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1. (WO2017133990) PYRAZOL-PYRIDINE DERIVATIVES AS EAAT3 INHIBITORS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/133990 International Application No.: PCT/EP2017/051873
Publication Date: 10.08.2017 International Filing Date: 30.01.2017
IPC:
C07D 401/04 (2006.01) ,C07D 409/14 (2006.01) ,A61K 31/4439 (2006.01) ,A61P 25/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
409
Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
14
containing three or more hetero rings
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
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4427
containing further heterocyclic ring systems
4439
containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
Applicants:
F. HOFFMANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse 124 4070 Basel, CH (AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BE, BF, BG, BH, BJ, BN, BR, BW, BY, BZ, CA, CF, CG, CH, CI, CL, CM, CN, CO, CR, CU, CY, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, FR, GA, GB, GD, GE, GH, GM, GN, GQ, GR, GT, GW, HN, HR, HU, ID, IE, IL, IN, IR, IS, IT, JP, KE, KG, KH, KM, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MC, MD, ME, MG, MK, ML, MN, MR, MT, MW, MX, MY, MZ, NA, NE, NG, NI, NL, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SI, SK, SL, SM, SN, ST, SV, SY, SZ, TD, TG, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, UZ, VC, VN, ZA, ZM, ZW)
HOFFMANN-LA ROCHE INC. [US/US]; Overlook at Great Notch, 150 Clove Road, 8th Floor, Suite 8 - Legal Department Little Falls, New Jersey 07424, US (US)
Inventors:
WICHMANN, Juergen; CH
HOENER, Marius; CH
Agent:
BERNARD, Guillaume; CH
Priority Data:
16153741.002.02.2016EP
Title (EN) PYRAZOL-PYRIDINE DERIVATIVES AS EAAT3 INHIBITORS
(FR) DÉRIVÉS PYRAZOL-PYRIDINE UTILISÉS COMME INHIBITEURS D'EAAT3
Abstract:
(EN) The present invention relates to compounds of formula I wherein R1' is CH3; R1 is CH3, ethyl, CF3, CH2OH, cyclopropyl or cyano, or R1' and R1 may form together a 1,1-dioxo-tetrahydro-thiophen-3-yl ring; R2 is hydrogen, CH3, ethyl, isopropyl, tert-butyl, cyclopropyl, cyclopropyl-methyl or hydroxy- methyl; R3 is hydrogen, CI, F, CF3, CH3, isopropyl, methoxy, cyano or cyclopropyl; R4 is hydrogen, CH3, F or CI; or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds of formula I may be used in the treatment of psychiatric disorders such as schizophrenia, bipolar disorder, obsessive-compulsive disorder or autism spectrum disorder.
(FR) La présente invention concerne des composés de formule I où R1' est CH3 ; R1 est CH3, éthyle, CF3, CH2OH, cyclopropyle ou cyano, ou R1' et R1 peuvent former ensemble un cycle 1,1-dioxo-tétrahydro-thiophène-3-yle ; R2 est hydrogène, CH3, éthyle, isopropyle, tert-butyle, cyclopropyle, cyclopropyl-méthyle ou hydroxy-méthyle ; R3 est hydrogène, CI, F, CF3, CH3, isopropyle, méthoxy, cyano ou cyclopropyle ; R4 est hydrogène, CH3, F ou CI ; ou un sel ou sel d'addition acide pharmaceutiquement acceptable, un mélange racémique, ou un énantiomère et/ou isomère optique et/ou stéréoisomère correspondant. Les composés de formule (I) peuvent être utilisés pour le traitement de troubles psychiatriques, par exemple la schizophrénie, les troubles bipolaires, les troubles obsessionnels-compulsifs ou les troubles du spectre de l'autisme.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, 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, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (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, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
AR107490CN108473462US20180339975EP3411365