JP2018532706A5 - - Google Patents
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- JP2018532706A5 JP2018532706A5 JP2018512319A JP2018512319A JP2018532706A5 JP 2018532706 A5 JP2018532706 A5 JP 2018532706A5 JP 2018512319 A JP2018512319 A JP 2018512319A JP 2018512319 A JP2018512319 A JP 2018512319A JP 2018532706 A5 JP2018532706 A5 JP 2018532706A5
- Authority
- JP
- Japan
- Prior art keywords
- disorder
- composition
- sulfur
- nitrogen
- compound according
- 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.)
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- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 53
- 150000001875 compounds Chemical class 0.000 claims description 39
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 36
- 208000035475 disorder Diseases 0.000 claims description 34
- 229910052757 nitrogen Inorganic materials 0.000 claims description 31
- 229910052717 sulfur Chemical group 0.000 claims description 31
- 239000011593 sulfur Chemical group 0.000 claims description 31
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 30
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 28
- 125000005842 heteroatom Chemical group 0.000 claims description 28
- 229910052760 oxygen Inorganic materials 0.000 claims description 28
- 239000001301 oxygen Chemical group 0.000 claims description 28
- 238000000034 method Methods 0.000 claims description 25
- 150000003839 salts Chemical class 0.000 claims description 18
- 229920006395 saturated elastomer Polymers 0.000 claims description 14
- 229910052736 halogen Inorganic materials 0.000 claims description 12
- 150000002367 halogens Chemical class 0.000 claims description 12
- 230000002062 proliferating effect Effects 0.000 claims description 12
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 9
- 125000000623 heterocyclic group Chemical group 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- 208000023275 Autoimmune disease Diseases 0.000 claims description 6
- 208000017701 Endocrine disease Diseases 0.000 claims description 6
- 101000844245 Homo sapiens Non-receptor tyrosine-protein kinase TYK2 Proteins 0.000 claims description 6
- 208000012902 Nervous system disease Diseases 0.000 claims description 6
- 102100032028 Non-receptor tyrosine-protein kinase TYK2 Human genes 0.000 claims description 6
- 125000001931 aliphatic group Chemical group 0.000 claims description 6
- 208000030172 endocrine system disease Diseases 0.000 claims description 6
- 229910052739 hydrogen Inorganic materials 0.000 claims description 6
- 239000001257 hydrogen Substances 0.000 claims description 6
- 208000027866 inflammatory disease Diseases 0.000 claims description 6
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 4
- 208000011231 Crohn disease Diseases 0.000 claims description 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 4
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 4
- 208000030289 Lymphoproliferative disease Diseases 0.000 claims description 4
- 201000004681 Psoriasis Diseases 0.000 claims description 4
- 208000029052 T-cell acute lymphoblastic leukemia Diseases 0.000 claims description 4
- 208000000389 T-cell leukemia Diseases 0.000 claims description 4
- 208000028530 T-cell lymphoblastic leukemia/lymphoma Diseases 0.000 claims description 4
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims description 4
