BR112022001931A2 - Derivados de bis-[n-((5-carbamoil)-1h-benzo[d]imidazol-2-il)-pirazol-5-carboxamida e compostos relacionados como agonistas de sting (estimulador de genes de interferon) para o tratamento de câncer - Google Patents
Derivados de bis-[n-((5-carbamoil)-1h-benzo[d]imidazol-2-il)-pirazol-5-carboxamida e compostos relacionados como agonistas de sting (estimulador de genes de interferon) para o tratamento de câncerInfo
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- BR112022001931A2 BR112022001931A2 BR112022001931A BR112022001931A BR112022001931A2 BR 112022001931 A2 BR112022001931 A2 BR 112022001931A2 BR 112022001931 A BR112022001931 A BR 112022001931A BR 112022001931 A BR112022001931 A BR 112022001931A BR 112022001931 A2 BR112022001931 A2 BR 112022001931A2
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- Prior art keywords
- imidazol
- carbamoyl
- benzo
- treatment
- pyrazol
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- 150000001875 compounds Chemical class 0.000 title abstract 6
- 108010050904 Interferons Proteins 0.000 title abstract 2
- 206010028980 Neoplasm Diseases 0.000 title 1
- 229940044665 STING agonist Drugs 0.000 title 1
- 229940053202 antiepileptics carboxamide derivative Drugs 0.000 title 1
- 201000011510 cancer Diseases 0.000 title 1
- 208000035473 Communicable disease Diseases 0.000 abstract 1
- 206010067125 Liver injury Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 238000012512 characterization method Methods 0.000 abstract 1
- 231100000234 hepatic damage Toxicity 0.000 abstract 1
- 230000008818 liver damage Effects 0.000 abstract 1
- 230000004060 metabolic process Effects 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
- 230000009385 viral infection Effects 0.000 abstract 1
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- 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
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- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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Abstract
a presente invenção refere-se a compostos de fórmula (ia') como agonistas de sting (estimulador de genes de interferon), para uso no tratamento de, por exemplo, doenças infecciosas, incluindo, mas não limitadas a, obesidade, lesão hepática, metabolismo açúcar-lipídico e infecção por vírus. a presente descrição descreve a síntese e caracterização de compostos exemplares, bem como dados farmacológicos dos mesmos (por exemplo, páginas 128 a 286; exemplos 1 a 54, tabelas 1, 2a, 2b e 3). um complosto exemplar é, por exemplo 1: (e)-n-(5-carbamoil-1-(4-(5-carbamoil-2-(4-etil-2-metiloxazol-5-carboxamido)-7-(3-hidroxipropóxi)-1h-benzo[d]imidazol-1-il)-7-metóxi-1h-benzo[d]imidazol-2-il)-4-etil-2-metiloxazol-5-carboxamida (composto 9). (composto 9)
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201962882081P | 2019-08-02 | 2019-08-02 | |
US201962944643P | 2019-12-06 | 2019-12-06 | |
US202062982935P | 2020-02-28 | 2020-02-28 | |
