JP2020515611A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2020515611A5 JP2020515611A5 JP2019553573A JP2019553573A JP2020515611A5 JP 2020515611 A5 JP2020515611 A5 JP 2020515611A5 JP 2019553573 A JP2019553573 A JP 2019553573A JP 2019553573 A JP2019553573 A JP 2019553573A JP 2020515611 A5 JP2020515611 A5 JP 2020515611A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- halo
- optionally substituted
- alkoxy
- aryl
- 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.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims description 279
- 125000003545 alkoxy group Chemical group 0.000 claims description 107
- 125000003118 aryl group Chemical group 0.000 claims description 101
- 150000001875 compounds Chemical class 0.000 claims description 77
- 229910052739 hydrogen Inorganic materials 0.000 claims description 74
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical group C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims description 68
- 239000001257 hydrogen Substances 0.000 claims description 68
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 62
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 57
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 56
- 125000005138 alkoxysulfonyl group Chemical group 0.000 claims description 50
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 50
- -1 nitro, amino Chemical group 0.000 claims description 49
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 42
- 235000010290 biphenyl Nutrition 0.000 claims description 36
- 239000004305 biphenyl Substances 0.000 claims description 34
- 125000001072 heteroaryl group Chemical group 0.000 claims description 34
- 125000000623 heterocyclic group Chemical group 0.000 claims description 28
- 208000002193 Pain Diseases 0.000 claims description 26
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 26
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 26
- 125000000033 alkoxyamino group Chemical group 0.000 claims description 25
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 24
- 239000000203 mixture Substances 0.000 claims description 21
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims description 20
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims description 19
- 125000004738 (C1-C6) alkyl sulfinyl group Chemical group 0.000 claims description 17
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims description 17
- 238000000034 method Methods 0.000 claims description 13
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 12
- 150000003839 salts Chemical class 0.000 claims description 11
- 239000012453 solvate Substances 0.000 claims description 9
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims description 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 8
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims description 8
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims description 6
- 150000002431 hydrogen Chemical class 0.000 claims description 6
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims description 4
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims description 4
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims description 4
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims description 4
- 206010011224 Cough Diseases 0.000 claims description 4
- 206010015958 Eye pain Diseases 0.000 claims description 4
- 241000124008 Mammalia Species 0.000 claims description 4
- 208000003251 Pruritus Diseases 0.000 claims description 4
- 230000001154 acute effect Effects 0.000 claims description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
- 208000004296 neuralgia Diseases 0.000 claims description 4
- 229910052757 nitrogen Inorganic materials 0.000 claims description 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 4
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 206010058019 Cancer Pain Diseases 0.000 claims description 2
- 208000000094 Chronic Pain Diseases 0.000 claims description 2
- 208000006561 Cluster Headache Diseases 0.000 claims description 2
- 206010061788 Corneal infection Diseases 0.000 claims description 2
- 208000028006 Corneal injury Diseases 0.000 claims description 2
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims description 2
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims description 2
- 206010013774 Dry eye Diseases 0.000 claims description 2
- 201000009273 Endometriosis Diseases 0.000 claims description 2
- 206010015150 Erythema Diseases 0.000 claims description 2
- 208000001640 Fibromyalgia Diseases 0.000 claims description 2
