Abstract: The present invention relates to compounds which are CCR-5 receptor antagonists of the general formula I: wherein R1, R2, R3, R4, Ra, Rb, Rc, Rd, X, m and n are as defined herein. The invention further comprises pharmaeceutical compositions comprising such compounds, as well as the use of such compounds to treat CCR-5 mediated disorders.

Abstract: Indolinone derivatives, such as compounds of the formula (I): wherein A, m, n, R1, R2, R3, R5 and R6 are described herein, are disclosed herein as being useful in treating mammal having disease-states alleviated by the inhibition of PDK-1 activity.

Abstract: Compounds of Formula I, wherein Y1, Y2, R1-R6, Q and Z are as defined herein, are vitamin D derivatives. These compounds are useful for, e.g., the treatment hyperprolifierative diseases of the skin, tumor diseases and precancerous stages, auto-immune diseases, rejection reactions in the case of autologous, allogenic or xenogenic transplants, AIDS, atopic skin conditions, secondary hyperparathyroidism, renal osteodystrophia, senile and postmenopausal osteoporosis, diabetes mellitus type II, degenerative diseases of the peripheral and central nervous system, hypercalcemias, granulomatous diseases, paraneoplastic hypercalcemias, hypercalcemias in hyperparathyroidism, hirsutism, ateriosclerosis, and/or inflammatory diseases.

Abstract: Described are compunds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10—(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is SO2; R1 is aryl; R2 is a bicyclic heteroaryl group comprising one ring nitrogen atom with the exception that R2 cannot represent 2-phthalimidyl; any of R3, R4, R5 and R6, independently of the other, is H or a substituent other than hydrogen; and R7 and R8, independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.

Abstract: Compounds of the following formula (I): where a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.

Abstract: This invention relates to new piperazine derivatives of general formula I, in which V, W, n, R, R?, i, j, Y and Z have the meaning that is indicated in the description. The compounds according to the invention are distinguished by a diazacycloalkane substituent. They have at their disposal a special action with respect to the action that destabilizes the androgen receptor and can be used, for example, for treating prostrate cancer.

Abstract: Compounds of the following formula (I): where a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.

Abstract: Compounds of the following formula (I): where a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.

Abstract: The invention relates to novel benzimidazole derivatives with general formula I, whereby radicals R1, R2, R3, A, B and Y have the meanings that are indicated in the description and the claims, the use of these compounds for the production of a pharmaceutical agent for treating and for preventing diseases that are associated with microglia activation, as well as pharmaceutical preparations that contain these compounds.

Abstract: The present invention relates to a series of compounds which are CCR-5 receptor antagonists of the general formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are defined herein.

Abstract: The present invention relates to antibodies, and antigen-binding antibody fragments, directed against an RG1 polypeptide. The invention further relates to methods for utilizing the antibodies, and antibody fragments, for diagnostic and therapeutic applications.

Abstract: The present invention is directed to a method for preventing or decreasing the incidence of or treating aneurysm or cardiac hypertrophy, comprising administering an effective amount of a rho-kinase inhibitor, such as fasudil, to a subject in need thereof.

Abstract: Preeclampsia and preterm labor in a pregnant female mammal are treated by administering thereto a combination of a progestin and a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in further combination with one or more of a cyclooxygenase inhibitor, a PGI2-mimetic, a thromboxane (TXA2) inhibitor, a compound possessing TXA2-agonistic and TXA2-inhibiting properties, a compound possessing TXA2-antagonistic and PGI2-memetic activities, and a TXA2 antagonist.

Abstract: The present invention relates to recombinant human interferon-?-1b (“IFN-?-1b”) polypeptides, or fragments, analogs, derivatives, or variants thereof, having an improved specific activity. The present invention also relates to pharmaceutical compositions comprising such IFN-?-1b polypeptides, or fragments, analogs, derivatives, or variants thereof, useful for treating multiple sclerosis. The present invention further relates to methods of producing such IFN-?-1b compositions.

Abstract: The invention relates to compounds of formula (I) and their tautomeric and isomeric forms and salts, as well as to a method for producing said compounds and their use in medicines.

Abstract: This invention relates to novel modified corin molecules, or fragments or derivatives thereof, comprising a substitute activation sequence. The modified corin molecules are cleaved at the substitute activation sequence, thereby generating activated corin molecules, or fragments or derivatives thereof, that exhibit the functional activity of naturally occurring, wild-type corin molecules. The modified corin molecules can be used to treat a variety of diseases or disorders, including congestive heart failure and acute myocardial infarction.

Abstract: The present invention provides for novel prodrugs of 1-(1-Hydroxy-5-isoquinolinesulfonyl)homopiperazine of the following Formula I 1

Abstract: The invention relates to a process for the production of peracylated 1-O-glycosides of general formula I or salts thereof in which sugar1 is a monosaccharide that is functionalized in 1-OH-position, R represents methyl, ethyl, propyl, isopropyl, tbutyl, phenyl, n means 2, 3 or 4, X means —COO— or —NH—and L means a straight-chain, branched, saturated or unsaturated C1-C30 carbon chain, which optionally is interrupted or substituted by groups. The process according to the invention starts from economical starting materials, provides good yields and allows the production of peracylated saccharides with 1-O-functionalized side chains on an enlarged scale.

Abstract: The invention relates to the human PEM polypeptide that plays an important role for the maturation of sperm and for Alzheimer's disease, and the nucleic acid that codes for them. The invention comprises the use of PEM as a target in male birth control and for the treatment and diagnosis of male infertility and Alzheimer's disease. The invention also includes a selection process for PEM antagonists as well as the production of binding molecules, which specifically detect PEM. In addition, genes that are regulated by the PEM gene are part of this invention.

Abstract: A process for the production of ergosterol and its intermediate products using recombinant yeasts and plasmids for transformation of yeasts is described.