Polycyclo Ring System Having The Oxazole Ring As One Of The Cyclos Patents (Class 548/217)
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Publication number: 20110177055Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g.Type: ApplicationFiled: March 29, 2011Publication date: July 21, 2011Applicant: IRM LLCInventors: David C. Tully, Arnab K. Chatterjee, Hank Michael James Petrassi, Badry Bursulaya, Glen Spraggon
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Publication number: 20110178083Abstract: Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.Type: ApplicationFiled: July 9, 2009Publication date: July 21, 2011Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Patent number: 7982036Abstract: The present invention provides compounds of formula I wherein Ring A, Ring B, m, Rx, Ry, W and R1 are as defined herein, pharmaceutically acceptable salts and compositions thereof, and methods of using the same.Type: GrantFiled: October 17, 2008Date of Patent: July 19, 2011Assignee: Avila Therapeutics, Inc.Inventors: Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter, Richland W. Tester
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Patent number: 7981925Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: GrantFiled: August 26, 2009Date of Patent: July 19, 2011Assignee: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20110166130Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.Type: ApplicationFiled: June 12, 2009Publication date: July 7, 2011Applicant: BIONOMICS LIMITEDInventors: Andrew John Harvey, Bernard Luke Flynn, Jorgen Alvar Mould, Dharam Paul, Gurmit Singh Gill, Justin Anthony Ripper, Rachel Christine Cooke, Julia Stephanie Crossman, Jonathan Bayldon Baell, Nathan Wayne Kuchel, Rajinder Singh
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Publication number: 20110166297Abstract: Molecularly imprinted smart polymers (MISPs) are provided herein, as well as novel monomers for preparing MISPs, and processes for preparing MISPs. The MISPs can be used applications such as, for example, detecting/absorbing or isolating biological and non-biological agents. The MISPs described herein comprise responsive monomeric units which undergo a physico-chemical change (e.g., a bond formation or cleavage) in response to an external change, such that the MISP selectively binds to a target molecule and releases a bound target molecule in response to the external change.Type: ApplicationFiled: September 9, 2009Publication date: July 7, 2011Applicant: Sailo Nanotechnologies Ltd.Inventors: Flavio Grynszpan, Eran Partouche, Vladimir Shkoulev, Alex Aizikovich, Sharon Gazal, Rachel Nakash-Ozeri, Isaac Zigelboim
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Publication number: 20110152246Abstract: The embodiments provide compounds of the general Formulae I, II, III, IV, or V as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: December 16, 2010Publication date: June 23, 2011Applicant: InterMune, Inc.Inventors: Brad Buckman, John B. Nicholas, Vladimir Serebryany, Scott D. Seiwert
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Patent number: 7960544Abstract: Indoles that have activity as inhibitors of FAAH are described as are indoles and indole derivatives that have activity as inhibitors of DAO.Type: GrantFiled: December 18, 2006Date of Patent: June 14, 2011Assignee: Ironwood Pharmaceuticals, Inc.Inventors: Wilmin Bartolini, Brian M. Cali, Barbara Chen, Yueh-Tyng Chien, Mark G. Currie, G. Todd Milne, James Philip Pearson, John Jeffrey Talley, Jane Yang, Craig Zimmerman, Charles Kim, Kevin Sprott, Timothy Barden, Regina Lundigran, Ara Mermerian
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Publication number: 20110130381Abstract: Inhibitors of dihydroorotate dehydrogenase (DHODH) for the Plasmodium enzyme have been identified and characterized. The inhibitors have high specificity, submicromolar efficacy against cultured parasite strains, exhibit drug-like properties, and are not overtly cytotoxic.Type: ApplicationFiled: May 7, 2009Publication date: June 2, 2011Inventors: Cecilia Bastos, Michael L. Booker, Cassandra A. Celatka, Jon C. Clardy, Joseph Cortese, Vishal P. Patel, Renato Skerlj, Roger C. Wiegand, Dyann F. Wirth
