公开(公告)号：US20070129404A1

公开(公告)日：2007-06-07

申请号：US10575645

申请日：2004-10-15

申请人： Masahiko Hagihara ,  Ken-ichi Komori ,  Hidetoshi Sunamoto ,  Hiroshi Nishida ,  Takeshi Matsugi ,  Tadashi Nakajima ,  Masakazu Hatano ,  Kazutaka Kido ,  Hideaki Hara

发明人： Masahiko Hagihara ,  Ken-ichi Komori ,  Hidetoshi Sunamoto ,  Hiroshi Nishida ,  Takeshi Matsugi ,  Tadashi Nakajima ,  Masakazu Hatano ,  Kazutaka Kido ,  Hideaki Hara

IPC分类号： A61K31/4439 ,  A61K31/416 ,  C07D403/02 ,  C07D231/56

CPC分类号： C07D231/56 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04

摘要： An object of the present invention is to create a novel indazole derivative useful as a drug and to find a novel pharmacological action of the derivative. The compound of the present invention is represented by the formula [I] and has an excellent Rho kinase inhibiting action. In the formula, a ring X is a benzene ring or a pyridine ring; R1 and R2 are H or alkyl; R3 and R4 are halogen, H, OH, alkoxy, alkenyloxy, alkynyloxy, cycloalkyloxy, cycloalkenyloxy, aryloxy, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, carboxy, hydrocarbonyl, alkylcarbonyl, etc.; and R5 is halogen atom, H, OH, alkoxy, aryloxy, alkyl or aryl. Each group can be substituted.

摘要翻译： 本发明的目的是产生一种可用作药物的新型吲唑衍生物，并找到该衍生物的新药理作用。 本发明的化合物由式[I]表示，具有优异的Rho激酶抑制作用。 在该式中，环X为苯环或吡啶环; R 1和R 2均为H或烷基; R 3和R 4是卤素，H，OH，烷氧基，烯氧基，炔氧基，环烷氧基，环烯氧基，芳氧基，烷基，烯基，炔基，环烷基，环烯基，芳基， 羧基，烃基，烷基羰基等; R 5是卤素原子，H，OH，烷氧基，芳氧基，烷基或芳基。 每组可以替代。

公开(公告)号：US6020496A

公开(公告)日：2000-02-01

申请号：US308018

申请日：1999-05-12

申请人： Hiroyuki Miyata ,  Kikuo Ataka ,  Nobuya Satake ,  Masahiko Hagihara

发明人： Hiroyuki Miyata ,  Kikuo Ataka ,  Nobuya Satake ,  Masahiko Hagihara

IPC分类号： C07D263/44 ,  C07D413/04 ,  C07D417/04

CPC分类号： C07D263/44 ,  C07D413/04 ,  C07D417/04

摘要： 5-Alkoxy-2(3H)-oxazolone compounds represented by general formula (1); and a R.sup.1 process for the preparation thereof, wherein R.sup.1 is hydrogen, optionally substituted C.sub.1 -C.sub.10 alkyl, optionally substituted C.sub.3 -C.sub.10 cycloalkyl, optionally substituted C.sub.2 -C.sub.10 alkenyl or optionally substituted phenyl; R.sup.2 is hydrogen, optionally substituted C.sub.1 -C.sub.10 alkyl, optionally substituted phenyl or unsubstituted C.sub.2 -C.sub.10 alkenyl; R.sup.3 is optionally substituted C.sub.1 -C.sub.10 alkyl, optionally substituted C.sub.3 -C.sub.10 cycloalkyl, optionally substituted C.sub.2 -C.sub.10 alkenyl excluding 2-alkenyl, or optionally substituted phenyl. ##STR1##

摘要翻译： PCT No.PCT / JP97 / 04157 Sec。 371日期1999年5月12日 102（e）日期1999年5月12日PCT 1997年11月14日PCT公布。 第WO98 / 22449号公报 日期：19985年5月28日 - 由通式（1）表示的烷氧基-2（3H） - 恶唑酮化合物; 和其制备方法，其中R1为氢，任选取代的C 1 -C 10烷基，任选取代的C 3 -C 10环烷基，任选取代的C 2 -C 10烯基或任选取代的苯基; R 2是氢，任选取代的C 1 -C 10烷基，任选取代的苯基或未取代的C 2 -C 10烯基; R 3是任选取代的C 1 -C 10烷基，任选取代的C 3 -C 10环烷基，任选取代的C2-C10链烯基或任选取代的苯基。

