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1. 发明授权

US5604219A Indolocarbazole derivatives that stimulate platelet production 失效
标题翻译：刺激血小板生成的吲哚咔唑衍生物
公开(公告)号：US5604219A
公开(公告)日：1997-02-18
申请号：US404961
申请日：1995-03-16
申请人： Chikara Murakata , Junichi Watanabe , Yutaka Saitoh , Yukimasa Shiotsu , Takako Shiraki , Fumihiko Kanai , Tatsuya Tamaoki , Shiro Akinaga , Masami Okabe
发明人： Chikara Murakata , Junichi Watanabe , Yutaka Saitoh , Yukimasa Shiotsu , Takako Shiraki , Fumihiko Kanai , Tatsuya Tamaoki , Shiro Akinaga , Masami Okabe
IPC分类号： C07D498/22 , C07H9/06 , A61K31/55
CPC分类号： C07D498/22 , C07H9/06
摘要： Disclosed is an indolocarbazole derivative represented by the following formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## [wherein R.sup.1 represents substituted or unsubstituted lower alkyl, R.sup.2 represents hydrogen, substituted or unsubstituted lower alkyl, R.sup.3 and R.sup.4 are the same or different, and represent hydrogen, nitro, NR.sup.5 R.sup.6, OR.sup.9, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl, or CH.dbd.NNR.sup.10 R.sup.11, W represents two hydrogen atoms or oxygen, and Me represents methyl, provided that when R.sup.1 is unsubstituted lower alkyl, R.sup.3 and R.sup.4 are not simultaneously hydrogen.
摘要翻译：公开了下式（I）表示的吲哚咔唑衍生物或其药学上可接受的盐：其中R 1表示取代或未取代的低级烷基，R 2表示氢，取代或未取代的低级烷基，R 3和R 4 代表氢，硝基，NR5R6，OR9，取代或未取代的低级烷基，取代或未取代的低级链烯基或CH = NNR10R11，W代表两个氢原子或氧，Me代表甲基，条件是当R 1 未取代的低级烷基，R3和R4不同时为氢。

2. 发明授权

US5629304A Therapeutic agent for thrombocytopenia and indolocarbazole derivatives 失效
标题翻译：血小板减少症和吲哚并咔唑衍生物的治疗剂
公开(公告)号：US5629304A
公开(公告)日：1997-05-13
申请号：US637590
申请日：1996-04-25
申请人： Chikara Murakata , Fumihiko Kanai , Yutaka Saitoh , Yukimasa Shiotsu , Takako Shiraki , Tatsuya Tamaoki , Shiro Akinaga , Masami Okabe
发明人： Chikara Murakata , Fumihiko Kanai , Yutaka Saitoh , Yukimasa Shiotsu , Takako Shiraki , Tatsuya Tamaoki , Shiro Akinaga , Masami Okabe
IPC分类号： A61K31/40 , A61K31/404 , A61K31/407 , A61K31/415 , A61K31/4178 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5377 , C07D403/14 , C07D487/14 , C07D487/12
CPC分类号： C07D403/14 , A61K31/40 , A61K31/404 , A61K31/407 , A61K31/415 , A61K31/4178 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5377 , C07D487/14
摘要： The present invention provides a method of treating thrombocytopenia, which comprises administering to a patient suffering from thrombocytopenia, an effective amount of an indolocarbazole derivative represented by formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group or a tetrahydropyranyl group; R.sup.2A and R.sup.3A, which may be the same or different, each represent a hydrogen atom, a substituted or unsubstituted lower alkyl group, a lower alkenyl group, a substituted or unsubstituted aralkyl group or a monosaccharide residue where a hydroxyl group at the anomer position is removed; R.sup.4A and R.sup.5A, which may be the same or different, each represent a hydrogen atom, a formyl group, a hydroxyl group or a halogen atom; W.sup.A1 and W.sup.A2 represent hydrogen atoms or are combined together to form an oxygen atom; and X.sup.A1 and X.sup.A2 represents two hydrogen atoms or are combined together to form a single bond, provided that when X.sup.A forms a single bond, then R.sup.1, R.sup.2A, R.sup.3A, R.sup.4A, R.sup.5A, and W.sup.A do not simultaneously represent a hydrogen atom, or a pharmaceutically acceptable salt.
摘要翻译：本发明提供一种治疗血小板减少症的方法，其包括向患有血小板减少症的患者施用有效量的由式（I）表示的吲哚并咔唑衍生物：其中R 1表示氢原子，取代或未取代的低级烷基，取代或未取代的芳烷基或四氢吡喃基; R2A和R3A可以相同或不同，分别表示氢原子，取代或未取代的低级烷基，低级链烯基，取代或未取代的芳烷基或单末端残基，其中前体位置的羟基为删除 R4A和R5A可以相同或不同，分别表示氢原子，甲酰基，羟基或卤素原子; WA1和WA2表示氢原子，或者组合在一起形成氧原子; 并且XA1和XA2表示两个氢原子，或者组合在一起形成单键，条件是当XA形成单键时，则R1，R2A，R3A，R4A，R5A和WA不同时表示氢原子，或药学上可接受的盐。

