130368-98-8Relevant academic research and scientific papers
SUBSTITUTED QUINAZOLINES AS NLRP3 MODULATORS, FOR USE IN THE TREATMENT OF CANCER
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Page/Page column 89, (2020/07/31)
The present invention provides compounds of Formula (I): Formula (I) wherein all of the variables are as defined herein. These compounds are modulators of NLRP3, which may be used as medicaments for the treatment of proliferative disorders, such as cancer in a subject (e.g., a human).
CHEMICAL COMPOUNDS AS H-PGDS INHIBITORS
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, (2019/01/08)
A compound of formula (I) wherein R1, R2, R3, R4, X, Y, and A are as defined herein. The compounds of the present invention are inhibitors of hematopoietic prostaglandin D synthase (H-PGDS) and can be useful in the treatment of Duchenne muscular dystrophy. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting H-PGDS activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
PYRROLO PYRIMIDINE DERIVATIVE
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Paragraph 0366, (2016/09/26)
The compound represented by general formula (I) has strong Axl inhibition activity by means of a pyridone ring structure being introduced into a pyrrolo pyrimidine skeleton, and so the result can serve as a treatment agent for Axl-related diseases, for example cancers such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glial tumors, renal disease, immune system disorders, and cardiovascular disease.
FLUOROPHENYL BICYCLIC HETEROARYL COMPOUNDS
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Page/Page column 75, (2012/09/22)
The present invention provides a compound of formula (I); a method for manufacturing the compounds of the invention, and its use as a IGF-1R inhibitor. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
ETHER DERIVATIVES OF BICYCLIC HETEROARYLS
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Page/Page column 89, (2011/04/18)
The invention relates to compounds of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; such compounds as a medicament; such compounds for the treatment of a proliferative disease
BENZENE-FUSED 6-MEMBERED OXYGEN-CONTAINING HETEROCYCLIC DERIVATIVES OF BICYCLIC HETEROARYLS
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Page/Page column 63-64, (2011/06/23)
The invention relates to new derivatives of formula I, wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a proliferative disease.
Discovery of 4-[3-(trans-3-Dimethylaminocyclobutyl)-1H-indol-5-ylmethyl](4S)-oxazolidin- 2-one (4991W93), a 5HT1b/1d receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation
Jandu,Barrett,Brockwell,Cambridge,Farrant,Foster,Giles,Glen,Hill,Hobbs,Honey,Martin,Salmon,Smith,Woollard,Selwood
, p. 681 - 693 (2007/10/03)
Utilizing a pharmacophoric model of binding of 3-(2-aminoethyl)indoles to 5HT1B/1D receptors, we identified the 3-aminocyclobutyl group as a potential ethylamine isostere. A novel multidimensional chemometric approach was used to predict the intrinsic activity (degree of agonism) at the receptor. A qualitative model for pharmacokinetic properties was then used to guide the synthesis toward molecules likely to have oral bioavailability in humans. A novel synthetic route to 3-(3-dimethylaminocyclobutyl)indoles was developed. Analogues showed generally lower intrinsic activity at 5HT1B/1D receptors than their ethylamine counterparts. 4-[3-(trans-3-Dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin- 2-one (4991W93, 1) was identified as a partial agonist against 5HT1B/1D receptors, with low intrinsic activity. This molecule also has significant activity against 5HT1F receptors but is selective over other 5HT receptors. In addition this compound was found to be an exceptionally potent inhibitor of electrically induced plasma extravasation. Compound 1 may have utility in the treatment and prophylaxis of migraine.
Process for preparation of intermediates of carbocyclic nucleoside analogs
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, (2008/06/13)
A compound of the formula: STR1 wherein A is a purin-9-yl group, a heterocyclic isostere of a purin-9-yl group, a pyrimidin-1-yl group or a heterocyclic isostere of a pyrimidin-1-yl group; E is hydrogen, --CH2 OH or --OH; and G and D are indepe
