RU2005117612A - Новые модуляторы дофаминовой нейротрансмиссии - Google Patents
Новые модуляторы дофаминовой нейротрансмиссии Download PDFInfo
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- RU2005117612A RU2005117612A RU2005117612/04A RU2005117612A RU2005117612A RU 2005117612 A RU2005117612 A RU 2005117612A RU 2005117612/04 A RU2005117612/04 A RU 2005117612/04A RU 2005117612 A RU2005117612 A RU 2005117612A RU 2005117612 A RU2005117612 A RU 2005117612A
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- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 title 2
- 229960003638 dopamine Drugs 0.000 title 1
- 230000005062 synaptic transmission Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 16
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 16
- 238000000034 method Methods 0.000 claims abstract 13
- 150000003839 salts Chemical class 0.000 claims abstract 11
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 6
- -1 3,3,3-trifluoropropyl Chemical group 0.000 claims abstract 4
- 208000035475 disorder Diseases 0.000 claims abstract 4
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims abstract 2
- 230000000642 iatrogenic effect Effects 0.000 claims 8
- 208000019901 Anxiety disease Diseases 0.000 claims 4
- 208000019022 Mood disease Diseases 0.000 claims 4
- 208000028683 bipolar I disease Diseases 0.000 claims 4
- 239000000126 substance Substances 0.000 claims 4
- 230000036506 anxiety Effects 0.000 claims 3
- 201000000980 schizophrenia Diseases 0.000 claims 3
- 208000007848 Alcoholism Diseases 0.000 claims 2
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 2
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims 2
- 206010003805 Autism Diseases 0.000 claims 2
- 208000020706 Autistic disease Diseases 0.000 claims 2
- 208000020925 Bipolar disease Diseases 0.000 claims 2
- 208000012661 Dyskinesia Diseases 0.000 claims 2
- 208000014094 Dystonic disease Diseases 0.000 claims 2
- 208000023105 Huntington disease Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 208000027089 Parkinsonian disease Diseases 0.000 claims 2
- 206010034010 Parkinsonism Diseases 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- 208000028017 Psychotic disease Diseases 0.000 claims 2
- 208000000323 Tourette Syndrome Diseases 0.000 claims 2
- 206010001584 alcohol abuse Diseases 0.000 claims 2
- 208000025746 alcohol use disease Diseases 0.000 claims 2
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 2
- 208000010877 cognitive disease Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 206010013663 drug dependence Diseases 0.000 claims 2
- 208000010118 dystonia Diseases 0.000 claims 2
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 claims 2
- 238000002347 injection Methods 0.000 claims 2
- 239000007924 injection Substances 0.000 claims 2
- 208000019116 sleep disease Diseases 0.000 claims 2
- 208000011117 substance-related disease Diseases 0.000 claims 2
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 230000000698 schizophrenic effect Effects 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 101100203601 Caenorhabditis elegans sor-3 gene Proteins 0.000 abstract 1
- 210000003169 central nervous system Anatomy 0.000 abstract 1
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- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/06—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals
- C07D295/073—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals with the ring nitrogen atoms and the substituents separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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- C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
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- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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Claims (30)
1. Соединение 3-замещенного 4-(фенил-N-алкил)пиперазин формулы 1
где R1 выбран из группы, состоящей из OSO2CF3, OSO2CH3, SO2R3, COCF3, COCH3 и COCH2CH3, где R3 такой, как определено ниже;
R2 выбран из группы, состоящей из C1-C4 алкилов, аллилов, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-трифторпропила, 4,4,4-трифторбутила;
R3 выбран из группы, состоящей из С1-С3 алкилов, CF3 и N(CH3)2, при условии, что, когда R1 является SO2R3, и R3 является С1-С3 алкилом, тогда R2 не является CH2CH2OCH3;
или его фармацевтически приемлемая соль.
2. Соединение по п.1 или 2, где R1 выбран из группы, состоящей из OSO2CF3, OSO2CH3, SO2СН3, SO2CF3, COCH3.
3. Соединение по п.1 или 2, где R2 выбран из н-пропила и этила.
4. Фармацевтическая композиция, содержащая соединение по любому из пп.1-3 и один или более фармацевтически приемлемых носителей или разбавителей.
