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    Peptidylaminodiols
    12.
    发明授权
    Peptidylaminodiols 失效
    肽基氨基二醇

    公开(公告)号：US5214129A

    公开(公告)日：1993-05-25

    申请号：US793773

    申请日：1991-11-18

    Applicant: Jay R. Luly ,  Jacob J. Plattner ,  Dale J. Kempf

    Inventor： Jay R. Luly ,  Jacob J. Plattner ,  Dale J. Kempf

    IPC: A61K38/00 ,  C07D233/54 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/078 ,  C07K5/08 ,  C07K5/083 ,  C07K5/097

    CPC classification number: C07D233/64 ,  C07K5/0202 ,  C07K5/0227 ,  C07K5/06026 ,  C07K5/06043 ,  C07K5/0606 ,  C07K5/06078 ,  C07K5/0802 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/0821 ,  C07K5/0823 ,  A61K38/00

    Abstract: 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 loweralkyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl, loweralkenyl, 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.

    Abstract translation: 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，硫代苯氧基 或anilino; 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，低级烯基，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。

    Peptidylaminodiols
    14.
    发明授权
    Peptidylaminodiols 失效
    肽基氨基二醇

    公开(公告)号：US4845079A

    公开(公告)日：1989-07-04

    申请号：US217106

    申请日：1988-07-11

    Applicant: Jay R. Luly ,  Jacob J. Plattner ,  Dale J. Kempf

    Inventor： Jay R. Luly ,  Jacob J. Plattner ,  Dale J. Kempf

    IPC: A61K38/00 ,  C07D233/54 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/078 ,  C07K5/08 ,  C07K5/083 ,  C07K5/097

    CPC classification number: C07D233/64 ,  C07K5/0227 ,  C07K5/06026 ,  C07K5/06043 ,  C07K5/0606 ,  C07K5/06078 ,  C07K5/0802 ,  C07K5/0808 ,  C07K5/0823 ,  A61K38/00 ,  Y10S530/86

    Abstract: 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-napththyl)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, loweralkenyl, 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.

    Abstract translation: 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-萘乙基）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， 或anilino; 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，低级烯基，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。

    Anti-infective agents
    18.
    发明授权
    Anti-infective agents 有权
    抗感染剂

    公开(公告)号：US07951800B2

    公开(公告)日：2011-05-31

    申请号：US12613607

    申请日：2009-11-06

    Applicant: Rolf Wagner ,  Pamela L. Donner ,  Dale J. Kempf ,  Clarence J. Maring ,  Vincent S. Stoll

    Inventor： Rolf Wagner ,  Pamela L. Donner ,  Dale J. Kempf ,  Clarence J. Maring ,  Vincent S. Stoll

    IPC: C07D498/02 ,  C07D417/04 ,  A61K31/549

    CPC classification number: C07D495/04

    Abstract: The present invention provides HCV polymerase inhibiting compounds having the formula (I): where R1 is cyclobutyl-N(Ra)—, n is 1, 2, 3 or 4, and at least one R5 is RaSO2N(Rj)alkyl-. In a non-limiting example, a compound of the present invention is N-[(3-{1-[(cyclobutyl)amino]-4-hydroxy-2-oxo-1,2-dihydro-quinolin-3-yl}-1,1-dioxo-1,4-dihydro-1λ6-thieno[2,3-e][1,2,4]thiadiazin-7-yl)methyl]methanesulfonamide. The present invention also features compositions comprising the compounds of the present invention or pharmaceutically acceptable salts, stereoisomers or tautomers thereof, and methods of using the same to treat or prevent HCV infection.

    Abstract translation: 本发明提供了具有式（I）的HCV聚合酶抑制化合物：其中R1是环丁基-N（Ra） - ，n是1,2,3或4，并且至少一个R5是RaSO2N（Rj）烷基 - 。 在非限制性实例中，本发明的化合物是N - [（3- {1 - [（环丁基）氨基] -4-羟基-2-氧代-1,2-二氢 - 喹啉-3-基} -1,1-二氧代-1,4-二氢-1λ6-噻吩并[2,3-e] [1,2,4]噻二嗪-7-基）甲基]甲磺酰胺。 本发明还特征在于包含本发明化合物或其药学上可接受的盐，立体异构体或互变异构体的组合物及其用于治疗或预防HCV感染的方法。

    ANTI-VIRAL COMPOUNDS
    19.
    发明申请
    ANTI-VIRAL COMPOUNDS 有权
    反虚构化合物

    公开(公告)号：US20100168384A1

    公开(公告)日：2010-07-01

    申请号：US12495299

    申请日：2009-06-30

    Applicant: Keith F. McDaniel ,  Dale J. Kempf

    Inventor： Keith F. McDaniel ,  Dale J. Kempf

    IPC: C07K5/10

    CPC classification number: C07K5/0804 ,  C07K5/0802

    Abstract: Compounds capable of inhibiting replication of the hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.

    Abstract translation: 描述了能够抑制丙型肝炎病毒（“HCV”）复制的化合物。 本发明还涉及制备这些化合物的方法，包含这些化合物的组合物，以及使用这些化合物治疗HCV感染的方法。

    Anti-Infective Agents
    20.
    发明申请
    Anti-Infective Agents 有权
    抗感染剂

    公开(公告)号：US20100120753A1

    公开(公告)日：2010-05-13

    申请号：US12613607

    申请日：2009-11-06

    Applicant: Rolf Wagner ,  Pamela L. Donner ,  Dale J. Kempf ,  Clarence J. Maring ,  Vincent S. Stoll

    Inventor： Rolf Wagner ,  Pamela L. Donner ,  Dale J. Kempf ,  Clarence J. Maring ,  Vincent S. Stoll

    IPC: A61K31/54 ,  C07D285/20 ,  A61P31/12

    CPC classification number: C07D495/04

    Abstract: The present invention provides HCV polymerase inhibiting compounds having the formula (I): where R1 is cyclobutyl-N(Ra)—, n is 1, 2, 3 or 4, and at least one R5 is RaSO2N(Rj)alkyl-. In a non-limiting example, a compound of the present invention is N-[(3-{1-[(cyclobutyl)amino]-4-hydroxy-2-oxo-1,2-dihydro-quinolin-3-yl}-1,1-dioxo-1,4-dihydro-1λ6-thieno[2,3-e][1,2,4]thiadiazin-7-yl)methyl]methane-sulfonamide. The present invention also features compositions comprising the compounds of the present invention or pharmaceutically acceptable salts, stereoisomers or tautomers thereof, and methods of using the same to treat or prevent HCV infection.

    Abstract translation: 本发明提供了具有式（I）的HCV聚合酶抑制化合物：其中R1是环丁基-N（Ra） - ，n是1,2,3或4，并且至少一个R5是RaSO2N（Rj）烷基 - 。 在非限制性实例中，本发明的化合物是N - [（3- {1 - [（环丁基）氨基] -4-羟基-2-氧代-1,2-二氢 - 喹啉-3-基} -1,1-二氧代-1,4-二氢-1λ6-噻吩并[2,3-e] [1,2,4]噻二嗪-7-基）甲基]甲磺酰胺。 本发明还特征在于包含本发明化合物或其药学上可接受的盐，立体异构体或互变异构体的组合物及其用于治疗或预防HCV感染的方法。

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