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1. 发明授权

US4020157A Shortened analogs of somatostatin 失效
标题翻译：缩短生长抑素类似物
公开(公告)号：US4020157A
公开(公告)日：1977-04-26
申请号：US594159
申请日：1975-07-08
申请人： Nedumparambil A. Abraham , Hans U. Immer , Verner R. Nelson , Kazimir Sestanj
发明人： Nedumparambil A. Abraham , 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##HSCH.sub.2 CH(R)CO--Lys--Asn--Phe--Phe--Trp--Lys--Thr--Phe--Thr--Ser--NHCH.sub.2 CH.sub.2 SH (1a)In which R is hydrogen or NHR.sup.1 in which R.sup.1 is lower aliphatic acyl containing from 1 - 6 carbon atoms or benzoyl, 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 in mammals. Methods for their use also are disclosed.
摘要翻译：式1或1a的化合物CO-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-NHCH2CH2SH（1a）IN其中R是氢或NHR1，其中R1 是含有1-6个碳原子的低级脂族酰基或苯甲酰基，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哺乳动物肢端肥大症的治疗。其使用方法也被公开。

2. 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

3. 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。

4. 发明授权

US4159980A 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：US4159980A
公开(公告)日：1979-07-03
申请号：US456343
申请日：1974-03-29
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 , C07C103/52
CPC分类号： C07K5/0821 , 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 comprises the following steps: Condensing N-(5-oxo-L-prolyl)-L-histidine hydrazide by means of the azide method with L-tryptophan benzyl ester and treating the resulting compound with hydrazine hydrate to obtain N-[N-(5-oxo-L-prolyl)-L-histidyl]-L-tryptophan hydrazide (II); treating N-[O-benzyl-N-carboxy-L-tyrosyl]glycine N-benzyl ester with ethyl chloroformate to obtain the corresponding mixed anhydride which is reacted with t-butyl carbazate to obtain the corresponding 2-carboxyhydrazide t-butyl ester which is hydrogenolyzed to N-L-tyrosylglycine 2-carboxyhydrazide t-butyl ester, and condensing the latter with N-carboxy-L-seryl N-benzyl ester 2,4-dinitrophenyl ester followed by hydrogenolysis of the reaction product to obtain N-(N-L-seryl-L-tyrosyl)glycine 2-carboxyhydrazide t-butyl ester (III); condensing N-carboxy-L-proline N-benzyl ester with glycine ethyl ester in the presence of dicyclohexylcarbodiimide, treating the resulting product with ammonia and then hydrogenolyzing, to obtain 2-[(L-prolyl)amino]acetamide, which is condensed with N-carboxy-N.sup.G -nitro-L-arginine N-t-butyl ester in the presence of dicyclohexylcarbodiimide and N-hydroxysuccinimide to obtain N-[N-(N-carboxy-N.sup.G -nitro-L-arginyl)-L-prolyl)]glycinamide N-t-butyl ester (IV); or alternatively condensing L-proline methyl ester with N-carboxy-N.sup.G -nitro-arginine N-t-butyl ester in the presence of dicyclohexylcarbodiimide, condensing the resulting product with glycine ethyl ester in the presence of dicyclohexylcarbodiimide, and treating the resulting product with ammonia to obtain the same compound IV as above; treating said compound IV with acid and then with N-carboxy-L-leucine N-benzyl ester 2,4,5-trichlorophenyl ester and hydrogenolyzing the resulting product in acetic acid, to obtain N-[N-[N-(N-L-leucyl)-L-arginyl]-L-prolyl]-glycinamide diacetate (V); condensing compound II with compound III by means of the azide method to obtain the hexapeptide N-[N-[N-[N-[N-(5-oxo-L-prolyl)-L-histidyl]-L-tryptophyl]-L-seryl]-L-tyrosyl]glycine 2-carboxyhydrazide t-butyl ester, or condensing N-[N-(5-oxo-L-prolyl)-L-histidyl]-L-tryptophan with compound III in the presence of dicyclohexylcarbodiimide to obtain the same hexapeptide as above, and deprotecting and converting the latter to its trifluoroacetate salt (VI); and condensing compound V with compound VI by means of the azide method, to obtain the decapeptide of formula I which is isolated as the diacetate salt and optionally converted to other pharmaceutically acceptable salts.

5. 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。

6. 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。

7. 发明授权

US4000122A Novel hydrazinocarboxamide derivatives and preparation thereof 失效
标题翻译：新型氢氯氰菊酯衍生物及其制备方法
公开(公告)号：US4000122A
公开(公告)日：1976-12-28
申请号：US565332
申请日：1975-04-07
申请人： Amedeo Failli , Verner R. Nelson , Hans U. Immer , Manfred K. Gotz
发明人： Amedeo Failli , Verner R. Nelson , Hans U. Immer , Manfred K. Gotz
IPC分类号： C07D207/40 , C07K5/04 , C07C103/52 , A61K37/00
CPC分类号： C07C243/00 , C07D207/40
摘要： .alpha.-Hydrazinocarboxamide and .alpha.-(.alpha.'-acylhydrazino)-carboxamide derivatives of formula I ##STR1## in which R.sup.1 and R.sup.2 each are lower alkyl or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are joined form a piperidino or morpholino radical; R.sup.3 is hydrogen, lower alkanoyl, benzoyl, p-nitrobenzoyl, p-aminobenzoyl, p-chlorobenzoyl, isocyanoacetyl, or protected amino acyl radicals, for example, N-formylglycyl or ##STR2## (N-carbobenzoxyglycylglycyl); R.sup.4 is lower alkyl, CHR.sup.7 COOR.sup.8 or CH.sub.2 CH.sub.2 COOR.sup.8 wherein R.sup.7 is hydrogen or phenyl and R.sup.8 is hydrogen or lower alkyl; R.sup.5 is hydrogen or lower alkyl; or R.sup.4 and R.sup.5 together with the carbon atom to which they are joined form a cyclohexylidene radical; and R.sup.6 is a cyclohexyl or CHR.sup.9 COY wherein R.sup.9 is hydrogen or benzyl and Y is hydroxyl, lower alkoxy or amine, with the provisos that when Y is hydroxyl then R.sup.8 is hydrogen, that when Y is lower alkoxy than R.sup.8 is lower alkyl and that when Y is amino R.sup.4 is lower alkyl, are disclosed herein along with the related .alpha.-hydrazino-carboxamide and .alpha.-(.alpha.'-acylhydrazino)carboxamide compounds of formula III ##STR3## in which R.sup.1, R.sup.2, R.sup.3 , R.sup.5 and R.sup.7 are as defind above and Y is lower alkoxy. These compounds possess antibacterial activity. Methods for their preparation and use are disclosed also.

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