Three Or More Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 514/228.5)
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Publication number: 20120283239Abstract: The invention relates to 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derived Cathepsin S inhibitors of Formula (I), wherein R1 is H or (C1-3)alkyl; R2 is halogen or (C1-4)alkyl, optionally substituted with one or more halogens; n is 1-3; X is O or CH2; U, V and W are CH; or one of U, V and W is N; Y is a group capable of interacting with the Sn . . . S2 substites of the active site of Cathepsin S; or a pharmaceutically acceptable salt thereof, 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, 2011Publication date: November 8, 2012Applicant: MSD OSS B.V.Inventors: Jiaqiang Cai, David Jonathan Bennett, Philip Stephen Jones
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Publication number: 20120277214Abstract: Compounds which are tricyclopyrazole derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.Type: ApplicationFiled: November 24, 2010Publication date: November 1, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Teresa Disingrini, Sergio Mantegani, Mario Varasi
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Publication number: 20120277219Abstract: The invention relates to pyrido[2,3-b]pyrazine compounds of general formulae (Ia) and (Ib), to their preparation and use, for example, for the treatment of malignant disorders and other disorders based on pathological cell proliferations.Type: ApplicationFiled: July 5, 2012Publication date: November 1, 2012Applicant: Aeterna Zentaris GmbHInventors: Matthias Gerlach, Irene Seipelt, Eckhard Guenther, Emmanuel Polymeropoulos, Tilmann Schuster, Eckhard Claus
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Publication number: 20120270866Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders.Type: ApplicationFiled: October 8, 2010Publication date: October 25, 2012Applicant: aFRAXis Inc.Inventors: Benedikt Vollrath, Daivd Campbell, Sergio G. Durón, Warren Wade
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Publication number: 20120264747Abstract: 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 21, 2012Publication date: October 18, 2012Inventors: 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: 20120252779Abstract: The invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.Type: ApplicationFiled: October 19, 2010Publication date: October 4, 2012Inventors: Nigel Ramsden, Richard John Harrison, Sally Oxenford, Kathryn Bell, Nelly Piton, Claudio Dagostin, Cyrille Boussard, Andrew Ratcliffe
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Publication number: 20120252799Abstract: 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: ApplicationFiled: June 11, 2012Publication date: October 4, 2012Applicant: 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: 8258129Abstract: The present invention encompasses compounds of general formula (1) wherein X and R1 to R3 are as defined in the disclosure, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.Type: GrantFiled: July 5, 2007Date of Patent: September 4, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Harald Engelhardt, Gerd Bader, Guido Boehmelt, Ralph Brueckner, Thomas Gerstberger, Maria Impagnatiello, Daniel Kuhn, Otmar Schaaf, Heinz Stadtmueller, Irene Waizenegger, Andreas Zoephel
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Publication number: 20120220566Abstract: The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals.Type: ApplicationFiled: October 15, 2010Publication date: August 30, 2012Applicant: Rib-X Pharmaceuticals, Inc.Inventors: Erin M. Duffy, Ashoke Bhattacharjee, Hardwin O'Dowd, Marco DeVivo, Zoltan F. Kanyo, Jacek G. Martinow, Ik-Hyeon Paik, Matthew H. Scheideman, Sandra Sinishtaj, Brian T. Wimberly, Yusheng Wu
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Publication number: 20120220572Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein X, Y, Z, R3 and R4 are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.Type: ApplicationFiled: February 28, 2012Publication date: August 30, 2012Applicant: ABBOTT LABORATORIESInventors: Yunsong Tong, Thomas D. Penning, Alan S. Florjancic, Julie Miyashiro, Keith W. Woods
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Publication number: 20120214768Abstract: The invention relates to pyrido[2,3-b]pyrazine compounds of general formulae (Ia) and (Ib), to their preparation and use, for example, for the treatment of malignant disorders and other disorders based on pathological cell proliferations.Type: ApplicationFiled: April 25, 2012Publication date: August 23, 2012Applicant: Aeterna Zentaris GmbHInventors: Matthias Gerlach, Irene Seipelt, Eckhard Guenther, Emmanuel Polymeropoulos, Tilmann Schuster, Eckhard Claus
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Publication number: 20120202788Abstract: Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, and methods of manufacturing a compound of Formula I.Type: ApplicationFiled: September 14, 2011Publication date: August 9, 2012Inventors: Toby Jonathan Blench, Charles Ellwood, Simon Charles Goodacre, Yingjie Lai, Jun Liang, Calum Macleod, Steven R. Magnuson, Vickie H. Tsui, Karen Williams, Birong Zhang
