AR087919A1 - Heterociclos biciclicos como inhibidores de irak4 - Google Patents
Heterociclos biciclicos como inhibidores de irak4Info
- Publication number
- AR087919A1 AR087919A1 ARP120103448A ARP120103448A AR087919A1 AR 087919 A1 AR087919 A1 AR 087919A1 AR P120103448 A ARP120103448 A AR P120103448A AR P120103448 A ARP120103448 A AR P120103448A AR 087919 A1 AR087919 A1 AR 087919A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- alkyl
- independently selected
- occurrence
- hydrogen
- Prior art date
Links
- 101000977771 Homo sapiens Interleukin-1 receptor-associated kinase 4 Proteins 0.000 title 1
- 102100023533 Interleukin-1 receptor-associated kinase 4 Human genes 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000001072 heteroaryl group Chemical group 0.000 abstract 5
- 150000002431 hydrogen Chemical class 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000001475 halogen functional group Chemical group 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000001188 haloalkyl group Chemical group 0.000 abstract 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 2
- -1 stereoisomers Substances 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 2
- 125000003107 substituted aryl group Chemical group 0.000 abstract 2
- 101100440695 Dictyostelium discoideum corB gene Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 239000003085 diluting agent Substances 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 229940043355 kinase inhibitor Drugs 0.000 abstract 1
- 239000002207 metabolite Substances 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Formulaciones farmacéuticas que comprenden al menos uno de los compuestos inhibidores de quinasa de fórmula (1) junto con un vehículo, diluyente o excipiente aceptable desde el punto de vista farmacéutico. Reivindicación 1: Un compuesto de fórmula (1) y sus derivados, profármacos, N-óxidos, estereoisómeros, solvatos, sales aceptables desde el punto de vista farmacéutico y metabolitos biológicamente activos de los mismos; caracterizado porque, X se selecciona de O, S, y NH; A se selecciona de arilo o heteroarilo; R en cada aparición se selecciona independientemente de hidrógeno, ciano, halo, hidroxi, -NO₂, -NR³R⁴, alquilo opcionalmente sustituido, arilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido o heteroarilo opcionalmente sustituido; donde el sustituyente opcional, en cada aparición, se selecciona independientemente de halo, alquilo, haloalquilo, ciano, -NR⁵R⁶ o -COOR⁷; R¹ en cada aparición se selecciona independientemente de hidrógeno, halógeno, alquilo, arilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo, Y-arilalquilo o Y-cicloalquilo; donde cicloalquilo, arilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo y arilalquilo pueden ser sustituidos opcionalmente con hidroxi, alquilo, haloalquilo, ciano o halo; Y se selecciona de enlace directo, O, -C(O)- o NR⁷; R² en cada ocurrencia se seleccione independientemente de hidrógeno, carboxi, ciano, hidroxi, hidroxialquilo, alquilo, arilo, heteroarilo, -SO₂R⁵ u oxo; R³ y R⁴ se seleccionan independientemente de hidrógeno, hidroxialquilo, aminoalquilo, alquilo opcionalmente sustituido, heterociclilo opcionalmente sustituido, arilo opcionalmente sustituido; donde el sustituyente opcional, en cada aparición, se selecciona independientemente de halo, haloalquilo o -COOR⁷; R⁵ y R⁶ se seleccionan independientemente de hidrógeno, alquilo, COR⁷ o -COOR⁷; R⁷ en cada aparición se selecciona independientemente de hidrógeno o alquilo; y m, n y p se seleccionan de 1, 2 ó 3.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN3206CH2011 | 2011-09-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR087919A1 true AR087919A1 (es) | 2014-04-23 |
Family
ID=47178257
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120103448A AR087919A1 (es) | 2011-09-19 | 2012-09-19 | Heterociclos biciclicos como inhibidores de irak4 |
Country Status (2)
| Country | Link |
|---|---|
| AR (1) | AR087919A1 (es) |
| WO (1) | WO2013042137A1 (es) |
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| WO2014180908A1 (en) * | 2013-05-08 | 2014-11-13 | Deutsches Krebsforschungszentrum | Acip/peptide-based inhibition of cancer cachexia |
