专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US4954642A Forskolin compounds 失效
标题翻译：福斯康林化合物
公开(公告)号：US4954642A
公开(公告)日：1990-09-04
申请号：US361763
申请日：1989-05-30
申请人： Tochiro Tatee , Takashi Takahira , Kouwa Yamashita , Masao Sakurai , Akira Shiozawa , Kazuhisa Narita
发明人： Tochiro Tatee , Takashi Takahira , Kouwa Yamashita , Masao Sakurai , Akira Shiozawa , Kazuhisa Narita
IPC分类号： A61K31/35 , C07D311/92 , C07D405/12
CPC分类号： C07D311/92
摘要： This invention relates to forskolin derivatives, their physiologically acceptable salts, and a process for producing these compounds. The forskolin derivative is represented by the general formula ##STR1## wherein; I. when R.sup.1 is hydrogen and R.sup.4 is vinyl, ethyl, or cyclopropyl,(1) either of R.sup.2 and R.sup.3 denotes a residue represented by the formula ##STR2## wherein each of R.sup.5 and R.sup.6 denotes hydrogen or lower alkyl or R.sup.5 and R.sup.6 combine with each other to form a lower alkylene chain which may or may not contain an oxygen or nitrogen atom and m is an integer of 1 to 5, and the other one of R.sup.2 and R.sup.3 denotes hydrogen or a residue represented by the formula CO(CH.sub.2).sub.n X, X being hydrogen or ##STR3## wherein, each of R.sup.7 and R.sup.8 denotes hydrogen or lower alkyl or R.sup.7 and R.sup.8 combine with each other to form a lower alkylene chain which may or may not contain an oxygen or nitrogen atom, and n being an integer of 1 to 5, or(2) R.sup.2 denotes hydrogen or --COCH.sub.2 CH.sub.2 CO.sub.2 H and R.sup.3 denotes hydrogen, --COCH.sub.3, --COCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H, or --COCH(OH)CH.sub.2 OH with the proviso that R.sup.3 is one of the last two residues when R.sup.2 is hydrogen, andII. whenR.sup.1 is a residue represented by a formula of CO(CH.sub.2).sub.p CO.sub.2 H and ##STR4## wherein, each of R.sup.9 and R.sup.10 denotes hydrogen or lower alkyl, p is an integer of 0 to 5, and q is an integer of 1 to 5,R.sup.2 denotes hydrogen , R.sup.3 denotes acetyl, and R.sup.4 denotes vinyl.
摘要翻译：本发明涉及毛喉素衍生物及其生理学上可接受的盐，以及这些化合物的制备方法。毛喉素衍生物由通式表示，其中：当R1是氢并且R4是乙烯基，乙基或环丙基时，（1）R2和R3中的任一个表示由下式表示的残基：其中R 5和R 6各自表示氢或低级烷基或R 5和R 6结合彼此形成可以含有或不含有氧或氮原子并且m为1〜5的整数的低级亚烷基链，R2和R3中的另一个表示氢或由式CO（CH2）表示的残基）n X，X为氢或者其中，R 7和R 8各自表示氢或低级烷基，或者R 7和R 8彼此结合形成可含有或不含有氧或氮原子的低级亚烷基链，n 为1〜5的整数，或（2）R2表示氢或-COCH2 CH2CO2H，R3表示氢，-COCH3，-COCH2CH2CH2CO2H或-COCH（OH）CH2OH，条件是R3为最后两个残基之一， R2是氢，II。当R 1是由CO（CH 2）p CO 2 H和的式表示的残基时，R 9和R 10各自表示氢或低级烷基，p是0至5的整数，q是1至5的整数，R2表示氢，R3表示乙酰基，R4表示乙烯基。

