JP2017514838A5 - - Google Patents
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- JP2017514838A5 JP2017514838A5 JP2016565398A JP2016565398A JP2017514838A5 JP 2017514838 A5 JP2017514838 A5 JP 2017514838A5 JP 2016565398 A JP2016565398 A JP 2016565398A JP 2016565398 A JP2016565398 A JP 2016565398A JP 2017514838 A5 JP2017514838 A5 JP 2017514838A5
- Authority
- JP
- Japan
- Prior art keywords
- pyrrolo
- amino
- methyl
- disease
- pyrimidin
- 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 description 35
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 34
- 201000010099 disease Diseases 0.000 claims description 30
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 28
- 206010028980 Neoplasm Diseases 0.000 claims description 11
- 201000011510 cancer Diseases 0.000 claims description 11
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims description 10
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims description 10
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims description 10
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims description 10
- 208000005176 Hepatitis C Diseases 0.000 claims description 8
- 208000006454 hepatitis Diseases 0.000 claims description 7
- 231100000283 hepatitis Toxicity 0.000 claims description 7
- 125000005842 heteroatom Chemical group 0.000 claims description 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 6
- -1 3-((2-amino-4- (pentylamino) -5H-pyrrolo [3,2-d] pyrimidin-5-yl) methyl) -4-methoxyphenyl Chemical group 0.000 claims description 5
- 208000023275 Autoimmune disease Diseases 0.000 claims description 5
- 206010004146 Basal cell carcinoma Diseases 0.000 claims description 5
- 206010006187 Breast cancer Diseases 0.000 claims description 5
- 208000026310 Breast neoplasm Diseases 0.000 claims description 5
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 5
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 5
- 206010009944 Colon cancer Diseases 0.000 claims description 5
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 5
- 208000011231 Crohn disease Diseases 0.000 claims description 5
- 201000004624 Dermatitis Diseases 0.000 claims description 5
- 201000004681 Psoriasis Diseases 0.000 claims description 5
- 206010039710 Scleroderma Diseases 0.000 claims description 5
- 201000006704 Ulcerative Colitis Diseases 0.000 claims description 5
- 208000024780 Urticaria Diseases 0.000 claims description 5
- 208000036142 Viral infection Diseases 0.000 claims description 5
- 208000009621 actinic keratosis Diseases 0.000 claims description 5
- 208000006673 asthma Diseases 0.000 claims description 5
- 206010006451 bronchitis Diseases 0.000 claims description 5
- 230000000694 effects Effects 0.000 claims description 5
- 208000002672 hepatitis B Diseases 0.000 claims description 5
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 5
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 5
- 208000015181 infectious disease Diseases 0.000 claims description 5
- 208000027866 inflammatory disease Diseases 0.000 claims description 5
- 206010025135 lupus erythematosus Diseases 0.000 claims description 5
- 201000006417 multiple sclerosis Diseases 0.000 claims description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- 208000023504 respiratory system disease Diseases 0.000 claims description 5
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 5
- 230000009385 viral infection Effects 0.000 claims description 5
