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1. 发明授权

US5616567A 2'-Cyano pyrimidine nucleoside compounds 失效
标题翻译： 2'-氰基嘧啶核苷化合物
公开(公告)号：US5616567A
公开(公告)日：1997-04-01
申请号：US301720
申请日：1994-09-07
申请人： Takuma Sasaki , Akira Matsuda , Tohru Ueda, deceased
发明人： Takuma Sasaki , Akira Matsuda , Tohru Ueda, deceased
IPC分类号： A61K31/505 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7135 , A61P35/00 , C07D405/04 , C07F7/18 , C07H19/06 , C07H19/067 , C07H19/16 , C07H23/00 , C07H19/09
CPC分类号： C07D405/04 , C07H19/06 , C07H23/00 , Y10S514/908
摘要： The pyrimidine compounds of the present invention are represented by the following formula: ##STR1## and pharmaceutically acceptable salts thereof, wherein, R.sup.1 represents a hydroxyl or an amino which may be substituted by an acyl group; R.sup.2 represents a hydrogen atom or an alkyl having 1 to 4 carbons; R.sup.3 represents a hydrogen or a hydroxyl; and R.sup.4 and R.sup.5 each represent a hydrogen or together form a group --R.sup.6 R.sup.7 Si--O--SiR.sup.6' R.sup.7' --, wherein R.sup.6, R.sup.7, R.sup.6' and R.sup.7' are the same or different from one another and each represent an alkyl having 1 to 4 carbons. The compounds of the present invention exhibit an excellent antitumor effect.
摘要翻译：本发明的嘧啶化合物由下式表示：其中R1表示羟基或可被酰基取代的氨基， ; R2表示氢原子或碳原子数1〜4的烷基， R3表示氢或羟基; 并且R 4和R 5各自表示氢或一起形成-R 6 R 7 Si-O-SiR 6'R 7'基团，其中R 6，R 7，R 6'和R 7'彼此相同或不同，并且各自表示具有1至 4个碳。本发明的化合物表现出优异的抗肿瘤效果。

2. 发明授权

US5811408A 2'-deoxy-2'-(substituted or unsubstituted)methylidene-4'-thionucleosides 失效
标题翻译： 2'-脱氧-2' - （取代或未取代的）亚甲基-4'-硫代核苷
公开(公告)号：US5811408A
公开(公告)日：1998-09-22
申请号：US765403
申请日：1997-02-21
申请人： Yuichi Yoshimura , Akira Matsuda , Shinji Miura , Takuma Sasaki , Hiroshi Satoh
发明人： Yuichi Yoshimura , Akira Matsuda , Shinji Miura , Takuma Sasaki , Hiroshi Satoh
IPC分类号： C07D409/04 , C07H19/04 , C07H19/207 , A61K31/70 , C07H19/10 , C07H19/173 , C07H19/73
CPC分类号： C07D409/04 , C07H19/04
摘要： The present invention relates to 2'-deoxy-2'-(substituted or unsubstituted)methylidene-4'-thionucleosides having excellent antitumor activity, represented by formula �I!: ##STR1## wherein B represents a pyrimidine or purine base, R.sub.1 and R.sub.2, which may be the same or different, represent hydrogen, a cyano group or alkyl group, and R.sub.3 represents hydrogen or a phosphoric acid residue, and a method for producing the same, and a use of the same.
摘要翻译： PCT No.PCT / JP95 / 01385 Sec。 371日期1997年2月21日 102（e）日期1997年2月21日PCT提交1995年7月12日PCT公布。出版物WO96 / 01834 日期：1996年1月25日本发明涉及由式[I]表示的具有优异抗肿瘤活性的2'-脱氧-2' - （取代或未取代）亚甲基-4'-硫代核苷酸：其中B表示嘧啶或嘌呤碱，R1和R2可以相同或不同，代表氢，氰基或烷基，R3代表氢或磷酸残基，及其制备方法，以及一样。

