公开(公告)号：WO1996015100A1

公开(公告)日：1996-05-23

申请号：PCT/DK1995000444

申请日：1995-11-08

Applicant: NOVO NORDISK A/S ,  PELLICCIARI, Roberto ,  LUNEIA, Roberto ,  LOMBARDI, Grazia ,  MORONI, Flavio

Inventor： NOVO NORDISK A/S

IPC: C07C229/46

CPC classification number: C07D257/04 ,  C07C17/2637 ,  C07C45/30 ,  C07C45/46 ,  C07C61/39 ,  C07C63/49 ,  C07C229/50 ,  C07C2602/08 ,  C07C2602/10 ,  C07D209/42 ,  C07D307/84 ,  C07D333/68 ,  C07C22/04 ,  C07C47/546 ,  C07C49/84 ,  C07C49/792

Abstract: The present invention relates to therapeutically active heterocyclic compounds of formula (I), wherein n is 0, 1 or 2; and X is -O-, -S, -N(R )- or -CH2-; and R is H, NH2, NHR or OH; and R and R independently are H, COOH; COOR , CONH2, CONHR , CON(R )2, CONHSO2R or tetrazole; and R is H, OH, NH2, NHR ; CF3, C1-8-alkyl, C2-8-alkenyl, C2-8-alkynyl, C3-6-cycloalkyl, phenyl or C1-4-alkoxy; and R is H, C1-8-alkyl, C2-8-alkenyl, C2-8-alkynyl, phenyl or C3-6-cycloalkyl; and ring A can be partly or completely saturated or aromatic, or a salt thereof with a pharmaceutically acceptable acid or base, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system related to the metabotropic glutamate receptor system.

Abstract translation: 本发明涉及式（I）的治疗活性杂环化合物，其中n为0,1或2; 并且X是-O - ， - S，-N（R 5） - 或-CH 2 - ; 并且R 1是H，NH 2，NHR 5或OH; R 2和R 3独立地为H，COOH; COOR 5，CONH 2，CONHR 5，CON（R 5）2，CONHSO 2 R 5或四唑; 且R 4为H，OH，NH 2，NHR 5; CF 3，C 1-8烷基，C 2-8 - 烯基，C 2-8 - 炔基，C 3-6 - 环烷基，苯基或C 1-4 - 烷氧基; R 5为H，C 1-8 - 烷基，C 2-8 - 烯基，C 2-8 - 炔基，苯基或C 3-6 - 环烷基; 并且环A可以是部分或完全饱和的或芳族的，或其与药学上可接受的酸或碱的盐，其制备方法和包含该化合物的药物组合物。 该新化合物可用于治疗与代谢型谷氨酸受体系统相关的中枢神经系统疾病。

公开(公告)号：WO1996015099A1

公开(公告)日：1996-05-23

申请号：PCT/DK1994000421

申请日：1994-11-09

Applicant: NOVO NORDISK A/S ,  PELLICCIARI, Roberto ,  LUNEIA, Roberto ,  LOMBARDI, Grazia ,  MORONI, Flavio

Inventor： NOVO NORDISK A/S

IPC: C07C229/46

CPC classification number: C07D257/04 ,  C07C17/2637 ,  C07C45/30 ,  C07C45/46 ,  C07C61/39 ,  C07C63/49 ,  C07C229/50 ,  C07C2602/08 ,  C07C2602/10 ,  C07D209/42 ,  C07D307/84 ,  C07D333/68 ,  C07C22/04 ,  C07C47/546 ,  C07C49/84 ,  C07C49/792

Abstract: The present invention relates to therapeutically active heterocyclic compounds of formula (I) wherein n is 0, 1 or 2; and X is -O-, -S, -N(R )- or -CH2-; and R is H, NH2, NHR or OH; and R and R independently are H, COOH, COOR , CONH2, CONHR , CON(R )2, CONHSO2R or tetrazole; and R is H, OH, NH2, NHR , CF3, C1-8-alkyl, C2-8-alkenyl, C2-8-alkynyl, C3-6-cycloalkyl, phenyl or C1-4-alkoxy; and R is H, C1-8-alkyl, C2-8-alkenyl, C2-8-alkynyl, phenyl or C3-6-cycloalkyl; and ring A can be partly or completely saturated or aromatic, or a salt thereof with a pharmaceutically acceptable acid or base, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system related to the metabotropic glutamate receptor system.

Abstract translation: 本发明涉及式（I）的治疗活性杂环化合物，其中n为0,1或2; 并且X是-O - ， - S，-N（R 5） - 或-CH 2 - ; 并且R 1是H，NH 2，NHR 5或OH; R 2和R 3独立地是H，COOH，COOR 5，CONH 2，CONHR 5，CON（R 5）2，CONHSO 2 R 5或四唑; 和R 4是H，OH，NH 2，NHR 5，CF 3，C 1-8烷基，C 2-8 - 烯基，C 2-8 - 炔基，C 3-6 - 环烷基，苯基或C 1-4 - 烷氧基 ; R 5为H，C 1-8 - 烷基，C 2-8 - 烯基，C 2-8 - 炔基，苯基或C 3-6 - 环烷基; 并且环A可以是部分或完全饱和的或芳族的，或其与药学上可接受的酸或碱的盐，其制备方法和包含该化合物的药物组合物。 该新化合物可用于治疗与代谢型谷氨酸受体系统相关的中枢神经系统疾病。