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1. 发明申请

WO03047512A3 COMPOUNDS DERIVED FROM AN AMINE NUCLEUS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME 审中-公开
标题翻译：衍生自胺核的化合物和包含它们的药物组合物
公开(公告)号：WO03047512A3
公开(公告)日：2003-10-16
申请号：PCT/US0238038
申请日：2002-11-27
申请人： SQUIBB BRISTOL MYERS CO , LIU CHUNJIAN , DHAR MURALI T G , GU HENRY H , IWANOWICZ EDWIN J , LEFTHERIS KATERINA , PITTS WILLIAM J , HERPIN TIMOTHY F , PI ZULAN , BISACCHI GREGORY S
发明人： LIU CHUNJIAN , DHAR MURALI T G , GU HENRY H , IWANOWICZ EDWIN J , LEFTHERIS KATERINA , PITTS WILLIAM J , HERPIN TIMOTHY F , PI ZULAN , BISACCHI GREGORY S
IPC分类号： A61K45/06 , C07D263/32 , C07D263/48 , C07D413/12 , C07D413/14 , C07D417/12 , C07D521/00 , A61K31/33 , A61K31/41 , A61K31/42 , A61K31/425 , A61K31/505 , A61K31/53 , C07D239/00 , C07D239/02 , C07D251/00 , C07D253/00 , C07D271/00 , C07D413/00
CPC分类号： C07D413/12 , A61K45/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D263/32 , C07D263/48 , C07D413/14 , C07D417/12
摘要： Compounds having the formula (I), are effective as inhibitors of IMPDH enzyme and/or serine protease Factor VIIa, wherein B is a monocyclic or bicyclic carbocyclic or heterocyclic ring, D is a monocyclic or bicyclic carbocyclic or heterocyclic ring except when A is a heterocyclic ring, then D is a heterocyclic ring system, R is hydrogen or C1-4alkyl, and A, R1, R2 and R4 are as defined in the specification.
摘要翻译：具有式（I）的化合物作为IMPDH酶和/或丝氨酸蛋白酶因子VIIa的抑制剂是有效的，其中B是单环或双环碳环或杂环，D是单环或双环碳环或杂环，除了当A是杂环，则D为杂环系统，R为氢或C 1-4烷基，并且A，R 1，R 2和R 4如说明书中所定义。