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Patent number: 7951838Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, X and Z are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formula II, intermediates and processes useful for the preparation of compounds of Formulas I and II.Type: GrantFiled: August 20, 2010Date of Patent: May 31, 2011Assignee: Amgen Inc.Inventors: Daniel La, Patricia Lopez, Vinod F. Patel, Wenge Zhong
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Patent number: 7947719Abstract: The present invention relates to a novel group of compounds having antibiotic, antifungal and/or cytostatic properties, which are obtainable from myxobacteria, especially of the genus Sorangium, preferably Sorangium cellulosum.Type: GrantFiled: July 13, 2006Date of Patent: May 24, 2011Assignee: Hemholtz-Zentrum fur Infektionsforschung GmbHInventors: Herbert Irschik, Rolf Jansen, Florenz Sasse
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Patent number: 7947506Abstract: A hydroxyquinolone compound formulated as a fluorescent dye for protein detection, assay, quantitation, etc. The hydroxyquinolone compound may be modified, for example, by adding or removing sulfate groups, changing hydrocarbon chain lengths, etc. to result in more desirable properties such as enhanced binding to basic proteins, enhanced solubility, etc. The dye has enhanced sensitivity over commercially available protein stains, and may be used to stain proteins in solution, proteins separated on gels, proteins transferred to solid supports, etc. Methods of using the dyes are also disclosed.Type: GrantFiled: June 2, 2006Date of Patent: May 24, 2011Assignee: Pierce Biotechnology, Inc.Inventors: Brian David Wolf, Surbhi Desai, Peter T. Czerney, Frank G. Lehmann, Bernd G. Schweder, Matthias S. Wenzel
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Publication number: 20110111162Abstract: A novel indolium compound of general formula (I) and an optical recording material containing the indolium compound. In formula (I), ring A is a benzene ring, etc.; ring B is a 5- or 6-membered heterocyclic ring; R1 is a group of general formula (II), etc.; R2 is an organic group having 1 to 30 carbon atoms, etc.; Y1 is an alkyl group having 1 to 10 carbon atoms, etc.; Z1 and Z2 are each, e.g., an alkyl group having 1 to 8 carbon atoms optionally substituted with a halogen atom and optionally interrupted by —O—, etc.; a is an integer of 0 to 6; b is an integer of 0 to 5; Anq? is a q-valent anion; q is 1 or 2; and p is a number necessary to neutralize an electric charge.Type: ApplicationFiled: September 26, 2008Publication date: May 12, 2011Applicant: ADEKA CORPORATIONInventors: Toru Yano, Yohei Aoyama
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Patent number: 7939669Abstract: The present invention relates to a light emitting transition metal compound of Chemical Formula 1 and an organic electroluminescence device including the compound. In the Chemical Formula 1, M is selected from Ir, Pt, Rh, Re, and Os, m is 2 or 3, n is 0 or 1, the sum of m and n is 3, provided that the sum of m and n is 2 M is Pt. X is a N or P atom, and Y is S, O, or Se.Type: GrantFiled: January 8, 2007Date of Patent: May 10, 2011Assignees: Samsung Electronics Co., Ltd., Industry-University Cooperation Foundation, Hanyang UniversityInventors: Dong-Hack Suh, Jin-Sik Choi, Jin-Soo Lim, Song-Ho Kim, Chi-Hun Kim
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Patent number: 7939670Abstract: A compound of the formula (I), (II), (III) or (IV) wherein Z, A, B, C, R, R1, R2, Q, and n are as described herein.Type: GrantFiled: February 23, 2009Date of Patent: May 10, 2011Assignee: Purdue Pharma L.P.Inventors: Qun Sun, R. Richard Goehring, Donald Kyle, Zhengming Chen, Sam Victory, John Whitehead
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Patent number: 7939528Abstract: The present invention relates to novel compounds which are antagonist or inverse agonists at an opioid receptor. Such compounds are useful in the treatment of obesity and related diseases and/or conditions in mammals, particularly humans. Methods of making and using such compounds are also disclosed.Type: GrantFiled: October 12, 2006Date of Patent: May 10, 2011Assignee: GlaxoSmithKline LLCInventors: Kevin Karl Barvian, Jason Daniel Speake, David John Cowan, Andrew Lamont Larkin, Jerzy Ryszard Szewczyk
