Bicyclo Ring Having The Additional Six-membered Nitrogen Hetero Ring As One Of The Cyclos Patents (Class 514/253.04)
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Publication number: 20120135989Abstract: The present invention provides a (di)azaindole derivative represented by the formula (I). A compound of the present invention inhibits a Cdc7 protein kinase activity and suppresses cell proliferation.Type: ApplicationFiled: June 29, 2011Publication date: May 31, 2012Applicants: CRYSTALGENOMICS, INC., SBI BIOTECH CO., LTD.Inventors: Yoko Funakoshi, Chika Tanaka, Choul Hong Park, Seong Gu Ro
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Publication number: 20120129853Abstract: This invention pertains to methods of treating systemic lupus erythematosus, lupus nephritis or Sjogren's Syndrome with compounds that selectively inhibit the activity of Bcl-2 anti-apoptotic proteins. Specifically, the current invention is directed to treatment with compounds that selectively inhibit the activity of Bcl-2 proteins, with a lesser affinity for inhibiting the activity of other BCL-2 family proteins, including Bcl-xL.Type: ApplicationFiled: November 22, 2011Publication date: May 24, 2012Applicant: Abbott LaboratoriesInventors: Steven Elmore, Andrew Souers, Li Chun Wang, Tariq Ghayur, Stuart J. Perper
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Publication number: 20120129852Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, (I) are useful as kinase modulators, including Btk modulation, wherein A1, A2, A3, R4 are as defined herein.Type: ApplicationFiled: August 11, 2010Publication date: May 24, 2012Inventors: Jingwu Duan, Bin Jiang, Zhonghui Lu
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Publication number: 20120121540Abstract: Provided are certain chemical entities, pharmaceutical compositions, and methods of treatment of a member of the flaviviradae family of viruses such as hepacivirus (Hepatitis C or HCV).Type: ApplicationFiled: August 8, 2008Publication date: May 17, 2012Inventors: Franz Ulrich Schmitz, Vincent W.F Tai, Roopa Ral, Christopher Don Roberts, Ali Dehghani Mohammad Abadi, Subramanian Baskaran, Irina Slobodov, Jack Maung, Martin Leon Neitzel
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Publication number: 20120122858Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: ApplicationFiled: January 20, 2012Publication date: May 17, 2012Applicant: Incyte CorporationInventors: Wenqing Yao, Chunhong He, David M. Burns, Jincong Zhuo, Meizhong Xu, Colin Zhang, Ding-Quan Qian, Brian Metcalf
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Publication number: 20120122817Abstract: Compounds of formula (IA) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: May 28, 2010Publication date: May 17, 2012Applicant: ASTRAZENECA ABInventors: Neil Bifulco, Allison Laura Choy, Olga Quiroga, Brian Alan Sherer
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Publication number: 20120122842Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. Disclosed are compounds which inhibit the activity of ROCK, compositions containing the compounds and methods of treating diseases during which ROCK is expressed.Type: ApplicationFiled: November 11, 2011Publication date: May 17, 2012Applicant: Abbott LaboratoriesInventors: Michael L. Curtin, Bryan K. Sorensen, Howard R. Heyman, Richard F. Clark, Kevin R. Woller, Omar J. Shah, Michael Michaelides, Chris Tse, Anil Vasudevan, Helmut Mack, Todd M. Hansen, Ramzi Sweis, Marina A. Pliushchev
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Publication number: 20120122860Abstract: Solid forms of phenyl sulfonamide compounds of formula (I) active on protein kinases, including Raf protein kinases, are described, as well as methods of using such solid forms to treat diseases and conditions associated with activity of protein kinases, e.g. Raf protein kinases, including pain, polycystic kidney disease, melanoma and colorectal cancer.Type: ApplicationFiled: May 4, 2010Publication date: May 17, 2012Inventors: Gary Conard Visor, Prabha N. Ibrahim, Wayne Spevak, Hanna Cho, Songyuan Shi, Guoxian Wu
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Publication number: 20120122792Abstract: S-t-butyl protected cysteine di-peptide analogs and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).Type: ApplicationFiled: November 11, 2011Publication date: May 17, 2012Applicant: PROMENTIS PHARMACEUTICALS, INC.Inventors: Edward M. Johnson, II, Daniel G. Lawton