- DAMMDMFUWSPYOK-FQEVSTJZSA-N (2S)-1-[[4-[[2-amino-4-(pentylamino)pyrrolo[3,2-d]pyrimidin-5-yl]methyl]-3-methoxyphenyl]methyl]pyrrolidine-2-carboxylic acid Chemical compound NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(CN1[C@@H](CCC1)C(=O)O)C=C2)OC)NCCCCC DAMMDMFUWSPYOK-FQEVSTJZSA-N 0.000 claims description 4
- 101000669402 Homo sapiens Toll-like receptor 7 Proteins 0.000 claims description 4
- WPXQRVLICLGUCL-UHFFFAOYSA-N N1N=NN=C1CC=1C=CC(=C(CN2C=CC=3N=C(N=C(C32)NCCCCC)N)C1)OC Chemical compound N1N=NN=C1CC=1C=CC(=C(CN2C=CC=3N=C(N=C(C32)NCCCCC)N)C1)OC WPXQRVLICLGUCL-UHFFFAOYSA-N 0.000 claims description 4
- JPMCLZUWKYUICG-UHFFFAOYSA-N N1N=NN=C1CCC=1C=CC(=C(CN2C=CC=3N=C(N=C(C32)NCCCCC)N)C1)OC Chemical compound N1N=NN=C1CCC=1C=CC(=C(CN2C=CC=3N=C(N=C(C32)NCCCCC)N)C1)OC JPMCLZUWKYUICG-UHFFFAOYSA-N 0.000 claims description 4
- YAPMMXHTJBSLQT-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C(=O)O)C=CC2OC)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C(=O)O)C=CC2OC)NCCCCC YAPMMXHTJBSLQT-UHFFFAOYSA-N 0.000 claims description 4
- DGBUFDBJFRAKLI-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)CC(=O)O)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)CC(=O)O)NCCCCC DGBUFDBJFRAKLI-UHFFFAOYSA-N 0.000 claims description 4
- 206010039085 Rhinitis allergic Diseases 0.000 claims description 4
- 102100039390 Toll-like receptor 7 Human genes 0.000 claims description 4
- 201000010105 allergic rhinitis Diseases 0.000 claims description 4
- 210000004027 cell Anatomy 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 230000002062 proliferating effect Effects 0.000 claims description 4
- 206010005003 Bladder cancer Diseases 0.000 claims description 3
- 208000035473 Communicable disease Diseases 0.000 claims description 3
- YATPCANSKUAXLN-HXUWFJFHSA-N NC=1N=C(C2=C(N1)C=CN2CC=2C=C(CN1[C@H](CCC1)C(=O)O)C=CC2OC)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC=2C=C(CN1[C@H](CCC1)C(=O)O)C=CC2OC)NCCCCC YATPCANSKUAXLN-HXUWFJFHSA-N 0.000 claims description 3
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 3
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 3
- XBPWCXCQZZVVDJ-UHFFFAOYSA-N C(CCCCC)NC=1C2=C(N=C(N1)N)C=CN2CC2=C(C=CC(=C2)C2=NN=NN2)OC Chemical compound C(CCCCC)NC=1C2=C(N=C(N1)N)C=CN2CC2=C(C=CC(=C2)C2=NN=NN2)OC XBPWCXCQZZVVDJ-UHFFFAOYSA-N 0.000 claims description 2
- ZMXZKMDODWPMFT-UHFFFAOYSA-N COC1=C(CN2C=CC=3N=C(N=C(C32)NCCCCC)N)C=C(C=C1)C1=NN=NN1 Chemical compound COC1=C(CN2C=CC=3N=C(N=C(C32)NCCCCC)N)C=C(C=C1)C1=NN=NN1 ZMXZKMDODWPMFT-UHFFFAOYSA-N 0.000 claims description 2
- BIQPCKWQIOGLRO-UHFFFAOYSA-N COC1=C(CN2C=CC=3N=C(N=C(C32)NCCCCC)N)C=CC(=C1)C1=NN=NN1 Chemical compound COC1=C(CN2C=CC=3N=C(N=C(C32)NCCCCC)N)C=CC(=C1)C1=NN=NN1 BIQPCKWQIOGLRO-UHFFFAOYSA-N 0.000 claims description 2
- LERPKRPELMLJGL-UHFFFAOYSA-N FC(C=1C=CC(=C(CN2C=CC=3N=C(N=C(C32)NCCCCC)N)C1)OC)(C1=NN=NN1)F Chemical compound FC(C=1C=CC(=C(CN2C=CC=3N=C(N=C(C32)NCCCCC)N)C1)OC)(C1=NN=NN1)F LERPKRPELMLJGL-UHFFFAOYSA-N 0.000 claims description 2
- MHHIXFORUFMUNC-UHFFFAOYSA-N N1N=NN=C1C(C)(C)C=1C=CC(=C(CN2C=CC=3N=C(N=C(C32)NCCCCC)N)C1)OC Chemical class N1N=NN=C1C(C)(C)C=1C=CC(=C(CN2C=CC=3N=C(N=C(C32)NCCCCC)N)C1)OC MHHIXFORUFMUNC-UHFFFAOYSA-N 0.000 claims description 2
- ZJCMDZVSGDFLGB-KRWDZBQOSA-N N1N=NN=C1C(C)(C)C=1C=CC(=C(CN2C=CC=3N=C(N=C(C32)N[C@H](CO)CCCC)N)C1)OC Chemical compound N1N=NN=C1C(C)(C)C=1C=CC(=C(CN2C=CC=3N=C(N=C(C32)N[C@H](CO)CCCC)N)C1)OC ZJCMDZVSGDFLGB-KRWDZBQOSA-N 0.000 claims description 2
