CN111194318B - 用于调节激酶的化合物固体形式 - Google Patents

用于调节激酶的化合物固体形式 Download PDF

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CN111194318B
CN111194318B CN201880063415.XA CN201880063415A CN111194318B CN 111194318 B CN111194318 B CN 111194318B CN 201880063415 A CN201880063415 A CN 201880063415A CN 111194318 B CN111194318 B CN 111194318B
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compound
free acid
disease
salt
amorphous
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CN111194318A (zh
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P·N·易卜拉欣
H·礼萨伊
M·尼西
B·鲍威尔
R·帕特尔
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Opna Bio SA
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Opna Biology
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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)
  • 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)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Quinoline Compounds (AREA)
  • Control Of Indicators Other Than Cathode Ray Tubes (AREA)
CN201880063415.XA 2017-10-13 2018-10-11 用于调节激酶的化合物固体形式 Active CN111194318B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762572099P 2017-10-13 2017-10-13
US62/572,099 2017-10-13
PCT/US2018/055473 WO2019075243A1 (en) 2017-10-13 2018-10-11 SOLID FORMS OF A COMPOUND FOR MODULATING KINASES

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CN111194318A CN111194318A (zh) 2020-05-22
CN111194318B true CN111194318B (zh) 2023-06-09

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EP (1) EP3694855A1 (enExample)
JP (1) JP7675519B2 (enExample)
CN (1) CN111194318B (enExample)
AU (1) AU2018348241B2 (enExample)
CA (1) CA3079029A1 (enExample)
TW (1) TW201922742A (enExample)
WO (1) WO2019075243A1 (enExample)

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CN108137585B (zh) 2015-09-21 2021-10-22 普莱希科公司 杂环化合物及其应用
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JP7175309B2 (ja) 2017-10-27 2022-11-18 プレキシコン インコーポレーテッド キナーゼを調節する化合物の製剤
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US20240108639A1 (en) * 2020-12-11 2024-04-04 Board Of Regents, The University Of Texas System Compositions and methods of making cocrystals using dielectric heating with dispersive and distributive mixing
CN113456626B (zh) * 2021-08-16 2022-05-06 吉林大学 一种黄嘌呤氧化酶抑制剂及其筛选方法和应用
CN116473968A (zh) * 2022-01-24 2023-07-25 华中科技大学 Ezh2特异性抑制剂在治疗哮喘的用途
CN114984011A (zh) * 2022-07-11 2022-09-02 中南大学湘雅二医院 吡咯并吡啶类化合物在制备治疗狼疮药物中的应用
CN120916769A (zh) * 2022-12-20 2025-11-07 星座制药公司 用于治疗较低风险骨髓增生异常综合征的方法
AU2023415105A1 (en) 2022-12-30 2025-07-17 Avicenna Biosciences, Inc. Azaindole rock inhibitors
KR20250044972A (ko) * 2023-09-25 2025-04-01 주식회사 마스터메디텍 이델라리십 함유 경구투여용 고형제제 및 그 제조방법
CN119219631B (zh) * 2024-12-04 2025-04-18 山东大学 一种bet蛋白溴结构域bd1选择性共价抑制剂及其制备方法与应用

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