RU2017143776A - Пролекарства альвоцидиба, имеющие повышенную биодоступность - Google Patents
Пролекарства альвоцидиба, имеющие повышенную биодоступность Download PDFInfo
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- RU2017143776A RU2017143776A RU2017143776A RU2017143776A RU2017143776A RU 2017143776 A RU2017143776 A RU 2017143776A RU 2017143776 A RU2017143776 A RU 2017143776A RU 2017143776 A RU2017143776 A RU 2017143776A RU 2017143776 A RU2017143776 A RU 2017143776A
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- pharmaceutically acceptable
- acceptable salt
- compound according
- following structure
- compound
- Prior art date
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/453—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/661—Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion or mevinphos
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/06—Phosphorus compounds without P—C bonds
- C07F9/08—Esters of oxyacids of phosphorus
- C07F9/09—Esters of phosphoric acids
- C07F9/12—Esters of phosphoric acids with hydroxyaryl compounds
-
- 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
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
- C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
- C07D311/22—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
- C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
- C07D311/22—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
- C07D311/26—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3
- C07D311/28—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3 with aromatic rings attached in position 2 only
- C07D311/30—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3 with aromatic rings attached in position 2 only not hydrogenated in the hetero ring, e.g. flavones
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
Claims (41)
1. Соединение, имеющее следующую структуру (I):
(I)
или его стереоизомер, таутомер или фармацевтически приемлемая соль, где:
один из R1, R2 или R3 является -P(=O)(OH)2, и два другие из R1, R2 и R3 каждый является H.
2. Соединение по п. 1, имеющее следующую структуру (I′):
(I′)
3. Соединение по п. 1, имеющее следующую структуру (IA):
(IA)
4. Соединение по п. 3, имеющее следующую структуру (IA′):
(IA′)
5. Соединение по п. 1, имеющее следующую структуру (IB):
(IB)
6. Соединение по п. 5, имеющее следующую структуру (IB′):
(IB′)
7. Соединение по п. 1, имеющее следующую структуру (IC):
(IC)
8. Соединение по п. 7, имеющее следующую структуру (IC′):
(IC′)
9. Фармацевтически приемлемая соль соединения по любому из пп. 1-8.
10. Фармацевтически приемлемая соль по п. 9, где фармацевтически приемлемой солью является основно-аддитивная соль.
11. Фармацевтически приемлемая соль по п. 10, где фармацевтически приемлемой солью является соль натрия.
12. Фармацевтически приемлемая соль по п. 9, где фармацевтически приемлемой солью является кислотно-аддитивная соль.
13. Фармацевтически приемлемая соль по п. 12, где фармацевтически приемлемой солью является гидрохлорид.
14. Фармацевтическая композиция, содержащая фармацевтически приемлемый носитель или наполнитель и соединение по любому из пп. 1-13.
15. Фармацевтическая композиция по п. 14, где фармацевтическая композиция составлена для перорального введения.
16. Способ лечения заболевания, связанного со сверхэкспрессией циклинзависимой киназы (ЦЗК) у млекопитающих, нуждающихся в таковом, где способ включает введение терапевтически эффективного количества соединения по любому из пп. 1-13 или композиции по любому из пп. 14 или 15 млекопитающему.
17. Способ по п. 16, где заболеванием является рак.
18. Способ по п. 17, где раком является гемобластоз.
19. Способ по п. 18, где гемобластоз выбирают острого миелогенного лейкоза (ОМЛ), множественной миеломы, фолликулярной лимфомы, острого лимфобластного лейкоза (ОЛЛ), хронического лимфоцитарного лейкоза (ХЛЛ) и неходжкинской лимфомы.
20. Способ по п. 19, где гемолбластозом является острый миелогенный лейкоз (ОМЛ).
21. Способ по п. 19, где гемобластозом является хронический лимфоцитарный лейкоз (ХЛЛ).
22. Способ по п. 18, где гемобластозом является миелодиспластический синдром (МДС).
23. Способ по любому из пп. 16-22, где способ включает пероральное введение соединения по любому из пп. 1-13 или композиции по любому из пп. 14 или 15 млекопитающему.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562163188P | 2015-05-18 | 2015-05-18 | |
US62/163,188 | 2015-05-18 | ||
PCT/US2016/033099 WO2016187316A1 (en) | 2015-05-18 | 2016-05-18 | Alvocidib prodrugs having increased bioavailability |
Publications (3)
Publication Number | Publication Date |
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RU2017143776A true RU2017143776A (ru) | 2019-06-18 |
RU2017143776A3 RU2017143776A3 (ru) | 2019-11-08 |
RU2752729C2 RU2752729C2 (ru) | 2021-07-30 |
Family
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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RU2017143776A RU2752729C2 (ru) | 2015-05-18 | 2016-05-18 | Пролекарства альвоцидиба, имеющие повышенную биодоступность |
Country Status (20)
Country | Link |
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US (5) | US9758539B2 (ru) |
EP (3) | EP4086264B1 (ru) |
JP (4) | JP6510075B2 (ru) |
KR (1) | KR102608921B1 (ru) |
CN (2) | CN111349118B (ru) |
AU (2) | AU2016264212B2 (ru) |
BR (1) | BR112017024933A8 (ru) |
CA (1) | CA2985804A1 (ru) |
CY (1) | CY1121851T1 (ru) |
DK (2) | DK3298021T3 (ru) |
ES (2) | ES2739749T3 (ru) |
HK (1) | HK1251941B (ru) |
HU (1) | HUE045585T2 (ru) |
IL (1) | IL255465B (ru) |
MX (1) | MX2017014645A (ru) |
PL (1) | PL3298021T3 (ru) |
PT (1) | PT3298021T (ru) |
RU (1) | RU2752729C2 (ru) |
TR (1) | TR201911032T4 (ru) |
WO (1) | WO2016187316A1 (ru) |
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TW202038957A (zh) | 2018-12-21 | 2020-11-01 | 日商第一三共股份有限公司 | 抗體-藥物結合物與激酶抑制劑之組合 |
JP2022525149A (ja) * | 2019-03-20 | 2022-05-11 | スミトモ ダイニッポン ファーマ オンコロジー, インコーポレイテッド | ベネトクラクスが失敗した急性骨髄性白血病(aml)の処置 |
KR20210141621A (ko) | 2019-03-22 | 2021-11-23 | 스미토모 다이니폰 파마 온콜로지, 인크. | Pkm2 조정제를 포함하는 조성물 및 그를 사용한 치료 방법 |
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