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1. 发明申请

US20080300413A1 Methods of Preparing Hetercyclic Boronic Acids and Derivatives Thereof 有权
标题翻译：制备杂环硼酸及其衍生物的方法
公开(公告)号：US20080300413A1
公开(公告)日：2008-12-04
申请号：US11996792
申请日：2006-07-27
申请人： David Alan Campbell , David T. Winn
发明人： David Alan Campbell , David T. Winn
IPC分类号： C07F5/02 , C07D207/04
CPC分类号： C07F5/025
摘要： In the context of synthesizing heterocyclic boronic acid compounds, a convergent synthetic methodology is particularly efficient for preparing boropyrrolidines and derivatives of boropyrrolidines.
摘要翻译：在合成杂环硼酸化合物的情况下，收敛的合成方法对于制备硼氮杂环丁烷和硼吡咯烷的衍生物是特别有效的。

2. 发明授权

US07923433B2 Activity-based probes and methods of their preparation and use 有权
标题翻译：基于活性的探针及其制备和使用方法
公开(公告)号：US07923433B2
公开(公告)日：2011-04-12
申请号：US10530646
申请日：2003-10-08
申请人： David Winn , David Alan Campbell
发明人： David Winn , David Alan Campbell
IPC分类号： A61K38/05
CPC分类号： C07D311/90 , C07D311/82 , C12Q1/37
摘要： The present invention provides compositions and methods for assessing profiles of catalytically active enzymes in compositions containing a plurality of proteins. In preferred embodiments, the enzyme is a hydrolase, most preferably a cysteine protease. The methods described herein use activity based probes (“ABPs”) that have an affinity moiety for directing the binding of the ABP to one or more catalytically active target enzymes, a reactive group for forming a covalent bond at an active site of the target enzyme(s), and a TAG (e.g., a detectable label, preferably a fluorophore). One or more ABPs may be combined with a protein-containing sample under conditions for binding and reaction of the ABP(s) with target enzyme(s) that are present in the sample. The resulting products may then be used to assess the active enzyme profile of the sample, and can be correlated to the presence, amount, or activity of one or more target enzyme(s) present in the original complex protein mixture.
摘要翻译：本发明提供了用于在含有多种蛋白质的组合物中评估催化活性酶的谱的组合物和方法。在优选的实施方案中，酶是水解酶，最优选半胱氨酸蛋白酶。本文描述的方法使用具有亲和部分的活性基探针（“ABP”），该亲和部分用于引导ABP与一种或多种催化活性靶酶的结合，用于在靶酶的活性位点形成共价键的反应性基团（例如，可检测标记，优选荧光团）。可以在ABP与样品中存在的目标酶的结合和反应的条件下，将一种或多种ABP与含蛋白质的样品组合。然后可以将所得产物用于评估样品的活性酶谱，并且可与存在于原始复合蛋白混合物中的一种或多种目标酶的存在，量或活性相关。

3. 发明授权

US07786312B2 Methods of preparing heterocyclic boronic acids and derivatives thereof 有权
标题翻译：制备杂环硼酸及其衍生物的方法
公开(公告)号：US07786312B2
公开(公告)日：2010-08-31
申请号：US11996792
申请日：2006-07-27
申请人： David Alan Campbell , David T. Winn
发明人： David Alan Campbell , David T. Winn
IPC分类号： C07F5/02
CPC分类号： C07F5/025
摘要： In the context of synthesizing heterocyclic boronic acid compounds, a convergent synthetic methodology is particularly efficient for preparing boropyrrolidines and derivatives of boropyrrolidines.
摘要翻译：在合成杂环硼酸化合物的情况下，收敛的合成方法对于制备硼氮杂环丁烷和硼吡咯烷的衍生物是特别有效的。

4. 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。

5. 发明申请

US20100087658A1 METHODS AND INTERMEDIATES FOR SYNTHESIS OF SELECTIVE DPP-IV INHIBITORS 审中-公开
标题翻译：合成DPP-IV抑制剂的方法和中间体
公开(公告)号：US20100087658A1
公开(公告)日：2010-04-08
申请号：US12529016
申请日：2008-03-05
申请人： David Alan Campbell , Emília P.T. Leitão , Zhen-Ping Wu , Peng Wang
发明人： David Alan Campbell , Emília P.T. Leitão , Zhen-Ping Wu , Peng Wang
IPC分类号： C07F5/02 , C07D403/12 , C07D207/00
CPC分类号： C07F5/025 , C07D207/14
摘要： Methods and intermediates for the synthesis of selective inhibitors of dipeptidyl peptidase IV (DPP-IV) are provided. Coupling of a carboxylate salt with a boro-proline derivative provides a protected form of a DPP-IV inhibitor, which may be deblocked to yield the medicinal compound. The carboxylate salt can be a crystalline form of a sodium salt or a dicyclohexylammonium salt. The inhibitor can be used in the treatment of diabetes.
摘要翻译：提供了合成二肽基肽酶IV（DPP-IV）选择性抑制剂的方法和中间体。羧酸盐与硼 - 脯氨酸衍生物的偶联提供了DPP-IV抑制剂的保护形式，其可以被解封以产生药用化合物。羧酸盐可以是钠盐或二环己基铵盐的结晶形式。该抑制剂可用于治疗糖尿病。

6. 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。

7. 发明授权

US5816626A Spring lock coupling 失效
标题翻译：弹簧锁联轴器
公开(公告)号：US5816626A
公开(公告)日：1998-10-06
申请号：US567617
申请日：1995-12-05
申请人： Claudia Mills Anderson , David Alan Campbell , Fred Georg Schroeder
发明人： Claudia Mills Anderson , David Alan Campbell , Fred Georg Schroeder
IPC分类号： F16K51/00 , F16J15/06 , F16L37/22 , F16L39/02
CPC分类号： F16L37/22
摘要： There is disclosed herein a tubular coupling comprising a first tube, a cage disposed on an end portion of the first tube, a bead for retaining the cage on the end portion of the first tube and a second tube telescopically engageable with the first tube. The coupling further include a spring disposed around the cage for preventing telescopic disengagement of the second tube from the first tube as well as a plurality of o-rings disposed on the end of the first tube. One of the o-rings is disposed at the pivot point of the coupling, the pivot point being defined as the midpoint of the distance between a first contact point and a second contact point between the first tube and the second tube when the tubes are engaged.
摘要翻译：这里公开了一种管状联接器，其包括第一管，设置在第一管的端部上的保持架，用于将保持架保持在第一管的端部上的胎圈和可与第一管可伸缩接合的第二管。联接器还包括围绕保持架设置的弹簧，用于防止第二管从第一管伸出分离以及设置在第一管的端部上的多个O形环。 O形环中的一个设置在联轴器的枢转点处，枢转点被定义为当管接合时第一管和第二管之间的第一接触点和第二接触点之间的距离的中点。

8. 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。

9. 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。

10. 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。

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