CN106854207B - 呔嗪类衍生物、其制备方法、药物组合物和用途 - Google Patents

呔嗪类衍生物、其制备方法、药物组合物和用途 Download PDF

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Publication number
CN106854207B
CN106854207B CN201510900083.4A CN201510900083A CN106854207B CN 106854207 B CN106854207 B CN 106854207B CN 201510900083 A CN201510900083 A CN 201510900083A CN 106854207 B CN106854207 B CN 106854207B
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alkyl
substituents
substituted
independently selected
pain
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Chinese (zh)
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CN106854207A (zh
Inventor
李帅
孙勇
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Shanghai Semerode Biotechnology Co ltd
Shanghai Simr Biotechnology Co ltd
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Shanghai Semerode Biotechnology Co Ltd
Shanghai Sai Murrow Biotechnology Co Ltd
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Application filed by Shanghai Semerode Biotechnology Co Ltd, Shanghai Sai Murrow Biotechnology Co Ltd filed Critical Shanghai Semerode Biotechnology Co Ltd
Priority to CN201510900083.4A priority Critical patent/CN106854207B/zh
Priority to US16/060,256 priority patent/US11220503B2/en
Priority to PCT/CN2016/108975 priority patent/WO2017097217A1/zh
Priority to JP2018530763A priority patent/JP6669868B2/ja
Priority to EP16872406.0A priority patent/EP3388433B1/en
Publication of CN106854207A publication Critical patent/CN106854207A/zh
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201510900083.4A 2015-12-08 2015-12-08 呔嗪类衍生物、其制备方法、药物组合物和用途 Active CN106854207B (zh)

Priority Applications (5)

Application Number Priority Date Filing Date Title
CN201510900083.4A CN106854207B (zh) 2015-12-08 2015-12-08 呔嗪类衍生物、其制备方法、药物组合物和用途
US16/060,256 US11220503B2 (en) 2015-12-08 2016-12-08 Phthalazine derivatives, preparation method, pharmaceutical composition and usage thereof
PCT/CN2016/108975 WO2017097217A1 (zh) 2015-12-08 2016-12-08 呔嗪类衍生物、其制备方法、药物组合物和用途
JP2018530763A JP6669868B2 (ja) 2015-12-08 2016-12-08 フタラジン誘導体、その製造方法、医薬組成物および使用
EP16872406.0A EP3388433B1 (en) 2015-12-08 2016-12-08 Phthalazine derivatives, and preparation method, pharmaceutical composition and use thereof

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN201510900083.4A CN106854207B (zh) 2015-12-08 2015-12-08 呔嗪类衍生物、其制备方法、药物组合物和用途

Publications (2)

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CN106854207A CN106854207A (zh) 2017-06-16
CN106854207B true CN106854207B (zh) 2019-10-29

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Country Status (5)

Country Link
US (1) US11220503B2 (enExample)
EP (1) EP3388433B1 (enExample)
JP (1) JP6669868B2 (enExample)
CN (1) CN106854207B (enExample)
WO (1) WO2017097217A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3766882B1 (en) * 2018-03-12 2023-08-23 Shanghai Simr Biotechnology Co., Ltd. Phthalazine isoxazole alkoxy derivatives, preparation method thereof, pharmaceutical composition and use thereof
CN112979655A (zh) 2019-12-16 2021-06-18 上海赛默罗生物科技有限公司 三唑并哒嗪类衍生物、其制备方法、药物组合物和用途
US20240059691A1 (en) * 2020-12-01 2024-02-22 Kalvista Pharmaceuticals Limited Enzyme inhibitors
CN112441901B (zh) * 2020-12-15 2023-08-29 山东泰和科技股份有限公司 一种乙酸酐的合成方法
CN116008443B (zh) * 2023-03-28 2023-06-30 上海赛默罗生物科技有限公司 α5-GABAA受体调节剂类药物中有关物质的检测方法
CN119019425A (zh) * 2023-05-26 2024-11-26 武汉人福创新药物研发中心有限公司 一种作为α5-GABAA受体调节剂的杂环化合物

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998050385A1 (en) * 1997-05-08 1998-11-12 Merck Sharp & Dohme Limited SUBSTITUTED 1,2,4-TRIAZOLO[3,4-a]PHTHALAZINE DERIVATIVES AS GABA ALPHA 5 LIGANDS
WO2002042305A1 (en) * 2000-11-23 2002-05-30 Merck Sharp & Dohme Limited Nitrogen substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives for enhancing cognition
CN1871008A (zh) * 2003-10-21 2006-11-29 默克公司 用于治疗神经病变性疼痛的三唑并－哒嗪化合物和它们的衍生物

