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Title:
THERAPEUTIC AGENT FOR OCULAR DISEASE OR PROPHYLACTIC AGENT FOR OCULAR DISEASE
Document Type and Number:
WIPO Patent Application WO/2015/060208
Kind Code:
A1
Abstract:
3-[(3S,4R)-3-methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile suppresses increases in retinal blood vessel permeability induced by VEGF and therefore can be used as an active component in therapeutic agents or prophylactic agents for a variety of ocular diseases to which VEGF contributes, such as age-related macular degeneration, diabetic retinopathy, macular edema, neovascular maculopathy, retinal vein occlusion, and neovascular glaucoma.

Inventors:
OKIGAMI HIROMI (JP)
KUROSE TATSUJI (JP)
FUJISAWA KOUSHI (JP)
KIKKAWA CHINAMI (JP)
Application Number:
PCT/JP2014/077651
Publication Date:
April 30, 2015
Filing Date:
October 17, 2014
Export Citation:
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Assignee:
JAPAN TOBACCO INC (JP)
International Classes:
A61K31/519; A61K9/08; A61P3/10; A61P9/10; A61P27/02; A61P27/06; A61P43/00
Foreign References:
JP2011046700A2011-03-10
JP2013500977A2013-01-10
JP2012176930A2012-09-13
US20090082470A12009-03-26
JP2011046700A2011-03-10
Other References:
KANAKO IZUMI-NAGAI ET AL.: "Interleukin-6 Receptor-Mediated Activation of Signal Transducer and Activator of Transcription-3 (STAT3) Promotes Choroidal Neovascularization", THE AMERICAN JOURNAL OF PATHOLOGY, vol. 170, no. ISSUE, 2007, pages 2149 - 2158, XP055339393
HAIBO WANG ET AL.: "VEGF-Mediated STAT3 Activation Inhibits Retinal Vascularization by Down-Regulating Local Erythropoietin Expression", THE AMERICAN JOURNAL OF PATHOLOGY, vol. 180, no. ISSUE, 2012, pages 1243 - 1253, XP055237244
CRAWFORD, Y: "VEGF inhibition: insights from preclinical and clinical studies", CELL TISSUE RES, vol. 335, no. 1, January 2009 (2009-01-01), pages 261 - 269, XP019658518
DVORAK, HF ET AL.: "Vascular permeability factor/vascular endothelial growth factor and the significance of microvascular hyperpermeability in angiogenesis", CURR TOP MICROBIOL IMMUNOL., vol. 237, 1999, pages 97 - 132
XU, Q ET AL.: "Sensitive blood-retinal barrier breakdown quantitation using Evans blue", INVEST OPHTHALMOL VIS SCI., vol. 42, no. 3, March 2001 (2001-03-01), pages 789 - 794
EDELMAN, JL ET AL.: "Corticosteroids inhibit VEGF-induced vascular leakage in a rabbit model of blood-retinal and blood-aqueous barrier breakdown", EXP EYE RES., vol. 80, no. 2, February 2005 (2005-02-01), pages 249 - 258, XP004723793, DOI: doi:10.1016/j.exer.2004.09.013
See also references of EP 3061455A4
Attorney, Agent or Firm:
KOSEKI, KOSHI (JP)
Yukifumi Koseki (JP)
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