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1. 发明公开

EP1308441A1 2-AMINOPYRIDINE COMPOUNDS AND USE THEREOF AS DRUGS 有权
标题翻译：伊马利亚二氨基嘌呤维生素A
公开(公告)号：EP1308441A1
公开(公告)日：2003-05-07
申请号：EP01955633.1
申请日：2001-08-09
申请人： Eisai Co., Ltd.
发明人： HARADA, Hitoshi , ASANO, Osamu , MIYAZAWA, Shuhei , UEDA, Masato , YASUDA, Masahiro , YASUDA, Nobuyuki
IPC分类号： C07D213/82 , C07D213/85 , C07D405/12 , C07D405/14 , A61K31/443 , A61K31/444 , A61K31/4436 , A61K31/455 , A61K31/4409 , A61P43/00 , A61P1/00 , A61P1/10 , A61P3/06 , A61P3/10 , A61P27/02 , A61P11/06 , A61P7/10 , A61P9/10 , A61P19/10 , A61P25/16 , A61P25/28
CPC分类号： C07D213/80 , A61K31/4409 , A61K31/443 , A61K31/4436 , A61K31/444 , A61K31/455 , C07D213/82 , C07D213/85 , C07D405/04 , C07D405/14 , C07D409/14
摘要： The present invention provides 2-aminopyridine compound having an excellent adenosine receptor (A 1 , A 2a , A 2b receptors) antagonism, which is represented by the following formula:
(wherein, R 1 represents cyano group, carboxyl group or an optionally substituted carbamoyl group; R 2 represents hydrogen atom, hydroxyl group, an optionally substituted C 1-6 alkoxy group, an optionally substituted C 6-14 aromatic hydrocarbon cyclic group or an optionally substituted 5- to 14-membered aromatic heterocyclic group; and R 3 and R 1 are the same as or different from each other and each represents a C 6-14 aromatic hydrocarbon cyclic group, a 5- to 14-membered non-aromatic heterocyclic group or a 5- to 14-membered aromatic heterocyclic group which may be substituted, respectively) or a salt thereof.
摘要翻译：本发明提供由下式表示的具有优异的腺苷受体（A1，A2a，A2b受体）拮抗作用的2-氨基吡啶化合物：（其中，R 1表示氰基，羧基或任选地取代的氨基甲酰基; R 2表示氢原子，羟基，任选取代的C 1-6烷氧基，任选取代的C 6-14芳族烃环基或任选取代的5至14元芳族杂环基; R 3和R 1彼此相同或不同，各自表示C 6-14芳族烃环基，5至14元非芳族杂环基或5至14元芳族分别为可被取代的杂环基）或其盐。

2. 发明公开

EP1221444A1 FUSED IMIDAZOLE COMPOUNDS AND REMEDIES FOR DIABETES MELLITUS 有权
标题翻译：简明咪唑衍生物预防糖尿病药物
公开(公告)号：EP1221444A1
公开(公告)日：2002-07-10
申请号：EP00940909.5
申请日：2000-06-30
申请人： Eisai Co., Ltd.
发明人： ASANO, Osamu , HARADA, Hitoshi , YOSHIKAWA, Seiji , WATANABE, Nobuhisa , INOUE, Takashi , HORIZOE, Tatsuo , YASUDA, Nobuyuki , OHASHI, Kaya , MINAMI, Hiroe , NAGAOKA, Junsaku , MURAKAMI, Manabu , KOBAYASHI, Seiichi , TANAKA, Isao , KAWATA, Tsutomu , SHIMOMURA, Naoyuki , AKAMATSU, Hiroshi , OZEKI, Naoki , SHIMIZU, Toshikazu , HAYASHI, Kenji , HAGA, Toyokazu , NEGI, Shigeto , NAITO, Toshihiko
IPC分类号： C07D473/34 , C07D473/18 , C07D471/08 , C07D473/40 , C07D239/48 , C07D213/73 , C07D213/75 , C07D235/18 , C07D471/04 , C07D487/04 , A61K31/437 , A61K31/52 , A61K31/522 , A61P3/10 , A61P43/00
CPC分类号： C07D471/04 , C07D473/00 , C07D473/34 , C07D473/40
摘要： The present invention provides a preventive or therapeutic agent for diabetes mellitus and diabetic complications, which is a new type based on an adenosine A2 receptor antagonist action.
That is, it provides a novel condensed imidazole compound which has an adenosine A2 receptor antagonist action, is effective for preventing or treating diabetes mellitus and diabetic complications, and is represented by the formula (I):
(wherein R 1 represents e.g. an amino group which may be substituted with an alkyl group; R 2 represents e.g. hydrogen atom, an alkyl group, a cycloalkyl group or an alkyl group, alkenyl group or alkynyl group which may be substituted with hydrox etc.; R 3 represents e.g. an optionally substituted alkyl group, alkenyl group, alkynyl group, aryl group, heteroaryl group, pyridinone group, pyrimidinone group or piperadinone group; Ar represents e.g. an optionally substituted aryl or heteroaryl group; and Q and W are the same as or different from each other and each represents N or CH), a pharmacologically acceptable salt or hydrates thereof.

