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    • 3. 发明申请
    • QUATERNARY SALTS OF 4-SUBSTITUTED PIPERIDINES, PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
    • 四取代哌嗪的季铵盐,其制备方法和含有其的药物组合物
    • WO1993018002A1
    • 1993-09-16
    • PCT/FR1993000215
    • 1993-03-03
    • ELF SANOFI
    • ELF SANOFIEMONDS-ALT, XavierPROIETTO, VincenzoVAN BROECK, DidierBRELIERE, Jean-Claude
    • C07D211/14
    • C07D401/06C07D211/14C07D211/44C07D211/48C07D211/52C07D211/58C07D409/12
    • Quaternary ammonium salts of formula (I), wherein J is a Ar-CXX'-CX" group or a Ar-(CH2)xCX1 group wherein Ar is optionally substituted phenyl, cycloalkyl, pyridyl or thienyl; X is hydrogen; X' is hydrogen or combined with X" below to form a carbon-carbon bond, or X and X' together form an oxo group; x is 0 or 1; X1 is hydrogen (x=0), hydroxyl, alkoxy, acyloxy, carboxy, carbalkoxy, cyano, carbamoylalkyl, mercapto or alkylthio; Q is an alkyl or benzyl group; A is an anion; m is 2 or 3; Ar' is optionally substituted phenyl, thienyl, benzothienyl, naphthyl or optionally N-substituted indolyl; R is hydrogen or C1-6 alkyl; T is -CO- or -CW-NH-, wherein W is an oxygen or sulphur atom; and Z is either hydrogen or M or OM when T is the -CO- group, or M when T is the -CW-NH- group; M in particular is alkyl, alpha -hydroxybenzyl, alpha -hydroxybenzylalkyl, phenylalkyl, pyridylalkyl, naphthylalkyl, pyridylthioalkyl or styryl. The salts may be used particularly in drugs for treating pathological phenomena involving the neurokinin system.
    • 式(I)的季铵盐,其中J为Ar-CXX'-CX“基或Ar-(CH2)xCX1基,其中Ar为任选取代的苯基,环烷基,吡啶基或噻吩基; X为氢; X'为 氢或与X“结合形成碳 - 碳键,或X和X'一起形成氧代基; x为0或1; X 1为氢(x = 0),羟基,烷氧基,酰氧基,羧基,烷氧羰基,氰基,氨基甲酰基烷基,巯基或烷硫基; Q是烷基或苄基; A < - >是阴离子; m为2或3; Ar'是任选取代的苯基,噻吩基,苯并噻吩基,萘基或任选的N-取代的吲哚基; R是氢或C 1-6烷基; T是-CO-或-CW-NH-,其中W是氧或硫原子; 当T为-CO-基团时,Z为氢或M或OM;当T为-CW-NH-基时,Z为M; M特别是烷基,α-羟基苄基,α-羟基苄基烷基,苯基烷基,吡啶基烷基,萘基烷基,吡啶基硫代烷基或苯乙烯基。 盐可以特别用于治疗涉及神经激肽系统的病理现象的药物中。
    • 7. 发明申请
    • INDOLINE DERIVATIVES HAVING AN AMIDE FUNCTION, THEIR PREPARATION, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    • 具有酰胺官能团的吲哚衍生物,其制备物和含有它们的药物组合物
    • WO1993003013A1
    • 1993-02-18
    • PCT/FR1992000758
    • 1992-07-31
    • ELF SANOFI
    • ELF SANOFIWAGNON, JeanPLOUZANE, ClaudeSERRADEIL-LEGAL, ClaudineNISATO, DinoTONNERRE, Bernard
    • C07D209/42
    • C07D401/06C07D209/42C07D401/12C07D403/06C07D417/06
    • The invention relates to compounds of formula (I), wherein R1 is a halogen atom, C1-C4 alkyl, hydroxyl, C1-C4 alkoxy, a group benzyloxy, cyano, trifluoromethyl, nitro or amino; R2 is C1-C6 alkyl, C3-C7 cycloalkyl, C5-C7 cycloalcen, a phenyl unsubstituted or substituted one or a plurality of times, C1-C4 alkoxy, halogen, a group trifluoromethyl, a group amino, or R2 is a nitrophenyl unsubstituted or substituted one or a plurality of times; R3 is a hydrogen atom; R4 is a carbamyl group having the formula CONR6R7; R5 is C1-C4 alkyl; naphtyl-1; naphtyl-2; dimethylamino-5 naphtyl-1; a phenyl unsubstituted or substituted one or a plurality of times, or R5 is nitrophenyl unsubstituted or substituted one or a plurality of times; R6 is C1-C6 alkyl, or R6 is similar to R7; R7 is a group piperidin-4-yl; a group azetidin-3-yl, said groups being substituted or unsubstituted on the nitrogen by C1-C4 alkyl, by a benzyloxycarbonyl or by an alkoxycarbonyl in C1-C4; a group (CH2)r itself substituted by a group pyridyl-2, -3 or -4, by a group hydroxyl, by an amino group free or substituted by one or two substituants; or R6 and R7 form together with the nitrogen atom to which they are linked a heterocycle selected amongst: morpholin, thiomorpholin, thiazolidin or 2,2-dimethylthiazolidin unsubstituted or substituted by R8, piperazin unsubstituted or substituted in 4 by a group R''8, an unsaturated mononitrogenated cycle with 5 links substituted by R8 or a saturated mononitrogenated cycle with 3, 4, 5, 6 or 7 links substituted by R8 and R9; R8 is R'8 or a group (CH2)r itself substituted by hydroxyl or by a free amino or substituted by one or two C1-C4 alkyls; R'8 is a group (CH2)q itself substituted by a carboxyl group, a group C1-C4 alkoxycarbonyl, a benzyloxycarbonyl group, a group carbamoyl free or substituted by a hydroxyl or by one or two C1-C4 alkyls, or a group aminocarbothioyl free or substituted by one or two C1-C4 alkyls; R''8 is R'8 or a group (CH2)2NH2 free or substituted by one or two C1-C4; R9 is hydrogen, halogen, a group (CH2)rOR10, a group (CH2)rNR11R12, a group (CH2)sCONR11R'11, a group azido; R10 is hydrogen, C1-C4 alkyl, mesyl or tosyl; R11, R'11 and R12 are each hydrogen or C1-C4 alkyl or R11 is hydrogen and R12 is C1-C4 alkoxycarbonyl or benzyloxycarbonyl; n is 0, 1 or 2; m is 0, 1, or 2; q is 0, 1, 2 or 3; r is 0, 1, 2 or 3 with the provision that r is different from 0 when R8 or R9 is in the alpha position of the intracyclic amidic nitrogen; s is 0 or 1; as well as its optional salts. These compounds are useful in the treatment of affections of the central nervous system, the cardiovascular system and the gastric system in human beings and animals.