AR064702A1 - PROTEIN G HETEROCICLIC RECEPTORS AGONISTS, A PHARMACEUTICAL COMPOSITION THAT INCLUDES THEM AND THEIR USE IN THE TREATMENT OF DIABETES AND METABOLIC DISORDERS. - Google Patents

PROTEIN G HETEROCICLIC RECEPTORS AGONISTS, A PHARMACEUTICAL COMPOSITION THAT INCLUDES THEM AND THEIR USE IN THE TREATMENT OF DIABETES AND METABOLIC DISORDERS.

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Publication number
AR064702A1
AR064702A1 ARP070105977A AR064702A1 AR 064702 A1 AR064702 A1 AR 064702A1 AR P070105977 A ARP070105977 A AR P070105977A AR 064702 A1 AR064702 A1 AR 064702A1
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AR
Argentina
Prior art keywords
group
alkyl
haloalkyl
aryl
cycloalkyl
Prior art date
Application number
Other languages
Spanish (es)
Inventor
Zuchun Zhao
Xin Chen
John S Chen
Edward L Clemens
Jeffrey D Johnson
Jingyuan Ma
Alison Murphy
Imad Nashashibi
Christopher J Rabbat
Jiangao Song
Maria E Wilson
Yan Zhu
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Metabolex Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40261614&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR064702(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Metabolex Inc filed Critical Metabolex Inc
Publication of AR064702A1 publication Critical patent/AR064702A1/en

