Polycyclo Ring System Having The Oxazole Ring As One Of The Cyclos Patents (Class 514/375)
  • Patent number: 10786473
    Abstract: It is provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of trans-thyretin-associated amyloidosis. It is also provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis in combination therapy with another COMT inhibitor, a benzoxazole derivative, iododiflunisal, diflunisal, resveratrol, tauroursodeoxycholic acid, doxocycline, or epigallocatechin-3-gallate.
    Type: Grant
    Filed: September 12, 2019
    Date of Patent: September 29, 2020
    Assignee: SOM Innovation Biotech, S.L.
    Inventors: Marc Centellas Casado, Raúl Insa Boronat, Nuria Reig Bolaño, Núria Gavaldà Batalla
  • Patent number: 10759768
    Abstract: The present invention provides a prophylactic or therapeutic agent for an autism spectrum disorder containing compound (I) having melatonin receptor affinity. A compound represented by the formula: wherein each symbol is as described in the specification, or a salt thereof.
    Type: Grant
    Filed: January 5, 2017
    Date of Patent: September 1, 2020
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Keisuke Hirai, Takashi Ishikawa
  • Patent number: 10449169
    Abstract: It is provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis. It is also provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis in combination therapy with another COMT inhibitor, a benzoxazole derivative, iododiflunisal, diflunisal, resveratrol, tauroursodeoxycholic acid, doxocycline, or epigallocatechin-3-gallate.
    Type: Grant
    Filed: August 13, 2018
    Date of Patent: October 22, 2019
    Assignee: SOM Innovation Biotech, S.L.
    Inventors: Marc Centellas Casado, Raúl Insa Boronat, Núria Reig Bolano, Nuria Gavaldà Batalla
  • Patent number: 10251869
    Abstract: A method of treating a bacterial infection in a subject in need thereof includes administering to the subject therapeutically effective amounts of at least one ?-lactam antibiotic and at least one bisthiazolidine metallo-?-lactamase inhibitor.
    Type: Grant
    Filed: March 20, 2017
    Date of Patent: April 9, 2019
    Assignee: CASE WESTERN RESERVE UNIVERSITY
    Inventors: Robert Bonomo, Alejandro Jose Vila, S. Graciela Mahler
  • Patent number: 10213416
    Abstract: The present invention relates to substituted benzoxazolone derivatives as acid ceramidase inhibitors, pharmaceutical compositions containing these inhibitors and methods of inhibiting acid ceramidase for the treatment of disorders in which modulation of the levels of ceramide is clinically relevant. The invention also provides substituted benzoxazolone derivatives for use in the treatment of cancer, inflammation, pain, inflammatory pain or pulmonary diseases.
    Type: Grant
    Filed: November 8, 2016
    Date of Patent: February 26, 2019
    Assignees: The Regents of the University of Chicago, Fondazione Istituto Italiano di Technologia
    Inventors: Daniele Piomelli, Daniela Pizzirani, Anders Bach, Rita Scarpelli, Laurin Melzig, Marco Mor
  • Patent number: 10076504
    Abstract: Provided herein are compounds, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof which have glucagon receptor antagonist or inverse agonist activity. Further, provided herein are 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 glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. Moreover, provided herein are methods of making or manufacturing compounds disclosed herein, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof.
    Type: Grant
    Filed: June 11, 2015
    Date of Patent: September 18, 2018
    Inventor: Lin Zhi
  • Patent number: 10045956
    Abstract: It is provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis. It is also provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis in combination therapy with another COMT inhibitor, a benzoxazole derivative, iododiflunisal, diflunisal, resveratrol, tauroursodeoxycholic acid, doxocycline, or epigallocatechin-3-gallate.
    Type: Grant
    Filed: March 2, 2017
    Date of Patent: August 14, 2018
    Assignee: SOM Innovation Biotech, S.L.
    Inventors: Marc Centellas Casado, Raúl Insa Boronat, Núria Reig Bolano, Nuria Gavaldà Batalla
  • Patent number: 9610270
    Abstract: It is provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis. It is also provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis in combination therapy with another COMT inhibitor, a benzoxazole derivative, iododiflunisal, diflunisal, resveratrol, tauroursodeoxycholic acid, doxocycline, or epigallocatechin-3-gallate.
    Type: Grant
    Filed: October 23, 2012
    Date of Patent: April 4, 2017
    Assignee: SOM INNOVATION BIOTECH, S.L.
