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1. WO2021139843 - COMPOSITION AND METHOD OF TREATMENT TO SIMULTANEOUSLY INCREASE THE ANALGESIC EFFICACY OF OPIOIDS AND REDUCE THEIR ADDICTIVE POWER

Publication Number WO/2021/139843
Publication Date 15.07.2021
International Application No. PCT/CU2020/050010
International Filing Date 18.12.2020
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 31/5513 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
55having seven-membered rings, e.g. azelastine, pentylenetetrazole
551having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
55131,4-Benzodiazepines, e.g. diazepam
A61K 45/06 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
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 25/02 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
02for peripheral neuropathies
A61P 25/30 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
30for treating abuse or dependence
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 31/5513
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
55having seven-membered rings, e.g. azelastine, pentylenetetrazole
551having two nitrogen atoms, e.g. dilazep
55131,4-Benzodiazepines, e.g. diazepam ; or clozapine
A61K 45/06
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
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 25/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
02for peripheral neuropathies
A61P 25/30
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
30for treating abuse or dependence
C07D 471/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Applicants
  • CENTRO DE INVESTIGACIÓN Y DESARROLLO DE MEDICAMENTOS CIDEM [CU]/[CU]
  • UNIVERSIDAD DE LA HABANA [CU]/[CU]
Inventors
  • GARRIDO SUÁREZ, Bárbara Beatriz
  • BÁRZAGA-FERNÁNDEZ, Pedro Gilberto
  • PADRÓN-YAQUIS, Alejandro Saúl
  • VERDECIA REYES, Yamila
  • OCHOA RODRIGUEZ, Estael
Agents
  • BÁRZAGA-FERNÁNDEZ, Pedro Gilberto
Priority Data
2019-011426.12.2019CU
Publication Language Spanish (es)
Filing Language Spanish (ES)
Designated States
Title
(EN) COMPOSITION AND METHOD OF TREATMENT TO SIMULTANEOUSLY INCREASE THE ANALGESIC EFFICACY OF OPIOIDS AND REDUCE THEIR ADDICTIVE POWER
(ES) COMPOSICIÓN Y MÉTODO DE TRATAMIENTO PARA SIMULTÁNEAMENTE INCREMENTAR LA EFICACIA ANALGÉSICA DE LOS OPIOIDES Y REDUCIR SU PODER ADICTIVO
(FR) COMPOSITION ET MÉTHODE DE TRAITEMENT POUR AUGMENTER SIMULTANÉMENT L'EFFICACITÉ ANALGÉSIQUE DES OPIOÏDES ET RÉDUIRE LEUR POUVOIR ADDICTIF
Abstract
(EN) The present invention describes a pharmaceutical composition that includes a novel molecule with neuroprotective activity, to inhibit the neuroadaptations induced by opioids (tolerance and hyperalgesia) that lead to the successive escalation of doses in the treatment of pain. In this way, the composition increases the analgesic efficacy of opioids under normal conditions and in the presence of neural damage, since this favors the appearance of tolerance / hyperalgesia and resistance to opioid treatment. Likewise, the composition reduces the spontaneous signs of withdrawal associated with withdrawal from opioids and consequently physical dependence and possible addiction. In addition, the present invention describes a method for the treatment of pain with a neuropathic component that is supported by drug interaction and safety studies that show its synergy for the mechanical antihypernociceptive effect.
(ES) La presente invención describe una composición farmacéutica que incluye a una novedosa molécula con actividad neuroprotectora, para inhibir las neuroadaptaciones inducidas por los opioides (tolerancia e hiperalgesia) que conducen al escalado sucesivo de sus dosis en el tratamiento del dolor. De esta forma incrementar su eficacia analgésica en condiciones normales y de daño neural, ya que este favorece la aparición de tolerancia/hiperalgesia y resistencia al tratamiento con opioides. Asimismo, reducir los signos espontáneos de abstinencia asociados a su retirada y en consecuencia la dependencia física y posible adicción. Además, describe un método para el tratamiento del dolor con componente neuropático que es sustentado por los estudios de interacción y seguridad farmacológica que muestran su sinergia para el efecto antihipernociceptivo mecánico.
(FR) La présente invention concerne une composition pharmaceutique qui comprend une nouvelle molécule à activité neuroprotectrice, pour inhiber les neuroadaptations induites par les opioïde (tolérance et hyperalgésie) qui conduisent à l'escalade successive de leurs doses dans le traitement de la douleur. Et également pour augmenter son efficacité analgésique dans des conditions normales et de lésion neurale, puisque cette composition favorise l'apparition de tolérance/hyperalgésie et résistance au traitement avec des opioïdes. Puis, pour réduire les signes spontanés d'abstinence associés à son retrait et par conséquent la dépendance physique et la possible addiction. L'invention concerne, en outre, une méthode de traitement de la douleur avec un composant neuropatique qui est soutenu par les études d'interaction et de sécurité pharmacologique qui montrent sa synergie pour un effet anti-hypernociceptif mécanique.
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