AR104259A1 - Inhibidores de bromodominio - Google Patents
Inhibidores de bromodominioInfo
- Publication number
- AR104259A1 AR104259A1 ARP160101014A ARP160101014A AR104259A1 AR 104259 A1 AR104259 A1 AR 104259A1 AR P160101014 A ARP160101014 A AR P160101014A AR P160101014 A ARP160101014 A AR P160101014A AR 104259 A1 AR104259 A1 AR 104259A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydrogen
- halogen
- cycloalkylalkyl
- alkoxy
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
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- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/428—Thiazoles condensed with carbocyclic rings
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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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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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
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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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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- 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
- C07D401/14—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 three or more hetero rings
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- 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
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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
-
- 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
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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
- C07D417/04—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 directly linked by a ring-member-to-ring-member bond
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- 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
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- 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
- C07D471/06—Peri-condensed systems
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- 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
- C07D491/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
Abstract
Compuestos derivados heterocíclicos sustituidos, a composiciones que comprenden dichos compuestos, y al uso de dichos compuestos y composiciones para la regulación epigenética por inhibición del reconocimiento mediado por bromodominio de regiones de acetil lisina de las proteínas, tales como histonas. Dichas composiciones y métodos son útiles para el tratamiento del cáncer y las enfermedades neoplásicas. Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable de dicho compuesto, en donde el Anillo A es un anillo heteroarilo de 5 ó 6 miembros opcionalmente sustituido que contiene al menos un átomo de S o N, o un anillo heterociclilo de 5 ó 6 miembros opcionalmente sustituido que contiene al menos un átomo de S o N; X² es N o C-R¹², en el cual R¹² es hidrógeno, halógeno, alquilo o alcoxi; X⁵ es N o C-R¹⁵, en el cual R¹⁵ es hidrógeno, halógeno, -CN, alquilo o alcoxi; X⁶ es N o C-R¹⁶, en el cual R¹⁶ es