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31. 发明授权

US5463028A Reagents for generating a polyclonal hydrolytic antibody response against cocaine and the monoclonal hydrolytic antibodies against cocaine derived through these reagents 失效
标题翻译：用于产生针对可卡因的多克隆水解抗体应答的试剂和通过这些试剂衍生的可卡因的单克隆水解抗体
公开(公告)号：US5463028A
公开(公告)日：1995-10-31
申请号：US862801
申请日：1992-04-03
申请人： Donald W. Landry , Kang Zhao
发明人： Donald W. Landry , Kang Zhao
IPC分类号： G01N33/53 , A61K31/46 , A61K38/00 , A61K39/00 , A61K47/48 , A61P39/02 , C07D451/02 , C07D451/04 , C07F9/6561 , C07F9/6571 , C07F9/6584 , C07K14/76 , C07K16/00 , C07K16/44 , C07K19/00 , C12N9/00 , C07K17/02 , C07K16/46
CPC分类号： C07D451/02 , A61K47/48384 , C07F9/6561 , C07F9/657172 , C07F9/6584 , C07K16/44 , C12N9/0002 , A61K38/00
摘要： This invention provides a compound comprising a methyl ecgonine group chemically attached to a phenylphosphonic group which is an analog to an intermediate of the hydrolysis transition-state of a cocaine benzoyl ester group. This invention also provides such analogs linked to carrier proteins, and antibodies thereto.
摘要翻译：本发明提供了一种化合物，其包含与苯基膦酸基化学连接的甲基厄吲嗪基，其与可卡因苯甲酰酯基的水解转变状态的中间体类似。本发明还提供了与载体蛋白质及其抗体连接的类似物。

32. 发明授权

US09260391B2 Hypoglycemic dihydropyridones 有权
标题翻译：低血糖二氢吡啶酮
公开(公告)号：US09260391B2
公开(公告)日：2016-02-16
申请号：US13058142
申请日：2009-08-07
申请人： Yuli Xie , Shixian Deng , Donald W. Landry , Paul Harris , Antonella Maffei
发明人： Yuli Xie , Shixian Deng , Donald W. Landry , Paul Harris , Antonella Maffei
IPC分类号： A61K31/45 , A61K31/351 , C07D211/74 , C07D309/30 , C07D211/94 , C07D211/76 , C07D211/88 , C07D309/32 , C07D471/04
CPC分类号： C07D211/94 , C07D211/76 , C07D211/88 , C07D309/32 , C07D471/04
摘要： The present invention provides, inter alia, a compound of formula I: wherein the substituent designations are indicated in the Specification. The present invention also provides pharmaceutical compositions comprising a compound of formula I, and methods of treatment or prevention of diabetes or hyperglycemia in a patient, and of normalizing blood glucose levels in a subject, by administering an effective amount of a compound of formula I.
摘要翻译：本发明尤其提供式I化合物：其中取代基名称在说明书中指出。本发明还提供了包含式I化合物的药物组合物，以及通过施用有效量的式I化合物来治疗或预防患者中的糖尿病或高血糖并使受试者血糖水平正常化的方法。

33. 发明授权

US08846742B2 Neuronal pain pathway modulators 有权
标题翻译：神经元疼痛途径调节剂
公开(公告)号：US08846742B2
公开(公告)日：2014-09-30
申请号：US11674965
申请日：2007-02-14
申请人： Richard Ambron , Ying-Ju Sung , Jeremy Greenwood , Leah Frye , Shi-Xian Deng , Yuli Xie , Donald W. Landry
发明人： Richard Ambron , Ying-Ju Sung , Jeremy Greenwood , Leah Frye , Shi-Xian Deng , Yuli Xie , Donald W. Landry
IPC分类号： A61K31/415 , A61K31/335
CPC分类号： A61K31/40 , A61K31/235 , A61K31/335
摘要： The present invention relates to compounds that may be used to inhibit activation of protein kinase G (“PKG”). It is based, at least in part, on the discovery of the tertiary structure of PKG and the identification of molecules that either bind to the active site of PKG and/or are analogs of balanol.
摘要翻译：本发明涉及可用于抑制蛋白激酶G（“PKG”）活化的化合物。至少部分基于PKG的三级结构的发现以及与PKG的活性位点结合的分子的鉴定和/或是平衡醇的类似物。

