HRP20160382T1 - Pirolopirazin-spirociklični piperidin amidi kao modulatori ionskih kanala - Google Patents
Pirolopirazin-spirociklični piperidin amidi kao modulatori ionskih kanala Download PDFInfo
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- HRP20160382T1 HRP20160382T1 HRP20160382TT HRP20160382T HRP20160382T1 HR P20160382 T1 HRP20160382 T1 HR P20160382T1 HR P20160382T T HRP20160382T T HR P20160382TT HR P20160382 T HRP20160382 T HR P20160382T HR P20160382 T1 HRP20160382 T1 HR P20160382T1
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- -1 piperidine amides Chemical class 0.000 title claims 19
- 102000004310 Ion Channels Human genes 0.000 title 1
- NQRYJNQNLNOLGT-UHFFFAOYSA-N tetrahydropyridine hydrochloride Natural products C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 title 1
- 125000004122 cyclic group Chemical group 0.000 claims 36
- 150000001875 compounds Chemical class 0.000 claims 29
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 24
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 19
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 17
- 125000005843 halogen group Chemical group 0.000 claims 15
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 15
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 11
- 101001032455 Dianthus caryophyllus Glutathione S-transferase 1 Proteins 0.000 claims 10
- 101100533877 Hypocrea jecorina (strain QM6a) sor8 gene Proteins 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 10
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 10
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 10
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 10
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 8
- 101100134927 Gallus gallus COR8 gene Proteins 0.000 claims 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 6
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 6
- 208000002193 Pain Diseases 0.000 claims 6
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 claims 6
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 5
- 125000006345 2,2,2-trifluoroethoxymethyl group Chemical group [H]C([H])(*)OC([H])([H])C(F)(F)F 0.000 claims 4
- JNCMHMUGTWEVOZ-UHFFFAOYSA-N F[CH]F Chemical compound F[CH]F JNCMHMUGTWEVOZ-UHFFFAOYSA-N 0.000 claims 4
- 108010081348 HRT1 protein Hairy Proteins 0.000 claims 4
- 102100021881 Hairy/enhancer-of-split related with YRPW motif protein 1 Human genes 0.000 claims 4
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 4
- 208000004296 neuralgia Diseases 0.000 claims 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 2
- 125000004793 2,2,2-trifluoroethoxy group Chemical group FC(CO*)(F)F 0.000 claims 2
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 2
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 2
- 208000019695 Migraine disease Diseases 0.000 claims 2
- 108010052164 Sodium Channels Proteins 0.000 claims 2
- 102000018674 Sodium Channels Human genes 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 2
- 239000012472 biological sample Substances 0.000 claims 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 230000001419 dependent effect Effects 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 2
- 206010027599 migraine Diseases 0.000 claims 2
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 125000006340 pentafluoro ethyl group Chemical group FC(F)(F)C(F)(F)* 0.000 claims 2
- 125000003107 substituted aryl group Chemical group 0.000 claims 2
- 125000004213 tert-butoxy group Chemical group [H]C([H])([H])C(O*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 125000001973 tert-pentyl group Chemical group [H]C([H])([H])C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 125000002827 triflate group Chemical group FC(S(=O)(=O)O*)(F)F 0.000 claims 2
- 125000001889 triflyl group Chemical group FC(F)(F)S(*)(=O)=O 0.000 claims 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- 206010002383 Angina Pectoris Diseases 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 206010003591 Ataxia Diseases 0.000 claims 1
- 208000008035 Back Pain Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 201000006474 Brain Ischemia Diseases 0.000 claims 1
- 206010058019 Cancer Pain Diseases 0.000 claims 1
- 206010008120 Cerebral ischaemia Diseases 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 208000006561 Cluster Headache Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 206010019233 Headaches Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010021639 Incontinence Diseases 0.000 claims 1
- 206010065390 Inflammatory pain Diseases 0.000 claims 1
- 208000016285 Movement disease Diseases 0.000 claims 1
- 206010061533 Myotonia Diseases 0.000 claims 1
- 206010028836 Neck pain Diseases 0.000 claims 1
- 208000001294 Nociceptive Pain Diseases 0.000 claims 1
- 206010033557 Palpitations Diseases 0.000 claims 1
- 206010036376 Postherpetic Neuralgia Diseases 0.000 claims 1
- 208000004550 Postoperative Pain Diseases 0.000 claims 1
- 206010059604 Radicular pain Diseases 0.000 claims 1
- 208000008765 Sciatica Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 206010003119 arrhythmia Diseases 0.000 claims 1
- 230000006793 arrhythmia Effects 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 206010008118 cerebral infarction Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 230000001037 epileptic effect Effects 0.000 claims 1
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 208000015706 neuroendocrine disease Diseases 0.000 claims 1
- 230000002981 neuropathic effect Effects 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 230000003349 osteoarthritic effect Effects 0.000 claims 1
- 230000002085 persistent effect Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 238000011946 reduction process Methods 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 230000009529 traumatic brain injury Effects 0.000 claims 1
- 206010044652 trigeminal neuralgia Diseases 0.000 claims 1
- 208000009935 visceral pain Diseases 0.000 claims 1
- 239000013585 weight reducing agent Substances 0.000 claims 1
Classifications
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Claims (25)
1. Spoj formule I:
[image]
ili njegova farmaceutski prihvatljiva sol,
u kojem, nezavisno od svakog slučaja:
R1 je H, C1-C8 alkil, C3-C8 cikloalkil, halo, CN, NR8SO2R8, SO2R8, SR8, SOR8, NR8COR8, NR8CO2R8, CON(R8)2, SO2N(R8)2, CF3, heterocikloalkil ili linearni, razgranati ili ciklični (C1-C8)-R9 gdje do dvije CH2 jedinice mogu biti zamijenjene sa O, CO, S, SO, SO2 ili NR8, ili dva R1 uzeta zajedno formiraju okso grupu, ili 3 do 7-člani fuzionirani cikloalkil prsten, ili 3 do 7-člani spirocikličan prsten;
R2 je H, C1-C8 alkil, halo, C1-C8 haloalkil, CN, OH, SO2R8, SR8, SOR8, COR8, CO2R8, CON(R8)2, SO2N(R8)2, CF3, CHF2 ili linearni, razgranati ili ciklični (C1-C8)-R9 gdje do dvije CH2 jedinice mogu biti zamijenjene sa O, CO, S, SO, SO2, CF2 ili NR8;
R3 je H, C1-C8 alkil, C3-C8 cikloalkil, CO2R8, COR8, COH, CON(R8)2, CF3, CH2CF3, CH2CHF2 ili linearni, razgranati ili ciklični (C1-C8)-R9 gdje do dvije CHF2 jedinice mogu biti zamijenjene sa O, CO, S, SO, SO2 ili NR8;
R4 je H, C1-C8 alkil, halo, C3-C8 cikloalkil, gdje do dvije CH2 jedinice mogu biti zamijenjene sa O, CO, S, SO, SO2 ili NR8, ili 2 R4 uzeti zajedno formiraju fuzionirani 3 do 7-člani cikloalkil prsten;
R8 je H, C1-C8 alkil, CF3, C3-C8 cikloalkil, fluoroalkil, aril, heteroaril ili linearni, razgranati ili ciklični (C1-C8)-R9 gdje do dvije CH2 jedinice mogu biti zamijenjene sa O, CO, S, SO, SO2 ili NR, ili 2 R8 uzeta zajedno sa atomima za koje su vezani formiraju prsten;
R9 je H, CF3, CO2R, OH, aril, heteroaril, C3-C8 cikloalkil, heterocikloalkil, N(R)2, NRCOR, CON(R)2, CN, halo ili SO2R;
R je H, C1-C8 alkil, aril, heteroaril, C3-C8 cikloalkil ili heterocikloalkil;
A je izborno supstituiran aril, heteroaril ili heterociklik;
m je cijeli broj od 0 do 4 uključujući 0 i 4;
n je cijeli broj od 0 do 3 uključujući 0 i 3; i
o je cijeli broj od 0 do 4 uključujući 0 i 4.
