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1. 发明授权

US07767828B2 Methyl and ethyl substituted pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV 有权
标题翻译：甲基和乙基取代的吡咯烷化合物和二肽基肽酶-IV的选择性抑制方法
公开(公告)号：US07767828B2
公开(公告)日：2010-08-03
申请号：US11381090
申请日：2006-05-01
申请人： David Alan Campbell , David T. Winn , Juan Manuel Betancort
发明人： David Alan Campbell , David T. Winn , Juan Manuel Betancort
IPC分类号： A61K31/69 , C07D403/12 , 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。

2. 发明授权

US07576121B2 Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV 有权
标题翻译：吡咯烷化合物和选择性抑制二肽基肽酶-IV的方法
公开(公告)号：US07576121B2
公开(公告)日：2009-08-18
申请号：US11381082
申请日：2006-05-01
申请人： David Alan Campbell , David T. Winn , Juan Manuel Betancort
发明人： David Alan Campbell , David T. Winn , Juan Manuel Betancort
IPC分类号： A61K31/4025 , C07D207/10
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。

3. 发明授权

US07825139B2 Compounds and methods for selective inhibition of dipeptidyl peptidase-IV 失效
标题翻译：选择性抑制二肽基肽酶-IV的化合物和方法
公开(公告)号：US07825139B2
公开(公告)日：2010-11-02
申请号：US11420273
申请日：2006-05-25
申请人： David Alan Campbell , David T. Winn , Juan Manuel Betancort
发明人： David Alan Campbell , David T. Winn , Juan Manuel Betancort
IPC分类号： A61K31/445 , C07D401/14
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。

4. 发明授权

US07317109B2 Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV 有权
标题翻译：吡咯烷化合物和选择性抑制二肽基肽酶-IV的方法
公开(公告)号：US07317109B2
公开(公告)日：2008-01-08
申请号：US11381085
申请日：2006-05-01
申请人： David Alan Campbell , David T. Winn , Juan Manuel Betancort
发明人： David Alan Campbell , David T. Winn , Juan Manuel 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。

5. 发明授权

US07884217B2 Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV 有权
标题翻译：吡咯烷化合物和选择性抑制二肽基肽酶-IV的方法
公开(公告)号：US07884217B2
公开(公告)日：2011-02-08
申请号：US11930337
申请日：2007-10-31
申请人： David Alan Campbell , David T. Winn , Juan Manuel Betancort
发明人： David Alan Campbell , David T. Winn , Juan Manuel 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。

6. 发明申请

US20100323953A1 MACROCYCLIC HEPATITIS C PROTEASE INHIBITORS 审中-公开
标题翻译：大环内酯类抗生素C蛋白酶抑制剂
公开(公告)号：US20100323953A1
公开(公告)日：2010-12-23
申请号：US12526018
申请日：2008-01-04
申请人： David Alan Campbell , Michael E. Hepperle , David T. Winn , Juan Manuel Betancort
发明人： David Alan Campbell , Michael E. Hepperle , David T. Winn , Juan Manuel Betancort
IPC分类号： A61K38/12 , C07K5/12 , A61P31/14
CPC分类号： C07K5/0827 , A61K38/00 , C07K5/0804 , C07K5/0812
摘要： The present invention provides novel macrocyclic compounds that mimic peptide substrates of the hepatitis C viral protease and inhibit the viral protease, more particularly as inhibitors of the NS3 serine protease from hepatitis C virus. Methods for synthesis of the compounds are also provided. The compounds find utility as antiviral agents directed at hepatitis C. The invention further provides methods of employing such inhibitors, alone or in combination with other therapeutic agents, to treat hepatitis C infection in a subject in need of such treatment.
摘要翻译：本发明提供了模拟丙型肝炎病毒蛋白酶的肽底物并抑制病毒蛋白酶的新的大环化合物，更特别地，作为来自丙型肝炎病毒的NS3丝氨酸蛋白酶的抑制剂。还提供了合成化合物的方法。该化合物可用作针对丙型肝炎的抗病毒剂。本发明还提供了使用这种抑制剂单独或与其它治疗剂组合的方法来治疗需要这种治疗的受试者中的丙型肝炎感染。

