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1. 发明申请

WO1996033989A1 RADICICOL DERIVATIVES 审中-公开
标题翻译： RADICICOL衍生物
公开(公告)号：WO1996033989A1
公开(公告)日：1996-10-31
申请号：PCT/JP1996001158
申请日：1996-04-26
申请人： KYOWA HAKKO KOGYO CO., LTD. , AGATSUMA, Tsutomu , SAITOH, Yutaka , YAMASHITA, Yoshinori , MIZUKAMI, Tamio , AKINAGA, Shiro , GOMI, Katsushige , AKASAKA, Kazuhito , TAKAHASHI, Isami
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D313/00
CPC分类号： C07D313/00
摘要： Radicicol derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, wherein R and R may be the same or different and each represents hydrogen, alkanoyl, alkenoyl or tert -butyldimethylsilyl; and (1) when X represents halogeno, then Y represents oxygen or R -O-N (R being hydrogen or (un)substituted lower alkyl) and R represents hydrogen, alkanoyl, alkenoyl, etc.; while (2) when X is combined with R to represent a single bond, Y represents R -O-N (R being the same as R ). The derivatives have a tyrosine kinase inhibitory activity and thus have various pharmacological activities such as antitumor, antibacterial and immunosuppressive effects.
摘要翻译：由通式（I）表示的脱甲硅烷醇衍生物或其药理学上可接受的盐，其中R 1和R 2可以相同或不同，各自代表氢，链烷酰基，烯酰基或叔丁基二甲基甲硅烷基 ; 和（1）当X表示卤代时，则Y表示氧或R 4 -O-N（R 4表示氢或（取代的）低级烷基），R 3表示氢，烷酰基，烯酰基等。而（2）当X与R 3结合以表示单键时，Y表示R 4B -O-N（R 4与R 4相同）。该衍生物具有酪氨酸激酶抑制活性，因此具有各种药理活性，如抗肿瘤，抗菌和免疫抑制作用。

2. 发明申请

WO1993009110A1 COMPOUND DC8118 审中-公开
标题翻译：化合物DC8118
公开(公告)号：WO1993009110A1
公开(公告)日：1993-05-13
申请号：PCT/JP1992001408
申请日：1992-10-30
申请人： KYOWA HAKKO KOGYO CO., LTD. , NAKANO, Hirofumi , HARA, Mitsunobu , KATSUYAMA, Toshiyuki , UOZAKI, Yoichi , GOMI, Katsushige
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D309/36
CPC分类号： C12P17/06 , C07D309/36
摘要： Compound DC8118 represented by general formula (I) wherein R represents -CH(OH)CH3 or -COCH3. It has antibacterial and antitumor activities.
摘要翻译：由通式（I）表示的化合物DC8118，其中R表示-CH（OH）CH3或-COCH3。具有抗菌，抗肿瘤活性。

3. 发明申请

WO1997000260A1 DC107 DERIVATIVES 审中-公开
标题翻译： DC107衍生物
公开(公告)号：WO1997000260A1
公开(公告)日：1997-01-03
申请号：PCT/JP1996001646
申请日：1996-06-14
申请人： KYOWA HAKKO KOGYO CO., LTD. , KANDA, Yutaka , SAITOH, Yutaka , SAITO, Hiromitsu , ASHIZAWA, Tadashi , SUGIYAMA, Kazuyo , GOMI, Katsushige , KAKITA, Shingo , TAKAHASHI, Yuichi , MURAKATA, Chikara
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D513/08
CPC分类号： C07D513/08
摘要： DC107 derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, wherein R represents hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR , etc.; R represents hydrogen or COR ; R represents lower alkyl, lower alkenyl, aralkyl optionally substituted by optionally substituted aryl, lower alkoxyalkyl, aralkyloxyalkyl, optionally substituted aryloxyalkyl, lower alkoxycarbonylalkyl, lower alkanoyloxy-alkyl, alicyclic alkanoyloxyalkyl, etc., or R forms a single bond together with Y; Y forms a single bond together with R or Z; Z represents hydrogen or forms a single bond together with Y; and W represents oxygen or NR , excluding the compound (DC107) wherein R , R and Z are each hydrogen, R forms a single bond together with Y and W is oxygen.
摘要翻译：由通式（I）表示的DC107衍生物或其药学上可接受的盐，其中R 1表示氢，低级烷氧基烷基，芳烷氧基烷基，低级烷氧基烷氧基烷基，低级烷氧基烷氧基烷氧基烷基，芳烷基，四氢吡喃基，COR4等; R 2表示氢或COR 5; R 3表示低级烷基，低级烯基，任选被任意取代的芳基取代的芳烷基，低级烷氧基烷基，芳烷氧基烷基，任选取代的芳氧基烷基，低级烷氧基羰基烷基，低级烷酰氧基 - 烷基，脂环族烷酰氧基烷基等，或R 3形成单与Y键合; Y与R 3或Z一起形成单键; Z表示氢或与Y一起形成单键; W表示氧或NR 6，不包括其中R 1，R 2和Z各自为氢的化合物（DC107），R 3与Y一起形成单键，W是氧。

