Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.

Abstract: 9-Amino camptothecin of formula (I) ##STR1## is prepared by: 1) reducing a compound of formula (II): ##STR2## wherein Hal is 10- or 12-halogen, in a single step to the 9-amino-camptothecin of formula (I) or, alternatively, 2a) reductively removing the Hal group from a compound of formula (II) so obtaining the compound of formula (III): ##STR3## and 2b) reducing the compound of formula (III) so obtaining the 9-amino camptothecin of formula (I); the said steps 1 and 2a) and, optionally, step 2b) each being carried out in the presence of a catalytic amount of a compound of formula PdL.sub.2 wherein L is acetate or halogen and, additionally, in the presence of an ammonium formate as a hydrogen source. The 9-amino camptothecin of formula (I) is useful as inhibitor of the enzyme topoisomerase I. It is useful in the treatment of cancers, in particular leukaemia, colon and rectal tumours.

Abstract: A process for removal of heavy metal contaminants from organic compounds, especially campthothecin analogs.

Abstract: The present invention is directed compositions of the formula: ##STR1## wherein: D is a biologically active moiety;X is an electron withdrawing group;Y and Y' are independently O or S;R.sub.1 is selected from the group consisting of H, C.sub.1-6 alkyls, aryls, substituted aryls, aralkyls, heteroalkyls, substituted heteroalkyls and substituted C.sub.1-6 alkyls;(n) is an integer from 1 to about 12; andR.sub.2 is a polyalkylene oxide.In preferred embodiments, the prodrugs contain a polyethylene glycol having a molecular weight of at least about 20,000.

Abstract: A compound of formula (I): ##STR1## in which R.sup.1, R.sup.2, X and Y are as defined in the description, the isomers thereof and the addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same are useful in the treatment of certain cancers.

Abstract: A polymeric conjugate consists essentially of: (i) from 60 to 99 mol % of N-(2-hydroxypropyl) methacryloylamide units represented by formula 1: ##STR1## (ii) from 1 to 40 mol % of 20-0-(N-methacryloylglycyl-aminoacyl) camptothecin units represented by formula 2 ##STR2## wherein ?A! is a spacer group having respective terminal amino and carbonyl groups which are separated by at least three atoms and O-CPT represents a residue of a camptothecin, the C-20 hydroxy group of the camptothecin being linked to the terminal carbonyl group of the spacer group ?A!; and (iii) from 0 to 10 mol % of N-methacryloylglycine or N-(2-hydroxy-propyl)methacryloylglycinamide units represented by formula 3: ##STR3## wherein Z represents hydroxy or a residue of formula --NH--CH.sub.2 --CH(OH)--CH.sub.3.

Abstract: Pentacyclic derivatives having the general formulae (Ia), (Ib) and (Ic) ##STR1## denote: hydrogen, alkyl with 1 to 20 carbon atoms polyoxyhydrocarbyl, phenyl, phenylalkyl with 1 to 3 carbon atoms in the alkyl chain, wherein the alkyl residues or/and phenyl residues can be substituted by one or several hydroxy, halogen, sulfo, carboxy or alkoxycarbonyl groups in which alkoxy can have 1 to 4 carbon atoms;R.sup.7 denotes an alkyl group with 1 to 7 carbon atoms, substituted by at least one halogen, or denotes a carboxyalkyl group or a phenyl group which is substituted by a carboxy or alkoxycarbonyl group located at the o-position relative to the carbon atom bound to the pentacyclic ring system and by at least one halogen, wherein alkoxy can have 1 to 4 carbon atoms, or a carboxymethylene-oxy-alkyloxy group; the residues R.sup.14 and R.sup.

Abstract: A process for the preparation of water soluble camptothecin analogs, including methods for the preparation of intermediates thereof, and the compounds prepared by said process. Water soluble camptothecin analogs are prepared which may be used for inhibiting the growth of tumor cells sensitive to such analogs.

Abstract: Derivatives of camptothecin are disclosed and are represented by the general formula: ##STR1## wherein when R.sub.2 is H, R.sub.1 is a C.sub.2 -C.sub.15 alkyl group, a C.sub.2 -C.sub.15 alkenyl group or an epoxy group; and when R.sub.2 is a nitro group, R.sub.1 is a C.sub.1 -C.sub.15 alkyl group, a C.sub.1 -C.sub.15 alkenyl group or an epoxy group. Processes for making these derivatives and for using them in cancer treatment are also disclosed.

