-
公开(公告)号:US20100041655A1
公开(公告)日:2010-02-18
申请号:US12278054
申请日:2007-02-05
申请人: Naoya Ono , Tetsuo Takayama , Fumiyasu Shiozawa , Hironori Katakai , Tetsuya Yabuuchi , Tomomi Ota , Makoto Yagi , Masakazu Sato
发明人: Naoya Ono , Tetsuo Takayama , Fumiyasu Shiozawa , Hironori Katakai , Tetsuya Yabuuchi , Tomomi Ota , Makoto Yagi , Masakazu Sato
IPC分类号: A61K31/5377 , C07D249/08 , A61K31/4196 , C07D403/12 , A61K31/497 , C07D413/14
CPC分类号: C07D249/08
摘要: An object of the present invention is to provide a compound having an action of inhibiting binding between S1P and its receptor, Edg-1 (S1P1), and is useful as a pharmaceutical compound. A compound or a pharmaceutically acceptable salt thereof, which compound is represented by the formula below (where A represents an oxygen atom, a sulfur atom, a group represented by Formula —SO—, a group represented by Formula —SO2— or the like, R1 represents a hydrogen atom, an alkyl group having 1-6 carbon atoms, or the like, R1A represents a hydrogen atom or the like, R2 represents an alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-6 carbon atoms, or the like, represents an aryl group, R4 represents a hydrogen atom or an alkyl group having 1-6 carbon atoms and optionally substituted with a carboxyl group, and R5 represents an alkyl group having 1-carbon atoms, a cycloalkyl group having 3-8 carbon atoms, an aryl group which is optionally substituted, or the like).
摘要翻译: 本发明的目的是提供具有抑制S1P与其受体Edg-1(S1P1)结合的作用的化合物,可用作药物化合物。 一种化合物或其药学上可接受的盐,该化合物由下式表示(其中A表示氧原子,硫原子,由式-SO-表示的基团,由式-SO2-等表示的基团, R1表示氢原子,具有1-6个碳原子的烷基等,R1A表示氢原子等,R2表示具有1-6个碳原子的烷基,具有3-6个碳原子的环烷基 等表示芳基,R 4表示氢原子或具有1-6个碳原子并且任选被羧基取代的烷基,R 5表示具有1个碳原子的烷基,环烷基具有3个 -8个碳原子,任选取代的芳基等)。
-
公开(公告)号:US20090182144A1
公开(公告)日:2009-07-16
申请号:US12278477
申请日:2007-02-06
申请人: Naoya Ono , Tetsuo Takayama , Fumiyasu Shiozawa , Hironori Katakai , Tetsuya Yabuuchi , Tomomi Ota , Takeshi Koami , Rie Nishikawa
发明人: Naoya Ono , Tetsuo Takayama , Fumiyasu Shiozawa , Hironori Katakai , Tetsuya Yabuuchi , Tomomi Ota , Takeshi Koami , Rie Nishikawa
IPC分类号: C07D401/02 , C07D233/00 , C07D231/10 , C07D413/02 , C07D417/02
CPC分类号: C07D233/70 , C07D233/84 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要: The present invention aims to provide compounds which have an inhibitory effect on the binding between S1P and its receptor Edg-1(S1P1) and which are useful for pharmaceutical purposes.A compound represented by formula (I) or a pharmaceutically acceptable salt thereof: [wherein Ar represents a monocyclic heterocyclic ring containing one or two nitrogen atoms, A represents an oxygen atom or the like, Y1, Y2 and Y3 each represent a carbon atom or a nitrogen atom, R1 represents a hydrogen atom, a C1-C6 alkyl group or the like, R2 represents a C1-C6 alkyl group, a C3-C8 cycloalkyl group or the like, R3 represents a C1-C18 alkyl group or the like, R4 represents a hydrogen atom or a C1-C6 alkyl group, and R5 represents a C1-C10 alkyl group or the like].
摘要翻译: 本发明的目的是提供对S1P与其受体Edg-1(S1P1)之间的结合具有抑制作用并且可用于制药目的的化合物。 由式(I)表示的化合物或其药学上可接受的盐:[其中Ar表示含有一个或两个氮原子的单环杂环,A表示氧原子等,Y1,Y2和Y3表示碳原子或 氮原子,R1表示氢原子,C1-C6烷基等,R2表示C1-C6烷基,C3-C8环烷基等,R3表示C1-C18烷基等 R4代表氢原子或C1-C6烷基,R5代表C1-C10烷基等]。
-
公开(公告)号:US06822112B1
公开(公告)日:2004-11-23
申请号:US10048926
申请日:2002-02-05
申请人: Fumie Sato , Tohru Tanami , Hideo Tanaka , Naoya Ono , Makoto Yagi
发明人: Fumie Sato , Tohru Tanami , Hideo Tanaka , Naoya Ono , Makoto Yagi
IPC分类号: C07C6976
CPC分类号: C07C405/00
摘要: A prostaglandin derivative represented by the formula: wherein X is a halogen atom, R1 is a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl group, m is an integer of 0 to 5, and Y is a group represented by the formula: wherein R2 is a C3-10 cycloalkyl group, a C3-10 cycloalkyl group substituted with C1-4 alkyl group(s), a C1-4 alkyl group substituted with C3-10 cycloalkyl group(s), a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group or a bridged cyclic hydrocarbon group, or a group represented by the formula: wherein n is an integer of 1 to 8; a pharmaceutically acceptable salt thereof or a hydrate thereof.
