Patent classifications
C07C229/34
SYNTHESIS OF ENDOCHIN-LIKE QUINOLONES
Described herein are new synthetic routes for production of Endochin-Like Quinolone (ELQ) compounds. Synthetic routes to 3-substituted 4(1H)-quinolones are presented that are amenable to industrial scale preparation. One herein presented approach is relatively short, does not require palladium, and involves no chromatographic separation. A second herein presented approach is similarly relatively short, does not require palladium, involves no chromatographic separation, and also avoids high vacuum distillation. Additionally, both approaches require no protecting group chemistry because the insoluble 4(1H)-quinolone is not formed until the final reaction step.
SHORT ACTING PHENYLALKYLAMINE CALCIUM CHANNEL BLOCKERS AND USES THEREOF
The present invention relates to the use of a pharmaceutically effective amount of an short-acting calcium channel blocking compound to treat ischemic heart conditions, cardiac arrhythmias, hypertensive crisis in an emergency room setting, hypertension before, during, or after surgery, no-reflow phenomenon following reperfusion, and diseases associated with decreased skeletal muscle blood flow. The invention also relates to pharmaceutical compositions formulated for use in such methods and to kits for such methods.
SHORT ACTING PHENYLALKYLAMINE CALCIUM CHANNEL BLOCKERS AND USES THEREOF
The present invention relates to the use of a pharmaceutically effective amount of an short-acting calcium channel blocking compound to treat ischemic heart conditions, cardiac arrhythmias, hypertensive crisis in an emergency room setting, hypertension before, during, or after surgery, no-reflow phenomenon following reperfusion, and diseases associated with decreased skeletal muscle blood flow. The invention also relates to pharmaceutical compositions formulated for use in such methods and to kits for such methods.
Agonists that enhance binding of integrin-expressing cells to integrin receptors
A method of enhancing binding of cells to an integrin-binding ligand comprises treating integrin-expressing cells in vitro with an agonist of integrin, wherein the integrin is selected from the group consisting of ?4?1, ?5?1, ?4?7, ?v?3 and ?L?2, and contacting the treated cells with an integrin-binding ligand; integrin agonist compounds having the general formula I; methods of treating integrin-expressing cells with such agonists to enhance binding; and therapeutic methods comprising administering agonist-treated cells or agonist compounds to a mammal.
Agonists that enhance binding of integrin-expressing cells to integrin receptors
A method of enhancing binding of cells to an integrin-binding ligand comprises treating integrin-expressing cells in vitro with an agonist of integrin, wherein the integrin is selected from the group consisting of ?4?1, ?5?1, ?4?7, ?v?3 and ?L?2, and contacting the treated cells with an integrin-binding ligand; integrin agonist compounds having the general formula I; methods of treating integrin-expressing cells with such agonists to enhance binding; and therapeutic methods comprising administering agonist-treated cells or agonist compounds to a mammal.
β-substituted β-amino acids and analogs as chemotherapeutic agents
-Substituted -amino acids, -substituted -amino acid derivatives, and -substituted -amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the -substituted -amino acid derivatives and -substituted -amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.
β-substituted β-amino acids and analogs as chemotherapeutic agents
-Substituted -amino acids, -substituted -amino acid derivatives, and -substituted -amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the -substituted -amino acid derivatives and -substituted -amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.
METHOD FOR CRYSTALLIZATION OF AROMATIC AMINO ACIDS, ENABLING SUSTAINABLE CYCLE OF AMMONIA
The present application provides: a method for crystallization of an aromatic amino acid, enabling sustainable cycle of ammonia; and aromatic amino acid crystals produced by the method.
METHOD FOR CRYSTALLIZATION OF AROMATIC AMINO ACIDS, ENABLING SUSTAINABLE CYCLE OF AMMONIA
The present application provides: a method for crystallization of an aromatic amino acid, enabling sustainable cycle of ammonia; and aromatic amino acid crystals produced by the method.
Pain relief compounds
The present invention relates to the use of compounds for the treatment or prevention of pain in mammals, in particularly in human beings, and also to a process for preparing these compounds.