公开(公告)号：US08754226B2

公开(公告)日：2014-06-17

申请号：US13698257

申请日：2011-05-13

申请人： Thomas Daniel Aicher ,  Josef Roland Bencsik ,  Kevin Ronald Condroski ,  Jay Bradford Fell ,  John P. Fischer ,  Ronald Jay Hinklin ,  Scott Alan Pratt ,  Ajay Singh ,  Timothy M. Turner ,  David A. Mareska ,  Steven Armen Boyd

发明人： Thomas Daniel Aicher ,  Josef Roland Bencsik ,  Kevin Ronald Condroski ,  Jay Bradford Fell ,  John P. Fischer ,  Ronald Jay Hinklin ,  Scott Alan Pratt ,  Ajay Singh ,  Timothy M. Turner ,  David A. Mareska ,  Steven Armen Boyd

IPC分类号： A01N43/40 ,  A61K31/445 ,  A61K31/44 ,  C07D401/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D421/00

CPC分类号： C07D413/14 ,  C07D401/14 ,  C07D405/14

摘要： Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which X1, X2, L, R3, R4, R5, R6, R6a, R7, R9, R9a, and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.

摘要翻译： 其中X1，X2，L，R3，R4，R5，R6，R6a，R7，R9，R9a和n具有本说明书中给出的含义的式（I）化合物及其药学上可接受的盐是GPR119的调节剂 并且可用于治疗或预防诸如但不限于2型糖尿病，糖尿病并发症，糖尿病症状，代谢综合征，肥胖症，血脂异常和相关病症等疾病。

公开(公告)号：US20130158009A1

公开(公告)日：2013-06-20

申请号：US13698257

申请日：2011-05-13

申请人： Thomas Daniel Aicher ,  Josef Roland Bencsik ,  Kevin Ronald Condroski ,  Jay Bradford Fell ,  John P. Fischer ,  Ronald Jay Hinklin ,  Scott Alan Pratt ,  Ajay Singh ,  Timothy M. Turner ,  Steven Armen Boyd

发明人： Thomas Daniel Aicher ,  Josef Roland Bencsik ,  Kevin Ronald Condroski ,  Jay Bradford Fell ,  John P. Fischer ,  Ronald Jay Hinklin ,  Scott Alan Pratt ,  Ajay Singh ,  Timothy M. Turner ,  Steven Armen Boyd

IPC分类号： C07D413/14 ,  C07D405/14 ,  C07D401/14

CPC分类号： C07D413/14 ,  C07D401/14 ,  C07D405/14

摘要： Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which X1, X2, L, R3, R4, R5, R6, R6a, R7, R9, R9a, and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.

摘要翻译： 其中X1，X2，L，R3，R4，R5，R6，R6a，R7，R9，R9a和n具有本说明书中给出的含义的式（I）化合物及其药学上可接受的盐是GPR119的调节剂 并且可用于治疗或预防诸如但不限于2型糖尿病，糖尿病并发症，糖尿病症状，代谢综合征，肥胖症，血脂异常和相关病症等疾病。

公开(公告)号：US20130184257A1

公开(公告)日：2013-07-18

申请号：US13823041

申请日：2011-09-15

申请人： Thomas Daniel Aicher ,  Josef R. Bencsik ,  Steven Armen Boyd ,  Kevin Ronald Condroski ,  Jay Bradford Fell ,  John P. Fischer ,  Ronald Jay Hinklin ,  Scott Alan Pratt

发明人： Thomas Daniel Aicher ,  Josef R. Bencsik ,  Steven Armen Boyd ,  Kevin Ronald Condroski ,  Jay Bradford Fell ,  John P. Fischer ,  Ronald Jay Hinklin ,  Scott Alan Pratt

IPC分类号： C07D413/14 ,  C07D401/04 ,  C07D401/14 ,  C07D211/76

CPC分类号： C07D413/14 ,  A61K31/4468 ,  A61K31/454 ,  C07D211/76 ,  C07D401/04 ,  C07D401/14

摘要： Compounds of Formula (I) and pharmaceutically acceptable salts thereof in which X1, X2, L, R3, R4, R5, R7 and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.

