JP2020537657A5 - - Google Patents
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- JP2020537657A5 JP2020537657A5 JP2020521522A JP2020521522A JP2020537657A5 JP 2020537657 A5 JP2020537657 A5 JP 2020537657A5 JP 2020521522 A JP2020521522 A JP 2020521522A JP 2020521522 A JP2020521522 A JP 2020521522A JP 2020537657 A5 JP2020537657 A5 JP 2020537657A5
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- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- alkoxy
- membered
- substituted
- 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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- 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 claims description 878
- 125000000217 alkyl group Chemical group 0.000 claims description 442
- 125000003118 aryl group Chemical group 0.000 claims description 227
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 179
- 125000003545 alkoxy group Chemical group 0.000 claims description 145
- 150000001875 compounds Chemical class 0.000 claims description 141
- 125000005843 halogen group Chemical group 0.000 claims description 134
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 124
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 108
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 104
- 125000002950 monocyclic group Chemical group 0.000 claims description 98
- 125000001424 substituent group Chemical group 0.000 claims description 91
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims description 70
- 125000004043 oxo group Chemical group O=* 0.000 claims description 68
- 229910005965 SO 2 Inorganic materials 0.000 claims description 61
- ONIKNECPXCLUHT-UHFFFAOYSA-N 2-chlorobenzoyl chloride Chemical compound ClC(=O)C1=CC=CC=C1Cl ONIKNECPXCLUHT-UHFFFAOYSA-N 0.000 claims description 60
- 125000005842 heteroatom Chemical group 0.000 claims description 48
- 229910052739 hydrogen Inorganic materials 0.000 claims description 47
- 229910052717 sulfur Inorganic materials 0.000 claims description 46
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 42
- 125000000623 heterocyclic group Chemical group 0.000 claims description 42
- 229910052757 nitrogen Inorganic materials 0.000 claims description 42
- 125000001072 heteroaryl group Chemical group 0.000 claims description 39
- 229910052760 oxygen Inorganic materials 0.000 claims description 36
- 239000001257 hydrogen Substances 0.000 claims description 35
- -1 C 1 to C 6 alkyl Chemical group 0.000 claims description 34
- 125000004429 atom Chemical group 0.000 claims description 31
- 125000004104 aryloxy group Chemical group 0.000 claims description 27
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 25
- 229910052799 carbon Inorganic materials 0.000 claims description 22
- 201000010099 disease Diseases 0.000 claims description 22
- 239000008194 pharmaceutical composition Substances 0.000 claims description 22
- 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
- 125000002619 bicyclic group Chemical group 0.000 claims description 20
- 150000002431 hydrogen Chemical class 0.000 claims description 20
- 230000001575 pathological effect Effects 0.000 claims description 18
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 17
- 208000035475 disorder Diseases 0.000 claims description 17
- 125000006580 bicyclic heterocycloalkyl group Chemical group 0.000 claims description 15
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 14
- 125000006584 (C3-C10) heterocycloalkyl group Chemical group 0.000 claims description 11
- 108010001946 Pyrin Domain-Containing 3 Protein NLR Family Proteins 0.000 claims description 11
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 8
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 8
- 239000001301 oxygen Substances 0.000 claims description 8
- 239000011593 sulfur Chemical group 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 7
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims description 6
