JP5567349B2 - 置換ヘテロ環縮合ガンマ−カルボリンの合成 - Google Patents

置換ヘテロ環縮合ガンマ−カルボリンの合成 Download PDF

Info

Publication number
JP5567349B2
JP5567349B2 JP2009553626A JP2009553626A JP5567349B2 JP 5567349 B2 JP5567349 B2 JP 5567349B2 JP 2009553626 A JP2009553626 A JP 2009553626A JP 2009553626 A JP2009553626 A JP 2009553626A JP 5567349 B2 JP5567349 B2 JP 5567349B2
Authority
JP
Japan
Prior art keywords
formula
compound
alkyl
acid
iii
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.)
Active
Application number
JP2009553626A
Other languages
English (en)
Japanese (ja)
Other versions
JP2010521464A5 (OSRAM
JP2010521464A (ja
Inventor
ジョン・チャールズ・トメッシュ
リ・ペン
ヤオ・ウェイ
ジャン・キアン
ジェイムズ・デイビッド・ビアード
アンドリュー・エス・トンプソン
チェン・フア
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39759858&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=JP5567349(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Intra Cellular Therapies Inc filed Critical Intra Cellular Therapies Inc
Publication of JP2010521464A publication Critical patent/JP2010521464A/ja
Publication of JP2010521464A5 publication Critical patent/JP2010521464A5/ja
Application granted granted Critical
Publication of JP5567349B2 publication Critical patent/JP5567349B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/26Psychostimulants, e.g. nicotine, cocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • 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
    • 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
    • C07D471/02Heterocyclic 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 two hetero rings
    • 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
    • C07D471/02Heterocyclic 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 two hetero rings
    • C07D471/04Ortho-condensed systems
    • 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
    • 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
    • C07D471/14Ortho-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Anesthesiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Hematology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Catalysts (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2009553626A 2007-03-12 2008-03-12 置換ヘテロ環縮合ガンマ−カルボリンの合成 Active JP5567349B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US90647307P 2007-03-12 2007-03-12
US60/906,473 2007-03-12
PCT/US2008/003340 WO2008112280A1 (en) 2007-03-12 2008-03-12 Substituted heterocycle fused gamma-carbolines synthesis

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2014126495A Division JP5918306B2 (ja) 2007-03-12 2014-06-19 置換ヘテロ環縮合ガンマ−カルボリンの合成

Publications (3)

Publication Number Publication Date
JP2010521464A JP2010521464A (ja) 2010-06-24
JP2010521464A5 JP2010521464A5 (OSRAM) 2011-05-06
JP5567349B2 true JP5567349B2 (ja) 2014-08-06

Family

ID=39759858

Family Applications (7)

Application Number Title Priority Date Filing Date
JP2009553626A Active JP5567349B2 (ja) 2007-03-12 2008-03-12 置換ヘテロ環縮合ガンマ−カルボリンの合成
JP2014126495A Active JP5918306B2 (ja) 2007-03-12 2014-06-19 置換ヘテロ環縮合ガンマ−カルボリンの合成
JP2016077538A Active JP6231151B2 (ja) 2007-03-12 2016-04-07 置換ヘテロ環縮合ガンマ−カルボリンの合成
JP2017201937A Active JP6522710B2 (ja) 2007-03-12 2017-10-18 置換ヘテロ環縮合ガンマ−カルボリンの合成
JP2019082541A Active JP6773837B2 (ja) 2007-03-12 2019-04-24 置換ヘテロ環縮合ガンマ−カルボリンの合成
JP2020166874A Withdrawn JP2021006559A (ja) 2007-03-12 2020-10-01 置換ヘテロ環縮合ガンマ−カルボリンの合成
JP2022144080A Pending JP2022180440A (ja) 2007-03-12 2022-09-09 置換ヘテロ環縮合ガンマ-カルボリンの合成

Family Applications After (6)

