公开(公告)号：US07803940B2

公开(公告)日：2010-09-28

申请号：US12114048

申请日：2008-05-02

申请人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa ,  Koji Fuji

发明人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa ,  Koji Fuji

IPC分类号： C07D401/00

CPC分类号： C07D413/10 ,  C07D413/14 ,  C07D417/14

摘要： A compound represented by the formula (I): wherein R1 is an oxo group, ═N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: R3 and R4 are each H, or C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 alkylamino, di(C1-C6)alkylamino or C1-C6 alkylthio, each of which is optionally substituted; and R5 is H, or C1-C6 alkyl, C2-C6 alkenyl, cyclic group, each of which is optionally substituted, —CO—R8 or —O—R8′, or a salt thereof. The compound of the present invention is useful as a drug for the prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases.

摘要翻译： 由式（I）表示的化合物：其中R 1是氧代基，或= N-R等; 由下式表示的基团是由下式表示的基团：R 2是由下式表示的基团：R 3和R 4各自为H或C 1 -C 6烷基，C 3 -C 6环烷基，C 1 -C 6烷氧基，C 1 -C 6 烷基氨基，二（C 1 -C 6）烷基氨基或C 1 -C 6烷硫基，其各自任选被取代; 和R 5为H或C 1 -C 6烷基，C 2 -C 6烯基，环状基团，各自为任选取代的-CO-R 8或-O-R 8'或其盐。 本发明的化合物可用作预防或治疗心血管疾病，代谢疾病和/或中枢神经系统疾病的药物。

公开(公告)号：US20100113780A1

公开(公告)日：2010-05-06

申请号：US12625619

申请日：2009-11-25

申请人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa ,  Koji Fuji

发明人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa ,  Koji Fuji

IPC分类号： C07D413/14

CPC分类号： C07D413/10 ,  C07D413/14 ,  C07D417/14

摘要： A compound represented by the formula (I): wherein R1 is an oxo group, ═N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: R3 and R4 are each H, or C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 alkylamino, di(C1-C6)alkylamino or C1-C6 alkylthio, each of which is optionally substituted; and R5 is H, or C1-C6 alkyl, C2-C6 alkenyl, cyclic group, each of which is optionally substituted, —CO—R8 or —O—R8′, or a salt thereof. The compound of the present invention is useful as a drug for the prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases.

公开(公告)号：US20090176812A1

公开(公告)日：2009-07-09

申请号：US12114048

申请日：2008-05-02

申请人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa ,  Koji Fuji

发明人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa ,  Koji Fuji

IPC分类号： A61K31/505 ,  C07D239/54 ,  C07D413/08 ,  A61P9/10

CPC分类号： C07D413/10 ,  C07D413/14 ,  C07D417/14

摘要： A compound represented by the formula (I): wherein R1 is an oxo group, ═N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: R3 and R4 are each H, or C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 alkylamino, di(C1-C6)alkylamino or C1-C6 alkylthio, each of which is optionally substituted; and R5 is H, or C1-C6 alkyl, C2-C6 alkenyl, cyclic group, each of which is optionally substituted, —CO—R8 or —O—R8′, or a salt thereof. The compound of the present invention is useful as a drug for the prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases.

摘要翻译： 由式（I）表示的化合物：其中R1是氧代基，-N-R等; 由下式表示的基团是由下式表示的基团：R 2是由下式表示的基团：R 3和R 4各自为H或C 1 -C 6烷基，C 3 -C 6环烷基，C 1 -C 6烷氧基，C 1 -C 6 烷基氨基，二（C 1 -C 6）烷基氨基或C 1 -C 6烷硫基，其各自任选被取代; 和R 5为H或C 1 -C 6烷基，C 2 -C 6烯基，环状基团，各自为任选取代的-CO-R 8或-O-R 8'或其盐。 本发明的化合物可用作预防或治疗心血管疾病，代谢疾病和/或中枢神经系统疾病的药物。

公开(公告)号：US08501750B2

公开(公告)日：2013-08-06

申请号：US12451602

申请日：2008-05-20

申请人： Takanobu Kuroita ,  Hideyuki Igawa ,  Hiroki Sakamoto ,  Kouhei Asano ,  Minoru Sasaki

