Abstract: In one aspect, the present invention provides novel derivatives of trioxacarin analogs of the formula (I) wherein the variables are as defined herein. The application also provides compositions, methods of treatment, and methods of synthesis thereof.

Abstract: The present invention provides a method for the preparation of orally available pentacyclic taxane compounds, as well as intermediates useful in their preparation.

Abstract: Analogs of (?)-Picropodophyllin, synthesis thereof, and uses in pharmaceuticals as inhibitors of IGF1RK.

Abstract: Intermediates and methods of their use in the synthesis of analogs of halichondrin B are provided.

Abstract: The present invention relates to the use of new and known dithiine derivatives for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to new dithiine derivatives, to processes for preparing them, to their use, and to crop protection compositions comprising these new dithiine derivatives.

Abstract: The present invention relates to solid forms of 13-(N-Boc-?-isobutylserinyl)-14-?hydroxybaccatin III 1, 14-carbonate (Ortataxel). Amorphous Form A, crystalline Form B, mixtures thereof and processes for preparing them are disclosed. Amorphous Form A is prepared by fast precipitation of Ortataxel from a mixture of acetone and water. Form A transforms in Form B when suspended and stirred in a mixture of ethanol and water for 4-8 hours. If the suspension is stirred for less than 4 hours, mixtures of Form B and Form A are obtained. Form B or mixtures of Forms A and B can also be obtained dissolving Ortataxel in a protic organic solvent, followed by addition of water.

Abstract: The present invention provides a method for the preparation of orally available pentacyclic taxane compounds, as well as intermediates useful in their preparation.

Abstract: The present invention relates to methods for the synthesis of galanthamine, morphine, intermediates, salts and derivatives thereof. In preferred embodiments, the invention relates to methods for improving the efficiency and overall yield of said morphine, morphine related derivatives and intermediates thereof. In further embodiments, the invention relates to methods for improving the efficiency and overall yield of galanthamine and intermediates thereof.

Abstract: Provided is a polymerizable compound represented by the following general formula (ca-1) or (cb-1): wherein the variables in the formulae are defined in the specification.

Abstract: Provided is a polymerizable compound represented by the following general formula (ca-1) or (cb-1): wherein the variables in the formulae are defined in the specification.

Abstract: The invention relates to a method for synthesizing 4?-amino-4?-demethyl-4-desoxypodophyllotoxin of formula (1), characterized by comprising the following successive steps: a) reacting, in a pure weak acid or in a mixture consisting of acid, water and of organic solvent, without another solvent, at a temperature higher than the ambient temperature, thiourea with 4?-halogenoacetamido-4?-demethyl-4-desoxypodophyllotoxin, and; b) recovering the 4?-amino-4?-demethyl-4-desoxypodophyllotoxin.

Abstract: The present invention relates primarily to the novel compound of the formula (II) and certain mixtures comprising the compound of the formula (II) and use thereof as perfume. In addition the invention relates to perfume mixtures and perfumed products comprising a (preferably sensorially effective) amount of the compound of the formula (II) or a mixture according to the invention.

Abstract: The present invention provides a method for the preparation of orally available pentacyclic taxane compounds, as well as intermediates useful in their preparation.

Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.

Abstract: The invention relates to the use, or methods (especially with regard to animals, especially human, that are in need of such treatment) comprising the use, of an extract and/or one or more natural compounds from plants or parts of plants, respectively, from a genus selected from the group consisting of Schisandra, Illicium, Kadsura, Steganotaenia and Magnolia, alone or as supplement, as active ingredient in the regulation of body weight and/or fat loss and/or for the management of obesity, either in humans or in animals, to the use of said extract and/or natural compound(s) or mixtures in the manufacture of a pharmaceutical or nutraceutical formulation for the regulation of body weight and/or fat loss and/or for the management of obesity either in humans or in animals. The above extract and/or compound(s) can further be used to reduce one or more adverse metabolic parameters in a subject.

Abstract: There is disclosed use of certain picro derivatives of cyclolignans for prophylaxis or treatment of diseases or conditions characterised by a hyperactive immune system. Examples of cyclolignans according to the invention include picropodophyllin, deoxypicropodophyllin, anhydropicropodophyllol or deoxyanhydropicropodophyllol.

Abstract: The invention relates to a method for synthesizing 4.beta.-amino-4?-demethyl-4-desoxypodophyllotoxin of formula (1), characterized by comprising the following successive steps: a) reacting, in a pure weak acid or in a mixture consisting of acid, water and of organic solvent, without another solvent, at a temperature higher than the ambient temperature, thiourea with 4.beta.-halogenoacetamido-4?-demethyl-4-desoxypodophyllotoxin, and; b) recovering the 4.beta.-amino-4?-demethyl-4-desoxypodophyllotoxin.

