RU2012138445A - Соль конденсированного гетероциклического производного и его кристаллы - Google Patents
Соль конденсированного гетероциклического производного и его кристаллы Download PDFInfo
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- 239000013078 crystal Substances 0.000 title 1
- 150000003839 salts Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 17
- 230000001419 dependent effect Effects 0.000 claims abstract 11
- 239000003795 chemical substances by application Substances 0.000 claims abstract 8
- 238000000034 method Methods 0.000 claims abstract 8
- 201000010099 disease Diseases 0.000 claims abstract 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 6
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 6
- 230000001850 reproductive effect Effects 0.000 claims abstract 6
- 210000000056 organ Anatomy 0.000 claims abstract 5
- 230000016087 ovulation Effects 0.000 claims abstract 5
- 230000002980 postoperative effect Effects 0.000 claims abstract 5
- 206010028980 Neoplasm Diseases 0.000 claims abstract 4
- 201000011510 cancer Diseases 0.000 claims abstract 4
- 239000003433 contraceptive agent Substances 0.000 claims abstract 4
- 238000010586 diagram Methods 0.000 claims abstract 4
- 210000004392 genitalia Anatomy 0.000 claims abstract 4
- 239000005556 hormone Substances 0.000 claims abstract 4
- 229940088597 hormone Drugs 0.000 claims abstract 4
- 230000001939 inductive effect Effects 0.000 claims abstract 4
- 239000000126 substance Substances 0.000 claims abstract 4
- 230000002265 prevention Effects 0.000 claims abstract 3
- 229940124558 contraceptive agent Drugs 0.000 claims abstract 2
- 230000002254 contraceptive effect Effects 0.000 claims abstract 2
- 238000004455 differential thermal analysis Methods 0.000 claims abstract 2
- 239000002474 gonadorelin antagonist Substances 0.000 claims abstract 2
- 238000004519 manufacturing process Methods 0.000 claims abstract 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims abstract 2
- 239000007790 solid phase Substances 0.000 claims abstract 2
- 238000001460 carbon-13 nuclear magnetic resonance spectrum Methods 0.000 claims 1
- 238000000806 fluorine-19 nuclear magnetic resonance spectrum Methods 0.000 claims 1
- 239000003163 gonadal steroid hormone Substances 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 238000000655 nuclear magnetic resonance spectrum Methods 0.000 abstract 1
- 238000000371 solid-state nuclear magnetic resonance spectroscopy Methods 0.000 abstract 1
- 238000001228 spectrum Methods 0.000 abstract 1
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Abstract
1. Соединение, представленное формулой:2. Соединение по п.1, которое является кристаллическим.3. Соединение по п.2, имеющее характерные пики при углах дифракции, (2θ(º)) 7,1, 11,5, 19,4, 20,3, 21,5, 22,0, 22,6, 23,5 и 26,2 в диаграмме порошковой дифракции рентгеновских лучей.4. Соединение по п.2, имеющее характерные пики значений химических сдвигов (δ(ppm)) 155,8, 149,8, 145,3, 118,0, 113,7, 111,6, 110,3, 98,1, 69,8, 58,7, 57,1 и 55,5 в твердотельном спектре ЯМРC.5. Соединение по п.2, имеющее характерные пики значений химических сдвигов (δ(ppm)) из -131,6, -145, и -151,8 в спектре ЯМРF в твердой фазе.6. Соединение по любому одному из пп.2-5, имеющее эндотермический пик около 213ºC в диаграмме дифференциально-термического анализа.7. Фармацевтическая композиция, содержащая в качестве активного компонента, соединение по любому одному из пп.1-6.8. Фармацевтическая композиция по п.7, которая является антагонистом гонадотропин-релизинг гормона.9. Фармацевтическая композиция по п.7, которая является средством для предотвращения или лечения полового гармон-зависимого заболевания, регулятором воспроизводства, контрацептивом, средством, вызывающим овуляцию, или средством для предотвращения послеоперационных рецидивов рака половых гормонально-зависимых органов.10. Применение соединения по любому одному из пп.1-6 в изготовлении средства для предотвращения или лечения полового гармон-зависимого заболевания, регулятора воспроизводства, контрацептивов, средства, вызывающего овуляцию, или средства для предотвращения послеоперационных рецидивов рака половых гормонально-зависимых органов.11. Способ предотвращения или лечения полового гармон-зависимого заболевания, способ репродуктивного регулирования, спо
Claims (11)
1. Соединение, представленное формулой:
2. Соединение по п.1, которое является кристаллическим.
