JP2015505321A5 - - Google Patents
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- Publication number
- JP2015505321A5 JP2015505321A5 JP2014552376A JP2014552376A JP2015505321A5 JP 2015505321 A5 JP2015505321 A5 JP 2015505321A5 JP 2014552376 A JP2014552376 A JP 2014552376A JP 2014552376 A JP2014552376 A JP 2014552376A JP 2015505321 A5 JP2015505321 A5 JP 2015505321A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- compound according
- alkyl
- cycloalkyl
- 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 53
- 150000003839 salts Chemical class 0.000 claims description 27
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 26
- 229910002091 carbon monoxide Inorganic materials 0.000 claims description 26
- 125000004122 cyclic group Chemical group 0.000 claims description 24
- 229910052757 nitrogen Inorganic materials 0.000 claims description 24
- 229910052760 oxygen Inorganic materials 0.000 claims description 24
- 229910052717 sulfur Inorganic materials 0.000 claims description 24
- 229910052799 carbon Inorganic materials 0.000 claims description 23
- 125000001072 heteroaryl group Chemical group 0.000 claims description 22
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 22
- 229910052739 hydrogen Inorganic materials 0.000 claims description 21
- 125000005843 halogen group Chemical group 0.000 claims description 20
- 125000003118 aryl group Chemical group 0.000 claims description 14
- 208000002193 Pain Diseases 0.000 claims description 13
- -1 heterocycloalkoxy Chemical group 0.000 claims description 12
- 208000004296 neuralgia Diseases 0.000 claims description 9
- 239000000203 mixture Substances 0.000 claims description 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 6
- 125000003107 substituted aryl group Chemical group 0.000 claims description 6
- 208000019695 Migraine disease Diseases 0.000 claims description 5
- 206010027599 migraine Diseases 0.000 claims description 5
- 125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 claims description 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 4
- 108010052164 Sodium Channels Proteins 0.000 claims description 4
- 102000018674 Sodium Channels Human genes 0.000 claims description 4
- 125000004429 atom Chemical group 0.000 claims description 4
- 125000005842 heteroatom Chemical group 0.000 claims description 4
- 125000000623 heterocyclic group Chemical group 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
- 208000006561 Cluster Headache Diseases 0.000 claims description 3
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims description 3
- 206010019233 Headaches 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
- 206010061533 Myotonia Diseases 0.000 claims description 3
- 206010028836 Neck pain Diseases 0.000 claims description 3
- 208000001294 Nociceptive Pain Diseases 0.000 claims description 3
- 206010036376 Postherpetic Neuralgia Diseases 0.000 claims description 3
- 208000004550 Postoperative Pain Diseases 0.000 claims description 3
- 208000008765 Sciatica Diseases 0.000 claims description 3
- 230000001154 acute effect Effects 0.000 claims description 3
- 208000005298 acute pain 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
- 239000012472 biological sample Substances 0.000 claims description 3
- 230000001684 chronic effect Effects 0.000 claims description 3
- 208000018912 cluster headache syndrome Diseases 0.000 claims description 3
- 206010015037 epilepsy Diseases 0.000 claims description 3
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims description 3
- 231100000869 headache Toxicity 0.000 claims description 3
- 208000002551 irritable bowel syndrome Diseases 0.000 claims description 3
- 201000006417 multiple sclerosis Diseases 0.000 claims description 3
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 3
- 208000015706 neuroendocrine disease Diseases 0.000 claims description 3
- 230000002981 neuropathic effect Effects 0.000 claims description 3
- 208000021722 neuropathic pain Diseases 0.000 claims description 3
- 201000008482 osteoarthritis Diseases 0.000 claims description 3
- 208000020016 psychiatric disease Diseases 0.000 claims description 3
- 230000009885 systemic effect Effects 0.000 claims description 3
- 206010044652 trigeminal neuralgia Diseases 0.000 claims description 3
- 208000009935 visceral pain Diseases 0.000 claims description 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims description 2
- 206010002383 Angina Pectoris Diseases 0.000 claims description 2
- 208000020925 Bipolar disease Diseases 0.000 claims description 2
- 201000006474 Brain Ischemia Diseases 0.000 claims description 2
- 206010008120 Cerebral ischaemia Diseases 0.000 claims description 2
- 206010020772 Hypertension Diseases 0.000 claims description 2
- 206010033557 Palpitations Diseases 0.000 claims description 2