Abstract: To produce defined isomer mixtures of compounds with spirocyclic beta-aminocarboxyl and/or beta-aminocarbonyl systems the invention supposes that they be dissolved in solvents which have good dissolving power for these compounds, whose relative permittivity is sufficient to stabilize the amphoteric intermediates occuring in isomerization, which as proton donors constitute hydrogen bridges, whose basicity is less than that of the compounds for isomerization and whose boiling point is so high that an adequate reaction speed can be attained by raising temperature. Further, the invention proposes that the isomerization be prevented, influenced, or terminated by altering at least one of these factors and or by altering the temperature.

Abstract: Non-toxic camptothecin prodrugs are prepared by esterifying the 20-position hydroxyl group of camptothecin derivatives.

Abstract: A process for preparing 9-amino camptothecin comprising the steps of: (1) reacting a compound of formula (III) ##STR1## wherein the hydroxy group on ring A is in the 10- or 12-position, with a nitrating agent, to form the corresponding 9-nitro compound; (2) converting the 9-nitro compound into a corresponding compound of formula (V) ##STR2## wherein XO is a group that can be removed reductively; and (3) reductively removing the XO group and reducing the nitro group of the compound of formula (V), to form the 9-amino camptothecin, a known antitumor compound. The present invention also includes compound having the above formula (V) and their 9-amino analogs, which have antitumor activity.

Abstract: Water-soluble prodrugs of the formula: ##STR1## wherein: D is a biologically active nucleophile;M is X or Q;x is an electron withdrawing group;Q is a moiety containing a free electron pair positioned five or six atoms from Y';Y and Y' are oxygen or sulfur;R is a polyalkylene oxide; andZ is OH, C.sub.1-4 alkyl moieties or ##STR2## are disclosed.

Abstract: Methods for purifying 20(S)-camptothecin are described. The 20(S)-camptothecin in purified form is useful in the treatment of cancer.

Abstract: The present invention relates to new camptothecin derivatives of the formula (I) ##STR1## wherein B is a group B' or B" ##STR2## wherein each of (x) and (y) is a single or double bond. The present invention also provides processes for their preparation as well as pharmaceutical compositions containing the same.

Abstract: Compounds of formula (I): ##STR1## wherein R.sub.3, R.sub.4, R.sub.5, R.sub.6, X and Y are defined in the description.Those compounds are used therapeutically in the treatment of cancerous tumours.

Abstract: Substituted analogues of camptothecin possessing cytotoxic activity towards cancer cells, of the general structure: ##STR1## wherein E is H, CO.sub.2 R, CONH.sub.2, CONHR, CONR.sub.2, acyl, or CN; X is H, OH, or OR; R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, or hydroxyalkyl group, or an aryl group; R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, alkoxy, hydroxyalkyl, or aminoalkoxy group, or an aryl or aryloxy group, or a C-glycal, or CO.sub.2 R, nitro, cyano, Cl, F, Br, I, SR.sup.10, NR.sup.11 R.sup.12, OR.sup.13 ; R is H, or a linear or branched chain alkyl, alkylaryl, or hydroxyalkyl group, or an aryl group; R.sup.10, R.sup.11 and R.sup.12 are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, hydroxyalkyl, or acyl group, or an aryl group; R.sup.

Abstract: Methods for purifying 20(S)-camptothecin are described. The 20(S)-camptothecin in purified form is useful in the treatment of cancer.

Abstract: Substituted analogues of camptothecin possessing cytotoxic activity towards cancer cells, of the general structure: ##STR1## wherein E is H, CO.sub.2 R, CONH.sub.2, CONHR, CONR.sub.2, or CN; R.sup.0 and R.sup.1 are independently the same or different and are H, or a linear or branched alkyl, linear or branched alkylaryl, hydroxyalkyl or aryl group; R.sup.2, R.sup.3 and R.sup.4 are independently the same or different and are H, or a linear or branched alkyl, linear or branched alkylaryl, hydroxyalkyl or aryl group; R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are independently the same or different and are H, or a linear or branched alkyl, linear or branched alkylaryl or aryl group, or an alkoxy, aryloxy, hydroxyalkyl, C-glycal, nitro, cyano or aminoalkoxy group, or CO.sub.2 R, Cl, F, Br, I, SR.sup.10, NR.sup.11 R.sup.12 or OR.sup.13 ; R is H, an alkyl, aryl, alkylaryl or hydroxyalkyl group; R.sup.10, R.sup.11 and R.sup.

