Abstract:
The invention relates to compouns derived from betulin, and to the use thereof as antibacterial agents in pharmaceutical and cosmetic applications.
Abstract:
Aphidicolane derivatives of the formula: ##STR1## wherein R.sup.1 stands for hydrogen or a hydroxy radical, R.sup.2 stands for a hydroxy or methyl radical, or the group CR.sup.1 R.sup.2 stands for a keto group; R.sup.3 stands for a formyl or hydroxymethyl radical, or for the group --CH.sub.2 O.CO.OR.sup.6, wherein R.sup.6 stands for a defined radical or R.sup.2 and R.sup.3 are joined together to form the group --O.CO.OCH.sub.2 --; R.sup.4 stands for a hydroxy radical; R.sup.5 stands for a formyl radical, a hydroxyalkyl radical --(CH.sub.2).sub.1-3 OH, a radical --CHR.sup.7 OH, wherein R.sup.7 stands for a defined radical, or R.sup.5 stands for an azidomethyl or pyrrolidinylcarbonyloxymethyl radical, or for the group --CH.sub.2 O.CO.OR.sup.8, wherein R.sup.8 stands for a defined radical, or R.sup.5 stands for the group --CH.sub.2 O.CO.(CH.sub.2).sub.m.CR.sup.11 R.sup.12.(CH.sub.2).sub.n.NR.sup.9 R.sup.10, wherein m, n, R.sup.9, R.sup.10, R.sup.11 and R.sup.12 have defined values, or R.sup.5 stands for the group --CH.sub.2 O.SO.sub.2.R.sup.13, wherein R.sup.13 stands for a defined radical; or R.sup.4 and R.sup.5 are joined together to form the group --O.CH.sub.2 -- or --O.CO.OCH.sub.2 --; and, where appropriate, pharmaceutically-acceptable salts thereof. Processes for the preparation of said aphidicolane derivatives. Pharmaceutical compositions comprising one of the compounds and a pharmaceutical diluent or carrier. The compounds exhibit inhibitory activity against DNA-containing viruses and they inhibit the growth of some tumors.
Abstract:
Novel physiologically active substances Ks-504a, KS-504b and KS-504d having a vasodilative activity and a novel physiologically active substance KS-504e having an activity to inhibit histamine secretion are produced by culturing a microorganism of the genus Mollisia.
Abstract:
Novel physiologically active substances KS-504a, KS-504b and KS-504d having a vasodilative activity and a novel physiologically active substance KS-504e having an activity to inhibit histamine secretion are produced by culturing a microorganism of the genus Mollisia.
Abstract:
Compounds having the formula ##STR1## R.sub.1 is hydrogen, benzyl or an ester moiety; Y is --CH(R.sub.2 ")CH(R.sub.2)-- or --CH(R.sub.3)CH hd 2--;R.sub.2 " is hydrogen or methyl;R.sub.2 is OH or X-substituted (C.sub.1-6)alkyl;R.sub.3 is OH, cyano or X-substituted (C.sub.1-3)alkyl;X is --OR.sub.6, --SR.sub.6, --S(O)R.sub.6, --S(O).sub.2 R.sub.6, --NR.sub.6 R.sub.7, --COOR.sub.7, --CONR.sub.7 R.sub.8 or oxo;with the proviso that when X is --NR.sub.6 R.sub.7, --COOR.sub.7 or --CONR.sub.7 R.sub.8, said group is located on the terminal carbon atom of R.sub.2 or R.sub.3 ;R.sub.6 is hydrogen, (C.sub.1-6)alkyl or acetyl;each of R.sub.7 and R.sub.8 is hydrogen or (C.sub.1-6)alkyl;s is an integer of 1 or 2;with the proviso that when R.sub.6 is acetyl, R.sub.7 is hydrogen and X is other than S(O)R.sub.6 or S(O).sub.2 R.sub.6 ;Z-W is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain, and their use as CNS agents, antidiarrheals and anti-emetics. Processes for their preparation and intermediates therefor are described.
