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1. 发明授权

US4459407A 1-(4-Aminobenzyl)-2,3-dioxopiperazine derivatives and salts thereof 失效
标题翻译： 1-（4-氨基苄基）-2,3-二氧代哌嗪衍生物及其盐
公开(公告)号：US4459407A
公开(公告)日：1984-07-10
申请号：US345055
申请日：1982-02-02
申请人： Takako Hori , Chosaku Yoshida , Yasuo Kiba , Ryuko Takeno , Joji Nakano , Jun Nitta , Sumiko Kishimoto , Shohachi Murakami , Hisatsugu Tsuda , Isamu Saikawa
发明人： Takako Hori , Chosaku Yoshida , Yasuo Kiba , Ryuko Takeno , Joji Nakano , Jun Nitta , Sumiko Kishimoto , Shohachi Murakami , Hisatsugu Tsuda , Isamu Saikawa
IPC分类号： C07D241/08 , C07D403/10 , A61K31/495 , A61K31/505 , C07D403/12
CPC分类号： C07D241/08 , Y10S514/908
摘要： A 1-(4-aminobenzyl)-2,3-dioxopiperazine derivative represented by the formula: ##STR1## and a salt thereof have excellent carcinostatic activity but a low toxicity. Therefore, said compounds are useful as medicines and also as intermediates.
摘要翻译：由下式表示的1-（4-氨基苄基）-2,3-二氧代哌嗪衍生物及其盐具有优异的制癌活性，但毒性低。因此，所述化合物可用作药物，也可用作中间体。

2. 发明授权

US4436921A 1-(4-Aminobenzyl)-2,3-dioxopiperazine derivatives, acid addition salts thereof and process for producing same 失效
公开(公告)号：US4436921A
公开(公告)日：1984-03-13
申请号：US169457
申请日：1980-07-16
申请人： Takako Hori , Chosaku Yoshida , Yasuo Kiba , Ryuko Takeno , Joji Nakano , Jun Nitta , Sumiko Kishimoto , Shohachi Murakami , Hisatsugu Tsuda , Isamu Saikawa
发明人： Takako Hori , Chosaku Yoshida , Yasuo Kiba , Ryuko Takeno , Joji Nakano , Jun Nitta , Sumiko Kishimoto , Shohachi Murakami , Hisatsugu Tsuda , Isamu Saikawa
IPC分类号： A61K31/495 , A61P35/00 , C07D241/08 , C07D241/20 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/14 , C07D405/14 , C07D417/10 , C07D401/00
CPC分类号： C07D241/08
摘要： A 1-(4-aminobenzyl)-2,3-dioxopiperazine derivative represented by the formula: ##STR1## and an acid addition salt thereof have excellent carcinostatic activity but a low toxicity. Therefore, said compounds are useful as medicines and also as intermediates.

3. 发明授权

US06166068A Immunomodulator, cell adhesion inhibitor, and agent for treating, and preventing autoimmune diseases 有权
标题翻译：免疫调节剂，细胞粘附抑制剂和治疗和预防自身免疫疾病的药剂
公开(公告)号：US06166068A
公开(公告)日：2000-12-26
申请号：US346932
申请日：1999-07-02
申请人： Keiichi Tanaka , Shinji Makino , Ichiro Oshio , Tomoya Shimotori , Yukihiko Aikawa , Takihiro Inaba , Chosaku Yoshida , Shuntaro Takano , Yoichi Taniguchi
发明人： Keiichi Tanaka , Shinji Makino , Ichiro Oshio , Tomoya Shimotori , Yukihiko Aikawa , Takihiro Inaba , Chosaku Yoshida , Shuntaro Takano , Yoichi Taniguchi
IPC分类号： C07D311/22 , C07D311/24 , C07D311/26 , A61K31/35 , A61K31/38 , A61K31/40
CPC分类号： C07D311/26 , C07D311/22 , C07D311/24
摘要： Autoimmune diseases, cell adhesion inhibition and immunomodulation are treated or effected by a method, comprising, treating a patient with a therapeutically effective amount of a 4H-1-benzopyran-4-one compound represented by the following formula or a salt thereof: ##STR1## wherein R.sup.1 is an unsubstituted or halogen-substituted alkyl, alkenyl or aryl group; R.sup.2 is a hydrogen atom or an alkyl or acyl group; R.sup.3 is a hydrogen or halogen atom or a cyano, azido, carboxyl, hydroxyl, formyl or alkoxycarbonyl group or a substituted or unsubstituted alkyl, alkoxy, phenoxy, cycloalkyl, carbamoyl, amino or phenyl group; R.sup.4 is a hydrogen or halogen atom, a nitro, cyano, carboxyl, acyl, hydroxyl or alkoxycarbonyl group, or a substituted or unsubstituted alkyl, alkoxy, alkylthio, phenylthio, alkynyl, alkenyl, sulfamoyl, alkanesulfonyl, alkanesulfonyl, amidino, phenyl or heterocyclic group or a group of the formula ##STR2## where R.sup.6 is a hydrogen atom, a hydroxyl, cyano or alkoxycarbonyl group or a substituted or unsubstituted alkyl, cycloalkyl, phenyl, amino, acyl, carbamoyl, alkanesulfonyl, iminomethyl or amidino group and R.sup.7 is a hydrogen atom or a substituted or unsubstituted alkyl, alkoxy, phenyl, cycloalkyl or heterocyclic group, or R.sup.6 and R.sup.7, when taken together with the nitrogen atom to which the two are bonded, form a 3- to 7-membered, substituted or unsubstituted heterocyclic group; R.sup.5 is a substituted or unsubstituted phenyl, thienyl, furyl or pyridyl group; Z is an oxygen or sulfur atom or an imino group; and the broken line means a single or double bond.
摘要翻译：自身免疫疾病，细胞粘附抑制和免疫调节通过包括用治疗有效量的下式表示的4H-1-苯并吡喃-4-酮化合物或其盐治疗患者的方法进行治疗或实现：其中R1 是未取代的或卤素取代的烷基，烯基或芳基; R2是氢原子或烷基或酰基; R3是氢或卤原子或氰基，叠氮基，羧基，羟基，甲酰基或烷氧基羰基或取代或未取代的烷基，烷氧基，苯氧基，环烷基，氨基甲酰基，氨基或苯基; R4是氢或卤原子，硝基，氰基，羧基，酰基，羟基或烷氧基羰基，或取代或未取代的烷基，烷氧基，烷硫基，苯硫基，炔基，烯基，氨磺酰基，烷磺酰基，烷磺酰基，脒基，苯基或杂环基团或下式的基团，其中R 6是氢原子，羟基，氰基或烷氧基羰基或取代或未取代的烷基，环烷基，苯基，氨基，酰基，氨基甲酰基，烷磺酰基，亚氨基甲基或脒基，R7是氢原子或取代或未取代的烷基，烷氧基，苯基，环烷基或杂环基，或R6和R7与两个键合的氮原子一起形成3-至7-元，取代或未取代的杂环基; R5是取代或未取代的苯基，噻吩基，呋喃基或吡啶基; Z是氧或硫原子或亚氨基; 虚线表示单键或双键。