2. 发明申请

WO2004004665A2 SUBSTITUTED HETEROCYCLIC DERIVATIVES USEFUL AS ANTIDIABETIC AND ANTIOBESITY AGENTS AND METHOD 审中-公开
标题翻译：用作抗糖尿病药和抗衰老药的取代的杂环衍生物和方法
公开(公告)号：WO2004004665A2
公开(公告)日：2004-01-15
申请号：PCT/US0322149
申请日：2003-07-02
申请人： SQUIBB BRISTOL MYERS CO , CHENG PETER T W , CHEN SEAN , DEVASTHALE PRATIK , DING CHARLES Z , HERPIN TIMOTHY F , WU SHUNG , ZHANG HAO , WANG WEI , YE XIANG-YANG
发明人： CHENG PETER T W , CHEN SEAN , DEVASTHALE PRATIK , DING CHARLES Z , HERPIN TIMOTHY F , WU SHUNG , ZHANG HAO , WANG WEI , YE XIANG-YANG
IPC分类号： A61K31/155 , A61K31/216 , A61K31/22 , A61K31/365 , A61K31/366 , A61K31/397 , A61K31/401 , A61K31/422 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/506 , A61K31/517 , A61K31/616 , A61K31/64 , A61K38/28 , A61K45/00 , A61P1/04 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P7/02 , A61P9/10 , A61P17/06 , A61P19/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07D403/06 , C07D403/08 , C07D403/10 , C07D403/14 , C07D413/12 , C07D413/14 , A61K
CPC分类号： C07D413/12 , C07D413/14
摘要： Formula, wherein Z is (CH2)q or C=O; Z is (CH2)p or C=O; D is -CH= or C=O or (CH2)m where m is 0, 1, 2 or 3; n = 0, 1 or 2; p = 1 or 2; q = 0, 1 or 2; Q is C or N; A is (CH2)x where x is 1 to 5, or A is (CH2)x , where x is 1 to 5 with an alkenyl bond or an alkynyl bond embedded anywhere in the chain, or A is -(CH2)x -O-(CH2)x - where x is 0 to 5 and x is 0 to 5, provided that at least one of x and x is other than 0; B is a bond or is (CH2)x where x is 1 to 5; X is CH or N; X2 is C, N, O or S; X3 is C, N, O or S; X4 is C, N, O or S; X5 is C, N, O or S; X6 is C, N, O or S; provided that at least one of X2, X3, X4 X5 and X6 is N; and at least one of X2, X3, X4 X5 and X6 is C. R is H or alkyl; R is H, alkyl, alkoxy, halogen, amino, substituted amino or cyano; R , R and R may be the same or different and are selected from H, alkyl, alkoxy, halogen, amino, substituted amino or cyano; and R , E, Z and Y are as defined herein.
摘要翻译：式，其中Z 1是（CH 2）q或C = O; Z 2是（CH 2）p或C = O; D是-CH =或C = O或（CH 2）m，其中m是0,1,2或3; n = 0,1或2; p = 1或2; q = 0,1或2; Q是C或N; A是（CH 2）x，其中x是1至5，或A是（CH 2）x 1，其中x 1是1至5且链中任何位置嵌入烯基键或炔基键，或A是 - （CH 2）x 2 -O-（CH 2）x 3 - 其中x 2为0至5且x 3为0至5，条件是x 2和x中的至少一个 <3>不是0; B是键或是（CH 2）x 4，其中x 4是1至5; X是CH或N; X2是C，N，O或S; X3是C，N，O或S; X4是C，N，O或S; X5是C，N，O或S; X6是C，N，O或S; 条件是X2，X3，X4，X5和X6中的至少一个是N; 并且X 2，X 3，X 4，X 5和X 6中的至少一个是C.R 1是H或烷基; R 2是H，烷基，烷氧基，卤素，氨基，取代的氨基或氰基; R 2a，R 2b和R 2c可以相同或不同，并且选自H，烷基，烷氧基，卤素，氨基，取代的氨基或氰基; 并且R 3，E，Z和Y如本文所定义。

