- Glycinamide derivative as well as preparation method and application thereof
-
The invention discloses a glycinamide derivative as well as a preparation method and application thereof. The derivative with a structural formula as shown in the following formula (I) is provided; and in the formula, R1 is selected from Cl and H, R2 is one selected from H, CH3 and CH2CH3; and X is one selected from NHCH3, NHCH2CH3, N (CH2CH3) 2, a pyrrolyl group and a piperidyl group. During preparation, different phenyl glutaric acid compounds are selected as raw materials and are respectively subjected to amidation reaction twice with an aminoindane hydrochloride derivative and an ethylenediamine derivative to obtain a target derivative. The prepared derivative or the pharmaceutically acceptable salt thereof, or the pharmaceutical composition thereof can be used as an S-adenosyl homocysteine hydrolase inhibitor for the development of antitumor drugs .
- -
-
Paragraph 0013; 0031-0032; 0034-0036
(2021/06/12)
-
- INHIBITORS OF PROLYL-TRNA-SYNTHETASE
-
The present application provides compounds which are inhibitors of aminoacyl tRNA-synthetase (e.g., prolyl-tRNA-synthetase) and are useful for treating disorders associated with aminoacyl tRNA-synthetase activity and/or expression. Pharmaceutical compositions comprising the compounds and methods of using the compounds are also provided.
- -
-
-
- TACHYKININ RECEPTOR ANTAGONISTS
-
The present invention relates to selective NK-1 receptor antagonists of Formula (I) or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess of tachykinins.
- -
-
-
- Synthesis and structure-activity relationships of trisubstituted phenyl urea derivatives as neuropeptide Y5 receptor antagonists
-
1-((1R,2R)-2-Hydroxy-1-methyl-2-phenylethyl)-1-methyl-3-(4-phenoxyphenyl)urea (1) was identified as a hit from the screening of the neuropeptide Y5 (NPY5) receptor. This lead was optimized for in vitro potency by changing the stereochemistry, the phenylethyl segment, the urea portion, and the 4-phenoxyphenyl group on the molecule. Over 40 analogues of 1 were prepared to study the structure-activity relationship for this series. The most potent compounds in this class have IC50S less than 0.1 nM at the NPY5 receptor (e.g., 40f, 44a, and 47). To determine the functional activity for this series of compounds, selected analogues were tested in a cellular assay measuring forskolin-induced cyclic AMP accumulation in 293 cells transfected with the human NPY5 receptor. All urea analogues tested in the functional assay acted as antagonists (e.g., 1, 32, 40a, and 44e).
- Fotsch,Sonnenberg,Chen,Hale,Karbon,Norman
-
p. 2344 - 2356
(2007/10/03)
-
- Amino-benzocycloalkane derivatives
-
Compounds of the formula I wherein R2—C, R3—C, R4—C or R5—C may be replaced by N; and wherein n is 1, 2 or 3; R1is aryl, cycloalkyl or heterocyclyl; R2, R3, R4and R5are independently hydrogen, optionally substituted alkyl, halo, amino, substituted amino, trifluoromethyl, cyano, carboxyl, alkoxycarbonyl, aralkoxycarbonyl, (alkyl, aryl or aralkyl)-thio, (alkyl, aryl or aralkyl)-oxy, acyloxy, (alkyl, aryl or aralkyl)-aminocarbonyloxy; or any two of R2, R3, R4and R5at adjacent positions are alkylenedioxy; R6is hydrogen, optionally substituted alkyl, amino, substituted amino, acylamino, wherein Rais hydrogen or optionally substituted alkyl, Rband Rcare independently hydrogen, optionally substituted alkyl, cycloalkyl, aryl or heterocyclyl; or Rband Rctogether represent lower alkylene or lower alkylene interrupted by O, S, or N—(H, alkyl or aralkyl); Rdis optionally substituted alkyl, cycloalkyl, aryl or heterocyclyl; and Reis optionally substituted alkyl, aryl, heterocyclyl, cycloalkyl, amino or substituted amino; and pharmaceutically acceptable salts thereof; and enantiomers thereof; which are useful as inhibitors of microsomal triglyceride transfer protein (MTP) and of apolipoprotein B (ApoB) secretion.
- -
-
-
- DERIVATIVES OF 4-(AMINOMETHYL) PIPERIDINE, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
-
Compounds of general formula (I) STR1 in which n is 1 or 2; R represents a linear or branched C 1-C 3-alkyl group; andX represents at least one substituent chosen from hydrogen, halogen, C 1-C 3-alkyl and C 1-C 3-alkoxy, in the form of a free base or an acid addition salt thereof, and their therapeutic application.
- -
-
-
- Comparison of Biological Effects of N-Alkylated Congeners of β-Phenylethylamine Derived from 2-Aminotetralin, 2-Aminoindan, and 6-Aminobenzocycloheptene
-
Three series of bicyclic, semirigid congeners of β-phenethylamine have been prepared for evaluation of the effect of ring size (and of concomitant conformational variation) on biological activity in a variety of assays for adrenergic and dopaminergic actions.Pharmacologic activity was associated with 2-aminotetralin and 2-aminoindan derivatives, but was not found with 6-aminobenzocycloheptene derivatives.Noteworthy is the ability of several aminotetralins and aminoindans to increase the hot-plate reaction time without eliciting dopaminergic effects.This action was not blocked by pretreatment with naloxone.
- Cannon, Joseph G.,Perez, Julio A.,Pease, Jonathan P,Long, John Paul,Flynn, Jan R.,et al.
-
p. 745 - 749
(2007/10/02)
-