公开(公告)号：US20170224716A1

公开(公告)日：2017-08-10

申请号：US15376281

申请日：2016-12-12

Applicant: Academia Sinica

Inventor： Chih-Cheng Chen ,  Yun-Lian Lin ,  Jim-Min Fang ,  Yijuang Chern ,  Chia-Ching John Lin ,  Wei-Nan Chen ,  Chun-Jung Lin

IPC: A61K31/7076 ,  A61K45/06 ,  A61K36/8988

CPC classification number: A61K31/7076 ,  A61K36/8988 ,  A61K45/06 ,  A61K2300/00

Abstract: The invention provides a new use of adenosine analogs for the treatment of pain through activation of neurokinin 1 (NK1) receptor signaling pathway, thereby inducing the activation of activation of M-type potassium channel to induce outward currents. A method and pharmaceutical composition for treating pain comprising an adenonsine analog that activates NK1 receptor signaling, thereby inducing outward current are also provided.

公开(公告)号：US12129273B2

公开(公告)日：2024-10-29

申请号：US18227782

申请日：2023-07-28

Applicant: Academia Sinica

Inventor： Chih-Cheng Chen ,  Jim-Min Fang ,  Cheng-Han Lee ,  Jen-Yao Chang

IPC: C07H19/16 ,  A61K31/7076 ,  A61K38/04 ,  A61K47/55 ,  A61P29/00

CPC classification number: C07H19/16 ,  A61K31/7076 ,  A61K38/046 ,  A61K47/55 ,  A61P29/00

Abstract: Compounds for use in prevention and/or treatment of pain are disclosed. The compounds are derived by conjugation of N6-(4-hydroxybenzyl)adenosine and analogous compounds with amino acids or peptides. In one embodiment of the invention, the compound is 5′-glycylcarbonyl-N6-(4-hydroxybenzyl)adenosine (I-a1). In another embodiment of the invention, the compound is 5′-deoxy-5′-(N′-glycylureido)-N6-(4-hydroxybenzyl)adenosine (I-d1). Also disclosed are methods of making and using the same.

公开(公告)号：US11753432B2

公开(公告)日：2023-09-12

申请号：US16481042

申请日：2018-01-26

Applicant: Academia Sinica

Inventor： Chih-Cheng Chen ,  Jim-Min Fang ,  Cheng-Han Lee ,  Jen-Yao Chang

IPC: C07H19/16 ,  A61K47/55 ,  A61P29/00 ,  A61K31/7076 ,  A61K38/04

CPC classification number: C07H19/16 ,  A61K31/7076 ,  A61K38/046 ,  A61K47/55 ,  A61P29/00

Abstract: Compounds for use in prevention and/or treatment of pain are disclosed. The compounds are derived by conjugation of N6-(4-hydroxybenzyl)adenosine and analogous compounds with amino acids or peptides. In one embodiment of the invention, the compound is 5′-O-(glycine-N-carbonyl-N6-(4-hydroxybenzyl)adenosine (I-a1). In another embodiment of the invention, the compound is 5-deoxy-5′-(glycine-N-amido)-N6-(4-hydroxybenzyl)adenosine (I-d1). Also disclosed are methods of making and using the same.

公开(公告)号：US20150038445A1

公开(公告)日：2015-02-05

申请号：US14378013

申请日：2013-02-11

Applicant: Academia Sinica

Inventor： Chih-Cheng Chen ,  Yun-Lian Lin ,  Jim-Min Fang ,  Yijuang Chern ,  Chia-Ching John Lin ,  Wei-Nan Chen ,  Chun-Jung Lin

IPC: A61K31/7076 ,  A61K36/8988

CPC classification number: A61K31/7076 ,  A61K36/8988 ,  A61K45/06 ,  A61K2300/00

Abstract: The disclosure provides a new use of adenosine analogs for the treatment of pain through activation of neurokinin 1 (NK1) receptor signaling pathway, thereby inducing the activation of M-type potassium channel to induce outward currents. A method and pharmaceutical composition for treating pain comprising an adenonsine analog that activates NK1 receptor signaling, thereby inducing outward current are also provided.

