公开(公告)号：US08921380B2

公开(公告)日：2014-12-30

申请号：US13418811

申请日：2012-03-13

申请人： Koichi Tanimoto ,  Mariko Oi ,  Yasunori Tsuboi ,  Yasunori Moritani

发明人： Koichi Tanimoto ,  Mariko Oi ,  Yasunori Tsuboi ,  Yasunori Moritani

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/00 ,  C07D487/04

CPC分类号： C07D487/04

摘要： Pyrazolo[1,5-a]pyrimidine compound, having CB1 receptor-antagonizing activity, of formula [I]: wherein R1 and R2 are the same or different and each is an optionally substituted aryl group, etc., R0 is hydrogen, an alkyl group, etc., E is —C(═O)— or —SO2—, R is a group of formula [i], [ii] or [iii], etc: Ring A is a C3-8 cycloalkyl group optionally fused to a benzene ring or a benzene ring, Q is a single bond or a methylene group, Ring B is a 4- to 7-membered aliphatic heterocyclic group, said cyclic group binding via its ring-carbon atom to the adjacent nitrogen atom, X is sulfur atom, etc., R3 is an alkyl group optionally substituted by an alkylthio group, R4 is hydrogen atom, an alkyl group, etc., one of RA and RB is an alkyl group, etc., and the other is hydrogen, an alkyl group, etc., or a pharmaceutically acceptable salt thereof.

摘要翻译： 具有式[I]的CB 1受体拮抗活性的吡唑并[1,5-a]嘧啶化合物：其中R1和R2相同或不同，并且各自为任选取代的芳基等，R 0是氢， 烷基等，E是-C（= O） - 或-SO 2 - ，R是式[ⅰ]，[ⅱ]或[ⅲ]等基团：环A是任选的C 3-8环烷基 稠合到苯环或苯环，Q是单键或亚甲基，环B是4-至7-元脂族杂环基，所述环状基团通过其环碳原子与相邻氮原子结合， X是硫原子等，R 3是任选被烷硫基取代的烷基，R 4是氢原子，烷基等，RA和RB之一是烷基等，另一个是氢 ，烷基等，或其药学上可接受的盐。

公开(公告)号：US20120016119A1

公开(公告)日：2012-01-19

申请号：US13145627

申请日：2010-01-22

申请人： Yasunori Tsuboi ,  Kimihiro Shirai

发明人： Yasunori Tsuboi ,  Kimihiro Shirai

IPC分类号： C07D487/04

CPC分类号： A61K31/519 ,  C07D487/04

摘要： Disclosed is a novel pyrrolo[2,3-d]pyrimidine compound represented by formula [I] or a pharmacologically acceptable salt thereof, which has a GPR119 receptor agonistic activity and is useful for a pharmaceutical. In formula [I], E represents a group represented by formula: —NH—, or the like; ring A represents a 6-membered aromatic ring which may contain 1 to 2 nitrogen atoms as heteroatoms (the aromatic ring may be substituted by a halogen atom, a group represented by formula: —CONRaRb, or the like; Ra and Rb are the same or different and independently represent hydrogen, alkyl, hydroxyalkyl, or the like); R1 represents an acyl group or the like; and R2 represents a halogen atom or a cyano group.

摘要翻译： 公开了由式[I]表示的新颖的吡咯并[2,3-d]嘧啶化合物或其药理学上可接受的盐，其具有GPR119受体激动活性，可用于药物。 在式[I]中，E表示由式-NH-等表示的基团; 环A表示可以含有1〜2个氮原子作为杂原子的6元芳香环（芳香环可以被卤素原子取代，由式-CONRaRb表示的基团等），Ra和Rb相同 或不同且独立地表示氢，烷基，羟基烷基等）; R1表示酰基等; R 2表示卤素原子或氰基。

公开(公告)号：US20080081817A1

公开(公告)日：2008-04-03

申请号：US11632725

申请日：2005-07-22

申请人： Iwao Takamuro ,  Saburo Kawanami ,  Yasunori Tsuboi ,  Toshiyuki Himiyama ,  Yuko Hasegawa ,  Hideki Mochida ,  Kouji Nogi

