An antitumor effect potentiator for potentiating one or more other antitumor agents, comprising, as an active ingredient, an imidazooxazine compound represented by Formula (I), or a pharmaceutically acceptable salt thereof, [structure] wherein A, B, C, and D represent Câ€”R 1a , Câ€”R 1b , Câ€”R 1c , and Câ€”R 1d , respectively, or one or two of A, B, C, and D represent an N atom; at least two of R 1a , R 1b , R 1c , and R 1d represent hydrogen, and the other(s) represent(s) halogen; cyano; C 1-6 alkyl that may have hydroxyl group(s) as substituent(s); C 1-6 alkoxy; carbonyl having, as a substituent, hydroxyl, amino, optionally substituted mono- or di-(C 1-6 alkyl)amino, or mono- or di-(C 1-6 alkoxy)amino; or an unsaturated heterocyclic group; R 2 represents phenyl, pyridyl, or thienyl; R 3 represents hydrogen, methyl, ethyl, or cyclopropyl; and R 4 represents hydrogen or hydroxy.

Claims

12 · 7 independent · depth 2

12 granted claims

›1.independentA method for potentiating one or more antitumor agents, comprising administering an imidazooxazine compound represented by Formula (I), or a pharmaceu…+3

›3.independentA method for potentiating one or more antitumor agents, comprising administering an imidazooxazine compound of any one of the following (a) to (t), or…

A method for potentiating one or more antitumor agents, comprising administering an imidazooxazine compound of any one of the following (a) to (t), or a salt thereof, as an active ingredient, in combination with one or more antitumor agents, to a patient in need of such treatment,n(a) trans-3-amino-1-cyclopropyl-3-(4-(10-fluoro-3-phenyl-5H-benzo[e]imidazo[1,2-c][1,3]oxazin-2-yl)phenyl)cyclobutanol,(b) trans-3-amino-1-cyclopropyl-3-(4-(10-fluoro-3-(pyridin-4-yl)-5H-benzo[e]imidazo[1,2-c][1,3]oxazin-2-yl)phenyl)cyclobutanol,(c) trans-3-amino-1-cyclopropyl-3-(4-(3-phenyl-5H-benzo[e]imidazo[1,2-c][1,3]oxazin-2-yl)phenyl)cyclobutanol,(d) trans-3-amino-1-cyclopropyl-3-(4-(10-methoxy-3-phenyl-5H-benzo[e]imidazo[1,2-c][1,3]oxazin-2-yl)phenyl)cyclobutanol,(e) trans-3-amino-1-cyclopropyl-3-(4-(9-methoxy-3-phenyl-5H-benzo[e]imidazo[1,2-c][1,3]oxazin-2-yl)phenyl)cyclobutanol,(f) trans-3-amino-1-cyclopropyl-3-(4-(8-methoxy-3-phenyl-5H-benzo[e]imidazo[1,2-c][1,3]oxazin-2-yl)phenyl)cyclobutanol,(g) trans-3-amino-1-cyclopropyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[2,3-e][1,3]oxazin-2-yl)phenyl)cyclobutanol,(h) trans-3-amino-1-methyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[2,3-e][1,3]oxazin-2-yl)phenyl)cyclobutanol,(i) trans-3-amino-1-ethyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[2,3-e][1,3]oxazin-2-yl)phenyl)cyclobutanol,(j) trans-3-amino-1-cyclopropyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenyl)cyclobutanol,(k) trans-3-amino-1-methyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenyl)cyclobutanol,(l) trans-3-amino-1-cyclopropyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[4,3-e][1,3]oxazin-2-yl)phenyl)cyclobutanol,(m) trans-3-amino-1-methyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[4,3-e][1,3]oxazin-2-yl)phenyl)cyclobutanol,(n) trans-3-amino-1-cyclopropyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,2-e][1,3]oxazin-2-yl)phenyl)cyclobutanol,(o) trans-3-amino-1-cyclopropyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrazino[2,3-e][1,3]oxazin-2-yl)phenyl)cyclobutanol,(p) trans-3-amino-3-(4-(9-(hydroxymethyl)-3-phenyl-5H-benzo[e]imidazo[1,2-c][1,3]oxazin-2-yl)phenyl)-1-methylcyclobutanol,(q) 2-(4-(trans-1-amino-3-hydroxy-3-methylcyclobutyl)phenyl)-3-phenyl-5H-benzo[e]imidazo[1,2-c][1,3]oxazine-9-carbonitrile,(r) trans-3-amino-1-methyl-3-(4-(3-phenyl-9-(1H-pyrazol-5-yl)-5H-benzo[e]imidazo[1,2-c][1,3]oxazin-2-yl)phenyl)cyclobutanol,(s) 2-(4-(trans-1-amino-3-hydroxy-3-methylcyclobutyl)phenyl)-N-methyl-3-phenyl-5H-benzo[e]imidazo[1,2-c][1,3]oxazine-8-carboxamide, and(t) 2-(4-(trans-1-amino-3-hydroxy-3-methylcyclobutyl)phenyl)-N-ethoxy-3-phenyl-5H-benzo[e]imidazo[1,2-c][1,3]oxazine-8-carboxamide.

›4.independentAn antitumor composition comprising an imidazooxazine compound or a pharmaceutically acceptable salt thereof in combination with one or more antitumor…+1

›5.independentA method for making an antitumor composition, comprising combining an imidazooxazine compound or a pharmaceutically acceptable salt thereof with one o…

›7.independentA pharmaceutical composition comprising an imidazooxazine compound or a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable carrie…

›8.independentA method for treating a malignant tumor in which AKT (serine/threonine-specific kinase) is frequently activated or highly expressed, comprising admini…+1

›9.independentA kit for the treatment of malignant tumors, comprising an imidazooxazine compound or a pharmaceutically acceptable salt thereof and one or more antit…

Classifications

7 codes

IPC · International Patent Classification

Section A — Human necessities

A61K31/337
A61K31/5383
A61K31/5365
A61K45/06
A61K39/00

Section C — Chemistry; metallurgy

C07D498/04
C07D498/14

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Kahsay Habte

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Type	Document	Date
related publication	US 20150164909 A1	18 Jun 2015

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