RU2016143751A - Фармацевтическая композиция - Google Patents
Фармацевтическая композиция Download PDFInfo
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- RU2016143751A RU2016143751A RU2016143751A RU2016143751A RU2016143751A RU 2016143751 A RU2016143751 A RU 2016143751A RU 2016143751 A RU2016143751 A RU 2016143751A RU 2016143751 A RU2016143751 A RU 2016143751A RU 2016143751 A RU2016143751 A RU 2016143751A
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- 239000008194 pharmaceutical composition Substances 0.000 title claims 3
- 239000000203 mixture Substances 0.000 claims 14
- 208000010238 Uterine Inertia Diseases 0.000 claims 6
- 206010046763 Uterine atony Diseases 0.000 claims 6
- 208000032843 Hemorrhage Diseases 0.000 claims 5
- 208000018525 Postpartum Hemorrhage Diseases 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 150000001875 compounds Chemical class 0.000 claims 5
- 230000002265 prevention Effects 0.000 claims 5
- 208000034158 bleeding Diseases 0.000 claims 4
- 230000000740 bleeding effect Effects 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000003963 antioxidant agent Substances 0.000 claims 3
- 230000003078 antioxidant effect Effects 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 239000007788 liquid Substances 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 208000019901 Anxiety disease Diseases 0.000 claims 2
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 claims 2
- 239000006172 buffering agent Substances 0.000 claims 2
- 230000035606 childbirth Effects 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 2
- 229930182817 methionine Natural products 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- KDYFGRWQOYBRFD-UHFFFAOYSA-N succinic acid group Chemical group C(CCC(=O)O)(=O)O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 1
- 125000004203 4-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 208000004998 Abdominal Pain Diseases 0.000 claims 1
- 206010003805 Autism Diseases 0.000 claims 1
- 208000020706 Autistic disease Diseases 0.000 claims 1
- 208000008035 Back Pain Diseases 0.000 claims 1
- 206010010774 Constipation Diseases 0.000 claims 1
- 206010057671 Female sexual dysfunction Diseases 0.000 claims 1
- 206010061974 Gastrointestinal obstruction Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 claims 1
- 206010057672 Male sexual dysfunction Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 206010035138 Placental insufficiency Diseases 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 208000004396 mastitis Diseases 0.000 claims 1
- 125000001360 methionine group Chemical group N[C@@H](CCSC)C(=O)* 0.000 claims 1
- 230000036407 pain Effects 0.000 claims 1
- 230000032696 parturition Effects 0.000 claims 1
- 230000003169 placental effect Effects 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 230000000638 stimulation Effects 0.000 claims 1
- 239000001384 succinic acid Substances 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- 230000029663 wound healing Effects 0.000 claims 1
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Claims (18)
1. Жидкая (например, водная) композиция, содержащая:
соединение формулы (I):
где: n выбран из 0, 1 и 2; p выбран из 0, 1, 2, 3, 4, 5 и 6; R1 выбран из арила, возможно замещенного по меньшей мере одним заместителем, представляющим собой ОН, F, Cl, Br, алкил или О-алкил; R2 выбран из R4, Н, алкила, циклоалкила, арила и 5- и 6-членных гетероароматических кольцевых систем; R3 выбран из Н и ковалентной связи с R2, когда R2 представляет собой R4, с образованием кольцевой структуры; R4 представляет собой C1-6алкиленовую группировку, замещенную по меньшей мере одним заместителем, представляющим собой О-алкил, S-алкил или ОН; каждый W и X независимо выбран из СН2 и S, но оба не могут представлять собой СН2; алкил выбран из C1-6алкила с прямой цепью и C4-8алкила с разветвленной цепью и возможно имеет по меньшей мере один гидроксильный заместитель; арил выбран из фенила и моно- или поли-замещенного фенила; при условии, что когда R2 представляет собой Н, p равен 1, R3 представляет собой Н, n равен 1, и W и X оба представляют S, тогда R1 не представляет собой 4-гидроксифенил, или его сольвата или фармацевтически приемлемой соли;
и антиоксидант, где значение рН композиции составляет от 5,0 до 6,0.
2. Композиция по п. 1, где значение рН составляет от 5,1 до 6, например от 5,2 до 5,65 или от 5,26 до 5,8.
3. Композиция по п. 1 или 2, где фармацевтическое соединение представляет собой соединение формулы (II):
(FE 202767) или его фармацевтически приемлемую соль.
4. Композиция по любому из пп. 1-3, содержащая буферный агент.
5. Композиция по п. 4, где буферный агент представляет собой янтарную кислоту.
6. Композиция по любому из пп. 1-5, где антиоксидант представляет собой метионин, EDTA или комбинацию метионина и EDTA.
7. Композиция по любому из пп. 1-6, дополнительно содержащая агент для поддержания изотоничности.
8. Композиция по любому из пп. 1-7 для применения в лечении или предупреждении атонии матки, например, после рождения ребенка естественным путем, рождения ребенка с помощью кесарева сечения, или для применения в лечении или предупреждении атонии матки у пациента, имеющего риск развития послеродового кровотечения (РРН); и/или для применения в лечении или предупреждении чрезмерного кровотечения после родов естественным путем.
9. Способ лечения или предупреждения осложненных состояний при кормлении грудью, нарушений при стимуляции родов, состояний атонии матки, чрезмерного кровотечения, воспаления, боли, абдоминальной боли, боли в спине, мужской и женской сексуальной дисфункции, синдрома раздраженного кишечника (IBS), запора, желудочно-кишечной обструкции, аутизма, стресса, тревоги, депрессии, тревожного расстройства, кровопотери при хирургическом вмешательстве, послеродового кровотечения, заживления ран, инфекции, мастита, нарушения рождения плаценты, остеопороза и способ диагностики рака и плацентарной недостаточности, включающий: введение пациенту, нуждающемуся в этом, жидкой (например, водной) фармацевтической композиции, содержащей фармацевтическое соединение формулы (I) или (II), как определено выше, или его фармацевтически активную соль, где значение рН композиции составляет от 5,0 до 6,0.
10. Способ лечения или предупреждения атонии матки (например, после рождения ребенка естественным путем или рождения ребенка с помощью кесарева сечения, или у пациента, имеющего риск развития РРН) или чрезмерного кровотечения после родов естественным путем, включающий стадию введения пациенту, нуждающемуся в этом, композиции по любому из пп. 1-7.
11. Набор, содержащий: жидкую фармацевтическую композицию, содержащую соединение формулы (I) или (II), как определено выше, или его соль и, возможно, антиоксидант, где значение рН композиции составляет от 5,0 до 6,0, и контейнер для этой композиции.
12. Композиция по любому из пп. 1-7 для применения в изготовлении лекарственного средства для лечения или предупреждения атонии матки, например, после рождения ребенка естественным путем, рождения ребенка с помощью кесарева сечения, или для применения в изготовлении лекарственного средства для лечения или предупреждения атонии матки у пациента, имеющего риск развития РРН; и/или для применения в изготовлении лекарственного средства для лечения или предупреждения чрезмерного кровотечения после родов естественным путем.
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| AU2018312956B2 (en) * | 2017-08-11 | 2022-03-10 | Ferring B.V. | Method of manufacturing a pharmaceutical composition |
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