2. Spoj prema patentnom zahtjevu 1, naznačen time što nezavisno od svakog slučaja:
R1 je H, C1-C6 alkil, C3-C8 cikloalkil, halo, CN, NR8SO2R8, SO2R8, SR8, SOR8, NR8COR8, NR8CO2R8, CON(R8)2, SO2N(R8)2, CF3, heterocikloalkil ili linearni, razgranati ili ciklični (C1-C8)-R9 gdje do dvije CH2 jedinice mogu biti zamijenjene sa O, CO, S, SO, SO2 ili NR8, ili dva R1 uzeta zajedno formiraju okso grupu, ili 3 do 7-člani fuzionirani cikloalkil prsten, ili 3 do 7-člani spirociklični prsten;
R2 je H, C1-C6 alkil, C1-C6 haloalkil, CN, OH, SO2R8, SR8, SOR8, CO2R8, CON(R8)2, SO2N(R8)2, CF3, CHF2, ili linearni, razgranati ili ciklični (C1-C8)-R9 gdje do dvije CH2 jedinice mogu biti zamijenjene sa O, CO, S, SO, SO2, CF2 ili NR8;
R3 je H, C1-C6 alkil, C3-C8 cikloalkil, CO2R8, COR8, COH, CON(R8)2, CF3, CH2CF3, CH2CHF2 ili linearni, razgranati ili ciklični (C1-C8)-R9 gdje do dvije CH2 jedinice mogu biti zamijenjene sa O, CO, S, SO, SO2 ili NR8;
R4 je H, C1-C6 alkil, halo, C3-C8 cikloalkil, gdje do dvije CH2 jedinice mogu biti zamijenjene sa O, CO, S, SO, SO2 ili NR8, ili 2 R4 uzeti zajedno formiraju fuzionirani 3 do 7-člani cikloalkil prsten;
R8 je H, C1-C6 alkil, CF3, C3-C8 cikloalkil ili linearni, razgranati ili ciklični (C1-C8)-R9 gdje do dvije CH2 jedinice mogu biti zamijenjene sa O, CO, S, SO, SO2 ili NR, ili 2 R8 uzeta zajedno sa atomima za koje su vezani formiraju prsten;
R9 je H, CF3, CO2R, OH, aril, heteroaril, C3-C8 cikloalkil, heterocikloalkil, N(R)2, NRCOR, CON(R)2, CN ili SO2R;
R je H, C1-C6 alkil, aril, heteroaril, C3-C8 cikloalkil ili heterocikloalkil;
A je izborno supstituiran aril, heteroaril ili heterociklik;
m je cijeli broj od 0 do 4 uključujući 0 i 4;
n je cijeli broj od 0 do 3 uključujući 0 i 3; i
o je cijeli broj od 0 do 4 uključujući 0 i 4.
3. Spoj prema patentnom zahtjevu 1, naznačen time što R2 je H, C1-C8 alkil, halo, CF3, CN, COR8, CON(R8)2, ili linearni, razgranati ili ciklični (C1-C8)-R9 gdje do dvije CH2 jedinice mogu biti zamijenjene sa O, CO, S, SO, SO2, CF2 ili NR8.
4. Spoj prema patentnom zahtjevu 1, naznačen time što R2 je COCF3, COtBu, Cl, COCH3, CF2CF3, CH2CF3, CF3, CN, Br, COCH(CH3)2, COCH2CH3, CH(OH)CF3, SO2CH3,
[image]
COPh,
[image]
ili
[image]
5. Spoj prema patentnom zahtjevu 1, naznačen time što R3 je H, C1-C8 alkil, CO2R8, COR8, COH, CON(R8)2 ili linearni, razgranati ili ciklični (C1-C8)-R9 gdje do dvije CH2 jedinice mogu biti zamijenjene sa O, CO, S, SO, SO2 ili NR8.
6. Spoj prema patentnom zahtjevu 1, naznačen time što R3 je H, CH3, CH2CH3, CH2CH2OCH3, CH2CH2OH, CH2CO2CH2CH3, CH2CON(CH3)2, CH2CONH2, CH2CN, benzil, ciklobutil, CH2CH(CH2)2, CH(CH2)2, CH2CF3, CH2CHF2, COCH3, COCH2CH3, CO2CH3, CO2CH2CH3, COH, CONH(CH3)2 ili CONHCH3.
