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1. 发明专利

JP2010248137A Method for producing gamma-thujaplicin 有权
标题翻译：用于生产GAMMA-THUJAPLICIN的方法
公开(公告)号：JP2010248137A
公开(公告)日：2010-11-04
申请号：JP2009100155
申请日：2009-04-16
申请人： Kotobuki Seiyaku Kk , 壽製薬株式会社
发明人： TOMIYAMA TAKESHI , TOMIYAMA YASUSHI , YOKOTA MASAYUKI
IPC分类号： C07C45/64 , C07C45/81 , C07C49/717
摘要： PROBLEM TO BE SOLVED: To provide a method for readily obtaining γ-thujaplicin useful as a pharmaceutical drug intermediate at a low cost in a high yield.
SOLUTION: The method for producing γ-thujaplicin comprises: (1) a first step of reacting cyclopentadiene with sodium amide in an N, N-dimethylformamide solvent so as to prepare sodium cyclopentadienylide and reacting the same with an isopropylating agent so as to obtain an isopropyl cyclopentadiene mixture; (2) a second step of reacting the isopropyl cyclopentadiene mixture with dichloroketene so as to obtain a 7,7-dichlorobicyclo[3.2.0]-hepto-2-en-6-one derivative mixture; and (3) a third step of subjecting the 7,7-dichlorobicyclo[3.2.0]-hepto-2-en-6-one derivative mixture to solvolysis under a basic condition so as to obtain a crude product and isolating γ-thujaplicin from the same by crystallization.
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供一种容易地以高产率低成本获得用作药物中间体的γ-苏吡布毒素的方法。解决方案：γ-胡椒碱的制造方法包括：（1）在N，N-二甲基甲酰胺溶剂中使环戊二烯与氨基钠反应的第一工序，制备环戊二烯基钠，并与异丙基化试剂反应，得到异丙基环戊二烯混合物; （2）使异丙基环戊二烯混合物与二氯代烯酮反应以获得7,7-二氯双环[3.2.0] - 庚-2-烯-6-酮衍生物混合物的第二步; 和（3）在碱性条件下使7,7-二氯双环[3.2.0] - 庚-2-烯-6-酮衍生物混合物进行溶剂分解的第三步，得到粗产物，并分离γ-硫代吡啶从同样的结晶。版权所有（C）2011，JPO＆INPIT

2. 发明专利

JP2010001291A Method for producing glycolipid derivative 有权
标题翻译：生产甘油衍生物的方法
公开(公告)号：JP2010001291A
公开(公告)日：2010-01-07
申请号：JP2009159985
申请日：2009-07-06
申请人： Kotobuki Seiyaku Kk , 壽製薬株式会社
发明人： TOMIYAMA YASUSHI , YANAGISAWA TAKASHI , FUTAMURA MASAYUKI , NODA ATSUSHI , TOMIYAMA TAKESHI
IPC分类号： C07D309/10 , A61K31/351 , A61P35/00 , A61P37/04 , C07B61/00
摘要： PROBLEM TO BE SOLVED: To provide a method for producing a glycolipid derivative of formula (e), having antitumor activity and immunoactivating effect, stable to glucosidase metabolism, acids and bases, and storable for a long period at room temperature.
SOLUTION: The method for producing the glycolipid derivative of formula (e) includes conducting a catalytic reduction of a compound of formula (d). In the formulas (d) and (e), R
0 is -OH, -NH
2 or -NHAc group; W is a 9-17C saturated or unsaturated hydrocarbon chain; X is a 11-25C saturated or unsaturated hydrocarbon chain; Z is -CO- or -SO
2 -; and b is an integer of 1-5.
COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供一种具有抗肿瘤活性和免疫活化作用的式（e）的糖脂衍生物的制备方法，其对葡糖苷酶代谢，酸和碱稳定，并可在室温下长时间储存。解决方案：制备式（e）的糖脂衍生物的方法包括进行式（d）化合物的催化还原。在式（d）和（e）中，R 0是-SH，-NHC 2或-NHAc基团; W是9-17C饱和或不饱和烃链; X是11-25℃饱和或不饱和烃链; Z是-CO-或-SO- SB 2。 b为1-5的整数。版权所有（C）2010，JPO＆INPIT

