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Details for Patent: 5,883,099

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Details for Patent: 5,883,099

Title: Inhibitors of microsomal triglyceride transfer protein and method
Abstract:Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.7, Q, X and Y are as defined herein.
Inventor(s): Biller; Scott A. (Hopewell, NJ), Dickson; John K. (Eastampton, NJ), Lawrence; R. Michael (Yardley, PA), Magnin; David R. (Hamilton, NJ), Poss; Michael A. (Lawrenceville, NJ), Sulsky; Richard B. (Franklin Park, NJ), Tino; Joseph A. (Lawrenceville, NJ), Lawson; John E. (Wallingford, CT), Holava; Henry M. (Meriden, CT), Partyka; Richard A. (Neshanic, NJ)
Assignee: Bristol-Myers Squibb Company (Princeton, NJ)
Filing Date:Jul 21, 1997
Application Number:08/896,872
Claims:1. A compound which has the stricture ##STR444## wherein m is 2 or:3; R.sup.2, R.sup.3, R.sup.4 are independently hydrogen, halo, alkyl, alkenyl, alkoxy, aryloxy, aryl, arylalkyl, alkylmercapto, arylmercapto, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, hydroxyl or haloalkyl;

R.sup.7 is alkyl, aryl or arylalkyl wherein alkyl by itself or as part of arylalky is optionally substituted with oxo ##STR445## or a pharmaceutically acceptable salt thereof;

with the provisos that

(1) where R.sup.2, R.sup.3 and R.sup.4 are each H or where one of R.sup.2, R.sup.3 and R.sup.4 is 6-fluoro, and the others are H, R.sup.7 will be other then 4-(2-methoxyphenyl); and (2) where R.sup.2, R.sup.3 and R.sup.4 are each H or where one of R.sup.2, R.sup.3 and R.sup.4, is 6-fluoro, and the others are H, then where R.sup.7 is alkyl or arylalkyl, the alkyl by itself or as part of arylalkyl will not be substituted with oxo ##STR446##

2. The compound as defined in claim 1

wherein:

R.sup.2, R.sup.3, R.sup.4 are independently hydrogen, halo, alkyl, alkenyl, alkoxy, aryloxy, aryl, arylalkyl, alkylmercapto, arylmercapto.

3. A method for treating atherosclerosis; pancreatitis obesity or hyperglycemia, responsive to a decrease in MTP activity, in a patient, which comprises administering to a patient in need of treatment an MTP activity decreasing amount of a compound of the structure ##STR447## wherein m is 2 or 3;

R.sup.2, R.sup.3, R.sup.4 are independently hydrogen, halo, alkyl, alkenyl, alkoxy, aryloxy, axyl, arylalkyl, alkylmercapto, arylmercapto, cyoloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, hydroxy or haloalkyl;

R.sup.7 is alkyl, aryl or arylalkyl wherein alkyl by itself or as part of arylalkyl is optionally substituted with oxo ##STR448## or a pharmaceutically acceptable salt thereof.

4. A method of lowering serum lipid levels, cholesterol or triglycerides, or treatins hyperlipemia, hyperlipidemia, hyperlipoproteinemia, hyplrcholesterolemia or hypertriglyceridemia, responsive to a decrease in MTP activity, in a patient, which comprises administering to a patient in need of treatment an MTP activity decreasing amount of a compound of the structure ##STR449## wherein m is 2 or 3;

R.sup.2, R.sup.3, R.sup.4 are independently hydrogen, halo, alkyl, alkenyl, alkoxy, aryloxy, aryl, arylalkyl, alkylmercapto, arylmercapto, cycloalkyl cycloalkylalkyl, heteroaryl, heteroarylalkyl, hydroxy or haloalkyl;

R.sup.7 is alkyl, aryl or arylalkyl wherein alkyl by itself or as part of arylalkyl is optionally substituted with oxo ##STR450## or a pharmaceutically acceptable salt thereof.

5. The compound as defined in claim 1 wherein Y is ##STR451## .

6. The compound as defined in claim 1 wherein R.sup.7 is aryl.

7. The compound as defined in claim 1 wherein R.sup.7 is phenyl or phenyl substituted with alkoxy.

8. The compound as defined in claim 1 wherein R.sup.7 is phenyl or 2-methoxyphenyl.

9. A compound which is 3,4-dihydro-3-[[4-phenyl-1-piperazinyl]methyl]-1(2H)-naphthalenone; or

3,4-dihydro-3-[[4-(2-methoxyphenyl)-1-piperazinyl]-carbonyl]-1(2H) -naphthalenone.
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