Additional Hetero Ring Containing Patents (Class 546/187)
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Publication number: 20140275010Abstract: The present invention provides quaternary salts, such as those of Formula I: as well as the use thereof in methods of treatment for cancer.Type: ApplicationFiled: March 11, 2014Publication date: September 18, 2014Inventors: Guo Zhu Zheng, Yuan Wang, Gregg F. Keany, Kenzo Arai, Kazunobu Kira, Xiang Liu, Nick Gearhart, Baudouin Gerard
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Patent number: 8835648Abstract: Heterocyclic compounds that modulate the hedgehog signaling pathway, pharmaceutical composition thereof and their therapeutic applications.Type: GrantFiled: June 9, 2010Date of Patent: September 16, 2014Assignee: 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: 20140256756Abstract: Compounds of Formula (I) and pharmaceutically acceptable salts thereof in which X1, X2, X3, L, R3, R4, R5, R7 and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.Type: ApplicationFiled: October 30, 2012Publication date: September 11, 2014Inventors: Thomas Daniel Aicher, Josef Roland Benscik, Steven Armen Boyd, Kevin Ronald Condroski, Jay Bradford Fell, John Peter Fischer, Ronald Jay Hinklin, Scott Pratt, Ajay Singh, Timothy M. Turner
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Patent number: 8829199Abstract: A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which can inhibit a fibroblast growth factor receptor (FGFR) family kinase in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a C6-10 aryl group; R1 and R2 independently represent H, OH, X, CN, NO2, a C1-4 haloalkyl group, a C1-6 alkyl group, or the like <R1 and R2 together form a (substituted) 3- to 10-membered heterocyclyl group or a (substituted) 5- to 10-membered heteroaryl group>; R3 represents H, a C1-5 alkyl group, a C6-10 aryl group, a C1-5 alkyl group, or a C1-4 haloalkyl group; and R4 represents H, X, a C1-3 alkyl group, a C1-4 haloalkyl group, OH, CN, NO2, or the like.Type: GrantFiled: August 5, 2010Date of Patent: September 9, 2014Assignees: Chugai Seiyaku Kabushiki Kaisha, F. Hoffmann-La Roche AGInventors: Naoki Taka, Masayuki Ohmori, Kyoko Takami, Masayuki Matsushita, Tadakatsu Hayase, Ikumi Hyodo, Masami Kochi, Hiroki Nishii, Hirosato Ebiike, Yoshito Nakanishi, Toshiyuki Mio, Lisha Wang, Weili Zhao
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Publication number: 20140249130Abstract: The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, or are prodrugs thereof, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis and cancer.Type: ApplicationFiled: May 4, 2012Publication date: September 4, 2014Inventors: Denis Deschenes, Michael D. Altman, John Michael Ellis, Christian Fischer, Andrew M. Haidle, Solomon D. Kattar, Alan B. Northrup, Adam J. Schell, Graham F. Smith, Brandon M. Taoka, Corey Bienstock, Maria Emilia Di Francesco, Anthony Donofrio, Scott Peterson, Kerrie B. Spencer, James Patrick Jewell, Amjad Ali, David Jonathan Bennett, Qun Dang, John Wai
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Patent number: 8815868Abstract: The present invention relates to novel oxindole derivatives of the general formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases.Type: GrantFiled: December 28, 2007Date of Patent: August 26, 2014Assignee: Abbott GmbH & Co. KGInventors: Astrid Netz, Thorsten Oost, Herve Geneste, Wilfried Braje, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch, Andrea Hager-Wernet
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Publication number: 20140235641Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.Type: ApplicationFiled: September 21, 2012Publication date: August 21, 2014Inventors: Jason Brubaker, Joshua Close, Tony Siu, Graham Frank Smith, Luis E. Torres, Hyun Chong Woo, Jonathan R. Young, Zhongyong Wei, Feng Shi
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Patent number: 8809370Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: GrantFiled: March 13, 2013Date of Patent: August 19, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
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Publication number: 20140221334Abstract: 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: April 10, 2014Publication date: August 7, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Guy William Bemis, Francois Maltais, Tiansheng Wang, Ronald Marcellus Alphonsus Knegtel, Christopher John Davis, Damien Fraysse, Dean Boyall, Luca Settimo, Stephen Young, Michael Paul Mortimore
