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1. 发明公开

EP1924275A2 THIO-CONTAINING INHIBITORS OF AMINOPEPTIDASE P, COMPOSITIONS THEREOF AND METHOD OF USE 失效
标题翻译：硫基抑制剂氨肽酶P，THEREOF组合物及其使用方法
公开(公告)号：EP1924275A2
公开(公告)日：2008-05-28
申请号：EP06813820.5
申请日：2006-08-28
申请人： Simmons, William H.
发明人： Simmons, William H.
IPC分类号： A61K38/00
CPC分类号： A61K38/556 , C07K5/0202 , C07K5/0823 , A61K2300/00
摘要： The present invention is directed to a thio-containing compound inhibiting aminopeptidase P (mAPP or APP), whose natural substrate is bradykinin. The compound allows bradykinin to exert its beneficial effects on the cardiovascular system, to improve renal function, and to improve glucose tolerance and insulin-sensitivity. The present invention is also directed to a pharmaceutical composition comprising the mAPP inhibitor of the present invention and a pharmaceutically acceptable carrier. In another aspect, the present invention is directed to a method of inhibiting bradykinin degradation in a mammalian patient, preferably human, in need of treatment comprising administering to the patient a therapeutically effective amount of an a thio-containing compound of the present invention. The method of the present invention also contemplates the further step of administering to the mammalian patient in need of treatment a therapeutically effective amount of an inhibitor of angiotensin converting enzyme (ACE).

2. 发明公开

EP3223613A4 4-FLUORO-THIO-CONTAINING INHIBITORS OF APP2, COMPOSITIONS THEREOF AND METHOD OF USE 有权
公开(公告)号：EP3223613A4
公开(公告)日：2018-07-18
申请号：EP15862635
申请日：2015-10-30
申请人： SIMMONS WILLIAM H
发明人： SIMMONS WILLIAM H
IPC分类号： C07K5/08 , A61K38/00
CPC分类号： C07K5/0823 , A61K38/00 , A61K38/06
摘要： The present invention has multiple aspects. In its first aspect, it is directed to a compound that is a 4(S)-fluoro-thio-tripeptide analog that has the unexpectedly superior property of specifically inhibiting the enzyme, membrane-bound aminopeptidase P2 (APP2), whose natural substrate is bradykinin, but not the enzyme angiotensin converting enzyme (ACE) which also cleaves bradykinin. In its second aspect, the present invention is directed to a pharmaceutical composition comprising the 4(S)-fluoro-thio-tripeptide analog and a pharmaceutically acceptable carrier. In its third aspect, the invention is directed to a method of inhibiting bradykinin degradation in a mammalian patient, comprising administering a therapeutically effective amount of the compound of the invention to a mammalian patient in need of inhibition of bradykinin degradation.

3. 发明授权

EP1924275B1 THIO-CONTAINING INHIBITORS OF AMINOPEPTIDASE P, COMPOSITIONS THEREOF AND METHOD OF USE 失效
标题翻译：硫基抑制剂氨肽酶P，THEREOF组合物及其使用方法
公开(公告)号：EP1924275B1
公开(公告)日：2012-08-08
申请号：EP06813820.5
申请日：2006-08-28
申请人： Simmons, William H.
发明人： Simmons, William H.
IPC分类号： A61K38/00
CPC分类号： A61K38/556 , C07K5/0202 , C07K5/0823 , A61K2300/00
摘要： The present invention is directed to a thio-containing compound inhibiting aminopeptidase P (mAPP or APP), whose natural substrate is bradykinin. The compound allows bradykinin to exert its beneficial effects on the cardiovascular system, to improve renal function, and to improve glucose tolerance and insulin-sensitivity. The present invention is also directed to a pharmaceutical composition comprising the mAPP inhibitor of the present invention and a pharmaceutically acceptable carrier. In another aspect, the present invention is directed to a method of inhibiting bradykinin degradation in a mammalian patient, preferably human, in need of treatment comprising administering to the patient a therapeutically effective amount of an a thio-containing compound of the present invention. The method of the present invention also contemplates the further step of administering to the mammalian patient in need of treatment a therapeutically effective amount of an inhibitor of angiotensin converting enzyme (ACE).

4. 发明公开

EP1924275A4 THIO-CONTAINING INHIBITORS OF AMINOPEPTIDASE P, COMPOSITIONS THEREOF AND METHOD OF USE 失效
标题翻译：硫基抑制剂氨肽酶P，THEREOF组合物及其使用方法
公开(公告)号：EP1924275A4
公开(公告)日：2009-07-29
申请号：EP06813820
申请日：2006-08-28
申请人： SIMMONS WILLIAM H
发明人： SIMMONS WILLIAM H
IPC分类号： A61K38/00
CPC分类号： A61K38/556 , C07K5/0202 , C07K5/0823 , A61K2300/00

5. 发明授权

EP3223613B1 4-FLUORO-THIO-CONTAINING INHIBITORS OF APP2, COMPOSITIONS THEREOF AND METHOD OF USE 有权
公开(公告)号：EP3223613B1
公开(公告)日：2019-09-04
申请号：EP15862635.8
申请日：2015-10-30
申请人： Simmons, William H.
发明人： Simmons, William H.
IPC分类号： C07K5/08 , A61K38/00