摘要翻译： 其中X1，X2，L，R3，R4，R5，R7和n具有本说明书中给出的含义的式（I）化合物及其药学上可接受的盐是GPR119的调节剂，可用于治疗或预防疾病 例如但不限于2型糖尿病，糖尿病并发症，糖尿病症状，代谢综合征，肥胖症，血脂异常和相关病症。

公开(公告)号：US20090286791A1

公开(公告)日：2009-11-19

申请号：US12309493

申请日：2007-07-20

申请人： Shuji Kitamura ,  Thomas Daniel Aicher ,  Steve Gonzales ,  Yvan Le Huerou ,  Scott Alan Pratt ,  Tim Turner ,  Yoshihisa Nakada

发明人： Shuji Kitamura ,  Thomas Daniel Aicher ,  Steve Gonzales ,  Yvan Le Huerou ,  Scott Alan Pratt ,  Tim Turner ,  Yoshihisa Nakada

IPC分类号： A61K31/4155 ,  C07D401/12 ,  C07D403/12 ,  C07D413/14 ,  C07D231/14 ,  A61P3/04 ,  A61P3/10 ,  A61K31/4439 ,  A61K31/4184 ,  A61K31/498 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/506

CPC分类号： C07D401/12 ,  C07D207/08 ,  C07D213/81 ,  C07D233/90 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/06 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

摘要： The present invention provides compounds represented by the formula (Ia): the formula (Ib): the formula (Ic): and the formula (Id): wherein each symbol is as defined in the specification.According to the present invention, these compounds have a DGAT inhibitory activity and are useful for the prophylaxis, treatment or improvement of diseases or pathologies caused by high expression or high activation of DGAT.

摘要翻译： 本发明提供由式（Ia）表示的化合物：式（Ib）：式（Ic）：和式（Id）：其中每个符号如说明书中所定义。 根据本发明，这些化合物具有DGAT抑制活性，可用于预防，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：US20120065196A1

公开(公告)日：2012-03-15

申请号：US12309480

申请日：2007-07-20

申请人： Shuji Kitamura ,  Thomas Daniel Aicher ,  Steve Gonzales ,  Yvan Le Huerou ,  Scott Alan Pratt ,  Yoshihisa Nakada

发明人： Shuji Kitamura ,  Thomas Daniel Aicher ,  Steve Gonzales ,  Yvan Le Huerou ,  Scott Alan Pratt ,  Yoshihisa Nakada

IPC分类号： A61K31/541 ,  A61K31/454 ,  A61K31/445 ,  C07D401/12 ,  C07D413/12 ,  A61K31/4245 ,  C07D513/00 ,  A61K31/428 ,  A61K31/497 ,  C07D403/12 ,  A61K31/5377 ,  C07D417/12 ,  A61P3/04 ,  A61P3/10 ,  A61P3/06 ,  C07D401/06

CPC分类号： C07D401/12 ,  C07D231/14 ,  C07D231/56 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08

摘要： The present invention provides compounds represented by the formula (Ie): and the formula (If): wherein each symbol is as defined in the specification.According to the present invention, these compounds have a DGAT inhibitory activity and are useful for the prophylaxis, treatment or improvement of diseases or pathologies caused by high expression or high activation of DGAT.

摘要翻译： 本发明提供由式（Ie）表示的化合物：和式（If）：其中每个符号如说明书中所定义。 根据本发明，这些化合物具有DGAT抑制活性，可用于预防，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：US20100056515A1

公开(公告)日：2010-03-04

申请号：US12312087

申请日：2007-10-24

申请人： Kazuyoshi Aso ,  Michiyo Mochizuki ,  Takuto Kojima ,  Katsumi Kobayashi ,  Scott Alan Pratt ,  Albert Charles Gyorkos ,  Christopher Peter Corrette ,  Suk Young Cho

发明人： Kazuyoshi Aso ,  Michiyo Mochizuki ,  Takuto Kojima ,  Katsumi Kobayashi ,  Scott Alan Pratt ,  Albert Charles Gyorkos ,  Christopher Peter Corrette ,  Suk Young Cho

