Abstract: This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3- (S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic form has advantages over the other known forms of 2-(R)-(1-(R)-(3,5-bis(trifluoro-methyl)-phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.

Abstract: The most thermodynamically stable crystalline form of the benzoic acid salt of 4″-deoxy-4″-epi-methylamino avermectin B1a/B1b as the hemihydrate is obtained by crystallization from organic solvents containing a controlled amount of water.

Abstract: Polymorphic, amorphous and hydrated forms of the title compound having the following structure: are disclosed. The compound is a potent and selective cyclooxygenase-2 (COX-2) inhibitor.

Abstract: This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic form has advantages over the other known forms of 2-(R)-(1-(R)-(3,1-bis(trifluoro-methyl)-phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.

Abstract: A crystalline pharmaceutically acceptable benzenesulfonate salt of Compound A of formula: and solvates thereof are disclosed. Compound A and its benzenesulfonate salts are alpha 1a adrenergic receptor antagonists useful in the treatment of benign prostatic hyperplasia. Pharmaceutical compositions employing the crystalline salts, and processes for making and using the crystalline salts are also disclosed.

Abstract: There is disclosed 3-(5-methylisoxazol-3-yl)-6-(1-methyl-1,2,3-triazol-4-yl)methyloxy-1,2,4-triazolo[3,4-a]phthalazine in the form of a dihydrate, a dehydrate of the dihydrate and a pentahydrate, pharmaceutical compositions comprising the forms, the use of the forms for enhancing cognition, processes for producing the forms, their incorporation in pharmaceutical compositions comprising pamoate ions and the use of such ions for solubilizing neutral molecules.

Abstract: This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic form has advantages over the other known forms of 2-(R)-(1-(R)-(3,1-bis(trifluoro-methyl)-phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.

Abstract: This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic form has advantages over the other known forms of 2-(R)-(1-(R)-(3,,5-bis(trifluoro-methyl)-phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.

Abstract: This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3-(S)-(4-fluoro)phe nyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic form has advantages over the other known forms of 2-(R)-(1-(R)-(3,5-bis(trifluoro-methyl)-phenyl)ethoxy)-3-(S)-(4-fluoro)phe nyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.

Abstract: Disclosed is a new process for producing finasteride which involves reacting the magnesium halide salt of 17.beta.-carboalkoxy-4-aza-5.alpha.-androst-1-en-3-one with t-butylamino magnesium halide, present in at least a 2:1 molar ratio to the ester, formed from t-butyl amine and an aliphatic/aryl magnesium halide at ambient temperature in an inert organic solvent under an inert atmosphere followed by heating and recovering the product finasteride.Also disclosed are two polymorphic crystalline Forms I and II of finasteride, and methods of their production.

Abstract: The bisulfate salt of N,N-dimethyl-2-?5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl!ethylamine is a selective agonist of 5-HT.sub.1 -like receptors and is useful in the treatment of migraine and associated disorders.

Abstract: This invention is concerned with polymorphic forms of the compound N-?1(R)-?(1,2-dihydro-1-methanesulfonylspiro?3H-indole-3,4'-piperdin!-1'-y l)carbonyl!-2-(phenylmethyloxy)ethyl!-2-amino-2-methylpropanamide methanesulfonate which is a growth hormone secretagogue that is useful in food animals to promote their growth thereby rendering the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, and to treat medical conditions which are improved by the anabolic effects of growth hormone. The instant polymorphic forms have advantages over the other known forms of N-?1(R)-?(1,2-dihydro-1-methanesulfonylspiro?3H-indole-3,4'-piperdin!-1'-y l)carbonyl!-2-(phenylmethyloxy)-ethyl!-2-amino-2-methylpropanamide methanesulfonate in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.

Abstract: A process for producing polymorphic Form I of finasteride, 17B-(N-tert-butyl carbamoyl)-4-aza-5.alpha.-androst-1-en-3-one, in substantially pure form comprising the steps of: (1) crystallization from a solution of finasteride in a water immiscible organic solvent and 0% or more by weight of water, producing solvated and non-solvated finasteride in solution, such that the amount of organic solvent and water in the solution is sufficient to cause the solubility of the non-solvated form of finasteride to be exceeded and the non-solvated form of finasteride to be less soluble than any other form of finasteride in the organic solvent and water solution: (2) recovering the resultant solid phase; and (3) removing the solvent therefrom; wherein the water immiscible organic solvent is ethyl acetate or isopropyl acetate and the amount of water in the solvent mixture is below 4 mg./ml.

Abstract: Polymorphic forms of Losartan (Formula I) ##STR1## and a process for the preparation of Form II of Losartan. Losartan is known to be useful in the treatment of hypertension.

Abstract: By this invention, there is provided a process for producing crystalline 4,7.beta.-dimethyl-4-aza-5.alpha.-cholestan-3-one of structural formula (I) from 4,7.beta.-dimethyl-4-aza-5.alpha.-cholestan-3-one oil. ##STR1## This crystallization process of the present invention comprises crystallization of the oil optionally containing residual solvent with vigorous but controlled agitation. Preferably, this crystallization process is carried out at select and controlled temperatures. Further, 4,7.beta.-dimethyl-4-aza-5.alpha.-cholestan-3-one has been found to exist in at least two novel polymorphic nonsolvated forms, herein referred to as Form I and Form II. Form I can be prepared pure by careful control of the crystallization process.

Abstract: Disclosed is a new process for producing finasteride which involves reacting the magnesium halide salt of 17.beta.B-carboalkoxy-4-aza-5.alpha.-androst-1-en-3-one with t-butylamino magnesium halide, present in at least a 2:1 molar ratio to the ester, formed from t-butyl amine and an aliphatic/aryl magnesium halide at ambient temperature in an inert organic solvent under an inert atmosphere followed by heating and recovering said product finasteride.Also disclosed are two polymorphic crystalline Forms I and II of finasteride, and methods of their production.

Abstract: A process for isomerizing an alpha methylated azetidinone alkyl ester to the corresponding beta-methyl isomer, which is an intermediate in the synthesis of 1-beta-methylcarbapenem antibacterial agents. The process involves treating the dianion of structure I, being the alpha isomer, with a P-H or S-H containing organic protic acid, organometallic Sn or Pb hydride, metallic cation salt or trialkyl borane, followed by quenching with an OH protic organic acid or mineral acid.