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Abstract

Se proveen compuestos y composiciones farmacéuticas para el tratamiento, inter alia, de diabetes de tipo II y otras enfermedades asociadas con un bajo control glucémico. Reivindicacion 1 Un compuesto que tiene la formula 1, en donde, X. Y y Z están seleccionados cada uno de modo independiente, del grupo que consiste en O, N, N(R3), S y C(R3) y al menos uno de X, Y y Z está seleccionado de O, N, N(R3) y S; el subíndice r es un numero entero de 0 a 3; el subíndice s es un numero entero de 0 a 3 y la suma de r + s es <= 4; el subíndice q es un numero entero de 0 a 4, A es C(R4) o N; L es -(CH2)n-, en donde n es un numero entero de 2 a 4 y al menos un CH2 está reemplazado por O, N(R5), S, S(O) o S(O)2 y todo CH2 restante está sustituido opcionalmente con uno o dos miembros seleccionados de halogeno, alquilo C1-4 y haloalquilo C1-4; Ar es un grupo arilo o heteroarilo de 5 a 10 miembros, opcionalmente sustituido con uno a cinco sustituyentes R6; R1 es un miembro seleccionado del grupo que consiste en alquilo C1-10, haloalquilo C1-10, cicloalquilo C3-7, alquenilo C2-10, alquinilo C2-10, -X1-CORa, -X1-CO2Ra, -X1-CONRaRb, -SO2Ra, un grupo heterociclo de 4 a 7 miembros, arilo y un grupo heteroarilo de 5 a 10 miembros, en donde cada uno de dicho grupo heterociclo y dicho grupo arilo y heteroarilo está opcionalmente sustituido con uno a cuatro sustituyentes seleccionados de modo independiente, de halo, alquilo C1-10, haloalquilo C1-10, cicloalquilo C3-7, alquenilo C2-10, alquinilo C2-10, arilo, heteroarilo, CN, NO2, -ORa, -NRaRb, -CO2Ra, -CONRaRb, -NRaCORb, -NRaCO2Rb, -S(O)mRa, -NRaS(O)2Rb y -SO2NRaRb; y X1 está seleccionado del grupo que consiste en un enlace, -C(O)- y -C(O)-(CH2)1-4-, en donde las porciones alifáticas de X1 están opcionalmente sustituidas con uno a tres miembros seleccionados de halogeno, alquilo C1-4 y haloalquilo C1-4, cada R2 es un miembro seleccionado, de modo independiente, del grupo que consiste en halo, alquilo C1-8, haloalquilo C1-8, cicloalquilo C3-7, -CORa, -CO2Ra, -CONRaRb, -ORa, -NRaRb, -NRaCORb, -SO2Ra y -SO2NRaRb; R3 es un miembro seleccionado del grupo que consiste en hidrogeno, halogeno, alquilo C1-4, haloalquilo C1-4, cicloalquilo C3-7, arilo y ORa; R4 es un miembro seleccionado del grupo que consiste en H, halo, alquilo C1-6, ORa y CN; R5 es un miembro seleccionado del grupo que consiste en -Ra, -CORa y -SO2Ra, cada R6 está seleccionado, de modo independiente, del grupo que consiste en halo, alquilo C1-10, haloalquilo C1-10, cicloalquilo C3-7, alquenilo C2-10, alquinilo C2-10, CN, NO2, -ORa, NRaRb, -CORa, -CO2Ra, -CONRaRb, -NRaCORb, -NRaCO2Rb, -S(O)mRa, -NRaS(O)mRb, -SO2NRaRb, un grupo heterociclo de 4 a 7 miembros, arilo y un grupo heteroarilo de 5 a 10 miembros, en donde cada uno de dichos grupos heterociclo, dichos grupos arilo y heteroarilo están opcionalmente sustituidas con uno a cuatro sustituyentes seleccionados, de modo independiente, del grupo que consiste en halo, oxo, alquilo C1-4, haloalquilo C1-4, cicloalquilo C3-7; CN, NO2, -ORa, NRaRb, -CO2Ra, -CONRaRb, -NRaCORb, -NRaCO2Rb, -S(O)mRa, -NRaSO2Rb y -SO2NRaRb, y en donde el subíndice m es un numero entero de 0 a 2; y cada Ra y Rb está seleccionado de modo independiente, del grupo que consiste en hidrogeno, alquilo C1-10, haloalquilo C1-10, cicloalquilo C3-10, heterociclilo, alquenilo C2-10, alquinilo C2-10, arilo, heteroarilo de 5 a 6 miembros y arilalquilo C1-4; y en donde las porciones alifáticas de cada uno de dichos Ra y Rb está opcionalmente sustituido con uno a tres miembros seleccionados del grupo que consiste en -ORn, -OC(O)N(Rn)2, -SRn, -S(O)Rn, -S(O)2Rn, -S(O)2N(Rn)2, -NRnS(O)2Rn, -C(O)N(Rn)2, -C(O)Rn, -NRnC(O)Rn, -NRnC(O)N(Rn)2, - CO2Rn, -NRnCO2Rn, -CN, -NO2, -N(Rn)2 y -NRnS(O)2N(Rn)2, en donde cada Rn es, de modo independiente, hidrogeno o un alquilo C1-6 no sustituido; y en donde las porciones de arilo y heteroarilo están opcionalmente sustituidas con uno a tres miembros seleccionados de halogeno, -ORm, -OC(O)N(Rm)2, -SRm, -S(O)Rm, -S(O)2Rm, -S(O)2N(Rm)2, -NRmS(O)2Rm, -C(O)N(Rm)2, -C(O)Rm, -NRmC(O)Rm, -NRmC(O)N(Rm)2, -CO2Rm, -NRmCO2Rm, -CN, -NO2, -N(Rm)2 y -NRmS(O)2N(Rm)2, en donde cada Rm es, de modo independiente, hidrogeno o un alquilo C1-6 