AR094148A1 - Dihidropiridopirazinonas inhibidoras de la proteina bet - Google Patents
Dihidropiridopirazinonas inhibidoras de la proteina betInfo
- Publication number
- AR094148A1 AR094148A1 ARP130104872A ARP130104872A AR094148A1 AR 094148 A1 AR094148 A1 AR 094148A1 AR P130104872 A ARP130104872 A AR P130104872A AR P130104872 A ARP130104872 A AR P130104872A AR 094148 A1 AR094148 A1 AR 094148A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- cyano
- cycloalkyl
- substituents
- Prior art date
Links
- 230000002401 inhibitory effect Effects 0.000 title 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 10
- -1 oxazolin-2-yl Chemical group 0.000 abstract 10
- 125000001424 substituent group Chemical group 0.000 abstract 10
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 9
- 125000004043 oxo group Chemical group O=* 0.000 abstract 9
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 6
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 4
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 4
- CPPKAGUPTKIMNP-UHFFFAOYSA-N cyanogen fluoride Chemical compound FC#N CPPKAGUPTKIMNP-UHFFFAOYSA-N 0.000 abstract 4
- 229910052731 fluorine Inorganic materials 0.000 abstract 4
- 239000011737 fluorine Substances 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical group 0.000 abstract 4
- 125000004366 heterocycloalkenyl group Chemical group 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 abstract 2
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 2
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 abstract 2
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 abstract 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 229940121649 protein inhibitor Drugs 0.000 abstract 2
- 239000012268 protein inhibitor Substances 0.000 abstract 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 108091005625 BRD4 Proteins 0.000 abstract 1
- 102100029895 Bromodomain-containing protein 4 Human genes 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 208000036142 Viral infection Diseases 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 230000003143 atherosclerotic effect Effects 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 150000001602 bicycloalkyls Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 230000035558 fertility Effects 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 150000002431 hydrogen Chemical group 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000009385 viral infection Effects 0.000 abstract 1
Classifications
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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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/16—Masculine contraceptives
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/10—Spiro-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Communicable Diseases (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Psychiatry (AREA)
- Rheumatology (AREA)
- Virology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Peptides Or Proteins (AREA)
Abstract
La presente se refiere a dihidropiridopirazinonas inhibidoras de la proteína BET, especialmente inhibidoras de BRD4. Esta también se refiere al uso de inhibidores de la proteína BET en infecciones virales, en trastornos neurodegenerativos, en enfermedades inflamatorias, en trastornos ateroscleróticos y en el control de la fertilidad masculina. Reivindicación 1: Compuestos de fórmula general (1) en la que A representa -NH- o -O-; X representa -N-; n representa 0 ó 1; R¹ representa -C(=O)NR⁸R⁹ o representa -S(=O)₂NR⁸R⁹, o representa oxazolin-2-ilo que puede estar opcionalmente mono- o disustituido con sustituyentes alquilo C₁₋₃ iguales o diferentes; R² representa hidrógeno, halógeno, ciano, alquilo C₁₋₄, alquenilo C₂₋₄, alquinilo C₂₋₄, halo-alquil C₁₋₄-, alcoxi C₁₋₄-, alcoxi