Abstract: A new process for the production of triiodotrimesic acid that is used as an intermediate product for the synthesis of x-ray contrast media is described.

Abstract: Ortho-substituted anthranilic acid amides and use thereof as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis are described.

Abstract: The method for testing of substances for hormonal effects, especially for androgenic or anti-androgenic effects, includes exposing cells transfected with two vectors to the substances, wherein one vector contains a DNA, which codes for a nuclear receptor protein, or a fragment thereof, especially a human nuclear receptor protein, or a fragment thereof, and the other vector contains a DNA, which codes for the HSRNAAM co-modulator, or a fragment thereof; and measuring transcription activity, which the nuclear receptor protein, or its fragment, activates or releases in the presence of the HSRNAAM co-modulator, or its fragment, and/or measuring the influence of the substance on the interaction between the nuclear receptor protein, or its fragment, and the HSRNAAM co-modulator, or its fragment, by protein-protein interaction or by protein-protein-DNA interaction. Also a method for determining interference in the co-modulation mechanism between androgen receptor protein and HSRNAAM co-modulator is described.

Abstract: Compounds of formula I wherein Z1, Z2, X, R2 and R3 are as defined herein, are suitable as NMR shift reagents.

Abstract: This invention relates to new antiestrogens of the general formula in which the substituents have the meanings that are explained in more detail in the description. The new compounds are a) pure antiestrogens or b) antiestrogens with partial estrogenic action (tissue-selective estrogens). Based on these properties, the new compounds are suitable for the production of pharmaceutical agents: in the case of a), for example, for the treatment of breast cancer; in the case of b), for example, for hormone replacement therapy.

Abstract: The invention relates to novel vitamin D derivatives of general formula (I), a method for the production thereof, intermediate products of the method and the utilization of vitamin D derivatives for producing medicaments.

Abstract: This invention describes a safe method for the production of sulfamoyl chloride from chlorosulfonyl isocyanate and formic acid in the presence of a amide catalyst, taming the hazardous nature of this reaction by circumventing heat accumulation processes, as well as the sulfamoylation of alcohols and phenols with the resulting sulfamoyl chloride in N,N-dimethyl acetamide or N-methyl pyrrolidone thereby avoiding the formation of side-products which were inevitable with the methods of the prior art using dimethyl formamide or dichloromethane as a solvent. The current invention allows industrial scale applications and describes as an example the process of manufacture of the biologically active compound 17?-Hydroxyestra-1,3,5(10)-triene-3-yl sulfamate.

Abstract: The invention relates to the use of biogenic estrogen sulfamates for the oral discontinuous application for hormone replacement therapy (HRT). The discontinuous administration takes place in intervals ranging from 2 to 40 days. The invention also provides the additional application of gestagens, preferably continuously in the form of an implant or in the form of an intrauterine releasing system (IUD). Estrone sulfamate, estradiol sulfamate or an N-acyl sulfamate of estrone, estradiol or estriol having up to 7 C-atoms in the acyl chain, or a combination comprised of two or more of said active ingredients are used as biogenic estrogen sulfamates.

Abstract: This invention relates to a process for the production of 4-(17?-alkoxymethyl-17?-substituted-3-oxoestra-4,9-dien-11?-yl)benzaldehyde-(1E)-oxime derivatives of general formula (I) in which R means an amino group, an O—C1-7-alkyl- or O-aryl radical, an S—C1-7-alkyl- or S-aryl radical, an NH—C1-7-alkyl- or NH-aryl radical or an N-di-C1-7-alkyl radical, and R1 means a hydrogen atom or a C1-6-alkyl radical, which yields the target compounds of formula (I) with high yield and selectivity.

Abstract: The invention relates to 3,5-dihydroxy-2,2-dimethyl-valeronitriles for the synthesis of epothilones and epothilone derivatives and process for the production of these new intermediate products in the synthesis and the use for the production of epothilones or epothilone derivatives.

