JP2017504591A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2017504591A5 JP2017504591A5 JP2016538757A JP2016538757A JP2017504591A5 JP 2017504591 A5 JP2017504591 A5 JP 2017504591A5 JP 2016538757 A JP2016538757 A JP 2016538757A JP 2016538757 A JP2016538757 A JP 2016538757A JP 2017504591 A5 JP2017504591 A5 JP 2017504591A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- benzamido
- dihydrogen phosphate
- pain
- alkyl
- 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
- 150000001875 compounds Chemical class 0.000 claims description 77
- 229910052736 halogen Inorganic materials 0.000 claims description 56
- 150000002367 halogens Chemical class 0.000 claims description 56
- 208000002193 Pain Diseases 0.000 claims description 44
- 239000000203 mixture Substances 0.000 claims description 43
- 125000000217 alkyl group Chemical group 0.000 claims description 38
- 150000001768 cations Chemical class 0.000 claims description 20
- 238000000034 method Methods 0.000 claims description 17
- 208000004296 neuralgia Diseases 0.000 claims description 17
- 229910052739 hydrogen Inorganic materials 0.000 claims description 16
- 239000001257 hydrogen Substances 0.000 claims description 16
- 150000002431 hydrogen Chemical class 0.000 claims description 14
- 208000021722 neuropathic pain Diseases 0.000 claims description 11
- 229910052801 chlorine Inorganic materials 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 230000005855 radiation Effects 0.000 claims description 8
- 206010028391 Musculoskeletal Pain Diseases 0.000 claims description 7
- 206010065390 Inflammatory pain Diseases 0.000 claims description 6
- 208000027418 Wounds and injury Diseases 0.000 claims description 6
- 239000003960 organic solvent Substances 0.000 claims description 6
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 6
- 208000005298 acute pain Diseases 0.000 claims description 5
- 239000003814 drug Substances 0.000 claims description 5
- 208000014674 injury Diseases 0.000 claims description 5
- 208000005890 Neuroma Diseases 0.000 claims description 4
- 206010034620 Peripheral sensory neuropathy Diseases 0.000 claims description 4
- 102000016913 Voltage-Gated Sodium Channels Human genes 0.000 claims description 4
- 108010053752 Voltage-Gated Sodium Channels Proteins 0.000 claims description 4
- 230000006378 damage Effects 0.000 claims description 4
- 229910052731 fluorine Inorganic materials 0.000 claims description 4
- 210000005036 nerve Anatomy 0.000 claims description 4
- 201000005572 sensory peripheral neuropathy Diseases 0.000 claims description 4
- 208000011580 syndromic disease Diseases 0.000 claims description 4
- 206010044652 trigeminal neuralgia Diseases 0.000 claims description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 4
- 206010058019 Cancer Pain Diseases 0.000 claims description 3
- 208000010693 Charcot-Marie-Tooth Disease Diseases 0.000 claims description 3
- 208000000094 Chronic Pain Diseases 0.000 claims description 3
- 206010011224 Cough Diseases 0.000 claims description 3
- 206010021639 Incontinence Diseases 0.000 claims description 3
- 206010036376 Postherpetic Neuralgia Diseases 0.000 claims description 3
- 230000006793 arrhythmia Effects 0.000 claims description 3
- 206010003119 arrhythmia Diseases 0.000 claims description 3
- NBIIXXVUZAFLBC-UHFFFAOYSA-M dihydrogenphosphate Chemical compound OP(O)([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-M 0.000 claims description 3
- 230000000968 intestinal effect Effects 0.000 claims description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 3
- 201000006417 multiple sclerosis Diseases 0.000 claims description 3
