JP2017514839A5 - - Google Patents
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- JP2017514839A5 JP2017514839A5 JP2016565403A JP2016565403A JP2017514839A5 JP 2017514839 A5 JP2017514839 A5 JP 2017514839A5 JP 2016565403 A JP2016565403 A JP 2016565403A JP 2016565403 A JP2016565403 A JP 2016565403A JP 2017514839 A5 JP2017514839 A5 JP 2017514839A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- pyrrolo
- methyl
- pyrimidin
- alkyl
- 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.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims 22
- 125000005842 heteroatom Chemical group 0.000 claims 12
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 11
- 201000010099 disease Diseases 0.000 claims 10
- 125000004193 piperazinyl group Chemical group 0.000 claims 9
- 125000002757 morpholinyl group Chemical group 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 4
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 4
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- -1 2- (morpholin-4-yl) ethyl Chemical group 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 206010004146 Basal cell carcinoma Diseases 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- CHBISLXEGUDRRV-SFHVURJKSA-N CCCC[C@H](C)NC1=NC(=NC2=C1N(C=C2)CC3=C(C=CC(=C3)CN4CCNCC4)OC)N Chemical compound CCCC[C@H](C)NC1=NC(=NC2=C1N(C=C2)CC3=C(C=CC(=C3)CN4CCNCC4)OC)N CHBISLXEGUDRRV-SFHVURJKSA-N 0.000 claims 2
- SBILKCCWZZAMEO-UHFFFAOYSA-N COC1=C(CN2C=CC=3N=C(N=C(C32)NCCCCC)N)C=C(C=C1)CN1CCNCC1 Chemical compound COC1=C(CN2C=CC=3N=C(N=C(C32)NCCCCC)N)C=C(C=C1)CN1CCNCC1 SBILKCCWZZAMEO-UHFFFAOYSA-N 0.000 claims 2
- LMXTZUAHGZBEKB-UHFFFAOYSA-N COC1=C(CN2C=CC=3N=C(N=C(C32)NCCCCC)N)C=CC(=C1)CN1CCNCC1 Chemical compound COC1=C(CN2C=CC=3N=C(N=C(C32)NCCCCC)N)C=CC(=C1)CN1CCNCC1 LMXTZUAHGZBEKB-UHFFFAOYSA-N 0.000 claims 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims 2
- 208000011231 Crohn disease Diseases 0.000 claims 2
- 201000004624 Dermatitis Diseases 0.000 claims 2
- 208000005176 Hepatitis C Diseases 0.000 claims 2
- QRJUJOQGEKSMAJ-UHFFFAOYSA-N NC=1C=CC(=C(CN2C=CC=3N=C(N=C(C32)NCCCCC)N)C1)OC Chemical compound NC=1C=CC(=C(CN2C=CC=3N=C(N=C(C32)NCCCCC)N)C1)OC QRJUJOQGEKSMAJ-UHFFFAOYSA-N 0.000 claims 2
- IIILSKLUXKONMT-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CC(=O)OCC(=O)N2CCOCC2)OC)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CC(=O)OCC(=O)N2CCOCC2)OC)NCCCCC IIILSKLUXKONMT-UHFFFAOYSA-N 0.000 claims 2
- GTZVTPGTXBZOIN-FQEVSTJZSA-N NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CN2CCNCC2)OC)N[C@H](CO)CCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CN2CCNCC2)OC)N[C@H](CO)CCCC GTZVTPGTXBZOIN-FQEVSTJZSA-N 0.000 claims 2
- QLZDGWRAIFYJAV-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)CC(=O)OCC(=O)N2CCOCC2)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)CC(=O)OCC(=O)N2CCOCC2)NCCCCC QLZDGWRAIFYJAV-UHFFFAOYSA-N 0.000 claims 2
- KNMSPDSJHHYLOT-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC=2C=C(OCC(=O)O)C=CC2OC)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC=2C=C(OCC(=O)O)C=CC2OC)NCCCCC KNMSPDSJHHYLOT-UHFFFAOYSA-N 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 206010039710 Scleroderma Diseases 0.000 claims 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 2
