Abstract: The invention provides compounds of formula I: wherein A, B, W, Y, Z, and R1 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: The present invention relates to the preparation of compounds which are capable of inducing cell death such as apoptotic cell death (apoptosis), and/or for reducing a cell proliferative disorder.

Abstract: The invention relates to the method of manufacturing of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]-carbonyloxycamptothecin by condensation of 7-ethyl-10-hydroxycamptothecin with 1-chlorocarbonyl-4-piperidinopiperidine hydrochloride in a polar aprotic solvent in the presence of 4-dimethylaminopyridine.

Abstract: The present application describes deuterium-enriched topotecan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: The present application describes deuterium-enriched irinotecan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: Formula (I) compounds are described: (I) where the groups are as defined in the description here below, the racemic mixtures, their individual enantiomers, their individual diastereoisomers, their mixtures, and their pharmaceutically acceptable salts. Said compounds are topoisomerase I inhibitors.

Abstract: A pharmaceutical composition comprising a camptothecin as active ingredient is herein described. In particular immediate-release therapeutic systems are described for the improved oral absorption of 7-[(E)-t-butyloxyminomethyl] camptothecin, comprising a matrix consisting of liquid amphiphilic substances or having a melting point lower than 60° C., in which the active principle is at least partially dissolved and/or dispersed and/or inglobated.

Abstract: It is intended to provide water-soluble derivative of camptothecins which are excellent in therapeutic effect and suitable for chemotherapy for cancer. Namely, a water-soluble high-molecular weight derivative of camptothencins being excellent in sustained-release which is obtained by ester-bonding a carboxylic acid group of a polyethylene glycol-polycarboxylic acid polymer to a phenolic hydroxyl group of phenolic camptothencins.

Abstract: Compositions comprising extracts or isolated or purified compounds from plants of the genus Corydalis provide prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Corydalis compounds and their derivatives of natural and synthetic origins lower total cholesterol, LDL-cholesterol, and triglycerides and increase hepatic LDL receptor expression and activate AMP-activated protein kinase. Specific stereoisomers of Corydalis compounds with lipid lowering activity include 14R-(+)-corypalmine, 14R,13S-(+)-corydaline, 14R-(+)-tetrahydropalmatin, (+)-corlumidin, d-(+)-bicuculline, and (+)-egenine.

Abstract: A compound represented by the following formula (1): [wherein R1 and R2 each independently represents hydroxy, provided that R1 and R2 may be bonded to each other to form methylenedioxy, etc.; X represents halogeno; and R3 represents a protective is subjected to a cyclization reaction with the aid of an organic silyl hydride and then aromatized with an oxidizing agent to produce a benzo [c] phenanthridine derivative represented by the following formula (2): [wherein R1, R2, and R3 have the same meanings as defined above].

Abstract: A method for preparing a novel crystalline polymorphic irinotecan hydrochloride which is excellent in the solubility in water and reduced in the content of impurities is provided. A method for preparing c-type crystals of irinotecan hydrochloride having diffraction peaks (2?) at 9.15°, 10.00°, 11.80°, 12.20°, 13.00° and 13.40° in the powder X-ray diffractometry characterized by mixing irinotecan with one or more solvents selected from the group consisting of acetone, acetonitrile and tetrahydrofuran, adding hydrochloric acid, and collecting the formed crystals.

Abstract: In order to efficiently supply CPT, which is a starting compound of irinotecan hydrochloride and a variety of camptothecin derivatives, by a practical total synthesis, the invention provides a means of efficiently preparing a tricyclic ketone that corresponds to a CDE ring moiety of a camptothecin (CPT) skeleton.

Abstract: A crystalline polymorph of 7-ethyl-10-hydroxycamptothecin exhibiting an X-ray diffraction pattern having peaks at 10.9±0.2, 13.2±0.2, 23.9±0.2, and 26.1±0.2 2-theta degree.

Abstract: A four arm-polyethylene glycol-7-ethyl-10-hydroxycamptothecin conjugate, such as, is disclosed. Methods of making the conjugates and methods of treating mammals using the same are also disclosed.