公开(公告)号：US09187450B2

公开(公告)日：2015-11-17

申请号：US13809115

申请日：2011-07-08

申请人： Tsuyoshi Nakamura ,  Hidenori Namiki ,  Naoki Terasaka ,  Akiko Shima ,  Masahiko Hagihara ,  Noriaki Iwase ,  Katsunori Takata ,  Osamu Kikuchi ,  Kazunari Tsuboike ,  Hiroyuki Setoguchi ,  Kenji Yoneda ,  Hidetoshi Sunamoto ,  Koji Ito

发明人： Tsuyoshi Nakamura ,  Hidenori Namiki ,  Naoki Terasaka ,  Akiko Shima ,  Masahiko Hagihara ,  Noriaki Iwase ,  Katsunori Takata ,  Osamu Kikuchi ,  Kazunari Tsuboike ,  Hiroyuki Setoguchi ,  Kenji Yoneda ,  Hidetoshi Sunamoto ,  Koji Ito

IPC分类号： A01N55/00 ,  A61K31/695 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07F7/18

CPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07F7/1804

摘要： The present invention provides a substituted pyridine compound or a pharmacologically acceptable salt thereof which has excellent CETP inhibition activity and is useful as a medicament. The present invention provides a compound represented by a general formula (I), wherein R1 is H, optionally substituted alkyl, OH, optionally substituted alkoxy, alkylsulfonyl, optionally substituted amino, carboxy, optionally substituted carbonyl, CN, halogeno, optionally substituted phenyl, optionally substituted aromatic heterocyclyl, optionally substituted saturated heterocyclyl, optionally substituted saturated heterocyclyloxy or optionally substituted saturated heterocyclylcarbonyl, etc., and the like.

摘要翻译： 本发明提供了具有优异的CETP抑制活性并可用作药物的取代的吡啶化合物或其药学上可接受的盐。 本发明提供由通式（I）表示的化合物，其中R 1为H，任选取代的烷基，OH，任选取代的烷氧基，烷基磺酰基，任选取代的氨基，羧基，任选取代的羰基，CN，卤代，任选取代的苯基， 任选取代的芳族杂环基，任选取代的饱和杂环基，任选取代的饱和杂环氧基或任选取代的饱和杂环基羰基等，等等。

公开(公告)号：US08232308B2

公开(公告)日：2012-07-31

申请号：US12925367

申请日：2010-10-20

申请人： Masahiko Hagihara ,  Ken-ichi Komori ,  Hidetoshi Sunamoto ,  Hiroshi Nishida ,  Takeshi Matsugi ,  Tadashi Nakajima ,  Masakazu Hatano ,  Kazutaka Kido ,  Hideaki Hara

发明人： Masahiko Hagihara ,  Ken-ichi Komori ,  Hidetoshi Sunamoto ,  Hiroshi Nishida ,  Takeshi Matsugi ,  Tadashi Nakajima ,  Masakazu Hatano ,  Kazutaka Kido ,  Hideaki Hara

IPC分类号： A01N43/56 ,  A61K31/40 ,  C07D231/00 ,  C07D233/56

CPC分类号： C07D231/56 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04

摘要： A method for treating a disease in which Rho kinase is involved. The method is carried out by administering to a patient in need thereof a pharmaceutically effective amount of a compound of the following formula or a pharmaceutically acceptable salt thereof: wherein the ring X is a benzene ring or a pyridine ring; R1 and R2 are hydrogen or alkyl or together form a cycloalkene ring; R3 is hydrogen, substituted alkyl, unsubstituted alkenyl, carboxyl or an ester or an amide thereof, amino or a cyano; R4 is hydrogen, hydroxyl, substituted or unsubstituted alkoxy, unsubstituted alkenyloxy, unsubstituted cycloalkyloxy substituted or unsubstituted alkyl, unsubstituted alkenyl, unsubstituted cycloalkyl, amino, substituted or unsubstituted alkylamino, nitro, cyano or a monocyclic heterocycle; and R5 is a halogen atom or a hydrogen atom.

