摘要:
Substituted steroid compounds which represent selective inhibitors of 17β-hydroxysteroid dehydrogenase type I (17β-HSD1) and, in addition, which may represent inhibitors of the steroid sulfatase, salts thereof, pharmaceutical preparations containing these compounds, and a process for the preparation of these compounds. Also disclosed is a therapeutic method of using such substituted steroid compounds, particularly in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17β-hydroxysteroid dehydrogenase type I and/or steroid sulfatase enzymes and/or requiring lowering of the endogenous 17β-estradiol concentration.
摘要:
A method of treating or inhibiting non-digestive tract derived abdominal disorders associated with pain, in particular interstitial cystitis, chronic pelvic pain syndrome and/or abdominal pain associated with endometriosis, in a patient in need thereof, by administering to the patient a pharmaceutically effective amount of a 5-HT3 receptor antagonist, in particular cilansetron, or a pharmacologically compatible derivative thereof, such as a salt and/or a solvates.
摘要:
The pharmaceutical use of lipases related to the Thermomyces lanuginosus (Humicola lanuginosa) lipase comprising amino acids 1-269 of SEQ ID NO: 2, optionally in combination with a protease and/or an amylase. Examples of medical indications are: Treatment of digestive disorders, pancreatic exocrine insufficiency (PEI), pancreatitis, cystic fibrosis, diabetes type I, and/or diabetes type II. The lipases of the invention have, e.g., an improved digestion performance in vitro, an improved activity at a pH in the neutral range, an improved stability at low pH, an are stable against protease-degradation, and/or are stable in the presence of pepsin and bile salts. The invention also relates to methods of determining digestion performance in vitro of lipases, as well as to certain novel variants of the lipase of T. lanuginosus.
摘要翻译:与包含SEQ ID NO:2的氨基酸1-269的Thermomyces lanuginosus(Humicola lanuginosa)脂肪酶相关的脂肪酶的药物用途,任选地与蛋白酶和/或淀粉酶组合。 医学适应症的例子有:消化系统疾病,胰腺外分泌功能不全(PEI),胰腺炎,囊性纤维化,I型糖尿病和/或II型糖尿病的治疗。 本发明的脂肪酶具有例如体外改进的消化性能,在中性范围内的pH值改善的活性,在低pH下的改进的稳定性,对蛋白酶降解是稳定的,和/或在存在时是稳定的 的胃蛋白酶和胆汁盐。 本发明还涉及确定脂肪酶的体外消化性能的方法以及T.lanuginosus的脂肪酶的某些新颖变体。
摘要:
The use of compounds corresponding to formula I: in which R1, R2, R3, R4, R5 and R6 have the meanings given in the description for treating cardiac arrhythmias and other disease states.
摘要:
Substituted estratriene compounds of formula (I) useful in therapy, especially in the treatment or inhibition of a steroid hormone dependent disorder requiring the inhibition of a 17β-hydroxysteroid dehydrogenase (17β-HSD) type 1, type 2 and/or type 3 enzyme, as well as their salts, pharmaceutical compositions containing such compounds and processes for preparing such compounds.
摘要:
Compounds having neutral endopeptidase (NEP) and/or human soluble endopeptidase (hSEP) inhibitory activity corresponding to the formula I, wherein the substituents R1, R2, R3 and R4 have the meanings given in the description and also pharmaceutical compositions containing these compounds, in particular pharmaceutical compositions suitable for treating or inhibiting cardiovascular diseases, sexual dysfunction and/or adverse conditions associated with apoptosis.
摘要:
Treatment and/or inhibition of renal dysfunction, disease or disorder in larger mammals, and particularly in humans, especially in human patients suffering from diabetes, using benzazepine-N-acetic acid derivatives which contain an oxo-group in the α-position to the nitrogen atom and are substituted in position 3 by a 1-(carboxyalkyl)cyclopentylcarbonylamino radical, and/or salts or biolabile esters or physiologically acceptable solvates thereof, and production of pharmaceutical compositions and products suitable for treatment and/or inhibition of renal dysfunction, disease or disorder, particularly in diabetic patients, but also in patients with syndrome X or in patients with a renal dysfunction, disease and/or disorder, which patients are additionally hypertensive, obese, hyperglycemic and/or subject to a metabolic disorder.
摘要:
The invention relates to a group of hydronopol derivatives which are agonists on human ORL1 (nociceptin) receptors. The invention also relates to the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these novel hydronopol derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which ORL1 receptors are involved.The invention relates to compounds of the general formula (1) wherein the symbols have the meanings as given in the description.
摘要:
A method and apparatus for concentrating and stabilizing conjugated estrogens from pregnant mare urine on solid adsorbent supports to obtain a starting material for pharmaceuticals that contain a natural mixture of conjugated estrogen mixtures on cartridges in the vicinity of the horses. The adsorbent cartridges can be loaded at the site of urine collection so it is unnecessary to transport large volumes of urine to a central processing point. The loading process can take continuously over a period of weeks until the column is saturated. The effluent urine remains at the site where facilities for its disposal are available. Only the loaded cartridge is transported, and transport can occur at longer intervals of up to several weeks. The stability of the conjugated estrogens on the adsorber assures there is no risk of decomposition.
摘要:
A method and apparatus for concentrating and stabilizing conjugated estrogens from pregnant mare urine on solid adsorbent supports to obtain a starting material for pharmaceuticals that contain a natural mixture of conjugated estrogens as active ingredient. The apparatus is suitable for decentralized concentration and stabilization of conjugated estrogen mixtures on cartridges in the vicinity of the horses. The adsorber cartridges can be loaded at the site of urine collection so it is unnecessary to transport large volumes of urine to a central processing point. The loading process can take continuously over a period of weeks until the column is saturated. The effluent urine remains at the site where facilities for its disposal are available. Only the loaded cartridge is transported, and transport can occur at longer intervals of up to several weeks. The stability of the conjugated estrogens on the adsorber assures there is no risk of decomposition.