Five-membered Nitrogen Hetero Ring Attached Directly Or Indirectly To The 1,3-diazine Ring By Nonionic Bonding Patents (Class 514/252.19)
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Publication number: 20110269772Abstract: Axl kinase inhibitory compounds are disclosed, as well as compositions and methods of using the same in the treatment of cancer and other conditions mediated by and/or associated with Axl kinase.Type: ApplicationFiled: July 14, 2011Publication date: November 3, 2011Applicant: SUPERGEN, INC.Inventors: David J. BEARSS, Hariprasad VANKAYALAPATI, Yong XU
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Publication number: 20110269732Abstract: The present invention relates to drug discovery methods, particularly methods for assaying compounds for activity as Aurora kinase inhibitors. This invention also relates to a pharmacophore describing compounds that are able to promote a conformational change in the protein AuroraB and whose binding constant for the two-step process is given as Ki*. Finally, this invention also relates to compounds having the features of the pharmacophore.Type: ApplicationFiled: October 14, 2009Publication date: November 3, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Julian M.C. GOLEC, John POLLARD, James WESTCOTT, Hayley Marie BINCH, Michael Paul MORTIMORE, Daniel David ROBINSON
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Publication number: 20110269721Abstract: Provided herein are method of treating, ameliorating, or delaying at least one symptom of a genetic blood disorder, e.g. sickle cell disorder or thalassemia, in a patient in need thereof, comprising administering a therapeutically effective amount of a Jak2 inhibitor. Also provided in part is a method of reducing an enlarged spleen in a patient suffering from thalassemia, comprising administering a therapeutically effective amount of a Jak2 inhibitor.Type: ApplicationFiled: August 3, 2009Publication date: November 3, 2011Applicant: TargeGen, Inc.Inventor: John D. Hood
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Patent number: 8048881Abstract: The invention relates to 4-aminocarbonyl-pyrimidine derivatives and their use as P2Y12 receptor antagonists in the treatment and/or prevention and/or treatment of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.Type: GrantFiled: April 27, 2006Date of Patent: November 1, 2011Assignee: Actelion Pharmaceuticals Ltd.Inventors: Eva Caroff, Heinz Fretz, Kurt Hilpert, Olivier Houille, Francis Hubler, Emmanuel Meyer
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Publication number: 20110263525Abstract: The invention describes a cytotoxic composition containing a drug combination targeting two or more functional elements in pancreatic cancer cells, the functional elements comprising EGFR or Src and Stat3 or Jaks. Preferred drugs in the drug combination are selected from ZD and S3I-201, Das and S3I-201, ZD and AG490, Das and AG490, and combinations thereof. In a preferred embodiment of the invention, the drug combination further includes a nucleoside analog inhibitory for DNA replication, for example, Gemcitabine. Disclosed is also a method of cytotoxically affecting pancreatic cancer cells using the described drug combination. A method of making the cytotoxic composition is additionally described.Type: ApplicationFiled: November 30, 2009Publication date: October 27, 2011Inventor: James Turkson
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Publication number: 20110263609Abstract: The invention described herein relates to diagnostic and treatment methods and compositions useful in the management of disorders, for example cancers, involving NUP214-ABL1 positive T-cell malignancies and methods for treating an individual suffering from a NUP214-ABL1 positive T cell malignancy.Type: ApplicationFiled: November 14, 2008Publication date: October 27, 2011Inventors: Alfonso Quintas-Cardama Lee, Guillermo Garcia-Manero
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Publication number: 20110263596Abstract: Described are compounds which inhibit, regulate and/or modulate kinase signal transduction, for example of Met kinase. The compounds are of the formulae A1 to A148 and B1 described herein, including 2-oxobenzoxazol-3-ylmethyl]phenyl}carbamate and 2-oxooxazolo[4,5-b]pyridin-3-ylmethyl)phenyl]carbamate compounds, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. Also described are compositions containing these compounds. Also described are methods for the treatment of diseases in which the inhibition, regulation and/or modulation of kinase signal transduction plays a role by administering these compounds.Type: ApplicationFiled: July 6, 2011Publication date: October 27, 2011Inventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
