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    CARBOXYLIC ACIDS
    2.
    发明公开
    CARBOXYLIC ACIDS 审中-公开
    CARBONSÄUREN

    公开(公告)号：EP1375484A1

    公开(公告)日：2004-01-02

    申请号：EP02707188.5

    申请日：2002-03-27

    申请人： Eisai Co., Ltd.

    发明人： HARADA, Hitoshi ,  SHINODA, Masanobu ,  CLARK, Richard ,  MATSUURA, Fumiyoshi ,  EMORI, Eita ,  KASAI, Shunji ,  YOSHITOMI, Hideki ,  YAMAZAKI, Kazuto ,  INOUE, Takashi ,  MIYASHITA, Sadakazu ,  HIHARA, Taro

    IPC分类号： C07D213/64 ,  A61K31/4409 ,  A61K31/4412 ,  A61P1/04 ,  A61P3/06 ,  A61P3/10 ,  A61P29/00 ,  A61P43/00

    CPC分类号： C07D213/64 ,  C07D213/79

    摘要： The present invention provides a novel carboxylic acid derivative, a salt thereof or a hydrate of them which is useful as an insulin sensitizer, and a medicament comprising the derivative as the effective ingredient. More specifically, it provides a carboxylic acid compound represented by the formula (I), a salt thereof or a hydrate of them.
    In the formula, Ar represents a 6- to 14-membered aromatic ring group which may have at least one substituent; R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are the same as or different from each other and each represents a hydrogen atom, a halogen atom, a hydroxyl group, a C 1-6 alkyl group or a C 1-6 alkoxy group; X represents an oxygen atom or a methylene group; Y represents a group represented by the formula (II) or (III):
    (wherein Z represents a group represented by the formula (IV):
    (wherein R 9 , R 10 , R 11 and R 12 are the same as or different from each other and each represents a hydrogen atom, a halogen atom, a hydroxyl group, a C 1-6 alkyl group or a C 1-6 alkoxy group)); m is 0 or 1; and n is 0 or 1.

    摘要翻译： 本发明提供可用作胰岛素敏化剂的新型羧酸衍生物，其盐或其水合物，以及包含该衍生物作为有效成分的药物。 更具体地，它提供由式（I）表示的羧酸化合物，其盐或它们的水合物。 式中，Ar表示可以具有至少一个取代基的6〜14元芳香族环基; R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8彼此相同或不同， 表示氢原子，卤素原子，羟基，C 1-6烷基或C 1-6烷氧基; X表示氧原子或亚甲基; Y表示由式（II）或（III）表示的基团：（其中Z表示由式（IV）表示的基团：CHEM>（其中R 9，R 10， 11＆gt;和R 12彼此相同或不同，各自表示氢原子，卤素原子，羟基，C 1-6烷基或C 1-6烷氧基））。 m为0或1; n为0或1。

    PURINE DERIVATIVES AND ADENOSINE A2 RECEPTOR ANTAGONISTS SERVING AS PREVENTIVES/REMEDIES FOR DIABETES
    3.
    发明公开
    PURINE DERIVATIVES AND ADENOSINE A2 RECEPTOR ANTAGONISTS SERVING AS PREVENTIVES/REMEDIES FOR DIABETES 有权
    嘌呤衍生物和腺苷A2受体的拮抗剂，它们的提供或治愈糖尿病的

    公开(公告)号：EP1054012A1

    公开(公告)日：2000-11-22

    申请号：EP98961528.1

    申请日：1998-12-24

    申请人： Eisai Co., Ltd.

    发明人： ASANO, Osamu ,  HARADA, Hitoshi ,  HOSHINO, Yorihisa ,  YOSHIKAWA, Seiji ,  INOUE, Takashi ,  HORIZOE, Tatsuo ,  YASUDA, Nobuyuki ,  NAGATA, Kaya ,  NAGAOKA, Junsaku ,  MURAKAMI, Manabu ,  KOBAYASHI, Seiichi

    IPC分类号： C07D473/00 ,  C07D473/04 ,  C07D473/30 ,  C07D473/34 ,  C07D473/40 ,  C07D487/04 ,  C07D487/14 ,  A61K31/505 ,  A61K31/52 ,  A61K31/645 ,  A61K45/00

