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1. 发明授权

US4603120A Cyclic octapeptides and pharmaceutical preparations thereof, as well as processes for their manufacture, and their use 失效
标题翻译：循环八肽及其药物制剂，以及其制备方法及其用途
公开(公告)号：US4603120A
公开(公告)日：1986-07-29
申请号：US451630
申请日：1982-12-20
申请人： Bruno Kamber
发明人： Bruno Kamber
IPC分类号： C07K7/64 , A61K38/00 , A61K38/04 , A61P5/00 , A61P7/04 , C07K1/113 , C07K14/575 , C07K14/655 , A61K37/24 , C07K7/26
CPC分类号： C07K14/6555 , A61K38/00 , Y10S930/16
摘要： Cyclic octapeptides of the formula ##STR1## in which Aaa represents a radical of a straight-chained .alpha.,.omega.-diaminoalkanoic acid having from 4 to 7 carbon atoms,trp represents a radical L-Trp or, especially, D-Trp, or a radical derived therefrom, which carries a halogen atom in the indole nucleus,Ac.sub.A represents an acyl radical Ac of an optionally substituted carboxylic acid which is positioned at the .omega.-amino group, or represents an amidino group or hydrogen, andAc.sub.B represents an acyl radical Ac.sup.1 of an amino acid or of an oligopeptide which is positioned at the .epsilon.-amino group, or, preferably, represents hydrogen,as well as physiologically tolerable salts and therapeutically acceptable complexes thereof can be used as antidiabetics and for the treatment of gastro-intestinal bleeding in an analogous manner to somatostatin. They can be obtained by conventional processes of peptide chemistry, especially by the cyclization of corresponding linear peptides.
摘要翻译：其中Aaa表示具有4至7个碳原子的直链α，ω-二氨基链烷酸基团的式（I）的环状八肽，trp表示基团L-Trp或特别是D-Trp 或衍生自其的衍生物，其在吲哚核中携带卤素原子，AcA表示位于ω-氨基上的任选取代的羧酸的酰基Ac，或表示脒基或氢，并且AcB表示位于ε-氨基，或优选代表氢的氨基酸或寡肽的酰基Ac1以及生理上可耐受的盐和其可治疗可接受的复合物可用作抗糖尿病药物和治疗胃肠道出血以类似于生长抑素的方式出血。它们可以通过肽化学的常规方法获得，特别是通过相应的线性肽的环化获得。

2. 发明授权

US4612366A Cyclic hexapeptide somatostatin analogs 失效
标题翻译：循环六肽生长抑素类似物
公开(公告)号：US4612366A
公开(公告)日：1986-09-16
申请号：US745459
申请日：1985-06-17
申请人： Ruth F. Nutt
发明人： Ruth F. Nutt
IPC分类号： C07K7/64 , A61K38/00 , A61K38/22 , A61P5/00 , C07K1/113 , C07K14/575 , C07K14/655 , C07K7/26 , A61K37/24
CPC分类号： C07K14/6555 , A61K38/00 , Y10S514/806 , Y10S930/16
摘要： Somatostatin analogs are prepared wherein a cyclic hexapeptide contains a secondary amino acid which replaces seven of the ring amino acids of somatostatin. The cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These cyclic hexapeptides are prepared by the solid phase method and/or solution synthesis.
摘要翻译：制备生长抑素类似物，其中环状六肽含有替代生长抑素的七个环氨基酸的仲氨基酸。环状六肽更容易合成，具有较长的活性持续时间，并且许多具有比生长抑素更高的活性水平。该化合物具有抑制胰高血糖素，生长激素和胰岛素释放的性质。某些化合物还能够抑制胃酸分泌物的释放。该化合物特别可用于治疗肢端肥大症，糖尿病，糖尿病性视网膜病变和消化性溃疡。这些环状六肽通过固相法和/或溶液合成制备。

