JP2017506675A5 - - Google Patents
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- JP2017506675A5 JP2017506675A5 JP2016572363A JP2016572363A JP2017506675A5 JP 2017506675 A5 JP2017506675 A5 JP 2017506675A5 JP 2016572363 A JP2016572363 A JP 2016572363A JP 2016572363 A JP2016572363 A JP 2016572363A JP 2017506675 A5 JP2017506675 A5 JP 2017506675A5
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- Prior art keywords
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- pharmaceutically acceptable
- acceptable salt
- pharmaceutical composition
- compound
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- 150000001875 compounds Chemical class 0.000 claims description 47
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 42
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 38
- 208000035475 disorder Diseases 0.000 claims description 34
- 150000003839 salts Chemical class 0.000 claims description 32
- 229910052757 nitrogen Inorganic materials 0.000 claims description 28
- 125000005842 heteroatom Chemical group 0.000 claims description 26
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 24
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 24
- 229910052760 oxygen Inorganic materials 0.000 claims description 24
- 239000001301 oxygen Chemical group 0.000 claims description 24
- 238000000034 method Methods 0.000 claims description 22
- 239000008194 pharmaceutical composition Substances 0.000 claims description 22
- 229910052717 sulfur Chemical group 0.000 claims description 22
- 239000011593 sulfur Chemical group 0.000 claims description 22
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 18
- 229920006395 saturated elastomer Polymers 0.000 claims description 18
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 14
- 229910052739 hydrogen Inorganic materials 0.000 claims description 12
- 239000001257 hydrogen Substances 0.000 claims description 12
- 229910052736 halogen Inorganic materials 0.000 claims description 10
- 150000002367 halogens Chemical class 0.000 claims description 10
- 125000000623 heterocyclic group Chemical group 0.000 claims description 10
- 230000002062 proliferating effect Effects 0.000 claims description 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 9
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 8
- 101000844245 Homo sapiens Non-receptor tyrosine-protein kinase TYK2 Proteins 0.000 claims description 7
- 102100032028 Non-receptor tyrosine-protein kinase TYK2 Human genes 0.000 claims description 7
- 208000023275 Autoimmune disease Diseases 0.000 claims description 6
- 208000017701 Endocrine disease Diseases 0.000 claims description 6
- 208000012902 Nervous system disease Diseases 0.000 claims description 6
- 125000001931 aliphatic group Chemical group 0.000 claims description 6
- 125000000217 alkyl group Chemical group 0.000 claims description 6
- 208000030172 endocrine system disease Diseases 0.000 claims description 6
- 208000027866 inflammatory disease Diseases 0.000 claims description 6
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 6
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 4
- 208000011231 Crohn disease Diseases 0.000 claims description 4
- 208000022559 Inflammatory bowel 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
- 125000002837 carbocyclic group Chemical group 0.000 claims description 4
- 201000010099 disease Diseases 0.000 claims description 4
- 208000032839 leukemia Diseases 0.000 claims description 4
- 125000003386 piperidinyl group Chemical group 0.000 claims description 4
- 150000002431 hydrogen Chemical group 0.000 claims description 3
- 238000002054 transplantation Methods 0.000 claims description 3
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims description 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims description 2
- 208000024827 Alzheimer disease 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
- 206010028980 Neoplasm 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
- 125000003118 aryl group Chemical group 0.000 claims description 2
- 208000006673 asthma Diseases 0.000 claims description 2
- 239000012472 biological sample Substances 0.000 claims description 2
- 201000011510 cancer 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
- 230000002489 hematologic effect Effects 0.000 claims description 2
- 125000001072 heteroaryl group Chemical group 0.000 claims description 2
- 125000001183 hydrocarbyl group Chemical group 0.000 claims description 2
- 230000002401 inhibitory effect Effects 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
- 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
- -1 pyrazol-4-yl 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
- 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
- 230000019491 signal transduction Effects 0.000 description 2
- 102000004127 Cytokines Human genes 0.000 description 1
- 108090000695 Cytokines Proteins 0.000 description 1
- 102000001253 Protein Kinase Human genes 0.000 description 1
- 108010010057 TYK2 Kinase Proteins 0.000 description 1
