RU2018134262A - Производное 5-этил-4-метил-пиразол-3-карбоксамида, обладающее активностью агониста taar - Google Patents
Производное 5-этил-4-метил-пиразол-3-карбоксамида, обладающее активностью агониста taar Download PDFInfo
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- RU2018134262A RU2018134262A RU2018134262A RU2018134262A RU2018134262A RU 2018134262 A RU2018134262 A RU 2018134262A RU 2018134262 A RU2018134262 A RU 2018134262A RU 2018134262 A RU2018134262 A RU 2018134262A RU 2018134262 A RU2018134262 A RU 2018134262A
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- SONZLIIHTSKJMC-UHFFFAOYSA-N 5-ethyl-4-methyl-1h-pyrazole-3-carboxamide Chemical class CCC=1NN=C(C(N)=O)C=1C SONZLIIHTSKJMC-UHFFFAOYSA-N 0.000 title 1
- 102000011829 Trace amine associated receptor Human genes 0.000 title 1
- 108050002178 Trace amine associated receptor Proteins 0.000 title 1
- 239000000556 agonist Substances 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 12
- 208000035475 disorder Diseases 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 11
- 208000020925 Bipolar disease Diseases 0.000 claims 5
- 201000000980 schizophrenia Diseases 0.000 claims 4
- 208000024827 Alzheimer disease Diseases 0.000 claims 3
- 208000019901 Anxiety disease Diseases 0.000 claims 3
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 3
- 206010012335 Dependence Diseases 0.000 claims 3
- 208000002249 Diabetes Complications Diseases 0.000 claims 3
- 206010012655 Diabetic complications Diseases 0.000 claims 3
- 208000032928 Dyslipidaemia Diseases 0.000 claims 3
- 208000030814 Eating disease Diseases 0.000 claims 3
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 3
- 206010020772 Hypertension Diseases 0.000 claims 3
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 3
- 208000019695 Migraine disease Diseases 0.000 claims 3
- 208000008589 Obesity Diseases 0.000 claims 3
- 208000018737 Parkinson disease Diseases 0.000 claims 3
- 238000010521 absorption reaction Methods 0.000 claims 3
- 230000009045 body homeostasis Effects 0.000 claims 3
- 206010012601 diabetes mellitus Diseases 0.000 claims 3
- 235000014632 disordered eating Nutrition 0.000 claims 3
- 206010015037 epilepsy Diseases 0.000 claims 3
- 206010027599 migraine Diseases 0.000 claims 3
- 235000020824 obesity Nutrition 0.000 claims 3
- 208000019116 sleep disease Diseases 0.000 claims 3
- 201000009032 substance abuse Diseases 0.000 claims 3
- 231100000736 substance abuse Toxicity 0.000 claims 3
- 208000011117 substance-related disease Diseases 0.000 claims 3
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 208000017164 Chronobiology disease Diseases 0.000 claims 2
- 208000020401 Depressive disease Diseases 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- XHHXGKRFUPEPFM-OAHLLOKOSA-N 5-ethyl-4-methyl-N-[4-[(2S)-morpholin-2-yl]phenyl]-1H-pyrazole-3-carboxamide Chemical compound C(C)C1=C(C(=NN1)C(=O)NC1=CC=C(C=C1)[C@H]1CNCCO1)C XHHXGKRFUPEPFM-OAHLLOKOSA-N 0.000 claims 1
- 208000013200 Stress disease Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 230000006399 behavior Effects 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 208000028683 bipolar I disease Diseases 0.000 claims 1
- 208000025307 bipolar depression Diseases 0.000 claims 1
- 238000003776 cleavage reaction Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000002526 effect on cardiovascular system Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 150000002780 morpholines Chemical class 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000033764 rhythmic process Effects 0.000 claims 1
- 230000007017 scission Effects 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A61K9/2022—Organic macromolecular compounds
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- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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Claims (17)
1. Морфолиновое производное формулы
и его фармацевтически приемлемая соль присоединения кислоты.
2. Соединение формулы I, которое представляет собой 5-этил-4-метил-N-[4-[(2S)морфолин-2-ил]фенил]-1Н-пиразол-3-карбоксамид.
3. Способ получения соединения формулы I согласно пп. 1 и 2, включающий
а) отщепление N-защитной группы (PG) у соединений формулы
с образованием соединения формулы
где PG является N-защитной группой, выбранной из -С(O)O-трет-бутила (ВОС), и,
при желании, превращение полученных соединений в фармацевтически приемлемые соли присоединения кислоты.
4. Соединение формулы I согласно пп. 1 и 2 для применения в качестве терапевтически активного вещества.
5. Соединение формулы I по пп. 1 и 2 для применения в лечении депрессии, тревожных расстройств, биполярного расстройства, синдрома гиперактивности с дефицитом внимания (СГДВ), связанных со стрессом расстройств, шизофрении, болезни Паркинсона, болезни Альцгеймера, эпилепсии, мигрени, гипертензии, злоупотребления веществами, аддикции, нарушений пищевого поведения, диабета, диабетических осложнений, ожирения, дислипидемии, нарушений поглощения энергии и ассимиляции, расстройств и нарушения гомеостаза температуры тела, расстройств сна и циркадного ритма и сердечно-сосудистых расстройств.
