Fluoroalkyl-functional organopolysiloxane-containing compositions
    71.
    发明授权
    Fluoroalkyl-functional organopolysiloxane-containing compositions 失效
    含氟烷基官能的含有机聚硅氧烷的组合物

    公开(公告)号:US5849942A

    公开(公告)日:1998-12-15

    申请号:US984163

    申请日:1997-12-03

    摘要: An aqueous alcoholic fluoroalkyl functional group containing organopolysiloxane- composition, comprising: organopolysiloxanes of formula I: RO�Si(A)(CH.sub.3).sub.z (OR).sub.1-z O!.sub.a �Si(B)(R.sup.2).sub.y (OR).sub.1-y O!.sub.b �Si(C)(CH.sub.3)O!.sub.c �Si(D)(OR)O!.sub.d R.multidot.(HX)(I) wherein A is an aminoalkyl radical derived from the compound of formula II:H.sub.2 N(CH.sub.2).sub.f (NH).sub.g (CH.sub.2).sub.h Si(OR).sub.3-z (CH.sub.3).sub.z (II) wherein 0.ltoreq.f.ltoreq.6, 9=0 if f=0 and g=1 if f>0, 0.ltoreq.h.ltoreq.6 and 0.ltoreq.z.ltoreq.1, and B is a fluoroalkyl radical derived from the compound of formula III: R.sup.1 --Y--(CH.sub.2).sub.2 Si(R.sup.2)y(OR).sub.3-y (III) wherein R.sup.1 is a mono-, oligo- or perfluorinated alkyl group having 1-9 C atoms or a mono-, oligo- or perfluorinated aryl group, Y is a CH.sub.2, O or S group, R.sub.2 is a linear, branched or cyclic alkyl group having 1-8 C atoms or an aryl group and 0.ltoreq.y.ltoreq.1, and C is an alkyl radical derived from the compound of formula IV: R.sup.3 --Si(CH.sub.3)(OR).sub.2 (IV) and D is also an alkyl radical derived from the compound of formula V: R.sup.3 --Si(OR).sub.3 (V) wherein R.sup.3 in the preceding formulae is in each case identical or different, and is a linear, branched or cyclic alkyl group having 1-8 C atoms, R in the preceding formulae is in each case identical or different, and is a linear, branched or cyclic alkyl group having 1-8 C atoms or an aryl group, and HX is an acid, in which X is an inorganic or organic acid radical, and 0.ltoreq.y.ltoreq.1, 0.ltoreq.z.ltoreq.1, a>0, b>0, c>0, d>0, e>0 and (a+b+c+d).gtoreq.2.

    摘要翻译: 含有有机聚硅氧烷组合物的含水醇的氟代烷基官能团包括:式I的有机聚硅氧烷:RO [Si(A)(CH3)z(OR)1-zO] a [Si(B)(R2)y(OR) yO] b [Si(C)(CH3)O] c [Si(D)(OR)O] dRx(HX)(I)其中A是衍生自式II化合物的氨基烷基:H 2 N(CH 2)f (NH)g(CH 2)h Si(OR)3-z(CH 3)z(II)其中0 0,则g = R =(Y) - (CH 2)2 Si(R 2)y(OR)3-y (III)其中R1是具有1-9个C原子的单,低聚或全氟烷基或单,低聚或全氟化的芳基,Y是CH 2,O或S基团,R 2是直链,支链 或具有1-8个碳原子或芳基且0≤y≤1的环状烷基,C是衍生自式IV化合物的烷基:R3-Si(CH3)(OR)2( IV),D也是衍生自式V化合物的烷基:R 3 -Si(OR)3(V)其中前述通式中的R 3在每种情况下相同 或者不同的是具有1-8个C原子的直链,支链或环状的烷基,前述式中的R各自相同或不同,为具有1-8个C原子的直链,支链或环状的烷基或 芳基,HX是酸,其中X是无机或有机酸基,且0≤z≤1,a> 0,b> 0, c> 0,d> 0,e> 0和(a + b + c + d)> / = 2。

    Carboxamide compounds and their use as calpain inhibitors
    74.
    发明授权
    Carboxamide compounds and their use as calpain inhibitors 有权
    羧酰胺化合物及其作为钙蛋白酶抑制剂的用途

    公开(公告)号:US09018206B2

    公开(公告)日:2015-04-28

    申请号:US13610975

    申请日:2012-09-12

    摘要: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y is a moiety CH2—CH2, CH2—CH2—CH2, N(Ry#)—CH2, N(Ry#)—CH2—CH2 or CH═CH—CH═, each optionally having 1 or 2 H-atoms replaced with identical or different radicals Ry, wherein Ry and Ry# have the meanings mentioned in the claims.

    摘要翻译: 本发明涉及新的羧酰胺化合物及其用于制备药物的用途。 羧酰胺化合物是钙蛋白酶(钙依赖性半胱氨酸蛋白酶)的抑制剂。 因此,本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。 羧酰胺化合物是通式I的化合物,其中R 1,R 2,R 3a,R 3b,R 4,Q,Y,A和X具有权利要求和说明书中所述的含义及其互变异构体及其药学上合适的盐。 特别地,化合物具有通式Ia和Ib,其中R1,r,R2b,R3a,R3b,R4,Y和X具有权利要求中提及的含义,包括其互变异构体及其药学上合适的盐。 在这些化合物中,优选其中Y为CH2-CH2,CH2-CH2-CH2,N(Ry#)-CH2,N(Ry#)-CH2-CH2或CH = CH-CH≡,各自任选具有1 或2个H原子被相同或不同的基团Ry取代,其中Ry和Ry#具有权利要求中提及的含义。

    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS
    77.
    发明申请
    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 审中-公开
    羧酰胺化合物及其作为钙蛋白酶抑制剂的用途

    公开(公告)号:US20130150367A1

    公开(公告)日:2013-06-13

    申请号:US13610975

    申请日:2012-09-12

    摘要: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y is a moiety CH2—CH2, CH2—CH2—CH2, N(Ry#)—CH2, N(Ry#)—CH2—CH2 or CH═CH—CH═, each optionally having 1 or 2 H-atoms replaced with identical or different radicals Ry, wherein Ry and Ry# have the meanings mentioned in the claims.

    摘要翻译: 本发明涉及新的羧酰胺化合物及其用于制备药物的用途。 羧酰胺化合物是钙蛋白酶(钙依赖性半胱氨酸蛋白酶)的抑制剂。 因此,本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。 羧酰胺化合物是通式I的化合物,其中R 1,R 2,R 3a,R 3b,R 4,Q,Y,A和X具有权利要求和说明书中所述的含义及其互变异构体及其药学上合适的盐。 特别地,化合物具有通式Ia和Ib,其中R1,r,R2b,R3a,R3b,R4,Y和X具有权利要求中提及的含义,包括其互变异构体及其药学上合适的盐。 在这些化合物中,优选其中Y为CH2-CH2,CH2-CH2-CH2,N(Ry#)-CH2,N(Ry#)-CH2-CH2或CH = CH-CH =,各自任选具有1 或2个H原子被相同或不同的基团Ry取代,其中Ry和Ry#具有权利要求中提及的含义。