CN106939005A - 晶态的(1r,4r)‑6’‑氟‑N,N‑二甲基‑4‑苯基‑4’,9’‑二氢‑3’H‑螺[环己烷‑1,1’‑吡喃并[3,4,b]吲哚]‑4‑胺 - Google Patents
晶态的(1r,4r)‑6’‑氟‑N,N‑二甲基‑4‑苯基‑4’,9’‑二氢‑3’H‑螺[环己烷‑1,1’‑吡喃并[3,4,b]吲哚]‑4‑胺 Download PDFInfo
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- CN106939005A CN106939005A CN201710173425.6A CN201710173425A CN106939005A CN 106939005 A CN106939005 A CN 106939005A CN 201710173425 A CN201710173425 A CN 201710173425A CN 106939005 A CN106939005 A CN 106939005A
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- Prior art keywords
- ray diffraction
- dimethyl
- phenyl
- dihydro
- amine
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- 125000004836 hexamethylene group Chemical group [H]C([H])([*:2])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[*:1] 0.000 title claims 2
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- 229960004274 stearic acid Drugs 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 229920003051 synthetic elastomer Polymers 0.000 description 1
- 239000005061 synthetic rubber Substances 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 235000015523 tannic acid Nutrition 0.000 description 1
- 229920002258 tannic acid Polymers 0.000 description 1
- 229940033123 tannic acid Drugs 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- WHRNULOCNSKMGB-UHFFFAOYSA-N tetrahydrofuran thf Chemical compound C1CCOC1.C1CCOC1 WHRNULOCNSKMGB-UHFFFAOYSA-N 0.000 description 1
- 238000002076 thermal analysis method Methods 0.000 description 1
- 238000000003 thermogravimetry coupled to Fourier transform infrared spectroscopy Methods 0.000 description 1
- 239000004408 titanium dioxide Substances 0.000 description 1
- OGIDPMRJRNCKJF-UHFFFAOYSA-N titanium oxide Inorganic materials [Ti]=O OGIDPMRJRNCKJF-UHFFFAOYSA-N 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 150000004684 trihydrates Chemical class 0.000 description 1
- 150000004670 unsaturated fatty acids Chemical class 0.000 description 1
- 235000021122 unsaturated fatty acids Nutrition 0.000 description 1
- 208000009935 visceral pain Diseases 0.000 description 1
- 230000003245 working effect Effects 0.000 description 1
- 239000011787 zinc oxide Substances 0.000 description 1
- 235000014692 zinc oxide Nutrition 0.000 description 1
- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical compound [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 description 1
- 229940057977 zinc stearate Drugs 0.000 description 1
- NWONKYPBYAMBJT-UHFFFAOYSA-L zinc sulfate Chemical compound [Zn+2].[O-]S([O-])(=O)=O NWONKYPBYAMBJT-UHFFFAOYSA-L 0.000 description 1
- 229910000368 zinc sulfate Inorganic materials 0.000 description 1
- 229960001763 zinc sulfate Drugs 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- 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
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Anesthesiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Indole Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11005587.8 | 2011-07-08 | ||
| EP11005587 | 2011-07-08 | ||