发明人： Iwao Takamuro ,  Saburo Kawanami ,  Yasunori Tsuboi ,  Toshiyuki Himiyama ,  Yuko Hasegawa ,  Hideki Mochida ,  Kouji Nogi

IPC分类号： A61K31/497 ,  A61K31/519 ,  A61P43/00 ,  C07D401/00 ,  C07D487/00

CPC分类号： C07D471/04 ,  C07D487/04

摘要： A novel nitrogenous fused bicyclic compound represented by the following general formula [1] or a pharmacologically acceptable salt of the compound. They have excellent SK channel blocking activity and are useful as a medicine. [I] (In the formula, R0 represents hydrogen, halogeno, etc.; R1 represents a group represented by the formula (a) or (b); A represents a group represented by the formula (X) or (Y); D1, D2 and D3 each represents N or CH; R2 represents halogeno or optionally halogenated lower alkyl, etc.; R3 represents hydrogen or lower alkyl; and Q represents lower alkylene.)

摘要翻译： 由以下通式[1]表示的新型含氮稠合双环化合物或该化合物的药理学上可接受的盐。 它们具有优异的SK通道阻断活性，可用作药物。 [I]（式中，R 0表示氢，卤素等; R 1表示由式（a）或（b）表示的基团; A 表示由式（X）或（Y）表示的基团; D 1，D 2和D 3各自表示N或CH; R 2表示卤代或任选卤代的低级烷基等; R 3表示氢或低级烷基; Q表示低级亚烷基。）

公开(公告)号：US20050282808A1

公开(公告)日：2005-12-22

申请号：US10508512

申请日：2003-03-27

申请人： Takayuki Kawaguchi ,  Hidenori Akatsuka ,  Toru Iijima ,  Yasunori Tsuboi ,  Takashi Mitsui ,  Jun Murakami

发明人： Takayuki Kawaguchi ,  Hidenori Akatsuka ,  Toru Iijima ,  Yasunori Tsuboi ,  Takashi Mitsui ,  Jun Murakami

IPC分类号： A61P7/02 ,  C07D307/85 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  A61K31/551 ,  A61K31/343 ,  A61K31/443 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377

CPC分类号： C07D413/14 ,  C07D307/85 ,  C07D405/12 ,  C07D405/14 ,  C07D417/14

摘要： The present invention provides a benzofuran derivative of the formula [1]: wherein x is a group of the formula: —N═ or —CH═; Y is an optionally substituted amino group, an optionally substituted cycloalkyl group or an optionally substituted saturated heterocyclic group; A is a single bond, a carbon chain optionally having a double bond within or at the end(s) of the chain, or an oxygen atom; R1 is a hydrogen atom or a halogen atom; Ring B is an optionally substituted benzene ring; and R3 is a hydrogen atom, or a pharmaceutically acceptable salt thereof, which is useful as a medicament, especially as an activated blood coagulation factor X inhibitor.

摘要翻译： 本发明提供式[1]的苯并呋喃衍生物：其中x是下式的基团：-N-或-CH-; Y是任选取代的氨基，任选取代的环烷基或任选取代的饱和杂环基; A是单键，在链的末端或其末端具有双键的碳链或氧原子; R 1是氢原子或卤素原子; 环B是任选取代的苯环; R 3是氢原子或其药学上可接受的盐，其可用作药物，特别是作为活化凝血因子X抑制剂。