    Inventors: Marc Centellas Casado, Raúl Insa Boronat, Nuria Reig Bolaño, Núria Gavaldà Batalla
  • Patent number: 9586917
    Abstract: A polymerizable compound has a practical low melting point, excellent solubility in a general-purpose solvent, and can produce an optical film at low cost, exhibits low reflected luminance, and achieves uniform conversion of polarized light over a wide wavelength band, an optically anisotropic article. A carbonyl compound is useful as a raw material for producing the polymerizable compound. (In the formula (I), Y1 to Y8 represent —C(?O)—O—, G1 and G2 represent a C1-20 divalent linear aliphatic group, Z1 and Z2 represent a C2-10 alkenyl group that is unsubstituted, or substituted with a halogen atom, Ax represents a C2-30 organic group with at least one aromatic ring, Ay represents a hydrogen atom or C1-20 alkyl group, A1 represents a trivalent aromatic group, A2 and A3 represent a C3-30 divalent alicyclic hydrocarbon group, A4 and A5 represent a C6-30 divalent aromatic group or the like, and Q1 represents a hydrogen atom.
    Type: Grant
    Filed: May 30, 2013
    Date of Patent: March 7, 2017
    Assignee: ZEON CORPORATION
    Inventors: Kei Sakamoto, Satoshi Kiriki, Kumi Okuyama, Kanako Taira
  • Patent number: 9404915
    Abstract: The disclosure provides methods for analysis of disease cell response to a therapeutic agent. In embodiments, a method comprises administering the therapeutic agent to a disease cell sample from the subject in a device that measures at least one physiological parameter of a cell; determining whether a change occurs in the physiologic parameter of the disease cell sample in response to the therapeutic agent as compared to a baseline measurement or the physiological parameter before administration of the therapeutic agent, and selecting the therapeutic agent that results in the change in the at least one physiologic parameter. In embodiments, the disease cells are whole, viable, and/or label free.
    Type: Grant
    Filed: January 6, 2015
    Date of Patent: August 2, 2016
    Assignee: Celcuity LLC
    Inventors: Lance Gavin Laing, Brian Francis Sullivan
  • Patent number: 9249112
    Abstract: The present invention relates to solid forms of the N-methyl-D-glucamine (meglumine) salt of 6-carboxy-2-(3,5-dichlorophenyl)-benzoxazole and to methods for their preparation. The invention is also directed to pharmaceutical compositions containing at least one solid form and to the therapeutic or prophylactic use of such solid forms and compositions.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: February 2, 2016
    Assignee: PFIZER INC.
    Inventors: Richard Frederic Labaudiniere, Michael Henry O'Neill
  • Patent number: 9067905
    Abstract: The invention provides sulphone compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various sulphone compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
    Type: Grant
    Filed: April 23, 2012
    Date of Patent: June 30, 2015
    Assignee: Zafgen, Inc.
    Inventors: Hazel J. Dyke, Susan M. Cramp, Thomas D. Pallin, Janusz J. Kulagowski, John G. Montana, Robert Zahler
  • Publication number: 20150148256
    Abstract: A bioluminescence imaging-based high-throughput assay for inhibitors of ABCG2 is described. Compositions of inhibitors of ABCG2 and methods of using ABCG2 inhibitors are also described.
    Type: Application
    Filed: August 21, 2014
    Publication date: May 28, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: MARTIN GILBERT POMPER, YIMAO ZHANG, JOHN LATERRA
  • Publication number: 20150148308
    Abstract: A harmful arthropod control composition comprising a compound represented by the following Formula (1) wherein each symbol represents definitions described in the specification, and one or more fungicidal compounds, which are selected from among azoles, strobilurins, phenylamides, rice blast controlling compounds, rice sheath blight disease controlling compounds, and other fungicidal compounds. The composition has an excellent controlling effect against harmful arthropods.
    Type: Application
    Filed: June 5, 2013
    Publication date: May 28, 2015
    Applicant: Sumitomo Chemical Company, Limited
    Inventors: Tatsuya Suzuki, Atsushi Iwata, Yoshihiko Nokura
  • Publication number: 20150126567
    Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of familial amyloid polyneuropathy may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of transthyretin-related hereditary amyloidosis, neurodegenerative diseases, amyloidosis, neuropathic pain, amyloid fibril formation and cardiomyopathy related diseases.
