RU2017131862A - КРИСТАЛЛИЧЕСКИЕ ФОРМЫ (S)-5-БЕНЗИЛ-N-(5-МЕТИЛ-4-ОКСО-2,3,4,5-ТЕТРАГИДРОБЕНЗО[b][1,4]ОКСАЗЕПИН-3-ИЛ)-4H-1,2,4-ТРИАЗОЛ-3-КАРБОКСАМИДА - Google Patents
КРИСТАЛЛИЧЕСКИЕ ФОРМЫ (S)-5-БЕНЗИЛ-N-(5-МЕТИЛ-4-ОКСО-2,3,4,5-ТЕТРАГИДРОБЕНЗО[b][1,4]ОКСАЗЕПИН-3-ИЛ)-4H-1,2,4-ТРИАЗОЛ-3-КАРБОКСАМИДА Download PDFInfo
- Publication number
- RU2017131862A RU2017131862A RU2017131862A RU2017131862A RU2017131862A RU 2017131862 A RU2017131862 A RU 2017131862A RU 2017131862 A RU2017131862 A RU 2017131862A RU 2017131862 A RU2017131862 A RU 2017131862A RU 2017131862 A RU2017131862 A RU 2017131862A
- Authority
- RU
- Russia
- Prior art keywords
- crystalline form
- methyl
- oxazepin
- carboxamide
- triazole
- Prior art date
Links
- 239000013078 crystal Substances 0.000 title 1
- LYPAFUINURXJSG-AWEZNQCLSA-N 5-benzyl-n-[(3s)-5-methyl-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-1h-1,2,4-triazole-3-carboxamide Chemical compound N([C@H]1COC2=CC=CC=C2N(C1=O)C)C(=O)C(N=1)=NNC=1CC1=CC=CC=C1 LYPAFUINURXJSG-AWEZNQCLSA-N 0.000 claims 21
- 239000012453 solvate Substances 0.000 claims 21
- 238000002447 crystallographic data Methods 0.000 claims 11
- 238000000634 powder X-ray diffraction Methods 0.000 claims 11
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 6
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
- YKYONYBAUNKHLG-UHFFFAOYSA-N propyl acetate Chemical compound CCCOC(C)=O YKYONYBAUNKHLG-UHFFFAOYSA-N 0.000 claims 4
- -1 (C 1 -C 4 ) alkyl acetate Chemical compound 0.000 claims 3
- JWUJQDFVADABEY-UHFFFAOYSA-N 2-methyltetrahydrofuran Chemical compound CC1CCCO1 JWUJQDFVADABEY-UHFFFAOYSA-N 0.000 claims 3
- SKTCDJAMAYNROS-UHFFFAOYSA-N methoxycyclopentane Chemical compound COC1CCCC1 SKTCDJAMAYNROS-UHFFFAOYSA-N 0.000 claims 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 2
- NTIZESTWPVYFNL-UHFFFAOYSA-N Methyl isobutyl ketone Chemical compound CC(C)CC(C)=O NTIZESTWPVYFNL-UHFFFAOYSA-N 0.000 claims 2
- UIHCLUNTQKBZGK-UHFFFAOYSA-N Methyl isobutyl ketone Natural products CCC(C)C(C)=O UIHCLUNTQKBZGK-UHFFFAOYSA-N 0.000 claims 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 claims 2
- KXKVLQRXCPHEJC-UHFFFAOYSA-N acetic acid trimethyl ester Natural products COC(C)=O KXKVLQRXCPHEJC-UHFFFAOYSA-N 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- IEJIGPNLZYLLBP-UHFFFAOYSA-N dimethyl carbonate Chemical compound COC(=O)OC IEJIGPNLZYLLBP-UHFFFAOYSA-N 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- JMMWKPVZQRWMSS-UHFFFAOYSA-N isopropanol acetate Natural products CC(C)OC(C)=O JMMWKPVZQRWMSS-UHFFFAOYSA-N 0.000 claims 2
- 229940011051 isopropyl acetate Drugs 0.000 claims 2
- GWYFCOCPABKNJV-UHFFFAOYSA-N isovaleric acid Chemical compound CC(C)CC(O)=O GWYFCOCPABKNJV-UHFFFAOYSA-N 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- 238000000034 method Methods 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C223/00—Compounds containing amino and —CHO groups bound to the same carbon skeleton
- C07C223/04—Compounds containing amino and —CHO groups bound to the same carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of the carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
- C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D267/02—Seven-membered rings
- C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
- C07D267/12—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D267/14—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562115674P | 2015-02-13 | 2015-02-13 | |
| US62/115,674 | 2015-02-13 | ||
| PCT/IB2016/050755 WO2016128936A1 (en) | 2015-02-13 | 2016-02-12 | Crystalline forms of (s)-5-benzyl-n-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4h-1,2,4-triazole-3-carboxamide |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2017131862A true RU2017131862A (ru) | 2019-03-13 |
| RU2017131862A3 RU2017131862A3 (https=) | 2019-06-06 |
Family
ID=55359562
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2017131862A RU2017131862A (ru) | 2015-02-13 | 2016-02-12 | КРИСТАЛЛИЧЕСКИЕ ФОРМЫ (S)-5-БЕНЗИЛ-N-(5-МЕТИЛ-4-ОКСО-2,3,4,5-ТЕТРАГИДРОБЕНЗО[b][1,4]ОКСАЗЕПИН-3-ИЛ)-4H-1,2,4-ТРИАЗОЛ-3-КАРБОКСАМИДА |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US10287280B2 (https=) |
