AU2018259040B2 - Fused pentacyclic imidazole derivatives as modulators of TNF activity - Google Patents

Fused pentacyclic imidazole derivatives as modulators of TNF activity Download PDF

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Publication number
AU2018259040B2
AU2018259040B2 AU2018259040A AU2018259040A AU2018259040B2 AU 2018259040 B2 AU2018259040 B2 AU 2018259040B2 AU 2018259040 A AU2018259040 A AU 2018259040A AU 2018259040 A AU2018259040 A AU 2018259040A AU 2018259040 B2 AU2018259040 B2 AU 2018259040B2
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disorder
methyl
mmol
difluoromethoxy
methanobenzimidazo
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AU2018259040A
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AU2018259040A1 (en
Inventor
Daniel Christopher Brookings
Teresa DE HARO GARCIA
Yann Foricher
Helen Tracey Horsley
Martin Clive Hutchings
James Andrew Johnson
Malcolm Maccoss
Mengyang XUAN
Zhaoning Zhu
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UCB Biopharma SRL
Sanofi SA
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UCB Biopharma SRL
Sanofi SA
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Publication of AU2018259040A1 publication Critical patent/AU2018259040A1/en
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    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2018259040A 2017-04-25 2018-04-24 Fused pentacyclic imidazole derivatives as modulators of TNF activity Active AU2018259040B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP17168027 2017-04-25
EP17168027.5 2017-04-25
PCT/EP2018/060489 WO2018197503A1 (en) 2017-04-25 2018-04-24 Fused pentacyclic imidazole derivatives as modulators of tnf activity

Publications (2)

Publication Number Publication Date
AU2018259040A1 AU2018259040A1 (en) 2019-10-31
AU2018259040B2 true AU2018259040B2 (en) 2022-04-28

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ID=58632834

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AU2018259040A Active AU2018259040B2 (en) 2017-04-25 2018-04-24 Fused pentacyclic imidazole derivatives as modulators of TNF activity

Country Status (33)

Country Link
US (4) US10980814B2 (https=)
EP (2) EP3615534B1 (https=)
JP (2) JP7083358B2 (https=)
KR (1) KR102565132B1 (https=)
CN (1) CN110582495B (https=)
AR (1) AR111426A1 (https=)
AU (1) AU2018259040B2 (https=)
CA (1) CA3058980A1 (https=)
CL (1) CL2019002875A1 (https=)
CO (1) CO2019012856A2 (https=)
CR (1) CR20190526A (https=)
DK (1) DK3615534T3 (https=)
EA (1) EA039049B1 (https=)
ES (2) ES2893807T3 (https=)
HR (1) HRP20211927T1 (https=)
HU (1) HUE056593T2 (https=)
IL (1) IL269890B (https=)
LT (1) LT3615534T (https=)
MA (2) MA49055B1 (https=)
MX (1) MX2019012443A (https=)
MY (1) MY197212A (https=)
PE (1) PE20200662A1 (https=)
PH (1) PH12019502182B1 (https=)
PL (2) PL3939980T3 (https=)
PT (2) PT3939980T (https=)
PY (1) PY1829804A (https=)
RS (1) RS62596B1 (https=)
SG (1) SG11201908871SA (https=)
SI (1) SI3615534T1 (https=)
TW (1) TWI801378B (https=)
UY (1) UY37700A (https=)
WO (1) WO2018197503A1 (https=)
ZA (1) ZA201906255B (https=)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10766906B2 (en) * 2016-04-01 2020-09-08 UCB Biopharma SRL Fused hexacyclic imidazole derivatives as modulators of TNF activity
WO2018119142A1 (en) 2016-12-21 2018-06-28 Amgen Inc. Anti-tnf alpha antibody formulations
CA3117344A1 (en) * 2018-10-24 2020-04-30 UCB Biopharma SRL Fused pentacyclic imidazole derivatives as modulators of tnf activity
CN120418259A (zh) 2022-11-23 2025-08-01 弗沃德医疗公司 TNFα活性的调节剂
TW202508596A (zh) 2023-04-26 2025-03-01 法商賽諾菲公司 使用腫瘤壞死因子α之小分子抑制劑治療乾癬
WO2024251282A1 (zh) * 2023-06-09 2024-12-12 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
TW202519231A (zh) 2023-07-04 2025-05-16 法商賽諾菲公司 結晶形式
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
WO2025068505A1 (en) 2023-09-29 2025-04-03 Sanofi Preparation of bridged pentacyclic imidazole derivatives as modulators of tnf activity, intermeditates and their preparation
TW202602881A (zh) * 2024-03-27 2026-01-16 大陸商海思科醫藥集團股份有限公司 雜環衍生物及其在醫藥上的應用
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
WO2025247401A1 (zh) * 2024-05-31 2025-12-04 海思科医药集团股份有限公司 一种稠合杂环衍生物及其在医药上的应用
WO2025252251A1 (zh) * 2024-06-07 2025-12-11 上海翰森生物医药科技有限公司 含氧杂环类衍生物抑制剂、其制备方法和应用
WO2026012303A1 (en) * 2024-07-09 2026-01-15 Hangzhou Highlightll Pharmaceutical Co., Ltd NOVEL BENZO [4, 5] IMIDAZO COMPOUNDS AS TNFα MODULATORS
WO2026022134A1 (en) 2024-07-23 2026-01-29 Sanofi Novel aminocarbonylation processes
WO2026021586A1 (zh) * 2024-07-26 2026-01-29 上海瀚辰星泰医药科技有限公司 一种多环化合物及其制备方法和应用
WO2026027449A1 (en) 2024-07-29 2026-02-05 Sanofi Fused pentacyclic imidazole derivatives
WO2026051930A1 (zh) * 2024-09-04 2026-03-12 苏州湃玥生物科技有限公司 一种作为tnf活性调节剂的稠合五环苯并咪唑衍生物及其制备方法和应用
WO2026055519A1 (en) 2024-09-06 2026-03-12 Rapt Therapeutics, Inc. Fused ring imidazole compounds
WO2026064602A1 (en) * 2024-09-23 2026-03-26 Synnovation Therapeutics, Inc. HETEROCYCLIC COMPOUNDS AS MODULATORS OF TNFα ACTIVITY
WO2026068677A1 (en) 2024-09-27 2026-04-02 Sanofi Processes for the preparation of fused pentacyclic imidazoles and intermediates

