JP2012508726A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2012508726A5 JP2012508726A5 JP2011536026A JP2011536026A JP2012508726A5 JP 2012508726 A5 JP2012508726 A5 JP 2012508726A5 JP 2011536026 A JP2011536026 A JP 2011536026A JP 2011536026 A JP2011536026 A JP 2011536026A JP 2012508726 A5 JP2012508726 A5 JP 2012508726A5
- Authority
- JP
- Japan
- Prior art keywords
- disorder
- pain
- stereoisomers
- fluoro
- benzimidazol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
- 208000002193 Pain Diseases 0.000 claims 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 10
- 208000035475 disorder Diseases 0.000 claims 7
- 150000001204 N-oxides Chemical class 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 5
- 206010047700 Vomiting Diseases 0.000 claims 4
- 230000008673 vomiting Effects 0.000 claims 4
- 208000019901 Anxiety disease Diseases 0.000 claims 3
- 206010010904 Convulsion Diseases 0.000 claims 3
- 206010026749 Mania Diseases 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 208000010877 cognitive disease Diseases 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 125000001475 halogen functional group Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 3
- 208000024714 major depressive disease Diseases 0.000 claims 3
- 208000004296 neuralgia Diseases 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- 208000008811 Agoraphobia Diseases 0.000 claims 2
- 208000020925 Bipolar disease Diseases 0.000 claims 2
- 201000006474 Brain Ischemia Diseases 0.000 claims 2
- 206010006550 Bulimia nervosa Diseases 0.000 claims 2
- 206010008120 Cerebral ischaemia Diseases 0.000 claims 2
- 208000028698 Cognitive impairment Diseases 0.000 claims 2
- 208000019695 Migraine disease Diseases 0.000 claims 2
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims 2
- 206010008118 cerebral infarction Diseases 0.000 claims 2
- 230000027288 circadian rhythm Effects 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 206010027599 migraine Diseases 0.000 claims 2
- 208000021722 neuropathic pain Diseases 0.000 claims 2
- 208000019906 panic disease Diseases 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 201000000980 schizophrenia Diseases 0.000 claims 2
- 208000011117 substance-related disease Diseases 0.000 claims 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 2
- XPPAIETVYLUERI-UHFFFAOYSA-N 2-[1-[3-(2,4-dimethoxypyrimidin-5-yl)-4-fluorophenyl]benzimidazol-5-yl]propan-2-ol Chemical compound COC1=NC(OC)=NC=C1C1=CC(N2C3=CC=C(C=C3N=C2)C(C)(C)O)=CC=C1F XPPAIETVYLUERI-UHFFFAOYSA-N 0.000 claims 1
- DKVUQZXJVMWXQI-UHFFFAOYSA-N 2-[1-[3-(2-chloro-3-fluoropyridin-4-yl)-4-fluorophenyl]benzimidazol-5-yl]propan-2-ol Chemical compound C1=NC2=CC(C(C)(O)C)=CC=C2N1C(C=1)=CC=C(F)C=1C1=CC=NC(Cl)=C1F DKVUQZXJVMWXQI-UHFFFAOYSA-N 0.000 claims 1
- TVDBMVXZWKOECA-UHFFFAOYSA-N 2-[1-[3-(2-chloropyridin-3-yl)-4-fluorophenyl]benzimidazol-5-yl]propan-2-ol Chemical compound C1=NC2=CC(C(C)(O)C)=CC=C2N1C(C=1)=CC=C(F)C=1C1=CC=CN=C1Cl TVDBMVXZWKOECA-UHFFFAOYSA-N 0.000 claims 1
- BCJUNMJDGDTVKE-UHFFFAOYSA-N 2-[1-[3-(3-chloropyridin-4-yl)-4-fluorophenyl]benzimidazol-5-yl]propan-2-ol Chemical compound C1=NC2=CC(C(C)(O)C)=CC=C2N1C(C=1)=CC=C(F)C=1C1=CC=NC=C1Cl BCJUNMJDGDTVKE-UHFFFAOYSA-N 0.000 claims 1
- PDMUJHXKKUKMGY-UHFFFAOYSA-N 2-[1-[4-fluoro-3-(2-fluoropyridin-3-yl)phenyl]benzimidazol-5-yl]propan-2-ol Chemical compound C1=NC2=CC(C(C)(O)C)=CC=C2N1C(C=1)=CC=C(F)C=1C1=CC=CN=C1F PDMUJHXKKUKMGY-UHFFFAOYSA-N 0.000 claims 1
