CA2827057C - Crystalline forms and processes for the preparation of condensed azacycles (cannabinoid receptor modulators) - Google Patents

Crystalline forms and processes for the preparation of condensed azacycles (cannabinoid receptor modulators) Download PDF

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Publication number
CA2827057C
CA2827057C CA2827057A CA2827057A CA2827057C CA 2827057 C CA2827057 C CA 2827057C CA 2827057 A CA2827057 A CA 2827057A CA 2827057 A CA2827057 A CA 2827057A CA 2827057 C CA2827057 C CA 2827057C
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CA
Canada
Prior art keywords
crystalline form
anhydrous crystalline
pain
tetrahydro
pyrazin
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Active
Application number
CA2827057A
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English (en)
French (fr)
Other versions
CA2827057A1 (en
Inventor
Anthony C. Blackburn
Sangdon Han
Robert M. Jones
Antonio Garrido Montalban
Biman B. PAL
Jaimie Karyn Rueter
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Arena Pharmaceuticals Inc
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Arena Pharmaceuticals Inc
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Publication date
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Publication of CA2827057A1 publication Critical patent/CA2827057A1/en
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Publication of CA2827057C publication Critical patent/CA2827057C/en
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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA2827057A 2011-02-25 2012-02-24 Crystalline forms and processes for the preparation of condensed azacycles (cannabinoid receptor modulators) Active CA2827057C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201161446732P 2011-02-25 2011-02-25
US61/446,732 2011-02-25
US201161448542P 2011-03-02 2011-03-02
US61/448,542 2011-03-02
PCT/US2012/026506 WO2012116276A1 (en) 2011-02-25 2012-02-24 Crystalline forms and processes for the preparation of condensed azacycles ( cannabinoid receptor modulators)

Publications (2)

Publication Number Publication Date
CA2827057A1 CA2827057A1 (en) 2012-08-30
CA2827057C true CA2827057C (en) 2022-06-07

Family

ID=45841624

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2827057A Active CA2827057C (en) 2011-02-25 2012-02-24 Crystalline forms and processes for the preparation of condensed azacycles (cannabinoid receptor modulators)

Country Status (20)

Country Link
US (4) US9458136B2 (OSRAM)
EP (3) EP3395812B8 (OSRAM)
JP (1) JP5945554B2 (OSRAM)
KR (1) KR102036932B1 (OSRAM)
CN (1) CN103608343B (OSRAM)
AU (1) AU2012222146B2 (OSRAM)
BR (1) BR112013021549B1 (OSRAM)
CA (1) CA2827057C (OSRAM)
CL (1) CL2013002436A1 (OSRAM)
CO (1) CO6852066A2 (OSRAM)
DK (1) DK3395812T3 (OSRAM)
EA (1) EA035989B1 (OSRAM)
ES (1) ES2932441T3 (OSRAM)
IL (1) IL227782A (OSRAM)
MX (1) MX346533B (OSRAM)
MY (1) MY165767A (OSRAM)
PH (1) PH12013501726A1 (OSRAM)
SG (1) SG192817A1 (OSRAM)
WO (1) WO2012116276A1 (OSRAM)
ZA (1) ZA201306402B (OSRAM)

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US9597340B2 (en) 2011-02-25 2017-03-21 Arena Pharmaceuticals, Inc. Cannabinoid receptor modulators
MX346533B (es) * 2011-02-25 2017-03-14 Arena Pharm Inc Formas cristalinas y procesos para la preparacion de azaciclos condensados (moduladores de receptores canabinoides).
JP6043733B2 (ja) 2011-02-25 2016-12-14 アリーナ ファーマシューティカルズ, インコーポレイテッド カンナビノイド受容体モジュレーター
WO2016085941A1 (en) * 2014-11-25 2016-06-02 Arena Pharmaceuticals, Inc. Processes for the preparation of cannabinoid receptor modulators
CN109310673A (zh) * 2016-04-10 2019-02-05 艾尼纳制药公司 用选择性cb2受体激动剂治疗的方法
WO2018208847A1 (en) 2017-05-08 2018-11-15 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of pain from inflammatory bowel disease
EP3621619B1 (en) * 2017-05-08 2023-06-28 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of visceral pain
WO2021047581A1 (zh) * 2019-09-12 2021-03-18 四川海思科制药有限公司 一种六氢化苯并吡唑衍生物及其制备
TW202330496A (zh) 2021-10-05 2023-08-01 美商艾尼納製藥公司 用於製備大麻素受體調節劑之結晶形式及方法

