Compounds that are agonists of muscarinic receptors and tha may be effective in treating pain, alzheimer's disease and/or schizophreniaCompounds of Formulae I, or pharmaceutically acceptable salts thereof: I wherein X, R1, R2 and R3 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.Formula i compound, its pharmacy acceptable salt, diastereomer, enantiomer or their mixture:whereinr 1be selected from c 6-10aryl, c 2-9heteroaryl, c 3-5heterocyclylalkyl, c 6-10aryl-c 1-3alkyl, c 2-9heteroaryl-c 1-3alkyl, c 3-5heterocyclylalkyl-c 1-3alkyl, c 3-6cycloalkyl, c 3-6cycloalkyl-c 1-3alkyl and c 1-6alkyl, wherein said c 6-10aryl, c 2-9heteroaryl, c 6-10aryl-c 1-3alkyl, c 6-10aryl-o-c 1-3alkyl, c 2-9heteroaryl-c 1-3alkyl, c 3-6cycloalkyl, c 3-6cycloalkyl-c 1-3alkyl and c 1-6alkyl is optional by one or more following group replacement: c that are selected from 6-10aryl, c 1-9heteroaryl, c 3-5heterocyclylalkyl, c 6-10aryl-c 1-3alkyl, c 6-10aryl-o-c 1-3alkyl, c 2-9heteroaryl-c 1-3alkyl, c 3-5heterocyclylalkyl-c 1-3alkyl ,-cn ,-sr ,-or ,-o (ch 2) m-or, r ,-c (=o)-r ,-co 2r ,-so 2r ,-so 2nr 2, halogen ,-no 2,-nr 2,-(ch 2) mnr 2,-(ch 2) mnhc (=o)-nr 2,-nhc (=o)-r ,-n[c (=o) r] 2,-(ch 2) mnhs (=o) 2-r ,-(ch 2) mnhc (=o)-r ,-(ch 2) mn[c (=o)-r] 2with-c (=o)-nr 2r 2and r 3be independently selected from c 1-6alkyl, c 2-6thiazolinyl and c 1-6alkoxyl group, wherein said c 1-6alkyl, c 2-6thiazolinyl and c 1-6alkoxyl group is optional by one or more amino, halogen, c of being selected from 1-6alkoxyl group and-group among the cn replaces; perhaps r 2and r 3form heterocyclylalkyl with the nitrogen that they connected, wherein said heterocyclylalkyl is optional by one or more following group replacement: c that are selected from 6-10aryl, c 2-9heteroaryl, c 3-6cycloalkyl, c 3-5heterocyclylalkyl, c 6-10aryl-c 1-3alkyl, c 2-9heteroaryl-c 1-3alkyl, c 3-5heterocyclylalkyl-c 1-3alkyl ,-cn ,-sr ,-or ,-(ch 2) mor, r ,-co 2r ,-so 2r ,-so 2nr 2, halogen ,-no 2,-nr 2,-(ch 2) mnr 2with-c (=o)-nr 2each r is hydrogen, c independently 1-6alkyl, c 2-6thiazolinyl or halo c 1-6alkyl; and x is selected from-c (=o)-,-c (=o)-nh-,-c (=o)-o-and-s (=o) 2-; condition is:when x be-c (=o)-and r 2and r 3when forming piperidyl with the nitrogen that they connected, r 1not 4-amino-5-chloro-2-alkoxyl phenyl, 4-amino-5-chloro-2-cycloalkyloxy phenyl, 4-amino-5-chloro-2-cycloalkyl-phenalkyloxy-, 4-butoxy phenyl, 3-butoxy phenyl, 4-pentyloxy phenyl, 4-isobutoxy phenyl, 4-benzyloxy phenyl and 7-(2, the 3-dihydro) benzofuryl.
