Abstract: This invention relates to a method for selectively preparing the 3-oxo-4-aza-5¥á-androstane compound which is used as an intermediate of finasteride by heating 3-oxo-4-aza-5-androstene in a mixture of formic acid and an alkanediol in the presence of zinc.

Abstract: This invention is related to heteroatom containing diamondoids (i.e., “heterodiamondoids”) which are compounds having a diamondoid nucleus in which one or more of the diamondoid nucleus carbons has been substitutionally replaced with a noncarbon atom. These heteroatom substituents impart desirable properties to the diamondoid. In addition, the heterodiamondoids are functionalized affording compounds carrying one or more functional groups covalently pendant therefrom. This invention is further related to polymerizable functionalized heterodiamondoids. In a preferred aspect of this invention the diamondoid nuclei are triamantane and higher diamondoid nuclei. In another preferred aspect, the heteroatoms are selected to give rise to diamondoid materials which can serve as n- and p-type materials in electronic devices can serve as optically active materials.

Abstract: A method for preparing a 1-androstene derivative which comprises reacting a 2-iodo-androstane derivative with an oxidizing agent while maintaining the pH of the reaction mixture at a specific range gives the 1-androstene derivative with high purity and yield.

Abstract: A crystalline Form II of 17?-N-[2,5-bis (trifluoromethyl)phenyl]carbamoyl-4-aza-5-?-androst-1-en-3-one (dutasteride) is provided. The preferred crystalline Form II of dutasteride has an X-ray powder diffraction pattern, expressed in terms of d-spacing (in ° A), with peaks at about 13.42, 6.96, 6.13, 5.27, 4.77, 4.70, 4.58, 4.46 and 3.82. A process for preparation of a crystalline Form II of dutasteride is also provided and includes dissolving a crude form of dutasteride in an alcoholic solvent having from 1 to 5 carbon atoms; removing the alcoholic solvent to obtain a residue; adding an ester solvent to the residue; and filtering the resulting separated solids. The processes of the invention are believed to be simple, eco-friendly, and commercially viable.

Abstract: New anthrapyridone compounds represented by the general formula (14): {wherein R represents a hydrogen atom, an alkyl group (optionally substituted with mono- or di-alkylamino group), a lower alkyl group (optionally substituted with a hydroxyl group or a cyano group), or a cyclohexyl group; Y represents a chlorine atom, a hydroxyl group, an amino group, mono- or di-alkylamino group (optionally substituted with a sulfonic acid group, a carboxy group, or a hydroxyl group), an aralkyl- or cycloalkyl-amino group, an alkoxy group, a phenoxy group (optionally substituted with a sulfonic acid group, a carboxy group, an acetylamino group, an amino group, or a hydroxyl group), an anilino group (optionally substituted with a sulfonic acid group or a carboxy group), or a naphthylamino group (optionally substituted with a sulfonic acid group); and X represents a bridging group}; or salts thereof and magenta inks containing the same, which have hues and vividness suitable for ink-jet recording and give records excelle

Abstract: A dye is disclosed, which is represented by the following formula: wherein Z is an atomic group necessary to form a 6-membered nitrogen containing aromatic ring; R11 is a hydrogen bonding group; R12, R13 and R14 are independently a hydrogen atom or a substituent; n11 and n13 are each an integer of 1 to 4; n12 is an integer of 1 to 3. There is also disclosed an ink for ink jet printing which contains the foregoing dye.

Abstract: The invention provides compounds of formula I: wherein: R1-R5, “a” and X 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 invention provides novel classes of Isoquinoline Derivatives. Pharmaceutical compositions and methods of making and using the compounds, are also described.

Abstract: A process for producing crystalline form I of cabergoline, which process comprises crystallization of the desired form from a toluene/diethyl ether mixture comprising raw cabergoline, followed by recovery and drying of the resulting crystals. A new solvate form V of cabergoline, useful as an intermediate, is also provided.

