Aromatic hydroxamix acid compounds, their production and use
    2.
    发明授权
    Aromatic hydroxamix acid compounds, their production and use 失效
    芳香族异羟肟酸化合物,其生产和使用

    公开(公告)号:US5891916A

    公开(公告)日:1999-04-06

    申请号:US662240

    申请日:1996-06-14

    CPC分类号: C07C271/60 C07C259/06

    摘要: A compound represented by the formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 independently represent an optionally substituted aromatic group; Q represents an optionally substituted divalent aliphatic hydrocarbon group optionally containing O or S; R.sup.1 represents H, acyl group, etc.; and X represents an electron-withdrawing group, an optionally substituted aromatic group, a group of the formula: ##STR2## wherein R.sup.2 and R.sup.3 independently represent H, acyl group or an optionally substituted hydrocarbon group, etc., etc.; or salts thereof are useful as an excellent anti-neurodegenerative agent.

    摘要翻译: 由下式表示的化合物:其中Ar 1和Ar 2独立地表示任选取代的芳基; Q表示任选含有O或S的任选取代的二价脂族烃基; R1代表H,酰基等; X表示吸电子基团,可以具有取代基的芳基,下式的基团:其中R2和R3独立地表示H,酰基或任意取代的烃基等; 或其盐可用作优异的抗神经变性剂。

    Process for producing amine derivatives
    3.
    发明授权
    Process for producing amine derivatives 失效
    制备胺衍生物的方法

    公开(公告)号:US06784314B2

    公开(公告)日:2004-08-31

    申请号:US10240574

    申请日:2002-10-01

    IPC分类号: C07C23305

    摘要: This invention provides a convenient and industrially advantageous process producing amine derivatives having the action of inhibiting the secretion and accumulation of amyloid &bgr; protein. In Compound (I), the ether linkage is selectively cleaved without cleaving the amide linkage present in the same molecule and tertiary amines are not converted into quaternary salts, and thus Amine Derivative (V) with good qualities having the action of inhibiting the secretion and accumulation of amyloid &bgr; protein can be obtained in high yield.

    摘要翻译: 本发明提供了方便和工业上有利的方法,产生具有抑制淀粉样蛋白β蛋白分泌和积累作用的胺衍生物。在化合物(I)中,醚键被选择性地切割而不裂解同一分子中存在的酰胺键和叔 胺不会转化为季盐,因此可以高产率获得具有抑制淀粉样β蛋白分泌和积累作用的具有良好品质的胺衍生物(V)。

    Amine compounds, their production and use
    5.
    发明授权
    Amine compounds, their production and use 有权
    胺化合物,其生产和使用

    公开(公告)号:US06613805B2

    公开(公告)日:2003-09-02

    申请号:US09931140

    申请日:2001-08-16

    IPC分类号: A61K31137

    摘要: A compound of the formula: wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) —S—, —SO— or —SO2—, (iii) C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene, etc., (iv) —CO—O— or (v) —(CH2)p-X1—, —(CH2)p-X1-(CH2)q-, —(CH2)r-CO-X1-, —SO2—NR8— or —(CH2)r-SO2—NR8— wherein X1 is O or NR8, R8 is H, a hydrocarbon group which may be substituted or an acyl, p is 0 to 5, q is 1 to 5, p+q is 1 to 5, and r is 1 to 4; Y is a divalent C1-6 aliphatic hydrocarbon group optionally containing O or S, which may be substituted; R1 and R2 each is H or a lower alkyl which may be substituted, or R1 and R2 form a N-containing heterocyclic ring which may be substituted; Ring A is a benzene ring which may be further substituted; and Ring B is a 4- to 8-membered ring which may be further substituted, or a salt thereof has the effect of inhibiting amyloid-&bgr; protein production and/or secretion and is useful as a pharmaceutical composition for preventing and/or treating the neurodegenerative disease, etc.

    摘要翻译: 下式的化合物:其中Ar是可被取代的芳环组合基团或可被取代的稠合芳基; X是(i)键,(ii)-S-,-SO-或-SO 2 - ,(iii)C 1-6亚烷基,C 2-6亚烯基或C 2-6亚炔基等,(iv)-CO- O-或(V) - (CH 2)p -X 1 - , - (CH 2)p -X 1 - (CH 2)q - , - (CH 2)r -CO-X 1 - ,-SO 2 -NR 8 - 或 - (CH 2) r-SO 2 -NR 8 - ,其中X 1为O或NR 8,R 8为H,可被取代的烃基或酰基,p为0至5,q为1至5,p + q为1至5,r 是1到4; Y是任选地含有O或S的二价C 1-6脂族烃基,其可被取代; R 1和R 2各自为H或可被取代的低级烷基,或R 1和R 2形成可被取代的含氮杂环; 环A是可以被进一步取代的苯环; 环B为可进一步取代的4-至8-元环,或其盐具有抑制淀粉样蛋白β蛋白产生和/或分泌的作用,并且可用作预防和/或治疗 神经变性疾病等

    &bgr;-amyloid protein production/secretion inhibitors
    6.
    发明授权
    &bgr;-amyloid protein production/secretion inhibitors 失效
    β-淀粉样蛋白生成/分泌抑制剂