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims description 2
- 208000006011 Stroke Diseases 0.000 claims description 2
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims description 2
- 208000027418 Wounds and injury Diseases 0.000 claims description 2
- 230000002159 abnormal effect Effects 0.000 claims description 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 2
- 210000004556 brain Anatomy 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
- 230000005176 gastrointestinal motility Effects 0.000 claims description 2
- 208000014674 injury Diseases 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 230000000472 traumatic effect Effects 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 0 *C(CCC1)OC1(CC1)CIN1C(C1=CC=CC=CC=CC=C1)=O Chemical compound *C(CCC1)OC1(CC1)CIN1C(C1=CC=CC=CC=CC=C1)=O 0.000 description 6
- 125000003545 alkoxy group Chemical group 0.000 description 3
- 125000000217 alkyl group Chemical group 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 201000010099 disease Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261586875P | 2012-01-16 | 2012-01-16 | |
| US61/586,875 | 2012-01-16 | ||
| PCT/US2013/021535 WO2013109521A1 (en) | 2012-01-16 | 2013-01-15 | Pyran-spirocyclic piperidine amides as modulators of ion channels |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015505321A JP2015505321A (ja) | 2015-02-19 |
| JP2015505321A5 true JP2015505321A5 (enExample) | 2016-03-03 |
| JP6215230B2 JP6215230B2 (ja) | 2017-10-18 |
Family
ID=47595110
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014552376A Active JP6215230B2 (ja) | 2012-01-16 | 2013-01-15 | 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 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9403839B2 (enExample) |
| EP (1) | EP2804868B1 (enExample) |
| JP (1) | JP6215230B2 (enExample) |
| CN (1) | CN104136442B (enExample) |
| AU (1) | AU2013209958B2 (enExample) |
| CA (1) | CA2863343A1 (enExample) |
| ES (1) | ES2631611T3 (enExample) |
| MX (1) | MX2014008591A (enExample) |
| NZ (1) | NZ627259A (enExample) |
| WO (1) | WO2013109521A1 (enExample) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6337109B2 (ja) | 2013-07-19 | 2018-06-06 | 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 | ナトリウムチャネルの調節剤としてのスルホンアミド |
| JP6463580B2 (ja) | 2013-12-13 | 2019-02-06 | 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 | 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 |
| BR112019024016A2 (pt) | 2017-05-16 | 2020-06-09 | Vertex Pharma | amidas de piridona deuteradas e profármacos das mesmas como moduladores de canais de sódio |
| CA3069720A1 (en) | 2017-07-11 | 2019-01-17 | Vertex Pharmaceuticals Incorporated | Carboxamides as modulators of sodium channels |
| KR102731924B1 (ko) * | 2017-11-01 | 2024-11-19 | 브리스톨-마이어스 스큅 컴퍼니 | 파르네소이드 x 수용체 조정제로서의 스피로시클릭 화합물 |
| CN108276307A (zh) * | 2018-01-17 | 2018-07-13 | 常熟浸大科技有限公司 | 3-氰基-4-烃氧基苯甲酸酯的合成方法 |
| EP3752152A1 (en) | 2018-02-12 | 2020-12-23 | Vertex Pharmaceuticals Incorporated | A method of treating pain |
| WO2019160882A1 (en) | 2018-02-13 | 2019-08-22 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| CN110156674A (zh) * | 2018-02-13 | 2019-08-23 | 中国科学院上海有机化学研究所 | 一种作为吲哚胺-2,3-双加氧酶抑制剂的螺环化合物 |
| WO2019204609A1 (en) | 2018-04-19 | 2019-10-24 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| CA3105748A1 (en) | 2018-07-09 | 2020-01-16 | Lieber Institute, Inc. | Pyridazine compounds for inhibiting nav1.8 |
| CA3105657A1 (en) | 2018-07-09 | 2020-01-16 | Lieber Institute, Inc. | Pyridine carboxamide compounds for inhibiting nav1.8 |
| BR112020026746A2 (pt) | 2018-07-13 | 2021-03-30 | Gilead Sciences, Inc. | Composto, composição farmacêutica, métodos para inibir pd-1, pd-l1 e/ou a interação de pd-1/pd-l1 e para tratar câncer, e, kit para tratar ou prevenir câncer ou uma doença ou condição. |
| CN112955435B (zh) | 2018-10-24 | 2024-09-06 | 吉利德科学公司 | Pd-1/pd-l1抑制剂 |
| WO2020146612A1 (en) | 2019-01-10 | 2020-07-16 | Vertex Pharmaceuticals Incorporated | Esters and carbamates as modulators of sodium channels |
| US12441703B2 (en) | 2019-01-10 | 2025-10-14 | Vertex Pharmaceuticals Incorporated | Carboxamides as modulators of sodium channels |
| WO2020176763A1 (en) | 2019-02-27 | 2020-09-03 | Vertex Pharmaceuticals Incorporated | Dosage form comprising prodrug of na 1.8 sodium channel inhibitor |
| WO2020219867A1 (en) | 2019-04-25 | 2020-10-29 | Vertex Pharmaceuticals Incorporated | Pyridone amide co-crystal compositions for the treatment of pain |
| DK4069691T3 (da) | 2019-12-06 | 2024-10-28 | Vertex Pharma | Substituerede tetrahydrofuraner som modulatorer af natriumkanaler |
| CA3221939A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels |
| JP2024520648A (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置換テトラヒドロフラン－２－カルボキサミド |
