ARYL CARBAMATE OLIGOMERS FOR HYDROLYZABLE PRODRUGS AND PRODRUGS COMPRISING SAME
申请人:Ekwuribe Nnochiri N.
公开号:US20080146778A1
公开(公告)日:2008-06-19
The present invention provides a compound having a formula: where R
1
is selected from the group consisting of alkyl, CH
2
(OC
2
H
4
)OCH
3
, and —(OC
2
H
4
)OCH
3
; n is 0-4; Olig is an oligomer having a formula:
-L-O-PAGR.R
2
]
q
where L is a optional linker moiety selected from the group consisting of —CH
2
O—, —CH
2
OX—, —OX—, —C(O)—, —C(O)X, —NH—, —NHC(O)—, —XNHC(O)—, —NHC(O)X—, —C(O)NH—, —C(O)NHX—, and
where X is alky
1-6
or is not present, Y is N or O or is not present, and R
3
is alkyl
1-6
; PAG is a linear or branched polyalkylene glycol moiety; R
2
is an alkyl
1-22
capping moiety if X is present or alkyl
2-22
if X is not present; and q is a number from 1 to the maximum number of branches on PAG; and m is 1-5.
NATRIURETIC COMPOUNDS, CONJUGATES, AND USES THEREOF
申请人:James Kenneth D.
公开号:US20100216714A1
公开(公告)日:2010-08-26
Modified natriuretic compounds and conjugates thereof are disclosed in the present invention. In particular, conjugated forms of hBNP are provided that include at least one modifying moiety attached thereto. The modified natriuretic compound conjugates retain activity for stimulating cGMP production, binding to NPR-A receptor, and in some embodiments an improved half-life in circulation as compared to unmodified counterpart natriuretic compounds. Oral, parenteral, enteral, subcutaneous, pulmonary, and intravenous forms of the compounds and conjugates may be prepared as treatments and/or therapies for heart conditions particularly congestive heart failure. Modifying moieties comprising oligomeric structures having a variety of lengths and configurations are also disclosed. Analogs of the natriuretic compound are also disclosed, having an amino acid sequence that is other than the native sequence.