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James Doherty
Dorn Conrad P, Finke Paul E, Maccoss Malcolm, Doherty James B, Shah Shrenik K, Hagmann William K: New substituted azetidinones as anti-inflammatory and antidegenerative agents.. Merck & Co, April 22, 1992: EP0481671-A1 (40 worldwide citation)

New substituted azetidinones of the general formula (A') which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described. e


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Kevin Rodzinak
Armstrong Donna J, Hu Essa H, Kelly Michael J Iii, Layton Mark E, Li Yiwei, Liang Jun, Rodzinak Kevin J, Rossi Michael A, Sanderson Philip E, Wang Jiabing: Inhibiteurs de lactivite akt, Inhibitors of akt activity. Merck & Co, Merck Sharp & Dohme, Gowling Lafleur Henderson, February 8, 2011: CA2610888

The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt ...


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Valentino J Stella, Paul E Kennedy: Prodrugs of rapamycin. University of Kansas, Arthur G Seifert, March 17, 1987: US04650803 (223 worldwide citation)

Water soluble prodrugs of rapamycin are disclosed which are useful as components in injectable pharmaceutical formulations for the treatment of tumors in mammals.


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Amedeo A Failli, Robert J Steffan: Silyl ethers of rapamycin. American Home Products Corporation, Arnold S Milowsky, June 9, 1992: US05120842 (208 worldwide citation)

A compound of the structure ##STR1## wherein R.sup.1 is --SiR.sup.3 R.sup.4 R.sup.5 ;


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Jerauld S Skotnicki, Christina L Leone, Guy A Schiehser: Rapamycin hydroxyesters. American Home Products Corporation, Arnold S Milowsky, November 8, 1994: US05362718 (195 worldwide citation)

A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or --CO(CR.sup.3 R.sup.4).sub.b (CR.sup.5 R.sup.6).sub.d CR.sup.7 R.sup.8 R.sup.9 ;


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Joseph A Walder, Roxanne Y Walder, Paul S Eder, John M Dagle: Methods for blocking the expression of specifically targeted genes. University of Iowa Research Foundation, Pennie & Edmonds, February 13, 1996: US05491133 (170 worldwide citation)

The use of oligodeoxynucleotides modified at the 3'-terminal internucleotide link as therapeutic agents by a method of hybridizing the modified oligonucleotide to a complementary sequence within a targeted mRNA and cleaving the mRNA within the RNA-DNA helix by the enzyme RNaseH to block the expressi ...


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Wenling Kao, Robert L Vogel, John H Musser: Carbamates of rapamycin. American Home Products Corporation, Arnold S Milowsky, June 2, 1992: US05118678 (166 worldwide citation)

A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or --CONH(CR.sup.3 R.sup.4).sub.n --X;


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Craig E Caufield, Guy A Schiehser: Rapamycin acetals as immunosuppressant and antifungal agents. American Home Products Corporation, Robert F Boswell Jr, September 29, 1992: US05151413 (164 worldwide citation)

Derivatives of Rapamycin where the hydroxy group at position 31 and/or 42 are reacted with acetal forming reagents have been shown to have immunosuppressant and antifungal properties. These derivatives are represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 independently are hydrogen, - ...