公开(公告)号：WO1996017862A1

公开(公告)日：1996-06-13

申请号：PCT/US1995014488

申请日：1995-11-08

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  SWENSON, Rolf, E. ,  HAVIV, Fortuna ,  MORT, Nicholas, A.

IPC: C07K07/23

CPC classification number: C07K7/23 ,  A61K38/00 ,  Y10S930/13

Abstract: Peptides possessing LHRH antagonistic activity, and useful for controlling the release of LHRH in mammals are decapeptide analogues of LHRH having a lactam group at the N-terminus of formula (I), where n is 1, 2, or 3 and R is selected from the group consisting of hydrogen, benzyl, 4-chlorobenzyl, 2-methylnaphth-1-yl, 1-methylnaphth-2-yl, and quinolin-3-ylmethyl.

Abstract translation: 具有LHRH拮抗活性并且可用于控制哺乳动物中LHRH释放的肽是在式（I）的N末端具有内酰胺基的LHRH的十肽类似物，其中n为1,2或3，R 1为 选自氢，苄基，4-氯苄基，2-甲基萘-1-基，1-甲基萘-2-基和喹啉-3-基甲基。

公开(公告)号：WO1995004540A1

公开(公告)日：1995-02-16

申请号：PCT/US1994008577

申请日：1994-07-29

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  HAVIV, Fortuna ,  FITZPATRICK, Timothy, D. ,  SWENSON, Rolf, E. ,  NICHOLS, Charles, J. ,  MORT, Nicholas, A.

IPC: A61K37/00

CPC classification number: C07K7/23 ,  A61K38/00

Abstract: Decapeptides substituted on the N-terminal nitrogen atom by acyl groups are potent antagonists of LHRH and are useful for suppressing the levels of sex hormones in mammals.

Abstract translation: 在N-末端氮原子上被酰基取代的十肽是LHRH的有效拮抗剂，可用于抑制哺乳动物中的性激素水平。

公开(公告)号：WO1995004541A1

公开(公告)日：1995-02-16

申请号：PCT/US1994008678

申请日：1994-07-29

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  HAVIV, Fortuna ,  FITZPATRICK, Timothy, D. ,  SWENSON, Rolf, E. ,  NICHOLS, Charles, J. ,  MORT, Nicholas, A.

IPC: A61K37/00

CPC classification number: C07K7/23 ,  A61K38/00

Abstract: Decapeptide and undecapeptides substituted on the N-terminal nitrogen atom by acyl groups which include furo-2-yl, isonicotinyl, nicotinyl, 2-, 3-, and 4-quinolinecarbonyl, shikimyl, dihydroshikimyl, and tetrahydrofur-2-oyl are potent antagonists of LHRH and are useful for hormones the levels of sex hormones in mammals.

Abstract translation: 通过包括呋喃-2-基，异烟酰基，烟酰基，2-，3-和4-喹啉羰基，莽草酰基，二氢嘧啶基和四氢呋喃-2-基的酰基在N-末端氮原子上取代的十肽和十一肽是有效的拮抗剂 的LHRH，可用于激素，哺乳动物性激素水平。

公开(公告)号：EP1066304A1

公开(公告)日：2001-01-10

申请号：EP99912259.1

申请日：1999-03-11

Applicant: ABBOTT LABORATORIES

Inventor： SAUER, Daryl, R. ,  HAVIV, Fortuna ,  RANDOLPH, John ,  MORT, Nicholas, A. ,  DALTON, Christopher, R. ,  BRUNCKO, Milan ,  KAMINSKI, Michele, A. ,  CRAWFORD, Bradley, W. ,  FREY, Lisa, Marie ,  GREER, Jonathon

IPC: C07H1/00

CPC classification number: C07H17/08

Abstract: Disclosed are 3'-N-desmethyl-3'-N-susbstituted-6-O-methyl-11-deoxy-11, 12-cyclic carbamate erythromycin A derivatives which are antagonists of lutenizing hormone-releasing hormone (LHRH). Also disclosed are pharmaceutical compositions comprising the compounds, to methods of using the compounds and to the process of making the same.

