Five-membered Nitrogen Hetero Ring Attached Directly Or Indirectly To The 1,3-diazine Ring By Nonionic Bonding Patents (Class 514/252.19)
  • FAK INHIBITORS
    Publication number: 20130017194
    Abstract: A compound of the formula (I): where R1 or R2 is a cyclc amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.
    Type: Application
    Filed: July 6, 2012
    Publication date: January 17, 2013
    Applicant: Cancer Therapeutics CRC Pty Limited
    Inventors: Ian Peter Holmes, Ylva Bergman, Gillian Elizabeth Lunniss, Marica Nikac, Neil Choi, Catherine Fae Hemley, Scott Raymond Walker, Richard Charles Foitzik, Danny Ganame, Romina Lessene
  • Pyrimidine Sulphonamide Derivatives as Chemokine Receptor Modulators
    Publication number: 20130012490
    Abstract: A compound of formula (1), 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: Application
    Filed: September 14, 2012
    Publication date: January 10, 2013
    Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
  • Biomarker Identifying the Reactivation of STAT3 After Src Inhibition
    Publication number: 20130012519
    Abstract: A method of identifying cancer or an associated disorder comprising identifying and quantifying STAT3 occurring in a biological sample taken from a subject after administering a SFK inhibitor to said subject.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 10, 2013
    Applicants: BRISTOL-MYERS SQUIBB COMPANY, BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Faye M. Johnson, Nicholas J. Donato, Francis Y. Lee
  • ANILINOPIPERAZINE DERIVATIVES AND METHODS OF USE THEREOF
    Publication number: 20120328691
    Abstract: The present invention relates to novel Anilinopiperazine Derivatives of Formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, cancer, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.
    Type: Application
    Filed: October 29, 2007
    Publication date: December 27, 2012
    Inventors: Gerald W. Shipps, JR., Cliff C. Cheng, Xiaohua Huang, Thierry O. Fischmann, Jose S. Duca, Matthew Richards, Hongbo Zeng, Binyuan Sun, Panduranga Adulla Reddy, Tzu T. Wong, Praveen K. Tadikonda, M. Arshad Siddiqui, Marc A. Labroli, Cory Poker, Timothy J. Guzi
  • BENZYLIC OXINDOLE PYRIMIDINES
    Publication number: 20120329771
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R5 to R10, A, L1, B, m and p are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.
    Type: Application
    Filed: December 19, 2011
    Publication date: December 27, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias TREU, Stephan Karl ZAHN, Patricia AMOUZEGH, Cristina LECCI, Heather TYE
  • Heterocyclic kinase inhibitors
    Patent number: 8338425
    Abstract: This invention relates to novel 2-{6-[4-(2-hydroxy-ethyl)-piperazin-1-yl]-2-methyl-pyrimidin-4-ylamino}-thiazole-5-carboxylic acid (2-chloro-6-methyl-phenyl)-amide derivatives, and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by the inhibition of kinases including Src-kinase and Bcr-Abl kinase.
    Type: Grant
    Filed: December 9, 2008
    Date of Patent: December 25, 2012
    Assignee: Concert Pharmaceuticals, Inc.
    Inventor: Roger Tung
  • Assay for Metastatic Colorectal Cancer
    Publication number: 20120321615
    Abstract: Disclosed herein is a method for predicting the prognosis, the likelihood of metastasis in, or the desirability of administering an aggressive therapy to, a subject with colorectal cancer, comprising determining, in a sample from the subject, the level of phosphorylation of one or more of certain proteins compared to a positive and/or negative reference standard; or the total amount of COX-2 protein compared to a positive and/or negative reference standard. Also described are methods for treating subjects likely to develop metastatic colorectal carcinoma, and pharmaceutical compositions and kits for implementing the methods of the invention.
    Type: Application
    Filed: May 25, 2012
    Publication date: December 20, 2012
    Inventors: Emanuel Petricoin, III, Lance A. Liotta, Mariaelena Pierobon, Valerie Calvert
  • COMBINATION CANCER THERAPY WITH HERV INHIBITION
    Publication number: 20120321637
    Abstract: Embodiments are directed to compositions and methods related combination therapy with HERV inhibition.
