RU2008108618A - 3, 5-дизамещенные фенил-пиперидины в качестве модуляторов нейротрансмиссии допамина - Google Patents
3, 5-дизамещенные фенил-пиперидины в качестве модуляторов нейротрансмиссии допамина Download PDFInfo
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- RU2008108618A RU2008108618A RU2008108618/04A RU2008108618A RU2008108618A RU 2008108618 A RU2008108618 A RU 2008108618A RU 2008108618/04 A RU2008108618/04 A RU 2008108618/04A RU 2008108618 A RU2008108618 A RU 2008108618A RU 2008108618 A RU2008108618 A RU 2008108618A
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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
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 17
- 150000001875 compounds Chemical class 0.000 claims abstract 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 9
- 208000035475 disorder Diseases 0.000 claims abstract 9
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims abstract 4
- 208000012661 Dyskinesia Diseases 0.000 claims abstract 4
- 208000028017 Psychotic disease Diseases 0.000 claims abstract 4
- 210000003169 central nervous system Anatomy 0.000 claims abstract 4
- 208000015114 central nervous system disease Diseases 0.000 claims abstract 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims abstract 4
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims abstract 4
- 150000003839 salts Chemical class 0.000 claims abstract 4
- 208000012902 Nervous system disease Diseases 0.000 claims abstract 3
- PHRDGRSMZPOCAB-UHFFFAOYSA-N 1-ethyl-4-(3-fluoro-5-methylsulfonylphenyl)piperidine Chemical compound C1CN(CC)CCC1C1=CC(F)=CC(S(C)(=O)=O)=C1 PHRDGRSMZPOCAB-UHFFFAOYSA-N 0.000 claims abstract 2
- PKMDJEDRPXYECK-UHFFFAOYSA-N 4-(3-fluoro-5-methylsulfonylphenyl)-1-propylpiperidine Chemical compound C1CN(CCC)CCC1C1=CC(F)=CC(S(C)(=O)=O)=C1 PKMDJEDRPXYECK-UHFFFAOYSA-N 0.000 claims abstract 2
- 208000020925 Bipolar disease Diseases 0.000 claims abstract 2
- 208000014094 Dystonic disease Diseases 0.000 claims abstract 2
- 208000023105 Huntington disease Diseases 0.000 claims abstract 2
- 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 abstract 2
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims abstract 2
- 208000019430 Motor disease Diseases 0.000 claims abstract 2
- 208000018737 Parkinson disease Diseases 0.000 claims abstract 2
- 208000027089 Parkinsonian disease Diseases 0.000 claims abstract 2
- 206010034010 Parkinsonism Diseases 0.000 claims abstract 2
- 206010044565 Tremor Diseases 0.000 claims abstract 2
- 239000003085 diluting agent Substances 0.000 claims abstract 2
- 239000003937 drug carrier Substances 0.000 claims abstract 2
- 208000010118 dystonia Diseases 0.000 claims abstract 2
- 230000000642 iatrogenic effect Effects 0.000 claims abstract 2
- 238000004519 manufacturing process Methods 0.000 claims abstract 2
- 238000002360 preparation method Methods 0.000 claims abstract 2
- 201000000980 schizophrenia Diseases 0.000 claims abstract 2
- 239000000126 substance Substances 0.000 claims 3
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 2
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims 2
- 206010012289 Dementia Diseases 0.000 claims 2
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 2
- 230000006931 brain damage Effects 0.000 claims 2
- 231100000874 brain damage Toxicity 0.000 claims 2
- 208000029028 brain injury Diseases 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 206010003805 Autism Diseases 0.000 claims 1
- 208000020706 Autistic disease Diseases 0.000 claims 1
- 208000020401 Depressive disease Diseases 0.000 claims 1
- 208000030814 Eating disease Diseases 0.000 claims 1
- 208000027534 Emotional disease Diseases 0.000 claims 1
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 1
- 201000004311 Gilles de la Tourette syndrome Diseases 0.000 claims 1
- 206010019233 Headaches Diseases 0.000 claims 1
- 206010020852 Hypertonia Diseases 0.000 claims 1
- 206010021143 Hypoxia Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 208000019022 Mood disease Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 206010033799 Paralysis Diseases 0.000 claims 1
- 208000000323 Tourette Syndrome Diseases 0.000 claims 1
- 208000016620 Tourette disease Diseases 0.000 claims 1
- 230000007000 age related cognitive decline Effects 0.000 claims 1
- 230000003920 cognitive function Effects 0.000 claims 1
- 230000001054 cortical effect Effects 0.000 claims 1
- 235000014632 disordered eating Nutrition 0.000 claims 1
- 231100000317 environmental toxin Toxicity 0.000 claims 1
- 231100000869 headache Toxicity 0.000 claims 1
- 230000001146 hypoxic effect Effects 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000002458 infectious effect Effects 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 230000002503 metabolic effect Effects 0.000 claims 1
- 230000007659 motor function Effects 0.000 claims 1
- 230000001613 neoplastic effect Effects 0.000 claims 1
- 210000000653 nervous system Anatomy 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 230000036407 pain Effects 0.000 claims 1
- 208000012201 sexual and gender identity disease Diseases 0.000 claims 1
- 208000015891 sexual disease Diseases 0.000 claims 1