    CPC分类号： C07D473/30 ,  A61K31/52 ,  C07D473/00 ,  C07D473/34

    摘要： The present invention provides a preventive or therapeutic agent of a new type for diabetes mellitus and diabetic complications on the basis of an adenosine A2 receptor antagonistic action.
    A purine compound represented by the formula (I), its pharmacologically acceptable salt or hydrates thereof has an adenosine A2 receptor antagonistic action and is useful for prevention or therapy of diabetes mellitus and diabetic complications. In addition, adenosine A2 receptor antagonists having different structures from those of the compounds described above, for example KW6002, are also effective for prevention or therapy of diabetes mellitus and diabetic complications.
    In the formula, W is -CH 2 CH 2 -, -CH=CH- or -C≡C-; R 1 is:
    (in the formula, X is hydrogen atom, hydroxyl group, a lower alkyl group, a lower alkoxy group, etc.; and R 5 and R 6 are the same as or different from each other and each represents hydrogen atom, a lower alkyl group, a cycloalkyl group, etc.) and the like; R 2 is an amino group, etc. which may be substituted with a lower alkyl group, etc.; R 3 is a cycloalkyl group, an optionally substituted aryl group, etc.; and R 4 is a lower alkyl group, etc.

    摘要翻译： 本发明提供了一种新型的用于治疗糖尿病和糖尿病并发症的腺苷A2受体拮抗作用的基础上的预防或治疗剂。 由式（I）表示的嘌呤化合物，其药理学上可接受的盐或其水合物具有腺苷A 2受体拮抗作用，并且是用于预防或糖尿病和糖尿病并发症的治疗是有用的。 此外，具有腺苷A 2受体拮抗剂不同的结构与上述那些，例如KW6002的化合物的，所以有效地预防或糖尿病和糖尿病并发症是治疗。 在该式中，W是-CH 2 CH 2，-CH = CH-或-C IDENTICAL C-; [R <1>为：（式中，X是氢原子，羟基，低级烷基，低级烷氧基等;且R <5>和R <6>是相同的或 从海誓山盟并且每个darstellt氢原子，低级烷基，环烷基，等）等不同; [R <2>是氨基，等。可以是与substituiertem低级烷基等; [R <3>为环烷基，在OPTIONALLY substituiertem芳基等; 且R <4>是低级烷基等

    PYRIMIDONE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
    4.
    发明公开
    PYRIMIDONE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME 有权
    PYRIMIDONVERBINDUNGEN UND PHARMAZEUTISCHE ZUSAMMENSETZUNGEN，DIEE ENTHALTEN

    公开(公告)号：EP1439176A1

    公开(公告)日：2004-07-21

    申请号：EP02802051.9

    申请日：2002-10-22

    申请人： Eisai Co., Ltd.

    发明人： HARADA, Hitoshi ,  ASANO, Osamu ,  UEDA, Masato ,  MIYAZAWA, Shuhei ,  KOTAKE, Yoshihiko ,  KABASAWA, Yasuhiro ,  YASUDA, Masahiro ,  YASUDA, Nobuyuki

    IPC分类号： C07D401/04 ,  C07D405/14 ,  C07D409/14 ,  A61K31/513 ,  A61P1/04 ,  A61P1/10 ,  A61P3/04 ,  A61P3/10 ,  A61P7/10 ,  A61P9/12 ,  A61P11/06 ,  A61P19/10 ,  A61P25/16 ,  A61P25/28 ,  A61P27/02 ,  A61P43/00

