Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 546/23)
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Publication number: 20120252761Abstract: Compounds are provided for use with kinases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: April 2, 2012Publication date: October 4, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Jason W. Brown, Qing Dong, Bheema R. Paraselli, Nicholas Scorah, Jeffrey A. Stafford, Michael B. Wallace, Hasanthi Wijesekera
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Publication number: 20120245354Abstract: The technology of this invention concerns a method for the manufacture of hydroxy diphosphonic acids containing an amino moiety. The method specifically involves reacting a liquid P4O6 with an aminocarboxylic acid in the presence of a sulfonic acid. The aminocarboxylic acid is selected from 3 structurally different compounds. The amino hydroxy diphosphonic acids can be synthesized with high selectivity and purity and the unreacted starting raw materials can easily and conveniently be recirculated.Type: ApplicationFiled: October 4, 2010Publication date: September 27, 2012Applicant: STRAITMARK HOLDING AGInventors: Samuel Corentin Cogels, David Lemin, Patrick Notté
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Patent number: 8252774Abstract: Novel 5-azaindole bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders.Type: GrantFiled: September 22, 2009Date of Patent: August 28, 2012Assignee: Isis Innovation Ltd.Inventors: Frank Hallock Ebetino, Adam Mazur, Mark Walden Lundy, Robert Graham Russell
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Publication number: 20120184510Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.Type: ApplicationFiled: January 14, 2011Publication date: July 19, 2012Inventors: Raymond W. Colburn, Scott L. Dax, Christopher Flores, Jay Matthews, Ning Qin, Laura Reany, Christopher Teleha, Mark A. Youngman
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Patent number: 8222415Abstract: The present invention relates to novel chiral phosphorus compounds which can be readily prepared from quinoline derivatives as inexpensive starting compounds and have the general formula (I) wherein R1, R2, R3, R4, R5 are chiral or achiral organic residues which are derived from substituted or unsubstituted straight or branched chain or cyclic aliphatic or aromatic groups and which, in the case of the pairs R1/R2 and R4/R5, may be interconnected. Further, the invention relates to methods for the synthesis of chiral phosphorus compounds of general formula (I) and their use as catalyst components in processes for the preparation of optically active products.Type: GrantFiled: October 1, 2007Date of Patent: July 17, 2012Assignee: Johnson Matthey Public Limited CompanyInventors: Brian Adger, Alan Dyke, Giancarlo Francio, Frederick Ernest Hancock, Walter Leitner, Thomas Pullman, Andreas Seger, Antonio Zanotti-Gerosa
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Publication number: 20120177681Abstract: Immunopotentiators can be adsorbed to insoluble metal salts, such as aluminium salts, to modify their pharmacokinetics, pharmacodynamics, intramuscular retention time, and/or immunostimulatory effect. Immunopotentiators are modified to introduce a moiety, such as a phosphonate group, which can mediate adsorption. These modified compounds can retain or improve their in vivo immunological activity even when delivered in an adsorbed form.Type: ApplicationFiled: September 1, 2011Publication date: July 12, 2012Inventors: Manmohan Singh, David A.G. Skibinski, Tom Yao-Hsiang Wu, Yongkai Li, Alex Cortez, Xiaoyue Zhang, Yefen Zou, Timothy Z. Hoffman, Jianfeng Pan, Kathy Yue
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Publication number: 20120178679Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.Type: ApplicationFiled: March 13, 2012Publication date: July 12, 2012Applicant: KANEQ PHARMA INC.Inventors: John COLUCCI, Marie-Claire WILSON, Yongxin HAN, Claude DUFRESNE, Michel BELLEY, Cheuk K. LAU, Christopher BAYLY
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Patent number: 8217174Abstract: The present invention relates to a method for preparing montelukast, an inhibitor against leukotrienes, and an intermediate used therein. According to the inventive method, high-purity montelukast or its sodium salt can be prepared in a high yield.Type: GrantFiled: December 11, 2007Date of Patent: July 10, 2012Assignee: Hanmi Holdings Co., Ltd.Inventors: Gwan Sun Lee, Young-Kil Chang, Jaeheon Lee, Chul Hyun Park, Eun-Ju Park, Jaeho Yoo
