RU2012102896A - Энантиомеры спиро-оксиндольных соединений и их применение в качестве терапевтических средств - Google Patents
Энантиомеры спиро-оксиндольных соединений и их применение в качестве терапевтических средств Download PDFInfo
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- RU2012102896A RU2012102896A RU2012102896/04A RU2012102896A RU2012102896A RU 2012102896 A RU2012102896 A RU 2012102896A RU 2012102896/04 A RU2012102896/04 A RU 2012102896/04A RU 2012102896 A RU2012102896 A RU 2012102896A RU 2012102896 A RU2012102896 A RU 2012102896A
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- pain
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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 compound C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 title 1
- 230000001225 therapeutic effect Effects 0.000 title 1
- 208000002193 Pain Diseases 0.000 claims abstract 21
- 238000000034 method Methods 0.000 claims abstract 11
- 201000010099 disease Diseases 0.000 claims abstract 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 9
- 241000124008 Mammalia Species 0.000 claims abstract 8
- 239000000651 prodrug Substances 0.000 claims abstract 8
- 229940002612 prodrug Drugs 0.000 claims abstract 8
- 239000012453 solvate Substances 0.000 claims abstract 8
- 206010019233 Headaches Diseases 0.000 claims abstract 4
- 208000014674 injury Diseases 0.000 claims abstract 4
- 230000001404 mediated effect Effects 0.000 claims abstract 4
- 230000008733 trauma Effects 0.000 claims abstract 4
- 208000033808 peripheral neuropathy Diseases 0.000 claims abstract 3
- 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 abstract 2
- 206010058019 Cancer Pain Diseases 0.000 claims abstract 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims abstract 2
- 208000000094 Chronic Pain Diseases 0.000 claims abstract 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims abstract 2
- 206010010904 Convulsion Diseases 0.000 claims abstract 2
- 206010065390 Inflammatory pain Diseases 0.000 claims abstract 2
- 208000019695 Migraine disease Diseases 0.000 claims abstract 2
- 208000012902 Nervous system disease Diseases 0.000 claims abstract 2
- 208000000693 Neurogenic Urinary Bladder Diseases 0.000 claims abstract 2
- 206010029279 Neurogenic bladder Diseases 0.000 claims abstract 2
- 208000025966 Neurological disease Diseases 0.000 claims abstract 2
- 208000004983 Phantom Limb Diseases 0.000 claims abstract 2
- 206010056238 Phantom pain Diseases 0.000 claims abstract 2
- 206010040744 Sinus headache Diseases 0.000 claims abstract 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims abstract 2
- 238000002512 chemotherapy Methods 0.000 claims abstract 2
- 230000036461 convulsion Effects 0.000 claims abstract 2
- 231100000869 headache Toxicity 0.000 claims abstract 2
- 206010027599 migraine Diseases 0.000 claims abstract 2
- 208000004296 neuralgia Diseases 0.000 claims abstract 2
- 208000021722 neuropathic pain Diseases 0.000 claims abstract 2
- 201000001119 neuropathy Diseases 0.000 claims abstract 2
- 230000007823 neuropathy Effects 0.000 claims abstract 2
- 230000002085 persistent effect Effects 0.000 claims abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract 2
- 208000020016 psychiatric disease Diseases 0.000 claims abstract 2
- 208000023504 respiratory system disease Diseases 0.000 claims abstract 2
- 238000001356 surgical procedure Methods 0.000 claims abstract 2
- 208000004371 toothache Diseases 0.000 claims abstract 2
- 206010044652 trigeminal neuralgia Diseases 0.000 claims abstract 2
- 208000009935 visceral pain Diseases 0.000 claims abstract 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 3
- 229910052708 sodium Inorganic materials 0.000 claims 3
- 239000011734 sodium Substances 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 150000002500 ions Chemical class 0.000 claims 2
- 208000019901 Anxiety disease Diseases 0.000 claims 1
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- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 1
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- 108091006146 Channels Proteins 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
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- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
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- 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
- 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
- 206010028424 Myasthenic syndrome Diseases 0.000 claims 1
- 206010061533 Myotonia Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000012075 Paroxysmal dystonia Diseases 0.000 claims 1
- 208000010886 Peripheral nerve injury Diseases 0.000 claims 1
- 206010036376 Postherpetic Neuralgia Diseases 0.000 claims 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 1
- 208000003251 Pruritus Diseases 0.000 claims 1
- 206010037113 Pseudoaldosteronism Diseases 0.000 claims 1
- 208000005793 Restless legs syndrome 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
- 206010043994 Tonic convulsion Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
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- 206010003119 arrhythmia Diseases 0.000 claims 1
- 230000006793 arrhythmia Effects 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
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- 201000011510 cancer Diseases 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
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- 239000003053 toxin Substances 0.000 claims 1
