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Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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Pharmaceuticals Containing Other Organic And Inorganic Compounds
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Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur
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Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems
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Claims (17)
1.Jedinjenje, naznačeno time, što ima Formulu Iili neka njegova farmaceutski prihvatljiva so, pri čemu:prsten A je izabran iz prstena A-1 i A-2 sa sledećim strukturama:gde naborana linija označena sa 1 pokazuje tačku spajanja prsten A na prsten B, a naborana linija označena sa 2 pokazuje tačku spajanja prstena A na W;X je N ili CH;Y je H ili F;R1 je H, (1-3C)alkoksi ili halogen;pri čemu kada prsten B je B-1,gde naborana linija označena sa 3 pokazuje tačku spajanja na prsten A, a naborana linija označena sa 4 pokazuje tačku spajanja na pirazolo[1,5-a]pirimidinski prsten iz Formule I;W je O, NH ili CH2, pri čemu kada prsten A je A-2, tada W je CH2;m je 0, 1 ili 2;D je ugljenik, R2 i R2a su nezavisno H, F, (1-3 C)alkil ili OH (pod uslovom da R2 i R2a nisu oba OH), a R3 i R3a su nezavisno H, (1-3 C)alkil ili hidroksi(1-3 C)alkil,Z je *-NR4aC(=O)-, pri čemu zvezda pokazuje tačku spajanja Z na ugljenik koji nosi R3;R4a je H, (1-6C)alkil, fluoro(1-6C)alkil, difluoro(1-6C)alkil, trifluoro(1-6C)alkil, hidroksi(1-6C alkil) ili dihidroksi(2-6C alkil); aR5 i R6 su nezavisno H, halogen, OH, (1-6C)alkil ili hidroksi(1-6C)alkil.1. A compound of Formula I or a pharmaceutically acceptable salt thereof, wherein: ring A is selected from rings A-1 and A-2 having the following structures: where the wrinkled line marked with 1 shows the point of joining ring A to the ring B, and the wrinkled line marked 2 shows the point of attachment of ring A to W; X is N or CH; Y is H or F; R 1 is H, (1-3C) alkoxy or halogen; wherein when ring B is B-1 ,where the folded line labeled 3 shows the point of attachment to ring A, and the folded line labeled 4 shows the point of attachment to the pyrazolo[1,5-a]pyrimidine ring of Formula I; W is O, NH, or CH2, wherein when the ring A is A-2, then W is CH2; m is 0, 1 or 2; D is carbon, R2 and R2a are independently H, F, (1-3 C)alkyl or OH (provided that R2 and R2a are not both OH), and R3 and R3a are independently H, (1-3 C)alkyl or hydroxy(1-3 C)alkyl, Z is *-NR4aC(=O)-, where the star indicates the point of attachment of Z to the carbon bearing R3;R4a is H, (1-6C)alkyl, fluoro(1-6C)alkyl, difluoro(1-6C)alkyl, trifluoro(1-6C)alkyl, hydroxy(1-6C alkyl) or dihydroxy(2-6C alkyl); aR5 and R6 are independently H, halogen, OH, (1-6C)alkyl or hydroxy(1-6C)alkyl.2.Jedinjenje u skladu sa zahtevom 1, naznačeno