CN109982699A - 一种mor激动剂与kor激动剂的药物组合物及其用途 - Google Patents
一种mor激动剂与kor激动剂的药物组合物及其用途 Download PDFInfo
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- CN109982699A CN109982699A CN201880004339.5A CN201880004339A CN109982699A CN 109982699 A CN109982699 A CN 109982699A CN 201880004339 A CN201880004339 A CN 201880004339A CN 109982699 A CN109982699 A CN 109982699A
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- A—HUMAN NECESSITIES
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/45—Non condensed piperidines, e.g. piperocaine having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/07—Tetrapeptides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Abstract
一种μ阿片受体(MOR)激动剂与κ阿片受体(KOR)激动剂联合在制备缓解和/或治疗疼痛的药物中的用途。所述MOR激动剂选自如通式(I)所示化合物,或其互变异构体、内消旋体、外消旋体、对映异构体、非对映异构体或其混合物形式,或其可药用的盐。一种含有所述MOR激动剂与KOR激动剂的药物组合物。
Description
PCT国内申请,说明书已公开。
Claims (14)
- PCT国内申请,权利要求书已公开。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710242435 | 2017-04-14 | ||
| CN2017102424350 | 2017-04-14 | ||
| PCT/CN2018/082912 WO2018188641A1 (zh) | 2017-04-14 | 2018-04-13 | 一种mor激动剂与kor激动剂的药物组合物及其用途 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN109982699A true CN109982699A (zh) | 2019-07-05 |
Family
ID=63792284
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201880004339.5A Pending CN109982699A (zh) | 2017-04-14 | 2018-04-13 | 一种mor激动剂与kor激动剂的药物组合物及其用途 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20200054594A1 (zh) |
| EP (1) | EP3610874A4 (zh) |
| JP (1) | JP2020516591A (zh) |
| KR (1) | KR20190133047A (zh) |
| CN (1) | CN109982699A (zh) |
| AU (1) | AU2018251118A1 (zh) |
| BR (1) | BR112019020691A2 (zh) |
| CA (1) | CA3058272A1 (zh) |
| MX (1) | MX388643B (zh) |
| TW (1) | TW201836606A (zh) |
| WO (1) | WO2018188641A1 (zh) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111065390B (zh) * | 2017-12-06 | 2023-01-24 | 江苏恒瑞医药股份有限公司 | Kor激动剂与mor激动剂联合在制备治疗疼痛的药物中的用途 |
| WO2019205983A1 (zh) * | 2018-04-28 | 2019-10-31 | 四川科伦博泰生物医药股份有限公司 | 氧杂螺环类化合物及其制备方法和用途 |
| WO2020147848A1 (zh) * | 2019-01-17 | 2020-07-23 | 上海海雁医药科技有限公司 | 三环取代的氧杂螺环衍生物、其制法与医药上的用途 |
| CN111662284B (zh) * | 2019-03-06 | 2021-08-10 | 上海海雁医药科技有限公司 | 双杂环取代的氧杂螺环衍生物、其制法与医药上的用途 |
| CN114615976A (zh) * | 2019-08-07 | 2022-06-10 | 人福医药美国公司 | κ阿片受体肽酰胺激动剂 |
| CN112789276B (zh) * | 2019-08-14 | 2024-07-30 | 上海海雁医药科技有限公司 | 镇痛化合物、其制法与医药上的用途 |
| CN112552374B (zh) * | 2019-09-10 | 2024-06-04 | 西藏海思科制药有限公司 | 一种肽酰胺类化合物及其中间体的制备方法 |
| KR102847070B1 (ko) * | 2020-01-17 | 2025-08-14 | 상하이 하이옌 파마슈티컬 테크놀로지 컴퍼니, 리미티드 | 아자비시클릭 치환된 옥사스피로 유도체, 이의 제조 방법 및 의학적 용도 |
| CN118221680A (zh) * | 2020-01-17 | 2024-06-21 | 上海海雁医药科技有限公司 | 光学纯的氧杂螺环取代的吡咯并吡唑衍生物、其制法与医药上的用途 |
| CN113214264B (zh) * | 2020-01-21 | 2022-08-09 | 上海海雁医药科技有限公司 | 二氢吡咯并五元杂芳基取代的氧杂螺环衍生物、其制法与医药上的用途 |
| CN115884963A (zh) | 2020-06-25 | 2023-03-31 | 人福医药美国公司 | 用于治疗医学病症的肽 |
| US20240156781A1 (en) * | 2021-03-04 | 2024-05-16 | Socium Inc. | Cancer therapeutic agent |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN101627049A (zh) * | 2006-11-10 | 2010-01-13 | 卡拉治疗学股份有限公司 | 合成酞酰胺 |
| CN103702561A (zh) * | 2011-03-23 | 2014-04-02 | 特维娜有限公司 | 阿片样物质受体配体以及使用和制备其的方法 |
| WO2017063509A1 (zh) * | 2015-10-15 | 2017-04-20 | 江苏恒瑞医药股份有限公司 | 氧杂螺环类衍生物、其制备方法及其在医药上的应用 |
| CN107098871A (zh) * | 2016-02-23 | 2017-08-29 | 江苏恒瑞医药股份有限公司 | 苯基丙酰胺类衍生物、其制备方法及其在医药上的应用 |
| CN110049980A (zh) * | 2017-04-14 | 2019-07-23 | 江苏恒瑞医药股份有限公司 | 一种阿片样物质受体(mor)激动剂的盐、其富马酸盐i晶型及制备方法 |
