- GLP-1R AGONISTS AND USES THEREOF
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Provided herein are compounds of Formula (I) and pharmaceutical compositions thereof, for use in, e.g. treating type 2 diabetes mellitus, pre-diabetes, obesity, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, and cardiovascular disease.
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Page/Page column 59; 113
(2020/10/21)
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- Synthesis, biological evaluation and SAR studies of benzimidazole derivatives as H1-antihistamine agents
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A series of benzimidazole derivatives have been designed, synthesized and evaluated for H1 antihistamine activity. Six compounds have showed potent antihistamine H1 activity. The primary SAR analysis indicated that benzyl or benzylidinyl substituted on the exo-nitrogen atom and C2 of the benzimidazole were significant. Further experiments indicated that compound 17d displayed excellent activity to reduce mast cell degranulation, moderate anti-PAF activity and decreased potency on hERG compared to astermizole. Hence compound 17d could serve as anti-allergic agent for further development.
- Wang, Xiao Jian,Xi, Mei Yang,Fu, Ji Hua,Zhang, Fu Rong,Cheng, Gui Fang,Yin, Da Li,You, Qi Dong
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p. 707 - 710
(2012/07/03)
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- QUINAZOLINE AND QUINOLINE DERIVATIVES AS IRREVERSIBLE PROTEIN TYROSINE KINASE INHIBITORS
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A compound of formula (I), a pharmaceutically acceptable salt, or hydrate thereof, and a method of preparing the same. A method of treating or preventing a physiological disorder caused by abnormal protein tyrosine kinase activity in a mammal comprising administering to said mammal a pharmaceutical composition comprising a compound of formula (I).
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Page/Page column 12
(2009/05/29)
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- INREVERSIBLE PROTEIN TYROSINE KINASES INHIBITORS AND THE PREPARATION METHODS AND USES THEREOF
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The compounds which could inhibit protein tyrosine kinases activity or the pharmaceutical acceptable salts or hydrates thereof. The uses of the compounds in treating or preventing physiological abnormal induced by protein tyrosine kinases overexpression in mammal. The preparation methods of the compounds.
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Page/Page column 19
(2011/08/10)
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- Metabolites of tricyclic amides useful for inhibition of G-protein function and methods of treatment of proliferative diseases
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The present invention relates to metabolites of tricyclic amides, and structurally related compounds, represented by the structural formula (I): and pharmaceutically acceptable isomers, salts, solvates or esters of the compound of formula (I), wherein: R1 is selected from the group consisting of H and ═O; R2-R5 can be the same or different, each being independently selected from the group consisting of H, —OH, halide, —NH2 and ═O; and, the combination solid-dashed lines independently represent either single bonds or double bonds, wherein the number of combination solid-dashed lines that are double bonds is not greater than 2, and when, the double bonds are not adjacent, and when 0, one of R1-R5 is not H. Also disclosed are methods of treatment of proliferative diseases and methods for inhibiting the abnormal growth of cells, and for inhibiting farnesyl protein transferase using the novel compounds.
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Page/Page column 6-7
(2008/06/13)
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- REVERSE HYDROXAMIC ACID DERIVATIVES
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Reverse hydroxamic acid derivatives having specific structure represented by a general formula (Ia): (wherein A is a hydrogen atom or the like; Ar1 is an arylene or the like; Ar2 is an optionally substituted aryl, a heteroaryl or the
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Page 116-117
(2008/06/13)
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- BENZOFURAN DERIVATIVE
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The present invention provides a benzofuran derivative of the formula [1]: wherein x is a group of the formula: -N="or" -CH=; Y is an optionally substituted amino group, an optionally substituted cycloalkyl group or an optionally substituted saturated heterocyclic group; A is a single bond, a carbon chain optionally having a double bond within or at the end(s) of the chain, or an oxygen atom; R1 is a hydrogen atom or a halogen atom; Ring B is an optionally substituted benzene ring; and R3 is a hydrogen atom, or a pharmaceutically acceptable salt thereof, which is useful as a medicament, especially as an activated blood coagulation factor X inhibitor.
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- Compounds with growth hormone releasing properties
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Compounds of peptide mimetic nature having the general formula I STR1 wherein a and b are independently 1 or 2, R1 and R2 are independently H or C1-6 alkyl, G and J are independently, inter alia, aromats, and D and E are independently several different groups are growth hormone secretagogous with improved bioavailability.
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- Synthesis and in vitro characterization of new growth hormone secretagogues derived from ipamorelin with dipeptidomimetic N-terminals
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The structural requirements for N-terminal features for the minimal structure of growth hormone secretagogues derived from ipamorelin are investigated. It is found, that incorporation of nonpolar peptidomimetic amino acids at the N-terminal can replace the Aib-His moiety and lead to compounds with high in vitro potency with respect to their growth hormone secretagogue properties. New unnatural amino acids with double bonds, ether- linkages, and 1,3-phenylene-moieties in the backbone proved to be valuable dipeptidomimetics. Using them, growth hormone secretagogues with high potencies were obtained.
- Peschke, Bernd,Ankersen, Michael,Sehested Hansen, Birgit,Kruse Hansen, Thomas,Langeland Johansen, Nils,Lau, Jesper,Madsen, Kjeld,Petersen, Hans,Thogersen, Henning,Watson, Brett
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p. 363 - 380
(2007/10/03)
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