Unsaturated Carbocyclic Ring Attached Directly To The Quinoline Ring System By Nonionic Bonding (e.g., Quinophthalones, Etc.) Patents (Class 546/173)
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Publication number: 20140107097Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.Type: ApplicationFiled: October 15, 2013Publication date: April 17, 2014Applicant: Janssen Pharmaceutica NVInventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Taraneh Mirzadegan, Kelly Ganamet
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Publication number: 20140100213Abstract: This invention relates to the use of triazolone 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 triazolones in the treatment of cancer.Type: ApplicationFiled: November 4, 2013Publication date: April 10, 2014Applicant: GlaxoSmithKline LLCInventors: Nicholas David Adams, Christopher Joseph Aquino, Amita M. Chaudhari, Jonathan Michael Chergurovich, Terence John Kiesow, Cynthia Ann Parrish, Alexander Joseph Reif, Kenneth Wiggall
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Publication number: 20140094610Abstract: The present invention is directed to an improved process for the preparation of Compounds of Formula (I) or salts thereof which are useful in the treatment of HIV infection. In particular, the present invention is directed to an improved process for the preparation of (2S)-2-tert-butoxy-2-(4-(2,3-dihydropyrano[4,3,2-de]quinolin-7-yl)-2-methylquinolin-3-yl)acetic acid or salt thereof which is useful in the treatment of HIV infection.Type: ApplicationFiled: October 3, 2013Publication date: April 3, 2014Inventors: Wenjie LI, Philomen DECROOS, Keith R. FANDRICK, Joe Ju GAO, Nizar HADDAD, Zhi-Hui LU, Bo QU, Sonia RODRIGUEZ, Chris H. SENANAYAKE, Yongda ZHANG, Wenjun TANG
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Publication number: 20140094609Abstract: The present invention is directed to an improved process for the preparation of Compounds of Formula (I), which are useful in the treatment of HIV infection. In particular, the present invention is directed to an improved process for the preparation of (2S)-2-tert-butoxy-2-(4-(2,3-dihydropyrano[4,3,2-de]quinolin-7-yl)-2-methylquinolin-3-yl)acetic acid, which is useful in the treatment of HIV infection.Type: ApplicationFiled: October 2, 2013Publication date: April 3, 2014Inventors: Brandon H. Brown, Xiang Wang, Keith R. Fandrick, Joe Ju Gao, Nizar Haddad, Serge R. Landry, Wenjie Li, Zhi-Hui Lu, Bo Qu, Diana C. Reeves, Carl Thibeault, Yongda Zhang
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Publication number: 20140061601Abstract: An anthracene compound and organic light emitting diode including the same are disclosed. The organic light emitting diode includes, at least two stacks formed between a first electrode and a second electrode and a charge generation layer (CGL) including an N-type CGL and a P-type CGL formed between the stacks, wherein the N-type CGL is formed of the anthracene compound.Type: ApplicationFiled: December 26, 2012Publication date: March 6, 2014Applicant: LG DISPLAY CO., LTD.Inventors: Hyoseok KIM, Jeongdae SEO, Eunju JEON, Shinhan KIM
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Publication number: 20140061600Abstract: A pyrene compound and an organic light emitting diode device including the same are disclosed. The organic light emitting diode device includes at least two stacks provided between a first electrode and a second electrode, and a charge generation layer provided between the stacks and including an N type charge generation layer and a P type charge generation layer, wherein the N type charge generation layer is made of the pyrene compound.Type: ApplicationFiled: December 21, 2012Publication date: March 6, 2014Applicant: LG DISPLAY CO., LTD.Inventors: Shinhan Kim, Jeongdae Seo, Hyoseok kim, Youngkwan Jung, Eunju Jeon
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Patent number: 8664399Abstract: The present invention relates to sodium channel inhibitors of Formula (I): in which R1, R2, R3, R4, R5, X, Y, and Z are as defined herein, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: December 6, 2012Date of Patent: March 4, 2014Assignee: Gilead Sciences, Inc.Inventors: Matthew Abelman, Robert H. Jiang, Jeff Zablocki
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Publication number: 20140058109Abstract: A method for producing a drug substance of crystalline pitavastatin calcium excellent in stability, is presented. In the production of a compound (pitavastatin calcium) represented by the formula (1): The water content is adjusted to a level of from 5 to 15%, and the crystal form is controlled to be crystal form A, thereby to obtain a drug substance excellent in stability.Type: ApplicationFiled: October 30, 2013Publication date: February 27, 2014Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Yoshio OHARA, Yasutaka Takada, Hiroo Matsumoto, Akihiro Yoshida
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Publication number: 20140051854Abstract: The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.Type: ApplicationFiled: July 25, 2011Publication date: February 20, 2014Applicant: LEK PHARMACEUTICALS D.D.Inventors: Zdenko Casar, Damjan Sterk, Marko Jukic
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Publication number: 20140045825Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.Type: ApplicationFiled: September 14, 2011Publication date: February 13, 2014Applicant: Exelixis, Inc.Inventor: James William Leahy
