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1. 发明授权

US06545151B2 Pentacyclic compound 有权
标题翻译：五环化合物
公开(公告)号：US06545151B2
公开(公告)日：2003-04-08
申请号：US09759378
申请日：2001-01-16
申请人： Hirofumi Terasawa , Tsunehiko Soga , Takashi Ishiyama
发明人： Hirofumi Terasawa , Tsunehiko Soga , Takashi Ishiyama
IPC分类号： C07D49308
CPC分类号： C07D493/08 , C07D305/14
摘要： The present invention relates to a novel taxol derivative having an antitumor-activity which is represented by formula (1). [In the formula (I), R1: a phenyl group, R2: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R3: a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group —O—R31, an acyloxy group or a group —O—CO—R31 (in which R31: an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R4 and R5: a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z1: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z2: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z3: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group].
摘要翻译：本发明涉及由式（1）表示的具有抗肿瘤活性的新型紫杉醇衍生物[式（I）中，R 1为苯基，R 2为烷基，烯基，炔基，环烷基或烷氧基，R3：氢原子，羟基，卤素原子，烷氧基，-O-R31基，酰氧基或-O-CO-R31基（其中R31 ：烷基氨基，烯基，炔基，环烷基，芳基或杂环基），R4和R5：氢原子，烷基，烯基，炔基，芳基或杂环基，Z 1：氢原子，羟基，卤原子或烷基，Z 2：氢原子，羟基，卤素原子或烷基，Z 3：烷基，烯基，炔基，环烷基，芳基或杂环基]。

2. 发明授权

US06646123B2 Pentacyclic Compound 失效
标题翻译：五环化合物
公开(公告)号：US06646123B2
公开(公告)日：2003-11-11
申请号：US10126653
申请日：2002-04-22
申请人： Hirofumi Terasawa , Tsunehiko Soga , Takashi Ishiyama
发明人： Hirofumi Terasawa , Tsunehiko Soga , Takashi Ishiyama
IPC分类号： C07D49308
CPC分类号： C07D493/08 , C07D305/14
摘要： The present invention relates to a novel taxol derivative having an antitumor activity which is represented by formula (1). [In the formula (I), R1: a phenyl group, R2: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R3: a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group —O—R311 an acyloxy group or a group —O—CO—R31, (in which R31: an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R4 and R5: a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z1: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z2: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z3: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group].
摘要翻译：本发明涉及由式（1）表示的具有抗肿瘤活性的新型紫杉醇衍生物[在式（I）中，R 1：苯基，R 2：烷基，烯基基团，炔基，环烷基或烷氧基，R 3：氢原子，羟基，卤素原子，烷氧基，基团-OR 31，酰氧基或基团， O-CO-R 31（其中R 31：烷基氨基，烯基，炔基，环烷基，芳基或杂环基），R 4和R 5 >：氢原子，烷基，烯基，炔基，芳基或杂环基，Z 1：氢原子，羟基，卤素原子或烷基，Z 2 >：氢原子，羟基，卤素原子或烷基，Z 3：烷基，烯基，炔基，环烷基，芳基或杂环基]。

3. 发明授权

US06211363B1 Pentacyclic compound 有权
标题翻译：五环化合物
公开(公告)号：US06211363B1
公开(公告)日：2001-04-03
申请号：US09513852
申请日：2000-02-25
申请人： Hirofumi Terasawa , Tsunehiko Soga , Takashi Ishiyama
发明人： Hirofumi Terasawa , Tsunehiko Soga , Takashi Ishiyama
IPC分类号： C07D49308
CPC分类号： C07D493/08 , C07D305/14
摘要： The present invention relates to a novel taxol derivative having an antitumor-activity which is represented by formula (1). [In the formula (I), R1: a phenyl group, R2: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R3: a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group —O—R31, an acyloxy group or a group —O—CO—R31, (in which R31: an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R4 and R5: a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z1: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z2: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z3: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group].
摘要翻译：本发明涉及由式（1）表示的具有抗肿瘤活性的新型紫杉醇衍生物[式（I）中，R 1为苯基，R 2为烷基，烯基，炔基，环烷基或烷氧基，R3：氢原子，羟基，卤素原子，烷氧基，-O-R31基，酰氧基或-O-CO-R31基（其中 R 31：烷基氨基，烯基，炔基，环烷基，芳基或杂环基），R 4和R 5：氢原子，烷基，烯基，炔基，芳基或杂环基，Z1：氢原子，羟基，卤素原子或烷基，Z2：氢原子，羟基，卤素原子或烷基，Z3：烷基，烯基，炔基，环烷基，芳基或杂环基]。