    Type: Application
    Filed: June 18, 2012
    Publication date: December 20, 2012
    Applicant: The Board of Regents of the University of Texas System
    Inventors: Jianli Dong, Gengming Huang
  • COMPOUNDS COMPRISING A SPIRO-RING AND METHODS OF USE
    Publication number: 20120315247
    Abstract: The present invention provides novel compounds useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Application
    Filed: August 17, 2012
    Publication date: December 13, 2012
    Applicants: SUNSHINE LAKE PHARMA CO., LTD.
    Inventor: Ning Xi
  • Imidazole-2,4-Dione Inhibitors of Casein Kinase 1
    Publication number: 20120316155
    Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), the TGF? pathway and/or the Wnt 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?), the TGF? pathway and/or the Wnt pathway.
    Type: Application
    Filed: February 17, 2011
    Publication date: December 13, 2012
    Applicant: Jasco Pharmaceuticals, LLC
    Inventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger
  • AMINOPYRIMIDINES AS SYK INHIBITORS
    Publication number: 20120309735
    Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
    Type: Application
    Filed: December 16, 2010
    Publication date: December 6, 2012
    Inventors: Michael D. Altman, Kenneth L. Arrington, Jason Burch, Bernard Cote, Jean-Francois Fournier, Jacques Yves Gauthier, Solomon Kattar, Sandra Lee Knowles, Jongwon Lim, Michelle R. Machacek, Alan B. Northrup, Michael H. Reutershan, Joel S. Robichaud, Adam J. Schell, Kerrie B. Spencer
  • PURINE AND PYRIMIDINE CDK INHIBITORS AND THEIR USE FOR THE TREATMENT OF AUTOIMMUNE DISEASES
    Publication number: 20120309723
    Abstract: The present invention relates to the use of an inhibitor of CDK2 and/or CDK7 and/or CDK9, or a pharmaceutically acceptable salt thereof, in the preparation of a medicament for treating a disease associated with antinuclear antibodies, wherein the inhibitor of CDK2 and/or CDK7 and/or CDK9 or pharmaceutically acceptable salt thereof is administered in an amount sufficient to down-regulate the levels of antinuclear antibodies. A further aspect of the invention relates to a combination comprising an inhibitor of CDK2 and/or CDK7 and/or CDK9, or a pharmaceutically acceptable salt thereof, and methylprednisolone, and its use in the treatment of diseases associated with antinuclear antibodies, such as SLE.
    Type: Application
    Filed: May 4, 2012
    Publication date: December 6, 2012
    Applicant: CYCLACEL LIMITED
    Inventors: Ariela BENIGNI, Carla ZOJA, Giuseppe REMUZZI, Athos GIANELLA-BORRADORI
  • Aminooxazole Inhibitors of Cyclin Dependent Kinases
    Publication number: 20120302578
    Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.
    Type: Application
    Filed: May 23, 2012
    Publication date: November 29, 2012
    Applicant: Neosome Life Sciences, LLC
    Inventors: Laxman S. Desai, Srinivas Chittaboina
  • COMPOUNDS AND METHODS
    Publication number: 20120289495
    Abstract: Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, Y, Q, X, B and L are as defined herein, and methods of making and using the same.
    Type: Application
    Filed: January 13, 2011
    Publication date: November 15, 2012
    Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby Schmidt
  • SUBSTITUTED N-PHENYLPYRIMIDIN-2-AMINE ANALOGS AS INHIBITORS OF THE AXL KINASE
    Publication number: 20120283261
    Abstract: In one aspect, the invention relates to substituted N-phenylpyrimidin-2-amine analogs, derivatives thereof, and related compounds, which are useful as inhibitors of Axl kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions for treating disorders associated with dysfunction of the Axl kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: March 31, 2012
    Publication date: November 8, 2012
    Inventors: David J. Bearss, Hariprasad Vankayalapati, Alexis Mollard, Steven L. Warner, Sunil Sharma
  • Pyrazolylmethylamine compounds as calcium channel modulators and preparation method thereof
    Patent number: 8299072
    Abstract: The present invention relates to pyrazolylmethylamine-piperazine derivatives and their pharmaceutically acceptable salts effective as calcium channel modulators and a method of manufacturing the same. The present invention also relates to the medicinal use of the above compounds as therapeutic treatment of diseases due to their effect as calcium channel modulators.
