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1. (WO2018129274) OXADIAZOLE INHIBITORS OF HIPK2 FOR TREATING KIDNEY FIBROSIS
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Pub. No.: WO/2018/129274 International Application No.: PCT/US2018/012512
Publication Date: 12.07.2018 International Filing Date: 05.01.2018
IPC:
C07D 271/04 (2006.01) ,C07D 271/06 (2006.01) ,C07D 271/07 (2006.01) ,C07D 271/08 (2006.01) ,C07D 271/10 (2006.01) ,C07D 271/107 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
271
Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
02
not condensed with other rings
04
1,2,3-Oxadiazoles; Hydrogenated 1,2,3-oxadiazoles
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
271
Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
02
not condensed with other rings
06
1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
271
Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
02
not condensed with other rings
06
1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
07
with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
271
Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
02
not condensed with other rings
08
1,2,5-Oxadiazoles; Hydrogenated 1,2,5-oxadiazoles
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
271
Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
02
not condensed with other rings
10
1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
271
Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
02
not condensed with other rings
10
1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
107
with two aryl or substituted aryl radicals attached in positions 2 and 5
Applicants:
ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI [US/US]; One Gustave L. Levy Place Box 1675 New York, New York 10029, US
UNIVERSITY OF KANSAS [US/US]; 245 Strong Hall 1450 Jayhawk Boulevard Lawrence, Kansas 66045, US
Inventors:
HE, John Cijiang; US
LIU, Ruijie; US
DAS, Bhaskar; US
XIAO, Wenzhen; US
LI, Zhengzhe; US
LEE, Kyung; US
Agent:
HANSEN, Philip E.; US
Priority Data:
62/443,37006.01.2017US
62/445,46112.01.2017US
Title (EN) OXADIAZOLE INHIBITORS OF HIPK2 FOR TREATING KIDNEY FIBROSIS
(FR) INHIBITEURS D'OXADIAZOLE DE HIPK2 POUR LE TRAITEMENT DE LA FIBROSE RÉNALE
Abstract:
(EN) Compounds that are selective inhibitors of Smad3 activation are disclosed. The compounds have the structure (I) in which Z is an oxadiazole. The compounds disclosed are useful in treatment of fibrotic disease, particularly renal fibrosis, and similar diseases associated with the dysregulation of the HIPK2/Smad3 signaling pathway.
(FR) L'invention concerne des composés qui sont des inhibiteurs sélectifs de l'activation de Smad3. Les composés présentent la structure (I) dans laquelle Z est un oxadiazole. Les composés décrits sont utiles dans le traitement d'une maladie fibrotique, en particulier d'une fibrose rénale, et de maladies similaires associées à la dérégulation de la voie de signalisation HIPK2/Smad3.
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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, JO, 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 Office (AM, AZ, BY, KG, KZ, 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, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)