公开(公告)号：US20110028476A1

公开(公告)日：2011-02-03

申请号：US12873971

申请日：2010-09-01

申请人： Masahiro Kajino ,  Atsushi Hasuoka ,  Naoki Tarui ,  Terufumi Takagi

发明人： Masahiro Kajino ,  Atsushi Hasuoka ,  Naoki Tarui ,  Terufumi Takagi

IPC分类号： A61K31/5377 ,  C07D207/48 ,  A61K31/40 ,  C07D409/12 ,  A61K31/4025 ,  C07D403/12 ,  A61K31/506 ,  C07D401/12 ,  A61K31/4439 ,  C07D405/12 ,  C07D417/12 ,  A61K31/428 ,  A61K31/4178 ,  C07D403/04 ,  A61K31/4155 ,  C07D487/04 ,  A61K31/519 ,  A61K31/501 ,  C07D413/12 ,  A61P1/00

CPC分类号： C07D207/48 ,  A61K31/4025 ,  A61K31/41 ,  A61K31/4439 ,  A61K31/501 ,  A61K31/506 ,  C07D207/335 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D417/12 ,  C07D487/04

摘要： A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof. or a prodrug thereof is provided.

摘要翻译： 一种含有式（I）表示的化合物的质子泵抑制剂，其中X和Y相同或不同，并且各自是主链中的键或具有1至20个碳原子的间隔基，R 1是任选取代的烃基或 任选取代的杂环基，R 2，R 3和R 4相同或不同，各自为氢原子，任选取代的烃基，任选取代的噻吩基，任选取代的苯并[b]噻吩基，任选取代的呋喃基 ，任选取代的吡啶基，任选取代的吡唑基，任选取代的嘧啶基，酰基，卤素原子，氰基或硝基，R 5和R 6相同或不同，各自为氢原子或 任选取代的烃基，其具有优异的质子泵作用，并且在体内转化为质子泵抑制剂之后显示出抗溃疡活性等，或其中的盐 的。 或其前药。

公开(公告)号：US07795267B2

公开(公告)日：2010-09-14

申请号：US10570270

申请日：2004-08-26

申请人： Kohji Fukatsu ,  Yutaka Nakayama ,  Naoki Tarui ,  Masaaki Mori ,  Hirokazu Matsumoto ,  Osamu Kurasawa ,  Hiroshi Banno

发明人： Kohji Fukatsu ,  Yutaka Nakayama ,  Naoki Tarui ,  Masaaki Mori ,  Hirokazu Matsumoto ,  Osamu Kurasawa ,  Hiroshi Banno

IPC分类号： A61K31/4965

CPC分类号： C07D487/04 ,  C07D513/04

摘要： The present invention provides a compound represented by the formula: wherein R1 is —(C═O)—NR7R8 or —(C═O)—OR6, R2 is a hydrocarbon group which may be substituted or the like, R3 is a hydrocarbon group which may be substituted or the like, R4 is a hydrocarbon group which may be substituted or the like, n is from 0 to 4, and X is an oxygen atom, or a salt thereof. The invention also provides a compound which has a TGR23 antagonist activity and thus is useful for prevention and treatment of cancer.

摘要翻译： 本发明提供由下式表示的化合物：其中R 1为 - （C = O）-NR 7 R 8或 - （C = O）-OR 6，R 2为可被取代的烃基等，R 3为烃基 其可以被取代或类似，R 4是可以被取代的烃基等，n是0-4，X是氧原子或其盐。 本发明还提供具有TGR23拮抗剂活性的化合物，因此可用于预防和治疗癌症。

公开(公告)号：US07622487B2

公开(公告)日：2009-11-24

申请号：US10516252

申请日：2003-05-29

申请人： Yoshinori Ikeura ,  Tadatoshi Hashimoto ,  Naoki Tarui ,  Junya Shirai

发明人： Yoshinori Ikeura ,  Tadatoshi Hashimoto ,  Naoki Tarui ,  Junya Shirai

IPC分类号： A61K31/445 ,  C07D403/12

CPC分类号： C07D405/14 ,  C07D211/46 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/10 ,  C07D409/06 ,  C07D409/10 ,  C07D413/06 ,  C07D413/10 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14

摘要： The present invention provides a compound represented by the formula: wherein Ar is an aryl group, an aralkyl group or an aromatic heterocyclic group, each of which may be substituted, R1 is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group or an optionally substituted heterocyclic group, X is an oxygen atom or an optionally substituted imino group, Z is an optionally substituted methylene group, Ring A is an optionally further substituted piperidine ring, and Ring B is an optionally substituted aromatic ring, provided that when Z is a methylene group substituted with an oxo group, R1 is not a methyl group, and when Z is a methylene group substituted with a methyl group, Ring B is a substituted aromatic ring, or a salt thereof, which is a novel piperidine derivative having excellent antagonistic action for a tachykinin receptor and useful as a medicament, particularly an agent for preventing and/or treating urinary frequency and/or urinary incontinence.

