Abstract: Aromatic camptothecin ester compounds having the formula: are described as well as formulations containing the compounds. Methods of treating cancer and/or tumors are also disclosed.

Abstract: A process for preparing the anti-cancer drug camptothecin (CPT) and certain derivatives thereof. The process includes the reacting of three base reagents and a five-step process for synthesizing optically pure CPT in high overall yield from inexpensive starting materials.

Abstract: Novel water soluble C-ring analogues of 20(S)-camptothecin having the general formula 1. All the compounds of the formula 1 are prepared from the compounds of the general formula 2 having 20(S)-chiral carbon. The compounds of the formula 1 possess potent anti-cancer and anti-viral properties. The invention also provides an alternate process for the preparation of known C-5 substituted compounds of the formula 1.

Abstract: A method of synthesizing compounds having the formula via a 4+1 radical annulation/cyclization wherein the precursor is reacted with an aryl isonitrile having the formula wherein X is selected from the group consisting of Br and I, ≡Y is ≡N or ≡C—R3, R1, R2, and R6 are independently hydrogen, a normal alkyl group, a branched alkyl group, an allyl group, a benzyl group, an alkynyl group, a propargyl group, an alkoxyl group, a halogen group, a trialkylsilyl group, an amino group, an alkyl amino group, a dialkylamino group, an aminoalkyl group, a cyano group, or R16CO—, wherein R16 is an alkyl group, an alkoxyl group, or an amino group, R3 is hydrogen, a normal alkyl group, a branched alkyl group, an allyl group, a benzyl group, an alkynyl group, a propargyl group, an alkoxyl group, a halogen group, a trialkylsilyl group, an amino group, an alkyl amino group, a dialkylamino group, an aminoalkyl group, a cyano group, or R16CO

Abstract: The present invention relates to alkynyl-substituted camptothecins of formula (I) wherein X, R1, R2 are as defined herein, and the pharmaceutically salts thereof. These compounds are useful in therapy as antitumor agents.

Abstract: A compound has the formula in racemic form, enantiomerically enriched form or enantiomerically pure form. R6 is preferably —Si(R8R9R10) or —(R7)Si(R8R9R10), wherein R7 is an alkylene group, an alkenylene group, or an alkynylene group; and R8, R9 and R10 are independently a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group, an aryl group or a —(CH2)NR11 group, wherein N is an integer within the range of 1 through 10 and R11 is a hydroxy group, alkoxy group, an amino group, an alkylamino group, a dialkylamino group, a halogen atom, a cyano group, —SRc or a nitro group. R1-R can be broadly substituted. R5 is preferably a C1-10 alkyl group, an alkenyl group, an alkynyl group, or a benzyl group. R13 is preferably H, F or —CH3. R16 is R16 is —C(O)Rf or H. The E-ring (the lactone ring) may be opened. A method of synthesis of compound (1) and intermediates in the synthesis thereof are provided.

Abstract: The present invention provides covalent conjugates of topoisomerase I and topoisomerase II inhibitors. Such compounds have a structure according to formula I: TI—L—TII  (I) wherein: TI is a topoisomerase I inhibitor such as a camptothecin group; TII is a topoisomerase II inhibitor such as an amsacrine, ellipticine, epipodophyllotoxin, or anthracycline antibiotic group; and L is a linking group. The compounds are useful for inhibiting topoisomerase I and II enzymes, for promoting cellular differentiation, and for treating cancer.

Abstract: The present invention is directed to methods of forming esters of tertiary alcohols. The methods include reacting a compound containing a tertiary alcohol with an acyl heteroaromatic ion-based compound of the formula: wherein R1 is an aromatic or aliphatic acid residue; Y is O or S; Z is CR2 or N; X is selected from the group consisting of wherein R2 and R3 are independently selected from the group consisting of H, C1-6 alkyls, C1-6 substituted alkyls, C1-6 heteroalkyls, C3-8 branched alkyls, C3-8 cycloalkyls, C1-6 substituted heteroalkyls, aryls, substituted aryls, C1-6 alkyl aralkyls, C1-6 heteroalkyl aralkyls, C3-8 branched alkyl aralkyls and C3-8 cycloalkyl aralkyls; and R2′ is the same as R2 except that R2′ is not H; in the presence of a lanthanideIII metal-based catalyst and a base.

