摘要:
Compounds are described of the formula ##STR1## wherein: R.sup.1 is C.sub.3-6 alkyl or C.sub.1-3 alkylthioC.sub.1-3 alkyl;R.sup.2 is an optionally substituted C.sub.1-6 alkyl or C.sub.1-6 alkoxy group, aryl, heteroaryl, arylC.sub.1-4 alkyl, heteroarylC.sub.1-4 alkyl or a side-chain of a natural .alpha.-amino acid;R.sup.3 is hydrogen, C.sub.1-6 alkyl, CHR.sup.4 COR.sup.5 (where R.sup.4 is a side-chain of a natural .alpha.-amino acid and R.sup.5 is hydroxyl, C.sub.1-6 alkoxy or NHR.sup.6 where R.sup.6 represents a hydrogen atom or a C.sub.1-6 alkyl group) or a group (CH.sub.2).sub.n X (where n is 1 to 6 and X is hydroxyl, C.sub.1-4 alkoxy, heteroaryl or a group NR.sup.7 R.sup.8 where R.sup.7 and R.sup.8 are each hydrogen or C.sub.1-6 alkyl or the group NR.sup.7 R.sup.8 forms a 5 to 7 membered cyclic amine); andHet is an optionally substituted cyclic imide where the cyclic imide ring system has the formula (i), (ii) or (iii) ##STR2## in which A, B, C and D are each CH or 1 or 2 of A, B, C and D represents N and the others represent CH, and E and F may each independently represent CH or N; and physiologically acceptable salts and solvates thereof.These compounds inhibit metalloproteases involved in tissue degradation. Compounds of the invention may be formulated for use in a variety of conditions involving tissue degradation including arthropathy, dermatological conditions, bone resorption, inflammatory diseases, tumour invasion and multiple sclerosis and related diseases involving myelin degradation, and in the promotion of wound healing.
摘要:
The invention provides novel antibiotic cefuroxime esters of the formula ##STR1## (wherein R.sup.1 is a primary or secondary alkyl group containing 1 to 4 carbon atoms and R.sup.2 is a primary or secondary alkyl group containing 1 to 6 carbon atoms provided that at least one of the groups R.sup.1 and R.sup.2 is methyl). These compounds are useful as orally administrable broad spectrum antibiotics.
摘要:
The invention provides novel antibiotic compounds which are 7.beta.-acylamidoceph-3-em-4-carboxylic acids, and non-toxic derivatives thereof, and 6.beta.-acylamidopenam-3-carboxylic acids, and non-toxic derivatives thereof, characterized in that the acylamido group has the structure ##STR1## where R is a hydrogen atom or an organic group and R.sup.a is a hydrogen atom or an acyl group. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive and gram negative organisms coupled with particularly high stability to .beta.-lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.
摘要:
The invention provides novel antibiotic compounds which are 6.beta.-acylamidopenam-3-carboxylic acids and non-toxic derivatives thereof, characterized in that the acylamido group has the structure ##EQU1## WHERE R is a hydrogen atom or an organic group and R.sup.a is a hydrogen atom or an acyl group. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive and gram negative organisms coupled with particularly high stability to .beta.-lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.
摘要翻译:本发明提供了新颖的抗生素化合物,它们是6β-酰基氨基青蒿素-3-羧酸及其无毒的衍生物,其特征在于酰基酰胺基具有结构RCCONH PARALLEL N | ORA,其中R是氢原子或有机基团, Ra是氢原子或酰基。 这些化合物是顺式异构体,或作为含有至少75%的顺式异构体的混合物存在。 这些抗生素化合物对革兰氏阳性和革兰氏阴性生物体的一系列革兰氏阴性菌具有很高的抗菌活性,与各种革兰氏阴性生物产生的β-内酰胺酶具有特别高的稳定性。 本发明还涉及化合物的给药。
摘要:
A method and system for analyzing a public switched communications network from a remote place via the public Internet. The system comprises an access device which collects data from one or more links in a public switched communications network. The system further includes a server computer which receives the collected data from the access device via a dedicated network or the Internet. The server computer executes one or more applications to perform protocol analysis based on the received data. A client computer executing a Web browser may be used to communicate with the server computer via the Internet and access the outcome of the protocol analysis.
摘要:
The present invention relates to 2,6-diaminopurine-.beta.-D-ribofuranuronamide derivatives of the following formula (I). These compounds and their salts and solvates are useful as anti-inflammatory agents, particularly in the treatment of patients with inflammatory conditions who are susceptible to leukocyte-induced tissue damage. ##STR1##
摘要:
A method and system for testing at least one link in a communications network. The system includes first and second analyzer units that are configured to test an existing link in the network. Alternatively, the first and second analyzer units may be configured to establish and test a link between them. A computer remotely controls the first and second analyzer units to perform testing of various communication parameters, such as packet loss and latency. Each analyzer unit may be configured to collect data over a predetermined duration to establish a network baseline of operation, which may be used to detect future network malfunctions. The computer estimates the deviation of communication parameters from the network baseline.
摘要:
Compounds of the general formula ##STR1## (wherein R represents a methyl or 2-chloroethyl group and * represents an asymmetric carbon atom). The above compounds are useful as orally administrable antibiotics.
摘要:
The invention provides novel antibiotic compounds which are 7.beta.-acylamidoceph-3-em-4-carboxylic acids, and non-toxic derivatives thereof, and 6.beta.-acylamidopenam-3-carboxylic acids, and non-toxic derivatives thereof, characterized in that the acylamido group has the structure ##STR1## where R is a hydrogen atom or an organic group and R.sup.a is a hydrogen atom or an acyl group. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive and gram negative organisms coupled with particularly high stability to .beta.-lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.
摘要:
The present invention relates to compounds of formula (IV): ##STR1## wherein R.sup.a and R.sup.b each represent a hydrogen atom or together form an alkylidene group.