- 208000010412 Glaucoma Diseases 0.000 claims description 2
- 208000007514 Herpes zoster Diseases 0.000 claims description 2
- 208000019695 Migraine disease Diseases 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 208000004550 Postoperative Pain Diseases 0.000 claims description 2
- 208000027520 Somatoform disease Diseases 0.000 claims description 2
- 239000000654 additive Substances 0.000 claims description 2
- 230000000996 additive effect Effects 0.000 claims description 2
- 206010003246 arthritis Diseases 0.000 claims description 2
- 125000002047 benzodioxolyl group Chemical group O1OC(C2=C1C=CC=C2)* 0.000 claims description 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 2
- 150000004074 biphenyls Chemical class 0.000 claims description 2
- 125000003016 chromanyl group Chemical group O1C(CCC2=CC=CC=C12)* 0.000 claims description 2
- 230000001684 chronic effect Effects 0.000 claims description 2
- 208000018912 cluster headache syndrome Diseases 0.000 claims description 2
- 125000004856 decahydroquinolinyl group Chemical group N1(CCCC2CCCCC12)* 0.000 claims description 2
- 231100000321 erythema Toxicity 0.000 claims description 2
- 125000003983 fluorenyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3CC12)* 0.000 claims description 2
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims description 2
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims description 2
- 208000028867 ischemia Diseases 0.000 claims description 2
- 206010027599 migraine Diseases 0.000 claims description 2
- 201000006417 multiple sclerosis Diseases 0.000 claims description 2
- 125000001624 naphthyl group Chemical group 0.000 claims description 2
- 201000008482 osteoarthritis Diseases 0.000 claims description 2
- 208000027753 pain disease Diseases 0.000 claims description 2
- 230000001314 paroxysmal effect Effects 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000003386 piperidinyl group Chemical group 0.000 claims description 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 2
- 210000003497 sciatic nerve Anatomy 0.000 claims description 2
- 238000001356 surgical procedure Methods 0.000 claims description 2
- 208000011580 syndromic disease Diseases 0.000 claims description 2
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 claims description 2
- 125000005843 halogen group Chemical group 0.000 claims 26
- 102000016913 Voltage-Gated Sodium Channels Human genes 0.000 claims 1
- 108010053752 Voltage-Gated Sodium Channels Proteins 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 210000003901 trigeminal nerve Anatomy 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 description 26
- 0 C*([C@](C1)OC(c2ccccc2)=*)C(*2)(C([C@](CCC(O)=O)N3)NC2=[N+])N1C3=N Chemical compound C*([C@](C1)OC(c2ccccc2)=*)C(*2)(C([C@](CCC(O)=O)N3)NC2=[N+])N1C3=N 0.000 description 9
- XCLVGMYWSJRLDK-YJQWLVMKSA-O CC(C(NC(C1N2)C(N(C)C)=O)N(C[C@@H](C3O)OC(c4ccccc4)=O)C13C(C)=CC2=[NH2+])=[IH] Chemical compound CC(C(NC(C1N2)C(N(C)C)=O)N(C[C@@H](C3O)OC(c4ccccc4)=O)C13C(C)=CC2=[NH2+])=[IH] XCLVGMYWSJRLDK-YJQWLVMKSA-O 0.000 description 1
- 108010052164 Sodium Channels Proteins 0.000 description 1
- 102000018674 Sodium Channels Human genes 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 201000001119 neuropathy Diseases 0.000 description 1
- 230000007823 neuropathy Effects 0.000 description 1
- 208000033808 peripheral neuropathy Diseases 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 208000020049 trigeminal nerve disease Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762478519P | 2017-03-29 | 2017-03-29 | |
| US62/478,519 | 2017-03-29 | ||
| PCT/US2018/025304 WO2018183782A1 (en) | 2017-03-29 | 2018-03-29 | 11,13-modified saxitoxins for the treatment of pain |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020515611A JP2020515611A (ja) | 2020-05-28 |
| JP2020515611A5 true JP2020515611A5 (enExample) | 2021-05-06 |
Family
ID=62002497
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019553573A Pending JP2020515611A (ja) | 2017-03-29 | 2018-03-29 | 疼痛の処置のための１１，１３−修飾サキシトキシン |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US11279706B2 (enExample) |
| EP (1) | EP3601290B1 (enExample) |
| JP (1) | JP2020515611A (enExample) |
| CN (1) | CN110914276A (enExample) |
| WO (1) | WO2018183782A1 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US20240400544A1 (en) | 2021-06-04 | 2024-12-05 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs 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 |
