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41. 发明授权

US5296608A Intermediates for analogs of tyrosine sulfate or tyrosine phosphate containing peptides 失效
标题翻译：用于酪氨酸硫酸酯或含酪氨酸磷酸酯的肽类似物的中间体
公开(公告)号：US5296608A
公开(公告)日：1994-03-22
申请号：US865431
申请日：1992-04-09
申请人： Waleed Danho , Jefferson W. Tilley , Joseph Triscari , Rolf Wagner
发明人： Waleed Danho , Jefferson W. Tilley , Joseph Triscari , Rolf Wagner
IPC分类号： A61K38/00 , C07K14/595 , A61K31/41 , C07D257/04
CPC分类号： C07K14/595 , A61K38/00
摘要： Analogs of Tyrosine Sulfate or Tyrosine Phosphate containing peptides, the novel intermediate compounds used in the preparation of these analogs, as well as a method for suppressing appetite in subjects by administering to the subject an effective amount of CCK analog wherein one or more of any Tyrosine Sulfate present is substituted with a radical of the invention.
摘要翻译：含有酪氨酸硫酸酯或含酪氨酸磷酸酯的肽的类似物，用于制备这些类似物的新型中间体化合物，以及通过向受试者施用有效量的CCK类似物来抑制受试者的食欲的方法，其中一种或多种任何酪氨酸硫酸盐存在被本发明的基团取代。

42. 发明授权

US5190921A Amino acids and peptides having a modified tyrosine residue, their preparation and their application as medicaments 失效
标题翻译：具有改性酪氨酸残基的氨基酸和肽，其制备及其作为药物的应用
公开(公告)号：US5190921A
公开(公告)日：1993-03-02
申请号：US825294
申请日：1992-01-24
申请人： Bernard P. Roques , Isabelle Marseigne , Bruno Charpentier
发明人： Bernard P. Roques , Isabelle Marseigne , Bruno Charpentier
IPC分类号： C07K1/06 , A61K38/00 , C07C323/66 , C07F9/12 , C07F9/38 , C07F9/40 , C07F9/58 , C07K1/113 , C07K5/02 , C07K7/02 , C07K7/06 , C07K14/595
CPC分类号： C07K14/595 , C07F9/3882 , C07F9/4056 , C07K5/0212 , C07K7/02 , A61K38/00
摘要： These compounds are represented by formula (I), in which each of R.sub.1 R.sub.2 =H, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl, or aromatic; (when R.sub.1 =H, R.sub.2 can be an amine function-protecting radical, amino acid residue or peptide fragment; R.sub.1 and R.sub.2 being capable of forming, with N, a 5-7 component ring); A=carbonyl or methylene; W=hydroxy, phenoxy, C.sub.1 -C.sub.8 alkoxy; phenoxy(C.sub.1 -C.sub.8 alkyl), amino, (C.sub.1 -C.sub.8 alkyl)amino, di(C.sub.1 -C.sub.8 alkyl)amino, (when A=carbonyl, W=amino acid residue or peptide fragment); Y=--OSO.sub.2 OR.sub.3 (II), --OPO(OR.sub.3).sub.2 (III), --(CH.sub.2 (.sub.m --SO.sub.2 OR.sub.3 (IV) or --(CH.sub.2).sub.m --PO(OR.sub.3).sub.2 (V) [R.sub.3 =H, C.sub.1 -C.sub.8 alkyl; m=1 to 4]; Z=cyclohexane, pyridyl or phenyl; n=0 to 4; on the condition that when Y=(II) or (III), -A-W is other than a sequence composed of natural amino acids. They have antipsychotic properties, an effect facilitating the memorization processes, analgesic properties; they are useful as anorexia-producing agents, and they have stimulatory effects on intestinal motility. ##STR1##
摘要翻译：这些化合物由式（I）表示，其中R 1和R 2各自为H，C 1 -C 8烷基，C 3 -C 7环烷基或芳族; （当R1 = H时，R2可以是胺官能保护基，氨基酸残基或肽片段; R1和R2能够与N形成5-7组分环）; A =羰基或亚甲基; W =羟基，苯氧基，C 1 -C 8烷氧基; 苯氧基（C 1 -C 8烷基），氨基，（C 1 -C 8烷基）氨基，二（C 1 -C 8烷基）氨基，（当A =羰基，W =氨基酸残基或肽片段时） Y = -OSO 2OR 3（II），-OPO（OR 3）2（III）， - （CH 2（m-SO 2 OR 3（Ⅳ））或 - （CH 2）m PO（OR 3）2（Ⅴ） C8烷基; m = 1〜4]; Z =环己烷，吡啶基或苯基; n = 0〜4;在Y =（II）或（III）的情况下，-AW不是由天然氨基酸，它们具有抗精神病性质，促进记忆过程，止痛性质的作用;它们可用作厌食产生剂，并且对肠蠕动具有刺激作用。

