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    PDE IV inhibitors
    2.
    发明授权
    PDE IV inhibitors 失效
    PDE IV抑制剂

    公开(公告)号：US07115623B2

    公开(公告)日：2006-10-03

    申请号：US10480378

    申请日：2002-06-11

    申请人： Tomoji Aotsuka ,  Kentarou Kumazawa ,  Nagatoshi Wagatsuma ,  Kouki Ishitani ,  Takashi Nose

    发明人： Tomoji Aotsuka ,  Kentarou Kumazawa ,  Nagatoshi Wagatsuma ,  Kouki Ishitani ,  Takashi Nose

    IPC分类号： C07D471/02 ,  A61K31/44

    CPC分类号： C07D471/04

    摘要： The purpose is to provide selective PDE IV inhibitors which have a potent anti-asthmatic profile with excellent safety. A compound of the formula (1): wherein A is methylene, lower alkylmethylene, carbonyl, etc., Y is a 5- or 6-membered heteroaryl group containing one or two heteroatoms selected from nitrogen, sulfur and oxygen, Z is i) a fused ring in which any of 5- or 6-membered heteroaryl groups is fused to a benzene ring, or ii) a phenyl group which may be unsubstituted or optionally substituted with one or more members selected from the group consisting of nitro, amino, an amino nitrogen-containing group, etc., provided that when A is methylene, Y is a 5- or 6-membered heteroaryl group selected from the group consisting of pyrrolyl, pyridyl, etc., and Z is a phenyl group which may be unsubstituted or substituted, the substituent on said phenyl group is amino, or an amino nitrogen-containing group; or a pharmaceutically acceptable salt thereof, possesses excellent PDE IV inhibition and is useful as a pharmaceutical drug, preferably an anti-asthmatic, etc.

    摘要翻译： 目的是提供选择性PDE IV抑制剂，其具有优异的抗哮喘特征，具有优异的安全性。 式（1）的化合物：其中A是亚甲基，低级烷基亚甲基，羰基等，Y是含有一个或两个选自氮，硫和氧的杂原子的5或6元杂芳基，Z是i） 其中5-或6-元杂芳基中的任一个与苯环稠合的稠合环，或ii）可以是未取代的或任选被一个或多个选自以下的成员取代的苯基：硝基，氨基， 氨基含氮基团等，条件是当A是亚甲基时，Y是选自吡咯基，吡啶基等的5或6元杂芳基，Z是可以是 未取代或取代的，所述苯基上的取代基是氨基或氨基含氮基团; 或其药学上可接受的盐具有优异的PDE IV抑制作用，并且可用作药物，优选抗哮喘等。

    1,8-naphthyridin-2(1H)-one derivatives
    3.
    发明授权
    1,8-naphthyridin-2(1H)-one derivatives 失效
    1,8-二氮杂萘-2（1H） - 酮衍生物

    公开(公告)号：US06642250B2

    公开(公告)日：2003-11-04

    申请号：US09889107

    申请日：2001-07-11

    申请人： Tomoji Aotsuka ,  Kentarou Kumazawa ,  Nagatoshi Wagatsuma ,  Kouki Ishitani

    发明人： Tomoji Aotsuka ,  Kentarou Kumazawa ,  Nagatoshi Wagatsuma ,  Kouki Ishitani

    IPC分类号： A61K3144

    CPC分类号： C07D471/04

    摘要： The purpose is to provide selective PDE IV inhibitors which have a potent anti-asthmatic profile with excellent safety. A compound of the formula (1): wherein: A is an unsubstituted or optionally substituted 5 or 6 membered heteroaryl group or a fused benzene ring in which any of the above-defined heteroaryl groups is fused to a benzene ring, B is carbon or nitrogen, R1 is hydrogen, lower alkyl, trifluoromethyl, hydroxyl, lower alkoxy, a residue derived from a carboxylic acid or a derivative thereof, amino, or an amino nitrogen-containing group, R2 is hydrogen, halogen, cyano, nitro, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, trifluoromethyl, hydroxyl, lower alkoxy, a residue derived from a carboxylic acid or a derivative thereof, amino, or an amino nitrogen-containing group, and m is an integer of from 1 to 8, both inclusive; or a pharmaceutically acceptable salt thereof possesses selective PDE IV inhibition and is useful as a pharmaceutical drug, preferably an anti-asthmatic, etc.

