RU2016116516A - Композиции ингибиторов тирозинкиназных рецепторов белков - Google Patents
Композиции ингибиторов тирозинкиназных рецепторов белков Download PDFInfo
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- RU2016116516A RU2016116516A RU2016116516A RU2016116516A RU2016116516A RU 2016116516 A RU2016116516 A RU 2016116516A RU 2016116516 A RU2016116516 A RU 2016116516A RU 2016116516 A RU2016116516 A RU 2016116516A RU 2016116516 A RU2016116516 A RU 2016116516A
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- Prior art keywords
- pain
- substituted
- group
- aryl
- heteroaryl
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- 239000003112 inhibitor Substances 0.000 title claims 3
- 208000002193 Pain Diseases 0.000 claims 32
- 125000001072 heteroaryl group Chemical group 0.000 claims 30
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 24
- 150000001875 compounds Chemical class 0.000 claims 23
- 239000002552 dosage form Substances 0.000 claims 23
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 21
- 125000003277 amino group Chemical group 0.000 claims 18
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 18
- -1 hydrocarbon radical Chemical class 0.000 claims 17
- 239000008194 pharmaceutical composition Substances 0.000 claims 16
- 125000004432 carbon atom Chemical group C* 0.000 claims 15
- 229910052739 hydrogen Inorganic materials 0.000 claims 15
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- 125000004122 cyclic group Chemical group 0.000 claims 9
- 229910052736 halogen Inorganic materials 0.000 claims 9
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- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 9
- 229910052757 nitrogen Inorganic materials 0.000 claims 9
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- 101150111783 NTRK1 gene Proteins 0.000 claims 3
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
- C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 radicals, substituted by hetero atoms, attached to ring carbon atoms
- C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/06—Peri-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/40—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
- 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
- A61K31/404—Indoles, e.g. pindolol
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4355—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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Claims (111)
1. Фармацевтическая композиция, содержащая терапевтически эффективное количество соединения структурной формулы (VIa.11):
где:
nn представляет собой целое число от 0 до 4;
A64 представляет собой O или S;
A65 представляет собой N или CR1;
A66 представляет собой NR73 или CR73R74;
Y представляет собой O, S, NR6 или C(R6R7);
каждый из R1, R5, R6 и R7 независимо представляет собой водород, галоген, алкил, замещенный алкил, арил, замещенный арил, гетероарил или замещенный гетероарил;
R72 независимо представляет собой водород, аминогруппу, замещенную аминогруппу, сульфонил, замещенный сульфонил, замещенный или незамещенный, насыщенный или ненасыщенный, разветвленный, неразветвленный или циклический одновалентный углеводородный радикал, содержащий от 1 до 20 атомов углерода, гетероарил, замещенный гетероарил, арил или арил, в котором один атом водорода заменен на заместитель, и где гетероарильная группа выбрана из группы, состоящей из акридина, β-карболина, хромана, хромена, циннолина, фурана, имидазола, индазола, индола, индолина, индолизина, изобензофурана, изохромена, изоиндола, изоиндолина, изохинолина, изотиазола, изоксазола, нафтиридина, оксадиазола, оксазола, перимидина, фенантридина, фенантролина, феназина, фталазина, птеридина, пурина, пирана, пиразина, пиразола, пиридазина, пиридина, пиримидина, пиррола, пирролизина, хиназолина, хинолина, хинолизина, хиноксалина, тетразола, тиадиазола, тиазола, тиофена, триазола, ксантена, флуоридина;
