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1. WO2020063821 - POLYPEPTIDE CONJUGATE OF ODN OR DERIVATIVE THEREOF, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF

Publication Number WO/2020/063821
Publication Date 02.04.2020
International Application No. PCT/CN2019/108414
International Filing Date 27.09.2019
IPC
C07K 7/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
7Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
04Linear peptides containing only normal peptide links
06having 5 to 11 amino acids
A61K 38/08 2019.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
08Peptides having 5 to 11 amino acids
C07C 317/22 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
317Sulfones; Sulfoxides
16having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton
22with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
A61P 19/02 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
02for joint disorders, e.g. arthritis, arthrosis
A61P 19/10 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
08for bone diseases, e.g. rachitism, Paget's disease
10for osteoporosis
CPC
A61K 38/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
08Peptides having 5 to 11 amino acids
A61P 19/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
02for joint disorders, e.g. arthritis, arthrosis
A61P 19/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
08for bone diseases, e.g. rachitism, Paget's disease
10for osteoporosis
C07C 317/22
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
317Sulfones; Sulfoxides
16having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton
22with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
C07K 7/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
7Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
04Linear peptides containing only normal peptide links
06having 5 to 11 amino acids
Applicants
  • 北京和理咨询有限公司 BEIJING HELI CONSULTING CO. LTD [CN]/[CN]
Inventors
  • 刘振丽 LIU, Zhenli
  • 张保亭 ZHANG, Baoting
  • 鲁军 LU, Jun
  • 梁超 LIANG, Chao
  • 党蕾 DANG, Lei
  • 吕诚 LU, Cheng
Agents
  • 北京市隆安律师事务所 BEIJING LONGAN LAW FIRM
Priority Data
201811154973.530.09.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) POLYPEPTIDE CONJUGATE OF ODN OR DERIVATIVE THEREOF, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
(FR) CONJUGUÉ POLYPEPTIDIQUE D'ODN OU D'UN DÉRIVÉ DE CELUI-CI, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION
(ZH) ODN或衍生物的多肽偶合物及其制备方法和应用
Abstract
(EN)
A polypeptide conjugate of ODN or a derivative thereof, and a preparation method therefor, the conjugate is a compound represented by formula (I): (I) the compound has the characteristics of good targeting, strong biological activity, low toxicity and side effects, good water solubility, and high bioavailability; the preparation process is simple, scientific and reasonable, while the quality is controllable, the reproducibility is good, and the process is suitable for production; the compound may specifically inhibit the activity of cathepsin secreted by osteoclasts in bone tissue, thereby inhibiting bone resorption activity, and may effectively delay the pathological progress of osteoporosis and osteoarthritis, while having good biocompatibility and safety, and being easy to use.
(FR)
L'invention concerne un conjugué polypeptidique d'ODN ou d'un dérivé de celui-ci, et son procédé de préparation, le conjugué étant un composé représenté par la formule (I) : (I) le composé présente des caractéristiques en termes d'un bon ciblage, d'une forte activité biologique, d'une faible toxicité et de moins d'effets secondaires, ainsi qu'une bonne solubilité dans l'eau et une biodisponibilité élevée ; le procédé de préparation est simple, scientifique et raisonnable, la qualité peut être contrôlée, la reproductibilité est bonne, et le procédé est approprié pour la production ; le composé peut inhiber de manière spécifique l'activité de la cathepsine sécrétée par des ostéoclastes dans un tissu osseux, ce qui permet d'inhiber l'activité de résorption osseuse, et peut retarder de manière efficace la progression pathologique de l'ostéoporose et de l'arthrose, tout en ayant une bonne biocompatibilité et une bonne sécurité, et en étant facile à utiliser.
(ZH)
一种ODN或其衍生物的多肽偶合物及其制备方法,所述偶合物为式(I)化合物:(I)该化合物具有靶向性好、生物活性强、毒副作用低,水溶性好、生物利用度高的特点;制备工艺简单,科学合理,质量可控,重现性好,适于生产;所述化合物可特异性地抑制骨组织内破骨细胞分泌的组织蛋白酶活性,进而抑制骨吸收活性,可有效延缓骨质疏松症和骨关节炎的病理进程,并具有良好的生物相容性和安全性,使用简便。
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