CN114302724A - 用于治疗镰状细胞病的pde9抑制剂 - Google Patents

用于治疗镰状细胞病的pde9抑制剂 Download PDF

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Publication number
CN114302724A
CN114302724A CN202080041606.3A CN202080041606A CN114302724A CN 114302724 A CN114302724 A CN 114302724A CN 202080041606 A CN202080041606 A CN 202080041606A CN 114302724 A CN114302724 A CN 114302724A
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Prior art keywords
pharmaceutical composition
compound
flavoring
pharmaceutically acceptable
hydrate
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CN202080041606.3A
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Chinese (zh)
Inventor
尼尔斯·斯文斯楚普
瓦尼克·彼得罗西安
大卫·蒂西
杰弗里·沃辛顿
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Cardurion Pharmaceuticals Inc
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Imara Inc
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    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
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    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2068—Compounds of unknown constitution, e.g. material from plants or animals
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61P7/06—Antianaemics

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  • Health & Medical Sciences (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biophysics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Botany (AREA)
  • Zoology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
CN202080041606.3A 2019-04-05 2020-04-03 用于治疗镰状细胞病的pde9抑制剂 Pending CN114302724A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962829784P 2019-04-05 2019-04-05
US62/829,784 2019-04-05
PCT/US2020/026696 WO2020206336A1 (en) 2019-04-05 2020-04-03 Pde9 inhibitors for treating sickle cell disease

Publications (1)

Publication Number Publication Date
CN114302724A true CN114302724A (zh) 2022-04-08

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CN202080041606.3A Pending CN114302724A (zh) 2019-04-05 2020-04-03 用于治疗镰状细胞病的pde9抑制剂

Country Status (9)

Country Link
US (1) US20220023302A1 (https=)
EP (1) EP3946348A4 (https=)
JP (1) JP2022527630A (https=)
CN (1) CN114302724A (https=)
BR (1) BR112021019876A2 (https=)
CA (1) CA3136128A1 (https=)
IL (1) IL286976A (https=)
WO (1) WO2020206336A1 (https=)
ZA (1) ZA202107544B (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT3865484T (pt) 2015-07-07 2024-01-30 H Lundbeck As Inibidor da pde9 com esqueleto de imidazo pirazinona para tratamento de doenças periféricas
CA3100988A1 (en) 2018-05-25 2019-11-28 Imara Inc. Monohydrate and crystalline forms of 6-[(3s,4s)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-3-tetrahydropyran-4-yl-7h-imidazo[1,5-a]pyrazin-8-one
CA3110680A1 (en) 2018-08-31 2020-03-05 Imara Inc. Pde9 inhibitors for treating sickle cell disease

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018009424A1 (en) * 2016-07-06 2018-01-11 Imara, Inc. Pde9 inhibitors for treatment of peripheral diseases
US20180194770A1 (en) * 2015-07-07 2018-07-12 H. Lundbeck A/S Pde9 inhibitors with imidazo triazinone backbone and imidazo pyrazinone backbone for treatment of peripheral diseases
WO2018218104A1 (en) * 2017-05-26 2018-11-29 Imara, Inc. Methods of making and using pde9 inhibitors

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009507032A (ja) * 2005-09-02 2009-02-19 アボット・ラボラトリーズ 新規なイミダゾ系複素環
JP4941977B2 (ja) * 2007-04-11 2012-05-30 大蔵製薬株式会社 ベンズイソキサゾール誘導体の経口ゼリー状医薬組成物
BR112015007731B1 (pt) * 2011-10-10 2022-05-31 H. Lundbeck A/S Composto, composição farmacêutica que o compreende e uso do mesmo
EP2868319A4 (en) * 2012-06-29 2016-02-24 Maruishi Pharma ORAL PHARMACEUTICAL ARIPIPRAZONE PREPARATION
US10045991B2 (en) * 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
EP3965768A1 (en) * 2019-05-07 2022-03-16 Imara Inc. Pde9 inhibitors for treating thalassemia

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20180194770A1 (en) * 2015-07-07 2018-07-12 H. Lundbeck A/S Pde9 inhibitors with imidazo triazinone backbone and imidazo pyrazinone backbone for treatment of peripheral diseases
WO2018009424A1 (en) * 2016-07-06 2018-01-11 Imara, Inc. Pde9 inhibitors for treatment of peripheral diseases
WO2018218104A1 (en) * 2017-05-26 2018-11-29 Imara, Inc. Methods of making and using pde9 inhibitors

Also Published As

Publication number Publication date
WO2020206336A1 (en) 2020-10-08
ZA202107544B (en) 2022-08-31
BR112021019876A2 (pt) 2022-01-18
IL286976A (en) 2021-12-01
JP2022527630A (ja) 2022-06-02
CA3136128A1 (en) 2020-10-08
US20220023302A1 (en) 2022-01-27
EP3946348A4 (en) 2023-08-02
EP3946348A1 (en) 2022-02-09

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Effective date of registration: 20240610

Address after: Massachusetts, USA

Applicant after: Cadurion Pharmaceuticals

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Applicant before: IMARA Inc.

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Application publication date: 20220408