63016-85-3

Upstream product

• 699-98-9 Pyridine-2,3-dicarboxylic anhydride 
• 32315-10-9 bis(trichloromethyl) carbonate 
• 1462-86-8 3-amino-pyridine-2-carboxylic acid 
• 569687-82-7 3-tert-butoxycarbonylaminopyridine-2-carboxylic acid 
• 530-62-1 1,1'-carbonyldiimidazole 

Downstream Products

• 686267-59-4 1-benzyl-2H-pyrido[3,2-d][1,3]oxazine-2,4(1H)-dione 
• 1335147-65-3 C₁₅H₁₃N₃O₂ 
• 1437787-09-1 4-Benzyl-2-thioxo-3,4-dihydro-1H-pyrido[3,2-e][1,4]diazepin-5(2H)-one 
• 1437787-10-4 4-(4-methoxybenzyl)-2-thioxo-3,4-dihydro-1H-pyrido[3,2-e][1,4]diazepin-5(2H)-one 
• 1437787-12-6 4-benzyl-2-(pyrrolidin-1-yl)-3H-pyrido[3,2-e][1,4]diazepin-5(4H)-one 
• 1437787-13-7 4-benzyl-2-thiomorpholino-3H-pyrido[3,2-e][1,4]diazepin-5(4H)-one 
• 1437787-14-8 4-benzyl-2-morpholino-3H-pyrido[3,2-e][1,4]diazepin-5(4H)-one 
• 1437787-15-9 4-benzyl-2-(4-phenylpiperazin-1-yl)-3H-pyrido[3,2-e][1,4]diazepin-5(4H)-one 
• 1437787-16-0 4-benzyl-2-(4-benzylpiperazin-1-yl)-3H-pyrido[3,2-e][1,4]diazepin-5(4H)-one 
• 1437787-17-1 4-benzyl-2-(benzylamino)-3H-pyrido[3,2-e][1,4]diazepin-5(4H)-one 
• 1437787-18-2 4-benzyl-2-(3-methoxybenzylamino)-3H-pyrido[3,2-e][1,4]diazepin-5(4H)-one 
• 1437787-19-3 4-benzyl-2-(3-fluorobenzylamino)-3H-pyrido[3,2-e][1,4] diazepin-5(4H)-one 
• 1437787-20-6 4-benzyl-2-(2-chloro-3-fluorobenzylamino)-3H-pyrido[3,2-e][1,4]diazepin-5(4H)-one 
• 1437787-21-7 4-benzyl-2-(phenethylamino)-3H-pyrido[3,2-e][1,4]diazepin-5(4H)-one 

Relevant academic research and scientific papers

PDE9 inhibitor and application thereof

The invention belongs to the technical field of medicine and particularly relates to a PDE9 inhibitor compound shown as formula (I) or its pharmaceutically acceptable salts and stereoisomers, as wellas pharmaceutical preparations and pharmaceutical compositions of these compounds, and their application. The compounds herein are applicable to the preparation of drugs to treat or prevent PDE9-mediated related diseases.

A convenient synthesis of new pyrido[3,2-e][1,4]diazepine-2,5-diones and pyrido[2,3-e][1,4]diazepine-2,5-diones

A convenient synthesis of a series of pyrido[3,2-e][1,4]-diazepine-2,5- diones 8 and pyrido[2,3-e][1,4]diazepine-2,5-diones 9, is reported using the condensation of α-amino acid methyl ester derivatives with 1H-pyrido[3,2-d][1,3]oxazine-2,4-dione and 1H-p

BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS ANTIVARAL AGENTS

The invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined in the specification, and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together

Anti-infective agents

Compounds having the formula are hepatitis C(HCV) polymerase inhibitors. Also disclosed are a composition and method for inhibiting hepatitis C(HCV) polymerase, processes for making the compounds, and synthetic intermediates employed in the processes.

Anti-infective agents

Compounds having the formula are hepatitis C (HCV) polymerase inhibitors. Also disclosed are a composition and method for inhibiting hepatitis C (HCV) polymerase, processes for making the compounds, and synthetic intermediates employed in the processes.

NOVEL COMPOUNDS

Compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating atherosclerosis. In Formula (I) R1, R2, R3, R4, R5, R6, X and Y are as d

Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents

Heterocyclic analogues of 1192U90, 2-amino-N-(4-(4-(1,2-benzisothiazol- 3-yl)-1-piperazinyl)-butyl)benzamide hydrochloride (1), were prepared and evaluated as potential antipsychotic agents. These analogues were evaluated in vitro for their binding to the dopamine D2, serotonin 5-HT2, and serotonin 5-HT(1a) receptors and in vivo for their ability to antagonize the apomorphine-induced climbing response in mice. Nine different types of heterocyclic carboxamides were studied in this investigation (i.e., pyridine- , thiophene-, benzothiophene-, quinoline-, 1,2,3,4-tetrahydroquinoline-, 2,3- dihydroindole-, indole-, benzimidazole-, and indazolecarbox-amides). Two derivatives exhibited potent in vivo activities comparable to 1: 3-amino-N- (4(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)butyl)-2-pyridinecarboxamide (16) and 3-amino-N-(4(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)butyl)-2- thiophenecarboxamide (29). Furthermore, these derivatives were found to be much less active in behavioral models predictive of extrapyramidal side effects than in the mouse climbing assay, which predicts antipsychotic activity. Carboxamides 16 and 29 were selected for further evaluation as potential backup compounds to 1.

Indolo[2,1-biquinazoline-6,12-dione antibacterial compounds and methods of use thereof

Methods, compounds and compositions are provided form inhibiting the growth of pathogenic mycobacteria in vitro and of treatment of pathogenic mycobacterial infections in vivo using indolo[2,1-b]quinazoline-6,12-dione compounds of the formula (I): STR1 wherein A, B, C, D, E, F, G and H are independently selected from carbon and nitrogen, or A and B or C and D can be taken together to be nitrogen or sulfur, and the pharmaceutically acceptable salts thereof. The methods, compounds and compositons are particularly useful for inhibiting the growth of Mycobacterium tuberculosis, and may be used alone, or in combination with other anti-Mycobacterium tuberculosis agents, such as isoniazid, rifampin, pyrazinamide, rifabutin, streptomycin and ciprofloxacin, to provide new agents for the treatment of tuberculosis, including multidrug-resistant tuberculosis (MDRTB).