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    Phenol derivative
    1.
    发明授权
    Phenol derivative 有权
    苯酚衍生物

    公开(公告)号：US08367843B2

    公开(公告)日：2013-02-05

    申请号：US13499190

    申请日：2010-09-29

    申请人： Seiichi Kobashi ,  Junichiro Uda ,  Sachiho Miyata ,  Tsutomu Inoue ,  Naoki Ashizawa ,  Koji Matsumoto ,  Tetsuya Taniguchi ,  Takashi Iwanaga ,  Osamu Nagata

    发明人： Seiichi Kobashi ,  Junichiro Uda ,  Sachiho Miyata ,  Tsutomu Inoue ,  Naoki Ashizawa ,  Koji Matsumoto ,  Tetsuya Taniguchi ,  Takashi Iwanaga ,  Osamu Nagata

    IPC分类号： A61K31/428 ,  C07D277/62

    CPC分类号： C07D277/62 ,  C07D417/02 ,  C07D417/10

    摘要： Disclosed are a novel compound and a pharmaceutical product, each having a remarkable uricosuric effect. Specifically disclosed are: a novel phenol derivative represented by general formula (1) that is shown in FIG. 1; a pharmaceutically acceptable salt thereof; a hydrate of the derivative or the salt; and a solvate of the derivative or the salt. (In the formula, R1 and R2 may be the same or different and each represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a lower alkoxy group, a haloalkyl group, a haloalkoxy group, an alkylsulfanyl group, an alkylsulfinyl group, an alkylsulfonyl group, a lower alkyl-substituted carbamoyl group, a saturated nitrogen-containing heterocyclic N-carbonyl group, a halogen atom, a cyano group or a hydrogen atom; R3 represents a lower alkyl group, a haloalkyl group, a halogen atom, a hydroxy group or a hydrogen atom; and X represents a sulfur atom, an —S(═O)— group or an —S(═O)2— group.)

    摘要翻译： 公开了一种新型化合物和药物，其具有显着的尿酸营养作用。 具体公开的是：图1所示的通式（1）表示的新型苯酚衍生物。 1; 其药学上可接受的盐; 衍生物或盐的水合物; 和衍生物或盐的溶剂化物。 （式中，R 1，R 2可以相同或不同，表示低级烷基，低级烯基，低级炔基，低级烷氧基，卤代烷基，卤代烷氧基，烷基硫烷基， 烷基亚磺酰基，烷基磺酰基，低级烷基取代氨基甲酰基，饱和含氮杂环N-羰基，卤素原子，氰基或氢原子; R3表示低级烷基，卤代烷基， 卤素原子，羟基或氢原子; X表示硫原子，-S（= O） - 基或-S（= O）2 - 基）。

    NOVEL PHENOL DERIVATIVE
    2.
    发明申请
    NOVEL PHENOL DERIVATIVE 有权
    新颖的酚醛衍生物

    公开(公告)号：US20120184587A1

    公开(公告)日：2012-07-19

    申请号：US13499190

    申请日：2010-09-29

    申请人： Seiichi Kobashi ,  Junichiro Uda ,  Sachiho Miyata ,  Tsutomu Inoue ,  Naoki Ashizawa ,  Koji Matsumoto ,  Tetsuya Taniguchi ,  Takashi Iwanaga ,  Osamu Nagata

    发明人： Seiichi Kobashi ,  Junichiro Uda ,  Sachiho Miyata ,  Tsutomu Inoue ,  Naoki Ashizawa ,  Koji Matsumoto ,  Tetsuya Taniguchi ,  Takashi Iwanaga ,  Osamu Nagata

    IPC分类号： A61K31/428 ,  C07D417/10 ,  A61P7/00 ,  A61P3/04 ,  A61P19/06 ,  A61P3/10 ,  A61P9/12 ,  A61P9/10 ,  A61P7/02 ,  C07D277/62 ,  A61P3/06

    CPC分类号： C07D277/62 ,  C07D417/02 ,  C07D417/10

    摘要： Disclosed are a novel compound and a pharmaceutical product, each having a remarkable uricosuric effect. Specifically disclosed are: a novel phenol derivative represented by general formula (1) that is shown in FIG. 1; a pharmaceutically acceptable salt thereof; a hydrate of the derivative or the salt; and a solvate of the derivative or the salt. (In the formula, R1 and R2 may be the same or different and each represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a lower alkoxy group, a haloalkyl group, a haloalkoxy group, an alkylsulfanyl group, an alkylsulfinyl group, an alkylsulfonyl group, a lower alkyl-substituted carbamoyl group, a saturated nitrogen-containing heterocyclic N-carbonyl group, a halogen atom, a cyano group or a hydrogen atom; R3 represents a lower alkyl group, a haloalkyl group, a halogen atom, a hydroxy group or a hydrogen atom; and X represents a sulfur atom, an —S(═O)— group or an —S(═O)2— group.)

    摘要翻译： 公开了一种新型化合物和药物，其具有显着的尿酸营养作用。 具体公开的是：图1所示的通式（1）表示的新型苯酚衍生物。 1; 其药学上可接受的盐; 衍生物或盐的水合物; 和衍生物或盐的溶剂化物。 （式中，R 1，R 2可以相同或不同，表示低级烷基，低级烯基，低级炔基，低级烷氧基，卤代烷基，卤代烷氧基，烷基硫烷基， 烷基亚磺酰基，烷基磺酰基，低级烷基取代氨基甲酰基，饱和含氮杂环N-羰基，卤素原子，氰基或氢原子; R3表示低级烷基，卤代烷基， 卤素原子，羟基或氢原子; X表示硫原子，-S（= O） - 基或-S（= O）2 - 基）。

    2-substituted benzothiazole derivatives and prophylactic and therapeutic agents for the treatment of diabetic complications
    3.
    发明授权
    2-substituted benzothiazole derivatives and prophylactic and therapeutic agents for the treatment of diabetic complications 失效
    2-取代苯并噻唑衍生物和治疗糖尿病并发症的预防和治疗剂

    公开(公告)号：US5700819A

    公开(公告)日：1997-12-23

    申请号：US562061

    申请日：1995-11-22

    申请人： Tomoji Aotsuka ,  Naoki Abe ,  Naoki Ashizawa

    发明人： Tomoji Aotsuka ,  Naoki Abe ,  Naoki Ashizawa

    IPC分类号： C07D277/64 ,  C07D277/74 ,  A61K31/425

    CPC分类号： C07D277/74 ,  C07D277/64

    摘要： Unique benzothiazole derivatives which exert superior aldose redactase inhibiting actions are unexpectedly and advantageously useful in the prophylactic and therapeutic treatment of diabetic complications. A benzothiazole derivative compound of the formula (1): ##STR1## wherein X is halogen, R.sup.1 and R.sup.2, which are the same or different, are each independently hydrogen or halogen, A is a methylene group or a sulfur atom, and --B--COOR.sup.3 is a group as defined in the specification; or a pharmaceutically acceptable salt and a pharmaceutical composition comprising the same which is a useful prophylactic or therapeutic agent for the treatment of diabetic complications.

    摘要翻译： 发挥优异的醛糖再激酶抑制作用的独特的苯并噻唑衍生物意外和有利地用于预防和治疗糖尿病并发症。 式（1）的苯并噻唑衍生物化合物：其中X为卤素，R 1和R 2相同或不同，各自独立地为氢或卤素，A为亚甲基或硫原子， 和-B-COOR3是说明书中定义的基团; 或其药学上可接受的盐和包含其的药物组合物，其是用于治疗糖尿病并发症的有用的预防或治疗剂。

    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。

    1,8-naphthyridin-2-one derivative and use thereof
    5.
    发明授权
    1,8-naphthyridin-2-one derivative and use thereof 失效
    1,8-萘啶-2-酮衍生物及其用途