3. 发明授权

US5696097A Antineoplastic 5'-diacylglycerylphosphatidyl-2-deoxy-2'-methylenylcytidines and method of making 失效
标题翻译：抗肿瘤性5'-二酰基甘油基磷脂酰基-2-脱氧-2'-亚甲基胞苷及其制备方法
公开(公告)号：US5696097A
公开(公告)日：1997-12-09
申请号：US525606
申请日：1995-09-15
申请人： Akira Matsuda , Takuma Sasaki , Satoshi Shutou , Akihiro Fujii , Takashi Ono , Shinji Sakata , Takanori Miyashita
发明人： Akira Matsuda , Takuma Sasaki , Satoshi Shutou , Akihiro Fujii , Takashi Ono , Shinji Sakata , Takanori Miyashita
IPC分类号： C07H19/10 , A61K31/70 , C07H19/207
CPC分类号： C07H19/10
摘要： Novel 2'-methylidenenucleotide compounds of the formula (I) ##STR1## wherein R is a hydrogen or a halogen, R.sup.1 and R.sup.2 are the same or different and each is a fatty acid residue or a hydrocarbon residue, and R.sup.3 and R.sup.4 are the same or different and each is a hydrogen, a halogen or an alkyl; salts thereof; methods for production thereof; and pharmaceutical use thereof. The compounds and salts thereof show an excellent antitumor effect in mammals. More specifically, they show a remarkable activity of inhibiting growth of mouse tumors, cultured human tumor cells, and human tumors transplanted to nude mice, and are useful for the treatment and prevention of recurrence of lung cancer, gastrointestinal cancer, breast cancer, cervical cancer, gynecological cancer, urinological cancer, leukemia, melanoma, lymphogenous metastatic tumor and the like in mammals. They are also useful as antitumor agents since they have an increased bioavailability and low toxicity. In addition, they have the effects of maintaining and enhancing their activities.
摘要翻译： PCT No.PCT / JP94 / 00427 Sec。 371 1995年9月15日第 102（e）日期1995年9月15日PCT 1994年3月16日PCT公布。第WO94 / 21659号公报日期1994年9月29日新颖的式（I）的2'-亚甲基二核苷酸化合物其中R是氢或卤素，R 1和R 2相同或不同，各自为脂肪酸残基或烃残基，R 3和R 4相同或不同，各自为氢，卤素或烷基; 的盐; 生产方法; 及其药物用途。其化合物和盐在哺乳动物中表现出优异的抗肿瘤效果。更具体地说，它们显示了抑制小鼠肿瘤，培养的人肿瘤细胞和移植到裸鼠的人肿瘤生长的显着活性，并且可用于治疗和预防肺癌，胃肠癌，乳腺癌，宫颈癌的复发，妇科癌症，尿毒症，白血病，黑素瘤，淋巴瘤转移瘤等。它们也可用作抗肿瘤剂，因为它们具有增加的生物利用度和低毒性。此外，它们还具有维护和增强活动的效果。

4. 发明授权

US5691319A Pyrimidine nucleoside derivatives having anti-tumor activity, their preparation and use 失效
标题翻译：嘧啶核苷衍生物具有抗肿瘤活性，其制备和用途
公开(公告)号：US5691319A
公开(公告)日：1997-11-25
申请号：US465127
申请日：1995-06-05
申请人： Masakatsu Kaneko , Hitoshi Hotoda , Tomoyuki Shibata , Tomowo Kobayashi , Yoshihiro Mitsuhashi , Akira Matsuda , Takuma Sasaki
发明人： Masakatsu Kaneko , Hitoshi Hotoda , Tomoyuki Shibata , Tomowo Kobayashi , Yoshihiro Mitsuhashi , Akira Matsuda , Takuma Sasaki
IPC分类号： A61K31/505 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61P35/00 , C07D405/04 , C07H19/06 , C07H19/073 , C07H19/09
CPC分类号： C07H19/06 , C07H19/073
摘要： Compounds of formula (I): ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected from the group consisting of hydrogen atoms, optionally substituted alkanoyl groups and alkenylcarbonyl groups, PROVIDED THAT at least one of R.sup.1, R.sup.2 and R.sup.3 represents an unsubstituted alkanoyl group having from 5 to 24 carbon atoms, said substituted alkanoyl group or said alkenylcarbonyl group; and one of R.sup.4 and R.sup.5 represents a hydrogen atom and the other represents a cyano group; have valuable anti-tumor activity.
摘要翻译：式（I）的化合物：其中：R1，R2和R3独立地选自氢原子，任选取代的烷酰基和烯基羰基，提供了R1，R2和R3中的至少一个表示具有5至24个碳原子的未取代的烷酰基，所述取代的烷酰基或所述烯基羰基; R 4和R 5中的一个表示氢原子，另一个表示氰基; 具有有价值的抗肿瘤活性。

