JP2016532716A5 - - Google Patents
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- Publication number
- JP2016532716A5 JP2016532716A5 JP2016540921A JP2016540921A JP2016532716A5 JP 2016532716 A5 JP2016532716 A5 JP 2016532716A5 JP 2016540921 A JP2016540921 A JP 2016540921A JP 2016540921 A JP2016540921 A JP 2016540921A JP 2016532716 A5 JP2016532716 A5 JP 2016532716A5
- Authority
- JP
- Japan
- Prior art keywords
- chloro
- propyl
- phenoxy
- fluoro
- phenyl
- 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.)
- Granted
Links
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 42
- 150000001875 compounds Chemical class 0.000 claims 22
- 208000002193 Pain Diseases 0.000 claims 19
- 150000003839 salts Chemical class 0.000 claims 18
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 12
- -1 3- (5-chloro-2- (2-chloro-5-fluoro-4- (N- (thiazol-2-yl) sulfamoyl) phenoxy) phenyl) propyl Chemical group 0.000 claims 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 10
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 9
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 9
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims 6
- DUWWHGPELOTTOE-UHFFFAOYSA-N n-(5-chloro-2,4-dimethoxyphenyl)-3-oxobutanamide Chemical compound COC1=CC(OC)=C(NC(=O)CC(C)=O)C=C1Cl DUWWHGPELOTTOE-UHFFFAOYSA-N 0.000 claims 6
- 235000019260 propionic acid Nutrition 0.000 claims 6
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 5
- KJIOILLRHLJKQM-UHFFFAOYSA-N CCCN(CCCc1cc(Cl)ccc1Oc1cc(F)c(cc1Cl)S(=O)(=O)Nc1nccs1)CC(O)=O Chemical compound CCCN(CCCc1cc(Cl)ccc1Oc1cc(F)c(cc1Cl)S(=O)(=O)Nc1nccs1)CC(O)=O KJIOILLRHLJKQM-UHFFFAOYSA-N 0.000 claims 4
- 208000004296 neuralgia Diseases 0.000 claims 4
- 230000002265 prevention Effects 0.000 claims 4
- 208000001294 Nociceptive Pain Diseases 0.000 claims 3
- KTMCKUSSWVWNTC-UHFFFAOYSA-N OC(=O)CCN(CCCc1cc(Cl)ccc1Oc1cc(F)c(cc1Cl)S(=O)(=O)Nc1nccs1)CC#C Chemical compound OC(=O)CCN(CCCc1cc(Cl)ccc1Oc1cc(F)c(cc1Cl)S(=O)(=O)Nc1nccs1)CC#C KTMCKUSSWVWNTC-UHFFFAOYSA-N 0.000 claims 3
- 208000003251 Pruritus Diseases 0.000 claims 3
- 208000021722 neuropathic pain Diseases 0.000 claims 3
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 2
- CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 claims 2
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 2
- WSFSSNUMVMOOMR-UHFFFAOYSA-N Formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 claims 2
- 201000001947 Reflex Sympathetic Dystrophy Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 201000001119 neuropathy Diseases 0.000 claims 2
- 230000007823 neuropathy Effects 0.000 claims 2
- 230000003040 nociceptive effect Effects 0.000 claims 2
- 208000033808 peripheral neuropathy Diseases 0.000 claims 2
- 230000011514 reflex Effects 0.000 claims 2
- 206010003694 Atrophy Diseases 0.000 claims 1
- 206010003840 Autonomic nervous system imbalance Diseases 0.000 claims 1
- 206010058019 Cancer Pain Diseases 0.000 claims 1
- 208000001387 Causalgia Diseases 0.000 claims 1
- 206010008334 Cervicobrachial syndrome Diseases 0.000 claims 1
- 108091006146 Channels Proteins 0.000 claims 1
- 208000009043 Chemical Burns Diseases 0.000 claims 1
- 206010008874 Chronic Fatigue Syndrome Diseases 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 208000034656 Contusions Diseases 0.000 claims 1
- 206010010904 Convulsion Diseases 0.000 claims 1
- 208000001640 Fibromyalgia Diseases 0.000 claims 1
- 206010018429 Glucose tolerance impaired Diseases 0.000 claims 1
- 206010019233 Headaches Diseases 0.000 claims 1
