445490-79-9Relevant academic research and scientific papers
NOVEL NITROGEN-CONTAINING COMPOUND OR SALT THEREOF, OR METAL COMPLEX THEREOF
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, (2016/08/17)
The present invention provides a compound represented by the formula (1) or a salt thereof, or a complex of the compound or the salt with a metal, in the formula (1), A1 represents a chelate group; R1 represents a hydrogen atom or the like; R2 represents a hydrogen atom or the like; and Z1, Z2, Z3, Z4, and Z5 are the same or different and each represent a nitrogen atom or CR3 or the like wherein R3 represents a hydrogen atom or an optionally substituted C1-6 alkyl group or the like; L1 represents a group represented by the formula (3) wherein R13, R14, R15, and R16 are the same or different and each represent a hydrogen atom or the like; L2 represents an optionally substituted C1-6 alkylene group; and L3 represents an optionally substituted C1-6 alkylene group.
TREATMENT AGENT FOR DIAGNOSIS OR TREATMENT OF DISEASE ASSOCIATED WITH INTEGRIN
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, (2018/10/03)
PROBLEM TO BE SOLVED: To provide a treatment agent for diagnosis or treatment of disease associated with integrin. SOLUTION: A treatment agent comprises a complex of a compound represented by formula (1) or salt thereof and metal. In the formula (1), A1 is a chelate group; R1 and R2 independently represent H, alkyl, or an amino protective group; Z1-Z5 independently represent N or CR3; R3 is H or a substituted/unsubstituted C1-6 alkyl group or the like; L1 is a group represented by formula (3); L2 and L3 independently represent a substituted/unsubstituted C1-6 alkylene group. In the formula (3), R13-R16 independently represent H, alkyl or the like. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
Non-peptidic αvβ3 antagonists containing indol-1-yl propionic acids
Leonard, Kristi,Pan, Wenxi,Anaclerio, Beth,Gushue, Joan M.,Guo, Zihong,DesJarlais, Renee L.,Chaikin, Marge A.,Lattanze, Jennifer,Crysler, Carl,Manthey, Carl L.,Tomczuk, Bruce E.,Marugan, Juan Jose
, p. 2679 - 2684 (2007/10/03)
We describe the synthesis and structure/activity relationship of RGD mimetics that are potent inhibitors of the integrin αvβ 3. Indol-1-yl propionic acids containing a variety of basic moieties at the 5-position, as well as substitutions alpha and beta to the carboxy terminus were synthesized and evaluated. Novel compounds with improved potency have been identified.
Substituted indoles and their use as integrin antagonists
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, (2008/06/13)
The present invention relates to novel substituted indole compounds that are antagonists of alpha V (αv) integrins, for example αvβ3 and αvβ5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by αvβ3 and αvβ5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, D, X, W, a, m, n, i, j, k and v are defined herein.
