Abstract: There are provided compounds of general formula ##STR1## (wherein R.sup.1 is a hydrogen atom or a methyl group;R.sup.2 is a hydrogen or halogen atom or a methyl group;and one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is a group --NR.sup.5 R.sup.6 [where R.sup.5 is a hydrogen atom and R.sup.6 is a group --COCH.sub.2 NR.sup.7 R.sup.8 (wherein R.sup.7 and R.sup.8, which may be the same or different, each represents a hydrogen atom or a C.sub.3-7 cycloalkyl group of a C.sub.1-4 alkyl group optionally substituted by a hydroxyl or benzoyloxy group, or --NR.sup.7 R.sup.8 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring an oxygen or sulphur atom or a group --NH-- or --N(R)-- where R is a C.sub.1-4 alkyl group optionally substituted by a hydroxyl group) or R.sup.6 is a group --COCH.sub.2 NH(CH.sub.2).sub.n NR.sup.7 R.sup.8 (where n is an integer from 2 to 5 inclusive and R.sup.7, R.sup.8 and --NR.sup.7 R.sup.8 are as defined above) or R.sup.

Abstract: A process is described for the preparation of compounds of formula (1) ##STR1## [where OR is hydroxyl, protected hydroxyl or OP(O)(OCH.sub.2 Ph)(OR.sup.1) (where Ph is phenyl and OR.sup.1 is hydroxyl or protected hydroxyl)] and salts thereof, which comprises reacting a compound of formula (2) ##STR2## with a compound of formula (3) ##STR3## (where OR is as defined above and one of X.sup.1 and X.sup.2 is a leaving group and the other is a hydrogen atom) or a salt thereof, followed, if desired, by removal of the hydroxyl protecting group when present and/or by salt formation.The compounds of formula (1) are either anticancer agents or intermediates useful in the synthesis of anticancer agents.

Abstract: Compounds of formula (I) ##STR1## (wherein R.sup.1 is a hydrogen atom or a methyl group;R.sup.2 is a hydrogen atom or a hydroxyl, C.sub.1-4 alkoxy or C.sub.2-4 alkanoyloxy group;R.sup.3 is a hydrogen atom, or (when R.sup.2 is other than a hydrogen atom) optionally a hydroxyl, C.sub.1-4 alkoxy or C.sub.2-4 alkanoyloxy group, or R.sup.2 and R.sup.3 together are a methylenedioxy group;R.sup.4 is a hydrogen or halogen atom or a methyl group;R.sup.5 and R.sup.6 is each a hydrogen atom or a group --OCOCH.sub.2 NR.sup.7 R.sup.8 [where R.sup.7 and R.sup.8, which may be the same or different, each is a hydrogen atom or a C.sub.3-7 cycloalkyl group or a straight or branched C.sub.1-4 alkyl group optionally substituted by a hydroxyl group, or --NR.sup.7 R.sup.8 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring an oxygen or sulphur atom or a group --NH-- or --N(R) where R is a C.sub.

Abstract: There are provided compounds of the general formula (1) ##STR1## (wherein R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom, a hydroxyl group or a group --OP(O) (OH) (OR.sup.4) [where R.sup.4 represents a hydrogen atom or an alkyl (optionally substituted by a hydroxyl, alkoxy, cyclic ether or cycloalkyl group), alkenyl cycloalkyl, aryl, aralkyl or aroylalkyl group], with the proviso that at least one of R.sup.1 and R.sup.2 represents a group --OP(O) (OH) (OR.sup.4); and R.sup.3 represents a hydrogen or halogen atom or a methyl group), and salts thereof. The novel compounds exhibit interesting anti-cancer activity.