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Patent number: 8791136Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: GrantFiled: July 29, 2011Date of Patent: July 29, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
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Patent number: 8785449Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: GrantFiled: September 18, 2012Date of Patent: July 22, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
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Patent number: 8778929Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.Type: GrantFiled: September 28, 2009Date of Patent: July 15, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
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Publication number: 20140194440Abstract: The present invention relates to novel 5,6-disubstituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the manufacture of a medicament.Type: ApplicationFiled: September 27, 2013Publication date: July 10, 2014Inventors: Wilfried Braje, Thorsten Oost, Astrid Netz, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
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Publication number: 20140187581Abstract: The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to 5-HT4 receptors.Type: ApplicationFiled: January 5, 2012Publication date: July 3, 2014Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Suresh Yarlagadda, Srinivasa Rao Ravella, Anil Karbhari Shinde, Ramasastri Kamphampati, Praveen Kumar Roayapalley, Pradeep Jayarajan, Gopinadh Bhyrapuneni, Sriramachandra Murthy Patnala, Jyothsna Ravula, Venkateswarlu Jasti
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Publication number: 20140179686Abstract: The present invention relates to novel vanilloid receptor ligands, to a process for the production thereof, to pharmaceutical preparations containing these compounds and to the use of these compounds for the production of pharmaceutical preparations.Type: ApplicationFiled: February 25, 2014Publication date: June 26, 2014Applicant: Gruenenthal GmbHInventors: Jeewoo LEE, Hyung Chul Ryu, Robert FRANK, Gregor BAHRENBERG, Jean DE VRY, Thomas CHRISTOPH, Derek John SAUNDERS, Klaus SCHIENE, Bernd SUNDERMANN
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Publication number: 20140179738Abstract: The present invention provides N-substituted-heterocycloalkyloxybenzamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment of the invention is a compound having the structure in which R1, R2, R3, R4, T, n, w and x are as described herein. In certain embodiments of the invention, a compound of the present invention activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: February 25, 2014Publication date: June 26, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Jiaxin Yu, Hui Hong, Sambaiah Thota, Xiang Xu, Ihab S. Darwish
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Publication number: 20140161731Abstract: Described are a compound of formula (II) or (III): The compounds are effective in the treatment of disease, including a tauopathy condition or a disease of tau protein aggregation.Type: ApplicationFiled: February 14, 2014Publication date: June 12, 2014Applicant: WisTa Laboratories Ltd.Inventors: Scott Clunas, John Mervyn David Storey, Janet Elizabeth Rickard, David Horsley, Charles Robert Harrington, Claude Michel Wischik
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Publication number: 20140148467Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: February 3, 2014Publication date: May 29, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
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Publication number: 20140142081Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.Type: ApplicationFiled: November 21, 2013Publication date: May 22, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Yongsheng Chen
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Patent number: 8729532Abstract: The present invention provides a light-absorbing material capable of providing high photoelectric conversion efficiency when applied to a photoelectric conversion element. The light-absorbing material of the present invention has a structure represented by Formula (1) below: X—Y??(1) (wherein X represents a light-absorbing site, and Y represents a radical site that becomes a radical when in an oxidized state and/or when in a reduced state, and is capable of repeated oxidation-reduction).Type: GrantFiled: May 21, 2010Date of Patent: May 20, 2014Assignees: Panasonic Corporation, Waseda UniversityInventors: Takashi Sekiguchi, Hiroyuki Nishide, Michio Suzuka, Takeyuki Yamaki, Kenichi Oyaizu, Fumiaki Kato, Satoko Kambe
