AR096246A1 - Derivados de benzimidazol como inhibidores de bromodominio - Google Patents
Derivados de benzimidazol como inhibidores de bromodominioInfo
- Publication number
- AR096246A1 AR096246A1 ARP140101893A ARP140101893A AR096246A1 AR 096246 A1 AR096246 A1 AR 096246A1 AR P140101893 A ARP140101893 A AR P140101893A AR P140101893 A ARP140101893 A AR P140101893A AR 096246 A1 AR096246 A1 AR 096246A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- aryl
- groups
- optionally substituted
- heteroarylalkyl
- Prior art date
Links
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical class C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000172 C5-C10 aryl group Chemical group 0.000 abstract 6
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 5
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 5
- -1 azido, carbamoyl Chemical group 0.000 abstract 5
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 5
- 125000005843 halogen group Chemical group 0.000 abstract 4
- 125000004404 heteroalkyl group Chemical group 0.000 abstract 4
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 abstract 3
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 abstract 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 125000001188 haloalkyl group Chemical group 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 1
- LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 abstract 1
- ZMZDMBWJUHKJPS-UHFFFAOYSA-M Thiocyanate anion Chemical compound [S-]C#N ZMZDMBWJUHKJPS-UHFFFAOYSA-M 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000003368 amide group Chemical group 0.000 abstract 1
- 125000005620 boronic acid group Chemical group 0.000 abstract 1
- 125000003739 carbamimidoyl group Chemical group C(N)(=N)* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- ZMZDMBWJUHKJPS-UHFFFAOYSA-N hydrogen thiocyanate Natural products SC#N ZMZDMBWJUHKJPS-UHFFFAOYSA-N 0.000 abstract 1
- 125000001841 imino group Chemical group [H]N=* 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 1
- 150000003573 thiols Chemical class 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Epidemiology (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Reivindicación 1: Un compuesto de fórmula (1) donde R¹ᵃ y R¹ᵇ son en forma independiente entre sí alquilo C₁₋₆ opcionalmente sustituido con entre 1 y 5 grupos R²⁰; R²ᵃ y R²ᵇ son en forma independiente entre sí H o halo; R³ es ácido borónico o halo; o -C(O)ORᵃ, -NHC(O)ORᵃ, -NHS(O)₂Rᵃ, o -S(O)₂NRᵃRᵇ; o se selecciona entre el grupo que consiste en alquilo C₁₋₁₀, alcoxi C₁₋₁₀, amino, arilo C₅₋₁₀, arilalquilo C₆₋₂₀, heteroalquilo C₁₋₁₀, heteroarilo C₅₋₁₀, y heteroarilalquilo C₆₋₁₀, cada uno de los cuales está opcionalmente sustituido con entre 1 y 5 grupos R²⁰; uno de R⁴ᵃ y R⁴ᵇ se selecciona entre el grupo que consiste en H y alquilo C₁₋₆ opcionalmente sustituido con entre 1 y 5 grupos R²⁰, y el otro se encuentra ausente; R⁵ es -C(O)ORᵃ, -NHC(O)ORᵃ, -NHS(O)₂Rᵃ, o -S(O)₂NRᵃRᵇ; o se selecciona entre el grupo que consiste en H, alquilo C₁₋₁₀, haloalquilo C₁₋₁₀, alcoxi C₁₋₁₀, amino, arilo C₅₋₁₀, arilalquilo C₆₋₂₀, heteroalquilo C₁₋₁₀, heteroarilo C₅₋₁₀, y heteroarilalquilo C₆₋₂₀, cada uno de los cuales está opcionalmente sustituido con entre 1 y 5 grupos R²⁰; cada Rᵃ y Rᵇ se selecciona en forma independiente entre el grupo que consiste en H, alquilo C₁₋₁₀, arilo C₅₋₁₀, arilalquilo C₆₋₂₀, heteroalquilo C₁₋₁₀, heteroarilo C₁₋₁₀, y heteroarilalquilo C₆₋₂₀, cada uno de los cuales está opcionalmente sustituido con entre 1 y 5 grupos R²⁰; y cada R²⁰ se selecciona en forma independiente entre el grupo que consiste en acilo, alquilo C₁₋₁₀, alcoxi C₁₋₁₀, amino, amido, amidino, arilo C₅₋₁₀, arilalquilo C₆₋₂₀, azido, carbamoilo, carboxilo, éster de carboxilo, ciano, guanidino, halo, haloalquilo C₁₋₁₀, heteroalquilo C₁₋₁₀, heteroarilo C₅₋₁₀, heteroarilalquilo C₆₋₂₀, hidroxi, hidrazino, hidroxilo, imino, oxo, nitro, sulfinilo, ácido sulfónico, sulfonilo, tiocianato, tiol, y tiona; donde los grupos alquilo C₁₋₁₀, arilo C₅₋₁₀, arilalquilo C₆₋₂₀, heteroalquilo C₁₋₁₀, heteroarilo C₅₋₁₀, y heteroarilalquilo C₆₋₂₀ están opcionalmente sustituidos con entre 1 y 3 sustituyentes seleccionados en forma independiente entre alquilo C₁₋₆, arilo C₅₋₁₀, halo, haloalquilo C₁₋₆, ciano, hidroxilo, y alcoxi C₁₋₆; o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361821612P | 2013-05-09 | 2013-05-09 | |
