Additional Polycyclo Heterocyclic Ring System Containing Patents (Class 548/159)
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Publication number: 20130040999Abstract: The present invention provides novel compounds of Chemical Formula I, a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, a preparation thereof and a composition for the alleviation, prevention or treatment of osteoporosis, comprising thereof in an effective amount, and a method for alleviating, preventing or treating osteoporosis.Type: ApplicationFiled: June 14, 2012Publication date: February 14, 2013Applicant: Ewha University-Industry Collaboration FoundationInventors: Hea-Young PARKCHOO, Kyung-Eun Doh, Mijung Yim, Jung-Min Lee
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Publication number: 20130035324Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the heterocyclic entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.Type: ApplicationFiled: August 17, 2010Publication date: February 7, 2013Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Simon Fraser Campbell
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Publication number: 20130035332Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: April 25, 2011Publication date: February 7, 2013Inventors: Mark E. Layton, Michael J. Kelly
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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
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Patent number: 8344010Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.Type: GrantFiled: December 23, 2009Date of Patent: January 1, 2013Assignee: Glenmark Pharmaceuticals S.A.Inventors: V. S. Prasadarao Lingam, Abraham Thomas, Shantaram Kashinath Phatangare, Ajit Shankar Mindhe, Javed Yusuf Khatik, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
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Patent number: 8344007Abstract: A cantharimide compound may include the backbone of formula (1). R1, R2, R3, and R4 may be independently selected from the group consisting of H, C(O)OR5, C(O)R6, C(O)NR7R8, NR9C(O)R10, N—R11R12, O—R13, S—R14, P(O)(OR15)(OR16), As(O)(OR17)(OR18), SO2R19, SO3R20, and B(OR21). X1 to X4 may be independently selected from the group consisting of nitrogen and carbon, such that X1 to X4 are not all hydrogen. Y1, Y2 and R5 to R21 may be independently selected from the group consisting of hydrogen, C1-12-alkyl, -aryl, heteroaryl, and a bioactive polymer.Type: GrantFiled: April 23, 2009Date of Patent: January 1, 2013Assignee: The Hong Kong Polytechnic UniversityInventors: Johnny Cheuk-on Tang, Albert Sun-chi Chan, Kim-hung Lam, Chung-hin Chui, Stanton Hon Lung Kok, Marcus Chun Wah Yuen, Sau Hing Chan, Chor Hing Cheng, Filly Cheung
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Patent number: 8344008Abstract: Aryl-substituted bridged or fused diamine compounds, pharmaceutical compositions containing them, and methods of using the compounds and the pharmaceutical compositions for leukotriene A4 hydrolase (LTA4H or LTA4H) modulation and for the treatment of disease states, disorders, and conditions mediated by LTA4H activity, such as allergy, asthma, autoimmune diseases, pruritis, inflammatory bowel disease, ulcerative colitis, and cardiovascular disease, including atherosclerosis and prevention of myocardial infarction.Type: GrantFiled: April 21, 2011Date of Patent: January 1, 2013Assignee: Janssen Pharmaceutica NVInventors: Genesis M. Bacani, Scott D. Bembenek, Wendy Eccles, James P. Edwards, Matthew T. Epperson, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Kelly J. McClure, Taraneh Mirzadegan, Alexandro Santillán, Jr.
