RU2018103338A - Производные диарил- и арилгетероарилмочевины для профилактики и лечения галлюцинаций, ассоциированных с нейродегенеративным заболеванием - Google Patents
Производные диарил- и арилгетероарилмочевины для профилактики и лечения галлюцинаций, ассоциированных с нейродегенеративным заболеванием Download PDFInfo
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- A61K31/00—Medicinal preparations containing organic active ingredients
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- 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
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- 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
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- 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
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- 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
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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
- A61K31/55—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
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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
- A61K31/55—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
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- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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- 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
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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Claims (15)
1. Способ профилактики и/или лечения зрительных галлюцинаций у субъекта, нуждающегося в этом, предусматривающий введение указанному субъекту терапевтически эффективного количества обратного агониста 5-HT2A.
2. Способ по п. 1, где обратный агонист 5-HT2A выбран из нелотансерина, пимавансерина, прувансерина, эпливансерина, волинансерина, глемансерина, кетансерина, ритансерина, клозапина и их фармацевтически приемлемой соли, гидрата, полиморфа или сольвата.
3. Способ по п. 2, где обратный агонист 5-HT2A 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 приблизительно 10 мг до приблизительно 160 мг.
5. Способ по п. 1, где обратный агонист 5-HT2A находится в фармацевтической композиции, которая обладает возможностью немедленного высвобождения, пролонгированного высвобождения, отсроченного высвобождения или любой их комбинации.
6. Способ по п. 1, где обратный агонист 5-HT2A 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 деменции, связанной с тельцами Леви, возможной 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, бредовых иллюзий, тревожного возбуждения, тревожного возбуждения при болезни Альцгеймера, агрессивности, нарушения поведения во время REM-фазы сна, шизофрении и любой их комбинации.
9. Способ по п. 7, где у человека одновременно диагностированы зрительные галлюцинации и состояние, выбранное из деменции, связанной с тельцами Леви, возможной 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, бредовых иллюзий, тревожного возбуждения, тревожного возбуждения при болезни Альцгеймера, агрессивности, нарушения поведения во время REM-фазы сна, шизофрении и любой их комбинации.
10. Способ по п. 7, где у человека диагностирована возможная деменция с тельцами Леви, где диагноз возможной деменции с тельцами Леви определяется наличием деменции и по меньшей мере одного из следующего:
по меньшей мере два основных критерия, выбранных из зрительных галлюцинаций, когнитивной неустойчивости и паркинсонизма и любой их комбинации; и
один основной критерий, выбранный из зрительных галлюцинаций, когнитивной неустойчивости и паркинсонизма и любой их комбинации; и по меньшей мере один предположительный критерий, выбранный из нарушения поведения во время REM-фазы сна, тяжелой нейролептической чувствительности; низкого поглощения транспортера дофамина при визуализирующем сканировании DaT SPECT и любой их комбинации.
11. Способ по п. 7, где у человека диагностирована деменция с тельцами Леви.
12. 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.
13. Способ по п. 1, где лечение или профилактика приводят к уменьшению частоты, тяжести зрительных галлюцинаций или их комбинации.
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562192939P | 2015-07-15 | 2015-07-15 | |
| US62/192,939 | 2015-07-15 | ||
| US201562236618P | 2015-10-02 | 2015-10-02 | |
| US62/236,618 | 2015-10-02 | ||
| US201562261381P | 2015-12-01 | 2015-12-01 | |
| US62/261,381 | 2015-12-01 | ||
| PCT/US2016/042556 WO2017011767A2 (en) | 2015-07-15 | 2016-07-15 | Diaryl and arylheteroaryl urea derivatives as modulators of the 5-ht2a serotonin receptor useful for the prophylaxis and treatment of hallucinations associated with a neurodegenerative disease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2018103338A3 RU2018103338A3 (ru) | 2019-08-15 |
