RU2018115718A - Терапевтические соединения и способы их применения - Google Patents
Терапевтические соединения и способы их применения Download PDFInfo
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- RU2018115718A RU2018115718A RU2018115718A RU2018115718A RU2018115718A RU 2018115718 A RU2018115718 A RU 2018115718A RU 2018115718 A RU2018115718 A RU 2018115718A RU 2018115718 A RU2018115718 A RU 2018115718A RU 2018115718 A RU2018115718 A RU 2018115718A
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- alkyl
- pharmaceutically acceptable
- acceptable salt
- membered
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- 150000001875 compounds Chemical class 0.000 title claims 24
- 230000001225 therapeutic effect Effects 0.000 title claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 15
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 229910052799 carbon Inorganic materials 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000004452 carbocyclyl group Chemical group 0.000 claims 6
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 5
- 229910052794 bromium Inorganic materials 0.000 claims 5
- 229910052801 chlorine Inorganic materials 0.000 claims 5
- 229910052731 fluorine Inorganic materials 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 229910052740 iodine Inorganic materials 0.000 claims 5
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 4
- 125000003282 alkyl amino group Chemical group 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000006648 (C1-C8) haloalkyl group Chemical group 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 125000004663 dialkyl amino group Chemical group 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- -1 hydroxy, amino Chemical group 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000000069 prophylactic effect Effects 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- A—HUMAN NECESSITIES
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D405/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Pyridine Compounds (AREA)
Claims (100)
1. Соединение формулы (Ix)
или его фармацевтически приемлемая соль, где
каждый RAA независимо выбран из группы, состоящей из F, Cl, Br, I, -CN,
C(=O)ORA1, SO2RA1, -ORA1, -(XRA)-(3-15-членного карбоциклила), -(XRA)-(6-12-членного арила), (XRA)-(5-12-членного гетероарила) и -RA2, где указанный 3-15-членный карбоциклил, 6-12-членный арил и 5-12-членный гетероарил в RAA необязательно замещен 1-5 заместителями Rb, независимо выбранными из группы, состоящей из F, Cl, Br, I, C1-4 алкила, C1-4 галогеналкила, амино, C1-4 алкиламино, ди(C1-4алкил)амино, C1-4(галоген)алкокси и C(O)N(Rc)2; RA1 выбран из группы, состоящей из водорода, C1-8 алкила, C2-8 алкенила, C1-8 галогеналкила, C3-8 циклоалкила, фенила и бензила; RA2 выбран из группы, состоящей из C1-8 алкила, который необязательно замещен одним или более заместителями, выбранными из оксо (=O), фтора, гидрокси, амино, C1-4 алкиламино и ди(C1-4алкил)амино; XRA выбран из группы, состоящей из отсутствующей группы, C(=O) и C1-4 алкилена; где любой C1-4 алкилен в XRA необязательно замещен 1-3 заместителями, выбранными из группы, состоящей из C1-4 алкила, C1-4 галогеналкила и фенила, который необязательно замещен 1-5 заместителями, выбранными из F, Cl, Br, I, -NH2, -OH, -CN, -NO2, C1-4 алкила, C1-4 галогеналкила, C1-4 алкокси, C1-4(галоген)алкокси, C1-4 алкиламино и C1-4 диалкиламино;
кольцо «A» представляет собой 5-12-членный гетероарил или 3-15-членный гетероциклил;
кольцо B представляет собой 5, 6 или 7-членный карбоциклил или 5, 6 или 7-членный гетероциклил, где указанный 5, 6 или 7-членный карбоциклил и 5, 6 или 7-членный гетероциклил необязательно замещен одной или более группами, независимо выбранными из C1-4 алкила, галогена и галогенC1-4 алкила;
R1b представляет собой H или C1-4 алкил;
R3, R4 и R5, каждый независимо, выбраны из группы, состоящей из H, F, Cl, Br, I, -CN, C1-8 алкила, C3-8 циклоалкила, C1-8 галогеналкила и C1-8 алкокси;
R6 выбран из группы, состоящей из H, C1-8 алкила, C3-8 циклоалкила, арила и арил(C1-4 алкила); и R7 выбран из группы, состоящей из C1-8 алкила, 3-15-членного гетероциклила, 5-12-членного гетероарила, C(O)N(Rc)2 и C(=NCN)N(Rc)2; или R6 и R7, вместе с атомом азота, к которому они присоединены, образуют 3-15-членный гетероциклил или 5-12-членный гетероарил; где любой C1-8 алкил, C3-8 циклоалкил, арил, аралкил, 3-15-членный гетероциклил и 5-12-членный гетероарил необязательно замещен одной или более группами Rd, которые независимо выбраны из группы, состоящей из F, Cl, Br, I, -NH2, -OH, -CN, -NO2, C1-4 алкила, C1-4 галогеналкила, C1-4 алкокси, C1-4(галоген)алкокси, C1-4 алкиламино и C1-4 диалкиламино; каждый Rc независимо выбран из группы, состоящей из водорода, C1-8 алкила, C3-8 циклоалкила, фенила и бензила; и
n равен 0, 1, 2, 3, 4, 5 или 6.
