CA2997541C - Therapeutic compounds for pain and synthesis thereof - Google Patents

Therapeutic compounds for pain and synthesis thereof Download PDF

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Publication number
CA2997541C
CA2997541C CA2997541A CA2997541A CA2997541C CA 2997541 C CA2997541 C CA 2997541C CA 2997541 A CA2997541 A CA 2997541A CA 2997541 A CA2997541 A CA 2997541A CA 2997541 C CA2997541 C CA 2997541C
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Canada
Prior art keywords
compound
formula
reacting
making
acid
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CA2997541A
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English (en)
French (fr)
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CA2997541A1 (en
Inventor
Bart Lieven Daniel DECORTE
Jacob Cornelis RUSSCHER
Menno Cornelis Franciscus MONNEE
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/18—Bridged 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
    • A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06—Oxygen atoms
    • C07D451/10—Oxygen atoms acylated by aliphatic or araliphatic carboxylic acids, e.g. atropine, scopolamine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06—Oxygen atoms
    • C07D451/12—Oxygen atoms acylated by aromatic or heteroaromatic carboxylic acids, e.g. cocaine

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pyridine Compounds (AREA)
CA2997541A 2015-09-04 2016-09-01 Therapeutic compounds for pain and synthesis thereof Active CA2997541C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201562214734P 2015-09-04 2015-09-04
US201562214727P 2015-09-04 2015-09-04
US62/214,727 2015-09-04
US62/214,734 2015-09-04
PCT/US2016/049877 WO2017040767A1 (en) 2015-09-04 2016-09-01 Therapeutic compounds for pain and synthesis thereof

Publications (2)

Publication Number Publication Date
CA2997541A1 CA2997541A1 (en) 2017-03-09
CA2997541C true CA2997541C (en) 2022-01-11

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Family Applications (5)

Application Number Title Priority Date Filing Date
CA2997541A Active CA2997541C (en) 2015-09-04 2016-09-01 Therapeutic compounds for pain and synthesis thereof
CA2997501A Active CA2997501C (en) 2015-09-04 2016-09-01 Therapeutic compound for pain and synthesis thereof
CA2997430A Active CA2997430C (en) 2015-09-04 2016-09-01 Therapeutic compounds for pain and synthesis thereof
CA2997545A Active CA2997545C (en) 2015-09-04 2016-09-01 Therapeutic compounds for pain and synthesis thereof
CA2997543A Active CA2997543C (en) 2015-09-04 2016-09-01 Therapeutic compounds for pain and synthesis thereof

Family Applications After (4)

Application Number Title Priority Date Filing Date
CA2997501A Active CA2997501C (en) 2015-09-04 2016-09-01 Therapeutic compound for pain and synthesis thereof
CA2997430A Active CA2997430C (en) 2015-09-04 2016-09-01 Therapeutic compounds for pain and synthesis thereof
CA2997545A Active CA2997545C (en) 2015-09-04 2016-09-01 Therapeutic compounds for pain and synthesis thereof
CA2997543A Active CA2997543C (en) 2015-09-04 2016-09-01 Therapeutic compounds for pain and synthesis thereof

Country Status (11)

Country Link
US (9) US10040797B2 (enExample)
EP (5) EP3344627B9 (enExample)
JP (5) JP6868008B2 (enExample)
CN (5) CN109153679B (enExample)
CA (5) CA2997541C (enExample)
DK (4) DK3344627T5 (enExample)
ES (4) ES2807901T3 (enExample)
IL (5) IL257732B (enExample)
MA (1) MA45011A (enExample)
TW (11) TWI639597B (enExample)
WO (5) WO2017040767A1 (enExample)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2997541C (en) * 2015-09-04 2022-01-11 Janssen Pharmaceutica Nv Therapeutic compounds for pain and synthesis thereof

