At Least Two Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 548/311.7)
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Patent number: 9801960Abstract: Provided is a novel probe for a biological specimen for labelling by itself and clearly visualizing one of a specific cell and a specific cell organ in a living body, the probe having excellent spectral characteristics and exhibiting excellent storage stability. The probe for a biological specimen contains, as an active agent, at least one kind of compound represented by a general formula (I).Type: GrantFiled: February 17, 2015Date of Patent: October 31, 2017Assignee: CANON KABUSHIKI KAISHAInventors: Taichi Shintou, Takeshi Miyazaki, Masashi Hirose, Taketoshi Okubo, Kohei Watanabe, Tsuyoshi Nomoto, Toshio Tanaka, Yuhei Nishimura, Yasuhito Shimada, Norihiro Nishimura
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Publication number: 20150133444Abstract: The present disclosure provides derivatives of melampomagnolide B (MMB), including carbonates, carbamates, and thiocarbamates. The derivatives may be synthesized via an MMB triazole intermediate. These derivatives are useful for treating cancer in humans.Type: ApplicationFiled: November 10, 2014Publication date: May 14, 2015Inventors: Venumadhav Janganati, Narsimha Reddy Penthala, Peter A. Crooks, Craig T. Jordan
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Publication number: 20150119406Abstract: Tricyclic pyrone compounds having high oral bioavailability, excellent blood-brain barrier permeability, and low toxicity are presented. Administration of the compounds to Alzheimer's Disease transgenic models resulted in substantially reduced soluble and insoluble A? species in the brain without affecting general behavior and motor coordination. Furthermore, in addition to blocking the toxicity and formation of both intraneuronal and extracellular A? aggregates, the compounds also increase cellular cholesterol efflux, restore axonal trafficking, and enhance hippocampal synaptic plasticity.Type: ApplicationFiled: September 30, 2014Publication date: April 30, 2015Inventors: Duy H. Hua, Lee-way Jin, Izumi Maezawa, Xinmin Xie
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Patent number: 8969341Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: GrantFiled: November 28, 2012Date of Patent: March 3, 2015Assignee: Novartis AGInventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
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Publication number: 20150045327Abstract: The present invention discloses compounds according to Formula I: wherein R1 is as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment cystic fibrosis by administering a compound of the invention.Type: ApplicationFiled: August 5, 2014Publication date: February 12, 2015Inventors: Steven Emiel VAN DER PLAS, Hans KELGTERMANS, Sébastien Jean Jacques Cédric DROPSIT MONTOVER, Sébastien Laurent Xavier MARTINA, Martin James Inglis ANDREWS
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Patent number: 8937184Abstract: The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid CB2 receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which cannabinoid CB2 receptors are involved. The compounds have the general formula (I) wherein R1-R4 have the meanings given in the specification.Type: GrantFiled: February 14, 2006Date of Patent: January 20, 2015Assignee: Abbvie B.V.Inventors: Josephus H. M. Lange, Herman H. Van Stuivenberg, Bernard J. Van Vliet
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Publication number: 20150010504Abstract: Disclosed are compounds of formula (I) for use as antiviral agents, particularly as anti-hepatitis virus C agents, wherein A, B, U, R1-R7, m, n, and q are as described herein. Also disclosed are pharmaceutical compositions and methods of treating or preventing viral infection in a host by the use of these compounds, either alone or in combination with other pharmaceutically active agents. Further disclosed are methods of preparing such compounds.Type: ApplicationFiled: February 9, 2013Publication date: January 8, 2015Applicant: Lupin LimitedInventors: Vidya Ramdas, Advait Arun Joshi, Moloy Manoj Banerjee, Amit Kumar Das, Deepak Sahebrao Walke, Venkata P. Palle, Rajender Kumar Kamboj
