TW202216711A - 治療自體免疫疾病的氫異喹啉或氫㖠啶化合物 - Google Patents
治療自體免疫疾病的氫異喹啉或氫㖠啶化合物 Download PDFInfo
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- TW202216711A TW202216711A TW110125634A TW110125634A TW202216711A TW 202216711 A TW202216711 A TW 202216711A TW 110125634 A TW110125634 A TW 110125634A TW 110125634 A TW110125634 A TW 110125634A TW 202216711 A TW202216711 A TW 202216711A
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- Prior art keywords
- methyl
- pyridin
- dihydro
- alkyl
- piperazin
- Prior art date
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- 150000001875 compounds Chemical class 0.000 title claims abstract description 279
- 238000011282 treatment Methods 0.000 title claims description 15
- 208000023275 Autoimmune disease Diseases 0.000 title description 4
- 150000004800 hydroisoquinoline derivatives Chemical class 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims abstract description 57
- 238000000034 method Methods 0.000 claims abstract description 22
- -1 methanoyl piperazinyl Chemical group 0.000 claims description 272
- 125000000217 alkyl group Chemical group 0.000 claims description 152
- 238000002360 preparation method Methods 0.000 claims description 93
- 125000003545 alkoxy group Chemical group 0.000 claims description 61
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims description 36
- JUJWROOIHBZHMG-UHFFFAOYSA-N pyridine Substances C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 33
- 101000669402 Homo sapiens Toll-like receptor 7 Proteins 0.000 claims description 32
- 102000008235 Toll-Like Receptor 9 Human genes 0.000 claims description 31
- 108010060818 Toll-Like Receptor 9 Proteins 0.000 claims description 31
- 102100039390 Toll-like receptor 7 Human genes 0.000 claims description 30
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 30
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- 101000800483 Homo sapiens Toll-like receptor 8 Proteins 0.000 claims description 28
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- 229910052799 carbon Inorganic materials 0.000 claims description 27
- 102100033110 Toll-like receptor 8 Human genes 0.000 claims description 26
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims description 25
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims description 25
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims description 24
- 125000004193 piperazinyl group Chemical group 0.000 claims description 22
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- 125000001424 substituent group Chemical group 0.000 claims description 18
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- BCIIMDOZSUCSEN-UHFFFAOYSA-N piperidin-4-amine Chemical compound NC1CCNCC1 BCIIMDOZSUCSEN-UHFFFAOYSA-N 0.000 claims description 17
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- NGXSWUFDCSEIOO-UHFFFAOYSA-N pyrrolidin-3-amine Chemical compound NC1CCNC1 NGXSWUFDCSEIOO-UHFFFAOYSA-N 0.000 claims description 16
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 15
- 125000003386 piperidinyl group Chemical group 0.000 claims description 14
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- 150000002367 halogens Chemical class 0.000 claims description 13
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- 125000002347 octyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 5
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- HDOWRFHMPULYOA-UHFFFAOYSA-N piperidin-4-ol Chemical compound OC1CCNCC1 HDOWRFHMPULYOA-UHFFFAOYSA-N 0.000 claims description 3
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Classifications
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- 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
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- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| WOPCT/CN2020/101904 | 2020-07-14 | ||
| CN2020101904 | 2020-07-14 | ||
| WOPCT/CN2021/094138 | 2021-05-17 | ||
| CN2021094138 | 2021-05-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TW202216711A true TW202216711A (zh) | 2022-05-01 |
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Family Applications (1)
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|---|---|---|---|
| TW110125634A TW202216711A (zh) | 2020-07-14 | 2021-07-13 | 治療自體免疫疾病的氫異喹啉或氫㖠啶化合物 |
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|---|---|
| US (1) | US20240317735A1 (https=) |
| EP (1) | EP4182032A1 (https=) |
| JP (1) | JP2023533807A (https=) |
| CN (1) | CN115835910A (https=) |
| TW (1) | TW202216711A (https=) |
| WO (1) | WO2022013136A1 (https=) |
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| EP4196222A1 (en) * | 2020-08-14 | 2023-06-21 | Minerva Neurosciences, Inc. | Condensed azacycles as sigma ligand compounds and uses thereof |
| PE20250401A1 (es) * | 2021-09-24 | 2025-02-11 | Hoffmann La Roche | Compuestos de pirazolo[3,4-b]piridina para el tratamiento de enfermedades auto/inmunitarias |
| CN120230100B (zh) * | 2025-05-30 | 2025-09-05 | 中国药科大学 | 一种咪唑并[1,2-a]吡嗪或咪唑并[1,2-a]吡啶类化合物及其医药用途 |
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| JP2013032290A (ja) * | 2009-11-20 | 2013-02-14 | Dainippon Sumitomo Pharma Co Ltd | 新規縮合ピリミジン誘導体 |
| JP6306750B2 (ja) | 2014-03-07 | 2018-04-04 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | B型肝炎ウイルス感染症の治療および予防のための新規な6−縮合ヘテロアリールジヒドロピリミジン |
| HRP20220144T1 (hr) * | 2016-09-09 | 2022-04-15 | Novartis Ag | Spojevi i pripravci kao inhibitori endosomskih toll-u sličnih receptora |
| WO2018218197A2 (en) * | 2017-05-26 | 2018-11-29 | Board Of Regents, The University Of Texas System | Tetrahydropyrido[4,3-d]pyrimidine inhibitors of atr kinase |
| EP3728218B1 (en) * | 2017-12-20 | 2021-12-01 | Bristol-Myers Squibb Company | Amino indole compounds useful as tlr inhibitors |
| JP7407740B2 (ja) | 2018-05-18 | 2024-01-04 | ノバルティス アーゲー | Tlr7/tlr8阻害剤の結晶形態 |
| EP3802539B1 (en) | 2018-06-05 | 2023-09-20 | F. Hoffmann-La Roche AG | Tetrahydro-1h-pyrazino[2,1-a]isoindolylquinoline compounds for the treatment of autoimmune disease |
| MX2021012223A (es) * | 2019-04-09 | 2021-11-03 | Hoffmann La Roche | Compuestos de hexahidro-1h-pirazino[1,2-a]pirazina para el tratamiento de una enfermedad autoinmunitaria. |
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2021
- 2021-07-12 US US18/016,289 patent/US20240317735A1/en active Pending
- 2021-07-12 EP EP21748533.3A patent/EP4182032A1/en active Pending
- 2021-07-12 CN CN202180049160.3A patent/CN115835910A/zh active Pending
- 2021-07-12 JP JP2023502631A patent/JP2023533807A/ja not_active Ceased
- 2021-07-12 WO PCT/EP2021/069294 patent/WO2022013136A1/en not_active Ceased
- 2021-07-13 TW TW110125634A patent/TW202216711A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2023533807A (ja) | 2023-08-04 |
| WO2022013136A1 (en) | 2022-01-20 |
| US20240317735A1 (en) | 2024-09-26 |
| EP4182032A1 (en) | 2023-05-24 |
| CN115835910A (zh) | 2023-03-21 |
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