- Compounds for treating spinal muscular atrophy
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Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy. In a specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN2 into mRNA that is transcribed from the SMN2 gene. In another specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 into mRNA that is transcribed from the SMN1 gene. In yet another embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 and SMN2 into mRNA that is transcribed from the SMN1 and SMN2 genes, respectively.
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Page/Page column 398
(2017/05/02)
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- CYCLOPROPANE COMPOUND
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A cyclopropane compound represented by the following formula (A) or a pharmaceutically acceptable salt thereof has orexin receptor antagonism, and therefore has a potencial of usefulness for the treatment of sleep disorder for which orexin receptor antagonism is effective, for example, insomnia: wherein Q represents —CH— or a nitrogen atom, R1a and R1b each independently represent a C1-6 alkyl group and the like, R1c represents a hydrogen atom and the like, R2a, R2b, R2c and R2d each independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group and the like, R3a, R3b and R3c each independently represent a hydrogen atom, a halogen atom and the like, and R3d represents a hydrogen atom and the like.
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Page/Page column 160
(2012/04/23)
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- Synthesis of novel 5,6-substituted furo[2,3-d]pyrimidines via Pd-catalyzed cyclization of alkynylpyrimidinols with aryl iodides
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A flexible method for the synthesis of 5,6-disubstituted furo[2,3-d]pyrimidine derivatives is described. The key step is a palladium-catalyzed arylative cyclization of alkynylpyrimidinols with various aryl iodides, which gave the title compounds in 36-75% yield.
- Liu, Zhende,Li, Dewen,Li, Shukun,Bai, Donglu,He, Xuchang,Hu, Youhong
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p. 1931 - 1936
(2007/10/03)
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- Metabolites of the angiotensin II antagonist tasosartan: The importance of a second acidic group
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Described in this paper is the synthesis and pharmacological activity of five metabolites of the angiotensin II antagonist tasosartan (1). Of particular interest is the effect of the additional acidic group of the enol metabolite (8) on activity. As suggested by the structural-activity relationship of other angiotensin II antagonist series, a second acidic group can improve receptor binding activity but decrease in vivo activity after oral dosing. The metabolic introduction of a second acidic group in tasosartan bypasses this problem and contributes to the excellent profile of the compound. A molecular modeling study provides a rationale for the role of the enol group of 8 in AT1 receptor binding.
- Ellingboe, John W.,Collini, Michael D.,Quagliato, Dominick,Chen, James,Antane, Madelene,Schmid, Jean,Hartupee, Dale,White, Valerie,Park, C. Hyung,Tanikella, Tarak,Bagli, Jehan F.
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p. 4251 - 4260
(2007/10/03)
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- Substituted pyridopyrimidines and antihypertensives
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This invention relates to substituted pyridopyrimidinones of general formula (I): STR1 wherein R1 and R2 are independently H, lower alkyl containing 1 to 6 carbon atoms, hydroxyalkyl containing 1 to 6 carbon atoms, formyl, carbonylalkyl containing 1 to 6 carbon atoms, carboxy, or carboxyalkyl containing 1 to 6 carbon atoms; R3 and R4 are independently H, lower alkyl containing 1 to 6 carbon atoms, hydroxy; R3a and R4a are H, and when taken together with R3 and R4 respectively comprise a carbonyl; with the proviso that at least one of the groups R1 and R2 must be hydroxyalkyl, formyl, carbonylalkyl containing 1 to 6 carbon atoms, carboxy, or carboxyalkyl containing 1 to 6 carbon atoms; or R3 and R4 must be hydroxy or taken together with R3a and R4a respectively must comprise a carbonyl; n is 0 to 3; Ar1 is STR2 wherein W is H, lower alkyl containing 1 to 6 carbon atoms, halogen, hydroxy, or lower alkoxy containing 1 to 6 carbon atoms; Ar2 is STR3 wherein X is CO2 H, CN, or STR4 wherein R5 is H, CH3, tert-butyl, tri-n-butylstannyl, or triphenylmethyl; and the pharmaceutically acceptable salts thereofuseful for treating hypertension and congestive heart failure, to pharmaceutical compositions, and to methods for production thereof.
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