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1. 发明申请

WO1996028447A1 PYRROLOCARBAZOLE DERIVATIVES 审中-公开
标题翻译：吡咯烷酮衍生物
公开(公告)号：WO1996028447A1
公开(公告)日：1996-09-19
申请号：PCT/JP1996000557
申请日：1996-03-07
申请人： KYOWA HAKKO KOGYO CO., LTD. , IKUINA, Yoji , MURAKATA, Chikara , SAITOH, Yutaka , SHIOTSU, Yukimasa , IIDA, Takako , TAMAOKI, Tatsuya , YAMASHITA, Kinya , AKINAGA, Shiro
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Pyrrolocarbazole derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, wherein R represents lower alkyl or aralkyl; R represents hydrogen, optionally substituted lower alkyl, lower alkenyl or optionally substituted aralkyl; R , R , R , R and R are the same or different and each represents hydrogen, halogeno, nitro, optionally substituted lower alkanoyl, NR R or OR ; and R represents hydrogen or forms together with R -CONR -, provided that R , R , R , R , R , R and R do not represent hydrogen at the same time when R is benzyl. The compounds have the effect of promoting the production of thrombocytes and thus are useful in the treatment of thrombocytopenia.
摘要翻译：由通式（I）表示的吡咯并咔唑衍生物或其药理学上可接受的盐，其中R 1表示低级烷基或芳烷基; R 2表示氢，任选取代的低级烷基，低级烯基或任选取代的芳烷基; R 3，R 4，R 5，R 6和R 7相同或不同，各自表示氢，卤代，硝基，任选取代的低级烷酰基，NR 9 R 10 >或OR <11>; R 8表示氢或与R 3 -CONR 12一起形成，条件是R 2，R 3，R 4，R 5，R 6，R 当R 1是苄基时，R 7和R 8不同时代表氢。这些化合物具有促进凝血细胞生成的作用，因此可用于治疗血小板减少症。

2. 发明申请

WO1994006799A1 THROMBOCYTOPENIA REMEDY 审中-公开
标题翻译：硫唑嘌呤补救
公开(公告)号：WO1994006799A1
公开(公告)日：1994-03-31
申请号：PCT/JP1993001346
申请日：1993-09-20
申请人： KYOWA HAKKO KOGYO CO., LTD. , TAMAOKI, Tatsuya , SHIOTSU, Yukimasa , MURAKATA, Chikara , AKINAGA, Shiro , OKABE, Masami , SAITOH, Yutaka , WATANABE, Junichi , SHIRAKI, Takako
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D487/14
CPC分类号： C07D498/22 , C07H9/06 , C07H19/044
摘要： A thrombocytopenia remedy containing an indolocarbazole derivative represented by general formula (I) or a pharmacologically acceptable salt thereof as the active ingredient, and a novel indolocarbazole derivative.
摘要翻译：含有由通式（I）表示的吲哚并咔唑衍生物或其药理学上可接受的盐作为活性成分的血小板减少症药物和新的吲哚并咔唑衍生物。

