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 (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10179781B2 (en) * | 2013-03-15 | 2019-01-15 | Chromocell Corporation | Sodium channel modulators for the treatment of pain |
| 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 |
| EP3193610A4 (en) * | 2014-09-09 | 2018-04-04 | Chromocell Corporation | Selective nav1.7 inhibitors for the treatment of diabetes |
| CN108699015A (zh) | 2015-12-18 | 2018-10-23 | 默沙东公司 | 对电压门控性钠通道具有选择性活性的羟基烷基胺-和羟基环烷基胺-取代的二胺-芳基磺胺化合物 |
| WO2017201468A1 (en) | 2016-05-20 | 2017-11-23 | Xenon Pharmaceuticals Inc. | Benzenesulfonamide compounds and their use as therapeutic agents |
| 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 |
| EP3551626B1 (en) | 2016-12-09 | 2023-10-25 | Xenon Pharmaceuticals Inc. | Benzenesulfonamide compounds and their use as therapeutic agents |
| 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 |
| AU2019285184B2 (en) | 2018-06-13 | 2023-11-16 | Xenon Pharmaceuticals Inc. | Benzenesulfonamide compounds and their use as therapeutic agents |
| MA53488A (fr) | 2018-08-31 | 2021-12-08 | Xenon Pharmaceuticals Inc | Composés de sulfonamide substitués par hétéroaryle et leur utilisation en tant qu'inhibiteurs de canaux sodiques |
| US10981905B2 (en) | 2018-08-31 | 2021-04-20 | Xenon Pharmaceuticals Inc. | Heteroaryl-substituted sulfonamide compounds and their use as therapeutic 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 |
| WO2026090267A1 (en) * | 2024-10-23 | 2026-04-30 | Pelthos Therapeutics Inc. | Ophthalmic formulations |
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 |
| PT1368355E (pt) * | 2001-03-14 | 2006-09-29 | Gruenenthal Gmbh | Pirazolopirimidinas e tiazolopirimidinas substituidas, como analgesicos |
| US7659082B2 (en) | 2002-02-19 | 2010-02-09 | Xenon Pharmaceuticals Inc. | Methods for identifying analgesic agents |
| CA2744893A1 (en) | 2002-06-27 | 2004-01-08 | Novo Nordisk A/S | Aryl carbonyl derivatives as glucokinase activators |
| GB0324792D0 (en) | 2003-10-23 | 2003-11-26 | Sterix Ltd | Compound |
| EP1689719A1 (en) | 2003-11-25 | 2006-08-16 | Eli Lilly And Company | 7-phenyl-isoquinoline-5-sulfonylamino derivatives as inhibitors of akt (proteinkinase b) |
| EP1751136B1 (en) | 2004-05-07 | 2014-07-02 | Amgen Inc. | Nitrogenated heterocyclic derivatives as protein kinase modulators and use for the treatment of angiogenesis and cancer |
| WO2006011050A2 (en) * | 2004-07-23 | 2006-02-02 | Pfizer Limited | Pyridine derivatives |
| WO2006046916A1 (en) | 2004-10-29 | 2006-05-04 | Astrazeneca Ab | Novel sulphonamide derivatives as glucocorticoid receptor modulators for the treatment of inflammatory diseases |
| US7622496B2 (en) * | 2005-12-23 | 2009-11-24 | Zealand Pharma A/S | Modified lysine-mimetic compounds |
| CA2677493A1 (en) * | 2007-02-05 | 2008-08-14 | Xenon Pharmaceuticals Inc. | Pyridopyrimidinone compounds useful in treating sodium channel-mediated diseases or conditions |
| JP5460589B2 (ja) | 2007-07-13 | 2014-04-02 | アイカジェン， インコーポレイテッド | ナトリウムチャネル阻害物質 |
