ES2532764T3 - Inhibidores de pirazol p38 MAP quinasa - Google Patents
Inhibidores de pirazol p38 MAP quinasa Download PDFInfo
- Publication number
- ES2532764T3 ES2532764T3 ES11713510.3T ES11713510T ES2532764T3 ES 2532764 T3 ES2532764 T3 ES 2532764T3 ES 11713510 T ES11713510 T ES 11713510T ES 2532764 T3 ES2532764 T3 ES 2532764T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- chain
- optionally substituted
- amino
- saturated
- 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.)
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- 102000002574 p38 Mitogen-Activated Protein Kinases Human genes 0.000 title description 25
- 108010068338 p38 Mitogen-Activated Protein Kinases Proteins 0.000 title description 25
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 title description 7
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 title description 3
- 150000001875 compounds Chemical class 0.000 abstract description 7
- 229910052717 sulfur Inorganic materials 0.000 abstract 7
- 125000005843 halogen group Chemical group 0.000 abstract 6
- 125000005842 heteroatom Chemical group 0.000 abstract 6
- 229910052760 oxygen Inorganic materials 0.000 abstract 6
- 229920006395 saturated elastomer Polymers 0.000 abstract 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- 125000000623 heterocyclic group Chemical group 0.000 abstract 5
- 229910052757 nitrogen Inorganic materials 0.000 abstract 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000004043 oxo group Chemical group O=* 0.000 abstract 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 abstract 2
- 125000004442 acylamino group Chemical group 0.000 abstract 2
- 125000002947 alkylene group Chemical group 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000001188 haloalkyl group Chemical group 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 abstract 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 abstract 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- -1 amino amino Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000004404 heteroalkyl group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 230000000155 isotopic effect Effects 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 239000011593 sulfur Substances 0.000 abstract 1
- 102000001708 Protein Isoforms Human genes 0.000 description 10
- 108010029485 Protein Isoforms Proteins 0.000 description 10
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 description 6
- 102000043136 MAP kinase family Human genes 0.000 description 4
- 108091054455 MAP kinase family Proteins 0.000 description 4
- 210000004027 cell Anatomy 0.000 description 4
- 239000003112 inhibitor Substances 0.000 description 4
- MVCOAUNKQVWQHZ-UHFFFAOYSA-N doramapimod Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)NC=2C3=CC=CC=C3C(OCCN3CCOCC3)=CC=2)=CC(C(C)(C)C)=N1 MVCOAUNKQVWQHZ-UHFFFAOYSA-N 0.000 description 3
- 230000002401 inhibitory effect Effects 0.000 description 3
- 230000026731 phosphorylation Effects 0.000 description 3
- 238000006366 phosphorylation reaction Methods 0.000 description 3
- 210000001519 tissue Anatomy 0.000 description 3
- 108090000695 Cytokines Proteins 0.000 description 2
