HRP20211927T1 - Derivati spojenih pentacikličnih imidazola kao modulatori aktivnosti tnf - Google Patents
Derivati spojenih pentacikličnih imidazola kao modulatori aktivnosti tnf Download PDFInfo
- Publication number
- HRP20211927T1 HRP20211927T1 HRP20211927TT HRP20211927T HRP20211927T1 HR P20211927 T1 HRP20211927 T1 HR P20211927T1 HR P20211927T T HRP20211927T T HR P20211927TT HR P20211927 T HRP20211927 T HR P20211927T HR P20211927 T1 HRP20211927 T1 HR P20211927T1
- Authority
- HR
- Croatia
- Prior art keywords
- methanobenzimidazo
- benzodiazocin
- difluoromethoxy
- amino
- methyl
- Prior art date
Links
- 150000002460 imidazoles Chemical class 0.000 title 1
- 229940079865 intestinal antiinfectives imidazole derivative Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 2
- UROFXMLQPAUCGV-WOJBJXKFSA-N (1R,11R)-5-[2-(1-aminocyclobutyl)pyrimidin-5-yl]-18-(difluoromethoxy)-12-methyl-2,9,12-triazapentacyclo[9.8.1.02,10.03,8.014,19]icosa-3(8),4,6,9,14(19),15,17-heptaen-13-one Chemical compound CN1[C@@H]2C[C@H](c3c(OC(F)F)cccc3C1=O)n1c2nc2ccc(cc12)-c1cnc(nc1)C1(N)CCC1 UROFXMLQPAUCGV-WOJBJXKFSA-N 0.000 claims 1
- SFCCDCHZSHIFBN-UPCIGPOOSA-N (1R,11R)-5-[6-[(1R,2S)-1-amino-2-methylcyclobutyl]-5-fluoropyridin-3-yl]-18-(difluoromethoxy)-2,9,12-triazapentacyclo[9.8.1.02,10.03,8.014,19]icosa-3(8),4,6,9,14(19),15,17-heptaen-13-one Chemical compound N[C@]1([C@H](CC1)C)C1=C(C=C(C=N1)C=1C=CC2=C(C=1)N1[C@H]3C4=C(C(N[C@@H](C1=N2)C3)=O)C=CC=C4OC(F)F)F SFCCDCHZSHIFBN-UPCIGPOOSA-N 0.000 claims 1
- SFCCDCHZSHIFBN-GCOUEFSDSA-N (1R,11R)-5-[6-[(1S,2R)-1-amino-2-methylcyclobutyl]-5-fluoropyridin-3-yl]-18-(difluoromethoxy)-2,9,12-triazapentacyclo[9.8.1.02,10.03,8.014,19]icosa-3(8),4,6,9,14(19),15,17-heptaen-13-one Chemical compound C[C@@H]1CC[C@@]1(N)C1=C(F)C=C(C=N1)C1=CC2=C(C=C1)N=C1[C@H]3C[C@@H](N21)C1=C(C=CC=C1OC(F)F)C(=O)N3 SFCCDCHZSHIFBN-GCOUEFSDSA-N 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- -1 cyano, hydroxy Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000030533 eye disease Diseases 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 230000000926 neurological effect Effects 0.000 claims 1
- 230000003040 nociceptive effect Effects 0.000 claims 1
- 230000000771 oncological effect Effects 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Classifications
-
- 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
-
- 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
- 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
Landscapes
- 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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP17168027 | 2017-04-25 | ||
| PCT/EP2018/060489 WO2018197503A1 (en) | 2017-04-25 | 2018-04-24 | Fused pentacyclic imidazole derivatives as modulators of tnf activity |
| EP18719178.8A EP3615534B1 (en) | 2017-04-25 | 2018-04-24 | Fused pentacyclic imidazole derivatives as modulators of tnf activity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20211927T1 true HRP20211927T1 (hr) | 2022-03-18 |
Family
ID=58632834
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20211927TT HRP20211927T1 (hr) | 2017-04-25 | 2018-04-24 | Derivati spojenih pentacikličnih imidazola kao modulatori aktivnosti tnf |
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)