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Patent number: 8173659Abstract: Substituted pyrazolo[4,3-c]pyridine 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: GrantFiled: April 13, 2011Date of Patent: May 8, 2012Assignee: Nerviano Medical Sciences S.R.L.Inventors: Tiziano Bandiera, Andrea Lombardi Borgia, Paolo Polucci, Manuela Villa, Marcella Nesi, Mauro Angiolini, Mario Varasi
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Patent number: 8173635Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: October 31, 2008Date of Patent: May 8, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Michael Mortimore, Andrew Miller, Philip Collier, Stephen Young, Guy Brenchley, Chris Davis, Heather Twin, Chau Mak, Dean Boyall, Shazia Keily, Luca Settimo
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Publication number: 20120108590Abstract: A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises subjecting to elevated temperature the compound of Formula I, the water-soluble polymeric carrier and the surfactant, to provide an extrudable semi-solid mixture; extruding the semi-solid mixture; and cooling the resulting extrudate to to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer or an immune or autoimmune disease.Type: ApplicationFiled: October 5, 2011Publication date: May 3, 2012Applicant: ABBOTT LABORATORIESInventors: Esther Birtalan, Peter Hoelig, David J. Lindley, Yeshwant D. Sanzgiri, Ping Tong
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Publication number: 20120101093Abstract: The present invention is directed to substituted imidazo[1,2-a]pyridine derivatives, pharmaceutically acceptable salts thereof, and tautomers of such compounds or salts, that inhibit ?-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which BACE is involved.Type: ApplicationFiled: August 22, 2011Publication date: April 26, 2012Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Adnan M. M. Mjalli, Anitha Hari, Bapu Gaddam, Devi Reddy Gohimukkula, Dharma Rao Polisetti, Hassan El Abdellaoui, Mohan Rao, Robert Carl Andrews, Rongyuan Xie, Tan Ren
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Patent number: 8163756Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions, hyperproliferative diseases, cancer, and diseases characterized by hyper-vascularization are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein, abl kinase protein, ber-abl kinase protein, braf kinase protein, VEGFR kinase protein, or PDGFR kinase protein comprises the step of contacting said kinase protein with the novel compounds.Type: GrantFiled: December 21, 2007Date of Patent: April 24, 2012Assignee: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A. Petillo
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Patent number: 8163737Abstract: The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.Type: GrantFiled: December 13, 2007Date of Patent: April 24, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Corey Anderson, Andreas Termin, Sara Hadida-Ruah, Pramod Joshi, Sanghee Yoo, Daniele Bergeron, Hayley Binch, Jon Come, Jingrong Cao, Suganthi Nanthakumar, Elaine Krueger, John Maxwell, Arnaud Le Tiran, Yusheng Liao
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Publication number: 20120094944Abstract: For the prevention and/or treatment of chymase-mediated diseases such as skin diseases, circulatory diseases, digestive system diseases, respiratory diseases, liver diseases, ocular diseases or the like, a drug is provided having as an active ingredient a compound having extremely strong chymase inhibitory activity, high safety, and high metabolic stability. The compound represented by the formula (I): wherein all symbols have the same meanings as in the description, a salt thereof, an N-oxide thereof or a solvate thereof, or a prodrug thereof, is useful as a pharmaceutical ingredient having chymase inhibitory activity for preventing and/or treating of chymase-mediated disease, such as skin diseases, circulatory diseases, digestive system diseases, respiratory diseases, liver diseases, ocular diseases or the like.Type: ApplicationFiled: June 16, 2010Publication date: April 19, 2012Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Jun Takeuchi, Takayuki Inukai, Masaru Sakai
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Publication number: 20120095017Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.Type: ApplicationFiled: December 13, 2011Publication date: April 19, 2012Inventors: Tao Wang, Zhongxing Zhang, Nicholas A. Meanwell, John F. Kadow, Zhiwei Yin, Qiufen May Xue, Alicia Regueiro-Ren, John D. Matiskella, Yasutsugu Ueda