hidrógeno, halógeno o -W-X, en donde W es un enlace, -O-, -S- o -NH-, y X es alquilo, alquinilo, arilo, aralquilo, cicloalquilo, cicloalquilalquilo, cicloalquilalquinilo, heterociclilo, heterociclilalquilo, heteroarilo o heteroarilalquilo; y G es un compuesto de fórmula (2) en donde, R²² es alquilo; R²³ es hidrógeno, halógeno o alquilo; u opcionalmente, cuando R²³ es alquilo, R²² y R²³ se unen para formar un anillo opcionalmente sustituido; R²⁵ es hidrógeno, halógeno, alquilo, alcoxi o alquenilo; R²⁶ es hidrógeno, halógeno, alquilo, alcoxi, aminoalquilo o alquenilo; u opcionalmente, cuando R²³ es hidrógeno, R²⁵ no es hidrógeno y R²⁶ no es hidrógeno o halógeno, R²⁵ y R²⁶ se unen para formar un anillo opcionalmente sustituido; con la condición de que el compuesto de fórmula (1) no sea: 4-(3,4-dihidro-2H-benzo[b][1,4]oxazin-6-il)-2-metilisoquinolin-1(2H)-ona; 2-metil-4-(2-oxoindolin-6-il)isoquinolin-1(2H)-ona; 4-metil-6-(2-metil-1-oxo-1,2-dihidroisoquinolin-4-il)-2H-benzo[b][1,4]oxazin-3(4H)-ona; ni 4-(1-ciclobutil-4H-spiro[benzo[d][1,3]dioxin-2,4-piperidin]-6-il)-2-metilisoquinolin-1(2H)-ona. Reivindicación 4: Un compuesto de fórmula (3), o una sal farmacéuticamente aceptable de dicho compuesto, en donde cada R¹² es independientemente hidrógeno, halógeno, alquilo o alcoxi; R¹³ es -Y-Z, en donde Y se selecciona de un enlace, -CH₂- o -CH(alquilo C₁₋₄)-; Z se selecciona de -SO₂Rᵇ, -N(Rᵃ)SO₂Rᵇ, -SO₂N(Rᵃ)₂, -N(Rᵃ)SO₂N(Rᵃ)₂, -CON(Rᵃ)₂, -N(Rᵃ)CO₂Rᵃ, -N(Rᵃ)CON(Rᵃ)₂, -N(Rᵃ)CORᵃ, -OC(O)N(Rᵃ)₂, -OSO₂N(Rᵃ)₂ o -N(Rᵃ)SO₃Rᵇ; cada Rᵃ es independientemente hidrógeno, alquilo, cicloalquilo, cicloalquilalquilo, arilo, aralquilo, heterociclilo, heterociclilalquilo, heteroarilo o heteroarilalquilo; Rᵇ es alquilo, cicloalquilo, cicloalquilalquilo, arilo, aralquilo, heterociclilo, heterociclilalquilo, heteroarilo o heteroarilalquilo; R¹⁶ es alquilo, alquinilo, arilo, aralquilo, cicloalquilo, cicloalquilalquilo, cicloalquilalquinilo, heterociclilo, heterociclilalquilo, heteroarilo o heteroarilalquilo; y G es un resto de fórmula (2) en donde, R²² es alquilo; R²³ es hidrógeno, halógeno o alquilo; u opcionalmente, cuando R²³ es alquilo, entonces R²² y R²³ se unen para formar un anillo opcionalmente sustituido; R²⁵ es hidrógeno, halógeno, alquilo, alcoxi o alquenilo; R²⁶ es hidrógeno, halógeno, alquilo, alcoxi, aminoalquilo o alquenilo; u, opcionalmente, cuando R²³ es hidrógeno, R²⁵ no es hidrógeno, y R²⁶ no es hidrógeno o halógeno, entonces R²⁵ y R²⁶ se unen para formar un anillo opcionalmente sustituido. Reivindicación 52: Un compuesto de fórmula (4), o una sal farmacéuticamente aceptable de dicho compuesto, en donde, el Anillo A es un anillo heteroarilo de 5 ó 6 miembros opcionalmente sustituido que contiene al menos un átomo de S o N, o un anillo heterociclilo de 5 ó 6 miembros opcionalmente sustituido que contiene al menos un átomo de S o N; X² es N o C-R¹², en el cual R¹² es hidrógeno, halógeno, alquilo o alcoxi; X⁵ es N o C-R¹⁵, en el cual R¹⁵ es hidrógeno, halógeno, -CN, alquilo o alcoxi; y X⁶ es N o C-R¹⁶, en el cual R¹⁶ es hidrógeno, halógeno o -W-X, en donde W es un enlace, -O-, -S- o -NH-, y X