4. 发明授权

US6075140A Pentacyclic compound 失效
标题翻译：五环化合物
公开(公告)号：US6075140A
公开(公告)日：2000-06-13
申请号：US945276
申请日：1998-02-05
申请人： Hirofumi Terasawa , Tsunehiko Soga , Takashi Ishiyama
发明人： Hirofumi Terasawa , Tsunehiko Soga , Takashi Ishiyama
IPC分类号： C07D305/14 , C07D493/08
CPC分类号： C07D493/08 , C07D305/14
摘要： The present invention relates to a novel taxol derivative having an antitumor activity which is represented by formula (1). ##STR1## [In the formula (I), R.sup.1 : a phenyl group, R.sup.2 : an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R.sup.3 : a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group --O--R.sup.31, an acyloxy group or a group --O--CO--R.sup.31, (in which R.sup.31 : an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R.sup.4 and R.sup.5 : a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z.sup.1 : a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z.sup.2 : a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z.sup.3 : an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group].
摘要翻译： PCT No.PCT / JP96 / 01145 Sec。 371日期：1998年2月5日 102（e）1998年2月5日PCT 1996年4月25日PCT PCT。出版物WO96 / 33998 日期：1996年10月31日本发明涉及由式（1）表示的具有抗肿瘤活性的新型紫杉醇衍生物。 [式（I）中，R 1为苯基，R 2为烷基，烯基，炔基，环烷基或烷氧基，R 3为氢原子，羟基，卤素原子，烷氧基，基团-O-R31，酰氧基或基团-O-CO-R31（其中R31：烷基氨基，烯基，炔基，环烷基，芳基或杂环基），R4和R5：氢原子，烷基，烯基，炔基，芳基或杂环基，Z1：氢原子，羟基，卤素原子或烷基， Z2：氢原子，羟基，卤原子或烷基，Z3：烷基，烯基，炔基，环烷基，芳基或杂环基）。

5. 发明授权

US5767296A Deacetoxytaxol derivatives 失效
标题翻译：脱乙酰氧基紫杉醇衍生物
公开(公告)号：US5767296A
公开(公告)日：1998-06-16
申请号：US750374
申请日：1996-12-06
申请人： Hirofumi Terasawa , Tsunehiko Soga , Kiyoshi Nakayama
发明人： Hirofumi Terasawa , Tsunehiko Soga , Kiyoshi Nakayama
IPC分类号： C07D305/14 , C07D407/12
CPC分类号： C07D407/12 , C07D305/14
摘要： A novel taxol derivative having the formula (I), in which the 10-position is modified to have a carbon-carbon bond, is disclosed. The taxol derivative of the present invention has an antitumor activity. ##STR1##
摘要翻译： PCT No.PCT / JP95 / 01163 Sec。 371日期1996年12月6日第 102（e）日期1996年12月6日PCT Filed 1995年6月9日PCT公布。第WO95 / 33740号公报 1995年12月14日，公开了具有式（I）的新型紫杉醇衍生物，其中10位被改性为具有碳 - 碳键。本发明的紫杉酚衍生物具有抗肿瘤活性。（一）

