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1. 发明公开

EP0431571A3 Cis-Bicyclo[4.3.0]non-2-ene derivatives 失效
标题翻译：顺式 - 双环[4.3.0]壬-2-烯衍生物
公开(公告)号：EP0431571A3
公开(公告)日：1992-01-02
申请号：EP90123253.8
申请日：1990-12-04
申请人： SAGAMI CHEMICAL RESEARCH CENTER , TOA EIYO LTD.
发明人： Shibasaki, Masakatsu , Takahasi, Atsuo , Aoki, Tuyosi , Sato, Hiroyasu , Yamada, Shin-ichi , Kudo, Michiko , Yamaguchi, Takaji , Kogi, Kentaro , Narita, Sen-ichi
IPC分类号： C07C405/00 , C07C69/738 , C07C69/712 , A61K31/557
CPC分类号： C07C69/738 , C07C59/46 , C07C59/62 , C07C69/712 , C07C69/732 , C07C405/0083 , Y02P20/55
摘要： A cis-bicyclo[4.3.0]non-2-ene derivative of the formula:

wherein R is a hydrogen atom, or a protecting group for a hydroxyl group, R¹ is a hydrogen atom, a
C₁-C₁₂
straight or branched chain alkyl group, a substituted or unsubstituted phenyl group, a
C₆-C₁₂
aralkyl group containing a condensed aromatic ring or an aromatic hetero ring, or 1 equivalent of a cation, A is
-CH=CH-
CH₂-,
or
-CH₂-CH₂-O- ,
R² is a
C₃-C₁₀
straight or branched chain alkyl group, a
C₁-C₃
alkyl group substituted by an aryloxy group which may be substituted, a
C₃-C₁₂
straight or branched chain alkenyl group, a
C₃-C₈
straight or branched chain alkynyl group, or a
C₁-C₃
alkyl group substituted by a phenyl or phenoxy group which may be substituted, by a
C₁-C₆
alkoxy group or by a
C₅-C₈
cycloalkyl group, R³ is a hydrogen atom, a methyl group, or a vinyl group, and X is a halogen atom.
摘要翻译：下式的顺式 - 二环[4.3.0]壬-2-烯衍生物：其中R是氢原子或羟基保护基，R 1是氢原子，C 1 -C 12直链或支链烷基取代或未取代的苯基，含有稠合芳环或芳香杂环的C 6 -C 12芳烷基，或1当量的阳离子，A是-CH = CH-CH 2 - 或-CH 2 -CH 2 -O - ，R 2为C 3 -C 10直链或支链烷基，被可被取代的芳氧基取代的C 1 -C 3烷基，C 3 -C 12直链或支链链烯基，C 3 -C 8直链或支链炔基或被苯基或苯氧基取代的C 1 -C 3烷基，它们可以是取代的通过C 1 -C 6烷氧基或C 5 -C 8环烷基取代，R 3是氢原子，甲基或乙烯基，X是卤素原子。

2. 发明公开

EP0431571A2 Cis-Bicyclo[4.3.0]non-2-ene derivatives 失效
标题翻译： Cis-Bicyclo¬4.3.O非2-en-Derivate
公开(公告)号：EP0431571A2
公开(公告)日：1991-06-12
申请号：EP90123253.8
申请日：1990-12-04
申请人： SAGAMI CHEMICAL RESEARCH CENTER , TOA EIYO LTD.
发明人： Shibasaki, Masakatsu , Takahasi, Atsuo , Aoki, Tuyosi , Sato, Hiroyasu , Yamada, Shin-ichi , Kudo, Michiko , Yamaguchi, Takaji , Kogi, Kentaro , Narita, Sen-ichi
IPC分类号： C07C405/00 , C07C69/738 , C07C69/712 , A61K31/557
CPC分类号： C07C69/738 , C07C59/46 , C07C59/62 , C07C69/712 , C07C69/732 , C07C405/0083 , Y02P20/55
摘要： A cis-bicyclo[4.3.0]non-2-ene derivative of the formula:

wherein R is a hydrogen atom, or a protecting group for a hydroxyl group, R¹ is a hydrogen atom, a