| AU2022284886A1 (en) | 2021-06-04 | 2023-11-30 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamides 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 |
| US20240294512A1 (en) | 2021-06-04 | 2024-09-05 | Vertex Pharmaceuticals Incorporated | Hydroxy and (halo)alkoxy substituted tetrahydrofurans 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 |
| AU2023255558A1 (en) | 2022-04-22 | 2024-10-31 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
Family Cites Families (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3536809A (en) | 1969-02-17 | 1970-10-27 | Alza Corp | Medication method |
| US3598123A (en) | 1969-04-01 | 1971-08-10 | Alza Corp | Bandage for administering drugs |
| US3957996A (en) | 1971-12-08 | 1976-05-18 | Astra Pharmaceutical Products, Inc. | Pharmaceutical local anesthetic compositions |
| US3845770A (en) | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| US3916899A (en) | 1973-04-25 | 1975-11-04 | Alza Corp | Osmotic dispensing device with maximum and minimum sizes for the passageway |
| US4008719A (en) | 1976-02-02 | 1977-02-22 | Alza Corporation | Osmotic system having laminar arrangement for programming delivery of active agent |
| KR890002631B1 (ko) | 1984-10-04 | 1989-07-21 | 몬산토 캄파니 | 생물학적으로 활성인 소마토트로핀을 지속적으로 유리하는 조성물 |
| IE58110B1 (en) | 1984-10-30 | 1993-07-14 | Elan Corp Plc | Controlled release powder and process for its preparation |
| US5073543A (en) | 1988-07-21 | 1991-12-17 | G. D. Searle & Co. | Controlled release formulations of trophic factors in ganglioside-lipsome vehicle |
| IT1229203B (it) | 1989-03-22 | 1991-07-25 | Bioresearch Spa | Impiego di acido 5 metiltetraidrofolico, di acido 5 formiltetraidrofolico e dei loro sali farmaceuticamente accettabili per la preparazione di composizioni farmaceutiche in forma a rilascio controllato attive nella terapia dei disturbi mentali organici e composizioni farmaceutiche relative. |
| PH30995A (en) | 1989-07-07 | 1997-12-23 | Novartis Inc | Sustained release formulations of water soluble peptides. |
| US5120548A (en) | 1989-11-07 | 1992-06-09 | Merck & Co., Inc. | Swelling modulated polymeric drug delivery device |
| US5733566A (en) | 1990-05-15 | 1998-03-31 | Alkermes Controlled Therapeutics Inc. Ii | Controlled release of antiparasitic agents in animals |
| US5580578A (en) | 1992-01-27 | 1996-12-03 | Euro-Celtique, S.A. | Controlled release formulations coated with aqueous dispersions of acrylic polymers |
| TW333456B (en) | 1992-12-07 | 1998-06-11 | Takeda Pharm Ind Co Ltd | A pharmaceutical composition of sustained-release preparation the invention relates to a pharmaceutical composition of sustained-release preparation which comprises a physiologically active peptide. |
| US5591767A (en) | 1993-01-25 | 1997-01-07 | Pharmetrix Corporation | Liquid reservoir transdermal patch for the administration of ketorolac |
| US6087324A (en) | 1993-06-24 | 2000-07-11 | Takeda Chemical Industries, Ltd. | Sustained-release preparation |
| IT1270594B (it) | 1994-07-07 | 1997-05-07 | Recordati Chem Pharm | Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida |
| CA2224381A1 (en) | 1995-06-27 | 1997-01-16 | Takeda Chemical Industries, Ltd. | Method of producing sustained-release preparation |
| TW448055B (en) | 1995-09-04 | 2001-08-01 | Takeda Chemical Industries Ltd | Method of production of sustained-release preparation |
| JP2909418B2 (ja) | 1995-09-18 | 1999-06-23 | 株式会社資生堂 | 薬物の遅延放出型マイクロスフイア |
| US5980945A (en) | 1996-01-16 | 1999-11-09 | Societe De Conseils De Recherches Et D'applications Scientifique S.A. | Sustained release drug formulations |
| US6264970B1 (en) | 1996-06-26 | 2001-07-24 | Takeda Chemical Industries, Ltd. | Sustained-release preparation |
| US6419961B1 (en) | 1996-08-29 | 2002-07-16 | Takeda Chemical Industries, Ltd. | Sustained release microcapsules of a bioactive substance and a biodegradable polymer |
| CA2217134A1 (en) | 1996-10-09 | 1998-04-09 | Sumitomo Pharmaceuticals Co., Ltd. | Sustained release formulation |
| CA2219698C (en) | 1996-10-31 | 2007-09-04 | Takeda Chemical Industries, Ltd. | Sustained-release preparation |
| KR20000057693A (ko) | 1996-12-20 | 2000-09-25 | 다케다 야쿠힌 고교 가부시키가이샤 | 지효성 제제의 제조 방법 |
| EP0857972A1 (en) | 1997-01-24 | 1998-08-12 | Tepual, S.A. | Immunoassay for the detection and quantitation of toxins causing paralytic shellfish poisoning |
| US5891474A (en) | 1997-01-29 | 1999-04-06 | Poli Industria Chimica, S.P.A. | Time-specific controlled release dosage formulations and method of preparing same |
| CN1081034C (zh) | 1997-03-07 | 2002-03-20 | 潘心富 | 一种双胍基氢化嘌呤环类化合物的戒毒药 |
