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    Peptide and peptide analog protease inhibitors
    3.
    发明授权
    Peptide and peptide analog protease inhibitors 失效
    肽和肽类似物蛋白酶抑制剂

    公开(公告)号：US6015879A

    公开(公告)日：2000-01-18

    申请号：US442662

    申请日：1995-05-17

    申请人： Ian Alexander McDonald ,  Elisabeth Albrecht ,  Benito Munoz

    发明人： Ian Alexander McDonald ,  Elisabeth Albrecht ,  Benito Munoz

    IPC分类号： A61K38/00 ,  A61K31/00 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  C07C237/22 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/078 ,  C07K5/08 ,  C07K5/083 ,  A61K38/06

    CPC分类号： C07K5/0808 ,  C07C237/22 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06043 ,  C07K5/06078 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/06191 ,  A61K38/00

    摘要： Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided Among the compounds are those of formulae I and II: ##STR1## in which R.sub.1 is preferably 2-methyl propene, 2-butene, cyclohexyl or cyclohexylmethyl; R.sub.2, R.sub.4, and R.sub.8 are each independently methyl or ethyl; R.sub.3 is preferably iso-butyl or phenyl; R.sub.5 is preferably iso-butyl; R.sub.6 is H or methyl; R.sub.7 --(Q).sub.n is preferably benzyloxycarbonyl or acetyl; Q is preferably --C(O)--; R.sub.B is preferbly iso-butyl; --R.sub.A =--(T).sub.m --(D).sub.m --R.sub.1, is which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C.sub.3-4 alkenyl being more preferred; and X is preferably an .alpha.-ketoester or .alpha.-ketoamide or aldehyde.

    摘要翻译： 提供化合物和化合物用于治疗以沉淀淀粉样蛋白为特征的疾病的方法在这些化合物中是式I和II的化合物：其中R 1优选为2-甲基丙烯，2-丁烯，环己基或环己基甲基; R2，R4和R8各自独立地是甲基或乙基; R3优选为异丁基或苯基; R5优选为异丁基; R6是H或甲基; R7-（Q）n优选为苄氧羰基或乙酰基; Q优选为-C（O） - ; RB优选为异丁基; -RA = - （T）m-（D）m -R 1，其中T优选为氧或碳，D优选为单不饱和C 3-4烯基为更优选的; 并且X优选为α-酮酯或α-酮酰胺或醛。

    Peptide and peptide analog protease inhibitors
    4.
    发明授权
    Peptide and peptide analog protease inhibitors 失效
    肽和肽类似物蛋白酶抑制剂

    公开(公告)号：US5804560A

    公开(公告)日：1998-09-08

    申请号：US369422

    申请日：1995-01-06

    申请人： Ian Alexander McDonald ,  Elisabeth Albrecht ,  Benito Munoz

    发明人： Ian Alexander McDonald ,  Elisabeth Albrecht ,  Benito Munoz

    IPC分类号： A61K38/00 ,  A61K31/00 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  C07C237/22 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/078 ,  C07K5/08 ,  C07K5/083 ,  A61K38/05

    CPC分类号： C07K5/0808 ,  C07C237/22 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06043 ,  C07K5/06078 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/06191 ,  A61K38/00

    摘要： Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds are those of formulae I and II: ##STR1## in which R.sub.1 is preferably 2-methyl propene, 2-butene, cyclohexyl or cyclohexylmethyl; R.sub.2, R.sub.4, and R.sub.8 are each independently methyl or ethyl; R.sub.3 is preferably iso-butyl or phenyl; R.sub.5 is preferably iso-butyl; R.sub.6 is H or methyl; R.sub.7 -(Q).sub.n is preferably benzyloxycarbonyl or acetyl; Q is preferably --C(O)--; R.sub.B is preferbly iso-butyl; R.sub.A =--(T).sub.m--(D).sub.m--R.sub.1, is which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C.sub.3-4 alkenyl being more preferred; and X is preferably an .alpha.-ketoester or .alpha.-ketoamide or aldehyde.