7. 发明申请

US20090325889A1 HEPATITIS C SERINE PROTEASE INHIBITORS AND USES THEREFOR 审中-公开
标题翻译： HEPATITIS C丝氨酸蛋白酶抑制剂及其用途
公开(公告)号：US20090325889A1
公开(公告)日：2009-12-31
申请号：US11996280
申请日：2006-07-28
申请人： David Alan Campbell , David T. Winn , Juan Manuel Betancort , Michael E. Hepperle
发明人： David Alan Campbell , David T. Winn , Juan Manuel Betancort , Michael E. Hepperle
IPC分类号： A61K38/06 , C12N9/99 , A61K38/05 , C07K5/083 , C07F5/02 , A61P31/12
CPC分类号： A61K38/05 , C07K5/06191
摘要： The present invention provides novel compounds which mimic peptides with a C-terminal penultimate proline, such compounds being useful as protease inhibitors, particularly as inhibitors of serine proteases, and more particularly as inhibitors of the NS3 serine protease from hepatitis C. The compounds find utility as antiviral agents directed at hepatitis C. The invention further provides methods of employing such inhibitors, alone or in combination with other therapeutic agents, to treat hepatitis C infection in a subject in need of such treatment.
摘要翻译：本发明提供了新型化合物，其模拟具有C-末端倒数第二脯氨酸的肽，这些化合物可用作蛋白酶抑制剂，特别是作为丝氨酸蛋白酶的抑制剂，更具体地，作为来自丙型肝炎的NS3丝氨酸蛋白酶的抑制剂。作为针对丙型肝炎的抗病毒剂。本发明还提供了使用这种抑制剂单独或与其它治疗剂组合的方法来治疗需要这种治疗的受试者中的丙型肝炎感染。

8. 发明申请

US20090304631A1 HEPATITIS C SERINE PROTEASE INHIBITORS AND USES THEREFOR 审中-公开
标题翻译： HEPATITIS C丝氨酸蛋白酶抑制剂及其用途
公开(公告)号：US20090304631A1
公开(公告)日：2009-12-10
申请号：US12162268
申请日：2007-01-25
申请人： David Alan Campbell , Michael E. Hepperle , Juan Manuel Betancort , David T. Winn
发明人： David Alan Campbell , Michael E. Hepperle , Juan Manuel Betancort , David T. Winn
IPC分类号： A61K31/69 , C07F5/02 , C07D403/12 , A61K39/395 , A61K38/16 , A61K38/21 , A61P31/12
CPC分类号： C07F5/025 , A61K38/212 , A61K2300/00
摘要： The invention provides compounds that inhibit a viral protease enzyme of the hepatitis C virus (HCV). The compounds are adapted for treatment of a HCV infection in a patient with the disease. The compounds include analogs of tripeptides and tetrapeptides that resemble the viral protease substrate. The invention also provides pharmaceutical compositions and combinations, methods of preparation of the compounds, and methods of treatment of patients afflicted with HCV using the compounds.
摘要翻译：本发明提供抑制丙型肝炎病毒（HCV）病毒蛋白酶的化合物。该化合物适于治疗患有该疾病的患者中的HCV感染。这些化合物包括类似于病毒蛋白酶底物的三肽和四肽的类似物。本发明还提供药物组合物和组合，化合物的制备方法，以及使用该化合物治疗患有HCV的患者的方法。

9. 发明授权

US08415295B2 Heterocyclic boronic acid compounds 有权
标题翻译：杂环硼酸化合物
公开(公告)号：US08415295B2
公开(公告)日：2013-04-09
申请号：US12692276
申请日：2010-01-22
申请人： David Alan Campbell , David T. Winn , Juan Manuel Betancort
发明人： David Alan Campbell , David T. Winn , Juan Manuel Betancort
IPC分类号： A61K38/28 , A61K31/69 , C07F5/02 , 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(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; 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。

10. 发明授权

US07906658B2 Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV 有权
标题翻译：吡咯烷化合物和选择性抑制二肽基肽酶-IV的方法
公开(公告)号：US07906658B2
公开(公告)日：2011-03-15
申请号：US11833063
申请日：2007-08-02
申请人： David Alan Campbell , David T. Winn , Juan Manuel Betancort
发明人： David Alan Campbell , David T. Winn , Juan Manuel Betancort
IPC分类号： A61K31/69 , C07D403/12
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，

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