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73. 发明授权

US5091575A Peptidylaminodiols 失效
标题翻译：肽基氨基二醇
公开(公告)号：US5091575A
公开(公告)日：1992-02-25
申请号：US713644
申请日：1991-06-10
申请人： Jay R. Luly , Jacob J. Plattner , Dale J. Kempf
发明人： Jay R. Luly , Jacob J. Plattner , Dale J. Kempf
IPC分类号： A61K38/00 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/078
CPC分类号： C07K5/0227 , C07K5/06043 , C07K5/06078 , C07K5/06139 , A61K38/00
摘要： A renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is C.dbd.O or CHOH; U is CH.sub.2 or NR.sup.2, provided that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, .alpha.,.alpha.-dimethylbenzyl, 1-benzyloxyethyl; phenethyl, phenoxy, thiophenoxy or anilino; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is loweralkyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl; lowerakenyl, benzyl or heterocyclic ring substituted methyl; R.sub.4 is loweralkyl, cycloalkylmethyl or benzyl; R.sub.5 is vinyl, formyl, hydroxymethyl or hydrogen; R.sub.7 is hydrogen or loweralkyl; R.sub.8 and R.sub.9 are independently selected from OH and NH.sub.2 ; and R.sub.6 is hydrogen, loweralkyl, vinyl or arylalkyl; provided that when R.sub.5 and R.sub.7 are both hydrogen and R.sub.8 and R.sub.9 are OH, the carbon bearing R.sub.5 is of the "R" configuration and the carbon bearing R.sub.6 is of the "S" configuration; or pharmaceutically acceptable salts or esters thereof. Also disclosed are renin inhibiting compositions, a method of treating hypertension, methods of making the renin inhibiting compounds and intermediates useful in making the renin inhibiting compounds.
摘要翻译：下式的肾素抑制化合物：其中A是取代基; W是C = O或CHOH; U是CH 2或NR 2，条件是当W是CHOH时，U是CH 2; R1是低级烷基，环烷基甲基，苄基，4-甲氧基苄基，卤代苄基，（1-萘基）甲基，（2-萘基）甲基，（4-咪唑基）甲基，α，α-二甲基苄基，1-苄氧基乙基; 苯乙基，苯氧基，硫代苯氧基或苯胺基; R2是氢或低级烷基; R3是低级烷基，[（烷氧基）烷氧基]烷基，（硫代烷氧基）烷基; 苄基或杂环取代的甲基; R4是低级烷基，环烷基甲基或苄基; R5是乙烯基，甲酰基，羟甲基或氢; R7是氢或低级烷基; R8和R9独立地选自OH和NH2; 和R6是氢，低级烷基，乙烯基或芳基烷基; 条件是当R 5和R 7均为氢且R 8和R 9为OH时，碳原子的R 5为“R”构型，碳原子的R 6为“S”构型; 或其药学上可接受的盐或酯。还公开了肾素抑制组合物，治疗高血压的方法，制备肾素抑制化合物的方法和可用于制备肾素抑制化合物的中间体。

