Three Or More Ring Hetero Atoms In The Tricyclo Ring System Patents (Class 546/82)
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Patent number: 8772312Abstract: This application relates to a compound of Formula ! (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an antagonist of receptor CRTH2, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: October 9, 2008Date of Patent: July 8, 2014Assignees: CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd., Centaurus Biopharma Co., Ltd.Inventor: Wei W. Yuan
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Patent number: 8771682Abstract: The present invention relates generally to methods and compositions for reducing Interleukin-4 or Interleukin-13 signaling, in particular to treat asthma and atopic dermatitis. The inventors have found that Rac/PAK mediated endocytosis of the ligand bound type I (IL-4R with the chains IL-4Ra and IL-2-Rg) and/or type II receptor (IL-13R with the chains IL-4Ra and IL-13Ra1) is needed for the IL-4 and/or IL-13 mediated activation of downstream signalling events including phosphorylation of Stat family transcrition factors. These discoveries enable new methods of screening compounds that modulate Interleukin-4 and Interleukin-13 signalling, as well as new methods for treating conditions characterized by increased Interleukin-4 and Interleukin-13 levels. These conditions include inflammatory conditions, asthma bronchiale, atopic dermatitis, allergies, atopic syndromes, allergic rhinitis, and th2-induced conditions.Type: GrantFiled: April 26, 2012Date of Patent: July 8, 2014Assignee: Technische Universtität DresdenInventors: Christian Bökel, Thomas Weidemann
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Publication number: 20140179671Abstract: The present invention provides a novel class of fused ring azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.Type: ApplicationFiled: September 12, 2013Publication date: June 26, 2014Applicant: Corcept Therapeutics, Inc.Inventors: Robin D. Clark, Nicholas C. Ray, Paul M. Blaney, Christopher A. Hurley, Karen Williams
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Patent number: 8759345Abstract: The present invention is directed to benzoimidazole compounds of the formula (1) and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.Type: GrantFiled: April 28, 2009Date of Patent: June 24, 2014Assignee: Janssen Pharmaceutica NVInventors: Frances Meredith Hocutt, Barry Eastman Leonard, Jr., Hillary M Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
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Publication number: 20140171407Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: ApplicationFiled: February 17, 2014Publication date: June 19, 2014Applicant: Genentech, Inc.Inventors: Hazel Joan Dyke, Lewis Gazzard, Karen Williams, Huifen Chen, Samuel Kintz, Joy Drobnick, Joseph P. Lyssikatos, Simon Goodacre, Calum Macleod, Charles Ellwood
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Publication number: 20140171462Abstract: Novel quinoline compounds pharmaceutical compositions containing such compounds and their use in therapy.Type: ApplicationFiled: August 15, 2012Publication date: June 19, 2014Applicant: GlaxcoSmithKline LLCInventors: Emmanuel Hubert Demont, Katherine Louise Jones, Robert J. Watson
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Publication number: 20140141033Abstract: A conjugated compound of formula Q-Z—R4 wherein Q is a TLR7 and/or TLR8 agonist and Z—R4 is a TLR2 agonist, and the uses thereof in the treatment of infection, cancer or immune disorders or for use in vaccines.Type: ApplicationFiled: March 15, 2013Publication date: May 22, 2014Applicant: CAYLAInventors: Fabienne VERNEJOUL, Arnaud DEBIN, Daniel DROCOURT, Eric PEROUZEL, Gerard TIRABY, Thierry LIOUX
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Patent number: 8728486Abstract: The present disclosure provides novel imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof, and methods of making and using such compounds. The present disclosure also provides TLR7 agonists and TLR7/TLR8 dual agonists, probes, tissue-specific molecules, adjuvants, immunogenic compositions, therapeutic compositions, and self-adjuvanting vaccines including the imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof. Derivatives of the imidazoquinoline derived compounds also include dendrimers and dimers of the imidazoquinoline derived compounds, and methods of making and using the dendrimeic and dimeric imidazoquinoline derived compounds. The present disclosure also provides dual TLR2/TLR7 hybrid agonists that include imidazoquinoline derived compounds of the present disclosure.Type: GrantFiled: May 18, 2012Date of Patent: May 20, 2014Assignee: University of KansasInventors: Sunil A. David, Nikunj M. Shukla