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Patent number: 8044055Abstract: The invention relates to 2-phenyl-6-aminocarbonyl-pyrimidine derivatives and their use as P2Y12 receptor antagonists in the treatment and/or prevention and/or treatment of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals. Formula (I).Type: GrantFiled: October 24, 2007Date of Patent: October 25, 2011Assignee: Actelion Pharmaceuticals Ltd.Inventors: Eva Caroff, Kurt Hilpert, Emmanuel Meyer
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Patent number: 8026241Abstract: Therapeutic benzimidazoles and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers,Type: GrantFiled: February 6, 2009Date of Patent: September 27, 2011Assignee: Amgen Inc.Inventors: Chenera Balan, Yunxin Bo, Celia Dominguez, Christopher H. Fotsch, Vijay K. Gore, Vu Van Ma, Mark H. Norman, Vassil I. Ognyanov, Yi-xin Qian, Xianghong Wang, Ning Xi, Shimin Xu
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Publication number: 20110224197Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, such as inhibitors of GSK-3. The invention provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. The invention provides processes for preparing compounds of the invention. The invention provides methods of identifying compounds useful for treatment of diabetes, diabetic neuropathy, osteoporosis, Alzheimer's disease, Huntington's disease, Parkinson's disease, AIDS-associated dementia, bipolar disorder, amyotrophic lateral sclerosis, multiple sclerosis, schizophrenia, leukocytopenia, cardiomyocyte hypertrophy, stroke, post-stroke, spinal cord injury, traumatic brain injury, Charcot-Marie-Tooth, peripheral nerve regeneration, and rheumatoid arthritis.Type: ApplicationFiled: September 9, 2010Publication date: September 15, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: Gregory William Henkel, Michael Liu, Timothy Neuberger
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Publication number: 20110212077Abstract: The invention provides biaryl meta-pyrimidine compounds having the general structure (A). The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the Jak kinase family, and various other specific receptor and non-receptor kinases.Type: ApplicationFiled: August 24, 2010Publication date: September 1, 2011Applicant: TargeGen, Inc.Inventors: Glenn Noronha, Chi Ching Mak, Jianguo Cao, Joel Renick, Andrew McPherson, Binqi Zeng, Ved P. Pathak, Daniel L. Lohse, John D. Hood, Richard M. Soll
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Publication number: 20110207719Abstract: A series of novel anthra[1,2-d]imidazole-6,11-dione derivatives, and the preparation method and application of said derivatives, wherein said application includes a pharmaceutical composition containing said derivatives for treating cancer, and said application involves effects of said derivatives for inhibiting telomerase activity, inhibiting the growth of cancer cell, treating cancer and the like.Type: ApplicationFiled: February 25, 2010Publication date: August 25, 2011Inventor: Hsu-Shan HUANG
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Publication number: 20110207741Abstract: Provided herein are methods of treating a medical condition in which RAS activation is increased. The method comprises the step of administering to a subject a c-Src inhibitor in an amount effective to treat the medical condition. The invention also provides a method of treating or preventing a cardiac arrhythmia. The method comprises the step of administering to the subject a c-Src inhibitor in an amount effective to treat or prevent the cardiac arrhythmia. The invention additionally provides a method of delaying the onset of sudden cardiac death. The method comprises the step of administering to the subject a c-Src inhibitor in an amount effective to delay the onset of SCD. Methods of augmenting gap junction function and methods of increasing Connexin 43 levels in a subject in need thereof are further provided.Type: ApplicationFiled: February 22, 2011Publication date: August 25, 2011Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventor: Samuel Dudley
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Publication number: 20110207699Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: December 9, 2010Publication date: August 25, 2011Applicant: ABBOTT LABAORATORIESInventors: David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, Allan C. Krueger, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Todd N. Soltwedel, Douglas K. Hutchinson, Charles A. Flentge, Rolf Wagner, Clarence J. Maring, Michael D. Tufano, David A. Betebenner, Todd W. Rockway, Dachun Liu, John K. Pratt, Michael J. Lavin, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi, William A. Carroll