发明人： Takanobu Kuroita ,  Hideyuki Igawa ,  Hiroki Sakamoto ,  Kouhei Asano ,  Minoru Sasaki

IPC分类号： C07D495/04 ,  A61K31/519 ,  C07D239/545 ,  C07D513/04 ,  C07D471/02 ,  C07D243/06 ,  C07D235/00 ,  A61K31/4365 ,  A61K31/5513 ,  A61K31/4188 ,  A61K31/506

CPC分类号： C07D413/10 ,  C07D495/04 ,  C07D495/14 ,  C07D513/04

摘要： Heterocyclic compounds, pharmaceutical agent and methods thereof, having superior pharmacological action and/or physicochemical properties, which are useful for the prophylaxis or treatment of circulatory diseases such as hypertension, cardiac diseases, arteriosclerosis, renal diseases and cerebral apoplexy and/or metabolic diseases such as hyperlipidemia, obesity and diabetes and/or central nervous disorders such as cerebral infarction, and/or mental diseases such as dementia depression and depression.

摘要翻译： 具有优异的药理作用和/或物理化学性质的杂环化合物，药物及其方法，其可用于预防或治疗诸如高血压，心脏病，动脉硬化，肾脏疾病和脑中风和/或代谢疾病之类的循环系统疾病 如高脂血症，肥胖症和糖尿病和/或中枢神经障碍如脑梗死和/或精神疾病如痴呆抑郁症和抑郁症。

公开(公告)号：US20130131050A1

公开(公告)日：2013-05-23

申请号：US13811755

申请日：2011-07-22

申请人： Nobuyuki Matsunaga ,  Hideo Suzuki ,  Kouhei Asano ,  Hidekazu Tokuhara ,  Takeshi Yamamoto ,  Rei Okamoto

发明人： Nobuyuki Matsunaga ,  Hideo Suzuki ,  Kouhei Asano ,  Hidekazu Tokuhara ,  Takeshi Yamamoto ,  Rei Okamoto

IPC分类号： C07D471/04 ,  A61K31/542 ,  C07D487/04 ,  C07D513/04 ,  A61K31/519 ,  A61K31/5383 ,  C07D495/04

CPC分类号： C07D471/04 ,  C07D475/02 ,  C07D487/04 ,  C07D513/04

摘要： The present invention provides a compound useful for the prophylaxis or treatment of eicosanoid-associated diseases such as atherosclerosis, atherothrombosis, diabetes, obesity, asthma, fever, pain, cancer, rheumatism, osteoarthritis, atopic dermatitis and the like, and having superior pharmacological action, physicochemical properties and the like.The present invention relates to a compound represented by the following formula: wherein each symbol is as defined in the specification, or a salt thereof.

摘要翻译： 本发明提供了可用于预防或治疗类二十烷酸相关疾病如动脉粥样硬化，动脉粥样硬化血栓形成，糖尿病，肥胖症，哮喘，发烧，疼痛，癌症，风湿病，骨关节炎，特应性皮炎等的化合物，并且具有优异的药理作用 ，物理化学性质等。 本发明涉及由下式表示的化合物：其中每个符号如说明书中所定义，或其盐。

公开(公告)号：US20090048258A1

公开(公告)日：2009-02-19

申请号：US11883357

申请日：2006-01-31

申请人： Masaki Ogino ,  Yoshihisa Nakada ,  Mitsuyuki Shimada ,  Kouhei Asano ,  Norikazu Tamura ,  Minori Masago

发明人： Masaki Ogino ,  Yoshihisa Nakada ,  Mitsuyuki Shimada ,  Kouhei Asano ,  Norikazu Tamura ,  Minori Masago

IPC分类号： A61K31/5375 ,  C07D277/46 ,  A61K31/426 ,  A61K31/167 ,  A61P3/10 ,  A61P3/04 ,  C07C233/11 ,  C07D265/30

CPC分类号： C07D277/46 ,  C07C235/78 ,  C07D207/34 ,  C07D213/75 ,  C07D215/38 ,  C07D231/14 ,  C07D231/38 ,  C07D239/42 ,  C07D295/12 ,  C07D333/36 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

