公开(公告)号：JP2013245220A

公开(公告)日：2013-12-09

申请号：JP2013171956

申请日：2013-08-22

Applicant: Array Biopharma Inc ,  アレイ バイオファーマ、インコーポレイテッド

Inventor： AICHER THOMAS DANIEL ,  BOYD STEVEN ARMEN ,  CHICARELLI MARK JOSEPH ,  CONDROSKI KEVIN RONALD ,  HINKLIN RONALD JAY ,  SINGH AJAY

IPC: C07D417/12 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/519 ,  A61P3/10 ,  A61P5/50 ,  A61P43/00 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04 ,  C07D498/04

CPC classification number: C07D417/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

Abstract: PROBLEM TO BE SOLVED: To provide a novel compound serving as a glucokinase activator.SOLUTION: Compounds of formula I are useful in treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Methods of treating or preventing diseases and disorders, which are characterized by underactivation of glucokinase or can be treated by activating glucokinase, are also provided. One embodiment of this invention provides the compound of the formula (I), solvate compounds, metabolites, salts, and pharmaceutically acceptable prodrugs thereof.

Abstract translation: 要解决的问题：提供一种用作葡萄糖激酶活化剂的新型化合物。溶液：式I化合物可用于治疗和/或预防由葡萄糖激酶水平不足的疾病（如糖尿病）介导的疾病。 还提供了治疗或预防疾病和病症的方法，其特征在于葡萄糖激酶过度活化或可通过激活葡糖激酶进行治疗。 本发明的一个实施方案提供式（I）的化合物，其溶剂合物，代谢物，盐和药学上可接受的前药。

公开(公告)号：WO2009042435A8

公开(公告)日：2009-10-08

申请号：PCT/US2008076401

申请日：2008-09-15

Applicant: ARRAY BIOPHARMA INC ,  AICHER THOMAS DANIEL ,  BOYD STEVEN ARMEN ,  CHICARELLI MARK JOSEPH ,  CONDROSKI KEVIN RONALD ,  FELL JAY BRADFORD ,  FISCHER JOHN P ,  GUNAWARDANA INDRANI W ,  HINKLIN RONALD JAY ,  SINGH AJAY ,  TURNER TIMOTHY M ,  WALLACE ELI M

Inventor： AICHER THOMAS DANIEL ,  BOYD STEVEN ARMEN ,  CHICARELLI MARK JOSEPH ,  CONDROSKI KEVIN RONALD ,  FELL JAY BRADFORD ,  FISCHER JOHN P ,  GUNAWARDANA INDRANI W ,  HINKLIN RONALD JAY ,  SINGH AJAY ,  TURNER TIMOTHY M ,  WALLACE ELI M

IPC: C07D417/12 ,  A61K31/433 ,  A61P3/10 ,  C07D417/14

CPC classification number: C07D401/14 ,  C07D213/75 ,  C07D401/12 ,  C07D417/12 ,  C07D417/14

Abstract: Provided are compounds of Formula (I): wherein R2, R3, R13, L and D2 are as defined in the specification, which are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.

Abstract translation: 提供了式（I）的化合物：其中R 2，R 3，R 13，L和D 2如说明书中所定义，其可用于治疗和/或预防由葡萄糖激酶活性水平不足所介导的疾病或病症， 通过激活包括但不限于糖尿病，葡萄糖耐量降低，IFG（空腹葡萄糖受损）和IFG（空腹血糖受损）以及其他疾病和病症（例如本文讨论的那些）的葡萄糖激酶来治疗。

公开(公告)号：WO2007117381A9

公开(公告)日：2008-03-27

申请号：PCT/US2007007444

申请日：2007-03-23

Applicant: ARRAY BIOPHARMA INC ,  AICHER THOMAS DANIEL ,  BOYD STEVEN ARMEN ,  CHICARELLI MARK JOSEPH ,  CONDROSKI KEVIN RONALD ,  HINKLIN RONALD JAY ,  SINGH AJAY

Inventor： AICHER THOMAS DANIEL ,  BOYD STEVEN ARMEN ,  CHICARELLI MARK JOSEPH ,  CONDROSKI KEVIN RONALD ,  HINKLIN RONALD JAY ,  SINGH AJAY

IPC: C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

CPC classification number: C07D417/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

Abstract: Provided are compounds of formula I that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes meilitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.