4. 发明公开

EP1557165A1 COMBINATION DRUG 审中-公开
标题翻译： KOMBINATIONSARZNEIMITTEL
公开(公告)号：EP1557165A1
公开(公告)日：2005-07-27
申请号：EP03798438.2
申请日：2003-09-22
申请人： Eisai Co., Ltd.
发明人： YASUDA, Nobuyuki , YAMAZAKI, Kazuto
IPC分类号： A61K31/155 , A61K45/00 , A61K31/496 , A61K31/5025 , A61K31/522 , A61P1/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P5/50 , A61P43/00
CPC分类号： A61K31/496 , A61K31/155 , A61K31/5025 , A61K31/522 , A61K45/06 , A61K2300/00
摘要： The present invention provides pharmaceutical agents comprising a dipeptidyl peptidase IV (DPPIV) inhibitor and a biguanide agent in combination, which enhance the effects of active circulating glucagon-like peptide-1 (GLP-1) and/or active circulating glucagon-like peptide-2 (GLP-2).
摘要翻译：本发明提供了包含二肽基肽酶IV（DPPIV）抑制剂和双胍类药物组合的药剂，其增强了活性循环胰高血糖素样肽-1（GLP-1）和/或活性循环胰高血糖素样肽 - 2（GLP-2）。

5. 发明公开

EP1054012A1 PURINE DERIVATIVES AND ADENOSINE A2 RECEPTOR ANTAGONISTS SERVING AS PREVENTIVES/REMEDIES FOR DIABETES 有权
标题翻译：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

6. 发明授权

EP1283056B1 MEDICINAL COMPOSITIONS PROMOTING BOWEL MOVEMENT 有权
标题翻译：医药组合物，为了促进激活GUTS
公开(公告)号：EP1283056B1
公开(公告)日：2004-12-15
申请号：EP01925974.6
申请日：2001-04-26
申请人： Eisai Co., Ltd.
发明人： YASUDA, Masahiro , HARADA, Hitoshi , MIYAZAWA, Shuhei , KOBAYASHI, Seiichi , HARADA, Kokichi , HIDA, Takayuki , SHIBATA, Hisashi , YASUDA, Nobuyuki , ASANO, Osamu , KOTAKE, Yoshihiko
IPC分类号： A61K45/00 , A61K31/506 , A61K31/5377 , A61K31/522 , A61K31/519 , A61P43/00 , A61P1/10 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D513/04 , C07D487/04
CPC分类号： A61K31/506 , A61K31/519 , A61K31/522 , A61K31/5377 , A61K31/7076 , H04B10/112

7. 发明公开

EP1439175A1 PYRIMIDINE COMPOUND AND MEDICINAL COMPOSITION THEREOF 有权
标题翻译：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。

