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公开(公告)号:NO991022D0
公开(公告)日:1999-03-02
申请号:NO991022
申请日:1999-03-02
Applicant: ABBOTT LAB
Inventor: OR YAT SUN , MA ZHENKUN , CLARK RICHARD F , CHU DANIEL T , PLATTNER JACOB J
Abstract: 6-Substituted ketolides of e.g. formula (II) or (III), and their salts, esters and prodrugs are new: Y + Z = X; X = OH, =NOR1 or =NOC(R5)(R6)OR1; or one of Y and Z = H; and the other = H, OH, protected OH or NR7R8; R1 = 1-12C alkyl (optionally substituted), 3-12C cycloalkyl or SiR2R3R4; R2-R4 = 1-12C alkyl or aryl; R5, R6 = H or 1-12C alkyl (optionally substituted), or R5 + R6 = 3-12C cycloalkyl; R7, R8 = H or 1-6C alkyl; or NR7R8 = 3-7 membered ring which, when the ring is 5-7 membered may optionally contain O, NH, N(1-6C alkyl), N(aryl), N(aryl-1-6C alkyl), N (substituted aryl-1-6C alkyl), N(heteroaryl), N(heteroaryl-1-6C alkyl), N(substituted heteroaryl-1-6C alkyl), S or S(O)n; n = 1 or 2; Ra = H or OH; Rc = H or hydroxy protecting group; R9 = 1-6C alkyl (optionally substituted), 3-7C cycloalkyl or optionally substituted aryl or heteroaryl; M = CONH, NHCO, NH, N=, NMe, NHCOO, NHCONH, OCONHY, OCOO, O, S(O)n, COO, OCO or CO; R = methyl (substituted by CN, F, CO2R10, S(O)nR10, NHCOR10, NHCONR11R12, aryl, substituted aryl, heteroaryl or substituted heteroaryl); 2-10C alkyl (optionally substituted), 3C alkenyl (substituted by halo, CHO, CO2R10, COR9, CONR11R12, CN, optionally substituted aryl or heteroaryl, 3-7C cycloalkyl or 1-12C alkyl substituted by heteroaryl); 4-10C alkenyl (optionally substituted), or 3-10C alkynyl optionally substituted); R10 = 1-3C alkyl (optionally aryl substituted), or heteroaryl substituted 1-3C alkyl; R11, R12 = H or 1-3C alkyl (optionally substituted); A, B, D, E = H, 1-6C alkyl (optionally substituted by optionally substituted), 3-7C cycloalkyl, optionally substituted aryl or heteroaryl, heterocycloalkyl or 1-6C alkyl substituted by MR9; provided that \- 2 of A, B, D and E = H; or any one pair of substituents, consisting of AB, AD, AE, BD, BE or DE taken with the atoms to which they are attached, form a 3- to 7-membered ring optionally containing O, NH, N(1-6C alkyl), N(aryl-1-6C alkyl), N(substituted aryl-1-6C alkyl), N(heteroaryl-1-6C alkyl), N(substituted heteroaryl-1-6C alkyl), S, S(O)n, CONH, CONR12, NHCO, NR12CO or C(=NH)NH.
