The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/127)
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Patent number: 7678792Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFR?, PDGFR?, CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGF?, SRC, EGFR, trkB, FGFR3, FLT3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2?, BRK, KDR, c-raf or b-raf kinase, or mutant forms thereof.Type: GrantFiled: October 16, 2007Date of Patent: March 16, 2010Assignee: IRM LLCInventors: Donatella Chianelli, Christopher Cow, Yun He, Songchun Jiang, Xiaolin Li, Xiaodong Liu, Zuosheng Liu, Jon Loren, Valentina Molteni, Juliet Nabakka, Pingda Ren, Taebo Sim, Xiaodong Wang, Shuli You
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Patent number: 7678911Abstract: Disclosed are compounds of formula (I): wherein R3, R5, R7 and R8 are defined herein, which are useful as inhibitors SYK kinase and are thus useful for treating diseases resulting from inappropriate mast cell activation, which include allergic and inflammatory diseases. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.Type: GrantFiled: January 15, 2008Date of Patent: March 16, 2010Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles L. Cywin, Scott E. Jakes, Joachim Heider, Mark A. Bobko, Renee L. Des Jarlais, Mark Player, James Rinker, Michael Winters, Bao-ping Zhao
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Publication number: 20100056511Abstract: The invention provides compounds of formula (I), and pharmaceutically acceptable salts thereof wherein: R1, R2, R3, R4, R5, R6, R7, X and X1 are as defined herein. These compounds are useful in the manufacture of medicaments for use in the prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.Type: ApplicationFiled: November 21, 2007Publication date: March 4, 2010Inventors: Robert Downham, Edward Sibley Morris, Lloyd James Payne, Philip Neil Edwards, Gareth Morse Davies
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Publication number: 20100056516Abstract: 1-Hydroxy naphthyridine compounds (e.g., 1-hydroxy naphthyridin-2(1H)-one compounds of Formula I are inhibitors of HIV integrase and/or HIV RNase H and inhibitors of HIV replication: (I) wherein X and R1-R6 are as defined herein. The compounds are useful in the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other anti-HIV agents such as HIV antivirals, immunomodulators, antibiotics and vaccines.Type: ApplicationFiled: July 13, 2007Publication date: March 4, 2010Inventors: Peter D. Williams, Shankar Venkatraman, H. Marie Langford, Boyoung Kim, Theresa M. Booth, Jay A. Grobler, Donnette Staas, Rowena D. Ruzek, Mark W. Embrey, Catherine M. Wiscount, Terry A. Lyle
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Publication number: 20100048560Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).Type: ApplicationFiled: March 20, 2008Publication date: February 25, 2010Applicant: GENKYOTEX SAInventors: Patrick Page, Mike Orchard, Leiticia Fioraso, Bianca Mottiromi
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Publication number: 20100048557Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.Type: ApplicationFiled: June 19, 2009Publication date: February 25, 2010Inventors: Bing-Yan ZHU, Michael SIU, Steven R. MAGNUSON, Richard PASTOR, He HAIYING, Xiao YISONG, Zheng JIFU, Xu XING, Zhao JUNPING
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Publication number: 20100048558Abstract: The invention relates to novel thienopyridine derivatives of formula (I), wherein R1, R2, R3, R4 and Y have the meaning cited in claim 1, are HSP90-inhibitors and can be used for producing a medicament for treating illnesses, wherein the inhibition, regulation and/or modulation of HSP90 plays a roll.Type: ApplicationFiled: May 27, 2005Publication date: February 25, 2010Inventors: Hans-Michael Eggenweiler, Michael Wolf
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Publication number: 20100036118Abstract: The present invention provides novel fused ring heterocycle kinase modulators and methods of using the novel fused ring heterocycle kinase modulators to treat diseases mediated by kinase activity.Type: ApplicationFiled: August 11, 2009Publication date: February 11, 2010Inventors: William D. Arnold, Pierre Bounaud, Chixu Chen, Brian Eastman, Andreas Gosberg, Stefan N. Gradl, Stephanie Hopkins, Zhe Li, Ian McDonald, Paul A. Sprengeler, Ruo W. Steensma, Mark E. Wilson