公开(公告)号：EP1181296A1

公开(公告)日：2002-02-27

申请号：EP99931986.6

申请日：1999-06-28

Applicant: ABBOTT LABORATORIES

Inventor： ARENDSEN, David, L. ,  BHATIA, Pramila ,  BOYD, Steven, A. ,  CONDROSKI, Kevin, R. ,  FREEMAN, Jennifer, C. ,  GUNAWARDANA, Indrani, W. ,  LARTEY, Kraig ,  MCCARTY, Catherine, M. ,  MORT, Nicholas, A. ,  PATEL, Meena V. ,  STAEGER, Michael, A. ,  STEWART, Andrew, O. ,  STOUT, David, M. ,  ZHU, Gui-Dong

IPC: C07D495/04

CPC classification number: C07D471/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

Abstract: Compounds having formula (I) are useful for treating inflammation. Also disclosed are pharmaceutical compositions comprising compounds of formula (I), and methods of inhibiting/treating inflammatory diseases in a mammal.

Abstract translation: 具有式（I）的化合物可用于治疗炎症。 还公开了包含式（I）化合物的药物组合物，以及在哺乳动物中抑制/治疗炎性疾病的方法。

公开(公告)号：EP1066304B1

公开(公告)日：2005-02-23

申请号：EP99912259.1

申请日：1999-03-11

Applicant: Abbott Laboratories

Inventor： SAUER, Daryl, R. ,  HAVIV, Fortuna ,  RANDOLPH, John ,  MORT, Nicholas, A. ,  DALTON, Christopher, R. ,  BRUNCKO, Milan ,  KAMINSKI, Michele, A. ,  CRAWFORD, Bradley, W. ,  FREY, Lisa, Marie ,  GREER, Jonathon

IPC: C07H17/08 ,  A61K31/70

CPC classification number: C07H17/08

Abstract: Disclosed are 3'-N-desmethyl-3'-N-susbstituted-6-O-methyl-11-deoxy-11, 12-cyclic carbamate erythromycin A derivatives which are antagonists of lutenizing hormone-releasing hormone (LHRH). Also disclosed are pharmaceutical compositions comprising the compounds, to methods of using the compounds and to the process of making the same.

公开(公告)号：EP1090009A2

公开(公告)日：2001-04-11

申请号：EP99926157.1

申请日：1999-06-03

Applicant: ABBOTT LABORATORIES

Inventor： STEWART, Andrew, O. ,  BOYD, Steven, A. ,  ARENDSEN, David, L. ,  BHATIA, Pramila ,  CONDROSKI, Kevin, R. ,  FREEMAN, Jennifer, C. ,  GUNAWARDANA, Indrani, W. ,  ZHU, Gui-Dong ,  LARTEY, Kraig ,  MCCARTY, Catherine, M. ,  MORT, Nicholas, A. ,  PATEL, Meena V. ,  STAEGER, Michael, A. ,  STOUT, David, M.

IPC: C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D471/04 ,  C07D491/04 ,  A61K31/44 ,  A61K31/50 ,  A61K31/505

CPC classification number: C07D471/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

Abstract: Compounds having Formula (I) are useful for treating inflammation. Also disclosed are pharmaceutical compositions comprising compouns of Formula (I), and methods of inhibiting/treating inflammatory diseases in a mammal.

Abstract translation: 具有式（I）的化合物可用于治疗炎症。 还公开了包含式（I）化合物的药物组合物，以及在哺乳动物中抑制/治疗炎性疾病的方法。

公开(公告)号：EP1066307A1

公开(公告)日：2001-01-10

申请号：EP99914036.1

申请日：1999-03-22

Applicant: ABBOTT LABORATORIES

Inventor： SAUER, Daryl, R. ,  HAVIV, Fortuna ,  RANDOLPH, John ,  MORT, Nicholas, A. ,  DALTON, Christopher, R. ,  BRUNCKO, Milan ,  KAMINSKI, Michele, A. ,  CRAWFORD, Bradley, W. ,  FREY, Lisa, Marie ,  GREER, Jonathon

IPC: C07H17/08 ,  A61K31/70

CPC classification number: C07H17/08

Abstract: Disclosed are 3',3'-N-bisdesmethyl-3',3'-N-bis-substituted-6-O-methyl-11-deoxy-11,12-cyclic carbamate erythromycin A derivatives of formula (I) which are antagonists of lutenizing hormone-releasing hormone (LHRH). Also disclosed are pharmaceutical compositions comprising the compounds, methods of using the compounds and the process of making the same.