3. 发明授权

US5674867A Indolocarbazole derivatives and therapeutic method for stimulating megakaicyocyte production 失效
标题翻译：吲哚咯唑衍生物和刺激巨核细胞产生的治疗方法
公开(公告)号：US5674867A
公开(公告)日：1997-10-07
申请号：US244111
申请日：1994-05-18
申请人： Tatsuya Tamaoki , Yukimasa Shiotsu , Chikara Murakata , Shiro Akinaga , Masami Okabe , Yutaka Saito , Junichi Watanabe , Takako Shiraki
发明人： Tatsuya Tamaoki , Yukimasa Shiotsu , Chikara Murakata , Shiro Akinaga , Masami Okabe , Yutaka Saito , Junichi Watanabe , Takako Shiraki
IPC分类号： C07D498/22 , C07H9/06 , C07H19/044 , A61K31/55
CPC分类号： C07D498/22 , C07H19/044 , C07H9/06
摘要： The present invention relates to therapeutic agents for thrombocytopenia which contain an indolocarbazole derivative represented by the formula (I) given below or a pharmaceutically acceptable salt thereof as an active ingredient, and to novel indolocarbazole derivatives. ##STR1##
摘要翻译： PCT No.PCT / JP93 / 01346 Sec。 371日期：1994年5月18日 102（e）日期1994年5月18日PCT提交1993年9月20日PCT公布。第WO94 / 06799号公报日期：1994年3月3日本发明涉及血小板减少症治疗剂，其含有下述式（I）表示的吲哚并咔唑衍生物或其药学上可接受的盐作为活性成分，以及新的吲哚并咔唑衍生物。（一）

4. 发明授权

US5344926A Process for producing staurosporine derivatives 失效
标题翻译：生产星形孢菌素衍生物的方法
公开(公告)号：US5344926A
公开(公告)日：1994-09-06
申请号：US79560
申请日：1993-06-22
申请人： Chikara Murakata , Toshimitsu Takiguchi , Shigeo Katsumata , Akira Mihara , Keiichi Takahashi , Hiromitsu Saito , Shiro Akinaga , Masami Okabe , Yutaka Saito
发明人： Chikara Murakata , Toshimitsu Takiguchi , Shigeo Katsumata , Akira Mihara , Keiichi Takahashi , Hiromitsu Saito , Shiro Akinaga , Masami Okabe , Yutaka Saito
IPC分类号： C07D498/22 , C07H9/06 , C07H19/04
CPC分类号： C07D498/22 , C07H19/04 , C07H9/06
摘要： Disclosed is a process for producing a staurosporine derivative represented by Formula (I): Q is defined as in specification: ##STR1## The staurosporine derivative (I-1) possesses selective protein kinase C-inhibitory and cell growth-inhibiting activities, and platelet-increasing activity.
摘要翻译：（I）星形孢菌素衍生物（I-1）具有选择性蛋白激酶C抑制和细胞生长抑制活性的方法，，血小板增多活性。

5. 发明授权

US5565489A Epoxycyclohexenedione derivatives 失效
标题翻译：环氧环己烯二酮衍生物
公开(公告)号：US5565489A
公开(公告)日：1996-10-15
申请号：US436359
申请日：1995-05-18
申请人： Masami Kaneko , Yutaka Saitoh , Shiro Akinaga , Masami Okabe , Kazuhito Akasaka , Hirofumi Nakano
发明人： Masami Kaneko , Yutaka Saitoh , Shiro Akinaga , Masami Okabe , Kazuhito Akasaka , Hirofumi Nakano
IPC分类号： C07D303/36 , A61K31/335 , C07D303/02
CPC分类号： C07D303/36
摘要： The present invention relates to an epoxycyclohexenedione derivative represented by formula (I): ##STR1## wherein R is a straight-chain or branched alkanoyl group having 10 to 25 carbon atoms, a straight-chain alkenoyl group having 10 to 25 carbon atoms, or a group represented by formula (A): ##STR2## wherein n is an integer of 1 to 4; or a pharmaceutically acceptable salt thereof.The compounds exhibit antimicrobial activity and antitumor activity.
摘要翻译： PCT No.PCT / JP94 / 01542 Sec。 371日期1995年5月18日 102（e）日期1995年5月18日PCT 1994年9月20日PCT公布。公开号WO95 / 08546 日期：1995年3月30日本发明涉及式（I）表示的环氧环己烯二酮衍生物：其中R为碳原子数为10〜25的直链或支链烷酰基，直链烯酰基具有10至25个碳原子，或由式（A）表示的基团：其中n为1至4的整数; 或其药学上可接受的盐。该化合物表现出抗微生物活性和抗肿瘤活性。

