NZ586695A - TRICYCLIC COMPOUNDS AS MODULATORS OF TNF-alpha SYNTHESIS AND AS PDE4 INHIBITORS - Google Patents
TRICYCLIC COMPOUNDS AS MODULATORS OF TNF-alpha SYNTHESIS AND AS PDE4 INHIBITORSInfo
- Publication number
- NZ586695A NZ586695A NZ586695A NZ58669509A NZ586695A NZ 586695 A NZ586695 A NZ 586695A NZ 586695 A NZ586695 A NZ 586695A NZ 58669509 A NZ58669509 A NZ 58669509A NZ 586695 A NZ586695 A NZ 586695A
- Authority
- NZ
- New Zealand
- Prior art keywords
- methoxy
- quinoline
- pyrimido
- dione
- chloro
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims abstract description 146
- 108060008682 Tumor Necrosis Factor Proteins 0.000 title abstract description 78
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 title abstract description 58
- 230000015572 biosynthetic process Effects 0.000 title description 8
- 238000003786 synthesis reaction Methods 0.000 title description 8
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 title description 3
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 title description 3
- MZOFCQQQCNRIBI-VMXHOPILSA-N (3s)-4-[[(2s)-1-[[(2s)-1-[[(1s)-1-carboxy-2-hydroxyethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-[[2-[[(2s)-2,6-diaminohexanoyl]amino]acetyl]amino]-4-oxobutanoic acid Chemical compound OC[C@@H](C(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@@H](N)CCCCN MZOFCQQQCNRIBI-VMXHOPILSA-N 0.000 title description 2
- 238000000034 method Methods 0.000 claims abstract description 272
- 150000003839 salts Chemical class 0.000 claims abstract description 52
- 239000000203 mixture Substances 0.000 claims abstract description 41
- IISWCMIDUMTUPJ-UHFFFAOYSA-N 3-(3-chlorophenyl)-1-(1-ethylsulfonylpiperidin-4-yl)-7-methoxypyrimido[5,4-c]quinoline-2,4-dione Chemical compound C1CN(S(=O)(=O)CC)CCC1N1C(=O)N(C=2C=C(Cl)C=CC=2)C(=O)C2=CN=C3C(OC)=CC=CC3=C21 IISWCMIDUMTUPJ-UHFFFAOYSA-N 0.000 claims abstract description 7
- QBTZSDNOQVLDBB-INIZCTEOSA-N 3-(3-chlorophenyl)-7-methoxy-1-[(3s)-1-methylsulfonylpyrrolidin-3-yl]pyrimido[5,4-c]quinoline-2,4-dione Chemical compound COC1=CC=CC2=C1N=CC(C(N(C=1C=C(Cl)C=CC=1)C1=O)=O)=C2N1[C@H]1CCN(S(C)(=O)=O)C1 QBTZSDNOQVLDBB-INIZCTEOSA-N 0.000 claims abstract description 6
- QBTZSDNOQVLDBB-MRXNPFEDSA-N 3-(3-chlorophenyl)-7-methoxy-1-[(3r)-1-methylsulfonylpyrrolidin-3-yl]pyrimido[5,4-c]quinoline-2,4-dione Chemical compound COC1=CC=CC2=C1N=CC(C(N(C=1C=C(Cl)C=CC=1)C1=O)=O)=C2N1[C@@H]1CCN(S(C)(=O)=O)C1 QBTZSDNOQVLDBB-MRXNPFEDSA-N 0.000 claims abstract description 5
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- SUUKGKCXNMAFGK-UHFFFAOYSA-N 1h-pyrimido[5,4-c]quinoline-2,4-dione Chemical compound C1=CC=CC2=NC=C(C(=O)NC(=O)N3)C3=C21 SUUKGKCXNMAFGK-UHFFFAOYSA-N 0.000 claims description 8