公开(公告)号：US08163759B2

公开(公告)日：2012-04-24

申请号：US12303177

申请日：2007-07-04

申请人： Koichi Tanimoto ,  Mariko Oi ,  Yasunori Tsuboi ,  Yasunori Moritani

发明人： Koichi Tanimoto ,  Mariko Oi ,  Yasunori Tsuboi ,  Yasunori Moritani

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/00

CPC分类号： C07D487/04

摘要： The present invention provides a pyrazolo[1,5-a]pyrimidine compound, having CB1 receptor-antagonizing activity, of the following formula [I]: in which R1 and R2 are the same or different and each an optionally substituted aryl group etc, R0 is hydrogen atom, an alkyl group etc, E is a group of the formula: —C(═O)— or —SO2—, R is a group of the following formula [i], [ii]or [iii] etc: Ring A is (a) a C3-8 cycloalkyl group optionally fused to a benzene ring or (b) a benzene ring, Q is a single bond or a methylene group, Ring B is a 4- to 7-membered aliphatic heterocyclic group, said cyclic group binding via its ring-carbon atom to the adjacent nitrogen atom, X is sulfur atom etc, R3 is an alkyl group optionally substituted by an alkylthio group, R4 is hydrogen atom, an alkyl group etc, one of RA and RB is an alkyl group etc, and the other is hydrogen atom, an alkyl group etc, or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明提供具有下式[I]的具有CB1受体拮抗活性的吡唑并[1,5-a]嘧啶化合物：其中R1和R2相同或不同，各自为任选取代的芳基等， R 0是氢原子，烷基等，E是下式的基团-C（= O） - 或-SO 2 - ，R是下式[i]，[ii]或[iii]等的基团 ：环A是（a）任选地与苯环稠合的C 3-8环烷基或（b）苯环，Q是单键或亚甲基，环B是4-至7-元脂族杂环基 所述环状基团通过其环碳原子与相邻的氮原子结合，X是硫原子等，R 3是任选被烷硫基取代的烷基，R 4是氢原子，烷基等，RA和RB之一 是烷基等，另一个是氢原子，烷基等，或其药学上可接受的盐。

公开(公告)号：US07531537B2

公开(公告)日：2009-05-12

申请号：US10508512

申请日：2003-03-27

申请人： Takayuki Kawaguchi ,  Hidenori Akatsuka ,  Toru Iijima ,  Yasunori Tsuboi ,  Takashi Mitsui ,  Jun Murakami

发明人： Takayuki Kawaguchi ,  Hidenori Akatsuka ,  Toru Iijima ,  Yasunori Tsuboi ,  Takashi Mitsui ,  Jun Murakami

IPC分类号： A61K31/5377 ,  A61K31/443 ,  C07D413/14 ,  C07D405/12

CPC分类号： C07D413/14 ,  C07D307/85 ,  C07D405/12 ,  C07D405/14 ,  C07D417/14

摘要： The present invention provides a benzofuran derivative of the formula [1]: wherein x is a group of the formula: —N═ or —CH═; Y is an optionally substituted amino group, an optionally substituted cycloalkyl group or an optionally substituted saturated heterocyclic group; A is a single bond, a carbon chain optionally having a double bond within or at the end(s) of the chain, or an oxygen atom; R1 is a hydrogen atom or a halogen atom; Ring B is an optionally substituted benzene ring; and R3 is a hydrogen atom, or a pharmaceutically acceptable salt thereof, which is useful as a medicament, especially as an activated blood coagulation factor X inhibitor.

摘要翻译： 本发明提供式[1]的苯并呋喃衍生物：其中x是下式的基团：-N-或-CH-; Y是任选取代的氨基，任选取代的环烷基或任选取代的饱和杂环基; A是单键，在链的末端或其末端具有双键的碳链或氧原子; R1是氢原子或卤素原子; 环B是任选取代的苯环; 并且R3是氢原子或其药学上可接受的盐，其可用作药物，特别是作为活化凝血因子X抑制剂。

公开(公告)号：US20070167440A1

公开(公告)日：2007-07-19

申请号：US11579950

申请日：2005-05-27

申请人： Yasunori Moritani ,  Shigeru Furukubu ,  Yasunori Tsuboi ,  Chieko Okagaki ,  Akira Oku ,  Naomitsu Hirano

发明人： Yasunori Moritani ,  Shigeru Furukubu ,  Yasunori Tsuboi ,  Chieko Okagaki ,  Akira Oku ,  Naomitsu Hirano

