Abstract:
PROBLEM TO BE SOLVED: To provide new semi-synthesized macrolides having antibacterial activity, a pharmaceutical composition including these compounds, and a medical treatment method of remedy.SOLUTION: There is provided a 6-O-substituted erythromycin ketolide derivative expressed by formula (IV-A), where in formula, Rc is hydrogen or a hydroxy-protective group; R is a substituted methyl group; A, B, D and E are each selected from hydrogen, a 1-6C alkyl which may be substituted by a substituent, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, hydroxy, 1-6C alkoxy, and halogen of Br, Cl, F or I, or the like, under conditions that at least two of A, B, D and E are both hydrogen.
Abstract:
PROBLEM TO BE SOLVED: To provide a new semisynthesized macrolide having antibacterial activity.SOLUTION: The antibacterial compound having formula (II) or the like, and pharmaceutically acceptable salts, esters or prodrugs thereof, are provided. Pharmaceutical compositions each containing such a compound; methods for treating bacterial infections by administering such a compound; and a method for producing the compound; are also provided.
Abstract:
PROBLEM TO BE SOLVED: To provide antibacterial compounds. SOLUTION: Antibacterial compounds represented by formula (II), pharmaceutically acceptable salts, esters or prodrugs thereof, medicinal compositions including the same, methods for treating bacterial infections by administration of such compounds and a method for producing the compound are provided. COPYRIGHT: (C)2010,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide novel semi-synthetic macrolides having antibacterial activity and pharmaceutical compositions containing these compounds and to provide medical methods for treating bacterial infection. SOLUTION: Antimicrobial compounds having formula (III) as well as pharmaceutically acceptable salts, esters or prodrugs thereof are provided herein. COPYRIGHT: (C)2010,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide a new antibacterial compound with enhanced activity. SOLUTION: Antibacterial compounds represented by formula (II) or the like, pharmaceutically acceptable salts, esters or prodrugs thereof, medicinal compositions including the same, treatment methods for bacterial infections by administration of such compounds and a method for producing the compound are provided. COPYRIGHT: (C)2009,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide a medicine for bacterial infection. SOLUTION: The invention relates to the compounds represented by formula (IV) in the specification. COPYRIGHT: (C)2009,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide a new class 6-O-substituted erythromycin derivative having increased acid stability to erythromycin A and 6-O-methylerythromycin A, and enhanced activity to gram-negative bacteria and macrolide-resisting gram-positive bacteria. SOLUTION: Provided are an antibacterial compound having structural formula (V) and the like as well as pharmaceutically permissible salts, esters or prodrugs thereof; pharmaceutical compositions comprising the compound; a therapeutic method of bacterial infection by administering the compound; and a production method of the compound. COPYRIGHT: (C)2009,JPO&INPIT
Abstract:
The present invention relates to compounds of formula (I); Pharmaceutical compositions and methods that are useful in the treatment or prevention of metabolic diseases or conditions are also provided.
Abstract:
The present invention relates to compounds of formula (I), wherein R 1 is selected from the group consisting of hydrogen, cycloalkyl, alkyl and haloalkyl; Y is selected from the group consisting of -(CR 4a R- 4b ) m -, -C(O)-, -O-, -N(H)-, -N(alkyl)- and -S-; wherein m is 1, 2 or 3; Ar 3 is phenyl or monocyclic heteroaryl; wherein Ar 3 is substituted with 1, 2 or 3 or 4 substituents. Ar 1 is selected from the group consisting of phenyl and a monocyclic, five or six- membered heteroaryl; Ar 2 is a monocyclic five membered heteroaryl, wherein each Ar 2 is independently unsubstituted or substituted with 1 or 2 substituents selected from the group consisting of alkyl, alkenyl, halogen, -CN, -NO 2 , hydroxy, alkoxy, -NH 2 , -N(H)(alkyl), -N(alkyl) 2 . -C(O)OH, -C(O)Oalkyl, -C(O)H, -C(O)alkyl, and haloalkyl; Z is selected from the group consisting of -OR 9a , -alkylenyl-OR 9a , -NR 6 R9 9b ; and -alkylenyl-NR 6 R 9b ; which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type U diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.
Abstract translation:本发明涉及式(I)化合物,其中R 1选自氢,环烷基,烷基和卤代烷基; Y选自 - (CR 4a),-S(O) - , - C(O) - , - ,-N(H) - , - N(烷基) - 和-S-; 其中m为1,2或3; Ar 3是苯基或单环杂芳基; 其中Ar 3 3被1,2或3或4个取代基取代。 Ar 1选自苯基和单环,五或六元杂芳基; Ar 2是单环五元杂芳基,其中每个Ar 2 2独立地是未取代的或被1或2个选自烷基,烯基,卤素, CN,-NO 2,羟基,烷氧基,-NH 2,-N(H)(烷基), - N(烷基) 。 -C(O)OH,-C(O)O烷基,-C(O)H,-C(O)烷基和卤代烷基; Z选自-OR 9a, - 亚烷基-OR 9a,-NR 6 R 9 9b,/ N >; 和 - 亚烷基-NR 6 R 9b; 其抑制乙酰辅酶A羧化酶(ACC),并且可用于预防或治疗人类的代谢综合征,U型糖尿病,肥胖症,动脉粥样硬化和心血管疾病。
Abstract:
A compound having the formula selected from the group consisting of a compound of formula (I), a compound of formula (II), and a compound of formula (III) as well as pharmaceutically acceptable salts, esters, solvates, metabolites, and prodrugs thereof, are useful in treating bacterial infections. Also provided are pharmaceutically acceptable compositions, methods of treating bacterial infections, and processes for the preparation of the compounds.