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1. 发明授权

US5106868A Epoxycyclohexenone amides with antibacterial activity 失效
标题翻译：具有抗菌活性的环氧环己烯酮
公开(公告)号：US5106868A
公开(公告)日：1992-04-21
申请号：US696610
申请日：1991-05-07
申请人： Hirofumi Nakano , Mitsunobu Hara , Yutaka Saito , Yoji Ikuina , Toshimitsu Takiguchi , Masami Okabe
发明人： Hirofumi Nakano , Mitsunobu Hara , Yutaka Saito , Yoji Ikuina , Toshimitsu Takiguchi , Masami Okabe
IPC分类号： C07D303/36 , C07D303/46 , C12P17/02
CPC分类号： C12R1/465 , C07D303/36 , C07D303/46 , C12P17/02
摘要： Compounds UCF1 and derivatives thereof exhibit anti-bacterial and anti-tumor activities and may be used for the preparation of anti-bacterial and anti-tumor agents.Compounds UCF1 may be produced by fermentation of a microorganism of the genus Streptomyces capable of producing compounds UCF1, preferably Streptomyces sp. UOF1 (FERM BP-2844) and recovering the desired compounds from the cultured broth.The compounds UCF1 have the formula ##STR1## wherein R represents either ##STR2## The compounds may be oxidized to obtain derivatives of formula ##STR3## which exhibit similar pharmacological activities.

2. 发明授权

US4914198A Novel substance UCY1003 and process for preparing the same 失效
标题翻译：新型物质UCY1003及其制备方法
公开(公告)号：US4914198A
公开(公告)日：1990-04-03
申请号：US946842
申请日：1986-12-29
申请人： Hirofumi Nakano , Mitsunobu Hara , Yoshinori Yamashita , Isao Kawamoto , Katsuhiko Ando , Hiroshi Sano , Toru Yasuzawa , Katsuichi Shuto
发明人： Hirofumi Nakano , Mitsunobu Hara , Yoshinori Yamashita , Isao Kawamoto , Katsuhiko Ando , Hiroshi Sano , Toru Yasuzawa , Katsuichi Shuto
IPC分类号： A61K31/58 , A61P9/12 , A61P25/04 , A61P31/04 , A61P31/10 , C07J71/00 , C12P33/00 , C12R1/80
CPC分类号： C12P33/00 , C07J71/001
摘要： Novel substance UCY1003 produced by culturing of a microorganism has the following chemical structure and analgesic, hypotensive and antifungal activities: ##STR1##
摘要翻译：通过培养微生物产生的新物质UCY1003具有以下化学结构和镇痛，降血压和抗真菌活性：

3. 发明授权

US5066817A DC115A compounds produced by streptomyces sp. 失效
标题翻译： DC115A由STREPTOMYCES SP生产的化合物
公开(公告)号：US5066817A
公开(公告)日：1991-11-19
申请号：US516304
申请日：1990-04-30
申请人： Hirofumi Nakano , Mitsunobu Hara , Tsuyoshi Mokudai , Isao Kawamoto , Mayumi Yoshida , Eiji Kobayashi
发明人： Hirofumi Nakano , Mitsunobu Hara , Tsuyoshi Mokudai , Isao Kawamoto , Mayumi Yoshida , Eiji Kobayashi
IPC分类号： C07D407/04 , C12P17/06
CPC分类号： C07D407/04 , C12P17/06 , Y10S435/886
摘要： Disclosed are DC115A compounds represented by the following general formula: ##STR1## wherein R represents ethyl, propyl or 1-propenyl, and which have antibacterial and anti-tumor activity. DC115A compounds are produced by culturing a microorganism belonging to the genus Streptomyces.