no sustituido; y sus sales y ésteres farmacéuticamente aceptables; en donde el peso molecular de dicho compuesto es menor que 1200.Compounds and pharmaceutical compositions are provided for the treatment, inter alia, of type II diabetes and other diseases associated with low glycemic control. Claim 1 A compound having the formula 1, wherein X. Y and Z are each independently selected from the group consisting of O, N, N (R3), S and C (R3) and at least one of X, Y and Z is selected from O, N, N (R3) and S; the subscript r is an integer from 0 to 3; the subscript s is an integer from 0 to 3 and the sum of r + s is <= 4; the subscript q is an integer from 0 to 4, A is C (R4) or N; L is - (CH2) n-, where n is an integer from 2 to 4 and at least one CH2 is replaced by O, N (R5), S, S (O) or S (O) 2 and all CH2 remaining is optionally substituted with one or two members selected from halogen, C1-4 alkyl and C1-4 haloalkyl; Ar is a 5-10 membered aryl or heteroaryl group, optionally substituted with one to five R6 substituents; R1 is a member selected from the group consisting of C1-10 alkyl, C1-10 haloalkyl, C3-7 cycloalkyl, C2-10 alkenyl, C2-10 alkynyl, -X1-CORa, -X1-CO2Ra, -X1-CONRaRb, -SO2Ra, a 4-7 membered heterocycle group, aryl and a 5-10 membered heteroaryl group, wherein each of said heterocycle group and said aryl and heteroaryl group is optionally substituted with one to four independently selected substituents, halo, C1-10 alkyl, C1-10 haloalkyl, C3-7 cycloalkyl, C2-10 alkenyl, C2-10 alkynyl, aryl, heteroaryl, CN, NO2, -ORa, -NRaRb, -CO2Ra, -CONRaRb, -NRaCORb , -NRaCO2Rb, -S (O) mRa, -NRaS (O) 2Rb and -SO2NRaRb; and X1 is selected from the group consisting of a bond, -C (O) - and -C (O) - (CH2) 1-4-, wherein the aliphatic portions of X1 are optionally substituted with one to three members selected from halogen, C1-4 alkyl and C1-4 haloalkyl, each R2 is a member independently selected from the group consisting of halo, C1-8 alkyl, C1-8 haloalkyl, C3-7 cycloalkyl, -CORa, -CO2Ra , -CONRaRb, -ORa, -NRaRb, -NRaCORb, -SO2Ra and -SO2NRaRb; R3 is a member selected from the group consisting of hydrogen, halogen, C1-4 alkyl, C1-4 haloalkyl, C3-7 cycloalkyl, aryl and ORa; R4 is a member selected from the group consisting of H, halo, C1-6 alkyl, ORa and CN; R5 is a member selected from the group consisting of -Ra, -CORa and -SO2Ra, each R6 is independently selected from the group consisting of halo, C1-10 alkyl, C1-10 haloalkyl, C3-7 cycloalkyl, C2-10 alkenyl, C2-10 alkynyl, CN, NO2, -ORa, NRaRb, -CORa, -CO2Ra, -CONRaRb, -NRaCORb, -NRaCO2Rb, -S (O) mRa, -NRaS (O) mRb, -SO2NRaRb , a 4-7 membered heterocycle group, aryl and a 5-10 membered heteroaryl group, wherein each of said heterocycle groups, said aryl and heteroaryl groups are optionally substituted with one to four substituents independently selected from the group consisting of halo, oxo, C1-4 alkyl, C1-4 haloalkyl, C3-7 cycloalkyl; CN, NO2, -ORa, NRaRb, -CO2Ra, -CONRaRb, -NRaCORb, -NRaCO2Rb, -S (O) mRa, -NRaSO2Rb and -SO2NRaRb, and where the subscript m is an integer from 0 to 2; and each Ra and Rb is independently selected from the group consisting of hydrogen, C1-10 alkyl, C1-10 haloalkyl, C3-10 cycloalkyl, heterocyclyl, C2-10 alkenyl, C2-10 alkynyl, aryl, heteroaryl of 5 6 members and C1-4 arylalkyl; and wherein the aliphatic portions of each of said Ra and Rb is optionally substituted with one to three members selected from the group consisting of -ORn, -OC (O) N (Rn) 2, -SRn, -S (O) Rn, -S (O) 2Rn, -S (O) 2N (Rn) 2, -NRnS (O) 2Rn, -C (O) N (Rn) 2, -C (O) Rn, -NRnC (O) Rn, -NRnC (O) N (Rn) 2, - CO2Rn, -NRnCO2Rn, -CN, -NO2, -N (Rn) 2 and -NRnS (O) 2N (Rn) 2, where each Rn is, of independent mode, hydrogen or an unsubstituted C1-6 alkyl; and wherein the aryl and heteroaryl portions are optionally substituted with one to three members selected from halogen, -ORm, -OC (O) N (Rm) 2, -SRm, -S (O) Rm, -S (O) 2Rm, -S (O) 2N (Rm) 2, -NRmS (O) 2Rm, -C (O) N (Rm) 2, -C (O) Rm, -NRmC (O) Rm, -NRmC (O) N (Rm) 2, -CO2Rm, -NRmCO2Rm, -CN, -NO2, -N (Rm) 2 and -NRmS (O) 2N (Rm) 2, where each Rm is, independently, hydrogen or an alkyl C1-6 unsubstituted; and its pharmaceutically acceptable salts and esters; wherein the molecular weight of said compound is less than 1200.

