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    Methods of treating neurodegenerative disorders using protease inhibitors
    31.
    发明授权
    Methods of treating neurodegenerative disorders using protease inhibitors 失效
    使用蛋白酶抑制剂治疗神经变性疾病的方法

    公开(公告)号：US5863902A

    公开(公告)日：1999-01-26

    申请号：US444912

    申请日：1995-05-18

    申请人： Benito Munoz ,  Ian A. McDonald ,  Elisabeth Albrecht

    发明人： Benito Munoz ,  Ian A. McDonald ,  Elisabeth Albrecht

    IPC分类号： A61K38/00 ,  C07C237/22 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/078 ,  C07K5/083 ,  A61K38/05

    CPC分类号： C07K5/0808 ,  C07C237/22 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06043 ,  C07K5/06078 ,  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), (II) and (III): ##STR1## in which R.sub.1 is preferably 2-methyl propene, 2-butene, norleucine; 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)--; RB 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 an alcohol, particularly a secondary alcohol.

    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，正亮氨酸;式（I），（II）和（III）的化合物为： 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; X是醇，特别是仲醇。

    Peptide and peptide analog protease inhibitors
    32.
    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。

    VLA-4 Antagonists
    36.
    发明申请
    VLA-4 Antagonists 审中-公开
    VLA-4拮抗剂

    公开(公告)号：US20090048308A1

    公开(公告)日：2009-02-19

    申请号：US11918100

    申请日：2006-04-10

    申请人： Nicholas S. Stock ,  Nicholas D. Smith ,  Benito Munoz

    发明人： Nicholas S. Stock ,  Nicholas D. Smith ,  Benito Munoz

    IPC分类号： A61K31/4439 ,  C07D401/12 ,  A61P35/02 ,  A61P9/10 ,  A61P35/00 ,  A61P11/06 ,  A61P19/02 ,  A61P1/00

    CPC分类号： C07D401/12

    摘要： 4-Thio, 4-sulfinyl and 4-sulfonyl proline derivatives of the present invention are antagonists of the VLA-4 integrin and are useful in the treatment, prevention and suppression of diseases mediated by VLA-4-binding and cell adhesion and activation. Moreover, the compounds of the present invention demonstrate significant receptor occupancy of VLA-4 bearing cells after oral administration and are suitable for once-, twice-, or thrice-a-day oral administration. This invention also relates to compositions containing such compounds and methods of treatment using such compounds.

    摘要翻译： 本发明的4-硫代，4-亚磺酰基和4-磺酰基脯氨酸衍生物是VLA-4整联蛋白的拮抗剂，可用于治疗，预防和抑制由VLA-4结合和细胞粘附和活化介导的疾病。 此外，本发明的化合物在口服给药后显示VLA-4携带细胞的显着受体占有率，并且适合于一天一次，两次或每日三次口服给药。 本发明还涉及含有这些化合物的组合物和使用这些化合物的治疗方法。

    Prodrugs of diaryl-2-(5h)-furanone cyclooxygenase-2 inhibitors
    38.
    发明申请
    Prodrugs of diaryl-2-(5h)-furanone cyclooxygenase-2 inhibitors 失效
    二芳基-2-（5h） - 呋喃酮环加氧酶-2抑制剂的前药

    公开(公告)号：US20070123587A1

    公开(公告)日：2007-05-31

    申请号：US10574655

    申请日：2004-10-18

    申请人： Jeannie Arruda ,  Benito Munoz ,  Brian Stearns

    发明人： Jeannie Arruda ,  Benito Munoz ,  Brian Stearns

    IPC分类号： A61K31/235 ,  C07C317/24

    CPC分类号： C07C317/46 ,  C07C2601/02

    摘要： The invention encompasses the novel compounds of Formula (I) and Formula (II), which are prodrugs that convert in vivo to diaryl-2-(5H)-furanones useful in the treatment of cyclooxygenase-2 mediated diseases. These prodrugs are far more soluble in aqueous media than the active agents into which they convert, in vivo. As such compounds of Formula (I) and (II) are advantageous for, among other things intravenous administration. The invention also encompasses certain pharmaceutical compositions and methods for treatment of cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula (I) and Formula (II).

    摘要翻译： 本发明包括式（I）和式（II）的新型化合物，其是在体内转化成可用于治疗环氧合酶-2介导的疾病的二芳基-2-（5H） - 呋喃酮的前药。 这些前药在水性介质中比在体内转化的活性剂更易溶于水。 因为式（I）和（II）的这样的化合物除了其它的静脉内给药之外是有利的。 本发明还包括用于治疗环氧合酶-2介导的疾病的某些药物组合物和方法，其包括使用式（I）和式（II）的化合物。

    Nitric oxide releasing drugs for Alzheimer's disease
    40.
    发明申请
    Nitric oxide releasing drugs for Alzheimer's disease 审中-公开
    一氧化氮释放药物用于阿尔茨海默病

    公开(公告)号：US20050054714A1

    公开(公告)日：2005-03-10

    申请号：US10889917

    申请日：2004-07-13

    申请人： Benito Munoz ,  Peptiboon Prasit ,  Thomas Reger

    发明人： Benito Munoz ,  Peptiboon Prasit ,  Thomas Reger

    IPC分类号： A61K31/00 ,  C07C291/02 ,  A61K31/405 ,  C07D209/42

    CPC分类号： C07C291/02 ,  A61K31/00

    摘要： The present invention encompasses compounds of Formula I or pharmaceutically acceptable salts thereof, wherein each R1 may be substituted at any substitutable position on A and each R1 is independently selected from the group consisting of: halo, cyano, C1-4alkoxy, C1-4alkylthio and C1-4alkyl, each of said C1-4alkoxy, C1-4alkylthio and C1-4alkyl optionally substituted with 1 to 3 halo groups, R2 is selected from the group consisting of: C1-6alkyl and C3-6cycloalkyl, R3 is selected from the group consisting of: hydrogen, C1-6alkyl and C3-6cycloalkyl and R4 is a nitric oxide releasing moiety. Pharmaceutical composition comprising said compounds and methods of using said compounds are also encompassed. The compounds of the present invention lower the level of Aβ42 and are therefore useful for treating or preventing Alzheimer's Disease. The compounds of the invention also release nitric oxide in vivo and have a reduced potency for cyclooxygenase activity. Therefore, the compounds of the present invention do not possess the gastrointestinal side effects associated with nonsteroidal antiinflammatory drugs (NSAIDs).

    摘要翻译： 本发明包括式I化合物或其药学上可接受的盐，其中每个R 1可以在A上的任何可取代的位置被取代，每个R 1独立地选自：卤素，氰基，C1- 烷氧基，C 1-4烷硫基和C 1-4烷基，所述C 1-4烷氧基，C 1-4烷硫基和任选被1至3个卤素取代的C 1-4烷基，R 2选自：C 1-6烷基和C 3 -6-环烷基，R 3选自：氢，C 1-6烷基和C 3-6环烷基，R 4是一氧化氮释放部分。 还包括包含所述化合物的药物组合物和使用所述化合物的方法。 本发明的化合物降低Aβ42的水平，因此可用于治疗或预防阿尔茨海默病。 本发明的化合物还在体内释放一氧化氮，并且具有降低的环氧合酶活性的效力。 因此，本发明的化合物不具有与非甾体抗炎药（NSAID）相关的胃肠道副作用。