Abstract: The present invention provides an amorphous form of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid. This invention also provides processes for preparing the amorphous form and pharmaceutical compositions including the amorphous form.

Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor

Abstract: This invention provides compounds of the formulae: wherein: R1 is hydrogen, —C(O)CH3 or alkyl of 1-6 carbon atoms; R2 and R3 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl, alkoxy of 1-6 carbon atoms, —CH2OH, fluoroalkyl, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, aryl, or aroyl; R4 and R5 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, fluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R6 and R7 are each independently hydrogen, C1-C6 alkyl or cycloalkyl; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions containing these

Abstract: Processes are described for preparing 42-pegylated rapamycins including reacting a rapamycin with an acylating agent in the presence of a lipase to form an acylated rapamycin and reacting the acylated rapamycin with a methoxy poly(ethylene glycol) derivative in the presence of a base. Also described are processes for preparing 32-pegylated tacrolimus and/or ascomycin using these steps.

Abstract: The present invention provides processed for preparing a calicheamicin conjugate comprising removing glycosylation of a protein and reacting (i) an activated calicheamicin—hydrolyzable linker derivative and (ii) the deglycosylated protein. In one embodiment, the protein is an antibody, such as an anti-CD33 antibody (e.g., hp67.6), an anti-CD22 antibody (e.g., G544), an anti-Lewis Y antibody (e.g., G193), an anti-5T4 antibody (e.g., H8) or an anti-CD20 antibody (e.g., rituximab). In another embodiment, the calicheamicin derivative is an N-acyl derivative of calicheamicin or a disulfide analog of calicheamicin, such as N-acetyl gamma calicheamicin dimethyl hydrazide (N-acetyl calicheamicin DMH) and the hydrolyzable linker is 4-(4-acetylephenoxy) butanoic acid (AcBut) or (3-Acetylphenyl) acetic acid (AcPAc). Also provided are calicheamicin conjugates produced by such processes.

Abstract: Processes are provided for purifying a compound of the structure: wherein, A, B, T, Q and R1 are defined herein, and wherein the process includes dissolving the compound of formula I in a solution containing acetone, water and a base at about 30° C.; filtering the solution containing the compound of formula I at about 30° C.; and precipitating the purified compound of formula I by adjusting the filtered solution to an acidic pH. Desirably, the compound of formula I is 5-(2-thioxospiro[cyclohexane-1,3-[3H]indol]-5-yl)-1-methylpyrrole-2-carbonitrile or tanaproget.

Abstract: The present invention provides monoclonal antibodies that react against high molecular weight melanoma-associated antigen. These antibodies may be used for diagnostic and/or therapeutic purposes.

Abstract: A compound of the structure is described. This compound and its use for preparing medicines useful in the treatment of neurodegenerative disorders is described.

Abstract: The present invention relates generally to substituted indoles and methods of using them.

Abstract: A method for the regiospecific synthesis of rapamycin 42-ester derivatives is described. The method involves lipase-catalyzed acetylation of 42-hydroxy of rapamycin with an acyl donor such as a vinyl ester, an isopropenyl ester or an anhydride in a suitable organic solvent.

Abstract: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.

Abstract: The present invention provides methods of treating skin disorders includes delivering to a mammal a composition containing a compound of formula I, or tautomers thereof, in a regimen, wherein formula I is: and wherein R1-R5 and Q1 are defined as described herein. Specifically, methods for treating acne, hirsutism, and conditioning the skin are described. Also provided are novel PR modulators of formula II.

Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided: wherein: A is alkylenyl of 1 to 4 carbon atoms, or alkenylenyl of 2 to 4 carbon atoms; R1 and R2 are, independently, hydrogen or a C5 to C7 aryl optionally substituted with 1 to 2 substituents, independently, selected from the group consisting of —C(O)R3, halogen, cyano, nitro, hydroxyl, C1-C6 alkyl, and C1-C6 alkoxy, with the proviso that at least one of R1 and R2 is not hydrogen; R3 is, independently, hydrogen, —OR4, alkyl, aryl, or heteroaryl; R4 is hydrogen, alkyl, aryl, or heteroaryl; R5 and R6 are, independently, hydrogen, alkyl, hydroxyl, alkoxy, or C5 to C7 aryl; wherein any R3 to R6 group having an aryl or heteroaryl moiety can optionally be substituted on the aryl or heteroaryl moiety with 1 to about 5 substituents, independently, selected from the group consisting of halogen, cyano, nitro, hydroxyl, C1-C6 alkyl, and C1-C6 alkoxy.

Abstract: The invention relates to soluble proteins which bind to the molecule known as IL-TIF/IL-22. The proteins can antagonize the effect of IL-TIF/IL-22 on target cells. The nucleic acid molecules encoding the proteins, and uses of the protein, are also described.

Abstract: The present invention is directed to radiolabeled 3-cyanoquinolines of the formula: and methods of synthesizing the same, wherein G1, G2 R1, R4, Z, X, and n are as defined herein. The present invention is also directed to a radiolabeled intermediate compounds of formula (VII): wherein PG, G1, R1, R4, R10, and R11 are as defined herein, and synthesis of the same.

Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particularly those mediated by certain calcium channel subtype targets.

Abstract: The present invention is directed to pharmaceutical formulations and tablet compositions of pharmacological active agents of Formula I that are estrogen receptor modulators, and preparative processes thereof.

Abstract: The present invention is directed to liquid or semi-solid pharmaceutical formulations of pharmacologically active agents of Formula I that are estrogen receptor modulators, and pharmaceutical compositions and preparative processes thereof.

Abstract: The present invention is directed to pharmaceutical formulations of a monohydrate crystal form of an estrogen receptor modulator, and pharmaceutical compositions and preparative processes thereof.

Abstract: The present invention is directed to pharmaceutical formulations of an anhydrous crystal form of an estrogen receptor modulator, and pharmaceutical compositions and preparative processes thereof.