摘要翻译： 本发明提供由下式表示的化合物：其中Ar是芳基，芳烷基或芳族杂环基，其各自可以被取代，R 1是氢原子，任选取代的烃基，酰基或 任选取代的杂环基，X是氧原子或任选取代的亚氨基，Z是任选取代的亚甲基，环A是任选进一步取代的哌啶环，环B是任选取代的芳环，条件是当Z 是被氧基取代的亚甲基，R1不是甲基，当Z是被甲基取代的亚甲基时，环B是取代的芳香环或其盐，它是具有 用于速激肽受体的优异拮抗作用，可用作药物，特别是用于预防和/或治疗尿频和/或尿失禁的药剂。

公开(公告)号：US20090275568A1

公开(公告)日：2009-11-05

申请号：US12498629

申请日：2009-07-07

申请人： Masahiro Kajino ,  Nicholas William Hird ,  Naoki Tarui ,  Hiroshi Banno ,  Yasuhiko Kawano ,  Nobuhiro Inatomi

发明人： Masahiro Kajino ,  Nicholas William Hird ,  Naoki Tarui ,  Hiroshi Banno ,  Yasuhiko Kawano ,  Nobuhiro Inatomi

IPC分类号： A61K31/437 ,  C07D471/04 ,  C07D413/14 ,  C07D417/14 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/541 ,  A61P1/00 ,  A61P25/24

CPC分类号： C07D471/04

摘要： The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) wherein R1 is a hydrogen atom and the like; R2 is a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; R3 is unsubstituted (i.e., absence), a hydrogen atom and the like; R4 and R5 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; R6 is (cyclic group optionally having substituent(s))-carbonyl, and the like; R7, R8, R9 and R10 are the same or different and each is a hydrogen atom, halogen and the like; or R7 and R8, R8 and R9, and R9 and R10 may form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5; represents unsubstituted (i.e., absence) or a single bond; and represents a single bond or a double bond, or a salt thereof, and the like.

摘要翻译： 本发明旨在提供具有神经激肽2（NK2）受体拮抗作用的喹啉衍生物，其涉及式（I）表示的化合物，其中R1为氢原子等; R2是氢原子，任选具有取代基的烃基等; R3是未取代的（即不存在），氢原子等; R 4和R 5相同或不同，各自为氢原子，任选具有取代基的烃基等; R6是（任选具有取代基的环状基团） - 羰基等; R 7，R 8，R 9和R 10相同或不同，各自为氢原子，卤素等; 或R 7和R 8，R 8和R 9，并且R 9和R 10可与相邻碳原子一起形成环; n为1〜5的整数， 表示未取代的（即不存在）或单键; ＆lt; img id =“CUSTOM-CHARACTER-00002”he =“2.46mm”wi =“4.23mm”file =“US20090275568A1-20091105-P00002.TIF”img-content =“character”img-format =“tif”/ >表示单键或双键，或其盐等。

公开(公告)号：US20080139639A1

公开(公告)日：2008-06-12

申请号：US11664346

申请日：2005-09-30

申请人： Masahiro Kajino ,  Atsushi Hasuoka ,  Naoki Tarui ,  Terufumi Takagi

发明人： Masahiro Kajino ,  Atsushi Hasuoka ,  Naoki Tarui ,  Terufumi Takagi

IPC分类号： A61K31/40 ,  C07D207/48 ,  A61P1/04

CPC分类号： C07D207/48 ,  A61K31/4025 ,  A61K31/41 ,  A61K31/4439 ,  A61K31/501 ,  A61K31/506 ,  C07D207/335 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D417/12 ,  C07D487/04

摘要： A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof. or a prodrug thereof is provided.

