Abstract: The present invention provides a method for physically separating the active pharmaceutical ingredient (API) from the excipients in a pharmaceutical formulation before the API is fully characterized by standard techniques. The presently disclosed method is based on making use of the difference in density of the API and that of the excipients. In the method, the API is not dissolved, nor is the crystal form of the API changed.

Abstract: The present invention provides a method for physically separating the active pharmaceutical ingredient (API) from the excipients in a pharmaceutical formulation before the API is fully characterized by standard techniques. The presently disclosed method is based on making use of the difference in density of the API and that of the excipients. In the method, the API is not dissolved, nor is the crystal form of the API changed.

Abstract: The present invention relates to novel phosphoric acid salts of 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine, and polymorphs, hydrates and solvates thereof, which are potent inhibitors of dipeptidyl peptidase-IV useful for the prevention and/or treatment of non-insulin dependent diabetes mellitus, also referred to as type 2 diabetes. The present invention also relates to the process for preparing the novel phosphoric acid salts of 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine, as well as pharmaceutical compositions containing the novel phosphoric acid salts, and methods of use thereof for the treatment of diabetes, obesity, and high blood pressure.

Abstract: A method for the preparation of calix[n]arene derivatives, in particular phosphonated calix[n]arenes. The present invention also relates to nano-structures of phosphonated calix[n]arenes.

Abstract: A method of using a crystallographic framework of sterically bulky calixarene molecules to selectively separate and/or store volatile gas components. Sterically bulky calix[4]arenes or their derivatives form a crystalline lattice that has relatively large lattice voids, is nonporous, and is held together predominately by van der Weals forces. The calix[4]arene lattice can form a guest-host assembly by absorbing a desired volatile gas guest component into the crystalline lattice without any phase shift or other change to the lattice structure. The crystalline calixarene can also be desirably used to purify a gas mixture by removing one or more volatile gas contaminants or by removing and storing the desired volatile gas component. This method can preferably be used to purify a hydrogen gas stream by removing the carbon dioxide and carbon monoxide contaminants or to remove and store oxygen from the air or carbon dioxide and carbon monoxide from combustion gases.

Abstract: A method of using a crystallographic framework of sterically bulky calixarene molecules to selectively separate and/or store volatile gas components. Sterically bulky calix[4]arenes or their derivatives form a crystalline lattice that has relatively large lattice voids, is nonporous, and is held together predominately by van der Waals forces. The calix[4]arene lattice can form a guest-host assembly by absorbing a desired volatile gas guest component into the crystalline lattice without any phase shift or other change to the lattice structure. The crystalline calixarene can also be desirably used to purify a gas mixture by removing one or more volatile gas contaminants or by removing and storing the desired volatile gas component. This method can preferably be used to purify a hydrogen gas stream by removing the carbon dioxide and carbon monoxide contaminants or to remove and store oxygen from the air or carbon dioxide and carbon monoxide from combustion gases.

Abstract: A method for the preparation of calix[n]arene derivatives, in particular phosphonated calix[n]arenes. The present invention also relates to nano-structures of phosphonated calix[n]arenes.

Abstract: A guest host assembly comprising a host assembly formed of calixarene molecules and a guest component located within the host assembly. A crystallographic assembly of layers of the calixarene molecules and stacked along the crystallographic c axis of the assembly in a repeating configuration associated together predominantly by van der Waal forces. The guest component is transferable through the host assembly in a direction normal to the stacked layers. The calixarene molecules are configured in bilayers of adjacent layers along the c axis. The bilayers are shifted along the a or b axis so the assembly, relative to a corresponding assembly of the calixarene molecules without the inclusion of the guest component is shifted. The calixarene are calix(N)arenes in which N is an integer within the range of 4–8. The calixarene molecules are distally substituted with a substituent such as methyl, ethyl, propyl, butyl amyl or phenyl groups.

Abstract: Disclosed are the general principles upon which closed molecular or ionic structural frameworks may be prepared. These frameworks are based upon the self-assembly (wherein the term self-assembly refers to the association of chemical components through inter-component bonds) of n>4 subunits where surface curvature is supplied by edge sharing of subunits.

Abstract: A guest-host assembly having a generally spheroidal host assembly formed of trimers of calixarene molecules in a hexagonal close-packed assembly and its preparation. The calixarene trimers are associated together predominantly by van der Waals forces to provide dilated channels having void volumes within the range of 100-200 ?3. A guest component, such as hydrogen, methane, or another hydrocarbon or halocarbon, is encapsulated within the dilated channels of the spheroidal host assembly and retained within the channels primarily by van der Waals forces. The guest-host assembly is stable at a temperature of 150° C. or higher. The temperature at which the onset of the release of the guest component occurs is within the range of 150-300° C.

Abstract: A composition comprising a guest/host assembly having a spheroidal host assembly comprised of a hexamer of a methylene-bridged trihydroxybenzene tetramer and a guest component encapsulated within the spheroidal host assembly to provide a highly stable guest/host assembly. A guest component, specifically a pharmaceutically active agent, is encapsulated within the spheroidal host assembly to provide a guest/host assembly exhibiting a high stability, being stable upon a solubilization in a mixture of acetone and water in a one-to-one ratio for a period of one day at a temperature of 37° C. The pharmaceutically active agent encapsulated within the spheroidal hexamer is selected from the group consisting of Depakote, Wellbutrin, Allegra, Neurontin, Zovirax, and Claritin. A process for the preparation of a hexameric complex, as described above, from a methylene-bridged tetramer solubilized in an amphiphilic organic solvent. An activator is incorporated into the amphiphilic solvent containing the tetramer.

