CN113747870B - 氟利色林的氘化形式和衍生物 - Google Patents

氟利色林的氘化形式和衍生物

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Publication number
CN113747870B
CN113747870B CN201980092743.7A CN201980092743A CN113747870B CN 113747870 B CN113747870 B CN 113747870B CN 201980092743 A CN201980092743 A CN 201980092743A CN 113747870 B CN113747870 B CN 113747870B
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China
Prior art keywords
compound
deuterium
compounds
mmol
pharmaceutically acceptable
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CN201980092743.7A
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English (en)
Chinese (zh)
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CN113747870A (zh
Inventor
S·温特劳布
S·L·哈比森
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Tailan Biotechnology Co ltd
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Tailan Biotechnology Co ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C07D211/22—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61J—CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
    • A61J1/00—Containers specially adapted for medical or pharmaceutical purposes
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/10—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/14—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/70571—Receptors; Cell surface antigens; Cell surface determinants for neuromediators, e.g. serotonin receptor, dopamine receptor
    • 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
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Endocrinology (AREA)
  • Toxicology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Cell Biology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN201980092743.7A 2018-12-21 2019-12-20 氟利色林的氘化形式和衍生物 Active CN113747870B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862784056P 2018-12-21 2018-12-21
US62/784,056 2018-12-21
PCT/US2019/067885 WO2020132461A1 (en) 2018-12-21 2019-12-20 Deuterated forms and derivatives of volinanserin

Publications (2)

Publication Number Publication Date
CN113747870A CN113747870A (zh) 2021-12-03
CN113747870B true CN113747870B (zh) 2025-08-01

Family

ID=71101633

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Application Number Title Priority Date Filing Date
CN201980092743.7A Active CN113747870B (zh) 2018-12-21 2019-12-20 氟利色林的氘化形式和衍生物

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US (2) US20220106272A1 (enExample)
EP (1) EP3897507A4 (enExample)
JP (2) JP7548906B2 (enExample)
KR (1) KR20210124976A (enExample)
CN (1) CN113747870B (enExample)
AU (1) AU2019403391A1 (enExample)
BR (1) BR112021012082A8 (enExample)
CA (1) CA3124399A1 (enExample)
EA (1) EA202191731A1 (enExample)
IL (1) IL284201A (enExample)
MX (1) MX2021007437A (enExample)
SG (1) SG11202106692UA (enExample)
WO (1) WO2020132461A1 (enExample)
ZA (1) ZA202104656B (enExample)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115057774A (zh) * 2022-04-28 2022-09-16 北京绮一舟新材料技术有限公司 一种α-氘代羧酸衍生物类化合物及氘代药物的合成方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009020569A1 (en) * 2007-08-06 2009-02-12 Merck & Co., Inc. Treatment of psychosis with a 5ht2a antagonist and a metabotropic glutamate receptor agonist or potentiator
CN103649019A (zh) * 2011-06-20 2014-03-19 H.隆德贝克有限公司 用于治疗精神分裂症的氘化的1-哌嗪子基-3-苯基-茚满
CN103702961A (zh) * 2011-05-23 2014-04-02 赛诺菲 含有n-烷基的氘代化合物的制备方法
WO2018023009A1 (en) * 2016-07-29 2018-02-01 Concert Pharmaceuticals, Inc. Deuterated lurasidone

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2570961C (en) * 2004-06-21 2015-09-01 University Of Mississippi Anticancer and antiprotozoal dihydroartemisinene and dihydroartemisitene dimers with desirable chemical functionalities
US8198305B2 (en) * 2007-04-13 2012-06-12 Concert Pharmaceuticals Inc. 1,2-benzisoxazol-3-yl compounds
US8609673B2 (en) * 2008-01-22 2013-12-17 Concert Pharmaceuticals, Inc. Vandetanib derivatives
WO2012039660A1 (en) * 2010-09-20 2012-03-29 A. Carlsson Research Ab Phenylpiperidine compounds for the treatment of neurological and psychiatric disorders
WO2014145718A2 (en) * 2013-03-15 2014-09-18 Longevity Biotech, Inc. Peptides comprising non-natural amino acids and methods of making and using the same

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009020569A1 (en) * 2007-08-06 2009-02-12 Merck & Co., Inc. Treatment of psychosis with a 5ht2a antagonist and a metabotropic glutamate receptor agonist or potentiator
CN103702961A (zh) * 2011-05-23 2014-04-02 赛诺菲 含有n-烷基的氘代化合物的制备方法
CN103649019A (zh) * 2011-06-20 2014-03-19 H.隆德贝克有限公司 用于治疗精神分裂症的氘化的1-哌嗪子基-3-苯基-茚满
WO2018023009A1 (en) * 2016-07-29 2018-02-01 Concert Pharmaceuticals, Inc. Deuterated lurasidone

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Krisztina Németh，et al..Development ofnovelchiralcapillaryelectrophoresismethodsforthe serotonin receptor(5-HT2A) antagonistMDL100,907(volinanserin) and foritskeyintermediatecompound.《Journal ofPharmaceuticalandBiomedicalAnalysis》.2013,第88卷579-583. *

Also Published As

Publication number Publication date
SG11202106692UA (en) 2021-07-29
IL284201A (en) 2021-08-31
JP2024163142A (ja) 2024-11-21
JP7548906B2 (ja) 2024-09-10
KR20210124976A (ko) 2021-10-15
AU2019403391A1 (en) 2021-08-05
US20250066302A1 (en) 2025-02-27
BR112021012082A8 (pt) 2023-03-21
US20220106272A1 (en) 2022-04-07
WO2020132461A1 (en) 2020-06-25
EP3897507A1 (en) 2021-10-27
CA3124399A1 (en) 2020-06-25
BR112021012082A2 (pt) 2021-08-31
CN113747870A (zh) 2021-12-03
EP3897507A4 (en) 2022-09-14
JP2022515156A (ja) 2022-02-17
MX2021007437A (es) 2021-09-08
ZA202104656B (en) 2022-10-26
EA202191731A1 (ru) 2021-10-28

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