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1. 发明专利

JP2005145951A New fused imidazole derivative 有权
标题翻译：新熔融咪唑衍生物
公开(公告)号：JP2005145951A
公开(公告)日：2005-06-09
申请号：JP2004249414
申请日：2004-08-30
申请人： Eisai Co Ltd , エーザイ株式会社
发明人： YOSHIKAWA SEIJI , EMORI EITA , MATSUURA FUMIYOSHI , CLARK RICHARD , IKUTA HIRONORI , KIRA KAZUNOBU , YASUDA NOBUYUKI , NAGAKURA TEI , YAMAZAKI KAZUTO
IPC分类号： C07D471/04 , A61K31/496 , A61K31/5025 , A61K31/522 , A61K31/5377 , A61K31/541 , A61P1/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P15/00 , A61P15/08 , A61P19/02 , A61P19/10 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D473/04 , C07D473/06 , C07D473/18 , C07D473/22 , C07D473/24 , C07D473/30 , C07D473/36 , C07D473/40 , C07D487/04 , C07D491/14
CPC分类号： C07D473/30 , C07D471/04 , C07D473/04 , C07D473/06 , C07D473/18 , C07D473/36 , C07D473/40 , C07D487/04 , C07D491/14
摘要： PROBLEM TO BE SOLVED: To provide a compound having a DPPIV (dipeptidyl peptidase IV) inhibitory activity useful as a treating/preventing/improving agent of diseases of diabetes mellitus, etc. SOLUTION: This fused imidazole compound is expressed by general formula (wherein, T 1 is a single ring-formed or two ring-formed 4 to 12-membered heterocyclic ring which may have substituents, and containing one or two nitrogen atoms in the ring; X is a 1-6C alkyl which may have substituents; Z 1 , Z 2 are each independently N or a group expressed by formula: CR 2 ; and R 1 , R 2 are each independently H, a 1-6C alkyl which may have substituents or a 1-6C alkoxy which may have substituents) or its salts or its hydride. These new compounds exhibit excellent DPPIV inhibitory activities. COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译：待解决的问题：提供具有DPPIV（二肽基肽酶IV）抑制活性的化合物，其可用作糖尿病等的治疗/预防/改善剂。解决方案：该稠合咪唑化合物被表达通式（其中，T 1 是可以具有取代基且在环中含有一个或两个氮原子的单环形成或两个环形成的4至12元杂环; X 是可以具有取代基的1-6C烷基; Z 1 ，Z 2 各自独立地为N或由式表示的基团：CR 2 R 1和R 2各自独立地为氢，可具有取代基的1-6C烷基或可具有取代基的1-6C烷氧基或其盐或其氢化物。这些新化合物表现出优异的DPPIV抑制活性。版权所有（C）2005，JPO＆NCIPI

2. 发明专利

JP2003034639A Pharmaceutical application of n-carbamoylazole derivative 有权
标题翻译： N-羧甲基衍生物的药物应用
公开(公告)号：JP2003034639A
公开(公告)日：2003-02-07
申请号：JP2002135555
申请日：2002-05-10
申请人： Eisai Co Ltd , エーザイ株式会社
发明人： YASUDA NOBUYUKI , NAGAKURA TEI , YAMAZAKI KAZUTO , YOSHIKAWA SEIJI , OKADA TOSHIMI , IKUTA HIRONORI , KOYANAGI MIKA
IPC分类号： C07D249/12 , A61K31/4196 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/46 , A61P1/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P9/00 , A61P15/08 , A61P19/10 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D451/04
摘要： PROBLEM TO BE SOLVED: To provide a compound showing excellent action of inhibiting dipeptidylpeptitase IV.
SOLUTION: The dipeptidylpeptitase IV inhibitor contains a compound represented by general formula, [wherein, R
1a means a 6-10C aromatic hydrocarbon cyclic group which may have substituents; n means an integer of 0 to 2; W means a 1-6C alkylene group; X
1 and X
2 each means independly a nitrogen atom or a methyn group; Z means the formula, (wherein R
2a and R
2b each means independently a 1-6C alkyl group, a 2-6C alkenyl group or a phenyl group; Z
2 means a sulfur atom or a methyn group)].
COPYRIGHT: (C)2003,JPO
摘要翻译：要解决的问题：提供抑制二肽基肽酶IV的优异作用的化合物。解决方案：二肽基肽酶IV抑制剂含有由通式表示的化合物[其中，R 1a表示可具有取代基的6-10C芳族烃环基; n表示0〜2的整数， W表示1-6C亚烷基; X 1和X 2各自独立地表示氮原子或甲炔基; Z表示式（其中R 2a和R 2b各自独立地表示1-6C烷基，2-6C烯基或苯基; Z 2表示硫原子或甲炔基） ]。