6. 发明授权

US06291694B1 Process and intermediates useful to produce vitamin D analogs 失效
标题翻译：用于生产维生素D类似物的方法和中间体
公开(公告)号：US06291694B1
公开(公告)日：2001-09-18
申请号：US09633670
申请日：2000-08-07
申请人： Andrzej Robert Daniewski , Marek Michal Kabat , Masami Okabe , Roumen Nikolaev Radinov
发明人： Andrzej Robert Daniewski , Marek Michal Kabat , Masami Okabe , Roumen Nikolaev Radinov
IPC分类号： C07C40100
CPC分类号： C07C69/732 , C07D303/32 , C07D303/40 , C07F7/1804 , C07F7/1892
摘要： A stereospecific method for accomplishing the below reaction: results in the compound of formula 2 having the same stereochemistry at both carbon 1 and carbon 3 as that in the compound of formula 1. Thus, if carbon 3 is in the R-configuration in the compound of formula 1, then carbon 3 will be in the R-configuration in the compound of resulting formula 2. In the above process, R1 is C1-C6 alkyl that can be straight-chain or branched. The process functions using a fluorinated alcohol having a pKa less than about 9, in the presence of a palladium catalyst. The compounds of formula 1, as well as novel intermediates in this process, are useful in manufacturing vitamin D analogs.
摘要翻译：用于实现以下反应的立体特异性方法：导致式2的化合物在碳1和碳3上与式1化合物具有相同的立体化学性质。因此，如果碳3在化合物中为R-构型式3的化合物中的碳原子为R构型。在上述方法中，R 1是可以是直链或支链的C 1 -C 6烷基。该方法在钯催化剂存在下使用pKa小于约9的氟化醇来进行。式1的化合物以及该方法中的新型中间体可用于制备维生素D类似物。

7. 发明授权

US06294688B1 Process useful to produce vitamin D analogs 失效
标题翻译：生产维生素D类似物的方法
公开(公告)号：US06294688B1
公开(公告)日：2001-09-25
申请号：US09633672
申请日：2000-08-07
申请人： Andrzej Robert Daniewski , Marek Michal Kabat , Masami Okabe , Roumen Nikolaev Radinov
发明人： Andrzej Robert Daniewski , Marek Michal Kabat , Masami Okabe , Roumen Nikolaev Radinov
IPC分类号： C07C6726
CPC分类号： C07C69/732 , C07D303/32 , C07D303/40 , C07F7/1804 , C07F7/1892
摘要： A stereospecific method for accomplishing the below reaction: results in the compound of formula 2 having the same stereochemistry at both carbon 1 and carbon 3 as that in the compound of formula 1. Thus, if carbon 3 is in the R-configuration in the compound of formula 1, then carbon 3 will be in the R-configuration in the compound of resulting formula 2. In the above process, R1 is C1-C6 alkyl that can be straight-chain or branched. The process functions using a fluorinated alcohol having a pKa less than about 9, in the presence of a palladium catalyst. The compounds of formula 1, as well as novel intermediates in this process, are useful in manufacturing vitamin D analogs.
摘要翻译：用于实现以下反应的立体特异性方法：导致式2的化合物在碳1和碳3上与式1化合物具有相同的立体化学性质。因此，如果碳3在化合物中为R-构型式3的化合物中的碳原子为R构型。在上述方法中，R 1是可以是直链或支链的C 1 -C 6烷基。该方法在钯催化剂存在下使用pKa小于约9的氟化醇来进行。式1的化合物以及该方法中的新型中间体可用于制备维生素D类似物。

