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Chimeric somatostatin analogues and dopamine, a Pharmaceutical formula using these analogues, for the preparation of a medicament

机译:嵌合生长抑素类似物和多巴胺,一种使用这些类似物的药物配方,用于制备药物

摘要

Dopamine synthesis in similar equation (1)X is H, CL, BR, I, F, -CN or C1-5 tar; R1 is H, tar, Alilo, C1-4 Alquenio, O-CN; R2 and R3 are H or not H, respectively, if R2 and R3 are not, there is a double connection between the carbon atoms to which they are connected; R4 is h or CH3; and es-o-,-C (O) -- yes.S- (CH2) s-C (O) --S (O) --S (O) 2--SC (O)..-OC (o)..-N (R5) - C (o) - o-n (R6) -; R5, R6, R7 and R8 are h, each of which is an independent C1-5 tar; R6 is h or C1-5 tar; m is 0 or 1; n is 0-10; L is - (CH) 2) P-C (o) -,When it's -S-S (O) --S (O) 2--O- o -N (R6) -I am a C (o) - (cr7r8) Q -,When it is - n (R6) -,-O-O-SI am... You areWhen it is - C (o)it is life.-OC (o)..-S- (CH2) s-C (O) - o -N (R5) -C (O) -P is 1-10; q is 2-4; s is 1-10; t is 1-10; Z is similar to somatostina or a group composed of - h-oh, alcoxyl (C1-6),Arilalcoxi, NH2, o-nr9r10, wherein R9 and R10 are independent h or C1-5 asphalt, or one of the pharmaceutically acceptable salts. 1. A compound of formula (2), wherein X is the tar of H, Cl, Br, I, F, - CN or C1-5; R1 is the tar of C1-4, h, alilo, alquenilo or CN; R2 and R3 are h or h respectively, or in the absence of R2 and R3, there is a double-layer link between the attached carbon atoms; R4 is h or CH3; R5 is a set of C1-5 tar, or a set of - (CH2) Rn (CH3) Q formulas; and is - or--C (O) -- yes.-SC (O)..-OC (o)..-N (R6) -C (O) --N (R7) - o -N (R8) - (CH2) s-C (O) -R6, R7, R8, R9 and R10 are h, each of which is an independent C1-5 tar; L is - (CH2) P-C (o) -.When it's -S-O- o -N (R7) -L es -C (O) - (CR9R10) q-C (O) -When it's - n (R7) -,-O-O-SI am... You areWhen it is - C (o)it is life.-OC (o)..-N (R8) - (CH2) s-C (O) - o -N (R6) -C (O) -M equals 0 or 1; n equals 2-10; R equals 1-8; Q equals 2-4; P equals 1-10; s equals 1-10; t equals 1-10; and Z is similar to somatostina or a group composed of - h-oh, alcoxi C1-6, arilalcoxilo, NH2, o-nr9r10 or one of the pharmaceutically acceptable salts, which maintain monomer and dopamine activity. An example is: 6-n-propil-8b-energetically methodical-d-phe-c (cys-tyr-d-trp-lys-abu-cys) - thr-nh2. It also describes the formulation and composition of a drug, as well as the use of these similar substances in the production of drugs for the treatment of lung cancer, blood cells, anorexia, hypothyroidism, hypertension, H.pylori diffusion, acrylonitrile, restenosis.Crohn's disease, systemic sclerosis, pseudocyst and internal and external pancreatic cyst, tumor, Nestle