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公开(公告)号:US5374622A
公开(公告)日:1994-12-20
申请号:US10234
申请日:1993-01-28
CPC分类号: C07K14/75 , C07K5/1016
摘要: A fibrinogen receptor antagonist of the formulaAc-Cys-Asn-Pro-(L-AMF)-Gly-Asp-Cys-OHorAc-Cys-Asn-(DiMeTzl)-(L-AMF)-Gly-Asp-Cys-OH.
摘要翻译: 式Ac-Cys-Asn-Pro-(L-AMF)-Gly-Asp-Cys-OH或Ac-Cys-Asn-(DiMeTzl) - (L-AMF)-Gly-Asp-Cys的纤维蛋白原受体拮抗剂 -哦。
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公开(公告)号:US5338723A
公开(公告)日:1994-08-16
申请号:US948331
申请日:1992-09-21
CPC分类号: C07K14/75 , C07K5/1016
摘要: A fibrinogen receptor antagonist of the formula ##STR1## wherein XX represents a synthetic alpha-amino acid containing a linear side chain and ZZ represents a sequence of 1, 2, 3 or 4 amino acids.
摘要翻译: 一种下式的纤维蛋白原受体拮抗剂,其中XX代表含有线性侧链的合成α-氨基酸,ZZ代表1,2,3或4个氨基酸的序列。
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公开(公告)号:US5091366A
公开(公告)日:1992-02-25
申请号:US534001
申请日:1990-06-04
摘要: Analogs of the 17-membered ring portion of ANF wherein the cysteine moiety is replaced with dipeptidyl moieties, specifically, Phe-Pro, NMP-Pro, Pro-Pro, Val-Pro, Lys-Pro, Ile-Pro, Arg-Pro, HAr-Pro, Dly-Pro, Arg-Pro, Lys-BAr, Arg-Pro, CyA-CyA, Cys-Cys, or with .alpha.-aminoheptanoic acid result in analogs of ANF having increased potencies and metabolic stability.
摘要翻译: ANF的17-元环部分的类似物,其中半胱氨酸部分被二肽基部分,特别是Phe-Pro,NMP-Pro,Pro-Pro,Val-Pro,Lys-Pro,Ile-Pro,Arg-Pro, HAr-Pro,Dly-Pro,Arg-Pro,Lys-BAr,Arg-Pro,CyA-CyA,Cys-Cys或α-氨基庚酸导致ANF的类似物具有增加的效力和代谢稳定性。
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公开(公告)号:US5061693A
公开(公告)日:1991-10-29
申请号:US386533
申请日:1989-07-28
申请人: Ruth F. Nutt , Stephen F. Brady , Daniel F. Veber
发明人: Ruth F. Nutt , Stephen F. Brady , Daniel F. Veber
摘要: A fibrinogen receptor antagonist compound of the structure:A--B--C--Gly--Asp--D--E (I)wherein A, B, C, D and E are preferably defined as follows:A is L-asparagine, D-asparagine or acylated asparagineB is an L-or D-isomer of proline, thioproline, .beta.,.beta.-dimethylthioproline, or N-methylalanine;C is arginine;D is phenylalanine, tryptophan .alpha.-naphthylalanine, .beta.-napthlalanine, arginine or lysine; andE is OH.
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公开(公告)号:US5023233A
公开(公告)日:1991-06-11
申请号:US386395
申请日:1989-07-28
申请人: Ruth F. Nutt , Stephen F. Brady , Daniel F. Veber
发明人: Ruth F. Nutt , Stephen F. Brady , Daniel F. Veber
摘要: A fibrinogen receptor antagonist of the formula: ##STR1## wherein A, B, C, D, E, R, R.sup.1 and X-Y are preferably defined as follows:A is acylamido;R and R.sup.1 are H;X-Y is S--S;B is L-asparagine;C is proline or thioproline or .beta., .beta.-dimethylthroprolineD is arginine; andE is COOH.
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公开(公告)号:US5672582A
公开(公告)日:1997-09-30
申请号:US322049
申请日:1994-10-12
申请人: Daniel F. Veber , S. Dale Lewis , Jules A. Shafer , Dong-Mei Feng , Ruth F. Nutt , Stephen F. Brady
发明人: Daniel F. Veber , S. Dale Lewis , Jules A. Shafer , Dong-Mei Feng , Ruth F. Nutt , Stephen F. Brady
IPC分类号: C07D211/36 , A61K31/16 , A61K31/19 , A61K31/215 , A61K31/40 , A61K31/445 , A61K38/00 , A61P7/02 , A61P43/00 , C07C237/10 , C07C271/22 , C07D207/16 , C07D211/60 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/087 , A61K38/05
CPC分类号: C07K5/0812 , C07K5/0202 , C07K5/06078 , C07K5/06191 , A61K38/00
摘要: 4-substituted cyclohexylamine derivatives which are thrombin catalytic site inhibitors and which are useful as anticoagulants. These compounds show selectivity for thrombin over other trypsin-like enzymes and have oral bioavailability. They have the formula ##STR1## for example ##STR2##
摘要翻译: 4-取代的环己胺衍生物,它们是凝血酶催化位点抑制剂,可用作抗凝剂。 这些化合物显示凝血酶比其它胰蛋白酶样酶具有选择性并具有口服生物利用度。 它们具有公式
,例如 -
公开(公告)号:US5204328A
公开(公告)日:1993-04-20
申请号:US789378
申请日:1991-11-05
摘要: Atrial natriuretic factor analogs containing N-alkylated amino acids and showing enhanced potency and increased metabolic stability. These analogs have natriuretic, diuretic and vasorelaxant activity, making them suitable for treating congestive heart failure and renal hypertension.