IPC分类号： A61K31/5377 ,  A61K31/4412 ,  A61K31/4166 ,  C07D413/10 ,  C07D401/12 ,  C07D235/26 ,  A61P25/24 ,  A61P25/22

CPC分类号： C07D235/26 ,  C07D235/30 ,  C07D401/12 ,  C07D403/12

摘要： There is provided a compound of the formula (I): wherein R1 is an optionally substituted C1-10 alkyl; R2 is H, or a C1-6 alkyl which may be substituted with 1 to 3 substituents; R3 is a 5- or 6-membered aromatic group which may be substituted with 1 to 5 substituents, wherein the 5- or 6-membered aromatic group may be fused with a 5- or 6-membered ring which may be substituted with 1 to 3 C1-6 alkyls; R4 is a hydrogen, a halogen, a hydroxy, a cyano, a C1-6 alkyl or a C1-6 alkoxy; Z is —O—, —S—, —SO—, —SO2—, or —NR5— wherein R5 is a hydrogen or a C1-6 alkyl; or a salt thereof or a prodrug thereof, which have CRF receptor antagonist activity and use thereof.

摘要翻译： 提供式（I）的化合物：其中R 1是任选取代的C 1-10烷基; R2是H或可被1至3个取代基取代的C 1-6烷基; R3是可被1至5个取代基取代的5或6元芳族基团，其中5或6元芳族基团可以与可被1至5个取代基取代的5或6元环稠合 3 C 1-6烷基; R4是氢，卤素，羟基，氰基，C1-6烷基或C1-6烷氧基; Z是-O - ， - S - ， - SO - ， - SO 2 - 或-NR 5 - ，其中R 5是氢或C 1-6烷基; 或其盐或其前药，其具有CRF受体拮抗剂活性及其用途。

公开(公告)号：US08163935B2

公开(公告)日：2012-04-24

申请号：US11919435

申请日：2006-04-26

申请人： Kazuyoshi Aso ,  Michiyo Mochizuki ,  Albert Charles Gyorkos ,  Christopher Peter Corrette ,  Suk Young Cho ,  Scott Alan Pratt ,  Christopher Stephen Siedem

发明人： Kazuyoshi Aso ,  Michiyo Mochizuki ,  Albert Charles Gyorkos ,  Christopher Peter Corrette ,  Suk Young Cho ,  Scott Alan Pratt ,  Christopher Stephen Siedem

IPC分类号： C07D403/02 ,  C07D235/24 ,  C07D235/26 ,  C07D235/30 ,  A61K31/415

CPC分类号： C07D403/04 ,  C07D235/26 ,  C07D235/30 ,  C07D335/02 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D413/04 ,  C07D417/10 ,  C07D471/04 ,  C07D471/06 ,  C07D495/04

摘要： There is provided a CRF receptor antagonist comprising a compound of the formula (I): wherein R1 is an optionally substituted hydrocarbyl, an optionally substituted C-linked heterocyclic group, an optionally substituted N-linked heteroaryl group, a cyano or an acyl; R2 is an optionally substituted cyclic hydrocarbyl or an optionally substituted heterocyclic group; X is oxygen, sulfur or —NR3— (wherein R3 is a hydrogen, an optionally substituted hydrocarbyl or an acyl); Y1, Y2 and Y3 are each an optionally substituted carbon or a nitrogen, provided that one or less of Y1, Y2 and Y3 is nitrogen; and Z is a bond, —CO—, oxygen, sulfur, —SO—, —SO2—, —NR4—, —NR4-alk-, —CONR4— or —NR4CO— (wherein alk is an optionally substituted C1-4 alkylene and R4 is a hydrogen, an optionally substituted hydrocarbyl or an acyl); or a salt thereof or a prodrug thereof.

