JP6629847B2 - 縮合五員環イミダゾール誘導体 - Google Patents

縮合五員環イミダゾール誘導体 Download PDF

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Publication number
JP6629847B2
JP6629847B2 JP2017518131A JP2017518131A JP6629847B2 JP 6629847 B2 JP6629847 B2 JP 6629847B2 JP 2017518131 A JP2017518131 A JP 2017518131A JP 2017518131 A JP2017518131 A JP 2017518131A JP 6629847 B2 JP6629847 B2 JP 6629847B2
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Japan
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alkyl
formula
heteroaryl
difluoromethoxy
optionally substituted
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Japanese (ja)
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JP2017531648A5 (enExample
JP2017531648A (ja
Inventor
ハロ ガルシア、テレサ デ
ハロ ガルシア、テレサ デ
デリグニー、マイケル
ポール ヘール、ジャグ
ポール ヘール、ジャグ
レイチェル クインシー、ジョアンナ
レイチェル クインシー、ジョアンナ
シュアン、メンヤン
チュー、チャオニン
クリストファー ブルッキングス、ダニエル
クリストファー ブルッキングス、ダニエル
ダニエル カルミアーノ、マーク
ダニエル カルミアーノ、マーク
エブラール、イブ
クライブ ハッチングス、マーティン
クライブ ハッチングス、マーティン
ジョンソン、ジェイムズ、アンドリュー
ジャド、ソフィー
キイェルツ、ジャン
コス、マルカム マック
コス、マルカム マック
ダンカン セルビー、マシュー
ダンカン セルビー、マシュー
アラン ショウ、マイケル
アラン ショウ、マイケル
ルイ レオン スウィンネン、ドミニーク
ルイ レオン スウィンネン、ドミニーク
スキオ、ローラン
フォリシェール、ヤン
− ロム、ブルーノ フィロシェ
− ロム、ブルーノ フィロシェ
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Sanofi SA
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Sanofi SA
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K31/41—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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/18—Bridged systems
    • 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
    • C07D487/08—Bridged systems
    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/12—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains three hetero rings
    • C07D493/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/18—Bridged systems
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
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    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Transplantation (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2017518131A 2014-10-03 2015-10-02 縮合五員環イミダゾール誘導体 Active JP6629847B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
EP14290299.8 2014-10-03
EP14290299 2014-10-03
EP15162641 2015-04-07
EP15162641.3 2015-04-07
EP15171036 2015-06-08
EP15171036.5 2015-06-08
PCT/EP2015/072868 WO2016050975A1 (en) 2014-10-03 2015-10-02 Fused pentacyclic imidazole derivatives

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JP2017531648A JP2017531648A (ja) 2017-10-26
JP2017531648A5 JP2017531648A5 (enExample) 2018-11-08
JP6629847B2 true JP6629847B2 (ja) 2020-01-15