C₁₋₄-alquil C₁₋₄-, halo-alcoxi C₁₋₄-, alquiltio C₁₋₄-, halo-alquiltio C₁₋₄- o -NR¹⁰R¹¹; R³ representa halógeno, alquilo C₁₋₃, alcoxi C₁₋₃-, alcoxi C₁₋₄-alquil C₁₋₄-, trifluorometil- o ciano y puede estar unido a cualquiera de las posiciones que aún no están ocupadas en el sistema aromático; R⁴ representa metilo o etilo; R⁵ representa hidrógeno o alquilo C₁₋₃; R⁶ representa hidrógeno o alquilo C₁₋₃; o R⁵ y R⁶ juntos representan alquileno C₂₋₅; R⁷ representa alquilo C₁₋₆, cicloalquilo C₃₋₈, heterocicloalquilo de 4 a 8 miembros, fenilo o fenil-alquilo C₁₋₃, en el que el alquilo C₁₋₆ puede estar opcionalmente mono-, di- o trisustituido con sustituyentes iguales o diferentes del grupo que consiste en flúor, oxo, ciano, hidroxi, alcoxi C₁₋₃- y -NR¹⁰R¹¹, y en el que el radical fenilo puede estar, en cada caso, opcionalmente mono-, di- o trisustituido con sustituyentes iguales o diferentes del grupo que consiste en halógeno, ciano, alquilo C₁₋₄, alquenilo C₂₋₄, alquinilo C₂₋₄, alcoxi C₁₋₄-, halo-alquil C₁₋₄- y halo-alcoxi C₁₋₄-, y en el que el heterocicloalquilo de 4 a 8 miembros puede estar opcionalmente mono- o disustituido con sustituyentes iguales o diferentes del grupo que consiste en oxo, flúor, ciano, alquilo C₁₋₄, alcoxi C₁₋₄-, alquilcarbonil C₁₋₄- y alcoxicarbonil C₁₋₄-; R⁸ representa alquilo C₁₋₆ que puede estar opcionalmente mono-, di- o trisustituido con sustituyentes iguales o diferentes del grupo que consiste en hidroxi, oxo, flúor, ciano, alcoxi C₁₋₄-, halo-alcoxi C₁₋₄-, -NR¹⁰R¹¹, cicloalquilo C₃₋₈, cicloalquenilo C₄₋₈, heterocicloalquilo de 4 a 8 miembros, heterocicloalquenilo de 4 a 8 miembros, espirocicloalquilo C₅₋₁₁, heteroespirocicloalquilo C₅₋₁₁, cicloalquilo C₆₋₁₂ puenteado, heterocicloalquilo C₆₋₁₂ puenteado, bicicloalquilo C₆₋₁₂, heterobicicloalquilo C₆₋₁₂, fenilo o heteroarilo de 5 a 6 miembros, en el que el cicloalquilo C₃₋₈, cicloalquenilo C₄₋₈, heterocicloalquilo de 4 a 8 miembros, heterocicloalquenilo de 4 a 8 miembros, espirocicloalquilo C₅₋₁₁, heteroespirocicloalquilo C₅₋₁₁, cicloalquilo C₆₋₁₂ puenteado, heterocicloalquilo C₆₋₁₂ puenteado, bicicloalquilo C₆₋₁₂, heterobicicloalquilo C₆₋₁₂ pueden estar, en cada caso, opcionalmente monosustituidos con oxo, alquilo C₁₋₄ o alcoxicarbonil C₁₋₄-, y en el que el fenilo y el heteroarilo de 5 a 6 miembros pueden estar opcionalmente mono- o disustituidos con sustituyentes iguales o diferentes del grupo que consiste en halógeno, ciano, trifluorometil-, alquilo C₁₋₃ y alcoxi C₁₋₃-, o representa alquenilo C₃₋₆ o alquinilo C₃₋₆, o representa cicloalquilo C₃₋₈, cicloalquenilo C₄₋₈, espirocicloalquil C₅₋₁₁-, cicloalquil C₆₋₁₂ puenteado- o bicicloalquil C₆₋₁₂- que pueden estar opcionalmente mono o disustituidos con sustituyentes iguales o diferentes del grupo que consiste en hidroxi, oxo, ciano, flúor, alquil C₁₋₃-, alcoxi C₁₋₃-, trifluorometil-, -NR¹⁰R¹¹ y heterocicloalquilo de 4 a 8 miembros, o representa heterocicloalquilo de 4 a 8 miembros, heterocicloalquenilo de 4 a 8 miembros, heteroespirocicloalquilo C₅₋₁₁, heterocicloalquilo C₆₋₁₂ puenteado o heterobicicloalquilo C₆₋₁₂ que pueden estar opcionalmente mono- o disustituidos con sustituyentes iguales o diferentes del grupo que consiste en hidroxi, oxo, ciano, flúor, alquilo C₁₋₃, alcoxi C₁₋₃-, trifluorometil-, -NR¹⁰R¹¹, alquilcarbonil C₁₋₄- y alcoxicarbonil C₁₋₄-, o representa hidrógeno; R⁹ representa hidrógeno o alquilo C₁₋₃; o R⁸ y R⁹ junto con el átomo de nitrógeno al que están unidos representan heterocicloalquilo de 4 a 8 miembros, heterocicloalquenilo de 4 a 8 miembros, heteroespirocicloalquilo C₅₋₁₁, heterocicloalquilo C₆₋₁₂ puenteado o heterobicicloalquilo C₆₋₁₂ que pueden estar opcionalmente mono- o disustituidos con sustituyentes iguales o diferentes del grupo que consiste en hidroxi, oxo, ciano, flúor, alquilo C₁₋₃, cicloalquilo