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Publication number: 20120094999Abstract: The present invention relates to novel pyrimidine, pyrrolo-pyrimidine, pyrrolo-pyridine, pyridine, purine and triazine compounds which are able to modulate epidermal growth factor receptor (EGFR), including Her-kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.Type: ApplicationFiled: May 5, 2010Publication date: April 19, 2012Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Pasi Janne, Michael J. Eck, Wenjun Zhou
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Publication number: 20120088766Abstract: The present application relates to therapeutic organic compounds, compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.Type: ApplicationFiled: June 14, 2010Publication date: April 12, 2012Applicant: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Hwan Geun Choi, Taebo Sim, Nathanael Gray, Wenjun Zhou, Jae Won Chang, Jianming Zhang, Ellen Weisberg
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Publication number: 20120088752Abstract: Heterocyclic compounds that modulate the hedgehog signaling pathway, pharmaceutical composition thereof and their therapeutic applications.Type: ApplicationFiled: June 9, 2010Publication date: April 12, 2012Applicant: SIENA BIOTECH S.p.A.Inventors: J. Russell Thomas, Gal.la Pericot Mohr, Chiara Caramelli, Giacomo Minetto, Marta Bellini
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Publication number: 20120083482Abstract: The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds of general formula (A) wherein A1 is sulfur, A3 is CH, A2 is CH, D is heterocycle, Z is oxygen, SO0-2 or NR, Ar is phenyl and G is not a ring, and methods for inhibiting VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: ApplicationFiled: December 8, 2011Publication date: April 5, 2012Inventors: Oscar Mario Saavedra, Stephen William Claridge, Lijie Zhan, Franck Raeppel, Arkadii Vaisburg, Stephane Raeppel, Michael Mannion, Frederic Gaudette, Ljubomir Isakovic, Marie-Claude Granger, Naomy Bernstein
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Publication number: 20120077787Abstract: New compounds of the Formula (I): for the treatment of non-insulin-dependent diabetes mellitus.Type: ApplicationFiled: December 6, 2011Publication date: March 29, 2012Applicant: NOVARTIS AGInventors: Daniel Kaspar Baeschlin, Nils OSTERMANN, Francois GESSIER, Finton SIROCKIN, Kenji NAMOTO
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Patent number: 8143257Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.Type: GrantFiled: November 23, 2005Date of Patent: March 27, 2012Assignee: PTC Therapeutics, Inc.Inventors: Soongyu Choi, Young-Choon Moon, Nadarajan Tamilarasu
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Publication number: 20120071494Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: January 26, 2011Publication date: March 22, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Dean Boyall, Guy Brenchley, Chris Davis, Damien Fraysse, Julian Golec, Juan-Miguel Jimenez, Andrew Miller, Luca Settimo, Heather Twin, Stephen Young
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Publication number: 20120071539Abstract: Methods and compositions comprising chemical compounds that modulate the silencing of a polynucleotide of interest in a cell are provided. Such chemical compounds when used in combination with an appropriate silencing element can be used to modulate (increase or decrease) the level of the polynucleotide targeted by the silencing element. Methods of using such compositions both in therapies involving RNAi-mediated suppression of gene expression, as well as, in vitro methods that allow for the targeted modulation of expression of a polynucleotide of interest are provided. Pharmaceutical or cosmetic compositions comprising such compounds and silencing elements also are disclosed. Methods for screening a compound of interest for the ability to modulate the activity of a heterologous silencing element also are provided.Type: ApplicationFiled: December 12, 2007Publication date: March 22, 2012Applicant: Emory UniversityInventor: Peng Jin
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Patent number: 8133893Abstract: A process of production of trazodone or trazodone hydrochloride that comprises the steps of: (a) preparing an organic phase comprising trazodone in at least one organic solvent; (b) preparing an aqueous phase comprising at least one basic compound; (c) mixing said aqueous phase with said organic phase; (d) heating at a temperature of at least 40° C. for at least 30 minutes; (e) recovering said trazodone; and, optionally, (f) treating said trazodone with hydrochloric acid to obtain trazodone hydrochloride. Trazodone or trazodone hydrochloride comprising less than 15 ppm of alkylating substances, and a pharmaceutical composition comprising said trazodone hydrochloride.Type: GrantFiled: July 23, 2008Date of Patent: March 13, 2012Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.Inventors: Marcello Marchetti, Tommaso Iacoangeli, Giovanni Battista Ciottoli, Giuseppe Biondi
