50735-33-6Relevant articles and documents
EIF4E INHIBITORS AND USES THEREOF
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Paragraph 00630; 00666, (2021/09/11)
The present invention provides compounds inhibiting elF4E activity and compositions and methods of using thereof.
Synthetic method of 2-amino-methyl-5-chloronicotinate
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Paragraph 0008; 0009; 0010; 0011, (2017/08/28)
The invention belongs to the field of organic synthesis, and particularly relates to a synthetic method of 2-amino-methyl-5-chloronicotinate. The synthetic method comprises the following step: (1) preparation of the 2-amino-methyl-5-chloronicotinate: reacting methyl-2-aminonicotinate with N-chlorosuccinimide in a proper solvent at the temperature of 0 to 100 DEG C for 2 to 8 hours to obtain the 2-amino-methyl-5-chloronicotinate, cooling to the room temperature at the end of the reaction, performing suction filtration, and recovering the solvent to obtain a 2-amino-methyl 5-chloronicotinate product. In the step (1), the temperature is 0 DEG C, 40 DEG C, 60 DEG C and 80 DEG C. In the step (1), the solvent is at least one of acetonitrile, N,N-dimethylformamide and N,N-dimethylacetamide. The synthetic method has the advantages of adoption of readily-available reaction raw materials, reasonable price, mild reaction conditions, easiness in operation, control and posttreatment, and has stable product quality and high purity.
HETEROCYCLIC SUBSTITUTED PYRIDINE COMPOUNDS WITH CXCR3 ANTAGONIST ACTIVITY
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Page/Page column 99-100, (2008/06/13)
The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, zenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
NOVEL HETEROCYCLIC SUBSTITUTED PYRIDINE OR PHENYL COMPOUNDS WITH CXCR3 ANTAGONIST ACTIVITY
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Page/Page column 126-127, (2008/06/13)
The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1 or a pharmaceutically acceptable salt, solvate or ester thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, zenograft rejection), infectious diseases (e.g , tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
HETEROARYL SUBSTITUTED PYRAZINYL-PIPERAZINE-PIPERIDINES WITH CXCR3 ANTAGONIST ACTIVITY
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Page/Page column 124, (2008/06/13)
The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts or solvates of said compound, or of said prodrug, said compound having the general structure shown in Formula 1 and the pharmaceutically acceptable salts, solvates or esters thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non limiting example(s) include, psoriasis), autoimmune diseases (non limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g , tuberculoid leprosy), fixed drug eruptions, cutaneous delayed type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
HETEROCYCLIC SUBSTITUTED PIPERAZINES WITH CXCR3 ANTAGONIST ACTIVITY
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Page/Page column 120, (2008/06/13)
The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having th
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists
Becker, Daniel P.,Flynn, Daniel L.,Moormann, Alan E.,Nosal, Roger,Villamil, Clara I.,Loeffler, Richard,Gullikson, Gary W.,Moummi, Chafiq,Yang, Dai-C.
, p. 1125 - 1139 (2007/10/03)
A series of pyrrolizidine esters, amides, and ureas was prepared and tested for 5-HT4 and 5-HT3 receptor binding, 5-HT4 receptor agonism in the rat tunica muscularis mucosae (TMM) assay, and for 5-HT3 receptor-mediated functional antagonism in the Bezold-Jarisch reflex assay. Several pyrrolizidine derivatives were identified with high affinity for the 5-HT4 receptor, including benzamide 12a (SC-53116), a potent and selective 5-HT4 partial agonist that exhibits efficacy in promoting antral contractions and activity in promoting gastric emptying in canine models. Also discovered were 5-HT4 receptor antagonists, including imidazopyridine amide 12h (SC-53606), which is a potent and selective 5-HT4 receptor antagonist with a pA2 value of 8.13 in the rat TMM assay. N-Methyl indole ester 13d was identified as a potent 5-HT 4 antagonist with a pA2 value of 8.93. High selectivity was observed for these pyrrolizidine derivatives versus other monoamine receptors, including 5-HT1, 5-HT2, D1, D 2, α1, α2, and β receptors. 2006 American Chemical Society.