43. 发明授权

US5059679A Method of selectively sulfating peptides 失效
标题翻译：选择性硫酸化肽的方法
公开(公告)号：US5059679A
公开(公告)日：1991-10-22
申请号：US331292
申请日：1989-03-30
申请人： Haruaki Yajima , Nobutaka Fujii , Shinya Kiyama
发明人： Haruaki Yajima , Nobutaka Fujii , Shinya Kiyama
IPC分类号： C07K1/06 , C07K1/00 , C07K1/113 , C07K14/00 , C07K14/575 , C07K14/595
CPC分类号： C07K1/006 , C07K14/595 , Y02P20/55
摘要： The invention provides a method and reagent for the modification of polypeptides useful in experimental research in the area of genetic engineering starting from a polypeptide such as hCCK-33 in an unsulfated form which contains Tyr and Ser and/or Thr residues by first protecting the amino-groups in the starting polypeptide, masking the OH-groups in the Ser and/or Thr residues and selectively sulfating the OH-groups in the Tyr residues after deprotection.
摘要翻译：本发明提供了一种用于修饰可用于基因工程领域的实验研究领域的多肽的方法和试剂，其以多肽例如hCCK-33（其含有Tyr和Ser和/或Thr残基的未硫酸化形式）首先保护氨基 - 起始多肽中的基团，掩蔽Ser和/或Thr残基中的OH-基团，并且在去保护后选择性硫酸化Tyr残基中的OH-基团。

44. 发明授权

US5013722A Cholecystokinin analogs for controlling appetite 失效
标题翻译：胆囊收缩素类似物用于控制食欲
公开(公告)号：US5013722A
公开(公告)日：1991-05-07
申请号：US400177
申请日：1989-08-25
申请人： Waleed Danho , Vincent S. Madison , Joseph Triscari
发明人： Waleed Danho , Vincent S. Madison , Joseph Triscari
IPC分类号： A61K38/00 , C07K14/595
CPC分类号： C07K14/595 , C07K14/5955 , A61K38/00
摘要： Cholecystokinin analogs useful for suppressing food intake in mammals and humans.
摘要翻译：用于抑制哺乳动物和人类食物摄入的缩胆囊素类似物。