PCT/US2020/044538 WO2021026009A1 (en) | 2019-08-02 | 2020-07-31 | 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 |
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BR112022001931A2 true BR112022001931A2 (pt) | 2022-06-21 |
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US (2) | US11155567B2 (pt) |
EP (1) | EP4007758A1 (pt) |
JP (1) | JP2022543086A (pt) |
KR (1) | KR20220056176A (pt) |
CN (1) | CN114585623A (pt) |
AU (1) | AU2020324388A1 (pt) |
BR (1) | BR112022001931A2 (pt) |
CA (1) | CA3149482A1 (pt) |
IL (1) | IL290212A (pt) |
MX (1) | MX2022001407A (pt) |
TW (1) | TW202120500A (pt) |
WO (1) | WO2021026009A1 (pt) |
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CN109843327B (zh) | 2016-07-07 | 2022-05-13 | 小利兰·斯坦福大学托管委员会 | 抗体佐剂缀合物 |
CN113563313B (zh) * | 2019-01-31 | 2022-11-04 | 成都先导药物开发股份有限公司 | 一种免疫调节剂 |
JP2022525594A (ja) | 2019-03-15 | 2022-05-18 | ボルト バイオセラピューティクス、インコーポレーテッド | Her2を標的とする免疫結合体 |
BR112022001931A2 (pt) | 2019-08-02 | 2022-06-21 | Mersana Therapeutics Inc | Derivados de bis-[n-((5-carbamoil)-1h-benzo[d]imidazol-2-il)-pirazol-5-carboxamida e compostos relacionados como agonistas de sting (estimulador de genes de interferon) para o tratamento de câncer |
MX2022012304A (es) * | 2020-04-02 | 2022-11-30 | Mersana Therapeutics Inc | Conjugados de anticuerpo-farmaco que comprenden agonistas de sting. |
EP4134098A4 (en) | 2020-04-10 | 2024-05-15 | ONO Pharmaceutical Co., Ltd. | CANCER THERAPY METHODS |
WO2022177307A1 (ko) * | 2021-02-17 | 2022-08-25 | 한국화학연구원 | 벤즈이미다졸 유도체를 유효 성분으로 포함하는 인터페론 유전자 자극제 조성물 |
WO2022247743A1 (en) * | 2021-05-24 | 2022-12-01 | Fulgent Genetics, Inc. | Compounds and their use as vaccine adjuvants |
CN114948955A (zh) * | 2022-06-06 | 2022-08-30 | 中国科学技术大学 | 靶向环鸟苷酸-腺苷酸合成酶的小分子共价抑制剂及其用途 |
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GB0018891D0 (en) | 2000-08-01 | 2000-09-20 | Novartis Ag | Organic compounds |
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HUE10161767T1 (hu) | 2002-07-03 | 2019-03-28 | Ono Pharmaceutical Co | Immunpotenciáló kompozíciók, amelyek anti-PD-L1 antitesteket tartalmaznak |
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PT2170959E (pt) | 2007-06-18 | 2014-01-07 | Merck Sharp & Dohme | Anticorpos para o receptor humano de morte programada pd-1 |
EP3569251A1 (en) | 2007-06-25 | 2019-11-20 | Endocyte, Inc. | Conjugates containing hydrophilic spacer linkers |
WO2009097128A1 (en) | 2008-01-29 | 2009-08-06 | Ludwig Institute For Cancer Research Ltd. | Membrane transporter napi2b (slc34a2) epitope for antibody therapy, antibodies directed thereto, and target for cancer therapy |
EP2262837A4 (en) | 2008-03-12 | 2011-04-06 | Merck Sharp & Dohme | PD-1 BINDING PROTEINS |
CN102203125A (zh) | 2008-08-25 | 2011-09-28 | 安普利穆尼股份有限公司 | Pd-1拮抗剂及其使用方法 |
WO2010036959A2 (en) | 2008-09-26 | 2010-04-01 | Dana-Farber Cancer Institute | Human anti-pd-1, pd-l1, and pd-l2 antibodies and uses therefor |
MX356367B (es) | 2008-12-09 | 2018-05-25 | Genentech Inc | Anticuerpos anti-pd-l1 y su uso para mejorar la funcion de celulas t. |
