Patents Represented by Attorney Matthew A. Leff
-
Patent number: 8187630Abstract: A bilayer solid composition comprising (a) an immediate release first layer comprising an anti-allergic effective amount of desloratadine and at least one pharmaceutically acceptable excipient and (b) a sustained release second layer comprising an effective amount of a nasal decongestant, e.g. pseudoephedrine sulfate and a pharmaceutically acceptable sustained release agent wherein the composition contains less than about 2% of desloratadine decomposition products is disclosed. A solid composition comprising an anti-allergic effective amount of desloratadine and at least one, and preferably two pharmaceutically acceptable antioxidants is also disclosed.Type: GrantFiled: October 2, 2009Date of Patent: May 29, 2012Assignee: Schering-Plough CorporationInventor: Wing-Kee Philip Cho
-
Patent number: 8173172Abstract: The invention relates to a method of producing an agglomerate of drug and solid binder. The process involves producing individual agglomerate particles and then converting the convertible amorphous content of same, following agglomeration, by the application of, for example, moisture. Agglomerates capable of conversion as well as the finished agglomerates and oral and nasal dosing systems including same are also contemplated. The process produces agglomerates which are rugged but which will produce an acceptable fine particle fraction during dosing.Type: GrantFiled: November 29, 2007Date of Patent: May 8, 2012Assignee: Schering CorporationInventor: Tsong-Toh Yang
-
Patent number: 8168652Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: GrantFiled: March 3, 2010Date of Patent: May 1, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Philip E. Sanderson, Mark E. Layton, Kevin J. Rodzinak
-
Patent number: 8101621Abstract: The present invention relates to a compound of general formula I: wherein: n1 and n2 are the same or different, and are 0 or 1; R is aryl, heteroaryl, etc.; Re is hydrogen atom or lower alkyl; two groups selected from four groups consisting of (i) either one of Ra1 and Ra1?, (ii) either one of Ra2 and Ra2?, (iii) either one of Rb1 and Rb1?, and (iv) either one of Rb2 and Rb2?, are combined to form ā(CH2)nā where n is 1, 2 or 3; and among Ra1, Ra1?, Ra2, Ra2?, Rb1, Rb1?, Rb2 and Rb2?, the groups which do not form ā(CH2)nā are each independently hydrogen atom, etc.; X1, X2, X3 and X4 are each independently CH, N, etc.; Y1, Y2, Y3 and Y4 are the same or different and are CH or N, etc.; W is a 5-membered aromatic heterocyclic group, or a pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: April 25, 2007Date of Patent: January 24, 2012Assignee: MSD K.K.Inventors: Tetsuya Kato, Nobuhiko Kawanishi, Takashi Mita, Keita Nagai, Katsumasa Nonoshita, Mitsuru Ohkubo
-
Patent number: 8071623Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts, stereoisomers or tautomers thereof which are inhibitors of poly (ADP-ribose) polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes, neurodegenerative diseases, retroviral infection, retinal damage or skin senescence and UV-induced skin damage, and as chemo- and/or radiosensitizers for cancer treatment.Type: GrantFiled: January 8, 2008Date of Patent: December 6, 2011Assignee: Instituto di Ricerche di Biologia Molecolare P. Angeletti SpAInventors: Philip Jones, Jesus Maria Ontoria Ontoria, Rita Scarpelli, Carsten Schultz-Fademrecht
-
Patent number: 8008317Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: GrantFiled: June 7, 2006Date of Patent: August 30, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Donna J. Armstrong, Essa H. Hu, Michael J. Kelly, III, Mark E. Layton, Yiwei Li, Jun Liang, Kevin J. Rodzinak, Michael J. Rossi, Philip E. Sanderson, Jiabing Wang
-
Patent number: 8003643Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.Type: GrantFiled: November 18, 2009Date of Patent: August 23, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D. P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
-
