Abstract: Emulsome compositions comprising phosphatidylcholine, cholesterol, tristearin, and one or more lipophilic bioactive agents such as vinpocetine are provided. The emulsomes may further comprise surface modifications of either [N-(carbonyl-methoxypropylethyleneglycol-2000)-1,2-distearoyl-sn-glycero-3-phosphoethanolamine, sodium salt] (MPEG-DSPE) for peglyation or stearylamine for cationization. Methods of improving brain delivery of lipophilic bioactive agents by intranasally administering such emulsome compositions are also provided.

Abstract: Emulsome compositions comprising phosphatidylcholine, cholesterol, tristearin, and one or more lipophilic bioactive agents such as vinpocetine are provided. The emulsomes may further comprise surface modifications of either [N-(carbonyl-methoxypropylethyleneglycol-2000)-1,2-distearoyl-sn-glycero-3-phosphoethanolamine, sodium salt] (MPEG-DSPE) for peglyation or stearylamine for cationization. Methods of improving brain delivery of lipophilic bioactive agents by intranasally administering such emulsome compositions are also provided.

Abstract: Disclosed embodiments concern polycyclic alkaloid compounds and methods for their use and synthesis. Particular embodiments concern polycyclic alkaloids having a fused, six-membered ring, while other embodiments concern polycyclic alkaloids having a fused, five-membered ring. Methods for making the polycyclic alkaloids are disclosed, as well as methods for their use as prophylactics or treatments for certain diseases. Also disclosed are pharmaceutical compositions comprising the polycyclic alkaloids and their use.

Abstract: The present invention provides random copolymers containing phosphorylcholine and one or more functional agents, and methods of preparing such random copolymers.

Abstract: Disclosed embodiments concern polycyclic alkaloid compounds and methods for their use and synthesis. Particular embodiments concern polycyclic alkaloids having a fused, six-membered ring, while other embodiments concern polycyclic alkaloids having a fused, five-membered ring. Methods for making the polycyclic alkaloids are disclosed, as well as methods for their use as prophylactics or treatments for certain diseases. Also disclosed are pharmaceutical compositions comprising the polycyclic alkaloids and their use.

Abstract: The present invention relates to pharmaceutical technical field, to melonine bisindole compounds, pharmaceutical compositions thereof, and preparation methods thereof. Specifically, the present invention relates to melonine bisindole compounds of Formula I, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts thereof. The present invention further relates to method for preparing the melonine bisindole compounds of Formula I or pharmaceutically acceptable salts thereof, and the use of the melonine bisindole compounds of Formula I or pharmaceutically acceptable salts thereof in the manufacture of a medicament for the treatment or prophylaxis of cancers.

Abstract: The present invention relates to compounds of the formula (1), formula (2), formula (3) and formula (4) which are suitable for use in electronic devices, in particular organic electroluminescent devices.

Abstract: A camptothecin-containing pharmaceutical composition which contains: (a) camptothecin or a derivative thereof, and (b) one or more compounds selected from among ascorbic acid or a salt thereof, sodium hydrogen sulfite, sodium sulfite, potassium pyrosulfite, sodium erythorbate, sodium thioglycolate, sodium pyrosulfite, and ?-thioglycerin. The pharmaceutical composition is useful in that, after storage for a long period of time or under light-irradiation conditions, camptothecin or a derivative thereof contained therein undergoes minimum degradation.

Abstract: An objective of the present invention is to provide water-soluble prodrugs that can be administered parenterally, and which show excellent water solubility and small interspecies or individual differences and are rapidly converted to the active form by chemical conversion. This invention provides water-soluble prodrugs represented by formula (1), or pharmaceutically acceptable salts, or hydrates or solvates thereof, (wherein, R1 represents a hydrogen atom, or C1-C6 alkyl group; W represents a divalent group comprising a tertiary amino group or sulfonyl group; and Y represents a residue of a compound represented by Y—OH comprising an alcoholic hydroxyl group).

Abstract: The present invention relates to the use, for the preparation of a medicament intended for the treatment or the prevention of pathologies linked to, or caused by mycobacteria, of at least one of the compounds of the following formula (I): in which B represents in particular a nitrogen atom, and R1, R2, R3, R4, R5, R6, R7 and R8 represent in particular a hydrogen atom.

Abstract: Compound of formula (I): wherein: R1, R2, R3, R4, R5, R80, R90, R81, R91, Alk and G are as defined in the description. Medicinal products containing the same which are useful in the treatment of cancer diseases.

