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1. 发明申请

US20100210591A1 BIS(TRIMETHYLSILYL)PHENYL COMPOUND OR SALT THEREOF, AND USE THEREOF 失效
标题翻译： BIS（三甲基甲硅烷基）苯基化合物或其盐，及其用途
公开(公告)号：US20100210591A1
公开(公告)日：2010-08-19
申请号：US12682097
申请日：2008-10-10
申请人： Yoshimitsu Suda , Hiromi Oshiumi , Koji Murakami
发明人： Yoshimitsu Suda , Hiromi Oshiumi , Koji Murakami
IPC分类号： A61K31/695 , C07F7/10
CPC分类号： C07F7/0812 , C07F7/081
摘要： The present invention provides a compound that exhibits an excellent antitumor effect and reduces side effects, such as skin disorders, of the existing retinoid by selectively activating on the nuclear receptor RARα, thereby possibly producing significant improvement of clinical profits. Specifically, the present invention provides a bis(trimethylsilyl)phenyl compound represented by Formula (I): wherein X is N or CH; Y is O or S; R1, R2, and R3 are the same or different and are hydrogen or lower alkyl; R4 and R5 are the same or different and are hydrogen, lower alkyl, or halogen; and a bond between a carbon atom to which R1 is attached and a carbon atom to which R2 is attached is a single bond or a double bond; or a salt thereof.
摘要翻译：本发明提供通过选择性活化核受体RARα而显示出优异的抗肿瘤效果并降低现有类视色素的副作用，例如皮肤病，从而可能显着改善临床利益。具体地说，本发明提供由式（I）表示的双（三甲基甲硅烷基）苯基化合物：其中X是N或CH; Y为O或S; R1，R2和R3相同或不同，为氢或低级烷基; R4和R5相同或不同，为氢，低级烷基或卤素; 并且R 1所连接的碳原子和R 2所连接的碳原子之间的键为单键或双键; 或其盐。

2. 发明授权

US07855300B2 Bis(trimethylsilyl)phenyl compound or salt thereof, and use thereof 失效
标题翻译：双（三甲基甲硅烷基）苯基化合物或其盐及其用途
公开(公告)号：US07855300B2
公开(公告)日：2010-12-21
申请号：US12682097
申请日：2008-10-10
申请人： Yoshimitsu Suda , Hiromi Oshiumi , Koji Murakami
发明人： Yoshimitsu Suda , Hiromi Oshiumi , Koji Murakami
IPC分类号： C07F7/10
CPC分类号： C07F7/0812 , C07F7/081
摘要： The present invention provides a compound that exhibits an excellent antitumor effect and reduces side effects, such as skin disorders, of the existing retinoid by selectively activating on the nuclear receptor RARα, thereby possibly producing significant improvement of clinical profits. Specifically, the present invention provides a bis(trimethylsilyl)phenyl compound represented by Formula (I): wherein X is N or CH; Y is O or S; R1, R2, and R3 are the same or different and are hydrogen or lower alkyl; R4 and R5 are the same or different and are hydrogen, lower alkyl, or halogen; and a bond between a carbon atom to which R1 is attached and a carbon atom to which R2 is attached is a single bond or a double bond; or a salt thereof.
摘要翻译：本发明提供通过选择性活化核受体RARα，显示出优异的抗肿瘤效果并降低现有类视黄醇的副作用，例如皮肤病，从而可能显着改善临床利益。具体地说，本发明提供由式（I）表示的双（三甲基甲硅烷基）苯基化合物：其中X是N或CH; Y为O或S; R1，R2和R3相同或不同，为氢或低级烷基; R4和R5相同或不同，为氢，低级烷基或卤素; 并且R 1所连接的碳原子和R 2所连接的碳原子之间的键为单键或双键; 或其盐。

3. 发明授权

US06951843B2 Peptide derivatives and their pharmaceutically acceptable salts, thereof, processes for preparation of both and use thereof 失效
标题翻译：肽衍生物及其药学上可接受的盐，其制备方法及其用途
公开(公告)号：US06951843B2
公开(公告)日：2005-10-04
申请号：US10168540
申请日：2001-11-02
申请人： Kenji Yamamoto , Yoshimitsu Suda , Tetsuji Asao
发明人： Kenji Yamamoto , Yoshimitsu Suda , Tetsuji Asao
IPC分类号： A61K38/00 , A61P1/02 , A61P43/00 , C07C271/22 , C07D295/185 , C07K5/072 , C07K5/093
CPC分类号： C07D295/185 , A61K38/00 , C07C271/22 , C07K5/06104 , C07K5/0819 , Y02P20/55
摘要： The present invention provides a peptide derivative of formula (I) wherein X is —CHOH— or —CO—; R1 and R2 are hydrogen or substituted oxycarbonyl; R3 is substituted oxycarbonyl; R4 is hydroxyl, lower alkoxy, optionally substituted piperazinyl or the like; R5 is a R-group side chain of an α-amino acid optionally protected by a protective group, R6 is hydroxyl, lower alkoxy or the like; m is 0 or 1; and n is an integer of 2 to 6; or a pharmaceutically acceptable salt thereof. The present invention further provides a production process and use thereof.
摘要翻译：本发明提供式（I）的肽衍生物，其中X是-CHOH-或-CO-; R 1和R 2是氢或取代的氧羰基; R 3是取代的氧羰基; R 4是羟基，低级烷氧基，任选取代的哌嗪基等; R 5是任选被保护基保护的α-氨基酸的R基侧链，R 6是羟基，低级烷氧基等; m为0或1; n为2〜6的整数。或其药学上可接受的盐。本发明还提供了一种制备方法及其用途。