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公开(公告)号:DE69032493T2
公开(公告)日:1999-02-18
申请号:DE69032493
申请日:1990-05-17
Applicant: ABBOTT LAB
Inventor: KEMPF DALE J , NORBECK DANIEL W , ERICKSON JOHN W , CODACOVI LYNN M , SHAM HING LEUNG , PLATTNER JACOB J
IPC: C07D295/18 , A61K31/00 , A61K31/10 , A61K31/12 , A61K31/135 , A61K31/15 , A61K31/165 , A61K31/195 , A61K31/335 , A61K31/40 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/535 , A61K31/54 , A61K38/00 , A61P31/12 , A61P37/04 , C07C31/125 , C07C33/18 , C07C33/26 , C07C33/46 , C07C39/12 , C07C43/164 , C07C43/174 , C07C43/205 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/313 , C07C43/315 , C07C45/00 , C07C45/29 , C07C45/56 , C07C45/59 , C07C45/62 , C07C45/67 , C07C45/74 , C07C49/04 , C07C49/12 , C07C49/17 , C07C49/175 , C07C49/20 , C07C49/215 , C07C49/233 , C07C49/24 , C07C49/255 , C07C53/134 , C07C69/34 , C07C69/65 , C07C69/732 , C07C211/27 , C07C215/06 , C07C215/18 , C07C215/20 , C07C215/28 , C07C217/04 , C07C225/06 , C07C229/08 , C07C229/26 , C07C229/34 , C07C233/35 , C07C233/36 , C07C233/40 , C07C233/78 , C07C235/10 , C07C235/12 , C07C235/34 , C07C235/78 , C07C237/04 , C07C237/10 , C07C237/20 , C07C237/22 , C07C239/08 , C07C239/10 , C07C239/18 , C07C239/20 , C07C247/10 , C07C251/40 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/00 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/05 , C07C311/06 , C07C311/13 , C07C311/18 , C07C317/10 , C07C317/28 , C07C317/44 , C07C323/11 , C07C323/12 , C07C323/25 , C07C323/41 , C07C323/60 , C07C381/00 , C07D207/06 , C07D207/08 , C07D207/12 , C07D207/16 , C07D207/24 , C07D209/42 , C07D211/22 , C07D211/54 , C07D211/62 , C07D211/96 , C07D213/30 , C07D213/40 , C07D213/42 , C07D213/55 , C07D213/56 , C07D213/70 , C07D213/81 , C07D213/82 , C07D215/16 , C07D217/14 , C07D217/16 , C07D217/26 , C07D231/10 , C07D233/60 , C07D233/61 , C07D233/84 , C07D239/38 , C07D263/06 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/36 , C07D277/42 , C07D277/56 , C07D279/12 , C07D295/088 , C07D295/14 , C07D295/15 , C07D295/155 , C07D295/185 , C07D295/20 , C07D295/205 , C07D295/215 , C07D295/22 , C07D295/26 , C07D303/04 , C07D303/22 , C07D303/36 , C07D303/48 , C07D305/14 , C07D307/42 , C07D317/12 , C07D413/12 , C07D417/12 , C07D487/04 , C07D521/00 , C07F7/02 , C07F9/30 , C07F9/32 , C07F9/53 , C07K5/02 , C07K5/04 , C07K5/06 , C07K5/062 , C07K5/078 , C07D211/44 , C07D215/14 , C07D211/34 , C07D215/18 , C07D295/145 , C07D303/23
Abstract: A retroviral protease inhibiting compound of the formula A - X - B or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein X is a linking group; A is (1) substituted amino, (2) substituted carbonyl, (3) functionalized imino, (4) functionalized alkyl, (5) functionalized acyl, (6) functionalized heterocyclic or (7) functionalized (heterocyclic)alkyl; and B is (1) substituted carbonyl independently defined as herein, (2) substituted amino independently defined as herein, (3) functionalized imino independently defined as herein, (4) functionalized alkyl independently defined as herein, (5) functionalized acyl independently defined as herein, (6) functionalized heterocyclic independently defined as herein or (7) functionalized (heterocyclic)alkyl independently defined as herein. o
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公开(公告)号:DE69032493D1
公开(公告)日:1998-08-27
申请号:DE69032493
申请日:1990-05-17
Applicant: ABBOTT LAB
Inventor: KEMPF DALE J , NORBECK DANIEL W , ERICKSON JOHN W , CODACOVI LYNN M , SHAM HING LEUNG , PLATTNER JACOB J