- LDGLRXLZQXFAQH-HNNXBMFYSA-N N1N=NN=C1CC=1C=CC(=C(CN2C=CC=3N=C(N=C(C32)N[C@H](CO)CCC)N)C1)OC Chemical compound N1N=NN=C1CC=1C=CC(=C(CN2C=CC=3N=C(N=C(C32)N[C@H](CO)CCC)N)C1)OC LDGLRXLZQXFAQH-HNNXBMFYSA-N 0.000 claims description 2
- QTGPSLBHJHDMAA-INIZCTEOSA-N N1N=NN=C1CC=1C=CC(=C(CN2C=CC=3N=C(N=C(C32)N[C@H](CO)CCCC)N)C1)OC Chemical compound N1N=NN=C1CC=1C=CC(=C(CN2C=CC=3N=C(N=C(C32)N[C@H](CO)CCCC)N)C1)OC QTGPSLBHJHDMAA-INIZCTEOSA-N 0.000 claims description 2
- VHPPHGRMEQLRTI-UHFFFAOYSA-N N1N=NN=C1COC=1C=CC(=C(CN2C=CC=3N=C(N=C(C32)NCCCCC)N)C1)OC Chemical compound N1N=NN=C1COC=1C=CC(=C(CN2C=CC=3N=C(N=C(C32)NCCCCC)N)C1)OC VHPPHGRMEQLRTI-UHFFFAOYSA-N 0.000 claims description 2
- YEGDWVRORNWXCA-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(OCC(=O)O)C=C2)OC)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC2=C(C=C(OCC(=O)O)C=C2)OC)NCCCCC YEGDWVRORNWXCA-UHFFFAOYSA-N 0.000 claims description 2
- LNDUPESSOYMSJP-HNNXBMFYSA-N NC=1N=C(C2=C(N1)C=CN2CC2=C(C=CC(=C2)C2=NN=NN2)OC)N[C@H](CO)CCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC2=C(C=CC(=C2)C2=NN=NN2)OC)N[C@H](CO)CCCC LNDUPESSOYMSJP-HNNXBMFYSA-N 0.000 claims description 2
- XNZLVNCYIWAOFE-VQHVLOKHSA-N NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)/C=C/C(=O)O)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)/C=C/C(=O)O)NCCCCC XNZLVNCYIWAOFE-VQHVLOKHSA-N 0.000 claims description 2
- YIHAVTSAPRGDNW-INIZCTEOSA-N NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)CC(=O)O)N[C@H](CO)CCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)CC(=O)O)N[C@H](CO)CCCC YIHAVTSAPRGDNW-INIZCTEOSA-N 0.000 claims description 2
- YVHVMLRGFSLIND-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)CCC(=O)O)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)CCC(=O)O)NCCCCC YVHVMLRGFSLIND-UHFFFAOYSA-N 0.000 claims description 2
- NNOMZLJTXKTXQJ-KRWDZBQOSA-N NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)CCC(=O)O)N[C@H](CO)CCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)CCC(=O)O)N[C@H](CO)CCCC NNOMZLJTXKTXQJ-KRWDZBQOSA-N 0.000 claims description 2
- AJLRGBCKWKXKJK-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)P(O)(O)=O)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC=2C=C(C=CC2OC)P(O)(O)=O)NCCCCC AJLRGBCKWKXKJK-UHFFFAOYSA-N 0.000 claims description 2
- MKYWYRKMBXGWJU-UHFFFAOYSA-N NC=1N=C(C2=C(N1)C=CN2CC=2C=C(CC=1N=NN(N1)CC(=O)O)C=CC2OC)NCCCCC Chemical compound NC=1N=C(C2=C(N1)C=CN2CC=2C=C(CC=1N=NN(N1)CC(=O)O)C=CC2OC)NCCCCC MKYWYRKMBXGWJU-UHFFFAOYSA-N 0.000 claims description 2
- FVQOAYDCQJAKTH-WOJBJXKFSA-N NC=1N=C(C2=C(N=1)C=CN2CC=1C=C(C=CC=1OC)CC[C@H](C[C@H](CC(=O)O)O)O)NCCCCC Chemical compound NC=1N=C(C2=C(N=1)C=CN2CC=1C=C(C=CC=1OC)CC[C@H](C[C@H](CC(=O)O)O)O)NCCCCC FVQOAYDCQJAKTH-WOJBJXKFSA-N 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 description 14
- 238000000034 method Methods 0.000 description 8
- 208000005440 Basal Cell Neoplasms Diseases 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- 108010060825 Toll-Like Receptor 7 Proteins 0.000 description 1
- 102000008236 Toll-Like Receptor 7 Human genes 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- 150000001735 carboxylic acids Chemical class 0.000 description 1
- 230000004663 cell proliferation Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 206010039083 rhinitis Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461987321P | 2014-05-01 | 2014-05-01 | |
