Plural Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/234.5)
-
Publication number: 20130029964Abstract: An object of the present invention is to provide a novel low molecular weight compound exhibiting an osteogenesis-promoting action. This object is achieved by a compound having the general formula (I) or a pharmacologically acceptable salt thereof. In the general formula (I), R1 and R2 represent hydrogen atoms, and the like; R3 represents a hydrogen atom, and the like; X, Y, and Z represent nitrogen atoms, and the like; A represents a phenylene group, and the like; n represents 1 or 2, and the like; and V and W represent oxygen atoms, and the like.Type: ApplicationFiled: August 27, 2012Publication date: January 31, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Kazumasa Aoki, Satoshi Matsui, Kenji Yoshikawa, Hiroki Shimizu, Junko Sasaki, Katsuyoshi Nakajima, Osamu Kanno, Kiyoshi Oizumi
-
Publication number: 20130023525Abstract: The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.Type: ApplicationFiled: April 24, 2012Publication date: January 24, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Paul S. Charifson, David D. Deininger, Anne-Laure Grillot, Yusheng Liao, Steven Ronkin, Dean Stamos, Emanuele Perola, Tiansheng Wang, Arnaud Le Tiran, Joseph Drumm
-
Publication number: 20130018040Abstract: Compositions and methods for the treatment of toxoplasmosis, caused by the infectious eukaryotic parasite Toxoplasma gondii (T. gondii) and for the treatment of cryptosporidiosis, caused by the infectious eukaryotic parasites Cryptosporidium parvum (C. parvum) and Cryptosporidium hominus (C. hominus) are described. In particular, the present disclosure is directed to compositions and methods for inhibiting either T. gondii calcium dependent protein kinases (TgCDPKs) or C. parvum and C. hominus calcium dependent protein kinases (CpCDPKs) using pyrazolopyrimidine and/or imidazo[1,5-a]pyrazine inhibitors, of the formula, wherein the variables X, Y, Z, L, R1, and R3 are defined herein.Type: ApplicationFiled: July 30, 2012Publication date: January 17, 2013Applicant: University of Washington through its Center for CommercializationInventors: Wesley C. VAN VOORHIS, Wilhelmus G.J. HOL, Eric T. LARSON, Dustin James MALY, Ethan MERRITT, Kayode K. OJO
-
Publication number: 20130018043Abstract: 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 the variables 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: July 11, 2012Publication date: January 17, 2013Inventors: Joseph A. Bilotta, Adrian Wai-Hing Cheung, Fariborz Firooznia, Kevin Richard Guertin, Stuart Hayden, Nancy-Ellen Haynes, Christine M. Lukacs-Lesburg, Nicholas Marcopulos, Eric Mertz, Lida Qi, Yimin Qian, Sung-Sau So, Jenny Tan, Kshitij C. Thakkar
-
Publication number: 20130018033Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: ApplicationFiled: August 27, 2010Publication date: January 17, 2013Applicant: ARRAY BIOPHARMA INC.Inventors: Ignacio Aliagas, Stefan Gradl, Janet Gunzner, Wendy Lee, Simon Mathieu, Joachim Rudolph, Zhaoyang Wen, Guiling Zhao, Alexandre J. Buckmelter, Jonas Grina, Joshua D. Hansen, Ellen Laird, David Moreno, Li Ren, Steven Mark Wenglowsky
-
Publication number: 20130018041Abstract: This invention is directed to compounds of formula (I): where n, m, Y, R1, R2, R3, R4 and R5 are disclosed herein, as isolated stereoisomers or mixtures thereof, or pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising the compounds of formula (I); and methods of using the compounds and the pharmaceutical compositions in treating diseases or conditions associated with JAK2 activity.Type: ApplicationFiled: September 14, 2012Publication date: January 17, 2013Applicant: Rigel Pharmaceutical, Inc.Inventors: Somasekhar Bhamidipati, Jeffrey Clough, Ankush Argade, Rajinder Singh, Vadim Markovtosov, Pingyu Ding, Jiaxin Yu, Andy Atuegbu, Hui Hong, Ihab Darwish, Sambaiah Thota
-
