40230-94-2Relevant academic research and scientific papers
Copper-Catalyzed Ring Opening of [1.1.1]Propellane with Alkynes: Synthesis of Exocyclic Allenic Cyclobutanes
Lasányi, Dániel,Tolnai, Gergely L.
supporting information, p. 10057 - 10062 (2019/12/24)
Despite the long history and interesting properties of propellanes, these compounds still have tremendous potential to be exploited in synthetic organic chemistry. Herein we disclose an experimentally simple procedure to achieve cyclobutane-containing allenes and alkynes through a copper-catalyzed ring opening of [1.1.1]propellane and subsequent reaction with ethynes.
ALKYNE COMPOUNDS AS S-NITROSOGLUTATHIONE REDUCTASE INHIBITORS
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Page/Page column 57; 125, (2016/05/02)
Provided are compounds of formula (Ia) and pharmaceutically acceptable salts thereof, wherein A, B, R 1, R 2, m and n are as defined herein, which are active as inhibitors of S-Nitrosoglutathione reductase (GSNOR). These compounds prevent, inhibit, or suppress the action of GSNOR and are therefore useful in the treatment of GSNOR mediated diseases, disorders, syndromes or conditions such as, e.g., pulmonary hypertension, acute respiratory distress syndrome (ARDS), asthma, bronchospasm, cough, pneumonia, pulmonary fibrosis, interstitial lung diseases, cystic fibrosis and chronic obstructive pulmonary disease (COPD).
Identification of (R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H- indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management
Gomtsyan, Arthur,Bayburt, Erol K.,Schmidt, Robert G.,Surowy, Carol S.,Honore, Prisca,Marsh, Kennan C.,Hannick, Steven M.,McDonald, Heath A.,Wetter, Jill M.,Sullivan, James P.,Jarvis, Michael F.,Faltynek, Connie R.,Lee, Chih-Hung
, p. 392 - 395 (2008/09/17)
Vanilloid receptor TRPV1 is a cation channel that can be activated by a wide range of noxious stimuli, including capsaicin, acid, and heat. Blockade of TRPV1 activation by selective antagonists is under investigation by several pharmaceutical companies in an effort to identify novel agents for pain management. Here we report that replacement of substituted benzyl groups by an indan rigid moiety in a previously described N-indazole-N′-benzyl urea series led to a number of TRPV1 antagonists with significantly increased in vitro potency and enhanced drug-like properties. Extensive evaluation of pharmacological, pharmacokinetic, and toxicological properties of synthesized analogs resulted in identification of (R)-7 (ABT-102). Both the analgesic activity and drug-like properties of (R)-7 support its advancement into clinical pain trials.
Hammett analysis of selective thyroid hormone receptor modulators reveals structural and electronic requirements for hormone antagonists
Nguyen, Ngoc-Ha,Apriletti, James W.,Baxter, John D.,Scanlan, Thomas S.
, p. 4599 - 4608 (2007/10/03)
Selective thyroid hormone modulators that function as isoform-selective agonists or antagonists of the thyroid hormone receptors (TRs) might be therapeutically useful in diseases associated with aberrant hormone signaling. The most potent thyroid hormone
ANTIBACTERIAL BENZOIC ACID DERIVATIVES
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Page 294, (2010/02/06)
The invention provides antimicrobial agents and methods of using the agents for sterilization, sanitation, antisepsis, disinfection, and treatment of infections in mammals.
Palladium-catalyzed carbon-carbon coupling reactions using aryl Grignards
Gottardo, Christine,Aguirre, Andrea
, p. 7091 - 7094 (2007/10/03)
Coupling reactions using Pd(PPh3)4 were investigated with a number of electron donating and electron withdrawing substituents. High yields were obtained with both types of substituents. In competitive reactions the electron-withdrawi
