RU2014113548A - Нейроактивные стероиды, композиции и их применения - Google Patents
Нейроактивные стероиды, композиции и их применения Download PDFInfo
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- RU2014113548A RU2014113548A RU2014113548/04A RU2014113548A RU2014113548A RU 2014113548 A RU2014113548 A RU 2014113548A RU 2014113548/04 A RU2014113548/04 A RU 2014113548/04A RU 2014113548 A RU2014113548 A RU 2014113548A RU 2014113548 A RU2014113548 A RU 2014113548A
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- substituted
- compound
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- hydrogen
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- 239000000203 mixture Substances 0.000 title 1
- 150000003431 steroids Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 46
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 27
- 239000001257 hydrogen Substances 0.000 claims abstract 27
- 125000000217 alkyl group Chemical group 0.000 claims abstract 18
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 13
- 150000003839 salts Chemical class 0.000 claims abstract 9
- 229910052736 halogen Inorganic materials 0.000 claims abstract 7
- 150000002367 halogens Chemical group 0.000 claims abstract 7
- 150000002431 hydrogen Chemical group 0.000 claims abstract 7
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 7
- 125000002947 alkylene group Chemical group 0.000 claims abstract 4
- 125000003342 alkenyl group Chemical group 0.000 claims abstract 3
- 125000000304 alkynyl group Chemical group 0.000 claims abstract 3
- 125000004043 oxo group Chemical group O=* 0.000 claims abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
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- 238000000034 method Methods 0.000 claims 5
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 4
- 230000009529 traumatic brain injury Effects 0.000 claims 4
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- 208000029560 autism spectrum disease Diseases 0.000 claims 2
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- 125000004474 heteroalkylene group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 208000028173 post-traumatic stress disease Diseases 0.000 claims 2
- 201000000980 schizophrenia Diseases 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
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- 208000020706 Autistic disease Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 206010010904 Convulsion Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 206010012335 Dependence Diseases 0.000 claims 1
- 206010049119 Emotional distress Diseases 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 208000019022 Mood disease Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 claims 1
- 206010041250 Social phobia Diseases 0.000 claims 1
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 claims 1
- 208000009205 Tinnitus Diseases 0.000 claims 1
- 206010048010 Withdrawal syndrome Diseases 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 125000004452 carbocyclyl group Chemical group 0.000 claims 1
- 229960003920 cocaine Drugs 0.000 claims 1
- 230000009429 distress Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000024732 dysthymic disease Diseases 0.000 claims 1
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- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 206010022437 insomnia Diseases 0.000 claims 1
- 206010027175 memory impairment Diseases 0.000 claims 1
- 238000012544 monitoring process Methods 0.000 claims 1
- 229940127240 opiate Drugs 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 208000022821 personality disease Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 208000022610 schizoaffective disease Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 231100000886 tinnitus Toxicity 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 abstract 6
- 125000004450 alkenylene group Chemical group 0.000 abstract 2
- 125000004419 alkynylene group Chemical group 0.000 abstract 2
- 0 CC(CCC(*)(C(F)(F)F)C(F)(F)F)C(CC1)C(C)(CC2)C1C1C2C(C)(CC[C@](C2)O)C2=CC1 Chemical compound CC(CCC(*)(C(F)(F)F)C(F)(F)F)C(CC1)C(C)(CC2)C1C1C2C(C)(CC[C@](C2)O)C2=CC1 0.000 description 2
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- KDXZYACKHRNMSB-RTQKIXDOSA-N CC(CCC(C)(C)O)[C@@H](CC1)[C@@](C)(CC2)C1C1C2[C@@H](CC[C@@H](C2)S)C2=CC1 Chemical compound CC(CCC(C)(C)O)[C@@H](CC1)[C@@](C)(CC2)C1C1C2[C@@H](CC[C@@H](C2)S)C2=CC1 KDXZYACKHRNMSB-RTQKIXDOSA-N 0.000 description 1