3. 发明专利

JP2009263391A New glycolipid derivative and pharmaceutical preparation comprising the same as active component 有权
标题翻译：新型GLYCOLIPID衍生物和药物制剂，将其作为活性成分
公开(公告)号：JP2009263391A
公开(公告)日：2009-11-12
申请号：JP2009159984
申请日：2009-07-06
申请人： Kotobuki Seiyaku Kk , 壽製薬株式会社
发明人： TOMIYAMA YASUSHI , YANAGISAWA TAKASHI , FUTAMURA MASAYUKI , NODA ATSUSHI , TOMIYAMA TAKESHI
IPC分类号： C07D309/10 , A61K31/351 , A61K31/70 , A61P35/00 , A61P37/04 , C07H15/14
摘要： PROBLEM TO BE SOLVED: To provide a glycolipid derivative with an α-C-glycoside bond, having a powerful antitumor activity and immunostimulation action, stable to glucosidase metabolism, acids and bases, and stored for a long time at room temperature.
SOLUTION: There is provided the compound represented by general formula (I) or its pharmaceutically permissible salts, [wherein W is a 9-17C saturated or unsaturated hydrocarbon chain and further contains a hydroxy group in some cases, X is an 11-25C saturated or unsaturated hydrocarbon chain and further contains a hydroxy group in some cases. Y represents -(CH
2 )
a -CH=CH-(CH
2 )
a - or -(CH
2 )
a - (in the proviso that a, a' are each an integer of 0-5, and a+a'≤5), Z represents -CO- or -SO
2 -, R represents a -CH
2 OH, -CO
2 H, -CH
2 OCH
2 CO
2 H, or -CH
2 OSO
3 H group, and R
0 represents a -OH, -NH
2 , or -NHAc group].
COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供具有强大的抗肿瘤活性和免疫刺激作用的具有α-C-糖苷键的糖脂衍生物，对葡糖苷酶代谢，酸和碱稳定，并在室温下长时间储存。提供由通式（I）表示的化合物或其药学上可允许的盐[其中W是9-17C饱和或不饱和烃链，并且在某些情况下还含有羟基，X是11 -25℃饱和或不饱和烃链，在某些情况下还含有羟基。 Y表示 - （CH 2 ） -CH = CH-（CH 2 （条件是a，a'分别为0-5的整数，a + a'≤5），Z表示-CO - 或 - -SO 2 - ， - R表示-CH 2 S 2，-CO 2 SBH 2， CH 2，OCH 2，SO 2，SO 2，CH 3，SO 2，CH 2，表示-OH，-NH SB 2或-NHAc基团]。版权所有（C）2010，JPO＆INPIT

