JP2010528035A5 - - Google Patents
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- JP2010528035A5 JP2010528035A5 JP2010509512A JP2010509512A JP2010528035A5 JP 2010528035 A5 JP2010528035 A5 JP 2010528035A5 JP 2010509512 A JP2010509512 A JP 2010509512A JP 2010509512 A JP2010509512 A JP 2010509512A JP 2010528035 A5 JP2010528035 A5 JP 2010528035A5
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- JP
- Japan
- Prior art keywords
- optionally substituted
- pain
- independently
- compound
- heteroaryl
- 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.)
- Pending
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- 150000001875 compounds Chemical class 0.000 claims description 86
- -1 —OH Chemical group 0.000 claims description 82
- 208000002193 Pain Diseases 0.000 claims description 69
- 125000001931 aliphatic group Chemical group 0.000 claims description 44
- 229910052739 hydrogen Inorganic materials 0.000 claims description 44
- 239000001257 hydrogen Substances 0.000 claims description 44
- 125000005843 halogen group Chemical group 0.000 claims description 34
- 125000001072 heteroaryl group Chemical group 0.000 claims description 33
- 150000002431 hydrogen Chemical class 0.000 claims description 23
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 18
- 230000001154 acute effect Effects 0.000 claims description 18
- 229910052757 nitrogen Inorganic materials 0.000 claims description 14
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 14
- 125000003107 substituted aryl group Chemical group 0.000 claims description 14
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 12
- 125000003545 alkoxy group Chemical group 0.000 claims description 12
- 125000003118 aryl group Chemical group 0.000 claims description 12
- 230000001684 chronic effect Effects 0.000 claims description 12
- 239000000203 mixture Substances 0.000 claims description 12
- 208000004296 neuralgia Diseases 0.000 claims description 12
- 125000004043 oxo group Chemical group O=* 0.000 claims description 12
- 208000008035 Back Pain Diseases 0.000 claims description 11
- 125000002723 alicyclic group Chemical group 0.000 claims description 11
- 150000003839 salts Chemical class 0.000 claims description 11
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- 208000021722 neuropathic pain Diseases 0.000 claims description 10
- 230000002981 neuropathic effect Effects 0.000 claims description 8
- 208000011580 syndromic disease Diseases 0.000 claims description 7
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- 206010028836 Neck pain Diseases 0.000 claims description 6
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- 125000002252 acyl group Chemical group 0.000 claims description 6
- 125000000217 alkyl group Chemical group 0.000 claims description 6
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 6
- 208000009935 visceral pain Diseases 0.000 claims description 6
- 208000008930 Low Back Pain Diseases 0.000 claims description 5
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims description 4
- 206010002383 Angina Pectoris Diseases 0.000 claims description 4
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- 208000004404 Intractable Pain Diseases 0.000 claims description 4
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- 125000005842 heteroatom Chemical group 0.000 claims description 4
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 4
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- 201000008482 osteoarthritis Diseases 0.000 claims description 4
- 229910052717 sulfur Inorganic materials 0.000 claims description 4