45. 发明授权

US4997950A Novel C-terminal gastrin antagonists 失效
公开(公告)号：US4997950A
公开(公告)日：1991-03-05
申请号：US341084
申请日：1989-04-20
申请人： Richard Finbar Murphy , Alistair J. Douglas , Brian Walker
发明人： Richard Finbar Murphy , Alistair J. Douglas , Brian Walker
IPC分类号： A61K38/00 , C07K5/02 , C07K5/06 , C07K5/087 , C07K5/097 , C07K5/117 , C07K14/595
CPC分类号： C07K5/0821 , C07K14/595 , C07K5/02 , C07K5/0202 , C07K5/06043 , C07K5/0812 , C07K5/1024 , A61K38/00
摘要： A series of derivatives of the biologically active C-terminus of gastrin was synthesized to study the structural activity of the molecule and also to determine the smallest and highest affinity inhibitor of gastrin. Earlier work speculated that a peptide resistant to dipeptidase contained in a receptor would be an effective gastrin antagonist. Methods: Five dogs with both chronic gastric fistulae and Heidenhein pouches were used. After an 18 hour fast, gastric juice was collected both from the gastric fistula and pouch over 200 minutes at 10 minute intervals. MMC (Migrating Motor Complex) was monitored by a small balloon in the gastric antrum. Collections were initiated at the beginning of phase I of the MMC and were obtained under 3 conditions: Control, pentagastrin infusion (0.5 .mu.g/Kg/h, i.v.) and pentagastrin+peptide infusion (Indole propionic acid [IPA]- Leu-Asp-Phenethyl amine [PEA], Boc-Trp-Leu-.beta.Ala, IPA-Leu-.beta.Ala, or Boc-Trp-Leu-Asp-methyl meta Aminobenzoic acid {mABAOMe] at 20 pmol/kg/h for 70 min.). Pentagastrin infusion was started immediately before the next peak of the MMC. Peptides were infused 60 minutes after starting pentagastrin infusion. Results: All four peptides inhibited the stimulated acid secretion causing it to approach the control level.______________________________________ Inhibition of the stimulated acid secretion (.DELTA. meq/kg) Heidenhein Gastric Fistula Pouch ______________________________________ IPA--Leu--Asp--PEA .dwnarw.303 .+-. 120* .dwnarw.18 .+-. 11* Boc--Trp--Leu-.beta.Ala .dwnarw.618 .+-. 168** .dwnarw.35 .+-. 8** IPA--Leu-.beta.Ala .dwnarw.562 .+-. 249* .dwnarw.34 .+-. 12* Boc--Trp--Leu--Asp- .dwnarw.446 .+-. 172** .dwnarw.40 .+-. 16** mABAOMe ______________________________________ (*p

46. 发明授权

US4636490A Novel peptidic derivatives inhibiting gastric secretion, process for preparing them and drugs containing them 失效
标题翻译：抑制胃分泌的新型肽衍生物，其制备方法和含有它们的药物
公开(公告)号：US4636490A
公开(公告)日：1987-01-13
申请号：US597427
申请日：1984-04-06
申请人： Jean Martinez , Jean-Pierre Bali , Bertrand Castro , Dino Nisato , Henri Demarne
发明人： Jean Martinez , Jean-Pierre Bali , Bertrand Castro , Dino Nisato , Henri Demarne
IPC分类号： A61K38/22 , A61K38/00 , A61P1/00 , C07K7/06 , C07K14/595 , A61K37/43
CPC分类号： C07K14/595 , A61K38/00
摘要： The invention relates to peptides of general formula:R--A--Gly--Trp--B--Asp--NH.sub.2 (I)in which:Asp NH.sub.2 represents the amide in .alpha. position of the aspartic acid of formula: ##STR1## R represents hydrogen, a protector group of the terminal amine function such as t.butyloxy carbonyl (BOC), benzyloxy carbonyl (Z), lower alkanoyl,A designates:either tyrosine, tyrosine-O-sulfate, threonine or methionine;or a dipeptide selected from: --Ala--TYR--, --TYR--Thr--, --TYR Met--, TYR designating either of the 2 amino-acids tyrosine or tyrosine-O-sulfate;or a tripeptide selected from: --Glu--Ala--TYR--, Asp--TYR--Thr--, --Asp--TYR--MET--;or a tetrapeptide selected from: --Glu--Glu--Ala--TYR--, --Gln Asp--TYR--Thr--, --Arg--ASP--TYR--Met--;or a pentapeptide selected from: --Glu--Glu--Glu--Ala--TYR--, --Pyr--Gln--Asp--TYR--Thr--, --Asp--Arg--Asp--TYR--Met;B designates methionine, leucine or norleucine.
摘要翻译：本发明涉及通式为：RA-Gly-Trp-B-Asp-NH 2（I）的肽，其中：Asp NH 2表示式中天冬氨酸的α位置的酰胺：R表示氢，保护基末端胺官能团如叔丁氧基羰基（BOC），苄氧基羰基（Z），低级烷酰基，A表示：酪氨酸，酪氨酸-O-硫酸盐，苏氨酸或甲硫氨酸; 或选自以下的二肽：-Ala-TYR-，-TYR-Thr-，-TYR Met-，TYR，其指定2个氨基酸酪氨酸或酪氨酸-O-硫酸盐中的任一个; 或选自以下的三肽：-Glu-Ala-TYR-，Asp-TYR-Thr-，-Asp-TYR-MET-; 或选自以下的四肽：-Glu-Glu-Ala-TYR-，-Gln Asp-TYR-Thr-，-Arg-ASP-TYR-Met-; 或选自以下的五肽：-Glu-Glu-Glu-Ala-TYR-，-Pyr-Gln-Asp-TYR-Thr-，-Asp-Arg-Asp-TYR-Met; B表示甲硫氨酸，亮氨酸或正亮氨酸。

