HRP20110917T1 - Derivati azabicikličkih alkana supstituirani fuzioniranim bicikloheterociklima aktivni u središnjem živčanom sustavu - Google Patents
Derivati azabicikličkih alkana supstituirani fuzioniranim bicikloheterociklima aktivni u središnjem živčanom sustavu Download PDFInfo
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- HRP20110917T1 HRP20110917T1 HR20110917T HRP20110917T HRP20110917T1 HR P20110917 T1 HRP20110917 T1 HR P20110917T1 HR 20110917 T HR20110917 T HR 20110917T HR P20110917 T HRP20110917 T HR P20110917T HR P20110917 T1 HRP20110917 T1 HR P20110917T1
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- 150000001335 aliphatic alkanes Chemical class 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 claims abstract 15
- 229910052739 hydrogen Inorganic materials 0.000 claims 11
- 239000001257 hydrogen Substances 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 229940079593 drug Drugs 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 150000002431 hydrogen Chemical group 0.000 claims 5
- 208000024827 Alzheimer disease Diseases 0.000 claims 4
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 4
- 208000010877 cognitive disease Diseases 0.000 claims 4
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims 3
- 102000019315 Nicotinic acetylcholine receptors Human genes 0.000 claims 3
- 108050006807 Nicotinic acetylcholine receptors Proteins 0.000 claims 3
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 3
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- JYGFTBXVXVMTGB-UHFFFAOYSA-N Oxindol Natural products C1=CC=C2NC(=O)CC2=C1 JYGFTBXVXVMTGB-UHFFFAOYSA-N 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 206010040070 Septic Shock Diseases 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000005083 alkoxyalkoxy group Chemical group 0.000 claims 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 2
- 125000000676 alkoxyimino group Chemical group 0.000 claims 2
- 125000005138 alkoxysulfonyl group Chemical group 0.000 claims 2
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- -1 amino, carboxy Chemical group 0.000 claims 2
- 230000015624 blood vessel development Effects 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 208000026278 immune system disease Diseases 0.000 claims 2
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 201000000980 schizophrenia Diseases 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 206010065040 AIDS dementia complex Diseases 0.000 claims 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 206010067889 Dementia with Lewy bodies Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010065390 Inflammatory pain Diseases 0.000 claims 1
- 201000002832 Lewy body dementia Diseases 0.000 claims 1
- 208000000609 Pick Disease of the Brain Diseases 0.000 claims 1
- 208000004550 Postoperative Pain Diseases 0.000 claims 1
- 206010039966 Senile dementia Diseases 0.000 claims 1
- 206010044248 Toxic shock syndrome Diseases 0.000 claims 1
- 231100000650 Toxic shock syndrome Toxicity 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000004423 acyloxy group Chemical group 0.000 claims 1
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 239000003693 atypical antipsychotic agent Substances 0.000 claims 1
- 229940127236 atypical antipsychotics Drugs 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 230000007278 cognition impairment Effects 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 1
- 230000003247 decreasing effect Effects 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 150000002367 halogens Chemical group 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 208000000509 infertility Diseases 0.000 claims 1
- 230000036512 infertility Effects 0.000 claims 1
- 231100000535 infertility Toxicity 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 208000027061 mild cognitive impairment Diseases 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 125000002206 pyridazin-3-yl group Chemical group [H]C1=C([H])C([H])=C(*)N=N1 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 230000036303 septic shock Effects 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 230000009529 traumatic brain injury Effects 0.000 claims 1
- 230000029663 wound healing Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 abstract 2
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- C07D451/06—Oxygen atoms
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- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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Abstract
Spoj formule (I), ili njegova farmaceutski prihvatljiva sol, naznačen time, dan je 1, 2 ili 3; A je N ili N+-O-;R je vodik, alkil, cikloaIkilaIkil i arilalkil; L je odabran iz skupine koju čine O, S i -N(Ra)-;Ar1 je 6-eročlani aril ili 6-eročlani heteroarilni prsten; Ar2 je fuzionirani deveteročlani biciklički heteroaril; aRa je odabran iz skupine koju čine vodik, alkil i alkilkarbonil; pod uvjetom da kada je Ar1tada L je O ili S. Patent sadrži još 13 patentnih zahtjeva.
Claims (14)
1. Spoj formule (I),
[image]
ili njegova farmaceutski prihvatljiva sol, naznačen time, da
n je 1, 2 ili 3;
A je N ili N+-O-;
R je vodik, alkil, cikloaIkilaIkil i arilalkil;
L je odabran iz skupine koju čine O, S i -N(Ra)-;
Ar1 je 6-eročlani aril ili 6-eročlani heteroarilni prsten;
Ar2je fuzionirani deveteročlani biciklički heteroaril; a
Raje odabran iz skupine koju čine vodik, alkil i alkilkarbonil; pod uvjetom da kada je Ar1
[image]
tada L je O ili S.
