- 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 400; 401
(2017/05/02)
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- Dipyridine ligands with axial chirality and synthetic method thereof
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The invention relates to dipyridine ligands with axial chirality. A synthetic method adopts 3-hydroxy-2-halogen pyridine as an initial raw material, and includes loading a chiral skeleton with the pyridine through a Mitsunobu reaction with a chiral diol, and achieving pyridine coupling through an Ullman reaction catalyzed by nickel (0) or copper (0) to obtain the dipyridine ligands induced by the chiral diol. The method is simple and convenient in operation and high in yield. The synthetic method is more practical when being compared with traditional methods.
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Paragraph 0047; 0048
(2016/10/17)
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- 2,3-DIHYDRO-1H-INDEN-1-YL-2,7-DIAZASPIRO[3.5] NONANE DERIVATIVES
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The present invention provides a compound of Formula (I) or a pharmaceutically salt thereof wherein R1, R2, Ra, L, Z, Z1 and Z2 are as defined herein, that act as Ghrelin antagonists or inverse agonists; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the antagonism of the Ghrelin receptor.
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Page/Page column 32
(2011/10/10)
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- Preparation of functionalized 3,4-pyridynes via 2-magnesiated diaryl sulfonates
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The preparation of functionalized 3,4-pyridynes of type 1 as highly reactive intermediates has been achieved by the controlled elimination of readily generated 2-magnesiated diaryl sulfonates of type 2 obtained by a low temperature I/Mg- or Br/Mg-exchange starting from the corresponding halides of type 3. After trapping with furan, moderate to good yields of the desired functionalized cycloadducts of type 4 are obtained. The addition of a magnesium arylthiolate or magnesium phenylselenide to 3,4-pyridyne followed by quenching with an electrophile is also described.
- Lin, Wenwei,Chen, Ling,Knochel, Paul
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p. 2787 - 2797
(2007/10/03)
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- ANTIPRURITICS
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It is intended to provide antipruritics (drugs to control itching, antiitch agents and drugs to stop itching). It is found out that a compound having an agonistic activity to the cannabinoid receptor shows an antipruritics effect.
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Page/Page column 35; 36
(2008/06/13)
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- PYRIDONE DERIVATIVE HAVING AFFINITY FOR CANNABINOID 2-TYPE RECEPTOR
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It was found that the compound having a binding activity to the cannabinoid type 2 receptor represented by the formula (I): wherein R' is a group represented by the formula: -Y1-Y2-Y3Ra wherein Y1 is single bond or the like; Y2 is -C(=O)-NH- or the like; Y3 is optionally substituted aryl or the like; R2 is hydrogen or the like; R3 is alkyl or the like; R4 is alkyl or the like; R5 is optionally substituted alkyl or the like; or R3 and R4 taken together with the adjacent atom form cyclic group or the like.
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Page/Page column 54
(2008/06/13)
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- Synthesis of novel substituted pyridines as inhibitors of endothelin converting enzyme-1 (ECE-1)
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A series of bi-aryl pyridine carboxylic acids has been prepared and evaluated as inhibitors of ECE-1. The analogs were prepared by Pd catalyzed cross couplings of halogenated pyridines with heteroaryl organo -boranes, - tinate or -zincate derivatives.
- Massa, Mark A.,Patt, William C.,Ahn, Kyunghye,Sisneros, Andre M.,Herman, Sarah B.,Doherty, Annette
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p. 2117 - 2122
(2007/10/03)
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