4. 发明专利

JP2009062381A Glucolipid derivative, its manufacturing method and medicine containing it as effective component 有权
标题翻译：葡萄糖衍生物及其制造方法和药物作为有效成分
公开(公告)号：JP2009062381A
公开(公告)日：2009-03-26
申请号：JP2008263962
申请日：2008-10-10
申请人： Kotobuki Seiyaku Kk , 壽製薬株式会社
发明人： TOMIYAMA YASUSHI , YANAGISAWA TAKASHI , FUTAMURA MASAYUKI , NODA ATSUSHI , TOMIYAMA TAKESHI
IPC分类号： C07D309/10 , A61K31/351 , A61P35/00 , A61P35/04 , A61P37/04
摘要： PROBLEM TO BE SOLVED: To provide a glucolipid derivative having an α-S-glucosidic linkage which is useful as an antitumor medicine and an immunopotentiator, and its manufacturing method, and medicines containing it as an effective component. SOLUTION: This glucolipid derivative is a compound represented by general formula (I) (wherein W is a 9-17C saturated or unsaturated carbon chain and further in some case contains a hydroxy group, X is an 11-25C saturated or unsaturated carbon chain and further in some case contains a hydroxy group, Y represents -S(O) 0-2 CH 2 -, Z represents -CO- or -SO 2 -, R represents -CH 2 OH, -CO 2 H, -CO 2 OCH 2 CO 2 H, or -CH 2 OSO 3 H group, and R 0 represents -OH, -NH 2 , or -NHAc group), or its pharmaceutically permissible salts. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：提供可用作抗肿瘤药和免疫增强剂的具有α-S-糖苷键的糖脂衍生物及其制备方法以及含有它作为有效成分的药物。解决方案：该糖脂衍生物为通式（I）表示的化合物（其中W为9-17C饱和或不饱和碳链，并且在某些情况下还含有羟基，X为11-25℃饱和或不饱和的碳链，并且在某些情况下还含有羟基，Y表示-S（O），S表示-CO-或-SO 2 - ，R表示-CH 2 OH，-CO 2 H，-CO 2 / SB> CO 2 H或-CH 2 OSO 3 H基，R SB 0表示-OH ，-NH 2 SBA或-NHAc基团）或其药学上允许的盐。版权所有（C）2009，JPO＆INPIT

5. 发明专利

JP2013010712A Tricyclic compound and pharmaceutical composition containing the same 有权
标题翻译：三元复合物和含有它们的药物组合物
公开(公告)号：JP2013010712A
公开(公告)日：2013-01-17
申请号：JP2011144216
申请日：2011-06-29
申请人： Kotobuki Seiyaku Kk , 壽製薬株式会社
发明人： TOMIYAMA TAKESHI , TOMIYAMA YASUSHI , YOKOTA MASAYUKI , MUROGA SHOTA
IPC分类号： C07D409/12 , A61K31/403 , A61K31/407 , A61K31/422 , A61K31/433 , A61K45/00 , A61P7/02 , A61P9/10 , A61P29/00 , A61P43/00 , C07D209/80 , C07D209/88 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/052 , C07D491/113 , C07D495/04
摘要： PROBLEM TO BE SOLVED: To provide a compound which provides EP3 receptor antagonism, and a pharmaceutical composition which contains the compound and is for prevention against and treatment of prostaglandin mediated disorders.SOLUTION: There is disclosed the compound represented by general formula (I), where Rand Rare a hydrogen atom, a lower alkyl group, a lower haloalkyl group, a lower alkoxy group, or a halogen atom, Ris a monocyclic or bicyclic aromatic ring or heterocyclic ring, or a cyclo ring, Ris a monocyclic or bicyclic aromatic ring or heterocyclic ring, X is -CH- or a carbon atom having a lower alkyl group, Y is -CHCH-(CH)m- or -CR=CR-(CH)m- (Rand Rmay be identical or different and a hydrogen atom or a halogen atom), -O-CH-(CH)m-, (cyclo ring (1-5 carbons))-(CH)m-, or (monocyclic or bicyclic aromatic ring)-(CH)m-, where m is 0-5, Z is a bond or -SO-, and n is 0-5.
摘要翻译：待解决的问题：提供提供EP3受体拮抗作用的化合物和含有该化合物并用于预防和治疗前列腺素介导的病症的药物组合物。解决方案：公开了由通式（I）表示的化合物，其中R 1 和R 2 是氢原子，低级烷基，低级卤代烷基，低级烷氧基或卤素原子，单环或双环芳环或杂环，或环，R 4是单环或双环芳环或杂环，X是-CH 2，或碳原子具有低级烷基，Y是-CH 2 - （CH 2 < / SB>）m-或-CR 5 = CR 6 - （CH 2 < / SB>）m-（R 5 和R 6 可以相同或不同，氢原子或卤素原子），-O-CH 2 - （CH 2 ）m-，（环环（1-5个碳）） - （ m - 或（单环或双环芳环） - （CH 2 ）m-，其中m为0 -5，Z是一个债券o r -SO 2 - ，n为0-5。版权所有（C）2013，JPO＆INPIT

