CN110799501B - 一种食欲素受体拮抗剂的晶型及其制备方法和用途 - Google Patents

一种食欲素受体拮抗剂的晶型及其制备方法和用途 Download PDF

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CN110799501B
CN110799501B CN201880040538.1A CN201880040538A CN110799501B CN 110799501 B CN110799501 B CN 110799501B CN 201880040538 A CN201880040538 A CN 201880040538A CN 110799501 B CN110799501 B CN 110799501B
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crystal form
compound
preparation
present
solvent
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Chinese (zh)
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CN110799501A (zh
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陈敏华
张炎锋
黄春香
张晓宇
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Bojian Pharmaceutical Co ltd
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Crystal Pharmaceutical Suzhou Co Ltd
Bojian Pharmaceutical Co ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • 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)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Anesthesiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201880040538.1A 2017-08-01 2018-07-31 一种食欲素受体拮抗剂的晶型及其制备方法和用途 Active CN110799501B (zh)

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CN202211397034.XA CN115710250A (zh) 2017-08-01 2018-07-31 一种食欲素受体拮抗剂的晶型及其制备方法和用途

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CN2017106481352 2017-08-01
CN201710648135 2017-08-01
PCT/CN2018/097797 WO2019024845A1 (zh) 2017-08-01 2018-07-31 一种食欲素受体拮抗剂的晶型及其制备方法和用途

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CN110799501B true CN110799501B (zh) 2022-11-22

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CN202211397034.XA Pending CN115710250A (zh) 2017-08-01 2018-07-31 一种食欲素受体拮抗剂的晶型及其制备方法和用途

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US (1) US10759779B2 (https=)
JP (2) JP7179049B2 (https=)
CN (2) CN110799501B (https=)
WO (1) WO2019024845A1 (https=)

Families Citing this family (7)

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Publication number Priority date Publication date Assignee Title
JP7179049B2 (ja) * 2017-08-01 2022-11-28 ベルゲン ファーマシューティカル、 エルエルシー オレキシン受容体拮抗薬の結晶形及びその製造方法並びに用途
TW202432509A (zh) * 2019-05-15 2024-08-16 日商衛材R&D企管股份有限公司 對於食慾素-2受體拮抗劑之製備有用之方法及化合物、以及雜質少之萊博雷生
WO2020263253A1 (en) * 2019-06-26 2020-12-30 Moline Margaret Lemborexant for treating sleep issues
CN114502167A (zh) * 2019-09-13 2022-05-13 卫材R&D管理有限公司 用于治疗失眠的药物组合物
US12534448B2 (en) 2019-12-11 2026-01-27 Tapi Czech Industries S.R.O Solid state form of lemborexant
US20230103250A1 (en) * 2020-01-16 2023-03-30 Eisai R&D Management Co., Ltd. Drug substance of lemborexant and medicinal composition comprising same
CN119285556B (zh) * 2024-12-13 2025-02-28 四川健林药业有限责任公司 莱博雷生中间体的合成纯化方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104114524A (zh) * 2012-02-17 2014-10-22 卫材R&D管理有限公司 用于食欲肽-2受体拮抗剂的合成的方法和化合物
CN104592184A (zh) * 2014-12-15 2015-05-06 云南省药物研究所 灯盏乙素苷元晶型及其制备方法

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Publication number Priority date Publication date Assignee Title
US6020157A (en) * 1997-04-30 2000-02-01 Smithkline Beecham Corporation Polynucleotides encoding HFGAN72X receptor
US6166193A (en) * 1997-07-25 2000-12-26 Board Of Regents, University Of Texas System Polynucleotides encoding MY1 receptor
PE20081229A1 (es) 2006-12-01 2008-08-28 Merck & Co Inc Antagonistas de receptor de orexina de diazepam sustituido
PE20091010A1 (es) 2007-10-10 2009-08-08 Actelion Pharmaceuticals Ltd Derivados de tetrahidroquinolina
WO2012039371A1 (ja) 2010-09-22 2012-03-29 エーザイ・アール・アンド・ディー・マネジメント株式会社 シクロプロパン化合物
MX376164B (es) * 2014-10-23 2025-03-07 Eisai R&D Man Co Ltd Composiciones y metodos para tratar el insomnio.
JP7179049B2 (ja) * 2017-08-01 2022-11-28 ベルゲン ファーマシューティカル、 エルエルシー オレキシン受容体拮抗薬の結晶形及びその製造方法並びに用途

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104114524A (zh) * 2012-02-17 2014-10-22 卫材R&D管理有限公司 用于食欲肽-2受体拮抗剂的合成的方法和化合物
CN104592184A (zh) * 2014-12-15 2015-05-06 云南省药物研究所 灯盏乙素苷元晶型及其制备方法

Also Published As

Publication number Publication date
CN110799501A (zh) 2020-02-14
CN115710250A (zh) 2023-02-24
US10759779B2 (en) 2020-09-01
US20200190060A1 (en) 2020-06-18
WO2019024845A1 (zh) 2019-02-07
JP2023027066A (ja) 2023-03-01
JP7179049B2 (ja) 2022-11-28
JP2020528913A (ja) 2020-10-01

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Effective date of registration: 20210513

Address after: Delaware, USA

Applicant after: Bojian Pharmaceutical Co.,Ltd.

Address before: 215123 Bio-nano Park B4301, No. 218 Xinghu Street, Suzhou Industrial Park, Jiangsu Province

Applicant before: CRYSTAL PHARMACEUTICAL (SUZHOU) Co.,Ltd.

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IP01 Partial invalidation of patent right

Commission number: 4W118289

Conclusion of examination: The invention patent No. 201880040538.1 is invalid for claims 1-2, and the parallel technical solutions 1-2 in claim 3, and claims 4-6 are invalid, and the patent right is maintained valid based on the parallel technical solution 3 in claim 3 of the authorized announcement text.

Decision date of declaring invalidation: 20250225

Decision number of declaring invalidation: 584735

Denomination of invention: A crystalline form of an orexin receptor antagonist and its preparation method and uses

Granted publication date: 20221122

Patentee: Bojian Pharmaceutical Co.,Ltd.

IP01 Partial invalidation of patent right