    摘要翻译： 提供了化合物和化合物用于治疗以沉淀淀粉样蛋白为特征的疾病的方法。 其中R 1优选为2-甲基丙烯，2-丁烯，环己基或环己基甲基;其中R 1优选为2-甲基丙烯，2-丁烯，环己基或环己基甲基; R2，R4和R8各自独立地是甲基或乙基; R3优选为异丁基或苯基; R5优选为异丁基; R6是H或甲基; R7-（Q）n优选为苄氧羰基或乙酰基; Q优选为-C（O） - ; RB优选为异丁基; RA = - （T）m-（D）m -R 1，其中T优选为氧或碳，D优选为单不饱和C 3-4烯基; 并且X优选为α-酮酯或α-酮酰胺或醛。

    Phosphotetrahydropyran compounds for the treatment of wounds and fibrotic disorders
    5.
    发明授权
    Phosphotetrahydropyran compounds for the treatment of wounds and fibrotic disorders 失效
    用于治疗伤口和纤维化疾病的磷酸四氢吡喃化合物

    公开(公告)号：US08557783B2

    公开(公告)日：2013-10-15

    申请号：US13318065

    申请日：2010-04-28

    申请人： Alan D. Robertson ,  Diego Silva ,  Ian Alexander McDonald

    发明人： Alan D. Robertson ,  Diego Silva ,  Ian Alexander McDonald

    IPC分类号： A61K31/70 ,  A61K31/7028

    CPC分类号： A61K31/665

    摘要： Methods of using phosphotetrahydropyran compounds for treatment of fibrotic and scarring disorders, e.g. pulmonary fibrosis, fibrosis associated with surgical procedures, wound healing disorders, scar formation, sclerotic disorders, ocular fibrotic disorders, ocular healing disorders, ocular fibrosis after surgery, glaucoma, tendon scarring disorders, joint scarring disorders, kidney interstitial fibrosis and glomerular fibrosis and tubular fibrosis of the kidney.

    摘要翻译： 使用磷酸四氢吡喃化合物治疗纤维化和瘢痕障碍的方法，例如 肺纤维化，与外科手术相关的纤维化，伤口愈合障碍，瘢痕形成，硬化性疾病，眼部纤维化病症，眼部愈合障碍，手术后眼部纤维化，青光眼，腱瘢痕障碍，关节瘢痕形成障碍，肾间质性纤维化和肾小球纤维化和肾小管 肾纤维化。

    PHOSPHOTETRAHYDROPYRAN COMPOUNDS FOR THE TREATMENT OF WOUNDS AND FIBROTIC DISORDERS
    7.
    发明申请
    PHOSPHOTETRAHYDROPYRAN COMPOUNDS FOR THE TREATMENT OF WOUNDS AND FIBROTIC DISORDERS 失效
    用于治疗伤口和纤维性疾病的磷酸三氢吡喃化合物

    公开(公告)号：US20120045455A1

    公开(公告)日：2012-02-23

    申请号：US13318065

    申请日：2010-04-28

    申请人： Alan D. Robertson ,  Diego Silva ,  Ian Alexander McDonald

    发明人： Alan D. Robertson ,  Diego Silva ,  Ian Alexander McDonald

    IPC分类号： A61K39/395 ,  A61P17/02 ,  A61P11/00 ,  A61K31/665

    CPC分类号： A61K31/665

    摘要： Methods of using phosphotetrahydropyran compounds for treatment of fibrotic and scarring disorders, e.g. pulmonary fibrosis, fibrosis associated with surgical procedures, wound healing disorders, scar formation, sclerotic disorders, ocular fibrotic disorders, ocular healing disorders, ocular fibrosis after surgery, glaucoma, tendon scarring disorders, joint scarring disorders, kidney interstitial fibrosis and glomerular fibrosis and tubular fibrosis of the kidney.

    摘要翻译： 使用磷酸四氢吡喃化合物治疗纤维化和瘢痕障碍的方法，例如 肺纤维化，与外科手术相关的纤维化，伤口愈合障碍，瘢痕形成，硬化性疾病，眼部纤维化病症，眼部愈合障碍，手术后眼部纤维化，青光眼，腱瘢痕障碍，关节瘢痕形成障碍，肾间质性纤维化和肾小球纤维化和肾小管 肾纤维化。