4. 发明授权

US5686606A UCF116 compounds 失效
标题翻译： UCF116化合物
公开(公告)号：US5686606A
公开(公告)日：1997-11-11
申请号：US682514
申请日：1996-07-12
申请人： Tamio Mizukami , Mikito Itoh , Mitsunobu Hara , Hirofumi Nakano , Yumiko Aotani , Keiko Ochiai , Shiro Akinaga , Akira Mihara
发明人： Tamio Mizukami , Mikito Itoh , Mitsunobu Hara , Hirofumi Nakano , Yumiko Aotani , Keiko Ochiai , Shiro Akinaga , Akira Mihara
IPC分类号： C07D225/06 , C12P17/10 , A61K31/415
CPC分类号： C07D225/06 , C12P17/10
摘要： The present invention relates to UCF116 compounds represented by the formula (I) : ##STR1## wherein an example of Q.sup.1 representation is ##STR2## and an example of Q.sup.2 representation is ##STR3## which have antibacterial and antitumor activity and are useful as antibacterial and antitumor agents.
摘要翻译： PCT No.PCT / JP95 / 02325 Sec。 371日期：1996年7月12日 102（e）日期1996年7月12日PCT提交1995年11月14日PCT公布。公开号WO96 / 15114 日期：1996年5月23日本发明涉及由式（I）表示的UCF116化合物：其中Q1表示的实例是活性并可用作抗细菌剂和抗肿瘤剂。

5. 发明授权

US4999196A Compound DC-107 produced by Streptomyces sp. 失效
标题翻译：由Streptomyces sp。生产的复合DC-107
公开(公告)号：US4999196A
公开(公告)日：1991-03-12
申请号：US330990
申请日：1989-03-29
申请人： Hirofumi Nakano , Mitsunobu Hara , Isami Takahashi , Kozo Asano , Takao Iida , Makoto Morimoto
发明人： Hirofumi Nakano , Mitsunobu Hara , Isami Takahashi , Kozo Asano , Takao Iida , Makoto Morimoto
IPC分类号： A61K35/74 , A61K31/425 , A61P35/00 , C07D513/20 , C12P1/06 , C12P17/18 , C12R1/465
CPC分类号： C12P1/06 , Y10S435/886
摘要： A novel compound, DC-107, is produced by culturing a microorganism belonging to the genus Streptomyces. It is useful as a medicine because of its antibacterial and anti-tumor activity.

6. 发明授权

US5082857A Chemical compound 失效
标题翻译：化合物
公开(公告)号：US5082857A
公开(公告)日：1992-01-21
申请号：US612317
申请日：1990-11-13
申请人： Hirofumi Nakano , Mitsunobu Hara , Yohichi Uosaki , Isao Kawamoto , Keiiechi Takahashi , Katsushige Gomi
发明人： Hirofumi Nakano , Mitsunobu Hara , Yohichi Uosaki , Isao Kawamoto , Keiiechi Takahashi , Katsushige Gomi
IPC分类号： C12P17/16 , A61K31/35 , A61P35/00 , C07D493/04 , C12N1/20 , C12P17/06 , C12R1/465
CPC分类号： C07D493/04 , C12P17/06
摘要： The present invention relates to a compound designated "DC114-C" having excellent anti-bacterial and anti-tumor activities. This compound may be obtained by fermentation of a microorganism of the genus Streptomyces, preferably Streptomyces sp. DO-114 (FERM BP-2641).

