6-substituted benzoxazines

45 The compound of claim 1 selected from the group consisting of:

• 4-Fluoro-N-[2-((R)-indan-1-ylamino)-4H-benzo[d][1,3]oxazin-6-ylmethyl]-benzamide,
• (R)-Indan-1-yl-[6-(5-methyl-[1,2,4]oxadiazol-3-yl)-4H-benzo[d][1,3]oxazin-2-yl]-amine,
• (R)-Indan-1-yl-(6-vinyl-4H-benzo[d][1,3]oxazin-2-yl)-amine,
• N′-{2-[(3-cyclopropylphenyl)amino]-4H-benzo[d][1,3]oxazin-6-yl}-N,N-dimethylsulfamide,
• N6-Benzyl-N2-(3-cyclopropyl-phenyl)-4H-benzo[d][1,3]oxazine-2,6-diamine,
• 1-[2-(3-Cyclopropyl-phenylamino)-4H-benzo[d][1,3]oxazin-6-yl]-3-(1-isopropyl-piperidin-4-yl)-urea,
• N2—(R)-Indan-1-yl-N6-(5-trifluoromethyl-[1,3,4]oxadiazol-2-yl)-4H-benzo[d][1,3]oxazine-2,6-diamine,
• 1-[2-(2,2-Dimethyl-2,3-dihydro-benzofuran-7-ylamino)-4H-benzo[d][1,3]oxazin-6-yl]-3-isopropyl-urea,
• (R)-Indan-1-yl-[6-((E)-styryl)-4H-benzo[d][1,3]oxazin-2-yl]-amine, and
• rac-2-(4-Methoxy-2,3-dihydro-benzofuran-3-ylamino)-4H-benzo[d][1,3]oxazine-6-carbonitrile.

A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula I

• wherein
• X is a bond, —NH—, —NH—S(O)2—, —NH—CH2—, —CH2—, —NH—C(O)—, —CH2—NH—C(O)—, —NH—C(O)—CH2—, —NH—C(O)—CH2—NH—, —NRa—C(O)—NRb—, or —NH—S(O)2—NH—;
• R1 is halo;
• C1-7-alkyl, optionally substituted by OH, C1-7 alkoxy or CN;
• C1-7-alkoxy;
• NRaRb;
• —C(NH2)N(OH);
• cyano;
• nitro;
• cycloalkyl;
• heterocycloalkyl;
• aryl;
• heteroaryl;
• or
• vinyl;
• wherein each of said cycloalkyl, heterocycloalkyl, aryl and heteroaryl is optionally substituted by one or more halo, cyano, nitro, C1-7-alkyl, C1-7-haloalkyl, C1-7-hydroxyalkyl, C1-7-cyanoalkyl, C1-7-alkoxy, C1-7-alkoxy-alkyl, —NRaRb, or 3- to 7-membered monocyclic cycloalkyl;
• and
• wherein said vinyl is optionally substituted by phenyl or a 5- or 6-membered monocyclic heteroaryl;
• Y is a bond, —CH2— or —CH2—CH2—O—;
• R2 is cycloalkyl;
• heterocycloalkyl;
• aryl;
• heteroaryl;
• or
• 5- or 6-membered cycloalkyl or heterocycloalkyl, anellated with a benzo ring;
• wherein each of said cycloalkyl, heterocycloalkyl, aryl, heteroaryl, 5- or 6-membered cycloalkyl or heterocycloalkyl anellated with a benzo ring is optionally substituted by one or more halo, hydroxyl, C1-7-alkyl, C1-7-alkoxy, or 3- to 7-membered monocyclic cycloalkyl;
• and
• Ra and Rb are each independently hydrogen or C1-7-alkyl;
• or a pharmaceutically acceptable salt or ester thereof and a pharmaceutically acceptable carrier.