- 201000006704 Ulcerative Colitis Diseases 0.000 claims description 4
- 125000004429 atom Chemical group 0.000 claims description 4
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims description 4
- 208000032839 leukemia Diseases 0.000 claims description 4
- 125000002950 monocyclic group Chemical group 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 238000002054 transplantation Methods 0.000 claims description 4
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 3
- 125000001072 heteroaryl group Chemical group 0.000 claims description 3
- 201000001268 lymphoproliferative syndrome Diseases 0.000 claims description 3
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 2
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 206010073478 Anaplastic large-cell lymphoma Diseases 0.000 claims description 2
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims description 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 2
- 208000009329 Graft vs Host Disease Diseases 0.000 claims description 2
- 102000002227 Interferon Type I Human genes 0.000 claims description 2
- 108010014726 Interferon Type I Proteins 0.000 claims description 2
- 208000032004 Large-Cell Anaplastic Lymphoma Diseases 0.000 claims description 2
- 206010052779 Transplant rejections Diseases 0.000 claims description 2
- 230000003213 activating effect Effects 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 208000006673 asthma Diseases 0.000 claims description 2
- 125000002527 bicyclic carbocyclic group Chemical group 0.000 claims description 2
- 239000012472 biological sample Substances 0.000 claims description 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 208000024908 graft versus host disease Diseases 0.000 claims description 2
- 125000001183 hydrocarbyl group Chemical group 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 208000007282 lymphomatoid papulosis Diseases 0.000 claims description 2
- 230000001404 mediated effect Effects 0.000 claims description 2
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 2
- 125000001620 monocyclic carbocycle group Chemical group 0.000 claims description 2
- 201000006417 multiple sclerosis Diseases 0.000 claims description 2
- 230000035772 mutation Effects 0.000 claims description 2
- 201000010065 polycystic ovary syndrome Diseases 0.000 claims description 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 239000000523 sample Substances 0.000 claims description 2
- 230000011664 signaling Effects 0.000 claims description 2
- 125000003003 spiro group Chemical group 0.000 claims description 2
- 208000011580 syndromic disease Diseases 0.000 claims description 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims description 2
- 239000003981 vehicle Substances 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 22
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000002489 hematologic effect Effects 0.000 claims 1
- -1 hydroxymethyl compound Chemical class 0.000 claims 1
- 0 *C(*)(c1c(*)c(-c2ccccc2)nc(C2=CC=C([*-])C=C*=CC2)c11)NC1=O Chemical compound *C(*)(c1c(*)c(-c2ccccc2)nc(C2=CC=C([*-])C=C*=CC2)c11)NC1=O 0.000 description 4
- 201000005787 hematologic cancer Diseases 0.000 description 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562213475P | 2015-09-02 | 2015-09-02 | |
| US62/213,475 | 2015-09-02 | ||
