A Phase 1-2, Multicenter, Randomized, Double-Blind, Placebo Controlled, Prospective Study to Evaluate the Safety and Potential Efficacy of Single, Increasing Doses of TG100-115 in Subjects Undergoing Percutaneous Coronary Intervention for Acute Anterior ST Elevation Myocardial Infarction

TG100-115 is able to reduce the size of heart attacks in pre-clinical models. The hypothesis of this study is that TG100-115 can be given safely to patients who suffer a heart attack and undergo angioplasty to restore blood flow. We will also evaluate whether TG100-115 reduces heart muscle damage.

Start Date01 Jan 2005

Sponsor / Collaborator

TargeGen, Inc.

100 Clinical Results associated with TG-100115

100 Translational Medicine associated with TG-100115

100 Patents (Medical) associated with TG-100115

Literatures (Medical) associated with TG-100115

01 Jun 2024·Current Organic Synthesis

Heteroaromatization of Coumarin Part I: Design, Synthesis, Reactions, Antitumor Activities of Novel Pyridine and Naphthyridine Derivatives

Article

Author: El-Wahab, Ashraf Hassan Fekry Abd ; Borik, Rita Mohammed Ahmed

Abstract:A novel series of chromen-3-yl-pyridine moieties were synthesized. IR, NMR, and MS spec-troscopy were used to confirm the structure of these novel compounds and study antitumor activity of these compounds. The structure-activity relationship investigation demonstrated that 2,4-diamino-5-(3-methoxyphenyl)-7-(2-oxo-2H-chromen-3-yl)-1,8-naphthyridine-3-carbonitrile (16), naphthyridine-3-carbonitrile derivatives 17, 18 and pyrido[2,3-d]pyrimidine derivative 12 were found to be more effec-tive, while compounds 5a,b, 9c, 11, 13 and 14 showed moderate activity for antitumor activities.Objectives:The objective was to design a series of new chromen-3-yl-pyridine and pyrido[2,3-d]py-rimidine derivatives and study the antitumor of these compoundsMaterials and Methods:The condensation reaction of 3-acetyl-2H-chromen-2-one with 3-methoxy benzaldehyde and malononitrile or ethyl cyanoacetate in the presence of ammonium acetate and acetic acid under reflux to give the corresponding chromen-3-yl pyridine-3-carbonitrile derivatives.Results:In this study, the antitumor activity of the synthesized compounds chromen-3-yl-pyridine de-rivatives has been determined for the broad spectrum of cytotoxic activity toward the investigated three cell lines and 5-Fluorouracil, as reference drugsConclusion:A series of new chromen-3-yl-pyridine and pyrido[2,3-d]pyrimidine derivatives were syn-thesized in this work. All compounds were evaluated for cytotoxic activity.

01 Mar 2023·Medicinal Chemistry

Design, Synthesis, and Molecular Docking Study of Novel 3-Cyanopyridine Derivatives for the Anti-Cancer Drug Target Survivin Protein

Article

Author: Wu, Ai-Qun ; Lu, Jia-Hao ; Jiang, Li-He ; Lai, Wu-Ji ; Lei, Fu-Hou ; Shen, Li-Qun

Background:Survivin is an important member of the antiapoptotic protein family and controls the cell’s life cycle. Overexpression of survivin in tumor cells leads to inhibition of apoptosis, thus contributing to cancer cell proliferation. The largest binding pocket in the survivin dimer was located in the BIR domain. The key to the efficacy of 3-cyanopyridines was their surface interaction with the survivin amino acid Ile74.Method:Through the optimization of the 3-cyanopyridine, 29 new compounds with a 3- Cyanopyridine structure were designed, synthesized, and characterized by NMR, IR, and mass spectrometry. The antitumor activity of the compounds in vitro was detected by the MTT method.Results:In vitro anti-tumor experiments showed that some compounds exhibited good anti-cancer effects. The IC50 values of the compound 2-amino-6-(2,4-difluorophenyl)-4-(4-hydroxyphenyl) nicotinonitrile (10n) against human liver cancer (Huh7), human glioma (U251), and human melanoma (A375) cells were 5.9, 6.0 and 7.2 μM, respectively. The IC50 values of the compound 6-(2,4-difluorophenyl)- 4-(4-hydroxyphenyl)-2-oxo-1,2-dihydropyridine-3-carbonitrile (9o) against Huh7, U251 and A375 cells were 2.4, 17.5 and 7.2 μM, respectively, which were better than those of 10- hydroxycamptothecin and 5-fluorouracil. Analysis of the results of molecular dynamics simulation established that the BIR domain is the optimal binding site on the survivin protein, and the fingerprints of the eight most active compounds and the molecular docking to the survivin protein are analyzed.Conclusion:3-Cyanopyridine is an excellent backbone for antitumor lead compounds, 10n and 9o, as derivatives of 3-Cyanopyridine are excellent survivin protein-targeting inhibitors worthy of further study. The key factor in inhibiting survivin protein through the action of amino acid Ile74.