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TWI713879B (zh) 2020-12-21
DK3344626T5 (da) 2021-09-06
CN109071540A (zh) 2018-12-21
CA2997501C (en) 2022-05-10
TWI683815B (zh) 2020-02-01
ES2808048T3 (es) 2021-02-25
EP3344626B1 (en) 2020-07-08
JP6868008B2 (ja) 2021-05-12
CN108290890B (zh) 2021-08-06
EP3344628A1 (en) 2018-07-11
US10155762B2 (en) 2018-12-18
JP2018527355A (ja) 2018-09-20
CN108290890A (zh) 2018-07-17
MA45011A (fr) 2021-06-02
DK3344627T5 (da) 2021-08-30
CN109071540B (zh) 2021-06-04
JP6736660B2 (ja) 2020-08-05
TWI686393B (zh) 2020-03-01
JP6639651B2 (ja) 2020-02-05
TW201716409A (zh) 2017-05-16
CN108349934A (zh) 2018-07-31
IL257732A (en) 2018-04-30
TWI695836B (zh) 2020-06-11
CA2997501A1 (en) 2017-03-09
IL257737A (en) 2018-04-30
TW201722954A (zh) 2017-07-01
US10358448B2 (en) 2019-07-23
JP2018526387A (ja) 2018-09-13
CN108495854B (zh) 2021-10-15
EP3344626B9 (en) 2021-08-11
CA2997545C (en) 2022-01-11
IL257740A (en) 2018-04-30
IL257735A (en) 2018-04-30
DK3344626T3 (da) 2020-07-27
TW201722951A (zh) 2017-07-01
DK3344614T3 (da) 2020-07-27
TW201920176A (zh) 2019-06-01
TWI639597B (zh) 2018-11-01
TWI636054B (zh) 2018-09-21
WO2017040772A1 (en) 2017-03-09
ES2812233T9 (es) 2022-02-18
EP3344628A4 (en) 2019-03-27
DK3344628T3 (da) 2020-08-03
IL257737B2 (en) 2023-02-01
EP3344614A1 (en) 2018-07-11
US20190112311A1 (en) 2019-04-18
TW201811786A (zh) 2018-04-01
EP3344629A4 (en) 2019-03-27
US20170066768A1 (en) 2017-03-09
EP3344614B1 (en) 2020-07-08
WO2017040772A9 (en) 2019-03-07
US20170066770A1 (en) 2017-03-09
ES2812233T3 (es) 2021-03-16
JP2018531907A (ja) 2018-11-01
US20180291024A1 (en) 2018-10-11
TW201722955A (zh) 2017-07-01
EP3344627B1 (en) 2020-07-01
US10040797B2 (en) 2018-08-07
CA2997543A1 (en) 2017-03-09
US10040795B2 (en) 2018-08-07
US10351565B2 (en) 2019-07-16
US10040796B2 (en) 2018-08-07
IL257734A (en) 2018-04-30
EP3344614A4 (en) 2019-03-27
TWI641608B (zh) 2018-11-21
TW201833110A (zh) 2018-09-16
ES2807901T3 (es) 2021-02-24
CN109153679B (zh) 2022-04-08
IL257732B (en) 2020-11-30
TW201835082A (zh) 2018-10-01
TW201819381A (zh) 2018-06-01
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ES2808048T9 (es) 2022-02-01
US20170066767A1 (en) 2017-03-09
EP3344628B9 (en) 2021-06-30
ES2809703T9 (es) 2022-01-24
TWI663167B (zh) 2019-06-21
TWI707854B (zh) 2020-10-21
US20170066769A1 (en) 2017-03-09
IL257734B (en) 2021-07-29
US10766898B2 (en) 2020-09-08
US20180327406A1 (en) 2018-11-15
DK3344614T5 (da) 2021-08-30
EP3344627A1 (en) 2018-07-11
EP3344614B9 (en) 2021-07-28
CA2997430C (en) 2021-05-11
ES2807901T9 (es) 2022-01-31
TWI672303B (zh) 2019-09-21
CN108349934B (zh) 2021-10-22
EP3344629A1 (en) 2018-07-11
EP3344628B1 (en) 2020-07-15
US10351566B2 (en) 2019-07-16
TWI654188B (zh) 2019-03-21
CA2997545A1 (en) 2017-03-09
US20170066760A1 (en) 2017-03-09
IL257735B (en) 2022-01-01
CA2997543C (en) 2022-07-19
TW201843153A (zh) 2018-12-16
CN109153679A (zh) 2019-01-04
EP3344626A4 (en) 2019-03-27
WO2017040764A1 (en) 2017-03-09
EP3344627A4 (en) 2019-03-27
CA2997541A1 (en) 2017-03-09
US9994572B2 (en) 2018-06-12
US20180327405A1 (en) 2018-11-15
DK3344628T5 (da) 2021-07-26
IL257737B (en) 2022-10-01
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