CN110997662B - 作为腺苷受体拮抗剂的苯并咪唑衍生物 - Google Patents

作为腺苷受体拮抗剂的苯并咪唑衍生物 Download PDF

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CN110997662B
CN110997662B CN201880054520.7A CN201880054520A CN110997662B CN 110997662 B CN110997662 B CN 110997662B CN 201880054520 A CN201880054520 A CN 201880054520A CN 110997662 B CN110997662 B CN 110997662B
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cancer
compounds
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adenosine
receptor
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CN110997662A (zh
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E-M.坦策
K.席曼
M.克莱因
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Merck Patent GmbH
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CN201880054520.7A 2017-08-21 2018-08-20 作为腺苷受体拮抗剂的苯并咪唑衍生物 Active CN110997662B (zh)

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PCT/EP2018/072398 WO2019038215A1 (en) 2017-08-21 2018-08-20 BENZIMIDAZOLE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11497752B2 (en) 2018-01-30 2022-11-15 Foghorn Therapeutics Inc. Compounds and uses thereof
US12509453B2 (en) 2019-01-29 2025-12-30 Foghorn Therapeutics Inc. BRM/BRG1 inhibitors and uses thereof
WO2021155264A1 (en) * 2020-01-29 2021-08-05 Foghorn Therapeutics Inc. Compounds and uses thereof
AU2021213811A1 (en) 2020-01-29 2022-07-28 Foghorn Therapeutics Inc. Compounds and uses thereof
US11618751B1 (en) 2022-03-25 2023-04-04 Ventus Therapeutics U.S., Inc. Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 derivatives
US20240116897A1 (en) * 2021-01-29 2024-04-11 Korea Research Institute Of Chemical Technology Benzothiazole and benzimidazole derivatives, pharmaceutically acceptable salt thereof, preparation method therefor, and pharmaceutical composition comprising same as active ingredient
US12606553B2 (en) 2021-03-09 2026-04-21 Foghorn Therapeutics Inc. Crystalline forms, compositions containing same, and methods of their use
US11319319B1 (en) 2021-04-07 2022-05-03 Ventus Therapeutics U.S., Inc. Compounds for inhibiting NLRP3 and uses thereof
EP4351640A1 (en) 2021-06-07 2024-04-17 Ares Trading S.A. Combination treatment of cancer
US12331048B2 (en) 2022-10-31 2025-06-17 Ventus Therapeutics U.S., Inc. Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 inhibitors
AU2024271907A1 (en) * 2023-05-15 2025-12-11 Wigen Biomedicine Technology (shanghai) Co., Ltd. Hdac1/2 selective inhibitor and use thereof

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005116026A1 (en) * 2004-05-24 2005-12-08 F. Hoffmann-La Roche Ag 4-hydroxy-4-methyl-piperidine-1-carboxylic acid (4-methoxy-7-morpholin-4-yl-benzothiazol-2-yl)-amide
WO2006008041A1 (en) * 2004-07-22 2006-01-26 F. Hoffmann-La Roche Ag Benzothiazole derivatives
CN1791600A (zh) * 2003-05-19 2006-06-21 弗·哈夫曼-拉罗切有限公司 用作腺苷受体的配体的苯并噻唑衍生物
CN102731488A (zh) * 2011-04-02 2012-10-17 中国医学科学院药物研究所 苯并咪唑类衍生物、及其制法和药物组合物与用途

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4207554A (en) 1972-08-04 1980-06-10 Med-El Inc. Method and apparatus for automated classification and analysis of cells
US4125828A (en) 1972-08-04 1978-11-14 Med-El Inc. Method and apparatus for automated classification and analysis of cells
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
DE69720965T2 (de) 1996-02-13 2004-02-05 Astrazeneca Ab Chinazolinderivate und deren verwendung als vegf hemmer
NZ331191A (en) 1996-03-05 2000-03-27 Zeneca Ltd 4-anilinoquinazoline derivatives and pharmaceutical compositions thereof
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
AU1688599A (en) 1998-01-05 1999-07-26 Eisai Co. Ltd. Purine derivatives and adenosine a2 receptor antagonists serving as preventives/remedies for diabetes
GB9900334D0 (en) 1999-01-07 1999-02-24 Angiogene Pharm Ltd Tricylic vascular damaging agents
GB9900752D0 (en) 1999-01-15 1999-03-03 Angiogene Pharm Ltd Benzimidazole vascular damaging agents
US6841549B1 (en) 1999-07-02 2005-01-11 Eisai Co., Ltd. Condensed imidazole compounds and a therapeutic agent for diabetes mellitus
AU2001258628A1 (en) 2000-05-31 2001-12-11 Astrazeneca Ab Indole derivatives with vascular damaging activity
MXPA02012905A (es) 2000-07-07 2004-07-30 Angiogene Pharm Ltd Derivados de colquinol como agentes de dano vascular..
MXPA02012903A (es) 2000-07-07 2004-07-30 Angiogene Pharm Ltd Derivados de colquinol como inhibidores de angiogenesis.
WO2004089942A2 (en) 2001-10-02 2004-10-21 Acadia Pharmaceuticals Inc. Benzimidazolidinone derivatives as muscarinic agents
EP1465634B1 (en) 2001-12-12 2014-10-22 The Government of the United States of America, as represented by the Secretary Department of Health and Human Services Methods for using adenosine receptor inhibitors to enhance immune response and inflammation
US20080070932A1 (en) 2003-04-09 2008-03-20 Chi Vu Triazolo[ 1,5-A] Pyrimidines And Pyrazolo[ 1,5-A] Pyrimidines And Methods Of Making And Using The Same
KR100710453B1 (ko) 2003-05-13 2007-04-24 에프. 호프만-라 로슈 아게 아데노신 수용체 리간드로서의 2-이미다조-벤조싸이아졸
MXPA05012369A (es) 2003-05-21 2006-02-02 Hoffmann La Roche Derivados de benzotiazol y uso de los mismos en el tratamiento de enfermedades relacionadas con el receptor a2a de adenosina.
RU2006112847A (ru) 2003-09-19 2007-11-10 Ф. Хоффманн-Ля Рош Аг (Ch) Производные тиазолопиридина в качестве лигандов аденозинового рецептора
US20060223849A1 (en) * 2005-03-14 2006-10-05 Mjalli Adnan M Benzazole derivatives, compositions, and methods of use as beta-secretase inhibitors

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1791600A (zh) * 2003-05-19 2006-06-21 弗·哈夫曼-拉罗切有限公司 用作腺苷受体的配体的苯并噻唑衍生物
WO2005116026A1 (en) * 2004-05-24 2005-12-08 F. Hoffmann-La Roche Ag 4-hydroxy-4-methyl-piperidine-1-carboxylic acid (4-methoxy-7-morpholin-4-yl-benzothiazol-2-yl)-amide
WO2006008041A1 (en) * 2004-07-22 2006-01-26 F. Hoffmann-La Roche Ag Benzothiazole derivatives
CN102731488A (zh) * 2011-04-02 2012-10-17 中国医学科学院药物研究所 苯并咪唑类衍生物、及其制法和药物组合物与用途

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US20220306588A1 (en) 2022-09-29
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CN110997662A (zh) 2020-04-10
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