Abstract:
본 발명은 신규한 아미드 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 포함하는 통증의 예방 또는 치료용 약학적 조성물에 관한 것으로써, 본 발명에 따른 신규한 아미드 유도체 또는 이의 약학적으로 허용가능한 염은 나트륨 채널 활성을 억제하고, 말초 신경 손상, 중추 신경 손상뿐만 아니라, 염증으로 유발된 통증을 억제하는 효과가 있으며, 척수 손상 후 활성화되는 MMP-2 및 MMP-9를 억제하는 효과가 우수하므로 신경병증성 통증 예방 또는 치료용 약학적 조성물로 유용하게 사용될 수 있다.
Abstract:
This invention relates to a composition for relieving pain, comprising the compounds of formula (I) or pharmaceutically acceptable salts thereof as an effective substance. The composition of the present invention relieves pain, particularly neuropathic pain and inflammatory pain, and so is useful for preventing or treating pain not controlled by previous analgesics.
Abstract:
Non-peptide compounds are provided to inhibit activity of bradykinin, chronic neuropathic pain and inflammatory pain, so that they are useful for prevention and treatment of disease caused by bradykinin such as pain. The non-peptide compounds represented by the formula(1) or pharmaceutically acceptable salts thereof are provided, wherein R1 and R2 are each independently hydrogen; C1-C4 alkyl; C1-C4 alkoxy; C3-C10 cycloalkyl; C6-C20 aryl and C5-C20 heteroaryl which are optionally substituted by at least one substituent selected from group consisting of C1-C4 alkyl, C1-C4 alkoxy or halogen; C1-C4 alkyl substituted by C6-C20 aryl which is optionally substituted by at least one substituent selected from group consisting of C1-C4 alkyl, C1-C4 alkoxy or halogen; and C1-C4 alkyl substituted by C5-C20 hetero aryl which is optionally substituted by at least one substituent selected from group consisting of C1-C4 alkyl, C1-C4 alkoxy or halogen; X is C1-C4 alkylenyl optionally substituted by C1-C4 alkyl, C1-C4 alkoxy or halogen; C2-C6 alkenylenyl optionally substituted by C1-C4 alkyl, C1-C4 alkoxy or halogen, -CH2YCH2- or -CH2CH2Y-; Y is O, S or NR3; R3 is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, halogen or -COO-C1-C4 alkyl; Z and Z' are each independently hydrogen, hydroxy or halogen; and n is an integer from 1 to 3.
Abstract:
A compound is provided to suppress effectively chronic neuropathic pain and inflammatory pain by suppressing T-type calcium channel activity. A compound is indicated as a chemical formula 1. In the chemical formula 1: R1 is hydrogen; cycloalkyl of CH2-C3~C10; benzyl substituted or non-substituted to one or more radicals selected from a group consisting of linear or branched alkyl of C1~C10, alkoxy of C1~C4, halogen, nitro and N(CH3)2. In the chemical formula 1: R2 is NR5R6; R3 and R4 are aryl of C6~C20 or aryl of C6~C20 substituted to halogen; R5 and R6 are hydrogen, p- tolyloxy or C6~C20 of aryl; n is integer of 1 to 5.
Abstract:
본 발명은 신규한 비펩타이드성 화합물, 이의 제조방법 및 이를 포함하는 약학 조성물에 관한 것이다. 본 발명의 비펩타이드성 화합물은 브라디키닌 활성 억제효과가 우수하고, 만성 신경병증성 통증 및 염증성 통증의 억제효과가 우수하므로, 브라디키닌에 의해 유발되는 질환, 특히 통증의 예방 또는 치료에 유용하게 사용될 수 있다.
Abstract:
A composition for relieving pain is provided to relieve pain, particularly neuropathic pain and inflammatory pain and be useful for preventing or treating pain not controlled by previous analgesics. A composition for relieving pain such as neuropathic pain comprises a compound represented by a formula(1) or a pharmaceutically acceptable salt thereof as an effective ingredient, wherein R^1 is isopropyl, benzyl, 4-methylbenzyl, 4-methoxybenzyl, l-methyl-3-phenyl propyl, 3,4,5-trimethoxybenzyl, 2-(4-(4-chlorophenyl)thiazole), 3-(5-t-butylisoxazole), 2-(4-(4-bromophenyl)thiazole), cyclohexyl, 5-(3-methylisoxazole) or 3,4-dibenzyloxypenethyl; R^2 is H or R^3CO; and R^3 is methyl, phenyl, benzyl, naphthyl(C10H7) or C10H7CH2. A method for relieving pain comprises a step of administering the compound of the formula(I) or the pharmaceutically acceptable salt thereof to a subject.
Abstract translation:提供减轻疼痛的组合物以减轻疼痛,特别是神经性疼痛和炎症性疼痛,并且可用于预防或治疗以前的镇痛药不能控制的疼痛。 用于缓解疼痛的组合物,例如神经性疼痛包括由式(1)表示的化合物或其药学上可接受的盐作为有效成分,其中R 1是异丙基,苄基,4-甲基苄基,4-甲氧基苄基,1-甲基 (4-(4-氯苯基)噻唑),3-(5-叔丁基异恶唑),2-(4-(4-溴苯基)噻唑), 环己基,5-(3-甲基异恶唑)或3,4-二苄氧基乙基乙基; R 2是H或R 3,3CO; R 3是甲基,苯基,苄基,萘基(C 10 H 7)或C 10 H 7 CH 2。 减轻疼痛的方法包括向受试者施用式(I)化合物或其药学上可接受的盐的步骤。