摘要翻译: 由下式表示的前列腺素衍生物:其中X是卤素原子,R 1是氢原子,C 1-10烷基或C 3-10环烷基,m是0-5的整数,Y是 由下式表示的基团:其中R 2为C 3-10环烷基,被C 1-4烷基取代的C 3-10环烷基,被C 3-10环烷基取代的C 1-4烷基 C 1-10烷基,C 2-10烯基,C 2-10炔基或桥连环烃基,或由下式表示的基团:其中n为1至8的整数; 其药学上可接受的盐或其水合物。
-
公开(公告)号:US06740772B1
公开(公告)日:2004-05-25
申请号:US10070643
申请日:2002-03-11
申请人: Fumie Sato , Tohru Tanami , Hideo Tanaka , Naoya Ono , Makoto Yagi , Hitomi Hirano
发明人: Fumie Sato , Tohru Tanami , Hideo Tanaka , Naoya Ono , Makoto Yagi , Hitomi Hirano
IPC分类号: C07C17700
CPC分类号: C07C405/00 , C07C405/0016
摘要: A prostaglandin derivative represented by the formula: wherein X is a halogen atom in the &agr;- or &bgr;-position, Y is an ethylene group, a vinylene group or an ethynylene group, A is a group represented by the formula: O(CH2)n, S(O)p(CH2)n, O(CH2)qO(CH2)r, O(CH2)qS(O)p(CH2)r, S(O)p(CH2)qS(O)p(CH2)r or S(O)p(CH2)qO(CH2)r (wherein n is an integer of 1 to 5, p is 0, 1 or 2, q is an integer of 1 to 3, and r is 0 or 1), R1 is a C3-10 cycloalkyl group, a C1-4 alkyl-C3-10 cycloalkyl group, a C3-10 cycloalkyl-C1-4 alkyl group, a C5-10 alkyl group, a C5-10 alkenyl group, a C5-10 alkynyl group or a bridged cyclic hydrocarbon group, R2 is a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl group, and m is 0, 1 or 2], a pharmaceutically acceptable salt thereof or a hydrate thereof. The present invention is to provide novel PG derivatives having an excellent PGD2-like agonistic activity and a sleep-inducing action.
摘要翻译: 由下式表示的前列腺素衍生物:其中X是α-位或β-位的卤素原子,Y是亚乙基,亚乙烯基或亚乙炔基,A是由下式表示的基团:O(CH 2) (O)p(CH2)q(O)p(CH2)q(O)p(CH2)q(O)p(CH2) CH 2)r或S(O)p(CH 2)q O(CH 2)r(其中n为1〜5的整数,p为0,1或2,q为1〜3的整数,r为0或1 ),R 1为C 3-10环烷基,C 1-4烷基-C 3-10环烷基,C 3-10环烷基-C 1-4烷基,C 5-10烷基,C 5-10烯基 基团,C5-10炔基或桥连环烃基,R 2是氢原子,C 1-10烷基或C 3-10环烷基,m是0,1或2],药学上可接受的 其盐或其水合物。本发明提供具有优异的PGD 2样激动活性和睡眠诱导作用的新型PG衍生物。
-
公开(公告)号:US5639899A
公开(公告)日:1997-06-17
申请号:US133171
申请日:1993-10-19
申请人: Fumie Sato , Takehiro Amano , Kazuya Kameo , Tohru Tanami , Masaru Mutoh , Naoya Ono , Jun Goto
发明人: Fumie Sato , Takehiro Amano , Kazuya Kameo , Tohru Tanami , Masaru Mutoh , Naoya Ono , Jun Goto
IPC分类号: C07C405/00 , C07C59/00
CPC分类号: C07C405/00
摘要: Object: To provide novel prostaglandin E.sub.1 analogues which have more excellent pharmaceutical effects, longer duration of the effects and less side-effects than the prior art prostaglandin E.sub.1 's.Constitution: A PGE.sub.1 analogue represented by the formula: ##STR1## (wherein A is a vinylene group or an ethynylene group, R.sup.1 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or an allyl group, R.sup.2 is a branched aliphatic hydrocarbon group having 5 to 10 carbon atoms), or a salt thereof.