- 208000024780 Urticaria Diseases 0.000 claims 2
- 208000036142 Viral infection Diseases 0.000 claims 2
- 208000009621 actinic keratosis Diseases 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 206010006451 bronchitis Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 208000006454 hepatitis Diseases 0.000 claims 2
- 231100000283 hepatitis Toxicity 0.000 claims 2
- 208000015181 infectious disease Diseases 0.000 claims 2
- 206010025135 lupus erythematosus Diseases 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 208000023504 respiratory system disease Diseases 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 230000009385 viral infection Effects 0.000 claims 2
- QWJGXSAWJMJJNM-UHFFFAOYSA-N 2-(dimethylamino)ethyl 4-[[2-amino-4-(pentylamino)pyrrolo[3,2-d]pyrimidin-5-yl]methyl]-3-methoxybenzoate Chemical compound NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C(=O)OCCN(C)C)C=C2)OC)NCCCCC QWJGXSAWJMJJNM-UHFFFAOYSA-N 0.000 claims 1
- 208000005440 Basal Cell Neoplasms Diseases 0.000 claims 1
- MYRNVYLFILMXIA-UHFFFAOYSA-N CCCCCNC1=NC(N)=NC2=C1N(CC(C=C(C=C1)OOC(C)=O)=C1OC)C=C2 Chemical compound CCCCCNC1=NC(N)=NC2=C1N(CC(C=C(C=C1)OOC(C)=O)=C1OC)C=C2 MYRNVYLFILMXIA-UHFFFAOYSA-N 0.000 claims 1
- 208000035473 Communicable disease Diseases 0.000 claims 1
- 101000669402 Homo sapiens Toll-like receptor 7 Proteins 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- OWWMDXNTWDIJTR-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C(=O)OCCOCCN(C)C)C=C2)OC)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C(=O)OCCOCCN(C)C)C=C2)OC)NCCCCC OWWMDXNTWDIJTR-UHFFFAOYSA-N 0.000 claims 1
- ZXQMNLAFFOUHIX-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CC(=O)OCC(=O)N(C)C)OC)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CC(=O)OCC(=O)N(C)C)OC)NCCCCC ZXQMNLAFFOUHIX-UHFFFAOYSA-N 0.000 claims 1
- CWZMIMVFFXBCGL-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CC(=O)OCC(=O)N(CCC)CCC)OC)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CC(=O)OCC(=O)N(CCC)CCC)OC)NCCCCC CWZMIMVFFXBCGL-UHFFFAOYSA-N 0.000 claims 1
- ANQLBQCZOMUHDE-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CC(=O)OCC(=O)OCC2=CC=CC=C2)OC)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CC(=O)OCC(=O)OCC2=CC=CC=C2)OC)NCCCCC ANQLBQCZOMUHDE-UHFFFAOYSA-N 0.000 claims 1
- MEQGHEXQNNTNNQ-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CC(=O)OCCCCN(C)C)OC)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CC(=O)OCCCCN(C)C)OC)NCCCCC MEQGHEXQNNTNNQ-UHFFFAOYSA-N 0.000 claims 1
- URJBQKFMEUCALS-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CC(=O)OCCN2CCN(CC2)C)OC)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CC(=O)OCCN2CCN(CC2)C)OC)NCCCCC URJBQKFMEUCALS-UHFFFAOYSA-N 0.000 claims 1
- LIHUPNDPYYFZRX-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CC(=O)OCCN2CCNCC2)OC)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CC(=O)OCCN2CCNCC2)OC)NCCCCC LIHUPNDPYYFZRX-UHFFFAOYSA-N 0.000 claims 1
- CXFIJOIUEFZMPL-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CC(=O)OCCN2CCOCC2)OC)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CC(=O)OCCN2CCOCC2)OC)NCCCCC CXFIJOIUEFZMPL-UHFFFAOYSA-N 0.000 claims 1
- GUQLIIRSXGTEOH-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CC(=O)OCCO)OC)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CC(=O)OCCO)OC)NCCCCC GUQLIIRSXGTEOH-UHFFFAOYSA-N 0.000 claims 1