6. 发明公开

EP3223613A1 4-FLUORO-THIO-CONTAINING INHIBITORS OF APP2, COMPOSITIONS THEREOF AND METHOD OF USE 有权
标题翻译： APP2的含4-氟取代的抑制剂及其组合物和使用方法
公开(公告)号：EP3223613A1
公开(公告)日：2017-10-04
申请号：EP15862635.8
申请日：2015-10-30
申请人： Simmons, William H.
发明人： Simmons, William H.
IPC分类号： A01N43/38
CPC分类号： C07K5/0823 , A61K38/00 , A61K38/06
摘要： The present invention has multiple aspects. In its first aspect, it is directed to a compound that is a 4(S)-fluoro-thio-tripeptide analog that has the unexpectedly superior property of specifically inhibiting the enzyme, membrane-bound aminopeptidase P2 (APP2), whose natural substrate is bradykinin, but not the enzyme angiotensin converting enzyme (ACE) which also cleaves bradykinin. In its second aspect, the present invention is directed to a pharmaceutical composition comprising the 4(S)-fluoro-thio-tripeptide analog and a pharmaceutically acceptable carrier. In its third aspect, the invention is directed to a method of inhibiting bradykinin degradation in a mammalian patient, comprising administering a therapeutically effective amount of the compound of the invention to a mammalian patient in need of inhibition of bradykinin degradation.
摘要翻译：本发明具有多个方面。在其第一方面，其涉及一种化合物，其是具有意想不到的优异特性的4（S） - 氟 - 硫代 - 三肽类似物，其特异性抑制其天然底物是酶 - 膜结合氨肽酶P2（APP2）缓激肽，而不是血管紧张素转换酶（ACE），它也能分解缓激肽。在其第二方面，本发明涉及包含4（S） - 氟 - 硫 - 三肽类似物和药学上可接受的载体的药物组合物。在其第三方面，本发明涉及一种抑制哺乳动物患者中缓激肽降解的方法，该方法包括给需要抑制缓激肽降解的哺乳动物患者施用治疗有效量的本发明化合物。

7. 发明申请

WO2007032887A2 THIO-CONTAINING INHIBITORS OF AMINOPEPTIDASE P, COMPOSITIONS THEREOF AND METHOD OF USE 审中-公开
标题翻译：氨基磷酸酯P的含THI的抑制剂及其使用方法
公开(公告)号：WO2007032887A2
公开(公告)日：2007-03-22
申请号：PCT/US2006/033398
申请日：2006-08-28
申请人： SIMMONS, William, H.
发明人： SIMMONS, William, H.
IPC分类号： A61K38/05 , C07K5/06
CPC分类号： A61K38/556 , C07K5/0202 , C07K5/0823 , A61K2300/00
摘要： The present invention is directed to an a thio-containing compound that is capable of inhibiting the enzyme, membrane aminopeptidase P (mAPP or APP), whose natural substrate is bradykinin. The compound is useful as a pharmaceutical agent because by inhibiting bradykinin degradation, the compound allows bradykinin to exert its beneficial effects on the cardiovascular system, to improve renal function, and to improve glucose tolerance and insulin-sensitivity. The present invention is also directed to a pharmaceutical composition comprising the mAPP inhibitor of the present invention and a pharmaceutically acceptable carrier. In another aspect, the present invention is directed to a method of inhibiting bradykinin degradation in a mammalian patient, preferably human, in need of treatment comprising administering to the patient a therapeutically effective amount of an a thio-containing compound of the present invention. The method of the present invention also contemplates the further step of administering to the mammalian patient in need of treatment a therapeutically effective amount of an inhibitor of angiotensin converting enzyme (ACE).
摘要翻译：本发明涉及能够抑制其天然底物是缓激肽的酶的氨基肽酶P（mAPP或APP）的含硫化合物。该化合物可用作药剂，因为通过抑制缓激肽降解，该化合物允许缓激肽对心血管系统发挥有益作用，改善肾功能，并改善葡萄糖耐量和胰岛素敏感性。本发明还涉及包含本发明的mAPP抑制剂和药学上可接受的载体的药物组合物。另一方面，本发明涉及在需要治疗的哺乳动物患者，优选人类中抑制缓激肽降解的方法，包括向患者施用治疗有效量的本发明的含硫化合物。本发明的方法还考虑到需要治疗哺乳动物患者治疗有效量的血管紧张素转化酶（ACE）抑制剂的进一步步骤。

