JPWO2020102100A5 - - Google Patents
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- JPWO2020102100A5 JPWO2020102100A5 JP2021525010A JP2021525010A JPWO2020102100A5 JP WO2020102100 A5 JPWO2020102100 A5 JP WO2020102100A5 JP 2021525010 A JP2021525010 A JP 2021525010A JP 2021525010 A JP2021525010 A JP 2021525010A JP WO2020102100 A5 JPWO2020102100 A5 JP WO2020102100A5
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- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- independently selected
- ring
- compound
- 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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- 125000000217 alkyl group Chemical group 0.000 claims description 243
- 150000001875 compounds Chemical class 0.000 claims description 236
- 125000003118 aryl group Chemical group 0.000 claims description 184
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 125
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 121
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 93
- 125000005843 halogen group Chemical group 0.000 claims description 87
- 125000003545 alkoxy group Chemical group 0.000 claims description 69
- 125000006413 ring segment Chemical group 0.000 claims description 62
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 60
- 125000001424 substituent group Chemical group 0.000 claims description 56
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims description 52
- ONIKNECPXCLUHT-UHFFFAOYSA-N 2-chlorobenzoyl chloride Chemical compound ClC(=O)C1=CC=CC=C1Cl ONIKNECPXCLUHT-UHFFFAOYSA-N 0.000 claims description 44
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 43
- 229910052757 nitrogen Inorganic materials 0.000 claims description 39
- 229910052760 oxygen Inorganic materials 0.000 claims description 34
- 229910052717 sulfur Inorganic materials 0.000 claims description 32
- 201000010099 disease Diseases 0.000 claims description 26
- 125000001072 heteroaryl group Chemical group 0.000 claims description 26
- 125000006584 (C3-C10) heterocycloalkyl group Chemical group 0.000 claims description 25
- 125000000623 heterocyclic group Chemical group 0.000 claims description 25
- 125000000304 alkynyl group Chemical group 0.000 claims description 21
- 229910052739 hydrogen Inorganic materials 0.000 claims description 21
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims description 21
- 239000008194 pharmaceutical composition Substances 0.000 claims description 19
- -1 C 1 -C 6 alkoxy Chemical group 0.000 claims description 17
- 208000035475 disorder Diseases 0.000 claims description 17
- 125000004043 oxo group Chemical group O=* 0.000 claims description 16
- 239000001257 hydrogen Substances 0.000 claims description 15
- 206010028980 Neoplasm Diseases 0.000 claims description 14
- 201000011510 cancer Diseases 0.000 claims description 14
- 125000002837 carbocyclic group Chemical group 0.000 claims description 14
- 102000000874 Pyrin Domain-Containing 3 Protein NLR Family Human genes 0.000 claims description 12
- 108010001946 Pyrin Domain-Containing 3 Protein NLR Family Proteins 0.000 claims description 12
- 125000005842 heteroatom Chemical group 0.000 claims description 12
- 150000003839 salts Chemical class 0.000 claims description 12
- 125000004432 carbon atom Chemical group C* 0.000 claims description 11
- 229910052799 carbon Inorganic materials 0.000 claims description 10
- 150000002431 hydrogen Chemical class 0.000 claims description 9
- 125000002950 monocyclic group Chemical group 0.000 claims description 9
- 229940046728 tumor necrosis factor alpha inhibitor Drugs 0.000 claims description 9
- 239000002452 tumor necrosis factor alpha inhibitor Substances 0.000 claims description 9
- 125000002619 bicyclic group Chemical group 0.000 claims description 8
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 6
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 6
- 229920006395 saturated elastomer Polymers 0.000 claims description 6
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims description 5
- 201000005099 Langerhans cell histiocytosis Diseases 0.000 claims description 5
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims description 5
- 208000023275 Autoimmune disease Diseases 0.000 claims description 4
- 208000019693 Lung disease Diseases 0.000 claims description 4
- 208000023178 Musculoskeletal disease Diseases 0.000 claims description 4
