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1. 发明申请

US20120184521A1 SUBSTITUTED AMIDE COMPOUND 有权
标题翻译：取代的化合物
公开(公告)号：US20120184521A1
公开(公告)日：2012-07-19
申请号：US13498159
申请日：2010-09-24
申请人： Eiji Kawaminami , Tatsuhisa Takahashi , Takatoshi Kanayama , Yuta Fukuda , Hiroyuki Kaizawa , Yutaka Kondoh , Ryushi Seo , Kazuyuki Kuramoto , Kazuhiko Take , Kazuyuki Sakamoto
发明人： Eiji Kawaminami , Tatsuhisa Takahashi , Takatoshi Kanayama , Yuta Fukuda , Hiroyuki Kaizawa , Yutaka Kondoh , Ryushi Seo , Kazuyuki Kuramoto , Kazuhiko Take , Kazuyuki Sakamoto
IPC分类号： A61K31/426 , C07D417/12 , A61K31/427 , A61K31/496 , A61P43/00 , A61K31/513 , A61K31/538 , A61K31/454 , A61K31/541 , C07D277/56 , A61K31/4439
CPC分类号： A61K31/426 , A61K31/341 , A61K31/381 , A61K31/401 , A61K31/415 , A61K31/42 , A61K31/427 , A61K31/44 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/4965 , C07D207/34 , C07D213/81 , C07D263/34 , C07D277/56 , C07D307/68 , C07D333/38 , C07D417/12
摘要： A substituted amide compound is useful as an active ingredient of a pharmaceutical composition, in particular a pharmaceutical composition for treating diseases caused by lysophosphatidic acid (LPA). The compound is of a formula: In this formula, A is an optionally substituted aryl, etc.; B is an optionally substituted 5-membered aromatic hetero ring group; X is a single bond or —(CRX1RX2)n—; n is 1, 2, 3, or 4; RX1 and RX2 are hydrogen, etc.; Y1 to Y5 are each CRY or N; each RY is hydrogen, etc.; R1 and R2 are hydrogen, etc.; m is 1, 2, or 3; R3 is hydrogen, etc.; and R4 is an optionally substituted lower alkyl, etc.
摘要翻译：取代的酰胺化合物可用作药物组合物的活性成分，特别是用于治疗由溶血磷脂酸（LPA）引起的疾病的药物组合物。该化合物具有下式：在该式中，A是任选取代的芳基等; B是任选取代的5元芳族杂环基团; X是单键或 - （CRX1RX2）n-; n为1,2,3或4; RX1和RX2是氢等; Y1〜Y5分别为CRY或N; 每个RY是氢等; R1和R2是氢等; m为1,2或3; R3是氢等; 并且R 4是任选取代的低级烷基等。

2. 发明授权

US07166598B2 Piperazine derivatives 失效
标题翻译：哌嗪衍生物
公开(公告)号：US07166598B2
公开(公告)日：2007-01-23
申请号：US10968473
申请日：2004-10-20
申请人： Kazuhiko Take , Nobukiyo Konishi , Shinji Shigenaga , Natsuko Kayakiri , Hidenori Azami , Yoshiteru Eikyu , Kazuo Nakai , Junya Ishida , Masataka Morita
发明人： Kazuhiko Take , Nobukiyo Konishi , Shinji Shigenaga , Natsuko Kayakiri , Hidenori Azami , Yoshiteru Eikyu , Kazuo Nakai , Junya Ishida , Masataka Morita
IPC分类号： A61K31/5355 , C07D413/06 , A61K31/496 , C07D401/06
CPC分类号： C07D401/06 , C07D241/04 , C07D401/14 , C07D403/06 , C07D403/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D471/04 , C07D491/08 , C07D495/04 , C07D498/04 , C07D498/08 , C07F7/1804
摘要： This invention relates to piperazine derivatives of the formula: wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising the same, and to a use of the same for treating or preventing Tachykinin-mediated diseases in human being or animals.
摘要翻译：本发明涉及下式的哌嗪衍生物：其中每个符号如说明书中所定义，及其药学上可接受的盐，其制备方法，包含其的药物组合物及其用于治疗或预防的用途速激肽介导的人类或动物疾病。