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Publication number: 20120178744Abstract: The present invention provides Fused Tricyclic Compounds of the Formula (I) wherein Q, R1, R2, R3, and R4 are as defined herein, and pharmaceutically acceptable salts of such Fused Tricyclic Compounds. The Fused Tricyclic Compounds are useful in the treatment of cancer and other proliferative disorders.Type: ApplicationFiled: June 30, 2010Publication date: July 12, 2012Inventors: Cliff C. Cheng, Hongbo Zeng, Gerald W. Shipps, JR., Yongqi Deng, Zhaoyang Meng, Lianyun Zhao, Yang Nan, Binyuan Sun, Duan Liu, Panduranga A. Reddy, M. Arshad Siddiqui
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Patent number: 8211854Abstract: The present invention provides methods for inhibiting protein kinases selected from the group consisting of AKT, Checkpoint kinase, Aurora kinase, Pim kinases, and tyrosine kinase using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with protein kinases using such compounds.Type: GrantFiled: January 15, 2010Date of Patent: July 3, 2012Assignee: Schering CorporationInventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, David A. Parry
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Publication number: 20120165311Abstract: Thieno[2,3-c]pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: ApplicationFiled: February 24, 2012Publication date: June 28, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Daniele Fancelli, Paola Vianello, Mario Varasi, Simona Bindi, Sergio Vioglio, Dania Tesei
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Publication number: 20120165310Abstract: The invention relates to compounds of formula I, wherein the substituents are as defined in the specification; to processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; such compounds as a medicament; such compounds for the treatment of a proliferative disease.Type: ApplicationFiled: September 10, 2010Publication date: June 28, 2012Applicant: NOVARTIS AGInventors: Bei Chen, Robin Alec Fairhurst, Andreas Floersheimer, Pascal Furet, Vito Guagnano, Jiang Songchun, Wenshuo Lu, Thomas H. Marsilje, III, Clive McCarthy, Pierre-Yves Michellys, Frederic Stauffer, Stefan Stutz, Andrea Vaupel
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Publication number: 20120165314Abstract: This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds and compositions for the prevention and/or treatment of hyper-proliferative disorders and diseases associated with angiogenesis.Type: ApplicationFiled: March 7, 2012Publication date: June 28, 2012Applicant: Bayer HealthCare LLCInventors: Julie Dixon, Barton Phillips, Yamin Wang, Tindy Li, Kyle Parcella, Jason Newcom, Harold C.E. Kluender, Zhenqiu Hong, Brent Chandler, Zhonghua Zhang, Steven Magnuson, Kristen M. Allegue, Zheng Liu
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Patent number: 8207161Abstract: Tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I), their preparation methods, pharmaceutical compositions containing the derivatives and uses thereof as medicaments, especially as dipeptidyl peptidase IV inhibitors, wherein the substituents of formula (I) are defined as same as the description.Type: GrantFiled: November 27, 2008Date of Patent: June 26, 2012Assignees: Jiangsu Hengrui Medicine Co. Ltd., Shanghai Hengrui Pharmaceutical Co. Ltd.Inventors: Peng Cho Tang, Fanglong Yang, Jiang Fan, Hu Feng, Yang Wang, Tao Yang
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Patent number: 8203001Abstract: The present invention encompasses compounds of general formula (1) wherein R1, M1, L1 and Q are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or anomalous cell proliferation, and the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.Type: GrantFiled: June 13, 2007Date of Patent: June 19, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Ulrich Reiser, Peter Ettmayer, Oliver Kraemer, Peter Sennhenn, Walter Spevak
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Publication number: 20120149677Abstract: The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: August 16, 2010Publication date: June 14, 2012Inventors: Vadim Y. Dudkin, Mark E. Fraley, Cheng Wang, Robert M. Garbaccio, Douglas C. Beshore, Scott K. Kuduk, Jason W. Skudlarek
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Publication number: 20120142665Abstract: The invention is concerned with triazolopyridine compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as pharmaceuticals.Type: ApplicationFiled: December 1, 2011Publication date: June 7, 2012Inventors: Alexander Flohr, Luca Gobbi, Katrin Groebke Zbinden, Matthias Koerner, Jens-Uwe Peters
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Publication number: 20120142678Abstract: A novel compound able to inhibit JAK is disclosed, this compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.Type: ApplicationFiled: December 2, 2011Publication date: June 7, 2012Inventors: Christel Jeanne Marie Menet, Koen Kurt Smits
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Publication number: 20120135977Abstract: The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: September 28, 2011Publication date: May 31, 2012Inventors: Douglas C. Beshore, Vadim Dudkin, Robert M. Garbaccio, Adam W. Johnson, Scott D. Kuduk, Jason W. Skudlarek, Cheng Wang, Mark E. Fraley