Abstract: A formulation for male contraception comprising a progestin possessing both estrogenic and androgenic properties is remarkably effective for spermatogenesis suppression in males. The progestin Norethisterone (NET), particularly its derivatives Norethisterone acetate and Norethisterone enanthate in sufficient doses induce oligozoospermia or azoospermia in males. Formulations further comprising an androgen, such as a testosterone derivative such as a testosterone ester, particularly testosterone undecanoate, are especially effective male contraceptive formulations.

Abstract: The invention relates to 17?-alkyl-17?-oxy-estra-1,3,5(10)-trienes that have an antiestrogenic action with general formula I. In addition, the invention also relates to 17-oxo-estra-1,3,5(10)-trienes as well as 17?-hydroxy-estra-1,3,5(10)-trienes as intermediate products in the production of the estratrienes according to the invention. The invention also relates to the use of 17?-alkyl-17?-oxy-estratrienes for the production of pharmaceutical agents as well as pharmaceutical preparations that contain at least one 17?-alkyl-17?-oxy-estratriene as well as at least one pharmaceutically compatible vehicle.

Abstract: Substituted anthranilamides and use thereof as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis as well as their intermediate products for the production of anthranilamides are described.

Abstract: Disclosed are epothilone compounds of formula I, which are useful as pharmaceutical compounds for treating, for example, malignant tumors and chronic inflammatory diseases and are useful in anti-angiogenesis therapy.

Abstract: The present invention relates to a female mammal contraceptive process consisting of the sequential administration for at least 28 days of (a) a gestagen in an ovulation-preventing dose for at least 28 days in combination with (b) a natural oestrogen for 5 to 10 days at the end of the sequential dosage of at least 28 days, and a contraception kit.

Abstract: The method of isolating an anhydrous etidronate disodium particulate includes preparing a liquid-liquid dispersion consisting of an aqueous-organic phase and an etidronate-disodium-salt-containing aqueous phase; adjusting a temperature of the liquid-liquid dispersion to between 0 and 30° C. and intensely agitating so that a coarse-particle fraction precipitates from the liquid-liquid dispersion, then drawing off a fine-particle suspension and allowing a fine-particle fraction to precipitate from it and filtering and drying the coarse particle fraction. In a preferred embodiment the fine-particle fraction is separated from the fine-particle suspension for recycling The resulting anhydrous etidronate disodium particulate has a grain size of from about 0.1 to 1 mm and a bulk density of 0.4 to 0.6 g/cm2 with good properties for pharmaceutical applications.

Abstract: The invention relates to novel 18-norsteroids (gonatrienes) of general formula (I), wherein R1, R2, R3, R6, R7, R8, R9, R11, R11?, R14, R15, R15?, R16, R17 and R17? have the meaning cited in the description, and to the use of said compounds as pharmaceutical active ingredients. Said compounds exhibit a high affinity in vitro for estrogen receptor preparations of rat prostate and in an estrogen receptor preparation of rat uterus. Said compounds exhibit in vivo preferential activity on bones as compared to the uterus and/or significant activity with regard to stimulating the expression of 5HT2a-receptors and transporter molecules. The invention also relates to the production of said compounds, therapeutic use and galenic form of said compounds contained in the novel compounds of invention.

Abstract: Pharmaceutical compositions comprising low doses of sensitive complexes between an estrogen and a cyclodextrin are provided with improved stability. In specific embodiments the composition comprises a complex between ethinyl estradiol and ?-cyclodextrin in a granulate preparation and in yet another embodiment the composition comprises a limited amount of polyvinylpyrrolidone since this excipient was found to degrade ethinyl estradiol. Furthermore, a method for improving the stability of an estrogen in a composition and for manufacturing such a stable composition is provided. Essentially, the granulate preparation are manufactured under careful control of the relative humidity.

Abstract: 1,4,7,10-Tetraazacyclodedecane butyltriols of general formula IA in which R1 means hydrogen or a metal ion equivalent independent of one another and R2 means a butyltriol radical as well as their salts with organic or inorganic bases or amino acids are valuable pharmaceutical agents.

Abstract: The invention relates to the use of aromatics sulfonamides of the general formula I as peroxynitrite rearrangement catalysts, to the preparation thereof and to the use thereof as medicament for the treatment of various disorders.