AU2016329201A1 - 11,13-modified saxitoxins for the treatment of pain - Google Patents
11,13-modified saxitoxins for the treatment of pain Download PDFInfo
- Publication number
- AU2016329201A1 AU2016329201A1 AU2016329201A AU2016329201A AU2016329201A1 AU 2016329201 A1 AU2016329201 A1 AU 2016329201A1 AU 2016329201 A AU2016329201 A AU 2016329201A AU 2016329201 A AU2016329201 A AU 2016329201A AU 2016329201 A1 AU2016329201 A1 AU 2016329201A1
- Authority
- AU
- Australia
- Prior art keywords
- halo
- optionally substituted
- 6alkyl
- aryl
- 6alkoxy
- 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.)
- Abandoned
Links
- 0 O=C(*1)C(CCCC2)C2C1=O Chemical compound O=C(*1)C(CCCC2)C2C1=O 0.000 description 8
- YJEPYGSJFPRFTO-DPWYMQNISA-O CC(C)c1cccc(C(N[C@@H](CN(C2(C([C@H](CN(C(CC3)=O)C3=O)N3)N4)NC4=[NH2+])C3=N)[C@H]2[O]#C)=O)c1 Chemical compound CC(C)c1cccc(C(N[C@@H](CN(C2(C([C@H](CN(C(CC3)=O)C3=O)N3)N4)NC4=[NH2+])C3=N)[C@H]2[O]#C)=O)c1 YJEPYGSJFPRFTO-DPWYMQNISA-O 0.000 description 1
- WNBXXSWQEZUHIX-UDXKHGJESA-N CCC(C(C([C@H](CO)N1)N2)(C=CC3)N3C1=C)C2=C Chemical compound CCC(C(C([C@H](CO)N1)N2)(C=CC3)N3C1=C)C2=C WNBXXSWQEZUHIX-UDXKHGJESA-N 0.000 description 1
- DRWVYTJCVOPKRH-QOHJYPKISA-N N=C(NC1C(CN2OCCC2=O)N2)N[C@]1(C([C@H](C1)OC(c3c(C(F)(F)F)ccc(C(F)(F)F)c3)=O)(O)O)N1C2=N Chemical compound N=C(NC1C(CN2OCCC2=O)N2)N[C@]1(C([C@H](C1)OC(c3c(C(F)(F)F)ccc(C(F)(F)F)c3)=O)(O)O)N1C2=N DRWVYTJCVOPKRH-QOHJYPKISA-N 0.000 description 1
- SPCKTUAGGFSMCU-CMFSEANSSA-N N=C(NC1[C@H](CN(C(CS2)=O)C2=O)N2)NC1(C(C(C1)OC(c3c(C(F)(F)F)ccc(C(F)(F)F)c3)=O)(O)O)N1C2=N Chemical compound N=C(NC1[C@H](CN(C(CS2)=O)C2=O)N2)NC1(C(C(C1)OC(c3c(C(F)(F)F)ccc(C(F)(F)F)c3)=O)(O)O)N1C2=N SPCKTUAGGFSMCU-CMFSEANSSA-N 0.000 description 1
- UKVACZPOQCMRIJ-CIEVUDSRSA-P [NH2+]=C(N[C@H]1[C@H](CN(C(CC2)=O)C2=O)N2)NC1([C@@H](CC1)[O]=O)N1C2=[NH2+] Chemical compound [NH2+]=C(N[C@H]1[C@H](CN(C(CC2)=O)C2=O)N2)NC1([C@@H](CC1)[O]=O)N1C2=[NH2+] UKVACZPOQCMRIJ-CIEVUDSRSA-P 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/14—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Anesthesiology (AREA)
- Cardiology (AREA)
- Psychology (AREA)
- Psychiatry (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562235412P | 2015-09-30 | 2015-09-30 | |
| US62/235,412 | 2015-09-30 | ||
| PCT/US2016/055050 WO2017059385A1 (en) | 2015-09-30 | 2016-09-30 | 11,13-modified saxitoxins for the treatment of pain |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2016329201A1 true AU2016329201A1 (en) | 2018-04-26 |
| AU2016329201A8 AU2016329201A8 (en) | 2018-05-17 |
Family
ID=57200084
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2016329201A Abandoned AU2016329201A1 (en) | 2015-09-30 | 2016-09-30 | 11,13-modified saxitoxins for the treatment of pain |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US10112953B2 (enExample) |
| EP (1) | EP3356370B1 (enExample) |
| JP (1) | JP2018534270A (enExample) |
| CN (1) | CN108473503A (enExample) |
| AU (1) | AU2016329201A1 (enExample) |
| CA (1) | CA3000708A1 (enExample) |
| ES (1) | ES2895155T3 (enExample) |
| IL (1) | IL258471A (enExample) |
| WO (1) | WO2017059385A1 (enExample) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2944549A1 (en) | 2014-04-09 | 2015-10-15 | Siteone Therapeutics, Inc. | 10',11'-modified saxitoxin useful for the treatment of pain |
| BR112019020111A2 (pt) * | 2017-03-29 | 2020-05-05 | Siteone Therapeutics Inc | saxitoxinas 11,13-modificadas para o tratamento de dor |
| JP2020515611A (ja) | 2017-03-29 | 2020-05-28 | サイトワン セラピューティクス, インコーポレイテッド | 疼痛の処置のための11,13−修飾サキシトキシン |
| US12162886B2 (en) | 2018-10-03 | 2024-12-10 | Siteone Therapeutics, Inc. | 11,13-modified saxitoxins for the treatment of pain |
| HUE069128T2 (hu) | 2019-12-06 | 2025-02-28 | Vertex Pharma | Szubsztituált tetrahidrofurán vegyületek mint nátriumcsatornák modulátorai |
