- Multimodal Anion Exchange Matrices
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The invention discloses a separation matrix which comprises a plurality of separation ligands, defined by the formula R1-L1-N(R3)-L2-R, immobilized on a support, wherein R1 is a five- or six-membered, substituted or non-substituted ring structure or a hydroxyethyl or hydroxypropyl group; L1 is either a methylene group or a covalent bond; R2 is a five- or six-membered, substituted or non-substituted ring structure; L2 is either a methylene group or a covalent bond; R3 is a methyl group; and wherein if R1 is a hydroxyethyl group and L1 is a covalent bond, R2 is a substituted aromatic ring structure or a substituted or non-substituted aliphatic ring structure.
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Paragraph 0081; 0083; 0084; 0085; 0088
(2015/11/23)
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- A strategy for the construction of caged diols using a photolabile protecting group
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Caged analogues of biologically active compounds have received widespread attention as temporally and spatially controlled probes of cell-based processes. Recently, a coumarin-4-ylmethyl derivative has been used to cage carboxylates, sulfonates, carbamates, and phosphates. We describe herein a synthetic strategy that furnishes photosensitive caged diols and provides an entry into the protection/photodeprotection of functionality with modest leaving group abilities.
- Lin, Weiying,Lawrence, David S.
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p. 2723 - 2726
(2007/10/03)
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- Tyrosine kinase inhibitors. 13. Structure - Activity relationships for soluble 7-substituted 4-[(3-bromophenyl)amino]pyrido[4,3-d]pyrimidines designed as inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor
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The general class of 4-(phenylamino)quinazolines are potent (some members with IC50 values 40 mM) and retention of overall inhibitory activity (IC50's of 0.5-10 nM against isolated enzyme and 8-40 nM for inhibition of EGFR autophosphorylation in A431 cells) were weakly basic amine derivatives. These results are broadly consistent with a proposed model for the binding of these compounds to EGFR, in which the 6- and 7-positions of the pyridopyrimidine ring are in a largely hydrophobic binding region of considerable steric freedom, at the entrance of the adenine binding cleft. The most active cationic analogues have a weakly basic side chain where the amine moiety is three or more carbon atoms away from the nucleus. Two of the compounds (bearing weakly basic morpholinopropyl and strongly basic (dimethylamino)butyl solubilizing groups) produced in vivo tumor growth delays of 13-21 days against advanced stage A431 epidermoid xenografts in nude mice, when administered ip twice per day on days 7-21 posttumor implant. Treated tumors did not increase in size during therapy and resumed growth at the termination of therapy, indicating an apparent cytostatic effect for these compounds under these treatment conditions. The data suggest that continuous long-term therapy with these compounds may result in substantial tumor growth inhibition.
- Thompson, Andrew M.,Murray, Donna K.,Elliott, William L.,Fry, David W.,Nelson, James A.,Showalter, H.D. Hollis,Roberts, Bill J.,Vincent, Patrick W.,Denny, William A.
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p. 3915 - 3925
(2007/10/03)
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- propanolamines. 1. Novel β-Blockers with Ultrashort Duration of Action
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Novel propanolamines were synthesized and investigated as potential ultrashort-acting β-adrenergic receptor blockers.Many of these analogues exhibited good potency and short duration.The N-ureidoalkyl analogue 85 (ACC-9089) has a potency equal to propranolol and a duration of action of about 21 min in the dog.It has been selected as a candidate for further clinical study.Structure-activity relationships and structure-duration relationships for these new β-blockers are also discussed.
- Kam, Sheung-Tsam,Matier, William L.,Mai, Khuong X.,Barcelon-Yang, Cynthia,Borgman, Robert J.,et al.
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p. 1007 - 1016
(2007/10/02)
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