Abstract: The present invention comprises an improved process for the preparation of substituted quinoxaline I by cyclization of the corresponding dianiline.

Abstract: The subject invention provides a varenicline composition that comprises varenicline, or a pharmaceutically acceptable salt thereof, and an amount of a compound selected from one or more of several mononitro, monoamino, mixed aminonitro, diamino or dinitro intermediates, and the concentration of said compound is greater than 0 ppm and not greater than about 500 ppm, not greater than about 100 ppm or not greater than about 10 ppm. Methods for synthesizing and using such varenicline compositions are also provided.

Abstract: The instant invention provides crystal forms of 5-chloro-N-[(1S,2R)-3-[3R,4S]-3,4-dihydroxy-1-pyrrolidinyl]-2-hydroxy-3-oxo-1-(phenylmethyl)propyl]-1H-indole-2-carboxamide (I) 1

Abstract: The subject invention provides a ziprasidone composition that comprises not greater than 1000 ppm des-chloro ziprasidone, preferably not greater than about 500 ppm des-chloro ziprasidone, and more preferably not greater than about 100 ppm des-chloro ziprasidone. Methods for synthesizing and using such ziprasidone compositions are also provided.

Abstract: The instant invention provides novel processes and intermediates useful in the preparation of certain N-(indole-2-carbonyl)-&bgr;-alaninamide compounds, which compounds are glycogen phosphorylase inhibitors useful in the treatment of diseases such as hypercholesterolemia, hyperglycemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis, diabetes, diabetic cardiomyopathy, infection, tissue ischemia, myocardial ischemia, and in inhibiting tumor growth.

Abstract: The instant invention provides crystal forms of 5-chloro-N-[(1S,2R)-3-[3R,4S]-3,4-dihydroxy-1-pyrrolidinyl]-2-hydroxy-3-oxo-1-(phenyl) methyl)propyl]-1H-indole-2-carboxamide (I) processes for the production of such crystal forms; pharmaceutical compositions comprising such crystal forms; and methods of treating glycogen phosphorylase dependent diseases, or conditions with such crystal forms, or such pharmaceutical compositions.

Abstract: This invention relates to improved processes for preparing compounds of Formula II, and compounds of Formula III, wherein R1, R2, R3 and Prt are defined as set forth in the specification.

Abstract: The instant invention provides crystal forms of 5-chloro-N-[(1S,2R)-3-[3R,4S]-3,4-dihydroxy-1-pyrrolidinyl]-2-hydroxy-3-oxo-1-(phenylmethyl)propyl]-1H-indole-2-carboxamide (I) 1

Abstract: The instant invention provides novel processes and intermediates useful in the preparation of certain N-(indole-2-carbonyl)-&bgr;-alaninamide compounds, which compounds are glycogen phosphorylase inhibitors useful in the treatment of diseases such as hypercholesterolemia, hyperglycemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis, diabetes, diabetic cardiomyopathy, infection, tissue ischemia, myocardial ischemia, and in inhibiting tumor growth.

Abstract: This invention relates to methods of preparing sodium-hydrogen exchanger type 1 (NHE-1) inhibitors of formula I′ and methods of preparing pharmaceutical compositions comprising such NHE-1 inhibitors.

Abstract: This invention relates to improved processes for preparing compounds of Formula II, 1

Abstract: This invention relates to methods of preparing sodium-hydrogen exchanger type 1 (NHE-1) inhibitors of formula I′ 1

Abstract: This invention relates to improved processes for preparing compounds of Formula II, and compounds of Formula III, wherein R1, R2, R3 and Prt are defined as set forth in the specification.

Abstract: This invention relates to improved processes for preparing compounds of Formula II, 1

Abstract: The invention is directed to the mesylate dihydrate salts of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydro-2H-indol-2-one, pharmaceutical compositions containing said ziprasidone mesylate dihydrates, and methods of adminsitering the ziprasidone mesylate dihydrates to treat psychotic diseases.

Abstract: Mesylate Trihydrate Salt of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydr o-2(1H)-indol-2-one (=Ziprasidone), Its Preparation and Its Use as Dopamine D2 AntagonistThe invention relates to the mesylate trihydrate salt of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydr o-2(1H)-indol-2-one ("ziprasidone mesylate trihydrate"), to pharmaceutical compositions containing ziprasidone mesylate trihydrate, and to methods of administering ziprasidone mesylate trihydrate to treat psychotic diseases.

Abstract: Processes for the synthesis of tigogenin beta-O-cellobioside heptaalkanoate which is an intermediate for the known hypo-cholesterolemic agent tigogenin beta-cellobioside. The process comprises reacting .alpha.-cellobiosyl bromide heptaalkanoate and .beta.-tigogenin in the presence of zinc fluoride or zinc cyanide under conditions capable of forming said tigogenyl .beta.-O-cellobioside heptaalkanoate. The analogous preparations of hecogenin .beta.-O-cellobioside heptaalkanoate 11-ketotigogenin .beta.-O-cellobioside heptaalkanoate, and diosgenin .beta.-O-cellobioside heptaalkanoate are also disclosed. The process provides both high .beta.-anomeric selectivity and high yields.

Abstract: Processes for the synthesis of tigogenin beta-O-cellobioside heptaalkanoate which is an intermediate for the known hypocholesterolemic agent tigogenin beta-cellobioside. The process comprises reacting .alpha.-cellobiosyl bromide heptaalkanoate and .beta.-tigogenin in the presence of zinc fluoride or zinc cyanide under conditions capable of forming said tigogenyl .beta.-O-cellobioside heptaalkanoate. The analogous preparations of hecogenin .beta.-O-cellobioside heptaalkanoate, 11-ketotigogenin .beta.-O-cellobioside heptaalkanoate, and diosgenin .beta.-O-cellobioside heptaalkanoate are also disclosed. The process provides both high .beta.-anomeric selectivity and high yields.

Abstract: A method for preparing a compound of the formula ##STR1## wherein Q is C--H or N; R.sup.1 is C.sub.1-C.sub.4 alkyl, benzyl or p-nitrobenzyl and X and Y are independently selected from fluoro and chloro comprising reacting a compound of the formula ##STR2## wherein Q is >C--H or N; X and Y are independently selected from fluoro and chloro; and Z is fluoro, chloro, 1-imidazolyl or substituted 1-imidazolyl, wherein the 1-imidazolyl group is substituted with one or two substituents independently selected from C.sub.1 to C.sub.4 alkyl, with a compound of the formula[M.sup.n+ ].sub.p [V.sup.p- ].sub.nwherein M is an alkaline earth metal, Cu or Mn, n is 2, V.sup.p-, wherein p is 1 or 2, is an anion of the formula ##STR3## or a dianion of the formula ##STR4## and R.sup.1 is C.sub.1 to C.sub.6 alkyl or paranitrobenzyl, with the proviso that when Z is 1-imidazolyl or substituted 1-imidazole, M is magnesium, copper or manganese and with the proviso that when Z is fluoro, chloro or bromo, V.sup.

Abstract: A process for preparing a compounds of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof, which comprises reacting a piperazine salt of the formula ##STR2## with an alkyl halide containing compound of the formula ##STR3## in water with a reagent to neutralize the hydrohalic acid and heating the mixture under conditions which are suitable to effect the coupling of said piperazine salt with said alkyl halide containing compound.