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1. (WO2012129353) BIS(FLUOROALKYL)-1,4-BENZODIAZEPINONE COMPOUNDS
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2012/129353 International Application No.: PCT/US2012/030021
Publication Date: 27.09.2012 International Filing Date: 22.03.2012
IPC:
C07D 243/24 (2006.01) ,A61K 31/5513 (2006.01) ,A61P 35/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
243
Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
06
having the nitrogen atoms in positions 1 and 4
10
condensed with carbocyclic rings or ring systems
14
1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
16
substituted in position 5 by aryl radicals
18
substituted in position 2 by nitrogen, oxygen or sulfur atoms
24
Oxygen atoms
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
55
having seven-membered rings, e.g. azelastine, pentylenetetrazole
551
having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
5513
1,4-Benzodiazepines, e.g. diazepam
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
QUESNELLE, Claude [CA/US]; US (UsOnly)
KIM, Soong-Hoon [US/US]; US (UsOnly)
LEE, Francis [CN/US]; US (UsOnly)
GAVAI, Ashvinikumar [US/US]; US (UsOnly)
BRISTOL-MYERS SQUIBB COMPANY [US/US]; P.O. Box 4000 Route 206 and ProvinceLine Road Princeton, New Jersey 08543-4000, US (AllExceptUS)
Inventors:
QUESNELLE, Claude; US
KIM, Soong-Hoon; US
LEE, Francis; US
GAVAI, Ashvinikumar; US
Agent:
GREENBLATT, Gary D.; Bristol-Myers Squibb Company P.O. Box 4000 Princeton, New Jersey 08543-4000, US
Priority Data:
61/466,23822.03.2011US
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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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)