77992-44-0Relevant academic research and scientific papers
CD206 MODULATORS THEIR USE AND METHODS FOR PREPARATION
-
Paragraph 0263, (2021/06/26)
Compounds of Formula I, Formula II, and Formula III and the pharmaceutically acceptable salts thereof are disclosed. The variables X, a, b, c, d, R1-4, R10-15 and R17-22 are disclosed herein. The compounds are useful for treating cancer disorders, especially those involving M2 phenotype of macrophages. Pharmaceutical compositions containing compounds of Formula I or Formula II or Formula III and methods of treatment comprising administering compounds of Formula I and Formula II and Formula III are also disclosed.
TrkB POSITIVE ALLOSTERIC MODULATORS
-
Page/Page column 62-63, (2021/02/12)
The present invention relates to the field of pharmaceutical composition comprising "LIT-TB" derivatives of formula I. More particularly it relates to "LIT-TB" derivatives for use in the treatment of neurodegenerative diseases, and more particularly in th
Dual Reactivity of 1,2,3,4-Tetrazole: Manganese-Catalyzed Click Reaction and Denitrogenative Annulation
Chattopadhyay, Buddhadeb,Das, Sandip Kumar,Khatua, Hillol,Roy, Satyajit
supporting information, p. 304 - 312 (2020/10/29)
A general catalytic method using a Mn-porphyrin-based catalytic system is reported that enables two different reactions (click reaction and denitrogenative annulation) and affords two different classes of nitrogen heterocycles, 1,5-disubstituted 1,2,3-triazoles (with a pyridyl motif) and 1,2,4-triazolo-pyridines. Mechanistic investigations suggest that although the click reaction likely proceeds through an ionic mechanism, which is different from the traditional click reaction, the denitrogenative annulation reaction likely proceeds via an electrophilic metallonitrene intermediate rather than a metalloradical intermediate. Collectively, this method is highly efficient and offers several advantages over other methods. For example, this method excludes a multi-step synthesis of the N-heterocyclic molecules described and produces only environmentally benign N2 gas a by-product.
Compound and application thereof
-
Paragraph 0126-0130, (2021/11/10)
The invention provides a compound and application thereof. The compound has a structure as shown in a formula I, and is used as a material of an electron transport layer in an organic electroluminescent device. The organic electroluminescent device comprises a first electrode, a second electrode and an organic layer between the first electrode and the second electrode, wherein the organic layer contains any one or a combination of at least two of the compounds. The compound has relatively high electron injection and migration performance. When the compound is used as an electron transport layer material in an organic electroluminescent device, the luminous efficiency of the device can be improved, and the starting voltage of the device can be reduced.
TRIAZOLOPYRIDIN-3-ONES OR THEIR SALTS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
-
Paragraph 018-0184, (2020/07/07)
The present technology provides triazolopyridin-3-ones or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and uses thereof. The triazolopyridin-3-ones or their pharmaceutically acceptable salts exhibit inhibitory activity on VAP-1 and therefore can be usefully applied, e.g., for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).
Metal free [4+1] and [5+1] annulation reactions to prepare heterocycles using DMF and its derivatives as one-carbon source
Liu, Lingfeng,Qiao, Chunhua,Shen, Bei,Xu, Yiwen
supporting information, (2020/04/01)
1,2,4-Triazolo[3,4-a]pyridines and related heterocycles and substituted triazines were commonly discovered scaffolds in a variety of pharmaceutical and agrochemical agents. Herein, we report a highly efficient and practical method using DMF and its derivative for the [4+1] and [5+1] annulation reactions to prepare these heterocycles. This metal free reaction takes advantages of shelf stable DMF as solvent and carbon donor, imidazole chloride as a catalyst, the mild reaction condition tolerates a broad substrate range and substitutes. The prepared 3-unsubstituted 1,2,4-triazolo[3,4-a]pyridine and derivatives allow further introduction of a variety of functional group1 at 3-position.
ION CHANNEL MODULATORS
-
Paragraph 00419, (2019/12/25)
The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including neurological disorders (e.g., Dravet syndrome, epilepsy), pain, and neuromuscular disorders are also provided herein.
Iron(II)-Based Metalloradical Activation: Switch from Traditional Click Chemistry to Denitrogenative Annulation
Roy, Satyajit,Khatua, Hillol,Das, Sandip Kumar,Chattopadhyay, Buddhadeb
supporting information, p. 11439 - 11443 (2019/07/17)
A unique concept for the intermolecular denitrogenative annulation of 1,2,3,4-tetrazoles and alkynes was discovered by using a catalytic amount of Fe(TPP)Cl and Zn dust. The reaction precludes the traditional, more favored click reaction between an organic azide and alkynes, and instead proceeds by an unprecedented metalloradical activation. The method is anticipated to advance access to the construction of important basic nitrogen heterocycles, which will in turn enable discoveries of new drug candidates.
TRIAZOLONES DERIVATIVES FOR USE IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE
-
Page/Page column 32, (2017/04/18)
The present invention relates to a compound having the general formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, codrug, cocrystal, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
SUBSTITUTED FUSED HETEROCYCLES AS GPR119 MODULATORS FOR THE TREATMENT OF DIABETES, OBESITY, DYSLIPIDEMIA AND RELATED DISORDERS
-
Page/Page column 57, (2015/11/17)
The present invention relates to substituted fused heterocyclic compounds. The substituted fused heterocyclic compounds are GPR1 19 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of substituted fused heterocyclic compounds as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
