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98 条记录 (耗时 0.093 秒)

    Carbocyclic nucleoside analogs
    88.
    发明授权
    Carbocyclic nucleoside analogs 失效
    碳环核苷类似物

    公开(公告)号：US5246931A

    公开(公告)日：1993-09-21

    申请号：US694538

    申请日：1991-05-01

    申请人： Daniel W. Norbeck ,  Jacob J. Plattner ,  Terry J. Rosen ,  David L. Garmaise ,  Richard J. Pariza ,  Steven M. Hannick ,  Thomas J. Sowin

    发明人： Daniel W. Norbeck ,  Jacob J. Plattner ,  Terry J. Rosen ,  David L. Garmaise ,  Richard J. Pariza ,  Steven M. Hannick ,  Thomas J. Sowin

    IPC分类号： C07C215/42 ,  C07C271/18 ,  C07C271/20 ,  C07C271/24 ,  C07C275/50 ,  C07D213/69 ,  C07D239/46 ,  C07D239/54 ,  C07D251/16 ,  C07D253/065 ,  C07D471/04 ,  C07D473/00 ,  C07D487/04 ,  C07F7/18 ,  C07F9/6561

    CPC分类号： C07D213/69 ,  C07C215/42 ,  C07C271/18 ,  C07C271/20 ,  C07C271/24 ,  C07C275/50 ,  C07D239/47 ,  C07D239/54 ,  C07D251/16 ,  C07D253/065 ,  C07D471/04 ,  C07D473/00 ,  C07D487/04 ,  C07F7/1856 ,  C07F9/65616 ,  C07C2101/04

    摘要： A compound of the formula: ##STR1## wherein A is a purin-9-yl group, a heterocyclic isostere of a purin-9-yl group, a pyrimidin-1-yl group or a heterocyclic isostere of a pyrimidin-1-yl group; E is hydrogen, --CH.sub.2 OH or --OH; and G and D are independently selected from hydrogen, C.sub.1 to C.sub.10 alkyl, --OH, --CH.sub.2 OH, --CH.sub.2 OR.sub.20 wherein R.sub.20 is C.sub.1 to C.sub.6 alkyl, --CH.sub.2 OC(O)R.sub.21 wherein R.sub.21 is C.sub.1 to C.sub.10 alkyl, --CH.sub.2 OC(O)CH(R.sub.22)(NHR.sub.23) wherein R.sub.22 is the side chain of any of the naturally occurring amino acids and R.sub.23 is hydrogen or --C(O)CH(R.sub.24)(NH.sub.2) wherein a R.sub.24 is the side chain of any of the naturally occurring amino acids, --CH.sub.2 SH, --CH.sub.2 Cl, --CH.sub.2 F, --CH.sub.2 Br, --CH.sub.2 I, --C(O)H, --CH.sub.2 CN, --CH.sub.2 N.sub.3, --CH.sub.2 NR.sub.1 R.sub.2, --CO.sub.2 R.sub.1, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 OR.sub.20 wherein R.sub.20 is as defined above, --CH.sub.2 CH.sub.2 OC(O)R.sub.21 wherein R.sub.21 is as defined above, --CH.sub.2 CH.sub.2 OC(O)CH(R.sub.22)(NHR.sub.23) wherein R.sub.22 and R.sub.23 are as defined above, --CH.sub.2 CH.sub.2 PO.sub.3 H.sub.2, --CH.sub.2 OPO.sub.3 H.sub.2, --OCH.sub.2 PO.sub.3 H.sub.2 and --CH.sub.2 CO.sub.2 R.sub.3 wherein R.sub.1 and R.sub.2 are independently selected from hydrogen and C.sub.1 to C.sub.10 alkyl and R.sub.3 is hydrogen, C.sub.1 to C.sub.10 alkyl, carboxyalkyl or aminoalkyl; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 下式的化合物：其中A是嘌呤-9-基，嘌呤-9-基的杂环等价基，嘧啶-1-基或嘧啶-1-基的杂环等价基 组; E是氢，-CH 2 OH或-OH; 并且G和D独立地选自氢，C1-C10烷基，-OH，-CH2OH，-CH2OR20，其中R20是C1-C6烷基，-CH2OC（O）R21，其中R21是C1-C10烷基，-CH2OC（O） CH（R22）（NHR23）其中R22是任何天然存在的氨基酸的侧链，R 23是氢或-C（O）CH（R 24）（NH 2），其中R 24是任何天然存在的氨基酸的侧链 发生的氨基酸，-CH 2 SH，-CH 2 Cl，-CH 2 F，-CH 2 Br，-CH 2 I，-C（O）H，-CH 2 CN，-CH 2 N 3，-CH 2 NR 1 R 2，-CO 2 R 1，-CH 2 CH 2 OH，-CH 2 CH 2 OR 20，其中R 20如上定义， -CH 2 CH 2 OC（O）R 21，其中R 21如上定义，-CH 2 CH 2 OC（O）CH（R 22）（NHR 23）其中R 22和R 23如上定义，-CH 2 CH 2 PO 3 H 2，-CH 2 OPO 3 H 2，-OCH 2 PO 3 H 2和-CH 2 CO 2 R 3，其中R 1和R 2是 独立地选自氢和C1至C10烷基，R3是氢，C1至C10烷基，羧基烷基或氨基烷基; 或其药学上可接受的盐。

    Peptidylaminodiols
    89.
    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

    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 ,  C07D233/54 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/078 ,  C07K5/08 ,  C07K5/083 ,  C07K5/097

    CPC分类号： 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

    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 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.

    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，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
    90.
    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

    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 ,  C07D233/54 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/078 ,  C07K5/08 ,  C07K5/083 ,  C07K5/097

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

    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-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.

    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。