HRP20160732T1 - Enantiomeri spirooksindolskih spojeva i njihova upotreba kao terapijska sredstva - Google Patents
Enantiomeri spirooksindolskih spojeva i njihova upotreba kao terapijska sredstva Download PDFInfo
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- HRP20160732T1 HRP20160732T1 HRP20160732TT HRP20160732T HRP20160732T1 HR P20160732 T1 HRP20160732 T1 HR P20160732T1 HR P20160732T T HRP20160732T T HR P20160732TT HR P20160732 T HRP20160732 T HR P20160732T HR P20160732 T1 HRP20160732 T1 HR P20160732T1
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- pain
- pharmaceutically acceptable
- acceptable solvate
- diseases
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- 239000003814 drug Substances 0.000 title claims 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 title 1
- 229940124597 therapeutic agent Drugs 0.000 title 1
- 208000002193 Pain Diseases 0.000 claims 10
- 201000010099 disease Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- 241000124008 Mammalia Species 0.000 claims 5
- 102000016913 Voltage-Gated Sodium Channels Human genes 0.000 claims 3
- 108010053752 Voltage-Gated Sodium Channels Proteins 0.000 claims 3
- 206010010904 Convulsion Diseases 0.000 claims 2
- 208000003251 Pruritus Diseases 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 201000011384 erythromelalgia Diseases 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 150000002500 ions Chemical class 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 208000033808 peripheral neuropathy Diseases 0.000 claims 2
- NEBUOXBYNAHKFV-UHFFFAOYSA-N 1'-[[5-(trifluoromethyl)furan-2-yl]methyl]spiro[6h-furo[2,3-f][1,3]benzodioxole-7,3'-indole]-2'-one Chemical compound O1C(C(F)(F)F)=CC=C1CN1C2=CC=CC=C2C2(C3=CC=4OCOC=4C=C3OC2)C1=O NEBUOXBYNAHKFV-UHFFFAOYSA-N 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 206010003658 Atrial Fibrillation Diseases 0.000 claims 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 206010058019 Cancer Pain Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 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
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 208000001640 Fibromyalgia Diseases 0.000 claims 1
- 206010019233 Headaches Diseases 0.000 claims 1
- 101000620451 Homo sapiens Leucine-rich glioma-inactivated protein 1 Proteins 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 206010020844 Hyperthermia malignant Diseases 0.000 claims 1
- 206010065390 Inflammatory pain Diseases 0.000 claims 1
- 208000007914 Labor Pain Diseases 0.000 claims 1
- 208000035945 Labour pain Diseases 0.000 claims 1
- 102100022275 Leucine-rich glioma-inactivated protein 1 Human genes 0.000 claims 1
- 208000026709 Liddle syndrome Diseases 0.000 claims 1
- 208000018717 Malignant hyperthermia of anesthesia Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 206010061533 Myotonia Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000000693 Neurogenic Urinary Bladder Diseases 0.000 claims 1
- 206010029279 Neurogenic bladder Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 208000012075 Paroxysmal dystonia Diseases 0.000 claims 1
- 208000010886 Peripheral nerve injury Diseases 0.000 claims 1
- 208000004983 Phantom Limb Diseases 0.000 claims 1
- 206010056238 Phantom pain Diseases 0.000 claims 1
- 206010036376 Postherpetic Neuralgia Diseases 0.000 claims 1
- 208000037674 Primary erythromelalgia Diseases 0.000 claims 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 1
- 206010037113 Pseudoaldosteronism Diseases 0.000 claims 1
- 208000005793 Restless legs syndrome Diseases 0.000 claims 1
- 206010039020 Rhabdomyolysis Diseases 0.000 claims 1
- 206010040744 Sinus headache Diseases 0.000 claims 1
- 108010052164 Sodium Channels Proteins 0.000 claims 1
- 102000018674 Sodium Channels Human genes 0.000 claims 1
- 208000027520 Somatoform disease Diseases 0.000 claims 1
- 208000001871 Tachycardia Diseases 0.000 claims 1
- 206010057040 Temperature intolerance Diseases 0.000 claims 1
- 206010043269 Tension headache Diseases 0.000 claims 1
- 208000008548 Tension-Type Headache Diseases 0.000 claims 1
- 206010043994 Tonic convulsion Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis 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
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- 201000011510 cancer Diseases 0.000 claims 1
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- 208000010118 dystonia Diseases 0.000 claims 1
- 230000001667 episodic effect Effects 0.000 claims 1
- 230000008543 heat sensitivity Effects 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 201000007004 malignant hyperthermia Diseases 0.000 claims 1
- 210000004962 mammalian cell Anatomy 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 230000001537 neural effect Effects 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 230000004112 neuroprotection Effects 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 208000027753 pain disease Diseases 0.000 claims 1
- 230000001314 paroxysmal effect Effects 0.000 claims 1
- 208000019865 paroxysmal extreme pain disease Diseases 0.000 claims 1
- 230000002085 persistent effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 208000017692 primary erythermalgia Diseases 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
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- 208000011580 syndromic disease Diseases 0.000 claims 1
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- 239000003053 toxin Substances 0.000 claims 1
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- 230000000472 traumatic effect Effects 0.000 claims 1
- 206010044652 trigeminal neuralgia Diseases 0.000 claims 1
- 208000003663 ventricular fibrillation Diseases 0.000 claims 1
- 208000009935 visceral pain Diseases 0.000 claims 1
- 230000003313 weakening effect Effects 0.000 claims 1
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- C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
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Claims (9)
1. (S)-Enantiomer 1′-{[5-(trifluormetil)furan-2-il]metil}spiro[furo[2,3-f][1,3]benzodioksol-7,3′-indol]-2′(1′H)-ona, naznačen time što ima sljedeću formulu (I-S):
[image]
ili njegov farmaceutski prihvatljiv solvat.
