JP2011503112A5 - - Google Patents
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- JP2011503112A5 JP2011503112A5 JP2010533335A JP2010533335A JP2011503112A5 JP 2011503112 A5 JP2011503112 A5 JP 2011503112A5 JP 2010533335 A JP2010533335 A JP 2010533335A JP 2010533335 A JP2010533335 A JP 2010533335A JP 2011503112 A5 JP2011503112 A5 JP 2011503112A5
- Authority
- JP
- Japan
- Prior art keywords
- pain
- aliphatic
- compound according
- compound
- acute
- 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.)
- Withdrawn
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- 208000002193 Pain Diseases 0.000 claims description 59
- 150000001875 compounds Chemical class 0.000 claims description 57
- 125000001931 aliphatic group Chemical group 0.000 claims description 44
- 125000001475 halogen functional group Chemical group 0.000 claims description 20
- 229910052739 hydrogen Inorganic materials 0.000 claims description 20
- 230000001154 acute effect Effects 0.000 claims description 17
- 208000004296 neuralgia Diseases 0.000 claims description 15
- 239000001257 hydrogen Substances 0.000 claims description 14
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 14
- 230000001684 chronic effect Effects 0.000 claims description 11
- 208000021722 neuropathic pain Diseases 0.000 claims description 9
- 208000019695 Migraine disease Diseases 0.000 claims description 7
- 208000004550 Postoperative Pain Diseases 0.000 claims description 7
- 206010027599 migraine Diseases 0.000 claims description 7
- 201000006417 multiple sclerosis Diseases 0.000 claims description 7
- 230000002981 neuropathic effect Effects 0.000 claims description 7
- 208000008930 Low Back Pain Diseases 0.000 claims description 6
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical group C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims description 6
- 125000003118 aryl group Chemical group 0.000 claims description 6
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- 208000011580 syndromic disease Diseases 0.000 claims description 6
- 150000004867 thiadiazoles Chemical group 0.000 claims description 6
- 208000006561 Cluster Headache Diseases 0.000 claims description 5
- 206010019233 Headaches Diseases 0.000 claims description 5
- 206010028836 Neck pain Diseases 0.000 claims description 5
- 206010036376 Postherpetic Neuralgia Diseases 0.000 claims description 5
- 208000005298 acute pain Diseases 0.000 claims description 5
- 208000018912 cluster headache syndrome Diseases 0.000 claims description 5
- 208000002551 irritable bowel syndrome Diseases 0.000 claims description 5
- 239000000203 mixture Substances 0.000 claims description 5
- 206010044652 trigeminal neuralgia Diseases 0.000 claims description 5
- 208000009935 visceral pain Diseases 0.000 claims description 5
- 206010002383 Angina Pectoris Diseases 0.000 claims description 4
- 208000005615 Interstitial Cystitis Diseases 0.000 claims description 4
- 208000007914 Labor Pain Diseases 0.000 claims description 4
- 208000035945 Labour pain Diseases 0.000 claims description 4
- 208000006011 Stroke Diseases 0.000 claims description 4
- 208000014674 injury Diseases 0.000 claims description 4
- 201000001119 neuropathy Diseases 0.000 claims description 4
- 230000007823 neuropathy Effects 0.000 claims description 4
- 201000008482 osteoarthritis Diseases 0.000 claims description 4
- 208000033808 peripheral neuropathy Diseases 0.000 claims description 4
