公开(公告)号：US08680118B2

公开(公告)日：2014-03-25

申请号：US13525950

申请日：2012-06-18

Applicant: Donald J. Kyle ,  Qun Sun ,  Laykea Tafesse

Inventor： Donald J. Kyle ,  Qun Sun ,  Laykea Tafesse

IPC: C07D401/04 ,  A61K31/444

CPC classification number: C07D211/78 ,  C07D213/02 ,  C07D401/02 ,  C07D401/04 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

Abstract: A compound of formula: wherein Ar1, Ar2, V, X, R3, R4, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cyclo(hetero)alkenyl Compound”); compositions comprising an effective amount of a Cyclo(hetero)alkenyl Compound; and methods for treating or preventing, e.g., pain, UI, an ulcer, IBD, or IBS in an animal, comprising administering to an animal in need thereof an effective amount of a Cyclo(hetero)alkenyl Compound are disclosed herein.

Abstract translation: 下式的化合物：其中Ar1，Ar2，V，X，R3，R4和m如本文所公开或其药学上可接受的盐（“环（杂）烯基化合物”）; 包含有效量的环（杂）烯基化合物的组合物; 以及用于在动物中治疗或预防例如疼痛，UI，溃疡，IBD或IBS的方法，包括向有需要的动物施用有效量的环（杂）烯基化合物。

公开(公告)号：US20140050749A1

公开(公告)日：2014-02-20

申请号：US13817261

申请日：2011-08-18

Applicant: Donald J. Kyle ,  Daniel A. Soltis ,  Lynda G. Tussey

Inventor： Donald J. Kyle ,  Daniel A. Soltis ,  Lynda G. Tussey

IPC: C07K7/06

CPC classification number: A61K39/0005 ,  A61K39/00 ,  C07K7/06 ,  C07K14/4747 ,  C07K14/4748 ,  C12N9/0077 ,  C12N9/1241 ,  G01N33/505 ,  G01N33/6878 ,  G01N2333/70539 ,  G01N2500/04 ,  G01N2500/10

Abstract: The invention provides for the synthesis of more effective generators of a T-cell immune response by providing peptide derivatives that are MHC class I-restricted antigens. The peptide derivatives of the present invention are prepared or derived from a parent peptide of 8 to 11 amino acid residues in length, wherein the peptide derivative contains a non-natural amino acid substituted in place of a naturally-occurring amino acid residue at one or more primary anchor positions in the parent peptide or at position 6, position 7, or the C-terminus. The exemplary polypeptides are derived from the survivin, hTERT, CYP1B1 and MART-1 antigens.

Abstract translation: 本发明通过提供作为MHC I类限制性抗原的肽衍生物来提供更有效的T细胞免疫应答发生器的合成。 本发明的肽衍生物是长度为8至11个氨基酸残基的母体肽制备或衍生的，其中肽衍生物含有非天然氨基酸代替天然存在的氨基酸残基 在母体肽中或位置6，位置7或C-末端具有更多的主要锚定位置。 示例性多肽衍生自存活蛋白，hTERT，CYP1B1和MART-1抗原。

公开(公告)号：US08227467B2

公开(公告)日：2012-07-24

申请号：US12706571

申请日：2010-02-16

Applicant: Donald J. Kyle ,  Qun Sun ,  Laykea Tafesse

Inventor： Donald J. Kyle ,  Qun Sun ,  Laykea Tafesse

IPC: C07D417/02 ,  A61K31/495

CPC classification number: C07D211/78 ,  C07D213/02 ,  C07D401/02 ,  C07D401/04 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

Abstract: A compound of formula: wherein Ar1, Ar2, V, X, R3, R4, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cyclo(hetero)alkenyl Compound”); compositions comprising an effective amount of a Cyclo(hetero)alkenyl Compound; and methods for treating or preventing, e.g., pain, UI, an ulcer, IBD, or IBS in an animal, comprising administering to an animal in need thereof an effective amount of a Cyclo(hetero)alkenyl Compound are disclosed herein.

