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    • 2. 发明授权
    • Compounds bearing sulphamoyl and amidino radicals, their preparation
process and pharmaceutical compositions containing them
    • 带有氨磺酰基和脒基的化合物,其制备方法和含有它们的药物组合物
    • US5674890A
    • 1997-10-07
    • US582887
    • 1996-01-04
    • Bernard ChristopheLoic FoulonAlain PelletClaudine Serradeil-Le GalGerard Valette
    • Bernard ChristopheLoic FoulonAlain PelletClaudine Serradeil-Le GalGerard Valette
    • A61K31/16A61K31/155A61K31/18A61K38/00A61P9/00A61P25/00C07C311/18C07D215/36C07K1/113C07K5/06C07K5/065C07K5/078C07D333/22A61K31/38C07D409/12C07D413/12
    • C07K5/06078C07K5/06139A61K38/00
    • A compound of formula I ##STR1## in which Ar.sub.1 is naphthyl and phenyl, quinolyl or isoquinolyl optionally substituted; Ar.sub.2 is phenyl or thienyl optionally substituted; R.sub.1, R.sub.2 and R'.sub.2 are independently of each other H or (C.sub.1 -C.sub.4)alkyl or R.sub.1 represents a bond and N is covalently bonded to Ar.sub.2, and optionally R.sub.2 and R'.sub.2 form a double bond, or R.sub.1 or R.sub.2 is covalently bonded to Ar.sub.2 and represents a (C.sub.1 -C.sub.3 )alkylene; R.sub.3 and R.sub.4 are independently of each other H or (C.sub.1 -C.sub.4)alkyl or form, with the nitrogen atom to which they are attached pyrrolidine, ppiperidine, or hexahydroazepine; Z.sub.1 represents (C.sub.1 -C.sub.12)alkylene, optionally interrupted by a radical selected from the group consisting of (C.sub.5 -C.sub.7)cycloalkyl and phenyl or substituted with a radical selected from the group consisting of (C.sub.5 -C.sub.7)cycloalkyl and phenyl; Q.sub.1 is selected from the group consisting of methyl, amino, (C.sub.1 -C.sub.4)alkoxycarbonylamino, (C.sub.1 -C.sub.4)alkylamino, di(C.sub.1 -C.sub.4)-alkylamino, pyrrolidinyl, piperidino, morpholino, piperazinyl, 4-(C.sub.1 -C.sub.4)alkylpiperazinyl, amidino, (C.sub.1 -C.sub.4)-alkylamidino, guanidino, (C.sub.1 -C.sub.4)alkylguanidino, pyridyl, imidazolyl, pyrimidinyl, indolyl, hydroxy,(C.sub.1 -C.sub.4)alkoxy,(C.sub.2 -C.sub.8)alkoxycarbonyl,N-�amino(C.sub.1 -C.sub.4)alkyl!-N-�(C.sub.1 -C.sub.4)alkyl!amino, carbamoyl, phenyl and phenyl substituted by a radical selected from the group consisting of Cl, F, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy and hydroxyle; Q.sub.2 is selected from the group consisting of H and (C.sub.1 -C.sub.4)alkyl; Q.sub.3 is selected from the group consisting of H and (C.sub.1 -C.sub.4)alkyl or Q.sub.1 and Q.sub.3 are attached to form a heterocycle and together represent (C.sub.2 -C.sub.3)alkylene, whereas Z.sub.1 represents a bond, in the form of pure enantiomer or mixture thereof in any proportions as well as its salt with acid.