- 208000019901 Anxiety disease Diseases 0.000 claims description 3
- 206010003591 Ataxia Diseases 0.000 claims description 3
- 208000008035 Back Pain Diseases 0.000 claims description 3
- 208000000003 Breakthrough pain Diseases 0.000 claims description 3
- 206010058019 Cancer Pain Diseases 0.000 claims description 3
- 208000000094 Chronic Pain Diseases 0.000 claims description 3
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims description 3
- 206010021639 Incontinence Diseases 0.000 claims description 3
- 206010065390 Inflammatory pain Diseases 0.000 claims description 3
- 208000004404 Intractable Pain Diseases 0.000 claims description 3
- 206010026749 Mania Diseases 0.000 claims description 3
- 208000016285 Movement disease Diseases 0.000 claims description 3
- 208000001294 Nociceptive Pain Diseases 0.000 claims description 3
- 208000008765 Sciatica Diseases 0.000 claims description 3
- 230000036506 anxiety Effects 0.000 claims description 3
- 206010003119 arrhythmia Diseases 0.000 claims description 3
- 230000006793 arrhythmia Effects 0.000 claims description 3
- 206010003246 arthritis Diseases 0.000 claims description 3
- 206010015037 epilepsy Diseases 0.000 claims description 3
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 3
- 208000015706 neuroendocrine disease Diseases 0.000 claims description 3
- 208000020016 psychiatric disease Diseases 0.000 claims description 3
- 206010000599 Acromegaly Diseases 0.000 claims description 2
- 208000006820 Arthralgia Diseases 0.000 claims description 2
- 208000020925 Bipolar disease Diseases 0.000 claims description 2
- 206010005063 Bladder pain Diseases 0.000 claims description 2
- 206010006002 Bone pain Diseases 0.000 claims description 2
- 201000006474 Brain Ischemia Diseases 0.000 claims description 2
- 206010064012 Central pain syndrome Diseases 0.000 claims description 2
- 206010008120 Cerebral ischaemia Diseases 0.000 claims description 2
- 206010008479 Chest Pain Diseases 0.000 claims description 2
- 208000024720 Fabry Disease Diseases 0.000 claims description 2
- 206010016059 Facial pain Diseases 0.000 claims description 2
- 208000001640 Fibromyalgia Diseases 0.000 claims description 2
- 206010019909 Hernia Diseases 0.000 claims description 2
- 208000007514 Herpes zoster Diseases 0.000 claims description 2
- 206010020772 Hypertension Diseases 0.000 claims description 2
- 206010061218 Inflammation Diseases 0.000 claims description 2
- 206010024229 Leprosy Diseases 0.000 claims description 2
- 206010028289 Muscle atrophy Diseases 0.000 claims description 2
- 206010028391 Musculoskeletal Pain Diseases 0.000 claims description 2
- 208000030858 Myofascial Pain Syndromes Diseases 0.000 claims description 2
- 208000005890 Neuroma Diseases 0.000 claims description 2
- 206010033425 Pain in extremity Diseases 0.000 claims description 2
- 206010033557 Palpitations 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
- 206010037779 Radiculopathy 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
- 206010043269 Tension headache Diseases 0.000 claims description 2
- 208000008548 Tension-Type Headache Diseases 0.000 claims description 2
- 208000030886 Traumatic Brain injury Diseases 0.000 claims description 2
- 206010046543 Urinary incontinence 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
- 208000034757 axonal type 2FF Charcot-Marie-Tooth disease Diseases 0.000 claims description 2
