Substituted pyrroles
AssigneeHoffman-La Roche Inc.
InventorsPeter D. Davis, Christopher H. Hill, Goeffrey Lawton
Life of this patent
Estimating the term…
Abstract
Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X, m, n, p, and q are as set forth in the specification, as well as pharmaceutically acceptable salts of acidic compounds of formula I with bases and of basic compounds of formula I with acids, which are useful in the control or prevention of inflammatory, immunological, oncological, bronchopulmonary, dermatological or cardiovascular disorders or for the treatment of asthma, AIDS or diabetic complications or for the stimulation of hair growth are described.
Claims24
A compound of the formula ##STR8## wherein R.sup.1 and R.sup.3 together form a bond and R.sup.2 is hydrogen or R.sup.1 and R.sup.2 together form a bond and R.sup.3 is hydrogen;
- R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently are hydrogen, halogen, C.sub.1-7 alkyl, halo C.sub.1-7 alkyl, C.sub.1-7 alkoxy, nitro, amino, C.sub.1-7 alkanoylamino, aroylamino, C.sub.1-7 alkylthio or C.sub.1-7 alkylsulfonyl;
- R.sup.8 is hydrogen, C.sub.1-7 alkyl or aryl C.sub.1-7 alkyl;
- X is --N(R.sup.9)-- or --CHN(R.sup.10,R.sup.11)-- in which R.sup.9, R.sup.10 and R.sup.11 each are hydrogen, C.sub.1-7 alkyl, aryl C.sub.1-7 alkyl or C.sub.1-7 alkanoyl;
- m is 0-2 and n is 1-3, with the proviso that the sum of m and n is 1-3;
- p is 0-4 and q is 0-4, with the proviso that the sum of p and q is 2-4 when X is --N(R.sup.9)--, that the sum of p and q is 1-5 when X is --CHN(R.sup.10, R.sup.11)-- and R.sup.1 and R.sup.2 together form a bond, that the sum of p and q is 0-4 when X is --CHN(R.sup.10, R.sup.11)-- and R.sup.1 and R.sup.3 together form a bond, and that p is 1-4 when X is --N(R.sup.9)--, R.sup.1 and R.sup.3 together represent a bond and m is 0,
- or a pharmaceutically acceptable salt of an acidic compound of formula I with a base or of a basic compound of formula I with an acid.
A compound of the formula ##STR9## wherein R.sup.1 and R.sup.3 together form a bond and R.sup.2 is hydrogen or R.sup.1 and R.sup.2 together form a bond and R.sup.3 is hydrogen;
- R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently are hydrogen, halogen, C.sub.1-7 alkyl, halo C.sub.1-7 alkyl, C.sub.1-7 alkoxy, nitro, amino, C.sub.1-7 alkanoylamino, aroylamino, C.sub.1-7 alkylthio or C.sub.1-7 alkylsulfonyl;
- R.sup.8 is hydrogen, C.sub.1-7 alkyl or aryl-C.sub.1-7 -alkyl;
- m is 0-2 and n is 1-3, with the proviso that the sum of m and n is 1-3;
- p is 0-4 and q is 0-4, with the proviso that the sum of p and q is 2-4 when X' is --N(R.sup.9')--, that the sum of p and q is 1-5 when X' is --CHN(R.sup.10', .sup.11'")-- and R.sup.1 and R.sup.2 together form a bond, that the sum of p and q is 0-4 when X' is --CHN(R.sup.10',R.sup.11')-- and R.sup.1 and R.sup.3 together form a bond, and that p is 1-4 when X' is --N(R.sup.9')--, R.sup.1 and R.sup.3 together represent a bond and m is O, X' is --N(R.sup.9')-- or --CHN(R.sup.10',R.sup.11')-- in which R.sup.9', R.sup.10' and R.sup.11' each are hydrogen, C.sub.1-7 alkyl, aryl-C.sub.1-7 -alkyl, C.sub.1-7 alkanoyl, alkoxycarbonyl or aryloxycarbonyl.
A pharmaceutical composition comprising an effective amount of a compound of the formula ##STR10## wherein R.sup.1 and R.sup.3 together form a bond and R.sup.2 is hydrogen or R.sup.1 and R.sup.2 together form a bond and R.sup.3 is hydrogen;
- R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently are hydrogen, halogen, C.sub.1-7 alkyl, halo C.sub.1-7 alkyl, C.sub.1-7 alkoxy, nitro, amino, C.sub.1-7 alkanoylamino, aroylamino, C.sub.1-7 alkylthio or C.sub.1-7 alkylsulfonyl;
- R.sup.8 is hydrogen, C.sub.1-7 alkyl or aryl C.sub.1-7 alkyl;
- X is --N(R.sup.9)-- or --CHN(R.sup.10,R.sup.11)-- in which R.sup.9, R.sup.10 and R.sup.11 each are hydrogen, C.sub.1-7 alkyl, aryl C.sub.1-7 alkyl or C.sub.1-7 alkanoyl;
- m is 0-2 and n is 1-3, with the proviso that the sum of m and n is 1-3;
- p is 0-4 and q is 0-4, with the proviso that the sum of p and q is 2-4 when X is --N(R.sup.9)--, that the sum of p and q is 1-5 when X is --CHN(R.sup.10,R.sup.11)-- and R.sup.1 and R.sup.2 together form a bond, that the sum of p and q is 0-4 when X is --CHN(R.sup.10,R.sup.11)-- and R.sup.1 and R.sup.3 together form a bond, and that p is 1-4 when X is --N(R.sup.9)--, R.sup.1 and R.sup.3 together represent a bond and m is 0, or a pharmaceutically acceptable salt of an acidic compound of formula I with a base or a basic compound of formula I with an acid, and a therapeutically inert carrier.
The compound, trans-3-[2,3,3a,4,11,11a-Hexahydro-2-methyl-1H-pyrrolo[3',4':4,5]pyrido[1, 2-a]indol-10-yl]-4-(1-methyl-3-indolyl)-1H-pyrrole-2,5-dione.
Dependencies are inferred from the claim text.