HRP20050004A2 - New compounds, compositions and methods for treatment of inflammatory diseases and conditions - Google Patents
New compounds, compositions and methods for treatment of inflammatory diseases and conditionsInfo
- Publication number
- HRP20050004A2 HRP20050004A2 HR20050004A HRP20050004A HRP20050004A2 HR P20050004 A2 HRP20050004 A2 HR P20050004A2 HR 20050004 A HR20050004 A HR 20050004A HR P20050004 A HRP20050004 A HR P20050004A HR P20050004 A2 HRP20050004 A2 HR P20050004A2
- Authority
- HR
- Croatia
- Prior art keywords
- inflammatory
- steroid
- conditions
- methods
- inflammatory diseases
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 208000027866 inflammatory disease Diseases 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 title 1
- 150000003431 steroids Chemical class 0.000 abstract 4
- 230000003110 anti-inflammatory effect Effects 0.000 abstract 3
- 239000003120 macrolide antibiotic agent Substances 0.000 abstract 3
- MZOFCQQQCNRIBI-VMXHOPILSA-N (3s)-4-[[(2s)-1-[[(2s)-1-[[(1s)-1-carboxy-2-hydroxyethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-[[2-[[(2s)-2,6-diaminohexanoyl]amino]acetyl]amino]-4-oxobutanoic acid Chemical compound OC[C@@H](C(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@@H](N)CCCCN MZOFCQQQCNRIBI-VMXHOPILSA-N 0.000 abstract 1
- 108090000695 Cytokines Proteins 0.000 abstract 1
- 102000004127 Cytokines Human genes 0.000 abstract 1
- 102000003676 Glucocorticoid Receptors Human genes 0.000 abstract 1
- 108090000079 Glucocorticoid Receptors Proteins 0.000 abstract 1
- 102100039620 Granulocyte-macrophage colony-stimulating factor Human genes 0.000 abstract 1
- 101000746373 Homo sapiens Granulocyte-macrophage colony-stimulating factor Proteins 0.000 abstract 1
- 206010020751 Hypersensitivity Diseases 0.000 abstract 1
- -1 ICAM Proteins 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 108010002352 Interleukin-1 Proteins 0.000 abstract 1
- 241001465754 Metazoa Species 0.000 abstract 1
- 108060008682 Tumor Necrosis Factor Proteins 0.000 abstract 1
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 abstract 1
- 208000026935 allergic disease Diseases 0.000 abstract 1
- 230000007815 allergy Effects 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 230000028993 immune response Effects 0.000 abstract 1
- 210000004969 inflammatory cell Anatomy 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 229940041033 macrolides Drugs 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Ovaj izum se odnosi (a) na nove spojeve prikazaneFormulom I:gdje M predstavlja makrolidnu podjedinicu (makrolidni dio) izveden iz makrolida koji imasvojstvo nakupljanja u upalnim stanicama, S predstavlja steroidnu podjedinicu (steroidni dio) izvedenu iz steroidnog lijeka s protuupalnom aktivnošćui L predstavlja lanac koji povezuje M i S, (b) nanjihove farmaceutski prihvatljive soli, prolijekove i solvate, (c) na postupke i međuprodukte za njihovu pripravu i (d) na njihovu uporabu u tretiranju upalnih bolesti i stanja kod ljudi i životinja,Takvi spojevi inhibiraju mnoge citokine i medijatore upale uključene u imunološke odgovore koji uzrokuju upalu, alergiju ili aloimunoat, uključujući bez ograničenja IL-1, 2, 4, 5, 6, 10, 12, GMCSF, ICAM, i TNF-α. Važno, protuupalni steroidi pokazuju izravan protuupalni učinak preko vezanja na glukokortikoidni receptor.The present invention relates (a) to novel compounds represented by Formula I: where M represents a macrolide subunit (macrolide moiety) derived from macrolides having a buildup property in inflammatory cells, S represents a steroid subunit (steroid moiety) derived from a steroid drug with anti-inflammatory activity and L represents a chain which binds M and S, (b) their pharmaceutically acceptable salts, prodrugs and solvates, (c) the methods and intermediates for their preparation, and (d) their use in treating inflammatory diseases and conditions in humans and animals, Such compounds inhibit many cytokines and inflammatory mediators involved in immune responses that cause inflammation, allergy or alloimmunoate, including without limitation IL-1, 2, 4, 5, 6, 10, 12, GMCSF, ICAM, and TNF-α. Importantly, anti-inflammatory steroids exhibit a direct anti-inflammatory effect via binding to the glucocorticoid receptor.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| HR20050004A HRP20050004A2 (en) | 2002-07-08 | 2005-01-04 | New compounds, compositions and methods for treatment of inflammatory diseases and conditions |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US39467002P | 2002-07-08 | 2002-07-08 | |
| PCT/HR2003/000037 WO2004005310A2 (en) | 2002-07-08 | 2003-07-08 | New compounds, compositions and methods for treatment of inflammatory diseases and conditions |
| HR20050004A HRP20050004A2 (en) | 2002-07-08 | 2005-01-04 | New compounds, compositions and methods for treatment of inflammatory diseases and conditions |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20050004A2 true HRP20050004A2 (en) | 2007-02-28 |
Family
ID=37904039
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20050004A HRP20050004A2 (en) | 2002-07-08 | 2005-01-04 | New compounds, compositions and methods for treatment of inflammatory diseases and conditions |
Country Status (1)
| Country | Link |
|---|---|
| HR (1) | HRP20050004A2 (en) |
-
2005
- 2005-01-04 HR HR20050004A patent/HRP20050004A2/en not_active Application Discontinuation
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A1OB | Publication of a patent application | ||
| AIPI | Request for the grant of a patent on the basis of a substantive examination of a patent application | ||
| ODRP | Renewal fee for the maintenance of a patent |
Payment date: 20100630 Year of fee payment: 8 |
|
| OBST | Application withdrawn |