摘要:
The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.
摘要:
The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.
摘要:
The present invention relates to 2-Mesitylsulfonylamino-3-{3′[(pyridinylamino)methyl][1,1-biphenyl]-4-yl}propanoic acid, pharmaceutical compositions thereof, their preparation, their use in the treatment of cancer, arteriosclerosis, restenosis, osteolytic disorders, ophthalmic disorders, and their use as integrin antagonists. The compounds according to the invention have the formula (I):
摘要:
The present invention relates to compounds of the general formula (I): and their preparation and use for the production of pharmaceuticals, and pharmaceuticals comprising these compounds.
摘要:
The present invention relates to compounds of the general formula (1) wherein R4 is —SO2R4′, —COOR4″, —COR4′, —CONR4′2 or —CSNR4′2; R4′ is hydrogen, a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; R4″ is a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; L is a sulphonamide, amide, ether, ester, keto, urea, thioether, sulphoxide or sulphone unit optionally extended by one or two methylene groups; and X is N, O or S; and their physiologically acceptable salts and stereoisomers. The present invention furthermore relates to a process for the preparation of the compounds of the formula (1), a pharmaceutical composition containing at least one of these compounds, and the use of compounds of the formula (1) for the production of a pharmaceutical composition having integrin-antagonistic action and in particular for the therapy and prophylaxis of cancer, osteolytic diseases such as osteoporosis, arteriosclerosis, restenosis and ophthalmic disorders.
摘要翻译:本发明涉及通式(1)的化合物,其中R 4是-SO 2 R 4',-COOR 4“,-COR 4', - CONR 4'2或-CSNR 4'2; R 4'是氢,取代或未取代的烷基或环烷基残基,取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; R 4“是取代或未取代的烷基或环烷基残基,取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; L是任选被一个或两个亚甲基延伸的磺酰胺,酰胺,醚,酯,酮,脲,硫醚,亚砜或砜单元; X为N,O或S; 及其生理上可接受的盐和立体异构体。 本发明还涉及制备式(1)化合物的方法,含有这些化合物中的至少一种的药物组合物,以及式(1)化合物在制备药物组合物中的用途 具有整合素拮抗作用,特别是用于治疗和预防癌症,溶骨性疾病如骨质疏松症,动脉硬化,再狭窄和眼科疾病。
摘要:
The present invention relates to compounds of the general formula (1) wherein R4 is —SO2R4, —COOR4′, —COR4′, —CONR4′2 or —CSNR4′2; R4′ is hydrogen, a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; R4″ is a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; L is a sulphonamide, amide, ether, ester, keto, urea, thioether, sulphoxide or sulphone unit optionally extended by one or two methylene groups; and X is N, O or S; and their physiologically acceptable salts and stereoisomers. The present invention furthermore relates to a process for the preparation of the compounds of the formula (1), a pharmaceutical composition containing at least one of these compounds, and the use of compounds of the formula (1) for the production of a pharmaceutical composition having integrin-antagonistic action and in particular for the therapy and prophylaxis of cancer, osteolytic diseases such as osteoporosis, arteriosclerosis, restenosis and ophthalmic disorders.
摘要翻译:本发明涉及通式(1)的化合物,其中R4是-SO2R4,-COOR4',-COR4',-CONR4'2或-CSNR4'2; R 4'是氢,取代或未取代的烷基或环烷基残基,取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; R 4“是取代或未取代的烷基或环烷基残基,取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; L是任选被一个或两个亚甲基延伸的磺酰胺,酰胺,醚,酯,酮,脲,硫醚,亚砜或砜单元; X为N,O或S; 及其生理上可接受的盐和立体异构体。 本发明还涉及制备式(1)化合物的方法,含有这些化合物中的至少一种的药物组合物,以及式(1)化合物在制备药物组合物中的用途 具有整合素拮抗作用,特别是用于治疗和预防癌症,溶骨性疾病如骨质疏松症,动脉硬化,再狭窄和眼科疾病。