公开(公告)号：WO1998004573A1

公开(公告)日：1998-02-05

申请号：PCT/US1997013128

申请日：1997-07-25

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  LIU, Jih-Hua ,  RILEY, David, A. ,  SPANTON, Stephen, G.

IPC: C07H17/08

CPC classification number: C07H17/08

Abstract: The present invention concerns the novel antiobiotic 6-O-methylerythromycin A crystal Form I, a process for its preparation, pharmaceutical compositions comprising this compound and a method of use as a therapeutic agent.

Abstract translation: 本发明涉及新型抗生素6-O-甲基红霉素A晶型I，其制备方法，包含该化合物的药物组合物和用作治疗剂的方法。

公开(公告)号：WO1997036912A1

公开(公告)日：1997-10-09

申请号：PCT/US1997001952

申请日：1997-02-06

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  YANG, Chengxi ,  PATEL, Hemantkumar, H. ,  KU, Yi-Kin ,  LIU, Jih-Hua

IPC: C07H17/08

CPC classification number: C07H17/08 ,  Y02P20/55

Abstract: A process of preparing a 6-O-methyl erythromycin A derivative using a 2'-protected, 9-etheroxime erythromycin A intermediate is provided. A preferred protecting group for the 2'-position is acetyl. 2'-protected, 9-etheroxime erythromycin A derivatives are also provided. Also disclosed is a method for inhibiting quaternary salt formation at the 3' amine without the need for 3'N-protecting groups.

Abstract translation: 提供了使用2'-保护的9-乙烯基肟红霉素A中间体制备6-O-甲基红霉素A衍生物的方法。 2位的优选保护基是乙酰基。 还提供了2'-保护的9-乙酰肟红霉素A衍生物。 还公开了抑制在3'胺上形成季盐的方法，而不需要3'N保护基团。

公开(公告)号：WO1997021685A1

公开(公告)日：1997-06-19

申请号：PCT/US1996020440

申请日：1996-12-06

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  SHAM, Hing, Leung ,  NORBECK, Daniel, W. ,  CHEN, Xiaoqi ,  BETEBENNER, David, A. ,  KEMPF, Dale, J. ,  HERRIN, Thomas, R. ,  KUMAR, Gondi, N. ,  CONDON, Stephen, L. ,  COOPER, Arthur, J. ,  DICKMAN, Daniel, A. ,  HANNICK, Steven, M. ,  KOLACZKOWSKI, Lawrence ,  OLIVER, Patricia, A. ,  PLATA, Daniel, J. ,  STENGEL, Peter, J. ,  STONER, Eric, J. ,  TIEN, Jieh-Heh, J. ,  LIU, Jih-Hua ,  PATEL, Ketan, M.

IPC: C07D239/10

CPC classification number: C07D207/27 ,  C07D207/404 ,  C07D207/408 ,  C07D223/10 ,  C07D233/32 ,  C07D233/42 ,  C07D239/10 ,  C07D239/22 ,  C07D241/08 ,  C07D241/18 ,  C07D253/06 ,  C07D263/22 ,  C07D307/20 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12

Abstract: A compound of formula (I) is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

Abstract translation: 公开了式（I）化合物作为HIV蛋白酶抑制剂。 还公开了用于抑制HIV感染的方法和组合物。

公开(公告)号：WO1998031699A1

公开(公告)日：1998-07-23

申请号：PCT/US1997023607

申请日：1997-12-19

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  SPANTON, Stephen, G. ,  HENRY, Rodger, F. ,  RILEY, David, A. ,  LIU, Jih-Hua

IPC: C07H17/08

CPC classification number: C07H17/08

Abstract: The present invention concerns the novel antibiotic 6-O-methylerythromycin A form 0 solvate of formula (I), a process for its preparation, pharmaceutical compositions comprising this compound and a method of use as a therapeutic agent.

Abstract translation: 本发明涉及式（I）的新型抗生素6-O-甲基红霉素A型0溶剂合物，其制备方法，包含该化合物的药物组合物和用作治疗剂的方法。

公开(公告)号：WO1997019096A3

公开(公告)日：1997-05-29

申请号：PCT/US1996017017

申请日：1996-10-25

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  LIU, Jih-Hua ,  FOSTER, George, A., Jr. ,  MONTGOMERY, Stephen, H.

IPC: C07H17/08

公开(公告)号：WO1997019095A1

公开(公告)日：1997-05-29

申请号：PCT/US1996015772

申请日：1996-10-01

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  LIU, Jih-Hua ,  CELEBUSKI, Joseph, E.

IPC: C07H17/08

CPC classification number: C07H17/08

Abstract: An antibacterial compound is disclosed having formula (II), wherein R1 is loweralkyl or a pharmaceutically acceptable salt, ester or prodrug thereof, processes and intermediates useful in the preparation of the above compounds, as well as compositions containing the same and methods for their use.

Abstract translation: 公开了具有式（II）的抗菌化合物，其中R 1是低级烷基或其药学上可接受的盐，酯或前药，可用于制备上述化合物的方法和中间体，以及含有它们的组合物及其使用方法 。

公开(公告)号：EP0915899B1

公开(公告)日：2004-08-04

申请号：EP97934319.1

申请日：1997-07-28

Applicant: Abbott Laboratories

Inventor： LIU, Jih-Hua ,  RILEY, David, A.

IPC: C07H17/08

CPC classification number: C07H17/08

Abstract: The present invention provides a process for the preparation of 6-O-methylerythromycin A Form II comprising converting erythromycin A to 6-O-methylerythromycin A and treating the 6-O-methylerythromycin A with a number of common organic solvents or mixtures of common organic solvents.

公开(公告)号：EP0874862B1

公开(公告)日：2003-04-09

申请号：EP96936904.0

申请日：1996-10-25

Applicant: ABBOTT LABORATORIES

Inventor： LIU, Jih-Hua ,  FOSTER, George, A., Jr. ,  MONTGOMERY, Stephen, H.

IPC: C07H17/08

CPC classification number: C07H17/08 ,  Y02P20/55

公开(公告)号：EP1042340A1

公开(公告)日：2000-10-11

申请号：EP98958055.0

申请日：1998-11-17

Applicant: Abbott Laboratories

Inventor： MONTGOMERY, Stephen, H. ,  LIU, Jih-Hua

IPC: C07H17/08 ,  A61K31/70

CPC classification number: C07H17/08

Abstract: A process of preparing a 6-O-alkyl derivative of 9-oxime erythromycin B is provided. Intermediates used in the preparation of a 6-O-alkyl 9-oxime erythromycin B are also provided. Pharmaceutical compositions containing a 6-O-alkyl derivative of 9-oxime erythromycin B and the use of those compositions to treat bacterial infections are also provided.

公开(公告)号：EP1036084A1

公开(公告)日：2000-09-20

申请号：EP98959495.7

申请日：1998-11-17

Applicant: ABBOTT LABORATORIES

Inventor： MONTGOMERY, Stephen, H. ,  IVES, Michael, D. ,  LIU, Jih-Hua

IPC: C07H17/08

CPC classification number: C07H17/08 ,  Y02P20/55

Abstract: A process of preparing a 6-O-alkyl derivative of erythromycin C is provided. The process includes the steps of protecting the 2',4'- and 9-oxime hydroxyls with acetyl and ketal protecting groups, alkylating the 6-hydroxyl, removing the protecting groups and deoximating. Intermediates used in the process are also provided.