KR20250151389A - 치환 피라졸로피리미딘 화합물 및 그의 의약 용도 - Google Patents
치환 피라졸로피리미딘 화합물 및 그의 의약 용도Info
- Publication number
- KR20250151389A KR20250151389A KR1020257027024A KR20257027024A KR20250151389A KR 20250151389 A KR20250151389 A KR 20250151389A KR 1020257027024 A KR1020257027024 A KR 1020257027024A KR 20257027024 A KR20257027024 A KR 20257027024A KR 20250151389 A KR20250151389 A KR 20250151389A
- Authority
- KR
- South Korea
- Prior art keywords
- alkyl
- group
- substituted
- compound
- disease
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- 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
- 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
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- C07D487/04—Ortho-condensed 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JPJP-P-2023-027432 | 2023-02-24 | ||
| JP2023027432 | 2023-02-24 | ||
| PCT/JP2024/006433 WO2024177127A1 (ja) | 2023-02-24 | 2024-02-22 | 置換ピラゾロピリミジン化合物及びその医薬用途 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20250151389A true KR20250151389A (ko) | 2025-10-21 |
Family
ID=92501386
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020257027024A Pending KR20250151389A (ko) | 2023-02-24 | 2024-02-22 | 치환 피라졸로피리미딘 화합물 및 그의 의약 용도 |
Country Status (13)
| Country | Link |
|---|---|
| EP (1) | EP4671247A1 (https=) |
| JP (2) | JP7737490B2 (https=) |
| KR (1) | KR20250151389A (https=) |
| CN (1) | CN120752239A (https=) |
| AR (1) | AR131919A1 (https=) |
| AU (1) | AU2024226032A1 (https=) |
| CL (1) | CL2025002505A1 (https=) |
| CO (1) | CO2025011311A2 (https=) |
| IL (1) | IL322520A (https=) |
| MX (1) | MX2025009965A (https=) |
| PE (1) | PE20252572A1 (https=) |
| TW (1) | TW202448887A (https=) |
| WO (1) | WO2024177127A1 (https=) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN120230110A (zh) * | 2023-12-31 | 2025-07-01 | 杭州百新生物医药科技有限公司 | 吡唑并嘧啶类化合物及其医药用途 |
| WO2025153532A1 (en) | 2024-01-16 | 2025-07-24 | NodThera Limited | Nlrp3 inhibitors and glp-1 agonists combination therapies |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10005781B2 (en) * | 2013-10-30 | 2018-06-26 | Shanghai Hengrui Pharmaceutical Co., Ltd. | Pyrazolopyrimidone or pyrrolotriazone derivatives, method of preparing same, and pharmaceutical applications thereof |
| WO2017205766A1 (en) * | 2016-05-27 | 2017-11-30 | Pharmacyclics Llc | Inhibitors of interleukin-1 receptor-associated kinase |
| ES2930151T3 (es) * | 2019-01-14 | 2022-12-07 | Innate Tumor Immunity Inc | Moduladores heterocíclicos de NLRP3, para su uso en el tratamiento del cáncer |
| EP3911641A1 (en) * | 2019-01-14 | 2021-11-24 | Innate Tumor Immunity, Inc. | Nlrp3 modulators |
| US20230399319A1 (en) * | 2019-12-27 | 2023-12-14 | Japan Tobacco Inc. | Acylsulfamide Compound and Pharmaceutical Use Therefor |
| US20240382488A1 (en) * | 2021-03-29 | 2024-11-21 | Halia Therapeutics, Inc. | Nek7 inhibitors |
| JP2024513227A (ja) * | 2021-04-05 | 2024-03-22 | ハリア・セラピューティクス・インコーポレイテッド | Nek7阻害剤 |
| WO2023032987A1 (ja) * | 2021-08-31 | 2023-03-09 | 日本たばこ産業株式会社 | 6-アミノピラゾロピリミジン化合物及びその医薬用途 |
| AR130318A1 (es) * | 2022-08-29 | 2024-11-27 | Japan Tobacco Inc | Compuestos de pirazolopirimidina y su uso médico |
| EP4694980A1 (en) * | 2023-04-14 | 2026-02-18 | Takeda Pharmaceutical Company Limited | Pyrazolopyrimidine derivatives as inhibitors of nlrp3 |
-
2024
- 2024-02-22 WO PCT/JP2024/006433 patent/WO2024177127A1/ja not_active Ceased
- 2024-02-22 EP EP24760425.9A patent/EP4671247A1/en active Pending