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Nitrogen-Containing Fused Heterocyclic Compounds and Their use as Beta Amyloid Production Inhibitors
Publication number: 20120053171Abstract: A compound represented by the formula [I]: or a pharmacologically acceptable salt or ester thereof, wherein Ring A represents a five-membered aromatic heterocyclic group or the like fused with a non-aromatic ring group, which may be substituted, Ring B represents a phenyl group or the like which may be substituted, X1 represents a single bond or the like, R1 and R2 each represent a C1-6 alkyl group or the like, m represents an integer of 0 to 3, and n represents an integer of 0 to 2, is effective as a therapeutic agent for a disease caused by A?.Type: ApplicationFiled: February 24, 2010Publication date: March 1, 2012Inventors: Noritaka Kitazawa, Daisuke Shinmyo, Koichio Ito, Nobuaki Sato, Daiju Hasegawa, Toshiyuki Uemura, Toru Watanabe -
Publication number: 20120053175Abstract: Provided are compounds having an inhibitory effect on Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders which comprise the inhibition of Mixed Lineage Kinases.Type: ApplicationFiled: November 25, 2009Publication date: March 1, 2012Applicant: UNIVERSITY OF ROCHESTERInventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Colin J. Loweth, Torsten Wiemann
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Publication number: 20120053177Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.Type: ApplicationFiled: September 23, 2011Publication date: March 1, 2012Inventors: Prabha N. Ibrahim, Dean R. Artis, Ryan Bremer, Gaston Habets, Shumeye Mamo, Marika Nespi, Chao Zhang, Jiazhong Zhang, Yong-Liang Zhu, Rebecca Zuckerman, Brian West, Yoshisa Suzuki, James Tsai, Klaus-Peter Hirth, Gideon Bollag, Wayne Spevak, Hanna Cho, Samuel J. Gillette, Guoxian Wu, Hongyao Zhu, Shenghua Shi
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Publication number: 20120046246Abstract: This invention relates to therapeutic methods for treating or preventing an osteoclast-related disease or disorder in a subject identified as in need of a treatment of bone diseases, compounds for such uses, and compositions thereof.Type: ApplicationFiled: December 18, 2009Publication date: February 23, 2012Applicant: University of Florida Research FoundationInventors: Lexie Shannon Holliday, David A. Ostrov
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Publication number: 20120040942Abstract: The invention relates to novel compounds having the general formula (I), and which compounds are useful to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma.Type: ApplicationFiled: February 24, 2010Publication date: February 16, 2012Applicant: RESPIRATORIUS ABInventors: Martin Johansson, Viveca Thornqvist Otlner, Jorgen Toftered, David Wensbo, Maria Dalence
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Publication number: 20120040936Abstract: Low molecular weight compound exhibiting an osteogenesis-promoting action having the general formula (I) or a pharmacologically acceptable salt thereof:Type: ApplicationFiled: October 5, 2011Publication date: February 16, 2012Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Osamu Kanno, Katsuyoshi Nakajima, Kazumasa Aoki, Ryoichi Tanaka, Shimpei Hirano, Kiyoshi Oizumi, Satoru Naito
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Publication number: 20120035171Abstract: The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: ApplicationFiled: April 15, 2010Publication date: February 9, 2012Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Gordon Saxty, Valerio Berdini, Eddy Jean Edgard Freyne, Alexandra Papanikos, Pascal Benderitter, Werner Constant Johan Embrechts, Berthold Wroblowski, Rhalid Akkari