5. Фармацевтическая композиция по п.4, пригодная для лечения состояния, выбранного из группы, состоящей из таких как ятрогенный и не ятрогенный паркинсонизм, дискинезии и дистонии, болезнь Туретта.
6. Фармацевтическая композиция по п.4, пригодная для лечения болезни Паркинсона.
7. Фармацевтическая композиция по п.4, пригодная для лечения состояний, выбранных из группы, состоящей из ятрогенных и не ятрогенных психозов и галлюцинозов.
8. Фармацевтическая композиция по п.4, пригодная для лечения состояний, выбранных из шизофрении и шизофреноподобных заболеваний.
9. Фармацевтическая композиция по п.4, пригодная для лечения состояний, выбранных из группы, состоящей из расстройств настроения и тревожных состояний.
10. Фармацевтическая композиция по п.9, где указанные расстройства настроения и тревожные состояния выбраны из маниакально-депрессивного заболевания, депрессии и обсессивно-компульсивного заболевания.
11. Фармацевтическая композиция по п.4, пригодная для лечения состояний, выбранных из группы, состоящей из расстройств, связанных с дефицитом внимания, аутизма, когнитивных дисфункций.
12. Фармацевтическая композиция по п.4, пригодная для лечения заболевания Хантингтона.
13. Фармацевтическая композиция по п.4, пригодная для лечения расстройств сна.
14. Фармацевтическая композиция по п.4, пригодная для лечения расстройств, вызванных веществами, к которым относятся злоупотребление алкоголем или привыкание к лекарству.
15. Фармацевтическая композиция по любому из пп.4-14, приготовленная для орального введения.
16. Фармацевтическая композиция по п.15, приготовленная в виде таблетки.
17. Фармацевтическая композиция по п.15, приготовленная в виде капсулы.
18. Фармацевтическая композиция по любому из пп.4-14, приготовленная для введения путем инъекции.
19. Способ лечения состояний, выбранных из группы, состоящей из ятрогенного и не ятрогенного паркинсонизма, дискинезии и дистонии, болезни Туретта, включающий введение пациенту фармацевтически эффективного количества соединения или фармацевтически приемлемой соли по любому одному из пп.1-3.
20. Способ лечения болезни Паркинсона, включающий введение пациенту фармацевтически эффективного количества соединения или фармацевтически приемлемой соли по любому одному из пп.1-3.
21. Способ лечения состояний, выбранных из группы, состоящей из ятрогенных и не ятрогенных психозов и галлюцинозов, включающий введение пациенту фармацевтически эффективного количества соединения или фармацевтически приемлемой соли по любому одному из пп.1-3.
22. Способ лечения состояний, выбранных из группы, состоящей из шизофрении и шизофреноподобных заболеваний, включающий введение пациенту фармацевтически эффективного количества соединения или фармацевтически приемлемой соли по любому одному из пп.1-3.
23. Способ лечения состояний, выбранных из группы, состоящей из расстройств настроения и тревожных состояний, включающий введение пациенту фармацевтически эффективного количества соединения или фармацевтически приемлемой соли по любому одному из пп.1-3.
24. Способ по п.23, где указанное расстройство настроения и тревожное состояние выбрано из группы, состоящей из маниакально-депрессивного заболевания, депрессии и обсессивно-компульсивной болезни.
25. Способ лечения состояний, выбранных из группы, состоящей из расстройств, связанных с дефицитом внимания, аутизмом и когнитивной дисфункцией, включающий введение пациенту фармацевтически эффективного количества соединения или фармацевтически приемлемой соли по любому одному из пп.1-3
26. Способ лечения заболевания Хантингтона, включающий введение пациенту фармацевтически эффективного количества соединения или фармацевтически приемлемой соли по любому одному из пп.1-3.
27. Способ лечения расстройств сна, включающий введение пациенту фармацевтически эффективного количества соединения или фармацевтически приемлемой соли по любому одному из пп.1-3.
28. Способ лечения расстройств, вызванных веществами, к которым относятся злоупотребление алкоголем или привыкание к лекарству, включающий введение пациенту фармацевтически эффективного количества соединения или фармацевтически приемлемой соли по любому одному из пп.1-3.
29. Способ по любому одному из пп.19-28, в котором вещество вводят орально.
30. Способ по любому одному из пп.19-28, в котором вещество вводят путем инъекции.
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