The present invention related to novel inhibitors of metallo-β3-lactamases of formula (I)

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wherein R.sup.1 is an optionally substituted aryl group of an optionally substituted heteroaryl group, and the use thereof in the treatment of bacterial infections, especially in combination with β-lactam antibiotics.

The present invention provides sulfamoylating reagents of formula R.sup.uN.sup.−—S(O).sub.2X.sup.+, wherein X is a cyclic tertiary amine or a nitrogen-containing heteroaryl and R.sup.u is an amine protecting group or hydrogen.

The present invention provides sulfamoylating reagents of formula R.sup.uN.sup.−—S(O).sub.2X.sup.+, wherein X is a cyclic tertiary amine or a nitrogen-containing heteroaryl and R.sup.u is an amine protecting group or hydrogen.

The present invention relates to: a polymerizable compound represented by a formula (I); a polymerizable composition comprising the polymerizable compound and an initiator; a polymer obtained by polymerizing the polymerizable compound or the polymerizable composition; and an optically anisotropic article comprising the polymer [in the formula, Y.sup.1 to Y.sup.8 are a chemical single bond, —O—, —O—C(═O)—, —C(═O)—O—, or the like; G.sup.1 and G.sup.2 are a divalent aliphatic group having 1 to 20 carbon atoms, or the like; Z.sup.1 and Z.sup.2 are an alkenyl group having 2 to 10 carbon atoms, or the like; A.sup.1 is a tetravalent aromatic group, or the like; A.sup.2 and A.sup.3 are a divalent alicyclic hydrocarbon group having 3 to 30 carbon atoms, or the like; A.sup.4 and A.sup.5 are a divalent aromatic group having 4 to 30 carbon atoms, or the like; A.sup.x1 and A.sup.x2 are an organic group having 2 to 30 carbon atoms that includes an aromatic ring, or the like; A.sup.y1 and A.sup.y2 are a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like; Q.sup.1 and Q.sup.2 are a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like; and m and n are 0 or 1]. According to the present invention, a polymerizable compound, a polymerizable composition, and a polymer that have a practical low melting point, exhibit excellent solubility in a general-purpose solvent, can be produced at low cost, and can produce an optical film that achieves uniform conversion of polarized light over a wide wavelength band, and also provide an optically anisotropic article. ##STR00001##

The present invention relates to: a polymerizable compound represented by a formula (I); a polymerizable composition comprising the polymerizable compound and an initiator; a polymer obtained by polymerizing the polymerizable compound or the polymerizable composition; and an optically anisotropic article comprising the polymer [in the formula, Y.sup.1 to Y.sup.8 are a chemical single bond, —O—, —O—C(═O)—, —C(═O)—O—, or the like; G.sup.1 and G.sup.2 are a divalent aliphatic group having 1 to 20 carbon atoms, or the like; Z.sup.1 and Z.sup.2 are an alkenyl group having 2 to 10 carbon atoms, or the like; A.sup.1 is a tetravalent aromatic group, or the like; A.sup.2 and A.sup.3 are a divalent alicyclic hydrocarbon group having 3 to 30 carbon atoms, or the like; A.sup.4 and A.sup.5 are a divalent aromatic group having 4 to 30 carbon atoms, or the like; A.sup.x1 and A.sup.x2 are an organic group having 2 to 30 carbon atoms that includes an aromatic ring, or the like; A.sup.y1 and A.sup.y2 are a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like; Q.sup.1 and Q.sup.2 are a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like; and m and n are 0 or 1]. According to the present invention, a polymerizable compound, a polymerizable composition, and a polymer that have a practical low melting point, exhibit excellent solubility in a general-purpose solvent, can be produced at low cost, and can produce an optical film that achieves uniform conversion of polarized light over a wide wavelength band, and also provide an optically anisotropic article. ##STR00001##

Described are RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders. ##STR00001##

Described are RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders. ##STR00001##

The present invention relates to (S)-3-(2-(4-(benzyl)-3-oxopiperazin-1-yl)acetamido)-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)pentanoic acid derivatives and related compounds as caspase inhibitors for treating e.g. cardiovascular, kidney, liver, lung, skin, joints, CNS, inflammatory and autoimmune diseases.

The present invention relates to (S)-3-(2-(4-(benzyl)-3-oxopiperazin-1-yl)acetamido)-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)pentanoic acid derivatives and related compounds as caspase inhibitors for treating e.g. cardiovascular, kidney, liver, lung, skin, joints, CNS, inflammatory and autoimmune diseases.

Methods for preparing a cell targeting conjugate, which conjugate comprises a cell binding moiety conjugated to a secondary functional moiety. The disclosure further relates to the cell targeting conjugates obtainable by the method, to a pharmaceutical composition comprising the conjugates and to the secondary functional moieties as such. The disclosure also relates to the use of the cell targeting conjugates in the treatment of cancer.