CN112513031A - 可用于治疗与tlr7调节相关的疾病的含酸性基团的嘧啶化合物 - Google Patents

可用于治疗与tlr7调节相关的疾病的含酸性基团的嘧啶化合物 Download PDF

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Publication number
CN112513031A
CN112513031A CN201980050020.0A CN201980050020A CN112513031A CN 112513031 A CN112513031 A CN 112513031A CN 201980050020 A CN201980050020 A CN 201980050020A CN 112513031 A CN112513031 A CN 112513031A
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compound
pharmaceutically acceptable
formula
pharmaceutical composition
acceptable salt
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Chinese (zh)
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T·Y-H·吴
A·T·米勒
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Apros Therapeutics Inc
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Apros Therapeutics Inc
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • C07D239/49Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/10Heterocyclic 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)
CN201980050020.0A 2018-06-04 2019-06-03 可用于治疗与tlr7调节相关的疾病的含酸性基团的嘧啶化合物 Pending CN112513031A (zh)

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 (1)

Publication Number Publication Date
CN112513031A true CN112513031A (zh) 2021-03-16

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Family Applications (1)

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CN201980050020.0A Pending CN112513031A (zh) 2018-06-04 2019-06-03 可用于治疗与tlr7调节相关的疾病的含酸性基团的嘧啶化合物

Country Status (7)

Country Link
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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103313725A (zh) * 2010-09-01 2013-09-18 诺华有限公司 免疫增强剂吸附不溶性金属离子
CN103342682A (zh) * 2007-11-22 2013-10-09 阿斯利康(瑞典)有限公司 用于制备嘧啶衍生物的中间体
CN104302628A (zh) * 2012-05-18 2015-01-21 大日本住友制药株式会社 羧酸化合物

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GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
BR9707495A (pt) 1996-02-13 1999-07-27 Zeneca Ltd Derivado de quinazolina processo para a preparação do mesmo composição farmacêutica e processo para a produç o de um efeito antiangiogênico e/ou de redução de permeabilidade vascular em um animal de sangue quente
US6291455B1 (en) 1996-03-05 2001-09-18 Zeneca Limited 4-anilinoquinazoline derivatives
ATE283855T1 (de) 1996-07-03 2004-12-15 Sumitomo Pharma Neue purinderivate
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SK288365B6 (sk) 1999-02-10 2016-07-01 Astrazeneca Ab Medziprodukty pre chinazolínové deriváty ako inhibítory angiogenézy
CZ301689B6 (cs) 1999-11-05 2010-05-26 Astrazeneca Ab Derivát chinazolinu a farmaceutický prostredek, který ho obsahuje
SI1255752T1 (sl) 2000-02-15 2007-12-31 Pharmacia & Upjohn Co Llc S pirolom substituirani zaviralci 2-indolinon protein kinaza
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JO3257B1 (ar) 2009-09-02 2018-09-16 Novartis Ag مركبات وتركيبات كمعدلات لفاعلية tlr
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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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103342682A (zh) * 2007-11-22 2013-10-09 阿斯利康(瑞典)有限公司 用于制备嘧啶衍生物的中间体
CN103313725A (zh) * 2010-09-01 2013-09-18 诺华有限公司 免疫增强剂吸附不溶性金属离子
CN104302628A (zh) * 2012-05-18 2015-01-21 大日本住友制药株式会社 羧酸化合物

Also Published As

Publication number Publication date
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
JP7351859B2 (ja) 2023-09-27
EP3802519A1 (en) 2021-04-14

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Application publication date: 20210316