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    • 2. 发明授权
    • 2-아릴 프로피온산 및 이를 함유하는 약제학적 조성물
    • 2-아릴프로피온산및이를함유하는약제학적조성물
    • KR101060064B1
    • 2011-08-29
    • KR1020107017598
    • 2002-11-19
    • 돔페 파르마 에스.피.에이.
    • 알레그레티,마르첼로세스타,마리아칸디다베르티니,리카르도비짜리,신지아콜로타,프란세스코
    • A61K31/192C07C57/42C07C63/08A61P29/00
    • A61K31/192A61K31/196C07C57/30C07C57/38C07C57/42C07C57/46C07C57/58C07C59/135C07C59/48C07C229/42C07C307/02C07C307/10C07C309/65C07C309/67C07C309/73C07C311/08C07C311/09C07C311/21C07C317/44
    • (R,S)-2-Aryl-propionic acids are useful as inhibitors of interleukin-8 induced human polymorphonucleated neutrophils (PMN) chemotaxis. (R,S)-2-Aryl-propionic acids of formula (I), their single (R) and (S) enantiomers or salts are useful as inhibitors of interleukin-8 (IL-8) induced human polymorphonucleated neutrophils (PMN) chemotaxis. [Image] Ar : phenyl ring (substituted by T in meta position, T1 in para position or T2 in ortho position); T : linear or branched 1-5C alkyl, 2-5C alkenyl, or 2-5C alkynyl (optionally substituted by 1-5C alkoxycarbonyl, optionally substituted phenyl, linear or branched 1-5C hydroxyalkyl or arylhydroxymethyl); T1benzoyloxy, benzoylamino, benzenesulfonyloxy, benzenesulfonylamino, benzenesulfonylmethyl (all optionally substituted), 1-5C acyloxy, 1-5C acylamino, 1-5C sulfonyloxy, 1-5C alkanesulfonylamino, 1-5C alkanesulfonylmethyl, 3-6C cycloalkyl, 2-furyl, 3-tetrahydrofuryl, 2- thiophenyl, 2-tetrahydrothiophenyl or ((1-8C)-alkanoyl, -cycloalkanoyl or -arylalkanoyl)-1-5C-alkylamino (preferably acetyl-N-methyl-amino or pivaloyl-N-ethyl-amino); and T2arylmethyl, aryloxy or acylamino (all optionally substituted by 1-4C alkyl, 1-4C-alkoxy, chlorine, fluorine or trifluoromethyl). The meta linear or branched 1-5C alkyl together with a substituent in ortho or para position and the benzene ring forms optionally saturated or optionally substituted bicyclo aryls. INDEPENDENT CLAIM are included for the following: (1) preparation of (I); and (2) use of (I) in the preparation of a medicament for the treatment of e.g. psoriasis, ulcerative colitis, melanoma and chronic obstructive pulmonary disease (COPD). - ACTIVITY : Antipsoriatic; Antiulcer; Respiratory-Gen.; Antirheumatic; Antiarthritic; Nephrotropic; Vasotropic; Antiinflammatory; Gastrointestinal-Gen.; Cytostatic. - MECHANISM OF ACTION : Interleukin-8 (IL-8) inhibitor; GROalpha inhibitor; CXCR2 agonist/antagonist. The ability of (R,S) 2-[(3'-isopropyl)phenyl]propionic acid (A) to inhibit IL-8 induced chemotaxis of human monocytes was tested as described in Van Damme J. et al. (Eur. J. Immunol., 19, 2367, 1989). (A) showed inhibition (%) of 51+-12.