- 231100000765 toxin Toxicity 0.000 claims 1
- 208000003663 ventricular fibrillation Diseases 0.000 claims 1
- 230000035606 childbirth Effects 0.000 abstract 1
- 210000000578 peripheral nerve Anatomy 0.000 abstract 1
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Abstract
1. (S)-энантиомер 1'-{[5-(трифторметил)фуран-2-ил]метил}спиро[фуро[2,3-f][1,3]бензодиоксол-7,3'-индол]-2'(1'H)-она, имеющий следующую формулу(I-S):или его фармацевтически приемлемый сольват или пролекарство.2. Фармацевтическая композиция, включающая фармацевтически приемлемый эксципиент и (S)-энантиомер по п.1 или его фармацевтически приемлемый сольват или пролекарство.3. Способ лечения заболевания или состояния у млекопитающего, выбранного из группы, включающей боль, депрессию, сердечно-сосудистые заболевания, респираторные заболевания, психические заболевания, неврологические заболевания и судороги, и их сочетания, где указанный способ включает введение млекопитающему, нуждающемуся в этом, терапевтически эффективного количества (S)-энантиомера по п.1, или его фармацевтически приемлемого сольвата или пролекарства.4. Способ по п.3, где указанное заболевание или состояние выбрано из группы, включающей невропатическую боль, воспалительную боль, висцеральную боль, раковую боль, зубную боль, боль, вызванную химиотерапией, боль, вызванную травмой, боль, вызванную хирургическим вмешательством, боль при родах, нейрогенный мочевой пузырь, язвенный колит, хроническую боль, персистентную боль, периферически-опосредованную боль, центрально-опосредованную боль, хроническую головную боль, мигреневую головную боль, синусовую головную боль, тензионную головную боль, фантомную боль в ампутированных конечностях, травму периферического нерва и их сочетания.5. Способ по п.3, где указанное заболевание или состояние выбрано из группы, включающей боль, связанную с ВИЧ, лечением ВИЧ-индуцированной невропатии, невралгию тройничного нерва, постгерп
Claims (8)
1. (S)-энантиомер 1'-{[5-(трифторметил)фуран-2-ил]метил}спиро[фуро[2,3-f][1,3]бензодиоксол-7,3'-индол]-2'(1'H)-она, имеющий следующую формулу(I-S):
или его фармацевтически приемлемый сольват или пролекарство.
2. Фармацевтическая композиция, включающая фармацевтически приемлемый эксципиент и (S)-энантиомер по п.1 или его фармацевтически приемлемый сольват или пролекарство.
3. Способ лечения заболевания или состояния у млекопитающего, выбранного из группы, включающей боль, депрессию, сердечно-сосудистые заболевания, респираторные заболевания, психические заболевания, неврологические заболевания и судороги, и их сочетания, где указанный способ включает введение млекопитающему, нуждающемуся в этом, терапевтически эффективного количества (S)-энантиомера по п.1, или его фармацевтически приемлемого сольвата или пролекарства.
4. Способ по п.3, где указанное заболевание или состояние выбрано из группы, включающей невропатическую боль, воспалительную боль, висцеральную боль, раковую боль, зубную боль, боль, вызванную химиотерапией, боль, вызванную травмой, боль, вызванную хирургическим вмешательством, боль при родах, нейрогенный мочевой пузырь, язвенный колит, хроническую боль, персистентную боль, периферически-опосредованную боль, центрально-опосредованную боль, хроническую головную боль, мигреневую головную боль, синусовую головную боль, тензионную головную боль, фантомную боль в ампутированных конечностях, травму периферического нерва и их сочетания.
5. Способ по п.3, где указанное заболевание или состояние выбрано из группы, включающей боль, связанную с ВИЧ, лечением ВИЧ-индуцированной невропатии, невралгию тройничного нерва, постгерпетическую невралгию, эвдинию, чувствительность к теплу, саркоидоз, синдром раздраженной толстой кишки, болезнь Крона, боль, связанную с рассеянным склерозом, боковым амиотрофическим склерозом, зуд, гиперхолестеринемию, доброкачественную гиперплазию предстательной железы, диабетическую невропатию, периферическую невропатию, артрит, ревматоидный артрит, остеоартрит, пароксизмальную дистонию, миастенические синдромы, миотонию, злокачественную гипертермию, кистозный фиброз, псевдоальдостеронизм, острый некроз скелетных мышц, биполярную депрессию, тревогу, шизофрению, заболевания, связанные с токсином натриевых каналов, наследственную эритермалгию, первичную эритромелалгию, наследственную ректальную боль, пароксизмальное эпизодическое болевое расстройство, рак, эпилепсию, парциальные и общие тонические судороги, синдром беспокойных ног, аритмию, фибромиалгию, нейропротекцию при ишемических состояниях, вызванных инсультом или неврологической травмой, тахиаритмию, мерцательную аритмию и фибрилляцию желудочков.
6. Способ лечения заболевания или состояния у млекопитающего путем ингибирования ионного потока через потенциалзависимый воротный натриевый канал у млекопитающего, где указанный способ включает введение млекопитающему, нуждающемуся в этом, терапевтически эффективного количества (S)-энантиомера по п.1 или его фармацевтически приемлемого сольвата или пролекарства.
7. Способ уменьшения ионного потока через потенциалзависимый воротный натриевый канал в клетке у млекопитающего, включающий контактирование клетки с (S)-энантиомером по п.1 или его фармацевтически приемлемым сольватом или пролекарством.
8. Применение (S)-энантиомера по п.1 для получения лекарственного средства для лечения заболевания или состояния, которое можно улучшить или облегчить путем ингибирования потенциалзависимого воротного натриевого канала у млекопитающего.
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