3. 发明申请

WO1998025934A1 DC 107 DERIVATIVES (2) 审中-公开
标题翻译： DC 107衍生物（2）
公开(公告)号：WO1998025934A1
公开(公告)日：1998-06-18
申请号：PCT/JP1997004584
申请日：1997-12-12
申请人： KYOWA HAKKO KOGYO CO., LTD. , KANDA, Yutaka , ARAI, Hitoshi , YAMAGUCHI, Hiroyuki , ASHIZAWA, Tadashi , IKEDA, Shun-ichi , MURAKATA, Chikara , TAMAOKI, Tatsuya
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D513/18
CPC分类号： C07D513/08 , C07H15/26 , C07H17/02
摘要： DC 107 derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, each having antibacterial and antitumor activities, wherein R represents CO(CR R )n1[O(CH2)p1]n2OR , wherein n1 represents an integer of 1 or 2; R and R are the same or different and each represents hydrogen or lower alkyl; p1 and n2 are each an integer of 1 to 10; and R represents hydrogen, lower alkyl, etc.; or formula (II), (wherein A , A , A and A are the same or different and each represents hydrogen, hydroxy, etc.); R represents hydrogen or COR (wherein R represents lower alkyl, aralkyl, optionally substituted aryl, etc.); R represents lower alkyl, lower alkenyl, aralkyl having optionally substituted aryl, alicyclic alkanoyloxy-alkyl, -CH2OCOR , etc., or R may form a bond together with Y; Y forms a bond together with R or Z; Z represents hydrogen or may form a bond together with Y; and W represents oxygen or NR .
摘要翻译：通式（I）表示的DC107衍生物或其药理学上可接受的盐，各自具有抗细菌和抗肿瘤活性，其中R 1表示CO（CR 4 R 4）n1 [O（CH 2）p1] n OR 2， 5>，其中n1表示1或2的整数; R 4A和R 4B相同或不同，各自表示氢或低级烷基; p1和n2各自为1〜10的整数， R 5表示氢，低级烷基等; 或式（II）（其中A 1，A 2，A 3和A 4相同或不同，各自表示氢，羟基等）; R 2表示氢或COR 6（其中R 6表示低级烷基，芳烷基，任选取代的芳基等）; R 3表示低级烷基，低级烯基，具有任意取代的芳基的芳烷基，脂环族烷酰氧基 - 烷基，-CH 2 OCOR 7等，或R 3可与Y一起形成键; Y与R 3或Z一起形成键; Z表示氢或可与Y一起形成键; W表示氧或NR 8。

4. 发明申请

WO1998017629A1 1,4-BENZOQUINONE DERIVATIVES 审中-公开
标题翻译： 1,4-苯醌衍生物
公开(公告)号：WO1998017629A1
公开(公告)日：1998-04-30
申请号：PCT/JP1997003873
申请日：1997-10-24
申请人： KYOWA HAKKO KOGYO CO., LTD. , HAMAI, Hitomi , MAEDA, Yutaka , KANDA, Yutaka , HARA, Mitsunobu , AKASAKA, Kazuhito , AKINAGA, Shiro , MURAKATA, Chikara , IKEDA, Shun-ichi , SHONO, Kendo
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07C233/32
CPC分类号： C07D213/70 , C07C233/32 , C07C235/22 , C07C237/06 , C07C323/12 , C07C323/35 , C07C323/41 , C07C323/52 , C07C323/56 , C07D235/28 , C07D249/12 , C07D257/04 , C07D277/74 , C07D285/01 , C07D295/135 , C07D307/52
摘要： 1,4-Benzoquinone derivatives represented by general formula (I) or pharmacologically acceptable salts thereof: (I) wherein ----- represents a single or double bond; X and Y each represents hydrogen, halogeno, etc.; R and R each represents lower alkoxyl, or both represent oxygen; and R represents 2,6,10-trimethyl-1,5,9-undecatrienyl represented by formula (A) or aryloxymethyl represented by formula (B) where W represents hydrogen, halogeno, etc. The compounds have a farnesyl transferase inhibitory activity and are useful as an antitumor agent.
摘要翻译：由通式（I）表示的1,4-苯并醌衍生物或其药理学上可接受的盐：（I）其中， - - - 表示单键或双键; X和Y各自表示氢，卤素等; R 1和R 2各自表示低级烷氧基，或两者均代表氧; 和R 3代表由式（A）表示的2,6,10-三甲基-1,5,9-十一碳三烯基或由式（B）表示的芳氧基甲基，其中W表示氢，卤素等。该化合物具有法呢基转移酶抑制活性，可用作抗肿瘤剂。