    • 其中Ar1是萘基和苯基,任选取代的喹啉基或异喹啉的式I化合物(I) Ar 2是任选取代的苯基或噻吩基; R 1,R 2和R'2彼此独立地为H或(C 1 -C 4)烷基或R 1表示键,并且N与Ar 2共价连接,并且任选地R 2和R'2形成双键,或者R 1或R 2为 共价结合Ar2,代表(C1-C3)亚烷基; R3和R4彼此独立地为H或(C1-C4)烷基或与其连接的氮原子形成吡咯烷,哌啶或六氢氮杂; Z1代表(C1-C12)亚烷基,任选被选自(C 5 -C 7)环烷基和苯基的基团或被选自(C 5 -C 7)环烷基和苯基的基团取代的基团间隔; Q1选自甲基,氨基,(C1-C4)烷氧基羰基氨基,(C1-C4)烷基氨基,二(C1-C4) - 烷基氨基,吡咯烷基,哌啶子基,吗啉代,哌嗪基,4-(C1-C4) 烷基脒基,胍基,(C1-C4)烷基胍基,吡啶基,咪唑基,嘧啶基,吲哚基,羟基,(C1-C4)烷氧基,(C2-C8)烷氧基羰基,N- [ C 1 -C 4烷基] -N - [(C 1 -C 4)烷基]氨基,氨基甲酰基,苯基和被选自Cl,F,(C 1 -C 4)烷基,(C 1 -C 4) 烷氧基和羟基; Q2选自H和(C1-C4)烷基; Q3选自H和(C1-C4)烷基或Q1和Q3连接形成杂环,并且一起代表(C 2 -C 3)亚烷基,而Z 1表示以纯对映异构体或混合物形式的键 以及其与酸的盐。
    • 3. 发明授权
    • Compounds bearing sulphamoyl and amidino radicals, their preparation
process and pharmaceutical compositions containing them
    • 带有氨磺酰基和脒基的化合物,其制备方法和含有它们的药物组合物
    • US5506258A
    • 1996-04-09
    • US195281
    • 1994-02-14
    • Bernard ChristopheLoic FoulonAlain PelletClaudine Serradeil-Le GalGerard Valette
    • Bernard ChristopheLoic FoulonAlain PelletClaudine Serradeil-Le GalGerard Valette
    • A61K31/16A61K31/155A61K31/18A61K38/00A61P9/00A61P25/00C07C311/18C07D215/36C07K1/113C07K5/06C07K5/065C07K5/078A61K31/40C07D295/192
    • C07K5/06078C07K5/06139A61K38/00
    • The subject of the invention is the compounds of formula I ##STR1## in which Ar.sub.1 represents naphtyl, phenyl, quinolyl or isoquinolyl optionally substituted;Ar.sub.2 represents a phenyl or thienyl optionally substituted;R.sub.1, R.sub.2 and R'.sub.2 are independently of each other, H or (C.sub.1 -C.sub.4)alkyl;R.sub.1 represents nothing and N is attached to Ar.sub.2, and optionally R.sub.2 and R'.sub.2 form a double bond; or R.sub.1 or R.sub.2 is attached to Ar.sub.2 and represents a (C.sub.1 -C.sub.3)alkylene;R.sub.3 and R.sub.4, which are identical or different, represent H, (C.sub.1 -C.sub.4)alkyl or form, with the nitrogen atom to which they are attached, a (C.sub.5 -C.sub.7) saturated heterocycle selected from pyrrolidine, piperidine and hexahydroazepine;Z.sub.1 represents a (C.sub.1 -C.sub.12)alkylene, optionally interrupted or extended by a (C.sub.5 -C.sub.7)cycloalkyl or phenyl;Q.sub.1 represents methyl, amino, alkoxycarbonylamino, alkylamino, dialkylamino, a (C.sub.5 -C.sub.7) saturated heterocyclic amino group, amidino, alkylamidino, guanidino, alkylguanidino, pyridyl, imidazolyl, pyrimidinyl, indolyl, hydroxy, alkoxy, (C.sub.2 -C.sub.8)alkoxycarbonyl, amino(C.sub.1 -C.sub.4)alkyl-N-(C.sub.1 -C.sub.4)alkylamino or carbamoyl, or phenyl optionally substituted;Q.sub.2 represents H or alkyl;Q.sub.3 represents H or (C.sub.1 -C.sub.4)alkyl;or Q.sub.1 and Q.sub.3 are attached to form a heterocycle and together represent a (C.sub.2) or (C.sub.3)alkylene, whereas Z.sub.1 represents nothing, in the form of pure enantiomers or mixtures thereof in any proportions, as well as their salts with acids.These compounds have an affinity for the biological receptors of neuropeptides Y (NPY), which are present in the central and peripheral nervous system.
    • 本发明的主题是其中Ar 1表示任选取代的萘基,苯基,喹啉基或异喹啉的式I化合物(I) Ar2表示任选取代的苯基或噻吩基; R 1,R 2和R'2彼此独立地为H或(C 1 -C 4)烷基; R1不表示,N与Ar2连接,任选地R 2和R'2形成双键; 或者R 1或R 2与Ar 2相连,表示(C1-C3)亚烷基; R3和R4相同或不同,代表H,(C1-C4)烷基或与其连接的氮原子一起形成选自吡咯烷,哌啶和六氢氮杂的(C5-C7)饱和杂环; Z1表示(C 1 -C 12)亚烷基,任选地被(C 5 -C 7)环烷基或苯基中断或延伸; Q1代表甲基,氨基,烷氧基羰基氨基,烷基氨基,二烷基氨基,(C5-C7)饱和杂环氨基,脒基,烷基脒基,胍基,烷基胍基,吡啶基,咪唑基,嘧啶基,吲哚基,羟基,烷氧基,(C2-C8)烷氧基羰基, 氨基(C 1 -C 4)烷基-N-(C 1 -C 4)烷基氨基或氨基甲酰基或任选取代的苯基; Q2表示H或烷基; Q3表示H或(C1-C4)烷基; 或Q 1和Q 3连接以形成杂环并且一起表示(C 2)或(C 3)亚烷基,而Z 1不以任何比例的纯对映异构体或其混合物的形式以及它们与酸的盐形式表示。 这些化合物对存在于中枢和外周神经系统中的神经肽Y(NPY)的生物受体具有亲和力。