2. Spoj iz patentnog zahtjeva 1, naznačen time, da je Ar1 odabran iz skupine koju čine:
[image]
[image]
[image]
[image]
[image]
pri čemu su R1, R2, R3, R4 i R5 neovisno jedan o drugom odabrani iz skupine koju čine acil, aciloksi, alkenil, alkoksi, alkoksialkoksi, alkoksialkil, alkoksikarbonil, alkoksiimino, alkoksisulfonil, alkil, alkilsulfonil, alkinil, amino, karboksi, cijano, formil, haloalkoksi, haloalkil, halo, hidroksi, hidroksialkil, merkapto, nitro, tioalkoksi, NRgRj, (NRgRj)alkil, (NRgRj)alkoksi, (NRgRj) karbonil i (NRgRj)sulfonil;
Rg i Rj su neovisno jedan o drugom odabrani iz skupine koju čine vodik i alkil.
3. Spoj iz patentnog zahtjeva 1, naznačen time, da je Ar2 odabran iz skupine koju čine
[image]
[image]
[image]
[image]
pri čemu su Z1, Z2, Z3 i Z4 neovisno jedan o drugom dušik ili ugljik, pri čemu je atom ugljika po izboru supstituiran supstituentom koji je odabran iz skupine koju čine vodik, halogen, alkil, -ORC, -alkil- ORC, -NRdRe, i -alkil-NRdRe;
Rb je odabran iz skupine koju čine vodik, alkil i alkilkarbonil;
Rc je alkil;
Rd i Re su neovisno jedan o drugom odabrani iz skupine koju čine vodik i alkil,
R6 i R7 su neovisno jedan o drugom odabrani iz skupine koju čine vodik, alkenil, alkoksi, alkoksialkoksi, alkoksialkil, alkoksikarbonil, alkoksiimino, alkoksisulfonil, alkil, alkilkarbonil, alkilkarboniloksi, alkilsulfonil, alkinil, karboksi, cijano, formil, haloalkoksi, haloalkil, halo, vodik, hidroksi, hidroksialkil, merkapto, nitro, tioalkoksi, -NRgRj, (NRgRj)alkil, (NRgRj)alkoksi, (NRgRj)karbonil i (NRgRj)sulfonil;
Rg i Rj su neovisno jedan o drugom odabrani iz skupine koju čine vodik i alkil.
4. Spoj iz patentnog zahtjeva 2, naznačen time, da
A je N;
R je metil ili vodik;
L je 0;
n je 2; a
Ar2 je odabran iz skupine koju čine:
[image]
5. Spoj iz patentnog zahtjeva 2, naznačen time, da A je N; R je metil ili vodik; L je O, n je 2; Ar1 je
[image]
6. Spoj iz patentnog zahtjeva 2, naznačen time, da A je N; R je metil ili vodik; L je O; n je 2; Ar1 je
[image]
a Ar2 je
[image]
7. Spoj iz patentnog zahtjeva 1, naznačen time, da je odabran iz skupine koju čine:
5-{6-[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-piridazin-3-il}-1H-indol;
(endo)-3-(6-benzo[b]tiofen-5-il-piridazin-3-iloksi)-8-metil-8-aza biciklo[3.2.1]oktan;
(endo)-3-[6-(benzofuran-5-il)-piridazin-3-iloksi]-8-metil-8-aza-biciklo[3.2.1]oktan;
6-{6-[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-piridazin-3-il}-1H-indol;
5-{6-[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-piridazin-3-il}-1H-indazol;
1-metil-5-{6-[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-piridazin-3-il}-1H-indol;
5-{6-[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-piridazin-3-il}-2-trifluorometil-1H-indol;
5-{6-[(egzo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-piridazin-3-il}-1H-indol;
5-{5[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-piridin-2-il}-1H-indol;
(endo)-3-(6-benzo[b]tiofen-5-il-piridin-3-iloksi)-8-metil-8-aza-biciklo[3.2.1]oktan;
5-{5-[(egzo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-piridin-2-il}-1H-indol;
(egzo)-3-[6-(benzofuran-5-il)-piridin-3-iloksi]-8-metil-8-aza-biciklo[3.2.1]oktan;
5-{5-[(egzo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-piridin-2-il}-1H-indazol;
5-{5-[(egzo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-piridin-2-il}-2-trifluorometil-1H-indol;
