WO2011114148A1 - Dérivés de 4h-[1,2,4]triazolo[5,1-b]pyrimidin-7-one à titre d'antagonistes des récepteurs ccr2b - Google Patents
Dérivés de 4h-[1,2,4]triazolo[5,1-b]pyrimidin-7-one à titre d'antagonistes des récepteurs ccr2b Download PDFInfo
- Publication number
- WO2011114148A1 WO2011114148A1 PCT/GB2011/050515 GB2011050515W WO2011114148A1 WO 2011114148 A1 WO2011114148 A1 WO 2011114148A1 GB 2011050515 W GB2011050515 W GB 2011050515W WO 2011114148 A1 WO2011114148 A1 WO 2011114148A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- methyl
- triazolo
- pyrimidin
- amino
- chlorophenyl
- Prior art date
Links
- 0 C*(C)(C1=*C(*)=**11)C(*)=C(*)C1=O Chemical compound C*(C)(C1=*C(*)=**11)C(*)=C(*)C1=O 0.000 description 2
- KKXHIHNJSLKPTQ-UHFFFAOYSA-N CC(Nc1nc(N)n[n]11)=C(Cc(cc2Cl)ccc2Cl)C1=O Chemical compound CC(Nc1nc(N)n[n]11)=C(Cc(cc2Cl)ccc2Cl)C1=O KKXHIHNJSLKPTQ-UHFFFAOYSA-N 0.000 description 1
- QZXNNFXAOXSUAR-UHFFFAOYSA-N CC(Nc1nc(N)n[n]11)=C(Cc2cc(Br)ccc2)C1=O Chemical compound CC(Nc1nc(N)n[n]11)=C(Cc2cc(Br)ccc2)C1=O QZXNNFXAOXSUAR-UHFFFAOYSA-N 0.000 description 1
- NWADGPUZZCEWTP-UHFFFAOYSA-N CC(Nc1nc(N)n[n]11)=C(Cc2cc(C(F)(F)F)cc(F)c2)C1=O Chemical compound CC(Nc1nc(N)n[n]11)=C(Cc2cc(C(F)(F)F)cc(F)c2)C1=O NWADGPUZZCEWTP-UHFFFAOYSA-N 0.000 description 1
- YFJUOPJXTZDDOM-UHFFFAOYSA-N CC(Nc1nc(N)n[n]11)=C(Cc2cc(OC)ccc2)C1=O Chemical compound CC(Nc1nc(N)n[n]11)=C(Cc2cc(OC)ccc2)C1=O YFJUOPJXTZDDOM-UHFFFAOYSA-N 0.000 description 1
- MYLKWPCNOLLYCH-UHFFFAOYSA-N CC(Nc1ncn[n]1C1=O)=C1Oc1cccc(Cl)c1 Chemical compound CC(Nc1ncn[n]1C1=O)=C1Oc1cccc(Cl)c1 MYLKWPCNOLLYCH-UHFFFAOYSA-N 0.000 description 1
- XZXWUTWMPLYWHJ-UHFFFAOYSA-N CCC(Nc1nc(N)n[n]11)=C(Cc2cc(Cl)ccc2)C1=O Chemical compound CCC(Nc1nc(N)n[n]11)=C(Cc2cc(Cl)ccc2)C1=O XZXWUTWMPLYWHJ-UHFFFAOYSA-N 0.000 description 1
- ZJECUUTUFAPBBT-UHFFFAOYSA-N CCOC(C(Cc1cccc(N)c1)C(C1CC1)=O)=O Chemical compound CCOC(C(Cc1cccc(N)c1)C(C1CC1)=O)=O ZJECUUTUFAPBBT-UHFFFAOYSA-N 0.000 description 1
- YPWCFTBQMGQMFN-UHFFFAOYSA-N COCCC(Nc1ncn[n]11)=C(Cc2cc(Cl)ccc2)C1=O Chemical compound COCCC(Nc1ncn[n]11)=C(Cc2cc(Cl)ccc2)C1=O YPWCFTBQMGQMFN-UHFFFAOYSA-N 0.000 description 1
- XYIYGIRFYWODOS-UHFFFAOYSA-N Cc(nc1NC(C2CCC2)=C2Cc(cc3C(F)(F)F)ccc3F)n[n]1C2=C Chemical compound Cc(nc1NC(C2CCC2)=C2Cc(cc3C(F)(F)F)ccc3F)n[n]1C2=C XYIYGIRFYWODOS-UHFFFAOYSA-N 0.000 description 1
- GAAAMBFVILNOPY-UHFFFAOYSA-N Clc1cccc(CBr)n1 Chemical compound Clc1cccc(CBr)n1 GAAAMBFVILNOPY-UHFFFAOYSA-N 0.000 description 1
- YLVBQGLIQXQGPH-UHFFFAOYSA-N Nc(nc1NC(C2CC2)=C2Cc3cc(Cl)ccc3)n[n]1C2=O Chemical compound Nc(nc1NC(C2CC2)=C2Cc3cc(Cl)ccc3)n[n]1C2=O YLVBQGLIQXQGPH-UHFFFAOYSA-N 0.000 description 1
- KQWVKOTUZVLZPY-UHFFFAOYSA-N O=C1[n]2ncnc2NC(C2CCC2)=C1Cc1cccc(F)c1 Chemical compound O=C1[n]2ncnc2NC(C2CCC2)=C1Cc1cccc(F)c1 KQWVKOTUZVLZPY-UHFFFAOYSA-N 0.000 description 1
- ZXPGYUNUEOEGHU-UHFFFAOYSA-N OCCC(Nc1ncn[n]11)=C(Cc(cc2C(F)(F)F)ccc2Cl)C1=O Chemical compound OCCC(Nc1ncn[n]11)=C(Cc(cc2C(F)(F)F)ccc2Cl)C1=O ZXPGYUNUEOEGHU-UHFFFAOYSA-N 0.000 description 1