4. 发明申请

WO1995029179A1 DC-89 DERIVATIVE 审中-公开
公开(公告)号：WO1995029179A1
公开(公告)日：1995-11-02
申请号：PCT/JP1995000779
申请日：1995-04-20
申请人： KYOWA HAKKO KOGYO CO., LTD. , AMISHIRO, Nobuyoshi , NAGAMURA, Satoru , SAITO, Hiromitsu , KOBAYASHI, Eiji , OKAMOTO, Akihiko , GOMI, Katsushige
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A DC-89 derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, wherein X represents Cl or Br; R represents (un)substituted alkyl, (un)substituted aralkyl, COR or SO2R ; and Y represents the group (a) or (b). The compound has an excellent antitumor activity and is useful as an antitumor drug.
摘要翻译：由通式（I）表示的DC-89衍生物或其药理学上可接受的盐，其中X表示Cl或Br; R表示（未）取代的烷基，（未）取代的芳烷基，COR 1或SO 2 R 7; Y表示（a）或（b）。该化合物具有优异的抗肿瘤活性，可用作抗肿瘤药物。

5. 发明申请

WO1994010135A1 BENZENESULFONAMIDE DERIVATIVE 审中-公开
标题翻译：苯并呋喃衍生物
公开(公告)号：WO1994010135A1
公开(公告)日：1994-05-11
申请号：PCT/JP1992001429
申请日：1992-11-05
申请人： KYOWA HAKKO KOGYO CO., LTD. , KINOSHITA, Iwao , TAKAI, Haruki , KOSAKA, Nobuo , SUGAWARA, Katsura , ISHII, Akio , ISHIDA, Hiroyuki , GOMI, Katsushige
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07C311/29
CPC分类号： C07C323/49 , C07C311/29 , C07C2601/14 , C07C2601/18 , C07C2603/74 , C07D211/58 , C07D277/46 , C07D295/26
摘要： A benzenesulfonamide derivative represented by general formula (I), which is useful for treating osteoporosis, or a pharmacologically acceptable salt thereof, wherein R and R may be the same or different from each other and each represents hydrogen or lower alkanoyl; and R and R may be the same or different from each other and each represents hydrogen, lower alkyl, alicyclic alkyl, (un)substituted polycyclic alkyl, substituted aryl or (un)substituted heterocycle, or alternatively R and R are combined together with the adjacent nitrogen atom to represent (un)substituted alicyclic heterocycle.
摘要翻译：可用于治疗骨质疏松症的通式（I）表示的苯磺酰胺衍生物或其药理学上可接受的盐，其中R 1和R 2可以相同或不同，各自表示氢或低级烷; R 3和R 4可以彼此相同或不同，各自表示氢，低级烷基，脂环族烷基，（取代的）多环烷基，取代的芳基或（取代的）取代的杂环， 3>和R 4与相邻的氮原子一起代表（未）取代的脂环族杂环。