- IPOKHQKKYBVTRQ-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CCC(=O)OCC(=O)N2CCOCC2)OC)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(C=C2)CCC(=O)OCC(=O)N2CCOCC2)OC)NCCCCC IPOKHQKKYBVTRQ-UHFFFAOYSA-N 0.000 claims 1
- QVOMNIZXHGDOSF-VQHVLOKHSA-N NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)/C=C/C(=O)OCC(=O)N2CCOCC2)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)/C=C/C(=O)OCC(=O)N2CCOCC2)NCCCCC QVOMNIZXHGDOSF-VQHVLOKHSA-N 0.000 claims 1
- DWUQECPGRFUAPF-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)C(C(=O)OC)(F)F)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)C(C(=O)OC)(F)F)NCCCCC DWUQECPGRFUAPF-UHFFFAOYSA-N 0.000 claims 1
- XKTDCSNRVNSJCL-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)CC(=O)OC)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)CC(=O)OC)NCCCCC XKTDCSNRVNSJCL-UHFFFAOYSA-N 0.000 claims 1
- AZSRICQTDGPXHM-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)CCC(=O)OCC(=O)N2CCOCC2)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)CCC(=O)OCC(=O)N2CCOCC2)NCCCCC AZSRICQTDGPXHM-UHFFFAOYSA-N 0.000 claims 1
- CGJMKTBLNLYJHB-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)CCC(=O)OCC)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)CCC(=O)OCC)NCCCCC CGJMKTBLNLYJHB-UHFFFAOYSA-N 0.000 claims 1
- JLVGGBGDDHERCL-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC=2C=C(OCC(=O)OCCN(C)C)C=CC2OC)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC=2C=C(OCC(=O)OCCN(C)C)C=CC2OC)NCCCCC JLVGGBGDDHERCL-UHFFFAOYSA-N 0.000 claims 1
- SVVQSCXECIIRGC-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC=2C=C(OCC(=O)OCCN1CCN(CC1)C)C=CC2OC)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC=2C=C(OCC(=O)OCCN1CCN(CC1)C)C=CC2OC)NCCCCC SVVQSCXECIIRGC-UHFFFAOYSA-N 0.000 claims 1
- DTXPCGHJNKAOON-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC=2C=C(OCC(=O)OCCN1CCNCC1)C=CC2OC)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC=2C=C(OCC(=O)OCCN1CCNCC1)C=CC2OC)NCCCCC DTXPCGHJNKAOON-UHFFFAOYSA-N 0.000 claims 1
- 208000007222 Physiological Sexual Dysfunction Diseases 0.000 claims 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-N Propionic acid Chemical compound CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- 108010060825 Toll-Like Receptor 7 Proteins 0.000 claims 1
- 102000008236 Toll-Like Receptor 7 Human genes 0.000 claims 1
- 102100039390 Toll-like receptor 7 Human genes 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000004894 pentylamino group Chemical group C(CCCC)N* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 1
- 206010039083 rhinitis Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461987314P | 2014-05-01 | 2014-05-01 | |
| US61/987,314 | 2014-05-01 | ||
| PCT/US2015/028285 WO2015168279A1 (en) | 2014-05-01 | 2015-04-29 | Compounds and compositions as toll-like receptor 7 agonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017514839A JP2017514839A (ja) | 2017-06-08 |
| JP2017514839A5 true JP2017514839A5 (enExample) | 2018-06-14 |
| JP6541689B2 JP6541689B2 (ja) | 2019-07-10 |
Family
ID=53264739
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016565403A Expired - Fee Related JP6541689B2 (ja) | 2014-05-01 | 2015-04-29 | Toll様受容体7アゴニストとしての化合物および組成物 |
