RU2017115925A - Сокристаллы модуляторов регулятора трансмембранной проводимости при кистозном фиброзе - Google Patents
Сокристаллы модуляторов регулятора трансмембранной проводимости при кистозном фиброзе Download PDFInfo
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- RU2017115925A RU2017115925A RU2017115925A RU2017115925A RU2017115925A RU 2017115925 A RU2017115925 A RU 2017115925A RU 2017115925 A RU2017115925 A RU 2017115925A RU 2017115925 A RU2017115925 A RU 2017115925A RU 2017115925 A RU2017115925 A RU 2017115925A
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- 239000013078 crystal Substances 0.000 title claims 16
- 229940125904 compound 1 Drugs 0.000 claims 17
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims 13
- 238000000034 method Methods 0.000 claims 8
- 125000001931 aliphatic group Chemical group 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- 229940124597 therapeutic agent Drugs 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- KCVWRCXEUJUXIG-UHFFFAOYSA-N 1,3-bis(icosanoyloxy)propan-2-yl icosanoate Chemical compound CCCCCCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCCCCCC KCVWRCXEUJUXIG-UHFFFAOYSA-N 0.000 claims 2
- XDSPGKDYYRNYJI-IUPFWZBJSA-N 1,3-bis[(13z)-docos-13-enoyloxy]propan-2-yl (13z)-docos-13-enoate Chemical compound CCCCCCCC\C=C/CCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCC\C=C/CCCCCCCC)COC(=O)CCCCCCCCCCC\C=C/CCCCCCCC XDSPGKDYYRNYJI-IUPFWZBJSA-N 0.000 claims 2
- MJUVRTYWUMPBTR-MRXNPFEDSA-N 1-(2,2-difluoro-1,3-benzodioxol-5-yl)-n-[1-[(2r)-2,3-dihydroxypropyl]-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)indol-5-yl]cyclopropane-1-carboxamide Chemical compound FC=1C=C2N(C[C@@H](O)CO)C(C(C)(CO)C)=CC2=CC=1NC(=O)C1(C=2C=C3OC(F)(F)OC3=CC=2)CC1 MJUVRTYWUMPBTR-MRXNPFEDSA-N 0.000 claims 2
- 201000003883 Cystic fibrosis Diseases 0.000 claims 2
- UFSKUSARDNFIRC-UHFFFAOYSA-N lumacaftor Chemical compound N1=C(C=2C=C(C=CC=2)C(O)=O)C(C)=CC=C1NC(=O)C1(C=2C=C3OC(F)(F)OC3=CC=2)CC1 UFSKUSARDNFIRC-UHFFFAOYSA-N 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims 2
- 238000001228 spectrum Methods 0.000 claims 2
- URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 claims 2
- PVNIQBQSYATKKL-UHFFFAOYSA-N tripalmitin Chemical compound CCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCC PVNIQBQSYATKKL-UHFFFAOYSA-N 0.000 claims 2
- DCXXMTOCNZCJGO-UHFFFAOYSA-N tristearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCCCC DCXXMTOCNZCJGO-UHFFFAOYSA-N 0.000 claims 2
- UBEIMDKGOYBUKT-FLIQGJDUSA-N 1,2,3-trilinolenoylglycerol Chemical compound CC\C=C/C\C=C/C\C=C/CCCCCCCC(=O)OCC(OC(=O)CCCCCCC\C=C/C\C=C/C\C=C/CC)COC(=O)CCCCCCC\C=C/C\C=C/C\C=C/CC UBEIMDKGOYBUKT-FLIQGJDUSA-N 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 1
- 206010014561 Emphysema Diseases 0.000 claims 1
- 229910005429 FeSSIF Inorganic materials 0.000 claims 1
- PHYFQTYBJUILEZ-UHFFFAOYSA-N Trioleoylglycerol Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC(OC(=O)CCCCCCCC=CCCCCCCCC)COC(=O)CCCCCCCC=CCCCCCCCC PHYFQTYBJUILEZ-UHFFFAOYSA-N 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 229960005475 antiinfective agent Drugs 0.000 claims 1
- 239000004599 antimicrobial Substances 0.000 claims 1
- 230000003115 biocidal effect Effects 0.000 claims 1
- 229940124630 bronchodilator Drugs 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000003172 expectorant agent Substances 0.000 claims 1
- 230000002496 gastric effect Effects 0.000 claims 1
- 125000003976 glyceryl group Chemical group [H]C([*])([H])C(O[H])([H])C(O[H])([H])[H] 0.000 claims 1
- 235000013773 glyceryl triacetate Nutrition 0.000 claims 1
- 239000001087 glyceryl triacetate Substances 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 claims 1
- 229940066491 mucolytics Drugs 0.000 claims 1
- 235000016709 nutrition Nutrition 0.000 claims 1
- AICOOMRHRUFYCM-ZRRPKQBOSA-N oxazine, 1 Chemical compound C([C@@H]1[C@H](C(C[C@]2(C)[C@@H]([C@H](C)N(C)C)[C@H](O)C[C@]21C)=O)CC1=CC2)C[C@H]1[C@@]1(C)[C@H]2N=C(C(C)C)OC1 AICOOMRHRUFYCM-ZRRPKQBOSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229960002622 triacetin Drugs 0.000 claims 1
