JP2019510787A5 - - Google Patents
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- JP2019510787A5 JP2019510787A5 JP2018552246A JP2018552246A JP2019510787A5 JP 2019510787 A5 JP2019510787 A5 JP 2019510787A5 JP 2018552246 A JP2018552246 A JP 2018552246A JP 2018552246 A JP2018552246 A JP 2018552246A JP 2019510787 A5 JP2019510787 A5 JP 2019510787A5
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- Prior art keywords
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- cyclic
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- 125000000217 alkyl group Chemical group 0.000 claims description 150
- 125000003277 amino group Chemical group 0.000 claims description 80
- 150000003839 salts Chemical class 0.000 claims description 73
- 229910052717 sulfur Inorganic materials 0.000 claims description 68
- 229910052739 hydrogen Inorganic materials 0.000 claims description 64
- 239000001257 hydrogen Substances 0.000 claims description 64
- 150000001875 compounds Chemical class 0.000 claims description 62
- 125000005843 halogen group Chemical group 0.000 claims description 60
- 125000003396 thiol group Chemical group [H]S* 0.000 claims description 55
- 150000002431 hydrogen Chemical group 0.000 claims description 53
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 51
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims description 50
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 44
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 44
- 125000005113 hydroxyalkoxy group Chemical group 0.000 claims description 44
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 42
- 125000003545 alkoxy group Chemical group 0.000 claims description 41
- 125000004076 pyridyl group Chemical group 0.000 claims description 41
- 125000003342 alkenyl group Chemical group 0.000 claims description 40
- 229910052760 oxygen Inorganic materials 0.000 claims description 40
- 125000000304 alkynyl group Chemical group 0.000 claims description 38
- 125000002883 imidazolyl group Chemical group 0.000 claims description 38
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 38
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims description 33
- 125000001624 naphthyl group Chemical group 0.000 claims description 33
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 33
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 33
- 125000000335 thiazolyl group Chemical group 0.000 claims description 33
- 125000001399 1,2,3-triazolyl group Chemical group N1N=NC(=C1)* 0.000 claims description 30
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 27
- 229910052736 halogen Inorganic materials 0.000 claims description 26
- 150000002367 halogens Chemical class 0.000 claims description 26
- 125000001424 substituent group Chemical group 0.000 claims description 21
- 201000010099 disease Diseases 0.000 claims description 17
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 17
- 239000008194 pharmaceutical composition Substances 0.000 claims description 16
- 150000001540 azides Chemical class 0.000 claims description 15
- 229910052799 carbon Inorganic materials 0.000 claims description 12
- 229910052757 nitrogen Inorganic materials 0.000 claims description 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 11
- 239000002253 acid Substances 0.000 claims description 11
- 125000005360 alkyl sulfoxide group Chemical group 0.000 claims description 11
- 125000004422 alkyl sulphonamide group Chemical group 0.000 claims description 11