摘要翻译: PCT No.PCT / JP92 / 00513 Sec。 371日期:1993年10月19日 102(e)日期1993年10月19日PCT 1992年4月21日PCT PCT。 第WO92 / 18472号公报 日期1990年10月29日二氧化物目标:提供与现有技术的前列腺素E1相比,具有更优异的药物作用,更长的作用时间和更少的副作用的新型前列腺素E1类似物。 结构:由下式表示的PGE1类似物:其中A是亚乙烯基或亚乙炔基,R 1是氢原子,具有1至6个碳原子的烷基或烯丙基,R 2是支链脂族 具有5〜10个碳原子的烃基)或其盐。
-
公开(公告)号:US5491254A
公开(公告)日:1996-02-13
申请号:US373226
申请日:1995-01-19
申请人: Fumie Sato , Takehiro Amano , Kazuya Kameo , Tohru Tanami , Masaru Mutoh , Naoya Ono , Jun Goto
发明人: Fumie Sato , Takehiro Amano , Kazuya Kameo , Tohru Tanami , Masaru Mutoh , Naoya Ono , Jun Goto
IPC分类号: C07C405/00 , C07C177/00 , A61K31/557
CPC分类号: C07C405/0016 , C07C405/00
摘要: ObjectNovel PG derivatives having an excellent platelet aggregation inhibition activity are provided.ConstructionProstaglandin derivatives represented by formula: ##STR1## and salts thereof.
摘要翻译: 提供了具有优异的血小板聚集抑制活性的新型PG衍生物。 前述前列腺素衍生物,其结构式如下:< IMAGE>及其盐。
-
公开(公告)号:US09181229B2
公开(公告)日:2015-11-10
申请号:US14004997
申请日:2012-03-15
申请人: Naoya Ono , Shoichi Kuroda , Yoshihisa Shirasaki , Tetsuo Takayama , Yoshinori Sekiguchi , Fumihito Ushiyama , Yusuke Oka
发明人: Naoya Ono , Shoichi Kuroda , Yoshihisa Shirasaki , Tetsuo Takayama , Yoshinori Sekiguchi , Fumihito Ushiyama , Yusuke Oka
IPC分类号: C07D413/04 , C07D403/04 , C07D417/04 , C07D413/14
CPC分类号: C07D413/04 , C07D403/04 , C07D413/14 , C07D417/04
摘要: Provided are novel compounds that bind to FKBP12 or pharmaceutically acceptable salts thereof, as well as new therapeutics useful in the prevention or treatment of alopecia which comprise those compounds or pharmaceutically acceptable salts thereof. Specifically, compounds represented by formula (1) [where R1 represents either the following formula (2) or (3)] or pharmaceutically acceptable salts thereof are provided.
摘要翻译: 提供与FKBP12或其药学上可接受的盐结合的新化合物,以及可用于预防或治疗脱发的新治疗剂,其包含那些化合物或其药学上可接受的盐。 具体地,提供由式(1)表示的化合物[其中R 1表示下式(2)或(3)]或其药学上可接受的盐。
-
公开(公告)号:US09045466B2
公开(公告)日:2015-06-02
申请号:US14235686
申请日:2012-07-27
申请人: Tetsuya Tanikawa , Yasunobu Ushiki , Fumihito Ushiyama , Toru Yamaguchi , Naoya Ono , Keiko Yamamoto , Risa Tsuruta , Yasuhiro Tsutsui , Noritomo Fujino , Ayumu Mori
发明人: Tetsuya Tanikawa , Yasunobu Ushiki , Fumihito Ushiyama , Toru Yamaguchi , Naoya Ono , Keiko Yamamoto , Risa Tsuruta , Yasuhiro Tsutsui , Noritomo Fujino , Ayumu Mori
IPC分类号: C07D417/12 , C07D417/04 , C07D277/20 , C07D277/28 , C07D277/30 , C07D277/34 , C07D277/48 , C07D277/56 , C07D285/08
CPC分类号: C07D417/12 , C07D277/20 , C07D277/28 , C07D277/30 , C07D277/34 , C07D277/48 , C07D277/56 , C07D285/08 , C07D417/04
摘要: An amidine compound represented by formula (I) (wherein A1 represents a nitrogen atom or a group represented by formula CR6; A2 and A3 are the same as or different from each other and independently represent a nitrogen atom or a group represented by formula CH; R1 represents an aryl group which may be substituted by 1 to 5 substituents independently selected from a substituent group (2) or the like; R2 and R3 are the same as or different from each other and independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C1-6 haloalkyl group or a C1-6 alkoxy group; and R4 and R5 are the same as or different from each other and independently represent a hydrogen atom, a C1-6 haloalkyl group, a C1-6 alkyl group or the like) or a salt thereof. The compound is useful as an anti-fungal agent.