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Publication number: 20120165352Abstract: 6-amino quinazoline or 3-cyano quinoline derivatives, preparation methods and pharmaceutical uses thereof are disclosed. Specifically, the present disclosure discloses novel 6-amino quinazoline or 3-cyano quinoline derivatives presented by general formula (I), or tautomers, enantiomers, diastereomers, racemates or pharmaceutically acceptable salts thereof, or metabolites, metabolic precursors or prodrugs thereof, and their uses as treatment agents especially as protein kinase inhibitors, in which each substitutent group of general formula (I) is as defined in the specification.Type: ApplicationFiled: August 26, 2010Publication date: June 28, 2012Applicants: SHANGHAI HENGRUI PHARMACEUTICAL CO., LTD., JIANGSU HENGRUI MEDICINE CO., LTD.Inventors: Peng Cho Tang, Xin Li, Bin Wang, Jun Wang, Lijun Chen
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Publication number: 20120142635Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:Type: ApplicationFiled: February 8, 2012Publication date: June 7, 2012Applicant: Morphochem Aktiengesellschaft Fur Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Müller, Michael W. Cappi
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Publication number: 20120135961Abstract: The present invention relates to the use of compounds, in which the pharmacophores of quinolone and oxazolidinone are chemically linked together through a linker that is stable under physiological conditions, for the treatment of anthrax and other infections.Type: ApplicationFiled: January 10, 2011Publication date: May 31, 2012Applicant: Morphochem Aktiengesellschaft Fur Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Hans Locher, Christine Schmitt
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Publication number: 20120129809Abstract: The invention provides a method for treating NSCLC, especially in cases of KRAS mutation, involving the administration of deforolimus.Type: ApplicationFiled: March 2, 2010Publication date: May 24, 2012Applicant: MERCK & CO.,Inventor: Scot Ebbinghaus
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Publication number: 20120122817Abstract: Compounds of formula (IA) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: May 28, 2010Publication date: May 17, 2012Applicant: ASTRAZENECA ABInventors: Neil Bifulco, Allison Laura Choy, Olga Quiroga, Brian Alan Sherer
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Publication number: 20120116079Abstract: Reagents are provided for the introduction of phosphonate groups into fluorescent dyes. Methods are also provided for preparing dye conjugates.Type: ApplicationFiled: August 29, 2011Publication date: May 10, 2012Inventors: Eugeny Lukhtanov, Alexei Vorobiev
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Publication number: 20120101064Abstract: The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+—O? or CR3; Y is N, N+—O? or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.Type: ApplicationFiled: April 30, 2010Publication date: April 26, 2012Applicants: Astex Therapeutics Limited, Novartis AGInventors: Steven Howard, Paul Neil Mortenson, Steven Douglas Hiscock, Alison Jo-Anne Woolford, Andrew James Woodhead, Gianni Chessari, Marc O'reilly, Miles Stuart Congreve, Claudio Dagostin, Young Shin Cho, Fan Yang, Christine Hiu-Tung Chen, Christopher Thomas Brain, Bharat Lagu, Yaping Wang, Sunkyu Kim, John Grialdes, Michael Joseph Luzzio, Lawrence Blas Perez
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Patent number: 8163911Abstract: The invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as mentioned in the specification and claims, which are suitable for preparing a medicament for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.Type: GrantFiled: September 4, 2008Date of Patent: April 24, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Elke Langkopf, Alexander Pautsch, Corinna Schoelch, Annette Schuler-Metz, Ruediger Streicher, Holger Wagner
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Patent number: 8163910Abstract: The present invention provides amide-substituted xanthene fluorescent dyes and reagent for the introduction of phosphonate or sulfo groups into the fluorescent dyes.Type: GrantFiled: October 2, 2008Date of Patent: April 24, 2012Assignee: Elitech Holding B.V.Inventor: Eugene Lukhtanov
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Publication number: 20120094958Abstract: The invention relates to a compound of formula (I) wherein the substituents are as described in the specification, which are useful as farnesyl pyrophosphate synthase modulators, e.g. in the treatment of proliferative diseases, to methods of manufacturing such compounds and to intermediates thereof.Type: ApplicationFiled: February 26, 2009Publication date: April 19, 2012Applicant: NOVARTIS AGInventors: Rene Amstutz, Guido Bold, Simona Cotesta, Wolfgang Jahnke, Andreas Marzinzik, Juliane Constanze Desiree Hartwieg, Silvio Ofner, Frédérik Stauffer, Johann Zimmermann
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Patent number: 8158797Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria.Type: GrantFiled: December 20, 2004Date of Patent: April 17, 2012Assignee: Morphochem Aktiengesellschaft fur Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Müller, Michael W. Cappi
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Publication number: 20120088916Abstract: The present invention relates to an octahydro biquinoline compound. Provided is also a method of separating the octahydro biquinoline compound into enantiomers. The octahydro biquinoline compound is of the general formula (V): In formula (V) R1 is one of H, a protective group and an aliphatic group, with the aliphatic group having a main chain of a length of 1 to about 10 carbon atoms, comprising 0 to about 6 heteroatoms selected from the group consisting of N, O, S, Se and Si. R2 and R3 are independent from one another selected from the group consisting of (i) H, (ii) one of an aliphatic, an alicyclic, an aromatic, an arylaliphatic, and an arylalicyclic group comprising 0 to about 6 heteroatoms selected from the group consisting of N, O, S, Se and Si, an ester, a carbonate group, a carbamoyl group and a phosphate ester.Type: ApplicationFiled: May 17, 2010Publication date: April 12, 2012Applicant: Nanyang Technological UniversityInventors: Teck Peng Loh, Jian Xiao
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Publication number: 20120068168Abstract: The present invention relates to a carbazole-based phosphine oxide compound, and an organic electroluminescent device including the same. According to the present invention, provided are a compound for an organic electroluminescent device which can improve the thermal stability and efficiency characteristics which are unstable and low, respectively, corresponding to problems of known compounds for organic electroluminescent devices, and particularly, can implement excellent efficiency characteristics in a pure blue phosphorescent device, by using the carbazole-based phosphine oxide compound of the compound for the organic electroluminescent device, and the organic electroluminescent device. According to one aspect of the present invention, the carbazole-based phosphine oxide compound of the compound for the organic electroluminescent device is provided, and the organic electroluminescent device containing the same which can implement thermal stability and high efficiency characteristics is also provided.Type: ApplicationFiled: November 16, 2009Publication date: March 22, 2012Applicant: INDUSTRY-ACADEMIC COOPERATION FOUNDATION, DANKOOK UNIVERSITYInventors: Jun-Yeob Lee, Soon-Ok Jeon, Kyoung-Soo Yook, Oh-Young Kim
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Publication number: 20120053347Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.Type: ApplicationFiled: August 31, 2010Publication date: March 1, 2012Inventors: Raymond W. Colburn, Scott L. Dax, Christopher Flores, Jay Matthews
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Publication number: 20120040936Abstract: Low molecular weight compound exhibiting an osteogenesis-promoting action having the general formula (I) or a pharmacologically acceptable salt thereof:Type: ApplicationFiled: October 5, 2011Publication date: February 16, 2012Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Osamu Kanno, Katsuyoshi Nakajima, Kazumasa Aoki, Ryoichi Tanaka, Shimpei Hirano, Kiyoshi Oizumi, Satoru Naito
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Publication number: 20120040430Abstract: The present invention provides dyes, reactive dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins and nucleic acids. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes are also provided that comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been modified by the addition of charged and polar groups to provide beneficial properties.Type: ApplicationFiled: June 17, 2009Publication date: February 16, 2012Applicant: ENZO LIFE SCIENCES, INC. C/O ENZO BIOCHEM, INC.Inventors: Yuejun Xiang, Praveen Pande, Rajesh Khazanchi, Elazar Rabbani, Dakai Liu, Wei Cheng
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Publication number: 20120013966Abstract: An electrochromic compound represented by the following Chemical Formula 1: Also disclosed is an electrochromic device including the electrochromic compound.Type: ApplicationFiled: June 29, 2011Publication date: January 19, 2012Applicant: SAMSUNG ELECTRONICS CO., LTD.Inventors: Rupasree Ragini DAS, Chang-Ho NOH, Seog-Jin JEON
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Publication number: 20120004411Abstract: The present invention relates to novel chiral phosphorus compounds which can be readily prepared from quinoline derivatives as inexpensive starting compounds and have the general formula (I) wherein R1, R2, R3, R4, R5 are chiral or achiral organic residues which are derived from substituted or unsubstituted straight or branched chain or cyclic aliphatic or aromatic groups and which, in the case of the pairs R1/R2 and R4/R5, may be interconnected. Further, the invention relates to methods for the synthesis of chiral phosphorus compounds of general formula (I) and their use as catalyst components in processes for the preparation of optically active products.Type: ApplicationFiled: October 1, 2007Publication date: January 5, 2012Applicant: JOHNSON MATTHEY PLCInventors: Brian Adger, Alan Dyke, Giancarlo Francio, Frederick Emest Hancock, Walter Leitner, Thomas Pullmann, Andreas Seger, Antonio Zanotti-Gerosa
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Publication number: 20110294758Abstract: The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.Type: ApplicationFiled: May 25, 2011Publication date: December 1, 2011Applicant: Metabasis Therapeutics, Inc.Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
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Publication number: 20110288054Abstract: 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: ApplicationFiled: September 22, 2009Publication date: November 24, 2011Applicant: Schering CorporationInventors: 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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Publication number: 20110282062Abstract: The present invention provides a compound of the formula (I) or a pharmaceutically acceptable salt thereof:Type: ApplicationFiled: November 27, 2009Publication date: November 17, 2011Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Kazuo Hattori, Takehiro Okada, Osamu Kondoh, Toshiyuki Tsukaguchi, Masaki Shibata, Satoshi Tanida
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Publication number: 20110282061Abstract: The compounds of the subject invention are adjuvant molecules that comprise a imidazoquinoline molecule covalently linked to a phospho- or phosphonolipid group. The compounds of the invention have been shown to be inducers of interferon-a, IL-12 and other immunostimulatory cytokines and possess an improved activity profile in comparison to known cytokine inducers when used as adjuvants for vaccine antigens.Type: ApplicationFiled: October 23, 2009Publication date: November 17, 2011Applicant: GLAXOSMITHKLINE BIOLOGICALS SAInventor: David A. Johnson
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Publication number: 20110269705Abstract: The present invention provides a quinolone compound that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the quinolone compound of the invention is represented by Formula (1): wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents halogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydrogen or the like.Type: ApplicationFiled: December 4, 2009Publication date: November 3, 2011Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Kenji Otsubo, Takahito Yamauchi, Yuji Ochi
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Publication number: 20110257100Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and ophthalmic diseases, disorders and conditions.Type: ApplicationFiled: April 8, 2011Publication date: October 20, 2011Inventors: Stëphane Raeppel, Franck Raeppel, Stephen William Claridge, Lijie Zhan, Frëdëric Gaudette, Michael Mannion, Norifumi Sato, Yohei Yuki, Masashi Kishida, Arkadii Vaisburg
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Publication number: 20110257130Abstract: Compounds are provided which can be useful in reducing the activity of an angiotensin-converting enzyme and thus be used to treat or prevent a renin-angiotensin aldosterone system-related disorder. These compounds include lipoic acid derivatives such as prolyl lipoic acid and pipecolinyl lipoic acid, and other compounds, and these compounds are useful in treating hypertension, stroke, or other renin-angiotensin aldosterone system-related disorders in human or animal patients. Pharmaceutical compositions prepared using these compounds and methods of treatment using these compounds are also provided.Type: ApplicationFiled: October 16, 2009Publication date: October 20, 2011Inventor: Desikan Rajagopal
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Publication number: 20110235150Abstract: Disclosed is an electrochromic material including a compound represented by Chemical Formula 1 and an electrochromic device including the electrochromic material. In Chemical Formula 1, R1, R2, L1, and L2 are as defined in the detailed description.Type: ApplicationFiled: March 3, 2011Publication date: September 29, 2011Applicant: SAMSUNG ELECTRONICS CO., LTD.Inventors: Rupasree Ragini DAS, Ji-Min LEE, Chang-Ho NOH, Seog-Jin JEON
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Publication number: 20110237550Abstract: Novel 5-azaindole bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders.Type: ApplicationFiled: September 22, 2009Publication date: September 29, 2011Applicant: ISIS INNOVATION LTD.Inventors: Frank Hallock Ebetino, Adam Mazur, Mark Walden Lundy, Robert Graham Russell
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Patent number: 8026388Abstract: Synthesis of biphosphonate compounds can be advantageously carried out in a solvent/diluent comprising a compound of formula (3) wherein R is hydrogen or a C1-C6 alkyl group; each of R1 is a C1-C6 alkyl group or both R1 groups are linked to form a C1-C3 alkylene group; and R2 is hydrogen, a C1-C6 alkyl group, a C1-C6 alkoxy group, or is linked together with R to form a C3-C7 carbon ring.Type: GrantFiled: July 10, 2009Date of Patent: September 27, 2011Assignee: Synthon BVInventor: Jiri Bartl
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Publication number: 20110230443Abstract: Novel imidazo[1,2-?]pyridinyl bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders.Type: ApplicationFiled: September 22, 2009Publication date: September 22, 2011Applicant: ISIS INNOVATION LTD.Inventors: Frank Hallock Ebetino, Adam Mazur, Mark Walden Lundy, Robert Graham Russell
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Patent number: 8012949Abstract: The disclosure provides, inter alia, novel bisphosphonate compounds and methods of making and using such compounds. In certain embodiments, compounds of the invention include bisphosphonates that are capable of selectively inhibiting one or more of farnesyl diphosphate synthase (FPPS), geranylgeranyl diphosphate synthase (GGPPS), and decaprenyl pyrophosphate synthase (DPPS). In preferred embodiments, compounds of the invention are capable of selectively inhibiting two or more of FPPS, GGPPS, and DPPS. In embodiments, compounds and methods of the invention demonstrate superior activity levels, such as in the anti-cancer context, immunostimulation context, and other contexts, which in several cases exceed the activity levels of previous generation bisphosphonate drugs by orders of magnitude. In embodiments, the invention provides compounds and methods in connection with research and therapeutic applications, e.g.Type: GrantFiled: April 11, 2008Date of Patent: September 6, 2011Assignee: The Board of Trustees of the University of IllinoisInventors: Eric Oldfield, Yonghui Zhang, Fenglin Yin
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Patent number: 7994320Abstract: The present invention provides prodrugs derived from the sparingly soluble anticancer isocarbostyril narciclasine, a component of various Narcissus species, said prodrugs having potential for use against animal and human cancers. Also disclosed is an efficient procedure for the synthetic conversion of narciclasine to several more soluble cyclic phosphate compounds, including “narcistatin”.Type: GrantFiled: September 10, 2008Date of Patent: August 9, 2011Assignee: Arizona Board of Regents, a Body Corporate of the State of Arizona, Acting for and on behalf of Arizona State UniversityInventors: George R. Pettit, Noeleen Melody
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Publication number: 20110190489Abstract: The invention provides a compound of Formula (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih), (Ii), (Ij), (Ik), or (Il) as defined herein, pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: December 1, 2010Publication date: August 4, 2011Applicant: Abbott LaboratoriesInventors: Neil Wishart, Maria A. Argiriadi, David J. Calderwood, Anna M. Ericsson, Bryan R. Fiamengo, Kristine E. Frank, Michael Friedman, Dawn M. George, Eric R. Goedken, Nathan S. Josephsohn, Biqin C. Li, Michael J. Morytko, Kent D. Stewart, Jeffrey W. Voss, Grier A. Wallace, Lu Wang, Kevin R. Woller, Eric C. Breinlinger, Kelly D. Mullen, Gagandeep Somal
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Publication number: 20110178001Abstract: The present invention relates to phosphonated Rifamycins, and methods of making and using such compounds. These compounds are useful as antibiotics for prophylaxis and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.Type: ApplicationFiled: August 10, 2009Publication date: July 21, 2011Applicant: TARGANTA THERAPEUTICS CORP.Inventors: Evelyne Dietrich, Ranga Reddy, Kelly Tanaka, Ting Kang, Yanick Lafontaine, Adel Rafai Far
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Publication number: 20110172191Abstract: A series of thieno[2,3-b]pyridine derivatives, attached at the 2-position to a substituted anilino moiety, which are substituted in the 3-position by a carbonyl group linked to a pyrrolidin-1-yl ring which in turn forms part of a heteroatom-containing fused bicyclic ring system, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.Type: ApplicationFiled: December 17, 2010Publication date: July 14, 2011Applicant: UCB Pharma S.A.Inventors: James Andrew Johnson, Daniel Christopher Brookings, Barry John Langham, Judi Charlotte Neuss, Joanna Rachel Thorne
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Publication number: 20110172193Abstract: The present invention is directed to pro-drugs of (E)-7-(3-(2-amino-1-fluoroethylidene)piperidin-1-yl)-1-cyclopropyl-6-fluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid, pharmaceutical compositions containing them and the use of said pro-drugs and pharmaceutical compositions as antimicrobial agents against pathogenic microorganisms, particularly against resistant microbes.Type: ApplicationFiled: January 3, 2011Publication date: July 14, 2011Inventors: Mark MACIELAG, Gary Eichenbaum, Tim Gaekens, Michel Guillaume, Brian Shook
