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    • 5. 发明申请
    • Piperazine derivatives useful as CCR5 antagonists
    • 哌嗪衍生物可用作CCR5拮抗剂
    • US20060105964A1
    • 2006-05-18
    • US11255643
    • 2005-10-21
    • Ragulan RamanathanAnima GhosalMichael MillerSwapan ChowdhuryKevin Alton
    • Ragulan RamanathanAnima GhosalMichael MillerSwapan ChowdhuryKevin Alton
    • A61K31/7052A61K31/513A61K31/506C07D403/14
    • C07D401/14C07D401/06C07H17/02
    • The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; 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R是任选取代的苯基,吡啶基,噻吩基或萘基; R 1是氢或烷基; R 2是取代的苯基,取代的杂芳基,萘基,芴基,二苯基甲基或任选取代的苯基或杂芳基 - 烷基; R 3是氢,烷基,烷氧基烷基,环烷基,环烷基烷基或任选取代的苯基,苯基烷基,萘基,萘基烷基,杂芳基或杂芳基烷基; R 4,R 5和R 7是氢或烷基; R 6是氢,烷基或链烯基; 公开了用于治疗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,炎症性肠病,特应性皮炎,牛皮癣,哮喘,过敏或多发性硬化的新型化合物,以及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。
    • 8. 发明授权
    • Piperazine derivatives useful as CCR5 antagonists
    • 哌嗪衍生物可用作CCR5拮抗剂
    • US07825121B2
    • 2010-11-02
    • US11255643
    • 2005-10-21
    • Ragulan RamanathanAnima GhosalMichael W. MillerSwapan K. ChowdhuryKevin B. Alton
    • Ragulan RamanathanAnima GhosalMichael W. MillerSwapan K. ChowdhuryKevin B. Alton
    • A61K31/497A01N43/54C07D403/00C07D239/00
    • C07D401/14C07D401/06C07H17/02
    • The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; 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R是任选取代的苯基,吡啶基,噻吩基或萘基; R1是氢或烷基; R 2是取代的苯基,取代的杂芳基,萘基,芴基,二苯基甲基或任选取代的苯基或杂芳基 - 烷基; R 3是氢,烷基,烷氧基烷基,环烷基,环烷基烷基或任选取代的苯基,苯基烷基,萘基,萘基烷基,杂芳基或杂芳基烷基; R4,R5和R7是氢或烷基; R6是氢,烷基或烯基; 公开了用于治疗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,炎症性肠病,特应性皮炎,牛皮癣,哮喘,过敏或多发性硬化的新型化合物,以及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。