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Publication number: 20120028939Abstract: The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 is selected from among —O—R3 or —NR3R4, R3 is C1-6-alkyl which is substituted by R5 and R6, R5 is selected from hydrogen, branched or linear C1-6-alkyl, C2-6-alkenyl, —C1-6-alkylen-O—C1-3-alkyl, C1-3-haloalkyl, R6 is ring X wherein n is either 0 or 1, and is a either a single or a double bond and wherein A, B, D and E are each independently from one another selected from CH2, CH, C, N, NH, O or S and wherein ring X is attached to the molecule either via position A, B, D or E, wherein said ring X may optionally be further substituted by one, two or three residues each selected individually from the group consisting of -oxo, hydroxy, —C1-3-alkyl, —C1-3-haloalkyl, —O—C1-3-alkyl, —C1-3-alkanol and halogen, and wherein R4, R2, R7, R8, R9, R10, R11 and Q may have the meanings as given in claim 1, as welType: ApplicationFiled: January 26, 2011Publication date: February 2, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Hoffmann, Georg Hoffmann, Dennis Fiegen, Sandra Handschuh, Jasna Klicic, Guenter Linz, Gerhard Schaenzle, Andreas Schnapp, Stephen Peter East, Michael Philip Mazanetz, Robert John Scott, Edward Walker
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Publication number: 20120028974Abstract: The present invention relates to a compound according to formula I, wherein R1, R2 and A are as defined herein, which exhibit PDE4 inhibitory activity and may be used in the treatment of inflammatory diseases or autoimmune diseases, in particular inflammatory or proliferative dermal diseases.Type: ApplicationFiled: December 18, 2009Publication date: February 2, 2012Applicant: LEO PHARMA A/SInventors: Simon Feldbaek Nielsen, Thomas Vifian, Anne Marie Horneman, Jesper Faergemann Lau
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Patent number: 8106069Abstract: Compounds which are pyrrolo[2,3-b]pyridine derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders; also disclosed is a process under SPS conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.Type: GrantFiled: April 23, 2010Date of Patent: January 31, 2012Assignee: Pfizer Italia S.r.l.Inventors: Barbara Salom, Matteo D'Anello, Maria Gabriella Brasca, Patrizia Giordano, Katia Martina, Francesco Angelucci, Frederick Arthur Brookfield, William John Trigg, Edward Andrew Boyd, Jonathan Anthony Larard
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Publication number: 20120014917Abstract: The invention relates to methods of treating patients infected with human immunodeficiency virus (HIV) with a therapeutic that has anti-fibrotic effects, for example, pirfenidone and analogs thereof.Type: ApplicationFiled: September 26, 2011Publication date: January 19, 2012Applicants: University of Minnesota, INTERMUNE, INC.Inventors: Karl Kossen, Timothy Schacker, Ashley T. Haase
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Publication number: 20120015907Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: April 19, 2011Publication date: January 19, 2012Applicant: NOVARTIS AGInventors: David BARNES, Rajiv CHOPRA, Scott Louis COHEN, Jiping FU, Mitsunori Kato, Peichao LU, Mohindra SEEPERSAUD, Wei ZHANG
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Publication number: 20120015926Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: ApplicationFiled: November 9, 2009Publication date: January 19, 2012Inventors: Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Joseph A. Kozlowski, Michael K.C. Wong, Lei Chen, Guowei Zhou, Razia K. Rizvi, Robert Feltz, Aneta Maria Kosinski, De-Yi Yang, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristen E. Rosner, M. Arshad Siddiqui, Liping Yang
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Publication number: 20120010206Abstract: Novel imidazolopyridine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, ECM degradation, joint degradation and/or inflammation, and others.Type: ApplicationFiled: May 25, 2011Publication date: January 12, 2012Inventors: Paul John EDWARDS, Sébastien Laurent Xavier MARTINA, Martin James Inglis ANDREWS, Grégory Louis Joseph BAR, Brigitte ALLART, Andrew BURRITT, Xueliang TAO, Friedrich Erich Karl KROLL
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Publication number: 20120010214Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are 3-imidazoyl-pyrazolo[3,4-b]pyridine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.Type: ApplicationFiled: May 9, 2011Publication date: January 12, 2012Applicant: ChemoCentryx, Inc.Inventors: Lianfa Li, Andrew M.K. Pennell, Penglie Zhang
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Publication number: 20120010201Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein X, Y, A, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as therapeutics.Type: ApplicationFiled: June 29, 2011Publication date: January 12, 2012Inventors: Luca Gobbi, Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Publication number: 20120004221Abstract: Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(?O)NR6—, —S(O)NR6—, —C(?O)O— or —S(?O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N; R2 and R3 are as defined in the description.Type: ApplicationFiled: June 7, 2011Publication date: January 5, 2012Applicant: Biota Europe LimitedInventors: David John Haydon, Lloyd George Czaplewski, Nicholas John Palmer, Dale Robert Mitchell, John Frederick Atherall, Christopher Richard Steele, Tamara Ladduwahetty