5. 发明授权

US5126361A Imidazole derivatives and use thereof 失效
标题翻译：咪唑衍生物及其用途
公开(公告)号：US5126361A
公开(公告)日：1992-06-30
申请号：US702210
申请日：1991-05-15
申请人： Tohru Ueda , Akira Matsuda , Noriaki Minakawa , Takuma Sasaki , Yoshikazu Yanagi
发明人： Tohru Ueda , Akira Matsuda , Noriaki Minakawa , Takuma Sasaki , Yoshikazu Yanagi
IPC分类号： C07D233/90 , C07H19/052
CPC分类号： C07H19/052 , C07D233/90 , Y02P20/55
摘要： Disclosed are imidazole derivatives represented by formula [I]: ##STR1## wherein R is a hydrogen atom or ##STR2## wherein R.sup.2 is a hydrogen atom or a hydroxy protecting group, R.sup.2 protecting either a single hydroxy or two hydroxies together when R.sup.2 is a hydroxy protecting group, and R.sup.3 is a hydrogen atom or OR.sup.2 ; A is CONH.sub.2 or CN; and R.sup.1 is a hydrogen atom, lower alkyl, hydroxy lower alkyl, or phenyl.Also disclosed are six processes for producing these novel compounds among which a typical process comprises reacting a starting imidazole compound having a halogen at the 5-position thereof with an acetylene derivative to alkynylate the 5-position.Furthermore, the compounds have remarkable antitumor activities and therefore can provide novel antitumor agents.

6. 发明授权

US5026835A Pyrimidine 2'-methylidene nucleoside compounds 失效
标题翻译：嘧啶2'-亚甲基核苷化合物
公开(公告)号：US5026835A
公开(公告)日：1991-06-25
申请号：US447512
申请日：1989-12-07
申请人： Tohru Ueda , Takuma Sasaki , Akira Matsuda , Takanori Miyashita , Shinji Sakata , Keiji Yamagami , Akihiro Fujii
发明人： Tohru Ueda , Takuma Sasaki , Akira Matsuda , Takanori Miyashita , Shinji Sakata , Keiji Yamagami , Akihiro Fujii
IPC分类号： C07H19/06
CPC分类号： C07H19/06
摘要： Pyrimidine 2'-deoxy-2'-methylidene nucleoside compounds: ##STR1## wherein R.sup.1 represents amino, hydroxy, silylamino, silyloxy, acylamino or acyloxy; R.sup.2 represents hydrogen, halogen, a lower alkyl, a lower alkenyl, a lower alkynyl or haloalkyl; R.sup.3 and R.sup.4 represent the same or different hydrogen, silyl, acyl or aminoacyl, or a pharmaceutically acceptable salt or hydrate thereof, except that R.sup.1 is amino or hydroxy, and both of R.sup.3 and R.sup.4 are hydrogen.Said compounds possess excellent antitumor and antiviral activities, thus providing novel anticancer and antiviral agent.

7. 再颁专利

USRE38090E1 3′-substituted nucleoside derivative 有权
标题翻译： 3'-取代核苷衍生物
公开(公告)号：USRE38090E1
公开(公告)日：2003-04-22
申请号：US09584171
申请日：2000-05-26
申请人： Akira Matsuda , Takuma Sasaki
发明人： Akira Matsuda , Takuma Sasaki
IPC分类号： A61K3170
CPC分类号： C07H19/06 , C07H19/04 , C07H19/10 , C07H19/16 , C07H19/20 , Y02P20/55
摘要： The invention relates to a 3′-substituted nucleoside derivative represented by the following general formula (1): wherein B means a nucleic acid base which may have a substituent, Z represents a lower alkynyl or lower alkenyl group which may be substituted by a group represented by the formula: in which Ra, Rb and Rc are individually a lower alkyl group or a phenyl group, or an oxiranyl group which may have at least one lower alkyl group, R1 and R2 individually represent H or an ester-forming residue capable of easily leaving in a living body, and R3 is H, a mono- or polyphosphoric acid residue, or an ester-forming residue capable of easily leaving in a living body, with the proviso that the sugar moiety is ribose, or a pharmaceutically acceptable salt thereof. The 3′-substituted nucleoside derivative according to the invention has an excellent antitumor activity and is hence useful for treatment for and prevention of cancers.
摘要翻译：本发明涉及由以下通式（1）表示的3'-取代核苷衍生物：其中B表示可具有取代基的核酸碱基，Z表示可被基团取代的低级炔基或低级烯基由下式表示：其中Ra，Rb和Rc分别为低级烷基或苯基，或可具有至少一个低级烷基的环氧乙烷基，R 1和R 2分别表示H或成酯残基容易地离开生物体，R3是H，单磷酸或多磷酸残基或能够容易地在活体中离开的酯形成残基，条件是糖部分是核糖或药学上可接受的的盐。根据本发明的3'-取代的核苷衍生物具有优异的抗肿瘤活性，因此可用于治疗和预防癌症。

