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1. 发明授权

US07381736B2 Thiazole and thiadiazole inhibitors of tyrosine phosphatases 失效
标题翻译：噻唑和噻二唑抑制剂酪氨酸磷酸酶
公开(公告)号：US07381736B2
公开(公告)日：2008-06-03
申请号：US11219402
申请日：2005-09-02
申请人： Zacharia S. Cheruvallath , Colin J. Loweth , Ruth F. Nutt , Darryl Rideout , Joseph E. Semple , Jing Wang , Feiyue Wu , Shankari Mylvaganam , Hengyi Zhu , Jianzhong Sun
发明人： Zacharia S. Cheruvallath , Colin J. Loweth , Ruth F. Nutt , Darryl Rideout , Joseph E. Semple , Jing Wang , Feiyue Wu , Shankari Mylvaganam , Hengyi Zhu , Jianzhong Sun
IPC分类号： A61K31/427 , C07D277/18
CPC分类号： C07D277/38 , C07D277/42 , C07D285/135 , C07D417/12 , C07D417/14 , C07F9/6539 , C07F9/65395
摘要： Compounds and compositions are provided for modulating the activity of protein tyrosine phosphatases. In one embodiment, the compounds and compositions are thiazoles and thiadiazoles that inhibit the activity of protein tyrosine phosphatase 1B.
摘要翻译：提供化合物和组合物用于调节蛋白酪氨酸磷酸酶的活性。在一个实施方案中，化合物和组合物是抑制蛋白酪氨酸磷酸酶1B活性的噻唑和噻二唑。

2. 发明授权

US5681844A Methionine sulfone and s-substituted cysteine sulfone derivatives as enzyme inhibitors 失效
标题翻译：甲硫氨酸砜和s取代的半胱氨酸砜衍生物作为酶抑制剂
公开(公告)号：US5681844A
公开(公告)日：1997-10-28
申请号：US234811
申请日：1994-04-28
申请人： Matthew M. Abelman , Robert J. Ardecky , Ruth F. Nutt
发明人： Matthew M. Abelman , Robert J. Ardecky , Ruth F. Nutt
IPC分类号： A61K38/00 , A61P7/02 , C07K5/06 , C07K5/062 , C07K5/072 , C07K5/078 , A61K31/40 , C07D207/06
CPC分类号： C07K5/0606 , A61K38/00
摘要： This invention relates to compounds which inhibit thrombin or factor Xa. The compounds contain an aldehyde functionality and a methionine sulfone or S-substituted cysteine sulfone residue. The compounds and their pharmaceutical compositions are useful for preventing thrombosis in mammals which are suspected of having a condition characterized by abnormal thrombosis.
摘要翻译：本发明涉及抑制凝血酶或因子Xa的化合物。该化合物含有醛官能团和甲硫氨酸砜或S-取代的半胱氨酸砜残基。化合物及其药物组合物可用于预防怀疑具有以异常血栓形成为特征的病症的哺乳动物的血栓形成。

3. 发明授权

US5087562A Humoral hypercalcemic factor antagonists with modification at position 13 . . . 失效
标题翻译：在13位修饰的体液高钙血症因子拮抗剂。。。
公开(公告)号：US5087562A
公开(公告)日：1992-02-11
申请号：US514633
申请日：1990-04-25
申请人： Michael Rosenblatt , Eliahu Roubini , Michael Chorev , Ruth F. Nutt
发明人： Michael Rosenblatt , Eliahu Roubini , Michael Chorev , Ruth F. Nutt
IPC分类号： A61K38/00 , C07K14/575 , G01N33/574
CPC分类号： G01N33/574 , C07K14/575 , A61K38/00 , Y10S930/29
摘要： The present invention relates to the use of peptide analogues as inhibitors of their respective naturally occurring peptides. The structure of the peptide hormone analogues is exemplified by human humoral hypercalcemic factor (hHCF), wherein Lys.sup.13 is modified so as to produce HCF analogues which can inhibit the action of HCF.
摘要翻译：本发明涉及肽类似物作为其各自天然存在的肽的抑制剂的用途。肽激素类似物的结构以人体液高钙血症因子（hHCF）为例，其中Lys13被修饰以产生可抑制HCF作用的HCF类似物。