| CA3188924A1 (en) * | 2020-08-14 | 2022-02-17 | Hassan Pajouhesh | Non-hydrated ketone inhibitors of nav1.7 for the treatment of pain |
| US20240294512A1 (en) | 2021-06-04 | 2024-09-05 | Vertex Pharmaceuticals Incorporated | Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels |
| US20240285596A1 (en) | 2021-06-04 | 2024-08-29 | 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 |
| US20240400544A1 (en) | 2021-06-04 | 2024-12-05 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels |
| 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 |
| AU2022284886A1 (en) | 2021-06-04 | 2023-11-30 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamides as modulators of sodium channels |
| US20240368135A1 (en) | 2021-06-04 | 2024-11-07 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels |
| CN113943243B (zh) * | 2021-10-14 | 2023-08-01 | 南开大学 | 一种用于同时鉴定和定量氨基酸的氟探针的制备与应用 |
| AU2023255558A1 (en) | 2022-04-22 | 2024-10-31 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| TW202404969A (zh) | 2022-04-22 | 2024-02-01 | 美商維泰克斯製藥公司 | 用於治療疼痛之雜芳基化合物 |
| JP2025513454A (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 |
| CN119522214A (zh) | 2022-04-22 | 2025-02-25 | 沃泰克斯药物股份有限公司 | 用于治疗疼痛的杂芳基化合物 |
| KR20250120351A (ko) | 2022-12-06 | 2025-08-08 | 버텍스 파마슈티칼스 인코포레이티드 | 나트륨 채널의 치환된 테트라하이드로푸란 조절제의 합성을 위한 방법 |
| 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 |
| 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 |
| 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 |
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| US9107925B2 (en) * | 2010-02-10 | 2015-08-18 | Phytotox Limited | Sodium channel blocker for treatment of loss of superficial sensitivity |
| EP3009427B1 (en) * | 2011-03-03 | 2019-12-18 | Zalicus Pharmaceuticals Ltd. | Benzimidazole inhibitors of the sodium channel |
| CA2944549A1 (en) | 2014-04-09 | 2015-10-15 | Siteone Therapeutics, Inc. | 10',11'-modified saxitoxin useful for the treatment of pain |
-
2016
- 2016-09-30 CA CA3000708A patent/CA3000708A1/en not_active Abandoned
- 2016-09-30 CN CN201680068998.6A patent/CN108473503A/zh active Pending
- 2016-09-30 AU AU2016329201A patent/AU2016329201A1/en not_active Abandoned
- 2016-09-30 EP EP16785597.2A patent/EP3356370B1/en active Active
- 2016-09-30 ES ES16785597T patent/ES2895155T3/es active Active
- 2016-09-30 JP JP2018517286A patent/JP2018534270A/ja not_active Withdrawn
- 2016-09-30 US US15/283,187 patent/US10112953B2/en active Active
- 2016-09-30 WO PCT/US2016/055050 patent/WO2017059385A1/en not_active Ceased
-
2018
- 2018-03-29 IL IL258471A patent/IL258471A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2017059385A8 (en) | 2017-11-02 |
| US20170233398A1 (en) | 2017-08-17 |
| ES2895155T3 (es) | 2022-02-17 |
| US10112953B2 (en) | 2018-10-30 |
| EP3356370A1 (en) | 2018-08-08 |
| JP2018534270A (ja) | 2018-11-22 |
| WO2017059385A1 (en) | 2017-04-06 |
| CN108473503A (zh) | 2018-08-31 |
| AU2016329201A8 (en) | 2018-05-17 |
| CA3000708A1 (en) | 2017-04-06 |
| EP3356370B1 (en) | 2021-08-18 |
| IL258471A (en) | 2018-05-31 |
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Legal Events
| Date | Code | Title | Description |
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| TH | Corrigenda |
Free format text: IN VOL 32 , NO 16 , PAGE(S) 2274 UNDER THE HEADING PCT APPLICATIONS THAT HAVE ENTERED THE NATIONAL PHASE - NAME INDEX UNDER THE NAME SITEONE THERAPEUTICS, INC.; THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY, APPLICATION NO. 2016329201, UNDER INID (72) ADD CO-INVENTOR MILJANICH, GEORGE |
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| MK5 | Application lapsed section 142(2)(e) - patent request and compl. specification not accepted |