JP7570235B2 - Ｓｔｉｎｇ活性化剤としての三環式複素環式化合物 - Google Patents
Ｓｔｉｎｇ活性化剤としての三環式複素環式化合物 Download PDFInfo
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- JP7570235B2 JP7570235B2 JP2020565764A JP2020565764A JP7570235B2 JP 7570235 B2 JP7570235 B2 JP 7570235B2 JP 2020565764 A JP2020565764 A JP 2020565764A JP 2020565764 A JP2020565764 A JP 2020565764A JP 7570235 B2 JP7570235 B2 JP 7570235B2
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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| PCT/US2019/033944 WO2019227007A1 (en) | 2018-05-25 | 2019-05-24 | Tricyclic heterocyclic compounds as sting activators |
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| EP (1) | EP3802534B1 (https=) |
| JP (2) | JP7570235B2 (https=) |
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| MA (1) | MA52754A (https=) |
| WO (1) | WO2019227007A1 (https=) |
Cited By (1)
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| JP2024133472A (ja) * | 2018-05-25 | 2024-10-02 | インサイト・コーポレイション | Ｓｔｉｎｇ活性化剤としての三環式複素環式化合物 |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2019011655A (es) | 2017-03-29 | 2019-12-19 | Legochem Biosciences Inc | Profarmaco de dimero de pirrolobenzodiazepina y compuesto conjugado ligando-conector de este. |
| KR20190043437A (ko) | 2017-10-18 | 2019-04-26 | 씨제이헬스케어 주식회사 | 단백질 키나제 억제제로서의 헤테로고리 화합물 |
| WO2020010451A1 (en) * | 2018-07-10 | 2020-01-16 | Trillium Therapeutics Inc. | Heteroaromatic-fused imidazolyl amides, compositions and uses thereof as sting agonists |
| US10875872B2 (en) | 2018-07-31 | 2020-12-29 | Incyte Corporation | Heteroaryl amide compounds as sting activators |
| US11008344B2 (en) | 2018-07-31 | 2021-05-18 | Incyte Corporation | Tricyclic heteroaryl compounds as STING activators |
| KR102195348B1 (ko) | 2018-11-15 | 2020-12-24 | 에이치케이이노엔 주식회사 | 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물 |
| US11596692B1 (en) | 2018-11-21 | 2023-03-07 | Incyte Corporation | PD-L1/STING conjugates and methods of use |
| US12129267B2 (en) | 2019-01-07 | 2024-10-29 | Incyte Corporation | Heteroaryl amide compounds as sting activators |
| WO2021013234A1 (en) | 2019-07-25 | 2021-01-28 | Beigene, Ltd. | Cyclic dinucleotides as sting agonists |
| CA3149482A1 (en) | 2019-08-02 | 2021-02-11 | Mersana Therapeutics, Inc. | Bis-[n-((5-carbamoyl)-1h-benzo[d]imidazol-2-yl)-pyrazol-5-carboxamide] derivatives and related compounds as sting (stimulator of interferon genes) agonists for the treatment of cancer |
| US20220289768A1 (en) * | 2019-10-10 | 2022-09-15 | Beigene, Ltd. | Heterocyclic compounds as sting modulators |
| CN112778336B (zh) * | 2019-11-02 | 2023-05-05 | 上海凌达生物医药有限公司 | 一类含氮稠环类sting调节剂类化合物、制备方法和用途 |
| CN114981265B (zh) * | 2019-12-18 | 2025-01-03 | Ctxt私人有限公司 | 化合物 |
| CA3173510A1 (en) * | 2020-03-25 | 2021-09-30 | Takao Kiyoi | Novel benzimidazole derivative |
| WO2021202984A1 (en) | 2020-04-02 | 2021-10-07 | Mersana Therapeutics, Inc. | Antibody drug conjugates comprising sting agonists |
| WO2021206158A1 (ja) | 2020-04-10 | 2021-10-14 | 小野薬品工業株式会社 | がん治療方法 |
| WO2021239068A1 (en) * | 2020-05-28 | 2021-12-02 | Beigene, Ltd. | Heterocyclic compounds as sting modulators |
