5-c]quinolin-4-amines with a hydroxy, alkoxy, hydroxyalkoxy, or alkoxyalkoxy 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: November 3, 2006Publication date: September 3, 2009Inventors: Tushar A. Kshirsagar, Philip D. Heppner, Scott E. Langer
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Patent number: 7576209Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: GrantFiled: December 4, 2007Date of Patent: August 18, 2009Assignee: Merck & Co., Inc.Inventors: Michael J. Kelly, III, Mark E. Layton, Philip E. Sanderson
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Publication number: 20090203684Abstract: The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine derivatives of formula (I) that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: ApplicationFiled: July 6, 2007Publication date: August 13, 2009Inventors: Christopher J. Dinsmore, Matthew H. Katcher, Alan B. Northrup
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Publication number: 20090156557Abstract: Compounds are provided for use with kinases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: April 15, 2008Publication date: June 18, 2009Applicant: TAKEDA SAN DIEGO, INC.Inventors: Jason W. Brown, Qing Dong, Bheema R. Paraselli, Jeffrey A. Stafford, Xianchang Gong, Yan Liu, Nicholas Scorah, Michael B. Wallace
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Publication number: 20090131423Abstract: The present invention relates to imidazo[1,2-a]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: ApplicationFiled: October 18, 2006Publication date: May 21, 2009Applicant: MERCK & CO., INC.Inventors: Christopher J. Dinsmore, Ana Esther Gabarda Ortega, Jongwon Lim, Michelle R. Machacek, Alan B. Northrup, Jonathan R. Young
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Publication number: 20090124611Abstract: Pyrazolopyridine-1,4-diamines and analogs thereof, e.g., pyrazolo[3,4-c]pyridine-1,4-diamines, pyrazolo[3,4-c]quinoline-1,4-diamines, 6,7,8,9-tetrahydro pyrazolo[3,4-c]quinoline-1,4-diamines, and pyrazolo[3,4-c]naphthyridine-1,4-di-amines, pharmaceutical compositions containing the compounds, intermediates, methods of making these compounds, 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: March 31, 2006Publication date: May 14, 2009Applicant: Coley Pharmaceutical Group, Inc.Inventors: David S. Hays, Shri Niwas, Gregory D. Lundquist Jr.
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Publication number: 20090099161Abstract: Imidazoquinolines and imidazonaphthyridines with a substituent containing a functional group, e.g., an amide, sulfonamide, urea, or heterocyclyl group, at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making 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: February 10, 2006Publication date: April 16, 2009Applicant: Coley Pharmaceutial Group, Inc.Inventors: Michael J. Rice, Chad A. Haraldson, John F. Gerster, Joshua R. Wurst, Philip D. Heppner, Bryon A. Merrill, Tushar A. Kshirsagar
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Publication number: 20090093454Abstract: The present invention provides compounds of Formula (I) comprising: including salts, solvates, and physiologically functional derivatives thereof, pharmaceutical formulations containing them, processes for their preparation, and methods of treatment using them.Type: ApplicationFiled: March 1, 2006Publication date: April 9, 2009Inventors: Kristjan Gudmundsson, John G. Catalano, Angilique Svolto
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Publication number: 20090075980Abstract: Pyrazolopyridin-4-amines, pyrazoloquinolin-4-amines, pyrazolonaphthyridin-4-amines, 6,7,8,9-tetrahydropyrazoloquinolin-4-amines, and prodrugs thereof, pharmaceutical compositions containing the compounds, intermediates, methods of making, 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: ApplicationFiled: March 31, 2006Publication date: March 19, 2009Applicant: Coley Pharmaceutical Group, Inc.Inventors: David S. Hays, Michael E. Danielson, John F. Gerster, Shri Niwas, Ryan B. Prince, Tushar A. Kshirsagar, Philip D. Heppner, William H. Moser, Joan T. Moseman, Matthew R. Radmer, Maureen A. Kavanagh, Sarah A. Strong, Jason D. Bonk