Country Status (15)
| Country | Link |
|---|---|
| US (3) | US9944649B2 (enExample) |
| EP (1) | EP3137468B1 (enExample) |
| JP (1) | JP6541689B2 (enExample) |
| KR (1) | KR20160144399A (enExample) |
| CN (1) | CN106459058B (enExample) |
| AU (1) | AU2015253225B2 (enExample) |
| BR (1) | BR112016025048A2 (enExample) |
| CA (1) | CA2945504A1 (enExample) |
| EA (1) | EA032487B1 (enExample) |
| ES (1) | ES2908150T3 (enExample) |
| IL (1) | IL248311B (enExample) |
| MX (1) | MX380777B (enExample) |
| NZ (1) | NZ724878A (enExample) |
| SG (1) | SG11201608299TA (enExample) |
| WO (1) | WO2015168279A1 (enExample) |
Families Citing this family (65)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX362341B (es) | 2014-05-01 | 2019-01-11 | Novartis Ag | Compuestos y composiciones como agonistas del receptor tipo toll 7. |
| CN110759916B (zh) | 2014-08-15 | 2021-02-19 | 正大天晴药业集团股份有限公司 | 作为tlr7激动剂的吡咯并嘧啶化合物 |
| CN105732635A (zh) * | 2014-12-29 | 2016-07-06 | 南京明德新药研发股份有限公司 | 一类Toll样受体7激动剂 |
| MA44334A (fr) * | 2015-10-29 | 2018-09-05 | Novartis Ag | Conjugués d'anticorps comprenant un agoniste du récepteur de type toll |
| CN107043380A (zh) | 2016-02-05 | 2017-08-15 | 正大天晴药业集团股份有限公司 | 一种tlr7激动剂的马来酸盐、其晶型c、晶型d、晶型e、制备方法和用途 |
| CN107043377A (zh) * | 2016-02-05 | 2017-08-15 | 正大天晴药业集团股份有限公司 | 一种tlr7激动剂的三氟乙酸盐、晶型b及其制备方法、药物组合物和用途 |
| US10662416B2 (en) | 2016-10-14 | 2020-05-26 | Precision Biosciences, Inc. | Engineered meganucleases specific for recognition sequences in the hepatitis B virus genome |
| AR111651A1 (es) * | 2017-04-28 | 2019-08-07 | Novartis Ag | Conjugados de anticuerpos que comprenden agonistas del receptor de tipo toll y terapias de combinación |
| US10487084B2 (en) | 2017-08-16 | 2019-11-26 | Bristol-Myers Squibb Company | Toll-like receptor 7 (TLR7) agonists having a heterobiaryl moiety, conjugates thereof, and methods and uses therefor |
| US10494370B2 (en) | 2017-08-16 | 2019-12-03 | Bristol-Myers Squibb Company | Toll-like receptor 7 (TLR7) agonists having a pyridine or pyrazine moiety, conjugates thereof, and methods and uses therefor |
| US10457681B2 (en) | 2017-08-16 | 2019-10-29 | Bristol_Myers Squibb Company | Toll-like receptor 7 (TLR7) agonists having a tricyclic moiety, conjugates thereof, and methods and uses therefor |
| US10472361B2 (en) | 2017-08-16 | 2019-11-12 | Bristol-Myers Squibb Company | Toll-like receptor 7 (TLR7) agonists having a benzotriazole moiety, conjugates thereof, and methods and uses therefor |
| US10508115B2 (en) | 2017-08-16 | 2019-12-17 | Bristol-Myers Squibb Company | Toll-like receptor 7 (TLR7) agonists having heteroatom-linked aromatic moieties, conjugates thereof, and methods and uses therefor |
| US10618896B2 (en) | 2017-08-22 | 2020-04-14 | Dynavax Technologies Corporation | Alkyl chain modified imidazoquinoline TLR7/8 agonist compounds and uses thereof |
| US11806364B2 (en) | 2017-09-28 | 2023-11-07 | Industry-Academic Cooperation Foundation, Yonsei University | Method for producing myeloid-derived suppressor cells, myeloid-derived suppressor cells produced thereby, and methods thereof |
| US10722591B2 (en) | 2017-11-14 | 2020-07-28 | Dynavax Technologies Corporation | Cleavable conjugates of TLR7/8 agonist compounds, methods for preparation, and uses thereof |