- 208000016222 Pancreatic disease Diseases 0.000 claims description 4
- 208000036142 Viral infection Diseases 0.000 claims description 4
- 208000015114 central nervous system disease Diseases 0.000 claims description 4
- 208000028774 intestinal disease Diseases 0.000 claims description 4
- 208000017169 kidney disease Diseases 0.000 claims description 4
- 208000019423 liver disease Diseases 0.000 claims description 4
- 208000030159 metabolic disease Diseases 0.000 claims description 4
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 4
- 208000017520 skin disease Diseases 0.000 claims description 4
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 4
- 208000019553 vascular disease Diseases 0.000 claims description 4
- 230000009385 viral infection Effects 0.000 claims description 4
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims description 3
- 208000036762 Acute promyelocytic leukaemia Diseases 0.000 claims description 3
- 208000020084 Bone disease Diseases 0.000 claims description 3
- 208000034578 Multiple myelomas Diseases 0.000 claims description 3
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 3
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims description 3
- 208000030533 eye disease Diseases 0.000 claims description 3
- 208000030507 AIDS Diseases 0.000 claims description 2
- 208000009304 Acute Kidney Injury Diseases 0.000 claims description 2
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 201000001320 Atherosclerosis Diseases 0.000 claims description 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 2
- 208000000668 Chronic Pancreatitis Diseases 0.000 claims description 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 2
- 208000011231 Crohn disease Diseases 0.000 claims description 2
- 206010016654 Fibrosis Diseases 0.000 claims description 2
- 208000007465 Giant cell arteritis Diseases 0.000 claims description 2
- 208000010412 Glaucoma Diseases 0.000 claims description 2
- 201000005569 Gout Diseases 0.000 claims description 2
- 208000030836 Hashimoto thyroiditis Diseases 0.000 claims description 2
- 206010019799 Hepatitis viral Diseases 0.000 claims description 2
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 206010027476 Metastases Diseases 0.000 claims description 2
- 208000008589 Obesity Diseases 0.000 claims description 2
- 208000001132 Osteoporosis Diseases 0.000 claims description 2
- 206010033645 Pancreatitis Diseases 0.000 claims description 2
- 206010033647 Pancreatitis acute Diseases 0.000 claims description 2
- 206010033649 Pancreatitis chronic Diseases 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 201000004681 Psoriasis Diseases 0.000 claims description 2
- 206010061481 Renal injury Diseases 0.000 claims description 2
- 206010039710 Scleroderma Diseases 0.000 claims description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims description 2
- 201000003229 acute pancreatitis Diseases 0.000 claims description 2
- 230000032683 aging Effects 0.000 claims description 2
- 125000002947 alkylene group Chemical group 0.000 claims description 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 2
- 125000004104 aryloxy group Chemical group 0.000 claims description 2
- 208000006673 asthma Diseases 0.000 claims description 2
- 230000001684 chronic effect Effects 0.000 claims description 2
- 230000007882 cirrhosis Effects 0.000 claims description 2
- 208000019425 cirrhosis of liver Diseases 0.000 claims description 2
- 239000002552 dosage form Substances 0.000 claims description 2
- 206010017758 gastric cancer Diseases 0.000 claims description 2
- 239000003862 glucocorticoid Substances 0.000 claims description 2
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 208000002780 macular degeneration Diseases 0.000 claims description 2
- 230000009401 metastasis Effects 0.000 claims description 2
- 201000006417 multiple sclerosis Diseases 0.000 claims description 2
- 230000035772 mutation Effects 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims description 2
- 235000020824 obesity Nutrition 0.000 claims description 2
- 201000008482 osteoarthritis Diseases 0.000 claims description 2
- 208000002865 osteopetrosis Diseases 0.000 claims description 2
- 230000002018 overexpression Effects 0.000 claims description 2