6. 发明申请

WO1995014003A1 PROPENONE DERIVATIVE 审中-公开
标题翻译：丙酮衍生物
公开(公告)号：WO1995014003A1
公开(公告)日：1995-05-26
申请号：PCT/JP1994001934
申请日：1994-11-16
申请人： KYOWA HAKKO KOGYO CO., LTD. , IKEDA, Shun-ichi , KIMURA, Uichiro , ASHIZAWA, Tadashi , GOMI, Katsushige , SAITO, Hiromitsu , KASAI, Masaji
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D209/12
CPC分类号： C07D401/06 , C07D209/12 , C07D209/30 , C07D405/06
摘要： A propenone derivative represented by general formula (I) and a pharmacologically acceptable salt thereof, wherein R represents hydrogen, lower alkyl, lower alkanoyl, lower alkoxycarbonyl, lower alkylsulfonyl, aralkyl, (un)substituted aroyl, (un)substituted arylsulfonyl, (un)substituted heteroarylcarbonyl, (un)substituted heteroarylsulfonyl, diglycolyl or a group of formula (a), R represents hydrogen, lower alkyl, halogen, (un)substituted aryl or (un)substituted heteroaryl; R represents hydrogen, lower alkyl or (un)substituted aryl; and R , R , R and R represent each independently hydrogen, lower alkyl, lower alkoxy, aralkyloxy, hydroxy, nitro, halogen, trifluoromethyl or -NR R , wherein R and R represent each independently hydrogen, lower alkyl, lower alkanoyl, lower alkoxycarbonyl or (un)substituted aroyl.
摘要翻译：由通式（I）表示的丙烯酮衍生物及其药理学可接受的盐，其中R 1表示氢，低级烷基，低级烷酰基，低级烷氧基羰基，低级烷基磺酰基，芳烷基，（取代的）取代的芳酰基，（未）取代的芳基磺酰基，（un）取代的杂芳基羰基，（un）取代的杂芳基磺酰基，二油基或式（a）的基团，R 2表示氢，低级烷基，卤素，（未）取代的芳基或（取代） R 3表示氢，低级烷基或（未）取代的芳基; R 4，R 5，R 6和R 7各自独立地表示氢，低级烷基，低级烷氧基，芳烷氧基，羟基，硝基，卤素，三氟甲基或-NR 8 R 9。其中R 8和R 9各自独立地表示氢，低级烷基，低级烷酰基，低级烷氧基羰基或（取代的）取代的芳酰基。

7. 发明申请

WO1993002076A1 1,2-DITHIOLANE COMPOUND 审中-公开
标题翻译： 1,2-二苯酚化合物
公开(公告)号：WO1993002076A1
公开(公告)日：1993-02-04
申请号：PCT/JP1991000957
申请日：1991-07-18
申请人： KYOWA HAKKO KOGYO CO., LTD. , KANDA, Yutaka , FUKUYAMA, Tohru , SAITO, Hiromitsu , GOMI, Katsushige , NOMURA, Kayo
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D339/04
CPC分类号： C07D339/04
摘要： A 1,2-dithiolane compound with antibacterial and cell growth inhibitory activities represented by general formula (I), wherein n represents an integer of 0 to 2; R represents OR (wherein R represents hydrogen or lower alkyl), NR R (wherein R and R may be the same or different from each other and each represents hydrogen, lower alkyl, alicyclic alkyl or benzyl), or alpha (wherein p represents an integer of 2 to 8); and R represents hydrogen or lower alkyl.
摘要翻译：一种具有由通式（I）表示的抗细菌和细胞生长抑制活性的1,2-二硫戊环化合物，其中n表示0至2的整数; R 1表示OR 3（其中R 3表示氢或低级烷基），NR 4 R 5（其中R 4和R 5可以彼此相同或不同并且各自表示氢，低级烷基，脂环族烷基或苄基）或α（其中p表示2至8的整数）; R 2表示氢或低级烷基。

8. 发明申请

WO1996010405A1 ANTITUMOR AGENT 审中-公开
标题翻译：抗菌剂
公开(公告)号：WO1996010405A1
公开(公告)日：1996-04-11
申请号：PCT/JP1995001893
申请日：1995-09-20
申请人： KYOWA HAKKO KOGYO CO., LTD. , SAITO, Hiromitsu , AMISHIRO, Nobuyoshi , NAGAMURA, Satoru , KOBAYASHI, Eiji , OKAMOTO, Akihiko , GOMI Katsushige , YAMASHITA, Kinya , SATO, Kiyoshi , NAKAKURA, Masashi , HAYAKAWA, Eiji
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： A61K31/40
CPC分类号： C07D487/04 , C07D487/10
摘要： An antitumor agent against drug-fast tumors containing a compound represented by general formula (2) or (a) or a pharmacologically acceptable salt thereof as the active ingredient; wherein X represents Cl or Br; and R represents NR R (wherein R and R represent each independently hydrogen or C1-C4 linear or branched alkyl) or a group of formula (b) (wherein R represents CH2 or N-CH3). The agent has an excellent antitumor activity against drug-insensitive tumors and is useful as an antitumor agent against drug-fast tumors.
摘要翻译：一种含有通式（2）或（a）所示化合物或其药理学上可接受的盐作为有效成分的药物抗肿瘤药物的抗肿瘤剂; 其中X表示Cl或Br; 和R表示NR 1 R 2（其中R 1和R 2各自独立地表示氢或C 1 -C 4直链或支链烷基）或式（b）的基团（其中R 3表示 CH2或N-CH3）。该药剂对药物不敏感的肿瘤具有优异的抗肿瘤活性，可用作抗药物肿瘤的抗肿瘤剂。