- 2024-02-22 KR KR1020257027024A patent/KR20250151389A/ko active Pending
- 2024-02-22 CN CN202480014319.1A patent/CN120752239A/zh active Pending
- 2024-02-22 AU AU2024226032A patent/AU2024226032A1/en active Pending
- 2024-02-22 TW TW113106397A patent/TW202448887A/zh unknown
- 2024-02-22 JP JP2024025063A patent/JP7737490B2/ja active Active
- 2024-02-22 PE PE2025001836A patent/PE20252572A1/es unknown
- 2024-02-22 IL IL322520A patent/IL322520A/en unknown
- 2024-02-22 AR ARP240100407A patent/AR131919A1/es unknown
-
2025
- 2025-08-20 CL CL2025002505A patent/CL2025002505A1/es unknown
- 2025-08-21 CO CONC2025/0011311A patent/CO2025011311A2/es unknown
- 2025-08-22 MX MX2025009965A patent/MX2025009965A/es unknown
- 2025-08-29 JP JP2025143871A patent/JP2025176085A/ja active Pending
Non-Patent Citations (86)
| Title |
|---|
| Akosua Vilaysane et al., The NLRP3 Inflammasome Promotes Renal Inflammation and Contributes to CKD. J Am Soc Nephrol. 2010 Oct; 21(10): 1732-1744. |
| Alcocer-Gomez E et al., NLRP3 inflammasome is activated in mononuclear blood cells from patients with major depressive disorder. Brain Behav Immun. 2014 Feb; 36: 111-7. |
| Amo-Aparicio J et al., Inhibition of the NLRP3 inflammasome by OLT1177 induces functional protection and myelin preservation after spinal cord injury. Exp Neurol. 2022 Jan; 347: 113889. |
| Andersson, A et al., Pivotal advance: HMGB1 expression in active lesions of human and experimental multiple sclerosis. J Leukoc Biol., 2008, Vol 84(5), p. 1248-55 |
| Bauer c. et al., Protective and aggravating effects of NLRP3 inlammasome activation in IBD models: influence of genetic and environmental factors. Dig. Dis 2012vol 30suppl 182-90. |
| Benjamin J Fowler, et al., Nucleoside reverse transcriptase inhibitors possess intrinsic anti-inflammatory activity, Science. 2014 Nov 21; 346(6212): 1000-3. |
| Bing Li, et al., Early onset drusen and RPE dysfunction in a patient with NLRP3-AID, Ocul Immunol Inflamm. 2022 Nov 17; 1-4. |
| Broderick L et al., The inflammasomes and autoinflammatory syndromes. Annu Rev Pathol. 2015; 10: 395-424. |
| Brydges SD et al., Divergence of IL-1, IL-18, and cell death in NLRP3 inflammasomopathies. J Clin Invest. 2013 Nov; 123(11): 4695-705. |
| Chen KP et al., A selective inhibitor of the NLRP3 inflammasome as a potential therapeutic approach for neuroprotection in a transgenic mouse model of Huntington's disease. J Neuroinflammation. 2022 Feb 26; 19(1): 56. |
| De Benedetti F et al., canakinumab for the Treatment of Autoinflammatory Recurrent Fever Syndromes. N Engl J Med. 2018 May 17; 378(20): 1908-1919. |
| Dellalibera-Joviliano R et al., Kinins and cytokines in plasma and cerebrospinal fluid of patients with neuropsychiatric lupus. J Rheumatol. 2003 Mar; 30(3): 485-92. |
| Dempsey C et al., . Inhibiting the NLRP3 inflammasome with MCC950 promotes non-phlogistic clearance of amyloid-β and cognitive function in APP/PS1 mice. Brain Behav Immun. 2017 Mar; 61: 306-316. |
| Denis, G et al., NLRP3 Plays a Critical Role in the Development of Experimental Autoimmune Encephalomyelitis by Mediating Th1 and Th17 Responses. J Immunol., 2010, Vol 185(2) p974-981 |
| Deora V et al., The microglial NLRP3 inflammasome is activated by amyotrophic lateral sclerosis proteins. Glia. 2020 Feb; 68(2): 407-421. |
| Ding H et al., Fisetin ameliorates cognitive impairment by activating mitophagy and suppressing neuroinflammation in rats with sepsis-associated encephalopathy. CNS Neurosci Ther. 2022 Feb; 28(2): 247-258. |