- 201000001119 neuropathy Diseases 0.000 claims description 3
- 230000007823 neuropathy Effects 0.000 claims description 3
- 230000003349 osteoarthritic effect Effects 0.000 claims description 3
- 208000033808 peripheral neuropathy Diseases 0.000 claims description 3
- 229940124597 therapeutic agent Drugs 0.000 claims description 3
- OZJQFNSUXWRNPJ-UHFFFAOYSA-N 2-(4-fluoro-2-methylphenoxy)-4-(trifluoromethyl)benzamide Chemical compound FC1=CC(=C(OC2=C(C(=O)N)C=CC(=C2)C(F)(F)F)C=C1)C OZJQFNSUXWRNPJ-UHFFFAOYSA-N 0.000 claims description 2
- 208000008035 Back Pain Diseases 0.000 claims description 2
- 206010006074 Brachial plexus injury Diseases 0.000 claims description 2
- 208000011231 Crohn disease Diseases 0.000 claims description 2
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims description 2
- 208000001640 Fibromyalgia Diseases 0.000 claims description 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 2
- 206010019233 Headaches Diseases 0.000 claims description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 2
- 208000002472 Morton Neuroma Diseases 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 208000031481 Pathologic Constriction Diseases 0.000 claims description 2
- 208000004983 Phantom Limb Diseases 0.000 claims description 2
- 206010056238 Phantom pain Diseases 0.000 claims description 2
- 206010037660 Pyrexia Diseases 0.000 claims description 2
- 208000008765 Sciatica Diseases 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 238000002266 amputation Methods 0.000 claims description 2
- 238000011225 antiretroviral therapy Methods 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 208000003295 carpal tunnel syndrome Diseases 0.000 claims description 2
- 238000002512 chemotherapy Methods 0.000 claims description 2
- 238000000113 differential scanning calorimetry Methods 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims description 2
- 230000003619 fibrillary effect Effects 0.000 claims description 2
- 239000011737 fluorine Substances 0.000 claims description 2
- 231100000869 headache Toxicity 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 230000001575 pathological effect Effects 0.000 claims description 2
- 239000000843 powder Substances 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 239000011734 sodium Substances 0.000 claims description 2
- 239000007787 solid Substances 0.000 claims description 2
- 230000036262 stenosis Effects 0.000 claims description 2
- 208000037804 stenosis Diseases 0.000 claims description 2
- 230000001954 sterilising effect Effects 0.000 claims description 2
- 238000004659 sterilization and disinfection Methods 0.000 claims description 2
- 238000003756 stirring Methods 0.000 claims description 2
- 208000004371 toothache Diseases 0.000 claims description 2
- 230000000472 traumatic effect Effects 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims 5
- 208000004550 Postoperative Pain Diseases 0.000 claims 3
- 208000009935 visceral pain Diseases 0.000 claims 2
- -1 4- (2- (4-fluorophenoxy) -5- (trifluoromethyl) benzamido) -2-oxopyridin-1 (2H) -yl Chemical group 0.000 claims 1
- 206010052428 Wound Diseases 0.000 claims 1
- 230000002567 autonomic effect Effects 0.000 claims 1
- 201000003146 cystitis Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000020431 spinal cord injury Diseases 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 5
- 201000010099 disease Diseases 0.000 description 3
- 208000035475 disorder Diseases 0.000 description 2
- 0 **c(cc1)cc(*)c1Oc(cc(*)c(*)c1)c1C(NC(C=CN1CO*)=CC1=O)=O Chemical compound **c(cc1)cc(*)c1Oc(cc(*)c(*)c1)c1C(NC(C=CN1CO*)=CC1=O)=O 0.000 description 1
