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91. 发明授权

US5145837A Treatment of arthritis 失效
标题翻译：治疗关节炎
公开(公告)号：US5145837A
公开(公告)日：1992-09-08
申请号：US715937
申请日：1991-06-14
申请人： Jean H. M. Feyen , Janos Pless
发明人： Jean H. M. Feyen , Janos Pless
IPC分类号： A61K38/04 , A61K38/00 , A61K38/31 , A61P29/00 , C07K14/655
CPC分类号： C07K14/6555 , A61K38/31
摘要： Somatostatin analogues and derivatives in free form or in pharmaceutically acceptable salt or complex form are useful for treating degenerative and inflammatory processes in bone or catilage, e.g. arthritic conditions or diseases.
摘要翻译：游离形式或药学上可接受的盐或复合物形式的生长抑素类似物和衍生物可用于治疗骨或呕吐中的退行性和炎性过程，例如，关节炎病症或疾病。

92. 发明授权

US5073541A Treatment of small cell lung cancer with somatostatin analogs 失效
标题翻译：用SOMATOSTATIN模拟物治疗小细胞肺癌
公开(公告)号：US5073541A
公开(公告)日：1991-12-17
申请号：US231136
申请日：1988-08-11
申请人： John E. Taylor , Arthur E. Bogden , Jacques-Pierre Moreau , David H. Coy
发明人： John E. Taylor , Arthur E. Bogden , Jacques-Pierre Moreau , David H. Coy
IPC分类号： A61K38/04 , A61K38/00 , A61P35/00 , C07K14/655
CPC分类号： C07K14/6555 , A61K38/00
摘要： A method of treating a mammal suffering from cancer by administering to the mammal somatostatin or an analog thereof, the analog being a hexapeptide analog or higher, in a dosage of at least 25 .mu.g/kg/day.
摘要翻译：通过以至少25μg/ kg /天的剂量向哺乳动物生长抑素或其类似物（类似物为六肽类似物或更高剂量）治疗患有癌症的哺乳动物的方法。

93. 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。

94. 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。

95. 发明授权

US4485101A Peptides 失效
标题翻译：多肽
公开(公告)号：US4485101A
公开(公告)日：1984-11-27
申请号：US540380
申请日：1983-10-11
申请人： David H. Coy , William A. Murphy
发明人： David H. Coy , William A. Murphy
IPC分类号： C07K7/08 , A61K38/00 , A61K38/04 , A61K38/22 , A61P5/00 , C07K14/575 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号： C07K14/6555 , A61K38/00 , Y10S930/16
摘要： In one aspect, dodecapeptides capable of inhibiting GH, insulin, and glucagon secretion and having the formulaN-acetyl-Cys-Lys-Asn-A-Phe-D-Trp-Lys-Thr-Phe-Thr-Ser-B-NH.sub.2wherein A is Phe or 4-X-Phe wherein X is Cl, Br, or F, and B is Cys or D-Cys; or a pharmaceutically acceptable salt thereof.
摘要翻译：一方面，能够抑制GH，胰岛素和胰高血糖素分泌并具有式N-乙酰基-Cys-Lys-Asn-A-Phe-D-Trp-Lys-Thr-Phe-Thr-Ser-B-NH 2的十二肽其中A是Phe或4-X-Phe，其中X是Cl，Br或F，B是Cys或D-Cys; 或其药学上可接受的盐。

96. 发明授权

US4395403A Polypeptides, processes for their production, pharmaceutical compositions comprising said polypeptides and their use 失效
标题翻译：新型多肽，其制备方法，包含所述多肽的药物组合物及其用途
公开(公告)号：US4395403A
公开(公告)日：1983-07-26
申请号：US321663
申请日：1981-11-16
申请人： Wilfried Bauer , Janos Pless
发明人： Wilfried Bauer , Janos Pless
IPC分类号： C07K7/06 , A61K38/00 , A61K38/22 , A61P1/00 , A61P5/00 , C07C231/00 , C07K1/113 , C07K14/575 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号： C07K14/6555 , A61K38/00 , Y10S930/26
摘要： Straight-chain and mono-cyclic polypeptides containing the basic sequence ##STR1## wherein X is an amino acid residue, the residues in the 1- and 6-positions being linked by an --S--S-- bridge when the polypeptide is monocyclic, have pharmacological, in particular GH--, gastric- and pancreatic-secretion inhibiting activity.
摘要翻译：含有碱基序列“IMAGE”的直链和单环多肽，其中X为氨基酸残基，当多肽为单环时，通过-SS-桥连接的1位和6位的残基具有药理学，特别是GH-，胃和胰腺分泌抑制活性。