6. 发明授权

US4028070A Method of recovering ethylene oxide 失效
标题翻译：回收环氧乙烷的方法
公开(公告)号：US4028070A
公开(公告)日：1977-06-07
申请号：US638841
申请日：1975-12-08
申请人： Jiro Uchii , Masatsugu Kodo , Tsunehiko Soga , Yutaka Morimoto
发明人： Jiro Uchii , Masatsugu Kodo , Tsunehiko Soga , Yutaka Morimoto
IPC分类号： B01D19/00 , B01D19/04
CPC分类号： B01D19/0005 , B01D19/0409
摘要： A method of recovering ethylene oxide from the reaction product gas that is obtained by the catalytic vapor phase oxidation of ethylene with molecular oxygen over a silver-containing catalyst, which comprises conducting the reaction product gas to an absorption column maintained at a pressure in the range of 2 - 40 kg/cm.sup.2, countercurrently contacting reaction product gas with an aqueous absorbent in the absorption column to dissolve ethylene oxide in the aqueous absorbent to form an aqueous ethylene oxide solution, conducting the thus formed aqueous solution to a stripping column, stripping and recovering ethylene oxide from aqueous ethylene oxide solution at the stripping column, and thereafter recycling the remaining aqueous solution which is obtained after stripping ethylene oxide to the absorption column to be again used as the aqueous absorbent; characterized by using as the aqueous absorbent one containing ethylene glycol in the range of 0.1 - 40% by weight and a defoaming agent in the range of 0.5 - 1000 ppm and having a pH in the range of 3 - 12.
摘要翻译：从通过在含银催化剂上分子氧的乙烯的催化气相氧化获得的反应产物气体中回收环氧乙烷的方法，其包括将反应产物气体导入保持在该范围内的压力的吸收塔 2-40kg / cm 2，将反应产物气体与吸收塔中的含水吸收剂逆流接触以溶解含水吸收剂中的环氧乙烷以形成环氧乙烷水溶液，将由此形成的水溶液导入汽提塔，汽提和在汽提塔处从环氧乙烷水溶液中回收环氧乙烷，然后将汽提环氧乙烷后得到的剩余水溶液再循环到吸收塔，再次用作水性吸收剂; 其特征在于使用含有0.1-40重量％的乙二醇和0.5-1000ppm范围内的消泡剂并且pH在3-12范围内的含水吸收剂。

7. 发明申请

US20090312310A1 Imidazothiazole derivatives 审中-公开
标题翻译：咪唑噻唑衍生物
公开(公告)号：US20090312310A1
公开(公告)日：2009-12-17
申请号：US12456131
申请日：2009-06-11
申请人： Haruko Kawato , Masaki Miyazaki , Yuuichi Sugimoto , Hiroyuki Naito , Tooru Okayama , Tsunehiko Soga , Kouichi Uoto
发明人： Haruko Kawato , Masaki Miyazaki , Yuuichi Sugimoto , Hiroyuki Naito , Tooru Okayama , Tsunehiko Soga , Kouichi Uoto
IPC分类号： A61K31/551 , C07D513/04 , A61K31/496 , A61K31/429 , A61P35/00
CPC分类号： C07D513/04 , C07D513/10 , C07D519/00
摘要： There is provided a novel compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity. The present invention provides an imidazothiazole derivative represented by the following formula (1) having various substituents that inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity: wherein R1, R2, R3, R4, and R5 in the formula (1) each has the same meaning as defined in the specification.
摘要翻译：提供抑制鼠双分钟2（Mdm2）蛋白与p53蛋白之间相互作用的新型化合物，具有抗肿瘤活性。本发明提供具有抑制Mdm2蛋白和p53蛋白之间的相互作用的各种取代基的下述式（1）表示的抗肿瘤活性的式（1）所示的咪唑并噻唑衍生物：式（1）中的R1，R2，R3，R4和R5 ）各自具有与说明书中定义的相同的含义。

8. 发明授权

US5006647A Phosphorus containing disaccharide derivatives 失效
标题翻译：含磷二糖衍生物
公开(公告)号：US5006647A
公开(公告)日：1991-04-09
申请号：US162932
申请日：1988-03-02
申请人： Tsuneo Kusama , Tsunehiko Soga , Tetsuo Shiba
发明人： Tsuneo Kusama , Tsunehiko Soga , Tetsuo Shiba
IPC分类号： A61K31/70 , C07H13/06 , C07H15/04
CPC分类号： C07H13/06 , C07H15/04
摘要： A disaccharide compound represented by formula (I): ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are as defined in the specification and a salt thereof are disclosed. The compound exhibits excellent antitumor activity and low toxicity and is useful as an antitumor agent.

9. 发明授权

US06677456B2 Pentacyclic taxan compound 有权
标题翻译：五环类紫杉烷化合物
公开(公告)号：US06677456B2
公开(公告)日：2004-01-13
申请号：US10091023
申请日：2002-03-06
申请人： Tsunehiko Soga , Kouichi Uoto , Yasuyuki Takeda
发明人： Tsunehiko Soga , Kouichi Uoto , Yasuyuki Takeda
IPC分类号： C07D40508
CPC分类号： C07D493/04 , A61K31/4355
摘要： This invention is to provide a novel taxol derivative useful as an antitumor compound having respective substituent groups, represented by the following formula (I) which can be orally administered
摘要翻译：本发明提供一种新颖的紫杉醇衍生物，其可用作具有各自取代基的抗肿瘤化合物，由下式（I）表示，其可以口服给药

