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1. (WO2019008156) INHIBITORS OF THE PD-1/PD-L1 PROTEIN/PROTEIN INTERACTION
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Pub. No.: WO/2019/008156 International Application No.: PCT/EP2018/068419
Publication Date: 10.01.2019 International Filing Date: 06.07.2018
IPC:
C07C 255/54 (2006.01) ,C07C 271/12 (2006.01) ,C07C 205/34 (2006.01) ,C07D 335/02 (2006.01) ,C07C 217/14 (2006.01) ,C07C 217/48 (2006.01) ,C07C 217/76 (2006.01) ,C07C 323/25 (2006.01) ,C07D 213/30 (2006.01) ,C07D 213/36 (2006.01) ,C07D 305/06 (2006.01) ,C07D 309/14 (2006.01) ,A61K 31/4409 (2006.01) ,A61P 35/00 (2006.01) ,A61P 31/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
255
Carboxylic acid nitriles
49
having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
54
containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
271
Derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups
06
Esters of carbamic acids
08
having oxygen atoms of carbamate groups bound to acyclic carbon atoms
10
with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
12
to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
205
Compounds containing nitro groups bound to a carbon skeleton
27
the carbon skeleton being further substituted by etherified hydroxy groups
34
having nitro groups bound to carbon atoms of six-membered aromatic rings and etherified hydroxy groups bound to acyclic carbon atoms of the carbon skeleton
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
335
Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
02
not condensed with other rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
217
Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
02
having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
04
the carbon skeleton being acyclic and saturated
06
having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted
14
the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
217
Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
02
having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
48
the carbon skeleton being unsaturated and containing rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
217
Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
76
having amino groups bound to carbon atoms of six-membered aromatic rings and etherified hydroxy groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
323
Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
23
containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
24
having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
25
the carbon skeleton being acyclic and saturated
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
213
Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02
having three double bonds between ring members or between ring members and non-ring members
04
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
24
with substituted hydrocarbon radicals attached to ring carbon atoms
28
Radicals substituted by singly-bound oxygen or sulfur atoms
30
Oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
213
Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02
having three double bonds between ring members or between ring members and non-ring members
04
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
24
with substituted hydrocarbon radicals attached to ring carbon atoms
36
Radicals substituted by singly-bound nitrogen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
305
Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
02
not condensed with other rings
04
having no double bonds between ring members or between ring members and non-ring members
06
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
309
Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
02
having no double bonds between ring members or between ring members and non-ring members
08
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
14
Nitrogen atoms not forming part of a nitro radical
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
4409
only substituted in position 4, e.g. isoniazid, iproniazid
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
Applicants:
RIJKSUNIVERSITEIT GRONINGEN [NL/NL]; Broerstraat 5 9712 CP Groningen, NL
Inventors:
DÖMLING, Alexander; NL
Agent:
FORSTMEYER, Dietmar; DE
PAUSTIAN, Othmar; DE
LIECK, H.-Peter; DE
Priority Data:
17180369.507.07.2017EP
Title (EN) INHIBITORS OF THE PD-1/PD-L1 PROTEIN/PROTEIN INTERACTION
(FR) INHIBITEURS DE L'INTERACTION PROTÉINE/PROTÉINE PD-1/PD-L1
Abstract:
(EN) The present invention provides novel compounds of formula (I) that are useful as inhibitors of the PD-1/PD-L1 protein/protein interaction. The compounds may be used in the treatment of cancer, infectious diseases and neurodegenerative diseases such as schizophrenia, Alzheimer, multiple sclerosis or Parkinson.
(FR) La présente invention concerne de nouveaux composés de formule (I) qui sont utiles en tant qu'inhibiteurs de l’interaction protéine/protéine PD-1/PD-L1. Les composés peuvent être utilisés dans le traitement du cancer, de maladies infectieuses et de maladies neurodégénératives telles que la schizophrénie, la maladie d'Alzheimer, la sclérose en plaques ou la maladie de Parkinson.
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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)