CN102952138B - 一种吡唑并嘧啶酮化合物的盐、多晶型物及其药物组合物、制备方法和应用 - Google Patents

一种吡唑并嘧啶酮化合物的盐、多晶型物及其药物组合物、制备方法和应用 Download PDF

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Publication number
CN102952138B
CN102952138B CN201110236585.3A CN201110236585A CN102952138B CN 102952138 B CN102952138 B CN 102952138B CN 201110236585 A CN201110236585 A CN 201110236585A CN 102952138 B CN102952138 B CN 102952138B
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China
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compound
methyl
solution
ethyl
acid
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Chinese (zh)
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CN102952138A (zh
Inventor
李剑峰
田广辉
王震
索瑾
蒋翔锐
刘正
杨小军
谢竹
赵显国
朱维良
蒋华良
沈敬山
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Shanghai Institute of Materia Medica of CAS
Topharman Shanghai Co Ltd
Topharman Shandong Co Ltd
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Shanghai Institute of Materia Medica of CAS
Topharman Shanghai Co Ltd
Topharman Shandong Co Ltd
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Priority to CN201110236585.3A priority Critical patent/CN102952138B/zh
Application filed by Shanghai Institute of Materia Medica of CAS, Topharman Shanghai Co Ltd, Topharman Shandong Co Ltd filed Critical Shanghai Institute of Materia Medica of CAS
Priority to IN2022CHN2014 priority patent/IN2014CN02022A/en
Priority to EA201490464A priority patent/EA201490464A1/ru
Priority to JP2014525284A priority patent/JP2014521729A/ja
Priority to EP12823704.7A priority patent/EP2746284B1/en
Priority to AU2012297498A priority patent/AU2012297498A1/en
Priority to PCT/CN2012/001082 priority patent/WO2013023439A1/zh
Priority to MX2014001756A priority patent/MX2014001756A/es
Priority to KR1020147007059A priority patent/KR20140059241A/ko
Priority to CA2845250A priority patent/CA2845250A1/en
Priority to US14/238,790 priority patent/US9527849B2/en
Priority to BR112014003696-9A priority patent/BR112014003696A2/pt
Publication of CN102952138A publication Critical patent/CN102952138A/zh
Priority to IL230907A priority patent/IL230907A0/en
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    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/06—Antiabortive agents; Labour repressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Otolaryngology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN201110236585.3A 2011-08-17 2011-08-17 一种吡唑并嘧啶酮化合物的盐、多晶型物及其药物组合物、制备方法和应用 Active CN102952138B (zh)

Priority Applications (13)

Application Number Priority Date Filing Date Title
CN201110236585.3A CN102952138B (zh) 2011-08-17 2011-08-17 一种吡唑并嘧啶酮化合物的盐、多晶型物及其药物组合物、制备方法和应用
US14/238,790 US9527849B2 (en) 2011-08-17 2012-08-14 Salt and polymorph of pyrazolopyrimidinone compound, and pharmaceutical composition containing the same, preparation method and use thereof
JP2014525284A JP2014521729A (ja) 2011-08-17 2012-08-14 ピラゾロピリミジノン化合物の塩、多形体およびその薬物組成物、製造方法および応用
EP12823704.7A EP2746284B1 (en) 2011-08-17 2012-08-14 Salt and polymorph of pyrazolopyrimidinone compound and drug composition, preparation method and use thereof
AU2012297498A AU2012297498A1 (en) 2011-08-17 2012-08-14 Salt and polymorph of pyrazolopyrimidinone compound, and pharmaceutical composition containing the same, preparation method and use thereof
PCT/CN2012/001082 WO2013023439A1 (zh) 2011-08-17 2012-08-14 一种吡唑并嘧啶酮化合物的盐、多晶型物及其药物组合物、制备方法和应用
IN2022CHN2014 IN2014CN02022A (OSRAM) 2011-08-17 2012-08-14
KR1020147007059A KR20140059241A (ko) 2011-08-17 2012-08-14 피라졸로피리미디논 화합물의 염과 다형체, 약물 조성물, 및 그의 제조 방법과 용도
CA2845250A CA2845250A1 (en) 2011-08-17 2012-08-14 Salt and polymorph of pyrazolopyrimidinone compound, and pharmaceutical composition containing the same, preparation method and use thereof
EA201490464A EA201490464A1 (ru) 2011-08-17 2012-08-14 Соль и полиморф пиразолопиримидинонового соединения и фармацевтическая композиция, содержащая их, их способ получения и применение
BR112014003696-9A BR112014003696A2 (pt) 2011-08-17 2012-08-14 sal e polimorfo do composto de pirazolopirimidinona e composição farmacêutica contendo o mesmo método de preparo e seu uso
MX2014001756A MX2014001756A (es) 2011-08-17 2012-08-14 Compuesto de sal y polimorfo de pirazolopirimidinona, y composición farmacéutica que lo contiene, método de preparación y uso del mismo.
IL230907A IL230907A0 (en) 2011-08-17 2014-02-10 Salt and formations of a pyrazolopyrimidine compound, a medical composition that includes the above, and a preparation and use process for them