4. 发明授权

US07067476B2 Peptide derivative, and pharmaceutically acceptable salt thereof, process for producing the same, and use thereof 失效
标题翻译：肽衍生物及其药学上可接受的盐，其制备方法及其用途
公开(公告)号：US07067476B2
公开(公告)日：2006-06-27
申请号：US10493060
申请日：2002-11-14
申请人： Kenji Yamamoto , Yoshimitsu Suda , Tetsuji Asao
发明人： Kenji Yamamoto , Yoshimitsu Suda , Tetsuji Asao
IPC分类号： A01N61/00 , A61K38/00
CPC分类号： C07C279/36 , Y02P20/55
摘要： The present invention provides a peptide derivative of formula (I) or a pharmaceutically acceptable salt thereof wherein X is —CH(OH)— or —CO—; R1 is hydrogen or an amino protecting group; R2 is hydroxyl or lower alkoxy; one of R3 and R4 is the side chain (R group) of lysine the amino group of which may be protected with a protecting group and the other of R3 and R4 is the side chain (R group) of arginine the guanidino group of which may be protected with a protecting group; and R5 and R6 may be the same or different and are hydrogen, lower alkyl or aralkyl. The present invention further provides a production process and use thereof.
摘要翻译：本发明提供式（I）的肽衍生物或其药学上可接受的盐，其中X为-CH（OH） - 或-CO-; R 1是氢或氨基保护基; R 2是羟基或低级烷氧基; R 3和R 4之一是赖氨酸的侧链（R基团），其氨基可被保护基保护，另一个R ^{3和R 4是其胍基可被保护基保护的精氨酸的侧链（R基团）; R 5和R 6可以相同或不同，为氢，低级烷基或芳烷基。本发明还提供了一种制备方法及其用途。}

5. 发明授权

US08304427B2 Acylthiourea compound or salt thereof, and use thereof 有权
标题翻译：酰基硫脲化合物或其盐及其用途
公开(公告)号：US08304427B2
公开(公告)日：2012-11-06
申请号：US12937312
申请日：2009-04-09
申请人： Yoshimitsu Suda , Kosuke Egami , Hidenori Fujita
发明人： Yoshimitsu Suda , Kosuke Egami , Hidenori Fujita
IPC分类号： A61K31/04 , C07D215/38
CPC分类号： C07D215/48 , C07D401/12 , C07D405/12 , C07D409/12
摘要： Provided is a c-Met inhibitory antitumor agent which mitigates side effects by selectively affecting tumor cells in which c-Met is specifically expressed, having a formula (I) or its salt: wherein each of R1 and R2 are independently a hydrogen atom, an optionally substituted C1-6 alkyl, C3-10 cycloalkyl, C6-14 aromatic hydrocarbon, or saturated or unsaturated heterocyclic group, or R1 and R2 may form, together with the nitrogen atom to which they are attached, an optionally substituted nitrogen-containing heterocyclic ring; R3 is a C1-6 alkyl group; and R4, R5, and R6, are independently a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 alkylamino group, an optionally substituted aromatic hydrocarbon group, or an optionally substituted saturated or unsaturated heterocyclic group, or R5 and R6 may form a ring together with the phenyl ring to which they are attached.
摘要翻译：本发明提供一种c-Met抑制性抗肿瘤剂，其通过选择性地影响c-Met特异性表达的具有式（I）或其盐的肿瘤细胞来减轻副作用：其中R1和R2各自独立地为氢原子，任选取代的C 1-6烷基，C 3-10环烷基，C 6-14芳烃或饱和或不饱和杂环基，或R 1和R 2可以与它们所连接的氮原子一起形成任选取代的含氮杂环环; R3是C1-6烷基; 和R 4，R 5和R 6独立地为氢原子，卤素原子，任选取代的C 1-6烷基，C 1-6烷氧基，C 1-6烷基氨基，任选取代的芳族烃基或任选取代的饱和或不饱和杂环基，或R 5和R 6可以与它们所连接的苯环一起形成环。