- AVEYSPAUIFFBHG-UHFFFAOYSA-N OCCC(Nc1ncn[n]11)=C(Cc(cc2C(F)(F)F)ccc2F)C1=O Chemical compound OCCC(Nc1ncn[n]11)=C(Cc(cc2C(F)(F)F)ccc2F)C1=O AVEYSPAUIFFBHG-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
Abstract
Cette invention concerne de nouveaux composés destinés à être utilisés dans les compositions, des procédés pour leur préparation, des intermédiaires utiles dans leur préparation et leur utilisation à titre d'agents thérapeutiques. Cette invention concerne également des compositions pharmaceutiques, qui comprennent des composés qui agissent par antagonisme du récepteur CCR2b pour lequel MCP-1 est un des ligands connus et peuvent, par conséquent, être utilisés pour traiter la maladie inflammatoire, l'athérosclérose, le diabète, l'obésité, le cancer, la pneumopathie obstructive chronique (COPD), la polyarthrite rhumatoïde et/ou la douleur neuropathique, qui est médié(e) par ces récepteurs.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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US31481810P | 2010-03-17 | 2010-03-17 | |
US61/314,818 | 2010-03-17 |
Publications (1)
Publication Number | Publication Date |
---|---|
WO2011114148A1 true WO2011114148A1 (fr) | 2011-09-22 |
Family
ID=43943216
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/GB2011/050515 WO2011114148A1 (fr) | 2010-03-17 | 2011-03-16 | Dérivés de 4h-[1,2,4]triazolo[5,1-b]pyrimidin-7-one à titre d'antagonistes des récepteurs ccr2b |
Country Status (1)
Country | Link |
---|---|
WO (1) | WO2011114148A1 (fr) |
Cited By (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20120277224A1 (en) * | 2011-04-26 | 2012-11-01 | Bioenergenix | Heterocyclic compounds for the inhibition of pask |
JP2013538838A (ja) * | 2010-09-27 | 2013-10-17 | プロクシマゲン リミテッド | 7−ヒドロキシ−ピラゾロ[1,5−a]ピリミジン化合物およびccr2レセプターアンタゴニストとしてのその使用 |
WO2015036563A1 (fr) | 2013-09-16 | 2015-03-19 | Bayer Pharma Aktiengesellschaft | Trifluorométhylpyrimidones disubstituées et leur utilisation comme antagonistes du ccr2 |
WO2016113205A1 (fr) | 2015-01-13 | 2016-07-21 | Bayer Pharma Aktiengesellschaft | Pentafluoréthylpyrimidinones substituées et leur utilisation |
CN106749271A (zh) * | 2016-12-07 | 2017-05-31 | 青岛科技大学 | 一类[1,2,4]‑三氮唑并[1,5‑a]嘧啶酮类杂环化合物、其制备方法及其用途 |
WO2018071282A1 (fr) * | 2016-10-12 | 2018-04-19 | Merck Sharp & Dohme Corp. | Inhibiteurs de kdm5 |
WO2018071283A1 (fr) * | 2016-10-12 | 2018-04-19 | Merck Sharp & Dohme Corp. | Inhibiteurs de kdm5 |
US10392389B2 (en) | 2012-10-25 | 2019-08-27 | Bioenergenix Llc | Heterocyclic compounds for the inhibition of PASK |
US10781185B2 (en) | 2009-09-03 | 2020-09-22 | Bioenergenix Llc | Heterocyclic compounds for the inhibition of PASK |
JP2021512115A (ja) * | 2018-02-02 | 2021-05-13 | 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 | グレリンo−アシルトランスフェラーゼ(goat)阻害剤として使用するためのトリアゾロピリミジン誘導体 |
WO2021108408A1 (fr) * | 2019-11-25 | 2021-06-03 | Amgen Inc. | Composés hétérocycliques en tant qu'inhibiteurs de delta-5 désaturase et procédés d'utilisation |
