HRP20200549T1 - Određeni amino-pirimidini, njihovi sastavi, i metode njihove upotrebe - Google Patents
Određeni amino-pirimidini, njihovi sastavi, i metode njihove upotrebe Download PDFInfo
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- HRP20200549T1 HRP20200549T1 HRP20200549TT HRP20200549T HRP20200549T1 HR P20200549 T1 HRP20200549 T1 HR P20200549T1 HR P20200549T T HRP20200549T T HR P20200549TT HR P20200549 T HRP20200549 T HR P20200549T HR P20200549 T1 HRP20200549 T1 HR P20200549T1
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- 150000005005 aminopyrimidines Chemical class 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- 101150100019 NRDC gene Proteins 0.000 claims 56
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 53
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 42
- 125000001424 substituent group Chemical group 0.000 claims 41
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 39
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 38
- 125000003710 aryl alkyl group Chemical group 0.000 claims 31
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 30
- 229910052736 halogen Inorganic materials 0.000 claims 30
- 150000001875 compounds Chemical class 0.000 claims 29
- 150000002367 halogens Chemical class 0.000 claims 29
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 26
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims 26
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 25
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 25
- 150000003839 salts Chemical class 0.000 claims 23
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 22
- 229910052739 hydrogen Inorganic materials 0.000 claims 20
- 239000001257 hydrogen Substances 0.000 claims 20
- 125000001072 heteroaryl group Chemical group 0.000 claims 16
- 125000000753 cycloalkyl group Chemical group 0.000 claims 15
- 229910052799 carbon Inorganic materials 0.000 claims 14
- 125000004432 carbon atom Chemical group C* 0.000 claims 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 150000002431 hydrogen Chemical class 0.000 claims 10
- -1 cyclobutyl 3-fluorocyclobutyl Chemical group 0.000 claims 6
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000002541 furyl group Chemical group 0.000 claims 6
- 125000002883 imidazolyl group Chemical group 0.000 claims 6
- 125000001786 isothiazolyl group Chemical group 0.000 claims 6
- 125000000842 isoxazolyl group Chemical group 0.000 claims 6
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 6
- 125000002971 oxazolyl group Chemical group 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000000168 pyrrolyl group Chemical group 0.000 claims 6
- 125000003831 tetrazolyl group Chemical group 0.000 claims 6
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 6
- 125000000335 thiazolyl group Chemical group 0.000 claims 6
- 125000001544 thienyl group Chemical group 0.000 claims 6
- 125000001425 triazolyl group Chemical group 0.000 claims 6
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 5
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 4
- 125000001624 naphthyl group Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 208000002320 spinal muscular atrophy Diseases 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- 229910052731 fluorine Inorganic materials 0.000 claims 3
- 239000011737 fluorine Substances 0.000 claims 3
- 125000005412 pyrazyl group Chemical group 0.000 claims 3
- 125000005495 pyridazyl group Chemical group 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- 206010028289 Muscle atrophy Diseases 0.000 claims 2
- 208000005764 Peripheral Arterial Disease Diseases 0.000 claims 2
- 208000030831 Peripheral arterial occlusive disease Diseases 0.000 claims 2
- 208000018262 Peripheral vascular disease Diseases 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 201000000585 muscular atrophy Diseases 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 1
- 206010007558 Cardiac failure chronic Diseases 0.000 claims 1
- 206010008874 Chronic Fatigue Syndrome Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 108010010803 Gelatin Proteins 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 1
- 229930195725 Mannitol Natural products 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010049565 Muscle fatigue Diseases 0.000 claims 1
- 208000021642 Muscular disease Diseases 0.000 claims 1
- 201000009623 Myopathy Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 229920002472 Starch Polymers 0.000 claims 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims 1
- 229930006000 Sucrose Natural products 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 1
- SIKJAQJRHWYJAI-UHFFFAOYSA-N benzopyrrole Natural products C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 239000001913 cellulose Substances 0.000 claims 1
- 229920002678 cellulose Polymers 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 230000006735 deficit Effects 0.000 claims 1
- 239000008273 gelatin Substances 0.000 claims 1
- 229920000159 gelatin Polymers 0.000 claims 1
- 235000019322 gelatine Nutrition 0.000 claims 1
- 235000011852 gelatine desserts Nutrition 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 claims 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 238000007918 intramuscular administration Methods 0.000 claims 1