6. 发明专利

JPS6133172A 1,3-substituted-2-imidazolidinone derivative, agent for promoting gastroenteric movement, and its preparation 失效
标题翻译： 1,3-取代的2-咪唑啉酮衍生物，用于促进胃肠运动的药剂及其制备
公开(公告)号：JPS6133172A
公开(公告)日：1986-02-17
申请号：JP15384484
申请日：1984-07-24
申请人： Kotobuki Seiyaku Kk
发明人： TOMIYAMA TAKESHI , TOMIYAMA ITARU
IPC分类号： C07D317/00 , A61K31/415 , A61K31/4166 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/445 , A61P1/14 , C07D205/00 , C07D211/00 , C07D213/00 , C07D233/00 , C07D233/32 , C07D233/34 , C07D307/00 , C07D401/04 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/14
摘要： NEW MATERIAL:The 1,3-substituted-2-imidazolidinone derivative of formula I [A is formula II W formula V (R
1 is H or Cl; R
2 and R
3 are Cl, CH
3 or CH
3 O); B is di-lower alkylamino, substituted azetidyl, pyrrolidino, piperazino, piperidyl or morpholino; n is 0 or 1; m is 2 or 3] and its pharmacologically permissible acid addition salt.
EXAMPLE: 1-(5-Chloropyridin-2-yl)-3-(2-pyrrolidinoethyl)-2-imidazolidinone.
USE: Agent for promoting the gastroenteric movement.
PREPARATION: The compound of formula I can be prepared by reacting the compound of formula VI [Y is A-(CH
2 )n or B-(CH
2 )n] with the compound of formula X-Z [X is halogen; when Y is A-(CH
2 )n, then Z is B-(CH
2 )m, and when Y is B-(CH
2 )m, Z is A-(CH
2 )n].
COPYRIGHT: (C)1986,JPO&Japio
摘要翻译：新物质：式I的1,3-取代-2-咪唑烷酮衍生物[A为式II-式V（R 1为H或Cl; R 2和R 3为Cl，CH 3或CH 3 O）; B是二低级烷基氨基，取代的氮杂环丁烷基，吡咯烷子基，哌嗪基，哌啶基或吗啉代; n为0或1; m为2或3]及其药理学上允许的酸加成盐。实施例：1-（5-氯吡啶-2-基）-3-（2-吡咯烷基乙基）-2-咪唑啉酮。使用：促进胃肠道运动的药剂。制备：式I化合物可以通过式VI化合物[Y是A-（CH 2）n或B-（CH 2）n]与式X-Z化合物反应制备[X是卤素; 当Y为A-（CH2）n时，Z为B-（CH2）m，当Y为B-（CH2）m时，Z为A-（CH2）n]。

7. 发明专利

JPS5759862A Novel pyprolidonecarboxylic acid derivative, antiulcer agent containing said compound, and its preparation 失效
标题翻译：新型PYPROLIDONECARBOXYLIC酸衍生物，含有化合物的抗微生物剂及其制备
公开(公告)号：JPS5759862A
公开(公告)日：1982-04-10
申请号：JP13543380
申请日：1980-09-29
申请人： Kotobuki Seiyaku Kk
发明人： TOMIYAMA TAKESHI , TOMIYAMA ITARU
IPC分类号： C07D207/277 , A61K31/40 , A61K31/4015 , A61P1/04
摘要： NEW MATERIAL:The pyrrolidonecarboxylic acid derivative of formulaI[R
1 is phenetyl or cyclohexyl; R
2 is cyclopentylamino, p-methoxybenzylamino, o-methoxy- benzylamino, phenylethanolamino, 2-(4-methoxyphenyl)ethylamino, 2-(4-chloro- phenyl)ethylamino, etc.].
USE: Useful as a remedy for gastric ulcer and gastritis. It has low toxicity.
PROCESS: The compound of formulaIis prepared, e.g. by reacting the N-substituted pyrrolidonecarboxylic acid of formula II with the amine of formula R
2 -H. The compound of formula II can be obtained e.g. by melting itaconic acid with the amine of formula H
2 N-R
1 .
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：新材料：式I的吡咯烷酮羧酸衍生物[R1是苯乙基或环己基; R2是环戊基氨基，对甲氧基苄基氨基，邻甲氧基 - 苄基氨基，苯基乙醇氨基，2-（4-甲氧基苯基）乙基氨基，2-（4-氯 - 苯基）乙基氨基等]。用途：可用作胃溃疡和胃炎的补救措施。毒性低。方法：制备式I的化合物。通过使式II的N-取代的吡咯烷酮羧酸与式R2-H的胺反应。式II的化合物可以例如获得。通过用式H2N-R1的胺溶解衣康酸。

8. 发明专利

JPS5735555A 3-substituted 2-propenenitrile derivative and its preparation 失效
标题翻译： 3-取代的2-丙酮衍生物及其制备
公开(公告)号：JPS5735555A
公开(公告)日：1982-02-26
申请号：JP10906080
申请日：1980-08-08
申请人： Kotobuki Seiyaku Kk
发明人： TOMIYAMA TAKESHI , TOMIYAMA ITARU
IPC分类号： C07D333/24 , A61K31/165 , A61K31/17 , A61K31/34 , A61K31/341 , A61K31/41 , A61P1/04 , C07C67/00 , C07C239/00 , C07C261/04 , C07C275/24 , C07C325/00 , C07C327/44 , C07D307/52 , C07D307/54 , C07D333/10 , C07D405/06 , C07D405/12 , C07D409/06 , C07D417/06
摘要： NEW MATERIAL:A compound shown by the formula I [A is furanyl, thienyl, phenyl; when R
1 is S, R
2 is amino (the case wherein R
1 and R
2 are subjected to ring formation by -COCH
2 CO- is included); when R
1 is =N-CN or =N-CONH
2 , R
2 is -NHR
3 (R
3 is H, alkyl, cyclohexyl, pyridyl, piperazyl, -NH.NH-COC
2 H
5 ].
EXAMPLE: 3-(2-Thienyl)-2-propenylthioamide.
USE: An inhibitor for secretion of gastric juice.
PROCESS: A 3 substituted propennitrile shown by the formula II (R is lower alkyl) is reacted with an alcohol, to give an iminoether shown by the formula III, which is reacted with cyanamide and HR
2 , to give a compound shown by the formula I.
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：新材料：由式I表示的化合物[A是呋喃基，噻吩基，苯基; 当R 1为S时，R 2为氨基（其中R 1和R 2经由-COCH 2 CO-形成环的情况）; 当R 1为= N-CN或= N-CONH 2时，R 2为-NHR 3（R 3为H，烷基，环己基，吡啶基，哌嗪基，-NH.NH-COC 2 H 5]。实施例3-（2-噻吩基）丙烯硫基酰胺用途：胃液分泌抑制剂方法：将式II所示的3位取代的丙腈（R为低级烷基）与醇反应，得到式III所示的亚氨基醚，与氰胺反应和HR2，得到式I所示的化合物。

9. 发明专利

JPS6153281A 1,3-substituted-2-imidazolidinone derivative, promoter for gastrointestinal motion and its preparation 失效
标题翻译： 1,3-取代的2-咪唑啉酮衍生物，促进剂用于气体运动及其制备
公开(公告)号：JPS6153281A
公开(公告)日：1986-03-17
申请号：JP17515384
申请日：1984-08-24
申请人： Kotobuki Seiyaku Kk
发明人： TOMIYAMA TAKESHI , TOMIYAMA ITARU
IPC分类号： C07D401/12 , A61K31/435 , A61K31/4427 , A61K31/443 , A61K31/445 , A61P1/14 , C07D211/00 , C07D221/00 , C07D233/00 , C07D317/00 , C07D405/14 , C07D491/113
摘要： NEW MATERIAL:A compound shown by the formula I {A is group shown by the formula II [R1 and R2 are H, Cl, or RO- (R is lower alkyl)], or group shown by the formula III; B is group shown by the formula IV (R3 is H, or group shown by the formula V-VII; R4 is H, or OH); n is 2, or 3}, its acid addition salt. EXAMPLE:1-(m-Chlorophenyl)-3-[2-( N-benzylpiperidin-4-yl )amino]ethyl-2-imidazolidinone.hydrochloride. USE:A promoter for gastrointestinal motion, having low action like prolactin. PREPARATION:A compound shown by the formula IX is reacted with a compound shown by the formula X-(CH2)n-B(X ia halogen).
摘要翻译：新物质：由式I所示的化合物（A为式II所示的基团[R 1和R 2为H，Cl或RO-（R为低级烷基）]或式III所示的基团; B是式IV所示的基团（R3是H，或者由式V-VII表示的基团; R4是H或OH）; n为2或3}，其酸加成盐。实施例：1-（间氯苯基）-3- [2-（N-苄基哌啶-4-基）氨基]乙基-2-咪唑啉酮盐酸盐。用途：胃肠运动的促进剂，具有较低的作用，如催乳素。制备：式IX所示的化合物与式X-（CH 2）n -B（X ia卤素）所示的化合物反应。

10. 发明专利

JPS59155375A Thiazole derivative and its preparation 失效
标题翻译：噻唑衍生物及其制备
公开(公告)号：JPS59155375A
公开(公告)日：1984-09-04
申请号：JP2704783
申请日：1983-02-22
申请人： Kotobuki Seiyaku Kk
发明人： TOMIYAMA TAKESHI , TOMIYAMA ITARU
IPC分类号： C07D277/20 , A61K31/425 , A61K31/426 , A61K31/445 , A61K31/495 , A61P1/04 , C07D277/40 , C07D277/44 , C07D417/12
摘要： NEW MATERIAL:A thiazole derivative shown by the formula I (A is NH
2 , or lower acylamino; B is pyridyl, piperidyl, lower alkyl-substituted piperidyl, 4,4- substituted piperidyl, piperazyl, pyrazyl, pyrazolyl, imidazolyl, or pyridazyl; n is 1, 2 or 3) or its acid addition salt.
EXAMPLE: 2-Amino-4-[2-(piperidin-1-yl)ethyl]thiomethylthiazole.
USE: A gastric secretion inhibitor.
PREPARATION: A compound shown by the formula II(Y is SH or group shown by the formula III) is reacted with a compound shown by the formula X-(CH
2 )
n - B(X is halogen) to give a compound shown by the formula I . Or, a compound shown by the formula IV in the compound shown by the formula I obtained by the above-mentioned method is reacted with a lower fatty acid anhydride or lower acylhalide to give a compound shown by the formula V in the compound shown by the formula I . If necessary, the prepared base is converted into its salt.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新材料：式I所示的噻唑衍生物（A为NH 2或低级酰氨基; B为吡啶基，哌啶基，低级烷基取代的哌啶基，4,4-取代的哌啶基，哌嗪基，吡唑基，吡唑基，咪唑基或哒嗪基; n为1,2或3）或其酸加成盐。实施例：2-氨基-4- [2-（哌啶-1-基）乙基] thiomethylthiazole。用途：胃分泌抑制剂。制备：将式II所示的化合物（Y为SH或式III所示的基团）与式X-（CH 2）n -B所示的化合物（X为卤素）反应，得到公式I 或者，将通过上述方法得到的式I化合物中的式Ⅳ所示化合物与低级脂肪酸酐或低级酰卤反应，得到式V所示的化合物公式I 如果需要，将制备的碱转化成其盐。

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