7. Spoj prema patentnom zahtjevu 1, naznačen time što A je
[image]
u kojem:
R5 je H, C1-C8 alkil, C3-C8 cikloalkil, C1-C8 alkoksi, halo, CN, OH, OR8, N(R8)2, NR8SO2R8, SO2R8, SOR8, SR8, CO2R8, NR8COR8, NR8CO2R8, CON(R8)2, SO2N(R8)2, CHF2, CF3, OCF3, OCHF2, R9, heterocikloalkil, heterocikloalkoksi, aril, heteroaril ili linearni, razgranati ili ciklični (C1-C8)-R9 gdje do tri CH2 jedinice mogu biti zamijenjene sa O, CO, S, SO, SO2 ili NR8;
R6 je H, C1-C8 alkil, C3-C8 cikloalkil, C1-C8 alkoksi, C3-C8 cikloalkoksi, halo, CN, OH, OR8, N(R8)2, NR8SO2R8, SO2R8, SOR8, SR8, CO2R8, NR8COR8, NR8CO2R8, CON(R8)2, SO2N(R8)2, CF3, OCF3, OCHF2, R9, heterocikloalkil, heterocikloalkoksi, aril, heteroaril ili linearni, razgranati ili ciklični (C1-C8)-R9 gdje do tri CH2 jedinice mogu biti zamijenjene sa O, CO, S, SO, SO2 ili NR8;
R7 je H, C1-C8 alkil, C3-C8 cikloalkil, C1-C8 alkoksi, halo, CN, OH, OR8, N(R8)2, NR8SO2R8, SO2R8, OSO2R8, SOR8, SR8, CO2R8, NR8COR8,NR8CO2R8, CON(R8)2, SO2N(R8)2, CF3, OCF3, OCHF2, R9, heterocikloalkil, heterocikloalkoksi, aril, heteroaril ili linearni, razgranati ili ciklični (C1-C8)-(R9)p, gdje p je 1 ili 2 i gdje do tri CH2 jedinice mogu biti zamijenjene sa O, CO, S, SO, SO2 ili NR8; ili
dva slučaja R5 i R6, ili R6 i R7 su oba C1-C8 alkil i zajedno sa ugljicima za koje su vezani formiraju izborno supstituirani prsten koji sadrži do 2 heteroatoma.
8. Spoj prema patentnom zahtjevu 7, naznačen time što R5 je H, C1-C8 alkil, C1-C8 alkoksi, halo, OCF3, OCHF2, R9, ili linearni, razgranati ili ciklični (C1-C8)-R9 gdje do tri CH2 jedinice mogu biti zamijenjene sa O, CO, S, SO, SO2 ili NR7.
9. Spoj prema patentnom zahtjevu 7, naznačen time što R5 je H, CH3, OCH3, OCF3, OPh, Ph, OCHF2 ili F.
10. Spoj prema patentnom zahtjevu 7, naznačen time što R6 je H, C1-C8 alkil, C1-C8 alkoksi, halo, R9, ili linearni, razgranati ili ciklični (C1-C8)-R9 gdje do tri CH2 jedinice mogu biti zamijenjene sa O, CO, S, SO, SO2 ili NR8.
11. Spoj prema patentnom zahtjevu 7, naznačen time što R6 je H, CH3, OCH3, OCH2CH3, OCH2CH2CH3, OCH(CH3)2, CF3, CN, Ph, SO2CH3, OH, CH(CH3)2, OCH2CH2CH2CH3, F, Cl ili CH2OH.
12. Spoj prema patentnom zahtjevu 7, naznačen time što R7 je H, C1-C8 alkil, C1-C8 alkoksi, SO2R8, OSO2R8, SO2N(R8)2, R9, OCHF2, OCF3 ili linearni, razgranati ili ciklični (C1-C8)-(R9)p, gdje p je 1 ili 2 i gdje do tri CH2 jedinice mogu biti zamijenjene sa O, CO, S, SO, SO2 ili NR8.
13. Spoj prema patentnom zahtjevu 7, naznačen time što R7 je H, CH3, CH2CH3, tBu, Cl, F, OH, C(=CH2)CH3, OC(=CH2)CH3, OCH3, OCH2CH2CH2CH3, CH2OH, OCH2CH2OH, OCH2CH2CH2OH, OtBu, OCH(CH3)(CH2CH3), OCH2C(CH3)2OH, C(CH3)2OH, CH2C(CH3)2OH, CH(OH)CH(CH3)2, C(CH3)2CH2OH, OCH2CH2CH(CH3)2, OCH2CH2CH3, OCH(CH3)2, OCH2CH2OCH3,
[image]
SO2CH3, SO2tBu, SO2CH2CH3, SO2CH2CH(CH3)2, SO2CH(CH3)2,
[image]
, SO2NH(CH3), SO2NH(CH(CH2)2), SO2NH(CH2CH3), SO2NH(CH(CH3)2), SO2N(CH3)2,
[image]
, OPh, Ph,
[image]
, OCH2CH2OCH3, CH(CH3)2, SO2N(CH2CH3)2, CH2CH2CH2CH3, CH2CH2CH3, OCH2CH2CH2CH3, CH2OPh,
[image]
, OCH2Ph, CH2CH2CH2CH2CH3, OCH2CH3, OCH2CH(CH3)2, CH2CH3, CH2Ph,
[image]
, CCCH2OCH3, SO2CHF2, OCF3,
[image]
, OCHF2,
[image]
, CH2CH(CH3)2, OCH2tBu,
[image]
, OCH2CF3,
[image]
,
[image]
, CH2OCH2CH2CF3, CH2OCH2CF3, SO2CF3, C(CH3)2CH2CH3, C(CH2CH3)3, CH(OCH2CF3)2,
[image]
, CF3, OCH2C(CH3)2F,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
, CH(OH)CH2OCH2CF3, CH(OCH2CF3)CH2OH, OSO2CF3,
[image]
ili OCH2CH2OCF3.