摘要翻译： 提供了包含式（I）化合物的CRF受体拮抗剂：其中R1是任选取代的烃基，任选取代的C连接的杂环基，任选取代的N-连接的杂芳基，氰基或酰基; R2是任选取代的环状烃基或任选取代的杂环基; X是氧，硫或-NR 3 - （其中R 3是氢，任选取代的烃基或酰基）; Y1，Y2和Y3各自为任选取代的碳或氮，条件是Y 1，Y 2和Y 3中的一个或多个为氮; 并且Z是键，-CO-，氧，硫，-SO - ， - SO 2 - ， - NR 4 - ， - NR 4 - 烷 - ， - CONR 4 - 或-NR 4 CO-（其中，alk是任选取代的C 1-4亚烷基 和R4是氢，任选取代的烃基或酰基）; 或其盐或其前药。

公开(公告)号：US07514441B2

公开(公告)日：2009-04-07

申请号：US10525158

申请日：2003-08-21

申请人： Tsuneo Yasuma ,  Akira Mori ,  Masahiro Kawase ,  Hiroyuki Kimura ,  Masato Yoshida ,  Albert Charles Gyorkos ,  Scott Alan Pratt ,  Christopher Peter Corrette

发明人： Tsuneo Yasuma ,  Akira Mori ,  Masahiro Kawase ,  Hiroyuki Kimura ,  Masato Yoshida ,  Albert Charles Gyorkos ,  Scott Alan Pratt ,  Christopher Peter Corrette

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P19/08 ,  A61P19/10

CPC分类号： C07D487/04

摘要： There is provided a calcium receptor modulator comprising a compound of the formula (I): wherein ring A is an optionally substituted 5- to 7-membered ring; ring B is an optionally substituted 5- to 7-membered heterocyclic ring; X1 is CR1, CR1R2, N or NR13; X2 is N or NR3; Y is C, CR4 or N, Z is CR5, CR5R6, N or NR7; Ar is an optionally substituted cyclic group; R is H, an optionally substituted hydrocarbon group, etc.; and  is a single bond or a double bond; R1, R2, R3, R4, R5, R6, R7 and R13 are independently H, an optionally substituted hydrocarbon group; or a salt thereof or a prodrug thereof. Compounds of the formula (II) and (III): wherein ring A is an optionally substituted 5- to 7-membered ring; Q is C, CR5 or N; R8, R9, R10, R11 and R12 are independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided. Also specify X1, R3, R1, Y and X3 in formula (II) and (III) as before.

摘要翻译： 提供了包含式（I）化合物的钙受体调节剂：其中环A是任选取代的5-至7-元环; 环B是任选取代的5-至7-元杂环; X1是CR1，CR1R2，N或NR13; X2是N或NR3; Y为C，CR4或N，Z为CR5，CR5R6，N或NR7; Ar是任选取代的环状基团; R为H，任选取代的烃基等; “=”1.78mm“wi =”3.89mm“file =”US07514441-20090407-P00001.TIF“alt =”自定义字符“img-content =”character“img- format =“tif”/>是单键或双键; R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 13独立地为H，任选取代的烃基; 或其盐或其前药。 式（II）和（III）的化合物：其中环A是任选取代的5-至7-元环; Q为C，CR5或N; R8，R9，R10，R11和R12独立地为氢，任选取代的烃基等，或其盐。 也如前所述，在式（II）和（III）中指定X1，R3，R1，Y和X3。

公开(公告)号：US07714009B2

公开(公告)日：2010-05-11

申请号：US10577334

申请日：2004-10-27

申请人： Albert Charles Gyorkos ,  Christopher Peter Corrette ,  Suk Young Cho ,  Timothy Mark Turner ,  Scott Alan Pratt ,  Kazuyoshi Aso ,  Masakuni Kori ,  Michiyo Gyoten

发明人： Albert Charles Gyorkos ,  Christopher Peter Corrette ,  Suk Young Cho ,  Timothy Mark Turner ,  Scott Alan Pratt ,  Kazuyoshi Aso ,  Masakuni Kori ,  Michiyo Gyoten