| EP2999470B1 (en) | 2013-05-22 | 2017-08-16 | Children's Hospital Medical Center | Combination therapy for mds |
| GB201311888D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| TWI667233B (zh) * | 2013-12-19 | 2019-08-01 | 德商拜耳製藥公司 | 新穎吲唑羧醯胺，其製備方法、含彼等之醫藥製劑及其製造醫藥之用途 |
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| MA46191A (fr) | 2016-09-09 | 2021-04-21 | Incyte Corp | Dérivés de pyrazolopyridine comme modulateurs de hpk1 et leurs utilisations pour le traitement du cancer |
| TW201811799A (zh) | 2016-09-09 | 2018-04-01 | 美商英塞特公司 | 吡唑并嘧啶化合物及其用途 |
| US20180072718A1 (en) | 2016-09-09 | 2018-03-15 | Incyte Corporation | Pyrazolopyridine compounds and uses thereof |
| WO2018060072A1 (de) | 2016-09-29 | 2018-04-05 | Bayer Pharma Aktiengesellschaft | Neue substituierte benzimidazole, verfahren zu ihrer herstellung, pharmazeutische präparate die diese enthalten, sowie deren verwendung zur herstellung von arzneimitteln |
| WO2018060174A1 (de) | 2016-09-29 | 2018-04-05 | Bayer Pharma Aktiengesellschaft | Substituierte benzimidazole, pharmazeutische präparate diese enthaltend, sowie deren verwendung zur herstellung von arzneimitteln |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| US11547696B2 (en) | 2016-10-28 | 2023-01-10 | Children's Hospital Medical Center | Methods and compositions for treatment of myelodysplastic syndromes and/or acute myeloid leukemias |
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| TWI876442B (zh) | 2017-10-10 | 2025-03-11 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| KR102697663B1 (ko) | 2017-10-31 | 2024-08-21 | 쿠리스 인코퍼레이션 | 혈액학적 장애를 치료하기 위한 화합물 및 조성물 |
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| WO2020150626A1 (en) * | 2019-01-18 | 2020-07-23 | Biogen Ma Inc. | Imidazo[1,2-a]pyridinyl derivatives as irak4 inhibitors |
| CR20220097A (es) | 2019-08-06 | 2022-06-01 | Incyte Corp | Formas sólidas de un inhibidor de hpk1 |
| EP4076520A4 (en) | 2019-12-17 | 2024-03-27 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| US11591332B2 (en) | 2019-12-17 | 2023-02-28 | Kymera Therapeutics, Inc. | IRAK degraders and uses thereof |
| US20230107927A1 (en) | 2020-02-28 | 2023-04-06 | First Wave Bio, Inc. | Methods of treating iatrogenic autoimmune colitis |
| TW202210483A (zh) | 2020-06-03 | 2022-03-16 | 美商凱麥拉醫療公司 | Irak降解劑之結晶型 |
| US20230295146A1 (en) * | 2020-07-24 | 2023-09-21 | The University Of Rochester | Inhibitors of interleukin-1 receptor-associated kinases 1 and 4 |
| JP7422242B2 (ja) | 2020-09-30 | 2024-01-25 | 旭化成ファーマ株式会社 | マクロサイクル化合物 |
| JP7433463B2 (ja) | 2020-09-30 | 2024-02-19 | 旭化成ファーマ株式会社 | ピリミジン含有含窒素二環化合物 |
| TW202241891A (zh) | 2020-12-30 | 2022-11-01 | 美商凱麥拉醫療公司 | Irak降解劑及其用途 |
| CA3207049A1 (en) | 2021-02-15 | 2022-08-18 | Jared Gollob | Irak4 degraders and uses thereof |
| KR20240004476A (ko) | 2021-04-08 | 2024-01-11 | 쿠리스 인코퍼레이션 | 암 치료를 위한 병용 요법 |
| JP2024519215A (ja) | 2021-05-07 | 2024-05-09 | カイメラ セラピューティクス， インコーポレイテッド | Ｃｄｋ２分解剤およびそれらの使用 |
| TW202334165A (zh) | 2021-10-29 | 2023-09-01 | 美商凱麥拉醫療公司 | Irak4降解劑及其製備 |
| WO2023088435A1 (zh) * | 2021-11-19 | 2023-05-25 | 成都奥睿药业有限公司 | 三取代吡啶衍生物的制备及作为芳香烃受体调节物的应用 |
| IL314437A (en) | 2022-01-31 | 2024-09-01 | Kymera Therapeutics Inc | IRAK joints and their uses |
| JP2025513716A (ja) | 2022-03-23 | 2025-04-30 | ライジェル・ファーマシューティカルズ・インコーポレイテッド | Ｉｒａｋ阻害剤としてのピリミド－２－イル－ピラゾール化合物 |
| WO2024011116A2 (en) * | 2022-07-07 | 2024-01-11 | Dana-Farber Cancer Institute, Inc. | Potent and selective irreversible inhibitors of irak1 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE391505T1 (de) * | 2001-11-27 | 2008-04-15 | Hoffmann La Roche | Benzothiazole derivative |
| EP1628661A2 (en) * | 2003-06-05 | 2006-03-01 | Vertex Pharmaceuticals Incorporated | Modulators of vr1 receptor |
| WO2006080821A1 (en) * | 2005-01-28 | 2006-08-03 | Daewoong Pharmaceutical Co., Ltd. | Novel benzoimidazole derivatives and pharmaceutical composition comprising the same |
-
2012
- 2012-09-14 WO PCT/IN2012/000615 patent/WO2013042137A1/en not_active Ceased
- 2012-09-19 AR ARP120103448A patent/AR087919A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| WO2013042137A1 (en) | 2013-03-28 |
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