    Type: Application
    Filed: February 27, 2013
    Publication date: May 7, 2015
    Inventor: Mahesh Kandula
  • Patent number: 9024038
    Abstract: Inhibitors of HIV-1 protease and compositions containing them are described. Use of the inhibitors and compositions containing them to treat HIV, AIDS, and AIDS-related diseases is described.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: May 5, 2015
    Assignee: Purdue Research Foundation
    Inventors: Arun K. Ghosh, Bruno D. Chapsal, Hiroaki Mitsuya, Cuthbert D. Martyr
  • Publication number: 20150111935
    Abstract: The present invention relates to a novel class of 1,3-benzoxazol-2(3H)-ones and their use as a medicament, preferably as a dermatologic agent, and as a cosmetic. These novel compounds are particularly useful in treating and/or preventing inflammation, irritation, itching, pruritus, pain, oedema and/or pro-allergic or allergic conditions in a patient. Usually they are topically applied to the skin or mucosa in the form of a pharmaceutical or cosmetic composition comprising the compound and a pharmaceutically and/or cosmetically acceptable carrier.
    Type: Application
    Filed: May 21, 2013
    Publication date: April 23, 2015
    Applicant: DR. AUGUST WOLFF GMBH & CO. KG ARZNEIMITTEL
    Inventors: Chrsitoph Abels, Ulrich Knie, Michael Soeberdt
  • Patent number: 9012481
    Abstract: Novel benzoarylureido compounds and a use thereof for prevention and/or treatment of the neurodegenerative brain disease are provided. The neurodegenerative brain diseases may include Alzheimer's disease, dementia, Parkinson's disease, stroke, amyloidosis, Pick's disease, Lou Gehrig's disease, Huntington's disease, Creutzfeld-Jakob disease, and the like.
    Type: Grant
    Filed: December 29, 2009
    Date of Patent: April 21, 2015
    Assignee: Korea Institute of Science and Technology
    Inventors: Hoh-Gyu Hahn, Kee-Dal Nam, Dong-Yun Shin, Chan-Ho Park, Sung-Woo Cho, Eun-A Kim, Ghil-Soo Nam, Kyung-Il Chol, Seon-Hee Seo, Hee-Sup Shin, Dong-Jin Kim, Ae-Nim Pae, Hye-Jin Chung, Hyun-Ah Choo, Hye-Whon Rhim, Yong-Seo Cho, Eun-Joo Roh, Gyo-Chang Keum, Kee-Hyun Choi, Kye-Jung Shin, Chan-Seong Cheong, Jae-Kyun Lee, Yong-Koo Kang, Young-Soo Kim, Woong-Seo Park, Key-Sun Kim, He-Sson Chung, Chi-Man Song, Sun-Joon Min, Eunice Eun-Kyeong Kim, Cheol-Ju Lee, Soon-Bang Kang
  • Publication number: 20150105403
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 16, 2015
    Inventors: Nicholas D. Smith, Steven P. Govek, Mehmet Kahraman, Jackaline D. Julien, Johnny Y. Nagasawa, Karensa L. Douglas, Celine Bonnefous, Andiliy G. Lai
  • Publication number: 20150099730
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including those mediated by inhibition of fatty acid synthase (FASN) enzyme, such as, cancer, obesity or related discorders, and liver related disorders. Such compounds are represented by formula (I) as follows: wherein L1, a, b, m, n, R1, R2, R3, R4, and R5 are defined herein.
    Type: Application
    Filed: September 6, 2013
    Publication date: April 9, 2015
    Applicant: Janssen Pharmaceutica, NV
    Inventor: Peter J. Connolly
  • Publication number: 20150094329
    Abstract: A compound represented by formula (1) and an N-oxide thereof have excellent pest control effect. (In the formula, Het to which R1—S(O)n is bonded represents a five-membered aromatic heterocyclic ring represented by formula H1, H2, H3 or H4 (wherein Y1 represents an oxygen atom or the like; Y2 represents an oxygen atom or the like; G1, G2 and G3 may be the same or different and each represents a nitrogen atom or the like; R1 represents a C1-C6 alkyl group which may have one or more atoms or groups selected from the group X, or the like; and n represents 0, 1 or 2); A1 represents an oxygen atom or the like; A2 represents a nitrogen atom or the like; A3 represents a nitrogen atom or the like; and R2 and R3 may be the same or different and each represents a C1-C6 chain hydrocarbon group which may have one or more atoms or groups selected from the group X, or the like.
