摘要:
Substituted β-lactones (oxetanones) corresponding to the formula I, wherein R1, R2 and n have the meanings given in the specification, and pharmaceutical compositions which contain these compounds and have a pancreatic lipase-inhibiting action, as well as a process for the preparation of the compounds of Formula I and intermediate products of this process.
摘要:
The pharmaceutical use of proteases related to amino acids 1-274 of SEQ ID NO: 2, the serine protease derived from Bacillus licheniformis, which is also designated subtilisin Carlsberg, optionally in combination with a lipase 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.
摘要翻译:与SEQ ID NO:2的氨基酸1-274相关的蛋白酶的药物用途,来自地衣芽孢杆菌的丝氨酸蛋白酶,其也被指定为枯草杆菌蛋白酶卡尔斯伯格,任选与脂肪酶和/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。
摘要:
The invention relates to novel variants of a protease derived from Nocardiopsis sp. (SEQ ID NO: 1) and closely related proteases, as well as their pharmaceutical use. The variants show improved performance in the treatment of pancreatic exocrine insufficiency (PEI). The variants may be combined with a lipase and/or an amylase. Other examples of medical indications are: Treatment of digestive disorders, pancreatitis, cystic fibrosis, diabetes type I, and/or diabetes type II.
摘要翻译:本发明涉及来自诺卡氏菌属(Nocardiopsis sp。)的蛋白酶的新变体。 (SEQ ID NO:1)和紧密相关的蛋白酶,以及它们的药物用途。 这些变体在胰腺外分泌功能不全(PEI)的治疗中表现出改善的表现。 变体可以与脂肪酶和/或淀粉酶组合。 医学适应症的其他例子有:消化系统疾病,胰腺炎,囊性纤维化,I型糖尿病和/或II型糖尿病的治疗。
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 pharmaceutical use of lipases related to a variant of the Thermomyces lanuginosus (Humicola lanuginosa) lipase comprising amino acids 1-269 of SEQ ID NO: 1, 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 an improved efficacy in vivo, are stable against protease-degradation, and/or are stable in the presence of bile salts.
摘要翻译:与包含SEQ ID NO:1的氨基酸1-269的Thermomyces lanuginosus(Humicola lanuginosa)脂肪酶的变体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。 本发明的脂肪酶在体内具有改善的功效,对蛋白酶降解是稳定的,和/或在胆汁盐存在下是稳定的。
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 pharmaceutical use of proteases related to a protease derived from Nocardiopsis sp. NRRL 18262 (SEQ ID NO: 1), optionally in combination with a lipase 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.
摘要翻译:与来自诺卡氏菌属的蛋白酶有关的蛋白酶的药物用途 NRRL 18262(SEQ ID NO:1),任选与脂肪酶和/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。
摘要:
The pharmaceutical use of proteases related to amino acids 1-274 of SEQ ID NO: 2, the serine protease derived from Bacillus licheniformis, which is also designated subtilisin Carlsberg, optionally in combination with a lipase 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.
摘要翻译:与SEQ ID NO:2的氨基酸1-274相关的蛋白酶的药物用途,来自地衣芽孢杆菌的丝氨酸蛋白酶,其也被指定为枯草杆菌蛋白酶卡尔斯伯格,任选与脂肪酶和/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。
摘要:
The invention relates to novel variants of a protease derived from Nocardiopsis sp. (SEQ ID NO: 1) and closely related proteases, as well as their pharmaceutical use. The variants show improved performance in the treatment of pancreatic exocrine insufficiency (PEI). The variants may be combined with a lipase and/or an amylase. Other examples of medical indications are: Treatment of digestive disorders, pancreatitis, cystic fibrosis, diabetes type I, and/or diabetes type II.
摘要翻译:本发明涉及来自诺卡氏菌属(Nocardiopsis sp。)的蛋白酶的新变体。 (SEQ ID NO:1)和紧密相关的蛋白酶,以及它们的药物用途。 这些变体在胰腺外分泌功能不全(PEI)的治疗中表现出改善的表现。 变体可以与脂肪酶和/或淀粉酶组合。 医学适应症的其他例子有:消化系统疾病,胰腺炎,囊性纤维化,I型糖尿病和/或II型糖尿病的治疗。
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, and 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。 本发明的脂肪酶例如在体外具有改善的消化性能,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,并且对蛋白酶降解是稳定的,和/或在存在下是稳定的 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。