14. Spoj prema patentnom zahtjevu 7, naznačen time što
[image]
je:
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
ili
[image]
15. Spoj prema patentnom zahtjevu 1, naznačen time što spoj ima formulu IA:
[image]
u kojem:
R2 je C1-C8 alkil, halo, C1-C8 haloalkil, CN, OH, SO2R8, SR8, SOR8, COR8, CO2R8, CON(R8)2, SO2N(R8)2, CF3, CHF2 ili linearni, razgranati ili ciklični (C1-C8)-R9 gdje do dvije CH2 jedinice mogu biti zamijenjene sa O, CO, S, SO, SO2 CF2 ili NR8;
R3 je H, C1-C8 alkil, CO2R8, COR8, COH, CON(R8)2, CF3 ili linearni, razgranati ili ciklični (C1-C8)-R9 gdje do dvije CH2 jedinice mogu biti zamijenjene sa CF2, O, CO, S, SO, SO2 ili NR8;
R6 je H, C1-C8 alkil, C3-C8 cikloalkil, C1-C8 alkoksi, C3-C8 cikloalkoksi, halo, CN, OH, OR8, N(R8)2, NR8SO2R8, SO2R8, SOR8, SR8, CO2R8, NR8COR8, NR8CO2R8, CON(R8)2, SO2N(R8)2, CF3, OCF3, OCHF2,
R9, heterocikloalkil, heterocikloalkoksi, aril, heteroaril ili linearni, razgranati ili ciklični (C1-C8)-R9 gdje do tri CH2 jedinice mogu biti zamijenjene sa O, CO, S, SO, SO2 ili NR8;
R7 je H, C1-C8 alkil, C3-C8 cikloalkil, C1-C8 alkoksi, halo, CN, OH, OR8, N(R8)2, NR8SO2R8, SO2R8, SOR8, SR8, CO2R8, NR8COR8, NR8CO2R8, CON(R8)2, SO2N(R8)2, CF3, OCF3, OCHF2, R9, heterocikloalkil, heterocikloalkoksi, aril, heteroaril ili linearni, razgranati ili ciklični (C1-C8)-R9 gdje do tri CH2 jedinice mogu biti zamijenjene sa O, CO, S, SO, SO2 ili NR8.
16. Spoj prema patentnom zahtjevu 15, naznačen time što R2 je H, COCF3, COtBu, Cl, COCH3, CF2CF3, CH2CF3, CF3, CN, Br, COCH(CH3)2, COCH2CH3, CH(OH)CF3, SO2CH3,
[image]
COPh,
[image]
ili
[image]
17. Spoj prema patentnom zahtjevu 15, naznačen time što R3 je H, CH3, CH2CH3, CH2CH2OCH3, CH2CH2OH, CH2CO2CH2CH3, CH2CON(CH3)2, CH2CONH2, CH2CN, benzil, ciklobutil, CH2CH(CH2)2, CH(CH2)2, CH2CF3, CH2CHF2, COCH3, COCH2CH3, CO2CH3, CO2CH2CH3, COH, CONH(CH3)2 ili CONHCH3.
18. Spoj prema patentnom zahtjevu 15, naznačen time što R6 je H, CH3, OCH3, OCH2CH3, OCH2CH2CH3, OCH(CH3)2, CF3, CN, Ph, SO2CH3, OH, CH(CH3)2, OCH2CH2CH2CH3, F, Cl ili CH2OH.
19. Spoj prema patentnom zahtjevu 15, naznačen time što R7 je H, CH3, CH2CH3, tBu, Cl, F, OH, C(=CH2)CH3, OC(=CH2)CH3, OCH3, OCH2CH2CH2CH3, CH2OH, OCH2CH2OH, OCH2CH2CH2OH, OtBu, OCH(CH3)(CH2CH3), OCH2C(CH3)2OH, C(CH3)2OH, CH2C(CH3)2OH, CH(OH)CH(CH3)2, C(CH3)2CH2OH, OCH2CH2CH(CH3)2, OCH2CH2CH3, OCH(CH3)2, OCH2CH2OCH3,
[image]
SO2CH3, SO2tBu, SO2CH2CH3, SO2CH2CH(CH3)2, SO2CH(CH3)2,
[image]
, SO2NH(CH3), SO2NH(CH(CH2)2), SO2NH(CH2CH3), SO2NH(CH(CH3)2), SO2N(CH3)2,
[image]
, OPh, Ph,
[image]
, OCH2CH2OCH3, CH(CH3)2, SO2N(CH2CH3)2, CH2CH2CH2CH3, CH2CH2CH3, OCH2CH2CH2CH3, CH2OPh,
[image]
, OCH2Ph, CH2CH2CH2CH2CH3, OCH2CH3, OCH2CH(CH3)2, CH2CH3, CH2Ph,
[image]
, CCCH2OCH3, SO2CHF2, OCF3,
[image]
, OCHF2,
[image]
, CH2CH(CH3)2, OCH2tBu,
[image]
, OCH2CF3,
[image]
,
[image]
, CH2OCH2CH2CF3, CH2OCH2CF3, SO2CF3, C(CH3)2CH2CH3, C(CH2CH3)3, CH(OCH2CF3)2,
[image]
, CF3, OCH2C(CH3)2F,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
, CH(OH)CH2OCH2CF3, CH(OCH2CF3)CH2OH, OSO2CF3,
[image]
ili OCH2CH2OCF3.
20. Spoj prema patentnom zahtjevu 15, naznačen time što
[image]
grupa je:
[image]
[image]
[image]
[image]
[image]
[image]
[image]
ili
[image]
21. Spoj prema patentnom zahtjevu 1, naznačen time što je spoj izabran iz slijedeće tabele:
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.
22. Farmaceutska kompozicija koja sadrži spoj prema patentnom zahtjevu 1 i farmaceutski prihvatljiv nosač.
23. Spoj prema patentnom zahtjevu 1 za uporabu u postupku inhibicije od napona zavisnog natrijeva ionskog kanala u:
pacijentu; ili
biološkom uzorku;
koji sadrži primjenu na pacijenta, ili dovođenje u kontakt biološkog uzorka, sa spojem prema patentnom zahtjevu 1.
24. Spoj za uporabu prema patentnom zahtjevu 23, naznačen time što od napona ovisan natrijev ionski kanal je NaV 1.7.
25. Spoj prema patentnom zahtjevu 1 za uporabu u postupku liječenja ili redukcije težine kod subjekta akutne, kronične, neuropatske ili inflamatorne boli, artritisa, migrene, klaster glavobolja, trigeminalne neuralgije, herpatične neuralgije, općih neuralgija, epilepsije ili epileptičnih stanja, neurodegenerativnih bolesti, psihijatrijskih poremećaja, anksioznosti, depresije, bipolarnog poremećaja, miotonije, aritmije, poremećaja kretanja, neuroendokrinih poremećaja, ataksije, multiple skleroze, sindroma iritabilnog crijeva, inkontinencije, viscerale boli, osteoartritične boli, postherpetične neuralgije, dijabetičke neuropatije, radikularne boli, išijasa, boli u leđima, boli u glavi ili vratu, teške ili uporne boli, nociceptivne boli, probadajuće boli, post-kirurške boli, kancerske boli, moždanog udara, cerebralne ishemije, traumatske povrede mozga, amiotrofne lateralne skleroze, angine incirane stresom ili tjelesnim vježbama, palpitacija, hipertenzije, migrene ili abormalne gastro-intestinalne pokretljivosti, koji sadrži primjenu efikasne količine spoja prema patentnom zahtjevu 1.