| Duewell P et al., NLRP3 inflammasomes are required for atherogenesis and activated by cholesterol crystals. Nature. 2010 Apr 29; 464(7293): 1357-61. |
| Emmi G et al., Efficacy and safety profile of anti-interleukin-1treatment in Behcet's disease: a multicenter retrospective study. Clin. Rheumatol., 35(2016), pp. 1281-1286. |
| Fann DY et al., Intravenous immunoglobulin suppresses NLRP1 and NLRP3 inflammasome-mediated neuronal death in ischemic stroke. Cell Death Dis. 2013 Sep 5; 4(9): e790. |
| Feng L et al., P2X7R blockade prevents NLRP3 inflammasome activation and brain injury in a rat model of intracerebral hemorrhage: involvement of peroxynitrite. J Neuroinflammation. 2015 Oct 17; 12: 190. |
| Fu Q et al., NLRP3/Caspase-1 Pathway-Induced Pyroptosis Mediated Cognitive Deficits in a Mouse Model of Sepsis-Associated Encephalopathy. Inflammation. 2019 Feb; 42(1): 306-318. |
| Funatsu 영양, 황반 부종의 치료 진보, 당뇨병 48(10): 721-723, 2005. |
| Garg M et al., rilonacept maintains long-term inflammatory remission in patients with deficiency of the IL-1 receptor antagonist. JCI Insight. 2017 Aug 17; 2(16). |
| Gong W et al., NLRP3 deletion protects against renal fibrosis and attenuates mitochondrial abnormality in mouse with 5/6nephrectomy. Am J Physiol Renal Physiol. 2016 May 15; 310(10): F1081-8 |
| Gordon R et al., Inflammasome inhibition prevents α-synuclein pathology and dopaminergic neurodegeneration in mice. Sci Transl Med. 2018 Oct 31; 10(465): eaah4066. |
| Guangrui Chai et al., NLRP3 Blockade Suppresses Pro-Inflammatory and Pro-Angiogenic Cytokine Secretion in Diabetic Retinopathy. Diabetes Metab Syndr Obes. 2020 Aug 25; 13: 3047-3058. |
| Guo, C et al., Development and Characterization of a Hydroxyl-Sulfonamide Analogue, 5-Chloro-N-[2-(4-hydroxysulfamoyl-phenyl)-ethyl]-2-methoxy-benzamide, as a Novel NLRP3 Inflammasome Inhibitor for Potential Treatment of Multiple Sclerosis. ACS Chem Neurosci., 2017, Vol 8(10), p2194-2201 |
| Heneka MT et al., NLRP3 is activated in Alzheimer's disease and contributes to pathology in APP/PS1mice. Nature. 2013 Jan 31; 493(7434): 674-8. |
| Hernandez-Pedro, N et al., PAMP-DAMPs interactions mediates development and progression of multiple sclerosis. Front Biosci(Schol Ed), 2016, Vol 8, p13-28. |
| Ising C, et al., NLRP3 inflammasome activation drives tau pathology. Nature. 2019 Nov; 575(7784): 669-673. |
| Ismael S et al., MCC950, the Selective Inhibitor of Nucleotide Oligomerization Domain-Like Receptor Protein-3 Inflammasome, Protects Mice against Traumatic Brain Injury. J Neurotrauma. 2018 Jun 1; 35(11): 1294-1303. |
| Iwata M et al., Psychological Stress Activates the Inflammasome via Release of Adenosine Triphosphate and Stimulation of the Purinergic Type 2X7 Receptor. Biol Psychiatry. 2016 Jul 1; 80(1): 12-22. |
| J. A Diaz-Perez et al., Extracellular ATP and IL-23 Form a Local Inflammatory Circuit Leading to the Development of a Neutrophil-Dependent Psoriasiform Dermatitis. J Invest Dermatol. (2018) 138: 2595-605. |
| Jha, S et al., The inflammasome sensor, NLRP3, regulates CNS inflammation and demyelination via caspase-1 and interleukin-18. J Neurosci., 2010 Vol 30(47), p15811-20 |
| Jia M et al., Activation of NLRP3 inflammasome in peripheral nerve contributes to paclitaxel-induced neuropathic pain. Mol Pain. 2017 Jan-Dec; 13: 1744806917719804. |
| Jiang H et al., Identification of a selective and direct NLRP3 inhibitor to treat inflammatory disorders. J Exp Med. 2017 Nov 6; 214(11): 3219-3238. |