Patent number: 7981910Abstract: Triazole derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.Type: GrantFiled: October 16, 2006Date of Patent: July 19, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Sherman T. Waddell, James M. Balkovec, Nancy J. Kevin, Xin Gu
-
Patent number: 7964578Abstract: This invention features conjugates, degradable linkers, compositions, methods of synthesis, and applications thereof, including cholesterol, folate, galactose, galactosamine, N-acetyl galactosamine, PEG, phospholipid, peptide and human serum albumin (HSA) derived conjugates of biologically active compounds, including antibodies, antivirals, chemotherapeutics, peptides, proteins, hormones, nucleosides, nucleotides, non-nucleosides, and nucleic acids including enzymatic nucleic acids, DNAzymes, allozymes, antisense, dsRNA, siNA, siRNA, triplex oligonucleotides, 2,5-A chimeras, decoys and aptamers.Type: GrantFiled: October 16, 2008Date of Patent: June 21, 2011Assignee: Sirna Therapeutics, Inc.Inventors: Chandra Vargeese, Peter Haeberli, Weimin Wang, Tongqian Chen
-
Patent number: 7915263Abstract: The present invention relates to a compound of formula I: wherein: R1 is a hydrogen atom, F, CN, etc.; R1? is a hydrogen atom or lower alkyl which may be substituted; R2 is O, S, SO, SO2, etc.; R3 is a phenyl which may be substituted; X1, X2, and X3 each independently CH, N, etc. provided, however, that among X1, X2 and X3, the number of nitrogen is 0 or 1; W is the following residue: wherein: W1, W2, and W3 each independently CH, N, etc., or a pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: August 29, 2007Date of Patent: March 29, 2011Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshikazu Iwasawa, Tetsuya Kato, Nobuhiko Kawanishi, Kouta Masutani, Takashi Mita, Katsumasa Nonoshita, Mitsuru Ohkubo
-
Patent number: 7910561Abstract: The present invention is directed to compounds which contain substituted naphthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention. These substituted naphthyridines have unexpected advantageous properties when compared to other naphthyridines reported in PCT publication WO2003/086394, such unexpected advantageous properties may include increased cellular potency/solubility, greater selectivity, enhanced pharmacokinetic properties, lack of off target activity and so on.Type: GrantFiled: December 9, 2005Date of Patent: March 22, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Jeannie M. Arruda, Brian T. Campbell, Nicholas D. P. Cosford, Jacob M. Hoffman, Essa H. Hu, Mark E. Layton, Yiwei Li, Jun Liang, Kevin J. Rodzinak, Tony Siu, Brian A. Stearns, Lida R. Tehrani, Mark T. Bilodeau, Peter J. Manley
-
Patent number: 7893302Abstract: The present invention relates to novel cationic lipids, transfection agents, microparticles, nanoparticles, and short interfering nucleic acid (siNA) molecules. The invention also features compositions, and methods of use for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of gene expression and/or activity in a subject or organism. Specifically, the invention relates to novel cationic lipids, microparticles, nanoparticles and transfection agents that effectively transfect or deliver biologically active molecules.Type: GrantFiled: November 12, 2009Date of Patent: February 22, 2011Assignee: Sirna Therapeutics, Inc.Inventors: Tongqian Chen, Chandra Vargeese, Kurt Vagle, Weimin Wang, Ye Zhang
-
Patent number: 7834018Abstract: The present invention relates to a compound represented by the general formula (I): wherein m1 and m2 are 1, 2, or 3; n1 and n2 are 0 or 1; i is an integer of any of 1 to m1; j is an integer of 1 to m2; R is aryl, heteroaryl, or cycloalkyl any of which may be substituted; Rai and Rai? is hydrogen atom, etc. and Rbj and Rbj? is hydrogen atom, etc.; Rc, Rd, and Re are hydrogen atom, etc; X1 is CH, CX1a, or N; X2 is CH, N, etc.; X3 is CH, N, etc.; X4 is CH or N; Y1, Y2, and Y3 are each independently CH or N; Z1 and Z2 are each independently CH or N; W is a 5-membered aromatic heterocyclic group such as pyrazolyl, thiazolyl, etc., or a pharmaceutically acceptable salt or ester thereof; a pharmaceutical composition or antitumor agent containing the same; and combinations of the antitumor agent with other antitumor agent(s).Type: GrantFiled: December 3, 2008Date of Patent: November 16, 2010Assignee: Banyu Pharmaceutical Co., LtdInventors: Mitsuru Ohkubo, Tetsuya Kato, Nobuhiko Kawanishi, Takashi Mita, Toshiyasu Shimomura