Abstract: The present invention relates to novel alkaloids from Mappia foetida, foetidine 1 and 2, having anticancer and antiviral properties. These alkaloids, soluble in water, are present in all the parts of the plant, and are the precursors of camptothecin and of 9-methoxy-camptothecin, which are alkaloids known to have pharmacodynamic properties but also to be insoluble in water. The particular water solubility of the novel compounds make them particularly suitable for the treatment of the patients by the parenteral route, avoiding the use of toxic excipients or of unsuitable chemical derivatizations.

Abstract: Disclosed are new methods of making camptothecin and camptothecin analogs defined by Formula I: ##STR1## wherein R is loweralkyl; R.sub.1 is H, loweralkyl, loweralkoxy, or halo; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkylthiol, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, aminomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom. The methods comprise cyclizing a compound of Formula IV: ##STR2## wherein X is Br or I, and Y is H, by an Aryl-to-Aryl free radical coupling reaction to yield a compound of Formula I. Compounds of Formula IV are made by alkylating a compound of Formula III: ##STR3## wherein R is loweralkyl and Y is H with a compound of Formula II-x: ##STR4## wherein X is a Br or I and V is hydroxy, by a Mitsunobu reaction to yield the compound of Formula IV.

Abstract: The novel compounds 11-hydroxy-7-ethyl camptothecin and 11-hydroxy-7-methoxy camptothecin (11,7-HECPT and 11,7-HMCPT) are active anticancer compounds which are poorly soluble in water. Because of their novelty, 11,7-HECPT and 11,7-HMCPT derivatives have not been directly administered by parenteral or oral routes to human subjects as an antitumor composition for the purpose of inhibiting the growth of cancer cells. The claimed compositions are useful as compared to the water soluble camptothecin derivatives, such as CPT-11, in clinical trials. The unpredictable interpatient variability in the metabolic production of an active metabolite from CPT-11 limits the utility of CPT-11. This invention overcomes these limitations by claiming novel pharmaceutically acceptable lactone stable formulations of 11,7-HECPT or 11,7-HMCPT, to directly administer to patients.

Abstract: The present invention provides a process for the asymmetric synthesis of camptothecin analogs as well as novel chemical intermediates of Formula I, II, and III. In general, the present process comprises conversion of a cis dioxolanone, having the same desired absolute configuration as the desired camptothecin analog, to a compound of Formula I, II, or III, which compound is then converted to the desired camptothecin analog.

Abstract: A method of making racemic DE ring intermediates for the synthesis of camptothecin and camptothecin analogs employing novel intermediates of Formula (XX) and (XXI): ##STR1## wherein R.sub.20 is loweralkyl, R is loweralkyl, Y is H or halogen, and R.sub.21 is loweralkoxy; as precursors to the DE ring intermediate.The present invention also provides a camptothecin analog of Formula (I-A): ##STR2## wherein: Hal is a halogen;and the remainder of the variables are as defined in the specification.Additionally, other novel compounds useful in the preparation of the compounds of Formula (I-A) and methods of producing compounds of (I-A) are also provided.

Abstract: Substituted analogues of camptothecin possessing cytotoxic activity towards cancer cells, of the general structure: ##STR1## wherein E is H, CO.sub.2 R, CONH.sub.2, CONHR, CONR.sub.2, acyl, or CN; X is H, OH, or OR; R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently the same or different and are H, linear or branched alkyl, linear or branched alkylaryl, hydroxyalkyl, or aryl; R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 are independently the same or different and are H, linear or branched alkyl, linear or branched alkylaryl, aryl, CO.sub.2 R, alkoxy, aryloxy, hydroxyalkyl, C-glycal, nitro, cyano, aminoalkoxy, Cl, F, Br, I, SR.sup.10, NR.sup.11 R.sup.12, or OR.sup.13 ; R is H, alkyl, aryl, alkylaryl, hydroxyalkyl, or hydroxyalkyl; R.sup.10, R.sup.11 and R.sup.12 are independently the same or different and are H, alkyl, aryl, alkylaryl, hydroxyalkyl, or acyl; R.sup.13 is glycosyl; n is 0 or 1; with the proviso that when R.sup.1 is ethyl, and n is 0, E, R.sup.2, R.sup.3, and R.sup.4 are not all H.

