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    • 4. 发明申请
    • CYCLOPEPTIDE DERIVATIVES
    • CYCLO肽衍生物
    • WO1997014716A1
    • 1997-04-24
    • PCT/EP1996004462
    • 1996-10-14
    • MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER HAFTUNGJONCZYK, AlfredGOODMAN, Simon, LawrenceDIEFENBACH, BeateSUTTER, ArneKESSLER, Horst
    • MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER HAFTUNG
    • C07K14/75
    • C07K7/64A61K38/00C07K14/75Y02P20/55
    • The invention relates to compounds of the formula (I) R -Q -X-Q -R , in which: Q , Q , each independent of one another, are missing or are -NH-(CH2)n-CO-; R , R , each independent of one another, are missing or are cyclo-(Arg-Gly-Asp-Z), wherein Z is missing in the side chain of Q or Q or if Q and/or Q are missing, is bound to X, at least one of the groups R or R always having to be included; X is -CO-R -CO-, and if R -Q - or R -Q - are missing is R , R , R , Het-CO or a fluorescent pigment residue linked through a -CONH-, -COO-, -NH-C(=S)-NH-, -NH-C(=O)-NH-, -SO2NH- or -NHCO- bond; and Z, R , R , R , R , Het and n have the meanings given in claim 1. The invention also relates to the salts of said compounds. Said compounds and their salts can be used as integrin inhibitors, in particular for the prevention and treatment of circulatory diseases, thrombosis, heart infarct, coronary heart diseases, arteriosclerosis, angiogenic diseases and in tumour therapy.
    • 式(I)R <1> -Q <1> -XQ <2> -R <2>其中Q <1>,Q <2>各自独立地不存在或-NH-(CH 2)N-CO-的化合物 ,R <1>,R <2>不存在各自独立地为或环 - (Arg - 甘氨酸 - 天冬氨酸-Z),其中Z在侧链至Q <1>或Q <2>,或者,如果Q <1>,和 /或Q <2>不存在,键合至X,并且其中R中的至少一个<1>或R <2>必须始终包含的,X是-CO-R <18> - CO-和如果R <1 > -Q <1> - 或R <2> -Q <2> - 缺失 - [R <10>,R <13>,R <16>中,Het-CO,或经由-CONH-,-COO - , - NH-C(= S)-NH-,-NH-C(= O)-NH - , - SO 2 NH-或-NHCO-键连接的荧光染料基团,和Z,R <10>,R <13>, [R <16>,R <18>中,Het和n具有权利要求1中给出的含义和它们的盐可以用作整联蛋白抑制剂,特别是用于循环,血栓形成障碍,心肌梗死,冠状动脉心脏疾病,动脉硬化症的预防和治疗, 血管生成病症和在肿瘤治疗中使用。
    • 8. 发明申请
    • LIQUID-CRYSTAL COMPOUNDS
    • 液晶化合物
    • WO1992013928A1
    • 1992-08-20
    • PCT/EP1992000270
    • 1992-02-07
    • MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER ...REIFFENRATH, VolkerPLACH, HerbertPAULUTH, DetlefHITTICH, ReinhardPOETSCH, EikeGEELHAAR, ThomasWEBER, GeorgBARTMANN, Ekkehard
    • MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER ...
    • C09K19/30
    • C07C17/2635C07C17/269C07C17/354C07C25/18C07C25/24C07C39/42C07C43/1747C07C43/192C07C43/225C07C63/72C07C69/76C07C2601/14C09K19/12C09K19/3003C09K19/3028C09K19/3048C09K2019/0407C09K2019/0444C07C21/18
    • Described are liquid-crystal compounds of formula (I), in which R may be H, an alkyl or alkylene group with 1 to 15 C-atoms which is unsubstituted or which is substituted with a single CN or CF3 group or with at least one halogen atom, whereby one or more CH2 groups in these alkyl or alkylene groups may be replaced, independently of each other, by -O-, -S-, - -, -CO-, -CO-O-, O-CO- or -O-CO-O in such a way that O-atoms are not bonded directly to each other; Z1 and Z, independently of each other, may be -CH2CH2-, -CH=CH-, -C=C- or a single bond, whereby one of the groups Z1 and Z may also be -(CH2)4 or -CH=CH-CH2CH2-; A and A1, independently of each other, may be the trans-1,4-cyclohexylene group (in which one or two non-adjacent CH2 groups may be replaced by -O-), an unsubstituted 1,4-phenylene group or a 1,4-phenylene group substituted with one or two F and/or Cl atoms, wherein one or two CH groups may be replaced by N; m may be 0, 1, 2 or 3; o and s may be 0, 1 or 2, with the provision that s + o >/= 2; W may be -O-, -COO- or a single bond; Q may be -O-, -CH=CH- or a single bond; r may be from 1 to 7; t may be from 0 to 7; and Y may be F, Cl, CF3, OCF3, CHF2, OCHF2 or OCH2F. Such compounds are suitable for use as components of liquid-crystal media.
    • 描述了式(I)的液晶化合物,其中R可以是H,具有1至15个C原子的烷基或亚烷基是未取代的或被单个CN或CF 3基团取代或至少一个 卤素原子,其中这些烷基或亚烷基中的一个或多个CH 2基团可以彼此独立地被-O - , - S - , - , - , - CO - , - CO-O-,O -CO-或-O-CO-O,使得O原子彼此不直接键合; Z 1和Z彼此独立地可以是-CH 2 CH 2 - , - CH = CH - , - C = C-或单键,其中基团Z 1和Z中的一个也可以是 - (CH 2)4或-CH = CH-CH 2 CH 2; A和A1彼此独立地可以是反式-1,4-亚环己基(其中一个或两个不相邻的CH 2基可被-O-取代),未取代的1,4-亚苯基或 被一个或两个F和/或Cl原子取代的1,4-亚苯基,其中一个或两个CH基团可被N代替; m可以是0,1,2或3; o和s可以是0,1或2,其规定为s + o> / = 2; W可以是-O-,-COO-或单键; Q可以是-O - , - CH = CH-或单键; r可以是1到7; t可以是0到7; Y可以是F,Cl,CF 3,OCF 3,CHF 2,OCHF 2或OCH 2 F。 这些化合物适合用作液晶介质的组分。