3. 发明授权

US5256824A Substituted-amine compound and a process for the preparation thereof 失效
标题翻译：取代的胺化合物及其制备方法
公开(公告)号：US5256824A
公开(公告)日：1993-10-26
申请号：US665669
申请日：1991-03-07
申请人： Youichi Shiokawa , Kazuo Okumura , Kazuhiko Take , Kazunori Tsubaki
发明人： Youichi Shiokawa , Kazuo Okumura , Kazuhiko Take , Kazunori Tsubaki
IPC分类号： A61K31/13 , A61K31/135 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P11/00 , A61P13/02 , A61P15/00 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/04 , C07C209/04 , C07C209/24 , C07C209/68 , C07C211/00 , C07C211/40 , C07C213/00 , C07C213/02 , C07C215/08 , C07C215/42 , C07C215/44 , C07D295/02 , C07D295/033 , C07D295/08
CPC分类号： C07D295/033 , C07C211/40 , C07C215/08 , C07C215/42 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2101/10 , C07C2101/14 , C07C2101/16
摘要： The compound (-)-N-t-butyl-4,4-diphenyl-2-cyclopentenylamine, or its hydrochloride salt has anticholinergic activity, and thus has a variety of pharmaceutical utilities.

4. 发明授权

US5192779A Substituted-acetamide compound and a process for the preparation thereof 失效
标题翻译：取代的乙酰胺化合物及其制备方法
公开(公告)号：US5192779A
公开(公告)日：1993-03-09
申请号：US751120
申请日：1991-08-28
申请人： Youichi Shiokawa , Kazuo Okumura , Kazuhiko Take , Kazunori Tsubaki
发明人： Youichi Shiokawa , Kazuo Okumura , Kazuhiko Take , Kazunori Tsubaki
IPC分类号： C07C233/40 , C07C235/34 , C07C237/20 , C07C237/22 , C07D211/22 , C07D211/26 , C07D211/46 , C07D211/70 , C07D213/40 , C07D233/34 , C07D295/125 , C07D335/14
CPC分类号： C07D213/40 , C07C233/40 , C07C235/34 , C07C237/20 , C07C237/22 , C07D211/22 , C07D211/26 , C07D211/46 , C07D211/70 , C07D233/34 , C07D295/125 , C07D335/14 , C07C2101/02 , C07C2101/08 , C07C2101/14 , C07C2101/18
摘要： Compounds of the formula ##STR1## wherein R.sup.1 is aryl which may have one or more suitable substituent(s)R.sup.2 is aryl which may have one or more suitable substituent(s), lower alkyl or cyclo(lower)alkyl,R.sup.3 is hydrogen, hydroxy, halogen, lower alkenyl, amino or protected amino,R.sup.4 is a group of the formula: ##STR2## wherein R.sup.5 is lower alkyl which may have one or more suitable substituent(s), cyclo(lower)alkyl, aryl, ar(lower)alkyl which may have one or more suitable substituent(s), andR.sup.6 is hydrogen or lower alkyl; or N-containing heterocyclic group which may have one or more suitable substituent(s), andA is lower alkylene or lower alkynylene, in which R.sup.1 and R.sup.2 may be linked through an oxygen atom, their preparation and use in treatment of dysuria, and starting materials for their preparation.
摘要翻译：其中R 1是可以具有一个或多个合适的取代基的芳基的化合物R 2是可具有一个或多个合适取代基的芳基，低级烷基或环（低级）烷基，R 3是氢，羟基，卤素，低级烯基，氨基或保护的氨基，R4是下式的基团：其中R5是可以具有一个或多个合适取代基的低级烷基，环（低级）烷基，芳基，低级）烷基，其可以具有一个或多个合适的取代基，并且R 6是氢或低级烷基; 或可以具有一个或多个合适的取代基的含氮杂环基，A是低级亚烷基或低级亚炔基，其中R 1和R 2可以通过氧原子连接，其制备和用于治疗排尿困难，以及起始材料的准备。