Publication number: 20130018039Abstract: Disclosed are compounds having the formula: wherein R1A, R1B, R2 and R3 are defined herein, and methods of making and using the same.Type: ApplicationFiled: March 31, 2011Publication date: January 17, 2013Inventors: Vera Q. Bodmer, Linda N. Casillas, Michael P. DeMartino, Philip A. Harris, Bryan W. King, Ami Lakdawala Shah, Lara Kathryn Leister, Joshi M. Ramanjulu, Joseph J. Romano, Gren Z. Wang, Matthew A. Wilson, David Duff Wisnoski
-
Publication number: 20130018036Abstract: Substituted indazole 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 deregulated protein kinase activity, like cancer.Type: ApplicationFiled: September 12, 2012Publication date: January 17, 2013Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Andrea LOMBARDI BORGIA, Maria MENICHINCHERI, Paolo ORSINI, Achille PANZERI, Ettore PERRONE, Ermes VANOTTI, Marcella NESI, Chiara MARCHIONNI
-
Patent number: 8354399Abstract: Substituted indazole 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 deregulated protein kinase activity, like cancer.Type: GrantFiled: December 15, 2009Date of Patent: January 15, 2013Assignee: Nerviano Medical Sciences S.R.L.Inventors: Maria Menichincheri, Jay Aaron Bertrand, Chiara Marchionni, Marcella Nesi, Paolo Orsini, Achille Panzeri
-
Publication number: 20130012508Abstract: The present invention relates to chemical compounds of general formula (I) which may possess useful therapeutic activity in a range of central nervous system disorders, and in particular, anxiety disorders.Type: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Applicant: Bionomics LimitedInventors: Jonathan Bayldon Baell, Brad Sleebs, Bernard Luke Flynn, Ian Phillip Street, Nurul Quazi, Chinh Thien Bui
-
Publication number: 20130012489Abstract: The invention relates to compounds of the formulae (I), (II) and (III) in which R1, R2, R3, R4, Y, W1, W2, L, A, Alk, Cyc, Ar, Het1, Het2, Hal and n have the meaning indicated in claim 1, and/or physiologically acceptable salts, tautomers and stereo-isomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formulae (II) and (III) and optionally conversion of a base or acid of the compounds of the formula (I) into one of their salts.Type: ApplicationFiled: February 17, 2011Publication date: January 10, 2013Applicant: MERCK PATENT GMBHInventors: Werner Mederski, Thomas Fuchss, Frank Zenke
-
Publication number: 20130012511Abstract: The invention relates to compounds having the structure of Formula (I) and pharmaceutically acceptable salts thereof, which are soluble guanylate cyclase activators. The compounds are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver.Type: ApplicationFiled: March 22, 2011Publication date: January 10, 2013Inventors: Darby Schmidt, Subharekha Raghavan, John Stelmach, Jian Guo, Jonathan Groeper, Linda Brockunier, Keith Rosauer, Hong Shen, Rui Liang, Fa-Xiang Ding
-
Publication number: 20130012510Abstract: The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of novel 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1 and CX3CR1, and to their use in a method for treating or preventing diseases based on the expression of MCP-1 and CX3CR1.Type: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Applicant: AZIENDE CHIM. RIUN. ANGEL. FRA. A.C.R.A.F. S.p.A.Inventors: Angelo GUGLIELMOTTI, Guido FURLOTTI, Giorgina MANGANO, Nicola CAZZOLLA
-
Publication number: 20130012509Abstract: The present invention relates to chemical compounds of general formula (I) which may possess useful therapeutic activity in a range of central nervous system disorders, and in particular, anxiety disorders.Type: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Applicant: Bionomics LimitedInventors: Jonathan Bayldon Baell, Brad Sleebs, Bernard Luke Flynn, Ian Philip Street, Nurul Quazi, Chinh Thien Bui
-
Publication number: 20130012493Abstract: The present invention relates to compounds of the general formula (I): wherein ring A, ring B, G, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.Type: ApplicationFiled: March 22, 2011Publication date: January 10, 2013Inventors: He Zhao, Ping Chen, Peishan Lin, Peng Dai, Jason Louis Davis, Duane E. DeMong, Michael W. Miller, Xing Dai, Michael K. Wong, Brian J. Lavey, Wensheng Yu, Guowei Zhou, Andrew W. Stamford, Joseph A. Kozlowski, William J. Greenlee
-
