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    HETEROCYCLIC BORONIC ACID COMPOUNDS
    1.
    发明申请
    HETEROCYCLIC BORONIC ACID COMPOUNDS 审中-公开
    杂环硼酸化合物

    公开(公告)号：US20070185061A1

    公开(公告)日：2007-08-09

    申请号：US11556944

    申请日：2006-11-06

    申请人： David Campbell ,  David Winn ,  Juan Betancort ,  Kevin Shreder ,  Yi Hu ,  Bei Li ,  Melissa Wong ,  Lifu Ma ,  William Ripka ,  Min Wu

    发明人： David Campbell ,  David Winn ,  Juan Betancort ,  Kevin Shreder ,  Yi Hu ,  Bei Li ,  Melissa Wong ,  Lifu Ma ,  William Ripka ,  Min Wu

    IPC分类号： A61K31/69 ,  C07F5/02

    CPC分类号： C07F5/025

    摘要： 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, R2, R3, R4 and R5 are as described herein.

    摘要翻译： 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是CH 2 2; S; O; CF 2或C（CH 3）2）2。 Z是H; 卤素; 羟; （C 1-6）烷氧基; （C 1-12）烷基; （C 3-12）环烷基; 苯基; 或杂芳基; 其中苯基和杂芳基任选被R 7独立或独立地取代; 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R 1，R 2，R 2，R 3，R 3， R 4和R 5如本文所述。

    PYRROLIDINE COMPOUNDS AND METHODS FOR SELECTIVE INHIBITION OF DIPEPTIDYL PEPTIDASE-IV
    2.
    发明申请
    PYRROLIDINE COMPOUNDS AND METHODS FOR SELECTIVE INHIBITION OF DIPEPTIDYL PEPTIDASE-IV 有权
    吡咯啉化合物和选择性抑制DIPEPTIDYL PEPTIDASE-IV的方法

    公开(公告)号：US20070299036A1

    公开(公告)日：2007-12-27

    申请号：US11833063

    申请日：2007-08-02

    申请人： David Campbell ,  David Winn ,  Juan Betancort

    发明人： David Campbell ,  David Winn ,  Juan Betancort

    IPC分类号： A61K31/69 ,  A61P3/10 ,  C12N9/99

    CPC分类号： C07F5/025

    摘要： The present invention is directed to a method of treatment of a malcondition that can be regulated or normalized via inhibition of DPP-IV. The method involves administration of an effective amount of a pyrrolidine compound of the invention, such as would be present in a pharmaceutical composition of the invention, to mammals, especially humans, to affect a malcondition that can be regulated or normalized via inhibition of DPP-IV.

    摘要翻译： 本发明涉及一种通过抑制DPP-IV来调节或归一化的病症的方法。 该方法包括将有效量的本发明的吡咯烷化合物（例如将存在于本发明的药物组合物中）施用于哺乳动物，特别是人，以影响可通过抑制DPP-1调节或归一化的病症， 四，

    Heterocyclic boronic acid compounds
    3.
    发明申请
    Heterocyclic boronic acid compounds 失效
    杂环硼酸化合物

    公开(公告)号：US20070060547A1

    公开(公告)日：2007-03-15

    申请号：US10514575

    申请日：2004-11-12

    申请人： David Campbell ,  David Winn ,  Juan Betancort

    发明人： David Campbell ,  David Winn ,  Juan Betancort

    IPC分类号： C07F5/02 ,  A61K31/69

    CPC分类号： C07F5/025

    摘要： 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.

    摘要翻译： 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是CH 2 2; S; O; CF 2或C（CH 3）2）2。 Z是H; 卤素; 羟; （C 1-6）烷氧基; （C 1-12）烷基; （C 3-12）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R i，R i，R i，R i，R i，R i，R i， R 4和R 5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。

    COMPOUNDS AND METHODS FOR SELECTIVE INHIBITION OF DIPEPTIDYL PEPTIDASE-IV
    4.
    发明申请
    COMPOUNDS AND METHODS FOR SELECTIVE INHIBITION OF DIPEPTIDYL PEPTIDASE-IV 失效
    选择性抑制DIPEPTIDYL PEPTIDASE-IV的化合物和方法

    公开(公告)号：US20060276410A1

    公开(公告)日：2006-12-07

    申请号：US11420273

    申请日：2006-05-25

    申请人： David Campbell ,  David Winn ,  Juan Betancort

    发明人： David Campbell ,  David Winn ,  Juan Betancort

    IPC分类号： A61K38/04 ,  C07F5/02 ,  A61K31/69

    CPC分类号： C07F5/025

    摘要： Compounds that selectively inhibit dipeptidyl peptidase-IV over closely related dipeptidyl peptidases are those of Formula (I): as well as pharmaceutically acceptable salts thereof, cyclic isomers thereof, prodrugs thereof, and solvates thereof, where all the variables are defined herein. These compounds can be used, alone or in combination with other drugs, for the treatment of diabetes and related diseases.