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Publication number: 20090075995Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity, including inflammatory and immune diseases, having the structure of formula (I): an enantiomer, diastereomer, or tautomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which: Z is heterocyclo or heteroaryl; A is a 5- to 8-membered carbocyclic ring or a 5- to 8-membered heterocyclic ring; B is a cycloalkyl, cycloalkenyl, aryl, heterocyclo, or heteroaryl ring, wherein each ring is fused to the A ring on adjacent atoms and optionally substituted by one to four groups which are the same or different and are independently selected from R5, R6, R7, and R8; J1, J2, and J3 are at each occurrence the same or different and are independently -A1QA2-; Q is a bond, O, S, S(O), or S(O)2; A1 and A2 are the same or different and are at each occurrence independently selected from a bond, C1-3alkylene, substitutedType: ApplicationFiled: August 8, 2007Publication date: March 19, 2009Inventors: David S. Weinstein, Ping Chen, T.G. Murali Dhar, Jingwu Duan, Hua Gong, Bin Jiang, Bingwei Vera Yang, Arthur M. Doweyko
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Publication number: 20090069314Abstract: Certain imidazoquinolines with a hydroxymethyl or hydroxyethyl substituent at the 2-position, and an aryl or heteroaryl substituent at the 7-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for preferentially inducing IFN-? biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: ApplicationFiled: February 22, 2006Publication date: March 12, 2009Applicant: Coley Pharmaceutical Group, Inc.Inventors: Tushar A. Kshirsagar, Bryon A. Merrill, Shri Niwas, Gregory D. Lundquist, JR., Philip D. Heppner, Michael E. Danielson
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Publication number: 20090062272Abstract: Imidazoquinolinyl, imidazopyridinyl, and imidazonaphthyridinyl sulfonamide compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of making 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: December 23, 2004Publication date: March 5, 2009Inventors: Jason D. Bonk, Joseph F. Dellaria, JR.
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Publication number: 20090054429Abstract: This invention provides novel arylindenopyridines and arylindenopyrimidines of the formula: wherein R1, R2, R3, R4, and X are as defined above, and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing adenosine A2a receptors. This invention also provides therapeutic and prophylactic methods using the instant compounds and pharmaceutical compositions.Type: ApplicationFiled: October 23, 2008Publication date: February 26, 2009Inventors: Geoffrey R. Heintzelman, James Lawrence Bullington, Kenneth C. Rupert
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Publication number: 20090042876Abstract: The present invention relates to inhibitors of protein kinases of formula I: which can be used in the treatment of various diseases, notably cancer, inflammation or disorders of the central nervous system. It also relates to pharmaceutical compositions containing the compounds according to the invention and their use in therapy.Type: ApplicationFiled: June 30, 2006Publication date: February 12, 2009Applicant: Pierre Fabre MedicamentInventors: Hugues Bienayme, Antoine Dumoulin, Serge Grisoni, Bachir Kaloun El, Stephane Poigny, Remi Rabot, Rachid Rahali, Eric Tam, Pascaline Klein, Karim Bedjeguelal, Houcine Rahali
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Publication number: 20090029983Abstract: This application relates to novel fused tricyclic thienopyridines of Formulas I and II, which useful for treating Hepatitis B infection and other diseases. This application also relates to pharmaceutical compositions comprising thienopyridines and to the use of such compositions to treat Hepatitis B and other diseases.Type: ApplicationFiled: January 3, 2008Publication date: January 29, 2009Applicant: Valeant Research & DevelopmentInventors: Huanming Chen, Robert Tam, Anneke K. Raney
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Publication number: 20090029939Abstract: Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed. A1 and A2 are moieties forming a five, six, or seven membered ring. L is a bond or a linker connecting a ring atom of Ar to N. X is O, S, or substituted nitrogen. Ar is aryl or heteroaryl, Q is N, +NR, or CR4. The aryl carbons may be independently substituted with substituents other than hydrogen. The compounds may include prodrug moieties covalently attached at any site.Type: ApplicationFiled: May 25, 2007Publication date: January 29, 2009Inventors: James M. Chen, Xiaowu Chen, Maria Fardis, Haolun Jin, Choung U. Kim, Laura N. Schacherer