Abstract: Pharmaceutical compositions for combatting cancer comprising a compound of formula (I) ##STR1## (wherein R.sup.1 represents a hydrogen atom or a C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl group;R.sup.2 represents a hydrogen atom or a hydroxyl, C.sub.1-4 alkoxy or C.sub.2-4 alkanoyloxy group;R.sup.3 represents a hydrogen atom, or (when R.sup.2 is other than a hydrogen atom) optionally a hydroxyl, C.sub.1-4 alkoxy or C.sub.2-4 alkanoyloxy group, or R.sup.2 and R.sup.3 together represent a methylenedioxy group;R.sup.4 represents a hydrogen or halogen atom or a C.sub.1-3 alkyl group or a phenyl group optionally substituted by a halogen atom or a hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.1-4 alkanoyloxy group; and the ring A represents a group of formula ##STR2## where R.sup.5 and R.sup.6 each represent a hydrogen atom or a hydroxyl, C.sub.1-4 alkoxy or C.sub.1-4 alkanoyloxy group,R.sup.7 and R.sup.8 each represents a hydrogen atom or a methyl group, and one of X, X.sup.1, X.sup.2 and X.sup.

Abstract: 5,14-Dihydrobenz[5,6]isoindolo[2,1-b]isoquinoline-8,13-dione ##STR1## exhibits anticancer activity. The compound can be prepared by reaction of 2-formyl-3-carboxyl-1,2,3,4-tetrahydroisoquinoline with 1,4-naphthoquinone and is particularly suitably administered parenterally in microcrystalline suspension form.

Abstract: Androstane carbothioic acids of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, a hydroxy group in the .alpha.-configuration, a methyl group which may be in either the .alpha.- or .beta.-configuration, or a methylene group;R.sup.2 represents a hydroxy or protected hydroxy group in either the .alpha.- or .beta.-configuration or an oxo group;R.sup.3 represents a hydrogen, bromine, chlorine or fluorine atom; or R.sup.2 and R.sup.3 together represent a carbon-carbon bond or an epoxy group in the .beta.-configuration;R.sup.4 represents a hydrogen or fluorine atom; and the symbol represents a single or double bond and the salts thereof are useful as intermediates in the preparation of anti-inflammatory androstane 17.beta.-carbothioate esters.The compounds of formula I are prepared by reaction of a reactive derivative of a 17.beta.-carboxylic acid corresponding to the compound of formula I with hydrogen sulphide or a sulphide or hydrosulphide salt.

Abstract: Compounds of the general formula: ##STR1## wherein X represents a halogen atom or a trifluoromethyl group; R.sup.1 represents a hydrogen atom or a lower alkyl group and Het represents an optionally substituted C-attached 5-7 membered aromatic heterocyclic ring which ring contains one or more heteroatoms selected from O, N and S and optionally carries a fused ring and where an acidic or basic group is present, the salts thereof have been found to possess excellent metaphase arresting ability and are of use in combating abnormal cell proliferation. Thus a knowledge of the cell division cycles of the normal and abnormal cells enables a cytotoxic drug to be administered while the abnormal cells are in a phase susceptible to attack and while the normal cells are in a non-susceptible phase.The compounds of the invention are prepared by alkylation, deprotection of a protected keto group, oxidation or electrophilic halogenation.

Abstract: Compounds of the general formula: ##STR1## (wherein X represents a halogen atom or a trifluoromethyl group; R.sup.1 represents an optionally substituted C.sub.6-10 carbocyclic aromatic group; and R.sup.2 represents a hydrogen atom or a lower alkyl, C.sub.7-16 aralkyl or C.sub.6-10 aryl group or the group COR.sup.1a, in which R.sup.1a is as defined for R.sup.1, R.sup.1 and R.sup.1a being the same or different) and where an acidic or basic group is present, the salts thereof have been found to possess excellent metaphase arresting ability and are of use in combating abnormal cell proliferation. Thus a knowledge of the cell division cycles of the normal and abnormal cells enables a cytotoxic drug to be administered while the abnormal cells are in a phase susceptible to attack and while the normal cells are in a non-susceptible phase.The compounds of the invention are prepared by alkylation, deprotection of a protected keto group, oxidation or electrophilic halogenation.

