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1. CN109331185 - Medicine containing liver-targeting specific ligand and thyroxine receptor agonist

Office China
Application Number 201811452803.5
Application Date 30.11.2018
Publication Number 109331185
Publication Date 15.02.2019
Grant Number 109331185
Grant Date 29.11.2019
Publication Kind B
IPC
A61K 47/54
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
A61K 47/61
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
56the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
61the organic macromolecular compound being a polysaccharide or a derivative thereof
A61K 31/198
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
19Carboxylic acids, e.g. valproic acid
195having an amino group
197the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid (GABA), beta-alanine, epsilon-aminocaproic acid, pantothenic acid
198Alpha-amino acids, e.g. alanine, edetic acid (EDTA)
A61P 1/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
16for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
CPC
A61K 31/198
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic, hydroximic acids
19Carboxylic acids, e.g. valproic acid
195having an amino group
197the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid, pantothenic acid
198Alpha-aminoacids, e.g. alanine, edetic acids [EDTA],
A61K 31/44
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
44Non condensed pyridines; Hydrogenated derivatives thereof
A61K 47/549
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
549Sugars, nucleosides, nucleotides or nucleic acids
A61K 47/61
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
56the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
61the organic macromolecular compound being a polysaccharide or a derivative thereof
A61P 1/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
16for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
Applicants KYLONOVA (XIAMEN) BIOPHARMA CO., LTD.
厦门甘宝利生物医药有限公司
Inventors CUI KUNYUAN
崔坤元
Agents 北京精金石知识产权代理有限公司 11470
Priority Data 2017112481858 01.12.2017 CN
Title
(EN) Medicine containing liver-targeting specific ligand and thyroxine receptor agonist
(ZH) 含有肝靶向特异性配体和甲状腺素受体激动剂的药物
Abstract
(EN)
The invention provides a medicine structurally containing a liver-targeting specific ligand and a thyroxine receptor agonist. The liver-targeting specific ligand and the thyroxine receptor agonist areconnected by branched chains, connectors and connecting chains to form a novel medicine structure. Thyroxine receptors (TRs) are divided into two subtypes, namely TR-alpha and TR-beta, wherein the TR-beta is mainly expressed in the liver, and the TR-alpha is mainly expressed in the heart, the nervous system and the like. In some embodiments, the medicine provided by the invention is expected to have a liver-targeting effect and can specifically bring the thyroxine receptor agonist into the liver so as to prevent the thyroxine receptor agonist from entering the heart and other tissues, so thatside effects triggered by the effect of the thyroxine receptor agonist on the other tissues can be avoided and the therapeutic effect of the medicine on treatment of lipid metabolism disorders and related complications is maintained.

(ZH)
本文提供了结构中含有肝靶向特异性配体和甲状腺素受体激动剂的药物,是通过支链、接头和连接链将肝靶向特异性配体和甲状腺素受体激动剂连接,成为一个新的药物结构。甲状腺激素受体(TRs)分为两个亚型,TR‑α和TR‑β,其中TR‑β主要表达在肝脏,TR‑α主要表达在心脏、神经系统等。在某些实施方案中,预期本文提供的药物具有肝靶向的作用,可以把甲状腺素受体激动剂特异性的带入到肝脏,使其不进入到心脏和其他组织,可以避免甲状腺素受体激动剂对其他组织的作用引发副作用,并保持其治疗脂质代谢紊乱及相关并发症的疗效。

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