47. 发明授权

US4444682A Method of sulfation 失效
标题翻译：硫酸化方法
公开(公告)号：US4444682A
公开(公告)日：1984-04-24
申请号：US439312
申请日：1982-11-04
申请人： Jean E. F. Rivier , Botond Penke
发明人： Jean E. F. Rivier , Botond Penke
IPC分类号： C07D207/16 , C07D213/20 , C07D213/74 , C07K1/00 , C07K7/23 , C07K14/595 , C07C103/52 , C07C147/02 , C07C149/20 , C07C149/40
CPC分类号： C07D213/20 , C07D207/16 , C07D213/74 , C07K1/006 , C07K14/595 , C07K7/23 , Y10S930/13
摘要： A method for sulfating a hydroxy amino acid or a residue of such an amino acid in a peptide by reaction with a reagent which is a tertiaryammonium salt of acetylsulfuric acid having the formula:[CH.sub.3 COOSO.sub.3 ].sup.- [R].sup.+wherein R is triethylamine, ethyldiisopropylamine, pyridine, 4-methylmorpholine or 4-N,N-dimethylaminopyridine. The .alpha.-amino group and any other labile side chains present may be protected or may be left unprotected at the time the sulfation takes place.
摘要翻译：通过与具有下式的[CH3COOSO3] - [R] +的乙酰硫酸的叔铵盐的试剂反应来硫酸化肽中的羟基氨基酸或这种氨基酸的残基的方法，其中R是三乙胺，乙基二异丙胺，吡啶，4-甲基吗啉或4-N，N-二甲基氨基吡啶。存在的α-氨基和任何其它不稳定的侧链可以被保护，或者可能在硫酸化发生时不被保护。

48. 发明授权

US4368192A Peptides 失效
标题翻译：多肽
公开(公告)号：US4368192A
公开(公告)日：1983-01-11
申请号：US145500
申请日：1980-04-29
申请人： Erich Wunsch
发明人： Erich Wunsch
IPC分类号： A61K38/00 , C07K1/06 , C07K14/595 , A61K37/00 , C07C103/52
CPC分类号： C07K14/595 , C07K1/065 , A61K38/00
摘要： Peptides having the carboxyl terminated sequence of the pancreozymin-cholstokinin 25-33 modified such that the amino acid group 25 carries a strongly basic group, the amino acid group 28 exhibits a hydrophilic character similar to that of the hydroxyamino acids and the amino acid group 31 exhibits a strongly hydrophobic character similar to that of amino acids with aliphatic side chains, and in particular nonapeptides having the sequence H--X--Asp--Tyr(SO.sub.3 H)--Y--Gly--Trp--Z--Asp--Phe--NN.sub.2 wherein X is arginine, homoarginine, norarginine, N.sub..epsilon.,N.sub..epsilon. -dialkyllysine, N.sub..delta. or N.sub..delta. -dialkyl-ornithine, Y is threonine, serine or hydroxy-proline and Z is norleucine, leucine, norvaline or .alpha.-amino-butyric acid, possess pronounced pancreozymin activity and can be employed in pharmaceutical preparations for controlling the function of the gall bladder and for controlling the enzyme secretion of the pancreas. Tyrosine-O-sulfate-barium salt and its N-acyl derivatives can be used as intermediate products for the preparation of peptides. For introducing the amino acid group 27 an N-acyl-tyrosine is reacted with an excess of pyridine-SO.sub.3 in a polar organic solvent, the resulting solution is extracted with water, the barium salt of the N-acyl-tyrosine-O-sulfate is precipitated from the aqueous phase by addition of a soluble barium compound, possibly the acyl group is split off in conventional manner, and the resulting tyrosine-O-sulfate-barium salt or its acyl derivative are processed employing the usual methods of peptide synthesis.
摘要翻译：具有胰蛋白酶 - 缩胆囊素25-33羧基末端序列的肽被修饰，使得氨基酸25携带强碱性基团，氨基酸组28表现出与羟基氨基酸和氨基酸组31相似的亲水性表现出类似于具有脂族侧链的氨基酸的强疏水性，特别是具有序列HX-Asp-Tyr（SO3H）-Y-Gly-Trp-Z-Asp-Phe-NN2的非肽，其中X是精氨酸，精氨酸，降血清蛋白，Nε，Nε-二烷基赖氨酸，N或N二烷基鸟氨酸，Y是苏氨酸，丝氨酸或羟基脯氨酸，Z是正亮氨酸，亮氨酸，正缬氨酸或α-氨基丁酸，具有显着的胰酶活性，可用于控制胆囊功能和控制胰腺酶分泌的药物制剂中。酪氨酸-O-硫酸盐钡盐及其N-酰基衍生物可用作制备肽的中间产物。为了引入氨基酸组27，使N-酰基酪氨酸与极性有机溶剂中过量的吡啶-SO 3反应，所得溶液用水萃取，N-酰基 - 酪氨酸-O-硫酸盐的钡盐通过加入可溶性钡化合物从水相中沉淀出来，可能以常规方式将酰基分离出来，所得到的酪氨酸-O-硫酸盐 - 钡盐或其酰基衍生物使用通常的肽合成方法进行处理。