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Publication number: 20110105749Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: June 14, 2010Publication date: May 5, 2011Inventors: Weiwen YING, David James, Shijie Zhang, Teresa Przewloka, Junghyun Chae, Dinesh U. Chimmanamada, Chi-Wan Lee, Elena Kostik, Howard P. Ng, Kevin Foley, Zhenjian Du, James Barsoum
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Publication number: 20110105762Abstract: The present invention relates to certain compounds and to methods for the preparation of certain compounds that can be used in the fields of chemistry and medicine. Specifically, described herein are methods for the preparation of various compounds and intermediates, and the compounds and intermediates themselves. More specifically, described herein are methods for synthesizing Salinosporamide A and its analogs from a compound of formula (V).Type: ApplicationFiled: October 27, 2010Publication date: May 5, 2011Applicant: NEREUS PHARMACEUTICALS, INC.Inventors: Taotao Ling, Venkata Rami Reddy Macherla, Barbara Christine Potts, Rama Rao Manam, Katherine A. McArthur
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Patent number: 7935713Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: May 11, 2007Date of Patent: May 3, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Ronald M. Kim, Emma R. Parmee, Qiang Tan, Cangming Yang, Ashley Rouse Lins
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Patent number: 7935706Abstract: It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: wherein Z is N or CR1, A1 is a nitrogen-containing aromatic monocyclic group which is optionally substituted, a nitrogen-containing aromatic fused cyclic group which is optionally substituted etc., A2 is an aromatic hydrocarbon cyclic group or an aromatic heterocyclic group, each optionally having a substituent, R1, R2, Ra, Rb, Rc and Rd are each independently hydrogen, hydroxy, etc., w is 2 or 3, t is 1 or 2, X is —(CR3R4)m-, —CO(CR3R4)n-, —CONR5(CR3R4)n- etc., m is an integer of 1 to 4, n is an integer of 0 to 4, R3 and R4 are each independently hydrogen, halogen, hydroxy etc., and R5 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt, or a solvate thereof.Type: GrantFiled: February 21, 2007Date of Patent: May 3, 2011Assignee: Shionogi & Co., Ltd.Inventors: Moriyasu Masui, Makoto Adachi, Hidenori Mikamiyama, Akira Matsumura, Naoki Tsuno
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Publication number: 20110098479Abstract: The invention relates to a method for producing an azoline compound represented by the general formula (3): wherein R1 represents an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; R3, R4, R5 and R6 may be the same or different and each represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; two arbitrary groups selected from R3, R4, R5 and R6 may bond to each other to form a ring; and Z1 represents an oxygen atom, a sulfur atom or a selenium atom; comprising reacting a carboxylic acid or a carboxylic acid derivative represented by the general formula (1): R1CO2R2 ??(1) wherein RType: ApplicationFiled: December 29, 2010Publication date: April 28, 2011Inventors: KAZUSHI MASHIMA, Takashi Ohshima, Takanori Iwasaki, Hironori Maeda, Kenya Ishida
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Patent number: 7928105Abstract: Disclosed are compounds of the following formula: in which R1, R2, R5, R6, R7, R31, u, and X are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: GrantFiled: January 21, 2010Date of Patent: April 19, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Publication number: 20110086817Abstract: Embodiments herein provide compounds and methods of making and using such compounds for prevention and treatment of multidrug resistant bacteria. In particular, embodiments are directed to anti-bacterial agents from benzo[d]heterocyclic scaffolds for prevention and treatment of multidrug resistant bacteria.Type: ApplicationFiled: May 29, 2009Publication date: April 14, 2011Applicant: University of Notre Dame du LacInventors: Marvin J. Miller, Garrett C. Moraski
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Publication number: 20110070297Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with glucokinase that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.Type: ApplicationFiled: December 1, 2010Publication date: March 24, 2011Applicants: Takeda San Diego, Inc., Takeda Pharmaceutical Company LimitedInventors: Sheldon X. Cao, Jun Feng, Yasuhiro Imaeda, Stephen L. Gwaltney, David J. Hosfield, Nobuyuki Takakura, Mingnam Tang