| CN111511754B (zh) | 2017-12-20 | 2023-09-12 | 捷克共和国有机化学与生物化学研究所 | 活化sting转接蛋白的具有膦酸酯键的2’3’环状二核苷酸 |
| KR102492187B1 (ko) | 2017-12-20 | 2023-01-27 | 인스티튜트 오브 오가닉 케미스트리 앤드 바이오케미스트리 에이에스 씨알 브이.브이.아이. | Sting 어댑터 단백질을 활성화하는 포스포네이트 결합을 가진 3'3' 사이클릭 다이뉴클레오티드 |
| KR102526964B1 (ko) | 2018-02-26 | 2023-04-28 | 길리애드 사이언시즈, 인코포레이티드 | Hbv 복제 억제제로서의 치환된 피롤리진 화합물 |
| EP3774883A1 (en) | 2018-04-05 | 2021-02-17 | Gilead Sciences, Inc. | Antibodies and fragments thereof that bind hepatitis b virus protein x |
| TWI833744B (zh) | 2018-04-06 | 2024-03-01 | 捷克科學院有機化學與生物化學研究所 | 3'3'-環二核苷酸 |
| TW202005654A (zh) | 2018-04-06 | 2020-02-01 | 捷克科學院有機化學與生物化學研究所 | 2,2,─環二核苷酸 |
| TWI818007B (zh) | 2018-04-06 | 2023-10-11 | 捷克科學院有機化學與生物化學研究所 | 2'3'-環二核苷酸 |
| TW201945388A (zh) | 2018-04-12 | 2019-12-01 | 美商精密生物科學公司 | 對b型肝炎病毒基因體中之識別序列具有特異性之最佳化之經工程化巨核酸酶 |
| US11485741B2 (en) | 2018-04-24 | 2022-11-01 | Bristol-Myers Squibb Company | Macrocyclic toll-like receptor 7 (TLR7) agonists |
| US20190359645A1 (en) | 2018-05-03 | 2019-11-28 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2'3'-cyclic dinucleotides comprising carbocyclic nucleotide |
| WO2020028097A1 (en) | 2018-08-01 | 2020-02-06 | Gilead Sciences, Inc. | Solid forms of (r)-11-(methoxymethyl)-12-(3-methoxypropoxy)-3,3-dimethyl-8-0x0-2,3,8,13b-tetrahydro-1h-pyrido[2,1-a]pyrrolo[1,2-c] phthalazine-7-c arboxylic acid |
| US11554120B2 (en) | 2018-08-03 | 2023-01-17 | Bristol-Myers Squibb Company | 1H-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (TLR7) agonists and methods and uses therefor |
| HRP20240541T1 (hr) | 2018-10-31 | 2024-07-05 | Gilead Sciences, Inc. | Supstituirani spojevi 6-azabenzimidazola kao inhibitori hpk1 |
| WO2020089811A1 (en) * | 2018-10-31 | 2020-05-07 | Novartis Ag | Dc-sign antibody drug conjugates |
| KR102658602B1 (ko) | 2018-10-31 | 2024-04-19 | 길리애드 사이언시즈, 인코포레이티드 | Hpk1 억제 활성을 갖는 치환된 6-아자벤즈이미다졸 화합물 |
| EP3914263A4 (en) * | 2019-01-22 | 2022-09-21 | Tufts Medical Center, Inc. | METHODS AND COMPOSITIONS FOR THE TREATMENT AND PREVENTION OF EYE DISEASES AND DISORDERS |
| AU2020231115B2 (en) | 2019-03-07 | 2025-02-20 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3'-cyclic dinucleotides and prodrugs thereof |
| DK3934757T3 (da) | 2019-03-07 | 2023-04-17 | Inst Of Organic Chemistry And Biochemistry Ascr V V I | 2'3'-cykliske dinukleotider og prodrugs deraf |
| WO2020178768A1 (en) | 2019-03-07 | 2020-09-10 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator |
| TWI751516B (zh) | 2019-04-17 | 2022-01-01 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
| TW202212339A (zh) | 2019-04-17 | 2022-04-01 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
| US11453681B2 (en) | 2019-05-23 | 2022-09-27 | Gilead Sciences, Inc. | Substituted eneoxindoles and uses thereof |
| US11744876B2 (en) | 2019-06-10 | 2023-09-05 | Sutro Biopharma, Inc. | Immunomodulator antibody drug conjugates and uses thereof |
| CN114269749B (zh) * | 2019-06-10 | 2024-10-01 | 苏特罗生物制药公司 | 5H-吡咯并[3,2-d]嘧啶-2,4-二氨基化合物及其抗体偶联物 |
| WO2021034804A1 (en) | 2019-08-19 | 2021-02-25 | Gilead Sciences, Inc. | Pharmaceutical formulations of tenofovir alafenamide |