- 102000004127 Cytokines Human genes 0.000 description 2
- 206010061218 Inflammation Diseases 0.000 description 2
- 206010028980 Neoplasm Diseases 0.000 description 2
- 230000003110 anti-inflammatory effect Effects 0.000 description 2
- 239000003246 corticosteroid Substances 0.000 description 2
- 208000027866 inflammatory disease Diseases 0.000 description 2
- 230000004054 inflammatory process Effects 0.000 description 2
- 210000004072 lung Anatomy 0.000 description 2
- 210000002540 macrophage Anatomy 0.000 description 2
- 230000000770 proinflammatory effect Effects 0.000 description 2
- 238000011144 upstream manufacturing Methods 0.000 description 2
- IQFIWJDBZRZLNO-UHFFFAOYSA-N 1h-pyrazole;urea Chemical class NC(N)=O.C=1C=NNC=1 IQFIWJDBZRZLNO-UHFFFAOYSA-N 0.000 description 1
- JBNWDYGOTHQHOZ-UHFFFAOYSA-N 2-[5-[4-[(4-fluorophenyl)methyl]piperidine-1-carbonyl]-6-methoxy-1-methylindol-3-yl]-n,n-dimethyl-2-oxoacetamide Chemical compound COC1=CC=2N(C)C=C(C(=O)C(=O)N(C)C)C=2C=C1C(=O)N(CC1)CCC1CC1=CC=C(F)C=C1 JBNWDYGOTHQHOZ-UHFFFAOYSA-N 0.000 description 1
- RQVKVJIRFKVPBF-VWLOTQADSA-N 2-[[(2s)-2-amino-3-phenylpropyl]amino]-3-methyl-5-naphthalen-2-yl-6-pyridin-4-ylpyrimidin-4-one Chemical compound C([C@H](N)CNC=1N(C(C(C=2C=C3C=CC=CC3=CC=2)=C(C=2C=CN=CC=2)N=1)=O)C)C1=CC=CC=C1 RQVKVJIRFKVPBF-VWLOTQADSA-N 0.000 description 1
- FYSRKRZDBHOFAY-UHFFFAOYSA-N 6-(N-carbamoyl-2,6-difluoroanilino)-2-(2,4-difluorophenyl)-3-pyridinecarboxamide Chemical compound FC=1C=CC=C(F)C=1N(C(=O)N)C(N=1)=CC=C(C(N)=O)C=1C1=CC=C(F)C=C1F FYSRKRZDBHOFAY-UHFFFAOYSA-N 0.000 description 1
- 102100023274 Dual specificity mitogen-activated protein kinase kinase 4 Human genes 0.000 description 1
- 102100023401 Dual specificity mitogen-activated protein kinase kinase 6 Human genes 0.000 description 1
- 102000003676 Glucocorticoid Receptors Human genes 0.000 description 1
- 108090000079 Glucocorticoid Receptors Proteins 0.000 description 1
- 101001115395 Homo sapiens Dual specificity mitogen-activated protein kinase kinase 4 Proteins 0.000 description 1
- 101000624426 Homo sapiens Dual specificity mitogen-activated protein kinase kinase 6 Proteins 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- 108090001007 Interleukin-8 Proteins 0.000 description 1
- 241000824268 Kuma Species 0.000 description 1
- 239000012826 P38 inhibitor Substances 0.000 description 1
- 108091000080 Phosphotransferase Proteins 0.000 description 1
- 210000001744 T-lymphocyte Anatomy 0.000 description 1
- 108060008682 Tumor Necrosis Factor Proteins 0.000 description 1
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 239000012190 activator Substances 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 208000037976 chronic inflammation Diseases 0.000 description 1
- 230000006020 chronic inflammation Effects 0.000 description 1
- 229960001334 corticosteroids Drugs 0.000 description 1
- 230000008878 coupling Effects 0.000 description 1
- 238000010168 coupling process Methods 0.000 description 1
- 238000005859 coupling reaction Methods 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 230000009266 disease activity Effects 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 210000002889 endothelial cell Anatomy 0.000 description 1
