CA2948601A1 - Mth1 inhibitors for treatment of inflammatory and autoimmune conditions - Google Patents
Mth1 inhibitors for treatment of inflammatory and autoimmune conditions Download PDFInfo
- Publication number
- CA2948601A1 CA2948601A1 CA2948601A CA2948601A CA2948601A1 CA 2948601 A1 CA2948601 A1 CA 2948601A1 CA 2948601 A CA2948601 A CA 2948601A CA 2948601 A CA2948601 A CA 2948601A CA 2948601 A1 CA2948601 A1 CA 2948601A1
- Authority
- CA
- Canada
- Prior art keywords
- optionally substituted
- groups selected
- diamine
- chloro
- ring
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
- 238000011282 treatment Methods 0.000 title claims abstract description 42
- 230000001363 autoimmune Effects 0.000 title description 24
- 230000002757 inflammatory effect Effects 0.000 title description 7
- 239000003112 inhibitor Substances 0.000 title description 7
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- 150000001875 compounds Chemical class 0.000 claims abstract description 229
- 230000004968 inflammatory condition Effects 0.000 claims abstract description 18
- 208000023275 Autoimmune disease Diseases 0.000 claims abstract description 17
- 150000003839 salts Chemical class 0.000 claims abstract description 14
- 229910052739 hydrogen Inorganic materials 0.000 claims description 358
- 238000000034 method Methods 0.000 claims description 297
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims description 160
- -1 3,5-dichlorophenyl Chemical group 0.000 claims description 150
- 239000001257 hydrogen Substances 0.000 claims description 138
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- 150000002367 halogens Chemical group 0.000 claims description 103
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 81
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 65
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 64
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- 125000005843 halogen group Chemical group 0.000 claims description 4
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- 238000002953 preparative HPLC Methods 0.000 description 119
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 description 112
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- IAZDPXIOMUYVGZ-WFGJKAKNSA-N Dimethyl sulfoxide Chemical compound [2H]C([2H])([2H])S(=O)C([2H])([2H])[2H] IAZDPXIOMUYVGZ-WFGJKAKNSA-N 0.000 description 104
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- CSNNHWWHGAXBCP-UHFFFAOYSA-L Magnesium sulfate Chemical compound [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 description 56
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| CN106687114B (zh) | 2014-06-13 | 2021-08-31 | 尤马治疗公司 | 嘧啶化合物及其使用方法 |
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| WO2017142804A1 (en) * | 2016-02-17 | 2017-08-24 | Merck Sharp & Dohme Corp. | Processes for the preparation of a bace inhibitor |
| LT3433234T (lt) | 2016-03-22 | 2021-12-10 | Merck Sharp & Dohme Corp. | Nikotino acetilcholino receptorių alosteriniai moduliatoriai |
| JP2019513804A (ja) * | 2016-04-18 | 2019-05-30 | セルジーン クオンティセル リサーチ,インク. | 治療用化合物 |
| US10617680B2 (en) | 2017-04-18 | 2020-04-14 | Celgene Quanticel Research, Inc. | Therapeutic compounds |
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| CN109467538A (zh) | 2017-09-07 | 2019-03-15 | 和记黄埔医药(上海)有限公司 | 环烯烃取代的杂芳环类化合物及其用途 |
| US20200360386A1 (en) * | 2017-12-30 | 2020-11-19 | Unity Biotechnology, Inc. | Inhibitors of HSP90, PI3-Kinase, Proteasome, HDAC, and P97 Pathways for Selective Removal of Senescent Cells in the Treatment of Age Related Conditions |
| CN112074511B (zh) | 2018-03-01 | 2024-04-26 | 托马斯·黑勒戴药物研究基金会 | 取代的苯并二唑及其在治疗中的用途 |
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| AR116635A1 (es) * | 2018-10-15 | 2021-05-26 | Servier Lab | Proceso para la síntesis de derivados de piperazinil-etoxi-bromofenilo y su aplicación en la producción de compuestos que los contienen |
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| DE60127970T2 (de) | 2000-06-30 | 2007-12-20 | Eli Lilly And Co., Indianapolis | Zusammensetzung, welche ein antifolate und ein methylmalonsäuresenkendes mittel enthält |
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| US7419984B2 (en) | 2002-10-17 | 2008-09-02 | Cell Therapeutics, Inc. | Pyrimidines and uses thereof |
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| EP1678147B1 (en) * | 2003-09-15 | 2012-08-08 | Lead Discovery Center GmbH | Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases |
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| CA2714743C (en) | 2008-02-19 | 2017-01-17 | Janssen Pharmaceutica N.V. | Aryl-hydroxyethylamino-pyrimidines and triazines as modulators of fatty acid amide hydrolase |
| US8268846B2 (en) * | 2008-07-11 | 2012-09-18 | Abbott Laboratories | Amino heterocyclic linked pyrimidine derivatives |
| EP2362775B1 (en) | 2008-11-20 | 2015-08-05 | GlaxoSmithKline LLC | Chemical compounds |
| EP2496231A1 (en) | 2009-11-05 | 2012-09-12 | Lexicon Pharmaceuticals, Inc. | Tryptophan hydroxylase inhibitors for the treatment of cancer |
| US20130137635A1 (en) | 2010-02-10 | 2013-05-30 | Lexicon Pharmaceuticals, Inc. | Tryptophan hydroxylase inhibitors for the treatment of metastatic bone disease |
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| BR112015011497B1 (pt) * | 2012-11-27 | 2023-01-10 | Thomas Helledays Stiftelse För Medicinsk Forskning | Composto, e, formulação farmacêutica |
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| CN104288170B (zh) | 2014-10-22 | 2018-02-16 | 吉林大学 | 松果菊苷在抗肿瘤药物中的应用 |
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- 2015-06-04 CN CN201580029524.6A patent/CN106794181A/zh active Pending
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2016
- 2016-11-27 IL IL249223A patent/IL249223A0/en unknown
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2018
- 2018-08-31 US US16/120,170 patent/US10632125B2/en active Active
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|---|---|
| US20170196873A1 (en) | 2017-07-13 |
| IL249223A0 (en) | 2017-02-28 |
| CN106794181A (zh) | 2017-05-31 |
| RU2016151390A3 (OSRAM) | 2018-12-20 |
| JP6635949B2 (ja) | 2020-01-29 |
| SG11201609981RA (en) | 2016-12-29 |
| EP3151833A1 (en) | 2017-04-12 |
| RU2016151390A (ru) | 2018-07-17 |
| EP3151833A4 (en) | 2018-01-10 |
| US10632125B2 (en) | 2020-04-28 |
| JP2017516826A (ja) | 2017-06-22 |
| US10064869B2 (en) | 2018-09-04 |
| AU2015268962A1 (en) | 2017-01-12 |
| US20190000856A1 (en) | 2019-01-03 |
| WO2015187089A1 (en) | 2015-12-10 |
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