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- MUQKVPSLHRVESB-UHFFFAOYSA-N 3-(3-chlorophenyl)-7-methoxy-1-(1-methylsulfonylpiperidin-4-yl)pyrimido[5,4-c]quinoline-2,4-dione Chemical compound COC1=CC=CC2=C1N=CC(C(N(C=1C=C(Cl)C=CC=1)C1=O)=O)=C2N1C1CCN(S(C)(=O)=O)CC1 MUQKVPSLHRVESB-UHFFFAOYSA-N 0.000 claims description 7
- 239000012131 assay buffer Substances 0.000 claims description 6
- 125000004494 ethyl ester group Chemical group 0.000 claims description 5
- NMCBQDCTQPGXHQ-UHFFFAOYSA-N 1-cyclopentyl-7-methoxy-3-(3-methylphenyl)pyrimido[5,4-c]quinoline-2,4-dione Chemical compound COC1=CC=CC2=C1N=CC(C(N(C=1C=C(C)C=CC=1)C1=O)=O)=C2N1C1CCCC1 NMCBQDCTQPGXHQ-UHFFFAOYSA-N 0.000 claims description 4
- 101000988419 Homo sapiens cAMP-specific 3',5'-cyclic phosphodiesterase 4D Proteins 0.000 claims description 4
- CTKRVYLHFHYHOK-GOSISDBHSA-N tert-butyl (3r)-3-[3-(3-chlorophenyl)-7-methoxy-2,4-dioxopyrimido[5,4-c]quinolin-1-yl]pyrrolidine-1-carboxylate Chemical compound COC1=CC=CC2=C1N=CC(C(N(C=1C=C(Cl)C=CC=1)C1=O)=O)=C2N1[C@@H]1CCN(C(=O)OC(C)(C)C)C1 CTKRVYLHFHYHOK-GOSISDBHSA-N 0.000 claims description 4
- 238000002877 time resolved fluorescence resonance energy transfer Methods 0.000 claims description 4
- XBMCCMKXNQMPDO-UHFFFAOYSA-N 1-cyclopentyl-7-methoxy-3-(4-methylthiophen-2-yl)pyrimido[5,4-c]quinoline-2,4-dione Chemical compound COC1=CC=CC2=C1N=CC(C(N(C=1SC=C(C)C=1)C1=O)=O)=C2N1C1CCCC1 XBMCCMKXNQMPDO-UHFFFAOYSA-N 0.000 claims description 3
- BOWZLOCTDYTWKK-UHFFFAOYSA-N 3-(3-chlorophenyl)-1-cyclohexyl-7-methoxypyrimido[5,4-c]quinoline-2,4-dione Chemical compound COC1=CC=CC2=C1N=CC(C(N(C=1C=C(Cl)C=CC=1)C1=O)=O)=C2N1C1CCCCC1 BOWZLOCTDYTWKK-UHFFFAOYSA-N 0.000 claims description 3
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- PEPXWYFVYAYCEQ-HNNXBMFYSA-N 3-(3-chlorophenyl)-7-methoxy-1-[(3s)-pyrrolidin-3-yl]pyrimido[5,4-c]quinoline-2,4-dione Chemical compound COC1=CC=CC2=C1N=CC(C(N(C=1C=C(Cl)C=CC=1)C1=O)=O)=C2N1[C@H]1CCNC1 PEPXWYFVYAYCEQ-HNNXBMFYSA-N 0.000 claims description 2
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- PEPXWYFVYAYCEQ-OAHLLOKOSA-N 3-(3-chlorophenyl)-7-methoxy-1-[(3r)-pyrrolidin-3-yl]pyrimido[5,4-c]quinoline-2,4-dione Chemical compound COC1=CC=CC2=C1N=CC(C(N(C=1C=C(Cl)C=CC=1)C1=O)=O)=C2N1[C@@H]1CCNC1 PEPXWYFVYAYCEQ-OAHLLOKOSA-N 0.000 claims 1
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| HUE042374T2 (hu) | 2012-06-13 | 2019-06-28 | Incyte Holdings Corp | Szubsztituált triciklusos vegyületek mint FGFR inhibitorok |
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| KR102469849B1 (ko) | 2013-04-19 | 2022-11-23 | 인사이트 홀딩스 코포레이션 | Fgfr 저해제로서 이환식 헤테로사이클 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| AU2016219822B2 (en) | 2015-02-20 | 2020-07-09 | Incyte Holdings Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| TN2017000485A1 (en) * | 2015-06-17 | 2019-04-12 | Pfizer | Tricyclic compounds and their use as phosphodiesterase inhibitors |