Abstract: Novel compounds, formulations and methods of treating patients with cancer are provided for in this invention. The compounds are derivatives of camptothecin, and specifically relate to compounds having novel substitutions at the C-7 position of the camptothecin scaffold B-ring. The formula I compounds are highly lipophilic, lactone stable, do not require metabolic activation, and are potent antineoplastic compounds.

Abstract: The invention concerns rhodamine derivatives of the general formulae in which Ca-Cd each denote a C atom, and Ca and Cb as well as Cc and Cd are either linked together by a single bond or by a double bond; X1 to X16 denote independently of one another halogen, sulfonic acid, hydrogen or an alkyl residue with 1-20 C atoms in which the alkyl residue can be substituted with one or several halogen or sulfonic acid residues; R1 and R2 are either identical or different and denote either hydrogen, alkyl with 1-20 C atoms, polyoxyhydrocarbyl units, phenyl or phenylalkyl with 1-3 carbon atoms in the alkyl chain in which the alkyl and/or phenyl residues can be substituted by one or several hydroxy, halogen, sulfonic acid, amino, carboxy or alkoxycarbonyl groups where alkoxy can have 1-4 carbon atoms, R1 contains at least one activatable group, R2 and X4 can be optionally linked together via a bridge composed of 0-2 C atoms.

Abstract: The present invention is directed to a method for selecting compounds for use in treating sickle cell disease in a patient. The method comprises the steps of selecting a first set of HbS ligands from a first group of chemical compounds, selecting from the first set of HbS ligands a seconds set that exhibit inhibition of HbS polymerization, and selecting from the second set a third set that display anti-sickling activity of red blood cells when in the presence thereof. The method may include the step of performing a methemoglobin S proteolysis assay measuring a percent protease protection for each compound. The method may additionally include the steps of measuring HbS aggregation, inhibition of protease, deoxy-HbS gelation inhibition activity, O2 affinity of HbS, and cytotoxic effect to cell activity. The method may further include assessing red blood cell morphology, and eliminating compounds that contain moieties that bind to heme.

Abstract: Intermediates for the synthesis of camptothecin of the formula II wherein: R1 is —(CH2)2NR1R2, where R1 is an amino protecting group and R2 is C2-C5 alkyl, hydroxyethyl or acetoxyethyl group, and of the formula III wherein: n is 1 or 2; R3 is hydrogen or —OR4, where R4 is hydrogen, —COR5, —CONHR6 or CH2OR7, where R5 is methyl or —CH2OCH3, R6 is isopropyl, phenyl or —CH2CH2Cl, and R7 is methyl, ethyl or —CH2CH2OCH3; with the proviso that when n is 2, R3 is not hydrogen.

Abstract: Novel water soluble C-ring analogues of 20(S)-camptothecin having the general formula 1, All the compounds of the formula 1 are prepared from the compounds of the general formula 2 having 20(S)-chiral carbon where R1 to R5 have the meaning given above. The compounds of the formula 1 possess potent anti-cancer and anti-viral properties.

Abstract: This invention relates to novel derivatives of camptothecin, and will, particularly to derivatives having a substitution at the C-7 position, or at one of the C-9, C-10, C-11 or C-12 positions, or to disubstituted derivatives having a first substitution at C-7 and a second at one of C-9, C-10, C-11 or C-12. The invention also includes methods of using the compounds as Topoisomerase I inhibitors to treat patients with cancer. The invention also includes pharmaceutical formulations which consist of the novel compounds in solution or suspension with one or more pharmaceutical excipients or dilutes.

Abstract: The present invention relates to glycoconjugates of camptothecin derivatives in which at least one carbohydrate component is linked via suitable spacers with the A or B ring of a camptothecin derivative. The invention furthermore relates to processes for preparing the compounds according to the invention and to their use as medicaments, in particular in connection with cancer.