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Publication number: 20120330020Abstract: According to the present invention, a method for preparing tetrazole methanesulfonic acid salts comprises an acylation reaction using a novel 4-iodine-4H-chromene-2-carbothionic acid S-benzothiazole-2-yl ester. The method of the present invention can shorten a reaction time and improve safety as compared to conventional methods, and can prepare high-purity tetrazole methanesulfonic acid salts at a high yield rate without using a column chromatography method.Type: ApplicationFiled: January 14, 2011Publication date: December 27, 2012Applicant: HANMI SCIENCE CO., LTDInventors: Keuk Chan Bang, Bum Woo Park, Jong Won Choi, Jae Chul Lee, Yong Hoon An, Young Gil Ahn, Maeng Sup Kim
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Publication number: 20120328569Abstract: Disclosed are compounds of formula (I) that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.Type: ApplicationFiled: March 2, 2011Publication date: December 27, 2012Inventors: Casey Cameron McComas, Nigel J. Liverton, Richard Soll, Peng Li, Xuanjia Peng, Hao Wu, Frank Narjes, Joerg Habermann, Uwe Koch, Shilan Liu
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Publication number: 20120322787Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-?, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 27, 2012Publication date: December 20, 2012Applicant: Genzyme CorporationInventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Frederic Vinick, Thomas H. Jozefiak, Yibin Xiang, John Kane, Junkai Liao
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Patent number: 8329907Abstract: The present invention relates to compounds according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.Type: GrantFiled: March 9, 2010Date of Patent: December 11, 2012Assignee: Merck Patent GmbHInventors: Melanie Schultz, Kai Schiemann, Wolfgang Staehle
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Publication number: 20120302748Abstract: The disclosure relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. Also provided are pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. Provided are methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1B1 and allelic variants thereof. Finally, provided is a method for determining the efficacy of a compound as described herein in treating cancer.Type: ApplicationFiled: February 28, 2012Publication date: November 29, 2012Applicant: THE UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEEInventors: Steven Albert Everett, Saraj Ulhaq
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Publication number: 20120296093Abstract: This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center.Type: ApplicationFiled: July 31, 2012Publication date: November 22, 2012Inventors: George Wu, Anantha R. SUDHAKAR, Tao WANG, Ji XIE, Frank Xing CHEN, Marc POIRIER, Mingsheng HUANG, Vijay SABESAN, Daw-long KWOK, Jian CUI, Xiaojing YANG, Tiruvettipuram K. THIRUVENGADAM, Jing LIAO, Ilia A. Zavialov, Hoa N. NGUYEN, Ngiap Kie LIM
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Patent number: 8314248Abstract: The present invention describes a novel process for preparing an epothilone derivative using substituted pyridines and methyltrioxorhenium as catalyst.Type: GrantFiled: November 30, 2011Date of Patent: November 20, 2012Assignee: Bayer Pharma AGInventors: Johannes Platzek, Orlin Petrov, Stephan Prühs
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Patent number: 8314257Abstract: The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2.Type: GrantFiled: September 17, 2008Date of Patent: November 20, 2012Assignee: Oxagen LimitedInventors: David Middlemiss, Mark Richard Ashton, Edward Andrew Boyd, Frederick Arthur Brookfield, Michael George Hunter, Mark Whittaker, Chris Palmer, Eric R. Pettipher
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Publication number: 20120270859Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: June 14, 2012Publication date: October 25, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias TREU, Ulrich GUERTLER, Thomas KARNER, Oliver KRAEMER, Jens Juergen QUANT, Stephan Karl ZAHN
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Publication number: 20120270868Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: October 17, 2011Publication date: October 25, 2012Applicant: Boehringer Ingelheim International GmbHInventors: Thomas Martin KIRRANE, Daniel Richard MARSHALL, Robert SIBLEY, Roger John SNOW, Fariba SOLEYMANZADEH, Ronald John SORCEK
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Publication number: 20120270912Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.Type: ApplicationFiled: June 27, 2012Publication date: October 25, 2012Inventors: Michael Lee Jones, David Gunn, John Howard Jones, Michael C. Van Zandt
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Patent number: 8293774Abstract: The present invention relates to an optically active (R)-aryloxypropionic acid amide compound which has high selectivity and safety for protecting a crop such as rice, wheat, barley and soy bean, and exhibits excellent herbicidal activity against weeds, and a herbicidal composition comprising the same.Type: GrantFiled: July 2, 2008Date of Patent: October 23, 2012Assignee: Kyung Nong CorporationInventors: Joo-kyung Kim, Dong-hoo Kim, Hyung-ho Kim, Kyung-hyun Kim, Cheol-su Yoon, In-cheon Hwang