| CN111065390A (zh) * | 2017-12-06 | 2020-04-24 | 江苏恒瑞医药股份有限公司 | Kor激动剂与mor激动剂联合在制备治疗疼痛的药物中的用途 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100648133B1 (ko) | 2005-04-25 | 2006-11-23 | 일동제약주식회사 | 펩티드 데포르밀라제 저해제로서 신규의 히드록사믹 산유도체 및 그 제조방법 |
| US8906859B2 (en) | 2006-11-10 | 2014-12-09 | Cera Therapeutics, Inc. | Uses of kappa opioid synthetic peptide amides |
| US7842662B2 (en) | 2006-11-10 | 2010-11-30 | Cara Therapeutics, Inc. | Synthetic peptide amide dimers |
| US9805310B2 (en) * | 2012-03-04 | 2017-10-31 | Adam Jeffries | Utilizing spatial statistical models to reduce data redundancy and entropy |
| US20160250277A1 (en) | 2013-10-28 | 2016-09-01 | Cara Therapeutics, Inc. | Peripheral kappa opioid receptor agonists for preventing, inhibiting or treating nausea and vomiting |
| WO2016073443A2 (en) | 2014-11-05 | 2016-05-12 | Cara Therapeutics, Inc. | Peripheral kappa opioid receptor agonists for hard tissue pain |
| WO2016187537A1 (en) * | 2015-05-21 | 2016-11-24 | The Arizona Board Of Regents On Behalf Of The University Of Arizona | Multifunctional opioid receptor ligands and methods of treating pain |
-
2018
- 2018-04-13 KR KR1020197032604A patent/KR20190133047A/ko not_active Withdrawn
- 2018-04-13 US US16/499,931 patent/US20200054594A1/en not_active Abandoned
- 2018-04-13 CA CA3058272A patent/CA3058272A1/en not_active Abandoned
- 2018-04-13 AU AU2018251118A patent/AU2018251118A1/en not_active Abandoned
- 2018-04-13 CN CN201880004339.5A patent/CN109982699A/zh active Pending
- 2018-04-13 WO PCT/CN2018/082912 patent/WO2018188641A1/zh not_active Ceased
- 2018-04-13 TW TW107112741A patent/TW201836606A/zh unknown
- 2018-04-13 MX MX2019011904A patent/MX388643B/es unknown
- 2018-04-13 BR BR112019020691-4A patent/BR112019020691A2/pt not_active Application Discontinuation
- 2018-04-13 JP JP2019553307A patent/JP2020516591A/ja not_active Ceased
- 2018-04-13 EP EP18783681.2A patent/EP3610874A4/en not_active Withdrawn
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101627049A (zh) * | 2006-11-10 | 2010-01-13 | 卡拉治疗学股份有限公司 | 合成酞酰胺 |
| CN103702561A (zh) * | 2011-03-23 | 2014-04-02 | 特维娜有限公司 | 阿片样物质受体配体以及使用和制备其的方法 |
| WO2017063509A1 (zh) * | 2015-10-15 | 2017-04-20 | 江苏恒瑞医药股份有限公司 | 氧杂螺环类衍生物、其制备方法及其在医药上的应用 |
| CN107098871A (zh) * | 2016-02-23 | 2017-08-29 | 江苏恒瑞医药股份有限公司 | 苯基丙酰胺类衍生物、其制备方法及其在医药上的应用 |
| CN110049980A (zh) * | 2017-04-14 | 2019-07-23 | 江苏恒瑞医药股份有限公司 | 一种阿片样物质受体(mor)激动剂的盐、其富马酸盐i晶型及制备方法 |
| CN111065390A (zh) * | 2017-12-06 | 2020-04-24 | 江苏恒瑞医药股份有限公司 | Kor激动剂与mor激动剂联合在制备治疗疼痛的药物中的用途 |
Non-Patent Citations (2)
| Title |
|---|
| XIAO-TAO CHEN等: "Structure−Activity Relationships and Discovery of a G Protein Biased μ Opioid Receptor Ligand, [(3-Methoxythiophen-2-yl)methyl]({2-[(9R)‑9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the Treatment of Acute Severe Pain", 《J. MED. CHEM.》 * |
| XIN LI等: "Discovery of SHR9352: A Highly Potent G Protein-Biased μ‑Opioid Receptor Agonist", 《ACS OMEGA》 * |
Also Published As
| Publication number | Publication date |
|---|---|
| CA3058272A1 (en) | 2018-10-18 |
| US20200054594A1 (en) | 2020-02-20 |
| EP3610874A4 (en) | 2021-01-06 |
| AU2018251118A1 (en) | 2019-10-17 |
| MX2019011904A (es) | 2019-11-25 |
| EP3610874A1 (en) | 2020-02-19 |
| JP2020516591A (ja) | 2020-06-11 |
| AU2018251118A8 (en) | 2019-10-31 |
| BR112019020691A2 (pt) | 2020-05-12 |
| MX388643B (es) | 2025-03-20 |
| TW201836606A (zh) | 2018-10-16 |
| KR20190133047A (ko) | 2019-11-29 |
| WO2018188641A1 (zh) | 2018-10-18 |
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