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1. 发明授权

US6133279A Therapeutic agents for renal diseases and organ preservatives 失效
标题翻译：肾脏疾病和器官防腐剂的治疗剂
公开(公告)号：US6133279A
公开(公告)日：2000-10-17
申请号：US202593
申请日：1998-12-17
申请人： Osamu Cynshi , Yoshiaki Takashima , Kunio Tamura , Akira Ishikawa , Yoshiaki Kato
发明人： Osamu Cynshi , Yoshiaki Takashima , Kunio Tamura , Akira Ishikawa , Yoshiaki Kato
IPC分类号： A61K31/08 , A61K31/085 , A61K31/216 , A61K31/34 , A61K31/343 , A61K31/351 , A61K31/352 , A61K31/38 , A61K31/381 , A61K31/4525 , C07D307/79 , C07D307/80 , C07D307/81 , C07D307/85 , C07D307/94 , C07D333/54 , C07D333/56 , C07D333/58 , C07D333/60 , C07D407/04 , C07D409/04 , A61K31/22
CPC分类号： C07D307/79 , A61K31/08 , A61K31/085 , A61K31/216 , A61K31/34 , A61K31/343 , A61K31/351 , A61K31/352 , A61K31/38 , A61K31/381 , A61K31/4525 , C07D307/80 , C07D307/81 , C07D307/85 , C07D307/94 , C07D333/54 , C07D333/56 , C07D333/58 , C07D333/60 , C07D407/04 , C07D409/04
摘要： Herein disclosed are therapeutic agents for renal diseases and organ preservatives containing a compound represented by the general formula (1): ##STR1## wherein X represents an oxygen atom or a group represented by the general formula (2): ##STR2## where n represents an integer from 0 to 2, R.sub.1 represents a hydrogen atom or an acyl group, R.sub.2 represents a hydrogen atom, a lower alkyl group or a lower alkenyl group, R.sub.3 represents a lower alkyl group, R.sub.4, R.sub.5 and R.sub.6, which may be the same or different, each represents a hydrogen atom or an optionally substituted alkyl group, and R.sub.6 further represents a formyl, carboxyl, lower alkoxycarbonyl or optionally substituted carbamoyl group, or R.sub.3 and R.sub.4 may be taken together to form a five-membered ring, or R.sub.5 and R.sub.6 may be taken together to form a cycloalkyl group, provided that when the five-membered ring formed by R.sub.3 and R.sub.4 and the benzene ring form benzofuran or benzo[b]thiophene, R.sub.6 is absent.
摘要翻译： PCT No.PCT / JP97 / 01729 Sec。 371日期1998年12月17日第 102（e）日期1998年12月17日PCT提交1997年5月23日PCT公布。出版物WO97 / 49388 1997年12月31日，日本公开了含有通式（1）表示的化合物的肾脏疾病和器官防腐剂的治疗剂：其中X表示氧原子或由通式（2）表示的基团：其中n表示 0〜2的整数，R1表示氢原子或酰基，R2表示氢原子，低级烷基或低级烯基，R3表示低级烷基，R4，R5，R6表示相同或不同的，各自表示氢原子或任选取代的烷基，R 6还表示甲酰基，羧基，低级烷氧基羰基或任选取代的氨基甲酰基，或者R 3和R 4可以一起形成五元环，或R 5 并且R6可以一起形成环烷基，条件是当由R3和R4形成的五元环和苯环形成苯并呋喃或苯并[b]噻吩时，R6不存在。

2. 发明授权

US06403639B1 2,3-dihydrobenzofuran derivatives 失效
标题翻译： 2,3-二氢苯并呋喃衍生物
公开(公告)号：US06403639B1
公开(公告)日：2002-06-11
申请号：US09424456
申请日：1999-11-23
申请人： Akira Ishikawa , Yoshiaki Kato , Kunio Tamura , Yoshiaki Takashima , Osamu Cynshi
发明人： Akira Ishikawa , Yoshiaki Kato , Kunio Tamura , Yoshiaki Takashima , Osamu Cynshi
IPC分类号： A61K31343
CPC分类号： C07D307/79 , A61K31/343 , C07D307/94
摘要： 2,3-Dihydrobenzofuran derivatives of general formula (1): wherein R1 represents a hydrogen atom or an acyl group; R2, R3 and R4 represent a hydrogen atom, a lower alkyl group or a lower alkenyl group; R5 and R6 represent a hydrogen atom or an optionally substituted alkyl group, or R5 and R6 combine to form a cycloalkyl group or a saturated heterocyclic group containing one or more oxygen atoms or alkyl-substituted nitrogen atoms, provided that R2 and R3 can not simultaneously represent a t-butyl group, or optically active isomers or pharmaceutically acceptable salts thereof are useful as therapeutic or prophylactic agents for various renal diseases and as organ preservatives.
摘要翻译：通式（1）的2,3-二氢苯并呋喃衍生物：其中R1表示氢原子或酰基; R2，R3和R4表示氢原子，低级烷基或低级烯基; R 5和R 6表示氢原子或任选取代的烷基，或者R 5和R 6结合形成环烷基或含有一个或多个氧原子或烷基取代的氮原子的饱和杂环基，条件是R 2和R 3不能同时代表叔丁基，或其光学活性异构体或其药学上可接受的盐可用作各种肾脏疾病的治疗剂或预防剂和作为器官防腐剂。

