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公开(公告)号:US5712263A
公开(公告)日:1998-01-27
申请号:US663929
申请日:1996-06-14
申请人: Chihiro Yokoo , Hisaya Wada , Hidemichi Mitome , Tatsuhiko Sano , Katsuo Hatayama , Yasuji Yamada
发明人: Chihiro Yokoo , Hisaya Wada , Hidemichi Mitome , Tatsuhiko Sano , Katsuo Hatayama , Yasuji Yamada
CPC分类号: C07J21/006 , C07J17/00 , C07J7/002 , C07J9/00
摘要: To provide novel steroid derivatives having an antitumor action which can be synthesized efficiently and stereoselectively by means of synthetic organic chemistry. A steroid derivative represented by the formula: ##STR1## wherein R is an alkyl group having 1 to 13 carbon atoms, A is a hydroxyl group or a group easily hydrolyzable to a hydroxyl group, X and Y together form an oxo group or an alkylenedioxy group having 2 or 3 carbon atoms, X is a hydroxyl group, an alkoxy group having 1 to 5 carbon atoms or a group easily hydrolyzable to a hydroxyl group, Y is a hydrogen atom or an alkoxy group having 1 to 5 carbon atoms, with the proviso that when X is a hydroxyl group or a group easily hydrolyzable to a hydroxyl group, Y is a hydrogen atom, and when X is an alkoxy group having 1 to 5 carbon atoms, Y is an alkoxy group having 1 to 5 carbon atoms, or a salt thereof.
摘要翻译: 提供具有抗肿瘤作用的新型类固醇衍生物,其可以通过合成有机化学有效地和立体选择性地合成。 由下式表示的类固醇衍生物:其中R是具有1至13个碳原子的烷基,A是羟基或易于水解成羟基的基团,X和Y一起形成氧代基 或具有2或3个碳原子的亚烷基二氧基,X是羟基,具有1至5个碳原子的烷氧基或易于水解成羟基的基团,Y是氢原子或具有1至5个碳原子的烷氧基 原子,条件是当X是羟基或易于水解成羟基的基团时,Y是氢原子,当X是具有1至5个碳原子的烷氧基时,Y是具有1至 5个碳原子,或其盐。
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公开(公告)号:US5281717A
公开(公告)日:1994-01-25
申请号:US30089
申请日:1993-03-26
IPC分类号: A61K31/40 , A61K31/401 , A61K31/4025 , A61K38/00 , A61P43/00 , C07D405/12 , C07K5/062
CPC分类号: C07D405/12 , C07K5/06034 , A61K38/00 , Y02P20/55
摘要: An epoxysuccinamic acid derivartive represented by the formula: ##STR1## (wherein R.sup.1 is an alkyl group having 1 to 10 carbon atoms, a phenyl group or a benzyl group), a pharmaceutically acceptable salt thereof, and an intermediate thereof are disclosed The compound of Formula I is useful as a therapeutical agent for muscular atrophy diseases.
摘要翻译: PCT No.PCT / JP91 / 01288 Sec。 371日期1993年3月26日 102(e)1993年3月26日PCT PCT 1991年9月27日PCT公布。 公开号WO92 / 06090 日期:1992年4月16日。由式(*化学结构*)I(其中R 1为具有1〜10个碳原子的烷基,苯基或苄基)表示的环氧琥珀酰胺酸衍生物,药学上可接受的盐 并且其中间体被公开。式I的化合物可用作肌肉萎缩性疾病的治疗剂。
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公开(公告)号:US07279584B2
公开(公告)日:2007-10-09
申请号:US10568708
申请日:2004-08-18
IPC分类号: C07D207/16
CPC分类号: C07D207/16 , Y02P20/55
摘要: The present invention provides a safer method for production of a cis-4-fluoro-L-proline derivative under milder conditions and in good yield to give a product of high purity on an industrial scale at low cost. Namely, the present invention provides a method for producing a cis-4-fluoro-L-proline derivative, which comprises reacting a trans-4-hydroxy-L-proline derivative of the following Formula [I]: (wherein R1 represents a protecting group for an α-amino group, and R2 represents a protecting group for a carboxyl group) with N,N-diethyl-N-(1,1,2,3,3,3-hexafluoropropyl)amine in the presence of a hydrogen fluoride-scavenger.
摘要翻译: 本发明提供了一种在更温和的条件下生产顺式-4-氟-L-脯氨酸衍生物的更安全的方法,并以良好的产率,以低成本在工业规模上得到高纯度的产物。 即,本发明提供顺式-4-氟-L-脯氨酸衍生物的制造方法,该方法包括使下式[I]的反式-4-羟基-L-脯氨酸衍生物:其中R < 1代表α-氨基的保护基,R 2代表羧基的保护基)与N,N-二乙基-N-(1,1,2 ,3,3,3-六氟丙基)胺在氟化氢 - 清除剂的存在下反应。
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公开(公告)号:US20060281927A1
公开(公告)日:2006-12-14
申请号:US10568708
申请日:2004-08-18
IPC分类号: C07D207/02
CPC分类号: C07D207/16 , Y02P20/55
摘要: The present invention provides a safer method for production of a cis-4-fluoro-L-proline derivative under milder conditions and in good yield to give a product of high purity on an industrial scale at low cost. Namely, the present invention provides a method for producing a cis-4-fluoro-L-proline derivative, which comprises reacting a trans-4-hydroxy-L-proline derivative of the following Formula [I]: (wherein R1 represents a protecting group for an α-amino group, and R2 represents a protecting group for a carboxyl group) with N,N-diethyl-N-(1,1,2,3,3,3-hexafluoropropyl)amine in the presence of a hydrogen fluoride-scavenger.
摘要翻译: 本发明提供了一种在更温和的条件下生产顺式-4-氟-L-脯氨酸衍生物的更安全的方法,并以良好的产率,以低成本在工业规模上得到高纯度的产物。 即,本发明提供顺式-4-氟-L-脯氨酸衍生物的制造方法,该方法包括使下式[I]的反式-4-羟基-L-脯氨酸衍生物:其中R < 1代表α-氨基的保护基,R 2代表羧基的保护基)与N,N-二乙基-N-(1,1,2 ,3,3,3-六氟丙基)胺在氟化氢 - 清除剂的存在下反应。
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公开(公告)号:US4937332A
公开(公告)日:1990-06-26
申请号:US286171
申请日:1988-12-19
IPC分类号: A61K31/545 , C07D501/36 , C07D501/59
CPC分类号: C07D501/59 , Y02P20/55
摘要: A cephalosporin derivative represented by the general formula ##STR1## wherein R.sup.1 is a hydrogen atom or a protecting group of the amino group, R.sup.2 is a hydrogen atom or a protecting group of the hydroxyl group, R.sup.3 is a hydrogen atom or a protecting group of the carboxyl group, and R.sup.4 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, and the non-toxic salts thereof are useful as antibacterial agents.
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公开(公告)号:US4699981A
公开(公告)日:1987-10-13
申请号:US893783
申请日:1986-08-06
申请人: Yoshiaki Watanabe , Chihiro Yokoo , Masami Goi , Akira Onodera , Mitsuo Murata , Hiroshi Fukushima , Kaoru Sota
发明人: Yoshiaki Watanabe , Chihiro Yokoo , Masami Goi , Akira Onodera , Mitsuo Murata , Hiroshi Fukushima , Kaoru Sota
IPC分类号: A61K31/545 , C07D501/36 , C07D501/59
CPC分类号: C07D501/59
摘要: Cephalosporin derivatives represented by the general formula ##STR1## Wherein X represents a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, an allyl group, a cycloalkyl group having 5 or 6 carbon atoms or a benzyl group, and the non-toxic salts thereof are disclosed. These compounds are useful as antibacterial agents.
摘要翻译: 其中X表示氢原子,具有1至4个碳原子的低级烷基,烯丙基,具有5或6个碳原子的环烷基或苄基的通式为其的头孢菌素衍生物 ,并公开了其无毒盐。 这些化合物可用作抗菌剂。
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公开(公告)号:US4921953A
公开(公告)日:1990-05-01
申请号:US309160
申请日:1989-02-13
IPC分类号: A61K31/545 , C07D501/36 , C07D501/59
CPC分类号: C07D501/59 , Y02P20/55
摘要: A cephalosporin derivative represented by the formula ##STR1## wherein R.sup.1 is a hydrogen atom or a protecting group of the amino group, R.sup.2 is a hydrogen atom or a protecting group of the hydroxyl group, R.sup.3 is a hydrogen atom or a protecting group of the carboxyl group, X is a halogen atom, a cyano group, a vinyl group, a lower alkoxy group having 1 to 4 carbon atoms or a lower alkylthio group having 1 to 4 carbon atoms and n is an integer of 1 to 3, and a non-toxic salt thereof are useful as antibacterial agents for oral administration.
摘要翻译: 由下式表示的头孢菌素衍生物,其中R1为氢原子或氨基保护基,R2为氢原子或羟基保护基,R3为氢原子或保护基, 羧基,X为卤素原子,氰基,乙烯基,碳原子数1〜4的低级烷氧基或碳原子数1〜4的低级烷硫基,n为1〜3的整数, 其无毒盐可用作口服给药的抗菌剂。
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公开(公告)号:US4190581A
公开(公告)日:1980-02-26
申请号:US929566
申请日:1978-07-31
申请人: Yoshiaki Watanabe , Chihiro Yokoo , Toshifumi Asaka , Jiro Sawada
发明人: Yoshiaki Watanabe , Chihiro Yokoo , Toshifumi Asaka , Jiro Sawada
IPC分类号: C07D241/42 , C07D471/04 , C07D499/00 , C07D499/68 , C07D499/50 , C07D401/04
CPC分类号: C07D471/04 , C07D241/42 , C07D499/00
摘要: Novel penicillin derivatives of the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R is hydrogen or hydroxy, are produced by acylating ampicillin, amoxicillin or a salt thereof with 4-hydroxy-pyrazino[2,3-f]quinoline-3-carboxylic acid or its functional derivative. They have high anti-pseudomonas activity and other antibacterial activity against gram-positive and gram-negative bacteria, and are of extremely low toxicity.
摘要翻译: 通过用4-羟基 - 吡嗪并[2,3-f]将氨苄青霉素,阿莫西林或其盐酰化来制备其中R为氢或羟基的新颖的式
+ TR 及其药学上可接受的盐的青霉素衍生物 ]喹啉-3-羧酸或其官能衍生物。 它们对革兰氏阳性和革兰氏阴性细菌具有很高的抗假单胞菌活性和其他抗菌活性,毒性极低。 -
公开(公告)号:US4841044A
公开(公告)日:1989-06-20
申请号:US943037
申请日:1986-12-18
申请人: Yoshiaki Watanabe , Chihiro Yokoo , Masami Goi , Akira Onodera , Mitsuo Murata , Hiroshi Fukushima , Minoru Taguchi , Kaoru Sota
发明人: Yoshiaki Watanabe , Chihiro Yokoo , Masami Goi , Akira Onodera , Mitsuo Murata , Hiroshi Fukushima , Minoru Taguchi , Kaoru Sota
IPC分类号: A61K31/545 , C07D501/36 , C07D501/59
CPC分类号: C07D501/59
摘要: Cephalosporin derivatives represented by the general formula ##STR1## wherein R is a hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, R' is a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a cycloalkyl group having 5 or 6 carbon atoms or a benzyl group, or R and R' together with the nitrogen atom to which they are attached form a tetrahydropyridinyl group, a morpholinyl group or pyrroridinyl group, and the non-toxic salts thereof are disclosed. These compounds are useful as antibacterial agents.
摘要翻译: 其中R为氢原子或碳原子数为1〜4的低级烷基,R'为氢原子,碳原子数1〜4的低级烷基, ,具有5或6个碳原子的环烷基或苄基,或R和R'与它们所连接的氮原子一起形成四氢吡啶基,吗啉基或吡咯烷基,其无毒盐是 披露 这些化合物可用作抗菌剂。
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公开(公告)号:US4357470A
公开(公告)日:1982-11-02
申请号:US256780
申请日:1981-04-23
申请人: Yoshiaki Watanabe , Chihiro Yokoo , Toshifumi Asaka , Akira Onodera , Kaoru Sota , Jiro Sawada
发明人: Yoshiaki Watanabe , Chihiro Yokoo , Toshifumi Asaka , Akira Onodera , Kaoru Sota , Jiro Sawada
IPC分类号: C07D519/06 , A61K31/545 , A61P31/04 , C07D471/04 , C07D501/26 , C07D501/36 , C07D501/56
CPC分类号: C07D471/04
摘要: Novel cephalosporin compounds having the general formula ##STR1## wherein X represents hydrogen atom or hydroxy group, and the non-toxic pharmacologically acceptable salts thereof are disclosed. These compounds are useful as antibacterial agents.
摘要翻译: 公开了具有通式
+ TR 的新型头孢菌素化合物,其中X表示氢原子或羟基,并且其无毒的药理学上可接受的盐被公开。 这些化合物可用作抗菌剂。
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