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US 2004/0176421 A1Published application
Tryptase inhibitors
AssigneeAltana Pharma AG
InventorsThomas Martin, Wolf-Rudiger Ulrich
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I) in which M, B1, B2, R1, R2, R6, R7, K1 and K2 have the meanings indicated in the description are novel active tryptase inhibitors. 1
Claims8
A compound of formula I
- 14
- in which
- M is a central structural unit selected from the following list
- 15
- where
- n is 1 or 2,
- U1 and U2 are identical or different and are methylene [—CH2—], ethylene [—CH2—CH2—], trimethylene [—CH2—CH2—CH2], tetramethylene [—CH2—CH2—CH2—CH2—] or isopropylidene [—C(CH3)2—],
- K1 is —B3-Z1-B5X1,
- K2 is —B4-Z2-B6-X2,
- B1 and B2 are identical or different and are —O—, —NH—, —O—(CH2)m—O— or —O—(CH2)m—NH—,
- m is 1, 2, 3 or 4,
- B3 and B4 are identical or different and are a bond or 1-2C-alkylene,
- B5 and B6 are identical or different and are a bond or 1-2C-alkylene,
- X1 and X2 are identical or different and are amino, aminocarbonyl, amidino or guanidino,
- Z1 and Z2 are identical or different and are 5,2-pyridinylene, 6-methyl-5,2-pyridinylene, 4,1-piperidinylene, 3,6-indazolylene, 3,6-indolylene, 1,3-phenylene, 1,4-phenylene, 1,3-cyclohexylene or 1,4-cyclohexylene,
- R1 and R2 are identical or different and are —C(O)OR3 or —C(O)N(R4)R5, where
- R3 is hydrogen, 1-4C-alkyl, 3-7C-cycloalkyl, 3-7C-cycloalkylmethyl or benzyl,
- R4 and R5 are, independently of one another, hydrogen, 1-4C-alkyl, 3-7C-cycloalkyl or
- 3-7C-cycloalkylmethyl, or in which R4 and R5 together and with inclusion of the nitrogen atom to which they are bonded are a 1-pyrrolidinyl, 1-piperidinyl, 1-hexahydroazepinyl, 1-piperazinyl or 4-morpholinyl radical,
- R6 and R7 are identical or different and are hydrogen or 1-2C-alkyl,
- or a salt of this compound.
18 more elements
Dependencies are inferred from the claim text.