    Type: Application
    Filed: May 23, 2013
    Publication date: April 2, 2015
    Inventors: Yoshihiko Nokura, Mai Ito, Chie Shimizu, Hajime Mizuno
  • Patent number: 8993607
    Abstract: The invention provides compounds of formula I, II, and III as defined herein, as well as salts thereof. The compounds may have activity as anti-proliferative agents.
    Type: Grant
    Filed: August 1, 2008
    Date of Patent: March 31, 2015
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Joseph E. Rice
  • Publication number: 20150087680
    Abstract: Provided herein are compounds, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof which have glucagon receptor antagonist or inverse agonist activity. Further, provided herein are 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 glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. Moreover, provided herein are methods of making or manufacturing compounds disclosed herein, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or Co-crystals and prodrugs thereof.
    Type: Application
    Filed: November 26, 2014
    Publication date: March 26, 2015
    Inventors: Jorge E. Gomez-Galeno, Scott J. Hecker, Qun Dang, Mali Venkat Reddy, Zhili Sun, Matthew P. Grote, Thanh Huu Nguyen, Robert Huerta Lemus, Haiqing Li
  • Publication number: 20150072958
    Abstract: Various embodiments of the present invention relate to, among other things, compounds and methods of using those compounds to treat an HIV infection. The compounds of the various embodiments of the present invention provide, among other things, therapeutic agents having enhanced penetration capability across the blood-brain barrier, such that they can enter the CNS to treat an HIV-1 infection in the CNS.
    Type: Application
    Filed: September 10, 2014
    Publication date: March 12, 2015
    Inventors: Arun K. Ghosh, Hiroaki Mitsuya, Sofiya Yashchuk
  • Publication number: 20150057320
    Abstract: A method for treating a disease characterized by excessive lipofuscin accumulation in the retina of a mammal afflicted therewith comprising administering to the mammal an effective amount of a transthyretin (TTR) ligand.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 26, 2015
    Applicant: The Trustees of Columbia University in the City of New York
    Inventor: Konstantin PETRUKHIN
  • Patent number: 8957097
    Abstract: The present invention is directed to hemi phorboxazole A: and its stereoisomers, as well as derivatives of hemi phorboxazole A of formula I: wherein ring A is aryl or a 5- or 6-membered heteroaryl optionally substituted with one or more of halogen, —OH, or —C1-6alkyl; and R is —CN, a 5- or 6-membered heteroaryl, or halogen; and the pharmaceutically acceptable salt forms thereof, in addition to methods of using these compounds.
    Type: Grant
    Filed: July 23, 2010
    Date of Patent: February 17, 2015
    Assignees: The Trustees Of The University Of Pennsylvania, The Regents Of The University Of California
    Inventors: Amos B. Smith, III, Zhuqing Liu, Anne-Marie L. Hogan, Doralyn S. Dalisay, Tadeusz F. Molinski
  • Publication number: 20150045402
    Abstract: A compound which is useful as a dopamine D1 receptor positive allosteric modulator (D1 PAM) is provided. The present inventors have studied a compound which has a dopamine D1 receptor positive allosteric modulating activity and is useful as an active ingredient of a pharmaceutical composition for preventing and/or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like, and they have thus found that a heterocyclic acetamide compound has a dopamine D1 receptor positive allosteric modulating activity, thereby completing the present invention. The heterocyclic acetamide compound of the present invention has a dopamine D1 receptor positive allosteric modulating activity and can be used as an agent for preventing and/or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like.
    Type: Application
    Filed: October 28, 2014
    Publication date: February 12, 2015
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Ryota Shiraki, Takahiko TOBE, Shimpei KAWAKAMI, Hiroyuki MORITOMO, Makoto OHMIYA
  • Publication number: 20150045368
    Abstract: Compounds of Formula (I) and Formula (II) are useful inhibitors of tankyrase. Compounds of Formula (I) and Formula (II) have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: March 1, 2013
    Publication date: February 12, 2015
    Inventors: Howard Bregman, John L. Buchanan, Nagasree Chakka, Erin F. Dimauro, Hakan Gunaydin, Angel Guzman-Perez, Zihao Hua, Hongbing Huang, Xin Huang, Matthew W. Martin, Vinod F. Patel
  • Publication number: 20150045346
    Abstract: The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Application
    Filed: June 27, 2012
    Publication date: February 12, 2015
    Applicants: MERCK SHARP & DOHME CORP., ALECTOS THERAPEUTICS INC.