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Publication number: 20110200597Abstract: The present invention relates to the identification and diagnostic use of biomarkers in primary colorectal cancer tumors whose activation level are predictive of the likelihood of the onset of metastatic disease. These biomarkers may be used to determine the suitability of a patient for aggressive and/or targeted treatments. Kits and compositions of the invention are also provided.Type: ApplicationFiled: August 5, 2009Publication date: August 18, 2011Applicant: George Mason Intellectual Properties, Inc.Inventors: Emanuel F. Petricoin, III, Lance A. Liotta, Mariaelena Pierobon, Alessandra Sllvestri
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Publication number: 20110190220Abstract: The present invention pertains to the use of defensin ?1 and/or defensin ?4, as a marker for predicting and following the response of a patient suffering from chronic myeloid leukaemia to a treatment with imatinib.Type: ApplicationFiled: July 17, 2009Publication date: August 4, 2011Inventors: Béatrice Turcq, Gabriel Etienne, Maryse Dupouy, François-Xavier Mahon, Bertrand Garbay, Patricia Costaglioli
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Publication number: 20110190271Abstract: The present invention provides 2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferative diseases such as tumorigenic cancers.Type: ApplicationFiled: December 29, 2010Publication date: August 4, 2011Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Ankush Argade, Rajinder Singh, Hui Li, David Carroll, Susan Catalano
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Publication number: 20110189167Abstract: Methods of modulating a kinase activity of a wild-type kinase species, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs of any of the foregoing, are provided which employ compounds of the formula Ia:Type: ApplicationFiled: August 4, 2010Publication date: August 4, 2011Inventors: Daniel L. FLYNN, Peter A. PETILLO, Michael D. KAUFMAN
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Publication number: 20110178095Abstract: The present invention relates to tyrosine kinase inhibitors that contain a zinc-binding moiety and their use in the treatment of tyrosine related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.Type: ApplicationFiled: January 20, 2011Publication date: July 21, 2011Inventors: Xiong Cai, Changgeng Qian, Stephen Gould, Haixiao Zhai
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Publication number: 20110178153Abstract: Methods of treating or preventing chemoresistance or relapse growth of cancer cells are provided. Methods of treating or preventing resistance to tyrosine kinase based chemotherapeutic treatment in hematologic and solid tumors are provided. BCR-ABL drug resistance in chronic myelogenous leukemia (CML) and models for conducting further study on the same are presented. The methods comprise administering a therapeutically effective amount of one or more SIRT1 modulators to the cells or subject in need thereof. The methods may be administered in combination with, prior to or subsequent to chemotherapy or may be administered to counteract the effect of a spontaneous genetic mutation. Methods of using SIRT1 inhibitors to treat or prevent insulin and transferrin-induced resistance are also presented. A novel cell model to study mechanisms of acquired chemoresistance is also provided.Type: ApplicationFiled: February 5, 2008Publication date: July 21, 2011Inventor: Wenyong CHEN
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Publication number: 20110172242Abstract: A method of treating exposure to organophosphate agents through the use of compounds comprising tetrahydroindolone and arylpiperazine moieties.Type: ApplicationFiled: October 14, 2010Publication date: July 14, 2011Inventors: David HELTON, David FICK
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Publication number: 20110166154Abstract: Methods and compositions are provided useful in the diagnosis, treatment and management of cancers wherein cancer cells express certain polynucleotides and/or polypeptides that are differentially expressed in colon cancer subtypes that are sensitive to therapy with abl kinase inhibitors and src kinase inhibitors. In particular, PTK-7, PLK-2 and PLK-3 could be identified as markers for determining the responsiveness of cancer to dasatinib.Type: ApplicationFiled: January 23, 2009Publication date: July 7, 2011Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Dennis J. Slamon, Richard S. Finn, Judy Dering, J. Randolph Hecht, Zev A. Wainberg, Edwin A. Clark, Charles L. Ginther
