HRP20160125T1 - Spojevi 1h-indazol-3-karboksamida kao inhibitori glikogen sinteze kinaze-3 beta - Google Patents
Spojevi 1h-indazol-3-karboksamida kao inhibitori glikogen sinteze kinaze-3 beta Download PDFInfo
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- HRP20160125T1 HRP20160125T1 HRP20160125TT HRP20160125T HRP20160125T1 HR P20160125 T1 HRP20160125 T1 HR P20160125T1 HR P20160125T T HRP20160125T T HR P20160125TT HR P20160125 T HRP20160125 T HR P20160125T HR P20160125 T1 HRP20160125 T1 HR P20160125T1
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- indazole
- alkoxy
- carboxamide
- alkyl
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- 150000008581 1H-indazole-3-carboxamides Chemical class 0.000 title 1
- 102000019058 Glycogen Synthase Kinase 3 beta Human genes 0.000 title 1
- 108010051975 Glycogen Synthase Kinase 3 beta Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- DITBWPUMEUDVLU-UHFFFAOYSA-N 1h-indazole-3-carboxamide Chemical compound C1=CC=C2C(C(=O)N)=NNC2=C1 DITBWPUMEUDVLU-UHFFFAOYSA-N 0.000 claims 21
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 13
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 12
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 12
- 229910052736 halogen Inorganic materials 0.000 claims 11
- 125000001424 substituent group Chemical group 0.000 claims 11
- 150000002367 halogens Chemical group 0.000 claims 10
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 8
- 208000035475 disorder Diseases 0.000 claims 7
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 5
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims 5
- 125000002837 carbocyclic group Chemical group 0.000 claims 5
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 208000024714 major depressive disease Diseases 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 208000015122 neurodegenerative disease Diseases 0.000 claims 4
- 208000020925 Bipolar disease Diseases 0.000 claims 3
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 3
- 150000007522 mineralic acids Chemical class 0.000 claims 3
- 230000004770 neurodegeneration Effects 0.000 claims 3
- 150000007524 organic acids Chemical class 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 201000000980 schizophrenia Diseases 0.000 claims 3
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 2
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 2
- 208000020401 Depressive disease Diseases 0.000 claims 2
- 206010013654 Drug abuse Diseases 0.000 claims 2
- 206010022489 Insulin Resistance Diseases 0.000 claims 2
- 208000019022 Mood disease Diseases 0.000 claims 2
- 201000009916 Postpartum depression Diseases 0.000 claims 2
- 125000001931 aliphatic group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 208000025748 atypical depressive disease Diseases 0.000 claims 2
- 239000002585 base Substances 0.000 claims 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 239000000460 chlorine Substances 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 208000012672 seasonal affective disease Diseases 0.000 claims 2
- 208000011117 substance-related disease Diseases 0.000 claims 2
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000009810 Catatonic Schizophrenia Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000001495 Disorganized Schizophrenia Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000028017 Psychotic disease Diseases 0.000 claims 1
- 208000036755 Schizophrenia simple Diseases 0.000 claims 1
- 208000036754 Schizophrenia, catatonic type Diseases 0.000 claims 1
- 208000036752 Schizophrenia, paranoid type Diseases 0.000 claims 1
- 208000036750 Schizophrenia, residual type Diseases 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 239000003513 alkali Substances 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 206010007776 catatonia Diseases 0.000 claims 1