8. 发明授权

US5705630A 2'-methylidenepyrimidine nucleoside compounds 失效
标题翻译： 2'-亚甲基嘧啶核苷化合物
公开(公告)号：US5705630A
公开(公告)日：1998-01-06
申请号：US818656
申请日：1992-01-07
申请人： Tohru Ueda , Takuma Sasaki , Akira Matsuda , Keiji Yamagami , Akihiro Fujii
发明人： Tohru Ueda , Takuma Sasaki , Akira Matsuda , Keiji Yamagami , Akihiro Fujii
IPC分类号： C07H19/06 , C07H19/10 , C07H19/073
CPC分类号： C07H19/06 , C07H19/10
摘要： 2'-Methylidenepyrimidine nucleoside compounds of the general formula: ##STR1## wherein R.sup.1 stands for amino or hydroxy group; R.sup.2 stands for a halogen or a lower alkyl when R.sup.1 is amino or R.sup.2 stands for an alkyl having 2 to 4 carbon atoms, an alkynyl having 2 to 4 carbon atoms or a haloalkyl when R.sup.1 is hydroxy group; and R.sup.3 stands for hydrogen or a phosphoric acid residue, or salts thereof, anticancer compositions containing one or more of these compounds and methods for production of these compounds. Said compounds and salts thereof exhibit noticeable antitumor activities and are useful as anticancer agents.
摘要翻译： 2'-亚甲基嘧啶核苷化合物，其通式如下：其中R1代表氨基或羟基; 当R 1为氨基或R 2表示具有2至4个碳原子的烷基，具有2至4个碳原子的炔基或R 1为羟基时的卤代烷基时，R 2表示卤素或低级烷基; R3表示氢或磷酸残基或其盐，含有这些化合物中的一种或多种的抗癌组合物及其制备方法。所述化合物及其盐具有显着的抗肿瘤活性，可用作抗癌剂。

9. 发明授权

US5401726A 2'methylidenepyrimidine nucleoside compounds, their use and method for production thereof 失效
标题翻译：二亚甲基嘧啶核苷化合物，其用途及其制备方法
公开(公告)号：US5401726A
公开(公告)日：1995-03-28
申请号：US44039
申请日：1993-04-08
申请人： Tohru Ueda , Takuma Sasaki , Akira Matsuda , Keiji Yamagami , Akihiro Fujii
发明人： Tohru Ueda , Takuma Sasaki , Akira Matsuda , Keiji Yamagami , Akihiro Fujii
IPC分类号： C07H19/06 , C07H19/10 , A61K31/70
CPC分类号： C07H19/06 , C07H19/10
摘要： 2'-Methylidenepyrimidine nucleoside compounds of the general formula: ##STR1## wherein R.sup.1 stands for amino or hydroxy group; R.sup.2 stands for a halogen or a lower alkyl when R.sup.1 is amino or R.sup.2 stands for an alkyl having 2 to 4 carbon atoms, an alkynyl having 2 to 4 carbon atoms or a haloalkyl when R.sup.1 is hydroxy group; and R.sup.3 stands for hydrogen or a phosphoric acid residue, or salts thereof, compositions containing one or more of these compounds and methods for production of these compounds are disclosed.Said compounds and salts thereof exhibit noticeable antitumor activities.
摘要翻译： 2'-亚甲基嘧啶核苷化合物，其通式如下：其中R1代表氨基或羟基; 当R 1为氨基或R 2表示具有2至4个碳原子的烷基，具有2至4个碳原子的炔基或R 1为羟基时的卤代烷基时，R 2表示卤素或低级烷基; R3代表氢或磷酸残基，或其盐，含有这些化合物中的一种或多种的组合物和这些化合物的制备方法。所述化合物及其盐具有显着的抗肿瘤活性。

10. 发明授权

US5059590A Imidazole derivatives, process for production thereof, and use thereof 失效
标题翻译：咪唑衍生物，其生产方法及其用途
公开(公告)号：US5059590A
公开(公告)日：1991-10-22
申请号：US316969
申请日：1989-02-28
申请人： Tohru Ueda , Akira Matsuda , Noriaki Minakawa , Takuma Sasaki , Yoshikazu Yanagi
发明人： Tohru Ueda , Akira Matsuda , Noriaki Minakawa , Takuma Sasaki , Yoshikazu Yanagi
IPC分类号： C07D233/90 , C07H19/052
CPC分类号： C07H19/052 , C07D233/90 , Y02P20/55
摘要： Disclosed are imidazole derivatives represented by formula [I]: ##STR1## wherein R is a hydrogen atom or ##STR2## wherein R.sup.2 is a hydrogen atom or a hydroxy protecting group, R.sup.2 protecting either a single hydroxy or two hydroxies together when R.sup.2 is a hydroxy protecting group, and R.sup.3 is a hydrogen atom or OR.sup.2 ; A is CONH.sub.2 or CN; and R.sup.1 is a hydrogen atom, lower alkyl, hydroxy lower alkyl, or phenyl.Also disclosed are six processes for producing these novel compounds among which a typical process comprises reacting a starting imidazole compound having a halogen at the 5-position thereof with an acetylene derivative to alkynylate the 5-position.Furthermore, the compounds having remarkable antitumor activities and therefore can provide novel antitumor agents.

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