time, što prsten A je prsten A-1 sa strukturom:2. The compound according to claim 1, characterized in that ring A is ring A-1 with the structure:3.Jedinjenje u skladu sa zahtevom 1, naznačeno time, što prsten A je prsten A-2 sa strukturom:3. Compound according to claim 1, characterized in that ring A is ring A-2 with the structure:4.Jedinjenje u skladu sa bilo kojim od zahteva 1-3, naznačeno time, što Y je F.4. A compound according to any one of claims 1-3, characterized in that Y is F.5.Jedinjenje u skladu sa bilo kojim od zahteva 1-4, naznačeno time, što R1 je H.5. A compound according to any one of claims 1-4, characterized in that R1 is H.6.Jedinjenje u skladu sa bilo kojim od zahteva 1-5, naznačeno time, što R4a je vodonik.6. A compound according to any one of claims 1-5, characterized in that R4a is hydrogen.7.Jedinjenje u skladu sa bilo kojim od zahteva 1-6, naznačeno time, što R2 i R2a su atomi vodonika.7. The compound according to any one of claims 1-6, characterized in that R2 and R2a are hydrogen atoms.8.Jedinjenje u skladu sa bilo kojim od zahteva 1-7, naznačeno time, što W je CH2.8. A compound according to any one of claims 1-7, characterized in that W is CH2.9.Jedinjenje u skladu sa bilo kojim od zahteva 1-8, naznačeno time, što m je 0.9. A compound according to any one of claims 1-8, wherein m is 0.10.Jedinjenje u skladu sa bilo kojim od zahteva 1-8, naznačeno time, što m je 1.10. A compound according to any one of claims 1-8, characterized in that m is 1.11.Jedinjenje iz zahteva 1, naznačeno time, što je izabrano iz sledećih jedinjenja: (6R)-9-fluoro-2,11,15,19,20,23-heksaazapentaciklo[15.5.2.17,110.2,6.020,24]pentakosa-1(23),7,9,17(24),18,21-heksaen-16,25-dion; (6R)-9-fluoro-13-oksa-2,11,17,21,22,25-heksaazapentaciklo[17.5.2.02,6.07,12.022,26]heksakosa-1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9-fluoro-15-hidroksi-13-oksa-2,11,17,21,22,25-heksaazapentaciklo[17.5.2.02,6.07,120.22,26]heksakosa-1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R,13S)-9-fluoro-13-hidroksi-2,11,15,19,20,23-heksaazapentaciklo-[15.5.2.17,11.02,6.020,24]pentakosa-1(23),7,9,17(24),18,21-heksaen-16,25-dion; (6R,15R)-9-fluoro-15-hidroksi-13-oksa-2,11,17,21,22,25-heksaazapentaciklo-[17.5.2.02,6.07,12.022,26]heksakosa-1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R,13R)-9-fluoro-13-hidroksi-2,11,15,19,20,23-heksaazapentaciklo-[15.5.2.17,11.02,6.020,24]pentakosa-1(23),7,9,17(24),18,21-heksaen-16,25-dion; (6R)-9-fluoro-13-oksa-2,11,16,20,21,24-heksaazapentaciklo[16.5.2.02,6.07,12.021,25]pentakosa-1(24),7,9,11,18(25),19,22-heptaen-17-on; (6R)-9-fluoro-13-oksa-2,11,18,22,23,26-heksaazapentaciklo[18.5.2.02,6.07,12.023,27]heptakosa-1(26),7,9,11,20(27),21,24-heptaen-19-on; (6R)-9-fluoro-2,11,16,20,21,24-heksaazapentaciklo[16.5.2.17,11.02,6.021,25]heksakosa-1(24),7,9,18(25),19,22-heksaen-17,26-dion; (6R)