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1. 发明授权

US5204345A 6-epifumagillols and the pharmaceutical use thereof 失效
标题翻译： 6-EPIFUMAGILLOLS及其药物用途
公开(公告)号：US5204345A
公开(公告)日：1993-04-20
申请号：US489010
申请日：1990-03-06
申请人： Shoji Kishimoto , Takeshi Fujita
发明人： Shoji Kishimoto , Takeshi Fujita
IPC分类号： C07D303/22 , C07D405/12
CPC分类号： C07D303/22 , C07D405/12
摘要： The present invention relates to a compound of the formula: ##STR1## wherein R.sup.1 is 2-methyl-1-propenyl group or isobutyl group; R.sup.2 is hydrogen atom, an optionally substituted aliphatic hydrocarbon residue or an optionally substituted acyl group, or a salt thereof.The compound (I) of the invention has, among others, angiogenesis inhibiting activity, cell-proliferation inhibiting activity and immune reaction inhibiting activity, thus being useful as medicines, etc.

2. 发明授权

US5166172A Fumagillol derivatives and pharmaceutical compositions thereof 失效
标题翻译：烟曲霉醇衍生物及其药物组合物
公开(公告)号：US5166172A
公开(公告)日：1992-11-24
申请号：US662120
申请日：1991-02-28
申请人： Shoji Kishimoto , Takeshi Fujita
发明人： Shoji Kishimoto , Takeshi Fujita
IPC分类号： A61K31/335 , C07D303/22 , C07D405/14 , C07D407/14 , C07D417/14 , C07D521/00
CPC分类号： C07D303/22 , A61K31/335 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/14 , C07D407/14 , C07D417/14
摘要： The present invention is related to a compound of the formula ##STR1## wherein R.sup.1 is a 2-methyl-1-propenyl or isobutyl group which may be substituted and R.sup.2 is (1) a substituted alkanoyl group, (2) a substituted aroyl group having at least one substituent selected from the group consisting of C.sub.2-6 alkyl, amino, halogen, hydroxyl, lower alkoxy, cyano, carbamoyl and carboxyl, (3) an aromatic heterocycle-carbonyl, which may optionally be substituted, (4) a carbamoyl group, which may optionally be substituted, (5) an alkyl group, which may optionally be substituted, (6) a benzenesulfonyl group, which may optionally be substituted, (7) an alkylsulfonyl group, which may optionally be substituted, (8) a sulfamoyl group, which may optionally be substituted, (9) an alkoxycarbonyl group, which may optionally be substituted or (10) a phenoxycarbonyl group, which may optionally be substituted; or a salt thereof.The compound (I) has a strong angiogenesis inhibitory activity.
摘要翻译：本发明涉及下式化合物：其中R1是可被取代的2-甲基-1-丙烯基或异丁基，R2是（1）取代的烷酰基，（2）取代的芳酰基具有至少一个选自C 2-6烷基，氨基，卤素，羟基，低级烷氧基，氰基，氨基甲酰基和羧基的取代基的取代基，（3）可任意取代的芳族杂环羰基，（4）可任选被取代的（5）可任选被取代的烷基，（6）可任意被取代的苯磺酰基，（7）可任意被取代的烷基磺酰基，（8））可任选被取代的氨磺酰基，（9）可任选被取代的烷氧基羰基或可任选被取代的（10）苯氧基羰基; 或其盐。化合物（I）具有强的血管生成抑制活性。