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Publication number: 20120122840Abstract: The invention relates to compounds, pharmaceutical compositions, and uses thereof, including therapeutic uses thereof, such as methods useful for treating cancer.Type: ApplicationFiled: September 23, 2011Publication date: May 17, 2012Applicant: Myrexis, Inc.Inventors: Dange Vijay Kumar, Ian A. McAlexander, Matthew Gregory Bursavich, Christophe Hoarau, Paul M. Slattum, David A. Gerrish, Jeffrey W. Lockman, Weston R. Judd, Michael Saunders, Daniel P. Parker, Daniel Feodore Zigar, In Chul Kim, J. Adam Willardsen, Kraig M. Yager, Mark D. Shenderovich, Brandi L. Williams, Keith D. Tardif
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Patent number: 8178671Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.Type: GrantFiled: July 30, 2004Date of Patent: May 15, 2012Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
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Publication number: 20120114739Abstract: The present invention provides methods for inhibiting mTOR using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with mTOR using such compounds.Type: ApplicationFiled: April 8, 2010Publication date: May 10, 2012Inventors: Yongqi Deng, Binyuan Sun, Hongbo Zeng, Matthew Richards, Gerald W. Shipps, JR., Cliff C. Cheng, Yinyan Zhao, Andrew McRiner, Zhaoyang Meng, Yang Nan, Mehul F. Patel, Iwona E. Wrona, Panduranga Adulla Reddy, Brian M. Eklov, Shuyi Tang, Duan Liu, Amit K. Mandal, Lianyun Zhao, M. Asshad Siddiqui
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Publication number: 20120094987Abstract: The invention relates to compounds of general formula (I); 1a, 1b, 1c and 1d. The invention also relates to a method for the production thereof, pharmaceutical preparations containing said compounds and/or physiologically compatible salts thereof which can be produced therefrom and/or solvates thereof, and to the pharmaceutical use of said compounds, salts or solvates thereof as inhibitors of phosphodiesterase 4. The compounds comprise active ingredients for the treatment of diseases which can have a positive influence by inhibiting the activity of phosphodiesterase 4 and/or TNF?-release, for example, in lymphocytes, eosinophile and basophile granulocytes, macrophages and mastocytes.Type: ApplicationFiled: October 3, 2011Publication date: April 19, 2012Inventors: Claudia Reichelt, Alexander Ludwig, Alexander Schulze, Mohammed Daghish, Siegfried Leistner, Andreas Krödel, Jochen Heinicke
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Publication number: 20120094975Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R1 to R4, X1, X1, X3, L1 and L2 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell pro-liferation, and the use thereof in such a treatment.Type: ApplicationFiled: September 8, 2009Publication date: April 19, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Andreas Mantoulidis, Georg Dahmann, Peter Ettmayer, Christian Klein, Steffen Steurer, Irene Waizenegger, Stephan Karl Zahn
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Patent number: 8143247Abstract: Disclosed are pharmaceutical compositions for the treatment of diseases which involve cell proliferation. Also disclosed are methods for the treatment of said diseases, comprising co-administration of a compound 1 of Formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings given herein and of an effective amount of an active compound 2 and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of a compound 1 of Formula (I) and of an effective amount of an active compound 2 and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations.Type: GrantFiled: May 7, 2009Date of Patent: March 27, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Gerd Munzert, Martin Steegmaier, Anke Baum
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Patent number: 8138172Abstract: The present invention provides 8-oxoadenine derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The 8-oxoadenine derivatives act as modulators of Toll-like Receptor (TLR) 7 and thus may be used in the treatment of asthma, hepatitis, allergic diseases, viral and bacterial infection as well as cancer.Type: GrantFiled: July 3, 2007Date of Patent: March 20, 2012Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co Ltd.Inventors: Anthony Cook, Tom McInally, Stephen Thom, Hiroki Wada
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Publication number: 20120065189Abstract: The present invention provides a novel heterocyclic compound. A heterocyclic compound represented by general formula (1) wherein, R1 and R2, each independently represent hydrogen; a phenyl lower alkyl group that may have a substituent(s) selected from the group consisting of a lower alkyl group and the like on a benzene ring and/or a lower alkyl group; or a cyclo C3-C8 alkyl lower alkyl group; or the like; R3 represents a lower alkynyl group or the like; R4 represents a phenyl group that may have a substituent(s) selected from the group consisting of a 1,3,4-oxadiazolyl group that may have e.g., halogen or a heterocyclic group selected from pyridyl group and the like; the heterocyclic group may have at least one substituent(s) selected from a lower alkoxy group and the like or a salt thereof.Type: ApplicationFiled: May 27, 2010Publication date: March 15, 2012Inventors: Akira Takahashi, Masaki Suzuki, Yuichi Nakamura, Yohji Sakurai