-
Patent number: 7834015Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment.Type: GrantFiled: May 29, 2007Date of Patent: November 16, 2010Assignee: Instituto di Ricerche Di Biologia Molecolare P. Angeletti SpAInventors: Philip Jones, Olaf Kinzel, Laura Llauger Bufi, Ester Muraglia, Giovanna Pescatore, Caterina Torrisi
-
Patent number: 7750151Abstract: The present invention is directed to compounds which contain substituted napthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.Type: GrantFiled: April 5, 2005Date of Patent: July 6, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Mark T. Bilodeau, Chixu Chen, Nicholas D. P. Cosford, Brian W. Eastman, John C. Hartnett, Essa H. Hu, Peter J. Manley, Lou Anne Neilson, Lida R. Tehrani, Zhicai Wu
-
Patent number: 7705014Abstract: The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: GrantFiled: April 10, 2006Date of Patent: April 27, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Chixu Chen, Brian W. Eastman, Essa H. Hu
-
Patent number: 7691887Abstract: The present invention provides a method for the treatment or prevention of conditions which can be ameliorated by Smo antagonism, which method comprises administration to a patient in need thereof of an effective amount of a compound of formula I or a composition comprising a compound of formula I: or a pharmaceutically acceptable salt or solvate thereof; wherein: 2 of X, Y and Z represent nitrogen atoms, and the other represents an oxygen atom; R1 and R2 are taken together with the atom to which they are attached and represent a cyclobutyl ring, optionally substituted with 1-2 fluorine atoms, and R3 represents hydrogen or a fluorine atom; or R1 represents methyl, R2 represents methyl or a fluorine atom and R3 represents a fluorine atom.Type: GrantFiled: April 15, 2008Date of Patent: April 6, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: James M. Balkovec, Rolf Thieringer, Sherman T. Waddell
-
Patent number: 7691405Abstract: The present invention relates to novel cationic lipids, transfection agents, microparticles, nanoparticles, and short interfering nucleic acid (siNA) molecules. Specifically, the invention relates to novel cationic lipids, microparticles, nanoparticles and transfection agents that effectively transfect or deliver short interfering nucleic acid (siNA). The compositions described herein are generally referred to as formulated molecular compositions (FMC) or lipid nanoparticles (LNP).Type: GrantFiled: February 7, 2008Date of Patent: April 6, 2010Assignee: Sirna Therapeutics, IncInventors: Tongqian Chen, Kurt Vagle, Chandra Vargeese, Weimin Wang, Ye Zhang
-
Patent number: 7655649Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.Type: GrantFiled: April 5, 2005Date of Patent: February 2, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D. P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
-
Patent number: 7641915Abstract: The present invention relates to novel cationic lipids, transfection agents, microparticles, nanoparticles, and short interfering nucleic acid (siNA) molecules. The invention also features compositions, and methods of use for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of gene expression and/or activity in a subject or organism. Specifically, the invention relates to novel cationic lipids, microparticles, nanoparticles and transfection agents that effectively transfect or deliver biologically active molecules, such as antibodies (e.g., monoclonal, chimeric, humanized etc.Type: GrantFiled: March 13, 2008Date of Patent: January 5, 2010Assignee: Sirna Therapeutics, IncInventors: TongQian Chen, Chandra Vargeese, Kurt Vagle, WeiMin Wang, Ye Zhang