3. 发明授权

US4675397A 1-sulfo-2-oxoazetidine derivatives and their production 失效
标题翻译： 1-磺基-2-氧代氮杂环丁烷衍生物及其制备
公开(公告)号：US4675397A
公开(公告)日：1987-06-23
申请号：US405592
申请日：1982-08-05
申请人： Taisuke Matsuo, deceased , Michihiko Ochiai , Shoji Kishimoto
发明人： Taisuke Matsuo, deceased , Michihiko Ochiai , Shoji Kishimoto
IPC分类号： C07D205/085 , C07D205/095 , C07D209/48 , C07D257/04 , C07D277/20 , C07D277/46 , C07D311/22 , C07D401/06 , C07D403/04 , C07D413/14 , C07D417/12 , C07D417/14 , C07D498/04 , C07F7/08 , C07F7/10 , C07F9/6558 , C07D205/08 , A61K31/425 , A61K31/395
CPC分类号： C07D209/48 , C07D205/085 , C07D205/095 , C07D257/04 , C07D277/46 , C07D277/587 , C07D311/22 , C07D401/06 , C07D403/04 , C07D413/14 , C07D417/12 , C07D417/14 , C07F7/0812 , C07F7/10 , C07F9/65583
摘要： Disclosed are compounds of the general formula: ##STR1## wherein R.sub.1 is amino, an acylated amino or a protected amino group, X is hydrogen or methoxy, and R' is hydrogen, R or R.sup.4 wherein R is an organic residue attached to the azetidine ring through a carbon atom therein and R.sub.4 is azido, a halogen, an amino group which may optionally be acylated or a group of the formula --OR.sub.5, ##STR2## or --S--S--R.sub.5 wherein R.sub.5 is an organic residue and n is 0, 1 or 2, and pharmaceutically acceptable salts and esters thereof.The compounds have antimicrobial and/or .beta.-lactamase-inhibitory activity and are of value as drugs for human beings and domesticated animals.
摘要翻译：公开了以下通式的化合物：其中R 1是氨基，酰化氨基或被保护的氨基，X是氢或甲氧基，R'是氢，R或R 4，其中R是与氮杂环丁烷连接的有机残基 R 4是叠氮基，卤素，可任选被酰化的氨基或式-OR5，或-SS-R5的基团，其中R5是有机残基且n是0， 1或2，及其药学上可接受的盐和酯。这些化合物具有抗微生物和/或β-内酰胺酶抑制活性，并且对于人类和驯养动物具有价值。

4. 发明授权

US4560508A 4-Cyano-2-azetidinones and production thereof 失效
标题翻译： 4-氰基-2-氮杂环丁酮及其制备
公开(公告)号：US4560508A
公开(公告)日：1985-12-24
申请号：US451323
申请日：1982-12-20
申请人： Taisuke Matsuo, deceased , Michihiko Ochiai , Shoji Kishimoto
发明人： Taisuke Matsuo, deceased , Michihiko Ochiai , Shoji Kishimoto
IPC分类号： C07D205/08 , C07D205/085 , C07D409/14 , C07D417/12 , C07F7/08 , C07F7/10 , A61K31/395 , C07D401/12 , C07D403/12
CPC分类号： C07D409/14 , C07D205/085 , C07D417/12 , C07F7/0812 , C07F7/10
摘要： 4-Cyano-2-azetidinone derivatives represented by the formula ##STR1## wherein R.sup.1 is an amino group which may be acylated or protected, X is a hydrogen atom or a methoxy group and W is a hydrogen atom or a sulfo group, and methods of producing the same, for example, as represented by ##STR2## wherein R.sup.2 is an acylated or protected amino group, Y is a halogen atom or a group having the formula --OCOR.sup.3, --SCOR.sup.3 or --S(O).sub.n --R.sup.3 (R.sup.3 being a hydrocarbyl group and n an integer 1 or 2), R.sup.4 is an amino group which may be acylated or protected and X is as defined above. Compounds [I] are useful as advantageous intermediates for the synthesis of optically active 4-substituted-2-azetidinone derivatives, and, when W=SO.sub.3 H, [I] are also useful as antimicrobial agents and as beta-lactamase inhibitors.
摘要翻译：由下式表示的4-氰基-2-氮杂环丁酮衍生物[Ⅰ]其中R1是可被酰化或保护的氨基，X是氢原子或甲氧基，W是氢原子或磺基和其制备方法，例如，由如下所示的方法，其中R 2是酰化或保护的氨基，Y是卤素原子或具有式-OCOR 3，-SCOR 3或 - S（O）n -R 3（R 3为烃基，n为整数1或2），R 4为可被酰化或保护的氨基，X如上述定义。化合物[I]可用作合成光学活性4-取代-2-氮杂环丁酮衍生物的有利中间体，并且当W = SO 3 H时，[I]也可用作抗微生物剂和β-内酰胺酶抑制剂。

