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    [Alkoxy-, alkenyloxy-, alkynyloxy-, and phenylmethyloxyalkoxycycloalkyl or alkoxycycloheteroalkyl]naphtho[2,3-c]furan-1(3H)-one inhibitors of 5-lipoxygenase
    4.
    发明授权
    [Alkoxy-, alkenyloxy-, alkynyloxy-, and phenylmethyloxyalkoxycycloalkyl or alkoxycycloheteroalkyl]naphtho[2,3-c]furan-1(3H)-one inhibitors of 5-lipoxygenase 失效
    烷氧基 - ，烯氧基 - ，炔氧基 - 和苯基甲氧基烷氧基环烷基或烷氧基环杂烷基]萘并[2,3-c]呋喃-1（3H） - 酮抑制剂5-脂氧合酶

    公开(公告)号：US5426111A

    公开(公告)日：1995-06-20

    申请号：US344774

    申请日：1994-11-23

    申请人： Joseph F. Dellaria ,  James D. Ratajczyk ,  Clint D. W. Brooks ,  Anwer Basha

    发明人： Joseph F. Dellaria ,  James D. Ratajczyk ,  Clint D. W. Brooks ,  Anwer Basha

    IPC分类号： C07C65/26 ,  C07D307/92 ,  C07D405/04 ,  C07D405/14 ,  C07D407/12 ,  C07D407/14 ,  C07D409/04 ,  C07D409/14 ,  A61K31/435 ,  C07C63/64 ,  C07D315/00 ,  C07D409/00

    CPC分类号： C07D307/92 ,  C07C65/26 ,  C07D405/04 ,  C07D405/14 ,  C07D407/12 ,  C07D407/14 ,  C07D409/04 ,  C07D409/14

    摘要： Compounds of formula ##STR1## Ar is selected from (a) phenyl, (b) phenyl substituted with one or more groups selected from halogen, cyano, alkyl, haloalkyl, alkoxy, and alkoxycarbonyl, (c) furyl, (d) furyl substituted with one or more groups selected from halogen, alkyl, and alkoxy, (e) pyridyl, (f) pyridyl substituted with one or more groups selected from halogen, alkyl, and alkoxy, (g) thienyl, and (h) thienyl substituted with one or more groups selected from halogen, alkyl, and alkoxy; L is selected from alkylene of one to three carbon atoms, alkenylene of two to three carbon atoms, and alkynylene of two to three carbon atoms, and ##STR2## wherein p is an integer of 1 to 4, inclusive, and R.sup.4 is selected from the group consisting of hydrogen, alkyl of one to four carbon atoms, halogen, haloalkyl of one to four carbon atoms, and alkoxy of one to six carbon atoms;R.sup.1 is alkyl; R.sup.2 is hydrogen or alkyl; m is 1 or 2; Z is oxygen or CHOR.sup.3, and n is 0 or 1 are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.

    摘要翻译： 式（Ia）化合物选自（a）苯基，（b）被一个或多个选自卤素，氰基，烷基，卤代烷基，烷氧基和烷氧基羰基的基团取代的苯基，（c）呋喃基，（d （f）吡啶基，（f）被一个或多个选自卤素，烷基和烷氧基的基团取代的吡啶基，（g）噻吩基，和（h）被卤素，烷基和烷氧基取代的吡啶基， 被一个或多个选自卤素，烷基和烷氧基的基团取代的噻吩基; L选自1至3个碳原子的亚烷基，2至3个碳原子的亚烯基和2至3个碳原子的亚炔基，和其中p是1至4的整数，并且R 4选自 由氢，1-4个碳原子的烷基，卤素，1-4个碳原子的卤代烷基和1至6个碳原子的烷氧基组成的组; R1是烷基; R2是氢或烷基; m为1或2; Z是氧或CHOR3，n是0或1是脂氧合酶的有效抑制剂，从而抑制白细胞三烯的生物合成。 这些化合物可用于治疗或改善过敏性和炎性疾病状态。

    [1-(2-Benzoxazolyl)hydrazino]alkyl nitrile derivatives
    5.
    发明授权
    [1-(2-Benzoxazolyl)hydrazino]alkyl nitrile derivatives 失效
    [1-（2-苯并恶唑基）肼基]烷基腈衍生物

