RU2017101377A - Производные эксендина-4 в качестве селективных агонистов рецепторов глюкагона - Google Patents
Производные эксендина-4 в качестве селективных агонистов рецепторов глюкагона Download PDFInfo
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- IDHVLSACPFUBDY-QCDLPZBNSA-N xenin Chemical compound C([C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(C)C)C(O)=O)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCSC)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CN=CN1 IDHVLSACPFUBDY-QCDLPZBNSA-N 0.000 claims 1
- 108010006643 xenin 25 Proteins 0.000 claims 1
- UBQNRHZMVUUOMG-UHFFFAOYSA-N zonisamide Chemical compound C1=CC=C2C(CS(=O)(=O)N)=NOC2=C1 UBQNRHZMVUUOMG-UHFFFAOYSA-N 0.000 claims 1
- 229960002911 zonisamide Drugs 0.000 claims 1
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- A61K38/22—Hormones
- A61K38/2278—Vasoactive intestinal peptide [VIP]; Related peptides (e.g. Exendin)
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Claims (94)
1. Пептидное соединение с формулой (I):
Tza-Ser-Gln-Gly-Thr-Phe-Thr-Ser-Asp-X10-Ser-Lys-Gln-X14-Glu-Ser-Arg-Arg-Ala-Gln-X21-Phe-Ile-Glu-Trp-Leu-Leu-Ala-X29-Gly-Pro-Glu-Ser-Gly-Ala-Pro-Pro-Pro-Ser-R1
(I),
при этом X10 представляет собой аминокислотный остаток, выбранный из Tyr, Leu, Val, Ile, Phe, фенилглицина, 1-нафтилаланина, 2-фторфенилаланина, циклогексилглицина и трет-лейцина,
X14 представляет собой аминокислотный остаток, выбранный из Leu и Nle,
X21 представляет собой аминокислотный остаток, выбранный из Asp и Glu,
X29 представляет собой аминокислотный остаток, выбранный из Gly и Thr,
R1 представляет собой ОН или NH2,
или его соль или сольват.
2. Соединение по п. 1, где
C-концевая группа R1 представляет собой OH.
3. Соединение по любому из пп. 1-2, где
X10 представляет собой Leu,
X14 представляет собой аминокислотный остаток, выбранный из Leu и Nle,
X21 представляет собой аминокислотный остаток, выбранный из Asp и Glu,
X29 представляет собой аминокислотный остаток, выбранный из Gly и Thr,
R1 представляет собой OH,
или его соль или сольват.
4. Соединение по любому из пп. 1-3, где
X10 представляет собой Tyr,
X14 представляет собой аминокислотный остаток, выбранный из Leu и Nle,
X21 представляет собой Glu,
X29 представляет собой аминокислотный остаток, выбранный из Gly и Thr,
R1 представляет собой OH,
или его соль или сольват.
5. Соединение по любому из пп. 1-4, где
X10 представляет собой 1-нафтилаланин,
X14 представляет собой аминокислотный остаток, выбранный из Leu и Nle,
X21 представляет собой аминокислотный остаток, выбранный из Asp и Glu,
X29 представляет собой Thr,
R1 представляет собой OH,
или его соль или сольват.
6. Соединение по любому из пп. 1-5, где
X10 представляет собой циклогексилглицин,
X14 представляет собой аминокислотный остаток, выбранный из Leu и Nle,
X21 представляет собой аминокислотный остаток, выбранный из Asp и Glu,
X29 представляет собой Thr,
R1 представляет собой OH,
или его соль или сольват.
7. Соединение по любому из пп. 1-6, где
X10 представляет собой аминокислотный остаток, выбранный из Tyr, Leu, Val, Ile, фенилглицина, 1-нафтилаланина, 2-фторфенилаланина и циклогексилглицина,
X14 представляет собой Leu,
X21 представляет собой аминокислотный остаток, выбранный из Asp и Glu,
X29 представляет собой аминокислотный остаток, выбранный из Gly и Thr,
R1 представляет собой OH,
или его соль или сольват.