Application Number Title Priority Date Filing Date
JP2014126495A Active JP5918306B2 (ja) 2007-03-12 2014-06-19 置換ヘテロ環縮合ガンマ−カルボリンの合成
JP2016077538A Active JP6231151B2 (ja) 2007-03-12 2016-04-07 置換ヘテロ環縮合ガンマ−カルボリンの合成
JP2017201937A Active JP6522710B2 (ja) 2007-03-12 2017-10-18 置換ヘテロ環縮合ガンマ−カルボリンの合成
JP2019082541A Active JP6773837B2 (ja) 2007-03-12 2019-04-24 置換ヘテロ環縮合ガンマ−カルボリンの合成
JP2020166874A Withdrawn JP2021006559A (ja) 2007-03-12 2020-10-01 置換ヘテロ環縮合ガンマ−カルボリンの合成
JP2022144080A Pending JP2022180440A (ja) 2007-03-12 2022-09-09 置換ヘテロ環縮合ガンマ-カルボリンの合成

Country Status (12)

Country Link
US (11) US8309722B2 (OSRAM)
EP (2) EP3663294A1 (OSRAM)
JP (7) JP5567349B2 (OSRAM)
KR (7) KR102372149B1 (OSRAM)
CN (2) CN103626766B (OSRAM)
AU (5) AU2008226814C1 (OSRAM)
CA (1) CA2679754C (OSRAM)
DK (1) DK2134710T3 (OSRAM)
ES (1) ES2776889T3 (OSRAM)
IN (1) IN2009DN05670A (OSRAM)
MX (3) MX2009009773A (OSRAM)
WO (1) WO2008112280A1 (OSRAM)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016155849A (ja) * 2007-03-12 2016-09-01 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. 置換ヘテロ環縮合ガンマ−カルボリンの合成