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Publication number: 20110158983Abstract: In alternative embodiments, this invention provides compositions and methods for treating cancer or any condition caused by dysfunctional cells, side effects from treatments for cancer or any condition caused by dysfunctional cells, e.g., mucositis therapies (e.g., for oral mucositis; digestive mucositis; esophageal mucositis; intestinal mucositis). In alternative embodiments, the invention provides cytoprotection products that may be used either alone or in combination with other medical therapies such as cancer chemotherapies and radiation therapies.Type: ApplicationFiled: March 5, 2009Publication date: June 30, 2011Inventors: Newell Bascomb, John Maki, Fredric S. Young
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Patent number: 7968550Abstract: The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have the stated meanings the N-oxides and the physiologically tolerated salts thereof and process for the preparation thereof are described. The compounds are suitable for example as anorectic agents.Type: GrantFiled: January 11, 2007Date of Patent: June 28, 2011Assignees: Aventis Pharma Deutschland GmbH, Sanofi-Aventis Deutschland GmbHInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Thomas Boehme, Gerhard Hessler, Petra Stahl, Dirk Gretzke
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Publication number: 20110152235Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.Type: ApplicationFiled: December 23, 2010Publication date: June 23, 2011Applicant: Jasco Pharmaceuticals, LLCInventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger, Yvonne L. Flanders, Stephane A. Dumas
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Publication number: 20110129463Abstract: Provided are quinazolin-4(3A)-one derivatives, which are inhibitors of the ubiquitin ligase activity of a human polypeptide, particularly to POSH inhibitors, and to compositions and methods for the treatment RING E3 ubiquitin ligase related diseases.Type: ApplicationFiled: November 26, 2010Publication date: June 2, 2011Applicant: Proteologics, Ltd.Inventors: Omri EREZ, Philippe NAKACHE
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Publication number: 20110124619Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.Type: ApplicationFiled: November 17, 2010Publication date: May 26, 2011Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
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Publication number: 20110112096Abstract: The invention provides novel pyrimidine derivatives of formula (I) and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-IR) or analplastic lymphoma kinase (ALK).Type: ApplicationFiled: June 24, 2009Publication date: May 12, 2011Applicant: ITM LLCInventors: Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Xiaohui He, Songchun Jiang, Kunyong Yang
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Publication number: 20110105520Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, and L, A, and Ra are defined herein.Type: ApplicationFiled: October 28, 2010Publication date: May 5, 2011Inventors: STEVEN J. COATS, HAIYAN BIAN, PETER J. CONNOLLY, GILLES BIGNAN, CHAOZHONG CAI, SCOTT L. DAX, BART L. DECORTE, SHU-CHEN LIN, LI LIU, MARK J. MACIELAG, PHILIP M. PITIS, YUE-MEI ZHANG, BIN ZHU, WEI HE
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Patent number: 7935704Abstract: Compounds represented by the following structure (I) are disclosed: as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R1, R1?, R1?, R2, R3, R4, R5, and R6, X1 and X2, Y, Z, Z1, Z2, Z3, and Z4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating vascular proliferation are also disclosed.Type: GrantFiled: February 4, 2005Date of Patent: May 3, 2011Assignee: Nereus Pharmaceuticals, Inc.Inventors: Michael A. Palladino, George Kenneth Lloyd, Yoshio Hayashi, Benjamin Nicholson
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Publication number: 20110098296Abstract: The present invention provides thiazole and oxazole compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.Type: ApplicationFiled: December 4, 2008Publication date: April 28, 2011Inventors: George Adjabeng, Neil Bifulco, Ronda G. Davis-Ward, Scott Howard Dickerson, Keith Hornberger, Kimberly Petrov, Tara Renae Rheault, Daivd Edward Uehling, Alex Gregory Waterson