- 230000007170 pathology Effects 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 230000011664 signaling Effects 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- 208000024891 symptom Diseases 0.000 claims description 2
- 208000011580 syndromic disease Diseases 0.000 claims description 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims description 2
- 206010043207 temporal arteritis Diseases 0.000 claims description 2
- 238000002560 therapeutic procedure Methods 0.000 claims description 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 2
- 201000001862 viral hepatitis Diseases 0.000 claims description 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 5
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 4
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 1
- 125000005330 8 membered heterocyclic group Chemical group 0.000 claims 1
- 101001043818 Mus musculus Interleukin-31 receptor subunit alpha Proteins 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 238000000034 method Methods 0.000 description 63
- 125000001188 haloalkyl group Chemical group 0.000 description 33
- 125000004429 atom Chemical group 0.000 description 26
- 125000004438 haloalkoxy group Chemical group 0.000 description 16
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 14
- 125000003342 alkenyl group Chemical group 0.000 description 11
- 125000002373 5 membered heterocyclic group Chemical group 0.000 description 6
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 5
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 description 5
- 125000001153 fluoro group Chemical group F* 0.000 description 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 5
- 239000005557 antagonist Substances 0.000 description 4
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 description 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 description 1
- 208000022873 Ocular disease Diseases 0.000 description 1
- 208000033626 Renal failure acute Diseases 0.000 description 1
- 201000011040 acute kidney failure Diseases 0.000 description 1
- 230000003042 antagnostic effect Effects 0.000 description 1
- 210000000988 bone and bone Anatomy 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 208000037806 kidney injury Diseases 0.000 description 1
- 208000017445 musculoskeletal system disease Diseases 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
Applications Claiming Priority (13)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862760244P | 2018-11-13 | 2018-11-13 | |
| US201862760248P | 2018-11-13 | 2018-11-13 | |
| US201862760279P | 2018-11-13 | 2018-11-13 | |
| US62/760,248 | 2018-11-13 | ||
| US62/760,279 | 2018-11-13 | ||
| US62/760,244 | 2018-11-13 | ||
| US201962795373P | 2019-01-22 | 2019-01-22 | |
| US62/795,373 | 2019-01-22 | ||
| US201962796361P | 2019-01-24 | 2019-01-24 | |
| US201962796356P | 2019-01-24 | 2019-01-24 | |
| US62/796,361 | 2019-01-24 | ||
| US62/796,356 | 2019-01-24 | ||
| PCT/US2019/060775 WO2020102100A1 (en) | 2018-11-13 | 2019-11-11 | Compounds and compositions for treating conditions associated with nlrp activity |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022506898A JP2022506898A (ja) | 2022-01-17 |
| JPWO2020102100A5 true JPWO2020102100A5 (https=) | 2022-11-21 |
| JP2022506898A5 JP2022506898A5 (https=) | 2022-11-21 |
Family
ID=68916531
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021525010A Pending JP2022506898A (ja) | 2018-11-13 | 2019-11-11 | Ｎｌｒｐ活性に関連する状態を処置するための化合物及び組成物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US12134611B2 (https=) |
| EP (1) | EP3880666B1 (https=) |
| JP (1) | JP2022506898A (https=) |
| CN (1) | CN113166081A (https=) |
| ES (1) | ES2957692T3 (https=) |
| WO (1) | WO2020102100A1 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3649112A1 (en) * | 2017-07-07 | 2020-05-13 | Inflazome Limited | Sulfonylureas and sulfonylthioureas as nlrp3 inhibitors |
| CA3105521A1 (en) | 2018-07-20 | 2020-01-23 | F. Hoffmann-La Roche Ag | Sulfonimidamide compounds as inhibitors of interleukin-1 activity |
| EP3986879B1 (en) * | 2019-06-21 | 2024-10-02 | AC Immune SA | Fused 1,2-thiazoles and 1,2-thiazines which act as nlrp3 modulators |
| US11932630B2 (en) | 2021-04-16 | 2024-03-19 | Novartis Ag | Heteroaryl aminopropanol derivatives |
| CN117185965B (zh) * | 2023-09-18 | 2024-10-11 | 安徽金桐精细化学有限公司 | 一种磺酸基丙烯酸盐复配表面活性剂的制备方法 |
