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    NOVEL ACETYL-COA CARBOXYLASE (ACC) INHIBITORS AND THEIR USE IN DIABETES, OBESITY AND METABOLIC SYNDROME
    3.
    发明申请
    NOVEL ACETYL-COA CARBOXYLASE (ACC) INHIBITORS AND THEIR USE IN DIABETES, OBESITY AND METABOLIC SYNDROME 审中-公开
    新型乙酰胆碱酯酶（ACC）抑制剂及其在糖尿病，肥胖和代谢综合征中的应用

    公开(公告)号：WO2007095603A3

    公开(公告)日：2008-03-13

    申请号：PCT/US2007062181

    申请日：2007-02-15

    Applicant: ABBOTT LAB ,  GU YU GUI ,  XU XIANGDONG ,  WEITZBERG MOSHE ,  SHAM HING

    Inventor： GU YU GUI ,  XU XIANGDONG ,  WEITZBERG MOSHE ,  SHAM HING

    IPC: C07D277/34 ,  A61K31/426 ,  A61K31/427 ,  C07D417/04

    CPC classification number: C07D277/34 ,  C07D417/04

    Abstract: The present invention is directed to compounds of formula (I), or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or combination thereof, wherein Y is selected from the group consisting of-CR x R y -, -C(O)-, -O-, -N(H)-, -N(alkyl)- and -S-; wherein each of R x and R y is independently selected from the group consisting of hydrogen. alkyl, hydroxyalkyl, and haloalkyl; or R x and R y together with the carbon to which they are attached form a monocyclic cycloalkyl or heterocycle ring, Ar 1 is selected from the group consisting of phenyl and a monocyclic, five or six- membered heteroaryl, Ar 3 is phenyl or monocyclic heteroaryl, wherein Ar 3 is substituted with 1, 2, 3 or 4 substituents Ar 2 is a group of formula (a), (b), (c), (d), or (e); wherein R is hydrogen, cycloalkyj, alkyl or haloalkyl, Z 1 , Z 2 , Z 3 and Z 4 are C(R 101 ), or one or two of Z 1 , Z 2 , Z 3 and Z 4 is N and the others are C(R 101 ); Z 5 , Z 6 and Z 7 are C( 102 ). or one or two of Z 5 , Z 6 and Z 7 are N, and the others are C(R 102 ), Z is selected from the group consisting of -OR 5 , -alkylenyl-OR 5 , -N(R 6 )(R 7 ) and -alkylenyI-N(R 6 )(R 7 ), which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type II diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.

    Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，前药，前体药物或其组合的盐，其中Y选自-CR 1 x R -C（O） - ， - O - ， - N（H） - ， - N（烷基） - 和-S-; 其中R x和R y y各自独立地选自氢。 烷基，羟基烷基和卤代烷基; 或R x和R y与它们所连接的碳一起形成单环环烷基或杂环，Ar 1选自 由苯基和单环五元或六元杂芳基组成的基团是苯基或单环杂芳基，其中Ar 3 3被1,2,3或4个取代 取代基Ar 2是式（a），（b），（c），（d）或（e）的基团。 其中R是氢，环烷基，烷基或卤代烷基，Z 1，Z 2，Z 3和Z 4。 是C（R 101），或Z 1，Z 2，Z 3和Z 1中的一个或两个 4是N，其余是C（R 101）; Z 5，Z 6和Z 7是C（C 102）。 或Z 5，Z 6和Z 7中的一个或多个为N，其余为C（R 102） Z）选自-OR 5， - 亚烷基-OR 5，-N（R 6）（R 6） R 7）和 - 亚烷基-N（R 6 S）（R 7），其抑制乙酰辅酶A羧化酶（ACC）并且是有用的 用于预防或治疗人类的代谢综合征，II型糖尿病，肥胖症，动脉粥样硬化和心血管疾病。

    5,6,7-trisubstituted-4-amino-pyrido[2,3-d]pyrimidine compounds useful for inhibiting adenosine kinase
    7.
    发明专利
    5,6,7-trisubstituted-4-amino-pyrido[2,3-d]pyrimidine compounds useful for inhibiting adenosine kinase 未知

    公开(公告)号：NZ337125A

    公开(公告)日：2001-06-29

    申请号：NZ33712598

    申请日：1998-04-13

    Applicant: ABBOTT LAB

    Inventor： BHAGWAT SHRIPAD S ,  PERNER RICHARD J ,  GU YU GUI

    IPC: A61P25/04 ,  A61K31/519 ,  A61P1/00 ,  A61P3/10 ,  A61P9/00 ,  A61P25/08 ,  A61P25/18 ,  A61P25/22 ,  A61P29/00 ,  A61P31/00 ,  A61P37/06 ,  A61P43/00 ,  C07D471/04

    Abstract: A 5,6,7-trisubstituted-4-aminopyrido[2,3-d]pyrimidine derivative or a pharmaceutically acceptable salt or amide thereof has the formula (I) wherein: A) R1 and R2 are independently H, alkyl, arylalkyl or acyl or together with the nitrogen atom to which they are attached may form a 5 to 7 membered ring optionally containing 1-3 additional heteroatoms selected from N, O or S; R3 and R4 are independently alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, heteroaryl, or a heterocyclic group R5 is aryl, aralkyl, heteroaryl or a heterocyclic group and the dashed lines indicate a double bond is optionally present or B) R1 and R2 are independently H, alkyl, arylalkyl -C(O)-alkyl, -C(O)-aryl, -C(O)-heterocyclic or together with the nitrogen atom to which they are attached may form a 5 to 7 membered ring optionally containing 1-2 additional heteroatoms selected from N, O or S; R3 and R4 are independently alkyl, alkenyl, alkynyl, cycloalkyl, or optionally substituted heteroarylalkyl, aryl, arylalkyl, heteroarylalkenyl, arylalkenyl, arylalkynyl or heteroarylalkynyl and R5 is optionally substituted heteroarylalkyl, aryl, arylalkyl, heteroarylalkenyl, arylalkenyl, arylalkynyl or heteroarylalkynyl; with the proviso that the compound may not be: i) 4-amino-5-(4-chlorophenyl)-7-(4-nitrophenyl)pyrido[2,3-d]pyrimidine; ii) 4-amino-5-(4-methoxyphenyl)-7-(4-nitrophenyl)pyrido[2,3-d]pyrimidine; iii) 4-amino-5-(4-fluorophenyl)-7-(4-fluorophenyl)pyrido[2,3-d]pyrimidine; iv) 4-amino-5-(4-chlorophenyl)-7-(4-fluorophenyl)pyrido[2,3-d]pyrimidine; v) 4-amino-5-phenyl-7-(4-aminophenyl)pyrido[2,3-d]pyrimidine; vi) 4-amino-5-phenyl-7-(4-bromophenyl)pyrido[2,3-d]pyrimidine; vii) 4-amino-5-(4-methoxyphenyl)-7-(4-aminophenyl)pyrido[2,3-d]pyrimidine; viii) 4-amino-5-(4-methoxyphenyl)-7-(4-bromophenyl)pyrido[2,3-d]pyrimidine and ix) 4-amino-5,7-diphenylpyrido[2,3-d]pyrimidine. A pharmaceutical composition thereof is useful for inhibiting adenosine kinase, ischemia, neurological disorders, nociperception, inflammation, immunosuppression, gastrointestinal disjunctions, diabetes or sepsis.

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