RU2021114918A - Композиции и способы лечения хронической боли - Google Patents

Композиции и способы лечения хронической боли Download PDF

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RU2021114918A
RU2021114918A RU2021114918A RU2021114918A RU2021114918A RU 2021114918 A RU2021114918 A RU 2021114918A RU 2021114918 A RU2021114918 A RU 2021114918A RU 2021114918 A RU2021114918 A RU 2021114918A RU 2021114918 A RU2021114918 A RU 2021114918A
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acid
pain
administration
pharmaceutical composition
pain associated
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Махеш КАНДУЛА
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Целликс Био Прайвет Лимитед
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Claims (41)

1. Соединение с формулой V,
Figure 00000001
Формула V,
и его фармацевтически приемлемые гидраты, сольваты, пролекарства, энантиомеры и стереоизомеры;
где
RH независимо представляет собой
фосфолипиды, фосфатидилхолин, ментол, ретиноевую кислоту, витамин А, ретинол, ретиналь, изотретиноин, куркумин, третиноин, α-каротин β-каротин ретинол, эргостерол d2, эргокальциферол, 7-дегидрохолестерин, холекальциферол, 25-гидроксихолекальциферол, кальцитриол (1,25-дигидроксихолекальциферол), кальцитроевую кислоту, дигидроэргокальциферол d4, альфакальцидол, дигидротахистерол, кальципотриол, такальцитол, парикальцитол, токоферол, нафтохинон, филлохинон (k1), менахиноны (k2), менадион (k3), менадиол (k4), тиамин, ацефуртиамин, аллитиамин, бенфотиамин, фурсультиамин, октотиамин, просультиамин, сульбутиамин, рибофлавин, ниацин, никотинамид, пантотеновую кислоту, декспантенол, пантетин, пиридоксин, пиридоксальфосфат, пиридоксамин, пиритинол, биотин, фолиевую кислоту, дигидрофолиевую кислоту, фолиновую кислоту, левомефолиевую кислоту, аденозилкобаламин, цианокобаламин, гидроксокобаламин, метилкобаламин, холин, аскорбиновую кислоту, дегидроаскорбиновую кислоту, 1-докозанол или
Figure 00000002
;
где при условии, что R1, R2, R3 независимо представляет собой
Figure 00000003
,
Figure 00000004
,
Figure 00000005
,
Figure 00000006
,
Figure 00000007
,
Figure 00000008
,
Figure 00000009
,
Figure 00000010
,
Figure 00000011
,
Figure 00000012
,
Figure 00000013
,
Figure 00000014
,
Figure 00000015
,
Figure 00000016
,
Figure 00000017
,
Figure 00000018
,
Figure 00000019
,
Figure 00000020
или
Figure 00000021
.
2. Соединение с формулой VII,
Figure 00000022
Формула VII,
и его фармацевтически приемлемые гидраты, сольваты, пролекарства, энантиомеры и стереоизомеры;
где
RH независимо представляет собой
каприловую кислоту, 1-гидрокси-2-нафтойную кислоту, 2,2-дихлоруксусную кислоту, 2-гидроксиэтансульфоновую кислоту, 2-оксоглутаровую кислоту, 4-ацетамидобензойную кислоту, 4-аминосалициловую кислоту, уксусную кислоту, адипиновую кислоту, аскорбиновую кислоту, аспарагиновую кислоту, бензолсульфоновую кислоту, бензойную кислоту, камфорную кислоту, камфора-10-сульфоновую кислоту, каприновую кислоту (декановую кислоту), капроновую кислоту (гексановую кислоту), угольную кислоту, коричную кислоту, лимонную кислоту, цикламиновую кислоту, додецилсерную кислоту, этан-1,2-дисульфокислоту, этансульфоновую кислоту, муравьиную кислоту, фумаровую кислоту, галактаровую кислоту, гентизиновую кислоту, глюкогептоновую кислоту, глюконовую кислоту, глюкуроновую кислоту, глутаминовую кислоту, глутаровую кислоту, глицерофосфорную кислоту, гликолевую кислоту, гиппуровую кислоту, бромистоводородную кислоту, изомасляную кислоту, молочную кислоту, лактобионовую кислоту, лауриновую кислоту, малеиновую кислоту, яблочную кислоту, малоновую кислоту, миндальную кислоту, метансульфоновую кислоту, нафталин-1,5-дисульфоновую кислоту, нафталин-2-сульфоновую кислоту, никотиновую кислоту, азотную кислоту, олеиновую кислоту, щавелевую кислоту, пальмитиновую кислоту, памоевую кислоту, фосфорную кислоту, пропионовую кислоту, пироглутаминовую кислоту, салициловую кислоту, себациновую кислоту, стеариновую кислоту, янтарную кислоту, серную кислоту, винную кислоту, тиоциановую кислоту, толуолсульфоновую кислоту, ундециленовую кислоту, жирные кислоты омега-3, жирные кислоты омега-6, н-ацетилцистеин (nac), фуроат, метилфуроат, этилфуроат, аминокапроновую кислоту, капроновую кислоту, каприловую кислоту, каприновую кислоту, лауриновую кислоту, альфа-липоевую кислоту, R-липоевую кислоту, миристиновую кислоту, миристоленовую кислоту, пальмитиновую кислоту, пальмитолеиновую кислоту, фосфолипиды, фосфатидилхолин, олеиновую кислоту, элаидиновую кислоту, линолевую кислоту, линоленовую кислоту, ментол, ретиноевую кислоту, витамин А, ретинол, линолэлаидиновую кислоту, арахидоновую кислоту, фосфолипиды, фосфатидилхолин, ментол, ретиноевую кислоту, витамин а, ретинол, ретиналь, изотретиноин, куркумин, третиноин, α-каротин β-каротин ретинол, эргостерол d2, эргокальциферол, 7-дегидрохолестерин, холекальциферол, 25-гидроксихолекальциферол, кальцитриол (1,25-дигидроксихолекальциферол), кальцитроевую кислоту, дигидроэргокальциферол d4, альфакальцидол, дигидротахистерол, кальципотриол, такальцитол, парикальцитол, токоферол, нафтохинон, филлохинон (k1), менахиноны (k2), менадион (k3), менадиол (k4), тиамин, ацефуртиамин, аллитиамин, бенфотиамин, фурсультиамин, октотиамин, просультиамин, сульбутиамин, рибофлавин, ниацин, никотинамид, пантотеновую кислоту, декспантенол, пантетин, пиридоксин, пиридоксальфосфат, пиридоксамин, пиритинол, биотин, фолиевую кислоту, дигидрофолиевую кислоту, фолиновую кислоту, левомефолиевую кислоту, аденозилкобаламин, цианокобаламин, гидроксокобаламин, метилкобаламин, холин, аскорбиновую кислоту, дегидроаскорбиновую кислоту, 1-докозанол или
Figure 00000002
;
где при условии, что R1, R2, R3 независимо представляет собой
Figure 00000023
,
Figure 00000024
,
Figure 00000005
,
Figure 00000006
,
Figure 00000007
,
Figure 00000008
,
Figure 00000009
,
Figure 00000010
,
Figure 00000011
,
Figure 00000012
,
Figure 00000013
,
Figure 00000014
,
Figure 00000015
,
Figure 00000016
,
Figure 00000017
,
Figure 00000018
,
Figure 00000019
,
Figure 00000020
или
Figure 00000021
.
3. Соединение с формулой VIII,
Figure 00000025
Формула VIII,
и его фармацевтически приемлемые гидраты, сольваты, пролекарства, энантиомеры и стереоизомеры;
где
RH независимо представляет собой
каприловую кислоту, 1-гидрокси-2-нафтойную кислоту, 2,2-дихлоруксусную кислоту, 2-гидроксиэтансульфоновую кислоту, 2-оксоглутаровую кислоту, 4-ацетамидобензойную кислоту, 4-аминосалициловую кислоту, уксусную кислоту, адипиновую кислоту, аскорбиновую кислоту, аспарагиновую кислоту, бензолсульфоновую кислоту, бензойную кислоту, камфорную кислоту, камфора-10-сульфоновую кислоту, каприновую кислоту (декановую кислоту), капроновую кислоту (гексановую кислоту), угольную кислоту, коричную кислоту, лимонную кислоту, цикламиновую кислоту, додецилсерную кислоту, этан-1,2-дисульфокислоту, этансульфоновую кислоту, муравьиную кислоту, фумаровую кислоту, галактаровую кислоту, гентизиновую кислоту, глюкогептоновую кислоту, глюконовую кислоту, глюкуроновую кислоту, глутаминовую кислоту, глутаровую кислоту, глицерофосфорную кислоту, гликолевую кислоту, гиппуровую кислоту, бромистоводородную кислоту, изомасляную кислоту, молочную кислоту, лактобионовую кислоту, лауриновую кислоту, малеиновую кислоту, яблочную кислоту, малоновую кислоту, миндальную кислоту, метансульфоновую кислоту, нафталин-1,5-дисульфоновую кислоту, нафталин-2-сульфоновую кислоту, никотиновую кислоту, азотную кислоту, олеиновую кислоту, щавелевую кислоту, пальмитиновую кислоту, памоевую кислоту, фосфорную кислоту, пропионовую кислоту, пироглутаминовую кислоту, салициловую кислоту, себациновую кислоту, стеариновую кислоту, янтарную кислоту, серную кислоту, винную кислоту, тиоциановую кислоту, толуолсульфоновую кислоту, ундециленовую кислоту, жирные кислоты омега-3, жирные кислоты омега-6, н-ацетилцистеин (nac), фуроат, метилфуроат, этилфуроат, аминокапроновую кислоту, капроновую кислоту, каприловую кислоту, каприновую кислоту, лауриновую кислоту, альфа-липоевую кислоту, R-липоевую кислоту, миристиновую кислоту, миристоленовую кислоту, пальмитиновую кислоту, пальмитолеиновую кислоту, фосфолипиды, фосфатидилхолин, олеиновую кислоту, элаидиновую кислоту, линолевую кислоту, линоленовую кислоту, ментол, ретиноевую кислоту, витамин А, ретинол, линолэлаидиновую кислоту, арахидоновую