4-{5-[(egzo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-piridin-2-il)-1H-indol;
5-{6-[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-piridin-3-il}-1H-indol;
(endo)-3-(5-benzo[b]tiofen-5-il-piridin-2-iloksi)-8-metil-8-aza-biciklo[3.2.1]oktan;
5-{6-[(egzo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-piridin-3-il}-1H-indol;
[6-(1H-indol-5-il)-piridin-3-il]-[(endo)-8-metil-8-aza-bicilo[3.2.1]okt-3-il]-amin;
[6-(benzofuran-5-il)-piridin-3-il]-[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-il]-amin;
[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-il]-[6-(2-trifluorometil-1H-indol-5-il)-piridin-3-il]-amin;
[6-(1H-indazol-5-il)-piridin-3-il]-[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-il]-amin;
[6-(1H-indol-4-il)-piridin-3-il)-[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-il]-amin;
[(endo)-8-aza-biciklo[3.2.1]okt-3-il]-[6-(1H-indol-5-il)-piridin-3-il]-amin;
[4-(1H-indol-5-il)-fenil]-[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-il]-amin;
[4-(1H-indazol-5-il)-fenil]-[(endo)-8-metil-8-aza-bicilo[3.2.1]okt-3-il]-amin;
[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-il]-[4-(1-metil-1H-indol-5-il)-fenil]-amin;
(4-benzo[b]tiofen-5-il-fenil)-[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-il]-amin;
[4-(benzofuran-5-il)-fenil]-[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-il]-amin;
[4-(1H-indol-4-il)-fenil]-[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-il]-amin;
[3-(1H-indol-5-il)-fenil]-[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-il]-amin;
[3-(1H-indol-4-il)-fenil]-[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-il]-amin;
5-{6-[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-piridazin-3-il}-2-trifluorometil-1H-indol;
4-{6-[(egzo)-8-metil-8-aza-bicilo[3.2.1]okt-3-iloksi]-piridazin-3-il}-1H-indol;
5-{6-[(egzo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-piridin-3-il}-1H-indol;
5-{6-[(egzo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-piridin-3-il}-2-trifluorometil-1H-indol;
4-{6-[(egzo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-piridazin-3-il}-1H-indol;
6-{5-[(egzo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-piridin-2-il}-1H-indol;
5-{5-[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-pirazin-2-il]-1H-indol;
4-{5-[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-pirazin-2-il]-1H-indol;
6-{5-[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-pirazin-2-il]-1H-indol;
[6-(1H-indol-6-il)-piridin-3-il]-[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-il]-amin;
5-{6-[(endo)-9-metil-9-azabiciklo[3.3.1]nonan-3-iloksi]piridazin-3-il}-1H-indol;
(endo)-3-[6-(benzo[b]tiofen-5-il)piridazin-3-iloksi]-9-metil-9-azabiciklo[3.3.1]nonan;
5-{5-[(endo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-pirazin-2-il}-1H-pirolo[2,3-b]piridin;
5-{5-[(egzo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-piridin-2-il}-1H-pirolo[2,3-b]piridin;
5-{5-[(egzo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-piridin-3-il}-1H-indol;
5-{5-[(egzo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-pirazin-2-il}-1H-indol;
4-{5-[(egzo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-pirazin-2-il}-1H-indol;
6-{5-[(egzo)-8-metil-8-aza-biciklo[3.2.1]okt-3-iloksi]-pirazin-2-il}-1H-indol.