- 206010008118 cerebral infarction Diseases 0.000 claims description 2
- 230000006378 damage Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 210000004696 endometrium Anatomy 0.000 claims description 2
- 230000005176 gastrointestinal motility Effects 0.000 claims description 2
- 231100000869 headache Toxicity 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
- 230000004054 inflammatory process Effects 0.000 claims description 2
- 208000003243 intestinal obstruction Diseases 0.000 claims description 2
- 201000010901 lateral sclerosis Diseases 0.000 claims description 2
- 208000005264 motor neuron disease Diseases 0.000 claims description 2
- 230000020763 muscle atrophy Effects 0.000 claims description 2
- 201000000585 muscular atrophy Diseases 0.000 claims description 2
- 210000000496 pancreas Anatomy 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 208000001297 phlebitis Diseases 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
- 210000000278 spinal cord Anatomy 0.000 claims description 2
- 208000020431 spinal cord injury Diseases 0.000 claims description 2
- 208000005198 spinal stenosis Diseases 0.000 claims description 2
- 230000007863 steatosis Effects 0.000 claims description 2
- 231100000240 steatosis hepatitis Toxicity 0.000 claims description 2
- 208000024891 symptom Diseases 0.000 claims description 2
- 201000004415 tendinitis Diseases 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
- 208000026533 urinary bladder disease Diseases 0.000 claims description 2
- 208000014001 urinary system disease Diseases 0.000 claims description 2
- 238000000034 method Methods 0.000 description 3
- VZWOXDYRBDIHMA-UHFFFAOYSA-N Cc1ncc[s]1 Chemical compound Cc1ncc[s]1 VZWOXDYRBDIHMA-UHFFFAOYSA-N 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- HGSMSUKMTHXJCL-UHFFFAOYSA-N CC(C)Cc1cnc[s]1 Chemical compound CC(C)Cc1cnc[s]1 HGSMSUKMTHXJCL-UHFFFAOYSA-N 0.000 description 1
- UEYSZHNQBHWVAE-UHFFFAOYSA-N CCC(C)C1=CCCC=NS1 Chemical compound CCC(C)C1=CCCC=NS1 UEYSZHNQBHWVAE-UHFFFAOYSA-N 0.000 description 1
- QMHIMXFNBOYPND-UHFFFAOYSA-N Cc1c[s]cn1 Chemical compound Cc1c[s]cn1 QMHIMXFNBOYPND-UHFFFAOYSA-N 0.000 description 1
- QLXOJLUHWBDVKZ-UHFFFAOYSA-N Cc1ncn[s]1 Chemical compound Cc1ncn[s]1 QLXOJLUHWBDVKZ-UHFFFAOYSA-N 0.000 description 1
- RQSCFNPNNLWQBJ-UHFFFAOYSA-N Cc1nnc[s]1 Chemical compound Cc1nnc[s]1 RQSCFNPNNLWQBJ-UHFFFAOYSA-N 0.000 description 1
- XQFRJNBWHJMXHO-RRKCRQDMSA-N IDUR Chemical compound C1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C(I)=C1 XQFRJNBWHJMXHO-RRKCRQDMSA-N 0.000 description 1
- 241000283080 Proboscidea <mammal> Species 0.000 description 1
- 206010059604 Radicular pain Diseases 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 230000003349 osteoarthritic effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US98748507P | 2007-11-13 | 2007-11-13 | |
| US8814108P | 2008-08-12 | 2008-08-12 | |
| PCT/US2008/083165 WO2009064747A2 (en) | 2007-11-13 | 2008-11-12 | 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011503112A JP2011503112A (ja) | 2011-01-27 |
| JP2011503112A5 true JP2011503112A5 (https=) | 2012-12-13 |
Family
ID=40380263
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010533335A Withdrawn JP2011503112A (ja) | 2007-11-13 | 2008-11-12 | 疼痛の処置のためのイオンチャンネルのモジュレーターとしての４（−３−（−２−（フェニル）モルホリノ）−２−オキソピロリジン−１−イル）−ｎ−（チアゾール−２−イル）ベンゼンスルホンアミド誘導体および関連化合物 |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US7994166B2 (https=) |
