A virtual biotech company engaged Organix to assist in the design and synthesis of compounds in which an existing drug would be bound to a polymer backbone by a linker engineered to possess specific functional attributes.
In the course of 9 months, Organix (1-2 FTEs) produced over 60 novel compounds by 5-7 step synthetic routes
on a 300-500 mg scale. These large compounds required tangential flow filtration (TFF) for purification
as well as the development of a unique GPC technique to quantify loading ratios of the active molecule to the polymer backbone. This work resulted in patent filings focused on two lead compounds. Organix then transferred synthetic processes to a large-scale facility for substantial scale-up and Organix personnel provided training to the scale-up company in the use of TFF for purification of large molecules. Organix was later retained for the synthesis of critical impurities obtained in the cGMP process. The impurity profile required RAFT polymerization techniques that Organix implemented in order to obtain different molecular weight polymers.

Organix has provided substantial services to three research centers of a multinational pharmaceutical company
over a period of 7 years. During this period the allocation of Organix staff has varied between 4 to 8 FTEs.
The breadth of this work has spanned the isolation of a lead natural product and the design and synthesis of derivatives
of this natural product, to the synthesis of families of compounds for SAR studies. In addition, Organix services have been employed to optimize synthetic routes and consequently to enable bulk synthesis of key intermediates.
Compound libraries have been synthesized to advance hit-to-lead programs.

Organix provided services to a biotech company involved in the development of CNS agents based upon a complex natural product alkaloid. The project was focused on developing SAR that included the optimization of pharmacokinetic properties. Over the course of 4 years, 6 FTEs were applied to the project and Organix developed syntheses for over 140 compounds on a 20 mg scale, each compound requiring between 5 to 10 synthetic steps. Final compounds were chiral and were characterized by formation of diastereomeric derivatives as well as by optical rotation. The complexity
of the compound required 2D-NMR to assign structure and stereochemistry unequivocally. The success of the project led to the subsequent scale-up of a lead compound as a backup clinical candidate.

This client had an ongoing project at Organix that was focused on the improvement of certain pharmacological properties of a drug already marketed by the client. This large pharmaceutical company first engaged Organix’ services
in with 1-2 FTEs and the project has continued to grow. Over the past 3 years, 4 FTEs have been engaged in the design
of synthetic pathways and synthesis of the chiral products. During this period, over 270 novel water-soluble compounds have been provided to the client on a scale of 20 mg to 100 mg. These complex DEA Scheduled alkaloid analogs
have been entered into an SAR program and have been protected in patent filings.