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 | 2014-06-04 | ||
| SE1450681-0 | 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 (OSRAM) | 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 (OSRAM) |
| EP (1) | EP3151833A4 (OSRAM) |
| JP (1) | JP6635949B2 (OSRAM) |
| CN (1) | CN106794181A (OSRAM) |
| AU (1) | AU2015268962A1 (OSRAM) |
| CA (1) | CA2948601A1 (OSRAM) |
| IL (1) | IL249223A0 (OSRAM) |
| RU (1) | RU2016151390A (OSRAM) |
| SG (1) | SG11201609981RA (OSRAM) |
| WO (1) | WO2015187089A1 (OSRAM) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20181109T1 (hr) * | 2013-12-11 | 2018-11-02 | Biogen Ma Inc. | Spojevi biarila korisni za liječenje ljudskih bolesti u onkologiji, neurologiji i imunologiji |
| CN106794181A (zh) * | 2014-06-04 | 2017-05-31 | 托马斯·黑勒戴药物研究基金会 | 用于治疗炎性和自身免疫性病况的mth1抑制剂 |
| CA2949785A1 (en) * | 2014-06-04 | 2015-12-10 | Thomas Helledays Stiftelse For Medicinsk Forskning | Mth1 inhibitors for treatment of cancer |
| CA2952230C (en) | 2014-06-13 | 2023-03-21 | Yuma Therapeutics, Inc. | Pyrimidine compounds and methods using the same |
| CR20180323A (es) | 2015-11-20 | 2018-08-06 | Idorsia Pharmaceuticals Ltd | Derivados de indol n-sustituídos como moduladores de los receptores de pge2 |
| WO2017142804A1 (en) * | 2016-02-17 | 2017-08-24 | Merck Sharp & Dohme Corp. | Processes for the preparation of a bace inhibitor |
| GEAP202014908A (en) | 2016-03-22 | 2020-03-10 | Merck Sharp & Dohme | Allosteric modulators of nicotinic acetylcholine receptors |
| WO2017184462A1 (en) * | 2016-04-18 | 2017-10-26 | Celgene Quanticel Research, Inc. | Therapeutic compounds |
| WO2018195155A1 (en) | 2017-04-18 | 2018-10-25 | Celgene Quanticel Research, Inc. | Therapeutic compounds |
| CN110612296A (zh) | 2017-05-18 | 2019-12-24 | 爱杜西亚药品有限公司 | 作为pge2受体调节剂的苯基衍生物 |
| JP7093791B2 (ja) | 2017-05-18 | 2022-06-30 | イドーシア ファーマシューティカルズ リミテッド | Ｐｇｅ２レセプター調節剤としてのベンゾフラン及びベンゾチオフェン誘導体 |
| AU2018268311B2 (en) | 2017-05-18 | 2022-02-10 | Idorsia Pharmaceuticals Ltd | Pyrimidine derivatives as PGE2 receptor modulators |
| TW201900180A (zh) | 2017-05-18 | 2019-01-01 | 瑞士商愛杜西亞製藥有限公司 | 嘧啶衍生物 |
| 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 |
| CN111892516A (zh) * | 2018-08-08 | 2020-11-06 | 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 |
| JP2024510503A (ja) * | 2021-03-17 | 2024-03-07 | 武田薬品工業株式会社 | 血漿カリクレイン阻害剤 |
| 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 |
| KR20250100559A (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 (OSRAM) | 1970-12-28 | 1974-05-30 | ||
| JPS4921147B1 (OSRAM) | 1970-12-28 | 1974-05-30 | ||
| JPS62501632A (ja) | 1985-02-05 | 1987-07-02 | ジ・アップジョン・カンパニ− | ４−置換−６−アリ−ルピリミジン化合物 |
| US6169086B1 (en) | 1997-01-27 | 2001-01-02 | Daiichi Pharmaceutical Co., Ltd. | Pyrazole derivatives |
| CN1320122A (zh) | 1998-07-24 | 2001-10-31 | 第一制药株式会社 | 吡唑衍生物及其盐 |
| WO2002002093A2 (en) | 2000-06-30 | 2002-01-10 | Eli Lilly And Company | Combination containing an antifolate and methylmalonic acid lowering agent |
| EP1412327A2 (en) | 2001-05-30 | 2004-04-28 | LG Biomedical Institute | Inhibitors of protein kinase for the treatment of disease |
| WO2003015776A1 (en) | 2001-08-13 | 2003-02-27 | Janssen Pharmaceutica N.V. | 2,4,5-trisubstituted thiazolyl derivatives and their antiinflammatory activity |
| 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 |
| EP1678147B1 (en) | 2003-09-15 | 2012-08-08 | Lead Discovery Center GmbH | Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases |
| EP1735319B1 (en) | 2004-03-26 | 2017-05-03 | MethylGene Inc. | Inhibitors of histone deacetylase |
| 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 |
| TW200904437A (en) | 2007-02-14 | 2009-02-01 | Janssen Pharmaceutica Nv | 2-aminopyrimidine modulators of the histamine H4 receptor |
| 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 |
| US8697685B2 (en) | 2008-11-20 | 2014-04-15 | Glaxosmithkline Llc | Chemical compounds |
| JP2013510092A (ja) | 2009-11-05 | 2013-03-21 | レクシコン ファーマシューティカルズ インコーポレイテッド | がんの治療のためのトリプトファンヒドロキシラーゼ阻害剤 |
| CA2789229A1 (en) | 2010-02-10 | 2011-08-18 | Lexicon Pharmaceuticals, Inc. | Tryptophan hydroxylase inhibitors for the treatment of metastatic bone disease |
| US20140031547A1 (en) | 2010-12-14 | 2014-01-30 | Electrophoretics Limited | CASEIN KINASE 1delta (CK 1delta) INHIBITORS AND THEIR USE IN THE TREATMENT OF NEURODE-GENERATIVE DISEASES SUCH AS TAUOPATHIES |
| 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 |
| RU2672916C2 (ru) * | 2012-11-27 | 2018-11-21 | Томас Хелледайс Стифтелсе Фёр Медисинск Форскнинг | Производные пиримидин-2,4-диамина для лечения рака |
| CN106794181A (zh) * | 2014-06-04 | 2017-05-31 | 托马斯·黑勒戴药物研究基金会 | 用于治疗炎性和自身免疫性病况的mth1抑制剂 |
| 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 CN CN201580029524.6A patent/CN106794181A/zh active Pending
- 2015-06-04 US US15/315,478 patent/US10064869B2/en active Active
- 2015-06-04 EP EP15802742.5A patent/EP3151833A4/en not_active Withdrawn
- 2015-06-04 JP JP2016571095A patent/JP6635949B2/ja active Active
- 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 AU AU2015268962A patent/AU2015268962A1/en not_active Abandoned
- 2015-06-04 SG SG11201609981RA patent/SG11201609981RA/en unknown
- 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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