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    • 1. 发明申请
    • NON-GLYCOSYLATED/NON-GLYCOSIDIC/NON-PEPTIDIC SMALL MOLECULE PSGL-1 MIMETICS FOR THE TREATMENT OF INFLAMMATORY DISORDERS
    • 非糖苷酸/非糖蛋白/非小分子小分子PSGL-1用于治疗炎症性疾病的物质
    • WO2005090284A1
    • 2005-09-29
    • PCT/EP2005/002920
    • 2005-03-18
    • REVOTAR BIOPHARMACEUTICALS AGKRANICH, RemoAYDT, Ewald, Mirko
    • KRANICH, RemoAYDT, Ewald, Mirko
    • C07C233/00
    • C07D307/68C07C235/34C07C235/38C07C237/22C07C2601/14C07D207/16C07D333/24
    • Pharmaceutical compositions comprising at least one compound of the formulas (Ia) or (Ib) and a pharmaceutically acceptable carrier which is useful in a medicine, formula (Ia) and formula (Ib), wherein the symbols, indices and substituents have the following meaning R 1 =H, CN, NO 2 , CF 3 , F, Cl, Br, I, CH 3 R 2 =H, CN, NO 2 , CF 3 , F, Cl, Br, I, CH 3 , Et, n-Pr, i-Pr, n-Bu, t-Bu, phenyl, thienyl, furyl, thiazolyl and either R 1 or R 2 must be H R 3 =H, CN, NO 2 , CF 3 , F, Cl, Br, I, CH 3 , Et, n-Pr, i-Pr, n-Bu, t-Bu, phenyl, thienyl, furyl, thiazolyl then X is e.g., formula (II), or, formula (III), with R 4 being H, CH 3 , CH 2 CH 3 or, formula (IV), or, formula (V), and Y being, formula (VI), or, formula (VII), or the pharmaceutically acceptable salts, esters or amides and prodrugs of the above identified compounds of formula (Ia) or (Ib). The compounds are applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.
    • 包含至少一种式(Ia)或(Ib)化合物的药物组合物和可用于药物,式(Ia)和式(Ib)的药学上可接受的载体,其中符号,指数和取代基具有以下含义 R 1 = H,CN,NO 2,CF 3,F,Cl,Br,I,CH 3 R 2 = H,CN,NO 2,CF 3,F,Cl,Br,I,CH 3,Et,n-Pr ,i-Pr,n-Bu,t-Bu,苯基,噻吩基,呋喃基,噻唑基,R 1或R 2必须为HR 3 = H,CN,NO 2,CF 3,F,Cl, Br,I,CH3,Et,n-Pr,i-Pr,n-Bu,t-Bu,苯基,噻吩基,呋喃基,噻唑基,则X是例如式(II)或式(III) 式(Ⅳ)或式(Ⅴ),Y为式(Ⅵ)或式(Ⅶ)或其药学上可接受的盐,酯或酰胺和前体药物 的上述式(Ia)或(Ib)的化合物。 该化合物被用于调节由E-,P-或L-选择蛋白结合介导的体外和体内结合过程。
    • 3. 发明申请
    • PROCESS FOR THE PREPARATION OF BIMOSIAMOSE
    • 制备双酚A的方法
    • WO2011138365A1
    • 2011-11-10
    • PCT/EP2011/057130
    • 2011-05-04
    • REVOTAR BIOPHARMACEUTICALS AGKRANICH, RemoBOCK, Daniel
    • KRANICH, RemoBOCK, Daniel
    • A61P11/00C07H15/203
    • C07H15/203
    • A process for the preparation of 1,6-Bis-[3-(3-carboxymethylphenyl)-4-(2-α-D-mannopyranosyloxy)-phenyl] hexane (I) which comprises the steps of converting the compound (2'-Methoxy-biphenyl-3-yl)-acetic acid (A) into the (2'-Methoxy-biphenyl-3-yl)-acetic acid ethyl ester, which is reacted with adipoyl chloride to 1,4-Bis-[3-(3-carboethoxymethylphenyl)-4-methoxybenzoyl]-butane (B) which is catalytically reduced to 1,6-Bis-[3-(3-carboethoxy-methylphenyl)-4-methoxy- phenyl] -hexane (C), which is reacted with boron tribromide in a solvent to 1,6-Bis-[3-(3- carboethoxy-methylphenyl)-4-hydroxyphenyl]-hexane (D), which is reacted with a mannopyranosyl derivative to obtain 1,6-Bis-[3-(3-carboethoxy-methylphenyl)-4-(tetra-0- pivaloyl-α-D-mannopyranosyloxy)-phenyl]-hexane (E), which is reacted to form 1,6-Bis- [3-(3-carboxymethyl-phenyl)-4-(2-α-D-mannopyranosyloxy)-phenyl] hexane, which is re- crystallized, leads to the product (I) with high purity.