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- KEXGJVHTVFVZAK-PCNQZJBLSA-N C[C@H](CCC(C)(C)N)[C@@H](CC1)[C@@](C)(CC2)C1C1C2[C@@](C)(CC[C@@H](C2)O)C2=CC1 Chemical compound C[C@H](CCC(C)(C)N)[C@@H](CC1)[C@@](C)(CC2)C1C1C2[C@@](C)(CC[C@@H](C2)O)C2=CC1 KEXGJVHTVFVZAK-PCNQZJBLSA-N 0.000 description 1
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- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
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- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
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- C—CHEMISTRY; METALLURGY
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- C07J—STEROIDS
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- C07J—STEROIDS
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- C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
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- C—CHEMISTRY; METALLURGY
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- C07J—STEROIDS
- C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
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- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
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- C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
- C07J41/0011—Unsubstituted amino radicals
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- C—CHEMISTRY; METALLURGY
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- C07J—STEROIDS
- C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
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- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
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- C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
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- C07J9/005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton
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- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
1. Соединение формулы:или его фармацевтически приемлемая соль;где Z представляет собой группу формул (i), (ii), (iii), (iv) или (v):Lи Lвыбраны из группы, состоящей из связи, замещенного или незамещенного C-Салкилена, замещенного или незамещенного C-Салкенилена, замещенного или незамещенного C-Салкинилена, замещенного или незамещенного гетеро(C-C)алкилена, замещенного или незамещенного гетеро(C-C)алкенилена и замещенного или незамещенного гетеро(C-C)алкинилена;Lпредставляет собой замещенный или незамещенный C-Салкилен, замещенный или незамещенный C-Салкенилен, замещенный или незамещенный C-Салкинилен, замещенный или незамещенный гетеро(C-C)алкилен, замещенный или незамещенный гетеро(C-C)алкенилен или замещенный или незамещенный гетеро(C-C)алкинилен;каждый из Xи Xнезависимо представляет собой -O-, -S- или -NH-;Rпредставляет собой водород или замещенный или незамещенный алкил;Rпредставляет собой водород;Rпредставляет собой водород, замещенный или незамещенный алкил, замещенный или незамещенный алкенил или замещенный или незамещенный алкинил;каждый из R, Rи Rнезависимо представляет собой водород или -OR, где Rпредставляет собой водород или замещенный или незамещенный алкил, или Rи Rсвязаны с образованием оксогруппы (=O);каждый из Rи Rнезависимо представляет собой водород, галоген или замещенный или незамещенный алкил, ипредставляет собой одинарную или двойную связь при условии, что если содержится двойная связь, то один из Rили Rотсутствует, и при условии, что если содержится одинарная связь, то водород при C5 находится в альфа- или бета-положении;каждый из Rи Rнезависимо представляет собой водород или -CH,и каждый из Rи Rнезависимо представляет
Claims (41)
1. Соединение формулы:
или его фармацевтически приемлемая соль;
где Z представляет собой группу формул (i), (ii), (iii), (iv) или (v):
L1 и L2 выбраны из группы, состоящей из связи, замещенного или незамещенного C1-С6алкилена, замещенного или незамещенного C2-С6алкенилена, замещенного или незамещенного C2-С6алкинилена, замещенного или незамещенного гетеро(C1-C6)алкилена, замещенного или незамещенного гетеро(C2-C6)алкенилена и замещенного или незамещенного гетеро(C2-C6)алкинилена;
L3 представляет собой замещенный или незамещенный C1-С6алкилен, замещенный или незамещенный C2-С6алкенилен, замещенный или незамещенный C2-С6алкинилен, замещенный или незамещенный гетеро(C1-C6)алкилен, замещенный или незамещенный гетеро(C2-C6)алкенилен или замещенный или незамещенный гетеро(C2-C6)алкинилен;
каждый из X1 и X2 независимо представляет собой -O-, -S- или -NH-;
R1 представляет собой водород или замещенный или незамещенный алкил;
R3b представляет собой водород;