- 208000026725 cyclothymic disease Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000024732 dysthymic disease Diseases 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 239000011630 iodine Substances 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000003995 melancholia Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 208000002851 paranoid schizophrenia Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 201000010065 polycystic ovary syndrome Diseases 0.000 claims 1
- 239000003368 psychostimulant agent Substances 0.000 claims 1
- 208000020431 spinal cord injury Diseases 0.000 claims 1
- 208000002320 spinal muscular atrophy Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
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- C07D401/02—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 containing two hetero rings
- C07D401/12—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 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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Claims (22)
1. Spojevi 1H-indazol-3-karboksamida, naznačeni time, da imaju sljedeću opću formulu (I):
[image]
u kojoj
su svaki od Ra i Ra' međusobno isti ili različiti, sljedeći: vodikov atom; atom halogena; hidroksi skupina, skupine C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil i C1-C6 alkoksi, opcijski supstituirane s jednim ili više supstituenata odabranih iz skupine koju čine halogen, hidroksi, -NH2, i C1-C3 alkoksi; karbociklički ili heterociklički prsten, alifatski ili aromatski, koji ima od 3 do 12 članova, opcijski supstituiran s jednim ili više supstituenata odabranih iz skupine koju čine halogen hidroksi, C1-C6 alkil, C1-C6 alkoksi, -NR1R2, -C(O)OH, -C(O)OR1 i -C(O)NR1R2;
[image]
Y je veza, skupine C1-C6 alkil, C2-C6 alkenil i C2-C6 alkinil, opcijski supstituirane s jednim ili više supstituenata odabranih iz skupine koju čine halogen, hidroksi,-NH2 i C1-C3 alkoksi;
Rb je C1-C6 alkoksi-skupina; -C(O)OH; -C(O)OR1; -NO2; -NHC(O)R1;
R1 i R2 su neovisno vodikov atom, C1-C4 alkil-skupina, C2-C4 alkenil-skupina,
C2-C4 alkinil-skupina i fenil-skupina;
te njegove adicijske soli s farmaceutski prihvatljivim organskim i anorganskim kiselinama i lužinama.
2. Spojevi 1H-indazol-3-karboksamida prema zahtjevu 1, naznačeni time, da su svaki od Ra i Ra' međusobno isti ili različiti, sljedeći: vodikov atom; atom halogena odabran od klora, broma i joda; hidroksi skupina; skupine C1-C6 alkil i C1-C6 alkoksi, opcijski supstituirane s jednim ili više supstituenata odabranih iz skupine koju čine halogen, hidroksi, -NH2, ili C1-C3 alkoksi; karbociklički ili heterociklički prsten, zasićen ili nezasićen, koji ima od 4 do 10 članova, opcijski supstituiran s jednim ili više supstituenata odabranih iz skupine koju čine halogen, hidroksi, C1-C6 alkil,
C1-C6 alkoksi, -NR1R2, -C(O)OH, -C(O)OR1 i -C(O)N1R2; i
R1 i R2 su neovisno vodikov atom, C1-C4 alkil-skupina, C2-C1 alkenil-skupina,C2-C4 alkinil-skupina i fenil-skupina.
3. Spojevi 1H-indazol-3-karboksamida prema zahtjevu 2, naznačeni time, da su svaki od Ra i Ra' međusobno isti ili različiti, sljedeći: atom halogena odabran od klora ili broma; hidroksi skupina; C1-C6 alkil-skupina; C1-C6 alkoksi-skupina; ili karbociklički ili heterociklički prsten, zasićen ili nezasićen, koji ima od 5 do 6 članova, opcijski supstituiran s jednim ili više supstituenata odabranih iz skupine koju čine halogen, hidroksi, C1-C6 alkil, C1-C6 alkoksi, -NR1R2 -COOH; i
R1 i R2 su neovisno vodikov atom, C1-C4 alkil-skupina, C2-C4 alkenil-skupina,
C2-C4 alkinil-skupina i fenil-skupina.
4. Spojevi 1H-indazol-3-karboksamida prema zahtjevu 3, naznačeni time, da su svaki od Ra i Ra' međusobno isti ili različiti, sljedeći: atom broma; hidroksi skupina; C1-C3 alkoksi-skupina; ili nezasićeni karbociklički ili heterociklički prsten koji ima 6 članova, opcijski supstituiran s jednim ili dva supstituenta odabrana iz skupine koju čine halogen, hidroksi, C1-C3 alkil, C1-C3 alkoksi, -NR1R2i -COOH; i
R1 i R2 su neovisno vodikov atom, C1-C4 alkil-skupina, C2-C4 alkenil-skupina,
C2-C4 alkinil-skupina i fenil-skupina.