8. 发明授权

US06245900B1 Platelet production promoting agent 失效
标题翻译：血小板生产促进剂
公开(公告)号：US06245900B1
公开(公告)日：2001-06-12
申请号：US08696988
申请日：1996-08-16
申请人： Motoo Yamasaki , Masami Okabe , Toshiyuki Suzawa , Ken Kobayashi , Kumiko Maruyama
发明人： Motoo Yamasaki , Masami Okabe , Toshiyuki Suzawa , Ken Kobayashi , Kumiko Maruyama
IPC分类号： A61K3819
CPC分类号： C07K14/535 , A61K38/00
摘要： The invention relates to a polypeptide wherein at least one of the amino, carboxyl, mercapto or guanidino group in a polypeptide molecule having human granulocyte colony stimulating factor activity is chemically modified by a chemical modifying agent, and a platelet production promoter comprising said polypeptide, a method for treating a patient with decreased platelet counts comprising administering an effective amount of said polypeptide to the patient, the use of said polypeptide for the production of pharmaceutical compositions which are useful for the treatment of the patient with decreased platelet counts, and the compositions for treating the patient with decreased platelet counts, which comprises an effective dose of said polypeptide in a pharmaceutically acceptable dosage form with a pharmaceutical acceptable carrier.
摘要翻译：本发明涉及一种多肽，其中具有人粒细胞集落刺激因子活性的多肽分子中的氨基，羧基，巯基或胍基中的至少一个被化学修饰剂化学修饰，并且包含所述多肽的血小板产生启动子，用于治疗血小板计数降低的患者的方法包括向患者施用有效量的所述多肽，所述多肽用于制备可用于治疗血小板计数减少的患者的药物组合物的用途，以及用于用减少的血小板计数治疗患者，其包含药学上可接受的剂型中的有效剂量的所述多肽与药学上可接受的载体。

9. 发明授权

US5795968A Polypeptide derivatives of human granulocyte colony stimulating factor 失效
标题翻译：人粒细胞集落刺激因子的多肽衍生物
公开(公告)号：US5795968A
公开(公告)日：1998-08-18
申请号：US783288
申请日：1997-01-10
申请人： Tetsuro Kuga , Hiromasa Miyaji , Moriyuki Sato , Masami Okabe , Makoto Morimoto , Seiga Itoh , Motoo Yamasaki , Yoshiharu Yokoo , Kazuo Yamaguchi , Hajime Yoshida , Yoshinori Komatsu
发明人： Tetsuro Kuga , Hiromasa Miyaji , Moriyuki Sato , Masami Okabe , Makoto Morimoto , Seiga Itoh , Motoo Yamasaki , Yoshiharu Yokoo , Kazuo Yamaguchi , Hajime Yoshida , Yoshinori Komatsu
IPC分类号： A61K38/00 , C07K1/107 , C07K1/113 , C07K1/12 , C07K14/535 , C07K16/24 , C07K17/06 , C12N15/70
CPC分类号： C07K1/1077 , C07K1/113 , C07K14/535 , C07K16/243 , C07K17/06 , C12N15/70 , A61K38/00
摘要： Novel hG-CSF polypeptide derivatives having an amino acid sequence derived from the amino acid sequence of the human granulocyte colony stimulating factor polypeptide by substitution of at least one amino acid by a different amino acid and/or deletion of at least one amino acid, recombinant plasmids containing a DNA fragment insert coding for any of these hG-CSF polypeptide derivatives, microorganisms carrying one of such plasmids, methods of producing the hG-CSF polypeptide derivatives using the microorganisms, a monoclonal antibody binding to the hG-CSF polypeptide derivative, and chemically modified hG-CSF or derivatives thereof are disclosed.
摘要翻译：具有衍生自人粒细胞集落刺激因子多肽的氨基酸序列的氨基酸序列的新型hG-CSF多肽衍生物通过用不同氨基酸取代至少一个氨基酸和/或缺失至少一个氨基酸，重组体含有编码这些hG-CSF多肽衍生物中的任何一种的DNA片段插入片段的质粒，携带这种质粒之一的微生物，使用微生物生产hG-CSF多肽衍生物的方法，与hG-CSF多肽衍生物结合的单克隆抗体，以及公开了化学修饰的hG-CSF或其衍生物。

10. 发明申请

US20060040865A1 Platelet production promoting agent 有权
公开(公告)号：US20060040865A1
公开(公告)日：2006-02-23
申请号：US11253617
申请日：2005-10-20
申请人： Motoo Yamasaki , Masami Okabe , Toshiyuki Suzawa , Ken Kobayashi , Kumiko Maruyama
发明人： Motoo Yamasaki , Masami Okabe , Toshiyuki Suzawa , Ken Kobayashi , Kumiko Maruyama
IPC分类号： A61K38/17 , C07K14/47
CPC分类号： C07K14/535 , A61K38/00
摘要： The invention relates to a polypeptide wherein at least one of the amino, carboxyl, mercapto or guanidino group in a polypeptide molecule having human granulocyte colony stimulating factor activity is chemically modified by a chemical modifying agent, and a platelet production promoter comprising said polypeptide, a method for treating a patient with decreased platelet counts comprising administering an effective amount of said polypeptide to the patient, the use of said polypeptide for the production of pharmaceutical compositions which are useful for the treatment of the patient with decreased platelet counts, and the compositions for treating the patient with decreased platelet counts, which comprises an effective dose of said polypeptide in a pharmaceutically acceptable dosage form with a pharmaceutical acceptable carrier.

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