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Patent number: 8729081Abstract: The present invention provides compounds which antagonize epsilon protein kinase C (PKC?). These compounds have a structural formula (Ia), (Ic) or (II). The present invention also provides pharmaceutical compositions containing these compounds and methods of treating various diseases, conditions, and/or symptoms by using these compounds.Type: GrantFiled: October 12, 2009Date of Patent: May 20, 2014Assignee: VM Discovery Inc.Inventor: Jay Jie-Qiang Wu
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Publication number: 20140135304Abstract: The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to Histamine H3 receptors.Type: ApplicationFiled: June 7, 2011Publication date: May 15, 2014Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Ramasastri Kambhampati, Amol Dinakar Deshpande, Adi Reddy Dwarampudi, Narasimhareddy Gangadasari, Sangram Keshari Saraf, Vishwottam Nagaraj Kandikere, Pradeep Jayarajan, Ishtiyaque Ahmad, Mohmadsadik Abdulhamid Mulla, Venkateswarlu Jasti
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Patent number: 8716312Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: GrantFiled: November 17, 2009Date of Patent: May 6, 2014Assignee: Merck Sharp & Dohme CorporationInventors: Pauline C. Ting, Robert Aslanian, Mary Ann Caplen, Jianhua Cao, Tin-Yau Chan, David Kim, Hyunjin Kim, Jae-Hun Kim, Rongze Kuang, Joe F. Lee, John Schwerdt, Heping Wu, Nicolas Zorn
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Patent number: 8703775Abstract: The present invention relates to novel amidomethyl-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders.Type: GrantFiled: December 5, 2008Date of Patent: April 22, 2014Assignee: AbbVie Deutschland GmbH & Co. KGInventors: Thorsten Oost, Astrid Netz, Herve Geneste, Wilfried Braje, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch, Andrea Hager-Wernet
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Patent number: 8703774Abstract: The present invention relates to novel carbamate-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders.Type: GrantFiled: December 5, 2008Date of Patent: April 22, 2014Assignee: AbbVie Deutschland GmbH & Co. KGInventors: Astrid Netz, Thorsten Oost, Herve Geneste, Wilfried Braje, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch, Andrea Hager-Wernet
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Patent number: 8691846Abstract: The present invention relates to piperidine sulphonamide derivatives of formula wherein Ar1, Ar2, R1, R2, m and n are as defined in the description and claims, or pharmaceutically suitable acid addition salts thereof. The compounds of formula I are orexin receptor antagonists and the related compounds can be useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.Type: GrantFiled: April 2, 2013Date of Patent: April 8, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Patent number: 8685959Abstract: Benzimidazole, benzopyrazole and benzotriazole compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.Type: GrantFiled: November 30, 2012Date of Patent: April 1, 2014Assignee: ChemoCentryx, Inc.Inventors: Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jay Powers, Ju Yang
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Patent number: 8674113Abstract: 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, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.Type: GrantFiled: December 8, 2011Date of Patent: March 18, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Henning Priepke, Henri Doods, Alexander Heim-Riether, Raimund Kuelzer, Roland Pfau, Klaus Rudolf, Dirk Stenkamp