    Type: Grant
    Filed: September 28, 2009
    Date of Patent: October 30, 2012
    Assignee: Korea Institute of Science and Technology
    Inventors: Ghilsoo Nam, Kyung Il Choi, Hye Ran Kim, Seon Hee Seo, Yoon Jee Kim, Hee Sup Shin, Dong Jin Kim, Ae Nim Pae, Hye Jin Chung, Hyunah Choo, Hyewhon Rhim, Yong Seo Cho, Eun Joo Roh, Gyo Chang Keum, Kee Hyun Choi, Kye Jung Shin, Hoh Gyu Hahn, Chan Seong Cheong, Jae Kyun Lee, Kee Dal Nam, Yong Koo Kang, Youngsoo Kim, Woong Seo Park, Eunice Eun-Kyeong Kim, Key-Sun Kim, Hesson Chung, Dong Yun Shin, Chi man Song
  • Combination of Local and Systemic Immunomodulative Therapies for Enhanced Treatment of Cancer
    Publication number: 20120263677
    Abstract: A method for the treatment of cancer comprising administration of a therapeutically effective amount of an intralesional chemoablative pharmaceutical composition, or variant of said composition, in combination with a therapeutically effective amount of a systemic immunomodulatory anticancer agent. A further method for the treatment of cancer comprising administration of a therapeutically effective amount of an intralesional chemoablative pharmaceutical composition, or variant of said composition, in combination with a therapeutically effective amount of a systemic targeted anticancer agent. The present invention is further directed to pharmaceutical compositions for treatment of cancer. The intralesional chemoablative pharmaceutical composition can comprise an IL chemoablative agent comprising primarily a halogenated xanthene.
    Type: Application
    Filed: March 9, 2012
    Publication date: October 18, 2012
    Inventors: Craig J. Eagle, H. Craig Dees, Eric A. Wachter, Jamie Singer
  • 6-(3-aza-bicyclo[3.1.0]hex-3-yl)-2-phenyl-pyrimidines
    Patent number: 8288385
    Abstract: The present invention relates to 6-(3-aza-bicyclo[3.1.0]hex-3-yl)-2-phenyl-pyrimidine derivatives and their use as P2Y12 receptor antagonists in the treatment and/or prevention 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: Grant
    Filed: April 7, 2010
    Date of Patent: October 16, 2012
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Eva Caroff, Kurt Hilpert, Francis Hubler, Emmanuel Meyer, Dorte Renneberg
  • Melanocortin receptor agonists
    Patent number: 8288386
    Abstract: The present invention relates to a compound having a good agonistic activity to melanocortin receptor, or pharmaceutically acceptable salt or isomer thereof, and an agonistic composition for melanocortin receptor comprising the same as an active ingredient.
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: October 16, 2012
    Assignee: LG Life Sciences Ltd.
    Inventors: Koo Lee, Sang Dae Lee, Sang Pil Moon, In Ae Ahn, Sung Pil Choi, Hyun Ho Lee, Dong Sup Shim, Soo Yong Chung, Hyun Min Lee
  • METHODS INVOLVING PDGFRBETA INHIBITORS
    Publication number: 20120252736
    Abstract: The invention refers to PDGFRbeta inhibitor for use in the antiproliferative treatment of T-cell lymphoma, in particular NHL, ALCL and PTCL.
    Type: Application
    Filed: September 28, 2010
    Publication date: October 4, 2012
    Applicant: MEDIZINISCHE UNIVERSITAET WIEN
    Inventors: Lukas Kenner, Daniela Laimer
  • HEAT SHOCK PROTEIN BINDING COMPOUNDS, COMPOSITIONS, AND METHODS FOR MAKING AND USING SAME
    Publication number: 20120252818
    Abstract: The present subject matter relates to a compound represented by the general formula (I) or (I?) or a pharmacologically acceptable salt thereof; pharmaceutical compositions containing at least one of these compounds; methods of making at least one of these compounds; methods of using at least one of these compounds for treating and/or preventing various cancers and/or proliferation disorders; methods of using at least one of these compounds for monitoring the effectiveness of an anticancer therapy against various cancers. In one embodiment, the subject matter relates to compounds that bind with a level of specificity to heat shock protein 70 (Hsp70). In another embodiment, the subject matter relates to compounds that bind with a level of specificity to inhibit both heat shock protein 70 (Hsp70) and heat shock cognate protein 70 (Hsc70).