| FI4037708T3 (fi) | 2019-09-30 | 2024-10-31 | Gilead Sciences Inc | Hbv-rokotteita ja menetelmiä, hbv:n hoitamiseksi |
| EP4567109A3 (en) | 2019-12-06 | 2025-09-17 | Precision Biosciences, Inc. | Optimized engineered meganucleases having specificity for a recognition sequence in the hepatitis b virus genome |
| EP4097102A1 (en) | 2020-01-27 | 2022-12-07 | Bristol-Myers Squibb Company | 1h-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (tlr7) agonists |
| US20230127326A1 (en) | 2020-01-27 | 2023-04-27 | Bristol-Myers Squibb Company | C3-SUBSTITUTED 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS |
| CN115151548A (zh) | 2020-01-27 | 2022-10-04 | 百时美施贵宝公司 | 作为Toll样受体7(TLR7)激动剂的1H-吡唑并[4,3-d]嘧啶化合物 |
| EP4097105A1 (en) | 2020-01-27 | 2022-12-07 | Bristol-Myers Squibb Company | 1h-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (tlr7) agonists |
| KR20220132590A (ko) * | 2020-01-27 | 2022-09-30 | 브리스톨-마이어스 스큅 컴퍼니 | 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물 |
| CN115135655B (zh) | 2020-01-27 | 2024-07-02 | 百时美施贵宝公司 | 作为Toll样受体7(TLR7)激动剂的1H-吡唑并[4,3-d]嘧啶化合物 |
| CN115151547A (zh) | 2020-01-27 | 2022-10-04 | 百时美施贵宝公司 | 作为Toll样受体7(TLR7)激动剂的1H-吡唑并[4,3-d]嘧啶化合物 |
| EP4097104A1 (en) | 2020-01-27 | 2022-12-07 | Bristol-Myers Squibb Company | 1h-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (tlr7) agonists |
| CN115279765B (zh) | 2020-01-27 | 2024-11-12 | 百时美施贵宝公司 | 作为Toll样受体7(TLR7)激动剂的1H-吡唑并[4,3-d]嘧啶化合物 |
| US11718637B2 (en) | 2020-03-20 | 2023-08-08 | Gilead Sciences, Inc. | Prodrugs of 4′-C-substituted-2-halo-2′- deoxyadenosine nucleosides and methods of making and using the same |
| TW202310852A (zh) | 2021-05-13 | 2023-03-16 | 美商基利科學股份有限公司 | TLR8調節化合物及抗HBV siRNA療法之組合 |
| CN117480155A (zh) | 2021-06-23 | 2024-01-30 | 吉利德科学公司 | 二酰基甘油激酶调节化合物 |
| KR20240005901A (ko) | 2021-06-23 | 2024-01-12 | 길리애드 사이언시즈, 인코포레이티드 | 디아실글리세롤 키나제 조절 화합물 |
| CN117355531A (zh) | 2021-06-23 | 2024-01-05 | 吉利德科学公司 | 二酰基甘油激酶调节化合物 |
| US11999733B2 (en) | 2021-06-23 | 2024-06-04 | Gilead Sciences, Inc. | Diacylglycerol kinase modulating compounds |
| CN113476600B (zh) * | 2021-07-09 | 2023-05-30 | 海南大学 | Avc-29作为疫苗佐剂的用途以及含有该佐剂的疫苗组合物 |
| AR130904A1 (es) * | 2022-10-31 | 2025-01-29 | Astellas Pharma Inc | Conjugado de anticuerpo-fármaco que contiene un compuesto agonista dual del receptor tipo toll 7/8 |
| AU2023403422A1 (en) | 2022-11-30 | 2025-07-17 | Regeneron Pharmaceuticals, Inc. | Tlr7 agonists and antibody-drug-conjugates thereof |
| WO2025240243A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies with bulevirtide and an inhibitory nucleic acid targeting hepatitis b virus |
| WO2025240244A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies comprising bulevirtide and lonafarnib for use in the treatment of hepatitis d virus infection |
| WO2025240242A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies with ribavirin |
| WO2025240246A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies with ribavirin |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE147386T1 (de) | 1991-08-12 | 1997-01-15 | Takeda Chemical Industries Ltd | Kondensierte pyrimidinderivate, ihre herstellung und ihre verwendung als antitumormittel |
| WO1995033752A1 (en) | 1994-06-09 | 1995-12-14 | Smithkline Beecham Corporation | Endothelin receptor antagonists |
