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1. 发明申请

WO1994002488A1 BIS-STAUROSPORINE AND K-252a DERIVATIVES 审中-公开
标题翻译： BIS-STAUROSPORINE和K-252a衍生物
公开(公告)号：WO1994002488A1
公开(公告)日：1994-02-03
申请号：PCT/US1993006974
申请日：1993-07-26
申请人： CEPHALON, INC. , KYOWA HAKKO KOGYO CO., LTD.
发明人： CEPHALON, INC. , KYOWA HAKKO KOGYO CO., LTD. , LEWIS, Michael, E. , NEFF, Nicola , ROBERTS-LEWIS, Jill , MURAKATA, Chikara , SAITO, Hiromitsu , MATSUDA, Yuzuru , KAUER, James, C.
IPC分类号： C07D498/22
CPC分类号： C07D487/14 , A61K31/407 , A61K31/5377 , A61K31/553 , A61K31/7056 , A61K2300/00
摘要： The invention features novel derivatives of K-252a, as well as novel bis-N-substituted derivatives of staurosporine. Also, a method for treating diseased neuronal cells involving the administration of either the novel staurosporine derivatives or specified functional derivatives of K-252a.
摘要翻译：本发明的特征在于K-252a的新衍生物以及星形孢菌素的新型双-N-取代衍生物。另外，用于治疗患有神经元细胞的方法，涉及施用新型星形孢菌素衍生物或K-252a的特定功能衍生物。

2. 发明申请

WO1996013506A1 PROTEIN KINASE INHIBITORS FOR TREATMENT OF NEUROLOGICAL DISORDERS 审中-公开
标题翻译：用于治疗神经病的蛋白激酶抑制剂
公开(公告)号：WO1996013506A1
公开(公告)日：1996-05-09
申请号：PCT/US1995012965
申请日：1995-10-04
申请人： CEPHALON, INC. , KYOWA HAKKO KOGYO CO., LTD.
发明人： CEPHALON, INC. , KYOWA HAKKO KOGYO CO., LTD. , LEWIS, Michael, E. , KAUER, James, C. , NEFF, Nicola , GLICKSMAN, Marcie , ROBERTS-LEWIS, Jill , MURAKATA, Chikara , SAITO, Hiromitsu , MATSUDA, Yuzuru , KANAI, Fumihiko , KANEKO, Masami
IPC分类号： C07D498/22
CPC分类号： C07D487/14 , A61K31/407 , A61K31/5377 , A61K31/553 , A61K31/7056 , A61K2300/00
摘要： The invention features novel derivatives of K-252a e.g. (II-4) as well as novel bis-N-substituted derivatives of staurosporine of Formula (I). The invention also features a method for treating diseased neuronal cells involving the administration of either the novel staurosporine derivatives or specified functional derivatives of K-252a. In the formula (I): [Stau] -N(CH3)-W-N(CH3)-[Stau], [Stau] represents a residue of formula (a) and W represents a radical of the formula: -C(=Y)-NH-W'-NH-C(=Y)- where W' is a hydrocarbylene radical of 2-20 carbon atoms and Y is O or S. In formula (II-4) R , R , Z , and Z are each H; X is CH2OH; and R is OCH3.
摘要翻译：本发明具有K-252a的新型衍生物，例如（II-4）以及式（I）的星形孢菌素的新型双-N-取代衍生物。本发明还涉及一种用于治疗患有神经元细胞的方法，涉及施用新型星形孢菌素衍生物或K-252a的特定功能衍生物。在式（I）中：[Stau] -N（CH 3）-WN（CH 3） - [Stau]，[Stau]表示式（a）的残基，W表示下式的基团-C（= Y ）-NH-W'-NH-C（= Y） - 其中W'是2-20个碳原子的亚烃基，Y是O或S.在式（II-4）中，R 1，R 2 ，Z 1和Z 2各自为H; X是CH 2 OH; 和R是OCH 3。

