Abstract: Novel 1H-pyrrolo[2,3-b]pyridines which are represented by formula (I): wherein R is a hydrogen or halogen atom or a group selected from —CN, —OH, —OCOR4, —(CH2)nNH2, —(CH2)nNHR4, —(CH2)nNHCOR4, —(CH2)nNHCONR4R5, —(CH2)nNHCOOR4, or —(CH2)nNHSO2R4, wherein n is either 0 or 1, R4 and R5 are as described in the specification; R1 is hydrogen or an optionally substituted alkyl group; R2 is an optionally substituted group selected from alkyl or aryl; R3 is hydrogen or a group selected from —CONR4R5, —COOR4, —CONHOR4, —SO2NHR4, alkylsulphonylaminocarbonyl or perfluorinated alkylsulphonylaminocarbonyl; or a pharmaceutically acceptable salt thereof, are disclosed. These compounds are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.

Abstract: The present invention is drawn to a device for the transdermal administration of dextromethorphan, (+)-3-methoxy-17-methyl-9a,13a,14a-morphanin, and salts, prodrugs and metabolites thereof, together with a pharmaceutically acceptable carrier, to a human being or animal in need thereof, to achieve an antitussive effect. The present invention is further drawn to a method of achieving an antitussive effect in a human being or animal which comprises transdermally administering dextromethorphan, (+)-3-methoxy-17-methyl-9a,13a,14a-morphanin, and salts, prodrugs and metabolites thereof, together with a pharmaceutically acceptable carrier.

Abstract: This invention is therapeutically useful 2-aminotetralins and pharmaceutically acceptable acid addition salts thereof of the formula These compounds are useful to treat central nervous system disorders, hypertension, diabetes, sexual impotency and to control appetite.

Abstract: Nuclear magnetic resonance methods for identifying sites in a DNA-binding and dimerization domain of a papillomavirus E2 protein are disclosed. Preferably the sites are ligand binding sites.

Abstract: A crystalline form of mammalian TRAP (tartrate-resistant and purple acid phosphatase) is described. The enzyme is activated by cleavage prior to crystallization with a protease and the crystalline form of the mammalian TRAP is capable of being used for X-ray studies.

Abstract: The invention relates to polymeric conjugates of 20-O-[glycyl-aminoacyl-glycyl]-camptothecins and a process for producing the same.

Abstract: 4-phenyl-4-oxo-butanoic acid derivatives for use in the treatment of the human or animal body by therepy; particularly as kynurenine-3-hydroxylase inhibitors, in the prevention and/or treatment of a neurodegenerative disease wherein the inhibition of such an enyzme is needed. The present invention further comprises a selected class of the above mentioned 4-phenyl-4-oxo-butanoic acid derivatives, their pharmaceutically acceptable salts, a process for their preparation and pharmaceutical compositions containing them.

Abstract: A compound of formula (1) wherein R1 is hydrogen, hydroxy, a group of formula OR5 wherein R5 is C1-C6 alkyl, C2-C6 alkenyl or C3-C8 cycloalkyl, halogen, amino which may be unsubstituted or mono or disubstituted by C1-C6 alkyl, C2-C6 alkenyl, aralkyl, acyl or trifluoroacetyl; R2 is hydrogen, hydroxy, a group NR6R7 wherein R6 and R7 independently represent hydrogen, an optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C3-C8 cycloalkyl or, taken together with the nitrogen atom, represent an optionally substituted C3-C8 heterocyclic ring; R3 is hydrogen, hydroxy, R4 is a 2-substituted thiazolyl or imidazolyl system and the pharmaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.

Abstract: A process for preparing a compound of the formula I: or pharmaceutical acceptable salts thereof wherein X is —NR1—, —S(O)g—, or —O—; R1 is —H, C1-6 alkyl optionally substituted with one or more —OH, —CN, or halo, or R1 is —(CH2)h-aryl, —COR1-1, —COOR1-2, —CO—(CH2)h—COR1-1, C1-6 alkyl sulfonyl, —SO2—(CH2)h-aryl, or —(CO)i-Het; R2 is —H, C1-6 alkyl, —(CH2)h-aryl, or halo; R3 and R4 are the same or different and are —H or halo; R6 is —H, C1-12 alkyl optionally substituted with one or more halo, C3-12 cycloalkyl, C1-6 alkoxy. The compounds are useful antimicrobial agents.

Abstract: The present invention provides for 8-hydroxy-7-substituted quinoline compounds such as formula IA These compounds are useful as anti-viral agents. Specifically, these compounds have anti-viral activity against the herpes virus, cytomegalovirus (CMV). Many of these compounds are also active against other herpes viruses, such as the varicella zoster virus, the Epstein-Barr virus, the herpes simplex virus and the human herpes virus type 8 (HHV-8).

