CA3050853A1 - Heterocyclic spiro compounds as magl inhibitors - Google Patents
Heterocyclic spiro compounds as magl inhibitors Download PDFInfo
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- CA3050853A1 CA3050853A1 CA3050853A CA3050853A CA3050853A1 CA 3050853 A1 CA3050853 A1 CA 3050853A1 CA 3050853 A CA3050853 A CA 3050853A CA 3050853 A CA3050853 A CA 3050853A CA 3050853 A1 CA3050853 A1 CA 3050853A1
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- 229940068543 zelapar Drugs 0.000 description 1
- BPKIMPVREBSLAJ-QTBYCLKRSA-N ziconotide Chemical compound C([C@H]1C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H]2C(=O)N[C@@H]3C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@H](C(N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSSC2)C(N)=O)=O)CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC3)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(N1)=O)CCSC)[C@@H](C)O)C1=CC=C(O)C=C1 BPKIMPVREBSLAJ-QTBYCLKRSA-N 0.000 description 1
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- 150000003751 zinc Chemical class 0.000 description 1
- 239000011701 zinc Substances 0.000 description 1
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- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical compound [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 description 1
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- XZVHHLNLLVICFA-SNVBAGLBSA-N α-difluoromethyl-dopa Chemical compound FC(F)[C@](C(O)=O)(N)CC1=CC=C(O)C(O)=C1 XZVHHLNLLVICFA-SNVBAGLBSA-N 0.000 description 1
Classifications
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/10—Spiro-condensed systems
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- 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
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
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- A—HUMAN NECESSITIES
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- 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
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- 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
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
- C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
- C07D221/20—Spiro-condensed ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/10—Spiro-condensed systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
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- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
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- Neurology (AREA)
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- Epidemiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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| JP6832914B2 (ja) | 2015-07-31 | 2021-02-24 | ファイザー・インク | Ｍａｇｌ阻害薬としての１，１，１−トリフルオロ−３−ヒドロキシプロパン−２−イルカルバマート誘導体および１，１，１−トリフルオロ−４−ヒドロキシブタン−２−イルカルバマート誘導体 |
| JP7106462B2 (ja) | 2016-07-01 | 2022-07-26 | ジー１ セラピューティクス， インコーポレイテッド | Ｎ－（ヘテロアリール）－ピロロ［３，２－ｄ］ピリミジン－２－アミンの合成 |
| CA3050625C (en) * | 2017-01-20 | 2021-07-20 | Pfizer Inc. | 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives as magl inhibitors |
| US10927105B1 (en) | 2017-05-23 | 2021-02-23 | Lundbeck La Jolla Research Center, Inc. | Pyrazole MAGL inhibitors |
| CA3076477A1 (en) * | 2017-09-29 | 2019-04-04 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| US10662159B2 (en) * | 2017-11-22 | 2020-05-26 | Makscientific, Llc | ABHD6 and dual ABHD6/MGL inhibitors and their uses |
| CN111566105A (zh) | 2018-01-08 | 2020-08-21 | 豪夫迈·罗氏有限公司 | 作为MAGL抑制剂的八氢吡啶并[1,2-α]吡嗪类化合物 |
| US20210309669A1 (en) * | 2018-07-19 | 2021-10-07 | Pfizer Inc. | Heterocyclic Spiro Compounds As MAGL Inhibitors |
| EP3840756B1 (en) | 2018-08-24 | 2025-11-05 | Pharmacosmos Holding A/S | Improved synthesis of 1,4-diazaspiro[5.5]undecan-3-one |