| WO2017089347A1 (en) | 2015-11-25 | 2017-06-01 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Methods and pharmaceutical compositions for the treatment of braf inhibitor resistant melanomas |
| MA47106A (fr) | 2016-12-21 | 2019-10-30 | Amgen Inc | Formulations d'anticorps anti-tnf alpha |
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| CN109705037A (zh) * | 2019-01-24 | 2019-05-03 | 广西师范大学 | 4-氨基喹啉-3-甲酸酯衍生物及其制备方法和应用 |
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| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| KR102766496B1 (ko) | 2019-08-09 | 2025-02-10 | 주식회사 엘지에너지솔루션 | 연쇄발화 방지를 위한 에너지 드레인 저항체를 구비한 배터리 팩 |
| US12122767B2 (en) | 2019-10-01 | 2024-10-22 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021076602A1 (en) | 2019-10-14 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| JP7720840B2 (ja) | 2019-12-04 | 2025-08-08 | インサイト・コーポレイション | Fgfr阻害剤としての三環式複素環 |
| KR20220131900A (ko) | 2019-12-04 | 2022-09-29 | 인사이트 코포레이션 | Fgfr 억제제의 유도체 |
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| CN111808098B (zh) * | 2020-06-29 | 2021-08-24 | Vtv治疗有限责任公司 | 喹啉衍生物,其药学上可接受的盐及其使用方法 |
| TW202220986A (zh) * | 2020-07-28 | 2022-06-01 | 美商維特衛治療有限責任公司 | 喹啉衍生物的鹽酸鹽的結晶形式 |
| CN116529247A (zh) * | 2020-07-28 | 2023-08-01 | 维特卫治疗有限责任公司 | 喹啉衍生物的盐酸盐的晶型 |
| CA3215903A1 (en) | 2021-04-12 | 2022-10-20 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| EP4352059A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2022261159A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| CA3241173A1 (en) * | 2021-12-15 | 2023-06-22 | Innovstone Therapeutics Limited | Aromatic heterocyclic compounds, preparation method therefor and uses thereof |
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| JPH0741479A (ja) * | 1993-07-28 | 1995-02-10 | Taisho Pharmaceut Co Ltd | 7−アザプテリジン類およびその製造方法 |
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| US6930101B1 (en) * | 1999-05-17 | 2005-08-16 | The Regents Of The University Of California | Thiazolopyrimidines useful as TNFα inhibitors |
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| JP2012519159A (ja) | 2009-02-27 | 2012-08-23 | 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 | Pde4阻害剤及びnsaidを含有する複合薬 |
| WO2010097334A1 (de) | 2009-02-27 | 2010-09-02 | Boehringer Ingelheim International Gmbh | Arzneimittelkombinationen enthaltend pde4-inhibitoren und nsaids |
| EP2555774B1 (de) | 2010-04-08 | 2015-10-21 | Boehringer Ingelheim International GmbH | Arnzeimittelkombinationen enthaltend pde4-inhibitoren und ep4-rezeptor-antagonisten |
| JP2013529184A (ja) | 2010-04-08 | 2013-07-18 | 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 | Pde4阻害剤及びep4受容体アンタゴニストを含有する医薬の組み合わせ |
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