    CPC分类号： C07D239/34 ,  A61K31/513

    摘要： The present invention provides a novel pyrimidone compound having an excellent adenosine receptor (A 1 A 2A , A 2B receptor) antagonistic action. More specifically, it provides a compound represented by the following formula, a salt thereof or a solvate of them.
    In the formula, R 1 and R 2 are the same as or different from each other and each represents a hydrogen atom, an alkyl group having one to six carbon atoms which may be substituted, an alkenyl group having two to six carbon atoms which may be substituted, an alkynyl group having two to six carbon atoms which may be substituted, a cycloalkyl group having three to eight carbon atoms which may be substituted, a cycloalkenyl group having three to eight carbon atoms which may be substituted, a 5 to 14-membered non-aromatic heterocyclic group which may be substituted, an aromatic cyclic hydrocarbon group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted, an acyl group having one to six carbon atoms which may be substituted or an alkylsulfonyl group having one to six carbon atoms which may be substituted; R 3 represents a hydrogen atom, an alkyl group having one to six carbon atoms which may be substituted, an alkenyl group having two to six carbon atoms which may be substituted, or an alkynyl group having two to six carbon atoms which may be substituted; R 4 represents an C 6-14 aromatic cyclic hydrocarbon group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted or a 5 to 14-membered non-aromatic heterocyclic group having at least one unsaturated bond which may be substituted; and R 5 represents an aromatic cyclic hydrocarbon group having six to fourteen which may be substituted or a 5 to 14-membered aromatic heterocyclic group which may be substituted.

    摘要翻译： 本发明提供具有优异的腺苷受体（A1A2A，A2B受体）拮抗作用的新的嘧啶酮化合物。 更具体地，其提供由下式表示的化合物，其盐或它们的溶剂合物。 式中，R 1和R 2彼此相同或不同，表示氢原子，可被取代的碳原子数1〜6的烷基，具有取代基的碳原子数为1〜 可被取代的2至6个碳原子，可被取代的具有2至6个碳原子的炔基，可被取代的具有3至8个碳原子的环烷基，可具有3至8个碳原子的环烯基 可被取代的5至14元非芳族杂环基，可被取代的具有6至14个碳原子的芳族环状烃基，可被取代的5至14元芳族杂环基，酰基 具有1至6个可被取代的碳原子的基团或可被取代的具有1至6个碳原子的烷基磺酰基; R 3表示氢原子，可以被取代的碳原子数为1〜6的烷基，可以被取代的碳原子数为2〜6的烯基或可以具有2〜6个碳原子的炔基 取代; R 4表示可以被取代的具有6〜14个碳原子的C6-14芳香族环状烃基，可以被取代的5〜14元芳香族杂环基或5〜14元非芳香族杂环基， 至少一个可被取代的不饱和键; R 5表示可被取代的具有6〜14个的芳香族环状烃基或可以被取代的5〜14元芳香族杂环基。

    CARBOXYLIC ACID DERIVATIVE AND SALT THEREOF
    6.
    发明公开
    CARBOXYLIC ACID DERIVATIVE AND SALT THEREOF 审中-公开
    碳氢化合物在DALEN SALZE

    公开(公告)号：EP1380562A1

    公开(公告)日：2004-01-14

    申请号：EP02720489.0

    申请日：2002-04-18

    申请人： Eisai Co., Ltd.

    发明人： MATSUURA, Fumiyoshi ,  EMORI, Eita ,  SHINODA, Masanobu ,  CLARK, Richard ,  KASAI, Shunji ,  YOSHITOMI, Hideki ,  YAMAZAKI, Kazuto ,  INOUE, Takashi ,  MIYASHITA, Sadakazu ,  HIHARA, Taro ,  HARADA, Hitoshi ,  OHASHI, Kaya

    IPC分类号： C07C59/64

    CPC分类号： C07D413/12 ,  C07C59/58 ,  C07C59/68 ,  C07C59/72 ,  C07C233/25 ,  C07C235/24 ,  C07C251/48 ,  C07C251/52 ,  C07C251/54 ,  C07C255/37 ,  C07C255/54 ,  C07C259/10 ,  C07C271/14 ,  C07C271/16 ,  C07C271/22 ,  C07C271/28 ,  C07C271/58 ,  C07C309/73 ,  C07C309/75 ,  C07C311/19 ,  C07C317/18 ,  C07C317/22 ,  C07C323/20 ,  C07D209/08 ,  C07D209/18 ,  C07D209/24 ,  C07D213/30 ,  C07D213/65 ,  C07D213/68 ,  C07D213/73 ,  C07D213/75 ,  C07D215/14 ,  C07D215/18 ,  C07D215/26 ,  C07D235/06 ,  C07D235/12 ,  C07D277/56 ,  C07D295/096 ,  C07D295/192 ,  C07D307/79 ,  C07D317/54 ,  C07D417/12

