公开(公告)号：US20130296281A1

公开(公告)日：2013-11-07

申请号：US13704531

申请日：2011-06-16

Applicant: Donald J. Kyle ,  Chiyou Ni ,  Laykea Tafesse ,  Jiangchao Yao

Inventor： Donald J. Kyle ,  Chiyou Ni ,  Laykea Tafesse ,  Jiangchao Yao

IPC: C07D209/20 ,  C07D209/12 ,  C07D401/12 ,  C07D209/18 ,  C07D231/56 ,  G01N33/50 ,  C07D413/06 ,  C07D209/14 ,  C07D471/04

CPC classification number: C07D209/20 ,  C07B59/002 ,  C07B2200/05 ,  C07D209/12 ,  C07D209/14 ,  C07D209/16 ,  C07D209/18 ,  C07D231/56 ,  C07D401/12 ,  C07D413/06 ,  C07D471/04 ,  G01N33/5008

Abstract: The invention relates to aryl and heteroaryl substituted compounds of Formula (I), and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, R1, and Z1-Z5 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.

Abstract translation: 本发明涉及式（I）的芳基和杂芳基取代的化合物及其药学上可接受的盐，前药或溶剂化物，其中G，R1和Z1-Z5如说明书所述定义。 本发明还涉及式（I）化合物用于治疗对钠通道阻断作出反应的病症。 本发明的化合物特别适用于治疗疼痛。

公开(公告)号：US20110281885A1

公开(公告)日：2011-11-17

申请号：US12879885

申请日：2010-09-10

Applicant: Donald J. Kyle ,  Qun Sun ,  Laykea Tafesse ,  Chongwu Zhang ,  Xiaoming Zhou

Inventor： Donald J. Kyle ,  Qun Sun ,  Laykea Tafesse ,  Chongwu Zhang ,  Xiaoming Zhou

IPC: A61K31/496 ,  A61K31/497 ,  C12N5/07 ,  C07D417/04 ,  C07D401/04 ,  A61P25/00

CPC classification number: C07D213/74 ,  C07D213/85 ,  C07D237/20 ,  C07D239/42 ,  C07D241/20 ,  C07D285/06 ,  C07D333/16

Abstract: A compound of formula: wherein A, Ar, R3, R6, and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Cyanoiminopiperazine Compound”), compositions comprising an effective amount of a Cyanoiminopiperazine 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 Cyanoiminopiperazine Compound are disclosed.

Abstract translation: 本文公开的其中A，Ar，R 3，R 6和m的化合物或其药学上可接受的盐（“氰基亚氨基哌嗪化合物”），包含有效量的氰基亚氨基哌嗪化合物的组合物，以及治疗或预防的方法 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，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，痴呆，视网膜病变，肌肉痉挛，偏头痛，呕吐，运动障碍或抑郁症，包括向有需要的动物施用有效量的氰基亚氨基哌嗪化合物。

公开(公告)号：US09120752B2

公开(公告)日：2015-09-01

申请号：US13810089

申请日：2011-07-15

Applicant: Donald J. Kyle ,  Chiyou Ni ,  Minnie Park ,  Laykea Tafesse

Inventor： Donald J. Kyle ,  Chiyou Ni ,  Minnie Park ,  Laykea Tafesse

IPC: C07D213/79 ,  C07D213/81 ,  C07D401/12 ,  C07D413/12 ,  C07B59/00 ,  C07D413/14

CPC classification number: C07D213/79 ,  C07B59/002 ,  C07D213/56 ,  C07D213/81 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14

Abstract: The invention relates to substituted pyridine compounds of Formula I: (I) or a pharmaceutically acceptable salt, prodrug, or solvate thereof wherein A1, X, A2, R1a, R1b, R1c, G, and z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.

Abstract translation: 本发明涉及式I的取代的吡啶化合物：（I）或其药学上可接受的盐，前药或溶剂化物，其中A1，X，A2，R1a，R1b，R1c，G和z定义如说明书 。 本发明还涉及式I化合物用于治疗对钠通道阻断有反应的病症。 本发明的化合物特别适用于治疗疼痛。

公开(公告)号：US08703962B2

公开(公告)日：2014-04-22

申请号：US12603684

申请日：2009-10-22

Applicant: Donald J. Kyle ,  Laykea Tafesse

Inventor： Donald J. Kyle ,  Laykea Tafesse

IPC: C07D277/62 ,  C07D277/64 ,  C07D277/82 ,  A61K31/425

CPC classification number: C07D213/61 ,  C07D213/82

Abstract: The invention relates to compounds of formula I and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof.

