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1. 发明授权

US09212206B1 4-Fluoro-Thio-containing inhibitors of APP2, compositions thereof and method of use 有权
标题翻译： APP2的含有4-氟-Thio的抑制剂，其组合物和使用方法
公开(公告)号：US09212206B1
公开(公告)日：2015-12-15
申请号：US14544096
申请日：2014-11-24
申请人： William H Simmons
发明人： William H Simmons
IPC分类号： A61K38/06 , C07K5/097 , 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.
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。

2. 发明授权

US5656603A Aminopeptidase P inhibitors and uses thereof 失效
标题翻译：氨肽酶P抑制剂及其用途
公开(公告)号：US5656603A
公开(公告)日：1997-08-12
申请号：US455281
申请日：1995-05-31
申请人： William H. Simmons
发明人： William H. Simmons
IPC分类号： A61K38/00 , C07K5/02 , C07K5/097 , A61K38/06 , C07K5/00 , C07K7/00 , C07K16/00
CPC分类号： C07K5/0821 , C07K5/0202 , A61K38/00
摘要： The present invention is directed to a compound of the formula: ##STR1## or a pharmaceutically acceptable addition salt thereof, wherein C.sup.3 and C.sup.2 in combination have the configuration S,R or R,S;wherein Y is straight or branched chain lower alkyl having 1 to 6 carbon atoms, straight or branched chain lower alkenyl or alkynyl having 2-6 carbon atoms, cyclic alkyl or alkenyl having 5 or 6 carbon atoms, or benzyl; andwherein X is an amino acid or an oligopeptide having from 1 to 8 amino acid residues, the first amino acid residue at the N-terminus of X being a natural or a synthetic L-amino acid having a radius of gyration of less than 1.54 .ANG., X also having a carboxyl or a carboxyamide moiety at its carboxy terminus. The present invention is further directed to a pharmaceutical composition and to a method of inhibiting bradykinin degradation in a patient using the above-described compound.
摘要翻译：本发明涉及下式的化合物或其药学上可接受的加成盐，其中C3和C2的组合具有结构S，R或R，S; 其中Y是具有1-6个碳原子的直链或支链低级烷基，具有2-6个碳原子的直链或支链低级烯基或炔基，具有5或6个碳原子的环状烷基或链烯基，或苄基; 并且其中X是具有1至8个氨基酸残基的氨基酸或寡肽，X的N末端的第一个氨基酸残基是具有小于1.54的回转半径的天然或合成的L-氨基酸 ANGSTROM，X在其羧基末端也具有羧基或羧酰胺部分。本发明还涉及使用上述化合物的药物组合物和抑制患者缓激肽降解的方法。

3. 发明授权

US3393564A Sight level gauge clearing apparatus 失效
标题翻译：视距仪清除装置
公开(公告)号：US3393564A
公开(公告)日：1968-07-23
申请号：US59147366
申请日：1966-11-02
申请人： WILLIAM H SIMMONS
发明人： SIMMONS THOMAS R
IPC分类号： F04D13/16 , G01F23/02
CPC分类号： F04D13/16 , G01F23/02

4. 发明授权

US1212144A Stock-feeding machine. 失效
标题翻译：送料机
公开(公告)号：US1212144A
公开(公告)日：1917-01-09
申请号：US1914856304
申请日：1914-08-11
申请人： WILLIAM H SIMMONS
发明人： MEYER ALFRED F
CPC分类号： B02C4/42 , Y10S241/603

5. 发明授权

US07390789B2 Thio-containing inhibitors of aminopeptidase P, and compositions thereof 有权
标题翻译：氨基肽酶P的含Thio的抑制剂及其组合物
公开(公告)号：US07390789B2
公开(公告)日：2008-06-24
申请号：US11225748
申请日：2005-09-13
申请人： William H Simmons
发明人： William H Simmons
IPC分类号： A61K38/06
CPC分类号： A61K38/556 , C07K5/0202 , C07K5/0823 , A61K2300/00
摘要： The present invention is directed to an α 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 α 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）的能够抑制酶的α硫代化合物。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α硫代化合物。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。

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