R73 независимо представляет собой водород, аминогруппу, замещенную аминогруппу, сульфонил, замещенный сульфонил, замещенный или незамещенный, насыщенный или ненасыщенный, разветвленный, неразветвленный или циклический одновалентный углеводородный радикал, содержащий от 1 до 20 атомов углерода, гетероарил, замещенный гетероарил, арил или арил, в котором один атом водорода заменен на заместитель;
R74 независимо представляет собой водород, аминогруппу, замещенную аминогруппу, сульфонил, замещенный сульфонил, замещенный или незамещенный, насыщенный или ненасыщенный, разветвленный, неразветвленный или циклический одновалентный углеводородный радикал, содержащий от 1 до 20 атомов углерода, гетероарил, замещенный гетероарил, арил или арил, в котором один атом водорода заменен на заместитель;
где заместители для насыщенных атомов углерода выбраны из группы -Ra, галоген, -O-, =O, -ORb, -SRb, -S-, =S, -NRcRc, =NRb, =N-ORb, тригалогенметил, -CF3, -CN, -OCN, -SCN, -NO, -NO2, =N2, -N3, -S(O)2Rb, -S(O)2O-, -S(O)2ORb, -OS(O)2Rb, -OS(O)2ORb, -P(O)(O-)2 ,-P(O)(ORb)(O-), -P(O)(ORb)(ORb), -C(O)Rb, -C(S)Rb, -C(NRb)Rb, -C(O)O-, -C(O)ORb, -C(S)ORb, -C(O)NRcRc, -OC(O)Rb, -OC(S)Rb, -OC(O)O-, -OC(O)ORb, -OC(S)ORb, -NRbC(O)Rb, - NRbC(S)Rb, -NRbC(O)O-, -NRbC(O)ORb, -NRbC(S)ORb, -NRbC(O)NRcRc, -NRbC(NRb)Rb и -NRbC(NRb)NRcRc, где Ra выбран из группы, состоящей из алкила, арилалкила, алкилдиила, арила, гетероалкила, замещенного гетероалкила, гетероалкилдиила, гетероарила, гетероарилалкила; каждый из Rb независимо представляет собой водород или Ra; и каждый из Rc независимо представляет собой Rb, или, альтернативно, два радикала Rc вместе с атомом азота, к которому они присоединены, образуют циклогетероалкильное кольцо, которое может включать от 1 до 4 одинаковых или разных дополнительных гетероатомов, выбранных из группы, состоящей из O, N и S;
где заместители для ненасыщенных атомов углерода выбраны из группы -Ra, галоген, -O-, -ORb, -SRb, -S-,-NRcRc, -CN, -OCN, -SCN, -NO, -NO2, -N3, -S(O)2Rb, -S(O)2O-, -S(O)2ORb, -OS(O)2Rb, -OS(O)2ORb, -P(O)(O-)2 ,-P(O)(ORb)(O-), -P(O)(ORb)(ORb), -C(O)Rb, -C(S)Rb, -C(NRb)Rb, -C(O)O-, -C(O)ORb, -C(S)ORb, -C(O)NRcRc, -OC(O)Rb, -OC(S)Rb, -OC(O)O-, -OC(O)ORb, -OC(S)ORb, -NRbC(O)Rb, - NRbC(S)Rb, -NRbC(O)O-, -NRbC(O)ORb, -NRbC(S)ORb, -NRbC(O)NRcRc, -NRbC(NRb)Rb и -NRbC(NRb)NRcRc, где Ra, Rb и Rc определены выше;
или его соль или сложный эфир;
и по меньшей мере один фармацевтически приемлемый носитель.
2. Фармацевтическая композиция по п. 1, где композиция представляет собой пероральную единичную дозированную форму, внутривенную единичную дозированную форму, интраназальную единичную дозированную форму, суппозиторную единичную дозированную форму, внутрикожную единичную дозированную форму, внутримышечную единичную дозированную форму, внутрибрюшинную единичную дозированную форму, подкожную единичную дозированную форму, эпидуральную единичную дозированную форму, сублингвальную единичную дозированную форму или внутричерепную единичную дозированную форму.
3. Фармацевтическая композиция по п. 1, где композиция представляет собой пероральную единичную дозированную форму и пригодна для введения в количестве от 0,001 мг до 200 мг соединения на килограмм массы тела нуждающегося пациента; и пациент является животным; более предпочтительно, пациент является млекопитающим; и наиболее предпочтительно, пациент является человеком.
4. Фармацевтическая композиция по п. 1, в форме, выбранной из таблеток, пилюль, пеллет, капсул, порошков, ромбовидных рассасываемых таблеток-леденцов, гранул, растворов, суспензий, эмульсии, сиропов, эликсиров, составов с замедленным высвобождением, аэрозолей и спреев.