3. 发明授权

US06686389B2 2,3-dihydrobenzofuran derivatives 失效
标题翻译： 2,3-二氢苯并呋喃衍生物
公开(公告)号：US06686389B2
公开(公告)日：2004-02-03
申请号：US10121663
申请日：2002-04-15
申请人： Akira Ishikawa , Yoshiaki Kato , Kunio Tamura , Yoshiaki Takashima , Osamu Cynshi
发明人： Akira Ishikawa , Yoshiaki Kato , Kunio Tamura , Yoshiaki Takashima , Osamu Cynshi
IPC分类号： A61K31335
CPC分类号： C07D307/79 , A61K31/343 , C07D307/94
摘要： 2,3-Dihydrobenzofuran derivatives of general formula (1): wherein R1 represents a hydrogen atom or an acyl group; R2, R3 and R4 represent a hydrogen atom, a lower alkyl group or a lower alkenyl group; R5 and R6 combine to form a cycloalkyl group or a saturated heterocyclic group containing one or more oxygen atoms or sulfur atoms, provided that R2 and R3 can not simultaneously represent a t-butyl group, or optically active isomers or pharmaceutically acceptable salts thereof are useful as therapeutic or prophylactic agents for various renal diseases and as organ preservatives.
摘要翻译：通式（1）的2,3-二氢苯并呋喃衍生物：其中R1表示氢原子或酰基; R2，R3和R4表示氢原子，低级烷基或低级烯基; R 5和R 6结合形成含有一个或多个氧原子或硫原子的环烷基或饱和杂环基，条件是R 2和R 3不能同时代表叔丁基，或其光学活性异构体或药学上可接受的盐是有用的作为各种肾脏疾病的治疗剂或预防剂和作为器官防腐剂。

4. 发明授权

US5574178A 4,6-Di-t-butyl-dihydrobenzofuran-5-ol and its derivatives 失效
标题翻译： 4,6-二叔丁基 - 二氢苯并呋喃-5-醇及其衍生物
公开(公告)号：US5574178A
公开(公告)日：1996-11-12
申请号：US416862
申请日：1995-04-17
申请人： Kunio Tamura , Yoshiaki Kato , Mitsutaka Yoshida , Osamu Cynshi , Yasuhiro Ohba
发明人： Kunio Tamura , Yoshiaki Kato , Mitsutaka Yoshida , Osamu Cynshi , Yasuhiro Ohba
IPC分类号： C07C43/23 , C07C47/277 , C07C69/017 , C07C69/157 , C07D307/79 , C07D307/94
CPC分类号： C07D307/79 , C07C43/23 , C07C47/277 , C07C69/017 , C07D307/94
摘要： Compounds represented by the general formula as well as intermediates for the synthesis of thereof: ##STR1## where R.sup.1 is a hydrogen atom or an acyl group; R.sup.2 is a lower alkyl group; R.sup.3 is a hydrogen atom or a lower alkyl group; R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, are a hydrogen atom or an optionally substituted alkyl, alkenyl, alkynyl or aryl group; R.sup.2 and R.sup.4, when taken together, may form a 5-membered ring; R.sup.5 and R.sup.6, when taken together, may form a cycloalkyl group or a heterocyclic group in which at least one methylene on the ring of a cycloalkyl group is substituted by an oxygen atom, a sulfur atom or an alkyl-substituted nitrogen atom, provided that R.sup.6 is not present if the ring formed by R.sup.2 and R.sup.4 taken together is a benzofuran ring. The compounds represented by the general formula (I) have a highly selective anti-oxidative activity and are useful as therapeutics of ischemic diseases such as arteriosclerosis and myocardial infarction.
摘要翻译： PCT No.PCT / JP93 / 01489 371日期1995年04月17日 102（e）日期1995年04月17日PCT 1993年10月18日PCT公布。出版物WO94 / 08930 日本1994年4月28日由通式表示的化合物及其合成中间体：其中R 1是氢原子或酰基; R2是低级烷基; R3是氢原子或低级烷基; R 4，R 5和R 6可以相同或不同，为氢原子或任选取代的烷基，烯基，炔基或芳基; 当R 2和R 4一起时可以形成5元环; R 5和R 6一起可以形成环烷基或杂环基，其中环烷基环上的至少一个亚甲基被氧原子，硫原子或烷基取代的氮原子取代，条件是如果由R2和R4形成的环在一起是苯并呋喃环，则R6不存在。由通式（I）表示的化合物具有高度选择性的抗氧化活性，并且可用作缺血性疾病如动脉硬化和心肌梗死的治疗剂。

