RU2017145976A - Производные диарил- и арилгетероарилмочевины, применимые для профилактики и лечения нарушения поведения во время REM-фазы сна - Google Patents

Производные диарил- и арилгетероарилмочевины, применимые для профилактики и лечения нарушения поведения во время REM-фазы сна Download PDF

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RU2017145976A
RU2017145976A RU2017145976A RU2017145976A RU2017145976A RU 2017145976 A RU2017145976 A RU 2017145976A RU 2017145976 A RU2017145976 A RU 2017145976A RU 2017145976 A RU2017145976 A RU 2017145976A RU 2017145976 A RU2017145976 A RU 2017145976A
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sleep
subject
rem
combination
phase
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RU2017145976A
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Лоуренс Тим ФРИДХОФФ
Шанкар РАМАСВАМИ
Яньдун ВЭНЬ
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Аксовант Сайенсиз Гмбх
Лоуренс Тим ФРИДХОФФ
Шанкар РАМАСВАМИ
Яньдун ВЭНЬ
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the 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
    • A61K31/198—Alpha-aminoacids, e.g. alanine, edetic acids [EDTA]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/27—Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system

Claims (15)

1. Способ профилактики и/или лечения нарушения поведения во время REM-фазы сна, идиопатического нарушения поведения во время REM-фазы сна или их комбинации у субъекта, нуждающегося в этом, включающий введение указанному субъекту терапевтически эффективного количества обратного агониста 5-НТ2А.
2. Способ по п. 1, где обратный агонист 5-НТ2А выбран из нелотансерина, пимавансерина, прувансерина, эпливансерина, волинансерина, глемансерина, кетансерина, ритансерина, клозапина или их фармацевтически приемлемой соли, гидрата, полиморфа или сольвата.
3. Способ по п. 2, где обратный агонист 5-НТ2А представляет собой нелотансерин или его фармацевтически приемлемую соль, гидрат, полиморф или сольват.
4. Способ по п. 3, где терапевтически эффективное количество нелотансерина или его фармацевтически приемлемой соли, гидрата, полиморфа или сольвата составляет от 10 мг до приблизительно 160 мг.
5. Способ по п. 1, где обратный агонист 5-НТ2А обладает возможностью немедленного высвобождения, пролонгированного высвобождения, отсроченного высвобождения или любой их комбинации.
6. Способ по п. 1, где обратный агонист 5-НТ2А находится в фармацевтической композиции, и где фармацевтическая композиция составлена для перорального введения.
7. Способ по п. 1, где субъектом является человек.
8. Способ по п. 7, где человек является взрослым человеком, у которого диагностировано состояние, выбранное из вероятной деменции с тельцами Леви, деменции с тельцами Леви, деменции при болезни Паркинсона, болезни Паркинсона, множественной системной атрофии, болезни Альцгеймера, сосудистой деменции, деменции, умеренного когнитивного нарушения, психоза при болезни Паркинсона, психоза при болезни Альцгеймера, нарушения сна, бессонницы и любой их комбинации.
9. Способ по п. 7, где у человека одновременно диагностированы нарушение поведения во время REM-фазы сна, идиопатическое нарушение поведения во время REM-фазы сна или их комбинация и состояние, выбранное из вероятной деменции с тельцами Леви, деменции при болезни Паркинсона, болезни Паркинсона, множественной системной атрофии, умеренного когнитивного нарушения, психоза при болезни Паркинсона, психоза при болезни Альцгеймера, нарушения сна, бессонницы и их комбинации.
10. Способ по п. 1, где субъект одновременно получает терапевтически эффективное количество по меньшей мере одного дополнительного терапевтического средства, выбранного из группы, состоящей из мелатонина, кветиапина, клоназепама, леводопы, карбидопы, противопаркинсонического лекарственного средства, ингибитора ацетилхолинэстеразы, антагониста NMDA-рецепторов и их комбинации.
11. Способ по п. 1, где лечение или профилактика приводят к уменьшению частоты, тяжести эпизодов нарушения поведения во время REM-фазы сна или их комбинации.
12. Способ по п. 1, где лечение или профилактика приводят к уменьшению частоты эпизодов аномальной вокализации и двигательного поведения за период сна.
13. Способ профилактики и/или лечения нарушения поведения во время REM-фазы сна, идиопатического нарушения поведения во время REM-фазы сна или их комбинации у субъекта, нуждающегося в этом, включающий введение указанному субъекту суточной дозы нелотансерина, составляющей приблизительно 40 мг.
14. Способ профилактики и/или лечения нарушения поведения во время REM-фазы сна, идиопатического нарушения поведения во время REM-фазы сна или их комбинации у субъекта, нуждающегося в этом, включающий введение указанному субъекту суточной дозы нелотансерина, составляющей приблизительно 80 мг.
15. Способ профилактики и/или лечения нарушения поведения во время REM-фазы сна, идиопатического нарушения поведения во время REM-фазы сна или их комбинации у субъекта, нуждающегося в этом, включающий введение указанному субъекту дозы нелотансерина, составляющей приблизительно 40 мг, в первый период времени с последующим введением указанному субъекту дозы нелотансерина, составляющей приблизительно 80 мг, во второй период времени.
RU2017145976A 2015-06-12 2016-06-10 Производные диарил- и арилгетероарилмочевины, применимые для профилактики и лечения нарушения поведения во время REM-фазы сна RU2017145976A (ru)

Applications Claiming Priority (11)

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US201562174983P 2015-06-12 2015-06-12
US62/174,983 2015-06-12
US201562194084P 2015-07-17 2015-07-17
US62/194,084 2015-07-17
US201562236562P 2015-10-02 2015-10-02
US62/236,562 2015-10-02
US201562263967P 2015-12-07 2015-12-07
US62/263,967 2015-12-07
US201662278198P 2016-01-13 2016-01-13
US62/278,198 2016-01-13
PCT/US2016/037090 WO2016201373A1 (en) 2015-06-12 2016-06-10 Diaryl and arylheteroaryl urea derivatives useful for the prophylaxis and treatment of rem sleep behavior disorder

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US (3) US10022355B2 (ru)
EP (2) EP4119141A1 (ru)
JP (2) JP2018516992A (ru)
KR (1) KR20180022792A (ru)
CN (1) CN109562085A (ru)
AU (2) AU2016276966A1 (ru)
CA (1) CA2989343A1 (ru)
HK (1) HK1245660A1 (ru)
IL (1) IL256231A (ru)
MX (1) MX2017016413A (ru)
NO (1) NO20180040A1 (ru)
RU (1) RU2017145976A (ru)
TW (1) TW201717939A (ru)
WO (1) WO2016201373A1 (ru)
ZA (1) ZA201800186B (ru)

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