Abstract translation: 提供可用于治疗和/或预防由葡萄糖激酶活性水平不足（例如糖尿病）引起的疾病的式I化合物。 还提供治疗或预防葡萄糖激酶活性降低或可通过激活葡萄糖激酶进行治疗的疾病和病症的方法。

公开(公告)号：WO2013086397A1

公开(公告)日：2013-06-13

申请号：PCT/US2012068547

申请日：2012-12-07

Applicant: ARRAY BIOPHARMA INC ,  AMGEN INC

Inventor： HOUZE JONATHAN B ,  DRANSFIELD PAUL ,  PATTAROPONG VATEE ,  DU XIAOHUI ,  FU ZICE ,  LAI SUJEN ,  PARK JAEHYEON ,  JIAO XIANYUN ,  KOHN TODD J ,  AICHER THOMAS DANIEL ,  BOYD STEVEN ARMEN ,  BENCSIK JOSEF ,  CONDROSKI KEVIN RONALD ,  HINKLIN RONALD JAY ,  KRASER CHRISTOPHER F ,  PRATT SCOTT ,  SINGH AJAY ,  WENGLOWSKY STEVEN MARK ,  BOYS MARK LAURENCE ,  CHICARELLI MARK JOSEPH ,  MOHR PETER J ,  CARDOZO MARIO G

IPC: C07C275/00

CPC classification number: C07D401/14 ,  C07D213/75 ,  C07D213/85 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D411/04 ,  C07D413/04 ,  C07D417/04 ,  C07D419/04 ,  C07D471/04 ,  C07D491/052 ,  C07D493/04 ,  C07D493/10 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention relates to compounds, to pharmaceutical compositions comprising the compounds, to a process for making the compounds and to the use of the compounds in therapy. More particularly, it relates to certain glucokinase activators of Formulas 1 and 1a, useful in the treatment of diseases and disorders that would benefit from activation of glucokinase.

Abstract translation: 本发明涉及化合物，包含该化合物的药物组合物，涉及制备化合物的方法和该化合物在治疗中的用途。 更具体地说，本发明涉及式1和1a的某些葡糖激酶活化剂，可用于治疗可受益于葡萄糖激酶活化的疾病和病症。

公开(公告)号：WO2008118718A3

公开(公告)日：2008-11-13

申请号：PCT/US2008057543

申请日：2008-03-19

Applicant: ARRAY BIOPHARMA INC ,  AICHER THOMAS DANIEL ,  BOYD STEVEN ARMEN ,  CHICARELLI MARK JOSEPH ,  CONDROSKI KEVIN RONALD ,  HINKLIN RONALD JAY ,  SINGH AJAY

Inventor： AICHER THOMAS DANIEL ,  BOYD STEVEN ARMEN ,  CHICARELLI MARK JOSEPH ,  CONDROSKI KEVIN RONALD ,  HINKLIN RONALD JAY ,  SINGH AJAY

IPC: C07D417/14 ,  A61K31/427 ,  A61K31/4427 ,  A61P3/10 ,  C07D471/04 ,  C07D495/04 ,  C07D498/04

CPC classification number: C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D498/04

Abstract: Provided are compounds of formula (I) that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.

Abstract translation: 提供式（I）化合物，其可用于治疗和/或预防由缺乏水平的葡糖激酶活性（例如糖尿病）介导的疾病。 还提供了治疗或预防以葡萄糖激酶不足活性为特征的疾病和病症的方法，或者可以通过激活葡糖激酶治疗。

公开(公告)号：WO2007117381A3

公开(公告)日：2008-02-14

申请号：PCT/US2007007444

申请日：2007-03-23

Applicant: ARRAY BIOPHARMA INC ,  AICHER THOMAS DANIEL ,  BOYD STEVEN ARMEN ,  CHICARELLI MARK JOSEPH ,  CONDROSKI KEVIN RONALD ,  HINKLIN RONALD JAY ,  SINGH AJAY

Inventor： AICHER THOMAS DANIEL ,  BOYD STEVEN ARMEN ,  CHICARELLI MARK JOSEPH ,  CONDROSKI KEVIN RONALD ,  HINKLIN RONALD JAY ,  SINGH AJAY

IPC: C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

CPC classification number: C07D417/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

Abstract: Provided are compounds of formula I that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes meilitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.