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Patent number: 8710047Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.Type: GrantFiled: July 12, 2013Date of Patent: April 29, 2014Assignee: Albany Molecular Research, Inc.Inventors: David D. Manning, Christopher L. Cioffi
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Patent number: 8710046Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.Type: GrantFiled: June 30, 2010Date of Patent: April 29, 2014Assignee: Albany Molecular Research, Inc.Inventors: Peter R. Guzzo, David D. Manning, William Earley
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Publication number: 20140107141Abstract: The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3? or GSK3?) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychriatic disorders, metabolic disorders, and cancer.Type: ApplicationFiled: October 11, 2013Publication date: April 17, 2014Applicants: The General Hospital Corporation d/b/a Massachusetts General Hospital, The Broad Institute, Inc.Inventors: Florence Fevrier Wagner, Jennifer Q. Pan, Sivaraman Dandapani, Andrew Germain, Edward Holson, Benito Munoz, Partha P. Nag, Michel Weiwer, Michael C. Lewis, Stephen J. Haggarty, Joshua A. Bishop
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Publication number: 20140093505Abstract: The present invention relates to a pyridonaphthyridine compound as represented by general formula (I), which has a dual PI3K and mTOR inhibition effect, and its pharmaceutically acceptable salt, stereoisomer and deuteride thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the specification; the present invention also relates to a method for preparing said compound, a pharmaceutical composition and a pharmaceutical formulation containing said compound, and uses of said compound in treating and/or preventing a proliferative disease and in the manufacture of a medicament for treating and/or preventing a proliferative disease.Type: ApplicationFiled: June 4, 2012Publication date: April 3, 2014Applicant: Xuanzhu Pharma Co., Ltd.Inventors: Frank Wu, Yan Zhang
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Patent number: 8680089Abstract: Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.Type: GrantFiled: January 17, 2011Date of Patent: March 25, 2014Assignee: Xuanzhu Pharma Co., Ltd.Inventors: Zhenhua Huang, Yan Zhang, Yuntao Song
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Patent number: 8673933Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of JAK2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.Type: GrantFiled: April 30, 2012Date of Patent: March 18, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Ashok V. Purandare, James W. Grebinski, Amy C. Hart, Jennifer Inghrim, Gretchen M. Schroeder, Honghe Wan
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Publication number: 20140051689Abstract: Compounds of formula (I), and their use as in the treatment of infections involving viruses of the Pneumovirinae sub-family (RSV) are disclosed. In the formula ring (A) may be phenyl, pyridyl etc., (B-C) may be CH2—CH2 etc., (R1) may be phenyl and substituted forms thereof, (R2) may be assorted substituents.Type: ApplicationFiled: October 24, 2013Publication date: February 20, 2014Applicant: Biota Scientific Management Pty Ltd.Inventors: Silas Bond, Vanessa Anne Sanford, John Nicholas Lambert, Chin Yu Lim, Alistair George Draffan, Roland Henry Nearn, Jeffrey Peter Mitchell
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Publication number: 20140051695Abstract: The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof where in formula I the variables R1, R2, R3, R4 and R5 are as defined in the claims and where X is C—R6 or N, Y is C—R7 or N, where R6 and R7 are, inter alia, hydrogen, halogen, alkoxy, haloalkoxy and the like. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.Type: ApplicationFiled: August 15, 2013Publication date: February 20, 2014Inventors: Hervé GENESTE, Michael OCHSE, Karla DRESCHER, Clarissa JAKOB
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Patent number: 8653097Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4, A, X, m and k are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: GrantFiled: October 15, 2009Date of Patent: February 18, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Lars Van Der Veen, Darryl McConnell, Tobias Wunberg