97. 发明授权

US4374060A Process for the preparation of cyclic hexapeptide 失效
标题翻译：制备环六肽的方法
公开(公告)号：US4374060A
公开(公告)日：1983-02-15
申请号：US283404
申请日：1981-07-15
申请人： Ruth F. Nutt
发明人： Ruth F. Nutt
IPC分类号： C07K7/64 , A61K38/00 , A61K38/04 , C07K14/575 , C07K14/655 , C07C103/52
CPC分类号： C07K14/6555 , Y10S930/16
摘要： There is disclosed a process for preparing a cyclic hexapeptide somatostatin analog, specifically cyclo (D-Trp-Lys-Val-Phe-N-Me-Ala-Tyr). The cyclic hexapeptide is synthesized in large quantities in a solution synthesis procedure. However, because of the unexpectedly rapid cyclization rate of this compound, conditions have been developed such that a much more concentrated solution, and thus smaller volumes of the reaction medium, may be employed than would be expected.
摘要翻译：公开了一种制备环状六肽生长抑素类似物，特别是环（D-Trp-Lys-Val-Phe-N-Me-Ala-Tyr）的方法。在溶液合成方法中大量合成了环状六肽。然而，由于这种化合物意想不到的快速环化速率，已经开发了条件，使得可以使用比预期的更多的浓缩溶液，因此反应介质的体积更小。

98. 发明授权

US4316890A Peptides and processes for the manufacture thereof 失效
标题翻译：肽及其制造方法
公开(公告)号：US4316890A
公开(公告)日：1982-02-23
申请号：US129066
申请日：1980-03-10
申请人： Bruno Kamber , Hans Rink , Peter Sieber
发明人： Bruno Kamber , Hans Rink , Peter Sieber
IPC分类号： C07K14/575 , A61K38/00 , A61K38/04 , A61P5/00 , A61P5/02 , C07K1/113 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号： C07K14/6555 , A61K38/00 , Y10S930/16
摘要： The somatostatin-analogous peptides according to the invention of the general formula ##STR1## in which Bmp represents the desaminocysteine radicalX represents Asn or His,trp represents D-Trp that may be substituted in the benzene ring by a halogen atom, andY represents the radical of a secondary .alpha.-amino acid having a maximum of 8 carbon atomsand the corresponding peptide amides and also acid addition salts and complexes thereof are distinguished by strong insulin-antagonistic and glucagon-antagonistic effects and are therefore therapeutically acceptable, preferably in the form of pharmaceutical preparations, in similar indications to those of somatostatin, especially also as antidiabetics. The compounds are manufactured by conventional processes of peptide synthesis, especially by liberation from corresponding protected intermediates and by the formation of the cystine disulphide bridge by means of oxidation.
摘要翻译：根据本发明的通式（IMAGE）的生长抑素类似物肽，其中Bmp表示脱氨基半胱氨酸基团X表示Asn或His，trp表示可在苯环中被卤素原子取代的D-Trp，Y表示具有最多8个碳原子的次级α-氨基酸的基团和相应的肽酰胺及其酸加成盐和复合物的特征在于强的胰岛素拮抗作用和胰高血糖素拮抗作用，并且因此是治疗上可接受的，优选在形式的药物制剂，类似于生长抑素的适应症，特别是抗糖尿病药。该化合物通过肽合成的常规方法制备，特别是通过相应的受保护的中间体的释放和通过氧化形成胱氨酸二硫桥。