- 206010044652 trigeminal neuralgia Diseases 0.000 claims description 4
- 108010052164 Sodium Channels Proteins 0.000 claims description 3
- 102000018674 Sodium Channels Human genes 0.000 claims description 3
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- 208000004998 Abdominal Pain Diseases 0.000 claims description 2
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- 206010008120 Cerebral ischaemia Diseases 0.000 claims description 2
- 206010008479 Chest Pain Diseases 0.000 claims description 2
- 201000009273 Endometriosis Diseases 0.000 claims description 2
- 206010015150 Erythema Diseases 0.000 claims description 2
- 206010016059 Facial pain Diseases 0.000 claims description 2
- 208000001640 Fibromyalgia Diseases 0.000 claims description 2
- 206010020772 Hypertension Diseases 0.000 claims description 2
- 206010020853 Hypertonic bladder Diseases 0.000 claims description 2
- 206010021639 Incontinence Diseases 0.000 claims description 2
- 208000005615 Interstitial Cystitis Diseases 0.000 claims description 2
- 208000007914 Labor Pain Diseases 0.000 claims description 2
- 208000035945 Labour pain Diseases 0.000 claims description 2
- 208000016285 Movement disease Diseases 0.000 claims description 2
- 206010028391 Musculoskeletal Pain Diseases 0.000 claims description 2
- 208000005890 Neuroma Diseases 0.000 claims description 2
- 208000001294 Nociceptive Pain Diseases 0.000 claims description 2
- 208000009722 Overactive Urinary Bladder Diseases 0.000 claims description 2
- 206010033645 Pancreatitis Diseases 0.000 claims description 2
- 206010033647 Pancreatitis acute Diseases 0.000 claims description 2
- 208000000450 Pelvic Pain Diseases 0.000 claims description 2
- 208000010886 Peripheral nerve injury Diseases 0.000 claims description 2
- 208000004983 Phantom Limb Diseases 0.000 claims description 2
- 206010056238 Phantom pain Diseases 0.000 claims description 2
- 206010037596 Pyelonephritis Diseases 0.000 claims description 2
- 206010038419 Renal colic Diseases 0.000 claims description 2
- 206010040037 Sensory neuropathy hereditary Diseases 0.000 claims description 2
- 208000000491 Tendinopathy Diseases 0.000 claims description 2
- 206010043255 Tendonitis Diseases 0.000 claims description 2
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- 208000009205 Tinnitus Diseases 0.000 claims description 2
- 208000030886 Traumatic Brain injury Diseases 0.000 claims description 2
- 208000027418 Wounds and injury Diseases 0.000 claims description 2
- 210000001015 abdomen Anatomy 0.000 claims description 2
- 230000002159 abnormal effect Effects 0.000 claims description 2
- 201000003229 acute pancreatitis Diseases 0.000 claims description 2
- 150000007824 aliphatic compounds Chemical class 0.000 claims description 2
- 125000003342 alkenyl group Chemical group 0.000 claims description 2
- 125000005133 alkynyloxy group Chemical group 0.000 claims description 2
- 125000003368 amide group Chemical group 0.000 claims description 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 2
- 230000036506 anxiety Effects 0.000 claims description 2
- 206010003119 arrhythmia Diseases 0.000 claims description 2
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- 125000004104 aryloxy group Chemical group 0.000 claims description 2
- 125000004429 atom Chemical group 0.000 claims description 2
- 208000034757 axonal type 2FF Charcot-Marie-Tooth disease Diseases 0.000 claims description 2
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 229910052799 carbon Inorganic materials 0.000 claims description 2
- 206010008118 cerebral infarction Diseases 0.000 claims description 2
