摘要:
The present invention is directed to novel pyrazolo-estrien and triazolo-estrien-derivatives, pharmaceutical compositions containing them and their use in the treatment or prevention of disorders and diseases mediated by an estrogen receptor such as hot flashes, vaginal dryness, osteopenia, osteoporosis, hyperlipidemia, loss of cognitive function, degenerative brain diseases, cardiovascular diseases, cerebrovascular diseases, hormone sensitive cancers and hyperplasia (in tissues including breast, endometrium, and cervix in women and prostate in men), endometriosis, uterine fibroids, osteoarthritis; and as contraceptive agents either alone or in combination with a progestogen or progestogen antagonist. The compounds of the invention are selective estrogen receptor modulators.
摘要:
A process for preparing α-functionalized thiazolidines or oxazolidines, each of which are oxycarbonyl-functionalized in the 4-position, by adding a base to a reaction mixture comprising an oxycarbonyl-functionalized thiazolidine or oxazolidine and an electrophile at a temperature of greater than −40° C.
摘要:
A process for preparing an &agr;-haloketone of the formula (1) where R1 is an optionally heteroatom-containing and optionally substituted hydrocarbon radical, R2 is a hydrogen, alkyl, aralkyl or aryl radical, and X is a halogen radical, by reacting a carboxylic acid derivative of the general formula (2) where L is a leaving group, with a mono- or dienolate of a silyl ester of the formula (3) where R3 and R4 are identical or different alkyl, aryl, alkenyl or aralkyl radicals; and hydrolyzing the reaction product immediately afterwards by adding acid and decarboxylating to (1). The product &agr;-haloketone may be reduced to the corresponding &agr;-haloalcohol.
摘要:
New chelating agents as well as their tricarbonyl complexes with technetium and rhenium and the use of these compounds in radiodiagnosis and radiotherapy are described. The new chelating agents are coupled to substances that accumulate in the diseased tissue.
摘要:
The invention relates to microparticle preparations made of biodegradable copolymers for use in treatment and diagnosis, especially ultrasonic diagnosis, as well as a process for their production.
摘要:
The invention relates to ultrasonic contrast agents comprising microparticles which comprise synthetic biodegradable polymers and a gas and/or a fluid with a boiling point below 60° C., processes for the preparation thereof and their use as diagnostic and therapeutic agents.
摘要:
The invention relates to radioactive stents, characterized in that the stent is coated on the surface with the radioactive isotope, as well as processes for their production.
摘要:
The invention relates to a process for therapeutic treatment of proliferative diseases, which is characterized in that first an administration catheter is placed on the site of the lesion, and a radioactive substance is administered topically via the catheter, then the catheter is again removed, and the radioactive substance remains on the site of the lesion.
摘要:
The invention relates to new microparticles containing active ingredients, which contain at least one gas or a gaseous phase in addition to the active ingredient(s), agents containing these particles (microparticulate systems), their use for ultrasound-controlled in vivo release of active ingredients, as well as a process for the production of particles and agents.
摘要:
The invention relates to ultrasonic contrast agents consisting of microparticles which consist of amyloses and synthetic biodegradable polymers and a gas and/or a fluid with a boiling point below 60° C., process for the preparation thereof and their use as diagnostic and therapeutic agents.