3. 发明授权

US4585755A Cyclic and bridged cyclic somatostatin analogs useful as local anti-inflammatory agents 失效
标题翻译：循环和桥接的环状生长抑素类似物可用作局部抗炎剂
公开(公告)号：US4585755A
公开(公告)日：1986-04-29
申请号：US728019
申请日：1985-04-29
申请人： Evan R. Morgan , Sanford L. Steelman
发明人： Evan R. Morgan , Sanford L. Steelman
IPC分类号： A61K38/04 , A61K38/22 , A61K38/31 , A61P5/00 , A61P5/02 , A61K37/43 , C07K7/26
CPC分类号： A61K38/31 , Y10S514/806 , Y10S930/16
摘要： Cyclic and bridged cyclic somatostatin analogs have been found to be useful as local anti-inflammatory agents in the treatment of such conditions, as, for example, psoriasis, eczema, seborrhea, and other localized inflammatory and allergic conditions.
摘要翻译：已经发现循环和桥接的环状生长抑素类似物可用作治疗诸如牛皮癣，湿疹，皮脂溢和其它局部炎症和变态反应的条件的局部抗炎剂。

4. 发明授权

US4728638A Somatostatine derivatives 失效
标题翻译：生长激素衍生物
公开(公告)号：US4728638A
公开(公告)日：1988-03-01
申请号：US816663
申请日：1986-01-07
申请人： Wilfried Bauer , Janos Pless , Rene Huguenin
发明人： Wilfried Bauer , Janos Pless , Rene Huguenin
IPC分类号： A61K38/00 , C07K14/655 , A61K37/24 , C07K7/26
CPC分类号： C07K14/6555 , A61K38/00 , Y10S514/806 , Y10S930/16
摘要： Somatostatine derivatives of the general formula ##STR1## wherein either (a)A is ##STR2## W is -CO-N(A.sub.4) or -N(A.sub.5)-CO- and Y.sub.1 and Y.sub.2 are H or together a bondor (b)A is H, alkyl, phenylalkyl or RCO andY.sub.1 and Y.sub.2 are acyl groups as defined in claim 1,A', B, C, D, E, F, A.sub.1, A.sub.2, A.sub.3, A.sub.4, A.sub.5, R and Z having the meanings recited in claim 1, have pharmacological, in particular GH-, gastric- and pancreatic secretion inhibiting activity.
摘要翻译：其中（a）A是-CO-N（A4）或-N（A5）-CO-，Y1和Y2是H或一起键或（b）的通式的生长激素衍生物）A是H，烷基，苯基烷基或RCO，Y 1和Y 2是如权利要求1中定义的酰基，A'，B，C，D，E，F，A1，A2，A3，A4，A5，R和Z具有权利要求1所述的含义具有药理学，特别是GH-，胃和胰腺分泌抑制活性。

5. 发明授权

US4621073A Cyclic peptides having somatostatin activity 失效
标题翻译：具有生长抑素活性的环肽
公开(公告)号：US4621073A
公开(公告)日：1986-11-04
申请号：US575703
申请日：1984-01-31
申请人： Axel Friedrich , Wolfgang Konig , Volker Teetz , Rolf Geiger , Jurgen K. Sandow
发明人： Axel Friedrich , Wolfgang Konig , Volker Teetz , Rolf Geiger , Jurgen K. Sandow
IPC分类号： C07K7/64 , A61K38/00 , A61K38/04 , A61P5/00 , A61P5/02 , C07C231/00 , C07K1/113 , C07K7/06 , C07K14/575 , C07K14/655 , A61K37/24 , C07K7/26
CPC分类号： C07K14/6555 , A61K38/00 , Y10S514/806 , Y10S930/16
摘要： The invention relates to cyclic hexapeptides of the general formula III ##STR1## in which X represents the radical of an L-aminoacid of the general formula IIIa ##STR2## in which A and B are identical or different and denote alkyl having 1 to 3 carbon atoms, or A and B together represent a saturated, unsaturated or aromatic monocyclic or bicyclic structure having 3 to 6 carbon atoms, n denotes 0 or 1, and Y represents an aliphatic or aromatic L-aminoacid the side chain of which can be hydroxylated, and their salts with physiologically tolerated acids, and to a process for their preparation and their use and their intermediates.
摘要翻译：本发明涉及通式III“IMAGE”的环状六肽，其中X表示通式IIIa（IIIa）的L-氨基酸的基团，其中A和B相同或不同，表示具有1 至3个碳原子，或A和B一起表示具有3至6个碳原子的饱和，不饱和或芳族单环或双环结构，n表示0或1，Y表示脂族或芳族L-氨基酸，其侧链可以羟基化，以及它们与生理上耐受的酸的盐，以及它们的制备方法及其用途及其中间体。

