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1. 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。

2. 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。

3. 发明公开

EP0273216A2 Prostacyclin analogue and anti-ulcer composition containing it as active ingredient 失效
标题翻译： Prostacyclinanalog und dieses als aktiven Bestandteil enthaltendes，gegenMagengeschwürewirkendes Mittel。
公开(公告)号：EP0273216A2
公开(公告)日：1988-07-06
申请号：EP87117704.4
申请日：1987-11-30
申请人： SAGAMI CHEMICAL RESEARCH CENTER , TOA EIYO LTD.
发明人： Shibasaki, Masakatsu , Takahashi, Atsuo , Aoki, Tuyoshi , Mashiko, Toshihisa , Kogi, Kentaro , Yamaguchi, Takashi TOA EIYO LTD. , Nara, Takeshi TOA EIYO LTD. , Narita, Senichi TOA EIYO LTD.
IPC分类号： C07C177/00 , A61K31/557
CPC分类号： C07C405/0083 , Y02P20/55
摘要： A prostacyclin analogue having the formula:
wherein R¹ is a hydrogen atom or a lower alkyl group; R² and R³ each is a hydrogen atom or a lower alkyl group; R⁴ is a hydrogen atom, a halogen atom or a lower alkoxy group.
摘要翻译：具有下式的前列环素类似物：其中R 1是氢原子或低级烷基; R 2和R 3各自为氢原子或低级烷基; R 4是氢原子，卤素原子或低级烷氧基。

4. 发明公开

EP0273216A3 Prostacyclin analogue and anti-ulcer composition containing it as active ingredient 失效
标题翻译：前体化合物模拟物和含有作为活性成分的抗坏血酸组合物
公开(公告)号：EP0273216A3
公开(公告)日：1988-07-20
申请号：EP87117704
申请日：1987-11-30
申请人： SAGAMI CHEMICAL RESEARCH CENTER , TOA EIYO LTD.
发明人： Shibasaki, Masakatsu , Takahashi, Atsuo , Aoki, Tuyoshi , Mashiko, Toshihisa , Kogi, Kentaro , Yamaguchi, Takashi TOA EIYO LTD. , Nara, Takeshi TOA EIYO LTD. , Narita, Senichi TOA EIYO LTD.
IPC分类号： C07C177/00 , A61K31/557
CPC分类号： C07C405/0083 , Y02P20/55
摘要： A prostacyclin analogue having the formula:
wherein R¹ is a hydrogen atom or a lower alkyl group; R² and R³ each is a hydrogen atom or a lower alkyl group; R⁴ is a hydrogen atom, a halogen atom or a lower alkoxy group.

5. 发明授权

EP0234576B1 Prostacyclin analogue, and blood circulation improving agent and anti-ulcer composition containing it as active ingredient 失效转让
标题翻译： PROSTACYCLIN模拟和血液循环改善剂和防腐剂组合物作为活性成分
公开(公告)号：EP0234576B1
公开(公告)日：1991-01-30
申请号：EP87102721.5
申请日：1987-02-26
申请人： SAGAMI CHEMICAL RESEARCH CENTER , TOA EIYO LTD.
发明人： Shibasaki, Masakatsu , Takahashi, Atsuo , Aoki, Tuyoshi , Kogi, Kentaro TOA EIYO LTD. Fukushima Kenkyusho , Nishimiya, Yozo TOA EIYO LTD. Fukushima Kenkyusho , Nara, Takeshi TOA EIYO LTD. Fukushima Kenkyusho , Yamaguchi,Takashi TOA EIYO LTD.Fukushima Kenkyusho
IPC分类号： C07C405/00 , A61K31/557
CPC分类号： C07C405/0083