3. 发明申请

WO2004004655A2 SUBSTITUTED HETEROCYCLIC DERIVATIVES USEFUL AS ANTIDIABETIC AND ANTIOBESITY AGENTS AND METHOD 审中-公开
标题翻译：作为抗真菌剂和抗菌剂和方法有用的取代的杂环衍生物
公开(公告)号：WO2004004655A2
公开(公告)日：2004-01-15
申请号：PCT/US0321331
申请日：2003-07-08
申请人： SQUIBB BRISTOL MYERS CO , CHENG PETER T W , CHEN SEAN , DING CHARLES Z , HERPIN TIMOTHY F
发明人： CHENG PETER T W , CHEN SEAN , DING CHARLES Z , HERPIN TIMOTHY F
IPC分类号： A61K31/41 , A61K31/42 , A61K31/435 , A61K31/50 , A61K31/52 , C07D233/54 , C07D249/06 , C07D263/32 , C07D271/06 , C07D413/12 , A61K
CPC分类号： C07D233/64 , C07D249/06 , C07D263/32 , C07D271/06 , C07D413/12
摘要： Compounds are provided which are useful as antidiabetic agents and antiobesity agents and have the structure (I) wherein m is 0, 1 or 2; n is 0, 1 or 2; Q is C or N; A is (CH2)x where x is 1 to 5, or A is (CH2)x1 where x is 1 to 5 with an alkenyl bond or an alkynyl bond embedded anywhere in the chain, or A is -(CH2)x -O-(CH2)x - where x is 0 to 5 and x is 0 to 5, provided that at least one of x and x is other than 0; B is a bond or is (CH2)x where x is 1 to 5; X is CH or N; X2 is C, N, O or S; X3 is C, N, O or S; X4 is C, N, O or S; X5 is C, N, O or S; X6 is C, N, O or S; provided that at least one of X2, X3, X4 X5 and X6 is N; and at least one of X2, X3, X4, X5 and X6 is C, and specifically excluding the structure (II) where X2 = N, X3 = C, X4 = O or S, Z = o or a bond; R is H or alkyl; R is H, alkyl, alkoxy, halogen, amino or substituted amino or cyano; R , R and R may be the same or different and are selected from H, alkyl, alkoxy, halogen, amino or substituted amino or cyano; and R and Y are as defined herein, which compounds are useful in treating diabetes and obesity.
摘要翻译：提供可用作抗糖尿病药和抗肥胖剂的化合物，并具有其中m为0,1或2的结构（I）; n为0,1或2; Q是C或N; A是（CH 2）x，其中x是1至5，或A是（CH 2）x1，其中x 1是1至5，链烯基或炔基键嵌入链中的任何位置，或A是 - （CH 2） x 2 -O-（CH 2）x 3 - 其中x 2为0至5且x 3为0至5，条件是x 2和x 3中的至少一个为 0以外; B是键或是（CH 2）x 4，其中x 4是1至5; X是CH或N; X2是C，N，O或S; X3为C，N，O或S; X4为C，N，O或S; X5为C，N，O或S; X6为C，N，O或S; 条件是X 2，X 3，X 4 X 5和X 6中的至少一个为N; X2，X3，X4，X5和X6中的至少一个为C，并且具体排除其中X2 = N，X3 = C，X4 = O或S，Z = o或键的结构（II） R 1是H或烷基; R 2是H，烷基，烷氧基，卤素，氨基或取代的氨基或氰基; R 2a，R 2b和R 2c可以相同或不同，并且选自H，烷基，烷氧基，卤素，氨基或取代的氨基或氰基; R 3和Y如本文所定义，该化合物可用于治疗糖尿病和肥胖症。

4. 发明公开

EP1656368A4 SUBSTITUTED HERTOCYCLIC DERIVATIVES USEFUL AS ANTIDIABETIC AND ANTIOBESITY AGENTS AND METHOD 审中-公开
标题翻译： AS抗糖尿病和手段对抗肥胖合适的取代的杂环衍生物方法
公开(公告)号：EP1656368A4
公开(公告)日：2009-08-26
申请号：EP03763485
申请日：2003-07-02
申请人： SQUIBB BRISTOL MYERS CO
发明人： CHENG PETER T W , CHEN SEAN , DEVASTHALE PRATIK , DING CHARLES Z , HERPIN TIMOTHY F , WU SHUNG , ZHANG HAO , WANG WEI , YE XIANG-YANG
IPC分类号： C07D403/06 , A61K31/155 , A61K31/216 , A61K31/22 , A61K31/365 , A61K31/366 , A61K31/397 , A61K31/401 , A61K31/422 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/506 , A61K31/517 , A61K31/616 , A61K31/64 , A61K38/28 , A61K45/00 , A61P1/04 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P7/02 , A61P9/10 , A61P17/06 , A61P19/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07D403/08 , C07D403/10 , C07D403/14 , C07D413/12 , C07D413/14
CPC分类号： C07D413/12 , C07D413/14

6. 发明公开

EP1531810A4 SUBSTITUTED HETEROCYCLIC DERIVATIVES USEFUL AS ANTIDIABETIC AND ANTIOBESITY AGENTS AND METHOD 有权
标题翻译：取代的杂环衍生物作为预防糖尿病剂和肥胖程序
公开(公告)号：EP1531810A4
公开(公告)日：2008-05-28
申请号：EP03763345
申请日：2003-07-08
申请人： SQUIBB BRISTOL MYERS CO
发明人： CHENG PETER T W , CHEN SEAN , DING CHARLES Z , HERPIN TIMOTHY F
IPC分类号： A61K31/41 , A61K31/42 , A61K31/435 , A61K31/50 , A61K31/52 , C07D233/54 , C07D249/06 , C07D263/32 , C07D271/06 , C07D413/12
CPC分类号： C07D233/64 , C07D249/06 , C07D263/32 , C07D271/06 , C07D413/12