Abstract translation: 下式的化合物：其中Ar1，Ar2，V，X，R3，R4和m如本文所公开或其药学上可接受的盐（“环（杂）烯基化合物”）; 包含有效量的环（杂）烯基化合物的组合物; 以及用于在动物中治疗或预防例如疼痛，UI，溃疡，IBD或IBS的方法，包括向有需要的动物施用有效量的环（杂）烯基化合物。

公开(公告)号：US20110136846A1

公开(公告)日：2011-06-09

申请号：US13055873

申请日：2009-07-30

Applicant: Donald J. Kyle ,  R. Richard Goehring ,  Marian E. Fundytus

Inventor： Donald J. Kyle ,  R. Richard Goehring ,  Marian E. Fundytus

IPC: A61K31/485 ,  C07D489/00 ,  A61P25/00

CPC classification number: C07D489/12 ,  C07D489/02

Abstract: The present invention is directed to Buprenorphine Analog compounds of the Formula I, Formula II or Formula III shown below, wherein R1, R2, R8, R3, R3a, R3b, X, Z and Y are as defined herein, R1 H3CO (I) OCH3 OCH3 (III) Compounds of the Invention are useful for treating pain and other conditions modulated by activity of opioid and ORL1 receptors.

Abstract translation: 本发明涉及如下所示的式I，式II或式III的丁丙诺啡类似物，其中R1，R2，R8，R3，R3a，R3b，X，Z和Y如本文所定义，R1H3CO（I） OCH 3 OCH 3（III）本发明化合物可用于治疗由阿片样物质和ORL1受体活性调节的疼痛和其它状况。

公开(公告)号：US20100259286A1

公开(公告)日：2010-10-14

申请号：US12671309

申请日：2008-07-30

Applicant: Camelia Prodan ,  Victor I Ilyin ,  Donald J. Kyle ,  Kevin Carlin ,  Gang Wu

Inventor： Camelia Prodan ,  Victor I Ilyin ,  Donald J. Kyle ,  Kevin Carlin ,  Gang Wu

IPC: G01R27/08 ,  C40B30/06 ,  C40B60/12

CPC classification number: G01N33/6872 ,  G01N33/5008

Abstract: A method for measuring membrane potential using dielectric spectroscopy is described. A new theoretical model allows for the determination of membrane potential from low-frequency impedance measurements to provide a non-evasive method which is both rapid and inexpensive.

Abstract translation: 描述了使用介电光谱测量膜电位的方法。 新的理论模型允许从低频阻抗测量中确定膜电位，以提供快速和便宜的非回避方法。

公开(公告)号：US07696208B2

公开(公告)日：2010-04-13

申请号：US11344937

申请日：2006-01-31

Applicant: Donald J. Kyle ,  Qun Sun

Inventor： Donald J. Kyle ,  Qun Sun

IPC: C07D213/75 ,  A61K31/44 ,  A61K31/496

CPC classification number: C07D401/04 ,  C07D213/74 ,  C07D213/85

Abstract: Compounds of formulae: where X is S or O and Ar2, R1, R2, R3, R8, n, m, and t are disclosed herein, or a pharmaceutically acceptable salt thereof (a “3-substituted Pyridyl Compound”), compositions comprising an effective amount of a 3-substituted Pyridyl Compound, and methods for treating or preventing pain, urinary incontinence, an ulcer, inflammatory-bowel disease, irritable-bowel syndrome, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia or depression in an animal comprising administering to an animal in need thereof an effective amount of a 3-substituted Pyridyl Compound are disclosed herein.

Abstract translation: 式中的化合物：其中X为S或O且Ar 2，R 1，R 2，R 3，R 8，n，m和t在本文中公开，或其药学上可接受的盐（“3-取代的吡啶基化合物”）， 有效量的3-取代的吡啶基化合物，以及治疗或预防疼痛，尿失禁，溃疡，炎性肠病，肠易激综合征，成瘾性疾病，帕金森病，帕金森综合征，焦虑症，癫痫，中风， 包括施用于癫痫发作，瘙痒症状，精神病，认知障碍，记忆缺陷，限制性脑功能，亨廷顿氏舞蹈病，肌萎缩性侧索硬化症，痴呆，视网膜病变，肌肉痉挛，偏头痛，呕吐，运动障碍或抑郁症 有需要的动物本文公开了有效量的3-取代的吡啶基化合物。

公开(公告)号：US07696207B2

公开(公告)日：2010-04-13

申请号：US11893916

申请日：2007-08-17

Applicant: Donald J. Kyle ,  Qun Sun

Inventor： Donald J. Kyle ,  Qun Sun

IPC: C07D403/04 ,  C07D403/14

CPC classification number: C07D237/24

Abstract: A compound of formula: wherein X is S or O and A, R1, R2, R3, R4, n, and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Pyridazinylpiperazine Compound”), compositions comprising a Pyridazinylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD and IBS in an animal comprising administering to an animal in need thereof an effective amount of a Pyridazinylpiperazine Compound are disclosed herein.

