JOP20190193B1 - ممركبات 2-أريل غير متجانس-3-أكسو-2، 3-ثنائي هيدرو بيريدازين-4-كربوكساميد لمعالجة السرطان - Google Patents
ممركبات 2-أريل غير متجانس-3-أكسو-2، 3-ثنائي هيدرو بيريدازين-4-كربوكساميد لمعالجة السرطانInfo
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- JOP20190193B1 JOP20190193B1 JOJO/P/2019/0193A JOP20190193A JOP20190193B1 JO P20190193 B1 JOP20190193 B1 JO P20190193B1 JO P20190193 A JOP20190193 A JO P20190193A JO P20190193 B1 JOP20190193 B1 JO P20190193B1
- Authority
- JO
- Jordan
- Prior art keywords
- compounds
- dihydropyridazine
- oxo
- hythryl
- carboxymide
- Prior art date
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- C07—ORGANIC CHEMISTRY
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- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/04—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having less than three double bonds between ring members or between ring members and non-ring members
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D237/14—Oxygen atoms
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- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Microbiology (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Peptides Or Proteins (AREA)
Abstract
يتعلق الاختراع الحالي بمركبات 2-اريل غير متجانس-3-أكسو-2، 3-ثنائي هيدرو بيريدازين-4-كربوكساميد بالصيغة العامة (I): (I) حيث X، R1، R2، R3، R4، وR5 كما هي موضحة ومحددة في هذه الوثيقة، بطرق لتحضير المركبات المذكورة، بمركبات وسيطة مفيدة في تحضير المركبات المذكورة، بتراكيب وتوليفات صيدلانية تشتمل على المركبات المذكورة، وباستخدام المركبات المذكورة في تصنيع تراكيب صيدلانية مستخدمة في العلاج أو الوقاية من الأمراض، ولا سيما السرطان أو حالات مرضية مقترنة باختلال الاستجابات المناعية وغيرها من الاضطرابات المصاحبة لتأشير AHR الشاذ، كعامل وحيد أو بشكل مؤتلف مع مكونات نشطة أخرى.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP17155406 | 2017-02-09 | ||
| EP17202882 | 2017-11-21 | ||
| PCT/EP2018/052627 WO2018146010A1 (en) | 2017-02-09 | 2018-02-02 | 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamides for the treatment of cancer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JOP20190193A1 JOP20190193A1 (ar) | 2019-08-08 |
| JOP20190193B1 true JOP20190193B1 (ar) | 2024-04-18 |
Family
ID=61188789
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JOJO/P/2019/0193A JOP20190193B1 (ar) | 2017-02-09 | 2018-02-02 | ممركبات 2-أريل غير متجانس-3-أكسو-2، 3-ثنائي هيدرو بيريدازين-4-كربوكساميد لمعالجة السرطان |
Country Status (39)
| Country | Link |
|---|---|
| US (3) | US12522594B2 (ar) |
| EP (1) | EP3580211B1 (ar) |
| JP (1) | JP7128826B2 (ar) |
| KR (1) | KR102627266B1 (ar) |
| CN (3) | CN116531380B (ar) |
| AU (1) | AU2018217860B2 (ar) |
| BR (1) | BR112019016497A2 (ar) |
| CA (1) | CA3052718A1 (ar) |
| CL (1) | CL2019002255A1 (ar) |
| CO (1) | CO2019008684A2 (ar) |
| CR (1) | CR20190364A (ar) |
| CU (1) | CU24564B1 (ar) |
| CY (1) | CY1124484T1 (ar) |
| DK (1) | DK3580211T3 (ar) |
| DO (1) | DOP2019000206A (ar) |
| EC (1) | ECSP19057713A (ar) |
| ES (1) | ES2847162T3 (ar) |
| GE (2) | GEP20217281B (ar) |