- 208000004454 Hyperalgesia Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010065390 Inflammatory pain Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 208000005890 Neuroma 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
- 208000004550 Postoperative Pain Diseases 0.000 claims 1
- 208000001280 Prediabetic State Diseases 0.000 claims 1
- 208000003782 Raynaud disease Diseases 0.000 claims 1
- 208000012322 Raynaud phenomenon Diseases 0.000 claims 1
- 208000000491 Tendinopathy Diseases 0.000 claims 1
- 206010043255 Tendonitis Diseases 0.000 claims 1
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 1
- 102000016913 Voltage-Gated Sodium Channels Human genes 0.000 claims 1
- 108010053752 Voltage-Gated Sodium Channels Proteins 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 206010053552 allodynia Diseases 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 238000003556 assay Methods 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 230000037444 atrophy Effects 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 230000036760 body temperature Effects 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 230000003247 decreasing effect Effects 0.000 claims 1
- 230000001419 dependent effect Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000000835 fiber Substances 0.000 claims 1
- 231100000869 headache Toxicity 0.000 claims 1
- 230000000642 iatrogenic effect Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 230000007803 itching Effects 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 208000029766 myalgic encephalomeyelitis/chronic fatigue syndrome Diseases 0.000 claims 1
- 210000005036 nerve Anatomy 0.000 claims 1
- 230000002981 neuropathic effect Effects 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 208000005877 painful neuropathy Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 230000035945 sensitivity Effects 0.000 claims 1
- 208000020431 spinal cord injury Diseases 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 230000002889 sympathetic effect Effects 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 201000004415 tendinitis Diseases 0.000 claims 1
- 125000000437 thiazol-2-yl group Chemical group [H]C1=C([H])N=C(*)S1 0.000 claims 1
- 125000004495 thiazol-4-yl group Chemical group S1C=NC(=C1)* 0.000 claims 1
- 230000000699 topical effect Effects 0.000 claims 1
- 230000008733 trauma Effects 0.000 claims 1
- 206010044652 trigeminal neuralgia Diseases 0.000 claims 1
- 208000009935 visceral pain Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361876046P | 2013-09-10 | 2013-09-10 | |
| US61/876,046 | 2013-09-10 | ||
| PCT/US2014/054764 WO2015038533A2 (en) | 2013-09-10 | 2014-09-09 | Sodium channel modulators for the treatment of pain and diabetes |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016532716A JP2016532716A (ja) | 2016-10-20 |
| JP2016532716A5 true JP2016532716A5 (enExample) | 2017-10-19 |
| JP6445565B2 JP6445565B2 (ja) | 2018-12-26 |
Family
ID=52666496
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016540921A Active JP6445565B2 (ja) | 2013-09-10 | 2014-09-09 | とう痛及び糖尿病の治療用ナトリウムチャネル調節物質 |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US20160221974A1 (enExample) |
| EP (1) | EP3043787B1 (enExample) |
| JP (1) | JP6445565B2 (enExample) |
| KR (1) | KR20160054570A (enExample) |
| CN (1) | CN105611923B (enExample) |
| AU (1) | AU2014318979B2 (enExample) |
| BR (1) | BR112016005271A2 (enExample) |
| CA (1) | CA2922851C (enExample) |
| ES (1) | ES2687598T3 (enExample) |
| IL (1) | IL244506B (enExample) |
| MX (1) | MX2016002881A (enExample) |
| MY (1) | MY181928A (enExample) |