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Publication number: 20100035878Abstract: The present invention provides novel compounds of formula I and their use in the inhibition of c-Jun N-terminal kinases. The present invention further provides the use of these compounds in medicine, in particular in the prevention and/or treatment of neurodegenerative disorders related to apoptosis and/or inflammation.Type: ApplicationFiled: October 6, 2009Publication date: February 11, 2010Applicant: EISAI R & D MANAGEMENT CO., LTD.Inventors: Afzal KHAN, Darren Peter MEDLAND, Gurpreet BHATIA
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Publication number: 20100035875Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.Type: ApplicationFiled: June 19, 2009Publication date: February 11, 2010Inventors: Bing-Yan ZHU, Michael SIU, Steven R. MAGNUSON, Richard PASTOR, He HAIYING, Xiao YISONG, Zheng JIFU, Xu XING, Zhao JUNPING, Wendy LIU
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Publication number: 20100029637Abstract: Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving chymase.Type: ApplicationFiled: September 27, 2007Publication date: February 4, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stéphane De Lombaert, Michel Jose Emmanuel
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Publication number: 20100022521Abstract: The present invention relates to new mGluR1 and mGluR5 receptor subtype preferring ligands of formula (I) wherein X represents a group selected from SO, SO2; Y represents a group selected from (CH2)n, NH, NHCH2; n is an integer of 0 to 1; Z is H or monosubstituted by alkyl, nitro, halogen, alkoxy, trifluoromethyl, cyano, amino, alkylamino, dialkylamino, aminomethyl, e alkylaminomethyl, dialkylaminomethyl, hydroxyl, alkylsulfonylamino; R1 is an optionally substituted alkyl, cycloalkyl, phenyl, biphenyl, heterocyclyl; R2 is an optionally substituted phenyl, heterocyclyl, or NR3R4 group wherein R3 and R4 are independently selected from the group of hydrogen and an optionally substituted alkyl, or R3 and R4 together with the N atom to which they are attached form an optionally substituted C5-7 heterocyclyl group, containing one or more heteroatom(s), or NH—CO—NR5R6 group, wherein R5 and R6 are independently selected from the group of hydrogen and an optionally substituted alkyl, or R5 and R6 together with the N aType: ApplicationFiled: December 19, 2006Publication date: January 28, 2010Applicant: Hansa Metallwerke AGInventors: Katalin Nogradi, Gabor Wagner, Gyorgy Keseru, Attila Bielik, Tamas Gati, Viktor Hada, Janos Koti, Krisztina Gal, Monika Vastag, Amrita Agnes Bobok
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Publication number: 20100016307Abstract: The present invention relates to compounds of formula (I): and processes for preparing them, compositions containing them and their use in treating diseases relating to inappropriate c-Met activity.Type: ApplicationFiled: October 24, 2007Publication date: January 21, 2010Inventors: Toshihiro Hamajima, Hiroko Nakamura, Jun Tang
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Publication number: 20100004239Abstract: The present invention relates to pyrrolo[3,2-c]pyridine-4-one 2-indolinone compounds of Formula (I) and their pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8X, Y and have the meaning cited in the specification. Also disclosed are the pharmaceutical compositions containing the foregoing compounds, methods for the preparation and pharmaceutical use thereof, particularly as protein kinase inhibitors. Formula (I).Type: ApplicationFiled: January 24, 2007Publication date: January 7, 2010Inventors: Peng Cho Tang, Yidong Su, Lei Zhang, Lu Xiao
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Publication number: 20100004235Abstract: The present application relates to novel heterocyclyl-substituted fused pyrazole derivatives, to processes for their preparation, to their use, alone or in combination, for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: April 17, 2007Publication date: January 7, 2010Applicant: BAYER HEALTHCARE AGInventors: Hartmut Schirok, Nils Griebenow, Chantal Fürstner, Joachim Mittendorf, Johannes-Peter Stasch, Frank Wunder, Karl-Heinz Schlemmer, Stefan Heitmeier, Friederike Stoll