C₃₋₆, alcoxi C₁₋₃-, trifluorometil-, -NR¹⁰R¹¹, alquilcarbonil C₁₋₄- o alcoxicarbonil C₁₋₄-; R¹⁰ y R¹¹ independientemente entre sí representan hidrógeno o representan alquilo C₁₋₆ que está opcionalmente mono-, di- o trisustituido con sustituyentes iguales o diferentes del grupo que consiste en hidroxi, oxo y flúor, o representan alquilcarbonil C₁₋₄- o alcoxicarbonil C₁₋₄-, o R¹⁰ y R¹¹ junto con el átomo de nitrógeno al que están unidos representan heterocicloalquilo de 4 a 8 miembros que puede estar opcionalmente mono- o disustituido con sustituyentes iguales o diferentes del grupo que consiste en hidroxi, oxo, ciano, flúor, alquilo C₁₋₃, halo-alquil C₁₋₄-, cicloalquil C₃₋₆-, cicloalquil C₃₋₆-alquil C₁₋₃-, bencilo o alcoxicarbonil C₁₋₄-; y los diastereómeros, racematos, polimorfos y sales fisiológicamente aceptables de los mismos.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12198623 | 2012-12-20 | ||
| EP13182252 | 2013-08-29 | ||
| EP13191933 | 2013-11-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR094148A1 true AR094148A1 (es) | 2015-07-15 |
Family
ID=49779903
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130104872A AR094148A1 (es) | 2012-12-20 | 2013-12-19 | Dihidropiridopirazinonas inhibidoras de la proteina bet |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20160193206A1 (es) |
| EP (1) | EP2935260A1 (es) |
| JP (1) | JP2016504990A (es) |
| CN (1) | CN105229002A (es) |
| AR (1) | AR094148A1 (es) |
| CA (1) | CA2895404A1 (es) |
| HK (1) | HK1213899A1 (es) |
| TW (1) | TW201427981A (es) |
| UY (1) | UY35205A (es) |
| WO (1) | WO2014095774A1 (es) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2935260A1 (de) * | 2012-12-20 | 2015-10-28 | Bayer Pharma Aktiengesellschaft | Bet-proteininhibitorische dihydropyridopyrazinone |
| MX366703B (es) | 2013-03-15 | 2019-07-22 | Incyte Holdings Corp | Heterociclos tricíclicos como inhibidores de la proteína bet. |
| EP3019502B1 (en) | 2013-07-08 | 2017-05-17 | Incyte Holdings Corporation | Tricyclic heterocycles as bet protein inhibitors |
| JP2016523941A (ja) * | 2013-07-09 | 2016-08-12 | バイエル ファーマ アクチエンゲゼルシャフト | 改変されたｂｅｔタンパク質阻害性ジヒドロキノキサリノンおよびジヒドロピリドピラジノン |
| CA2918910A1 (en) | 2013-07-25 | 2015-01-29 | Dana-Farber Cancer Institute, Inc. | Inhibitors of transcription factors and uses thereof |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| US9399640B2 (en) | 2013-11-26 | 2016-07-26 | Incyte Corporation | Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors |
| WO2015095492A1 (en) | 2013-12-19 | 2015-06-25 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| US10793571B2 (en) | 2014-01-31 | 2020-10-06 | Dana-Farber Cancer Institute, Inc. | Uses of diazepane derivatives |
| CA2936871A1 (en) * | 2014-01-31 | 2015-08-06 | Dana-Farber Cancer Institute, Inc. | Dihydropteridinone derivatives and uses thereof |
| CN106029653A (zh) | 2014-01-31 | 2016-10-12 | 达纳-法伯癌症研究所股份有限公司 | 二氨基嘧啶苯砜衍生物及其用途 |
| KR102702503B1 (ko) | 2014-04-23 | 2024-09-05 | 인사이트 홀딩스 코포레이션 | BET 단백질의 저해제로서의 1H-피롤로[2,3-c]피리딘-7(6H)-온 및 피라졸로[3,4-c]피리딘-7(6H)-온 |
| CN106573931A (zh) * | 2014-06-18 | 2017-04-19 | 拜耳医药股份有限公司 | 抑制BET蛋白的具有间位取代的芳族氨基或醚基的3，4‑二氢吡啶并[2，3‑b]吡嗪酮 |
| WO2015193217A1 (de) * | 2014-06-18 | 2015-12-23 | Bayer Pharma Aktiengesellschaft | Bet-proteininhibitorische dihydropyrido[2,3-b]pyrazinon-derivate mit para-substituierter aromatischer amino- oder ethergruppe |
| MY187540A (en) | 2014-08-01 | 2021-09-28 | Nuevolution As | Compounds active towards bromodomains |
| MX2017001757A (es) * | 2014-08-08 | 2017-05-30 | Dana Farber Cancer Inst Inc | Derivados de dihidropteridinona y sus usos. |
| MX2017001756A (es) | 2014-08-08 | 2017-05-30 | Dana Farber Cancer Inst Inc | Derivados de diazepano y sus usos. |
| WO2016044130A1 (en) | 2014-09-15 | 2016-03-24 | Incyte Corporation | Tricyclic heterocycles for use as bet protein inhibitors |