- OZASCMUSVHNLGI-UHFFFAOYSA-N 2-[1-[4-fluoro-3-(2-methoxypyridin-3-yl)phenyl]benzimidazol-5-yl]propan-2-ol Chemical compound COC1=NC=CC=C1C1=CC(N2C3=CC=C(C=C3N=C2)C(C)(C)O)=CC=C1F OZASCMUSVHNLGI-UHFFFAOYSA-N 0.000 claims 1
- HDNARMOIXLHSDI-UHFFFAOYSA-N 2-[1-[4-fluoro-3-(3-fluoropyridin-4-yl)phenyl]benzimidazol-5-yl]propan-2-ol Chemical compound C1=NC2=CC(C(C)(O)C)=CC=C2N1C(C=1)=CC=C(F)C=1C1=CC=NC=C1F HDNARMOIXLHSDI-UHFFFAOYSA-N 0.000 claims 1
- WKWWUCDURKSXSF-UHFFFAOYSA-N 4-[2-fluoro-5-[5-(2-hydroxypropan-2-yl)benzimidazol-1-yl]phenyl]pyridine-3-carbonitrile Chemical compound C1=NC2=CC(C(C)(O)C)=CC=C2N1C(C=1)=CC=C(F)C=1C1=CC=NC=C1C#N WKWWUCDURKSXSF-UHFFFAOYSA-N 0.000 claims 1
- CEVRKJINHDZMMD-UHFFFAOYSA-N 5-[2-fluoro-5-[5-(2-hydroxypropan-2-yl)benzimidazol-1-yl]phenyl]pyridine-3-carbonitrile Chemical compound C1=NC2=CC(C(C)(O)C)=CC=C2N1C(C=1)=CC=C(F)C=1C1=CN=CC(C#N)=C1 CEVRKJINHDZMMD-UHFFFAOYSA-N 0.000 claims 1
- 206010001497 Agitation Diseases 0.000 claims 1
- 201000004384 Alopecia Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000000103 Anorexia Nervosa Diseases 0.000 claims 1
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 208000019888 Circadian rhythm sleep disease Diseases 0.000 claims 1
- 208000020406 Creutzfeldt Jacob disease Diseases 0.000 claims 1
- 208000003407 Creutzfeldt-Jakob Syndrome Diseases 0.000 claims 1
- 208000010859 Creutzfeldt-Jakob disease Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 208000020401 Depressive disease Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- 208000030814 Eating disease Diseases 0.000 claims 1
- 208000002091 Febrile Seizures Diseases 0.000 claims 1
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 1
- 208000001640 Fibromyalgia Diseases 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- 206010019196 Head injury Diseases 0.000 claims 1
- 206010019233 Headaches Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000001456 Jet Lag Syndrome Diseases 0.000 claims 1
- 208000020358 Learning disease Diseases 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 208000026139 Memory disease Diseases 0.000 claims 1
- 208000019022 Mood disease Diseases 0.000 claims 1
- 208000007101 Muscle Cramp Diseases 0.000 claims 1
- 208000008238 Muscle Spasticity Diseases 0.000 claims 1
- 208000012905 Myotonic disease Diseases 0.000 claims 1
- 206010029216 Nervousness Diseases 0.000 claims 1
- 206010029333 Neurosis Diseases 0.000 claims 1
- 208000001294 Nociceptive Pain Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010033892 Paraplegia Diseases 0.000 claims 1
- 208000018737 Parkinson disease 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
- 206010034912 Phobia Diseases 0.000 claims 1
- 208000000609 Pick Disease of the Brain Diseases 0.000 claims 1
- 206010036376 Postherpetic Neuralgia Diseases 0.000 claims 1
- 208000031649 Postoperative Nausea and Vomiting Diseases 0.000 claims 1
- 208000004550 Postoperative Pain Diseases 0.000 claims 1
- 206010036618 Premenstrual syndrome Diseases 0.000 claims 1
- 206010066962 Procedural nausea Diseases 0.000 claims 1
- 208000028017 Psychotic disease Diseases 0.000 claims 1
- 208000000810 Separation Anxiety Diseases 0.000 claims 1
- 206010041250 Social phobia Diseases 0.000 claims 1
- 208000005392 Spasm Diseases 0.000 claims 1