| US61/987,321 | 2014-05-01 | ||
| PCT/US2015/028264 WO2015168269A1 (en) | 2014-05-01 | 2015-04-29 | Compounds and compositions as toll-like receptor 7 agonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017514838A JP2017514838A (ja) | 2017-06-08 |
| JP2017514838A5 true JP2017514838A5 (enExample) | 2018-04-05 |
| JP6484253B2 JP6484253B2 (ja) | 2019-03-13 |
Family
ID=53284501
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016565398A Active JP6484253B2 (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 (30)
| Country | Link |
|---|---|
| US (1) | US9902730B2 (enExample) |
| EP (1) | EP3137470B1 (enExample) |
| JP (1) | JP6484253B2 (enExample) |
| KR (1) | KR102139847B1 (enExample) |
| CN (1) | CN106232603B (enExample) |
| AP (1) | AP2016009485A0 (enExample) |
| AR (1) | AR100244A1 (enExample) |
| AU (1) | AU2015253215B2 (enExample) |
| BR (1) | BR112016025423A2 (enExample) |
| CA (1) | CA2946408C (enExample) |
| CL (1) | CL2016002751A1 (enExample) |
| CR (1) | CR20160512A (enExample) |
| CU (1) | CU24401B1 (enExample) |
| DO (1) | DOP2016000295A (enExample) |
| EA (1) | EA030603B1 (enExample) |
| ES (1) | ES2877050T3 (enExample) |
| GT (1) | GT201600233A (enExample) |
| IL (1) | IL248347B (enExample) |
| MX (1) | MX362341B (enExample) |
| NI (1) | NI201600164A (enExample) |
| NZ (1) | NZ724792A (enExample) |
| PE (1) | PE20170325A1 (enExample) |
| PH (1) | PH12016501966A1 (enExample) |
| PL (1) | PL3137470T3 (enExample) |
| PT (1) | PT3137470T (enExample) |
| SG (1) | SG11201608161VA (enExample) |
| SV (1) | SV2016005311A (enExample) |
| TW (1) | TWI666212B (enExample) |
| UY (1) | UY36103A (enExample) |
| WO (1) | WO2015168269A1 (enExample) |
Families Citing this family (67)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015168279A1 (en) | 2014-05-01 | 2015-11-05 | Novartis Ag | Compounds and compositions as toll-like receptor 7 agonists |
| LT3190113T (lt) | 2014-08-15 | 2021-08-25 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Pirolopirimidino junginiai, naudotini kaip tlr7 agonistai |
| PL3097102T3 (pl) | 2015-03-04 | 2018-04-30 | Gilead Sciences Inc | Związki 4,6-diamino-pirydo[3,2-d]pirymidyny modulujące działanie receptora toll-podobnego |
| SG10201912699RA (en) | 2015-07-20 | 2020-02-27 | Genzyme Corp | Colony stimulating factor-1 receptor (csf-1r) inhibitors |
| CN108430515B (zh) | 2015-10-29 | 2021-11-12 | 诺华股份有限公司 | 包含toll-样受体激动剂的抗体缀合物 |
| 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 |
| CN107043379A (zh) * | 2016-02-05 | 2017-08-15 | 正大天晴药业集团股份有限公司 | 一种tlr7激动剂的晶型a、其制备方法和医药用途 |
| CN107043378A (zh) * | 2016-02-05 | 2017-08-15 | 正大天晴药业集团股份有限公司 | 一种吡咯并[3,2-d]嘧啶类化合物的制备方法及其中间体 |
| ES2826748T3 (es) | 2016-09-02 | 2021-05-19 | Gilead Sciences Inc | Derivados de 4,6-diamino-pirido[3,2-d]pirimidina como moduladores de receptores de tipo Toll |
| KR102268448B1 (ko) | 2016-09-02 | 2021-06-22 | 길리애드 사이언시즈, 인코포레이티드 | 톨 유사 수용체 조정제 화합물 |
| MA46535A (fr) | 2016-10-14 | 2019-08-21 | Prec Biosciences Inc | Méganucléases modifiées spécifiques de séquences de reconnaissance dans le génome du virus de l'hépatite b |
| CN106727768A (zh) * | 2017-02-06 | 2017-05-31 | 灞卞嘲 | 一种治疗子宫内膜炎的药物组合物 |
| 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 |
| 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 |
| 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 |
| 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 |