- 238000007912 intraperitoneal administration Methods 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 239000008101 lactose Substances 0.000 claims 1
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 claims 1
- 239000001095 magnesium carbonate Substances 0.000 claims 1
- 229910000021 magnesium carbonate Inorganic materials 0.000 claims 1
- 235000019359 magnesium stearate Nutrition 0.000 claims 1
- 239000000594 mannitol Substances 0.000 claims 1
- 235000010355 mannitol Nutrition 0.000 claims 1
- DOTMOQHOJINYBL-UHFFFAOYSA-N molecular nitrogen;molecular oxygen Chemical group N#N.O=O DOTMOQHOJINYBL-UHFFFAOYSA-N 0.000 claims 1
- 230000020763 muscle atrophy Effects 0.000 claims 1
- 230000003387 muscular Effects 0.000 claims 1
- 208000029766 myalgic encephalomeyelitis/chronic fatigue syndrome Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 208000018360 neuromuscular disease Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 239000008107 starch Substances 0.000 claims 1
- 235000019698 starch Nutrition 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 239000005720 sucrose Substances 0.000 claims 1
- 229910052717 sulfur Chemical group 0.000 claims 1
- 239000011593 sulfur Chemical group 0.000 claims 1
- 239000000454 talc Substances 0.000 claims 1
- 229910052623 talc Inorganic materials 0.000 claims 1
Classifications
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- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- C07D213/04—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 having three double bonds between ring members or between ring members and non-ring members 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
- C07D213/60—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 having three double bonds between ring members or between ring members and non-ring members 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 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07D401/00—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
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- C—CHEMISTRY; METALLURGY
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- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
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- C07—ORGANIC CHEMISTRY
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- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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- C07D513/04—Ortho-condensed systems
Claims (26)
1. Spoj formule I:
[image]
ili njegova farmaceutski prihvatljiva sol, gdje :
R1 je izabran od vodika, halogena, CN, CF3 i metila;
R2 je izabran od C3-8 cikloalkila, C3-8 cikloalkenila, 3-8-članog heterocikloalkila, 3-8-članog heterocikloalkenila, C6-10 arila, 5-10-članog heteroarila i NRbRc, gdje svaki od C3-8 cikloalkila, C3-8 cikloalkenila, 3-8-članog heterocikloalkila, 3-8-članog heterocikloalkenila, C6-10 arila i 5-10-člane heteroarilne grupe je opcionalno supstituiran s 1, 2, 3, 4 ili 5 supstituta izabranih od halogena, CN, okso, (CH2)nORa, (CH2)nOC(O)Ra, (CH2)nOC(O)ORa, (CH2)nOC(O)NRbRc, (CH2)nNRbRc, (CH2)nNRdC(O)Ra, (CH2)nNRdC(O)ORa, (CH2)nNRdC(O)NRbRc, (CH2)nNRdC(O)C(O)NRbRc, (CH2)nNRdC(S)Ra, (CH2)nNRdC(S)ORa, (CH2)nNRdC(S)NRbRc, (CH2)nNRdC(NRe)NRbRc, (CH2)nNRdS(O)Ra, (CH2)nNRdSO2Ra, (CH2)nNRdSO2NRbRc, (CH2)nC(O)Ra, (CH2)nC(O)ORa, (CH2)nC(O)NRbRc, (CH2)nC(S)Ra, (CH2)nC(S)ORa, (CH2)nC(S)NRbRc, (CH2)nC(NRe)NRbRc, (CH2)nSRa, (CH2)nS(O)Ra, (CH2)nSO2Ra, (CH2)nSO2NRbRc, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, (CH2)nC3-8 cikloalkila, (CH2)n3-8-članog heterocikloalkila, (CH2)nC6-10 arila i (CH2)n5-10-članog heteroarila, gdje je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, (CH2)nC3-8 cikloalkil, (CH2)n3-8-člani heterocikloalkil, (CH2)nC6-10 aril i (CH2)n5-10-člane heteroarilne grupe opcionalno supstituiran s 1, 2, 3, 4 ili 5 Rf supstituta;
R3 je izabran od vodika, halogena, CN, CF3 i metila;
R4 je izabran od vodika, C1-6 alkila, C1-6 haloalkila, C(O)Ra, C(O)ORa, C(O)NRbRc i SO2Ra;
R5 i R6 zajedno s ugljikovim atomom za koji su vezani oblikuju grupu izabranu između C3-8 cikloalkila, C3-8 cikloalkenila, 3-8-članog heterocikloalkila i 3-8-članog heterocikloalkenila, svaku opcionalno supstituiranu s 1, 2, 3, 4 ili 5 supstituta izabranih od halogena, CN, okso, ORa, OC(O)Ra, OC(O)ORa, NRbRc, C(O)Ra, C(O)ORa, C(O)NRbRc, S(O)Ra, SO2Ra, SO2NRbRc, C1-6 alkila i C1-6 haloalkila;
R7 je izabran od C3-8 cikloalkila, C3-8 cikloalkenila, 3-8-članog heterocikloalkila, 3-8-članog heterocikloalkenila, C6-10 arila i 5-10-članog heteroarila, svakog opcionalno supstituiranog s 1, 2, 3, 4 ili 5 supstituta izabranih od halogena, CN, okso, ORa, OC(O)Ra, OC(O)ORa, OC(O)NRbRc, NRbRc, NRdC(O)Ra, NRdC(O)ORa, NRdC(O)NRbRc, NRdC(O)C(O)NRbRc, NRdC(S)Ra, NRdC(S)ORa, NRdC(S)NRbRc, NRdC(NRe)NRbRc, NRdS(O)Ra, NRdSO2Ra, NRdSO2NRbRc, C(O)Ra, C(O)ORa, C(O)NRbRc, C(S)Ra, C(S)ORa, C(S)NRbRc, C(NRe)NRbRc, SRa, S(O)Ra, SO2Ra, SO2NRbRc, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, C3-8 cikloalkila, C3-8 cikloalkenila, 3-8-članog heterocikloalkila, 3-8-članog heterocikloalkenila, C6-10 arila, C7-11 aralkil, i 5-10-članog heteroarila, gdje je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C3-8 cikloalkil, C3-8 cikloalkenil, 3-8-člani heterocikloalkil, 3-8-člani heterocikloalkenil, C6-10 aril, C7-11 aralkil i 5-10-člane heteroarilne grupe opcionalno supstituiran s 1, 2, 3, 4 ili 5 Rf supstituta;
