Abstract: The present invention relates to a diarylo[a,g]quinolizidine compound of formula (I), enantiomer, diastereoisomer, racemate, mixture, pharmaceutically acceptable salt, crystalline hydrate or solvate thereof; the preparation method thereof, and uses thereof in preparing an experimental model drugs related to dopamine receptors and 5-HT receptors or a medicament for treating or preventing a disease related to dopamine receptors and 5-HT receptors.

Abstract: A subclass of camptothecin derivatives is disclosed to be useful for the preparation of a medicament for the treatment of pediatric tumors such as for examplerhabdomyosarcoma, primitive neuroectodermal tumors (PNET) and neuroblastoma.

Abstract: An indolo[3,2,1-jk] carbazole derivative is represented by the following Formula 1. In Formula 1, X is a carbon atom or a nitrogen atom. At least one of X is a nitrogen atom. when X is a nitrogen atom, R is not present. When X is a carbon atom, R is hydrogen, an alkyl group, an alkoxy group, an aryl group, or a heteroaryl group. L is an electron acceptor, and m and n represent an integer of greater than or equal to 1.

Abstract: A semiconducting layer comprising a non-polymeric quinoid heteroacene compound of the formula (I) wherein X stands for O, S or NR, each of R, R1, R2, R3, R4, R5, R6, R7, R8 being independently selected from hydrogen and an organic residue, or 2 or more thereof together forming one or more annealed rings, which may be substituted or unsubstituted, carbocyclic or helerocyclic, aromatic, quinoid or aliphatic, may be used e.g. for the manufacture of a diode, an organic field effect transistor, an organic thin film transistor, or a device containing a diode and/or an organic field effect transistor and/or organic thin film transistor.

Abstract: The invention relates to a novel crystalline form of topotecan hydrochloride, and methods of making the same. The characteristic XRPD pattern and FT-IT patterns are shown in FIGS. 1 and 2.

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

Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.

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: (20) esters of camptothecin analogs are provided. The compounds are (20) esters of an aminoalkanoic acid or an imidoalkanoic acid and homocamptothecin, which is optionally substituted at the 7, 9, 10, 11, and 12 positions of the homocamptothecin ring. The compounds are useful for treating cancer.

Abstract: The present invention relates to a process for preparing 5-alkoxy-substituted oxazoles, in particular for preparing 4-methyl-5-alkoxy-substituted oxazoles and also a process for preparing pyridoxine derivatives.

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

Abstract: The present invention relates to yohimbine dimer compounds, pharmaceutical compositions containing such dimer compounds, methods of making such dimer compounds, and uses thereof.

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 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: 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: The instant invention is a series of compounds which are MCP-1 receptor antagonists of Formula I 1

Abstract: Heterocycle-condensed morphinoid derivatives of formula (I), or solvates or salts thereof, are potent and selective delta opioid agonists and antagonists and are useful as i.a. analgesics. Pharmaceutical compositions containing such compounds, the use of such compounds as therapeutic agents, a method of treatment comprising the administration of such compounds, and a process for the preparation of such compounds are also described.

Abstract: The present invention describes methods for preventing and treating sexual dysfunctions in patients by orally administering at least one &agr;-adrenergic receptor antagonist and at least one compound that elevates endogenous nitric oxide or endothelium-derived relaxing factor in vivo. The present invention also describes orally administrable compositions comprising at least one &agr;-adrenergic receptor antagonist and at least one compound that elevates endogenous nitric oxide or endothelium-derived relaxing factor in vivo. In the present invention, the &agr;-adrenergic receptor antagonist is preferably yohimbine or phentolamine, and the compound that elevates endogenous nitric oxide or endothelium-derived relaxing factor in vivo is preferably L-arginine.

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 novel phenanthridinium derivative represented by general formula (A): wherein R1 is a substituted or unsubstituted lower aliphatic hydrocarbon group; R is an aliphatic hydrocarbon chain having 2 to 6 carbon atoms which may optionally be substituted with a substituent selected from the group consisting of a lower alkyl group, a halogen and a hydroxy group; each of Y and Z independently represents a hydrogen, a hydroxy or a lower alkoxy group; or Y and Z are combined together to form methylenedioxy or a phenyl ring; and, X− is an acid residue or a hydrogen acid residue, exhibits an antitumor activity and has resistance to chemical reduction as well as biological metabolic reactions and is thus advantageous for use as a medicine.

Abstract: Process for the preparation of pigment preparations, which comprises wet milling the crude pigments which are present in coarsely crystalline state, or prepigments or pigments which are present in a form in which they are difficult to disperse, in a concentration of from 20 to 60% by weight based on the total weight of the pigment preparation, in a flocculation-stable liquid medium and in a stirred ball mill which is operated with a peripheral stirrer speed of more than 12 m/s, under the action of nonmetallic grinding media with a diameter of less than or equal to 1.0 mm, until the desired degree of fine division is reached, and then isolating the pigment preparation.

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: A method of preparing substantially purified alkaloids from seeds, stems, uit-rind and bark of a plant selected from Picralima nitida, Gongronema latifolia, Dorstenia multiradiata, Cola attiensis, Rothmania withfieldii and Desmodium gangeticum, for use in the treatment of protozoal diseases, comprising:pulverizing said plant;a first solvent, drying the extracted material and re-extracting the dried material with a different solvent;extracting a fresh sample of said plant with boiling water;filtering and concentrating the boiling water solvent extracts under reduced pressure;concentrating the dried extract to a gum and re-extracting said gum with an aqueous acidic HCl solution;filtering the acidic extract and making it alkaline to a pH of about 9 with a concentration NaOH solution;extracting the alkaline solution with dichloromethane;concentrating organic layers of the extracted alkaline solution to dryness under reduced pressure to obtain an alkaloid fraction; andseparating the alkaloid fraction by liquid chr

Abstract: A unique process for preparing certain (2R-trans)hexahydroaroquinolizines, especially (2R-trans)-N-[2-(1,3,4,6,7,12b-hexahydro-2'-oxospiro[aro-[2,3-a]-quinolizi ne-2,4'-imidazolidin]-3'-yl) ethyl)-methanesulfonamide from (2R-trans)-N-[2-[(2-cyano-(1,3,4,6,7,12b-hexahydro-aro-[2,3-a]quinolizin-2 -yl)amino]ethyl]methanesulfonamide is described.

Abstract: Compounds having the following general formula: ##STR1## wherein R is an alkyl or aminoalkyl group having 1 to 8 carbon atoms, or a hydrogen atom; R.sub.2 and R.sub.3 are either hydrogen atoms or, together, an additional carbon-carbon bond, as well as the mineral or organic acid addition salts thereof. These compounds are used as anti-arhythmic agents.

Abstract: Process for the stereoselective reduction of certain amino-substituted indoles and amino-substituted indole-containing structures to trans-dihydroindoles comprising the sequential steps of (1) reacting a strong acid addition salt of such an indole with a borohydride in an appropriate solvent in the absence of acid, and (2) acidifying the step (1) reaction product by which it is reduced and hydrolyzed to form the corresponding trans-dihydroindole. Many dihydroindoles so produced, for example, the trans-2-(adamantylemethyl)-=2,3,4,4a,5,9b-hexahydro-5-phenyl-1H-pyrido[4,3 -b]indole, are useful as pharmaceutical materials, such as tranquilizers.

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.