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Publication number: 20120252047Abstract: A latent fluorophore is derived from salicylic acid, and containing a fluorogenic group and a moiety represented by formula I wherein the fluorogenic group is directly linked to the moiety of formula I or indirectly linked thereto via a linkage structure. In addition, a method of preparing a latent fluorophore, a method of using the same and a kit containing the same are also introduced.Type: ApplicationFiled: March 30, 2011Publication date: October 4, 2012Applicant: NATIONAL TAIPEI UNIVERSITY OF TECHNOLOGYInventor: Sheng-Tung HUANG
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Publication number: 20120252770Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicamentsType: ApplicationFiled: March 23, 2012Publication date: October 4, 2012Inventors: Markus Berger, Jan Dahmén, Karl Edman, Anders Eriksson, Balint Gabos, Thomas Hansson, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepistö, Darren McKerrencher, Magnus Munck af Rosenschöld, Stinabritt Nilsson, Hartmut Rehwinkel, Camilla Taflin
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Patent number: 8268803Abstract: The present invention relates to 5,6-ring annulated indole derivatives of the formula (I), compositions comprising at least one 5,6-ring annulated indole derivatives, and methods of using the 5,6-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: GrantFiled: December 17, 2007Date of Patent: September 18, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Frank Bennett, Srikanth Venkatraman, F. George Njoroge, Kevin X. Chen, Neng-Yang Shih, Stuart B. Rosenblum, Joseph A. Kozlowski
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Publication number: 20120214786Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), 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, R6, R7, R8 have meanings given in the description.Type: ApplicationFiled: August 17, 2011Publication date: August 23, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Benjamin PELCMAN, Robert ROENN
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Patent number: 8247415Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: GrantFiled: April 2, 2009Date of Patent: August 21, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Cheng Zhu
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Publication number: 20120208827Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of benzimidazoles in the treatment of cancer.Type: ApplicationFiled: October 27, 2010Publication date: August 16, 2012Inventors: Steven Dock, Jason Hallman, Christopher Laudeman, Ronggang Liu, Aaron Miller, Michael Lee Moore, David Musso, Cynthia Parrish
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Publication number: 20120208812Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.Type: ApplicationFiled: October 21, 2010Publication date: August 16, 2012Applicant: Janssen Pharmaceutica N.V.Inventors: Wenying Chai, Michael A. Letavic, Kiev S. Ly, Daniel J. Pippel, Dale A. Rudolph, Kathleen C. Sappey, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman, Akinola Soyode-Johnson, Emily M. Stocking, Devin M. Swanson
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Patent number: 8231754Abstract: An dye compound of the following formula (1): wherein D represents a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group; L represents ?CR2—, ?N—, or ?N—NH—; R1 represents a monovalent substituent; R2 represents a hydrogen atom or a cyano group; n indicates an integer of from 0 to 4; when n is 2 or more, then plural R1's may be the same or different.Type: GrantFiled: February 27, 2009Date of Patent: July 31, 2012Assignee: FUJIFILM CorporationInventors: Yoshihiko Fujie, Tetsuya Watanabe, Hisashi Mikoshiba
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Publication number: 20120190639Abstract: The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.Type: ApplicationFiled: April 30, 2010Publication date: July 26, 2012Applicant: UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEEInventors: Steven Albert Everett, Saraj Ulhaq
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Patent number: 8202871Abstract: The present application discloses compounds of the formula: and pharmaceutical compositions containing same and their use for treating and preventing various pathologies, including obesity, appetite disorders, excess weight and diabetes.Type: GrantFiled: January 24, 2011Date of Patent: June 19, 2012Assignee: Sanofi-AventisInventors: Marco Baroni, Letizia Puleo
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Publication number: 20120115845Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.Type: ApplicationFiled: November 7, 2011Publication date: May 10, 2012Inventors: Jack McQueen ALLEN, Roger John Butlin, Clive Green, William McCoull, Graeme Richard Robb, James Matthew Wood