5. Фармацевтическая композиция по п. 1, которая находится в форме таблетки или капсулы.
6. Фармацевтическая композиция по п. 1, которая представляет собой пероральный жидкий препарат.
7. Фармацевтическая композиция по п. 1, где композиция представляет собой пероральную единичную дозированную форму и дополнительно содержащую один или более дополнительных агентов, выбранных из подсластителей, ароматизаторов, красителей, консервантов, материалов, задерживающих время дезинтеграции, стандартных пероральных средств, подходящих носителей, наполнителей или разбавителей.
8. Фармацевтическая композиция по п. 1, где композиция представляет собой внутривенную единичную дозированную форму, где внутривенная единичная дозированная форма пригодна для введения в количестве от 0,01 мг до 100 мг соединения на килограмм массы тела.
9. Фармацевтическая композиция по п. 1, где композиция представляет собой интраназальную единичную дозированную форму, где интраназальная единичная дозированная форма пригодна для введения в количестве от 0,01 мг до 1 мг соединения на килограмм массы тела.
10. Фармацевтическая композиция по п. 8 или 9, где дозированная лекарственная форма находится в виде водного раствора.
11. Фармацевтическая композиция по п. 1, где композиция представляет собой суппозиторную единичную дозированную форму, где суппозиторная единичная дозированная форма пригодна для введения в количестве от 0,01 мг до 50 мг соединения на килограмм массы тела и содержит активный ингредиент в диапазоне от 0,5% до 10% по весу.
12. Фармацевтическая композиция по п. 1, где композиция представляет собой внутрикожную, внутримышечную, внутрибрюшинную, подкожную, эпидуральную, сублингвальную или внутричерепную единичную дозированную форму;
где внутрикожная, внутримышечная, внутрибрюшинная, подкожная, эпидуральная, сублингвальная или внутричерепная единичная дозированная форма пригодна для введения в количестве от 0,001 мг до 200 мг соединения на килограмм массы тела.
13. Фармацевтическая композиция по пп. 3, 8, 9, 11 или 12, где соединение структурной формулы (VIa.11) выбрано из группы, состоящей из
14. Соединение, выбранное из группы, состоящей из
или его соли или сложного эфира.
15. Применение соединения структурной формулы (VIa.11):
где:
nn представляет собой целое число от 0 до 4;
A64 представляет собой O или S;
A65 представляет собой N или CR1;
A66 представляет собой NR73 или CR73R74;
Y представляет собой O, S, NR6 или C(R6R7);
каждый из R1, R5, R6 и R7 независимо представляет собой водород, галоген, алкил, замещенный алкил, арил, замещенный арил, гетероарил или замещенный гетероарил;
R72 независимо представляет собой водород, аминогруппу, замещенную аминогруппу, сульфонил, замещенный сульфонил, замещенный или незамещенный, насыщенный или ненасыщенный, разветвленный, неразветвленный или циклический одновалентный углеводородный радикал, содержащий от 1 до 20 атомов углерода, гетероарил, замещенный гетероарил, арил или арил, в котором один атом водорода заменен на заместитель, и где гетероарильная группа выбрана из группы, состоящей из акридина, β-карболина, хромана, хромена, циннолина, фурана, имидазола, индазола, индола, индолина, индолизина, изобензофурана, изохромена, изоиндола, изоиндолина, изохинолина, изотиазола, изоксазола, нафтиридина, оксадиазола, оксазола, перимидина, фенантридина, фенантролина, феназина, фталазина, птеридина, пурина, пирана, пиразина, пиразола, пиридазина, пиридина, пиримидина, пиррола, пирролизина, хиназолина, хинолина, хинолизина, хиноксалина, тетразола, тиадиазола, тиазола, тиофена, триазола, ксантена, флуоридина;