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN201110236585.3A CN102952138B (zh) 2011-08-17 2011-08-17 一种吡唑并嘧啶酮化合物的盐、多晶型物及其药物组合物、制备方法和应用

Publications (2)

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CN102952138A CN102952138A (zh) 2013-03-06
CN102952138B true CN102952138B (zh) 2016-07-06

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Country Status (13)

Country Link
US (1) US9527849B2 (OSRAM)
EP (1) EP2746284B1 (OSRAM)
JP (1) JP2014521729A (OSRAM)
KR (1) KR20140059241A (OSRAM)
CN (1) CN102952138B (OSRAM)
AU (1) AU2012297498A1 (OSRAM)
BR (1) BR112014003696A2 (OSRAM)
CA (1) CA2845250A1 (OSRAM)
EA (1) EA201490464A1 (OSRAM)
IL (1) IL230907A0 (OSRAM)
IN (1) IN2014CN02022A (OSRAM)
MX (1) MX2014001756A (OSRAM)
WO (1) WO2013023439A1 (OSRAM)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
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CN104129803A (zh) * 2014-08-12 2014-11-05 天津市嵩锐医药科技有限公司 稳定的硝普钠晶体化合物、其药物组合物及制备方法
CN105055336A (zh) * 2015-09-24 2015-11-18 青岛华之草医药科技有限公司 一种治疗泌尿外科疾病的枸橼酸西地那非组合物颗粒剂
ES2949662T3 (es) * 2018-02-02 2023-10-02 Genentech Inc Compuesto farmacéutico, sales del mismo, formulaciones del mismo y métodos de fabricación y uso del mismo
CN113493459B (zh) * 2020-04-07 2022-12-13 广州白云山医药集团股份有限公司白云山制药总厂 Pde5抑制剂化合物及其制备方法和应用

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Also Published As

Publication number Publication date
AU2012297498A1 (en) 2014-04-03
BR112014003696A2 (pt) 2017-06-13
MX2014001756A (es) 2014-09-15
IN2014CN02022A (OSRAM) 2015-05-29
EA201490464A1 (ru) 2014-11-28
US20140309241A1 (en) 2014-10-16
CN102952138A (zh) 2013-03-06
EP2746284B1 (en) 2017-04-12
JP2014521729A (ja) 2014-08-28
WO2013023439A1 (zh) 2013-02-21
US9527849B2 (en) 2016-12-27
CA2845250A1 (en) 2013-02-21
EP2746284A1 (en) 2014-06-25
EP2746284A4 (en) 2015-01-14
KR20140059241A (ko) 2014-05-15
IL230907A0 (en) 2014-03-31

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