| EP (1) | EP3256467A1 (https=) |
| JP (1) | JP2018505199A (https=) |
| KR (1) | KR20170117472A (https=) |
| CN (1) | CN107207485A (https=) |
| AU (1) | AU2016217496B2 (https=) |
| BR (1) | BR112017017411A2 (https=) |
| CA (1) | CA2976172A1 (https=) |
| IL (1) | IL253731A0 (https=) |
| RU (1) | RU2017131862A (https=) |
| WO (1) | WO2016128936A1 (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6754772B2 (ja) | 2015-10-23 | 2020-09-16 | 武田薬品工業株式会社 | 複素環化合物 |
| MA44007A (fr) | 2016-02-05 | 2018-12-19 | Denali Therapeutics Inc | Inhibiteurs du récepteur interagissant avec protéine kinase 1 |
| HRP20220636T1 (hr) | 2016-12-09 | 2022-07-22 | Denali Therapeutics Inc. | Spojevi korisni kao inhibitori ripk1 |
| WO2019123219A1 (en) * | 2017-12-20 | 2019-06-27 | Glaxosmithkline Intellectual Property Development Limited | Crystalline salt form of (s)-5-benzyl-n-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4h-1,2,4-triazole-3-carboxamide |
| UA128160C2 (uk) | 2018-05-03 | 2024-04-24 | Райджел Фармасутікалс, Інк. | Сполуки, що інгібують rip1, а також способи їх одержання та застосування |
| EA202092580A1 (ru) | 2018-05-03 | 2021-04-07 | Ригел Фармасьютикалз, Инк. | Соединения, ингибирующие rip1, а также способы их получения и применения |
| BR112021023040A2 (pt) * | 2019-05-17 | 2021-12-28 | Glaxosmithkline Ip Dev Ltd | Composição de matriz compreendendo (s)-5-benzil-n-(5- metil-4-oxo-2,3,4,5-tetrahidrobenzo[b][1,4]oxazepin-3-il)-4h-1,2,4- triazol-3-carboxamida |
| CA3149926A1 (en) | 2019-09-06 | 2021-03-11 | Yan Chen | Rip1 inhibitory compounds and methods for making and using the same |
| KR102793185B1 (ko) | 2019-09-06 | 2025-04-09 | 리겔 파마슈티칼스, 인크. | Rip1 억제 화합물 및 그를 제조 및 사용하는 방법 |
| AU2020378407B2 (en) | 2019-11-07 | 2024-02-01 | Rigel Pharmaceuticals, Inc. | Heterocyclic RIP1 inhibitory compounds |
| AR121717A1 (es) | 2020-04-02 | 2022-06-29 | Rigel Pharmaceuticals Inc | Inhibidores de rip1k |
| TWI840311B (zh) | 2020-07-01 | 2024-04-21 | 美商雷傑製藥公司 | Rip1k抑制劑 |
| AR125587A1 (es) | 2021-03-11 | 2023-08-02 | Rigel Pharmaceuticals Inc | Inhibidores heterocíclicos de la quinasa de rip1 |
| IL314082A (en) | 2022-01-12 | 2024-09-01 | Denali Therapeutics Inc | Crystal forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydropyrido[3,2-b][1,4]oxazapin-3-yl)- H4- 1,2,4-triazole-3-carboxamide |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI648274B (zh) | 2013-02-15 | 2019-01-21 | 英商葛蘭素史克智慧財產發展有限公司 | 作為激酶抑制劑之雜環醯胺類 （二） |
-
2016
- 2016-02-12 CN CN201680010191.7A patent/CN107207485A/zh active Pending
- 2016-02-12 US US15/548,500 patent/US10287280B2/en active Active
- 2016-02-12 WO PCT/IB2016/050755 patent/WO2016128936A1/en not_active Ceased
- 2016-02-12 EP EP16704713.3A patent/EP3256467A1/en not_active Withdrawn
- 2016-02-12 AU AU2016217496A patent/AU2016217496B2/en not_active Ceased
- 2016-02-12 KR KR1020177025358A patent/KR20170117472A/ko not_active Withdrawn
- 2016-02-12 RU RU2017131862A patent/RU2017131862A/ru not_active Application Discontinuation
- 2016-02-12 CA CA2976172A patent/CA2976172A1/en not_active Abandoned
- 2016-02-12 BR BR112017017411A patent/BR112017017411A2/pt not_active Application Discontinuation
- 2016-02-12 JP JP2017542048A patent/JP2018505199A/ja active Pending
-
2017
- 2017-07-30 IL IL253731A patent/IL253731A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2016217496A1 (en) | 2017-08-17 |
| KR20170117472A (ko) | 2017-10-23 |
| US20180022737A1 (en) | 2018-01-25 |
| RU2017131862A3 (https=) | 2019-06-06 |
| EP3256467A1 (en) | 2017-12-20 |
| IL253731A0 (en) | 2017-09-28 |
| CN107207485A (zh) | 2017-09-26 |
| US10287280B2 (en) | 2019-05-14 |
| CA2976172A1 (en) | 2016-08-18 |
| BR112017017411A2 (pt) | 2018-04-03 |
| WO2016128936A1 (en) | 2016-08-18 |
| JP2018505199A (ja) | 2018-02-22 |
| AU2016217496B2 (en) | 2019-03-07 |
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Legal Events
| Date | Code | Title | Description |
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| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20190920 |