JP2017516826A5 - - Google Patents
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- JP2017516826A5 JP2017516826A5 JP2016571095A JP2016571095A JP2017516826A5 JP 2017516826 A5 JP2017516826 A5 JP 2017516826A5 JP 2016571095 A JP2016571095 A JP 2016571095A JP 2016571095 A JP2016571095 A JP 2016571095A JP 2017516826 A5 JP2017516826 A5 JP 2017516826A5
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- 125000000217 alkyl group Chemical group 0.000 claims description 73
- 229910052736 halogen Inorganic materials 0.000 claims description 66
- 150000002367 halogens Chemical class 0.000 claims description 56
- 229910052739 hydrogen Inorganic materials 0.000 claims description 48
- 239000001257 hydrogen Substances 0.000 claims description 48
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 36
- 150000001875 compounds Chemical class 0.000 claims description 34
- 125000001153 fluoro group Chemical group F* 0.000 claims description 32
- 125000001072 heteroaryl group Chemical group 0.000 claims description 30
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 26
- 125000005842 heteroatom Chemical group 0.000 claims description 20
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 20
- 150000002431 hydrogen Chemical class 0.000 claims description 20
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 16
- 229910052757 nitrogen Inorganic materials 0.000 claims description 14
- 125000003118 aryl group Chemical group 0.000 claims description 12
- 125000002950 monocyclic group Chemical group 0.000 claims description 12
- 201000010099 disease Diseases 0.000 claims description 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 10
- 125000005843 halogen group Chemical group 0.000 claims description 10
- 229910052799 carbon Inorganic materials 0.000 claims description 8
- 125000006574 non-aromatic ring group Chemical group 0.000 claims description 8
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 8
- -1 3,5-dichlorophenyl Chemical group 0.000 claims description 6
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims description 6
- 125000004429 atom Chemical group 0.000 claims description 6
- 125000004432 carbon atom Chemical group C* 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- 125000005330 8 membered heterocyclic group Chemical group 0.000 claims description 4
- 201000001320 Atherosclerosis Diseases 0.000 claims description 4
- ZOXJGFHDIHLPTG-UHFFFAOYSA-N Boron Chemical compound [B] ZOXJGFHDIHLPTG-UHFFFAOYSA-N 0.000 claims description 4
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 4
- 208000011231 Crohn disease Diseases 0.000 claims description 4
- 201000004681 Psoriasis Diseases 0.000 claims description 4
- 201000006704 Ulcerative Colitis Diseases 0.000 claims description 4
- 125000002619 bicyclic group Chemical group 0.000 claims description 4
- 229910052796 boron Inorganic materials 0.000 claims description 4
- 239000013066 combination product Substances 0.000 claims description 4
- 229940127555 combination product Drugs 0.000 claims description 4
- 201000006417 multiple sclerosis Diseases 0.000 claims description 4
- 210000000056 organ Anatomy 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims description 4
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims description 4
- 238000002054 transplantation Methods 0.000 claims description 4
- 208000030289 Lymphoproliferative disease Diseases 0.000 claims description 3
- 125000004122 cyclic group Chemical group 0.000 claims description 3
