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.)
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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
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- 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
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- 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
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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 (cg-RX-API-DMAC7.html) | 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)
Families Citing this family (67)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2908150T3 (es) * | 2014-05-01 | 2022-04-27 | Novartis Ag | Compuestos y composiciones como agonistas del receptor de tipo Toll 7 |
| EA032824B1 (ru) | 2014-08-15 | 2019-07-31 | Чиа Тай Тяньцин Фармасьютикал Груп Ко., Лтд. | Пирролопиримидиновые соединения, используемые в качестве агониста tlr7 |
| PH12021551982A1 (en) | 2015-03-04 | 2022-09-05 | Gilead Sciences Inc | Toll-like receptor modulating 4,6-diamino-pyrido[3,2-d]pyrimidine compounds |
| IL305843B2 (en) | 2015-07-20 | 2025-01-01 | Genzyme Corp | CSF-1R receptor antibodies |
| MA44334A (fr) | 2015-10-29 | 2018-09-05 | Novartis Ag | Conjugués d'anticorps comprenant un agoniste du récepteur de type toll |
| 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 |
| 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 |
| 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 |
| US10370342B2 (en) | 2016-09-02 | 2019-08-06 | Gilead Sciences, Inc. | Toll like receptor modulator compounds |
| US10640499B2 (en) | 2016-09-02 | 2020-05-05 | Gilead Sciences, Inc. | Toll like receptor modulator compounds |
| PE20191353A1 (es) | 2016-10-14 | 2019-10-01 | Prec Biosciences Inc | Meganucleasas disenadas especificamente para el reconocimiento de secuencias en el genoma del virus de la hepatitis 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 |
| 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 |
| 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 |
| 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 |
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| 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 |
| AU2018392213B2 (en) | 2017-12-20 | 2021-03-04 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3' cyclic dinucleotides with phosphonate bond activating the STING adaptor protein |
| JP7098748B2 (ja) | 2017-12-20 | 2022-07-11 | インスティチュート オブ オーガニック ケミストリー アンド バイオケミストリー エーエスシーアール，ヴイ．ヴイ．アイ． | Ｓｔｉｎｇアダプタータンパク質を活性化するホスホン酸結合を有する２’３’環状ジヌクレオチド |
| AU2019223182B2 (en) | 2018-02-26 | 2021-08-19 | Gilead Sciences, Inc. | Substituted pyrrolizine compounds as HBV replication inhibitors |
| US10870691B2 (en) | 2018-04-05 | 2020-12-22 | 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 |
| 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 |
| US11142750B2 (en) | 2018-04-12 | 2021-10-12 | Precision Biosciences, Inc. | Optimized engineered meganucleases having specificity for a recognition sequence in the Hepatitis B virus genome |
| 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 |
| EP3816166A4 (en) * | 2018-05-25 | 2022-04-06 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Tlr7 agonist and pharmaceutical combination thereof for treating lung cancer |
| 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 |
| TWI721624B (zh) | 2018-10-31 | 2021-03-11 | 美商基利科學股份有限公司 | 經取代之6-氮雜苯并咪唑化合物 |
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| JP7530360B2 (ja) * | 2018-11-30 | 2024-08-07 | 武田薬品工業株式会社 | Ｔｙｋ２阻害剤およびその使用 |
| 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 |
| AU2020231201B2 (en) | 2019-03-07 | 2025-02-20 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2'3'-cyclic dinucleotides and prodrugs thereof |
| 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 |
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