RU2002128352A - Производные 4,5-дигидро-1н-пиразола, обладающие cb1-антагонистической активностью - Google Patents
Производные 4,5-дигидро-1н-пиразола, обладающие cb1-антагонистической активностьюInfo
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- RU2002128352A RU2002128352A RU2002128352/04A RU2002128352A RU2002128352A RU 2002128352 A RU2002128352 A RU 2002128352A RU 2002128352/04 A RU2002128352/04 A RU 2002128352/04A RU 2002128352 A RU2002128352 A RU 2002128352A RU 2002128352 A RU2002128352 A RU 2002128352A
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- MCGBIXXDQFWVDW-UHFFFAOYSA-N 4,5-dihydro-1h-pyrazole Chemical class C1CC=NN1 MCGBIXXDQFWVDW-UHFFFAOYSA-N 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 claims abstract 39
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 7
- 239000001257 hydrogen Substances 0.000 claims abstract 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 6
- 125000000217 alkyl group Chemical group 0.000 claims abstract 5
- 125000004076 pyridyl group Chemical group 0.000 claims abstract 5
- 125000001624 naphthyl group Chemical group 0.000 claims abstract 4
- 125000001544 thienyl group Chemical group 0.000 claims abstract 4
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims abstract 3
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims abstract 3
- 125000003668 acetyloxy group Chemical group [H]C([H])([H])C(=O)O[*] 0.000 claims abstract 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims abstract 2
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 238000000034 method Methods 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 150000001412 amines Chemical class 0.000 claims 3
- 229930003827 cannabinoid Natural products 0.000 claims 3
- 239000003557 cannabinoid Substances 0.000 claims 3
- 238000006243 chemical reaction Methods 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 230000005062 synaptic transmission Effects 0.000 claims 3
- -1 trifluoromethoxy, nitro, amino Chemical group 0.000 claims 3
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000006239 protecting group Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- NWZSZGALRFJKBT-KNIFDHDWSA-N (2s)-2,6-diaminohexanoic acid;(2s)-2-hydroxybutanedioic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O.NCCCC[C@H](N)C(O)=O NWZSZGALRFJKBT-KNIFDHDWSA-N 0.000 claims 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 208000027559 Appetite disease Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 208000014094 Dystonic disease Diseases 0.000 claims 1
- 241001331845 Equus asinus x caballus Species 0.000 claims 1
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 1
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000028017 Psychotic disease Diseases 0.000 claims 1
- 208000000323 Tourette Syndrome Diseases 0.000 claims 1
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 claims 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 125000003368 amide group Chemical group 0.000 claims 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 230000006735 deficit Effects 0.000 claims 1
- 208000010643 digestive system disease Diseases 0.000 claims 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
- 208000010118 dystonia Diseases 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 208000018685 gastrointestinal system disease Diseases 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 230000002140 halogenating effect Effects 0.000 claims 1
- IKDUDTNKRLTJSI-UHFFFAOYSA-N hydrazine monohydrate Substances O.NN IKDUDTNKRLTJSI-UHFFFAOYSA-N 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 206010027175 memory impairment Diseases 0.000 claims 1
- 150000002730 mercury Chemical class 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 125000005034 trifluormethylthio group Chemical group FC(S*)(F)F 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 125000001889 triflyl group Chemical group FC(F)(F)S(*)(=O)=O 0.000 claims 1
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 102000009132 CB1 Cannabinoid Receptor Human genes 0.000 abstract 1
- 108010073366 CB1 Cannabinoid Receptor Proteins 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 1
- 240000004308 marijuana Species 0.000 abstract 1
- 230000003389 potentiating effect Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/06—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
-
- A—HUMAN NECESSITIES
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/06—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D231/08—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with oxygen or sulfur atoms directly attached to ring carbon atoms
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Child & Adolescent Psychology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Claims (16)
1. Соединение формулы (I)
где R и R1 могут быть одинаковыми или различными и обозначают фенил, тиенил или пиридил, причем указанные группы могут быть замещены 1, 2 или 3 заместителями Y, которые могут быть одинаковыми или различными, из группы, включающей С1-3-алкил или алкокси, гидрокси, галоген, трифторметил, трифторметилтио, трифторметокси, нитро, амино, моно- или диалкил (С1-2) амино, моно- или диалкил (Сl-2) амидо, (С1-3) алкилсульфонил, диметилсульфамидо, С1-3-алкоксикарбонил, карбоксил, трифторметилсульфонил, циано, карбамоил, сульфамоил и ацетил, или R и/или R1, обозначают нафтил;
R2 обозначает водород, гидрокси, C1-3-алкокси, ацетилокси или пропионилокси;
Аа обозначает одну из групп (i), (ii), (iii), (iv) или (v)
где R4 и R5 независимо друг от друга обозначают водород или C1-8 разветвленный или неразветвленный алкил, или С3-8 циклоалкил или R4 обозначает ацетамидо или диметиламино, или 2,2,2-трифторэтил, или фенил, или пиридил, при условии, что R6 обозначает водород, R6 обозначает водород или C1-3 неразветвленный алкил;
Bb обозначает сульфонил или карбонил;
R3 обозначает бензил, фенил, тиенил или пиридил, которые могут быть замещены 1, 2 или 3 заместителями Y, которые могут быть одинаковыми или различными, или R3 обозначает C1-8 разветвленный или неразветвленный алкил или С3-8 циклоалкил, или R3 обозначает нафтил,
и его таутомеры, пролекарства и соли.