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Publication number: 20140045834Abstract: Novel quinoline compounds pharmaceutical compositions containing such compounds and their use in therapy.Type: ApplicationFiled: April 19, 2012Publication date: February 13, 2014Applicant: GlaxoSmithKline LLCInventors: Emmanuel Hubert Demont, Katherine Louise Jones, Robert J. Watson
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Publication number: 20140045819Abstract: This invention relates to tricyclic triazole analogues of the formula I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthetase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthetase.Type: ApplicationFiled: April 20, 2012Publication date: February 13, 2014Applicants: ElexoPharm GmbH, SCHERING CORPORATIONInventors: Scott B. Hoyt, Whitney Lane Petrilli, Clare London, Yusheng Xiong, Jerry Andrew Taylor, Amjad Ali, Michael Man-Chu Lo, Timothy J. Henderson, Qingzhong Hu, Rolf Hartmann, Lina Yin, Ralf Heim, Emmanuel Bey, Rohit Saxena, Swapan Kumar Samanta, Bheemashankar A. Kulkarni
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Publication number: 20140038926Abstract: The present invention provides heteroaryl ketone fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.Type: ApplicationFiled: May 24, 2013Publication date: February 6, 2014Applicant: Corcept Therapeutics, Inc.Inventors: Hazel Hunt, Tony Johnson, Nicholas Ray, Iain Walters
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Publication number: 20140031362Abstract: The present invention relates to compounds of following general formula (I): and to the pharmaceutically acceptable salts of same, the tautomers of same, the stereoisomers or mixture of stereoisomers in any proportions of same, such as a mixture of enantiomers, notably a racemic mixture, as well as to methods for preparing same and uses of same, notably as an antineoplastic agent.Type: ApplicationFiled: April 12, 2012Publication date: January 30, 2014Applicant: PIERRE FABRE MEDICAMENTInventors: Rémi Rabot, Karim Bedjeguelal, El Bachir Kaloun, Philippe Schmitt, Nicolas Rahier, Patrice Mayer, Emmanuel Fournier
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Patent number: 8637670Abstract: The present invention provides the compounds of formula (I): The present invention relates to imidazo[4,5-c]quinoline derivatives of formula (I), process for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases mediated by phosphatidylinositol-3-kinase (PBK) and/or mammalian target of rapamycin (mTOR) and/or tumor necrosis factor-? (TNF-oc) and/or interleukin-6 (IL-6), particularly in the treatment of cancer and inflammation.Type: GrantFiled: June 30, 2009Date of Patent: January 28, 2014Assignee: Piramal Enterprises LimitedInventors: Sanjay Kumar, Ram Vishwakarma, Ramswaroop Mundada, Vijaykumar Deore, Pramod Kumar, Somesh Sharma
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Publication number: 20140023614Abstract: The present invention relates to substituted fused tricyclic compounds of formula (I) or (Ia), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by JAK activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders mediated by JAK activity.Type: ApplicationFiled: March 21, 2012Publication date: January 23, 2014Inventors: Dinesh Barawkar, Tanushree Bende, Robert Zahler, Anish Bandyopadhyay, Robindro Singh Sarangthem, Jignesh Doshi, Yogesh Waman, Rushikesh Jadhav, Umesh Prasad Singh
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Publication number: 20140011777Abstract: Imidazo-quinoline, -pyridine, and -naphthyridine ring systems (particularly quinolines, tetrahydroquinolines, pyridines, [1,5]naphthyridines, [1,5]tetrahydronaphthyridines) substituted at the 1-position with a cyclic substituent, pharmaceutical compositions containing the compounds, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: ApplicationFiled: September 9, 2013Publication date: January 9, 2014Applicant: 3M INNOVATIVE PROPERTIES COMPANYInventors: Doris Stoermer, Joseph F. Dellaria, Jr., David T. Amos, Bernhard M. Zimmermann, Luke T. Dressel, Jason D. Bonk
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Publication number: 20140004111Abstract: The present invention relates to polycyclic antiviral compounds, and salts thereof, methods for their preparation and compositions containing them, and the use of the compounds and composition in the treatment of viral infections.Type: ApplicationFiled: August 30, 2013Publication date: January 2, 2014Applicant: Biota Scientific Management Pty Ltd.Inventors: Jeffrey Peter Mitchell, Alistair George Draffan, Vanessa Anne Sanford, Silas Bond, Chin Yu Lim, Anne Mayes