| WO2024220889A1 (en) * | 2023-04-20 | 2024-10-24 | Seagen Inc. | Sting agonist compounds and conjugates thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017175156A1 (en) | 2016-04-07 | 2017-10-12 | Glaxosmithkline Intellectual Property Development Limited | Heterocyclic amides useful as protein modulators |
| WO2017175147A1 (en) | 2016-04-07 | 2017-10-12 | Glaxosmithkline Intellectual Property Development Limited | Heterocyclic amides useful as protein modulators |
| JP2020536106A (ja) | 2017-10-05 | 2020-12-10 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ | Ｈｉｖの処置に有用なインターフェロン遺伝子の刺激物質（ｓｔｉｎｇ）の調節物質 |
Family Cites Families (63)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| ATE459616T1 (de) | 1998-08-11 | 2010-03-15 | Novartis Ag | Isochinoline derivate mit angiogenesis-hemmender wirkung |
| US6133031A (en) | 1999-08-19 | 2000-10-17 | Isis Pharmaceuticals Inc. | Antisense inhibition of focal adhesion kinase expression |
| GB9905075D0 (en) | 1999-03-06 | 1999-04-28 | Zeneca Ltd | Chemical compounds |
| GB0004890D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| ATE273695T1 (de) | 2000-06-28 | 2004-09-15 | Smithkline Beecham Plc | Nassvermahlung |
| IL160915A0 (en) | 2001-09-19 | 2004-08-31 | Aventis Pharma Sa | Indolizines inhibiting kinase proteins |
| ES2269793T3 (es) | 2001-10-30 | 2007-04-01 | Novartis Ag | Derivados de estaurospina como inhibidores de la actividad de tirosina quinasa receptora flt3. |
| TW200406374A (en) | 2002-05-29 | 2004-05-01 | Novartis Ag | Diaryl urea derivatives useful for the treatment of protein kinase dependent diseases |
| GB0215676D0 (en) | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
| CL2003002353A1 (es) | 2002-11-15 | 2005-02-04 | Vertex Pharma | Compuestos derivados de diaminotriazoles, inhibidores d ela proteina quinasa; composicion farmaceutica; procedimiento de preparacion; y su uso del compuesto en el tratamiento de enfermedades de desordenes alergicos, proliferacion, autoinmunes, condic |
| UA80767C2 (en) | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
| GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
| AR045944A1 (es) | 2003-09-24 | 2005-11-16 | Novartis Ag | Derivados de isoquinolina 1.4-disustituidas |
| RU2007123675A (ru) | 2004-11-24 | 2008-12-27 | Новартис АГ (CH) | Комбинации ингибиторов jak |
| PL2931738T3 (pl) | 2012-12-13 | 2019-07-31 | Aduro Biotech, Inc. | Kompozycje zawierające cykliczne dinukleotydy purynowe o zdefiniowanej stereochemii i sposoby ich otrzymywania i zastosowania |
| CN109394752A (zh) | 2013-10-21 | 2019-03-01 | 德雷克塞尔大学 | 治疗慢性乙型肝炎病毒感染的sting激动剂的用途 |
| JP2016538344A (ja) | 2013-11-19 | 2016-12-08 | ザ・ユニバーシティ・オブ・シカゴＴｈｅ Ｕｎｉｖｅｒｓｉｔｙ Ｏｆ Ｃｈｉｃａｇｏ | 癌処置としてのｓｔｉｎｇアゴニストの使用 |
| KR102409739B1 (ko) | 2014-03-20 | 2022-06-17 | 카펠라 테라퓨틱스, 인크. | 암 치료용의 ｅｒｂｂ 티로신 키나제 억제제로서의 벤즈이미다졸 유도체 |
| PE20170198A1 (es) | 2014-06-04 | 2017-04-08 | Glaxosmithkline Ip Dev Ltd | Dinucleotidos ciclicos como moduladores de sting |
| WO2016096577A1 (en) | 2014-12-16 | 2016-06-23 | Invivogen | Combined use of a chemotherapeutic agent and a cyclic dinucleotide for cancer treatment |
