CN116113622A - 新的盐、晶体和共晶体 - Google Patents

新的盐、晶体和共晶体 Download PDF

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Publication number
CN116113622A
CN116113622A CN202180054461.5A CN202180054461A CN116113622A CN 116113622 A CN116113622 A CN 116113622A CN 202180054461 A CN202180054461 A CN 202180054461A CN 116113622 A CN116113622 A CN 116113622A
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CN
China
Prior art keywords
salt
crystal
meipai
free base
lumepirone
Prior art date
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Pending
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CN202180054461.5A
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English (en)
Chinese (zh)
Inventor
李鹏
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Intra Cellular Therapies Inc
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Intra Cellular Therapies Inc
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Publication date
Application filed by Intra Cellular Therapies Inc filed Critical Intra Cellular Therapies Inc
Publication of CN116113622A publication Critical patent/CN116113622A/zh
Pending legal-status Critical Current

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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)
CN202180054461.5A 2020-09-04 2021-09-03 新的盐、晶体和共晶体 Pending CN116113622A (zh)

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 (1)

Publication Number Publication Date
CN116113622A true CN116113622A (zh) 2023-05-12

Family

ID=80492079

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202180054461.5A Pending CN116113622A (zh) 2020-09-04 2021-09-03 新的盐、晶体和共晶体

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 (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017165843A1 (en) * 2016-03-25 2017-09-28 Intra-Cellular Therapies, Inc. Organic compounds
CN110636845A (zh) * 2017-04-10 2019-12-31 雷迪博士实验室有限公司 卢美哌隆对甲苯磺酸盐的无定形形式和固体分散体
WO2020047241A1 (en) * 2018-08-29 2020-03-05 Intra-Cellular Therapies, Inc. Novel compositions and methods
CN116327770A (zh) * 2017-03-24 2023-06-27 细胞内治疗公司 新组合物和方法

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11014925B2 (en) * 2016-03-28 2021-05-25 Intra-Cellular Therapies, Inc. Co-crystals of 1-(4-fluoro-phenyl)-4-((6bR,1OaS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H- pyrido[3′,4′:4,51_pyrrolo [1,2,3-delqcuinoxalin-8-yl)-butan-1-one with nicotinamide or isonicotinamide
CN111107847A (zh) * 2017-09-26 2020-05-05 细胞内治疗公司 新的盐和晶体
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
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 (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017165843A1 (en) * 2016-03-25 2017-09-28 Intra-Cellular Therapies, Inc. Organic compounds
CN116327770A (zh) * 2017-03-24 2023-06-27 细胞内治疗公司 新组合物和方法
CN110636845A (zh) * 2017-04-10 2019-12-31 雷迪博士实验室有限公司 卢美哌隆对甲苯磺酸盐的无定形形式和固体分散体
WO2020047241A1 (en) * 2018-08-29 2020-03-05 Intra-Cellular Therapies, Inc. Novel compositions and methods

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ANAËLLE TILBORG等: "Pharmaceu tical salts and cocrystals involving amino acids: A brief structural overview of the state-of- art", EUROPEAN JOURNAL OF MEDICI NAL CHEMISTRY, vol. 74, 31 December 2014 (2014-12-31), pages 411 - 426 *

Also Published As

Publication number Publication date
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
JP2023540506A (ja) 2023-09-25
CA3186537A1 (en) 2022-03-10
MX2023002468A (es) 2023-03-23
EP4208434A4 (en) 2024-10-16
US20230312573A1 (en) 2023-10-05

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