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Publication number: 20140005193Abstract: The present invention is directed to benzoimidazole compounds of the formula: and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.Type: ApplicationFiled: September 3, 2013Publication date: January 2, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Frances Meredith Hocutt, BARRY EASTMAN LEONARD, JR., HILLARY M. PELTIER, VICTOR K. PHUONG, MICHAEL H. RABINOWITZ, MARK D. ROSEN, KYLE T. TARANTINO, HARIHARAN VENKATESAN, LUCY XIUMIN ZHAO
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Publication number: 20140005163Abstract: The invention relates to the use of 1H-imidazo[4,5-c]quinolinone derivatives and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1H-imidazo[4,5-c]quinolinone derivatives for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1H-imidazo[4,5-c]quinolinone derivatives to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1H-imidazo[4,5-c]quinolinone derivative, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1H-imidazo[4,5-c]quinolinone derivatives; and a process for the preparation of the novel 1H-imidazo[4,5-c]quinolinone derivatives.Type: ApplicationFiled: May 24, 2013Publication date: January 2, 2014Applicant: NOVARTIS AGInventors: Pascal Furet, Frank Stephan Kalthoff, Robert Mah, Christian Ragot, Frederic Stauffer
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Publication number: 20130345426Abstract: An object of the present invention is to provide a drug having the inhibitory activity on ENPP2 which is a different target from that of the existing drug, as a medicament useful in a urinary excretion disorder patient for whom the existing drug has the insufficient effect. The present invention provides a compound represented by the general formula (I): (wherein definition of each group is as defined in the description) having the ENPP2 inhibitory activity, a salt thereof or a solvate thereof or a prodrug thereof, and an agent for preventing or treating urinary excretion disorder and/or improving symptoms thereof, containing them as an active ingredient.Type: ApplicationFiled: January 5, 2012Publication date: December 26, 2013Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Akira Ohata, Shingo Nakatani, Tetsuya Sugiyama, Takashi Morimoto
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Publication number: 20130338134Abstract: The present invention relates to tricyclic compounds, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.Type: ApplicationFiled: June 12, 2013Publication date: December 19, 2013Inventors: Liangxing Wu, Colin Zhang, Chunhong He, Yaping Sun, Liang Lu, Ding-Quan Qian, Meizhong Xu, Jincong Zhuo, Wenqing Yao
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Patent number: 8609845Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, Q, X1, X2, Y, R1, R2, R3, R4, R4?, R5, R6 and R6? are as described herein.Type: GrantFiled: August 10, 2009Date of Patent: December 17, 2013Assignee: Genentech, Inc.Inventors: Frederick Cohen, Vickie Hsiao-Wei Tsui, Cuong Ly, John A. Flygare
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Publication number: 20130331409Abstract: The present invention provides a compound having a superior PDE10A inhibitory action and use thereof. The compound is a compound represented by the following formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.Type: ApplicationFiled: March 15, 2012Publication date: December 12, 2013Inventors: Takahiko Taniguchi, Jun Kunitomo, Masato Yoshikawa, Tomoaki Hasui, Eiji Honda, Keisuke Imamura, Haruhi Kamisaki, Shinkichi Suzuki, Kasei Miura
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Patent number: 8598193Abstract: Compounds of formula (I), and their use as in the treatment of infections involving viruses of the Pneumovirinae sub-family (RSV) are disclosed. In the formula ring (A) may be phenyl, pyridyl etc., (B—C) may be CH2—CH2 etc., (R1) may be phenyl and substituted forms thereof, (R2) may be assorted substituents.Type: GrantFiled: December 24, 2004Date of Patent: December 3, 2013Assignee: Biota Scientific Management Pty Ltd.Inventors: Silas Bond, Vanessa Anne Sanford, John Nicholas Lambert, Chin Yu Lim, Jeffrey Peter Mitchell, Alistair George Draffan, Roland Henry Nearn
