Hypoxia-inducible factor-prolyl hydroxylase inhibitors in the treatment of anemia of chronic kidney disease.

The present application provides intermediates for preparing prostaglandin analogues and processes for preparing prostaglandin analogues and intermediates thereof. The intermediates include: A compound of formula (6): R1 represents H, C1-C5-alkyl, or benzyl, in particular isopropyl.

Process for the preparation of prostaglandin analogues and intermediates thereof

Clinical relevance of sodium/glucose cotransporter 2 (SGLT2) inhibitors has been rapidly evolving across several therapy areas, apart from type 2 diabetes mellitus. While some of these developments are based on recognized scientific explanations, unexpected study findings have also shaped much of our present understanding. As the role of these agents evolves in various facets of cardiology, nephrology, hepatology and endocrinology, their optimum clinical value propositions should be realized in line with the principles of personalized medicine. An updated pharmaco-ergonomic qualification tool, based on the present evidence with these agents, would be a step in this direction. This review describes the present evidence on diverse pharmacological and therapeutic aspects for various SGLT2 inhibitors, as an attempt to provide useful guidance for optimum application in clinical practice.

/pdf/basic-and-clinical-pharmaco-therapeutics-of-sglt2-inhibitors-1gtic6y6z0.pdf

Basic and Clinical Pharmaco-Therapeutics of SGLT2 Inhibitors: A Contemporary Update

Prostaglandin analogues represented by general formula (I), pharmaceutically acceptable salts thereof, or hydrates of both: wherein A is ethylene, vinylene or ethynylene; Y and Y are each independently hydrogen, halogeno, cyano, CONR R (wherein R and R are each independently hydrogen or C1-6 alkyl, or R and R together with the nitrogen atom adjacent thereto may form C4-8 cyclic amine), C1-3 aminoalkyl, C1-6 hydroxyalkyl, NR R (wherein R and R are each independently hydrogen or C1-6 alkyl), hydroxyl, C1-6 alkoxy, C1-9 alkyl, C1-6 haloalkyl, C1-5 acyl, or COOR (wherein R is hydrogen, C1-6 alkyl, or phenyl); R and R are each independently hydrogen, halogeno, C1-9 alkyl, or C1-6 haloalkyl; m is an integer of 0 to 6; and n is an integer of 0 to 3.

Prostaglandin e analogues

Object: to provide a novel prostaglandin E1 which is excellent in drug efficacy while reduced in adverse reactions as compared with conventional ones. Constitution: a PGE1 analogue represented by general formula (I) and its salt, wherein A represents vinylene or ethynylene; R1 represents hydrogen, C?1? to C6 alkyl or aryl; and R?2? represents C?5? to C10 branched aliphatic hydrocarbyl.

Prostaglandin e1 analogue

A prostaglandin E1 analog represented by formula (I), wherein R1 represents hydrogen or C?1?-C6 alkyl; and X represents oxygen and R?2? represents (a) or (b); or alternatively, X represents sulfur and R2 represents (c). This compound has a potent and persistent platelet aggregation inhibitor activity and is useful for treating various thrombotic diseases typified by peripheral circulatory disturbance.

Prostaglandin e1 analog

A process for stereoselectively obtaining an optically active O-acylpropargyl alcohol compound represented by general formula (2) (wherein R?1 and R2? represent each hydrogen or C?1?-C3 alkyl; R?3? represents phenyl which may be substituted by C?1?-C5 alkyl, halogeno or trifluoromethyl at an arbitrary position of the ring, C1-C8 alkyl or C5-C8 cycloalkyl; R?4? represents C?1?-C10 alkyl or phenyl which may be substituted by phenyl or halogeno at an arbitrary position of the ring; and the asterisk represents optical activity) by the reaction of an (RS)-propargyl alcohol compound represented by general formula (1) (wherein R?1, R2 and R3? are each as defined above) with an acylating agent R4COOR (wherein R4 is as defined above; and R represents arbitrary alkyl or alkenyl) in the presence of an enzyme; and a process for obtaining an optically active propargyl alcohol compound either by hydrolyzing the above O-acyl compound or from the solution of the above acylation reaction.

Process for producing optically active propargyl alcohol compound

To produce a prostaglandin E in a short time and in a high yield while minimizing the formation of isomers. A process for producing a prostaglandin E represented by general formula (I) wherein A represents an arbitrary group not participating in the reaction; B represents vinylene or ethynylene; R?4 and R5? may be the same or different from each other and each represents hydrogen or a protective group for a hydroxyl group; and R?6 and R7? represent each an arbitrary group not participating in the reaction, which comprises reacting an allyl ester of a prostaglandin E represented by general formula (II) wherein R?1 and R2? may be the same or different from each other and each represents hydrogen or lower alkyl; R3 represents hydrogen, lower alkyl, alkenyl or aryl; and R?4, R5, R6, R7?, A and B are each as defined above, with one or two compounds selected from the group consisting of bases and formic acid in the presence of a complex compound or a complex salt of 0-valent or divalent palladium atom.

Process for producing prostaglandin e.

Object: to provide a novel prostaglandin E1 which is excellent in drug efficacy while reduced in adverse reactions as compared with conventional ones. Constitution: a PGE1 analogue represented by general formula (I) and its salt, wherein A represents vinylene or ethynylene; R represents hydrogen, C1 to C6 alkyl or aryl; and R represents C5 to C10 branched aliphatic hydrocarbyl.

Prostaglandin e 1? analogue.

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