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1. 发明公开

EP0279681A3 Saturated heterocyclic carboxamide derivatives 失效
标题翻译：饱和杂环碳酰胺衍生物
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.

2. 发明公开

EP0214732A2 (Substituted benzyl)-thio heterocyclic compounds having a leukotriene-antagonist activity 失效
标题翻译：（取代苄基） - 硫代杂环维生素，死亡白细胞素拮抗剂 - 维尔京。
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。

3. 发明公开

EP0125919A3 Catechol derivatives, their production and intermediates therefor, and pharmaceutical compositions containing them 失效
标题翻译： CATECHOL衍生物及其生产及其中间体及含有它们的药物组合物
公开(公告)号：EP0125919A3
公开(公告)日：1987-01-21
申请号：EP84303257
申请日：1984-05-14
申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD.
发明人： Murase, Kiyoshi , Arima, Hideki , Mase, Toshiyasu , Tomioka, Kenichi
IPC分类号： C07C39/11 , C07C37/00 , C07C49/245 , C07C43/23 , C07C41/26 , C07C41/30 , A61K31/05 , A61K31/12 , C07C45/29 , C07C45/68
CPC分类号： C07C59/64 , C07C37/002 , C07C37/055 , C07C37/62 , C07C39/11 , C07C41/26 , C07C43/23 , C07C45/292 , C07C45/59 , C07C45/673 , C07C45/68 , C07C45/71 , C07C45/72 , C07C49/245 , C07C49/248 , C07C49/255 , C07C49/84 , C07C59/52 , C07C2601/14 , C07F9/4006 , C07C43/1783 , C07C39/245
摘要： A catechol derivative represented by the formula
wherein R' represents a hydrogen atom or a C, to C 5 alkyl group; R 2 represents a hydrogen atom or a halogen atom; X represents a straight chain or branched alkylene group having 1 to 15 carbon atoms or a vinylene group; Y represents a carbonyl group or a group represented by
represents a hydrogen atom or a C, to C. alkyl group) and Z represents a hydrogen atom, a straight chain or branched alkyl group having 1 to 15 carbon atoms ora cycloalkyl group; the sum of the carbon atoms of said X and Z being at least 3. The compounds of this invention are useful for the prophylaxis and treatment for various allergic diseases, ischemic heart diseases an inflammations caused by slow reacting substance of anaphylaxis (SRS-A), since the compounds inhibit very potently the formation and release of SRS-A.
摘要翻译：由式表示的儿茶酚衍生物本发明的化合物可用于预防和治疗由过敏反应物质（SRS-A）引起的各种过敏性疾病，缺血性心脏病和炎症，因为该化合物非常抑制有力地形成和释放SRS-A。

4. 发明公开

EP0082712A3 2-Phenylimidazo(2,1-b)benzothiazole compounds, salts thereof, process for producing them, and pharmaceutical compositions containing them 失效
标题翻译： 2-苯基咪唑（2,1-B）苯并噻唑化合物，其制备方法及其制备方法，以及含有它们的药物组合物
公开(公告)号：EP0082712A3
公开(公告)日：1984-08-01
申请号：EP82306804
申请日：1982-12-20
申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD.
发明人： Murase, Kiyoshi , Mase, Toshiyasu , Arima, Hideki , Niigata, Kunihiro , Tomioka, Kenichi , Kobayashi, Shinichiro
IPC分类号： C07D513/04 , A61K31/425 , C07D277/00 , C07D235/00
CPC分类号： C07D513/04
摘要： Novel 2-phenylimidazo[2,1-b]benzothiazole compounds shown by general formula I TAKE IN
and the salts thereof, a process of producing the compounds, and pharmaceutical compositions containing the compounds. The compounds of this invention act on immune response, in particular, suppress delayed type hypersensitivity reaction, and are useful as antiallergic agents, antirheumatics, therapeutic agents for autoimmune diseases, and suppressants of rejection after tissue transplantation and skin graft.

5. 发明公开

EP0030436A1 2-Hydroxyoxanilic acid derivatives and salts, their preparation and pharmaceutical compositions containing them 失效
标题翻译： 2-Hydroxyoxalsäureanilid和它们的盐，它们的制备的衍生物和含有它们的药物组合物。
公开(公告)号：EP0030436A1
公开(公告)日：1981-06-17
申请号：EP80304303.3
申请日：1980-11-28
申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD.
发明人： Murase, Kiyoshi , Mase, Toshiyasu , Arima, Hideki , Tomioka, Kenichi , Numasaki, Yoso Nishiageo
IPC分类号： C07C103/38 , C07C103/42 , C07C103/44 , C07C103/46 , C07C103/85 , C07C102/04 , C07C109/087 , C07C121/80 , C07C125/065 , C07C127/19 , C07C143/68
CPC分类号： C07D295/185 , C07C243/00 , C07C255/00 , C07C275/40
摘要： 2-hydroxyoxanilic acid derivatives shown by the following formula
and salts thereof possess an immunoregulatory action and can be useful as antiallergic agents, antiasthmatics, antirheumatics, carcinostatic agents, therapeutic agents for autoimmune disease, and suppressants of rejection in tissue transplants and skin grafts. They can be made from the corresponding aminophenols and oxalylic acids.
摘要翻译：由下式所示的2- hydroxyoxanilic酸衍生物... ...和它们的盐具有免疫调节作用，并且可以是作为抗过敏剂，抗哮喘药，抗风湿药，制癌剂，用于治疗自身免疫疾病的治疗剂，并在排斥抑制剂有用组织移植和皮肤移植。他们可以从相应的氨基苯酚和oxalylic酸制成。