3. 发明公开

EP1092435A1 REMEDIES FOR DIABETES 有权
标题翻译：抗炎药物MEDIKAMENTE
公开(公告)号：EP1092435A1
公开(公告)日：2001-04-18
申请号：EP99926903.8
申请日：1999-07-02
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： SHIMADA, Junichi , OHTA, Yoshihisa , TAKASAKI, Kotaro , SUDA, Miho , KUSAKA, Hideaki , YANO, Hiroshi , NAKANISHI, Satoshi , MATSUDA, Yuzuru
IPC分类号： A61K31/505
CPC分类号： C07D487/14 , A61K31/505 , A61K31/519 , Y10S514/866
摘要： A medicament for the therapeutic treatment of diabetes which comprises as an active ingredient a compound represented by the general formula (I):
wherein R 1 represents a hydrogen atom, a lower alkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aromatic heterocyclic group, R 2 represents a hydrogen atom, a lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aromatic heterocyclic group, R 3 represents a hydrogen atom, a lower alkyl group or a substituted or unsubstituted aralkyl group, X 1 and X 2 independently represent a hydrogen atom, a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group, and the symbol "n" represents an integer of from 0 to 3, or a physiologically acceptable salt thereof.
摘要翻译：一种用于治疗糖尿病的药物，其包含作为活性成分的由通式（I）表示的化合物：其中R 1表示氢原子，低级烷基，取代或未取代的芳基，或取代或未取代的芳族杂环基，R 2表示氢原子，低级烷基，取代或未取代的芳烷基，取代或未取代的芳基或取代或未取代的芳族杂环基，R 3，表示氢原子，低级烷基或取代或未取代的芳烷基，X 1和X 2独立地表示氢原子，低级烷基，取代或未取代的芳烷基或取代或未取代的芳基组，符号“n”表示0〜3的整数，或其生理上可接受的盐。

4. 发明公开

EP0832983A1 PHYSIOLOGICALLY ACTIVE SUBSTANCE EI-2128-1 失效
标题翻译：生理学基础物质EI-2128-1
公开(公告)号：EP0832983A1
公开(公告)日：1998-04-01
申请号：EP97914580.2
申请日：1997-04-02
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： TANAKA, Takeo , KOIZUMI, Fumito , AGATSUMA, Tsutomu , KONDO, Hidemasa , SAITOH, Yutaka , ANDO, Katsuhiko , MATSUDA, Yuzuru
IPC分类号： C12P17/04 , C07D493/20
CPC分类号： C07D493/20 , C12P17/181
摘要： A novel compound EI-2128-1 represented by formula (I) and having an IL-1 production inhibitory effect.
摘要翻译：由式（I）表示的具有IL-1产生抑制作用的新化合物EI-2128-1。

5. 发明授权

EP0788501B1 PROTEIN KINASE INHIBITORS FOR TREATMENT OF NEUROLOGICAL DISORDERS 失效
标题翻译：蛋白激酶C抑制剂用于治疗神经疾病的治疗
公开(公告)号：EP0788501B1
公开(公告)日：2002-06-05
申请号：EP95937391.1
申请日：1995-10-04
申请人： CEPHALON, INC. , KYOWA HAKKO KOGYO CO., LTD.
发明人： LEWIS, Michael, E. , KAUER, James, C. , NEFF, Nicola , GLICKSMAN, Marcie , ROBERTS-LEWIS, Jill , MURAKATA, Chikara , SAITO, Hiromitsu , MATSUDA, Yuzuru , KANAI, Fumihiko , KANEKO, Masami
IPC分类号： C07D498/22 , A61K31/55 , C07D487/14 , A61K31/40
CPC分类号： C07D487/14 , A61K31/407 , A61K31/5377 , A61K31/553 , A61K31/7056 , A61K2300/00
摘要： The invention features novel derivatives of K-252a e.g. (II-4) as well as novel bis-N-substituted derivatives of staurosporine of Formula (I). The invention also features a method for treating diseased neuronal cells involving the administration of either the novel staurosporine derivatives or specified functional derivatives of K-252a. In the formula (I): [Stau] -N(CH3)-W-N(CH3)-[Stau], [Stau] represents a residue of formula (a) and W represents a radical of the formula: -C(=Y)-NH-W'-NH-C(=Y)- where W' is a hydrocarbylene radical of 2-20 carbon atoms and Y is O or S. In formula (II-4) R?1, R2, Z1, and Z2¿ are each H; X is CH¿2?OH; and R is OCH3.