Abstract: (+)-Narciclasine (2), available in quantity from certain Amaryllidaceae species or by total synthesis, is employed in for a ten step synthetic conversion (3.6% overall yield) to natural (+)-pancratistatin (1a). The key procedures involve the epoxidation of natural (+)-narciclasine (2) to an epoxide (6), reduction of the epoxide (6) to diol (8), formation of cyclic sulfate (12) and its ring opening with cesium benzoate followed by saponification of the benzoate to afford (+)-pancratistatin (1a).

Abstract: A sulphamate compound suitable for use as an inhibitor of oestrone sulphatese (E.C.3.1.6.2) is described. The compound is a polycyclic compound comprising at least two ring components, wherein the polycyclic compound comprises at least one sulphamate group attached to at least one of the ring components, and wherein at least one of the ring components of the polycyclic structure is a heterocyclic ring.

Abstract: The invention provides organic compounds of the general structure (1) 1

Abstract: The 17&bgr;-(substituted)-3-oxo-&Dgr;1,2-4-azasteroids (I), wherein R1 is C1-C4 alkyl, OR2, wherein R2 is a C1-C4 alkyl radical, or NR3R4, wherein R3 and R4, equal or different, represent hydrogen or a C1-C4 alkyl radical, can be obtained by means of a process comprising cleaving the oxazolidinedione ring present in a 2-(substituted)-3-hydroxyoxazolidinedione of formula (IV), wherein R5 is Br or trichloromethylsulfonyl, and removing the substituent at position 2, to form a double bond at position 1,2. Some compounds (I) are testosterone-5&agr;-reductase inhibitors and can be used in the treatment of hyperandrogenic disorders.

Abstract: The invention provides novel classes of substituted Indeno[1,2-c]isoquinoline Compounds. Pharmaceutical compositions and methods of making and using the compounds, are also described.

Abstract: This invention relates generally to tetracyclic tetrahydroquinoline compounds, and analogues thereof, and pharmaceutically acceptable salt forms thereof, which are selective inhibitors of serine protease enzymes, especially factor VIIa; pharmaceutical compositions containing the same; and methods of using the same as anticoagulant agents for modulation of the coagulation cascade.

Abstract: The present invention pertains, at least in part, to novel 7-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

Abstract: The present invention pertains, at least in part, to novel 7-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

Abstract: The present invention pertains, at least in part, to novel 9- substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

Abstract: Compounds of formula 1 modulate the activity of Rho C: wherein R1 is H, OH, or lower alkyl; R2, R3, R4, R5, and R6 are each independently H, halo, lower alkyl, OH, lower alkoxy, NH2, lower alkylamino, di(lower alkyl)amino, SH, lower alkylthio, NO2, or two residues together form a heterocyclic ring; R7, R8, R9, and R10 are each independently H, lower alkyl, OH, NH2, aryl, or aralkyl, where aryl and aralkyl are substituted with 0-3 moieties selected from the group consisting of halo, OH, NH2, lower alkyl, lower alkoxy, SH, lower alkylthio, and lower alkylamino; R11, R12, R13, R14, R15, and R16 are each independently H, halo, lower alkyl, OH, lower alkoxy, or NO2; or a pharmaceutically acceptable salt thereof.

Abstract: An improved process for preparing steriods, such as 3-oxo-4-azasteroids, is described. Compounds of this type are known to be useful in the preparation of compounds having 5a-reductase inhibitor activity. The process comprises the hydrogenation of the corresponding steroid alkene in the presence of ammonium acetate, ammonium formate, and/or ammonium propionate and an appropriate catalyst.

Abstract: Substituted tetracycline compounds, methods of synthesis, and methods of use are discussed. Tetracyclines useful for treating tetracycline related disorders are also discussed. Intermediates useful for synthesizing other tetracycline compounds are also included.