-9-fluoro-2,11,13,16,20,21,24-heptaazapentaciklo[16.5.2.02,6.07,12.021,25]pentakosa-1(24),7,9,11,18(25),19,22-heptaen-17-on; (6R)-9-fluoro-2,11,13,17,21,22,25-heptaazapentaciklo[17.5.2.02,6.07,12.022,26]heksakosa-1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9-fluoro-14-oksa-2,11,18,19,22-pentaazapentaciklo[14.5.2.17,11.02,6.019,23]tetracosa-1(22),7,9,16(23),17,20-heksaen-15,24-dion; (6R,13R)-9,13-difluoro-2,11,15,19,20,23-heksaazapentaciklo[15.5.2.17,11.02,6.020,24]pentakosa-1 (23), 7,9,17(24),18,21-heksaen-16,25-dion; (6R)-9-fluoro-17-metil-13-oksa-2,11,17,21,22,25-heksaazapentaciklo[17.5.2.02,6.07,12.022,26]-heksakosa-1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9,15,15-trifluoro-13-oksa-2,11,17,21,22,25-heksaazapentaciklo-[17.5.2.02,6.07,12.022,26]heksakosa-1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9-fluoro-2,11,16,20,21,24-heksaazapentaciklo[16.5.2.02,6.07,12.021,25]pentakosa-1(24),7,9,11,18(25),19,22-heptaen-17-on; (6R)-9-fluoro-15-metil-2,11,16,20,21,24-heksaazapentaciklo-[16.5.2.02,6.07,12.021,25]pentakosa-1(24),7,9,11,18(25),19,22-heptaen-17-on; (6R,13R)-9-fluoro-13-metil-2,11,15,19,20,23-heksaazapentaciklo-[15.5.2.17,11.02,6.020,24pentakosa-1(23),7,9,17(24),18,21-heksaen-16,25-dion; (6R,13S)-9-fluoro-13-metil-2,11,15,19,20,23-heksaazapentaciklo-[15.5.2.17,11.02,6.020,24]pentakosa-1(23),7,9,17(24),18,21-heksaen-16,25-dion; (6R)-9-fluoro-15,15-dimetil-13-oksa-2,11,17,21,22,25-heksaazapentaciklo-[17.5.2.02,6.07,12.022,26]heksakosa-1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9-fluoro-15,15-dimetil-2,11,16,20,21,24-heksaazapentaciklo-[16.5.2.02,6.07,12.021,25]pentakosa-1(24),7,9,11,18(25),19,22-heptaen-17-on; i (6R)-9-fluoro-13,13-dimetil-2,11,15,19,20,23-heksaazapentaciklo[15.5.2.17,11.02,6.020,24]-pentakosa-1(23),7,9,17(24),18,21-heksaen-16,25-dion; ili neka njegova farmaceutski prihvatljiva so.11.Jedinjenje iz nadrava 1, nadsenato time, što je obslavano iz nadvejnih compounds: (6R)-9-fluoro-2,11,15,19,20,23-hexaazapentacyclo[15.5.2.17,110.2,6.020,24]pentakosa -1(23),7,9,17(24),18,21-hexaene-16,25-dione; (6R)-9-fluoro-13-oksa-2,11,17,21,22,25-hexaazapentacyclo[17.5.2.02,6.07,12.022,26]heksakosa-1(25),7,9,11,19 (26),20,23-heptaen-18-one; (6R)-9-fluoro-15-hydroxy-13-oxa-2,11,17,21,22,25-hexaazapentacyclo[17.5.2.02,6.07,120.22,26]heksakosa-1(25),7,9 ,11,19(26),20,23-heptaen-18-one; (6R,13S)-9-fluoro-13-hydroxy-2,11,15,19,20,23-hexaazapentacyclo-[15.5.2.17,11.02,6.020,24]pentakosa-1(23),7,9, 17(24),18,21-hexaene-16,25-dione; (6R,15R)-9-fluoro-15-hydroxy-13-oksa-2,11,17,21,22,25-hexaazapentacyclo-[17.5.2.02,6.07,12.022,26]heksakosa-1(25), 7,9,11,19(26),20,23-heptaen-18-one; (6R,13R)-9-fluoro-13-hydroxy-2,11,15,19,20,23-hexaazapentacyclo-[15.5.2.17,11.02,6.020,24]pentakosa-1(23),7,9, 17(24),18,21-hexaene-16,25-dione; (6R)-9-fluoro-13-oxa-2,11,16,20,21,24-hexaazapentacyclo[16.5.2.02,6.07,12.021,25]pentakosa-1(24),7,9,11,18 (25),19,22-heptaen-17-one; (6R)-9-fluoro-13-oxa-2,11,18,22,23,26-hexaazapentacyclo[18.5.2.02,6.07,12.023,27]heptakosa-1(26),7,9,11,20 (27),21,24-heptaen-19-one; (6R)-9-fluoro-2,11,16,20,21,24-hexaazapentacyclo[16.5.2.17,11.02,6.021,25]heksakosa-1(24),7,9,18(25),19, 22-hexaene-17,26-dione; (6R)-9-fluoro-2,11,13,16,20,21,24-heptaazapentacyclo[16.5.2.02,6.07,12.021,25]pentakosa-1(24),7,9,11,18(25 ),19,22-heptaen-17-one; (6R)-9-fluoro-2,11,13,17,21,22,25-heptaazapentacyclo[17.5.2.02,6.07,12.022,26]heksakosa-1(25),7,9,11,19(26 ),20,23-heptaen-18-one; (6R)-9-fluoro-14-oxa-2,11,18,19,22-pentaazapentacyclo[14.5.2.17,11.02,6.019,23]tetracosa-1(22),7,9,16(23), 17,20-hexaene-15,24-dione; (6R,13R)-9,13-difluoro-2,11,15,19,20,23-hexaazapentacyclo[15.5.2.17,11.02,6.020,24]pentakosa-1 (23), 7,9,17(24 ),18,21-hexaene-16,25-dione; (6R)-9-fluoro-17-metil-13-oksa-2,11,17,21,22,25-hexaazapentacyclo[17.5.2.02,6.07,12.022,26]-heksakosa-1(25),7, 9,11,19(26),20,23-heptaen-18-one; (6R)-9,15,15-trifluoro-13-oksa-2,11,17,21,22,25-hexaazapentaciklo-[17.5.2.02,6.07,12.022,26]heksakosa-1(25),7, 9,11,19(26),20,23-heptaen-18-one; (6R)-9-fluoro-2,11,16,20,21,24-hexaazapentacyclo[16.5.2.02,6.07,12.021,25]pentakosa-1(24),7,9,11,18(25), 19,22-heptaen-17-one; (6R)-9-fluoro-15-methyl-2,11,16,20,21,24-hexaazapentacyclo-[16.5.2.02,6.07,12.021,25]pentakosa-1(24),7,9,11, 18(25),19,22-heptaen-17-one; (6R,13R)-9-fluoro-13-methyl-2,11,15,19,20,23-hexaazapentacyclo-[15.5.2.17,11.02,6.020,24pentakosa-1(23),7,9,17( 24),18,21-hexaene-16,25-dione; (6R,13S)-9-fluoro-13-methyl-2,11,15,19,20,23-hexaazapentacyclo-[15.5.2.17,11.02,6.020,24]pentakosa-1(23),7,9, 17(24),18,21-hexaene-16,25-dione; (6R)-9-fluoro-15,15-dimethyl-13-oksa-2,11,17,21,22,25-hexaazapentacyclo-[17.5.2.02,6.07,12.022,26]heksakosa-1(25), 7,9,11,19(26),20,23-heptaen-18-one; (6R)-9-fluoro-15,15-dimethyl-2,11,16,20,21,24-hexaazapentacyclo-[16.5.2.02,6.07,12.021,25]pentakosa-1(24),7,9, 11,18(25),19,22-heptaen-17-one; i (6R)-9-fluoro-13,13-dimethyl-2,11,15,19,20,23-hexaazapentacyclo[15.5.2.17,11.02,6.020,24]-pentakosa-1(23),7,9 ,17(24),18,21-hexaene-16,25-dione; ili neka njega pharmaceutics acceptable so.12.Jedinjenje iz zahteva 1, naznačeno time, što je izabrano iz sledećih jedinjenja: (6R)-9-fluoro-13-oksa-2,11,17,21,22,25-heksaazapentaciklo[17.5.2.02,6.07,12.022,26]heksakosa-1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9-fluoro-15-hidroksi-13-oksa-2,11,17,21,22,25-heksaazapentaciklo[17.5.2.02.6.07,12.022,26]-heksakosa-1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R,15R)-9-fluoro-15-hidroksi-13-oksa-2,11,17,21,22,25-heksaazapentaciklo-[17.5.2.02,6.07,12.022,26]heksakosa-1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9-fluoro-13-oksa-2,11,16,20,21,24-heksaazapentaciklo[16.5.2.02,6.07,12.021,25]pentakosa-1(24),7,9,11,18