| ES2321055T3 (es) | 1999-05-05 | 2009-06-02 | Aventis Pharma Limited | Compuestos biblicos sustituidos. |
| US7968557B2 (en) | 2004-02-14 | 2011-06-28 | Novartis Ag | Substituted pyrrolo[2,3-2]pyrimidines as protein kinase inhibitors |
| JPWO2005092892A1 (ja) | 2004-03-26 | 2008-02-14 | 大日本住友製薬株式会社 | 8−オキソアデニン化合物 |
| WO2005107760A1 (en) * | 2004-04-30 | 2005-11-17 | Irm Llc | Compounds and compositions as inducers of keratinocyte differentiation |
| CN1993362B (zh) * | 2004-06-02 | 2010-12-15 | 武田药品工业株式会社 | 稠合的杂环化合物 |
| AU2005250285B2 (en) | 2004-06-02 | 2011-08-18 | Takeda Pharmaceutical Company Limited | Fused heterocyclic compound |
| CN101500574A (zh) * | 2005-03-15 | 2009-08-05 | Irm责任有限公司 | 用作蛋白激酶抑制剂的化合物和组合物 |
| JPWO2007034917A1 (ja) | 2005-09-22 | 2009-03-26 | 大日本住友製薬株式会社 | 新規なアデニン化合物 |
| CL2008000467A1 (es) | 2007-02-14 | 2008-08-22 | Janssen Pharmaceutica Nv | Compuestos derivados de 2-aminopirimidina, moduladores del receptor histamina h4; su procedimiento de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar un trastorno inflamatorio seleccionado de alegia, asma |
| AU2008271127C1 (en) | 2007-06-29 | 2014-04-17 | Gilead Sciences, Inc. | Purine derivatives and their use as modulators of Toll-like receptor 7 |
| BRPI0908433A2 (pt) | 2008-02-06 | 2019-09-24 | Novartis Ag | pirrolo[2,3-d]piridinas e empregos destas como inibidores tirosina cinase |
| WO2010036928A1 (en) * | 2008-09-26 | 2010-04-01 | Takeda Pharmaceutical Company Limited | Prevention and treatment of cancer with lkb1 non-expression (deletion or mutation) |
| WO2010048149A2 (en) | 2008-10-20 | 2010-04-29 | Kalypsys, Inc. | Heterocyclic modulators of gpr119 for treatment of disease |
| AR074760A1 (es) | 2008-12-18 | 2011-02-09 | Metabolex Inc | Agonistas del receptor gpr120 y usos de los mismos en medicamentos para el tratamiento de diabetes y el sindrome metabolico. |
| WO2010093436A2 (en) * | 2009-02-11 | 2010-08-19 | Carson Dennis A | Toll-like receptor modulators and treatment of diseases |
| WO2010117936A1 (en) | 2009-04-06 | 2010-10-14 | Schering Corporation | Combinations of a hcv inhibitor such as bicyclic pyrrole derivatives and a therapeutic agent |
| WO2011140338A1 (en) | 2010-05-05 | 2011-11-10 | Gatekeeper Pharmaceuticals, Inc. | Compounds that modulate egfr activity and methods for treating or preventing conditions therewith |
| DK2975042T3 (en) * | 2010-06-23 | 2019-01-21 | Hanmi Science Co Ltd | Novel fused pyrimidine derivatives to inhibit tyrosine kinase activity |
| WO2012066336A1 (en) | 2010-11-19 | 2012-05-24 | Astrazeneca Ab | Benzylamine compounds as toll -like receptor 7 agonists |
| EP2570125A1 (en) | 2011-09-16 | 2013-03-20 | Almirall, S.A. | Ep1 receptor ligands |
| US8697888B2 (en) | 2012-01-06 | 2014-04-15 | Vanderbilt University | Substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs as antagonists of muscarinic acetylcholine M1 receptors |
| WO2014056953A1 (en) * | 2012-10-10 | 2014-04-17 | Janssen R&D Ireland | Pyrrolo[3,2-d]pyrimidine derivatives for the treatment of viral infections and other diseases |
| MX362341B (es) * | 2014-05-01 | 2019-01-11 | Novartis Ag | Compuestos y composiciones como agonistas del receptor tipo toll 7. |
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