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ATE368037T1 (de) 1999-04-28 2007-08-15 Sanofi Aventis Deutschland Di-aryl-säurederivate als ppar rezeptor liganden
EP1461027A4 (en) 2001-12-07 2005-09-07 Univ Virginia Commonwealth TREATMENT OF NEOPLASIA
SE0300010D0 (sv) 2003-01-07 2003-01-07 Astrazeneca Ab Novel Compounds
WO2005123677A1 (en) 2004-06-16 2005-12-29 Actelion Pharmaceuticals Ltd 4-carbonyl substituted 1,1,2-trimethyl-1a,4,5,5a-tetrahydro-1h-4-aza-cyclopropa'a!pentalene derivatives as agonists for the g-protein-coupled receptor s1p1/edg1 and immunosuppressive agents
NZ580387A (en) 2004-07-12 2011-06-30 Cadila Healthcare Ltd Tricyclic pyrazole derivatives as cannabinoid receptor modulators
FR2875230A1 (fr) 2004-09-13 2006-03-17 Sanofi Aventis Sa Derives de pyrazole condense, leur preparation et leur application en therapeutique
DE102004054666A1 (de) 2004-11-12 2006-05-18 Bayer Cropscience Gmbh Substituierte Pyrazol-3-carboxamide, Verfahren zur Herstellung und Verwendung als Herbizide und Pflanzenwachstumsregulatoren
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PL1902034T3 (pl) * 2005-06-02 2011-09-30 Glenmark Pharmaceuticals Sa Nowe ligandy receptorów kanabinoidowych, kompozycja farmaceutyczna je zawierająca oraz proces ich wytwarzania
ATE459352T1 (de) 2006-07-04 2010-03-15 Janssen Pharmaceutica Nv Benzimidazol-cannabinoid-agonisten mit einer substituierten heterocyclischen gruppe
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MX346533B (es) 2011-02-25 2017-03-14 Arena Pharm Inc Formas cristalinas y procesos para la preparacion de azaciclos condensados (moduladores de receptores canabinoides).
WO2012116278A1 (en) 2011-02-25 2012-08-30 Arena Pharmaceuticals, Inc. Cannabinoid receptor modulators
US9597340B2 (en) 2011-02-25 2017-03-21 Arena Pharmaceuticals, Inc. Cannabinoid receptor modulators
JP6043733B2 (ja) 2011-02-25 2016-12-14 アリーナ ファーマシューティカルズ, インコーポレイテッド カンナビノイド受容体モジュレーター

Also Published As

Publication number Publication date
MX2013009760A (es) 2014-06-11
PH12013501726A1 (en) 2014-01-13
CA2827057A1 (en) 2012-08-30
CN103608343A (zh) 2014-02-26
NZ614787A (en) 2014-08-29
JP2014506602A (ja) 2014-03-17
SG192817A1 (en) 2013-09-30
EP3395812B1 (en) 2022-09-28
DK3395812T3 (da) 2022-11-28
CO6852066A2 (es) 2014-01-30
AU2012222146B2 (en) 2017-05-11
AU2012222146A1 (en) 2013-09-19
CL2013002436A1 (es) 2014-01-24
US9458136B2 (en) 2016-10-04
EA035989B1 (ru) 2020-09-09
US11560369B2 (en) 2023-01-24
EP3395812B8 (en) 2022-11-02
US20210380560A1 (en) 2021-12-09
EP2678330A1 (en) 2014-01-01
EP3395812A1 (en) 2018-10-31
US20190308952A1 (en) 2019-10-10
US10183930B2 (en) 2019-01-22
US10981895B2 (en) 2021-04-20
MX346533B (es) 2017-03-14
EP4166552B1 (en) 2025-03-19
EP4166552A1 (en) 2023-04-19
IL227782A0 (en) 2013-09-30
US20140135345A1 (en) 2014-05-15
IL227782A (en) 2017-02-28
WO2012116276A1 (en) 2012-08-30
CN103608343B (zh) 2019-02-01
EA201391233A1 (ru) 2014-02-28
JP5945554B2 (ja) 2016-07-05
ES2932441T3 (es) 2023-01-19
BR112013021549A2 (pt) 2016-11-01
KR20140025353A (ko) 2014-03-04
MY165767A (en) 2018-04-23
KR102036932B1 (ko) 2019-10-25
ZA201306402B (en) 2022-03-30
BR112013021549B1 (pt) 2022-01-11
US20170144993A1 (en) 2017-05-25

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EEER Examination request

Effective date: 20170131

FZDE Discontinued

Effective date: 20210301

FZDC Discontinued application reinstated

Effective date: 20210531

FZDC Discontinued application reinstated

Effective date: 20210531