| CN201280032432.XA CN103649094B (zh) | 2011-07-08 | 2012-07-06 | 晶态的(1r,4r)‑6’‑氟‑N,N‑二甲基‑4‑苯基‑4’,9’‑二氢‑3’H‑螺[环己烷‑1,1’‑吡喃并[3,4,b]吲哚]‑4‑胺 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280032432.XA Division CN103649094B (zh) | 2011-07-08 | 2012-07-06 | 晶态的(1r,4r)‑6’‑氟‑N,N‑二甲基‑4‑苯基‑4’,9’‑二氢‑3’H‑螺[环己烷‑1,1’‑吡喃并[3,4,b]吲哚]‑4‑胺 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106939005A true CN106939005A (zh) | 2017-07-11 |
Family
ID=46717800
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710173425.6A Pending CN106939005A (zh) | 2011-07-08 | 2012-07-06 | 晶态的(1r,4r)‑6’‑氟‑N,N‑二甲基‑4‑苯基‑4’,9’‑二氢‑3’H‑螺[环己烷‑1,1’‑吡喃并[3,4,b]吲哚]‑4‑胺 |
| CN201280032432.XA Active CN103649094B (zh) | 2011-07-08 | 2012-07-06 | 晶态的(1r,4r)‑6’‑氟‑N,N‑二甲基‑4‑苯基‑4’,9’‑二氢‑3’H‑螺[环己烷‑1,1’‑吡喃并[3,4,b]吲哚]‑4‑胺 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280032432.XA Active CN103649094B (zh) | 2011-07-08 | 2012-07-06 | 晶态的(1r,4r)‑6’‑氟‑N,N‑二甲基‑4‑苯基‑4’,9’‑二氢‑3’H‑螺[环己烷‑1,1’‑吡喃并[3,4,b]吲哚]‑4‑胺 |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US8618156B2 (OSRAM) |
| EP (2) | EP2729470B1 (OSRAM) |
| JP (2) | JP6276689B2 (OSRAM) |
| CN (2) | CN106939005A (OSRAM) |
| AR (1) | AR087081A1 (OSRAM) |
| AU (2) | AU2012283449B2 (OSRAM) |
| BR (1) | BR112014000358A2 (OSRAM) |
| CA (1) | CA2841032C (OSRAM) |
| CY (1) | CY1120525T1 (OSRAM) |
| DK (2) | DK3235821T3 (OSRAM) |
| EA (1) | EA026750B1 (OSRAM) |
| ES (1) | ES2641299T3 (OSRAM) |
| HR (1) | HRP20170968T1 (OSRAM) |
| HU (1) | HUE033043T2 (OSRAM) |
| IL (1) | IL230331B (OSRAM) |
| LT (1) | LT2729470T (OSRAM) |
| MX (1) | MX2014000297A (OSRAM) |
| PL (1) | PL2729470T3 (OSRAM) |
| PT (1) | PT2729470T (OSRAM) |
| RS (1) | RS56343B1 (OSRAM) |
| SI (1) | SI2729470T1 (OSRAM) |
| TW (1) | TWI585092B (OSRAM) |
| WO (1) | WO2013007361A1 (OSRAM) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2729470B1 (en) * | 2011-07-08 | 2017-06-21 | Grünenthal GmbH | Crystalline (1r,4r)-6'-fluoro-n,n-dimethyl-4-phenyl-4',9'-dihydro-3'h-spiro[cyclohexane-1,1'-pyrano[3,4,b]indol]-4-amine |
| US10022353B2 (en) * | 2015-01-23 | 2018-07-17 | Grünenthal GmbH | Cebranopadol for treating pain in subjects with impaired hepatic and/or impaired renal function |
| ES2713960T3 (es) | 2015-02-02 | 2019-05-24 | Ratiopharm Gmbh | Composición que comprende cebranopadol en forma disuelta |
| WO2017148595A1 (en) | 2016-02-29 | 2017-09-08 | Grünenthal GmbH | Titration of cebranopadol |
| CN112313202A (zh) * | 2019-05-21 | 2021-02-02 | 江苏众强药业有限公司 | 曲前列尼尔钠盐新晶型及制备方法 |
| CN112254496A (zh) * | 2020-09-25 | 2021-01-22 | 榆林学院 | 一种煤泥收集装置 |
| WO2024129782A1 (en) | 2022-12-12 | 2024-06-20 | Park Therapeutics, Inc. | Regimens and compositions useful for alleviating pain |
| EP4665333A1 (en) | 2023-02-15 | 2025-12-24 | Adneuris Therapeutics, Inc. | Regimens and compositions useful for alleviating pain |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1735619A (zh) * | 2002-11-11 | 2006-02-15 | 格吕伦塔尔有限公司 | 螺环环己烷衍生物 |
| WO2006108565A1 (de) * | 2005-04-11 | 2006-10-19 | Grünenthal GmbH | Spirocyclishe cyclohexanderivate zur behandlung von substanzabhängigkeit |
| WO2008009415A2 (de) * | 2006-07-18 | 2008-01-24 | Grünenthal GmbH | 4-heteroaryl-substituierte 1-aminocyclohexan-1- und cyclohexen-1-derivate mit wirkung auf das opiod rezeptor system |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102006046745A1 (de) | 2006-09-29 | 2008-04-03 | Grünenthal GmbH | Gemischte ORL1/µ-Agonisten zur Behandlung von Schmerz |