Abstract: A method of making racemic DE ring intermediates for the synthesis of camptothecin and camptothecin analogs employing novel intermediates of Formula XX and XXI: ##STR1## as precursors to the DE ring intermediate. The present invention also provides camptothecin analog of Formula I-A ##STR2## wherein: Hal is a halogen is selected from the group consisting of F, Cl, and Br;R may be loweralkyl;R.sub.1 may be H, loweralkyl, loweralkoxy, or halo;R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may each independently be H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkyl-thio, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, amninomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom.Additionally, novel compounds useful in the preparation of the compounds of Formula I-A are also provided.

Abstract: Trans-hexahydrobenzo[a]phenanthridine of the formula ##STR1## wherein R is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sub.1 is hydrogen or a phenoxy protecting group, X is fluoro, chloro, bromo, iodo or a group of the formula--OR.sub.5, and R.sub.2, R.sub.3, and R.sub.4 are independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl, fluoro, chloro, bromo, iodo, or a group --OR.sub.1 provided that at least one of R.sub.2, R.sub.3, and R.sub.4 are other than hydrogen, are novel ligands for dopamine receptors.

Abstract: There are described rhodamine derivatives of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each hydrogen or substituted or unsubstituted C.sub.1 -C.sub.4 -alkyl, or R.sup.2 is paired off with R.sup.5 or R.sup.4 with R.sup.6 to form 1,3-propylene, which can be substituted,R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are each hydrogen or methyl,R.sup.9 is hydrogen, substituted or unsubstituted C.sub.1 -C.sub.4 -alkyl or a radical of the formula (C.sub.2 H.sub.4 O--).sub.n H, where n is 2 or 3, andAn.sup..crclbar. is the equivalent of an anion derived from an addition or condensation polymer that contains acid groups, novel cyclic rhodamine dyes, and the use of the novel rhodamine derivatives and cyclic rhodamine dyes for dyeing polyacrylonitrile fibers, for incorporation into polymers or for preparing inks.

Abstract: The present invention provides a process for the asymmetric synthesis of camptothecin analogues as well as novel chemical intermediates of Formula I, II, and III. In general, the present process comprises conversion of a cis dioxolanone, having the same desired absolute configuration as the desired camptothecin analogue, to a compound of Formula I, II, or III, which compound is then converted to the desired camptothecin analogue.

Abstract: A method for synthesizing camptothecin and camptothecin analogs using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogs produced by the process. The camptothecin analogs are effective inhibitors of topoisomerase. I and show antileukemic and anti-tumor activity.

Abstract: Substituted analoguss of camptothecin possessing cytotoxic activity towards cancer cells, of the general structure: ##STR1## wherein E is H, CO.sub.2 R, CONH.sub.2, CONHR, CONR.sub.2, acyl, or CN; X is H OH, or OR; R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, or hydroxyalkyl group, or an aryl group; R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, alkoxy, hydroxyalkyl, or aminoalkoxy group, or an aryl or aryloxy group, or a C-glycal, or CO.sub.2 R, nitro, cyano, Cl, F, Br, I, SR.sup.10, NR.sup.11 R.sup.12, or OR.sup.13 ; R is H, or a linear or branched chain alkyl, alkylaryl, or hydroxyalkyl group, or an aryl group; R.sup.10, R.sup.11 and R.sup.12 are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, hydroxyalkyl, or acyl group, or an aryl group; R.sup.

Abstract: Methods for purifying camptothecin compounds are described. The camptothecin compounds in purified form are useful in the treatment of cancer.