es alquilo, alquinilo, arilo, aralquilo, cicloalquilo, cicloalquilalquilo, cicloalquilalquinilo, heterociclilo, heterociclilalquilo, heteroarilo o heteroarilalquilo. Reivindicación 57: Un compuesto de fórmula (5), o una sal farmacéuticamente aceptable de dicho compuesto, en el cual la fórmula (5) es como se muestra, en donde n es 0 a 4; m es 0 ó 1; RA es un halógeno, alquilo C₁₋₃ o alcoxi C₁₋₃; J es N o C-R¹², en donde R¹² es hidrógeno, halógeno, alquilo o alcoxi; R¹³ es -Y-Z, en el cual Y es un enlace, -CH₂- o -CH(alquilo C₁₋₄)-, y Z es -SO₂R²¹, -N(R²²)SO₂R²¹, -SO₂N(R²²)₂, -N(R²²)SO₂N(R²²)₂, -CON(R²²)₂, -N(R²²)CO₂R²¹, -N(R²²)CON(R²²)₂, -N(R²²)COR²¹, -COR²¹, -OC(O)N(R²²)₂, -OSO₂N(R²²)₂ o -N(R²²)SO₃R²¹, en donde cada R²¹ es independientemente alquilo, cicloalquilo, cicloalquilalquilo, arilo, aralquilo, heterociclilo, heterociclilalquilo, heteroarilo o heteroarilalquilo, y cada R²² es independientemente hidrógeno, alquilo, cicloalquilo, cicloalquilalquilo, arilo, aralquilo, heterociclilo, heterociclilalquilo, heteroarilo o heteroarilalquilo; K es N o C-R¹⁴, en donde R¹⁴ es hidrógeno, halógeno, -CN, alquilo, cicloalquilo o alcoxi; Q es N o C-R¹⁵, en donde R¹⁵ es hidrógeno, halógeno, -CN, alquilo, alcoxi, ariloxi, aralquiloxi, cicloalquilalquiloxi, heterocicliloxi, heteroarilalquiloxi o alquiniloxi; y R¹⁶ es hidrógeno, halógeno, -N(H)COX o -W-X, en donde W es un enlace, -O-, -S- o -NH-, y X se selecciona de alquilo, arilo, aralquilo, cicloalquilo, cicloalquilalquilo, alquinilo, cicloalquilalquinilo, heterociclilo, heterociclilalquilo, heteroarilo o heteroarilalquilo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US201562148098P | 2015-04-15 | 2015-04-15 |
Publications (1)
Publication Number | Publication Date |
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AR104259A1 true AR104259A1 (es) | 2017-07-05 |
Family
ID=57126317
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP160101014A AR104259A1 (es) | 2015-04-15 | 2016-04-14 | Inhibidores de bromodominio |
Country Status (21)
Country | Link |
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US (3) | US9908885B2 (es) |
EP (2) | EP3283077B1 (es) |
JP (1) | JP6856543B2 (es) |
KR (1) | KR20170135938A (es) |
CN (1) | CN107635558A (es) |
AR (1) | AR104259A1 (es) |
AU (1) | AU2016249273B2 (es) |
CA (1) | CA2982588A1 (es) |
CL (1) | CL2017002606A1 (es) |
CO (1) | CO2017011484A2 (es) |
EA (1) | EA201792229A1 (es) |
EC (1) | ECSP17070706A (es) |
ES (1) | ES2868355T3 (es) |
HK (1) | HK1243326A1 (es) |
IL (1) | IL255006A0 (es) |
MX (1) | MX2017013207A (es) |
PE (1) | PE20180258A1 (es) |
PH (1) | PH12017501888A1 (es) |
SG (1) | SG11201708470SA (es) |
TW (1) | TW201643153A (es) |
WO (1) | WO2016168682A2 (es) |
Families Citing this family (31)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AR104259A1 (es) * | 2015-04-15 | 2017-07-05 | Celgene Quanticel Res Inc | Inhibidores de bromodominio |
US10836742B2 (en) | 2015-08-11 | 2020-11-17 | Neomed Institute | N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals |
MX2018001751A (es) | 2015-08-11 | 2018-08-01 | Neomed Inst | Dihidroquinolinonas aril-sustituidas, su preparacion y su uso como farmaceuticos. |