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Publication number: 20110092490Abstract: A compound of formula (I) and its pharmaceutically acceptable salts or solvates and physiologically hydrolysable, solubilising or immobilisable derivatives wherein: Ar is a 5-membered heteroaryl ring wherein X1 and X2 are one or two heteroatoms or Ar is a 6-membered aromatic ring, wherein heteroatoms are selected from S, O, N, Se; Z is NH, NHCO, NHSO2, N-alkyl, CH2NH, CH2N-alkyl, CH2, CH2CH2, CH?CH, CH2CONH, SO2, or SO; Y is N CR3; R1, R2, R5, R6, R7, R8 and R9 are each independently H, or a substituent; R3, when present, is selected from alkyl and a substituent, with the proviso that when Y is CR3, Ar is a 5-membered heterocycle comprising one or two N heteroatoms and Z is NH, then R3 is selected from C3+ alkyl and a substituent; R4 is selected from H, alkyl and R13 as hereinbefore defined, with the proviso that when R3 is absent, R4 is selected from alkyl and a substituent; processes for the preparation thereof, intermediates and precursors therefore and the use thereof as a medicament, and therapeutic compType: ApplicationFiled: March 26, 2009Publication date: April 21, 2011Applicant: THE UNIVERSITY OF NOTTINGHAMInventors: Shudong Wang, Shenhua Shi, Andrey Zaytsev, Peter Martin Fischer
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Publication number: 20110086856Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. 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.Type: ApplicationFiled: December 14, 2010Publication date: April 14, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Juliam M.C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard
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Patent number: 7919489Abstract: The invention relates to heterocyclylamide-substituted imidazoles and methods for their preparation, their use for the treatment and/or prophylaxis of diseases as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, in particular for the use as antiviral agents, especially against cytomegaloviruses.Type: GrantFiled: August 20, 2007Date of Patent: April 5, 2011Assignee: Aicuris GmbH & Co. KGInventors: Holger Zimmermann, David Brueckner, Kerstin Henninger, Ulrich Rosentreter, Martin Hendrix, Joerg Keldenich, Dieter Lang, Martin Radtke, Daniela Paulsen, Armin Kern
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Patent number: 7910585Abstract: Novel pyrimidine derivatives of formula I to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: GrantFiled: August 26, 2005Date of Patent: March 22, 2011Assignee: Novartis AGInventors: Eiji Kawahara, Takahiro Miyake, Johannes Roesel
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Publication number: 20110065706Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as GPR119 modulators, methods for their therapeutic use, particularly in the treatment of obesity and diabetes mellitus, and pharmaceutical compositions containing them.Type: ApplicationFiled: September 10, 2010Publication date: March 17, 2011Applicant: AstraZeneca ABInventors: Alan Martin Birch, Roger John Butlin, David Stephen Clarke, Andrew Leach, Philip Alexander MacFaul, Charles John O'Donnell, James Stewart Scott, Paul Robert Owen Whittamore, Dan Anders Broo, Öjvind Percy Davidsson, Kjell Erik Johansson, Hanna De La Motte
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Patent number: 7902184Abstract: The present invention relates to compounds of formula I and their pharmaceutically acceptable salts wherein formula I is: wherein X, Y, Z, R1 and R2 are as defined in the description and claims. The compounds of the present invention act as antagonists and/or inverse agonists at the histamine 3 receptor and are useful for the treatment and/or prevention of diseases such as obesity, metabolic syndrome (syndrome X), and other eating disorders.Type: GrantFiled: May 21, 2007Date of Patent: March 8, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Heinrich Nettekoven, Olivier Roche
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Publication number: 20110053916Abstract: The present invention relates to compounds useful as inhibitors of treating tuberculosis.Type: ApplicationFiled: August 12, 2010Publication date: March 3, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: Tiansheng Wang, Brian Hanzelka, Ute Muh, Guy Bemis
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Patent number: 7893064Abstract: The present invention is directed to novel bicyclic pyrimidine compounds of Formula (I) or a form or composition thereof as inhibitors of ATP-protein kinase interactions, wherein substituents on each side of the iminomethyl double bond in Formula (I) may be in the E or Z configuration; and wherein R1, R2, R3 and R4 are as defined herein.Type: GrantFiled: October 12, 2007Date of Patent: February 22, 2011Assignee: Janssen Pharmaceutica NVInventors: Guozhang Xu, Lily Lee Searle, Shenlin Huang