5. 发明申请

WO1998009967A1 PYRROLOCARBAZOLE DERIVATIVES 审中-公开
标题翻译：吡咯烷酮衍生物
公开(公告)号：WO1998009967A1
公开(公告)日：1998-03-12
申请号：PCT/JP1997003153
申请日：1997-09-08
申请人： KYOWA HAKKO KOGYO CO., LTD. , INO, Yoji , KANAI, Fumihiko , MURAKAMI, Satoru , MURAKATA, Chikara , AKAMA, Tsutomu , SHIOTSU, Yukimasa , YAMASHITA, Kinya , AKINAGA, Shiro , TAMAOKI, Tatsuya
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Pyrrolocarbazole derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, wherein the ring (C) represents a benzene or cyclohexene ring; X and Y are the same or different and each represents carbonyl or methylene; R represents lower alkyl or aralkyl; R represents hydrogen, optionally substituted lower alkyl, lower alkenyl, or optionally substituted aralkyl; and R , R , R , R , R , R , R , R and R are the same or different and each represents hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl, halogeno, nitro, optionally substituted lower alkanoyl, NR R , OR , NHCONHR , or COR . These compounds have the effect of promoting thrombopoiesis, which makes them useful in the treatment of thrombopenia.
摘要翻译：由通式（I）表示的吡咯并咔唑衍生物或其药理学上可接受的盐，其中环（C）表示苯或环己烯环; X和Y相同或不同，各自表示羰基或亚甲基; R 1表示低级烷基或芳烷基; R 2表示氢，任选取代的低级烷基，低级烯基或任选取代的芳烷基; 和R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10和R 11是相同或不同的并且各自表示氢，任选取代的低级烷基，任选取代的低级烯基，卤代，硝基，任选取代的低级烷酰基，NR 12 R 13，OR 14，NHCONHR 16或COR 17。这些化合物具有促进血小板生成的作用，这使它们可用于治疗血小板减少症。

6. 发明申请

WO1996001263A1 PROCESS FOR PRODUCING INDOLOCARBAZOLE DERIVATIVE 审中-公开
标题翻译：用于制备吲哚胺唑衍生物的方法
公开(公告)号：WO1996001263A1
公开(公告)日：1996-01-18
申请号：PCT/JP1995001309
申请日：1995-06-30
申请人： KYOWA HAKKO KOGYO CO., LTD. , KINUGAWA, Masahiko , MASUDA, Yoshiaki , MIMURA, Yukiteru , MURAKATA, Chikara , SAITO, Hiromitsu , OGASA, Takehiro , KASAI, Masaji , TOMIOKA, Shinji
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D498/22
CPC分类号： C07D487/22 , C07D498/22
摘要： A process for producing an indolocarbazole derivative represented by general formula (II) by the acidic treatment of a silylated indolocarbazole derivative represented by general formula (VI) wherein R , R and R represent each independently lower alkyl or aryl; and R represents lower alkyl.
摘要翻译：通过酸性处理由通式（VI）表示的甲硅烷基化吲哚咔唑衍生物，其中R 1，R 2和R 3各自独立地表示低级烷基，由通式（II）表示的吲哚咔唑衍生物或芳基; R 4表示低级烷基。

7. 发明申请

WO1988007045A1 DERIVATIVES OF PHYSIOLOGICALLY ACTIVE SUBSTANCE K-252 审中-公开
标题翻译：生理活性物质K-252的衍生物
公开(公告)号：WO1988007045A1
公开(公告)日：1988-09-22
申请号：PCT/JP1987000144
申请日：1987-03-09
申请人： KYOWA HAKKO KOGYO CO., LTD. , MURAKATA, Chikara , SATO, Akira , TAKAHASHI, Mitsuru , KOBAYASHI, Eiji , MORIMOTO, Makoto , AKINAGA, Shiro , HIRATA, Tadashi , MOCHIDA, Kenichi , KASE, Hiroshi , YAMADA, Koji , IWAHASHI, Kazuyuki
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D498/22
CPC分类号： C07D498/22
摘要： Novel derivatives of K-252 ((8R*, 9S*, 11S*)-(-)-9-hydroxy-9-methoxycarbonyl-8-methyl-2,3,9,10-tetrahydro-8,11-epoxy-1H,8H,11H-2,7b,11a-triazadibenzo[a,g]cycloocta[cde]trinden-1-one) represented by formula (I) (wherein W1, W2, R1, R2, R3, R4, X, and Y represent various substituents) are disclosed. These compounds are physiologically active substances having a protein kinase C-inhibiting activity and an oncostatic activity, thus being useful as medicines.

