ES2427892T3 - Inhibidores de MAP quinasa p38 - Google Patents
Inhibidores de MAP quinasa p38 Download PDFInfo
- Publication number
- ES2427892T3 ES2427892T3 ES09713855T ES09713855T ES2427892T3 ES 2427892 T3 ES2427892 T3 ES 2427892T3 ES 09713855 T ES09713855 T ES 09713855T ES 09713855 T ES09713855 T ES 09713855T ES 2427892 T3 ES2427892 T3 ES 2427892T3
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- ES
- Spain
- Prior art keywords
- alkyl
- optionally substituted
- hydrogen
- radical
- amino
- 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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- 102000043136 MAP kinase family Human genes 0.000 title description 12
- 108091054455 MAP kinase family Proteins 0.000 title description 12
- 239000012826 P38 inhibitor Substances 0.000 title description 7
- 150000001875 compounds Chemical class 0.000 claims abstract description 94
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract description 73
- 239000001257 hydrogen Substances 0.000 claims abstract description 61
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims abstract description 47
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims abstract description 33
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract description 32
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract description 29
- 125000006413 ring segment Chemical group 0.000 claims abstract description 25
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims abstract description 20
- 230000003834 intracellular effect Effects 0.000 claims abstract description 18
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims abstract description 16
- 125000002950 monocyclic group Chemical group 0.000 claims abstract description 16
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract description 16
- 108090000371 Esterases Proteins 0.000 claims abstract description 13
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract description 13
- 229910052799 carbon Inorganic materials 0.000 claims abstract description 11
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims abstract description 10
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- 125000004185 ester group Chemical group 0.000 claims abstract description 9
- 125000002527 bicyclic carbocyclic group Chemical group 0.000 claims abstract description 6
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- 125000001424 substituent group Chemical group 0.000 claims description 20
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- 125000000217 alkyl group Chemical group 0.000 claims description 12
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- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 11
- 238000011282 treatment Methods 0.000 claims description 11
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 8
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 6
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- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 claims description 2
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- 239000004474 valine Substances 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/73—Unsubstituted amino or imino radicals
-
- 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
- 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
- A61P11/00—Drugs for disorders of the respiratory system
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- 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
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- 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
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- 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
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Transplantation (AREA)
- Emergency Medicine (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Obesity (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0803748 | 2008-02-29 | ||
| GB0803748A GB0803748D0 (en) | 2008-02-29 | 2008-02-29 | Ihibitors of p38 MAP kinase |
| GB0815544 | 2008-08-27 | ||
| GB0815544A GB0815544D0 (en) | 2008-08-27 | 2008-08-27 | Inhibitors of p38 map kinase |
| PCT/GB2009/000553 WO2009106844A1 (en) | 2008-02-29 | 2009-02-27 | Inhibitors of p38 map kinase |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2427892T3 true ES2427892T3 (es) | 2013-11-04 |
