摘要:
Etoposide analogs such as 4′-O-demethyl-4β-[4″-(methyl-L-tyrosine-N-carbonyl)-anilino]-4-desoxy-podophyllotoxin (12) and 4′-O-demethyl-4β-[4″-(methyl-L-tryptophan-N-carbonyl)-anilino]-4-desoxypodophyllotoxin (13) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.
摘要:
Dibenzonaphthyrone of formula (I) 1 wherein A1 and A2 independently of each other are unsubstituted or mono- to tetra-substituted o-C6-C18arylene, with the proviso that formula (I) does not represent a dibenzonaphthyrone of the formula 2 The invention further relates to processes for the preparation thereof, to the use thereof for colouring/pigmenting high-molecular-weight organic material and to substance compositions comprising dibenzonaphthyrones.
摘要:
The invention provides compounds of formula (I), ##STR1## wherein R.sup.1 represents C.sub.1-4 alkoxy optionally substituted by one or more fluorine atoms; R.sup.2 represents H or C.sub.1-6 alkoxy optionally substituted by one or more fluorine atoms; R.sup.3 represents one or more groups independently selected from H, halogen, C.sub.1-4 alkoxy and CF.sub.3 ; in addition, R.sup.2 and one R.sup.3 group may together represent --OCH.sub.2 --, the methylene group being attached to the ortho-position of the pendant phenyl ring; R.sup.4 represents a 4-, 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent or represents a cyclic group or an open chain group; and pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful in the treatment of inter alia benign prostatic hyperplasia.
摘要:
There are provided novel (2-imidazolin-2-yl) fused heteropyridine compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.
摘要:
There are provided novel (2-imidazolin-2-yl) fused heteropyridine compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.
摘要:
The invention provides novel persistent free radicals useful in Overhauser MRI being triarylmethyl radicals having as at least one aryl group a group of formula ##STR1## (wherein each X which may be the same or different is an oxygen or sulphur atom or a group CO or S(O).sub.n, (where n is 1 to 3) with the proviso that at least one group X is a sulphur atom or a S(O).sub.n group; R.sup.1 is a hydrogen atom or group of formula --M, --XM, --X--Ar.sup.2, or --Ar.sup.2 where M is a water solubilizing group, and Ar.sup.2 represents a 5-10 membered aromatic ring optionally substituted by a water solubilizing group M; and each of the groups R.sup.7, which may be the same or different, is a hydrogen atom, or a hydrocarbon group or a water solubilizing group M, or two groups R.sup.7 together with the atom to which they are bound represent a carbonyl group or a 5 to 8 membered cycloalkylidene, mono- or di-oxacycloalkylidene, mono- or di-azacycloalkylidene or mono- or di-thiacycloalkylidene group optionally with the ring attachment carbon replaced by a silicon atom, and R.sup.7 where it is other than hydrogen, is optionally substituted by a hydroxyl group, an optionally alkoxylated, optionally hydroxylated acyloxy or alkyl group or a water solubilizing group M)). The novel radicals have good stability, long relaxation times and good relaxivity.
摘要:
There are provided novel (2-imidazolin-2-yl) fused heteropyridine compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.
摘要:
The present invention is concerned with compounds of formula 1: ##STR1## wherein R.sub.1 is straight or branched alkyl having 1-4 C-atoms, halogen or cyano;n has the value 0-1;R.sub.2 is hydrogen, (1-6 C)alkyl, (3-6 C)alkenyl, (3-6 C)alkenyl, (3-6 C)cycloalkyl, (3-6 C)cycloalkyl-(1-4 C) alkyl, phenyl, phenyl-(1-3 C)alkyl, COOR.sub.6, COR.sub.6, CONR.sub.6 R.sub.7 or SO.sub.2 --R.sub.6, wherein R.sub.6 and R.sub.7 independently of each other are hydrogen, (1-6 C)alkyl, (3-6 C)cycloalkyl, phenyl or phenyl-(1-4 C)alkyl, wherein the benzene ring is optionally substituted with a methyl group or a halogen atom, with the proviso that R.sub.6 is not hydrogen when R.sub.2 is a group COOR.sub.6 or SO.sub.2 R.sub.6 ;R.sub.3 is hydrogen, straight or branched (1-6 C)alkyl or a phenyl-(1-3 C)alkyl group optionally substituted in the benzene ring; andA is a group of formula 2 or 3 ##STR2## wherein one of the groups R.sub.8, R.sub.9 and R.sub.10 is hydrogen, (1-C)alkyl, (3-6 C)cycloalkyl, (3-4 C)alkenyl or (3-4 C)alkynyl and the two other groups, independently of each other, are hydrogen or (1-4 C)alkyl, and the pharmacologically acceptable acid addition salts thereof, which are pharmaceutically useful as strong and selective antagonists of "neuronal" 5-hydroxy tryptamine (5-HT) receptors.
摘要:
This invention relates to novel substituted derivatives of 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acid and analogs thereof, which are useful for the treatment of hypertension, as well as, novel pharmaceutical compositions and methods of use.