Venable J.D.,Johnson and Johnson Pharmaceutical Research and Development L.L.C. |
Kindrachuk D.E.,Johnson and Johnson Pharmaceutical Research and Development L.L.C. |
Peterson M.L.,TransForm Pharmaceuticals Inc. |
Edwards J.P.,Johnson and Johnson Pharmaceutical Research and Development L.L.C.
Tetrahedron Letters | Year: 2010
Treatment of phenylenediamines with methyl trimethoxyacetate led to the formation of 3-methoxy-quinoxalin-2-ones with the assistance of lanthanide-based Lewis acids. © 2009 Elsevier Ltd. All rights reserved.
Popov A.,TransForm Pharmaceuticals Inc. |
Hickey M.B.,TransForm Pharmaceuticals Inc. |
Hiremath R.,TransForm Pharmaceuticals Inc. |
Peterson M.,TransForm Pharmaceuticals Inc. |
And 4 more authors.
Pharmaceutical Research | Year: 2011
Purpose: Low molecular weight hydrogelators typically require a stimulus such as heat, antisolvent, or pH adjustment to produce a gel. This study examines gelation of a novel histamine H4 receptor antagonist that forms hydrogels spontaneously at room temperature. Methods: To elucidate the mechanism and structural moieties responsible for this unusual gelation, hydrogels were characterized by rheology, optical microscopy, and XRD. SEM was performed on xerogels; NMR measurements were conducted in gelator solutions in the presence of a gel-breaker. The influence of temperature, concentration, pH, and ionic strength on elastic and viscous moduli of the hydrogels was evaluated; gel points were established via thorough rheological criteria. Results: The observed are "true" gels with a fibrillar texture and lamellar microstructure. On a molecular level, the gels are composed of aggregates of partially ionized species stabilized by hydrophobic interactions of aromatic moieties. The gel-to-sol transition occurs at physiologically relevant temperatures and is concentration-, pH-, and ionic strength-dependent. Conclusions: We hypothesize that this spontaneous gelation is due to the so-called "spring" effect, a high energy salt form that transiently increases aqueous solubility above its equilibrium limit. Upon equilibration, this supersaturated system undergoes aggregation that avoids crystallization and produces a hydrogel. © 2011 Springer Science+Business Media, LLC.
Transform Pharmaceuticals Inc. and University of South Florida | Date: 2013-05-07
Crystalline salts, polymorphs, solvates, and hydrates of bicalutamide, 5-fluorouracil, donepezil, anastrozole, nelfinavir, mirtazapine, lansoprazole, and tamsulosin, or derivatives thereof are provided by the subject invention. Methods of making and using the same are also provided.
Transform Pharmaceuticals Inc. | Date: 2014-04-30
Disclosed herein are novel polymorphs of 7-[(3-chloro-6,11-dihydro-6-methyldibenzo[c,f][1,2]thiazepin-11-yl)amino]heptanoic acid S,S-dioxide. Also described herein are novel pharmaceutical compositions comprising one or more 7-[(3-chloro-6,11-dihydro-6-methyldibenzo[c,f][1,2]thiazepin-11-yl)amino]heptanoic acid S,S-dioxide polymorphs, methods of making, and related methods of treatment.
Transform Pharmaceuticals Inc. | Date: 2011-06-29
The invention relates to methods of screening mixtures containing a pharmaceutical compound and an excipient to identify properties of the pharmaceutical compound/excipient combination that retard solid-state nucleation. The invention further relates to increasing the solubility, dissolution and bioavailability of a drug with low solubility in gastric fluids conditions by combining the drug with a precipitation retardant and an optional enhancer.
Transform Pharmaceuticals Inc, University of South Florida and University of Michigan | Date: 2010-06-02
A pharmaceutical composition comprising a co-crystal of an API and a co-crystal former; wherein the API has at least one functional group selected from ether, thioether, alcohol, thiol, aldehyde, ketone, thioketone, nitrate ester, phosphate ester, thiophosphate ester, ester, thioester, sulfate ester, carboxylic acid, phosphonic acid, phosphinic acid, sulfonic acid, amide, primary amine, secondary amine, ammonia, tertiary amine, imine, thiocyanate, cyanamide, oxime, nitrile diazo, organohalide, nitro, S-heterocyclic ring, thiophene, N-heterocyclic ring, pyrrole, O-heterocyclic ring, furan, epoxide, peroxide, hydroxamic acid, imidazole, pyridine and the co-crystal former has at least one functional group selected from amine, amide, pyridine, imidazole, indole, pyrrolidine, carbonyl, carboxyl, hydroxyl, phenol, sulfone, sulfonyl, mercapto and methyl thio, such that the API and co-crystal former are capable of co-crystallizing from a solution phase under crystallization conditions.
Transform Pharmaceuticals Inc. | Date: 2011-06-22
The present invention is directed to methods of identifying agents which affect cell state. The instant invention provides rapid and efficient methods for identifying agents which affect cell state. Methods are directed toward the screening of complex combinations of agents for their ability to affect cell state. In one embodiment, cells are incubated under suitable conditions and subjected to different agents. After an appropriate amount of time, the cells are assayed to determine what, if ant characteristics they possess. Cell characteristics can be organised in a manner such that different and novel cell states can be identified.
Transform Pharmaceuticals Inc. and University of South Florida | Date: 2010-08-23
A polymorph of aspirin is provided by the present invention. Methods of making and using the same are also provided.
PubMed | TransForm Pharmaceuticals Inc.
Type: | Journal: Annals of the New York Academy of Sciences | Year: 2010
Interleukin (IL)-12 and IL-23 are related cytokines that have been implicated in the pathogenesis of several immune-mediated disorders. IL-12 and IL-23 are heterodimers made up of a common p40 subunit complexed to unique p35 (IL-12) or p19 (IL-23) subunits. Ustekinumab is a human monoclonal antibody that specifically binds the p40 subunit of IL-12/23. Ustekinumab prevents IL-12 and IL-23 from binding their cell surface receptor complexes, thereby blocking the T helper (Th) 1 (IL-12) and Th17 (IL-23) inflammatory pathways. Here, we discuss the preclinical and human translational data supporting a role for IL-12/23 in the pathogenesis of immune-mediated disorders, and how that rationale was challenged in the clinic during the course of the ustekinumab development program in several indications including psoriasis, psoriatic arthritis, Crohns disease, and multiple sclerosis. We review the key efficacy and safety data in each of these immune-mediated diseases and compare and contrast the safety lessons learned from IL-12/23 genetically-deficient mice and humans in context of the overall clinical trial experience with ustekinumab.