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Publication number: 20140034913Abstract: A condensation compound is represented by Formula 1, 2, or 3 where R1 to R24 and A to F are further defined in the detailed description.Type: ApplicationFiled: January 8, 2013Publication date: February 6, 2014Inventors: So-Yeon KIM, Yoon-Hyun KWAK, Bum-Woo PARK, Jong-Won CHOI, Wha-II CHOI, Sun-Young LEE, Ji-Youn LEE, Jin-Young YUN
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Publication number: 20140031335Abstract: The present invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same. The compounds of the present invention show the effect of CETP activity inhibition. It means that the compounds can increase HDL-cholesterol and decrease LDL-cholesterol.Type: ApplicationFiled: April 12, 2012Publication date: January 30, 2014Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.Inventors: SeoHee Lee, Jung Taek Oh, JaeKwang Lee, JaeWon Lee, Suyeal Bae, Nina Ha, Sera Lee
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Publication number: 20140031545Abstract: Processes for making an organozinc reagents are disclosed comprising reacting (A) organomagnesium or organozinc complexes with (B) at least one coordination compound comprising one or more carboxylate groups and/or alcoholate groups and/or tertiary amine groups, optionally in combination with zinc ions and/or lithium ions and/or halide ions, wherein the halide ions are selected from chloride, bromide and iodide, the organozinc complex comprises an aryl group, a heteroaryl group or a benzyl group when the coordinating compound is a chelating polyamine, and the reaction is conducted in the presence of zinc complexed with at least one coordinating compound when reactant (A) comprises at least one organomagnesium complex. The resulting organozinc reagents may optionally be isolated from solvents to obtain a solid reagent. The reagents may be used for making organic compounds via Negishi cross-coupling reactions or via aldehyde and/or ketone oxidative addition reactions.Type: ApplicationFiled: December 21, 2011Publication date: January 30, 2014Applicant: LUDWIG-MAXIMILIAN-UNIVERSITAT MUNCHENInventors: Paul Knochel, Sebastian Bernhardt, Georg Manolikakes
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Patent number: 8633320Abstract: Disclosed are methods for the preparation of bromo-substituted quinolines of the formula (I) where R is aryl, heteroaryl, alkyl, alkenyl or alkynyl, which are useful as intermediates in the preparation of agents for the treatment of hepatitis C viral (HCV) infections: Formula (I).Type: GrantFiled: May 3, 2010Date of Patent: January 21, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Nitinchandra D. Patel, Chris H. Senanayake, Wenjun Tang, Xudong Wei, Nathan K. Yee
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Publication number: 20140014925Abstract: A compound represented by Formula 1 below and an organic light-emitting device including the compound are provided: Substituents in Formula 1 are the same as defined in the specification.Type: ApplicationFiled: June 21, 2013Publication date: January 16, 2014Inventors: Hye-Jin Jung, Seok-Hwan Hwang, Young-Kook Kim, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim, Jun-Ha Park, Eun-Young Lee, Chang-Ho Lee, Jong-Hyuk Lee
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Patent number: 8628863Abstract: Provided is an organic light-emitting device having an optical output with high luminance and high color purity with extremely high efficiency. The organic light-emitting device includes an organic layer between the anode and the cathode, in which one of the anode and the cathode is a transparent electrode or a semi-transparent electrode and at least one layer of the organic layer contains at least one kind of indenopyrene compound having a specific structure.Type: GrantFiled: November 6, 2009Date of Patent: January 14, 2014Assignee: Canon Kabushiki KaishaInventors: Takeshi Sekiguchi, Hiroshi Tanabe, Hiroki Ohrui, Masanori Seki
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Publication number: 20140012004Abstract: The invention relates to palladium(0) tris{tri-[3,5-bis(trifluoromethyl)-phenyl]-phosphine} complex of formula (I), as well as to its preparation and use. This compound is outstandingly stable, and can be used as catalyst with excellent results.Type: ApplicationFiled: December 13, 2011Publication date: January 9, 2014Applicant: H4SEP KFTInventors: Zoltán Daliczek, Tibor Soós, Zoltán Finta, Géza Timári, Gábor Vlád
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Publication number: 20140005402Abstract: The present invention is directed to new crystalline forms of Pitavastatin hemicalcium salt, referred to hereinafter as polymorphic Forms A, B, C, D, E and F, as well as the amorphous form. Furthermore, the present invention is directed to processes for the preparation of these crystalline forms and the amorphous form and pharmaceutical compositions comprising these crystalline forms or the amorphous forms.Type: ApplicationFiled: September 3, 2013Publication date: January 2, 2014Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Paul Adriaan VAN DER SCHAAF, Fritz Blatter, Martin Szelagiewicz, Kai-Uwe Schoening
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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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Patent number: 8586739Abstract: Substituted bicyclic heteroaryls having the general structure: and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity.Type: GrantFiled: May 10, 2012Date of Patent: November 19, 2013Assignee: Amgen Inc.Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian S. Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer L. Seganish, Youngsook Shin, Dawei Zhang
