公开(公告)号：WO9950275A3

公开(公告)日：2001-02-22

申请号：PCT/US9904658

申请日：1999-03-11

Applicant: ABBOTT LAB

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: A61K31/7042 ,  A61K31/7048 ,  A61K31/7056 ,  A61P5/24 ,  A61P13/08 ,  A61P15/00 ,  A61P35/00 ,  A61P43/00 ,  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.

Abstract translation: 公开了作为促黄体激素释放激素（LHRH）的拮抗剂的3'-N-去甲基-3'-N-疑似取代的-6-O-甲基-11-脱氧-11,12-环状氨基甲酸酯红霉素A衍生物。 还公开了包含该化合物的药物组合物，使用该化合物的方法及其制备方法。

公开(公告)号：BG104844A

公开(公告)日：2001-07-31

申请号：BG10484400

申请日：2000-10-11

Applicant: ABBOTT LAB

Inventor： SAUER DARYL R ,  HAVIV FORTUNA ,  RANDOLPH JOHN ,  MORT NICHOLAS A ,  DALTON CHRISTOPHER R ,  BRUNCKO MILAN ,  KAMINSKI MICHELE A ,  CRAWFORD BRADLEY W ,  FREY LISA M ,  GREER JONATHON

IPC: A61K31/7042 ,  A61K31/7048 ,  A61K31/7056 ,  A61P5/24 ,  A61P13/08 ,  A61P15/00 ,  A61P35/00 ,  A61P43/00 ,  C07H17/08 ,  C07H1/00

Abstract: Disclosed are 3'-N-desmethyl-3'-N-substituted-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. 15 claims

公开(公告)号：SK13972000A3

公开(公告)日：2001-07-10

申请号：SK13972000

申请日：1999-03-11

Applicant: ABBOTT LAB

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 JONATHAN

IPC: A61K31/7042 ,  A61K31/7048 ,  A61K31/7056 ,  A61P5/24 ,  A61P13/08 ,  A61P15/00 ,  A61P35/00 ,  A61P43/00 ,  C07H17/08 ,  A61K31/70 ,  C07H1/00

Abstract: Disclosed are 3'-N-desmethyl-3'-N-substituted-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：CA2407043C

公开(公告)日：2010-02-16

申请号：CA2407043

申请日：2001-04-25

Applicant: ABBOTT LAB

Inventor： BRUNCKO MILAN ,  DALTON CHRISTOPHER R ,  GIRANDA VINCENT L ,  GONG JIANCHUN ,  MCCLELLAN WILLIAM J ,  NIENABER VICKI L ,  ROCKWAY TODD W ,  SAUER DARYL R ,  WEITZBERG MOSHE

IPC: C07D217/02 ,  A61K31/472 ,  A61K31/4725 ,  A61P9/00 ,  A61P15/16 ,  A61P15/18 ,  A61P19/02 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D217/04 ,  C07D217/06 ,  C07D217/26 ,  C07D401/06 ,  C07D405/04 ,  C07D405/10

Abstract: Compounds having formula (I) are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions, methods for the preparation of urokinase-inhibitors, and a method of inhibiting urokinase in a mammal.

公开(公告)号：ES2238828T3

公开(公告)日：2005-09-01

申请号：ES99912259

申请日：1999-03-11

Applicant: ABBOTT LAB

Inventor： SAUER DARYL R ,  HAVIV FORTUNA ,  RANDOLPH JOHN ,  MORT NICHOLAS A ,  DALTON CHRISTOPHER R ,  BRUNCKO MILAN

IPC: A61K31/7042 ,  A61K31/7048 ,  A61K31/7056 ,  A61P5/24 ,  A61P13/08 ,  A61P15/00 ,  A61P35/00 ,  A61P43/00 ,  C07H17/08 ,  A61K31/70