- PHYFQTYBJUILEZ-IUPFWZBJSA-N triolein Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC(OC(=O)CCCCCCC\C=C/CCCCCCCC)COC(=O)CCCCCCC\C=C/CCCCCCCC PHYFQTYBJUILEZ-IUPFWZBJSA-N 0.000 claims 1
- 229940117972 triolein Drugs 0.000 claims 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
- C07D215/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
- A61K31/225—Polycarboxylic acids
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- A—HUMAN NECESSITIES
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/04—Artificial tears; Irrigation solutions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
- C07C69/02—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen
- C07C69/12—Acetic acid esters
- C07C69/18—Acetic acid esters of trihydroxylic compounds
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- C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
- C07C69/02—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen
- C07C69/22—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety
- C07C69/30—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety esterified with trihydroxylic compounds
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Emergency Medicine (AREA)
- Pulmonology (AREA)
- Ophthalmology & Optometry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Quinoline Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Claims (43)
1. Сокристалл, содержащий Соединение 1 и только один триглицерид, где триглицерид выбирают из следующих структурных формул:
где R1, R2 и R3 независимо представляют собой C1-29 алифатические группы,
и где Соединение 1 представлено следующей структурной формулой:
2. Сокристалл по п.1, отличающийся тем, что имеет картину порошковой дифракции рентгеновского излучения с характерными пиками, выраженными в градусах 2-тэта±0,2, в следующих положениях: 3,5, 6,9 и 10,9.
3. Сокристалл по п.1, отличающийся тем, что имеет картину порошковой дифракции рентгеновского излучения с характерными пиками, выраженными в градусах 2-тэта±0,2, в следующих положениях: 3,5, 6,9, 9,2, 10,9, 16,9, 18,0 и 23,8.
4. Сокристалл по п.1, отличающийся тем, что имеет спектр 13C ssNMR с характерными пиками, выраженными в м.д. ±0,1, в следующих положениях: 178,6, 155,0 и 119,4.
5. Сокристалл по п.1, отличающийся тем, что имеет спектр 13C ssNMR с характерными пиками, выраженными в м.д. ±0,1, в следующих положениях: 178,6, 155,0, 130,5 и 119,4.
6. Сокристалл по любому из пп.1-5, где стехиометрия Соединения 1 по отношению к триглицериду составляет 3:1.
7. Сокристалл по любому из пп.1-5, где стехиометрия Соединения 1 по отношению к триглицериду составляет 6:1.
8. Сокристалл по любому из пп.1-7, где Соединение 1 формирует гексамер в сокристалле и где, кроме того, R1, R2 и R3 независимо представляют собой C7-29 алифатические группы.
9. Сокристалл по любому из пп.1-8, где сокристалл растворяется в модельной желудочно-кишечной среде после еды (FeSSIF) с получением концентрации Соединения 1 больше чем 0,4 мг/мл, и эта концентрация поддерживается в течение, по меньшей мере, 10 часов.
10. Сокристалл по любому из пп.1-8, где триглицерид выбирают из: глицерилтриолеата, глицерилтристеарата, глицерилтридеканоата, глицерилтригексаноата, глицерилтридеканоата, глицерилтриоктаноата, глицерилтримиристата, глицерилтрипальмитата, глицерилтрибутирата, глицерилтрилинолеата, глицерилтридодеканоата, глицерилдеканоата, глицерилтрипальмитолеата, глицерилтриэруката, глицерилтрипропионата, пальмитодиолеина, триарахидонина, глицерилтрилинолената, триэруцина, глицерилтриарахидата, глицерилтри(цис-13-докозеноата), глицерилтрипетроселината, глицерилтрибехената, глицерилтриелаидата и триацетина.
11. Сокристалл, содержащий Соединение 1 и триглицерид, где триглицерид выбирают из следующих структурных формул,
где R1, R2 и R3 независимо представляют собой C1-29 алифатические группы
и где Соединение 1 представлено следующей структурной формулой
где сокристалл получают с помощью способа, включающего:
объединение Соединения 1 и триглицерида с образованием сокристалла.