3. 发明专利

JP2004043429A New xanthine derivative and dppiv inhibitor 审中-公开
标题翻译：新西兰衍生物和DPPIV抑制剂
公开(公告)号：JP2004043429A
公开(公告)日：2004-02-12
申请号：JP2003044771
申请日：2003-02-21
申请人： Eisai Co Ltd , エーザイ株式会社
发明人： YOSHIKAWA SEIJI , EMORI EITA , MATSUURA FUMIYOSHI , CLARK RICHARD , IKUTA HIRONORI , YASUDA NOBUYUKI , NAGAKURA TEI , YAMAZAKI KAZUTO , AOKI MIKA
IPC分类号： C07D473/04 , A61K31/522 , A61K31/551 , A61P1/04 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P9/00 , A61P15/08 , A61P19/10 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D473/06 , C07D473/08 , C07D487/22 , C07D519/00
摘要： PROBLEM TO BE SOLVED: To provide a new compound exhibiting excellent DPPIV (dipeptidyl peptidase IV) inhibiting action. SOLUTION: The new compound exhibiting excellent DPPIV inhibiting action is represented by general formula (1) (wherein m is 0 or 1; n is 0; R 31 , R 32 , R 33 , R 34 , R 35 , R 36 , R 37 , R 38 , R 39 , R 40 , R 41 and R 42 are each a hydrogen atom; X is an alkynyl group, an aryl group or the like which may be substituted; R 1 and R 2 are each independently a hydrogen atom, an alkyl group, an alkoxy group or the like), its salt or a hydrate thereof. COPYRIGHT: (C)2004,JPO
摘要翻译：要解决的问题：提供显示优异的DPPIV（二肽基肽酶IV）抑制作用的新化合物。解决方案：通过通式（1）（其中m是0或1; n是0; SP>，R 33 ，R 34 ，R 35 ，R SP SP 36， SP>，R 38 ，R 39 ，R 40 ，R SP SP 41， SP>各自为氢原子; X为可被取代的炔基，芳基等; R SP 1和R SP 2各自独立地为氢原子，烷基，烷氧基等），其盐或其水合物。版权所有（C）2004，JPO

4. 发明专利

JP2008031042A Method for producing n-(3-chloro-1h-indol-7-yl)-4-sulfamoylbenzenesulfonamide 审中-公开
标题翻译：生产N-（3-氯代-1H-吲哚-7-基）-4-磺酰氨基苯甲酰胺的方法
公开(公告)号：JP2008031042A
公开(公告)日：2008-02-14
申请号：JP2004332758
申请日：2004-11-17
申请人： Eisai Co Ltd , エーザイ株式会社
发明人： IKUTA HIRONORI , SHIMOMURA NAOYUKI , AKAMATSU HIROSHI
IPC分类号： C07D209/30
CPC分类号： C07D209/30 , B01J23/468 , C07D209/08
摘要： PROBLEM TO BE SOLVED: To provide a method for producing 3-chloro-7-nitroindole (II) and N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzene sulfonamide (VI) in good efficiency.
SOLUTION: The method for producing N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide (VI) having a high purity comprises chlorinating 7-nitroindole with N-chlorosuccinimide in a hydrous solvent to produce 3-chloro-7-nitroindole (II) and reducing the compound (II) to obtain 3-chloro-7-aminoindole or its hydrochloride and reacting the 3-chloro-7-aminoindole or its hydrochloride in the presence of a base with 4-sulfamoylbenzenesulfonyl chloride synthesized from 4-aminobenzenesulfonamide.
COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：待解决的问题：提供良好的3-氯-7-硝基吲哚（II）和N-（3-氯-1H-吲哚-7-基）-4-氨磺酰基苯磺酰胺（VI）的制备方法效率。解决方案：制备具有高纯度的N-（3-氯-1H-吲哚-7-基）-4-氨磺酰基苯磺酰胺（Ⅵ）的方法包括用N-氯代琥珀酰亚胺在含水溶剂中氯化7-硝基吲哚以产生 3-氯-7-硝基吲哚（II）并还原化合物（II），得到3-氯-7-氨基吲哚或其盐酸盐，并在碱的存在下将3-氯-7-氨基吲哚或其盐酸盐与4 - 氨磺酰基苯磺酰氯，由4-氨基苯磺酰胺合成。版权所有（C）2008，JPO＆INPIT