摘要： The present invention relate to a compound represented by the formula (I) or (II) wherein ring A is an optionally substituted ring (the ring should not be pyrrolidine, piperidine and piperazine), ring B is an optionally substituted aromatic ring, ring D is an optionally substituted ring, R1 and R2 are each independently a hydrogen atom or a substituent, R3 is a hydrogen atom or a C1-6 alkyl group, or R3 is bonded to ring A to form a non-aromatic ring, ring Aa is an optionally substituted aromatic hydrocarbon, Y is CH or N, Ra1 is an optionally substituted hydrocarbon group, and Ra2 and Ra3 are each independently a hydrogen atom or a substituent, or a salt thereof. The present invention provides a compound having a DGAT inhibitory activity, which is useful for the treatment or amelioration of diseases or pathologies caused by high expression or high activation of DGAT.

摘要翻译： 本发明涉及由式（I）或（II）表示的化合物，其中环A为任选取代的环（该环不应为吡咯烷，哌啶和哌嗪），环B为任选取代的芳环，环D 是任选取代的环，R 1和R 2各自独立地为氢原子或取代基，R 3为氢原子或C 1-6烷基，或R 3与环A键合形成非芳香环，环A a为 任选取代的芳烃，Y是CH或N，Ra1是任选取代的烃基，Ra2和Ra3各自独立地是氢原子或取代基，或其盐。 本发明提供具有DGAT抑制活性的化合物，其可用于治疗或改善由高表达或高活化DGAT引起的疾病或病理。

公开(公告)号：US20080207654A1

公开(公告)日：2008-08-28

申请号：US11943910

申请日：2007-11-21

申请人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa

发明人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa

IPC分类号： A61K31/506 ,  C07D239/22 ,  A61P3/10 ,  A61P3/04

CPC分类号： C07D413/14 ,  C07D413/10 ,  C07D417/14

摘要： A compound represented by the formula (I): wherein R1 is an oxo group, ═N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: R3 and R4 are each H, or C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 alkylamino, di(C1-C6)alkylamino or C1-C6 alkylthio, each of which is optionally substituted; and R5 is H, or C1-C6 alkyl, C2-C6 alkenyl, cyclic group, each of which is optionally substituted, —CO—R8 or —O—R8′, or a salt thereof. The compound of the present invention is useful as a drug for the prophylaxis or treatment of circulatory diseases, metabolic diseases and/or central nervous system diseases.

摘要翻译： 由式（I）表示的化合物：其中R1是氧代基，-N-R等; 由下式表示的基团是由下式表示的基团：R 2是由下式表示的基团：R 3和R 4各自为H或C 1 -C 6烷基，C 3 -C 6环烷基，C 1 -C 6烷氧基，C 1 -C 6 烷基氨基，二（C 1 -C 6）烷基氨基或C 1 -C 6烷硫基，其各自任选被取代; 和R 5为H或C 1 -C 6烷基，C 2 -C 6烯基，环状基团，各自为任选取代的-CO-R 8或-O-R 8'或其盐。 本发明的化合物可用作预防或治疗循环系统疾病，代谢疾病和/或中枢神经系统疾病的药物。

公开(公告)号：US07998968B2

公开(公告)日：2011-08-16

申请号：US12625622

申请日：2009-11-25

申请人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa ,  Koji Fuji

发明人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa ,  Koji Fuji

IPC分类号： A61K31/505

CPC分类号： C07D413/10 ,  C07D413/14 ,  C07D417/14

摘要： A compound represented by the formula (I): wherein R1 is an oxo group, ═N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: R3 and R4 are each H, or C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 alkylamino, di(C1-C6)alkylamino or C1-C6 alkylthio, each of which is optionally substituted; and R5 is H, or C1-C6 alkyl, C2-C6 alkenyl, cyclic group, each of which is optionally substituted, —CO—R8 or —O—R8′, or a salt thereof. For example, the compound may be substituted pyrimidines and pharmaceutical compositions of the formula (I) where X=—CR3; X1=—CR2 or —NR2; and X2=—CR5 or —NR5. The compound of the present invention is useful as a drug for the prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases.

