摘要:
Compounds of formula I ##STR1## wherein Z, R, R.sub.1, R.sub.2 and X are as defined in the description, have valuable pharmaceutical properties and are effective especially against tumours. They are prepared in a manner known per se.
摘要:
Compounds of formula I ##STR1## wherein Z is thiazolyl or isothiazolyl, and X, R, R.sub.0, R.sub.1, R.sub.2 and R.sub.3 are as defined in the description, have valuable pharmaceutical properties and are effective especially against tumors.
摘要:
2-heterocyclythio-lower alkyl-2-penem compounds of the formula ##STR1## in which R.sub.1 represents hydrogen or methyl, R.sub.2 represents an optionally protected hydroxy group, R.sub.3 represents carboxy or protected carboxy R.sub.3 ', R.sub.4 represents an unsaturated monocyclic heterocyclyl radical that is bonded via a ring carbon atom to the sulphur atom, and m is 2, 3 or 4, and salts of such compounds of the formula I that have a salt-forming group, optical isomers of compounds of the formula I and mixtures of these optical isomers, possess antibiotic properties. The compounds are manufactured according to processes known per se.
摘要:
Apparatus for filling syringe barrels (1) with a product (A, B), includes at least one vacuum unit, at least one filling device, and a metering head (10) which can be moved with respect to the syringe barrel (1). The metering head (10) has a first material inlet valve (11a) and a second material inlet valve (11b) as well as a first vacuum valve (20a) and a second vacuum valve (20b). The material inlet valves (11a, 11b) and the vacuum valves (20a, 20b) are connected to channels (25a, 25b), to each of which a chamber (2a, 2b) of the syringe barrels (1) can be connected, as a result of which the syringe barrel (1) can be filled through the same openings (5a, 5b) as those through which the product (A, B) can be forced out of the chambers (2a, 2b) by pistons (3) for use of the product, where the pistons (3) are inserted into the syringe barrels (1) before the barrels are filled.
摘要:
The invention relates to compounds of the formula I, in which R1 and R2 are, independently of each other, lower alkyl or lower alkoxy-lower alkyl; R3 and R4 are, independently of each other, sec-lower alkyl or tert-lower alkyl; R5 is phenyl or cyclohexyl; and R6 and R7 are, independently of each other, lower alkyl, or, together with the linking nitrogen atom, pyrrolidino, piperidino, 4-lower alkylpiperidino, 1,2,4-triazol-1-yl or 1,2,4-triazol-4-yl; or a salt thereof, provided that at least one salt-forming group is present. These compounds are inhibitors of HIV protease and are therefore suitable, for example, for treating AIDS or its preliminary stages.
摘要翻译:本发明涉及式I化合物,其中R 1和R 2彼此独立地为低级烷基或低级烷氧基 - 低级烷基; R 3和R 4彼此独立地为低级烷基或叔 - 低级烷基; R5是苯基或环己基; R 6和R 7彼此独立地为低级烷基,或与连接氮原子一起为吡咯烷子基,哌啶子基,4-低级烷基哌啶子基,1,2,4-三唑-1-基或1,2,4-三唑 -4-基或其盐,条件是至少存在一个成盐基团。这些化合物是HIV蛋白酶的抑制剂,因此适用于例如用于治疗AIDS或其初级阶段。
摘要:
There are described 7H-pyrrolo[2,3-d]pyrimidine derivatives of the formula I in which the substituents are as defined in claim 1. These compounds inhibit the tyrosine kinase activity of the receptor for the epidermal growth factor (EGF) and c-erbB2 kinase and can be used as anti-tumor agents.
摘要:
There are described compounds of formula I*, ##STR1## wherein R.sub.1 is lower alkoxycarbonyl, R.sub.2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl, R.sub.3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C.sub.4 -C.sub.8 cycloalkyl, R.sub.4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, sulfinyl (--SO--) and sulfonyl (--SO.sub.2 --) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl, R.sub.5, independently of R.sub.2, has one of the meanings mentioned for R.sub.2, and R.sub.6, independently of R.sub.1, is lower alkoxycarbonyl, or salts thereof, provided that at least one salt-forming group is present.The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS. They exhibit outstanding pharmacodynamic properties.
摘要:
The present invention relates to the use of inhibitors of HIV aspartate proteases, such as HIV-1- or HIV-2-protease, and their salts and to prodrugs for inhibiting the growth of tumors, especially those tumors which do not respond to the inhibition of HIV aspartate proteases themselves, and in the preparation of pharmaceutical compositions intended for use in the prophylaxis and especially the treatment of tumor diseases, and to methods and pharmaceutical compositions for the treatment of tumors with those compounds.
摘要:
Compounds of formula I ##STR1## wherein Z, X, R, R.sub.0, R.sub.1, R.sub.2 and R.sub.3 are as defined in the description, have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.