2440-60-0Relevant academic research and scientific papers
CARBOCYCLIC NUCLEOSIDE ANALOGUE
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Page/Page column 11; 14, (2020/12/30)
The present invention relates to novel hydrolytically stable carbocyclic 5-aza-2-deoxycytidine and carbocyclic 5-aza-cytidine compounds and prodrugs thereof as hypomethylating agents.
The preparation method of the overall tablet sizes hydrochloride (by machine translation)
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Paragraph 0027; 0028; 0029, (2017/08/29)
The invention discloses a method for preparing the acid salt of the overall tablet sizes. In order to 2, 6 - dichloro acetic acid and methoxy isourea hydrochloride as the starting material, by catalytic condensation, aminolysis, salt, purifying to obtain the hydrochloric acid overall tablet sizes. The preparation method of mild reaction conditions, the operation is simple, compared with the prior art, reduce the operation step, reducing the total reaction time, reduce energy consumption, pollution is smaller, is beneficial to the environment. (by machine translation)
Thioimidazoline based compounds reverse glucocorticoid resistance in human acute lymphoblastic leukemia xenografts
Toscan, Cara E.,Rahimi, Marwa,Bhadbhade, Mohan,Pickford, Russell,McAlpine, Shelli R.,Lock, Richard B.
, p. 6299 - 6312 (2015/06/08)
Glucocorticoids form a critical component of chemotherapy regimens for pediatric acute lymphoblastic leukemia (ALL) and the initial response to glucocorticoid therapy is a major prognostic factor, where resistance is predictive of poor outcome. A high-throughput screen identified four thioimidazoline-containing compounds that reversed dexamethasone resistance in an ALL xenograft derived from a chemoresistant pediatric ALL. The lead compound (1) was synergistic when used in combination with the glucocorticoids, dexamethasone or prednisolone. Synergy was observed in a range of dexamethasone-resistant xenografts representative of B-cell precursor ALL (BCP-ALL) and T-cell ALL. We describe here the synthesis of twenty compounds and biological evaluation of thirty two molecules that explore the structure-activity relationships (SAR) of this novel class of glucocorticoid sensitizing compounds. SAR analysis has identified that the most effective dexamethasone sensitizers contain a thioimidazoline acetamide substructure with a large hydrophobic moiety on the acetamide. This journal is
AZACYCLIC COMPOUNDS AS INHIBITORS OF SENSORY NEURONE SPECIFIC CHANNELS
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Page 50, (2010/02/10)
Compounds of the formula (I), and pharmaceutically acceptable salts thereof, are found to be antagonists of SNS sodium channels. They are therefore useful as analgesic and neuroprotective agents wherein: X is -N- or -CH-; n is from 0 to 3.
Preparation of substituted guanidine derivatives
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, (2008/06/13)
Substituted guanidine derivatives of the formula I are prepared by a) converting urea into an alkylated isourea of the formula II and b) reacting the alkylated isourea with a primary or secondary amine of the formula III where the substituents R1, R2 and R10 have the meanings explained in the description.
Imidazolyl-alkenoic acids useful as angiotensin II receptor antagonists
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, (2008/06/13)
Angiotensin II receptor antagonists having the formula: STR1 which are useful in regulating hypertension and in the treatment of congestive heart failure, renal failure, and glaucoma, pharmaceutical compositions including these antagonists, and methods of using these compounds to produce angiotensin II receptor antagonism in mammals.
(cyanomethyl)pyridines useful as PAF antagonists
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, (2008/06/13)
57 The present invention relates to new (cyanomethyl)pyridines of general formula I: wherein Ais nitrogen and Bis -CH-, or Bis nitrogen and Ais -CH-; the group Y-W-represents a group of formula N-CR1(CN)-, N-CH2-CH(CN)-, CH-CH(CN)- or C=C(CN)- wherein R1 is hydrogen or a C1-C6 alkyl group; Rrepresents a group of formula R2CO-,R3R4N-(CH2)nCO- or R5-(CH2)m- wherein R2 represents C1-C15 alkyl, aryl, aryl-(C1-C6)-alkyl, aryl-(C1-C6)-alkenyl, diaryl-(C1-C6)-alkyl, diaryl-(C1-C6)-alkenyl, arylhydroxy-(C1-C6)-alkyl, diarylhydroxy-(C1-C6)-alkyl, aryl-(C1-C6)-alkoxy, diaryl-(C1-C6)-alkoxy, or heteroaryl-(C1-C6)-alkyl group; n is 0, 1, 2 or 3; R3 is hydrogen, C1-C6 alkyl, aryl or aryl-(C1-C6)-alkyl group; R4 is C3-C6 cycloalkyl, aryl, aryl-(C1-C6)-alkyl, diaryl-(C1-C6)-alkyl, aryl-(C1-C6)-alkylcarbonyl or diaryl-(C1-C6)-alkylcarbonyl group; m is 0, 1 or 2; and R5 is aryl-(C1-C6)-alkyl, diaryl-(C1-C6)-alkyl, diaryl-(C1-C6)-alkylcarbonylamino or diaryl-(C1-C6)-alkylaminocarbonyl group. These compounds are potent, orally active PAF antagonists and consequently, useful in the treatment of the diseases in which this substance is involved.