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Patent number: 8088761Abstract: Compounds of formula (I), are aurora kinase inhibitors: wherein X is —N—, —CH2-N—, —CH2-CH—, or —CH—; R1 is a radical of formula (IA) wherein Z is —CH2-, —NH—, -0-, —S(O)— —S—, —S(O)2 or a divalent monocyclic carbocyclic or heterocyclic radical having 3-7 ring atoms; Alk is an optionally substituted divalent C1-C6 alkylene radical; A is hydrogen or an optionally substituted monocyclic carbocyclic or heterocyclic ring having 5-7 ring atoms; r, s and t are independently 0 or 1, provided that when A is hydrogen then at least one of r and s is 1; R2 is halogen, —CN, —CF3, —OCH3, or cyclopropyl; and R3 is a radical of formula (IB) wherein Q is hydrogen or an optionally substituted phenyl or monocyclic heterocyclic ring with 5 or 6 ring atoms; Z&It;1> is —S—, —S(O)—, —S(O)2-, —O—, —SO2NH—, —NHSO2-, NHC(?O)NH, —NH(C?S)NH—, Or —N(R4)— wherein R4 is hydrogen, C1-C3 alkyl, cycloalkyl, or benzyl; and Alk&It;1> and Alk&It;2> are, independently, optionally substituted divalent C1-C3 alkyleType: GrantFiled: December 21, 2006Date of Patent: January 3, 2012Assignee: Cancer Research Technology LimitedInventors: Vassilios Bavetsias, Edward McDonald, Spyridon Linardopoulos
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Patent number: 8084449Abstract: The present invention is directed to novel compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions and their use as dual chromaphores having inhibitory activity against PDE4 and muscarinic acetylcholine receptors (mAChRs), and thus being useful for treating respiratory diseases.Type: GrantFiled: February 5, 2009Date of Patent: December 27, 2011Assignee: Glaxo Group LimitedInventors: James Francis Callahan, Guoliang Lin, Zehong Wan, Hongxing Yan
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Publication number: 20110311516Abstract: Provided herein is a method for chemically programmed vaccination. Methods include inducing a covalent-binding polyclonal antibody response in a subject and programming the polyclonal response with a targeting compound.Type: ApplicationFiled: February 10, 2010Publication date: December 22, 2011Applicant: THE SCRIPPS RESEARCH INSTITUTEInventor: Carlos F. Barbas, III
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Publication number: 20110312959Abstract: The present invention relates to compounds of general formula I and use thereof as inhibitors of protein kinases AbI and Src and the method of production thereof. The present invention also relates to pharmaceutical compositions and medici-nal products comprising these compounds.Type: ApplicationFiled: February 12, 2010Publication date: December 22, 2011Inventors: Abdelaziz Yasri, Gwénaël Cheve, Cédric Bories, Louis Delon
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Patent number: 8080546Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of pro-inflammatory cytokine mediated diseases, and in particular, p38 activity mediated inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, A3, A4, A5, R1, R2 and R3 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of inflammatory diseases including rheumatoid arthritis, psoriasis and other disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.Type: GrantFiled: October 24, 2008Date of Patent: December 20, 2011Assignee: Amgen Inc.Inventors: Liping H. Pettus, Andrew Tasker, Shimin Xu, Ryan Wurz
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Patent number: 8080547Abstract: The invention relates to the triazolopyridine carboxamide derivative and trizolopyrimidine carboxamide derivative of general Formula (I): Wherein X, R1 and R2 are as defined herein. The invention further relates to preparation methods and therapeutic use thereof.Type: GrantFiled: October 6, 2009Date of Patent: December 20, 2011Assignee: Sanofi-AventisInventors: Luc Even, Christian Hoornaert
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Publication number: 20110306609Abstract: Provided herein are novel sirtuin-modulating compounds of Structural Formula (Ia) and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: December 18, 2009Publication date: December 15, 2011Inventors: Christopher Oalmann, Jeremy S. Disch, Pui Yee Ng, Robert Perni