Patents Represented by Attorney Yong Zhao
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Patent number: 8288407Abstract: 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 11, 2011Date of Patent: October 16, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Michael J. Kelly, III, Mark E. Layton, Philip E. Sanderson
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Patent number: 8268827Abstract: 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: November 14, 2008Date of Patent: September 18, 2012Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti SpA.Inventors: Danila Branca, Gabriella Dessole, Federica Ferrigno, Philip Jones, Olaf Kinzel, Samuele Lillini, Ester Muraglia, Giovanna Pescatore, Carsten Schultz-Fademrecht
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Patent number: 8263632Abstract: The present invention relates to a compound of Formula (I): wherein: n is 0 or 1; X is 0 or CH2; R1 is H or C1-2 alkyl; R2 is H or C1-3 alkyl; R3 and R4 are each independently H or C1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from R10; R5 is H or OCH3; R10 is F or Cl; or a pharmaceutically acceptable salt or ester thereofType: GrantFiled: March 15, 2010Date of Patent: September 11, 2012Assignees: Vertex Pharmaceuticals Incoporated, MSD K.K.Inventors: Toshiharu Iwama, Nobuhiko Kawanishi, Michael Mortimore, Mitsuru Ohkubo, Tomoko Sunami
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Patent number: 8258132Abstract: The present invention is directed to novel pharmaceutical compositions of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine. The pharmaceutical compositions of this invention useful in the treatment or prevention of disorders such as psychiatric disorders including depression and anxiety, inflammatory diseases and emesis.Type: GrantFiled: December 9, 2002Date of Patent: September 4, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: H. William Bosch, Elaine Liversidge, Suhas D. Shelukar, Karen C. Thompson
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Patent number: 8207169Abstract: The compounds of Formula D are of the class of triazolo-pyrido-pyrazines which are inhibitors of AKT useful for the treatment of cancerType: GrantFiled: May 28, 2009Date of Patent: June 26, 2012Assignee: MSD K.K.Inventors: Hidetomo Furuyama, Yasuhiro Goto, Nobuhiko Kawanishi, Mark E. Layton, Takashi Mita, Akira Naya, Yoshio Ogino, Yu Onozaki, Kevin J. Rodzinak, Toshihiro Sakamoto, Philip E. Sanderson, Jiabing Wang
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Patent number: 8188247Abstract: This invention features conjugates, compositions, methods of synthesis, and applications thereof, including folate derived conjugates of nucleosides, nucleotides, non-nucleosides, and nucleic acids including enzymatic nucleic acids and antisense nucleic acid molecules.Type: GrantFiled: August 30, 2010Date of Patent: May 29, 2012Assignee: Sirna Therapeutics, Inc.Inventors: Leonid Beigelman, Jasenka Matulic-Adamic
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Patent number: 8188084Abstract: 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 25, 2007Date of Patent: May 29, 2012Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti SpA.Inventors: Philip Jones, Olaf Kinzel, Giovanna Pescatore, Laura Llauger Bufi, Carsten Schultz-Fademrecht, Federica Ferrigno
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Patent number: 8133885Abstract: The present invention relates to compounds having general Formula (I) or a pharmaceutically acceptable salt thereof. The present invention also relates to pharmaceutical compositions comprising said compounds and the use of these derivatives to modulate glucocorticoid receptor activity.Type: GrantFiled: February 14, 2006Date of Patent: March 13, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Ralf Plate, Guido Jenny Rudolf Zaman, Pedro Harold Han Hermkens, Christiaan Gerardus Johannes Maria Jans, Rogier Christian Buijsman, Adrianus Petrus Antonius De Man, Paolo Giovanni Martino Conti, Scott James Lusher, Willem Hendrik Abraham Dokter
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Patent number: 8124633Abstract: The present invention is directed to certain hydroxymethyl ether hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, LUTS, depression, and anxiety.Type: GrantFiled: April 7, 2008Date of Patent: February 28, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Robert J. DeVita, Sander G. Mills, Jinlong Jiang, Andrew J. Kassick, Jianming Bao