R8 i R9, u svakom slučaju, su svaki nezavisno izabrani između vodika, halogena i C1-6 alkila;
X je veza;
ili alternativno, X, R2 i R3, zajedno s ugljikovim atomima za koji su vezani, oblikuju 5-6-člani prsten koji opcionalno sadrži jedan ili više heteroatoma izabranih između kisika dušika i sumpora, i opcionalno sadrži jednu ili više dvostrukih veza, i opcionalno supstituiran s 1, 2, 3, 4 ili 5 Rf supstituta;
Ra, u svakom slučaju, je nezavisno izabran između vodika, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, C3-8 cikloalkila, C3-8 cikloalkenila, 3-8-članog heterocikloalkila, 3-8-članog heterocikloalkenila, C6-10 arila, C7-11 aralkila i 5-10-članog heteroarila, gdje je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C3-8 cikloalkil, C3-8 cikloalkenil, 3-8-člani heterocikloalkil, 3-8-člani heterocikloalkenil, C6-10 aril, C7-11 aralkil i 5-10-člane heteroarilne grupe opcionalno supstituiran s 1, 2, 3, 4 ili 5 Rf supstituta;
Rb i Rc, u svakom slučaju, su svaki nezavisno izabrani između vodika, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, C3-8 cikloalkila, C3-8 cikloalkenila, 3-8-članog heterocikloalkila, 3-8-članog heterocikloalkenila, C6-10 arila, C7-11 aralkila, 5-10-članog heteroarila, C(O)Rg, C(O)ORg, C(O)NRiRj i SO2Rg, gdje je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C3-8 cikloalkil, C3-8 cikloalkenil, 3-8-člani heterocikloalkil, 3-8-člani heterocikloalkenil, C6-10 aril, C7-11 aralkil i 5-10-člane heteroarilne grupe opcionalno supstituiran s 1, 2, 3, 4 ili 5 Rf supstituta;
Rd, u svakom slučaju, je nezavisno izabran između vodika i C1-6 alkila;
Re, u svakom slučaju, je nezavisno izabran između vodika, CN, OH, C1-6 alkoksi, C1-6 alkil i C1-6 haloalkila;
Rf, u svakom slučaju, je nezavisno izabran između halogena, CN, ORh, OC(O)Rh, OC(O)ORh, OC(O)NRiRj, NRiRj, NRdC(O)Rh, NRdC(O)ORh, NRdC(O)NRiRj, NRdC(O)C(O)NRiRj, NRdC(S)Rh, NRdC(S)ORh, NRdC(S)NRiRj, NRdC(NRe)NRiRj, NRdS(O)Rh, NRdSO2Rh, NRdSO2NRiRj, C(O)Rh, C(O)ORh, C(O)NRiRj, C(S)Rh, C(S)ORh, C(S)NRiRj, C(NRe)NRiRj, SRh, S(O)Rh, SO2Rh, SO2NRiRj, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, C3-8 cikloalkila, C3-8 cikloalkenila, 3-8-članog heterocikloalkila, 3-8-članog heterocikloalkenila, C6-10 arila, C7-11 aralkila i 5-10-članog heteroarila, gdje je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C3-8 cikloalkil, C3-8 cikloalkenil, 3-8-člani heterocikloalkil, 3-8-člani heterocikloalkenil, C6-10 aril, C7-11 aralkil i 5-10-člane heteroarilne grupe opcionalno supstituiran s 1, 2, 3, 4 ili 5 Rk supstituta;
ili dva Rf supstituta vezana za jedan ugljikov atom, zajedno s ugljikovim atomom za koji su oba vezana oblikuju grupu izabranu između karbonila, C3-8 cikloalkila i 3-8-članog heterocikloalkila;
Rg, u svakom slučaju, je nezavisno izabran između C1-6 alkila, C1-6 haloalkila, fenila, naftila, i C7-11 aralkila, svakog opcionalno supstituiranog s 1, 2, 3, 4 ili 5 supstituta izabranih od halogena, CN, OH, C1-6 alkoksi, C1-6 alkila i C1-6 haloalkila;
Rh, u svakom slučaju, je nezavisno izabran između vodika, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, C3-8 cikloalkila, C3-8 cikloalkenila, 3-8-članog heterocikloalkila, 3-8-članog heterocikloalkenila, C6-10 arila, C7-11 aralkil i 5-10-članog heteroarila, gdje je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C3-8 cikloalkil, C3-8 cikloalkenil, 3-8-člani heterocikloalkil, 3-8-člani heterocikloalkenil, C6-10 aril, C7-11 aralkil i 5-10-člane heteroarilne grupe opcionalno supstituiran s 1, 2, 3, 4 ili 5 Rk supstituta;
Ri i Rj, u svakom slučaju, su svaki nezavisno izabrani između vodika, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, C3-8 cikloalkila, C3-8 cikloalkenila, 3-8-članog heterocikloalkila, 3-8-članog heterocikloalkenila, C6-10 arila, C7-11 aralkila, 5-10-članog heteroarila, C(O)Rg, i C(O)ORg, gdje je svaki C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C3-8 cikloalkila, C3-8 cikloalkenila, 3-8-članog heterocikloalkil, 3-8-člani heterocikloalkenil, C6-10 aril, C7-11 aralkil i 5-10-člane heteroarilne grupe opcionalno supstituiran s 1, 2, 3, 4 ili 5 supstituta izabranih od halogena, CN, OH, C1-6 alkoksi, C1-6 alkila i C1-6 haloalkila;
Rk, u svakom slučaju, je nezavisno izabran između halogena, CN, OH, C1-6 alkoksi, NH2, NH(C1-6 alkil), N(C1-6 alkil)2, NHC(O)C1-6 alkila, NHC(O)C7-11 aralkila, NHC(O)OC1-6 alkila, NHC(O)OC7-1, aralkila, OC(O)C1-6 alkila, OC(O)C7-11 aralkila, OC(O)OC1-6 alkila, OC(O)OC7-11 aralkila, C(O)C1-6 alkila, C(O)C7-11 aralkila, C(O)OC1-6 alkila, C(O)OC7-11 aralkila, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, i C2-6 alkinila, gdje svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, i C7-11 aralkil supstitut je opcionalno supstituiran s 1, 2 ili 3 supstituta izabranih od OH, C1-6 alkoksi, NH2, NH(C1-6 alkil), N(C1-6 alkil)2, NHC(O)C1-6 alkil, NHC(O)C7-11 aralkil, NHC(O)OC1-6 alkil, i NHC(O)OC7-11 aralkil; ili dva Rk supstituta vezana za jedan ugljikov atom, zajedno s ugljikovim atomom za koji su oba vezana oblikuje karbonilnu skupinu;
m je 0,1 ili 2;
n, u svakom slučaju, nezavisno je 0, 1 ili 2;
p je 0, 1 ili 2; i
q je 0, 1 ili 2.
2. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, gdje je m 0 ili gdje je m 1.
3. Spoj prema zahtjevu 2, ili njegova farmaceutski prihvatljiva sol, gdje m je 1 i R8 i R9 su svaki vodik.
4. Spoj prema bilo kojem od zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, gdje R5 i R6 zajedno s ugljikovim atomom za koji su vezani oblikuju C3-8 cikloalkil opcionalno supstituiran s 1, 2, 3, 4 ili 5 supstituta izabranih od halogena, CN, okso, ORa, OC(O)Ra, OC(O)ORa, NRbRc, C(O)Ra, C(O)ORa, C(O)NRbRc, S(O)Ra, SO2Ra, SO2NRbRc, C1-6 alkila i C1-6 haloalkila.
5. Spoj prema zahtjevu 4, ili njegova farmaceutski prihvatljiva sol, gdje R5 i R6 zajedno s ugljikovim atomom za koji su vezani oblikuju grupu izabranu između ciklopropila, ciklobutila, ciklopentila i cikloheksila, svaku opcionalno supstituiranu s 1, 2, 3, 4 ili 5 supstituta izabranih od halogena, CN, okso, ORa, OC(O)Ra, OC(O)ORa, NRbRc, C(O)Ra, C(O)ORa, C(O)NRbRc, S(O)Ra, SO2Ra, SO2NRbRc, C1-6 alkila i C1-6 haloalkila.
6. Spoj prema zahtjevu 5, ili njegova farmaceutski prihvatljiva sol, gdje R5 i R6 zajedno s ugljikovim atomom za koji su vezani oblikuju ciklobutil opcionalno supstituiran s 1, 2, 3, 4 ili 5 supstituta izabranih od halogena, CN, okso, ORa, OC(O)Ra, OC(O)ORa, NRbRc, C(O)Ra, C(O)ORa, C(O)NRbRc, S(O)Ra, SO2Ra, SO2NRbRc, C1-6 alkila i C1-6 haloalkila.
7. Spoj prema zahtjevu 6, ili njegova farmaceutski prihvatljiva sol, gdje R5 i R6 zajedno s ugljikovim atomom za koji su vezani oblikuju ciklobutil opcionalno supstituiran s jednim ili dva halogena, posebno, gdje R5 i R6 zajedno s ugljikovim atomom za koji su vezani oblikuju grupu izabranu između ciklobutil 3-fluorociklobutila i 3,3-difluorociklobutila.
8. Spoj prema zahtjevu 6, gdje je spoj formule V(a) ili V(b), ili njegova farmaceutski prihvatljiva sol:
[image]
gdje su Rm i Rn svaki nezavisno izabrani između vodika, halogena, , i C1-6 alkila.
9. Spoj prema zahtjevu 8, ili njegova farmaceutski prihvatljiva sol,
gdje je jedan od Rm i Rn vodik a drugi je halogen,
posebno gdje halogen i R7 su u trans konfiguraciji jedan u odnosu na drugi na ciklobutil prstenu; ili gdje su halogen i R7 u cis konfiguraciji jedan u odnosu na drugi na ciklobutil prstenu.
10. Spoj prema bilo kojem od zahtjeva 8-9, ili njegova farmaceutski prihvatljiva sol, gdje jedan od Rm i Rn je vodik a drugi je fluor.
11. Spoj prema bilo kojem prethodnom zahtjevu, ili njegova farmaceutski prihvatljiva sol, gdje je R7 fenil opcionalno supstituiran s 1, 2, 3, 4 ili 5 supstituta izabranih od halogena, CN, okso, ORa, OC(O)Ra, OC(O)ORa, OC(O)NRbRc, NRbRc, NRdC(O)Ra, NRdC(O)ORa, NRdC(O)NRbRc, NRdC(O)C(O)NRbRc, NRdC(S)Ra, NRdC(S)ORa, NRdC(S)NRbRc, NRdC(NRe)NRbRc, NRdS(O)Ra, NRdSO2Ra, NRdSO2NRbRc, C(O)Ra, C(O)ORa, C(O)NRbRc, C(S)Ra, C(S)ORa, C(S)NRbRc, C(NRe)NRbRc, SRa, S(O)Ra, SO2Ra, SO2NRbRc, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, C3-8 cikloalkila, C3-8 cikloalkenila, 3-8-članog heterocikloalkila, 3-8-članog heterocikloalkenila, C6-10 arila, C7-11 aralkila, i 5-10-članog heteroarila, gdje je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C3-8 cikloalkil, C3-8 cikloalkenil, 3-8-člani heterocikloalkil, 3-8-člani heterocikloalkenil, C6-10 aril, C7-11 aralkil i 5-10-člane heteroarilne grupe opcionalno supstituiran s 1, 2, 3, 4 ili 5 Rf supstituta; ili gdje R7 je 5-10-člani heteroaril opcionalno supstituiran s 1, 2, 3, 4 ili 5 supstituta izabranih od halogena, CN, okso, ORa, OC(O)Ra, OC(O)ORa, OC(O)NRbRc, NRbRc, NRdC(O)Ra, NRdC(O)ORa, NRdC(O)NRbRc, NRdC(O)C(O)NRbRc, NRdC(S)Ra, NRdC(S)ORa, NRdC(S)NRbRc, NRdC(NRe)NRbRc, NRdS(O)Ra, NRdSO2Ra, NRdSO2NRbRc, C(O)Ra, C(O)ORa, C(O)NRbRc, C(S)Ra, C(S)ORa, C(S)NRbRc, C(NRe)NRbRc, SRa, S(O)Ra, SO2Ra, SO2NRbRc, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, C3-8 cikloalkila, C3-8 cikloalkenila, 3-8-članog heterocikloalkila, 3-8-članog heterocikloalkenila, C6-10 arila, C7-11 aralkila, i 5-10-članog heteroarila, gdje je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C3-8 cikloalkil, C3-8 cikloalkenil, 3-8-člani heterocikloalkil, 3-8-člani heterocikloalkenil, C6-10 aril, C7-11 aralkil i 5-10-člane heteroarilne grupe je opcionalno supstituiran s 1, 2, 3, 4 ili 5 Rf supstituta.
