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1. WO2012129353 - BIS(FLUOROALKYL)-1,4-BENZODIAZEPINONE COMPOUNDS

Publication Number WO/2012/129353
Publication Date 27.09.2012
International Application No. PCT/US2012/030021
International Filing Date 22.03.2012
IPC
C07D 243/24 2006.01
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 2006.01
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
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
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
A61K 31/337
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
337having four-membered rings, e.g. taxol
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 nitrogen atoms, e.g. dilazep
55131,4-Benzodiazepines, e.g. diazepam ; or clozapine
A61K 31/555
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
555containing heavy metals, e.g. hemin, hematin, melarsoprol
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 cyclopenta[a]hydrophenanthrene ring systems; Derivatives, 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 ; or aldosterone
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
Applicants
  • BRISTOL-MYERS SQUIBB COMPANY [US]/[US] (AllExceptUS)
  • QUESNELLE, Claude [CA]/[US] (UsOnly)
  • KIM, Soong-Hoon [US]/[US] (UsOnly)
  • LEE, Francis [CN]/[US] (UsOnly)
  • GAVAI, Ashvinikumar [US]/[US] (UsOnly)
Inventors
  • QUESNELLE, Claude
  • KIM, Soong-Hoon
  • LEE, Francis
  • GAVAI, Ashvinikumar
Agents
  • GREENBLATT, Gary D.
Priority Data
61/466,23822.03.2011US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) BIS(FLUOROALKYL)-1,4-BENZODIAZEPINONE COMPOUNDS
(FR) COMPOSÉS BIS(FLUOROALKYL)-1,4-BENZODIAZÉPINONE
Abstract
(EN)
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.
(FR)
L'invention concerne des composés de Formule (I) ou leurs promédicaments ; dans laquelle R1 représente CH2CF3 ou CH2CH2CF3 ; R2 représente CH2CF3, CH2CH2CF3, ou CH2CH2CH2CF3 ; R3 représente H ou CH3; chaque Ra représente indépendamment F, Cl, -CN, -OCH3 et/ou NHCH2CH2OCH3 ; et z vaut zéro, 1 ou 2. Elle concerne également des procédés d'utilisation de ces composés pour inhiber le récepteur Notch, et des compositions pharmaceutiques comprenant ces composés. Ces composés sont utiles dans le traitement, la prévention ou le ralentissement de l'évolution de maladies ou de troubles dans divers domaines thérapeutiques, comme le traitement du cancer.
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