74. 发明授权

US5032577A Peptidylaminodiols 失效
标题翻译：肽基氨基二醇
公开(公告)号：US5032577A
公开(公告)日：1991-07-16
申请号：US132356
申请日：1987-12-18
申请人： Anthony K. L. Fung , Dale J. Kempf , Jay R. Luly , Saul H. Rosenberg , Jacob J. Plattner
发明人： Anthony K. L. Fung , Dale J. Kempf , Jay R. Luly , Saul H. Rosenberg , Jacob J. Plattner
IPC分类号： C12N9/99 , A61K31/165 , A61K31/44 , A61K31/4406 , A61K38/00 , A61P9/12 , C07C67/00 , C07C235/06 , C07C235/08 , C07C235/10 , C07C235/34 , C07C235/74 , C07C235/78 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/20 , C07C237/22 , C07C239/00 , C07C271/20 , C07C271/24 , C07C313/00 , C07C317/44 , C07C323/60 , C07C325/00 , C07C327/20 , C07C333/02 , C07D213/00 , C07D213/71 , C07D213/78 , C07D233/54 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/08 , C07K5/083 , C07K5/097 , C07K14/81
CPC分类号： C07D233/64 , C07K5/0202 , C07K5/0227 , C07K5/06026 , C07K5/06078 , C07K5/0802 , C07K5/0806 , C07K5/0808 , C07K5/0821 , C07K5/0823 , A61K38/00
摘要： A renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is C.dbd.O or CHOH; U is CH.sub.2 or NR.sub.2, provided that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, (alpha,alpha)-dimethylbenzyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is loweralkenyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl, lowerakenyl, benzyl or heterocyclic ring substituted methyl; R.sub.4 is loweralkyl, cycloalkylmethyl or benzyl; R.sub.5 is vinyl, formyl, hydroxymethyl or hydrogen; R.sub.7 is hydrogen or loweralkyl; R.sub.8 and R.sub.9 are independently selected from OH and NH.sub.2 ; and R.sub.6 is hydrogen, loweralkyl, vinyl or arylalkyl; provided that when R.sub.5 and R.sub.7 are both hydrogen and R.sub.8 and R.sub.9 are OH, the carbon bearing R.sub.5 is of the "R" configuration and the carbon bearing R.sub.6 is of the "S" configuration, or pharmaceutically acceptable salts or esters thereof. Also disclosed are renin inhibiting compositions, a method of treating hypertension, methods of making the renin inhibiting compounds and intermediates useful in making the renin inhibiting compounds.
摘要翻译：下式的肾素抑制化合物：其中A是取代基; W是C = O或CHOH; U是CH 2或NR 2，条件是当W是CHOH时，U是CH 2; （1-萘基）甲基，（2-萘基）甲基，（4-咪唑基）甲基，（α，α） - 二甲基苄基，1-苄氧基乙基，苯乙基，苯氧基，噻吩氧基或苯胺基; R2是氢或低级烷基; R3是低级烯基，[（烷氧基）烷氧基]烷基，（硫代烷氧基）烷基，低级，苄基或杂环取代的甲基; R4是低级烷基，环烷基甲基或苄基; R5是乙烯基，甲酰基，羟甲基或氢; R7是氢或低级烷基; R8和R9独立地选自OH和NH2; 和R6是氢，低级烷基，乙烯基或芳基烷基; 条件是当R 5和R 7均为氢且R 8和R 9为OH时，含碳的R 5为“R”构型，并且含碳的R 6为“S”构型，或其药学上可接受的盐或酯。还公开了肾素抑制组合物，治疗高血压的方法，制备肾素抑制化合物的方法和可用于制备肾素抑制化合物的中间体。

75. 发明授权

US4994477A Heterocyclic renin inhibitors 失效
标题翻译：杂环肾素抑制剂
公开(公告)号：US4994477A
公开(公告)日：1991-02-19
申请号：US173382
申请日：1988-03-24
申请人： Dale J. Kempf , Saul H. Rosenberg , Jacob J. Plattner , Hing L. Shan , Biswanath De
发明人： Dale J. Kempf , Saul H. Rosenberg , Jacob J. Plattner , Hing L. Shan , Biswanath De
IPC分类号： A61K38/00 , C07D233/54 , C07D405/12 , C07D417/12 , C07K5/02 , C07K5/078
CPC分类号： C07D233/64 , C07D405/12 , C07D417/12 , C07K5/0207 , C07K5/06139 , A61K38/00
摘要： A renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; R.sub.1 is loweralkyl, loweralkenyl, alkoxyalkyl, [(alkoxy)alkoxy]alkyl, alkoxycarbonylalkyl, carboxyalkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; R.sub.2 is hydrogen, loweralkyl, cycloalkylmethyl or benzyl; D is a substituent; or pharmaceutically acceptable salts or esters thereof.Also disclosed are renin inhibiting compositions, a method of treating hypertension, methods of making the renin inhibiting compounds and intermediates useful in making the renin inhibiting compounds.
摘要翻译：下式的肾素抑制化合物：其中A是取代基; R1是低级烷基，低级烯基，烷氧基烷基，[（烷氧基）烷氧基]烷基，烷氧基羰基烷基，羧基烷基，（硫代烷氧基）烷基，苄基或杂环取代的甲基; R2是氢，低级烷基，环烷基甲基或苄基; D是取代基; 或其药学上可接受的盐或酯。还公开了肾素抑制组合物，治疗高血压的方法，制备肾素抑制化合物的方法和可用于制备肾素抑制化合物的中间体。

76. 发明申请

US20110091423A1 COMPOSITIONS AND METHODS OF USE OF RITONAVIR FOR TREATING HCV 有权
标题翻译：用于治疗HCV的RITONAVIR的组合物和方法
公开(公告)号：US20110091423A1
公开(公告)日：2011-04-21
申请号：US12958899
申请日：2010-12-02
申请人： Dale J. Kempf , Kennan C. Marsh
发明人： Dale J. Kempf , Kennan C. Marsh
IPC分类号： A61K38/21 , A61K31/497 , A61K31/403 , A61K31/427 , A61K31/7056 , A61P31/14
CPC分类号： A61K38/212 , A61K31/407 , A61K31/4965 , A61K31/497 , A61K31/7056 , A61K2300/00
摘要： The present invention discloses compositions and a method of improving the pharmacokinetics of pharmaceutical agents (or pharmaceutically acceptable salts, esters, and prodrugs thereof) which are metabolized by cytochrome P450 monoxygenase comprising coadministering ritonavir or a pharmaceutically acceptable salt, ester, and prodrug thereof.
摘要翻译：本发明公开了通过包含联合利托那韦或其药学上可接受的盐，酯和前药的细胞色素P450单加氧酶代谢的药物（或其药学上可接受的盐，酯和前体药物）的药代动力学的组合物和方法。