Abstract: This invention relates to a metal complex of formula (I). The metal complex is capable of cleaving a bulge-containing nucleic acid at the bulge site with high specificity.

Abstract: The invention relates to a process for the production of compounds of general formula (I), wherein R1 is a —NH-tert-butyl group or a 4-methyl-piperidino group, by bioconversion of compounds of general formula (II), wherein R1 is as described above, using a biocatalyst having steroid-&Dgr;1-dehydrogenase enzyme activity, wherein the activity of the enzyme needed for the bioconversion is produced by induction.

Abstract: The invention provides compounds of formula I: 1

Abstract: The invention provides compounds of formula I: 1

Abstract: The invention relates to novel phenanthridine derivatives and to medicaments, which are for use in antitumoral therapy and prophylaxis and which contain these phenanthridine derivatives. It could be shown that up to now specifically substituted phenanthridine derivatives of the prior art neither have a known nor an antitumoral activity that is to be expected.

Abstract: A dye is disclosed, which is represented by the following formula: 1

Abstract: An androgenic steroid compound of the formula: 1

Abstract: A process for producing crystalline form I of cabergoline, which process comprises crystallization of the desired form from a toluene/diethyl ether mixture comprising raw cabergoline, followed by recovery and drying of the resulting crystals. A new solvate form V of cabergoline, useful as an intermediate, is also provided.

Abstract: A crystalline Form II of 17&bgr;-N-[2,5-bis (trifluoromethyl)phenyl]carbamoyl-4-aza-5-&agr;-androst-1-en-3-one (dutasteride) is provided. The preferred crystalline Form II of dutasteride has an X-ray powder diffraction pattern, expressed in terms of d-spacing (in ° A), with peaks at about 13.42, 6.96, 6.13, 5.27, 4.77, 4.70, 4.58, 4.46 and 3.82. A process for preparation of a crystalline Form II of dutasteride is also provided and includes dissolving a crude form of dutasteride in an alcoholic solvent having from 1 to 5 carbon atoms; removing the alcoholic solvent to obtain a residue; adding an ester solvent to the residue; and filtering the resulting separated solids. The processes of the invention are believed to be simple, eco-friendly, and commercially viable.

Abstract: The present invention relates to the preparation of the optical isomer (R)-(+)-8,9-dihydroxy-2,3,7,11b-tetrahydro-1H-napth[1,2,3-de]isoquinoline. This invention also relates to the use of pharmaceutical compositions comprising (R)-(+)-8,9-dihydroxy-2,3,7,11b-tetrahydro-1H-napth[1,2,3-de]isoquinoline for use for the treatment of movement disorders.

Abstract: An improved process for preparing steriods, such as 3-oxo-4-azasteroids, is described. Compounds of this type are known to be useful in the preparation of compounds having 5a-reductase inhibitor activity. The process comprises the hydrogenation of the corresponding steroid alkene in the presence of ammonium acetate, ammonium formate, and/or ammonium propionate and an appropriate catalyst.

Abstract: The invention provides novel classes of Isoquinoline Derivatives. Pharmaceutical compositions and methods of making and using the compounds, are also described.

Abstract: The invention relates to novel phenanthridine derivatives and to medicaments, which are for use in antitumoral therapy and prophylaxis and which contain these phenanthridine derivatives. It could be shown that up to now specifically substituted phenanthridine derivatives of the prior art neither have a known nor an antitumoral activity that is to be expected.