JP2021523177A (ja) * | 2018-05-11 | 2021-09-02 | ディザル(ジァンスー)ファーマシューティカル・カンパニー・リミテッド | トリアゾロピリミジン化合物およびがんの処置におけるそれらの使用 |
CN113692306A (zh) * | 2019-04-03 | 2021-11-23 | 泰拉强石株式会社 | 基于胸腺嘧啶核酸碱基的三唑并嘧啶类及其制造方法 |
US11191765B2 (en) | 2012-10-25 | 2021-12-07 | Bioenergenix Llc | Heterocyclic compounds for the inhibition of PASK |
RU2808622C1 (ru) * | 2022-12-26 | 2023-11-30 | Федеральное государственное автономное образовательное учреждение высшего образования "Уральский федеральный университет имени первого Президента России Б.Н. Ельцина" | 3-Бензил-5-метил-6-(фенилтио)-[1,2,4]триазоло[1,5-a]пиримидин-7(3H)-он, обладающий противовирусной активностью в отношении коронавируса SARS-CoV2 |
US11976082B2 (en) | 2020-05-22 | 2024-05-07 | Boehringer Ingelheim International Gmbh | Continuous process for manufacturing alkyl 7-amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridine-carboxylate |
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WO1997030035A1 (fr) | 1996-02-13 | 1997-08-21 | Zeneca Limited | Derives de la quinazoline utilises comme inhibiteurs du vegf |
WO1997032856A1 (fr) | 1996-03-05 | 1997-09-12 | Zeneca Limited | Derives de 4-anilinoquinazoline |
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WO2000040529A1 (fr) | 1999-01-07 | 2000-07-13 | Angiogene Pharmaceuticals Ltd. | Derives de colchinol utilises comme agents de degradation vasculaire |
WO2000041669A2 (fr) | 1999-01-15 | 2000-07-20 | Angiogene Pharmaceuticals Ltd. | Agents de degradation vasculaire aux benzimidazoles |
WO2001092224A1 (fr) | 2000-05-31 | 2001-12-06 | Astrazeneca Ab | Derives d'indole possedant une activite endommageant les vaisseaux sanguins |
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WO2002008213A1 (fr) | 2000-07-07 | 2002-01-31 | Angiogene Pharmaceuticals Limited | Derives de colchinol utiles comme inhibiteurs de l'angiogenese |
WO2002069973A1 (fr) | 2001-03-02 | 2002-09-12 | Sepracor, Inc. | Ligand piperidine-piperazine pour recepteurs neurotransmetteurs |
WO2006067401A1 (fr) | 2004-12-24 | 2006-06-29 | Astrazeneca Ab | Composés hétérocycliques en tant qu'antagonistes de ccr2b |
WO2007134449A1 (fr) * | 2006-05-19 | 2007-11-29 | Waratah Pharmaceuticals Inc. | Procédés de criblage pour modulateurs de bêta-amyloïde |
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Cited By (28)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US10781185B2 (en) | 2009-09-03 | 2020-09-22 | Bioenergenix Llc | Heterocyclic compounds for the inhibition of PASK |
US11459307B2 (en) | 2009-09-03 | 2022-10-04 | Bioenergenix Llc | Heterocyclic compounds for the inhibition of PASK |
JP2013538838A (ja) * | 2010-09-27 | 2013-10-17 | プロクシマゲン リミテッド | 7−ヒドロキシ−ピラゾロ[1,5−a]ピリミジン化合物およびccr2レセプターアンタゴニストとしてのその使用 |
US20120277224A1 (en) * | 2011-04-26 | 2012-11-01 | Bioenergenix | Heterocyclic compounds for the inhibition of pask |
US10953012B2 (en) * | 2011-04-26 | 2021-03-23 | Bioenergenix Llc | Heterocyclic compounds for the inhibition of pask |
US11191765B2 (en) | 2012-10-25 | 2021-12-07 | Bioenergenix Llc | Heterocyclic compounds for the inhibition of PASK |
