CN114728972B - C-c趋化因子受体4型拮抗剂的结晶形式及其用途 - Google Patents

C-c趋化因子受体4型拮抗剂的结晶形式及其用途 Download PDF

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Publication number
CN114728972B
CN114728972B CN202080076933.2A CN202080076933A CN114728972B CN 114728972 B CN114728972 B CN 114728972B CN 202080076933 A CN202080076933 A CN 202080076933A CN 114728972 B CN114728972 B CN 114728972B
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disease
pyrazin
pyrazolo
dichlorophenyl
azetidin
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CN114728972A (zh
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D·J·亚诺尔德
O·罗布莱斯
D·E·鲁迪西尔
D·J·武斯特罗
M·齐宾斯基
S·卡拉博尔尼
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Rapt Medical Co
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Rapt Medical Co
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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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • 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
    • 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
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2818—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against CD28 or CD152
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN202080076933.2A 2019-11-13 2020-11-13 C-c趋化因子受体4型拮抗剂的结晶形式及其用途 Active CN114728972B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962935007P 2019-11-13 2019-11-13
US62/935,007 2019-11-13
PCT/US2020/060575 WO2021097339A1 (en) 2019-11-13 2020-11-13 Crystalline forms of c-c chemokine receptor type 4 antagonist and uses thereof

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CN114728972A CN114728972A (zh) 2022-07-08
CN114728972B true CN114728972B (zh) 2024-12-10

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US (2) US12006318B2 (https=)
EP (1) EP4058456A1 (https=)
JP (2) JP2023501584A (https=)
KR (1) KR20220101099A (https=)
CN (1) CN114728972B (https=)
BR (1) BR112022009331A2 (https=)
CA (1) CA3158521A1 (https=)
IL (1) IL292755A (https=)
MX (1) MX2022005795A (https=)
WO (1) WO2021097339A1 (https=)
ZA (1) ZA202204943B (https=)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4058456A1 (en) 2019-11-13 2022-09-21 RAPT Therapeutics, Inc. Crystalline forms of c-c chemokine receptor type 4 antagonist and uses thereof
CN121002023A (zh) * 2023-04-24 2025-11-21 浙江华海药业股份有限公司 趋化因子受体调节剂制备方法和用途

Citations (2)

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WO2019090272A1 (en) * 2017-11-06 2019-05-09 Flx Bio, Inc. Chemokine receptor modulators for treatment of epstein barr virus positive cancer
CN109789146A (zh) * 2016-07-29 2019-05-21 Flx生物公司 趋化因子受体调节剂及其用途

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US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US3916899A (en) 1973-04-25 1975-11-04 Alza Corp Osmotic dispensing device with maximum and minimum sizes for the passageway
US4911920A (en) 1986-07-30 1990-03-27 Alcon Laboratories, Inc. Sustained release, comfort formulation for glaucoma therapy
FR2588189B1 (fr) 1985-10-03 1988-12-02 Merck Sharp & Dohme Composition pharmaceutique de type a transition de phase liquide-gel
DE3815221C2 (de) 1988-05-04 1995-06-29 Gradinger F Hermes Pharma Verwendung einer Retinol- und/oder Retinsäureester enthaltenden pharmazeutischen Zubereitung zur Inhalation zur Einwirkung auf die Schleimhäute des Tracheo-Bronchialtraktes einschließlich der Lungenalveolen
JP2594486B2 (ja) 1991-01-15 1997-03-26 アルコン ラボラトリーズ インコーポレイテッド 局所的眼薬組成物
US5212162A (en) 1991-03-27 1993-05-18 Alcon Laboratories, Inc. Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions
US5698155A (en) 1991-05-31 1997-12-16 Gs Technologies, Inc. Method for the manufacture of pharmaceutical cellulose capsules
JP2008530211A (ja) * 2005-02-16 2008-08-07 メルク エンド カムパニー インコーポレーテッド ケモカイン受容体のモジュレーターとなる置換ピラゾール
TW201024298A (en) * 2008-09-23 2010-07-01 Palau Pharma Sa (R)-3-(N,N-dimethylamino)pyrrolidine derivatives
US8383812B2 (en) * 2009-10-13 2013-02-26 Bristol-Myers Squibb Company N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-A][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, a dual modulator of chemokine receptor activity, crystalline forms and processes
JP2013031931A (ja) * 2011-08-01 2013-02-14 Hitachi Koki Co Ltd 携帯式作業機
TW201311693A (zh) * 2011-09-02 2013-03-16 Kyowa Hakko Kirin Co Ltd 化學激活激素受體活性調節劑
AR096758A1 (es) * 2013-06-28 2016-02-03 Abbvie Inc Inhibidores cristalinos de bromodominios
US10246462B2 (en) * 2016-09-09 2019-04-02 Flx Bio, Inc. Chemokine receptor modulators and uses thereof
JP2020533332A (ja) * 2017-09-12 2020-11-19 アルデア バイオサイエンシーズ インク． 障害を処置するためのｃｘｃｒ−２阻害剤
CN109796457B (zh) * 2019-03-28 2020-03-06 苏州国匡医药科技有限公司 一种2-(3-(氮杂环丁烷-3-基)哌啶-1-基)乙基-1-醇的制备方法及其应用
EP4058456A1 (en) 2019-11-13 2022-09-21 RAPT Therapeutics, Inc. Crystalline forms of c-c chemokine receptor type 4 antagonist and uses thereof

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109789146A (zh) * 2016-07-29 2019-05-21 Flx生物公司 趋化因子受体调节剂及其用途
WO2019090272A1 (en) * 2017-11-06 2019-05-09 Flx Bio, Inc. Chemokine receptor modulators for treatment of epstein barr virus positive cancer

Also Published As

Publication number Publication date
CN114728972A (zh) 2022-07-08
JP2023501584A (ja) 2023-01-18
JP2026012675A (ja) 2026-01-27
US12006318B2 (en) 2024-06-11
AU2020383625A1 (en) 2022-05-05
ZA202204943B (en) 2023-11-29
KR20220101099A (ko) 2022-07-19
WO2021097339A1 (en) 2021-05-20
TW202132303A (zh) 2021-09-01
EP4058456A1 (en) 2022-09-21
MX2022005795A (es) 2022-06-08
IL292755A (en) 2022-07-01
CA3158521A1 (en) 2021-05-20
US20210139487A1 (en) 2021-05-13
US20240317768A1 (en) 2024-09-26
BR112022009331A2 (pt) 2022-08-09

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