2. 发明授权

US5302730A Process for the preparation of 6,7-diacyl-7-deacetylforskolin derivatives 失效
标题翻译：制备6,7-二酰基-7-脱乙酰福斯克林衍生物的方法
公开(公告)号：US5302730A
公开(公告)日：1994-04-12
申请号：US71616
申请日：1993-06-04
申请人： Tochiro Tatee , Akira Shiozawa , Hirotaka Yamamoto , Yuh-ichiro Ichikawa , Aya Narita , Chikara Komuro , Kazuhisa Narita
发明人： Tochiro Tatee , Akira Shiozawa , Hirotaka Yamamoto , Yuh-ichiro Ichikawa , Aya Narita , Chikara Komuro , Kazuhisa Narita
IPC分类号： C07D311/92
CPC分类号： C07D311/92
摘要： This invention relates to a process for the preparation of a 6,7-diacyl-7-deacetylforskolin derivative represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 each stands for an acyl group and R.sup.3 stands for an aliphatic group having 2 to 3 carbon atoms, which comprises eliminating the acyl group at position 1 in a 1,6,7-triacyl-7-deacetylforskolin derivative represented by the general formula: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, by solvolysis. The compound of the formula (I) is expected as medicine.
摘要翻译：本发明涉及一种制备由以下通式表示的6,7-二酰基-7-脱乙酰福斯克林衍生物的方法：（*化学结构*）（I）其中R1和R2各自代表酰基，R3代表具有2至3个碳原子的脂族基团，其包括通过以下通式除去在通式为（* CHEMICAL STRUCTURE *）（III）表示的1,6,7-三酰基-7-脱乙酰福斯克林衍生物中的第1位的酰基，其中R1 ，R2和R3如上定义，通过溶剂分解。预期式（I）化合物为药物。

3. 发明授权

US5610315A Process for the preparation of 6,7-diacyl-7-deacetylforskolin derivatives 失效
标题翻译：制备6,7-二酰基-7-脱乙酰福斯克林衍生物的方法
公开(公告)号：US5610315A
公开(公告)日：1997-03-11
申请号：US442403
申请日：1995-05-16
申请人： Tochiro Tatee , Akira Shiozawa , Hirotaka Yamamoto , Yuh-ichiro Ichikawa , Aya Ishikawa , Chikara Komuro , Kazuhisa Narita
发明人： Tochiro Tatee , Akira Shiozawa , Hirotaka Yamamoto , Yuh-ichiro Ichikawa , Aya Ishikawa , Chikara Komuro , Kazuhisa Narita
IPC分类号： C07D311/92
CPC分类号： C07D311/92
摘要： This invention relates to a process for the preparation of a 6,7-diacyl-7-deacetylforskolin derivative represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 each stands for an acyl group and R.sup.3 stands for an aliphatic group having 2 to 3 carbon atoms, which comprises eliminating the acyl group at position 1 in a 1,6,7-triacyl-7-deacetylforskolin derivative represented by the general formula: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, by solvolysis. The compound of the formula (I) is expected as medicine.
摘要翻译：本发明涉及一种制备由以下通式表示的6,7-二酰基-7-脱乙酰福斯克林衍生物的方法：其中R1和R2各自代表酰基，R3代表脂族基团具有2至3个碳原子，其包括在通式（III）表示的1,6,7-三酰基-7-脱乙酰福斯克林衍生物中除去第1位的酰基，其中R 1，R 2和R 3为通过溶剂分解来定义。预期式（I）化合物为药物。