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Publication number: 20090325953Abstract: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.Type: ApplicationFiled: June 10, 2009Publication date: December 31, 2009Inventors: Soumya P. Sahoo, Meng-Hsin Chen, Kevin D. Dykstra, Hiroo Koyama, Peter T. Meinke, Stephen J. O'Keefe, Ginger Xu-qiang Yang
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Publication number: 20090325952Abstract: The invention provides a compound of formula (I) or a salt thereof: wherein Ar has the sub-formula (x): as defined herein, and the use of the compounds as inhibitors of PDE4.Type: ApplicationFiled: July 31, 2007Publication date: December 31, 2009Inventors: David George Allen, Nicola Mary Aston, Rodger Phillip Barnett, Reshma Manesh Chudasama, Caroline Jane Day, Christopher David Edlin, Leanda Jane Kindon, Naimisha Trivedi
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Publication number: 20090325936Abstract: The present invention relates to compounds represented by Formula (I) and Formula (II): (I) (II) or pharmaceutically acceptable salts thereof. The present invention also provides pharmaceutical compositions comprising the instant compounds. This invention further provides methods to treat and prevent pain, respiratory and non-respiratory diseases.Type: ApplicationFiled: December 14, 2007Publication date: December 31, 2009Inventors: Mark T. Bilodeau, Christopher S. Burgey, Zhengwu James Deng, Nathan R. Kett, Jeffrey Melamed, Peter M. Munson, Kausik K. Nanda, Wayne Thompson, B. Wesley Trotter, Zhicai Wu, John C. Hartnett
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Publication number: 20090318428Abstract: 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: ApplicationFiled: September 4, 2007Publication date: December 24, 2009Inventors: Konrad Honold, Wolfgang Schaefer, Stefan Scheiblich
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Publication number: 20090318425Abstract: The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula wherein the variables are as defined herein. The invention also relates to 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: June 23, 2009Publication date: December 24, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Edcon Chang, Stephen L. Gwaltney, Angie Vassar
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Publication number: 20090318439Abstract: Compounds are disclosed. The compounds act as MCH1 modulators. Other embodiments are also disclosed.Type: ApplicationFiled: January 9, 2008Publication date: December 24, 2009Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter Robert Guzzo, Matthew David Surman
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Publication number: 20090318437Abstract: The present invention is directed to substituted pyrazolo[1,5-a]pyridines and related methods for their synthesis and use.Type: ApplicationFiled: June 10, 2009Publication date: December 24, 2009Inventors: Federico C.A. Gaeta, Matthew Gross, Kirk W. Johnson
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Patent number: 7635695Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory, immunoregulatory, metabolic, infectious and cell proliferative diseases or conditions are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, metabolism, infection and cell proliferation. The subject compounds contain a fused heterobicyclic ring.Type: GrantFiled: February 21, 2007Date of Patent: December 22, 2009Assignee: Amgen Inc.Inventors: Simon A. Burkitt, Mario G. Cardozo, Timothy D. Cushing, Michael R. DeGraffenreid, Christopher N. Farthing, Xiaolin Hao, Juan C. Jaen, Xian Yun Jiao, David J. Kopecky, Marc Labelle, Sarah E. Lively, Dustin L. McMinn, Sven P. Rasmussen, Youngsook Shin, Marie-Louise Smith, Andrew Smith
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Publication number: 20090312321Abstract: Described are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or prevent disease or disordered associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activity of kinases such as Abl, ALK, AMPK, Aurora, Axl, Bcr-Abl, BIK, Bmx, BRK, BTK, c-Kit, CSK, cSrc, CDK1, CHK2, CK1, CK2, CaMKII, CaMKIV, DYRK2, EGFR, EphB1, FES, FGFR1, FGFR2, FGFR3, Flt1, Flt3, FMS, Fyn, GSK3?, IGF-1R, IKK?, IKK?, IR, IRAK4, ITK, JAK2, JAK3, JNK1?1, JNK2?, KDR, Lck, LYN, MAPK1, MAPKAP-K2, MEK1, MET, MKK4, MKK6, MST2, NEK2, NLK, p70S6K, PAK2, PDGFR, PDGFR?, PDK1, Pim-2, Plk3, PKA, PKB?, PKC?, PKCtheta, PKD2, c-Raf, RET, ROCK-I, ROCK-II, Ron, Ros, Rsk1, SAPK2a, SAPK2b, SAPK3, SAPK4, SGK, SIK, Syk, Tie2, TrkB, WNK3, and ZAP-70.Type: ApplicationFiled: April 6, 2007Publication date: December 17, 2009Applicant: IRM LLCInventors: Pingda Ren, Guobao Zhang, Shuli You, Taebo Sim, Nathanael S. Gray, Yongping Xie, Xing Wang, Yun He