34. 发明授权

US08637009B2 Thermostabilization of proteins 失效
标题翻译：蛋白质的稳定性
公开(公告)号：US08637009B2
公开(公告)日：2014-01-28
申请号：US12667895
申请日：2008-07-10
申请人： Donald W. Landry , James H. Woods , Roger K. Sunahara , Diwahar L. Narasimhan , Joanne MacDonald , Milan N. Stojanovich , John J. Tesmer , Remy L. Brim
发明人： Donald W. Landry , James H. Woods , Roger K. Sunahara , Diwahar L. Narasimhan , Joanne MacDonald , Milan N. Stojanovich , John J. Tesmer , Remy L. Brim
IPC分类号： A61K38/46 , C12N9/96
CPC分类号： A61K38/465 , A61K9/0019 , A61K31/505 , A61K45/06 , A61K47/12 , A61K47/18 , A61K47/22 , A61K47/542 , A61K47/545 , A61K47/60 , C12N9/18 , C12Q1/44 , C12Y301/01084 , G01N2333/918 , A61K2300/00
摘要： Provided are compositions comprising a cocaine esterase (CocE) and a compound that thermostabilizes the CocE. Also provided are methods of thermostabilizing a cocaine esterase. Additionally provided are methods of treating a mammal undergoing a cocaine-induced condition. Methods of determining whether a compound is a thermostabilizing agent for a protein are also provided. Uses of the above-described compositions for the treatment of a cocaine-induced condition is additionally provided. Additionally provided is an isolated nucleic acid encoding a CocE polypeptide having the substitutions L169K and G173Q, and the CocE polypeptide encoded by that nucleic acid, and pharmaceutical compositions thereof. Further provided is the use of that composition for the manufacture of a medicament for the treatment of a cocaine-induced condition and for the treatment of a cocaine-induced condition.
摘要翻译：提供了包含可卡因酯酶（CocE）和使CocE稳定化合物的组合物。还提供了热稳定可卡因酯酶的方法。另外提供了治疗经历可卡因诱导病症的哺乳动物的方法。还提供了确定化合物是否是蛋白质的热稳定剂的方法。另外提供了上述用于治疗可卡因诱导病症的组合物的用途。另外提供了编码具有取代L169K和G173Q的CocE多肽和由该核酸编码的CocE多肽的分离的核酸及其药物组合物。还提供了该组合物用于制备用于治疗可卡因诱导的病症和用于治疗可卡因诱导病症的药物的用途。

35. 发明申请

US20120269828A1 ANTI-DRUG VACCINES 有权
标题翻译：抗药灭活剂
公开(公告)号：US20120269828A1
公开(公告)日：2012-10-25
申请号：US13452019
申请日：2012-04-20
申请人： Shi-Xian Deng , Donald W. Landry , Gavreel Kalantarov , Trakht IIya
发明人： Shi-Xian Deng , Donald W. Landry , Gavreel Kalantarov , Trakht IIya
IPC分类号： A61K39/385 , A61P37/04 , A61K39/44 , A61P25/30 , C07D451/12 , C07K17/02
CPC分类号： A61K39/0013 , A61K31/44 , A61K39/385 , A61K47/643 , A61K47/646 , A61K2039/505 , A61K2039/55566 , A61K2039/6056 , A61K2039/6081
摘要： The present invention relates to anti-drug vaccines based on conjugates between the drug and a non-immunogenic carrier protein. In preferred embodiments, it provides for anti-cocaine vaccines and their use to diminish the effects and/or use of cocaine in a subject.
摘要翻译：本发明涉及基于药物和非免疫原性载体蛋白质之间的缀合物的抗药物疫苗。在优选的实施方案中，它提供了抗可卡因疫苗及其用于减少受试者中可卡因的作用和/或使用的用途。

