6-n-propyl-2-nitrophenol 在
钯氩 、 氢气 、 甲醇 、 silica gel 作用下,
以
甲醇 为溶剂,
反应 16.17h,
以chromatography of the resulting solid on silica gel (5% MeOH/CH2Cl2) gave the desired product(1.50 g, 80.2%)的产率得到2-Amino-6-propyl-phenol
[EN] IL-8 RECEPTOR ANTAGONISTS<br/>[FR] ANTAGONISTES DES RECEPTEURS D'IL-8
申请人:SMITHKLINE BEECHAM CORPORATION
公开号:WO1996025157A1
公开(公告)日:1996-08-22
(EN) This invention relates to the novel use of phenyl ureas in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).(FR) Cette invention se rapporte à une nouvelle utilisation des urées phényliques dans le traitement d'états pathologiques dont le médiateur est la chimiokine, appelée interleukine-8 (IL-8).
Alkyl-substituted benzoxazinorifamycin derivative, process for preparing
申请人:Kanegafuchi Kagaku Kogyo Kabushiki Kaisha
公开号:US04859661A1
公开(公告)日:1989-08-22
A novel rifamycin derivative having the formula (I): ##STR1## wherein X.sup.1 is an alkyl group with 1 to 6 carbon atoms or a cycloalkyl group with 3 to 8 carbon atoms; X.sup.2 is a hydrogen atom or an alkyl group with 1 to 4 carbon atoms; R.sup.1 is hydrogen atom or acetyl group; A is a group represented by the formula: ##STR2## wherein R.sup.2 is an alkyl group with 1 to 4 carbon atoms or an alkoxyalkyl group with 2 to 6 carbon atoms and R.sup.3 is an alkyl group with 1 to 6 carbon atoms or an alkoxyalkyl group with 2 to 6 carbon atoms, or a group represented by the formula ##STR3## wherein ##STR4## is a 3 to 9 membered cyclic amino group with 2 to 8 carbon atoms, R.sup.4 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, or salts thereof, a process for preparing the same and antibacterial agents containing the same as an effective ingredient. The rifamycin derivative of the present invention having the formula (I) shows a strong antibacterial activity against the Gram-positive bacteria and the acid-fast bacteria.
This invention relates to novel compounds of Formula (I), and a novel use of these compounds in treating chemokine mediated diseases, wherein the chemokine binds to an IL-8 a or b receptor. Compounds of Formula (1) are represented by the structure:
wherein interalia, X is oxygen or sulfur;
R is any functional moiety having an ionizable hydrogen and a pKa of 10 or less;
R1 is independently selected from hydrogen; halogen; nitro; cyano; C1-C10 alkyl; halosubstituted C1-10 alkyl; C2-10 alkenyl; C1-10 alkoxy; halosubstituted C1-10 alkoxy; azide; (CR8R8)qS(O)tR4; hydroxy; hydroxy substituted C1-4 alkyl; aryl; aryl C1-4 alkyl; aryl C2-10 alkenyl; aryloxy; aryl C1-4 alkyloxy; heteroaryl; heteroarylalkyl; heteroaryl C2-10 alkenyl; heteroaryl C1-4 alkyloxy; heterocyclic, heterocyclic C1-4 alkyl; heterocyclic C1-4 alkyloxy; heterocyclic C2-10 alkenyl;
q is 0 or an integer having a value of 1 to 10; n is an integer having a value of 1 to 3;
m is an integer having a value of 1 to 3;
n is an integer having a value of 1 to 3;
Y is hydrogen; halogen; nitro; cyano; halosubstituted C1-10 alkyl; C1-10 alkyl; C2-10 alkenyl; C1-10 alkoxy; halosubstituted C1-1- alkoxy; azide; (CR8R8)qS(O)tR4, (CR8R8)qOR4; hydroxy; hydroxy substituted C1-4 alkyl; aryl; aryl C1-4 alkyl; aryloxy; aryC1-4 alkyloxy; aryl C2-10 alkenyl; heteroaryl; heteroarylalkyl; heteroaryl C1-4 alkyloxy; heteroaryl C2-10 alkenyl; heterocyclic, heterocyclic C1-4 alkyl; heterocyclic C2-10 alkenyl;
or a pharmaceutically acceptable salt thereof.