- 210000002216 heart Anatomy 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 229940125369 inhaled corticosteroids Drugs 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 210000004698 lymphocyte Anatomy 0.000 description 1
- 238000012423 maintenance Methods 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 210000000440 neutrophil Anatomy 0.000 description 1
- 210000000496 pancreas Anatomy 0.000 description 1
- 210000003819 peripheral blood mononuclear cell Anatomy 0.000 description 1
- 230000002085 persistent effect Effects 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 102000020233 phosphotransferase Human genes 0.000 description 1
- 230000007115 recruitment Effects 0.000 description 1
- 230000019491 signal transduction Effects 0.000 description 1
- 210000002027 skeletal muscle Anatomy 0.000 description 1
- 210000000813 small intestine Anatomy 0.000 description 1
- ZMELOYOKMZBMRB-DLBZAZTESA-N talmapimod Chemical compound C([C@@H](C)N(C[C@@H]1C)C(=O)C=2C(=CC=3N(C)C=C(C=3C=2)C(=O)C(=O)N(C)C)Cl)N1CC1=CC=C(F)C=C1 ZMELOYOKMZBMRB-DLBZAZTESA-N 0.000 description 1
- 210000001550 testis Anatomy 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 description 1
- 239000005483 tyrosine kinase inhibitor Substances 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- 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
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- A61P37/08—Antiallergic agents
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Diabetes (AREA)
- Ophthalmology & Optometry (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Otolaryngology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB201005589 | 2010-04-01 | ||
| GBGB1005589.5A GB201005589D0 (en) | 2010-04-01 | 2010-04-01 | Novel compounds |
| PCT/GB2011/050668 WO2011121366A1 (en) | 2010-04-01 | 2011-04-01 | Pyrazole p38 map kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2532764T3 true ES2532764T3 (es) | 2015-03-31 |
Family
ID=42228808
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES11713510.3T Active ES2532764T3 (es) | 2010-04-01 | 2011-04-01 | Inhibidores de pirazol p38 MAP quinasa |
Country Status (6)
| Country | Link |
|---|---|
| US (3) | US20130029990A1 (enExample) |
| EP (1) | EP2556065B1 (enExample) |
| JP (1) | JP5902668B2 (enExample) |
| ES (1) | ES2532764T3 (enExample) |
| GB (1) | GB201005589D0 (enExample) |
| WO (1) | WO2011121366A1 (enExample) |
Families Citing this family (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA019974B1 (ru) | 2007-12-19 | 2014-07-30 | Кансер Рисерч Текнолоджи Лимитед | 8-ЗАМЕЩЕННЫЕ ПИРИДО[2,3-b]ПИРАЗИНЫ И ИХ ПРИМЕНЕНИЕ |
| GB0905955D0 (en) * | 2009-04-06 | 2009-05-20 | Respivert Ltd | Novel compounds |
| CN102906090B (zh) | 2010-02-01 | 2015-06-24 | 癌症研究技术有限公司 | 1-(5-叔丁基-2-苯基-2h-吡唑-3-基)-3-[2-氟-4-(1-甲基-2-氧代-2,3-二氢-1h-咪唑并[4,5-b]吡啶-7-基氧基)-苯基]-脲和相关化合物及它们在治疗中的应用 |
| GB201005589D0 (en) | 2010-04-01 | 2010-05-19 | Respivert Ltd | Novel compounds |
| JP5787977B2 (ja) | 2010-04-08 | 2015-09-30 | レスピバート・リミテツド | Ｐ３８ｍａｐキナーゼ阻害剤 |
| US9260410B2 (en) | 2010-04-08 | 2016-02-16 | Respivert Ltd. | P38 MAP kinase inhibitors |