    Type: Application
    Filed: August 17, 2010
    Publication date: October 4, 2012
    Applicant: MEMORIAL SLOAN-KETTERING CANCER CENTER
    Inventors: Gabriela Chiosis, Tony Taldone, Anna Rodina, Pallav Patel, Yanlong Kang
  • NOVEL PIPERAZINE ANALOGS WITH SUBSTITUTED HETEROARYL GROUPS AS BROAD-SPECTRUM INFLUENZA ANTIVIRALS
    Publication number: 20120245176
    Abstract: A compound of Formula I is set forth, including pharmaceutically acceptable salts thereof: wherein Het is a 5 or 6-membered heterocycle with —N, —O, or —S adjacent to the —Ar substituent or adjacent to the point of attachment for the —Ar substituent; Ar is aryl or heteroaryl; R is —CH3, —CH2F, —CHF2 or —CH?CH2; V is —H, —CH3 or ?O; W is —NO2, —Cl, —Br, —CH2OH, or —CN; X is —Cl, —Br, —F, —CH3, —OCH3, or —CN; Y is —CH or —N; and Z is —CH or —N. This compound is useful in compositions for the prevention and treatment of influenza virus.
    Type: Application
    Filed: September 23, 2011
    Publication date: September 27, 2012
    Inventors: Christopher W. Cianci, Samuel Gerritz, Sean Kim, David R. Langley, Guo Li, Bradley C. Pearce, Annapurna Pendri, Shuhao Shi, Weixu Zhai, Shirong Zhu
  • Substituted Phenoxypropylcycloamine Derivatives as Histamine-3 (H3) Receptor Ligands
    Publication number: 20120238551
    Abstract: The present invention provides compounds of formula I: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.
    Type: Application
    Filed: December 22, 2011
    Publication date: September 20, 2012
    Applicants: Cephalon France, Cephalon, Inc.
    Inventors: Edward R. Bacon, Thomas R. Bailey, Sankar Chatterjee, Derek D. Dunn, Greg A. Hostetler, Robert L. Hudkins, Brigitte Lesur, Babu G. Sundar, Allizon L. Zulli, Christophe Yue
  • Substituted pyrimidines useful as protein kinase inhibitors
    Patent number: 8268829
    Abstract: The present invention provides a facile process for the preparation of tri- and tetra-substituted pyrimidines. The process is useful for preparing inhibitors of protein kinases, especially Aurora kinase. These inhibitors are useful for treating or lessening the severity of Aurora-mediated diseases or conditions.
    Type: Grant
    Filed: May 6, 2009
    Date of Patent: September 18, 2012
    Assignee: Vertex Pharmaceuticals Inc.
    Inventors: Jean-Damien Charrier, Francesca Mazzei, David Kay, Andrew Miller
  • METHODS AND COMPOSITIONS FOR THE TREATMENT OF MYELOPROLIFERATIVE DISEASES AND OTHER PROLIFERATIVE DISEASES
    Publication number: 20120225057
    Abstract: Compounds of the present invention, alone and in combination with other active agents, find utility in the treatment of hyperproliferative diseases, mammalian cancers and especially human cancers including but not limited to for example malignant melanomas, myeloproliferative diseases, chronic myelogenous leukemia, acute lymphocytic leukemia, a disease caused by c-ABL kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.
    Type: Application
    Filed: September 8, 2011
    Publication date: September 6, 2012
    Applicant: DECIPHERA PHARMACEUTICALS, LLC
    Inventors: Daniel L. Flynn, Michael D. Kaufman
  • PYRAZOLE COMPOUNDS AND THIAZOLE COMPOUNDS AS PROTEIN KINASES INHIBITORS
    Publication number: 20120225880
    Abstract: A compound of formula (I): wherein A, B, D, X, Y, R1, R2, R3, m, p, and q are defined herein. Also disclosed is a method for inhibiting FMS-like tyrosine kinase 3, aurora kinase, or vascular endothelial growth factor receptor.
    Type: Application
    Filed: March 1, 2012
    Publication date: September 6, 2012
    Applicant: National Health Research Institutes
    Inventors: Weir-Torn Jiaang, Tsu-An Hsu, Wen-Hsing Lin, Yu-Sheng Chao
  • OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION
    Publication number: 20120220561
    Abstract: The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: August 12, 2011
    Publication date: August 30, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Alessandra BARTOLOZZI, Todd BOSANAC, Zhidong CHEN, Stephane DE LOMBAERT, John D. HUBER, Ho Yin LO, Pui Leng LOKE, Weimin LIU, Tina Marie MORWICK, Alan OLAGUE, Doris RIETHER, Heather TYE, Lifen WU, Renee M. ZINDELL
  • TETRAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS
    Publication number: 20120214789
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5 and R6 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.