12. Spoj prema zahtjevu 11, ili njegova farmaceutski prihvatljiva sol,
gdje R7 je piridil opcionalno supstituiran s 1, 2, 3, 4 ili 5 supstituta izabranih od halogena, CN, okso, ORa, OC(O)Ra, OC(O)ORa, OC(O)NRbRc, NRbRc, NRdC(O)Ra, NRdC(O)ORa, NRdC(O)NRbRc, NRdC(O)C(O)NRbRc, NRdC(S)Ra, NRdC(S)ORa, NRdC(S)NRbRc, NRdC(NRe)NRbRc, NRdS(O)Ra, NRdSO2Ra, NRdSO2NRbRc, C(O)Ra, C(O)ORa, C(O)NRbRc, C(S)Ra, C(S)ORa, C(S)NRbRc, C(NRe)NRbRc, SRa, S(O)Ra, SO2Ra, SO2NRbRc, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, C3-6 cikloalkila, C3-6 cikloalkenila, 3-6-članog heterocikloalkila, 3-6-članog heterocikloalkenila, fenila, naftila, C7-11 aralkila, i 5-10-članog heteroarila, gdje je svaki od C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C3-8 cikloalkila, C3-8 cikloalkenila, 3-8-članog heterocikloalkila, 3-8-članog heterocikloalkenila, C6-10 arila, C7-11 aralkila i 5-10-člane heteroarilne grupe opcionalno supstituiran s 1, 2, 3, 4 ili 5 Rf supstituta,
posebno, gdje R7 je 2-piridil opcionalno supstituiran s 1, 2, 3, 4 ili 5 supstituta izabranih od halogena, CN, okso, ORa, OC(O)Ra, OC(O)ORa, OC(O)NRbRc, NRbRc, NRdC(O)Ra, NRdC(O)ORa, NRdC(O)NRbRc, NRdC(O)C(O)NRbRc, NRdC(S)Ra, NRdC(S)ORa, NRdC(S)NRbRc, NRdC(NRe)NRbRc, NRdS(O)Ra, NRdSO2Ra, NRdSO2NRbRc, C(O)Ra, C(O)ORa, C(O)NRbRc, C(S)Ra, C(S)ORa, C(S)NRbRc, C(NRe)NRbRc, SRa, S(O)Ra, SO2Ra, SO2NRbRc, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, C3-6 cikloalkila, C3-6 cikloalkenila, 3-6-članog heterocikloalkila, 3-6-članog heterocikloalkenila, fenila, naftila, C7-11 aralkila, i 5-10-članog heteroarila, gdje je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C3-8 cikloalkil, C3-8 cikloalkenil, 3-8-člani heterocikloalkil, 3-8-člani heterocikloalkenil, C6-10 aril, C7-11 aralkil i 5-10-člane heteroarilne grupe opcionalno supstituiran s 1, 2, 3, 4 ili 5 Rf supstituta.
13. Spoj prema bilo kojem prethodnom zahtjevu, ili njegova farmaceutski prihvatljiva sol, gdje R2 je fenil opcionalno supstituiran s 1, 2, 3, 4 ili 5 supstituta izabranih od halogena, CN, (CH2)nORa, (CH2)nOC(O)Ra, (CH2)nOC(O)ORa, (CH2)nOC(O)NRbRc, (CH2)nNRbRc, (CH2)nNRdC(O)Ra, (CH2)nNRdC(O)ORa, (CH2)nNRdC(O)NRbRc, (CH2)nNRdC(O)C(O)NRbRc, (CH2)nNRdC(S)Ra, (CH2)nNRdC(S)ORa, (CH2)nNRdC(S)NRbRc, (CH2)nNRdC(NRe)NRbRc, (CH2)nNRdS(O)Ra, (CH2)nNRdSO2Ra, (CH2)nNRdSO2NRbRc, (CH2)nC(O)Ra, (CH2)nC(O)ORa, (CH2)nC(O)NRbRc, (CH2)nC(S)Ra, (CH2)nC(S)ORa, (CH2)nC(S)NRbRc, (CH2)nC(NRe)NRbRc, (CH2)nSRa, (CH2)nS(O)Ra, (CH2)nSO2Ra, (CH2)nSO2NRbRc, C1-6 alkila, C1-6 haloalkila, C2-6 alkenil, C2-6 alkinila, (CH2)nC3-8 cikloalkila, (CH2)n3-8-članog heterocikloalkila, (CH2)nfenila, (CH2)nnaftila i (CH2)n5-10-članog heteroarila, gdje je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, (CH2)nC3-8 cikloalkil, (CH2)n3-8-člani heterocikloalkil, (CH2)nfenil, (CH2)nnaftil i (CH2)n5-10-člane heteroarilne grupe opcionalno supstituiran s 1, 2, 3, 4 ili 5 Rf supstituta.