5. 发明授权

US4725601A Certain imidazo[1,2-a]pyridines useful in the treatment of ulcers 失效
标题翻译：某些咪唑并[1,2-a]吡啶可用于治疗溃疡
公开(公告)号：US4725601A
公开(公告)日：1988-02-16
申请号：US865331
申请日：1986-05-21
申请人： Ikuo Ueda , Youichi Shiokawa , Kazuhiko Take , Hiromichi Itani
发明人： Ikuo Ueda , Youichi Shiokawa , Kazuhiko Take , Hiromichi Itani
IPC分类号： A61K31/44 , A61K31/495 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： Certain imidazo[1,2-a]heterocyclic compounds useful in the treatment of ulcers are provided.
摘要翻译：提供了可用于治疗溃疡的某些咪唑并[1,2-a]杂环化合物。

6. 发明授权

US08669246B2 Substituted amide compound 有权
标题翻译：取代的酰胺化合物
公开(公告)号：US08669246B2
公开(公告)日：2014-03-11
申请号：US13498159
申请日：2010-09-24
申请人： Eiji Kawaminami , Tatsuhisa Takahashi , Takatoshi Kanayama , Yuta Fukuda , Hiroyuki Kaizawa , Yutaka Kondoh , Ryushi Seo , Kazuyuki Kuramoto , Kazuhiko Take , Kazuyuki Sakamoto
发明人： Eiji Kawaminami , Tatsuhisa Takahashi , Takatoshi Kanayama , Yuta Fukuda , Hiroyuki Kaizawa , Yutaka Kondoh , Ryushi Seo , Kazuyuki Kuramoto , Kazuhiko Take , Kazuyuki Sakamoto
IPC分类号： A61K31/341 , A61K31/381 , A61K31/401 , A61K31/415 , C07D207/34 , C07D213/81 , C07D263/34 , C07D277/56 , C07D307/68 , C07D333/38 , C07D417/12
CPC分类号： A61K31/426 , A61K31/341 , A61K31/381 , A61K31/401 , A61K31/415 , A61K31/42 , A61K31/427 , A61K31/44 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/4965 , C07D207/34 , C07D213/81 , C07D263/34 , C07D277/56 , C07D307/68 , C07D333/38 , C07D417/12
摘要： A substituted amide compound is useful as an active ingredient of a pharmaceutical composition, in particular a pharmaceutical composition for treating diseases caused by lysophosphatidic acid (LPA). The compound is of a formula: In this formula, A is an optionally substituted aryl, etc.; B is an optionally substituted 5-membered aromatic hetero ring group; X is a single bond or —(CRX1RX2)n—; n is 1, 2, 3, or 4; RX1 and RX2 are hydrogen, etc.; Y1 to Y5 are each CRY or N; each RY is hydrogen, etc.; R1 and R2 are hydrogen, etc.; m is 1, 2, or 3; R3 is hydrogen, etc.; and R4 is an optionally substituted lower alkyl, etc.
摘要翻译：取代的酰胺化合物可用作药物组合物的活性成分，特别是用于治疗由溶血磷脂酸（LPA）引起的疾病的药物组合物。该化合物具有下式：在该式中，A是任选取代的芳基等; B是任选取代的5元芳族杂环基团; X是单键或 - （CRX1RX2）n-; n为1,2,3或4; RX1和RX2是氢等; Y1〜Y5分别为CRY或N; 每个RY是氢等; R1和R2是氢等; m为1,2或3; R3是氢等; 并且R 4是任选取代的低级烷基等。