    Type: Application
    Filed: May 2, 2012
    Publication date: August 23, 2012
    Inventors: Michael Patrick Dillon, Ronald Charles Hawley, Li Chen, Lichun Feng, Minmin Yang
  • 6,5-HETEROCYCLIC PROPARGYLIC ALCOHOL COMPOUNDS AND USES THEREFOR
    Publication number: 20120214762
    Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Application
    Filed: March 15, 2012
    Publication date: August 23, 2012
    Applicant: Genentech, Inc.
    Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A.G.N. Montalbetti
  • UROTENSIN II RECEPTOR ANTAGONISTS
    Publication number: 20120214817
    Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.
    Type: Application
    Filed: April 30, 2012
    Publication date: August 23, 2012
    Inventors: Bruce E Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
  • OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION
    Publication number: 20120214787
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: August 23, 2011
    Publication date: August 23, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Alessandra BARTOLOZZI, Todd BOSANAC, Zhidong CHEN, Stephane DE LOMBAERT, Jonathon Alan DINES, John D. HUBER, Weimin LIU, Ho Yin LO, Pui Leng LOKE, Tina Marie MORWICK, Peter Allen NEMOTO, Alan OLAGUE, Doris RIETHER, Heather Tye, Lifen WU, Renee M. ZINDELL
  • Novel Heteroaryl Substituted Benzothiazoles
    Publication number: 20120207679
    Abstract: The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.
    Type: Application
    Filed: April 23, 2012
    Publication date: August 16, 2012
    Applicant: ASTRAZENECA AB
    Inventors: Ylva Gravenfors, Catrin Jonasson, Jonas Malmström, Gunnar Nordvall, David Pyring, Can Slivo, Daniel Sohn, Peter Ström, David Wensbo
  • NOVEL N-PYRIMIDIN-4-YL-3-AMINO-PYRROLO[3,4-C]PYRAZOLE DERIVATIVES AS PKC KINASE INHIBITORS
    Publication number: 20120202809
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disase pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.
    Type: Application
    Filed: April 18, 2012
    Publication date: August 9, 2012
    Inventors: Hui Li, Seiji Nukui, Stephanie Anne Scales, Min Teng, Chunfeng Yin
  • METHODS TO IDENTIFY TARGETS AND MOLECULES REGULATING PURINOSOMES AND THEIR USES
    Publication number: 20120190620
    Abstract: The present invention discloses methods to identify targets, pathways and molecules regulating purinosomes and their uses for treating pathophysiological disorders associated with purinosomes. Disclosed are methods related to both label-free cellular assays and fluorescence imaging to confirm the regulatory roles of various targets and molecules in purinosome dynamics. Disclosed are methods to classify molecules and the uses of these molecules for different indications. Specifically, the purinosome-disrupting molecules can be used for improved prevention and treatment of cancer development.
    Type: Application
    Filed: July 18, 2011
    Publication date: July 26, 2012
    Inventors: Stephen Benkovic, Ye Fang, Songon An, Florence Verrier
  • MOLECULAR DIAGNOSTIC METHODS FOR PREDICTING BRAIN METASTASIS OF BREAST CANCER
    Publication number: 20120184560
    Abstract: Disclosed are molecular diagnostic compositions and methods for predicting brain metastasis of breast cancer, as well as methods for drug repositioning to identify existing and new therapeutics for use in developing individualized, patient-specific treatment regimens for improving diagnoses and patient outcomes in individuals at risk for brain metastasis of breast cancer.
    Type: Application
    Filed: September 26, 2011
    Publication date: July 19, 2012
    Applicant: The Methodist Hospital Research Institute
    Inventors: Stephen T.C. Wong, Hong Zhao
  • Hepatitis C virus inhibitors
    Patent number: 8221737
    Abstract: 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: Grant
    Filed: June 15, 2010
    Date of Patent: July 17, 2012
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
  • 1, 2, 4-triazole derivatives as serotonergic modulators
    Patent number: 8222254
    Abstract: The invention relates to novel 5-hydroxytryptamine (5-HT) receptor modulator compounds of formula (I); wherein A, B, R1-R5, T, W, X, Y, Z and m are defined herein, to pharmaceutical compositions comprising these compounds and to their use in the treatment of conditions associated with 5-HT action.