9. 发明申请

WO1995019343A1 INDOLE DERIVATIVE 审中-公开
公开(公告)号：WO1995019343A1
公开(公告)日：1995-07-20
申请号：PCT/JP1995000019
申请日：1995-01-11
申请人： KYOWA HAKKO KOGYO CO., LTD. , MACHII, Daisuke , TAKAI, Haruki , KOSAKA, Nobuo , SEO, Hisakatsu , SUGIYAMA, Tomomi , NAKAMURA, Joji , ISHIDA, Hiroyuki , GOMI, Katsushige , SATO, Soichiro , UCHII, Masako
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D209/42
CPC分类号： C07D209/42
摘要： An indole derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, wherein R and R may be the same or different and each represents hydrogen, lower alkyl, -(CH2)n-OR (R representing hydrogen or lower alkyl, and n representing an integer of 1 to 6), or -(CH2)m-NR R (wherein R and R may be the same or different and each represents hydrogen or lower alkyl, or alternatively R and R are combined to represent, together with the nitrogen atom to which they are bonded, an (un)substituted heteroalicyclic group, and m represents an integer of 2 to 6); R represents hydrogen, lower alkyl or -(CH2)p-NR R (wherein R and R may be the same or different and each represents hydrogen or lower alkyl, or alternatively R and R are combined to represent, together with the nitrogen atom to which they are bonded, an (un)substituted heteroalicyclic group, and p represents an integer of 2 to 6); and R and R may be the same or different and each represents hydrogen, lower alkyl, cycloalkyl, (un)substituted aryl or (un)substituted heterocycle, or alternatively R and R are combined to represent, together with the nitrogen atom to which they are bonded, an (un)substituted heteroalicyclic group.
摘要翻译：由通式（I）表示的吲哚衍生物或其药理学上可接受的盐，其中R 1和R 2可以相同或不同，各自表示氢，低级烷基， - （CH 2）n -OR 6 （R 6表示氢或低级烷基，n表示1〜6的整数）或 - （CH 2）m -NR 7 R 8（其中R 7和R 8可以相同或不同，各自表示氢或低级烷基，或者R 7和R 8与它们所键合的氮原子一起代表与（un）取代的杂脂环基，m 表示2〜6的整数）; R 3表示氢，低级烷基或 - （CH 2）p -NR NR 9 R 10（其中R 9和R 10可以相同或不同，各自表示氢或低级烷基，或或者R 9和R 10与它们所键合的氮原子一起代表（取代的）杂脂环基，p表示2〜6的整数）。 R 4和R 5可以相同或不同，各自表示氢，低级烷基，环烷基，（未）取代的芳基或（未）取代的杂环，或者R 4和R 5分别为与它们所键合的氮原子一起表示（（un）取代的杂脂环基。

10. 发明申请

WO1994012458A1 SAINTOPIN DERIVATIVE 审中-公开
标题翻译： SAINTOPIN衍生物
公开(公告)号：WO1994012458A1
公开(公告)日：1994-06-09
申请号：PCT/JP1993001680
申请日：1993-11-17
申请人： KYOWA HAKKO KOGYO CO., LTD. , NAKANO, Hirofumi , FUJII, Noboru , YAMASHITA, Yoshinori , SAITOH, Yutaka , AGATSUMA, Tsutomu , ANDO, Katsuhiko , NISHIIE, Yasushi , KITA, Katsunori , MORISHIMA, Naoki , GOMI, Katsushige
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07C50/36
CPC分类号： C07C305/26 , C07C50/38 , C07C305/22 , C12P29/00
摘要： A saintopin E derivative represented by general formula (I) and useful as an antibacterial and antitumor agent, wherein when R represents hydrogen, then R represents SO2OH (in the case of UCE1022), while when R represents acetyl, then R represents hydrogen (in the case of saintopin E).
摘要翻译：由通式（I）表示的saintopin E衍生物，可用作抗细菌和抗肿瘤剂，其中当R 1表示氢时，R 2表示SO 2 OH（在UCE1022的情况下），而当R 1表示氢时，表示乙酰基，则R 2表示氢（在saintopin E的情况下）。

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