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1. (WO2011095625) 1,2,4-TRIAZINE-4-AMINE DERIVATIVES
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2011/095625 International Application No.: PCT/EP2011/051755
Publication Date: 11.08.2011 International Filing Date: 07.02.2011
IPC:
C07D 253/07 (2006.01) ,C07D 401/04 (2006.01) ,C07D 401/12 (2006.01) ,C07D 401/14 (2006.01) ,C07D 403/04 (2006.01) ,C07D 403/12 (2006.01) ,C07D 405/04 (2006.01) ,C07D 405/10 (2006.01) ,C07D 413/04 (2006.01) ,C07D 417/12 (2006.01) ,C07D 487/04 (2006.01) ,A61K 31/53 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
253
Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/166
02
not condensed with other rings
06
1,2,4-Triazines
065
having three double bonds between ring members or between ring members and non-ring members
07
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
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02
containing two hetero rings
10
linked by a carbon chain containing aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
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
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02
in which the condensed system contains two hetero rings
04
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
53
having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
Applicants:
CONGREVE, Miles Stuart [GB/GB]; GB (UsOnly)
ANDREWS, Stephen Philippe [GB/GB]; GB (UsOnly)
MASON, Jonathan Stephen [GB/GB]; GB (UsOnly)
RICHARDSON, Christine Mary [GB/GB]; GB (UsOnly)
BROWN, Giles Albert [GB/GB]; GB (UsOnly)
HEPTARES THERAPEUTICS LIMITED [GB/GB]; BioPark Broadwater Road Welwyn Garden City Hertfordshire AL7 3AX, GB (AllExceptUS)
Inventors:
CONGREVE, Miles Stuart; GB
ANDREWS, Stephen Philippe; GB
MASON, Jonathan Stephen; GB
RICHARDSON, Christine Mary; GB
BROWN, Giles Albert; GB
Agent:
SNODIN, Michael D; Potter Clarkson LLP Park View House 58 The Ropewalk Nottingham Nottinghamshire NG1 5DD, GB
Priority Data:
61/302,06005.02.2010US
61/381,76410.09.2010US
Title (EN) 1,2,4-TRIAZINE-4-AMINE DERIVATIVES
(FR) DÉRIVÉS DE 1,2,4-TRIAZINE-4-AMINE
Abstract:
(EN) According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A1- A2b or, particularly, the A2a receptor wherein the compound of formula A1 has the structure, wherein, A represents Cy1 or HetA; Cy1 represents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one, two or three rings, which Cy1 group is optionally substituted by one or more R4a substituents; HetA represents a 5- to 14-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one, two or three rings and which HetA group is optionally substituted by one or more R4b substituents; B represents a Cy2 or HetB; Cy2 represents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, which Cy2 group is optionally substituted by one or more R4c substituents; HetB represents a 3- to 10-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one or two rings and which HetB group is optionally substituted by one or more R4d substituents.
(FR) L'invention concerne un composé de formule A1 qui peut être utile pour le traitement d'un état ou trouble amélioré par l'inhibition d'A1-A2b ou, particulièrement, du récepteur A2a. Selon l'invention, le composé de formule A1 a la structure dans laquelle A représente Cy1 ou HetA ; Cy1 représente un système cyclique carbocyclique aromatique, complètement saturé ou partiellement insaturé de 5 à 14 éléments comprenant un, deux ou trois cycles, ledit groupe Cy1 étant éventuellement substitué par un ou plusieurs substituants R4a ; HetA représente un groupe hétérocyclique de 5 à 14 éléments qui peut être aromatique, complètement saturé ou partiellement insaturé, et qui contient un ou plusieurs hétéroatomes choisis parmi O, S et N, ledit groupe hétérocyclique pouvant comprendre un, deux ou trois cycles et ledit groupe HetA étant éventuellement substitué par un ou plusieurs substituants R4b ; B représente Cy2 ou HetB ; Cy2 représente un système cyclique carbocyclique aromatique, complètement saturé ou partiellement insaturé de 3 à 10 éléments comprenant un ou deux cycles, ledit groupe Cy2 étant éventuellement substitué par un ou plusieurs substituants R4c ; HetB représente un groupe hétérocyclique de 3 à 10 éléments qui peut être aromatique, complètement saturé ou partiellement insaturé, et qui contient un ou plusieurs hétéroatomes choisis parmi O, S et N, ledit groupe hétérocyclique pouvant comprendre un ou deux cycles et ledit groupe HetB étant éventuellement substitué par un ou plusieurs substituants R4d.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, 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, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, 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, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)