5. 发明授权

US5663373A 4-alkoxy-2, 6-di-t-butylphenol derivatives 失效
公开(公告)号：US5663373A
公开(公告)日：1997-09-02
申请号：US700834
申请日：1996-08-21
申请人： Kunio Tamura , Yoshiaki Kato , Mitsutaka Yoshida , Osamu Cynshi , Yasuhiro Ohba
发明人： Kunio Tamura , Yoshiaki Kato , Mitsutaka Yoshida , Osamu Cynshi , Yasuhiro Ohba
IPC分类号： C07C43/23 , C07C47/277 , C07C69/017 , C07C69/157 , C07D307/79 , C07D307/94
CPC分类号： C07D307/79 , C07C43/23 , C07C47/277 , C07C69/017 , C07D307/94
摘要： Compounds represented by the general formula (I), as well as intermediates for the synthesis of thereof: ##STR1## where R.sup.1 is a hydrogen atom or an acyl group; R.sup.2 is a lower alkyl group; R.sup.3 is a hydrogen atom or a lower alkyl group; R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, are a hydrogen atom or an optionally substituted alkyl, alkenyl, alkynyl or aryl group; R.sup.2 and R.sup.4, when taken together, may form a 5-membered ring; R.sup.5 and R.sup.6, when taken together, may form a cycloalkyl group or a heterocyclic group in which at least one methylene on the ring of a cycloalkyl group is substituted by an oxygen atom, a sulfur atom or an alkyl-substituted nitrogen atom, provided that R.sup.6 is not present if the ring formed by R.sup.2 and R.sup.4 taken together is a benzofuran ring. The compounds represented by the general formula (I) have a highly selective anti-oxidative activity and are useful as therapeutics of ischemic diseases such as arteriosclerosis and myocardial infarction.

6. 发明授权

US5606089A 4-alkoxy-2, 6-di-t-butylphenol derivatives 失效
标题翻译： 4-烷氧基-2,6-二叔丁基苯酚衍生物
公开(公告)号：US5606089A
公开(公告)日：1997-02-25
申请号：US444055
申请日：1995-05-18
申请人： Kunio Tamura , Yoshiaki Kato , Mitsutaka Yoshida , Osamu Cynshi , Yasuhiro Ohba
发明人： Kunio Tamura , Yoshiaki Kato , Mitsutaka Yoshida , Osamu Cynshi , Yasuhiro Ohba
IPC分类号： C07C43/23 , C07C47/277 , C07C69/017 , C07C69/157 , C07D307/79 , C07D307/94 , C07C69/773
CPC分类号： C07D307/79 , C07C43/23 , C07C47/277 , C07C69/017 , C07D307/94
摘要： Compounds represented by the general formula (I), as well as intermediates for the synthesis of thereof: ##STR1## where R.sup.1 is a hydrogen atom or an acyl group; R.sup.2 is a lower alkyl group; R.sup.3 is a hydrogen atom or a lower alkyl group; R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, are a hydrogen atom or an optionally substituted alkyl, alkenyl, alkynyl or aryl group; R.sup.2 and R.sup.4, when taken together, may form a 5-membered ring; R.sup.5 and R.sup.6, when taken together, may form a cycloalkyl group or a heterocyclic group in which at least one methylene on the ring of a cycloalkyl group is substituted by an oxygen atom, a sulfur atom or an alkyl-substituted nitrogen atom, provided that R.sup.6 is not present if the ring formed by R.sup.2 and R.sup.4 taken together is a benzofuran ring. The compounds represented by the general formula (I) have a highly selective anti-oxidative activity and are useful as therapeutics of ischemic diseases such as arteriosclerosis and myocardial infarction.
摘要翻译：由通式（I）表示的化合物及其合成中间体：其中R 1是氢原子或酰基; R2是低级烷基; R3是氢原子或低级烷基; R 4，R 5和R 6可以相同或不同，为氢原子或任选取代的烷基，烯基，炔基或芳基; 当R 2和R 4一起时可以形成5元环; R 5和R 6一起可以形成环烷基或杂环基，其中环烷基环上的至少一个亚甲基被氧原子，硫原子或烷基取代的氮原子取代，条件是如果由R2和R4形成的环在一起是苯并呋喃环，则R6不存在。由通式（I）表示的化合物具有高度选择性的抗氧化活性，并且可用作缺血性疾病如动脉硬化和心肌梗死的治疗剂。

