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Restrict the search for
methyl salicylate
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Class (Stereo):
CHEMICAL (ACHIRAL)
Benfosformin (also known as JAV 852), a phosphorylated biguanide that was studied as a hypoglycemic and antidiabetic agent. However, the information about the studies of this compound now is not available.
Status:
Investigational
Source:
NCT01226277: Phase 1 Interventional Completed Solid Cancers
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
GDC-0917 (CUDC-427) is an orally available, monovalent mimetic of the second mitochondrial-derived activator of caspases (Smac/DIABLO) and inhibitor of IAPs (Inhibitor of Apoptosis Proteins) with potential antineoplastic activity. Smac mimetic GDC-0917 binds to the Smac binding groove on IAPs, including the direct caspase inhibitor X chromosome-linked IAP (XIAP) and the cellular IAPs 1 and 2. This inhibits the activities of these IAPs and promotes the induction of apoptosis through apoptotic signaling pathways. GDC-0917 demonstrated single-agent antitumor activity in mouse xenograft models bearing subcutaneous MDA-MB-231 tumors. In addition, CUDC-427 demonstrated additive activity in combination with chemotherapeutic agents and tumor necrosis factor apoptosis-inducing ligand (TRAIL) receptor targeting antibodies in xenograft tumor models. Preclinical safety and pharmacokinetic testing established an expected therapeutic range of doses as well as elucidated possible toxicities including inflammatory cytokine and chemokine proteins that could cause an inflammatory reaction, and reversible mild to moderate inflammation in the lungs and liver. GDC-0917 had been in phase I clinical trials by Genentech, Inc. for the treatment of Refractory Solid Tumors or Lymphoma. The principal toxicities related to CUDC-427 were mild to moderate in severity and included fatigue, nausea, vomiting, and rash.
Status:
Investigational
Source:
NCT00927823: Phase 1 Interventional Completed Cancer
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
PF-04691502 is a PI3K/mTOR dual inhibitor. It was tested in phase 2 clinical trials against endometrial cancer and breast cancer, but its development was discontinued due to unacceptable toxicity.
Status:
Investigational
Source:
NCT00069511: Phase 2 Interventional Unknown status Hepatitis C
(2003)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
UT-231B is an iminosugar that was under development by United Therapeutics Corporation as an oral drug for the treatment of hepatitis C virus (HCV). UT-231B completed acute and chronic Phase I dosing studies in early 2003. A Phase II proof-of-concept study for UT-231B in patients infected with hepatitis C who have failed conventional therapies was started, but the development of drug seemed to be discontinued.
Status:
Investigational
Source:
NCT02216669: Phase 1 Interventional Withdrawn Solid Tumors
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT01528735: Phase 2 Interventional Completed Hepatitis C, Chronic
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Deleobuvir is a drug for the treatment of Hepatitis C, developed by Boehringer Ingelheim. Deleobuvir is a non-nucleoside HCV NS5B polymerase inhibitor that reversibly and noncovalently binds to the thumb pocket 1. It has shown rapid and strong antiviral activity when administered in combination with peginterferon-a2a and ribavirin. In 2014 Boehringer Ingelheim decided to halt further development of deleobuvir because preliminary analysis of phase 3 clinical trials indicated a low efficacy of the drug.
Status:
Investigational
Source:
NCT01154101: Phase 2 Interventional Completed Psoriasis
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
SRT2104, also known as GSK2245840, is a novel, first in class, highly selective small molecule activator of the NAD + dependent deacetylase SIRT1. SIRT1 has been suggested as putative therapeutic target in multiple age-related diseases including type 2 diabetes and dyslipidemias. SRT2104 in the phase II of clinical trial to treat type 2 diabetes mellitus and psoriasis also in the phase I for its use in case of colitis. Also was reported, that we report that SRT2104, penetrated the blood-brain barrier, attenuated brain atrophy, improved motor function, and extended survival in a mouse model of Huntington's disease.
Status:
Investigational
Source:
NCT01530529: Phase 1 Interventional Completed Healthy
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT02419456: Phase 1 Interventional Completed HIV Infections
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
MK-2048, diketo acid derivative, is a second-generation integrase strand transfer inhibitor (INSTI) developed to retain activity against HIV containing mutations associated with resistance to first-generation INSTIs, raltegravir (RAL) and elvitegravir (EVG). MK-2048 implements its inhibitory mechanism by modifying viral integrase-DNA interactions, the important step of the linear HIV-1 cDNA integration into the host genome. It binds to and inactivates the synaptic complex, an intermediate in the concerted integration pathway in vitro thereby preventing target DNA binding and concerted integration. MK-2048 is active against viruses resistant to RAL and EVG. MK-2048 is equally potent against wild-type IN and raltegravir-resistant IN mutant N155H with a low IC50 value of 42 nM for inhibiting concerted integration. It inhibits R263K mutants slightly more effectively than G118R mutants. MK-2048 exposure leads to the selection of G118R as a possible novel resistance mutation.
Status:
Investigational
Source:
NCT02072863: Phase 1/Phase 2 Interventional Completed Multiple Myeloma
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Oprozomib (PR-047) is an orally bioavailable derivative of carfilzomib, with similar biological activity, i.e. inhibition of the chymotrypsin-like activity of the proteasome. It inhibits the activity of the proteasome, thereby blocking the targeted proteolysis normally performed by the proteasome; this may result in an accumulation of unwanted or misfolded proteins. Disruption of various cell signaling pathways may follow, eventually leading to the induction of apoptosis and inhibition of tumor growth. Oprozomib (PR-047) is being investigated for the treatment of hematologic malignancies, specifically, multiple myeloma, with Phase I/II trial ongoing.