Estrogen receptor ligands. Part 9: Dihydrobenzoxathiin SERAMs with alkyl substituted pyrrolidine side chains and linkers
摘要:
A series of dihydrobenzoxathiin SERAMs with alkylated pyrrolidine side chains or alkylated linkers was prepared. Minor modifications in the side chain or linker resulted in significant effects on biological activity, especially in uterine tissue.
Estrogen receptor ligands. Part 9: Dihydrobenzoxathiin SERAMs with alkyl substituted pyrrolidine side chains and linkers
摘要:
A series of dihydrobenzoxathiin SERAMs with alkylated pyrrolidine side chains or alkylated linkers was prepared. Minor modifications in the side chain or linker resulted in significant effects on biological activity, especially in uterine tissue.
2-PYRIDINECARBOXAMIDE DERIVATIVE HAVING GK-ACTIVATING EFFECT
申请人:Hashimoto Noriaki
公开号:US20080090799A1
公开(公告)日:2008-04-17
Compounds of a formula (I) and their pharmaceutically-acceptable salts are disclosed. The compounds have glucokinase-activating effect and are therefore useful for treatment of diabetes and obesity.
R
1
and R
2
each independently represent a lower alkyl group; X
1
represent a group of a formula (II-1):
wherein:
R
11
and R
12
each independently represent a hydrogen atom or a lower alkyl group, or taken together with the nitrogen atom to which they bond, R
11
and R
12
may form a 4- to 7-membered nitrogen-containing aliphatic ring (one carbon atom constituting the 4- to 7-membered nitrogen-containing aliphatic ring may be replaced by an oxygen atom), or taken together with a carbon atom in (CH
2
)
m
, R
11
and R
12
may form a 4- to 7-membered nitrogen-containing aliphatic ring; m indicates an integer of from 1 to 3.
The present invention relates to a compound represented by the formula:
or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are each independently a lower alkyl group, X is CH or the like, and X1 is an aminoalkoxy group or the like, which has a glucokinase-activating effect and thus is useful in the treatment of diabetes, obesity, and the like.
[EN] QUINAZOLINE DERIVATIVES<br/>[FR] DERIVES DE QUINAZOLINE
申请人:ASTRAZENECA AB
公开号:WO2002016352A1
公开(公告)日:2002-02-28
The invention concerns quinazoline derivatives of Formula (I) wherein each of m, R?1, n, R2 and R3¿ have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease.
[EN] QUINAZOLINE DERIVATIVES FOR THE TREATMENT OF TUMOURS<br/>[FR] DERIVES DE LA QUINAZOLINE POUR LE TRAITEMENT DE TUMEURS
申请人:ASTRAZENECA AB
公开号:WO2001094341A1
公开(公告)日:2001-12-13
The invention concerns quinazoline derivatives of Formula (I) wherein each of Q1, Z, m, R?1, R2, R3 and Q2¿ have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease.
The invention concerns quinazoline derivatives of Formula (I) wherein each of Q
1
, Z, m, R
1
, R
2
, R
3
and Q
2
have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease.
1