JP2023540506A - 新規の塩、結晶および共結晶 - Google Patents

新規の塩、結晶および共結晶 Download PDF

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Publication number
JP2023540506A
JP2023540506A JP2023514771A JP2023514771A JP2023540506A JP 2023540506 A JP2023540506 A JP 2023540506A JP 2023514771 A JP2023514771 A JP 2023514771A JP 2023514771 A JP2023514771 A JP 2023514771A JP 2023540506 A JP2023540506 A JP 2023540506A
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Japan
Prior art keywords
salt
crystal
lumateperone
free base
lysine
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JP2023514771A
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English (en)
Japanese (ja)
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JPWO2022051770A5 (https=
JP2023540506A5 (https=
Inventor
リ，ポン
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Intra Cellular Therapies Inc
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Intra Cellular Therapies Inc
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Publication of JP2023540506A publication Critical patent/JP2023540506A/ja
Publication of JPWO2022051770A5 publication Critical patent/JPWO2022051770A5/ja
Publication of JP2023540506A5 publication Critical patent/JP2023540506A5/ja
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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
    • C07D471/12—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 three hetero rings
    • C07D471/16—Peri-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
    • A61K31/495—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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B63/00—Purification; Separation; Stabilisation; Use of additives
    • C07B63/02—Purification; Separation; Stabilisation; Use of additives by treatment giving rise to a chemical modification
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/26—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one amino group bound to the carbon skeleton, e.g. lysine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
    • 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • 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
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (AREA)
JP2023514771A 2020-09-04 2021-09-03 新規の塩、結晶および共結晶 Pending JP2023540506A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063075019P 2020-09-04 2020-09-04
US63/075,019 2020-09-04
PCT/US2021/071366 WO2022051770A2 (en) 2020-09-04 2021-09-03 Novel salts, crystals, and co-crystals

Publications (3)

Publication Number Publication Date
JP2023540506A true JP2023540506A (ja) 2023-09-25
JPWO2022051770A5 JPWO2022051770A5 (https=) 2024-09-11
JP2023540506A5 JP2023540506A5 (https=) 2024-09-11

Family

ID=80492079

Family Applications (1)

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JP2023514771A Pending JP2023540506A (ja) 2020-09-04 2021-09-03 新規の塩、結晶および共結晶

Country Status (10)

Country Link
US (1) US20230312573A1 (https=)
EP (1) EP4208434A4 (https=)
JP (1) JP2023540506A (https=)
KR (1) KR20230104121A (https=)
CN (1) CN116113622A (https=)
AU (1) AU2021338439A1 (https=)
CA (1) CA3186537A1 (https=)
IL (1) IL300886A (https=)
MX (1) MX2023002468A (https=)
WO (1) WO2022051770A2 (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL268970B2 (en) 2017-03-24 2023-12-01 Intra Cellular Therapies Inc Oral transmucosal formulations of substituted heterocycle fused gamma carbolines
WO2019178484A1 (en) 2018-03-16 2019-09-19 Intra-Cellular Therapies, Inc. Novel methods
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
CN118566395B (zh) * 2024-08-02 2024-10-25 则正(济南)生物科技有限公司 测定甲苯磺酸卢美哌隆口崩片中杂质含量的方法、应用和系统

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019067591A1 (en) * 2017-09-26 2019-04-04 Intra-Cellular Therapies, Inc. NEW SALTS AND CRYSTALS
JP2019512525A (ja) * 2016-03-25 2019-05-16 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． 有機化合物
JP2019513140A (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． 新規共結晶

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
IL321985A (en) * 2018-06-06 2025-09-01 Intra Cellular Therapies Inc New salts and crystals
CA3106447A1 (en) * 2018-06-11 2019-12-19 Intra-Cellular Therapies, Inc. Substituted heterocycle fused gamma-carbolines synthesis
EP3843729A4 (en) * 2018-08-29 2022-06-01 Intra-Cellular Therapies, Inc. NOVEL COMPOSITIONS AND PROCESSES
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
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019512525A (ja) * 2016-03-25 2019-05-16 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． 有機化合物
JP2019513140A (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． 新規共結晶
WO2019067591A1 (en) * 2017-09-26 2019-04-04 Intra-Cellular Therapies, Inc. NEW SALTS AND CRYSTALS

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
平山令明, 有機化合物結晶作製ハンドブック, JPN6014035600, 2008, pages 17 - 23, ISSN: 0005743765 *
芦澤一英, 医薬品の多形現象と晶析の化学, JPN6015027444, 2002, pages 273 - 278, ISSN: 0005743764 *

Also Published As

Publication number Publication date
CN116113622A (zh) 2023-05-12
KR20230104121A (ko) 2023-07-07
WO2022051770A2 (en) 2022-03-10
IL300886A (en) 2023-04-01
WO2022051770A3 (en) 2022-04-14
AU2021338439A1 (en) 2023-02-23
EP4208434A2 (en) 2023-07-12
CA3186537A1 (en) 2022-03-10
MX2023002468A (es) 2023-03-23
EP4208434A4 (en) 2024-10-16
US20230312573A1 (en) 2023-10-05

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