| WO2025153532A1 (en) | 2024-01-16 | 2025-07-24 | NodThera Limited | Nlrp3 inhibitors and glp-1 agonists combination therapies |
| WO2026064385A1 (en) * | 2024-09-18 | 2026-03-26 | Ventus Therapeutics U.S., Inc. | Oxadiazolone inhibitors of nlrp3 and uses thereof |
| CN119775202A (zh) * | 2024-12-31 | 2025-04-08 | 河南旭瑞新材料科技有限公司 | 一种2-巯基烟酰甘氨酸的合成方法 |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4987071A (en) | 1986-12-03 | 1991-01-22 | University Patents, Inc. | RNA ribozyme polymerases, dephosphorylases, restriction endoribonucleases and methods |
| US5116742A (en) | 1986-12-03 | 1992-05-26 | University Patents, Inc. | RNA ribozyme restriction endoribonucleases and methods |
| AU630497B2 (en) | 1989-09-05 | 1992-10-29 | Immunex Corporation | Tumor necrosis factor-alpha and -beta receptors |
| ZA929699B (en) | 1991-12-20 | 1994-06-14 | Lilly Co Eli | Sulfonimidamides |
| US5705398A (en) | 1994-03-02 | 1998-01-06 | The Scripps Research Institute | Methods for identifying inhibitors of LPS-mediated LBP binding |
| US6090382A (en) | 1996-02-09 | 2000-07-18 | Basf Aktiengesellschaft | Human antibodies that bind human TNFα |
| DK0929578T3 (da) | 1996-02-09 | 2003-08-25 | Abbott Lab Bermuda Ltd | Humane antistoffer, der binder human TNFalfa |
| CA2329065A1 (en) | 1998-05-05 | 1999-11-11 | Francisco Xavier Talamas | Pyrazole derivatives as p-38 map kinase inhibitors |
| KR101120857B1 (ko) | 2003-06-26 | 2012-04-12 | 노파르티스 아게 | 5원의 헤테로사이클-기재 ｐ38 키나제 억제제 |
| US20080280910A1 (en) | 2007-03-22 | 2008-11-13 | Keith Allan Menear | Phthalazinone derivatives |
| US8884006B2 (en) | 2011-09-19 | 2014-11-11 | University Of Puerto Rico | Small-molecule inhibitors of Rac1 in metastatic breast cancer |
| ITMI20131658A1 (it) | 2013-10-08 | 2015-04-09 | Getters Spa | Combinazione di materiali per dispositivi di rilascio di mercurio e dispositivi contenenti detta combinazione di materiali |
| US9714288B2 (en) | 2014-09-30 | 2017-07-25 | The Regents Of The University Of California | Antisense compounds and uses thereof |
| SI3259253T1 (sl) * | 2015-02-16 | 2020-07-31 | The University Of Queensland | Sulfonilsečnine in sorodne spojine ter njihova uporaba |
| US11447460B2 (en) * | 2016-04-18 | 2022-09-20 | Novartis Ag | Compounds and compositions for treating conditions associated with NLRP activity |
| US11339136B2 (en) | 2016-04-18 | 2022-05-24 | Novartis Ag | Compounds and compositions for treating conditions associated with NLRP activity |
| CA3021349A1 (en) | 2016-04-19 | 2017-10-26 | Innate Tumor Immunity, Inc. | Nlrp3 modulators |
| JP6962941B2 (ja) | 2016-06-14 | 2021-11-05 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | Ａｐｊ受容体アゴニストとしての４−ヒドロキシ−３−スルホニルピリジン−２（１ｈ）−オン |
| EP3571187B1 (en) | 2017-01-23 | 2023-11-22 | Genentech, Inc. | Chemical compounds as inhibitors of interleukin-1 activity |
| WO2018225018A1 (en) | 2017-06-09 | 2018-12-13 | Cadila Healthcare Limited | Novel substituted sulfoximine compounds |
| JP7349981B2 (ja) * | 2017-07-24 | 2023-09-25 | ノバルティス アーゲー | Ｎｌｒｐ活性に関連する状態を治療するための化合物及び組成物 |
| ES2988798T3 (es) | 2017-07-24 | 2024-11-21 | Novartis Ag | Compuestos y composiciones para el tratamiento de afecciones asociadas a la actividad de NLRP |
| EP3668840A1 (en) | 2017-08-15 | 2020-06-24 | Inflazome Limited | Novel sulfonamide carboxamide compounds |
| CA3105521A1 (en) | 2018-07-20 | 2020-01-23 | F. Hoffmann-La Roche Ag | Sulfonimidamide compounds as inhibitors of interleukin-1 activity |
| GB201902327D0 (en) | 2019-02-20 | 2019-04-03 | Inflazome Ltd | Novel compounds |
| BR112021003665A2 (pt) | 2018-09-13 | 2021-05-18 | Bayer Aktiengesellschaft | derivados de heterocicleno como agentes de controle de pragas |
| EP3911323A4 (en) | 2019-01-18 | 2022-11-16 | Nuvation Bio Inc. | HETEROCYCLIC COMPOUNDS AS ADENOSINE ANTAGONISTS |
| EP3986879B1 (en) | 2019-06-21 | 2024-10-02 | AC Immune SA | Fused 1,2-thiazoles and 1,2-thiazines which act as nlrp3 modulators |
-
2019
- 2019-11-11 US US17/292,887 patent/US12134611B2/en active Active
- 2019-11-11 CN CN201980078239.1A patent/CN113166081A/zh active Pending
- 2019-11-11 WO PCT/US2019/060775 patent/WO2020102100A1/en not_active Ceased
- 2019-11-11 ES ES19821320T patent/ES2957692T3/es active Active
- 2019-11-11 EP EP19821320.9A patent/EP3880666B1/en active Active
- 2019-11-11 JP JP2021525010A patent/JP2022506898A/ja active Pending
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