5. Spojevi 1H-indazol-3-karboksamida prema bilo kojem od prethodnih zahtjeva, naznačeni time, da Y je veza, C1-C6 alkil-skupina opcijski supstituirana s jednim ili više supstituenata odabranih iz skupine koju čine halogen, hidroksi, -NH2 i C1-C3 alkoksi.
6. Spojevi 1H-indazol-3-karboksamiđa prema zahtjevu 5, naznačeni time, da
Y je C1-C6 alkil-skupina.
7. Spojevi 1H-indazol-3-karboksamida prema zahtjevu 6, naznačeni time, da
Y je C4-C3 alkil-skupina.
8. Spojevi 1H-indazol-3-karboksamida prema bilo kojem od prethodnih zahtjeva, naznačeni time, da Rb je C1-C6 alkoksi-skupina; C(O)OH; -C(O)OR1; -NHCOR1.
9. Spojevi 1H-indazol-3-karboksamida prema zahtjevu 8, naznačeni time, da Rb je C1-C6 alkoksi-skupina; C(O)OH.
10. Spojevi lH-indazol-3-karboksamida prema zahtjevu 9, naznačeni time, da Rb je C1C3 alkoksi-skupina; C(O)OH.
11. Spojevi 1H-indazol-3-karboksamida prema bilo kojem od prethodnih zahtjeva, naznačeni time, da R1 i R2 su neovisno C1-C3 alkil-skupina.
12. Spojevi 1H-indazol-3-karboksamida, koji imaju sljedeću opću formulu (I):
[image]
u kojoj
su svaki od Ra i Ra' međusobno isti ili različiti, sljedeći: vodikov atom; atom halogena; hidroksi skupina, skupine C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil i C1-C6 alkoksi, opcijski supstituirane s jednim ili više supstituenata odabranih iz skupine koju čine halogen, hidroksi, -NH2 i C1-C3 alkoksi; karbociklički ili heterociklički prsten, alifatski ili aromatski, koji ima od 3 do 12 članova, opcijski supstituiran s jednim ili više supstituenata odabranih iz skupine koju čine halogen, hidroksi, C1-C6 alkil, C1-C6 alkoksi, -NR1R2, -C(O)OH, -C(O)OR1 i -C(O)NR1R2;
Y je veza, skupine C1-C6 alkil, C2-C6 alkenil i C2-C6 alkinil, opcijski supstituirane s jednim ili više supstituenata odabranih iz skupine koju čine halogen, hidroksi,-NH2 i C1-C3 alkoksi;
Rb je C1-C6 alkoksi-skupina; -C(O)OH; -C(O)OR1; -NO2; -NHC(O)R1;R1 i R2 su neovisno vodikov atom, C1-C4 alkil-skupina, C2-C4 alkenil-skupina,
C2-C4 alkinil-skupina i fenil-skupina;
te njegove adicijske soli s farmaceutski prihvatljivim organskim i anorganskim kiselinama i lužinama; naznačeni time, da se upotrebljavaju u liječenju bolesti koje se pojavljuju zbog nekontroliranog aktiviranja i/ili zbog pretjeranog izražavanja GSK-3P, odabranih iz skupine koju čine (i) poremećaji zbog otpornosti na inzulin, (ii) neurodegenerativne bolesti, (iii) poremećaji raspoloženja, (iv) shizofrenični poremećaji,
(v) kancerozni poremećaji, (vi) upala, (vii) poremećaji zbog zlouporaba droga, (viii) epilepsije, i (ix) neuropatski bolovi.
13. 1H-indazol-3-karboksamid za uporabu prema zahtjevu 12,naznačen time, da su navedeni poremećaji zbog otpornosti na inzulin, odabrani iz skupine koju čine dijabetes tipa 2, sindrom X, pretilost i sindrom policističnih jajnika.
14. 1H-indazol-3-karboksamid za uporabu prema zahtjevu 12, naznačen time, da su navedene neurodegenerativne bolesti odabrane iz skupine koju čine Parkinsonova bolest, Alzheimerova bolest, Hungtingtonova bolest i spinalni neurođegenerativni poremećaji.
15. 1H-indazol-3-karboksamid za uporabu prema zahtjevu 14, naznačen time, da su navedeni spinalni neurođegenerativni poremećaji odabrani iz skupine koju čine amiotrofna lateralna skleroza, multipla skleroza, spinalna muskularna atrofija i neurođegeneracija zbog ozljede kralježnične moždine.
16. 1H-inđazol-3-karboksamid za uporabu prema zahtjevu 12, naznačen time, da su navedeni poremećaji raspoloženja, odabrani iz skupine koju čine bipolarni poremećaji i depresivni poremećaji.
17. 1H-indazol-3-karboksamid za uporabu prema zahtjevu 16, naznačen time, da su navedeni bipolarni poremećaji odabrani iz skupine koju čine bipolar I, bipolar II, ciklotimija i bipolarni poremećaj koji nije drugačije opisan (BD-NOS).
18. 1H-indazol-3-karboksamid za uporabu prema zahtjevu 16, naznačen time, da su navedeni depresivni poremećaji odabrani iz skupine koju čine značajan depresivni poremećaj (MDD), netipična depresija (AD), melankolična depresija, psihotička značajna depresija (PMD), katatonička depresija, postporođajna depresija (PPD), sezonski afektivni poremećaj (SAD), distimija i depresivni poremećaj koji nije drugačije opisan (DD-NOS).
19. 1H-indazol-3-karboksamid za uporabu prema zahtjevu 12, naznačen time, da su navedeni poremećaji zbog zlouporabe droga, odabrani iz skupine poremećaja zlostavljanja zbog psihostimulacijskih sredstava.
20. 1H-indazoI-3-karboksamid za uporabu prema zahtjevu 12, naznačen time, da su navedeni shizofrenični poremećaji odabrani iz skupine koju čine paranoidna shizofrenija, dezorganizacijska shizofrenija, katatonička shizofrenija, jednostavna shizofrenija, rezidualna shizofrenija i nediferencirana shizofrenija.
21. 1 H-indazol-3-karboksamid za uporabu prema zahtjevu 12, naznačen time, da su navedeni kancerogeni poremećaji odabrani iz skupine koju čine rak prostate, rak gušterače, rak jajnika i kolorektalni rak, te leukemija povezana s MLL.
22. Farmaceutski sastav, naznačen time, da on obuhvaća učinkovitu količinu najmanje jednog spoja formule (I) prema bilo kojem od zahtjeva 1 do 11, njegovu sol s farmaceutski prihvatljivom organskom ili anorganskom kiselinom ili lužinom, ili njegovu estersku prosupstancu, te najmanje jedno inertno farmaceutski prihvatljivo pomoćno sredstvo.