| GB201501462D0 (en) | 2015-01-29 | 2015-03-18 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| WO2017011444A1 (en) | 2015-07-13 | 2017-01-19 | The Wistar Institute Of Anatomy And Biology | Methods and compositions for treating b cell cancers |
| TW201717968A (zh) | 2015-07-14 | 2017-06-01 | 春季銀行製藥公司 | 誘導ｒｉｇ－ｉ和其他模式辨識受體之化合物及組成物 |
| US10844051B2 (en) | 2015-07-22 | 2020-11-24 | The Royal Institution For The Advancement Of Learning/Mcgill University | Substituted oxazoles for the treatment of cancer |
| CR20180101A (es) | 2015-08-13 | 2018-04-12 | Merck Sharp & Dohme | Compuestos di-nucleóticos cíclicos como agonistas de sting |
| WO2017053537A1 (en) | 2015-09-23 | 2017-03-30 | Capella Therapeutics, Inc. | Benzimidazoles for use in the treatment of cancer and inflammatory diseases |
| CN105367617A (zh) | 2015-09-25 | 2016-03-02 | 武汉品生科技有限公司 | 一种基于环二腺核苷酸的衍生物、tat多肽及其在一型干扰素小分子中抑制剂的应用 |
| US20170146519A1 (en) | 2015-11-20 | 2017-05-25 | Oregon Health & Science University | Sting agonists and methods of selecting sting agonists |
| TWI704154B (zh) | 2015-12-03 | 2020-09-11 | 英商葛蘭素史克智慧財產發展有限公司 | 新穎化合物 |
| EP3386536A4 (en) | 2015-12-07 | 2019-07-31 | Opi Vi- IP Holdco LLC | COMPOSITION OF ANTIBODY CONSTRUCT AGONIST CONJUGATES AND METHOD FOR USE THEREOF |
| US20180369268A1 (en) | 2015-12-16 | 2018-12-27 | Aduro Biotech, Inc. | Methods for identifying inhibitors of "stimulator of interferon gene"- dependent interferon production |
| WO2017123657A1 (en) | 2016-01-11 | 2017-07-20 | Gary Glick | Cyclic dinucleotides for treating conditions associated with sting activity such as cancer |
| RS67188B1 (sr) | 2016-01-11 | 2025-10-31 | Innate Tumor Immunity Inc | Ciklični dinukleotidi za lečenje stanja povezanih sa aktivnošću sting kao što je kancer |
| MX2018010586A (es) | 2016-03-02 | 2019-03-28 | Univ Texas | Nanovacuna de activacion de "sting" para inmunoterapia. |
| SG10201912074PA (en) | 2016-03-18 | 2020-02-27 | Immune Sensor Llc | Cyclic di-nucleotide compounds and methods of use |
| WO2017186711A1 (en) | 2016-04-25 | 2017-11-02 | Invivogen | Novel complexes of immunostimulatory compounds, and uses thereof |
| US10537590B2 (en) | 2016-09-30 | 2020-01-21 | Boehringer Ingelheim International Gmbh | Cyclic dinucleotide compounds |
| US10414747B2 (en) | 2016-10-04 | 2019-09-17 | Merck Sharp & Dohme Corp. | Benzo[b]thiophene compounds as sting agonists |
| WO2018119263A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Heterocyclic compounds derivatives as pd-l1 internalization inducers |
| ES2874756T3 (es) | 2016-12-22 | 2021-11-05 | Incyte Corp | Derivados de triazolo[1,5-A]piridina como inmunomoduladores |
| AU2017382870B2 (en) | 2016-12-22 | 2022-03-24 | Incyte Corporation | Benzooxazole derivatives as immunomodulators |
| ES2899402T3 (es) | 2016-12-22 | 2022-03-11 | Incyte Corp | Derivados de piridina como inmunomoduladores |
| EP3558990B1 (en) | 2016-12-22 | 2022-08-10 | Incyte Corporation | Tetrahydro imidazo[4,5-c]pyridine derivatives as pd-l1 internalization inducers |
| WO2018119286A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Bicyclic heteroaromatic compounds as immunomodulators |
| JP2020524718A (ja) | 2017-06-22 | 2020-08-20 | キュラデブ・ファーマ・リミテッドＣｕｒａｄｅｖ Ｐｈａｒｍａ Ｌｉｍｉｔｅｄ | ヒトｓｔｉｎｇの複素環式小分子調節因子 |
