CN103608343B - 用于制备作为大麻素受体调节剂的稠合氮杂环的晶形和制备方法 - Google Patents

用于制备作为大麻素受体调节剂的稠合氮杂环的晶形和制备方法 Download PDF

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Publication number
CN103608343B
CN103608343B CN201280020512.3A CN201280020512A CN103608343B CN 103608343 B CN103608343 B CN 103608343B CN 201280020512 A CN201280020512 A CN 201280020512A CN 103608343 B CN103608343 B CN 103608343B
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CN
China
Prior art keywords
pyrazine
diaza
amide
crystalline form
hydroxymethyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
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CN201280020512.3A
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English (en)
Chinese (zh)
Other versions
CN103608343A (zh
Inventor
A.C.布莱克本
韩相敦
R.M.琼斯
安东尼奥·加利多·蒙塔尔班
B.B.帕尔
J.K.鲁特
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Arena Pharmaceuticals Inc
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Arena Pharmaceuticals Inc
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Expired - Fee Related legal-status Critical Current
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    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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
    • 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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  • 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)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201280020512.3A 2011-02-25 2012-02-24 用于制备作为大麻素受体调节剂的稠合氮杂环的晶形和制备方法 Expired - Fee Related CN103608343B (zh)

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
CN103608343A CN103608343A (zh) 2014-02-26
CN103608343B true CN103608343B (zh) 2019-02-01

Family

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Family Applications (1)

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CN201280020512.3A Expired - Fee Related CN103608343B (zh) 2011-02-25 2012-02-24 用于制备作为大麻素受体调节剂的稠合氮杂环的晶形和制备方法

Country Status (20)

Country Link
US (4) US9458136B2 (enExample)
EP (3) EP4166552B1 (enExample)
JP (1) JP5945554B2 (enExample)
KR (1) KR102036932B1 (enExample)
CN (1) CN103608343B (enExample)
AU (1) AU2012222146B2 (enExample)
BR (1) BR112013021549B1 (enExample)
CA (1) CA2827057C (enExample)
CL (1) CL2013002436A1 (enExample)
CO (1) CO6852066A2 (enExample)
DK (1) DK3395812T3 (enExample)
EA (1) EA035989B1 (enExample)
ES (1) ES2932441T3 (enExample)
IL (1) IL227782A (enExample)
MX (1) MX346533B (enExample)
MY (1) MY165767A (enExample)
PH (1) PH12013501726A1 (enExample)
SG (1) SG192817A1 (enExample)
WO (1) WO2012116276A1 (enExample)
ZA (1) ZA201306402B (enExample)

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CN102596913B (zh) 2009-08-28 2016-11-09 艾尼纳制药公司 大麻素受体调节剂
WO2012116277A1 (en) 2011-02-25 2012-08-30 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
EA035989B1 (ru) * 2011-02-25 2020-09-09 Арена Фармасьютикалз, Инк. Кристаллические формы и способы получения модуляторов каннабиноидного рецептора
WO2016085941A1 (en) * 2014-11-25 2016-06-02 Arena Pharmaceuticals, Inc. Processes for the preparation of cannabinoid receptor modulators
EA201892280A1 (ru) * 2016-04-10 2019-04-30 Арена Фармасьютикалз, Инк. Способы лечения селективными агонистами cb-рецептора
WO2018208847A1 (en) 2017-05-08 2018-11-15 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of pain from inflammatory bowel disease
MX2019013311A (es) * 2017-05-08 2020-08-03 Arena Pharm Inc Compuestos y metodos para el tratamiento del dolor visceral.
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
WO2023059610A1 (en) 2021-10-05 2023-04-13 Arena Pharmaceuticals, Inc. Crystalline forms and processes for the preparation of cannabinoid receptor modulators

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CN101238107A (zh) * 2005-06-02 2008-08-06 格兰马克药品股份有限公司 新的大麻素受体配体，含有该配体的药物组合物及其制备方法
CN102596913A (zh) * 2009-08-28 2012-07-18 艾尼纳制药公司 大麻素受体调节剂