3. Соединение по п.2, имеющее характерные пики при углах дифракции, (2θ(º)) 7,1, 11,5, 19,4, 20,3, 21,5, 22,0, 22,6, 23,5 и 26,2 в диаграмме порошковой дифракции рентгеновских лучей.
4. Соединение по п.2, имеющее характерные пики значений химических сдвигов (δ(ppm)) 155,8, 149,8, 145,3, 118,0, 113,7, 111,6, 110,3, 98,1, 69,8, 58,7, 57,1 и 55,5 в твердотельном спектре ЯМР 13C.
5. Соединение по п.2, имеющее характерные пики значений химических сдвигов (δ(ppm)) из -131,6, -145, и -151,8 в спектре ЯМР 19F в твердой фазе.
6. Соединение по любому одному из пп.2-5, имеющее эндотермический пик около 213ºC в диаграмме дифференциально-термического анализа.
7. Фармацевтическая композиция, содержащая в качестве активного компонента, соединение по любому одному из пп.1-6.
8. Фармацевтическая композиция по п.7, которая является антагонистом гонадотропин-релизинг гормона.
9. Фармацевтическая композиция по п.7, которая является средством для предотвращения или лечения полового гармон-зависимого заболевания, регулятором воспроизводства, контрацептивом, средством, вызывающим овуляцию, или средством для предотвращения послеоперационных рецидивов рака половых гормонально-зависимых органов.
10. Применение соединения по любому одному из пп.1-6 в изготовлении средства для предотвращения или лечения полового гармон-зависимого заболевания, регулятора воспроизводства, контрацептивов, средства, вызывающего овуляцию, или средства для предотвращения послеоперационных рецидивов рака половых гормонально-зависимых органов.
11. Способ предотвращения или лечения полового гармон-зависимого заболевания, способ репродуктивного регулирования, способ контрацепции, способ, вызывающий овуляцию или способ предотвращения послеоперационных рецидивов рака половых гормонально-зависимых органов, включающий введение эффективного количества соединения по любому одному из пп.1-6.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2010-027806 | 2010-02-10 | ||
| JP2010027806 | 2010-02-10 | ||
| PCT/JP2011/052719 WO2011099507A1 (ja) | 2010-02-10 | 2011-02-09 | 縮合複素環誘導体の塩及びその結晶 |
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| Publication Number | Publication Date |
|---|---|
| RU2012138445A true RU2012138445A (ru) | 2014-03-20 |
| RU2557237C2 RU2557237C2 (ru) | 2015-07-20 |
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| Application Number | Title | Priority Date | Filing Date |
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| RU2012138445/04A RU2557237C2 (ru) | 2010-02-10 | 2011-02-09 | Соль конденсированного гетероциклического производного и его кристаллы |
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| Country | Link |
|---|---|
| US (5) | US9169266B2 (ru) |
| EP (1) | EP2535342B1 (ru) |
| JP (1) | JP5337261B2 (ru) |
| KR (1) | KR101631143B1 (ru) |
| CN (1) | CN102753557B (ru) |
| AU (1) | AU2011215250B2 (ru) |
| BR (1) | BR112012020110B1 (ru) |
| CA (1) | CA2788533C (ru) |
| ES (1) | ES2502740T3 (ru) |
| FR (1) | FR22C1049I2 (ru) |
| IL (1) | IL221325A (ru) |
| MX (1) | MX2012009323A (ru) |
| NZ (1) | NZ601684A (ru) |
| RU (1) | RU2557237C2 (ru) |
| SG (1) | SG183243A1 (ru) |
| TW (1) | TWI555751B (ru) |