2. Соединение формулы (I) по п.1, отличающееся тем, что R обозначает 4-хлорфенильную группу, R1 обозначает фенил, R2 обозначает водород, Аа обозначает группу (i), в которой R4 обозначает водород и R5 обозначает метил, Bb обозначает сульфонил и R3 обозначает 4-хлорфенил, и его соли.
3. Фармацевтическая композиция, включающая по меньшей мере одно соединение по п.1 в качестве активного компонента.
4. Способ получения фармацевтических композиций, отличающийся тем, что соединение по п.1 переводят в форму, подходящую для введения.
5. Способ получения соединения общей формулы I, отличающийся тем, что a) получают соединение, в котором R, R1-R3 и Bb имеют значения, указанные в п.1, и Аа обозначает группу формулы (i) или (ii) по п.1, посредством 1) реакции соединения формулы (II) с гидразином или гидратом гидразина с получением соединения формулы (III), которое подвергают реакции с соединением формулы (IVa) или (IVb) с получением соединения формулы (V), которое подвергают реакции с соединением формулы R3-SO2X или R3-COX, где Х обозначает галоген, или 2) реакции соединения формулы (III) с тиоизоцианатом формулы (VI) с получением соединения формулы (VII), которое подвергают реакции с амином в присутствии соли ртути (II), или 3) реакции соединения формулы (III) с соединением формулы (VIII) с получением соединения формулы (IX), которое подвергают реакции с галогенирующим агентом с получением соединения формулы (X), которое подвергают реакции с амином, или 4) реакции соединения формулы (III) с соединением формулы (XI) с получением соединения формулы (XII), которое подвергают реакции с амином, или b) получают соединение, в котором R, R1-R3 и Bb имеют значения, указанные в п.1, и Аа обозначает группу формулы (iii) или (iv) по п.1, посредством реакции соединения формулы (III) с соединением формулы (XIII) или (XIV), или с) получают соединение, в котором R, R1-R3 и Bb имеют значения, указанные в п.1, и Аа обозначает группу формулы (v) по п.1, посредством реакции соединения формулы (III) с соединением формулы (XV) или (XVI) с получением соединения формулы (XVII), от которого удаляют защитную группу с получением соединения формулы (V), которое подвергают реакции с соединением формулы R3-SO2Х или R3-COX, где Х обозначает галоген, или с соединением формулы R3-COOH.
6. Соединение формулы (III)
где R2 обозначает гидроксигруппу;
R и R1 имеют значения, определенные в п.1.
7. Соединение формулы (V)
где Аа имеет значение (i), (ii) или (v) по п.1;
R, R1, и R2 имеют значения, определенные в п.1.
8. Соединение формулы (VII)
где R, R1, R2, R3 и Bb имеют значения, указанные в п.1.
9. Соединение формулы (IX)
где R, R1, R2, R3 и Bb имеют значения, указанные в п.1.
10. Соединение формулы (X)
где R, R1, R2, R3 и Bb имеют значения, указанные в п.1;
R8 обозначает атом галогена.
11. Соединение формулы (XII)
где R, R1, R2, R3 и Bb имеют значения, указанные в п.1;
R9 обозначает С1-3 алкильную группу.
12. Соединение формулы (XVII)
где R, R1 и R2 имеют значения, указанные в п.1;
Аа имеет значение (v) по п.1;
Prot обозначает так называемую защитную группу.
13. Способ лечения заболеваний, опосредованных CB1-рецептором, включающий введение пациенту эффективного количества соединения по п.1.
14. Способ по п.13, отличающийся тем, что заболеванием являются психиатрические заболевания, такие как психоз, беспокойство, депрессия, дефицит внимания, нарушения памяти и расстройства аппетита, ожирение, неврологические заболевания, такие как болезнь Паркинсона, деменция, дистония, болезнь Альцгеймера, эпилепсия, болезнь Хантингтона, болезнь Туретта, ишемия, болевые синдромы и другие заболевания ЦНС, включающие каннабиноидную нейротрансмиссию.
15. Способ по п.13, отличающийся тем, что заболеванием является желудочно-кишечные расстройства, включающие каннабиноидную нейротрансмиссию.
16. Способ по п.13, отличающийся тем, что заболеванием является сердечно-сосудистые заболевания, включающие каннабиноидную нейротрансмиссию.
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| US9650375B2 (en) | 2013-03-14 | 2017-05-16 | Merck Sharp & Dohme Corp. | Indole derivatives useful as anti-diabetic agents |
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| WO2014151200A2 (en) | 2013-03-15 | 2014-09-25 | Synergy Pharmaceuticals Inc. | Compositions useful for the treatment of gastrointestinal disorders |
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| WO2015051496A1 (en) | 2013-10-08 | 2015-04-16 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| CA2948349C (en) | 2014-05-09 | 2023-03-28 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Pyrazole derivatives and their use as cannabinoid receptor mediators |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US5591764A (en) * | 1988-09-27 | 1997-01-07 | E. I. Du Pont De Nemours And Company | N-acylated pyrazolines |
| FR2692575B1 (fr) * | 1992-06-23 | 1995-06-30 | Sanofi Elf | Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| RU2149479C1 (ru) * | 1999-03-23 | 2000-05-20 | Научно-исследовательский институт электронных приборов | Способ сборки вакуумной оболочки рентгеновского электронно-оптического преобразователя |
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