- 208000019116 sleep disease Diseases 0.000 claims 1
- 201000009032 substance abuse Diseases 0.000 claims 1
- 231100000736 substance abuse Toxicity 0.000 claims 1
- 208000011117 substance-related disease Diseases 0.000 claims 1
- 231100000331 toxic Toxicity 0.000 claims 1
- 230000002588 toxic effect Effects 0.000 claims 1
- 230000000472 traumatic effect Effects 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—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
- C07D211/08—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
- C07D211/18—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
- 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
- C07D211/24—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 by sulfur atoms to which a second hetero atom is attached
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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
- A61K31/435—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
- A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
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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
- A61K31/435—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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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- A61P25/00—Drugs for disorders of the nervous system
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- A61P25/16—Anti-Parkinson drugs
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A61P25/20—Hypnotics; Sedatives
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- Hydrogenated Pyridines (AREA)
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Abstract
1. Соединение формулы 1: ! , ! где R выбран из группы, состоящей из С1-С3алкилов и аллила, и его фармацевтически приемлемые соли. ! 2. Соединение по п.1, где R выбран из группы, состоящей из н-пропила и этила. ! 3. Соединение по п.1, выбранное из группы, включающей: ! 1-этил-4-[3-фтор-5-(метилсульфонил)фенил]пиперидин, ! 4-[3-фтор-5-(метилсульфонил)фенил]-1-пропилпиперидин, ! 1-аллил-4-[3-фтор-5-(метилсульфонил)фенил]пиперидин. ! 4. Соединение по любому из пп.1-3 для лечения расстройства центральной нервной системы. ! 5. Применение соединения формулы 1: ! , ! где R выбран из группы, состоящей из C1-С3алкилов и аллила, или его фармацевтически приемлемой соли для изготовления фармацевтически активных препаратов для лечения расстройства центральной нервной системы. ! 6. Применение по п.5, где R выбран из группы, состоящей из н-пропила и этила. ! 7. Фармацевтическая композиция, содержащая соединение по любому из пп.1-3 и один или более фармацевтически приемлемых носителей или разбавителей. ! 8. Фармацевтическая композиция по п.7 для лечения расстройства центральной нервной системы. ! 9. Фармацевтическая композиция по п.7 для лечения двигательных расстройств, выбранных из группы, состоящей из болезни Паркинсона, паркинсонизма, дискинезий (включая дискинезии, индуцированные L-DOPA), дистоний, тиков, тремора и болезни Гентингтона. ! 10. Фармацевтическая композиция по п.7 для лечения состояния, выбранного из группы, состоящей из ятрогенных и неятрогенных психозов и галлюцинозов. ! 11. Фармацевтическая композиция по п.7 для лечения состояния, выбранного из группы, состоящей из шизофрении и шизофреноформных расстройств и биполярного расстройства. ! 12. Фармацевтическая композиц
Claims (19)
2. Соединение по п.1, где R выбран из группы, состоящей из н-пропила и этила.
3. Соединение по п.1, выбранное из группы, включающей:
1-этил-4-[3-фтор-5-(метилсульфонил)фенил]пиперидин,
4-[3-фтор-5-(метилсульфонил)фенил]-1-пропилпиперидин,
1-аллил-4-[3-фтор-5-(метилсульфонил)фенил]пиперидин.
4. Соединение по любому из пп.1-3 для лечения расстройства центральной нервной системы.
6. Применение по п.5, где R выбран из группы, состоящей из н-пропила и этила.
7. Фармацевтическая композиция, содержащая соединение по любому из пп.1-3 и один или более фармацевтически приемлемых носителей или разбавителей.
8. Фармацевтическая композиция по п.7 для лечения расстройства центральной нервной системы.
9. Фармацевтическая композиция по п.7 для лечения двигательных расстройств, выбранных из группы, состоящей из болезни Паркинсона, паркинсонизма, дискинезий (включая дискинезии, индуцированные L-DOPA), дистоний, тиков, тремора и болезни Гентингтона.
10. Фармацевтическая композиция по п.7 для лечения состояния, выбранного из группы, состоящей из ятрогенных и неятрогенных психозов и галлюцинозов.
11. Фармацевтическая композиция по п.7 для лечения состояния, выбранного из группы, состоящей из шизофрении и шизофреноформных расстройств и биполярного расстройства.
12. Фармацевтическая композиция по п.7 для лечения состояния, выбранного из группы, состоящей из расстройства настроения и тревожного расстройства, депрессии и обсессивно-компульсивного расстройства.
13. Фармацевтическая композиция по п.7 для лечения расстройств развития нервной системы, выбранных из группы, состоящей из расстройств типа аутизма, ADHD (синдром дефицита внимания с гиперактивностью), коркового паралича, синдрома Жиля де ля Туретта, и нейродегенеративных расстройств, выбранных из группы, состоящей из деменции и возрастного ухудшения когнитивных функций.
