Patent classifications
C07D295/125
Kappa opioid agonists and uses thereof
Provided are compounds of Formula I: ##STR00001##
and pharmaceutically acceptable salts and solvates thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are as described herein. The compounds of Formula I are agonists of the kappa opioid receptor and relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry.
Method for preparing pyrazolecarboxylic acid derivative, and intermediate thereof
Provided are a preparation method for synthesizing a pyrazolecarboxylic acid derivative of the following formula (I), which is suitable for industrial production, and an intermediate as shown by the following formula (II). The method is high in reaction yield in each step, low in waste gas and waste water and low in cost, and requires no special reaction equipment. ##STR00001##
Method for preparing pyrazolecarboxylic acid derivative, and intermediate thereof
Provided are a preparation method for synthesizing a pyrazolecarboxylic acid derivative of the following formula (I), which is suitable for industrial production, and an intermediate as shown by the following formula (II). The method is high in reaction yield in each step, low in waste gas and waste water and low in cost, and requires no special reaction equipment. ##STR00001##
Electronic device and compound
The invention relates to an electronic device comprising a compound having Formula (1): AB.sub.x (1), wherein A is a structural moiety that consists of at least two atoms and comprises a conjugated system of delocalized electrons, each B is independently selected from an imine functional group (1a), wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 are independently selected from C.sub.1-C.sub.30 alkyl, C.sub.2-C.sub.30 alkenyl, C.sub.2-C.sub.3 alkinyl, C.sub.3-C.sub.30 cycloalkyl, C.sub.6-C.sub.30 aryl, C.sub.2-C.sub.30 heteroaryl, C.sub.7-C.sub.30 arylalkyl, C.sub.3-C.sub.30 heteroarylalkyl, the wave line represents a covalent bond to the imine nitrogen atom, G is in each group (1a) independently selected from a quarternary carbon atom and from a cyclopropenylidene structural moiety, x is an integer equal one or higher, preferably equal two or higher, and the lone electron pair of the imine nitrogen atom and/or the pi-electrons of the imine double bond of at least one group B is conjugated with the conjugated system of delocalized electrons comprised in the structural moiety A, with the proviso that two or more of the substituents R.sup.1, R.sup.2, R.sup.3, R.sup.4 may be connected to form a ring that may contain also unsaturation and, if any of the substituents R.sup.1, R.sup.2, R.sup.3, R.sup.4 comprises two or more carbon atoms, up to one third of the overall count of the carbon atoms in the substituent or in any ring formed by two connected substituents can be replaced with heteroatoms independently selected from O, S, N and B as well as to an electrically semiconducting material and a compound for use in the electronic device. ##STR00001##
Electronic device and compound
The invention relates to an electronic device comprising a compound having Formula (1): AB.sub.x (1), wherein A is a structural moiety that consists of at least two atoms and comprises a conjugated system of delocalized electrons, each B is independently selected from an imine functional group (1a), wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 are independently selected from C.sub.1-C.sub.30 alkyl, C.sub.2-C.sub.30 alkenyl, C.sub.2-C.sub.3 alkinyl, C.sub.3-C.sub.30 cycloalkyl, C.sub.6-C.sub.30 aryl, C.sub.2-C.sub.30 heteroaryl, C.sub.7-C.sub.30 arylalkyl, C.sub.3-C.sub.30 heteroarylalkyl, the wave line represents a covalent bond to the imine nitrogen atom, G is in each group (1a) independently selected from a quarternary carbon atom and from a cyclopropenylidene structural moiety, x is an integer equal one or higher, preferably equal two or higher, and the lone electron pair of the imine nitrogen atom and/or the pi-electrons of the imine double bond of at least one group B is conjugated with the conjugated system of delocalized electrons comprised in the structural moiety A, with the proviso that two or more of the substituents R.sup.1, R.sup.2, R.sup.3, R.sup.4 may be connected to form a ring that may contain also unsaturation and, if any of the substituents R.sup.1, R.sup.2, R.sup.3, R.sup.4 comprises two or more carbon atoms, up to one third of the overall count of the carbon atoms in the substituent or in any ring formed by two connected substituents can be replaced with heteroatoms independently selected from O, S, N and B as well as to an electrically semiconducting material and a compound for use in the electronic device. ##STR00001##
BCL-3 INHIBITORS
The present application relates to compounds of any one of Formulae I, Ia, Ib, Ic, Id, Ie, and If. Compounds of Formula I have the structure:
##STR00001## wherein A, B, Y, Z, R.sup.2, R.sup.4, R.sup.5, R.sup.6, R.sup.q and q are as defined herein. The compounds can be used as inhibitors of Bcl-3 and can be used for the treatment of cancer, particularly metastatic cancer.
BCL-3 INHIBITORS
The present application relates to compounds of any one of Formulae I, Ia, Ib, Ic, Id, Ie, and If. Compounds of Formula I have the structure:
##STR00001## wherein A, B, Y, Z, R.sup.2, R.sup.4, R.sup.5, R.sup.6, R.sup.q and q are as defined herein. The compounds can be used as inhibitors of Bcl-3 and can be used for the treatment of cancer, particularly metastatic cancer.
Anti-fibrotic pyridinones
Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
Anti-fibrotic pyridinones
Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
Bioreducible Poly (Beta-Amino Ester)s For siRNA Delivery
Degradable polymers were synthesized that self-assemble with nucleic acids, proteins, hydrophobic drugs, and other small molecules to form particles that are effective for delivery into a cell, tissue and/or organism either in vitro or in vivo. The presently disclosed polymers demonstrate differential cell-type specificity, an ability to promote endosomal escape to protect the cargos from degradation and enhance delivery to the cytoplasm, and/or bioreducibility, which enables triggered intracellular drug release to be tuned to promote optimal delivery to the target cell type. The presently disclosed materials may be used to treat a wide variety of conditions or diseases, such as cancer, cardiovascular diseases, infectious diseases, and ophthalmic diseases.