Publication number: 20130011408Abstract: The current disclosure provides for specific peptides from the Epidermal Growth Factor Receptor (EGFR) protein and the derived ionization characteristics of those peptides that are advantageous for quantifying the EGFR directly in formalin fixed biological samples by the method of Selected Reaction Monitoring (SRM) mass spectrometry. Such fixed biological samples include: formalin-fixed tissue/cells, formalin-fixed/paraffin embedded (FFPE) tissue/cells, FFPE tissue blocks and cells from those blocks, and formalin fixed and paraffin embedded tissue culture cells. EGFR protein is quantitated in biological samples by the method of SRM/MRM mass spectrometry by quantitating one or more of the peptides described herein. The peptides can be quantitated if they reside in a modified or an unmodified form. Examples of potentially modified forms of an EGFR peptides include those bearing phosphorylation of a tyrosine, threonine, serine, and/or other amino acid residues within the peptide sequence.Type: ApplicationFiled: June 21, 2012Publication date: January 10, 2013Applicant: EXPRESSION PATHOLOGY, INC.Inventors: David B. Krizman, Todd Hembrough, Sheeno Thyparambil
-
Publication number: 20130005724Abstract: The present invention relates to derivatives of pyridino-pyridinones, and to their preparation and use thereof, having activity as inhibitors of kinase activity of receptors for PDGF (platelet derived growth factors) ligands and optionally of receptors for the FLT3 (fms-like tyrosine kinase receptor) ligand receptors, said derivatives comprising compounds of formula (I): wherein the various substituent groups are more specifically defined herein. The compounds are suitable as therapeutics for the treatment of various proliferative diseases.Type: ApplicationFiled: May 22, 2012Publication date: January 3, 2013Applicant: SANOFIInventors: Gilbert LASSALLE, Valérie MARTIN, Gary MCCORT, Cécile VOLLE-CHALLIER
-
Publication number: 20130005727Abstract: The invention concerns quinazoline derivatives of Formula I wherein each of Q1, Z, R1 and Q2 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosine kinases.Type: ApplicationFiled: September 10, 2012Publication date: January 3, 2013Applicant: ASTRAZENECA ABInventors: Robert Hugh BRADBURY, Laurent Francois Andre HENNEQUIN, Jason Grant KETTLE
-
Publication number: 20130005726Abstract: A method for treating in a subject with an inflammatory disorder and/or immunological disorder associated with NOD2 activation includes administering to the subject a therapeutically effective amount of at least one tyro sine kinase inhibitor that substantially inhibits nucleotide-binding oligomerization domain containing 2 (NOD2):receptor-interacting protein 2 (RIP2) signaling in a NOD2-bearing cell and is not cytotoxic to the cell.Type: ApplicationFiled: March 8, 2011Publication date: January 3, 2013Inventors: Derek Abbott, Justine Tigno-Aranjuez
-
Publication number: 20130005725Abstract: There is provided pyrimidinyl compounds of Formula (I), wherein: R2 is or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: July 2, 2012Publication date: January 3, 2013Applicant: AstraZeneca ABInventors: Kevin Michael Foote, Johannes Wilhelmus Maria Nissink, Paul Turner
-
Patent number: 8343954Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds.Type: GrantFiled: July 27, 2011Date of Patent: January 1, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
-
Publication number: 20120329795Abstract: The invention concerns quinazoline derivatives of Formula I: wherein each of R1, X1, R2, R3, R5, n and m have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of EGF and erbB receptor tyrosine kinases.Type: ApplicationFiled: September 10, 2012Publication date: December 27, 2012Inventors: Laurent Francois Andre Hennequin, Bernard Christophe Barlaam, Robert Hugh Bradbury
-