tumor, multiple insulin, gastric tumor, zoellinger Ellison syndrome, diarrhea, AIDS related diarrhea, chemotherapy-related diarrhea, sclerosis, irritable bowel syndrome, pancreatitis, Intestinal obstruction, gastrointestinal reflex, gastrointestinal reflex, gastrointestinal recession, gastric syndrome, gonorrhea, hyperthermia of thyroid, acute disease, diabetic neuropathy, Paget disease, polycystic ovarian disease, thyroid cancer, hepatoma, leukemia, meningitis, cancer caxia, static hypotension, Hypotension after prandiaPanic attack, adenoma GH secretion, acrylonitrile, adenoma TSH secretion, adenoma prolactina secretion, insulin deficiency, diabetes, insulin deficiency, syndrome X, vascular disease, proliferative retinopathy, dawn phenomenon, kidney disease, gastric secretion, Pelvic ulcer, intestinal fistula, pancreatitis, rapid vacuum syndrome, water diarrhea syndrome, pancreatitis, gastrointestinal hormone secreting tumor, angiopathy, arthritis, rejection of aloe vera, transplant blood vessel bleeding, hypertension, gastrointestinal bleeding, Obesity and drug overdose.
机译:在类似的等式(1)中,多巴胺的合成为H,CL,BR,I,F,-CN或C1-5焦油; R1是H,焦油,Alilo,C1-4 Alquenio,O-CN; R 2和R 3分别为H或不是H,如果R 2和R 3不为H,则它们所连接的碳原子之间存在双重连接。 R4为h或CH3;和es-o-,-C(O)-是。S-(CH2)sC(O)-S(O)-S(O)2--SC(O)..- OC(o) ..- N(R5)-C(o)-上(R6)-; R5,R6,R7和R8为h,各自为独立的C1-5焦油; R 6是h或C 1-5焦油; m为0或1; n为0-10; L是-(CH)2)PC(o)-,当它是-SS(O)-S(O)2--O- o -N(R6)-我是C(o)-(cr7r8) Q-,当它是-n(R6)-,-OO-SI am ...你是当它是-C(o)这就是生命。-OC(o)..- S-(CH2)sC(O )-o -N(R5)-C(O)-P为1-10; q是2-4; s是1-10; t是1-10; Z类似于生长抑素或由以下组成的组:-h-哦,羟甲氧基(C1-6),阿鲁西林,NH2,o-nr9r10,其中R9和R10是独立的h或C1-5沥青,或药学上可接受的盐之一。 1.式(2)的化合物,其中X是H,Cl,Br,I,F,-CN或C1-5的焦油; R1是C1-4,h,alilo,alquenilo或CN的焦油; R 2和R 3分别为h或h,或者在不存在R 2和R 3的情况下,连接的碳原子之间存在双层连接; R4为h或CH3; R5是一组C1-5焦油,或一组-(CH2)Rn(CH3)Q分子式;并且是-或-C(O)-是。-SC(O)..- OC(o)..- N(R6)-C(O)-N(R7)-o -N(R8 )-(CH 2)s C(O)-R 6,R 7,R 8,R 9和R 10为h,各自为独立的C 1-5焦油; L是-(CH2)PC(o)-。-SO- o -N(R7)-L es -C(O)-(CR9R10)qC(O)-它是-n(R7)-,- OO-SI是...你是当它-C(o)它就是生命。-OC(o)..- N(R8)-(CH2)sC(O)-o -N(R6)-C( O)-M等于0或1; n等于2-10; R等于1-8; Q等于2-4; P等于1-10; s等于1-10; t等于1-10; Z与生长激素类似,或由-h-oh,alcoxi C1-6,阿里洛昔洛,NH2,o-nr9r10或一种可药用的盐组成的组,它们保持单体和多巴胺的活性。一个例子是:6-n-propil-8b能量有序地d-phe-c(cys-tyr-d-trp-lys-abu-cys)-thr-nh2。它还描述了药物的配方和组成,以及这些类似物质在生产用于治疗肺癌,血细胞,厌食症,甲状腺功能减退,高血压,幽门螺杆菌扩散,丙烯腈,再狭窄的药物中的用途。克罗恩病,全身性硬化症,假性囊肿以及内部和外部胰腺囊肿,肿瘤,雀巢瘤,多种胰岛素,胃肿瘤,zoellinger Ellison综合征,腹泻,艾滋病相关的腹泻,化疗相关的腹泻,硬化症,肠易激综合征,胰腺炎,肠梗阻,胃肠道反射,胃肠道反射,胃肠道衰退,胃综合征,淋病,甲状腺热疗,急性疾病,糖尿病性神经病,佩吉特病,多囊卵巢疾病,甲状腺癌,肝癌,白血病,脑膜炎,癌症,慢性低血压,餐后低血压发作,腺瘤GH分泌,丙烯腈,腺瘤TSH分泌,泌乳腺腺瘤分泌n,胰岛素缺乏症,糖尿病,胰岛素缺乏症,X综合征,血管疾病,增殖性视网膜病,黎明现象,肾脏疾病,胃分泌物,盆腔溃疡,肠瘘,胰腺炎,快速真空综合征,水腹泻综合征,胰腺炎,胃肠激素分泌肿瘤,血管病,关节炎,芦荟排斥,移植血管出血,高血压,胃肠道出血,肥胖和药物过量。

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