Abstract: Compound of formula (I): wherein: R1, R2, R3, R4, R5, R80, R90, R81, R91, Alk, Alk?, X, X? and G are as defined in the description. Medicinal products containing the same which are useful in the treatment of cancer diseases.

Abstract: The invention provides vinblastine derivatives represented by the following formula 1 or their physiologically acceptable salts, their preparation, use and pharmaceutical compositions comprising the said derivatives. The said vinblastine derivatives show inhibiting activities against tumor cell lines and can be used as medicaments for treating malignant tumors.

Abstract: 4-O esters of podophyllotoxin and 4?-demethylepipodophyllotoxin are provided. The compounds are 4-O esters of an alkanoic acid or substituted alkanoic acid and podophyllotoxin and 4?-demethylepipodophyllotoxin. The compounds are useful for treating cancer.

Abstract: A method for the preparation of a compound of general Formula: or pharmaceutically acceptable derivatives and salts, racemates, isomers and/or tautomers thereof comprising cyclizing an azomethine ylide of general Formula: wherein, A is a cyclic or non-cyclic group; Z is a carbon or a heteroatom; n is selected from 0, 1, 2 or 3; W, X and Y may be the same or different and each are selected from hydrogen; optionally substituted alkyl, alkenyl, alkynyl, amino, alkoxy, alkenoxy, alkynoxy, aryl, alkylthio, heterocyclyl; carboxy, carboxy ester, carboxamido, acyl, acyloxy, mercapto, halogen, nitro, sulfate, phosphate, cyano and optionally protected hydroxy; or W and X, together with the nitrogen and carbon atoms to which they are attached, form a saturated or unsaturated nitrogen containing heterocyclic group which may be optionally substituted or optionally fused to a saturated or unsaturated carbocyclic group, aryl group or heterocyclic group is provided.

Abstract: The present invention relates to compositions and methods for preparing pharmaceutical compositions. In some embodiments, the invention includes compounds and methods of resolving chiral compounds. In some embodiments, the invention includes chiral and crystalline compositions and hydrates. In some embodiments, the invention contemplates compositions comprising camptothecin derivatives and synthetic intermediates thereof. In some embodiments, the invention includes methods of protecting, inserting, modifying, separating isomers, and removing chemical groups.

Abstract: Compounds and compositions useful in methods for treating cancer in mammals. The compounds of the invention are of the formula: or a pharmaceutically acceptable salt, entantiomer or disastereomer thereof, wherein the “A” ring is a nitrogen-aryl group; each occurrence of Y is independently oxygen or H2; Z is oxygen or —CH2—; X is nitrogen or —CH; R1, R2, R3, R4, R5, R6, and R7 are subsitutents; n is an integer from 1-7; m is an integer having a value of 1-5; and the dotted line represents an optional bond.

Abstract: New lamellarins are provided of the general formula III or a pharmaceutically acceptable salt, derivative, prodrug or stereoisomer thereof

Abstract: The present invention relates to novel vinorelbine derivatives. Pharmaceutical compositions containing these compounds as well as processes of preparation and processes of use for treatment of various conditions are also disclosed.

Abstract: The present invention relates to derivatives of vinca alkaloids. Pharmaceutical compositions containing these compounds as well as processes of preparation and treatment of various conditions are also disclosed.

Abstract: The invention relates to novel derivatives of 14,15-dihydro 20,21-dinoreburnamenin-14-ol, having formula (I) in which R represents a radical —AR? wherein A represents a heteroatom and R? represents a group selected from the group comprising linear or branched C1-C6 alkyl radicals, C2-C6 alkenyls, C2-C6 alkynyls, arylalkyls; esters comprising the formula —R1— CO—O—R2; amides comprising the formula —R3—CO—NZY, wherein Y and Z together can form a cycloalkyl radical or a heterocyclic radical, optionally substituted by one or more alkyl radicals; a radical selected from the group comprising alkyl radicals, alkenyls or alkynyls, substituted by at least one amine with formula —NZY; or one of the pharmaceutically-acceptable salts thereof, including the isomers, enantiomers and diastereoisomers thereof and mixtures thereof.

Abstract: A drug complex useful as a DDS compound, which is represented by the following formula: A-R—NH—Y—CH2—O—CO-Q, wherein A is a polymer as a drug carrier; R is a spacer, wherein the spacer is an amino acid or an oligopeptide comprising 2 to 8 amino acids; Y is phenylene group which may be substituted; and Q is a residue of a drug compound such as antineoplastic agents. The complex provides rapid and site-selective release of a drug compound such as antineoplastic or anti-inflammatory agents and surely exhibits expected efficacy.