IPC: C07D295/18 , A61K31/00 , A61K31/10 , A61K31/12 , A61K31/135 , A61K31/15 , A61K31/165 , A61K31/195 , A61K31/335 , A61K31/40 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/535 , A61K31/54 , A61K38/00 , A61P31/12 , A61P37/04 , C07C31/125 , C07C33/18 , C07C33/26 , C07C33/46 , C07C39/12 , C07C43/164 , C07C43/174 , C07C43/205 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/313 , C07C43/315 , C07C45/00 , C07C45/29 , C07C45/56 , C07C45/59 , C07C45/62 , C07C45/67 , C07C45/74 , C07C49/04 , C07C49/12 , C07C49/17 , C07C49/175 , C07C49/20 , C07C49/215 , C07C49/233 , C07C49/24 , C07C49/255 , C07C53/134 , C07C69/34 , C07C69/65 , C07C69/732 , C07C211/27 , C07C215/06 , C07C215/18 , C07C215/20 , C07C215/28 , C07C217/04 , C07C225/06 , C07C229/08 , C07C229/26 , C07C229/34 , C07C233/35 , C07C233/36 , C07C233/40 , C07C233/78 , C07C235/10 , C07C235/12 , C07C235/34 , C07C235/78 , C07C237/04 , C07C237/10 , C07C237/20 , C07C237/22 , C07C239/08 , C07C239/10 , C07C239/18 , C07C239/20 , C07C247/10 , C07C251/40 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/00 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/05 , C07C311/06 , C07C311/13 , C07C311/18 , C07C317/10 , C07C317/28 , C07C317/44 , C07C323/11 , C07C323/12 , C07C323/25 , C07C323/41 , C07C323/60 , C07C381/00 , C07D207/06 , C07D207/08 , C07D207/12 , C07D207/16 , C07D207/24 , C07D209/42 , C07D211/22 , C07D211/54 , C07D211/62 , C07D211/96 , C07D213/30 , C07D213/40 , C07D213/42 , C07D213/55 , C07D213/56 , C07D213/70 , C07D213/81 , C07D213/82 , C07D215/16 , C07D217/14 , C07D217/16 , C07D217/26 , C07D231/10 , C07D233/60 , C07D233/61 , C07D233/84 , C07D239/38 , C07D263/06 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/36 , C07D277/42 , C07D277/56 , C07D279/12 , C07D295/088 , C07D295/14 , C07D295/15 , C07D295/155 , C07D295/185 , C07D295/20 , C07D295/205 , C07D295/215 , C07D295/22 , C07D295/26 , C07D303/04 , C07D303/22 , C07D303/36 , C07D303/48 , C07D305/14 , C07D307/42 , C07D317/12 , C07D413/12 , C07D417/12 , C07D487/04 , C07D521/00 , C07F7/02 , C07F9/30 , C07F9/32 , C07F9/53 , C07K5/02 , C07K5/04 , C07K5/06 , C07K5/062 , C07K5/078 , C07D211/44 , C07D215/14 , C07D211/34 , C07D215/18 , C07D295/145 , C07D303/23
Abstract: A retroviral protease inhibiting compound of the formula A - X - B or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein X is a linking group; A is (1) substituted amino, (2) substituted carbonyl, (3) functionalized imino, (4) functionalized alkyl, (5) functionalized acyl, (6) functionalized heterocyclic or (7) functionalized (heterocyclic)alkyl; and B is (1) substituted carbonyl independently defined as herein, (2) substituted amino independently defined as herein, (3) functionalized imino independently defined as herein, (4) functionalized alkyl independently defined as herein, (5) functionalized acyl independently defined as herein, (6) functionalized heterocyclic independently defined as herein or (7) functionalized (heterocyclic)alkyl independently defined as herein. o
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公开(公告)号:CH689001A5
公开(公告)日:1998-07-15
申请号:CH233897
申请日:1991-11-19
Applicant: ABBOTT LAB
Inventor: WITTENBERGER STEVEN J , KEMPF DALE J , NORBECK DANIEL W , ZHAO CHEN , SOWIN THOMAS J , PLATTNER JACOB J , LYNN CODACONI M , HING LEUNG SHAM
IPC: A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/435 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/444 , A61K38/00 , A61P31/12 , A61P31/18 , A61P43/00 , C07C53/134 , C07C211/00 , C07C215/18 , C07C215/20 , C07C215/28 , C07C215/30 , C07C215/80 , C07C219/18 , C07C233/40 , C07C237/10 , C07C237/22 , C07C269/04 , C07C271/02 , C07C271/16 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/24 , C07D20060101 , C07D213/00 , C07D213/26 , C07D213/30 , C07D213/34 , C07D213/36 , C07D213/40 , C07D213/54 , C07D213/56 , C07D213/61 , C07D213/75 , C07D213/79 , C07D215/20 , C07D233/54 , C07D233/84 , C07D235/14 , C07D235/16 , C07D237/10 , C07D239/26 , C07D241/12 , C07D261/08 , C07D261/12 , C07D263/20 , C07D263/32 , C07D277/20 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/32 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/56 , C07D295/02 , C07D295/13 , C07D295/205 , C07D295/215 , C07D303/36 , C07D307/34 , C07D307/42 , C07D307/66 , C07D333/16 , C07D333/36 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D521/00 , C07K1/113 , C07K5/06 , C07K5/065 , C07K5/08 , C07K14/81
