Abstract: The present invention relates to a process for extracting an alkaloid. Particularly, the present invention relates to a process for extracting Rauwolscine from plant parts of Rauwolfia genus. Specifically, the present invention relates to a process for extracting Rauwolscine with an enhanced purity i.e. >95%.

Abstract: A method of treating cancer in a subject in need thereof comprises administering said subject reserpine, yohimbine, an analog thereof, or a pharmaceutically acceptable salt or prodrug thereof, in an amount effective to treat the cancer. Compounds and compositions useful for carrying out the method are also described.

Abstract: Embodiments of screening methods for determining test agents effective for modifying the appearance of pigmented skin are provided. The screening method may comprise the steps of contacting a cell, a cell culture, or bulk cells with the test agent, wherein the cell, the cell culture, or the bulk cells comprise ADR?1 receptors, and determining based on the binding interaction of the test agent with the ADR?1 receptors whether the test agent is an effective ADR?1 receptor antagonist suitable for modifying the appearance of pigmented skin, wherein a test agent is considered to be an effective ADR?1 receptor antagonist when it defines a half maximal inhibitory concentration of less than about 1000 ppm.

Abstract: Isolated and purified chemokine peptides, variants, and derivatives thereof, as well as chemokine peptide analogs, are provided.

Abstract: A method of treating cancer in a subject in need thereof comprises administering said subject reserpine, yohimbine, an analog thereof, or a pharmaceutically acceptable salt or prodrug thereof, in an amount effective to treat the cancer. Compounds and compositions useful for carrying out the method are also described.

Abstract: Yohimbine derivatives are disclosed having modification of the C-16 carboxyl group to include a sidechain and where the resulting derivative does not possess a second yohimbine pharmacophore (i.e., the compound is not a yohimbine dimer). The yohimbine derivatives of the present invention are preferably characterized by selective activity as ?2c-AR antagonists. Use of the compounds, or pharmaceutical composition containing them, for treating or preventing an ?2c adrenergic receptor mediated condition or disorder, and for antagonizing activity of an ?2c adrenergic receptor are also disclosed.

Abstract: Demethylation of 3?, 4?-dimethoxy or 3?, 4?, 5?-trimethoxy benzoic ester of a phenol is carried out in the presence of an excess of aluminum halide in an organic solvent to get 4?-Hydroxy, 3?-methoxy or 4? hydroxy, 3?, 5?-dimethoxy benzoic acid ester of a phenol. The reaction is also applicable to 3?, 4?, 5?-trimethoxy diaryl ketone and some natural products like reserpine.

Abstract: The present invention relates to yohimbine dimer compounds, pharmaceutical compositions containing such dimer compounds, methods of making such dimer compounds, and uses thereof. The yohimbine dimer compounds include compounds of formula (I): where R is any linker molecule which affords a yohimbine dimer that has activity as an &agr;2-AR antagonist and has selectivity for an &agr;2-AR subtype over another &agr;2-AR subtype.

Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof, wherein R1 is hydrogen, lower alkyl, COOR7, (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl, or (un)substituted heteroarylalkyl; R3 is hydrogen or lower alkyl; R2, R4, R5, and R6 independently represent hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy, cyano, nitro, amino, mono- or dialkylamino, carboxy, alkoxycarbonyl, carbamoyl, sulfamoyl, trifluoromethyl, or alkylthio; R7 is hydrogen or lower alkyl; and R8 is hydrogen or oxo. Also provided is a method for selectively antagonizing the M4 muscarinic receptor and a method for treating Parkinson's disease.

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: The invention relates to the preparation of pyrocarbonic acid diesters by an improved process and to the novel pyrocarbonic acid diesters prepared according to said process as well as to the use thereof. The core of the invention is a process for the preparation of a pyrocarbonic acid diester of formula (I) wherein R1 and R1′ are each independently of the other branched or straight-chain C1-C24alkyl, C3-C24alkenyl, C3-C24alkynyl, C4-C12cycloalkyl, C4-C12cycloalkenyl or C7-C24aralkyl, each of which is unsubstituted or substituted by one or more than one substituent which is inert under the reaction conditions, by reacting at least one ester carbonate of formula (II)  with 40-50 mol % of a sulfochloride of formula (IV)  in the presence of 0.

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: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.

Abstract: There is described a new process for the preparation of optically active 2-(2',2'-dihalogenovinyl)-cyclopropane-1-carboxylic acids substituted in the 3 position, and derivatives thereof. A racemate of certain cyclobutanones is reacted with a sulfurous acid salt of an optically active base to obtain a mixture of diastereomeric 4-(2',2',2'-trihalogenoethyl)-cyclobutane-2-sulfonic acid salts; this mixture is then separated into the pure diastereomeric sulfonic acid salts. Either the pure diastereomeric sulfonic acid salts are converted directly to the desired optically active products, or the optically active cyclobutanones obtained from the pure diastereomeric sulfonic acids salts by decomposition are converted, in the presence of a base, to the desired product. Optionally, the product, optically active 2-(2',2'-dihalogenovinyl)-cyclopropane-2-carboxylic acids can be converted to their 1',2'-dibromo derivatives.

Abstract: There is described a new process for the preparation of optically active 2-(2',2'-dihalogenovinyl)-cyclopropane-1-carboxylic acids substituted in the 3 position, and derivatives thereof. A racemate of certain cyclobutanones is reacted with a sulfurous acid salt of an optically active base to obtain a mixture of diastereomeric 4-2-(2',2',2'-trihalogenoethyl)-cyclobutane-1-sulfonic acid salts; this mixture is then separated into the pure diastereomeric sulfonic acid salts. Either the pure diastereomeric sulfonic acid salts are converted directly to the desired optically active products, or the optically active cyclobutanones obtained from the pure diastereomeric sulfonic acids salts by decomposition is converted, in the presence of a base to the desired product. Optionally, the product, optically active 2-(2',2'-dihalogenovinyl)-cyclopropane-1-carboxylic acids can be converted to their 1',2'-dibromo derivatives.

Abstract: Novel 3',4'-dehydro- and 4'-deoxo-vincristine and vinblastine compounds are obtained by coupling an indole unit of the catharanthine series and a dihydroindole unit of the vindoline series. Representative compounds of this series showed superior results when tested for activity against L1210 and P388 mouse leukemia.