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US (3) US10202405B2 (enExample)
EP (1) EP3201196B1 (enExample)
JP (1) JP6629847B2 (enExample)
KR (1) KR102442235B1 (enExample)
CN (1) CN107108672B (enExample)
AP (1) AP2017009809A0 (enExample)
AU (1) AU2015326798B2 (enExample)
BR (1) BR112017006669B1 (enExample)
CA (1) CA2962826C (enExample)
CL (1) CL2017000787A1 (enExample)
CO (1) CO2017003331A2 (enExample)
CR (1) CR20170167A (enExample)
DK (1) DK3201196T3 (enExample)
EA (1) EA032839B1 (enExample)
EC (1) ECSP17027306A (enExample)
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GT (1) GT201700044A (enExample)
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IL (1) IL251147B (enExample)
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MA (1) MA40770B1 (enExample)
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MY (1) MY181019A (enExample)
PE (1) PE20170693A1 (enExample)
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WO2016050975A1 (en) * 2014-10-03 2016-04-07 Ucb Biopharma Sprl Fused pentacyclic imidazole derivatives
EP3288939A1 (en) 2015-04-17 2018-03-07 AbbVie Inc. Tricyclic modulators of tnf signaling
UY36628A (es) 2015-04-17 2016-11-30 Abbvie Inc Indazolonas como moduladores de la señalización de tnf
UY36629A (es) 2015-04-17 2016-11-30 Abbvie Inc Indazolonas como moduladores de la señalización de tnf
GB201510758D0 (en) 2015-06-18 2015-08-05 Ucb Biopharma Sprl Novel TNFa structure for use in therapy
CA3018992A1 (en) * 2016-04-01 2017-10-05 Ucb Biopharma Sprl Fused hexacyclic imidazole derivatives as modulators of tnf activity
CN109195969B (zh) 2016-04-01 2021-12-21 Ucb生物制药私人有限公司 作为tnf活性调节剂的稠合五环咪唑衍生物
BR112018069931A2 (pt) 2016-04-01 2019-02-05 Sanofi Sa derivados de imidazol pentacíclicos fundidos como moduladores de atividade do tnf
CA3019245A1 (en) 2016-04-01 2017-10-05 Ucb Biopharma Sprl Fused pentacyclic imidazole derivatives as modulators of tnf activity
GB201620948D0 (en) 2016-12-09 2017-01-25 Ucb Biopharma Sprl Therapeutic agents
GB201621907D0 (en) 2016-12-21 2017-02-01 Ucb Biopharma Sprl And Sanofi Antibody epitope
MA47106A (fr) 2016-12-21 2019-10-30 Amgen Inc Formulations d'anticorps anti-tnf alpha
CN110461842A (zh) * 2017-03-15 2019-11-15 Ucb生物制药私人有限公司 作为tnf活性调节剂的稠合五环咪唑衍生物
CA3058980A1 (en) 2017-04-25 2018-11-01 Ucb Biopharma Sprl Fused pentacyclic imidazole derivatives as modulators of tnf activity
CA3089092A1 (en) * 2018-04-04 2019-10-10 Japan Tobacco Inc. Pyrazole compounds substituted with heteroaryl and pharmaceutical use thereof
WO2020084008A1 (en) 2018-10-24 2020-04-30 UCB Biopharma SRL Fused pentacyclic imidazole derivatives as modulators of tnf activity
CN113683505A (zh) * 2021-09-29 2021-11-23 厦门大华本安化工安全研究院有限公司 一种含氧代环丁基的羧酸酯类化合物的制备方法
CN120418259A (zh) * 2022-11-23 2025-08-01 弗沃德医疗公司 TNFα活性的调节剂
WO2024129763A1 (en) * 2022-12-13 2024-06-20 Forward Therapeutics, Inc. MODULATORS OF TNF-α ACTIVITY
WO2024148191A1 (en) * 2023-01-05 2024-07-11 Forward Therapeutics, Inc. MODULATORS OF TNF-α ACTIVITY
CN121038791A (zh) 2023-04-26 2025-11-28 赛诺菲 使用肿瘤坏死因子α的小分子抑制剂治疗银屑病
TW202513567A (zh) * 2023-06-09 2025-04-01 大陸商上海翰森生物醫藥科技有限公司 五環類衍生物抑制劑、其製備方法與應用
TW202521544A (zh) * 2023-08-16 2025-06-01 美商雷瑟拉股份有限公司 TNFα活性調節劑及其用途
TW202527952A (zh) 2023-09-29 2025-07-16 法商賽諾菲公司 合成方法
WO2025137267A1 (en) * 2023-12-21 2025-06-26 Forward Therapeutics, Inc. Modulators of tnf-alpha activity
WO2025201449A1 (zh) * 2024-03-27 2025-10-02 海思科医药集团股份有限公司 一种杂环衍生物及其在医药上的应用
WO2025212627A1 (en) * 2024-04-03 2025-10-09 Forward Therapeutics, Inc. Modulators of tnf-alpha activity
WO2025218735A1 (zh) * 2024-04-17 2025-10-23 上海翰森生物医药科技有限公司 五环类衍生物抑制剂、其制备方法和应用

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