253135-95-4

Upstream product

• 796038-21-6 (R)-3-amino-5-phenyl-1,3-dihydro-2H-benzo[e][1.4]-diazepin-2-one 
• 1117976-38-1 ((S)-(2,6-dichloro-4-methoxyphenyl)(2,4-dichlorophenyl)methyl) N-succinimidyl carbonate 
• 103343-47-1 3-amino-5-phenyl-1,3-dihydrobenzo[e][1,4]diazepin-2-one 
• 207600-12-2 [1-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-ylcarbamoyl)-2-phenylethyl] carbamic acid tert-butyl ester 
• 676127-93-8 (S,S)-N-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-3-phenyl-2-(3-phenylthioureido)propionamide 
• 108895-98-3 benzyl 2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-ylcarbamate 
• 108895-97-2 2-α-(benzyloxycarbonyl)glycinyl)amino>benzophenone 
• 161365-74-8 benzyl N-[[(2-benzoylphenyl)carbamoyl](1H-1,2,3-benzotriazol-1-yl)methyl]carbamate 
• 116842-76-3 (S,S)-2-amino-N-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-3-phenylpropionamide 

Downstream Products

• 676128-63-5 (S)-1-(2-fluorophenyl)-3-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea 

Relevant academic research and scientific papers

PROCESSES FOR THE RESOLUTION OF BENZODIAZEPIN-2-ONE AND BENZOAZEPIN-2-ONE DERIVATIVES

The present invention relates to processes and intermediates useful in the preparation of biologically active molecules, especially in the synthesis of Respiratory Syncytial Virus (RSV) inhibitors. The present invention also relates to processes and inter

COMBINATION PHARMACEUTICAL AGENTS AS RSV INHIBITORS

The present invention relates to pharmaceutical agents administered to a subject either in combination or in series for the treatment of a Respiratory Syncytial Virus (RSV) infection, wherein treatment comprises administering a compound effective to inhibit the function of the RSV and an additional compound or combinations of compounds having anti-RSV activity.

PROCESSES FOR THE PREPARATION OF BENZODIAZEPINE DERIVATIVES

The present invention relates to processes and intermediates useful in the preparation of biologically active molecules, especially in the synthesis of Respiratory Syncytial Virus (RSV) inhibitors. The present invention also relates to processes and intermediates for the preparation of compounds of formula (I). In particular, the present invention also relates to processes and intermediates for the preparation of compound (I-a).

BENZODIAZEPINE DERIVATIVES AS RSV INHIBITORS

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

IMPROVED SYNTHESIS OF CAPURAMYCIN AND ITS ANALOGUES

Provided herein are compounds of Formula I, Formula II, and Formula X, which are useful for the treatment of infectious diseases. Also provided herein are processes for preparing 1-[5-0-[4,6-Dideoxy-6-oxo-6-[[[(3S)-hexahydro-2-oxo-1H-azepine]-3-y1]amino]-Pβ-L-erythro-4- hexenopyranosyl]-3-0-methyl 6-deoxy-6-amino-α-L-talofuranuronosyl]-1,2,3,4-tetrahydro-2,4- dioxopyrimidine (capuramycin), analogues thereof, and intermediates useful therefore. Also provided herein are III, IIIa, and IX, which are useful in the process for preparing capuramycin and/or a certain compound of Formula I.

PRODRUGS OF 1,4-BENZODIAZEPINONE COMPOUNDS

Disclosed are compounds of Formula (I) and salts thereof, wherein: a) R1 is H or CH3, and R2 is Ry; or b) R1 is Rx and R2 is H; wherein Rx and Ry are disclosed herein.

FLUOROALKYL AND FLUOROCYCLOALKYL 1,4-BENZODIAZEPINONE COMPOUNDS AS NOTCH|INHIBITORS

Disclosed are compounds of Formula (I): (Formula (I)) wherein: R1 is -CH2CH2CF3; R2 is -CH2CH2CH2F, -CH2CF2CH3, -CH2CH

Improved synthesis of capuramycin and its analogues

Capuramycin and its congeners are considered to be important lead molecules for the development of a new drug for multidrug-resistant (MDR) Mycobacterium tuberculosis infections. Extensive structure-activity relationship studies of capuramycin to improve the efficacy have been limited because of difficulties in selectively chemically modifying the desired position(s) of the natural product with biologically interesting functional groups. We have developed efficient syntheses of capuramycin and its analogues by using new protecting groups, derived from the chiral (chloro-4-methoxyphenyl)(chlorophenyl)methanols, for the uridine ureido nitrogen and primary alcohol. The chiral nonracemic (2,6-dichloro-4-methoxyphenyl)(2,4-dichlorophenyl)methanol derivative is a useful reagent to resolve rac-3-amino-1,3-dihydro-5-phenyl-2H-1,4-benzodiazepin- 2-one, the (S)-configuration isomer of which plays a significant role in improving the mycobactericidal activity of capuramycin. Battling TB: Capuramycin and its congeners (see scheme) are considered to be important lead molecules for the development of a new drug for multidrug-resistant Mycobacterium tuberculosis infections. Efficient synthesis of capuramycin and its analogues by using new protecting groups for the uridine ureido nitrogen and primary alcohol was accomplished. Copyright

BISFLUOROALKYL-1,4-BENZODIAZEPINONE COMPOUNDS

Disclosed are compounds of Formula (I) or prodrugs thereof; wherein: R1 is —CH2CF3 or —CH2CH2CF3; R2 is —CH2CF3, —CH2CH2CF3, or —CH2CH2CH2CF3; R3 is H or —CH3; each Ra is independently F, Cl, —CN, —OCH3, and/or —NHCH2CH2OCH3; and z is zero, 1, or 2. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.

1,4-Benzodiazepines as inhibitors of respiratory syncytial virus. The identification of a clinical candidate

Respiratory syncytial virus (RSV) is the cause of one-fifth of all lower respiratory tract infections worldwide and is increasingly being recognized as representing a serious threat to patient groups with poorly functioning or immature immune systems. Rac