- 125000005012 alkyl thioether group Chemical group 0.000 claims description 11
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 11
- 125000003386 piperidinyl group Chemical group 0.000 claims description 11
- 239000012453 solvate Substances 0.000 claims description 11
- 102100031256 Cyclic GMP-AMP synthase Human genes 0.000 claims description 10
- 101710118064 Cyclic GMP-AMP synthase Proteins 0.000 claims description 10
- 229940002612 prodrug Drugs 0.000 claims description 10
- 239000000651 prodrug Substances 0.000 claims description 10
- 230000032683 aging Effects 0.000 claims description 9
- 230000009286 beneficial effect Effects 0.000 claims description 9
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 9
- 208000023275 Autoimmune disease Diseases 0.000 claims description 8
- 208000026935 allergic disease Diseases 0.000 claims description 8
- 208000035473 Communicable disease Diseases 0.000 claims description 7
- 208000027866 inflammatory disease Diseases 0.000 claims description 7
- 239000003814 drug Substances 0.000 claims description 6
- 125000000524 functional group Chemical group 0.000 claims description 5
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 4
- 208000021386 Sjogren Syndrome Diseases 0.000 claims description 4
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 4
- 208000015181 infectious disease Diseases 0.000 claims description 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 4
- 208000035408 type 1 diabetes mellitus 1 Diseases 0.000 claims description 4
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 201000001320 Atherosclerosis Diseases 0.000 claims description 2
- 208000011514 Familial renal glucosuria Diseases 0.000 claims description 2
- 208000023105 Huntington disease Diseases 0.000 claims description 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 201000004681 Psoriasis Diseases 0.000 claims description 2
- 206010038389 Renal cancer Diseases 0.000 claims description 2
- 206010039710 Scleroderma Diseases 0.000 claims description 2
- 208000034189 Sclerosis Diseases 0.000 claims description 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 2
- 201000001981 dermatomyositis Diseases 0.000 claims description 2
- 208000006454 hepatitis Diseases 0.000 claims description 2
- 231100000283 hepatitis Toxicity 0.000 claims description 2
- 125000001072 heteroaryl group Chemical group 0.000 claims description 2
- 125000000623 heterocyclic group Chemical group 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- 208000017169 kidney disease Diseases 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 208000010125 myocardial infarction Diseases 0.000 claims description 2
- 208000007278 renal glycosuria Diseases 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 208000011580 syndromic disease Diseases 0.000 claims description 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims description 2
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 25
- 125000004122 cyclic group Chemical group 0.000 claims 25
- -1 carbonyloxyl groups Chemical group 0.000 claims 22
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 claims 19
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 16
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 11
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 10
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 9
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 description 30