IPC分类号： A61K31/541 ,  A61K31/5377 ,  A61K31/5415 ,  A61K31/538

CPC分类号： C07D207/14 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D491/04

摘要： The present invention relates to a novel pyrrolidine compound, which has a potent antagonistic activity against central cannabinoid (CB1) receptor, having the formula [I]: wherein each of R1 and R2 is (A) optionally substituted aryl (or heteroaryl) group, or (B) both of the groups combine to form a group of the formula: one of R3 and R4 is hydrogen and another is hydrogen, hydroxyl, hydroxyalkyl, etc., or both of R3 and R4 combine to form oxo group, R5 is hydrogen or alkyl, Y is single bond, oxygen atom or a group of the formula: —N(R7)—, R6 is optionally substituted hydrocarbon group or optionally substituted cyclic group, R7 is alkyl or alkyloxycarbonylalkyl, provided that R6 is not 4-amino-5-chloro-2-methoxyphenyl group when Y is single bond and one of the R3 and R4 is hydrogen and another is hydroxymethyl, or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及一种新的吡咯烷化合物，其具有对中大麻素（CB1）受体的有效拮抗作用，具有式[I]：其中R 1和R 2各自为 /（A）任选取代的芳基（或杂芳基）基团，或（B）两个基团结合形成下式的基团：R 3和R 4中的一个 氢和氢是氢，羟基，羟基烷基等，或者R 3和R 4两者结合形成氧代基，R“ 5是氢或烷基，Y是单键，氧原子或下式基团-N（R 7） - ，R 6是任选的 取代的烃基或任选取代的环状基团，R 7是烷基或烷氧基羰基烷基，条件是R 6不是4-氨基-5-氯-2-甲氧基苯基，当Y 是单键，R 3和R 4之一是氢，另一个是羟甲基或药学上可接受的sa 其中。

公开(公告)号：US20120202992A1

公开(公告)日：2012-08-09

申请号：US13418811

申请日：2012-03-13

申请人： Koichi TANIMOTO ,  Mariko OI ,  Yasunori TSUBOI ,  Yasunori MORITANI

发明人： Koichi TANIMOTO ,  Mariko OI ,  Yasunori TSUBOI ,  Yasunori MORITANI

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： Pyrazolo[1,5-a]pyrimidine compound, having CB1 receptor-antagonizing activity, of formula [I]: wherein R1 and R2 are the same or different and each is an optionally substituted aryl group, etc., R0 is hydrogen, an alkyl group, etc., E is —C(═O)— or —SO2—, R is a group of formula [i], [ii] or [iii], etc: Ring A is a C3-8 cycloalkyl group optionally fused to a benzene ring or a benzene ring, Q is a single bond or a methylene group, Ring B is a 4- to 7-membered aliphatic heterocyclic group, said cyclic group binding via its ring-carbon atom to the adjacent nitrogen atom, X is sulfur atom, etc., R3 is an alkyl group optionally substituted by an alkylthio group, R4 is hydrogen atom, an alkyl group, etc., one of RA and RB is an alkyl group, etc., and the other is hydrogen, an alkyl group, etc., or a pharmaceutically acceptable salt thereof.

摘要翻译： 具有式[I]的CB 1受体拮抗活性的吡唑并[1,5-a]嘧啶化合物：其中R1和R2相同或不同，并且各自为任选取代的芳基等，R 0是氢， 烷基等，E是-C（= O） - 或-SO 2 - ，R是式[ⅰ]，[ⅱ]或[ⅲ]等基团：环A是任选的C 3-8环烷基 稠合到苯环或苯环，Q是单键或亚甲基，环B是4-至7-元脂族杂环基，所述环状基团通过其环碳原子与相邻氮原子结合， X是硫原子等，R 3是任选被烷硫基取代的烷基，R 4是氢原子，烷基等，RA和RB之一是烷基等，另一个是氢 ，烷基等，或其药学上可接受的盐。

公开(公告)号：US07384952B2

公开(公告)日：2008-06-10

申请号：US10542081

申请日：2004-01-23

申请人： Iwao Takamuro ,  Yasuo Sekine ,  Yasunori Tsuboi ,  Kouji Nogi ,  Hiroyuki Taniguchi