8. Соединение по любому из пп. 1-7, где
X10 представляет собой аминокислотный остаток, выбранный из Tyr, Leu, Ile, Phe, 1-нафтилаланина, циклогексилглицина и трет-лейцина,
X14 представляет собой Nle,
X21 представляет собой аминокислотный остаток, выбранный из Asp и Glu,
X29 представляет собой Thr,
R1 представляет собой OH,
или его соль или сольват.
9. Соединение по любому из пп. 1-8, где
X10 представляет собой аминокислотный остаток, выбранный из Leu, Phe, 1-нафтилаланина, 2-фторфенилаланина и циклогексилглицина,
X14 представляет собой аминокислотный остаток, выбранный из Leu и Nle,
X21 представляет собой Asp,
X29 представляет собой Thr,
R1 представляет собой OH,
или его соль или сольват.
10. Соединение по любому из пп. 1-9, где
X10 представляет собой аминокислотный остаток, выбранный из Tyr, Leu, Val, Ile, фенилглицина, 1-нафтилаланина, циклогексилглицина и трет-лейцина,
X14 представляет собой аминокислотный остаток, выбранный из Leu и Nle,
X21 представляет собой Glu,
X29 представляет собой аминокислотный остаток, выбранный из Gly и Thr,
R1 представляет собой OH,
или его соль или сольват.
11. Соединение по любому из пп. 1-10, где
X10 представляет собой аминокислотный остаток, выбранный из Tyr, Leu, Val, Ile, Phe, фенилглицина, 1-нафтилаланина, 2-фторфенилаланина, циклогексилглицина и трет-лейцина,
X14 представляет собой аминокислотный остаток, выбранный из Leu и Nle,
X21 представляет собой аминокислотный остаток, выбранный из Asp и Glu,
X29 представляет собой Thr,
R1 представляет собой OH,
или его соль или сольват.
12. Соединение по любому из пп. 1-11, где
X10 представляет собой аминокислотный остаток, выбранный из Tyr, Leu и Val,
X14 представляет собой Leu,
X21 представляет собой Glu,
X29 представляет собой Gly,
R1 представляет собой OH,
или его соль или сольват.
13. Соединение по любому из пп. 1-12, выбранное из соединений с SEQ ID NO: 3-25, а также их солей или сольватов.
14. Соединение по любому из пп. 1-13, выбранное из соединений с SEQ ID NO: 3, 5, 6, 9, 15, 20, 23, 24 и 25, а также их солей или сольватов.
15. Соединение по любому из пп. 1-14 для применения в медицине, в частности в медицине человека.
16. Соединение для применения по п. 15, которое присутствует в качестве активного средства в фармацевтической композиции вместе по меньшей мере с одним фармацевтически приемлемым носителем.