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US201161438685P | 2011-02-02 | 2011-02-02 | |
US201161440987P | 2011-02-09 | 2011-02-09 | |
US201161495538P | 2011-06-10 | 2011-06-10 | |
PCT/US2012/023593 WO2012106499A1 (en) | 2011-02-02 | 2012-02-02 | Pyrrolopyrazine-spirocyclic piperidine amides as modulators of ion channels |
EP12704985.6A EP2670752B1 (en) | 2011-02-02 | 2012-02-02 | Pyrrolopyrazine-spirocyclic piperidine amides as modulators of ion channels |
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EP (2) | EP2670752B1 (hr) |
JP (2) | JP6021824B2 (hr) |
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CN (2) | CN103403004B (hr) |
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Families Citing this family (59)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP5389030B2 (ja) | 2007-08-24 | 2014-01-15 | バーテックス ファーマシューティカルズ インコーポレイテッド | (特に)嚢胞性線維症の処置に有用なイソチアゾロピリジノン |
EP2595989B1 (en) | 2010-05-06 | 2016-07-13 | Vertex Pharmaceuticals Incorporated | Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels |
KR101923367B1 (ko) * | 2011-02-02 | 2018-12-04 | 버텍스 파마슈티칼스 인코포레이티드 | 이온 채널의 조절제로서의 피롤로피라진―스피로사이클릭 피페리딘 아미드 |
CA2827311A1 (en) | 2011-02-18 | 2012-08-23 | Vertex Pharmaceuticals Incorporated | Chroman-spirocyclic piperidine amides as modulators of ion channels |
EP2686325B1 (en) | 2011-03-14 | 2016-12-14 | Vertex Pharmaceuticals Incorporated | Morpholine-spirocyclic piperidine amides as modulators of ion channels |
CN104093716B (zh) | 2011-10-31 | 2017-06-23 | 克赛农制药股份有限公司 | 联芳醚磺酰胺化合物及其作为治疗剂的用途 |
EP2773637B1 (en) | 2011-10-31 | 2016-06-08 | Xenon Pharmaceuticals Inc. | Benzenesulfonamide compounds and their use as therapeutic agents |
AR091112A1 (es) | 2012-05-22 | 2015-01-14 | Genentech Inc | Benzamidas n-sustituidas como inhibidores de los canales de sodio nav1.7 |
KR101663436B1 (ko) | 2012-07-06 | 2016-10-06 | 제넨테크, 인크. | N-치환된 벤즈아미드 및 이의 사용 방법 |
WO2014022639A1 (en) | 2012-08-01 | 2014-02-06 | Vertex Pharmaceuticals Incorporated | Solid forms of (4-isopropoxy-3-methoxyphenyl)(2'-methyl-6'-(trifluoromethyl)-3',4'-dihydro-2'h-spiro[piperidine-4,1'-pyrrolo[1,2-a]pyrazine]-1-yl)methanone |
WO2014120808A1 (en) | 2013-01-31 | 2014-08-07 | Vertex Parmaceuticals Incorporated | Pyridone amides as modulators of sodium channels |
EP2951168B1 (en) | 2013-01-31 | 2017-01-04 | Vertex Pharmaceuticals Incorporated | Quinoline and quinoxaline amides as modulators of sodium channels |
US9828345B2 (en) | 2013-02-28 | 2017-11-28 | Bristol-Myers Squibb Company | Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors |
TW201444798A (zh) | 2013-02-28 | 2014-12-01 | 必治妥美雅史谷比公司 | 作爲強效rock1及rock2抑制劑之苯基吡唑衍生物 |
RU2015143906A (ru) | 2013-03-14 | 2017-04-18 | Дженентек, Инк. | Замещенные триазолопиридины и способы их применения |
RU2015143834A (ru) | 2013-03-15 | 2017-04-24 | Дженентек, Инк. | Замещенные бензоксазолы и способы их применения |
JP6605462B2 (ja) * | 2013-07-10 | 2019-11-13 | バーテックス ファーマシューティカルズ インコーポレイテッド | イオンチャネルのモジュレーターとしての縮合ピペリジンアミド |
PE20160548A1 (es) | 2013-07-19 | 2016-05-21 | Vertex Pharma | Sulfonamidas como moduladores de canales de sodio |
CN105793238B (zh) | 2013-11-27 | 2019-12-24 | 基因泰克公司 | 经取代的苯甲酰胺及其使用方法 |
PT3080134T (pt) | 2013-12-13 | 2018-11-08 | Vertex Pharma | Pró-fármacos de piridona amidas úteis como moduladores de canais de sódio |
CN106715418A (zh) | 2014-07-07 | 2017-05-24 | 基因泰克公司 | 治疗化合物及其使用方法 |
CN107835805A (zh) | 2015-05-22 | 2018-03-23 | 基因泰克公司 | 被取代的苯甲酰胺和其使用方法 |
WO2017035271A1 (en) | 2015-08-27 | 2017-03-02 | Genentech, Inc. | Therapeutic compounds and methods of use thereof |
RU2018115718A (ru) | 2015-09-28 | 2019-10-28 | Дженентек, Инк. | Терапевтические соединения и способы их применения |
JP2018535234A (ja) | 2015-11-25 | 2018-11-29 | ジェネンテック, インコーポレイテッド | ナトリウムチャネル遮断薬として有用な置換ベンズアミド |
EP3436432B1 (en) | 2016-03-30 | 2021-01-27 | Genentech, Inc. | Substituted benzamides and methods of use thereof |
BR112019007763A2 (pt) | 2016-10-17 | 2019-07-02 | Genentech Inc | composto de fórmula, composição farmacêutica, métodos para tratar uma doença ou condição, para tratar dores, para diminuir o fluxo de íons e para tratar prurido, uso de um composto e invenção |
CN106749330A (zh) * | 2016-12-29 | 2017-05-31 | 长春海谱润斯科技有限公司 | 一种杂环衍生物及使用该杂环衍生物的有机发光器件 |
JP2020511511A (ja) | 2017-03-24 | 2020-04-16 | ジェネンテック, インコーポレイテッド | ナトリウムチャネル阻害剤としての4−ピペリジン−n−(ピリミジン−4−イル)クロマン−7−スルホンアミド誘導体 |
US11358977B2 (en) | 2017-05-16 | 2022-06-14 | Vertex Pharmaceuticals Incorporated | Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels |
CN111065383A (zh) | 2017-07-11 | 2020-04-24 | 沃泰克斯药物股份有限公司 | 用作钠通道调节剂的羧酰胺 |
TW202002971A (zh) | 2018-02-12 | 2020-01-16 | 美商維泰克斯製藥公司 | 治療疼痛的方法 |
