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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- 238000011282 treatment Methods 0.000 title claims 3
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- 230000004770 neurodegeneration Effects 0.000 title 1
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- YCWSUKQGVSGXJO-NTUHNPAUSA-N nifuroxazide Chemical group C1=CC(O)=CC=C1C(=O)N\N=C\C1=CC=C([N+]([O-])=O)O1 YCWSUKQGVSGXJO-NTUHNPAUSA-N 0.000 title 1
- 238000000034 method Methods 0.000 claims 13
- 206010012289 Dementia Diseases 0.000 claims 12
- 208000024827 Alzheimer disease Diseases 0.000 claims 6
- 208000018737 Parkinson disease Diseases 0.000 claims 6
- 206010019075 Hallucination, visual Diseases 0.000 claims 5
- 208000019901 Anxiety disease Diseases 0.000 claims 4
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- 206010067889 Dementia with Lewy bodies Diseases 0.000 claims 2
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- COSPVUFTLGQDQL-UHFFFAOYSA-N Nelotanserin Chemical group C1=C(C=2N(N=CC=2Br)C)C(OC)=CC=C1NC(=O)NC1=CC=C(F)C=C1F COSPVUFTLGQDQL-UHFFFAOYSA-N 0.000 claims 2
- 208000027089 Parkinsonian disease Diseases 0.000 claims 2
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- 108010044266 Dopamine Plasma Membrane Transport Proteins Proteins 0.000 claims 1
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims 1
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims 1
- YJPIGAIKUZMOQA-UHFFFAOYSA-N Melatonin Natural products COC1=CC=C2N(C(C)=O)C=C(CCN)C2=C1 YJPIGAIKUZMOQA-UHFFFAOYSA-N 0.000 claims 1
- 229940099433 NMDA receptor antagonist Drugs 0.000 claims 1
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- 230000000561 anti-psychotic effect Effects 0.000 claims 1
- 230000006399 behavior Effects 0.000 claims 1
- 229960004205 carbidopa Drugs 0.000 claims 1
- TZFNLOMSOLWIDK-JTQLQIEISA-N carbidopa (anhydrous) Chemical compound NN[C@@](C(O)=O)(C)CC1=CC=C(O)C(O)=C1 TZFNLOMSOLWIDK-JTQLQIEISA-N 0.000 claims 1
- 239000000544 cholinesterase inhibitor Substances 0.000 claims 1
- DGBIGWXXNGSACT-UHFFFAOYSA-N clonazepam Chemical compound C12=CC([N+](=O)[O-])=CC=C2NC(=O)CN=C1C1=CC=CC=C1Cl DGBIGWXXNGSACT-UHFFFAOYSA-N 0.000 claims 1
- 229960003120 clonazepam Drugs 0.000 claims 1
- 229960004170 clozapine Drugs 0.000 claims 1
- QZUDBNBUXVUHMW-UHFFFAOYSA-N clozapine Chemical compound C1CN(C)CCN1C1=NC2=CC(Cl)=CC=C2NC2=CC=CC=C12 QZUDBNBUXVUHMW-UHFFFAOYSA-N 0.000 claims 1
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- VAIOZOCLKVMIMN-PRJWTAEASA-N eplivanserin Chemical compound C=1C=CC=C(F)C=1\C(=N/OCCN(C)C)\C=C\C1=CC=C(O)C=C1 VAIOZOCLKVMIMN-PRJWTAEASA-N 0.000 claims 1
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- FPCCSQOGAWCVBH-UHFFFAOYSA-N ketanserin Chemical compound C1=CC(F)=CC=C1C(=O)C1CCN(CCN2C(C3=CC=CC=C3NC2=O)=O)CC1 FPCCSQOGAWCVBH-UHFFFAOYSA-N 0.000 claims 1
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- RKEWSXXUOLRFBX-UHFFFAOYSA-N pimavanserin Chemical compound C1=CC(OCC(C)C)=CC=C1CNC(=O)N(C1CCN(C)CC1)CC1=CC=C(F)C=C1 RKEWSXXUOLRFBX-UHFFFAOYSA-N 0.000 claims 1
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- JUQLTPCYUFPYKE-UHFFFAOYSA-N ritanserin Chemical compound CC=1N=C2SC=CN2C(=O)C=1CCN(CC1)CCC1=C(C=1C=CC(F)=CC=1)C1=CC=C(F)C=C1 JUQLTPCYUFPYKE-UHFFFAOYSA-N 0.000 claims 1
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- 230000035945 sensitivity Effects 0.000 claims 1
- 239000002399 serotonin 2A agonist Substances 0.000 claims 1
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- 238000013268 sustained release Methods 0.000 claims 1
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- 229940124597 therapeutic agent Drugs 0.000 claims 1
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- 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
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- 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 or pantothenic acid
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- 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
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- 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
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- 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
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- 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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- Bioinformatics & Cheminformatics (AREA)
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- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Engineering & Computer Science (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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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 |
|---|---|
| RU2018103338A true RU2018103338A (ru) | 2019-08-15 |
| RU2018103338A3 RU2018103338A3 (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) |
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- 2016-07-15 CA CA2992518A patent/CA2992518A1/en not_active Abandoned
- 2016-07-15 WO PCT/US2016/042556 patent/WO2017011767A2/en active Application Filing
- 2016-07-15 RU RU2018103338A patent/RU2018103338A/ru unknown
- 2016-07-15 JP JP2018501972A patent/JP2018520187A/ja active Pending
- 2016-07-15 EP EP16825262.5A patent/EP3322415A4/en not_active Withdrawn
- 2016-07-15 MX MX2018000465A patent/MX2018000465A/es unknown
-
2018
- 2018-01-10 IL IL256831A patent/IL256831A/en unknown
- 2018-05-28 HK HK18106917.7A patent/HK1247555A1/zh unknown
- 2018-06-22 US US16/016,160 patent/US20190151287A1/en not_active Abandoned
-
2020
- 2020-11-20 US US17/100,528 patent/US11304932B2/en active Active
-
2021
- 2021-07-30 JP JP2021125769A patent/JP2021185144A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| BR112018000728A2 (pt) | 2018-09-04 |
| KR20180064373A (ko) | 2018-06-14 |
| CN108472285A (zh) | 2018-08-31 |
| US20210177804A1 (en) | 2021-06-17 |
| US20170014385A1 (en) | 2017-01-19 |
| EP3322415A2 (en) | 2018-05-23 |
| AU2016291673A1 (en) | 2018-01-25 |
| WO2017011767A2 (en) | 2017-01-19 |
| US20190151287A1 (en) | 2019-05-23 |
| JP2018520187A (ja) | 2018-07-26 |
| EP3322415A4 (en) | 2019-03-13 |
| JP2021185144A (ja) | 2021-12-09 |
| RU2018103338A3 (ru) | 2019-08-15 |
| MX2018000465A (es) | 2018-09-17 |
| HK1247555A1 (zh) | 2018-09-28 |
| US11304932B2 (en) | 2022-04-19 |
| WO2017011767A3 (en) | 2017-04-06 |
| CA2992518A1 (en) | 2017-01-19 |
| TW201720439A (zh) | 2017-06-16 |
| US10034859B2 (en) | 2018-07-31 |
| IL256831A (en) | 2018-03-29 |
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