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Publication number: 20120115856Abstract: A compound depicted by the formula below, or a pharmaceutically acceptable salt or solvate thereof. wherein, R1 represents (1) a C3-6 alkyl group, (2) a C1-6 alkyl group substituted with one or more substituent group(s) selected from those consisting a halogen atom, etc., (3) a C3-10 non-aromatic cyclic hydrocarbon group or a 5- to 6-membered non-aromatic heterocyclic group which respectively is optionally substituted with one or more substituent group(s) selected from those consisting an oxo group, etc., (4) an aromatic cyclic hydrocarbon group substituted with one or more substituent selected from the group consisting halogen atom and C1-4 alkoxy group; X represents NH, O, or S; Y represents CH or N; Z represents N or a C—R2; R2 represents (1) hydrogen atom, (2) a C1-6 alkyl group, a C2-6 alkenyl group or a C2-6 alkynyl group that respectively is optionally substituted with one or more substituent group(s) selected from among those consisting (a) a halogen atom, etc.Type: ApplicationFiled: May 28, 2010Publication date: May 10, 2012Inventors: Junichi Ishikawa, Koichi Saito, Norihisa Ohe, Kentaro Kobayashi
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Publication number: 20120108565Abstract: The present invention provides DNA Gyrase and/or Topo IV inhibitors of Formula (I), which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed by gram positive, gram negative and anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Pseudomonus spp., Acenetobacter spp., Mvraxalla spp., Chlamydia spp., Mycoplasma spp., Legionella spp., Mycobacterium spp., Helicobacter, Clostridium spp., Bacteroides spp., Cotynebacterium, Bacillus spp., Enterobactericeae (E. coli, Klebsiella spp., Proteus spp., etc.) or any combination thereof. Also provided, are processes for preparing compounds disclosed herein, pharmaceutical compositions containing compounds disclosed herein, and methods of treating bacterial infections.Type: ApplicationFiled: July 30, 2009Publication date: May 3, 2012Inventors: Lalima Sharma, Jitendra A. Sattigeri, Narest Kumar, Ajay Yadav, Rijwan Momim, Shahadat Ahmed, Ian A. Cliffe, Pradip Kumar Bhatnagar, Sanjay Ghosh, V. Samuel Raj, Dilip J. Upadhyay
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Publication number: 20120101103Abstract: Compounds of Formula I: (I) in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13.Type: ApplicationFiled: December 18, 2009Publication date: April 26, 2012Applicant: ARRAY BIOPHARMA INC.Inventors: Adam Cook, Kevin W. Hunt, Robert Kirk Delisle, Todd Romoff, Christopher T. Clark, Ganghyeok Kim, Christopher P. Corrette, George A. Doherty, Laurence E. Burgess
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Patent number: 8163936Abstract: The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2.Type: GrantFiled: September 17, 2008Date of Patent: April 24, 2012Assignee: Oxagen LimitedInventors: David Middlemiss, Mark Richard Ashton, Edward Andrew Boyd, Frederick Arthur Brookfield, Michael George Hunter, Mark Whittaker, Chris Palmer, Eric R. Pettipher
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Patent number: 8163931Abstract: The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2.Type: GrantFiled: September 17, 2008Date of Patent: April 24, 2012Assignee: Oxagen LimitedInventors: David Middlemiss, Mark Richard Ashton, Edward Andrew Boyd, Frederick Arthur Brookfield, Michael George Hunter, Mark Whittaker, Chris Palmer, Eric R. Pettipher
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Patent number: 8163932Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.Type: GrantFiled: February 8, 2010Date of Patent: April 24, 2012Assignee: Alinea Pharmaceuticals, Inc.Inventors: Michael Lee Jones, David Gunn, John Howard Jones, Michael C. Van Zandt
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Publication number: 20120095040Abstract: The invention relates to compounds of the general formula (I) where: R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, or NR8R9 group; m, n, o and p independently are a number from 0 to 3; A is a covalent bond, an oxygen atom, a C1-6-alkylene group or a —O—C1-6-alkylene group in which the end that is an oxygen atom is bonded to the R1 group while the end that is an alkylene group is bonded to the carbon of the bicyclic compound; R1 is an optionally substituted aryl or heteroaryl group; R3 is a hydrogen or fluorine atom or a C1-6-alkyl or trifluoromethyl group; R4 is an optionally substituted 5-membered heterocyclic compound; wherein the compounds can be in the state of a base or an acid addition salt. The invention can be used in therapeutics.Type: ApplicationFiled: May 11, 2010Publication date: April 19, 2012Applicant: SANOFIInventors: Ahmed Abouabdellah, Luc Even, Aude Fayol, Julien Vache, Philippe Yauche
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Patent number: 8153811Abstract: The present invention provides a sensitive fluorimetric indicator for analytes determination in the oxygen-insensitive DT-diaphorase-coupled dehydrogenases assay by omitting NADH, which is generated by reaction in the presence of analytes, which presents to the applicability as a biosensor for future clinical diagnostic. Furthermore, the novel long-wavelength latent fluorimetric indicator is also a user-friendly probe for monitoring DT-diaphorase activity. The fluorescence signal revealed by this process is specific and exhibited in the near red spectrum region.Type: GrantFiled: February 6, 2009Date of Patent: April 10, 2012Assignee: National Taipei University of TechnologyInventors: Sheng-Tung Huang, Yi-Xiang Peng
