| 主权项 |
1. A compound of formula Iwherein
Ar is selected from a group consisting of: wherein X is N;R3 is H, halogen, CN or —C(═O)—NH2; andR4 is selected from a group consisting of: wherein R7 is selected from a group consisting of H, CN, C1-6-alkyl, —O—(C1-3-alkyl), C2-4-alkynyl, C3-7-cycloalkyl, heterocyclyl, —(C1-3-alkyl)-heterocyclyl, —(C1-3-alkyl)-O-heterocyclyl, aryl, —(C1-3-alkyl)-aryl, 5- or 6-membered heteroaryl, —(C1-3-alkyl)-heteroaryl, —COOH, —(C═O)—O—(C1-6-alkyl), —(C═O)—N═S(═O)(C1-3-alkyl)2 and —(C═O)—NRN1RN2;wherein RN1 is H or C1-3-alkyl; andRN2 is selected from a group consisting of H, C1-6-alkyl, C2-5-alkynyl, C3-7-cycloalkyl, heterocyclyl, —(C1-3-alkyl)-heterocyclyl, —(C1-3-alkyl)-aryl and —SO2—(C1-3-alkyl);or RN1 and RN2 together with the N-atom to which they are attached form a azetidinyl, pyrrolidinyl, piperidinyl, 4-oxo-piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxo-thiomorpholinyl or 1-imino-1,4-thiazinane-1-oxide ring, which may be substituted with one OH, C1-3-alkyl or —O—C1-3-alkyl; and
wherein in R4, each heterocyclyl is selected from a group consisting of 4-, 5- or 6-membered saturated monocyclic ring systems containing 1, 2 or 3 heteroatoms independently of each other selected from the group consisting on O, S, N and NH, wherein one —CH2— group may be replaced by a —C(═O)— group and wherein each heterocyclyl group is optionally substituted with C1-3-alkyl;wherein in R4, each aryl is phenyl or naphthyl;wherein in R4, each heteroaryl is selected from a group consisting of 5- or 6-membered monocyclic heteroaromatic ring systems containing 1, 2 or 3 heteroatoms independently of each other selected from the group consisting on O, S, N and NH and is optionally substituted with C1-3-alkyl;wherein in R4, each alkyl is optionally substituted with 1 or more F or with one or two substituents independently selected from the group consisting of CN, OH, —O—(C1-3-alkyl), —O-tetrahydrofuranyl, NH2, —NH—(C═O)—(C1-3-alkyl), —NH—(C═O)—NH—(C1-3-alkyl) or —NH—SO2—(C1-3-alkyl); andwherein in R4, each cycloalkyl is optionally substituted with 1 or more F or one CN, OH, CF3, —O—(C1-3-alkyl) or ═O; and R8 and R9 are independently of each other selected from the group consisting of: H and C1-3-alkyl optionally substituted with 1-3 F or one OH or NH2; R1 is selected from a group consisting of: wherein R5 is selected from the group consisting of:
a) C1-3-alkyl, which is optionally substituted with a substituent selected from the group consisting of —O—(C1-3-alkyl), —O—C3-7-cycloalkyl, —O-heterocyclyl, C3-7-cycloalkyl, heterocyclyl and phenyl,
wherein each alkyl group is optionally substituted with one or more F; andb) C2-3-alkenyl, C2-3-alkynyl, C3-7-cycloalkyl, heterocyclyl, heteroaryl, and aryl; andR6 is C1-3-alkyl which is optionally substituted with one or more F,or wherein R5 and R6 together with the sulfur atom to which they are attached form a 4 to 7-membered saturated or partly unsaturated heterocycle that further to the sulfur atom may contain one additional heteroatom selected from the group consisting of O, S and NRN,
wherein RN is H, C1-3-alkyl, —C(═O)—(C1-3-alkyl), —C(═O)—O—(C1-4-alkyl), —C(═O)—(C1-3-alkyl)-O—(C1-4-alkyl), —C(═O)—NH2, —C(═O)—NH(C1-3-alkyl), —C(═O)—N(C1-3-alkyl)2 or —SO2(C1-4-alkyl);and wherein R5, R6 and the heterocycles formed by R5 and R6 together with the sulfur atom to which they are attached may each be independently substituted with halogen, CN, OH, NH2, —NH(C1-4-alkyl), —N(C1-4-alkyl)2, —NH—C(═O)—(C1-4-alkyl), —NH—C(═O)—O—(C1-4-alkyl), —NH—C(═O)—NH2, —NH—C(═O)—NH—(C1-4-alkyl), —NH—C(═O)—N(C1-4-alkyl)2, —N(C1-4-alkyl)-C(═O)—(C1-4-alkyl), —N(C1-4-alkyl)-C(═O)—O—(C1-4-alkyl), —N(C1-4-alkyl)-C(═O)—NH2, —N(C1-4-alkyl)-C(═O)—NH—(C1-4-alkyl), —N(C1-4-alkyl)-C(═O)—N(C1-4-alkyl)2, —O—(C1-4-alkyl), C1-6-alkyl, C3-7-cycloalkyl, heterocylcyl, heteroaryl, —C(═O)—NH2, —C(═O)—NH(C1-4-alkyl), —C(═O)—N(C1-4-alkyl)2, —COOH, —C(═O)—O—(C1-4-alkyl), —(C1-4-alkyl)-NH—C(═O)—(C1-4-alkyl); —SO—(C1-4-alkyl) or —SO2—(C1-4-alkyl); and R2 is selected from a group consisting of halogen, CN, OH, NH2, C1-3-alkyl, C2-3-alkenyl, C2-3-alkynyl, C3-5-cycloalkyl, —O—(C1-3-alkyl), —O-cyclopropyl and —S—C1-3-alkyl, wherein each alkyl group is optionally substituted with one or more F; and
wherein, if not otherwise specified, each alkyl group in the above definitions is linear or branched and may be substituted with one to three F;or a stereoisomer or salt thereof. |