    摘要： The present invention provides a novel carboxylic acid compound, a salt thereof or a hydrate of them useful as an insulin sensitizer, and a medicament comprising the compound as an active ingredient. That is, the present invention provides a carboxylic acid compound represented by the following formula, a salt thereof, an ester thereof or a hydrate of them.
    Wherein R 1 represents a hydrogen atom, hydroxyl group, halogen, carboxyl group, or a C 1-6 alkyl group etc., each of which may have one or more substituents; L represents a single bond, or a C 1-6 alkylene group, a C 2-6 alkenylene group or a C 2-6 alkynylene group, each of which may have one or more substituents; M represents a single bond, or a C 1-6 alkylene group, a C 2-6 alkenylene group or a C 2-6 alkynylene group, each of which may have one or more substituents; T represents a single bond, or a C 1-3 alkylene group, a C 2-3 alkenylene group or a C 2-3 alkynylene group, each of which may have one or more substituents; W represents a carboxyl group;
    - - -
    represents a single bond etc. ; X represents a single bond, oxygen atom, a group represented by -NR X1 CQ 1 O- (wherein Q 1 represents an oxygen atom or sulfur atom; and R X1 represents a hydrogen atom, formyl group, or a C 1-6 alkyl group etc., each of which may have one or more substituents), -OCQ 1 NR X1 - (wherein Q 1 and R X1 are as defined above), -CQ 1 NR x1 O- (wherein Q 1 and R X1 are as def ined above), ONR X1 CQ 1 - (wherein Q 1 and R X1 are as defined above), - Q 2 SO 2 - (wherein Q 2 is an oxygen atom or -NR X10 - (wherein R X10 represents a hydrogen atom, formyl group, or a C 1-6 alkyl group etc., each of which may have one or more substituents)) or -SO 2 Q 2 - (wherein Q 2 is as defined above),
    (wherein, provided that R X2 and R X3 , and/or R X4 and R X5 may together form a ring, Q 3 and Q 4 are the same as or different from each other and each represents an oxygen atom, (O)S(O) or NR X10 (wherein NR X10 is as defined above)); Y represents a 5- to 14-membered aromatic group etc., which may have one or more substituents and one or more hetero atoms; and the ring Z represents a 5-to 14-membered aromatic group which may have 0 to 4 substituents and one or more hetero atoms, and wherein part of the ring may be saturated.

    摘要翻译： 本发明提供了可用作胰岛素敏化剂的新型羧酸化合物，其盐或其水合物，以及包含该化合物作为活性成分的药物。 也就是说，本发明提供由下式表示的羧酸化合物，其盐，其酯或它们的水合物。 其中R 1表示氢原子，羟基，卤素，羧基或C 1-6烷基等，其各自可具有一个或多个取代基; L表示可以具有一个或多个取代基的单键或C 1-6亚烷基，C 2-6亚烯基或C 2-6亚炔基， M表示单键或C 1-6亚烷基，C 2-6亚烯基或C 2-6亚炔基，其各自可具有一个或多个取代基; T表示可以具有一个或多个取代基的单键或C 1-3亚烷基，C 2-3亚烯基或C 2-3亚炔基， W表示羧基; - - - 代表单一债券等; X表示单键，氧原子，-NR X X1表示的基团，其中Q 1表示氧原子或硫原子，R X1表示氢原子，甲酰基 ，或C 1-6烷基等，其各自可以具有一个或多个取代基），-OCQ 1 NR X1 - （其中Q 1和R X1如上所定义）， - CQ <1> NR O-（其中Q 1和R X 1如上所定义），ONR X1和Q 1 - （其中Q 1和R X1均为 （其中Q 2是氧原子或-NR X 10 - （其中R X 10表示氢原子，甲酰基或C 1-6烷基等） ，其中每个可以具有一个或多个取代基））或-SO 2 Q 2 - （其中Q 2如上所定义），（其中，条件是R X2和R X3，和/或 R X和R X可以一起形成环，Q 3和Q 4彼此相同或不同，并且各自表示氧原子，（O）S（O）或NR X10>（其中NR X10如上所定义））; Y表示可以具有一个或多个取代基和一个或多个杂原子的5至14元芳族基团等; 并且环Z表示可以具有0至4个取代基和一个或多个杂原子的5至14元芳族基团，并且其中部分环可以是饱和的。

    PYRIMIDINE COMPOUND AND MEDICINAL COMPOSITION THEREOF
    10.
    发明公开
    PYRIMIDINE COMPOUND AND MEDICINAL COMPOSITION THEREOF 有权
    玉米饼干精油

    公开(公告)号：EP1439175A1

    公开(公告)日：2004-07-21

    申请号：EP02802050.1

    申请日：2002-10-22

    申请人： Eisai Co., Ltd.