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Publication number: 20130302248Abstract: Imaging agents of formula (I) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formula (I) capable of binding to tau proteins and ?-amyloid peptides are presented herein. The invention also relates to methods of imaging A? and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formula (I) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.Type: ApplicationFiled: June 25, 2013Publication date: November 14, 2013Inventors: Umesh B. Gangadharmath, Hartmuth C. Kolb, Peter J.H. Scott, Joseph C. Walsh, Wei Zhang, Anna Katrin Szardenings, Anjana Sinha, Gang Chen, Eric Wang, Vani P. Mocharla, Chul Yu, Changhui Liu, Daniel Kurt Cashion, Dhanalakshmi Kasi
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Publication number: 20130303568Abstract: The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, anxiety, or manic depression, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.Type: ApplicationFiled: April 22, 2013Publication date: November 14, 2013Inventors: Nancy C. LAN, Yan Wang, Sui Xiong Cai
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Publication number: 20130285021Abstract: Charge transport compounds are provided. The compounds are useful in optoelectronic devices that include the compounds incorporated as a charge-transport layer. Methods for forming films of the compounds are also provided. Additionally, methods are provided for forming films of a charge-transport layer on an active layer of an optoelectronic device. The films are formed from a solution with solubility orthogonal to the solubility of the active layer, such that the active layer is not solvated during deposition of the charge-transport layer.Type: ApplicationFiled: February 14, 2013Publication date: October 31, 2013Applicant: University of Washington through its Center for CommercializationInventor: University of Washington through its Center for Commercialization
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Publication number: 20130261123Abstract: The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.Type: ApplicationFiled: December 16, 2011Publication date: October 3, 2013Inventors: Xicheng Sun, Jian Qiu, Adam Stout
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Patent number: 8546392Abstract: The invention relates to the use of non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment and prophylaxis of hormone-dependent, particularly estrogen-dependent, diseases. The invention further relates to suitable inhibitors and to a method for the production thereof.Type: GrantFiled: March 27, 2008Date of Patent: October 1, 2013Assignee: Universitaet des SaarlandesInventors: Rolf Hartmann, Martin Frotscher, Sandrine Oberwinkler, Erika Ziegler, Josef Messinger, Heinrich-Hubert Thole
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Publication number: 20130236395Abstract: Heterocyclic compounds of formula (I) useful as imaging probes of Tau pathology in Alzheimer's disease are described. Compositions and methods of making such compounds are also described.Type: ApplicationFiled: November 7, 2011Publication date: September 12, 2013Applicant: GE HEALTHCARE LIMITEDInventors: Clare Jones, Amanda Ewan, Duncan Wynn, Alessandra Gaeta, James Nairne
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Publication number: 20130237563Abstract: The present invention provides a solid of pitavastatin tert-butyl ester and process for its preparation. The present invention also provides a novel crystalline form of pitavastatin calcium, process for its preparation and pharmaceutical compositions comprising it.Type: ApplicationFiled: August 23, 2011Publication date: September 12, 2013Applicant: HETERO RESEARCH FOUNDATIONInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Samala Malla Reddy, Bandi Vamsi Krishna
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Publication number: 20130217671Abstract: The present invention directs a compound represented by formula (I).Type: ApplicationFiled: July 28, 2011Publication date: August 22, 2013Inventors: Yo Matsuo, Shoji Hisada, Yusuke Nakamura, Feryan Ahmed, Raymond Huntley, Joel R. Walker, Helene Decomez
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Publication number: 20130210801Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides 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 the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I).Type: ApplicationFiled: July 1, 2011Publication date: August 15, 2013Applicant: GILEAD SCIENCES, INC.Inventors: Kerim Babaoglu, Kyla Bjornson, Hongyan Guo, Randall L. Halcomb, John O. Link, Hongtao Liu, Michael L. Mitchell, Jianyu Sun, James Taylor, Randall W. Vivian, Lianhong Xu
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Patent number: 8507685Abstract: The present invention relates to novel phenyl bicyclic methyl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: April 13, 2012Date of Patent: August 13, 2013Assignee: Allergan, Inc.Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im
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Publication number: 20130204000Abstract: A method for producing a drug substance of crystalline pitavastatin calcium excellent in stability, is presented. In the production of a compound (pitavastatin calcium) represented by the formula (1): The water content is adjusted to a level of from 5 to 15%, and the crystal form is controlled to be crystal form A, thereby to obtain a drug substance excellent in stability.Type: ApplicationFiled: March 15, 2013Publication date: August 8, 2013Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventor: NISSAN CHEMICAL INDUSTRIES, LTD.