| US201562214018P | 2015-09-03 | 2015-09-03 | |
| US62/214,018 | 2015-09-03 | ||
| PCT/US2016/049852 WO2017040757A1 (en) | 2015-09-02 | 2016-09-01 | Tyk2 inhibitors and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019109248A Division JP2019172690A (ja) | 2015-09-02 | 2019-06-12 | Ｔｙｋ２阻害剤およびその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018532706A JP2018532706A (ja) | 2018-11-08 |
| JP2018532706A5 true JP2018532706A5 (https=) | 2019-07-18 |
| JP6802263B2 JP6802263B2 (ja) | 2020-12-16 |
Family
ID=58188382
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018512319A Active JP6802263B2 (ja) | 2015-09-02 | 2016-09-01 | Ｔｙｋ２阻害剤およびその使用 |
| JP2019109248A Withdrawn JP2019172690A (ja) | 2015-09-02 | 2019-06-12 | Ｔｙｋ２阻害剤およびその使用 |
| JP2021093678A Pending JP2021130712A (ja) | 2015-09-02 | 2021-06-03 | Ｔｙｋ２阻害剤およびその使用 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019109248A Withdrawn JP2019172690A (ja) | 2015-09-02 | 2019-06-12 | Ｔｙｋ２阻害剤およびその使用 |
| JP2021093678A Pending JP2021130712A (ja) | 2015-09-02 | 2021-06-03 | Ｔｙｋ２阻害剤およびその使用 |
Country Status (5)
| Country | Link |
|---|---|
| US (4) | US10023571B2 (https=) |
| EP (2) | EP3344624B8 (https=) |
| JP (3) | JP6802263B2 (https=) |
| TW (1) | TWI707852B (https=) |
| WO (1) | WO2017040757A1 (https=) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI788655B (zh) | 2015-02-27 | 2023-01-01 | 美商林伯士拉克許米公司 | 酪胺酸蛋白質激酶2(tyk2)抑制劑及其用途 |
| TWI707852B (zh) | 2015-09-02 | 2020-10-21 | 美商林伯士拉克許米公司 | Tyk2 抑制劑及其用途 |
| EP3528816A4 (en) * | 2016-10-21 | 2020-04-08 | Nimbus Lakshmi, Inc. | TYK2 INHIBITORS AND USES THEREOF |
| EP3532466A1 (en) | 2016-10-26 | 2019-09-04 | E-Therapeutics plc | Modulators of hedgehog (hh) signalling pathway |
| US20180153922A1 (en) | 2016-12-06 | 2018-06-07 | New York Society For The Ruptured And Crippled Maintaining The Hospital For Special Surgery | Inhibition of expansion and function of pathogenic age-associated b cells and use for the prevention and treatment of autoimmune disease |
| TW202515876A (zh) | 2017-03-08 | 2025-04-16 | 日商武田藥品工業股份有限公司 | Tyk2抑制劑及其用途 |
| CN107235982B (zh) * | 2017-06-29 | 2019-03-26 | 武汉药明康德新药开发有限公司 | 叔丁基7-羟基-7,8-二氢-4h-吡唑并二氮杂卓5(6h）羧酸酯的合成方法 |
| SI3658557T1 (sl) | 2017-07-28 | 2024-10-30 | Takeda Pharmaceutical Company Limited | Zaviralci TYK2 in njihova uporaba |
| AR117398A1 (es) * | 2018-03-12 | 2021-08-04 | Abbvie Inc | Inhibidores de la señalización mediada por tirosina cinasa 2 |
| CN113271940A (zh) | 2018-10-15 | 2021-08-17 | 林伯士拉克许米公司 | Tyk2抑制剂和其用途 |
| AR117189A1 (es) | 2018-11-02 | 2021-07-21 | Aicuris Gmbh & Co Kg | Derivados de 6,7-dihidro-4h-pirazolo[1,5-a]pirazin indol-2-carboxamidas activos contra el virus de la hepatitis b (vhb) |
| US12479816B2 (en) * | 2019-02-08 | 2025-11-25 | University of Pittsburgh—of the Commonwealth System of Higher Education | 20-HETE formation inhibitors |
| SG11202112043PA (en) | 2019-04-30 | 2021-11-29 | Celgene Corp | Combination therapies comprising apremilast and tyk2 inhibitors |
| CN111116456B (zh) * | 2019-12-26 | 2022-01-28 | 南通华祥医药科技有限公司 | 一种4,4-二氟哌啶盐酸盐的制备方法 |
| CN111053761B (zh) * | 2020-01-16 | 2022-05-03 | 杭州旦承医药科技有限公司 | 一种吸入用双膦酸类药物及其制备方法及其在慢性阻塞性肺疾病的用途 |
| JP7804941B2 (ja) * | 2020-03-24 | 2026-01-23 | 国立大学法人東海国立大学機構 | 遺伝性対側性色素異常症治療用医薬組成物、遺伝性対側性色素異常症モデルマウス、および、遺伝性対側性色素異常症治療用化合物のスクリーニング方法 |
