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Home Gene Therapy 6-11-bicyclic-erythromycin-derivatives

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 6,11-bicyclic erythromycin derivatives

Details
Inventors: Or, Yat Sun; Wang, Guoqiang; Phan, Ly Tam; Niu, Deqiang; Qiu, Yao-Ling; Vo, Nha Huu; Farmer, Jay Judson; Hou, Ying;
Assignee: Enanta Pharmaceuticals, Inc. (Watertown, MA)
Primary Examiner: Wilson; James O.
Assistant Examiner: Krishnan; Ganapathy
Attorney, Agent or Firm: Elmore, Craig & Vanstone, P.C. Vanstone; Darlene A. Elmore; Carolyn S.

The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: ##STR00001## which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

DETAILED DESCRIPTION OF THE INVENTION A first embodiment of the present invention is a compound of formula I as defined herein, or its pharmaceutically acceptable salt, ester, or prodrug.
Representative subgenera of the present invention are: A compound according to claim 1, which is represented by formula II: ##STR00005## where A, B, Q, R.
sub.
2', W, and Z are as previously defined; A compound according to claim 1, which is represented by formula III: ##STR00006## where A, B, Q, R.
sub.
2', and Z are as previously defined; A compound according to claim 1, which is represented by formula IV: ##STR00007## where A, B, Q, R.
sub.
2', and R.
sub.
4'' are as previously defined; A compound according to claim 1, which is represented by formula V: ##STR00008## where A, B, Q, and R.
sub.
2' are as previously defined; A compound according to claim 1, which is represented by formula VI: ##STR00009## where Ar.
sub.
1, Ar.
sub.
2, M, Q, R.
sub.
2', W, and Z are as previously defined; A compound according to claim 1, which is represented by formula VII: ##STR00010## where Ar.
sub.
1, Ar.
sub.
2, M, Q, R.
sub.
2', and Z are as previously defined; A compound according to claim 1, which is represented by formula VIII: ##STR00011## where Ar.
sub.
1, Ar.
sub.
2, M, R.
sub.
2', and Z are as previously defined; A compound according to claim 1, which is represented by formula IX: ##STR00012## where Ar.
sub.
1, Ar.
sub.
2, M, Q, R.
sub.
2', and R.
sub.
4'' are as previously defined; and A compound according to claim 1, which is represented by formula X: ##STR00013## where Ar.
sub.
1, Ar.
sub.
2, M, Q, and R.
sub.
2' are as previously defined.
Representative compounds according to the invention are those selected from: 1) Compound of formula IV: A and B taken together with the carbon atom to which they are attached=C.
dbd.
CH.
sub.
2, Q=OH, R.
sub.
2' is H, and R.
sub.
4''=Ac; 2) Compound of formula IV: A and B taken together with the carbon atom to which are attached=C.
dbd.
CH.
sub.
2, Q=H, R.
sub.
2=H, and R.
sub.
4''=Ac; 3) Compound of formula V: A and B taken together with the carbon atom to which they are attached=C



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