- 206010003497 Asphyxia Diseases 0.000 description 1
- SQDQNNKQTHOQHO-UHFFFAOYSA-N Cc1cc(F)ccc1Oc1cc(C(F)(F)F)ccc1C(NC(C=CN1COP(O)(O)=O)=CC1=O)=O Chemical compound Cc1cc(F)ccc1Oc1cc(C(F)(F)F)ccc1C(NC(C=CN1COP(O)(O)=O)=CC1=O)=O SQDQNNKQTHOQHO-UHFFFAOYSA-N 0.000 description 1
- 208000005615 Interstitial Cystitis Diseases 0.000 description 1
- 210000000467 autonomic pathway Anatomy 0.000 description 1
- 210000000278 spinal cord Anatomy 0.000 description 1
- 210000003901 trigeminal nerve Anatomy 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361915937P | 2013-12-13 | 2013-12-13 | |
| US61/915,937 | 2013-12-13 | ||
| PCT/US2014/069916 WO2015089361A1 (en) | 2013-12-13 | 2014-12-12 | Prodrugs of pyridone amides useful as modulators of sodium channels |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018221093A Division JP2019055974A (ja) | 2013-12-13 | 2018-11-27 | ナトリウムチャネルの調節剤として有用なピリドンアミドのプロドラッグ |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017504591A JP2017504591A (ja) | 2017-02-09 |
| JP2017504591A5 true JP2017504591A5 (enExample) | 2018-01-25 |
| JP6463580B2 JP6463580B2 (ja) | 2019-02-06 |
Family
ID=52293220
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016538757A Active JP6463580B2 (ja) | 2013-12-13 | 2014-12-12 | ナトリウムチャネルの調節剤として有用なピリドンアミドのプロドラッグ |
| JP2018221093A Withdrawn JP2019055974A (ja) | 2013-12-13 | 2018-11-27 | ナトリウムチャネルの調節剤として有用なピリドンアミドのプロドラッグ |
| JP2020134430A Active JP7465174B2 (ja) | 2013-12-13 | 2020-08-07 | ナトリウムチャネルの調節剤として有用なピリドンアミドのプロドラッグ |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018221093A Withdrawn JP2019055974A (ja) | 2013-12-13 | 2018-11-27 | ナトリウムチャネルの調節剤として有用なピリドンアミドのプロドラッグ |
| JP2020134430A Active JP7465174B2 (ja) | 2013-12-13 | 2020-08-07 | ナトリウムチャネルの調節剤として有用なピリドンアミドのプロドラッグ |
Country Status (33)
Families Citing this family (69)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013169939A2 (en) | 2012-05-08 | 2013-11-14 | Aeromics, Llc | New methods |
| PL2953931T3 (pl) | 2013-01-31 | 2017-09-29 | Vertex Pharmaceuticals Incorporated | Pirydonoamidy jako modulatory kanałów sodowych |
| KR102226587B1 (ko) | 2013-01-31 | 2021-03-11 | 버텍스 파마슈티칼스 인코포레이티드 | 나트륨 채널의 조절제로서의 퀴놀린 및 퀴나졸린 아미드 |
| RU2680401C2 (ru) | 2013-07-19 | 2019-02-21 | Вертекс Фармасьютикалз Инкорпорейтед | Сульфонамиды в качестве модуляторов натриевых каналов |
| KR20160079109A (ko) | 2013-11-06 | 2016-07-05 | 에어로믹스, 인코포레이티드 | 새로운 조성물 |
| SMT201800521T1 (it) * | 2013-12-13 | 2018-11-09 | Vertex Pharma | Profarmaci di piridonammidi utili come modulatori di canali del sodio |
| US11221329B2 (en) | 2015-10-30 | 2022-01-11 | Lieber Institute, Inc. | Treatment of neurological and neurodevelopmental diseases and disorders associated with aberrant ion channel expression and activity |
| US20170239183A1 (en) * | 2016-02-23 | 2017-08-24 | PixarBio Corporation | COMPOSITIONS COMPRISING NAv1.7 SELECTIVE INHIBITORS FOR TREATING ACUTE, POST-OPERATIVE, OR CHRONIC PAIN AND METHODS OF USING THE SAME |
| CN115093443A (zh) | 2016-05-13 | 2022-09-23 | 埃罗米克斯公司 | 晶体 |
| WO2018213426A1 (en) * | 2017-05-16 | 2018-11-22 | Vertex Pharmaceuticals Incorporated | Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels |
| WO2019014352A1 (en) | 2017-07-11 | 2019-01-17 | Vertex Pharmaceuticals Incorporated | CARBOXAMIDES AS INHIBITORS OF SODIUM CHANNELS |
| US10495175B2 (en) * | 2017-08-08 | 2019-12-03 | Ford Global Technologies, Llc | Composite materials having embedded metal ropes for increased damping capacity and methods of manufacturing same |