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Patent number: 7910579Abstract: It is intended to provide a benzoxazole derivative or a pharmaceutically acceptable salt or solvate thereof which is useful in the early diagnosis of a conformation disease; a composition or a kit containing the same for diagnosing a conformation disease; a medical composition for treating and/or preventing a conformation disease; and so on.Type: GrantFiled: July 4, 2007Date of Patent: March 22, 2011Assignee: Tohoku UniversityInventors: Yukitsuka Kudo, Syozo Furumoto, Nobuyuki Okamura
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Patent number: 7906553Abstract: Described herein are compounds of Formula (I) having the structure: where A, J, R1, R4, Z and X are described herein; and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: GrantFiled: August 26, 2009Date of Patent: March 15, 2011Assignee: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20110059964Abstract: The present invention relates to the orexin receptor antagonists compounds of the general formula (I) as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic application thereof.Type: ApplicationFiled: February 3, 2010Publication date: March 10, 2011Applicant: sanofi-aventisInventors: Michel Aletru, Peter Aranyi, Maria Balogh, Sandor Batori, Judit Bence, Philippe Bovy, Zoltan Kapui, Endre Mikus, Claudie Namane, Christophe Philippo, Tibor Szabo, Zsuzsanna Tomoskozi, Katalin Urban-Szabo
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Publication number: 20110046112Abstract: The invention is concerned with novel heterobicyclic derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, V, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: ApplicationFiled: November 8, 2010Publication date: February 24, 2011Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei, Ulrike Obst Sander
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Publication number: 20110039821Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: ApplicationFiled: October 27, 2010Publication date: February 17, 2011Inventors: Hao Bai, Simon Bailey, Dilip Ramakant Bhumralkar, Feng C. Bi, Fengli Guo, Mingying He, Paul Stuart Humphries, Anthony Lai Ling, Jihong Lou, Seiji Nukui, Ru Zhou
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Patent number: 7888509Abstract: One aspect of the invention relates to 1,8-diarylnaphthalene compounds. In certain embodiments, a compound of the invention is an N-oxide of a 1,8-diarylnaphthalene. In certain embodiments, the aryl group is an optionally substituted acridyl group. In certain embodiments, a compound of the invention is a single steroisomer. In certain embodiments, a compound of the invention is a single enantiomer. Another aspect of the present invention relates to a method of detecting the presence of an analyte in a sample by monitoring the fluorescence of a compound of the invention in a sample. In certain embodiments, the analyte is a metal ion. Another aspect of the present invention relates to a method of determining the enantiomeric purity of an analyte by monitoring the fluorescence of a compound of the invention in the presence of the analyte. In certain embodiments, the analyte is a compound that is capable of hydrogen bonding.Type: GrantFiled: November 1, 2004Date of Patent: February 15, 2011Assignee: Georgetown UniversityInventors: Christian Wolf, Xuefeng Mei
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Patent number: 7888513Abstract: The invention relates to a method for producing an azoline compound represented by the general formula (3): wherein R1 represents an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; R3, R4, R5 and R6 may be the same or different and each represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; two arbitrary groups selected from R3, R4, R5 and R6 may bond to each other to form a ring; and Z1 represents an oxygen atom, a sulfur atom or a selenium atom; comprising reacting a carboxylic acid or a carboxylic acid derivative represented by the general formula (1): R1CO2R2??(1) wherein R1Type: GrantFiled: December 4, 2006Date of Patent: February 15, 2011Assignee: Takasago International CorporationInventors: Kazushi Mashima, Takashi Ohshima, Takanori Iwasaki, Hironori Maeda, Kenya Ishida