- 229940046728 tumor necrosis factor alpha inhibitor Drugs 0.000 claims description 6
- 239000002452 tumor necrosis factor alpha inhibitor Substances 0.000 claims description 6
- 230000007170 pathology Effects 0.000 claims description 3
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 208000024891 symptom Diseases 0.000 claims description 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- 101001109463 Homo sapiens NACHT, LRR and PYD domains-containing protein 1 Proteins 0.000 claims 1
- 102100022698 NACHT, LRR and PYD domains-containing protein 1 Human genes 0.000 claims 1
- 102100022691 NACHT, LRR and PYD domains-containing protein 3 Human genes 0.000 claims 1
- 238000000034 method Methods 0.000 description 67
- 125000001188 haloalkyl group Chemical group 0.000 description 44
- 125000004438 haloalkoxy group Chemical group 0.000 description 26
- 125000003342 alkenyl group Chemical group 0.000 description 21
- 150000001345 alkine derivatives Chemical class 0.000 description 18
- 125000000304 alkynyl group Chemical group 0.000 description 15
- 206010028980 Neoplasm Diseases 0.000 description 11
- 201000011510 cancer Diseases 0.000 description 11
- 102000000874 Pyrin Domain-Containing 3 Protein NLR Family Human genes 0.000 description 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 9
- 0 Cc1nc(I*)c(*)[s]1 Chemical compound Cc1nc(I*)c(*)[s]1 0.000 description 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 7
- 125000001153 fluoro group Chemical group F* 0.000 description 6
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 5
- 239000000126 substance Substances 0.000 description 5
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 description 4
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 description 4
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 description 4
- 239000005557 antagonist Substances 0.000 description 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 4
- 125000000335 thiazolyl group Chemical group 0.000 description 4
- 208000031261 Acute myeloid leukaemia Diseases 0.000 description 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 description 3
- 125000002393 azetidinyl group Chemical group 0.000 description 3
- 125000001309 chloro group Chemical group Cl* 0.000 description 3
- 125000003016 chromanyl group Chemical group O1C(CCC2=CC=CC=C12)* 0.000 description 3
- DXASQZJWWGZNSF-UHFFFAOYSA-N n,n-dimethylmethanamine;sulfur trioxide Chemical group CN(C)C.O=S(=O)=O DXASQZJWWGZNSF-UHFFFAOYSA-N 0.000 description 3
- 208000002154 non-small cell lung carcinoma Diseases 0.000 description 3
- 125000000714 pyrimidinyl group Chemical group 0.000 description 3
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 description 3
- IANQTJSKSUMEQM-UHFFFAOYSA-N 1-benzofuran Chemical compound C1=CC=C2OC=CC2=C1 IANQTJSKSUMEQM-UHFFFAOYSA-N 0.000 description 2
- FCEHBMOGCRZNNI-UHFFFAOYSA-N 1-benzothiophene Chemical compound C1=CC=C2SC=CC2=C1 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 description 2
- 125000004066 1-hydroxyethyl group Chemical group [H]OC([H])([*])C([H])([H])[H] 0.000 description 2
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 description 2
- 206010059245 Angiopathy Diseases 0.000 description 2
- 208000023275 Autoimmune disease Diseases 0.000 description 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 description 2
- 208000020084 Bone disease Diseases 0.000 description 2
- 206010016654 Fibrosis Diseases 0.000 description 2
- 208000019693 Lung disease Diseases 0.000 description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 description 2
- 206010027476 Metastases Diseases 0.000 description 2
- 208000034578 Multiple myelomas Diseases 0.000 description 2
- 208000023178 Musculoskeletal disease Diseases 0.000 description 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 description 2
- 208000016222 Pancreatic disease Diseases 0.000 description 2