| JP2021512935A (ja) | 2018-02-12 | 2021-05-20 | 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 | 疼痛を処置する方法 |
| JP2021530478A (ja) | 2018-07-09 | 2021-11-11 | リーバー インスティチュート インコーポレイテッドLieber Institute, Inc. | NaV1.8を阻害するためのピリジンカルボキシアミド化合物 |
| AU2019302534B2 (en) | 2018-07-09 | 2024-10-03 | Lieber Institute, Inc. | Pyridazine compounds for inhibiting NaV1.8 |
| US12344595B2 (en) | 2018-11-02 | 2025-07-01 | Merck Sharp & Dohme Llc | 2-amino-n-phenyl-nicotinamides as NAV1.8 inhibitors |
| AU2019372057A1 (en) * | 2018-11-02 | 2021-05-27 | Merck Sharp & Dohme Llc | 2-amino-N-heteroaryl-nicotinamides as NAV1.8 inhibitors |
| US12440481B2 (en) | 2019-01-10 | 2025-10-14 | Vertex Pharmaceuticals Incorporated | Esters and carbamates as modulators of sodium channels |
| WO2020146682A1 (en) | 2019-01-10 | 2020-07-16 | Vertex Pharmaceuticals Incorporated | Carboxamides as modulators of sodium channels |
| CN112996774B (zh) * | 2019-01-25 | 2022-11-22 | 江苏恒瑞医药股份有限公司 | 2-氧代-1,2-二氢吡啶类衍生物、其制备方法及其在医药上的应用 |
| CN112996776B (zh) * | 2019-02-20 | 2024-03-15 | 福建盛迪医药有限公司 | 6-氧代-1,6-二氢哒嗪类前药衍生物、其制备方法及其在医药上的应用 |
| WO2020176763A1 (en) | 2019-02-27 | 2020-09-03 | Vertex Pharmaceuticals Incorporated | Dosage form comprising prodrug of na 1.8 sodium channel inhibitor |
| WO2020206119A1 (en) | 2019-04-02 | 2020-10-08 | Vertex Pharmaceuticals Incorporated | Process for making pyridone amides and prodrugs thereof useful as modulators of sodium channels |
| WO2020219867A1 (en) | 2019-04-25 | 2020-10-29 | Vertex Pharmaceuticals Incorporated | Pyridone amide co-crystal compositions for the treatment of pain |
| WO2021018165A1 (zh) * | 2019-07-30 | 2021-02-04 | 江苏恒瑞医药股份有限公司 | 吡啶苯甲酰胺类衍生物、其制备方法及其在医药上的应用 |
| TW202115038A (zh) * | 2019-08-19 | 2021-04-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 苯甲醯胺稠芳環類衍生物、其製備方法及其在醫藥上的應用 |
| PH12022550584A1 (en) * | 2019-09-12 | 2024-03-04 | Orion Corp | Pyridine oxynitride, preparation method therefor and use thereof |
| PH12022551379A1 (en) | 2019-12-06 | 2023-05-03 | Vertex Pharma | Substituted tetrahydrofurans as modulators of sodium channels |
| CN114437062B (zh) * | 2020-04-30 | 2024-05-17 | 成都海博为药业有限公司 | 一种可作为钠通道调节剂的化合物及其用途 |
| EP4168393A1 (en) | 2020-06-17 | 2023-04-26 | Merck Sharp & Dohme LLC | 2-oxoimidazolidine-4-carboxamides as nav1.8 inhibitors |
| CN113880771B (zh) * | 2020-07-03 | 2023-09-19 | 福建盛迪医药有限公司 | 一种选择性Nav抑制剂的结晶形式及其制备方法 |
| JP2023536509A (ja) * | 2020-08-05 | 2023-08-25 | ジャンスー・シムセレ・ファーマシューティカル・カンパニー・リミテッド | アクアポリン阻害剤の医薬組成物およびその製造方法 |
| TW202214259A (zh) * | 2020-08-19 | 2022-04-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 一種選擇性NaV抑制劑的前藥及其晶型 |
| CN111808019B (zh) * | 2020-09-08 | 2020-11-27 | 上海济煜医药科技有限公司 | 一种并环化合物及其应用 |
| CN114591293A (zh) * | 2020-12-07 | 2022-06-07 | 成都康弘药业集团股份有限公司 | 作为Nav1.8抑制剂的并环化合物及其用途 |
| CN114031518B (zh) * | 2020-12-08 | 2023-08-18 | 成都海博为药业有限公司 | 一种苄胺或苄醇衍生物及其用途 |
| MX2023007244A (es) * | 2020-12-18 | 2023-06-29 | Glaxosmithkline Ip Dev Ltd | Compuestos quimicos utiles para inhibir los canales de sodio activados por voltaje de nav1.8 y tratar las enfermedades mediadas por nav1.8. |
| TW202302118A (zh) * | 2021-02-26 | 2023-01-16 | 大陸商江蘇恒瑞醫藥股份有限公司 | 一種選擇性nav抑制劑的可藥用鹽、結晶形式及其製備方法 |
| EP4334293A1 (en) | 2021-05-07 | 2024-03-13 | Merck Sharp & Dohme LLC | Cycloalkyl 3-oxopiperazine carboxamides and cycloheteroalkyl 3-oxopiperazine carboxamides as nav1.8 inhibitors |
| US20240368135A1 (en) | 2021-06-04 | 2024-11-07 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels |
| US20250213555A1 (en) | 2021-06-04 | 2025-07-03 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran analogs as modulators of sodium channels |
