公开(公告)号：EP1496059A1

公开(公告)日：2005-01-12

申请号：EP03712828.7

申请日：2003-03-24

申请人： Kyorin Pharmaceutical Co., Ltd.

发明人： SETO, Shigeki ,  TANIOKA, Asao ,  IKEDA, Makoto ,  IZAWA, Shigeru

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61P1/02 ,  A61P1/04 ,  A61P1/08 ,  A61P11/06 ,  A61P11/14 ,  A61P13/00 ,  A61P19/02 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P29/00 ,  A61P37/08 ,  A61P39/00 ,  A61P43/00

CPC分类号： C07D487/04

摘要： A novel fused bicyclic pyrimidine derivative or a salt thereof that acts as a tachykinin receptor antagonist and, in particular, as an NK1 receptor antagonist is represented by the following general formula (1):
wherein the rings A and B are each a benzene ring having 1 to 3 substituents (any adjacent two of which may be bound to one another to form a ring); the ring C is a nitrogen-containing ring; R is a hydrogen atom, a C 1 to C 6 alkyl group, a C 1 to C 6 alkylcarbonyl group, or a C 1 to C 6 alkylsulfonyl group; m is 1 or 2; and n is 2 or 3.

摘要翻译： 作为速激肽受体拮抗剂，特别是作为NK 1受体拮抗剂起作用的新型稠合双环嘧啶衍生物或其盐，由以下通式（1）表示：其中环A和B各自为具有 1至3个取代基（其中任何相邻的两个可以彼此结合形成环）; 环C是含氮环; R为氢原子，C1-C6烷基，C1-C6烷基羰基或C1-C6烷基磺酰基; m是1或2; 和n是2或3。

公开(公告)号：EP1489083B1

公开(公告)日：2007-06-06

申请号：EP03712827.9

申请日：2003-03-24

申请人： KYORIN PHARMACEUTICAL CO., LTD.

发明人： SETO, Shigeki ,  TANIOKA, Asao ,  IKEDA, Makoto ,  IZAWA, Shigeru

IPC分类号： C07D498/04 ,  A61K31/496 ,  A61K31/551 ,  A61K31/553 ,  A61P1/00 ,  A61P1/04 ,  A61P1/08 ,  A61P11/06 ,  A61P11/14 ,  A61P13/00 ,  A61P13/02 ,  A61P19/02 ,  A61P25/02 ,  A61P25/04 ,  A61P25/06 ,  A61P29/00 ,  A61P43/00 ,  A61P13/10

CPC分类号： C07D498/04

摘要： A novel fused bicyclic pyridine derivative represented by the following general formula (1), which has an antagonistic effect on tachykinin receptors, especially on an NK1 receptor. It is a fused bicyclic pyridine derivative represented by the general formula (1): (1) (wherein rings A and B each represents a benzene ring optionally having one to three substituents (two adjacent substituents may be bonded to each other to form a ring) each independently selected among halogen atoms, optionally substituted C1-6 alkyls, and optionally substituted C1-6 alkoxys; R represents C1-6 alkylsulfonyl, C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, or formyl; m is 1 or 2; n is 2 or 3; and q is 1 or 2) or a salt of the derivative.

公开(公告)号：EP1457493A1

公开(公告)日：2004-09-15

申请号：EP02786049.3

申请日：2002-12-06

申请人： Kyorin Pharmaceutical Co., Ltd.

发明人： SETO, Shigeki ,  TANIOKA, Asao ,  IKEDA, Makoto ,  IZAWA, Shigeru

IPC分类号： C07D498/04 ,  A61K31/4353 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/553 ,  A61P1/00 ,  A61P1/02 ,  A61P1/04 ,  A61P1/08 ,  A61P11/06 ,  A61P11/14 ,  A61P13/00 ,  A61P13/10 ,  A61P19/02 ,  A61P25/04 ,  A61P25/06 ,  A61P29/00 ,  A61P43/00

CPC分类号： C07D498/04

摘要： A novel fused bicyclic pyridine derivative or a salt thereof that acts as a tachykinin receptor antagonist, in particular as an NK1 receptor antagonist, is represented by the following general formula (1):
   wherein the rings A and B are each a benzene'ring which may have 1 to 3 substituents (any adjacent two of which may be bound to one another to form a ring);
   the ring C is a nitrogen-containing ring having a hydrogen atom substituted with a nitrogen atom;
   R 1 and R 2 are each independently a hydrogen atom, a C 1 to C 6 alkyl group, a C 1 to C 6 alkylsulfonyl group, a C 1 to C 6 alkylcarbonyl group, or a C 1 to C 6 alkoxycarbonyl group, or R 1 and R 2 are bound to one another to form the ring D; m is 1 or 2; n is 2 or 3; and q is an integer from 1 to 4.

摘要翻译： 用作速激肽受体拮抗剂，特别是作为NK1受体拮抗剂的新型稠合双环吡啶衍生物或其盐由以下通式（1）表示：其中环A和B各自为苯 '环，其可以具有1至3个取代基（其中相邻的两个可以彼此结合形成环）; 环C是具有被氮原子取代的氢原子的含氮环; R 1和R 2各自独立地为氢原子，C 1至C 6烷基，C 1至C 6烷基磺酰基，C 1至C 6烷基羰基或C 1至C 6烷氧基羰基，或R 1， 和R 2彼此结合形成环D; m为1或2; n为2或3; q为1〜4的整数。

公开(公告)号：EP1473295B1

公开(公告)日：2009-04-01

申请号：EP03700567.5

申请日：2003-01-15

申请人： Kyorin Pharmaceutical Co., Ltd.