2. Farmaceutski pripravak, naznačen time što sadrži farmaceutski prihvatljivu pomoćnu tvar i (S)-enantiomer u skladu s patentnim zahtjevom 1, ili njegov farmaceutski prihvatljiv solvat.
3. (S)-Enantiomer u skladu s patentnim zahtjevom 1, ili njegov farmaceutski prihvatljiv solvat, naznačen time što je namijenjen upotrebi u liječenju bolesti ili stanja kod sisavca koje se bira iz skupine koju čine bol, depresija, kardiovaskularnane bolesti, respiratorne bolesti, psihijatrijske bolesti, neurološke bolesti i napadaji, te njihove kombinacije.
4. Spojevi namijenjeni upotrebi u skladu s patentnim zahtjevom 3, naznačeni time što se navedena bolest ili stanje bira iz skupine koju čine neuropatska bol, upalna bol, visceralna bol, bol uzrokovana rakom, zubobolja, bol uzrokovana kemoterapijom, traumatska bol, bol uzrokovana kirurškim zahvatom, porođajna bol, neurogeni mokraćni mjehur, ulcerozni kolitis, kronična bol, trajna bol, periferno posredovana bol, centralno posredovana bol, kronična glavobolja, migrenska glavobolja, sinusna glavobolja, tenzijska glavobolja, bol u fantomskom udu, ozljeda perifernog živca, te njihove kombinacije.
5. Spojevi namijenjeni upotrebi u skladu s patentnim zahtjevom 3, naznačeni time što se navedena bolest ili stanje bira iz skupine koju čine bol povezana s HIV-om, neuropatija uzrokovana liječenjem HIV-a, trigeminalna neuralgija, postherpetična neuralgija, eudinija, osjetljivost na toplinu, sarkoidoza, sindrom iritabilnih crijeva, Crohnova bolest, bol povezana s multiplom sklerozom, amiotrofna lateralna skleroza, svrbež, hiperkolesterolemija, dobroćudna hiperplazija prostate, dijabetična neuropatija, periferna neuropatija, artritis, reumatoidni artritis, osteoartritis, paroksizmalna distonija, mijetenični sindromi, miotonija, zloćudna hipertermija, cistična fibroza, pseudoaldosteronizam, rabdomioliza, bipolarna depresija, anksioznost, shizofrenija, bolesti povezane s toksinima za natrijske kanale, obiteljska eritermalgija, primarna eritromelalgija, porodična rektalna bol, poremećaj paroksizmalne epizodne boli, rak, epilepsija, djelomični i opći tonični napadaji, sindrom nemirnih nogu, aritmije, fibromialgija, neuroprotekcija kod ishemijskih stanja uzrokovanih inzultom ili neuralnom traumom, tahiaritmije, atrijska fibrilacija i ventrikularna fibrilacija.
6. (S)-Enantiomer u skladu s patentnim zahtjevom 1, ili njegov farmaceutski prihvatljiv solvat, naznačen time što je namijenjen upotrebi u liječenju bolesti ili stanja kod sisavca inhibiranjem struje iona kroz naponski natrijski kanal kod sisavca.
7. (S)-Enantiomer u skladu s patentnim zahtjevom 1, ili njegov farmaceutski prihvatljiv solvat, naznačen time što je namijenjen upotrebi u slabljenju struje iona kroz naponski natrijski kanal u stanici kod sisavca.
8. Upotreba (S)-enantiomera u skladu s patentnim zahtjevom 1 u pripravi medikamenta za liječenje bolesti ili stanja koja se ublažuju ili olakšavaju inhibiranjem naponskog natrijskog kanala kod sisavca.
9. (S)-Enantiomer u skladu s patentnim zahtjevom 1, ili njegov farmaceutski prihvatljiv solvat, naznačen time što je namijenjen upotrebi u liječenju svrbeža kod sisavca.
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| PCT/US2010/040187 WO2011002708A1 (en) | 2009-06-29 | 2010-06-28 | Enantiomers of spiro-oxindole compounds and their uses as therapeutic agents |
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