| JP2024520643A (ja) | 2021-06-04 | 2024-05-24 | 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 | ナトリウムチャネルの調節因子としてのヒドロキシ及び(ハロ)アルコキシ置換テトラヒドロフラン |
| EP4347584A1 (en) | 2021-06-04 | 2024-04-10 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels |
| EP4346818B1 (en) | 2021-06-04 | 2025-12-03 | Vertex Pharmaceuticals Incorporated | Solid dosage forms and dosing regimens comprising (2r,3s,4s,5r)-4-[[3-(3,4-difluoro-2-methoxy-phenyl)-4,5-dimethyl-5-(trifluoromethyl) tetrahydrofuran-2-carbonyl]amino]pyridine-2-carboxamide |
| DK4347031T3 (da) | 2021-06-04 | 2025-12-01 | Vertex Pharma | N-(hydroxyalkyl-(hetero)aryl)-tetrahydrofuran-carboxamider som modulatorer af natriumkanaler |
| AR126669A1 (es) | 2021-08-02 | 2023-11-01 | Eurofarma Laboratorios S A | COMPUESTOS N-ACILIDRAZÓNICOS INHIBIDORES DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, COMPOSICIONES, USOS, MÉTODOS DE TRATAMIENTO DE ESTOS Y KITS |
| AR126670A1 (es) | 2021-08-02 | 2023-11-01 | Eurofarma Laboratorios S A | COMPUESTOS N-ACILIDRAZÓNICOS INHIBIDORES DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, COMPOSICIONES, USOS, MÉTODOS DE TRATAMIENTO DE ESTOS Y KITS |
| CN114288289A (zh) * | 2022-02-17 | 2022-04-08 | 昆山彭济凯丰生物科技有限公司 | 具有镇痛和/或止痒功能的药物组合物及其应用 |
| CN116655497B (zh) * | 2022-02-25 | 2025-06-03 | 中国科学院上海药物研究所 | 脒类衍生化合物及其制备方法和用途 |
| EP4511115A1 (en) | 2022-04-22 | 2025-02-26 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| AU2023255558A1 (en) | 2022-04-22 | 2024-10-31 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| EP4511114A1 (en) | 2022-04-22 | 2025-02-26 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| KR20250005373A (ko) | 2022-04-22 | 2025-01-09 | 버텍스 파마슈티칼스 인코포레이티드 | 통증 치료를 위한 헤테로아릴 화합물 |
| CA3256486A1 (en) | 2022-04-25 | 2023-11-02 | Siteone Therapeutics Inc | Bicyclic Na V1.8 Heterocyclic Amide Inhibitors for Pain Management |
| JP2025518207A (ja) * | 2022-06-02 | 2025-06-12 | シャンハイ ジェミンケア ファーマシューティカル カンパニー,リミティド | ピリジン-n-オキシド化合物の調製方法 |
| TWI867570B (zh) * | 2022-06-09 | 2024-12-21 | 英商葛蘭素史密斯克藍智慧財產發展有限公司 | 化合物 |
| WO2024067783A1 (zh) * | 2022-09-28 | 2024-04-04 | 上海济煜医药科技有限公司 | 含磷类化合物及其制备方法和医药应用 |
| CN120603815A (zh) | 2022-12-06 | 2025-09-05 | 沃泰克斯药物股份有限公司 | 钠通道的取代四氢呋喃调节剂的合成方法 |
| AR131690A1 (es) | 2023-01-30 | 2025-04-23 | Eurofarma Laboratorios S A | COMPUESTOS FENÓLICOS BLOQUEADORES DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, SUS COMPOSICIONES, SUS USOS, LOS MÉTODOS DE TRATAMIENTO DE LOS MISMOS Y LOS KITS |
| AR131715A1 (es) | 2023-01-30 | 2025-04-23 | Eurofarma Laboratorios S A | AMIDAS BLOQUEADORAS DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, COMPOSICIONES, USOS, MÉTODOS DE TRATAMIENTO DE LOS MISMOS Y KITS |
| EP4660182A1 (en) | 2023-01-30 | 2025-12-10 | Eurofarma Laboratórios S.A. | Nav1.7- and/or nav1.8-inhibiting aryl pyridine compounds, processes for the preparation thereof, compositions, uses, methods for treatment using same, and kits |
| WO2024159287A1 (pt) | 2023-01-30 | 2024-08-08 | Eurofarma Laboratórios S.A. | Hidroxamatos bloqueadores de nav 1.7 e/ou nav 1.8, seus processos de obtenção, composições, usos, métodos de tratamento destes e kits |
| AR131658A1 (es) | 2023-01-30 | 2025-04-16 | Eurofarma Laboratorios S A | Hidrazidas bloqueadoras de nav 1.7 y/o nav 1.8, sus procesos de obtención, composiciones, usos, métodos de tratamiento de los mismos y sus kits |
| TW202535867A (zh) | 2023-10-23 | 2025-09-16 | 美商維泰克斯製藥公司 | 用於治療疼痛之鈉通道調節劑及其固體形式的製備方法 |
| WO2025090480A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| WO2025090516A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Methods of preparing compounds for treating pain and solid forms thereof |
