C07D273/00

Simplified structural mimetics of AIPS as quorum sensing inhibitors

Compounds provided are racemic, non-racemic or substantially enantiomerically pure dimers or salts or solvates thereof of formula: ##STR00001## where: W and W are S or NR.sub.1, or WCO or WCO is CHCH, where each R.sub.1 is hydrogen or an alkyl group having 1 to 3 carbon atoms; R and R are hydrogen or an straight-chain or branched alkyl group having 1-3 carbon atoms; R.sub.3 and R.sub.3 are hydrogen or a C1-C3 alkyl; X.sub.1, X.sub.1, X.sub.2 and X.sub.2 are optionally-substituted straight-chain or branched alkyl groups having 3-8 carbon atoms, optionally-substituted cycloalkyl groups having 3-12 carbon atoms; optionally-substituted aryl, optionally-substituted heteroaryl, optionally-substituted heterocycyl, optionally-substituted cycloalkylalkyl, optionally-substituted arylalkyl, optionally-substituted heteroarylalkyl and optionally-substituted heterocycylalkyl groups and L.sub.1, L.sub.1 and L.sub.2 are divalent chemical moieties. Dimers are employed to modulate quorum sensing and to thus inhibit virulence in Staphylococcus bacteria. Dimers are useful in treating infections of Staphylococcus bacteria. Methods for treating such bacterial infections are also provided.

1,2,4-Oxadiazole Derivatives as Immunomodulators

The present invention relates to synthetic methods for 1,2,4-oxadiazole compounds. The general synthetic scheme is:

##STR00001##

R.sub.1 substituents generally are optionally substituted methanol or ethanol moieties, R.sub.3 substituents generally are optionally substituted acetic or propanoic acids or their amides and Aaa is Thr or Ser which has a free, amidated or esterified C-terminus.

THERAPEUTIC CYCLIC COMPOUNDS AS IMMUNOMODULATORS

The present invention relates to cyclic compounds of formula (I) and their use to inhibit the programmed cell death 1 (PD-1) signaling pathway and/or for treatment of disorders by inhibiting an immunosuppressive signal induced by PD-1, PD-L1 or PD-L2.

THERAPEUTIC CYCLIC COMPOUNDS AS IMMUNOMODULATORS

The present invention relates to cyclic compounds of formula (I) and their use to inhibit the programmed cell death 1 (PD-1) signaling pathway and/or for treatment of disorders by inhibiting an immunosuppressive signal induced by PD-1, PD-L1 or PD-L2.

REACTIVE MESOGEN AND LIQUID CRYSTAL COMPOSITION INCLUDING THE SAME
20180023000 · 2018-01-25 ·

Provided are a reactive mesogen that may improve display quality of a liquid crystal display, and a liquid crystal composition including the same. The reactive mesogen is represented by the following Formula:

##STR00001## where A.sub.1, A.sub.2, and A.sub.3 are each independently a substituted or unsubstituted divalent hydrocarbon ring, or a substituted or unsubstituted divalent heterocycle, L.sub.1 and L.sub.2 are each independently a direct linkage, O, S, CO, COO, OCOO, O(CH.sub.2).sub.k1, S(CH.sub.2).sub.k1, O(CF.sub.2).sub.k1, S(CF.sub.2).sub.k1, (CH.sub.2).sub.k1, CF.sub.2CH.sub.2, (CF.sub.2).sub.k1, CHCH, CFCF, CC, CHCHCOO, or (CH.sub.2).sub.k1COO(CH.sub.2).sub.k2O, Z.sub.1 and Z.sub.2 are each independently a direct linkage, O, S, CO, COO, OCOO, O(CH.sub.2).sub.m1, S(CH.sub.2).sub.m1, O(CF.sub.2).sub.m1, S(CF.sub.2).sub.m1, (CH.sub.2).sub.m1, CF.sub.2CH.sub.2, (CF.sub.2).sub.m1, CHCH, CFCF, CC, CHCHCOO, (CH.sub.2).sub.m1COO, (CH.sub.2).sub.m1COO(CH.sub.2).sub.m2O, CH(S.sub.pPa), CH.sub.2CH(S.sub.pPa), or (CH(S.sub.pPa)CH(S.sub.pPa)), Pa is a polymerizable group, B is an unsubstituted heterocycle, a substituted or unsubstituted crown ether group, or

##STR00002##

wherein T.sub.1 and T.sub.2 are each independently OH, CH.sub.3, CF.sub.3, CHF.sub.2, CH.sub.2F, CH.sub.2Br, CHBr.sub.2, CHCl.sub.2, or CH.sub.2Cl.

MACROCYCLIC COMPOUNDS AS PROTEASOME SUBUNIT BETA TYPE-5 INHIBITORS

The present invention relates to certain macrocyclic compounds of the formula (I) and pharmaceutically acceptable salts thereof. These compounds are useful in the treatment or prevention of a disease associated with and/or caused by proteasome or immunoproteasome, selected from a cancer, an infectious disease, an inflammatory disease, and autoimmune disease.

##STR00001##

1,2,4-Oxadiazole Derivatives as Immunomodulators

The present invention relates to pharmaceutical compositions of 1,2,4-oxadiazole compounds or a pharmaceutically acceptable salt thereof of formula (I)

##STR00001##

In the formula Q is O, R.sub.1 is the side chain of Ser, R.sub.2 is CO-Thr, R.sub.3 is the side chain of Asn or Glu, and R.sub.4, R.sub.5 and R.sub.6 are each H.

1,2,4-Oxadiazole Derivatives as Immunomodulators

The present invention relates to pharmaceutical compositions of 1,2,4-oxadiazole compounds or a pharmaceutically acceptable salt thereof of formula (I)

##STR00001##

In the formula Q is O, R.sub.1 is the side chain of Ser, R.sub.2 is CO-Thr, R.sub.3 is the side chain of Asn or Glu, and R.sub.4, R.sub.5 and R.sub.6 are each H.

COMPOUND HAVING SUBSTITUTED TRIPHENYLENE RING STRUCTURE, AND ORGANIC ELECTROLUMINESCENT DEVICE

An organic compound having an excellent electron injection and transport performance is provided as a material for a low-power-consumption organic electroluminescent device. A low-power-consumption organic electroluminescent device is also provided by using the compound. The compound is a compound of general formula (1) or (2) having a substituted bipyridyl and triphenylene ring structure. The organic electroluminescent device includes a pair of electrodes, and one or more organic layers sandwiched between the pair of electrodes, and uses the compound as constituent material of at least one of the organic layers.

##STR00001##

1,2,4-oxadiazole derivatives as immunomodulators

The present invention relates to 1,2,4-oxadiazole and 1,2,4-thiadiazole compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signaling pathway. The invention also refers to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them.