BR112021003529A2 - derivados de tetra-hidropiridopirimidina como moduladores de ahr - Google Patents
derivados de tetra-hidropiridopirimidina como moduladores de ahr Download PDFInfo
- Publication number
- BR112021003529A2 BR112021003529A2 BR112021003529-0A BR112021003529A BR112021003529A2 BR 112021003529 A2 BR112021003529 A2 BR 112021003529A2 BR 112021003529 A BR112021003529 A BR 112021003529A BR 112021003529 A2 BR112021003529 A2 BR 112021003529A2
- Authority
- BR
- Brazil
- Prior art keywords
- minutes
- indol
- alkyl
- ethyl
- pyrimidine
- Prior art date
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- FHLXQXCQSUICIN-UHFFFAOYSA-N 1,2,3,4-tetrahydropyrido[3,2-d]pyrimidine Chemical class C1=CC=C2NCNCC2=N1 FHLXQXCQSUICIN-UHFFFAOYSA-N 0.000 title abstract description 3
- 150000001875 compounds Chemical class 0.000 claims abstract description 121
- 238000011282 treatment Methods 0.000 claims abstract description 26
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 35
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 31
- 229910052801 chlorine Inorganic materials 0.000 claims description 22
- 150000003839 salts Chemical class 0.000 claims description 20
- 125000000217 alkyl group Chemical group 0.000 claims description 19
- 229910052731 fluorine Inorganic materials 0.000 claims description 19
- 229910052736 halogen Inorganic materials 0.000 claims description 19
- 150000002367 halogens Chemical class 0.000 claims description 19
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 15
- 125000005842 heteroatom Chemical group 0.000 claims description 14
- 229910052760 oxygen Inorganic materials 0.000 claims description 13
- 239000008194 pharmaceutical composition Substances 0.000 claims description 13
- 229910052717 sulfur Inorganic materials 0.000 claims description 13
- 125000004174 2-benzimidazolyl group Chemical group [H]N1C(*)=NC2=C([H])C([H])=C([H])C([H])=C12 0.000 claims description 6
- 125000001072 heteroaryl group Chemical group 0.000 claims description 6
- 125000000814 indol-3-yl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([H])=C([*])C2=C1[H] 0.000 claims description 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 6
- 125000001424 substituent group Chemical group 0.000 claims description 6
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims description 5
- 229910052739 hydrogen Inorganic materials 0.000 claims description 5
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 4
- 229910006074 SO2NH2 Inorganic materials 0.000 claims description 3
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims description 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 3
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- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 120
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 102
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Classifications
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- 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
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic 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
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
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| EP3721894A1 (en) | 2019-04-10 | 2020-10-14 | Deutsches Krebsforschungszentrum, Stiftung des öffentlichen Rechts | Interleukin-4-induced gene 1 (il4i1) as a biomarker and uses thereof |
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| WO2016154110A1 (en) * | 2015-03-20 | 2016-09-29 | Cleave Biosciences, Inc. | Companion diagnostic for p97 inhibitor therapy and methods of use thereof |
| AU2017269870A1 (en) | 2016-05-25 | 2018-12-06 | Bayer Pharma Aktiengesellschaft | 3-oxo-2,6-diphenyl-2,3-dihydropyridazine-4-carboxamides |
| JP2023515128A (ja) | 2020-02-26 | 2023-04-12 | ジャガー セラピューティクス ピーティーイーリミテッド | Ａｈｒシグナル伝達の調節に有用なピリドピリミジン誘導体 |
-
2019
- 2019-08-23 WO PCT/EP2019/072641 patent/WO2020039093A1/en not_active Ceased
- 2019-08-23 AU AU2019323714A patent/AU2019323714A1/en not_active Abandoned
- 2019-08-23 EP EP19769387.2A patent/EP3841102B1/en active Active
- 2019-08-23 US US17/270,626 patent/US12221439B2/en active Active
- 2019-08-23 BR BR112021003529-0A patent/BR112021003529A2/pt not_active Application Discontinuation
- 2019-08-23 MX MX2021002215A patent/MX2021002215A/es unknown
- 2019-08-23 SG SG11202101441SA patent/SG11202101441SA/en unknown
- 2019-08-23 KR KR1020217008532A patent/KR20210049135A/ko not_active Ceased
- 2019-08-23 CN CN201980060477.XA patent/CN112739698A/zh active Pending
- 2019-08-23 JP JP2021534826A patent/JP2021535213A/ja active Pending
- 2019-08-23 CA CA3110402A patent/CA3110402A1/en active Pending
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2021
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- 2021-02-22 IL IL281023A patent/IL281023A/en unknown
- 2021-02-24 PH PH12021550382A patent/PH12021550382A1/en unknown
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|---|---|
| ZA202100931B (en) | 2021-10-27 |
| US20210332041A1 (en) | 2021-10-28 |
| CA3110402A1 (en) | 2020-02-27 |
| KR20210049135A (ko) | 2021-05-04 |
| AU2019323714A1 (en) | 2021-03-25 |
| US12221439B2 (en) | 2025-02-11 |
| SG11202101441SA (en) | 2021-03-30 |
| JP2021535213A (ja) | 2021-12-16 |
| MX2021002215A (es) | 2021-07-15 |
| IL281023A (en) | 2021-04-29 |
| EP3841102A1 (en) | 2021-06-30 |
| WO2020039093A1 (en) | 2020-02-27 |
| EP3841102B1 (en) | 2022-09-14 |
| CN112739698A (zh) | 2021-04-30 |
| PH12021550382A1 (en) | 2021-12-13 |
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