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    • 1. 发明申请
    • HETEROCYCLIC BORONIC ACID COMPOUNDS
    • 杂环硼酸化合物
    • US20100120661A1
    • 2010-05-13
    • US12692276
    • 2010-01-22
    • David A. CampbellDavid T. WinnJuan M. Betancort
    • David A. CampbellDavid T. WinnJuan M. Betancort
    • A61K38/28C07F5/02A61K31/69C12N9/99C07D205/02A61P3/10
    • C07F5/025
    • Dipeptidyl peptidase IV (DPP-IV)-inhibiting compounds are provided that have formula I: wherein n is 1 to 3; X is CH2; S; O; CF2 or C(CH2)2; Z is H; halogen; hydroxyl; (C1-6)alkoxy; (C1-12)alkyl; (C3-12)cycloalkyl; phenyl; or heteroaryl; where the phenyl and heteroaryl groups are optionally mono- or independently plurisubstituted with R7; optionally, X together with an adjacent ring carbon and Z form a fused cyclopropyl; and optionally, one of the bonds in the ring containing X is a double bond; and CriRii, R1, R1, R3, R4 and R5 are as described herein. Methods for preparing these compounds, and methods for treating diabetes, especially Type II diabetes, and other related diseases are described using the compounds of formula I in pharmaceutical compositions which contain these compounds. Pharmaceutical compositions which contain combinations of these compounds with other antidiabetic agents are also described herein.
    • 提供二肽基肽酶IV(DPP-IV)抑制化合物,其具有式I:其中n为1至3; X为CH 2; S; O; CF 2或C(CH 2)2; Z是H; 卤素; 羟; (C 1-6)烷氧基; (C 1-12)烷基; (C3-12)环烷基; 苯基; 或杂芳基; 其中苯基和杂芳基任选被R7单取代或独立地被二取代; 任选地,X与相邻的环碳一起形成稠合的环丙基; 并且任选地,含有X的环中的一个键是双键; CriRii,R1,R2,R3,R4和R5如本文所述。 使用含有这些化合物的药物组合物中的式I化合物来描述制备这些化合物的方法,以及治疗糖尿病,特别是II型糖尿病和其它相关疾病的方法。 含有这些化合物与其它抗糖尿病药物的组合的药物组合物也在本文中描述。
    • 3. 发明授权
    • Heterocyclic boronic acid compounds
    • 杂环硼酸化合物
    • US07674913B2
    • 2010-03-09
    • US10514575
    • 2004-11-12
    • David A. CampbellDavid T. WinnJuan M. Betancort
    • David A. CampbellDavid T. WinnJuan M. Betancort
    • A61K31/69C07D403/12C07F5/02
    • C07F5/025
    • Dipeptidyl peptidase IV (DPP-IV)-inhibiting compounds are provided that have formula I: wherein n is 1 to 3; X is CH2; S; O; CF2 or C(CH3)2; Z is H; halogen; hydroxyl; (C1-6)alkoxy; (C1-12)alkyl; (C3-12)cycloalkyl; phenyl; or heteroaryl; where the phenyl and heteroaryl groups are optionally mono- or independently plurisubstituted with R7; optionally, X together with an adjacent ring carbon and Z form a fused cyclopropyl; and optionally, one of the bonds in the ring containing X is a double bond; and CriRii, R1, R1, R3, R4 and R5 are as described herein. Methods for preparing these compounds, and methods for treating diabetes, especially Type II diabetes, and other related diseases are described using the compounds of formula I in pharmaceutical compositions which contain these compounds. Pharmaceutical compositions which contain combinations of these compounds with other antidiabetic agents are also described herein.
    • 提供二肽基肽酶IV(DPP-IV)抑制化合物,其具有式I:其中n为1至3; X为CH 2; S; O; CF 2或C(CH 3)2; Z是H; 卤素; 羟; (C 1-6)烷氧基; (C 1-12)烷基; (C3-12)环烷基; 苯基; 或杂芳基; 其中苯基和杂芳基任选被R7单取代或独立地被二取代; 任选地,X与相邻的环碳一起形成稠合的环丙基; 并且任选地,含有X的环中的一个键是双键; 和CriRii,R1,R1,R3,R4和R5如本文所述。 使用含有这些化合物的药物组合物中的式I化合物来描述制备这些化合物的方法,以及治疗糖尿病,特别是II型糖尿病和其它相关疾病的方法。 含有这些化合物与其它抗糖尿病药物的组合的药物组合物也在本文中描述。