摘要翻译： 一种治疗涉及Rho激酶的疾病的方法。 该方法通过向有需要的患者施用药学有效量的下式化合物或其药学上可接受的盐进行：其中环X是苯环或吡啶环; R1和R2是氢或烷基或一起形成环烯烃环; R 3是氢，取代的烷基，未取代的烯基，羧基或其酯或酰胺，氨基或氰基; R4是氢，羟基，取代或未取代的烷氧基，未取代的烯氧基，未取代的环烷基氧基取代或未取代的烷基，未取代的烯基，未取代的环烷基，氨基，取代或未取代的烷基氨基，硝基，氰基或单环杂环; R5为卤素原子或氢原子。

公开(公告)号：US08227480B2

公开(公告)日：2012-07-24

申请号：US12227890

申请日：2007-06-08

申请人： Masahiko Hagihara ,  Yasunori Tsuzaki ,  Ken-ichi Komori ,  Hiroshi Nishida ,  Kazutaka Kido ,  Tomokazu Fujimoto ,  Takeshi Matsugi ,  Atsushi Shimazaki

发明人： Masahiko Hagihara ,  Yasunori Tsuzaki ,  Ken-ichi Komori ,  Hiroshi Nishida ,  Kazutaka Kido ,  Tomokazu Fujimoto ,  Takeshi Matsugi ,  Atsushi Shimazaki

IPC分类号： A01N43/42 ,  A61K31/44 ,  C07D211/00 ,  C07D213/00 ,  C07D215/00 ,  C07D217/00 ,  C07D219/00 ,  C07D221/00

CPC分类号： C07D231/56 ,  C07D401/04

摘要： An object of the present invention is to create a novel indazole derivative having a spiro ring structure in a side chain, which is useful as a pharmaceutical, and to find a new pharmacological activity of the derivative. The present invention compound is represented by the general formula [I] and has an excellent Rho kinase inhibitory activity. In the formula, the ring X represents a benzene ring or a pyridine ring; R1 and R2 represent halogen, H, OH, alkoxy, cycloalkyloxy, aryloxy, alkyl, cycloalkyl or the like; R3 represents halogen, H or the like; R4 and R5 represent halogen, H or the like; R6 and R7 represent H, alkyl or the like; and m, n, p and q represent an integer of 0 to 3. In this connection, each group may have a substituent.

摘要翻译： 本发明的目的是在侧链中产生具有螺环结构的新型吲唑衍生物，其可用作药物，并找到衍生物的新药理活性。 本发明化合物由通式[I]表示，具有优异的Rho激酶抑制活性。 在该式中，环X表示苯环或吡啶环; R 1和R 2表示卤素，H，OH，烷氧基，环烷氧基，芳氧基，烷基，环烷基等; R3表示卤素，H等; R4和R5表示卤素，H等; R6和R7代表H，烷基等; m，n，p和q表示0〜3的整数。就此而言，各基团可以具有取代基。

公开(公告)号：US20090203729A1

公开(公告)日：2009-08-13

申请号：US12225762

申请日：2007-04-06

申请人： Teruhiko Inoue ,  Kazuyoshi Nakamura ,  Masahiko Hagihara ,  Hiroyuki Miyata ,  Yukinori Wada ,  Naoyuki Yokota

发明人： Teruhiko Inoue ,  Kazuyoshi Nakamura ,  Masahiko Hagihara ,  Hiroyuki Miyata ,  Yukinori Wada ,  Naoyuki Yokota

IPC分类号： A61K31/4365 ,  C07D495/04 ,  A61P7/00

CPC分类号： C07D495/04

摘要： The present invention is directed to providing prasugrel hydrochloride or the like with a reduced content of OXTP. A method for producing prasugrel hydrochloride with a reduced content of OXTP, comprising dissolving free prasugrel containing OXTP in an inert solvent and adding hydrochloric acid optionally dropwise to the solution for reaction is also provided.

摘要翻译： 本发明涉及提供具有降低的OXTP含量的普拉格雷盐酸盐等。 还提供了一种生产具有降低的OXTP含量的普拉格雷盐酸盐的方法，包括将含有OXTP的游离普拉格雷溶解在惰性溶剂中，并将盐酸任选地滴加到反应溶液中。

公开(公告)号：US20060063934A1

公开(公告)日：2006-03-23

申请号：US10528994

申请日：2003-09-25

申请人： Masahiko Hagihara ,  Nobuhiko Shibakawa ,  Masamichi Nishihara ,  Toshiyuki Shirai ,  Motohisa Shimizu ,  Tohru Hasegawa ,  Yasunori Tokunaga ,  Naoto Suzuki ,  Yukinori Wada