Abstract: The key intermediate in any synthesis of Irinotecan is 7-ethyl-10-hydroxy-20(S)-camptothecin. A process for the efficient synthesis of this intermediate is demonstrated proceeding through readily available 20(S)-camptothecin. Various other tecan compounds may be made by use of corresponding 7-alkyl-10-hydroxy-20(S)-camptothecin intermediates.

Abstract: A drug delivery system compound comprising a carboxy(C1-4)alkyldextran polyalcohol modified with a saccharide compound and a residue of drug compound bound to the carboxy(C1-4)alkyldextran polyalcohol, and a method for measuring a drug delivery system compound in which a polymer carrier and a residue of drug compound are bound to each other by a spacer comprising 2 to 8 amino acids linked by peptide bond(s), which comprises treating the drug delivery system compound with a peptidase, and measuring the resulting hydrolysate.

Abstract: The present invention relates to pharmaceutically acceptable salts formed by the compounds of general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs and pharmaceutically acceptable compositions containing them. The present invention also relates to a process for the preparation of the above said pharmaceutically acceptable salts, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, and pharmaceutical compositions containing them.

Abstract: The present invention relates to an improved and economical process for the isolation of anticancer agent Camptothecin from the twigs and stem of Nothapodytes foetida using hot extraction 20(S) Camptothecin is an alkaloid, which contains a pentacyclic ring system that includes a pyrrolo [3,4-b] quinoline moiety (ring A, B and C), the pyridone ring D and a chiral centre at C-20 in ring E.

Abstract: A polymorphic form of 9-nitrocamptothecin is provided, the polymorph being characterizable as having an IR spectrum with an absorption centered between 3625 cm−1 and 3675 cm−1 and containing more than a trace of water.

Abstract: Problem: A large scale production of camptothecin, which is a starting compound of irinotecan hydrochloride and various camptothecin derivatives, at a low cost and with ease.

Abstract: Conjugates of transferrin, albumin and polyethylence glycol consisting of native or thiolated transferrin or albumin or of polyethylene glycol (MW between approximately 5,000 and 20,0000) with at least one HS—, HO— or H2N group and cytostatic compounds derived through maleinimide or N-hydroxysuccinimide ester compounds, such as doxorubicin, daunorubicin, epirubicin, idarubicin, mitoxandrone, chloroambucil, melphalan, 5-fluorouracyl, 5′-desoxy-5-fluorouridine, thioguanine, methotrexate, paclitaxel, docetaxel, topotecan, 9-aminocamptothecin, etoposide, teniposide, mitopodoside, vinblastine, vincristine, vindesine, vinorelbine or a compound of general formula A, B, C or D, where n=0-6, X=—NH2, —OH, —COOH, —O—CO—R—COR*, —NH—CO—R—COR*, where R is an aliphatic carbon chain with 1-6 carbon atoms or a substituted or unsubstituted phenylene group and R*H, phenyl, alkyl with 1-6 carbon atoms.

Abstract: Compound of formula (I): wherein: n is 0, 1 or 2, R1 represents (C3-C11)cycloalkyl or (C3-C11)cycloalkylalkyl, R2, R3, R4 and R5 are selected from hydrogen, halogen, alkyl, alkenyl, alkynyl, perhaloalkyl, cycloalkyl, cycloalkylalkyl, hydroxy, hydroxyalkyl, alkoxy, alkoxyalkyl, alkoxycarbonyl, acyloxy, carboxy, nitro, cyano, aminocarbonyl (optionally substituted), and the groups (CH2)p—NaRb and —O—C(O)—N—RaRb, with p, Ra and Rb being as defined in the description, or two adjacent groups R2, R3, R4 and R5 together form a group —O—(CH2)t—O, t being integer from 1 to 3, R60, R70n, R80 and R90 represent a hydrogen atom, a hydroxy group, an alkoxy group, or an O—(CO)—X or O—(CO)—NXW group as defined in the description, R61, R71n, R81, and R91 represent a hydrogen atom, alkyl, alkenyl or alkynyl, or taken in pairs together form a bond or an oxirane group, or two groups together form an oxo group.

Abstract: Camptothecin derivatives of camptothecin of formula (I) 1

Abstract: The invention features polymeric biomaterials formed by nucleophilic addition reactions to conjugated unsaturated groups. These biomaterials may be used for medical treatments.

Abstract: Cascade esters of camptothecin are described. Processes for making these compounds and for using them in cancer treatment are also described.