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Publication number: 20090023720Abstract: 1H-Imidazo ring systems (e.g., imidazopyridines, imidazoquinolines, imidazonaphthyridines, 6,7,8,9-tetrahydro imidazoquinolines and imidazonaphthyridines) with an amino 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 modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: September 1, 2005Publication date: January 22, 2009Inventors: Tushar A. Kshirsagar, Scott E. Langer, Shri Niwas, Philip D. Heppner, David T. Amos
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Publication number: 20090018122Abstract: Imidazoquinoline compounds with an aryloxy or arylalkyleneoxy or hydroxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: August 27, 2004Publication date: January 15, 2009Inventors: Kyle J. Lindstrom, Hugues M.H. Martin, Bryon A. Merrill, Michael J. Rice, Joshua R. Wurst, Chad A. Haraldson, Tushar A. Kshirsagar, Philip D. Heppner, Shri Niwas, George W. Griesgraber, Matthew R. Radmer
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Publication number: 20090012076Abstract: The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: ApplicationFiled: July 9, 2007Publication date: January 8, 2009Inventors: Christopher J. Dinsmore, Matthew H. Katcher, Alan B. Northrup
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Publication number: 20090012077Abstract: The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases, including cathepsins B, K, C, F, H, L, O, S, W and X. Of particular interest are diseases associated with Cathepsin K.Type: ApplicationFiled: June 25, 2008Publication date: January 8, 2009Inventors: Alexander Graham Dossetter, Nicola Murdoch Heron
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Publication number: 20090005376Abstract: Imidazo-containing compounds (e.g., imidazonaphthyridines, imidazopyridines, imidazoquinolines, and imidazote-trahydroquinolines) with an alkoxy substituent at the 1-position, pharmaceutical compositions containing the compounds 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, 2005Publication date: January 1, 2009Inventors: Larry R. Krepski, Daniel E. Duffy, John F. Gerster, Joan T. Moseman
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Publication number: 20090005365Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and negatively modulating the ?5 subtype of GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: ApplicationFiled: June 6, 2008Publication date: January 1, 2009Applicant: Helicon Therapeutics, Inc.Inventors: Alan P. Kaplan, Varsha Gupta, Jan W.F. Wasley
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Publication number: 20080317712Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. 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: April 24, 2008Publication date: December 25, 2008Inventors: Deqiang Niu, Yat Sun Or, Zhe Wang
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Publication number: 20080318943Abstract: This invention relates to novel compounds having the structural formula I below: and their pharmaceutically acceptable salts, tautomers or in vivo-hydrolysable precursors, compositions and methods of use thereof, wherein R1, R2, R3, R4, R5, and R6 are defined in the specification. These novel compounds provide a treatment or prophylaxis of anxiety disorders, schizophrenia, cognitive disorders, and/or mood disorders.Type: ApplicationFiled: June 18, 2008Publication date: December 25, 2008Applicant: ASTRAZENECA ABInventors: Hui-Fang Chang, Marc Chapdelaine, Bruce Thomas Dembofsky, Keith John Herzog, Carey Horchler, Richard Jon Schmiesing
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Publication number: 20080312434Abstract: A process and intermediates for preparing 1H-imidazo[4,5-c]pyridin-4-amines are disclosed. The process includes providing a 7H-imidazo[4,5-c]tetrazolo[1,5-a]pyridine and converting a 7H-imidazo[4,5-c]tetrazolo[1,5-a]pyridine to a 1H-imidazo[4,5-c]pyridin-4-amine.Type: ApplicationFiled: May 1, 2008Publication date: December 18, 2008Applicant: Coley Pharmaceutical Group, Inc.Inventors: Kyle J. Lindstrom, Luke T. Dressel, Jason D. Bonk
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Patent number: 7465742Abstract: This application relates to novel fused tricyclic thienopyridines of Formulas I and II, which useful for treating Hepatitis B infection and other diseases. This application also relates to pharmaceutical compositions comprising thienopyridines and to the use of such compositions to treat Hepatitis B and other diseases.Type: GrantFiled: February 3, 2006Date of Patent: December 16, 2008Inventors: Huanming Chen, Robert Tam, Anneke K. Raney