- 238000000034 method Methods 0.000 description 8
- IVRMZWNICZWHMI-UHFFFAOYSA-N azide group Chemical group [N-]=[N+]=[N-] IVRMZWNICZWHMI-UHFFFAOYSA-N 0.000 description 6
- 239000000126 substance Substances 0.000 description 6
- 230000001225 therapeutic effect Effects 0.000 description 6
- 230000002757 inflammatory effect Effects 0.000 description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 4
- 230000000172 allergic effect Effects 0.000 description 3
- 229940124597 therapeutic agent Drugs 0.000 description 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 2
- 238000013160 medical therapy Methods 0.000 description 2
- 208000035143 Bacterial infection Diseases 0.000 description 1
- 208000030852 Parasitic disease Diseases 0.000 description 1
- 208000036142 Viral infection Diseases 0.000 description 1
- 208000022362 bacterial infectious disease Diseases 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 230000018109 developmental process Effects 0.000 description 1
- 238000011170 pharmaceutical development Methods 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 238000012827 research and development Methods 0.000 description 1
- 230000009385 viral infection Effects 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022072440A JP7530068B2 (ja) | 2016-04-05 | 2022-04-26 | ｃＧＡＳアンタゴニスト化合物 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662318435P | 2016-04-05 | 2016-04-05 | |
| US62/318,435 | 2016-04-05 | ||
| US201662355403P | 2016-06-28 | 2016-06-28 | |
| US62/355,403 | 2016-06-28 | ||
| PCT/US2017/026019 WO2017176812A1 (en) | 2016-04-05 | 2017-04-04 | cGAS ANTAGONIST COMPOUNDS |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022072440A Division JP7530068B2 (ja) | 2016-04-05 | 2022-04-26 | ｃＧＡＳアンタゴニスト化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019510787A JP2019510787A (ja) | 2019-04-18 |
| JP2019510787A5 true JP2019510787A5 (enExample) | 2020-05-14 |
| JP7116422B2 JP7116422B2 (ja) | 2022-08-10 |
Family
ID=60000680
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018552246A Active JP7116422B2 (ja) | 2016-04-05 | 2017-04-04 | ｃＧＡＳアンタゴニスト化合物 |
| JP2022072440A Active JP7530068B2 (ja) | 2016-04-05 | 2022-04-26 | ｃＧＡＳアンタゴニスト化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022072440A Active JP7530068B2 (ja) | 2016-04-05 | 2022-04-26 | ｃＧＡＳアンタゴニスト化合物 |
Country Status (10)
| Country | Link |
|---|---|
| US (4) | US10947206B2 (enExample) |
| EP (1) | EP3439667B1 (enExample) |
| JP (2) | JP7116422B2 (enExample) |
| KR (1) | KR102516038B1 (enExample) |
| CN (1) | CN109475565B (enExample) |
| AU (2) | AU2017246413B2 (enExample) |
| CA (1) | CA3020161A1 (enExample) |
| DK (1) | DK3439667T3 (enExample) |
| ES (1) | ES2976118T3 (enExample) |
| WO (1) | WO2017176812A1 (enExample) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK3439667T3 (da) | 2016-04-05 | 2024-04-02 | Immune Sensor Llc | Cgas antagonist forbindelser |
| CN109867648A (zh) * | 2017-12-02 | 2019-06-11 | 浙江医药股份有限公司新昌制药厂 | 一种依帕列净有关物质impd的合成方法 |
| MX2020008237A (es) | 2018-02-05 | 2020-09-25 | Univ Rockefeller | Inhibidores de 2,3,4,5-tetrahidro-1h-pirido[4,3-b]indol de cgas para tratar enfermedades autoinflamatorias. |
| WO2019195658A1 (en) | 2018-04-05 | 2019-10-10 | Dana-Farber Cancer Institute, Inc. | Sting levels as a biomarker for cancer immunotherapy |
| AU2019373407A1 (en) * | 2018-11-02 | 2021-05-20 | The Walter And Eliza Hall Institute Of Medical Research | Methods of treatment, prevention and diagnosis |