C₁-C₁₂

straight or branched chain alkyl group, a substituted or unsubstituted phenyl group, a

C₆-C₁₂

aralkyl group containing a condensed aromatic ring or an aromatic hetero ring, or 1 equivalent of a cation, A is

-CH=CH-

CH₂-,

or

-CH₂-CH₂-O- ,

R² is a

C₃-C₁₀

straight or branched chain alkyl group, a

C₁-C₃

alkyl group substituted by an aryloxy group which may be substituted, a

C₃-C₁₂

straight or branched chain alkenyl group, a

C₃-C₈

straight or branched chain alkynyl group, or a

C₁-C₃

alkyl group substituted by a phenyl or phenoxy group which may be substituted, by a

C₁-C₆

alkoxy group or by a

C₅-C₈

cycloalkyl group, R³ is a hydrogen atom, a methyl group, or a vinyl group, and X is a halogen atom.
摘要翻译：下式的顺式 - 双环[4.3.0]壬-2-烯衍生物：其中R是氢原子或羟基保护基，其中R 1是氢原子，C1- C12直链或支链烷基，取代或未取代的苯基，含有稠合芳环或芳族杂环的C 6 -C 12芳烷基或1当量阳离子，A为-CH = CH-CH 2 - 或 -CH 2 -CH 2 -O - ，R 2是C 3 -C 10直链或支链烷基，被可被取代的芳氧基取代的C1-C3烷基，C3-C12直链或支链烯基 C 3 -C 8直链或支链炔基或被可被取代的苯基或苯氧基取代的C 1 -C 3烷基，被C 1 -C 6烷氧基或C 5 -C 8环烷基取代，R 3 >是氢原子，甲基或乙烯基，X是卤素原子。

3. 发明公开

EP0661266A1 Substituted cyclic amine compounds as 5HT2 antagonists 失效
标题翻译：取代基旋转Aminverbindungen als 5HT2拮抗剂。
公开(公告)号：EP0661266A1
公开(公告)日：1995-07-05
申请号：EP94120698.9
申请日：1994-12-27
申请人： TOA EIYO LTD.
发明人： Aoki, Tsuyoshi , Takahashi, Atsuo , Sato, Hiroyasu , Shimanuki, Eiji , Gengyou, Kaoru , Nishimata, Toyoki , Ishigami, Sachiko , Yamada, Shin-ichi , Yamaguchi, Takahiro , Manome, Yoichi , Sato, Isamu , Kogi, Kentaro , Narita, Sen-ichi
IPC分类号： C07D211/32 , A61K31/395 , C07D401/06 , C07D405/12 , C07D417/06 , C07D401/12 , C07D295/14 , C07D295/12 , C07D417/12
CPC分类号： C07D295/13 , C07C43/215 , C07C43/23 , C07C45/44 , C07C47/277 , C07C69/734 , C07C235/56 , C07C255/37 , C07C255/40 , C07C311/21 , C07C311/29 , C07D211/32 , C07D295/145 , C07D295/15 , C07D401/06 , C07D401/12 , C07D405/12 , C07D417/06 , C07D417/12
摘要： A substituted cyclic amine compound represented by the following general formula (1)