Abstract translation:具有式的化合物,其中R1是氢,苄基或酯部分; Y是-CH(R 2“)CH(R 2) - 或-CH(R 3)CH hd 2-; R2“是氢或甲基; R2是OH或X取代的(C1-6)烷基; R3是OH,氰基或X取代(C1-3)烷基; X是-OR 6,-SR 6,-S(O)R 6,-S(O)2 R 6,-NR 6 R 7,-COOR 7,-CONR 7 R 8或氧代; 条件是当X是-NR 6 R 7,-COOR 7或-CONR 7 R 8时,所述基团位于R 2或R 3的末端碳原子上; R6是氢,(C1-6)烷基或乙酰基; R 7和R 8各自为氢或(C 1-6)烷基; s是1或2的整数; 条件是当R6为乙酰基时,R7为氢,X为S(O)R6或S(O)2R6; Z-W是可以具有作为烷基链的一部分的氧原子的烷基,苯基烷基或吡啶基烷基,它们用作CNS剂,抗腹泻剂和抗排毒剂。 描述了其制备方法及其中间体。
Abstract:
Bicyclo[3.3.0]octenylaldehyde derivatives represented by the formula: ##STR1## wherein R.sup.1 is a substituent selected from the group consisting of a hydrogen atom and a protective group of a hydroxy group;R.sup.2 is a substituent selected from the group consisting of --CH.sub.2 OR.sup.5, ##STR2## where R.sup.5 is a substituent selected from the group consisting of a hydrogen atom and a protective group of a hydroxy group,R.sup.6 is a substituent selected from the group consisting of an alkyl group, an alkenyl group and an alkynyl group, said substituent being straight, branched or cyclic and having 5 to 10 carbon atoms,X is a substituent selected from the group consisting of a vinylene group and an acetylene group, andR.sup.7 is a substituent selected from the group consisting of an alkyl, an alkenyl group, and an alkynyl group, said substituent being straight, branched or cyclic and having 5 to 10 carbon atoms; andR.sup.4 is a hydrogen atom,and a process for producing the derivatives are available for producing a 9(0)-methano-.DELTA..sup.6(9..alpha.) -PGI.sub.1.
Abstract:
A process is described for reacting "myrac aldehyde" having the structure: ##STR1## (which structure is representative of a mixture of two compounds, one where the carboxaldehyde is in the "4" position and the other wherein the carboxaldehyde is in the "5" position) with an acid hydrating agent at a temperature of from 0.degree. up to 120.degree. C, to produce a mixture containing a major proportion of 4-(4'-methyl-4'-hydroxyamyl)-.DELTA..sup.3 -cyclohexene carboxaldehyde and a minor proportion of 3-(4'-methyl-4'-hydroxyamyl)-.DELTA..sup.3 -cyclohexene carboxaldehyde (otherwise termed "Lyral") having the structure: ##STR2## and a minor proportion of 3-(4'-methyl-4'-hydroxyamyl)-.DELTA..sup.3 -cyclohexene carboxaldehyde having the structure: ##STR3## which mixture possesses a sweet, lilac-lily aromatic odor and isolating a mixture of the two carboxaldehydes. The products produced by the aforementioned process are useful in various aspects of perfumery.
Abstract:
The present invention relates to novel 2-cycloalkyl resorcinol compounds; to pharmaceutical compositions comprising the compounds; and to methods of preparing the compounds and uses thereof. The disclosed compounds can bind to and modulate the cannabinoid receptors and thus, they are specific ligands for these receptors. The invented compounds, when administered in a therapeutically effective amount to an individual or animal, results in a sufficiently high level of that compound in the individual or animal to cause a physiological response. The physiological response may be useful to treat a number of physiological conditions.
Abstract:
The present invention concerns a pharmaceutical compound having the Formula (1): or a pharmaceutically acceptable salt thereof, for use in the prevention or treatment of a cognitive, neurodegenerative or neuronal disorder or disease such as the Alzheimer Disease, a pharmaceutical composition and a method of preparing a pharmaceutical composition.