CA3186537A1 - Novel salts, crystals, and co-crystals - Google Patents

Novel salts, crystals, and co-crystals

Info

Publication number
CA3186537A1
CA3186537A1 CA3186537A CA3186537A CA3186537A1 CA 3186537 A1 CA3186537 A1 CA 3186537A1 CA 3186537 A CA3186537 A CA 3186537A CA 3186537 A CA3186537 A CA 3186537A CA 3186537 A1 CA3186537 A1 CA 3186537A1
Authority
CA
Canada
Prior art keywords
salt
crystal
lumateperone
free base
tosylate
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CA3186537A
Other languages
English (en)
French (fr)
Inventor
Peng Li
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Intra Cellular Therapies Inc
Original Assignee
Intra Cellular Therapies Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Intra Cellular Therapies Inc filed Critical Intra Cellular Therapies Inc
Publication of CA3186537A1 publication Critical patent/CA3186537A1/en
Pending legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B63/00Purification; Separation; Stabilisation; Use of additives
    • C07B63/02Purification; Separation; Stabilisation; Use of additives by treatment giving rise to a chemical modification
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02Compounds 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
    • C07C229/04Compounds 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
    • C07C229/26Compounds 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/28Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30Sulfonic 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
    • 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
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled
    • 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

Landscapes

  • 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)
CA3186537A 2020-09-04 2021-09-03 Novel salts, crystals, and co-crystals Pending CA3186537A1 (en)

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
CA3186537A1 true CA3186537A1 (en) 2022-03-10

Family

ID=80492079

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3186537A Pending CA3186537A1 (en) 2020-09-04 2021-09-03 Novel salts, crystals, and co-crystals

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

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL3407889T3 (pl) * 2016-03-25 2021-11-22 Intra-Cellular Therapies, Inc. Związki organiczne i ich zastosowanie w leczeniu lub zapobieganiu zaburzeniom ośrodkowego układu nerwowego
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
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
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
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

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
JP2023540506A (ja) 2023-09-25
MX2023002468A (es) 2023-03-23
EP4208434A4 (en) 2024-10-16
US20230312573A1 (en) 2023-10-05

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