6. 发明授权

US5382654A Radiolabelled peptide compounds 失效
标题翻译：放射性标记肽化合物
公开(公告)号：US5382654A
公开(公告)日：1995-01-17
申请号：US831724
申请日：1992-02-05
申请人： Leon R. Lyle , Raghavan Rajagopalan , Karen Deutsch
发明人： Leon R. Lyle , Raghavan Rajagopalan , Karen Deutsch
IPC分类号： A61K51/04 , A61K51/08 , C07B59/00 , C07D213/40 , C07D213/64 , C07D213/68 , C07F13/00 , C07K14/655 , C07K14/815 , C07K7/26 , A61K43/00 , A61K49/02
CPC分类号： C07K14/815 , A61K51/0478 , A61K51/083 , A61K51/088 , C07B59/004 , C07D213/40 , C07D213/64 , C07D213/68 , C07F13/005 , C07K14/6555 , A61K2121/00 , A61K2123/00
摘要： A diagnostic composition suitable for administration to a warm-blooded animal comprising somatostatin or a molecule capable of interacting with the somatostatin receptor labeled with a radionuclide by means of a chelate ligand capable of administration to an animal to produce reliable visual imaging of tumors or therapeutic effects on tumors.
摘要翻译：适用于向温血动物施用的诊断组合物，其包含生长抑素或能够通过能够施用于动物的螯合配体与放射性核素标记的生长抑素受体相互作用的分子以产生肿瘤的可靠视觉成像或治疗效果对肿瘤。

7. 发明授权

US4816438A Insulin-selective somatostatin analogs 失效
标题翻译：胰岛素选择性生长抑素类似物
公开(公告)号：US4816438A
公开(公告)日：1989-03-28
申请号：US033295
申请日：1987-04-01
申请人： Joachim Spiess , Bryan D. Noe
发明人： Joachim Spiess , Bryan D. Noe
IPC分类号： A61K38/00 , C07K14/655 , A61K37/02 , C07K7/26
CPC分类号： C07K14/655 , A61K38/00 , Y10S514/806 , Y10S930/16
摘要： Anglerfish somatostatin-28 has the formula: ##STR1## Anglerfish somatostation-28 is insulin-selective when administered in vivo and is useful for the treatment of insulinoma. The 14-residue C-terminal peptide may also be used.
摘要翻译： Anglerfish生长抑素-28具有以下分子式： + TR Anglerfish somatostation-28在体内施用时具有胰岛素选择性，可用于治疗胰岛素瘤。也可以使用14个残基的C末端肽。

8. 发明授权

US4798821A Antihypertensive therapy for diabetics 失效
标题翻译：糖尿病患者抗高血压治疗
公开(公告)号：US4798821A
公开(公告)日：1989-01-17
申请号：US20611
申请日：1987-03-02
申请人： John F. Hartmann
发明人： John F. Hartmann
IPC分类号： A61K38/00 , C07K14/655 , A61K37/02 , C07K7/26
CPC分类号： C07K14/6555 , A61K38/00 , Y10S514/806 , Y10S930/16 , Y10S930/26 , Y10S930/27
摘要： Process and compositions for lowering blood pressure in diabetic by employing a cyclopeptide compound is described.
摘要翻译：描述了通过使用环肽化合物降低糖尿病患者血压的方法和组合物。