| WO2020118206A1 (en) * | 2018-12-06 | 2020-06-11 | The Scripps Research Institute | Butenolide antagonists of the cgas/sting pathway |
| CN113286785A (zh) * | 2019-01-04 | 2021-08-20 | 贝尔布鲁克实验室有限责任公司 | 作为治疗剂的cGAS活性的抑制剂 |
| WO2020186027A1 (en) | 2019-03-13 | 2020-09-17 | Daisuke Tomita | Inhibitors of cgas for treating autoinflammatory diseases and cancer metastasis |
| JP2022116370A (ja) * | 2019-06-13 | 2022-08-10 | アグロカネショウ株式会社 | 新規な１－ベンジルアミン誘導体及びこれを有効成分とする農園芸用薬剤 |
| US20230106899A1 (en) | 2019-06-21 | 2023-04-06 | Ifm Due, Inc. | Methods of treating cancer |
| CN110305140B (zh) * | 2019-07-30 | 2020-08-04 | 上海勋和医药科技有限公司 | 二氢吡咯并嘧啶类选择性jak2抑制剂 |
| WO2021041532A1 (en) | 2019-08-26 | 2021-03-04 | Dana-Farber Cancer Institute, Inc. | Use of heparin to promote type 1 interferon signaling |
| KR102895957B1 (ko) * | 2020-01-31 | 2025-12-04 | (주)아모레퍼시픽 | 노화세포 회춘용 조성물 및 노화세포 회춘방법 |
| EP4153304A1 (en) * | 2020-05-20 | 2023-03-29 | F. Hoffmann-La Roche AG | New malonitrile derivatives |
| JP2024500877A (ja) * | 2020-12-22 | 2024-01-10 | アイエフエム デュー インコーポレイテッド | がんを処置する方法 |
| US20240122903A1 (en) | 2020-12-22 | 2024-04-18 | Ifm Due Inc. | Methods of treating cancer |
| JP2024500874A (ja) | 2020-12-22 | 2024-01-10 | アイエフエム デュー インコーポレイテッド | がんを処置する方法 |
| JP2024504002A (ja) * | 2020-12-22 | 2024-01-30 | アイエフエム デュー インコーポレイテッド | がんを処置する方法 |
| CN112592946A (zh) * | 2020-12-31 | 2021-04-02 | 河南巨龙生物工程股份有限公司 | 一种环保型高产鸟苷的工艺方法 |
| CN113651810B (zh) * | 2021-07-16 | 2023-10-13 | 上海毕得医药科技股份有限公司 | 一种3-甲酰基-1H-吡唑并[3,4-b]吡啶-5-羧酸甲酯的合成方法 |
| CN115073382A (zh) * | 2022-07-18 | 2022-09-20 | 乐威医药（江苏）股份有限公司 | 2-氯-嘧啶-5-甲醛的制备方法 |
| EP4638446A1 (en) * | 2022-12-20 | 2025-10-29 | Ventus Therapeutics U.S., Inc. | Thiadiazole derivatives as inhibitors of cyclic gmp-amp synthase and uses thereof |
| CN121517400A (zh) * | 2024-08-13 | 2026-02-13 | 中国科学院上海药物研究所 | 一类cGAS抑制剂、其制备方法和用途 |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5208250A (en) | 1988-05-25 | 1993-05-04 | Warner-Lambert Company | Known and selected novel arylmethylenyl derivatives of thiazolidinones, imidazolidinones and oxazolidinones useful as antiallergy agents and anti-inflammatory agents |
| IE940525L (en) | 1988-05-25 | 1989-11-25 | Warner Lambert Co | Known and selected novel arylmethylenyl derivatives of¹thiazolidinones, imidazolidinones and oxazolidinones useful¹as antiallergy agents and antiinflammatory agents |
| CA2080917C (en) | 1990-04-27 | 2001-06-12 | Reijo Baeckstroem | New pharmacologically active catechol derivatives |
| US5308853A (en) * | 1991-12-20 | 1994-05-03 | Warner-Lambert Company | Substituted-5-methylidene hydantoins with AT1 receptor antagonist properties |
| KR970002228A (ko) * | 1995-06-30 | 1997-01-24 | 배순훈 | 전원변동시 냉장고의 운전제어방법 |
| JP2000095770A (ja) | 1998-07-22 | 2000-04-04 | Toa Eiyo Ltd | Ｎ置換チアゾリジン誘導体及びそれを含有する医薬 |
| WO2003009807A2 (en) | 2001-07-23 | 2003-02-06 | Galileo Laboratories, Inc. | Cytoprotective compounds, pharmaceutical and cosmetic formulations, and methods |
| AU2003291613B2 (en) | 2002-04-30 | 2007-09-27 | Merck & Co., Inc. | Aryl-link-aryl substituted thiazolidine-dione and oxazolidine-dione as sodium channel blockers |
| US20040214872A1 (en) * | 2002-09-26 | 2004-10-28 | Pintex Pharmaceuticals, Inc. | Pin1-modulating compounds and methods of use thereof |
| US20060084682A1 (en) | 2002-12-13 | 2006-04-20 | Heerding Dirk A | Thrombopoietin mimetics |