7. 发明授权

US5789436A 4,6 Di-t-butyl-5-hydroxy-2,3-dihydrobenzothiophene 失效
标题翻译： 4,6二叔丁基-2,3-二氢苯并噻吩衍生物
公开(公告)号：US5789436A
公开(公告)日：1998-08-04
申请号：US727652
申请日：1996-10-09
申请人： Yoshiaki Kato , Akira Ishikawa , Kunio Tamura
发明人： Yoshiaki Kato , Akira Ishikawa , Kunio Tamura
IPC分类号： C07C333/04 , C07D333/50 , C07D333/54 , C07D333/56 , C07D333/58 , A61K31/38 , C07C321/00 , C07D333/52 , C07D333/64
CPC分类号： C07D333/50 , C07C333/04 , C07D333/54 , C07D333/56 , C07D333/58
摘要： A compound represented by formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom, a lower alkyl group or an acyl group; R.sub.2 and R.sub.3, which may be the same or different, each represents a hydrogen atom, an optionally substituted alkyl group, or an optionally substituted alkenyl group; R.sub.4 represents a hydrogen atom, an optionally substituted alkyl group, or an optionally substituted alkenyl group, or R.sub.4 forms a double bond between the carbon atom to which R.sub.3 is bonded and the adjacent carbon atom to form a benzothiophene skeleton, or R.sub.3 and R.sub.4 are taken together to form a 5- to 8-membered spiro ring which may contain a hetero atom, e.g., oxygen, sulfur or nitrogen; and n represents an integer of 0 to 2, or a pharmaceutically acceptable salt thereof. The compound of formula (I) exhibits an inhibitory action on the oxidative modification of LDL and is useful as therapeutics of arteriosclerosis.
摘要翻译： PCT No.PCT / JP95 / 00706 Sec。 371日期1996年10月9日第 102（e）日期1996年10月9日PCT提交1995年4月11日PCT公布。公开号WO95 / 27710 日期：1995年10月19日由式（I）表示的化合物：其中R 1表示氢原子，低级烷基或酰基; R 2和R 3可以相同或不同，各自表示氢原子，任选取代的烷基或任选取代的烯基; R4表示氢原子，任选取代的烷基或任选取代的烯基，或R 4在与R 3键合的碳原子和相邻碳原子之间形成双键，以形成苯并噻吩骨架，或者R3和R4为一起形成可含有杂原子（例如氧，硫或氮）的5-至8-元螺环; 和n表示0〜2的整数，或其药学上可接受的盐。式（I）化合物对LDL的氧化修饰具有抑制作用，可用作动脉硬化的治疗剂。

