Patent classifications
C07C2602/20
OPEN-FLASK HYDROBORATION AND THE USE THEREOF
The present disclosure generally relates to a process for hydroboration of an alkene or alkyne using ammonia borane (AB). In particular, the present invention relates to hydroboration of an alkene or alkyne in the presence of air or moisture, and a clean process for facile preparation of an alcohol by oxidizing the organoborane so formed with hydrogen peroxide. The products, including aminodialkylboranes, ammonia trialkylborane complexes, as well as various alcohols so prepared, are within the scope of this disclosure.
RADIATION-SENSITIVE COMPOSITION, PATTERN FORMATION METHOD, AND PHOTO-DEGRADABLE BASE
A radiation-sensitive composition contains a polymer having an acid-releasable group, and a compound (Q) represented by formula (1). In the formula (1), L.sup.1 represents an ester group, CONR.sup.3, a (thio)ether group, or a sulfonyl group. R.sup.4 represents a hydrogen atom, a substituted or unsubstituted C1 to C20 monovalent hydrocarbon group, a halogen atom, a hydroxy group, or a nitro group. R.sup.5 represents a C1 to C20 monovalent hydrocarbon group, a C1 to C20 monovalent halogenated hydrocarbon group, or a halogen atom, and optionally two R.sup.5s taken together represent an alicyclic structure together with the carbon atom(s) between the two R.sup.5s. L.sup.2 represents a single bond or a divalent linking group.
##STR00001##
SULFIDE ALKYL COMPOUNDS FOR HBV TREATMENT
The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
N-substituted benzamides and methods of use thereof
The invention provides novel compounds having the general formula: ##STR00001##
and pharmaceutically acceptable salts thereof, wherein the variables R.sup.A, subscript n, ring A, X.sup.2, L, subscript m, X.sup.1, B, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.N have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
γ-aminobutyric acid (GABA) analogues for the treatment of pain and other disorders
A compound of Formula 1 ##STR00001## wherein R.sub.1 represents hydrogen, halo, a C1-C4 alkyl group, a C1-C4 alkylhalide group, a C1-C4 alkoxy-C2-C4 alkyl group, a C2-C4 alkenyl group, a C2-C4 alkynyl group or a C3-C7 cycloalkyl group; R.sub.2 represents ##STR00002##
or a tautomer thereof; and R.sub.3 represents hydrogen, a C1-C4 alkyl group, a C1-C4 alkoxy-C2-C4 alkyl group or a C3-C7 cycloalkyl group; or a pharmaceutically acceptable salt or solvate thereof. Processes to prepare said compounds and novel intermediates are also claimed. Such compound finds utility in treating neuropathic pain and disorders of the central nervous system.
METHOD OF SYNTHESIS
Described is a method of synthesizing 6-(5-ethoxyhept-1-yl)bicyclo[3.3.0] octan-3-one by reacting 3-(5-ethoxyhept-1-yl) cyclopentane with dichloroketene. The resulting reaction products are reacted with acetic acid and zinc to produce 4-(5-ethoxyhept-1-yl)bicyclo[3.2.0]heptan-6-one and 4-(5-ethoxyhept-1-yl)bicyclo [3.2.0]heptan-7-one, which are reacted with trimethylsulfonium iodide to produce 2-(5-ethoxyhept-1-yl)spiro[bicyclo[3.2.0]heptane-6,2-oxirane] and 4-(5-ethoxyhept-1-yl)spiro-[bicyclo-[3.2.0]heptane-6,2-oxirane]. Lithium iodide is reacted with 2-(5-ethoxyhept-1-yl)spiro[bicyclo[3.2.0]heptane-6,2-oxirane] and 4-(5-ethoxyhept-1-yl)spiro-[bicyclo-[ 3.2.0]heptane-6,2-oxirane] to produce 6-(5-ethoxyhept-1-yl)bicyclo[3.3.0]octan-3-one. A method of synthesizing 6-(5-methoxyhept-1-yl)bicyclo[3.3.0]octan-3-one is also described.
BICYCLO [3.2.0] HEPTANE BIS(AMIDE) RXFP1 AGONISTS
The disclosure relates to compounds of Formula (I), which are RXFP1 receptor agonists, compositions containing them, and methods of using them, for example, in the treatment of heart failure, fibrotic diseases, and related diseases such as lung disease (e.g., idiopathic pulmonary fibrosis), kidney disease (e.g., chronic kidney disease), or hepatic disease (e.g., non-alcoholic steatohepatitis and portal hypertension).
##STR00001##
γ-aminobutyric acid (GABA) analogues for the treatment of pain and other disorders
A compound of Formula (1) wherein R.sub.1 represents hydrogen, halo, a C1-C4 alkyl group, a C1-C4 alkylhalide group, a C1-C4 alkoxy-C2-C4 alkyl group, a C2-C4 alkenyl group, a C2-C4 alkynyl group or a C3-C7 cyclo alkyl group; R.sub.2 represents Formula (1) or Formula (1) a tautomer thereof; and R.sub.3 represents hydrogen, a C1-C4 alkyl group, a C1-C4 alkoxy-C2-C4 alkyl group or a C7 cyclo alkyl group; or a pharmaceutically acceptable salt or solvate thereof. Processes to prepare said compounds and novel intermediates are also claimed. Such compound finds utility in treating neuropathic pain and disorders of the central nervous system. ##STR00001##
Sulfide alkyl compounds for HBV treatment
The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
NOVEL GAMMA-AMINOBUTYRIC ACID (GABA) ANALOGUES FOR THE TREATMENT OF PAIN AND OTHER DISORDERS
A compound of Formula 1
##STR00001## wherein R.sub.1 represents hydrogen, halo, a C1-C4 alkyl group, a C1-C4 alkylhalide group, a C1-C4 alkoxy-C2-C4 alkyl group, a C2-C4 alkenyl group, a C2-C4 alkynyl group or a C3-C7 cycloalkyl group; R.sub.2 represents
##STR00002##
or a tautomer thereof; and R.sub.3 represents hydrogen, a C1-C4 alkyl group, a C1-C4 alkoxy-C2-C4 alkyl group or a C3-C7 cycloalkyl group; or a pharmaceutically acceptable salt or solvate thereof.
Processes to prepare said compounds and novel intermediates are also claimed. Such compound finds utility in treating neuropathic pain and disorders of the central nervous system.