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1. 发明申请

US20100120661A1 HETEROCYCLIC BORONIC ACID COMPOUNDS 有权
标题翻译：杂环硼酸化合物
公开(公告)号：US20100120661A1
公开(公告)日：2010-05-13
申请号：US12692276
申请日：2010-01-22
申请人： David A. Campbell , David T. Winn , Juan M. Betancort
发明人： David A. Campbell , David T. Winn , Juan M. Betancort
IPC分类号： A61K38/28 , C07F5/02 , A61K31/69 , C12N9/99 , C07D205/02 , A61P3/10
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(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.
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。

2. 发明申请

US20100120716A1 MACROCYCLIC HEPATITIS C SERINE PROTEASE INHIBITORS AND USES THEREFOR 审中-公开
标题翻译：大环内酯类抗生素C丝氨酸蛋白酶抑制剂及其用途
公开(公告)号：US20100120716A1
公开(公告)日：2010-05-13
申请号：US12515941
申请日：2007-12-05
申请人： David A. Campbell , Michael E. Hepperle , David T. Winn , Juan M. Betancort
发明人： David A. Campbell , Michael E. Hepperle , David T. Winn , Juan M. Betancort
IPC分类号： A61K31/69 , C07D267/00 , C07D245/04 , A61P31/12
CPC分类号： C07F5/025
摘要： Macrocyclic inhibitors of Hepatitis C protease are provided, the inhibitors including a boronic acid or ester group, a macrocyclic ring of about 13 to 25 atoms including at least two amide linkages, a proline-analogous group, and a connecting segment joining moieties on either side of the proline-analogous group. Methods of making the HCV protease-inhibitory compounds, methods of using the compounds, formulations of the compounds, and pharmaceutical combinations including the compounds, are provided.
摘要翻译：提供丙型肝炎蛋白酶的大环抑制剂，所述抑制剂包括硼酸或酯基，约13至25个原子的大环，包括至少两个酰胺键，脯氨酸类似基团和连接部分连接任一侧的部分的脯氨酸类似组。提供制备HCV蛋白酶抑制化合物的方法，使用化合物的方法，化合物的制剂以及包括该化合物的药物组合。

3. 发明授权

US07674913B2 Heterocyclic boronic acid compounds 失效
标题翻译：杂环硼酸化合物
公开(公告)号：US07674913B2
公开(公告)日：2010-03-09
申请号：US10514575
申请日：2004-11-12
申请人： David A. Campbell , David T. Winn , Juan M. Betancort
发明人： David A. Campbell , David T. Winn , Juan M. Betancort
IPC分类号： A61K31/69 , C07D403/12 , 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, 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。

4. 发明申请

US20060135553A1 Imidazole derivatives 审中-公开
标题翻译：咪唑衍生物
公开(公告)号：US20060135553A1
公开(公告)日：2006-06-22
申请号：US11262394
申请日：2005-10-28
申请人： David A. Campbell , Juan M. Betancort
发明人： David A. Campbell , Juan M. Betancort
IPC分类号： A61K31/4745 , A61K31/444 , C07D471/02 , C07D403/14
CPC分类号： C07D403/12 , C07D235/06 , C07D401/12
摘要： Certain imidazole-containing compounds are useful for treating and/or preventing of various disease conditions, by way of methodology for modulating tyrosine kinases and angiogenesis. Illustrative of such conditions are inflammatory diseases and diseases characterized by abnormal cellular proliferation.
摘要翻译：通过用于调节酪氨酸激酶和血管生成的方法，某些含咪唑化合物可用于治疗和/或预防各种疾病状况。这些病症的说明是炎性疾病和以细胞增殖异常为特征的疾病。

5. 发明专利

IL175550D0 HETEROCYCLIC BORONIC ACID COMPOUNDS 未知
公开(公告)号：IL175550D0
公开(公告)日：2006-09-05
申请号：IL17555006
申请日：2006-05-10
申请人： PHENOMIX CORP , CAMPBELL DAVID ALAN , WINN DAVID T , JUAN M BETANCORT
IPC分类号： C07F20100101 , C07F5/02
摘要： Dipeptidyl peptidase IV (DPP-IV)-inhibiting compounds are provided that have formula (VI): including all cyclic isomers thereof, stereoisomers thereof, solvates thereof, hydrates thereof, and pharmaceutically acceptable salts thereof, and any prodrug thereof, their method of preparing and use, and a pharmaceutical composition of compound (VI).

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