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| EP12156292 | 2012-02-21 | ||
| EP13704910.2A EP2817302B1 (en) | 2012-02-21 | 2013-02-07 | 1h-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors |
| PCT/EP2013/052400 WO2013124158A1 (en) | 2012-02-21 | 2013-02-07 | 1h-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors |
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| RS54539B1 (en) * | 2012-02-21 | 2016-06-30 | Aziende Chimiche Riunite Angelini Francesco - A.C.R.A.F. - S.P.A. | USE OF 1H-INDASOL-3-CARBOXAMIDE COMPOUNDS AS A 3-BETA GLYCOGEN SYNTHETASE KINASE INHIBITOR |
| US8889730B2 (en) | 2012-04-10 | 2014-11-18 | Pfizer Inc. | Indole and indazole compounds that activate AMPK |
| US9394285B2 (en) | 2013-03-15 | 2016-07-19 | Pfizer Inc. | Indole and indazole compounds that activate AMPK |
| EP3119393A4 (en) | 2014-03-20 | 2018-02-28 | Samumed, LLC | 5-substituted indazole-3-carboxamides and preparation and use thereof |
| ES2913929T3 (es) * | 2016-06-08 | 2022-06-06 | Glaxosmithkline Ip Dev Ltd | Compuestos químicos como inhibidores de la ruta de ATF4 |
| CA3091913A1 (en) | 2018-02-23 | 2019-08-29 | Samumed, Llc | 5-heteroaryl substituted indazole-3-carboxamides and preparation and use thereof |
| GEP20227437B (en) * | 2018-05-07 | 2022-11-10 | Acraf | 1h-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors |
| US11510904B2 (en) | 2018-06-05 | 2022-11-29 | Actuate Therapeutics Inc. | Methods of treating malignant lymphoproliferative disorders |
| SG11202102406XA (en) | 2018-09-13 | 2021-04-29 | Bristol Myers Squibb Co | Indazole carboxamides as kinase inhibitors |
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| WO1994010174A1 (en) | 1992-11-05 | 1994-05-11 | Smithkline Beecham Plc | Piperidine derivatives as 5-ht4 receptor antagonists |
| IT1291569B1 (it) * | 1997-04-15 | 1999-01-11 | Angelini Ricerche Spa | Indazolammidi come agenti serotoninergici |
| GB0218625D0 (en) | 2002-08-10 | 2002-09-18 | Astex Technology Ltd | Pharmaceutical compounds |
| JP2006502133A (ja) * | 2002-08-10 | 2006-01-19 | アステックス、セラピューティックス、リミテッド | サイクリン依存キナーゼ（ｃｄｋ）インヒビターとしての３−（カルボニル）１ｈ−インダゾール化合物 |
| ITMI20030287A1 (it) | 2003-02-18 | 2004-08-19 | Acraf | Indazolammidi dotate di attivita' analgesica metodo, per |
| ITMI20030972A1 (it) | 2003-05-15 | 2004-11-16 | Acraf | Indazolo dotato di attivita' analgesica, metodo per prepararlo e composizione farmaceutica che lo comprende. |
| WO2005014554A1 (en) * | 2003-08-08 | 2005-02-17 | Astex Therapeutics Limited | 1h-indazole-3-carboxamide compounds as mapkap kinase modulators |
| GB0414438D0 (en) * | 2004-06-28 | 2004-07-28 | Syngenta Participations Ag | Chemical compounds |
| AR052660A1 (es) * | 2005-01-21 | 2007-03-28 | Astex Therapeutics Ltd | Derivados de pirazol para inhibir la cdk's y gsk's |
| EP1692939A1 (en) * | 2005-02-19 | 2006-08-23 | Bayer CropScience S.A. | Pesticidal substituted piperidines |
| AU2008262038A1 (en) | 2007-06-08 | 2008-12-18 | AbbVie Deutschland GmbH & Co. KG | 5-heteroaryl substituted indazoles as kinase inhibitors |
| UA99927C2 (uk) | 2007-11-12 | 2012-10-25 | Ацьенде Кимике Риуните Анджелини Франческо А.Чи.Р.А.Ф. С.П.А. | Медикамент, який є активним при невропатичному болі |
| US8377968B2 (en) * | 2008-06-02 | 2013-02-19 | Zalicus Pharmaceuticals, Ltd. | N-piperidinyl acetamide derivatives as calcium channel blockers |
| TW201040191A (en) | 2009-03-27 | 2010-11-16 | Abbott Gmbh & Co Kg | Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors |
| US7947728B1 (en) * | 2009-11-11 | 2011-05-24 | Hoffmann-La Roche Inc. | Indole and indazole analogs as glycogen synthase activators |
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