Patent classifications
C07D263/14
OXAZOLINE COMPOUND, SYNTHESIS METHOD THEREFOR AND APPLICATION THEREOF
Disclosed are an oxazoline compound, a synthesis method therefor and an application thereof. The oxazoline compound has a structure represented by formula (I), wherein in the formula (I), R is selected from groups represented by formula (I-1), formula (I-2), and formula (I-3), where an oxazoline derivative having a novel molecular structure is obtained by introducing a nitrogen heterocycle, an ether bond or a sulfonate structure into the oxazoline compound. The oxazoline derivative is useful in the field of agricultural protection, and has higher acaricidal activity than etoxazole, can inhibit the synthesis of chitin from mites, and can effectively control the embryogenesis and development of eggs of Tetranychus cinnabarinus, as well as the ecdysis process from larvae to adults, and therefore has a significant effect in killing mite eggs and larvae.
##STR00001##
Diamine derivatives as inhibitors of leukotriene A4 hydrolase
This invention is directed to compounds of formula (I): ##STR00001##
where r, q, R, R.sup.2, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.5c, R.sup.6a, R.sup.6b, R.sup.6c, R.sup.7, R.sup.8, and R.sup.9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A.sub.4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
Diamine derivatives as inhibitors of leukotriene A4 hydrolase
This invention is directed to compounds of formula (I): ##STR00001##
where r, q, R, R.sup.2, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.5c, R.sup.6a, R.sup.6b, R.sup.6c, R.sup.7, R.sup.8, and R.sup.9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A.sub.4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
METHODS FOR PREPARING FLORFENIOL AND INTERMEDIATE THEREOF
The present invention discloses a method for preparing florfenicol and its intermediate (V), comprising an addition reaction, a ring closure reaction, a hydrolysis reaction, a ring opening reaction, a reduction reaction, a ring reaction, a fluorination reaction and a ring opening reaction. In the present method for preparing florfenicol, respective reaction steps can be continuously operated, therefore the methods of the present invention features simplified process and shorter synthetic route, and obtained florfenicol has high chiral purity and is of high yield. The method of the present invention for preparing florfenicol (TM) using the intermediate (V) avoids waste water pollution and reduces the cost for treating wastewater and alleviates environmental pollution. At the same time, the methods of the present invention eliminates a chiral resolution procedure, thus increasing the utilization rate of atoms in the reaction. As a result, cost is reduced and process is simplified.
Polymers and Lubricating Compositions Containing Polymers
A polymer comprising units having the structure (I):
##STR00001##
wherein x is 2 or 3, wherein L is (CH.sub.2).sub.y, where y is an integer from 1 to 10, or wherein L is CH(CH.sub.3)CH.sub.2S(CH.sub.2).sub.z, where z is an integer from 1 to 5; wherein [Q] is absent or is a polymerised moiety consisting of units having the structure (II):
##STR00002##
wherein R is a hydrocarbyl group, or a hydrocarbyl group containing one or more heteroatoms, wherein R may be linear, branched or cyclic, saturated or unsaturated, and wherein R has from 1 to 30 carbon atoms; wherein [Q] either consists of identical units of structure (II), or wherein [Q] consists of more than one different units of structure (II), differing in group R; and wherein X is a halogen or another chain terminating group. The polymers may find use as additives in lubricating compositions where they provide friction improvement and wear reduction.
Polymers and Lubricating Compositions Containing Polymers
A polymer comprising units having the structure (I):
##STR00001##
wherein x is 2 or 3, wherein L is (CH.sub.2).sub.y, where y is an integer from 1 to 10, or wherein L is CH(CH.sub.3)CH.sub.2S(CH.sub.2).sub.z, where z is an integer from 1 to 5; wherein [Q] is absent or is a polymerised moiety consisting of units having the structure (II):
##STR00002##
wherein R is a hydrocarbyl group, or a hydrocarbyl group containing one or more heteroatoms, wherein R may be linear, branched or cyclic, saturated or unsaturated, and wherein R has from 1 to 30 carbon atoms; wherein [Q] either consists of identical units of structure (II), or wherein [Q] consists of more than one different units of structure (II), differing in group R; and wherein X is a halogen or another chain terminating group. The polymers may find use as additives in lubricating compositions where they provide friction improvement and wear reduction.
Max binders as MYC modulators and uses thereof
The present disclosure provides compounds of Formula (I), Formula (I), Formula (II), Formula (II-A), Formula (III), and Formula (IV). The compounds described herein are MAX binders and/or modulators of Myc, Mad, or Mxi1 (e.g., inhibitors of Myc, Mad, or Mxi1), and may be useful in treating a subject with a disease associated with Myc, such as proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions and kits including the compounds described herein, as well as methods of using and uses of the compounds, compositions, and kits. ##STR00001##
DIAMINE DERIVATIVES AS INHIBITORS OF LEUKOTRIENE A4 HYDROLASE
This invention is directed to compounds of formula (I):
##STR00001##
where r, q, R, R.sup.2, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.5c, R.sup.6a, R.sup.6b, R.sup.6c, R.sup.7, R.sup.8, and R.sup.9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A.sub.4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
DIAMINE DERIVATIVES AS INHIBITORS OF LEUKOTRIENE A4 HYDROLASE
This invention is directed to compounds of formula (I):
##STR00001##
where r, q, R, R.sup.2, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.5c, R.sup.6a, R.sup.6b, R.sup.6c, R.sup.7, R.sup.8, and R.sup.9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A.sub.4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
NOVEL CAPSAICIN ANALOGS AND USES THEREOF
The present invention provides compositions comprising compounds having formulas (I), (II) or
##STR00001## and additionally provides methods for the use thereof in the treatment of various disorders including neurological disorders, cancer, diabetes, and obesity, wherein R1-R7, X, A, and Q in (I), R1-R15 in (II) and R1-R15 in (III) are as defined herein. In certain embodiments, methods for the treatment of various disorders including pain and cancer comprise topically, locally or systemically (e.g., IV, IP or orally) administering to a subject in need thereof a therapeutically effective amount of a compound of formulas (I), (II) or (III).