    Type: Grant
    Filed: August 6, 2008
    Date of Patent: July 17, 2012
    Assignee: Prosarix Limited
    Inventors: Jonathan Richard Heal, Joseph Michael Sheridan, William Dennys Ormrod Hamilton, Simon James Grimshaw, Sorin Vasile Filip
  • PTEN PHOSPHORYLATION-DRIVEN RESISTANCE TO CANCER TREATMENT AND ALTERED PATIENT PROGNOSIS
    Publication number: 20120165340
    Abstract: Indicators that can guide clinical decisions in cancer, particularly posttranslational modification of proteins which result in altered prognosis and differential sensitivity to targeted cancer therapy, are provided. In particular, monitoring of phosphorylation of PTEN may be utilized to predict or assess drug response, drug sensitivity, and clinical outcome. Modulation of PTEN phosphorylation may be utilized to alter sensitivity and outcome in cancer patients. Posttranslational modification of PTEN, particularly phosphorylation, is correlated with resistance to targeted cancer therapy, including EGFR inhibitors, and with reduced survival prognosis. Methods and assays for determining phosphorylation of PTEN, particularly Y240 phosphorylation, are provided. Methods for sensitizing tumors to inhibition and targeted therapy by modulating PTEN phosphorylation are provided.
    Type: Application
    Filed: February 11, 2010
    Publication date: June 28, 2012
    Applicant: Ludwing Institute for Cancer Research Ltd.
    Inventors: Frank Furnari, Webster Cavenee, Timothy Fenton
  • METHODS AND COMPOSITIONS FOR MODULATION OF BLOOD-NEURAL BARRIER
    Publication number: 20120156187
    Abstract: Methods and compositions for modulating blood-neural barrier (BNB) for the treatment of CNS conditions such as edema, and for increased drug delivery efficacy across the BNB. The present invention further relates to improved tPA treatment of ischemic cerebrovascular and related diseases in combination with antagonism of the PDGF signaling pathway. The inventive method and composition is particularly suitable for conjunctive therapy of ischemic stroke using tPA and an anti-PDGF-C antagonist or an anti-PDGFR-? antagonist.
    Type: Application
    Filed: February 28, 2012
    Publication date: June 21, 2012
    Applicants: LUDWIG INSTITUTE FOR CANCER RESEARCH, THE REGENTS OF THE UNIVERSITY OF MICHIGAN, UNIVERSITY OF MARYLAND, BALTIMORE
    Inventors: Ulf Eriksson, Daniel Lawrence, Enming Joe Su, Dudley Strickland, Manuel Yepes, Linda Fredriksson
  • 4-piperazinyl-pyrimidine compounds suitable for treating disorders that respond to modulation of the dopamine Dreceptor
    Patent number: 8202868
    Abstract: The present invention relates to novel 4-piperazinylpyrimidine compounds. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D3 receptor. The 4-piperzinylpyrimidine compounds have the general formula I wherein Ar, X, A, R1 and R1a are as defined in the claims.
    Type: Grant
    Filed: August 8, 2005
    Date of Patent: June 19, 2012
    Assignee: Abbott GmbH & Co. KG
    Inventors: Andreas Haupt, Liliane Unger, Karla Drescher, Ana Lucia Jongen-Relo, Roland Grandel, Wilfried Braje, Herve Geneste
  • Substituted oxindole derivatives, medicaments containing the latter and use thereof
    Patent number: 8202870
    Abstract: The invention relates to novel oxindole derivatives of general formula (I), in which the substituents R1, R2, R3, Y1, Y2, m, n, W, X, B and Z are defined as cited in claim 1, to medicaments containing said derivatives and to the use of the latter for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases
    Type: Grant
    Filed: March 23, 2006
    Date of Patent: June 19, 2012
    Assignee: Abbott GmbH & Co. KG
    Inventors: Wilfried Lubisch, Thorsten Oost, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Hervé Geneste
  • MICROBIOCIDAL HETEROCYCLES
    Publication number: 20120142698
    Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or X—N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.
    Type: Application
    Filed: August 6, 2010
    Publication date: June 7, 2012
    Applicant: SYNGENTA CROP PROTECTION, LLC
    Inventors: Sarah Sulzer-Mosse, Clemens Lamberth, Laura Quaranta, Mathias Stephan Respondek
  • SUBSTITUTED INDOLE/INDAZOLE-PYRIMIDINYL COMPOUNDS
    Publication number: 20120142696
    Abstract: The present disclosure provides indole/indazole-pyrimidinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): wherein W, X, R1, R2, R3, R4, R5 and R6 are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating p38 kinase mediated diseases using the compound.
