The present teachings relate to piperazine metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulators having Formula (I); wherein the constituent variables are as defined herein. The present teachings further relate to methods for the preparation of the compounds and to methods for using the compounds for treatment of diseases and disorders including schizophrenia paranoia depression manic-depressive illness and anxiety.

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.

The present invention concerns processes for the production and purification of compounds of the formula:where R1-R10 are as defined in the specification. Preferred processes of the invention utilize a lithium bis(trimethylsilyl)amide lithium dicyclohexylamide or potassium bis(trimethylsilyl)amide base and a R1—X alkylating agent where X is as described in the specification. An alcohol preferably is added to the product solution is used to promote crystallization of the desired product.

The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.

This invention provides anti-inflammatory agents of formula I having the structurewherein A and R1-R10 are as defined in the specification or a N-oxide thereof or a pharmaceutically acceptable salt thereof or a prodrug thereof.

This invention provides progesterone receptor modulators having the structure:wherein R1 to R7 X and Q are as defined in the specification; or a pharmaceutically acceptable salt thereof.

Selective dual serotonin and norepinephrine reuptake inhibitors are provided. These compounds have a lower side-effect profile and are useful in compositions and products for use in treatment of a variety of conditions including depression fibromyalgia anxiety panic disorder agoraphobia post traumatic stress disorder premenstrual dysphoric disorder attention deficit disorder obsessive compulsive disorder social anxiety disorder generalized anxiety disorder autism schizophrenia obesity anorexia n...

The present invention relates generally to phenanthridine carbonyl compositions such as substituted phenanthridine carbonyl phenols of Formula 1:wherein R1 to R15 are as defined in the specification or pharmaceutically acceptable salts thereof; and methods of using them.

PROBLEM TO BE SOLVED: To provide a process for manufacturing the preparation of tigecycline suitable for intravenous infusion. SOLUTION: The process for manufacturing tigecycline as a reconstitutable powder having less than 0.9% of the total degradants comprises the steps: a. reducing and maintaining the oxygen level in WFI water to less than or equal to 0.5 ppm while maintaining the temperature at about 2C to about 8C; b. forming a solution of tigecycline in the water of step a at a concentrat...