| EP3856179A1 (en) * | 2018-09-28 | 2021-08-04 | Janssen Pharmaceutica N.V. | Monoacylglycerol lipase modulators |
| JP2022509206A (ja) * | 2018-11-28 | 2022-01-20 | ハー・ルンドベック・アクチエゼルスカベット | Ｍａｇｌ阻害剤による疾病の治療方法 |
| CN109485656A (zh) * | 2018-12-17 | 2019-03-19 | 上海药明康德新药开发有限公司 | 3-氧亚基-7-氧杂-2,10-二氮杂螺[4.6]十一烷-10-甲酸叔丁酯的制法 |
| MX2021008865A (es) * | 2019-01-25 | 2021-10-26 | H Lundbeck As | Inhibidores de magl para usarse para tratar enfermedades antecedentes. |
| CN114096545A (zh) * | 2019-07-09 | 2022-02-25 | 豪夫迈·罗氏有限公司 | 新杂环化合物 |
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| KR20220158785A (ko) * | 2020-03-26 | 2022-12-01 | 얀센 파마슈티카 엔.브이. | 모노아실글리세롤 리파아제 조절제로서의 아미노사이클로부탄 |
| WO2021228123A1 (zh) * | 2020-05-12 | 2021-11-18 | 北京广为医药科技有限公司 | 调节nmda受体活性的化合物、其药物组合物及用途 |
| ES2997114T3 (en) * | 2020-09-22 | 2025-02-14 | Janssen Pharmaceutica Nv | Cyclobutyl amide monoacylglycerol lipase modulators |
| US12029718B2 (en) | 2021-11-09 | 2024-07-09 | Cct Sciences, Llc | Process for production of essentially pure delta-9-tetrahydrocannabinol |
| US11434222B2 (en) * | 2020-11-13 | 2022-09-06 | H. Lundbeck A/S | MAGL inhibitors |
| WO2022135462A1 (zh) * | 2020-12-22 | 2022-06-30 | 鲁南制药集团股份有限公司 | Magl抑制剂的医药用途 |
| KR20240128870A (ko) | 2021-12-29 | 2024-08-27 | 싸이 테라퓨틱스, 인크. | 모노아실글리세롤 리파아제(magl) 억제 |
| AU2023264787A1 (en) * | 2022-05-04 | 2024-10-31 | H. Lundbeck A/S | Crystalline form of 1,1,1,3,3,3-hexafluoropropan-2-yl (s)-1-(pyridazin-3-ylcarbamoyl)-6 azaspiro[2.5]octane-6-carboxylate as monoacylglycerol lipase inhibitor. |
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| JP6832914B2 (ja) | 2015-07-31 | 2021-02-24 | ファイザー・インク | Ｍａｇｌ阻害薬としての１，１，１−トリフルオロ−３−ヒドロキシプロパン−２−イルカルバマート誘導体および１，１，１−トリフルオロ−４−ヒドロキシブタン−２−イルカルバマート誘導体 |
| US10030020B2 (en) * | 2016-05-12 | 2018-07-24 | Abide Therapeutics, Inc. | Spirocycle compounds and methods of making and using same |
-
2018
- 2018-01-09 CN CN201880007992.7A patent/CN110198944A/zh active Pending
- 2018-01-09 BR BR112019014099-9A patent/BR112019014099A2/pt not_active Application Discontinuation
- 2018-01-09 RU RU2019123020A patent/RU2726631C1/ru active
- 2018-01-09 CA CA3050853A patent/CA3050853A1/en not_active Abandoned
- 2018-01-09 EP EP18701578.9A patent/EP3571202B1/en active Active
- 2018-01-09 KR KR1020197021451A patent/KR20190097242A/ko not_active Withdrawn
- 2018-01-09 AU AU2018208848A patent/AU2018208848A1/en not_active Abandoned
- 2018-01-09 WO PCT/IB2018/050128 patent/WO2018134698A1/en not_active Ceased
- 2018-01-09 MX MX2019008690A patent/MX2019008690A/es unknown
- 2018-01-09 SG SG11201906427QA patent/SG11201906427QA/en unknown
- 2018-01-09 JP JP2019538585A patent/JP2020506903A/ja not_active Withdrawn
- 2018-01-18 TW TW107101775A patent/TWI665199B/zh not_active IP Right Cessation
- 2018-01-22 US US15/876,698 patent/US20180208608A1/en not_active Abandoned
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2019
- 2019-06-03 US US16/429,678 patent/US10858373B2/en active Active
- 2019-07-01 IL IL267781A patent/IL267781A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR20190097242A (ko) | 2019-08-20 |
| WO2018134698A1 (en) | 2018-07-26 |
| EP3571202B1 (en) | 2021-06-30 |
| IL267781A (en) | 2019-09-26 |
| US20190292203A1 (en) | 2019-09-26 |
| TWI665199B (zh) | 2019-07-11 |
| TW201838995A (zh) | 2018-11-01 |
| MX2019008690A (es) | 2019-09-18 |
| JP2020506903A (ja) | 2020-03-05 |
| US20180208608A1 (en) | 2018-07-26 |
| RU2726631C1 (ru) | 2020-07-15 |
| BR112019014099A2 (pt) | 2020-02-11 |
| AU2018208848A1 (en) | 2019-07-18 |
| SG11201906427QA (en) | 2019-08-27 |
| EP3571202A1 (en) | 2019-11-27 |
| US10858373B2 (en) | 2020-12-08 |
| CN110198944A (zh) | 2019-09-03 |
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| FZDE | Discontinued |
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| FZDE | Discontinued |
Effective date: 20221220 |