6. 发明授权

US06359551B1 Indication device 失效
标题翻译：指示装置
公开(公告)号：US06359551B1
公开(公告)日：2002-03-19
申请号：US09674625
申请日：2000-11-03
申请人： Yoshimitsu Suda
发明人： Yoshimitsu Suda
IPC分类号： B62J300
CPC分类号： B62J6/20 , B60Q1/32 , B60Q1/326 , F21L4/00 , F21L13/00
摘要： An indication device of the present invention includes a case body provided to a movable portion during in use by a both-sided adhesive tape or a fitting; luminous body provided with the case body and emits a light or a blinking light by using electric current generated in a power source; a first ON/OFF switch with an optical sensor interposed between the power source and luminous body, and a second ON/OFF switch turning on automatically during use. Therefore, the indication device can allow the others to become aware of person's whereabouts by emitting light or blinking light when in use. The device can be turned off automatically to prevent dissipation of power.
摘要翻译：本发明的指示装置包括在使用期间通过双面胶带或配件设置到可动部分的壳体; 发光体设置有壳体，并且通过使用在电源中产生的电流发出光或闪烁的光; 具有介于电源和发光体之间的光学传感器的第一ON / OFF开关，以及在使用期间自动开启的第二ON / OFF开关。因此，指示装置可以允许其他人在使用时通过发光或闪烁的光来识别人的下落。该设备可以自动关闭，以防止功率消耗。

7. 发明申请

US20110034439A1 ACYLTHIOUREA COMPOUND OR SALT THEREOF, AND USE THEREOF 有权
标题翻译：乙酰化合物或其盐，及其用途
公开(公告)号：US20110034439A1
公开(公告)日：2011-02-10
申请号：US12937312
申请日：2009-04-09
申请人： Yoshimitsu Suda , Kosuke Egami , Hidenori Fujita
发明人： Yoshimitsu Suda , Kosuke Egami , Hidenori Fujita
IPC分类号： A61K31/55 , C07D215/233 , A61K31/47 , A61K31/4709 , C07D413/12 , A61K31/5377 , C07D401/12 , A61P35/00
CPC分类号： C07D215/48 , C07D401/12 , C07D405/12 , C07D409/12
摘要： To provide an antitumor agent which exhibits excellent c-Met inhibitory effect and mitigates side effects by virtue of selectively affecting to tumor cells in which c-Met is specifically expressed.The invention provides an acylthiourea compound represented by formula (I): (wherein each of R1 and R2, which may be the same or different, represents a hydrogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted C3-10 cycloalkyl group, an optionally substituted C6-14 aromatic hydrocarbon group, or an optionally substituted saturated or unsaturated heterocyclic group, or R1 and R2 may form, together with the nitrogen atom to which they are attached, an optionally substituted nitrogen-containing heterocyclic ring; R3 represents a C1-6 alkyl group; and each of R4, R5, and R6, which may be identical to or different from one another, represents a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 alkylamino group, an optionally substituted aromatic hydrocarbon group, or an optionally substituted saturated or unsaturated heterocyclic group, or R5 and R6 may form a ring together with the phenyl ring to which they are attached) or a salt thereof.
摘要翻译：提供通过选择性地影响c-Met特异性表达的肿瘤细胞，其表现出优异的c-Met抑制作用并减轻副作用的抗肿瘤剂。本发明提供由式（I）表示的酰基硫脲化合物：其中R 1和R 2各自可以相同或不同，表示氢原子，任选取代的C 1-6烷基，任选取代的C 3-10环烷基基团，任选取代的C 6-14芳族烃基或任选取代的饱和或不饱和杂环基，或R 1和R 2可以与它们所连接的氮原子一起形成任选取代的含氮杂环; R 3 可以相同或不同的R4，R5，R6各自表示氢原子，卤素原子，任意取代的C1-6烷基，C1- C6烷氧基，C1-6烷基氨基，任选取代的芳族烃基或任选取代的饱和或不饱和杂环基，或者R 5和R 6可以与它们所代表的苯环一起形成环 e附着）或其盐。