- 125000004434 sulfur atom Chemical group 0.000 claims description 3
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims description 2
- QTYUBTIUPVVINO-JTQLQIEISA-N 4-n-[(1s)-1-(2,4-difluorophenyl)ethyl]-6-pyrazolo[1,5-a]pyrimidin-3-ylpyrimidine-2,4-diamine Chemical compound C1([C@@H](NC=2N=C(N)N=C(C=2)C2=C3N=CC=CN3N=C2)C)=CC=C(F)C=C1F QTYUBTIUPVVINO-JTQLQIEISA-N 0.000 claims description 2
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims description 2
- 208000003343 Antiphospholipid Syndrome Diseases 0.000 claims description 2
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- 208000023328 Basedow disease Diseases 0.000 claims description 2
- 208000009137 Behcet syndrome Diseases 0.000 claims description 2
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims description 2
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims description 2
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 2
- 241000701022 Cytomegalovirus Species 0.000 claims description 2
- 208000001708 Dupuytren contracture Diseases 0.000 claims description 2
- 208000007465 Giant cell arteritis Diseases 0.000 claims description 2
- 208000024869 Goodpasture syndrome Diseases 0.000 claims description 2
- 206010072579 Granulomatosis with polyangiitis Diseases 0.000 claims description 2
- 208000015023 Graves' disease Diseases 0.000 claims description 2
- 208000035895 Guillain-Barré syndrome Diseases 0.000 claims description 2
- 208000001204 Hashimoto Disease Diseases 0.000 claims description 2
- 208000030836 Hashimoto thyroiditis Diseases 0.000 claims description 2
- 241000701044 Human gammaherpesvirus 4 Species 0.000 claims description 2
- 206010021245 Idiopathic thrombocytopenic purpura Diseases 0.000 claims description 2
- 206010049567 Miller Fisher syndrome Diseases 0.000 claims description 2
- 208000003250 Mixed connective tissue disease Diseases 0.000 claims description 2
- 201000002481 Myositis Diseases 0.000 claims description 2
- 208000004362 Penile Induration Diseases 0.000 claims description 2
- 208000031845 Pernicious anaemia Diseases 0.000 claims description 2
- 208000020758 Peyronie disease Diseases 0.000 claims description 2
- 208000010366 Postpoliomyelitis syndrome Diseases 0.000 claims description 2
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims description 2
- 208000021386 Sjogren Syndrome Diseases 0.000 claims description 2
- 208000031981 Thrombocytopenic Idiopathic Purpura Diseases 0.000 claims description 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims description 2
- 206010047115 Vasculitis Diseases 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 208000004631 alopecia areata Diseases 0.000 claims description 2
- 230000000340 anti-metabolite Effects 0.000 claims description 2
- 229940100197 antimetabolite Drugs 0.000 claims description 2
- 239000002256 antimetabolite Substances 0.000 claims description 2
- 201000003710 autoimmune thrombocytopenic purpura Diseases 0.000 claims description 2
- 201000004982 autoimmune uveitis Diseases 0.000 claims description 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 2
- 201000001981 dermatomyositis Diseases 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 239000003862 glucocorticoid Substances 0.000 claims description 2
- 125000006588 heterocycloalkylene group Chemical group 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 2
- 239000003018 immunosuppressive agent Substances 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 206010028417 myasthenia gravis Diseases 0.000 claims description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 2