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Publication number: 20140073622Abstract: To develop an antibiotic having a novel mechanism of action, the present inventors have searched for a compound that has weak cytotoxicity, the physical property of high solubility in water, the effect of inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and sufficient antibacterial activity. As a result, the present inventors have completed the present invention by finding that a compound of the present invention represented by the general formula (1), a pharmacologically acceptable salt thereof, and a prodrug thereof have desirable properties. The present invention provides a pharmaceutical composition (particularly, a preventive or therapeutic composition for infectious disease) comprising a compound represented by the formula (1), a pharmacologically acceptable salt thereof, or a prodrug thereof as an active ingredient.Type: ApplicationFiled: September 13, 2013Publication date: March 13, 2014Applicant: Daiichi Sankyo Company, LimitedInventors: Tsuyoshi Soneda, Hiroshi Takeshita, Yoshiko Kagoshima, Yuko Yamamoto, Takafumi Hosokawa, Toshiyuki Konosu, Nobuhisa Masuda, Takuya Uchida, Issei Achiwa, Junichi Kuroyanagi, Tetsunori Fujisawa, Aki Yokomizo, Tetsuji Noguchi
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Publication number: 20140057895Abstract: The present invention relates to a novel indazole- or pyrrolopyridine-derivative comprising a 5 membered heterocyclic substituent at 1 position thereof which has an agonistic action or a partial agonistic action against serotonin-4 receptor, and a pharmaceutical composition comprising the same.Type: ApplicationFiled: June 6, 2012Publication date: February 27, 2014Inventors: Kazuhiro Mizuno, Junya Ikeda, Takanori Nakamura, Masato Iwata, Hiromichi Otaka, Nana Goto
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Patent number: 8658636Abstract: The present invention relates to quinoline analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.Type: GrantFiled: March 23, 2011Date of Patent: February 25, 2014Assignee: GlaxoSmithKline, LLCInventors: Carl A. Brooks, Mui Cheung, Hilary S. Eidam, Ryan M. Fox, Mark A. Hilfiker, Eric S. Manas, Guosen Ye
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Patent number: 8658131Abstract: Bipiperidinyl compounds and salts thereof are disclosed. The compounds include high affinity ligands for ?1 receptors. Some compounds are also highly selective for ?1 receptor compared to ?2 receptor. Compounds can comprise radioisotopes, including 18F or 11C. Radiolabeled compounds can be used as probes for imaging distribution of ?1 receptor in a subject such as a human using positron emission tomography (PET) scanning.Type: GrantFiled: June 21, 2011Date of Patent: February 25, 2014Assignee: Washington UniversityInventors: Zhude Tu, Robert H. Mach, Wei Wang, Stanley M. Parsons
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Publication number: 20140051673Abstract: Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, E, T, n and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: October 14, 2013Publication date: February 20, 2014Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Hui Hong, Xiang Xu, Jiaxin Yu, Rajinder Singh, Ihab S. Darwish, Sambaiah Thota
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Publication number: 20140051679Abstract: The present teachings provide a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.Type: ApplicationFiled: October 12, 2012Publication date: February 20, 2014Applicant: UNIVERISTY HEALTH NETWORKSInventors: Heinz W. Pauls, Radoslaw Laufer, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Yunhui Lang, Narendra Kumar B. Patel, Louise G. Edwards, Grace Ng, Peter B. Sampson, Miklos Feher, Donald E. Awrey
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Publication number: 20140045813Abstract: The present invention encompasses compounds of the formula (I) wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.Type: ApplicationFiled: August 8, 2013Publication date: February 13, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joerg Martin BENTZIEN, Angela Kay BERRY, Todd BOSANAC, Michael Jason BURKE, Darren Todd DISALVO, Joshua Courtney HORAN, Shuang LIANG, Can MAO, Wang MAO, Yue SHEN, Fariba SOLEYMANZADEH, Renee M. ZINDELL
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Patent number: 8642634Abstract: Disclosed are compounds of Formulae 1, 1A, 1B and 1C including all geometric and stereoisomers, N-oxides, and salts thereof, wherein R1, R2, R4a1, R4a2, A, Aa, G, M, W, Z1, Z3, X, J, J1 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: GrantFiled: July 27, 2007Date of Patent: February 4, 2014Assignee: E I du Pont de Nemours and CompanyInventors: Robert James Pasteris, Mary Ann Hanagan
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Publication number: 20140023611Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: ApplicationFiled: January 4, 2013Publication date: January 23, 2014Inventor: ARDELYX, INC.