发明人： Masahiko Hagihara ,  Nobuhiko Shibakawa ,  Masamichi Nishihara ,  Toshiyuki Shirai ,  Motohisa Shimizu ,  Tohru Hasegawa ,  Yasunori Tokunaga ,  Naoto Suzuki ,  Yukinori Wada

IPC分类号： C07D403/04

CPC分类号： C07D401/14 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  C07D403/14 ,  C07D487/04

摘要： The present invention relates to pyrazole compounds represented by the formula (I): wherein R1 represents phenyl which may be substituted, R2 represents H, halogen, alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl or substituted amino, Q represents CH or N, R3 represents H, alkyl or amino, R4 represents the formula (II) to (V): wherein R7 represents H or alkyl, R8 represents H, alkyl or substituted amino, R9 represents H or alkyl, R12 represents H, alkyl, halogeno alkyl or substituted amino, or pharmaceutically acceptable salts thereof, and a medical composition containing the same as effective ingredient.

摘要翻译： 本发明涉及由式（I）表示的吡唑化合物：

公开(公告)号：US20110039891A1

公开(公告)日：2011-02-17

申请号：US12925367

申请日：2010-10-20

申请人： Masahiko Hagihara ,  Ken-ichi Komori ,  Hidetoshi Sunamoto ,  Hiroshi Nishida ,  Takeshi Matsugi ,  Tadashi Nakajima ,  Masakazu Hatano ,  Kazutaka Kido ,  Hideaki Hara

发明人： Masahiko Hagihara ,  Ken-ichi Komori ,  Hidetoshi Sunamoto ,  Hiroshi Nishida ,  Takeshi Matsugi ,  Tadashi Nakajima ,  Masakazu Hatano ,  Kazutaka Kido ,  Hideaki Hara

IPC分类号： A61K31/454 ,  A61K31/415 ,  A61K31/4439 ,  A61K31/422 ,  A61K31/42 ,  A61P27/02 ,  A61P27/06

CPC分类号： C07D231/56 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04

摘要： A method for treating a disease in which Rho kinase is involved. The method is carried out by administering to a patient in need thereof a pharmaceutically effective amount of a compound of the following formula or a pharmaceutically acceptable salt thereof: wherein the ring X is a benzene ring or a pyridine ring; R1 and R2 are hydrogen or alkyl or together form a cycloalkene ring; R3 is hydrogen, substituted alkyl, unsubstituted alkenyl, carboxyl or an ester or an amide thereof, amino or a cyano; R4 is hydrogen, hydroxyl, substituted or unsubstituted alkoxy, unsubstituted alkenyloxy, unsubstituted cycloalkyloxy substituted or unsubstituted alkyl, unsubstituted alkenyl, unsubstituted cycloalkyl, amino, substituted or unsubstituted alkylamino, nitro, cyano or a monocyclic heterocycle; and R5 is a halogen atom or a hydrogen atom.

摘要翻译： 一种治疗涉及Rho激酶的疾病的方法。 该方法通过向有需要的患者施用药学有效量的下式化合物或其药学上可接受的盐进行：其中环X是苯环或吡啶环; R1和R2是氢或烷基或一起形成环烯烃环; R 3是氢，取代的烷基，未取代的烯基，羧基或其酯或酰胺，氨基或氰基; R4是氢，羟基，取代或未取代的烷氧基，未取代的烯氧基，未取代的环烷基氧基取代或未取代的烷基，未取代的烯基，未取代的环烷基，氨基，取代或未取代的烷基氨基，硝基，氰基或单环杂环; R5为卤素原子或氢原子。

公开(公告)号：US07855222B2

公开(公告)日：2010-12-21

申请号：US12456652

申请日：2009-06-19

申请人： Masahiko Hagihara ,  Ken-ichi Komori ,  Hidetoshi Sunamoto ,  Hiroshi Nishida ,  Takeshi Matsugi ,  Tadashi Nakajima ,  Masakazu Hatano ,  Kazutaka Kido ,  Hideaki Hara

发明人： Masahiko Hagihara ,  Ken-ichi Komori ,  Hidetoshi Sunamoto ,  Hiroshi Nishida ,  Takeshi Matsugi ,  Tadashi Nakajima ,  Masakazu Hatano ,  Kazutaka Kido ,  Hideaki Hara