    • 制备1,6-双 - [3-(3-羧甲基苯基)-4-(2-aD-甘露吡喃糖基氧基) - 苯基]己烷(I)的方法,其包括将化合物(2'-甲氧基 - 联苯-3-基) - 乙酸(A)加入到(2'-甲氧基 - 联苯-3-基) - 乙酸乙酯中,将其与己二酰氯与1,4-双[3-( (3-乙氧羰基甲基苯基)-4-甲氧基苯甲酰基]丁烷(B),其被催化还原成1,6-双 - [3-(3-乙酰氧基 - 甲基苯基)-4-甲氧基 - 苯基] - 己烷(C) 与三溴化硼在溶剂中与1,6-双 - [3-(3-乙酰氧基 - 甲基苯基)-4-羟基苯基] - 己烷(D)反应,其与甘草吡喃糖基衍生物反应,得到1,6-双 - [3-(3-乙酰氧基 - 甲基苯基)-4-(四-O-新戊酰基-DA-甘露吡喃糖基氧基) - 苯基] - 己烷(E),其反应形成1,6-双 - [3- 羧甲基 - 苯基)-4-(2-aD-甘露吡喃糖基氧基) - 苯基]己烷重结晶,得到高纯度的产物(I)。
    • 10. 发明公开
    • NON-GLYCOSYLATED/NON-GLYCOSIDIC/NON-PEPTIDIC SMALL MOLECULE PSGL-1 MIMETICS FOR THE TREATMENT OF INFLAMMATORY DISORDERS
    • 非糖基化/ NICHTGLYCOSIDISCHE /非肽的低分子PSGL-1模拟物用于治疗炎性疾病治疗的
    • EP1732882A1
    • 2006-12-20
    • EP05716209.1
    • 2005-03-18
    • Revotar Biopharmaceuticals AG
    • KRANICH, RemoAYDT, Ewald, Mirko
    • C07C233/00C07C237/00
    • C07D307/68C07C235/34C07C235/38C07C237/22C07C2601/14C07D207/16C07D333/24
    • Pharmaceutical compositions comprising at least one compound of the formulas (Ia) or (Ib) and a pharmaceutically acceptable carrier which is useful in a medicine, formula (Ia) and formula (Ib), wherein the symbols, indices and substituents have the following meaning R1=H, CN, NO2, CF3, F, Cl, Br, I, CH3 R2=H, CN, NO2, CF3, F, Cl, Br, I, CH3, Et, n-Pr, i-Pr, n-Bu, t-Bu, phenyl, thienyl, furyl, thiazolyl and either R1 or R2 must be H R3=H, CN, NO2, CF3, F, Cl, Br, I, CH3, Et, n-Pr, i-Pr, n-Bu, t-Bu, phenyl, thienyl, furyl, thiazolyl then X is e.g., formula (II), or, formula (III), with R4 being H, CH3, CH2CH3 or, formula (IV), or, formula (V), and Y being, formula (VI), or, formula (VII), or the pharmaceutically acceptable salts, esters or amides and prodrugs of the above identified compounds of formula (Ia) or (Ib). The compounds are applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.
    • 药物组合物包括下式的至少一种化合物(Ia)或(Ib)和药学可接受的载体的所有这在医学worin符号,指数有用和取代基具有以下含义R1═H,CN,NO 2,CF 3,F ,氯,溴,I,CH 3R2═H,CN,NO 2,CF 3,F,氯,溴,I,CH 3,等,正PR,I-PR,正丁基,叔卜,苯基,噻吩基, 呋喃基,噻唑基和R 1或R 2必须是HR3═H,CN,NO 2,CF 3,F,氯,溴,I,CH 3,等,正PR,I-PR,正丁基,叔卜,苯基 ,噻吩基,呋喃基,噻唑基,则X是例如 与R4为H,CH 3,CH 2 CH 3或Y是或其药学上可接受的盐,酯或酰胺和式(Ia)或(Ib)的上述确定的化合物的前药。 这些化合物适用于调节在体外和由E-,P-或L-选择素结合所介导的体内结合过程。