17. Соединение для применения по п. 15 или 16 вместе по меньшей мере с одним дополнительным терапевтически активным средством, где дополнительное терапевтически активное средство выбрано из ряда инсулина и производных инсулина, GLP-1, аналогов GLP-1 и агонистов рецептора GLP-1, двойных агонистов рецепторов GLP-1/глюкагона, двойных агонистов рецепторов GLP-1/GIP, PYY3-36 или его аналогов, панкреатического полипептида или его аналогов, агонистов рецептора глюкагона, агонистов или антагонистов рецептора GIP, антагонистов или обратных агонистов грелина, ксенина и его аналогов, ингибиторов DDP4, ингибиторов SGLT2, бигуанидов, тиазолидиндионов, двойных агонистов PPAR, сульфонилмочевин, меглитинидов, ингибиторов альфа-глюкозидазы, амилина и аналогов амилина, агонистов GPR119, циклосета, ингибиторов 11-бета-HSD, активаторов глюкокиназы, ингибиторов DGAT, ингибиторов протеин-тирозинфосфатазы 1, ингибиторов глюкозо-6-фосфатазы, ингибиторов фруктозо-1,6-бисфосфатазы, ингибиторов гликогенфосфорилазы, ингибиторов фосфоенолпируваткарбоксикиназы, ингибиторов киназы гликогенсинтазы, ингибиторов киназы пируватдегидрогеназы, альфа2-антагонистов, антагонистов CCR-2, ингибиторов HMG-CoA-редуктазы, фибратов, никотиновой кислоты и ее производных, агонистов или модуляторов PPAR-(альфа, гамма или альфа/гамма), агонистов PPAR-дельта, ингибиторов ACAT, ингибиторов абсорбции холестерина, веществ, связывающих желчные кислоты, ингибиторов IBAT, ингибиторов MTP, модуляторов PCSK9, соединений, повышающих уровень HDL, регуляторов ABC, активных веществ для лечения ожирения, таких как сибутрамин, тезофензин, орлистат, антагонисты рецептора CB-1, антагонисты MCH-1, агонисты рецептора MC4, антагонисты NPY5 или NPY2, агонисты NPY4, бета-3-агонисты, лептин или лептиномиметики, агонисты рецептора 5HT2c или комбинации бупропиона/налтрексона (CONTRAVE), бупропиона/зонисамида (EMPATIC), бупропиона/фентермина или прамлинтида/метрелептина, лекарственных средств для воздействия на высокое кровяное давление, хроническую сердечную недостаточность или атеросклероз, таких как антагонисты рецептора ангиотензина II, ингибиторы ACE, ингибиторы ECE, диуретики, бета-блокаторы, антагонисты кальция, средства против гипертензии центрального действия, антагонисты альфа-2-адренергических рецепторов, ингибиторы нейтральной эндопептидазы, ингибиторы агрегации тромбоцитов.
18. Соединение для применения по любому из пп. 15-17 для лечения гипогликемии, повышенного уровня глюкозы в крови или в качестве вспомогательной терапии с инсулином.
19. Соединение для применения по любому из пп. 15-17 для снижения и поддержания веса тела, в качестве антидота при интоксикации бета-блокаторами и блокаторами кальциевых каналов и для индуцирования временного расслабления желудочно-кишечной системы при применениях для рентгенологических процедур.
20. Соединение для применения по любому из пп. 15-17 для лечения или предупреждения гипогликемии, сахарного диабета 2-го типа и для задержки развития от преддиабета до сахарного диабета 2-го типа.
21. Фармацевтическая композиция, содержащая по меньшей мере одно соединение по любому из пп. 1-14 или физиологически приемлемые соль или растворители любого из них.
22. Способ лечения гипогликемии у пациента, причем способ включает введение пациенту эффективного количества по меньшей мере одного соединения формулы I по любому из пп. 1-14.
23. Способ лечения гипогликемии у пациента, причем способ включает введение пациенту эффективного количества по меньшей мере одного соединения формулы I по любому из пп. 1-14 и эффективного количества по меньшей мере одного другого соединения, пригодного для лечения гипогликемии.
24. Способ по любому из пп. 22-23, где эффективное количество по меньшей мере одного соединения формулы I и эффективное количество по меньшей мере одного другого соединения вводят одновременно, раздельно или последовательно.
25. Способ по любому из пп. 22-24, при котором введение осуществляют парентерально.