WO2019165290A1 (en) | 2018-02-26 | 2019-08-29 | Genentech, Inc. | Pyridine-sulfonamide compounds and their use against pain and related conditions |
CN111936494A (zh) * | 2018-03-30 | 2020-11-13 | 豪夫迈·罗氏有限公司 | 作为钠通道抑制剂的取代的氢-吡啶并-吖嗪 |
EP3820860A4 (en) | 2018-07-09 | 2022-04-20 | Lieber Institute, Inc. | PYRIDAZINEG COMPOUNDS TO INHIBIT NAV1.8 |
CN113271940A (zh) * | 2018-10-15 | 2021-08-17 | 林伯士拉克许米公司 | Tyk2抑制剂和其用途 |
WO2020146612A1 (en) | 2019-01-10 | 2020-07-16 | Vertex Pharmaceuticals Incorporated | Esters and carbamates as modulators of sodium channels |
US20230062053A1 (en) | 2019-01-10 | 2023-03-02 | Vertex Pharmaceuticals Incorporated | Carboxamides as modulators of sodium channels |
WO2020176763A1 (en) | 2019-02-27 | 2020-09-03 | Vertex Pharmaceuticals Incorporated | Dosage form comprising prodrug of na 1.8 sodium channel inhibitor |
BR112021017809A2 (pt) | 2019-03-11 | 2021-11-23 | Nocion Therapeutics Inc | Bloqueadores de canais iônicos substituídos por éster e métodos para uso |
US10786485B1 (en) | 2019-03-11 | 2020-09-29 | Nocion Therapeutics, Inc. | Charged ion channel blockers and methods for use |
JP2022527690A (ja) * | 2019-03-11 | 2022-06-03 | ノシオン セラピューティクス,インコーポレイテッド | 荷電したイオンチャンネル遮断薬および使用方法 |
US10934263B2 (en) | 2019-03-11 | 2021-03-02 | Nocion Therapeutics, Inc. | Charged ion channel blockers and methods for use |
WO2020219867A1 (en) | 2019-04-25 | 2020-10-29 | Vertex Pharmaceuticals Incorporated | Pyridone amide co-crystal compositions for the treatment of pain |
AU2020380118A1 (en) | 2019-11-06 | 2022-05-19 | Nocion Therapeutics, Inc. | Charged ion channel blockers and methods for use |
JP2023500890A (ja) | 2019-11-06 | 2023-01-11 | ノシオン セラピューティクス,インコーポレイテッド | 荷電したイオンチャンネル遮断薬および使用方法 |
CR20220316A (es) | 2019-12-06 | 2022-10-07 | Vertex Pharma | Tetrahidrofuranos sustituidos como moduladores de canales de sodio |
JP2023517604A (ja) | 2020-03-11 | 2023-04-26 | ノシオン セラピューティクス,インコーポレイテッド | 荷電したイオンチャンネル遮断薬および使用方法 |
EP4347033A1 (en) | 2021-06-04 | 2024-04-10 | Vertex Pharmaceuticals Incorporated | Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels |
BR112023025264A2 (pt) | 2021-06-04 | 2024-02-20 | Vertex Pharma | Formas farmacêuticas sólidas e regimes posológicos compreendendo (2r,3s,4s,5r)-4-[[3- (3,4-difluoro-2-metóxi-fenil)-4,5-dimetil-5-(trifluorometil) tetra-hidrofuran-2-carbonil]amino ]piridina-2-carboxamida |
CN117794918A (zh) | 2021-06-04 | 2024-03-29 | 沃泰克斯药物股份有限公司 | 经取代的四氢呋喃类似物作为钠通道调节剂 |
AU2022283934A1 (en) | 2021-06-04 | 2023-11-30 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels |
EP4347584A1 (en) | 2021-06-04 | 2024-04-10 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels |
IL308953A (en) | 2021-06-04 | 2024-01-01 | Vertex Pharma | N-Hydroalkyl(Hetero)Aryl)Tetrahydrofuran Carboxamides as Natrene Channel Modulators |
TW202408501A (zh) | 2022-04-22 | 2024-03-01 | 美商維泰克斯製藥公司 | 用於治療疼痛之雜芳基化合物 |
TW202404969A (zh) | 2022-04-22 | 2024-02-01 | 美商維泰克斯製藥公司 | 用於治療疼痛之雜芳基化合物 |
WO2023205468A1 (en) | 2022-04-22 | 2023-10-26 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
WO2023205465A1 (en) | 2022-04-22 | 2023-10-26 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
WO2024123815A1 (en) | 2022-12-06 | 2024-06-13 | Vertex Pharmaceuticals Incorporated | Process for the synthesis of substituted tetrahydrofuran modulators of sodium channels |
Family Cites Families (69)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3939159A (en) | 1974-05-29 | 1976-02-17 | American Hoechst Corporation | Spiro(pyrrolo (1,2-A)quinoxalines) |
PT67194B (en) | 1976-11-02 | 1979-03-23 | Lilly Co Eli | Process for preparing 4a-aryl-octahydro-1h-2-pyrindines |
PL117572B1 (en) | 1977-12-27 | 1981-08-31 | Lilly Co Eli | Process for preparing novel derivatives of trans-4a-phenyl-2,3,4,4a,5,6,7,7a-octahydro-1h-2-pyrindine3,4,4a,5,6,7,7a-oktagidro-1h-2-piridina |
US4353901A (en) | 1981-10-19 | 1982-10-12 | Syntex (U.S.A.) Inc. | 9-(1,4-Benzodioxan-2-ylalkyl and hydroxyalkyl)-1-oxa-4,9-diazaspiro[5.5]undecan-3-ones |
GB8827479D0 (en) | 1988-11-24 | 1988-12-29 | Zambeletti Spa L | Novel compounds |
IL96507A0 (en) | 1989-12-08 | 1991-08-16 | Merck & Co Inc | Nitrogen-containing spirocycles and pharmaceutical compositions containing them |
US5206240A (en) | 1989-12-08 | 1993-04-27 | Merck & Co., Inc. | Nitrogen-containing spirocycles |
US5304121A (en) | 1990-12-28 | 1994-04-19 | Boston Scientific Corporation | Drug delivery system making use of a hydrogel polymer coating |
JPH04297458A (ja) | 1991-03-27 | 1992-10-21 | Toray Ind Inc | イソキノリン誘導体およびその製造方法 |
GB9104656D0 (en) | 1991-03-05 | 1991-04-17 | Zambeletti Spa L | Pharmaceuticals |