Abstract: Formula (I) compounds are described: (I) where the groups are as defined in the description here below, the racemic mixtures, their individual enantiomers, their individual diastereoisomers, their mixtures, and their pharmaceutically acceptable salts. Said compounds are topoisomerase I inhibitors.

Abstract: A process is provided for the preparation of camptothecin derivatives, such as irinotecan, in a one-pot operation.

Abstract: Novel crystalline forms of topotecan hydrochloride and processes of making the same are disclosed.

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: This invention relates to compositions comprising thalidomide and another anti-cancer drug which can be used in the treatment or prevention of cancer. Preferred anti-cancer drugs are topoisomerase inhibitors. A particular composition comprises thalidomide, or a pharmaceutically acceptable salt, solvate, or clathrate thereof, and irinotecan. The invention also relates to methods of treating or preventing cancer which comprise the administration of a thalidomide and another anti-cancer drug to a patient in need of such treatment or prevention. The invention further relates to methods of reducing or avoiding adverse side effects associated with the administration of chemotherapy or radiation therapy which comprise the administration of thalidomide to a patient in need of such reduction or avoidance.

Abstract: The present invention provides for novel crystalline forms of irinotecan hydrochloride and processes for their preparation, pharmaceutical compositions containing the novel forms and methods for treating metastatic carcinoma of the colon or rectum using same.

Abstract: Compositions and methods for treating cancer and other hyperproliferatice disease conditions with topoisomerase inhibitors and their prodrugs are disclosed.

Abstract: The invention provides a butyrylchinesterase variant, a method of converting a camptothecin derivative to a topoisomerase inhibitor by contacting the camptothecin derivative with a butyrylcholinesterase variant and a method of treating cancer by administering to an individual an effective amount a butyrylcholinesterase variant exhibiting increased capability to convert a camptothecin derivative to a topoisomerase inhibitor compared to butyrylcholinesterase.

Abstract: The invention relates to an improved process for the preparation of Irinotecan hydrochloride trihydrate of formula (4) of enhanced yield, purity by contacting 1-chlorocarbonyl-4-piperidinopiperidine hydrochloride with 7-ethyl-10-hydroxy-camptothecin [IRT-3 (synthetic)] to obtain crude Irinotecan which is subsequently purified by solvent treatment, obtaining purified irinotecan which is converted into irinotecan hydrochloride trihydrate and the invention also relates to a report of the compound 1-chlorocorbonyl-4-piperidinopiperidine hydrochloride of formula (1) and its process for preparation.

Abstract: The invention provides new processes for preparing polyglutamic acid-therapeutic agent conjugates for clinical development and pharmaceutical use, and polyglutamic acid-therapeutic agent conjugates prepared by these processes.

Abstract: The current invention is in the field of molecular biology/pharmacology and provides compounds which modulate the effects of GPR30 as well as the classical estrogen receptors alpha and beta (ER? and ER?). These compounds may function as agonists and/or antagonists of one or more of the disclosed estrogen receptors.

Abstract: The present invention is related to a process for the preparation of [1,4?]bipiperidinyl-1?-carbonyl chloride or its hydrochloride using methylene chloride as a solvent in the reaction of 4-piperidinopiperidine with phosgene and the removing the reaction solvent by using an additional distillation solvent to raise the distillation temperature.

Abstract: The present invention is directed to a novel method for the preparation of high purity irinotecan. This can be achieved by eliminating the excess of the other reagent, bipiperidinyl-1?-carbonyl chloride after it has reacted with 7-ethyl-10-hydroxy camptothecin and crystallizing the final product from a suitable solvent.

Abstract: An objective is to provide an organic thin film transistor material exhibiting an excellent property as a transistor together with reduced aging degradation, and also to provide an organic thin film transistor, a field-effect transistor, a switching element, an organic semiconductor material and an organic semiconductor film employing the organic thin film transistor material. Disclosed is an organic thin film transistor material possessing a compound represented by the following Formula (1). where A composed of a condensed ring formed with a 6 membered aromatic cycle or a 6 membered aromatic heterocycle represents C—R, N or P; at least one of As is N or P; R represents a hydrogen atom, a halogen atom or a substituent; and R may be bonded with other Rs with each other to form a ring.

Abstract: Selective phosphorylation of phenpanstatin (3a) with tetrabutylammonium dihydrogen phosphate and dicyclohexyl-carbodiimide in pyridine followed by cation exchange chromatographic procedures was found to provide an efficient mute to a new series (3b-3d) of promising 3,4-O-cyclic phosphate prodrugs designated phenpanstatin phosphates. Application of analogous reaction conditions to pancratistatin (1a) led to a mixture of monophosphate derivatives where sodium paancratistatin 4-O-phosphate (4a) was isolated and the structure confirmed by x-ray craxtallography. Modification of the reaction conditions allowed direct phosphorylation of pancratistatin followed by cation exchange chromatography to afford sodium pancratistatin 3,4-O-cyclic phosphate (5b) which was selected for preclinical development.

Abstract: An article comprising the compound of Formula (I) wherein X is hydrogen or a radical of Formula (II), R1 independently at each occurrence is a C1-C20 aliphatic radical, a C3-C10 cycloaliphatic radical, or a C3-C10 aromatic radical; R2, R3, R4 and R5 are independently at each occurrence a halogen, a nitro group, a cyano group, a hydroxy group, a C1-C20 aliphatic radical, a C3-C20 cycloaliphatic radical, or a C6-C20 aromatic radical; and “n”, “q”, and “p” are each independently integers having a value of 0 to 3, and “m” is an integer having a value of 0 to 4.

Abstract: Camptothecin derivatives of camptothecin of formula (I) wherein the groups R1, R2 and R3 are as defined in the description are disclosed. The compounds of formula (I) are endowed with antitumor activity and show a good therapeutic index. Processes for the preparation of the compounds of formula (I) and their use in the preparation of medicaments useful in the treatment of tumors, viral infections and antiplasmodium falciparum are also disclosed.

Abstract: Methods of preparing CPT-esters are described. The methods include using at least one acid in the esterification reactions or acylation reactions of camptothecins.

Abstract: A novel group of apomorphine derivatives are provided that are well suited as radioimaging agents upon incorporation of radionuclides. Through reaction of D ring sites, the less reactive sites of the apomorphine A ring is modified in ways previously unattainable.

Abstract: The invention provides compounds of the invention pharmaceutical compositions comprising a compound of the invention, processes for preparing compounds of the invention, intermediates useful for preparing compounds of the invention, and therapeutic methods for treating cancer and other topoisomerase mediated conditions.

Abstract: The synthesis and biological activity of benzoisoindoloisoquinolone compounds are described. The synthesis and biological activity of C-11-substituted indenoisoquinolones are also described. Indenoisoquinolones substituted at C-11 are prepared by McMurry reactions of 11-ketoindenoisoquinolones with aldehydes.

Abstract: Compounds of formula (I) or (II) are described: where the groups are as defined in the description here below, the racemic mixtures, their individual enantiomers, their individual diastereoisomers, their mixtures, and their pharmaceutically acceptable salts. Said compounds are topoisomerase I inhibitors.

Abstract: A compound of Formula (I) wherein X is hydrogen or a radical of Formula (II), R1 independently at each occurrence is a C1–C20 aliphatic radical, a C3–C10 cycloaliphatic radical, or a C3–C10 aromatic radical; R2, R3, R4 and R5 are independently at each occurrence a halogen, a nitro group, a cyano group, a hydroxy group, a C1–C20 aliphatic radical, a C3–C20 cycloaliphatic radical, or a C6–C20 aromatic radical; and “n”, “q”, and “p” are each independently integers having a value of 0 to 3, and “m” is an integer having a value of 0 to 4.

Abstract: Tocopherol-modified therapeutic drug compounds; emulsion, microemulsion, and micelle formulations that include the compounds; methods for making the compounds and formulations; methods for administering the compounds and formulations; and methods for treating conditions using the compounds and formulations.

Abstract: The present invention relates to the field of prodrugs of chemotherapeutic agents and method of use thereof.