| US6030974A (en) | 1997-04-02 | 2000-02-29 | The Regents Of The University Of California | Method of anesthesia |
| US6326020B1 (en) | 1997-05-16 | 2001-12-04 | Children's Medical Center Corporation | Local anesthetic formulations |
| US6613358B2 (en) | 1998-03-18 | 2003-09-02 | Theodore W. Randolph | Sustained-release composition including amorphous polymer |
| KR19990085365A (ko) | 1998-05-16 | 1999-12-06 | 허영섭 | 지속적으로 약물 조절방출이 가능한 생분해성 고분자 미립구 및그 제조방법 |
| US6248363B1 (en) | 1999-11-23 | 2001-06-19 | Lipocine, Inc. | Solid carriers for improved delivery of active ingredients in pharmaceutical compositions |
| CN1382443A (zh) | 2001-04-25 | 2002-12-04 | 威克斯医疗仪器有限公司 | 钠离子通道阻断剂在制备用于局部神经麻醉或镇痛的药物中的应用 |
| JP2003012699A (ja) | 2001-07-04 | 2003-01-15 | Japan Science & Technology Corp | 抗麻酔性貝毒抗体の製法、新規抗体、該抗体を用いるｅｌｉｓａ測定キット、該製法による系標識毒標品 |
| CN1194693C (zh) | 2002-01-11 | 2005-03-30 | 中国科学院海洋研究所 | 麻痹性贝毒毒素作为制备疗治疼痛病症药物的应用 |
| WO2004050034A2 (en) | 2002-12-02 | 2004-06-17 | Massachusetts Institute Of Technology | Prolonged suppression of electrical activity in excitable tissues |
| AU2003901897A0 (en) | 2003-02-12 | 2003-05-08 | Australian Institute Of Marine Science | Conjugate |
| US20050137177A1 (en) | 2003-12-18 | 2005-06-23 | Shafer Steven L. | Ester combination local anesthetic |
| BRPI0510761A (pt) | 2004-05-07 | 2007-11-20 | Phytotox Ltd | métodos de tratar um paciente afligido com pelo menos uma enfermidade e de reduzir ou eliminar rugas |
| EP1796676B1 (en) | 2004-05-07 | 2016-03-09 | Phytotox Limited | Transdermal administration of phycotoxins |
| EP1799220A1 (en) * | 2004-09-22 | 2007-06-27 | Laboratorios del Dr. Esteve S.A. | Tetrodotoxin and its derivatives for the treatment of peripheral-nervously derived neuropathic pain |
| RU2277097C1 (ru) | 2004-12-27 | 2006-05-27 | Институт Молекулярной Генетики Российской Академии Наук (Имг Ран) | Высокомеченный тритием дигидрохлорид [3h]сакситоксина |
| CN101513408A (zh) | 2008-02-19 | 2009-08-26 | 熊平 | 双胍基嘌呤环类衍生物制备提高抗癌药药效的新应用 |
| WO2010019963A2 (en) | 2008-08-15 | 2010-02-18 | Georgetown University | Na channels, disease, and related assays and compositions |
| CA2760946C (en) | 2009-05-07 | 2019-06-25 | The Board Of Trustees Of The Leland Stanford Junior University | Methods and compositions for studying, imaging, and treating pain |
| 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 |
| CA3000708A1 (en) | 2015-09-30 | 2017-04-06 | Siteone Therapeutics, Inc. | 11,13-modified saxitoxins for the treatment of pain |
| 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 |
| BR112019020111A2 (pt) | 2017-03-29 | 2020-05-05 | Siteone Therapeutics Inc | saxitoxinas 11,13-modificadas para o tratamento de dor |
| US12162886B2 (en) | 2018-10-03 | 2024-12-10 | Siteone Therapeutics, Inc. | 11,13-modified saxitoxins for the treatment of pain |
-
2018
- 2018-03-29 JP JP2019553573A patent/JP2020515611A/ja active Pending
- 2018-03-29 EP EP18718368.6A patent/EP3601290B1/en active Active
- 2018-03-29 CN CN201880035538.2A patent/CN110914276A/zh active Pending
- 2018-03-29 US US16/499,201 patent/US11279706B2/en active Active
- 2018-03-29 WO PCT/US2018/025304 patent/WO2018183782A1/en not_active Ceased
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2020515611A5 (enExample) | ||
| JP2020515610A5 (enExample) | ||
| AU2023201821B2 (en) | Modulators of the integrated stress pathway | |
| TWI877863B (zh) | 整合應激路徑之前藥調節劑 | |
| CN112154142B (zh) | 整合应激通路的调节剂 | |
| AU2018358157B2 (en) | Modulators of the integrated stress pathway | |
| RU2014145544A (ru) | Солевая форма ингибитора гистон-метилтрансферазы ezh2 человека | |
| CN112218869A (zh) | 整合应激通路的调节剂 | |
| JP2015512942A5 (enExample) | ||
| JP2017504576A5 (enExample) | ||
| CN112204006A (zh) | 整合应激通路的调节剂 | |
| JP2011509309A5 (enExample) | ||
| JP2018534270A5 (enExample) | ||
| JP2010514758A5 (enExample) | ||
| RU2016122731A (ru) | Функционализированные и замещенные индолы в качестве противораковых агентов | |
| RU2007147344A (ru) | Новые производные 2-азетидинона для лечения гиперлипидемических заболеваний | |
| JPWO2022036297A5 (enExample) | ||
| JP2017534657A (ja) | 新型シチジン誘導体およびその適用 | |
| RU2017131354A (ru) | Замещенные амино шестичленные насыщенные гетероалициклы в качестве ингибиторов dpp-iv длительного действия | |
| JPWO2019214634A5 (enExample) | ||
| JP2007517007A5 (enExample) | ||
| CN115867542A (zh) | 新型苯并咪唑化合物 | |
| JP2017532299A5 (enExample) | ||
| JP2005511643A5 (enExample) | ||
| RU2824500C2 (ru) | Пролекарственные модуляторы интегрированного пути стресса |