| RU2018103338A true RU2018103338A (ru) | 2019-08-15 |
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| Application Number | Title | Priority Date | Filing Date |
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| RU2018103338A RU2018103338A (ru) | 2015-07-15 | 2016-07-15 | Производные диарил- и арилгетероарилмочевины для профилактики и лечения галлюцинаций, ассоциированных с нейродегенеративным заболеванием |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US10034859B2 (ru) |
| EP (1) | EP3322415A4 (ru) |
| JP (2) | JP2018520187A (ru) |
| KR (1) | KR20180064373A (ru) |
| CN (1) | CN108472285A (ru) |
| AU (1) | AU2016291673A1 (ru) |
| BR (1) | BR112018000728A2 (ru) |
| CA (1) | CA2992518A1 (ru) |
| HK (1) | HK1247555A1 (ru) |
| IL (1) | IL256831A (ru) |
| MX (1) | MX391031B (ru) |
| RU (1) | RU2018103338A (ru) |
| TW (1) | TW201720439A (ru) |
| WO (1) | WO2017011767A2 (ru) |
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| TWI415845B (zh) | 2006-10-03 | 2013-11-21 | Arena Pharm Inc | 用於治療與５-ｈｔ2ａ血清素受體相關聯病症之作為５-ｈｔ2ａ血清素受體之調節劑的吡唑衍生物 |
| WO2009123714A2 (en) | 2008-04-02 | 2009-10-08 | Arena Pharmaceuticals, Inc. | Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor |
| EP2364142B1 (en) | 2008-10-28 | 2018-01-17 | Arena Pharmaceuticals, Inc. | Compositions of a 5-ht2a serotonin receptor modulator useful for the treatment of disorders related thereto |
| WO2010062321A1 (en) | 2008-10-28 | 2010-06-03 | Arena Pharmaceuticals, Inc. | Processes useful for the preparation of 1-[3-(4-bromo-2-methyl-2h-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea and crystalline forms related thereto |
| CA2989343A1 (en) | 2015-06-12 | 2016-12-15 | Yandong Wen | Diaryl and arylheteroaryl urea derivatives useful for the prophylaxis and treatment of rem sleep behavior disorder |
| RU2018103338A (ru) | 2015-07-15 | 2019-08-15 | Аксовант Сайенсиз Гмбх | Производные диарил- и арилгетероарилмочевины для профилактики и лечения галлюцинаций, ассоциированных с нейродегенеративным заболеванием |
| PT3325444T (pt) | 2015-07-20 | 2021-09-22 | Acadia Pharm Inc | Métodos para preparar n-(4-fluorobenzil)-n-(1-metilpiperidina-4-il)-n'-(4-(2-metilpropiloxi)fenilmetil)carbamida e o seu sal de tartarato e forma polimórfica c |
| WO2017165635A1 (en) | 2016-03-25 | 2017-09-28 | Acadia Pharmaceuticals Inc. | Combination of pimavanserin and cytochrome p450 modulators |
| US10953000B2 (en) | 2016-03-25 | 2021-03-23 | Acadia Pharmaceuticals Inc. | Combination of pimavanserin and cytochrome P450 modulators |
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| EP3615028A1 (en) | 2017-04-28 | 2020-03-04 | Acadia Pharmaceuticals Inc. | Pimavanserin for treating impulse control disorder |
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| USD980157S1 (en) * | 2021-02-26 | 2023-03-07 | The Goodyear Tire & Rubber Company | Tire |
| KR102753583B1 (ko) * | 2021-11-11 | 2025-01-10 | 의료법인 명지의료재단 | Kras 특이적 활성화 t 세포 유도용 항원 조성물 |
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-
2016
- 2016-07-15 RU RU2018103338A patent/RU2018103338A/ru unknown
- 2016-07-15 CA CA2992518A patent/CA2992518A1/en not_active Abandoned
- 2016-07-15 HK HK18106917.7A patent/HK1247555A1/zh unknown
- 2016-07-15 EP EP16825262.5A patent/EP3322415A4/en not_active Withdrawn
- 2016-07-15 TW TW105122509A patent/TW201720439A/zh unknown
- 2016-07-15 AU AU2016291673A patent/AU2016291673A1/en not_active Abandoned
- 2016-07-15 US US15/211,638 patent/US10034859B2/en active Active
- 2016-07-15 BR BR112018000728A patent/BR112018000728A2/pt not_active Application Discontinuation
- 2016-07-15 WO PCT/US2016/042556 patent/WO2017011767A2/en not_active Ceased
- 2016-07-15 MX MX2018000465A patent/MX391031B/es unknown
- 2016-07-15 KR KR1020187004357A patent/KR20180064373A/ko not_active Ceased
- 2016-07-15 JP JP2018501972A patent/JP2018520187A/ja active Pending
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- 2018-06-22 US US16/016,160 patent/US20190151287A1/en not_active Abandoned
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| IL256831A (en) | 2018-03-29 |
| RU2018103338A3 (ru) | 2019-08-15 |
| BR112018000728A2 (pt) | 2018-09-04 |
| EP3322415A2 (en) | 2018-05-23 |
| US20210177804A1 (en) | 2021-06-17 |
| CN108472285A (zh) | 2018-08-31 |
| US11304932B2 (en) | 2022-04-19 |
| EP3322415A4 (en) | 2019-03-13 |
| MX2018000465A (es) | 2018-09-17 |
| HK1247555A1 (zh) | 2018-09-28 |
| CA2992518A1 (en) | 2017-01-19 |
| JP2018520187A (ja) | 2018-07-26 |
| US10034859B2 (en) | 2018-07-31 |
| US20170014385A1 (en) | 2017-01-19 |
| TW201720439A (zh) | 2017-06-16 |
| KR20180064373A (ko) | 2018-06-14 |
| WO2017011767A2 (en) | 2017-01-19 |
| AU2016291673A1 (en) | 2018-01-25 |
| WO2017011767A3 (en) | 2017-04-06 |
| JP2021185144A (ja) | 2021-12-09 |
| MX391031B (es) | 2025-03-21 |
| US20190151287A1 (en) | 2019-05-23 |
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