公开(公告)号：US4301045A

公开(公告)日：1981-11-17

申请号：US792524

申请日：1977-05-02

申请人： Emil Kaiser ,  Robert L. Colescott

发明人： Emil Kaiser ,  Robert L. Colescott

IPC分类号： A61K38/00 ,  C07K1/04 ,  C07K14/695 ,  C08L37/00 ,  C07C103/52

CPC分类号： C07K14/695 ,  C07K1/04 ,  A61K38/00 ,  Y10S930/28

摘要： Resin peptides useful in the preparation of peptides having biological activity, and particularly such resin peptides containing Pro--Asp--CH.sub.2 -- or Pro--Asn--CH.sub.2 -- at one end of an amino acid chain, being the resin and Pro, Asp and Asn being the residues of the amino acids proline, aspartic acid and asparagine; and processes for the preparation of such resin peptides.

摘要翻译： 可用于制备具有生物活性的肽的树脂肽，特别是在氨基酸链的一端含有Pro-Asp-CH2-或Pro-Asn-CH2-的树脂肽是树脂，Pro，Asp和Asn是 氨基酸脯氨酸，天冬氨酸和天冬酰胺的残基; 以及制备这种树脂肽的方法。

公开(公告)号：US4130514A

公开(公告)日：1978-12-19

申请号：US876752

申请日：1978-02-10

申请人： Takashi Enkoji ,  Martin O. Skibbe

发明人： Takashi Enkoji ,  Martin O. Skibbe

IPC分类号： A61K38/00 ,  C07K14/695 ,  C08L37/00 ,  A61K37/00 ,  C07C103/52

CPC分类号： C07K14/695 ,  C07K14/6955 ,  A61K38/00 ,  Y10S514/805

摘要： Peptides having adrenocorticotropic hormone activity and resin peptides useful in preparation of such peptides, particularly such peptides having asparagine at the carboxyl end thereof and more particularly such peptides having from 19 to 25 amino acids in their amino acid chains. The invention further involves new processes for the preparation of such peptides.

摘要翻译： 具有促肾上腺皮质激素活性的肽和可用于制备这些肽的树脂肽，特别是在其羧基末端具有天冬酰胺的肽，更特别是在其氨基酸链中具有19至25个氨基酸的肽。 本发明还涉及制备这些肽的新方法。

公开(公告)号：US4104371A

公开(公告)日：1978-08-01

申请号：US811859

申请日：1977-06-30

申请人： Hendrik Marie Greven ,  David DE Wied

发明人： Hendrik Marie Greven ,  David DE Wied

IPC分类号： A61K31/16 ,  A61K38/00 ,  A61P25/00 ,  C07K1/113 ,  C07K5/103 ,  C07K7/06 ,  C07K14/695 ,  C07C103/52

CPC分类号： C07K14/6955 ,  C07K5/1008 ,  A61K38/00

摘要： Biologically active novel peptides and peptide-derivatives of the general formula: ##STR1## where A represents H-(L or D)Met, H-(L or D)Met(.fwdarw.O), H-(L or D)Met(.fwdarw.O.sub.2)desamino-Met, desamino-Met(.fwdarw.O),desamino-Met(.fwdarw.O.sub.2) or the group H.sub.2 N--B--CO--;B represents a branched or straight-chain alkylene (C.sub.1 -C.sub.6) or alkylidene (C.sub.1 -C.sub.6) group;Q represents the amino-acid residue --NH--CHR--CO--;R represents alkyl (C.sub.1 -C.sub.6), p-hydroxyphenylmethyl, 3-indolylmethyl or phenylmethyl;R.sub.1 and R.sub.2 represent hydrogen or an alkyl(1-6C) group, andZ represents N-(phenylalkyl)amino, N-(.beta.-indolylalkyl)amino, L-Trp-OH, L-Phe-OH, L-Trp-Gly-OH or L-Phe-Gly-OH, as well as the functional derivatives thereof.

摘要翻译： 生物活性的新型肽和肽衍生物，通式如下：其中A表示H-（L或D）Met，H-（L或D）Met（ - > O），H-（L或D） （ - > O 2）desamino-Met，desamino-Met（ - > O），desamino-Met（ - > O 2）或H 2 N-B-CO-基团; B表示支链或直链亚烷基（C1-C6）或亚烷基（C1-C6）基团; Q表示氨基酸残基-NH-CHR-CO-; R代表烷基（C1-C6），对羟基苯基甲基，3-吲哚基甲基或苯基甲基; R 1和R 2表示氢或烷基（1-6C）基团，Z表示N-（苯基烷基）氨基，N-（β-吲哚基烷基）氨基，L-Trp-OH，L-Phe-OH，L-Trp- Gly-OH或L-Phe-Gly-OH，以及其功能衍生物。

公开(公告)号：US4071510A

公开(公告)日：1978-01-31

申请号：US683144

申请日：1976-05-04

申请人： Lars Ake Ingemar Carlsson ,  Jan Louis Mulder

发明人： Lars Ake Ingemar Carlsson ,  Jan Louis Mulder

IPC分类号： A61K38/00 ,  C07K14/695 ,  C07C103/52 ,  A61K37/00

CPC分类号： C07K14/695 ,  C07K14/6955 ,  A61K38/00 ,  Y10S514/805

摘要： The invention concerns peptides having the general formula X--Glu--His--Phe--Arg--Trp--Gly--Lys--Pro--Val--Gly--Lys--Lys--Y--NH.sub.2 wherein X represents alkyloxy carbonyl, aryl alkyloxy carbonyl or D-Ser-Met, and Y represents a residue of n diaminomonocarboxylic acids, n being an integer of 2-4, and a method of producing the same.

