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公开(公告)号:US06852867B2
公开(公告)日:2005-02-08
申请号:US10333220
申请日:2001-07-19
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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公开(公告)号:US6133279A
公开(公告)日:2000-10-17
申请号:US202593
申请日:1998-12-17
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。
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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。
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公开(公告)号:US4562565A
公开(公告)日:1985-12-31
申请号:US417497
申请日:1982-09-13
申请人: Kunio Tamura
发明人: Kunio Tamura
CPC分类号: G11B7/0903 , G11B21/106
摘要: A tracking servo system of a recording-disc reading and reproducing apparatus in which the information carried on a recording disc adapted to be driven for rotation is scanned by a signal pickup point displaced radially of the disc, comprising tracking error signal generator operative to detect an amount of deviation, if any, of the signal pickup medium from a target track on an information-carrying surface of the recording disc and produce a tracking error signal representative of the detected amount of deviation, and band eliminator such as a notch filter operative to eliminate a predetermined frequency in the tracking error signal.
摘要翻译: 一种记录盘读取和再现装置的跟踪伺服系统,其中由适于被驱动旋转的记录盘上携带的信息由盘的径向位移的信号拾取点扫描,包括跟踪误差信号发生器,用于检测一个 信号拾取介质从记录盘的信息载体表面上的目标轨道的偏差量(如果有的话)产生表示检测到的偏差量的跟踪误差信号,以及诸如陷波滤波器的频带消除器, 消除跟踪误差信号中的预定频率。
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公开(公告)号:US4597314A
公开(公告)日:1986-07-01
申请号:US544878
申请日:1983-10-24
申请人: Kunio Tamura , Takayuki Horiai
发明人: Kunio Tamura , Takayuki Horiai
CPC分类号: B67B7/164
摘要: An improved bottle opening machine for smoothly removing crown caps from bottle necks of empty bottles contained in bottle cases which are being conveyed on a conveyance system in a single file, in which the cap removing is carried out by the steps of engaging of cap removing sections on rotary discs with the crown caps on the bottle necks in an area where the circular movement path of the cap removing sections and the linear movement path of the bottle necks mutually converge in the tangential direction, removing of the crown caps from the bottle necks under the influence of a moment which is produced as the former is separated from the latter as the rotary discs are rotated, and releasing of the removed crown caps from the cap removing sections with the aid of cap releasing mechanisms. To ensure that the cap removing sections are positioned correctly with corresponding bottle necks, at least a synchronizing means is rotatably mounted on the frame structure. The synchronizing means comprises a synchronizing disc disposed adjacent to the rotary discs fixedly mounted on the drum. Alternatively, the synchronizing means may comprise a star wheel adapted to be engaged to the barrel of the bottles. The rotary discs are preferably mounted on a pair of arms adapted to swing upward and downward about pivotal pins on the frame structure.
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公开(公告)号:US06403639B1
公开(公告)日:2002-06-11
申请号:US09424456
申请日:1999-11-23
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。
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公开(公告)号:US06686389B2
公开(公告)日:2004-02-03
申请号:US10121663
申请日:2002-04-15
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。
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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。
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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.
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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。
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