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Patent number: 8598154Abstract: The present invention provides a novel class of pyridyl-amine fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.Type: GrantFiled: August 26, 2011Date of Patent: December 3, 2013Assignee: Corcept Therapeutics, Inc.Inventors: Robin Clark, Tony Johnson, Hazel Hunt, Ian McDonald
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Patent number: 8598192Abstract: Imidazo ring compounds (e.g., imidazoquinolines, 6,7,8,9-tetrahydroimidazoquinolines, imidazonaphthyridines, and imidazopyridines) with a hydroxylamine substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: GrantFiled: November 12, 2004Date of Patent: December 3, 2013Assignee: 3M Innovative Properties CompanyInventors: Tushar A. Kshirsagar, Gregory D. Lundquist, Jr., David T. Amos, Joseph F. Dellaria, Jr., Bernhard M. Zimmermann, Philip D. Heppner
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Patent number: 8598167Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: July 9, 2013Date of Patent: December 3, 2013Assignee: Epizyme, Inc.Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
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Publication number: 20130310374Abstract: The present invention relates to substituted imidazo[4,5-c]quinoline derivatives of formula (I), wherein R1, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions comprising compounds of the present invention and their use in the treatment of diseases or disorders mediated by one or more kinases, particularly proliferative diseases or disorders such as cancer. These compounds can also be used in the treatment of inflammation and angiogenesis related disorders.Type: ApplicationFiled: December 5, 2011Publication date: November 21, 2013Applicant: PIRAMAL ENTERPRISES LIMITED`Inventors: Sanjay Kumar, Rajiv Sharma, Vijaykumar Bhagwan Deore, Nilambari Nilkanth Yewalkar, Veena R. Agarwal, Nilesh Dagia, Nishigandha Naik
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Publication number: 20130310366Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: July 12, 2013Publication date: November 21, 2013Applicant: Albany Molecular Research, Inc.Inventors: David D. MANNING, Christopher L. CIOFFI
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Patent number: 8580405Abstract: The present invention provides a novel naphthothiophene compound having a high lowest excited triplet level (T1).Type: GrantFiled: April 11, 2011Date of Patent: November 12, 2013Assignee: Canon Kabushiki KaishaInventors: Naoki Yamada, Jun Kamatani, Akihito Saitoh
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Publication number: 20130296307Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:Type: ApplicationFiled: July 10, 2013Publication date: November 7, 2013Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
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Publication number: 20130289029Abstract: The present invention belongs to the technical field of medicine, relating in particular to: a fused ring compound as represented by Formula (I) for use as a mineralocorticoid receptor antagonist, a pharmaceutically acceptable salt thereof, and an isomer thereof; a preparation method for these compounds; a pharmaceutical preparation containing these compounds; and an application of these compounds, the pharmaceutically acceptable salt thereof, or the isomers thereof in the preparation of medicants for the treatment and/or prevention of kidney injury, cardiovascular diseases such as hypertension, and/or endocrine disease. The definitions of X, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4, Cy and n are as presented in the description.Type: ApplicationFiled: August 18, 2011Publication date: October 31, 2013Inventors: Zhenhua Huang, Jinyuan Wang, Dedong Zhang
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Publication number: 20130289064Abstract: The invention relates to particular crystalline forms of 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile, its hydrates and solvates, its salts and hydrates and solvates of its salts, certain processes for their preparation, pharmaceutical compositions containing these crystalline forms, and their use in diagnostic methods or, preferably, for the therapeutic treatment of warm-blooded animals, especially humans, and their use as an intermediate or for the preparation of pharmaceutical preparations for use in diagnostic methods or, preferably, for the therapeutic treatment of warm-blooded animals, especially humans.Type: ApplicationFiled: April 4, 2013Publication date: October 31, 2013Applicant: NOVARTIS AGInventors: Frank Stowasser, Markus Banziger, Sudhakar Devidasrao Garad
