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    • 11. 发明授权
    • Piperidine derivatives useful as CCR5 antagonists
    • 哌啶衍生物可用作CCR5拮抗剂
    • US06387930B1
    • 2002-05-14
    • US09562815
    • 2000-05-01
    • Bahige M. BaroudyJohn W. CladerHubert B. JosienStuart W. McCombieBrian A. McKittrickMichael W. MillerBernard R. NeustadtAnandan PalaniRuo SteensmaJayaram R. TagatSusan F. ViceMark A. Laughlin
    • Bahige M. BaroudyJohn W. CladerHubert B. JosienStuart W. McCombieBrian A. McKittrickMichael W. MillerBernard R. NeustadtAnandan PalaniRuo SteensmaJayaram R. TagatSusan F. ViceMark A. Laughlin
    • C07D40104
    • C07D401/14C07D211/58C07D413/14C07D417/14
    • The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein X is —C(R13)2—, —C(R13)(R19)—, —C(O)—, —O—, —NH—, —N(alkyl)—, R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is H, alkyl or alkenyl; R2 is optionally substituted phenyl, phenylalkyl, heteroaryl or heteroarylalkyl, naphthyl, fluorenyl or diphenylmethyl; R3 is optionally substituted phenyl, heteroaryl or naphthyl; R4 is H, alkyl, fluoro-alkyl, cyclopropylmethyl, —CH2CH2OH, —CH2CH2—O-alkyl, —CH2C(O)—O-alkyl, —CH2C(O)NH2, —CH2C(O)—NHalkyl or —CH2C(O)—N(alkyl)2; R19 is optionally substituted phenyl, heteroaryl or naphthyl, cycloalkyl, cycloalkylalkyl or alkoxyalkyl; and R5, R13, R14, R15 and R16 are hydrogen or alkyl for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.
    • 使用下式的CCR5拮抗剂或其药学上可接受的盐,其中X是-C(R 13)2 - , - C(R 13)(R 19) - , - C(O) - , - O - N(烷基) - ,R是任选取代的苯基,吡啶基,噻吩基或萘基; R1是H,烷基或烯基; R2是任选取代的苯基,苯基烷基,杂芳基或杂芳基烷基,萘基,芴基或二苯基甲基; R 3是任选取代的苯基, 杂芳基或萘基; R4是H,烷基,氟代烷基,环丙基甲基,-CH2CH2OH,-CH2CH2-O-烷基,-CH2C(O)-O-烷基,-CH2C(O)NH2,-CH2C(O) 或-CH 2 C(O)-N(烷基)2; R 19是任选取代的苯基,杂芳基或萘基,环烷基,环烷基烷基或烷氧基烷基; 和R 5,R 13,R 14,R 15和R 16是氢或烷基,用于治疗HIV,实体器官移植排斥,移植物抗宿主病,关节炎,类风湿性关节炎,炎性肠病,特应性皮炎,牛皮癣,哮喘,过敏或多发性硬化 以及新化合物,包含它们的药物组合物,以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。
    • 13. 发明授权
    • Quinoline-diones
    • 喹啉二恶英
    • US5179093A
    • 1993-01-12
    • US698204
    • 1991-05-10
    • Adriano AfonsoStuart W. McCombieJay Weinstein
    • Adriano AfonsoStuart W. McCombieJay Weinstein
    • C07D215/22C07D401/12
    • C07D215/22C07D401/12
    • Compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein, R is H, halogen, (C.sub.1 -C.sub.6) alkyl, N(C.sub.1 -C.sub.6 alkyl/aryl).sub.2, OH, O--(C.sub.1 -C.sub.6) alkyl/aryl, CH.sub.2 OH, COOH, COO-alkyl/aryl, SO.sub.2 NH.sub.2, or SO.sub.2 NH (C.sub.1 -C.sub.6 alkyl/aryl);R.sub.1 is C.sub.1 -C.sub.6 alkyl, cycloalkyl, C.sub.2 -C.sub.6 alkenyl, heteroaryl, substituted heteroaryl, heterocycloalkyl, --CH.sub.2 -aryl, --CH.sub.2 -substituted aryl, --CH.sub.2 -heteroaryl, or --CH.sub.2 -substituted heteroaryl;R.sub.2 is H, C.sub.1 -C.sub.6 alkyl or aryl; ##STR2## is an aromatic ring or a heteroaromatic ring; and X is O or N-(alkyl/aryl/alkyl-aryl/alkoxylalkoxyaryl)are described. These compounds are useful as agents for treating viruses.
    • 式I的化合物或其药学上可接受的盐,其中R是H,卤素,(C 1 -C 6)烷基,N(C 1 -C 6烷基/芳基)2,OH,O-(C 1 -C 6)烷基 芳基,CH 2 OH,COOH,COO-烷基/芳基,SO 2 NH 2或SO 2 NH(C 1 -C 6烷基/芳基); R 1是C 1 -C 6烷基,环烷基,C 2 -C 6烯基,杂芳基,取代的杂芳基,杂环烷基,-CH 2 - 芳基,-CH 2 - 取代的芳基,-CH 2 - 杂芳基或-CH 2 - 取代的杂芳基; R2是H,C1-C6烷基或芳基; 是芳环或杂芳环; 并且X是O或N-(烷基/芳基/烷基 - 芳基/烷氧基烷氧基芳基)。 这些化合物可用作治疗病毒的药剂。