Abstract translation: 本公开提供了腺苷类似物用于通过激活神经激肽1（NK1）受体信号传导途径治疗疼痛的新用途，从而诱导M型钾通道的活化以诱导外向电流。 还提供了一种用于治疗疼痛的方法和药物组合物，其包含激活NK1受体信号传导的腺苷类似物，从而诱导外向电流。

公开(公告)号：US10117890B2

公开(公告)日：2018-11-06

申请号：US15376281

申请日：2016-12-12

Applicant: Academia Sinica

Inventor： Chih-Cheng Chen ,  Yun-Lian Lin ,  Jim-Min Fang ,  Yijuang Chern ,  Chia-Ching John Lin ,  Wei-Nan Chen ,  Chun-Jung Lin

IPC: A01N43/04 ,  A61K31/70 ,  A61K31/7076 ,  A61K36/8988 ,  A61K45/06

Abstract: Methods for treating pain such as fibromyalgia, comprising administering to a subject in need thereof an effective amount of an adenosine analog, wherein the adenosine analog may be a compound of Formula (I): (I), or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions comprising the adenosine analog for use in treating pain (e.g., fibromyalgia), optionally further comprising Substance P (SP), are also provided.

公开(公告)号：US10301348B2

公开(公告)日：2019-05-28

申请号：US15031711

申请日：2014-10-22

Applicant: Academia Sinica

Inventor： Jim-Min Fang ,  Yun-Lian Lin ,  Jung-Hsin Lin ,  Chun-Jung Lin ,  Yijuang Chern ,  Nai-Kuei Huang ,  Hung-Li Wang ,  Benjamin Pang-hsien Tu ,  Chih-Cheng Chen

IPC: C07H19/167 ,  C07H19/16 ,  C07D473/34 ,  A61K31/7076

Abstract: Compounds for use in prevention and treatment of neurodegenerative disease and pain are disclosed. In one embodiment of the invention, the compound is selected from the group consisting of N6-[(3-halothien-2-yl)methyl]adenosine, N6-[(4-halothien-2-yl)methyl]adenosine, and N6-[(5-halothien-2-yl)methyl]adenosine. In another embodiment of the invention, the compound is selected from the group consisting of N6-[(2-bromothien-3-yl)methyl]adenosine, N6-[(4-bromothien-3-yl)methyl]adenosine, N6-[(5-bromothien-3-yl)methyl]adenosine N6-[(2-chlorothien-3-yl)methyl]adenosine, N6-[(4-chlorothien-3-yl)methyl]adenosine, and N6-[(5-chlorothien-3-yl)methyl]adenosine. Also disclosed are methods of making and using the same.

公开(公告)号：US20160264613A1

公开(公告)日：2016-09-15

申请号：US15031711

申请日：2014-10-22

Applicant: Academia Sinica

Inventor： Jim-Min Fang ,  Yun-Lian LIn ,  Jung-Hsin Lin ,  Chun-Jung Lin ,  Yijuang Chem ,  Nai-Kuei Huang ,  Hung-Li Wang ,  Benjamin Pang-hsien Tu ,  Chih-Cheng Chen

IPC: C07H19/16

CPC classification number: C07H19/16 ,  A61K31/7076 ,  C07D473/34 ,  C07H19/167 ,  Y02P20/582

Abstract: Compounds for use in prevention and treatment of neurodegenerative disease and pain are disclosed. In one embodiment of the invention, the compound is selected from the group consisting of N6-[(3-halothien-2-yl)methyl]adenosine, N6-[(4-halothien-2-yl)methyl]adenosine, and N6-[(5-halothien-2-yl)methyl]adenosine. In another embodiment of the invention, the compound is selected from the group consisting of N6-[(2-bromothien-3-yl)methyl]adenosine, N6-[(4-bromothien-3-yl)methyl]adenosine, N6-[(5-bromothien-3-yl)methyl]adenosine N6-[(2-chlorothien-3-yl)methyl]adenosine, N6-[(4-chlorothien-3-yl)methyl]adenosine, and N6-[(5-chlorothien-3-yl)methyl]adenosine. Also disclosed are methods of making and using the same.

Abstract translation: 公开了用于预防和治疗神经变性疾病和疼痛的化合物。 在本发明的一个实施方案中，该化合物选自N6 - [（3-卤代噻吩-2-基）甲基]腺苷，N6 - [（4-卤代噻吩-2-基）甲基]腺苷和N6 - [（5-卤代噻吩-2-基）甲基]腺苷。 在本发明的另一个实施方案中，该化合物选自N6 - [（2-溴噻吩-3-基）甲基]腺苷，N6 - [（4-溴噻吩-3-基）甲基]腺苷，N6- [（5-溴噻吩-3-基）甲基]腺苷N6 - [（2-氯噻吩-3-基）甲基]腺苷，N6 - [（4-氯噻吩-3-基）甲基]腺苷和N6 - [ 5-氯噻吩-3-基）甲基]腺苷。 还公开了制造和使用它们的方法。