IPC分类号： A61K31/4168 ,  C07D403/12 ,  C07D403/14 ,  C07D235/30

CPC分类号： C07D235/30 ,  C07D471/04

摘要： There is provided a CRF receptor antagonist comprising a compound of the formula (I): wherein, ring A is a 5-membered ring represented by the formula (A′): wherein X is a carbon and X1 is an oxygen, a sulfur or —NR5—, or formula (A″): wherein X is a nitrogen and R6 is an optionally substituted hydrocarbyl, R1 is an amino substituted by two optionally substituted hydrocarbyl groups, R2 is an phenyl, Y1 is CR3a or a nitrogen, Y2 is CR3b or a nitrogen and Y3 is CR3c or a nitrogen, provided that one or less of Y1, Y2, and Y3 is nitrogen, W is a bond, —(CH2)n-, and Z is a bond, —NR4—, etc.; or a salt thereof or a prodrug thereof.

摘要翻译： 提供了包含式（I）化合物的CRF受体拮抗剂：其中环A是由式（A'）表示的5元环：其中X是碳，X 1是氧，硫或 -NR5-或式（A“）：其中X是氮，R6是任选取代的烃基，R 1是被两个任选取代的烃基取代的氨基，R 2是苯基，Y 1是CR 3 a或氮，Y 2是 CR3b或氮，Y3为CR3c或氮，条件是Y1，Y2和Y3中的一个或多个为氮，W为键， - （CH2）n-，Z为键，-NR4-等 。 或其盐或其前药。

公开(公告)号：US20090215746A1

公开(公告)日：2009-08-27

申请号：US12263426

申请日：2008-10-31

申请人： Tsuneo Yasuma ,  Akira Mori ,  Masahiro Kawase ,  Hiroyuki Kimura ,  Masato Yoshida ,  Albert Charles Gyorkos ,  Scott Alan Pratt ,  Christopher Peter Corrette

发明人： Tsuneo Yasuma ,  Akira Mori ,  Masahiro Kawase ,  Hiroyuki Kimura ,  Masato Yoshida ,  Albert Charles Gyorkos ,  Scott Alan Pratt ,  Christopher Peter Corrette

IPC分类号： A61K31/519 ,  A61K31/55 ,  A61K31/541 ,  A61K31/5377 ,  C07D487/10 ,  C07D487/04 ,  A61P19/00

CPC分类号： C07D487/04

摘要： There is provided a calcium receptor modulator comprising a compound of the formula (I): wherein ring A is an optionally substituted 5- to 7-membered ring; ring B is an optionally substituted 5- to 7-membered heterocyclic ring; X1 is CR1, CR1R2, N or NR13; X2 is N or NR3; Y is C, CR4 or N, Z is CR5, CR5R6, N or NR7; Ar is an optionally substituted cyclic group; R is H, an optionally substituted hydrocarbon group, etc.; and is a single bond or a double bond; R1, R2, R3, R4, R5, R6, R7 and R13 are independently H, an optionally substituted hydrocarbon group; or a salt thereof or a prodrug thereof. Compounds of the formula (II) and (III): wherein ring A is an optionally substituted 5- to 7-membered ring; Q is C, CR5 or N; R8, R9, R10, R11 and R12 are independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided.Also specify X1, R3, R1, Y and X3 in formula (II) and (III) as before.

摘要翻译： 提供了包含式（I）化合物的钙受体调节剂：其中环A是任选取代的5至7元环; 环B是任选取代的5-至7-元杂环; X1是CR1，CR1R2，N或NR13; X2是N或NR3; Y为C，CR4或N，Z为CR5，CR5R6，N或NR7; Ar是任选取代的环状基团; R为H，任选取代的烃基等; ＆lt; img id =“CUSTOM-CHARACTER-00001”he =“3.13mm”wi =“8.47mm”file =“US20090215746A1-20090827-P00001.TIF”img-content =“character”img-format =“tif”/ >是单键或双键; R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 13独立地为H，任选取代的烃基; 或其盐或其前药。 式（II）和（III）的化合物：其中环A是任选取代的5-至7-元环; Q为C，CR5或N; R8，R9，R10，R11和R12独立地为氢，任选取代的烃基等，或其盐。 也如前所述，在式（II）和（III）中指定X1，R3，R1，Y和X3。