Back to results
US 2004/0002508 A1Published application
Rho-kinase inhibitors
AssigneeBayer Aktiengesellschaft
InventorsDhanapalan Nagarathnam, Jacques Dumas, Holia Hatoum-Mokdad, Stephen Boyer, Chunguang Wang, Hans Pluempe, Achim Feurer, Samir Bennabi
Life of this patent
Estimating the term…
Abstract
Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.
Claims15
A compound of formula I
- 105
- wherein
- R1 and R2 are each independently
- H, halo, alkyl, optionally substituted by halo up to the perhalo, cycloalkyl, alkenyl, alkynyl, NO2, NH2, NR6R7, or furyl, thienyl, pyridyl, trifluoromethyl or phenyl each optionally substituted with NH2, NO2, trifluoromethyl or alkoxy;
- or
- R1 and R2 may be taken together to form a ring of from 5 to 7 members optionally interrupted by N and optionally substituted on N by benzyl;
- R3 is NH2 or —NH— phenyl optionally substituted with halo, C1-C4 alkyl, trifluoromethyl, nitro or amino;
- R4 is
- 106
- or indol-5-yl (optionally) substituted on the N with pyridyl;
- X is a linker substituted at the 3 or 4 position of the ring and is O,S,—S—CH2—, —(CH2)m—, or —(C=0)—;
- A is phenyl optionally substituted with alkylthio or OH,
- pyridyl,
- quinolyl or
- isoquinolyl;
- each R5 independently is halo, alkyl optionally substituted by halo up to the perhalo level, cycloalkyl, alkoxy, alkenyl, alkynyl, NO2, NH2, or trifluoromethyl;
- n is 0,1,2,3 or 4;
- m is 1 or 2;
- and
- R6 and R7 are each independently H, alkyl, cycloalkyl, or phenyl optionally substituted with halo, CF3, alkyl, nitro or amino;
- or
- R6 and R7 may form, together with the N atom to which they are attached, a heterocyclic ring optionally substituted with alkyl, optionally interrupted by O, or optionally fused to phenyl;
- or a pharmaceutically acceptable salt thereof,
- with the proviso that formula I does not include the following compounds:
- 107 108 109 110 111 112 113 114 115 116 117 118
22 more elements
Dependencies are inferred from the claim text.