- MACROCYCLES AND THEIR USE
-
The present disclosure relates to macrocyclic compounds, pharmaceutical compositions containing macrocyclic compounds, and methods of using macrocyclic compounds to treat disease, such as cancer.
- -
-
Paragraph 0731; 0739; 0740
(2022/02/06)
-
- NEW ISOXAZOLYL ETHER DERIVATIVES AS GABA A ALPHA5 PAM
-
The invention provides novel compounds having the general formula (I) or (II) wherein R2, R3, R5, R99, W, Y and Z are as described herein, compositions including the compounds and methods of using the compounds.
- -
-
-
- NOVEL KETO-OXADIAZOLE DERIVATIVES AS CATHEPSIN INHIBITORS
-
Novel difluorinated amide derivatives of Formula (II) as inhibitors of cathepsin S, K, B, and L, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
- -
-
Page/Page column 38-39
(2008/06/13)
-
- AMINE COMPOUNDS AND USE THEREOF
-
It is intended to provide novel amine compounds which are efficacious against diseases such as infection with HIV virus, rheumatism and cancer metastasis. Namely, amine compounds represented by the following general formula (1):In a typical case, A1 and A2 represent each an optionally substituted monocyclic or polycyclic aromatic heterocycle; W represents cyclic C3-10 alkylene, an optionally substituted monocyclic or polycyclic aromatic heterocycle, a monocyclic or polycyclic aromatic ring or a partly saturated polycyclic aromatic ring; X represents O, CH2, C(=O) or NR11; and D is a group represented by the following general formula (4) or (6).-Q-Y-BIn the formula (6), Q represents a single bond, S, O or NR12; and Y is a group represented by the following general formula (7). z represents an optionally substituted monocyclic or polycyclic aromatic ring. In the formula (6), B represents NR25R26. In the above formulae, R1 to R26 each represents hydrogen, alkyl, alkenyl or alkynyl.
- -
-
Page/Page column 81
(2010/02/12)
-
- Selective cyclooxygenase-2 inhibitors: Heteroaryl modified 1,2-diarylimidazoles are potent, orally active antiinflammatory agents
-
A series of heteroaryl modified 1,2-diarylimidazoles has been synthesized and found to be potent and highly selective (1000-9000-fold) inhibitors of the human COX-2.3-Pyridyl derived COX-2 selective inhibitor (25) exhibited excellent activity in acute (carrageenan induced paw edema, ED50 = 5.4 mg/kg) and chronic (adjuvant induced arthritis, ED50 = 0.25 mg/kg) models of inflammation. The relatively long half-life of 25 in rat and dog prompted investigation of the pyridyl and other heteroaromatic systems containing potential metabolic functionalities. A number of substituted pyridyl and thiazole containing compounds (e.g., 44, 46, 54, 76, and 78) demonstrated excellent oral activity in every efficacy model evaluated. Several orally active diarylimidazoles exhibited desirable pharmacokinetics profiles and showed no GI toxicity in the rat up to 100 mg/kg in both acute and chronic models. The paper describes facile and practical syntheses of the targeted diarylimidazoles. The structure-activity relationships and antiinflammatory properties of a series of diarylimidazoles are discussed.
- Khanna,Yu,Huff,Weier,Xu,Koszyk,Collins,Cogburn,Isakson,Koboldt,Masferrer,Perkins,Seibert,Veenhuizen,Yuan,Yang,Zhang
-
p. 3168 - 3185
(2007/10/03)
-
- 6-(SUBSTITUTED)METHYLENE-PENICILLANIC AND 6-(SUBSTITUTED)HYDROXYMETHYL-PENICILLANIC ACIDS AND DERIVATIVES THEREOF
-
Beta-lactamase inhibiting compounds of the formula: or a pharmaceutically acceptable acid addition or carboxylate salt thereof; where n is zero, 1 or 2; X.3 is H or Br, R1 is H, the residue of certain carboxy-protecting groups or the residue of an ester group readily hydrolyzable in vivo; one of R12 and R13 is H and the other is vinyl, certain aryl, alkylthio, alkylsulfonyl or certain heterocyclyl, aminomethyl, thiocarboxamido or amidino groups; one or R2 and R3 is H and the other is as disclosed for the other of R12 and R13, or is Cl or CH2 OH, and R18 is H or certain acyl groups; intermediates useful in their production, methods for their preparation and use, and pharmaceutical compositions containing them
- -
-
-
- Synthesis of 2-(5'-Substituted Isoxazol-3'-yl)-4-oxo-3-thiazolidinylalkanoic Acids
-
A series of 2-substituted 4-oxo-3-thiazolidinylalkanoic acids bearing an isoxazole nucleus in the 2-position have been prepared.None of the compounds synthesised showed antibacterial activity in vitro.
- Baraldi, P. G.,Simoni, D.,Moroder, F.,Manfredini, S.,Mucchi, L.,et al.
-
p. 557 - 560
(2007/10/02)
-
- Annelation Reactions of N-Heterocycles to Condensed Pyridones with Bridgehead Nitrogen
-
The Horner-Wittig reaction of aromatic and heteroaromatic aldehydes with phosphono succinates gives the methylenesuccinates 2a-m and 4a-k in satisfactory yields.The compounds obtained have the E-configuration, as shown by 1H-NMR-spectroscopic and by chemi
- Linke, Siegfried,Kurz, Juergen,Lipinski, Dietmar,Gau, Wolfgang
-
p. 542 - 556
(2007/10/02)
-