6. 发明公开

EP0234576A1 Prostacyclin analogue, and blood circulation improving agent and anti-ulcer composition containing it as active ingredient 失效转让
标题翻译： Prostacyclinanalog，含有该作为活性成分，循环改善剂以及作用抗溃疡剂。
公开(公告)号：EP0234576A1
公开(公告)日：1987-09-02
申请号：EP87102721.5
申请日：1987-02-26
申请人： SAGAMI CHEMICAL RESEARCH CENTER , TOA EIYO LTD.
发明人： Shibasaki, Masakatsu , Takahashi, Atsuo , Aoki, Tuyoshi , Kogi, Kentaro TOA EIYO LTD. Fukushima Kenkyusho , Nishimiya, Yozo TOA EIYO LTD. Fukushima Kenkyusho , Nara, Takeshi TOA EIYO LTD. Fukushima Kenkyusho , Yamaguchi,Takashi TOA EIYO LTD.Fukushima Kenkyusho
IPC分类号： C07C405/00 , A61K31/557
CPC分类号： C07C405/0083
摘要： A prostacyclin analogue having the formula:
wherein R 1 is -CO 2 R 5 (wherein R 5 is a hydrogen atom, a straight chain or branched alkyl group having from 1 to 12 carbon atoms, an aralkyl group having from 7 to 12 carbon atoms, a cycloalkyl group having from 4 to 7 carbon atoms and unsubstituted or substituted by at least one alkyl group having form 1 to 4 carbon atoms, a substituted or unsubstituted phenyl group, or one equivalent of a cation), or -CONR 6 R 7 (wherein each of R 6 and R 7 is a hydrogen atom or an alkyl group having from 1 to 10 carbon atoms, or R 6 and R 7 together with the adjacent nitrogen atom, form a 5- or 6- membered substituted or unsubstituted hetero ring which may contain a hetero atom other than said nitrogen atom); A is - C H 2 CH 2 CH 2 -, CH 2 -O-CH 2 CH 2 -, -CH 2 CH 2 CH 2 CH 2 -, -CH 2 CH 2 -O-CH 2 - or -CH=CHCH 2 CH 2 -; B is trans -CH=CH-or-C=C-; R 2 is a straight chain or branched alkyl group having from 3 to 10 carbon atoms, a cycloalkyl group having from 4 to 7 carbon atoms and unsubstituted or substituted by at least one alkyl group having from 1 to 4 carbon atoms, a straight chain or branched alkenyl group having form 3 to 12 carbon atoms, a straight chain or branched alkynyl group having from 3 to 8 carbon atoms, or an alkyl group having from 1 to 3 carbon atoms substituted by a substituted or unsubstituted phenyl or phenyoxy group, by an alkoxy group having from 1 to 6 carbon atoms or by a cycloalkyl group having from 5 to 8 carbon atoms; R 3 is a hydrogen atom, a methyl group or a vinyl group; and R 4 is a hydrogen atom, an acyl group having from 1 to 7 carbon atoms, a tri-C 1 -C 7 hydrocarbon-silyl group or a group capable of forming an acetal bond together with the oxygen atom of a hydroxyl group; provided that the double bond in a substituent for A is E or Z, or a mixture thereof; the asymmetric center in a substituent for R 2 assumes a R-conformation or a S-conformation, or a mixture thereof; and the bonds shown by dotted lines at the 2-3 and 3-4 positions mean that either one of them is a double bond.

7. 发明公开

EP0171992A2 Pharmaceuticals containing prostaglandin I2 有权转让
标题翻译： Arzneimittel死亡前列腺素I2窒息。
公开(公告)号：EP0171992A2
公开(公告)日：1986-02-19
申请号：EP85305611.7
申请日：1985-08-07
申请人： MITSUBISHI KASEI CORPORATION , SAGAMI CHEMICAL RESEARCH CENTER
发明人： Ishibashi, Akira , Horii, Daijiro , Kanayama, Toshiji , Iseki, Katsuhiko , Shinoda, Masaki , Ishiyama, Chiyoko , Hayashi, Yosio , Shibasaki, Masakatsu , Sodeoka, Mikiko , Ogawa, Yuji , Mase, Toshiaki
IPC分类号： A61K31/557
CPC分类号： C07C405/0083 , A61K31/557
摘要： Disclosed is a pharmaceutical having circulation ameliorating effect and antiulcer effect containing a prostaglandin I 2 analogue represented by the formula shown below or a non-toxic salt of its salt or a cyclodextrin inclusion compound thereof as the effective ingredient:
wherein R' represents a hydrogen atom, an alkyl group having 1 to 12 carbon atoms, a cycloalkyl group having 4 to 7 carbon atoms or a phenyl group,
A represents a pentyl group, a cyclopentyl group, a cyclohexyl group, a 1-methyl-3-hexynyl group, a 2-methyl-3-hexynyl group, a 1-methythexyl group, a 2-phenethyl group, a 1,1-dimethylpentyl group, a 2-methylpentyl group, a 1-cyclohexylethyl group, a 2-methylhexyl group, a 1-methyl-3-pentynyl group or a 2,6-dimethyl-5-heptenyl group, the double bond between the carbon atoms at 4- and 5-positions is E or Z or a mixture thereof, the asymmetric center in the substituent represented by A is R-configuration or S-configuration or a mixture thereof.
The pharmaceuticals containing, as an active ingredient, prostaglandin 1 2 analogues of the present invention have potent platelet aggregation inhibiting effect, blood pressure depressing effect, vasodilative effect and antiulcer effect, and are also low in toxicity.
摘要翻译：本发明公开了含有前列腺素I2，由下述通式表示的类似物或其盐的无毒性盐或其环糊精包合物作为有效成分的循环改善效果和抗溃疡作用的药物：其中R 1 >表示氢原子，碳原子数1〜12的烷基，碳原子数4〜7的环烷基或苯基，A表示戊基，环戊基，环己基，1-甲基-3 己炔基，2-甲基-3-己炔基，1-甲基己基，2-苯乙基，1,1-二甲基戊基，2-甲基戊基，1-环己基乙基，2-甲基己基基团，2,6-二甲基-5-庚烯基上的1-甲基-3-戊炔基，4-和5-位的碳原子之间的双键是E或Z或其混合物，不对称中心在由A表示的取代基中是R构型或S-构型或其混合物。含有本发明的前列腺素I2类似物作为活性成分的药物具有有效的血小板聚集抑制作用，降血压作用，血管扩张作用和抗溃疡作用，毒性也低。

8. 发明公开

EP0134153A3 Bicyclo[3.3.0]octane derivative and preparation thereof 有权
标题翻译： BICYCLOÛ3.3.0 - 甲烷衍生物及其制备方法
公开(公告)号：EP0134153A3
公开(公告)日：1985-04-10
申请号：EP84305636
申请日：1984-08-17
申请人： SAGAMI CHEMICAL RESEARCH CENTER
发明人： Shibasaki, Masakatsu , Mase, Toshiaki , Sodeoka, Mikiko , Ogawa, Yuji
IPC分类号： C07C177/00 , A61K31/557 , C07F07/18 , C07D309/12
CPC分类号： C07F7/1856 , C07C405/0016 , C07C405/0025 , C07C405/0083 , Y02P20/55
摘要： There are disclosed a bicyclo[3.3.0]octane derivative represented by the formula:
wherein
R l : a hvdrooen atom or a protective group of a hydroxy group;
where
R 5 : a hydrogen atom or a protective group of a hydroxy group, R 6 : a straight, branched or cyclic alkyl group, alkenyl group or alkynyl group each having 5 to 10 carbon atoms, and X: a vinylene group or an acetylene group; R 3 : a formyl group, -Y-(CH 2 ) 2 -COOR 7 or -CH 2 R 8 ; where R 7 : a hydrogen atom or an alkyl group, R 8 : a hydroxy group, an acetyloxy group or a butenyl group, and Y: an ethylene group, a vinylene group or an alkylene group; R 4 : a hydroxy group when the compound being an octane derivative, or a hydrogen atom when the compound being an octene derivative; and dotted line: optional presence of a double bond; provided that when R 1 is -X-CH-R 6 , R 3 being -(CH 2 )4-COOR 7 is excluded, I O R5 and a process for producing the same. The compound of this invention and the process for producing the same are available for producing a 9(0)-methano--Δ 6(9.α) -PGI 1 -

9. 发明授权

EP0181581B1 beta-Aminothiol ester and process for preparing thereof 有权
标题翻译： BETA-AMINOTHIOL ESTER及其制备方法
公开(公告)号：EP0181581B1
公开(公告)日：1988-07-13
申请号：EP85113926.1
申请日：1985-11-01
申请人： SAGAMI CHEMICAL RESEARCH CENTER
发明人： Shibasaki, Masakatsu , Iimori, Takamasa
IPC分类号： C07C153/09
CPC分类号： C07D205/08 , C07C327/00 , Y02P20/55

10. 发明公开

EP0209886A3 beta-N-substituted aminothiol ester and process for preparing the same 失效
标题翻译： BETA-N-取代的氨基酸酯及其制备方法
公开(公告)号：EP0209886A3
公开(公告)日：1987-05-13
申请号：EP86110029
申请日：1986-07-22
申请人： SAGAMI CHEMICAL RESEARCH CENTER
发明人： Shibasaki, Masakatsu , Iimori, Takamasa
IPC分类号： C07F07/08 , C07D205/08
CPC分类号： C07F7/0818 , C07D205/08
摘要： β-N-Substituted aminothiol ester represented by the general formula (I) :
wherein R' is an alkyl group or an aryl group and R 2 is an aralkyl group, a process for preparing the same, and an azetidinone derivative represented by the general formula (VI) :
wherein R 2 is as above. The β-N-subsituted aminothiol ester (I) of the present invention can be an excellent intermediate for preparing the β-lactam (II).

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