On August 8, 2002, Lu, Tianbao; Lafrance, Louis Vincent; Markotan, Thomas P.; Marugan, Juan Jose; Marder, Victor J.; U’Prichard, David C.; Anaclerio, Beth M.; Guo, Zihong; Pan, Wenxi; Leonard, Kristi A. published a patent.Computed Properties of 445490-78-8 The title of the patent was Preparation of indoles and their use as αvβ3 and αvβ5 integrin antagonists. And the patent contained the following:
Title compounds I [R1-R5 = H, halo, alkyl, etc.; R6-R9 = H, alkyl, hydroxyalkyl, etc.; R10-R13 = H, OH, alkyl, etc.; R14 = H, or a functionality that acts as a prodrug; X = O, S, CH2, etc.; a, k, v = 0, 1; i, j, m, n = 0-4], their pharmaceutically acceptable salts, prodrugs and formulations were prepared For example, hydrogenation of acrylic ester II, prepared from 7-[2-[1-(2-Methoxycarbonyl-1-(pyridin-3-yl)vinyl)-1H-indol-5-yloxy]ethyl]-3,4-dihydro-2H-[1,8]naphthyridine-1-carboxylic acid tert-Bu ester and pyridin-3-ylpropynoic acid Me ester, followed by BOC deprotection, and ester hydrolysis provided claimed indole III. Indole III inhibited human αvβ3-vitronectin interaction at an IC50 of 0.24 nM, studies for an addnl. 6 examples are provided, ranging in values from 670 to 0.24 nM. Compounds I may be used in treatment of pathol. conditions mediated by αvβ3 and αvβ5 integrins, including such conditions as tumor growth, inflammation, rheumatoid arthritis, etc.. The experimental process involved the reaction of tert-Butyl 7-(2-hydroxyethyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxylate(cas: 445490-78-8).Computed Properties of 445490-78-8
The Article related to preparation indole integrin antagonist antitumor antiinflammatory antirheumatic, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Computed Properties of 445490-78-8
Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem