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1. 发明授权

US4743585A Renin inhibitors 失效
标题翻译：肾素抑制剂
公开(公告)号：US4743585A
公开(公告)日：1988-05-10
申请号：US920330
申请日：1986-11-21
申请人： James P. Hudspeth , James S. Kaltenbronn , Elizabeth A. Lunney , Joseph T. Repine , W. Howard Roark , Michael A. Stier , Francis J. Tinney , Peter W. K. Woo , Ernest D. Nicolaides
发明人： James P. Hudspeth , James S. Kaltenbronn , Elizabeth A. Lunney , Joseph T. Repine , W. Howard Roark , Michael A. Stier , Francis J. Tinney , Peter W. K. Woo , Ernest D. Nicolaides
IPC分类号： C07K5/02 , A61K37/02 , C07K5/08 , C07K5/10 , C07K7/06
CPC分类号： C07K5/0227 , C07K5/0205 , C07K5/0207 , Y10S530/86 , Y10S930/27
摘要： The invention concerns novel renin-inhibitory peptides which are useful for treating renin associated hypertension and for treating hyperaldosteronism. Novel intermediates, processes for preparing both the intermediates and the novel peptides, pharmaceutical compositions, and methods of treatment are included.
摘要翻译：本发明涉及可用于治疗肾素相关性高血压和治疗醛固酮增多症的新型肾素抑制肽。包括新的中间体，制备中间体和新型肽的方法，药物组合物和治疗方法。

2. 发明授权

US4863905A Renin inhibitors II 失效
标题翻译：肾素抑制剂二
公开(公告)号：US4863905A
公开(公告)日：1989-09-05
申请号：US11990
申请日：1987-02-04
申请人： James P. Hudspeth , James S. Kaltenbronn , Joseph T. Repine , Peter W. K. Woo
发明人： James P. Hudspeth , James S. Kaltenbronn , Joseph T. Repine , Peter W. K. Woo
IPC分类号： C07K5/02
CPC分类号： C07K5/0227 , C07K5/0207 , Y10S530/86
摘要： The invention concerns novel renin-inhibiting peptides which are modified as isosteres. These peptides are useful for treating renin-associated hypertension and hyperaldosteronism. Processes for preparing the peptides, compositions containing them and methods for using them are included. Also included is a diagnostic test using the peptides to determine the presence of renin-associated hypertension or hyperaldosteronism.
摘要翻译：本发明涉及被修饰为等位基因的新型肾素抑制肽。这些肽可用于治疗肾素相关性高血压和醛固酮增多症。包括肽的制备方法，含有它们的组合物和使用它们的方法。还包括使用肽来确定肾素相关性高血压或醛固酮增多症的存在的诊断测试。

3. 发明授权

US4278681A Antibacterial amide compounds and means for using the same 失效
标题翻译：抗菌酰胺化合物及其使用方法
公开(公告)号：US4278681A
公开(公告)日：1981-07-14
申请号：US112657
申请日：1980-01-31
申请人： Theodore H. Haskell , Marland P. Hutt, Jr. , Ernest D. Nicolaides , Peter W. K. Woo , Gin G. Huang
发明人： Theodore H. Haskell , Marland P. Hutt, Jr. , Ernest D. Nicolaides , Peter W. K. Woo , Gin G. Huang
IPC分类号： C07D207/16 , C07D207/28 , C07D213/80 , C07D213/85 , C07D499/00 , C07D499/64 , C07F7/10 , A61K31/455 , C07D499/68
CPC分类号： C07D213/80 , C07D207/16 , C07D207/28 , C07D213/85 , C07D499/00 , C07F7/10
摘要： Novel organic amide compounds which are N-[6-[(acylaminoacylamino or aminoacylamino)phenyl]-1,2-dihydro-2-oxonicotinyl] penicillin compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding N-6-[(acylaminoacylamino or aminoacylamino)-phenyl]-1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-aminopenicillanic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[6-[(acylaminoacylamino or aminoacylamino) phenyl]-1,2-dihydro-2-oxonicotinyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.
摘要翻译：通过以下方法提供了具有广谱抗菌效用的N- [6 - [（酰氨基酰氨基或氨基酰氨基）苯基] -1,2-二氢-2-氧代烟碱基]青霉素化合物的新型有机酰胺化合物：（a）使游离氨基酸适当的青霉素或其酸盐或甲硅烷基化衍生物或其配合物与相应的N-6 - [（酰氨基酰基氨基或氨基酰氨基） - 苯基] -1,2-二氢-2-氧代烟酸的反应性衍生物或（b）氨基酸6-氨基青霉烷酸或相关化合物或其酸式盐或甲硅烷基化衍生物与相应的DN- [6 - [（酰氨基酰基氨基或氨酰基氨基）苯基] -1,2-二氢-2-氧代烟酰基] - 2-取代甘氨酸。还公开了含有所述化合物的药物组合物和使用所述组合物治疗感染的方法。

4. 发明授权

US4997842A Metabolites of pirmenol 失效
标题翻译：哌醇的代谢物
公开(公告)号：US4997842A
公开(公告)日：1991-03-05
申请号：US476868
申请日：1990-02-08
申请人： Timothy R. Hurley , Dino A. Sherwood , Peter W. K. Woo , Karl-Otto Vollmer , Egmont Schaller , Wolfgang Klemisch , Albrecht V. Hodenberg
发明人： Timothy R. Hurley , Dino A. Sherwood , Peter W. K. Woo , Karl-Otto Vollmer , Egmont Schaller , Wolfgang Klemisch , Albrecht V. Hodenberg
IPC分类号： C07D401/06
CPC分类号： C07D401/06
摘要： The present invention relates to the + or - pirmenol stereoisomers and to selected metabolites of pirmenol or (+,-)-cis-.alpha.-[3-(2,6-dimethyl-1-piperidinyl))propyl]-.alpha.-phenyl-2-pyridinemethanol which are active as antiarrhythmic agents. The pharmacological use of the metabolites that is the present invention is as antiarrhythmic agents. Pharmaceutical compositions comprising the metabolites are also within the scope of the invention.
摘要翻译：本发明涉及戊醇或（+， - ） - 顺式-α-[3-（2,6-二甲基-1-哌啶基））丙基]-α-苯基 - 2-吡啶甲醇，其作为抗心律失常剂是有活性的。作为本发明的代谢物的药理学应用是抗心律失常药。包含代谢物的药物组合物也在本发明的范围内。

5. 发明授权

US4145529A Production of 3'-deoxybutirosina A 失效
标题翻译：生产3 {40-脱氧胆碱A
公开(公告)号：US4145529A
公开(公告)日：1979-03-20
申请号：US600677
申请日：1975-07-31
申请人： Peter W. K. Woo , Theodore H. Haskell
发明人： Peter W. K. Woo , Theodore H. Haskell
IPC分类号： C07H15/23 , A61K31/71 , C07H15/22
CPC分类号： C07H15/23
摘要： O-2,6-Diamino-2,3,6-trideoxy-.alpha.-D-ribo-hexopyranosyl-(1.fwdarw.4)-O-�.beta.-D-xylofuranosyl-(1.fwdarw.5)!-N.sup.1 -�(S)-4-amino-2-hydroxy-1-oxobutyl!-2-deoxystreptamine, also known as 3'-deoxybutirosin A and acid addition salts of said compound. These compounds exhibit a wide spectrum of antibacterial activity. The above compounds are produced by the reduction of a tetra-N-protected-3'-arylthio-3'-deoxybutirosin A compound having the formula: ##STR1##
摘要翻译： O-2,6-二氨基-2,3,6-三脱氧-α-D-核糖 - 六吡喃糖基 - （1-> 4）-O- [β--D-木糖呋喃糖基 - （1-> 5）] -N1- [（S）-4-氨基-2-羟基-1-氧代丁基] -2-脱氧链霉素，也称为3'-脱氧胆红素A和所述化合物的酸加成盐。这些化合物表现出广泛的抗菌活性。

6. 发明授权

US3960837A Polyamine compounds and methods for their production 失效
标题翻译：多胺化合物及其生产方法
公开(公告)号：US3960837A
公开(公告)日：1976-06-01
申请号：US503991
申请日：1974-09-06
申请人： Peter W. K. Woo
发明人： Peter W. K. Woo
IPC分类号： B01J23/00 , B01J25/00 , C07B61/00 , C07H15/23 , C07H5/06 , C07H15/22
CPC分类号： C07H15/23
摘要： O-2,6-Diamino-2,3,4,6-tetradeoxy-.alpha.-D-erythro-hexopyranosyl-(1.fwdarw.4)-O-[5-amino-5-deoxy-.beta.-D-xylofuranosyl-(1.fwdarw.5)]-N.sup.1 -[(S)-4-amino-2-hydroxy-1-oxobutyl]-2-deoxystreptamine, also known as aminotrideoxybutirosin A, and acid-addition salts. They have a wide spectrum of antibacterial activity.The above compounds can be produced from aminodeoxybutirosin A by the sequence of reactions which comprises protecting the five primary amino groups by converting them to arylmethoxycarbonyl derivatives, converting the 3',4'-hydroxyl groups to an acetal, acylating the remaining four hydroxyl groups, and hydrolyzing the acetal to produce a key intermediate which is an O-2,6-dideoxy-2,6-bis[[(arylmethoxy)carbonyl]amino]-.alpha.-D-glucopyranosyl-(1.fwdarw.4)-O-[2,3-di-O-acyl-5-deoxy-5-[[(arylmethoxy)carbonyl]amino]-.beta.-D-xylofuranosyl-(1.fwdarw.5)]-6-O-acyl-N.sup.1 -[(S)-2-acyloxy-1-oxo-4-[[(arylmethoxy)carbonyl]amino]-butyl]-2-deoxy-N.sup.3 -[(arylmethoxy)carbonyl]streptamine, generically also identified as protected 5"-aminodeoxybutirosin A. That compound is reacted with methanesulfonyl chloride in pyridine to introduce 3',4'-methanesulfonyloxy groups which are removed by reaction with zinc and sodium iodide to introduce a double bond at the 3',4' position. The acyl groups are hydrolyzed or cleaved as by reaction with ammonia in methanol and the product is reacted with hydrogen in the presence of a catalyst to remove the arylmethoxycarbonyl groups and hydrogenate the double bond with the formation of aminotrideoxybutirosin A.
摘要翻译： O-2,6-二氨基-2,3,4,6-四脱氧-α-D-赤式 - 六吡喃糖基 - （1-> 4）-O- [5-氨基-5-脱氧-β--D-木糖呋喃糖基 - （1-> 5）] - N1 - [（S）-4-氨基-2-羟基-1-氧代丁基] -2-脱氧链霉素，也称为氨基歧羟基丁硫氨酸A和酸加成盐。它们具有广谱的抗菌活性。

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