ES2904258T3 (es) * | 2015-08-12 | 2022-04-04 | Neomed Inst | Bencimidazoles sustituidos, su preparación y su uso como productos farmacéuticos |
US10501459B2 (en) | 2015-10-21 | 2019-12-10 | Neomed Institute | Substituted imidazo[1,2-a]pyridines as bromodomain inhibitors |
US10519151B2 (en) | 2016-01-28 | 2019-12-31 | Neomed Institute | Substituted [1,2,4]triazolo[4,3-A]pyridines, their preparation and their use as pharmaceuticals |
US10150754B2 (en) | 2016-04-19 | 2018-12-11 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
CN108314680A (zh) * | 2017-01-16 | 2018-07-24 | 凯惠科技发展(上海)有限公司 | 一种含芳环化合物、其制备方法、药物组合物及应用 |
TWI788343B (zh) | 2017-04-18 | 2023-01-01 | 美商塞爾基因定量細胞研究公司 | 治療用化合物 |
CN107098844B (zh) * | 2017-05-17 | 2019-07-30 | 许昌学院 | 一种c-5位硝基取代的酰基吲哚啉类化合物的合成方法 |
CA3086054A1 (en) * | 2017-12-20 | 2019-06-27 | Betta Pharmaceuticals Co., Ltd | Compound functioning as bromodomain protein inhibitor, and composition |
EP3746135A4 (en) | 2018-01-30 | 2022-03-09 | Foghorn Therapeutics Inc. | METHODS AND COMPOUNDS FOR TREATMENT OF DISEASE |
CN108516973A (zh) * | 2018-03-30 | 2018-09-11 | 广西师范大学 | 3-苯并噻唑-1-(3-二甲氨基)丙基喹啉-4-酮衍生物及其制备方法和应用 |
SG11202100346PA (en) * | 2018-07-23 | 2021-02-25 | Celgene Quanticel Research Inc | Process for the preparation of bromodomain inhibitor |
AU2019353144B2 (en) | 2018-10-05 | 2023-11-16 | Annapurna Bio, Inc. | Compounds and compositions for treating conditions associated with APJ receptor activity |
CA3116931A1 (en) | 2018-10-30 | 2020-05-07 | Nuvation Bio Inc. | Heterocyclic compounds as bet inhibitors |
CN113874016A (zh) * | 2019-01-29 | 2021-12-31 | 福宏治疗公司 | 化合物及其用途 |
US20220098190A1 (en) * | 2019-01-29 | 2022-03-31 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
WO2020160193A2 (en) * | 2019-01-29 | 2020-08-06 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
JP2022053557A (ja) * | 2019-02-08 | 2022-04-06 | マルホ株式会社 | ピリドン誘導体 |
US20220259200A1 (en) * | 2019-04-24 | 2022-08-18 | Convergene, Llc | Small molecule bromodomain inhibitors and uses therof |
CN112174945B (zh) * | 2019-07-02 | 2022-06-07 | 四川大学 | 具有抗癌作用的吲唑类化合物及其制备方法和用途 |
WO2021003310A1 (en) | 2019-07-02 | 2021-01-07 | Nuvation Bio Inc. | Heterocyclic compounds as bet inhibitors |
US20220289711A1 (en) * | 2019-07-31 | 2022-09-15 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
EP4096651A4 (en) | 2020-01-29 | 2024-01-24 | Foghorn Therapeutics Inc | COMPOUNDS AND THEIR USES |
WO2022025880A1 (en) * | 2020-07-29 | 2022-02-03 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
US11787800B2 (en) | 2020-07-29 | 2023-10-17 | Foghorn Therapeutics Inc. | BRD9 degraders and uses thereof |
WO2023283263A1 (en) | 2021-07-06 | 2023-01-12 | Foghorn Therapeutics Inc. | Citrate salt, pharmaceutical compositions, and methods of making and using the same |
CN114014842B (zh) * | 2021-11-04 | 2024-03-01 | 中国药科大学 | 一种杂环酮类化合物与其组合物及其制备方法和应用 |
WO2023090859A1 (ko) * | 2021-11-17 | 2023-05-25 | 일동제약(주) | 아이속사졸 유도체의 제조 방법 및 그의 신규한 중간체 |
GB202213163D0 (en) | 2022-09-08 | 2022-10-26 | Cambridge Entpr Ltd | Novel compounds, compositions and therapeutic uses thereof |