    Type: Application
    Filed: December 6, 2011
    Publication date: June 7, 2012
    Inventors: Shaun R. Selness, Joseph B. Monahan, John F. Schindler, Balekudru Devadas
  • SUBSTITUTED OXINDOLE DERIVATIVES, MEDICAMENTS CONTAINING THE LATTER AND USE THEREOF
    Publication number: 20120136001
    Abstract: The invention relates to novel oxindole derivatives of general formula (I), in which the substituents A, B, R1, R2 and R3 are defined as cited in claim 1, to medicaments containing said derivatives and to the use of the latter for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.
    Type: Application
    Filed: January 30, 2012
    Publication date: May 31, 2012
    Inventors: Wilfried Lubisch, Thorsten Oost, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Hervé Geneste
  • Crystalline (3-cyano-1H-indol-7-yl)-[4-(4-fluorophenethyl) piperazin-1-yl]methanone phosphate
    Patent number: 8188087
    Abstract: The present invention relates to novel crystalline forms of (3-cyano-1H-indol-7-yl)-[4-(4-fluorophenethyl)piperazin-1-yl]methanone phosphate and to pharmaceutical compositions containing said forms.
    Type: Grant
    Filed: April 24, 2007
    Date of Patent: May 29, 2012
    Assignee: Merck Patent GmbH
    Inventors: Susan Marie Reutzel-Eden, Gregory Alan Stephenson
  • PIPERAZINYL DERIVATIVES USEFUL AS MODULATORS OF THE NEUROPEPTIDE Y2 RECEPTOR
    Publication number: 20120129870
    Abstract: The present invention is directed to piperidinyl and piperazinyl derivatives of formula (II) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and/or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor.
    Type: Application
    Filed: December 17, 2008
    Publication date: May 24, 2012
    Inventors: Wenying Chai, Jill A. Jablonowski, Dale A. Rudolph, Chandravadan R. Shah, Devin M. Swanson, Victoria D. Wong
  • SUBSTITUTED DIHYDROPYRAZOLONES FOR TREATING CARDIOVASCULAR AND HEMATOLOGICAL DISEASES
    Publication number: 20120121727
    Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.
    Type: Application
    Filed: January 23, 2012
    Publication date: May 17, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Kai THEDE, Ingo FLAMME, Felix OEHME, Jens-Kerim ERGÜDEN, Friederike STOLL, Joachim SCHUHMACHER, Hanno WILD, Peter KOLKHOF, Hartmut BECK, Jörg KELDENICH, Metin AKBABA, Mario JESKE
  • Substituted Pyrrolo-Pyrimidine Derivatives, Process for Their Preparation and Their Use as Kinase Inhibitors
    Publication number: 20120122882
    Abstract: Substituted pyrrolo-pyrimidine 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 dysregulated protein kinase activity, like cancer.
    Type: Application
    Filed: September 25, 2008
    Publication date: May 17, 2012
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Michele Caruso, Italo Beria, Maria Gabriella Brasca, Helena Posteri, Marina Caldarelli, Walter Ceccarelli, Barbara Valsasina
  • NOVEL INHIBITORS OF HEPATITIS C VIRUS
    Publication number: 20120114600
    Abstract: The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: November 3, 2011
    Publication date: May 10, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Robert Murray McKINNELL, Daniel D. LONG, Lori Jean VAN ORDEN, Lan JIANG, Mandy LOO, Daisuke Roland SAITO, Shella ZIPFEL, Eric L. Stangeland, Kassandra Lepack, Gavin Ogawa
  • Low Viscosity, Highly Flocculated Triamcinolone Acetonide Suspensions for Intravitreal Injection
    Publication number: 20120115829
    Abstract: Triamcinolone acetonide suspension compositions are disclosed. The suspension compositions have a relatively low viscosity and are easy to extrude through a 27- or 30-gauge needle but are highly flocculated and easily redispersed. The compositions are particularly suitable for intravitreal injection.
    Type: Application
    Filed: January 17, 2012
    Publication date: May 10, 2012
    Applicant: Alcon Research, Ltd.
    Inventors: Bhagwati P. Kabra, Ruma Sarkar