14. Spoj prema bilo kojem od zahtjeva 1 do 12, ili njegova farmaceutski prihvatljiva sol, gdje R2 je 5-10-člani heteroaril opcionalno supstituiran s 1, 2, 3, 4 ili 5 supstituta izabranih od halogena, CN, okso, (CH2)nO-Ra, (CH2)nOC(O)Ra, (CH2)nOC(O)ORa, (CH2)nOC(O)NRbRc, (CH2)nNRbRc, (CH2)nNRdC(O)Ra, (CH2)nNRdC(O)ORa, (CH2)nNRdC(O)NRbRc, (CH2)nNRdC(O)C(O)NRbRc, (CH2)nNRdC(S)Ra, (CH2)nNRdC(S)ORa, (CH2)nNRdC(S)NRbRc, (CH2)nNRdC(NRe)NRbRc, (CH2)nNRdS(O)Ra, (CH2)nNRdSO2Ra, (CH2)nNRdSO2NRbRc, (CH2)nC(O)Ra, (CH2)nC(O)ORa, (CH2)nC(O)NRbRc, (CH2)nC(S)Ra, (CH2)nC(S)ORa, (CH2)nC(S)NRbRc, (CH2)nC(NRe)NRbRc, (CH2)nSRa, (CH2)nS(O)Ra, (CH2)nSO2Ra, (CH2)nSO2NRbRc, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, (CH2)nC3-8 cikloalkila, (CH2)n3-8-članog heterocikloalkila, (CH2)nfenila, (CH2)nnaftila i (CH2)n5-10-članog heteroarila, gdje je svaki C1-6 alkil, C2-6 alkenil,C2-6 alkinil, (CH2)nC3-8 cikloalkil, (CH2)n3-8-člani heterocikloalkil, (CH2)nfenil, (CH2)nnaftil i (CH2)n5-10-člane heteroarilne grupe opcionalno supstituiran s 1, 2, 3, 4 ili 5 Rf supstituta.
15. Spoj prema zahtjevu 14, ili njegova farmaceutski prihvatljiva sol,
gdje (i) R2 je izabran od indola, indazolila, benzimidazolila, benzoksazolila i benzoizoksazolila, svakog opcionalno supstituiranog s 1, 2, 3 ili 4 supstituta izabranih od halogena, CN, okso, (CH2)nORa, (CH2)nOC(O)Ra, (CH2)nOC(O)ORa (CH2)nOC(O)NRbRc, (CH2)nNRbRc, (CH2)nNRdC(O)Ra, (CH2)nNRdC(O)ORa, (CH2)nNRdC(O)NRbRc, (CH2)nNRdC(O)C(O)NRbRc, (CH2)nNRdC(S)Ra, (CH2)nNRdC(S)ORa, (CH2)nNRdC(S)NRbRc, (CH2)nNRdC(NRe)NRbRc, (CH2)nNRdS(O)Ra, (CH2)nNRdSO2Ra, (CH2)nNRdSO2NRbRc, (CH2)nC(O)Ra, (CH2)nC(O)ORa, (CH2)nC(O)NRbRc, (CH2)nC(S)Ra, (CH2)nC(S)ORa, (CH2)nC(S)NRbRc, (CH2)nC(NRe)NRbRc, (CH2)nSRa, (CH2)nS(O)Ra, (CH2)nSO2Ra, (CH2)nSO2NRbRc, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, (CH2)nC3-8 cikloalkila, (CH2)n3-8-članog heterocikloalkila, (CH2)nfenila, (CH2)nnaftila i (CH2)n5-10-članog heteroarila, gdje je svaki C1-6 alkil, C2-6 alkenil,C2-6 alkinil, (CH2)nC3-8 cikloalkil, (CH2)n3-8-člani heterocikloalkil, (CH2)nfenil, (CH2)nnaftil i (CH2)n5-10-člane heteroarilne grupe opcionalno supstituiran s 1, 2, 3, 4 ili 5 Rf supstituta; ili
gdje (ii) R2 je izabran od piridila, pirimidinila, pirazila, piridazila, triazila, furanila, pirolila, tiofenila, tiazolila, izotiazolila, tiadiazolila, oksazolila, izoksazolila, oksadiazolila, imidazolila, triazolila i tetrazolila, svakog opcionalno supstituiranog s 1, 2, 3 ili 4 supstituta izabranih od halogena, CN, okso, (CH2)nORa, (CH2)nOC(O)Ra, (CH2)nOC(O)ORa, (CH2)nOC(O)NRbRc, (CH2)nNRbRc, (CH2)nNRdC(O)Ra, (CH2)nNRdC(O)ORa, (CH2)nNRdC(O)NRbRc, (CH2)nNRdC(O)C(O)NRbRc, (CH2)nNRdC(S)Ra, (CH2)nNRdC(S)ORa, (CH2)nNRdC(S)NRbRc, (CH2)nNRdC(NRe)NRbRc, (CH2)nNRdS(O)Ra, (CH2)nNRdSO2Ra, (CH2)nNRdSO2NRbRc, (CH2)nC(O)Ra, (CH2)nC(O)ORa, (CH2)nC(O)NRbRc, (CH2)nC(S)Ra, (CH2)nC(S)ORa, (CH2)nC(S)NRbRc, (CH2)nC(NRe)NRbRc, (CH2)nSRa, (CH2)nS(O)Ra, (CH2)nSO2Ra, (CH2)nSO2NRbRc, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, (CH2)nC3-8 cikloalkila, (CH2)n3-8-članog heterocikloalkila, (CH2)nfenila, (CH2)nnaftila i (CH2)n5-10-članog heteroarila, gdje je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, (CH2)nC3-8 cikloalkila, (CH2)n3-8-člani heterocikloalkil, (CH2)nfenil, (CH2)nnaftil i (CH2)n5-10-člane heteroarilne grupe opcionalno supstituiran s 1, 2, 3, 4 ili 5 Rf supstituta.