4. 发明授权

US5324730A Phenoxyphosphoryloxymethyl cyclobutyl purines 失效
标题翻译：苯氧基磷酰氧基甲基环丁基嘌呤
公开(公告)号：US5324730A
公开(公告)日：1994-06-28
申请号：US704085
申请日：1991-05-22
申请人： Yuh-ichiro Ichikawa , Hiroshi Akaba , Yuka Sugawara , Hideo Sugimura , Kazuhisa Narita , Akira Shiozawa , Kouwa Yamashita , Sayuri Kato , Yukihiro Nishiyama , Kenichi Matsubara , Takemitsu Nagahata
发明人： Yuh-ichiro Ichikawa , Hiroshi Akaba , Yuka Sugawara , Hideo Sugimura , Kazuhisa Narita , Akira Shiozawa , Kouwa Yamashita , Sayuri Kato , Yukihiro Nishiyama , Kenichi Matsubara , Takemitsu Nagahata
IPC分类号： C07D473/00 , C07F9/6558 , C07F9/6561 , A61K31/52 , C07D473/18 , C07D473/32 , C07F9/09
CPC分类号： C07D473/00 , C07F9/65583 , C07F9/6561 , C07F9/65616
摘要： This invention relates to cyclobutane derivatives represented by the following general formula (1) and physiologically acceptable salts thereof: ##STR1## wherein B represents a nucleic acid base derivative, R.sup.1 and R.sup.2 independently represent hydrogen atom, dialkylaminoacyl group, 1,4-dihydro-1-methylnicotinoyl group or substituted phosphoric acid group, provided that either one of R.sup.1 and R.sup.2 is a group other than hydrogen atom.The compounds of this invention exhibit a high oral absorbability and are metabolized in vivo into the compounds of formula (1a). Accordingly, the compounds of this invention are expectedly useful as antiviral agent.
摘要翻译：本发明涉及由以下通式（1）表示的环丁烷衍生物及其生理学上可接受的盐：其中B表示核酸碱基衍生物，R1和R2独立地表示氢原子，二烷基氨基酰基，1,4 - 二氢-1-甲基烟酰基或取代的磷酸基，条件是R 1和R 2中的任一个是除氢原子之外的基团。本发明的化合物表现出高的口服吸收性，并且在体内被代谢为式（1a）的化合物。因此，预期本发明的化合物可用作抗病毒剂。

5. 发明授权

US5057535A Derivatives of an aminoketone 失效
标题翻译：氨基酮的衍生物
公开(公告)号：US5057535A
公开(公告)日：1991-10-15
申请号：US101134
申请日：1987-09-25
申请人： Akira Shiozawa , Michio Ishikawa , Giichi Izumi , Katsuhiko Sakitama , Kazuhisa Narita , Shuji Kurashige , Takeji Sakasai , Kazuo Ohtsuki , Hideo Sugimura , Hirotaka Yamamoto
发明人： Akira Shiozawa , Michio Ishikawa , Giichi Izumi , Katsuhiko Sakitama , Kazuhisa Narita , Shuji Kurashige , Takeji Sakasai , Kazuo Ohtsuki , Hideo Sugimura , Hirotaka Yamamoto
IPC分类号： C07C225/06 , C07D295/108
CPC分类号： C07D295/108 , C07C225/06 , C07C2101/14 , C07C2102/10
摘要： A new class of aminoketone derivatives according to the formula: ##STR1## and certain propiophenone derivatives in particular, corresponding to the formula: ##STR2## having central muscle relaxant activity.
摘要翻译：一类新的具有下式的氨基酮衍生物：特别是某些苯丙酮衍生物，特别是对应于具有中枢肌肉松弛剂活性的式：。

6. 发明授权

US5296492A Certain chroman derivatives useful for treating symptoms caused by contraction of smooth muscles, circulatory diseases or epilepsy 失效
标题翻译：某些苯并二氢吡喃衍生物可用于治疗由平滑肌，循环系统疾病或癫痫的收缩引起的症状
公开(公告)号：US5296492A
公开(公告)日：1994-03-22
申请号：US893403
申请日：1992-06-03
申请人： Akira Shiozawa , Atsuro Inubushi , Kazuhisa Narita , Yukihiro Sagawa , Makoto Hosono , Masashi Iida
发明人： Akira Shiozawa , Atsuro Inubushi , Kazuhisa Narita , Yukihiro Sagawa , Makoto Hosono , Masashi Iida
IPC分类号： A61K31/35 , A61K31/353 , A61K31/44 , A61K31/4433 , A61P9/00 , A61P21/00 , C07D213/50 , C07D213/64 , C07D311/20 , C07D311/68 , C07D405/04 , C07F7/18 , C07D407/04 , C07F7/02 , A61K31/695
CPC分类号： C07D405/04 , C07F7/1856
摘要： A chroman derivative represented by the following general formula [1]: ##STR1## wherein R.sub.1 represents cyano group, nitro group, halogenomethyl group or --SO.sub.2 --X group (X represents lower alkyl group having 1-6 carbon atoms or aryl group); R.sub.2 represents hydrogen atom or OA group (A represents hydrogen atom, nitro group, lower acyl group having 1-6 carbon atoms, arylcarbonyl group, lower alkylsulfonyl group having 1-6 carbon atoms, arylsulfonyl group, arylalkyl group, tetrahydropyranyl group, lower alkoxycarbonyl group having 1-6 carbon atoms, arylalkoxycarbonyl group or silyl derivative group); R.sub.3 singly represents a hydrogen atom; or R.sub.3 forms a bond jointly with R.sub.2 ; and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 each represent hydrogen atom, vinyl group, formyl group, --Y--(OA).sub.n group (Y represents straight or branched chain alkylene group having 1-6 carbon atoms or lower alkenyl group having 1-6 carbon atoms, A is as defined above, and n represents an integer of 1-3.The compound of this invention is expected to be effectively usable as an agent for treatment of various symptoms due to the contraction of smooth muscles, for treatment of the diseases of the circulatory system and for treatment of epilepsy.
摘要翻译：由下列通式（1）表示的苯并二氢吡喃衍生物：（*化学结构*）（1）其中R1表示氰基，硝基，卤代甲基或-SO2-X基（X表示具有1-6个碳原子的低级烷基原子或芳基）; R2表示氢原子或OA基（A表示氢原子，硝基，具有1-6个碳原子的低级酰基，芳基羰基，具有1-6个碳原子的低级烷基磺酰基，芳基磺酰基，芳基烷基，四氢吡喃基，低级烷氧基羰基具有1-6个碳原子的基团，芳基烷氧基羰基或甲硅烷基衍生物基团）; R3单独表示氢原子; 或R3与R2一起形成键; 和R 4，R 5，R 6和R 7各自表示氢原子，乙烯基，甲酰基，-Y-（OA）n基（Y表示具有1-6个碳原子的直链或支链亚烷基或具有1-6个碳原子的低级链烯基碳原子，A如上所定义，n表示1-3的整数。预期本发明化合物可有效地用作治疗由于平滑肌收缩引起的各种症状的药剂，用于治疗循环系统疾病和治疗癫痫。

7. 发明授权

US5103022A Process for producing an optically active aminoketone derivative 失效
标题翻译：光学活性氨基酮衍生物的制造方法
公开(公告)号：US5103022A
公开(公告)日：1992-04-07
申请号：US628993
申请日：1990-12-18
申请人： Akira Shiozawa , Kazuhisa Narita , Shuji Kurashige , Takeji Sakasai , Kazuo Ohtsuki , Hideo Sugimura , Hirotaka Yamamoto
发明人： Akira Shiozawa , Kazuhisa Narita , Shuji Kurashige , Takeji Sakasai , Kazuo Ohtsuki , Hideo Sugimura , Hirotaka Yamamoto
IPC分类号： C07C45/29 , C07C45/46 , C07C49/76 , C07C49/782 , C07C49/794 , C07C49/798 , C07C49/80 , C07C49/807 , C07C49/825 , C07C49/83 , C07C49/84 , C07C225/06 , C07D295/108 , C07D295/112
CPC分类号： C07D295/112 , C07C225/06 , C07C45/292 , C07C45/46 , C07C49/76 , C07C49/782 , C07C49/794 , C07C49/798 , C07C49/80 , C07C49/807 , C07C49/825 , C07C49/83 , C07C49/84 , C07D295/108 , C07C2101/14 , C07C2102/10
摘要： A process for producing an optically active aminoketone derivative having a central muscle relaxant activity is described wherein a racemic mixture of the aminoketone is reacted with optically active L-acetylphenylglycine and then isolating the optically active L-aminoketone from the diastereomeric salts formed by the reaction.
摘要翻译：其中描述了一种具有中心肌松弛活性的光学活性氨基酮衍生物的制备方法，其中将氨基酮的外消旋混合物与光学活性的L-乙酰基苯基甘氨酸反应，然后从由反应形成的非对映异构体盐分离光学活性的L-氨基酮。

8. 发明授权

US5166397A Process for producing optically active cyclobutylamines 失效
标题翻译：光学活性环丁胺的制备方法
公开(公告)号：US5166397A
公开(公告)日：1992-11-24
申请号：US757312
申请日：1991-09-10
申请人： Kazuhisa Narita , Masashi Nagai , Hideo Sugimura , Yukihiro Sagawa , Akira Shiozawa
发明人： Kazuhisa Narita , Masashi Nagai , Hideo Sugimura , Yukihiro Sagawa , Akira Shiozawa
IPC分类号： C07C213/10 , C07C215/42 , C07D473/00
CPC分类号： C07D473/00 , C07C213/10 , C07C215/42 , C07C2101/04 , Y02P20/55
摘要： This invention relates to a process for producing an optically active cyclobutylamine which comprises reacting a racemic modification of cyclobuthylamine represented by the following general formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 represent each a hydrogen atom or a protecting group; with an optically active N-acylphenylglycine to thereby give two corresponding diastereomeric salts, crystallizing the more difficultly soluble diastereomeric salt and isolating the corresponding optically active cyclobutylamine from the diastereomeric salt thus crystallized. The optically active substances of the compound of the above general formula [I] are useful as, for example, an intermediate in the synthesis of 9-[(1R, 2R, 3S)-2,3-bis(hydroxymethyl)-1-cyclobutyl]guanine which is expected as an antiviral agent.
摘要翻译：本发明涉及一种光学活性环丁胺的制备方法，其包括使由以下通式[I]表示的环丁胺的外消旋体：其中R 1和R 2各自表示氢原子或保护基; 与光学活性的N-酰基苯基甘氨酸反应，从而得到两个相应的非对映异构体盐，使难溶于水的非对映异构体盐结晶，并从如此结晶的非对映体盐中分离相应的光学活性环丁基胺。上述通式[I]的化合物的光学活性物质可用作例如合成9 - [（1R，2R，3S）-2,3-双（羟甲基）-1- 环丁基]鸟嘌呤，其被预期作为抗病毒剂。

9. 发明授权

US06221868B1 Remedies/preventives for frequent urination/urinary incontinence and tropone derivatives 失效
标题翻译：排尿/尿失禁和皮质酮衍生物的治疗/预防措施
公开(公告)号：US06221868B1
公开(公告)日：2001-04-24
申请号：US09446423
申请日：1999-12-20
申请人： Ichiro Koga , Kazuhisa Narita , Atsushi Okada
发明人： Ichiro Koga , Kazuhisa Narita , Atsushi Okada
IPC分类号： C07D21114
CPC分类号： C07D295/116 , C07C2601/16 , C07C2601/18 , C07D211/14 , C07D213/74 , C07D295/135
摘要： Remedies/preventives (therapeutic or preventive agents) against frequent urination (pollakiuria)/urinary incontinence which contain as an active ingredient compound having a tropone structure or pharmacologically acceptable salt thereof and a novel compound having the tropone structure. The compounds having a tropone structure and having the above pharmacological effects are those represented by, for example, general (1): wherein R1 and R2 represent each a hydrogen atom, lower alkyl group, etc., R3 represents —OR or —NR2; R4, R5 and R12 represents each a hydrogen atom or a lower alkyl group, X represents a nitrogen atom or CH, Z represents —CHAr2, an unsubstituted or substituted phenyl, etc. m is 1 or 2. These compounds are novel ones excluding those wherein Z is —CHAr2.
摘要翻译：含有作为具有托品酮结构的活性成分化合物或其药理学上可接受的盐的频繁排尿（尿频尿）/尿失禁的治疗或预防剂（治疗或预防剂）和具有托罗酮结构的新化合物。具有上述药理作用的具有托品酮结构的化合物是由例如通式（1）表示的化合物：其中，R 1和R 2各自表示氢原子，低级烷基等，R 3表示-OR或-NR 2; R4，R5和R12各自表示氢原子或低级烷基，X表示氮原子或CH，Z表示-CHAr2，未取代或取代的苯基等，m为1或2.这些化合物是除其中Z是-CHAr 2。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式