| EP (1) | EP2231655B1 (https=) |
| JP (1) | JP2011503112A (https=) |
| KR (1) | KR20100098396A (https=) |
| CN (1) | CN102036985A (https=) |
| AT (1) | ATE522526T1 (https=) |
| AU (1) | AU2008321137A1 (https=) |
| CA (1) | CA2705336A1 (https=) |
| IL (1) | IL205697A0 (https=) |
| MX (1) | MX2010005309A (https=) |
| NZ (1) | NZ585332A (https=) |
| RU (1) | RU2010123781A (https=) |
| WO (1) | WO2009064747A2 (https=) |
Families Citing this family (16)
| 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 |
| ATE527251T1 (de) * | 2005-05-16 | 2011-10-15 | Vertex Pharma | Bicyclische derivate als modulatoren von ionenkanälen |
| MX2008003337A (es) * | 2005-09-09 | 2008-09-26 | Vertex Pharma | Derivados biciclicos como modulares de canales ionicos regulados por voltaje. |
| EP1948597A1 (en) * | 2005-10-21 | 2008-07-30 | Vertex Pharmaceuticals Incorporated | Derivatives for modulation of ion channels |
| AU2008256937A1 (en) | 2007-05-25 | 2008-12-04 | Vertex Pharmaceuticals Incorporated | Ion channel modulators and methods of use |
| US7994174B2 (en) * | 2007-09-19 | 2011-08-09 | Vertex Pharmaceuticals Incorporated | Pyridyl sulfonamides as modulators of ion channels |
| EP2231655B1 (en) | 2007-11-13 | 2011-08-31 | Vertex Pharmaceuticals Incorporated | 4(-3-(-2-(phenyl)morpholino)-2-oxopyrrolidin-1-yl)-n-(thiazol-2-yl)benzenesulfonamide derivatives and related compounds as modulators of ion channels for the treatment of pain |
| CN101910166A (zh) * | 2007-11-13 | 2010-12-08 | 沃泰克斯药物股份有限公司 | 用作钠离子通道调节剂的杂环衍生物 |
| RU2011103451A (ru) * | 2008-07-01 | 2012-08-10 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Гетероциклические производные в качестве модуляторов ионных каналов |
| JP6215230B2 (ja) * | 2012-01-16 | 2017-10-18 | バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | イオンチャネルのモジュレーターとしてのピラン−スピロ環式ピペリジンアミド |
| JP2015536914A (ja) | 2012-10-12 | 2015-12-24 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | 置換フェニルカルバメート化合物 |
| EP2909170A1 (en) | 2012-10-16 | 2015-08-26 | F. Hoffmann-La Roche AG | Substituted carbamate compounds and their use as transient receptor potential (trp) channel antagonists |
| US9187506B2 (en) * | 2014-01-09 | 2015-11-17 | Bristol-Myers Squibb Company | (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one and its prodrugs for the treatment of psychiatric disorders |
| WO2018093694A1 (en) * | 2016-11-17 | 2018-05-24 | Merck Sharp & Dohme Corp. | Diamino-alkylamino-linked arylsulfonamide compounds with selective activity in voltage-gated sodium channels |
| CN115745910B (zh) | 2017-07-21 | 2025-05-27 | 安塔比奥公司 | 化学化合物 |
| CN113008999B (zh) * | 2019-12-19 | 2024-08-23 | 重庆药友制药有限责任公司 | 一种分离测定氟比洛芬酯中2种基因毒性杂质的方法 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5304121A (en) | 1990-12-28 | 1994-04-19 | Boston Scientific Corporation | Drug delivery system making use of a hydrogel polymer coating |
| US5886026A (en) | 1993-07-19 | 1999-03-23 | Angiotech Pharmaceuticals Inc. | Anti-angiogenic compositions and methods of use |
| US6099562A (en) | 1996-06-13 | 2000-08-08 | Schneider (Usa) Inc. | Drug coating with topcoat |
| WO2004103980A1 (en) * | 2003-05-21 | 2004-12-02 | Biovitrum Ab | Inhibitors of 11-beta-hydroxy steroid dehydrogenase type i |
| US7615563B2 (en) * | 2003-08-08 | 2009-11-10 | Gonzalez Iii Jesus E | Compositions useful as inhibitors of voltage-gated sodium channels |