| CA3000633C (en) | 2014-10-14 | 2023-10-03 | The Regents Of The University Of California | Use of cdk9 and brd4 inhibitors to inhibit inflammation |
| GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
| US10702527B2 (en) | 2015-06-12 | 2020-07-07 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| AU2016305513A1 (en) | 2015-08-11 | 2018-03-08 | Neomed Institute | Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals |
| WO2017024406A1 (en) * | 2015-08-11 | 2017-02-16 | Neomed Institute | N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals |
| JP6912039B2 (ja) | 2015-08-12 | 2021-07-28 | ネオメド インスティテュートＮｅｏｍｅｄ Ｉｎｓｔｉｔｕｔｅ | 置換ベンゾイミダゾール、それらの調製及び医薬品としてのそれらの使用 |
| HK1256417A1 (zh) | 2015-09-11 | 2019-09-20 | 达纳-法伯癌症研究所股份有限公司 | 氰基噻吩並三唑並二氮雜環庚三烯及其用途 |
| CR20180199A (es) | 2015-09-11 | 2018-05-25 | Dana Farber Cancer Inst Inc | Acetamida tienotriazolodiazepinas y usos de las mismas |
| US10501459B2 (en) | 2015-10-21 | 2019-12-10 | Neomed Institute | Substituted imidazo[1,2-a]pyridines as bromodomain inhibitors |
| US20170121347A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| RU2742035C2 (ru) | 2015-11-25 | 2021-02-01 | Дана-Фарбер Кэнсер Инститьют, Инк. | Бивалентные ингибиторы бромодоменов и пути их применения |
| 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 |
| DE102017005091A1 (de) | 2016-05-30 | 2017-11-30 | Bayer Pharma Aktiengesellschaft | Substituierte 3,4-Dihydropyrido[2,3-b]pyrazin-2(1H)-one |
| PH12021551886A1 (en) | 2016-06-20 | 2023-07-17 | Incyte Corp | Crystalline solid forms of a bet inhibitor |
| CN109350616B (zh) * | 2018-12-18 | 2020-04-21 | 南华大学 | I-brd9或其衍生物在制备抗癫痫药物中的应用 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| CN113717080A (zh) * | 2021-10-09 | 2021-11-30 | 西安瑞联新材料股份有限公司 | 一种4-氯-2-氰基苯磺酰氯的合成方法 |
| AU2023255396A1 (en) | 2022-04-19 | 2024-10-24 | Nuevolution A/S | Compounds active towards bromodomains |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19506742A1 (de) * | 1995-02-27 | 1996-08-29 | Bayer Ag | Verwendung von Chinoxalinen in Kombination mit Protease-Inhibitoren als Arzneimittel zur Behandlung von AIDS und/oder HIV-Infektionen |
| US7351709B2 (en) * | 2004-06-09 | 2008-04-01 | Wyeth | Estrogen receptor ligands |
| CN105693730A (zh) * | 2006-10-19 | 2016-06-22 | 西格诺药品有限公司 | 杂芳基化合物、其组合物以及它们作为蛋白激酶抑制剂的用途 |
| JP2012197231A (ja) * | 2009-08-06 | 2012-10-18 | Oncotherapy Science Ltd | Ｔｔｋ阻害作用を有するピリジンおよびピリミジン誘導体 |
| JP5913292B2 (ja) * | 2010-05-14 | 2016-04-27 | ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド | 代謝を調節する組成物および方法 |
| EP2935260A1 (de) * | 2012-12-20 | 2015-10-28 | Bayer Pharma Aktiengesellschaft | Bet-proteininhibitorische dihydropyridopyrazinone |
-
2013
- 2013-12-17 EP EP13807998.3A patent/EP2935260A1/de not_active Withdrawn
- 2013-12-17 WO PCT/EP2013/076784 patent/WO2014095774A1/de not_active Ceased
- 2013-12-17 US US14/654,572 patent/US20160193206A1/en not_active Abandoned
- 2013-12-17 JP JP2015548421A patent/JP2016504990A/ja not_active Ceased
- 2013-12-17 CA CA2895404A patent/CA2895404A1/en not_active Abandoned
- 2013-12-17 HK HK16101861.6A patent/HK1213899A1/zh unknown
- 2013-12-17 CN CN201380073359.5A patent/CN105229002A/zh active Pending
- 2013-12-19 AR ARP130104872A patent/AR094148A1/es unknown
- 2013-12-19 TW TW102147272A patent/TW201427981A/zh unknown
- 2013-12-19 UY UY0001035205A patent/UY35205A/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| CA2895404A1 (en) | 2014-06-26 |
| UY35205A (es) | 2014-07-31 |
| EP2935260A1 (de) | 2015-10-28 |
| JP2016504990A (ja) | 2016-02-18 |
| CN105229002A (zh) | 2016-01-06 |
| HK1213899A1 (zh) | 2016-07-15 |
| WO2014095774A1 (de) | 2014-06-26 |
| TW201427981A (zh) | 2014-07-16 |
| US20160193206A1 (en) | 2016-07-07 |
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