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Publication number: 20150010505Abstract: Disclosed are compounds of formula (I) for use as antiviral agents, particularly as anti-hepatitis virus C agents, wherein R-R 6 and q are as described herein. Also disclosed are pharmaceutical compositions and methods of treating or preventing viral infection in a host by the use of these compounds, either alone or in combination with other pharmaceutically active agents. Further disclosed are methods of preparing such compounds. (I).Type: ApplicationFiled: February 8, 2013Publication date: January 8, 2015Applicant: LUPIN LIMITEDInventors: Vidya Ramdas, Advait Arun Joshi, Moloy Manoj Banerjee, Amit Kumar Das, Deepak Sahebrao Walke, Venkata P. Palle, Rajender Kumar Kamboj
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Publication number: 20140364429Abstract: Provided are compounds antiviral compounds represented by formula Ia and Ib: that are highly potent as HCV NS5A inhibitors, where the structural variables are as defined herein. These compounds are useful in, for example, inhibiting Hepatitis C virus and treating Hepatitis C virus infections.Type: ApplicationFiled: June 6, 2014Publication date: December 11, 2014Applicant: AB PHARMA LTD.Inventor: Zheng-Yun James ZHAN
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Publication number: 20140350010Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: ApplicationFiled: November 28, 2012Publication date: November 27, 2014Applicant: NOVARTIS AGInventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
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Patent number: 8889726Abstract: Disclosed are compounds of Formula I, Formula II, and Formula III. Also disclosed are salts of the compounds, pharmaceutical composition comprising the compounds or salts, and methods for treating HCV infection by administration of the compounds or salts.Type: GrantFiled: August 6, 2012Date of Patent: November 18, 2014Assignee: GlaxoSmithKline LLCInventors: Subramanian Baskaran, Richard Martin Grimes, Wieslaw Mieczyslaw Kazmierski, Martin Robert Leivers
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Patent number: 8865709Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.Type: GrantFiled: September 24, 2013Date of Patent: October 21, 2014Assignee: Neosome Life Sciences, LLCInventors: Laxman S. Desai, Srinivas Chittaboina
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Patent number: 8859529Abstract: This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: GrantFiled: September 22, 2009Date of Patent: October 14, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Ling Tong, Michael K. C. Wong, Brian J. Lavey, Joseph A. Kozlowski, Lei Chen, Razia K. Rizvi, Aneta Maria Kosinski, De-Yi Yang, Guowei Zhou, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
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Patent number: 8841278Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: October 3, 2013Date of Patent: September 23, 2014Assignee: Gilead Pharmasset LLCInventors: Elizabeth M. Bacon, Eda Canales, Aesop Cho, Jeromy J. Cottell, Manoj C. Desai, Michael Graupe, Hongyan Guo, Randall L. Halcomb, Darryl Kato, Choung U. Kim, Thorsten A. Kirschberg, Evan S. Krygowski, Scott E. Lazerwith, John O. Link, Hongtao Liu, Qi Liu, Richard L. Mackman, Michael L. Mitchell, Jay P. Parrish, Hyung-Jung Pyun, Joseph H. Saugier, Scott D. Schroeder, Jianyu Sun, James G. Taylor, James D. Trenkle, Winston C. Tse, Randall W. Vivian, William J. Watkins, Lianhong Xu
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Patent number: 8822430Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: July 31, 2013Date of Patent: September 2, 2014Assignee: Gilead Pharmasset LLCInventors: Elizabeth M. Bacon, Eda Canales, Aesop Cho, Jeromy J. Cottell, Manoj C. Desai, Michael Graupe, Hongyan Guo, Randall L. Halcomb, Darryl Kato, Choung U. Kim, Thorsten A. Kirschberg, Evan S. Krygowski, Scott E. Lazerwith, John O. Link, Hongtao Liu, Qi Liu, Richard L. Mackman, Michael L. Mitchell, Jay P. Parrish, Hyung-Jung Pyun, Joseph H. Saugier, Scott D. Schroeder, Jianyu Sun, James G. Taylor, James D. Trenkle, Winston C. Tse, Randall W. Vivian, William J. Watkins, Lianhong Xu
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Patent number: 8822449Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula (I) and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.Type: GrantFiled: August 25, 2009Date of Patent: September 2, 2014Assignee: SanofiInventors: Nils Rackelmann, Laurent Bialy, Heinrich Englert, Klaus Wirth, Petra Arndt, John Weston, Uwe Heinelt, Markus Follmann