2. Соединение по п. 1, представляющее собой соединение формулы Ib
где кольцо B, содержащее X, представляет собой 5, 6 или 7-членный карбоциклил или 5, 6 или 7-членный гетероциклил; или его фармацевтически приемлемая соль.
3. Соединение по п. 2, представляющее собой соединение формулы Ic
или его фармацевтически приемлемая соль.
4. Соединение по п. 2, представляющее собой соединение формулы Id
где X представляет собой O, S, SO или SO2; m равен 0, 1, 2, 3, 4 или 5; и p равен 0, 1, 2, 3, 4 или 5; или его фармацевтически приемлемая соль.
5. Соединение по любому из пп. 1-4, представляющее собой соединение формулы Ih
или его фармацевтически приемлемая соль.
6. Соединение по любому из пп. 1-4, представляющее собой соединение формулы Ij
где m равен 0, 1, 2, 3, 4 или 5; и p равен 0, 1, 2, 3, 4 или 5; или его фармацевтически приемлемая соль.
7. Соединение по любому из пп. 1-6, отличающееся тем, что R7 представляет собой 5-12-членный гетероарил; или его фармацевтически приемлемая соль.
8. Соединение по любому из пп. 1-4, представляющее собой соединение формулы Ir
где кольцо B, содержащее X, представляет собой 5, 6 или 7-членный карбоциклил или 5, 6 или 7-членный гетероциклил; или его фармацевтически приемлемая соль.
или его фармацевтически приемлемая соль.
11. Соединение по п. 1, представляющее собой соединение формулы In
или его фармацевтически приемлемая соль.
12. Соединение по п. 1, представляющее собой соединение формулы Is
где m равен 0, 1, 2, 3, 4 или 5; и p равен 0, 1, 2, 3, 4 или 5; или его фармацевтически приемлемая соль.
13. Соединение по п. 2, выбранное из группы, состоящей из
или его фармацевтически приемлемая соль.
14. Фармацевтическая композиция, содержащая соединение по любому из пп. 1-13 или его фармацевтически приемлемую соль и фармацевтически приемлемое вспомогательное вещество.
15. Соединение по любому из пп. 1-13 или его фармацевтически приемлемая соль для профилактического или терапевтического лечения заболевания или расстройства, выбранного из группы, состоящей из боли, депрессии, сердечнососудистых заболеваний, респираторных заболеваний и психиатрических заболеваний, или их комбинации.
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562233863P | 2015-09-28 | 2015-09-28 | |
| US62/233,863 | 2015-09-28 | ||
| US201662298817P | 2016-02-23 | 2016-02-23 | |
| US62/298,817 | 2016-02-23 | ||
| CN2016096659 | 2016-08-25 | ||
| CNPCT/CN2016/096659 | 2016-08-25 | ||
| PCT/US2016/054011 WO2017058821A1 (en) | 2015-09-28 | 2016-09-27 | Therapeutic compounds and methods of use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2018115718A true RU2018115718A (ru) | 2019-10-28 |
| RU2018115718A3 RU2018115718A3 (ru) | 2019-12-27 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2018115718A RU2018115718A (ru) | 2015-09-28 | 2016-09-27 | Терапевтические соединения и способы их применения |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US10787446B2 (ru) |
| EP (1) | EP3356360A1 (ru) |
| JP (1) | JP6987746B2 (ru) |
| KR (1) | KR20180067561A (ru) |
| CN (1) | CN108290881B (ru) |
| AU (1) | AU2016330503B2 (ru) |
| BR (1) | BR112018006189A2 (ru) |
| CA (1) | CA2999769A1 (ru) |
| CL (1) | CL2018000805A1 (ru) |
| CO (1) | CO2018003909A2 (ru) |
| CR (1) | CR20180242A (ru) |
| HK (1) | HK1258056A1 (ru) |
| IL (1) | IL258192A (ru) |
| MX (1) | MX386501B (ru) |
| PE (1) | PE20181003A1 (ru) |
| PH (1) | PH12018500668A1 (ru) |
| RU (1) | RU2018115718A (ru) |