| TW202523313A (zh) | 2023-10-23 | 2025-06-16 | 美商維泰克斯製藥公司 | 用於治療疼痛之雜芳基化合物 |
| US20250186419A1 (en) | 2023-12-07 | 2025-06-12 | Vertex Pharmaceuticals Incorporated | Dosing regimens for treating pain |
| WO2025160286A1 (en) | 2024-01-24 | 2025-07-31 | Siteone Therapeutics, Inc. | 2-aryl cycloalkyl and heterocycloalkyl inhibitors of nav1.8 for the treatment of pain |
Family Cites Families (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH02245793A (ja) | 1989-03-20 | 1990-10-01 | Hitachi Ltd | マトリックス表示装置 |
| US5304121A (en) | 1990-12-28 | 1994-04-19 | Boston Scientific Corporation | Drug delivery system making use of a hydrogel polymer coating |
| US5994341A (en) | 1993-07-19 | 1999-11-30 | Angiogenesis Technologies, Inc. | Anti-angiogenic Compositions and methods for the treatment of arthritis |
| US6099562A (en) | 1996-06-13 | 2000-08-08 | Schneider (Usa) Inc. | Drug coating with topcoat |
| ES2273868T3 (es) | 2000-07-10 | 2007-05-16 | Vertex Pharmaceuticals (San Diego) Llc | Metodos de ensayo de canal ionico. |
| JP2003034671A (ja) | 2001-05-17 | 2003-02-07 | Nippon Nohyaku Co Ltd | ベンズアミド誘導体及び農園芸用薬剤並びにその使用方法 |
| PL218749B1 (pl) | 2002-02-14 | 2015-01-30 | Pharmacia Corp | Pochodna pirydynonu oraz jej zastosowanie do wytwarzania leku |
| TW200524888A (en) * | 2003-08-08 | 2005-08-01 | Vertex Pharma | Compositions useful as inhibitors of voltage-gated ion channels |
| EP1802580A2 (en) | 2004-07-23 | 2007-07-04 | Pfizer, Inc. | Pyridine derivatives |
| KR20080109918A (ko) | 2006-04-11 | 2008-12-17 | 버텍스 파마슈티칼스 인코포레이티드 | 전압 개폐 나트륨 채널의 억제제로서 유용한 조성물 |
| ATE545416T1 (de) | 2006-10-12 | 2012-03-15 | Xenon Pharmaceuticals Inc | Verwendung von spiro-oxindol-verbindungen als therapeutika |
| KR20100007956A (ko) | 2007-05-03 | 2010-01-22 | 화이자 리미티드 | 나트륨 채널 조절제로서의 2-피리딘 카복스아마이드 유도체 |
| NZ584475A (en) | 2007-10-11 | 2012-07-27 | Vertex Pharma | Heteroaryl amides useful as inhibitors of voltage-gated sodium channels |
| RU2010118481A (ru) * | 2007-10-11 | 2011-11-20 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Амиды, применимые в качестве ингибиторов потенциалзависимых натриевых каналов |
| MX2010003865A (es) * | 2007-10-11 | 2010-06-01 | Vertex Pharma | Aril amidas utiles como inhibidores de canales de sodio dependientes de voltaje. |
| ES2383273T3 (es) * | 2008-07-23 | 2012-06-19 | F. Hoffmann-La Roche Ag | Compuestos heterocíclicos antivíricos |
| PE20110574A1 (es) | 2008-10-29 | 2011-08-11 | Hoffmann La Roche | Derivados de fenilamida y de piridilamida como agonistas de gpbar1 |
| CA2745952A1 (en) | 2008-12-23 | 2010-07-01 | F.Hoffmann-La Roche Ag | Dihydropyridone amides as p2x7 modulators |
| TWI436986B (zh) | 2008-12-26 | 2014-05-11 | Dainippon Sumitomo Pharma Co | 新穎之2環性雜環化合物 |
| JP5685203B2 (ja) | 2009-05-29 | 2015-03-18 | ラクオリア創薬株式会社 | カルシウムチャネル遮断薬またはナトリウムチャネル遮断薬としてのアリール置換カルボキサミド誘導体 |
| TW201103904A (en) | 2009-06-11 | 2011-02-01 | Hoffmann La Roche | Janus kinase inhibitor compounds and methods |
| AR077252A1 (es) | 2009-06-29 | 2011-08-10 | Xenon Pharmaceuticals Inc | Enantiomeros de compuestos de espirooxindol y sus usos como agentes terapeuticos |
| WO2011026240A1 (en) | 2009-09-04 | 2011-03-10 | Zalicus Pharmaceuticals Ltd. | Oxopiperazine derivatives for the treatment of pain and epilepsy |
| WO2011140425A1 (en) | 2010-05-06 | 2011-11-10 | Vertex Pharmaceuticals Incorporated | Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels |
| KR20130119964A (ko) | 2010-12-22 | 2013-11-01 | 퍼듀 퍼머 엘피 | 나트륨 채널 차단제로서의 치환된 피리딘 |
| TW201604196A (zh) | 2011-02-02 | 2016-02-01 | 維泰克斯製藥公司 | 作為離子通道調節劑之吡咯并吡-螺環哌啶醯胺 |