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Publication number: 20110034507Abstract: The present invention relates to farnesoid X receptors (FXR, NR1H4). FXR is a member of the nuclear receptor class of ligand-activate transcription factors. More particularly, the present invention relates to compounds useful as agonists for FXR, pharmaceutical formulations comprising such compounds, and therapeutic use of the same. Novel isoxazole compounds are disclosed as part of pharmaceutical compositions for the treatment of a condition mediated by decreased FXR activity, such as obesity, diabetes, cholestatic liver disease, liver fibrosis, and metabolic syndrome.Type: ApplicationFiled: June 13, 2008Publication date: February 10, 2011Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Adwoa Akwabi-Ameyaw, David Norman Deaton, Robert Blount McFadyen, Frank Navas, III
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Publication number: 20110028466Abstract: The current invention pertains to nitroimidazooxazine and nitroimidazooxazole analogues, their methods of preparation, and uses of the compounds as treatment for Mycobacterium tuberculosis, for use as anti-tubercular drugs, for use as anti-protozoal agents with unexpectedly high potency against Trypanosoma cruzi or Leishmania donovani, and for the treatment of other microbial infections.Type: ApplicationFiled: July 30, 2010Publication date: February 3, 2011Applicant: Global Alliance for TB Drug DevelopmentInventors: Andrew Mark Thompson, William Alexander Denny, Adrian Blaser, Zhenkun Ma
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Publication number: 20110028463Abstract: [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. [Means for Solving Problems] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and as a result, they have found that various amide derivatives having a carboxylic group or an equivalent thereof exhibit an excellent EP4 receptor antagonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor antagonistic action, it is useful as an agent for preventing and/or treating chronic renal insufficiency or diabetic nephropathy.Type: ApplicationFiled: July 2, 2008Publication date: February 3, 2011Applicant: Astellas Pharma Inc.Inventors: Eisuke Nozawa, Ryotaro Ibuka, Kazuhiro Ikegai, Keisuke Matsuura, Tatsuya Zenkoh, Ryushi Seo
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Patent number: 7879850Abstract: The present invention provides compounds of the following structure; A-Q-B—C-D that are useful for treating conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: GrantFiled: September 26, 2008Date of Patent: February 1, 2011Assignee: Novartis AGInventors: Young-Shin Kwak, Gary Mark Coppola
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Publication number: 20110009448Abstract: A compound having Formula I wherein one of R1 and R2 is a group of the formula wherein R4 is selected from H and hydrocarbyl, R5 is a hydrocarbyl group and L is an optional linker group, or R1 and R2 together form a ring substituted with the group wherein R3 is H or a substituent, and wherein X is selected from S, O, NR6 and C(R7)(R8), wherein R6 is selected from H and hydrocarbyl groups, wherein each of R7 and R8 are independently selected from H and hydrocarbyl groups.Type: ApplicationFiled: July 23, 2010Publication date: January 13, 2011Inventors: Nigel Vicker, Su Xiangdong, Dharshini Ganeshapillai, Atul Purohit, Michael John Reed, Barry Victor Lloyd Potter
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Publication number: 20110009617Abstract: Ruthenium nanoparticles supported on non-cross-linked soluble polystyrene were prepared by reacting [RuCl2(C6H5CO2Et)]2 with polystyrene in open air. They effectively catalyze intra- and intermolecular carbenoid insertion into C—H and N—H bonds, alkene cyclopropanation, and ammonium ylide/[2,3]-sigmatropic rearrangement reactions. This supported ruthenium catalyst is much more reactive than [RuCl2(p-cymene)]2 and Ru(Por)CO] for catalytic intermolecular carbenoid C—H bond insertion into saturated alkanes. By using a-diazoacetamide as a substrate for intramolecular carbenoid C—H insertion, the supported ruthenium catalyst can be to recovered and reused for ten successive iterations without significant loss of activity.Type: ApplicationFiled: July 13, 2010Publication date: January 13, 2011Inventors: Chi-Ming Che, Kwok-Wai Matthew Choi