US10392389B2 (en) | 2012-10-25 | 2019-08-27 | Bioenergenix Llc | Heterocyclic compounds for the inhibition of PASK |
WO2015036563A1 (fr) | 2013-09-16 | 2015-03-19 | Bayer Pharma Aktiengesellschaft | Trifluorométhylpyrimidones disubstituées et leur utilisation comme antagonistes du ccr2 |
WO2016113205A1 (fr) | 2015-01-13 | 2016-07-21 | Bayer Pharma Aktiengesellschaft | Pentafluoréthylpyrimidinones substituées et leur utilisation |
WO2018071283A1 (fr) * | 2016-10-12 | 2018-04-19 | Merck Sharp & Dohme Corp. | Inhibiteurs de kdm5 |
US10975084B2 (en) | 2016-10-12 | 2021-04-13 | Merck Sharp & Dohme Corp. | KDM5 inhibitors |
WO2018071282A1 (fr) * | 2016-10-12 | 2018-04-19 | Merck Sharp & Dohme Corp. | Inhibiteurs de kdm5 |
CN106749271A (zh) * | 2016-12-07 | 2017-05-31 | 青岛科技大学 | 一类[1,2,4]‑三氮唑并[1,5‑a]嘧啶酮类杂环化合物、其制备方法及其用途 |
US11583532B2 (en) | 2018-02-02 | 2023-02-21 | Boehringer Ingelheim International Gmbh | Triazolopyrimidine derivatives for use as ghrelin o-acyl transferase (GOAT) inhibitors |
JP7083397B2 (ja) | 2018-02-02 | 2022-06-10 | 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 | グレリンo-アシルトランスフェラーゼ(goat)阻害剤として使用するためのトリアゾロピリミジン誘導体 |
JP2021512115A (ja) * | 2018-02-02 | 2021-05-13 | 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 | グレリンo−アシルトランスフェラーゼ(goat)阻害剤として使用するためのトリアゾロピリミジン誘導体 |
JP2021523177A (ja) * | 2018-05-11 | 2021-09-02 | ディザル(ジァンスー)ファーマシューティカル・カンパニー・リミテッド | トリアゾロピリミジン化合物およびがんの処置におけるそれらの使用 |
JP7418353B2 (ja) | 2018-05-11 | 2024-01-19 | ディザル(ジァンスー)ファーマシューティカル・カンパニー・リミテッド | トリアゾロピリミジン化合物およびがんの処置におけるそれらの使用 |
CN113692306A (zh) * | 2019-04-03 | 2021-11-23 | 泰拉强石株式会社 | 基于胸腺嘧啶核酸碱基的三唑并嘧啶类及其制造方法 |
US11512097B2 (en) | 2019-11-25 | 2022-11-29 | Amgen Inc. | Heterocyclic compounds as Delta-5 desaturase inhibitors and methods of use |
WO2021108408A1 (fr) * | 2019-11-25 | 2021-06-03 | Amgen Inc. | Composés hétérocycliques en tant qu'inhibiteurs de delta-5 désaturase et procédés d'utilisation |
KR20220106159A (ko) * | 2019-11-25 | 2022-07-28 | 암젠 인크 | 델타-5 불포화효소 억제제로서의 헤테로시클릭 화합물 및 사용 방법 |
TWI815061B (zh) * | 2019-11-25 | 2023-09-11 | 美商安進公司 | 作為δ-5去飽和酶抑制劑的雜環化合物以及使用方法 |
KR102598203B1 (ko) | 2019-11-25 | 2023-11-03 | 암젠 인크 | 델타-5 불포화효소 억제제로서의 헤테로시클릭 화합물 및 사용 방법 |
CN114728167A (zh) * | 2019-11-25 | 2022-07-08 | 安进公司 | 作为δ-5脱饱和酶抑制剂的杂环化合物以及使用方法 |
CN114728167B (zh) * | 2019-11-25 | 2024-03-19 | 安进公司 | 作为δ-5脱饱和酶抑制剂的杂环化合物以及使用方法 |
US11976082B2 (en) | 2020-05-22 | 2024-05-07 | Boehringer Ingelheim International Gmbh | Continuous process for manufacturing alkyl 7-amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridine-carboxylate |
RU2808622C1 (ru) * | 2022-12-26 | 2023-11-30 | Федеральное государственное автономное образовательное учреждение высшего образования "Уральский федеральный университет имени первого Президента России Б.Н. Ельцина" | 3-Бензил-5-метил-6-(фенилтио)-[1,2,4]триазоло[1,5-a]пиримидин-7(3H)-он, обладающий противовирусной активностью в отношении коронавируса SARS-CoV2 |
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