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Publication number: 20080306049Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below and can exist in tautomeric forms: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: ApplicationFiled: June 6, 2008Publication date: December 11, 2008Applicant: Helicon Therapeutics, Inc.Inventors: Alan P. Kaplan, Varsha Gupta, Jan W.F. Wasley
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Publication number: 20080306048Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: ApplicationFiled: June 6, 2008Publication date: December 11, 2008Applicant: Helicon Therapeutics, Inc.Inventors: Alan P. Kaplan, Varsha Gupta
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Publication number: 20080293712Abstract: The present invention relates to Benzo[c][2,7]naphthyridine Derivatives, compositions comprising an effective amount of a Benzo[c][2,7]naphthyridine Derivative, methods for treating or preventing a proliferative disorder or an autoimmune disease, comprising administering to a subject in need thereof an effective amount of a Benzo[c][2,7]naphthyridine Derivative, methods for modulating PDK-1 activity, PKA activity, Akt activity, S6K activity, or PKC activity, comprising administering to a subject in need thereof an effective amount of a Benzo[c][2,7]naphthyridine Derivative. The invention also relates to processes for preparing a Benzo[c][2,7]naphthyridine Derivative.Type: ApplicationFiled: March 4, 2008Publication date: November 27, 2008Applicant: WYETHInventors: Allan WISSNER, Middleton Brawner FLOYD, JR., Russell DUSHIN, Heidi L. FRASER, Yongbo HU, Andreas MADERNA, Thomas NITTOLI, Yanong Daniel WANG
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Publication number: 20080287432Abstract: The invention provides a novel class of compounds of formula I, 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 diseases or disorders that involve abnormal activation of the AbI, Bcr-AbI, Aurora-A, SGK, Tie-2, Trk-B, FGFR3, c-kit, b-RAF, c-RAF, DYRK2, Fms, Fyn and PDGFRalpha and PDGFR&bgr; kinases.Type: ApplicationFiled: August 15, 2006Publication date: November 20, 2008Applicants: IRM LLC, The Scripps Research InstituteInventors: Barun Okram, Pingda Ren, Nathanael S. Gray
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Publication number: 20080269209Abstract: New compounds 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: November 23, 2006Publication date: October 30, 2008Applicant: PALAU PHARMA, S.A.Inventors: Carmen Almansa Rosales, Marina Virgili Bernado
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Patent number: 7442710Abstract: The present invention relates to compounds of general formula IA or IB wherein X1 and X2 are each independently N or C—R? and R1, R2,R3, R4, R5, and R6 are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The compounds can be used for the treatment of diseases related to the glycine transporter inhibitor, such as schizophrenia and Alzheimer's disease.Type: GrantFiled: January 24, 2006Date of Patent: October 28, 2008Assignee: Hoffman-La Roche Inc.Inventors: Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard
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Publication number: 20080261969Abstract: This invention relates to compounds of formula (I) to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods of treatment comprising administering of such compounds.Type: ApplicationFiled: January 15, 2008Publication date: October 23, 2008Applicant: AVENTIS PHARMA S.A.Inventors: Jacques MAUGER, Anil NAIR, Nina MA, Kirsten BJERGARDE, Bruno FILOCHE-ROMME, Odile ANGOUILLANT-BONIFACE, Serge MIGNANI, Jean-Christophe CARRY, Francois CLERC, Herve MINOUX, Laurent SCHIO, Cecile COMBEAU
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Publication number: 20080255110Abstract: This invention is directed to a compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, Z, m, n, o, p and r are as defined herein, its preparation, pharmaceutical composition and use as an adenosine A3 receptor ligand preferably an antagonist.Type: ApplicationFiled: June 17, 2008Publication date: October 16, 2008Applicant: SANOFI-AVENTISInventors: Peter ARANYI, Laszlo BALAZS, Maria BALOGH, Sandor BATORI, Lajos T. NAGY, Geza TIMARI, Kinga BOER, Zoltan KAPUI, Endre MIKUS, Katalin GERBER, Judit VARGANE SZEREDI, Katalin URBAN-SZABO, Erzsebet WALCZ