发明人： SETO, Shigeki ,  TANIOKA, Asao ,  IKEDA, Makoto ,  IZAWA, Shigeru

IPC分类号： C07D498/04 ,  A61K31/519 ,  A61K31/553 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61P1/02 ,  A61P1/04 ,  A61P1/08 ,  A61P11/06 ,  A61P11/14 ,  A61P13/00 ,  A61P13/10 ,  A61P15/00 ,  A61P19/02 ,  A61P25/04 ,  A61P25/06 ,  A61P29/00 ,  A61P43/00

CPC分类号： C07D498/04 ,  A61K31/5365

摘要： It is intended to provide novel fused bicyclic pyrimidine derivatives represented by the general formula (1), which have a tachykinin receptor antagonism, in particular, an NK1 receptor antagonism, or salts thereof: (1) wherein the rings A and B represent each a benzene ring optionally having 1 to 3 substituents (wherein 2 adjacent substituents may be bonded to each other to form a ring); the ring C represents a nitrogen-containing ring; m is 1 or 2; and n is 2 or 3.

公开(公告)号：EP1496059B1

公开(公告)日：2007-08-15

申请号：EP03712828.7

申请日：2003-03-24

申请人： KYORIN PHARMACEUTICAL CO., LTD.

发明人： SETO, Shigeki ,  TANIOKA, Asao ,  IKEDA, Makoto ,  IZAWA, Shigeru

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61P1/02 ,  A61P1/04 ,  A61P1/08 ,  A61P11/06 ,  A61P11/14 ,  A61P13/00 ,  A61P19/02 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P29/00 ,  A61P37/08 ,  A61P39/00 ,  A61P43/00

CPC分类号： C07D487/04

摘要： It is intended to provide novel fused bicyclic pyrimidine derivatives represented by the following general formula (1) which have antagonism to tachykinin receptors, in particular, NK1 receptor antagonism. Namely, fused bicyclic pyrimidine derivatives represented by the following general formula (1) or salts thereof: (1) wherein the rings A and B represent each a benzene ring optionally having 1 to 3 substituents (wherein two adjacent substituents may be bonded to each other to form a ring); the ring C represents a nitrogen-containing ring; R represents hydrogen, C1-6 alkyl, C1-6 alkylcarbonyl or C1-6 alkylsulfonyl; m is 1 or 2; and n is 2 or 3.

公开(公告)号：EP1489083A1

公开(公告)日：2004-12-22

申请号：EP03712827.9

申请日：2003-03-24

申请人： Kyorin Pharmaceutical Co., Ltd.

发明人： SETO, Shigeki ,  TANIOKA, Asao ,  IKEDA, Makoto ,  IZAWA, Shigeru

IPC分类号： C07D498/04 ,  A61K31/496 ,  A61K31/551 ,  A61K31/553 ,  A61P1/00 ,  A61P1/04 ,  A61P1/08 ,  A61P11/06 ,  A61P11/14 ,  A61P13/00 ,  A61P13/02 ,  A61P19/02 ,  A61P25/02 ,  A61P25/04 ,  A61P25/06 ,  A61P29/00 ,  A61P43/00 ,  A61P13/10

CPC分类号： C07D498/04

摘要： A fused bicyclic pyridine derivative represented by the following general formula (1), or a salt thereof:
   wherein the rings A and B are each a benzene ring, which may have 1 to 3 substituents (any adjacent two of which may be bound to one another to form a ring) that are each independently selected from the group consisting of a halogen atom, a substituted or unsubstituted C 1 to C 6 alkyl group, and a substituted or unsubstituted C 1 to C 6 alkoxyl group;

R is a C 1 to C 6 alkylsulfonyl group, a C 1 to C 6 alkylcarbonyl group, a C 1 to C 6 alkoxycarbonyl group, or a formyl group;
m is 1 or 2;
n is 2 or 3; and
q is 1 or 2.

摘要翻译： 由以下通式（1）表示的稠合双环吡啶衍生物或其盐：其中环A和B各自为苯环，其可以具有1至3个取代基（其中相邻的两个可以是 彼此结合形成环），其各自独立地选自卤素原子，取代或未取代的C1至C6烷基和取代或未取代的C1至C6烷氧基; R是C1至C6烷基磺酰基，C1至C6烷基羰基，C1至C6烷氧基羰基或甲酰基; m为1或2; n为2或3; q为1或2。

公开(公告)号：EP1473295A1

公开(公告)日：2004-11-03

申请号：EP03700567.5

申请日：2003-01-15

申请人： Kyorin Pharmaceutical Co., Ltd.

发明人： SETO, Shigeki ,  TANIOKA, Asao ,  IKEDA, Makoto ,  IZAWA, Shigeru

IPC分类号： C07D498/04 ,  A61K31/519 ,  A61K31/553 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61P1/02 ,  A61P1/04 ,  A61P1/08 ,  A61P11/06 ,  A61P11/14 ,  A61P13/00 ,  A61P13/10 ,  A61P15/00 ,  A61P19/02 ,  A61P25/04 ,  A61P25/06 ,  A61P29/00 ,  A61P43/00

CPC分类号： C07D498/04 ,  A61K31/5365

摘要： A novel fused bicyclic pyrimidine derivative or a salt thereof that acts as a tachykinin receptor antagonist and, in particular, as an NK1 receptor antagonist is represented by the following general formula (1):
wherein the rings A and B are each a benzene ring having 1 to 3 substituents (any adjacent two of which may be bound to one another to form a ring); the ring C is a nitrogen-containing ring; m is 1 or 2; and n is 2 or 3.

摘要翻译： 用作速激肽受体拮抗剂，特别是作为NK1受体拮抗剂的新型稠合双环嘧啶衍生物或其盐由以下通式（1）表示：其中环A和B各自为 苯环具有1至3个取代基（任何相邻的两个可以彼此结合形成环）; 环C是含氮环; m为1或2; n为2或3。