Patent classifications
C07D409/06
COMPOUND HAVING LYSOPHOSPHATIDIC ACID RECEPTOR AGONIST ACTIVITY AND PHARMACEUTICAL USE THEREOF
A pharmaceutical containing a compound having an agonist activity for LPA3 as an active ingredient, wherein the compound is of formula (IY):
##STR00001##
wherein all symbols represent the same meaning as described in the specification, and which is useful as a preventive and/or therapeutic agent for, e.g., essential thrombocythemia or reactive thrombocytosis.
Aryl hydrocarbon receptor modulators
The disclosure discloses an aryl hydrocarbon receptor modulators of formula (I), and pharmaceutically acceptable salts, ##STR00001## R′ is H, CN, CH.sub.2(OH)R.sub.0, C.sub.mH.sub.2m+1, C.sub.nH.sub.2n-1, C.sub.nH.sub.2n-3, ##STR00002##
two R.sub.a is independently H, or two R.sub.a together form ═O or ═N—W.sub.3—R.sub.1; A is a C.sub.6 to C.sub.10 aromatic ring, or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom from N, O and S, or 4 to 7 membered non-aromatic heterocyclic ring containing 1 to 3 heteroatom from N, O and S and C═N, which are with no substituent or substituted by 1 or 3 R; Q is R, or a C.sub.6 to C.sub.10 aromatic ring or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom selected from N, O and S, which are with no substituent or substituted by 1 or 3 R; R is R.sub.c connected with C or R.sub.N connected with N.
Aryl hydrocarbon receptor modulators
The disclosure discloses an aryl hydrocarbon receptor modulators of formula (I), and pharmaceutically acceptable salts, ##STR00001## R′ is H, CN, CH.sub.2(OH)R.sub.0, C.sub.mH.sub.2m+1, C.sub.nH.sub.2n-1, C.sub.nH.sub.2n-3, ##STR00002##
two R.sub.a is independently H, or two R.sub.a together form ═O or ═N—W.sub.3—R.sub.1; A is a C.sub.6 to C.sub.10 aromatic ring, or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom from N, O and S, or 4 to 7 membered non-aromatic heterocyclic ring containing 1 to 3 heteroatom from N, O and S and C═N, which are with no substituent or substituted by 1 or 3 R; Q is R, or a C.sub.6 to C.sub.10 aromatic ring or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom selected from N, O and S, which are with no substituent or substituted by 1 or 3 R; R is R.sub.c connected with C or R.sub.N connected with N.
Enantioselective cross dehydrogenative coupling reactions and compounds synthesized by the reactions
Disclosed are enantioselective cross dehydrogenative coupling reactions for synthesizing tetrahydropyran compounds. Novel tetrahydropyran compounds may be synthesized by the disclosed methods as well as tetrahydropyran precursor compounds for synthesizing various naturally occurring compounds. The enantioselective cross dehydrogenative coupling reactions utilize in situ Lewis Acid activation in combination with oxidative formation of an oxocarbenium ion to provide a highly efficient and selective coupling reaction for synthesizing tetrahydropyran compounds.
Enantioselective cross dehydrogenative coupling reactions and compounds synthesized by the reactions
Disclosed are enantioselective cross dehydrogenative coupling reactions for synthesizing tetrahydropyran compounds. Novel tetrahydropyran compounds may be synthesized by the disclosed methods as well as tetrahydropyran precursor compounds for synthesizing various naturally occurring compounds. The enantioselective cross dehydrogenative coupling reactions utilize in situ Lewis Acid activation in combination with oxidative formation of an oxocarbenium ion to provide a highly efficient and selective coupling reaction for synthesizing tetrahydropyran compounds.
POLYCYCLIC AMINES AS OPIOID RECEPTOR MODULATORS
The present invention provides a genus of polycyclic amines that are useful as opioid receptor modulators. The compounds of the invention are useful in both therapeutic and diagnostic methods, including for treating pain, neurological disorders, cardiac disorders, bowel disorders, drug and alcohol addiction, drug overdose, urinary disorders, respiratory disorders, sexual dysfunction, psoriasis, graft rejection or cancer.
POLYCYCLIC AMINES AS OPIOID RECEPTOR MODULATORS
The present invention provides a genus of polycyclic amines that are useful as opioid receptor modulators. The compounds of the invention are useful in both therapeutic and diagnostic methods, including for treating pain, neurological disorders, cardiac disorders, bowel disorders, drug and alcohol addiction, drug overdose, urinary disorders, respiratory disorders, sexual dysfunction, psoriasis, graft rejection or cancer.
Histone deacetylases (HDACs) inhibitors
Histone deacetylases (HDACs) inhibitors are disclosed according to the following structural formula. ##STR00001##
The moiety A is a benzene ring, optionally substituted. The moiety B is a benzene ring attached at the 1,4 or 1,3 position, or a cyclohexane ring attached at the 1,4 position, optionally substituted. R and Z are further substituents. The HDACs inhibitors possess cytotoxicities to various cancer cell lines. They are useful for treating a tumor associated with deregulation of the activity of histone deacetylases in a subject in need thereof, in one embodiment, the HDACs inhibitors of the invention are useful for treating glioma, breast cancer, colon cancer, target cell lung cancer, adenocarcinoma of the lung, small cell lung cancer, stomach cancer, liver cancer, ovary adenocarcinoma, pancreas carcinoma, prostate carcinoma, promyiocytic leukemia, chronic myelocytic leukemia, or acute lymphocytic leukemia in a subject in need thereof.
Histone deacetylases (HDACs) inhibitors
Histone deacetylases (HDACs) inhibitors are disclosed according to the following structural formula. ##STR00001##
The moiety A is a benzene ring, optionally substituted. The moiety B is a benzene ring attached at the 1,4 or 1,3 position, or a cyclohexane ring attached at the 1,4 position, optionally substituted. R and Z are further substituents. The HDACs inhibitors possess cytotoxicities to various cancer cell lines. They are useful for treating a tumor associated with deregulation of the activity of histone deacetylases in a subject in need thereof, in one embodiment, the HDACs inhibitors of the invention are useful for treating glioma, breast cancer, colon cancer, target cell lung cancer, adenocarcinoma of the lung, small cell lung cancer, stomach cancer, liver cancer, ovary adenocarcinoma, pancreas carcinoma, prostate carcinoma, promyiocytic leukemia, chronic myelocytic leukemia, or acute lymphocytic leukemia in a subject in need thereof.
COMPOUNDS FOR THE TREATMENT OF PARAMYXOVIRUS VIRAL INFECTIONS
Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).