| PH (1) | PH12016500296A1 (enExample) |
| RU (1) | RU2016113156A (enExample) |
| SG (2) | SG10201805552PA (enExample) |
| UA (1) | UA120353C2 (enExample) |
| WO (1) | WO2015038533A2 (enExample) |
| ZA (1) | ZA201702410B (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112015022096A8 (pt) * | 2013-03-15 | 2019-11-26 | Chromocell Corp | compostos moduladores de canal de sódio, composição que os compreende e uso dos mesmos |
| CN105611923B (zh) | 2013-09-10 | 2019-08-23 | 卓莫赛尔公司 | 用于治疗疼痛和糖尿病的钠通道调节剂 |
| WO2016040315A1 (en) * | 2014-09-09 | 2016-03-17 | Chromocell Corporation | Selective nav1.7 inhibitors for the treatment of diabetes |
| TW201726637A (zh) | 2015-12-18 | 2017-08-01 | 默沙東藥廠 | 對電位閘控鈉通道具選擇活性之羥基烷基胺－及羥基環烷基胺－取代之二胺－芳基磺胺化合物 |
| KR102366077B1 (ko) | 2016-05-20 | 2022-02-21 | 제논 파마슈티칼스 인크. | 벤젠술폰아미드 화합물 및 치료제로서의 그의 용도 |
| CN105924670A (zh) * | 2016-06-02 | 2016-09-07 | 扬州兰都塑料科技有限公司 | 一种电力电缆用耐磨剂 |
| CN105924843A (zh) * | 2016-06-02 | 2016-09-07 | 扬州兰都塑料科技有限公司 | 一种耐刮擦的电力电缆 |
| CN106084535A (zh) * | 2016-06-02 | 2016-11-09 | 扬州兰都塑料科技有限公司 | 一种耐刮擦的电力电缆的制备方法 |
| KR20190086772A (ko) | 2016-12-09 | 2019-07-23 | 제논 파마슈티칼스 인크. | 벤젠술폰아미드 화합물 및 치료제로서의 그의 용도 |
| CN106892845B (zh) * | 2017-02-28 | 2018-10-30 | 四川同晟生物医药有限公司 | 一种2,4-二氨基丁酸衍生物及其制备方法 |
| WO2019200369A1 (en) * | 2018-04-13 | 2019-10-17 | Chromocell Corporation | Compounds and methods of using compounds for the prevention or treatment of peripheral nerve damage |
| WO2019217822A1 (en) * | 2018-05-11 | 2019-11-14 | Chromocell Corporation | Compounds and methods of using compounds for the prevention or treatment of inflammatory conditions |
| BR112020024729A2 (pt) | 2018-06-13 | 2021-03-23 | Xenon Pharmaceuticals, Inc. | compostos de benzenossulfonamida e seu uso como agentes terapêuticos |
| CA3104913A1 (en) | 2018-08-31 | 2020-03-05 | Xenon Pharmaceuticals Inc. | Heteroaryl-substituted sulfonamide compounds and their use as sodium channel inhibitors |
| IL279810B2 (en) | 2018-08-31 | 2025-03-01 | Xenon Pharmaceuticals Inc | Heteroaryl-modified sulfonamide compounds and their use as medicinal agents |
| CN113527281B (zh) * | 2020-04-20 | 2023-12-22 | 昆山彭济凯丰生物科技有限公司 | 杂环化合物及其制备方法和应用 |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5356897A (en) | 1991-09-09 | 1994-10-18 | Fujisawa Pharmaceutical Co., Ltd. | 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines |
| ATE404568T1 (de) * | 2001-03-14 | 2008-08-15 | Gruenenthal Gmbh | Substituierte thiazolopyrimidine als analgetika |
| US7659082B2 (en) | 2002-02-19 | 2010-02-09 | Xenon Pharmaceuticals Inc. | Methods for identifying analgesic agents |
| AU2003243921B2 (en) | 2002-06-27 | 2009-05-07 | Novo Nordisk A/S | Aryl carbonyl derivatives as therapeutic agents |
| GB0324792D0 (en) | 2003-10-23 | 2003-11-26 | Sterix Ltd | Compound |
| WO2005054202A1 (en) | 2003-11-25 | 2005-06-16 | Eli Lilly And Company | 7-phenyl-isoquinoline-5-sulfonylamino derivatives as inhibitors of akt (proteinkinase b) |
| AU2005245386B2 (en) | 2004-05-07 | 2008-11-27 | Amgen Inc. | Nitrogenated heterocyclic derivatives as protein kinase modulators and use for the treatment of angiogenesis and cancer |
| AP2007003887A0 (en) * | 2004-07-23 | 2007-02-28 | Pfizer | Pyridine derivatives |
| CA2584413A1 (en) | 2004-10-29 | 2006-05-04 | Astrazeneca Ab | Novel sulphonamide derivatives as glucocorticoid receptor modulators for the treatment of inflammatory diseases |
| DK1966130T3 (da) * | 2005-12-23 | 2014-02-10 | Zealand Pharma As | Modificerede lysin-mimetiske forbindelser |