Publication number: 20120329794Abstract: The present invention provides an Abelson kinase (Abl kinase) inhibitor which comprises, as an active ingredient, an indazole derivative represented by Formula (I) (wherein R1 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group) or a pharmaceutically acceptable salt thereof, an Abl kinase inhibitor which comprises, as an active ingredient, an indazole derivative represented by Formula (Ia) [wherein R2 represents CONR4aR4b (wherein R4a and R4b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like, or R4a and R4b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group) or the like, and R3 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like] or a pharmaceutically acceptable salt thereof, and the like.Type: ApplicationFiled: June 29, 2007Publication date: December 27, 2012Applicant: Kyowa Hakko Kirin Co., Ltd.Inventors: Yukimasa Shiotsu, Kenichi Ishii, Hiroshi Umehara, Shiro Akinaga
-
Publication number: 20120329778Abstract: The present invention relates to bicyclic heterocycles of general formula wherein Ra to Rc, A to E and X are defined as in claim 1, the tautomers, stereoisomers and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.Type: ApplicationFiled: September 5, 2012Publication date: December 27, 2012Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank HIMMELSBACH, Elke LANGKOPF, Thomas METZ, Flavio SOLCA, Birgit JUNG, Anke BAUM
-
Patent number: 8338414Abstract: A novel method for immunosuppressive in a mammal suffering from an immune disease, including administering to the mammal a therapeutically effective amount of a heterocyclic compound represented by the general formula (I) (wherein X or other variables are as defined in the specification) or a pharmaceutically acceptable salt thereof is disclosed. A novel heterocyclic compound represented by the general formula (II) (wherein X or other variables are as defined in the specification) or a pharmaceutically acceptable salt thereof is also disclosed.Type: GrantFiled: May 24, 2010Date of Patent: December 25, 2012Assignee: Zenyaku Kogyo KabushikiKaishaInventors: Kazuhiko Haruta, Shinichi Yaguchi, Toshiyuki Matsuno, Yoshio Tsuchida, Tetsuo Watanabe, Kimitomo Yoshioka, Ryogo Yui
-
Publication number: 20120321615Abstract: 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: ApplicationFiled: May 25, 2012Publication date: December 20, 2012Inventors: Emanuel Petricoin, III, Lance A. Liotta, Mariaelena Pierobon, Valerie Calvert
-
Publication number: 20120315247Abstract: 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: ApplicationFiled: August 17, 2012Publication date: December 13, 2012Applicants: SUNSHINE LAKE PHARMA CO., LTD.Inventor: Ning Xi
-
Publication number: 20120316165Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, X, Z, Ar, and n are as described in the claims, Ar is phenyl or heteroaryl, selected from the group consisting of 1H-indazole-3yl, pyridine-2-yl, pyridine-3-yl, pyridine-4-yl, pyrimidine-5-yl, 1H-pyrazole-3-yl, 1H-pyrazole-4-yl and 1H-pyrazole-5-yl; or to a pharmaceutically suitable acid addition salt thereof, which may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse, metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: June 1, 2012Publication date: December 13, 2012Inventors: Guido Galley, Roger Norcross, Philippe Pflieger
-
Publication number: 20120316166Abstract: Novel hetarylaminonaphthyridine derivatives of formula (I) wherein X, R1, R2, R3, R4, W1, W2, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.Type: ApplicationFiled: January 10, 2011Publication date: December 13, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Alfred Jonczyk, Dieter Dorsch, Frank Zenke, Christiane Amendt
-
Publication number: 20120316164Abstract: The present invention provides a method for inhibiting the growth of cancer stem cells, particularly colorectal cancer stem cells, liver cancer stem cells, lung cancer stem cells or breast cancer stem cells, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of antimycin A or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier.Type: ApplicationFiled: June 13, 2011Publication date: December 13, 2012Inventors: CHI-YING HUANG, CHI-TAI YEH, CHUN-HUNG WU, YU-WEN LIU
-
Publication number: 20120309756Abstract: Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use thereof.Type: ApplicationFiled: July 11, 2012Publication date: December 6, 2012Inventors: Jiazhong Zhang, Prabha N. Ibrahim, Dean R. Artis, Ryan Bremer, Guoxian Wu, Hongyao Zhu, Marika Nespi, Chao Zhang