7. 发明授权

US06492392B1 2-piperidone compounds 失效
标题翻译： 2-哌啶酮化合物
公开(公告)号：US06492392B1
公开(公告)日：2002-12-10
申请号：US09481542
申请日：2000-01-12
申请人： Yutaka Kanda , Rieko Tanaka , Mitsunobu Hara , Jun Eishima , Shiro Akinaga , Tadashi Ashizawa
发明人： Yutaka Kanda , Rieko Tanaka , Mitsunobu Hara , Jun Eishima , Shiro Akinaga , Tadashi Ashizawa
IPC分类号： A61K31445
CPC分类号： C07D401/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D405/14 , C07D409/14
摘要： The present invention provides 2-piperidone compounds or pharmaceutically acceptable salts thereof, which have a potent activity of inhibiting the proliferation of tumor cells and thus are useful as medicaments, as well as antitumor agents containing these compounds. The 2-piperidone compound is represented by the following formula (I): wherein R1 represents —(CH2)nR1a {wherein n is an integer of from 0 to 5, and R1a represents amino, lower alkylamino, di(lower alkyl)amino, substituted or unsubstituted aryl, or a substituted or unsubstituted heterocyclic group}, and R2 and R3 independently represent lower alkyl which may be substituted by lower alkoxycarboyl; lower alkenyl, aralkyl or lower alkynyl which may be substituted by substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group; substituted or unsubstituted aryl; or a substituted or unsubstituted heterocyclic group.
摘要翻译：本发明提供了具有抑制肿瘤细胞增殖的有效活性的2-哌啶酮化合物或其药学上可接受的盐，因此可用作药物，以及含有这些化合物的抗肿瘤剂。 2-哌啶酮化合物由下式（I）表示：其中R1表示 - （CH2）nR1a {其中n为0-5的整数，R1a表示氨基，低级烷基氨基，二（低级烷基）氨基，取代的或未取代的芳基，或取代或未取代的杂环基}，R2和R3独立地表示可以被低级烷氧基羰基取代的低级烷基; 可被取代或未取代的芳基或取代或未取代的杂环基取代的低级烯基，芳烷基或低级炔基; 取代或未取代的芳基; 或取代或未取代的杂环基。

8. 发明授权

US06861530B2 Piperidine derivatives 失效
标题翻译：哌啶衍生物
公开(公告)号：US06861530B2
公开(公告)日：2005-03-01
申请号：US09899186
申请日：2001-07-06
申请人： Shinji Nara , Rieko Nakatsu , Yutaka Kanda , Shiro Akinaga , Mitsunobu Hara , Jun Eishima , Timothy A. Grese , Douglas L. Gernert
发明人： Shinji Nara , Rieko Nakatsu , Yutaka Kanda , Shiro Akinaga , Mitsunobu Hara , Jun Eishima , Timothy A. Grese , Douglas L. Gernert
IPC分类号： C07D211/38 , A61K31/451 , A61K31/454 , A61K31/4545 , A61P35/00 , C07D401/04 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D211/68 , C07D211/80 , C07D213/02 , C07D401/00 , C07D409/00
CPC分类号： C07D211/38 , C07D401/04 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： This invention relates to substituted piperidine derivatives having at least one six-membered ring substituent. The piperidine derivatives exhibit antitumor activity and are useful as pharmaceuticals such as an antitumor agent.
摘要翻译：本发明涉及具有至少一个六元环取代基的取代哌啶衍生物。哌啶衍生物显示出抗肿瘤活性，并且可用作药物如抗肿瘤剂。