| US8202861B2 (en) | 2003-08-08 | 2012-06-19 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of voltage-gated sodium channels |
| JP2007261945A (ja) * | 2004-04-07 | 2007-10-11 | Taisho Pharmaceut Co Ltd | チアゾール誘導体 |
| KR20080015102A (ko) * | 2005-05-10 | 2008-02-18 | 버텍스 파마슈티칼스 인코포레이티드 | 이온 채널 조절인자로서의 바이사이클릭 유도체 |
| ATE527251T1 (de) | 2005-05-16 | 2011-10-15 | Vertex Pharma | Bicyclische derivate als modulatoren von ionenkanälen |
| WO2006127329A1 (en) | 2005-05-20 | 2006-11-30 | Vertex Pharmaceuticals Incorporated | Quinoline derivatives useful as modulators of ion channels |
| MX2007015726A (es) * | 2005-06-09 | 2008-03-04 | Vertex Pharma | Derivados de indano como moduladores de canales ionicos. |
| MX2008003337A (es) * | 2005-09-09 | 2008-09-26 | Vertex Pharma | Derivados biciclicos como modulares de canales ionicos regulados por voltaje. |
| RU2008118350A (ru) * | 2005-10-12 | 2009-11-20 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Бифенильные производные в качестве модуляторов потенциалзависимых ионных каналов |
| EP1948597A1 (en) * | 2005-10-21 | 2008-07-30 | Vertex Pharmaceuticals Incorporated | Derivatives for modulation of ion channels |
| NZ593074A (en) | 2005-12-21 | 2012-04-27 | Vertex Pharma | sulfonamide-pyrrolidone derivatives as Modulators of Ion Channels |
| WO2007075896A2 (en) * | 2005-12-22 | 2007-07-05 | Kemia, Inc. | Heterocyclic cytokine inhibitors |
| AU2008256937A1 (en) | 2007-05-25 | 2008-12-04 | Vertex Pharmaceuticals Incorporated | Ion channel modulators and methods of use |
| US7994174B2 (en) * | 2007-09-19 | 2011-08-09 | Vertex Pharmaceuticals Incorporated | Pyridyl sulfonamides as modulators of ion channels |
| EP2231655B1 (en) | 2007-11-13 | 2011-08-31 | Vertex Pharmaceuticals Incorporated | 4(-3-(-2-(phenyl)morpholino)-2-oxopyrrolidin-1-yl)-n-(thiazol-2-yl)benzenesulfonamide derivatives and related compounds as modulators of ion channels for the treatment of pain |
| CN101910166A (zh) * | 2007-11-13 | 2010-12-08 | 沃泰克斯药物股份有限公司 | 用作钠离子通道调节剂的杂环衍生物 |
| RU2011103451A (ru) | 2008-07-01 | 2012-08-10 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Гетероциклические производные в качестве модуляторов ионных каналов |
-
2008
- 2008-11-12 EP EP08850039A patent/EP2231655B1/en not_active Not-in-force
- 2008-11-12 US US12/269,108 patent/US7994166B2/en not_active Expired - Fee Related
- 2008-11-12 RU RU2010123781/04A patent/RU2010123781A/ru not_active Application Discontinuation
- 2008-11-12 MX MX2010005309A patent/MX2010005309A/es active IP Right Grant
- 2008-11-12 CN CN2008801225096A patent/CN102036985A/zh active Pending
- 2008-11-12 AT AT08850039T patent/ATE522526T1/de active
- 2008-11-12 WO PCT/US2008/083165 patent/WO2009064747A2/en not_active Ceased
- 2008-11-12 CA CA2705336A patent/CA2705336A1/en not_active Abandoned
- 2008-11-12 NZ NZ585332A patent/NZ585332A/en not_active IP Right Cessation
- 2008-11-12 AU AU2008321137A patent/AU2008321137A1/en not_active Abandoned
- 2008-11-12 KR KR1020107012968A patent/KR20100098396A/ko not_active Withdrawn
- 2008-11-12 JP JP2010533335A patent/JP2011503112A/ja not_active Withdrawn
-
2010
- 2010-05-11 IL IL205697A patent/IL205697A0/en unknown
-
2011
- 2011-07-08 US US13/178,877 patent/US20120010416A1/en not_active Abandoned
-
2013
- 2013-08-15 US US13/967,732 patent/US8841282B2/en active Active
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