    摘要翻译： 目的是提供选择性PDE IV抑制剂，其具有优异的抗哮喘特征，具有优异的安全性。 式（1）的化合物：其中：A是未取代或任选取代的5或6元杂芳基或稠合苯环，其中任何上述定义的杂芳基与苯环稠合，B是碳或 氮，R 1是氢，低级烷基，三氟甲基，羟基，低级烷氧基，衍生自羧酸或其衍生物的氨基，氨基或氨基含氮基团，R 2是氢，卤素， 氰基，硝基，低级烷硫基，低级烷基亚磺酰基，低级烷基磺酰基，三氟甲基，羟基，低级烷氧基，衍生自羧酸或其衍生物的氨基，氨基或氨基含氮基团，m为1〜 8，均包括在内;或其药学上可接受的盐具有选择性的PDE IV抑制作用，并且可用作药物，优选抗哮喘等。

    Pyrazole derivatives and COX inhibitors containing them
    4.
    发明授权
    Pyrazole derivatives and COX inhibitors containing them 有权
    吡唑衍生物和含有它们的COX抑制剂

    公开(公告)号：US6136831A

    公开(公告)日：2000-10-24

    申请号：US402433

    申请日：1999-10-07

    申请人： Tomoji Aotsuka ,  Nagatoshi Wagatsuma ,  Hideo Kato ,  Naoki Ashizawa

    发明人： Tomoji Aotsuka ,  Nagatoshi Wagatsuma ,  Hideo Kato ,  Naoki Ashizawa

    IPC分类号： C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428

    CPC分类号： C07D403/04 ,  C07D413/04 ,  C07D417/04

    摘要： The purpose is to provide anti-inflammatory agents which have potent pharmacological actions and exert a selective inhibitory activity on COX-2, thereby being expected to reduce adverse effects such as disorders in gastric mucosa. The present invention encompasses a compound of the formula (1): wherein R.sup.1 is hydrogen or halogen, R.sup.2 and R.sup.3 are each independently hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy or lower alkanoyloxy, R.sup.4 is lower haloalkyl or lower alkyl, X is sulfur, oxygen or NH, and Y is lower alkylthio, lower alkylsulfonyl or sulfamoyl, which exerts superior anti-inflammatory activity, and highly inhibits COX-2 induced in inflamed sites, with less inhibitory action on COX-1 present in stomach, kidney, etc. Pharmaceutical agents comprising the compound of the present invention are provided as selective COX-2 inhibitors, and anti-inflammatory agents rarely accompanying adverse actions including attacks on gastric mucosa.

    摘要翻译： PCT No.PCT / JP98 / 01664 Sec。 371 1999年10月7日第 102（e）日期1999年10月7日PCT提交1998年4月10日PCT公布。 公开号WO98 / 46594 日期1998年10月22日目的是提供具有有效药理作用并对COX-2具有选择性抑制活性的抗炎剂，从而预期减少诸如胃粘膜疾病的不良反应。 本发明包括式（1）的化合物：其中R1是氢或卤素，R2和R3各自独立地是氢，卤素，低级烷基，低级烷氧基，羟基或低级烷酰氧基，R4是低级卤代烷基或低级烷基，X 是硫，氧或NH，Y是低级烷硫基，低级烷基磺酰基或氨磺酰基，其具有优异的抗炎活性，并且高度抑制炎症部位诱导的COX-2，对胃，肾中COX-1的抑制作用较小 提供包含本发明化合物的药物作为选择性COX-2抑制剂，和很少伴随不良反应（包括攻击胃粘膜）的抗炎剂。