14. Фармацевтическая композиция по п.7 для лечения состояния, выбранного из группы, состоящей из расстройств сна, сексуальных расстройств, расстройств приема пищи, ожирения и головных болей или других болей при состояниях, характеризующихся повышенным мышечным тонусом.
15. Фармацевтическая композиция по п.7 для улучшения двигательных функций, когнитивных функций и родственных эмоциональных расстройств, и после повреждения мозга, вызванного травматическими, воспалительными, инфекционными, неопластическими, сосудистыми, гипоксическими или метаболическими причинами, или повреждения мозга, вызванного токсическими реакциями на экзогенные химические вещества, где экзогенные химические вещества выбраны из группы, состоящей из веществ, которыми злоупотребляют, фармацевтических соединений, токсинов окружающей среды.
16. Фармацевтическая композиция по п.7 для лечения расстройства, связанного со злоупотреблением веществом.
17. Фармацевтическая композиция по п.7 для лечения болезни Альцгеймера или родственных расстройств с деменцией.
18. Способ лечения расстройств центральной нервной системы путем введения терапевтически активного количества соединения по пп.1-3 млекопитающему, включая человека, страдающему таким расстройством центральной нервной системы.
19. Способ по п.18 для лечения расстройства, определенного в одном или более пп.7-17.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
SE0502254A SE529246C2 (sv) | 2005-10-13 | 2005-10-13 | Nya disubstituerade fenyl-piperidiner som modulatorer för dopaminneurotransmission |
SE0502254.6 | 2005-10-13 |
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RU2008108618A true RU2008108618A (ru) | 2009-11-20 |
RU2418787C2 RU2418787C2 (ru) | 2011-05-20 |
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RU2008108618/04A RU2418787C2 (ru) | 2005-10-13 | 2006-10-12 | 3,5-дизамещенные фенилпиперидины в качестве модуляторов нейротрансмиссии допамина |
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Country | Link |
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US (1) | US8501777B2 (ru) |
EP (1) | EP1948606B1 (ru) |
JP (1) | JP4857346B2 (ru) |
KR (1) | KR20080046720A (ru) |
CN (1) | CN101273014B (ru) |
AT (1) | ATE494277T1 (ru) |
AU (1) | AU2006301432B2 (ru) |
BR (1) | BRPI0617355A2 (ru) |
CA (1) | CA2625663A1 (ru) |
DE (1) | DE602006019470D1 (ru) |
DK (1) | DK1948606T3 (ru) |
ES (1) | ES2358537T3 (ru) |
HR (1) | HRP20110196T1 (ru) |
IL (1) | IL189298A0 (ru) |
MY (1) | MY143241A (ru) |
NO (1) | NO20082174L (ru) |
NZ (1) | NZ566015A (ru) |
PL (1) | PL1948606T3 (ru) |
RU (1) | RU2418787C2 (ru) |
SE (1) | SE529246C2 (ru) |
UA (1) | UA93380C2 (ru) |
WO (1) | WO2007042295A1 (ru) |
ZA (1) | ZA200802238B (ru) |
Families Citing this family (17)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SE9904723D0 (sv) | 1999-12-22 | 1999-12-22 | Carlsson A Research Ab | New modulators of dopamine neurotransmission II |
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EP1948606A1 (en) | 2008-07-30 |
CA2625663A1 (en) | 2007-04-19 |
IL189298A0 (en) | 2008-06-05 |
HK1125097A1 (en) | 2009-07-31 |
AU2006301432A1 (en) | 2007-04-19 |
AU2006301432B2 (en) | 2011-12-15 |
HRP20110196T1 (hr) | 2011-05-31 |
ZA200802238B (en) | 2009-10-28 |
CN101273014B (zh) | 2011-01-12 |
EP1948606B1 (en) | 2011-01-05 |
UA93380C2 (en) | 2011-02-10 |
SE529246C2 (sv) | 2007-06-12 |
KR20080046720A (ko) | 2008-05-27 |
PL1948606T3 (pl) | 2011-08-31 |
WO2007042295A1 (en) | 2007-04-19 |
NO20082174L (no) | 2008-07-11 |
DK1948606T3 (da) | 2011-04-04 |
US8501777B2 (en) | 2013-08-06 |
RU2418787C2 (ru) | 2011-05-20 |
MY143241A (en) | 2011-04-15 |
NZ566015A (en) | 2010-11-26 |
DE602006019470D1 (de) | 2011-02-17 |
JP4857346B2 (ja) | 2012-01-18 |
ATE494277T1 (de) | 2011-01-15 |
BRPI0617355A2 (pt) | 2011-07-26 |
US20080234321A1 (en) | 2008-09-25 |
CN101273014A (zh) | 2008-09-24 |
SE0502254L (sv) | 2007-04-14 |
ES2358537T3 (es) | 2011-05-11 |
JP2009511525A (ja) | 2009-03-19 |
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