8. 发明公开

EP1283056A1 MEDICINAL COMPOSITIONS PROMOTING BOWEL MOVEMENT 有权
标题翻译：药物组合物促进肠道运动
公开(公告)号：EP1283056A1
公开(公告)日：2003-02-12
申请号：EP01925974.6
申请日：2001-04-26
申请人： Eisai Co., Ltd.
发明人： YASUDA, Masahiro , HARADA, Hitoshi , MIYAZAWA, Shuhei , KOBAYASHI, Seiichi , HARADA, Kokichi , HIDA, Takayuki , SHIBATA, Hisashi , YASUDA, Nobuyuki , ASANO, Osamu , KOTAKE, Yoshihiko
IPC分类号： A61K45/00 , A61K31/506 , A61K31/5377 , A61K31/522 , A61K31/519 , A61P43/00 , A61P1/10 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D513/04 , C07D487/04
CPC分类号： A61K31/506 , A61K31/519 , A61K31/522 , A61K31/5377 , A61K31/7076 , H04B10/112
摘要： The present invention provides a medicament having a gentle but strong defecation-promoting action without causing diarrhea. That is, it provides a defecation-promoting agent comprising a compound having an adenosine A 2 receptor antagonism, preferably an adenosine A 2b receptor antagonism, or a salt thereof.
摘要翻译：本发明提供一种具有温和而强劲的排便促进作用而不引起腹泻的药物。即，它提供了一种排便促进剂，其包含具有腺苷A2受体拮抗作用，优选腺苷A2b受体拮抗作用的化合物或其盐。

9. 发明公开

EP1514552A1 NOVEL FUSED IMIDAZOLE DERIVATIVE 审中-公开
标题翻译：新型稠合咪唑衍生物
公开(公告)号：EP1514552A1
公开(公告)日：2005-03-16
申请号：EP03733276.4
申请日：2003-06-03
申请人： Eisai Co., Ltd.
发明人： YOSHIKAWA, Seiji , EMORI, Eita , MATSUURA, Fumiyoshi , RICHARD, Clark , IKUTA, Hironori , KIRA, Kazunobu , YASUDA, Nobuyuki , NAGAKURA, Tadashi , YAMAZAKI, Kazuto
IPC分类号： A61K35/00
CPC分类号： C07D473/30 , C07D471/04 , C07D473/04 , C07D473/06 , C07D473/18 , C07D473/36 , C07D473/40 , C07D487/04 , C07D491/14
摘要： The present invention is related to compounds represented by the following formula, or salts or hydrates thereof
wherein,
T 1 represents a 4- to 12-membered heterocyclic group containing one or two nitrogen atoms in the ring, which is a monocyclic or bicyclic structure that may have one or more substituents;
X represents a C 1-6 alkyl group which may have one or more substituents, or such;
Z 1 and Z 2 each independently represent a nitrogen atom or a group represented by the formula -CR 2 -;
R 1 and R 2 independently represent a hydrogen atom, a C 1-6 alkyl group which may have one or more substituents, or a C 1-6 alkoxy group which may have one or more substituents, or such.
These are novel compounds that exhibit an excellent DPPIV-inhibiting activity.
摘要翻译：本发明涉及由下式表示的化合物或其盐或水合物，其中，T1表示在环中含有一个或两个氮原子的4至12元杂环基，其为可以是单环或双环结构，具有一个或多个取代基; X表示可具有一个或多个取代基的C 1-6烷基等; Z 1和Z 2各自独立地表示氮原子或式-CR 2 - 表示的基团; R 1和R 2独立地表示氢原子，可具有一个或多个取代基的C 1-6烷基或可具有一个或多个取代基的C 1-6烷氧基等。这些是显示优异的DPPIV抑制活性的新型化合物。

10. 发明公开

EP1439176A1 PYRIMIDONE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME 有权
标题翻译： 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。

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