Abstract translation: 本发明涉及式I化合物及其药学上可接受的衍生物，包含有效量的式I化合物或其药学上可接受的衍生物的组合物，以及用于治疗或预防诸如疼痛，UI，溃疡，IBD的病症的方法 和IBS，包括向有需要的动物施用有效量的式I化合物或其药学上可接受的衍生物。

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：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：US07279493B2

公开(公告)日：2007-10-09

申请号：US10607563

申请日：2003-06-27

Applicant: Donald J. Kyle ,  Qun Sun ,  Laykea Tafesse ,  Chongwu Zhang ,  Xiaoming Zhou

Inventor： Donald J. Kyle ,  Qun Sun ,  Laykea Tafesse ,  Chongwu Zhang ,  Xiaoming Zhou

IPC: C07D277/04 ,  A61K43/80

CPC classification number: C07D213/74 ,  C07D213/85 ,  C07D237/20 ,  C07D239/42 ,  C07D241/20 ,  C07D285/06 ,  C07D333/16

Abstract: A compound of formula: wherein A, Ar, R3, R6, and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Cyanoiminopiperazine Compound”), compositions comprising an effective amount of a Cyanoiminopiperazine 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 Cyanoiminopiperazine Compound are disclosed.

Abstract translation: 式中的化合物：其中A，Ar，R 3，R 6和m在本文中公开，或其药学上可接受的盐（“氰基亚氨基哌嗪化合物”）， 包含有效量的氰基亚氨基哌嗪化合物的组合物，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， 包括给予一个或多个癫痫发作，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，痴呆，视网膜病变，肌肉痉挛，偏头痛，呕吐，运动障碍或抑郁症 公开了有效量的氰酰亚胺哌嗪化合物的需要动物。

公开(公告)号：US09221831B2

公开(公告)日：2015-12-29

申请号：US13825241

申请日：2011-09-20

Applicant: Donald J. Kyle ,  Laykea Tafesse

Inventor： Donald J. Kyle ,  Laykea Tafesse

IPC: A61K31/485 ,  C07D489/12

CPC classification number: C07D489/12

Abstract: The present invention is directed to Buprenorphine Analog compounds of the Formula (I), Formula (IA) or Formula (IB) shown below, wherein R1, R2, R8, R3a, R 3b, G, X, Z and Y are as defined herein. Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.

Abstract translation: 本发明涉及如下所示的式（I），式（IA）或式（IB）的丁丙诺啡类似物化合物，其中R 1，R 2，R 8，R 3a，R 3b，G，X，Z和Y如所定义 这里。 本发明的化合物可用于治疗由阿片样物质和ORL-1受体的活性调节的疼痛，便秘和其它状况。

公开(公告)号：US07799786B2

公开(公告)日：2010-09-21

申请号：US11899379

申请日：2007-09-04

Applicant: Donald J. Kyle ,  Qun Sun ,  Laykea Tafesse ,  Chongwu Zhang ,  Xiaoming Zhou

Inventor： Donald J. Kyle ,  Qun Sun ,  Laykea Tafesse ,  Chongwu Zhang ,  Xiaoming Zhou

IPC: C07D237/00 ,  C07D241/00 ,  A61K31/50 ,  A61K31/497

CPC classification number: C07D213/74 ,  C07D213/85 ,  C07D237/20 ,  C07D239/42 ,  C07D241/20 ,  C07D285/06 ,  C07D333/16

Abstract: A compound of formula: wherein A, Ar, R3, R6, and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Cyanoiminopiperazine Compound”), compositions comprising an effective amount of a Cyanoiminopiperazine 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 Cyanoiminopiperazine Compound are disclosed.

Abstract translation: 本文公开的其中A，Ar，R 3，R 6和m的化合物或其药学上可接受的盐（“氰基亚氨基哌嗪化合物”），包含有效量的氰基亚氨基哌嗪化合物的组合物，以及治疗或预防的方法 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，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，痴呆，视网膜病变，肌肉痉挛，偏头痛，呕吐，运动障碍或抑郁症，包括向有需要的动物施用有效量的氰基亚氨基哌嗪化合物。

公开(公告)号：US07683063B2

公开(公告)日：2010-03-23

申请号：US10867546

申请日：2004-06-14

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。