5. 发明公开

EP0607439A4 NITROGENOUS HETEROCYCLIC COMPOUND. 失效
标题翻译：含氮化合物HYDROCYCLISCHE。
公开(公告)号：EP0607439A4
公开(公告)日：1994-12-07
申请号：EP92920913
申请日：1992-09-30
申请人： EISAI CO LTD
发明人： TAKASE YASUTAKA , WATANABE NOBUHISA , MATSUI MAKOTO , IKUTA HIRONORI , KIMURA TEIJI , SAEKI TAKAO , ADACHI HIDEYUKI , TOKUMURA TADAKAZU , MOCHIDA HISATOSHI , AKITA YASUNORI , SOUDA SHIGERU
IPC分类号： C07D215/42 , A61K31/415 , A61K31/4184 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/454 , A61K31/4706 , A61K31/4709 , A61K31/496 , A61K31/505 , A61K31/517 , A61K31/519 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/06 , A61P37/00 , A61P43/00 , B60S1/16 , B60S1/24 , C07D215/48 , C07D235/06 , C07D235/08 , C07D239/78 , C07D239/84 , C07D239/86 , C07D239/88 , C07D239/90 , C07D239/94 , C07D239/95 , C07D239/96 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/12 , C07D471/04 , C07D491/04 , C07D491/056 , C07D521/00 , F16C7/02 , F16C11/04 , C07D215/00 , A61K31/47 , C07D235/00 , C07D239/72
CPC分类号： C07D491/04 , C07D215/42 , C07D231/12 , C07D233/56 , C07D235/06 , C07D239/84 , C07D239/86 , C07D239/88 , C07D239/94 , C07D239/95 , C07D239/96 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/10 , C07D413/12 , C07D471/04 , Y10T74/18184 , Y10T403/7015
摘要： A nitrogenous heterocyclic compound represented by general formula (I) or a pharmacologically acceptable salt thereof, efficacious in treating various ischemic cardiac diseases, wherein ring A represents a benzene, pyridine or cyclohexane ring; ring B represents a pyridine, pyrimidine or imidazole ring; R?1, R2, R3 and R4¿ represent each hydrogen, halogen, lower alkoxy, etc.; R5 represents -NR11R12 (wherein R?11 and R12¿ represent each hydrogen, lower alkyl, etc.), etc.; and R6 represents (a) (wherein R19 represents hydrogen, lower alkyl, etc.; R?20, R21 and R22¿ represent each hydrogen, halogen, hydroxy, etc.; and r represents an integer of 0.1 to 8), etc.

