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1. 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。

2. 发明授权

US5093233A Antagonists with position 13 modification 失效
标题翻译：具有13位修饰的拮抗剂
公开(公告)号：US5093233A
公开(公告)日：1992-03-03
申请号：US514394
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 , C07K14/635
CPC分类号： C07K14/635 , A61K38/00
摘要： The present invention relates to the use of peptide hormone analogues as inhibitors of their respective naturally occurring peptide hormone. The structure of the peptide hormone analogues is exemplified by parathyroid hormone (PTH), wherein Lys.sup.13 is substituted to increase the biological activity of the PTH analogues. Thus, there are disclosed peptides having the formulae:PTH(7-34)NH.sub.2 ;[Tyr.sup.34 ]PTH(7-34)NH.sub.2 ;[D-Trp.sup.12, Tyr.sup.34 ]PTH(7-34)NH.sub.2 ;[Nle.sup.8,18, D-Trp.sup.12, Tyr.sup.34 ]PTH(7-34)NH.sub.2 ;[Nle.sup.8,18, Tyr.sup.34 ]PTH(7-34)NH.sub.2 ;desamino[Nle.sup.8,18, D-Trp.sup.12, Tyr.sup.34 ]PTH(7-34)NH.sub.2 ; and,desamino[Nle.sup.8,18, D-Trp.sup.12, Tyr.sup.34 ]PTH(8-34)NH.sub.2wherein Lys.sup.13 is modified in the epsilon-amino acid group by N,N-diisobutyl or 3-phenylpropanoyl.
摘要翻译：本发明涉及肽激素类似物作为其各自天然存在的肽激素的抑制剂的用途。肽激素类似物的结构以甲状旁腺激素（PTH）为例，其中Lys13被取代以增加PTH类似物的生物学活性。因此，公开了具有下式的肽：PTH（7-34）NH 2; [Tyr34] PTH（7-34）NH2; [D-Trp12，Tyr34] PTH（7-34）NH2; [Nle8,18，D-Trp12，Tyr34] PTH（7-34）NH2; [Nle8,18，Tyr34] PTH（7-34）NH2; 脱氨基[Nle8,18，D-Trp12，Tyr34] PTH（7-34）NH 2; 和脱氨基[Nle8,18，D-Trp12，Tyr34] PTH（8-34）NH2，其中Lys13在ε-氨基酸基团中被N，N-二异丁基或3-苯基丙酰基修饰。

3. 发明授权

US5087561A Humoral hypercalcemic factor antagonists modified at position 13 by biotin 失效
标题翻译：通过生物素在13位修饰的体液高钙因子拮抗剂
公开(公告)号：US5087561A
公开(公告)日：1992-02-11
申请号：US545256
申请日：1990-06-28
申请人： Michael Rosenblatt , Michael Chorev , Eliahu Roubini , Ruth F. Nutt , Le T. Duong
发明人： Michael Rosenblatt , Michael Chorev , Eliahu Roubini , Ruth F. Nutt , Le T. Duong
IPC分类号： C07K14/575 , G01N33/74
CPC分类号： C07K14/575 , G01N33/74 , 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 or Lys.sup.11 is modified on the epsilon-amino group by biotin 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或Lys11通过生物素在ε-氨基上被修饰，从而产生可抑制HCF作用的HCF类似物。

4. 发明授权

US4771124A Parathyroid hormone antagonists with simplified synthetic methodology 失效
标题翻译：具有简化合成方法的甲状旁腺激素拮抗剂
公开(公告)号：US4771124A
公开(公告)日：1988-09-13
申请号：US54359
申请日：1987-05-26
申请人： Michael Rosenblatt , Lynn H. Caporale , Ruth F. Nutt , Jay J. Levy , Michael Chorev
发明人： Michael Rosenblatt , Lynn H. Caporale , Ruth F. Nutt , Jay J. Levy , Michael Chorev
IPC分类号： G01N33/53 , A61K38/00 , A61K38/22 , A61P3/00 , A61P9/12 , A61P19/10 , A61P37/00 , A61P43/00 , C07K1/00 , C07K14/00 , C07K14/575 , C07K14/635 , G01N33/566 , G01N33/74 , C07K7/10
CPC分类号： C07K14/635 , A61K38/00
摘要： The present invention relates to the use of peptide hormone analogues as inhibitors of their respective naturally occurring peptide hormone and methods of synthesis of such analogues. The structure of the peptide hormone analogues is exemplified by parathyroid hormone wherein Trp.sup.23 is substituted by L-Phe or other hydrophobic amino acids such as Leu, Nle, Val, Tyr, beta-napthylalanine and alpha-napthylalanine.

5. 发明授权

US5114843A Humoral hypercalcemic factor antagonists 失效
标题翻译：体液高钙血症因子拮抗剂
公开(公告)号：US5114843A
公开(公告)日：1992-05-19
申请号：US662340
申请日：1991-02-25
申请人： Michael Rosenblatt , Roberta L. McKee , Michael P. Caulfield , Ruth F. Nutt
发明人： Michael Rosenblatt , Roberta L. McKee , Michael P. Caulfield , Ruth F. Nutt
IPC分类号： A61K38/00 , C07K14/635
CPC分类号： C07K14/635 , A61K38/00
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 analogues is exemplified by an internal region of the N-terminus of humoral hypercalcemic factor hHCF, and truncations thereof: hHCF(14-34)NH.sub.2, hHCF(13-34)NH.sub.2, hHCF(12-34)NH.sub.2, hHCF(11-23)NH.sub.2, hHCF(10-34)NH.sub.2, hHCF(9-34)NH.sub.2, hHCF(8-34)NH.sub.2 and various amino acid substitutions.
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。肽类似物的结构的例子是体液高钙血症因子hHCF的N末端的内部区域及其截短：hHCF（14-34）NH2，hHCF（13-34）NH2，hHCF（12-34）NH2 ，hHCF（11-23）NH2，hHCF（10-34）NH2，hHCF（9-34）NH2，hHCF（8-34）NH2和各种氨基酸取代。

6. 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。

7. 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。

8. 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。

9. 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。

10. 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。

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