| GB201009731D0 (en) * | 2010-06-10 | 2010-07-21 | Pulmagen Therapeutics Inflamma | Kinase inhibitors |
| EP2582700B1 (en) | 2010-06-17 | 2016-11-02 | Respivert Limited | Respiratory formulations containing p38 mapk inhibitors |
| GB201010193D0 (en) | 2010-06-17 | 2010-07-21 | Respivert Ltd | Medicinal use |
| EP2578582A1 (en) | 2011-10-03 | 2013-04-10 | Respivert Limited | 1-Pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl)ureas as p38 MAP kinase inhibitors |
| PT2763984T (pt) | 2011-10-03 | 2016-07-25 | Respivert Ltd | 1-pirazolil-3-(4-((2-anilinopirimidin-4-il)oxi)naftalen-1-il) ureias como inibidores da map cinase p38 |
| CN103974953B (zh) * | 2011-12-09 | 2016-06-29 | 奇斯药制品公司 | 激酶抑制剂 |
| CN105968110B (zh) * | 2011-12-09 | 2018-04-27 | 奇斯药制品公司 | 激酶抑制剂 |
| CA2879431A1 (en) | 2012-07-17 | 2014-01-23 | Washington University | Anti-mucus drugs and uses therefor |
| GB201214750D0 (en) | 2012-08-17 | 2012-10-03 | Respivert Ltd | Compounds |
| US20150210722A1 (en) | 2012-08-29 | 2015-07-30 | Respivert Limited | Kinase inhibitors |
| GB201215357D0 (en) | 2012-08-29 | 2012-10-10 | Respivert Ltd | Compounds |
| WO2014033449A1 (en) * | 2012-08-29 | 2014-03-06 | Respivert Limited | Kinase inhibitors |
| WO2014033447A2 (en) | 2012-08-29 | 2014-03-06 | Respivert Limited | Kinase inhibitors |
| US9732063B2 (en) | 2012-11-16 | 2017-08-15 | Respivert Limited | Kinase inhibitors |
| US20160016934A1 (en) | 2013-03-14 | 2016-01-21 | Respivert Limited | Kinase inhibitors |
| EP2981534B1 (en) | 2013-04-02 | 2017-07-19 | Topivert Pharma Limited | Kinase inhibitors based upon n-alkyl pyrazoles |
| KR102283883B1 (ko) | 2013-04-02 | 2021-07-29 | 옥슬러 액퀴지션즈 리미티드 | 키나제 저해제 |
| US9908845B2 (en) | 2013-09-09 | 2018-03-06 | Peloton Therapeutics, Inc. | Aryl ethers and uses thereof |
| GB201320729D0 (en) | 2013-11-25 | 2014-01-08 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| GB201320732D0 (en) | 2013-11-25 | 2014-01-08 | Cancer Rec Tech Ltd | Methods of chemical synthesis |
| CA2934199A1 (en) | 2013-12-20 | 2015-06-25 | Respivert Limited | Urea derivatives useful as kinase inhibitors |
| US9447076B2 (en) | 2014-02-14 | 2016-09-20 | Respivert Ltd. | Inhibitor of p38 map kinase |
| MA40775A (fr) | 2014-10-01 | 2017-08-08 | Respivert Ltd | Dérivé d'acide 4-(4-(4-phényluréido-naphtalén -1-yl) oxy-pyridin-2-yl) amino-benzoïque utilisé en tant qu'inhibiteur de la kinase p38 |
| US10278942B2 (en) | 2015-03-11 | 2019-05-07 | Peloton Therapeutics, Inc. | Compositions for use in treating pulmonary arterial hypertension |
| US10512626B2 (en) | 2015-03-11 | 2019-12-24 | Peloton Therapeautics, Inc. | Compositions for use in treating glioblastoma |
| WO2016144825A1 (en) | 2015-03-11 | 2016-09-15 | Peloton Therapeutics, Inc. | Aromatic compounds and uses thereof |
| US10155726B2 (en) | 2015-03-11 | 2018-12-18 | Peloton Therapeutics, Inc. | Substituted pyridines and uses thereof |
| US10335388B2 (en) | 2015-04-17 | 2019-07-02 | Peloton Therapeutics, Inc. | Combination therapy of a HIF-2-alpha inhibitor and an immunotherapeutic agent and uses thereof |
| JP6994458B2 (ja) * | 2015-10-01 | 2022-02-04 | モンサント テクノロジー エルエルシー | ハロニトロ芳香族の接触水素化のためのプロセス |