- 206010035226 Plasma cell myeloma Diseases 0.000 description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 description 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 2
- 208000036142 Viral infection Diseases 0.000 description 2
- 208000015114 central nervous system disease Diseases 0.000 description 2
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 description 2
- 208000030533 eye disease Diseases 0.000 description 2
- 206010017758 gastric cancer Diseases 0.000 description 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 description 2
- 208000028774 intestinal disease Diseases 0.000 description 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 2
- AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical compound C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 description 2
- 208000017169 kidney disease Diseases 0.000 description 2
- 208000019423 liver disease Diseases 0.000 description 2
- 201000005202 lung cancer Diseases 0.000 description 2
- 208000020816 lung neoplasm Diseases 0.000 description 2
- 208000030159 metabolic disease Diseases 0.000 description 2
- 230000009401 metastasis Effects 0.000 description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 2
- 208000017445 musculoskeletal system disease Diseases 0.000 description 2
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 description 2
- 125000003226 pyrazolyl group Chemical group 0.000 description 2
- XSCHRSMBECNVNS-UHFFFAOYSA-N quinoxaline Chemical compound N1=CC=NC2=CC=CC=C21 XSCHRSMBECNVNS-UHFFFAOYSA-N 0.000 description 2
- 208000017520 skin disease Diseases 0.000 description 2
- 201000011549 stomach cancer Diseases 0.000 description 2
- 208000011580 syndromic disease Diseases 0.000 description 2
- CXWXQJXEFPUFDZ-UHFFFAOYSA-N tetralin Chemical compound C1=CC=C2CCCCC2=C1 CXWXQJXEFPUFDZ-UHFFFAOYSA-N 0.000 description 2
- 230000009385 viral infection Effects 0.000 description 2
- 125000005943 1,2,3,6-tetrahydropyridyl group Chemical group 0.000 description 1
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 description 1
- QKSLBKHGKROAFN-UHFFFAOYSA-N 3,4-dihydropyrrole Chemical compound [CH]1CCC=N1 QKSLBKHGKROAFN-UHFFFAOYSA-N 0.000 description 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 description 1
- 208000030507 AIDS Diseases 0.000 description 1
- 208000009304 Acute Kidney Injury Diseases 0.000 description 1
- 208000036762 Acute promyelocytic leukaemia Diseases 0.000 description 1
- 208000024827 Alzheimer disease Diseases 0.000 description 1
- 201000001320 Atherosclerosis Diseases 0.000 description 1
- 208000000668 Chronic Pancreatitis Diseases 0.000 description 1
- 206010009900 Colitis ulcerative Diseases 0.000 description 1
- 208000011231 Crohn disease Diseases 0.000 description 1
- 206010058314 Dysplasia Diseases 0.000 description 1
- 208000007465 Giant cell arteritis Diseases 0.000 description 1
- 208000010412 Glaucoma Diseases 0.000 description 1
- 201000005569 Gout Diseases 0.000 description 1
- 208000030836 Hashimoto thyroiditis Diseases 0.000 description 1
- 206010019799 Hepatitis viral Diseases 0.000 description 1
- 208000008589 Obesity Diseases 0.000 description 1
- 208000001132 Osteoporosis Diseases 0.000 description 1
- 206010033645 Pancreatitis Diseases 0.000 description 1
- 206010033647 Pancreatitis acute Diseases 0.000 description 1
- 206010033649 Pancreatitis chronic Diseases 0.000 description 1
- 208000018737 Parkinson disease Diseases 0.000 description 1
- 208000031845 Pernicious anaemia Diseases 0.000 description 1
- 201000004681 Psoriasis Diseases 0.000 description 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 description 1
- 208000033626 Renal failure acute Diseases 0.000 description 1
- 206010061481 Renal injury Diseases 0.000 description 1
- 206010039710 Scleroderma Diseases 0.000 description 1
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 description 1