| EP2600850B1 (en) * | 2010-08-04 | 2018-10-17 | Grünenthal GmbH | Pharmaceutical dosage form comprising 6'-fluoro-(n-methyl- or n,n-dimethyl-)-4-phenyl-4',9'-dihydro-3'h-spiro[cyclohexane-1,1'-pyrano[3,4,b]indol]-4-amine for the treatment of nociceptive pain |
| EP2729470B1 (en) * | 2011-07-08 | 2017-06-21 | Grünenthal GmbH | Crystalline (1r,4r)-6'-fluoro-n,n-dimethyl-4-phenyl-4',9'-dihydro-3'h-spiro[cyclohexane-1,1'-pyrano[3,4,b]indol]-4-amine |
-
2012
- 2012-07-06 EP EP12748646.2A patent/EP2729470B1/en active Active
- 2012-07-06 HU HUE12748646A patent/HUE033043T2/hu unknown
- 2012-07-06 AU AU2012283449A patent/AU2012283449B2/en not_active Ceased
- 2012-07-06 CA CA2841032A patent/CA2841032C/en active Active
- 2012-07-06 EA EA201400120A patent/EA026750B1/ru not_active IP Right Cessation
- 2012-07-06 DK DK17020200.6T patent/DK3235821T3/da active
- 2012-07-06 PT PT127486462T patent/PT2729470T/pt unknown
- 2012-07-06 DK DK12748646.2T patent/DK2729470T3/en active
- 2012-07-06 WO PCT/EP2012/002839 patent/WO2013007361A1/en not_active Ceased
- 2012-07-06 BR BR112014000358A patent/BR112014000358A2/pt not_active IP Right Cessation
- 2012-07-06 US US13/542,809 patent/US8618156B2/en active Active
- 2012-07-06 AR ARP120102454A patent/AR087081A1/es not_active Application Discontinuation
- 2012-07-06 JP JP2014517519A patent/JP6276689B2/ja active Active
- 2012-07-06 HR HRP20170968TT patent/HRP20170968T1/hr unknown
- 2012-07-06 SI SI201231030T patent/SI2729470T1/sl unknown
- 2012-07-06 MX MX2014000297A patent/MX2014000297A/es unknown
- 2012-07-06 ES ES12748646.2T patent/ES2641299T3/es active Active
- 2012-07-06 EP EP17020200.6A patent/EP3235821B1/en active Active
- 2012-07-06 CN CN201710173425.6A patent/CN106939005A/zh active Pending
- 2012-07-06 LT LTEP12748646.2T patent/LT2729470T/lt unknown
- 2012-07-06 CN CN201280032432.XA patent/CN103649094B/zh active Active
- 2012-07-06 PL PL12748646T patent/PL2729470T3/pl unknown
- 2012-07-06 RS RS20170921A patent/RS56343B1/sr unknown
- 2012-07-06 TW TW101124343A patent/TWI585092B/zh not_active IP Right Cessation
-
2013
- 2013-03-15 US US13/835,298 patent/US8765800B2/en active Active
-
2014
- 2014-01-06 IL IL230331A patent/IL230331B/en unknown
-
2017
- 2017-01-12 JP JP2017003194A patent/JP6559165B2/ja active Active
- 2017-07-04 AU AU2017204572A patent/AU2017204572B2/en not_active Ceased
- 2017-08-02 CY CY20171100830T patent/CY1120525T1/el unknown
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1735619A (zh) * | 2002-11-11 | 2006-02-15 | 格吕伦塔尔有限公司 | 螺环环己烷衍生物 |
| WO2006108565A1 (de) * | 2005-04-11 | 2006-10-19 | Grünenthal GmbH | Spirocyclishe cyclohexanderivate zur behandlung von substanzabhängigkeit |
| WO2008009415A2 (de) * | 2006-07-18 | 2008-01-24 | Grünenthal GmbH | 4-heteroaryl-substituierte 1-aminocyclohexan-1- und cyclohexen-1-derivate mit wirkung auf das opiod rezeptor system |
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Effective date of abandoning: 20200911 |