JPWO2021154669A5 - - Google Patents
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- Publication number
- JPWO2021154669A5 JPWO2021154669A5 JP2022545792A JP2022545792A JPWO2021154669A5 JP WO2021154669 A5 JPWO2021154669 A5 JP WO2021154669A5 JP 2022545792 A JP2022545792 A JP 2022545792A JP 2022545792 A JP2022545792 A JP 2022545792A JP WO2021154669 A5 JPWO2021154669 A5 JP WO2021154669A5
- Authority
- JP
- Japan
- Prior art keywords
- alkanediyl
- alkyl
- cancer
- formula
- cycloalkyl
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims 12
- -1 NH (C 1 -C 5 alkyl) Chemical group 0.000 claims 4
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 claims 4
- 150000001602 bicycloalkyls Chemical group 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 230000001093 anti-cancer Effects 0.000 claims 3
- 239000002955 immunomodulating agent Substances 0.000 claims 3
- 125000006729 (C2-C5) alkenyl group Chemical group 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 201000000849 skin cancer Diseases 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 229940045513 CTLA4 antagonist Drugs 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 229960005386 ipilimumab Drugs 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 229960003301 nivolumab Drugs 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 229960002621 pembrolizumab Drugs 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 201000000498 stomach carcinoma Diseases 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 206010044412 transitional cell carcinoma Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202062966137P | 2020-01-27 | 2020-01-27 | |
| US62/966,137 | 2020-01-27 | ||
| US202063058144P | 2020-07-29 | 2020-07-29 | |
| US63/058,144 | 2020-07-29 | ||
| PCT/US2021/014983 WO2021154669A1 (en) | 2020-01-27 | 2021-01-26 | 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2023512208A JP2023512208A (ja) | 2023-03-24 |
| JPWO2021154669A5 true JPWO2021154669A5 (ko) | 2024-02-02 |
Family
ID=74669538
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022545792A Pending JP2023512208A (ja) | 2020-01-27 | 2021-01-26 | トール様受容体７（ＴＬＲ７）アゴニストとしての１Ｈ－ピラゾロ［４，３－ｄ］ピリミジン化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20230144824A1 (ko) |
| EP (1) | EP4097108A1 (ko) |
| JP (1) | JP2023512208A (ko) |
| KR (1) | KR20220132602A (ko) |
| CN (1) | CN115279765A (ko) |
| WO (1) | WO2021154669A1 (ko) |
Family Cites Families (51)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU698419B2 (en) | 1996-07-03 | 1998-10-29 | Dainippon Sumitomo Pharma Co., Ltd. | A novel purine derivative |
| TW572758B (en) | 1997-12-22 | 2004-01-21 | Sumitomo Pharma | Type 2 helper T cell-selective immune response inhibitors comprising purine derivatives |
| JP4331944B2 (ja) | 2001-04-17 | 2009-09-16 | 大日本住友製薬株式会社 | 新規アデニン誘導体 |
| EP2336133A1 (en) | 2001-10-30 | 2011-06-22 | Conforma Therapeutics Corporation | Purine analogs having HSP90-inhibiting activity |
| US7754728B2 (en) | 2002-09-27 | 2010-07-13 | Dainippon Sumitomo Pharma Co., Ltd. | Adenine compound and use thereof |
| JP2004137157A (ja) | 2002-10-16 | 2004-05-13 | Sumitomo Pharmaceut Co Ltd | 新規アデニン誘導体を有効成分として含有する医薬 |
| US20070225303A1 (en) | 2004-03-26 | 2007-09-27 | Haruhisa Ogita | 8-Oxoadenine Compound |
| EA200702235A1 (ru) | 2005-05-04 | 2008-04-28 | Пфайзер Лимитед | Производные 2-амидо-6-амино-8-оксопурина в качестве модуляторов toll-подобных рецепторов для лечения рака и вирусных инфекций, таких как гепатит с |
| EA200800396A1 (ru) | 2005-09-02 | 2008-08-29 | Пфайзер Инк. | Гидроксизамещенные 1н-имидазопиридины и способы |
| WO2007034817A1 (ja) | 2005-09-22 | 2007-03-29 | Dainippon Sumitomo Pharma Co., Ltd. | 新規アデニン化合物 |
| US20090105212A1 (en) | 2005-09-22 | 2009-04-23 | Dainippon Sumitomo Pharma Co., Ltd. a corporation of Japan | Novel adenine compound |
| ATE532784T1 (de) | 2006-02-17 | 2011-11-15 | Pfizer Ltd | 3-deazapurinderivate als tlr7-modulatoren |
| SI2510946T1 (sl) | 2007-02-07 | 2015-12-31 | The Regents Of The University Of California | Konjugati sintetičnih agonistov TLR in njihove uporabe |
| PE20081887A1 (es) | 2007-03-20 | 2009-01-16 | Dainippon Sumitomo Pharma Co | Nuevo compuesto de adenina |