36. 发明申请

US20120129939A1 POLYAMINE INHIBITORS FOR THE TREATMENT AND PREVENTION OF PARKINSON'S DISEASE 审中-公开
标题翻译：用于治疗和预防帕金森病的多胺抑制剂
公开(公告)号：US20120129939A1
公开(公告)日：2012-05-24
申请号：US13203649
申请日：2010-03-01
申请人： Scott A. Small , Nicole Lewandowski , Donald W. Landry , Shi-Xiang Deng
发明人： Scott A. Small , Nicole Lewandowski , Donald W. Landry , Shi-Xiang Deng
IPC分类号： A61K31/197 , A61P25/16 , C07D243/04 , C07D241/08 , A61K31/132 , C07C229/26
CPC分类号： A61K31/13 , A61K31/00
摘要： Disclosed herein are methods for treating a disease involving α-synucleic aggregation using (1) a compound which reduces the amount of polyamines in an amount effective to reduce α-synucleic aggregation; (2) a compound which inhibits polyamine synthesis in an amount effective to reduce α-synucleic aggregation; or (3) a compound which inhibits α-synucleic aggregation in an amount effective to reduce α-synucleic aggregation. Also disclosed are methods for reducing the amount of α-synucleic aggregation in a brain cell using (1) a compound which reduces the amount of polyamines in an amount effective to reduce α-synucleic aggregation; (2) a compound which inhibits polyamine synthesis in an amount effective to reduce α-synucleic aggregation; or (3) a compound which inhibits α-synucleic aggregation in an amount effective to reduce α-synucleic aggregation. Disclosed herein are also compounds which can be used in the above described methods.
摘要翻译：本文公开了使用以下方法治疗涉及α-解聚聚集的疾病的方法：（1）减少多胺有效降低α-解磷聚集的量的化合物; （2）抑制多胺合成的化合物，其量有效降低α-解磷聚集; 或（3）以有效减少α-解聚聚集的量抑制α-突触聚集的化合物。还公开了使用（1）以有效减少α-鸟氨酸聚集的量减少多胺的量的化合物来减少脑细胞中的α-突触聚集的量的方法; （2）抑制多胺合成的化合物，其量有效降低α-解磷聚集; 或（3）以有效减少α-解聚聚集的量抑制α-突触聚集的化合物。本文公开的也是可以用于上述方法的化合物。

37. 发明申请

US20120076732A1 PHOSPHODIESTERASE INHIBITORS AND USES THEREOF 有权
标题翻译：磷酸二酯酶抑制剂及其用途
公开(公告)号：US20120076732A1
公开(公告)日：2012-03-29
申请号：US13167540
申请日：2011-06-23
申请人： Yan Feng , Ottavio Arancio , Shixian Deng , Donald W. Landry
发明人： Yan Feng , Ottavio Arancio , Shixian Deng , Donald W. Landry
IPC分类号： A61K31/4706 , A61K49/00 , A61K31/5025 , A61P25/00 , A61K31/519 , A61K31/4985 , C07D215/44 , A61P25/28
CPC分类号： A61K31/4706 , C07D215/48 , C07D215/54
摘要： The invention provides for compounds that are phosphodiesterase inhibitors. The invention further provides for a method for screening compounds that bind to and modulate a phosphosdiesterase protein. The invention also provides methods for treating conditions associated with accumulated amyloid-beta peptide deposit accumulations by administering a phosphodiesterase-binding compound to a subject.
摘要翻译：本发明提供了磷酸二酯酶抑制剂的化合物。本发明进一步提供了一种筛选结合并调节磷酸二酯酶蛋白质的化合物的方法。本发明还提供了通过向受试者施用磷酸二酯酶结合化合物来治疗与累积的淀粉样蛋白-β肽沉积物积累相关的病症的方法。