R73 независимо представляет собой водород, аминогруппу, замещенную аминогруппу, сульфонил, замещенный сульфонил, замещенный или незамещенный, насыщенный или ненасыщенный, разветвленный, неразветвленный или циклический одновалентный углеводородный радикал, содержащий от 1 до 20 атомов углерода, гетероарил, замещенный гетероарил, арил или арил, в котором один атом водорода заменен на заместитель;
R74 независимо представляет собой водород, аминогруппу, замещенную аминогруппу, сульфонил, замещенный сульфонил, замещенный или незамещенный, насыщенный или ненасыщенный, разветвленный, неразветвленный или циклический одновалентный углеводородный радикал, содержащий от 1 до 20 атомов углерода, гетероарил, замещенный гетероарил, арил или арил, в котором один атом водорода заменен на заместитель;
где заместители для насыщенных атомов углерода выбраны из группы -Ra, галоген, -O-, =O, -ORb, -SRb, -S-, =S, -NRcRc, =NRb, =N-ORb, тригалогенметил, -CF3, -CN, -OCN, -SCN, -NO, -NO2, =N2, -N3, -S(O)2Rb, -S(O)2O-, -S(O)2ORb, -OS(O)2Rb, -OS(O)2ORb, -P(O)(O-)2 ,-P(O)(ORb)(O-), -P(O)(ORb)(ORb), -C(O)Rb, -C(S)Rb, -C(NRb)Rb, -C(O)O-, -C(O)ORb, -C(S)ORb, -C(O)NRcRc, -OC(O)Rb, -OC(S)Rb, -OC(O)O-, -OC(O)ORb, -OC(S)ORb, -NRbC(O)Rb, - NRbC(S)Rb, -NRbC(O)O-, -NRbC(O)ORb, -NRbC(S)ORb, -NRbC(O)NRcRc, -NRbC(NRb)Rb и -NRbC(NRb)NRcRc, где Ra выбран из группы, состоящей из алкила, арилалкила, алкилдиила, арила, гетероалкила, замещенного гетероалкила, гетероалкилдиила, гетероарила, гетероарилалкила; каждый из Rb независимо представляет собой водород или Ra; и каждый из Rc независимо представляет собой Rb, или, альтернативно, два радикала Rc вместе с атомом азота, к которому они присоединены, образуют циклогетероалкильное кольцо, которое может включать от 1 до 4 одинаковых или разных дополнительных гетероатомов, выбранных из группы, состоящей из O, N и S;
где заместители для ненасыщенных атомов углерода выбраны из группы -Ra, галоген, -O-, -ORb, -SRb, -S-,-NRcRc, -CN, -OCN, -SCN, -NO, -NO2, -N3, -S(O)2Rb, -S(O)2O-, -S(O)2ORb, -OS(O)2Rb, -OS(O)2ORb, -P(O)(O-)2 ,-P(O)(ORb)(O-), -P(O)(ORb)(ORb), -C(O)Rb, -C(S)Rb, -C(NRb)Rb, -C(O)O-, -C(O)ORb, -C(S)ORb, -C(O)NRcRc, -OC(O)Rb, -OC(S)Rb, -OC(O)O-, -OC(O)ORb, -OC(S)ORb, -NRbC(O)Rb, - NRbC(S)Rb, -NRbC(O)O-, -NRbC(O)ORb, -NRbC(S)ORb, -NRbC(O)NRcRc, -NRbC(NRb)Rb и -NRbC(NRb)NRcRc, где Ra, Rb и Rc определены выше;
или его соль или сложный эфир;
в лечении
(a) боли, выбранной из группы, состоящей из: острой боли, хронической боли, воспалительной боли, невропатической боли, тонической боли, постоянной боли, послеоперационной боли, боли, вызванной химическими реагентами, боли, вызванной химиотерапевтическими средствами, боли при раке, боли, вызванной лекарственными средствами, костной боли, боли, связанной с гипералгезией, индуцированной алкоголем и их комбинации; и/или
(b) спазмов скелетной мышцы, приступов судорог, эпилепсии, рестеноза, атеросклероза, псориаза, тромбоза, ожога, посттравматического стрессового расстройства, сердечного расстройства, отказа от курения, воспаления и иммунно-опосредованных расстройств, и их комбинации; и/или
(c) невропатической боли, такой как каузальгия, диабета, коллагенового сосудистого заболевания, невралгии тройничного нерва, повреждения спинного мозга, повреждения ствола головного мозга, таламического синдрома Дежерина-Русси, комплексного регионального болевого синдрома типа I/симпатической рефлекторной дистрофии, синдрома Фабри, невропатии мелких волокон, рака, химиотерапии рака, хронического алкоголизма, инсульта, абсцесса, демиелинизирующего заболевания, вирусной инфекции, антивирусной терапии, СПИДа, терапии СПИДа, травмы, хирургической операции, ампутации, действия токсина, дезадаптирующего применения вещества, зависимости от психоактивных веществ, и/или злоупотребления психоактивными веществами, употребления или злоупотребления алкоголя, употребления или злоупотребления психоактивных веществ, употребления или злоупотребления наркотиков, эффекта, обусловленного лекарственным средством, метастаза; и/или
