- Heterocyclic derivatives as well as pharmaceutical compositions and application thereof
-
The invention discloses novel heterocyclic derivatives shown in a formula I, a formula II and a formula III, pharmaceutical compositions containing the heterocyclic derivatives and application of the heterocyclic derivatives in preparation of drugs for preventing and/or treating indications related to proton pump inhibition regulation. The heterocyclic derivatives disclosed by the invention are strong in drug effect and long in half-life period, are ideal efficient proton pump inhibitors, and can be used for treating or preventing diseases or diseases needing proton pump inhibition effect regulation, such as ulcer, esophagitis, gastritis, gastroesophageal reflux, helicobacter pylori infection, gastric cancer and the like.
- -
-
-
- KETONE INHIBITORS OF LYSINE GINGIPAIN
-
The present invention provides compounds according to Formula (I) as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.
- -
-
-
- Copper(II)-Catalyzed Single-Step Synthesis of Aryl Thiols from Aryl Halides and 1,2-Ethanedithiol
-
A highly efficient transition metal-catalyzed single-step synthesis of aryl thiols from aryl halides has been developed employing copper(II) catalyst and 1,2-ethanedithiol. The key features are use of readily available reagents, a simple operation, and relatively mild reaction conditions. This new protocol shows a broad substrate scope with excellent functional group compatibility. A variety of aryl thiols are directly prepared from aryl halides in high yields. Furthermore, the aryl thiols are used in situ for the synthesis of more advanced molecules such as diaryl sulfides and benzothiophenes.
- Liu, Yajun,Kim, Jihye,Seo, Heesun,Park, Sunghyouk,Chae, Junghyun
-
supporting information
p. 2205 - 2212
(2015/07/27)
-
- NOVEL AROMATIC COMPOUND AND POLYARYLENE COPOLYMER HAVING NITROGEN-CONTAINING HETEROCYCLE INCLUDING SULFONIC ACID GROUP IN SIDE CHAIN
-
Provided is a solid polymer electrolyte having increased heat resistance and high proton conductivity and a proton conductive membrane composed of the electrolyte. Also provided is a copolymer having a sulfonic acid group. The copolymer includes a repeating unit represented by Formula (1): (in the formula, Y denotes at least one kind of structure selected from the group consisting of —CO—, —SO2—, —SO—, —CONH—, —COO—, —(CF2)l— (l is an integer of 1 to 10), and —C(CF3)2—; W denotes at least one kind of structure selected from the group consisting of a direct bond, —CO—, —SO2—, —SO—, —CONH—, —COO—, —(CF2)l— (l is an integer of 1 to 10), —C(CF3)2—, —O—, and —S—; Z denotes a direct bond or at least one kind of structure selected from the group consisting of —(CH2)l—(l is an integer of 1 to 10), —C(CH3)2—, —O—, —S—, —CO—, and —SO2—; R30 denotes a nitrogen-containing aromatic ring having a substituent represented by —SO3H, —O(CH2)hSO3H, or —O(CF2)hSO3H (h is an integer of 1 to 12); p is an integer of 0 to 10; q is an integer of 0 to 10; r is an integer of 1 to 5; and k is an integer of 0 to 4).
- -
-
-
- Copper-catalyzed coupling of thiourea with aryl iodides: The direct synthesis of aryl thiols
-
A general, economical and efficient protocol for the direct copper-catalyzed coupling of thiourea with aryl iodides is developed and it will be potentially applied in large-scale industry as a preferred process.
- Qiao, Shu,Xie, Kun,Qi, Junsheng
-
scheme or table
p. 1441 - 1443
(2011/01/04)
-
- CARBACEPHEM β-LACTAM ANTIBIOTICS
-
Carbacephem -lactam antibiotics having structure (I) are disclosed, including stereoisomers, pharmaceutically acceptable salts, esters and prodrugs thereof, wherein Ar1, Ar2, R1 and R2 are as defined herein. The compounds are useful for the treatment of bacterial infections, in particular those caused by methicillin-resistant Staphylococcus spp.
- -
-
Page/Page column 71
(2010/04/06)
-
- CARBACEPHEM β-LACTAM ANTIBIOTICS
-
Carbacephem β-lactam antibiotics having the following chemical structures (I) and (II) are disclosed, including stereoisomers, pharmaceutically acceptable salts, esters and prodrugs thereof, wherein Ar2, R1, R2 and R3 are as defined herein. The compounds are useful for the treatment of bacterial infections, in particular those caused by methicillin-resistant Staphylococcus spp.
- -
-
Page/Page column 84-85
(2009/05/30)
-
- From haloquinolines and halopyridines to quinoline- and pyridinesulfonyl chlorides and sulfonamides
-
The action of sodium methanethiolate (in boiling DMF) towards haloazines (i.e. chloro- or bromo-pyridines and quinolines) (1) (with halogen substituent in non-aza-activated position) causes sequentially halogen ipso-substitution to methylthioazines (2) and then S-demethylation to azinethiolates (3A), which were: i) subjected to S-methylation, ii) oxidized to diazinyl disulfides (4) and iii) oxidatively chlorinated to azinesulfonyl chlorides (5). α- and γ-pyridine- and quinolinesulfonyl chlorides (5a, 5c, 5d and 5f) were prepared by oxidative chlorination of respective disulfides (4) performed in conc. hydrochloric acid and characterized by 1H and 13C NMR spectra. All azinesulfonyl chlorides (5) were effectively converted to corresponding azinesulfonamides (6).
- Maslankiewicz, Andrzej,Marciniec, Krzysztof,Pawlowski, Maciej,Zajdel, Pawel
-
p. 1975 - 1990
(2008/09/16)
-
- N-heterocyclic compounds as radioprotectors. 1. 2-Pyridinemethanethiol, 2-pyrazinemethanethiol and related compounds
-
2-Pyridinemethanethiol 1, which is structurally related to cysteamine, showed good radioprotective potency in mice, but 2-pyrazinemethanethiol 9 was inactive. Certain derivatives of 1 and 9 that were synthesized were radioprotective. The 3 isomeric mercaptopyridines showed activity. Further study of N-heteroaromatic compounds as radioprotectors is indicated. An improved method for the preparation of 9 is described.
- Barnes,Fatome,Esslemont,Jones
-
p. 515 - 519
(2007/10/02)
-