152351-91-2Relevant articles and documents
A predictive model for additions to: N -alkyl pyridiniums
Knight, Brian J.,Tolchin, Zachary A.,Smith, Joel M.
supporting information, p. 2693 - 2696 (2021/03/18)
Disclosed in this communication is a thorough study on the dearomative addition of organomagnesium nucleophiles to N-alkyl pyridinium electrophiles. The regiochemical outcomes have observable and predictable trends associated with the substituent patterns on the pyridinium electrophile. Often, the substituent effects can be either additive, giving high selectivities, or ablative, giving competing outcomes. Additionally, the nature of the organometallic nucleophilic component was also investigated for its role in the regioselective outcome. The effects of either reactive component are important to both the overall reactivity and site of nucleophilic addition. The utility of these observed trends is demonstrated in a concise, dearomative synthesis of a tricyclic compound shown to have insecticidal activity. This journal is
Pleuromutilin derivatives such, its pharmaceutical composition and synthetic method and use thereof
-
, (2016/11/21)
The present invention relates to a class of pleuromytilin compounds represented by the following general formula (I), pharmaceutically acceptable salts and preparation methods thereof, and compositions comprising the compound represented by the general fo
PHOSPHORUS DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
-
Page/Page column 165, (2008/06/13)
The present invention relates to a novel class of phosphorus derivatives. The phosphorus compounds can be used to treat cancer. The phosphorus compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differe
ORGANIC COMPOUNDS
-
Page/Page column 26, (2008/12/06)
The present disclosure relates to XIAP inhibitor compound of the formula I: [Chemical formula should be inserted here as it appears on Abstract in paper form] Formula I
TRIAZOLO-PYRIDAZINE COMPOUNDS AND DERIVATIVES THEREOF USEFUL IN THE TREATMENT OF NEUROPATHIC PAIN
-
Page/Page column 53, (2010/02/11)
The present invention is directed to a method of use of triazolo-pyridazine compounds in the treatment of neuropathic pain. The present invention is also directed to the use of triazolo-pyridazine compounds in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorders, and panic, as well as in the treatment of pain, Parkinson’s disease, cognitive dysfunction, epilepsy, circadian rhythm and sleep disorders - such as shift-work induced sleep disorder and jet-lag, drug addiction, drug abuse, drug withdrawal and other diseases. The present invention is also directed to novel triazolo-pyridazine compounds that selectively bind to α2δ-1 subunit of Ca channels.
ARYL / HETARYL SUBSTITUTED IMIDAZOQUINOLINES
-
Page 110, (2008/06/13)
Aryl substituted imidazoquinoline compounds, according to formula I, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing w or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral., and neoplastic, are disclosed. formula (I): wherein: R is selected from the group consisting of alkyl, alkoxy, hydroxy, and trifluoromethyl;. N is 0 or 1; R3 is selected from the group consisting of: -Z-Ar,-Z-Ar’-Y-R4, -Z-Ar’-X-Y-R4, Z-Ar’-R5, and-Z-Ar'-X-R5; Ar is selected from the group consisting of aryl and heteroaryl both of which can be unsubstituted or can be substituted by one or more substituents independently selected from the group consisting of alkyl, alkenyl, alkoxy, methylenedioxy, haloalkyl, haloalkoxy, halogen, nitro, hydroxy, hydroxyalkyl, mercapto, cyano, carboxy, formyl, aryl, aryloxy, arylalkoxy, heteroaryl, heteroaryloxy, heteroarylalkoxy; heterocyctyl, heterocyclylalkyl, amino, alkylamino, and dialkylamino.
Structural features of azidopyridinyl neonicotinoid probes conferring high affinity and selectivity for mammalian α4β2 and Drosophila nicotinic receptors
Zhang, Nanjing,Tomizawa, Motohiro,Casida, John E.
, p. 2832 - 2840 (2007/10/03)
The higher toxicity of neonicotinoid insecticides such as N-(6-chloropyridin-3-ylmethyl)-2-nitroiminoimidazolidine (imidacloprid) to insects than mammals is due in large part to target site specificity at the corresponding nicotinic acetylcholine receptors (nAChRs). We propose that neonicotinoids with a protonated N-unsubstituted imine or equivalent substituent recognize the anionic subsite of the mammalian α4β2 nAChR whereas the negatively charged (δ-) tip of the neonicotinoid, insecticides interacts with a putative cationic subsite of the insect nAChR. This hypothesis can be tested by using two photoaffinity probes that differ only in the N-unsubstituted imine vs negatively charged (δ-) tip. Synthesis methodology was developed for compounds combining three moieties: pyridin-3-ylmethyl or 6-chloropyridin-3-ylmethyl and their 4- and 5-azido analogues; imidazolidine, 4-imidazoline or 4-thiazoline; and N-unsubstituted imine, nitroimine, cyanoimine, or nitromethylene. Structure-activity studies compared displacement of [3H] nicotine binding in mammalian α4β2 nAChR and [3H]imidacloprid binding in Drosophila nAChR. Preferred compounds are N-(5-azido-6-chloropyridin-3-ylmethyl) with 2-iminothiazoline for α4β2 (Ki = 0.47 nM) and with 2-nitroiminothiazoline or 2-nitromethyleneimidazolidine for Drosophila (Ki = 0.72-3.9 nM).
METHANOANTHRACENEYL METHYL PIPERIDINYL COMPOUNDS
-
, (2008/06/13)
Compounds of formula I or I', STR1 wherein X and Y are independently selected from hydrogen, halo, and (1-6C)alkoxy;R 1 is selected from(A) (1-6C)alkyl; (B) phenyl and naphthyl or substituted versions thereof; (C) phenyl (1-3C)alkyl and naphthyl (1-3C) alkyl;(D) five-and six-membered heteroaryl rings;(E) heteroaryl (1-3C) alkyl and pharmaceutically acceptable salts thereof, useful in the treatment of neuropsychiatric disorders such as psychoses; pharmaceutical compositions comprising a compound of formula I or I' and a pharmaceutically acceptable diluent or carrier; and methods of treating neuropsychiatric disorders comprising administering to a mammal (including man) in need of such treatment an effective amount of a compound of formula I or I', or a pharmaceutically acceptable salt thereof are claimed. The invention also relates to novel processes for producing enantiomeric methanoanthracenyl sulfoxides.