Patent classifications
C07F9/65522
Functionalizing nanofibres
Methods for functionalizing the surface of nanofiber substrates, including electrospun fibers and non-woven or woven mats of fibers are described. Functionalized nanofiber substrates presenting biologically active moieties such as biotin and saccharides are described.
PRODRUGS OF TETRAHYDROCANNABINOL, COMPOSITIONS COMPRISING PRODRUGS OF TETRAHYDROCANNABINOL AND METHODS OF USING THE SAME
Described herein are ?.sup.9-THC prodrugs, methods of making ?.sup.9-THC prodrugs, formulations comprising ?.sup.9-THC prodrugs and methods of using ?.sup.9-THC. One embodiment described herein relates to the transdermal administration of a ?.sup.9-THC prodrug for treating and preventing diseases and/or disorders.
Dyes with phosphinic acid, phosphinate, phosphonate and phosphonamidate substituents as auxochromic groups and methods for preparing the same
Compounds of formula I are disclosed: ##STR00001##
wherein X.sup.1, X.sup.2, X.sup.3, X.sup.4 are independently H, F, Cl, Br, I, CN, NO.sub.2, OR.sup.1, SR.sup.1, NR.sup.1R.sup.2, COR.sup.1, COOR.sup.1, CONR.sup.1R.sup.2, PO.sub.3R.sup.1R.sup.2, SO.sub.2R.sup.1, SO.sub.3R.sup.1 or R.sup.3; R.sup.1 and R.sup.2 are, e.g., H, alkyl or aryl or optionally a ring; R.sup.3 is, e.g., alkyl, alkenyl, alkynyl, aryl or cycloalkyl; Y is OR.sup.1, NR.sup.1R.sup.2, or NR.sup.1R.sup.3; Q is O, S, SO.sub.2, NR, C(R.sup.3).sub.2, Si(R.sup.3).sub.2, Ge(R.sup.3).sub.2, P(O)R.sup.3 or P(O)OR.sup.3; Q and X.sup.1 can optionally form part of a ring; L and M are independently OR.sup.1, SR.sup.1, NR.sup.1R.sup.2 and R.sup.3; L and M can optionally form part of a ring; Z is O, S, NR.sup.1, CR.sup.1R.sup.3 or aryl; and Z and X.sup.4 can optionally form part of a ring.
Substituted bicyclic compounds
Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): ##STR00001##
and/or a salt thereof, wherein R.sub.1 is OH or OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
ANTIBODY-NANOPARTICLE CONJUGATES AND METHODS FOR MAKING AND USING SUCH CONJUGATES
Disclosed herein are antibody-nanoparticle conjugates that include two or more nanoparticles (such as gold, palladium, platinum, silver, copper, nickel, cobalt, iridium, or an alloy of two or more thereof) directly linked to an antibody or fragment thereof through a metal-thiol bond. Methods of making the antibody-nanoparticle conjugates disclosed herein include reacting an arylphosphine-nanoparticle composite with a reduced antibody to produce an antibody-nanoparticle conjugate. Also disclosed herein are methods for detecting a target molecule in a sample that include using an antibody-nanoparticle conjugate (such as the antibody-nanoparticle conjugates described herein) and kits for detecting target molecules utilizing the methods disclosed herein.
N-HYDROXYFORMAMIDE COMPOUNDS AND COMPOSITIONS COMPRISING THEM FOR USE AS BMP l, TLL1 AND/OR TLL2 INHIBITORS
Compounds of Formulas (I) and (II):
##STR00001##
and salts thereof; methods of making and using the same, including use for inhibiting BMP1, TLL1 and/or TLL2 and in treatment of diseases associated with BMP1, TLL1 and/or TLL2 activity.
BETA-LACTAMASE INHIBITORS, FORMULATIONS, AND USES THEREOF
Provided herein are heterocyclic compounds and pharmaceutical formulations that can be used to treat bacterial infections. Also provided herein are methods of making and using the heterocyclic compounds and pharmaceutical formulations.
siRNA DELIVERY VECTOR
There is provided a complex of a 6,7-dihydroxy coumarin phosphonium amphiphile together with a negatively charged agent. The complex self-assembles into a nanoparticle or non-viral vector for facilitating delivery of the negatively charged agent. The negatively charged agent may be a therapeutic agent or a diagnostic agent. Thus, the present invention provides a method of delivery of such negatively charged agents to a target cell, and in particular facilitates delivery of a therapeutic or diagnostic agent across the plasma membrane, as well as a method of treatment or diagnosis via delivery of the therapeutic or diagnostic agent. The 6,7-dihydroxy coumarin phosphonium amphiphile can be Mito-Esc and the negatively charged agent can be a nucleic acid such as siRNA. Additionally, the 6,7-dihydroxy coumarin phosphonium amphiphile is believed to be effective in the treatment of cancer.
Organic Semiconductive Layer Comprising Phosphine Oxide Compounds
The present invention relates to an. organic semiconductive layer which is an electron transport layer and/or an electron injection layer and/or an n-type charge generation layer, the organic semiconductive layer comprising at least one compound of formula (1) wherein R.sup.1 and R.sup.2 are each independently selected from C.sub.1 to C.sub.16 alkyl; Ar.sup.1 is selected from C.sub.6 to C.sub.14 arylene or C.sub.3 to C.sub.12 heteroarylene; Ar.sup.2 is independently selected from C.sub.14 to C.sub.40 arylene or C.sub.8 to C.sub.40 heteroarylene; R.sup.3 is independently selected from H, C.sub.1 to C.sub.12 alkyl or C.sub.10 to C.sub.20 aryl; wherein each of Ar.sup.1, Ar.sup.2 and R.sup.3 may each independently be unsubstituted or substituted with at least one C.sub.1 to C.sub.12 alky group; n is 0 or 1; and m is 1 in case of n=0; and m is 1 or 2 in case of n=1, phosphine oxide compounds comprised therein and to organic electroluminescent devices comprising such layers and compounds.
##STR00001##
HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF SUMO ACTIVATING ENZYME
Disclosed are chemical entities which are compounds of formula (I):
##STR00001##
or pharmaceutically acceptable salts thereof; wherein Y, R.sup.a, R.sup.a, R.sup.b, R.sup.c, X.sub.1, X.sub.2, X.sub.3, R.sup.d, Z.sub.1, and Z.sub.2 have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry. Chemical entities according to the disclosure can be useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular, and neurodegenerative diseases or disorders.