Abstract: The present invention relates to a new process for the synthesis of compounds of formula (I) (wherein the meaning of R is dimethylamino or acetyl group) using the compound of formula (II) (wherein the meaning of R is dimethylamino or 2-methyl-1,3-dioxolan-2-yl group) as starting material, as well as to the intermediate of the process.

Abstract: The present invention relates to a new stereoselective process for the synthesis of 17(?)-17-acetyl-17-hydroxy-estr-4-en-3-one of formula (I), as well as to the new intermediates of the process. The 17(?)-17-acetyl-17-hydroxy-estr-4-en-3-one (gestonorone) is an important intermediate in the synthesis of the active ingredients having progestogen activity—such as gestonorone capronate and nomegestroi acetate. Formulas (I), (II) and (III).

Abstract: The present invention relates to a new process for the synthesis of compounds of formula (I) (wherein the meaning of R is dimethylamino or acetyl group) using the compound of formula (II) (wherein the meaning of R is dimethylamino or 2-methyl-1,3-dioxolan-2-yl group) as starting material, as well as to the intermediate of the process.

Abstract: New methods for the refolding of recombinant granulocyte colony stimulating factor (G-CSF) from inclusion bodies are disclosed. The methods comprise two refolding steps. In particular, the methods comprise the solubilizing of G-CSF with a solubilizing agent, the oxidative refolding (first refolding step) of G-CSF in the presence of the solubilizing agent and an oxidizing agent, the efficient removal of the solubilizing agent, and a second refolding step to complete the folding of G-CSF in the absence of the solubilizing agent. Various methods are described for the efficient removal of the solubilizing agent from partially refolded G-CSF.

Abstract: New methods for the production of recombinant polypeptides from inclusion bodies are disclosed. Modulation of the cell culture conditions positively affects the yield of the recombinant polypeptide in active form. In one aspect, the methods comprise (a) cultivating a host cell at a first temperature, the host cell comprising a nucleic acid encoding a recombinant polypeptide, (b) lowering the cultivation temperature from the first temperature to a second temperature, and (c) cultivating the host cell at the second temperature.

Abstract: The present invention relates to a hormonal contraceptive including 21 to 25 hormone-containing daily units, which contain a combination of ethinyloestradiol in an amount of ?25 ?g and chlormadinone acetate in an amount of ?5 mg, and optionally 7 to 3 hormone-free daily units for oral administration to women.

Abstract: The present invention relates to novel crystalline Form II of 17?-acetoxy-21-methoxy-11?-[4-N,N-dimethylaminophenyl]-19-norpregna-4,9-diene-3,20-dione, (also known as CDB-4124), processes for the preparation thereof and pharmaceutical compositions comprising it. Form II can be crystallized from different medium such as esters of C1-C4 alcohols and carboxylic acids, ketones, cyclohexane, acetonitrile, dimethylformamide, dimethyl sulfoxide, water and any mixture thereof.

Abstract: Our invention relates to trans-(4-{4-[2-(4-amino-cyclohexyl)-ethyl]-piperazin-1-yl}-5,6-dichloro-pyrimidin-2-yl)-methylamine dihydrochloride monohydrate, the process for the synthesis of this compound, the new (4,5-dichloro-6-piperazin-1-yl-pyirimidin-2-yl)-methylamine monohydrochlorid used as starting material in this synthesis, as well as the industrial process for the synthesis of trans-N-(4- {2-[4-(5,6-dichloro-2-methyl-amino-pyirimidin-4-yl-)piperazin-1-yl]-ethly}cyclohexyl-propionamide starting from trans-(4-{4-[2-(4-amino-cyclohexyl)-ethyl]-piperazin-1-yl}-5,6-dichloro-pyrimidin-2-yl)-methylamine dihydrochloride monohydrate.

Abstract: The present invention relates to a hormonal contraceptive including at least 120 hormone-containing daily units, which contain 5 to 50 ?g of ethinyloestradiol and 1 to 5 mg of chlormadinone acetate, and optionally 7 to 3 hormone-free daily units for uninterrupted oral administration to women.

Abstract: The present invention relates to stable and bioavailable immediate release formulations comprising dopamine receptor ligands. Methods of treating various disorders by administering the formulations are also described.

Abstract: The present invention relates to stable and bioavailable immediate release formulations comprising dopamine receptor ligands. Methods of treating various disorders by administering the formulations are also described.

Abstract: New methods for the refolding of recombinant granulocyte colony stimulating factor (G-CSF) from inclusion bodies are disclosed. The methods comprise two refolding steps. In particular, the methods comprise the solubilising of G-CSF with a solubilising agent, the oxidative refolding (first refolding step) of G-CSF in the presence of the solubilising agent and an oxidizing agent, the efficient removal of the solubilising agent, and a second refolding step to complete the folding of G-CSF in the absence of the solubilising agent. Various methods are described for the efficient removal of the solubilising agent from partially refolded G-CSF.