| WO2008118454A2 (en) | 2007-03-23 | 2008-10-02 | Amgen Inc. | Derivatives of quinoline or benzopyrazine and their uses for the treatment of (inter alia) inflammatory diseases, autoimmune diseases or various kinds of cancer |
| MX2009013832A (es) | 2007-06-29 | 2010-03-10 | Gilead Sciences Inc | Derivados de purina y su uso como moduladores del receptor 7 similar a un puente. |
| ATE501136T1 (de) | 2007-08-03 | 2011-03-15 | Pfizer Ltd | Imidazopyridinone |
| ES2623794T3 (es) | 2008-12-09 | 2017-07-12 | Gilead Sciences, Inc. | Intermedios para la preparación de moduladores de receptores tipo toll |
| MX2011008500A (es) | 2009-02-11 | 2011-09-26 | Univ California | Moduladores del receptor tipo toll y tratamiento de enfermedades. |
| CN102666541B (zh) | 2009-10-22 | 2015-11-25 | 吉里德科学公司 | 用于治疗特别是病毒感染的嘌呤或脱氮嘌呤的衍生物 |
| KR20130056249A (ko) | 2010-04-30 | 2013-05-29 | 텔로메딕스 에스에이 | 인지질 약물 유사체 |
| AU2011247359A1 (en) | 2010-04-30 | 2012-11-15 | Telormedix Sa | Methods for inducing an immune response |
| US20130202629A1 (en) | 2010-04-30 | 2013-08-08 | The Regents Of The University Of California | Uses of phospholipid conjugates of synthetic tlr7 agonists |
| US20120083473A1 (en) | 2010-09-21 | 2012-04-05 | Johanna Holldack | Treatment of conditions by toll-like receptor modulators |
| US20120231023A1 (en) | 2011-03-08 | 2012-09-13 | Baylor Research Institute | Novel Vaccine Adjuvants Based on Targeting Adjuvants to Antibodies Directly to Antigen-Presenting Cells |
| PT2776439T (pt) | 2011-11-09 | 2018-11-02 | Janssen Sciences Ireland Uc | Derivados de purina para o tratamento de infeções virais |
| AU2013288600B2 (en) | 2012-07-13 | 2017-06-29 | Janssen Sciences Ireland Uc | Macrocyclic purines for the treatment of viral infections |
| UA114109C2 (xx) | 2012-08-24 | 2017-04-25 | Піразолопіримідинові сполуки | |
| KR102217111B1 (ko) | 2012-10-10 | 2021-02-18 | 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 | 바이러스 감염 및 다른 질환 치료를 위한 피롤로[3,2-d]피리미딘 유도체 |
| EP2732825B1 (en) | 2012-11-19 | 2015-07-01 | Invivogen | Conjugates of a TLR7 and/or TLR8 agonist and a TLR2 agonist |
| US9295732B2 (en) | 2013-02-22 | 2016-03-29 | Invivogen | Conjugated TLR7 and/or TLR8 and TLR2 polycationic agonists |
| EA202090547A3 (ru) | 2013-03-29 | 2020-12-30 | Янссен Сайенсиз Айрлэнд Юси | Макроциклические деаза-оксипурины для лечения вирусных инфекций |
| SG10201803331PA (en) | 2013-06-27 | 2018-06-28 | Janssen Sciences Ireland Uc | Pyrrolo[3,2-d]pyrimidine derivatives for the treatment of viral infections and other diseases |
| EP3033089A2 (en) | 2013-08-16 | 2016-06-22 | The Regents of The University of California | Uses of phospholipid conjugates of synthetic tlr7 agonists |
| WO2015036044A1 (en) | 2013-09-13 | 2015-03-19 | Telormedix Sa | Cationic lipid vehicles for delivery of tlr7 agonists for specific targeting of human cd14+ monocytes in whole blood |
| MX362341B (es) | 2014-05-01 | 2019-01-11 | Novartis Ag | Compuestos y composiciones como agonistas del receptor tipo toll 7. |
| KR20160144399A (ko) | 2014-05-01 | 2016-12-16 | 노파르티스 아게 | 톨-유사 수용체 7 효능제로서의 화합물 및 조성물 |
| 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 |
| CN108349982B (zh) | 2015-11-05 | 2020-05-05 | 正大天晴药业集团股份有限公司 | 作为tlr7激动剂的7-(噻唑-5-基)吡咯并嘧啶化合物 |
| KR102472198B1 (ko) | 2016-06-16 | 2022-11-28 | 얀센 파마슈티카 엔.브이. | Pi3k 베타 저해제로서의 아자벤즈이미다졸 유도체 |
| MY192084A (en) | 2016-11-28 | 2022-07-26 | Jiangsu Hengrui Medicine Co | Pyrazolo-heteroaryl derivative, preparation method and medical use thereof |
| 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 |
| 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 |
| 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 |
| JP7506981B2 (ja) | 2017-12-21 | 2024-06-27 | 住友ファーマ株式会社 | Ｔｌｒ７アゴニストを含む併用薬 |
| US11485741B2 (en) | 2018-04-24 | 2022-11-01 | Bristol-Myers Squibb Company | Macrocyclic toll-like receptor 7 (TLR7) agonists |
| 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 |
-
2021
- 2021-01-26 CN CN202180020862.9A patent/CN115279765A/zh active Pending
- 2021-01-26 EP EP21706770.1A patent/EP4097108A1/en active Pending
- 2021-01-26 JP JP2022545792A patent/JP2023512208A/ja active Pending
- 2021-01-26 KR KR1020227029361A patent/KR20220132602A/ko unknown
- 2021-01-26 WO PCT/US2021/014983 patent/WO2021154669A1/en unknown
- 2021-01-26 US US17/793,248 patent/US20230144824A1/en active Pending
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