Family
ID=40585513
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES09713855T Active ES2427892T3 (es) | 2008-02-29 | 2009-02-27 | Inhibidores de MAP quinasa p38 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8778953B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2245012B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP5555186B2 (cg-RX-API-DMAC7.html) |
| ES (1) | ES2427892T3 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2009106844A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007129040A1 (en) * | 2006-05-04 | 2007-11-15 | Chroma Therapeutics Ltd. | p38 MAP KINASE INHIBITORS |
| GB0803747D0 (en) * | 2008-02-29 | 2008-04-09 | Martin | Enzyme and receptor modulation |
| GB0903480D0 (en) | 2009-02-27 | 2009-04-08 | Chroma Therapeutics Ltd | Enzyme Inhibitors |
| GB201211310D0 (en) | 2012-06-26 | 2012-08-08 | Chroma Therapeutics Ltd | CSF-1R kinase inhibitors |
| BR112015008167B1 (pt) | 2012-10-17 | 2020-11-17 | Macrophage Pharma Limited | composto, composição farmacêutica, métodos para a inibição da atividade de uma enzima quinase map p38, para o tratamento ou a prevenção de doença autoimune ou inflamatória em um indivíduo, e para o tratamento, a melhoria ou a redução da incidência de doença proliferativa de células em um indivíduo, uso de composto, e, ácido |
| GB201306901D0 (en) * | 2013-04-16 | 2013-05-29 | Chroma Therapeutics Ltd | Combination |
| CN116570594A (zh) | 2016-06-23 | 2023-08-11 | 马里兰大学巴尔的摩分校 | 选择性p38α特异性MAPK抑制剂 |
| GB201713975D0 (en) | 2017-08-31 | 2017-10-18 | Macrophage Pharma Ltd | Medical use |
| CN113395963B (zh) | 2018-12-07 | 2024-06-25 | 马里兰大学巴尔的摩分校 | 非ATP/催化位点p38丝裂原活化蛋白激酶抑制剂 |
| US11286260B2 (en) * | 2020-05-18 | 2022-03-29 | Gen1E Lifesciences Inc. | P38α mitogen-activated protein kinase inhibitors |
| CN116367838A (zh) | 2020-10-29 | 2023-06-30 | Gen1E生命科学公司 | 结晶5-(二甲基氨基)-n-(4-(吗啉代甲基)苯基)萘-1-磺酰胺二盐酸盐二水合物 |
| US11555020B2 (en) | 2021-03-23 | 2023-01-17 | Gen1E Lifesciences Inc. | Substituted naphthyl p38α mitogen-activated protein kinase inhibitors |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5331006A (en) * | 1990-08-31 | 1994-07-19 | Warner-Lambert Company | Amino acid analogs as CCK antagonists |
| AU650953B2 (en) | 1991-03-21 | 1994-07-07 | Novartis Ag | Inhaler |
| US6448256B1 (en) * | 1999-05-24 | 2002-09-10 | University Of Massachusetts | Antibiotic prodrugs |
| BR0308429A (pt) * | 2002-03-14 | 2005-01-11 | Bayer Healthcare Ag | Aroilpiridinonas monocìclicas como agentes antiinflamatórios |
| EP1633751A1 (en) | 2003-06-16 | 2006-03-15 | Chroma Therapeutics Limited | Carboline and betacarboline derivatives for use as hdac enzyme inhibitors |
| SG145693A1 (en) | 2003-07-29 | 2008-09-29 | Signature R & D Holdings Llc | Amino acid prodrugs |
| EP3075247B1 (en) | 2004-02-02 | 2022-10-12 | BioSight Ltd. | Conjugates for cancer therapy and diagnosis |
| DE602005003951T4 (de) * | 2004-05-14 | 2012-10-11 | Millennium Pharmaceuticals, Inc. | Verbindungen und verfahren zur inhibierung der mitotischen progression durch hemmung von aurorakinase |
| PL1877098T3 (pl) * | 2005-05-05 | 2013-09-30 | Glaxosmithkline Ip Dev Ltd | Koniugaty estru alfa-aminokwasu z lekiem ulegające hydrolizie z udziałem karboksyloesterazy |
| WO2007129040A1 (en) * | 2006-05-04 | 2007-11-15 | Chroma Therapeutics Ltd. | p38 MAP KINASE INHIBITORS |
| GB0621830D0 (en) | 2006-11-02 | 2006-12-13 | Chroma Therapeutics Ltd | Inhibitors of p38 mitogen-activated protein kinase |
| JP2011503042A (ja) | 2007-11-07 | 2011-01-27 | クロマ セラピューティクス リミテッド | ｐ３８ＭＡＰキナーゼ阻害剤 |
-
2009
- 2009-02-27 EP EP09713855.6A patent/EP2245012B1/en not_active Not-in-force
- 2009-02-27 US US12/867,774 patent/US8778953B2/en active Active
- 2009-02-27 WO PCT/GB2009/000553 patent/WO2009106844A1/en not_active Ceased
- 2009-02-27 JP JP2010548176A patent/JP5555186B2/ja not_active Expired - Fee Related
- 2009-02-27 ES ES09713855T patent/ES2427892T3/es active Active
Also Published As
| Publication number | Publication date |
|---|---|
| EP2245012A1 (en) | 2010-11-03 |
| JP2011513288A (ja) | 2011-04-28 |
| EP2245012B1 (en) | 2013-07-03 |
| US8778953B2 (en) | 2014-07-15 |
| JP5555186B2 (ja) | 2014-07-23 |
| US20110034520A1 (en) | 2011-02-10 |
| WO2009106844A1 (en) | 2009-09-03 |
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