R3a представляет собой водород, замещенный или незамещенный алкил, замещенный или незамещенный алкенил или замещенный или незамещенный алкинил;
каждый из R2, R11a и R11b независимо представляет собой водород или -ORB1, где RB1 представляет собой водород или замещенный или незамещенный алкил, или R11a и R11b связаны с образованием оксогруппы (=O);
каждый из R6a и R6b независимо представляет собой водород, галоген или замещенный или незамещенный алкил, и представляет собой одинарную или двойную связь при условии, что если содержится двойная связь, то один из R6a или R6b отсутствует, и при условии, что если содержится одинарная связь, то водород при C5 находится в альфа- или бета-положении;
каждый из R19 и R20 независимо представляет собой водород или -CH3,
и каждый из R23a и R23b независимо представляет собой водород, галоген или замещенный или незамещенный алкил, или R23a и R23b связаны друг с другом с образованием замещенного или незамещенного C3-С6циклоалкила;
R24 представляет собой водород или замещенный или незамещенный алкил;
Y представляет собой -O-, -S- или -NRZ5-;
RZ4 независимо представляет собой замещенный или незамещенный алкил, замещенный или незамещенный алкенил, замещенный или незамещенный алкинил, замещенный или незамещенный карбоциклил, замещенный или незамещенный гетероциклил, замещенный или незамещенный арил, замещенный или незамещенный гетероарил, -ORZ5, -SRZ5 или -N(RZ5)2;
каждый из RZ5 независимо представляет собой водород или замещенный или незамещенный алкил, и
каждый из RZ6 независимо представляет собой водород или замещенный или незамещенный алкил, или две группы RZ6 связаны с образованием C3-6карбоциклического кольца, и
нижний индекс n равен 0 или 1;
при условии, что следующие ниже соединения конкретно исключают:
11. Соединение по п. 10, где Y представляет собой -O-, и L3 представляет собой алкиленовую или гетероалкиленовую группу.
14. Соединение по п. 13, где Y представляет собой -O-, и L3 представляет собой алкилен или гетероалкилен.
16. Соединение по п. 1, где группа -X1R3b находится в бета-положении, и R3a находится в альфа-положении.
17. Соединение по п. 1, где -X1R3b представляет собой -OH.
18. Соединение по п. 1, где R3a представляет собой водород.
19. Соединение по п. 1, где R3a представляет собой замещенный или незамещенный алкил.
21. Соединение по п. 1, где R6b представляет собой галоген или замещенный или незамещенный алкил.
22. Соединение по п. 1, где R2 представляет собой водород.
23. Соединение по п. 1, где R2 представляет собой -ORB.
24. Соединение по п. 1, где R11b представляет собой водород или -ORB, и R11a представляет собой водород.
25. Соединение по п. 1, где R11a и R11b совместно образуют оксогруппу.
28. Соединение по п. 1, где R19 представляет собой -CH3.
36. Фармацевтическая композиция, содержащая фармацевтически приемлемый носитель и эффективное количество соединения по любому из предшествующих пунктов.
37. Способ профилактики, лечения, улучшения состояния или контроля заболевания или патологического состояния, который включает введение пациенту, нуждающемуся в такой профилактике, лечении, улучшении состояния или контроле, профилактически или терапевтически эффективного количества соединения или фармацевтической композиции по любому из предшествующих пунктов.
38. Способ по п. 37, где заболевание или патологическое состояние представляет собой шизофрению, депрессию, биполярное расстройство (например, I и/или II), шизоаффективное расстройство, расстройства настроения, тревожные расстройства, расстройства личности, психозы, компульсивные расстройства, посттравматическое стрессовое расстройство (PTSD), расстройства аутистического спектра (ASD), дистимию (легкую степень депрессии), социальное тревожное расстройство, обсессивно-компульсивное расстройство (OCD), все болевые синдромы или расстройства, расстройства сна, нарушения памяти, деменцию, включая болезнь Альцгеймера, эпилепсию и любые судорожные расстройства, травматическое повреждение головного мозга (TBI), инсульт, аддиктивные расстройства, включая пристрастие к опиатам, кокаину и алкоголю, аутизм, болезнь Гентингтона, бессонницу, болезнь Паркинсона, абстинентные синдромы или тиннитус.
39. Способ по п. 38, где заболевание или патологическое состояние представляет собой шизофрению.
40. Способ по п. 38, где заболевание или патологическое состояние представляет собой травматическое повреждение головного мозга (TBI).
41. Способ по п. 38, где заболевание или патологическое состояние представляет собой инсульт.
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