| WO (1) | WO2011099507A1 (ru) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2014042176A1 (ja) * | 2012-09-14 | 2014-03-20 | キッセイ薬品工業株式会社 | 縮合複素環誘導体の製造方法およびその製造中間体 |
| UA123114C2 (uk) | 2016-08-08 | 2021-02-17 | Кіссеі Фармасьютікал Ко., Лтд. | СПОСІБ ЛІКУВАННЯ ЕНДОМЕТРІОЗУ 3-[2-ФТОР-5-(2,3-ДИФТОР-6-МЕТОКСИБЕНЗИЛОКСИ)-4-МЕТОКСИФЕНІЛ]-2,4-ДІОКСО-1,2,3,4-ТЕТРАГІДРОТІЄНО[3,4-d]ПІРИМІДИН-5-КАРБОНОВОЮ КИСЛОТОЮ |
| SG11201911598WA (en) * | 2017-06-05 | 2020-01-30 | ObsEva SA | Gonadotropin-releasing hormone antagonist dosing regimens for the treatment of endometriosis |
| SG11201911599XA (en) | 2017-06-05 | 2020-01-30 | ObsEva SA | Gonadotropin-releasing hormone antagonist dosing regimens for treating uterine fibroids and reducing menstrual blood loss |
| CA3117092A1 (en) | 2018-10-29 | 2020-05-07 | ObsEva S.A. | Compositions and methods for the treatment of adenomyosis and rectovaginal endometriosis |
| SG11202104053TA (en) | 2018-11-07 | 2021-05-28 | ObsEva SA | Compositions and methods for the treatment of estrogen-dependent disorders |
| AU2020325721A1 (en) | 2019-08-08 | 2022-03-03 | ObsEva S.A. | GnRH antagonists for the treatment of estrogen-dependent disorders |
| AU2020325655B2 (en) | 2019-08-08 | 2025-09-11 | Kissei Pharmaceutical Co., Ltd. | Compositions and methods for the treatment of estrogen-dependent disorders |
| CN115232144B (zh) * | 2021-04-22 | 2024-04-02 | 长春金赛药业有限责任公司 | 含氮稠环类衍生物、药物组合物及其制备方法和应用 |
| CN115636839B (zh) * | 2021-07-19 | 2025-11-14 | 上海科胜药物研发有限公司 | 一种稠合杂环衍生物晶型c及其制备方法 |
| CN118574626A (zh) | 2022-02-04 | 2024-08-30 | 橘生药品工业株式会社 | 经口固体制剂 |
| KR20240032679A (ko) * | 2022-09-02 | 2024-03-12 | 주식회사 렉스팜텍 | 신규 벤포티아민 콜린염 |
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| JPS56108787A (en) | 1980-01-31 | 1981-08-28 | Sato Yakugaku Kenkyusho:Kk | Camptothecin coline salt and its preparation |
| US4663348A (en) * | 1985-07-02 | 1987-05-05 | Warner-Lambert Co. | Furosemide salts and pharmaceutical preparations thereof |
| DE3830932A1 (de) * | 1988-09-12 | 1990-03-15 | Diamalt Ag | 2-hydroxy-n,n,n-trimethyl-ethanaminiumsalze von 5ss-cholan-24-saeure-derivaten |
| ZA200803335B (en) * | 2005-10-19 | 2009-10-28 | Kissei Pharmaceutical | Fused heterocyclic derivative, medicinal composition containing the same, and medicinal use thereof |
| PL1939204T6 (pl) * | 2005-10-19 | 2024-03-25 | Kissei Pharmaceutical Co., Ltd. | Skondensowana pochodna heterocykliczna, zawierająca ją kompozycja oraz jej zastosowanie medyczne |
| GB0603522D0 (en) * | 2006-02-22 | 2006-04-05 | Avidex Ltd | Kinase inhibition |
| RU2345996C1 (ru) * | 2007-07-17 | 2009-02-10 | Андрей Александрович Иващенко | Аннелированные азагетероциклические амиды, включающие пиримидиновый фрагмент, способ их получения и применения |
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2011
- 2011-02-09 JP JP2011553858A patent/JP5337261B2/ja active Active
- 2011-02-09 TW TW100104240A patent/TWI555751B/zh active
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- 2011-02-09 CA CA2788533A patent/CA2788533C/en active Active
- 2011-02-09 WO PCT/JP2011/052719 patent/WO2011099507A1/ja not_active Ceased
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