135964-75-9Relevant academic research and scientific papers
INHIBITORS OF HEPATITIS C VIRUS POLYMERASE
-
Paragraph 679; 680, (2016/10/11)
The present invention provides, among other things, compounds represented by the general Formula I: (I) and pharmaceutically acceptable salts thereof, wherein L and A (and further substituents) are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.
DERIVATIZED 3-STYRYL-CEPHALOSPORINS
-
Paragraph 00152, (2014/10/18)
Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Also provided are methods of making betalactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions for treatment or prevention of bacterial infections and methods of treatment of such infections.
Further optimization of sulfonamide analogs as EP1 receptor antagonists: Synthesis and evaluation of bioisosteres for the carboxylic acid group
Naganawa, Atsushi,Matsui, Toshiaki,Ima, Masaki,Saito, Tetsuji,Murota, Masayuki,Aratani, Yoshiyuki,Kijima, Hideomi,Yamamoto, Hiroshi,Maruyama, Takayuki,Ohuchida, Shuichi,Nakai, Hisao,Toda, Masaaki
, p. 7121 - 7137 (2007/10/03)
4-{[2-[(2-Furylsulfonyl)(isobutyl)amino]-5-(trifluoromethyl)phenoxy]methyl}benzoic acid analogs 2a and b and a series of the acid analogs, in which the carboxylic acid residue of 2b was replaced with various kinds of carboxylic acid bioisosteres, were synthesized and evaluated as EP1 receptor antagonists. Compound 2b and its monocyclic acid analogs, in which the carboxylic acid residue of 2b was replaced with monocyclic acid bioisosteres, were found to show potent EP1 receptor antagonist activity. Optimization of the linker Y between the phenyl moiety and the carboxylic acid residue of 2b was also carried out (Table 5). Compounds 2b and 16 and 17 possessing conformationally restricted linker Y were found to show the most optimized potency among the tested compounds. Cytochrome P450 inhibition of optimized compounds was also investigated. Details of the structure-activity relationship study are presented.
Novel phenylalanine derivatives
-
Page/Page column 31-32, (2010/02/14)
Specific phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin.
AMINE COMPOUNDS
-
Page 191-192, (2010/02/07)
The present invention provide a compound of the formula:wherein ring A represents an aromatic ring optionally having substituents; B, Y and Ya are the same or different and each represents a bond, etc.; R1 and R2 are the same or different and each represents a hydrogen atom, etc.; R3 represents a hydrogen atom, etc.; R4 and R5 are the same or different and each represents a hydrogen, etc.; R6 represents an indolyl group optionally having substituents; and Z and Za are the same or different and each represents a hydrogen atom, etc.; or a salt thereof or a prodrug thereof, having a somatostatin receptor binding inhibition activity and is useful for preventing and/or treating diseases associated with somatostatin.
QUINAZOLINE DERIVATIVES AND THEIR PREPARATION
-
, (2008/06/13)
A compound of the formula: STR1 in which R 1 and R 2 are each hydrogen, halogen, nitro, amino, protected amino, hydroxyamino, lower alkyl, hydroxy, protected hydroxy, sulfamoyl, carboxy, protected carboxy, mercapto, optionally substituted heterocyclic-car
Quinazoline derivatives
-
, (2008/06/13)
Compounds of the formula: STR1 are described wherein R 1, R 2, R 3 and A are described in the claims. These compounds show significant dopamine receptor agonist activity.
