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 PDF

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Publication number
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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CN
China
Prior art keywords
ray diffraction
dimethyl
phenyl
dihydro
amine
Prior art date
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Pending
Application number
CN201710173425.6A
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English (en)
Chinese (zh)
Inventor
M·格鲁斯
S·克卢格
S·普吕斯
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Grünenthal GmbH
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Grünenthal GmbH
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Publication of CN106939005A publication Critical patent/CN106939005A/zh
Pending legal-status Critical Current

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    • 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

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  • 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)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (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)
CN201710173425.6A 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 Pending CN106939005A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11005587 2011-07-08
EP11005587.8 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

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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 (cg-RX-API-DMAC10.html)
EP (2) EP2729470B1 (cg-RX-API-DMAC10.html)
JP (2) JP6276689B2 (cg-RX-API-DMAC10.html)
CN (2) CN106939005A (cg-RX-API-DMAC10.html)
AR (1) AR087081A1 (cg-RX-API-DMAC10.html)
AU (2) AU2012283449B2 (cg-RX-API-DMAC10.html)
BR (1) BR112014000358A2 (cg-RX-API-DMAC10.html)
CA (1) CA2841032C (cg-RX-API-DMAC10.html)
CY (1) CY1120525T1 (cg-RX-API-DMAC10.html)
DK (2) DK2729470T3 (cg-RX-API-DMAC10.html)
EA (1) EA026750B1 (cg-RX-API-DMAC10.html)
ES (1) ES2641299T3 (cg-RX-API-DMAC10.html)
HR (1) HRP20170968T1 (cg-RX-API-DMAC10.html)
HU (1) HUE033043T2 (cg-RX-API-DMAC10.html)
IL (1) IL230331B (cg-RX-API-DMAC10.html)
LT (1) LT2729470T (cg-RX-API-DMAC10.html)
MX (1) MX2014000297A (cg-RX-API-DMAC10.html)
PL (1) PL2729470T3 (cg-RX-API-DMAC10.html)
PT (1) PT2729470T (cg-RX-API-DMAC10.html)
RS (1) RS56343B1 (cg-RX-API-DMAC10.html)
SI (1) SI2729470T1 (cg-RX-API-DMAC10.html)
TW (1) TWI585092B (cg-RX-API-DMAC10.html)
WO (1) WO2013007361A1 (cg-RX-API-DMAC10.html)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8618156B2 (en) * 2011-07-08 2013-12-31 Gruenenthal 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
CN107427493A (zh) 2015-01-23 2017-12-01 格吕伦塔尔有限公司 用于治疗肝功能受损和/或肾功能受损的受试者的疼痛的Cebranopadol
US20180021304A1 (en) 2015-02-02 2018-01-25 Ratiopharm Gmbh Composition comprising cebranopadol in a dissolved form
MX2018010367A (es) 2016-02-29 2018-12-10 Guenenthal Gmbh Titulacion de cebranopadol.
JP7365073B2 (ja) * 2019-05-21 2023-10-19 ジァンスー フォアフロント ファーマシューティカル カンパニー,リミテッド トレプロスチニルナトリウムの新規な結晶形および製造方法
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
CN122458986A (zh) 2023-02-15 2026-07-24 艾德神经立治疗公司 有用于缓解疼痛的方案和组合物
WO2026035694A1 (en) 2024-08-05 2026-02-12 Adneuris Therapeutics, Inc. Cebranopadol useful for preventing or reducing opioid induced respiratory depression
WO2026161433A1 (en) 2025-01-21 2026-07-30 Adneuris Therapeutics, Inc. Cebranopadol useful for alleviating pain
WO2026161842A1 (en) 2025-01-27 2026-07-30 Adneuris Therapeutics, Inc. Cebranopadol useful for treating pain

Citations (3)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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
EP3459533A1 (en) * 2010-08-04 2019-03-27 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
US8618156B2 (en) * 2011-07-08 2013-12-31 Gruenenthal 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

Patent Citations (3)

* Cited by examiner, † Cited by third party
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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DK3235821T3 (da) 2020-04-20
CA2841032C (en) 2020-12-15
CY1120525T1 (el) 2019-07-10
EP2729470A1 (en) 2014-05-14
JP2017081981A (ja) 2017-05-18
MX2014000297A (es) 2014-01-31
CA2841032A1 (en) 2013-01-17
HUE033043T2 (hu) 2017-11-28
SI2729470T1 (sl) 2017-10-30
US20130012563A1 (en) 2013-01-10
JP6559165B2 (ja) 2019-08-14
EP3235821B1 (en) 2020-04-08
ES2641299T3 (es) 2017-11-08
WO2013007361A8 (en) 2013-04-04
HRP20170968T1 (hr) 2017-09-22
DK2729470T3 (en) 2017-09-11
TW201311694A (zh) 2013-03-16
US20130231381A1 (en) 2013-09-05
PT2729470T (pt) 2017-10-02
EP3235821A1 (en) 2017-10-25
BR112014000358A2 (pt) 2017-01-10
US8618156B2 (en) 2013-12-31
AU2012283449A8 (en) 2014-03-27
JP6276689B2 (ja) 2018-02-07
RS56343B1 (sr) 2017-12-29
CN103649094B (zh) 2017-05-24
WO2013007361A9 (en) 2013-12-27
AR087081A1 (es) 2014-02-12
WO2013007361A1 (en) 2013-01-17
PL2729470T3 (pl) 2017-11-30
AU2012283449B2 (en) 2017-04-06
US8765800B2 (en) 2014-07-01
AU2017204572A1 (en) 2017-07-27
TWI585092B (zh) 2017-06-01
JP2014518226A (ja) 2014-07-28
AU2017204572B2 (en) 2018-05-24
EA201400120A1 (ru) 2014-06-30
LT2729470T (lt) 2017-08-25
EA026750B1 (ru) 2017-05-31
CN103649094A (zh) 2014-03-19
IL230331B (en) 2018-11-29
EP2729470B1 (en) 2017-06-21
AU2012283449A1 (en) 2014-02-20

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Effective date of abandoning: 20200911