Abstract: The invention provides compounds of formula I or formula II: wherein: the bond represented by --- is a single bond or a double bond, and R1–R5, 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 or II, processes for preparing compounds of formula I or II, intermediates useful for preparing compounds of formula I or II, and therapeutic methods for treating cancer and other topoisomerase related conditions using compounds of formula I or II.

Abstract: The present invention describes novel dyes, including coumarins, rhodamines, and rhodols that incorporate additional fused aromatic rings. The dyes of the invention absorb at a longer wavelength than structurally similar dyes that do not possess the fused aromatic rings. Many of the dyes of the invention are useful fluorescent dyes. The invention includes chemically reactive dyes, dye-conjugates, and the use of such dyes in staining samples and detecting ligands or other analytes.

Abstract: A molecular conjugate is provided having the formula: wherein R1 is a de-hydroxyl or de-amino moiety respectively of a hydroxyl-bearing or amino-bearing biologically active molecule or an analog or derivative thereof, and Z is —O— or —NH—, respectively, Y is a straight or branched alkyl having 1 to 20 carbons that may be optionally substituted with one or more phenyl, a cycloalkyl optionally substituted with one or more alkyl or phenyl, or an aromatic group optionally substituted with one or more alkyl groups, electron-withdrawing groups, or electron-donating groups; and R2 is —CH?CH(W), —CH(OH)CH(OH)W, or —C(O)H, where W can be H, a straight or branched alkyl having 1 to 20 carbons that may be optionally substituted with one or more phenyl, a cycloalkyl optionally substituted with one or more alkyl or phenyl, or an aromatic group optionally substituted with one or more alkyl groups, electron-withdrawing groups, or electron-donating groups.

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 compound selected from those of formula (I): wherein: W1 represents, together with carbon to which it is bonded, phenyl, pyridyl, Z represents a group of formula U—V as defined in the description, Q1 represents oxygen, NR2 as defined in the description, Q2 represents oxygen, NR?2 as defined in the description, X1, X2, X?1 and X?2 each represents hydrogen, hydroxy, alkoxy, mercapto or alkylthio, Y1, Y2, Y?1 and Y?2 each represents hydrogen, or X1 and Y1, X2 and Y2, X?1 and Y?1, X?2 and Y?2 with carbon carrying them, together form carbonyl or thiocarbonyl, R1 is as defined in the description, its isomers, and addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful in the treatment of cancer.

Abstract: Disclosed are 3,5-disubstituted-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, R2, A, B and D are defined herein. The present invention relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Abstract: Camptothecin derivatives of camptothecin of formula (I) exhibit antitumor activity and show a good therapeutic index and are used in the treatment of tumors, viral infections and antiplasmodium falciparum.

Abstract: Described are pharmaceutically acceptable salts of a compound of formula (I) its tautomeric forms, its stereoisomers or its polymorphs, which is obtained by treating the compound of formula (I) with an acid selected from the group consisting of hydrohalo acid selected from the group consisting of hydrochloric acid or hydrobromic acid, acetic acid; sulfuric acid, nitric acid, phosphoric acid, boric acid, perchloric acid, tartaric acid, maleic acid, citric acid, methanesulfonic acid, benzoic acid, ascorbic acid, salicylic acid and benzene sulfonic acid wherein R1 represents substituted (C1–C6) alkyl wherein the substituent(s) is selected from mono (C1–C6) alkylamino or di (C1–C6) alkylamino; R2 represents hydroxy; R3, R4 and R5 represent hydrogen; and R6 represents hydrogen, or substituted (C1–C6) alkyl, wherein the substituent(s) is selected from halogen, hydroxy or (C1–C6) alkoxy and methods for using these compounds.

Abstract: This invention relates to improved liposomal camptothecin compositions and methods of manufacturing and using such compositions for treating neoplasia and for inhibiting angiogenesis.

Abstract: The invention provides compounds of formula I: wherein A, B, W, Y, Z, and R1 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) esters of camptothecin analogs are provided. The compounds are (20S) esters of an oxyalkanoic acid and camptothecin, which is are optionally substituted at the 7, 9, 10, 11, and 12 positions of the camptothecin ring. The compounds are useful for treating cancer.