8. 发明申请

WO2007032887A3 THIO-CONTAINING INHIBITORS OF AMINOPEPTIDASE P, COMPOSITIONS THEREOF AND METHOD OF USE 审中-公开
标题翻译：氨基磷酸酯P的含THI的抑制剂及其使用方法
公开(公告)号：WO2007032887A3
公开(公告)日：2007-10-04
申请号：PCT/US2006033398
申请日：2006-08-28
申请人： SIMMONS WILLIAM H
发明人： SIMMONS WILLIAM H
IPC分类号： A61K38/00
CPC分类号： A61K38/556 , C07K5/0202 , C07K5/0823 , A61K2300/00
摘要： The present invention is directed to a thio-containing compound inhibiting aminopeptidase P (mAPP or APP), whose natural substrate is bradykinin. The compound allows bradykinin to exert its beneficial effects on the cardiovascular system, to improve renal function, and to improve glucose tolerance and insulin-sensitivity. The present invention is also directed to a pharmaceutical composition comprising the mAPP inhibitor of the present invention and a pharmaceutically acceptable carrier. In another aspect, the present invention is directed to a method of inhibiting bradykinin degradation in a mammalian patient, preferably human, in need of treatment comprising administering to the patient a therapeutically effective amount of an a thio-containing compound of the present invention. The method of the present invention also contemplates the further step of administering to the mammalian patient in need of treatment a therapeutically effective amount of an inhibitor of angiotensin converting enzyme (ACE).
摘要翻译：本发明涉及抑制天然底物为缓激肽的氨基肽酶P（mAPP或APP）的含硫化合物。该化合物允许缓激肽对心血管系统发挥有益作用，改善肾功能，改善葡萄糖耐量和胰岛素敏感性。本发明还涉及包含本发明的mAPP抑制剂和药学上可接受的载体的药物组合物。另一方面，本发明涉及在需要治疗的哺乳动物患者，优选人类中抑制缓激肽降解的方法，包括向患者施用治疗有效量的本发明的含硫化合物。本发明的方法还考虑到需要治疗哺乳动物患者治疗有效量的血管紧张素转化酶（ACE）抑制剂的进一步步骤。

9. 发明申请

WO2016085530A1 4-FLUORO-THIO-CONTAINING INHIBITORS OF APP2, COMPOSITIONS THEREOF AND METHOD OF USE 审中-公开
标题翻译： APP2的含氟化物的含氟化合物的抑制剂及其组合物及其使用方法
公开(公告)号：WO2016085530A1
公开(公告)日：2016-06-02
申请号：PCT/US2015/000122
申请日：2015-10-30
申请人： SIMMONS, William H.
发明人： SIMMONS, William H.
IPC分类号： A01N43/38
CPC分类号： C07K5/0823 , A61K38/00 , A61K38/06
摘要： The present invention has multiple aspects. In its first aspect, it is directed to a compound that is a 4(S)-fluoro-thio-tripeptide analog that has the unexpectedly superior property of specifically inhibiting the enzyme, membrane-bound aminopeptidase P2 (APP2), whose natural substrate is bradykinin, but not the enzyme angiotensin converting enzyme (ACE) which also cleaves bradykinin. In its second aspect, the present invention is directed to a pharmaceutical composition comprising the 4(S)-fluoro-thio-tripeptide analog and a pharmaceutically acceptable carrier. In its third aspect, the invention is directed to a method of inhibiting bradykinin degradation in a mammalian patient, comprising administering a therapeutically effective amount of the compound of the invention to a mammalian patient in need of inhibition of bradykinin degradation.
摘要翻译：本发明具有多个方面。在其第一方面，涉及一种化合物，其是具有特异性抑制酶，膜结合的氨基肽酶P2（APP2）的意想不到的优异性质的4（S） - 氟 - 硫代 - 三肽类似物，其天然底物为缓激肽，而不是还能切割缓激肽的酶血管紧张素转换酶（ACE）。在其第二方面，本发明涉及包含4（S） - 氟 - 硫代 - 三肽类似物和药学上可接受的载体的药物组合物。在其第三方面，本发明涉及一种抑制哺乳动物患者缓激肽降解的方法，包括向需要抑制缓激肽降解的哺乳动物患者施用治疗有效量的本发明化合物。

10. 发明专利

CA2621262A1 THIO-CONTAINING INHIBITORS OF AMINOPEPTIDASE P, COMPOSITIONS THEREOF AND METHOD OF USE 未知
公开(公告)号：CA2621262A1
公开(公告)日：2007-03-22
申请号：CA2621262
申请日：2006-08-28
申请人： SIMMONS WILLIAM H
发明人： SIMMONS WILLIAM H
IPC分类号： A61K38/00
摘要： The present invention is directed to an alpha thio-containing compound that is capable of inhibiting the enzyme, membrane aminopeptidase P (mAPP or APP), whose natural substrate is bradykinin. The compound is useful as a pharmaceutical agent because by inhibiting bradykinin degradation, the compound allows bradykinin to exert its beneficial effects on the cardiovascular system, to improve renal function, and to improve glucose tolerance and insulin-sensitivity. The present invention is also directed to a pharmaceutical composition comprising the mAPP inhibitor of the present invention and a pharmaceutically acceptable carrier. In another aspect, the present invention is directed to a method of inhibiting bradykinin degradation in a mammalian patient, preferably human, in need of treatment comprising administering to the patient a therapeutically effective amount of an alpha thio-containing compound of the present invention. The method of the present invention also contemplates the further step of administering to the mammalian patient in need of treatment a therapeutically effective amount of an inhibitor of angiotensin converting enzyme (ACE).

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