WO2011066342A2 (en) | 2009-11-24 | 2011-06-03 | Amplimmune, Inc. | Simultaneous inhibition of pd-l1/pd-l2 |
KR20190133790A (ko) | 2011-08-01 | 2019-12-03 | 제넨테크, 인크. | Pd-1 축 결합 길항제 및 mek 억제제를 사용하는 암 치료 방법 |
SG10201704611WA (en) | 2012-12-13 | 2017-07-28 | Aduro Biotech Inc | Compositions comprising cyclic purine dinucleotides having defined stereochemistries and methods for their preparation and use |
LT2996473T (lt) | 2013-05-18 | 2019-12-10 | Aduro Biotech Inc | Kompozicijos ir būdai, skirti aktyvuoti nuo "interferono geno stimuliatoriaus" priklausomą signalinį kelią |
EP2996472B1 (en) | 2013-05-18 | 2019-03-27 | Aduro Biotech, Inc. | Compositions and methods for inhibiting "stimulator of interferon gene" dependent signalling |
CA2950033A1 (en) | 2014-06-04 | 2015-12-10 | Glaxosmithkline Intellectual Property Development Limited | Cyclic di-nucleotides as modulators of sting |
TWI695011B (zh) | 2014-06-18 | 2020-06-01 | 美商梅爾莎納醫療公司 | 抗her2表位之單株抗體及其使用之方法 |
WO2016096577A1 (en) | 2014-12-16 | 2016-06-23 | Invivogen | Combined use of a chemotherapeutic agent and a cyclic dinucleotide for cancer treatment |
PL3233882T3 (pl) | 2014-12-16 | 2020-04-30 | Kayla Therapeutics | Fluorowane cykliczne dinukleotydy do indukcji cytokin |
GB201501462D0 (en) | 2015-01-29 | 2015-03-18 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
KR102222186B1 (ko) | 2015-08-13 | 2021-03-03 | 머크 샤프 앤드 돔 코포레이션 | Sting 효능제로서 시클릭 디-뉴클레오티드 화합물 |
TW201726700A (zh) | 2015-10-28 | 2017-08-01 | 艾杜諾生物科技公司 | 用於活化「干擾素基因刺激子」依賴性訊號之組合物及方法 |
AU2016362697B2 (en) | 2015-12-03 | 2018-07-12 | Glaxosmithkline Intellectual Property Development Limited | Cyclic purine dinucleotides as modulators of STING |
EP3386536A4 (en) | 2015-12-07 | 2019-07-31 | Opi Vi- IP Holdco LLC | COMPOSITION OF ANTIBODY CONSTRUCT AGONIST CONJUGATES AND METHOD FOR USE THEREOF |
US20170158772A1 (en) | 2015-12-07 | 2017-06-08 | Opi Vi - Ip Holdco Llc | Compositions of antibody construct - agonist conjugates and methods of use thereof |
WO2017160754A1 (en) | 2016-03-15 | 2017-09-21 | Mersana Therapeutics,Inc. | Napi2b-targeted antibody-drug conjugates and methods of use thereof |
MX2018012266A (es) | 2016-04-07 | 2019-05-30 | Glaxosmithkline Ip Dev Ltd | Amidas heterociclicas como moduladores de proteinas. |
JP6746712B2 (ja) | 2016-04-07 | 2020-08-26 | 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 | タンパク質調節因子として有用な複素環式アミド |
EP3507367A4 (en) | 2016-07-05 | 2020-03-25 | Aduro BioTech, Inc. | CYCLIC DINUCLEOTID COMPOUNDS WITH INCLUDED NUCLEIC ACIDS AND USES THEREOF |
EP3523287B1 (en) | 2016-10-04 | 2021-09-01 | Merck Sharp & Dohme Corp. | Benzo[b]thiophene compounds as sting agonists |
AU2017359043B2 (en) | 2016-11-08 | 2022-06-16 | Regeneron Pharmaceuticals, Inc. | Steroids and protein-conjugates thereof |
US11135307B2 (en) | 2016-11-23 | 2021-10-05 | Mersana Therapeutics, Inc. | Peptide-containing linkers for antibody-drug conjugates |
CA3049791A1 (en) | 2017-01-27 | 2018-08-02 | Silverback Therapeutics, Inc. | Tumor targeting conjugates and methods of use thereof |