| EP3690030A4 (en) | 2017-09-28 | 2021-06-23 | Industry-Academic Cooperation Foundation, Yonsei University | METHOD FOR MANUFACTURING MYELOID-DERIVED SUPPRESSOR CELLS, SUPPRESSOR CELLS MANUFACTURED FROM MYEOLID 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 |
| EP3728283B1 (en) | 2017-12-20 | 2023-11-22 | Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. | 3'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein |
| KR102526964B1 (ko) | 2018-02-26 | 2023-04-28 | 길리애드 사이언시즈, 인코포레이티드 | Hbv 복제 억제제로서의 치환된 피롤리진 화합물 |
| WO2019195181A1 (en) | 2018-04-05 | 2019-10-10 | Gilead Sciences, Inc. | Antibodies and fragments thereof that bind hepatitis b virus protein x |
| 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 |
| 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 |
| 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 |
| 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 |
| WO2019209811A1 (en) | 2018-04-24 | 2019-10-31 | 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 |
| WO2019223788A1 (zh) * | 2018-05-25 | 2019-11-28 | 正大天晴药业集团股份有限公司 | 用于治疗肺癌的tlr7激动剂及其药物组合 |
| 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 |
| KR102658602B1 (ko) | 2018-10-31 | 2024-04-19 | 길리애드 사이언시즈, 인코포레이티드 | Hpk1 억제 활성을 갖는 치환된 6-아자벤즈이미다졸 화합물 |
| FI3873903T3 (fi) | 2018-10-31 | 2024-03-26 | Gilead Sciences Inc | Substituoituja 6-azabentsiimidatsoliyhdisteitä HPK1-inhibiittoreina |
| CA3120866A1 (en) * | 2018-11-30 | 2020-06-04 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
| EP3934757B1 (en) | 2019-03-07 | 2023-02-22 | Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. | 2'3'-cyclic dinucleotides and prodrugs thereof |
| CA3129011C (en) | 2019-03-07 | 2023-12-19 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3'-cyclic dinucleotides and prodrugs thereof |
| EP3935065A1 (en) | 2019-03-07 | 2022-01-12 | Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. | 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator |
| HUE064377T2 (hu) | 2019-04-12 | 2024-03-28 | Riboscience Llc | Biciklusos heteroaril-származékok mint ektonukleotid pirofoszfatáz foszfodiészteráz 1 inhibitorok |
| TWI751517B (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 |
| TW202210480A (zh) | 2019-04-17 | 2022-03-16 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
| TWI826690B (zh) | 2019-05-23 | 2023-12-21 | 美商基利科學股份有限公司 | 經取代之烯吲哚酮化物及其用途 |
| US12534465B2 (en) * | 2019-06-10 | 2026-01-27 | Sutro Biopharma, Inc. | 5H-pyrrolo[3,2-d]pyrimidine-2,4-diamino compounds and antibody conjugates thereof |
| TWI879779B (zh) | 2019-06-28 | 2025-04-11 | 美商基利科學股份有限公司 | 類鐸受體調節劑化合物的製備方法 |
| WO2021034804A1 (en) | 2019-08-19 | 2021-02-25 | Gilead Sciences, Inc. | Pharmaceutical formulations of tenofovir alafenamide |
| KR20220074917A (ko) | 2019-09-30 | 2022-06-03 | 길리애드 사이언시즈, 인코포레이티드 | Hbv 백신 및 hbv를 치료하는 방법 |
| DK4069729T3 (da) | 2019-12-06 | 2025-04-07 | Prec Biosciences Inc | Optimerede, modificerede meganukleaser med specificitet for en genkendelsessekvens i hepatitis b-virusgenomet |
| 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 |
| KR20220132591A (ko) | 2020-01-27 | 2022-09-30 | 브리스톨-마이어스 스큅 컴퍼니 | 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물 |
| WO2021154668A1 (en) | 2020-01-27 | 2021-08-05 | 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 |
| WO2021154662A1 (en) | 2020-01-27 | 2021-08-05 | 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 |
| 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 |