Abstract: Un compuesto representado por la fórmula: o una sal farmacéuticamente aceptable o éster del mismo, donde A se selecciona entre el grupo compuesto por: (a) -C, (b) -N, y (c) -O; X e Y se seleccionan independientemente en cada aparición entre el grupo compuesto por: (a) hidrógeno, (b) haluro, (c) trifluorometilo, (d) alcoxi, (e) alquilo, (f) arilo, y (g) arilo sustituido; R se selecciona entre el grupo compuesto por: (a) alquilo, (b) cicloalquilo, (c) cicloalquilo sustituido, (d) heterociclilo, (e) heterociclilo sustituido, (f) cicloalquilalquilo, (g) cicloalquilalquilo sustituido, (h) alquilarilo, (i) alquilheterociclilo, (j) alquenilo, (k) alquinilo, (l) -C(S)-NHR4, C(NR4)-NHR4, donde R4 es hidrógeno, alquilo, o arilo; y (m) -(CH2)n-C(CH2)m-R5, donde m es 2, 3, 4, o 5, y R5 es alquilo, alcoxi, arilo, o arilo sustituido; R2 y R3 son independientemente en cada aparición (a) hidrógeno, (b) metilo, o R2 y R3 juntos forman un resto cíclico, cuando A es C; R3 está ausente cuando A es N; R2 y R3 están ausentes cuando A es O; y n = 1, 2 o 3; o donde R es alquilo, alquenilo cicloalquilo, heterociclilo, (heterociclil)alquilo o cicloalquilalquilo; X e Y son independientemente en cada aparición cloro, flúor, dioxolano, hidrógeno o alcoxi, A es -C o N; R2 y R3 son independientemente en cada aparición hidrógeno o juntos forman un resto ciclopropilo y n es 1; con la condición de que se excluye el compuesto, en el que R es metilo, A es C, n es 3, R2 y R3 son H y X e Y son H.

公开(公告)号：AT289609T

公开(公告)日：2005-03-15

申请号：AT99912259

申请日：1999-03-11

Applicant: ABBOTT LAB

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: A61K31/7042 ,  A61K31/7048 ,  A61K31/7056 ,  A61P5/24 ,  A61P13/08 ,  A61P15/00 ,  A61P35/00 ,  A61P43/00 ,  C07H17/08 ,  A61K31/70

Abstract: Disclosed are 3'-N-desmethyl-3'-N-substituted-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：HU0102011A2

公开(公告)日：2001-11-28

申请号：HU0102011

申请日：1999-03-11

Applicant: ABBOTT LAB

Inventor： BRUNCKO MILAN ,  CRAWFORD BRADLEY W ,  DALTON CHRISTOPHER R ,  FREY LISA MARIE ,  GREER JONATHAN ,  HAVIV FORTUNA ,  KAMINSKI MICHELE A ,  MORT NICHOLAS A ,  RANDOLPH JOHN ,  SAUER DARYL R

IPC: A61K31/7042 ,  A61K31/7048 ,  A61K31/7056 ,  A61P5/24 ,  A61P13/08 ,  A61P15/00 ,  A61P35/00 ,  A61P43/00 ,  C07H17/08 ,  C07H1/00

Abstract: Disclosed are 3'-N-desmethyl-3'-N-substituted-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：SK13982000A3

公开(公告)日：2001-04-09

申请号：SK13982000

申请日：1999-03-22

Applicant: ABBOTT LAB

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 JONATHAN

IPC: A61K31/7042 ,  A61K31/7048 ,  A61P5/00 ,  A61P15/00 ,  A61P43/00 ,  C07H17/08 ,  A61K31/70

Abstract: Disclosed are 3',3'-N-bisdesmethyl-3',3'-N-bis-substituted-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：CA2325519A1

公开(公告)日：1999-10-07

申请号：CA2325519

申请日：1999-03-22

Applicant: ABBOTT LAB

Inventor： CRAWFORD BRADLEY W ,  KAMINSKI MICHELE A ,  FREY LISA MARIE ,  BRUNCKO MILAN ,  SAUER DARYL R ,  GREER JONATHON ,  HAVIV FORTUNA ,  RANDOLPH JOHN ,  MORT NICHOLAS A ,  DALTON CHRISTOPHER R

IPC: A61K31/7042 ,  A61K31/7048 ,  A61P5/00 ,  A61P15/00 ,  A61P43/00 ,  C07H17/08 ,  A61K31/70

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.

公开(公告)号：AT319689T

公开(公告)日：2006-03-15

申请号：AT01934906

申请日：2001-04-25

Applicant: ABBOTT LAB

Inventor： BRUNCKO MILAN ,  DALTON CHRISTOPHER R ,  GIRANDA VINCENT L ,  GONG JIANCHUN ,  MCCLELLAN WILLIAM J ,  NIENABER VICKI L ,  ROCKWAY TODD W ,  SAUER DARYL R ,  WEITZBERG MOSHE

IPC: A61K31/472 ,  A61K31/4725 ,  A61P9/00 ,  A61P15/16 ,  A61P15/18 ,  A61P19/02 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D217/02 ,  C07D217/04 ,  C07D217/06 ,  C07D217/26 ,  C07D401/06 ,  C07D405/04 ,  C07D405/10