7. 发明专利

PE20050767A1 AMINO-BENZAZOLES COMO INHIBIDORES DEL RECEPTOR P2Y1 未知
公开(公告)号：PE20050767A1
公开(公告)日：2005-10-06
申请号：PE2005000085
申请日：2005-01-21
申请人： SQUIBB BRISTOL MYERS CO
发明人： HERPIN TIMOTHY F , MORTON GEORGE C , REHFUSS ROBERT P , LAWRENCE R MICHAEL , POSS MICHAEL A , ROBERGE JACQUES Y , GUNGOR TIMUR
IPC分类号： A61K31/4178 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4439 , C07D235/30 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/02 , C07D413/12 , C07D413/14 , C07D417/02 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/04 , C07D513/04
摘要： SE REFIERE A AMINO-BENZAZOLES DE FORMULA I DONDE EL ANILLO A ES EL GRUPO a, X1 ES NR11, O, S(O)p, X2 ES CR11a, N; X3 ES CR11a, N; X4 ES CR11b, N; X5 ES CR11b, N; EL ANILLO E ES FENILO, PIRIDINILO, PIRIMIDILO, PIRAZINILO, PIRIDAZINILO SUBSTITUIDOS CON 1-4 R1; EL ANILLO B ES FENILO SUBSTITUIDO CON 0-4 R7 O UN HETEROARILO DE 5 A 6 MIEMBROS QUE COMPRENDE: ATOMOS DE CARBONO Y 1-4 HETEROATOMOSO EN EL ANILLO SELECCIONADOS DE O, N, NR6, S(O)p Y EL HETEROARILO ESTA SUBSTITUIDO CON 0-4 R7; R1 ES F, Cl, Br, I, OCF3, CF3, -CF2F3, CH, NO2, ENTRE OTROS; Y ES NR12, O, S(O)p; R5 ES CARBOCICLO C3-C10 SUBSTITUIDO CON 0-3 Rb O UN HETEROCICLO DE 5 A 10 MIEMBROS QUE COMPRENDEN ATOMOS DE C Y 1-4 HETEROATOMOS SELECCIONADOS DE N, O, S(O)p; R6 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C2-C6, ENTRE OTROS; R7 ES H, F, Cl, Br, I,. OCF3, ORc, ENTRE OTROS. SON COMPUESTOS PREFERIDOS [2-(2-TERT-BUTIL-FENOXI)-PIRIDINIL-3-IL]-(6-METIL-1H-BENZOIMIDAZOL-2-IL)-AMINA, (6-TERT-BUTIL-1H-BENZOIMIDAZOL-2-IL)-[2-(2-TERT-BUTIL-FENOXI)-6-METOXI-PIRIDINIL-3-IL]-AMINA, (6-TERT-BUTIL-1H-BENZOIMIDAZOL-2-IL)-[2-(3-TRIFLUOROMETIL-FENOXI)-PIRIDINIL-3-IL]-AMINA, ENTRE OTROS. LOS COMPUESTOS MENCIONADOS SON INHIBIDORES DEL RECEPTOR P2Y1 UTILES EN EL TRATAMIENTO DE ENFERMEDADES INFLAMATORIAS, ALZHEIMER