77. 发明申请

US20100280248A1 NOVEL COMPOUNDS THAT ARE USEFUL FOR IMPROVING PHARMACOKINETICS 有权
标题翻译：可用于改善药物动力学的新型化合物
公开(公告)号：US20100280248A1
公开(公告)日：2010-11-04
申请号：US12834315
申请日：2010-07-12
申请人： Dale J. Kempf
发明人： Dale J. Kempf
IPC分类号： C07D215/02 , C07D277/20 , C07D261/02 , C07D213/04 , C07D233/54 , C07D207/30
CPC分类号： C07D277/30 , A61K31/426 , A61K31/427 , A61K45/06 , C07C53/18 , C07D213/30 , C07D231/12 , C07D233/64 , C07D263/32 , C07D277/24 , C07D277/38 , C07D277/587 , C07D333/16 , C07D417/04
摘要： Novel compounds of formula 1 or a pharmaceutically acceptable salt thereof inhibit cytochrome P450 monooxygenase.
摘要翻译：新的式1化合物或其药学上可接受的盐抑制细胞色素P450单加氧酶。

78. 发明授权

US07320961B2 Method for treating a disease, disorder or adverse effect caused by an elevated serum concentration of an UGT1A1 substrate 有权
标题翻译：用于治疗由UGT1A1底物升高的血清浓度引起的疾病，障碍或不良反应的方法
公开(公告)号：US07320961B2
公开(公告)日：2008-01-22
申请号：US10802829
申请日：2004-03-18
申请人： Dale J. Kempf , Richard J. Bertz , Jeffrey F. Waring
发明人： Dale J. Kempf , Richard J. Bertz , Jeffrey F. Waring
IPC分类号： A61K31/425 , A61K38/00
CPC分类号： A61K31/436 , A61K31/167 , A61K31/282 , A61K31/427 , A61K31/4418 , A61K31/496 , A61K31/506 , A61K31/565 , A61K31/7048 , A61K31/7068 , A61K31/708
摘要： The present invention is directed to a method for inducing UGT1A1 isoform expression for treatment of a disease, disorder or adverse effect caused by an elevated serum concentration of an UGT1A1 substrate comprising the step of administering to a subject an effective amount of ritonavir. In particular, the present invention is directed to a method of treating unconjugated hyperbilirubinemia by UGT1A1 induction comprising the step of administering to a subject an effective amount of ritonavir.
摘要翻译：本发明涉及一种用于诱导UGT1A1同种型表达的方法，用于治疗由UGT1A1底物升高的血清浓度引起的疾病，障碍或不良反应，包括向受试者施用有效量的利托那韦的步骤。特别地，本发明涉及一种通过UGT1A1诱导处理未结合的高胆红素血症的方法，其包括向受试者施用有效量的利托那韦的步骤。

80. 发明授权

US6037157A Method for improving pharmacokinetics 失效
公开(公告)号：US6037157A
公开(公告)日：2000-03-14
申请号：US687774
申请日：1996-06-26
申请人： Daniel W. Norbeck , Dale J. Kempf , John M. Leonard , Richard J. Bertz
发明人： Daniel W. Norbeck , Dale J. Kempf , John M. Leonard , Richard J. Bertz
IPC分类号： C07D243/04 , A61K31/335 , A61K31/336 , A61K31/337 , A61K31/34 , A61K31/341 , A61K31/395 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/453 , A61K31/47 , A61K31/472 , A61K31/498 , A61K31/535 , A61K31/5375 , A61K31/55 , A61K31/7048 , A61K38/05 , A61K38/06 , A61K38/55 , A61P31/12 , A61P31/18 , C07D217/22 , C07D277/24 , C07D277/28 , C07D295/08 , C07D295/18 , C07D303/46 , C07D307/20 , C07D401/14 , C07D417/12 , C08F2/34 , C12N9/99
CPC分类号： A61K31/453 , A61K31/337 , A61K31/341 , A61K31/395 , A61K31/426 , A61K31/44 , A61K31/498 , A61K31/7048 , A61K38/05 , A61K38/06 , A61K38/55
摘要： A method is disclosed for improving the pharmacokinetics of a drug which is metabolized by cytochrome P450 monooxygenase.

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