Peptides and compounds that bind to the IL-5 receptor
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-038/00
C07K-005/00
출원번호
US-0478312
(1995-06-07)
발명자
/ 주소
Barrett Ronald W. (Saratoga CA) England Bruce P. (Fremont CA) Schatz Peter J. (Mountain View CA) Sloan Derek (Los Gatos CA) Chen Min-Jia (San Francisco CA)
출원인 / 주소
Affymax Technologies N.V. (Greenford GB2 03)
인용정보
피인용 횟수 :
77인용 특허 :
0
초록▼
Described are peptides and peptide mimetics that bind to and the IL-receptor. Such peptides and peptide mimetics are useful in methods for treating disorders that involve improper production of or response to IL-5 and or the production and accumulation of eosinophils, such as asthma, as well as in d
Described are peptides and peptide mimetics that bind to and the IL-receptor. Such peptides and peptide mimetics are useful in methods for treating disorders that involve improper production of or response to IL-5 and or the production and accumulation of eosinophils, such as asthma, as well as in diagnostic methods employing labeled peptides and peptide mimetics.
대표청구항▼
A compound that binds to IL-5 receptor, said compound comprising: (1) a core sequence of amino acids: C X1 RX2 X7 X8 X3 X4 X5 W X6 C where X1 is D, E, I, S, T, W, or Y; X2 is D, F, G, I, L, S, V, W, or Y; X3 is D, E, G, L, N, S, T, or W; X4 is H or R; X5 is A, K, R, S, T, V, or W; X6 is D, E, F, L,
A compound that binds to IL-5 receptor, said compound comprising: (1) a core sequence of amino acids: C X1 RX2 X7 X8 X3 X4 X5 W X6 C where X1 is D, E, I, S, T, W, or Y; X2 is D, F, G, I, L, S, V, W, or Y; X3 is D, E, G, L, N, S, T, or W; X4 is H or R; X5 is A, K, R, S, T, V, or W; X6 is D, E, F, L, M, P, Q, or V; X7 is I or V; and X8 is A or R (SEQ ID NO:1), and dimers and oligomers thereof, having (a) a molecular weight of less than about 5000 daltons, and (b) a binding affinity to IL5-R as expressed by an IC50 of no more than about 100 m2OC(O)NR－linkage; a phosphonate linkage; a －CH2S(O)2NR－linkage; a －CH2NR－linkage; and a －C(O)NR6－linkage; and a －NHC(O)NH－linkage where R is hydrogen or lower alkyl and R6 is lower alkyl, further wherein the N-terminus of said peptide or peptide mimetic is selected from the group consisting of a －NRR1 group; a －NRC(O)R group; a －NRC(O)OR group; a －NRS(O)2R group; a －NHC(O)NHR group; a succinimide group; a benzyloxycarbonyl-NH－group; and a benzyloxycarbonyl-NH－group having from 1 to 3 substituents on the phenyl ring selected from the group consisting of lower alkyl, lower alkoxy, chloro, and bromo, where R and R1 are independently selected from the group consisting of hydrogen and lower alkyl, and still further wherein the C-terminus of said peptide or peptide mimetic has the formula －C(O)R2 where R2 is selected from the group consisting of hydroxy, lower alkoxy, and －NR3R4 where R3 and R4 are independently selected from the group consisting of hydrogen and lower alkyl and where the nitrogen atom of the －NR3R4 group can optionally be the amine group of the N-terminus of the peptide so as to form a cyclic peptide, or a physiologically acceptable salt thereof.
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