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US 5,936,089 AGranted
Dipeptides which promote release of growth hormone
AssigneePfizer Inc.
InventorsPhilip A. Carpino, Paul A. Dasilva-Jardine, Bruce A. Lefker, John A. Ragan
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I) are growth hormone releasing peptide mimetics which are useful for the treatment and prevention of osteoporosis. ##STR1##
Claims14
A compound of the formula:
- ##STR57## wherein Z is --COCR.sup.1 R.sup.2c LCOANR.sup.4 R.sup.5, where L is NR.sup.6 ;
- W in combination with X is a benzo fusion in which W and X arc linked to form a phenyl ring substituted with T-R.sup.3b ;
- X in combination with W is a benzo fusion in which W and X are linked to form a phenyl ring substituted with T-R.sup.3b ;
- Y is hydrogen;
- R.sup.1 is indolyl (C.sub.1 -C.sub.6) alkyl;
- or phenyl (C.sub.0 -C.sub.5) alkyl-K.sup.1 -(C.sub.1 -C.sub.5) alkyl where K.sup.1 is O;
- R.sup.2c is hydrogen or (C.sub.1 -C.sub.6) alkyl;
- T is a bond;
- R.sup.3D is CONR.sup.8 OR.sup.9 ;
- SO.sub.2 NR.sup.8 R.sup.9 ;
- NR.sup.2 SO.sub.2 R.sup.9 ;
- or NR.sup.2 C(O)R.sup.D ;
- R.sup.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl or C.sub.1 -C.sub.6 halogenated alkyl;
- R.sup.4 and R.sup.5 are independently hydrogen of (C.sub.1 -C.sub.6) alkyl;
- R.sup.6 is hydrogen or (C.sub.1 -C.sub.6) alkyl;
- A is ##STR58## where x and y art independently 0-3;
- Z.sup.1 is a bond;
- and R.sup.7 and R.sup.7a are independently hydrogen, (C.sub.1 -C.sub.6) alkyl;
- or trifluoromethyl;
- R.sup.8 is hydrogen or (C.sub.1 -C.sub.6) alkyl;
- R.sup.9 is hydrogen, (C.sub.1 -C.sub.6) alkyl;
- or phenyl optionally substituted with CH.sub.3 or CF.sub.3 ;
- provided that R.sup.9 may not be hydrogen where R.sup.3b is NR.sup.2 SO.sub.2 R.sup.9 ;
- and
- m and n are both 1.
22 more elements
Dependencies are inferred from the claim text.