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1. (WO2018157800) MLKL INHIBITORS
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Pub. No.: WO/2018/157800 International Application No.: PCT/CN2018/077464
Publication Date: 07.09.2018 International Filing Date: 27.02.2018
IPC:
C07D 473/12 (2006.01) ,C07D 473/08 (2006.01) ,C07D 473/10 (2006.01) ,C07D 513/14 (2006.01) ,A61K 31/522 (2006.01) ,A61K 31/542 (2006.01) ,A61P 29/00 (2006.01) ,A61P 25/28 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
473
Heterocyclic compounds containing purine ring systems
02
with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6
04
two oxygen atoms
06
with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
12
with methyl radicals in positions 1, 3, and 7, e.g. caffeine
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
473
Heterocyclic compounds containing purine ring systems
02
with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6
04
two oxygen atoms
06
with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
08
with methyl radicals in positions 1 and 3, e.g. theophylline
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
473
Heterocyclic compounds containing purine ring systems
02
with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6
04
two oxygen atoms
06
with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
10
with methyl radicals in positions 3 and 7, e.g. theobromine
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
513
Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/, C07D477/232
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
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519
ortho- or peri-condensed with heterocyclic rings
52
Purines, e.g. adenine
522
having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
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
54
having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
542
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
29
Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
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
28
for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
Applicants:
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING [CN/CN]; 7 Science Park Rd., ZGC Life Science Park Changping District Beijing 102206, CN
Inventors:
ZHANG, Zhiyuan; CN
WANG, Xiaodong; CN
HUANG, Shaoqiang; CN
YAN, Bo; CN
LIU, Lei; CN
WANG, Huayi; CN
YAO, Zhenglin; CN
HAN, Jianguang; CN
HUANG, Zhi; CN
CAO, Weiye; CN
Priority Data:
PCT/CN2017/07524828.02.2017CN
Title (EN) MLKL INHIBITORS
(FR) INHIBITEURS MLKL
Abstract:
(EN) Purine derivatives that inhibit cellular necroptosis and/or human MLKL, pharmaceutical compositions thereof, and methods of treating an MLKL-mediated disorder with an effective amount of the compound or composition. Said MLKL-mediated disorder is pathology associated necroptosis, including ischemia-reperfusion damage, neurodegeneration, and inflammatory diseases such as acute pancreatitis, multiple sclerosis, inflammatory bowel disease, and allergic colitis.
(FR) L'invention concerne des dérivés de purine qui inhibent la nécroptose cellulaire et/ou MLKL humaine, des compositions pharmaceutiques associées, et des méthodes de traitement d'un trouble à médiation assurée par MLKL avec une dose efficace du composé ou de la composition. Le trouble à médiation assurée par MLKL est une pathologie associée à la nécroptose, notamment les lésions d'ischémie-reperfusion, la neurodégénérescence et les maladies inflammatoires de type pancréatite aiguë, sclérose en plaques, affection abdominale inflammatoire, et colite allergique.
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)