摘要翻译： 本发明涉及具有通式X-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Val-Gly-Lys-Lys-Y-NH 2的肽，其中X表示烷氧基羰基，芳基烷氧基羰基或D-Ser -Met，Y表示n个二氨基单羧酸的残基，n为2-4的整数，及其制备方法。

公开(公告)号：US3953415A

公开(公告)日：1976-04-27

申请号：US360198

申请日：1973-05-14

申请人： Lajos Kisfaludy ,  Miklos Low ,  Istvan Schon ,  Tamas Szirtes ,  Maria Sz. Sarkozi ,  Sandor Bajusz ,  Andrae Turan ,  Rosa Beks ,  Attila Juhasz ,  Laszlo Graf ,  Kalman Medzihradszky ,  Laszlo Szporny

发明人： Lajos Kisfaludy ,  Miklos Low ,  Istvan Schon ,  Tamas Szirtes ,  Maria Sz. Sarkozi ,  Sandor Bajusz ,  Andrae Turan ,  Rosa Beks ,  Attila Juhasz ,  Laszlo Graf ,  Kalman Medzihradszky ,  Laszlo Szporny

IPC分类号： A61K38/00 ,  C07C67/00 ,  C07C231/00 ,  C07C231/12 ,  C07C271/22 ,  C07K1/06 ,  C07K1/08 ,  C07K7/08 ,  C07K14/575 ,  C07K14/695 ,  C07C103/52 ,  C07G7/00

CPC分类号： C07C271/22 ,  C07K1/066 ,  C07K1/088 ,  C07K14/695 ,  A61K38/00

摘要： The invention relates to the preparation of biologically active polypeptides containing the aspartyl group, particularly an aspartyl-glycine moiety, using the active-ester technique.According to the method of the invention, human adrenocorticotropic hormone and its fragments characteristic to the individual species, as well as the blocked derivatives of such compounds are prepared by the pentafluorophenol method, i.e., the carboxy group of the acylating component is activated by converting it into pentafluorophenyl ester in the coupling reaction carried out with blocked peptides containing the aspartyl group or an aspartylglycine moiety. The acylation is carried out preferably using equimolar quantities of the respective reactants. The free peptides obtained after removing the blocking groups can be converted into their acid addition salts or pharmaceutically acceptable complexes or condensates.Human adrenocorticotropic hormone and its derivatives are valuable substances of therapeutical activity.

摘要翻译： 本发明涉及使用活性酯技术制备含有天冬氨酰基，特别是天冬氨酰 - 甘氨酸部分的生物活性多肽。

公开(公告)号：US3873511A

公开(公告)日：1975-03-25

申请号：US12454971

申请日：1971-03-15

申请人： SHIONOGI & CO

发明人： OTSUKA HIDEO ,  INOUYE KEN

IPC分类号： A61K38/00 ,  C07K14/695 ,  C07C103/52

CPC分类号： C07K14/695 ,  A61K38/00 ,  Y10S514/805

摘要： Highly active corticotropin peptides which have an Alpha aminoisobutyric acid residue at the amino-terminal in place of the serine in native corticotropin, derivatives thereof, intermediates therefor and compositions thereof are disclosed. Such peptides are useful as a medicament, because they show corticotropic properties remarkably improved in enhancement of potency and prolongation of action. They can be prepared by condensing the amino acids together one by one or by condensing the small peptide fragments together in a per se conventional manner.

摘要翻译： 公开了在天然促肾上腺皮质激素，其衍生物，其中间体及其组合物中在氨基末端具有α-氨基异丁酸残基代替丝氨酸的高活性促肾上腺皮质激素肽。 这样的肽可用作药物，因为它们显示出在提高效力和作用延长方面显着改善的皮质醇性质。 它们可以通过将氨基酸一个一个地缩合在一起，或者通过将这些小肽片段以本来常规的方式一起冷凝来制备。

公开(公告)号：US3810881A

公开(公告)日：1974-05-14

申请号：US26055472

申请日：1972-06-07

申请人： CIBA GEIGY CORP

发明人： RITTEL W ,  BRUGGER M

IPC分类号： A61K38/00 ,  C07D207/46 ,  C07K14/695 ,  C07C103/52 ,  C07G7/00

CPC分类号： C07D207/46 ,  A61K38/00 ,  C07K14/6955 ,  Y10S514/805

摘要： PEPTIDES AND PEPTIDE AMIDES CONTAINING 18-39 AMINOACIDS OF THE N-TERMINUS OF NATURAL CORTICOTROPINS, BUT IN WHICH THE FIRST AMINOACID IS REPLACED BY D-A-PHENYLGLYCINE AND THE AMINOACIDS IN THE POSITIONS 17 AND 18 ARE REPLACED BY L-LYSINE OR L-ORNITHINE, AND ANALOGUES OF THESE COMPOUNDS.