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公开(公告)号:AU689809B2
公开(公告)日:1998-04-09
申请号:AU7925894
申请日:1994-09-30
Applicant: ABBOTT LAB
Inventor: CHU DANIEL T , LI QUN , COOPER CURT S , FUNG ANTHONY K L , LEE CHEUK M , PLATTNER JACOB J
IPC: C07D491/052 , A61K31/40 , A61K31/435 , A61K31/495 , A61K31/54 , A61K38/00 , A61P31/04 , C07D213/61 , C07D213/68 , C07D455/02 , C07D471/04 , C07D491/107 , C07D491/113 , C07D491/16 , C07D519/00 , C07K5/06 , A61K31/535
Abstract: Antibacterical coumpounds having formula (I) and the pharmaceutically acceptable salts, esters and amides thereof, preferred examples of which include those coumpounds wherein R is cycloalkyl of from three to eight carbon atoms or substituted phenyl; R is selected from the group consisting of (a) halogen, (b) loweralkyl, (c) loweralkenyl, (d) cycloalkyl of from three to eight carbons, (e) cycloalkenyl of from four to eight carbons, (f) loweralkoxy, (g) aryloxy, (h) aryl(loweralkyl)oxy, (i) aryl(loweralkyl), (j) cycloalkyl(loweralkyl), (k) amino, (l) (loweralkyl)amino, (m) aryl(loweralkyl)amino, (n) hydroxy substituted (loweralkyl)amino, (o) phenyl, (p) substituted phenyl, (q) bicyclic nitrogen-containing heterocycle, (r) nitrogen-containingaromatic heterocycle, and (s) nitrogen-containing heterocycle having formula (Ia) where x is between zero and three; R is halogen; R is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group; R is hydrogen, loweralkyl, halo(loweralkyl), or -NR R ; and R is loweralkyl, as wellas pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.
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公开(公告)号:CA2263972A1
公开(公告)日:1998-03-12
申请号:CA2263972
申请日:1997-09-02
Applicant: ABBOTT LAB
Inventor: CHU DANIEL T , OR YAT SUN , CLARK RICHARD F , MA ZHENKUN , PLATTNER JACOB J , GRIESGRABER GEORGE
IPC: A61K31/70 , A61K31/7048 , A61P31/04 , C07H17/00 , C07H17/08
Abstract: Antimicrobial compounds having formula (II), (III), (IV), (IV-A) or (V) as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compunds.
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公开(公告)号:BR9407806A
公开(公告)日:1997-08-19
申请号:BR9407806
申请日:1994-09-30
Applicant: ABBOTT LAB
Inventor: CHU DANIEL T , LI QUN , COOPER CURT S , FUNG ANTHONY K L , LEE CHEUK M , PLATTNER JACOB J
IPC: C07D491/052 , A61K31/40 , A61K31/435 , A61K31/495 , A61K31/54 , A61K38/00 , A61P31/04 , C07D213/61 , C07D213/68 , C07D455/02 , C07D471/04 , C07D491/107 , C07D491/113 , C07D491/16 , C07D519/00 , C07K5/06 , A61K31/535
Abstract: Antibacterical coumpounds having formula (I) and the pharmaceutically acceptable salts, esters and amides thereof, preferred examples of which include those coumpounds wherein R is cycloalkyl of from three to eight carbon atoms or substituted phenyl; R is selected from the group consisting of (a) halogen, (b) loweralkyl, (c) loweralkenyl, (d) cycloalkyl of from three to eight carbons, (e) cycloalkenyl of from four to eight carbons, (f) loweralkoxy, (g) aryloxy, (h) aryl(loweralkyl)oxy, (i) aryl(loweralkyl), (j) cycloalkyl(loweralkyl), (k) amino, (l) (loweralkyl)amino, (m) aryl(loweralkyl)amino, (n) hydroxy substituted (loweralkyl)amino, (o) phenyl, (p) substituted phenyl, (q) bicyclic nitrogen-containing heterocycle, (r) nitrogen-containingaromatic heterocycle, and (s) nitrogen-containing heterocycle having formula (Ia) where x is between zero and three; R is halogen; R is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group; R is hydrogen, loweralkyl, halo(loweralkyl), or -NR R ; and R is loweralkyl, as wellas pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.
