Patent classifications
C07F9/58
IMMUNOMODULATOR COMPOUNDS
Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (II):
##STR00001## including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.6a, R.sup.6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
GPR40 AGONISTS
This disclosure is directed, at least in part, to GPR40 agonists useful for the treatment of conditions or disorders involving the gut-brain axis. In some embodiments, the GPR40 agonists are gut-restricted compounds. In some embodiments, the GPR40 agonists are full agonists or partial agonists. In some embodiments, the condition or disorder is a metabolic disorder, such as diabetes, obesity, nonalcoholic steatohepatitis (NASH), or a nutritional disorder such as short bowel syndrome.
GPR40 AGONISTS
This disclosure is directed, at least in part, to GPR40 agonists useful for the treatment of conditions or disorders involving the gut-brain axis. In some embodiments, the GPR40 agonists are gut-restricted compounds. In some embodiments, the GPR40 agonists are full agonists or partial agonists. In some embodiments, the condition or disorder is a metabolic disorder, such as diabetes, obesity, nonalcoholic steatohepatitis (NASH), or a nutritional disorder such as short bowel syndrome.
STING AGONISTIC COMPOUND
The object of the present invention is to provide a drug containing a compound having an agonistic activity to STING as an active ingredient.
As a result of intensive studies by the inventors of the present invention, the compound represented by the following general formula (I-1)
##STR00001##
[in the formula, all symbols represent the same meanings as described in the present specification.] or the like, having the agonistic activity to STING, as a substance capable of solving such objects, and this invention was completed.
Since the compound represented by the general formula (I-1) or the like of the present invention has the agonistic activity to STING, it can be used as an active ingredient of an agent for suppressing the progression of, suppressing the recurrence of and/or treating cancer or infectious disease.
NOVEL LYSOPHOSPHATIDIC ACID DERIVATIVE
The present invention aims to provide a compound acting as a specific agonist for LPA4 receptors, and a pharmaceutical composition containing the compound. The present invention relates to a novel lysophosphatidic acid derivative having an agonistic action on LPA4 receptors and useful for the prophylaxis and/or treatment of diseases associated with angiogenesis abnormalities involving LPA4 receptors, diseases associated with vascular disorders, or the symptoms associated therewith, and a pharmaceutical composition containing the derivative.
NOVEL LYSOPHOSPHATIDIC ACID DERIVATIVE
The present invention aims to provide a compound acting as a specific agonist for LPA4 receptors, and a pharmaceutical composition containing the compound. The present invention relates to a novel lysophosphatidic acid derivative having an agonistic action on LPA4 receptors and useful for the prophylaxis and/or treatment of diseases associated with angiogenesis abnormalities involving LPA4 receptors, diseases associated with vascular disorders, or the symptoms associated therewith, and a pharmaceutical composition containing the derivative.
18F-LABELED PSMA-TARGETED PET IMAGING AGENTS
Compounds of Marlush formula (I) described in the claims are useful in diagnostic methods for detecting and/or identifying cells presenting PSMA. Disclosed are also methods for preparing the compounds. Representative compounds according to the application are:
##STR00001##
18F-LABELED PSMA-TARGETED PET IMAGING AGENTS
Compounds of Marlush formula (I) described in the claims are useful in diagnostic methods for detecting and/or identifying cells presenting PSMA. Disclosed are also methods for preparing the compounds. Representative compounds according to the application are:
##STR00001##
NOVEL BISPHOSPHONIC ACID DERIVATIVE AND APPLICATION FOR SAME
The novel bisphosphonic acid ester derivatives represented by the following formula (1):
Y—Cy—(NH).sub.m—(CH.sub.2).sub.n—C(X)(PO(OR.sup.1)(OR.sup.2)).sub.2 (1)
wherein each symbol is as defined in the DESCRIPTION, which has an amino group substituted by a heterocyclic group or a heterocyclic group containing a nitrogen atom, and the acid moiety is esterified with a POM group, an n-butanoyloxymethyl (BuOM) group and the like, exhibit a superior direct or indirect cytotoxicity effect on tumor cells and virus infected cells.
NOVEL BISPHOSPHONIC ACID DERIVATIVE AND APPLICATION FOR SAME
The novel bisphosphonic acid ester derivatives represented by the following formula (1):
Y—Cy—(NH).sub.m—(CH.sub.2).sub.n—C(X)(PO(OR.sup.1)(OR.sup.2)).sub.2 (1)
wherein each symbol is as defined in the DESCRIPTION, which has an amino group substituted by a heterocyclic group or a heterocyclic group containing a nitrogen atom, and the acid moiety is esterified with a POM group, an n-butanoyloxymethyl (BuOM) group and the like, exhibit a superior direct or indirect cytotoxicity effect on tumor cells and virus infected cells.