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Publication number: 20120058997Abstract: The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of the following structure (I) and (II): or a stereoisomer, prodrug or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer and other Pim kinase-associated conditions are also disclosed.Type: ApplicationFiled: July 21, 2011Publication date: March 8, 2012Applicant: SuperGen, Inc.Inventors: Yong Xu, Benjamin G. Brenning, Steven G. Kultgen, Xiaohui Liu, Michael Saunders, Koc-Kan Ho
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Publication number: 20120058984Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular Itk activity.Type: ApplicationFiled: March 15, 2010Publication date: March 8, 2012Inventors: Catherine Mary Alder, Ian Robert Baldwin, Nicholas Paul Barton, Amanda Jennifer Campbell, Aurelie Cecile Champigny, John David Harling, Aoife Caitriona Maxwell, Juliet Kay Simpson, Ian Edward David Smith, Christopher John Tame, Caroline Wilson, James Michael Woolven
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Publication number: 20120040959Abstract: The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B: Such compounds possess useful antimicrobial activity. The variables R2, R3, R5, R6, R7, and R9 shown in Formula A and B are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.Type: ApplicationFiled: October 24, 2011Publication date: February 16, 2012Applicant: Achillion Pharmaceuticals, Inc.Inventors: Barton James Bradbury, Jason Allan Wiles, Qiuping Wang, Akhiro Hashimoto, Edlaine Lucien, Godwin Clarence Gilroy Pais, Milind Deshpande, Michael John Pucci, Ha Young Kim
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Patent number: 8088764Abstract: A novel compound able to inhibit JAK is disclosed, that comprises a compound according to Formula I: or a pharmaceutically acceptable salt thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.Type: GrantFiled: June 25, 2010Date of Patent: January 3, 2012Assignee: Galapagos NVInventors: Christel Jeanne Marie Menet, Koen Kurt Smits
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Patent number: 8088790Abstract: 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: GrantFiled: November 3, 2006Date of Patent: January 3, 2012Assignee: 3M Innovative Properties CompanyInventors: Tushar A. Kshirsagar, Philip D. Heppner, Scott E. Langer
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Publication number: 20110294790Abstract: Bicyclic pyrazole and isoxazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases mediated by HSP90 protein, like cancer and neurodegenerative disorders.Type: ApplicationFiled: November 19, 2009Publication date: December 1, 2011Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Sergio Mantegani, Maria Gabriella Brasca, Francesco Casuscelli, Ron Ferguson, Helena Posteri, Carlo Visco, Elena Casale, Fabio Zuccotto
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Publication number: 20110294796Abstract: The invention provides benzotriazine compounds having formula (I). The benzotriazine compounds of the invention are capable of inhibiting kinases, such members of the Src kinase family, and various other specific receptor and non-receptor kinases.Type: ApplicationFiled: December 28, 2010Publication date: December 1, 2011Applicant: TargeGen, Inc.Inventors: Xianchang Gong, Kathy Barrett, Jianguo Cao, Colleen Gritzen, John D. Hood, Chi Ching Mak, Andrew McPherson, Ved Prakash Pathak, Joel Renick, Richard M. Soll, Ute Splittgerber, Wolfgang Wrasidlo, Ningning Zhao, Elena Dneprovskaia, Binqi Zeng, Glenn Noronha
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Publication number: 20110294776Abstract: This invention relates to novel compounds of formula (I). Formula (I) in which the variable groups are as defined in the specification and claims, to pharmaceutical compositions containing them, and to a method of treatment using them for treatment of cancer.Type: ApplicationFiled: November 2, 2006Publication date: December 1, 2011Applicant: BAYER HEALTHCARE AGInventors: Stephen O'Connor, Jacques Dumas, Wendy Lee, Julie Dixon, David Cantin, David Gunn, Jennifer Burke, Barton Phillips, Derek Lowe, Tatiana Shelekhin, Gan Wang, Xin Ma, Shihong Ying, Andrea McClure, Furahi Achebe, Mario Lobell, Frederick Ehrgott, Christiana Iwuagwu, Kyle Parcella
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Patent number: 8067409Abstract: Compounds that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.Type: GrantFiled: November 20, 2008Date of Patent: November 29, 2011Assignee: Abbott LaboratoriesInventors: Nwe Y. Ba-Maung, Randy L. Bell, Richard F. Clark, Scott A. Erickson, Steve D. Fidanze, Robert D. Hubbard, Robert A. Mantei, George S. Sheppard, Bryan K. Sorensen, Gary T. Wang, Jieyi Wang