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Patent number: 7868004Abstract: A compound of the formula I in which X and Y are selected as follows: (i) X is H and Y is selected from the group consisting of (ii) X and Y together form a bivalent radical selected from the group consisting of —O—CH2—O—, —N?CH—O— and —N?CH—S— thus forming together with the carbon atoms to which the radical is attached a 5-membered ring. The compounds have cooling properties and are useful in, for example, foodstuffs, dentifrices and cosmetics.Type: GrantFiled: February 23, 2006Date of Patent: January 11, 2011Assignee: Givaudan S.A.Inventors: Lucienne Cole, Stefan Michael Furrer, Christophe C. Galopin, Pablo Victor Krawec, Adam Mazur, Jay Patrick Slack
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Patent number: 7863305Abstract: Compounds of formula I: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: GrantFiled: June 1, 2005Date of Patent: January 4, 2011Assignee: Roche Palo Alto LLCInventors: Robert Greenhouse, Saul Jaime-Figueroa, Lubica Raptova, Deborah Carol Reuter, Karin Ann Stein, Robert Weikert
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Publication number: 20100317832Abstract: The present invention applications for same. More particularly, the present invention relates to novel aziridine aldehydes and processes for preparing these novel compounds. The invention also relates to aziridine-conjugated amino derivatives, and processes for preparing the same. Pentacyclic compounds may be prepared using the aziridine aldehydes of the present invention, and the invention relates to these compounds and the processes by which they are made. The invention also relates to aziridine-conjugated bioactive molecules, such as amino acids and peptides, and processes for preparing such compounds.Type: ApplicationFiled: October 22, 2007Publication date: December 16, 2010Inventors: Andrei K. Yudin, Ryan Hili
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Publication number: 20100308310Abstract: Disclosed herein are compounds represented by a formula: R1—O-A-C?C-D, where R1, A, and D are defined as described herein. Compositions and light-emitting devices related thereto are also disclosed.Type: ApplicationFiled: May 26, 2010Publication date: December 9, 2010Applicant: Nitto Denko CorporatonInventors: SHIJUN ZHENG, Jensen Cayas, Sheng Li, Amane Mochizuki, Hyunsik Chae
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Patent number: 7842814Abstract: The present invention relates to certain compounds and to methods for the preparation of certain compounds that can be used in the fields of chemistry and medicine. Specifically, described herein are methods for the preparation of various compounds and intermediates, and the compounds and intermediates themselves. More specifically, described herein are methods for synthesizing Salinosporamide A and its analogs from a compound of formula (V).Type: GrantFiled: April 6, 2007Date of Patent: November 30, 2010Assignee: Nereus Pharmaceuticals, Inc.Inventors: Taotao Ling, Venkata Rami Reddy Macherla, Barbara Christine Potts, Rama Rao Manam, Katherine A. McArthur
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Publication number: 20100292240Abstract: Certain sulfonamide compounds are dual CCK1/CCK2 inhibitors useful in the treatment of CCK1/CCK2 mediated diseases.Type: ApplicationFiled: July 26, 2010Publication date: November 18, 2010Inventors: Brett Allison, Victor K. Phuong, Mama C.W. Pippel, Michael H. Rabinowitz, Hariharan Venkatesan
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Publication number: 20100291355Abstract: Lithographic printing plate precursor comprising (a) a lithographic substrate with a hydrophilic surface and (b) a radiation-sensitive coating on the hydrophilic surface comprising (i) one or more types of monomers and/or oligomers and/or polymers, each comprising at least one ethylenically unsaturated group accessible to a free-radical polymerization, (ii) at least one sensitizer, and (iii) at least one coinitiator capable of forming free radicals together with the sensitizer, said coinitiator being other than metallocenes, characterized in that the at least one sensitizer comprises a compound of formula (I) wherein at least one of the groups R9 to R12 is a bulky group which has a van der Waals volume of at least 55 ?3.Type: ApplicationFiled: January 31, 2007Publication date: November 18, 2010Inventors: Bernd Strehmel, Harald Baumann
