The present invention provides novel conjugates of camptothecin and camptothecin analogs with a linker and an HSA-binding moiety. The novel conjugates are prodrug forms of the camptothecin or camptothecin analogs and can be used to treat mammalian cell proliferative diseases, such as cancer.
Substituted &bgr;-amino acid inhibitors of methionine aminopeptidase-2
申请人:Abbott Laboratories
公开号:US06242494B1
公开(公告)日:2001-06-05
A class of substituted b-amino acids are potent inhibitor of methionine aminopeptidase type 2 (MetAP2) and are thus useful in inhibiting angiogenesis and disease conditions which depend upon angiogenesis for their development such as diabetic retinopathy, tumor growth, and conditions of inflammation. Pharmaceutical compounds containing the compounds and methods of inhibiting methionine aminopeptidase-2, and angiogenesis are also disclosed.
Process For Preparing Porphyrin Derivatives, Such As Protoporphyrin (IX) And Synthesis Intermediates
申请人:Martin Pierre
公开号:US20080242857A1
公开(公告)日:2008-10-02
The present invention relates to a process for preparing a porphyrin of formula (I), optionally in the form of a salt with an alkali metal and/or in the form of a metal complex:
in which:
R and R′ are as defined in claim
1
,
comprising:
a step of condensation, in an acidic medium, between a dipyrromethane of formula (II):
in which R′b is as defined above for (I),
and a dipyrromethane of formula (III):
in which R″ is as defined in claim
1
, and also the compounds of formula (III).
Quinolone based compounds exhibiting prolyl hydroxylase inhibitory activity, and compositions, and uses thereof
申请人:Allen R. Jennifer
公开号:US20070249605A1
公开(公告)日:2007-10-25
This invention relates to new quinolone based compounds that exhibit prolyl hydroxylase inhibitory activity. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one quinolone based compound. This invention further involves assays for the detection of a hydroxyproline residue in a HIF molecule.
Synthesis and biological activity of amino acid derivatives of sulfanilic acid
作者:N. M. Divanyan、L. Kh. Galstyan、A. A. Chachoyan、B. T. Garibdzhanyan、N. O. Stepanyan、Zh. M. Bunatyan、G. M. Paronikyan、L. G. Akopyan、R. V. Paronikyan、O. L. Mndzhoyan
DOI:10.1007/bf00761543
日期:1982.7
NaOH NaOH; HCI I V q H A m O H ~ I I a i r ~ I I j I IIa: R = C H a , A m = G l y ; I I b : R = C H s , A m = D A l a ; I i c : R-----CHa, A m = D L A l a ; l id: R = C~Hs, Am = D L A l a ; IIe: R-~-CHa, A m = L-Phe; I l l : R C ~ H s , Am ---D-Val; I Ig : R = C.~Hs, Am ----DL-Leu; IIh: R = CHz, Am L-Trp; I i i : R := CHa, Am = DL-Trp; 1Ii: Am ----DL-AIa; I l k : A m = D-Val; I11 : Am = DL-Leu.
氢氧化钠 氢氧化钠;HCI IV q HA m OH ~ II 空气 ~ II j I IIa:R = CH a ,A m = G ly ;II b : R = CH s ,A m = DA la ;I ic : R-----CHa, A m = DLA la ; l id:R = C~Hs,Am = DLA la;IIe:R-~-CHa,A m = L-Phe;Ill : RC ~ H s , Am ---D-Val; I Ig : R = C.~Hs, Am ----DL-Leu; IIh:R = CHZ,Am L-Trp;I ii : R := CHa,Am = DL-Trp;1Ii:是----DL-AIa;Ilk : A m = D-Val; I11:Am = DL-Leu。