公开(公告)号：DE69733422T2

公开(公告)日：2006-05-04

申请号：DE69733422

申请日：1997-09-02

Applicant: ABBOTT LAB

Inventor： OR SUN ,  MA ZHENKUN ,  CLARK F ,  CHU T ,  PLATTNER J

IPC: C07H17/08 ,  A61K31/70 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/00

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.

公开(公告)号：DE69733422D1

公开(公告)日：2005-07-07

申请号：DE69733422

申请日：1997-09-02

Applicant: ABBOTT LAB

Inventor： OR SUN ,  MA ZHENKUN ,  CLARK F ,  CHU T ,  PLATTNER J

IPC: A61K31/70 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/00 ,  C07H17/08

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.

公开(公告)号：SE8000843L

公开(公告)日：1980-08-06

申请号：SE8000843

申请日：1980-02-01

Applicant: ABBOTT LAB

Inventor： VOSS H F ,  PLATTNER J ,  HERRIN T R

IPC: C07F9/40 ,  C12Q1/46 ,  G01N33/532 ,  G01N33/542 ,  G01N33/54

Abstract: The present invention encompasses a method for determining ligands in test samples comprising intermixing with the test sample a ligand analog-irreversible enzyme inhibitor conjugate and a binding protein bindable to the ligand and the ligand analog-irreversible enzyme inhibitor conjugate and wherein the amount of ligand analog-irreversible enzyme inhibitor conjugate bound by the binding protein is related to the amount of ligand in the test sample, said binding protein inactivating the irreversible enzyme inhibitor when bound to the ligand analog portion of the conjugate; intermixing an enzyme which is irreversibly inhibited by the ligand analog-irreversible enzyme inhibitor conjugate unbound by the binding protein; and intermixing substrate to the enzyme and monitoring the enzyme substrate reaction. The invention also includes ligand analog-irreversible enzyme inhibitor conjugates useful as reagents in practicing the method. Methods and reagents of the present are particularly useful in determining drugs, hormones, and the like in biological fluids.

公开(公告)号：ZA8000371B

公开(公告)日：1981-03-25

申请号：ZA8000371

申请日：1980-01-22

Applicant: ABBOTT LAB

Inventor： HERRIN T ,  VOSS H ,  PLATTNER J

IPC: C07F9/40 ,  C12Q1/46 ,  G01N33/532 ,  G01N33/542 ,  G01N

CPC classification number: G01N33/542 ,  C07F9/4075 ,  G01N33/532 ,  Y10S435/81 ,  Y10S435/962 ,  Y10S436/825

公开(公告)号：DE69723848T2

公开(公告)日：2004-07-01

申请号：DE69723848

申请日：1997-04-25

Applicant: ABBOTT LAB

Inventor： ELLIOTT L ,  OR SUN ,  CHU T ,  GRIESGRABER W ,  PLATTNER J ,  PIREH DAISY

IPC: A61K31/04 ,  A61K31/70 ,  A61K31/7048 ,  A61K31/7052 ,  C07H17/08

Abstract: Novel 3-descladinose-2,3-anhydroerythromycin compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity selected from the group consisting of: (a) (I), (b) (II), (c) (III), and (d) (IV), pharmaceutical compositions comprising a therapeutically effective amount of a compound of formulas (I)-(IV) of the invention in combination with a pharmaceutically acceptable carrier, as well as a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of formulas (I)-(IV) of the invention.

公开(公告)号：DE69821009D1

公开(公告)日：2004-02-12

申请号：DE69821009

申请日：1998-09-01

Applicant: ABBOTT LAB

Inventor： OR SUN ,  CLARK F ,  CHU T ,  PLATTNER J

IPC: A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08 ,  A61K31/70

Abstract: Novel multicyclic erythromycin compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity having a formula (I) (II), (III), compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier, as well as a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention.

公开(公告)号：DE69723848D1

公开(公告)日：2003-09-04

申请号：DE69723848

申请日：1997-04-25

Applicant: ABBOTT LAB

Inventor： ELLIOTT L ,  OR SUN ,  CHU T ,  GRIESGRABER W ,  PLATTNER J ,  PIREH DAISY

IPC: A61K31/04 ,  A61K31/70 ,  A61K31/7048 ,  A61K31/7052 ,  C07H17/08

Abstract: Novel 3-descladinose-2,3-anhydroerythromycin compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity selected from the group consisting of: (a) (I), (b) (II), (c) (III), and (d) (IV), pharmaceutical compositions comprising a therapeutically effective amount of a compound of formulas (I)-(IV) of the invention in combination with a pharmaceutically acceptable carrier, as well as a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of formulas (I)-(IV) of the invention.

公开(公告)号：SE448259B

公开(公告)日：1987-02-02

申请号：SE8000843

申请日：1980-02-01

Applicant: ABBOTT LAB

Inventor： VOSS H F ,  PLATTNER J ,  HERRIN T R

IPC: C07F9/40 ,  C12Q1/46 ,  G01N33/532 ,  G01N33/542

Abstract: The present invention encompasses a method for determining ligands in test samples comprising intermixing with the test sample a ligand analog-irreversible enzyme inhibitor conjugate and a binding protein bindable to the ligand and the ligand analog-irreversible enzyme inhibitor conjugate and wherein the amount of ligand analog-irreversible enzyme inhibitor conjugate bound by the binding protein is related to the amount of ligand in the test sample, said binding protein inactivating the irreversible enzyme inhibitor when bound to the ligand analog portion of the conjugate; intermixing an enzyme which is irreversibly inhibited by the ligand analog-irreversible enzyme inhibitor conjugate unbound by the binding protein; and intermixing substrate to the enzyme and monitoring the enzyme substrate reaction. The invention also includes ligand analog-irreversible enzyme inhibitor conjugates useful as reagents in practicing the method. Methods and reagents of the present are particularly useful in determining drugs, hormones, and the like in biological fluids.

公开(公告)号：DE69830739T2

公开(公告)日：2006-04-20

申请号：DE69830739

申请日：1998-10-29

Applicant: ABBOTT LAB

Inventor： PHAN TAM ,  OR SUN ,  CHU T ,  PLATTNER J ,  CHEN YAN ,  CLARK F

IPC: C07H17/08 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04

Abstract: Novel 2-halo-6-O-substituted ketolide derivatives and pharmaceutically acceptable salts and esters thereof having antibacterial activity having formula (I) or (II), compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier, a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention, and processes for their preparation.

公开(公告)号：DE69830739D1

公开(公告)日：2005-08-04

申请号：DE69830739

申请日：1998-10-29

Applicant: ABBOTT LAB

Inventor： PHAN TAM ,  OR SUN ,  CHU T ,  PLATTNER J ,  CHEN YAN ,  CLARK F

IPC: A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08 ,  A61K31/70

Abstract: Novel 2-halo-6-O-substituted ketolide derivatives and pharmaceutically acceptable salts and esters thereof having antibacterial activity having formula (I) or (II), compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier, a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention, and processes for their preparation.