9. 发明授权

US4612302A Clinical use of somatostatin analogues 失效
标题翻译：生长抑素类似物的临床应用
公开(公告)号：US4612302A
公开(公告)日：1986-09-16
申请号：US550978
申请日：1983-11-14
申请人： Sandor Szabo , Klaus W. Usadel , Horst Kessler
发明人： Sandor Szabo , Klaus W. Usadel , Horst Kessler
IPC分类号： A61K38/00 , A61K38/31 , C07K14/655 , A61K37/24 , C07K7/26
CPC分类号： C07K14/6555 , A61K38/31 , Y10S514/806 , Y10S930/16 , Y10S930/26
摘要： A method of increasing the clearance of particles from the blood stream of a vertebrate, which comprises administering to a vertebrate having a surplus of particles in the blood stream of the vertebrate an amount of a somatostatin analogue sufficient to increase phagocytosis in the vertebrate is disclosed along with a method treating vascular lesions or deterioration of biological membranes comprising the step of administering to a human or other mammal suspected of having one or more vascular lesions or of having deterioration of a biological membrane in the liver of said human or mammal an amount of a somatostatin analogue sufficient to reduce the number or severity of said lesions or to prevent further deterioration or reduce the extent of deterioration of said membrane.
摘要翻译：一种从脊椎动物的血流中增加颗粒间隙的方法，其包括向脊椎动物的血流中具有多余颗粒的脊椎动物施用足以增加脊椎动物吞噬作用的生长抑素类似物的量包括处理血管病变或生物膜恶化的方法，包括向疑似患有一种或多种血管病变的人或其他哺乳动物施用或在所述人或哺乳动物的肝脏中使生物膜变质的步骤生长抑素类似物足以减少所述病变的数量或严重程度，或防止进一步恶化或降低所述膜的恶化程度。

10. 发明授权

US5968903A Inhibition of H. pylori proliferation 失效
标题翻译：抑制幽门螺杆菌增殖
公开(公告)号：US5968903A
公开(公告)日：1999-10-19
申请号：US74117
申请日：1998-05-07
申请人： Hiroshi Kaneko , Terunori Mitsuma , Koichi Yamashita , Barry Morgan
发明人： Hiroshi Kaneko , Terunori Mitsuma , Koichi Yamashita , Barry Morgan
IPC分类号： C12N15/09 , A61K38/00 , A61K38/22 , A61K38/31 , A61K45/00 , A61P1/04 , A61P31/04 , A61P35/00 , A61P43/00 , C07K14/655 , A61K37/43 , C07K7/26
CPC分类号： A61K38/31
摘要： The present invention is directed to a method of using somatostatin or a somatostatin agonist to inhibit the proliferation of Helicobacter pylori (H. pylori), which comprises administering to a patient in need thereof an effective amount of said somatostatin or somatostatin agonist. Preferably, a somatostatin sub-type receptor 2 (SSTR-2) selective somatostatin agonist is administered in a method of this invention. The inhibition of H. pylori proliferation is useful in treating various gastroduodenal diseases such as peptic ulcers, gastric cancer and gastric lymphoma.
摘要翻译：本发明涉及使用生长抑素或生长抑素激动剂来抑制幽门螺杆菌（幽门螺杆菌）增殖的方法，其包括向有需要的患者施用有效量的所述生长抑素或生长抑素激动剂。优选地，在本发明的方法中施用生长抑素亚型受体2（SSTR-2）选择性生长抑素激动剂。幽门螺杆菌增殖的抑制可用于治疗各种胃十二指肠疾病如消化性溃疡，胃癌和胃淋巴瘤。

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