8. 发明授权

US6110967A Epoxysuccinamide derivative or salt thereof 失效
标题翻译：环氧琥珀酰胺衍生物或其盐
公开(公告)号：US6110967A
公开(公告)日：2000-08-29
申请号：US202607
申请日：1998-12-17
申请人： Tetsuji Asao , Tomohiro Yamashita , Yoshimitsu Suda , Shigeo Okajima , Yukio Tada , Nobuhiko Katsunuma , Shozo Yamada , Kazuhiko Shigeno , Atsuhiko Uemura
发明人： Tetsuji Asao , Tomohiro Yamashita , Yoshimitsu Suda , Shigeo Okajima , Yukio Tada , Nobuhiko Katsunuma , Shozo Yamada , Kazuhiko Shigeno , Atsuhiko Uemura
IPC分类号： C07D303/40 , C07D303/48 , A61K31/495 , A61K31/41 , A61K31/435
CPC分类号： C07D303/48
摘要： The invention relates an epoxysuccinamide derivative represented by a formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl or aminoalkyl group, R.sup.2 represents an aminoalkyl group which May be substituted, an aryl group which may be substituted, a heterocyclic group which may be substituted, an aralkyl group which may be substituted, or an alkyl group substituted by a heterocyclic ring which may be substituted, or R.sup.1 and R.sup.2 may form a nitrogen-containing heterocyclic ring, which may be substituted, together with the adjacent nitrogen atoms, and R.sup.3 and R.sup.4 are the same or different from each other and independently represent a hydrogen atom, or an alkyl or aralkyl group, or a salt thereof, a preparation process thereof, and a medicine comprising such a derivative or salt as an active ingredient. This compound has a specific inhibitory activity for cathepsin L and family enzymes thereof, and is useful as an agent for preventing and treating metabolic osteopathy such as osteoporosis and hypercalcemia.
摘要翻译： PCT No.PCT / JP98 / 01778 Sec。 371日期1998年12月17日第 102（e）1998年12月17日日期PCT提交1998年4月17日PCT公布。第WO98 / 47887号公报日期：1998年10月29日本发明涉及由式（I）表示的环氧琥珀酰胺衍生物：其中R1表示氢原子，烷基或氨基烷基，R2表示可以被取代的氨基烷基，可以被取代的芳基，可以被取代的杂环基，可以被取代的芳烷基或被可被取代的杂环取代的烷基，或者可以被R 1和R 2形成可以被取代的含氮杂环，和相邻的氮原子和R3和R4彼此相同或不同，并且独立地表示氢原子或烷基或芳烷基或其盐，其制备方法和包含这种衍生物或盐的药物作为活性成分。该化合物对组织蛋白酶L及其家族酶具有特异性抑制活性，可用作预防和治疗代谢性骨病如骨质疏松症和高钙血症的药剂。

9. 发明授权

US5883121A Epoxysuccinamide derivative or salt thereof, and medicine comprising the same 失效
标题翻译：环氧琥珀酰胺衍生物或其盐，以及含有它们的药物
公开(公告)号：US5883121A
公开(公告)日：1999-03-16
申请号：US894050
申请日：1997-08-12
申请人： Tomohiro Yamashita , Yoshimitsu Suda , Yukio Tada , Nobuhiko Katunuma , Tetsuji Asao
发明人： Tomohiro Yamashita , Yoshimitsu Suda , Yukio Tada , Nobuhiko Katunuma , Tetsuji Asao
IPC分类号： C07D303/48 , A61K31/335 , C07D303/46
CPC分类号： C07D303/48
摘要： The invention relates an epoxysuccinamide derivative represented by the general formula (1) ##STR1## wherein R.sup.1 and R.sup.2 are the same or different from each other and independently represent H or an aromatic hydrocarbon group or aralkyl group which may be substituted, or R.sup.1 and R.sup.2 may form a nitrogen-containing heterocyclic ring together with the adjacent nitrogen atoms, R.sup.3 is H or an acyl group, R.sup.4 is H or an aralkyl group, and R.sup.5 is an aromatic hydrocarbon group or aralkyl group which may be substituted, or R.sup.5 may form an amino acid residue, which may be protected, together with the adjacent nitrogen atom, or a salt thereof, and a medicine comprising the derivative as an active ingredient; and this compound has an inhibiting activity against cathepsin, and particularly, specifically inhibits cathepsin L and is hence useful for prevention and treatment of osteopathy such as osteoporosis.
摘要翻译： PCT No.PCT / JP96 / 03603 Sec。 371日期：1997年8月12日 102（e）日期1997年8月12日PCT 1996年12月10日PCT PCT。出版物WO97 / 21694 日期：1996年6月19日本发明涉及由通式（1）表示的环氧琥珀酰胺衍生物彼此不同，独立地表示H或可被取代的芳香族烃基或芳烷基，或者R 1和R 2可以形成含氮杂环与相邻的氮原子一起，R3是H或酰基，R4是H或芳烷基，R5是可被取代的芳族烃基或芳烷基，或R5可以形成氨基酸残基，其中可以与相邻的氮原子或其盐一起保护，以及包含该衍生物作为活性成分的药物; 并且该化合物对组织蛋白酶具有抑制活性，特别是抑制组织蛋白酶L，因此可用于预防和治疗骨质疏松症等骨病。

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