(25),19,22-heptaen-17-on; (6R)-9-fluoro-13-oksa-2,11,18,22,23,26-heksaazapentaciklo[18.5.2.02,6.07,12.023,27]heptakosa-1(26),7,9,11,20(27),21,24-heptaen-19-on; (6R)-9-fluoro-2,11,13,16,20,21,24-heptaazapentaciklo[16.5.2.02,6.07,12.021,25]pentakosa-1(24),7,9,11,18(25),19,22-heptaen-17-on; (6R)-9-fluoro-2,11,13,17,21,22,25-heptaazapentaciklo[17.5.2.02,6.07,12.022,26]heksakosa-1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9-fluoro-17-metil-13-oksa-2,11,17,21,22,25-heksaazapentaciklo[17.5.2.02,6.07,12.022,26]-heksakosa-1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9,15,15-trifluoro-13-oksa-2,11,17,21,22,25-heksaazapentaciklo-[17.5.2.02,6.07,12.022,26]heksakosa-1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9-fluoro-2,11,16,20,21-,24-heksaazapentaciklo[16.5.2.02,6.07,12.021,25]pentakosa-1(24),7,9,11,18(25),19,22-heptaen-17-on; (6R)-9-fluoro-15-metil-2,11,16,20,21,24-heksaazapentaciklo-[16.5.2.02,6.07,12.021,25]pentakosa-1(24),7,9,11,18(25),19,22-heptaen-17-on; (6R)-9-fluoro-15,15-dimetil-13-oksa-2,11,17,21,22,25-heksaazapentaciklo-[17.5.2 .02,6.07,12.022,26]heksakosa-1(25),7,9,11,19(26),20,23-heptaen-18-on; i (6R)-9-fluoro-15,15-dimetil-2,11,16,20,21,24-heksaazapentaciklo-[16.5.2.02,6.07,12.021,25]pentakosa-1(24),7,9,11,18(25),19,22-heptaen-17-on; ili neka njegova farmaceutski prihvatljiva so.12.Jedinjenje from claim 1, indicated by the following compounds: (6R)-9-fluoro-13-oxa-2,11,17,21,22,25-hexaazapentacyclo[17.5.2.02,6.07,12.022 ,26]hexakosa-1(25),7,9,11,19(26),20,23-heptaen-18-one; (6R)-9-fluoro-15-hydroxy-13-oksa-2,11,17,21,22,25-hexaazapentacyclo[17.5.2.02.6.07,12.022,26]-heksakosa-1(25),7, 9,11,19(26),20,23-heptaen-18-one; (6R,15R)-9-fluoro-15-hydroxy-13-oksa-2,11,17,21,22,25-hexaazapentacyclo-[17.5.2.02,6.07,12.022,26]heksakosa-1(25), 7,9,11,19(26),20,23-heptaen-18-one; (6R)-9-fluoro-13-oxa-2,11,16,20,21,24-hexaazapentacyclo[16.5.2.02,6.07,12.021,25]pentakosa-1(24),7,9,11,18 (25),19,22-heptaen-17-one; (6R)-9-fluoro-13-oxa-2,11,18,22,23,26-hexaazapentacyclo[18.5.2.02,6.07,12.023,27]heptakosa-1(26),7,9,11,20 (27),21,24-heptaen-19-one; (6R)-9-fluoro-2,11,13,16,20,21,24-heptaazapentacyclo[16.5.2.02,6.07,12.021,25]pentakosa-1(24),7,9,11,18(25 ),19,22-heptaen-17-one; (6R)-9-fluoro-2,11,13,17,21,22,25-heptaazapentacyclo[17.5.2.02,6.07,12.022,26]heksakosa-1(25),7,9,11,19(26 ),20,23-heptaen-18-one; (6R)-9-fluoro-17-metil-13-oksa-2,11,17,21,22,25-hexaazapentacyclo[17.5.2.02,6.07,12.022,26]-heksakosa-1(25),7, 9,11,19(26),20,23-heptaen-18-one; (6R)-9,15,15-trifluoro-13-oksa-2,11,17,21,22,25-hexaazapentaciklo-[17.5.2.02,6.07,12.022,26]heksakosa-1(25),7, 9,11,19(26),20,23-heptaen-18-one; (6R)-9-fluoro-2,11,16,20,21-,24-hexaazapentacyclo[16.5.2.02,6.07,12.021,25]pentakosa-1(24),7,9,11,18(25) ,19,22-heptaen-17-one; (6R)-9-fluoro-15-methyl-2,11,16,20,21,24-hexaazapentacyclo-[16.5.2.02,6.07,12.021,25]pentakosa-1(24),7,9,11, 