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Patent number: 8557984Abstract: Novel compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.Type: GrantFiled: November 3, 2010Date of Patent: October 15, 2013Assignee: GlaxoSmithKline LLCInventors: Anne Marie Jeanne Bouillot, Frederic Donche, Francoise Jeanne Gellibert, Yann Lamotte, Olivier Mirguet
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Publication number: 20130261148Abstract: Provided are protected antimicrobial compounds which are useful for controlling microorganisms in aqueous or water-containing systems, such as oil or gas field fluids, at elevated temperature. The antimicrobial compounds are of the formula I: wherein R, R1, R2, X and Y are as defined herein.Type: ApplicationFiled: December 2, 2011Publication date: October 3, 2013Applicants: DOW GLOBAL TECHNOLOGIES LLC, ANGUS CHEMICAL COMPANYInventors: Charles E. Coburn, Michael V. Enzien, Heather R. McGinley, David W. Moore
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Publication number: 20130252993Abstract: The present invention relates to the compound represented by formula (I): (wherein, all the symbols have the same meaning as that of the specification), a salt thereof, a solvate thereof or a prodrug thereof. Since the compound of the present invention has an anti stress action, it is useful for preventive and/or therapeutic agent for a disease caused by stress, especially a digestive system disease caused by stress and is superior to oral absorption.Type: ApplicationFiled: May 17, 2013Publication date: September 26, 2013Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Kazuyuki OHMOTO, Masashi KATO, Yoshifumi KAGAMIISHI, Junichiro MANAKO
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Publication number: 20130245266Abstract: The present invention provides amorphous solid forms of the compound of Formula I, as well as methods for preparing the compound of Formula I by precipitation.Type: ApplicationFiled: May 7, 2013Publication date: September 19, 2013Applicant: Corcept Therapeutics, Inc.Inventors: Robin Clark, Doug Fry
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Publication number: 20130245049Abstract: The present invention relates to compounds of formula (A), as further defined herein, having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. The invention further relates to the use of such compounds, optionally combined with one or more other drugs having antiviral activity, for the treatment of animals suffering from viral infections, in particular HIV infection.Type: ApplicationFiled: November 15, 2011Publication date: September 19, 2013Applicant: Katholieke Universiteit LeuvenInventors: Patrick Chaltin, Frauke Christ, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Arnout Voet
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Patent number: 8536193Abstract: The instant invention provides for substituted [1,2,4]triazolo[4,3-a]-1,5-naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity, especially Akt1 by administering the compound to a patient in need of treatment of cancer.Type: GrantFiled: May 27, 2009Date of Patent: September 17, 2013Assignees: Merck Sharp & Dohme Corp., MSD K.K.Inventors: Hidetomo Furuyama, Yasuhiro Goto, Nobuhiko Kawanishi, Mark E. Layton, Takashi Mita, Yoshio Ogino, Yu Onozaki, Michael A. Rossi, Toshihiro Sakamoto, Philip E. Sanderson, Jiabing Wang
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Publication number: 20130230578Abstract: The compound N-(4-{[4-amino-2-butyl-1H-imidazo[4,5-c]quinolin-1-yl]oxy}butyl)octadecanamide is a useful drug compound for enhancing immune response and can be used, for example, as a vaccine adjuvant and a cancer treatment.Type: ApplicationFiled: August 16, 2011Publication date: September 5, 2013Applicant: 3M INNOVATIVE PROPERTIES COMPANYInventor: Paul D. Wightman
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Publication number: 20130225553Abstract: The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.Type: ApplicationFiled: March 7, 2013Publication date: August 29, 2013Applicant: ASTELLAS PHARMA INC.Inventor: ASTELLAS PHARMA INC.
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Publication number: 20130225633Abstract: The present invention provides phenyl-heterocycloalkyl fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.Type: ApplicationFiled: February 26, 2013Publication date: August 29, 2013Applicant: Corcept Therapeutics, Inc.Inventor: Corcept Therapeutics, Inc.