Abstract: The invention provides non-steroidal estrogenic compounds with estrogenic and anti-estrogenic compounds effects for treatment of estrogen-deficiency related disorders, which compounds are having formula (I) wherein, one of Ra or Rb is 'Re; Re and 'Re are OH, optionally independently etherified or esterified; X is N or —C(R1)—, wherein R1 is H1 halogen, CN, optionally substituted aryl, (1C-4C)alkyl, (2C-4C)alkenyl, (2C-4C)alkynyl or (3C-6C)cycloalkyl, which alkyl, alkenyl, alkynyl and cycloalkyl groups can optionally be substituted with one or more halogens; Y is N or —C(R2)—, with the proviso that X and Y are not both N, wherein R2 has the same meaning as defined for R1; Z is C(R3,'R3)— or —C(R4,∝R4)—C(R5,'R5)—, wherein R3, 'R3, R4, 'R4, R5, and 'R5, independently arc H, (1C-4C)alkyl, (2C-4C)alkenyl or (3C-6C) cycloalkyl, which alkyl, alkenyl and cycloalkyl groups can optionally be substituted with one or more halogens.

Abstract: Polymorphic Form (I) finasteride is prepared by first forming a substantially insoluble complex of finasteride and a Group (I) or Group (II) metal salt, such as lithium bromide, and then dissociating the complex by dissolving away the salt component with water, so as to obtain substantially pure Form (I) polymorphic crystalline finasteride.

Abstract: The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.

Abstract: The invention relates to compound of formula (I): wherein: G1 represents an alkylene chain as defined in the description, A represents R2 and R3 represent hydrogen, alkyl, alkoxy or hydroxy or together form oxo, R4 and R5 represent hydrogen, R1 is as defined in the description, and medicinal products containing the same which are useful in treating or preventing melatoninergic disorders.

Abstract: This invention relates generally to tetracyclic tetrahydroquinoline compounds, and analogues thereof, and pharmaceutically acceptable salt forms thereof, which are selective inhibitors of serine protease enzymes, especially factor VIIa; pharmaceutical compositions containing the same; and methods of using the same as anticoagulant agents for modulation of the coagulation cascade.

Abstract: A compound of the formula (I): wherein A is a hydrogen atom, an optionally substituted, unsaturated, N-containing heterocyclic group or a group of the formula (a): wherein R is an optionally substituted aryl group or an optionally substituted heterocyclic group; M is —(CH2)n-, —(CH2)n-O—(CH2)m-or —(CH2)n-NH—(CH2)m-, wherein n and m are independently 0, 1 or 2; Q is an optionally substituted cycloalkylene group, an optionally substituted arylene group or an optionally substituted divalent heterocyclic group; and the moiety of the formula (b): is an optionally substituted, unsaturated, mono-, di-, tri- or tetra-cyclic, N-containing heterocyclic group which may contain additional hetero atom(s) selected from the group consisting of nitrogen, oxygen and sulfur atoms as the ring member(s), its prodrug or a pharmaceutically acceptable salt thereof.

Abstract: The invention provides novel classes of substituted Indeno[1,2-c]isoquinoline Compounds. Pharmaceutical compositions and methods of making and using the compounds, are also described.

Abstract: Compounds of formula 1 modulate the activity of Rho C: 1

Abstract: The invention provides non-steroidal estrogenic compounds with estrogenic and anti-estrogenic compounds effects for treatment of estrogen-deficiency related disorders, which compounds are having formula (I) wherein, one of Ra or Rb is 'Re; Re and 'Re are OH, optionally independently etherified or esterified; X is N or —C(R1)—, wherein R1 is H, halogen, CN, optionally substituted aryl, (1C-4C)alkyl, (2C-4C)alkenyl, (2C-4C)alkynyl or (3C-6C)cycloalkyl, which alkyl, alkenyl, alkynyl and cycloalkyl groups can optionally be substituted with one or more halogens; Y is N or —C(R2)—, with the proviso that X and Y are not both N, wherein R2 has the same meaning as defined for R1; Z is C(R3,'R3)— or —C(R4,'R4)—C(R5,'R5)—, wherein R3, 'R3, R4, 'R4, R5, and 'R5, independently arc H, (1C-4C)alkyl, (2C-4C)alkenyl or (3C-6C) cycloalkyl, which alkyl, alkenyl and cycloalkyl groups can optionally be substituted with one or more halogens.