무스카린성 수용체의 효능제이며, 통증, 알츠하이머병 및/또는 정신분열증 치료에 효과적일 수 있는 화합물 본 발명에서 화학식 I의 화합물 또는 그의 제약상 허용되는 염 뿐만 아니라 이들 화합물을 포함하는 염 및 제약 조성물이 제조된다. 이들은 요법, 특히 통증 관리에 유용하다. <화학식 I>  상기 식에서, X, R1, R2 및 R3은 명세서에 정의된 바와 같다.화학식 I의 화합물, 그의 제약상 허용되는 염, 부분입체이성질체, 거울상이성질체, 또는 이들의 혼합물. <화학식 I> [이미지] 상기 식에서, R1은 C6-10아릴, C2-9헤테로아릴, C3-5헤테로시클로알킬, C6-10아릴-C1-3알킬, C2-9헤테로아릴-C1-3알킬, C3-5헤테로시클로알킬-C1-3알킬, C3-6시클로알킬, C3-6시클로알킬-C1-3알킬 및 C1-6알킬로부터 선택되고, 여기서 상기 C6-10아릴, C2-9헤테로아릴, C6-10아릴-C1-3알킬, C6-10아릴-O-C1-3알킬, C2-9헤테로아릴-C1-3알킬, C3-6시클로알킬, C3-6시클로알킬-C1-3알킬 및 C1-6알킬은 C6-10아릴, C1-9헤테로아릴, C3-5헤테로시클로알킬, C6-10아릴-C1-3알킬, C6-10아릴-O-C1-3알킬, C2-9헤테로아릴-C1-3알킬, C3-5헤테로시클로알킬-C1-3알킬, -CN, -SR, -OR, -O(CH2)m-OR, R, -C(=O)-R, -CO2R, -SO2R, -SO2NR2, 할로겐, -NO2, -NR2, -(CH2)mNR2, -(CH2)mNHC(=O)-NR2, -NHC(=O)-R, -N[C(=O)R]2, -(CH2)mNHS(=O)2-R, -(CH2)mNHC(=O)-R, -(CH2)mN[C(=O)-R]2 및 -C(=O)-NR2로부터 선택된 하나 이상의 기로 임의로 치환되고; R2 및 R3은 C1-6알킬, C2-6알케닐 및 C1-6알콕시로부터 독립적으로 선택되고, 여기서 상기 C1-6알킬, C2-6알케닐 및 C1-6알콕시는 아미노, 할로겐, C1-6알콕시 및 -CN으로부터 선택된 하나 이상의 기로 임의로 치환되거나; 또는 R2 및 R3은 이에 연결되어 있는 질소와 함께 헤테로시클로알킬을 형성하고, 여기서 상기 헤테로시클로알킬은 C6-10아릴, C2-9헤테로아릴, C3-6시클로알킬, C3-5헤테로시클로알킬, C6-10아릴-C1-3알킬, C2-9헤테로아릴-C1-3알킬, C3-5헤테로시클로알킬-C1-3알킬, -CN, -SR, -OR, -(CH2)mOR, R, -CO2R, -SO2R, -SO2NR2, 할로겐, -NO2, -NR2, -(CH2)mNR2 및 -C(=O)-NR2로부터 선택된 하나 이상의 기로 임의로 치환되고; R은 각각 독립적으로 수소, C1-6알킬, C2-6알케닐 또는 할로겐화된 C1-6알킬이고; X는 -C(=O)-, -C(=O)-NH-, -C(=O)-O- 및 -S(=O)2-로부터 선택되고, 단, X가 -C(=O)-이고, R2 및 R3이 이에 연결되어 있는 질소와 함께 상기 피페르디닐을 형성하는 경우; R1은 4-아미노-5-클로로-2-알콕실페닐, 4-아미노-5-클로로-2-시클로알콕시페닐, 4-아미노-5-클로로-2-시클로알킬-알콕시-페닐, 4-부톡시페닐, 3-부톡시페닐, 4-펜틸옥시페닐, 4-이소부톡시페닐, 4-벤조일옥시페닐 및 7-(2,3-디히드로)벤조푸라닐이 아니다.