Abstract: The present invention includes processes to prepare commercially important taxols (X) from substituted amino-3-phenyl (2R,3S) isoserinates (II). In addition processes to prepare the substituted amino-3-phenyl (2R,3S) isoserinates (II) as well as its precursor are set forth.

Abstract: A novel recombinant procaspase 8 protein lacking the death effector domains and a method for converting said novel procaspase protein to full active human caspase 8 by concentration of the procaspase 8 on a collection device.

Abstract: A product containing: (a) an immunosuppressant agent (A) and (b) at least one immunosuppressant 2,2′-bi-1H-pyrrole compound (B) having formula (I) wherein R1 is hydrogen, phenyl, C1-C20 alkyl or C2-C20 alkenyl, wherein the alkyl and alkenyl groups are unsubstituted or substituted by 1 to 3 substituents, which are the same or different, chosen independently from halogen, C1-C6 alkoxy, hydroxy, aryl and aryloxy; R2 is hydrogen, C1-C6 alkyl, cyano, carboxy or (C1-C6 alkoxy)carbonyl; R3 is halogen, hydroxy or C1-C11 alkoxy unsubstitued or substituted by phenyl; R4 is hydrogen, C1-C6 alkyl or phenyl; each of R5 and R6, which are the same or different, is independently hydrogen, C2-C20 alkanoyl, C3-C20 alkenoyl, phenyl, C1-C20 alkyl or C2-C20 alkenyl; or two of R4, R5 and R6, taken together, form a C4-C12 polymethylene chain, which is unsubstituted or substituted by a C1-C12 alkyl, by a C2-C12 alkenyl or by a C1-C12 alkylidene group; or a pharmaceutically acceptable salt thereof; as a combined preparation for

Abstract: The present invention provides the enzyme and enzymatic procedures for cleaving the &bgr; secretase cleavage site of the APP protein and associated nucleic acids, peptides, vectors, cells and cell isolates and assays. The invention further provides a modified APP protein and associated nucleic acids, peptides, vectors, cells, and cell isolates, and assays that are particularly useful for identifying candidate therapeutics for treatment or prevention of Alzheimer's disease.

Abstract: Unique Mg-quinolone complexes are disclosed. They are relatively highly soluble, they may exist as a solution without a precipitate forming and without any need for additional acid or base additions to adjust pH, they may be administered as a subcutaneous or intramuscular injection with a low injection site irritation profile, and they are rapidly absorbed and taken up into the bloodstream.

Abstract: A pharmaceutical composition comprising a lipid complex or a liposome of a phospholipid and a water-insoluble platinum dicarboxylate and method for the preparation of such compositions are described.

Abstract: A process for producing a compound of formula (I): wherein the dotted lines - - - independently represent a single or double bond and R, R1, R2 and R3 are each hydrogen or an organic radical, comprises treating the corresponding 17&bgr;-carbonylimidazole intermediates with anhydrous acids in the presence of an amine and, optionally, hydrogenating the resulting compound.

Abstract: According to the invention there is provided a sterile, pyrogen-free, ready-to-use solution of an anthracycline glycoside, especially doxorubicin, which consists essentially of a physiologically acceptable salt of an anthracycline glycoside dissolved in a physiologically acceptable solvent therefor, which has not been reconstituted from a lyophilizate and which has a pH of from 2.5 to 6.5. The solution of the invention is particularly advantageous for the administration by injection of the anthracycline glycoside drugs, e.g. doxorubicin, in the treatment of both human and animal tumors.

Abstract: There are provided compounds of formula (I), wherein R1 is a hydrogen, chlorine or bromine atom or a methyl, methylthio, hydroxy, cyano or carboxamido group; R2 is C1-C3 alkyl or an alkyl group; R3 and R4 are independently a hydrogen atom, a C1-C5 alkyl group, a C3-C5 alkenyl group, a C5-C6 cycloalkyl C1-C3 alkyl group, a phenyl-C3-C5 alkenyl or phenyl group: which groups are optionally substituted by C1-C3 alkyl, C1-C3 alkoxy, triflouromethyl, hydroxy or amino group; or a group of formula (a), wherein R6 is hydrogen atom or a C1-C3 alkyl group and R7 is a phenyl group, a substituted phenyl group as described above or a heterocyclic ring, R5 is a hydrogen or bromine atom or an organic residue and R is H or an organic residue, or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmaceutical compositions comprising them are also provided.