12. Фармацевтическая композиция, содержащая терапевтически эффективное количество Соединения 1 и фармацевтически приемлемый носитель или эксципиент, где Соединение 1 представлено следующей структурной формулой
где, кроме того, по меньшей мере, 30% Соединения 1 присутствует в виде сокристалла, содержащего Соединение 1 и триглицерид, где триглицерид выбирают из следующих структурных формул:
где R1, R2 и R3 независимо представляют собой C1-29 алифатические группы.
13. Фармацевтическая композиция по п.12, дополнительно содержащая дополнительный терапевтический агент, выбранный из муколитического агента, бронходилатора, антибиотика, противоинфекционного агента, противовоспалительного агента, модулятора CFTR иного, чем Соединение 1 или из питательного агента, или из их сочетаний.
14. Фармацевтическая композиция по п.13, в которой дополнительный терапевтический агент представляет собой модулятор CFTR иной, чем Соединение 1.
15. Фармацевтическая композиция по п.14, где модулятор CFTR представляет собой (3-(6-(1-(2,2-дифторбензо[d][1,3]диоксол-5-ил)циклопропанкарбоксамидо)-3-метилпиридин-2-ил)бензойную кислоту или (R)-1-(2,2-дифторбензо[d][1,3]диоксол-5-ил)-N-(1-(2,3-дигидроксипропил)-6-фтор-2-(1-гидрокси-2-метилпропан-2-ил)-1H-индол-5-ил)циклопропанкарбоксамид.
16. Способ лечения или облегчения тяжести заболевания у пациента, где указанное заболевание выбирают из кистозного фиброза, наследственной эмфиземы, COPD или болезни сухого глаза, причём способ включает стадию введения пациенту терапевтически эффективного количества сокристалла по любому из пп.1-11.
17. Способ по п.16, в котором заболевание представляет собой кистозный фиброз.
18. Способ по любому из пп.16 и 17, дополнительно включающий совместное введение субъекту одного или нескольких дополнительных терапевтических агентов.
19. Способ по п.18, в котором дополнительный терапевтический агент представляет собой (3-(6-(1-(2,2-дифторбензо[d][1,3]диоксол-5-ил)циклопропанкарбоксамидо)-3-метилпиридин-2-ил)бензойную кислоту или (R)-1-(2,2-дифторбензо[d][1,3]диоксол-5-ил)-N-(1-(2,3-дигидроксипропил)-6-фтор-2-(1-гидрокси-2-метилпропан-2-ил)-1H-индол-5-ил)циклопропанкарбоксамид.
20. Способ по п.19, в котором дополнительный терапевтический агент вводится одновременно с сокристаллом, до него или после него.
21. Способ получения сокристаллов, содержащих Соединение 1 и триглицерид,
где Соединение 1 представлено следующей структурной формулой
и где триглицерид выбирают из следующих структурных формул:
где R1, R2 и R3 независимо представляют собой C1-29 алифатические группы;
включающий стадии:
(a) приготовления смеси, содержащей Соединение 1 и триглицерид; и
(b) нагрева смеси.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462060828P | 2014-10-07 | 2014-10-07 | |
| US62/060,828 | 2014-10-07 | ||
| PCT/US2015/054577 WO2016057730A1 (en) | 2014-10-07 | 2015-10-07 | Co-crystals of modulators of cystic fibrosis transmembrane conductance regulator |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| RU2017115925A true RU2017115925A (ru) | 2018-11-15 |
| RU2017115925A3 RU2017115925A3 (ru) | 2019-05-14 |
| RU2749213C2 RU2749213C2 (ru) | 2021-06-07 |
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| Application Number | Title | Priority Date | Filing Date |
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| RU2017115925A RU2749213C2 (ru) | 2014-10-07 | 2015-10-07 | Сокристаллы модуляторов регулятора трансмембранной проводимости при кистозном фиброзе |
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| Country | Link |
|---|---|
| US (1) | US9701639B2 (ru) |
| EP (1) | EP3204358B1 (ru) |
| JP (1) | JP6746569B2 (ru) |
| KR (1) | KR20170063954A (ru) |
| CN (1) | CN107250113B (ru) |
| AU (1) | AU2015330923B2 (ru) |
| CA (1) | CA2963945C (ru) |
| ES (1) | ES2702288T3 (ru) |
| IL (1) | IL251623B (ru) |
| MX (1) | MX370450B (ru) |
| RU (1) | RU2749213C2 (ru) |
| WO (1) | WO2016057730A1 (ru) |
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| MX2017004631A (es) | 2017-06-19 |
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| RU2749213C2 (ru) | 2021-06-07 |
| JP6746569B2 (ja) | 2020-08-26 |
| AU2015330923B2 (en) | 2020-03-12 |
| KR20170063954A (ko) | 2017-06-08 |
| EP3204358A1 (en) | 2017-08-16 |
| CA2963945C (en) | 2023-01-10 |
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