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11. 发明授权

US3947569A Process for preparing the releasing hormone of luteinizing hormone (LH) and of follicle stimulating hormone (FSH), salts and compositions thereof, and intermediates therefor 失效
标题翻译：制备促黄体激素（LH）和促卵泡激素（FSH）的释放激素及其盐及其组合物及其中间体的方法
公开(公告)号：US3947569A
公开(公告)日：1976-03-30
申请号：US451328
申请日：1974-03-14
申请人： Hans U. Immer , Verner R. Nelson , Manfred K. Gotz
发明人： Hans U. Immer , Verner R. Nelson , Manfred K. Gotz
IPC分类号： A61K38/00 , C07K5/097 , C07K5/103 , C07K7/23 , A61K29/00 , A61K37/00
CPC分类号： C07K5/0825 , C07K5/1005 , C07K7/23 , A61K38/00 , Y10S514/80 , Y10S930/13
摘要： A process for preparing the LH- and FSH-releasing hormone of the formula Ih--pyr--His--Trp--Ser--Tyr--Gly--Leu--Arg--Pro--Gly--NH.sub.2which is isolated as the hydrochloride salt and optionally converted to other pharmaceutically acceptable salts or to pharmaceutically acceptable metal complexes.
摘要翻译：制备式I H-Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH 2的LH-和FSH释放激素的方法，其分离为盐酸盐，并任选转化为其它药学上可接受的盐或药学上可接受的金属络合物。

12. 发明授权

US4081530A Extended chain derivatives of somatostatin 失效
标题翻译：生长抑素的延伸链衍生物
公开(公告)号：US4081530A
公开(公告)日：1978-03-28
申请号：US583947
申请日：1975-06-04
申请人： Hans U. Immer , Verner R. Nelson , Kazimir Sestanj
发明人： Hans U. Immer , Verner R. Nelson , Kazimir Sestanj
IPC分类号： A61K38/00 , C07K5/103 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号： C07K14/655 , C07K5/1008 , A61K38/00 , Y10S514/806 , Y10S930/16
摘要： Compounds of the formula 1 or 1a ##STR1## wherein R.sup.1 is H--, H--Gly or H--Leu and R.sup.2 is H or COOH and pharmaceutically acceptable salts thereof, are disclosed. The compounds of formulae 1 and 1a are useful for the management of diabetes and the treatment of acromegaly. Methods for their use are also disclosed.
摘要翻译：式1或1a的化合物R1-Gly-Gly-Ala-Gly-（I）+ TRI-Gly-Gly-Ala-Gly-（Ia）+ tr其中R1是H，H -Gly或H-Leu，R2是H或COOH及其药学上可接受的盐。式1和1a的化合物可用于治疗糖尿病和肢端肥大症的治疗。还公开了它们的使用方法。

13. 发明授权

US4216209A Tripeptide angiotensin converting enzyme inhibitors 失效
标题翻译：三肽血管紧张素转换酶抑制剂
公开(公告)号：US4216209A
公开(公告)日：1980-08-05
申请号：US21737
申请日：1979-03-19
申请人： Francesco Bellini , Hans U. Immer
发明人： Francesco Bellini , Hans U. Immer
IPC分类号： C07K5/06 , C07K5/078 , C07K5/097 , A61K37/00 , C07C103/52
CPC分类号： C07K5/06165 , C07K5/06069 , C07K5/0823 , Y10S530/80
摘要： Compounds of the formula HSCH.sub.2 CHR.sup.1 CO--Pro--R.sup.2 --R.sup.3 --OH in which R.sup.1 is hydrogen or lower alkyl, R.sup.2 is an amino acid residue exclusive of prolyl and R.sup.3 is an amino acid residue exclusive of glutamyl are useful for alleviating angiotensin related hypertension.
摘要翻译： R 1为氢或低级烷基的式HSCH2CHR1CO-Pro-R2-R3-OH的化合物，R2为不含脯氨酰基的氨基酸残基，R3为不含谷氨酰基的氨基酸残基，可用于缓解血管紧张素相关的高血压。