| SG (1) | SG10202007787RA (ru) |
| TW (1) | TWI726916B (ru) |
| WO (1) | WO2017058821A1 (ru) |
| ZA (1) | ZA201802134B (ru) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN110546148A (zh) | 2017-03-24 | 2019-12-06 | 基因泰克公司 | 作为钠通道抑制剂的4-哌啶-n-(嘧啶-4-基)色满-7-磺酰胺衍生物 |
| TW202003490A (zh) | 2018-05-22 | 2020-01-16 | 瑞士商赫孚孟拉羅股份公司 | 治療性化合物及其使用方法 |
| CN112321494B (zh) * | 2020-11-17 | 2022-04-19 | 上海凌凯医药科技有限公司 | 一种制备2-氯-4-异丙基吡啶的方法 |
| WO2023028056A1 (en) * | 2021-08-24 | 2023-03-02 | Genentech, Inc. | 3-amino piperidyl sodium channel inhibitors |
| TWI860146B (zh) * | 2023-10-30 | 2024-10-21 | 泰盈光電股份有限公司 | 電致變色組成物及電致變色裝置 |
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-
2016
- 2016-09-27 MX MX2018003828A patent/MX386501B/es unknown
- 2016-09-27 KR KR1020187012064A patent/KR20180067561A/ko not_active Ceased
- 2016-09-27 PE PE2018000486A patent/PE20181003A1/es unknown
- 2016-09-27 SG SG10202007787RA patent/SG10202007787RA/en unknown
- 2016-09-27 AU AU2016330503A patent/AU2016330503B2/en not_active Ceased
- 2016-09-27 CA CA2999769A patent/CA2999769A1/en not_active Abandoned
- 2016-09-27 CR CR20180242A patent/CR20180242A/es unknown
- 2016-09-27 CN CN201680068263.3A patent/CN108290881B/zh not_active Expired - Fee Related
- 2016-09-27 WO PCT/US2016/054011 patent/WO2017058821A1/en not_active Ceased
- 2016-09-27 HK HK19100433.4A patent/HK1258056A1/zh unknown
- 2016-09-27 RU RU2018115718A patent/RU2018115718A/ru unknown
- 2016-09-27 JP JP2018516052A patent/JP6987746B2/ja not_active Expired - Fee Related
- 2016-09-27 EP EP16781926.7A patent/EP3356360A1/en not_active Withdrawn
- 2016-09-27 BR BR112018006189A patent/BR112018006189A2/pt not_active IP Right Cessation
- 2016-09-29 TW TW105131425A patent/TWI726916B/zh not_active IP Right Cessation
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2018
- 2018-03-18 IL IL258192A patent/IL258192A/en unknown
- 2018-03-26 PH PH12018500668A patent/PH12018500668A1/en unknown
- 2018-03-28 CL CL2018000805A patent/CL2018000805A1/es unknown
- 2018-03-28 US US15/939,112 patent/US10787446B2/en active Active
- 2018-04-03 ZA ZA2018/02134A patent/ZA201802134B/en unknown
- 2018-04-12 CO CONC2018/0003909A patent/CO2018003909A2/es unknown
-
2020
- 2020-09-24 US US17/031,348 patent/US20210171516A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| MX2018003828A (es) | 2018-06-22 |
| WO2017058821A1 (en) | 2017-04-06 |
| JP2018533551A (ja) | 2018-11-15 |
| AU2016330503A1 (en) | 2018-04-12 |
| AU2016330503B2 (en) | 2021-04-08 |
| JP6987746B2 (ja) | 2022-01-05 |
| US20180291014A1 (en) | 2018-10-11 |
| CO2018003909A2 (es) | 2018-07-19 |
| US10787446B2 (en) | 2020-09-29 |
| PH12018500668A1 (en) | 2018-10-01 |
| ZA201802134B (en) | 2020-08-26 |
| TWI726916B (zh) | 2021-05-11 |
| CL2018000805A1 (es) | 2018-07-06 |
| CN108290881B (zh) | 2021-12-07 |
| MX386501B (es) | 2025-03-19 |
| CN108290881A (zh) | 2018-07-17 |
| PE20181003A1 (es) | 2018-06-26 |
| TW201718556A (zh) | 2017-06-01 |
| SG10202007787RA (en) | 2020-09-29 |
| CR20180242A (es) | 2018-08-10 |
| CA2999769A1 (en) | 2017-04-06 |
| AU2016330503A8 (en) | 2018-04-19 |
| RU2018115718A3 (ru) | 2019-12-27 |
| IL258192A (en) | 2018-05-31 |
| HK1258056A1 (zh) | 2019-11-01 |
| EP3356360A1 (en) | 2018-08-08 |
| KR20180067561A (ko) | 2018-06-20 |
| BR112018006189A2 (pt) | 2018-10-09 |
| US20210171516A1 (en) | 2021-06-10 |
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