- 238000006243 chemical reaction Methods 0.000 claims description 2
- 238000002512 chemotherapy Methods 0.000 claims description 2
- 230000006378 damage Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 231100000321 erythema Toxicity 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 210000003414 extremity Anatomy 0.000 claims description 2
- 238000010304 firing Methods 0.000 claims description 2
- 230000005176 gastrointestinal motility Effects 0.000 claims description 2
- 208000037584 hereditary sensory and autonomic neuropathy Diseases 0.000 claims description 2
- 201000006847 hereditary sensory neuropathy Diseases 0.000 claims description 2
- 230000002757 inflammatory effect Effects 0.000 claims description 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 230000003340 mental effect Effects 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 125000002950 monocyclic group Chemical group 0.000 claims description 2
- 230000004770 neurodegeneration Effects 0.000 claims description 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 2
- 208000015706 neuroendocrine disease Diseases 0.000 claims description 2
- 201000001119 neuropathy Diseases 0.000 claims description 2
- 230000007823 neuropathy Effects 0.000 claims description 2
- 208000020629 overactive bladder Diseases 0.000 claims description 2
- 229910052760 oxygen Inorganic materials 0.000 claims description 2
- 210000000496 pancreas Anatomy 0.000 claims description 2
- 208000033808 peripheral neuropathy Diseases 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 208000001297 phlebitis Diseases 0.000 claims description 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 201000007094 prostatitis Diseases 0.000 claims description 2
- 238000001959 radiotherapy Methods 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 208000007056 sickle cell anemia Diseases 0.000 claims description 2
- 201000009890 sinusitis Diseases 0.000 claims description 2
- 208000020431 spinal cord injury Diseases 0.000 claims description 2
- 208000005198 spinal stenosis Diseases 0.000 claims description 2
- 208000024891 symptom Diseases 0.000 claims description 2
- 201000004415 tendinitis Diseases 0.000 claims description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 231100000886 tinnitus Toxicity 0.000 claims description 2
- 210000003371 toe Anatomy 0.000 claims description 2
- 208000004371 toothache Diseases 0.000 claims description 2
- 230000008733 trauma Effects 0.000 claims description 2
- 230000009529 traumatic brain injury Effects 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- PQNFLJBBNBOBRQ-UHFFFAOYSA-N benzocyclopentane Natural products C1=CC=C2CCCC2=C1 PQNFLJBBNBOBRQ-UHFFFAOYSA-N 0.000 claims 2
- 208000024720 Fabry Disease Diseases 0.000 claims 1
- 206010033557 Palpitations Diseases 0.000 claims 1
- 206010037779 Radiculopathy Diseases 0.000 claims 1
- 201000000182 femoral cancer Diseases 0.000 claims 1
- 210000002414 leg Anatomy 0.000 claims 1
- 230000003211 malignant effect Effects 0.000 claims 1
- 125000004957 naphthylene group Chemical group 0.000 claims 1
- 230000007863 steatosis Effects 0.000 claims 1
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 1
- 0 CC(*)(C(*=C)(*=C)I(C)*)NC Chemical compound CC(*)(C(*=C)(*=C)I(C)*)NC 0.000 description 29
- 238000000034 method Methods 0.000 description 6
- FUKPTAWOWUTIBA-UHFFFAOYSA-N CC(C(SC)=O)[n](cc1)c2c1c(F)cc(F)c2 Chemical compound CC(C(SC)=O)[n](cc1)c2c1c(F)cc(F)c2 FUKPTAWOWUTIBA-UHFFFAOYSA-N 0.000 description 1
- GDPJRYCXJJQWRN-UHFFFAOYSA-N CC(C[n](cc1)c2c1ccc(OC)c2)=O Chemical compound CC(C[n](cc1)c2c1ccc(OC)c2)=O GDPJRYCXJJQWRN-UHFFFAOYSA-N 0.000 description 1
