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1. US20150166489 - Bis(fluoroalkyl)-1,4-benzodiazepinone compounds and prodrugs thereof

Office
United States of America
Application Number 14627573
Application Date 20.02.2015
Publication Number 20150166489
Publication Date 18.06.2015
Grant Number 09273014
Grant Date 01.03.2016
Publication Kind B2
IPC
A61K 38/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
A61K 47/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
C07D 243/24
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
243Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
06having the nitrogen atoms in positions 1 and 4
10condensed with carbocyclic rings or ring systems
141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
16substituted in position 5 by aryl radicals
18substituted in position 2 by nitrogen, oxygen or sulfur atoms
24Oxygen atoms
A61K 31/5513
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
55having seven-membered rings, e.g. azelastine, pentylenetetrazole
551having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
55131,4-Benzodiazepines, e.g. diazepam
A61K 31/573
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopentahydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
57substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane, progesterone
573substituted in position 21, e.g. cortisone, dexamethasone, prednisone
A61K 31/675
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
66Phosphorus compounds
675having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
CPC
C07D 243/24
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
243Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
06having the nitrogen atoms in positions 1,4
10condensed with carbocyclic rings or ring systems
141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
16substituted in position 5 by aryl radicals
18substituted in position 2 by nitrogen, oxygen or sulfur atoms
24Oxygen atoms
A61K 9/0019
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
0012Galenical forms characterised by the site of application
0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
A61K 9/0095
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
0087Galenical forms not covered by A61K9/02 - A61K9/7023
0095Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
A61K 9/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
08Solutions
A61K 9/4866
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
48Preparations in capsules, e.g. of gelatin, of chocolate
4841Filling excipients; Inactive ingredients
4866Organic macromolecular compounds
A61K 31/138
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
13Amines
135having aromatic rings ; , e.g. ketamine, nortriptyline
138Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
Applicants Bristol-Myers Squibb Company
Inventors Ashvinikumar V. Gavai
George V. DeLucca
Daniel O'Malley
Patrice Gill
Claude A. Quesnelle
Brian E. Fink
Yufen Zhao
Francis Y. Lee
Agents Gary D. Greenblatt
Title
(EN) Bis(fluoroalkyl)-1,4-benzodiazepinone compounds and prodrugs thereof
Abstract
(EN)

Disclosed are compounds of Formula (I) and/or salts thereof:


wherein R1 is —CH2CH2CF3; R2 is —CH2CH2CF3 or —CH2CH2CH2CF3; R3 is H, —CH3, or Rx; R4 is H or Ry; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein. 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; or as prodrugs of such compounds.


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