摘要翻译： 一种质子泵抑制剂，其含有式（I）表示的化合物，其中X和Y相同或不同，并且各自是主链中具有1至20个碳原子的键或间隔基，R 1 >是任选取代的烃基或任选取代的杂环基，R 2，R 3和R 4相同或不同，并且各自 任选取代的苯并[b]噻吩基，任选取代的呋喃基，任意取代的吡啶基，任意取代的吡唑基，任意取代的嘧啶基 ，酰基，卤素原子，氰基或硝基，R 5和R 6相同或不同，各自为氢原子或任选地 取代烃基，其具有优异的质子泵作用，并显示出抗溃疡活性等 转化为体内的质子泵抑制剂或其盐。 或其前药。

公开(公告)号：US20080039452A1

公开(公告)日：2008-02-14

申请号：US11587788

申请日：2005-04-28

申请人： Masahiro Kajino ,  Nicholas Hird ,  Naoki Tarui ,  Hiroshi Banno ,  Yasuhiko Kawano ,  Nobuhiro Inatomi

发明人： Masahiro Kajino ,  Nicholas Hird ,  Naoki Tarui ,  Hiroshi Banno ,  Yasuhiko Kawano ,  Nobuhiro Inatomi

IPC分类号： A61K31/535 ,  A61P1/00 ,  C07D471/00

CPC分类号： C07D471/04

摘要： The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) wherein R1 is a hydrogen atom and the like; R2 is a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; R3 is unsubstituted (i.e., absence), a hydrogen atom and the like; R4 and R5 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; R6 is (cyclic group optionally having substituent(s))-carbonyl, and the like; R7, R8, R9 and R10 are the same or different and each is a hydrogen atom, halogen and the like; or R7 and R8, R8 and R9, and R9 and R10 may form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5; --- represents unsubstituted (i.e., absence) or a single bond; and represents a single bond or a double bond, or a salt thereof, and the like.

摘要翻译： 本发明旨在提供具有神经激肽2（NK2）受体拮抗作用的喹啉衍生物，其涉及式（I）表示的化合物，其中R 1为氢原子等; R 2是氢原子，任选具有取代基的烃基等; R 3是未取代的（即不存在），氢原子等; R 4和R 5相同或不同，各自为氢原子，任选具有取代基的烃基等; R 6是（任选具有取代基的环状基团） - 羰基等; R 7，R 8，R 9和R 10相同或不同，各自为氢原子 ，卤素等; 或R 7和R 8，R 8和R 9和R 9和/或 >和R 10可以与相邻的碳原子一起形成环; n为1〜5的整数， ---表示未取代（即不存在）或单键; “img id =”custom-character-00001“he =”2.79mm“wi =”4.57mm“file =”US20080039452A1-20080214-P00900.TIF“img-content =”character“img-format =”tif“/ >表示单键或双键，或其盐等。

公开(公告)号：US20060241051A1

公开(公告)日：2006-10-26

申请号：US10540494

申请日：2003-12-26

申请人： Chieko Kitada ,  Taiji Asami ,  Naoki Nishizawa ,  Tetsuya Ohtaki ,  Naoki Tarui ,  Hirokazu Matsumoto ,  Jiro Noguchi ,  Hisanori Matsui

发明人： Chieko Kitada ,  Taiji Asami ,  Naoki Nishizawa ,  Tetsuya Ohtaki ,  Naoki Tarui ,  Hirokazu Matsumoto ,  Jiro Noguchi ,  Hisanori Matsui

IPC分类号： A61K38/10 ,  C07K7/08

CPC分类号： C07K14/47 ,  A61K38/00

摘要： The present invention provides a metastin derivative in which the amino acids comprising metastin were modified by alternative chemical substituents resulting in metastin derivitives, having excellent blood stability and exhibiting cancer metastasis inhibiting action or cancer growth inhibiting action.

公开(公告)号：US07087597B1

公开(公告)日：2006-08-08

申请号：US10110381

申请日：2000-10-11

申请人： Tetsuo Miwa ,  Mitsuo Yamamoto ,  Takayuki Doi ,  Naoki Tarui

发明人： Tetsuo Miwa ,  Mitsuo Yamamoto ,  Takayuki Doi ,  Naoki Tarui

IPC分类号： C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  A61K31/506 ,  A61K31/5377

CPC分类号： C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D491/04

摘要： Compounds of the formula wherein R1, R2, R3, R4, X and Y are as defined, which have a superior cGMP specific phosphodiesterase (PDE) inhibitory activity, and can be used as an agent for the treatment of cardiovascular diseases such as angina pectoris, heart failure, cardiac infarction, hypertension, arteriosclerosis, and the like; allergic diseases such as asthma, or disorders of male or female genital function and the like.

