摘要:
The present invention relates to novel amide compounds of formula I, and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of HDAC6 is responsive, and the pharmaceutical composition containing such compounds.
摘要:
The present invention relates to new retinoid derivatives of formula I and to pharmaceutical compositions containing them for the treatment of patients affected by pathologies such as arthritic conditions, tumours, metastatic cancer, diabetic retinopathy, psoriasis, chronic inflammatory diseases or atherosclerosis.
摘要:
The present invention relates to a compound of Formula (I), its geometrical isomers, in an optically active form as enantiomers, diastereomers, as well as in the form of racemate, as well as pharmaceutically acceptable salts thereof, wherein R is selected from CONHOH, CONHCH2SH, CONHCH2SCOCH3, SH, SCOCH3, SCH3, N(OH)COH, COCONHCH3 and CF3 for the preparation of a medicament, in particular for selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells, for inducing differentiation of tumor cells in a tumor, for inhibiting the activity of histone deacetylase and for the treatment of primary cancer or secondary cancer.
摘要:
A process for the epoxidation of 17-oxo-15,16-methylene steroids, in particular of drospirenone precursors, comprising the use of sulfoxonium ylides, in particular of dimethylsulfoxonium methyl ylide. The process allows to prepare in good yields 17-spiro epoxides, which can be easily transformed into 17-spironolacto-steroids.
摘要:
The present invention describes a method of preparation of formulations of microcrystalline lutein, particularly in the form of esters, which are resistant to oxidation and are soluble in hydrophilic and/or lipophilic media. For these formulations, the esters of lutein are mixed with antioxidants, vegetable oils and/or organic solvents, and this initial mixture is submitted to various stages depending on the type of final formulation required. These formulations are suitable for direct application as colourants in the pharmaceutical, food and cosmetics fields. They can also be used as diet supplements.
摘要:
The invention is directed towards a process for the preparation of Cefuroxime acid or for a corresponding pharmaceutically acceptable salt or ester. The process comprises the carbamoylation of a Cefuroxime precursor with an activated isocyanate. Additionally, the process is characterized by the fact that a carbonic C1-C4 alkyl ester is used as a solvent for the carbamoylation reaction.
摘要:
There is disclosed a process for the biotechnological resolution, by enzymatic esterification of the corresponding racemic mixture of the S(+) and R(-) optical isomers of the oxazolidinonic compounds having formula (I): ##STR1## wherein R represents a, linear or branched, C.sub.1 -C.sub.8 alkyl group, which process is characterized in that, the racemic 3-alkyl-5-hydroxymethyl-oxazolidin-2-one derivative of formula (I) is reacted with an esterifying compound, selected from esters having formula (III): ##STR2## wherein R represents a, linear or branched, C.sub.1 -C.sub.10 alkyl or alkenyl group and R" represents a linear or branched, C.sub.1 -C.sub.4 alkyl, alkenyl group, a haloalkyl (chlorine, bromine) group or a diacyl glycerolic group or from acids having formula (IV):R'"--COOH (IV)wherein R'" represents a, linear or branched, C.sub.1 -C.sub.20 alkyl or alkenyl group or from anhydrides having formula (V): ##STR3## wherein R.sup.IV represents a, linear or branched, C.sub.1 -C.sub.6 alkyl group, in the presence of an enzyme, immobilized on a porous carrier, capable of giving rise selectively to the esterification reaction of the R(-) isomer, while leaving the S(+) isomer substantially unchanged, which latter is then separated according to known techniques.
摘要:
The present invention provides a new process of synthesis of a polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline of Formula I. Said quinoline compound is substantially pure of any impurities. The present invention further provides the use of the above-mentioned polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline in the synthesis of piperaquine or one of its pharmaceutically acceptable salts.
摘要:
The present invention relates to new carbamate derivatives of formula I, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of neurological disorders, such as neuropathic pain and anxiety.
摘要:
This invention relates to a process for preparing a crystalline form of (4S)-11(dimethoxymethyl)-4-ethyl-4-hydroxy-1H-pyrano[3′4′:6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione, also named 7-(dimethoxy-methyl)camptothecin). With the provision of a particular crystallization step, in appropriate way, a new crystalline form of the above compound is obtained. The process for the preparation of the polymorph Form II comprises transforming camptothecin to the corresponding 7-(dimethoxy-methyl)-camptothecin, and crystallizing from methanol.