IPC分类号： A01N43/56 ,  A61K31/40 ,  C07D231/00 ,  C07D233/56

CPC分类号： C07D231/56 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04

摘要： A method for treating a disease in which Rho kinase is involved. The method is carried out by administering to a patient in need thereof a pharmaceutically effective amount of a compound of the following formula or a pharmaceutically acceptable salt thereof: wherein the ring X is a benzene ring or a pyridine ring; R1 and R2 are hydrogen or alkyl or together form a cycloalkene ring; R3 is hydrogen, substituted alkyl, unsubstituted alkenyl, carboxyl or an ester or an amide thereof, amino or a cyano; R4 is hydrogen, hydroxyl, substituted or unsubstituted alkoxy, unsubstituted alkenyloxy, unsubstituted cycloalkyloxy, substituted or unsubstituted alkyl, unsubstituted alkenyl, unsubstituted cycloalkyl, amino, substituted or unsubstituted alkylamino, nitro, cyano or a monocyclic heterocycle; and R5 is a halogen atom or a hydrogen atom.

摘要翻译： 一种治疗涉及Rho激酶的疾病的方法。 该方法通过向有需要的患者施用药学有效量的下式化合物或其药学上可接受的盐进行：其中环X是苯环或吡啶环; R1和R2是氢或烷基或一起形成环烯烃环; R 3是氢，取代的烷基，未取代的烯基，羧基或其酯或酰胺，氨基或氰基; R4是氢，羟基，取代或未取代的烷氧基，未取代的烯氧基，未取代的环烷基氧基，取代或未取代的烷基，未取代的烯基，未被取代的环烷基，氨基，取代或未取代的烷基氨基，硝基，氰基或单环杂环; R5为卤素原子或氢原子。

公开(公告)号：US20090264468A1

公开(公告)日：2009-10-22

申请号：US12456652

申请日：2009-06-19

申请人： Masahiko Hagihara ,  Ken-ichi Komori ,  Hidetoshi Sunamoto ,  Hiroshi Nishida ,  Takeshi Matsugi ,  Tadashi Nakajima ,  Masakazu Hatano ,  Kazutaka Kido ,  Hideaki Hara

发明人： Masahiko Hagihara ,  Ken-ichi Komori ,  Hidetoshi Sunamoto ,  Hiroshi Nishida ,  Takeshi Matsugi ,  Tadashi Nakajima ,  Masakazu Hatano ,  Kazutaka Kido ,  Hideaki Hara

IPC分类号： A61K31/454 ,  A61K31/416 ,  A61K31/4439 ,  A61K31/421 ,  A61K31/42 ,  A61P9/00 ,  A61P11/00 ,  A61P35/00 ,  A61P29/00 ,  A61P15/00

CPC分类号： C07D231/56 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04

摘要： A method for treating a disease in which Rho kinase is involved. The method is carried out by administering to a patient in need thereof a pharmaceutically effective amount of a compound of the following formula or a pharmaceutically acceptable salt thereof: , wherein the ring X is a benzene ring or a pyridine ring; R1 and R2 are hydrogen or alkyl or together form a cycloalkene ring; R3 is hydrogen, substituted alkyl, unsubstituted alkenyl, carboxyl or an ester or an amide thereof, amino or a cyano; R4 is hydrogen, hydroxyl, substituted or unsubstituted alkoxy, unsubstituted alkenyloxy, unsubstituted cycloalkyloxy, substituted or unsubstituted alkyl, unsubstituted alkenyl, unsubstituted cycloalkyl, amino, substituted or unsubstituted alkylamino, nitro, cyano or a monocyclic heterocycle; and R5 is a halogen atom or a hydrogen atom.

摘要翻译： 一种治疗涉及Rho激酶的疾病的方法。 该方法通过向有需要的患者施用药学有效量的下式化合物或其药学上可接受的盐进行：其中环X是苯环或吡啶环; R1和R2是氢或烷基或一起形成环烯烃环; R 3是氢，取代的烷基，未取代的烯基，羧基或其酯或酰胺，氨基或氰基; R4是氢，羟基，取代或未取代的烷氧基，未取代的烯氧基，未取代的环烷基氧基，取代或未取代的烷基，未取代的烯基，未被取代的环烷基，氨基，取代或未取代的烷基氨基，硝基，氰基或单环杂环; R5为卤素原子或氢原子。