6. 发明授权

EP0082712B1 2-Phenylimidazo(2,1-b)benzothiazole compounds, salts thereof, process for producing them, and pharmaceutical compositions containing them 失效
标题翻译： 2-苯基咪唑（2,1-B）苯并噻唑化合物，其制备方法及其制备方法以及含有它们的药物组合物
公开(公告)号：EP0082712B1
公开(公告)日：1987-06-16
申请号：EP82306804.4
申请日：1982-12-20
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
发明人： Murase, Kiyoshi , Mase, Toshiyasu , Arima, Hideki , Niigata, Kunihiro , Tomioka, Kenichi , Kobayashi, Shinichiro
IPC分类号： C07D513/04 , A61K31/425
CPC分类号： C07D513/04

7. 发明授权

EP0030436B1 2-Hydroxyoxanilic acid derivatives and salts, their preparation and pharmaceutical compositions containing them 失效
标题翻译： 2-羟基羧酸衍生物及其制备及其含有它们的制剂和药物组合物
公开(公告)号：EP0030436B1
公开(公告)日：1984-05-09
申请号：EP80304303.3
申请日：1980-11-28
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
发明人： Murase, Kiyoshi , Mase, Toshiyasu , Arima, Hideki , Tomioka, Kenichi , Numasaki, Yoso Nishiageo
IPC分类号： C07C103/38 , C07C103/42 , C07C103/44 , C07C103/46 , C07C103/85 , C07C102/04 , C07C109/087 , C07C121/80 , C07C125/065 , C07C127/19 , C07C143/68
CPC分类号： C07D295/185 , C07C243/00 , C07C255/00 , C07C275/40

8. 发明公开

EP0082712A2 2-Phenylimidazo(2,1-b)benzothiazole compounds, salts thereof, process for producing them, and pharmaceutical compositions containing them 失效
标题翻译： 2-苯基咪唑（2,1-b）的苯并噻唑化合物，它们的盐，它们的制备方法和含有它们的药物组合物。
公开(公告)号：EP0082712A2
公开(公告)日：1983-06-29
申请号：EP82306804.4
申请日：1982-12-20
申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD.
发明人： Murase, Kiyoshi , Mase, Toshiyasu , Arima, Hideki , Niigata, Kunihiro , Tomioka, Kenichi , Kobayashi, Shinichiro
IPC分类号： C07D513/04 , A61K31/425
CPC分类号： C07D513/04
摘要： Novel 2-phenylimidazo[2,1-b]benzothiazole compounds shown by general formula I TAKE IN
and the salts thereof, a process of producing the compounds, and pharmaceutical compositions containing the compounds.
The compounds of this invention act on immune response, in particular, suppress delayed type hypersensitivity reaction, and are useful as antiallergic agents, antirheumatics, therapeutic agents for autoimmune diseases, and suppressants of rejection after tissue transplantation and skin graft.

9. 发明公开

EP0425134A1 Condensed pyrrolo derivatives, process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：稠合的吡咯衍生物，它们的制备方法和含有它们的药物组合物。
公开(公告)号：EP0425134A1
公开(公告)日：1991-05-02
申请号：EP90311144.1
申请日：1990-10-11
申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD.
发明人： Mase, Toshiyasu , Nagaoka, Hitoshi , Kondoh, Yutaka , Tomioka, Kenichi , Yamada, Toshimitsu
IPC分类号： C07D513/04 , A61K31/425 , A61K31/54
CPC分类号： C07D513/04
摘要： A heterocyclic compound of the formula (I):
and a pharmacologically acceptable salt thereof which have platelet activating factor (PAF) antagonizing activity are disclosed.
摘要翻译：式（I）的杂环化合物：及它们的哪个具有血小板活化因子的药理学上可接受的盐（PAF）拮抗活性的游离缺失光盘。

10. 发明公开

EP0279681A2 Saturated heterocyclic carboxamide derivatives 失效
标题翻译： Gesättigte杂种Carboxamidderivate。
公开(公告)号：EP0279681A2
公开(公告)日：1988-08-24
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.
摘要翻译：具有下列通式（I）的饱和杂环羧酰胺衍生物及其盐，其具有血小板活化因子（PAF）拮抗活性。 v

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