    公开(公告)号：US5658924A

    公开(公告)日：1997-08-19

    申请号：US448408

    申请日：1995-06-01

    申请人： Akihiro Matsuura ,  Naoki Ashizawa ,  Takema Hase

    发明人： Akihiro Matsuura ,  Naoki Ashizawa ,  Takema Hase

    IPC分类号： C07D471/04 ,  A61K31/44 ,  A61K31/505 ,  A61K31/56 ,  C07D470/04

    CPC分类号： C07D471/04

    摘要： The present invention relates to 1,8-naphthyridin-2-one derivatives, pharmaceutically acceptable acid addition salts and therapeutic agents comprising said compound as an active ingredient, which are used for the diseases such as circulatory diseases and respiratory diseases (e.g. hypertension, renal failure, heart failure, angina pectoris, myocardial infarction, arteriosclerosis, romsoongiitis obliterans, aortitis syndrome, bronchial asthma and peripheral diseases such as peripheral circulatory disorders), central nervous system diseases (e.g. depression, degradatior of central nervous function after cerebrovascular obliteration, cerebrovascular dementia, senile dementia, Alzheimer dementia and memory learning function disorders), various inflammations, and obesity.

    摘要翻译： PCT No.PCT / JP92 / 01575 Sec。 371日期：1995年6月1日 102（e）日期1995年6月1日PCT提交1992年12月1日PCT公布。 WO94 / 12499 PCT公开号 日期：1994年6月9日本发明涉及用于疾病如循环系统疾病和呼吸系统疾病的1,8-萘啶-2-酮衍生物，药学上可接受的酸加成盐和包含所述化合物作为活性成分的治疗剂 （例如高血压，肾功能衰竭，心力衰竭，心绞痛，心肌梗死，动脉硬化，闭塞性闭塞性闭塞性闭塞症，主动脉炎综合征，支气管哮喘和周围疾病如外周循环障碍），中枢神经系统疾病（例如抑郁症，中枢神经功能退化 脑血管性闭塞，脑血管性痴呆，老年痴呆，阿尔茨海默氏痴呆和记忆学习功能障碍），各种炎症和肥胖。

    1 2 4-triazole compound
    6.
    发明授权
    1 2 4-triazole compound 有权
    1 2 4-三唑化合物

    公开(公告)号：US07074816B2

    公开(公告)日：2006-07-11

    申请号：US10495322

    申请日：2002-12-03

    申请人： Hiroshi Nakamura ,  Soichi Kaneda ,  Takahiro Sato ,  Naoki Ashizawa ,  Koji Matsumoto ,  Takashi Iwanaga ,  Tsutomu Inoue

    发明人： Hiroshi Nakamura ,  Soichi Kaneda ,  Takahiro Sato ,  Naoki Ashizawa ,  Koji Matsumoto ,  Takashi Iwanaga ,  Tsutomu Inoue

    IPC分类号： C07D249/08 ,  A61K31/41

    CPC分类号： C07D413/10 ,  C07D311/16 ,  C07D401/04 ,  C07D401/14

    摘要： A novel 1,2,4-triazole compound which is useful as a therapeutic agent for hyperuricemia and gout due to hyperuricemia is provided. A compound is represented by the following general formula (1): wherein R2 represents an unsubstituted or substituted pyridyl group, R1 represents a similar pyridyl group, a pyridine-N-oxide group corresponding to these pyridyl groups, or a phenyl group, and R3 represents hydrogen or a lower alkyl group substituted with pivaloyloxy group and R3 bonds to a nitrogen atom in the ring. A process for production of a compound by reacting a nitrile and a hydrazide, and a therapeutic agent, particularly a xanthine oxidase inhibitor are also provided.

    摘要翻译： 提供了一种新颖的1,2,4-三唑化合物，其可用作高尿酸血症和由于高尿酸血症引起的痛风的治疗剂。 化合物由以下通式（1）表示：其中R 2代表未取代或取代的吡啶基，R 1代表类似的吡啶基，吡啶-N 对应于这些吡啶基的苯氧基或苯基，R 3表示氢或被三氟甲酰氧基取代的低级烷基和R 3键连接到氮原子上 在环中。 还提供了通过腈和酰肼反应生产化合物的方法，以及治疗剂，特别是黄嘌呤氧化酶抑制剂。