-
Publication number: 20120309736Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.Type: ApplicationFiled: February 21, 2011Publication date: December 6, 2012Inventors: Jinlong Jiang, Andrew J. Kassick, Ahmet Kekec, Iyassu K. Sebhat
-
Publication number: 20120309739Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: November 3, 2010Publication date: December 6, 2012Applicant: ALMAC DISCOVERY LIMITEDInventors: Mark Peter Bell, Colin Roderick O'Dowd, James Samuel Shane Rountree, Graham Peter Trevitt, Timothy Harrison, Mary Melissa McFarland
-
Publication number: 20120308567Abstract: The invention relates to methods and kits for the treatment of prevention of and lowering the chances of developing prolactinomas by the administration of a tyrosine kinase inhibitor, such as lapatinib.Type: ApplicationFiled: January 31, 2011Publication date: December 6, 2012Applicant: CEDARS-SINAI MEDICAL CENTERInventors: Hidenori Fukuoka, Odelia Cooper, Shlomo Melmed
-
Publication number: 20120309738Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), to pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R3, R4, R6, R2, R7, R8, R9, Ra, Rb have meanings given in the description.Type: ApplicationFiled: December 8, 2011Publication date: December 6, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning Priepke, Raimund Kuelzer, Juergen Mack, Roland Pfau, Dirk Stenkamp, Benjamin Pelcman, Robert Roenn, Dimitrijs Lubriks, Edgars Suna
-
Patent number: 8324205Abstract: The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.Type: GrantFiled: May 22, 2009Date of Patent: December 4, 2012Assignees: Millennium Pharmaceuticals, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: Anjali Pandey, Robert M. Scarborough, Kenji Matsuno, Michio Ichimura, Yuji Nomoto, Shinichi Ide, Eiji Tsukuda, Junko Sasaki, Shoji Oda
-
Patent number: 8324200Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: GrantFiled: January 22, 2010Date of Patent: December 4, 2012Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Sambaiah Thota, Rose Yen
-
Patent number: 8324206Abstract: A thienopyrimidine of formula (I): and the pharmaceutically acceptable salts thereof have activity as inhibitors of PI3K with selectivity for the P110? subtype, and may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour, particularly those associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.Type: GrantFiled: July 20, 2010Date of Patent: December 4, 2012Assignee: F. Hoffmann-La Roche AGInventors: Irina Chuckowree, Adrian Folkes, Tim Hancox, Stephen Shuttleworth
-
Publication number: 20120301470Abstract: The invention relates to methods and kits for the treatment of, prevention of, and lowering the chances of developing Cushing's Disease and/or hypercortisolism by the administration of a tyrosine kinase inhibitor, such as gefitinib.Type: ApplicationFiled: January 31, 2011Publication date: November 29, 2012Applicant: CEDARS-SINAI MEDICAL CENTERInventors: Hidenori Fukuoka, Shlomo Melmed
-
Publication number: 20120302544Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: August 3, 2012Publication date: November 29, 2012Inventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
-
Publication number: 20120301427Abstract: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HW).Type: ApplicationFiled: January 25, 2012Publication date: November 29, 2012Inventors: Gary BRIDGER, Al KALLER, Curtis HARWIG, Renato SKERLJ, David BOGUCKI, Trevor R. WILSON, Jason CRAWFORD, Ernest J. MCEACHERN, Bem ATSMA, Siqiao NAN, Yuanxi ZHOU, Dominique SCHOLS, Christopher D. SMITH, Maria R. DI FLURI
-
Publication number: 20120294930Abstract: The present invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth.Type: ApplicationFiled: February 23, 2012Publication date: November 22, 2012Applicant: Intellikine LLCInventors: Pingda Ren, Yi Liu, Katayoun Jessen, Xin Guo, Christian Rommel, Troy Edward Wilson
-