Abstract: The present invention relates to novel podophyllotoxin derivatives substituted in the 4-position by a substituted (poly)aminoalkylaminoacetamide chain, to their process of preparation and to their use as medicament as anticancer agents.

Abstract: The present invention relates to synergistic combinations of the compound 5, 6-dimethylxanthenone-4-acetic acid (DMXAA) and a compound selected from anthracyclines and topisomerase II inhibitors, which have anti-tumor activity. Preferably, the present invention relates to synergistic combinations of the compound 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and a compound selected from etoposide, and doxorubicin. More particularly, the invention is concerned with the use of such combinations in the treatment of cancer and pharmaceutical compositions containing such combinations. The invention further provides for methods of preparing the combinations of the invention.

Abstract: The present invention relates to the use of vanilloid receptor (VR) antagonists, and more particularly vanilloid receptor 1 (VR1) antagonist, as analgesics in the treatment and/or prohylaxis of cnidaria envenomations.

Abstract: A sterile composition of a pharmaceutical compound is prepared by combining solvent with a non-sterile pharmaceutical compound to form a solution and filtering to yield a sterile pharmaceutical compound, optionally removing all or part of the solvent, and under sterile conditions combining the compound with a pharmaceutically acceptable carrier.

Abstract: Taxol derivatives or their salts having the formula as following: Wherein, R1, R2, Z1, Z2, Z3 and Z4 are defined as the description. Their preparation methods and their use as antitumor agent are also disclosed.

Abstract: The present invention relates to new amino acid derivatives, process for the production, their use, in particular in transplantation, and pharmaceutical compositions containing them.

Abstract: Compounds which inhibit the insulin-like growth factor-1 receptor (IGF-1 R) and methods for using them for treating IGF-1 R dependent diseases, such as cancer.

Abstract: Provided is a method for manufacturing fullerene 1,3-dioxolane conveniently at high yield. Fullerene 1,3-dioxolane is manufactured by reacting a fullerene oxide and a carbonyl compound in the presence of a catalyst.

Abstract: The present invention is to provide ATR inhibitor containing tricyclic compound including Schizandrins and Gomisins as an active constituent, useful for an inhibitor of ATR protein kinase.

Abstract: Novel tellurium-containing compounds and uses thereof as immunomodulators are disclosed.

Abstract: Compounds, compositions, methods of making, and methods of using analogues of (?)-picropodophyllin, as well as a transgenic animal model and its use for identifying anticancer agents.

Abstract: Mixtures are described which comprise or consist of 3-(4-methylcyclohex-3-enyl)butyraldehyde (limonenal) and (4aR,5R,7aS,9R)-octahydro-2,2,5,8,8,9a-hexamethyl-4H-4a,9-methanoazuleno(5,6-d)-1,3-dioxole (Ambrocenide®), the weight ratio of limonenal to Ambrocenide® being in the range from 150:1 to 2500:1.

Abstract: A process for the production of a substance or composition for the therapeutic or prophylactic treatment of erectile dysfunction or the enhancement of libido in a male human or animal subject comprises the step of formulating the substance or composition from at least one of plant material and an extract of plant material of at least one plant species of the family Geraniaceae.

Abstract: The invention relates to a method for synthesizing 4?-amino-4?-demethyl-4-desoxypodophyllotoxin of formula (1), characterized by comprising the following successive steps: a) reacting, in a pure weak acid or in a mixture consisting of acid, water and of organic solvent, without another solvent, at a temperature higher than the ambient temperature, thiourea with 4?-halogenoacetamido-4?-demethyl-4-desoxypodophyllotoxin, and; b) recovering the 4?-amino-4?-demethyl-4-desoxypodophyllotoxin.

Abstract: Chemically amplified resist compositions comprising amine compounds having a fluorinated alkyl group offer an excellent resolution and a precise pattern profile and are useful in microfabrication by KrF, ArF, F2, EUV, EB or X-ray lithography. They are also effective in the immersion lithography.

Abstract: Compounds of Formula I are described: preferably subject to the proviso that either (a) R2 and R3 together form —O—CH(R10)—O—, or (b) R5 and R6 together form —O—CH(R10)—O—, wherein R10 is H, halo, or loweralkyl. Pharmaceutical salts, formulations, and methods of using the same in the treatment of cancer are also described.

Abstract: A process to obtain synthetic and semi-synthetic derivatives of lignans, especially dibenzylbutyrolactonic, tetrahydrofuranic, aryltetralynic, furofuranic and dibenzocyclooctanic lignans obtained by means of partial synthesis and/or full synthesis or also by isolation from plant extracts. It refers to a process to obtain synthetic and semi-synthetic derivatives of (?)-cubebin, such as: (?)-O-acetylcubebin; (?)-O-methylcubebin; (?)-O—N,N-(dimethylamino-ethyl)-cubebin; (?)-hinokinin; (?)-6,6?-dinitroinokinine; (?)-O-benzylcubebin; (?)-6,6?-diaminoinokinin, (?)-6,6?-dinitroinokinin, as well as to obtain dibenzocyclooctanic lignans from dibenzylbutyrolactoinic lignans by means of structural modifications in the positions 7, 7?, 8, 8?, 9? and in the aromatic rings (introduction and/or substitution of functional groups such as: —OH, —CO2H, —CO2CH3, —NO2, —NH2, —OCH3, —OAc, —SO2CH3, —SO2NH2, prenyl and halogens) is provided. A therapeutic method using the derivatives is also provided.