| Jiao J et al., MCC950, a Selective Inhibitor of NLRP3 Inflammasome, Reduces the Inflammatory Response and Improves Neurological Outcomes in Mice Model of Spinal Cord Injury. Front Mol Biosci. 2020 Mar 3; 7: 37. |
| Johann S et al., NLRP3 inflammasome is expressed by astrocytes in the SOD1mouse model of ALS and in human sporadic ALS patients. Glia. 2015 Dec; 63(12): 2260-73. |
| Joni A Turunen, et al., Keratoendotheliitis Fugax Hereditaria: A Novel Cryopyrin-Associated Periodic Syndrome Caused by a Mutation in the Nucleotide-Binding Domain, Leucine-Rich Repeat Family, Pyrin Domain-Containing 3(NLRP3) Gene, Am J Ophthalmol. 2018 Apr; 188: 41-50. |
| Junge G et al., Adult onset Still's disease-The evidence that anti-interleukin-1treatment is effective and well-tolerated(a comprehensive literature review). Seminars in Arthritis Rheumatism 2017 Oct; 47(2): 295-302. |
| Kawaguchi M et al., Inflammasome activation of cardiac fibroblasts is essential for myocardial ischemia/reperfusion injury. Circulation. 2011 Feb 15; 123(6): 594-604. |
| Keke Ge, et al., Down-expression of the NLRP3 inflammasome delays the progression of diabetic retinopathy, Microvasc Res. 2022 Jan; 139: 104265. |
| Klein AL et al., Phase 3 Trial of Interleukin-1 Trap rilonacept in Recurrent Pericarditis. N Engl J Med. 2021 Jan 7; 384(1): 31-41. |
| Krause K et al., Efficacy and safety of canakinumab in Schnitzler syndrome: A multicenter randomized placebo-controlled study. J Allergy Clin Immunol. 2017 Apr; 139(4): 1311-1320. |
| Krishnan S M et al., Pharmacological inhibition of the NLRP3 inflammasome reduces blood pressure, renal damage, and dysfunction in salt-sensitive hypertension. Cardiovasc. Res. (2019) 1154: 776-787. |
| Li W et al., Inhibition of the NLRP3 inflammasome with MCC950 prevents chronic social isolation-induced depression-like behavior in male mice. Neurosci Lett. 2021 Nov 20; 765: 136290. |
| Lin C et al., Omega-3 fatty acids regulate NLRP3 inflammasome activation and prevent behavior deficits after traumatic brain injury. Exp Neurol. 2017 Apr; 290: 115-122. |
| Liu HD et al., Expression of the NLRP3 inflammasome in cerebral cortex after traumatic brain injury in a rat model. Neurochem Res. 2013 Oct; 38(10): 2072-83. |
| Lu A et al., Hyperactivation of the NLRP3 Inflammasome in Myeloid Cells Leads to Severe Organ Damage in Experimental Lupus. J Immunol. 2017 Feb 1; 198(3): 1119-1129. |
| M Carlstrom et al., Genetic support for the role of the NLRP3 inflammasome in psoriasis susceptibility. Exp Dermatol. (2012) 21: 932-7. |
| Mao L et al., Loss-of-function CARD8 mutation causes NLRP3 inflammasome activation and Crohn's disease. J Clin Invest 2018: vol 128: 1793-1806. |
| Marchetti C et al., NLRP3 inflammasome inhibitor OLT1177 suppresses joint inflammation in murine models of acute arthritis. Arthritis Res Ther. 2018 Aug 3; 20(1): 169. |
| Martinon F et al., Gout-associated uric acid crystals activate the NALP3 inflammasome. Nature. 2006 Mar 9; 440(7081): 237-41. |
| Mathews RJ et al., Evidence of NLRP3-inflammasome activation in rheumatoid arthritis(RA); genetic variants within the NLRP3-inflammasome complex in relation to susceptibility to RA and response to anti-TNF treatment. Ann Rheum Dis. 2014 Jun; 73(6): 1202-10. |
| Meissner F et al., A. Mutant superoxide dismutase 1-induced IL-1beta accelerates ALS pathogenesis. Proc Natl Acad Sci U S A. 2010 Jul 20; 107(29): 13046-50. |
| Niu L et al., Upregulation of NLRP3 Inflammasome in the Tears and Ocular Surface of Dry Eye Patients. PLoS One. 2015 May 11; 10(5): e0126277. |
