CA3050853A1 - Heterocyclic spiro compounds as magl inhibitors - Google Patents
Heterocyclic spiro compounds as magl inhibitors Download PDFInfo
- Publication number
- 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
- Authority
- CA
- Canada
- Prior art keywords
- formula
- alkyl
- compound
- disease
- pharmaceutically acceptable
- 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
Classifications
-
- C—CHEMISTRY; METALLURGY
- 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
-
- 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
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
-
- 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
-
- 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
- A61K31/4439—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
-
- 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
- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
-
- 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
Landscapes
- 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)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- 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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762449242P | 2017-01-23 | 2017-01-23 | |
| US62/449,242 | 2017-01-23 | ||
| PCT/IB2018/050128 WO2018134698A1 (en) | 2017-01-23 | 2018-01-09 | Heterocyclic spiro compounds as magl inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3050853A1 true CA3050853A1 (en) | 2018-07-26 |
Family
ID=61028112
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3050853A Abandoned CA3050853A1 (en) | 2017-01-23 | 2018-01-09 | Heterocyclic spiro compounds as magl inhibitors |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US20180208608A1 (https=) |
| EP (1) | EP3571202B1 (https=) |
| JP (1) | JP2020506903A (https=) |
| KR (1) | KR20190097242A (https=) |
| CN (1) | CN110198944A (https=) |
| AU (1) | AU2018208848A1 (https=) |
| BR (1) | BR112019014099A2 (https=) |
| CA (1) | CA3050853A1 (https=) |
| IL (1) | IL267781A (https=) |
| MX (1) | MX2019008690A (https=) |
| RU (1) | RU2726631C1 (https=) |
| SG (1) | SG11201906427QA (https=) |
| TW (1) | TWI665199B (https=) |
| WO (1) | WO2018134698A1 (https=) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TN2017000544A1 (en) | 2015-07-31 | 2019-04-12 | Pfizer | 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives and 1,1,1-trifluoro-4-hydroxybutan-2-yl carbamate derivatives as magl inhibitors |
| 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 |
| RU2720203C1 (ru) * | 2017-01-20 | 2020-04-27 | Пфайзер Инк. | 1,1,1-трифтор-3-гидроксипропан-2-илкарбаматные производные как ингибиторы magl |
| US10927105B1 (en) | 2017-05-23 | 2021-02-23 | Lundbeck La Jolla Research Center, Inc. | Pyrazole MAGL inhibitors |
| BR112020005720A2 (pt) * | 2017-09-29 | 2020-10-20 | Takeda Pharmaceutical Company Limited | composto ou sal, medicamento, métodos para inibir monoacilglicerol lipase e para a profilaxia ou o tratamento de doença de alzheimer, doença de parkinson, doença de huntington, esclerose lateral amiotrófica, esclerose múltipla, distúrbio de ansiedade, dor, epilepsia ou depressão, e, uso do composto ou sal. |
| US10662159B2 (en) * | 2017-11-22 | 2020-05-26 | Makscientific, Llc | ABHD6 and dual ABHD6/MGL inhibitors and their uses |
| WO2019134985A1 (en) | 2018-01-08 | 2019-07-11 | F. Hoffmann-La Roche Ag | Octahydropyrido[1,2-alpha]pyrazines as magl inhibitors |
| MX2021000549A (es) * | 2018-07-19 | 2021-03-25 | Pfizer | Compuestos espiro heterociclicos como inhibidores de magl. |
| RS67557B1 (sr) * | 2018-08-24 | 2026-01-30 | Pharmacosmos Holding As | Unapređena sinteza 1,4-diazaspiro[5.5]undekan-3-ona |
| EP3856178B1 (en) | 2018-09-28 | 2026-03-11 | Janssen Pharmaceutica NV | Monoacylglycerol lipase modulators |
| WO2020065614A1 (en) | 2018-09-28 | 2020-04-02 | Janssen Pharmaceutica Nv | Monoacylglycerol lipase modulators |
| KR20210097734A (ko) * | 2018-11-28 | 2021-08-09 | 하. 룬드벡 아크티에셀스카브 | Magl 저해제에 의해 질병을 치료하는 방법 |