Abstract translation: 提供式I化合物，其可用于治疗和/或预防由缺乏葡萄糖激酶水平的活性介导的疾病，例如糖尿病。 还提供了治疗或预防以葡萄糖激酶不足活性为特征的疾病和病症的方法，或者可以通过激活葡糖激酶治疗。

公开(公告)号：BR112013006344A2

公开(公告)日：2016-06-21

申请号：BR112013006344

申请日：2011-09-15

Applicant: ARRAY BIOPHARMA INC

Inventor： SINGH AJAY ,  FELL JAY BRADFORD ,  FISCHER JOHN P ,  BENCSIK JOSEF R ,  CONDROSKI KEVIN RONALD ,  HINKLIN RONALD JAY ,  PRATT SCOTT ALAN ,  BOYD STEVEN ARMEN ,  AICHER THOMAS DANIEL ,  TURNER TIMOTHY M

IPC: C07D413/14 ,  A61K31/4468 ,  A61K31/454 ,  A61P3/04

Abstract: lactamas substituídas por piperdinila como moduladores de gpr119. a presente invenção refere-se a compostos de fórmula (i) e a sais farmaceuticamente aceitáveis dos mesmos, nos quais x^ 1^, x^ 2^, l, r^ 3^, r^ 4, r^ 5^, r^ 7^ e n têm os significados dados no relatório descritivo, que são moduladores de gpr119 e são úteis no tratamento ou na prevenção de doenças, tais como, mas não limitadas a, diabetes do tipo 2, complicações diabéticas, sintomas de diabetes, metabólica, obesidade, dislipidemia e condições relacionadas.

公开(公告)号：RS53981B1

公开(公告)日：2015-10-30

申请号：RSP20150314

申请日：2007-03-23

Applicant: ARRAY BIOPHARMA INC

Inventor： AICHER THOMAS DANIEL ,  BOYD STEVEN ARMEN ,  CHICARELLI MARK JOSEPH ,  CONDROSKI KEVIN RONALD ,  HINKLIN RONALD JAY ,  SINGH AJAY

IPC: C07D413/14 ,  A61K31/4427 ,  A61P3/10 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

Abstract: Provided are compounds of formula I that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.

公开(公告)号：PT2013204E

公开(公告)日：2015-06-09

申请号：PT07754021

申请日：2007-03-23

Applicant: ARRAY BIOPHARMA INC

Inventor： AICHER THOMAS DANIEL ,  BOYD STEVEN ARMEN ,  HINKLIN RONALD JAY ,  SINGH AJAY ,  CHICARELLI MARK JOSEPH ,  CONDROSKI KEVIN RONALD

IPC: C07D413/14 ,  A61K31/4427 ,  A61P3/10 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

公开(公告)号：CR20150131A

公开(公告)日：2015-04-30

申请号：CR20150131

申请日：2015-03-12

Applicant: ARRAY BIOPHARMA INC

Inventor： AICHER THOMAS DANIEL ,  BOYD STEVEN ARMEN ,  CHICARELLI MARK JOSEPH ,  CONDROSKI KEVIN RONALD ,  FELL JAY BRADFORD ,  FISCHER JOHN P ,  GUNAWARDANA INDRANI W ,  HINKLIN RONALD JAY ,  SINGH AJAY ,  TURNER TIMOTHY M ,  WALLACE ELI M

IPC: C07D417/12 ,  A61K31/433 ,  A61P3/10 ,  C07D417/14

Abstract: Se proporcionan compuestos de la Fórmula I, en donde R2, R3, R13, L y D2 son lo definido en la memoria descriptiva, que son útiles en el tratamiento y/o en la prevención de enfermedades o trastornos mediados por niveles deficientes de actividad de glucocinasa o que se pueden tratar activando glucocinasa que incluyen, en forma no taxativa, diabetes mellitus, deterioro de tolerancia de la glucosa, IFG (deterioro de glucosa en ayunas) e IFG (deterioro de glucemia en ayunas), así como otras enfermedades y trastornos tales como aquellos discutidos en la presente.