RU2505532C2 - Соединение - Google Patents
Соединение Download PDFInfo
- Publication number
- RU2505532C2 RU2505532C2 RU2009139443/04A RU2009139443A RU2505532C2 RU 2505532 C2 RU2505532 C2 RU 2505532C2 RU 2009139443/04 A RU2009139443/04 A RU 2009139443/04A RU 2009139443 A RU2009139443 A RU 2009139443A RU 2505532 C2 RU2505532 C2 RU 2505532C2
- Authority
- RU
- Russia
- Prior art keywords
- compound according
- acetyl
- ome
- oph
- compound
- Prior art date
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- 150000001875 compounds Chemical class 0.000 title claims abstract 13
- 230000004614 tumor growth Effects 0.000 claims abstract 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims abstract 2
- 125000002252 acyl group Chemical group 0.000 claims abstract 2
- 229910052736 halogen Inorganic materials 0.000 claims abstract 2
- 150000002367 halogens Chemical class 0.000 claims abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 6
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 239000002671 adjuvant Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- XSXHWVKGUXMUQE-UHFFFAOYSA-N osmium dioxide Inorganic materials O=[Os]=O XSXHWVKGUXMUQE-UHFFFAOYSA-N 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 0 *c1c(*)c(*)c(*)c(*)c1* Chemical compound *c1c(*)c(*)c(*)c(*)c1* 0.000 description 1
Images
Classifications
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
-
- 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
-
- 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
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Saccharide Compounds (AREA)
Abstract
Настоящее изобретение относится к области органической химии. Предложены соединение формулы (I), где А выбран из CH2 и C=O; B выбран из CH2, C=O и -S(=O)2-; R1 представляет собой -OSO2NH2; R2 выбран из С1-С6-алкоксигрупп; R3 представляет собой
где каждый R4, R5, R6, R7 и R8 независимо выбран из H, -OH, C1-C6-алкила, -O-C1-C5-алкила, -OPh, -O-CF3, ацила, -O-ацила, -NH-ацетила, -OSO2NH2, -NH2, -CN, -NO2 и галогенов; где R24 и R25 независимо выбраны из Н и -СН3; и каждый R27 и R28 представляет собой Н, и фармацевтическая композиция, содержащая соединение формулы (I), которая предназначена для предотвращения и/или ингибирования роста опухоли. 3 н. и 7 з.п. ф-лы, 2 ил., 1 табл.
Description
Claims (10)
1. Соединение формулы I:
где A выбран из CH2 и C=O;
B выбран из CH2, C=O и -S(=O)2-;
R1 представляет собой -OSO2NH2;
R2 выбран из C1-C6-алкоксигрупп;
R3 представляет собой
где каждый R4, R5, R6, R7 и R8 независимо выбран из H, -OH, C1-C6-алкила, -O-C1-C5-алкила, -OPh, -O-CF3, ацила, -O-ацила, -NH-ацетила, -OSO2NH2, -NH2, -CN, -NO2 и галогенов;
где R24 и R25 независимо выбраны из H и -CH3;
и каждый R27 и R28 представляет собой H.
где A выбран из CH2 и C=O;
B выбран из CH2, C=O и -S(=O)2-;
R1 представляет собой -OSO2NH2;
R2 выбран из C1-C6-алкоксигрупп;
R3 представляет собой
где каждый R4, R5, R6, R7 и R8 независимо выбран из H, -OH, C1-C6-алкила, -O-C1-C5-алкила, -OPh, -O-CF3, ацила, -O-ацила, -NH-ацетила, -OSO2NH2, -NH2, -CN, -NO2 и галогенов;
где R24 и R25 независимо выбраны из H и -CH3;
и каждый R27 и R28 представляет собой H.
2. Соединение по п.1, где R2 представляет собой метоксигруппу.
3. Соединение по п.1, где каждый R4, R5, R6, R7 и R8 независимо выбран из H, -OH, Me, Et, -ОМе, -OEt, -OPh, -O-iPr, -OCF3, F, Cl, -O-ацетила, -NH-ацетила, -O-SO2NH2, -NH2, -CN и -NO2.
