DR. MARQUARDT, TOBIAS,MONDRITZKI, THOMAS,DR. FREUDENBERGER, TILL,DR. KULLMANN, MAXIMILIAN ANDREAS,DR. WITTWER, MATTHIAS BEAT,DR. BRECHMANN, MARKUS,DR. TINEL, HANNA,DR. STRAUB, ALEXANDER,DR. BOULTADAKI
申请号:
ARP170102545
公开号:
AR109654A1
申请日:
2017.09.14
申请国别(地区):
AR
年份:
2019
代理人:
摘要:
Claim 1: consists of formula (1),X represents halogen; R1 represents hydrogen, or - nr8308; r83099;wherein R⁴ represents hydrogen, methyl, C₂₋₄ alkyl or C₃₋₆ cycloalkyl,where C₂₋₄ alkyl may be substituted with hydroxyl or even trisubstituted with fluorine and R⁵ represents C₁₋₆ alkyl,C₃₋₆ cycloalkyl,3 to 6 membered saturated heterocyclyl or C₁₋₄-sulfonyl alkyl, where C₁₋₆ alkyl,C₃₋₆ cycloalkyl and 3 to 6 membered saturated heterocyclyl may be up to trisubstituted, the same or different, with methyl, difluoromethyl, trifluoromethyl, hydroxyl, hydroxycarbonyl, oxo, methoxy, difluoromethoxy, trifluoromethoxy and cyano and further up to fluorinated tetrasubstituted, or and R⁵ together with the nitrogen atom to which they are attached form a 3 to 6 membered monocyclic or 6 to 10 membered saturated or partially unsaturated bicyclic heterocycle which may contain one or two more, same or different heteroatoms, of the group of N, O, S, SO and / or SO₂ as members of the ring,where the 3 to 6 membered monocyclic and 6 to 10 membered bicyclic heterocycle can each be substituted with 1 to 5 substituents independently selected from the C₁₋₄ alkyl group,2. Difluoromethane, trifluoroide, hydroxyl, hydrogen poisoning, oxo, alcox c832138;difluoromethoxy, trifluoromethoxy, cyano, C₁₋₃-carbonyl alkoxy, aminocarbonyl, mono-C₁₋₃-aminocarbonyloxy alkyl, -NHC (= O) R¹⁴A, -CH₂NHC (= O) R¹⁴B, -OC (= O) R¹⁵ and additionally up to tetrasubstituted with fluorine, wherein C₁₋₄ alkyl may be mono- or disubstituted, the same or different, with hydroxyl and C alco alkoxy and even tetrasubstituted with fluorine, R¹⁴A and R¹⁴B independently represent each other,C₁₋₃ alkyl or cyclopropyl, and wherein R¹⁵ represents C₁₋₄ alkyl;2. Represents a set of equations (2) or * - 1-ar 2,a. * indicates the connection point with the nitrogen atom of the rest of Amida, r8310; * represents c83218c83318324a;R⁶B represents hydrogen, C₁₋₄ alkyl,cyclopropyl, monofluoromethyl, difluoromethyl, trifluoromethyl, methoxymethy