(d) воспалительной боли, такой как ожог, солнечный ожог, артрит, колит, кардит, дерматит, миозит, неврит, мукозит, уретрит, цистит, гастрит, пневмонит и коллагеновые сосудистые заболевания; и/или
(e) генерализованного болевого расстройства, такого как фибромиалгия, синдром раздраженной толстой кишки, височно-нижнечелюстные расстройства; и/или
(f) воспаления, иммунного расстройства и их комбинации; и/или
(g) рака, связанного с TrkA.
16. Применение по п. 15, где лечение дополнительно включает введение по меньшей мере одного дополнительного активного агента, выбранного из группы, состоящей из ингибитора протеинкиназы А (PKA), ингибитора сАМР-сигнальной системы, нестероидного противовоспалительного лекарственного средства, ингибитора синтеза простагландинов, местного анестетика, антиконвульсанта, антидепрессанта, агониста опиоидных рецепторов, нейролептика, агониста ГАМКА-рецептора, анальгетика или противоракового средства, действующего по механизму, отличному от антагониста TrkA, бензодиазепина, барбитурата, нестероидного и ингаляционного анестетика, анестетика и противоракового лекарственного средства, модулятора рецептора mGluR5, и их комбинации.
17. Применение по п. 15 или 16, где заболевание, расстройство, симптом или состояние представляет собой боль, выбранную из группы, состоящей из: острой боли, хронической боли, воспалительной боли, невропатической боли, тонической боли, постоянной боли, послеоперационной боли, боли, вызванной химическими реагентами, боли, вызванной химиотерапевтическими средствами, боли при раке, боли, вызванной лекарственными средствами, костной боли, боли, связанной с гипералгезией, индуцированной алкоголем, и их комбинации.
18. Применение по п. 15 или 16, где заболевание, расстройство, симптом или состояние представляет собой хроническую боль.
19. Применение по п. 15 или 16, где заболевание, расстройство, симптом или состояние представляет собой невропатическую боль.
20. Применение по п. 15 или 16, где заболевание, расстройство, симптом или состояние выбрано из группы, состоящей из: спазмов скелетной мышцы, приступов судорог, эпилепсии, рестеноза, атеросклероза, псориаза, тромбоза, ожога, посттравматического стрессового расстройства, сердечного расстройства, курения, воспаления и иммунно-опосредованных расстройств, и их комбинации.
21. Применение по п. 15 или 16, где заболевание, расстройство, симптом или состояние благодаря или связано с каузальгией, диабетом, коллагеновым сосудистым заболеванием, невралгией тройничного нерва, повреждением спинного мозга, повреждением ствола головного мозга, таламическим болевым синдромом, комплексным региональным болевым синдромом типа I/симпатической рефлекторной дистрофии, синдромом Фабри, невропатией мелких волокон, химиотерапией рака, хроническим алкоголизмом, инсультом, абсцессом, демиелинизирующим заболеванием, вирусной инфекцией, антивирусной терапией, СПИДом, терапией СПИДа, ожогом, солнечным ожогом, артритом, колитом, кардитом, дерматитом, миозитом, невритом, мукозитом, уретритом, циститом, гастритом, пневмонитом, коллагеновым сосудистым заболеванием, травмой, хирургической операцией, ампутацией, действием токсином, дезадаптирующим применением вещества, зависимостью от психоактивных веществ, злоупотреблением психоактивными веществами, употреблением или злоупотреблением алкоголя, употреблением или злоупотреблением психоактивных веществ, употреблением или злоупотреблением наркотиков, эффектом, обусловленным лекарственным средством, метастазом, фибромиалгией, синдромом раздраженной толстой кишки, височно-нижнечелюстным расстройством, воспалением, иммунным расстройством и их комбинацией.