| HR (1) | HRP20210143T1 (ar) |
| HU (1) | HUE053191T2 (ar) |
| IL (1) | IL268469B (ar) |
| JO (1) | JOP20190193B1 (ar) |
| LT (1) | LT3580211T (ar) |
| MA (1) | MA47447B1 (ar) |
| MX (1) | MX2019009571A (ar) |
| MY (1) | MY198510A (ar) |
| NI (1) | NI201900085A (ar) |
| PE (1) | PE20191496A1 (ar) |
| PH (1) | PH12019501846A1 (ar) |
| PL (1) | PL3580211T3 (ar) |
| RS (1) | RS61401B1 (ar) |
| SA (1) | SA519402422B1 (ar) |
| SG (1) | SG11201907232XA (ar) |
| SI (1) | SI3580211T1 (ar) |
| TW (1) | TWI770113B (ar) |
| UA (1) | UA124507C2 (ar) |
| UY (1) | UY37606A (ar) |
| WO (1) | WO2018146010A1 (ar) |
| ZA (1) | ZA201905902B (ar) |
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| EA201892666A1 (ru) * | 2016-05-25 | 2019-08-30 | Байер Фарма Акциенгезельшафт | 3-оксо-2,6-дифенил-2,3-дигидропиридазин-4-карбоксамиды |
| CN116531380B (zh) | 2017-02-09 | 2025-11-07 | 拜耳股份公司 | 用于治疗癌症的2-杂芳基-3-氧代-2,3-二氢哒嗪-4-甲酰胺 |
| CN109813913B (zh) * | 2019-01-31 | 2021-11-09 | 中国医学科学院肿瘤医院 | 芳烃受体(AhR)在预测免疫治疗效果中的应用 |
| EP3715471A1 (en) * | 2019-03-29 | 2020-09-30 | Deutsches Krebsforschungszentrum, Stiftung des öffentlichen Rechts | Ahr signature marker set |
| EP3721894A1 (en) | 2019-04-10 | 2020-10-14 | Deutsches Krebsforschungszentrum, Stiftung des öffentlichen Rechts | Interleukin-4-induced gene 1 (il4i1) as a biomarker and uses thereof |
| CN112724256B (zh) * | 2019-10-28 | 2022-09-16 | 中国农业大学 | 一种高稳定性的磺胺类药物抗体hAb 4D11及其应用 |
| EP3835432A1 (en) | 2019-12-10 | 2021-06-16 | Deutsches Krebsforschungszentrum, Stiftung des öffentlichen Rechts | Interleukin-4-induced gene 1 (il4i1) and respective metabolites as biomarkers for cancer |
| CA3164474A1 (en) | 2019-12-16 | 2021-06-24 | Bayer Aktiengesellschaft | Combination of an ahr-inhibitor and an pd1-inhibitor antibody and its use in the treatment of cancer |
| KR20220153595A (ko) | 2020-02-26 | 2022-11-18 | 재규어 테라퓨틱스 피티이 리미티드 | AhR 신호전달의 조절에 유용한 피리도피리미딘 유도체 |
| US20230150970A1 (en) * | 2020-03-27 | 2023-05-18 | Dong-A St Co., Ltd. | Aminopyrimidine derivatives and their use as aryl hydrocarbon receptor modulators |
| US12570638B2 (en) | 2020-05-20 | 2026-03-10 | Sail Biomedicines, Inc. | Fused imidazole derivatives as AHR antagonists |
| CN114181212B (zh) * | 2020-09-15 | 2023-06-06 | 山东轩竹医药科技有限公司 | 哒嗪酮类AhR抑制剂 |
| WO2022078356A1 (zh) * | 2020-10-15 | 2022-04-21 | 山东轩竹医药科技有限公司 | 杂芳环类AhR抑制剂 |
| CN114539221A (zh) * | 2020-11-27 | 2022-05-27 | 苏州泽璟生物制药股份有限公司 | 氘代2-芳杂环-3-氧-2,3-二氢哒嗪-4-甲酰胺类抑制剂及其制备方法和应用 |
| CN114685426A (zh) * | 2020-12-28 | 2022-07-01 | 苏州泽璟生物制药股份有限公司 | 磺酰胺类抑制剂及其制备方法和应用 |
| CN114835687B (zh) * | 2021-04-02 | 2023-09-05 | 北京华森英诺生物科技有限公司 | AhR抑制剂 |
| CN118234710A (zh) * | 2021-09-14 | 2024-06-21 | 元启(苏州)生物制药有限公司 | 2-芳基或杂芳基-3-氧代-4-甲酰胺-6-环-二氢吡嗪芳基烃受体调节剂和其在治疗疾病和病症中的用途 |
| US20230190961A1 (en) | 2021-10-20 | 2023-06-22 | University Of Rochester | Compositions and methods for treating myelin deficiency by rejuvenating glial progenitor cells |
| CN119948035A (zh) | 2022-10-03 | 2025-05-06 | 捷豹治疗有限公司 | 可用于调节AhR信号传导的化合物 |
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