摘要:
Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and/or V1a receptor antagonists. Pharmaceutical compositions comprising such compounds are useful in the treatment of, inter alia, primary dysmenorrhoea.
摘要:
Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and/or V1a receptor antagonists. Pharmaceutical compositions comprising such compounds are useful in the treatment of, inter alia, primary dysmenorrhoea.
摘要翻译:根据通式1的新型化合物,其中G 1是NR 5 R 6或作为特异性OT受体激动剂的融合多环基团和/ 或V 1a受体拮抗剂。 包含这些化合物的药物组合物可用于治疗尤其是原发性痛经。
摘要:
The present invention concerns compounds inter alia according to general formula 1a. Compounds according to the invention are vasopressin V1a receptor antagonists. Pharmaceutical compositions of the compounds are useful as treatment of dysmenorrhoea.
摘要:
The present invention concerns compounds inter alia according to general formula 1a. Compounds according to the invention are vasopressin V1a receptor antagonists. Pharmaceutical compositions of the compounds are useful as treatment of dysmenorrhoea.
摘要:
The invention provides cyclopropanecarboxylic acid 4-(6-chloro-3-methyl-4,10-dihydro-3H-2,3,4,9-tetraazabenzo[f]azulene-9-carbonyl)-2-fluoro-benzylamide para-toluenesulphonate, pharmaceutical compositions containing it, and its use in therapy.
摘要:
Compounds according to general formula 1, wherein A1-A3 are selected from A5 and A6 where A5 is either ═CR13— or ═N— and A6 is —NR14—, —O— or —S—; A4 is either a covalent bond or A5, provided that when A4 is a covalent bond one of A1-A3 must be A6 and the other two must be A5 and when A4 is A5 then all of A1-A3 must be A5; R1 is selected from H, NHY′ and COY2, in which case R2 is H, or R1 and R2 may both be methyl or together represent ═O; R3, R4 and R5 are each independently selected from H and lower alkyl groups; R6, R7, R8, R9, R10, R11 and R12 are each independently selected from H, lower alkyl groups, NH2, halogens (F, Cl and Br) O-alkyl, CH2NM2 and CF3; R13 is selected from H, F, Cl Br, NO2, NH2, OH, Me, Et, OMe, NMe2 and CF3; R14 is selected from H, methyl and ethyl; W is selected from ═CH— and ═N—; X is selected from CH2, O, S, SO2, NH and N lower alkyl; Y1 is selected from CO-lower alkyl, CO(CH2)bY3, CO(CH2)bCOY3 and CO(CH)NHCOY3, where b is 1-3; Y2 is selected from OR15, NR16R17 and NH(CH2)CCOY3, where c is 1-3; Y3 is selected from OR15 and NR16R17; R15 is selected from H, lower alkyl and (CH2)aR16, where a is 0-4; R16 and R17 are each independently selected from H, lower alkyl and (CH2)aR16 or together are —(CH2)2-Z-(CH2)2—; R18 is OH a phenyl group or an aromatic heterocycle selected from pyridyl, pyrimidinyl, pyrazinyl, furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, triazolyl, oxadiazolyl and thiadiazolyl, each of which may optionally have a lower alkyl group substituent; and Z is selected from O, CH2, S, SO2, NH and N-lower alkyl, are new. They are useful in the treatment of breast and prostate cancer, endometriosis and benign prostate hyperplasia, in the regulation of fertility, and in in vitro fertilisation.
摘要:
Compounds according to general formula 1, wherein A1-A3 are selected from A5 and A6 where A5 is either ═CR13— or ═N— and A6 is —NR14—, —O— or —S—; A4 is either a covalent bond or A5, provided that when A4 is a covalent bond one of A1-A3 must be A6 and the other two must be A5 and when A4 is A5 then all of A1-A3 must be A5; R1 is selected from H, NHY′ and COY2, in which case R2 is H, or R1 and R2 may both be methyl or together represent ═O; R3, R4 and R5 are each independently selected from H and lower alkyl groups; R6, R7, R8, R9, R10, R11 and R12 are each independently selected from H, lower alkyl groups, NH2, halogens (F, Cl and Br) O-alkyl, CH2NM2 and CF3; R13 is selected from H, F, Cl, Br, NO2, NH2, OH, Me, Et, OMe, NMe2 and CF3; R14 is selected from H, methyl and ethyl; W is selected from ═CH— and ═N—; X is selected from CH2, O, S, SO2, NH and N-lower alkyl; Y1 is selected from CO-lower alkyl, CO(CH2)bY3, CO(CH2)bCOY3 and CO(CH2)bNHCOY3, where b is 1-3; Y2 is selected from OR15, NR16R17 and NH(CH2)cCOY3, where c is 1-3; Y3 is selected from OR15 and NR16R17; R15 is selected from H, lower alkyl and (CH2)aR16, where a is 0-4; R16 and R17 are each independently selected from H, lower alkyl and (CH2)aR16 or together are —(CH2)2-Z-(CH2)2—; R18 is OH, a phenyl group or an aromatic heterocycle selected from pyridyl, pyrimidinyl, pyrazinyl, furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, triazolyl, oxadiazolyl and thiadiazolyl, each of which may optionally have a lower alkyl group substituent; and Z is selected from O, CH2, S, SO2, NH and N-lower alkyl, are new. They are useful in the treatment of breast and prostate cancer, endometriosis and benign prostate hyperplasia, in the regulation of fertility, and in in vitro fertilisation.
摘要:
The invention provides cyclopropanecarboxylic acid 4-(6-chloro-3-methyl-4,10-dihydro-3H-2,3,4,9-tetraazabenzo[f]azulene-9-carbonyl)-2-fluoro-benzylamide para-toluenesulphonate, pharmaceutical compositions containing it, and its use in therapy.
摘要:
Anthranilic acids of formula (I): wherein each of R to R9 is an organic substituent, n is 0 or 1, m is 0 or an integer of 1 to 6, q is 0 or 1, X is a direct bond, O, S, —S—(CH2)p or —O—(CHO2)p— wherein p is from 1 to 6 and Ar is an unsaturated carbocyclic or heterocyclic group, and the pharmaceutically acceptable salts thereof, have activity as inhibitors of P-glycoprotein and may thus be used, inter alia, as modulators of multidrug resistance in the treatment of multidrug resistant cancers, for example to potentiate the cytotoxicity of a cancer drug.