22. Применение по п. 15 или 16, где соединение структурной формулы (VIa.11) выбрано из группы, состоящей из
23. Соединение структурной формулы (VIa.11):
где:
nn представляет собой целое число от 0 до 4;
A64 представляет собой O или S;
A65 представляет собой N или CR1;
A66 представляет собой NR73 или CR73R74;
Y представляет собой O, S, NR6 или C(R6R7);
каждый из R1, R5, R6 и R7 независимо представляет собой водород, галоген, алкил, замещенный алкил, арил, замещенный арил, гетероарил или замещенный гетероарил;
R72 независимо представляет собой водород, аминогруппу, замещенную аминогруппу, сульфонил, замещенный сульфонил, замещенный или незамещенный, насыщенный или ненасыщенный, разветвленный, неразветвленный или циклический одновалентный углеводородный радикал, содержащий от 1 до 20 атомов углерода, гетероарил, замещенный гетероарил, арил или арил, в котором один атом водорода заменен на заместитель, и где гетероарильная группа выбрана из группы, состоящей из акридина, β-карболина, хромана, хромена, циннолина, фурана, имидазола, индазола, индола, индолина, индолизина, изобензофурана, изохромена, изоиндола, изоиндолина, изохинолина, изотиазола, изоксазола, нафтиридина, оксадиазола, оксазола, перимидина, фенантридина, фенантролина, феназина, фталазина, птеридина, пурина, пирана, пиразина, пиразола, пиридазина, пиридина, пиримидина, пиррола, пирролизина, хиназолина, хинолина, хинолизина, хиноксалина, тетразола, тиадиазола, тиазола, тиофена, триазола, ксантена, флуоридина;
R73 независимо представляет собой водород, аминогруппу, замещенную аминогруппу, сульфонил, замещенный сульфонил, замещенный или незамещенный, насыщенный или ненасыщенный, разветвленный, неразветвленный или циклический одновалентный углеводородный радикал, содержащий от 1 до 20 атомов углерода, гетероарил, замещенный гетероарил, арил или арил, в котором один атом водорода заменен на заместитель;
R74 независимо представляет собой водород, аминогруппу, замещенную аминогруппу, сульфонил, замещенный сульфонил, замещенный или незамещенный, насыщенный или ненасыщенный, разветвленный, неразветвленный или циклический одновалентный углеводородный радикал, содержащий от 1 до 20 атомов углерода, гетероарил, замещенный гетероарил, арил или арил, в котором один атом водорода заменен на заместитель;
где заместители для насыщенных атомов углерода выбраны из группы -Ra, галоген, -O-, =O, -ORb, -SRb, -S-, =S, -NRcRc, =NRb, =N-ORb, тригалогенметил, -CF3, -CN, -OCN, -SCN, -NO, -NO2, =N2, -N3, -S(O)2Rb, -S(O)2O-, -S(O)2ORb, -OS(O)2Rb, -OS(O)2ORb, -P(O)(O-)2 ,-P(O)(ORb)(O-), -P(O)(ORb)(ORb), -C(O)Rb, -C(S)Rb, -C(NRb)Rb, -C(O)O-, -C(O)ORb, -C(S)ORb, -C(O)NRcRc, -OC(O)Rb, -OC(S)Rb, -OC(O)O-, -OC(O)ORb, -OC(S)ORb, -NRbC(O)Rb, - NRbC(S)Rb, -NRbC(O)O-, -NRbC(O)ORb, -NRbC(S)ORb, -NRbC(O)NRcRc, -NRbC(NRb)Rb и -NRbC(NRb)NRcRc, где Ra выбран из группы, состоящей из алкила, арилалкила, алкилдиила, арила, гетероалкила, замещенного гетероалкила, гетероалкилдиила, гетероарила, гетероарилалкила; каждый из Rb независимо представляет собой водород или Ra; и каждый из Rc независимо представляет собой Rb, или, альтернативно, два радикала Rc вместе с атомом азота, к которому они присоединены, образуют циклогетероалкильное кольцо, которое может включать от 1 до 4 одинаковых или разных дополнительных гетероатомов, выбранных из группы, состоящей из O, N и S;