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公开(公告)号:AU6153096A
公开(公告)日:1996-12-24
申请号:AU6153096
申请日:1996-06-05
Applicant: ABBOTT LAB
Inventor: CHU DANIEL T , LI QUN , COOPER CURT S , FUNG ANTHONY K L , LEE CHEUK M , PLATTNER JACOB J , MA ZHENKUN , WANG WEI-BO
IPC: A61K31/00 , A61K31/44 , A61K31/505 , A61K31/519 , A61K31/529 , A61K38/00 , A61P31/00 , A61P31/04 , C07D213/61 , C07D213/68 , C07D455/02 , C07D471/04 , C07D491/16 , C07D495/16 , C07D519/00 , C07K5/06 , A61K31/435
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公开(公告)号:AT131809T
公开(公告)日:1996-01-15
申请号:AT90119985
申请日:1990-10-18
Applicant: ABBOTT LAB
Inventor: CHU DANIEL T , PLATTNER JACOB J , KLEIN LARRY L , SHEN LINUS L
IPC: A61K31/47 , A61K31/495 , A61K31/535 , A61K31/54 , A61K31/55 , A61P35/00 , C07C333/06 , C07D513/04 , C07D513/14 , C07D519/00 , A61K31/435 , C07D275/00 , C07D221/00
Abstract: Isothiazolo-quinoline derivatives of the formula I which may exist as tautomers (formula II) are described which are cytotoxic for various tumor cell lines and are useful in the treatment of neoplastic diseases. wherein R is selected from (a) lower alkyl, (b) haloalkyl, (c) lowercycloalkyl, (d) alkylamino, (e) an aromatic heterocyclic group and (f) a phenyl group; W, X and Z are independently selected from hydrogen, halogen and lower alkyl; and Y is selected from a (a) phenyl group, (b) -NR2R3, (c) a bicyclic N-containing heterocyclic group, and (d) -OR10, wherein R10 is hydrogen, lower alkyl or a phenyl group; or any two of W, X, Y and Z taken together form a fused, substituted or unsubstituted, aromatic group or heterocyclic group.
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公开(公告)号:AT120370T
公开(公告)日:1995-04-15
申请号:AT88116399
申请日:1988-10-04
Applicant: ABBOTT LAB
Inventor: STEIN HERMAN H , CROWLEY STEVEN R , PLATTNER JACOB J
IPC: A61K31/16 , A61K31/21 , A61K31/215 , A61K31/255 , A61K31/265 , A61K31/42 , A61K31/421 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K38/55 , A61P27/02 , A61P27/06 , A61P43/00 , C07C233/16 , C07C235/08 , C07C237/08 , C07C271/22 , C07C271/34 , C07C305/04 , C07C307/06 , C07C309/64 , C07C317/28 , C07C317/44 , C07C323/52 , C07C323/60 , C07C323/64 , C07D211/44 , C07D211/46 , C07D211/74 , C07D233/64 , C07D263/22 , C07D263/24 , C07D295/20 , C07D405/12 , C07D413/06 , A61K38/07
Abstract: A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula: wherein A is a substituent; W is CO or CHOH and U is CH2 or NR2 wherein R2 is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is CH2; R1 is loweralkyl, cycloalkyl, benzyl, (alpha,alpha)-dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, 1-benzyloxyethyl, phenoxy, thiophenoxy or anilino; R3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)alkyl, carboxyalkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R4 is a substituted amino group; or pharmaceutically acceptable salts or esters thereof. Also disclosed are compositions, methods and kits for treating glaucoma or reducing and/or controlling intraocular pressure wherein the renin inhibiting compound is administered in combination with a beta-adrenergic antagonist, a steroidal antiinflammatory agent or an angiotensin converting enzyme inhibiting compound.
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