- 201000006704 Ulcerative Colitis Diseases 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 201000011040 acute kidney failure Diseases 0.000 description 1
- 201000003229 acute pancreatitis Diseases 0.000 description 1
- 230000032683 aging Effects 0.000 description 1
- 125000004419 alkynylene group Chemical group 0.000 description 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 description 1
- 230000003042 antagnostic effect Effects 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- 208000036923 autoimmune primary adrenal insufficiency Diseases 0.000 description 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 230000007882 cirrhosis Effects 0.000 description 1
- 208000019425 cirrhosis of liver Diseases 0.000 description 1
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 208000037902 enteropathy Diseases 0.000 description 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 description 1
- 230000004761 fibrosis Effects 0.000 description 1
- 239000003862 glucocorticoid Substances 0.000 description 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- PQNFLJBBNBOBRQ-UHFFFAOYSA-N indane Chemical compound C1=CC=C2CCCC2=C1 PQNFLJBBNBOBRQ-UHFFFAOYSA-N 0.000 description 1
- 125000003384 isochromanyl group Chemical group C1(OCCC2=CC=CC=C12)* 0.000 description 1
- GWVMLCQWXVFZCN-UHFFFAOYSA-N isoindoline Chemical compound C1=CC=C2CNCC2=C1 GWVMLCQWXVFZCN-UHFFFAOYSA-N 0.000 description 1
- 125000000842 isoxazolyl group Chemical group 0.000 description 1
- 208000037806 kidney injury Diseases 0.000 description 1
- 210000001821 langerhans cell Anatomy 0.000 description 1
- 208000032839 leukemia Diseases 0.000 description 1
- 208000002780 macular degeneration Diseases 0.000 description 1
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 125000002757 morpholinyl group Chemical group 0.000 description 1
- 201000006417 multiple sclerosis Diseases 0.000 description 1
- 230000035772 mutation Effects 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 description 1
- 235000020824 obesity Nutrition 0.000 description 1
- 201000008482 osteoarthritis Diseases 0.000 description 1
- 208000002865 osteopetrosis Diseases 0.000 description 1
- 230000002018 overexpression Effects 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- SFLGSKRGOWRGBR-UHFFFAOYSA-N phthalane Chemical compound C1=CC=C2COCC2=C1 SFLGSKRGOWRGBR-UHFFFAOYSA-N 0.000 description 1
- 230000002685 pulmonary effect Effects 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- VTGOHKSTWXHQJK-UHFFFAOYSA-N pyrimidin-2-ol Chemical compound OC1=NC=CC=N1 VTGOHKSTWXHQJK-UHFFFAOYSA-N 0.000 description 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 description 1
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 description 1
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical compound N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 description 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 206010039073 rheumatoid arthritis Diseases 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 description 1
- 206010043207 temporal arteritis Diseases 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 1
- 201000001862 viral hepatitis Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762573562P | 2017-10-17 | 2017-10-17 | |
| US62/573,562 | 2017-10-17 | ||
| PCT/US2018/055576 WO2019079119A1 (en) | 2017-10-17 | 2018-10-12 | SULFONAMIDES AND ASSOCIATED COMPOSITIONS FOR THE TREATMENT OF PATHOLOGICAL CONDITIONS ASSOCIATED WITH NLRP ACTIVITY |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020537657A JP2020537657A (ja) | 2020-12-24 |
| JP2020537657A5 true JP2020537657A5 (https=) | 2021-11-25 |
| JP7157804B2 JP7157804B2 (ja) | 2022-10-20 |
Family
ID=64051793
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020521522A Active JP7157804B2 (ja) | 2017-10-17 | 2018-10-12 | Ｎｌｒｐ活性に関連する病態を治療するためのスルホンアミド及びその組成物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US11718631B2 (https=) |