    公开(公告)号:US06586475B1

    公开(公告)日:2003-07-01

    申请号:US09856317

    申请日:2001-06-05

    IPC分类号: A61K31165

    摘要: A compound of the formula: wherein Ar is an aromatic group; X and Y are a bivalent group selected from —O—, —S—, —CO—, —SO2—, —NR8—, —CONR8—, SO2NR8 and —COO— (wherein R8 is H, a hydrocarbon group or acyl), or a bivalent C1-6 aliphatic hydrocarbon group which may contain one or two above bivalent groups; R1 and R2 are H or C1-6 alkyl, or R1 and R2 may form, together with the adjacent nitrogen atom, a nitrogen-containing heterocyclic ring; and ring A is a monocyclic aromatic ring, or a salt thereof or a prodrug thereof exhibits an excellent inhibitory activity of the production and/or the secretion of amyloid-&bgr; protein.

    摘要翻译: 下式的化合物:其中Ar是芳族基团; X和Y是选自-O - , - S - , - CO - , - SO 2 - , - NR 8 - , - CONR 8 - ,SO 2 NR 8和-COO-(其中R 8是H,烃基或酰基) ,或可以含有一个或两个上述二价基团的二价C 1-6脂族烃基; R1和R2是H或C1-6烷基,或R1和R2可以与相邻的氮原子一起形成含氮杂环; 环A是单环芳环,或其盐或其前药对淀粉样蛋白-β蛋白的产生和/或分泌具有优异的抑制活性。

    Amine compounds, their production and use as amyloid-&bgr; production inhibitors
    7.
    发明授权
    Amine compounds, their production and use as amyloid-&bgr; production inhibitors 有权
    胺化合物,其生产和用作淀粉样蛋白-β生产抑制剂

    公开(公告)号:US06310107B1

    公开(公告)日:2001-10-30

    申请号:US09331460

    申请日:1999-06-21

    IPC分类号: A61K31137

    摘要: A compound of the formula: wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) —S—, —SO— or —SO2—, (iii) C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene, etc., (iv) —CO—O— or (v) —(CH2)p-X1—, —(CH2)p-X1— (CH2)q-, —(CH2)r-CO—X1—, —SO2—NR8— or —(CH2)r-SO2—NR8— wherein X1 is O or NR8, R8 is H, a hydrocarbon group which may be substituted or an acyl, p is 0 to 5, q is 1 to 5, p+q is 1 to 5, and r is 1 to 4; Y is a divalent C1-6 aliphatic hydrocarbon group optionally containing O or S, which may be substituted; R1 and R2 each is H or a lower alkyl which may be substituted, or R1 and R2 form a N-containing heterocyclic ring which may be substituted; Ring A is a benzene ring which may be further substituted; and Ring B is a 4- to 8-membered ring which may be further substituted, or a salt thereof has the effect of inhibiting amyloid-&bgr; protein production and/or secretion and is useful as a pharmaceutical composition for preventing and/or treating the neurodegenerative disease, etc.

    摘要翻译: 下式的化合物:其中Ar是可被取代的芳环组合基团或可被取代的稠合芳基; X是(i)键,(ii)-S-,-SO-或-SO 2 - ,(iii)C 1-6亚烷基,C 2-6亚烯基或C 2-6亚炔基等,(iv)-CO- O-或(V) - (CH 2)p -X 1 - , - (CH 2)p -X 1 - (CH 2)q - , - (CH 2)r -CO-X 1 - ,-SO 2 -NR 8 - 或 - (CH 2) r-SO 2 -NR 8 - ,其中X 1为O或NR 8,R 8为H,可被取代的烃基或酰基,p为0至5,q为1至5,p + q为1至5,r 是1到4; Y是任选地含有O或S的二价C 1-6脂族烃基,其可被取代; R 1和R 2各自为H或可被取代的低级烷基,或R 1和R 2形成可被取代的含氮杂环; 环A是可以被进一步取代的苯环; 环B为可进一步取代的4-至8-元环,或其盐具有抑制淀粉样蛋白β蛋白产生和/或分泌的作用,并且可用作预防和/或治疗 神经变性疾病等

    Polyurethaneurea elastomer
    9.
    发明授权
    Polyurethaneurea elastomer 失效
    聚氨酯脲弹性体

    公开(公告)号:US5410009A

    公开(公告)日:1995-04-25

    申请号:US82368

    申请日:1993-06-28

    摘要: A polyurethaneurea elastomer obtained by reacting a polyisocyanate component obtained by reacting 1,5-naphthalene diisocyanate with a polyol, with an amine component consisting essentially of an amine compound of the formula (1): ##STR1## wherein R is a bivalent polyalkylene polyether or polyalkylene polyester having an average molecular weight of at least 200, which may contain unsaturated bonds in the polyalkylene.

    摘要翻译: 将通过使1,5-萘二异氰酸酯与多元醇反应获得的多异氰酸酯组分与主要由式(1)的胺化合物组成的胺组分反应得到的聚氨酯脲弹性体:其中R为二价 聚亚烷基聚醚或平均分子量至少为200的聚亚烷基聚酯,其可以在聚亚烷基中含有不饱和键。