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    • 3. 发明授权
    • Ethynyl-alanine aryl/alkylsulfonyl-terminated amino-diol compounds for
treatment of hypertension
    • 用于治疗高血压的乙炔基 - 丙氨酸芳基/烷基磺酰基封端的氨基二醇化合物
    • US5314920A
    • 1994-05-24
    • US916447
    • 1992-07-20
    • Barbara B. ChenGunnar J. HansonJohn S. Baran
    • Barbara B. ChenGunnar J. HansonJohn S. Baran
    • C07C317/44A61K31/16
    • C07C317/44C07C2101/02C07C2101/14
    • Compounds characterized generally as ethynyl alanine aryl/alkylsulfonyl-terminated amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein R.sup.1 is selected from isopropyl, isobutyl, sec-butyl, tert-butyl, phenyl, fluorophenyl, chlorophenyl, benzyl, fluorobenzyl, chlorobenzyl, naphthyl, fluoronaphthyl, chloronaphthyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is propargyl or a propargyl-containing moeity; wherein R.sup.7 is cyclohexylmethyl; and wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl.
    • 通常表示乙炔基丙氨酸芳基/烷基磺酰基封端的氨基二醇衍生物的化合物可用作治疗高血压的肾素抑制剂。 特别感兴趣的化合物是下式的化合物,其中R 1选自异丙基,异丁基,仲丁基,叔丁基,苯基,氟苯基,氯苯基,苄基,氟苄基,氯苄基,萘基,氟萘基,氯萘基,氟萘基甲基和氯萘基甲基 ; 其中R2选自氢,甲基,乙基和苯基; 其中R 3选自氢,环己基甲基,苄基,氟苄基,氯苄基,氟萘基甲基和氯萘基甲基; 其中R5是炔丙基或含炔丙基的摩尔; 其中R 7为环己基甲基; 并且其中R8选自正丙基,异丁基,环丙基,环丙基甲基,烯丙基和乙烯基。
    • 5. 发明授权
    • Cyclopropyl-alanine aryl/alkylsulfide/sulfonyl-terminated amino-diol
compounds for treatment of hypertension
    • 用于治疗高血压的环丙基 - 丙氨酸芳基/烷基硫化物/磺酰基封端的氨基二醇化合物
    • US5317039A
    • 1994-05-31
    • US916458
    • 1992-07-20
    • Barbara B. ChenGunnar J. HansonJohn S. Baran
    • Barbara B. ChenGunnar J. HansonJohn S. Baran
    • A61K31/16A61K31/165
    • A61K31/165A61K31/16
    • Compounds characterized generally as cyclopropyl alanine aryl/alkylsulfide/sulfonyl-terminated amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein R.sup.1 is selected from isopropyl, isobutyl, sec-butyl, tert-butyl, phenyl, fluorophenyl, chlorophenyl, benzyl, fluorobenzyl, chlorobenzyl, naphthyl, fluoronaphthyl, chloronaphthyl, fluoronapthylmethyl and chloronaphthylmethyl; wherein x is zero or two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is cyclopropylmethyl wherein R.sup.7 is cyclohexylmethyl; and wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl.
    • 通常以环丙基丙氨酸芳基/烷基硫醚/磺酰基封端的氨基二醇衍生物为特征的化合物可用作治疗高血压的肾素抑制剂。 特别感兴趣的化合物是下式的化合物,其中R 1选自异丙基,异丁基,仲丁基,叔丁基,苯基,氟苯基,氯苯基,苄基,氟苄基,氯苄基,萘基,氟萘基,氯萘基,氟萘基甲基和氯萘基甲基 ; 其中x为0或2; 其中R2选自氢,甲基,乙基和苯基; 其中R 3选自氢,环己基甲基,苄基,氟苄基,氯苄基,氟萘基甲基和氯萘基甲基; 其中R 5是环丙基甲基,其中R 7是环己基甲基; 并且其中R8选自正丙基,异丁基,环丙基,环丙基甲基,烯丙基和乙烯基。
    • 6. 发明授权
    • Propargyl-terminated cycloalkylalkyl-P2-site substituted
aryl/alkylsulfonyl-terminated alanine amino-diol compounds for
treatment of hypertension
    • 炔丙基封端的环烷基烷基-P2-位取代的芳基/烷基磺酰基封端的丙氨酸氨基二醇化合物用于治疗高血压
    • US5268391A
    • 1993-12-07
    • US916557
    • 1992-07-20
    • Gunnar J. HansonBarbara B. ChenJohn S. Baran
    • Gunnar J. HansonBarbara B. ChenJohn S. Baran
    • C07C317/44A61K31/16C07C323/25
    • C07C317/44C07C2101/02C07C2101/14
    • Compounds characterized generally as being propargyl-terminated aryl/alkylsulfonyl-terminated amino diol derivatives having a cycloalkylalkyl group at the P2 substitution site are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein R.sup.1 is selected from isopropyl, isobutyl, sec-butyl, tert-butyl, phenyl, fluorophenyl, chlorophenyl, benzyl, fluorobenzyl, chlorobenzyl, naphthyl, fluoronaphthyl, chloronaphthyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is selected from cycloalkylalkyl groups containing from three to about twelve carbon atoms; wherein R.sup.7 is cyclohexylmethyl; and wherein R.sup.8 is propargyl or a propargyl-containing moiety.
