会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 1. 发明授权
    • 20-alkyl-7-oxoprostacyclin derivatives useful as pharmaceuticals
    • 可用作药物的20-烷基-7-氧代前列环素衍生物
    • US5190973A
    • 1993-03-02
    • US599916
    • 1990-10-19
    • Robert NickolsonHelmut VorbrueggenClaus S. StuerzebecherMartin Haberey
    • Robert NickolsonHelmut VorbrueggenClaus S. StuerzebecherMartin Haberey
    • C07C405/00C07D307/935C07D307/937
    • C07D307/935C07C405/00C07D307/937
    • The invention concerns 20-alkyl-7-oxoprostacyclin derivatives of general Formula I ##STR1## wherein R.sub.1 is the residue OR.sub.3 where R.sub.3 means hydrogen or alkyl of 1-10 carbon atoms optionally substituted by halogen, phenyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -dialkylamino; cycloalkyl, aryl or a heterocyclic residue, or the residue NHR.sub.4 where R.sub.4 means hydrogen or an alkanoyl or alkanesulfonyl residue of respectively 1-10 carbon atoms,n is 1 or 2,A is a CH.sub.2 --CH.sub.2 --, cis--CH.dbd.CH-- or trans--CH.dbd.CH--group,W is a ##STR2## or a ##STR3## wherein the OH-group can respectively be esterified with a benzoyl or alkanoic acid residue of 1-4 carbon atoms, or etherified with a tetrahydropyranol, tetrahydrofuranyl, alkoxyalkyl or trialkylsilyl residue, wherein the free or esterified OH-group can be in the .alpha.- or .beta.-position,R.sub.2 is a straight-chain or branched-chain alkyl group of 1-6 carbon atoms,R.sub.5 is a hydroxy group which can be esterified with an alkanoic acid residue of 1-4 carbon atoms or etherified with a tetrahydropyranyl, tetrahydrofuranyl, alkoxyalkyl or trialkylsilyl residue,R.sub.6 and R.sub.7 are hydrogen or a straight-chain or branched-chain alkyl group of 1-4 carbon atoms, or R.sub.6 and R.sub.7 jointly represent a trimethylene group,R.sub.8 and R.sub.9 jointly represent a linkage or hydrogen or a straight-chain or branched-chain alkyl group of 1-4 carbon atoms,and, if R.sub.3 is hydrogen, the salts thereof with physiologically compatible bases; their production; and their use as medicinal agents.
    • 本发明涉及通式I(I)的20-烷基-7-氧代前列环素衍生物,其中R 1是残基OR 3,其中R 3表示氢或1-10个碳原子的任选被卤素,苯基,C 1 -C 4 - 烷氧基或C 1 -C 4 - 二烷基氨基; 环烷基,芳基或杂环残基,或残基NHR4,其中R4表示氢或分别为1-10个碳原子的烷酰基或烷磺酰基,n为1或2,A为CH2-CH2-,顺式-CH = CH- 或反式-CH = CH-基团,W为“IMAGE”或“IMAGE”,其中OH基团可分别用1-4个碳原子的苯甲酰基或链烷酸残基酯化,或用四氢吡喃醇醚化,四氢呋喃基 ,烷氧基烷基或三烷基甲硅烷基残基,其中游离或酯化的OH基可以是α或β-位,R2是1-6个碳原子的直链或支链烷基,R5是羟基, 可以用1-4个碳原子的链烷酸残基酯化,或与四氢吡喃基,四氢呋喃基,烷氧基烷基或三烷基甲硅烷基残基醚化,R6和R7是氢或1-4个碳原子的直链或支链烷基, 或R6和R7共同表示三亚甲基,R8和R9共同表示键或 氢或1-4个碳原子的直链或支链烷基,如果R 3是氢,则其与生理上相容的碱的盐; 他们的生产; 并将其用作药剂。
    • 5. 发明授权
    • N-oxide anthranylamide derivatives and their use as medicaments
    • N-氧化物苯甲酰胺衍生物及其作为药物的用途
    • US07459470B2
    • 2008-12-02
    • US10476755
    • 2002-05-03
    • Alexander ErnstAndreas HuthMartin KruegerKarl-Heniz ThierauchAndreas MenradMartin Haberey
    • Alexander ErnstAndreas HuthMartin KruegerKarl-Heniz ThierauchAndreas MenradMartin Haberey
    • A61K31/47C07D213/89
    • C07D213/89C07D401/12C07D405/12
    • Substituted N-oxidanthranilamide derivatives, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis are described. The compounds according to the invention can be used as or in the case of psoriasis, Kaposi's sarcoma, restenosis, endometriosis, Crohn's disease, Hodgkin's disease, leukemia; arthritis, such as rheumatoid arthritis, hemangioma, angiofibroma; eye diseases, such as diabetic retinopathy, neovascular glaucoma; renal diseases, such as glomerulonephritis, diabetic nephropathy, malignant nephrosclerosis, thrombic microangiopathic syndrome, transplant rejections and glomerulopathy; fibrotic diseases, such as cirrhosis of the liver, mesangial cell proliferative diseases, arteriosclerosis, injuries to nerve tissue, and inhibition of the reocclusion of vessels after balloon catheter treatment, in vascular prosthetics or after mechanical devices are used to keep vessels open, such as, e.g., stents, as immunosuppressive agents, as a support in scar-free healing, senile keratosis and contact dermatitis. The compounds according to the invention can also be used as VEGFR-3 inhibitors in the case of lymphangiogenesis.
    • 描述了取代的N-氧化邻氨基苯甲酰胺衍生物,其作为用于治疗由持续性血管生成触发的疾病的药剂的生产和用途被描述。 根据本发明的化合物可以用作银屑病,卡波西肉瘤,再狭窄,子宫内膜异位症,克罗恩病,霍奇金病,白血病,牛皮癣, 关节炎,如类风湿关节炎,血管瘤,血管纤维瘤; 眼睛疾病如糖尿病性视网膜病变,新生血管性青光眼; 肾脏疾病如肾小球性肾炎,糖尿病肾病,恶性肾硬化,血栓性微血管病综合征,移植排斥反应和肾小球病; 纤维化疾病,如肝硬化,肾小球膜细胞增生性疾病,动脉硬化,神经组织损伤,以及球囊导管治疗后血管再狭窄的抑制,血管修复术或机械装置用于保持血管开放的诸如 例如作为免疫抑制剂的支架,作为无疤痕愈合的支持,老年角化病和接触性皮炎。 在淋巴管生成的情况下,根据本发明的化合物也可以用作VEGFR-3抑制剂。