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Publication number: 20140018389Abstract: This disclosure concerns novel compounds of Formula (I) or as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.Type: ApplicationFiled: September 16, 2013Publication date: January 16, 2014Inventors: Rico Lavoie, John A. Bender, Jeffrey Lee Romine, Edward H. Ruediger, Carol Bachand, Omar D. Lopez, Qi Chen, Makonen Belema, John F. Kadow, Lawrence G. Hamann
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Patent number: 8623857Abstract: The present invention provide Imidazole Carboxamide Compounds of Formula (I): wherein D, T, R1, R2, R3, and R6 are as defined herein, and pharmaceutically acceptable salts of such Imidazole Carboxamide Compounds. The Imidazole Carboxamide Compounds are useful in the treatment of cancer and other aberrant conditions that result from overstimulation of the PDK-1 signaling pathway.Type: GrantFiled: May 24, 2011Date of Patent: January 7, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Hon-Chung Tsui, Sunil Paliwal, Hyunjin M. Kim, Angela D. Kerekes, Mary Ann Caplen, Sara J. Esposite, Brian A. McKittrick, Thierry Olivier Fischmann, Ronald J. Doll, Matthew Paul Rainka, Ang Li
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Publication number: 20140005174Abstract: Disclosed are the CCR2 antagonists of Formula I: I or pharmaceutically acceptable salt thereof wherein R7, A, X, B, and n are defined herein. Also disclosed are pharmaceutical compositions containing the compounds, methods of treatment using the compounds, and compositions to treat diseases or disorders associated with CCR2 activity.Type: ApplicationFiled: March 14, 2012Publication date: January 2, 2014Inventors: Anilkumar G. Nair, Joseph A. Kozlowski, Jose S. Duca, Stuart B. Rosenblum
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Publication number: 20130336920Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y, A, R1 and R2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: ApplicationFiled: January 4, 2013Publication date: December 19, 2013Applicant: ARDELYX, INC.Inventor: Ardelyx, Inc.
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Publication number: 20130323203Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.Type: ApplicationFiled: August 2, 2013Publication date: December 5, 2013Applicant: Gilead Sciences, Inc.Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Michael Mertzman Belmont, Philip Anthony Morganelli, William J. Watkins
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Publication number: 20130317213Abstract: The present disclosure relates to methods for making compounds useful in the treatment of Hepatitis C virus (HCV) infection.Type: ApplicationFiled: August 1, 2013Publication date: November 28, 2013Inventors: Shawn K. Pack, Steven Tymonko, Bharat P. Patel, Kenneth J. Natalie, JR., Makonen Belema
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Publication number: 20130303492Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.Type: ApplicationFiled: March 14, 2013Publication date: November 14, 2013Inventors: Erik Dean Raaum, Garrett Thomas Potter, Tai Wei Ly
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Patent number: 8574563Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: September 11, 2012Date of Patent: November 5, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
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Patent number: 8575168Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.Type: GrantFiled: October 1, 2010Date of Patent: November 5, 2013Assignee: IRM LLCInventors: Mihai Azimioara, Christopher Cow, Robert Epple, Gerald Lelais, John Mecom, Victor Nikulin
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Publication number: 20130289020Abstract: Disclosed are compounds that are antagonists of the CXCR4 receptor.Type: ApplicationFiled: October 13, 2011Publication date: October 31, 2013Applicant: Proximagen LimitedInventors: Edward Daniel Savory, Allson Stewart, Allison Cartey, Giles Brown, Iain Simpson, Kathryn Oliver, Lee Patient, Michael Higginbottom, Andrew Graham Cole
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Publication number: 20130288331Abstract: Provided herein are compounds and methods of using same for the perturbation and/or inhibition of protein-protein interactions. Also provided herein is a data mining method useful for the identification of protein-protein interactions that may be inhibited by these compounds.Type: ApplicationFiled: April 19, 2013Publication date: October 31, 2013Inventor: Kevin Burgess
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Patent number: 8569340Abstract: Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, E, T, n and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: GrantFiled: January 11, 2012Date of Patent: October 29, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Hong, Xiang Xu, Jiaxin Yu, Rajinder Singh, Ihab S. Darwish, Sambaiah Thota
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Publication number: 20130280211Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: June 17, 2013Publication date: October 24, 2013Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. ST. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann