Nonshared Hetero Atoms In At Least Two Rings Of The Polycyclo Ring System Patents (Class 514/81)
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Publication number: 20110009356Abstract: Novel cyclic phosphoramidate prodrugs of drugs of formula I their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are described.Type: ApplicationFiled: September 24, 2010Publication date: January 13, 2011Applicant: Metabasis Therapeutics, Inc.Inventors: Mark D. ERION, K. Raja Reddy, Serge H. Boyer
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Publication number: 20110009367Abstract: The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.Type: ApplicationFiled: March 4, 2010Publication date: January 13, 2011Applicant: Bayer Schering Pharma AktiengesellschaftInventors: Ulrich Niewöhner, Maria Niewöhner, Mazen Es-Sayed, Helmut Haning, Thomas Schenke, Karl-Heinz Schlemmer, Jörg Keldenich, Erwin Bischoff, Elisabeth Perzborn, Klaus Dembowsky, Peter Serno, Marc Nowakowski
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Publication number: 20100317623Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.Type: ApplicationFiled: October 19, 2007Publication date: December 16, 2010Inventors: Nigel J. Liverton, Vincenzo Summa, Joseph P. Vacca
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Publication number: 20100310574Abstract: The invention provides compositions and kits containing an atrogin-1 inhibitor compound useful for the treatment of a statin-mediated myopathy. Kits for the diagnosis of a statin-mediated myopathy are also provided. The invention further features methods for treating or preventing a statin-mediated myopathy in a subject via administration of a therapeutically effective amount of an atrogin-1 inhibitor compound. The invention further provides methods of diagnosing a subject as having a propensity to develop a statin-induced myopathy and methods of monitoring a statin-induced myopathy or a propensity to develop a statin-mediated myopathy in a subject. The invention also features methods for identifying a compound for the treatment of a statin-mediated myopathy and methods of identifying a statin compound as having the propensity to induce a statin-mediated myopathy.Type: ApplicationFiled: June 5, 2008Publication date: December 9, 2010Applicant: Beth Israel Deaconess Medical CenterInventors: Vikas P. Sukhatme, Stewart H. Lecker, Junichi Hanai
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Publication number: 20100298256Abstract: Lipid-modified phosphodiester nucleoside prodrugs are described herein. The prodrugs can be used to treat viral infections and cancer.Type: ApplicationFiled: December 23, 2008Publication date: November 25, 2010Inventors: Steven Dong, Mel C. Schroeder
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Publication number: 20100298269Abstract: Disclosed are prodrug compounds of formula (I) (wherein variables R1 and R2 are as described herein) which are analogues of an antagonist of CGRP receptors and which are useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.Type: ApplicationFiled: February 4, 2009Publication date: November 25, 2010Applicant: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Steven N. Gallicchio, Valentino J. Stella
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Publication number: 20100298209Abstract: The invention which is the subject of the present application relates to a compound of structure I: A-B-C for use in the prophylaxis and/or treatment of a viral infection, and in particular for preventing and/or inhibiting viral replication, in which A is a quinoline or a quinoline-type group, B is a single amino acid or a peptide or polypeptide having a given amino acid sequence, C is an O-phenoxy group and the symbol “-” indicates that the entities A, B and C are chemically bonded within the compound I. According to a particular embodiment, said compound is a protease inhibitor, in particular a caspase inhibitor, and more particularly the inhibitor Q-VD-OPh (N-(2(quinolyl)valyl-aspartyl-(2,6-difluorophenoxy)methyl ketone), optionally in an O-methylated form.Type: ApplicationFiled: October 31, 2008Publication date: November 25, 2010Inventors: Jérôme Estaquier, Mireille Laforge, Anna Senik
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Publication number: 20100292188Abstract: The present invention relates to compounds of formula (I) comprising a cyclobutoxy group, processes for preparing them, pharmaceutical compositions comprising said compounds and their use as pharmaceuticals.Type: ApplicationFiled: January 22, 2009Publication date: November 18, 2010Applicant: UCB PHARMA S.A.Inventors: Frédéric Denonne, Sylvain Celanire, Anne Valade, Sabine Defays, Véronique Durieu
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Publication number: 20100292189Abstract: A method of inhibiting replication of a flavivirus in animal cells, and an oligonucleotide compound for use in the method are disclosed. The oligonucleotide analog (i) has a nuclease-resistant backbone, (ii) is capable of uptake by the cells, (iii) contains between 8-40 nucleotide bases, and (iv) has a sequence of at least 8 bases complementary to a region of the virus' positive strand RNA genome that includes at least a portion of SEQ ID NOS:1-4. Exposure of cells infected with a flavivirus to the analog is effective to form within the cells, a heteroduplex structure composed of the virus ssRNA and the oligonucleotide, characterized by a Tm of dissociation of at least 45° C., and having disrupted base pairing between the virus' 5? and 3? cyclization sequences.Type: ApplicationFiled: August 2, 2010Publication date: November 18, 2010Applicant: AVI BIOPHARMA, INC.Inventors: Patrick L. Iversen, David A. Stein
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Publication number: 20100285122Abstract: The invention provides solid dose forms (e.g. tablets) comprising a compound of Formula I, a compound of Formula II, a compound of Formula III and a salt of Formula IV.Type: ApplicationFiled: February 4, 2010Publication date: November 11, 2010Applicant: Gilead Sciences, Inc.Inventors: Reza Oliyai, Mark M. Menning, Joanna M. Koziara
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PHYSICALLY/MOLECULARLY DISTRIBUTED AND/OR CHEMICALLY BOUND MEDICAMENTS IN EMPTY, HARD CAPSULE SHELLS
Publication number: 20100285116Abstract: The present invention incorporates medicaments in the empty hard capsule shells (body and cap). The medicament is either physically/molecularly distributed and/or chemically bound to the polymer matrix of the capsule shell composition. Other medicaments in the form of drug-loaded matrices (powders, granules, beads, pellets, mini-tablets, and mini-capsules) can be filled in the drug-loaded empty, hard capsule shells. The same capsule dosage form contains medicaments in the core matrix and in the shell.Type: ApplicationFiled: July 21, 2010Publication date: November 11, 2010Inventor: HEMANT NARAHAR JOSHI -
Publication number: 20100286094Abstract: Conformationally constrained compounds that are novel and mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins and having bicyclic framework are disclosed, as well as their prodrugs. Such reverse-turn mimetic structures and pro-drugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. The invention also relates to a use of such compounds for the preparation of a medicament for treating or preventing cancer including an acute myeloid leukemia.Type: ApplicationFiled: October 15, 2008Publication date: November 11, 2010Applicant: Choongwae Pharma CorporationInventors: Jae Uk Chung, Kyung-yun Jung, Min-Wook Jeong, Hee-Kyung Jung, Hyun-Ju La
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Publication number: 20100286088Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain 3-substituted-4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5]tetrazine-8-carboxylic acid amide (collectively referred to herein as 3TM compounds). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative disorders such as cancer, etc., and methods of preparing such compounds.Type: ApplicationFiled: December 16, 2008Publication date: November 11, 2010Applicant: PHARMINOX LIMITEDInventors: Malcolm Francis Graham Stevens, David Cousin, Sharon Jennings, Andrew James McCarroll, John Gareth Williams, Marc Geoffery Hummersone, Jihong Zhang
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Publication number: 20100267672Abstract: Disclosed are novel reverse turn mimetics based on the framework of pyrazino-triazinone, and the use thereof in the treatment of cancers, particularly, acute myeloid leukemia. A method is also provided for manufacturing the reverse turn mimetics on a mass scale.Type: ApplicationFiled: April 14, 2010Publication date: October 21, 2010Applicant: Choongwae Pharma CorporationInventors: Kyung-Yun Jung, Jae Uk Chung, Min-Wook Jeong, Hee-Kyung Jung, Hyun-Ju La, Sang-Ho Ma, Yong-Sil Lee
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Publication number: 20100261670Abstract: There is provided a composition comprising the reaction product of: (a) one or more phosphate derivatives of one or more hydroxylated actives; and (b) one or more complexing agents selected from the group consisting of amphoteric surfactants, cationic surfactants, amino acids having nitrogen functional groups and proteins rich in these amino acids.Type: ApplicationFiled: April 27, 2010Publication date: October 14, 2010Inventors: Simon Michael West, Robert J. Verdicchio, David Kannar
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Publication number: 20100256095Abstract: The present invention provides compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.Type: ApplicationFiled: June 18, 2010Publication date: October 7, 2010Applicant: Eisai Inc.Inventors: Vincent J. Kalish, Jie Zhang, Weizheng Xu, Jia-He Li, Amy Dongxia Xing, Qun Liu
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Patent number: 7807683Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.Type: GrantFiled: March 31, 2006Date of Patent: October 5, 2010Assignee: Schering CorporationInventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Alan Mallams, Carmen S. Alvarez, Kartik M. Keertikar, Jocelyn Rivera, Tin Yau Chan, Vincent Madison, Thierry O. Fischmann, Lawrence W. Dillard, Vinh D. Tran, Zhen Min He, Ray Anthony James, Haengsoon Park, Vidyadhar M. Paradkar, Douglas Walsh Hobbs
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Publication number: 20100249068Abstract: Disclosed herein are nucleotide analogs with protected phosphates, methods of synthesizing nucleotide analogs with protected phosphates and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with the nucleotide analogs with protected phosphates.Type: ApplicationFiled: March 19, 2010Publication date: September 30, 2010Applicant: Alios BioPharma, Inc.Inventors: Leonid Beigelman, Lawrence Blatt, Guangyi Wang
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Publication number: 20100249067Abstract: The invention relates to compounds of Formula (I), a polymorph, an enantiomer, a stereoisomer, a solvate, an N-oxide derivative, or a pharmaceutically acceptable salt thereof: Formula (I), which have inhibitory effect on one or more protein kinases that are involved in cell mitosis.Type: ApplicationFiled: January 30, 2008Publication date: September 30, 2010Applicant: Biogen Idec MA Inc.Inventors: Srinivas Rao Kasibhatla, Kevin Hong, Lin Zhang, Marcus F. Boehm, Junhua Fan, Jean-Yves LeBrazidec
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Patent number: 7803788Abstract: A novel method has led to the identification of novel mixed ester-amidates of PMPA for retroviral or hepadnaviral therapy, including compounds of structure (5a) having substituent groups as defined herein. Compositions of these novel compounds in pharmaceutically acceptable excipients and their use in therapy and prophylaxis are provided.Type: GrantFiled: April 28, 2008Date of Patent: September 28, 2010Assignee: Gilead Sciences, Inc.Inventors: Mark W. Becker, Harlan H. Chapman, Tomas Cihlar, Eugene J. Eisenberg, Gong-Xin He, Michael R. Kernan, William A. Lee, Ernest J. Prisbe, John C. Rohloff, Mark L. Sparacino
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Publication number: 20100240613Abstract: The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I] wherein each symbol is as defined in the specification and a method of therapeutically or prophylactically treating an undesirable cell proliferation, comprising administering such a compound. The compound of the present invention has superior activity in suppressing undesirable cell proliferation, particularly, an antitumor activity, and is useful as an antitumor agent for the prophylaxis or treatment of cancer, rheumatism, and the like. In addition, the compound of the present invention can be a more effective antitumor agent when used in combination with other antitumor agents such as an alkylating agent or metabolism antagonist.Type: ApplicationFiled: November 25, 2009Publication date: September 23, 2010Applicant: Japan Tobacco Inc.Inventors: Hisashi Kawasaki, Hiroyuki Abe, Kazuhide Hayakawa, Tetsuya Iida, Shinichi Kikuchi, Takayuki Yamaguchi, Toyomichi Nanayama, Hironori Kurachi, Masahiro Tamaru, Yoshikazu Hori, Mitsuru Takahashi, Takayuki Yoshida, Toshiyuki Sakai
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Publication number: 20100234444Abstract: The invention provides hindered ester-based biodegradable linkers for the delivery of oligonucleotides in vivo, as well as method of making and using the same.Type: ApplicationFiled: March 12, 2009Publication date: September 16, 2010Applicant: ENZON PHARMACEUTICALS, INC.Inventor: Hong ZHAO
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Publication number: 20100233190Abstract: The present invention provides single chain antibody-directed polymeric prodrugs containing multifunctional linkers. Methods of making the polymeric delivery systems and methods of treating mammals using the same are also disclosed.Type: ApplicationFiled: March 12, 2009Publication date: September 16, 2010Applicant: ENZON PHARMACEUTICALS, INC.Inventors: Hong ZHAO, Maria Belen RUBIO, Pasanna Reddy
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Publication number: 20100227798Abstract: The invention provides methods and tools for the in vivo self-assembly of drugs. This makes it possible to reduce problems associated with the lack of selectivity, reduced solubility and other disadvantages of intact drugs.Type: ApplicationFiled: March 20, 2007Publication date: September 9, 2010Applicant: Koninklijke Philips Electronics N.V.Inventors: Marc Stefan Robillard, Holger Cruell
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Publication number: 20100227831Abstract: A novel composition of a phosphonoformic acid partial ester chemically linked to an anticancer compound of the general formula: wherein R1 is selected from the group consisting of methyl, alkyl, cholesteryl, aryl and aralkyl, R2 is selected from the group consisting of hydrogen, methyl, alkyl, and a water-soluble cation, Y is selected from the group consisting of oxygen, sulfur, carbon and nitrogen, and R3 is a cytotoxic agent. Methods for making and administering these compositions for treatment of cancer are also disclosed.Type: ApplicationFiled: May 19, 2010Publication date: September 9, 2010Inventor: Jayanta Saha
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Publication number: 20100222303Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins as well as their prodrugs are disclosed. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds and prodrugs for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: ApplicationFiled: December 29, 2009Publication date: September 2, 2010Applicant: Choongwae Pharma CorporationInventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen, Soo Jin Lee
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Publication number: 20100222302Abstract: The invention relates to novel chimeric antibiotics of formula I wherein R1 is CH2NHCOR5, heteroarylmethyl, heteroaryloxymethyl or heteroarylaminomethyl; R2 is H, OH, OSO3H, OPO3H2, OCH2OPO3H2, OCOCH2CH2COOH, OCOR6; R3 is H or halogen; R4 is (C1-C3)alkyl, (C1-C3)haloalkyl or cycloalkyl; R5 is alkyl or haloalkyl; and R6 is the residue of a naturally occurring amino acid or of dimethylaminoglycine. These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).Type: ApplicationFiled: August 7, 2006Publication date: September 2, 2010Inventors: Christian Hubschwerlen, Philippe Panchaud, Christine Sigwalt, Jean-Luc Specklin
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Publication number: 20100216746Abstract: The present invention relates to compounds that are a non-nucleoside reverse transcriptase inhibitors, and to processes for the preparation and use of the same. Specifically, the present invention includes methods of using such compounds in the treatment of human immunodeficiency virus infection.Type: ApplicationFiled: June 5, 2008Publication date: August 26, 2010Applicant: GLAXOSMITHKLINE LLCInventors: PEK Yoke Chong, Andrew James Peat, Paul Richard Sebahar, Michael Youngman, Huichang Zhang
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Publication number: 20100210598Abstract: Provided herein are small molecule conjugates that are agonists or antagonists of one or more toll-like receptors.Type: ApplicationFiled: February 11, 2010Publication date: August 19, 2010Applicant: Regents of the University of California, San DiegoInventors: Dennis A. Carson, Howard B. Cottam, Tomoko Hayashi, Michael Chan
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Publication number: 20100210596Abstract: The present invention provides methods of treating immune disorders. The present invention provides methods of treating an autoimmune disorder; methods of reducing the risk of transplant rejection; methods of increasing transplant survival; and methods of treating graft-versus host disease. The methods generally involve administering to an individual in need thereof an effective amount of an aminopyrimidine compound.Type: ApplicationFiled: January 29, 2007Publication date: August 19, 2010Inventors: Jeffrey A. Bluestone, Arthur Weiss
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Publication number: 20100210597Abstract: According to the invention there are provided derivatives of a C21-deoxy ansamycin or salt thereof which contain a 1-hydroxyphenyl moiety bearing at position 3 an aminocarboxy substituent, in which position 5 and the aminocarboxy substituent at position 3 are connected by an aliphatic chain of varying length characterised in that the 1-hydroxy position of the phenyl ring is derivatised by an aminoalkyleneaminocarbonyl group, which alkylene group (which may optionally be substituted by alkyl groups) has a chain length of 2 or 3 carbon atoms, a phosphoric acid, or a phosphoric acid ester (such as an alkyl ester) group, or a salt thereof, and which derivatising group increases the water solubility and/or the bioavailability of the parent molecule. Such compounds are useful in therapy eg in the treatment of cancer and B-cell malignancies.Type: ApplicationFiled: March 3, 2008Publication date: August 19, 2010Inventors: Steven Moss, Christine Martin, Ming Zhang
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Publication number: 20100210599Abstract: This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R1 does not exist; W is C or N with the proviso that when W is N, R2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. wherein: L and M are independently selected from the group consisting of C1-C6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.Type: ApplicationFiled: April 26, 2010Publication date: August 19, 2010Inventors: Yasutsugu Ueda, Timothy P. Connolly, John F. Kadow, Nicholas A. Meanwell, Tao Wang, Chung-Pin H. Chen, Kap-Sun Yeung, Zhongxing Zhang, David Kenneth Leahy, Shawn K. Pack, Nachimuthu Soundararajan, Pierre Sirard, Kathia Levesque, Dominique Thoraval
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Publication number: 20100204307Abstract: The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of the HAMP gene (HAMP gene), comprising an antisense strand having a nucleotide sequence which is less that 30 nucleotides in length, generally 19-25 nucleotides in length, and which is substantially complementary to at least a part of the HAMP gene. The invention also relates to a pharmaceutical composition comprising the dsRNA together with a pharmaceutically acceptable carrier; methods for treating diseases caused by HAMP gene expression and the expression of the HAMP gene using the pharmaceutical composition.Type: ApplicationFiled: April 9, 2010Publication date: August 12, 2010Inventors: Tomoko Nakayama, Anke Geick, Pamela Tan, Herbert Y. Lin
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Publication number: 20100202977Abstract: Disclosed herein are compounds, compositions and methods for modulating the expression of STAT 6 in a cell, tissue, or animal. Also provided are uses of disclosed compounds and compositions in the manufacture of a medicament for treatment of diseases and disorders related to expression of STAT 6, airway hyperresponsiveness, and/or pulmonary inflammation.Type: ApplicationFiled: May 12, 2006Publication date: August 12, 2010Inventors: James Karras, Jeffrey R. Crosby, Brett P. Monia, Susan M. Freier
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Publication number: 20100204182Abstract: The present invention provides ectonucleotidase inhibitors represented by the following formula, including ecto-nucleotide triphosphate diphosphohydrolase (NTPDase) inhibitors and ecto-5?-nucleotidase (ecto-5?-NT) inhibitors, namely nucleotide mimetics as selective NTPDase or ecto-5?-NT inhibitors. It also provides methods for preparations of said compounds. Furthermore provided are pharmaceutical and diagnostic compositions comprising said compounds, and the use of said compounds in a medicament for treating diseases associated with ectonucleotidase activity and/or P1 or P2 receptors.Type: ApplicationFiled: May 24, 2007Publication date: August 12, 2010Applicant: RHEINISCHE FRIEDRICH-WILHELMS-UNIVERSITAT BONNInventors: Christa E. Müller, Andreas Brunschweiger, Jamshed Iqbal
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Publication number: 20100183600Abstract: The present invention provides imidazooxazole and imidazothiazole compounds and their syntheses. The compounds of the present invention are capable of inhibiting the activity of RAF kinase, such as B-RAFV600E. The compounds are useful for the treatment of cell proliferative disorders such as cancer.Type: ApplicationFiled: December 4, 2009Publication date: July 22, 2010Applicant: ARQULE, INC.Inventors: Jean-Marc Lapierre, Yanbin Liu, Manish Tandon, Mark A. Ashwell
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Publication number: 20100183517Abstract: Compounds of the formula, A-L-B, wherein A is glutamate or a glutamate analog; L is a phosphoramidate or a phosphoramidate analog; and B is serine or a serine analog are described which are potent inhibitors of prostate-specific membrane antigen (PMSA). Such compounds are useful in treatment of prostate cancer; and when chemically attached to a fluorescent dye, can efficiently and selectively label prostate cancer cells for fluorescent imaging.Type: ApplicationFiled: January 22, 2010Publication date: July 22, 2010Applicant: CANCER TARGETED TECHNOLOGY LLCInventor: Cliff Berkman
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Publication number: 20100179108Abstract: The present invention involves use of the compounds narciclasine (2a) and 7-deoxy-narciclasine (2c), which are obtained via isolation from the medicinal plant species Narcissus (Amaryllidaceae), as precursors in a novel synthesis method in which each of these compounds are selectively hydrogenated to produce trans-dihydronarciclasine (1a) and 7-deoxy-trans-dihydronarciclasine (1c). Also described herein is a novel synthesis method for producing sodium narcistatin (11) from narciclasine (2a). Further described herein are certain novel 3,4-cyclic phosphate prodrugs, including sodium-7-deoxynarcistatin (8), sodium-7-deoxy-transdihydronarcistatin (9), and sodium transdihydronarcistatin (10).Type: ApplicationFiled: March 15, 2010Publication date: July 15, 2010Applicant: AZ Board of Regents, a body corporate of the State of AZ, Acting for & on Behalf of AZ State Univ.Inventors: George R. Pettit, Noeleen Melody
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Publication number: 20100173870Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.Type: ApplicationFiled: February 5, 2010Publication date: July 8, 2010Inventors: Karl Y. Hostetler, James R. Beadle, Ganesh D. Kini
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Publication number: 20100173013Abstract: The present application is generally directed to compounds, compositions and methods of combination therapy for the treatment of neoplastic disorders.Type: ApplicationFiled: January 7, 2010Publication date: July 8, 2010Inventors: Denis Drygin, Kenna Anderes, Caroline B. Ho, Joshua R. Bliesath, Christopher B. Proffitt, Sean O'Brien, William G. Rice
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Publication number: 20100166826Abstract: The present disclosure relates to biodegradable intravaginal rings for the delivery of therapeutic or prophylactic agent, inter alia, antiviral agents. The present disclosure further relates to biodegradable polyurethanes which will allow therapeutic/prophylactic agents to be released in a controlled manner that will not degrade when in use, but will degrade upon disposal.Type: ApplicationFiled: January 22, 2008Publication date: July 1, 2010Applicant: University of Uath Research FoundationInventors: Patrick F. Kiser, Patrick Tresco, Mark Mitchnick, Kavita Gupta, Hyder Aliyar
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Publication number: 20100168064Abstract: 2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120 (Na+ form) to form disodium salts. The results of preliminary screening revealed that these phosphates showed significant anti-cancer activity. A novel intermediate, 2-selenophene 4-quinolone and ?/, ?/-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.Type: ApplicationFiled: December 7, 2007Publication date: July 1, 2010Applicant: China Medical UniversityInventors: Sheng-Chu Kuo, Che-Ming Teng, Kuo-Hsiung Lee, Li-Jiau Huang, Li-Chen Chou, Chih-Shiang Chang, Chung-Ming Sun, Tian-Shung Wu, Shiow-Lin Pan, Tzong-Der Way, Jang-Chang Lee, Jing-Gung Chung, Jai-Sing Yang, Chien-Ting Chen, Ching-Che Huang, Shih-Ming Huang
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Publication number: 20100143301Abstract: Provided are modulators of TLRs of Formula II: pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: December 7, 2009Publication date: June 10, 2010Applicant: Gilead Sciences, Inc.Inventors: Manoj C. Desai, Randall L. Halcomb, Paul Hrvatin, Hon Chung Hui, Ryan Mc Fadden, Paul A. Roethle, Hong Yang
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Publication number: 20100137253Abstract: Compositions and uses associated with the MT477 family of compounds are disclosed. Particular structural features and properties of the compounds are described in detail. Uses include administering an MT477 family member to a patient for therapeutic purposes. Compositions include chemicals belonging to the MT477 family and pharmaceuticals that contain such chemicals.Type: ApplicationFiled: December 10, 2009Publication date: June 3, 2010Applicant: Medisyn Technologies, Inc.Inventors: Javier Llompart, Jorge Galvez, Kollol Pal
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Publication number: 20100129321Abstract: The present invention relates to pharmaceutical compositions for treating virus infections and/or diseases caused thereby comprising 4{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide optionally combined with at least one additional therapeutic agent.Type: ApplicationFiled: December 6, 2006Publication date: May 27, 2010Applicant: BAYER HEALTHCARE LLCInventors: Olaf Weber, Bernd Riedl
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Patent number: 7723319Abstract: The present invention relates to an acyclic nucleoside phosphonate derivative which is useful as an antiviral agent (particularly, against hepatitis B virus), pharmaceutically acceptable salts, stereoisomers, and a process for the preparation thereof.Type: GrantFiled: September 9, 2009Date of Patent: May 25, 2010Assignee: LG Life Sciences Ltd.Inventors: Dong-Gyu Cho, Jae-Hong Lim, Jae-Taeg Hwang, Woo-Young Cho, Hyun-Sook Jang, Chang-Ho Lee, Tae-Saeng Choi, Chung-Mi Kim, Yong-Zu Kim, Tae-Kyun Kim, Seung-Joo Cho, Gyoung-Won Kim, Jong-Ryoo Choi, Jeong-Min Kim, Kee-Yoon Roh
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Publication number: 20100120717Abstract: Compounds are provided for use with kinases that comprise a compound selected from the group consisting of formula (I) wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture in comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: October 8, 2007Publication date: May 13, 2010Inventors: Jason W. Brown, Qing Dong, Bheema R. Paraselli, Jeffrey A. Stafford, Michael B. Wallace, Hasanthi Wijesekera
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Publication number: 20100120718Abstract: The present invention relates to combinations of A) oxazolidinones of the formula (I) with B) acetylsalicylic acid (aspirin) and C) an ADP receptor antagonist, in particular P2Y12 purinoreceptor blocker, to a process for producing these combinations and to the use thereof as medicaments, in particular for the prophylaxis and/or treatment of thromboembolic disorders.Type: ApplicationFiled: October 19, 2007Publication date: May 13, 2010Applicant: Bayer Schering Pharma AktiengesellschaftInventor: Elisabeth Perzborn
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Publication number: 20100113359Abstract: The present invention relates to new dimethylphenoxy inhibitors of viral protease or parasitic enzymes, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 5, 2009Publication date: May 6, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Patent number: 7709020Abstract: This invention concerns a new family of phosphorus-containing compounds containing a moiety JQA- in which: A is absent or is —O—, —S— or —NR2—; Q is absent or (if A is —O—, —S— or —NR2—) Q may be —V—, —OV—, —SV—, or —NR2V—, where V is an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, such that J is linked to the cyclohexyl ring directly, through A or through VA, OVA, SVA or NR2VA; K is O or S; each occurrence of Y is independently —O—, —S—, —NR2—, or a bond linking a R5 moiety to P; each occurrence of R2 and R5 is independently an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, or H; and each occurrence of R6 is independently —PK(YR5)(YR5), —SO2(YR5) or —C(O)(YR5); so long as any R2, or R5 moiety linked directly to P is not H; wherein two R2, R5 and/or R6 moieties may be chemically linked to one another to form a ring; each occurrence of G is independently —O—, —S—, —NR2— or (M)x; each occurrence of M is independently a substituted or unsubstituted methylene moiety, and any M-M? moieType: GrantFiled: January 5, 2007Date of Patent: May 4, 2010Assignee: ARIAD Pharmaceuticals, Inc.Inventors: David L. Berstein, Leonard W. Rozamus, Yihan Wang, Chester A. Metcalf, III