6. Соединение формулы I согласно пп. 1 и 2 для применения в лечении шизофрении, биполярного расстройства или депрессии.
7. Фармацевтическая композиция, содержащая соединение формулы I согласно пп. 1 или 2 и фармацевтически приемлемые эксципиенты.
8. Применение соединения формулы I согласно пп. 1 или 2 для изготовления лекарственного средства для лечения депрессии, тревожных расстройств, биполярного расстройства, синдрома гиперактивности с дефицитом внимания (СГДВ), связанных со стрессом расстройств, шизофрении, болезни Паркинсона, болезни Альцгеймера, эпилепсии, мигрени, гипертензии, злоупотребления веществами, аддикции, нарушений пищевого поведения, диабета, диабетических осложнений, ожирения, дислипидемии, нарушений поглощения энергии и ассимиляции, расстройств и нарушения гомеостаза температуры тела, расстройств сна и циркадного ритма и сердечно-сосудистых расстройств.
9. Способ лечения депрессии, тревожных расстройств, биполярного расстройства, синдрома гиперактивности с дефицитом внимания (СГДВ), связанных со стрессом расстройств, шизофрении, болезни Паркинсона, болезни Альцгеймера, эпилепсии, мигрени, гипертензии, злоупотребления веществами, аддикции, нарушений пищевого поведения, диабета, диабетических осложнений, ожирения, дислипидемии, нарушений поглощения энергии и ассимиляции, расстройств и нарушения гомеостаза температуры тела, расстройств сна и циркадного ритма и сердечно-сосудистых расстройств, включающий введение эффективного количества соединения формулы I согласно пп. 1 или 2.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16160790 | 2016-03-17 | ||
| EP16160790.8 | 2016-03-17 | ||
| PCT/EP2017/055885 WO2017157873A1 (en) | 2016-03-17 | 2017-03-14 | 5-ethyl-4-methyl-pyrazole-3-carboxamide derivative having activity as agonist of taar |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| RU2018134262A3 RU2018134262A3 (ru) | 2020-04-17 |
| RU2018134262A true RU2018134262A (ru) | 2020-04-17 |
| RU2731095C2 RU2731095C2 (ru) | 2020-08-28 |
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| RU2018134262A RU2731095C2 (ru) | 2016-03-17 | 2017-03-14 | Производное 5-этил-4-метил-пиразол-3-карбоксамида, обладающее активностью агониста taar |
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| EP (2) | EP3430010B1 (ru) |
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| BR (1) | BR112018015389B1 (ru) |
| CA (1) | CA3013696C (ru) |
| CL (1) | CL2018002583A1 (ru) |
| CO (1) | CO2018007515A2 (ru) |
| CR (1) | CR20180443A (ru) |
| DK (1) | DK3430010T3 (ru) |
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| UA (1) | UA122881C2 (ru) |
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| EP3997085A1 (en) | 2019-07-11 | 2022-05-18 | F. Hoffmann-La Roche AG | Process for the preparation of substituted pyrazole derivatives |
| EP4121428B1 (en) | 2020-03-19 | 2025-08-13 | F. Hoffmann-La Roche AG | Salts and crystalline forms of a taar1 agonist |
| TW202334100A (zh) | 2021-11-08 | 2023-09-01 | 瑞士商赫孚孟拉羅股份公司 | 芳香族硝基化合物之催化氫化 |
| CN114288304A (zh) * | 2021-12-31 | 2022-04-08 | 江苏海洋大学 | 一种抗精神分裂症组合物及其应用 |
| AR129909A1 (es) | 2022-07-15 | 2024-10-09 | Hoffmann La Roche | Cetorreductasa mutante con mayor actividad de cetorreductasa así como métodos y usos de esta |
| JP2025526040A (ja) * | 2022-08-12 | 2025-08-07 | エフ． ホフマン－ラ ロシュ アーゲー | 固体剤形の連続製造におけるコプロセス添加剤の使用 |
| JP2025526086A (ja) | 2022-08-12 | 2025-08-07 | エフ． ホフマン－ラ ロシュ アーゲー | ５－エチル－４－メチル－ｎ－［４－［（２ｓ）モルホリン－２－イル］フェニル］－１ｈ－ピラゾール－３－カルボキサミドを含む医薬組成物 |
| TW202440563A (zh) * | 2022-11-28 | 2024-10-16 | 美商住友製藥美國公司 | 2-苯基嗎啉與2-苯基(硫代)嗎啉化合物及其用途 |
| WO2024222860A1 (zh) * | 2023-04-28 | 2024-10-31 | 江苏豪森药业集团有限公司 | 一种吗啉杂环类化合物的盐及其制备方法和应用 |
| WO2024258900A2 (en) * | 2023-06-13 | 2024-12-19 | University Of Georgia Research Foundation, Inc. | Plasmodium falciparum blood stage inhibitors |
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