wherein each of R¹ to R⁵ represents a hydrogen atom, a hydroxyl group, an alkyl group or the like, D represents a methine moiety, a nitrogen atom or the like, P represents -CR⁶(R⁷)- or -NR⁸-, Q represents a methine moiety or a nitrogen atom, each of T and B is a single bond or represents a methylene moiety, a carbonyl group or the like, n is an integer of 1 to 6 and each of R⁶, R⁷ and R⁸ represents a hydrogen atom, an alkyl group or the like; and synthetic intermediates thereof.
The inventive compound is useful in preventing and treating circulatory organ-related diseases such as hypertension, ischemic heart disease, cerebrovascular disease, peripherol circulatory disease and the like.
摘要翻译：由以下通式（1）表示的取代环胺化合物其中R 1至R 5各自表示氢原子，羟基，烷基等，D表示次甲基部分，氮原子等，P表示-CR 6（R 7） - 或-NR 8 - ，Q表示次甲基部分或氮原子，T和B各自为单键或表示亚甲基部分，羰基等，n为1〜6的整数，R 6，R 7和R 8各自表示氢原子，烷基等; 及其合成中间体。本发明化合物可用于预防和治疗诸如高血压，缺血性心脏病，脑血管病，周围血管循环系统疾病等循环器官相关疾病。

4. 发明公开

EP0434999A1 Cycloheptenopyridine derivatives, process for preparation thereof and antiulcer agents containing the same 失效
标题翻译： Cycloheptenopyridinderivate，Verfahren zu ihrer Herstellung und diese enthaltende Antiulkusmitteln。
公开(公告)号：EP0434999A1
公开(公告)日：1991-07-03
申请号：EP90122644.9
申请日：1990-11-27
申请人： TOA EIYO LTD.
发明人： Yamada, Shin-ichi , Goto, Takao , Yorita, Rie , Shimanuki, Eizi , Yamaguchi, Takaji , Kogi, Kentaro , Narita, Senichi
IPC分类号： C07D401/12 , A61K31/415 , C07D471/04 , A61K31/435 , A61K31/44
CPC分类号： C07D401/12 , C07D471/04 , Y02P20/55 , Y10S514/926 , Y10S514/927
摘要： Provided are cycloheptenopyridine derivatives represented by the general formula
[wherin R represents a hydrogen atom or lower alkyl group; R 1 represents a hydrogen atom, hologen atom, lower alkoxy group, lower cycloalkoxy group, amido group, substituted phenoxy group, substituted benzyloxy group, lower alkoxy group optionally containing halogen atom(s), nitro group, hydroxyl group, lower alkenyloxy group, lower alkylthio group, or group-NR4Rs (wherein R 4 and R 5 may be the same or different and each represent a hydrogen atom or lower alkyl group, or R 4 and R 5 mutually combine together with the nitrogen atom adjacent thereto to form a 5- or 6- membered cycle); R 2 represents a hydrogen atom, halogen atom, lower alkyl group optionally containing a halogen atom, lower alkoxy group optionally containing a halogen atom, hydroxyl group, acyl group, lower alkoxycarbonyl group, nitro group or amino group; R 3 represents a lower alkyl group, lower alkoxymethyl group, lower alkylcarbonyl group, lower alkoxycarbonyl group, carbamoyl group, lower alkylcarbamoyl group, lower alkylcarbonylmethyl group, lower alkoxycarbonylmethyl group, lower acyloxymethyl group, lower alkylsulfonyl group, or physiologically acceptable protective group eliminable in an acid medium or under a physiological condition; n represents 0 or 1; and A represents a methine carbon or nitrogen atom] or their salts. These derivatives and their salts are useful as untiulcer agents.
摘要翻译：提供由通式表示的环庚烯并吡啶衍生物[R表示氢原子或低级烷基; R 1表示氢原子，氢原子，低级烷氧基，低级环烷氧基，酰胺基，取代苯氧基，取代苄氧基，任选含有卤素原子的低级烷氧基，硝基，羟基，低级烯氧基基团，低级烷硫基或基团-NR 4 R 5（其中R 4和R 5可以相同或不同，各自表示氢原子或低级烷基，或R 4表示氢原子或低级烷基，和R 5与其相邻的氮原子相互结合形成5-或6-元环）; R 2表示氢原子，卤素原子，任选含有卤素原子的低级烷基，任选含有卤素原子的低级烷氧基，羟基，酰基，低级烷氧基羰基，硝基或氨基; R 3表示低级烷基，低级烷氧基甲基，低级烷基羰基，低级烷氧基羰基，氨基甲酰基，低级烷基氨基甲酰基，低级烷基羰基甲基，低级烷氧基羰基甲基，低级酰氧基甲基，低级烷基磺酰基或生理上可接受的保护基在酸性介质中或在生理条件下可消除; n表示0或1; A表示次甲基碳或氮原子]或其盐。这些衍生物及其盐可用作脱水剂。