| US10385070B2 (en) | 2011-02-18 | 2019-08-20 | Vertex Pharmaceuticals Incorporated | Chroman-spirocyclic piperidine amides as modulators of ion channels |
| EP2681200A4 (en) | 2011-03-03 | 2015-05-27 | Zalicus Pharmaceuticals Ltd | INHIBITORS OF BENZIMIDAZOLE TYPE OF SODIUM CHANNEL |
| EP2686325B1 (en) | 2011-03-14 | 2016-12-14 | Vertex Pharmaceuticals Incorporated | Morpholine-spirocyclic piperidine amides as modulators of ion channels |
| TWI567061B (zh) * | 2011-07-01 | 2017-01-21 | 吉李德科學股份有限公司 | 用於治療成癮之化合物 |
| WO2013012104A1 (ko) | 2011-07-18 | 2013-01-24 | 엘지전자 주식회사 | 전자기기 및 전자기기의 동작 방법 |
| EP2753606B1 (en) * | 2011-09-02 | 2017-07-05 | Purdue Pharma LP | Pyrimidines as sodium channel blockers |
| US9079878B2 (en) | 2011-10-26 | 2015-07-14 | Pfizer Limited | (4-phenylimidazol-2-yl) ethylamine derivatives useful as sodium channel modulators |
| CN104136442B (zh) | 2012-01-16 | 2016-12-21 | 沃泰克斯药物股份有限公司 | 作为离子通道调节剂的吡喃‑螺环哌啶酰胺类 |
| WO2013114250A1 (en) | 2012-02-03 | 2013-08-08 | Pfizer Inc. | Benziimidazole and imidazopyridine derivatives as sodium channel modulators |
| US20130225529A1 (en) * | 2012-02-27 | 2013-08-29 | Basil Rigas | Phospho-ester derivatives and uses thereof |
| WO2013131018A1 (en) | 2012-03-02 | 2013-09-06 | Zalicus Pharmaceuticals Ltd. | Biaryl inhibitors of the sodium channel |
| EP2822953B9 (en) | 2012-03-06 | 2017-06-21 | Pfizer Inc | Macrocyclic derivatives for the treatment of proliferative diseases |
| KR102226587B1 (ko) | 2013-01-31 | 2021-03-11 | 버텍스 파마슈티칼스 인코포레이티드 | 나트륨 채널의 조절제로서의 퀴놀린 및 퀴나졸린 아미드 |
| AU2014212431B2 (en) | 2013-01-31 | 2018-04-05 | Vertex Pharmaceuticals Incorporated | Amides as modulators of sodium channels |
| PL2953931T3 (pl) | 2013-01-31 | 2017-09-29 | Vertex Pharmaceuticals Incorporated | Pirydonoamidy jako modulatory kanałów sodowych |
| TWI606048B (zh) | 2013-01-31 | 2017-11-21 | 帝人製藥股份有限公司 | 唑苯衍生物 |
| RU2680401C2 (ru) * | 2013-07-19 | 2019-02-21 | Вертекс Фармасьютикалз Инкорпорейтед | Сульфонамиды в качестве модуляторов натриевых каналов |
| SMT201800521T1 (it) * | 2013-12-13 | 2018-11-09 | Vertex Pharma | Profarmaci di piridonammidi utili come modulatori di canali del sodio |
| WO2019014352A1 (en) | 2017-07-11 | 2019-01-17 | Vertex Pharmaceuticals Incorporated | CARBOXAMIDES AS INHIBITORS OF SODIUM CHANNELS |
| JP2021512935A (ja) | 2018-02-12 | 2021-05-20 | 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 | 疼痛を処置する方法 |
-
2014
- 2014-12-12 SM SM20180521T patent/SMT201800521T1/it unknown
- 2014-12-12 BR BR122020007729-8A patent/BR122020007729B1/pt active IP Right Grant
- 2014-12-12 TW TW107147684A patent/TWI668226B/zh active
- 2014-12-12 RS RS20181154A patent/RS57700B1/sr unknown
- 2014-12-12 RU RU2016127914A patent/RU2692766C1/ru active
- 2014-12-12 CN CN201480068225.9A patent/CN105814067B/zh active Active
- 2014-12-12 LT LTEP14824658.0T patent/LT3080134T/lt unknown
- 2014-12-12 WO PCT/US2014/069916 patent/WO2015089361A1/en not_active Ceased
- 2014-12-12 CN CN201810375545.9A patent/CN108395452B/zh active Active
- 2014-12-12 US US14/568,391 patent/US9163042B2/en active Active
- 2014-12-12 ES ES14824658.0T patent/ES2688590T3/es active Active
- 2014-12-12 TW TW103143540A patent/TWI651329B/zh active
- 2014-12-12 NZ NZ760006A patent/NZ760006A/en unknown
- 2014-12-12 TW TW108123460A patent/TWI703154B/zh active
- 2014-12-12 MX MX2016007258A patent/MX379264B/es unknown
- 2014-12-12 GE GEAP201414203A patent/GEP20207082B/en unknown
- 2014-12-12 KR KR1020167018800A patent/KR102435145B1/ko active Active
- 2014-12-12 CA CA2931550A patent/CA2931550C/en active Active