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Publication number: 20130203756Abstract: The present invention is directed to isoindolinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: ApplicationFiled: October 24, 2011Publication date: August 8, 2013Inventors: Jamie L. Bunda, Christopher D. Cox, Vadim Y. Dudkin, Hannah D. Fiji, Michael J. Kelly, Mark E. Layton, Joseph E. Pero, William D. Shipe, Justin T. Sheen
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Publication number: 20130203727Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides 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 the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I).Type: ApplicationFiled: July 1, 2011Publication date: August 8, 2013Applicant: GILEAD SCIENCES, INC.Inventors: Kerim Babaoglu, Elizabeth Bacon, Kyla Bjornson, Hongyan Guo, Randall L. Halcomb, Paul Hrvatin, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Paul Roethle, James Taylor, James D. Trenkle, Randall W. Vivian, Lianhong Xu
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Publication number: 20130197231Abstract: Compounds of formula I: wherein R4, R6 and R7 are defined herein, are useful as inhibitors of HIV replication.Type: ApplicationFiled: November 21, 2012Publication date: August 1, 2013Applicant: Gilead Sciences, Inc.Inventor: Gilead Sciences, Inc.
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Publication number: 20130196971Abstract: This invention relates to the use of imidazole, triazole, and tetrazole 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 imidazoles, triazoles, and tetrazoles in the treatment of cancer.Type: ApplicationFiled: September 15, 2011Publication date: August 1, 2013Inventors: Christopher Joseph Aquino, Dennis Heyer, Terence John Kiesow, David Lee Musso, Cynthia A. Parrish
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Publication number: 20130190491Abstract: Compounds of formula I: wherein c, R2, R3, R4, R5, R6, R7 and R8 are defined herein, are useful as inhibitors of HIV replication.Type: ApplicationFiled: January 11, 2013Publication date: July 25, 2013Applicant: Gilead Sciences, Inc.Inventor: Gilead Sciences, Inc.
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Publication number: 20130184460Abstract: The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.Type: ApplicationFiled: September 16, 2011Publication date: July 18, 2013Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Minoru Moriya, Akito Yasuhara, Kazunari Sakagami, Hiroshi Ohta, Kumi Abe, Shuji Yamamoto, Yuko Araki, Hiroki Urabe, Xiang-Min Sun
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Patent number: 8487105Abstract: Processes for preparing pravastatin, intermediates and pharmaceutically acceptable salts thereof are provided Crystalline forms of pravastatin, intermediates and pharmaceutically acceptable salts thereof are also disclosed.Type: GrantFiled: January 18, 2010Date of Patent: July 16, 2013Assignee: MSN Laboratories LimitedInventors: Manne Satyanarayana Reddy, Sajja Eswaraiah, Maramreddy Sahadeva Reddy
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Publication number: 20130178499Abstract: The present invention is directed to novel quinoline compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.Type: ApplicationFiled: October 7, 2011Publication date: July 11, 2013Applicant: N30 PHARMACEUTICALS, INC.Inventors: Xicheng Sun, Jian Qiu, Adam Stout
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Publication number: 20130143880Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is 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, such as schizophrenia.Type: ApplicationFiled: August 5, 2011Publication date: June 6, 2013Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
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Patent number: 8455516Abstract: A new series of HIV-1 fusion inhibitors and methods of use are disclosed. The compounds are based on a substituted indole, benzimidazole, indoline or isoindoline fragment. The compounds find use in inhibiting or preventing HIV fusion from occurring, thus inhibiting or preventing entry of viral RNA into host cells. The compounds may be useful towards other biological targets involving protein-protein interactions.Type: GrantFiled: January 14, 2011Date of Patent: June 4, 2013Assignee: Touro UniversityInventors: Miriam Gochin, Guangyan Zhou
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Publication number: 20130116243Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: December 23, 2010Publication date: May 9, 2013Applicant: ALMAC DISCOVERY LIMITEDInventors: Lixin Zhang, Graham Peter Trevitt, Hugues Miel, Frank Burkamp, Timothy Harrison, Andrew John Wilkinson, Charles-Henry Fabritius
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Publication number: 20130109713Abstract: The invention provides a compound of formula I:or a salt thereof, wherein R3-R8 and X and Y have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as antibacterial agents.Type: ApplicationFiled: June 24, 2011Publication date: May 2, 2013Inventors: Edmond J. Lavoie, Ajit Parhi, Daniel S. Pilch
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Publication number: 20130102632Abstract: The present invention relates to sodium channel inhibitors of Formula (I): in which R1, R2, R3, R4, R5, X, Y, and Z are as defined herein, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: December 6, 2012Publication date: April 25, 2013Applicant: Gilead Sciences, Inc.Inventor: Gilead Sciences, Inc.