| Paldino E et al., Pyroptotic cell death in the R6/2 mouse model of Huntington's disease: new insight on the inflammasome. Cell Death Discov. 2020 Jul 31; 6: 69. |
| Paramel V G et al., NLRP3 Inflammasome Expression and Activation in Human Atherosclerosis. J Am Heart Assoc. 2016 May 20; 5(5): e003031. |
| Politis, M et al., Increased PK11195 PET binding in the cortex of patients with MS correlates with disability. Neurology, 2012, Vol 79(6), p523-30. |
| Ranson N et al., NLRP3-dependent and -independent processing Interleiukin-1β in active Ulcerative colitis. Int J mol Sci 2018: 20pii: E57. |
| Ridker P. M. et al., Antiinflammatory Therapy with canakinumab for Atherosclerotic Disease. Lancet(2017) 3901833-42. |
| Rodrigues FB et al., Cerebrospinal Fluid Inflammatory Biomarkers Reflect Clinical Severity in Huntington's Disease. PLoS One. 2016 Sep 22; 11(9): e0163479. |
| Ruperto N et al., Two randomized trials of canakinumab in systemic juvenile idiopathic arthritis. N Engl J Med. 2012 Dec 20; 367(25): 2396-406. |
| Sandanger O et al., The NLRP3 inflammasome is up-regulated in cardiac fibroblasts and mediates myocardial ischaemia-reperfusion injury. Cardiovasc Res. 2013 Jul 1; 99(1): 164-74. |
| Saresella M et al., Multiple inflammasome complexes are activated in autistic spectrum disorders. Brain Behav Immun. 2016 Oct; 57: 125-133. |
| Sarrauste M C et al., INFEVERS: the Registry for FMF and hereditary inflammatory disorders mutations. Nucleic Acids Res. 2003 Jan 1; 31(1): 282-5. |
| Shahzad K et al., Nlrp3-inflammasome activation in non-myeloid-derived cells aggravates diabetic nephropathy. Kidney Int. 2015 Jan; 87(1): 74-84. |
| Sheng Li et al., Protective effects of sulforaphane on diabetic retinopathy: activation of the Nrf2pathway and inhibition of NLRP3 inflammasome formation. Exp Anim. 2019 May 8; 68(2): 221-231. |
| So AK et al., Inflammation in gout: mechanisms and therapeutic targets. Nat Rev Rheumatol. 2017 Nov; 13(11): 639-647. |
| Sun X et al., The NLRP3-related inflammasome modulates pain behavior in a rat model of trigeminal neuropathic pain. Life Sci. 2021 Jul 15; 277: 119489. |
| Szabo D et al., Maternal P2X7 receptor inhibition prevents autism-like phenotype in male mouse offspring through the NLRP3-IL-1β pathway. Brain Behav Immun. 2022 Mar; 101: 318-332. |
| Tucci M et al., Glomerular accumulation of plasmacytoid dendritic cells in active lupus nephritis: role of interleukin-18. Arthritis Rheum. 2008 Jan; 58(1): 251-62. |
| Voet, S et al., A20 critically controls microglia activation and inhibits inflammasome-dependent neuroinflammation. Nat Commun., 2018, Vol 9(1), p2036. |
| Wallisch JS et al., Cerebrospinal Fluid NLRP3 is Increased After Severe Traumatic Brain Injury in Infants and Children. Neurocrit Care. 2017 Aug; 27(1): 44-50. |
| Wang Q et al., Renin-Dependent Hypertension in Mice Requires the NLRP3-Inflammasome. J. Hypertens(2014) 3: 187. |
| Watanabe H et al., Activation of the IL-1beta-processing inflammasome is involved in contact hypersensitivity. J Invest Dermatol. 2007 Aug; 127(8): 1956-63. |
| Wree A et al., NLRP3 inflammasome activation is required for fibrosis development in NAFLD. J Mol Med(Berl). 2014 Oct; 92(10): 1069-82. |
| Wu C et al., The Role of NLRP3 and IL-1β in Refractory Epilepsy Brain Injury. Front Neurol. 2020 Feb 7; 10: 1418. |
| Xu L et al., MiR-34c Ameliorates Neuropathic Pain by Targeting NLRP3 in a Mouse Model of Chronic Constriction Injury. Neuroscience. 2019 Feb 10; 399: 125-134. |
