JP6997718B2 - 新規共結晶 - Google Patents

新規共結晶 Download PDF

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JP6997718B2
JP6997718B2 JP2018550675A JP2018550675A JP6997718B2 JP 6997718 B2 JP6997718 B2 JP 6997718B2 JP 2018550675 A JP2018550675 A JP 2018550675A JP 2018550675 A JP2018550675 A JP 2018550675A JP 6997718 B2 JP6997718 B2 JP 6997718B2
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crystal
iti
free base
isonicotinamide
nicotinamide
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JP2019513140A5 (https=
JP2019513140A (ja
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ペン・リ
エドウィン・アレット
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Intra Cellular Therapies Inc
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Intra Cellular Therapies Inc
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/16Peri-condensed systems
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • C07D213/82Amides; Imides in position 3
    • 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
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A61K9/0024Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
JP2018550675A 2016-03-28 2017-03-28 新規共結晶 Active JP6997718B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662314339P 2016-03-28 2016-03-28
US62/314,339 2016-03-28
PCT/US2017/024597 WO2017172811A1 (en) 2016-03-28 2017-03-28 Novel co-crystals

Publications (3)

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JP2019513140A JP2019513140A (ja) 2019-05-23
JP2019513140A5 JP2019513140A5 (https=) 2020-04-30
JP6997718B2 true JP6997718B2 (ja) 2022-01-18

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JP2018550675A Active JP6997718B2 (ja) 2016-03-28 2017-03-28 新規共結晶

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US (1) US11014925B2 (https=)
EP (1) EP3436016B1 (https=)
JP (1) JP6997718B2 (https=)
WO (1) WO2017172811A1 (https=)

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CN105168219B (zh) * 2008-05-27 2018-11-20 细胞内治疗公司 用于睡眠障碍和其他疾病的方法和组合物
WO2013155504A1 (en) 2012-04-14 2013-10-17 Intra-Cellular Therapies, Inc. Novel methods
IL305990B2 (en) * 2013-12-03 2025-12-01 Intra Cellular Therapies Inc Long-acting injectable composition comprising polymeric microspheres of heterocycle fused gamma-carboline compounds or a pharmaceutical composition for sustained or delayed release comprising the compounds and their use in the treatment of bipolar disorder i and/or bipolar ii disorder
CN108883111B (zh) 2016-01-26 2021-10-08 细胞内治疗公司 有机化合物
JP2019513143A (ja) * 2016-03-28 2019-05-23 イントラ−セルラー・セラピーズ・インコーポレイテッドIntra−Cellular Therapies, Inc. 新規塩類および結晶
EP4001281A1 (en) 2016-08-09 2022-05-25 Teva Pharmaceuticals International GmbH Solid state forms of lumateperone ditosylate salt and preparation thereof
US11331316B2 (en) 2016-10-12 2022-05-17 Intra-Cellular Therapies, Inc. Amorphous solid dispersions
IL268970B2 (en) 2017-03-24 2023-12-01 Intra Cellular Therapies Inc Oral transmucosal formulations of substituted heterocycle fused gamma carbolines
JP2020513023A (ja) 2017-04-10 2020-04-30 ドクター・レディーズ・ラボラトリーズ・リミテッド ルマテペロンp−トシラートの非晶質形態および固体分散体
JP7224333B2 (ja) 2017-07-26 2023-02-17 イントラ-セルラー・セラピーズ・インコーポレイテッド 有機化合物
CN111107847A (zh) 2017-09-26 2020-05-05 细胞内治疗公司 新的盐和晶体
AU2019240226B2 (en) 2018-03-23 2024-11-28 Intra-Cellular Therapies, Inc. Organic compounds
IL321985A (en) 2018-06-06 2025-09-01 Intra Cellular Therapies Inc New salts and crystals
WO2019237037A1 (en) 2018-06-08 2019-12-12 Intra-Cellular Therapies, Inc. Novel methods
CA3108558A1 (en) * 2018-08-31 2020-03-05 Intra-Cellular Therapies, Inc. Novel methods
CN112584837A (zh) 2018-08-31 2021-03-30 细胞内治疗公司 新方法
US20220024924A1 (en) 2018-11-27 2022-01-27 Teva Czech Industries S.R.O Solid state forms of lumateperone salts and processes for preparation of lumateperone and salts thereof
IL283963B2 (en) 2018-12-17 2025-01-01 Intra Cellular Therapies Inc Synthesis of condensed gamma-carbolines and converted heterocycles
BR112021011792A2 (pt) 2018-12-17 2021-08-31 Intra-Cellular Therapies, Inc. Composto orgânico
US12195463B2 (en) 2018-12-21 2025-01-14 Intra-Cellular Therapies, Inc. Organic compounds
WO2020132605A1 (en) 2018-12-21 2020-06-25 Intra-Cellular Therapies, Inc. Organic compounds
JP7673040B2 (ja) 2019-07-07 2025-05-08 イントラ-セルラー・セラピーズ・インコーポレイテッド 新規方法
EP4034119A4 (en) 2019-09-25 2023-10-18 Intra-Cellular Therapies, Inc. NOVEL METHODS
EP4072554A4 (en) 2019-12-11 2023-12-20 Intra-Cellular Therapies, Inc. ORGANIC CONNECTION
WO2022051770A2 (en) * 2020-09-04 2022-03-10 Intra-Cellular Therapies, Inc. Novel salts, crystals, and co-crystals
IL308750A (en) * 2021-06-07 2024-01-01 Intra Cellular Therapies Inc Novel salts and crystals
US12414948B2 (en) 2022-05-18 2025-09-16 Intra-Cellular Therapies, Inc. Methods
WO2025240804A1 (en) 2024-05-16 2025-11-20 Intra-Cellular Therapies, Inc. Novel compositions, devices and methods

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