01 Dec 2022·Bioorganic Chemistry

Structure based design and synthesis of 3-(7-nitro-3-oxo-3,4-dihydroquinoxalin-2-yl)propanehydrazide derivatives as novel bacterial DNA-gyrase inhibitors: In-vitro, In-vivo, In-silico and SAR studies

Article

Author: Ezz Eldin, Rogy R ; Elmaaty, Ayman Abo ; Saleh, Moustafa M ; Saleh, Marwa A ; El Saeed, Hoda S ; Salah, Mohammed

Antimicrobial resistance (AMR) is one of the critical challenges that have been encountered over the past years. On the other hand, bacterial DNA gyrase is regarded as one of the most outstanding biological targets that quinolones can extensively inhibit, improving AMR. Hence, a novel series of 3-(7-nitro-3-oxo-3,4-dihydroquinoxalin-2-yl)propanehydrazide derivatives (3-6j) were designed and synthesized employing the quinoxaline-2-one scaffold and relying on the pharmacophoric features experienced by the quinolone antibiotic; ciprofloxacin. The antibacterial activity of the synthesized compounds was assessed via in-vitro approaches using eight different Gram-positive and Gram-negative bacterial species. Most of the synthesized compounds revealed eligible antibacterial activities. In particular, compounds 6d and 6e displayed promising antibacterial activity among the investigated compounds. For example, compounds 6d and 6e displayed MIC values of 9.40 and 9.00 µM, respectively, regarding S. aureus, and 4.70 and 4.50 µM, respectively, regarding S. pneumonia in comparison to ciprofloxacin (12.07 µM). The cytotoxicity of compounds 6d and 6e were performed on normal human WI-38 cell lines with IC50 values of 288.69 and 227.64 μM, respectively assuring their safety and selectivity. Besides, DNA gyrase inhibition assay of compounds 6d and 6e was carried out in comparison to ciprofloxacin, and interestingly, compounds 6d and 6e disclosed promising IC50 values of 0.242 and 0.177 μM, respectively, whereas ciprofloxacin displayed an IC50 value of 0.768 μM, assuring the proposed mechanism of action for the afforded compounds. Consequently, compounds 6d and 6e were further assessed via in-vivo approaches by evaluating blood counts, liver and kidney functions, and histopathological examination. Both compounds were found to be safer on the liver and kidney than the reference ciprofloxacin. Moreover, in-silico molecular docking studies were established and revealed reasonable binding affinities for all afforded compounds, particularly compound 6d which exhibited a binding score of -7.51 kcal/mol, surpassing the reference ciprofloxacin (-7.29 kcal/mol) with better anticipated stability at the DNA gyrase binding pocket. Moreover, ADME studies were conducted, disclosing an eligible bioavailability score of >0.55 for all afforded compounds, and reasonable GIT absorption without passing the blood brain barrier was attained for most investigated compounds, ensuring their efficacy and safety. Lastly, a structure activity relationship study for the synthesized compounds was established and unveiled that not only the main pharmacophores required for DNA gyrase inhibition are enough for exerting promising antimicrobial activities, but also derivatization with diverse aryl/hetero aryl aldehydes is essential for their enhanced antimicrobial potential.

News (Medical) associated with TG-100115

30 Jul 2007

·www.biospace.com

TargeGen, Inc. Initiates Multi-Center Phase II Clinical Trial Of TG100801, a Topically Applied Kinase Inhibitor In Macular Degeneration Patients

SAN DIEGO, July 30 /PRNewswire/ -- TargeGen, Inc. today announced that the Company has initiated a multi-center Phase II clinical trial of topically applied TG100801 in patients with age-related macular degeneration (AMD). (Logo: ) AMD is the leading cause of blindness in adults with more than 3.5 million estimated patients worldwide. Currently approved treatments for macular degeneration require repeated injection into the eye and act primarily by reducing VEGF mediated retinal leakage. TG100801 is administered non-invasively as an eye drop and is designed to suppress VEGF mediated leakage and additional kinase targets associated with inflammation, edema, and angiogenesis which are the pathological hallmarks of AMD and other back of the eye diseases including diabetic macular edema and proliferative diabetic retinopathy. "The initiation of this trial is a significant milestone for TargeGen," stated Peter G. Ulrich, President, CEO and Co-Founder of TargeGen. "TG100801 is an important drug candidate that potentially addresses the leading causes of debilitating vision loss in adults in a more comprehensive way and may eliminate or reduce the requirement for repeated injections into the eye." In addition to TG100801, TargeGen is developing TG101348, an oral Jak2 inhibitor for the potential treatment of myeloproliferative diseases and TG100115, a PI3K inhibitor for the potential treatment of certain inflammatory disorders. A second topically applied compound for eye disease, TG100948, is in early development. About TargeGen, Inc. TargeGen, Inc. is a privately held vascular biology-focused biopharmaceutical company based in San Diego, CA. TargeGen primarily develops small molecule kinase inhibitors that target vascular leakage (edema), vascular proliferation (angiogenesis) and inflammation. Edema, angiogenesis and inflammation are involved in the pathology of many major human diseases. TargeGen initiated operations in 2002 and has raised capital from top tier venture capital sources. Current investors include VantagePoint Venture Partners, Forward Ventures, Enterprise Partners, Chicago Growth Partners, BB BIOTECH, Innovis Investments, H&Q Capital Management, Pappas Ventures and other investors. Photo: NewsCom: AP Archive: PRN Photo Desk, photodesk@prnewswire.comTargeGen, Inc. CONTACT: TargeGen, Inc., +1-858-678-0760, fax, +1-858-678-0160,info@targegen.com Web site:

Small molecular drug

100 Deals associated with TG-100115

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Asthma	Phase 2	US	TargeGen, Inc.	-
Myocardial Infarction	Phase 2	-	Sanofi	-
Pulmonary Disease, Chronic Obstructive	Phase 2	US	TargeGen, Inc.	-
ST Elevation Myocardial Infarction	Phase 1	US	TargeGen, Inc.	01 Jan 2005
Myocardial Ischemia	Preclinical	US	Biopredict, Inc.	26 Dec 2006
Reperfusion Injury	Preclinical	US	Biopredict, Inc.	26 Dec 2006
Reperfusion Injury	Preclinical	US	TargeGen, Inc.	26 Dec 2006

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