Family Cites Families (68)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US1349418A (en) * | 1919-08-05 | 1920-08-10 | George F Flynn | Motor-support |
US3590036A (en) * | 1968-11-18 | 1971-06-29 | George Y Lesher | Naphthyridine-3-carboxylic acids,their derivatives and preparation thereof |
DE2011970A1 (en) | 1970-03-13 | 1971-11-18 | CH. Boehringer Sohn, 6507 Ingelheim | Imidazo-(1, 2-a)- pyrimidines prepn |
US3635667A (en) | 1970-07-23 | 1972-01-18 | Fmc Corp | Drycleaning with hydrogen peroxide |
GB1322318A (en) * | 1971-05-19 | 1973-07-04 | Sterling Drug Inc | 1-alkyl-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids and esters |
BE786028A (fr) | 1971-07-08 | 1973-01-08 | Boehringer Sohn Ingelheim | 2,3-dihydro-oxo-imidazo(1,2-a)-pyrimidines, leurs sels d'addition avec des acides et procedes pour les fabriquer |
DE2356005A1 (de) | 1973-11-09 | 1975-05-22 | Boehringer Sohn Ingelheim | Neue 7-amino-imidazo eckige klammer auf 1,2-a eckige klammer zu pyrimidine, diese enthaltende arzneimittel sowie verfahren zu deren herstellung |
AU577105B2 (en) | 1985-04-02 | 1988-09-15 | T.P.O. :Pharmachim: | Acylaminic penicillin derivatives |
US6117940A (en) | 1997-10-17 | 2000-09-12 | Mjalli; Adnan M. M. | Amino-ketone solid support templates |
EP1300396B1 (en) * | 2000-06-12 | 2009-01-14 | Eisai R&D Management Co., Ltd. | 1,2-dihydropyridine compounds, process for preparation of the same and use thereof |
GB0129260D0 (en) * | 2001-12-06 | 2002-01-23 | Eisai London Res Lab Ltd | Pharmaceutical compositions and their uses |
ES2298615T3 (es) | 2002-09-26 | 2008-05-16 | Pfizer Inc. | Pirazol amidas para el tratamiento de infecciones vih. |
JP2005089352A (ja) | 2003-09-16 | 2005-04-07 | Kissei Pharmaceut Co Ltd | 新規なイミダゾ[1,5−a]ピラジン誘導体、それを含有する医薬組成物およびそれらの用途 |
WO2005030791A2 (en) | 2003-09-23 | 2005-04-07 | Merck & Co., Inc. | Isoquinolinone potassium channel inhibitors |
CA2539546C (en) * | 2003-09-23 | 2010-07-13 | Merck & Co., Inc. | Isoquinoline potassium channel inhibitors |
KR100703068B1 (ko) | 2003-12-30 | 2007-04-05 | 에스케이케미칼주식회사 | 피리딘 유도체와 이의 제조방법, 및 이를 포함하는약제조성물 |
TW200536830A (en) * | 2004-02-06 | 2005-11-16 | Chugai Pharmaceutical Co Ltd | 1-(2H)-isoquinolone derivative |
JP4978192B2 (ja) | 2004-04-01 | 2012-07-18 | アステラス製薬株式会社 | ピラジン誘導体およびその医薬的使用 |
GB0420722D0 (en) | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
KR100781704B1 (ko) | 2005-04-20 | 2007-12-03 | 에스케이케미칼주식회사 | 피리딘 유도체와 이의 제조방법, 및 이를 포함하는약제조성물 |
US7452892B2 (en) | 2005-06-17 | 2008-11-18 | Bristol-Myers Squibb Company | Triazolopyrimidine cannabinoid receptor 1 antagonists |
ES2423006T3 (es) | 2005-07-26 | 2013-09-17 | Sanofi | Derivados de isoquinolona sustituidos con piperidinilo como inhibidores de la cinasa Rho |
CA2615663C (en) | 2005-07-26 | 2013-10-15 | Sanofi-Aventis | Cyclohexylamin isoquinolone derivatives as rho-kinase inhibitors |
US20070099911A1 (en) | 2005-10-28 | 2007-05-03 | Wyeth | Pyrroloquinolinone derivatives as 5-hydroxytryptamine-6 ligands |
CN101426373A (zh) * | 2006-03-10 | 2009-05-06 | 神经原公司 | 哌嗪基氧代烷基四氢异喹啉及相关类似物 |
GB0612428D0 (en) | 2006-06-22 | 2006-08-02 | Prolysis Ltd | Antibacterial agents |