- 208000030346 palmar fibromatosis Diseases 0.000 claims description 2
- 208000005987 polymyositis Diseases 0.000 claims description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
- 206010043207 temporal arteritis Diseases 0.000 claims description 2
- 229940046728 tumor necrosis factor alpha inhibitor Drugs 0.000 claims description 2
- 239000002452 tumor necrosis factor alpha inhibitor Substances 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 29
- 208000032671 Allergic granulomatous angiitis Diseases 0.000 claims 1
- 206010003827 Autoimmune hepatitis Diseases 0.000 claims 1
- 208000031229 Cardiomyopathies Diseases 0.000 claims 1
- 208000006344 Churg-Strauss Syndrome Diseases 0.000 claims 1
- 208000018428 Eosinophilic granulomatosis with polyangiitis Diseases 0.000 claims 1
- 241000721454 Pemphigus Species 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 229960003444 immunosuppressant agent Drugs 0.000 claims 1
- 230000001861 immunosuppressant effect Effects 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 210000004027 cell Anatomy 0.000 description 3
- 210000001744 T-lymphocyte Anatomy 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 101000744394 Homo sapiens Oxidized purine nucleoside triphosphate hydrolase Proteins 0.000 description 1
- 101000914514 Homo sapiens T-cell-specific surface glycoprotein CD28 Proteins 0.000 description 1
- 102100039792 Oxidized purine nucleoside triphosphate hydrolase Human genes 0.000 description 1
- 201000011152 Pemphigus Diseases 0.000 description 1
- PLXBWHJQWKZRKG-UHFFFAOYSA-N Resazurin Chemical compound C1=CC(=O)C=C2OC3=CC(O)=CC=C3[N+]([O-])=C21 PLXBWHJQWKZRKG-UHFFFAOYSA-N 0.000 description 1
- 102100027213 T-cell-specific surface glycoprotein CD28 Human genes 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 201000004984 autoimmune cardiomyopathy Diseases 0.000 description 1
- 208000037979 autoimmune inflammatory disease Diseases 0.000 description 1
- 230000005784 autoimmunity Effects 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 238000000423 cell based assay Methods 0.000 description 1
- 230000004663 cell proliferation Effects 0.000 description 1
- 230000003833 cell viability Effects 0.000 description 1
- 208000006454 hepatitis Diseases 0.000 description 1
- 231100000283 hepatitis Toxicity 0.000 description 1
- 229940125721 immunosuppressive agent Drugs 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 201000001976 pemphigus vulgaris Diseases 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 239000013641 positive control Substances 0.000 description 1
- 238000012289 standard assay Methods 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE1450681-0 | 2014-06-04 | ||
| SE1450681 | 2014-06-04 | ||
| PCT/SE2015/050654 WO2015187089A1 (en) | 2014-06-04 | 2015-06-04 | Mth1 inhibitors for treatment of inflammatory and autoimmune conditions |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017516826A JP2017516826A (ja) | 2017-06-22 |
| JP2017516826A5 true JP2017516826A5 (https=) | 2018-06-28 |
| JP6635949B2 JP6635949B2 (ja) | 2020-01-29 |
Family
ID=54767050
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016571095A Active JP6635949B2 (ja) | 2014-06-04 | 2015-06-04 | 炎症性および自己免疫性の病気の処置のためのｍｔｈ１阻害剤 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US10064869B2 (https=) |
| EP (1) | EP3151833A4 (https=) |
| JP (1) | JP6635949B2 (https=) |