Abstract: Androstane carbothioic acids of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, a hydroxy group in the .alpha.-configuration, a methyl group which may be in either the .alpha.- or .beta.-configuration, or a methylene group;R.sup.2 represents a hydroxy or protected hydroxy group in either the .alpha.- or .beta.-configuration or an oxo group;R.sup.3 represents a hydrogen, bromine, chlorine or fluorine atom; or R.sup.2 and R.sup.3 together represent a carbon-carbon bond or an epoxy group in the .beta.-configuration;R.sup.4 represents a hydrogen or fluorine atom; and the symbol represents a single or double bond and the salts thereof are useful as intermediates in the preparation of anti-inflammatory androstane 17.beta.-carbothioate esters.The compounds of formula I are prepared by reaction of a reactive derivative of a 17.beta.-carboxylic acid corresponding to the compound of formula I with hydrogen sulphide or a sulphide or hydrosulphide salt.

Abstract: R.sup.3 is a C.sub.1-6 alkyl group or a C.sub.3-7 cycloalkyl group; andR.sup.4 is a group --OR.sup.5 or --OCOR.sup.6 whereR.sup.5 is an optionally substituted alkyl or alkenyl group which may contain up to 6 carbon atoms, an optionally substituted C.sub.3-7 cycloalkyl group, a phenyl group or a carbon-attached 5-7 membered heterocyclic ring in which the hetero-atom is selected from nitrogen, oxygen and sulphur, andR.sup.6 is a hydrogen atom or a group R.sup.5 as defined above;provided that when the compounds contain a 5.beta.-hydrogen atom, R.sup.2 is a hydrogen atom and salts thereof, which compounds have activity as antidysthythmic agents.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is a C.sub.1-8 alkyl group or a C.sub.3-7 cycloalkyl group;R.sup.2 is a C.sub.1-6 alkyl group or a C.sub.3-7 cycloalkyl group;R.sup.3 is a hydroxy group or a group of formula --OR.sup.4 or --OCOR.sup.5 whereR.sup.4 is an alkyl or alkenyl group which may contain up to 6 carbon atoms (or such a group substituted by halogen, C.sub.1-6 alkoxy, carboxyl, phenyl, phenyl substituted by nitro, halo, C.sub.1-4 alkoxy or C.sub.1-4 alkyl), a C.sub.3-7 cycloalkyl group, a phenyl group (or such a group substituted by nitro, halo, C.sub.1-4 alkoxy or C.sub.1-4 alkyl), or a carbon-attached 5-7 membered heterocyclic ring in which the hetero atom is selected from nitrogen, oxygen and sulphur, andR.sup.5 is a hydrogen atom or a group R.sup.4 as defined above;and the D-homo analogues thereof having the group --CO.sub.2 R.sup.2 (wherein R.sup.2 is as defined above) at the 17a.beta.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is a C.sub.1-8 alkyl group or a C.sub.3-7 cycloalkyl group, and R.sup.2 is a C.sub.1-6 alkyl group or a C.sub.3-6 cycloalkyl group and the D-homo analogues thereof having the group --CO.sub.2 R.sup.2 (wherein R.sup.2 is as defined above) at the 17.alpha..beta.-position, and acid addition salts thereof have activity as antidysthythmic agents and may be applicable for the treatment of dysrthymias in humans or animals. The compounds may be provided in the form of compositions in admixture with pharmaceutical carriers and excipients and may be prepared by a variety of processes known for producing steroids of this type. The invention also provides intermediates for the preparation of the compounds of formula (I) wherein R.sup.2 and/or R.sup.1 are replaced with hydrogen atoms, and processes for the preparation of such intermediates.