8. 发明专利

PE07672005A1 AMINO-BENZAZOLES COMO INHIBIDORES DEL RECEPTOR P2Y1 未知
公开(公告)号：PE07672005A1
公开(公告)日：2005-10-06
申请号：PE0000852005
申请日：2005-01-21
申请人： SQUIBB BRISTOL MYERS CO
发明人： HERPIN TIMOTHY F , MORTON GEORGE C , REHFUSS ROBERT P , LAWRENCE R MICHAEL , POSS MICHAEL A , ROBERGE JACQUES Y , GUNGOR TIMUR
IPC分类号： A61K31/4178 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4439 , C07D235/30 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/02 , C07D413/12 , C07D413/14 , C07D417/02 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/04 , C07D513/04
CPC分类号： C07D401/12 , C07D235/30 , C07D401/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/04 , C07D513/04
摘要： SE REFIERE A AMINO-BENZAZOLES DE FORMULA I DONDE EL ANILLO A ES EL GRUPO a, X1 ES NR11, O, S(O)p, X2 ES CR11a, N; X3 ES CR11a, N; X4 ES CR11b, N; X5 ES CR11b, N; EL ANILLO E ES FENILO, PIRIDINILO, PIRIMIDILO, PIRAZINILO, PIRIDAZINILO SUBSTITUIDOS CON 1-4 R1; EL ANILLO B ES FENILO SUBSTITUIDO CON 0-4 R7 O UN HETEROARILO DE 5 A 6 MIEMBROS QUE COMPRENDE: ATOMOS DE CARBONO Y 1-4 HETEROATOMOSO EN EL ANILLO SELECCIONADOS DE O, N, NR6, S(O)p Y EL HETEROARILO ESTA SUBSTITUIDO CON 0-4 R7; R1 ES F, Cl, Br, I, OCF3, CF3, -CF2F3, CH, NO2, ENTRE OTROS; Y ES NR12, O, S(O)p; R5 ES CARBOCICLO C3-C10 SUBSTITUIDO CON 0-3 Rb O UN HETEROCICLO DE 5 A 10 MIEMBROS QUE COMPRENDEN ATOMOS DE C Y 1-4 HETEROATOMOS SELECCIONADOS DE N, O, S(O)p; R6 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C2-C6, ENTRE OTROS; R7 ES H, F, Cl, Br, I,. OCF3, ORc, ENTRE OTROS. SON COMPUESTOS PREFERIDOS [2-(2-TERT-BUTIL-FENOXI)-PIRIDINIL-3-IL]-(6-METIL-1H-BENZOIMIDAZOL-2-IL)-AMINA, (6-TERT-BUTIL-1H-BENZOIMIDAZOL-2-IL)-[2-(2-TERT-BUTIL-FENOXI)-6-METOXI-PIRIDINIL-3-IL]-AMINA, (6-TERT-BUTIL-1H-BENZOIMIDAZOL-2-IL)-[2-(3-TRIFLUOROMETIL-FENOXI)-PIRIDINIL-3-IL]-AMINA, ENTRE OTROS. LOS COMPUESTOS MENCIONADOS SON INHIBIDORES DEL RECEPTOR P2Y1 UTILES EN EL TRATAMIENTO DE ENFERMEDADES INFLAMATORIAS, ALZHEIMER

10. 发明专利

GEP20084475B SUBSTITUTED HETEROCYCLIC DERIVATIVES USEFUL AS ANTIDIABETIC AND ANTIOBESITY AGENTS AND METHOD FOR THEIR PRODUCTION 未知
公开(公告)号：GEP20084475B
公开(公告)日：2008-09-10
申请号：GEAU2003008617
申请日：2003-07-08
申请人： SQUIBB BRISTOL MYERS CO
发明人： CHENG PETER T W , CHEN SEAN , DING CHARLES Z , HERPIN TIMOTHY F
IPC分类号： A61K31/41 , A61K31/42 , A61K31/435 , A61K31/50 , A61K31/52 , C07D233/54 , C07D249/06 , C07D263/32 , C07D271/06 , C07D413/12
摘要： A compound of formula (1) (values R1, R2, R3, R2a, R2b, R2c, X, X2, X3, X4, X5, X6, Y, Q, A, m and n are defined in the descrip¬tion), a pharmaceutical composition comprising it and use thereof for treating diabetes and obesity.

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