8. 发明授权

US06440999B1 Intimal thickening inhibitory agent 失效
标题翻译：内膜增厚抑制剂
公开(公告)号：US06440999B1
公开(公告)日：2002-08-27
申请号：US09637022
申请日：2000-08-14
申请人： Osamu Cynshi , Reiko Sekimori , Yoshiaki Kato
发明人： Osamu Cynshi , Reiko Sekimori , Yoshiaki Kato
IPC分类号： A01N4312
CPC分类号： C07C323/20 , C07C43/23 , C07C317/22
摘要： An intimal thickening inhibitory agent comprising, as an active ingredient, a compound represented by formula (1): wherein x represents an oxygen atom or a group of formula (2) —S—(O)n (2) wherein n represents an integer of from 0 to 2, R1 represents a hydrogen atom or an acyl group; R2 represents a hydrogen atom, a lower alkyl group or a lower alkenyl group; R3 represents a lower alkyl group; and R4, R5, and R6, which may be the same or different, each represent a hydrogen atom or a substituted or unsubstituted alkyl group; or R3 and R4 may be taken together to form a 5-membered ring; or R5 and R6 may be taken together to form a cycloalkyl group; provided that R6 is nil when R3 and R4 are taken together to form benzofuran or benzo[b]thiophene.
摘要翻译：一种内膜增稠抑制剂，其包含作为活性成分的由式（1）表示的化合物：其中x表示氧原子或式（2）的基团，其中n表示0至2的整数，R 1表示氢原子或酰基; R2表示氢原子，低级烷基或低级烯基; R3表示低级烷基; 和可以相同或不同的R 4，R 5和R 6各自表示氢原子或取代或未取代的烷基; 或者R 3和R 4可以一起形成5元环; 或者R 5和R 6可以一起形成环烷基; 条件是当R 3和R 4一起形成苯并呋喃或苯并[b]噻吩时，R6为零。

9. 发明授权

US6103753A Intimal thickening inhibitory agent 失效
标题翻译：内膜增厚抑制剂
公开(公告)号：US6103753A
公开(公告)日：2000-08-15
申请号：US68610
申请日：1998-05-06
申请人： Osamu Cynshi , Reiko Sekimori , Yoshiaki Kato
发明人： Osamu Cynshi , Reiko Sekimori , Yoshiaki Kato
IPC分类号： C07C43/23 , C07C317/22 , C07C323/20 , A01N43/12
CPC分类号： C07C323/20 , C07C317/22 , C07C43/23
摘要： An intimal thickening inhibitory agent comprising, as an active ingredient, a compound represented by formula (1): ##STR1## wherein X represents an oxygen atom or a group of formula (2): ##STR2## wherein n represents an integer of from 0 to 2, R.sub.1 represents a hydrogen atom or an acyl group; R.sub.2 represents a hydrogen atom, a lower alkyl group or a lower alkenyl group; R.sub.3 represents a lower alkyl group; and R.sub.4, R.sub.5, and R.sub.6, which may be the same or different, each represent a hydrogen atom or a substituted or unsubstituted alkyl group; or R.sub.3 and R.sub.4 may be taken together to form a 5-membered ring; or R.sub.5 and R.sub.6 may be taken together to form a cycloalkyl group; provided that R.sub.6 is nil when R.sub.3 and R.sub.4 are taken together to form benzofuran or benzo[b]thiophene.
摘要翻译： PCT No.PCT / JP96 / 03279 Sec。 371日期：1998年5月6日 102（e）日期1998年5月6日PCT 1996年11月8日PCT PCT。公开号WO97 / 17066 日期：1997年5月15日一种内膜增稠抑制剂，其包含作为活性成分的由式（1）表示的化合物：其中X表示氧原子或式（2）的基团：其中n表示0至2的整数 R1表示氢原子或酰基; R2表示氢原子，低级烷基或低级烯基; R3表示低级烷基; 和可以相同或不同的R 4，R 5和R 6各自表示氢原子或取代或未取代的烷基; 或者R 3和R 4可以一起形成5元环; 或者R 5和R 6可以一起形成环烷基; 条件是当R 3和R 4一起形成苯并呋喃或苯并[b]噻吩时，R6为零。

10. 发明授权

US06852867B2 Process for preparation of a benzofuran derivative 失效
标题翻译：制备苯并呋喃衍生物的方法
公开(公告)号：US06852867B2
公开(公告)日：2005-02-08
申请号：US10333220
申请日：2001-07-19
申请人： Kunio Tamura , Hirohito Shimizu , Yoshiaki Kato , Masahiro Shimizu
发明人： Kunio Tamura , Hirohito Shimizu , Yoshiaki Kato , Masahiro Shimizu
IPC分类号： C07D307/79
CPC分类号： C07D307/79 , Y02P20/55
摘要： An industrially useful process for producing benzofuran derivatives of formula (1): by formylating a compound of formula (2): (where A1 is a protective group), followed by reaction with a compound of formula (4): (where X1 is a halogen atom), then performing a cyclizing reaction and subsequently performing a reaction for hydroxyl group deprotection.
摘要翻译：一种用于生产式（1）的苯并呋喃衍生物的工业上有用的方法：通过将式（2）的化合物（其中A 1是保护基）甲酰化，然后与式（4）的化合物反应:(其中X1是卤原子），然后进行环化反应，随后进行羟基脱保护反应。

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