Patent DE-102005009705-A1 (DE)
Title: Use of naphthalene derivatives for the treatment of hyperaldosteronism, heart failure, myocardial fibrosis, hypercortisolism and diabetes mellitus
Inventor: HARTMANN ROLF W
IPC: A61P9/00
Filed: 2005-03-03
Abstract: Use of naphthalene derivatives (I) or their salts for the treatment of hyperaldosteronism, heart failure, myocardial fibrosis, hypercortisolism and diabetes mellitus. Use of naphthalene derivatives of formula (I) or their salts for the treatment of hyperaldosteronism, heart failure, myocardial fibrosis, hypercortisolism and diabetes mellitus. Y1>(=C(R9>)2), (=N(R10>)), (=O) or (=S); T1>, U1>, V1>, W1>, X1>C or N; R1>, R2>H, halo, CN, OH, nitro, alkyl, alkoxy, alkyl carbonyl, alkylcarbonyloxy, alkylaminocarbonyl, alkylaminosulfonyl, thioalkyl, alkylsulfinyl or alkyl sulfonyl; R3>nitrogenous mono- or bicyclic heteroaryl residue (where partially or completely saturated equivalents and substituted) and N atom which is not substituted; R4>-R9>H, halo, CN, OH, nitro, lower alkyl, lower alkoxy, lower alkylcarbonyl, lower alkylcarbonyloxy, lower alkylaminocarbonyl, lower alkyaminosulfonyl, lower thioalkyl, lower alkylsulfinyl, lower alkylsulfonyl, arylalkyloxy, heteroarylalkyloxy; and n : 0-2. Full definitions are given in the DEFINITIONS (Full Definitions) Field. Independent claims are included for (1) a pharmaceutical composition comprising (I); (2) a naphthalene derivative (I) (with provisos); and (3) the preparation of (I). Provided that (in composition): when T1>, U1>, V1>, W1> and X1> are C, n is 1, and Y1> is O, CH2 or -CH, then R3> is not 1-imidazolyl; when T1>, U1>, V1>, W1>, X1> are C, n is 1, R1>, R2>, R4>-R9> is H, and R6> is H or methyl, then R3> is not 3-pyridyl; when T1>, U1>, V1> and Y1> are C, n is 1, R2>, R4>-R8> and R9> are H atom, and R1> is carboxylic acid, then R3> is not 4-pyridyl; when T1>, U1>, V1>, W1> and Y1> are C atom, X1> is N, n is 1, R1>, R2>, R4>, R5> and R7> are H atom, R9> is H or methyl and R8> with Y1> forms a double bond, then R3> is not pyridyl; when T1>, U1>, V1>, W1> and X1> are C, Y1> is N, n is 1, R1>, R2>, R4>-R7> are H and R8> with Y1> forms a double bond, then R3> is not 4-carboxy-2-pyridyl. Provided that: when T1>, U1>, V1>, W1> and X1> are C, n is 1, and Y1> is O, CH2 or -CH, then R3> is not 1-imidazolyl; when T1>, U1>, V1>, W1>, X1> are C, n is 1, R1>, R4>-R9> are H, R2> is H or methoxy and R6> is H or methyl, then R3> is not pyridyl, imidazolyl or oxazolyl; when T1>, U1>, V1>, W1>, X1> are C, n is 1, R2>, R4>-R9> are H and R1> is carboxylic acid, then R3> is not 4-pyridyl; when T1>, U1>, V1>, W1>, X1> are C, n is 1, R1>, R2>, R4>, R5> and R7> are H, R9> is H or methyl and R8> with Y1> forms double bond, then R3> is not pyridyl or quinolyl; when T1>, U1>, V1>, W1> and X1> are C, Y is N, n is 1, R1>, R2>, R4>-R7> are H and R8> with Y1> forms a double bond, then R3> is not 4-carboxy-2-pyridyl, 5-bromo-2-pyridyl, 6 -bromo-2-pyridyl, 5-bromo-3-pyridyl, 2-pyridyl, 3-pyridyl, 2-pyridazinyl, 2-pyrimidinyl or quinolyl; and when T1>, U1>, V1> and W1> are C, n is 1, R1>, R2>, R4>, R5> and R7> are H and R8> with Y1> forms a double bond, then R3> is not pyridyl or 2-quinolyl. [Image] ACTIVITY : Cardiant; Antiinflammatory; Antidiabetic. MECHANISM OF ACTION : Mammalian- P450-oxygenase inhibitor; Human or mammalian-aldosterone synthase or steroid-11beta -hydroxylase inhibitor; Human steroid-11beta -hydroxylase CYP11B1 or aldosterone synthase CYP11B2 inhibitor.