| EP1605967A1 (en) | 2003-03-13 | 2005-12-21 | Novo Nordisk A/S | Novel nph insulin preparations |
| US20060258561A1 (en) * | 2003-03-13 | 2006-11-16 | Novo Nordisk A/S | Novel NPH insulin preparations |
| CA2540460A1 (en) * | 2003-10-28 | 2005-05-12 | Reddy Us Therapeutics, Inc. | Heterocyclic compounds and methods of making and using thereof |
| WO2005040163A1 (en) * | 2003-10-28 | 2005-05-06 | Dr. Reddy's Laboratories Ltd | Heterocyclic compounds that block the effects of advanced glycation end products (age) |
| WO2007014838A1 (en) * | 2005-08-03 | 2007-02-08 | Boehringer Ingelheim International Gmbh | Dihydropteridinones in the treatment of respiratory diseases |
| US9173871B2 (en) * | 2008-01-28 | 2015-11-03 | New York University | Oxazole and thiazole compounds as beta-catenin modulators and uses thereof |
| UY31952A (es) * | 2008-07-02 | 2010-01-29 | Astrazeneca Ab | 5-metilideno-1,3-tiazolidina-2,4-dionas sustituidas como inhibidores de quinasa pim |
| EP2222272B1 (en) * | 2008-08-07 | 2012-11-07 | Pulmagen Therapeutics (Inflammation) Limited | Respiratory disease treatment |
| CN101361737B (zh) | 2008-09-28 | 2011-08-03 | 四川大学 | 5-苯亚甲基-2，4-噻唑烷二酮衍生物的用途 |
| EP2383263B1 (en) | 2008-12-30 | 2014-04-16 | Industry-academic Cooperation Foundation, Chosun University | Novel thiazolidinedione derivative and use thereof |
| KR20100097939A (ko) * | 2009-02-27 | 2010-09-06 | 연세대학교 산학협력단 | 신규 ｃｋ2 저해제 및 그의 제조 방법 |
| US9174951B2 (en) * | 2012-03-28 | 2015-11-03 | Ohio State Innovation Foundation | Glucose transporter inhibitors |
| WO2014024897A1 (ja) | 2012-08-06 | 2014-02-13 | Ｍｅｉｊｉ Ｓｅｉｋａファルマ株式会社 | チアゾリジンジオンおよびピロリジンジオン誘導体、並びにそれらを有効成分としてなる殺菌剤 |
| JP2016506408A (ja) | 2012-12-19 | 2016-03-03 | ボード・オブ・リージエンツ，ザ・ユニバーシテイ・オブ・テキサス・システム | 哺乳動物の環状ジヌクレオチドシグナル伝達経路の薬学的標的化 |
| JP2016524593A (ja) * | 2013-04-29 | 2016-08-18 | メモリアル スローン−ケタリング キャンサー センター | セカンドメッセンジャーのシグナル伝達を変えるための組成物及び方法 |
| EP3164411B1 (en) * | 2014-07-04 | 2019-08-28 | Paris Sciences et Lettres - Quartier Latin | Fluorogen activating and shifting tag (fast) |
| US10501413B2 (en) | 2015-03-23 | 2019-12-10 | University Of Miami | Inhibitors of the Notch transcriptional activation complex and methods for use of the same |
| DK3439667T3 (da) | 2016-04-05 | 2024-04-02 | Immune Sensor Llc | Cgas antagonist forbindelser |
| CN108825600B (zh) | 2018-06-15 | 2021-02-19 | 上海卫星工程研究所 | 一种应用于航天器钢丝构件无外力安装装置 |
-
2017
- 2017-04-04 DK DK17779694.3T patent/DK3439667T3/da active
- 2017-04-04 WO PCT/US2017/026019 patent/WO2017176812A1/en not_active Ceased
- 2017-04-04 AU AU2017246413A patent/AU2017246413B2/en active Active
- 2017-04-04 JP JP2018552246A patent/JP7116422B2/ja active Active
- 2017-04-04 CA CA3020161A patent/CA3020161A1/en active Pending
- 2017-04-04 KR KR1020187031853A patent/KR102516038B1/ko active Active
- 2017-04-04 EP EP17779694.3A patent/EP3439667B1/en active Active
- 2017-04-04 CN CN201780034803.0A patent/CN109475565B/zh active Active
- 2017-04-04 ES ES17779694T patent/ES2976118T3/es active Active
-
2018
- 2018-04-15 US US15/953,494 patent/US10947206B2/en active Active
-
2021
- 2021-03-03 US US17/191,305 patent/US11597707B2/en active Active
- 2021-08-31 AU AU2021225151A patent/AU2021225151B2/en active Active
-
2022
- 2022-04-26 JP JP2022072440A patent/JP7530068B2/ja active Active
-
2023
- 2023-01-23 US US18/158,046 patent/US12065416B2/en active Active
-
2024
- 2024-06-28 US US18/759,546 patent/US12655118B2/en active Active
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