| EP4178958A4 (en) * | 2020-07-10 | 2024-12-11 | Blossomhill Therapeutics, Inc. | MACROCYCLES AND THEIR USE |
| US20230339977A1 (en) * | 2020-08-13 | 2023-10-26 | Sunshine Lake Pharma Co., Ltd. | Substituted heteroaryl compound, and composition and application thereof |
| CN114075220A (zh) * | 2020-08-13 | 2022-02-22 | 广东东阳光药业有限公司 | 取代的杂芳基化合物及其组合物和用途 |
| US20240390369A1 (en) | 2021-09-30 | 2024-11-28 | Bristol-Myers Squibb Company | Methods for determining responsiveness to tyk2 inhibitors |
| EP4423086A1 (en) | 2021-10-25 | 2024-09-04 | Kymera Therapeutics, Inc. | Tyk2 degraders and uses thereof |
| US20250051360A1 (en) * | 2021-12-23 | 2025-02-13 | Sunshine Lake Pharma Co., Ltd. | Substituted heteroaryl compound, and composition and use thereof |
| AU2023204770A1 (en) * | 2022-01-05 | 2024-07-18 | Blossomhill Therapeutics, Inc. | Macrocyclic compounds and use as kinase inhibitors |
| CN114674813B (zh) * | 2022-03-21 | 2025-02-07 | 同济大学 | 一种利用芳基丙酸类药物半定量检测硫酸根自由基的方法 |
| CN117886669A (zh) * | 2024-01-10 | 2024-04-16 | 中国农业大学 | 一种将酰氯还原氘化为氘代醇的方法 |
| CN118955546A (zh) * | 2024-07-31 | 2024-11-15 | 上海毕得医药科技股份有限公司 | 一种化合物1-异丙基吡唑-3-硼酸频哪醇酯的合成方法 |
Family Cites Families (47)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US5516931A (en) | 1982-02-01 | 1996-05-14 | Northeastern University | Release tag compounds producing ketone signal groups |
| US5650270A (en) | 1982-02-01 | 1997-07-22 | Northeastern University | Molecular analytical release tags and their use in chemical analysis |
| US4709016A (en) | 1982-02-01 | 1987-11-24 | Northeastern University | Molecular analytical release tags and their use in chemical analysis |
| US4650750A (en) | 1982-02-01 | 1987-03-17 | Giese Roger W | Method of chemical analysis employing molecular release tag compounds |
| JPS63107966A (ja) * | 1986-05-22 | 1988-05-12 | Fujisawa Pharmaceut Co Ltd | ピリミジン誘導体 |
| DE4430639A1 (de) * | 1994-08-29 | 1996-03-07 | Bayer Ag | Verwendung von 5-substituierten Pyridin- und Hexahydrochinolin-3-carbonsäurederivaten |
| DE60037345T2 (de) | 1999-12-10 | 2008-11-13 | Pfizer Products Inc., Groton | Pyrrolo(2,3-d)pyrimidin-Verbindungen |
| PE20020354A1 (es) | 2000-09-01 | 2002-06-12 | Novartis Ag | Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda) |
| DE60217322T2 (de) | 2001-04-27 | 2007-10-04 | Zenyaku Kogyo K.K. | Heterocyclische verbindung und antitumormittel, das diese als wirkstoff enthält |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| PT1536827E (pt) | 2002-08-14 | 2009-03-20 | Silence Therapeutics Ag | Utilização de proteína cinase n beta |
| AU2004228668B2 (en) | 2003-04-03 | 2011-10-27 | Park Funding, Llc | PI-3 kinase inhibitor prodrugs |
| ES2382377T3 (es) | 2003-05-30 | 2012-06-07 | Gemin X Pharmaceuticals Canada Inc. | Compuestos triheterocíclicos, composiciones, y métodos para tratar cáncer |
| EP1692153A4 (en) | 2003-07-03 | 2007-03-21 | Univ Pennsylvania | INHIBITION OF EXPRESSION OF SYK-KINASE |
| WO2005025504A2 (en) * | 2003-09-12 | 2005-03-24 | Kemia, Inc. | Modulators of calcitonin and amylin activity |
| WO2005113556A1 (en) | 2004-05-13 | 2005-12-01 | Icos Corporation | Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta |
| AU2006206458B2 (en) | 2005-01-19 | 2012-10-25 | Rigel Pharmaceuticals, Inc. | Prodrugs of 2,4-pyrimidinediamine compounds and their uses |
