68557results about "Heterocyclic compound active ingredients" patented technology

A method for manufacturing a porous ceramic scaffold having an organic / inorganic hybrid coating layer containing a bioactive factor includes (a) forming a porous ceramic scaffold; (b) mixing a silica xerogel and a physiologically active organic substance in a volumetric ratio ranging from 30:70 to 90:10 and treating by a sol gel method to prepare an organic / inorganic hybrid composite solution; (c) adding a bioactive factor to the organic / inorganic hybrid composite solution and agitating until gelation occurs; and (d) coating the porous ceramic scaffold with the organic / inorganic composite containing the bioactive factor added thereto. In accordance with the method, the porous ceramic scaffold may be uniformly coated with the organic / inorganic hybrid composite while maintaining an open pore structure, and stably discharge the bioactive factor over a long period of time.

The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as other diagnostic and therapeutic moieties. The invention provides prodrugs and conjugates of the duocarmycin analogues with the linker arms of the invention.

Provided are modulators of TLRs of Formula II:pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.

Disclosed is an oral dosage form comprising (i) an opioid agonist in releasable form and (ii) a sequestered opioid antagonist which is substantially not released when the dosage form is administered intact, such that the ratio of the amount of antagonist released from said dosage form after tampering to the amount of said antagonist released from said intact dosage form is about 4:1 or greater, based on the in-vitro dissolution at 1 hour of said dosage form in 900 ml of Simulated Gastric Fluid using a USP Type II (paddle) apparatus at 75 rpm at 37 degrees C. wherein said agonist and antagonist are interdispersed and are not isolated from each other in two distinct layers.

The invention relates to compounds of formulawhereinR1, R2, and R3 are as defined herein and to a pharmaceutically suitable acid addition salts thereof for the treatment of CNS disorders.