- JCJVMJJPCWFFTR-UHFFFAOYSA-N CC(C[n]1c2cccc(F)c2cc1)=O Chemical compound CC(C[n]1c2cccc(F)c2cc1)=O JCJVMJJPCWFFTR-UHFFFAOYSA-N 0.000 description 1
- NXHFMBXQSRGPRD-UHFFFAOYSA-N Cc1c(cc[n]2CC=C)c2ccc1 Chemical compound Cc1c(cc[n]2CC=C)c2ccc1 NXHFMBXQSRGPRD-UHFFFAOYSA-N 0.000 description 1
- 108090000862 Ion Channels Proteins 0.000 description 1
- 102000004310 Ion Channels Human genes 0.000 description 1
- 208000030858 Myofascial Pain Syndromes Diseases 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 239000000664 voltage gated sodium channel blocking agent Substances 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US93172207P | 2007-05-25 | 2007-05-25 | |
| PCT/US2008/064314 WO2008147797A2 (en) | 2007-05-25 | 2008-05-21 | Ion channel modulators and methods of use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010528035A JP2010528035A (ja) | 2010-08-19 |
| JP2010528035A5 true JP2010528035A5 (enExample) | 2012-06-07 |
Family
ID=39876632
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010509512A Pending JP2010528035A (ja) | 2007-05-25 | 2008-05-21 | イオンチャネル調節物質およびその使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US8193194B2 (enExample) |
| EP (1) | EP2158183A2 (enExample) |
| JP (1) | JP2010528035A (enExample) |
| CN (1) | CN101687782A (enExample) |
| AU (1) | AU2008256937A1 (enExample) |
| CA (1) | CA2687764A1 (enExample) |
| MX (1) | MX2009012678A (enExample) |
| NZ (1) | NZ581309A (enExample) |
| WO (1) | WO2008147797A2 (enExample) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7615563B2 (en) * | 2003-08-08 | 2009-11-10 | Gonzalez Iii Jesus E | Compositions useful as inhibitors of voltage-gated sodium channels |
| WO2007030618A2 (en) * | 2005-09-09 | 2007-03-15 | Vertex Pharmaceuticals Incorporated | Bicyclic derivatives as modulators of voltage gated ion channels |
| EP1948597A1 (en) * | 2005-10-21 | 2008-07-30 | Vertex Pharmaceuticals Incorporated | Derivatives for modulation of ion channels |
| NZ581309A (en) | 2007-05-25 | 2012-02-24 | Vertex Pharma | Ion channel modulators and methods of use |
| AU2008321142A1 (en) * | 2007-11-13 | 2009-05-22 | Vertex Pharmaceuticals Incorporated | Heterocyclic derivatives as modulators of ion channels |
| AU2008321137A1 (en) | 2007-11-13 | 2009-05-22 | Vertex Pharmaceuticals Incorporated | 4(-3-(-2-(phenyl)morpholino)-2-oxopyrrolidin-1-yl)-n-(thiazol-2-yl)benzenesulfonamide derivati ves and related compounds as modulators of ion channels for the treatment of pain |
| WO2009133641A1 (ja) * | 2008-04-30 | 2009-11-05 | シャープ株式会社 | 照明装置、及び表示装置 |
| CA2812081A1 (en) * | 2010-09-13 | 2012-03-22 | Novartis Ag | Triazine-oxadiazoles |
| WO2012095781A1 (en) * | 2011-01-13 | 2012-07-19 | Pfizer Limited | Indazole derivatives as sodium channel inhibitors |
| JP6014155B2 (ja) | 2011-10-31 | 2016-10-25 | ゼノン・ファーマシューティカルズ・インコーポレイテッドＸｅｎｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃ． | ビアリールエーテルスルホンアミドおよび治療剤としてのそれらの使用 |
| ES2586213T3 (es) | 2011-10-31 | 2016-10-13 | Xenon Pharmaceuticals Inc. | Compuestos de bencenosulfonamida y su uso como agentes terapéuticos |
| BR112014029161A2 (pt) | 2012-05-22 | 2017-06-27 | Genentech Inc | benzamidas n-substituídas e seu uso no tratamento de dor |
| BR112015000187A2 (pt) | 2012-07-06 | 2017-06-27 | Genentech Inc | benzamidas substituídas com n e métodos de uso das mesmas |
| ES2857687T3 (es) | 2013-01-31 | 2021-09-29 | Vertex Pharma | Piridona amidas como moduladores de los canales de sodio |
| BR112015022488A2 (pt) | 2013-03-14 | 2017-07-18 | Genentech Inc | triazolopiridinas substituídas e métodos de uso das mesmas |