    Inventors: Tong-Shuang Li, Ernest J. McEachern, David J. Vocadlo, Yuanxi Zhou, Harold G. Selnick
  • Patent number: 8952058
    Abstract: Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFR? kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: February 10, 2015
    Assignee: Ambit Biosciences Corporation
    Inventors: Michael J. Hadd, Michael D. Hocker, Mark W. Holladay, Gang Liu, Martin W. Rowbottom, Shimin Xu
  • Publication number: 20150031694
    Abstract: The invention provides compounds of formula (I): wherein R1-R7 and W have any of the values defined in the specification, and salts thereof. The compounds have good solubility and are useful for treating bacterial infections.
    Type: Application
    Filed: March 21, 2013
    Publication date: January 29, 2015
    Inventors: Edmond J. LaVoie, Ajit Parhi, Yongzheng Zhang, Daniel S. Pilch, Malvika Kaul
  • Publication number: 20150031735
    Abstract: The present invention relates to solid forms of the N-methyl-D-glucamine (meglumine) salt of 6-carboxy-2-(3,5-dichlorophenyl)-benzoxazole and to methods for their preparation. The invention is also directed to pharmaceutical compositions containing at least one solid form and to the therapeutic or prophylactic use of such solid forms and compositions.
    Type: Application
    Filed: September 12, 2012
    Publication date: January 29, 2015
    Inventors: Richard Frederic Labaudiniere, MICHAEL HENRY O'Neill
  • Patent number: 8940764
    Abstract: Compositions and methods for treating macular degeneration and other forms of retinal disease whose etiology involves the accumulation of A2E and/or lipofuscin, and, more specifically, for preventing the formation and/or accumulation of A2E are disclosed.
    Type: Grant
    Filed: May 26, 2006
    Date of Patent: January 27, 2015
    Assignee: Aldexa Therapeutics, Inc.
    Inventors: Thomas A. Jordan, John E. Dowling, John Clifford Chabala
  • Publication number: 20150018388
    Abstract: The present invention relates to the identification of compounds and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided compounds.
    Type: Application
    Filed: December 11, 2013
    Publication date: January 15, 2015
    Inventors: Richard B. Silverman, Yinan Zhang
  • Publication number: 20150018398
    Abstract: Disclosed herein are methods useful for treating radiation damage in a subject.
    Type: Application
    Filed: July 15, 2014
    Publication date: January 15, 2015
    Inventors: Richard J. Pietras, Michael E. Jung
  • Publication number: 20150005283
    Abstract: The present invention provides compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 1, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Adrian Wai-Hing Cheung, Ryan Craig Schoenfeld, Weiya Yun, Shu-Hai Zhao
  • Publication number: 20140378493
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Application
    Filed: September 8, 2014
    Publication date: December 25, 2014
    Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha
  • Publication number: 20140378421
    Abstract: The present invention relates to novel compounds having ?2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
    Type: Application
    Filed: November 9, 2012
    Publication date: December 25, 2014
    Inventors: Jose Aiguade Bosch, Silvia Gual Roig, Maria Prat Quinones, Carlos Puig Duran
  • Publication number: 20140371278
    Abstract: Disclosed are compound of formula (I) and pharmaceutically accepted salts and prodrugs thereof, wherein each of R1, R2, R3, R4, R5, R6, X1 and X2 is as defined in the description. These compounds are protein kinases inhibitors, especially the inhibitors of Mek, which are useful in the treatment of cancers and inflammation of mammals. Disclosed are the treatment methods of cancers and inflammation of mammals as well as pharmaceutical compositions comprising the compounds described herein. The preparation of benzoheterocyclic compounds are disclosed. Disclosed are the preparation of potential drug candidates, such as benzooxazol, benzothiazol, benzothiadiazol and the like.
    Type: Application
    Filed: January 16, 2013
    Publication date: December 18, 2014
    Applicant: TIANJIN BINJIANG PHARMA, INC.
    Inventors: Hongqi Tian, Conghui Ji, Chunlei Liu, Li Kong, Ying Cheng, Gongchao Huang
  • Patent number: 8912186
    Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: December 16, 2014
    Assignee: Universitaet des Saarlandes
    Inventors: Matthias Engel, Wolfgang Fröhner, Adriane Stroba, Ricardo M. Biondi
  • Publication number: 20140364444
    Abstract: A fused heterocyclic compound the formula (1): wherein A1 represents —NR8—, and the like; A2 represents a nitrogen atom, and the like; A3 represents a nitrogen atom, and the like; R1 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R2, R3, R4, and R5 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more halogen atoms, and the like; R6 and R7 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R8 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group W, and the like; n represents 0, 1 or 2. The compound has an excellent activity of controlling pests.