Publication number: 20120295885Abstract: This application discloses compounds according to generic Formula I: wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.Type: ApplicationFiled: May 16, 2012Publication date: November 22, 2012Inventors: Roland Joseph Billedeau, Rama K. Kondru, Francisco Javier Lopez-Tapia, Yan Lou, Timothy D. Owens, Yimin Qian, Sung-Sau So, Kshitij C. Thakkar, Jutta Wanner
-
Publication number: 20120294872Abstract: A signature for breast cancer tissue derived from a patient is established that is indicative of the virulence and risk of lung metastasis by determining the expression levels to define a sample signature, and comparing this sample signature to a reference signature. This determination is used to define appropriate treatment and monitoring options for the patient. Risk of metastasis to the lung can be reduced by treatment with a therapeutic combination that either (1) contains a first agent effective to inhibit epiregulin activity and a second agent effective to inhibit activity of a protein selected from the group consisting of MMP1, MMP2 and PTGS2, or (2) contains a therapeutic agent or combination of agents effective to inhibit activity MMP1, MMP2 and PTGS2. Agents that inhibit the CXCL1 pathway also can be used individually or in combination with these combinations.Type: ApplicationFiled: April 16, 2012Publication date: November 22, 2012Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCHInventors: Gaorav P. Gupta, Joan Massague, Andy J. Minn
-
Publication number: 20120295902Abstract: Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.Type: ApplicationFiled: December 17, 2010Publication date: November 22, 2012Applicant: MERCK PATENT GMBHInventors: Alfred Jonczyk, Dieter Dorsch, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
-
Publication number: 20120295904Abstract: The present embodiments relate to compounds with physiological effects, such as the activation of hematopoietic growth factor receptors. The present embodiments also relate to use of the compounds to treat a variety of conditions, diseases and ailments such as hematopoietic conditions and disorders.Type: ApplicationFiled: October 12, 2010Publication date: November 22, 2012Applicant: LIGAND PHARMACEUTICALS INC.Inventors: Lin Zhi, Andrew R. Hudson, Cornelis A. Van Oeveren, Steven L. Roach, Bijan Pedram, Yixing Shen, Lino J. Valdez, Jillian Basinger, Virginia Heather Sharron Grant, Jason C. Pickens
-
Patent number: 8314099Abstract: The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of novel 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1 and CX3CR1, and to their use in a method for treating or preventing diseases based on the expression of MCP-1 and CX3CR1.Type: GrantFiled: March 6, 2009Date of Patent: November 20, 2012Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.Inventors: Angelo Guglielmotti, Guido Furlotti, Giorgina Mangano, Nicola Cazzolla
-
Publication number: 20120289500Abstract: Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein ring G1, R1, and R2 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.Type: ApplicationFiled: May 8, 2012Publication date: November 15, 2012Applicant: ABBOTT LABORATORIESInventors: Brian S. Brown, Tongmei Li, Sridhar Peddi, Arturo Perez-Medrano, David DeGoey
-
Publication number: 20120289504Abstract: This invention generally relates to substituted benzoimidazole compounds, particularly methyl 2-((2-(2,6-difluoro-4-(methylcarbamoyl)phenyl)-5-methyl-1H-benzo[d]imidazol-1-yl)methyl)morpholine-4-carboxylate and salts thereof. This invention also relates to pharmaceutical compositions and kits comprising such a compound, uses of such a compound (including, for example, treatment methods and medicament preparations), processes for making such a compound, and intermediates used in such processes.Type: ApplicationFiled: May 16, 2012Publication date: November 15, 2012Applicant: ASTRAZENECA ABInventors: Louis-David Cantin, Xuehong Luo, Miroslaw Jerzy Tomaszewski
-
Patent number: RE43878Abstract: The present invention provides amidophenoxyindazole compounds useful in the treatment of cancer.Type: GrantFiled: December 8, 2011Date of Patent: December 25, 2012Assignee: Eli Lilly and CompanyInventors: Tiechao Li, Mark Andrew Pobanz, Chuan Shih, Zhipei Wu, Wei Jennifer Yang, Boyu Zhong