99. 发明授权

US4282143A Octapeptides lowering growth hormone 失效
标题翻译：八肽降低生长激素
公开(公告)号：US4282143A
公开(公告)日：1981-08-04
申请号：US159327
申请日：1980-06-13
申请人： Dimitrios Sarantakis
发明人： Dimitrios Sarantakis
IPC分类号： A61K38/00 , C07K14/655 , C07C103/52 , C08L37/00
CPC分类号： C07K14/6555 , A61K38/00 , Y10S930/26
摘要： Polypeptides of the formula: ##STR1## in which X.sub.1 is Phe, D-Phe or C.sub.6 H.sub.5 CH.sub.2 CH.sub.2 CO--;X.sub.2 is Phe, Tyr, Trp, Met or Leu;X.sub.3 is Trp or D-Trp;X.sub.4 is Thr, Val, .alpha.-Abu or Phe;andX.sub.5 is Phe, D-Phe or --NHCH.sub.2 CH.sub.2 C.sub.6 H.sub.5 ;the linear precursor intermediates thereof and pharmaceutically acceptable salts and amides thereof are selective inhibitors of growth hormone release without materially altering blood serum levels of glucagon or insulin. In addition, the above-described compounds are active growth hormone suppressants for periods as long as two hours.
摘要翻译：其中X1是Phe，D-Phe或C6H5CH2CH2CO-的下式的多肽：; X2是Phe，Tyr，Trp，Met或Leu; X3是Trp或D-Trp; X4是Thr，Val，α-Abu或Phe; X5为Phe，D-Phe或-NHCH2CH2C6H5; 其线性前体中间体和其药学上可接受的盐和酰胺是生长激素释放的选择性抑制剂，而不会显着改变胰高血糖素或胰岛素的血清水平。此外，上述化合物是活性生长激素抑制剂长达两个小时。

100. 发明授权

US4238481A Novel cyclopeptides 失效
标题翻译：新型环肽
公开(公告)号：US4238481A
公开(公告)日：1980-12-09
申请号：US942565
申请日：1978-09-15
申请人： Hans Rink , Bruno Kamber , Peter Sieber
发明人： Hans Rink , Bruno Kamber , Peter Sieber
IPC分类号： A61K38/00 , A61K38/04 , A61K38/22 , A61P5/00 , A61P5/02 , A61P43/00 , C07K1/113 , C07K5/097 , C07K7/06 , C07K7/56 , C07K14/575 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号： C07K5/0821 , C07K14/6555 , A61K38/00 , Y02P20/55 , Y10S514/806 , Y10S930/16
摘要： Sulphur-free cyclopeptides with somatostatin-analogous aminoacid partial sequences, of the formula ##STR1## in which R is Asn, Ala or de-R, trp is D-Trp or L-Trp, which can be substituted in the benzene ring by halogen atoms or nitro groups, W is a free or etherified hydroxyl group or halogen atom present as a substituent on the benzene ring of the L-phenylalanine radical, or is hydrogen, X is the radical of an .omega.-amino-lower alkane-(mono or di)-carboxylic acid or de-X and Y is the radical of an .omega.-amino-lower alkane-(mono or di)-carboxylic acid or de-Y, and also acid addition salts and complexes thereof have biological properties similar to those of somatostatin and can be used, especially in the form of pharmaceutical preparations, for the treatment of excessive secretion of somatotropin, insulin and/or glucagon. The compounds according to the invention are obtained by cyclising a corresponding linear peptide compound in which the .epsilon.-amino group of the lysine radical and, if desired, also the hydroxyl group of the threonine radical are protected and detaching the protective groups which are present.
摘要翻译：具有生长抑素 - 类似氨基酸部分序列的无硫环肽，其中R为Asn，Ala或de-R，trp为式（I），其为可在苯中取代的D-Trp或L-Trp 卤素原子或硝基，W是在L-苯丙氨酸基团的苯环上作为取代基存在的游离的或醚化的羟基或卤素原子，或是氢，X是ω-氨基 - 低级烷烃的基团 - （单或二） - 羧酸或脱-X，Y是ω-氨基 - 低级烷烃 - （单或二） - 羧酸或脱Y的基团，并且其酸加成盐和络合物具有生物特性与生长抑素相似，可用于治疗生长激素，胰岛素和/或胰高血糖素过度分泌的药物制剂形式。根据本发明的化合物是通过环化相应的线性肽化合物而获得的，其中赖氨酸基团的ε-氨基和如果需要也保护苏氨酸基团的羟基并分离存在的保护基团。

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