Abstract: The present invention relates to non-steroidal progestins of the general formula (I) wherein R1 and R2 are independently of each other —H or —F, R3 is —CH3 or —CF3, and Ar is or a pharmaceutically acceptable derivative or analogue thereof. These progestins are suitable for selectively modulating progesterone receptor mediated effects in different target tissues, particularly in uterine tissue versus breast tissue. Therefore, the progestins of the present invention, optionally in combination with estrogens, may be used for contraception (in particular in estrogen-free oral contraceptives), hormone replacement therapy and the treatment of gynecological disorders. The present invention furthermore relates to methods for selectively modulating progesterone receptor mediated effects in different target tissues or organs.

Abstract: The invention relates to new protected 3,5-dihydroxy-2,2-dimethyl-valeroarnides for the synthesis of edothilones and derivatives and process for the production and the use of the new compounds for the production of epothilones or epothilone derivatives.

Abstract: The invention relates to 11?-halogen steroids with general formula (I), whereby R11 is halogen, X—Y-Z represents a group with one of the two structures CH?C—C or CH2—C?C and the other radicals have the meaning that is indicated in the claims, also the production and use of these compounds for the production of pharmaceutical agents as well as pharmaceutical preparations that contain 11?-halogen steroids.

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: This invention relates to processes for the production of 3-oxo-pregnane-21,17-carbolactones of formula II as well as 3-oxo-pregn-4-ene-21,17-carbolactones of formula III by the metal-free oxidation of 17-(3-hydroxypropyl)-3,17-dihydroxyandrostanes of formula I In addition, the invention relates to the dichloromethane hemisolvate of 6B,7B;15?,16?-diethylene-3-oxo-17?-pregnan-5?-ol-21,17-carbolactone (IV) as such.

Abstract: Macrocyclic pyrimidine derivatives of general formula I in which R1 to R5, X, Y, A, B, m and n have the meanings that are contained in the description, as inhibitors of the cyclin-dependent kinase, their processes for production as well as their use as medications for treating various diseases are described.

Abstract: This invention relates to pyrimidine derivatives of general formula I in which R1, R2, X, A and B have the meanings that are contained in the description, as inhibitors of the cyclin-dependent kinases, their production as well as their use as medications for treating various diseases.

Abstract: A novel method of synthesis for the manufacture of upstream products for the production of compounds with general formulas 8, 10, and 12 is described. In this synthesis, compounds with general formula 4,B are produced in a microbiological reaction.

Abstract: The present invention provides compositions and methods that modulate MDL-1 activity in a cell, in vivo or in vitro. In particular, the present invention provides methods for treatment of inflammatory diseases using synthetic or recombinant compositions that modulate MDL-1 activity in a mammalian cell, in vivo or in vitro. More particularly, the present invention provides protein compositions useful for the treatment of diseases having an inflammatory process mediated by MDL-1.

Abstract: The novel glucocorticoid receptor antagonists are 11?-substituted steroid compounds of formula (I): wherein R1 denotes a methyl group, a methoxy group, or an ethoxy group; wherein R2 denotes a tert.-butyl group, a 1-hydroxy-1-methylethyl group, a 1-methoxy-1-methylethyl group, an ethyl isocrotonate group, or a substituted phenyl group. The method of treating an individual suffering from glucocorticoid-mediated hypogonadism, sexual dysfunctions, and/or infertility includes administering a daily dosage consisting of an effective amount of one of these 11?-substituted steroid compounds.

Abstract: This invention relates to novel fusion proteins which are comprised of a targeting protein that binds tissue factor (TF), which is operably linked to the thrombomodulin (TM) EGF456 domain alone or in combination with at least one other TM domain selected from the group consisting of the N-terminal hydrophobic region domain, the EGF123 domain, the interdomain loop between EGF3 and EGF4, and the O-glycosylated Ser/Thr-rich domain, or analogs, fragments, derivatives or variants thereof. The fusion protein binds at the site of injury and prevents the initiation of thrombosis. The fusion protein can be used to treat a variety of thrombotic conditions including but not limited to deep vein thrombosis, disseminated intravascular coagulation, and acute coronary syndrome.

Abstract: In the method of determining hormonal effects of substances, a test substance is contacted with Ewing sarcoma protein (EWS) or a derivative of it and with an androgen receptor (NR) or a derivative of it; and the effect of the test substance on binding of EWS with the androgen receptor or its derivative or on ligand-induced activity of the androgen receptor is determined, preferably in a cellular system. A method for determining interference in the co-modulator mechanism between androgen receptor and EWS, which includes measurement of androgen receptor and EWS concentrations, is described. A method for identification and characterization of substances that influence the activity of a nuclear receptor, especially androgen receptor, using EWS or a derivative of it is disclosed.