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Patent number: 8815924Abstract: Novel heterocyclic compounds of the formula (I), in which R1, D, W, T and T? have the meanings indicated in Claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and conditions, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in fibroses and inflammatory processes of any type.Type: GrantFiled: April 4, 2005Date of Patent: August 26, 2014Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Rolf Gericke, Werner Mederski, Norbert Beier, Florian Lang
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Publication number: 20140221421Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.Type: ApplicationFiled: January 9, 2014Publication date: August 7, 2014Applicant: GILEAD SCIENCES, INC.Inventors: Steven S. BONDY, Carina E. CANNIZZARO, Chien-Hung CHOU, John O. LINK, Qi LIU, Scott D. SCHROEDER, Winston C. TSE, Jennifer R. ZHANG
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Publication number: 20140199264Abstract: The present invention relates to novel Tetracyclic Xanthene Derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, Y1, Y2, Z, Ra, Rb, R1a, R1b and R2 are as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Xanthene Derivative, and methods of using the Tetracyclic Xanthene Derivatives for treating or preventing HCV infection in a patient.Type: ApplicationFiled: March 16, 2012Publication date: July 17, 2014Inventors: Craig A. Coburn, Stuart B. Rosenblum, Joseph A. Kozlowski, Richard Soll, Hao Wu, Bin Hu, Bin Zhong, Dahai Wang, Changmao Shen, Fei Sun
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Patent number: 8772508Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers, stereoisomers and polymorphs thereof, wherein A, B and R1 are as defined throughout the description and the claims.Type: GrantFiled: April 18, 2008Date of Patent: July 8, 2014Assignee: Probiodrug AGInventors: Mirko Buchholz, Ulrich Heiser, Antje Hamann
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Publication number: 20140171476Abstract: Disclosed are compounds of Formula I, Formula II, and Formula III. Also disclosed are salts of the compounds, pharmaceutical composition comprising the compounds or salts, and methods for treating HCV infection by administration of the compounds or salts.Type: ApplicationFiled: August 6, 2012Publication date: June 19, 2014Applicant: GlaxoSmith Kline LLCInventors: Subramanian Baskaran, Richard Martin Grimes, Wieslaw Mieczyslaw Kazmierski, Martin Robert Leivers
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Publication number: 20140170111Abstract: The present invention relates to novel Fused Tetracycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A?, B, G, R1, U, V, W, W?, X, X?, Y and Y? are as defined herein. The present invention also relates to compositions comprising at least one Fused Tetracycle Derivative, and methods of using the Fused Tetracycle Derivatives for treating or preventing HCV infection in a patient.Type: ApplicationFiled: September 28, 2011Publication date: June 19, 2014Applicant: Merck Sharp & Dohmn Corp.Inventors: Craig A. Coburn, Brian J. Lavey, Michael P. Dwyer, Joseph A. Kozlowski, Stuart B. Rosenblum
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Publication number: 20140142307Abstract: Singly and multiply charged imidazolium cations (ICs) have been identified as a class of chemical compositions that possess potent antineoplastic, antibacterial and antimicrobial properties. The imidazolium cations disclosed demonstrate greater or equivalent potency towards cancerous cells as the current clinical standard, cisplatin. These imidazolium cations, however, achieve this efficacy without any of the known toxic side effects caused by heavy metal-based antineoplastic drugs such as cisplati.Type: ApplicationFiled: April 30, 2012Publication date: May 22, 2014Inventors: Wiley Youngs, Matthew Panzner, Claire Tessier, Michael Deblock, Brian Wright, Patrick Wagers, Nikki Robishaw
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Patent number: 8716492Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.Type: GrantFiled: December 15, 2011Date of Patent: May 6, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Jon J. Hangeland, Mimi L. Quan, Joanne M. Smallheer, Gregory S. Bisacchi, James R. Corte, Todd J. Friends, Zhong Sun, Karen A. Rossi, Cullen L. Cavallaro