US20180271996A1 (en) | 2017-02-28 | 2018-09-27 | Mersana Therapeutics, Inc. | Combination therapies of her2-targeted antibody-drug conjugates |
AR113224A1 (es) | 2017-04-28 | 2020-02-19 | Novartis Ag | Conjugados de anticuerpo que comprenden un agonista de sting |
EP3634401A1 (en) | 2017-06-07 | 2020-04-15 | Silverback Therapeutics, Inc. | Antibody construct conjugates |
MA49773A (fr) | 2017-08-04 | 2021-04-21 | Merck Sharp & Dohme | Combinaisons d'antagonistes de pd-1 et d'agonistes de sting benzo[b |
AU2018311966A1 (en) | 2017-08-04 | 2020-02-13 | Merck Sharp & Dohme Llc | Benzo[b]thiophene sting agonists for cancer treatment |
BR112020005390A2 (pt) | 2017-09-20 | 2020-09-29 | Mersana Therapeutics, Inc. | composições e métodos para prever a resposta à terapia direcionada ao napi2b |
US20200330556A1 (en) * | 2017-10-05 | 2020-10-22 | Glaxosmithkline Intellectual Property Development Limited | Methods for Administering STING Agonists |
BR112020006780A2 (pt) * | 2017-10-05 | 2020-10-06 | Glaxosmithkline Intellectual Property Development Limited | moduladores do estimulador de genes do interferon (sting) |
AU2018344902B2 (en) | 2017-10-05 | 2021-06-03 | Glaxosmithkline Intellectual Property Development Limited | Modulators of stimulator of interferon genes (STING) useful in treating HIV |
WO2019084060A1 (en) | 2017-10-24 | 2019-05-02 | Silverback Therapeutics, Inc. | CONJUGATES AND METHODS OF USE FOR THE SELECTIVE DELIVERY OF IMMUNOMODULATORY AGENTS |
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 |
CN110016021B (zh) | 2018-01-08 | 2021-05-07 | 成都先导药物开发股份有限公司 | 一种免疫调节剂 |
WO2019195063A1 (en) | 2018-04-03 | 2019-10-10 | Merck Sharp & Dohme Corp. | Aza-benzothiophene compounds as sting agonists |
EP3774764A1 (en) | 2018-04-03 | 2021-02-17 | Merck Sharp&Dohme Corp. | Benzothiophenes and related compounds as sting agonists |
EP3802534B1 (en) | 2018-05-25 | 2022-07-13 | Incyte Corporation | Tricyclic heterocyclic compounds as sting activators |
AU2019282150A1 (en) | 2018-06-04 | 2020-10-29 | Avacta Life Sciences, Limited | Tumor microenvironment-activated drug-binder conjugates, and uses related thereto |
WO2019243825A1 (en) | 2018-06-21 | 2019-12-26 | Curadev Pharma Limited | Small molecule modulators of human sting, conjugates and therapeutic applications |
KR20210025016A (ko) | 2018-06-28 | 2021-03-08 | 지앙수 헨그루이 메디슨 컴퍼니 리미티드 | 접합 삼중고리형 헤테로사이클 화합물과 그 치료 용도 |
WO2020010451A1 (en) * | 2018-07-10 | 2020-01-16 | Trillium Therapeutics Inc. | Heteroaromatic-fused imidazolyl amides, compositions and uses thereof as sting agonists |
WO2020028566A1 (en) | 2018-07-31 | 2020-02-06 | Incyte Corporation | Heteroaryl amide compounds as sting activators |
WO2020038387A1 (zh) | 2018-08-24 | 2020-02-27 | 杭州阿诺生物医药科技有限公司 | 高活性sting蛋白激动剂 |
WO2020042995A1 (zh) | 2018-08-29 | 2020-03-05 | 杭州阿诺生物医药科技有限公司 | 一种高活性sting蛋白激动剂化合物 |
BR112021004590A2 (pt) | 2018-09-12 | 2021-05-25 | Silverback Therapeutics, Inc. | composições para o tratamento de doença com conjugados imunoestimuladores |