Abstract: The invention relates to compound of formula (I): wherein: represents a single or double bond, R0 represents hydrogen or hydroxy or alkoxy, R1 and R2, which are identical or different, each represents hydrogen or halogen or alkyl, alkoxy, hydroxy, polyhaloalkyl, nitro or optionally substituted amino or  wherein m represents an integer such that 1≦m≦4, or form together with the carbon atoms carrying them an aromatic or non-aromatic, mono- or bi-cyclic group having from 5 to 12 ring members and optionally containing 1 or 2 hetero atoms selected from O, S and N, R3 represents hydrogen or aryl, heteroaryl, cycloalkyl, optionally substituted alkyl or a group of formula COR7 wherein R7 represents aryl, optionally substituted alkyl, optionally substituted amino or OR10 wherein R10 represents aryl or optionally substituted alkyl, X represents oxygen or sulphur or —CH2— or —CH2—CH2—, Ar represents aryl, heteroaryl or arylalkyl, its op

Abstract: The present invention pertains, at least in part, to novel 7-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

Abstract: The present invention relates to an efficient process for the preparation of 5-(substituted)-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-chromeno[3,4-f]quinolines.

Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using compounds of the formula: or a pharmaceutically acceptable salt, hydrate, prodrug, or mixtures thereof, wherein Y is alkylhalo, alkyl-CO—G, COG, a direct bond, C═O, O, NR11, or CR8; G is NR11R16, OR9, SR9, or R10; Z is O, S, or NR11; X is NR16, O, S, CR12R13, C═O, a bond, —CR12═CR13—, —C(R12R13)C(R14R15)—, or; Rhd 1, R2, R3, R4, R5, R6, R7, R8, R10, R12, R13, R14, or R15 are independently: hydrogen, halo, alkylhalo, hydroxy, C1-C9 straight or branched chain alkyl, C2-C9 straight or branched chain alkenyl group, C3-C8 cycloalkyl, C5-C7 cycloalkenyl, aryl, amino, alkylamino, nitro, nitroso, carboxy, or aralkyl; R9 is hydrogen, hydroxy, C1-C9 straight or branched chain alkyl, C2-C9 straight or branched chain alkenyl group, C3-C8 cycloalkyl, C5-C7 cycloalkenyl, aryl, amino, alkylamino, carboxy, or aralkyl; R11 or R16 are independently: hydrogen, halo, alkylha

Abstract: A number of indenoisoquinolines were prepared and evaluated for cytotoxicity in human cancer cell cultures and for activity versus topoisomerase I. The two most cytotoxic indenoisoquinolines proved to be cis-6-ethyl-5,6,12,13-tetrahydro-2,3-dimethoxy-8,9(methylenedioxy)-5,11-dioxo-11H-indeno[1,2-c]isoquinoline and cis-6-allyl-5,6,12,13-tetrahydro-2,3-dimethoxy-8,9-(methylenedioxy)-5,11-dioxo-(11H)indeno[1,2-c]isoquinoline. Two of the most potent topoisomerase I inhibitors were 6-(3-carboxy-1-propyl)-5,6-dihydro-5,11-dioxo-11H-indeno[1,2-c]isoquinoline (26) and 6-ethyl-2,3-dimethoxy-8,9-(methylenedioxy)-11H-indeno[1,2-c]isoquinolinium chloride (27).

Abstract: 17&bgr;-(N-tert-butylcarbamoyl)-3-one-4-aza-steroids (I) can be obtained by a process which comprises the reaction of 17&bgr;-(alkoxycarbonyl)-3-one-4-aza-steroid with lithium tert-butylamide in an organic solvent. Some compounds of formula (I), for example, finasteride, are useful as inhibitors of 5&agr;-reductase, and can be used in the treatment of benign prostatic hyperplasia and alopecia.

Abstract: The present invention pertains to novel 7,9-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.