38. 发明授权

US08022058B2 Agents for preventing and treating disorders involving modulation of the RyR receptors 有权
标题翻译：用于预防和治疗涉及RyR受体调节的病症的药剂
公开(公告)号：US08022058B2
公开(公告)日：2011-09-20
申请号：US11212309
申请日：2005-08-25
申请人： Andrew Robert Marks , Donald W. Landry , Shixian Deng
发明人： Andrew Robert Marks , Donald W. Landry , Shixian Deng
IPC分类号： A61P9/00 , A61P19/00 , A61P25/00 , A61K31/554 , C07D281/10
CPC分类号： C07D417/12 , C07D281/10 , C07D417/06 , C07D417/14
摘要： The present invention provides novel compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells. Such disorders and diseases include, by way of example only, cardiac disorders and diseases, skeletal muscular disorders and diseases, cognitive disorders and diseases, malignant hyperthermia, diabetes, and sudden infant death syndrome. Cardiac disorder and diseases include, but are not limited to, irregular heartbeat disorders and diseases; exercise-induced irregular heartbeat disorders and diseases; sudden cardiac death; exercise-induced sudden cardiac death; congestive heart failure; chronic obstructive pulmonary disease; and high blood pressure. Irregular heartbeat disorders and diseases include and exercise-induced irregular heartbeat disorders and diseases include, but are not limited to, atrial and ventricular arrhythmia; atrial and ventricular fibrillation; atrial and ventricular tachyarrhythmia; atrial and ventricular tachycardia; catecholaminergic polymorphic ventricular tachycardia (CPVT); and exercise-induced variants thereof. Skeletal muscular disorder and diseases include, but are not limited to, skeletal muscle fatigue, exercise-induced skeletal muscle fatigue, muscular dystrophy, bladder disorders, and incontinence. Cognitive disorders and diseases include, but are not limited to, Alzheimer's Disease, forms of memory loss, and age-dependent memory loss.
摘要翻译：本发明提供新的式I化合物及其盐，水合物，溶剂合物，络合物和前药。本发明还提供了合成式I化合物的方法。本发明另外提供包含式I化合物的药物组合物和使用式I药物组合物的方法，以治疗和预防与调节钙的RyR受体相关的疾病和疾病通道在单元格中起作用。这样的疾病和疾病仅包括心脏病和疾病，骨骼肌障碍和疾病，认知障碍和疾病，恶性高热，糖尿病和婴儿猝死综合征。心脏疾病和疾病包括但不限于不规则的心跳障碍和疾病; 运动引起的心律失常和疾病不规律; 心脏猝死; 运动性心源性猝死; 充血性心力衰竭; 慢性阻塞性肺疾病; 和高血压。不规律的心跳疾病和疾病包括运动诱发的心律失常和疾病的疾病包括但不限于心房和室性心律失常; 心房和心室颤动; 心房和心室快速性心律失常; 心房和室性心动过速; 儿茶酚胺能多态性室性心动过速（CPVT）; 和运动诱发的变体。骨骼肌障碍和疾病包括但不限于骨骼肌疲劳，运动引起的骨骼肌疲劳，肌营养不良，膀胱障碍和失禁。认知障碍和疾病包括但不限于阿尔茨海默病，记忆丧失的形式和年龄依赖性记忆丧失。

39. 发明申请

US20100152440A1 NOVEL ANTI-ARRHYTHMIC AND HEART FAILURE DRUGS THAT TARGET THE LEAK IN THE RYANODINE RECEPTOR (RyR2) 审中-公开
标题翻译：靶向RYANODE受体（RyR2）的新型抗神经和心脏衰竭药物
公开(公告)号：US20100152440A1
公开(公告)日：2010-06-17
申请号：US12480396
申请日：2009-06-08
申请人： Andrew Robert Marks , Donald W. Landry , Shi Xian Deng , Zhen Zhuang Cheng
发明人： Andrew Robert Marks , Donald W. Landry , Shi Xian Deng , Zhen Zhuang Cheng
IPC分类号： C07D417/06 , C07D281/08
CPC分类号： C07D281/10 , C07D267/14 , C07D417/06 , C07D417/12 , G01N2800/325 , G01N2800/326
摘要： The present invention provides novel 1,4-benzothiazepine intermediates and derivatives, methods for synthesizing same, and methods for assaying same. The present invention also provides methods for using these novel compounds to limit or prevent a decrease in the level of RyR2-bound FKBP12.6 in a subject; to prevent exercise-induced sudden cardiac death in a subject; and to treat or prevent heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia in a subject. The present invention further provides methods for identifying an agent that enhances binding of RyR2 and FKBP12.6, and agents identified by these methods. Additionally, the present invention provides methods for identifying agents for use in treating or preventing heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia, and in preventing exercise-induced sudden cardiac death. Also provided are agents identified by such methods.
摘要翻译：本发明提供新的1,4-苯并硫氮杂中间体及其衍生物，其合成方法及其测定方法。本发明还提供了使用这些新化合物来限制或防止受试者中RyR2结合的FKBP12.6水平降低的方法; 以防止受试者运动性心源性猝死; 并且治疗或预防受试者的心力衰竭，心房颤动或运动引起的心律失常。本发明还提供用于鉴定增强RyR2和FKBP12.6的结合的试剂以及通过这些方法鉴定的试剂的方法。此外，本发明提供用于鉴定用于治疗或预防心力衰竭，心房颤动或运动诱导的心律失常以及预防运动性心源性猝死的药剂的方法。还提供了通过这种方法鉴定的药剂。

