1
Bey Philippe, Angelastro Michael, Mehdi Shujaath: Novel peptidase inhibitors.. Merrell Dow Pharma, April 11, 1990: EP0363284-A2 (98 worldwide citation)

This invention relates to analogs of peptidase substrates in which the nitrogen atom of the scissile amide gorup of the substrate peptide has been replaced by H or a substituted carbonyl moiety. The contemplated peptidase inhibitors of the foregoing enzymes are selected from the generic formula R1NH ...


2
Bey Philippe, Angelastro Michael, Mehdi Shujaath: Novel peptidase inhibitors.. Merrell Dow Pharma, April 18, 1990: EP0364344-A2 (90 worldwide citation)

This invention relates to analogs of peptidase substrates in which the nitrogen atom of the scissile amide group of the substrate peptide has been replaced by a substituted malonyl moiety. The contemplated peptidase inhibitors of the foregoing enzymes are selected from the generic formula the hydrat ...


3
Bey Philippe, Peet Norton P, Angelastro Michael R, Mehdi Shujaath: Novel peptidase inhibitors.. Merrell Dow Pharma, January 30, 1991: EP0410411-A2 (81 worldwide citation)

This invention relates to activated electrophilic ketone analogs of certain peptidase substrates which are useful in inhibiting serine-, carboxylic acid- and metallo- proteolytic enzymes, the inhibition of which will have useful physiological consequences in a variety of disease states.


4
Peet Norton P, Angelastro Michael R, Burkhart Joseph P: Novel orally-active elastase inhibitors.. Merrell Dow Pharma, March 3, 1993: EP0529568-A1 (48 worldwide citation)

This invention relates to novel morpholinourea and related derivatives of pentafluoroethyl peptides which are orally active elastase inhibitors. Pharmaceutical compositions containing these compounds are useful in the treatment of various inflammatory diseases and emphysema.


5
Angelastro Michael R, Blohm Thomas R: C17-20 lyase inhibitors.. Merrell Dow Pharma, October 26, 1988: EP0288053-A1 (9 worldwide citation)

This invention is directed to 17 beta -(cyclopropylamino)androst-5-en-3 beta -ol and related compounds and also to a method for using such compounds in the treatment of androgen-dependent disorders. The compounds are prepared by the hydride reduction of an appropriate steroidal imine or enamine.


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Angelastro Michael R, Blohm Thomas R: (cyclopropylamino)Androst-5-en-3beta-ol and related compounds useful as c17-20 lyase inhibitors.. Merrell Dow Pharma, February 20, 1991: EP0413270-A2 (5 worldwide citation)

This invention is directed to 4-substituted 17 beta -(cyclopropylamino)androst-5-en-3 beta -ol and related compounds and also to a method for using such compounds in the treatment of androgen-dependent disorders. The compounds are prepared by the hydride reduction of an appropriate steroidal imine o ...


8
Angelastro Michael R, Blohm Thomas R: (cyclopropyloxy) Androst-5-en-3beta-ol and related compounds useful as c 17-20 lyase inhibitors.. Merrell Dow Pharma, November 23, 1988: EP0291717-A1 (4 worldwide citation)

This invention is directed to 17 beta -(cyclopropyloxy)androst-5-en-3 beta -ol and related compounds and also to a method for using such compounds in the treatment of androgen-dependent disorders. The ethers are prepared by using the Simmons-Smith reaction and an appropriate vinyl ether.


9
Cordell Barbara, Schirlin Daniel, Peet Norton P, Higaki Jeffrey N, Van, Dorsselaer Viviane, Angelastro Michael R: Inhibitors of $g(b)-amyloid protein production. Merrell Pharmaceuticals, Scois Nova, Cordell Barbara, Schirlin Daniel, Peet Norton P, Higaki Jeffrey N, Van, Dorsselaer Viviane, Angelastro Michael R, NESBITT Stephen L, April 13, 1995: WO/1995/009838 (1 worldwide citation)

This invention relates to compounds and pharmaceutical compositions, and methods for inhibiting or preventing the amyloid protein deposits in the brain which are associated with Alzheimer's disease and aged Down's syndrome patients. More particularly, it relates to the treatment of Alzheimer's disea ...


10
Angelastro Michael R, Bey Philippe, Doherty Niall S, Janusz Michael J, Mehdi Shujaath, Peet Norton P: Inhibitors of cathepsin g and elastase for preventing connective tissue degradation.. Merrell Dow Pharma, March 23, 1994: EP0587799-A1

Novel compounds which are chemically linked inhibitors of the proteases Elastase and Cathepsin G prevent connective tissue degradation associated with neutrophil induced inflammatory disease.