- 102000015774 TYK2 Kinase Human genes 0.000 description 1
- 229940123371 Tyrosine kinase 2 inhibitor Drugs 0.000 description 1
- 238000010835 comparative analysis Methods 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 230000031146 intracellular signal transduction Effects 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 108060006633 protein kinase Proteins 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461946358P | 2014-02-28 | 2014-02-28 | |
| US61/946,358 | 2014-02-28 | ||
| US201461971376P | 2014-03-27 | 2014-03-27 | |
| US61/971,376 | 2014-03-27 | ||
| US201462096231P | 2014-12-23 | 2014-12-23 | |
| US62/096,231 | 2014-12-23 | ||
| PCT/US2015/018071 WO2015131080A1 (en) | 2014-02-28 | 2015-02-27 | Tyk2 inhibitors and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018227179A Division JP2019048885A (ja) | 2014-02-28 | 2018-12-04 | Ｔｙｋ２阻害剤およびその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017506675A JP2017506675A (ja) | 2017-03-09 |
| JP2017506675A5 true JP2017506675A5 (cg-RX-API-DMAC7.html) | 2018-03-15 |
| JP6526065B2 JP6526065B2 (ja) | 2019-06-05 |
Family
ID=54009662
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016572363A Active JP6526065B2 (ja) | 2014-02-28 | 2015-02-27 | Ｔｙｋ２阻害剤およびその使用 |
| JP2018227179A Withdrawn JP2019048885A (ja) | 2014-02-28 | 2018-12-04 | Ｔｙｋ２阻害剤およびその使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018227179A Withdrawn JP2019048885A (ja) | 2014-02-28 | 2018-12-04 | Ｔｙｋ２阻害剤およびその使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (3) | US9340540B2 (cg-RX-API-DMAC7.html) |
| EP (2) | EP3110820B1 (cg-RX-API-DMAC7.html) |
| JP (2) | JP6526065B2 (cg-RX-API-DMAC7.html) |
| CN (1) | CN106661039B (cg-RX-API-DMAC7.html) |
| AU (1) | AU2015222865B2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2940666C (cg-RX-API-DMAC7.html) |
| ES (1) | ES2921874T3 (cg-RX-API-DMAC7.html) |
| TW (2) | TWI701245B (cg-RX-API-DMAC7.html) |
| WO (1) | WO2015131080A1 (cg-RX-API-DMAC7.html) |
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| 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 |
| WO2017040757A1 (en) * | 2015-09-02 | 2017-03-09 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
| CN109952303B (zh) * | 2016-10-14 | 2022-10-21 | 林伯士拉克许米公司 | Tyk2抑制剂及其用途 |
| US10647713B2 (en) * | 2016-10-21 | 2020-05-12 | Nimbus Lakshmi, Inc. | TYK2 inhibitors and uses thereof |
| WO2018165240A1 (en) * | 2017-03-08 | 2018-09-13 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors, uses, and methods for production thereof |
| US11419883B2 (en) | 2017-05-05 | 2022-08-23 | The Regents Of The University Of California | Inhibiting senescent processes in beta cells for the prevention of type 1 diabetes |
| EP3658557B1 (en) | 2017-07-28 | 2024-06-05 | Takeda Pharmaceutical Company Limited | Tyk2 inhibitors and uses thereof |
| BR112020002265A2 (pt) * | 2017-08-01 | 2020-07-28 | Theravance Biopharma R&D Ip, Llc | compostos pirazólicos e triazólicos bicíclicos como inibidores de jak quiinase |
| EP3689871B1 (en) * | 2017-09-28 | 2021-09-29 | Shanghai Haiyan Pharmaceutical Technology Co., Ltd. | 4,6,7-trisubstituted 1,2-dihydropyrrol[3,4-c]pyridin/pyrimidin-3-one derivative and use |
| KR20190043437A (ko) | 2017-10-18 | 2019-04-26 | 씨제이헬스케어 주식회사 | 단백질 키나제 억제제로서의 헤테로고리 화합물 |
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| US12486320B1 (en) * | 2018-01-15 | 2025-12-02 | Washington University | Compositions and methods for treatment of central nervous system (CNS) autoimmune associated diseases or disorders |
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| TW202112767A (zh) | 2019-06-17 | 2021-04-01 | 美商佩特拉製藥公司 | 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物 |
| BR112022004451A2 (pt) | 2019-09-13 | 2022-06-21 | Nimbus Saturn Inc | Antagonistas de hpk1 e usos dos mesmos |
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| WO2022053931A1 (en) * | 2020-09-08 | 2022-03-17 | Galderma Holding SA | Novel jak inhibitor compounds, method for synthesizing same and use thereof |
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-
2015
- 2015-02-27 CN CN201580021113.2A patent/CN106661039B/zh active Active
- 2015-02-27 CA CA2940666A patent/CA2940666C/en active Active
- 2015-02-27 EP EP15755242.3A patent/EP3110820B1/en active Active
- 2015-02-27 AU AU2015222865A patent/AU2015222865B2/en active Active
- 2015-02-27 JP JP2016572363A patent/JP6526065B2/ja active Active
- 2015-02-27 ES ES15755242T patent/ES2921874T3/es active Active
- 2015-02-27 US US14/634,041 patent/US9340540B2/en active Active
- 2015-02-27 EP EP22153229.4A patent/EP4019518A1/en active Pending
- 2015-02-27 WO PCT/US2015/018071 patent/WO2015131080A1/en not_active Ceased
- 2015-03-02 TW TW104106745A patent/TWI701245B/zh active
- 2015-03-02 TW TW108106527A patent/TWI754794B/zh active
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2016
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2017
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2018
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