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1. WO2022001784 - APPLICATION OF GLUTAMINASE INHIBITOR IN PREPARATION OF DRUG FOR TREATING PSORIASIS

Publication Number WO/2022/001784
Publication Date 06.01.2022
International Application No. PCT/CN2021/101850
International Filing Date 23.06.2021
IPC
A61K 31/42 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
42Oxazoles
A61K 31/501 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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
50Pyridazines; Hydrogenated pyridazines
501not condensed and containing further heterocyclic rings
A61K 31/473 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
435having six-membered rings with one nitrogen as the only ring hetero atom
47Quinolines; Isoquinolines
473ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
A61K 31/433 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
433Thiadiazoles
A61K 45/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
A61P 17/06 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
06Antipsoriatics
CPC
A61K 31/42
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
42Oxazoles
A61K 31/433
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
433Thidiazoles
A61K 31/473
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
435having six-membered rings with one nitrogen as the only ring hetero atom
47Quinolines; Isoquinolines
473ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
A61K 31/501
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
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
50Pyridazines; Hydrogenated pyridazines
501not condensed and containing further heterocyclic rings
A61K 45/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
A61P 17/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
06Antipsoriatics
Applicants
  • 广东省中医院 GUANGDONG PROVINCIAL HOSPITAL OF TCM [CN]/[CN]
  • 广州中医药大学第二附属医院 THE SECOND AFFILIATED HOSPITAL OF GUANGZHOU UNIVERSITY OF CHINESE MEDICINE [CN]/[CN]
  • 广州中医药大学第二临床医学院 THE SECOND CLINICAL COLLEGE OF GUANGZHOU UNIVERSITY OF CHINESE MEDICINE [CN]/[CN]
  • 广东省中医药科学院 GUANGDONG PROVINCIAL ACADEMY OF CHINESE MEDICAL SCIENCES [CN]/[CN]
Inventors
  • 卢传坚 LU, Chuanjian
  • 徐永跃 XU, Yongyue
  • 王茂杰 WANG, Maojie
  • 黄闰月 HUANG, Runyue
  • 包德威·伯格林 BOUDEWIJN, Burgering
  • 焦琳 JIAO, Lin
Agents
  • 北京商专润文专利代理事务所(普通合伙) RUNWEN PATENT LAW FIRM
Priority Data
202010618683.230.06.2020CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) APPLICATION OF GLUTAMINASE INHIBITOR IN PREPARATION OF DRUG FOR TREATING PSORIASIS
(FR) APPLICATION D'UN INHIBITEUR DE GLUTAMINASE DANS LA PRÉPARATION D'UN MÉDICAMENT POUR TRAITER LE PSORIASIS
(ZH) 谷氨酰胺酶抑制剂在制备治疗银屑病的药物中的应用
Abstract
(EN) Disclosed in the present invention is an application of a glutaminase inhibitor in preparation of a drug for treating psoriasis. According to the present invention, in-vitro cell experiments prove that the glutaminase inhibitor can inhibit keratinocyte metabolism glutamine, inhibit miR-31 induced up-regulated keratinocyte mitochondrial respiration, inhibit miR-31 induced mTOR pathway, reduce cell activity and promote cell apoptosis, and has an anti-inflammatory effect; animal experiments prove that the glutaminase inhibitor can be used for effectively treating imiquimod-induced mouse psoriasis-like pathology change, comprising remarkably reducing a Baker score of a skin lesion, effectively reducing an epidermal hypertrophy degree, remarkably reducing the number of subepidermal capillaries, remarkably reducing the number of epidermal Ki67 positive cells and reducing the expression of epidermal GLS. Therefore, the glutaminase inhibitor can be used for preparing a drug for treating psoriasis.
(FR) Est divulguée dans la présente invention une application d'un inhibiteur de la glutaminase dans la préparation d'un médicament destiné à traiter le psoriasis. Selon la présente invention, des expériences cellulaires in vitro prouvent que l'inhibiteur de la glutaminase peut inhiber la glutamine du métabolisme des kératinocytes, inhiber la respiration mitochondriale des kératinocytes régulée à la hausse et induite par miR-31, inhiber la voie mTOR induite par miR-31, réduire l'activité cellulaire et promouvoir l'apoptose cellulaire, et a un effet anti-inflammatoire; des expériences sur des animaux prouvent que l'inhibiteur de la glutaminase peut être utilisé pour traiter efficacement un changement de pathologie de type psoriasis murin induit par imiquimod, comprenant la réduction remarquable d'un score Baker d'une lésion cutanée, réduisant efficacement un degré d'hypertrophie épidermique, réduisant remarquablement le nombre de capillaires sous-épidermiques, réduisant remarquablement le nombre de cellules positives de Ki67 épidermiques et réduisant l'expression de GLS épidermique. Par conséquent, l'inhibiteur de la glutaminase peut être utilisé pour préparer un médicament pour traiter le psoriasis.
(ZH) 本发明公开谷氨酰胺酶抑制剂在制备治疗银屑病的药物中的应用。本发明通过体外细胞实验证实了谷氨酰胺酶抑制剂可以抑制角质细胞代谢谷氨酰胺、抑制miR-31诱导上调的角质细胞线粒体呼吸、抑制miR-31诱导的mTOR通路、降低细胞活性并促进细胞凋亡以及具有抗炎作用;以及通过动物实验证实了谷氨酰胺酶抑制剂可以有效治疗咪喹莫特诱导的小鼠银屑病样病理改变,包括:显著降低皮损的Baker评分、有效减轻表皮肥厚程度、显著减少表皮下微血管数量、显著减少表皮层Ki67阳性细胞数和降低表皮GLS的表达。因此,谷氨酰胺酶抑制剂可用于制备治疗银屑病的药物。
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