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Novel Piperidine-Amide Derivatives as CXCR4 Modulators
­ Application A new class of CXCR4 modulators for metastasis and inflammation. Key Benefits Selective for only one allosteric site on CXCR4. Lower adverse effects. Market Summary Multiple myeloma, acute myeloid leukemia, HIV, and rheumatoid arthritis all involve the G-protein receptor CXCR4. Currently, there is only one FDA approved CXCR4...
Published: 5/17/2022       Contributor(s): Hyunsuk Shim, Yoon Oum
Targeting SREBP1 for Managing Acquired Resistance to Osimertinib/AZD9291 and Other EGFR Inhibitors for Non-small Cell Lung Cancer Treatment
­ Application Small molecule combination therapy (adjuvant, sensitizing agent) for Osimertinib (to treat non-small cell lung cancer with common EGFR activating mutations and T790M resistant mutation). Key Benefits Therapy against EGFR-TKI resistant tumors with mutant EGFR (e.g., T790M). Market Summary Non-small cell lung cancer (NSCLC)...
Published: 5/13/2022       Contributor(s): Shi-Yong Sun, Zhen Chen
Small Molecule Compound to Treat Neurological Diseases
­ Application Neurological disease treatment. Key Benefits Exemplary compound EU1180-490 is a potent and selective potentiator of GluN1/GluN3 NMDARs. The compound has excellent Lipinski drug-like properties including low molecular weight and cLogP, as well as water solubility. The initial studies have determined that the compound can penetrate...
Published: 5/13/2022       Contributor(s): Dennis Liotta, Stephen Traynelis, Hongjie Yuan, Matthew Epplin, Samantha Summer, David Menaldino, Leon Jacobs, Adam McCallum
Small Molecules as Disinfectants and Antiseptics
­ Application Anti-microbial molecules with broad spectrum activities. Key Benefits Effective antimicrobial scaffolds with improved broad-spectrum activities compares to current commercial disinfectants. Technical Summary Resistant strains of bacteria cause 750,000 deaths worldwide each year. There is an increased effort in developing new...
Published: 3/16/2022       Contributor(s): William (Bill) Wuest, Kevin Minbiole
IACS-0107059 for Sensitizing Resistant Multiple Myeloma (MM) for Venetoclax Therapy
­ Application Combinatorial drug therapy for resistant multiple myeloma. Key Benefits Clinically approved drugs to repurpose for multiple myeloma. Therapies for multiple myeloma that is resistant to other therapies. Market Summary Multiple myeloma (MM) is a plasma cell malignancy estimated to account for 12K deaths and 32K new diagnoses in...
Published: 3/16/2022       Contributor(s): Malathy (mala) Shanmugam, Aditi Sharma
Small Molecule TrkB Agonist to Prevent Blindness from Eye Injuries
Application Small molecule HIOC derivatives as a therapeutic for preventing vision loss in traumatic eye injuries. Key Benefits Reduces blindness in a model of traumatic optical injury. May be administered systemically and penetrates tissues in and adjacent to the brain. This treatment method has potential for indications outside of retinal injury. Market...
Published: 5/5/2021       Contributor(s): Paul Iuvone, Frank Mcdonald, Christopher Walker
CFTR Modulators for Treating Rare Forms of Cystic Fibrosis
Application Small molecules to treat cystic fibrosis and other pulmonary diseases. Key Benefits Rescue rare variants of CFTR gene. Serve as PDE4 inhibitors with strong anti-inflammatory effects. Market Summary Cystic fibrosis (CF) is a progressive, genetic disorder that arises from mutations in the cystic fibrosis transmembrane conductance...
Published: 11/2/2020       Contributor(s): Eric Sorscher, Jeong Hong, Haian Fu, Yuhong Du, Huw Davies, Andras Rab, Candela Manfredi, Xun Yang, Zhi Ren
Small Molecule for Treatment or Prevention of Uremic Cardiomyopathy
Application Small molecule urea transporter (UT) inhibitors to treat or prevent conditions associated with chronic kidney disease. Key Benefits Provides a cardio-protective benefit in CKD patients. Suppresses cardiac hypertrophy and fibrosis. Market Summary Cardiovascular complications commonly occur in patients with chronic kidney disease...
Published: 11/2/2020       Contributor(s): Jeff Sands, Janet Klein, Xiaonan Wang
Class of Bcl-2 Inhibitors as Anti-Cancer Therapeutics
Application Small molecule inhibitors of Bcl-2, an anti-apoptotic protein, for cancer treatment. Key Benefits Developed specifically to target the BH4 homology domain of Bcl-2 in order to improve binding affinity and anti-tumor efficacy over other Bcl-2 inhibitors. Compounds may simultaneously suppress a wider range of anti-apoptotic proteins than...
Published: 10/2/2020       Contributor(s): Xingming Deng, Jia Zhou, Chunyong Ding
Development of Bax Activators as a New Class of Anti-Cancer Drugs
Application Therapeutic for treatment of cancer. Key Benefits The first in class, potent and selective agonists of Bax with nanomolar activity. Bax activators have significantly less apoptotic effect on normal cells as compared to cancer cells. Compounds have shown high selectivity for tumor cells. Technical Summary Patients with cancer have...
Published: 10/2/2020       Contributor(s): Xingming Deng, Jia Zhou, Chunyong Ding
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