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1. (WO2019027783) [1,2,4]TRIAZOLO[4,3-A]PYRAZIN-6(5H)-ONE DERIVATIVES
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Pub. No.: WO/2019/027783 International Application No.: PCT/US2018/043845
Publication Date: 07.02.2019 International Filing Date: 26.07.2018
IPC:
C07D 471/14 (2006.01) ,A61K 31/4985 (2006.01) ,A61P 13/12 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
12
in which the condensed system contains three hetero rings
14
Ortho-condensed systems
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
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
4985
Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13
Drugs for disorders of the urinary system
12
of the kidneys
Applicants:
ELI LILLY AND COMPANY [US/US]; Lilly Corporate Center Indianapolis, Indiana 46285, US
Inventors:
GENIN, Michael James; US
HOLLOWAY, William Glen; US
JOHNSTON, Richard Duane; US
MORPHY, John Richard; US
SHI, Qing; US
Agent:
LENTZ, Nelsen L.; US
EBERSOLE, Ted J.; US
Priority Data:
62/540,12202.08.2017US
Title (EN) [1,2,4]TRIAZOLO[4,3-A]PYRAZIN-6(5H)-ONE DERIVATIVES
(FR) DÉRIVÉS DE [1,2,4]TRIAZOLO[4,3-A]PYRAZIN-6(5H)-ONE
Abstract:
(EN) The present invention provides a compound of Formula (I), wherein X is H or C1-C3 alkyl optionally substituted with hydroxyl; Y is H, hydroxy, or methyl; R is ethyl, n-propyl, cyclopropyl, or Formula (II); and A is methyl, cyclopropyl or trifluorom ethyl; or a pharmaceutically acceptable salt thereof; with the proviso that when X and Y are both H and R is n-propyl, then A is other than methyl; for use as a human PDEl inhibitor.
(FR) La présente invention concerne un composé de formule (I), dans laquelle X représente H ou un alkyle en C1-C3 éventuellement substitué par hydroxyle ; Y représente H, hydroxy ou méthyle ; R représente éthyle, n-propyle, cyclopropyle ou formule (II) ; et A représente méthyle, cyclopropyle ou trifluorom éthyle ; ou un sel pharmaceutiquement acceptable de celui-ci ; à condition que lorsque X et Y sont tous les deux H, et R représente n-propyle, alors A est différent du méthyle ; l'invention concerne également l'utilisation du composé en tant qu'inhibiteur de PDEl humain.
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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)