摘要翻译: 含有N-烷基化氨基酸的心房利钠因子类似物,显示出增强的效力和增加的代谢稳定性。 这些类似物具有利钠,利尿和血管舒张活性,使其适用于治疗充血性心力衰竭和肾性高血压。
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公开(公告)号:US5340798A
公开(公告)日:1994-08-23
申请号:US961221
申请日:1992-10-14
申请人: Ruth F. Nutt , Daniel F. Veber
发明人: Ruth F. Nutt , Daniel F. Veber
CPC分类号: C07D403/14 , C07K5/06026 , A61K38/00
摘要: The present invention comprises fibrinogen receptor antagonist compounds, compositions containing them and methods for using them to inhibit fibrinogen binding to blood platelets. Compounds of the invention have the following formula ##STR1## wherein Z is ##STR2## X is COOH, CH.sub.2 SH or SH; R.sup.1 is Y--R.sup.3, wherein R.sup.3 is alkyl and Y is amino, pyridinyl, pyrimidinyl or piperidinyl;R.sup.2 is H, alkyl, aryl, or arylalkyl; andR.sup.4 is alkyl, heteroalkyl, aryl or heteroaryl, wherein the aryl or heteroaryl group can be mono- or bi-cyclic.An exemplary compound of the invention is ##STR3##
摘要翻译: 本发明包括纤维蛋白原受体拮抗剂化合物,含有它们的组合物和使用它们来抑制纤维蛋白原与血小板结合的方法。 本发明化合物具有下列结构式:其中Z为X,CO为COOH,CH 2 SH或SH; R1是Y-R3,其中R3是烷基,Y是氨基,吡啶基,嘧啶基或哌啶基; R2是H,烷基,芳基或芳基烷基; 并且R 4是烷基,杂烷基,芳基或杂芳基,其中芳基或杂芳基可以是单环或双环的。 本发明的示例性化合物是
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公开(公告)号:US4191754A
公开(公告)日:1980-03-04
申请号:US16218
申请日:1979-02-28
申请人: Daniel F. Veber , Ruth F. Nutt
发明人: Daniel F. Veber , Ruth F. Nutt
IPC分类号: A61K38/00 , C07K14/655 , A61K37/10 , C07C103/52
CPC分类号: C07K14/6555 , A61K38/00 , Y10S514/806 , Y10S930/16
摘要: Bicyclic somatostatin analogs and pharmaceutically acceptable non-toxic acid addition salts thereof are prepared by a combination of the solid phase method and the solution method. These analogs have the property of inhibiting the release of insulin, glucagon and growth hormone in humans and animals. The compounds are particularly useful in the treatment of diabetes. Due to the bicyclic structure, these analogs are resistant to enzymatic metabolism and have a longer duration of activity.
摘要翻译: 双相生长抑素类似物及其药学上可接受的无毒酸加成盐通过固相法和溶液法的组合制备。 这些类似物具有抑制人和动物中胰岛素,胰高血糖素和生长激素释放的性质。 该化合物特别可用于治疗糖尿病。 由于双环结构,这些类似物对酶代谢具有抗性并且具有更长的活性持续时间。
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公开(公告)号:US4161521A
公开(公告)日:1979-07-17
申请号:US695348
申请日:1976-06-14
申请人: Daniel F. Veber , Frederick W. Holly , Robert G. Strachan , William J. Paleveda , Ruth F. Nutt , Ralph F. Hirschmann
发明人: Daniel F. Veber , Frederick W. Holly , Robert G. Strachan , William J. Paleveda , Ruth F. Nutt , Ralph F. Hirschmann
IPC分类号: A61K38/00 , C07K5/103 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号: C07K14/6555 , C07K5/1013 , A61K38/00 , Y10S514/806 , Y10S930/16
摘要: Somatostatin analogs having the structural formula: ##STR1## are prepared by controlled stepwise procedures starting with individual amino acid components. These peptides have the property of lowering blood glucose, inhibiting gastric secretion, inhibiting growth hormone release and inhibiting glucagon release in humans and animals.
摘要翻译: 具有结构式:
+ tr 和 + tr 的生长抑素类似物通过从各个氨基酸组分开始的受控逐步程序制备。 这些肽具有降低血糖,抑制胃分泌,抑制生长激素释放和抑制人和动物中胰高血糖素释放的性质。
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