18(25),19,22-heptaen-17-one; (6R)-9-fluoro-15,15-dimethyl-13-oksa-2,11,17,21,22,25-hexaazapentacyclo-[17.5.2 .02,6.07,12.022,26]heksakosa-1(25 ),7,9,11,19(26),20,23-heptaen-18-one; i (6R)-9-fluoro-15,15-dimethyl-2,11,16,20,21,24-hexaazapentacyclo[16.5.2.02,6.07,12.021,25]pentakosa-1(24),7,9 ,11,18(25),19,22-heptaen-17-one; ili neka njega pharmaceutics acceptable so.13.Jedinjenje iz zahteva 1, naznačeno time, što je izabrano iz sledećih jedinjenja: (6R)-9-fluoro-2,11,15,19,20,23-heksaazapentaciklo[15.5.2.17,11.02,6.020,24]pentakosa-1(23),7,9,17(24),18,21-heksaen-16,25-dion; (6R,13S)-9-fluoro-13-hidroksi-2,11,15,19,20,23-heksaazapentaciklo-[15.5.2.17,11.02,6.020,24]-pentakosa-1(23),7,9,17(24),18,21-heksaen-16,25-dion; (6R,13R)-9-fluoro-13-hidroksi-2,11,15,19,20,23-heksaazapentaciklo-[15.5.2.17,11.02,6.020,24]-pentakosa-1(23),7,9,17(24),18,21-heksaen-16,25-dion; (6R)-9-fluoro-2,11,16,20,21,24-heksaazapentaciklo[16.5.2.17,11.02,6.021,25]heksakosa-1(24),7,9,18(25),19,22-heksaen-17,26-dion; (6R)-9-fluoro-14-oksa-2,11,18,19,22-pentaazapentaciklo[14.5.2.17,11.02,6.019,23]tetracosa-1(22),7,9, 16(23),17,20-heksaen-15,24-dion; (6R,13R)-9,13-difluoro-2,11,15,19,20,23-heksaazapentaciklo[15.5.2.17,11.02,6.020,24]pentakosa-1(23), 7,9,17(24),18,21-heksaen-16,25-dion; (6R,13R)-9-fluoro-13-metil-2,11,15,19,20,23-heksaazapentaciklo-[15.5.2.17,11.02,6.020,24]pentakosa-1(23),7,9,17(24),18,21-heksaen-16,25-dion; (6R,13,S)-9-fluoro-13-metil-2,11,15,19,20,23-heksaazapentaciklo-[15.5.2.17,11.02,6.020,24]pentakosa-1(23),7,9,17(24),18,21-heksaen-16,25-dion; i (6R)-9-fluoro-13,13-dimetil-2,11,15,19,20,23-heksaazapentaciklo[15.5.2.17,11.02,6.020,24]pentakosa-1(23),7,9,17(24),18,21-heksaen-16,25-dion; ili neka njegova farmaceutski prihvatljiva so.13. The compound of claim 1, characterized in that it is selected from the following compounds: (6R)-9-fluoro-2,11,15,19,20,23-hexaazapentacyclo[15.5.2.17,11.02,6.020,24]pentacosa -1(23),7,9,17(24),18,21-hexaene-16,25-dione; (6R,13S)-9-fluoro-13-hydroxy-2,11,15,19,20,23-hexaazapentacyclo-[15.5.2.17,11.02,6.020,24]-pentacosa-1(23),7,9 ,17(24),18,21-hexaene-16,25-dione; (6R,13R)-9-fluoro-13-hydroxy-2,11,15,19,20,23-hexaazapentacyclo-[15.5.2.17,11.02,6.020,24]-pentacosa-1(23),7,9 ,17(24),18,21-hexaene-16,25-dione; (6R)-9-fluoro-2,11,16,20,21,24-hexaazapentacyclo[16.5.2.17,11.02,6.021,25]hexacose-1(24),7,9,18(25),19, 22-hexaene-17,26-dione; (6R)-9-fluoro-14-oxa-2,11,18,19,22-pentaazapentacyclo[14.5.2.17,11.02,6.019,23]tetracosa-1(22),7,9, 16(23), 17,20-hexaene-15,24-dione; (6R,13R)-9,13-difluoro-2,11,15,19,20,23-hexaazapentacyclo[15.5.2.17,11.02,6.020,24]pentacosa-1(23), 7,9,17(24 ), 18,21-hexaene-16,25-dione; (6R,13R)-9-fluoro-13-methyl-2,11,15,19,20,23-hexaazapentacyclo-[15.5.2.17,11.02,6.020,24]pentacosa-1(23),7,9, 17(24),18,21-hexaene-16,25-dione; (6R,13,S)-9-fluoro-13-methyl-2,11,15,19,20,23-hexaazapentacyclo-[15.5.2.17,11.02,6.020,24]pentacosa-1(23),7, 9,17(24),18,21-hexaene-16,25-dione; and (6R)-9-fluoro-13,13-dimethyl-2,11,15,19,20,23-hexaazapentacyclo[15.5.2.17,11.02,6.020,24]pentacosa-1(23),7,9, 17(24),18,21-hexaene-16,25-dione; or a pharmaceutically acceptable salt thereof.14.Farmaceutska kompozicija, naznačena time, što sadrži jedinjenje sa Formulom I kao šta je definisano u bilo kojem od zahteva od 1 do 13, ili neku njegovu farmaceutski prihvatljivu so, i neki farmaceutski prihvatljivi razređivač ili nosilac.14. Pharmaceutical composition, characterized in that it contains a compound of Formula I as defined in any of claims 1 to 13, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable diluent or carrier.15.Jedinjenje sa Formula I, kao šta je definisano u bilo kojem od zahteva od 1 do 12, ili neka njegova farmaceutski prihvatljiva so, naznačeno time, što se upotrebljava u tretmanu boli, raka, zapaljenja, neurodegenerativnih bolesti ili infekcija sa Trypanosoma cruzi.15. A compound of Formula I, as defined in any of claims 1 to 12, or a pharmaceutically acceptable salt thereof, for use in the treatment of pain, cancer, inflammation, neurodegenerative diseases or infections with Trypanosoma cruzi.16.Jedinjenje za primenu iz zahteva 15, naznačeno time, što se upotrebljava u tretmanu raka.16. Compound for application from claim 15, characterized in that it is used in the treatment of cancer.17. Jedinjenje za primenu iz zahteva 16, naznačeno time, što pomenuti je rak izabran iz grupe koja obuhvata: neuroblastom, rak jajnika, kolorektalni rak, melanom, rak glave i vrata, karcinom želuca, karcinom pluća, rak dojke, glioblastom, meduloblastom, sekretorni rak dojke, rak pljuvačne žlezde, papilarni karcinom štitaste žlezde, mijeloidnu leukemiju odraslih, rak pankreasa, i rak prostate.17. Compound for use from claim 16, characterized in that said cancer is selected from the group comprising: neuroblastoma, ovarian cancer, colorectal cancer, melanoma, head and neck cancer, stomach cancer, lung cancer, breast cancer, glioblastoma, medulloblastoma, secretory breast cancer, salivary gland cancer, papillary thyroid cancer, adult myeloid leukemia, pancreatic cancer, and prostate cancer.
MEP-2017-161A2010-05-202011-05-13
Macrocyclic compounds as TRK kinase inhibitors
ME02808B
(en)
N-Acyl- (3-substituted) - (8-methyl) -5,6-dihydro- [1,2,4] triazolo [4,3-a] pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in disorders mediated by the NK-3 receptor
Compounds derived from imidazo [1,2-a] pyrazin-7-yl; pharmaceutical composition comprising one of the compounds; and use of one of the compounds in the preparation of a medicament useful for treating a disease related to the genus plasmodium in a subject.
Pharmaceutical formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one