Abstract: The present invention provides a method for the sterilization of a labile glucocorticosteroid, which method comprises heat-treating by moist heat the labile glucocorticosteroid in the form of a suspension for a sterilizing-effective time. The methods and compositions according to the invention are useful as therapeutic tools to prevent, reverse, and/or reduce the symptoms of allergic and/or inflammatory conditions in a mammalian patient. The invention also provides methods and compositions, which may be manipulated and fine-tuned to fit the condition(s) to be treated while producing fewer side effects.

Abstract: Provided is a method for manufacturing fullerene 1,3-dioxolane conveniently at high yield. Fullerene 1,3-dioxolane is manufactured by reacting a fullerene oxide and a carbonyl compound in the presence of a catalyst.

Abstract: Chemically amplified resist compositions comprising nitrogen-containing organic compounds having a 7-oxanorbornane-2-carboxylic ester structure have resolution and provide a precise pattern profile and are useful in microfabrication using electron beams or deep-UV light.

Abstract: A novel taxane derivative with anticancer activity, a process for its preparation and a process for the preparation of 14-?-hydroxy-1,14-carbonate-baccatine III and V derivatives 13-substituted by an isoserine residue.

Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein G1 is selected from the group consisting of a, b1 and b2, and A and G2 are as defined in the specification; or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

Abstract: The present invention relates to specific photochromic heterocyclically annellated indenochromene derivatives and the use thereof in plastics of all types, particularly for ophthalmic applications.

Abstract: Etoposide analogs such as 4?-O-demethyl-4?-[4?-(methyl-L-tyrosine-N-carbonyl)-anilino]-4-desoxy-podophyllotoxin (12) and 4?-O-demethyl-4?-[4?-(methyl-L-tryptophan-N-carbonyl)-anilino]-4-desoxypodophyllotoxin (13) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.

Abstract: The synthesis of taxol and other tricyclic and tetracyclic taxanes.

Abstract: The present invention relates to pharmaceutical and cosmetic compositions comprising at least one agonist ligand, which is specific for receptors of the RAR-&ggr; type, which are characterized as inducers of apoptosis in at least one cell population in which apoptosis can be induced by activating receptors of the RAR-&ggr; type. In one aspect of the present invention, there is provided a method of combating photoinduced or chronological ageing of skin, said method comprising administering an effective amount of at least one agonist ligand which is specific for receptors of the RAR-&ggr; type to combat photoinduced or chronological aging of skin, wherein the agonist ligand has a ratio R which is equal to or greater than 10.

Abstract: Etoposide analogs such as 4′-O-demethyl-4&bgr;-[4″-(methyl-L-tyrosine-N-carbonyl)-anilino]-4-desoxy-podophyllotoxin (12) and 4′-O-demethyl-4&bgr;-[4″-(methyl-L-tryptophan-N-carbonyl)-anilino]-4-desoxypodophyllotoxin (13) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.

Abstract: The present invention relates to specific photochromic heterocyclically annellated indenochromene derivatives and the use thereof in plastics of all types, particularly for ophthalmic applications.

Abstract: The present invention relates to the use of a dibenzocyclooctane lignan derivative of the following general formula (I) for treatment of neurodegenerative disorders: wherein R1 is H or C1-4 lower alkyl; R2, R3, R4 and R5 are respectively H, OH, C1-4 lower alkyl, C1-4 lower alkoxy, or R2 and R3 or R4 and R5 are respectively combined to form the group of —OCH2O—. Pharmaceutical preparations containing the dibenzocyclooctane lignan derivative as the active ingredient also are disclosed.

Abstract: Etoposide analogs such as 4′-O-demethyl-4&bgr;-[4″-(methyl-L-tyrosine-N-carbonyl)-anilino]-4-desoxy-podophyllotoxin (12) and 4′-O-demethyl-4&bgr;-[4″-(methyl-L-tryptophan-N-carbonyl)-anilino]-4-desoxypodophyllotoxin (13) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.

Abstract: New compounds of formula I are described: 1

Abstract: This invention provides compounds of the formula: 1

Abstract: A novel taxane derivative with anticancer activity, a process for its preparation and a process for the preparation of 14-?-hydroxy-1,14-carbonate-baccatine III and V derivatives 13-substituted by an isoserine residue.