где заместители для ненасыщенных атомов углерода выбраны из группы -Ra, галоген, -O-, -ORb, -SRb, -S-,-NRcRc, -CN, -OCN, -SCN, -NO, -NO2, -N3, -S(O)2Rb, -S(O)2O-, -S(O)2ORb, -OS(O)2Rb, -OS(O)2ORb, -P(O)(O-)2 ,-P(O)(ORb)(O-), -P(O)(ORb)(ORb), -C(O)Rb, -C(S)Rb, -C(NRb)Rb, -C(O)O-, -C(O)ORb, -C(S)ORb, -C(O)NRcRc, -OC(O)Rb, -OC(S)Rb, -OC(O)O-, -OC(O)ORb, -OC(S)ORb, -NRbC(O)Rb, - NRbC(S)Rb, -NRbC(O)O-, -NRbC(O)ORb, -NRbC(S)ORb, -NRbC(O)NRcRc, -NRbC(NRb)Rb и -NRbC(NRb)NRcRc, где Ra, Rb и Rc определены выше;
или его соль или сложный эфир;
при условии, что соединение не представляет собой
24. Соединение по п. 23, представляющее собой
или его соль или сложный эфир.
25. Фармацевтическая композиция по п. 1, где соединение структурной формулы (VIa.11) представляет собой:
26. Фармацевтическая композиция по пп. 3, 8, 9, 11 или 12, где соединение структурной формулы (VIa.11) представляет собой:
27. Фармацевтическая композиция по п. 1, в форме, выбранной из таблеток, пилюль, пеллет, капсул, порошков, ромбовидных рассасываемых таблеток-леденцов, гранул, растворов, суспензий, эмульсии, сиропов, эликсиров, составов с замедленным высвобождением, аэрозолей, спреев и перорального жидкого препарата, где соединение структурной формулы (VIa.11) представляет собой:
28. Применение по п. 15 или 16, где соединение структурной формулы (VIa.11) представляет собой:
29. Применение по п. 15 или 16, где заболевание, расстройство, симптом или состояние представляет собой боль, выбранную из группы, состоящей из: острой боли, хронической боли, воспалительной боли, невропатической боли, тонической боли, постоянной боли, послеоперационной боли, боли, вызванной химическими реагентами, боли, вызванной химиотерапевтическими средствами, боли при раке, боли, вызванной лекарственными средствами, костной боли, боли, связанной с гипералгезией, индуцированной алкоголем, и их комбинации, и где соединение структурной формулы (VIa.11) представляет собой:
30. Применение по п. 15 или 16, где заболевание, расстройство, симптом или состояние представляет собой острую боль, и где соединение структурной формулы (VIa.11) представляет собой:
31. Применение по п. 15 или 16, где заболевание, расстройство, симптом или состояние представляет собой хроническую боль, и где соединение структурной формулы (VIa.11) представляет собой:
32. Применение по п. 15 или 16, где заболевание, расстройство, симптом или состояние представляет собой воспалительную боль, и где соединение структурной формулы (VIa.11) представляет собой:
33. Применение по п. 15 или 16, где заболевание, расстройство, симптом или состояние представляет собой невропатическую боль, и где соединение структурной формулы (VIa.11) представляет собой:
34. Применение по п. 15 или 16, где заболевание, расстройство, симптом или состояние представляет собой рак, связанный с TrkA, и где соединение структурной формулы (VIa.11) представляет собой:
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