9. 发明授权

US06548536B2 Agent for inducing apoptosis 失效
标题翻译：诱导细胞凋亡的药物
公开(公告)号：US06548536B2
公开(公告)日：2003-04-15
申请号：US09793654
申请日：2001-02-27
申请人： Mitsunobu Hara , Takayuki Nakashima , Yutaka Kanda , Masami Hamano , Shun-ichi Ikeda , Yuko Uosaki , Yoko Takata , Junji Kanazawa
发明人： Mitsunobu Hara , Takayuki Nakashima , Yutaka Kanda , Masami Hamano , Shun-ichi Ikeda , Yuko Uosaki , Yoko Takata , Junji Kanazawa
IPC分类号： A61K3134
CPC分类号： C07D407/14 , A61K31/00 , A61K31/365 , C07H17/08
摘要： Agents for inducing apoptosis comprising a tetrocarcin derivative represented by the following formula (I) or a salt thereof as an active ingredient (---- represents a single bond or a double bond; j and k represent 0 or 1; R1 to R3, R7 to R10 and R14 represent a hydrogen atom, a lower alkyl group and the like; R4, R11, R12, R13 and R15 to R18 represent a hydrogen atom, a hydroxyl group, a lower alkyl group and the like; R5 and R6 represents a hydrogen atom, a hydroxyl group, a lower alkyl group, a group represented by the following formula (B) (R32 represents a formyl group and the like, R33 to R35 represent a hydrogen atom, a hydroxyl group, a lower alkyl group and the like); R19 represents a hydroxyl group, a lower alkoxyl group, a lower alkanoyloxy group and the like). The agents are useful as medicaments for preventive and/or therapeutic treatment of diseases resulting from increased expression of Bcl-2 family proteins, for example, cancers, AIDS and the like.
摘要翻译：用于诱导凋亡的药剂，其包含由下式（I）表示的四环卟啉衍生物或其盐作为活性成分（----表示单键或双键; j和k表示0或1; R 1至R 3， R 7〜R 10和R 14表示氢原子，低级烷基等; R 4，R 11，R 12，R 13，R 15〜R 18表示氢原子，羟基，低级烷基等; R 5，R 6表示氢原子，羟基，低级烷基，下式（B）表示的基团（R32表示甲酰基等，R33〜R35表示氢原子，羟基，低级烷基，类似）; R 19表示羟基，低级烷氧基，低级烷酰氧基等）。这些药剂可用作预防和/或治疗由Bcl-2家族蛋白（例如癌症，AIDS等）表达增加而引起的疾病的药物。

10. 发明授权

US06407087B1 UCF116 derivatives 失效
标题翻译： UCF116衍生物
公开(公告)号：US06407087B1
公开(公告)日：2002-06-18
申请号：US09605014
申请日：2000-06-27
申请人： Mitsunobu Hara , Shiro Akinaga , Yutaka Kanda , Timothy S. Powers , David A. Johnson
发明人： Mitsunobu Hara , Shiro Akinaga , Yutaka Kanda , Timothy S. Powers , David A. Johnson
IPC分类号： C07D22506
CPC分类号： C07D401/12 , C07D225/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D513/04
摘要： UCF116 derivatives represented by formula (I): wherein Q represents and R represents hydrogen, C(═O)R1a (wherein R1a represents methyl, ethyl, propyl, isopropyl, 2,2-dimethylpropyl, pentyl, alkyl having 6 to 10 carbon atoms, 1-propenyl, isopropenyl, 2-methyl-1-propenyl, substituted or unsubstituted alicyclic alkyl having 3 to 5 carbon atoms, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aralkyloxy, or substituted lower alkyl), C(═X)NHR1b (wherein X represents an oxygen or sulfur atom, and R1b represents substituted or unsubstituted lower alkyl, substituted or unsubstituted alicyclic alkyl, substituted or unsubstituted lower alkoxycarbonyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, or a substituted or unsubstituted heterocyclic group), or SO2R1c (wherein R1c represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, a substituted or unsubstituted heterocyclic group, or substituted or unsubstituted lower alkenyl), with the proviso that, when Q is R is not benzoyl; salts thereof; isomers thereof; hydrates thereof; or solvates thereof.
摘要翻译：由式（I）表示的UCF116衍生物：其中Q表示并且R表示氢，C（= O）R 1a（其中R 1a表示甲基，乙基，丙基，异丙基，2,2-二甲基丙基，戊基，具有6至10个碳原子的烷基，取代或未取代的芳基，取代或未取代的芳烷基，取代或未取代的杂环基，取代或未取代的芳烷氧基或取代或未取代的低级烷基烷基），C（= X）NHR1b（其中X表示氧或硫原子，并且R1b表示取代或未取代的低级烷基，取代或未取代的脂环族烷基，取代或未取代的低级烷氧基羰基，取代或未取代的芳基，取代或未取代的芳烷基，或取代或未取代的杂环基）或SO 2 R 1c（其中R 1c表示取代或未取代的低级烷基，取代或未取代的芳基，取代基芳基或未取代的芳烷基，取代或未取代的杂环基或取代或未取代的低级烯基），条件是当Q不是苯甲酰基时; 的盐; 异构体; 其水合物; 或溶剂化物。

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