14. 发明授权

US4118380A Decapeptide analogs of somatostatin 失效
标题翻译：生长抑素的十肽类似物
公开(公告)号：US4118380A
公开(公告)日：1978-10-03
申请号：US818500
申请日：1977-07-25
申请人： Hans U. Immer , Nedumparambil A. Abraham
发明人： Hans U. Immer , Nedumparambil A. Abraham
IPC分类号： A61K38/00 , C07K5/083 , C07K5/103 , C07K14/655 , C07C103/52
CPC分类号： C07K5/1005 , C07K14/655 , C07K5/0806 , A61K38/00 , Y10S930/16
摘要： Compounds of the formula 1 or 1a ##STR1##HSCH.sub.2 CH.sub.2 CO-A-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-NHCH.sub.2 CH.sub.2 SH (1a)in which A is Gly-Asn or Lys-Gly, or therapeutically acceptable salts thereof are disclosed. The compounds of formulae 1 and 1a are useful for the management of diabetes and the treatment of acromegaly in mammals. Compositions and methods for their use also are disclosed.
摘要翻译：式1或1a的化合物（1）HSCH2CH2CO-A-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-NHCH2CH2SH（1a）其中A是Gly-Asn或Lys-Gly，或公开了其治疗上可接受的盐。式1和1a的化合物可用于治疗糖尿病和哺乳动物肢端肥大症的治疗。其使用的组合物和方法也被公开。

15. 发明授权

US4824937A Synthetic natriuretic peptides 失效
标题翻译：合成利钠肽
公开(公告)号：US4824937A
公开(公告)日：1989-04-25
申请号：US50208
申请日：1987-05-14
申请人： Romano Deghenghi , Hans U. Immer
发明人： Romano Deghenghi , Hans U. Immer
IPC分类号： C07K14/575 , A61K38/00 , A61P9/08 , A61P9/12 , C07K14/00 , C07K14/58 , C07K7/10
CPC分类号： C07K14/582 , A61K38/00
摘要： Synthetic natriuretic peptides (SNP) composed of 23 amino acid residues of which residues 2-23 have the natural L-configuration while the amino-terminal residue is derived from an unnatural amino acid having the D-configuration. The compounds possess diuretic, natriuretic, vasorelaxant, smooth muscle relaxant, hypotensive, and anti-hypertensive activities, and a process for their preparation is also disclosed, together with pharmaceutical preparations thereof and with their use in the practice of medicine. Salts of said synthetic natriuretic peptides with pharmaceutically acceptable acids are also disclosed.
摘要翻译：由23个氨基酸残基组成的合成利钠肽（SNP），其中残基2-23具有天然的L-构型，而氨基末端残基源自具有D-构型的非天然氨基酸。该化合物具有利尿，利尿钠，血管舒张，平滑肌松弛剂，降血压和抗高血压活性，并且还公开了其制备方法及其药物制剂及其在药物实践中的用途。还公开了所述合成利钠肽与药学上可接受的酸的盐。

16. 发明授权

US4213895A N-[N-[N-[ N-[N-(5-Oxo-L-prolyl)-L-histidyl]-L-tryptophyl]-L-seryl]-L-tyrosyl]glycin e azide, an intermediate of the releasing agent of luteinizing hormone (LW) and of follicle stimulating hormone (FSH) 失效
标题翻译： N- [N- [N- [N- [N-（5-氧代-L-脯氨酰基）-L-组氨酰基] -L-色氨酸] -L-丝氨酰] -L-酪氨酰基]甘氨酸叠氮化物促黄体激素（LW）和促卵泡激素（FSH）的释放剂
公开(公告)号：US4213895A
公开(公告)日：1980-07-22
申请号：US23563
申请日：1979-03-26
申请人： Hans U. Immer , Verner R. Nelson , Menfred K. Gotz
发明人： Hans U. Immer , Verner R. Nelson , Menfred K. Gotz
IPC分类号： C07K5/103 , C07K7/23 , C07C103/52 , A61K37/00
CPC分类号： C07K5/1005 , C07K7/23 , Y10S514/80 , Y10S930/13
摘要： N-[N-[N-[N-[N-(5-Oxo-L-prolyl)-L-histidyl]-L-tryptophyl]-L-seryl]-L-tyrosyl]glycine hydrazide trifluoroacetate is converted to N-[N-[N-[N-[N-(5-oxo-L-prolyl)-L-histidyl]-L-tryptophy]-L-seryl]-L-tyrosyl]glycine azide, a useful intermediate for preparing LH and FSH releasing hormone.
摘要翻译： N- [N- [N- [N- [N-（5-氧代-L-脯氨酰基）-L-组氨酰基] -L-色氨酸] -L-丝氨酰] -L-酪蛋白]甘氨酰肼三氟乙酸盐转化为 N- [N- [N- [N- [N-（5-氧代-L-脯氨酰基）-L-组氨酰基] -L-色氨酸] -L-丝氨酰] -L-甲硅烷基]甘氨酸叠氮化物，有用的中间体用于制备LH和FSH释放激素。