Abstract: A guest host assembly comprising a host assembly formed of calixarene molecules and a guest component located within the host assembly. A crystallographic assembly of layers of the calixarene molecules and stacked along the crystallographic c axis of the assembly in a repeating configuration associated together predominantly by van der Waal forces. The guest component is transferable through the host assembly in a direction normal to the stacked layers. The calixarene molecules are configured in bilayers of adjacent layers along the c axis. The bilayers are shifted along the a or b axis so the assembly, relative to a corresponding assembly of the calixarene molecules without the inclusion of the guest component is shifted. The calixarene are calix(N)arenes in which N is an integer within the range of 4-8. The calixarene molecules are distally substituted with a substituent such as methyl, ethyl, propyl, butyl amyl or phenyl groups.

Abstract: Disclosed are the general principles upon which closed molecular or ionic structural frameworks may be prepared. These frameworks are based upon the self-assembly (wherein the term self-assembly refers to the association of chemical components through inter-component bonds) of n>4 subunits where surface curvature is supplied by edge sharing of subunits.

Abstract: A guest-host assembly having a generally spheroidal host assembly formed of trimers of calixarene molecules in a hexagonal close-packed assembly and its preparation. The calixarene trimers are associated together predominantly by van der Waals forces to provide dilated channels having void volumes within the range of 100-200 Å3. A guest component, such as hydrogen, methane, or another hydrocarbon or halocarbon, is encapsulated within the dilated channels of the spheroidal host assembly and retained within the channels primarily by van der Waals forces. The guest-host assembly is stable at a temperature of 150° C. or higher. The temperature at which the onset of the release of the guest component occurs is within the range of 150-300° C.

Abstract: A composition comprising a guest/host assembly having a spheroidal host assembly comprised of a hexamer of a methylene-bridged trihydroxybenzene tetramer and a guest component encapsulated within the spheroidal host assembly to provide a highly stable guest/host assembly. A guest component, specifically a pharmaceutically active agent, is encapsulated within the spheroidal host assembly to provide a guest/host assembly exhibiting a high stability, being stable upon a solubilization in a mixture of acetone and water in a one-to-one ratio for a period of one day at a temperature of 37° C. The pharmaceutically active agent encapsulated within the spheroidal hexamer is selected from the group consisting of Depakote, Wellbutrin, Allegra, Neurontin, Zovirax, and Claritin. A process for the preparation of a hexameric complex, as described above, from a methylene-bridged tetramer solubilized in an amphiphilic organic solvent. An activator is incorporated into the amphiphilic solvent containing the tetramer.

Abstract: Amphiphilic, polyhedron-shaped p-sulfonatocalix[4]arene building blocks, which have been shown previously to assemble into bilayers in an antiparallel fashion, assemble in a parallel alignment into spherical and helical tubular structures on the addition of pyridine N-oxide and lanthanide ions. The addition of greater amounts of pyridine N-oxide changed the curvature of the assembling surface and led to the formation of extended tubules. The inventive compositions and methods are useful for drug delivery and construction of nano-devices.

Abstract: This invention relates to a method of purifying afullerenes by recrystallization of a fullerene-complexing agent complex and to a fullerene-complexing agent complex.

Abstract: Calixarene derivatives, their synthesis and use as chloride channel blockers are described. Preferred calixarene derivatives are of the formula: ##STR1## wherein R is an acidic group or salt thereof, such as SO.sub.3 X or R.sup.1 SO.sub.3 X where X is H or Na, and R.sup.1 is ##STR2## where m=1-2, and R.sup.3 and R.sup.4 the same or different is each H or a C.sub.1-4 alkyl, or a nitrogen-containing group of the formula ##STR3## or A, wherein R.sup.5 is a C.sub.1-4 alkyl, R.sup.6 is a C.sub.1-4 alkyl and A is ##STR4## where R.sup.7 and R.sup.8, the same or different each is H or a C.sub.1-4 alkyl, and R.sup.9 and R.sup.10, the same or different, each is H or a C.sub.1-4 alkyl; R' is H or a C.sub.1-4 alkyl; and n is an integer of 4-8, preferably 4, 6 or 8.

Abstract: A liquid clathrate of a multidentate macromolecular compound complex salt of the formula:[M(multidentate macromolecular compound).sub.m ].sub.x [Al.sub.n R.sub.3n X].sub.y.pZwherein M is a mono-, di, or trivalent cation, R is a lower alkyl group of 1 to 8 carbon atoms, X is a monovalent, divalent or trivalent anion, n is an integer of 2 to 4, x and y are integers from 1 to 3 and m is 1 to 2, Z is an aromatic hydrocarbon compound and p is an integer from 1 to 40. The present liquid clathrate is useful in separating an aromatic hydrocarbon compound from a non-aromatic hydrocarbon compound as well as from a different aromatic hydrocarbon compound.

Abstract: The method for the liquefaction of a solid carbonaceous substance whereby the liquefaction takes place as a result of the addition of a liquid clathrate to said substance. The liquid clathrate layer then contains the liquified petroleum oil products which are then separated from the liquid clathrate.