CN107108672B - 稠合的五环咪唑衍生物 - Google Patents
稠合的五环咪唑衍生物 Download PDFInfo
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- CN107108672B CN107108672B CN201580053711.8A CN201580053711A CN107108672B CN 107108672 B CN107108672 B CN 107108672B CN 201580053711 A CN201580053711 A CN 201580053711A CN 107108672 B CN107108672 B CN 107108672B
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- alkyl
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- 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
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- A—HUMAN NECESSITIES
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- A61P25/04—Centrally acting analgesics, e.g. opioids
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
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- C—CHEMISTRY; METALLURGY
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- 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
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- C—CHEMISTRY; METALLURGY
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- 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
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- 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
- 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
- C07—ORGANIC CHEMISTRY
- 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
- C07—ORGANIC CHEMISTRY
- 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
- 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
- C07D495/12—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—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
- 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
- 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
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- 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)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Hospice & Palliative Care (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Psychiatry (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Transplantation (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)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14290299 | 2014-10-03 | ||
| EP14290299.8 | 2014-10-03 | ||
| EP15162641.3 | 2015-04-07 | ||
| EP15162641 | 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN107108672A CN107108672A (zh) | 2017-08-29 |
| CN107108672B true CN107108672B (zh) | 2019-11-08 |
Family
ID=54238452
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201580053711.8A Active CN107108672B (zh) | 2014-10-03 | 2015-10-02 | 稠合的五环咪唑衍生物 |
Country Status (36)
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3201196B1 (en) * | 2014-10-03 | 2021-07-28 | UCB Biopharma SRL | Fused pentacyclic imidazole derivatives |
| TW201706258A (zh) | 2015-04-17 | 2017-02-16 | 艾伯維有限公司 | 作為tnf信號傳遞調節劑之吲唑酮 |
| WO2016168638A1 (en) | 2015-04-17 | 2016-10-20 | Abbvie Inc. | Indazolones as modulators of tnf signaling |
| EP3288939A1 (en) | 2015-04-17 | 2018-03-07 | AbbVie Inc. | Tricyclic modulators of tnf signaling |
| GB201510758D0 (en) | 2015-06-18 | 2015-08-05 | Ucb Biopharma Sprl | Novel TNFa structure for use in therapy |
| BR112018069941A2 (pt) | 2016-04-01 | 2019-02-05 | Sanofi Sa | derivados de imidazol pentacíclicos fundidos como moduladores de atividade do tnf |
| CA3018992A1 (en) * | 2016-04-01 | 2017-10-05 | Ucb Biopharma Sprl | Fused hexacyclic imidazole derivatives as modulators of tnf activity |
| BR112018069931A2 (pt) | 2016-04-01 | 2019-02-05 | Sanofi Sa | derivados de imidazol pentacíclicos fundidos como moduladores de atividade do tnf |
| CA3019026A1 (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 |
| EP3558363A1 (en) | 2016-12-21 | 2019-10-30 | Amgen Inc. | Anti-tnf alpha antibody formulations |
| GB201621907D0 (en) | 2016-12-21 | 2017-02-01 | Ucb Biopharma Sprl And Sanofi | Antibody epitope |
| WO2018167176A1 (en) | 2017-03-15 | 2018-09-20 | Ucb Biopharma Sprl | Fused pentacyclic imidazole derivatives as modulators of tnf activity |
| SG11201908871SA (en) | 2017-04-25 | 2019-10-30 | Ucb Biopharma Sprl | Fused pentacyclic imidazole derivatives as modulators of tnf activity |
| WO2019194207A1 (ja) * | 2018-04-04 | 2019-10-10 | 日本たばこ産業株式会社 | ヘテロアリールで置換されたピラゾール化合物及びその医薬用途 |
| ES2951837T3 (es) * | 2018-10-24 | 2023-10-25 | UCB Biopharma SRL | Derivados de imidazol pentacíclicos condensados como moduladores de la actividad de TNF |
| 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 |
| JP2025540024A (ja) * | 2022-11-23 | 2025-12-11 | フォワード セラピューティクス, インコーポレイテッド | TNF-α活性の調節因子 |
| 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 |
| 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 |
| 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 |
| WO2025038927A1 (en) * | 2023-08-16 | 2025-02-20 | Raythera, Inc. | Modulators of tnf alpha activity and uses thereof |
| 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 |
| WO2025244936A1 (en) * | 2024-05-20 | 2025-11-27 | Forward Therapeutics, Inc. | Modulators of tnf-alpha activity |
| 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 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013186229A1 (en) * | 2012-06-11 | 2013-12-19 | Ucb Pharma S.A. | Tnf -alpha modulating benzimidazoles |
| WO2014009295A1 (en) * | 2012-07-13 | 2014-01-16 | Ucb Pharma S.A. | Imidazopyridine derivatives as modulators of tnf activity |
| WO2014009296A1 (en) * | 2012-07-13 | 2014-01-16 | Ucb Pharma S.A. | Imidazopyrazine derivatives as modulators of tnf activity |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0449649A3 (en) | 1990-03-30 | 1992-09-02 | Arizona Board Of Regents, Arizona State University | Antineoplastic quinones and methods of using same |
| FR2832711B1 (fr) | 2001-11-26 | 2004-01-30 | Warner Lambert Co | Derives de triazolo [4,3-a] pyrido [2,3-d] pyrimidin-5-ones, compositions les contenant, procede de preparation et utilisation |
| EP1603926A1 (en) | 2003-03-10 | 2005-12-14 | Pfizer Inc. | Phosphate/sulfate ester compounds and pharmaceutical compositions for inhibiting protein interacting nima (pin1) |
| DE102008030206A1 (de) | 2008-06-25 | 2009-12-31 | Bayer Schering Pharma Aktiengesellschaft | 3-Cyanoalky- und 3-Hydroxyalkyl-Indole und ihre Verwendung |
| AR088728A1 (es) | 2011-03-25 | 2014-07-02 | Bristol Myers Squibb Co | Moduladores de lxr como prodroga de imidazol |
| KR101941420B1 (ko) | 2011-06-20 | 2019-01-23 | 스페로 트리넴, 인코포레이티드 | 자이라제 및 토포이소머라제 억제제의 인산에스테르 |
| AU2014338549B2 (en) | 2013-10-25 | 2017-05-25 | Novartis Ag | Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors |
| GB201321728D0 (en) | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| GB201321729D0 (en) | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| CA2944140C (en) | 2014-04-15 | 2022-10-04 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases |
| EP3201196B1 (en) * | 2014-10-03 | 2021-07-28 | UCB Biopharma SRL | Fused pentacyclic imidazole derivatives |
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2015
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- 2015-10-02 US US15/513,357 patent/US10202405B2/en active Active
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- 2015-10-02 KR KR1020177011958A patent/KR102442235B1/ko active Active
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| WO2013186229A1 (en) * | 2012-06-11 | 2013-12-19 | Ucb Pharma S.A. | Tnf -alpha modulating benzimidazoles |
| WO2014009295A1 (en) * | 2012-07-13 | 2014-01-16 | Ucb Pharma S.A. | Imidazopyridine derivatives as modulators of tnf activity |
| WO2014009296A1 (en) * | 2012-07-13 | 2014-01-16 | Ucb Pharma S.A. | Imidazopyrazine derivatives as modulators of tnf activity |
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