    Type: Application
    Filed: August 21, 2014
    Publication date: December 11, 2014
    Inventors: Hayato TAKYO, Masaki TAKAHASHI, Takamasa TANABE, Yoshihiko NOKURA, Mai ITO, Atsushi IWATA
  • Publication number: 20140348746
    Abstract: The invention relates to a family of compounds that comprise fluorescent cyanine dyes. The compounds are near infrared absorbing heptamethine cyanine dyes with a 4,4-disubstituted cyclohexyl ring as part of the polymethine chromophore. The compounds are generally hydrophilic and can be chemically linked to biomolecules, such as proteins, nucleic acids, and therapeutic small molecules. The compounds can be used for imaging in a variety of medical, biological and diagnostic applications.
    Type: Application
    Filed: March 17, 2014
    Publication date: November 27, 2014
    Applicant: VisEn Medical, Inc.
    Inventor: Narasimhachari Narayanan
  • Patent number: 8895591
    Abstract: The present invention provides a compound represented by the formula which is useful as an agent for the prophylaxis or treatment of diseases related to the action of melatonin, or a salt thereof and the like.
    Type: Grant
    Filed: September 4, 2013
    Date of Patent: November 25, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Osamu Uchikawa, Tatsuki Koike, Yasutaka Hoashi, Takafumi Takai
  • Patent number: 8883833
    Abstract: The invention relates to substituted benzothiazoles, benzoxazoles—and their counterparts having pyridine and pyrimidine rings replacing the benzene ring—that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula I: in which A and B are carbocycles or heterocycles.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: November 11, 2014
    Assignee: Decode Genetics EHF
    Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Munagala Rao
  • Patent number: 8877773
    Abstract: Methods and compositions that down regulate the activity of orexins to treat panic disorder and panic-like responses associated with hypercapnic conditions are disclosed.
    Type: Grant
    Filed: October 21, 2010
    Date of Patent: November 4, 2014
    Inventors: Anantha Shekhar, Philip L. Johnson
  • Publication number: 20140322278
    Abstract: Compositions and methods are provided for modulating the physiological activation of tissue transglutaminase (TG2); which methods can include inhibiting the activation of TG2 associated with enteric inflammatory disorders, which disorders may include celiac disease, irritable bowel syndrome, Crohn's Disease, dermatitis herpetiformis, and the like. In other embodiments of the invention, methods are provided for reducing undesirable paracellular transport in enteric tissues, in particular the paracellular transport of molecules greater than about 500 mw, e.g. peptides, including without limitation immunogenic gluten peptides.
    Type: Application
    Filed: June 19, 2012
    Publication date: October 30, 2014
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Thomas DiRaimondo, Xi Jin, Cornelius Kloeck, Chaitan Khosla
  • Patent number: 8871738
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Grant
    Filed: October 25, 2012
    Date of Patent: October 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha
  • Publication number: 20140315945
    Abstract: The present invention relates to azole compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Applicant: EPIZYME, INC.
    Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
  • Publication number: 20140315881
    Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.
    Type: Application
    Filed: July 27, 2012
    Publication date: October 23, 2014
    Inventors: Erkan Baloglu, Gary J. Bohnert, Shomir GHOSH, Mercedes Lobera, Darby R. Schmidt, Leonard Sung
  • Publication number: 20140315963
    Abstract: [Problem] A compound which is useful as a dopamine D1 receptor positive allosteric modulator (D1 PAM) is provided. [Means for Solution] The present inventors have studied a compound which has a dopamine D1 receptor positive allosteric modulating activity and is useful as an active ingredient of a pharmaceutical composition for preventing and/or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like, and they have thus found that a heterocyclic acetamide compound has a dopamine D1 receptor positive allosteric modulating activity, thereby completing the present invention. The heterocyclic acetamide compound of the present invention has a dopamine D1 receptor positive allosteric modulating activity and can be used as an agent for preventing and/or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like.
    Type: Application
    Filed: April 18, 2014
    Publication date: October 23, 2014
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Ryota Shiraki, Takahiko Tobe, Shimpei Kawakami, Hiroyuki Moritomo, Makoto Ohmiya