Method of treatment for decreasing mortality resulting from congestive
heart failure
    1.
    发明授权
    Method of treatment for decreasing mortality resulting from congestive heart failure 失效
    减少充血性心力衰竭引起的死亡率的治疗方法

    公开(公告)号:US5760069A

    公开(公告)日:1998-06-02

    申请号:US483635

    申请日:1995-06-07

    CPC分类号: A61K31/403 A61K31/7048

    摘要: A method of treatment using a compound of Formula I: ##STR1## wherein: R.sub.1 is hydrogen, lower alkanoyl of up to 6 carbon atoms or aroyl selected from benzoyl and naphthoyl; R.sub.2 is hydrogen, lower alkyl of up to 6 carbon atoms or arylalkyl selected from benzyl, phenylethyl and phenylpropyl; R.sub.3 is hydrogen or lower alkyl of up to 6 carbon atoms; R.sub.4 is hydrogen or lower alkyl of up to 6 carbon atoms, or when X is oxygen, R.sub.4 together with R.sub.5 can represent --CH.sub.2 --O--; X is a valency bond, --CH.sub.2, oxygen or sulfur; Ar is selected from phenyl, naphthyl, indanyl and tetrahydronaphthyl; R.sub.5 and R.sub.6 are individually selected from hydrogen, fluorine, chlorine, bromine, hydroxyl, lower alkyl of up to 6 carbon atoms, a --CONH.sub.2 -- group, lower alkoxy of up to 6 carbon atoms, benzyloxy, lower alkylthio of up to 6 carbon atoms, lower alkysulphinyl of up to 6 carbon atoms and lower alkylsulphonyl of up to 6 carbon atoms; or R.sub.5 and R.sub.6 together represent methylenedioxy; or a pharmaceutically acceptable salt thereof, alone or in conjunction with one or more other therapeutic agents, said agents being selected from the group consisting of ACE inhibitors, diuretics, and digoxin for decreasing mortality resulting from congestive heart failure (CHF) in mammals, particularly humans.

    摘要翻译: 使用式I化合物的方法:其中:R1是氢,至多6个碳原子的低级烷酰基或选自苯甲酰基和萘甲酰基的芳酰基; R2是氢,至多6个碳原子的低级烷基或选自苄基,苯基乙基和苯基丙基的芳基烷基; R3是氢或至多6个碳原子的低级烷基; R4是氢或至多6个碳原子的低级烷基,或当X是氧时,R4与R5一起可以代表-CH2-O-; X是价键,-CH 2,氧或硫; Ar选自苯基,萘基,茚满基和四氢萘基; R 5和R 6分别选自氢,氟,氯,溴,羟基,至多6个碳原子的低级烷基,-CONH 2 - 基,至多6个碳原子的低级烷氧基,苄氧基,至多6个碳的低级烷硫基 原子,低至6个碳原子的低级烷基亚磺酰基和至多6个碳原子的低级烷基磺酰基; 或R5和R6一起表示亚甲二氧基; 特别是用于降低哺乳动物充血性心力衰竭(CHF)引起的死亡率的ACE抑制剂,利尿剂和地高辛,所述药物单独或与一种或多种其它治疗剂联合使用,或其药学上可接受的盐, 人类。

    Method of treatment for decreasing mortality resulting from congestive heart failure
    2.
    再颁专利
    Method of treatment for decreasing mortality resulting from congestive heart failure 有权
    减少充血性心力衰竭引起的死亡率的治疗方法

    公开(公告)号:USRE40000E1

    公开(公告)日:2008-01-08

    申请号:US10721020

    申请日:2003-11-25

    摘要: A method of treatment using a compound of Formula I: wherein: R1 is hydrogen, lower alkanoyl of up to 6 carbon atoms or aroyl selected from benzoyl and naphthoyl; R2 is hydrogen, lower alkyl of up to 6 carbon atoms or arylalkyl selected from benzyl, phenylethyl and phenylpropyl; R3 is hydrogen or lower alkyl of up to 6 carbon atoms; R4 is hydrogen or lower alkyl of up to 6 carbon atoms, or when X is oxygen, R4 together with R5 can represent —CH2—O—; X is a valency bond, —CH2, oxygen or sulfur; Ar is selected from phenyl, naphthyl, indanyl and tetrahydronapthyl; R5 and R6 are individually selected from hydrogen, fluorine, chlorine, bromine, hydroxyl, lower alkyl of up to 6 carbon atoms, a —CONH2— group, lower alkoxy of up to 6 carbon atoms, benzyloxy, lower alkylthio of up to 6 carbon atoms, lower alkysulphinyl of up to 6 carbon atoms and lower alkylsulphonyl of up to 6 carbon atoms; or R5 and R6 together represent methylenedioxy; or a pharmaceutically acceptable salt thereof, alone or in conjunction with one or more other therapeutic agents, said agents being selected from the group consisting of ACE inhibitors, diuretics, and digoxin for decreasing mortality resulting from congestive heart failure (CHF) in mammals, particularly humans.

    摘要翻译: 使用式I化合物的方法:其中:R 1是氢,至多6个碳原子的低级烷酰基或选自苯甲酰基和萘甲酰基的芳酰基; R 2是氢,至多6个碳原子的低级烷基或选自苄基,苯基乙基和苯基丙基的芳基烷基; R 3是氢或至多6个碳原子的低级烷基; R 4是氢或至多6个碳原子的低级烷基,或者当X是氧时,R 4与R 5一起可代表 - CH 2 -O-; X是价键,-CH 2,氧或硫; Ar选自苯基,萘基,茚满基和四氢萘基; R 5和R 6分别选自氢,氟,氯,溴,羟基,至多6个碳原子的低级烷基,-CONH 2, 最多6个碳原子的低级烷氧基,至多6个碳原子的低级烷硫基,至多6个碳原子的低级烷基亚磺酰基和至多6个碳原子的低级烷基磺酰基; 或R 5和R 6一起代表亚甲二氧基; 特别是用于降低哺乳动物充血性心力衰竭(CHF)引起的死亡率的ACE抑制剂,利尿剂和地高辛,所述药物单独或与一种或多种其它治疗剂联合使用,或其药学上可接受的盐, 人类。

    Parathormone fragments, their preparation and medicaments containing
these
    7.
    发明授权
    Parathormone fragments, their preparation and medicaments containing these 失效
    parathormone片段,它们的制备和含有这些的药物

    公开(公告)号:US5783558A

    公开(公告)日:1998-07-21

    申请号:US256363

    申请日:1994-07-20

    CPC分类号: C07K14/635 A61K38/00

    摘要: The invention concerns parathormone (PTH) fragments including the amino acid range of the natural parathormone of +3 to +35 and their physiologically compatible derivatives, a process for the preparation of the fragments according to the solid phase and liquid phase synthesis from partly blocked amino acids contained in the fragments which are coupled with one another in the sequence which corresponds to the amino acid sequence in the fragments to be prepared and medicaments containing at least one of the fragments, especially with calcium-regulating action in the body.

    摘要翻译: PCT No.PCT / EP93 / 00259 Sec。 371日期:1994年7月20日 102(e)日期1994年7月20日PCT提交1993年2月4日PCT公布。 公开号WO93 / 15109 日期:1993年8月5日本发明涉及包含+3至+35的天然parathormone的氨基酸范围及其生理上相容的衍生物的parathormone(PTH)片段,根据固相和液相制备片段的方法 从与待制备的片段中的氨基酸序列相对应的序列中彼此偶联的片段中包含的部分封闭的氨基酸合成,以及含有至少一个片段的药物,特别是在 身体。