| JP2010518026A (ja) * | 2007-02-05 | 2010-05-27 | 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 | ナトリウムチャネルが介在する疾患または状態の治療に有用なピリドピリミジノン化合物 |
| CA2694748A1 (en) | 2007-07-13 | 2009-01-22 | Icagen, Inc. | Sodium channel inhibitors |
| EP2173743A2 (en) | 2007-07-13 | 2010-04-14 | Icagen, Inc. | Sodium channel inhibitors |
| HUE025013T2 (hu) * | 2009-01-12 | 2016-04-28 | Pfizer Ltd | Szulfonamid-származékok |
| CN105254557A (zh) | 2009-05-29 | 2016-01-20 | 拉夸里亚创药株式会社 | 作为钙或钠通道阻滞剂的芳基取代羧酰胺衍生物 |
| JP2013525368A (ja) | 2010-04-23 | 2013-06-20 | キネタ・インコーポレイテツド | 抗ウイルス性化合物 |
| JP5872552B2 (ja) | 2010-07-09 | 2016-03-01 | ファイザー・リミテッドＰｆｉｚｅｒ Ｌｉｍｉｔｅｄ | 化学化合物 |
| JP5860045B2 (ja) | 2010-07-09 | 2016-02-16 | ファイザー・リミテッドＰｆｉｚｅｒ Ｌｉｍｉｔｅｄ | 化合物 |
| CA2804593C (en) * | 2010-07-09 | 2015-11-24 | Pfizer Limited | Biphenyloxybenzensulphonamide derivatives useful as sodium channel inhibitors |
| WO2012007883A1 (en) | 2010-07-12 | 2012-01-19 | Pfizer Limited | Sulfonamide derivatives as nav1.7 inhibitors for the treatment of pain |
| JP2014507136A (ja) | 2011-01-18 | 2014-03-27 | アムジエン・インコーポレーテツド | ＮａＶ１．７ノックアウトマウスとそれらの使用 |
| TWI622583B (zh) * | 2011-07-01 | 2018-05-01 | 基利科學股份有限公司 | 作為離子通道調節劑之稠合雜環化合物 |
| AU2012296529A1 (en) | 2011-08-17 | 2014-02-20 | Amgen Inc. | Heteroaryl sodium channel inhibitors |
| AU2012312266A1 (en) | 2011-09-21 | 2013-05-02 | Gilead Sciences, Inc. | Sodium channel blockers reduce glucagon secretion |
| 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 |
| EP2919770A4 (en) | 2012-11-14 | 2017-03-08 | The Board of Regents of The University of Texas System | Inhibition of hif-2 heterodimerization with hif1 (arnt) |
| BR112015022096A8 (pt) * | 2013-03-15 | 2019-11-26 | Chromocell Corp | compostos moduladores de canal de sódio, composição que os compreende e uso dos mesmos |
| SG11201601616SA (en) | 2013-09-09 | 2016-04-28 | Peloton Therapeutics Inc | Aryl ethers and uses thereof |
| CN105611923B (zh) | 2013-09-10 | 2019-08-23 | 卓莫赛尔公司 | 用于治疗疼痛和糖尿病的钠通道调节剂 |
| WO2016040315A1 (en) | 2014-09-09 | 2016-03-17 | Chromocell Corporation | Selective nav1.7 inhibitors for the treatment of diabetes |
-
2014
- 2014-09-09 CN CN201480049690.8A patent/CN105611923B/zh not_active Expired - Fee Related
- 2014-09-09 UA UAA201603676A patent/UA120353C2/uk unknown
- 2014-09-09 KR KR1020167009294A patent/KR20160054570A/ko not_active Ceased
- 2014-09-09 SG SG10201805552PA patent/SG10201805552PA/en unknown
- 2014-09-09 RU RU2016113156A patent/RU2016113156A/ru not_active Application Discontinuation
- 2014-09-09 SG SG11201601367QA patent/SG11201601367QA/en unknown
- 2014-09-09 EP EP14843353.5A patent/EP3043787B1/en active Active
- 2014-09-09 MY MYPI2016700824A patent/MY181928A/en unknown
- 2014-09-09 US US15/021,153 patent/US20160221974A1/en not_active Abandoned
- 2014-09-09 CA CA2922851A patent/CA2922851C/en active Active
- 2014-09-09 JP JP2016540921A patent/JP6445565B2/ja active Active
- 2014-09-09 BR BR112016005271-4A patent/BR112016005271A2/pt not_active IP Right Cessation
- 2014-09-09 ES ES14843353.5T patent/ES2687598T3/es active Active
- 2014-09-09 WO PCT/US2014/054764 patent/WO2015038533A2/en not_active Ceased
- 2014-09-09 AU AU2014318979A patent/AU2014318979B2/en not_active Ceased
- 2014-09-09 MX MX2016002881A patent/MX2016002881A/es active IP Right Grant
-
2016
- 2016-01-13 US US14/994,846 patent/US9458118B2/en active Active
- 2016-02-12 PH PH12016500296A patent/PH12016500296A1/en unknown
- 2016-03-09 IL IL244506A patent/IL244506B/en active IP Right Grant
-
2017
- 2017-04-05 ZA ZA2017/02410A patent/ZA201702410B/en unknown
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