| KR20220132594A (ko) | 2020-01-27 | 2022-09-30 | 브리스톨-마이어스 스큅 컴퍼니 | 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물 |
| KR20220132592A (ko) | 2020-01-27 | 2022-09-30 | 브리스톨-마이어스 스큅 컴퍼니 | 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물 |
| AR121620A1 (es) | 2020-03-20 | 2022-06-22 | Gilead Sciences Inc | Profármacos de nucleósidos 4-c-sustituidos-2-halo-2-deoxiadenosina y métodos de preparación y uso de los mismos |
| EP4267573A1 (en) | 2020-12-23 | 2023-11-01 | Genzyme Corporation | Deuterated colony stimulating factor-1 receptor (csf-1r) inhibitors |
| EP4337223A1 (en) | 2021-05-13 | 2024-03-20 | Gilead Sciences, Inc. | Combination of a tlr8 modulating compound and anti-hbv sirna therapeutics |
| KR20240005901A (ko) | 2021-06-23 | 2024-01-12 | 길리애드 사이언시즈, 인코포레이티드 | 디아실글리세롤 키나제 조절 화합물 |
| AU2022299051B2 (en) | 2021-06-23 | 2025-03-13 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| KR20240025616A (ko) | 2021-06-23 | 2024-02-27 | 길리애드 사이언시즈, 인코포레이티드 | 다이아실글리세롤 키나제 조절 화합물 |
| AU2022298639C1 (en) | 2021-06-23 | 2025-07-17 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| 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 |
| US20250345389A1 (en) | 2024-05-13 | 2025-11-13 | Gilead Sciences, Inc. | Combination therapies |
| WO2025240246A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies with ribavirin |
| WO2025240242A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies with ribavirin |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE69216509T2 (de) * | 1991-08-12 | 1997-05-28 | Takeda Chemical Industries Ltd | Kondensierte Pyrimidinderivate, ihre Herstellung und ihre Verwendung als Antitumormittel |
| EP0766684A4 (en) | 1994-06-09 | 1997-07-16 | Smithkline Beecham Corp | ENDOTHELINE RECEPTOR ANTAGONISTS |
| CA2372840C (en) | 1999-05-05 | 2008-07-22 | Aventis Pharma Limited | Substituted bicyclic compounds |
| CN1918158B (zh) * | 2004-02-14 | 2011-03-02 | Irm责任有限公司 | 作为蛋白激酶抑制剂的化合物和组合物 |
| 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 |
| MEP8409A (en) | 2004-06-02 | 2011-12-20 | Fused heterocyclic compound | |
| MX2007011316A (es) * | 2005-03-15 | 2007-11-12 | Irm Llc | Compuestos y composiciones como inhibidores de cinasa de proteina. |
| EP1939201A4 (en) * | 2005-09-22 | 2010-06-16 | Dainippon Sumitomo Pharma Co | NEW ADENINE CONNECTION |
| JP5395068B2 (ja) * | 2007-06-29 | 2014-01-22 | ギリアード サイエンシーズ， インコーポレイテッド | トール様受容体７の調節物質としてのプリン誘導体およびその使用 |
| CN101981036B (zh) | 2008-02-06 | 2013-09-04 | 诺瓦提斯公司 | 吡咯并[2,3-d]嘧啶及其作为酪氨酸激酶抑制剂的用途 |
| 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. |
| US20130137709A1 (en) | 2010-05-05 | 2013-05-30 | Nathanael S. Gray | Compounds that modulate EGFR activity and methods for treating or preventing conditions therewith |
| MX342164B (es) | 2010-06-23 | 2016-09-19 | Hanmi Science Co Ltd | Derivados de pirimidina fusionados novedosos para la inhibicion de la actividad de tirosina cinasa. |
| 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 |
| NZ705589A (en) * | 2012-10-10 | 2019-05-31 | Janssen Sciences Ireland Uc | Pyrrolo[3,2-d]pyrimidine derivatives for the treatment of viral infections and other diseases |
| WO2015168279A1 (en) | 2014-05-01 | 2015-11-05 | Novartis Ag | Compounds and compositions as toll-like receptor 7 agonists |
| TW201632515A (zh) | 2015-01-23 | 2016-09-16 | 協友股份有限公司 | 經取代之吡唑吡唑衍生物及其作爲除草劑的用途 |
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