- 208000013200 Stress disease Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000003028 Stuttering Diseases 0.000 claims 1
- 206010043269 Tension headache Diseases 0.000 claims 1
- 208000008548 Tension-Type Headache Diseases 0.000 claims 1
- 208000009205 Tinnitus Diseases 0.000 claims 1
- 208000031674 Traumatic Acute Stress disease Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 208000021017 Weight Gain Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 208000026345 acute stress disease Diseases 0.000 claims 1
- 208000029650 alcohol withdrawal Diseases 0.000 claims 1
- 201000002426 animal phobia Diseases 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 230000036461 convulsion Effects 0.000 claims 1
- 230000006735 deficit Effects 0.000 claims 1
- 230000003111 delayed effect Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 235000014632 disordered eating Nutrition 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 208000024732 dysthymic disease Diseases 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 125000004785 fluoromethoxy group Chemical group [H]C([H])(F)O* 0.000 claims 1
- 229960003692 gamma aminobutyric acid Drugs 0.000 claims 1
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 claims 1
- 208000024963 hair loss Diseases 0.000 claims 1
- 230000003676 hair loss Effects 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 1
- 201000008980 hyperinsulinism Diseases 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 208000033915 jet lag type circadian rhythm sleep disease Diseases 0.000 claims 1
- 201000003723 learning disability Diseases 0.000 claims 1
- 206010027175 memory impairment Diseases 0.000 claims 1
- 230000036651 mood Effects 0.000 claims 1
- 201000003152 motion sickness Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015238 neurotic disease Diseases 0.000 claims 1
- 230000003040 nociceptive effect Effects 0.000 claims 1
- 235000016709 nutrition Nutrition 0.000 claims 1
- 230000035764 nutrition Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 208000019899 phobic disease Diseases 0.000 claims 1
- 208000028173 post-traumatic stress disease Diseases 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 230000005855 radiation Effects 0.000 claims 1
- 230000000306 recurrent effect Effects 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 208000025874 separation anxiety disease Diseases 0.000 claims 1
- 208000019116 sleep disease Diseases 0.000 claims 1
- 208000020685 sleep-wake disease Diseases 0.000 claims 1
- 208000018198 spasticity Diseases 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 201000009032 substance abuse Diseases 0.000 claims 1
- 231100000736 substance abuse Toxicity 0.000 claims 1
- 201000006152 substance dependence Diseases 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 230000000153 supplemental effect Effects 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 208000016686 tic disease Diseases 0.000 claims 1
- 231100000886 tinnitus Toxicity 0.000 claims 1
- 206010044652 trigeminal neuralgia Diseases 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 230000009278 visceral effect Effects 0.000 claims 1
- 230000004584 weight gain Effects 0.000 claims 1
- 235000019786 weight gain Nutrition 0.000 claims 1
- 0 Cc(cnc(*)n1)c1I Chemical compound Cc(cnc(*)n1)c1I 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11496008P | 2008-11-14 | 2008-11-14 | |
| DKPA200801584 | 2008-11-14 | ||