10. 发明授权

US5432267A Amino sugar derivatives 失效
标题翻译：氨基糖衍生物
公开(公告)号：US5432267A
公开(公告)日：1995-07-11
申请号：US40987
申请日：1993-03-31
申请人： Tsuneo Kusama , Tsunehiko Soga , Akiko Tohgo
发明人： Tsuneo Kusama , Tsunehiko Soga , Akiko Tohgo
IPC分类号： C07H15/04 , C07H5/04 , C07H11/04 , C07H13/02
CPC分类号： C07H15/04
摘要： A compound represented by formula (I): ##STR1## wherein R.sup.1 represents --CO--Z.sup.1 --N(Z.sup.11)--CO--Z.sup.2 --H or --CO--Z.sup.3 --H, wherein Z.sup.1, Z.sup.2, and Z.sup.3 each represent an alkylene group having from 1 to 20 carbon atoms, a phenylene group, or a combination thereof, and Z.sup.11 represents a hydrogen atom, an alkyl group having from 1 to 20 carbon atoms which may be substituted with a phenyl group, a phenyl group which may be substituted with an alkyl group having from 1 to 20 carbon atoms, or an alkylene group having from 1 to 20 carbon atoms which may contain therein a phenylene group; R.sup.2 represents --CO--Z.sup.4 --N(Z.sup.12)--CO--Z.sup.5 --H, --CO--Z.sup.6 --H or a hydrogen atom, wherein Z.sup.4, Z.sup.5, and Z.sup.6 each have the same meaning as Z.sup.1, and Z.sup.12 has the same meaning as Z.sup.11 ; Q.sup.1 and Q.sup.2 each represent a carboxyl group or a phosphonoxy group; Q.sup.3 represents a hydrogen atom, a carboxyl group or a phosphonoxy group; m represents 0 or an integer of from 1 to 20; n represents 0 or an integer of from 1 to 20; Y.sup.1 represents an alkylene group having from 1 to 10 carbon atoms which may contain one or more substituents selected from --OCOR.sup.11 and --NHCOR.sup.12, wherein R.sup.11 represents --Z.sup.13 or --Z.sup.7 --N (Z.sup.14)--CO--Z.sup.8 --H (wherein Z.sup.7 and Z.sup.8 each have the same meaning as Z.sup.1, and Z.sup.13 and Z.sup.14 each have the same meaning as Z.sup.11) and R.sup.12 represents --Z.sup.15 or --Z.sup.9 --N(Z.sup.16)--CO--Z.sup.10 --H (wherein Z.sup.9 and Z.sup.10 each have the same meaning as Z.sup.1, and Z.sup.15 and Z.sup.16 each have the same meaning as Z.sup.11), and a salt thereof. The compound inhibits TNF derivation by endotoxin and is therefore useful for the treatment of multiorganic insufficiencies.
摘要翻译：由式（I）表示的化合物：其中Z 1，Z 2和Z 3各自表示具有1至20个碳原子的亚烷基，亚苯基或其组合，和 Z 11表示氢原子，可以被苯基取代的碳原子数1〜20的烷基，可以被碳原子数1〜20的烷基取代的苯基或具有碳原子数1〜20的亚烷基可含有亚苯基的1至20个碳原子; R2表示-CO-Z4-N（Z12）-CO-Z5-H，-CO-Z6-H或氢原子，其中Z4，Z5和Z6各自与Z1相同，Z12具有相同的含义如Z11; Q1和Q2各自表示羧基或膦酰氧基; Q3表示氢原子，羧基或膦氧基; m表示0或1〜20的整数， n表示0或1〜20的整数， Y1表示可含有一个或多个选自-OCOR 11和-NHCOR 12的取代基的具有1至10个碳原子的亚烷基，其中R11表示-Z13或-Z7-N（Z14）-CO-Z8-H（其中Z7和 Z 8各自具有与Z1相同的含义，Z 13和Z 14各自具有与Z 11相同的含义，R 12表示-Z 15或-Z 9 -N（Z 16）-CO-Z 10 -H（其中Z 9和Z 10各自具有相同的含义 Z1，Z15和Z16各自具有与Z11相同的含义）及其盐。该化合物通过内毒素抑制TNF衍生，因此可用于治疗多机能不足。

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