16. Spoj prema zahtjevu 15, ili njegova farmaceutski prihvatljiva sol,
gdje (ii-a) R2 je izabran od piridila, pirimidinila, pirazila, piridazila, triazila, furanila, pirolila, tiofenila, tiazolila, izotiazolila, tiadiazolila, oksazolila, izoksazolila, oksadiazolila, imidazolila, triazolila i tetrazolila, svakog opcionalno supstituiranog s supstitutom izabranim između (CH2)nC(O)ORa i (CH2)nC(O)NRbRc; i opcionalno supstituiranog s 1, 2 ili 3 dodatna supstituta izabrana od halogena, CN, okso, (CH2)nORa, (CH2)nOC(O)Ra, (CH2)nOC(O)ORa, (CH2)nOC(O)NRbRc, (CH2)nNRbRc, (CH2)nNRdC(O)Ra, (CH2)nNRdC(O)ORa, (CH2)nNRdC(O)NRbRc, (CH2)nNRdC(O)C(O)NRbRc, (CH2)nNRdC(S)Ra, (CH2)nNRdC(S)ORa, (CH2)nNRdC(S)NRbRc, (CH2)nNRdC(NRe)NRbRc, (CH2)nNRdS(O)Ra, (CH2)nNRdSO2Ra, (CH2)nNRdSO2NRbRc, (CH2)nC(O)Ra, (CH2)nC(O)ORa, (CH2)nC(O)NRbRc, (CH2)nC(S)Ra, (CH2)nC(S)ORa, (CH2)nC(S)NRbRc, (CH2)nC(NRe)NRbRc, (CH2)nSRa, (CH2)nS(O)Ra, (CH2)nSO2Ra, (CH2)nSO2NRbRc, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, (CH2)nC3-8 cikloalkila, (CH2)n3-8-članog heterocikloalkila, (CH2)nfenila, (CH2)nnaftila i (CH2)n5-10-članog heteroarila, gdje je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, (CH2)nC3-8 cikloalkil, (CH2)n3-8-člani heterocikloalkil, (CH2)nfenil, (CH2)nnaftil i (CH2)n5-10-člane heteroarilne grupe opcionalno supstituiran s 1, 2, 3, 4 ili 5 Rf supstituta,
posebno, gdje je R2 izabran od furanila, pirolila, tiofenila, tiazolila, izotiazolila, tiadiazolila, oksazolila, izoksazolila, oksadiazolila, imidazolila, triazolila i tetrazolila, svakog opcionalno supstituiranog s (CH2)nC(O)NRbRc; ili gdje (ii-b) R2 je izabran od piridila, pirimidinila, pirazila, piridazila, triazila, furanila, pirolila, tiofenila, tiazolila, izotiazolila, tiadiazolila, oksazolila, izoksazolila, oksadiazolila, imidazolila, triazolila i tetrazolila, svakog opcionalno supstituiranog s (CH2)nNRdC(O)Ra, gdje Ra je C1-6 alkil ili 3-8-člani heterocikloalkil, svaki opcionalno supstituiran s 1, 2 ili 3 dodatna supstituta izabrana od halogena, CN, okso, (CH2)nORa, (CH2)nOC(O)Ra, (CH2)nOC(O)ORa (CH2)nOC(O)NRbRc, (CH2)nNRbRc, (CH2)nNRdC(O)Ra, (CH2)nNRdC(O)ORa, (CH2)nNRdC(O)NRbRc, (CH2)nNRdC(O)C(O)NRbRc, (CH2)nNRdC(S)Ra, (CH2)nNRdC(S)ORa, (CH2)nNRdC(S)NRbRc, (CH2)nNRdC(NRe)NRbRc, (CH2)nNRdS(O)Ra, (CH2)nNRdSO2Ra, (CH2)nNRdSO2NRbRc, (CH2)nC(O)Ra, (CH2)nC(O)ORa, (CH2)nC(O)NRbRc, (CH2)nC(S)Ra, (CH2)nC(S)ORa, (CH2)nC(S)NRbRc, (CH2)nC(NRe)NRbRc, (CH2)nSRa, (CH2)nS(O)Ra, (CH2)nSO2Ra, (CH2)nSO2NRbRc, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, (CH2)nC3-8 cikloalkila, (CH2)n3-8-članog heterocikloalkila, (CH2)nfenila, (CH2)nnaftila i (CH2)n5-10-članog heteroarila, gdje je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, (CH2)nC3-8 cikloalkil, (CH2)n3-8-člani heterocikloalkil, (CH2)nfenil, (CH2)nnaftil i (CH2)n5-10-člane heteroarilne grupe opcionalno supstituiran s 1, 2, 3, 4 ili 5 Rf supstituta,
posebno, gdje je R2 izabran od furanila, pirolila, tiofenila, tiazolila, izotiazolila, tiadiazolila, oksazolila, izoksazolila, oksadiazolila, imidazolila, triazolila i tetrazolila, svakog opcionalno supstituiranog s (CH2)nNRdC(O)Ra, gdje Ra je izabran od C1-6 alkila, C1-6 alkil-OH i C1-6 alkil-NH2, svakog opcionalno supstituiranog s 1, 2 ili 3 dodatna supstituta izabrana od halogena, CN, (CH2)nORa, (CH2)nOC(O)Ra, (CH2)nOC(O)ORa, (CH2)nOC(O)NRbRc, (CH2)nNRbRc, (CH2)nNRdC(O)Ra, (CH2)nNRdC(O)ORa, (CH2)nNRdC(O)NRbRc, (CH2)nNRdSO2Ra, (CH2)nNRdSO2NRbRc, (CH2)nC(O)Ra, (CH2)nC(O)ORa, (CH2)nC(O)NRbRc, (CH2)nSRa, (CH2)nS(O)Ra, (CH2)nSO2Ra, (CH2)nSO2NRbRc, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, (CH2)nC3-8 cikloalkila, (CH2)n3-8-članog heterocikloalkila, (CH2)nfenila, (CH2)nnaftila i (CH2)n5-10-članog heteroarila.
17. Spoj prema bilo kojem prethodnom zahtjevu, ili njegova farmaceutski prihvatljiva sol, gdje je R1 vodik; i/ili gdje je R3 vodik; i/ili gdje je R4 vodik.
18. Spoj prema zahtjevu 1 izabran između:
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i
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ili njegova farmaceutski prihvatljiva sol.
19. Spoj prema zahtjevu 1 izabran između
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ili njegova farmaceutski prihvatljiva sol.
20. Spoj prema zahtjevu 1, gdje je spoj formule V(b), ili njegova farmaceutski prihvatljiva sol:
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gdje jedan od Rm i Rn je vodik, a drugi je fluor;
gdje fluor i R7 su u trans konfiguraciji jedan u odnosu na drugi na ciklobutil prstenu;
gdje X je veza;
gdje R1, R3 i R4 su svaki vodik;
gdje R2 je izabran od furanila, pirolila, tiofenila, tiazolila, izotiazolila, tiadiazolila, oksazolila, izoksazolila, oksadiazolila, imidazolila, triazolila i tetrazolila, svakog opcionalno supstituiranog s (CH2)nC(O)NRbRc; gdje R7 je 2-piridil opcionalno supstituiran s 1, 2, 3, 4 ili 5 supstituta izabranih od halogena, CN, okso, ORa, OC(O)Ra, OC(O)ORa, OC(O)NRbRc, NRbRc, NRdC(O)Ra, NRdC(O)ORa, NRdC(O)NRbRc, NRdC(O)C(O)NRbRc, NRdC(S)Ra, NRdC(S)ORa, NRdC(S)NRbRc, NRdC(NRe)NRbRc, NRdS(O)Ra, NRdSO2Ra, NRdSO2NRbRc, C(O)Ra, C(O)ORa, C(O)NRbRc, C(S)Ra, C(S)ORa, C(S)NRbRc, C(NRe)NRbRc, SRa, S(O)Ra, SO2Ra, SO2NRbRc, C1-6alkila, C1-6 haloalkila, C2-6alkenila, C2-6alkinila, C3-6cikloalkila, C3-6cikloalkenila, 3-6-članog heterocikloalkila, 3-6-članog heterocikloalkenila, fenila, naftila, C7-11 aralkila, i 5-10-članog heteroarila, gdje je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C3-8 cikloalkil, C3-8 cikloalkenil, 3-8-člani heterocikloalkil, 3-8-člani heterocikloalkenil, C6-10 aril, C7-11 aralkil i 5-10-člane heteroarilne grupe opcionalno supstituiran s 1, 2, 3, 4 ili 5 Rf supstituta; i gdje R8 i R9 su svaki vodik.
21. Spoj prema zahtjevu 1, koji je
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22. Farmaceutski sastav koji sadrži spoj prema bilo kojem od zahtjeva 1 do 20, ili njegovu farmaceutski prihvatljivu sol, ili na primjer spoj prema zahtjevu 21, gdje je farmaceutski sastav formuliran za oralno, sublingvalno, potkožno, parenteralno, intravenozno, intranazalno, lokalno, transdermalno, intraperitonealno, intramuskularno, intrapulmonarno, vaginalno, rektalno, ili intraokularno davanje, posebno, kada je farmaceutski sastav formuliran za oralno davanje.
23. Farmaceutski sastav koji sadrži
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ili njegovu farmaceutski prihvatljivu sol, i farmaceutski prihvatljiv nosač ili farmaceutski prihvatljivu pomoćnu tvar, gdje su farmaceutski prihvatljiv nosač ili farmaceutski prihvatljiva pomoćna tvar izabrani iz grupe koju čine manitol, laktoza, škrob, magnezijev stearat, natrijev saharin, talk, celuloza, natrijeva koskarameloza, glukoza, želatina, saharoza i magnezijev karbonat.
24. Spoj prema bilo kojem od zahtjeva 1 do 20, ili njegova farmaceutski prihvatljiva sol, ili spoj prema zahtjevu 21 za upotrebu u postupku liječenja bolesti ili stanja izabranih od neuromuskularnih bolesti, stanja trošenja mišića, muskularnih miopatija, deficita u vezi s rehabilitacijom, periferne vaskularne bolesti, periferne arterijske bolesti, slabosti, mišićne atrofije i umora, metaboličkog sindroma, sindroma kroničnog umora i pretilosti, ili za upotrebu u postupku liječenja bolesti ili stanja izabranih između bolesti kronične opstrukcije pluća i otkazivanja srca, ili za upotrebu u postupku liječenja bolesti izabrane između amiotrofične lateralne skleroze (ALS), spinalne mišićne atrofije (SMA) i mijastenije gravis ili za upotrebu u postupku liječenja bolesti izabrane između periferne vaskularne bolesti i periferne arterijske bolesti.
25. Spoj za upotrebu prema zahtjevu 24, gdje je bolest ili stanje amiotrofična lateralna skleroza (ALS).
26. Spoj za upotrebu prema zahtjevu 24, gdje je bolest ili stanje spinalna mišića atrofija (SMA).
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