Abstract: Halo-alkyl esters of camptothecin are described. Processes for making these compounds and for using them in cancer treatment, are also described.

Abstract: A polymorphic form of 9-nitrocamptothecin is provided, the polymorph being characterizable as having an IR spectrum with an absorption centered between 3625 cm−1 and 3675 cm−1 and containing more than a trace of water.

Abstract: The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amenable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug compounds and methods for synthesizing these 1-acyl-alkyl derivatives.

Abstract: Amorphous forms of 9-nitrocamptothecin are provided by grinding or pulverizing different polymorphic forms of 9-nitrocamptothecin, and the polymorphic forms are characterizable as having an X-ray powder diffraction pattern with discernable diffraction lines at different °2&thgr; values for Cu K&agr; radiation having a wavelength of 1.5406 Angstrom.

Abstract: Disclosed are novel aromatic compounds of the formula(I) wherein G, E, W, Ar, X, Y and Z. The compounds are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.

Abstract: A process for preparing S type 2-substituted hydroxy-2-indolidinylbutyric ester compound [II]: 1

Abstract: Compound of formula (I): 1

Abstract: A compound has the formula 1

Abstract: A compound selected from the group consisting of all possible isomers or racemates of a compound of the formula wherein the various substituents are as defined in the specification and its non-toxic, pharmaceutically acceptable salts with acids or bases having anti-anoxic, anti-ischemic and neuronal protective anti-depressant activities.

Abstract: Compound of formula (I): wherein: n is 0, 1 or 2, R1, R2, R3, R4 and R5 are selected from hydrogen, halogen, alkyl, alkenyl, alkynyl, perhaloalkyl, cycloalkyl, cycloalkylalkyl, hydroxy, hydroxyalkyl, alkoxy, alkoxyalkyl, alkoxycarbonyl, acyloxy, carboxy, nitro, cyano, aminocarbonyl (optionally substituted), and the groups (CH2)p—NRaRb and —O—C(O)—N—RaRb, with p, Ra and Rb being as defined in the description, or two adjacent groups R2, R3, R4 and R5 together form a group —O—(CH2)t—O, t being an integer from 1 to 3, R60, R70n, R80 and R90 represent a hydrogen atom, a hydroxy group, an alkoxy group, or an O—(CO)—X or O—(CO)—NXW group as defined in the description, R61, R71n, R81 and R91 represent a hydrogen atom, alkyl, alkenyl or alkynyl, or taken in pairs together form a bond or an oxirane group, or two groups together form an oxo group.

Abstract: A compound of the formula 1

Abstract: Compound of formula (I): 1

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: Water soluble polymeric conjugates of camptothecin consist essentially of N-(2-hydroxypropyl)methacryloylamide units linked via a spacer group to a residue of a camptothecin such as irinotecan or its non-soluble metabolite, 7-ethyl-10-hydroxy-camptothecin. The conjugates possess enhance antitumor activity and decreased toxicity with respect to the free drug. A process for their preparation and the pharmaceutical compositions containing them are also described.

Abstract: A compound selected from the group consisting of all possible isomers or racemates of a compound of the formula 1

Abstract: Water soluble polymeric conjugates of camptothecin consist essentially of N-(2-hydroxypropyl)methacryloylamide units linked via a spacer group to a residue of a camptothecin such as irinotecan or its non-soluble metabolite, 7-ethyl-10-hydroxy amptothecin. The conjugates possess enhance antitumor activity and decreased toxicity with respect to the free drug. A process for their preparation and the pharmaceutical compositions containing them are also described.

Abstract: Conjugates of transferrin, albumin and polyethylence glycol consisting of native or thiolated transferrin or albumin or of polyethylene glycol (MW between approximately 5,000 and 20,0000) with at least one HS—, HO— or H2N group and cytostatic compounds derived through maleinimide or N-hydroxysuccinimide ester compounds, such as doxorubicin, daunorubicin, epirubicin, idarubicin, mitoxandrone, chloroambucil, melphalan, 5-fluorouracyl, 5′-desoxy-5-fluorouridine, thioguanine, methotrexate, paclitaxel, docetaxel, topotecan, 9-aminocamptothecin, etoposide, teniposide, mitopodoside, vinblastine, vincristine, vindesine, vinorelbine or a compound of general formula A, B, C or D, where n=0-6, X=—NH2, —OH, —COOH, —O—CO—R—COR*, —NH—CO—R—COR*, where R is an aliphatic carbon chain with 1-6 carbon atoms or a substituted or unsubstituted phenylene group and R* H, phenyl, alkyl with 1-6 carbon atoms.