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 (https=) | 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 (https=) |
| EP (1) | EP2804868B1 (https=) |
| JP (1) | JP6215230B2 (https=) |
| CN (1) | CN104136442B (https=) |
| AU (1) | AU2013209958B2 (https=) |
| CA (1) | CA2863343A1 (https=) |
| ES (1) | ES2631611T3 (https=) |
| MX (1) | MX2014008591A (https=) |
| NZ (1) | NZ627259A (https=) |
| WO (1) | WO2013109521A1 (https=) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA119147C2 (uk) | 2013-07-19 | 2019-05-10 | Вертекс Фармасьютікалз Інкорпорейтед | Сульфонаміди як модулятори натрієвих каналів |
| CA2931550C (en) | 2013-12-13 | 2023-09-26 | Vertex Pharmaceuticals Incorporated | Prodrugs of pyridone amides useful as modulators of sodium channels |
| BR102018007822A2 (pt) | 2017-04-20 | 2018-11-06 | Gilead Sciences, Inc. | composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição |
| EP3625214B1 (en) | 2017-05-16 | 2022-07-06 | Vertex Pharmaceuticals Incorporated | Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels |
| AU2018300150A1 (en) | 2017-07-11 | 2020-01-30 | Vertex Pharmaceuticals Incorporated | Carboxamides as modulators of sodium channels |
| CA3081424A1 (en) * | 2017-11-01 | 2019-05-09 | Bristol-Myers Squibb Company | Spirocyclic compounds as farnesoid x receptor modulators |
| 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 |
| US11529337B2 (en) | 2018-02-12 | 2022-12-20 | Vertex Pharmaceuticals Incorporated | Method of treating pain |
| 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 |
| CR20200347A (es) | 2018-02-13 | 2020-09-23 | Gilead Sciences Inc | Inhibidores pd-1/pd-l1 |
| TWI712412B (zh) | 2018-04-19 | 2020-12-11 | 美商基利科學股份有限公司 | Pd‐1/pd‐l1抑制劑 |
| AU2019302534B2 (en) | 2018-07-09 | 2024-10-03 | 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 |
| SG11202012425QA (en) | 2018-07-13 | 2021-01-28 | Gilead Sciences Inc | Pd-1/pd-l1 inhibitors |
| WO2020086556A1 (en) | 2018-10-24 | 2020-04-30 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| WO2020146682A1 (en) | 2019-01-10 | 2020-07-16 | Vertex Pharmaceuticals Incorporated | Carboxamides as modulators of sodium channels |
| US12440481B2 (en) | 2019-01-10 | 2025-10-14 | Vertex Pharmaceuticals Incorporated | Esters and carbamates 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 |
| BR112022010924A2 (pt) | 2019-12-06 | 2022-09-06 | Vertex Pharma | Tetra-hidrofuranos substituídos como moduladores de canais de sódio |
| HRP20260068T1 (hr) | 2021-06-04 | 2026-02-27 | Vertex Pharmaceuticals Incorporated | Čvrsti farmaceutski oblici i režimi doziranja koji obuhvaćaju (2r,3s,4s,5r)-4-[[3-(3,4-difluor-2-metoksifenil)-4,5-dimetil-5-(trifluormetil)tetrahidrofuran-2-karbonil]amino]piridin-2-karboksamid |
| WO2022256842A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels |
| SMT202500481T1 (it) | 2021-06-04 | 2026-01-12 | Vertex Pharma | N-(idrossialchil(etero)aril)tetraidrofuran carbossammidi come modulatori di canali del sodio |
| CA3221938A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran analogs as modulators of sodium channels |
| US20240400544A1 (en) | 2021-06-04 | 2024-12-05 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels |
| AU2022283934A1 (en) | 2021-06-04 | 2023-11-30 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels |
| WO2023205463A1 (en) | 2022-04-22 | 2023-10-26 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| US20230382910A1 (en) | 2022-04-22 | 2023-11-30 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| CA3257285A1 (en) | 2022-04-22 | 2023-10-26 | Vertex Pharmaceuticals Incorporated | HETEROARYL COMPOUNDS FOR PAIN RELIEF |
| CA3256248A1 (en) | 2022-04-22 | 2023-10-26 | Vertex Pharmaceuticals Incorporated | HETEROARYL COMPOUNDS FOR PAIN RELIEF |
| WO2024123815A1 (en) | 2022-12-06 | 2024-06-13 | Vertex Pharmaceuticals Incorporated | Process for the synthesis of substituted tetrahydrofuran modulators of sodium channels |
| 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 |
| WO2025090465A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| 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 |
| US20250186419A1 (en) | 2023-12-07 | 2025-06-12 | Vertex Pharmaceuticals Incorporated | Dosing regimens for treating 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 |
| WO1997011940A1 (en) * | 1995-09-29 | 1997-04-03 | Eli Lilly And Company | Spiro compounds as inhibitors of fibrinogen-dependent platelet aggregation |
| WO2004037800A1 (en) * | 2002-10-22 | 2004-05-06 | Glaxo Group Limited | Aryloxyalkylamine derivates 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 |
| WO2009064752A2 (en) * | 2007-11-13 | 2009-05-22 | Vertex Pharmaceuticals Incorporated | Heterocyclic derivatives as modulators of ion channels |
| US7994166B2 (en) * | 2007-11-13 | 2011-08-09 | Vertex Pharmaceuticals Incorporated | Pyrrolidinone benzenesulfonamide derivatives as modulators of ion channels for the treatment of pain |
| WO2010002956A2 (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 |
| MX2013009393A (es) * | 2011-02-18 | 2013-08-29 | Vertex Pharma | Piperidinamidas cromano-espirociclicas como moduladores de canales de iones. |
| CN103517910B (zh) * | 2011-03-14 | 2016-12-14 | 沃泰克斯药物股份有限公司 | 作为离子通道调节剂的吗啉-螺环哌啶酰胺 |
-
2013
- 2013-01-15 NZ NZ627259A patent/NZ627259A/en not_active IP Right Cessation
- 2013-01-15 EP EP13700841.3A patent/EP2804868B1/en active Active
- 2013-01-15 ES ES13700841T patent/ES2631611T3/es active Active
- 2013-01-15 US US14/372,353 patent/US9403839B2/en active Active
- 2013-01-15 MX MX2014008591A patent/MX2014008591A/es unknown
- 2013-01-15 CA CA2863343A patent/CA2863343A1/en not_active Abandoned
- 2013-01-15 JP JP2014552376A patent/JP6215230B2/ja active Active
- 2013-01-15 CN CN201380010104.4A patent/CN104136442B/zh not_active Expired - Fee Related
- 2013-01-15 WO PCT/US2013/021535 patent/WO2013109521A1/en not_active Ceased
- 2013-01-15 AU AU2013209958A patent/AU2013209958B2/en not_active Expired - Fee Related
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