Abstract: Compounds of formula ##STR1## wherein: R.sup.1 is a C.sub.1-8 alkyl group or a C.sub.3-7 cycloalkyl group;R.sup.2 is a hydrogen atom, a C.sub.1-6 alkoxy group or a C.sub.2-5 alkanoyloxy group; andR is a C.sub.1-8 alkyl group or a C.sub.3-7 cycloalkyl group;provided that when the compounds contain a 5.beta.-hydrogen atom, R.sup.2 is a hydrogen atom, and the D-homo analogues thereof having the group --CO.sub.2 R.sup.3 (wherein R.sup.3 is as defined above) at the 17a.beta.-position, and salts thereof have activity as antidysrhythmic agents and may be applicable for treatment of ventricular dysrhythmias in humans or animals. The compounds may be provided in the form of compositions in admixture with pharmaceutical carriers and excipients and may be prepared by a variety of processes known for producing steroids of this type. The invention also provides intermediates for the preparation of the compounds of formula (I), wherein R.sup.3 and/or R.sup.

Abstract: Compounds of formula ##STR1## (wherein): R.sup.1 is a hydrogen atom, a C.sub.1-8 alkyl group or a C.sub.3-7 cycloalkyl group; andR.sup.2 is a hydrogen atom, a C.sub.1-6 alkyl group or a C.sub.3-6 cycloalkyl group; and the D-homo analogues thereof having the group --CO.sub.2 R.sup.2 (wherein R.sup.2 is as defined above) at the 17a.beta.-position and salts and zwitterionic forms thereof have activity as antidysrhythmic agents and may be applicable for treatment of ventricular dysrhythmias in humans or animals. The compounds may be provided in the form of compositions in admixture with pharmaceutical carriers and excipients and may be prepared by a variety of processes known for producing steroids of this type.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 represents a fluoro-, chloro- or bromo-methyl group or a 2'-fluoroethyl group, R.sup.2 represents a group COR.sup.6 where R.sup.6 is a C.sub.1-3 alkyl group or OR.sup.2 and R.sup.3 together form a 16.alpha.,17.alpha.-isopropylidenedioxy group; R.sup.3 represents a hydrogen atom, a methyl group (which may be in either the .alpha.- or .beta.-configuration) or a methylene group; R.sup.4 represents a hydrogen, chlorine or fluorine atom; R.sup.5 represents a hydrogen or fluorine atom and symbol represents a single or double bond have good anti-inflammatory activity, particularly on topical applications.The compounds of formula I are prepared by esterification, halogenation, reduction, deprotection and reaction at a 9,11-double bond to form a 9.alpha.-halo-11.beta.-hydroxy grouping.Pharmaceutical compositions containing the compounds of formula I and methods for the use of the compounds are described and claimed.

Abstract: Steroids of the androstane series are described which possess a 3.alpha.-hydroxy group, a 5.alpha.- or 5.beta.- hydrogen atom, a 10- methyl group, an 11.alpha.- substituted amino group. The 17-position may be unsubstituted or substituted by a methyl or ethyl group in the .beta.-configuration or by an oxo group, or there may be a 16.beta., 17.beta.-epoxide group. A 2.beta.-alkoxy group may optionally be present.The compounds, particularly their salts, have anaesthetic activity.

Abstract: Pregnanes and androstanes are described which essentially possess a 3.alpha.-hydroxy group, a 5.alpha.-hydrogen atom or a 4.5- or 5,6-double bond, a 17.alpha.-hydrogen atom and an 11.beta.-aminoester group. Other optional substituents or double bonds may be present. The compounds have anaesthetic activity.

Abstract: The specification describes anti-inflammatory steroids having the following formula ##STR1## wherein X represents a hydrogen or fluorine atom, R' represents a methyl, ethyl, n-propyl or iso-propyl group, R" represents a methyl, chloromethyl, fluoromethyl, bromomethyl or 2-fluoroethyl group and represents a single or double bond. The specification describes processes for preparing such compounds as well as pharmaceutical compositions containing the compounds.

Abstract: The specification describes new anti-inflammatory steroids having the formula ##SPC1##Wherein R.sup.1 represents a C.sub.1-4 alkyl or halo- C.sub.1-4 alkyl group, R.sup.2 represents a methyl, ethyl, n-propyl or iso-propyl group (an ethyl group being especially preferred), X represents a hydrogen, chlorine or fluorine atom and -- represents a single or double bond.The specification describes processes for the preparation of such compounds as well as pharmaceutical compositions containing these compounds.