Detail of "159635-49-1"

Reference

Preparation of indole-2-carboxamide derivatives as cytokine inhibitors

Preparation of indole-2-carboxamide derivatives as cytokine inhibitors. Gao, Donghong Amy; Moss, Neil; Wang, Ji; Wu, Jiang-Ping; Wu, Lifen; Xiong, Zhaoming (Boehringer Ingelheim Pharmaceuticals, Inc., USA).In this study，159635-49-1 is also used. U.S. Pat. Appl. Publ. US 2006046986 A1 2 Mar 2006, 57 pp. (English). (United States of America). CODEN: USXXCO. APPLICATION: US 2005-209234 23 Aug 2005. PRIORITY: US 2004-604254P 25 Aug 2004. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1 Compds. 159635-49-1 which is the cas registry number of one of substances is just one of reagents here. of formula (I) [n = 1-3; Ar = Q, Q1, each (un)substituted Ph or benzo-fused 5-7 membered heterocyclic ring; wherein one of A or B = N and the other = C, R1 is covalently attached to either A or B, and when nitrogen = N-R1, the double bond between A and B is not present; R1 = H, NO2, -N(Rc)2, J-C(O)-N(Rc)-, J-S(O)m-N(Rc)- (Rc = H, C1-6 alkyl); or R1 = cyano, C1-6 alkyl, C3-7 cycloalkyl, C1-5 alkoxyl or C3-7 cycloalkoxy, C1-5 alkylthiol or C3-7 cycloalkylthiol, C1-5 acyl, C1-5 alkoxycarbonyl, C1-5 acyloxy, C1-5 acylamino, etc.; R2 = H, halogen, C1-5 alkyl, C1-5 alkoxy, C1-5 alkyl-C1-5 alkoxy, HO, hydroxy-C1-5 alkyl, oxo, C1-5 alkyl-S(O)m-, (un)substituted amino; Rx = each (un)substituted C1-6 alkyl or C3-7 cycloalkyl; Q = N, (un)substituted CH2; Y = (un)substituted CH2, CH:CH, or NH, O, S(O)m (m = 0-2); X = CO, CH2, (un)substituted NH, O, S; Z1 = N, CH; Z2 = (un)substituted NH, O, CH2; Ry = H, C1-6 alkyl; Ry and R6 may combine to form a bridged group from the ring atoms to which they are attached; R3-R5 = H, C1-6 alkyl, halogen; R6 = O-J, CO-J, CO-O-J, J-S(O)m-NR7R8, J-S(O)m-, -C(O)H, -O-heterocycle , each (un)substituted CO-NH2, -CO-CO-NH2, NH2, C1-5 alkyl branched or unbranched, C2-5 alkenyl, C1-3 acyl, C1-3 alkyl(OH), oxo; J = C1-10 alkyl, (un)substituted carbocycle; m = 0-2], or pharmaceutically acceptable salts thereof are prepd. These compds. inhibit prodn. of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathol. conditions involving inflammation such as chronic inflammatory disease (no data). Thus, a soln. of triflate ester (II) (R = OSO2CF3) 37, Et piperazine-1-carboxylate 30, Pd(dppf)Cl2.CH2Cl2 10 mg in 2 mL degassed DMF was heated at 80° under CO (1 atom) overnight to give 48% II (R = Q1). ..

Preparation of indole-2-carboxamide derivatives as cytokine inhibitors

Preparation of indole-2-carboxamide derivatives as cytokine inhibitors. Gao, Donghong Amy; Moss, Neil; Wang, Ji; Wu, Jiang-Ping; Wu, Lifen; Xiong, Zhaoming (Boehringer Ingelheim Pharmaceuticals, Inc., USA).In this study，159635-49-1 is also used. U.S. Pat. Appl. Publ. US 2006046986 A1 2 Mar 2006, 57 pp. (English). (United States of America). CODEN: USXXCO. APPLICATION: US 2005-209234 23 Aug 2005. PRIORITY: US 2004-604254P 25 Aug 2004. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1 Compds. 159635-49-1 which is the cas registry number of one of substances is just one of reagents here. of formula (I) [n = 1-3; Ar = Q, Q1, each (un)substituted Ph or benzo-fused 5-7 membered heterocyclic ring; wherein one of A or B = N and the other = C, R1 is covalently attached to either A or B, and when nitrogen = N-R1, the double bond between A and B is not present; R1 = H, NO2, -N(Rc)2, J-C(O)-N(Rc)-, J-S(O)m-N(Rc)- (Rc = H, C1-6 alkyl); or R1 = cyano, C1-6 alkyl, C3-7 cycloalkyl, C1-5 alkoxyl or C3-7 cycloalkoxy, C1-5 alkylthiol or C3-7 cycloalkylthiol, C1-5 acyl, C1-5 alkoxycarbonyl, C1-5 acyloxy, C1-5 acylamino, etc.; R2 = H, halogen, C1-5 alkyl, C1-5 alkoxy, C1-5 alkyl-C1-5 alkoxy, HO, hydroxy-C1-5 alkyl, oxo, C1-5 alkyl-S(O)m-, (un)substituted amino; Rx = each (un)substituted C1-6 alkyl or C3-7 cycloalkyl; Q = N, (un)substituted CH2; Y = (un)substituted CH2, CH:CH, or NH, O, S(O)m (m = 0-2); X = CO, CH2, (un)substituted NH, O, S; Z1 = N, CH; Z2 = (un)substituted NH, O, CH2; Ry = H, C1-6 alkyl; Ry and R6 may combine to form a bridged group from the ring atoms to which they are attached; R3-R5 = H, C1-6 alkyl, halogen; R6 = O-J, CO-J, CO-O-J, J-S(O)m-NR7R8, J-S(O)m-, -C(O)H, -O-heterocycle , each (un)substituted CO-NH2, -CO-CO-NH2, NH2, C1-5 alkyl branched or unbranched, C2-5 alkenyl, C1-3 acyl, C1-3 alkyl(OH), oxo; J = C1-10 alkyl, (un)substituted carbocycle; m = 0-2], or pharmaceutically acceptable salts thereof are prepd. These compds. inhibit prodn. of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathol. conditions involving inflammation such as chronic inflammatory disease (no data). Thus, a soln. of triflate ester (II) (R = OSO2CF3) 37, Et piperazine-1-carboxylate 30, Pd(dppf)Cl2.CH2Cl2 10 mg in 2 mL degassed DMF was heated at 80° under CO (1 atom) overnight to give 48% II (R = Q1). ..