公开(公告)号：EP0454330A1

公开(公告)日：1991-10-30

申请号：EP91303264.5

申请日：1991-04-12

申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD.

发明人： Hara, Hiromu ,  Maruyama, Tatsuya ,  Saito, Munetoshi ,  Takeuchi, Makoto ,  Mase, Toshiyasu

IPC分类号： C07D235/26 ,  A61K31/415 ,  C07D403/04

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D235/26 ,  C07D249/08

摘要： Benzimidazolinone derivatives of the general formula (I):
wherein R 1 , R 2 and R 3 , which may be the same or different, each is a hydrogen or halogen atom or a lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxyl, lower alkoxy, aryloxy, acyl, cyano, carboxyl, a lower alkoxycarbonyl, carbamoyl, nitro or nitrogen-containing 5- or 6-membered heterocyclic group; A is an ethylene group which may optionally have at least one branch ; R 4 and R 5 , which may be the same or different, each is a lower alkyl group or R 4 and R 5 , together with the adjacent nitrogen atom, represent a pyrrolidinyl, piperidino or a morpholino group provided that when
is a piperidino or diethylamino group, at least one of R 1 , R 2 and R 3 is other than a hydrogen atom, or pharmaceutically acceptable salts thereof, methods of producing the same and pharmaceutical compositions containing the same are disclosed. Pharmacologically, the above compounds (I) have pulmonary surfactant secretion promoting activity.

摘要翻译： 通式（I）的苯并咪唑啉酮衍生物：其中R1，R2和R3可以相同或不同，各自是氢或卤原子或低级烷基，卤代低级烷基，羟基低级烷基，羟基，低级 烷氧基，芳氧基，酰基，氰基，羧基，低级烷氧羰基，氨基甲酰基，硝基或含氮的5-或6-元杂环基团; A是任选具有至少一个分支的亚乙基; R4和R5可以相同或不同，各自为低级烷基或R4和R5与相邻的氮原子一起代表吡咯烷基，哌啶子基或吗啉代基，条件是当为哌啶子基或二乙基氨基时，在 公开了R 1，R 2和R 3中的至少一个不是氢原子，或其药学上可接受的盐，其制备方法和包含其的药物组合物。 在药理学上，上述化合物（I）具有促进肺表面活性物质分泌的活性。

公开(公告)号：EP0350145A3

公开(公告)日：1990-07-04

申请号：EP89303137.7

申请日：1989-03-30

申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD.

发明人： Mase, Toshiyasu ,  Hara, Hiromu ,  Yamada, Toshimitsu

IPC分类号： C07D295/10 ,  C07D417/04 ,  C07D417/14 ,  A61K31/425

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D307/52 ,  C07D333/20 ,  C07D417/04 ,  C07D417/14

摘要： This invention provides pyridylthiazolidine carboxamide derivatives shown by general formula (I) and pharmaceutically acceptable salts thereof:
wherein A¹ is a single bond, carbonyl group or lower alkylene group which may include a carbonyl group and R¹ is a heterocyclic ring which may be substituted with a lower alkyl group; it further provides N-­substituted piperazine derivatives useful as intermediates for preparing said compounds (I). Compounds (I) and their salts have PAF-antagonistic activity.

公开(公告)号：EP0350145A2

公开(公告)日：1990-01-10

申请号：EP89303137.7

申请日：1989-03-30

申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD.

发明人： Mase, Toshiyasu ,  Hara, Hiromu ,  Yamada, Toshimitsu

IPC分类号： C07D295/10 ,  C07D417/04 ,  C07D417/14 ,  A61K31/425

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D307/52 ,  C07D333/20 ,  C07D417/04 ,  C07D417/14

摘要： This invention provides pyridylthiazolidine carboxamide derivatives shown by general formula (I) and pharmaceutically acceptable salts thereof:
wherein A¹ is a single bond, carbonyl group or lower alkylene group which may include a carbonyl group and R¹ is a heterocyclic ring which may be substituted with a lower alkyl group; it further provides N-­substituted piperazine derivatives useful as intermediates for preparing said compounds (I). Compounds (I) and their salts have PAF-antagonistic activity.