6. 发明公开

EP1217001A4 QUINUCLIDINE COMPOUNDS AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT 有权
标题翻译：胶原蛋白 - VERBINDUNGEN UND MEDIKAMENTE DIESE ALS AKTIVE WIRKSTOFFE ENTHALTEN
公开(公告)号：EP1217001A4
公开(公告)日：2002-12-18
申请号：EP00962889
申请日：2000-09-27
申请人： EISAI CO LTD
发明人： OKADA TOSHIMI , KURUSU NOBUYUKI , TANAKA KEIGO , MIYAZAKI KAZUKI , SHINMYO DAISUKE , SUGUMI HIROYUKI , IKUTA HIRONORI , HIYOSHI HIRONOBU , SAEKI TAKAO , YANAGIMACHI MAMORU , ITO MASASHI
IPC分类号： A61K31/444 , A61K31/4545 , A61K31/506 , A61K31/5377 , A61P3/06 , A61P9/10 , A61P43/00 , C07D453/02 , A61K31/439 , C07D491/04 , C07D491/10 , C07M7/00
CPC分类号： C07D453/02
摘要： Compounds represented by general formula (I), salts thereof, or hydrates of both, useful as excellent squalene synthase inhibitors wherein R1 is hydrogen or hydroxyl; HAr is an optionally substituted aromatic heterocycle; Ar is an optionally substituted aromatic ring; W is (1) a -CH¿2?-CH2- group which may be substituted, (2) a -CH=CH- group which may be substituted, (3) -C C-, (4) -NH-CO-, or the like; and X is a single bond, optionally substituted C1-6 alkylene, (5) -Q- [wherein Q is oxygen, sulfur, CO, or N(R?2¿) (wherein R2 is C¿1-6? alkyl or C1-6 alkoxy)], (6) -NH-CO-, or the like.
摘要翻译：通式（I）代表的化合物，其盐或两者的水合物，用作优良的角鲨烯合成酶抑制剂，其中R1是氢或羟基; HAr是任选取代的芳族杂环; Ar是任选取代的芳族环; W是（1）可被取代的-CH 2 -CH 2 - 基，（2）可被取代的-CH = CH-基，（3）-C≡C-，（4）-NH-CO - 等等; （5）-Q- [其中Q是氧，硫，CO或N（R 2'）（其中R 2是C 1-6 - 烷基）;或者X是单键，任选取代的C 1-6亚烷基， C 1-6烷氧基）]，（6）-NH-CO-等。

7. 发明公开

EP0686625A4 ANTHRANILIC ACID DERIVATIVE 失效
标题翻译： ANTHRANILSÄUREDERIVATE
公开(公告)号：EP0686625A4
公开(公告)日：1996-05-01
申请号：EP95903999
申请日：1994-12-27
申请人： EISAI CO LTD
发明人： OZAKI FUMIHIRO , ISHIBASHI KEIJI , IKUTA HIRONORI , ISHIHARA HIROKI , SOUDA SHIGERU
IPC分类号： A61K31/24 , A61K31/41 , A61K31/415 , A61K31/452 , A61P3/00 , C07C217/58 , C07C229/56 , C07C229/64 , C07C237/30 , C07C237/32 , C07C237/40 , C07C237/42 , C07C237/44 , C07C255/57 , C07C255/58 , C07C255/59 , C07C255/60 , C07C311/39 , C07C311/40 , C07C311/51 , C07D211/46 , C07D211/62 , C07D213/40 , C07D213/64 , C07D213/81 , C07D265/26 , C07D295/15 , C07D295/155 , C07D307/33 , C07D317/48 , C07D317/58 , C07D317/60 , C07D405/06 , C07D405/12 , C07D521/00 , A61K31/36 , A61K31/44 , A61K31/445 , A61K31/495
CPC分类号： C07D213/40 , C07C217/58 , C07C229/56 , C07C229/64 , C07C237/30 , C07C237/32 , C07C237/40 , C07C237/42 , C07C237/44 , C07C255/57 , C07C255/58 , C07C255/59 , C07C255/60 , C07C311/39 , C07C311/40 , C07C311/51 , C07C2601/14 , C07C2601/16 , C07D211/46 , C07D211/62 , C07D213/64 , C07D213/81 , C07D231/12 , C07D233/56 , C07D249/08 , C07D265/26 , C07D295/15 , C07D295/155 , C07D307/33 , C07D317/48 , C07D317/58 , C07D405/06 , C07D405/12
摘要： An anthranilic acid derivative having a cGMP-PDE inhibitory activity and represented by general formula (I), or a pharmacologically acceptable salt thereof wherein R?1, R2, R3 and R4¿ represent each independently hydrogen, halogen, hydroxy, optionally halogenated lower alkyl, optionally halogenated lower alkoxy, nitro, hydroxyalkyl, cyano, etc.; R?5 and R6¿ represent each independently hydrogen, halogen hydroxy, cyano, optionally halogenated lower alkyl, optionally halogenated lower alkoxy, etc.; W represents -N= or -CH=; R?7 and R8¿ represent each independently hydrogen, optionally halogenated lower alkyl, etc.; A represents hydrogen, optionally halogenated lower alkyl, etc.; Z represents hydroxy, optionally halogenated lower alkoxy, cyano, halogen, etc.; Y represents oxygen or sulfur; and n represents an integer of 0, 1 to 6.
摘要翻译：由通式（I）表示的具有cGMP-PDE抑制活性的邻氨基苯甲酸衍生物或其药理学上可接受的盐，其中R 1，R 2，R 3和R 4各自独立地表示氢卤素，羟基，任选卤代的低级烷基，任意卤代的低级烷氧基，硝基，羟烷基，氰基等; R 5和R 6各自独立地表示氢，卤素羟基，氰基，任选卤代的低级烷基，任选卤代的低级烷氧基等; W表示-N =或-CH =; R 7和R 8各自独立地表示氢，任选卤代的低级烷基等; A表示氢，任选卤代的低级烷基等; Z表示羟基，任选卤代的低级烷氧基，氰基，卤素等; Y表示氧或硫; n表示0〜1的整数