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Patent number: 7888361Abstract: The present invention relates to tyrosine kinase inhibitors that contain a zinc-binding moiety and their use in the treatment of tyrosine related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.Type: GrantFiled: September 10, 2007Date of Patent: February 15, 2011Assignee: Curis, Inc.Inventors: Xiong Cai, Changgeng Qian, Stephen Gould, Haixiao Zhai
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Publication number: 20110034470Abstract: The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein p, q, Y?, r, R1, R2, X, X1, X2, X3, and X4 are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.Type: ApplicationFiled: August 9, 2010Publication date: February 10, 2011Inventors: Leyi Gong, Xiaochun Han, Ferenc Makra, Wylie Solang Palmer, Lubica Raptova
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Publication number: 20110033461Abstract: Compositions which act synergistically to inhibit the growth of cancer cells and methods of use thereof are disclosed.Type: ApplicationFiled: March 12, 2009Publication date: February 10, 2011Inventors: Vladimir Ratushny, Erica Golemis, Igor Astsaturov, Iiya G. Serebriiskii, Louis M. Weiner
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Publication number: 20110028489Abstract: The present invention relates to a new use of pyrimidine derivatives of formula I, as a free base or a pharmaceutically acceptable salt thereof in the manufacture of a medicament in the treatment and/or prophylaxis of Alzheimer's Disease:Type: ApplicationFiled: August 16, 2010Publication date: February 3, 2011Inventors: Lars Andersson, Stefan Berg, Jeremy Burrows, Sven Hellberg, Fernando Huerta, Tobias Rein
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Publication number: 20110020376Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: ApplicationFiled: June 2, 2010Publication date: January 27, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Juan-Miguel Jimenez, Andrew Miller, Jeremy Green, Huai Gao, Gregory Henkel, Michael Liu, Timothy Neuberger
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Publication number: 20110021524Abstract: This invention provides a combination of ATP-competitive BCR-ABL inhibitor and a non-ATP competitive BCR-ABL inhibitor. The combination of the present invention may be used for treating cancers known to be associated with BCR-ABL.Type: ApplicationFiled: December 18, 2008Publication date: January 27, 2011Applicant: IRM LLCInventors: Francisco Adrian, Christine Dierks, Nathanael S. Gray, Markus Warmuth
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Publication number: 20110020217Abstract: There is described a pharmaceutical composition comprising dexanabinol, or a derivative thereof, in combination with a second therapeutic agent that targets BRAF or MEK, and a pharmaceutically acceptable adjuvant, diluent or carrier. There is also described a method of treating a patient suffering from melanoma and uses related thereto.Type: ApplicationFiled: October 10, 2008Publication date: January 27, 2011Applicant: E-THERAPEUTICS PLCInventors: Malcolm Philip Young, Catherine Mary Thomas, Olusola Clement Idowu
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Publication number: 20100324063Abstract: The present invention provides methods for inhibiting JAK2 tyrosine kinase. Further, the present invention also provides methods of treating or preventing myeloproliferative disorders.Type: ApplicationFiled: August 5, 2010Publication date: December 23, 2010Inventors: Carolyn A. Buser-Doepner, Steven J. Freedman, Jackson B. Gibbs, Frank J. Giles, Christopher G. Marshall, John R. Pollard
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Publication number: 20100316607Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: June 15, 2010Publication date: December 16, 2010Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
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Publication number: 20100310675Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: ApplicationFiled: June 8, 2010Publication date: December 9, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Hayley Binch, Michael Mortimore, Chris Davis, Dean Boyall, Simon Everitt, Daniel Robinson, Sharn Ramaya, Damien Fraysse, John Studley, Andrew Miller, Michael O'Donnell, Alistair Rutherford, Joanne Pinder
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Publication number: 20100311750Abstract: The present invention provides a compound of formula (I): wherein the variants R1, R2, R3, R4, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.Type: ApplicationFiled: December 1, 2008Publication date: December 9, 2010Inventors: Muneto Mogi, Toshio Kawanami, Ken Yamada, Kayo Yasoshima, Hidetomo Imase, Takahiro Miyake, Osamu Ohmori