4. 发明授权

US5922755A Immunomodulator, cell adhesion inhibtor, and agent for treating, and preventing autoimmune diseases 失效
标题翻译：免疫调节剂，细胞粘附抑制剂和治疗和预防自身免疫疾病的药物
公开(公告)号：US5922755A
公开(公告)日：1999-07-13
申请号：US530177
申请日：1996-05-06
申请人： Keiichi Tanaka , Shinji Makino , Ichiro Oshio , Tomoya Shimotori , Yukihiko Aikawa , Takihiro Inaba , Chosaku Yoshida , Shuntaro Takano , Yoichi Taniguchi
发明人： Keiichi Tanaka , Shinji Makino , Ichiro Oshio , Tomoya Shimotori , Yukihiko Aikawa , Takihiro Inaba , Chosaku Yoshida , Shuntaro Takano , Yoichi Taniguchi
IPC分类号： C07D311/22 , C07D311/24 , C07D311/26 , A61K31/35 , A61K31/415 , A61K31/42 , A61K31/535
CPC分类号： C07D311/26 , C07D311/22 , C07D311/24
摘要： A 4H-1-benzopyran-4-one derivative of the general formura �1!, ##STR1## or a salt thereof exerts excellent effects on immunomodulation and cell adhesion inhibition, and is further expected to have the effect of relieving autoimmune diseases at a level comparable to that of steroids. Thus, the compound of the general formula �1! is useful in the teatment and prevention of autoimmune diseases fundamentally caused by immunopathy or unusually accelerated cell adhesion, for example, chronic rheumatoid arthritis, systemic lupus erythematosus, scleroderma, mixed connective tissue disease,polyarteritis nodosa, polymyositis/dermatomyositis, Sjogren's syndrome, Behcet's disease, multiple sclerosis, autoimmune diabetes, Hashimoto's disease, psoriasis, primary myxedema, pernicious anemia, serious adynamia, ulcerative colitis, chronic active hepatitis, autoimmune hemolytic anemia idiopathic thrombocytopenic purpura and the like.
摘要翻译： PCT No.PCT / JP94 / 00585 Sec。 371日期：1996年5月6日 102（e）日期1996年5月6日PCT 1994年4月7日PCT PCT。第WO94 / 23714号公报日期：1994年10月27日一般形式的[1]的4H-1-苯并吡喃-4-酮衍生物或其盐对免疫调节和细胞粘附抑制作用效果优异，进一步预期具有缓解自身免疫性疾病的作用在类似于类固醇的水平。因此，通式[1]的化合物可用于免疫疾病或异常加速的细胞粘附，例如慢性类风湿性关节炎，系统性红斑狼疮，硬皮病，混合性结缔组织病，多发性动脉炎结节性多发性肌炎/皮肌炎，Sj + E，uml o + EE格伦综合征，贝切特氏病，多发性硬化症，自身免疫性糖尿病，桥本氏病，牛皮癣，原发性粘液性水肿，恶性贫血，严重adynamia，溃疡性结肠炎，慢性活动性肝炎，自身免疫性溶血性贫血特发性血小板减少性紫癜等。

5. 发明授权

US4954518A 4H-1-benzopyran-4-one derivative or its salt, process for producing the same and pharmaceutical composition comprising the same as active ingredient 失效
标题翻译： 4H-1-苯并吡喃-4-酮衍生物或其盐，其制备方法和包含其作为活性成分的药物组合物
公开(公告)号：US4954518A
公开(公告)日：1990-09-04
申请号：US255121
申请日：1988-10-07
申请人： Shuntaro Takano , Chosaku Yoshida , Takihiro Inaba , Keiichi Tanaka , Ryuko Takeno , Hideyoshi Nagaki , Tomoya Shimotori , Shinji Makino
发明人： Shuntaro Takano , Chosaku Yoshida , Takihiro Inaba , Keiichi Tanaka , Ryuko Takeno , Hideyoshi Nagaki , Tomoya Shimotori , Shinji Makino
IPC分类号： C07D213/70 , A61K31/34 , A61K31/35 , A61K31/352 , A61K31/38 , A61K31/40 , A61K31/4025 , A61K31/41 , A61K31/425 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/443 , A61K31/4433 , A61K31/445 , A61P29/00 , C07C311/08 , C07D20060101 , C07D213/62 , C07D213/74 , C07D257/04 , C07D295/12 , C07D295/18 , C07D311/22 , C07D311/24 , C07D311/26 , C07D311/30 , C07D311/36 , C07D311/42 , C07D311/54 , C07D311/56 , C07D311/58 , C07D333/30 , C07D405/00 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D417/04
CPC分类号： C07D405/04 , C07D311/22 , C07D311/24 , C07D311/30 , C07D311/36 , C07D311/54 , C07D311/56 , C07D405/12 , C07D409/12 , C07D417/04
摘要： This invention relates to a 4H-1-benzopyran-4-one derivative represented by the formula: ##STR1## or a salt thereof, a process for producing the same and a pharmaceutical composition comprising the same as active ingredient.
摘要翻译：本发明涉及由下式表示的4H-1-苯并吡喃-4-酮衍生物或其盐，其制备方法和含有该活性成分的药物组合物。

6. 发明授权

US4477664A Novel 1-(4-piperidiniobenzyl)-2,3-dioxopiperazine derivatives or acid addition salts thereof 失效
标题翻译：新型1-（4-哌啶基）苄基）-2,3-二氧代哌嗪衍生物或其酸加成盐
公开(公告)号：US4477664A
公开(公告)日：1984-10-16
申请号：US351256
申请日：1982-02-22
申请人： Takako Hori , Chosaku Yoshida , Yasuo Kiba , Ryuko Takeno , Joji Nakano , Jun Nitta , Sumiko Kishimoto , Shohachi Murakami , Hisatsugu Tsuda , Isamu Saikawa
发明人： Takako Hori , Chosaku Yoshida , Yasuo Kiba , Ryuko Takeno , Joji Nakano , Jun Nitta , Sumiko Kishimoto , Shohachi Murakami , Hisatsugu Tsuda , Isamu Saikawa
IPC分类号： A61K31/495 , A61P35/00 , C07D241/08 , C07D241/20 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/14 , C07D405/14 , C07D417/10 , C07D241/02
CPC分类号： C07D241/08
摘要： A 1-(4-aminobenzyl)-2,3-dioxopiperazine derivative represented by the formula: ##STR1## and an acid addition salt thereof have excellent carcinostatic activity but a low toxicity. Therefore, said compounds are useful as medicines and also as intermediates.
摘要翻译：由下式表示的1-（4-氨基苄基）-2,3-二氧代哌嗪衍生物及其酸加成盐具有优异的制癌活性，但毒性低。因此，所述化合物可用作药物，也可用作中间体。

7. 发明授权

US4448963A 4-[4-(Thiazolyl-amino)benzyl]-2,3-dioxopiperazine derivatives, acid addition salts thereof and process for producing same 失效
标题翻译： 4- [4-（噻唑基 - 氨基）苄基] -2,3-二氧代哌嗪衍生物及其酸加成盐及其制备方法
公开(公告)号：US4448963A
公开(公告)日：1984-05-15
申请号：US351257
申请日：1982-02-22
申请人： Takako Hori , Chosaku Yoshida , Yasuo Kiba , Ryuko Takeno , Joji Nakano , Jun Nitta , Sumiko Kishimoto , Shohachi Murakami , Hisatsugu Tsuda , Isamu Saikawa
发明人： Takako Hori , Chosaku Yoshida , Yasuo Kiba , Ryuko Takeno , Joji Nakano , Jun Nitta , Sumiko Kishimoto , Shohachi Murakami , Hisatsugu Tsuda , Isamu Saikawa
IPC分类号： A61K31/495 , A61P35/00 , C07D241/08 , C07D241/20 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/14 , C07D405/14 , C07D417/10 , C07D241/06 , A61K31/41
CPC分类号： C07D241/08
摘要： A 1-(4-aminobenzyl)-2,3-dioxopiperazine derivative represented by the formula: ##STR1## and an acid addition salt thereof have excellent carcinostatic activity but a low toxicity. Therefore, said compounds are useful as medicines and also as intermediates.
摘要翻译：由下式表示的1-（4-氨基苄基）-2,3-二氧代哌嗪衍生物及其酸加成盐具有优异的制癌活性，但毒性低。因此，所述化合物可用作药物，也可用作中间体。

8. 发明授权

US4112090A Novel penicillins and cephalosporins and process for producing the same 失效
标题翻译：新型青霉素和头孢菌素及其制备方法
公开(公告)号：US4112090A
公开(公告)日：1978-09-05
申请号：US654060
申请日：1976-01-30
申请人： Isamu Saikawa , Shuntaro Takano , Chosaku Yoshida , Okuta Takashima , Kaishu Momonoi , Seietsu Kuroda , Miwako Komatsu , Takashi Yasuda , Yutaka Kodama
发明人： Isamu Saikawa , Shuntaro Takano , Chosaku Yoshida , Okuta Takashima , Kaishu Momonoi , Seietsu Kuroda , Miwako Komatsu , Takashi Yasuda , Yutaka Kodama
IPC分类号： C07D499/00 , C07D499/64 , C07D501/20 , A61K31/43 , C07D499/66 , C07D499/68 , C07D499/70
CPC分类号： C07D499/00
摘要： Novel penicillins and cephalosporins and non-toxic salts thereof, which contain a mono- or di-oxo- or thioxo-piperazino(thio)carbonylamino group have been prepared. These compounds are valuable antibacterial compounds for use in mammals including man. A process for the preparation of the compounds has also been discovered.
摘要翻译：已经制备了含有单 - 或二 - 氧代或硫代 - 哌嗪子基（硫代）羰基氨基的新型青霉素和头孢菌素及其无毒盐。这些化合物是用于包括人在内的哺乳动物的有价值的抗菌化合物。还已经发现了制备化合物的方法。

9. 发明授权

US4087424A Novel penicillins and cephalosporins and process for producing the same 失效
标题翻译：新型青霉素和头孢菌素及其制备方法
公开(公告)号：US4087424A
公开(公告)日：1978-05-02
申请号：US571479
申请日：1975-04-24
申请人： Isamu Saikawa , Shuntaro Takano , Chosaku Yoshida , Okuta Takashima , Kaishu Momonoi , Seietsu Kuroda , Miwako Komatsu , Takashi Yasuda , Yutaka Kodama
发明人： Isamu Saikawa , Shuntaro Takano , Chosaku Yoshida , Okuta Takashima , Kaishu Momonoi , Seietsu Kuroda , Miwako Komatsu , Takashi Yasuda , Yutaka Kodama
IPC分类号： C07D241/08 , C07D499/00 , C07D499/46 , C07D499/64 , C07D501/20 , C07D501/24
CPC分类号： C07D499/00 , C07D241/08
摘要： Novel penicillins and cephalosporins and non-toxic salts thereof, which contain a mono- or di-oxo- or thioxo-piperazino(thio)carbonylamino group in molecule. These compounds are valuable antibacterial compounds for use in mammals including man. This disclosure relates to such compounds and a process for the preparation thereof.
摘要翻译：新型青霉素和头孢菌素及其无毒盐，其在分子中含有一个或二个氧代或二硫代哌嗪子基（硫代）羰基氨基。这些化合物是用于包括人在内的哺乳动物的有价值的抗菌化合物。本公开涉及这些化合物及其制备方法。

10. 发明授权

US4460774A 1-(4-Aminobenzyl)-2,3-dioxopiperazine derivatives, acid addition salts thereof and process for producing same 失效
标题翻译： 1-（4-氨基苄基）-2,3-二氧代哌嗪衍生物及其酸加成盐及其制备方法
公开(公告)号：US4460774A
公开(公告)日：1984-07-17
申请号：US348271
申请日：1982-02-12
申请人： Takako Hori , Chosaku Yoshida , Yasuo Kiba , Ryuko Takeno , Joji Nakano , Jun Nitta , Sumiko Kishimoto , Shohachi Murakami , Hisatsugu Tsuda , Isamu Saikawa
发明人： Takako Hori , Chosaku Yoshida , Yasuo Kiba , Ryuko Takeno , Joji Nakano , Jun Nitta , Sumiko Kishimoto , Shohachi Murakami , Hisatsugu Tsuda , Isamu Saikawa
IPC分类号： A61K31/495 , A61P35/00 , C07D241/08 , C07D241/20 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/14 , C07D405/14 , C07D417/10 , C07D403/12
CPC分类号： C07D241/08
摘要： A 1-(4-aminobenzyl)-2,3-dioxopiperazine derivative represented by the formula: ##STR1## and an acid addition salt thereof have excellent carcinostatic activity but a low toxicity. Therefore, said compounds are useful as medicines and also as intermediates.
摘要翻译：由下式表示的1-（4-氨基苄基）-2,3-二氧代哌嗪衍生物及其酸加成盐具有优异的制癌活性，但毒性低。因此，所述化合物可用作药物，也可用作中间体。

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