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1. (WO2019046931) COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USE THEREOF AS INHIBITORS OF RAN GTPASE
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Pub. No.: WO/2019/046931 International Application No.: PCT/CA2018/051045
Publication Date: 14.03.2019 International Filing Date: 30.08.2018
IPC:
C07D 307/20 (2006.01) ,A61K 31/122 (2006.01) ,A61K 31/135 (2006.01) ,A61K 31/14 (2006.01) ,A61K 31/166 (2006.01) ,A61K 31/17 (2006.01) ,A61K 31/18 (2006.01) ,A61K 31/24 (2006.01) ,A61K 31/277 (2006.01) ,A61K 31/341 (2006.01) ,A61K 31/381 (2006.01) ,A61K 31/426 (2006.01) ,A61K 31/444 (2006.01) ,A61K 31/495 (2006.01) ,A61P 35/00 (2006.01) ,C07C 211/27 (2006.01) ,C07C 211/50 (2006.01) ,C07C 211/63 (2006.01) ,C07C 275/58 (2006.01) ,C07C 233/65 (2006.01) ,C07C 237/42 (2006.01) ,C07C 255/57 (2006.01) ,C07C 275/40 (2006.01) ,C07C 275/62 (2006.01) ,C07C 311/16 (2006.01) ,C07C 327/02 (2006.01) ,C07C 43/23 (2006.01) ,C07D 213/30 (2006.01) ,C07D 213/38 (2006.01) ,C07D 257/04 (2006.01) ,C07D 277/56 (2006.01) ,C07D 295/03 (2006.01) ,C07D 295/073 (2006.01) ,C07D 295/096 (2006.01) ,C07D 295/135 (2006.01) ,C07D 307/24 (2006.01) ,C07D 307/52 (2006.01) ,C07D 307/66 (2006.01) ,C07D 333/20 (2006.01) ,C07D 417/04 (2006.01)
C CHEMISTRY; METALLURGY
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ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
307
Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02
not condensed with other rings
04
having no double bonds between ring members or between ring members and non-ring members
18
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
20
Oxygen atoms
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
12
Ketones
122
having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
13
Amines, e.g. amantadine
135
having aromatic rings, e.g. methadone
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
13
Amines, e.g. amantadine
14
Quaternary ammonium compounds, e.g. edrophonium, choline
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
16
Amides, e.g. hydroxamic acids
165
having aromatic rings, e.g. colchicine, atenolol, progabide
166
having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
16
Amides, e.g. hydroxamic acids
17
having the group N-C(O)-N or N-C(S)-N, e.g. urea, thiourea, carmustine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
16
Amides, e.g. hydroxamic acids
18
Sulfonamides
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
21
Esters, e.g. nitroglycerine, selenocyanates
215
of carboxylic acids
235
having an aromatic ring attached to a carboxyl group
24
having an amino or nitro group
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
275
Nitriles; Isonitriles
277
having a ring, e.g. verapamil
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
335
having oxygen as the only ring hetero atom, e.g. fungichromin
34
having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
341
not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
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
38
having sulfur as a ring hetero atom
381
having five-membered 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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425
Thiazoles
426
1,3-Thiazoles
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
444
containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
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
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
C CHEMISTRY; METALLURGY
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ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
211
Compounds containing amino groups bound to a carbon skeleton
01
having amino groups bound to acyclic carbon atoms
26
of an unsaturated carbon skeleton containing at least one six-membered aromatic ring
27
having amino groups linked to the six-membered aromatic ring by saturated carbon chains
C CHEMISTRY; METALLURGY
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ORGANIC CHEMISTRY
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ACYCLIC OR CARBOCYCLIC COMPOUNDS
211
Compounds containing amino groups bound to a carbon skeleton
43
having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
44
having amino groups bound to only one six-membered aromatic ring
49
having at least two amino groups bound to the carbon skeleton
50
with at least two amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
C CHEMISTRY; METALLURGY
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ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
211
Compounds containing amino groups bound to a carbon skeleton
62
Quaternary ammonium compounds
63
having quaternised nitrogen atoms bound to acyclic carbon atoms
C CHEMISTRY; METALLURGY
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ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
275
Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups
46
containing any of the groups X being a hetero atom, Y being any atom, e.g. acylureas
58
Y being a hetero atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
233
Carboxylic acid amides
64
having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
65
having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
C CHEMISTRY; METALLURGY
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ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
237
Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
28
having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
42
having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
C CHEMISTRY; METALLURGY
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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
57
containing cyano groups and carboxyl groups, other than cyano groups, bound to the carbon skeleton
C CHEMISTRY; METALLURGY
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ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
275
Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups
28
having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
40
being further substituted by nitrogen atoms not being part of nitro or nitroso groups
C CHEMISTRY; METALLURGY
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ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
275
Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups
46
containing any of the groups X being a hetero atom, Y being any atom, e.g. acylureas
58
Y being a hetero atom
62
Y being a nitrogen atom, e.g. biuret
C CHEMISTRY; METALLURGY
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ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
311
Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
15
Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
16
having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
C CHEMISTRY; METALLURGY
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ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
327
Thiocarboxylic acids
02
Monothiocarboxylic acids
C CHEMISTRY; METALLURGY
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ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
43
Ethers; Compounds having groups, groups or groups
02
Ethers
20
having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
23
containing hydroxy or O-metal groups
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
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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
38
having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
257
Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
02
not condensed with other rings
04
Five-membered rings
C CHEMISTRY; METALLURGY
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ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
277
Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
02
not condensed with other rings
20
having two or three double bonds between ring members or between ring members and non-ring members
32
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
56
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C CHEMISTRY; METALLURGY
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ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
295
Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
02
containing only hydrogen and carbon atoms in addition to the ring hetero elements
027
containing only one hetero ring
03
with the ring nitrogen atoms directly attached to acyclic carbon atoms
C CHEMISTRY; METALLURGY
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ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
295
Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
04
with substituted hydrocarbon radicals attached to ring nitrogen atoms
06
substituted by halogen atoms or nitro radicals
073
with the ring nitrogen atoms and the substituents separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
C CHEMISTRY; METALLURGY
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ORGANIC CHEMISTRY
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HETEROCYCLIC COMPOUNDS
295
Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
04
with substituted hydrocarbon radicals attached to ring nitrogen atoms
08
substituted by singly bound oxygen or sulfur atoms
096
with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
C CHEMISTRY; METALLURGY
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ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
295
Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
04
with substituted hydrocarbon radicals attached to ring nitrogen atoms
12
substituted by singly or doubly bound nitrogen atoms
135
with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
307
Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02
not condensed with other rings
04
having no double bonds between ring members or between ring members and non-ring members
18
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
24
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
307
Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02
not condensed with other rings
34
having two or three double bonds between ring members or between ring members and non-ring members
38
with substituted hydrocarbon radicals attached to ring carbon atoms
52
Radicals substituted by nitrogen atoms not forming part of a nitro radical
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
307
Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02
not condensed with other rings
34
having two or three double bonds between ring members or between ring members and non-ring members
56
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
66
Nitrogen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
333
Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
02
not condensed with other rings
04
not substituted on the ring sulfur atom
06
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
14
Radicals substituted by singly bound hetero atoms other than halogen
20
by nitrogen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
Applicants:
THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING/MCGILL UNIVERSITY [CA/CA]; Office of Sponsored Research James Administration Building 845 Sherbrooke Street West, 4th floor Montreal, Québec H3A 0G4, CA
VAL-CHUM, LIMITED PARTNERSHIP [CA/CA]; 3, Place Ville Marie, bureau 12350 Montreal, Québec H3B 0E7, CA
Inventors:
WU, Jian Hui; CA
BATIST, Gerald; CA
TIAN, Xiaochong; CN
LI, Xiaolong; CN
MES-MASSON, Anne-Marie; CA
PROVENCHER, Diane; CA
CARMONA, Euridice; CA
Agent:
LAVERY, DE BILLY, LLP; 1 Place Ville Marie, Suite 4000 Montréal, Québec H3B 4M4, CA
Priority Data:
62/554,15005.09.2017US
Title (EN) COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USE THEREOF AS INHIBITORS OF RAN GTPASE
(FR) COMPOSÉS, COMPOSITIONS PHARMACEUTIQUES ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE LA RAN GTPASE
Abstract:
(EN) Compounds of general formula IA, IB and IC outlined below, including pharmaceutically acceptable salts, solvates and hydrates thereof. Such compounds and pharmaceutical compositions comprising them may be used in medical conditions involving Ran GTPase.
(FR) L'invention concerne des composés de formule générale IA, IB et IC tels que décrits ci-dessous, comprenant des sels, des solvates et des hydrates pharmaceutiquement acceptables de ceux-ci. Les composés et les compositions pharmaceutiques les comprenant selon la présente invention peuvent être utilisés dans des états médicaux impliquant une Ran GTPase.
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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)