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

Abstract: A conductive organopolysiloxane composition is provided which includes (A) 100 parts by weight of an organopolysiloxane; and (B) 0.1 to 800 parts by weight of a conductive material obtained by subjecting a member selected from the group consisting of a conductive metal, a conductive metal compound, a filler surface-treated with a conductive metal and a filler surface-treated with a conductive metal compound, to surface treatment with a compound selected from the group consisting of a compound represented by the formula (1) and a compound represented by the formula (2). ##STR1## wherein R.sup.1 represents --O-- or --NH--, and R.sup.2 represents a hydrogen atom or a phenyl group. This composition is useful for the formation of a silicone rubber having a sufficient electrical conductivity and also stably retainable of electrical conductivity almost without undergoing a change in electrical conductivity even in a high-temperature environment.

Abstract: The present invention relates to a process for preparing camptothecin and camptothecin analogs of Formula (I) from compounds of Formula (II) and to novel intermediates useful in their preparation, ##STR1## wherein R.sub.1 to R.sub.6 represent various substituents.

Abstract: The invention provides compounds of formula I: whereinR.sub.1 -R.sub.8 and X and Y have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer using compounds of formula I.

Abstract: 20S-Camptothecin derivatives in which the 7-position bears as a substituent --CN, --CH(CN)R.sub.4, --CH.dbd.C(CN)R.sub.4, --C(.dbd.NOH)NH.sub.2, --C(.dbd.NH)NH.sub.2, --CH.dbd.C(NO.sub.2)R.sub.4, --CH(CN)R.sub.5, --CH(CH.sub.2 NO.sub.2)R.sub.5, tetrazol-5-yl, 4,5-dihydrooxazol-2-yl, or 1,2,4-oxadiazolin-3-yl-5-one. These compounds are active as topoisomerase I inhibitors, and can be used as antitumor drugs.

Abstract: The present invention describes xanthene dyes, including rhodamines, rhodols and fluoresceins that are substituted one or more times by a sulfonic acid or a salt of a sulfonic acid. The dyes of the invention, including chemically reactive dyes and dye-conjugates are useful as fluorescent probes, particularly in biological samples.

Abstract: The present invention is directed to methods of forming esters of tertiary alcohols. The methods include reacting a compound containing a tertiary alcohol with an acyl heteroaromatic ion-based compound of the formula: ##STR1## wherein R.sub.1 is an aromatic or aliphatic acid residue;Y is O or S;Z is R.sub.2 N;X is selected from the group consisting of ##STR2## wherein R.sub.2 and R.sub.3 are independently selected from the group consisting ofH, C.sub.1-6 alkyls, C.sub.1-6 substituted alkyls, C.sub.1-6 heteroalkyls, C.sub.3-8, branched alkyls, C.sub.3-8 cycloalkyls, C.sub.1-6 substituted heteroalkyls, aryls, substituted aryls, except that R.sub.2 is not H when X is ##STR3## C.sub.1-6 alkyl aralkyls, C.sub.1-6 heteroalkyl aralkyls, C.sub.3-8, branched alkyl aralkyls and C.sub.3-8 cycloalkyl aralkyls; and R.sub.2 ' is the same as R.sub.2 except that R.sub.2 ' is not H;in the presence of a lanthanide.sup.III metal-based catalyst and a base.

Abstract: An extraction technique for the isolation of Camptothecin from plant matter of the Camptotheca Acuminata. The plant matter is loaded into a high-pressure vessel of a supercritical fluid extraction system and is pressurized with supercritical carbon dioxide to extract plant waxes or other waste. A modifier, preferably methanol, is then added resulting in the extraction of the Camptothecin into the solvent.

Abstract: Invented are substituted thieno (2,3-b)pyrazolo(3,4-d)pyridin-3-ones, pharmaceutical compositions containing these compounds, and methods of using these compounds to enhance erythropoiesis. Also invented are intermediates and processess used in preparing these compounds.

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

Abstract: A water soluble camptothecin derivative which is 20(S)-7-ethyl-9(N-methyl-N-phenyl)amidino-camptothecin and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them and a process for their preparation are described. The compound of the invention and its pharmaceutically acceptable salts are useful antitumor agents and are further charactcrised by having a remarkable therapeutic index.

Abstract: Derivatives of Camptothecin are disclosed, particularly derivatives having multiple substitutions at the `A`, `B` and `E` rings thereof. The novel compounds are useful in treating a wide variety of susceptible tumors and are potent inhibitors of Topoisomerase I.

