Patent classifications
C07C235/12
PROSTAGLANDIN EP4 RECEPTOR ANTAGONIST COMPOUNDS
The disclosures herein relate to novel compounds of formula (1): (1) and salts thereof, wherein A, X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.10 and R.sup.11 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with EP.sub.4 receptors.
##STR00001##
COMPOUNDS FOR REDUCING THE VISCOSITY OF BIOLOGICAL FORMULATIONS
The present invention relates to pegylated amino acid compounds of Formula I:
##STR00001##
and pharmaceutically acceptable salts thereof, wherein X, R.sup.1, R.sup.2, R.sup.3A, R.sup.3B and n are as defined herein. The present invention also relates to compositions which comprise a pegylated amino acid compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, in combination with a high concentration of an active biological ingredient (ABI). In embodiments of the invention, the ABI is an anti-PD-1 antibody or antigen binding fragment thereof that specifically binds human programmed death receptor 1 (PD-1). The invention further relates to methods for lowering the viscosity of an aqueous solution of a pharmaceutical composition comprising adding a compound of the invention to the solution. The invention also provides methods for treating a pathological disease or condition, such as cancer, by administering to a subject in need of such treatment a therapeutically effective amount of a pharmaceutical composition of the invention.
COMPOUNDS FOR REDUCING THE VISCOSITY OF BIOLOGICAL FORMULATIONS
The present invention relates to pegylated amino acid compounds of Formula I:
##STR00001##
and pharmaceutically acceptable salts thereof, wherein X, R.sup.1, R.sup.2, R.sup.3A, R.sup.3B and n are as defined herein. The present invention also relates to compositions which comprise a pegylated amino acid compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, in combination with a high concentration of an active biological ingredient (ABI). In embodiments of the invention, the ABI is an anti-PD-1 antibody or antigen binding fragment thereof that specifically binds human programmed death receptor 1 (PD-1). The invention further relates to methods for lowering the viscosity of an aqueous solution of a pharmaceutical composition comprising adding a compound of the invention to the solution. The invention also provides methods for treating a pathological disease or condition, such as cancer, by administering to a subject in need of such treatment a therapeutically effective amount of a pharmaceutical composition of the invention.
Bifunctional chiral organocatalytic compound having excellent enantioselectivity, preparation method therefor, and method for producing non-natural gamma-amino acid from nitro compound by using same
The present invention relates to a bifunctional chiral organocatalytic compound having excellent enantioselectivity, a preparation method therefor, and a method for producing a non-natural gamma amino acid from a nitro compound by using the chiral organocatalytic compound. According to the present invention, the bifunctional chiral organocatalytic compound having excellent enantioselectivity can be easily synthesized, gamma-amino acids with high optical selectivity can be obtained at a high yield by an economical and convenient method using the chiral organocatalytic compound, and various (R)-configuration gamma-amino acids, which are not present in nature, can be produced with high optical purity in large quantities by using a small amount of a catalyst, and therefore, the present invention can be widely utilized in various industrial fields including the pharmaceutical industry.
COMPOUND, SALT OF COMPOUND, EXTERNAL AGENT FOR SKIN, COSMETIC, AND FOOD ADDITIVE
Provided is a compound represented by Formula (1) or a salt thereof (in the formula, R.sup.1 and R.sup.2 each independently represent a hydrogen atom or a linear or branched acyl group having 11 to 30 carbon atoms, a hydrocarbon group bonded to a carbonyl carbon of the acyl group is a saturated or unsaturated hydrocarbon group, and at least one of R.sup.1 and R.sup.2 represents the acyl group).
##STR00001##
COMPOUND, SALT OF COMPOUND, EXTERNAL AGENT FOR SKIN, COSMETIC, AND FOOD ADDITIVE
Provided is a compound represented by Formula (1) or a salt thereof (in the formula, R.sup.1 and R.sup.2 each independently represent a hydrogen atom or a linear or branched acyl group having 11 to 30 carbon atoms, a hydrocarbon group bonded to a carbonyl carbon of the acyl group is a saturated or unsaturated hydrocarbon group, and at least one of R.sup.1 and R.sup.2 represents the acyl group).
##STR00001##
Branched fluorine-containing compound
A novel branched fluorine-containing compound represented by formula (1): ##STR00001##
wherein L represents a predetermined carbon-containing linker moiety; Rf, in each occurrence, is the same or different and represents fluoroalkyl optionally having at least one ether bond; Y, in each occurrence, is the same or different and represents a predetermined divalent linking group or a bond; R.sup.Y, in each occurrence, is the same or different and represents hydrogen or an organic group; L represents an (n1+n2)-valent carbon-containing linker moiety having at least one carbon atom; n1 represents a number greater than or equal to 1; n2 represents a number greater than or equal to 1; n1+n2 is a number from 3 to 6; X, in each occurrence, is the same or different and represents a divalent linking group or a bond; A, in each occurrence, is the same or different and represents -ArSO.sub.3M or the like; M, in each occurrence, is the same or different and represents hydrogen, —NR.sub.4, or a metal salt; and R represents hydrogen or a C.sub.1-4 organic group.
Branched fluorine-containing compound
A novel branched fluorine-containing compound represented by formula (1): ##STR00001##
wherein L represents a predetermined carbon-containing linker moiety; Rf, in each occurrence, is the same or different and represents fluoroalkyl optionally having at least one ether bond; Y, in each occurrence, is the same or different and represents a predetermined divalent linking group or a bond; R.sup.Y, in each occurrence, is the same or different and represents hydrogen or an organic group; L represents an (n1+n2)-valent carbon-containing linker moiety having at least one carbon atom; n1 represents a number greater than or equal to 1; n2 represents a number greater than or equal to 1; n1+n2 is a number from 3 to 6; X, in each occurrence, is the same or different and represents a divalent linking group or a bond; A, in each occurrence, is the same or different and represents -ArSO.sub.3M or the like; M, in each occurrence, is the same or different and represents hydrogen, —NR.sub.4, or a metal salt; and R represents hydrogen or a C.sub.1-4 organic group.
Dendritic core compounds
The invention relates to compounds that are useful for the preparation of dendrimer compounds, the use of these compounds for preparing dendrimers and processes for preparing the compounds.
Dendritic core compounds
The invention relates to compounds that are useful for the preparation of dendrimer compounds, the use of these compounds for preparing dendrimers and processes for preparing the compounds.