Unsymmetrical cyclic diamine compound
    2.
    发明授权
    Unsymmetrical cyclic diamine compound 失效
    不对称环状二胺化合物

    公开(公告)号:US06552188B2

    公开(公告)日:2003-04-22

    申请号:US09893699

    申请日:2001-06-29

    IPC分类号: A61K31496

    摘要: Cyclic diamine compounds of formula (1) are disclosed: wherein A is (CH2)n, (CH2)n—CH═CH, CO—(CH2)n or CO—(CH2)n—CH═CH, in which n is a number of 0 to 3; Z represents a formula (2) or (3): in which R1, R2, R4, R5 and R6 are individually a hydrogen atom, alkyl group, alkoxy group, halogen atom or nitro group; R3is a hydrogen atom, alkyl group, alkoxy group, halogen atom, nitro group, naphthyl group, or phenyl group which may be substituted by 1 to 3 substituents selected from the group consisting of alkyl groups, alkoxy groups, halogen atoms, a nitro group and a phenyl group; and X and Y are individually CH or a nitrogen atom; and m is 1 or 2; an acid-addition salt thereof, or a hydrate thereof, and a medicine containing such a compound.

    摘要翻译: 公开了式(1)的环二胺化合物:其中A是(CH 2)n,(CH 2)n -CH = CH,CO-(CH 2)n或CO-(CH 2)n -CH = CH,其中n是 数字0到3; Z表示式(2)或(3):其中R1,R2,R4,R5和R6分别为氢原子,烷基,烷氧基,卤素原子或硝基; R3是氢原子,烷基,烷氧基,卤素原子,硝基,萘基或可以被1〜3个选自烷基,烷氧基,卤原子,硝基的取代基取代的苯基 和苯基; X和Y分别是CH或氮原子; m为1或2;其酸加成盐或其水合物,以及含有这种化合物的药物。

    Cyclic diamine compound with 5-membered ring groups
    5.
    发明授权
    Cyclic diamine compound with 5-membered ring groups 失效
    具有5元环基团的环状二胺化合物

    公开(公告)号:US06472386B1

    公开(公告)日:2002-10-29

    申请号:US09893682

    申请日:2001-06-29

    IPC分类号: A61K31551

    摘要: A compound of formula (1): wherein A is a single bond, C≡C, CONH or NHCO; W is a carbon atom or a nitrogen atom; X is CH, a nitrogen atom, an oxygen atom or a sulfur atom; Y is CH, CHR1, in which R1 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy-lower-alkyl, aryl, aryl-lower-alkyl or heteroaryl-lower-alkyl group, a nitrogen atom, an oxygen atom, a sulfur atom or NR2, in which R2 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy-lower-alkyl, aryl, aryl-lower-alkyl or heteroaryl-lower-alkyl group; Z is a nitrogen atom, an oxygen atom, a sulfur atom, CH or NR3, in which R3 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy-lower-alkyl, aryl, aryl-lower-alkyl or heteroaryl-lower-alkyl group; m is 1 or 2; and n is a number of 1 to 5, with the proviso that one or two of W, X, Y and Z are heteroatoms; an acid-addition salt thereof, or a hydrate thereof. The compounds have inhibitory effects on cell adhesion and are useful for prevention or treatment of diseases such as allergy, asthma, rheumatism, arteriosclerosis and inflammation.

    摘要翻译: 式(1)的化合物:其中A是单键,C = C,CONH或NHCO; W是碳原子或氮原子; X是CH,氮原子,氧原子或硫原子; Y是CH,CHR1,其中R1是氢原子,或低级烷基,羟基低级烷基,低级烷氧基 - 低级 - 烷基,芳基,芳基 - 低级 - 烷基或杂芳基 - 低级 - 烷基,氮原子, 氧原子,硫原子或NR 2,其中R2是氢原子,或低级烷基,羟基低级烷基,低级烷氧基 - 低级 - 烷基,芳基,芳基 - 低级 - 烷基或杂芳基 - 低级 - 烷基; Z是氮原子,氧原子,硫原子,CH或NR 3,其中R3是氢原子,或低级烷基,羟基低级烷基,低级烷氧基 - 低级 - 烷基,芳基,芳基 - 低级 - 烷基或 杂芳基 - 低级烷基; m为1或2; 并且n是1至5的数,条件是W,X,Y和Z中的一个或两个是杂原子; 其酸加成盐或其水合物。 这些化合物对细胞粘附具有抑制作用,可用于预防或治疗诸如过敏,哮喘,风湿病,动脉硬化和炎症等疾病。

    Piperazine derivative
    10.
    发明授权
    Piperazine derivative 失效
    哌嗪衍生物

    公开(公告)号:US06432957B1

    公开(公告)日:2002-08-13

    申请号:US09893681

    申请日:2001-06-29

    IPC分类号: A61K31496

    摘要: A piperazine compound represented by formula (1): wherein X is —CH2—, —C(O)— or —CH(CH3)—; R1 is a hydrogen atom or alkyl group; and R2 is a hydrogen atom, alkyl group, hydroxyalkyl group, arylalkyl group, heteroarylalkyl group, carboxyalkyl group, carboxamidoalkyl group, aminoalkyl group or guanidinoalkyl group; an acid-addition salt thereof, or a hydrate thereof. The compound has excellent inhibitory effects on both cell adhesion and cell infiltration and is useful for prevention or treatment of diseases such as allergy, asthma, rheumatism, arteriosclerosis and inflammation.

    摘要翻译: 由式(1)表示的哌嗪化合物:其中X是-CH 2 - , - C(O) - 或-CH(CH 3) - ; R1是氢原子或烷基; R2是氢原子,烷基,羟基烷基,芳基烷基,杂芳基烷基,羧基烷基,甲酰胺基烷基,氨基烷基或胍基烷基; 其酸加成盐或其水合物。 该化合物对细胞粘附和细胞浸润具有优异的抑制作用,可用于预防或治疗过敏,哮喘,风湿病,动脉硬化和炎症等疾病。