| US61/114,960 | 2008-11-14 | ||
| DKPA200801584 | 2008-11-14 | ||
| PCT/EP2009/065121 WO2010055128A1 (en) | 2008-11-14 | 2009-11-13 | Benzimidazole derivatives and their use for modulating the gabaa receptor complex |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012508726A JP2012508726A (ja) | 2012-04-12 |
| JP2012508726A5 true JP2012508726A5 (https=) | 2012-12-27 |
Family
ID=41563731
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011536026A Abandoned JP2012508726A (ja) | 2008-11-14 | 2009-11-13 | ベンゾイミダゾール誘導体及びｇａｂａａレセプター複合体を調節するためのそれらの使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20110257210A1 (https=) |
| EP (1) | EP2358701A1 (https=) |
| JP (1) | JP2012508726A (https=) |
| CN (1) | CN102388035A (https=) |
| AR (1) | AR074342A1 (https=) |
| CA (1) | CA2743531A1 (https=) |
| MX (1) | MX2011004736A (https=) |
| TW (1) | TW201029989A (https=) |
| WO (1) | WO2010055128A1 (https=) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8519134B2 (en) | 2009-11-17 | 2013-08-27 | Novartis Ag | Aryl-pyridine derivatives as aldosterone synthase inhibitors |
| CN114807015B (zh) * | 2022-05-20 | 2022-11-22 | 呈诺再生医学科技(北京)有限公司 | 一种促进胰岛α细胞转化为β细胞的诱导方法及其应用 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6900215B2 (en) * | 2000-12-15 | 2005-05-31 | Merck Sharp & Dohme Ltd. | Imidazo-pyrimidine derivatives as ligands for gaba receptors |
| TWI391381B (zh) * | 2006-03-24 | 2013-04-01 | Neurosearch As | 新穎的苯并咪唑衍生物、含有其之醫藥組成物、及其於製造藥物之用途 |
-
2009
- 2009-11-05 TW TW098137558A patent/TW201029989A/zh unknown
- 2009-11-13 MX MX2011004736A patent/MX2011004736A/es not_active Application Discontinuation
- 2009-11-13 EP EP09756151A patent/EP2358701A1/en not_active Withdrawn
- 2009-11-13 CN CN2009801454691A patent/CN102388035A/zh active Pending
- 2009-11-13 AR ARP090104401A patent/AR074342A1/es unknown
- 2009-11-13 CA CA2743531A patent/CA2743531A1/en not_active Abandoned
- 2009-11-13 US US13/129,186 patent/US20110257210A1/en not_active Abandoned
- 2009-11-13 WO PCT/EP2009/065121 patent/WO2010055128A1/en not_active Ceased
- 2009-11-13 JP JP2011536026A patent/JP2012508726A/ja not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2009530353A5 (https=) | ||
| JP2008524262A5 (https=) | ||
| JP2009538867A5 (https=) | ||
| WO2007085556A3 (en) | Use of 4-imidazole derivatives for cns disorders | |
| JP2009519995A5 (https=) | ||
| JP2011116780A5 (https=) | ||
| MX347239B (es) | Derivados de pirazol. | |
| MX2012007409A (es) | Derivados de benzamida sustituidos. | |
| NO20091480L (no) | Aminometyl-2-imidazoler med affinitet mot sporamin-assosierte reseptorer | |
| CA2543710A1 (en) | Novel norepinephrine reuptake inhibitors for the treatment of central nervous system disorders | |
| JP2009530237A (ja) | キナゾリノン及びカリウムチャネル活性化剤としてのその使用 | |
| MX2009013742A (es) | 2-imidazolinas. | |
| JP2010507664A (ja) | ベンズイミダゾール化合物 | |
| JP2013544277A5 (https=) | ||
| MX361761B (es) | Derivados de triazol carboxamida. | |
| JP2012508726A5 (https=) | ||
| JP2008526815A5 (https=) | ||
| JP2009537599A5 (https=) | ||
| JP2012508727A5 (https=) | ||
| MX2009005920A (es) | Nuevos 2-imidazoles como ligandos para receptores asociados con trazas de amina. | |
| JP2007530635A5 (https=) | ||
| JP2009518338A (ja) | バニロイドアンタゴニストとしての三置換キナゾリノン誘導体 | |
| MX2009006215A (es) | 4-imidazolinas como ligandos de aminas trazas. | |
| JP2005530814A5 (https=) | ||
| JP2009511547A5 (https=) |