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
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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
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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
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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
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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
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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
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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
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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
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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
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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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