Abstract: The present invention features proactive antitumor compounds of the following formula: ##STR1## wherein R.sup.1 is COOZ; Z being H, alkali metal, alkaline earth metal, an ammonium group which is optionally substituted with one or more alkyl groups, or a carboxyl protecting group; each of R.sup.2, R.sup.3, and R.sup.4, independently, is OH or OR.sup.a ; R.sup.a being a hydroxyl protecting group; X is benzene or pyridine, optionally substituted with R.sup.b ; R.sup.b being H, C.sub.1-5 alkyl, C.sub.1-5 alkoxy, NO.sub.2, F, Cl, Br, SO.sub.3 H, and CN; R.sup.5 is H or OH; and each of n and m, independently, is 0 or 1; or a salt thereof.

Abstract: Novel compounds, formulations and methods of treating patients with cancer are provided for in this invention. The compounds are derivatives of camptothecin, and specifically relate to compounds having novel substitutions at the C-7 position of the camptothecin scaffold B-ring. The formula I compounds are highly lipophilic, lactone stable, do not require metabolic activation, and are potent antineoplastic compounds.

Abstract: The present invention provides a 5,6-dihydrodibenzo[a,g]quinolizinium derivative and the salts thereof of formula (I) which specifically inhibits the sterol 14-reductase which is involved in the distal pathway of cholesterol biosynthesis, and the use of the compound of formula (I) for treating hypercholesterolaemia or hyperlipidaemia. ##STR1## wherein, R.sup.1 and R.sup.2 which may be the same or different from each other, represent a hydroxy group or an alkoxy group having 1 to 4 carbons or R.sup.1 and R.sup.2 together represent a methylenedioxy group;R.sup.3 represents a hydroxy group or an alkoxy group having 1 to 4 carbons;R.sup.

Abstract: A process for preparing S type 2-substituted hydroxy-2-indolidinyl-butyric ester compound [II]: ##STR1## wherein R.sup.0 is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of "R"(in which the nitrogen atom is protected), R.sup.1 and R.sup.2 are lower alkyl group, and E is ester residue, which is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, which comprises 2-ethylating 2-substituted hydroxy-2-indolidinylacetic ester compound [I]: ##STR2## wherein the symbols are as defined above.

Abstract: The present invention is directed to conjugates such as polymeric prodrugs of aromatic, hydroxyl-containing compounds and methods of making and using the same. These polymeric prodrugs are preferably esters of hydroxyl-containing aromatic compounds and are formed by reacting a desired aromatic, hydroxyl-containing compound with a substantially non-antigenic polymer so as to produce a transport form having an ester linkage between the aromatic compound and the polymer. Preferred aromatic hydroxyl-containing compositions include 10- and 11-hydroxycamptothecin derivatives. Methods of treatment are also disclosed.

Abstract: The novel compounds of the following chemical formulae (I) and (II) exhibit in vitro antifungal activity against fungi including cutaneous filamentous fungus, such as Epidermophyton, Microsporum, Trichophyton, Sporothrix schenckii, Aspergillus or Candida. The compounds of the present invention exhibit in vitro antifungal activity at the concentration of 1-100 .mu.g/ml. ##STR1## wherein R.sup.1, R.sup.2, and R.sup.4 may be the same or different, and represent C.sub.1 -C.sub.5 alkoxy, R.sup.3 represents hydrogen or C.sub.1 -C.sub.10 alkyl, A.sup.- represents inorganic acid ion, organic acid ion or halide, R.sup.5 represents hydrogen, pyridylmethyl, substituted pyridylmethyl or a group having the following chemical formula(XI) ##STR2## wherein Z.sup.1, Z.sup.2, Z.sup.3, Z.sup.4 and Z.sup.5 may be the same or different and represent hydrogen, halogen, C.sub.1 -C.sub.5 alkyl, trifluoromethyl, phenyl, substituted phenyl, nitro, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylamino, acetylamino, C.sub.1 -C.sub.