摘要翻译: 由式(I)表示的脒化合物(其中A1表示氮原子或式CR6表示的基团; A2和A3彼此相同或不同,并且独立地表示氮原子或由式CH表示的基团; R1表示可以被1〜5个独立地选自取代基(2)等的取代基取代的芳基; R2和R3彼此相同或不同,独立地表示氢原子,卤素原子, C 1-6烷基,C 1-6卤代烷基或C 1-6烷氧基; R 4和R 5彼此相同或不同,独立地表示氢原子,C1-6卤代烷基,C1 -6烷基等)或其盐。 该化合物可用作抗真菌剂。
-
公开(公告)号:US08022225B2
公开(公告)日:2011-09-20
申请号:US11659103
申请日:2005-08-04
申请人: Naoya Ono , Masakazu Sato , Fumiyasu Shiozawa , Makoto Yagi , Tetsuya Yabuuchi , Tetsuo Takayama , Hironori Katakai
发明人: Naoya Ono , Masakazu Sato , Fumiyasu Shiozawa , Makoto Yagi , Tetsuya Yabuuchi , Tetsuo Takayama , Hironori Katakai
IPC分类号: C07D249/12 , C07D249/08
CPC分类号: C07D249/12 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要: A compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof has an effect of inhibiting binding between S1P and its receptor Edg-1(S1P1), and is useful as a pharmaceutical product. [where A represents a sulfur atom, an oxygen atom, a formula —SO— or a formula —SO2—; R1 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like; R2 represents an alkyl group having 1 to 6 carbon atoms, a cycloalkyl group having 3 to 8 carbon atoms or the like; R3 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; R4 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a phenyl group or the like; R5 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; and R6 represents an alkyl group having 1 to 6 carbon atoms, a phenyl group or a substituted phenyl group].
摘要翻译: 由下式(I)表示的化合物或其药学上可接受的盐具有抑制S1P与其受体Edg-1(S1P1)结合的作用,可用作药物。 [其中A表示硫原子,氧原子,式-SO-或式-SO 2 - ; R1表示氢原子,碳原子数1〜6的烷基等; R2表示碳原子数1〜6的烷基,碳原子数3〜8的环烷基等; R3表示氢原子或碳原子数1〜6的烷基。 R4表示氢原子,碳原子数1〜6的烷基,苯基等; R5表示氢原子或碳原子数1〜6的烷基。 R6表示碳原子数1〜6的烷基,苯基或取代苯基]。
-
公开(公告)号:US20090131438A1
公开(公告)日:2009-05-21
申请号:US11659103
申请日:2005-08-04
申请人: Naoya Ono , Masakazu Sato , Fumiyasu Shiozawa , Makoto Yagi , Tetsuya Yabuuchi , Tetsuo Takayama , Hironori Katakai
发明人: Naoya Ono , Masakazu Sato , Fumiyasu Shiozawa , Makoto Yagi , Tetsuya Yabuuchi , Tetsuo Takayama , Hironori Katakai
IPC分类号: A61K31/4196 , A61P37/00 , A61P29/00 , A61P17/06 , C07D249/12 , C07D401/12 , C07D403/12 , C07D413/12 , A61K31/5377 , A61K31/454
CPC分类号: C07D249/12 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要: A compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof has an effect of inhibiting binding between S1P and its receptor Edg-1(S1P1), and is useful as a pharmaceutical product. [where A represents a sulfur atom, an oxygen atom, a formula —SO— or a formula —SO2—; R1 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like; R2 represents an alkyl group having 1 to 6 carbon atoms, a cycloalkyl group having 3 to 8 carbon atoms or the like; R3 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; R4 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a phenyl group or the like; R5 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; and R6 represents an alkyl group having 1 to 6 carbon atoms, a phenyl group or a substituted phenyl group].
摘要翻译: 由下式(I)表示的化合物或其药学上可接受的盐具有抑制S1P与其受体Edg-1(S1P1)结合的作用,可用作药物。 [其中A表示硫原子,氧原子,式-SO-或式-SO 2 - ; R1表示氢原子,碳原子数1〜6的烷基等; R2表示碳原子数1〜6的烷基,碳原子数3〜8的环烷基等; R3表示氢原子或碳原子数1〜6的烷基。 R4表示氢原子,碳原子数1〜6的烷基,苯基等; R5表示氢原子或碳原子数1〜6的烷基。 R6表示碳原子数1〜6的烷基,苯基或取代苯基]。
-
-
-
-
-
-
-
-
-