Abstract: The present invention relates to the synthesis of water soluble, camptothecin derivatives of formula (I), ##STR1## wherein: n represents the integer 1 or 2;R.sup.1 represents independently, hydrogen, lower alkyl, (C.sub.3-7)cycloalkyl, (C.sub.3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy lower alkyl; andR.sup.2 represents hydrogen andthe pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to certain substituted tetracyclic fused quinoline derivatives of formula (I): ##STR1## wherein: R.sup.1 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo, methoxy or amino;R.sup.2 is hydrogen, hydroxy, methoxy or amino;R.sup.3 is hydrogen, hydroxy, methoxy, methoxymethoxy, amino, --OCONH.sub.2, [2(5H)-3,4-dihydro-3-oxyfuranone], 2-hydroxyethoxy, 2-aminoethoxy, 3-hydroxypropoxy or 3-aminopropoxy; or taken together with R.sup.2 or R.sup.4, methylenedioxy or ethylenedioxy;R.sup.4 is hydrogen, hydroxy or amino;Z is --CH.sub.2 --, --O-- or --NH--; anda) X.sup.1 is hydrogen;X.sup.2 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo or methoxy; andX.sup.3 is hydrogen or hydroxy; orb) X.sup.2 taken together with X.sup.3 is methylenedioxy or ethylenedioxy, and X.sup.1 is hydrogenor a pharmaceutically acceptable salt thereof provided that:i) at least one of R.sup.1 through R.sup.4 is other than hydrogen.

Abstract: Compounds which are useful as substrates for enzymes are disclosed. An enzyme-controlled process is provided for generating a colored species from an initially substantially colorless material as a result of enzymatic attack. The process can be exploited to provide an enzyme-amplified diagnostic assay method to detect an analyte of interest present in a test sample.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: Compounds of Formula I ##STR1## are made in accordance with the following scheme: ##STR2## wherein R may be loweralkyl; R.sub.t may be H, loweralkyl, loweralkoxy, or halo: R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may each independently be H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkylthio, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, aminomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom; Y is H and W and X are halogen. Also disclosed are novel processes for making starting materials for the scheme given above, and novel intermediates employed in these processes.

Abstract: The invention provides a process for preparing single enantiomers of compounds represented by the formula: ##STR1## and chiral acid addition salts thereof; wherein: X and Y are independently hydrogen; lower alkyl; lower alkoxy; or halo; or X and Y taken together is methylenedioxy or ethylene-1,2-dioxy;which includes reduction of a compound represented by the formula: ##STR2## to give a mixture of stereoisomers represented by the formula: ##STR3## wherein each wavy line independently represents a bond in either the .alpha. or .beta. position;followed by dissolving the mixture of stereoisomers and a chiral resolving acid in a suitable solvent and allowing the solution to crystallize, giving a salt of the desired enantiomer.

Abstract: Compounds of the formula ##STR1## wherein: m is an integer of 1-6;n is an integer of 1 or 2;X and Y are independently hydrogen; hydroxy; lower alkyl; lower alkoxy; or halo; or X and Y when adjacent and taken together are methylenedioxy or ethylene-1,2-dioxy;R is ##STR2## wherein: R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl, or when taken together with the carbon to which they are attached are cycloalkyl;R.sup.3 is hydrogen, lower alkyl, lower alkoxy, hydroxy, trifluoromethyl or halo; and ##STR3## and pharmaceutically acceptable acid addition salts thereof. The compounds and salts exhibit useful pharmacological properties, including selective .alpha..sub.2 -adrenoceptor antagonist properties and 5-HT.sub.1A receptor partial agonist properties, and are particularly useful for the treatment of sexual dysfunction, depression and anxiety.

Abstract: A method for synthesizing camptothecin and camptothecin analogs using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogs produced by the process. The camptothecin analogs are effective inhibitors of topoisomerase I and show antileukemic and anti-tumor activity.

