[EN] HINDERED DISULFIDE DRUG CONJUGATES<br/>[FR] CONJUGUÉS MÉDICAMENTEUX À PONT DISULFURE ENCOMBRÉ
申请人:GENENTECH INC
公开号:WO2017064675A1
公开(公告)日:2017-04-20
The invention relates generally to disulfide drug conjugates wherein a linker comprising a sulfur-bearing carbon atom substituted with at least one hydrocarbyl or substituted hydrocarbyl is conjugated by a disulfide bond to a cysteine sulfur atom of a targeting carrier, and wherein the linker is further conjugated to a drug moiety. The invention further relates to activated linker-drug conjugates suitable for conjugation to a targeting carrier by a disulfide bond. The invention further relates to methods for preparing hindered disulfide drug conjugates.
2-NH-heteroarylimidazoles with antibacterial activity
申请人:Berge John
公开号:US20060014748A1
公开(公告)日:2006-01-19
Compounds of formula (I):
are inhibitors of bacterial methionyl tRNA synthetase and are of use in treating bacterial infections.
公式(I)的化合物是细菌甲硫氨酸tRNA合成酶的抑制剂,可用于治疗细菌感染。
2-NH-HETEROARYLIMIDAZOLES WITH ANTIBACTERIAL ACTIVITY
申请人:Berge John
公开号:US20070213362A1
公开(公告)日:2007-09-13
A method of inhibiting MetRS activity comprises administering to a patient in need thereof a MetRS inhibiting effective amount of a compound of the formula (I). A method of treating a resistant or multiply-resistant
E. faecalis
infection, a resistant or multiply-resistant
S. aureus
infection, and/or a resistant or multiply-resistant
S. epidermidis
infection comprises administering to a patient in need thereof an antibacterially effective amount of a compound of the formula (I).
The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I):
wherein the symbols are defined in the specification.
FUSED HETEROCYCLIC COMPOUNDS AS PHOSPHODIESTERASES (PDES) INHIBITORS
申请人:Taniguchi Takahiko
公开号:US20130172328A1
公开(公告)日:2013-07-04
The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):