CN101616909B (zh) | 2006-12-27 | 2013-09-11 | 塞诺菲-安万特股份有限公司 | 作为Rho-激酶抑制剂的被取代的异喹啉和异喹啉酮衍生物 |
DE602007010981D1 (de) | 2006-12-27 | 2011-01-13 | Sanofi Aventis | Cycloalkylaminsubstituierte isochinolin- und isochinolinonderivate |
RU2457203C2 (ru) | 2006-12-27 | 2012-07-27 | Санофи-Авентис | Замещенные циклоалкиламином производные изохинолона |
WO2009029214A1 (en) * | 2007-08-23 | 2009-03-05 | Amgen Inc. | Isoquinolone derivatives as phosphodiesterase 10 inhibitors |
JP5524083B2 (ja) | 2008-01-30 | 2014-06-18 | セファロン、インク. | ヒスタミン−3(h3)受容体リガンドとしての置換スピロ環状ピペリジン誘導体 |
JP5433691B2 (ja) | 2008-06-25 | 2014-03-05 | ブリストル−マイヤーズ スクイブ カンパニー | Hiv結合阻害剤としてのジケトピペリジン誘導体 |
WO2010039186A2 (en) * | 2008-09-23 | 2010-04-08 | Renovis, Inc. | Compounds useful as faah modulators and uses thereof |
EP2196465A1 (en) | 2008-12-15 | 2010-06-16 | Almirall, S.A. | (3-oxo)pyridazin-4-ylurea derivatives as PDE4 inhibitors |
EP2379564A1 (en) * | 2008-12-19 | 2011-10-26 | Schering Corporation | Bicyclic heterocyclic derivatives and methods of use thereof |
EP3070077B1 (en) | 2009-10-06 | 2018-11-28 | Millennium Pharmaceuticals, Inc. | Heterocyclic compounds useful as pdk1 inhibitors |
US8754113B2 (en) | 2009-12-15 | 2014-06-17 | Shionogi & Co., Ltd. | Oxadiazole derivative having endothelial lipase inhibitory activity |
CN102958930B (zh) | 2010-06-28 | 2018-04-27 | 默克专利有限公司 | 作为用于对抗癌症的激酶抑制剂的2,4-二芳基取代的[1,8]二氮杂萘化合物 |
JPWO2012086735A1 (ja) * | 2010-12-22 | 2014-06-05 | 大正製薬株式会社 | 縮合複素環化合物 |
CA2837199A1 (en) * | 2011-05-23 | 2012-11-29 | Elan Pharmaceuticals, Inc. | Cinnoline compounds as inhibitor of lrrk2 kinase activity |
RU2477723C2 (ru) * | 2011-06-16 | 2013-03-20 | Общество С Ограниченной Ответственностью "Фьюжн Фарма" | Ингибиторы протеинкиназ (варианты), их применение для лечения онкологических заболеваний и фармацевтическая композиция на их основе |
CN102827073A (zh) | 2011-06-17 | 2012-12-19 | 安吉奥斯医药品有限公司 | 治疗活性组合物和它们的使用方法 |
BR112014010368A2 (pt) | 2011-10-31 | 2017-04-25 | Xenon Pharmaceuticals Inc | biaril éter sulfonamidas e seu uso como agentes terapêuticos |
CN103183675A (zh) | 2011-12-27 | 2013-07-03 | 山东轩竹医药科技有限公司 | 磷酸二酯酶-4抑制剂 |
US9434743B2 (en) * | 2012-03-02 | 2016-09-06 | Takeda Pharmaceutical Company Limited | Indazole derivatives |
US9550737B2 (en) | 2012-06-11 | 2017-01-24 | Ucb Biopharma Sprl | TNF -α modulating benzimidazoles |
JP2014024838A (ja) * | 2012-06-21 | 2014-02-06 | Taisho Pharmaceutical Co Ltd | 縮合複素環化合物を有効成分として含有する血糖低下作用薬 |
EP2875007B1 (en) * | 2012-07-19 | 2016-08-24 | Bristol-Myers Squibb Company | Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase |
WO2014080291A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Biaryl derivatives as bromodomain inhibitors |
CN104903320B (zh) | 2013-01-11 | 2018-11-13 | 富士胶片株式会社 | 含氮杂环化合物或其盐 |
WO2014164596A1 (en) * | 2013-03-11 | 2014-10-09 | The Regents Of The University Of Michigan | Bet bromodomain inhibitors and therapeutic methods using the same |
RU2680100C9 (ru) * | 2013-03-15 | 2019-04-18 | Плексксикон Инк. | Гетероциклические соединения и их применения |