Abstract: The present invention relates to the combination of memantine and baclofen active ingredients, and also to the method for achieving body weight loss and thereby treating obesity and related co-morbidities by co-administration of baclofen and memantine.

Abstract: The present invention relates to a medicament, the active ingredient combination of which consists of a retinoid selected from the group consisting of acitretin [9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethylnona-2,4,6,8-tetraenoic acid], etretinate [ethyl 9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethylnona-2,4,6,8-tetraenoate], isotretinoin [3,7-dimethyl-9-(2,6,6-trimethyl-1-cyclohexen-1-yl)-2,4,6,8-nonatetraenoic acid] and tretinoin [3,7-dimethyl-9-(2,6,6-trimethyl-1-cyclohexenyl)nona-2,4,6,8-tetraenoic acid] and of a hormone combination with contraceptive action of an oestrogen component and a gestagen component, and to a dosage form consisting of at least 28 daily units, of which the final 7-3 daily units contain only the retinoid as active ingredient and the other daily units also contain the hormone-containing active ingredient combination, and to the use thereof for treating acne, seborrhoea or psoriasis.

Abstract: The invention relates to a process for the preparation of trans 4-amino-cyclohexil ethyl acetate HCl wherein d) hydrogenating 4-nitrophenyl acetic acid in a protic solvent at a temperature between 40-50° C. in the presence of Pd/C under 0.1-0.6 bar overpressure, and e) further hydrogenating the 4-aminophenyl acetic acid obtained in situ in step a) at a temperature between 50-60° C. under 1-4 bar overpressures, then f) heating to reflux the 4-aminocyclohexil acetic acid obtained in step b) for 1-3 hours in hydrochloric ethanol, and if desired after removing the solvent acetonitrile was added to the residue obtained and distilled off.

Abstract: The present invention relates to new dopamine D3 and D2 ligands of formula (I): wherein R1, R2 and Q are as described herein, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates and/or polymorphs thereof. The invention also relates to processes for preparing the same, to compositions containing the same and to their use in the treatment and/or prevention of conditions which requires modulation of dopamine receptors.

Abstract: The present invention relates to metabolites of(thio)-carbamoyl cyclohexane derivatives, particularly, metabolites of trans-4-{2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing the same and to their use in the treatment and/or prevention of a conditions which requires modulation of dopamine receptors.

Abstract: A dosage form for hormonal contraception containing a given number of hormone-containing daily units and a given number of hormone-free daily units for daily, oral administration, where the hormone-containing daily units each contain at most the minimum effective daily amount of folic acid for women and the hormone-free daily units contain at least a multiple of this amount up to the maximum permissible amount of folic acid for women.

Abstract: The invention relates to novel trans N-{4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine dihydrochloride monohydrate and a process for the preparation of the trans N-{4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine dihydrochloride monohydrate, said process comprising the steps a) reacting trans 2-{1-[4-(N-tert-butoxycarbonyl)amino]-cyclohexyl}-acetic acid ester with sodium borohydride and aluminum trichloride to give trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethanol; b) reacting trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]cyclohexyl}-ethanol obtained with methanesulfonic acid chloride in the presence of an acid binding agent to give trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethyl methanesulfonate; c) reacting trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethyl methanesulfonate obtained with 2,3-dichlorophenyl-piperazine in the presence of an acid binding agent to give trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-carb

Abstract: The invention relates to a new process for the preparation of compounds of general formula (I) wherein R1 and R2 represent independently hydrogen or C1-6 alkyl with straight or branched chain optionally substituted with aryl group, or C2-7 alkenyl containing 1-3 double bonds, or monocyclic, bicyclic or tricyclic aryl optionally substituted with one or more C1-6 alkoxy, trifluoro-C1-6 alkoxy, C1-6-alkoxycarbonil, C1-6alkanoyl, aryl, C1-6 alkylthio, halogen or cyano, or optionally substituted monocyclic, bicyclic or tricyclic C3-14 cycloalkyl group, R1 and R2 together with the adjacent nitrogen form a saturated or unsaturated optionally substituted monocyclic or bicyclic heterocyclic ring which may contain further heteroatoms selected from oxygen, nitrogen, or sulphur atoms and hydrochloric acid alts and/or hydrates and/or solvates thereof, by dissolving or suspending trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine of formula (III) or a salt or a hydrate or a solvate thereof in a