CN110944978A - 含恩替诺特的化合物,其化合物晶型及其制备方法和药物组合物 - Google Patents

含恩替诺特的化合物,其化合物晶型及其制备方法和药物组合物 Download PDF

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CN110944978A
CN110944978A CN201780092661.3A CN201780092661A CN110944978A CN 110944978 A CN110944978 A CN 110944978A CN 201780092661 A CN201780092661 A CN 201780092661A CN 110944978 A CN110944978 A CN 110944978A
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Prior art keywords
compound
entinostat
solvent
acid
solution
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盛晓红
盛晓霞
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SOLIPHARMA LLC
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SOLIPHARMA LLC
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/30—Oxygen atoms
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4406—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/15—Fumaric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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

Abstract

本发明涉及式(I)所示的恩替诺特与酸性对离子形成的化合物，与恩替诺特已知的固体形式相比，本发明的化合物在溶解度、稳定性等方面具有优势。本发明还涉及所述化合物的晶型及其制备方法，其药物组合物及其在制备用于预防和/或治疗与分化或增殖相关的疾病中的用途。
Figure DDA0002372862870000011

Description

PCT国内申请，说明书已公开。

Claims (19)

  1. PCT国内申请，权利要求书已公开。
CN201780092661.3A 2017-07-28 2017-07-28 含恩替诺特的化合物,其化合物晶型及其制备方法和药物组合物 Pending CN110944978A (zh)

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PCT/CN2017/094851 WO2019019130A1 (zh) 2017-07-28 2017-07-28 含恩替诺特的化合物，其化合物晶型及其制备方法和药物组合物

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11208382B2 (en) 2017-07-28 2021-12-28 Hangzhou Solipharma Co., Ltd. Entinostat-containing compound, crystal form of compound thereof, and preparation method therefor and pharmaceutical composition thereof
CA3218617A1 (en) 2021-05-10 2022-11-17 Thierry Bonnaud Novel forms of entinostat

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6174905B1 (en) * 1996-09-30 2001-01-16 Mitsui Chemicals, Inc. Cell differentiation inducer
JP2001131130A (ja) * 1999-11-09 2001-05-15 Mitsui Chemicals Inc モノアシルフェニレンジアミン誘導体の精製法
CN102137846A (zh) * 2008-08-29 2011-07-27 拜耳先灵医药股份有限公司 N-(2-氨基苯基)-4-[n-(吡啶-3-基)甲氧基羰基氨基甲基]苯甲酰胺(ms-275)多晶型物b

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3354090B2 (ja) * 1996-09-30 2002-12-09 シエーリング アクチエンゲゼルシャフト 分化誘導剤
AU2003292888A1 (en) * 2002-12-27 2004-07-22 Schering Aktiengesellschaft Pharmaceutical combinations of phthalazine vegf inhibitors and benzamide hdac inhibitors
US11208382B2 (en) 2017-07-28 2021-12-28 Hangzhou Solipharma Co., Ltd. Entinostat-containing compound, crystal form of compound thereof, and preparation method therefor and pharmaceutical composition thereof

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6174905B1 (en) * 1996-09-30 2001-01-16 Mitsui Chemicals, Inc. Cell differentiation inducer
JP2001131130A (ja) * 1999-11-09 2001-05-15 Mitsui Chemicals Inc モノアシルフェニレンジアミン誘導体の精製法
CN102137846A (zh) * 2008-08-29 2011-07-27 拜耳先灵医药股份有限公司 N-(2-氨基苯基)-4-[n-(吡啶-3-基)甲氧基羰基氨基甲基]苯甲酰胺(ms-275)多晶型物b

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WO2019019130A1 (zh) 2019-01-31
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Application publication date: 20200331