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Publication number: 20090306373Abstract: This invention relates generally to compounds and pharmaceutical compositions for the treatment of myosin heavy chain (MyHC)-mediated conditions, and in particular, cardiovascular conditions.Type: ApplicationFiled: December 19, 2006Publication date: December 10, 2009Inventors: Gabriel G. Gamber, Rishi K. Jain, Gary M. Ksander, Leslie W. McQuire, Lawrence S. Melvin, Moo J. Sung
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Publication number: 20090298820Abstract: The invention relates to 3-substituted-1H-pyrrolo[2,3-b]pyridine, and 3-substituted-1H-pyrrolo[3,2-b]pyridine compounds of the Formula 1: or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.Type: ApplicationFiled: May 28, 2009Publication date: December 3, 2009Applicant: WyethInventors: Hwei-Ru Tsou, Gary Harold Birnberg, Gloria Jean MacEwan, Semiramis Ayral-Kaloustian, Matthew Gregory Bursavich, Sabrina Lombardi, Nan Zhang, Adam Matthew Gilbert, George Theordore Grosu, Natasja Brooijmans, Thai Hiep Nguyen
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Publication number: 20090291942Abstract: The invention relates to novel imidazopyridine derivatives and to their use in the treatment of diseases and disorders which may e.g. involve angiogenesis and/or pain, including autoimmune and inflammatory diseases.Type: ApplicationFiled: May 19, 2009Publication date: November 26, 2009Inventors: Ivan Cornella Taracido, Edmund Martin Harrington, René Hersperger, René Lattmann, Wolfgang Miltz, Klaus Weigand
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Publication number: 20090291937Abstract: 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: ApplicationFiled: October 31, 2008Publication date: November 26, 2009Inventors: Juan-Miguel Jimenez, Michael Mortimore, Andrew Miller, Philip Collier, Stephen Young, Guy Brenchley, Chris Davis, Heather Twin, Chau Mak, Dean Boyall, Shazia Keily, Luca Settimo
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Publication number: 20090286777Abstract: The present invention is directed to certain 5,6-fused pyrrolidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.Type: ApplicationFiled: May 11, 2007Publication date: November 19, 2009Inventors: Jianming Bao, Robert J. DeVita, Sander G. Mills, Gregori J. Morriello
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Publication number: 20090286767Abstract: Substituted quinolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: ApplicationFiled: February 9, 2009Publication date: November 19, 2009Applicant: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Timothy M. Caldwell, Bertrand L. Chenard, Stéphane De Lombaert, Kevin J. Hodgetts
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Patent number: 7618964Abstract: 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: November 17, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Konrad Honold, Klaus Kaluza, Birgit Masjost, Wolfgang Schaefer, Stefan Scheiblich
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Publication number: 20090275570Abstract: The invention relates to novel compounds of Formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds possess CHK1 kinase inhibitory activity, PDK1 inhibitory activity and Pak kinase inhibitory activity and are accordingly useful in the treatment and/or prophylaxis of cancer.Type: ApplicationFiled: April 5, 2006Publication date: November 5, 2009Applicant: ASTRAZENECA ABInventors: Kevin Daly, Nicola Heron, Alexander Hird, Stephanos Ioannidis, James Janetka, Paul Lyne, Jaime Scott, Dorin Toader, Melissa Vasbinder, Dingwei Yu, Yan Yu
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Publication number: 20090270376Abstract: The present invention provides a compound of formula (I) having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases inflammatory diseases, and allergic diseases. The compound according to the present invention has an inhibition activity against JAK3 and is thus useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transmission (e.g., rejection during organ/tissue transplantation, autoimmune diseases, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, Alzheimer's disease, and atherosclerotic disease), or diseases caused by abnormal cytokine signal transmission (e.g., cancer and leukemia).Type: ApplicationFiled: December 25, 2006Publication date: October 29, 2009Applicant: Astellas Pharma Inc.Inventors: Takayuki Inoue, Akira Tanaka, Kazuo Nakai, Hiroshi Sasaki, Fumie Takahashi, Shohei Shirakami, Keiko Hatanaka, Yutaka Nakajima, Koichiro Mukoyoshi, Hisao Hamaguchi, Shigeki Kunikawa, Yasuyuki Higashi