| US8853250B2 (en) | 2007-07-13 | 2014-10-07 | Icagen, Inc. | Sodium channel inhibitors |
| CA2747419C (en) * | 2009-01-12 | 2014-07-08 | Icagen, Inc. | Sulfonamide derivatives |
| KR101605061B1 (ko) | 2009-05-29 | 2016-03-21 | 라퀄리아 파마 인코포레이티드 | 칼슘 또는 나트륨 채널 차단제로서의 아릴 치환된 카복사미드 유도체 |
| EP2560636A4 (en) | 2010-04-23 | 2013-11-27 | Kineta Inc | ANTIVIRAL CONNECTIONS |
| WO2012004743A1 (en) | 2010-07-09 | 2012-01-12 | Pfizer Limited | Benzenesulfonamides useful as sodium channel inhibitors |
| 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 |
| ES2526675T3 (es) | 2010-07-09 | 2015-01-14 | Pfizer Limited | N-sulfonilbenzamidas como inhibidores de los canales de sodio dependientes de voltaje |
| EP2593427B1 (en) | 2010-07-12 | 2014-12-24 | Pfizer Limited | Sulfonamide derivatives as nav1.7 inhibitors for the treatment of pain |
| WO2012099983A1 (en) | 2011-01-18 | 2012-07-26 | Amgen Inc. | Nav1.7 knockout mice and uses thereof |
| UY34171A (es) * | 2011-07-01 | 2013-01-31 | Gilead Sciences Inc | Compuestos heterocíclicos fusionados como moduladores del canal iónico |
| AU2012296529A1 (en) | 2011-08-17 | 2014-02-20 | Amgen Inc. | Heteroaryl sodium channel inhibitors |
| WO2013043925A1 (en) * | 2011-09-21 | 2013-03-28 | Gilead Sciences, Inc. | Sodium channel blockers reduce glucagon secretion |
| MX2014005304A (es) | 2011-10-31 | 2015-03-20 | Xenon Pharmaceuticals Inc | Biaril eter sulfonamidas y su uso como agentes terapeuticos. |
| US9757379B2 (en) | 2012-11-14 | 2017-09-12 | The Board Of Regents Of The University Of Texas System | Inhibition of HIF-2α heterodimerization with HIF1β (ARNT) |
| US10179781B2 (en) * | 2013-03-15 | 2019-01-15 | Chromocell Corporation | Sodium channel modulators for the treatment of pain |
| EP3417851B1 (en) | 2013-09-09 | 2020-07-22 | 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 |
| EP3193610A4 (en) | 2014-09-09 | 2018-04-04 | 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 US US15/021,153 patent/US20160221974A1/en not_active Abandoned
- 2014-09-09 RU RU2016113156A patent/RU2016113156A/ru not_active Application Discontinuation
- 2014-09-09 SG SG10201805552PA patent/SG10201805552PA/en unknown
- 2014-09-09 BR BR112016005271-4A patent/BR112016005271A2/pt not_active IP Right Cessation
- 2014-09-09 SG SG11201601367QA patent/SG11201601367QA/en unknown
- 2014-09-09 KR KR1020167009294A patent/KR20160054570A/ko not_active Ceased
- 2014-09-09 MX MX2016002881A patent/MX2016002881A/es active IP Right Grant
- 2014-09-09 UA UAA201603676A patent/UA120353C2/uk unknown
- 2014-09-09 ES ES14843353.5T patent/ES2687598T3/es active Active
- 2014-09-09 JP JP2016540921A patent/JP6445565B2/ja active Active
- 2014-09-09 AU AU2014318979A patent/AU2014318979B2/en not_active Ceased
- 2014-09-09 WO PCT/US2014/054764 patent/WO2015038533A2/en not_active Ceased
- 2014-09-09 MY MYPI2016700824A patent/MY181928A/en unknown
- 2014-09-09 CA CA2922851A patent/CA2922851C/en active Active
- 2014-09-09 EP EP14843353.5A patent/EP3043787B1/en active Active
-
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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