    摘要翻译： 选择性抑制二肽基肽酶-IV超过密切相关的二肽基肽酶的化合物是式（I）的化合物：及其药学上可接受的盐，其环状异构体，其前药和溶剂合物，其中所有变量均在本文中定义。 这些化合物可以单独使用或与其他药物组合使用，用于治疗糖尿病和相关疾病。

    METHYL AND ETHYL SUBSTITUTED PYRROLIDINE COMPOUNDS AND METHODS FOR SELECTIVE INHIBITION OF DIPEPTIDYL PEPTIDASE-IV
    5.
    发明申请
    METHYL AND ETHYL SUBSTITUTED PYRROLIDINE COMPOUNDS AND METHODS FOR SELECTIVE INHIBITION OF DIPEPTIDYL PEPTIDASE-IV 有权
    甲基和乙基取代的吡咯烷酮化合物及其选择性抑制DIPEPTIDYL PEPTIDASE-IV的方法

    公开(公告)号：US20060264401A1

    公开(公告)日：2006-11-23

    申请号：US11381090

    申请日：2006-05-01

    申请人： David Campbell ,  David Winn ,  Juan Betancort

    发明人： David Campbell ,  David Winn ,  Juan Betancort

    IPC分类号： A61K31/69 ,  C07F5/02

    CPC分类号： C07F5/025

    摘要： The present invention is directed to pyrrolidinylaminoacetyl pyrrolidine boronic acid compounds that display selective, potent dipeptidyl peptidase IV inhibitory activity. These compounds are useful for the treatment of disorders that can be regulated or normalized via inhibition of DPP-IV including those characterized by impaired glycemic control such as Diabetes Mellitus and related conditions. The compounds can be administered alone or with another medicament that displays pharmacological activity for treatment of these and other diseases.

    摘要翻译： 本发明涉及显示选择性，有效的二肽基肽酶IV抑制活性的吡咯烷基氨基乙酰基吡咯烷硼酸化合物。 这些化合物可用于治疗可以通过抑制DPP-IV调节或归一化的疾病，包括以血糖控制受损为特征的糖尿病和相关病症。 化合物可以单独施用或与另外一种显示用于治疗这些和其它疾病的药理活性的药物一起施用。

    PYRROLIDINE COMPOUNDS AND METHODS FOR SELECTIVE INHIBITION OF DIPEPTIDYL PEPTIDASE-IV
    6.
    发明申请
    PYRROLIDINE COMPOUNDS AND METHODS FOR SELECTIVE INHIBITION OF DIPEPTIDYL PEPTIDASE-IV 有权
    吡咯啉化合物和选择性抑制DIPEPTIDYL PEPTIDASE-IV的方法

    公开(公告)号：US20060264400A1

    公开(公告)日：2006-11-23

    申请号：US11381085

    申请日：2006-05-01

    申请人： David Campbell ,  David Winn ,  Juan Betancort

    发明人： David Campbell ,  David Winn ,  Juan Betancort

    IPC分类号： A61K31/69 ,  C07F5/02

    CPC分类号： C07F5/025

    摘要： The present invention is directed to pyrrolidinylaminoacetyl pyrrolidine boronic acid compounds that display selective, potent dipeptidyl peptidase IV inhibitory activity. These compounds are useful for the treatment of disorders that can be regulated or normalized via inhibition of DPP-IV including those characterized by impaired glycemic control such as Diabetes Mellitus and related conditions. The compounds can be administered alone or with another medicament that displays pharmacological activity for treatment of these and other diseases.

    摘要翻译： 本发明涉及显示选择性，有效的二肽基肽酶IV抑制活性的吡咯烷基氨基乙酰基吡咯烷硼酸化合物。 这些化合物可用于治疗可以通过抑制DPP-IV调节或归一化的疾病，包括以血糖控制受损为特征的糖尿病和相关病症。 化合物可以单独施用或与另外一种显示用于治疗这些和其它疾病的药理活性的药物一起施用。

    PYRROLIDINE COMPOUNDS AND METHODS FOR SELECTIVE INHIBITION OF DIPEPTIDYL PEPTIDASE-IV
    7.
    发明申请
    PYRROLIDINE COMPOUNDS AND METHODS FOR SELECTIVE INHIBITION OF DIPEPTIDYL PEPTIDASE-IV 有权
    吡咯啉化合物和选择性抑制DIPEPTIDYL PEPTIDASE-IV的方法