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Publication number: 20090258854Abstract: Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.Type: ApplicationFiled: April 9, 2009Publication date: October 15, 2009Inventors: Genesis M. Bacani, Diego Broggini, Eugene Y. Cheung, Christa C. Chrovian, Xiaohu Deng, Anne M. Fourie, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearny, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Jimmy T. Liang, Susanne Lochner, Neelakandha S. Mani, Alejandro Santillan, JR., Kathleen Sappey, Kia Sepassi, Virginia M. Tanis, Alvah T. Wickboldt, John J. M. Wiener, Hartmut Zinser
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Publication number: 20090252779Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: ApplicationFiled: April 3, 2009Publication date: October 8, 2009Applicant: ChemoCentryx, Inc.Inventors: Penglie Zhang, Andrew M.K. Pennell, John J. Kim Wright, Wei Chen, Manmohan R. Leleti, Yandong Li, Lianfa Li, Yuan Xu
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Publication number: 20090253689Abstract: New compounds of the Formula (I): for the treatment of non-insulin-dependent diabetes mellitus.Type: ApplicationFiled: March 29, 2007Publication date: October 8, 2009Inventors: Daniel Kaspar Baeschlin, Nils Ostermann, Francois Gessier, Finton Sirockin, Kenji Namoto
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Publication number: 20090253679Abstract: The present invention relates to imidazolone derivatives of formula (I) to methods of preparing such derivatives, intermediates thereto, pharmaceutical compositions comprising such derivatives, and methods of inhibiting protein kinase, and methods of treatment comprising administration of such derivatives.Type: ApplicationFiled: March 31, 2009Publication date: October 8, 2009Applicant: sanofi-aventisInventors: Vincent Leroy, Eric Bacque, Emmanuel Conseiller, Anke Steinmetz, Baptiste Ronan, Jean-Philippe Letallec
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Patent number: 7598243Abstract: The present invention is directed to compounds of the formula I: Wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.Type: GrantFiled: October 15, 2004Date of Patent: October 6, 2009Assignee: Merck & Co., Inc.Inventors: Gabor Butora, Stephen D. Goble, Alexander Pasternak, Lihu Yang, Changyou Zhou, Christopher R. Moyes
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Publication number: 20090247515Abstract: A compound according to Formula A: or a pharmaceutically acceptable salt thereof, wherein R11, G1 and G2 are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: March 13, 2009Publication date: October 1, 2009Applicant: Exelixis, Inc.Inventors: Richard Martin, Brenton T. Flatt, Jackline Eve Dalgard, Venkataiah Bollu, Ping Huang, Raju Mohan, Edwin Schweiger, Tie-Lin Wang
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Publication number: 20090227578Abstract: 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: September 10, 2009Inventors: Richard Engh, Hubert Hertenberger, Konrad Honold, Birgit Masjost, Petra Rueger, Wolfgang Schaefer, Stefan Scheiblich, Manfred Schwaiger
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Publication number: 20090227789Abstract: The invention relates a compound represented by the formula (1): Q1-Q2-C(?O)—N(R1)-Q3-N(R2)-T1-Q4??(1) wherein R1 and R2 represent H or the like; Q1 represents an aromatic ring, heterocyclic ring or the like; Q2 represents a single bond, aromatic ring, heterocyclic ring or the like; Q3 represents a group or the like, Q4 represents an aromatic ring, heterocyclic ring or the like; and T1 represents —CO— or —SO2—, and a medicine which comprises the compound and is useful for thrombosis and embolism.Type: ApplicationFiled: May 13, 2009Publication date: September 10, 2009Applicant: DAIICHI PHARMACEUTICAL CO., LTD.Inventors: Toshiharu YOSHINO, Tsutomu NAGATA, Noriyasu HAGINOYA, Kenji YOSHIKAWA, Hideyuki KANNO, Masatoshi NAGAMOCHI