8. 发明申请

WO1998025933A1 DC 107 DERIVATIVES (1) 审中-公开
标题翻译： DC 107衍生物（1）
公开(公告)号：WO1998025933A1
公开(公告)日：1998-06-18
申请号：PCT/JP1997004583
申请日：1997-12-12
申请人： KYOWA HAKKO KOGYO CO., LTD. , ARAI, Hitoshi , KANDA, Yutaka , YAMAGUCHI, Hiroyuki , ASHIZAWA, Tadashi , MURAKATA, Chikara , IKEDA, Shun-ichi , TAMAOKI, Tatsuya
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D513/18
CPC分类号： C07D513/18 , C07H15/26
摘要： DC 107 derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, each having antibacterial and antitumor activities, wherein R represents hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR , etc.; R represents hydrogen or COR ; R represents -CH2COOR , phthalimidomethyl, etc.; and W represents oxygen or NR (wherein R represents hydroxy, lower alkoxy, lower alkenyloxy, aralkyloxy, optionally substituted arylsulfonylamino or lower alkoxycarbonylamino).
摘要翻译：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，通式（I）表示的DC107衍生物或其药理学上可接受的盐，各自具有抗菌活性和抗肿瘤活性。等等 R 2表示氢或COR 6; R 3表示-CH 2 COOR 7，邻苯二甲酰亚氨基甲基等; W表示氧或NR 8（其中R 8表示羟基，低级烷氧基，低级烯氧基，芳烷氧基，任选取代的芳基磺酰基氨基或低级烷氧基羰基氨基）。

9. 发明申请

WO1998018780A1 RADICICOL DERIVATIVES 审中-公开
标题翻译： RADICICOL衍生物
公开(公告)号：WO1998018780A1
公开(公告)日：1998-05-07
申请号：PCT/JP1997003874
申请日：1997-10-24
申请人： KYOWA HAKKO KOGYO CO., LTD. , INO, Yoji , AMISHIRO, Nobuyoshi , MIYATA, Mayumi , MURAKATA, Chikara , OGAWA, Harumi , AKIYAMA, Tadakazu , AKINAGA, Shiro , SOGA, Shiroh , SHIOTSU, Yukimasa
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D313/00
CPC分类号： C07D493/04 , C07D313/00
摘要： Radicicol derivatives having an antityrosine kinase activity and represented by general formula (I) or pharmacologically acceptable salts thereof, wherein R and R are the same or different and each represents hydrogen, alkanoyl, alkenoyl, tert-butyldiphenylsilyl, or tert-butyldimethylsilyl; R represents Y- R {where Y represents optionally substituted alkylene, R represents CONR R (where R represents hydrogen, hydroxy, optionally substituted lower alkyl, optionally substituted higher alkyl, etc. and R represents hydroxy, substituted lower alkyl, etc.), CO2R (where R represents substituted lower alkyl, optionally substituted higher alkyl, etc.), etc.}; X represents halogeno or is bonded to R to represent a single bond; and R is bonded to X to represent a single bond or represents hydrogen alkanoyl, etc.
摘要翻译：具有抗酪氨酸激酶活性并由通式（I）表示的其它衍生物或其药学上可接受的盐，其中R 1和R 2相同或不同，各自表示氢，链烷酰基，烯酰基，叔丁基二苯基甲硅烷基或叔丁基二甲基; R 3表示Y-R 5（其中Y表示任选取代的亚烷基，R 5表示CONR 6 R 7（其中R 6表示氢，羟基，任选取代的低级烷基，任选取代的高级烷基等，R 7表示羟基，取代的低级烷基等），CO 2 R 12（其中R 12表示取代的低级烷基，任选取代的高级烷基等）等; X表示卤素或与R 4键合以表示单键; 并且R 4与X键合以表示单键或表示氢烷酰基等。

10. 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。

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