摘要翻译： 由式（I）表示的化合物：其中R 1是氧代基，或= N-R等; 由下式表示的基团是由下式表示的基团：R 2是由下式表示的基团：R 3和R 4各自为H或C 1 -C 6烷基，C 3 -C 6环烷基，C 1 -C 6烷氧基，C 1 -C 6 烷基氨基，二（C 1 -C 6）烷基氨基或C 1 -C 6烷硫基，其各自任选被取代; 和R 5为H或C 1 -C 6烷基，C 2 -C 6烯基，环状基团，各自为任选取代的-CO-R 8或-O-R 8'或其盐。 例如，化合物可以是取代的嘧啶和式（I）的药物组合物，其中X = -CR 3; X1 = -CR2或-NR2; X2 = -CR5或-NR5。 本发明的化合物可用作预防或治疗心血管疾病，代谢疾病和/或中枢神经系统疾病的药物。

公开(公告)号：US20100105709A1

公开(公告)日：2010-04-29

申请号：US12625622

申请日：2009-11-25

申请人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa ,  Koji Fuji

发明人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa ,  Koji Fuji

IPC分类号： A61K31/506 ,  C07D413/10 ,  C07D413/14 ,  A61P25/00 ,  A61P9/00 ,  A61P3/00

CPC分类号： C07D413/10 ,  C07D413/14 ,  C07D417/14

摘要： A compound represented by the formula (I): wherein R1 is an oxo group, ═N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: R3 and R4 are each H, or C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 alkylamino, di(C1-C6)alkylamino or C1-C6 alkylthio, each of which is optionally substituted; and R5 is H, or C1-C6 alkyl, C2-C6 alkenyl, cyclic group, each of which is optionally substituted, —CO—R8 or —O—R8′, or a salt thereof. The compound of the present invention is useful as a drug for the prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases.

摘要翻译： 由式（I）表示的化合物：其中R 1是氧代基，或= N-R等; 由下式表示的基团是由下式表示的基团：R 2是由下式表示的基团：R 3和R 4各自为H或C 1 -C 6烷基，C 3 -C 6环烷基，C 1 -C 6烷氧基，C 1 -C 6 烷基氨基，二（C 1 -C 6）烷基氨基或C 1 -C 6烷硫基，其各自任选被取代; 和R 5为H或C 1 -C 6烷基，C 2 -C 6烯基，环状基团，各自为任选取代的-CO-R 8或-O-R 8'或其盐。 本发明的化合物可用作预防或治疗心血管疾病，代谢疾病和/或中枢神经系统疾病的药物。

公开(公告)号：US09023858B2

公开(公告)日：2015-05-05

申请号：US13811755

申请日：2011-07-22

申请人： Nobuyuki Matsunaga ,  Hideo Suzuki ,  Kouhei Asano ,  Hidekazu Tokuhara ,  Takeshi Yamamoto ,  Rei Okamoto

发明人： Nobuyuki Matsunaga ,  Hideo Suzuki ,  Kouhei Asano ,  Hidekazu Tokuhara ,  Takeshi Yamamoto ,  Rei Okamoto

IPC分类号： A61K31/519 ,  C07D487/04 ,  C07D471/04 ,  C07D475/02 ,  C07D513/04

CPC分类号： C07D471/04 ,  C07D475/02 ,  C07D487/04 ,  C07D513/04

摘要： The present invention provides a compound useful for the prophylaxis or treatment of eicosanoid-associated diseases such as atherosclerosis, atherothrombosis, diabetes, obesity, asthma, fever, pain, cancer, rheumatism, osteoarthritis, atopic dermatitis and the like, and having superior pharmacological action, physicochemical properties and the like.The present invention relates to a compound represented by the following formula: wherein each symbol is as defined in the specification, or a salt thereof.

摘要翻译： 本发明提供了可用于预防或治疗类二十烷酸相关疾病如动脉粥样硬化，动脉粥样硬化血栓形成，糖尿病，肥胖症，哮喘，发烧，疼痛，癌症，风湿病，骨关节炎，特应性皮炎等的化合物，并且具有优异的药理作用 ，物理化学性质等。 本发明涉及由下式表示的化合物：其中每个符号如说明书中所定义，或其盐。