JP7351859B2 - Ｔｌｒ７の調節に関係する疾患を処置するのに有用な酸性基を含むピリミジン化合物 - Google Patents

Ｔｌｒ７の調節に関係する疾患を処置するのに有用な酸性基を含むピリミジン化合物 Download PDF

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JP7351859B2
JP7351859B2 JP2020567199A JP2020567199A JP7351859B2 JP 7351859 B2 JP7351859 B2 JP 7351859B2 JP 2020567199 A JP2020567199 A JP 2020567199A JP 2020567199 A JP2020567199 A JP 2020567199A JP 7351859 B2 JP7351859 B2 JP 7351859B2
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JP2021525771A (ja
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トム ヤオ－シャン ウー，
アンドリュー ティー． ミラー，
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アプロス セラピューティクス， インコーポレイテッド
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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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C07D239/49—Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • 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
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Inorganic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Otolaryngology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
JP2020567199A 2018-06-04 2019-06-03 Ｔｌｒ７の調節に関係する疾患を処置するのに有用な酸性基を含むピリミジン化合物 Active JP7351859B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862680324P 2018-06-04 2018-06-04
US62/680,324 2018-06-04
PCT/US2019/035247 WO2019236496A1 (en) 2018-06-04 2019-06-03 Pyrimidine compounds containing acidic groups useful to treat diseases connected to the modulation of tlr7

Publications (4)

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JP2021525771A JP2021525771A (ja) 2021-09-27
JP2021525771A5 JP2021525771A5 (https=) 2022-06-06
JPWO2019236496A5 JPWO2019236496A5 (https=) 2022-06-06
JP7351859B2 true JP7351859B2 (ja) 2023-09-27

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US (1) US10857153B2 (https=)
EP (1) EP3802519A1 (https=)
JP (1) JP7351859B2 (https=)
CN (1) CN112513031A (https=)
AR (1) AR114910A1 (https=)
TW (1) TW202003475A (https=)
WO (1) WO2019236496A1 (https=)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10786502B2 (en) 2016-12-05 2020-09-29 Apros Therapeutics, Inc. Substituted pyrimidines containing acidic groups as TLR7 modulators
JP7351859B2 (ja) 2018-06-04 2023-09-27 アプロス セラピューティクス， インコーポレイテッド Ｔｌｒ７の調節に関係する疾患を処置するのに有用な酸性基を含むピリミジン化合物

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009542645A (ja) 2006-07-05 2009-12-03 アストラゼネカ・アクチエボラーグ Ｔｌｒ７のモジュレーターとして作用する８−オキソアデニン誘導体
JP2011504497A (ja) 2007-11-22 2011-02-10 アストラゼネカ・アクチエボラーグ 喘息、ｃｏｐｄ、アレルギー性鼻炎、アレルギー性結膜炎、アトピー性皮膚炎、癌、ｂ型肝炎、ｃ型肝炎、ｈｉｖ、ｈｐｖ、細菌感染症および皮膚症の処置のためのピリミジン誘導体
JP2013503884A (ja) 2009-09-02 2013-02-04 アイアールエム・リミテッド・ライアビリティ・カンパニー Ｔｌｒ活性モジュレーターとしての化合物および組成物
JP2013538217A (ja) 2010-09-01 2013-10-10 ノバルティス アーゲー 不溶性金属塩への免疫増強物質の吸着
JP2015520729A (ja) 2012-05-18 2015-07-23 大日本住友製薬株式会社 カルボン酸化合物
JP7071392B2 (ja) 2016-12-05 2022-05-18 アプロス セラピューティクス， インコーポレイテッド 酸性基を含有するピリミジン化合物

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US6291455B1 (en) 1996-03-05 2001-09-18 Zeneca Limited 4-anilinoquinazoline derivatives
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JP7351859B2 (ja) 2018-06-04 2023-09-27 アプロス セラピューティクス， インコーポレイテッド Ｔｌｒ７の調節に関係する疾患を処置するのに有用な酸性基を含むピリミジン化合物

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009542645A (ja) 2006-07-05 2009-12-03 アストラゼネカ・アクチエボラーグ Ｔｌｒ７のモジュレーターとして作用する８−オキソアデニン誘導体
JP2011504497A (ja) 2007-11-22 2011-02-10 アストラゼネカ・アクチエボラーグ 喘息、ｃｏｐｄ、アレルギー性鼻炎、アレルギー性結膜炎、アトピー性皮膚炎、癌、ｂ型肝炎、ｃ型肝炎、ｈｉｖ、ｈｐｖ、細菌感染症および皮膚症の処置のためのピリミジン誘導体
JP2013503884A (ja) 2009-09-02 2013-02-04 アイアールエム・リミテッド・ライアビリティ・カンパニー Ｔｌｒ活性モジュレーターとしての化合物および組成物
JP2013538217A (ja) 2010-09-01 2013-10-10 ノバルティス アーゲー 不溶性金属塩への免疫増強物質の吸着
JP2015520729A (ja) 2012-05-18 2015-07-23 大日本住友製薬株式会社 カルボン酸化合物
JP7071392B2 (ja) 2016-12-05 2022-05-18 アプロス セラピューティクス， インコーポレイテッド 酸性基を含有するピリミジン化合物

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TW202003475A (zh) 2020-01-16
AR114910A1 (es) 2020-10-28
US20190365756A1 (en) 2019-12-05
JP2021525771A (ja) 2021-09-27
WO2019236496A1 (en) 2019-12-12
US10857153B2 (en) 2020-12-08
CN112513031A (zh) 2021-03-16
EP3802519A1 (en) 2021-04-14

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