7. 发明申请

US20070123532A1 PIPERAZINE DERIVATIVES 审中-公开
标题翻译：哌嗪衍生物
公开(公告)号：US20070123532A1
公开(公告)日：2007-05-31
申请号：US11562149
申请日：2006-11-21
申请人： Kazuhiko Take , Nobukiyo Konishi , Shinji Shigenaga , Natsuko Kayakiri , Hidenori Azami , Yoshiteru Eikyu , Kazuo Nakai , Junya Ishida , Masataka Morita
发明人： Kazuhiko Take , Nobukiyo Konishi , Shinji Shigenaga , Natsuko Kayakiri , Hidenori Azami , Yoshiteru Eikyu , Kazuo Nakai , Junya Ishida , Masataka Morita
IPC分类号： A61K31/5377 , A61K31/496
CPC分类号： C07D401/06 , C07D241/04 , C07D401/14 , C07D403/06 , C07D403/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D471/04 , C07D491/08 , C07D495/04 , C07D498/04 , C07D498/08 , C07F7/1804
摘要： This invention relates to piperazine derivatives of the formula: wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising the same, and to a use of the same for treating or preventing Tachykinin-mediated diseases in human being or animals.
摘要翻译：本发明涉及下式的哌嗪衍生物：其中每个符号如说明书中所定义，及其药学上可接受的盐，其制备方法，包含其的药物组合物及其用于治疗或预防的用途速激肽介导的人类或动物疾病。

8. 发明授权

US6087357A Piperazine derivatives as tachykinin antagonists 失效
标题翻译：哌嗪衍生物作为速激肽拮抗剂
公开(公告)号：US6087357A
公开(公告)日：2000-07-11
申请号：US91269
申请日：1998-06-18
申请人： Masaaki Matsuo , Takashi Manabe , Nobukiyo Konishi , Kazuhiko Take , Norihiro Igari , Shinji Shigenaga , Hiroshi Matsuda , Tadashi Terasaka
发明人： Masaaki Matsuo , Takashi Manabe , Nobukiyo Konishi , Kazuhiko Take , Norihiro Igari , Shinji Shigenaga , Hiroshi Matsuda , Tadashi Terasaka
IPC分类号： A61K31/00 , A61K31/495 , A61K31/4965 , A61K31/497 , A61K31/535 , A61K31/5375 , A61K31/54 , A61K31/541 , A61K31/55 , A61P1/00 , A61P1/08 , A61P25/00 , A61P43/00 , C07D241/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/06 , C07D413/06 , C07D413/14 , C07D417/14 , C07D471/08 , C07D487/08 , C07D495/04 , C07D413/00 , C07D417/00
CPC分类号： C07D401/12 , C07D241/04 , C07D401/14 , C07D403/04 , C07D403/06
摘要： This application is a 371 of PCT/JP96/03641 filed Dec. 12, 1996.
摘要翻译： PCT No.PCT / JP96 / 03641 Sec。 371日期1998年6月18日 102（e）1998年6月18日PCT 1996年12月12日PCT PCT。公开号WO97 / 22597 日期：1997年6月26日