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20150152065A1 (en) * 2012-06-11 2015-06-04 Ucb Biopharma Sprl TNF -Alpha Modulating Benzimidazoles
WO2016050975A1 (en) * 2014-10-03 2016-04-07 Ucb Biopharma Sprl Fused pentacyclic imidazole derivatives

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201212513D0 (en) * 2012-07-13 2012-08-29 Ucb Pharma Sa Therapeutic agents
CN104619709B (zh) * 2012-07-13 2016-11-09 Ucb生物制药私人有限公司 作为tnf活性调节剂的咪唑并吡啶衍生物
GB201321728D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
EP3288939A1 (en) * 2015-04-17 2018-03-07 AbbVie Inc. Tricyclic modulators of tnf signaling

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20150152065A1 (en) * 2012-06-11 2015-06-04 Ucb Biopharma Sprl TNF -Alpha Modulating Benzimidazoles
WO2016050975A1 (en) * 2014-10-03 2016-04-07 Ucb Biopharma Sprl Fused pentacyclic imidazole derivatives

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HRP20211927T1 (hr) 2022-03-18
US20210252012A1 (en) 2021-08-19
AU2018259040A1 (en) 2019-10-31
DK3615534T3 (da) 2021-10-18
MA49055A (fr) 2021-05-05
MA57699B1 (fr) 2023-11-30
PH12019502182B1 (en) 2024-01-31
CR20190526A (es) 2020-01-07
UY37700A (es) 2018-11-30
JP7299382B2 (ja) 2023-06-27
CL2019002875A1 (es) 2020-03-06
EP3939980B1 (en) 2023-07-26
US20200046723A1 (en) 2020-02-13
KR102565132B1 (ko) 2023-08-08
SI3615534T1 (sl) 2022-01-31
AR111426A1 (es) 2019-07-10
EP3615534B1 (en) 2021-09-15
CN110582495A (zh) 2019-12-17
JP2022116233A (ja) 2022-08-09
PL3615534T3 (pl) 2022-01-31
LT3615534T (lt) 2021-11-25
TWI801378B (zh) 2023-05-11
SG11201908871SA (en) 2019-10-30
PY1829804A (es) 2019-03-01
IL269890B (en) 2022-03-01
WO2018197503A1 (en) 2018-11-01
ZA201906255B (en) 2021-01-27
ES2956555T3 (es) 2023-12-22
HUE056593T2 (hu) 2022-02-28
MA49055B1 (fr) 2021-12-31
BR112019020314A2 (pt) 2020-04-28
EA201992407A1 (ru) 2020-04-06
MX2019012443A (es) 2020-01-13
EA039049B1 (ru) 2021-11-26
KR20190141200A (ko) 2019-12-23
US20230250105A1 (en) 2023-08-10
RS62596B1 (sr) 2021-12-31
JP7083358B2 (ja) 2022-06-10
PE20200662A1 (es) 2020-06-11
EP3615534A1 (en) 2020-03-04
ES2893807T3 (es) 2022-02-10
PT3615534T (pt) 2021-10-21
US10980814B2 (en) 2021-04-20
PH12019502182A1 (en) 2020-06-08
JP2020517637A (ja) 2020-06-18
CO2019012856A2 (es) 2020-01-17
EP3939980A1 (en) 2022-01-19
PL3939980T3 (pl) 2024-02-05
TW201841918A (zh) 2018-12-01
US20250127795A1 (en) 2025-04-24
NZ758198A (en) 2024-01-26
CN110582495B (zh) 2022-04-01
PT3939980T (pt) 2023-08-07
CA3058980A1 (en) 2018-11-01
MY197212A (en) 2023-06-01

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