| PL1888550T3 (pl) | 2005-05-12 | 2014-12-31 | Abbvie Bahamas Ltd | Promotory apoptozy |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| US7521557B2 (en) * | 2005-05-20 | 2009-04-21 | Bristol-Myers Squibb Company | Pyrrolopyridine-based inhibitors of dipeptidyl peptidase IV and methods |
| US7402325B2 (en) | 2005-07-28 | 2008-07-22 | Phoenix Biotechnology, Inc. | Supercritical carbon dioxide extract of pharmacologically active components from Nerium oleander |
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| JPWO2008047831A1 (ja) * | 2006-10-17 | 2010-02-25 | 協和発酵キリン株式会社 | Ｊａｋ阻害剤 |
| KR101566840B1 (ko) | 2007-03-12 | 2015-11-06 | 와이엠 바이오사이언시즈 오스트레일리아 피티와이 엘티디 | 페닐 아미노 피리미딘 화합물 및 이의 용도 |
| WO2008118802A1 (en) | 2007-03-23 | 2008-10-02 | Regents Of The University Of Minnesota | Therapeutic compounds |
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| EP2211620B1 (en) * | 2007-10-25 | 2013-12-25 | Merck Sharp & Dohme Corp. | 3-PYRAZIN SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AS JANUS KINASE INHIBITORS FOR THE TREATMENT OF CANCER DISEASES |
| HUE029767T2 (en) | 2008-03-11 | 2017-04-28 | Incyte Holdings Corp | JAK inhibitor azetidine and cyclobutane derivatives |
| EP2299816B1 (en) * | 2008-06-18 | 2013-11-13 | Merck Sharp & Dohme Corp. | Inhibitors of janus kinases |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| NZ601267A (en) * | 2009-12-23 | 2014-03-28 | Takeda Pharmaceutical | Fused heteroaromatic pyrrolidinones as syk inhibitors |
| AU2014308991B2 (en) * | 2013-08-21 | 2019-02-14 | Janssen Biopharma, Inc. | Antiviral compounds |
| WO2015131080A1 (en) | 2014-02-28 | 2015-09-03 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
| TWI788655B (zh) | 2015-02-27 | 2023-01-01 | 美商林伯士拉克許米公司 | 酪胺酸蛋白質激酶2(tyk2)抑制劑及其用途 |
| TWI707852B (zh) | 2015-09-02 | 2020-10-21 | 美商林伯士拉克許米公司 | Tyk2 抑制劑及其用途 |
| US10323036B2 (en) | 2016-10-14 | 2019-06-18 | Nimbus Lakshmi, Inc. | TYK2 inhibitors and uses thereof |
| EP3528816A4 (en) | 2016-10-21 | 2020-04-08 | Nimbus Lakshmi, Inc. | TYK2 INHIBITORS AND USES THEREOF |
| TW202515876A (zh) | 2017-03-08 | 2025-04-16 | 日商武田藥品工業股份有限公司 | Tyk2抑制劑及其用途 |
| SI3658557T1 (sl) | 2017-07-28 | 2024-10-30 | Takeda Pharmaceutical Company Limited | Zaviralci TYK2 in njihova uporaba |
| CN113271940A (zh) | 2018-10-15 | 2021-08-17 | 林伯士拉克许米公司 | Tyk2抑制剂和其用途 |
| CA3120866A1 (en) | 2018-11-30 | 2020-06-04 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
| CN113348021B (zh) | 2019-01-23 | 2025-07-11 | 武田药品工业株式会社 | Tyk2抑制剂和其用途 |
-
2016
- 2016-09-01 TW TW105128290A patent/TWI707852B/zh active
- 2016-09-01 EP EP16842967.8A patent/EP3344624B8/en active Active
- 2016-09-01 JP JP2018512319A patent/JP6802263B2/ja active Active
- 2016-09-01 EP EP23205337.1A patent/EP4327809A3/en active Pending
- 2016-09-01 WO PCT/US2016/049852 patent/WO2017040757A1/en not_active Ceased
- 2016-09-01 US US15/254,071 patent/US10023571B2/en active Active
-
2018
- 2018-06-13 US US16/007,099 patent/US10781204B2/en active Active
-
2019
- 2019-06-12 JP JP2019109248A patent/JP2019172690A/ja not_active Withdrawn
-
2020
- 2020-07-24 US US16/938,522 patent/US11434240B2/en active Active
-
2021
- 2021-06-03 JP JP2021093678A patent/JP2021130712A/ja active Pending
-
2022
- 2022-07-20 US US17/813,805 patent/US20230074228A1/en not_active Abandoned
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