公开(公告)号：US3775466A

公开(公告)日：1973-11-27

申请号：US12542671

申请日：1971-03-17

申请人： HOECHST AG

发明人： JAGER G ,  GEIGER R

IPC分类号： A61K38/00 ,  C07K1/06 ,  C07K1/12 ,  C07K5/02 ,  C07K5/09 ,  C07K5/097 ,  C07K5/103 ,  C07K5/107 ,  C07K14/695 ,  C07C133/10 ,  C07C125/04

CPC分类号： C07K5/0823 ,  A61K38/00 ,  C07K1/062 ,  C07K1/063 ,  C07K1/064 ,  C07K1/068 ,  C07K1/12 ,  C07K5/0215 ,  C07K5/0815 ,  C07K5/1005 ,  C07K5/1016 ,  C07K14/695

摘要： ISOBORNYLOXYCARBONYLAMINO ACIDS AND DERIVATIVES THEREOF, PARTICULARLY NA-BENZYLOXYCARBONYL-NG,NG-BIS - (ISOBORONYLOXYCARBONYL)ARGININE, NG,NG-BIS-(ISOBORONYOXYCARBONYL)-ARGININE, AND NG,NG,NG-TRIS-(ISOBORONYLOXYCARBONYL)-ARGINIE, USEFUL AS INTERMEDIATES IN THE SYNTHESIS OF PEPTIDES, PREPARED BY REACTING AN AMINO ACID OR DERIVATIVES THEREOF EITHER WITH ISOBORONYLOXYCARBONYL CHLORIDE OR WITH AN ISOBORONYLOXYCARBONYL ACTIVE ESTER.

公开(公告)号：US3761461A

公开(公告)日：1973-09-25

申请号：US3761461D

申请日：1967-01-10

申请人： SANDOZ LTD

发明人： PLESS J ,  GUTTMANN S ,  BOISSONNAS R

IPC分类号： A61K38/00 ,  C07K5/072 ,  C07K14/695 ,  C07C103/52

CPC分类号： C07K5/06104 ,  A61K38/00 ,  C07K14/6955 ,  Y02P20/55 ,  Y10S514/805

摘要： THE PRESENT INVENTION PROVIDES THE PENTACOSAPERPTIDES OF GENERAL FORMULA D-SERYL-L-TYROSYL-L-SERYL-L-NORLENCYLX-L-HISTIDYL-L-PHENYLALANYL-L-ARGINYL-L-TRYPTOPHANYL-GLYCYL-L-LYSYL-L-PROTYL-L-VALYL-GLYCYLL-LYSYL-L-LLYSYL-L-LYSYL-L-LYSYL-L-PROLYL-LVALYL-L-LYSYL-L-VALYL-L-TYROSYL-L-PROLYL-L-VALINAMIDE, IN WHICH X SIGNIFIES AN L-GLUTAMYL OR L-GLUTAMINYL RADICAL, THEIR THERAPEUTICALLY ACTIVE ACID ADDITION SALTS AND HEAVY METAL COMPLEXES. THE PENTACOSAPEPTIDES OF THE ABOVE FORMULA, THEIR SALTS AND HEAVY METAL COMPLEXES EXHIBIT A HIGH ADRENOCORTICOTROPIC EFFECT. THE PRODUCTION OF THESE PEPTIDES IS FURTHERMORE DESCRIBED.

公开(公告)号：US3759891A

公开(公告)日：1973-09-18

申请号：US3759891D

申请日：1971-03-22

申请人： SHIONOGI & CO

发明人： OTSUKA H ,  INOUYE K

IPC分类号： C07K14/695 ,  C07C103/52 ,  C07G7/00 ,  C08H1/00

CPC分类号： C07K14/695 ,  Y10S514/805 ,  Y10S930/29

摘要： CORTICOTROPICALLY ACTIVE OCTADECAPEPTIDES WHEREIN THE FIRST AMINO ACID, SERINE, AND THE FIFTEENTH AMINO ACID, LYSINE, IN THE NATIVE CORTICOTROPIN MOLECULE ARE SUBSTITUTED RESPECTIVELY BY B-ALANINE AND ORNITHINE, DERIVATIVES THEREOF, NON-TOXIC ACID ADDITION SALTS THEREOF AND COMPLEXES THEREOF ARE DISCLOSED. SUCH PEPTIDES ARE USEFUL AS A MEDICAMENT, BECAUSE THEY SHOW CORTICOTROPIC PROPERTIES REMARKABLY IMPROVED IN PROLONGATION OF ACTION. THEY CAN BE PREPARED BY CONDENSING THE AMINO ACIDS TOGETHER ONE BY ONE OR BY CONDENSING THE SMALL PEPTIDE FRAGMENTS TOGETHER IN A PER SE CONVENTIONAL MANNER.