4. Соединение по п.1, где R4 выбран из H, -OH и -CN.
5. Соединение по п.1, где R4 выбран из H, -OH, -OMe и -CN.
6. Соединение по п.1, где R5 выбран из H, -OH, Me, Et, -OMe, -OEt, -OPh, -O-iPr, -OCF3, F, Cl, -O-ацетила, -NH-ацетила, -O-SO2NH2, -NH2, -CN и -NO2.
7. Соединение по п.1, где R6 выбран из H, -OMe и -CN.
8. Соединение по п.1, где R7 выбран из H и -OMe.
9. Фармацевтическая композиция, предназначенная для предотвращения и/или ингибирования роста опухоли, которая включает:
(а) соединение по любому из пп.1-8, и
(б) фармацевтически приемлемый носитель, разбавитель, эксципиент или адъювант.
(а) соединение по любому из пп.1-8, и
(б) фармацевтически приемлемый носитель, разбавитель, эксципиент или адъювант.
10. Применение соединения по любому из пп.1-8 для изготовления лекарственного средства для предотвращения и/или ингибирования роста опухоли.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0706072.6A GB0706072D0 (en) | 2007-03-28 | 2007-03-28 | Compound |
| GB0706072.6 | 2007-03-28 | ||
| PCT/GB2008/001072 WO2008117061A2 (en) | 2007-03-28 | 2008-03-27 | Tetrahydroisoquinolines as tumour growth inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2009139443A RU2009139443A (ru) | 2011-05-10 |
| RU2505532C2 true RU2505532C2 (ru) | 2014-01-27 |
Family
ID=38050412
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2009139443/04A RU2505532C2 (ru) | 2007-03-28 | 2008-03-27 | Соединение |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US8394825B2 (ru) |
| EP (1) | EP2155192B1 (ru) |
| JP (1) | JP2010522735A (ru) |
| KR (1) | KR20090126312A (ru) |
| CN (1) | CN101677993A (ru) |
| AU (1) | AU2008231569A1 (ru) |
| CA (1) | CA2679267C (ru) |
| GB (1) | GB0706072D0 (ru) |
| IL (1) | IL200596A0 (ru) |
| RU (1) | RU2505532C2 (ru) |
| WO (1) | WO2008117061A2 (ru) |
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| TWI577670B (zh) | 2011-05-10 | 2017-04-11 | 基利科學股份有限公司 | 充當離子通道調節劑之稠合雜環化合物 |
| NO3175985T3 (ru) | 2011-07-01 | 2018-04-28 | ||
| TWI622583B (zh) | 2011-07-01 | 2018-05-01 | 基利科學股份有限公司 | 作為離子通道調節劑之稠合雜環化合物 |
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| JP2016513726A (ja) * | 2013-03-15 | 2016-05-16 | レクサン ファーマシューティカルズ インコーポレイテッド | がん細胞成長阻害剤としてのテトラヒドロイソキノリン−2−イル−(キナゾリン−4−イル)メタノン化合物 |
| US9422281B2 (en) | 2013-11-18 | 2016-08-23 | Forma Therapeutics, Inc. | Benzopiperazine compositions as BET bromodomain inhibitors |
| SMT202100125T1 (it) | 2013-11-18 | 2021-05-07 | Forma Therapeutics Inc | Composizioni di tetraidrochinolina come inibitori di bromodomini bet |
| TWI713455B (zh) | 2014-06-25 | 2020-12-21 | 美商伊凡克特治療公司 | MnK抑制劑及其相關方法 |
| GB201517216D0 (en) | 2015-09-29 | 2015-11-11 | Cancer Res Technology Ltd And Astex Therapeutics Ltd | Pharmaceutical compounds |
| GB201517217D0 (en) | 2015-09-29 | 2015-11-11 | Astex Therapeutics Ltd And Cancer Res Technology Ltd | Pharmaceutical compounds |
| CN108602814A (zh) | 2015-10-29 | 2018-09-28 | 效应治疗股份有限公司 | 抑制mnk1和mnk2的吡咯并-、吡唑并-、咪唑并-嘧啶和吡啶化合物 |