9. 发明授权

US5387710A Ethanolamine derivatives having sympathomimetic and anti-pollakiuria activities 失效
标题翻译：乙醇胺衍生物具有交感神经和抗尿频活性
公开(公告)号：US5387710A
公开(公告)日：1995-02-07
申请号：US117163
申请日：1993-09-17
申请人： Youichi Shiokawa , Masanobu Nagano , Kiyoshi Taniguchi , Kazuhiko Take , Takeshi Kato , Kazunori Tsubaki
发明人： Youichi Shiokawa , Masanobu Nagano , Kiyoshi Taniguchi , Kazuhiko Take , Takeshi Kato , Kazunori Tsubaki
IPC分类号： A61K31/13 , A61K31/135 , A61K31/19 , A61K31/24 , A61K31/275 , A61K31/34 , A61K31/341 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/42 , A61K31/4245 , A61K31/425 , A61K31/426 , A61K31/428 , A61K31/433 , A61K31/47 , A61P7/10 , A61P25/02 , C07C215/08 , C07C215/14 , C07C215/16 , C07C215/30 , C07C215/64 , C07C217/74 , C07C219/30 , C07C227/18 , C07C229/16 , C07C229/18 , C07C229/32 , C07C229/42 , C07C229/44 , C07C229/46 , C07C235/20 , C07C255/26 , C07C323/25 , C07D209/04 , C07D209/48 , C07D213/61 , C07D215/12 , C07D235/14 , C07D253/00 , C07D257/02 , C07D261/08 , C07D271/06 , C07D271/08 , C07D271/10 , C07D271/12 , C07D277/20 , C07D277/62 , C07D285/04 , C07D307/52 , C07D317/58 , C07D487/04 , C07D521/00 , C07C229/40 , A01N33/02
CPC分类号： C07C229/16 , C07C215/08 , C07C215/14 , C07C215/64 , C07C217/74 , C07C235/20 , C07D213/61 , C07D271/12 , C07D317/58 , C07C2102/12 , Y02P20/55
摘要： This invention relates to new ethanolamine derivatives having gut selective sympathomimetic and anti-pollakiuria activities and represented by the general formula [I]: ##STR1## wherein R.sup.1 is aryl or a heterocyclic group, each of which may be substituted with halogen, etc.,R.sup.2 is hydrogen, halogen, nitro, hydroxy, lower alkyl optionally substituted with acyl, lower alkenyl optionally substituted with acyl, lower alkoxy optionally substituted with acyl, or amino optionally substituted with acyl(lower)alkyl,R.sup.3 is hydrogen, an N-protective group, or lower alkyl optionally substituted with lower alkylthio,n is an integer of 0 to 3, anda heavy solid line means a single bond or a double bond,provided that when n is 1, then1) R.sup.1 is a condensed aromatic hydrocarbon group or a heterocyclic group, each of which may be substituted with halogen, etc., and the like,and pharmaceutically acceptable salts thereof to processes for the preparation thereof and to a pharmaceutical composition comprising the same.
摘要翻译：本发明涉及具有肠选择性交感神经和抗血尿功能的新型乙醇胺衍生物，其通式[I]表示：其中R 1为可被卤素取代的芳基或杂环基，等等，R2是氢，卤素，硝基，羟基，任选被酰基取代的低级烷基，任选被酰基取代的低级烯基，任选被酰基取代的低级烷氧基或任选被酰基（低级）烷基取代的氨基，R 3是氢， N-保护基或任选被低级烷硫基取代的低级烷基，n为0〜3的整数，重实线表示单键或双键，条件是当n为1时，则R1为稠合芳香族烃基或杂环基，其各自可以被卤素等取代，以及其药学上可接受的盐，其制备方法和药物组合物组合物上升一样

10. 发明授权

US06521643B1 Pyridine compounds and their pharmaceutical use 失效
标题翻译：吡啶化合物及其药物用途
公开(公告)号：US06521643B1
公开(公告)日：2003-02-18
申请号：US09913715
申请日：2001-08-17
申请人： Masaki Tomishima , Kazuhiko Take
发明人： Masaki Tomishima , Kazuhiko Take
IPC分类号： A61K3144
CPC分类号： C07D401/04 , C07D213/58 , C07D213/61 , C07D213/63 , C07D213/73 , C07D213/85 , C07D417/04 , C07D417/06 , C07D417/12
摘要： A compound of formula (I) wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof possess a strong inhibitory activity on the production of nitric oxide (NO), and are useful for prevention and/or treatment of NOS(nitric oxide synthasey)-mediated diseases such as adult respiratory distress syndrome, myocarditis, synovitis, septic shock, insulin-ependent diabetes mellitus, ulcerative colitis, cerebral infarction, rheumatoid arthritis, osteoarthritis, osteoporosis, systemic lupus erythematosus, rejection by organ transplantation, asthma, pain, ulcer, and the like in human being and animals.
摘要翻译：式（I）的化合物，其中每个符号如说明书中所定义，及其药学上可接受的盐。本发明的化合物（I）及其药学上可接受的盐对一氧化氮（NO）的产生具有很强的抑制活性，可用于预防和/或治疗NOS（一氧化氮合酶）介导的疾病，例如成人呼吸窘迫综合征，心肌炎，滑膜炎，脓毒性休克，胰岛素 - 后遗症糖尿病，溃疡性结肠炎，脑梗死，类风湿性关节炎，骨关节炎，骨质疏松症，系统性红斑狼疮，器官移植排斥反应，哮喘，疼痛，溃疡等人类和动物。

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