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1. WO2022002225 - INDOLE DERIVATIVE AND APPLICATION THEREOF

Publication Number WO/2022/002225
Publication Date 06.01.2022
International Application No. PCT/CN2021/104138
International Filing Date 02.07.2021
IPC
C07D 209/12 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
04Indoles; Hydrogenated indoles
10with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
12Radicals substituted by oxygen atoms
A61K 31/405 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403condensed with carbocyclic rings, e.g. carbazole
404Indoles, e.g. pindolol
405Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
A61P 25/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
A61P 17/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
A61P 21/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
21Drugs for disorders of the muscular or neuromuscular system
A61P 37/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
Applicants
  • 上海美迪西生物医药股份有限公司 SHANGHAI MEDICILON INC. [CN]/[CN]
Inventors
  • 任峰 REN, Feng
  • 吕裕斌 LV, Yubin
  • 王海龙 WANG, Hailong
  • 任月英 REN, Yueying
  • 陈春麟 CHEN, Chunlin
  • 罗阳春 LUO, Yangchun
  • 蔡金娜 CAI, Jinna
  • 李邦良 LI, Bangliang
Agents
  • 上海瀚桥专利代理事务所(普通合伙) HANQIAO PATENT
Priority Data
202010638390.003.07.2020CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) INDOLE DERIVATIVE AND APPLICATION THEREOF
(FR) DÉRIVÉ D'INDOLE ET SON APPLICATION
(ZH) 一种吲哚衍生物及其应用
Abstract
(EN) Provided are an indole derivative as shown in general formula (I-1) and use thereof in preparing a drug used for preventing and/or treating indications for disorders related to an S1P receptor. The indole derivative is respectively substituted by R1, R2, R5, and R6 at different sites. The modified indole derivative has an excellent biological activity, and is an ideal high efficiency S1P receptor regulator. A compound of general formula (I-1) can be used for treating and/or preventing multiple autoimmune and inflammatory diseases such as Crohn's disease, ulcerative colitis, psoriasis, rheumatoid arthritis, multiple sclerosis, atopic dermatitis, eosinophilic esophagitis, alopecia areata, primary cholangitis, pyoderma gangrenosum, graft-versus-host disease, amyotrophic lateral sclerosis, systemic lupus erythematosus, type I diabetes arteriosclerosis, atherosclerosis, scleroderma, autoimmune hepatitis, acne, microbial infection, and viral infection.
(FR) L'invention concerne un dérivé d'indole tel que représenté par la formule générale (I-1) et son utilisation dans la préparation d'un médicament utilisé pour des indications de prévention et/ou de traitement pour des troubles associés à un récepteur de la S1P. Le dérivé d'indole est respectivement substitué par R1, R2, R5 et R6 en différents sites. Le dérivé d'indole modifié a une excellente activité biologique et est un régulateur du récepteur de la S1P à haute efficacité idéal. Un composé de formule générale (I-1) peut être utilisé pour le traitement et/ou la prévention de multiples maladies auto-immunes et inflammatoires telles que la maladie de Crohn, la recto-colite ulcéro-hémorragique, le psoriasis, la polyarthrite rhumatoïde, la sclérose en plaques, la dermatite atopique, l'œsophagite à éosinophiles, l'alopécie en aires, une angiocholite primitive, la pyodermie gangréneuse, la maladie du greffon contre l'hôte, la sclérose latérale amyotrophique, le lupus érythémateux disséminé, l'artériosclérose du diabète de type I, l'athérosclérose, la sclérodermie, l'hépatite auto-immune, l'acné, une infection microbienne et une infection virale.
(ZH) 提供一种通式(I-1)所示的吲哚衍生物及其在制备预防和/或治疗与S1P受体相关障碍的适应症的药物中的用途。所述吲哚衍生物在不同位点分别被R 1、R 2、R 5和R 6取代,修饰后的吲哚衍生物具有优异的生物活性,是理想的高效S1P受体调节剂。通式(I-1)化合物可用于治疗和/或预防克罗恩病、溃疡性结肠炎、银屑病、类风湿性关节炎、多发性硬化症、特应性皮炎、嗜酸细胞性食管炎、斑秃、原发性胆管炎、坏疽性脓皮症、移植物抗宿主病、肌肉萎缩性侧索硬化症、系统性红斑狼疮、I型糖尿病动脉硬化、动脉粥样硬化、硬皮病、自身免疫性肝炎、痤疮、微生物感染和病毒感染等多种自身免疫和炎性疾病。
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