    • (R,S)-2-芳基 - 丙酸可用作白细胞介素-8诱导的人多形核中性粒细胞(PMN)趋化性的抑制剂。 (I)的(R,S)-2-芳基 - 丙酸,它们的单(R)和(S)对映体或盐可用作白细胞介素-8(IL-8)诱导的人多形核中性粒细胞(PMN) 趋化作用。 Ar:苯环(由间位T取代,对位取代T1或邻位T2取代); T:直链或支链1-5C烷基,2-5C链烯基或2-5C炔基(任选被1-5C烷氧基羰基,任选取代的苯基,直链或支链1-5C羟烷基或芳基羟甲基取代); 苯磺酰基氨基,苯磺酰基甲基(全部任选被取代),1-5C酰氧基,1-5C酰基氨基,1-5C磺酰氧基,1-5C烷基磺酰基氨基,1-5C烷基磺酰基甲基,3-6C环烷基,2-呋喃基,3 ((1-8C) - 烷酰基,环烷酰基或 - 芳基烷酰基)-1-5C-烷基氨基(优选乙酰基-N-甲基 - 氨基或新戊酰基-N-乙基 - 氨基) ; 和二芳基甲基,芳氧基或酰氨基(全部任选被1-4C烷基,1-4C-烷氧基,氯,氟或三氟甲基取代)。 间位直链或支链1-5C烷基与邻位或对位的取代基一起形成并且苯环任选地形成饱和的或任选取代的双环芳基。 独立请求包括以下内容:(1)准备(I); 和(2)(I)在制备用于治疗例如心脏病的药物中的用途。 牛皮癣,溃疡性结肠炎,黑素瘤和慢性阻塞性肺病(COPD)。 - 活动:抗牛皮癣; 抗溃疡; 呼吸根; 抗风湿; 抗关节炎; Nephrotropic; Vasotropic; 抗炎; 胃肠道根; 抑制细胞生长。 - 作用机制:白细胞介素-8(IL-8)抑制剂; GROalpha抑制剂; CXCR2激动剂/拮抗剂。 如Van Damme J.等人所述测试(R,S)2 - [(3'-异丙基)苯基]丙酸(A)抑制IL-8诱导的人单核细胞趋化性的能力。 (Eur.J.Immunol。,19,2367,1989)。 (A)显示51±12的抑制(%)。
    • 10. 发明公开
    • 펜에틸 벤조에이트 유도체 및 그의 제조방법
    • 苯乙烯衍生物及其制备方法
    • KR1020080036734A
    • 2008-04-29
    • KR1020060103352
    • 2006-10-24
    • 인제대학교 산학협력단
    • 이범종손은미구경아이찬우김한성
    • C07C63/08C07C69/773C07C69/78
    • A phenethyl benzoate derivative, and a method for preparing the phenethyl benzoate derivative are provided to obtain a novel phenethyl benzoate derivative having a hydroxyl group at the 2 and/or 3-positions. A phenethyl benzoate derivative is represented by the formula 1, wherein R1 to R14 are identical or different one another and are H, a halogen atom, a carboxyl group, an amino group, a nitro group, a cyano group, a substituted or unsubstituted C1-C20 alkyl group, a substituted or unsubstituted C1-C20 alkoxy group, a substituted or unsubstituted C2-C20 alkenyl group, a substituted or unsubstituted C2-C20 alkynyl group, a substituted or unsubstituted C1-C20 heteroalkyl group, a substituted or unsubstituted C6-C30 aryl group, a substituted or unsubstituted C7-C30 arylalkyl group, a substituted or unsubstituted C5-C30 heteroaryl group, or a substituted or unsubstituted C3-C30 heteroarylalkyl group, and at least of them can be combined to form a five, six or seven-membered ring, but at least one of R6, R7, R9 and R10 is a hydroxyl group.
    • 提供苯甲酸苯乙酯衍生物,以及制备苯甲酸苯乙酯衍生物的方法,以获得在2和/或3-位具有羟基的新型苯乙酸苯乙酯衍生物。 苯甲酸苯乙酯衍生物由式1表示,其中R 1至R 14彼此相同或不同,为H,卤素原子,羧基,氨基,硝基,氰基,取代或未取代的C1 -C 20烷基,取代或未取代的C 1 -C 20烷氧基,取代或未取代的C 2 -C 20烯基,取代或未取代的C 2 -C 20炔基,取代或未取代的C 1 -C 20杂烷基,取代或未取代的C 6 -C 30芳基,取代或未取代的C 7 -C 30芳烷基,取代或未取代的C 5 -C 30杂芳基或取代或未取代的C 3 -C 30杂芳基烷基,并且至少它们可以组合形成五 或七元环,但R 6,R 7,R 9和R 10中的至少一个为羟基。