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Publication number: 20120077984Abstract: The present invention describes a novel process for preparing an epothilone derivative using substituted pyridines and methyltrioxorhenium as catalyst.Type: ApplicationFiled: November 30, 2011Publication date: March 29, 2012Inventors: Johannes Platzek, Orlin Petrov, Stephan Prühs
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Publication number: 20120046250Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.Type: ApplicationFiled: March 2, 2010Publication date: February 23, 2012Applicant: STEMSYNERGY THERAPEUTICS, INCInventor: Darren Orton
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Publication number: 20120040974Abstract: The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.Type: ApplicationFiled: August 18, 2009Publication date: February 16, 2012Applicant: YALE UNIVERSITYInventors: William L. Jorgensen, Richard J. Bucala
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Publication number: 20120041207Abstract: A compound having Formula I wherein one of R1 and R2 is a group of the formula wherein R4 is selected from H and hydrocarbyl, R5 is a hydrocarbyl group and L is an optional linker group, or R1 and R2 together form a ring substituted with the group wherein R3 is H or a substituent, and wherein X is selected from S, O, NR6 and C(R7)(R8), wherein R6 is selected from H and hydrocarbyl groups, wherein each of R7 and R8 are independently selected from H and hydrocarbyl groups.Type: ApplicationFiled: August 10, 2011Publication date: February 16, 2012Applicant: Sterix LimitedInventors: Nigel Vicker, Su Xiangdong, Dharshini Ganeshapillai, Atul Purohit, Michael John Reed, Barry Victor Lloyd Potter
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Patent number: 8114893Abstract: In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.Type: GrantFiled: December 17, 2009Date of Patent: February 14, 2012Assignees: Genentech, Inc., Abbott Laboratories, The Walter and Eliza Hall Medical Research InstituteInventors: Jonathan Bayldon Baell, Chinh Thien Bui, Peter Colman, Danette A. Dudley, Wayne J. Fairbrother, John A. Flygare, Guillaume Laurent Lessene, Chudi Ndubaku, George Nikolakopoulos, Carl Steven Rye, Brad Edmund Sleebs, Brian John Smith, Keith Geoffrey Watson, Steven W. Elmore, Andrew M. Petros, Andrew J. Souers, Peter Czabotar
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Patent number: 8110686Abstract: The present invention relates to methods of treatment of certain metabolic diseases, and to novel compounds and their prodrugs, and/or pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds useful in treating such diseases. In particular, this invention relates to the use of novel compounds and compositions for treatment of cardiovascular diseases, diabetes, cancers, acidosis, and obesity through the inhibition of malonyl-CoA decarboxylase (MCD). These compounds have the formulae (I) and (II), wherein Y, C, R1, R2, R6, and R7 are defined herein.Type: GrantFiled: May 3, 2010Date of Patent: February 7, 2012Assignee: Chugai Seiyaki Kabushiki KaishaInventors: Thomas Arrhenius, Jie Fei Cheng, Mark E. Wilson, Rossy Serafimov, Alex M. Nadzan, Gary D. Lopaschuk, Jason R. Dyck
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Publication number: 20120028959Abstract: The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.Type: ApplicationFiled: March 26, 2010Publication date: February 2, 2012Applicant: MERCK SERONO S.A.Inventors: Siva Sanjeeva Rao Thunuguntla, Hosahalli Subramanya, Satish Reddy Kunnam, Sekhar Reddy Sanivaru Vijay, Chakrapani Bingi, Raviraj Kusanur, Matthias Schwarz, Michael Arlt
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Patent number: 8106215Abstract: The invention relates to 3-aza-bicyclo[3.3.0]octane derivatives of the formula (I) wherein R1, R2, R3, and A are as described in the description and their use as orexin receptor antagonists.Type: GrantFiled: July 2, 2008Date of Patent: January 31, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
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Publication number: 20120015976Abstract: The present invention relates to compounds according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.Type: ApplicationFiled: March 9, 2010Publication date: January 19, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANK TER HAFTUNGInventors: Melanie Schultz, Kai Schiemann, Wolfgang Staehle
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Patent number: 8088805Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: March 16, 2007Date of Patent: January 3, 2012Assignee: MethylGene Inc.Inventors: Daniel Delorme, Silvana Marcela Leit de Moradei, Sylvie Frechette
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Publication number: 20110312935Abstract: There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.Type: ApplicationFiled: September 25, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Roland Pfau, Kirsten Arndt, Henri Doods, Norbert Hauel, Klaus Klinder, Raimund Kuelzer, Juergen Mack, Henning Priepke, Dirk Stenkamp
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Publication number: 20110312996Abstract: The embodiments provide compounds of the general Formulae VI, VII, VIII, IX, X, XI, XII, XIII, XIV, and XV as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: May 16, 2011Publication date: December 22, 2011Applicant: InterMune, Inc.Inventors: Brad Buckman, John B. Nicholas, Vladimir Serebryany, Scott D. Seiwert