公开(公告)号：US20100240677A1

公开(公告)日：2010-09-23

申请号：US12693791

申请日：2010-01-26

申请人： Garry FENTON ,  Tahir Nadeem MAJID ,  Malcolm Norman PALFREYMAN

发明人： Garry FENTON ,  Tahir Nadeem MAJID ,  Malcolm Norman PALFREYMAN

IPC分类号： A61K31/497 ,  C07D213/75 ,  A61K31/44 ,  A61P19/02 ,  A61P31/04 ,  A61P19/00 ,  A61P11/06 ,  A61P37/06 ,  A61P33/06 ,  A61P31/18 ,  A61P1/04 ,  A61P3/10 ,  A61P13/12 ,  A61P17/06 ,  A61P35/02 ,  C07C235/56 ,  A61K31/167 ,  C07D333/36 ,  A61K31/381 ,  C07D241/20 ,  A61K31/4965 ,  C07D239/42 ,  A61K31/505 ,  C07D401/12

CPC分类号： C07D213/70 ,  C07C43/247 ,  C07C217/58 ,  C07C235/56 ,  C07C237/30 ,  C07C255/60 ,  C07C327/48 ,  C07C2601/08 ,  C07C2603/64 ,  C07C2603/66 ,  C07D213/65 ,  C07D213/69 ,  C07D213/75 ,  C07D213/79 ,  C07D213/81 ,  C07D213/82 ,  C07D213/89 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF).Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.

摘要翻译： 本发明涉及[二（醚或硫醚）杂芳基或氟取代的芳基]化合物或其N-氧化物或其药学上可接受的盐，其可用于抑制TNF在治疗中的产生或生理作用 患有与生理上有害的肿瘤坏死因子（TNF）过量相关的疾病状态的患者。 本发明范围内的化合物还抑制环AMP磷酸二酯酶，并且可用于治疗与通过抑制环AMP磷酸二酯酶调节的病理状况相关的疾病状态，所述疾病状态包括炎性和自身免疫性疾病，特别是IV型环AMP 磷酸二酯酶。 因此，本发明涉及其用于抑制TNF和/或环AMP磷酸二酯酶的药理学用途，包含该化合物的药物组合物及其制备方法。

公开(公告)号：US20080132706A1

公开(公告)日：2008-06-05

申请号：US11764317

申请日：2007-06-18

申请人： Garry FENTON ,  Tahir Nadeem MAJID ,  Malcolm Norman PALFREYMAN

发明人： Garry FENTON ,  Tahir Nadeem MAJID ,  Malcolm Norman PALFREYMAN

IPC分类号： C07D213/02 ,  C07C233/00

CPC分类号： C07D213/70 ,  C07C43/247 ,  C07C217/58 ,  C07C235/56 ,  C07C237/30 ,  C07C255/60 ,  C07C327/48 ,  C07C2601/08 ,  C07C2603/64 ,  C07C2603/66 ,  C07D213/65 ,  C07D213/69 ,  C07D213/75 ,  C07D213/79 ,  C07D213/81 ,  C07D213/82 ,  C07D213/89 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF).Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.

摘要翻译： 本发明涉及[二（醚或硫醚）杂芳基或氟取代的芳基]化合物或其N-氧化物或其药学上可接受的盐，其可用于抑制TNF在治疗中的产生或生理作用 患有与生理上有害的肿瘤坏死因子（TNF）过量相关的疾病状态的患者。 本发明范围内的化合物还抑制环AMP磷酸二酯酶，并且可用于治疗与通过抑制环AMP磷酸二酯酶调节的病理状况相关的疾病状态，所述疾病状态包括炎性和自身免疫性疾病，特别是IV型环AMP 磷酸二酯酶。 因此，本发明涉及其用于抑制TNF和/或环AMP磷酸二酯酶的药理学用途，包含该化合物的药物组合物及其制备方法。