(endo)-N-(5-(1H-Indol-5-il)piridin-3-il)-8-metil-8-azabiciklo[3.2.1]oktan-3-amin;
(endo)-N-(5-(1H-Indol-4-il)piridin-3-il)-8-metil-8-azabiciklo[3.2.1]oktan-3-amin;
(endo)-N-(5-(1H-Indol-6-il)piridin-3-il)-8-metil-8-azabiciklo[3.2.1]oktan-3-amin;
(endo)-N-{5-[2-(trifluorometil)-1H-indol-5-il]piridin-3-il}-8-Metil-8-azabiciklo[3.2.1]oktan-3-amin;
5-{5-[(endo)-8-Metil-8-azabiciklo[3.2.1]oktan-3-iloksi]piridin-2-il}-1H-pirolo[2,3-b]piridin;
5-{5-[(endo)-8-Metil-8-azabiciklo[3.2.1]oktan-3-iloksi]piridin-2-il}indolin-2-on;
5-{5-[(endo)-8-Azabiciklo[3.2.1]oktan-3-iloksi]piridin-2-il}-1H-indol;
(1R,3r,5S,8s)-3-(6-(1H-Indol-5-il)piridin-3-iloksi)-8-metil-8-azabiciklo[3.2.1]oktan 8-oksid;
(1R,3r,5S,8r)-3-(6-(1H-Indol-5-il)piridin-3-iloksi)-8-metil-8-azabiciklo[3.2.1]oktan 8-oksid;
4-{5-[(endo)-8-Azabiciklo[3.2.1]oktan-3-iloksi]piridin-2-il}-1H-indol;
5-{5-[(egzo)-8-Azabiciklo[3.2.1]oktan-3-iloksi]piridin-2-il}-1H-indol;
5-{5-[(endo)-8-Azabiciklo[3.2.1]oktan-3-iloksi]piridin-2-il}indolin-2-on;
5-{5-[(endo)-8-Azabiciklo[3.2.1]oktan-3-iloksi]piridin-2-il}-1H-pirolo[2,3-b]piridin;
5-{5-[(egzo)-8-Azabiciklo[3.2.1]oktan-3-iloksi]piridin-2-il}-1H-pirolo[2,3-b]piridin.
8. Farmaceutski pripravak koji sadrži terapijski učinkovitu količinu spoja iz patentnog zahtjeva 1, naznačen time, da je spravljen u kombinaciji s farmaceutski prihvatljivom pomoćnom tvari.
9. Uporaba terapijski učinkovite količine spoja iz bilo kojeg patentnog zahtjeva 1 do 7 ili njegove farmaceutski prihvatljive soli, naznačena time, da se koristi za proizvodnju lijeka za selektivnu modulaciju učinaka a nikotinskih acetilkolinskih receptora, a4p2 nikotinskih acetilkolinskih receptora ili a i a4p2 nikotinskih acetilkolinskih receptora zajedno.
10. Uporaba terapijski učinkovite količine spoja iz bilo kojeg patentnog zahtjeva 1 do 7 ili njegove farmaceutski prihvatljive soli, naznačena time, da se koristi za proizvodnju lijeka za liječenje ili sprječavanje stanja ili poremećaja odabranih iz skupine koju čine: poremećaj pažnje, poremećaj pažnje i hiperaktivnost (ADHD), Alzheimerova bolest (AD), lagani kognitivni poremećaj, senilna demencija, demencija izazvana AIDS-om, Pickova bolest, demencija s Lewyjevim tjelešcima, demencija povezana s Downovim sindromom, amiotrofna lateralna skleroza, Huntingtonova bolest, smanjena funkcija CNS-a povezana s traumatskom ozljedom mozga, akutna bol, postkirurška bol, kronična bol, upale, upalna bol, neuropatska bola, neplodnost, potreba za razvojem nove krvne žile povezana s cijeljenjem rane, potreba za razvojem nove krvne žile povezana s vaskularizacijom kožnih presadaka i nedostatkom cirkulacije, reumatoidni artritis, Crohnova bolest, ulcerativni colitis, upalna bolest crijeva, odbacivanje presađenog organa, akutna imuna bolest povezana s presađivanjem organa, kronična imuna bolest povezana s presađivanjem organa, septički šok, sindrom toksičkog šoka, septički sindrom, depresija i reumatoidni spondilitis.
11. Uporaba spoja iz bilo kojeg patentnog zahtjeva 1 do 7 ili njegove farmaceutski prihvatljiva soli, naznačena time, da se koristi za proizvodnju lijeka za liječenje ili sprječavanje stanja ili poremećaja odabranih iz skupine koju čine: kognitivni poremećaj, neurodegeneracija, schizophrenia i kognitivni deficit povezan sa schizophrenijom.
12. Uporaba u skladu s patentnim zahtjevom 9, 10 ili 11, naznačena time, da uključuje uporabu spoja iz bilo kojeg patentnog zahtjeva 1 do 7 ili njegove farmaceutski prihvatljive soli u kombinaciji s atipičnim antipsihotikom.
13. Uporaba u skladu s patentnim zahtjevom 9, 10 ili 11, naznačena time, da uključuje uporabu spoja iz bilo kojeg patentnog zahtjeva 1 do 7 ili njegove farmaceutski prihvatljive soli u kombinaciji s medikacijom koja se koristi za liječenje poremećaja pažnje i hiperaktivnosti i ostalih kognitivnih poremećaja.
14. Uporaba u skladu s patentnim zahtjevom 13, naznačena time, da je medikacija koja se koristi za liječenje ostalih kognitivnih poremećaja medikacija koja se koristi za liječenje Alzheimerove bolesti.
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