US5994341A (en) | 1993-07-19 | 1999-11-30 | Angiogenesis Technologies, Inc. | Anti-angiogenic Compositions and methods for the treatment of arthritis |
DE4341403A1 (de) | 1993-12-04 | 1995-06-08 | Basf Ag | N-substituierte 3-Azabicycloalkan-Derivate, ihre Herstellung und Verwendung |
US6017768A (en) | 1994-05-06 | 2000-01-25 | Pharmacopeia, Inc. | Combinatorial dihydrobenzopyran library |
WO1995030642A1 (en) | 1994-05-06 | 1995-11-16 | Pharmacopeia, Inc. | Combinatorial dihydrobenzopyran library |
US6099562A (en) | 1996-06-13 | 2000-08-08 | Schneider (Usa) Inc. | Drug coating with topcoat |
IT1276462B1 (it) | 1995-07-03 | 1997-10-31 | Rotta Research Lab | Diamidi aromatiche acide ad attivita' antigastrinica, procedimento per la loro preparazione e loro uso farmaceutico |
ATE274499T1 (de) | 1995-09-29 | 2004-09-15 | Lilly Co Eli | Spiro verbindungen als inhibitoren der fibrinogen-abhängigen blutplättchen aggregation |
US20040266802A1 (en) | 1999-06-07 | 2004-12-30 | Alain Calvet | Tricyclic analgesics |
BR0011427A (pt) * | 1999-06-07 | 2002-03-26 | Warner Lambert Co | Analgésicos tricìclicos |
US20020151712A1 (en) | 1999-09-14 | 2002-10-17 | Nan-Horng Lin | 3-pyrrolidinyloxy-3'-pyridyl ether compounds useful for controlling chemical synaptic transmission |
AU2001289831A1 (en) | 2000-09-06 | 2002-03-22 | Bayer Aktiengesellschaft | Medicaments against viral infections |
US20040014744A1 (en) | 2002-04-05 | 2004-01-22 | Fortuna Haviv | Substituted pyridines having antiangiogenic activity |
AU2003235912A1 (en) | 2002-05-10 | 2003-11-11 | Taisho Pharmaceutical Co., Ltd. | Spiro-ring compound |
EP1533314A4 (en) | 2002-06-11 | 2006-08-02 | Sankyo Co | PROCESS FOR THE PREPARATION OF CYCLIC THIOETHERES, AND SYNTHETIC INTERMEDIATE DAF R |
EP1554260A1 (en) | 2002-10-22 | 2005-07-20 | Glaxo Group Limited | Aryloxyalkylamine derivatives as h3 receptor ligands |
WO2004037828A1 (ja) | 2002-10-24 | 2004-05-06 | Sankyo Company, Limited | 光学活性なスルホキシドの製造法 |
JP2006511554A (ja) | 2002-12-13 | 2006-04-06 | スミスクライン ビーチャム コーポレーション | Ccr5アンタゴニストとしてのピペリジン誘導体 |
CA2512886A1 (en) | 2003-02-28 | 2004-09-10 | Galderma Research & Development, S.N.C. | Ligands that modulate lxr-type receptors |
WO2004092179A1 (ja) | 2003-04-14 | 2004-10-28 | Nippon Soda Co. Ltd. | スピロ誘導体、製造法および抗酸化薬 |
FR2856685B1 (fr) | 2003-06-25 | 2005-09-23 | Merck Sante Sas | Derives de thiazolylpiperidine, leurs procedes de preparation et les compositions pharmaceutiques qui les contiennent |
BRPI0415165A (pt) | 2003-10-01 | 2007-01-09 | Adolor Corp | composto heterocìclico espirocìclico, composição farmacêutica, método para ligar receptores opióides, métodos para prevenir ou tratar dor, disfunção gastrointestinal, um distúrbio do trato urogenital, um distúrbio imunomodulatório, um distúrbio inflamatório, um distúrbio de função respiratória, ansiedade, distúrbio do humor, um distúrbio relacionado a estresse, distúrbio do sistema nervoso simpático, tosse, e um distúrbio motor, método para tratar uma lesão traumática ao sistema nervoso central, métodos para prevenir ou tratar acidente vascular, arritmia cardìaca, glaucoma, e disfunção sexual, métodos para tratar uma condição selecionada do grupo consistindo de choque, edema cerebral, isquemia cerebral, déficit cerebral após cirurgia cardìaca (bypass) e enxerto, lupus eritematoso sistêmico, doença de hodgkin, doença de sjogren, epilepsia, e rejeição em transplantes de órgão e enxertos de pele, e para tratar dependência de substáncias, métodos para melhorar a sobrevivência de órgãos e células, e cardioproteção após infarto do miocárdio, métodos para reduzir a necessidade de anestesia, para produzir ou manter um estado anestésico, derivado radiomarcado de um composto, derivado isotopicamente marcado de um composto, composto e método de diagnóstico por imagem |
US20070078120A1 (en) | 2003-10-21 | 2007-04-05 | Hitoshi Ban | Novel piperidine derivative |
TWI350168B (en) | 2004-05-07 | 2011-10-11 | Incyte Corp | Amido compounds and their use as pharmaceuticals |
WO2005121090A1 (en) | 2004-06-02 | 2005-12-22 | Abbott Laboratories | Substituted piperidines that have antiangiogenic activity |
US7598261B2 (en) | 2005-03-31 | 2009-10-06 | Adolor Corporation | Spirocyclic heterocyclic derivatives and methods of their use |
JP2008540395A (ja) | 2005-05-03 | 2008-11-20 | ファイザー・インク | アミドレソルシノール化合物 |
WO2007050124A1 (en) | 2005-05-19 | 2007-05-03 | Xenon Pharmaceuticals Inc. | Fused piperidine derivatives and their uses as therapeutic agents |
US7935712B2 (en) | 2005-07-19 | 2011-05-03 | Merck Sharp & Dohme Corp. | Spirochromanone derivatives as acetyl coenzyme A carboxylase (ACC) inhibitors |