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CN101070316A (zh) 1999-04-28 2007-11-14 萨诺费－阿文蒂斯德国有限公司 作为ppar受体配体的二芳基酸衍生物
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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
WO2012116278A1 (en) 2011-02-25 2012-08-30 Arena Pharmaceuticals, Inc. Cannabinoid receptor modulators
EA035989B1 (ru) 2011-02-25 2020-09-09 Арена Фармасьютикалз, Инк. Кристаллические формы и способы получения модуляторов каннабиноидного рецептора

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006030124A1 (fr) * 2004-09-13 2006-03-23 Sanofi-Aventis Derives de pyrazole condense, leur preparation et leur application en therapeutique.
CN101238107A (zh) * 2005-06-02 2008-08-06 格兰马克药品股份有限公司 新的大麻素受体配体，含有该配体的药物组合物及其制备方法
CN102596913A (zh) * 2009-08-28 2012-07-18 艾尼纳制药公司 大麻素受体调节剂

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US20140135345A1 (en) 2014-05-15
KR102036932B1 (ko) 2019-10-25
AU2012222146B2 (en) 2017-05-11
CA2827057A1 (en) 2012-08-30
US20190308952A1 (en) 2019-10-10
EP4166552B1 (en) 2025-03-19
US11560369B2 (en) 2023-01-24
AU2012222146A1 (en) 2013-09-19
EP3395812B8 (en) 2022-11-02
MY165767A (en) 2018-04-23
BR112013021549B1 (pt) 2022-01-11
EP2678330A1 (en) 2014-01-01
CN103608343A (zh) 2014-02-26
EP3395812A1 (en) 2018-10-31
US20210380560A1 (en) 2021-12-09
SG192817A1 (en) 2013-09-30
ES2932441T3 (es) 2023-01-19
BR112013021549A2 (pt) 2016-11-01
DK3395812T3 (da) 2022-11-28
US10981895B2 (en) 2021-04-20
PH12013501726A1 (en) 2014-01-13
CL2013002436A1 (es) 2014-01-24
EA201391233A1 (ru) 2014-02-28
JP2014506602A (ja) 2014-03-17
EA035989B1 (ru) 2020-09-09
CO6852066A2 (es) 2014-01-30
MX2013009760A (es) 2014-06-11
US10183930B2 (en) 2019-01-22
IL227782A (en) 2017-02-28
MX346533B (es) 2017-03-14
EP3395812B1 (en) 2022-09-28
IL227782A0 (en) 2013-09-30
ZA201306402B (en) 2022-03-30
US9458136B2 (en) 2016-10-04
JP5945554B2 (ja) 2016-07-05
CA2827057C (en) 2022-06-07
WO2012116276A1 (en) 2012-08-30
NZ614787A (en) 2014-08-29
KR20140025353A (ko) 2014-03-04
US20170144993A1 (en) 2017-05-25
EP4166552A1 (en) 2023-04-19

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C06 Publication
PB01 Publication
CB03 Change of inventor or designer information

Inventor after: A.C. Blackburn

Inventor after: Han Xiangdun

Inventor after: R.M. Jones

Inventor after: Antonio Garrido Montalban

Inventor after: B.B. Parr

Inventor after: J.K. Rutter

Inventor before: A.C. Blackburn

Inventor before: Han Xiangdun

Inventor before: R.M. Jones

Inventor before: Montalban Antonio Garrido

Inventor before: B.B. Parr

Inventor before: J.K. Rutter

CB03 Change of inventor or designer information
COR Change of bibliographic data

Free format text: CORRECT: INVENTOR; FROM: BLACKBURN ANTHONY C. HAN SANGDON R.M.JONES MONTALBAN ANTHONIO GARRIDO PAL BIMAN B. RUETER JAIMIE KARYN TO: BLACKBURN ANTHONY C. HAN SANGDON R.M.JONES PAL BIMAN B. RUETER JAIMIE KARYN

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CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20190201

CF01 Termination of patent right due to non-payment of annual fee