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Publication number: 20100285470Abstract: Monomethine dyes that have no or minimal fluorescence in buffer or in the presence of single stranded DNA or RNA, but strongly fluoresce in the presence of double-stranded DNA. In one embodiment, the dye is useful in quantitative RT-PCR.Type: ApplicationFiled: September 30, 2008Publication date: November 11, 2010Applicant: Thermo Fisher Scientific (Milwaukee) LLCInventors: Charles K. Brush, Jianqin Liu, Peter Czerney, Matthias Wenzel
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Patent number: 7825155Abstract: Disclosed is a compound represented by the formula (1) below, a prodrug thereof or a pharmaceutically acceptable salt of either, which is useful as a therapeutic, preventive or ameliorating agent for diabetes and the like. (In the formula, R3 represents an optionally substituted carbamoyl group or the like; X represents a hydroxyl group or the like; W1 and W2 independently represent a single bond or methylene; R7 and R8 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; and Ar represents an optionally substituted aryl group or the like.Type: GrantFiled: September 13, 2006Date of Patent: November 2, 2010Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Teruhisa Tokunaga, Tsuyoshi Takasaki, Kozo Yoshida, Ryu Nagata
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Patent number: 7825145Abstract: The present invention relates to a method of treatment and/or prophylaxis of a microbial infection, comprising the step of administering an effective amount of a compound of formula (I), in which X and Y are either the same or different and selected from a heteroatom; is a double or single bond depending on the heteroatoms X and Y; R1 to R5 are either the same or different and selected from hydrogen or a non-deleterious substituent; and R6 and R7 are either the same or different and selected from hydrogen and a non-deleterious substituent or one of R6 and R7 are absent when there is a double bond present, pharmaceutically acceptable salts or derivatives, pro-drugs, tautomers and/or isomers thereof. The present invention also relates to a method for protecting a subject from radiation damage, a method of cancer radiotherapy and use as an antimicrobial or radioprotective agent of the compound of formula (I) defined above.Type: GrantFiled: October 24, 2007Date of Patent: November 2, 2010Assignee: Biodiem LtdInventors: Peter Prokofievich Denisenko, Nickolay Sergeevich Sapronov, Alexander Alexandrovich Tarasenko
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Publication number: 20100267961Abstract: Provided is a process for the preparation of 5-(ethylsulfonyl)-2-(naphthalen-2-yl) benzo[d]oxazole useful in the treatment of Duchenne muscular dystrophy.Type: ApplicationFiled: August 14, 2008Publication date: October 21, 2010Inventors: Graham Wynne, Alexander Weymouth-Wilson, Robert Clarkson, Renate Van Well, Stephen Wren, Olivier De Moor
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Patent number: 7816536Abstract: Disclosed are 4-substituted and 7-substituted indoles, benzofurans, benzothiophenes, benzimidazoles, benzoxazoles, and benzothiazoles. Also disclosed are methods for making 4-substituted and 7-substituted indoles, benzofurans, benzothiophenes, benzimidazoles, benzoxazoles, and benzothiazoles, including those having the formulae. The methods include contacting a 4-substituted-6,7-dihydro indole, benzofuran, benzothiophene, benzimidazole, benzoxazole, or benzothiazole compound or a 7-substituted-4,5-dihydro indole, benzofuran, benzothiophene, benzimidazole, benzoxazole, or benzothiazole compound with a vinyldiazo compound in the presence of a dirhodium catalyst.Type: GrantFiled: June 9, 2006Date of Patent: October 19, 2010Assignee: The Research Foundation of State University of New YorkInventors: Huw M. L. Davies, James Manning
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Publication number: 20100261725Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: August 26, 2009Publication date: October 14, 2010Applicant: CALCIMEDICA, INC.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey