57165-84-1

Upstream product

• 1181778-59-5 N-(1,1,1-trifluoro-2-hydroxy-4-amino-N-butyl)phthalimide 
• 453-34-9 4,4,4-trifluoro-3-hydroxybutanamide 
• 57165-85-2 3-hydroxy-4,4,4-trifluorobutyronitrile 

Downstream Products

• 57165-71-6 bis-(2-chloro-ethyl)-(2-oxo-6-trifluoromethyl-2λ⁵-[1,3,2]oxazaphosphinan-2-yl)-amine 
• 263346-51-6 4-[bis-[[3-(trifluoromethoxy)phenyl]methyl]amino]-1,1,1-trifluoro-2-butanol 
• 1289648-00-5 C₂₂H₁₇F₆N₃O₃ 
• 78149-86-7 diethyl-(2-oxo-6c-trifluoromethyl-2λ⁵-[1,3,2]oxazaphosphinan-2r-yl)-amine 
• 78149-86-7 2-(Diethylamino)tetrahydro-6-trifluormethyl-2H-1,3,2-oxazaphosphorin-2-oxid 

Relevant academic research and scientific papers

Insights on nuclease mechanism: The role of proximal ammonium group on phosphate esters cleavage

(Figure Presented) The role of remotely located ammonium groups in the active site of many phosphate-cleaving enzymes is investigated by using model systems thus providing mechanistic hints to a still unsolved problem.

CONDENSED HETEROCYCLES AS BCL-2 INHIBITORS

The disclosure includes compounds of Formula (A) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11, h, j, m, n, k, v, s, g, V, W, L, Z1 Q1, Q2, Q3, Q4, Q5, Q6, and Q7, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a neorodegenerative disease with these compounds.

HOT MELT EXTRUDED SOLID DISPERSIONS CONTAINING A BCL2 INHIBITOR

A pro-apoptotic solid dispersion comprises, a Bcl -2 family protein inhibitory compound of Formula A as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier, and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises subjecting to elevated temperature the compound of Formula A, the water-soluble polymeric carrier, and the surfactant to provide an extrudable semi-solid mixture; extruding the semi-solid mixture; and cooling the resulting extrudate to provide a solid matrix comprising the polymeric carrier, and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl -2 family proteins, for example cancer or an immune or autoimmune disease.

BCL-2 INHIBITORS

The disclosure includes compounds of Formula (A), (A) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11, h, j, m, n, k, v, s, g, V, W, L, Z1, Q1, Q2, Q3, Q4, Q5, Q6, and Q7, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a neorodegenerative disease with these compounds.

CONDENSED HETEROCYCLIC DERIVATIVES AS BCL-2 INHIBITORS FOR THE TREATMENT OF NEOPLASTIC DISEASES

The disclosure includes compounds of Formula (A) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12, j, k, m, n, Y, W, W1, W2, W3, V, L, Z1, Q1, Q2, Q3, and Q4, are defined herein. Also disclosed is a method for treatinga neoplastic disease, an autoimmune disease, or a neorodegenerative disease with these compounds.

Novel indazoles for the treatment and prophylaxis of respiratory syncytial virus infection

The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds.

Novel indazoles for the treatment and prophylaxis of respiratory syncytial virus infection

The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds.

NOVEL INDAZOLES FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS INFECTION

The invention provides novel compounds having the general formula: formula (I) wherein R1, R2, R3, R4, R5, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds.

One-pot sequence for the decarboxylation of α-amino acids

Treatment of an α-amino acid with N-bromosuccinimide in water at pH 5 or in an alcoholic-aqueous ammonium chloride mixture, followed by addition of nickel(II) chloride and sodium borohydride, effected an overall decarboxylation via an intermediate nitrile to afford the corresponding amine in good yield.

Synthesis and antitumor activity of 6 trifluoromethylcyclophosphamide and related compounds

In an attempt to increase the combined toxicity of the metabolic end products [acrolein (4) and phosphoramide mustard (3)] from cyclophosphamide (1), the analog 2 [bis(2 chloroethyl)amino] tetrahydro 6 trifluoromethyl 2H 1,3,2 oxazaphosphorine 2 oxide (2,6 trifluoromethyl cyclophosphamide) was synthesized and its metabolism and antitumor activity studied. Following metabolism of 2 by rat liver microsomes the predicted formation of 4,4,4 trifluorocrotonaldehyde (5) was confirmed by isolation and identification, by mass spectrometry, of its dinitrophenylhydrazone. The therapeutic indices (LD50/ID90) for 2 against the ADJ/PC6 mouse tumor and the Walker 256 tumor in the rat were 28.6 and 7.7, respectively, and were lower than the corresponding values for 1 (91.8 and 33.2, respectively) although the toxicities toward Walker cells in a bioassay system of 1 and 2 dollowing microsomal metabolism were similar. In order to study the toxicities of 4 and 5 released under drug metabolizing conditions independently of the production of a toxic mustard the analogs 18 [2 (diethylamino)tetrahydro 2H 1,3,2 oxazaphosphorine 2 oxide) and 6 [2 (diethylamino)tetrahydro 6 trifluoromethyl 2H 1,3,2 oxazaphosphorine 2 oxide] were also synthesized. The release of 5 from 6 following metabolism was confirmed and shown by use of the bioassay system to be an event of similar toxicity to release of 4 from 18; in vivo, however, 6 (LD50330 mg/kg) was more toxic to mice than 18 (ld50>500 mg/kg).