    公开(公告)号：US20060258621A1

    公开(公告)日：2006-11-16

    申请号：US11381082

    申请日：2006-05-01

    申请人： David Campbell ,  David Winn ,  Juan Betancort

    发明人： David Campbell ,  David Winn ,  Juan Betancort

    IPC分类号： A61K31/69 ,  C07F5/02

    CPC分类号： C07F5/025

    摘要： The present invention is directed to pyrrolidinylaminoacetyl pyrrolidine boronic acid compounds that display selective, potent dipeptidyl peptidase IV (DPP-IV) inhibitory activity. These compounds are useful for the treatment of disorders that can be regulated or normalized via inhibition of DPP-IV including those characterized by impaired glycemic control such as Diabetes Mellitus and related conditions. The compounds can be administered alone or with another medicament that displays pharmacological activity for treatment of these and other diseases.

    摘要翻译： 本发明涉及显示选择性，有效的二肽基肽酶IV（DPP-IV）抑制活性的吡咯烷基氨基乙酰基吡咯烷硼酸化合物。 这些化合物可用于治疗可以通过抑制DPP-IV调节或归一化的疾病，包括以血糖控制受损为特征的糖尿病和相关病症。 化合物可以单独施用或与另外一种显示用于治疗这些和其它疾病的药理活性的药物一起施用。

    Constrained cyano compounds
    8.
    发明申请
    Constrained cyano compounds 失效
    约束氰基化合物

    公开(公告)号：US20060009518A1

    公开(公告)日：2006-01-12

    申请号：US11179797

    申请日：2005-07-12

    申请人： David Campbell ,  Juan Betancort ,  David Winn

    发明人： David Campbell ,  Juan Betancort ,  David Winn

    IPC分类号： A61K31/277

    CPC分类号： C07D513/04

    摘要： Certain constrained cyano compounds are useful as inhibitors of post-proline/alanine cleaving amino-dipeptidases. Accordingly, these compounds can be employed, alone or with another therapeutic agent, to treat diabetes (especially, Type II diabetes), hyperglycemia, Syndrome X, diabetic complications, hyperinsulinemia, obesity, atherosclerosis and related diseases, as well as various immunomodulatory diseases and chronic inflammatory bowel disease.

    摘要翻译： 某些受限的氰基化合物可用作后脯氨酸/丙氨酸切割氨基二肽酶的抑制剂。 因此，这些化合物可以单独或与另一种治疗剂一起用于治疗糖尿病（特别是II型糖尿病），高血糖症，X综合征，糖尿病并发症，高胰岛素血症，肥胖症，动脉粥样硬化和相关疾病以及各种免疫调节性疾病，以及 慢性炎性肠病。

    Acyl-nucleotide probes and methods of their synthesis and use in proteomic analysis
    9.
    发明申请
    Acyl-nucleotide probes and methods of their synthesis and use in proteomic analysis 有权
    酰基核苷酸探针及其合成方法，用于蛋白质组学分析

    公开(公告)号：US20050043507A1

    公开(公告)日：2005-02-24

    申请号：US10817454

    申请日：2004-04-01

    申请人： David Campbell ,  Marek Liyanage ,  Anna Szardenings ,  Min Wu

    发明人： David Campbell ,  Marek Liyanage ,  Anna Szardenings ,  Min Wu

    IPC分类号： C07F9/6512 ,  C07H19/10 ,  C07H19/20 ,  C07H21/04 ,  C07K9/00 ,  C12Q20060101 ,  C12Q1/68

    CPC分类号： C07H19/10 ,  C07H19/20 ,  C07H21/04 ,  C12Q1/485

    摘要： The present invention provides tagged acyl phosphate probes (“TAPPs”), and methods of their preparation and use. The subject methods and compositions can provide enhanced simplicity and accuracy in identifying changes in the presence, amount, or activity of target proteins in a complex protein mixture, preferably nucleotide binding proteins using nucleotide binding protein-directed TAPPs. The profiling methods described herein can have a number of steps leading to the identification of target nucleotide binding protein(s) in a complex protein mixture.

    摘要翻译： 本发明提供标记的酰基磷酸酯探针（“TAPPs”）及其制备和使用的方法。 本发明的方法和组合物可以提供增强的简单性和准确性，以鉴别复合蛋白混合物中靶蛋白的存在，量或活性的变化，优选使用核苷酸结合蛋白质导向的TAPP的核苷酸结合蛋白。 本文描述的谱分析方法可以具有导致鉴定复合蛋白质混合物中的靶核苷酸结合蛋白的多个步骤。