| US20200138827A1 (en) | 2017-06-22 | 2020-05-07 | Curadev Pharma Limited | Small molecule modulators of human sting |
| PE20200696A1 (es) | 2017-06-22 | 2020-06-16 | Curadev Pharma Ltd | Moduladores de moleculas pequenas de sting humana |
| US11312772B2 (en) | 2017-08-04 | 2022-04-26 | Merck Sharp & Dohme Corp. | Combinations of PD-1 antagonists and benzo [b] thiophene STING agonists for cancer treatment |
| US11285131B2 (en) | 2017-08-04 | 2022-03-29 | Merck Sharp & Dohme Corp. | Benzo[b]thiophene STING agonists for cancer treatment |
| CN107335049B (zh) | 2017-08-18 | 2019-10-18 | 中国药科大学 | 菊科类型环肽化合物作为cGAS-STING信号通路抑制剂的应用 |
| CA3077337A1 (en) | 2017-10-05 | 2019-04-11 | Glaxosmithkline Intellectual Property Development Limited | Modulators of stimulator of interferon genes (sting) |
| CN111194214A (zh) | 2017-10-05 | 2020-05-22 | 葛兰素史密斯克莱知识产权发展有限公司 | 施用sting激动剂的方法 |
| CN110016025B (zh) | 2018-01-08 | 2021-08-06 | 成都先导药物开发股份有限公司 | 一种免疫调节剂 |
| DE102018200540A1 (de) | 2018-01-15 | 2019-07-18 | Robert Bosch Gmbh | Verfahren zum Betreiben eines Kraftfahrzeugbordnetzes |
| CR20200520A (es) | 2018-03-30 | 2021-03-09 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
| GB201807924D0 (en) | 2018-05-16 | 2018-06-27 | Ctxt Pty Ltd | Compounds |
| ES2929415T3 (es) | 2018-05-25 | 2022-11-29 | Incyte Corp | Compuestos heterocíclicos tricíclicos como activadores de STING |
| JP2021530442A (ja) | 2018-06-28 | 2021-11-11 | ジエンス ヘンルイ メデイシンカンパニー リミテッドJiangsu Hengrui Medicine Co., Ltd. | 縮合三環系複素環化合物およびその治療上の使用 |
| US10875872B2 (en) | 2018-07-31 | 2020-12-29 | Incyte Corporation | Heteroaryl amide compounds as sting activators |
| US11008344B2 (en) | 2018-07-31 | 2021-05-18 | Incyte Corporation | Tricyclic heteroaryl compounds as STING activators |
| WO2020132549A1 (en) | 2018-12-21 | 2020-06-25 | Nimbus Titan, Inc. | Sting heterocycle agonists and uses thereof |
| US12129267B2 (en) | 2019-01-07 | 2024-10-29 | Incyte Corporation | Heteroaryl amide compounds as sting activators |
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017175156A1 (en) | 2016-04-07 | 2017-10-12 | Glaxosmithkline Intellectual Property Development Limited | Heterocyclic amides useful as protein modulators |
| WO2017175147A1 (en) | 2016-04-07 | 2017-10-12 | Glaxosmithkline Intellectual Property Development Limited | Heterocyclic amides useful as protein modulators |
| JP2020536106A (ja) | 2017-10-05 | 2020-12-10 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ | Ｈｉｖの処置に有用なインターフェロン遺伝子の刺激物質（ｓｔｉｎｇ）の調節物質 |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2024133472A (ja) * | 2018-05-25 | 2024-10-02 | インサイト・コーポレイション | Ｓｔｉｎｇ活性化剤としての三環式複素環式化合物 |
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| WO2019227007A1 (en) | 2019-11-28 |
| JP2021525706A (ja) | 2021-09-27 |
| MA52754A (fr) | 2021-04-14 |
| JP2024133472A (ja) | 2024-10-02 |
| CA3101368A1 (en) | 2019-11-28 |
| US11713317B2 (en) | 2023-08-01 |
| US20190359608A1 (en) | 2019-11-28 |
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| US10947227B2 (en) | 2021-03-16 |
| EP3802534B1 (en) | 2022-07-13 |
| EP3802534A1 (en) | 2021-04-14 |
| ES2929415T3 (es) | 2022-11-29 |
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