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| PCT/EP2015/063607 WO2015193381A1 (en) | 2014-06-18 | 2015-06-17 | Exendin-4 derivatives as selective glucagon receptor agonists |
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| UA116217C2 (uk) | 2012-10-09 | 2018-02-26 | Санофі | Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону |
| CA2894765A1 (en) | 2012-12-21 | 2014-06-26 | Sanofi | Exendin-4 derivatives as dual glp1/gip or trigonal glp1/gip/glucagon agonists |
| WO2015086728A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Exendin-4 peptide analogues as dual glp-1/gip receptor agonists |
| WO2015086730A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Non-acylated exendin-4 peptide analogues |
| WO2015086733A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Dual glp-1/glucagon receptor agonists |
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| WO2015086731A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Exendin-4 peptide analogues as dual glp-1/glucagon receptor agonists |
| WO2015086730A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Non-acylated exendin-4 peptide analogues |
| EP3080151A1 (en) | 2013-12-13 | 2016-10-19 | Sanofi | Exendin-4 peptide analogues |
| WO2015086728A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Exendin-4 peptide analogues as dual glp-1/gip receptor agonists |
| CN103665148B (zh) | 2013-12-17 | 2016-05-11 | 中国药科大学 | 一种可口服给药的降糖多肽及其制法和用途 |
| CN103980358B (zh) | 2014-01-03 | 2016-08-31 | 杭州阿诺生物医药科技股份有限公司 | 一种制备利拉鲁肽的方法 |
| RU2016132386A (ru) | 2014-01-09 | 2018-02-14 | Санофи | Стабилизированные фармацевтические составы без глицерина на основе инсулиновых аналогов и/или инсулиновых производных |
| AU2015205624A1 (en) | 2014-01-09 | 2016-07-14 | Sanofi | Stabilized pharmaceutical formulations of insulin analogues and/or insulin derivatives |
| TW201625670A (zh) | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | 衍生自ｅｘｅｎｄｉｎ－４之雙重ｇｌｐ－１／升糖素受體促效劑 |
| TW201625668A (zh) | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | 作為胜肽性雙重ｇｌｐ－１／昇糖素受體激動劑之艾塞那肽－４衍生物 |
| TW201625669A (zh) | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | 衍生自艾塞那肽－４（Ｅｘｅｎｄｉｎ－４）之肽類雙重ＧＬＰ－１／升糖素受體促效劑 |
| US9932381B2 (en) | 2014-06-18 | 2018-04-03 | Sanofi | Exendin-4 derivatives as selective glucagon receptor agonists |
| CN104926934B (zh) | 2014-09-23 | 2016-11-09 | 蒋先兴 | 胃泌酸调节素类似物 |
| AR105284A1 (es) | 2015-07-10 | 2017-09-20 | Sanofi Sa | Derivados de exendina-4 como agonistas peptídicos duales específicos de los receptores de glp-1 / glucagón |
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- 2015-06-16 TW TW104119339A patent/TW201613633A/zh unknown
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- 2015-06-17 CA CA2951077A patent/CA2951077A1/en not_active Abandoned
- 2015-06-17 KR KR1020177001097A patent/KR20170018433A/ko not_active Withdrawn
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| US20150368311A1 (en) | 2015-12-24 |
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| AR100888A1 (es) | 2016-11-09 |
| CY1121032T1 (el) | 2019-12-11 |
| CN106715466A (zh) | 2017-05-24 |
| CA2951077A1 (en) | 2015-12-23 |
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| PT3157949T (pt) | 2018-11-09 |
| AU2015276203A1 (en) | 2016-12-15 |
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| US9932381B2 (en) | 2018-04-03 |
| HRP20181708T1 (hr) | 2018-12-28 |
| LT3157949T (lt) | 2018-11-12 |
| JP6581606B2 (ja) | 2019-09-25 |
| MX2016016868A (es) | 2017-03-27 |
| SI3157949T1 (sl) | 2018-11-30 |
| TW201613633A (en) | 2016-04-16 |
| RU2017101377A3 (ru) | 2019-02-06 |
| EP3157949B1 (en) | 2018-07-18 |
| DK3157949T3 (en) | 2018-11-12 |
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| CN106715466B (zh) | 2020-09-15 |
| UY36179A (es) | 2016-01-29 |
| ES2691534T3 (es) | 2018-11-27 |
| EP3157949A1 (en) | 2017-04-26 |
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| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
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