公开(公告)号：US20070010528A1

公开(公告)日：2007-01-11

申请号：US10574048

申请日：2004-09-29

申请人： Keiji Kubo ,  Takanobu Kuroita ,  Masaki Kawamura ,  Hiroki Sakamoto

发明人： Keiji Kubo ,  Takanobu Kuroita ,  Masaki Kawamura ,  Hiroki Sakamoto

IPC分类号： A61K31/496 ,  A61K31/454 ,  A61K31/426 ,  C07D417/02

CPC分类号： C07D417/06 ,  C07D277/42 ,  C07D417/04 ,  C07D417/12

摘要： A thiazoline derivative represented by Formula (I): wherein R is a cyclic hydrocarbon group which may be substituted, or a heterocyclic group which may be substituted; X is a bond or a divalent chain hydrocarbon group which may be substituted; X′ is a bond or —N(R5)—; Y is a divalent hydrocarbon group which may be substituted; Y′ is a bond or —C(═O)—; ring A is a nitrogen-containing heterocycle which may be substituted; Z1 and Z3 are each independently a bond or a divalent chain hydrocarbon group which may be substituted; Z2 is a bond or —N(R6)—; and B is a group represented by the formula: which is useful as a therapeutic drug for thrombosis, is provided.

摘要翻译： 由式（I）表示的噻唑啉衍生物：其中R是可被取代的环状烃基或可被取代的杂环基; X是可以被取代的键或二价链烃基; X'是键或-N（R 5） - ; Y是可以被取代的二价烃基; Y'是键或-C（-O） - ; 环A是可以被取代的含氮杂环; Z 1和Z 3各自独立地为可以被取代的键或二价链烃基; Z 2是键或-N（R 6） - ; 并且B是由下式表示的基团：其可用作血栓形成的治疗药物。

公开(公告)号：US07534887B2

公开(公告)日：2009-05-19

申请号：US10574048

申请日：2004-09-29

申请人： Keiji Kubo ,  Takanobu Kuroita ,  Masaki Kawamura ,  Hiroki Sakamoto

发明人： Keiji Kubo ,  Takanobu Kuroita ,  Masaki Kawamura ,  Hiroki Sakamoto

IPC分类号： C07D413/00 ,  A61K31/497

CPC分类号： C07D417/06 ,  C07D277/42 ,  C07D417/04 ,  C07D417/12

摘要： A thiazoline derivative represented by Formula (I): wherein R is a cyclic hydrocarbon group which may be substituted, or a heterocyclic group which may be substituted; X is a bond or a divalent chain hydrocarbon group which may be substituted; X′ is a bond or —N(R5)—; Y is a divalent hydrocarbon group which may be substituted; Y′ is a bond or —C(═O)—; ring A is a nitrogen-containing heterocycle which may be substituted; Z1 and Z3 are each independently a bond or a divalent chain hydrocarbon group which may be substituted; Z2 is a bond or —N(R6)—; and B is a group represented by the formula: which is useful as a therapeutic drug for thrombosis, is provided.

摘要翻译： 由式（I）表示的噻唑啉衍生物：其中R是可被取代的环状烃基或可被取代的杂环基; X是可以被取代的键或二价链烃基; X'是键或-N（R 5） - ; Y是可以被取代的二价烃基; Y'是键或-C（-O） - ; 环A是可以被取代的含氮杂环; Z 1和Z 3各自独立地为可被取代的键或二价链烃基; Z2是键或-N（R6） - ; 并且B是由下式表示的基团：其可用作血栓形成的治疗药物。

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：US20060281795A1

公开(公告)日：2006-12-14

申请号：US11466633

申请日：2006-08-23

申请人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Mami Ojima

发明人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Mami Ojima

IPC分类号： A61K31/4245 ,  C07D413/02 ,  C07D413/14

CPC分类号： C07D413/14

摘要： The present invention relates to a compound represented by the formula (I) wherein R1 is a group represented by the formula wherein R2, R3, R4, R5, R6, R7 and R8 are each independently a hydrogen atom or a C1-6 alkyl, or a salt thereof. The compound of the present invention is useful as an agent for the prophylaxis or treatment of circulatory diseases such as hypertension and the like and metabolic diseases such as diabetes and the like.

摘要翻译： 本发明涉及由式（I）表示的化合物，其中R 1为由下式表示的基团：其中R 2，R 3， R 4，R 5，R 6，R 7和R 8，R 8， >各自独立地为氢原子或C 1-6烷基，或其盐。 本发明的化合物可用作预防或治疗诸如高血压等循环系统疾病和糖尿病等代谢疾病的药剂。

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：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：US20110112120A9

公开(公告)日：2011-05-12

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：US07875637B2

公开(公告)日：2011-01-25

申请号：US12458092

申请日：2009-06-30

申请人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Mami Ojima

发明人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Mami Ojima

IPC分类号： C07D271/07 ,  A61K31/4245

CPC分类号： C07D413/14

摘要： The present invention relates to a compound represented by the formula (I) wherein R1 is a group represented by the formula wherein R2, R3, R4, R5, R6, R7 and R8 are each independently a hydrogen atom or a C1-6 alkyl, or a salt thereof. The compound of the present invention is useful as an agent for the prophylaxis or treatment of circulatory diseases such as hypertension and the like and metabolic diseases such as diabetes and the like.

摘要翻译： 本发明涉及由式（I）表示的化合物，其中R 1是下式表示的基团其中R 2，R 3，R 4，R 5，R 6，R 7和R 8各自独立地为氢原子或C 1-6烷基， 或其盐。 本发明的化合物可用作预防或治疗诸如高血压等循环系统疾病和糖尿病等代谢疾病的药剂。

公开(公告)号：US20100137281A1

公开(公告)日：2010-06-03

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： A61K31/519 ,  C07D495/04 ,  A61K31/5377 ,  A61K31/551 ,  A61P9/00

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

摘要： The present invention aims to provide a compound having superior pharmacological action, physicochemical properties and the like, which is useful for the prophylaxis or treatment s of circulatory diseases such as hypertension, cardiac diseases, arteriosclerosis, renal diseases, cerebral apoplexy and the like and/or metabolic diseases such as hyperlipidemia, obesity, diabetes and the like, central nervous disorders such as cerebral infarction and the like, mental diseases such as dementia, depression and the like, and the like.A compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

摘要翻译： 本发明的目的在于提供具有优异的药理作用，理化特性等的化合物，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，脑中风等的循环系统疾病和/ 或代谢性疾病如高脂血症，肥胖症，糖尿病等，中枢神经障碍如脑梗塞等，精神疾病如痴呆，抑郁症等。 由式（I）表示的化合物或其盐，其中每个符号如说明书中所定义。