CN116903624A - 墨蝶呤及其盐的多晶型物 - Google Patents

墨蝶呤及其盐的多晶型物 Download PDF

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Publication number
CN116903624A
CN116903624A CN202310843616.4A CN202310843616A CN116903624A CN 116903624 A CN116903624 A CN 116903624A CN 202310843616 A CN202310843616 A CN 202310843616A CN 116903624 A CN116903624 A CN 116903624A
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Prior art keywords
free base
ray diffraction
aminopterin
crystalline
peaks
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CN202310843616.4A
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Chinese (zh)
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D.E.莱维
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Ptc Medical Mp Co
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Ptc Medical Mp Co
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
    • C07D475/02—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4
    • C07D475/04—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • 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
    • C07B2200/07—Optical isomers
    • 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Reproductive Health (AREA)
  • Emergency Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
CN202310843616.4A 2016-11-29 2017-11-28 墨蝶呤及其盐的多晶型物 Pending CN116903624A (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201662427686P 2016-11-29 2016-11-29
US62/427686 2016-11-29
US201762546390P 2017-08-16 2017-08-16
US62/546390 2017-08-16
PCT/US2017/063517 WO2018102315A1 (en) 2016-11-29 2017-11-28 Polymoprhs of sepiapterin and salts thereof
CN201780084821.XA CN110248948B (zh) 2016-11-29 2017-11-28 墨蝶呤及其盐的多晶型物

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201780084821.XA Division CN110248948B (zh) 2016-11-29 2017-11-28 墨蝶呤及其盐的多晶型物

Publications (1)

Publication Number Publication Date
CN116903624A true CN116903624A (zh) 2023-10-20

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CN201780084821.XA Active CN110248948B (zh) 2016-11-29 2017-11-28 墨蝶呤及其盐的多晶型物

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US (4) US11072614B2 (https=)
EP (1) EP3548497A4 (https=)
JP (3) JP7148533B2 (https=)
KR (3) KR102561697B1 (https=)
CN (2) CN116903624A (https=)
AU (3) AU2017366879C1 (https=)
BR (1) BR122021026889A8 (https=)
CA (1) CA3043502A1 (https=)
CO (1) CO2019006018A2 (https=)
IL (2) IL266955B2 (https=)
MA (1) MA46973A (https=)
MX (3) MX386520B (https=)
WO (1) WO2018102315A1 (https=)

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MA46973A (fr) 2016-11-29 2019-10-09 Censa Pharmaceuticals Inc Polymorphes de sépiaptérine et leurs sels
MA46972A (fr) 2016-11-29 2019-10-09 Censa Pharmaceuticals Inc Forme polymorphe de sépiaptérine
JP7811085B2 (ja) * 2017-09-01 2026-02-04 ピーティーシー セラピューティクス エムピー，インコーポレイテッド セピアプテリンを含む医薬組成物及びその使用
FI3801536T3 (fi) 2018-05-30 2024-08-29 Ptc Therapeutics Mp Inc Sepiapteriinin antaminen ilman ruokaa käytettäväksi menetelmässä sepiapteriinin plasma-altistuksen lisäämiseksi
EP3801534B1 (en) 2018-05-30 2026-02-18 PTC Therapeutics MP, Inc. Treatment of phenylketonuria with sepiapterin
AU2019277372B2 (en) 2018-05-30 2024-12-19 Ptc Therapeutics Mp, Inc. Pharmaceutically acceptable salts of sepiapterin
IL290321B1 (en) 2019-08-05 2026-04-01 Ptc Therapeutics Inc Use of spiapterin and its metabolites for radiation exposure treatment
IL291565B1 (en) * 2019-09-25 2026-04-01 Ptc Therapeutics Inc Method for treating phenylalanine irregularity
EP4093405A1 (en) 2020-01-24 2022-11-30 PTC Therapeutics MP, Inc. Methods for treating parkinson's disease with sepiapterin
WO2022173823A1 (en) 2021-02-09 2022-08-18 Ptc Therapeutics Mp, Inc. Methods for treating covid-19 with sepiapterin
IL305037A (en) 2021-02-09 2023-10-01 Ptc Therapeutics Mp Inc Methods of treating glioblastomas with spiafatrin
PE20241579A1 (es) 2021-09-29 2024-08-01 Ptc Therapeutics Inc Composicion farmaceutica de sepiapterina
WO2024249602A2 (en) * 2023-05-30 2024-12-05 The Board Of Trustees Of The Leland Stanford Junior University Restless leg syndrome (rls) and periodic leg movements (plms) during sleep: biomarker and drug target
CN117205164B (zh) * 2023-09-30 2024-07-26 山东新时代药业有限公司 一种盐酸沙丙蝶呤片剂及其制备方法

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US20070270581A1 (en) * 2004-11-17 2007-11-22 Biomarin Pharmaceutical Inc. Stable Tablet Formulation
CN104736539A (zh) * 2012-05-07 2015-06-24 白鸟制药株式会社 墨蝶呤和四氢乳酰蝶呤的制造法
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JP7148533B2 (ja) 2022-10-05
KR20250051124A (ko) 2025-04-16
BR112019010222A8 (pt) 2022-11-22
US12269829B2 (en) 2025-04-08
KR102789662B1 (ko) 2025-04-03
CO2019006018A2 (es) 2019-06-19
MX2021011676A (es) 2021-10-22
US20240043426A1 (en) 2024-02-08
MA46973A (fr) 2019-10-09
JP2019535836A (ja) 2019-12-12
BR122021026889A2 (https=) 2019-08-27
IL266955A (en) 2019-07-31
AU2017366879C1 (en) 2022-08-11
WO2018102315A8 (en) 2018-09-07
KR20190086686A (ko) 2019-07-23
JP2024123011A (ja) 2024-09-10
IL301470A (en) 2023-05-01
US11773097B2 (en) 2023-10-03
AU2022203481B2 (en) 2023-10-19
EP3548497A4 (en) 2020-09-02
CA3043502A1 (en) 2018-06-07
CN110248948A (zh) 2019-09-17
AU2022203481A1 (en) 2022-06-16
JP2023002532A (ja) 2023-01-10
AU2024200344A1 (en) 2024-02-08
US11072614B2 (en) 2021-07-27
BR122021026889A8 (pt) 2022-11-22
US20210300930A1 (en) 2021-09-30
AU2024200344B2 (en) 2025-11-06
KR102561697B1 (ko) 2023-07-28
BR112019010222A2 (pt) 2019-08-27
CN110248948B (zh) 2023-07-28
NZ753504A (en) 2025-10-31
EP3548497A1 (en) 2019-10-09
WO2018102315A1 (en) 2018-06-07
IL266955B1 (en) 2023-05-01
US20190308975A1 (en) 2019-10-10
MX2019006206A (es) 2019-08-14
AU2017366879A1 (en) 2019-05-30
MX386520B (es) 2025-03-19
US20250230164A1 (en) 2025-07-17
MX2021011683A (es) 2021-10-22
KR20230117467A (ko) 2023-08-08
AU2017366879B2 (en) 2022-02-24
IL266955B2 (en) 2023-09-01

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