5. 发明授权

EP0434999B1 Cycloheptenopyridine derivatives, process for preparation thereof and antiulcer agents containing the same 失效
标题翻译： Cycloheptenopyridinderivate，涉及它们的制备方法和含有抗溃疡剂的方法。
公开(公告)号：EP0434999B1
公开(公告)日：1994-08-17
申请号：EP90122644.9
申请日：1990-11-27
申请人： TOA EIYO LTD.
发明人： Yamada, Shin-ichi , Goto, Takao , Yorita, Rie , Shimanuki, Eizi , Yamaguchi, Takaji , Kogi, Kentaro , Narita, Senichi
IPC分类号： C07D401/12 , A61K31/415 , C07D471/04 , A61K31/435 , A61K31/44
CPC分类号： C07D401/12 , C07D471/04 , Y02P20/55 , Y10S514/926 , Y10S514/927

6. 发明公开

EP0277701A1 Thiazolopyridine derivative, their production and cardiovascular treating agents containing them 失效
标题翻译：噻唑并吡啶衍生物，它们的生产和含有它们的心血管治疗剂
公开(公告)号：EP0277701A1
公开(公告)日：1988-08-10
申请号：EP88300109.1
申请日：1988-01-07
申请人： TOA EIYO LTD.
发明人： Yamada, Shin-ichi , Goto, Takao , Mashiko, Toshihisa , Kogi, Kentaro , Oguchi, Yukiko , Narita, Senichi
IPC分类号： C07D513/04 , A61K31/435
CPC分类号： C07D513/04
摘要： A 4,7-dihydroisothiazolo[5,4-b]pyridine derivative represented by the general formula
wherein

R 1 represents an alkyl group which may be substituted,
R 2 represents a hydrogen atom, a hydroxyl group, a benzyloxy group, a lower alkoxy group, a group of the formula
in which R 3 and R 4 are identical or different and each represents a hydrogen atom, a lower alkyl group, an aralkyl group, an aralkynyl group, an aryloxyalkyl group, an arylaminoalkyl group, a pyridylalkyl group or a benzazolylalkyl group, or R 3 and R 4 form a ring and represent a group of the formula
where X represents a methine group, a nitrogen atom or an oxygen atom, n is an integer of 1 or 2, and when X is a methine group or a nitrogen atom, R 5 represents a hydrogen atom, a lower alkyl group, a lower hydroxyalkyl group, an aryl group, an aryloxy group, an aralkyl group, a furoyl group, a pyridyl group or a diphenylmethane group each of which group may be substituted, and

m is an integer of 1 to 3, or an acid addition salt thereof. Processes for producing said derivative and a cardiovascular treating agent comprising said derivative as an active ingredient are also provided.
摘要翻译：由下列通式表示的4,7-二氢异噻唑并[5,4-b]吡啶衍生物其中R1代表可被取代的烷基，R2代表氢原子，羟基，苄氧基，低级烷氧基，其中R 3和R 4相同或不同并且各自表示氢原子，低级烷基，芳烷基，芳炔基，芳氧基烷基，芳基氨基烷基，吡啶基烷基或苯并唑基烷基的式的基团，或者R3和R4形成环，并且代表下式的基团，其中X代表次甲基，氮原子或氧原子，n是1或2的整数，并且当X是次甲基或氮原子时， R5表示各自可被取代的氢原子，低级烷基，低级羟烷基，芳基，芳氧基，芳烷基，糠酰基，吡啶基或二苯基甲烷基，m为 1至3的整数，或酸加成盐复查。还提供了产生所述衍生物的方法和包含所述衍生物作为活性成分的心血管治疗剂。

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