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Patent number: 8119681Abstract: The present invention is directed to 2-[1-phenyl-5-hydroxy or methoxy-4alpha-methyl-hexahydrocyclopenta[f]indazol-5-yl]ethyl phenyl derivatives of formula I (I) as glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: October 23, 2007Date of Patent: February 21, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher J. Bungard, Jesse J. Manikowski, James J. Perkins, Robert Meissner
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Patent number: 7923568Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.Type: GrantFiled: September 29, 2006Date of Patent: April 12, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Mark L. Greenlee, Dongfang Meng, Dann L. Parker, Jr., Wanying Sun, Kenneth J. Wildonger, Robert R. Wilkening
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Combination therapy for the treatment of urinary frequency, urinary urgency and urinary incontinence
Patent number: 7893091Abstract: This invention concerns compositions for the treatment of urinary frequency, urinary urgency and urinary incontinence comprising (R)-N-[4-[2-[[2-hydroxy-2-(pyridin-3 -yl)ethyl]amino]ethyl]phenyl]-4-[4-(4-trifluoromethylphenyl)thiazol-2-yl]benzenesulfonamide and pharmaceutically acceptable salts thereof. In another aspect, this invention concerns combination therapy for urinary frequency, urinary urgency and urinary incontinence wherein one of the active agents is (R)-N-[4-[2-[[2-hydroxy-2-(pyridin-3-yl)ethyl]amino]ethyl]phenyl]-4-[4-(4-trifluoromethylphenyl)thiazol-2-yl]benzenesulfonamide and pharmaceutically acceptable salts thereof.Type: GrantFiled: September 29, 2006Date of Patent: February 22, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Keith M. Gottesdiener, Stuart A. Green, Euan MacIntyre -
Patent number: 7732432Abstract: The present invention encompasses compounds of Formula (I) or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: January 16, 2004Date of Patent: June 8, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, James M. Balkovec, Donald W. Graham, Mark L. Greenlee, Gayle E. Taylor
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Patent number: 7709508Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, age-related mild cognitive impairment, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, irritable bowel syndrome, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.Type: GrantFiled: February 12, 2009Date of Patent: May 4, 2010Assignee: Merck Sharp & DohmeInventors: Mark L. Greenlee, Dongfang Meng, Donald M. Sperbeck, Kenneth J. Wildonger
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Patent number: 7683068Abstract: The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.Type: GrantFiled: June 23, 2006Date of Patent: March 23, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Jinlong Jiang, Robert J. DeVita, Sanjeev Kumar, Sander G. Mills, Richard A. Tschirret-Guth
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Patent number: 7662846Abstract: The present invention encompasses compounds of Formula (I) and Formula (II) or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: April 19, 2004Date of Patent: February 16, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, James M. Balkovec, Richard Beresis, Steven L. Colletti, Donald W. Graham, Gool F. Patel, Cameron J. Smith
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Patent number: 7659294Abstract: The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.Type: GrantFiled: October 18, 2005Date of Patent: February 9, 2010Assignee: Merck & Co., Inc.Inventors: Jeffrey John Hale, Lin Yan
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Patent number: 7652058Abstract: The present invention is directed to certain hydropyranopyrrolidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.Type: GrantFiled: December 12, 2005Date of Patent: January 26, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Robert J. DeVita, Jinlong Jiang, Sander G. Mills, Jonathan R. Young
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Patent number: 7625937Abstract: The present invention encompasses compounds of Formula I: or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: September 26, 2007Date of Patent: December 1, 2009Assignee: Merck & Co., Inc.Inventors: Amjad Ali, James M. Balkovec, Donald W. Graham, Christopher F. Thompson, Nazia Quraishi
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Patent number: 7605171Abstract: The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.Type: GrantFiled: December 13, 2004Date of Patent: October 20, 2009Assignee: Merck & Co., Inc.Inventors: Vincent J. Colandrea, George A. Doherty, Jeffrey J. Hale, Pei Huo, Irene E. Legiec, Leslie Toth, Petr Vachal, Lin Yan