| 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 |
| CA3125636A1 (en) * | 2019-01-25 | 2020-07-30 | H. Lundbeck A/S | Methods of treating disease with magl inhibitors |
| BR112021026899A2 (pt) * | 2019-07-09 | 2022-05-10 | Hoffmann La Roche | Compostos heterocíclicos |
| MX2022003819A (es) | 2019-09-30 | 2022-05-11 | Janssen Pharmaceutica Nv | Ligandos de pet de mgl radiomarcados. |
| CA3176113A1 (en) * | 2020-03-26 | 2021-09-30 | Janssen Pharmaceutica Nv | Aminocyclobutanes as monoacylglycerol lipase modulators |
| 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 |
| MX2023003240A (es) * | 2020-09-22 | 2023-06-16 | Janssen Pharmaceutica Nv | Moduladores de monoacilglicerol lipasa de ciclobutilamida. |
| US12029718B2 (en) | 2021-11-09 | 2024-07-09 | Cct Sciences, Llc | Process for production of essentially pure delta-9-tetrahydrocannabinol |
| TWI904281B (zh) * | 2020-11-13 | 2025-11-11 | 丹麥商Ｈ 朗德貝克公司 | Magl抑制劑 |
| 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 |
| CA3242372A1 (en) | 2021-12-29 | 2023-07-06 | Psy Therapeutics, Inc. | Inhibiting monoacylglycerol lipase (magl) |
| KR20250005229A (ko) * | 2022-05-04 | 2025-01-09 | 하. 룬드벡 아크티에셀스카브 | 모노아실글리세롤 리파제 억제제로서 1,1,1,3,3,3-헥사플루오로프로판-2-일 (s)-1-(피리다진-3-일카르바모일)-6 아자스피로[2.5]옥탄-6-카르복실레이트의 결정질 형태 |
| EP4665718A1 (en) | 2023-02-13 | 2025-12-24 | Apogee Pharmaceuticals, Inc. | Small molecules as monoacylglycerol lipase (magl) inhibitors, compositions and use thereof |
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|---|---|---|---|---|
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| KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| JPH10503768A (ja) | 1994-08-02 | 1998-04-07 | メルク シヤープ エンド ドーム リミテツド | アゼチジン、ピロリジンおよびピペリジン誘導体 |
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| JP2018513119A (ja) * | 2015-03-18 | 2018-05-24 | アビデ セラピューティクス，インク． | ピペラジンカルバメート、およびピペラジンカルバメートを製造ならびに使用する方法 |
| TN2017000544A1 (en) | 2015-07-31 | 2019-04-12 | Pfizer | 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives and 1,1,1-trifluoro-4-hydroxybutan-2-yl carbamate derivatives as magl inhibitors |
| US10781211B2 (en) * | 2016-05-12 | 2020-09-22 | Lundbeck La Jolla Research Center, Inc. | Spirocycle compounds and methods of making and using same |
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2018
- 2018-01-09 CN CN201880007992.7A patent/CN110198944A/zh active Pending
- 2018-01-09 EP EP18701578.9A patent/EP3571202B1/en active Active
- 2018-01-09 JP JP2019538585A patent/JP2020506903A/ja not_active Withdrawn
- 2018-01-09 WO PCT/IB2018/050128 patent/WO2018134698A1/en not_active Ceased
- 2018-01-09 KR KR1020197021451A patent/KR20190097242A/ko not_active Withdrawn
- 2018-01-09 CA CA3050853A patent/CA3050853A1/en not_active Abandoned
- 2018-01-09 RU RU2019123020A patent/RU2726631C1/ru active
- 2018-01-09 SG SG11201906427QA patent/SG11201906427QA/en unknown
- 2018-01-09 MX MX2019008690A patent/MX2019008690A/es unknown
- 2018-01-09 AU AU2018208848A patent/AU2018208848A1/en not_active Abandoned
- 2018-01-09 BR BR112019014099-9A patent/BR112019014099A2/pt not_active Application Discontinuation
- 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 |
|---|---|
| EP3571202B1 (en) | 2021-06-30 |
| CN110198944A (zh) | 2019-09-03 |
| SG11201906427QA (en) | 2019-08-27 |
| AU2018208848A1 (en) | 2019-07-18 |
| WO2018134698A1 (en) | 2018-07-26 |
| KR20190097242A (ko) | 2019-08-20 |
| TWI665199B (zh) | 2019-07-11 |
| JP2020506903A (ja) | 2020-03-05 |
| BR112019014099A2 (pt) | 2020-02-11 |
| US20180208608A1 (en) | 2018-07-26 |
| MX2019008690A (es) | 2019-09-18 |
| RU2726631C1 (ru) | 2020-07-15 |
| US10858373B2 (en) | 2020-12-08 |
| IL267781A (en) | 2019-09-26 |
| EP3571202A1 (en) | 2019-11-27 |
| US20190292203A1 (en) | 2019-09-26 |
| TW201838995A (zh) | 2018-11-01 |
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| EEER | Examination request |
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| FZDE | Discontinued |
Effective date: 20221220 |