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标题翻译： Heteroarylsulfonamides和CCR2

公开(公告)号：EP2474532A1

公开(公告)日：2012-07-11

申请号：EP12162572.7

申请日：2006-01-13

申请人： ChemoCentryx, Inc.

发明人： Ungashe, Solomon , Pennell, Andrew M. K. , Punna, Sreenivas , Wei, Zheng , Wright, John Jessen , Zeng, Yibin , Badak, Arindrajit , Charvat, Trevor T. , Dairaghi, Daniel , Hanson, Derek , Jin, Jeff , Moore, Jimmie

IPC分类号： C07D213/02

CPC分类号： C07C311/21 , C07D213/48 , C07D213/61 , C07D213/643 , C07D213/70 , C07D213/73 , C07D213/76 , C07D213/79 , C07D213/81 , C07D213/89 , C07D241/22 , C07D263/32 , C07D401/04 , C07D405/04 , C07D409/12 , C07D413/06 , C07D413/10 , C07D417/12 , C07D471/04

摘要： A compound of the formula (I), or a salt thereof:

where
Ar is selected from the group consisting of substituted or unsubstituted C 6-10 aryl and substituted or unsubstituted 5- to 10-membered heteroaryl;
R 1 is selected from the group consisting of hydrogen, unsubstituted C 1 alkyl, substituted or unsubstituted C 3-8 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, and substituted or unsubstituted 3- to 10-membered heterocyclyl;
Y 1 is selected from the group consisting of -CR 2a -, -N-, and -N + (O) - -;
Y 2 is selected from the group consisting of -CR 2b -, -N-, and -N + (O) - -;
Y 3 is selected from the group consisting of -CR 2c -, -N-, and -N + (O) - -;
R 2a , R 2b , and R 2c are each independently selected from the group consisting of hydrogen, halogen, -CN, -C(O)R 3 , -CO 2 R 3 , -C(O)NR 3 R 4 , -OR 3 , - OC(O)R 3 , -OC(O)NR 3 R 4 , -SR 3 , -S(O)R 3 , -S(O) 2 R 3 , -S(O) 2 NR 3 R 4 , -NO 2 , -NR 3 R 4 , -NR 3 C(O)R 4 , -NR 3 C(O)OR 4 , -NR 3 S(O) 2 R 4 , -NR 3 C(O)NR 4 R 5 , substituted or unsubstituted C 1-8 alkyl, substituted or unsubstituted C 2-8 alkenyl, substituted or unsubstituted C 2-8 alkynyl, substituted or unsubstituted 3- to 10-membered heterocyclyl, substituted or unsubstituted C 6-10 aryl, and substituted or unsubstituted 5- to 10-membered heteroaryl;
R 3 , R 4 , and R 5 are each independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-8 alkyl, substituted or unsubstituted C 2-8 alkenyl, substituted or unsubstituted C 2-8 alkynyl, substituted or unsubstituted C 6-10 aryl, substituted or unsubstituted 5- to 10-membered heteroaryl, and substituted or unsubstituted 3- to 10-membered heterocyclyl;
R 3 and R 4 , R 4 and R 5 or R 3 and R 5 may, together with the atoms to which they are attached, form a substituted or unsubstituted 5-, 6-, or 7-membered ring;
Y 4 is selected from the group consisting of -N- and -N + (O) - -;
L is selected from the group consisting of a bond, -O-, -S-, -S(O)-, S(O) 2 -, - CR 6 R 7 -, -NR 8 -, -C(O)- and -NR 8 C(O)-;
R 6 and R 7 are each independently selected from the group consisting of hydrogen, halogen, substituted or unsubstituted C 1-8 alkyl, substituted or unsubstituted 3- to 10-membered heterocyclyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, -CN, -OR 9 , -NR 10 R 11 , -S(O)R 9 , and -S(O) 2 R 9 ;
R 6 and R 7 may, together with the carbon atom to which they are attached, form substituted or unsubstituted C 3-8 cycloalkyl or substituted or unsubstituted 3-to 10-membered heterocyclic ring;
R 9 is selected from the group consisting of hydrogen, substituted or unsubstituted C 1-8 alkyl, substituted or unsubstituted C 2-8 alkenyl, substituted or unsubstituted C 2-8 alkynyl, substituted or unsubstituted C 6-10 aryl, substituted or unsubstituted 5- to 10-membered heteroaryl, and substituted or unsubstituted 3- to 10-membered heterocyclyl;
R 10 and R 11 are each independently selected from the group consisting of substituted or unsubstituted C 1-8 alkyl, substituted or unsubstituted 3- to 10-membered heterocyclyl, substituted or unsubstituted C 6-10 aryl, substituted or unsubstituted 5- to 10-membered heteroaryl, substituted or unsubstituted C 2-8 alkenyl, and substituted or unsubstituted C 2-8 alkynyl;
R 10 and R 11 of -NR 10 R 11 may, together with the nitrogen, form a substituted or unsubstituted C 3-8 cycloalkyl or substituted or unsubstituted 3- to 10-membered heterocyclyl;
R 8 is selected from the group consisting of hydrogen, C(O)R 12 , S(O) 2 R 12 , CO 2 R 12 , substituted or unsubstituted C 1-8 alkyl, substituted or unsubstituted 3- to 10-membered heterocyclyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
R 12 is selected from the group consisting of substituted or unsubstituted C 1-8 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted 3- to 10-membered heterocyclyl, substituted or unsubstituted C 6-10 aryl, and substituted or unsubstituted 5- to 10-membered heteroaryl;
Z 1 is selected from the group consisting of substituted or unsubstituted C 6-10 aryl, substituted or unsubstituted 5- to 10-membered heteroaryl, substituted or unsubstituted 3- to 10-membered heterocyclyl, and -NR 13 R 14 ;
R 13 and R 14 are each independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-8 alkyl, substituted or unsubstituted C 2-8 alkenyl, substituted or unsubstituted C 2-8 alkynyl, substituted or unsubstituted 3- to 10-membered heterocyclyl, substituted or unsubstituted C 6-10 aryl, substituted or unsubstituted 5- to 10-membered heteroaryl, substituted or unsubstituted (C 1-4 alkyl)-(C 6-10 aryl), and substituted or unsubstituted (C 1-4 alkyl)-(5- to 10-membered heteroaryl);
R 13 and R 14 may, together with the nitrogen, form a substituted or unsubstituted 4-, 5-, 6-, or 7-membered heterocyclyl
with the proviso that compounds of formula CC are excluded:

where
X 14 is selected from the group consisting of -Cl, -NO 2 , -OCH 3 , -CH 3 , - NHC(O)CH 3 , and -CH 2 CH 2 -(phenyl);
R 65 is selected from the group consisting of hydrogen, substituted or unsubstituted C 1-4 alkyl, and substituted or unsubstituted -SO 2 (phenyl); and
R 60 is selected from the group consisting of -NR 61 CH 2 CH 2 OR 62 , - NR 61 CH 2 CH 2 NR 63 R 64 , -NR 61 CH 2 CH 2 SR 62 ,

where R 61 is selected from the group consisting of hydrogen and substituted or unsubstituted phenyl;
R 62 is selected from the group consisting of substituted or unsubstituted phenyl, and substituted or unsubstituted C 1-4 alkyl; and
R 63 and R 64 are each independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-8 alkyl, substituted or unsubstituted phenyl, substituted or unsubstituted -SO 2 (phenyl), - C(O)CH 3 , -C(O)C(O)OH, and -C(O) 2 C(CH 3 ) 3 .

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