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Publication number: 20110288067Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R, R2, and R3 are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: ApplicationFiled: May 18, 2011Publication date: November 24, 2011Inventors: Robert Than Hendricks, Johannes Hermann, Saul Jaime-Figueroa, Rama Kondru, Yan Lou, Stephen Lynch, Timothy D. Owens, Michael Soth, Calvin Yee
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Publication number: 20110288078Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: November 12, 2009Publication date: November 24, 2011Applicant: ARIAD PHARMACEUTICALS, INC.Inventors: Wei-Sheng Huang, R. Mathew Thomas
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Patent number: 8058270Abstract: Disclosed is the use of a compound of general Formula (1), optionally in form of its tautomers, racemates, enantiomers, diastereomers and the mixtures thereof and optionally in form of the pharmacologically acceptable acid addition salts, solvates, hydrates, polymorphs, physiologically functional derivatives or prodrugs thereof, for the preparation of a pharmaceutical composition for the treatment of diseases characterized by abnormal cell proliferation in a human or non-human mammalian body by inhibition of polo like kinases as mitotic regulators.Type: GrantFiled: May 15, 2008Date of Patent: November 15, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Gerd Munzert, Martin Steegmaier
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Publication number: 20110275609Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I The structures of rings A and B and substituents Ra, Rb and Rc are described in the specification. Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis, treatment and inhibition of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: ApplicationFiled: January 14, 2010Publication date: November 10, 2011Applicant: CARA THERAPEUTICS, INC.Inventor: Robert Zhiyong Luo
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Publication number: 20110269739Abstract: The present invention provides a new group of protein kinase inhibitors, pyrido[4,3,-d]pyrimidin-5-one derivatives, and pharmaceutically acceptable salts thereof that are useful for intreating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrido[4,3,-d]pyrimidin-5-one derivatives.Type: ApplicationFiled: October 29, 2010Publication date: November 3, 2011Applicants: Oscotec, Inc., GenoscoInventors: Hong Woo Kim, Jong Sung Koh, Jaekyoo Lee, Ho-Juhn Song, Youngsam Kim, Hee Kyu Lee, Jang-Sik Choi, Sun-Hee Lim, Sunhwa Chang
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Patent number: 8039505Abstract: Disclosed are compounds and compositions that modulate T-cells. Such compounds can be used to treat T-cell mediated disease like T-ALL, rheumatoid arthritis, multiple sclerosis, and graft-vs-host disease (GvHD), to name but a few. The compounds have a general structure as shown in Formula I. Ar1-L-Ar2??I wherein Ar1 and Ar2, are independent of one another, a substituted aryl, unsubstituted aryl, substituted heteroaryl, or unsubstituted heteroaryl; and L is a bond or a linker spanning two, three, four, or five atoms.Type: GrantFiled: April 11, 2008Date of Patent: October 18, 2011Assignee: University of Utah Research FoundationInventor: Nikolaus S. Trede
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Publication number: 20110245224Abstract: The present invention relates to compounds of Formula (I); to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.Type: ApplicationFiled: October 13, 2009Publication date: October 6, 2011Inventors: Kevin Barvian, Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Irene Hauck, Fei Zhou
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Publication number: 20110237575Abstract: The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: ApplicationFiled: November 10, 2009Publication date: September 29, 2011Inventors: Gerald W. Shipps, JR., Cliff C. Cheng, Xiaohua Huang, Abdelghani Abe Achab, Peter Orth, Johannes H. Voigt, Kyle Ann Soucy
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Publication number: 20110237564Abstract: The invention is concerned with novel imidazopyrimidine derivatives of formula (I) wherein R1, R2 and R8 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as pharmaceuticals.Type: ApplicationFiled: March 17, 2011Publication date: September 29, 2011Inventors: Rubén Alvarez Sánchez, Konrad Bleicher, Alexander Flohr, Luca Gobbi, Katrin Groebke Zbinden, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Markus Rudolph
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Publication number: 20110237574Abstract: This invention provides cells and methods for stimulating proliferation and migration of endogenous and exogenous mammalian stem cells in vivo and in vitro. The invention provides reagents and methods for efficiently proliferating mammalian stem cells in an animal in need thereof and producing stem cells that can be re-introduced into an animal in need thereof to alleviate neurological and corporal disorders.Type: ApplicationFiled: February 16, 2011Publication date: September 29, 2011Inventors: Kiminobu Sugaya, Tingyu Qu