8. 发明公开

EP1375496A4 N-ARYL-SUBSTITUTED CYCLIC AMINE DERIVATIVE AND MEDICINE CONTAINING THE SAME AS ACTIVE INGREDIENT 有权
标题翻译： N-ARYL-SUBSTITUIERTES CYCLISCHES AMINDERIVAT ANDD MEDIZIN，DIESES ALS WIRKSTOFFENTHÄLT
公开(公告)号：EP1375496A4
公开(公告)日：2004-06-16
申请号：EP02707189
申请日：2002-03-27
申请人： EISAI CO LTD
发明人： OKADA TOSHIMI , KURUSU NOBUYUKI , TANAKA KEIGO , YOSHIKAWA SEIJI , SHINMYO DAISUKE , WATANABE NOBUHISA , IKUTA HIRONORI , HIYOSHI HIRONOBU , SAEKI TAKAO , YANAGIMACHI MAMORU , ITO MASASHI
IPC分类号： A61K31/435 , A61K31/439 , A61K31/4545 , A61P3/06 , A61P9/00 , A61P9/10 , A61P9/12 , A61P43/00 , C07D401/04 , C07D401/14 , C07D453/04 , C07D471/18 , C07D491/10 , C07D491/113 , C07D451/14 , C07D453/02
CPC分类号： C07D401/04 , A61K31/435 , A61K31/439 , A61K31/4545 , C07D401/14 , C07D453/04 , C07D491/10
摘要： A compound having excellent squalene synthetase inhibitory activity. It is a compound (I) represented by the following general formula, a salt thereof, or a hydrate of either. (I) In the formula, R1 means optionally substituted vinyl or an optionally substituted aromatic ring; n is an integer of 0 to 2; X, Y, and Z are the same or different and each means optionally substituted carbon, nitrogen, etc.; CyA means an optionally substituted 5- to 14-membered nonaromatic cyclic amino group optionally containing oxygen or sulfur; W means -C=C-, etc.; and A means a group of the formula (II) (wherein R8 represents hydrogen, hydroxy, etc.; B2 represents optionally substituted carbon or nitrogen; and c is 0 or 1), etc.
摘要翻译：具有优异的角鲨烯合成酶抑制活性的化合物。它是由下列通式表示的化合物（I），其盐或任一种的水合物。（I）式中，R 1表示可以具有取代基的乙烯基或可以具有取代基的芳香族环; n是0至2的整数; X，Y和Z相同或不同，各自表示任选取代的碳，氮等; CyA是指任选取代有氧或硫的任选取代的5至14元非芳族环状氨基; W表示-C = C-等; A表示式（II）的基团（式中，R 8表示氢，羟基等，B 2表示可以被取代的碳或氮，c为0或1）等。

