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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Publication of CN103608343A publication Critical patent/CN103608343A/zh
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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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (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)

Application Number Title Priority Date Filing Date
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 (https=)
EP (3) EP4166552B1 (https=)
JP (1) JP5945554B2 (https=)
KR (1) KR102036932B1 (https=)
CN (1) CN103608343B (https=)
AU (1) AU2012222146B2 (https=)
BR (1) BR112013021549B1 (https=)
CA (1) CA2827057C (https=)
CL (1) CL2013002436A1 (https=)
CO (1) CO6852066A2 (https=)
DK (1) DK3395812T3 (https=)
EA (1) EA035989B1 (https=)
ES (1) ES2932441T3 (https=)
IL (1) IL227782A (https=)
MX (1) MX346533B (https=)
MY (1) MY165767A (https=)
PH (1) PH12013501726A1 (https=)
SG (1) SG192817A1 (https=)
WO (1) WO2012116276A1 (https=)
ZA (1) ZA201306402B (https=)

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CA2770866C (en) 2009-08-28 2017-10-10 Arena Pharmaceuticals, Inc. Cannabinoid receptor modulators
CN103492369B (zh) 2011-02-25 2019-03-29 艾尼纳制药公司 大麻素受体调节剂
US9597340B2 (en) 2011-02-25 2017-03-21 Arena Pharmaceuticals, Inc. Cannabinoid receptor modulators
US9458136B2 (en) * 2011-02-25 2016-10-04 Arena Pharmaceuticals, Inc. Crystalline forms and processes for the preparation of cannabinoid receptor modulators
WO2016085941A1 (en) * 2014-11-25 2016-06-02 Arena Pharmaceuticals, Inc. Processes for the preparation of cannabinoid receptor modulators
CA3019842A1 (en) * 2016-04-10 2017-10-19 Arena Pharmaceuticals, Inc. Methods of treatment with selective cb2 receptor agonists
EP3621619B1 (en) 2017-05-08 2023-06-28 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of visceral pain
WO2018208847A1 (en) 2017-05-08 2018-11-15 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of pain from inflammatory bowel disease
CN114391011A (zh) * 2019-09-12 2022-04-22 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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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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CN103492369B (zh) * 2011-02-25 2019-03-29 艾尼纳制药公司 大麻素受体调节剂
US9458136B2 (en) * 2011-02-25 2016-10-04 Arena Pharmaceuticals, Inc. Crystalline forms and processes for the preparation of cannabinoid receptor modulators
US9597340B2 (en) 2011-02-25 2017-03-21 Arena Pharmaceuticals, Inc. Cannabinoid receptor modulators
WO2012116278A1 (en) 2011-02-25 2012-08-30 Arena Pharmaceuticals, Inc. Cannabinoid receptor modulators

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

Also Published As

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

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Legal Events

Date Code Title Description
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

SE01 Entry into force of request for substantive examination
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GR01 Patent grant
GR01 Patent grant
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