Abstract: The present invention relates to 9-amino-10-(1-naphthylsulfonyloxy)-20(S)-camptothecin, 9-amino-10-phenylsulfonyloxy-20(S)-camptothecin, 7-ethyl-9-amino-10-(p-toluensulfonyloxy)-20(S)-camptothecin, their pharmaceutically acceptable salts, a process for their preparation, pharmaceutically compositions comprising them and their use as antitumor agents.

Abstract: The present invention provides compounds of formula (I): ##STR1## wherein R.sub.1 -R.sub.7, W, X, Y, and Z have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are are useful as anticancer agents. Also disclosed are pharmaceutical compositions comprising one or more compounds of formula I, processes for preparing compounds of formula I, and intermediates useful for preparing compounds of formula I.

Abstract: A camptothecin analog characterized in that the hydroxy lactone of the camptothecin is a .beta.-hydroxy lactone or the corresponding .beta.-hydroxyacid, resulting from the opening of said lactone, or a derivative of said .beta.-hydroxyacid, or a Pharmaceutically acceptable salt thereof, is disclosed. In particular, compounds of formulae (I) and (II) are disclosed. Methods for preparing the compounds of formulae (I) and (II), pharmaceutical compositions containing said containing said compounds, and their use, particularly as topoisomerase inhibitors and antitumoral drugs, are also disclosed.

Abstract: Novel water soluble C-ring analogs of 20(S)-camptothecin having the formula 1. ##STR1## The compounds of the formula 1 are prepared from the compounds of the formula 12 having C-20(S) chiral carbon. The compounds of the formula 1 possess potent anti-cancer and anti-viral properties.

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.4 alkyl group, a C.sub.6 -C.sub.15 alkl group, a C.sub.3 -C.sub.8 cycloalkyl group, a C.sub.2 -C.sub.15 alkenyl group or a C.sub.2 -C.sub.15 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.2 -C.sub.15 alkenyl group, a C.sub.3 -C.sub.8 cycloalkyl group, or an epoxy group. Processes for mailing these derivatives and for using them in cancer treatment are also disclosed.

Abstract: The present invention is directed compositions of the formula: ##STR1## wherein: D is a residue of biologically active moiety;X is an electron withdrawing group;Y and Y' are independently O or S;(n) is zero (0) or a positive integer, preferably from 1 to about 12;wherein: R.sub.1 and R.sub.2 are independently 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;wherein: R.sub.3 is a substantially non-antigenic polymer, C.sub.1-12 straight or branched alkyl or substituted allyl, C.sub.5-8 cycloalkyl or substituted cycloalkyl, carboxyalkyl, carboalkoxy alkyl, dialkylaminoalkyl, phenylalkyl, phenylaryl or ##STR2## wherein: R.sub.4 and R.sub.5 are independently 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 or jointly form a cyclic C.sub.5 -C.sub.7 ring.

Abstract: The present invention is directed to a novel dopamine receptor ligands of the formula: ##STR1## pharmaceutical formulations of such compounds, and a method using such compounds for treating a patient suffering from dopamine-related dysfunction of the central or peripheral nervous system.

Abstract: A compound represented by Chemical Formula (1), and salts thereof are provided. A process for production thereof is also provided. The fluoroethylcamptothecin derivative has high antineoplastic activity, being less toxic, and water-soluble, thus is a useful compound.

Abstract: A process for preparing S type 2-substituted hydroxy-2-indolidinyl-butyric ester compound ?II!: ##STR1## wherein R.sup.o is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of "R"(in which the nitrogen atom is protected), R.sup.1 and R.sup.2 are lower alkyl group, and E is ester residue, which is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, which comprises 2-ethylating 2-substituted hydroxy-2-indolidinylacetic ester compound ?I!: ##STR2## wherein the symbols are as defined above.

Abstract: A method is disclosed for the preparation of 9-nitrocamptothecin which involves reacting 20-camptothecin with at least one inorganic nitrate salt and at least one acid effective in catalyzing the formation of a nitronium ion, where the reaction occurs at a temperature and for a time sufficient to form the 9-nitrocamptothecin. Also, methods of further purifying the 9-nitrocamptothecin by column chromatography or by reprecipatation is also disclosed.

Abstract: The present invention relates to compounds of the following formulas: ##STR1## which are endowed with antitumor activity. The invention also relates to methods of treating tumors using these compounds.

