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    • 1. 发明授权
    • Nitrile derivatives that inhibit cathepsin K
    • 抑制组织蛋白酶K的腈衍生物
    • US06531612B2
    • 2003-03-11
    • US09745675
    • 2000-12-21
    • Tobias GabrielMichael PechSabine Wallbaum
    • Tobias GabrielMichael PechSabine Wallbaum
    • C07D20716
    • C07D403/06C07D207/16C07D207/48C07D209/52C07D277/06C07D405/12C07D405/14
    • Compounds of the formula: wherein R1 to R7 and Y are as defined in the specification, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof, are useful for treating diseases associated with cystein proteases, such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.
    • 下式的化合物:其中R 1至R 7和Y如说明书中所定义,及其药学上可接受的盐和/或其药学上可接受的酯可用于治疗与半胱氨酸蛋白酶相关的疾病,例如骨质疏松症,骨关节炎,类风湿性关节炎,肿瘤 转移,肾小球性肾炎,动脉粥样硬化,心肌梗塞,心绞痛,不稳定性心绞痛,中风,斑块破裂,短暂性脑缺血发作,黑素瘤假体,外周动脉闭塞性疾病,血管成形术后再狭窄和支架置入,腹主动脉瘤形成,炎症,自身免疫性疾病, 疟疾,眼底组织细胞病变和呼吸系统疾病。
    • 10. 发明授权
    • Sulfuric acid esters of sugar alcohols
    • 糖醇的硫酸酯
    • US5830920A
    • 1998-11-03
    • US639986
    • 1996-04-26
    • Alexander ChucholowskiJurgen FingerleNiggi IbergHans Peter MarkiRita MullerMichael PechMarianne RougeGerard SchmidThomas TschoppHans Peter Wessel
    • Alexander ChucholowskiJurgen FingerleNiggi IbergHans Peter MarkiRita MullerMichael PechMarianne RougeGerard SchmidThomas TschoppHans Peter Wessel
    • C07D251/70A61K31/165A61K31/27A61K31/35A61K31/352A61K31/53A61K31/70A61K31/7028A61P7/02A61P9/10A61P31/12A61P43/00C07C305/06C07C305/10C07D311/22C07H15/18A61K31/045C07C205/00
    • C07H15/18C07C305/06C07C305/10
    • Compounds of the formula ##STR1## wherein n.sup.1 -n.sup.9 are each independently 0 or 1; m.sup.1 -m.sup.9 are each independently 0 or 1, but with the proviso that at least one of m.sup.1, m.sup.2 and m.sup.3, at least one of m.sup.4, m.sup.5 and m.sup.6 and, when present, at least one of m.sup.7, m.sup.8 and m.sup.9 is 1; and wherein X.sup.1 -X.sup.18 each independently is --O--, --CONR.sup.1,--NR.sup.1 CO-- or --NR.sup.1 --; R.sup.1 is hydrogen or lower alkyl; W is a benzene or s-triazine; Y.sup.1 -Y.sup.9 each independently is an aromatic ring systems; A.sup.1 -A.sup.3 each independently is a residue of a sugar alcohol devoid of the 1-hydroxy group or a derivative thereof, a residue of a sugar acid devoid of the 1-carboxy group or a derivative thereof or tris-(hydroxymethyl)-methyl; D is the di-residue of a sugar alcohol devoid of 2 hydroxy groups or a derivative thereof or the di-residue of a sugar dicarboxylic acid devoid of 2 carboxy group or a derivative thereof; Q.sup.1 -Q.sup.3 and Z.sup.1 -Z3 each independently are the di-residue of a sugar alcohol devoid of 2 hydroxy groups or a derivative thereof or the di-residue of a sugar dicarboxylic acid devoid of 2 carboxy groups or a derivative thereof or didesoxyglycopyranoside or a derivative thereof, wherein at least one hydroxy group of residues A.sup.1 -A.sup.3, D, Q.sup.1 -Q.sup.3 and Z.sup.1 -Z.sup.3 is esterified with sulfuric acid, and pharmaceutically usable salts thereof are useful for the treatment of disorders which are characterized by excessive or destructive proliferation of smooth muscle cells.
    • 式Ia的化合物或其中n1-n9各自独立地为0或1; m1-m9各自独立地为0或1,但条件是m1,m2和m3中的至少一个,m4,m5和m6中的至少一个,并且当存在时,m7,m8和m9中的至少一个为1 ; 并且其中X1-X18各自独立地为-O - , - CONR1,-NR1CO-或-NR1-; R1是氢或低级烷基; W是苯或s-三嗪; Y1-Y9各自独立为芳环体系; A1-A3各自独立地为不含1-羟基或其衍生物的糖醇的残基,不含1-羧基的糖酸或其衍生物的残基或三 - (羟甲基) - 甲基; D是不含2个羟基的糖醇或其衍生物或不含2个羧基的糖二羧酸的二残基或其衍生物的二残基; Q1-Q3和Z1-Z3各自独立地为不含2个羟基的糖醇或其衍生物或不含2个羧基的糖二羧酸的二残基或其衍生物或二脱氧吡喃葡萄糖苷或二 其衍生物,其中残基A1-A3,D,Q1-Q3和Z1-Z3中的至少一个羟基用硫酸酯化,其药学上可用的盐可用于治疗以过度或破坏性增殖为特征的病症 的平滑肌细胞。