发明人： Iwao Takamuro ,  Yasuo Sekine ,  Yasunori Tsuboi ,  Kouji Nogi ,  Hiroyuki Taniguchi

IPC分类号： C07D487/04 ,  C07D519/00 ,  A61K31/519

CPC分类号： C07D487/04

摘要： The present invention provides a novel pyrazolopyrimidine compound of the formula [I]: wherein R′ is (A) a substituted aryl group, (B) an optionally substituted nitrogen-containing aliphatic heteromonocyclic group, (C) a substituted cyclo-lower alkyl group, (D) an optionally substituted amino group, or (E) a substituted heteroaryl group, R2 is (a) an optionally substituted heteroaryl group or (b) an optionally substituted aryl group, Y is a single bond, a lower alkylene group or a lower alkenylene group, Z is a group of the formula: —CO—, —CH2-, —SO2- or a group of the formula [II]: Q is a lower alkylene group, and q is an integer of 0 or 1 or a pharmaceutically acceptable sait thereof, which has a small conductance potassium channel (SK channel) blocking activity and is useful as a medicament and a process for preparing the same

摘要翻译： 本发明提供式[I]的新型吡唑并嘧啶化合物：其中R'为（A）取代芳基，（B）任选取代的含氮脂族杂单环基团，（C）取代的环低级烷基 ，（D）任选取代的氨基或（E）取代的杂芳基，R 2是（a）任选取代的杂芳基或（b）任选取代的芳基，Y是 单键，低级亚烷基或低级亚烯基，Z为下式基团：-CO - ， - CH 2 - ， - SO 2 - 或式[II]基团：Q为低级亚烷基， q是0或1的整数或其药学上可接受的sait，其具有小的电导钾通道（SK通道）阻断活性，并且可用作药物及其制备方法

公开(公告)号：US08034949B2

公开(公告)日：2011-10-11

申请号：US11579950

申请日：2005-05-27

申请人： Yasunori Moritani ,  Shigeru Furukubu ,  Yasunori Tsuboi ,  Chieko Okagaki ,  Akira Oku ,  Naomitsu Hirano

发明人： Yasunori Moritani ,  Shigeru Furukubu ,  Yasunori Tsuboi ,  Chieko Okagaki ,  Akira Oku ,  Naomitsu Hirano

IPC分类号： C07D213/72 ,  C07D207/00 ,  A61K31/44

CPC分类号： C07D207/14 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D491/04

摘要： The present invention relates to a novel pyrrolidine compound, which has a potent antagonistic activity against central cannabinoid (CB1) receptor, having the formula [I]: wherein each of R1 and R2 is (A) optionally substituted aryl (or heteroaryl) group, or (B) both of the groups combine to form a group of the formula: one of R3 and R4 is hydrogen and another is hydrogen, hydroxyl, hydroxyalkyl, etc., or both of R3 and R4 combine to form oxo group, R5 is hydrogen or alkyl, Y is single bond, oxygen atom or a group of the formula: —N(R7)—, R6 is optionally substituted hydrocarbon group or optionally substituted cyclic group, R7 is alkyl or alkyloxycarbonylalkyl, provided that R6 is not 4-amino-5-chloro-2-methoxyphenyl group when Y is single bond and one of the R3 and R4 is hydrogen and another is hydroxymethyl, or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及一种新的吡咯烷化合物，其具有对中大麻素（CB1）受体的有效拮抗活性，其具有式[I]：其中R1和R2各自为（A）任选取代的芳基（或杂芳基） 或（B）两个基团结合形成下式的基团：R 3和R 4中的一个是氢，另一个是氢，羟基，羟基烷基等，或者R 3和R 4都结合形成氧代基，R 5是 氢或烷基，Y是单键，氧原子或下式的基团-N（R7） - ，R6是任选取代的烃基或任选取代的环状基团，R 7是烷基或烷氧基羰基烷基，条件是R 6不是4- 氨基-5-氯-2-甲氧基苯基或其药学上可接受的盐，当Y为单键且R 3和R 4中的一个为氢时，另一个为羟甲基。