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9112504D0 (en) 1991-06-11 1991-07-31 Merck Sharp & Dohme Cell line
DE69320985T2 (de) 1992-12-10 1999-05-12 Merck Sharp & Dohme Stabil transfizierte zelllinien welche gaba-a rezeptoren exprimieren
GB9715977D0 (en) 1997-07-29 1997-10-01 Merck Sharp & Dohme Therapeutic agents
US6297235B1 (en) * 1997-08-28 2001-10-02 Merck Sharp & Dohme Ltd. Triazolopyridazine derivatives for treating anxiety and enhancing cognition
IL149550A0 (en) * 1999-11-12 2002-11-10 Neurogen Corp Bicyclic and tricyclic heteroaromatic compounds
US20050043982A1 (en) * 2003-08-22 2005-02-24 Nguyen Vinh Dinh Contextual workflow modeling
US10206921B2 (en) 2009-06-03 2019-02-19 The Regents Of The University Of California Methods and compositions for treating a subject for central nervous system (CNS) injury
US20150374705A1 (en) 2012-02-14 2015-12-31 Shanghai Institues for Biological Sciences Substances for treatment or relief of pain

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998050385A1 (en) * 1997-05-08 1998-11-12 Merck Sharp & Dohme Limited SUBSTITUTED 1,2,4-TRIAZOLO[3,4-a]PHTHALAZINE DERIVATIVES AS GABA ALPHA 5 LIGANDS
WO2002042305A1 (en) * 2000-11-23 2002-05-30 Merck Sharp & Dohme Limited Nitrogen substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives for enhancing cognition
CN1871008A (zh) * 2003-10-21 2006-11-29 默克公司 用于治疗神经病变性疼痛的三唑并－哒嗪化合物和它们的衍生物

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Identification and synthesis of [1,2,4]triazolo[3,4- a]phthalazine derivatives as high-affinity ligands to the α2δ-1 subunit of voltage;Alec D. Lebsack，等;《Bioorganic & Medicinal Chemistry Letters》;20041231;第14卷;第2463-2467页 *

Also Published As

Publication number Publication date
US11220503B2 (en) 2022-01-11
CN106854207A (zh) 2017-06-16
WO2017097217A1 (zh) 2017-06-15
US20200165253A1 (en) 2020-05-28
JP2018537480A (ja) 2018-12-20
JP6669868B2 (ja) 2020-03-18
EP3388433B1 (en) 2023-08-30
EP3388433A1 (en) 2018-10-17
EP3388433A4 (en) 2019-08-07

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Effective date of registration: 20190614

Address after: Room 1304, 781 Cailun Road, Zhangjiang High-tech Park, Pudong, Shanghai, 201210

Applicant after: SHANGHAI SIMR BIOTECHNOLOGY Co.,Ltd.

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Address before: Room 1304, 781 Cailun Road, Zhangjiang High-tech Park, Pudong, Shanghai, 201210

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CB02 Change of applicant information

Address after: Building 26, Lane 100, Banxia Road, Pudong New Area, Shanghai International Medical Park, Shanghai, 201321

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Address before: Room 1304, 781 Cailun Road, Zhangjiang High-tech Park, Pudong, Shanghai, 201210

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PE01 Entry into force of the registration of the contract for pledge of patent right

Denomination of invention: Pyrazine derivatives, their preparation methods, pharmaceutical compositions, and uses

Effective date of registration: 20230814

Granted publication date: 20191029

Pledgee: China Minsheng Banking Corp Shanghai branch

Pledgor: SHANGHAI SIMR BIOTECHNOLOGY Co.,Ltd.|Shanghai Semerode Biotechnology Co.,Ltd.|RUDONG SIMR BIOTECH Co.,Ltd.

Registration number: Y2023310000463

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Granted publication date: 20191029

Pledgee: China Minsheng Banking Corp Shanghai branch

Pledgor: SHANGHAI SIMR BIOTECHNOLOGY Co.,Ltd.|Shanghai Semerode Biotechnology Co.,Ltd.|RUDONG SIMR BIOTECH Co.,Ltd.

Registration number: Y2023310000463

PC01 Cancellation of the registration of the contract for pledge of patent right