5. 发明授权

US4550105A 1-Sulfo-2-oxoazetidine derivatives and their production 失效
标题翻译： 1-磺基-2-氧代氮杂环丁烷衍生物及其制备
公开(公告)号：US4550105A
公开(公告)日：1985-10-29
申请号：US326937
申请日：1981-12-03
申请人： Taisuke Matsuo , Shoji Kishimoto , Michihiko Ochiai
发明人： Taisuke Matsuo , Shoji Kishimoto , Michihiko Ochiai
IPC分类号： C07D205/08 , C07D205/085 , C07D205/095 , C07D209/48 , C07D257/04 , C07D277/46 , C07D401/06 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D495/04 , C07F7/08 , C07F7/10 , C07F9/6558 , A61K31/395
CPC分类号： C07D205/08 , C07D205/085 , C07D205/095 , C07D209/48 , C07D257/04 , C07D277/46 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D495/04 , C07F7/0812 , C07F7/10 , C07F9/65583
摘要： Disclosed are compounds of the general formula: ##STR1## wherein R.sub.1 is amino, an acylated amino or a protected amino group, X is hydrogen or methoxy, and R' is hydrogen, R or R.sup.4 wherein R is an organic residue attached to the azetidine ring through a carbon atom therein and R.sub.4 is azido, a halogen, an amino group which may optionally be acylated or a group of the formula --OR.sub.5, ##STR2## or --S--S--R.sub.5 wherein R.sub.5 is an organic residue and n is 0, 1 or 2, and pharmaceutically acceptable salts and esters thereof.The compounds have antimicrobial and/or .beta.-lactamase-inhibitory activity and are of value as drugs for human beings and domesticated animals.
摘要翻译：公开了以下通式的化合物：其中R 1是氨基，酰化氨基或被保护的氨基，X是氢或甲氧基，R'是氢，R或R 4，其中R是与氮杂环丁烷连接的有机残基 R 4是叠氮基，卤素，可任选被酰化的氨基或式-OR5，或-SS-R5的基团，其中R5是有机残基且n是0， 1或2，及其药学上可接受的盐和酯。这些化合物具有抗微生物和/或β-内酰胺酶抑制活性，并且对于人类和驯养动物具有价值。

6. 发明授权

US4355040A Hypotensive imidazole-5-acetic acid derivatives 失效
标题翻译：低血糖咪唑-5-乙酸衍生物
公开(公告)号：US4355040A
公开(公告)日：1982-10-19
申请号：US204357
申请日：1980-11-05
申请人： Yoshiyasu Furukawa , Shoji Kishimoto , Kohei Nishikawa
发明人： Yoshiyasu Furukawa , Shoji Kishimoto , Kohei Nishikawa
IPC分类号： A61K31/415 , A61K31/4164 , A61P9/12 , C07D233/64 , C07D233/68
CPC分类号： C07D233/68
摘要： Novel imidazole-5-acetic acid derivatives of the formula: ##STR1## wherein R.sup.1 is lower alkyl, cycloalkyl or, phenyl which may be substituted with one to three of halogen, nitro, amino, mono(lower alkyl)amino, di(lower alkyl)amino, lower alkyl, lower alkoxyl, benzyloxyl or/and hydroxyl; X.sup.1, X.sup.2 and X.sup.3 are each hydrogen, halogen, nitro, amino, lower alkyl, lower alkoxyl, benzyloxyl or hydroxyl; Y is halogen and R.sup.2 is hydrogen or lower alkyl; provided that X.sup.1 is halogen, lower alkyl, lower alkoxyl, benzyloxyl or hydroxyl when R.sup.1 is unsubstituted or substituted phenyl only with one halogen, di(lower alkyl)amino, lower alkyl or lower alkoxyl, and its salts have hypotensive activity.
摘要翻译：下式的新型咪唑-5-乙酸衍生物：其中R 1为低级烷基，环烷基或可被一至三个卤素，硝基，氨基，单（低级烷基）氨基，二（低级烷基）氨基，低级烷基，低级烷氧基，苄氧基或/和羟基; X 1，X 2和X 3各自为氢，卤素，硝基，氨基，低级烷基，低级烷氧基，苄氧基或羟基; Y是卤素，R 2是氢或低级烷基; 当R1为未取代的或低级烷氧基，苄氧基或羟基时，X1为卤素，二（低级烷基）氨基，低级烷基或低级烷氧基，其盐为低血压活性。

7. 发明授权

US5698586A Angiogenesis inhibitory agent 失效
标题翻译：血管生成抑制剂
公开(公告)号：US5698586A
公开(公告)日：1997-12-16
申请号：US917842
申请日：1992-07-21
申请人： Shoji Kishimoto , Takeshi Fujita , Tsuneo Kanamaru , Moses Judah Folkman , Donald Ingber
发明人： Shoji Kishimoto , Takeshi Fujita , Tsuneo Kanamaru , Moses Judah Folkman , Donald Ingber
IPC分类号： A61K31/335 , A61K31/336 , C07D303/22 , C07D303/28 , C07D405/14 , C07D407/14 , C07D417/14 , C07D521/00 , C07D407/08
CPC分类号： C07D303/22 , A61K31/335 , A61K31/336 , C07D231/12 , C07D233/56 , C07D249/08 , C07D303/28 , C07D405/14 , C07D407/14 , C07D417/14
摘要： O-substituted fumagillol derivatives and its salts have an angiogenesis inhibiting activity and are useful for prophylaxis and treatment of diseases induced by abnormally stimulated neovascularization.
摘要翻译： O-取代的烟曲霉醇衍生物及其盐具有血管生成抑制活性，可用于预防和治疗由异常刺激的新血管形成引起的疾病。

8. 发明授权

US4833134A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US4833134A
公开(公告)日：1989-05-23
申请号：US84882
申请日：1987-08-13
申请人： Shoji Kishimoto , Kiminori Tomimatsu , Michiyuki Sendai
发明人： Shoji Kishimoto , Kiminori Tomimatsu , Michiyuki Sendai
IPC分类号： A61K31/545 , C07D501/38 , C07D501/46
CPC分类号： C07D501/46
摘要： Cephem compounds of the formula: ##STR1## wherein Q stands for a nitrogen atom or CH, R.sup.1 stands for a hydrogen atom or an optionally substituted lower alkyl group, R.sup.2 stands for a hydrogen atom or a lower alkyl group, A stands for a sulfur atom or NH, and n denotes an integral number ranging from 2 to 4, or salts thereof, and processes for producing them. The compounds (I) or salts thereof show not only excellent antibacterial activities against a wide range of pathogenic bacteria from gram-positive to gram-negative ones, including a variety of strains isolated clinically but also hydrophilic properties, and therefore they are excellent antibiotic substances having desirable water-solubility when used as injections.
摘要翻译：下式的头孢烯化合物：其中Q代表氮原子或CH，R1代表氢原子或任选取代的低级烷基，R2代表氢原子或低级烷基 A表示硫原子或NH，n表示2〜4的整数，或其盐，及其制造方法。化合物（I）或其盐不仅具有针对从革兰氏阳性至革兰氏阴性菌的广泛病原菌的优良抗菌活性，包括临床分离的各种菌株，而且亲水性，因此它们是优异的抗生素物质当用作注射剂时具有所需的水溶性。

9. 发明授权

US4782147A 1-sulfo-2-oxoazetidine derivatives and their production 失效
标题翻译： 1-磺基-2-氧代氮杂环丁烷衍生物及其制备
公开(公告)号：US4782147A
公开(公告)日：1988-11-01
申请号：US499802
申请日：1983-05-31
申请人： Michihiko Ochiai , Shoji Kishimoto , Taisuke Matsuo, deceased
发明人： Michihiko Ochiai , Shoji Kishimoto , Taisuke Matsuo, deceased
IPC分类号： C07D205/08 , C07D205/085 , C07D205/095 , C07D209/48 , C07D257/04 , C07D277/20 , C07D277/46 , C07D311/22 , C07D401/06 , C07D403/04 , C07D413/14 , C07D417/12 , C07D417/14 , C07D498/04 , C07F7/08 , C07F7/10 , C07F9/6558 , A61K31/395 , A61K31/425
CPC分类号： C07D209/48 , C07D205/08 , C07D205/085 , C07D205/095 , C07D257/04 , C07D277/46 , C07D277/587 , C07D311/22 , C07D401/06 , C07D403/04 , C07D413/14 , C07D417/12 , C07D417/14 , C07F7/0812 , C07F7/10 , C07F9/65583
摘要： Disclosed are compounds of the general formula: ##STR1## wherein R.sub.1 is amino, an acylated amino or a protected amino group, X is hydrogen or methoxy, and R' is hydrogen, R or R.sup.4 wherein R is an organic residue attached to the azetidine ring through a carbon atom therein and R.sub.4 is azido, a halogen, an amino group which may optionally be acylated or a group of the formula ##STR2## wherein R.sub.5 is an organic residue and n is 0, 1 or 2, and pharmaceutically acceptable salts and esters thereof.The compounds have antimicrobial and/or .beta.-lactamase-inhibitory activity and are of value as drugs for human beings and domesticated animals.
摘要翻译：公开了以下通式的化合物：其中R 1是氨基，酰化氨基或被保护的氨基，X是氢或甲氧基，R'是氢，R或R 4，其中R是与氮杂环丁烷连接的有机残基 R 4为叠氮基，卤素，可任选被酰化的氨基或式为基团的基团，其中R 5为有机残基且n为0,1或2，以及药学上可接受的盐及其酯。这些化合物具有抗微生物和/或β-内酰胺酶抑制活性，并且对于人类和驯养动物具有价值。

10. 发明授权

US5288722A 6-amino-6-desoxyfumagillols, production and use thereof 失效
标题翻译： 6-氨基-6-脱氧脂肪酸，其生产和使用
公开(公告)号：US5288722A
公开(公告)日：1994-02-22
申请号：US762658
申请日：1991-09-19
申请人： Shoji Kishimoto , Shogo Marui , Takeshi Fujita
发明人： Shoji Kishimoto , Shogo Marui , Takeshi Fujita
IPC分类号： C07D303/36 , C07D405/04 , A61K31/40 , A61K31/335 , A61K31/445 , C07D303/02
CPC分类号： C07D405/04 , C07D303/36
摘要： The present invention relates to a compound of the formula: ##STR1## wherein R.sup.1 is 2-methyl-1-propenyl group or isobutyl group; R.sup.2 and R.sup.3 are each hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted acyl group or R.sup.2 and R.sup.3 may form a ring together with the adjacent nitrogen atom; and the bonding mark .about. represents an .alpha.-linkage or .beta.-linkage, or a salt thereof. The compound (I) of the present invention has, among others, angiogenesis inhibiting activity, cell-growth inhibiting activity and immune reaction inhibiting activity, thus being useful as medicines, etc.
摘要翻译：本发明涉及下式的化合物：其中R 1是2-甲基-1-丙烯基或异丁基; R2和R3各自为氢原子，任选取代的烃残基或任选取代的酰基，或者R 2和R 3可与相邻的氮原子一起形成环; 并且结合标记DIFFERENCE表示α连接或β连接或其盐。本发明的化合物（I）具有血管生成抑制活性，细胞生长抑制活性和免疫反应抑制活性，因此作为药物等有用。

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