Patent classifications
C07D305/14
Docetaxel-Aconitic Anhydride conjugate exhibiting anti-tumor activity without in vivo toxicity
Synthesizing a docetaxel-aconitic anhydride conjugate using docetaxel, including: mixing aconitic anhydride with a chlorinating reagent to produce a first mixture; dissolving the first mixture in an organic solvent to produce a dissolved mixture; stirring the dissolved mixture; evaporating the organic solvent from the dissolved mixture to produce a second mixture; washing the second mixture with an impurity remover to remove impurities and to produce an aconitic anhydride chloride solution; and mixing the docetaxel with the produced aconitic anhydride chloride solution to produce the docetaxel-aconitic anhydride conjugate.
INTEGRATED METHODS AND SYSTEMS FOR PRODUCING AMIDE AND NITRILE COMPOUNDS
Provided herein are integrated methods and systems for the production of acrylamide and acrylonitrile compounds and other compounds from at least beta-lactones and/or beta-hydroxy amides.
NAMPT MODULATORS
Provided are compounds of Formula (II) or a pharmaceutically acceptable salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and p are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula (II), or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula (II), or a pharmaceutically acceptable salt thereof.
##STR00001##
NAMPT MODULATORS
Provided are compounds of Formula (II) or a pharmaceutically acceptable salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and p are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula (II), or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula (II), or a pharmaceutically acceptable salt thereof.
##STR00001##
NOVEL PEG DERIVATIVE
Provided is a new therapeutic agent for a malignant tumor, which is highly safe, sustains an antitumor effect, and can improve the means for administration and the number of times of administration. Disclosed is a compound of Formula (1), or a salt thereof:
C[CH.sub.2O(CH.sub.2CH.sub.2O).sub.nCH.sub.2CO—R.sup.1—R.sup.2].sub.4 (1) wherein R.sup.1 represents a single bond, —N(R.sup.3)(CH.sub.2).sub.n1CO—, or —N(R.sup.4)(CH.sub.2).sub.n2N (R.sup.5)CO(CH.sub.2).sub.n3CO—; R.sup.2 represents a group of Formula (a), (b), (c), (d), (e), or (f):
##STR00001## ##STR00002## m represents a number of from 10 to 1,000; and an arrow represents a bonding site.
LIPIDS FOR DELIVERY OF NUCLEIC ACID SEGMENTS
Disclosed herein are compounds of Formula (I), Formula (III) or Formula (IIIa), or pharmaceutically acceptable salts thereof, wherein A, L, X.sup.1, X.sup.2, a, b, R.sup.1 and R.sup.2 are as defined herein. Also disclosed are lipid nanoparticles comprising a compound of Formula (I), Formula (III) or Formula (IIIa), or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a plurality of lipid nanoparticles comprising a compound of Formula (I), Formula (III) or Formula (IIIa), or a pharmaceutically acceptable salt thereof and a nucleic acid segment; as well as methods for delivering a nucleic acid segment comprising administering a plurality of lipid nanoparticles comprising a compound of Formula (I), Formula (III) or Formula (IIIa), or a pharmaceutically acceptable salt thereof, and a nucleic acid segment.
LIPIDS FOR DELIVERY OF NUCLEIC ACID SEGMENTS
Disclosed herein are compounds of Formula (I), Formula (III) or Formula (IIIa), or pharmaceutically acceptable salts thereof, wherein A, L, X.sup.1, X.sup.2, a, b, R.sup.1 and R.sup.2 are as defined herein. Also disclosed are lipid nanoparticles comprising a compound of Formula (I), Formula (III) or Formula (IIIa), or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a plurality of lipid nanoparticles comprising a compound of Formula (I), Formula (III) or Formula (IIIa), or a pharmaceutically acceptable salt thereof and a nucleic acid segment; as well as methods for delivering a nucleic acid segment comprising administering a plurality of lipid nanoparticles comprising a compound of Formula (I), Formula (III) or Formula (IIIa), or a pharmaceutically acceptable salt thereof, and a nucleic acid segment.
9, 10-α, α-oh-taxane analogs and methods for production thereof
Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G′ or Formula M′: ##STR00001##
with a second compound of generalized formula R.sub.8R.sub.9C(OCH.sub.3).sub.2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R.sub.1 and R.sub.2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R.sub.7 is an alkyl group, an olefinic group, or an aromatic group; P.sub.1 is a hydroxyl protecting group; P.sub.5 is H or an acid labile protecting group at the 7-O position; R.sub.8 is H, alkyl group, olefinic or aromatic group; and R.sub.9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.
9, 10-α, α-oh-taxane analogs and methods for production thereof
Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G′ or Formula M′: ##STR00001##
with a second compound of generalized formula R.sub.8R.sub.9C(OCH.sub.3).sub.2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R.sub.1 and R.sub.2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R.sub.7 is an alkyl group, an olefinic group, or an aromatic group; P.sub.1 is a hydroxyl protecting group; P.sub.5 is H or an acid labile protecting group at the 7-O position; R.sub.8 is H, alkyl group, olefinic or aromatic group; and R.sub.9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.
Integrated methods and systems for producing amide and nitrile compounds
Provided herein are integrated methods and systems for the production of acrylamide and acrylonitrile compounds and other compounds from at least beta-lactones and/or beta-hydroxy amides.