Patent classifications
C07D491/02
Furanone derivative
To provide a novel furanone derivative, and a medicine including the same. The furanone derivative is represented by the formula (I): ##STR00001##
wherein A represents COOR1 or a hydrogen atom; R1 represents a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocycle; R2 and R3 are the same or different and each independently represent a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted phenyl group, an optionally substituted heterocycle, an optionally substituted heterocyclic fused ring, or an optionally substituted amino group; or alternatively, R2 and R3, taken together with the nitrogen atom to which they are attached, may form an optionally substituted heterocycle or an optionally substituted heterocyclic fused ring; and R4 represents a hydrogen atom or a halogen atom; with the proviso that when A represents COOR1, R2 and R3 are not optionally substituted amino groups at the same time, and when A represents a hydrogen atom, R3 represents a hydrogen atom.
Ron inhibitors for use in preventing and treating bone loss
Provided herein are methods for inhibiting osteolysis or treating osteoporosis in a subject in need thereof, the method including administering to the subject at least one RON inhibitor. The osteolysis may be caused by a condition selected from the group consisting of cancer, inflammation, and cyst. The condition may include a bone tumor or a tumor located in bone. The subject may have been diagnosed with bone cancer. The inhibitor may be ASLAN002. The inhibitor may be OSI-296. The inhibitor may be selective or specific for RON. The inhibitor may not depend on the function of RANKL or TGF.
Substituted quinolizine derivatives useful as HIV integrase inhibitors
The present invention relates to Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.9 and R.sup.10 are as defined herein. The present invention also relates to compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject. ##STR00001##
BIFLUORODIOXALANE-AMINO-BENZIMIDAZOLE KINASE INHIBITORS FOR THE TREATMENT OF CANCER, AUTOIMMUNEINFLAMMATION AND CNS DISORDERS
The invention relates to a compound of the general formula (I) or a physiologically functional derivative, solvate or salt thereof,
##STR00001##
wherein
A is a bond, alkyl or alkoxy optionally substituted with one or more R as defined herein, *N(R)CO, *CON(R), *N(R)CON(R), S, SO, *N(R), *N(R)CO, *CON(R), CO, *COO, *OOC, *SO.sub.2N(R), SO.sub.2, or *N(R)SO.sub.2, wherein R is as defined herein and * specifies the point of attachment to X; X is aryl, cycloalkyl, aralkyl, heterocyclyl or heteroaryl, which may be substituted with one or more R.sup.X further described herein; L is a bond or *N(R.sup.N)CO, *CON(R.sup.N), *N(R.sup.N), *CN(R.sup.N), *N(R.sup.N)-alkyl-, *-alkyl-N(R.sup.N), *N(R.sup.N)CON(R.sup.N), *CO, *CO.sub.2, alkyl, *-alkyl-O-alkyl-, *NCOCHCH, *CHCHCONH, *SO.sub.2N(R.sup.N), *N(R.sup.N)SO.sub.2, or heterocyclyl, wherein * specifies the point of attachment to X; Y is H, alkyl, aryl, aralkyl, cycloalkyl, heterocyclyl or heteroaryl, which may be substituted with one or more R.sup.Y further described herein; and R and R.sup.N are further described herein; as well as their use as a medicament, a pharmaceutical composition comprising them, a method of treatment or prevention of a medical condition entailing the administration thereof, and the use thereof in the manufacture of a medicament for the treatment or prevention of a medical condition, particularly autoimmune inflammatory disorders, CNS disorders, sleeping disorders, or proliferative diseases including cancer. The invention further relates to a specific process for the preparation of said compounds.
Enantiomers of the 1′,6′-isomer of neplanocin A
Enantiomers of 1,6-isoneplanocin, including derivatives of the enantiomers of 1,6-isoneplanocin, are disclosed along with novel synthetic methods. In particular, a substituted cyclopentane epoxide is synthesized into the enantiomers of 1,6-isoneplanocin. Enantiomers of carbocyclic nucleoside analogs of 3-deazaneplanocin to provide D- and L-like 1,6-iso-3-deazaneplanocin are also disclosed. The small molecule chemotherapeutic compounds beneficially provide DNA and RNA antiviral activity, demonstrating activity towards, for example, human cytomegalovirus, measles, Ebola, norovirus, dengue, vaccinia and HBV. Compounds exhibiting reduced S-adenosylhomocysteine hydrolase inhibitory effects are disclosed and provide improved toxicity profiles in comparison to neplanocin. The invention provides improved prophylactic and/or therapeutic antiviral efficacy.
Substituted pyrazolylpyrazole derivative and use of same as herbicide
Provided is a compound capable of effectively control worst weeds of higher leaf stages that present practical problems. A specific pyrazolylpyrazole derivative of formula (I) is disclosed that is able to solve the above-mentioned problems. ##STR00001##
Bifluorodioxalane-amino-benzimidazole kinase inhibitors for the treatment of cancer, autoimmuneinflammation and CNS disorders
The invention relates to a compound of the general formula (I) or a physiologically functional derivative, solvate or salt thereof, ##STR00001##
wherein A, X, L, Y, R, and R.sup.N are as defined herein. The invention further relates to the use of the compounds of formula (I) as a medicament, a pharmaceutical composition comprising them, a method of treatment or prevention of a medical condition entailing the administration thereof, and the use thereof in the manufacture of a medicament for the treatment or prevention of a medical condition, particularly autoimmune inflammatory disorders, CNS disorders, sleeping disorders, or proliferative diseases including cancer. The invention further relates to a specific process for the preparation of said compounds.
Bifluorodioxalane-amino-benzimidazole kinase inhibitors for the treatment of cancer, autoimmuneinflammation and CNS disorders
The invention relates to a compound of the general formula (I) or a physiologically functional derivative, solvate or salt thereof, ##STR00001##
wherein A, X, L, Y, R, and R.sup.N are as defined herein. The invention further relates to the use of the compounds of formula (I) as a medicament, a pharmaceutical composition comprising them, a method of treatment or prevention of a medical condition entailing the administration thereof, and the use thereof in the manufacture of a medicament for the treatment or prevention of a medical condition, particularly autoimmune inflammatory disorders, CNS disorders, sleeping disorders, or proliferative diseases including cancer. The invention further relates to a specific process for the preparation of said compounds.
6-arylamino pyridone carboxamide as MEK inhibitors
The invention provides novel substituted 6-arylamino pyridone carboxamides represented by Formula I, or a pharmaceutically acceptable salt, solvate, poly-morph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans. ##STR00001##
Histone deacetylase inhibitors
This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).