кислоту, фосфолипиды, фосфатидилхолин, ментол, ретиноевую кислоту, витамин а, ретинол, ретиналь, изотретиноин, куркумин, третиноин, α-каротин β-каротин ретинол, эргостерол d2, эргокальциферол, 7-дегидрохолестерин, холекальциферол, 25-гидроксихолекальциферол, кальцитриол (1,25-дигидроксихолекальциферол), кальцитроевую кислоту, дигидроэргокальциферол d4, альфакальцидол, дигидротахистерол, кальципотриол, такальцитол, парикальцитол, токоферол, нафтохинон, филлохинон (k1), менахиноны (k2), менадион (k3), менадиол (k4), тиамин, ацефуртиамин, аллитиамин, бенфотиамин, фурсультиамин, октотиамин, просультиамин, сульбутиамин, рибофлавин, ниацин, никотинамид, пантотеновую кислоту, декспантенол, пантетин, пиридоксин, пиридоксальфосфат, пиридоксамин, пиритинол, биотин, фолиевую кислоту, дигидрофолиевую кислоту, фолиновую кислоту, левомефолиевую кислоту, аденозилкобаламин, цианокобаламин, гидроксокобаламин, метилкобаламин, холин, аскорбиновую кислоту, дегидроаскорбиновую кислоту, 1-докозанол или
Figure 00000002
;
где при условии, что R1, R2, R3 независимо представляет собой
Figure 00000023
,
Figure 00000024
,
Figure 00000005
,
Figure 00000006
,
Figure 00000007
,
Figure 00000008
,
Figure 00000009
,
Figure 00000010
,
Figure 00000011
,
Figure 00000012
,
Figure 00000013
,
Figure 00000014
,
Figure 00000015
,
Figure 00000016
,
Figure 00000017
,
Figure 00000018
,
Figure 00000019
,
Figure 00000020
или
Figure 00000021
.
4. Фармацевтическая композиция для лечения боли, содержащая эффективное количество соединения по п. 1 и фармацевтически приемлемый носитель.
5. Фармацевтическая композиция для лечения боли, содержащая эффективное количество соединения по п. 2 и фармацевтически приемлемый носитель.
6. Фармацевтическая композиция для лечения боли, содержащая эффективное количество соединения по п. 3 и фармацевтически приемлемый носитель.
7. Фармацевтическая композиция по п. 4, которая составлена для перорального введения, отсроченного или замедленного высвобождения, трансмукозального введения, в виде сиропа, местного, парентерального введения, инъекции, подкожного, перорального раствора, ректального введения, трансбуккального введения или трансдермального введения.
8. Фармацевтическая композиция по п. 5, которая составлена для перорального введения, отсроченного или замедленного высвобождения, трансмукозального введения, в виде сиропа, местного, парентерального введения, инъекции, подкожного, перорального раствора, ректального введения, трансбуккального введения или трансдермального введения.
9. Фармацевтическая композиция по п. 6, которая составлена для перорального введения, отсроченного или замедленного высвобождения, трансмукозального введения, в виде сиропа, местного, парентерального введения, инъекции, подкожного, перорального раствора, ректального введения, трансбуккального введения или трансдермального введения.
10. Фармацевтическая композиция по п. 7, где боль выбрана из хронической боли, боли, связанной с хирургической операцией, боли, связанной с раной, боли, связанной с язвой, нейропатической боли, боли в результате повреждения нерва центральной и периферической нервной системы.
11. Фармацевтическая композиция по п. 8, где боль выбрана из хронической боли, боли, связанной с хирургической операцией, боли, связанной с раной, боли, связанной с язвой, нейропатической боли, боли в результате повреждения нерва центральной и периферической нервной системы.
12. Фармацевтическая композиция по п. 9, где боль выбрана из хронической боли, боли, связанной с хирургической операцией, боли, связанной с раной, боли, связанной с язвой, нейропатической боли, боли в результате повреждения нерва центральной и периферической нервной системы.
13. Соединение по п. 1, характеризующееся формулой V,
Figure 00000026
.
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US11000487B2 (en) 2021-05-11
ZA201904653B (en) 2020-03-25
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AU2022201457A1 (en) 2022-03-24
AU2017385977B2 (en) 2022-03-17
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AU2017385977A1 (en) 2019-08-01
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BR112019013192A2 (pt) 2019-12-10
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