    发明人： HARADA, Hitoshi ,  ASANO, Osamu ,  UEDA, Masato ,  MIYAZAWA, Shuhei ,  KOTAKE, Yoshihiko ,  KABASAWA, Yasuhiro ,  YASUDA, Masahiro ,  YASUDA, Nobuyuki ,  IIDA, Daisuke ,  NAGAKAWA, Junichi ,  HIROTA, Kazuo ,  NAKAGAWA, Makoto

    IPC分类号： C07D401/04 ,  C07D405/14 ,  C07D409/14 ,  A61K31/506 ,  A61P1/00 ,  A61P1/10 ,  A61P3/04 ,  A61P3/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/02 ,  A61P19/10 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00

    CPC分类号： C07D405/14 ,  A61K31/506 ,  C07D401/04 ,  C07D409/14

    摘要： The present invention provides a novel pyrimidine compound having an excellent adenosine receptor (A 1 , A 2A , A 2B receptor) antagonistic action. More specifically, it provides a compound represented by the following formula, a salt thereof or a solvate of them.

    In the formula, R 1 and R 2 are the same as or different from each other and each represents a hydrogen atom, an alkyl group having one to six carbon atoms which may be substituted, an alkenyl group having two to six carbon atoms which may be substituted, an alkynyl group having two to six carbon atoms which may be substituted, a cycloalkyl group having three to eight carbon atoms which may be substituted, a cycloalkenyl group having three to eight carbon atoms which may be substituted, a 5 to 14-membered non-aromatic heterocyclic group which may be substituted, an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted, an acyl group having one to six carbon atoms which may be substituted or an alkylsulfonyl group having one to six carbon atoms which may be substituted; R 3 represents a hydrogen atom, a halogen atom, a cyano group, an alkyl group having one to six carbon atoms which may be substituted, an alkenyl group having two to six carbon atoms which may be substituted, an alkynyl group having two to six carbon atoms which may be substituted, an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted, a nitrogen atom which may be substituted, an oxygen atom which may be substituted or a sulfur atom which may be substituted; R 4 represents an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted or a 5 to 14-membered non-aromatic heterocyclic group having at least one or more unsaturated bonds which may be substituted; and R 5 represents an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted or a 5 to 14-membered aromatic heterocyclic group which may be substituted.

    摘要翻译： 本发明提供具有优异的腺苷受体（A1，A2A，A2B受体）拮抗作用的新型嘧啶化合物。 更具体地，其提供由下式表示的化合物，其盐或它们的溶剂合物。 式中，R 1和R 2彼此相同或不同，表示氢原子，可以被取代的碳原子数为1〜6的烷基， 具有2-6个可被取代的碳原子的烯基，可被取代的具有2-6个碳原子的炔基，可被取代的具有3-8个碳原子的环烷基，具有3-8个碳原子的环烯基 可被取代的原子，可被取代的5至14元非芳族杂环基，可被取代的具有6至14个碳原子的芳族烃环基，5至14元芳族杂环基，其可以是 取代的，可被取代的具有1至6个碳原子的酰基或可被取代的具有1至6个碳原子的烷基磺酰基; R 3表示氢原子，卤素原子，氰基，可以被取代的碳原子数为1〜6的烷基，可以被取代的碳原子数2〜6的烯基，具有2个 可以被取代的6个碳原子，可以被取代的具有6-14个碳原子的芳族烃环基，可被取代的5至14元芳族杂环基，可被取代的氮原子，氧原子 其可以被取代或可以被取代的硫原子; R 4表示可被取代的碳原子数为6〜14个的芳香族烃基，可以具有取代基的5〜14元芳香族杂环基或具有至少1个的5〜14元非芳香族杂环基 或更多的不饱和键; R 5表示可以被取代的碳原子数为6〜14的芳香族烃基或可以被取代的5〜14元芳香族杂环基。