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`PROVISIONAL APPLICATION FOR PATENT
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`s 1s a request or I mg a PR VI I N
`CATIONFOR PATENT under 37 CFR 1.53(b)(2,t'
`0 SO ALAPPLI
`I Docket Number I AM100144
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`INVENTOR(s) / APPLICANT(s)
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`RESIDENCE
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`5 Whitman Place, Monroe, New York, 10950
`I Dukes Court, Morristown, New Jersey, 07960
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`I
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`LAST NAME
`Zhu
`Fawzi
`
`FIRST NAME
`Tianmin
`Mahdi
`
`·~:r;
`
`TITLE OF THE INVENTION (280 characters max)
`
`WATER SOLUBLE RAPAMYCIN ESTERS
`
`CORRESPONDENCE ADDRESS
`
`')1! ~
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`l;gon E. Berg
`~erican Home Products Corporation
`"'Patent Law Department-2B
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`SIGNATURE
`TYPED OR PRINTED NAME ARNOLDS. MILOWSKY
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`DATE
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`September 19, 2000
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`REG.NO.
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`35,288
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`D Additional inventors are being named on separately numbered sheets attached hereto.
`A n EXHIBIT 1 l J 5
`; 5
`Deponent U
`~~Ii 7 g Rptr.( ~
`
`Breckenridge Exhibit 1092
`Zhu '973 Patent
`Page 0012
`
`I
`
`_
`
`

`

`18 September 2000
`1ED29:0CO:ASM:asm
`AM100144
`PATENT
`
`- 29 -
`
`5
`
`wherein
`R1 and R2 are each, independently, hydrogen or -CO(CR3R4)b(CR5R6)aCR7R8R9;
`R3 and R4 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkenyl of
`2-7 carbon atoms, alkynyl of 2-7 carbon atoms, trifluoromethyl, or -F;
`R5 and R6 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkenyl of
`2-7 carbon atoms, alkynyl of 2-7 carbon atoms, -(CR3R4)tOR 10, -CF3, -F, or
`-CO2Rll;
`R7 is hydrogen, alkyl of 1-6 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of
`2-7 carbon atoms, -(CR3R4)f0Rl0, -CF3, -F, or -C02Rll;
`R8 and R9 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkenyl of
`2-7 carbon atoms, alkynyl of 2-7 carbon atoms, -(CR3R4)f()Rl0, -CF3, -F, or
`-CO2Rll;
`R 10 is hydrogen or -COCH2-S-CH2CH2-(O-CH2-CH2)0-OCH3;
`b = 0-6;
`d = 0-6;
`f = 0-6;
`n = 5-450;
`with the proviso that R1 and R2 are both not hydrogen and further provided that either
`20 R1 or R2 contains at least one -(CR3R4)t<)R10 group in which RlO is
`-COCH2-S-CH2CH2-(O-CH2-CH2)0-OCH3, or a pharmaceutically acceptable salt
`thereof, and a pharmaceutical carrier.
`
`10
`
`15
`
`A compound which is rapamycin 42-ester with 3-hydroxy-2-(2-iodo-
`17.
`acetoxymethyl)-2-methyl-propionic acid.
`
`25
`
`18. A compound which is rapamycin 42-ester with 3-(2-Iodo-acetoxy)-2-(2-iodo-
`acetoxymethyl)-2-methyl-propionic acid.
`
`Breckenridge Exhibit 1092
`Zhu '973 Patent
`Page 0044
`
`