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Publication number: 20140081028Abstract: The purpose of the present invention is to provide an organic semiconductor material having liquid crystallinity and high electron mobility. The present invention is an organic semiconductor material having at least a charge-transporting molecular unit (A) having a structure of an aromatic fused ring system and a cyclic structural unit (B) bonded to the aforementioned unit via a single bond, wherein the unit (A) and/or the unit (B) has a side chain composed of a unit (C), and wherein the organic semiconductor material exhibits a liquid crystal phase that is different from an N-phase, an SmA-phase or an SmC-phase.Type: ApplicationFiled: March 9, 2012Publication date: March 20, 2014Inventors: Junichi Hanna, Takeo Kobori, Takayuki Usui, Yukiko Takayashiki, Hiroaki Iino, Akira Oono
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Patent number: 8669234Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: June 7, 2012Date of Patent: March 11, 2014Assignee: Gilead Sciences, Inc.Inventors: Hongyan Guo, Darryl Kato, Thorsten A. Kirschberg, Evan S. Krygowski, John O. Link, Michael L. Mitchell, Jay P. Parrish, James Taylor
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Publication number: 20140051660Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, Q, and G are defined herein.Type: ApplicationFiled: August 16, 2013Publication date: February 20, 2014Applicant: Janssen Pharmaceutica NVInventors: Michael WINTERS, Zhihua Sui, Christopher Flores
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Publication number: 20130345275Abstract: Compounds of formula I and a method for their preparation are described: where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R4 signifies -alkyl-aryl or -alkyl-heteroaryl; X signifies CH2, oxygen atom or sulphur atom; n is 2 or 3; including the individual (R)- and (S)-enantiomers or mixtures of enantiomers thereof; and including pharmaceutically acceptable salts and esters thereof. The compounds have potentially valuable pharmaceutical properties for the treatment of cardiovascular disorders such as hypertension and chronic heart failure.Type: ApplicationFiled: June 13, 2013Publication date: December 26, 2013Inventors: Patricio Manuel Vieira Araujo Soares Da Silva, David Alexander Learmonth, Alexander Beliaev
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Publication number: 20130320262Abstract: The present invention relates to a compound of a formula (I), (II) or (III), to the use of this compound in an electronic device, and to an electronic device comprising one or more compounds of the formula (I), (II) or (III). The invention furthermore relates to a process for the preparation of a compound of the formula (I), (II) or (III) and to a formulation comprising one or more compounds of the formula (I), (II) or (III).Type: ApplicationFiled: January 18, 2012Publication date: December 5, 2013Applicant: MERCK PATENT GMBHInventors: Irina Martynova, Amir Hossain Parham, Christof Pflumm
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Publication number: 20130289072Abstract: The present invention relates to provision of a novel indazole compound which is capable of inhibiting HSP90 and shows a cytostatic effect on cancer cells. The present invention also relates to provision of a drug useful for preventing and/or treating, on the basis of an HSP90 inhibitory effect, a disease in which HSP90 participates, in particular, cancer. A compound represented by the general formula (I) or a salt thereof: wherein X represents CH or N; any one or two of Y1, Y2, Y3, and Y4 represent C—R3 or N, and the others represent CH; A and B are the same or different and represent an optionally substituted monocyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S, and O; R1 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.; R2 represents a hydrogen atom, a halogen atom etc.; R3 represents a hydrogen atom, a halogen atom etc.; R4 and R5 are the same or different and represent a hydroxyl group etc.Type: ApplicationFiled: January 6, 2012Publication date: October 31, 2013Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Makoto Kitade, Shuichi Ohkubo, Chihoko Yoshimura
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Patent number: 8551992Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.Type: GrantFiled: May 23, 2012Date of Patent: October 8, 2013Assignee: Neosome Life Sciences, LLCInventors: Laxman S. Desai, Srinivas Chittaboina
