公开(公告)号：BG103900A

公开(公告)日：2000-06-30

申请号：BG10390099

申请日：1999-11-17

Applicant: BASF AG

Inventor： STEINER GERD ,  DULLWEBER UTA ,  STARCK DOROTHEA ,  BACH ALFRED ,  WICKE KARSTEN ,  TESCHENDORF HANS-JUERGEN ,  GARCIA-LADONA FRANCISCO-JAVIE ,  EMLING FRANZ

IPC: A61K31/495 ,  A61K31/519 ,  A61P25/00 ,  A61P25/24 ,  A61P43/00 ,  C07D495/04

Abstract: The invention relates to 3-substituted 3,4-dihydro-thieno-[2,3-d]pyrimidine derivatives with the formula where R1 & R2 are hydrogen or C1-C4-alkyl group, R3 optionally is mono- or disubstituted with halogen atoms C1-C4-alkyl, trifluormethyl, trifluoromethoxy, hydroxy, C1-C4 alkoxy, amino, monomethylamino, dimethylamino, cyano or nitrogroup, phenyl, pyridol, pyrimidinyl or pyrazinyl residue which optionally can be annelated with one benzene ring which optionally can be mono- or disubsituted with halogen atoms C1-C4-alkyl, nydroxy, trifluoromethyl, C1-C4-alkoxy, amino, cyano or nitrogroup and, optionally, it can contain one nitrogen atom or be annelated with 5- or 6-member ring which can contain 1 to 2 oxygen atoms, A is NH or oxgen atom, Y is the group CH2, CH2-CH2, CH2-CH2-CH2 or CH2-CH, Z is nitrogen atom or CH where the bond between Y and Z can be double, and n has the value of 2, 3 or 4. The invention also relates to physiologically compatible salts of 3-substituted 3,4-dihydrothieno[3,4-d]pyrimidine derivatives. 6 claims

公开(公告)号：BG103921A

公开(公告)日：2000-07-31

申请号：BG10392199

申请日：1999-11-24

Applicant: BASF AG

Inventor： STEINER GERD ,  DULLWEBER UTA ,  STARCK DOROTHEA ,  BACH ALFRED ,  WICKE KARSTEN ,  TESCHENDORF HANS-JUERGEN ,  GARCIA-LADONA FRANCISCO-JAVIE ,  EMLING FRANZ

IPC: A61K31/505 ,  A61K31/519 ,  A61P25/00 ,  A61P25/24 ,  A61P43/00 ,  C07D495/14

Abstract: The invention relates to 3-substituted 3,4,5,6,7,8-hexahydropyrido[3',4':4,5]thieno[2,3]pyrimidine derivatives with the formula where R1 is hydrogen, C1-C4-alkyl group, acetyl group, phenylalkyl-C1-C4-residue where the aromatic residue is optionally substituted with halogen, C1-C4-alkyl, trifluromethyl, hydroxy, C1-C4-alkoxy-, amino, cyano or nitrogroups or means phenylalkane resdue where the phenyl group can be substituted with halogen, R2 optionallly is mono- or disubstituted with halogen atoms, C1-C4-alkyl, trifluoromethyl, trifluoromethoxy, hydroxy, C1-C4-alkoxy, amino, monomethylamino, dimethylamino, cyano or nitrogroup, phenyl, pyridyl, pyrimidinyl or pyrazinyl residue which can optionally be annelated with one benzene ring which can optionally be mono- or disubstituted with halogen atoms, C1-C4-alkyl, hydroxy, trifluoromethyl, C1-C4-alkoxy, amino, cyano or nitrogroup, and optionally can contain 1 nitrogen atom or be annelated with 5- or 6-member ring which can contain from 1 to 2 oxygen atoms, A is NH or oxygen atom, Y is the group CH2, CH2-CH2, CH2-CH2-CH2 or CH2-CH, Z is nitrogen atom,carbon atom or CH where the bond bdtween Y and Z can be double, and n is the integer 2, 3 & 4. The invention also relates to physiologically acceptable salts of 3-substituted pyrido[3',4':4,5]-thieno[2,3-d]pyrimidine derivatives. The compounds show a high degree of affinity to the serotonin receptors 5-HT1B-, 5-HT1D- and 5-HT1A-. The affinity to these receptors is approximately the same or at least of the same order. Some of the compounds have good capacity for inhibiting the repeated binding of serotonin which is used in most of the antidepressants. 6 claims