- 3-(5-METHOXY-1-OXOISOINDOLIN-2-YL)PIPERIDINE-2,6-DIONE DERIVATIVES AND USES THEREOF
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The present disclosure relates to compounds of formula (I') and pharmaceutical compositions and their use in reducing Widely Interspaced Zinc Finger Motifs (WIZ) expression levels, or inducing fetal hemoglobin (HbF) expression, and in the treatment of inherited blood disorders (e.g., hemoglobinopathies, e.g., beta-hemoglobinopathies), such as sickle cell disease and beta-thalassemia.
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- Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor
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A series of 3-arylpropionylpiperazines were synthesized as antagonists of the melanocortin-4 receptor. Their potency was found to be increased by replacing the α-methyl substituent of the initial lead 11 with a larger s-Bu or i-Bu group. Further potency enhancement was observed when a glycine or β-alanine was incorporated onto the benzylamine. Some compounds demonstrated good potency, moderate selectivity, and oral bioavailability.
- Jiang, Wanlong,Tucci, Fabio C.,Chen, Caroline W.,Arellano, Melissa,Tran, Joe A.,White, Nicole S.,Marinkovic, Dragan,Pontillo, Joseph,Fleck, Beth A.,Wen, Jenny,Saunders, John,Madan, Ajay,Foster, Alan C.,Chen, Chen
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p. 4674 - 4678
(2007/10/03)
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- Practical asymmetric synthesis of α-branched 2- piperazinylbenzylamines by 1,2-additions of organometallic reagents to N-tert-butanesulfinyl imines
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2-[4-(tert-Butoxycarbonyl)piperazinyl] benzylidene-tert-butanesulfinamides underwent nucleophilic 1,2-addition with different organometallic reagents to give highly diastereomerically enriched adducts. X-ray crystallography of the resulting α-branched N-B
- Jiang, Wanlong,Chen, Chen,Marinkovic, Dragan,Tran, Joe A.,Chen, Caroline W.,Arellano, L. Melissa,White, Nicole S.,Tucci, Fabio C.
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p. 8924 - 8931
(2007/10/03)
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- AMINE COMPOUNDS
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The present invention provide a compound of the formula:wherein ring A represents an aromatic ring optionally having substituents; B, Y and Ya are the same or different and each represents a bond, etc.; R1 and R2 are the same or different and each represents a hydrogen atom, etc.; R3 represents a hydrogen atom, etc.; R4 and R5 are the same or different and each represents a hydrogen, etc.; R6 represents an indolyl group optionally having substituents; and Z and Za are the same or different and each represents a hydrogen atom, etc.; or a salt thereof or a prodrug thereof, having a somatostatin receptor binding inhibition activity and is useful for preventing and/or treating diseases associated with somatostatin.
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Page 165-166
(2010/02/07)
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