Families Citing this family (77)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2523580T3 (es) 2008-01-11 2014-11-27 Albany Molecular Research, Inc. Piridoindoles substituidos con (1-Azinona)
PL2262505T3 (pl) 2008-03-12 2015-04-30 Intra Cellular Therapies Inc Podstawione heterocykliczne skondensowane gamma-karboliny w postaci stałej
US8598119B2 (en) 2008-05-27 2013-12-03 Intra-Cellular Therapies, Inc. Methods and compositions for sleep disorders and other disorders
US9107696B2 (en) * 2008-08-06 2015-08-18 Emory University Method of embryo transfer that eliminates transferred air while hormonally inducing implantation and apparatus
US9625475B2 (en) 2008-09-29 2017-04-18 Abbvie Inc. Indole and indoline derivatives and methods of use thereof
US9063126B2 (en) 2008-09-29 2015-06-23 Abbvie Inc. Indole and indoline derivatives and methods of use thereof
JP2012532144A (ja) 2009-07-01 2012-12-13 アルバニー モレキュラー リサーチ, インコーポレイテッド アジノン置換アゼピノ[b]インドールおよびピリド−ピロロ−アゼピンmch−1拮抗薬、ならびにその作製方法および使用
US8618299B2 (en) 2009-07-01 2013-12-31 Albany Molecular Research, Inc. Azinone-substituted azapolycycle MCH-1 antagonists, methods of making, and use thereof
US9073925B2 (en) 2009-07-01 2015-07-07 Albany Molecular Research, Inc. Azinone-substituted azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine MCH-1 antagonists, methods of making, and use thereof
WO2011003007A1 (en) 2009-07-01 2011-01-06 Albany Molecular Research, Inc. Azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine mch-1 antagonists, methods of making, and use thereof
US8993572B2 (en) 2010-04-22 2015-03-31 Intra-Cellular Therapies, Inc. Pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalines derivatives and [1,4]oxazino[2,3,4-hi]pyrido[4,3-b]indole derivatives
US8697700B2 (en) 2010-12-21 2014-04-15 Albany Molecular Research, Inc. Piperazinone-substituted tetrahydro-carboline MCH-1 antagonists, methods of making, and uses thereof
US8993765B2 (en) 2010-12-21 2015-03-31 Albany Molecular Research, Inc. Tetrahydro-azacarboline MCH-1 antagonists, methods of making, and uses thereof
WO2013155504A1 (en) * 2012-04-14 2013-10-17 Intra-Cellular Therapies, Inc. Novel methods
WO2014145192A1 (en) 2013-03-15 2014-09-18 Intra-Cellular Therapies, Inc. Organic compounds
IL321987A (en) 2013-12-03 2025-09-01 Intra Cellular Therapies Inc A long-acting injectable preparation containing polymeric microspheres of modified compressed gamma-carboline heterocyclic compounds or a sustained-release pharmaceutical preparation containing these compounds for use in the treatment of bipolar I and/or bipolar II disorders
MX388258B (es) 2014-04-04 2025-03-19 Intra Cellular Therapies Inc Gamma-carbolinas fusionadas con heterociclos sustituidas con deuterio.
AU2015240526A1 (en) 2014-04-04 2016-11-24 Intra-Cellular Therapies, Inc. Organic compounds
US10179776B2 (en) 2014-06-09 2019-01-15 Intra-Cellular Therapies, Inc. Compounds and methods of use to treat schizophrenia
US10118890B2 (en) 2014-10-10 2018-11-06 The Research Foundation For The State University Of New York Trifluoromethoxylation of arenes via intramolecular trifluoromethoxy group migration
CN107922334B (zh) * 2015-04-30 2021-11-23 科罗拉多大学董事会 多环吲哚啉和假吲哚化合物
PT3407888T (pt) 2016-01-26 2021-03-19 Intra Cellular Therapies Inc Compostos de piridopirroloquinoxalina, suas composições e utilizações
JP6686168B2 (ja) 2016-03-25 2020-04-22 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
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
JP2019510039A (ja) 2016-03-28 2019-04-11 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. 新規組成物および方法
JP6997718B2 (ja) * 2016-03-28 2022-01-18 イントラ-セルラー・セラピーズ・インコーポレイテッド 新規共結晶
SI3497104T1 (sl) 2016-08-09 2021-12-31 Teva Pharmaceuticals International Gmbh Trdne oblike soli lumateperon ditosilata
US12343337B2 (en) 2016-09-29 2025-07-01 The Regents Of The University Of California Compounds for increasing neural plasticity
EP3525763B1 (en) 2016-10-12 2025-03-05 Intra-Cellular Therapies, Inc. Amorphous solid dispersions
US10906906B2 (en) 2016-12-29 2021-02-02 Intra-Cellular Therapies, Inc. Organic compounds
WO2018126140A1 (en) 2016-12-29 2018-07-05 Intra-Cellular Therapies, Inc. Organic compounds
CN116327770B (zh) 2017-03-24 2025-10-31 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
