摘要:
Compounds having the formula ##STR1## wherein R.sup.1, R.sup.4, R.sup.6, R.sup.7, and R.sup.8 are hydrogen or a substituent, R.sup.2 is a substituent, R.sup.5 is an optionally-substituted bicyclic ring system, especially a 7-benzofuranyl or 2,3-dihydrobenzofuran-7-yl substituent, R.sup.9 is hydrogen, alkyl, alkoxycarbonyl or, together with R.sup.8, forms the remainder of a heterocyclic ring, their pharmaceutically-accceptable salts, as well as their pharmaceutical compositions and use as prodrugs for compounds active for the treatment of mental disorders, are disclosed.
摘要:
Novel 2,3,4,5-tetrahydro-1H-3-benzazepines having the formula ##STR1## wherein R.sup.3 represents H, C.sub.1-3 -alkyl or C.sub.3-7 -cycloalkyl; R.sup.4 represents hydrogen or R.sup.4 together with R.sup.10 represents a bridge which connects the positions to which R.sup.4 and R.sup.10 are linked, said bridge being --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --O--CH.sub.2 -- or --S--CH.sub.2 --;R.sup.7 represent hydroxy, lower alkoxy;R.sup.10, R.sup.11, R.sup.12 independently represent hydrogen or halogen or alkyl or alkoxy or trifluoromethyl, or R.sup.10 together with R.sup.4 represents a bridge as described in connection with the definition of R.sup.4 ; or R.sup.10 together with R.sup.11 represents a bridge or R.sup.11 together with R.sup.12 represents a bridge, the bridge in both cases being chosen among --O--CH.sub.2 --CH.sub.2 --, --O--CH.sub.2 --CH.sub.2 --CH.sub.2 --, --O-CH.dbd.CH--, --CH.sub.2 -CH.sub.2 -CH.sub.2 --, --CH.sub.2 -CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 --;R.sup.13 represents hydrogen, halogen or lower alkyl.The compounds are useful in preparations for treatment of disorders in the central nervous system.
摘要:
Novel 2,3,4,5-tetrahydro-1H-3-benzazepines having the formula ##STR1## wherein R.sup.3 represents H, C.sub.1-3 -alkyl or C.sub.3-7 -cycloalkyl;R.sup.4 represents hydrogen or R.sup.4 together with R.sup.10 represents a bridge which connects the positions to which R.sup.4 and R.sup.10 are linked, said bridge being --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --O--CH.sub.2 -- or --S--CH.sub.2 --;R.sup.7 represents hydroxy, lower alkoxy;R.sup.10, R.sup.11, R.sup.12 independently represent hydrogen or halogen or alkyl or R.sup.10 together with R.sup.4 represents a bridge as described in connection with the definition of R.sup.4 ; or R.sup.10 together with R.sup.11 represents a bridge or R.sup.11 together with R.sup.12 represents a bridge, the bridge in both cases being chosen among--O--CH.sub.2 --CH.sub.2 --, --O--CH.sub.2 --CH.sub.2 --CH.sub.2 --, --O--CH.dbd.CH--, --CH.sub.2, --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 --;R-- represents hydrogen, halogen or lower alkyl.The compounds are useful in preparations for treatment of disorders in the central nervous system.
摘要:
Certain bile acids find use in the pharmaceutical industry. In view of the wide distribution of serious diseases such as HIV, AIDS and Bovine Spongiform Encephalopathy (BSE) it is desirable to avoid—as far as practicable—to have any components of animal origin in medicaments in order to eliminate any danger of infection. The present invention relates to a method of providing bile acids from non-animal starting materials.
摘要:
Sterol derivative compounds, structurally related to natural compounds which can be extracted from bull testes and from human follicular fluid, useful for regulating meiosis in oocytes and in male germ cells. Some of these compounds are useful in the treatment of infertility, whereas other compounds are useful as contraceptives.
摘要:
Indole derivatives of formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may be hydrogen or lower alkyl optionally substituted by halogen; X represents oxygen or sulfur; A.sup.1 represents a straight or branched alkylene chain containing from 2 to 4 carbon atoms; R.sup.5 is hydrogen or a straight or branched alkyl group; A.sup.2 is a straight or branched, saturated or unsaturated hydrocarbon chain containing from 2 to 6 carbon atoms; and R.sup.6 is selected from a group consisting of various structures, have been found to exhibit central nervous system activities.
摘要:
1-carboxyalkylquinoxaline-2,3(1H,4H)-dione compounds or tautomeric forms thereof of the formula ##STR1## wherein R represents hydrogen, C.sub.1-6 -alkyl, including branched chains, or aralkyl and n represents the number from 0 to 5;R.sup.4 represents hydrogen or hydroxy;R.sup.5, R.sup.6, R.sup.7 and R.sup.8 independently represent hydrogen, nitro, halogen, alkoxy, aryloxy, aralkoxy, C.sub.1-6 -alkyl including branched chains, or aryl;R.sup.9 represents hydrogen, lower alkyl, or aryl;R.sup.10 represents hydrogen, or alkyl.The compounds are useful in the treatment of neurological and psychiatric diseases.
摘要:
Novel penicillin and cephalosporin intermediates for the synthesis of 6-APA or 7-aminocephem compounds involving formation of a 6 or 7 phosphite amido compound and the conversion of such compound to a desired 6-APA or 7-aminocephem compound.
摘要:
Certain compounds, structurally related to natural compounds which can be extracted i.a. from bull testes and from human follicular fluid, can be used for regulating the meiosis in oocytes and in male germ cells. Some of these compounds are useful in the treatment of infertility, whereas other compounds are useful as contraceptives. These compounds have the structural formula wherein the substituents are as defined in the specification.