EP3004109A1 (en) * | 2013-05-27 | 2016-04-13 | Novartis AG | Imidazopyrrolidinone derivatives and their use in the treatment of disease |
EP3010917B1 (en) * | 2013-06-21 | 2018-01-31 | Zenith Epigenetics Ltd. | Novel substituted bicyclic compounds as bromodomain inhibitors |
WO2014205594A1 (en) * | 2013-06-24 | 2014-12-31 | Merck Sharp & Dohme Corp. | Substituted benzofuran compounds and methods of use thereof for treatment of viral diseases |
RS58273B1 (sr) * | 2013-06-26 | 2019-03-29 | Abbvie Inc | Primarni karboksamidi kao btk inhibitori |
ES2930305T3 (es) * | 2013-10-18 | 2022-12-09 | Celgene Quanticel Res Inc | Inhibidores del bromodominio |
US9315501B2 (en) * | 2013-11-26 | 2016-04-19 | Incyte Corporation | Bicyclic heterocycles as BET protein inhibitors |
RU2695664C1 (ru) * | 2013-12-09 | 2019-07-25 | Юсб Байофарма Спрл | Производные имидазопиридина в качестве модуляторов активности tnf |
WO2015105749A1 (en) * | 2014-01-07 | 2015-07-16 | Bristol-Myers Squibb Company | Sulfone amide linked benzothiazole inhibitors of endothelial lipase |
AU2015209189A1 (en) * | 2014-01-24 | 2016-07-28 | Confluence Life Sciences, Inc. | Substituted pyroolopyridines and pyrrolopyrazines for treating cancer or inflammatory diseases |
MX2016013851A (es) * | 2014-04-23 | 2017-07-14 | Incyte Corp | 1h-pirrolo[2,3-c]piridin-7(6h)-onas y pirazolo[3,4-c]piridin-7(6h) -onas como inhibidores de proteinas de bromodominio y extra terminal (bet). |
MA40943A (fr) * | 2014-11-10 | 2017-09-19 | Constellation Pharmaceuticals Inc | Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines |
MA40940A (fr) | 2014-11-10 | 2017-09-19 | Constellation Pharmaceuticals Inc | Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines |
WO2016086200A1 (en) * | 2014-11-27 | 2016-06-02 | Genentech, Inc. | 4,5,6,7-tetrahydro-1 h-pyrazolo[4,3-c]pyridin-3-amine compounds as cbp and/or ep300 inhibitors |
JP6857606B2 (ja) * | 2015-03-05 | 2021-04-14 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ブロモドメインbrd9の阻害剤としての新規ピリジノンおよびイソキノリノン |
AR104259A1 (es) * | 2015-04-15 | 2017-07-05 | Celgene Quanticel Res Inc | Inhibidores de bromodominio |
TW201642860A (zh) * | 2015-04-22 | 2016-12-16 | 塞爾基因定量細胞研究公司 | 布羅莫結構域抑制劑 |
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CL2017002606A1 (es) | 2018-05-18 |
EP3283077B1 (en) | 2021-03-10 |
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SG11201708470SA (en) | 2017-11-29 |
US20180134710A1 (en) | 2018-05-17 |
MX2017013207A (es) | 2018-02-19 |
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CA2982588A1 (en) | 2016-10-20 |
JP2018511626A (ja) | 2018-04-26 |
EA201792229A1 (ru) | 2018-05-31 |
TW201643153A (zh) | 2016-12-16 |
EP3831383A1 (en) | 2021-06-09 |
AU2016249273B2 (en) | 2020-07-09 |
CN107635558A (zh) | 2018-01-26 |
US10494371B2 (en) | 2019-12-03 |
US20200071332A1 (en) | 2020-03-05 |
EP3283077A4 (en) | 2019-01-23 |
AU2016249273A1 (en) | 2017-11-09 |
WO2016168682A3 (en) | 2016-12-08 |
ES2868355T3 (es) | 2021-10-21 |
PH12017501888A1 (en) | 2018-03-05 |
HK1243326A1 (zh) | 2018-07-13 |
US10807982B2 (en) | 2020-10-20 |
CO2017011484A2 (es) | 2018-01-31 |
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