Abstract translation: 下式的化合物：其中X为S或O且A，R 1，R 2，R 3，R 4，n和m在本文中公开，或其药学上可接受的盐（“哒嗪基哌嗪化合物”），包含哒嗪基哌嗪化合物， 以及用于在动物中治疗或预防疼痛，UI，溃疡，IBD和IBS的方法，包括向有需要的动物施用有效量的哒嗪基哌嗪化合物。

公开(公告)号：US20100063030A1

公开(公告)日：2010-03-11

申请号：US12595066

申请日：2008-04-08

Applicant: Donald J. Kyle ,  Jiangchao Yao

Inventor： Donald J. Kyle ,  Jiangchao Yao

IPC: A61K31/4468 ,  C07D211/56 ,  C07D207/48 ,  C07D223/04 ,  A61K31/40 ,  A61K31/55 ,  A61P25/00 ,  A61P9/12 ,  A61P25/24 ,  A61P25/22 ,  G01N33/53

CPC classification number: C07D211/96 ,  C07D207/48

Abstract: The invention relates to pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula I: and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1, R2, Z and m are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

Abstract translation: 本发明涉及式I的吡咯烷基，哌啶基和六氢氮杂卟啉化合物及其药学上可接受的盐，前药或溶剂化物，其中R1，R2，Z和m如本说明书所述定义。 本发明还涉及使用式I化合物来治疗对阻断钙通道，特别是N型钙通道有响应的病症。 本发明的化合物特别适用于治疗疼痛。

公开(公告)号：US20090239910A1

公开(公告)日：2009-09-24

申请号：US12225743

申请日：2007-03-29

Applicant: Zhengning Chen ,  Khondaker Islam ,  Bin Shao ,  Jiangchao Yao ,  Xiaoming Zhou ,  Donald J. Kyle

Inventor： Zhengning Chen ,  Khondaker Islam ,  Bin Shao ,  Jiangchao Yao ,  Xiaoming Zhou ,  Donald J. Kyle

IPC: A61K31/445 ,  C07D207/14 ,  C07D211/56 ,  A61K31/40 ,  A61P25/18 ,  A61P25/28 ,  A61P25/08 ,  A61P25/06 ,  A61P25/22 ,  A61P25/24 ,  A61P29/00 ,  A61P9/12 ,  A61P9/06

CPC classification number: C07D211/42 ,  C07D207/14 ,  C07D401/12

Abstract: The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula I and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

Abstract translation: 本发明涉及式I的氮杂环丁烷基，吡咯烷基，哌啶基和六氢氮杂卟啉化合物及其药学上可接受的盐，前药或溶剂合物，其中R1-R3和Z如说明书所述定义。 本发明还涉及使用式I的化合物来治疗，预防或改善对阻断钙通道，特别是N型钙通道有响应的病症。 本发明的化合物特别适用于治疗疼痛。

公开(公告)号：US20080200472A1

公开(公告)日：2008-08-21

申请号：US11893916

申请日：2007-08-17

Applicant: Donald J. Kyle ,  Qun Sun

Inventor： Donald J. Kyle ,  Qun Sun

IPC: A61K31/501 ,  C07D403/04

CPC classification number: C07D237/24

Abstract: A compound of formula: wherein X is S or O and A, R1, R2, R3, R4, n, and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Pyridazinylpiperazine Compound”), compositions comprising a Pyridazinylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD and IBS in an animal comprising administering to an animal in need thereof an effective amount of a Pyridazinylpiperazine Compound are disclosed herein.

Abstract translation: 下式的化合物：其中X是S或O，A，R 1，R 2，R 3，R 4， 本文公开的N，m和/或其药学上可接受的盐（“哒嗪基哌嗪化合物”），包含哒嗪基哌嗪化合物的组合物，以及治疗或预防疼痛，UI，溃疡，IBD和IBS的方法 包括向有需要的动物施用有效量的哒嗪基哌嗪化合物。