| EP4347033A1 (en) | 2021-06-04 | 2024-04-10 | Vertex Pharmaceuticals Incorporated | Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels |
| MA64853B1 (fr) | 2021-06-04 | 2025-11-28 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hétéro)aryl) tétrahydrofuran carboxamides utilisés en tant que modulateurs de canaux sodiques |
| JP2024520649A (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 | （２ｒ，３ｓ，４ｓ，５ｒ）－４－［［３－（３，４－ジフルオロ－２－メトキシ－フェニル）－４，５－ジメチル－５－（トリフルオロメチル）テトラヒドロフラン－２－カルボニル］アミノ］ピリジン－２－カルボキサミドを含む固体剤形及び投与レジメン |
| CN117794918A (zh) | 2021-06-04 | 2024-03-29 | 沃泰克斯药物股份有限公司 | 经取代的四氢呋喃类似物作为钠通道调节剂 |
| JP2025513455A (ja) | 2022-04-22 | 2025-04-24 | 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 | 疼痛の治療のためのヘテロアリール化合物 |
| EP4511115A1 (en) | 2022-04-22 | 2025-02-26 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| JP2025513452A (ja) | 2022-04-22 | 2025-04-24 | 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 | 疼痛の治療のためのヘテロアリール化合物 |
| AU2023255771A1 (en) | 2022-04-22 | 2024-10-31 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| EP4630405A1 (en) | 2022-12-06 | 2025-10-15 | Vertex Pharmaceuticals Incorporated | Process for the synthesis of substituted tetrahydrofuran modulators of sodium channels |
| WO2025090480A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| WO2025090465A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| WO2025090511A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Methods of preparing modulators of sodium channels and solid forms of the same for treating pain |
| WO2025090516A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Methods of preparing compounds for treating pain and solid forms thereof |
| WO2025122953A1 (en) | 2023-12-07 | 2025-06-12 | Vertex Pharmaceuticals Incorporated | Dosing regimens and formulations of suzetrigine for use in the treatment of acute and chronic pain |
| US20260001877A1 (en) | 2024-06-28 | 2026-01-01 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| WO2026013449A2 (en) | 2024-07-11 | 2026-01-15 | Sea4Us - Biotecnologia E Recursos Marinhos, Sa | Oxazolidone-derived compounds and their use in the treatment of chronic and acute pain |
| WO2026030525A1 (en) | 2024-07-31 | 2026-02-05 | Vertex Pharmaceuticals Incorporated | Zilvetrigine dosage forms and dosing regimens for treating pain |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US121652A (en) | 1871-12-05 | Improvement in picture-frame hangers | ||
| 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 |
| CA2233204A1 (en) * | 1995-09-29 | 1997-04-03 | Joseph A. Jakubowski | Spiro compounds as inhibitors of fibrinogen-dependent platelet aggregation |
| US20060052597A1 (en) * | 2002-10-22 | 2006-03-09 | Best Desmond J | Aryloxyalkylamine derivatives as h3 receptor ligands |
| US7576207B2 (en) * | 2006-04-06 | 2009-08-18 | Adolor Corporation | Spirocyclic heterocyclic derivatives and methods of their use |
| US20090012103A1 (en) * | 2007-07-05 | 2009-01-08 | Matthew Abelman | Substituted heterocyclic compounds |
| JP2011503112A (ja) * | 2007-11-13 | 2011-01-27 | 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 | 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 |
| JP2011503191A (ja) * | 2007-11-13 | 2011-01-27 | 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 | イオンチャネルのモジュレーターとしての複素環誘導体 |
| AU2009266979A1 (en) * | 2008-07-01 | 2010-01-07 | Vertex Pharmaceuticals Incorporated | Heterocyclic derivatives as modulators of ion channels |
| WO2010151815A2 (en) * | 2009-06-25 | 2010-12-29 | Abbott Laboratories | 3,9-diazaspiro[5,5]undecane amides and ureas and methods of use thereof |
| WO2010151595A1 (en) * | 2009-06-26 | 2010-12-29 | Schering Corporation | Pyrrolo-benzo-1,4-diazines useful as sodium channel blockers |
| AU2012217616B2 (en) * | 2011-02-18 | 2017-03-02 | Vertex Pharmaceuticals Incorporated | Chroman - spirocyclic piperidine amides as modulators of ion channels |
| US8828996B2 (en) * | 2011-03-14 | 2014-09-09 | Vertex Pharmaceuticals Incorporated | Morpholine-spirocyclic piperidine amides as modulators of ion channels |
-
2013
- 2013-01-15 US US14/372,353 patent/US9403839B2/en active Active
- 2013-01-15 JP JP2014552376A patent/JP6215230B2/ja active Active
- 2013-01-15 AU AU2013209958A patent/AU2013209958B2/en not_active Expired - Fee Related
- 2013-01-15 CA CA2863343A patent/CA2863343A1/en not_active Abandoned
- 2013-01-15 EP EP13700841.3A patent/EP2804868B1/en active Active
- 2013-01-15 ES ES13700841T patent/ES2631611T3/es active Active
- 2013-01-15 MX MX2014008591A patent/MX2014008591A/es unknown
- 2013-01-15 NZ NZ627259A patent/NZ627259A/en not_active IP Right Cessation
- 2013-01-15 WO PCT/US2013/021535 patent/WO2013109521A1/en not_active Ceased
- 2013-01-15 CN CN201380010104.4A patent/CN104136442B/zh not_active Expired - Fee Related
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