| CN (1) | CN106794181A (https=) |
| AU (1) | AU2015268962A1 (https=) |
| CA (1) | CA2948601A1 (https=) |
| IL (1) | IL249223A0 (https=) |
| RU (1) | RU2016151390A (https=) |
| SG (1) | SG11201609981RA (https=) |
| WO (1) | WO2015187089A1 (https=) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2014362231B2 (en) * | 2013-12-11 | 2019-04-04 | Biogen Ma Inc. | Biaryl compounds useful for the treatment of human diseases in oncology, neurology and immunology |
| WO2015187088A1 (en) * | 2014-06-04 | 2015-12-10 | Thomas Helledays Stiftelse För Medicinsk Forskning | Mth1 inhibitors for treatment of cancer |
| US10064869B2 (en) * | 2014-06-04 | 2018-09-04 | Thomas Helledays Stiftelse For Medicinsk Forskning | MTH1 inhibitors for treatment of inflammatory and autoimmune conditions |
| JP6779867B2 (ja) * | 2014-06-13 | 2020-11-04 | ユマ セラピューティクス，インコーポレーテッド | ピリミジン化合物およびその使用方法 |
| CR20180323A (es) | 2015-11-20 | 2018-08-06 | Idorsia Pharmaceuticals Ltd | Derivados de indol n-sustituídos como moduladores de los receptores de pge2 |
| US10618892B2 (en) * | 2016-02-17 | 2020-04-14 | Merck Sharp & Dohme Corp. | Processes for the preparation of a BACE inhibitor |
| UA120571C2 (uk) | 2016-03-22 | 2019-12-26 | Мерк Шарп Енд Дохме Корп. | Алостеричні модулятори нікотинових ацетилхолінових рецепторів |
| EP3445750A4 (en) * | 2016-04-18 | 2019-11-27 | Celgene Quanticel Research, Inc. | THERAPEUTIC COMPOUNDS |
| WO2018195155A1 (en) | 2017-04-18 | 2018-10-25 | Celgene Quanticel Research, Inc. | Therapeutic compounds |
| KR102612140B1 (ko) | 2017-05-18 | 2023-12-08 | 이도르시아 파마슈티컬스 리미티드 | 피리미딘 유도체 |
| TW201900179A (zh) | 2017-05-18 | 2019-01-01 | 瑞士商愛杜西亞製藥有限公司 | 作為pge2受體調節劑之苯并呋喃及苯并噻吩衍生物 |
| PE20191814A1 (es) | 2017-05-18 | 2019-12-27 | Idorsia Pharmaceuticals Ltd | Derivados de pirimidina como moduladores del receptor de pge2 |
| US11839613B2 (en) | 2017-05-18 | 2023-12-12 | Idorsia Pharmaceuticals Ltd | Pyrimidine derivatives as PGE2 receptor modulators |
| 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 |
| WO2019133904A1 (en) * | 2017-12-30 | 2019-07-04 | 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 |
| CA3091951A1 (en) | 2018-03-01 | 2019-09-06 | Thomas Helledays Stiftelse For Medicinsk Forskning | Substituted benzodiazoles and use thereof in therapy |
| CN111960985A (zh) * | 2018-08-08 | 2020-11-20 | 中国人民解放军总医院 | 抗肿瘤化合物 |
| 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 |
| CN117396474A (zh) * | 2021-03-17 | 2024-01-12 | 武田药品工业株式会社 | 血浆激肽释放酶抑制剂 |
| GB202108249D0 (en) * | 2021-06-09 | 2021-07-21 | Univ Of Sussex | Compounds |
| CN120379972A (zh) * | 2022-12-20 | 2025-07-25 | 深圳湾实验室 | 一种靶向usp1的小分子抑制剂及其应用 |
| WO2025143733A1 (ko) * | 2023-12-26 | 2025-07-03 | (주)아이젠사이언스 | 신규한 유비퀴틴 특이적 펩티드 분해효소 1 저해제 |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB681712A (en) | 1949-09-14 | 1952-10-29 | Burroughs Wellcome Co | Improvements in or relating to therapeutically useful pyrimidine compounds |
| JPS4921148B1 (https=) | 1970-12-28 | 1974-05-30 | ||
| JPS4921147B1 (https=) | 1970-12-28 | 1974-05-30 | ||
| WO1986004583A1 (en) | 1985-02-05 | 1986-08-14 | The Upjohn Company | 4-substituted-6-aryl pyrimidine compounds |
| US6169086B1 (en) | 1997-01-27 | 2001-01-02 | Daiichi Pharmaceutical Co., Ltd. | Pyrazole derivatives |
| US6573377B1 (en) | 1998-07-24 | 2003-06-03 | Daiichi Pharmaceuticals Co., Ltd. | Pyrazole derivatives and salts thereof |
| JP5102928B2 (ja) * | 2000-06-30 | 2012-12-19 | イーライ リリー アンド カンパニー | 新規な葉酸代謝拮抗薬の組み合わせ療法 |
