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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Pending
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CN202310843616.4A
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English (en)
Chinese (zh)
Inventor
D.E.莱维
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Ptc Medical Mp Co
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Ptc Medical Mp Co
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Publication of CN116903624A publication Critical patent/CN116903624A/zh
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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)
  • Neurology (AREA)
  • Biomedical Technology (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
CN201780084821.XA CN110248948B (zh) 2016-11-29 2017-11-28 墨蝶呤及其盐的多晶型物
PCT/US2017/063517 WO2018102315A1 (en) 2016-11-29 2017-11-28 Polymoprhs of sepiapterin and salts thereof

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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US (4) US11072614B2 (enExample)
EP (1) EP3548497A4 (enExample)
JP (3) JP7148533B2 (enExample)
KR (3) KR102561697B1 (enExample)
CN (2) CN116903624A (enExample)
AU (3) AU2017366879C1 (enExample)
BR (1) BR122021026889A8 (enExample)
CA (1) CA3043502A1 (enExample)
CO (1) CO2019006018A2 (enExample)
IL (2) IL266955B2 (enExample)
MA (1) MA46973A (enExample)
MX (3) MX386520B (enExample)
NZ (1) NZ753504A (enExample)
WO (1) WO2018102315A1 (enExample)

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IL266955B2 (en) 2016-11-29 2023-09-01 Ptc Therapeutics Mp Inc Polymorphs of spiafatrin and its salts
WO2019046849A1 (en) 2017-09-01 2019-03-07 Censa Pharmaceuticals Inc. PHARMACEUTICAL COMPOSITION COMPRISING SEPAPTERINE AND USES THEREOF
SMT202400430T1 (it) 2018-05-30 2024-11-15 Ptc Therapeutics Mp Inc Somministrazione di sepiapterina, senza alcun alimento, per uso in un metodo per incrementare l’esposizione plasmatica di sepiapterina
EP3801534A4 (en) 2018-05-30 2022-03-16 PTC Therapeutics MP, Inc. COMPOSITIONS AND METHODS TO INCREASE TETRAHYDROBIOPTERIN PLASMA EXPOSURE
CA3102070A1 (en) 2018-05-30 2019-12-05 Ptc Therapeutics Mp, Inc. Pharmaceutically acceptable salts of sepiapterin
ES2994060T3 (en) 2019-08-05 2025-01-16 Ptc Therapeutics Mp Inc Use of sepiapterin and metabolites thereof to treat radiation exposure
KR20220070477A (ko) * 2019-09-25 2022-05-31 피티씨 테라퓨틱스 엠피, 인크. 고페닐알라닌혈증 치료 방법
AU2021209935A1 (en) 2020-01-24 2022-08-18 Ptc Therapeutics Mp, Inc. Methods for treating Parkinson's disease with sepiapterin
JP2024506336A (ja) 2021-02-09 2024-02-13 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 膠芽腫の治療方法
WO2022173823A1 (en) 2021-02-09 2022-08-18 Ptc Therapeutics Mp, Inc. Methods for treating covid-19 with sepiapterin
WO2023055923A1 (en) 2021-09-29 2023-04-06 Ptc Therapeutics, Inc. Pharmaceutical composition of sepiapterin
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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CN110248948B (zh) 2023-07-28
AU2017366879B2 (en) 2022-02-24
CN110248948A (zh) 2019-09-17
EP3548497A1 (en) 2019-10-09
MA46973A (fr) 2019-10-09
BR112019010222A2 (pt) 2019-08-27
BR112019010222A8 (pt) 2022-11-22
AU2017366879C1 (en) 2022-08-11
WO2018102315A1 (en) 2018-06-07
MX2021011676A (es) 2021-10-22
BR122021026889A2 (enExample) 2019-08-27
KR20190086686A (ko) 2019-07-23
MX2021011683A (es) 2021-10-22
WO2018102315A8 (en) 2018-09-07
CO2019006018A2 (es) 2019-06-19
US20250230164A1 (en) 2025-07-17
US11773097B2 (en) 2023-10-03
AU2024200344A1 (en) 2024-02-08
IL266955B2 (en) 2023-09-01
US20190308975A1 (en) 2019-10-10
IL301470A (en) 2023-05-01
AU2024200344B2 (en) 2025-11-06
JP7148533B2 (ja) 2022-10-05
EP3548497A4 (en) 2020-09-02
US20210300930A1 (en) 2021-09-30
JP2023002532A (ja) 2023-01-10
US11072614B2 (en) 2021-07-27
IL266955A (en) 2019-07-31
KR20250051124A (ko) 2025-04-16
KR20230117467A (ko) 2023-08-08
AU2022203481B2 (en) 2023-10-19
JP2024123011A (ja) 2024-09-10
AU2017366879A1 (en) 2019-05-30
JP2019535836A (ja) 2019-12-12
KR102789662B1 (ko) 2025-04-03
AU2022203481A1 (en) 2022-06-16
MX386520B (es) 2025-03-19
KR102561697B1 (ko) 2023-07-28
CA3043502A1 (en) 2018-06-07
US12269829B2 (en) 2025-04-08
IL266955B1 (en) 2023-05-01
MX2019006206A (es) 2019-08-14
US20240043426A1 (en) 2024-02-08
NZ753504A (en) 2025-10-31
BR122021026889A8 (pt) 2022-11-22

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