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Publication number: 20130096101Abstract: Provided herein are compounds, pharmaceutical compositions, and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: December 4, 2012Publication date: April 18, 2013Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventor: PRESIDIO PHARMACEUTICALS, INC.
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Publication number: 20130096303Abstract: The present invention provides an improved process for preparing HMG-CoA reductase inhibitors such as rosuvastatin calcium, fluvastatin sodium, and pitavastatin calcium under a mild condition, using a novel amide-bond-containing compound having R2—N—O—R1 moiety as a key intermediate. And also, the present invention provides the novel compound, an intermediate useful for the preparation thereof, and a process for the preparation thereof.Type: ApplicationFiled: June 30, 2011Publication date: April 18, 2013Inventors: Hyun Ju, Sang-Sun Joung, Hyun-Jik Yi, Ja-Heouk Khoo, Jong-Chul Lim, Jae-Gyu Kim
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Publication number: 20130084346Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.Type: ApplicationFiled: February 28, 2011Publication date: April 4, 2013Inventors: Scott Wolkenberg, James C. Barrow, Michael S. Poslusney, Scott T. Harrison, B. Wesley Trotter, James Mulhearn, Kausik K. Nanda, Peter J. Manley, Zhijian Zhao, Jeffrey W. Schubert, Nathan Kett, Amy Zartman
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Publication number: 20130076604Abstract: Provided are a novel organic compound appropriate for emission of green light and an organic light-emitting device including the organic compound. Provided is a substituted or unsubstituted indeno[1,2,3-cd]naphtho[2,3-k]fluoranthene appropriate for emission of green light. The substituents of the indeno[1,2,3-cd]naphtho[2,3-k]fluoranthene are each independently selected from a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted amino group, a substituted or unsubstituted aryl group, and a substituted or unsubstituted heterocyclic group.Type: ApplicationFiled: May 26, 2011Publication date: March 28, 2013Applicant: CANON KABUSHIKI KAISHAInventors: Jun Kamatani, Naoki Yamada, Kengo Kishino, Akihito Saitoh
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Publication number: 20130072688Abstract: The present invention relates to a method for preparing (4R,6S)-(E)-6-[2-(2-cyclopropyl)-4-(4-fluorophenyl)quinolin-3-yl)-vinyl-2,2-dimethyl-1,3-dioxan-4-yl]acetic acid ester derivative, which is an intermediate of pitavastatin or of the salt thereof, into a crystalline solid form. In addition, the present invention relates to a novel solvate of the intermediate, and to a method for preparing pitavastatin or the salt thereof using the intermediate.Type: ApplicationFiled: March 11, 2011Publication date: March 21, 2013Applicant: H.L. GENOMICSInventors: Seo-Jin Lee, Hyun-Gyu Kim
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Publication number: 20130065897Abstract: The present invention provides novel compounds of the Formula I, pharmaceutical compositions comprising such compounds and methods for using such compounds as agents or drugs for inhibiting perforin activity and for treating a subject at risk of or susceptible to a disease or disorder, or having a disease or disorder associated with undesirable perforin activity.Type: ApplicationFiled: December 22, 2010Publication date: March 14, 2013Applicant: PETER MACCALLUM CANCER INSTITUTEInventors: Julie Ann Spicer, Kristiina Maria Huttunen, Dani Michelle Lyons, Joseph Albert Trapani, Mark John Smyth, William Alexander Denny