首页> 外国专利> CYCLIC OCTAPEPTIDE, RADIOPHARMACEUTICAL AGENT BASED THEREON AND METHOD FOR USING A RADIOPHARMACEUTICAL AGENT TO PRODUCE MEDICINAL (PHARMACEUTICAL) AGENTS FOR THE TREATMENT OF NEOPLASMS WHICH EXPRESS SOMATOSTATIN RECEPTORS

CYCLIC OCTAPEPTIDE, RADIOPHARMACEUTICAL AGENT BASED THEREON AND METHOD FOR USING A RADIOPHARMACEUTICAL AGENT TO PRODUCE MEDICINAL (PHARMACEUTICAL) AGENTS FOR THE TREATMENT OF NEOPLASMS WHICH EXPRESS SOMATOSTATIN RECEPTORS

机译:循环肽,基于其的放射性药物和使用放射性药物产生药物(药物)药剂治疗表达生长抑素受体的神经胶质的方法

摘要

The invention refers to cyclic octapeptides being analogues of somatistatin, which can be applied for obtaining of various pharmaceutical means applied upon diagnostics or treatment, i.e. refers to the area of chemistry and medicine. Octapeptide meets the general claims (I):and it is intended for obtaining of radiopharmaceutical means with radionuclides 111In, 90Y, 177Lu.;Cyclic octapeptide contains terminal amino acid lysine (Lys) capable of covalent attachment of the chelating agent and thus having the following structure (Ia) and (Ib)X = chelating agent;Cyclic octapeptide of the general claims (I) is a biologically active molecule, and being a somatostatin analogue, cyclic octapeptide under invention is applied for obtaining of radiopharmaceutical means with radionuclides 111In, 90Y, 177Lu;The obtained radiopharmaceutical means can be applied for obtaining of the medical preparations and treatment of neoplasms (tumors) expressing somatistain receptors.;Long with that, compounds of the claim (I) with radionuclides 111In, 90Y, 177Lu are obtained with the use of the chelating agents. These octapeptides under the invention inhibit release of such hormones as growth hormone, lactogenic hormone, decrease secretion of insulin, glucagon, thrombotonin; can be applied for the treatment of acromegaly, diabetes, acute pancreatitis.;3 independent claims, 1 dependent claim, 2 tables, 6 examples, 1 figure.
机译:本发明涉及作为生长抑素类似物的环状八肽,其可用于获得用于诊断或治疗的各种药物手段,即涉及化学和医学领域。八肽符合一般要求(I): <图像文件=“ IMGA0001.GIF” he =“ 16” imgContent =“ chem” imgFormat =“ GIF” wi =“ 92” /> 其目的是用于获得具有放射性核素 111 In, 90 Y, 177 Lu的放射性药物。环八肽含有末端氨基酸赖氨酸( Lys)能够与螯合剂共价连接,因此具有以下结构(Ia)和(Ib) <图像文件=“ IMGA0002.GIF” he =“ 18” imgContent =“ chem” imgFormat =“ GIF” wi =“ 96” /> <化学id =“ chema03” > <图像文件=“ IMGA0003.GIF” he =“ 16” imgContent =“ chem” imgFormat =“ GIF” wi =“ 102” /> X =螯合剂;一般性权利要求(I)的环八肽是生物活性分子,并且作为生长抑素类似物,本发明的环八肽用于获得具有放射性核素 111 In,< Sup> 90 Y, 177 Lu;所获得的放射性药物可用于制备药物制剂和治疗表达生长抑素受体的肿瘤(肿瘤)。使用螯合剂获得具有放射性核素 111 In, 90 Y, 177 Lu的权利要求(I)。根据本发明的这些八肽抑制诸如生长激素,生乳激素的激素的释放,减少胰岛素,胰高血糖素,血栓素的分泌;等等。可用于肢端肥大症,糖尿病,急性胰腺炎的治疗。; 3个独立权利要求,1个从属权利要求,2个表格,6个示例,1个数字。

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