Abstract: Novel compounds, formulations and methods of treating patients with cancer are provided for in this invention. The compounds are derivatives of camptothecin, and specifically relate to compounds having novel substitutions at the C-7 position of the camptothecin scaffold B-ring. The formula I compounds are highly lipophilic, lactone stable, do not require metabolic activation, and are potent antineoplastic compounds.

Abstract: A camptothecin derivative comprising a compound of the formula ?I!: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are (A) adjacent two groups combine to form alkylene, or both are H, and one of the remaining three groups is --X.sub.n --Alk.sub.m --R.sup.6, and the other two are H, alkyl or halogen, or (B) adjacent two groups combine to form alkylene, and one of the carbon atoms of said alkylene group is substituted by --X.sub.n --Alk.sub.m --R.sup.6, and the remaining three groups are H, alkyl or a halogen, and one or two --CH.sub.2 -- of the alkylene in (A) or (B) may optionally be replaced by --O--, --S-- or --NH--, X is --O-- or --NH--, Alk is alkylene, R.sup.6 is --NH.sub.2, ##STR2## or --OH, m and n are both 0 or 1, or m is 1 and n is 0, which camptothecin compound is bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof.

Abstract: High molecular weight, water-soluble prodrugs of the formula: ##STR1## wherein: D is a biologically active moiety;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 all moieties or ##STR2## are disclosed. In preferred embodiments, the prodrugs contain a polyethylene glycol having a molecular weight of at least about 20,000.

Abstract: This invention is concerned with 2-ureido-benzamide compounds of the formula (1) ##STR1## in which R.sup.1 is H, halogen atom, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy or (C.sub.1 -C.sub.4)dialkylamino and R.sup.2 is H, halogen atom, hydroxy, nitro, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, (C.sub.3 -C.sub.6) cycloalkylmethoxy, (C.sub.1 -C.sub.4) alkylthio, (C.sub.1 -C.sub.4) alkylsulfinyl, (C.sub.1 -C.sub.4)alkylsulfonyl or ##STR2## wherein j is an integer of from 0 to 2 and R.sup.3 and R.sup.4 are each independently H, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkanoyl, (C.sub.1 -C.sub.4)alkylsulfonyl or (C.sub.1 -C.sub.4)alkylcarbamoyl, NR.sup.3 R.sup.4 can to form a pyrrolidine, piperidine, morpholine, imidazole or pyrazole ring;X is a (C.sub.3 -C.sub.15)alkyl, (C.sub.3 -C.sub.6) cycloalkyl, (C.sub.3 -C.sub.6) cycloalkylmethyl, .omega.-(C.sub.1 -C.sub.4) alkoxy-(C.sub.1 -C.sub.4) alkyl group or ##STR3## wherein k is an integer of from 1 to 4 and R.sup.5 and R.sup.

Abstract: A process for isolating berberine from plants is described. An oral formulation of berberine is described.

Abstract: The present invention relates to substituted camptothecin derivatives of formula (I) wherein the symbol - - - - represents a single or double bond; R.sub.1, R.sub.2 and R.sub.3 are as defined under (a) or (b) below: (a) R.sub.1 and R.sub.2 are, each independently, hydrogen; C.sub.1 -C.sub.4 alkyl; C.sub.3 -C.sub.7 cycloalkyl; phenyl C.sub.1 -C.sub.6 alkyl; an optionally substituted phenyl ring; --NR.sub.5 R.sub.6 wherein one of R.sub.5 and R.sub.6 is hydrogen, C.sub.1 -C.sub.6 alkyl or benzyl and the other is hydrogen, C.sub.1 -C.sub.6 alkanoyl, an optionally substituted C.sub.1 -C.sub.6 alkoxycarbonyl, an optionally substituted benzoyl, phenyl C.sub.1 -C.sub.6 alkanoyl, an optionally substituted C.sub.1 -C.sub.6 alkoxycarbonyl, an optionally substituted phenoxycarbonyl or phenyl C.sub.1 -C.sub.6 alkoxycarbonyl, or R.sub.5 and R.sub.6, combined together with the nitrogen atom to which they are linked, form a 4-7 membered saturated, optionally substituted, heteromonocyclic ring residue; COOR.sub.8 wherein R.