| BR112015023397A2 (pt) | 2013-03-15 | 2017-07-18 | Genentech Inc | benzoxazois substituídos e métodos de uso dos mesmos |
| CR20160296A (es) | 2013-11-27 | 2016-09-20 | Genentech Inc | Benzamidas sustituidas y métodos para usarlas |
| EP2878339A1 (en) | 2013-12-02 | 2015-06-03 | Siena Biotech S.p.A. | SIP3 antagonists |
| EP3166939B1 (en) | 2014-07-07 | 2019-06-05 | Genentech, Inc. | Therapeutic compounds and methods of use thereof |
| KR102364840B1 (ko) | 2014-11-05 | 2022-02-18 | 삼성전자주식회사 | 신경세포의 탈수초화와 연관된 질환을 치료하기 위한 약학적 조성물 및 그를 이용하는 방법 |
| WO2016191312A1 (en) | 2015-05-22 | 2016-12-01 | Genentech, Inc. | Substituted benzamides and methods of use thereof |
| US9771335B2 (en) * | 2015-07-31 | 2017-09-26 | The Johns Hopkins University | Derivatives of rufinamide and their use in inhibtion of the activation of human voltage-gated sodium channels |
| MA42683A (fr) | 2015-08-27 | 2018-07-04 | Genentech Inc | Composés thérapeutiques et leurs méthodes utilisation |
| PE20181003A1 (es) | 2015-09-28 | 2018-06-26 | Genentech Inc | Compuestos terapeuticos y sus metodos de uso |
| TW201726128A (zh) * | 2015-10-08 | 2017-08-01 | 歌林達有限公司 | 經吡唑基取代之四氫哌喃基碸 |
| TW201718557A (zh) * | 2015-10-08 | 2017-06-01 | 歌林達有限公司 | 經吡唑基取代之四氫吡喃基碸 |
| CN108495851A (zh) | 2015-11-25 | 2018-09-04 | 基因泰克公司 | 取代的苯甲酰胺及其使用方法 |
| PT3426243T (pt) | 2016-03-09 | 2021-08-19 | Raze Therapeutics Inc | Inibidores de 3-fosfoglicerato desidrogenase e utilizações dos mesmos |
| EP3426244B1 (en) | 2016-03-09 | 2023-06-07 | Raze Therapeutics, Inc. | 3-phosphoglycerate dehydrogenase inhibitors and uses thereof |
| EP3854782A1 (en) | 2016-03-30 | 2021-07-28 | Genentech, Inc. | Substituted benzamides and methods of use thereof |
| RU2638784C1 (ru) * | 2016-09-14 | 2017-12-15 | Частное учреждение образовательная организация высшего образования "Медицинский университет "Реавиз" | Способ лечения миофасциальных болей в мышцах шеи по Гурову-Левину |
| SG11201903348UA (en) | 2016-10-17 | 2019-05-30 | Genentech Inc | Therapeutic compounds and methods of use thereof |
| WO2018175707A1 (en) | 2017-03-24 | 2018-09-27 | Genentech, Inc. | 4-piperidin-n-(pyrimidin-4-yl)chroman-7-sulfonamide derivatives as sodium channel inhibitors |
| EP3759098A1 (en) | 2018-02-26 | 2021-01-06 | Genentech, Inc. | Pyridine-sulfonamide compounds and their use against pain and related conditions |
| EP3774801A1 (en) | 2018-03-30 | 2021-02-17 | F. Hoffmann-La Roche AG | Fused ring hydro-pyrido compounds as sodium channel inhibitors |
| TW202003490A (zh) | 2018-05-22 | 2020-01-16 | 瑞士商赫孚孟拉羅股份公司 | 治療性化合物及其使用方法 |
| WO2024158872A1 (en) * | 2023-01-25 | 2024-08-02 | The Rockefeller University | 1,3-indole-propanamide inhibitors of sars-cov-2 plpro/nsp3 and derivatives thereof |
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-
2008
- 2008-05-21 NZ NZ581309A patent/NZ581309A/en not_active IP Right Cessation
- 2008-05-21 US US12/124,303 patent/US8193194B2/en active Active
- 2008-05-21 EP EP08769547A patent/EP2158183A2/en not_active Withdrawn
- 2008-05-21 MX MX2009012678A patent/MX2009012678A/es not_active Application Discontinuation
- 2008-05-21 WO PCT/US2008/064314 patent/WO2008147797A2/en not_active Ceased
- 2008-05-21 CN CN200880021348A patent/CN101687782A/zh active Pending
- 2008-05-21 AU AU2008256937A patent/AU2008256937A1/en not_active Abandoned
- 2008-05-21 CA CA002687764A patent/CA2687764A1/en not_active Abandoned
- 2008-05-21 JP JP2010509512A patent/JP2010528035A/ja active Pending
-
2012
- 2012-04-27 US US13/457,855 patent/US8883766B2/en active Active
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