9. 发明公开

EP0609440A4 PHOSPHORUS-SUBSTITUTED ISOPRENOID DERIVATIVE. 失效
标题翻译：磷酸二氢钠
公开(公告)号：EP0609440A4
公开(公告)日：1995-01-18
申请号：EP92918492
申请日：1992-08-27
申请人： EISAI CO LTD
发明人： TAGAMI KATSUYA , YOSHIDA ICHIRO , KOBAYASHI NAOKI , FUKUDA YOSHIO , EGUCHI YOSHIHITO , NAKAGAWA MAKOTO , HIYOSHI HIRONOBU , IKUTA HIRONORI , KAINO MAKOTO , HAYASHI KENJI , OHTSUKA ISSEI , ABE SHINYA , SOUDA SHIGERU
IPC分类号： A61K31/66 , A61P3/06 , C07C211/21 , C07C233/03 , C07F9/38 , C07F9/40
CPC分类号： C07F9/405 , C07C211/21 , C07C233/03 , C07F9/3808 , C07F9/3826 , C07F9/3843 , C07F9/3873 , C07F9/4006 , C07F9/4015 , C07F9/4025
摘要： A phosphorus-substituted isoprenoid derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, useful for preventing and treating diseases for which a squalene synthetase inhibition is efficacious. In formula (I), R?1 and R2¿ represent each hydrogen, lower alkyl, cycloalkyl, alkenyl, alkynyl, aryl which may be substituted, arylalkyl which may be substituted on the aryl moiety, heteroaryl or heteroarylalkyl; R?3 and R4¿ represent each hydrogen, lower alkyl or alkali metal; Y represents -P(O)(OR5)(OR6) (wherein R?5 and R6¿ represent each hydrogen, lower alkyl or alkali metal) or -CO¿2R?7 (wherein R7 represents hydrogen, lower alkyl or alkali metal); Z represents -(CH¿2?)m- (wherein m represents an integer of 0 or 1 to 3), -(CH2)p-CH=CH-(CH2)q- (wherein m represents 0 or 1 and q represents 1 or 2), or -A-NR?8-(CH¿2)r- (wherein R8 represents hydrogen or lower alkyl, A represents C¿1? to C5 alkylene, and r represents an integer of 0 or 1 to 5); and n represents an integer of 0 or 1 to 5.

10. 发明专利

JP2000273089A NITROGEN-CONTAINING HETEROCYCLIC COMPOUND 失效
公开(公告)号：JP2000273089A
公开(公告)日：2000-10-03
申请号：JP2000070138
申请日：2000-03-14
申请人： EISAI CO LTD
发明人： TAKASE YASUTAKA , WATANABE NOBUHISA , MATSUI MAKOTO , IKUTA HIRONORI , KIMURA TEIJI , SAEKI TAKAO , ADACHI HIDEYUKI , TOKUMURA CHUICHI , MOCHIDA HISATOSHI , AKITA YASUNORI , SODA SHIGERU
IPC分类号： C07D215/42 , A61K31/415 , A61K31/4184 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/454 , A61K31/4706 , A61K31/4709 , A61K31/496 , A61K31/505 , A61K31/517 , A61K31/519 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/06 , A61P37/00 , A61P43/00 , B60S1/16 , B60S1/24 , C07D215/48 , C07D235/06 , C07D235/08 , C07D239/78 , C07D239/84 , C07D239/86 , C07D239/88 , C07D239/90 , C07D239/94 , C07D239/95 , C07D239/96 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/12 , C07D471/04 , C07D491/04 , C07D491/056 , C07D521/00 , F16C7/02 , F16C11/04
摘要： PROBLEM TO BE SOLVED: To obtain a new nitrogen-containing heterocyclic compound having cGMP phosphodiesterase-inhiviting action and effective against various kinds of ischemic heart diseases. SOLUTION: This new nitrogen-containing heterocyclic compound is expressed by formula I (wherein R1-R4 are each H, a halogen a lower alkyl, a cycloalkyl, a lower alkoxy, a hydroxyalkyl or the like; R5 is H, a halogen, hydroxyl group, hydrazino, a lower alkyl or the like; R6 is H, a halogen, hydroxyl group, amino, a lower alkyl, a lower alkoxy or the like) and is e.g. a 5-chloro-2- methanesulfonyl-1-(3,4-methylenedioxybenzyl)benzimidazole of formula II. For example, by the condensation reaction of a benzimidazole derivative of formula III (wherein R5a is H, a halogen, a heteroaryl or the like; E is a leaving group) with a compound of formula IV (wherein R6a is a group selected from R6 except H, a halogen and a lower alkyl), a compound of formula V is obtained.

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