6. 发明授权

EP1092435B1 REMEDIES FOR DIABETES 有权
标题翻译：抗糖尿病药物
公开(公告)号：EP1092435B1
公开(公告)日：2007-04-04
申请号：EP99926903.8
申请日：1999-07-02
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： SHIMADA, Junichi , OHTA, Yoshihisa , TAKASAKI, Kotaro , SUDA, Miho , KUSAKA, Hideaki , YANO, Hiroshi , NAKANISHI, Satoshi , MATSUDA, Yuzuru
IPC分类号： A61K31/505 , A61K31/519 , C07D487/14
CPC分类号： C07D487/14 , A61K31/505 , A61K31/519 , Y10S514/866
摘要： Remedies for diabetes which contain as the active ingredient compounds represented by general formula (I) or physiologically acceptable salts thereof wherein R1 represents hydrogen, lower alkyl, optionally substituted aryl or optionally substituted heteroaryl; R2 represents hydrogen, lower alkyl, optionally substituted aralkyl, optionally substituted aryl or optionally substituted heteroaryl; R3 represents hydrogen, lower alkyl or optionally substituted aralkyl; X?1 and X2¿ independently represent each hydrogen, lower alkyl, optionally substituted aralkyl or optionally substituted aryl; and n is an integer of from 0 to 3.

7. 发明公开

EP0610519A1 ANTI-HIV DRUG 失效
标题翻译：抗HIV-MEDIKAMENT。
公开(公告)号：EP0610519A1
公开(公告)日：1994-08-17
申请号：EP94908806.6
申请日：1993-08-20
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： YANO, Hiroshi , NAKANISHI, Satoshi , MATSUDA, Yuzuru , NONOMURA, Yoshiaki , SASAKI, Hiroyuki
IPC分类号： A61K31/34 , A61K31/365 , C07D307/92 , C07D493/06
CPC分类号： A61K31/365 , A61K31/00 , A61K31/34
摘要： An anti-HIV drug containing a myosin light-chain kinase inhibitor such as wortmannin or MS-444 as the active ingredient.
摘要翻译：含有肌球蛋白轻链激酶抑制剂如渥曼青霉素或MS-444的抗HIV药物作为活性成分。

8. 发明授权

EP0610519B1 ANTI-HIV DRUG 失效
标题翻译：抗艾滋病药物
公开(公告)号：EP0610519B1
公开(公告)日：1999-12-01
申请号：EP94908806.6
申请日：1993-08-20
申请人： KYOWA HAKKO KOGYO CO., Ltd.
发明人： YANO, Hiroshi , NAKANISHI, Satoshi , MATSUDA, Yuzuru , NONOMURA, Yoshiaki , SASAKI, Hiroyuki
IPC分类号： A61K31/34 , A61K31/365 , C07D307/92 , C07D493/06 , A61K31/00
CPC分类号： A61K31/365 , A61K31/00 , A61K31/34

9. 发明公开

EP0788501A1 PROTEIN KINASE INHIBITORS FOR TREATMENT OF NEUROLOGICAL DISORDERS 失效
标题翻译：蛋白激酶C抑制剂用于治疗神经疾病的治疗
公开(公告)号：EP0788501A1
公开(公告)日：1997-08-13
申请号：EP95937391.0
申请日：1995-10-04
申请人： CEPHALON, INC. , KYOWA HAKKO KOGYO CO., LTD.
发明人： LEWIS, Michael, E. , KAUER, James, C. , NEFF, Nicola , GLICKSMAN, Marcie , ROBERTS-LEWIS, Jill , MURAKATA, Chikara , SAITO, Hiromitsu , MATSUDA, Yuzuru , KANAI, Fumihiko , KANEKO, Masami
IPC分类号： A61K31 , A61K38 , A61P9 , A61P25 , A61P31 , C07D487 , C07D498 , C07D519
CPC分类号： C07D487/14 , A61K31/407 , A61K31/5377 , A61K31/553 , A61K31/7056 , A61K2300/00
摘要： The invention features novel derivatives of K-252a e.g. (II-4) as well as novel bis-N-substituted derivatives of staurosporine of Formula (I). The invention also features a method for treating diseased neuronal cells involving the administration of either the novel staurosporine derivatives or specified functional derivatives of K-252a. In the formula (I): [Stau] -N(CH3)-W-N(CH3)-[Stau], [Stau] represents a residue of formula (a) and W represents a radical of the formula: -C(=Y)-NH-W'-NH-C(=Y)- where W' is a hydrocarbylene radical of 2-20 carbon atoms and Y is O or S. In formula (II-4) R?1, R2, Z1, and Z2¿ are each H; X is CH¿2?OH; and R is OCH3.

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