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Publication number: 20110172423Abstract: An organic light-emitting diode comprising at least one cyclic phosphazene compound, a light-emitting layer formed from at least one matrix material and at least one emitter material, wherein the at least one matrix material comprises at least one cyclic phosphazene compound, the use of cyclic phosphazene compounds in organic light-emitting diodes and a device selected from the group consisting of stationary visual display units, mobile visual display units and illumination units comprising at least one inventive organic light-emitting diode, and selected cyclic phosphazene compounds and processes for preparing them.Type: ApplicationFiled: June 17, 2009Publication date: July 14, 2011Applicants: BASF SE, KONINKLIJKE PHILIPS ELECTRONICS N.V., OSRAM OPTO SEMICONDUCTORS GMBHInventors: Evelyn Fuchs, Oliver Molt, Nicolle Langer, Christian Lennartz, Peter Strohriegl, Pamela Schroegel, Herbert Friedrich Boerner, Volker Van Elsbergen, Arvid Hunze, Ralf Krause
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Publication number: 20110152525Abstract: The present invention provides novel ruthenium based catalysts, and a process for preparing amines, by reacting a primary alcohol and ammonia in the presence of such catalysts, to generate the amine and water. According to the process of the invention, primary alcohols react directly with ammonia to produce primary amines and water in high yields and high turnover numbers. This reaction is catalyzed by novel ruthenium complexes, which are preferably composed of quinolinyl or acridinyl based pincer ligands.Type: ApplicationFiled: August 10, 2009Publication date: June 23, 2011Applicant: Yeda Research and Development Co. Ltd. at the Weizmann Institute of ScienceInventors: David Milstein, Chidambaram Gunanathan
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Publication number: 20110077222Abstract: The present invention provides sustained-release opiate compositions. In particular, the present invention provides sustained-release opiate compositions that include an opiate attached to a blood albumin binder. The present invention also relates to methods of administering an opiate with a sustained release pharmacokinetic profile.Type: ApplicationFiled: September 30, 2010Publication date: March 31, 2011Applicant: Mallinckrodt Inc.Inventors: Carl J. Schaefer, Gary L. Cantrell
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Publication number: 20110077221Abstract: This invention provides nuclear hormone receptor binding compounds, compositions comprising the same and methods of uses thereof in treating a variety of diseases or conditions in a subject, including, inter-alia, prostate cancer and/or diseases or disorders of bone and muscle.Type: ApplicationFiled: July 19, 2007Publication date: March 31, 2011Inventors: James T. Dalton, Duane D. Miller, Igor Rakov, Casey Bohl, Michael L. Mohler
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Publication number: 20110053162Abstract: The invention provides compounds and compositions of Formulas I-VII, and methods of using the compounds. The compounds can be used to prepare dye conjugates that are uniformly and substantially more fluorescent on proteins, nucleic acids or other biopolymers, than conjugates labeled with structurally similar known carbocyanine dyes. In addition to having more intense fluorescence emission than structurally similar dyes at virtually identical wavelengths, and decreased artifacts in their absorption spectra upon conjugation to biopolymers, the compounds can have greater photostability and/or higher absorbance (extinction coefficients) at the wavelength(s) of peak absorbance than such structurally similar dyes.Type: ApplicationFiled: August 31, 2010Publication date: March 3, 2011Applicant: PROMEGA CORPORATIONInventors: Cesear Corona, Dieter Klaubert, Mark McDougall
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Publication number: 20110053893Abstract: The invention provides a novel class of compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 7. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine.Type: ApplicationFiled: September 1, 2010Publication date: March 3, 2011Applicants: IRM LLC, Novartis AGInventors: Tom Yao Hsiang Wu, Yongkai Li, Alex Cortez, Kathy Yue, Xiaoyue Zhang, Manmohan Singh, David Skibinski
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Publication number: 20110054165Abstract: The invention provides a novel class of xanthene dyes, some of which are functionalized to allow their coupling to conjugation partners of interest, e.g. biomolecules, drugs, toxins and the like. Also provided are conjugates of the dyes, methods of preparing and using the dyes and their conjugates and kits including the dyes and their conjugates.Type: ApplicationFiled: November 8, 2010Publication date: March 3, 2011Applicant: BIOSEARCH TECHNOLOGIES, INC.Inventors: MARK REDDINGTON, MATT LYTTLE