| Yang CA et al., Sex-dependent differential activation of NLRP3 and AIM2 inflammasomes in SLE macrophages. Rheumatology(Oxford). 2015 Feb; 54(2): 324-31. |
| Yue J et al., NLRP3 inflammasome and endoplasmic reticulum stress in the epileptogenic zone in temporal lobe epilepsy: molecular insights into their interdependence. Neuropathol Appl Neurobiol. 2020 Dec; 46(7): 770-785. |
| Zeng J et al., Specific inhibition of the NLRP3 inflammasome suppresses immune overactivation and alleviates COVID-19 like pathology in mice. EBioMedicine. 2022 Jan; 75: 103803. |
| Zhang Y et al., Involvement of inflammasome activation in lipopolysaccharide-induced mice depressive-like behaviors. CNS Neurosci Ther. 2014 Feb; 20(2): 119-24. |
| Zhang Y et al., NLRP3 Inflammasome Plays an Important Role in the Pathogenesis of Collagen-Induced Arthritis. Mediators Inflamm. 2016; 2016: 9656270. |
| Zhang Y et al., Protection of Mcc950 against high-glucose-induced human retinal endothelial cell dysfunction. Cell Death Dis. 2017 Jul 20; 8(7): e2941. |
| Zheng Q et al., Reactive oxygen species activated NLRP3 inflammasomes initiate inflammation in hyperosmolarity stressed human corneal epithelial cells and environment-induced dry eye patients. Exp Eye Res. 2015 May; 134: 133-40. |
Also Published As
| Publication number | Publication date |
|---|---|
| JP7737490B2 (ja) | 2025-09-10 |
| EP4671247A1 (en) | 2025-12-31 |
| JP2025176085A (ja) | 2025-12-03 |
| AU2024226032A1 (en) | 2025-09-11 |
| WO2024177127A1 (ja) | 2024-08-29 |
| CL2025002505A1 (es) | 2025-11-14 |
| PE20252572A1 (es) | 2025-10-28 |
| JP2024120882A (ja) | 2024-09-05 |
| AR131919A1 (es) | 2025-05-14 |
| MX2025009965A (es) | 2025-09-02 |
| TW202448887A (zh) | 2024-12-16 |
| CN120752239A (zh) | 2025-10-03 |
| IL322520A (en) | 2025-10-01 |
| CO2025011311A2 (es) | 2025-09-08 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP7483810B2 (ja) | 6-アミノピラゾロピリミジン化合物及びその医薬用途 | |
| JP7585409B2 (ja) | ピラゾロピリミジン化合物及びその医薬用途 | |
| JP7741100B2 (ja) | ミエロイド細胞に発現するトリガー受容体2アゴニストとしての複素環化合物及び使用方法 | |
| TW201819380A (zh) | 作為抗病毒劑之稠合四環吡啶酮化合物 | |
| WO2023086800A1 (en) | Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use | |
| JP7737490B2 (ja) | 置換ピラゾロピリミジン化合物及びその医薬用途 | |
| JP7729000B2 (ja) | 6-アルコキシピラゾロピリミジン化合物及びその医薬用途 | |
| WO2022166741A1 (zh) | 含有苯并杂环的作为egfr激酶抑制剂的大环化合物、其药物组合物和用途 | |
| WO2024233847A2 (en) | Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use | |
| KR20230143611A (ko) | 바이사이클릭 고리를 포함하는 tyk2 억제제 화합물 | |
| JP2017095411A (ja) | ピラゾール誘導体の塩の結晶 | |
| HK40128856A (en) | Pyrazolopyrimidine compound and pharmaceutical use thereof | |
| CN117881682A (zh) | 6-氨基吡唑并嘧啶化合物及其医药用途 | |
| HK40112889A (en) | 6-aminopyrazolopyrimidine compound and pharmaceutical use thereof | |
| WO2024207945A1 (zh) | 作为aak1抑制剂的氮杂环类化合物 | |
| WO2017090716A1 (ja) | ピラゾール誘導体の結晶 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0105 | International application |
St.27 status event code: A-0-1-A10-A15-nap-PA0105 |
|
| PG1501 | Laying open of application |
St.27 status event code: A-1-1-Q10-Q12-nap-PG1501 |
|
| Q12 | Application published |
Free format text: ST27 STATUS EVENT CODE: A-1-1-Q10-Q12-NAP-PG1501 (AS PROVIDED BY THE NATIONAL OFFICE) |
|
| PN2301 | Change of applicant |
St.27 status event code: A-3-3-R10-R11-asn-PN2301 |
|
| R11 | Change to the name of applicant or owner or transfer of ownership requested |
Free format text: ST27 STATUS EVENT CODE: A-3-3-R10-R11-ASN-PN2301 (AS PROVIDED BY THE NATIONAL OFFICE) |