公开(公告)号：US06864261B2

公开(公告)日：2005-03-08

申请号：US10429078

申请日：2003-05-02

Applicant: Parviz Gharagozloo ,  Khondaker Islam ,  Donald J. Kyle ,  Qun Sun ,  Laykea Tafesse ,  John William Frank Whitehead ,  Ji Yang ,  Xiaoming Zhou

Inventor： Parviz Gharagozloo ,  Khondaker Islam ,  Donald J. Kyle ,  Qun Sun ,  Laykea Tafesse ,  John William Frank Whitehead ,  Ji Yang ,  Xiaoming Zhou

IPC: A61P25/00 ,  A61P29/00 ,  C07D213/74 ,  C07D213/80 ,  C07D213/85 ,  C07D401/04 ,  C07D401/14 ,  C07D405/12 ,  A61K31/496

CPC classification number: C07D213/74 ,  C07D213/80 ,  C07D213/85 ,  C07D401/04 ,  C07D401/14 ,  C07D405/12

Abstract: A compound of formula (wherein A, R1, R2, R6, m and n are disclosed herein) or a pharmaceutically acceptable salt thereof (a “Piperazine Compound”); pharmaceutical compositions comprising a Piperazine Compound; and methods for treating pain, urinary incontinence (UI), 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 (ALS), dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia and depression in an animal comprising administering to an animal in need thereof an effective amount of a Piperazine Compound are disclosed.

Abstract translation: 式（其中A，R 1，R 2，R 6，m和n在本文中公开）的化合物或其药学上可接受的盐（“哌嗪化合物”）; 包含哌嗪化合物的药物组合物; 和治疗疼痛，尿失禁（UI），成瘾性障碍，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，亨廷顿氏舞蹈症 ，肌萎缩性侧索硬化（ALS），痴呆，视网膜病变，肌肉痉挛，偏头痛，呕吐，运动障碍和抑郁症，包括向有需要的动物施用有效量的哌嗪化合物。

公开(公告)号：US20140057931A1

公开(公告)日：2014-02-27

申请号：US13825241

申请日：2011-09-20

Applicant: Donald J. Kyle ,  Laykea Tafesse

Inventor： Donald J. Kyle ,  Laykea Tafesse

IPC: 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：US08546388B2

公开(公告)日：2013-10-01

申请号：US12603733

申请日：2009-10-22

Applicant: Donald J. Kyle ,  Laykea Tafesse

Inventor： Donald J. Kyle ,  Laykea Tafesse

IPC: A61K31/535

CPC classification number: C07D401/04 ,  A61K31/4436 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  C07D401/14 ,  C07D409/04 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07F9/65583

Abstract: The invention relates to compounds of formulae I(a)-I(d): and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formulae I(a)-I(d) 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 formulae I(a)-I(d) or a pharmaceutically acceptable derivative thereof.

Abstract translation: 本发明涉及式I（a）-I（d）的化合物及其药学上可接受的衍生物：包含有效量的式I（a）-I（d）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和IBS的病症的方法，包括向有需要的动物施用有效量的式I（a）-I（d）化合物或其药学上可接受的衍生物 其中。

公开(公告)号：US20130012541A1

公开(公告)日：2013-01-10

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: A61K31/444 ,  A61P25/00 ,  A61K31/4545 ,  C07D401/04 ,  C07D401/14

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：US20080153835A1

公开(公告)日：2008-06-26

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: A61K31/501 ,  C07D401/04 ,  A61K31/497 ,  A61P25/04

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：US09212139B2

公开(公告)日：2015-12-15

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: C07D209/12 ,  C07D209/20 ,  C07D209/16 ,  C07D231/56 ,  C07D471/04 ,  C07D209/14 ,  C07D209/18 ,  C07D401/12 ,  C07D413/06 ,  G01N33/50

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：US20130345211A1

公开(公告)日：2013-12-26

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 ,  C07B59/00 ,  C07D213/81 ,  C07D413/12 ,  C07D413/14 ,  C07D401/12

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：US20110152324A1

公开(公告)日：2011-06-23

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: A61K31/444 ,  C07D401/14 ,  C07D211/68 ,  C07D401/04 ,  A61P29/00

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：US09656959B2

公开(公告)日：2017-05-23

申请号：US13996082

申请日：2011-12-21

Applicant: Chiyou Ni ,  Minnie Park ,  Bin Shao ,  Laykea Tafesse ,  Jiangchao Yao ,  Mark A. Youngman ,  Xiaoming Zhou

Inventor： Chiyou Ni ,  Minnie Park ,  Bin Shao ,  Laykea Tafesse ,  Jiangchao Yao ,  Mark A. Youngman ,  Xiaoming Zhou

IPC: C07D213/75 ,  C07D401/02 ,  C07D401/12 ,  C07D401/14 ,  C07D213/76 ,  C07D213/81 ,  C07D413/12

CPC classification number: C07D213/75 ,  C07D213/76 ,  C07D213/81 ,  C07D401/02 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12

Abstract: The invention relates to substituted pyridine compounds of Formula I: (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1a, R1b, R2a, R2b, R2c, A1, A2, and X 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.

公开(公告)号：US09598447B2

公开(公告)日：2017-03-21

申请号：US13996440

申请日：2011-12-21

Applicant: Dawit Tadesse ,  Laykea Tafesse ,  Xiaoming Zhou

Inventor： Dawit Tadesse ,  Laykea Tafesse ,  Xiaoming Zhou

IPC: C07F9/6561 ,  C07F9/6558

CPC classification number: C07F9/6561 ,  C07F9/65583

Abstract: The disclosure relates to Phosphorus-Substituted Quinoxaline-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable derivatives thereof wherein the dashed line, A, B, Q, R1, R2, R3, R4, Y1, Z, and a are as defined herein, compositions comprising an effective amount of a Phosphorus-Substituted Quinoxaline-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Phosphorus-Substituted Quinoxaline-Type Piperidine Compound.