ALLEN JENNIFER R.,HU ESSA,RZASA ROBERT M.,ZHONG WENGE,LIU QINGYIAN,FROHN MICHAEL J.,CHEN JIAN J.,RUMFELT SHANNON,PICKRELL ALEXANDER J.
申请号：
ARP110101668
公开号：
AR081627A1
申请日:
2011.05.13
申请国别(地区):
AR
年份:
2012
代理人:
摘要：
Compounds containing these substances and their preparation process. This method also provides methods for the treatment of treatable PDE10 inhibitory disorders or diseases, such as obesity, Huntington's disease, non insulin diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder and similar claim 1: formula compound (1),or a pharmaceutically acceptable salt thereof, characterized in that: X1 is N or CR6； X2 is N or CR2； X3 is N or CR3； X4 is N or CR6； X5 is N or CR6； wherein 1 to 2 of X1, X2, X3, X4 and X5 are N； R1 is halo, C1-8, C1-4 haloalk, -ORc, -N (Ra) C (= O) Rb, -C (= O) Ra, -C (= O) Rc, -C (= O ) -O-Ra, -NRaRc, -N (Rc) C (= O) Rb, -N (Ra) C (= O) Rc, -C (= O) NRaRb, -C (= O) NRaRc, or Alq C0-4-L1； wherein the C1-8 alq group is substituted by 0, 1, 2 or 3 groups which are halo, C1-3 haloalq, -OH, -Oalq C1-4, -NH2, -NHalq C1-4, -OC ( = O) C1-4, or -N (C1-4) C1-4； Y is an alq C0-4, -C (= O),So, O SO2； each R2 and R3 is an independent R1, h, halo, CN, oalq C1-4, Alq C1-4, haloalq C1-4, Alq c1-6o RA, C (= O) Alq C1-4, C (= O) NRA, Alq c0-4nhc (= O) Ra, or RC； or a ring containing x1, X2, X3, X4 and X5 can be replaced with a ring, or B (or C) ring,(3) (4)Among them, each ring a, ring B or ring C is a partially saturated or unsaturated carbon ring or unsaturated unsaturated unsaturated ring composed of 4 to 6 members, containing 0, 1, 2 or 3 heteroatoms； it is replaced by 0, 1 or 2 R10 groups； R4A is h, oh, halo, Alq C1-4, or haloaq C1-4； r4b is halo, CN, oalq C1-4, Alq C1-4, Alq C1-4, u Oxo； R5 es-alq c1-6ora, 5-6 member heteromorphic ring, 9-10 member unsaturated bicycle heteromorphic ring, or 11-15 member tricyclic heteromorphic ring； R5 is replaced by 0, 1, 2, 3 or 4 R8 groups； R6 is independent R1, h, halo, CN, ooalq C1-4, Alq C1-4 or haloaq C1-4； MES 0, 1, 2, 3 or 4；Each P and Q is independent of 0, 1, 2, 3, 4, 5 or 6； the sum of P and Q is 2 to 6； rings containing P and Q contain 0, 1 or 2 double links； RA is independent of H or RB； Rb is