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Patent number: 8546389Abstract: The present invention relates to viral polymerase inhibitors of formula (I), salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections:Type: GrantFiled: October 20, 2011Date of Patent: October 1, 2013Assignee: Biota Scientific Management Pty Ltd.Inventors: Rosliana Halim, Michael Harding, Richard Hufton, Craig James Morton, Saba Jahangiri, Brett Raymond Pool, Tyrone Pieter Jeynes, Alistair George Draffan, Barbara Frey, Michael John Lilly
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Patent number: 8541453Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: May 20, 2011Date of Patent: September 24, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Matthew Hamilton
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Publication number: 20130245015Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: ApplicationFiled: May 3, 2013Publication date: September 19, 2013Inventors: YUJIA DAI, STEVEN K. DAVIDSEN, ANNA M. ERICSSON, KRESNA HARTANDI, ZHIQIN JI, MICHAEL R. MICHAELIDES
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Patent number: 8487113Abstract: The invention deals with a preparation method of salts of 5-chloro-4-(2-imidazolin-2-yl-amino)-2,1,3-benzothiadiazole (tizanidine) of formula I, especially tizanidine hydrochloride, comprising preparation of a salt of tizanidine of formula I and a carboxylic acid as an intermediate, from which, after acidification with hydrogen chloride, tizanidine hydrochloride is obtained in a high yield and purity.Type: GrantFiled: December 18, 2009Date of Patent: July 16, 2013Assignee: Farmak, A.S.Inventors: Pavel Hradil, Lubomir Kvapil, Martin Grepl, Jan Novotny
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Patent number: 8455497Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: February 12, 2009Date of Patent: June 4, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill
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Publication number: 20130116240Abstract: Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.Type: ApplicationFiled: September 26, 2012Publication date: May 9, 2013Applicant: JAPAN TOBACCO INC.Inventor: Japan Tobacco Inc.
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Patent number: 8436023Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, X, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: GrantFiled: June 9, 2011Date of Patent: May 7, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Xuqing Zhang, Zhihua Sui, James C. Lanter
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Publication number: 20130102629Abstract: Compounds represented by formula (I) or pharmaceutically acceptable salts thereof, wherein A, B, B?, X, Y, R1, R2, R2?, R3, R3?, R4, R4?, R5, R5?, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: September 24, 2012Publication date: April 25, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
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Patent number: 8426590Abstract: The present invention relates to a process for the preparation of doxazosin or salts thereof.Type: GrantFiled: March 23, 2010Date of Patent: April 23, 2013Assignee: Cipla LimitedInventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Dilip Ramdas Birari
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Publication number: 20130029981Abstract: The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2-a]pyrimidinium salts precursors being active against biofilm formation. The invention also relates to imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent, and to substituted 2-aminoimidazoles wherein the amino group bears a terminal heterocyclic group such as a triazolyl group which are formed through azide-alkyne Huisgen cycloaddition starting from said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to a class of N-(azidoalkyl)pyrimidin-2-amines useful as starting materials for the synthesis of said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to antimicrobial compositions that include a microbial biofilm formation inhibiting amount of such substituted 2-aminoimidazoles or imidazo[1,2-a]pyrimidinium salts in combination with excipients.Type: ApplicationFiled: June 18, 2012Publication date: January 31, 2013Applicant: Katholieke Universiteit LeuvenInventors: Sigrid De Keersmaecker, Dirk De Vos, Denis Ermolatev, Hans Steenackers, Erik Van Der Eycken, Jozef Vanderleyden, Bharat S. Savaliya
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Publication number: 20130029970Abstract: The present disclosure relates to compounds of formula I useful as agonists of cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: July 9, 2010Publication date: January 31, 2013Applicant: IRONWOOD PHARMACEUTICALS, INCInventors: Kevin Sprott, Jason Rohde, Takashi Nakai, Bo Peng, John Jeffrey Talley
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Patent number: 8362068Abstract: Provided herein are 5,5-fused heteroarylene hepatitis C virus inhibitor compounds, for example, of Formula I, IA, or IB, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.Type: GrantFiled: December 17, 2010Date of Patent: January 29, 2013Assignee: Idenix Pharmaceuticals, Inc.Inventors: Cyril B. Dousson, David Dukhan, Christophe Claude Parsy, Claire Pierra, Francois-Rene Alexandre, Guillaume Brandt, Daniel Da Costa, Houcine Rahali, Jean-Laurent Paparin, Michel Derock, Thierry Convard, Dominique Surleraux
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Publication number: 20120302563Abstract: Described herein are substituted norindenoisoquinoline compounds, and pharmaceutical compositions and formulations comprising the norindenoisoquinoline compounds. Also described herein are methods for using the compounds for the treatment and/or prevention of topoisomerase mediated diseases, such as cancer.Type: ApplicationFiled: January 27, 2011Publication date: November 29, 2012Applicant: PURDUE RESEARCH FOUNDATIONInventors: Mark S. Cushman, Yunlong Song
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Patent number: 8299048Abstract: The present invention is directed to hexahydrocyclopentylf]indazole carboxamides and derivatives thereof as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: February 24, 2009Date of Patent: October 30, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: William P. Dankulich, Mildred L. Kaufman, Danielle M. McMaster, Robert S. Meissner, Helen J. Mitchell
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Publication number: 20120270853Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: ApplicationFiled: July 3, 2012Publication date: October 25, 2012Inventors: Donald J.P. Pinto, Joanne M. Smallheer, James R. Corte, Zilun Hu, Cullen L. Cavallaro, Paul J. Gilligan, Mimi L. Quan, Leon M. Smith
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Publication number: 20120264711Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: June 7, 2012Publication date: October 18, 2012Applicant: GILEAD SCIENCES, INC.Inventors: Hongyan Guo, Darryl Kato, Thorsten A. Kirschberg, Hongtao Liu, John O. Link, Michael L. Mitchell, Jay P. Parrish, Jianyu Sun, James Taylor, Elizabeth M. Bacon, Eda Canales, Aesop Cho, Choung U. Kim, Jeromy J. Cottell, Manoj C. Desai, Randall L. Halcomb, Michael Graupe, Evan S. Krygowski, Scott E. Lazerwith, Qi Liu, Richard L. Mackman, Hyung-Jung Pyun, Joseph H. Saugier, James D. Trenkle, Winston C. Tse, Randall W. Vivian, Scott D. Schroeder, William J. Watkins, Lianhong Xu
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Publication number: 20120251491Abstract: The present invention relates to novel Fused Tricyclic Aryl Compounds, compositions comprising at least one Fused Tricyclic Aryl Compound, and methods of using the Fused Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient.Type: ApplicationFiled: May 12, 2010Publication date: October 4, 2012Inventors: Stuart B. Rosenblum, Kevin X. Chen, Joseph A. Kozlowski, F. George Njoroge, Craig A. Coburn
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Patent number: 8273269Abstract: A composition, for producing dispersions, thermoplastic masses and/or color filters, comprising (a) a colorant of formula (1) wherein 20-100 mol % R1 are Br and 80-100 mol % R3 are H, especially of formula (Ib) and/or (Ic); (b) from 0 to 150% by weight, based on (a), of C. I. Pigment Red 144, 188, 190, 224, 242 or 2,4,6-trimethylphenylperylene diimide; (c) from 3 to 25% by weight, based on (a), of a di- or tri-azacyclopentylmethyl-substituted colorant (formulae given); (d) from 0 to 10% by weight, preferably from 0.01 to 8% by weight, based on the sum of (a) and (b), of an additionally sulfonated colorant of the same kernels as in (c); and (e) from 0 to 30% by weight, preferably from 3 to 25% by weight, especially from 5 to 20% by weight, based on (a), of a diketopyrrolopyrrole colorant substituted by at least one chain containing a plurality of nitrogen atoms (cf. formula (V)).Type: GrantFiled: May 5, 2009Date of Patent: September 25, 2012Assignee: BASF SEInventors: Roman Lenz, Gerardus De Keyzer, Mathias Duggeli, Patrick Christopher Holzhuter
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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