| WO2002096867A2 (en) | 2001-05-30 | 2002-12-05 | Lg Biomedical Institute | Inhibitors of protein kinase for the treatment of disease |
| ATE325608T1 (de) | 2001-08-13 | 2006-06-15 | Janssen Pharmaceutica Nv | 2,4,5-trisubstituted thiazolyl derivative und deren antiinflammatorische wirkung |
| US7419984B2 (en) | 2002-10-17 | 2008-09-02 | Cell Therapeutics, Inc. | Pyrimidines and uses thereof |
| WO2004080979A1 (en) | 2003-03-14 | 2004-09-23 | Lg Life Sciences Ltd. | Novel 3-(2-amino-4-pyrimidinyl)-4-hydroxyphenyl ketone derivatives |
| US8084457B2 (en) * | 2003-09-15 | 2011-12-27 | Lead Discovery Center Gmbh | Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases |
| MXPA06010900A (es) | 2004-03-26 | 2007-02-21 | Methylgene Inc | Inhibidores de histona desacetilasa. |
| WO2006078886A2 (en) | 2005-01-18 | 2006-07-27 | Irm Llc | Compounds and compositions as wnt signaling pathway modulators |
| US20100035863A1 (en) * | 2006-09-12 | 2010-02-11 | Ucb Pharma, S.A. | 2 Amino-Pyrimidine Derivatives As H4 Receptor Antagonists, Processes For Preparing Them And Their Use In Pharmaceutical Compositions |
| CL2008000467A1 (es) | 2007-02-14 | 2008-08-22 | Janssen Pharmaceutica Nv | Compuestos derivados de 2-aminopirimidina, moduladores del receptor histamina h4; su procedimiento de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar un trastorno inflamatorio seleccionado de alegia, asma |
| EP2254415B1 (en) | 2008-02-19 | 2013-01-23 | 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 |
| AR074199A1 (es) * | 2008-11-20 | 2010-12-29 | Glaxosmithkline Llc | Compuesto de 6-(4-pirimidinil)-1h-indazol, composiciones farmaceuticas que lo comprenden y su uso para preparar un medicamento util para el tratamiento o disminucion de la gravedad del cancer. |
| CN102711749A (zh) | 2009-11-05 | 2012-10-03 | 莱西肯医药有限公司 | 用于癌症治疗的色氨酸羟化酶抑制剂 |
| CN102753168A (zh) | 2010-02-10 | 2012-10-24 | 莱西肯医药有限公司 | 用于治疗转移性骨病的色氨酸羟化酶抑制剂 |
| WO2012080729A2 (en) | 2010-12-14 | 2012-06-21 | Electrophoretics Limited | CASEIN KINASE 1δ (CK1δ) INHIBITORS |
| WO2013066839A2 (en) | 2011-10-31 | 2013-05-10 | Glaxosmithkline Llc | Compounds and methods |
| GB201215502D0 (en) | 2012-08-31 | 2012-10-17 | Chalkiadakis Spyridon | Medical use |
| EP2925744B1 (en) * | 2012-11-27 | 2020-12-30 | Thomas Helledays Stiftelse För Medicinsk Forskning | Pyrimidine-2,4-diamine derivatives for treatment of cancer |
| US10064869B2 (en) * | 2014-06-04 | 2018-09-04 | Thomas Helledays Stiftelse For Medicinsk Forskning | MTH1 inhibitors for treatment of inflammatory and autoimmune conditions |
| 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 |
-
2015
- 2015-06-04 US US15/315,478 patent/US10064869B2/en active Active
- 2015-06-04 JP JP2016571095A patent/JP6635949B2/ja active Active
- 2015-06-04 EP EP15802742.5A patent/EP3151833A4/en not_active Withdrawn
- 2015-06-04 CN CN201580029524.6A patent/CN106794181A/zh active Pending
- 2015-06-04 SG SG11201609981RA patent/SG11201609981RA/en unknown
- 2015-06-04 AU AU2015268962A patent/AU2015268962A1/en not_active Abandoned
- 2015-06-04 CA CA2948601A patent/CA2948601A1/en not_active Abandoned
- 2015-06-04 WO PCT/SE2015/050654 patent/WO2015187089A1/en not_active Ceased
- 2015-06-04 RU RU2016151390A patent/RU2016151390A/ru not_active Application Discontinuation
-
2016
- 2016-11-27 IL IL249223A patent/IL249223A0/en unknown
-
2018
- 2018-08-31 US US16/120,170 patent/US10632125B2/en active Active
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