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.

公开(公告)号：US20150315201A1

公开(公告)日：2015-11-05

申请号：US14654727

申请日：2013-12-23

Applicant: Laykea TAFESSE

Inventor： Laykea Tafesse

IPC: C07D487/08

CPC classification number: C07D487/08 ,  C07D471/08

Abstract: The disclosure relates to indole-type piperidine compounds, indoline-type piperidine compounds and related piperidine-type bicyclic compounds containing a five-membered nitrogen-containing ring (e.g., pyrrole or dihydropyrrole) fused to a heteroaryl ring, compositions comprising an effective amount of such compounds, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of an indole-type piperidine compound, indoline-type piperidine compound or related piperidine-type bicyclic compound containing a five-membered nitrogen-containing ring (e.g., pyrrole or dihydropyrrole) fused to a heteroaryl ring.

Abstract translation: 本公开内容涉及吲哚型哌啶化合物，二氢吲哚型哌啶化合物和含有与杂芳基环稠合的五元含氮环（例如吡咯或二氢吡咯）的相关哌啶型双环化合物，其包含有效量的 这些化合物以及治疗或预防诸如疼痛的病症的方法，包括向有需要的动物施用有效量的吲哚型哌啶化合物，二氢吲哚型哌啶化合物或相关的哌啶型双环化合物，其含有五 （例如，吡咯或二氢吡咯）与杂芳基环稠合。

公开(公告)号：US20140135351A1

公开(公告)日：2014-05-15

申请号：US14075176

申请日：2013-11-08

Applicant: Jeffrey LOCKMAN ,  Laykea TAFESSE ,  Jiangchao YAO ,  Jianming YU

Inventor： Jeffrey LOCKMAN ,  Laykea TAFESSE ,  Jiangchao YAO ,  Jianming YU

IPC: C07D221/26 ,  C07D417/12 ,  C07D401/04 ,  C07D409/12 ,  C07D405/12 ,  C07D401/12

CPC classification number: C07D221/26 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

Abstract: The present invention is directed to Benzomorphan Analog compounds of the Formula I″, Formula IA″, Formula IB″, Formula IC″, or Formula ID″ as shown below; and related Formula I′, Formula IA′, Formula IB′, Formula IC′, or Formula ID′; Formula I, Formula IA, Formula IB, Formula IC, or Formula ID; wherein R1, R2a, R2b, R3 and R4 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”，式IB“，式IC”或式ID“的苯并咪唑类似物化合物。 和式I'，式IA'，式IB'，式IC'或式ID'; 式I，式IA，式IB，式IC或式ID; 其中R1，R2a，R2b，R3和R4如本文所定义。 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：US20130303526A1

公开(公告)日：2013-11-14

申请号：US13821732

申请日：2011-09-16

Applicant: Chiyou NI ,  Bin Shao ,  Laykea Tafesse ,  Jiangchao Yao ,  Jianming Yu ,  Xiaoming Zhou

Inventor： Chiyou NI ,  Bin Shao ,  Laykea Tafesse ,  Jiangchao Yao ,  Jianming Yu ,  Xiaoming Zhou

IPC: C07D213/30 ,  C07D213/81 ,  C07D213/58 ,  C07D213/643 ,  C07D401/12 ,  C07D401/04 ,  C07D401/14

CPC classification number: C07D213/81 ,  C07D213/30 ,  C07D213/46 ,  C07D213/50 ,  C07D213/57 ,  C07D213/58 ,  C07D213/643 ,  C07D213/65 ,  C07D213/74 ,  C07D213/79 ,  C07D213/84 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14

Abstract: The invention relates to substituted pyridine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1a, A1, A2, E, G, Z1, and Z2 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）的取代吡啶化合物及其药学上可接受的盐，前体药物和溶剂合物，其中R1a，A1，A2，E，G，Z1和Z2如本说明书所述定义。 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：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：US08546417B2

公开(公告)日：2013-10-01

申请号：US13486267

申请日：2012-06-01

Applicant: Zhengming Chen ,  Laykea Tafesse

Inventor： Zhengming Chen ,  Laykea Tafesse

IPC: A61K31/438 ,  A61K51/04 ,  C07D471/10

CPC classification number: C07D491/107 ,  C07D221/20 ,  C07D471/10 ,  G01N33/566

Abstract: The invention relates to fused and spirocycle compounds of Formula I: or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R1, R2, Q1-Q3, 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, 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的稠合和螺环化合物：或其药学上可接受的盐，前药或溶剂化物，其中R1，R2，Q1-Q3和Z如本说明书所述定义。 本发明还涉及式I化合物用于治疗，预防或改善对阻塞钙通道，特别是N型钙通道有响应的病症的用途。 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：US20080319020A1

公开(公告)日：2008-12-25

申请号：US12094556

申请日：2006-11-21

Applicant: Laykea Tafesse

Inventor： Laykea Tafesse

IPC: A61K31/454 ,  A61P25/00 ,  C07D413/04

CPC classification number: C07D413/04 ,  C07D413/14

Abstract: 4-Oxadiazolyl-piperidine compounds of formula (I) and (II), their compositions and use for the treatment of pain and diarrhoea.

Abstract translation: 式（I）和（II）的4-恶二唑基 - 哌啶化合物，其组合物和用于治疗疼痛和腹泻的用途。

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。