Abstract: Provided herein is a method for the manufacture of a compound of obicetrapib and salts thereof, such as calcium salts thereof. Also provided herein is amorphous obicetrapib hemicalcium. New intermediates for use in the synthesis of obicetrapib, and salts thereof are also provided, including obicetrapib HCl and a mesylate salt for the use in the synthesis of obicetrapib and amorphous obicetrapib hemicalcium.

Abstract: Provided herein is a method for the manufacture of a compound of obicetrapib and salts thereof, such as calcium salts thereof. Also provided herein is amorphous obicetrapib hemicalcium. New intermediates for use in the synthesis of obicetrapib, and salts thereof are also provided, including obicetrapib HCl and a mesylate salt for the use in the synthesis of obicetrapib and amorphous obicetrapib hemicalcium.

Abstract: Provided herein is a method for the manufacture of a compound of obicetrapib and salts thereof, such as calcium salts thereof. Also provided herein is amorphous obicetrapib hemicalcium. New intermediates for use in the synthesis of obicetrapib, and salts thereof are also provided, including obicetrapib HCl and a mesylate salt for the use in the synthesis of obicetrapib and amorphous obicetrapib hemicalcium.

Abstract: The present invention provides a novel process for preparing the compound I containing the compound [I(A)] (vadadustat) and the compound [I(B)] (roxadustat) which are useful as a medicine in an industrially advantageous manner, and a process for preparing the compound I which comprises reacting the compound (a1) or the compound (b1), the compound (2) or salts of the compound (2), with carbon monoxide in the presence of a palladium catalyst, in the presence or absence of a ligand, in the presence of a base, in a solvent to prepare the compound I (wherein structure formulae of the compound (a1), the compound (b1) or the compound (2), and the definitions of groups in the formulae are defined in the Description).

Abstract: Crystalline Forms I and II of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate and compositions, methods of manufacture and therapeutic uses thereof are described.

Abstract: Crystalline Forms I and II of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate and compositions, methods of manufacture and therapeutic uses thereof are described.

Abstract: Crystalline Forms I and II of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate and compositions, methods of manufacture and therapeutic uses thereof are described.

Abstract: Crystalline Forms I and II of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate and compositions, methods of manufacture and therapeutic uses thereof are described.

Abstract: Crystalline Forms I and II of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate and compositions, methods of manufacture and therapeutic uses thereof are described.

Abstract: Crystalline Forms I and II of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate and compositions, methods of manufacture and therapeutic uses thereof are described.

Abstract: Crystalline Forms I and II of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate and compositions, methods of manufacture and therapeutic uses thereof are described.

Abstract: Crystalline Forms I and II of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate and compositions, methods of manufacture and therapeutic uses thereof are described.

Abstract: The present invention relates to a method for preparing an optically active cyclic alcohol compound represented by general formula [I]: [wherein R represents a hydrogen atom or a protecting group for amino group, and * represents an asymmetric carbon atom.] which comprises a step of subjecting a cyclic ketone compound represented by general formula [II]: [wherein R has the same meaning as defined above.] to asymmetric reduction (A) in the presence of an optically active oxazaborolidine compound and a boron hydride compound, or (B) in the presence of an asymmetric transition metal complex obtained from a transition metal compound and an asymmetric ligand and a hydrogen donor, and relates to said compound.

Abstract: Crystalline Forms I and II of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate and compositions, methods of manufacture and therapeutic uses thereof are described.

Abstract: The present invention relates to a method for preparing an optically active cyclic alcohol compound represented by general formula [I]: [wherein R represents a hydrogen atom or a protecting group for amino group, and * represents an asymmetric carbon atom.] which comprises a step of subjecting a cyclic ketone compound represented by general formula [II]: [wherein R has the same meaning as defined above.] to asymmetric reduction (A) in the presence of an optically active oxazaborolidine compound and a boron hydride compound, or (B) in the presence of an asymmetric transition metal complex obtained from a transition metal compound and an asymmetric ligand and a hydrogen donor, and relates to said compound.

Abstract: Crystalline Forms I and II of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate and compositions, methods of manufacture and therapeutic uses thereof are described.

Abstract: The present invention relates to a method for preparing an optically active cyclic alcohol compound represented by general formula [I]: [wherein R represents a hydrogen atom or a protecting group for amino group, and * represents an asymmetric carbon atom.] which comprises a step of subjecting a cyclic ketone compound represented by general formula [II]: [wherein R has the same meaning as defined above.] to asymmetric reduction (A) in the presence of an optically active oxazaborolidine compound and a boron hydride compound, or (B) in the presence of an asymmetric transition metal complex obtained from a transition metal compound and an asymmetric ligand and a hydrogen donor, and relates to said compound.

Abstract: The present invention relates to a method for preparing an optically active cyclic alcohol compound represented by general formula [I]: [wherein R represents a hydrogen atom or a protecting group for amino group, and * represents an asymmetric carbon atom.] which comprises a step of subjecting a cyclic ketone compound represented by general formula [II]: [wherein R has the same meaning as defined above.] to asymmetric reduction (A) in the presence of an optically active oxazaborolidine compound and a boron hydride compound, or (B) in the presence of an asymmetric transition metal complex obtained from a transition metal compound and an asymmetric ligand and a hydrogen donor, and relates to said compound.

Abstract: The present invention relates to a method for preparing an optically active cyclic alcohol compound represented by general formula [I]: [wherein R represents a hydrogen atom or a protecting group for amino group, and * represents an astymmetric carbon atom.] which comprises a step of subjecting a cyclic ketone compound represented by general formula [II]: [wherein R has the same meaning as defined above.]to asymmetric reduction (A) in the presence of an optically active oxazaborolidine compound and a boron hydride compound, or (B) in the presence of an asymmetric transition metal complex obtained from a transition metal compound and an asymmetric ligand and a hydrogen donor, and relates to said compound.

Abstract: The present invention relates to a method for preparing an optically active 4-hydroxy-1,2,3,4-tetrahydroquinoline compound [I], which comprises the steps of: treating a racemic 4-hydroxy-1,2,3,4-tetrahydroquinoline compound represented by general formula [I]: [wherein R1 represents a hydrogen atom or a protecting group for amino group.] with an enzyme having an ability of selectively or preferentially acylating one enantiomer of the racemic compound [I] in the presence of an acyl donor; and if necessary, subjecting the reaction product to solvolysis.