ARP070105977 2006-12-28 2007-12-28 PROTEIN G HETEROCICLIC RECEPTORS AGONISTS, A PHARMACEUTICAL COMPOSITION THAT INCLUDES THEM AND THEIR USE IN THE TREATMENT OF DIABETES AND METABOLIC DISORDERS. AR064702A1 (en)

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US87790306P 2006-12-28 2006-12-28

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AR064702A1 true AR064702A1 (en) 2009-04-22

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ARP070105977 AR064702A1 (en) 2006-12-28 2007-12-28 PROTEIN G HETEROCICLIC RECEPTORS AGONISTS, A PHARMACEUTICAL COMPOSITION THAT INCLUDES THEM AND THEIR USE IN THE TREATMENT OF DIABETES AND METABOLIC DISORDERS.

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CN (1) CN101616586B (en)
AR (1) AR064702A1 (en)
CL (1) CL2007003841A1 (en)
TW (1) TWI414523B (en)
ZA (1) ZA200904281B (en)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7638541B2 (en) 2006-12-28 2009-12-29 Metabolex Inc. 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine
CA2719507C (en) * 2008-03-31 2018-03-27 Metabolex, Inc. Oxymethylene aryl compounds and uses thereof
JP5909185B2 (en) 2009-10-01 2016-04-26 シマベイ セラピューティクス， インコーポレーテッド Substituted tetrazol-1-ylphenoxymethylthiazol-2-ylpiperidinylpyrimidine salt
JP5960683B2 (en) * 2010-04-28 2016-08-02 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ Ketoheteroarylpiperidine and -piperazine derivatives as fungicides
JP5847813B2 (en) * 2010-06-23 2016-01-27 シマベイ セラピューティクス， インコーポレーテッド Composition of 5-ethyl-2- {4- [4- (4-tetrazol-1-yl-phenoxymethyl) -thiazol-2-yl] -piperidin-1-yl} -pyrimidine
CN103467398B (en) * 2013-09-03 2015-01-21 浙江医药高等专科学校 Triazole amide compounds, and preparation method and application thereof in resisting diabetes
KR20160100407A (en) * 2014-01-06 2016-08-23 리젠 파마슈티컬스 소시에떼 아노님 Novel inhibitors of glutaminase
CN109862896A (en) 2016-08-03 2019-06-07 西玛贝医药公司 For treating the Oxymethylene aryl compound of inflammatory gastrointestinal disease or gastrointestinal disorder
CN111072652B (en) * 2018-10-19 2023-05-23 暨南大学 Compounds for the treatment of diabetes and/or related disorders

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CN1829718A (en) * 2003-07-14 2006-09-06 艾尼纳制药公司 Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
WO2005061489A1 (en) * 2003-12-24 2005-07-07 Prosidion Limited Heterocyclic derivatives as gpcr receptor agonists

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CN101616586A (en) 2009-12-30
ZA200904281B (en) 2010-08-25
TWI414523B (en) 2013-11-11
TW200833688A (en) 2008-08-16
CN101616586B (en) 2014-08-13

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