CA2621255A1 (en) | 2005-09-21 | 2007-04-05 | Incyte Corporation | Amido compounds and their use as pharmaceuticals |
ES2407115T3 (es) | 2005-11-18 | 2013-06-11 | Ono Pharmaceutical Co., Ltd. | Compuesto que contiene un grupo básico y uso del mismo |
CN101360750A (zh) * | 2005-11-23 | 2009-02-04 | 英特芒尼公司 | 应激活化蛋白激酶系统的调节方法 |
AR057579A1 (es) | 2005-11-23 | 2007-12-05 | Merck & Co Inc | Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac) |
WO2007124045A2 (en) | 2006-04-20 | 2007-11-01 | Ampla Pharmaceuticals, Inc. | Piperidine and piperazine compounds for use in the treatment of obesity, eating disorders and sexual dysfunction by potentiation of mc4 receptor activity |
JP2009536175A (ja) | 2006-05-05 | 2009-10-08 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 特定の細胞サイクル酵素の阻害剤としてのスピロ−(tho)ベンゾピラン−2,4’−ピペリジン−及びシクロヘキサン誘導体 |
JP5257068B2 (ja) | 2006-05-16 | 2013-08-07 | 小野薬品工業株式会社 | 保護されていてもよい酸性基を含有する化合物およびその用途 |
EP2023924B1 (en) | 2006-05-18 | 2016-08-03 | Merck Sharp & Dohme Corp. | Aryl-fused spirocyclic compounds |
US20090325992A1 (en) | 2006-07-31 | 2009-12-31 | Ono Pharmaceutical Co., Ltd. | Compound having cyclic group bound thereto through spiro binding and use thereof |
CN101534819A (zh) | 2006-09-12 | 2009-09-16 | 阿得罗公司 | 含氮的螺环化合物用于增强认知功能的应用 |
TW200831497A (en) | 2006-10-12 | 2008-08-01 | Epix Delaware Inc | Carboxamide compounds and their use |
BRPI0721053A2 (pt) | 2006-11-29 | 2014-07-29 | Pfizer Prod Inc | INIBIDORES DE ESPIROCETONA ACETIL-CoA CARBOXILASE |
US7501432B2 (en) * | 2006-12-22 | 2009-03-10 | Hoffman-La Roche Inc. | Spiro-piperidine derivatives |
PE20081559A1 (es) | 2007-01-12 | 2008-11-20 | Merck & Co Inc | DERIVADOS DE ESPIROCROMANONA SUSTITUIDOS COMO INHIBIDORES DE ACETIL CoA CARBOXILASA |
WO2008088692A2 (en) | 2007-01-12 | 2008-07-24 | Merck & Co., Inc. | Spirochromanon derivatives |
JPWO2008102749A1 (ja) | 2007-02-20 | 2010-05-27 | 武田薬品工業株式会社 | 複素環化合物 |
EP2110377A1 (en) | 2008-04-15 | 2009-10-21 | DAC S.r.l. | Spirocyclic derivatives as histone deacetylase inhibitors |
WO2009144554A1 (en) | 2008-05-28 | 2009-12-03 | Pfizer, Inc. | Pyrazolospiroketone acetyl-c0a carboxylase inhibitors |
US8524730B2 (en) | 2008-07-04 | 2013-09-03 | Msd K.K. | Spirochromanone carboxylic acids |
US8822480B2 (en) | 2008-07-16 | 2014-09-02 | Merck Sharp & Dohme Corp. | Bicyclic heterocycle derivatives and use thereof as GPR119 modulators |
WO2010027567A2 (en) | 2008-07-23 | 2010-03-11 | Schering Corporation | Tricyclic spirocycle derivatives and methods of use thereof |
EP2488177B1 (en) | 2008-10-31 | 2016-10-12 | Pain Therapeutics, Inc. | Filamin a binding anti-inflammatory and analgesic |
EP2498600B1 (en) | 2008-10-31 | 2016-03-02 | Pain Therapeutics, Inc. | Filamin a-binding anti-inflammatory analgesic |
US8580807B2 (en) | 2009-04-03 | 2013-11-12 | Merck Sharp & Dohme Corp. | Bicyclic piperidine and piperazine derivatives as GPCR modulators for the treatment of obesity, diabetes and other metabolic disorders |
WO2010151595A1 (en) * | 2009-06-26 | 2010-12-29 | Schering Corporation | Pyrrolo-benzo-1,4-diazines useful as sodium channel blockers |
EP2470021B1 (en) | 2009-08-27 | 2014-10-22 | Merck Sharp & Dohme Corp. | Novel pyrrolidine derived beta 3 adrenergic receptor agonists |
UY33199A (es) | 2010-01-26 | 2011-08-31 | Boehringer Ingelheim Int | 5-alquinil-pirimidinas. |
EP2595989B1 (en) | 2010-05-06 | 2016-07-13 | Vertex Pharmaceuticals Incorporated | Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels |
KR101923367B1 (ko) * | 2011-02-02 | 2018-12-04 | 버텍스 파마슈티칼스 인코포레이티드 | 이온 채널의 조절제로서의 피롤로피라진―스피로사이클릭 피페리딘 아미드 |
CA2827311A1 (en) | 2011-02-18 | 2012-08-23 | Vertex Pharmaceuticals Incorporated | Chroman-spirocyclic piperidine amides as modulators of ion channels |
EP2686325B1 (en) | 2011-03-14 | 2016-12-14 | Vertex Pharmaceuticals Incorporated | Morpholine-spirocyclic piperidine amides as modulators of ion channels |
-
2012
- 2012-02-02 KR KR1020137023136A patent/KR101923367B1/ko active IP Right Grant
- 2012-02-02 CN CN201280011207.8A patent/CN103403004B/zh active Active
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- 2012-02-02 WO PCT/US2012/023593 patent/WO2012106499A1/en active Application Filing
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- 2012-02-02 CN CN201610319591.8A patent/CN106008504A/zh active Pending
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- 2012-02-02 JP JP2013552619A patent/JP6021824B2/ja active Active
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- 2012-02-02 BR BR112013019211A patent/BR112013019211A2/pt not_active Application Discontinuation
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