4. 发明授权

US4703034A Novel cyclic tetrapeptide 失效
标题翻译：新型环状四肽
公开(公告)号：US4703034A
公开(公告)日：1987-10-27
申请号：US856252
申请日：1986-04-28
申请人： Roger Freidinger , Ruth F. Nutt , Terry A. Lyle , Richard Saperstein
发明人： Roger Freidinger , Ruth F. Nutt , Terry A. Lyle , Richard Saperstein
IPC分类号： C07K5/02 , C07K5/12 , A61K37/02 , C07K7/26
CPC分类号： C07K5/0207 , C07K5/126 , Y10S514/806 , Y10S930/16 , Y10S930/27
摘要： There is disclosed a series of novel cyclic tetrapeptides related to somatostatin. The compounds have surprisingly been found to have the activity of increasing blood glucose when administered. The compounds are prepared using the solid phase or mixed anhydride synthesis methods and compositions and methods utilizing the novel compounds are also disclosed.
摘要翻译：公开了一系列与生长抑素相关的新型环状四肽。惊奇地发现化合物在施用时具有增加血糖的活性。使用固相或混合酸酐合成方法制备化合物，并且还公开了利用新化合物的组合物和方法。

5. 发明授权

US6008351A Aromatic hetherocyclic derivatives as enzyme inhibitors 失效
标题翻译：芳香族杂环衍生物作为酶抑制剂
公开(公告)号：US6008351A
公开(公告)日：1999-12-28
申请号：US573775
申请日：1995-12-18
申请人： Susan Yoshiko Tamura , Joseph Edward Semple , William Charles Ripka , Robert John Ardecky , Yu Ge , Stephen H. Carpenter , Terence K. Brunck , Marguerita S. L. Lim-Wilby , Ruth F. Nutt , Matthew M. Abelman
发明人： Susan Yoshiko Tamura , Joseph Edward Semple , William Charles Ripka , Robert John Ardecky , Yu Ge , Stephen H. Carpenter , Terence K. Brunck , Marguerita S. L. Lim-Wilby , Ruth F. Nutt , Matthew M. Abelman
IPC分类号： A61K31/44 , A61K31/495 , A61K31/505 , A61K38/00 , A61P7/02 , A61P43/00 , C07C257/18 , C07C279/24 , C07C279/34 , C07C281/06 , C07C311/54 , C07C327/48 , C07D211/56 , C07D211/76 , C07D213/75 , C07D213/76 , C07D239/46 , C07D239/47 , C07D239/52 , C07D239/54 , C07D239/545 , C07D401/12 , C07F7/18 , C07K5/06 , C07K5/078 , C07D239/02
CPC分类号： C07K5/06191 , C07D211/56 , C07D211/76 , C07D213/75 , C07D239/47 , C07D239/545 , C07D401/12 , C07K5/06139 , A61K38/00
摘要： The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
摘要翻译：本发明公开了肽醛，其是凝血酶的有效和特异性抑制剂，其药学上可接受的盐，药学上可接受的组合物，以及将其用作以异常血栓形成为特征的哺乳动物的疾病状态的治疗剂。

6. 发明授权

US5714499A 3-amino-2-oxo-1-piperidineacetic derivatives containing an arginine mimic as enzyme inhibitors 失效
标题翻译：含有作为酶抑制剂的精氨酸模拟物的3-氨基-2-氧代-1-哌啶乙酸衍生物
公开(公告)号：US5714499A
公开(公告)日：1998-02-03
申请号：US261498
申请日：1994-06-17
申请人： Joseph E. Semple , Odile E. Levy , Ruth F. Nutt , William C. Ripka
发明人： Joseph E. Semple , Odile E. Levy , Ruth F. Nutt , William C. Ripka
IPC分类号： A61K38/00 , C07K5/078 , A61K31/445 , C07D401/12
CPC分类号： C07K5/06139 , A61K38/00
摘要： The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
摘要翻译：本发明公开了肽醛，其是凝血酶的有效和特异性抑制剂，其药学上可接受的盐，药学上可接受的组合物，以及将其用作以异常血栓形成为特征的哺乳动物的疾病状态的治疗剂。

7. 发明授权

US5700905A Synthetic somatostatin mimics 失效
标题翻译：合成生长抑素模拟物
公开(公告)号：US5700905A
公开(公告)日：1997-12-23
申请号：US338890
申请日：1994-11-14
申请人： Ralph F. Hirschmann , Rolando A. Spanevello , Ruth F. Nutt
发明人： Ralph F. Hirschmann , Rolando A. Spanevello , Ruth F. Nutt
IPC分类号： A61K38/00 , C07K7/64 , C07K14/655 , A61K38/12 , A61K38/31
CPC分类号： C07K14/655 , C07K7/64 , A61K38/00 , Y02P20/55 , Y10S930/16
摘要： Relatively small cyclic peptides that mimic the biological and/or chemical activity of larger cyclic peptide such as somatostatin, as well as synthetic methods therefor. In certain embodiments, cyclic peptides of the invention have structure: ##STR1## wherein R.sub.NP1 is H, an amine protecting group, or a solid support and R.sub.NP2 is H or an amine protecting group.
摘要翻译：相对较小的环肽，其模拟较大环肽如生长抑素的生物和/或化学活性，以及其合成方法。在某些实施方案中，本发明的环肽具有以下结构：其中RNP1为H，胺保护基团或固体载体，RNP2为H或胺保护基团。