| EP (1) | EP3697758B1 (https=) |
| JP (1) | JP7157804B2 (https=) |
| CN (1) | CN111417622A (https=) |
| ES (1) | ES2927851T3 (https=) |
| WO (1) | WO2019079119A1 (https=) |
Families Citing this family (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MA49903A (fr) | 2017-08-15 | 2020-06-24 | Inflazome Ltd | Sulfonylureés et sulfonylthioureés en tant qu'inhibiteurs de nlrp3 |
| EP3759090A1 (en) | 2018-03-02 | 2021-01-06 | Inflazome Limited | Novel compounds |
| EP3759078A1 (en) | 2018-03-02 | 2021-01-06 | Inflazome Limited | Novel compounds |
| WO2019166627A1 (en) | 2018-03-02 | 2019-09-06 | Inflazome Limited | Novel compounds |
| US11530200B2 (en) | 2018-03-02 | 2022-12-20 | Inflazome Limited | Compounds |
| JP2021529186A (ja) * | 2018-07-03 | 2021-10-28 | ノバルティス アーゲー | Ｎｌｒｐ調節剤 |
| GB201902327D0 (en) | 2019-02-20 | 2019-04-03 | Inflazome Ltd | Novel compounds |
| KR20210053910A (ko) | 2018-08-15 | 2021-05-12 | 인플라좀 리미티드 | 신규한 설폰아마이드유레아 화합물 |
| GB201819083D0 (en) | 2018-11-23 | 2019-01-09 | Inflazome Ltd | Novel compounds |
| GB201905265D0 (en) | 2019-04-12 | 2019-05-29 | Inflazome Ltd | Inflammasome inhibition |
| EP3986879B1 (en) | 2019-06-21 | 2024-10-02 | AC Immune SA | Fused 1,2-thiazoles and 1,2-thiazines which act as nlrp3 modulators |
| KR20220064364A (ko) | 2019-07-17 | 2022-05-18 | 조마젠 바이오사이언시즈 엘티디 | 다발성 경화증(ms)의 치료를 위한 nlpr3 조절제로서의 n-((1,2,3,5,6,7-헥사하이드로-s-인다센-4-일)카바모일)-4,5,6,7-테트라하이드로벤조푸란-2-설폰아미드 유도체 및 관련 화합물 |
| EP3999179A1 (en) | 2019-07-17 | 2022-05-25 | Zomagen Biosciences Ltd | Nlrp3 modulators |
| WO2021032588A1 (en) | 2019-08-16 | 2021-02-25 | Inflazome Limited | Macrocyclic sulfonylamide derivatives useful as nlrp3 inhibitors |
| US20220289692A1 (en) | 2019-09-06 | 2022-09-15 | Inflazome Limited | Nlrp3 inhibitors |
| CN114641287A (zh) * | 2019-11-07 | 2022-06-17 | 英夫拉索姆有限公司 | 神经退行性病症的治疗和预防 |
| JP7392169B2 (ja) * | 2019-11-12 | 2023-12-05 | 成都百裕制薬股▲ふん▼有限公司 | アミド誘導体及びその調製方法並びに医薬における応用 |
| PH12022552447A1 (en) | 2020-03-16 | 2024-01-03 | Zomagen Biosciences Ltd | Nlrp3 modulators |
| AU2021257619A1 (en) | 2020-04-15 | 2022-12-15 | Janssen Pharmaceutica Nv | Pyrazolo[1,5-d][1,2,4]triazine-5(4H)-acetamides as inhibitors of the NLRP3 inflammasome pathway |
| CN115485026A (zh) | 2020-04-15 | 2022-12-16 | 詹森药业有限公司 | Nlrp3炎体途径抑制剂吡唑并[1，2-d][1，2，4]三嗪-2-基-乙酰胺 |
| EP4139312A1 (en) | 2020-04-23 | 2023-03-01 | JANSSEN Pharmaceutica NV | Tricyclic compounds as inhibitors of nlrp3 |
| MX2022013637A (es) | 2020-04-30 | 2022-11-16 | Janssen Pharmaceutica Nv | Nuevos compuestos de triazinoindol. |
| US20230202989A1 (en) | 2020-05-28 | 2023-06-29 | Janssen Pharmaceutica Nv | Compounds |
| AU2021291065B2 (en) | 2020-06-19 | 2025-06-26 | Ac Immune Sa | Dihydrooxazole and thiourea or urea derivatives modulating the nlrp3 inflammasome pathway |
| US12577211B2 (en) | 2020-06-29 | 2026-03-17 | Bacainn Biotherapeutics, Ltd. | Probenecid compounds for the treatment of inflammasome-mediated lung disease |
| WO2022023907A1 (en) | 2020-07-31 | 2022-02-03 | Novartis Ag | Methods of selecting and treating patients at elevated risk of major adverse cardiac events |
| EP3974415A1 (en) | 2020-09-24 | 2022-03-30 | Janssen Pharmaceutica NV | Nlrp3 modulators |
| CN116194445A (zh) | 2020-09-24 | 2023-05-30 | 詹森药业有限公司 | 新化合物 |
| CN114133345A (zh) * | 2020-12-17 | 2022-03-04 | 顺毅宜昌化工有限公司 | 一种2-氯磺酰基-4-甲磺酰胺甲基苯甲酸甲酯的制备方法 |
| CN116964052A (zh) | 2021-03-04 | 2023-10-27 | 詹森药业有限公司 | 调节nlrp3的4-氨基-6-氧代-哒嗪衍生物 |
| JP2024508017A (ja) | 2021-03-04 | 2024-02-21 | ヤンセン ファーマシューティカ エヌ．ベー． | Ｎｌｒｐ３を調節する４－アルコキシ－６－オキソ－ピリダジン誘導体 |
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| CN116917282A (zh) * | 2021-05-10 | 2023-10-20 | 成都百裕制药股份有限公司 | 酰胺衍生物及其应用 |
| KR20240029027A (ko) | 2021-07-01 | 2024-03-05 | 얀센 파마슈티카 엔브이 | 5-옥소-피리도[2,3-d]피리다진-6(5H)-일 아세트아미드 |
| CN115677616B (zh) * | 2021-11-03 | 2024-10-18 | 中国药科大学 | 大环磺酰胺类化合物及其制备方法和医药用途 |