Abstract: The present invention relates to certain substituted tetracyclic fused quinoline derivatives of formula (I): ##STR1## wherein: R.sup.1 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo, methoxy or amino;R.sup.2 is hydrogen, hydroxy, methoxy or amino;R.sup.3 is hydrogen, hydroxy, methoxy, methoxymethoxy, amino, --OCONH.sub.2, [2(5H)-3,4-dihydro-3-oxyfuranone], 2-hydroxyethoxy, 2-aminoethoxy, 3-hydroxypropoxy or 3-aminopropoxy; or taken together with R.sup.2 or R.sup.4, methylenedioxy or ethylenedioxy;R.sup.4 is hydrogen, hydroxy or amino;Z is --CH.sub.2 --, --O-- or --NH--; anda) X.sup.1 is hydrogen; X.sup.2 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo or methoxy; and X.sup.3 is hydrogen or hydroxy; orb) X.sup.2 taken together with X.sup.3 is methylenedioxy or ethylenedioxy, and X.sup.1 is hydrogenor a pharmaceutically acceptable salt thereof provided that:i) at least one of R.sup.1 through R.sup.4 is other than hydrogen;ii) when R.sup.1 is methoxy, R.sup.2 is hydroxy or methoxy, R.sup.

Abstract: Polycyclic diamines, incorporating a basic framework similar to [3.3.3]propellane, and derivatives of the basic polycyclic diamines and a process for preparing same are provided. The diamines are prepared by subjecting bispyridine compounds to electroreductive coupling in an acidic solution. The polycyclic diamines and derivatives thereof are useful as chain extenders, crosslinking agents and curatives in various polymer systems.

Abstract: The present invention relates to racemic or optically active cis octahydro-indolo [2,3-a] quinolizine diester derivatives.

Abstract: Novel heterocyclic alkaloids were isolated from a marine sponge. These compounds, and derivatives thereof, are useful antifungal and antitumor compounds. The novel compounds have the following structures: ##STR1## wherein R.sub.1 =H, alkyl, alkenyl, aryl, benzyl, acyl, benzoyl, or alkali metal;R.sub.2 and R'.sub.2 =O, S, NOX, or NNHX, wherein X is alkyl or aryl.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: A camptothecin analog having the structure shown below: ##STR1## where Z is H or C.sub.1-8 alkyl and R is NO.sub.2, NH.sub.2, N.sub.3, hydrogen, halogen, COOH, OH, O--C.sub.1-3 alkyl, SH, S--C.sub.1-3 alkyl, CN, CH.sub.2 NH.sub.2, NH--C.sub.1-3 alkyl, CH.sub.2 --NH--C.sub.1-3 alkyl, N(C.sub.1-3 alkyl).sub.2, CH.sub.2 N(C.sub.1-3 alkyl).sub.2, O--, NH--, or S--CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 OH).sub.2, O--, NH-- or S-- CH.sub.2 CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 OH).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 CH.sub.2 OH).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 CH.sub.2 OH.sub.2).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 N(C.sub.1-3 alkyl).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 CH.sub.2 N(C.sub.1-3 alkyl).sub.2, CHO, C.sub.1-3 alkyl or NHCOCHR.sup.1 NR.sup.2 R.sup.3, where R.sup.1 is the side-chain of an .alpha.-amino acid and R.sup.2 and R.sup.3, independently are hydrogen or a lower alkyl group or R.sup.

Abstract: Compounds of Formula I ##STR1## are made in accordance with the following scheme: ##STR2## wherein R may be loweralkyl; R.sub.1 may be H, loweralkyl, loweralkoxy, or halo; R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may each independently be H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkylthio, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, aminomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom; Y is H and W and X are halogen. Also disclosed are novel processes for making starting materials for the scheme given above, and novel intermediates employed in these processes.

Abstract: New intermediate compounds are disclosed of the formula I, ##STR1## wherein R.sub.1 and R.sub.2 are independently alkyl having 1 to 4 carbon atoms,or acid-addition salts thereof of formula Ib, ##STR2## wherein X represents an acid residue, and a process for the preparation of the intermediate compounds.

Abstract: A method for synthesizing camptothecin and camptothecin analogs using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogs produced by the process. The camptothecin analogs are effective inhibitors of topoisomerase I and show anti-leukemic and anit-tumor activity.

Abstract: The present invention relates to a method of manufacturing aromatic urethane, an aromatic mononitro-compound, an aromatic primary amine, and carbon monoxide being reacted using a catalyst containing a platinum group metal-containing compound as a major constituent to prepare N,N'-di-substituted urea. The resultant N,N'-di-substituted urea is reacted with a hydroxyl group-containing organic compound to prepare an aromatic primary amine and aromatic urethane, and the aromatic primary amine is separated to obtain aromatic urethane.