    公开(公告)号：US4476137A

    公开(公告)日：1984-10-09

    申请号：US471926

    申请日：1983-03-03

    申请人： Fortuna Haviv ,  James D. Ratajczyk ,  Francis E. Fischer

    发明人： Fortuna Haviv ,  James D. Ratajczyk ,  Francis E. Fischer

    IPC分类号： C07D209/40 ,  C07D263/58 ,  C07D277/82 ,  A61K31/42

    CPC分类号： C07D263/58 ,  C07D209/40 ,  C07D277/82

    摘要： Described are compounds of the formula ##STR1## wherein R is hydrogen or loweralkyl, X, Y and W independently of one another denote hydrogen, halogen, loweralkyl, nitro, amino, amido, loweralkoxy, hydroxy, nitrile, methylsulfone, methylsulfoxide, methylmercapto, or trifluoromethyl; Z is oxygen, sulfur or --CH.sub.2 ; n and m are each an integer from 0 to 6 inclusive, or pharmaceutically acceptable salts thereof.The compounds are effective as anti-inflammatory agents.

    摘要翻译： 描述了下式的化合物，其中R是氢或低级烷基，X，Y和W彼此独立地表示氢，卤素，低级烷基，硝基，氨基，酰胺基，低级烷氧基，羟基，腈，甲基砜，甲基亚砜，甲基巯基， 或三氟甲基; Z是氧，硫或-CH 2; n和m各自为0〜6的整数，或其药学上可接受的盐。 这些化合物作为抗炎剂是有效的。

    Compounds useful as alkaline phosphatase inhibitors and therapeutic agents
    6.
    发明授权
    Compounds useful as alkaline phosphatase inhibitors and therapeutic agents 失效
    可用作碱性磷酸酶抑制剂和治疗剂的化合物

    公开(公告)号：US5516647A

    公开(公告)日：1996-05-14

    申请号：US148142

    申请日：1993-11-05

    申请人： Mazhar Husain ,  Dominique Bridon ,  Mark Bures ,  James D. Ratajczyk ,  Fortuna Haviv ,  Christopher Bieniarz

    发明人： Mazhar Husain ,  Dominique Bridon ,  Mark Bures ,  James D. Ratajczyk ,  Fortuna Haviv ,  Christopher Bieniarz

    IPC分类号： C07D513/04 ,  C12Q1/42 ,  C07D513/02

    CPC分类号： C07D513/04 ,  C12Q1/42 ,  Y10S435/81

    摘要： The present invention discloses novel compounds useful as alkaline phosphatase inhibitors and therapeutic agents. Preferably, the novel compounds are useful as selective inhibitors of human alkaline phosphatases as opposed to Escherichia coli alkaline phosphatases. The novel compounds can also be used as cancer therapeutic agents, anti-depressive agents, anti-anergic agents, and antihelminthic agents. The novel compounds have the following general formula: ##STR1## wherein R' is an aryl, aryl ether, aryl thioether, aromatic heterocyclic, aromatic heterocyclic thioether, or aromatic heterocyclic ether group. More preferably, R' is a phenyl or a pyridine. Most preferably, R' is of the following formula: ##STR2## 2-thiopyridine, or ##STR3## 2-oxypyridine. R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.1 ', R.sub.2 ', R.sub.3 ', R.sub.4 ', and R.sub.5 ' can be the same or different, and at least one of which is selected from the group consisting of: H, C.sub.1 -C.sub.6 alkyl, halo C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, trifluoromethyl, nitro, amino, carboxy, and halo groups with the proviso that each novel compound has no more than three substituents. Hydrogen is not considered a substituent.

    摘要翻译： 本发明公开了可用作碱性磷酸酶抑制剂和治疗剂的新化合物。 优选地，新化合物可用作人碱性磷酸酶的选择性抑制剂，与大肠杆菌碱性磷酸酶相反。 新化合物也可以用作癌症治疗剂，抗抑郁剂，抗过敏剂和抗栓剂。 新化合物具有以下通式：其中R'为芳基，芳基醚，芳基硫醚，芳族杂环，芳族杂环硫醚或芳族杂环醚基团。 更优选地，R'是苯基或吡啶。 最优选地，R'具有下列结构式：2-甲基吡啶或2-氧代吡啶。 R1，R2，R3，R4，R1'，R2'，R3'，R4'和R5'可以相同或不同，其中至少一个选自：H，C 1 -C 6烷基 ，卤素C 1 -C 6烷基，苯基，C 1 -C 6烷氧基，苯氧基，三氟甲基，硝基，氨基，羧基和卤素基团，条件是每个新化合物不超过三个取代基。 氢不被认为是取代基。