40. 发明授权

US07704990B2 Agents for preventing and treating disorders involving modulation of the RyR receptors 有权
标题翻译：用于预防和治疗涉及RyR受体调节的病症的药剂
公开(公告)号：US07704990B2
公开(公告)日：2010-04-27
申请号：US11212413
申请日：2005-08-25
申请人： Donald W. Landry , Shixian Deng , Zhen Zhuang Cheng
发明人： Donald W. Landry , Shixian Deng , Zhen Zhuang Cheng
IPC分类号： C07D281/02 , A61K31/554
CPC分类号： C07D281/10 , C07D417/12 , C07D417/14
摘要： The present invention provides novel compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells. Such disorders and diseases include, by way of example only, cardiac disorders and diseases, skeletal muscular disorders and diseases, cognitive disorders and diseases, malignant hyperthermia, diabetes, and sudden infant death syndrome. Cardiac disorder and diseases include, but are not limited to, irregular heartbeat disorders and diseases; exercise-induced irregular heartbeat disorders and diseases; sudden cardiac death; exercise-induced sudden cardiac death; congestive heart failure; chronic obstructive pulmonary disease; and high blood pressure. Irregular heartbeat disorders and diseases include and exercise-induced irregular heartbeat disorders and diseases include, but are not limited to, atrial and ventricular arrhythmia; atrial and ventricular fibrillation; atrial and ventricular tachyarrhythmia; atrial and ventricular tachycardia; catecholaminergic polymorphic ventricular tachycardia (CPVT); and exercise-induced variants thereof. Skeletal muscular disorder and diseases include, but are not limited to, skeletal muscle fatigue, exercise-induced skeletal muscle fatigue, muscular dystrophy, bladder disorders, and incontinence. Cognitive disorders and diseases include, but are not limited to, Alzheimer's Disease, forms of memory loss, and age-dependent memory loss.
摘要翻译：本发明提供新的式I化合物及其盐，水合物，溶剂合物，络合物和前药。本发明还提供了合成式I化合物的方法。本发明另外提供包含式I化合物的药物组合物和使用式I药物组合物的方法，以治疗和预防与调节钙的RyR受体相关的疾病和疾病通道在单元格中起作用。这样的疾病和疾病仅包括心脏病和疾病，骨骼肌障碍和疾病，认知障碍和疾病，恶性高热，糖尿病和婴儿猝死综合征。心脏疾病和疾病包括但不限于不规则的心跳障碍和疾病; 运动引起的心律失常和疾病不规律; 心脏猝死; 运动性心源性猝死; 充血性心力衰竭; 慢性阻塞性肺疾病; 和高血压。不规律的心跳疾病和疾病包括运动诱发的心律失常和疾病的疾病包括但不限于心房和室性心律失常; 心房和心室颤动; 心房和心室快速性心律失常; 心房和室性心动过速; 儿茶酚胺能多态性室性心动过速（CPVT）; 和运动诱发的变体。骨骼肌障碍和疾病包括但不限于骨骼肌疲劳，运动引起的骨骼肌疲劳，肌营养不良，膀胱障碍和失禁。认知障碍和疾病包括但不限于阿尔茨海默病，记忆丧失的形式和年龄依赖性记忆丧失。

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