| BR112018008714A2 (pt) | 2015-10-29 | 2018-10-30 | Effector Therapeutics Inc | inibidores de isoindolina, azaisoindolina, dihidroindenona e dihidroazaindenona da mnk1 e mnk2 |
| WO2017087808A1 (en) | 2015-11-20 | 2017-05-26 | Effector Therapeutics, Inc. | Heterocyclic compounds that inhibit the kinase activity of mnk useful for treating various cancers |
| DE102017005091A1 (de) | 2016-05-30 | 2017-11-30 | Bayer Pharma Aktiengesellschaft | Substituierte 3,4-Dihydropyrido[2,3-b]pyrazin-2(1H)-one |
| DE102017005089A1 (de) | 2016-05-30 | 2017-11-30 | Bayer Pharma Aktiengesellschaft | Substitulerte 3,4-Dihydrochinoxalin-2(1H)-one |
| CN106146416B (zh) * | 2016-08-01 | 2019-02-19 | 河南大学 | 氮取代3-氧代-6-取代四氢喹喔啉结构化合物、其制备方法及其医药用途 |
| MX394700B (es) | 2017-02-14 | 2025-03-24 | Effector Therapeutics Inc | Inhibidores de mnk sustituidos con piperidina y métodos relacionados con los mismos. |
| GB201704966D0 (en) | 2017-03-28 | 2017-05-10 | Astex Therapeutics Ltd | Pharmaceutical compounds |
| GB201704965D0 (en) | 2017-03-28 | 2017-05-10 | Astex Therapeutics Ltd | Pharmaceutical compounds |
| CN106966969B (zh) * | 2017-03-29 | 2019-11-19 | 南阳师范学院 | 一种生物碱化合物及其制备方法和用途 |
| KR20210102211A (ko) | 2018-10-24 | 2021-08-19 | 이펙터 테라퓨틱스, 인크. | Mnk 억제제의 결정질 형태 |
| PL4097099T3 (pl) | 2020-02-07 | 2024-11-04 | Gasherbrum Bio, Inc. | Heterocykliczne agonisty glp-1 |
| IL322686A (en) | 2023-02-16 | 2025-10-01 | Gasherbrum Bio Inc | Heterocyclic glp-1 agonists |
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2007
- 2007-03-28 GB GBGB0706072.6A patent/GB0706072D0/en not_active Ceased
-
2008
- 2008-03-27 US US12/593,560 patent/US8394825B2/en not_active Expired - Fee Related
- 2008-03-27 AU AU2008231569A patent/AU2008231569A1/en not_active Abandoned
- 2008-03-27 CN CN200880010547A patent/CN101677993A/zh active Pending
- 2008-03-27 JP JP2010500357A patent/JP2010522735A/ja active Pending
- 2008-03-27 WO PCT/GB2008/001072 patent/WO2008117061A2/en not_active Ceased
- 2008-03-27 KR KR1020097022569A patent/KR20090126312A/ko not_active Withdrawn
- 2008-03-27 EP EP08718902.3A patent/EP2155192B1/en not_active Not-in-force
- 2008-03-27 RU RU2009139443/04A patent/RU2505532C2/ru not_active IP Right Cessation
- 2008-03-27 CA CA2679267A patent/CA2679267C/en not_active Expired - Fee Related
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Also Published As
| Publication number | Publication date |
|---|---|
| IL200596A0 (en) | 2010-05-17 |
| WO2008117061A3 (en) | 2009-05-14 |
| CN101677993A (zh) | 2010-03-24 |
| GB0706072D0 (en) | 2007-05-09 |
| EP2155192A2 (en) | 2010-02-24 |
| EP2155192B1 (en) | 2016-09-28 |
| CA2679267C (en) | 2015-12-29 |
| CA2679267A1 (en) | 2008-10-02 |
| WO2008117061A2 (en) | 2008-10-02 |
| KR20090126312A (ko) | 2009-12-08 |
| AU2008231569A1 (en) | 2008-10-02 |
| JP2010522735A (ja) | 2010-07-08 |
| RU2009139443A (ru) | 2011-05-10 |
| US20100222299A1 (en) | 2010-09-02 |
| US8394825B2 (en) | 2013-03-12 |
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