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Publication number: 20090215771Abstract: The present invention provides novel compounds of formula I and their use in the inhibition of c-Jun N-terminal kinases. The present invention further provides the use of these compounds in medicine, in particular in the prevention and/or treatment of neurodegenerative disorders related to apoptosis and/or inflammation.Type: ApplicationFiled: June 20, 2008Publication date: August 27, 2009Inventors: Piotr GRACZYK, Afzal KHAN, Gurpreet BHATIA, Yoichi IIMURA
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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: 20090203677Abstract: The present invention relates to novel compounds of Formula (I) and their use in the treatment of respiratory diseases, including anti-inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.Type: ApplicationFiled: February 5, 2009Publication date: August 13, 2009Applicant: Glaxo Group LimitedInventors: James Francis Callahan, Guoliang Lin, Zehong Wan, Hongxing Yan
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Publication number: 20090203668Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof wherein W, L, R3, R3a, R3b and R4 are defined herein.Type: ApplicationFiled: April 16, 2009Publication date: August 13, 2009Inventors: James J. Li, Lawrence G. Hamann, Haixia Wang, Zheming Ruan, Christopher B. Cooper, Jun Li, Jeffrey A. Robi
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Publication number: 20090203665Abstract: The present invention relates to compounds of formula I wherein R1, R2, and are defined in the specification and to pharmaceutically acceptable acid addition salts thereof.Type: ApplicationFiled: April 13, 2009Publication date: August 13, 2009Inventors: Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard
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Publication number: 20090197871Abstract: The present invention is directed to novel compounds of Formula (I), pharmaceutical compositions and their use in therapy, for example as inhibitors of phosphodiesterase type IV (PDE4) and as antagonists of muscarinic acetylcholine receptors (mAChRs), in the treatment of/and or prophylaxis of respiratory diseases, including antiinflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.Type: ApplicationFiled: February 5, 2009Publication date: August 6, 2009Applicant: Glaxo Group LimitedInventors: James Francis Callahan, Guoliang Lin, Zehong Wan, Hongxing Yan
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Publication number: 20090197881Abstract: The present invention creates an azaindole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further providing a therapeutic agent for treating allergic diseases. A compound of the general formula (I) wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.; the formula of -X1=X2-X3=X4- is a formula of —C(R1)?C(R2)—C(R3)?N— etc.; R1, R2, R3, R4 and R5 are independently a hydrogen atom or a halogen atom etc.; R6 is optionally substituted C1-C6 alkyloxy etc.; R7 is independently a halogen atom etc.; R8 is optionally substituted C1-C6 alky etc.; R9 is carboxy etc.; M is sulfonyl etc.; Y is a single bond etc.; L1, L2 and L3 are a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or hydrate thereof.Type: ApplicationFiled: July 20, 2006Publication date: August 6, 2009Inventors: Akira Kugimiya, Itsuo Makino, Naohiro Onodera
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Publication number: 20090197864Abstract: Furo[3,2-c]Pyridine and Thieno[3,2-c]pyridine compounds of Formula I, and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in disease treatment, including cancers, including conditions in which EMT is involved, including conditions mediated by protein kinase activity such as RON and/or MET.Type: ApplicationFiled: February 6, 2009Publication date: August 6, 2009Inventors: An-Hu Li, Arno G. Steinig, Andrew Kleinberg, Qinghua Weng, Mark J. Mulvihill, Jing Wang, Xin Chen, Ti Wang, Hanqing Dong, Meizhong Jin
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Publication number: 20090192150Abstract: The invention relates to compounds of the formula I having antithrombotic activity, which in particular inhibit the protease-activated receptor 1 (PAR1), processes for their preparation and use thereof as medicaments.Type: ApplicationFiled: February 2, 2009Publication date: July 30, 2009Applicant: sanofi-aventisInventors: Uwe HEINELT, Armin HOFMEISTER, Joerg CZECH