17. 发明授权

US4301066A Preparation of (D-Trp .sup.6)-LH-RH via the heptapeptide H-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH.sub.2 失效
标题翻译：通过七肽H-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH 2制备（D-Trp 6）-LH-RH
公开(公告)号：US4301066A
公开(公告)日：1981-11-17
申请号：US147884
申请日：1980-05-08
申请人： Francesco Bellini , Hans U. Immer
发明人： Francesco Bellini , Hans U. Immer
IPC分类号： A61K38/00 , C07K7/23 , C07C103/52
CPC分类号： C07K7/23 , A61K38/00 , Y10S930/13
摘要： Herein is described a process for preparing the decapeptide Pry-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH.sub.2 ([D-Trp.sup.6 ]-LH-RH) by coupling Pyr-His-Trp-NHNH.sub.2 with H-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH.sub.2. [D-Trp.sup.6 ]-LH-RH had been established to be an efficient agent for causing release of lutenizing hormone and follicle-stimulating hormone in mammals.
摘要翻译：本文描述了通过偶联Pyr-His-Trp（[D-Trp6] -LH-RH）制备十肽Pry-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH 2 -NHNH 2与H-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH 2。 [D-Trp6] -LH-RH已被确定为在哺乳动物中引起促黄体激素和促卵泡激素释放的有效药物。

18. 发明授权

US4093610A Process for producing triglycyl-lysine vasopressin and intermediates therefor 失效
标题翻译：制备三甘氨酰赖氨酸加压素及其中间体的方法
公开(公告)号：US4093610A
公开(公告)日：1978-06-06
申请号：US763772
申请日：1977-01-31
申请人： Nedumparambil A. Abraham , Hans U. Immer , Kazimir Sestanj
发明人： Nedumparambil A. Abraham , Hans U. Immer , Kazimir Sestanj
IPC分类号： A61K38/00 , C07K7/16 , C07C103/52 , C07G7/00
CPC分类号： C07K7/16 , A61K38/00 , Y10S930/15
摘要： A new process for preparing the cyclic dodecapeptide triglycyl-lysine vasopressin of the formula ##STR1## which comprises the preparation of a first hexapeptide of formula Boc--Gly--Gly--Gly--Cys(Trt)--Tyr--Phe--NHNH.sub.2 and a second hexapeptide of formula H--Gln(Mbh)--Asn(Mbh)--Cys(Trt)--Pro--Lys(Boc)--Gly--NH.sub.2 by a series of condensations involving the reaction of an appropriately protected peptide unit having an activated carboxyl with an appropriately protected peptide having a free amino group. Subsequently, the first and second hexapeptides are condensed according to the azide coupling method to obtain the linear protected dodecapeptide of formula Boc--Gly--Gly--Gly--Cys(Trt)--Tyr--Phe--Gln(Mbh)--Asn(Mbh)--Cys(Trt)--Pro--Lys(Boc)--Gly--NH.sub.2 ; thereafter the linear protected dodecapeptide is transformed into the desired cyclic dodecapeptide, triglycyllysine vasopressin, by oxidizing and deprotecting processes.
摘要翻译：制备式“IMAGE”的环十二肽三缩水甘油基赖氨酸加压素的新方法，其包括制备式Boc-Gly-Gly-Gly-Cys（Trt）-Tyr-Phe-NHNH 2的第一六肽和第二个六肽通过一系列缩合产生式H-Gln（Mbh）-Asn（Mbh）-Cys（Trt）-Pro-Lys（Boc）-Gly-NH 2）的反应，该缩合涉及适当保护的具有活性羧基的肽单元与适当的具有游离氨基的保护肽。随后，根据叠氮偶合法将第一和第二六肽缩合，得到式Boc-Gly-Gly-Gly-Cys（Trt）-Tyr-Phe-Gln（Mbh）-Asn（Mbh） - Cys（Trt）-Pro-Lys（Bo c）-Gly-NH 2; 此后，通过氧化和脱保护过程将线性保护的十二肽转化成所需的环十二肽，甘氨酰赖氨酸加压素。