- 2014-12-12 AP AP2016009287A patent/AP2016009287A0/en unknown
- 2014-12-12 SG SG10201913313QA patent/SG10201913313QA/en unknown
- 2014-12-12 UA UAA201607639A patent/UA121379C2/uk unknown
- 2014-12-12 JP JP2016538757A patent/JP6463580B2/ja active Active
- 2014-12-12 AU AU2014362255A patent/AU2014362255B2/en active Active
- 2014-12-12 EP EP14824658.0A patent/EP3080134B1/en active Active
- 2014-12-12 GE GEAP201414976A patent/GEP20217223B/en unknown
- 2014-12-12 PL PL14824658T patent/PL3080134T3/pl unknown
- 2014-12-12 EP EP18186616.1A patent/EP3459958B1/en active Active
- 2014-12-12 PE PE2016000745A patent/PE20161131A1/es unknown
- 2014-12-12 DK DK14824658.0T patent/DK3080134T3/en active
- 2014-12-12 SG SG11201604477SA patent/SG11201604477SA/en unknown
- 2014-12-12 ES ES18186616T patent/ES2986650T3/es active Active
- 2014-12-12 PT PT14824658T patent/PT3080134T/pt unknown
- 2014-12-12 HR HRP20181563TT patent/HRP20181563T1/hr unknown
- 2014-12-12 NZ NZ720444A patent/NZ720444A/en unknown
- 2014-12-12 SI SI201430873T patent/SI3080134T1/sl unknown
-
2015
- 2015-09-18 US US14/858,635 patent/US9464102B2/en active Active
-
2016
- 2016-05-24 ZA ZA2016/03546A patent/ZA201603546B/en unknown
- 2016-06-01 PH PH12016501028A patent/PH12016501028A1/en unknown
- 2016-06-03 MX MX2021000781A patent/MX2021000781A/es unknown
- 2016-06-06 IL IL246061A patent/IL246061B/en unknown
- 2016-06-08 CL CL2016001400A patent/CL2016001400A1/es unknown
- 2016-06-13 EC ECIEPI201625201A patent/ECSP16025201A/es unknown
- 2016-09-09 US US15/260,778 patent/US9828397B2/en active Active
-
2017
- 2017-10-24 US US15/791,982 patent/US10253054B2/en active Active
-
2018
- 2018-10-24 CY CY181101096T patent/CY1121030T1/el unknown
- 2018-11-27 JP JP2018221093A patent/JP2019055974A/ja not_active Withdrawn
-
2019
- 2019-02-25 US US16/283,904 patent/US10787472B2/en active Active
- 2019-11-26 AU AU2019271928A patent/AU2019271928B2/en active Active
-
2020
- 2020-08-07 JP JP2020134430A patent/JP7465174B2/ja active Active
- 2020-08-20 US US16/998,426 patent/US11773119B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2017504591A5 (enExample) | ||
| RU2526201C2 (ru) | Способ лечения артрита | |
| JP2020519661A5 (enExample) | ||
| DE68910945T2 (de) | Isoxazole und Isoxazolin-Derivate mit Antikonvulsiva und pharmazeutische Zusammensetzungen, die sie enthalten. | |
| DE602004008100T2 (de) | 4-biarylyl-1-phenylazetidin-2-one | |
| JP2020503374A5 (enExample) | ||
| JP2016525122A5 (enExample) | ||
| JP2016508500A5 (enExample) | ||
| JP2010514829A5 (enExample) | ||
| FI3856341T3 (fi) | (s)-1-(4-fluorifenyyli)-1-(2-(4-(6-(1-metyyli-1h-pyratsol-4-yyli)pyrrolo[2,1-f][1,2,4]triatsin-4-yyli)piperatsinyyli)pyrimidin-5-yyli)etaani-1-amiinin kidemuotoja ja valmistusmenetelmiä | |
| JP2014506602A5 (enExample) | ||
| JPH01226818A (ja) | アリールアミドアザビシクロアルカン類およびアリールチオアミドアザビシクロアルカン類からなる記憶力増進剤または記憶障害治療剤 | |
| RU2006126977A (ru) | Кристаллическая форма соли 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамида или сольвата этой соли и способы ее получения | |
| EP3083601B1 (en) | Piperidine derivatives having multimodal activity against pain | |
| JP2023036007A5 (enExample) | ||
| RU2010119458A (ru) | 1,3,5-тризамещенное производное триазола | |
| JP2013532668A5 (enExample) | ||
| JP2005506308A5 (enExample) | ||
| JP2015522551A5 (enExample) | ||
| JP7159440B2 (ja) | ジカチオン化合物及びその製造方法と使用 | |
| JP2020520957A5 (enExample) | ||
| JP2009534373A5 (enExample) | ||
| TWI694986B (zh) | 經取代之吡啶基-環烷基-羧酸、包含其之組合物及其用途 | |
| RU2014138619A (ru) | Новые соли тримебутина на основе сульфонатов | |
| JP2009040767A5 (enExample) |