摘要翻译： 本发明提供通式（I）所示的吡啶并噻唑烷羧酰胺衍生物及其药学上可接受的盐：其中A 1为单键，羰基或可包含羰基的低级亚烷基，R 1为 可以被低级烷基取代的杂环; 它还提供了用作制备所述化合物（I）的中间体的N-取代的哌嗪衍生物。 化合物（I）及其盐具有PAF拮抗活性。

公开(公告)号：EP0279681A3

公开(公告)日：1989-11-15

申请号：EP88301397.1

申请日：1988-02-19

申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD.

发明人： Mase, Toshiyasu ,  Hara, Hiromu ,  Nagaoka, Hitoshi ,  Takahasi, Takumi ,  Suzuki, Takeshi ,  Tomioka, Kenichi ,  Yamada, Toshimitsu

IPC分类号： C07D417/04 ,  C07D401/04 ,  C07D405/04 ,  C07D413/04 ,  A61K31/41 ,  A61K31/435

CPC分类号： C07D401/04 ,  C07D405/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14

摘要： A saturated heterocyclic carboxamide derivative of the following general formula (I) and salts thereof which have platelet activating factor (PAF) antagonizing activity.

公开(公告)号：EP0214732A2

公开(公告)日：1987-03-18

申请号：EP86305633.9

申请日：1986-07-22

申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD.

发明人： Mase, Toshiyasu ,  Murase, Kiyoshi ,  Tsuzuki, Ryuji ,  Tomioka, Kenichi ,  Hara, Hiromu

IPC分类号： C07D285/12 ,  C07D239/56 ,  C07D213/70 ,  C07D249/12 ,  C07D275/02 ,  A61K31/41 ,  A61K31/44 ,  A61K31/505

CPC分类号： C07D213/70 ,  C07D239/56 ,  C07D249/12 ,  C07D275/03 ,  C07D285/125 ,  C07D285/135

摘要： Heterocyclic compound of formula (I) and salts thereof are SRS-A antagonists:
wherein R' is a C 1 to C 8 acyl group; R 2 is a C 1 to C a alkyl group; Het- is a 5- or 6-membered heterocyclic ring which contains 1 to 3 nitrogen atoms and may additionally contain a sulfur atom or an oxygen atom; R 3 is a carboxy group, an amino group, a C 1 to C 8 alkylamino group which may be carboxy-substituted, a C, to C 8 alkanoylamino group which may be carboxy-substituted, a di-(C 1 -C 8 alkyl) amino group, a hydroxy group, a C 1 to C 8 alkoxy group which may be carboxy-substituted, a mercapto group, a C 1 -C 8 alkylthio group which may be carboxy-substituted, a group of formula:
or formula:
(wherein p is integer of 1 to 5, q is 0, 1 or 2, r is an integer of 1 to 5; R 4 is a carboxy group, a C 1 -C 8 alkoxy group which may be carboxy-substituted or a C 1 -C 8 alkyl group which may be carboxy-substituted and optionally additionally contain a sulfur atom or an oxygen atom in the carbon chain thereof); and n is 0 or an integer of to 3; provided that when the compound is substituted by a carboxy group, said carboxy group may be in the form of an ester, and when n is 2 or 3 different R 3 's is may be present.

摘要翻译： 式（I）的杂环化合物及其盐是SRS-A拮抗剂：... 其中R 1是C 1至C 8酰基; R 2是C 1至C 8烷基; Het是含有1至3个氮原子并可另外含有硫原子或氧原子的5-或6-元杂环; R 3是羧基，氨基，可被羧基取代的C1〜C8烷基氨基，可以被羧基取代的C1〜C8烷酰基氨基，二 - （C1-C8烷基）氨基， 羟基，可以被羧基取代的C1〜C8烷氧基，巯基，可以被羧基取代的C1-C8烷硫基，式：...... ...或式：...... ...（其中p为1至5的整数，q为0,1或2，r为1至5的整数; R 4为羧基，可为羧基的C 1 -C 8烷氧基 或可被羧基取代的C 1 -C 8烷基，并且任选地在其碳链中另外含有硫原子或氧原子）; n为0或1〜3的整数， 条件是当化合物被羧基取代时，所述羧基可以是酯的形式，当n是2或3个不同的R 3时，可以存在分子s。