Patent ID: 6340706
Filing Date: 2002-01-22
Classification: A61P,C07C

Abstract:
A leukotriene-B4 derivative of formula I whereinR1 is CH2OH, CH3, CF3, COOR4, or CONR5R6, R2 is H or an organic acid radical with 1-15 C atoms, R3 is H; C1-C4 alkyl optionally substituted by halogen atoms or phenyl; C3-C10 cycloalkyl optionally substituted in one or more places by C1-4 alkyl or halogen atoms; C6-C10 aryl optionally substituted in one or more places by halogen, phenyl, C1-C4 alkyl, C1-C4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carbonyl, carboxyl or hydroxy; or a 5- to 6-membered aromatic heterocyclic ring with at least 1 heteroatom, R4 is hydrogen; C1-C10 alkyl, C3-C10 cycloalkyl, or C6-C10 aryl in each case optionally substituted by 1-3 halogen, phenyl, C1-C4 alkyl, C1-C4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxyl or hydroxy; CH2â€”COâ€”(C6-C10) aryl; or a 5- to 6-membered ring with at least 1 heteroatom, A is trans, trans-CH&boxH;CHâ€”CH&boxH;CH, â€”CH2CH2â€”CH&boxH;CHâ€” or tetramethylene, B is C1-C10 straight-chain or branched-chain alkylene, which is optionally substituted by fluorine, or is D is a direct bond, oxygen, sulfur, â€”Câ‰¡Câ€”, â€”CH&boxH;CR7 or together with B can also be a direct bond; R5 and R6 are the same or different, and are each H or C1-C4 alkyl optionally substituted by hydroxy groups, or R6 is H and R5 is C1-C15 alkanoyl or R8SO2, R7 is H, C1-C5 alkyl, chlorine, or bromine, R8 is H; C1-C14 alkyl optionally substituted by halogen atoms or phenyl; C3-C10 cycloalkyl optionally substituted in one or more places by C1-4 alkyl or halogen atoms; C6-C10 aryl optionally substituted in one or more places by halogen, phenyl, C1-C4 alkyl, C1-C4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carbonyl, carboxyl or hydroxy; or a 5- to 6-membered aromatic heterocyclic ring with at least 1 heteroatom, m is 1-3, n is 2-5, o is 0-5, p is 0-5, X is a direct bond, oxygen, or sulfur, and Y is C1-C8 alkyl optionally substituted in one or more places, or C3-C10 cycloalkyl optionally substituted by aryl, and, if R4 is hydrogen, salts thereof with physiologically compatible bases and cyclodextrin clathrates thereof.