摘要翻译： 下式的化合物其中R 1，R 2，R 3，R 4，X和Y分别为 定义为具有优异的cGMP特异性磷酸二酯酶（PDE）抑制活性，可用作治疗心绞痛，心力衰竭，心肌梗塞，高血压，动脉硬化等心血管疾病的药剂; 过敏性疾病如哮喘或男性或女性生殖器功能紊乱等。

公开(公告)号：US20060167052A1

公开(公告)日：2006-07-27

申请号：US10516252

申请日：2003-05-29

申请人： Yoshinori Ikeura ,  Tadatoshi Hashimoto ,  Naoki Tarui ,  Junya Shirai ,  Masayuki Yamashita

发明人： Yoshinori Ikeura ,  Tadatoshi Hashimoto ,  Naoki Tarui ,  Junya Shirai ,  Masayuki Yamashita

IPC分类号： A61K31/454 ,  C07D403/02

CPC分类号： C07D405/14 ,  C07D211/46 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/10 ,  C07D409/06 ,  C07D409/10 ,  C07D413/06 ,  C07D413/10 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14

摘要： The present invention provides a compound represented by the formula: wherein Ar is an aryl group, an aralkyl group or an aromatic heterocyclic group, each of which may be substituted, R1 is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group or an optionally substituted heterocyclic group, X is an oxygen atom or an optionally lo substituted imino group, Z is an optionally substituted methylene group, Ring A is an optionally further substituted piperidine ring, and Ring B is an optionally substituted aromatic ring, provided that when Z is a methylene group substituted with an oxo group, R1 is not a methyl group, and 15 when Z is a methylene group substituted with a methyl group, Ring B is a substituted aromatic ring, or a salt thereof, which is a novel piperidine derivative having excellent antagonistic action for a tachykinin receptor and useful as a medicament, particularly an agent for preventing and/or treating urinary frequency and/or urinary incontinence.

摘要翻译： 本发明提供由下式表示的化合物：其中Ar是芳基，芳烷基或芳族杂环基，其各自可以被取代，R 1是氢原子，任选地 取代烃基，酰基或任选取代的杂环基，X是氧原子或任选取代的亚氨基，Z是任选取代的亚甲基，环A是任选进一步取代的哌啶环，环B是 任选取代的芳环，条件是当Z是被氧代基取代的亚甲基时，R 1不是甲基，而当Z是被甲基取代的亚甲基时，R 1是环B 是取代的芳香环或其盐，其是对速激肽受体具有优异拮抗作用的新型哌啶衍生物，并且可用作药物，特别是用于预防和/或治疗尿频和/或 尿失禁

公开(公告)号：US20050228020A1

公开(公告)日：2005-10-13

申请号：US11142885

申请日：2005-06-01

申请人： Masaomi Miyamoto ,  Junji Matsui ,  Hiroaki Fukumoto ,  Naoki Tarui

发明人： Masaomi Miyamoto ,  Junji Matsui ,  Hiroaki Fukumoto ,  Naoki Tarui

IPC分类号： A61K31/135 ,  A61K31/14 ,  A61K31/165 ,  A61K31/40 ,  A61K31/4164 ,  A61K31/4453 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07C207/04 ,  C07C217/60 ,  C07C235/34 ,  C07D295/096 ,  C07D521/00 ,  A61K31/445

CPC分类号： C07D295/096 ,  A61K31/135 ,  A61K31/14 ,  A61K31/165 ,  A61K31/40 ,  A61K31/4164 ,  A61K31/4453 ,  C07C207/04 ,  C07C217/60 ,  C07C235/34 ,  C07C2602/10 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： An excellent β secretase inhibitor is provided, which comprises a compound of the general formula: wherein Ar is an aromatic group; X is a divalent group selected from —O—, —S—, —CO—, —SO—, —SO2—, —NR8—, CONR8—, —SO2NR8—, and —COO— (wherein R8 is hydrogen, etc.), a divalent C1-6 aliphatic hydrocarbon group which may contain one or two of these divalent groups, or a bond; Y is a divalent group selected from —O—, —S—, —CO—, —SO—, —SO2—, —NR8—, —CONR8—, —SO2NR8—, and —COO—, or a divalent C1-6 aliphatic hydrocarbon group which may contain one or two of these divalent groups; R1 and R2 are hydrogen, a hydrocarbon group, etc., respectively; and A is a ring which may be further substituted, or a salt thereof.

摘要翻译： 提供了优异的β分泌酶抑制剂，其包含通式如下的化合物：其中Ar为芳族基团; X是选自-O - ， - S - ， - CO - ， - SO - ， - SO 2 - ， - NR 8 - ，CONR - ， - SO 2 - ， - COO-（其中R 8为氢等） ，可以含有一个或两个这些二价基团的二价C 1-6脂族烃基或键; Y是选自-O - ， - S - ， - CO - ， - SO - ， - SO 2 - ， - NR 8 - ， - CONR 2 - SO 2 - ， - SO 2 - ， - COO-或二价C 1-6 - 脂族基 可以含有一个或两个这些二价基团的烃基; R 1和R 2分别为氢，烃基等; A是可以被进一步取代的环，或其盐。