| US201361826912P | 2013-05-23 | 2013-05-23 | |
| US201361860229P | 2013-07-30 | 2013-07-30 | |
| US201461951347P | 2014-03-11 | 2014-03-11 | |
| PCT/US2014/037344 WO2014182929A1 (en) | 2013-05-09 | 2014-05-08 | Benzimidazole derivatives as bromodomain inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR096246A1 true AR096246A1 (es) | 2015-12-16 |
Family
ID=50897952
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP140101893A AR096246A1 (es) | 2013-05-09 | 2014-05-09 | Derivados de benzimidazol como inhibidores de bromodominio |
Country Status (25)
| Country | Link |
|---|---|
| US (4) | US20160075695A1 (es) |
| EP (1) | EP2994469B1 (es) |
| JP (1) | JP6049942B2 (es) |
| KR (1) | KR101761049B1 (es) |
| CN (1) | CN105324379B (es) |
| AP (1) | AP2015008869A0 (es) |
| AR (1) | AR096246A1 (es) |
| AU (1) | AU2014262622B2 (es) |
| BR (1) | BR112015028017A2 (es) |
| CA (1) | CA2911408C (es) |
| CL (1) | CL2015003280A1 (es) |
| CR (1) | CR20150639A (es) |
| EA (1) | EA029091B1 (es) |
| ES (1) | ES2710120T3 (es) |
| MD (1) | MD4592B1 (es) |
| MX (1) | MX2015015478A (es) |
| NZ (1) | NZ713718A (es) |
| PE (1) | PE20160029A1 (es) |
| PH (1) | PH12015502534A1 (es) |
| PT (1) | PT2994469T (es) |
| SG (1) | SG11201509220XA (es) |
| TW (1) | TWI527811B (es) |
| UA (1) | UA112618C2 (es) |
| UY (1) | UY35559A (es) |
| WO (1) | WO2014182929A1 (es) |
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| US9636328B2 (en) * | 2013-06-21 | 2017-05-02 | Zenith Epigenetics Ltd. | Substituted bicyclic compounds as bromodomain inhibitors |
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| CN105593224B (zh) | 2013-07-31 | 2021-05-25 | 恒元生物医药科技(苏州)有限公司 | 作为溴结构域抑制剂的新型喹唑啉酮类化合物 |
| US9315501B2 (en) | 2013-11-26 | 2016-04-19 | Incyte Corporation | Bicyclic heterocycles as BET protein inhibitors |
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| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
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| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| AR084070A1 (es) * | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| EP2681200A4 (en) | 2011-03-03 | 2015-05-27 | Zalicus Pharmaceuticals Ltd | INHIBITORS OF BENZIMIDAZOLE TYPE OF SODIUM CHANNEL |
| GB201106799D0 (en) * | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
| EP2765860B1 (en) * | 2011-10-13 | 2016-08-17 | Merck Sharp & Dohme Corp. | Mineralocorticoid receptor antagonists |
| WO2013097052A1 (en) * | 2011-12-30 | 2013-07-04 | Abbott Laboratories | Bromodomain inhibitors |
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2014
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- 2014-05-08 MD MDA20150121A patent/MD4592B1/ro not_active IP Right Cessation
- 2014-05-08 BR BR112015028017A patent/BR112015028017A2/pt not_active Application Discontinuation
- 2014-05-08 MX MX2015015478A patent/MX2015015478A/es unknown
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- 2014-05-08 NZ NZ713718A patent/NZ713718A/en not_active IP Right Cessation
- 2014-05-08 WO PCT/US2014/037344 patent/WO2014182929A1/en not_active Ceased
- 2014-05-08 CN CN201480035623.0A patent/CN105324379B/zh active Active
- 2014-05-08 KR KR1020157034918A patent/KR101761049B1/ko active Active
- 2014-05-08 SG SG11201509220XA patent/SG11201509220XA/en unknown
- 2014-05-08 AU AU2014262622A patent/AU2014262622B2/en active Active
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