8. 发明授权

US5091366A Peptides having ANF activity 失效
标题翻译：具有ANF活性的肽
公开(公告)号：US5091366A
公开(公告)日：1992-02-25
申请号：US534001
申请日：1990-06-04
申请人： Ruth F. Nutt , Terrence M. Ciccarone , Stephen F. Brady , Daniel F. Veber
发明人： Ruth F. Nutt , Terrence M. Ciccarone , Stephen F. Brady , Daniel F. Veber
IPC分类号： A61K38/00 , C07K14/58
CPC分类号： C07K14/58 , A61K38/00
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。

9. 发明授权

US4816443A Piptides having ANF activity 失效
标题翻译：具有ANF活性的鱼类
公开(公告)号：US4816443A
公开(公告)日：1989-03-28
申请号：US51980
申请日：1987-05-19
申请人： Stephen F. Brady , Ruth F. Nutt
发明人： Stephen F. Brady , Ruth F. Nutt
IPC分类号： A61K38/00 , A61P7/10 , A61P9/00 , A61P9/12 , C07K7/08 , C07K14/00 , C07K14/575 , C07K14/58 , A61K37/02 , C07K7/10
CPC分类号： C07K14/58 , A61K38/00
摘要： Novel peptides having potent natriuretic activity are disclosed with the following amino acid sequence: ##STR1## wherein Z is H, acetyl, Boc or Ser-Leu, E is Phe, NMP, OMT, ChA, F is Gly or DAl, G is Ala or Gly, H is Arg or DAr, Pro, Lys or Dly, I is Ile, Met, MeO, MO.sub.2, Leu, Nle, or Val, J is Aib, .alpha.MG or .alpha.MA, K is Arg or Lys, L is Ile or Val, M is Aib, Gly, Ala or DAl, N is Ala, NMA, Pro, Phe or NMP, O is Gln, DGl, Ala or DAl, P is Ser, His, Arg or Lys, Q is Gly, Pro, Ala or Dal, R is Leu, Phe or ChA, S is Gly, Ala or Dal, Arg or DAr, T is Asn DAs, Ala or Dal, U is Ser, DSe, Ala or DAl, V is Phe, DPh, Ala or DAl, Y is -OH or -NH.sub.2 and n is 0 or 1. Also included are the lower alkyl esters and the physiologically acceptable metal salts and acid addition salts of the foregoing peptides. Unless indicated otherwise all optically active amino acids have the L-configuration.

10. 发明授权

US4612366A Cyclic hexapeptide somatostatin analogs 失效
标题翻译：循环六肽生长抑素类似物
公开(公告)号：US4612366A
公开(公告)日：1986-09-16
申请号：US745459
申请日：1985-06-17
申请人： Ruth F. Nutt
发明人： Ruth F. Nutt
IPC分类号： C07K7/64 , A61K38/00 , A61K38/22 , A61P5/00 , C07K1/113 , C07K14/575 , C07K14/655 , C07K7/26 , A61K37/24
CPC分类号： C07K14/6555 , A61K38/00 , Y10S514/806 , Y10S930/16
摘要： Somatostatin analogs are prepared wherein a cyclic hexapeptide contains a secondary amino acid which replaces seven of the ring amino acids of somatostatin. The cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These cyclic hexapeptides are prepared by the solid phase method and/or solution synthesis.
摘要翻译：制备生长抑素类似物，其中环状六肽含有替代生长抑素的七个环氨基酸的仲氨基酸。环状六肽更容易合成，具有较长的活性持续时间，并且许多具有比生长抑素更高的活性水平。该化合物具有抑制胰高血糖素，生长激素和胰岛素释放的性质。某些化合物还能够抑制胃酸分泌物的释放。该化合物特别可用于治疗肢端肥大症，糖尿病，糖尿病性视网膜病变和消化性溃疡。这些环状六肽通过固相法和/或溶液合成制备。

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