| 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 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9550737B2 (en) * | 2012-06-11 | 2017-01-24 | Ucb Biopharma Sprl | TNF -α modulating benzimidazoles |
| 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 |
| MX380578B (es) * | 2014-10-03 | 2025-03-12 | Ucb Biopharma Sprl | Derivados de imidazol pentaciclicos fusionados. |
| EP3288939A1 (en) * | 2015-04-17 | 2018-03-07 | AbbVie Inc. | Tricyclic modulators of tnf signaling |
-
2018
- 2018-04-24 AU AU2018259040A patent/AU2018259040B2/en active Active
- 2018-04-24 CN CN201880025894.6A patent/CN110582495B/zh active Active
- 2018-04-24 CA CA3058980A patent/CA3058980A1/en active Pending
- 2018-04-24 EP EP18719178.8A patent/EP3615534B1/en active Active
- 2018-04-24 MX MX2019012443A patent/MX2019012443A/es unknown
- 2018-04-24 SI SI201830491T patent/SI3615534T1/sl unknown
- 2018-04-24 HR HRP20211927TT patent/HRP20211927T1/hr unknown
- 2018-04-24 SG SG11201908871S patent/SG11201908871SA/en unknown
- 2018-04-24 HU HUE18719178A patent/HUE056593T2/hu unknown
- 2018-04-24 PL PL21189378.9T patent/PL3939980T3/pl unknown
- 2018-04-24 CR CR20190526A patent/CR20190526A/es unknown
- 2018-04-24 ES ES18719178T patent/ES2893807T3/es active Active
- 2018-04-24 PH PH1/2019/502182A patent/PH12019502182B1/en unknown
- 2018-04-24 MY MYPI2019005903A patent/MY197212A/en unknown
- 2018-04-24 EP EP21189378.9A patent/EP3939980B1/en active Active
- 2018-04-24 LT LTEPPCT/EP2018/060489T patent/LT3615534T/lt unknown
- 2018-04-24 RS RS20211403A patent/RS62596B1/sr unknown
- 2018-04-24 ES ES21189378T patent/ES2956555T3/es active Active
- 2018-04-24 JP JP2019556874A patent/JP7083358B2/ja active Active
- 2018-04-24 TW TW107113777A patent/TWI801378B/zh active
- 2018-04-24 MA MA49055A patent/MA49055B1/fr unknown
- 2018-04-24 PT PT211893789T patent/PT3939980T/pt unknown
- 2018-04-24 DK DK18719178.8T patent/DK3615534T3/da active
- 2018-04-24 PE PE2019002028A patent/PE20200662A1/es unknown
- 2018-04-24 PT PT187191788T patent/PT3615534T/pt unknown
- 2018-04-24 PL PL18719178T patent/PL3615534T3/pl unknown
- 2018-04-24 EA EA201992407A patent/EA039049B1/ru unknown
- 2018-04-24 WO PCT/EP2018/060489 patent/WO2018197503A1/en not_active Ceased
- 2018-04-24 US US16/497,217 patent/US10980814B2/en active Active
- 2018-04-24 KR KR1020197034032A patent/KR102565132B1/ko active Active
- 2018-04-25 AR ARP180101067A patent/AR111426A1/es active IP Right Grant
- 2018-04-25 PY PY201801829804A patent/PY1829804A/es unknown
- 2018-04-25 UY UY0001037700A patent/UY37700A/es not_active Application Discontinuation
- 2018-08-24 MA MA57699A patent/MA57699B1/fr unknown
-
2019
- 2019-09-20 ZA ZA2019/06255A patent/ZA201906255B/en unknown
- 2019-10-07 IL IL269890A patent/IL269890B/en unknown
- 2019-10-09 CL CL2019002875A patent/CL2019002875A1/es unknown
- 2019-11-18 CO CONC2019/0012856A patent/CO2019012856A2/es unknown
-
2021
- 2021-02-15 US US17/176,018 patent/US20210252012A1/en not_active Abandoned
-
2022
- 2022-05-31 JP JP2022088172A patent/JP7299382B2/ja active Active
-
2023
- 2023-02-27 US US18/175,030 patent/US20230250105A1/en not_active Abandoned
-
2024
- 2024-08-29 US US18/819,527 patent/US20250127795A1/en active Pending
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