    • 通常作为在P2取代位置具有环烷基烷基的炔丙基封端的芳基/烷基磺酰基封端的氨基二醇衍生物的化合物可用作治疗高血压的肾素抑制剂。 特别感兴趣的化合物是下式的化合物,其中R 1选自异丙基,异丁基,仲丁基,叔丁基,苯基,氟苯基,氯苯基,苄基,氟苄基,氯苄基,萘基,氟萘基,氯萘基,氟萘基甲基和氯萘基甲基 ; 其中R2选自氢,甲基,乙基和苯基; 其中R 3选自氢,环己基甲基,苄基,氟苄基,氯苄基,氟萘基甲基和氯萘基甲基; 其中R 5选自含有3至约12个碳原子的环烷基烷基; 其中R 7为环己基甲基; 并且其中R8是炔丙基或含炔丙基的部分。
    • 7. 发明授权
    • Di-propargyl-containing aryl/alkylsulfonyl-terminated alanine amino-diol
compounds for treatment of hypertension
    • 含炔丙基的芳基/烷基磺酰基封端的丙氨酸氨基二醇化合物用于治疗高血压
    • US5246969A
    • 1993-09-21
    • US916571
    • 1992-07-20
    • Gunnar J. HansonBarbara B. ChenJohn S. Baran
    • Gunnar J. HansonBarbara B. ChenJohn S. Baran
    • C07C317/44C07C323/60
    • C07C323/60C07C317/44C07C2101/14
    • Compounds characterized generally as di-propargyl-containing aryl/alkylsulfonyl-terminated amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein R.sup.1 is selected from isopropyl, isobutyl, sec-butyl, tert-butyl, phenyl, fluorophenyl, chlorophenyl, benzyl, fluorobenzyl, chlorobenzyl, naphthyl, fluoronaphthyl, chloronaphthyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.2 is selected from hydrido, nethyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylnethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein each of R.sup.5 and R.sup.8 is independently propargyl or a propargyl-containing moiety; and wherein R.sup.7 is cyclohexylmethyl.
    • 通常被称为含二炔丙基的芳基/烷基磺酰基封端的氨基二醇衍生物的化合物可用作治疗高血压的肾素抑制剂。 特别感兴趣的化合物是下式的化合物,其中R1选自异丙基,异丁基,仲丁基,叔丁基,苯基,氟苯基,氯苯基,苄基,氟苄基,氯苄基,萘基,氟萘基,氯萘基,氟萘基甲基和氯萘基甲基 ; 其中R2选自氢,甲基,乙基和苯基; 其中R 3选自氢化,环己基乙基,苄基,氟苄基,氯苄基,氟萘基甲基和氯萘基甲基; 其中R 5和R 8各自独立地是炔丙基或含炔丙基的部分; 并且其中R 7为环己基甲基。
    • 8. 发明授权
    • Alkylaminoalkyl-sulfonyl-terminated &bgr;-alanineamide amino-diol compounds for treatment of hypertension
    • 用于治疗高血压的烷基氨基烷基 - 磺酰基封端的β-丙氨酰胺氨基二醇化合物
    • US06403648B2
    • 2002-06-11
    • US09761907
    • 2001-01-17
    • Gunnar J. HansonJohn S. BaranBarbara B. Chen
    • Gunnar J. HansonJohn S. BaranBarbara B. Chen
    • A61K3116
    • C07C317/44A61K31/16A61K31/165C07C2601/02C07C2601/14
    • Compounds characterized generally as alkylaminoalkyl-terminated &bgr;-alanineamide amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula wherein n is two or three; wherein x is a number selected from zero, one and two; wherein R2 is selected from hydrido, methyl, ethyl and phenyl; wherein R3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, napthylmethyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R5 is methyl; wherein R7 is cyclohexylmethyl; wherein R8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R9 and R10 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.
    • 通常以烷基氨基烷基封端的β-丙氨酰胺氨基二醇衍生物表征的化合物可用作治疗高血压的肾素抑制剂。 特别令人感兴趣的化合物是所述的那些,其中n是2或3; 其中x是选自零,一和二的数; 其中R2选自氢,甲基,乙基和苯基; 其中R 3选自氢,环己基甲基,苄基,氟苄基,氯苄基,萘基甲基,氟萘基甲基和氯萘基甲基; 其中R5是甲基; 其中R 7为环己基甲基; 其中R8选自正丙基,异丁基,环丙基,环丙基甲基,烯丙基和乙烯基; 并且其中R 9和R 10各自独立地选自甲基,乙基和异丙基; 或其药学上可接受的盐。