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Patent number: 7425554Abstract: In one aspect, the present invention provides compounds having formula (1) or (100), a salt thereof or a hydrate of the foregoing, which compounds exhibit excellent cell adhesion inhibitory action or cell infiltration inhibitory action, and are useful as therapeutic or prophylactic agents for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome; rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis. wherein R10 represents optionally substituted cycloalkyl, etc., R20-23 represent hydrogen, alkyl, alkoxy, etc., R30-32 represent hydrogen, alkyl, oxo, etc., and R40 represents optionally substituted alkyl, etc.Type: GrantFiled: December 27, 2004Date of Patent: September 16, 2008Assignee: Eisai R&D Management Co., Ltd.Inventors: Tetsuya Kawahara, Makoto Kotake, Naoki Yoneda, Shinsuke Hirota, Masayoshi Ohkuro
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Publication number: 20080214536Abstract: Compounds of a certain formula (I) in which R1, R2, R3, R31, R4, R5, R51, R6 and R7 have the meanings indicated in the description, are novel effective PDE4 inhibitors.Type: ApplicationFiled: March 9, 2006Publication date: September 4, 2008Applicant: NYCOMED GmbhInventors: Ulrich Kautz, Beate Schmidt, Dieter Flockerzi, Maria Vittoria Chiesa, Armin Hatzelmann, Christof Zitt, Johannes Barsig, Degenhard Marx, Hans-Peter Kley
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Publication number: 20080214538Abstract: The present disclosure relates to pyridoindolone derivatives of general formula (I): to processes for preparing the same and to their use in therapeutics.Type: ApplicationFiled: May 12, 2008Publication date: September 4, 2008Applicant: SANOFI-AVENTISInventors: Bernard Bourrie, Pierre Casellas, Paola Ciapetti, Jean-Marie Derocq, Samir Jegham, Yvette Muneaux, Camille-Georges Wermuth
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Patent number: 7419977Abstract: This invention is directed to a compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, Z, m, n, o, p and r are as defined herein, its preparation, pharmaceutical composition and use as an adenosine A3 receptor ligand preferably an antagonist.Type: GrantFiled: May 16, 2005Date of Patent: September 2, 2008Assignee: Sanofi-AventisInventors: Peter Aranyi, Laszlo Balazs, Maria Balogh, Sandor Batori, Lajos T. Nagy, Geza Timari, Kinga Boer, Zoltan Kapui, Endre Mikus, Katalin Gerber, Judit Vargane Szeredi, Katalin Urban Szabo, Erzsebet Walcz
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1-Heterocyclylalkyl-3-sulfonylazaindole or -azaindazole derivatives as 5-hydroxytryptamine-6 ligands
Patent number: 7411064Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptorType: GrantFiled: February 15, 2006Date of Patent: August 12, 2008Assignee: WyethInventors: Ronald Charles Bernotas, Steven Edward Lenicek, Hassan Mahmoud Elokdah, David Zenan Li -
Publication number: 20080167301Abstract: Compounds of the formula I in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors.Type: ApplicationFiled: March 2, 2005Publication date: July 10, 2008Applicant: Altana Pharma AGInventor: Ulrich Kautz
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Publication number: 20080146568Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety, depressive disorders and other diseases. The compounds of present invention are represented by the general formula (I) wherein R1 to R1, X and Y are as defined in the specification.Type: ApplicationFiled: November 30, 2007Publication date: June 19, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20080146546Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.Type: ApplicationFiled: February 4, 2008Publication date: June 19, 2008Inventors: Jun Yuan, Pamela Albaugh, Kenneth Shaw, Alan Hutchison
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Publication number: 20080139553Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety, depressive disorders and other diseases. The compounds of present invention are represented by the general formula (I) wherein R1 to R1, X and Y are as defined in the specification.Type: ApplicationFiled: November 30, 2007Publication date: June 12, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Patent number: 7375226Abstract: The present invention relates to compounds of formula IA wherein R1, R2, R3, and n are as defined in the specification, and to pharmaceutically active acid addition salts thereof. The compounds of the invention are useful in the treatment of neurological and neuropsychiatric disorders.Type: GrantFiled: December 8, 2005Date of Patent: May 20, 2008Assignee: Hoffman-La Roche Inc.Inventors: Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard