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

US6005098A 5'deoxycytidine derivatives 失效
标题翻译： 5'-脱氧胞苷衍生物
公开(公告)号：US6005098A
公开(公告)日：1999-12-21
申请号：US234200
申请日：1999-01-20
申请人： Kazuo Hattori , Tohru Ishikawa , Hideo Ishitsuka , Yasunori Kohchi , Nobuhiro Oikawa , Nobuo Shimma , Hitomi Suda
发明人： Kazuo Hattori , Tohru Ishikawa , Hideo Ishitsuka , Yasunori Kohchi , Nobuhiro Oikawa , Nobuo Shimma , Hitomi Suda
IPC分类号： C07H19/06 , A61K31/513 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61P35/00 , A61P43/00 , C07H19/067 , C07H19/16 , C07H19/167
CPC分类号： C07H19/16
摘要： Compounds of the formula (I) ##STR1## wherein R.sup.1 is each independently hydrogen or a group easily hydrolyzable under physiological conditions;R.sup.2 is --(CH.sub.2).sub.n -cycloalkyl wherein cycloalkyl contains 3 to 5 carbon atoms and n is an integer from 0 to 4, heteroaryl-(lower-alkyl), (lower-alkoxy)-(lower-alkyl), aryloxy-(lower-alkyl), aralkyloxy-(lower-alkyl), (lower-alkylthio)-(lower-alkyl), arylthio-(lower-alkyl), aralkylthio-(lower-alkyl), oxo-(lower-alkyl), acylamino-(lower-alkyl), cyclic amino-(lower-alkyl), (2-oxocyclic amino)-(lower-alkyl) wherein the alkylene chain is unsubstituted or substituted with one or two lower-alkyl group(s); andR.sup.3 is iodo, or a vinyl or ethynyl group which group is unsubstituted or substituted by one or more substituents selected from the group consisting of halogen, C.sub.1-4 alkyl, cycloalkyl, aralkyl, carbocyclic aromatic ring and heteorcyclic aromatic ring.The compounds of formula I are useful in the treatment of malignant diseases and can also be administered together with 5-fluorouracil or derivatives thereof to enhance the antitumour activity of the latter.
摘要翻译：式（I）的化合物，其中R 1各自独立地为氢或在生理条件下易于水解的基团; R 2为 - （CH 2）n - 环烷基，其中环烷基含有3至5个碳原子，n为0至4的整数，杂芳基 - （低级 - 烷基），（低级 - 烷氧基） - （低级 - 烷基），芳氧基 - （低级烷基），芳烷氧基 - （低级烷基），（低级 - 烷硫基） - （低级 - 烷基），芳硫基 - （低级烷基），芳烷硫基 - （低级烷基），氧代（低级烷基） - （低级烷基），环状氨基 - （低级 - 烷基），（2-氧代环氨基） - （低级烷基），其中亚烷基链未被取代或被一个或两个低级烷基取代; 或R 3为碘，或乙烯基或乙炔基，该基团是未取代的或被一个或多个选自卤素，C 1-4烷基，环烷基，芳烷基，碳环芳环和杂环芳环的取代基取代。式I化合物可用于治疗恶性疾病，也可与5-氟尿嘧啶或其衍生物一起施用以增强后者的抗肿瘤活性。

2. 发明授权

US06211166B1 5′-deoxy-cytidine derivative administration to treat solid tumors 有权
标题翻译： 5'-脱氧胞苷衍生物给药治疗实体瘤
公开(公告)号：US06211166B1
公开(公告)日：2001-04-03
申请号：US09534156
申请日：2000-03-24
申请人： Kazuo Hattori , Tohru Ishikawa , Hideo Ishitsuka , Yasunori Kohchi , Nobuhiro Oikawa , Nobuo Shimma , Hitomi Suda
发明人： Kazuo Hattori , Tohru Ishikawa , Hideo Ishitsuka , Yasunori Kohchi , Nobuhiro Oikawa , Nobuo Shimma , Hitomi Suda
IPC分类号： A01N4304
CPC分类号： C07H19/06 , Y02P20/55
摘要： Novel 5′-deoxy-cytidine derivatives represented by the general formula (I) wherein R1 is a hydrogen atom or a group easily hydrolyzable under physiological conditions; R2 is a hydrogen atom, or —CO—OR4 group [wherein R4 is a saturated or unsaturated, straight or branched hydrocarbon group consisting of one to fifteen carbon atoms, or a group of the formula —(CH2)n—Y (in which Y is cyclohexyl or phenyl; n is an integer from 0 to 4)]; R3 is a hydrogen atom, bromo, iodo, cyano, a C1-4 alkyl group [which may be substituted with halogen atom(s)], a vinyl or ethynyl group [which may be substituted with halogen atom(s), C1-4 alkyl, cycloalkyl, aralkyl, or aromatic ring which may have one or more hetero atom(s)], or an aralkyl group which may be substituted for use in medical therapy, especially tumor therapy.
摘要翻译：由通式（I）表示的新型5'-脱氧胞苷衍生物，其中R1是氢原子或在生理条件下容易水解的基团; R2是氢原子或-CO-OR4基团[其中R4是由1-15个碳原子组成的饱和或不饱和的直链或支链烃基，或式 - （CH2）nY（其中Y是环己基或苯基; n为0至4的整数）]; R3是氢原子，溴，碘，氰基，C1-4烷基[可以被卤素原子取代]，乙烯基或乙炔基[可以被卤原子取代，C1- 4烷基，环烷基，芳烷基或可能具有一个或多个杂原子的芳环]或可用于药物治疗，特别是肿瘤治疗的芳烷基。

3. 发明授权

US6114520A 5'-deoxy-cytidine derivatives 有权
标题翻译： 5'-脱氧胞苷衍生物
公开(公告)号：US6114520A
公开(公告)日：2000-09-05
申请号：US484174
申请日：2000-01-14
申请人： Kazuo Hattori , Tohru Ishikawa , Hideo Ishitsuka , Yasunori Kohchi , Nobuhiro Oikawa , Nobuo Shimma , Hitomi Suda
发明人： Kazuo Hattori , Tohru Ishikawa , Hideo Ishitsuka , Yasunori Kohchi , Nobuhiro Oikawa , Nobuo Shimma , Hitomi Suda
IPC分类号： C07H19/067 , A01N43/04 , A61K31/505 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61P35/00 , A61P43/00 , C07D239/553 , C07H19/06
CPC分类号： C07H19/06 , Y02P20/55
摘要： Novel 5'-deoxy-cytidine derivatives represented by the general formula (I) ##STR1## wherein R.sup.1 is a hydrogen atom or a group easily hydrolyzable under physiological conditions; R.sup.2 is a hydrogen atom, or --CO--OR.sup.4 group [wherein R.sup.4 is a saturated or unsaturated, straight or branched hydrocarbon group consisting of one to fifteen carbon atoms, or a group of the formula --(CH.sub.2).sub.n --Y (in which Y is cyclohexyl or phenyl; n is an integer from 0 to 4)]; R.sup.3 is a hydrogen atom, bromo, iodo, cyano, a C.sub.1-4 alkyl group [which may be substituted with halogen atom(s)], a vinyl or ethynyl group [which may be substituted with halogen atom(s), C.sub.1-4 alkyl, cycloalkyl, aralkyl, or aromatic ring which may have one or more hetero atom(s)], or an aralkyl group which may be substituted for use in medical therapy, especially tumor therapy.
摘要翻译：由通式（I）表示的新型5'-脱氧胞苷衍生物，其中R1是氢原子或在生理条件下容易水解的基团; R2是氢原子或-CO-OR4基团[其中R4是由1-15个碳原子组成的饱和或不饱和的直链或支链烃基，或式 - （CH2）nY（其中Y是环己基或苯基; n为0至4的整数）]; R3是氢原子，溴，碘，氰基，C1-4烷基[可以被卤素原子取代]，乙烯基或乙炔基[可以被卤原子取代，C1- 4烷基，环烷基，芳烷基或可能具有一个或多个杂原子的芳环]或可用于药物治疗，特别是肿瘤治疗的芳烷基。

4. 发明授权

US08084645B2 4-phenylamino-benzaldoxime derivatives and uses thereof as mitogen-activated protein kinase kinase (MEK) inhibitors 失效
标题翻译： 4-苯基氨基 - 苯甲醛肟衍生物及其作为丝裂原活化蛋白激酶激酶（MEK）抑制剂的用途
公开(公告)号：US08084645B2
公开(公告)日：2011-12-27
申请号：US10572255
申请日：2004-09-16
申请人： Yoshiaki Isshiki , Yasunori Kohchi , Kazuo Hattori , Nobuo Shimma , Masanori Miwa , Naohito Inagaki , Hitoshi Iikura , Yasuaki Matsubara
发明人： Yoshiaki Isshiki , Yasunori Kohchi , Kazuo Hattori , Nobuo Shimma , Masanori Miwa , Naohito Inagaki , Hitoshi Iikura , Yasuaki Matsubara
IPC分类号： C07C239/00 , C07C259/00 , C07C229/00 , C07D265/00 , A01N37/18 , A61K31/16
CPC分类号： C07D207/08 , A61K31/166 , C07C259/10 , C07C311/04 , C07C317/18 , C07C323/12 , C07C2601/02 , C07D207/27 , C07D211/46 , C07D213/30 , C07D233/32 , C07D233/64 , C07D263/32 , C07D295/088 , C07D295/155 , C07F7/1804
摘要： A compound of the present invention, or a pharmaceutically acceptable salt thereof is indicated by formula (1) below: wherein, R1, R2, R3, R4, R5, R6, Q, R8, and R9 have the same meanings as R1, R2, R3, R4, R5, R6, Q, R8, and R9 in the specification.
摘要翻译：本发明化合物或其药学上可接受的盐由下式（1）表示：其中，R 1，R 2，R 3，R 4，R 5，R 6，Q，R 8和R 9具有与R 1，R 2，，R3，R4，R5，R6，Q，R8和R9。

5. 发明申请

US20070105859A1 4-Phenylamino-benzaldoxime derivatives and uses thereof as mitogen-activated protein kinase kinase (mek) inhibitors 失效
标题翻译： 4-苯基氨基 - 苯甲醛肟衍生物及其作为丝裂原活化蛋白激酶激酶（mek）抑制剂的用途
公开(公告)号：US20070105859A1
公开(公告)日：2007-05-10
申请号：US10572255
申请日：2004-09-16
申请人： Yoshiaki Isshiki , Yasunori Kohchi , Kazuo Hattori , Nobuo Shimma , Masanori Miwa , Naohito Inagaki , Hitoshi IIkura , Yasuaki Matsubara
发明人： Yoshiaki Isshiki , Yasunori Kohchi , Kazuo Hattori , Nobuo Shimma , Masanori Miwa , Naohito Inagaki , Hitoshi IIkura , Yasuaki Matsubara
IPC分类号： A61K31/5375 , A61K31/495 , A61K31/445 , A61K31/44 , A61K31/4172 , A61K31/40 , A61K31/215
CPC分类号： C07D207/08 , A61K31/166 , C07C259/10 , C07C311/04 , C07C317/18 , C07C323/12 , C07C2601/02 , C07D207/27 , C07D211/46 , C07D213/30 , C07D233/32 , C07D233/64 , C07D263/32 , C07D295/088 , C07D295/155 , C07F7/1804
摘要： A compound of the present invention, or a pharmaceutically acceptable salt thereof is indicated by formula (1) below: wherein, R1, R2, R3, R4, R5, R6, Q, R8, and R9 have the same meanings as R1, R2, R3, R4, R5, R6, Q, R8, and R9 in the specification.
摘要翻译：本发明的化合物或其药学上可接受的盐由下式（1）表示：其中R 1，R 2，R 3， R SUP，R 4，R 5，R 6，Q，R 8和R 4 > 9 具有与R 1，R 2，R 3，R 4，R 4， R 5，R 6，R 6，R 8，R 9和R 9中的至少一个。

6. 发明授权

US07745663B2 5-Substituted-2-phenylamino benzamides as MEK inhibitors 有权
标题翻译： 5-取代的2-苯基氨基苯甲酰胺作为MEK抑制剂
公开(公告)号：US07745663B2
公开(公告)日：2010-06-29
申请号：US11658533
申请日：2005-07-26
申请人： Yoshiaki Isshiki , Yasunori Kohchi , Eisaku Mizuguchi , Hitoshi Iikura , Yasuaki Matsubara , Shinji Tsujii , Nobuo Shimma , Masanori Miwa , Satoshi Aida , Masami Kohchi , Takeshi Murata , Kosuke Aso
发明人： Yoshiaki Isshiki , Yasunori Kohchi , Eisaku Mizuguchi , Hitoshi Iikura , Yasuaki Matsubara , Shinji Tsujii , Nobuo Shimma , Masanori Miwa , Satoshi Aida , Masami Kohchi , Takeshi Murata , Kosuke Aso
IPC分类号： C07C239/00 , C07C259/00 , C07C233/00 , C07C235/00 , C07C237/00 , C07C229/00 , C07C251/00 , C07D265/00 , A61K31/535 , A01N37/18 , A61K31/16 , A61K31/165
CPC分类号： C07C259/10 , C07C317/18 , C07C323/12 , C07D207/27 , C07D211/76 , C07D239/10 , C07D261/04 , C07D263/22 , C07D265/02 , C07D265/32 , C07D273/00
摘要： An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases.The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].
摘要翻译：本发明的目的是提供具有强MEK抑制活性并且在体内稳定且可溶于水的化合物，其可用作增殖性疾病的预防或治疗剂。本发明的化合物及其药学上可接受的盐由下式（1）表示：[其中R1，R2，R3，R4和X与本专利申请中定义相同]。

7. 发明授权

US08575391B2 5-substituted-2-phenylamino benzamides as MEK inhibitors 有权
标题翻译： 5-取代-2-苯基氨基苯甲酰胺作为MEK抑制剂
公开(公告)号：US08575391B2
公开(公告)日：2013-11-05
申请号：US12752396
申请日：2010-04-01
申请人： Yoshiaki Isshiki , Yasunori Kohchi , Eisaku Mizuguchi , Hitoshi Iikura , Yasuaki Matsubara , Shinji Tsujii , Nobuo Shimma , Masanori Miwa , Satoshi Aida , Masami Kohchi , Takeshi Murata , Kosuke Aso
发明人： Yoshiaki Isshiki , Yasunori Kohchi , Eisaku Mizuguchi , Hitoshi Iikura , Yasuaki Matsubara , Shinji Tsujii , Nobuo Shimma , Masanori Miwa , Satoshi Aida , Masami Kohchi , Takeshi Murata , Kosuke Aso
IPC分类号： C07C239/00 , C07C259/00 , C07C233/00 , C07C235/00 , C07C237/00 , C07D265/00 , C07C229/00 , C07C251/00 , A61K31/535 , A01N37/18 , A61K31/16 , A61K31/165
CPC分类号： C07C259/10 , C07C317/18 , C07C323/12 , C07D207/27 , C07D211/76 , C07D239/10 , C07D261/04 , C07D263/22 , C07D265/02 , C07D265/32 , C07D273/00
摘要： An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases.The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].
摘要翻译：本发明的目的是提供具有强MEK抑制活性并且在体内稳定且可溶于水的化合物，其可用作增殖性疾病的预防或治疗剂。本发明的化合物及其药学上可接受的盐由下式（1）表示：[其中R1，R2，R3，R4和X与本专利申请中定义相同]。

8. 发明申请

US20090233915A1 5-Substituted-2-Phenylamino Benzamides as MEK Inhibitors 有权
标题翻译： 5-取代的2-苯基氨基苯甲酰胺作为MEK抑制剂
公开(公告)号：US20090233915A1
公开(公告)日：2009-09-17
申请号：US11658533
申请日：2005-07-26
申请人： Yoshiaki Isshiki , Yasunori Kohchi , Eisaku Mizuguchi , Hitoshi Iikura , Yasuaki Matsubara , Shinji Tsujii , Nobuo Shimma , Masanori Miwa , Satoshi Aida , Masami Kohchi , Takeshi Murata , Kosuke Aso
发明人： Yoshiaki Isshiki , Yasunori Kohchi , Eisaku Mizuguchi , Hitoshi Iikura , Yasuaki Matsubara , Shinji Tsujii , Nobuo Shimma , Masanori Miwa , Satoshi Aida , Masami Kohchi , Takeshi Murata , Kosuke Aso
IPC分类号： A61K31/535 , C07C233/64 , A61K31/166 , C07D265/02 , C07D261/04 , A61K31/42 , C07C229/58 , A61P35/00
CPC分类号： C07C259/10 , C07C317/18 , C07C323/12 , C07D207/27 , C07D211/76 , C07D239/10 , C07D261/04 , C07D263/22 , C07D265/02 , C07D265/32 , C07D273/00
摘要： An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases.The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].
摘要翻译：本发明的目的是提供具有强MEK抑制活性并且在体内稳定且可溶于水的化合物，其可用作增殖性疾病的预防或治疗剂。本发明的化合物及其药学上可接受的盐由下式（1）表示：[其中R1，R2，R3，R4和X与本专利申请中定义相同]。

9. 发明申请

US20100197676A1 5-Substituted-2-Phenylamino Benzamides as Mek Inhibitors 有权
标题翻译： 5-取代的2-苯基氨基苯甲酰胺作为Mek抑制剂
公开(公告)号：US20100197676A1
公开(公告)日：2010-08-05
申请号：US12752396
申请日：2010-04-01
申请人： Yoshiaki Isshiki , Yasunori Kohchi , Eisaku Mizuguchi , Hitoshi Iikura , Yasuaki Matsubara , Shinji Tsujii , Nobuo Shimma , Masanori Miwa , Satoshi Aida , Masami Kohchi , Takeshi Murata , Kosuke Aso
发明人： Yoshiaki Isshiki , Yasunori Kohchi , Eisaku Mizuguchi , Hitoshi Iikura , Yasuaki Matsubara , Shinji Tsujii , Nobuo Shimma , Masanori Miwa , Satoshi Aida , Masami Kohchi , Takeshi Murata , Kosuke Aso
IPC分类号： A61K31/539 , A61P19/02 , A61K31/16 , C07C259/00 , C07D209/32 , A61K31/4035 , C07D265/02 , A61K31/535 , C07D273/01
CPC分类号： C07C259/10 , C07C317/18 , C07C323/12 , C07D207/27 , C07D211/76 , C07D239/10 , C07D261/04 , C07D263/22 , C07D265/02 , C07D265/32 , C07D273/00
摘要： An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases.The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].
摘要翻译：本发明的目的是提供具有强MEK抑制活性并且在体内稳定且可溶于水的化合物，其可用作增殖性疾病的预防或治疗剂。本发明的化合物及其药学上可接受的盐由下式（1）表示：[其中R1，R2，R3，R4和X与本专利申请中定义相同]。

10. 发明授权

US08022247B2 Process for production of 2,3,4-trifluoro-5-(iodo or bromo)-benzoic acid 失效
标题翻译：制备2,3,4-三氟-5-（碘或溴） - 苯甲酸的方法
公开(公告)号：US08022247B2
公开(公告)日：2011-09-20
申请号：US11887843
申请日：2006-04-06
申请人： Hiroshi Koyano , Hitoshi Iikura , Yoshiaki Isshiki , Yasunori Kohchi
发明人： Hiroshi Koyano , Hitoshi Iikura , Yoshiaki Isshiki , Yasunori Kohchi
IPC分类号： C07C63/00
CPC分类号： C07C51/363 , C07C63/70
摘要： The invention provides a process for production of 2,3,4-trifluoro-5-(iodo or bromo)benzoic acid, the process comprising a halogenation step in which direct iodination or bromination of 2,3,4-trifluorobenzoic acid is performed with an iodinating agent or brominating agent in a reaction solvent in the presence of an oxidizing agent. According to the invention, there is provided a process for convenient production of 2,3,4-trifluoro-5-(iodo or bromo)benzoic acid in high yield and high purity in a highly regioselective manner.
摘要翻译：本发明提供了一种生产2,3,4-三氟-5-（碘或溴）苯甲酸的方法，该方法包括一个卤化步骤，其中对2,3,4-三氟苯甲酸进行直接碘化或溴化，碘化剂或溴化剂在反应溶剂中在氧化剂存在下进行。根据本发明，提供了以高度区域选择性方式以高产率和高纯度方便生产2,3,4-三氟-5-（碘或溴）苯甲酸的方法。

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