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| US20250109154A1 (en) * | 2022-01-27 | 2025-04-03 | The University Of Tokyo | Lysophosphatidylserine analogue, and lysophosphatidylserine analogue-containing phamaceutical composition for treating or preventing fibrosis |
| WO2023158824A1 (en) * | 2022-02-21 | 2023-08-24 | Viva Star Biosciences (Suzhou) Co., Ltd. | Novel bicyclic substituted sulfonylurea compounds as inhibitors of interleukin- 1 activity |
| EP4554945A1 (en) | 2022-07-14 | 2025-05-21 | AC Immune SA | Pyrrolotriazine and imidazotriazine derivatives as modulators of the nlrp3 inflammasome pathway |
| GEAP202516743A (en) | 2022-09-23 | 2025-08-11 | Merck Sharp & Dohme Llc | Phthalazine derivatives useful as inhibitors of nod-like receptor protein 3 |
| AU2024280075A1 (en) | 2023-06-02 | 2025-12-11 | Merck Sharp & Dohme Llc | 5,6-Unsaturated Bicyclic Heterocycles Useful as Inhibitors of Nod-Like Receptor Protein 3 |
| AR134646A1 (es) | 2023-12-14 | 2026-02-04 | Merck Sharp & Dohme Llc | Derivados de indazol útiles como inhibidores de la proteína 3 del receptor similar a nod |
| US20250223290A1 (en) | 2023-12-14 | 2025-07-10 | Merck Sharp & Dohme Llc | Azaindazole derivatives useful as inhibitors of nod-like receptor protein 3 |
| WO2025133307A1 (en) | 2023-12-22 | 2025-06-26 | Ac Immune Sa | Heterocyclic modulators of the nlrp3 inflammasome pathway |
| WO2025153532A1 (en) | 2024-01-16 | 2025-07-24 | NodThera Limited | Nlrp3 inhibitors and glp-1 agonists combination therapies |
| WO2025153624A1 (en) | 2024-01-17 | 2025-07-24 | Ac Immune Sa | Imidazo[1,2-d][1,2,4]triazine derivatives for use as inhibitors of the nlrp3 inflammasome pathway |
| WO2025153625A1 (en) | 2024-01-17 | 2025-07-24 | Ac Immune Sa | Imidazo[1,2-d][1,2,4]triazine derivatives for use as inhibitors of the nlrp3 inflammasome pathway |
| WO2025163069A1 (en) | 2024-01-31 | 2025-08-07 | Ac Immune Sa | Novel compounds |
| WO2026057747A1 (en) | 2024-09-11 | 2026-03-19 | Ac Immune Sa | Therapeutic use of nlrp3 inflammasome pathway inhibitor compounds |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4200954A1 (de) * | 1991-04-26 | 1992-10-29 | Bayer Ag | Heterocyclisch substituierte phenylessigsaeurederivate |
| PT1270565E (pt) * | 1997-01-29 | 2004-09-30 | Pfizer | Furano-2-sulfonamida 4-substituida e sua utilizacao na preparacao de derivados de sulfonilureia |
| GB9828442D0 (en) * | 1998-12-24 | 1999-02-17 | Karobio Ab | Novel thyroid receptor ligands and method II |
| AU7447500A (en) | 1999-09-30 | 2001-04-30 | Mitsubishi Chemical Corporation | Acylsulfonamide derivatives |
| MXPA04001253A (es) * | 2001-08-09 | 2004-06-03 | Ono Pharmaceutical Co | Derivados de acidos carboxilicos y agente farmaceutico que comprende los mismos como ingrediente activo. |
| GB0324269D0 (en) * | 2003-10-16 | 2003-11-19 | Pharmagene Lab Ltd | EP4 receptor antagonists |
| GB0725214D0 (en) * | 2007-12-24 | 2008-02-06 | Karobio Ab | Pharmaceutical compounds |
| CN103172547B (zh) | 2011-12-20 | 2016-10-12 | 天津市国际生物医药联合研究院 | 磺酰胺衍生物的制备及其应用 |
| CN103159674A (zh) | 2013-04-03 | 2013-06-19 | 苏州安诺生物医药技术有限公司 | 2-苯烷酰胺类化合物及其制备方法、药物组合物和用途 |
| FR3046933B1 (fr) * | 2016-01-25 | 2018-03-02 | Galderma Research & Development | Inhibiteurs nlrp3 pour le traitement des pathologies cutanees inflammatoires |
| US11447460B2 (en) * | 2016-04-18 | 2022-09-20 | Novartis Ag | Compounds and compositions for treating conditions associated with NLRP activity |
-
2018
- 2018-10-12 WO PCT/US2018/055576 patent/WO2019079119A1/en not_active Ceased
- 2018-10-12 CN CN201880077068.6A patent/CN111417622A/zh active Pending
- 2018-10-12 ES ES18796291T patent/ES2927851T3/es active Active
- 2018-10-12 JP JP2020521522A patent/JP7157804B2/ja active Active
- 2018-10-12 US US16/756,358 patent/US11718631B2/en active Active
- 2018-10-12 EP EP18796291.5A patent/EP3697758B1/en active Active
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