CN110963997A (zh) | 2018-09-28 | 2020-04-07 | 四川科伦博泰生物医药股份有限公司 | 杂环酰胺类化合物、包含其的药物组合物及其制备方法和用途 |
EP3890703B8 (en) * | 2018-12-06 | 2023-10-11 | GlaxoSmithKline Intellectual Property Development Ltd | Novel pharmaceutical formulation comprising a sting modulator |
WO2020132582A1 (en) * | 2018-12-21 | 2020-06-25 | Nimbus Titan, Inc. | Sting agonists and uses thereof |
WO2020132566A1 (en) * | 2018-12-21 | 2020-06-25 | Nimbus Titan, Inc. | Sting pyrazole agonists and uses thereof |
WO2020132549A1 (en) | 2018-12-21 | 2020-06-25 | Nimbus Titan, Inc. | Sting heterocycle agonists and uses thereof |
CN111393404B (zh) | 2019-01-02 | 2023-02-17 | 中国科学院上海药物研究所 | 一类苯并噻吩类化合物及其药物组合物及应用 |
US20220056049A1 (en) | 2019-01-07 | 2022-02-24 | Incyte Corporation | Heteroaryl amide compounds as sting activators |
WO2020151682A1 (zh) | 2019-01-23 | 2020-07-30 | 成都先导药物开发股份有限公司 | 一种大环类免疫调节剂 |
CN113563313B (zh) | 2019-01-31 | 2022-11-04 | 成都先导药物开发股份有限公司 | 一种免疫调节剂 |
MX2021010701A (es) | 2019-03-05 | 2022-02-21 | F Star Therapeutics Inc | Compuestos, composiciones y metodos para el tratamiento de enfermedad. |
SG11202109191SA (en) | 2019-03-28 | 2021-09-29 | Lupin Ltd | Macrocyclic compounds as sting agonists |
TW202104214A (zh) | 2019-04-05 | 2021-02-01 | 英商葛蘭素史密斯克藍智慧財產發展有限公司 | 化合物 |
WO2020214858A1 (en) | 2019-04-17 | 2020-10-22 | Avidea Technologies, Inc. | Compositions and methods of manufacturing star polymers for ligand display and/or drug delivery |
CN111848573B (zh) | 2019-04-30 | 2023-04-07 | 四川科伦博泰生物医药股份有限公司 | 苯并噻吩酰胺类化合物及其制备方法和用途 |
WO2020221038A1 (zh) | 2019-04-30 | 2020-11-05 | 四川科伦博泰生物医药股份有限公司 | 苯并噻吩类化合物及其制备方法和用途 |
WO2020227159A2 (en) | 2019-05-03 | 2020-11-12 | Flagship Pioneering Innovations V, Inc. | Methods of modulating immune activity |
WO2021000770A1 (zh) | 2019-07-02 | 2021-01-07 | 凯复制药有限公司 | 可增强免疫活性的杂环化合物、其制备方法及其在医药上的应用 |
GB201910305D0 (en) | 2019-07-18 | 2019-09-04 | Ctxt Pty Ltd | Compounds |
EP4004002A1 (en) | 2019-07-22 | 2022-06-01 | Lupin Limited | Macrocyclic compounds as sting agonists and methods and uses thereof |
WO2021013250A1 (zh) | 2019-07-25 | 2021-01-28 | 上海济煜医药科技有限公司 | 杂环酰胺类化合物及其制备方法和应用 |
BR112022001931A2 (pt) | 2019-08-02 | 2022-06-21 | Mersana Therapeutics Inc | Derivados de bis-[n-((5-carbamoil)-1h-benzo[d]imidazol-2-il)-pirazol-5-carboxamida e compostos relacionados como agonistas de sting (estimulador de genes de interferon) para o tratamento de câncer |
US20230074558A1 (en) | 2019-12-06 | 2023-03-09 | Mersana Therapeutics, Inc. | Dimeric compounds as sting agonists |
CN113248475B (zh) | 2020-02-11 | 2023-03-17 | 中国科学院上海药物研究所 | 一类杂环取代的苯并咪唑二聚体或其药学上可接受的盐、组合物及其用途 |
MX2022012304A (es) | 2020-04-02 | 2022-11-30 | Mersana Therapeutics Inc | Conjugados de anticuerpo-farmaco que comprenden agonistas de sting. |
AU2022205057A1 (en) | 2021-01-04 | 2023-07-13 | Mersana Therapeutics, Inc. | B7h4-targeted antibody-drug conjugates and methods of use thereof |
CN112898286A (zh) | 2021-01-28 | 2021-06-04 | 中国药科大学 | 苯并噻吩类化合物或其可药用的盐、异构体及其制备方法、药物组合物和用途 |
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