19. 发明授权

US4010260A Derivatives of retro-enantio-somatostatin, intermediates therefor, and process therefor 失效
标题翻译：复方生长抑素的衍生物，其中间体及其制备方法
公开(公告)号：US4010260A
公开(公告)日：1977-03-01
申请号：US599448
申请日：1975-07-28
申请人： Hans U. Immer , Nedumparambil A. Abraham , Verner R. Nelson
发明人： Hans U. Immer , Nedumparambil A. Abraham , Verner R. Nelson
IPC分类号： A61K38/00 , C07K14/655 , C07C103/52 , A61K37/00
CPC分类号： C07K14/6555 , A61K38/00 , Y10S514/806 , Y10S930/16
摘要： Compounds of the formula 1 or 1a ##STR1## IN WHICH R is hydrogen or CONHCH.sub.2 CONHCH.sub.2 CH.sub.3 are disclosed. The compounds are obtained by a process which comprises the following step: preparing peptide fragments II, III, V and VII see below, by a series of condensations involving the reaction of an appropriately protected peptide having an activated ester group with an appropriately protected peptide having a free amino group; condensing ##STR2## by means of the azide method with ##STR3## followed by hydrogenolysis of the reaction product to obtain ##STR4## condensing the latter by means of the azide method with ##STR5## followed by treating the resulting compound with hydrazine hydrate to obtain ##STR6## condensing the latter by means of the azide method with ##STR7## in which R is hydrogen or CONHCH.sub.2 CONHCH.sub.2 CH.sub.3 to obtain the linear protected peptide ##STR8## in which R is as defined herein; thereafter said linear peptide is transformed into the desired cyclic peptide of formula 1 by deprotecting and oxidizing processes. In addition, the linear, reduced form of the peptide of formula 1a is obtained by deprotection of the aforementioned linear peptide or by reduction of the cyclic peptide. The peptides of formulae 1 and 1a are useful for the management of diabetes and the treatment of acromegaly. Methods for their use are also disclosed.
摘要翻译：式1或1a的化合物

20. 发明授权

US4244947A Carba decapeptide derivatives of [TYR.sup.6 ]-somatostatin 失效
标题翻译：卡巴十肽衍生物[TYR6] - 促生长素抑制素
公开(公告)号：US4244947A
公开(公告)日：1981-01-13
申请号：US66258
申请日：1979-08-13
申请人： Nedumparampil A. Abraham , Francesco Bellini , Hans U. Immer , Marvin M. Kobric
发明人： Nedumparampil A. Abraham , Francesco Bellini , Hans U. Immer , Marvin M. Kobric
IPC分类号： A61K38/00 , C07K5/11 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号： C07K14/6555 , C07K5/1019 , A61K38/00 , Y10S514/806 , Y10S930/16
摘要： Peptides of formula I ##STR1## in which X is (CH.sub.2).sub.2, S--CH.sub.2 or CH.sub.2 --S or a therapeutically acceptable acid addition salt thereof are disclosed. The peptides of formula I are useful as agents for the treatment of acromegaly and the management of diabetes in a mammal. Compositions and methods for the preparation of the peptides of formula I are also disclosed.
摘要翻译：公开了其中X是（CH 2）2，S-CH 2或CH 2 -S或其治疗上可接受的酸加成盐的式I的肽（I）。式I的肽可用作治疗肢端肥大症和哺乳动物中糖尿病的治疗剂。还公开了制备式I肽的组合物和方法。

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