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1. WO2022116256 - COMPOSITION FOR TREATING MAJOR DEPRESSIVE DISORDER

Publication Number WO/2022/116256
Publication Date 09.06.2022
International Application No. PCT/CN2020/135895
International Filing Date 11.12.2020
IPC
A61K 31/485 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
485Morphinan derivatives, e.g. morphine, codeine
A61K 9/72 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
72for smoking or inhaling
A61K 9/20 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
20Pills, lozenges or tablets
A61K 9/08 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
08Solutions
A61P 25/24 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
24Antidepressants
CPC
A61K 31/485
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
485Morphinan derivatives, e.g. morphine, codeine
A61K 9/0043
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
0012Galenical forms characterised by the site of application
0043Nose
A61K 9/006
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
0012Galenical forms characterised by the site of application
0053Mouth and digestive tract, i.e. intraoral and peroral administration
006Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
A61K 9/0073
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
0012Galenical forms characterised by the site of application
007Pulmonary tract; Aromatherapy
0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy;
A61K 9/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
08Solutions
A61K 9/146
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
14Particulate form, e.g. powders, ; Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
141Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
146with organic macromolecular compounds
Applicants
  • 深圳善康医药科技股份有限公司 SHENZHEN SCIENCARE PHARMACEUTICAL CO., LTD [CN]/[CN]
Inventors
  • 尹述贵 YING, Shugui
  • 王实强 WANG, Shiqiang
  • 曲伟 QU, Wei
  • 张桐桐 ZHANG, Tongtong
  • 颜携国 YAN, Xieguo
  • 李勇 LI, Yong
  • 李远 LI, Yuan
  • 梁民彩 LIANG, Mincai
Agents
  • 北京精金石知识产权代理有限公司 JJS INTELLECTUAL PROPERTY AGENCY LTD.
Priority Data
202011400073.102.12.2020CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) COMPOSITION FOR TREATING MAJOR DEPRESSIVE DISORDER
(FR) COMPOSITION POUR LE TRAITEMENT DE DÉPRESSION MAJEURE
(ZH) 一种治疗重度抑郁症的组合物
Abstract
(EN) Disclosed is a composition for treating major depressive disorder, characterized by comprising a buprenorphine active ingredient and a dextromethorphan active ingredient. The weight ratio of the buprenorphine active ingredient to the dextromethorphan active ingredient is 1:7.5-300. By means of synergistic compounding of the buprenorphine and the dextromethorphan, the present invention acts to stimulate a μ-opioid receptor, antagonize a κ-opioid receptor, antagonize an NMDA receptor, stimulate a sigma-1 receptor, antagonize a 5-HT receptor and an NE receptor, and to block an inflammatory pathway, etc. to achieve combined effects of multiple targets and multiple mechanisms, making it possible to greatly improve therapeutic effects on patients with major depressive disorder (MDD), especially treatment-resistant depression (TRD). Furthermore, the dextromethorphan reduces the dosage and addictiveness of the buprenorphine, achieving the advantages of multiple targets, rapid onset, and low addictiveness.
(FR) La présente invention concerne une composition destinée à traiter la dépression majeure, caractérisée en ce qu'elle comprend un principe actif de buprénorphine et un principe actif de dextrométhorphane. Le rapport pondéral entre le principe actif buprénorphine et le principe actif dextrométhorphane est de 1:7,5 à 300. Grâce au mélangeage synergique de la buprénorphine et du dextrométhorphane, la présente invention agit pour stimuler un récepteur μ-opioïde, servir d'antagoniste à un récepteur κ-opioïde, servir d'antagoniste à un récepteur NMDA, stimuler un récepteur sigma-1, servir d'antagoniste à un récepteur 5-HT et à un récepteur NE, et bloquer une voie inflammatoire, etc. afin d'obtenir des effets combinés de cibles multiples et de mécanismes multiples, ce qui permet d'améliorer considérablement les effets thérapeutiques sur les patients souffrant de dépression majeure, en particulier de dépression résistante au traitement. En outre, le dextrométhorphane réduit le dosage de la buprénorphine et la dépendance à celle-ci, ce qui permet d'obtenir les avantages des cibles multiples, de l'action rapide et de la faible dépendance.
(ZH) 本发明公开了一种治疗重度抑郁症的组合物,其特征在于,包括丁丙诺啡活性成分和右美沙芬活性成分;所述丁丙诺啡活性成分和右美沙芬活性成分的重量比为1:7.5-300。本发明通过丁丙诺啡与右美沙芬的协同复配,通过作用激动μ阿片受体、拮抗κ阿片受体、拮抗NMDA受体、激动sigma-1受体、拮抗5-HT受体和NE受体、以及阻断炎症通路等多靶点、多重机理的共同作用,可以大幅提高对重度抑郁症患者(MDD),尤其是难治型抑郁症(TRD)的治疗效果,同时右美沙芬降低了丁丙诺啡的用量及成瘾性,具有多靶点、快速起效、低成瘾性的优点。
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