Schering Corporation

Cecilia A Orr

Ilia A Zavialov

Hoa N Nguyen

Fucheng Zhang

Vilas A Dahanukar

Anantha R Sudhakar

Craig D Boyle

Minzhang Chen

Kevin Joseph Klopfer

Jeonghan Park

George S Wong

Michael D Green

Vilas Hareshwar Dahanukar

Ingyu Jeon

Juergen Weber

Tetsuo Iwama

Vilas H Dahanukar

Albert W Buchholz, Jr

Funcheng Zhang

Jeffrey M Skell

A process for preparing xanthine phosphodiesterase V inhibitors, and compounds utilized in said process. The process includes a five-step methodology for efficient synthesis of Compound 5 without intermediate purifications or separations, a dihalogenation step to synthesize Compound 7, and a coupling reaction to produce Compound 9.   

Process for preparing xanthine phosphodiesterase V inhibitors and precursors thereof

In one embodiment, the present application relates to a process of making a compound of formula I: and to certain intermediate compounds that are made within the process of making the compound of formula I.

Process and intermediates for the preparation of (1R,2S,5S)-3-azabicyclo[3,1,0]hexane-2-carboxamide, N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[(2S)-2-[[[1,1-dimethylethyl]amino]carbonylamino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl

Crystalline polymorphs of 1-ethyl-3,7-dihydro-8-[(1R,2R) -(hydroxycyclopentyl)amino]-3-(2-hydroxyethyl)-7-[(3-bromo-4-methoxyphenyl)methyl]-1H-Purine-2,6-dione in Form 1 and Form 2, which exhibit x-ray powder diffraction profiles substantially the same as those shown in FIGS.and, respectively, and which exhibit differential scanning calorimtery profiles substantially the same as those shown in FIGS.and, respectively, and are represented by the formula:  Pharmaceutical compositions comprising the polymorph Form 1 or 2 of Compound 13 and at least one excipient or carrier, and methods of using the polymorph Form 1 or 2 of Compound 13 to treat a variety of physiological disorders, such as erectile dysfunction.

Xanthine phosphodiesterase V inhibitor polymorphs

A process for preparing xanthine phosphodiesterase V inhibitors, and compounds utilized in said process. The process includes a five-step methodology for efficient synthesis of Compound 5 without intermediate purifications or separations, a dihalogenation step to synthesize Compound 7, and a coupling reaction to produce Compound 9 

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Clark, NJ, United States of America

Cecilia A Orr