49. 发明授权

US3847891A Separation of secretin and cholecystokinin-pancreozymin from mixture thereof 失效
标题翻译：从其混合物中分离分离蛋白和选择性蛋白 - 胰蛋白酶
公开(公告)号：US3847891A
公开(公告)日：1974-11-12
申请号：US35224073
申请日：1973-04-18
申请人： EISAI CO LTD
发明人： TACHIBANA S
IPC分类号： A61K38/00 , C07K14/595 , A61K27/00 , C07C103/52
CPC分类号： C07K14/595 , A61K38/00 , Y10S530/844
摘要： 1. A PROCESS FOR THE SEPARATION OF SECRETIN AND CHOLECYSTOKININ-PANCREOZYMIN FROM A MIXTURE THEREOF, COMPRISING (A) CONTACTING THE MIXTURE IN AQUEOUS SOLUTION AT A PH RANGING FROM ABOUT 9 TO ABOUT 12, WITH AN ANIONEXCHANGE RESIN TO CAUSE SELECTIVE ADSORPTION OF CHOLECYSTOKININ-PANCREOZYMIN ON SAID RESIN AND RESERVING THE REMAINING AQUEOUS SOLUTION, (B) ELUTING THE CHLOECYSTOKININ-PANCREOZYMIN FROM SAID RESIN BY CONTACTING IT WITH AN AQUEOUS ELUTING MEDIUM AT PH LOWER THAN 9: AND (C9 RECOVERING THE CHOLECYSTOKININ-PANCREZYOIN FROM THE ELUATE OF STEP (B) AND RECOVERING THE SECRETIN FROM THE AQUEOUS SOLUTION OBTAINED FROM STEP 8A), WHICH SOLUTION CONTAINS THE SECRETION NOT ADSORBED BY SAID RESIN.

50. 发明授权

US10406207B2 Peptide conjugates of GLP-1 receptor agonists and gastrin and their use 有权
公开(公告)号：US10406207B2
公开(公告)日：2019-09-10
申请号：US15381993
申请日：2016-12-16
申请人： Zealand Pharma A/S
发明人： Trine Skovlund Ryge Neerup , Torben Østerlund , Jakob Lind Tolborg , Keld Fosgerau , Ulrika Martensson , Marianne Brorson , Kamilla Rolsted
IPC分类号： A61K38/00 , A61K38/22 , C07K14/575 , C07K14/595 , C07K14/605 , A61K38/26 , A61K45/06 , C07K14/46 , A61K47/60
摘要： The present invention relates, inter alia, to certain peptide conjugates, and to the use of the conjugates in the treatment of a variety of diseases or disorders, including diabetes (type 1 and/or type 2) and diabetes related diseases or disorders.

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