| CA3015978A1 (en) | 2016-04-06 | 2017-10-12 | Topivert Pharma Limited | Kinase inhibitors |
| CA3142097A1 (en) | 2018-05-30 | 2019-12-05 | Washington University | Mitogen-activated protein kinase inhibitors, methods of making, and methods of use thereof |
| EP3858814A4 (en) * | 2018-09-29 | 2022-10-05 | Jiangsu Yahong Meditech Co., Ltd. | NITROXOLINE PRODRUG AND ITS USE |
| EP3886854A4 (en) | 2018-11-30 | 2022-07-06 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| CA3140017A1 (en) | 2019-07-19 | 2021-01-28 | Aurore HICK | Polyaromatic urea derivatives and their use in the treatment of muscle diseases |
| EP4029501A1 (en) | 2021-01-19 | 2022-07-20 | Anagenesis Biotechnologies | Combination of polyaromatic urea derivatives and glucocorticoid or hdac inhibitor for the treatment of diseases or conditions associated with muscle cells and/or satellite cells |
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| US20080300281A1 (en) * | 1997-12-22 | 2008-12-04 | Jacques Dumas | Inhibition of p38 Kinase Activity Using Aryl and Heteroaryl Substituted Heterocyclic Ureas |
| UA73492C2 (en) | 1999-01-19 | 2005-08-15 | Aromatic heterocyclic compounds as antiinflammatory agents | |
| EP1751139B1 (en) | 2004-04-30 | 2011-07-27 | Bayer HealthCare LLC | Substituted pyrazolyl urea derivatives useful in the treatment of cancer |
| WO2006018718A2 (en) | 2004-08-12 | 2006-02-23 | Pfizer Limited | Triazolopyridinylsulfanyl derivatives as p38 map kinase inhibitors |
| GB0500435D0 (en) | 2005-01-10 | 2005-02-16 | Novartis Ag | Organic compounds |
| DE102005015253A1 (de) * | 2005-04-04 | 2006-10-05 | Merck Patent Gmbh | Pyrazolderivate |
| DE102005037499A1 (de) * | 2005-08-09 | 2007-02-15 | Merck Patent Gmbh | Pyrazolderivate |
| MX2008006979A (es) * | 2005-12-01 | 2009-01-14 | Bayer Healthcare Llc | Compuestos de urea utiles en el tratamiento contra el cancer. |
| CN101437512A (zh) | 2006-01-27 | 2009-05-20 | 阿雷生物药品公司 | 葡萄糖激酶活化剂 |
| EP1979355B1 (en) | 2006-01-30 | 2010-08-18 | Irm Llc | Spiro imidazole derivatives as ppar modulators |
| US20070194939A1 (en) | 2006-02-21 | 2007-08-23 | Alvarez Frank D | Healthcare facilities operation |
| GB0818033D0 (en) * | 2008-10-02 | 2008-11-05 | Respivert Ltd | Novel compound |
| BRPI0920707A2 (pt) * | 2008-10-02 | 2015-12-29 | Respivert Ltd | compostos |
| US8299074B2 (en) * | 2008-12-11 | 2012-10-30 | Respivert Ltd. | P38 MAP kinase inhibitors |
| GB0905955D0 (en) * | 2009-04-06 | 2009-05-20 | Respivert Ltd | Novel compounds |
| GB201005589D0 (en) | 2010-04-01 | 2010-05-19 | Respivert Ltd | Novel compounds |
| US9260410B2 (en) | 2010-04-08 | 2016-02-16 | Respivert Ltd. | P38 MAP kinase inhibitors |
| JP5787977B2 (ja) | 2010-04-08 | 2015-09-30 | レスピバート・リミテツド | Ｐ３８ｍａｐキナーゼ阻害剤 |
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| EP2556065B1 (en) | 2014-12-17 |
| GB201005589D0 (en) | 2010-05-19 |
| EP2556065A1 (en) | 2013-02-13 |
| US20170362208A1 (en) | 2017-12-21 |
| JP5902668B2 (ja) | 2016-04-13 |
| WO2011121366A1 (en) | 2011-10-06 |
| US20160130256A1 (en) | 2016-05-12 |
| US9771354B2 (en) | 2017-09-26 |
| JP2013523710A (ja) | 2013-06-17 |
| US20130029990A1 (en) | 2013-01-31 |
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