BR112020001666A2 (pt) 2017-07-26 2020-07-21 Intra-Cellular Therapies, Inc. compostos orgânicos
IL272252B2 (en) 2017-07-26 2024-03-01 Intra Cellular Therapies Inc Derivatives of substituted heterocycle fused gamma-carbolines, pharmaceutical compositions comnprising them and their use in treatment
JP2020535231A (ja) 2017-09-26 2020-12-03 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. 新規な塩および結晶
WO2019102240A1 (en) * 2017-11-27 2019-05-31 Egis Gyógyszergyár Zrt. Method for the manufacture of lumateperone and its salts
CA3094204A1 (en) 2018-03-16 2019-09-19 Intra-Cellular Therapies, Inc. Novel methods
MX2020009928A (es) 2018-03-23 2021-01-08 Intra Cellular Therapies Inc Compuestos organicos.
CA3095101A1 (en) 2018-03-23 2019-09-26 Intra-Cellular Therapies, Inc. Deuterated octahydro-quinoxaline derivatives and pharmaceutical compositions thereof use in the treatment of diseases involving serotonin 5-ht2a, dopamine d1/d2 and/or serotonin reuptake transporter (sert) pathways
KR102888393B1 (ko) 2018-06-06 2025-11-18 인트라-셀룰라 써래피스, 인코퍼레이티드. 신규한 염 및 결정
MX2020013335A (es) 2018-06-08 2021-05-27 Intra Cellular Therapies Inc Metodos novedosos.
KR102778034B1 (ko) 2018-06-11 2025-03-12 인트라-셀룰라 써래피스, 인코퍼레이티드. 치환된 헤테로환 융합 감마-카르볼린 합성
AU2019288476A1 (en) 2018-06-21 2021-03-18 Aquestive Therapeutics, Inc. System and method for making personalized individual unit doses containing pharmaceutical actives
EP4474017A3 (en) 2018-08-13 2025-02-26 F. Hoffmann-La Roche AG New heterocyclic compounds
EP3843729A4 (en) 2018-08-29 2022-06-01 Intra-Cellular Therapies, Inc. NEW COMPOSITIONS AND METHODS
US10695345B2 (en) 2018-08-31 2020-06-30 Intra-Cellular Therapies, Inc. Pharmaceutical capsule compositions comprising lumateperone mono-tosylate
EP3843738A4 (en) 2018-08-31 2022-06-01 Intra-Cellular Therapies, Inc. NEW METHODS
BR112021004053A2 (pt) 2018-09-07 2021-05-25 Aquestive Therapeutics, Inc. composições de filme oral e formas de dosagem tendo perfis de dissolução de ativo precisos
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
CA3121635A1 (en) 2018-12-17 2020-06-25 Intra-Cellular Therapies, Inc. Serotonin 5-ht2a receptor antagonist
WO2020131895A1 (en) 2018-12-17 2020-06-25 Intra-Cellular Therapies, Inc. Substituted heterocycle fused gamma-carbolines synthesis
MX2021007143A (es) 2018-12-17 2021-08-18 Intra Cellular Therapies Inc Sintesis de gamma-carbolinas fusionadas con heterociclo sustituido.
US12331052B2 (en) 2018-12-21 2025-06-17 Intra-Cellular Therapies, Inc. Organic compounds
WO2020132474A1 (en) 2018-12-21 2020-06-25 Intra-Cellular Therapies, Inc. Organic compound
EP3931189B1 (en) 2019-02-27 2025-12-24 The Regents Of The University Of California Azepino-indoles and other heterocycles for treating brain disorders
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
WO2021062307A1 (en) 2019-09-25 2021-04-01 Intra-Cellular Therapies, Inc. Novel methods
AU2020373100A1 (en) 2019-11-01 2022-05-19 Aquestive Therapeutics, Inc. Prodrug compositions and methods of treatment
CN110698474B (zh) * 2019-11-14 2021-11-02 福州大学 一种α位取代四氢-γ-咔啉类化合物及其制备方法和应用
CA3159389A1 (en) 2019-11-14 2021-05-20 Aquestive Therapeutics, Inc. Multimodal compositions comprising diazepam and methods of treatment
WO2021119334A1 (en) * 2019-12-11 2021-06-17 Intra-Cellular Therapies, Inc. Organic compound
JP7727634B2 (ja) 2019-12-19 2025-08-21 イントラ-セルラー・セラピーズ・インコーポレイテッド 統合失調症処置方法
CN112062767B (zh) * 2020-10-20 2022-03-11 杭州科巢生物科技有限公司 一种卢美哌隆的制备方法及其中间体
CA3208345A1 (en) 2021-01-15 2022-07-21 Aquestive Therapeutics, Inc. Prodrug compositions and methods of treatment
WO2022192476A1 (en) 2021-03-09 2022-09-15 Aquestive Therapeutics, Inc. Dosage forms having equivalent biocomparable profiles
CN113024554B (zh) * 2021-03-24 2023-03-14 上海法默生物科技有限公司 一种卢美哌隆中间体的制备方法
CN114105980B (zh) * 2021-12-13 2024-04-16 南方科技大学坪山生物医药研究院 卢美哌隆中间体化合物的制备方法及卢美哌隆中间体化合物
CN114105985B (zh) * 2021-12-13 2024-04-16 南方科技大学坪山生物医药研究院 不对称氢化构建卢美哌隆中间体的方法及卢美哌隆中间体
WO2023114313A1 (en) 2021-12-15 2023-06-22 Delix Therapeutics, Inc. Phenoxy and benzyloxy substituted psychoplastogens and uses thereof
US12414948B2 (en) 2022-05-18 2025-09-16 Intra-Cellular Therapies, Inc. Methods
CA3274836A1 (en) 2022-12-30 2024-07-04 Intra-Cellular Therapies, Inc. Fused heterocyclic gamma-carbolines acting on the 5-HT2A serotonin receptor
WO2024173901A1 (en) 2023-02-17 2024-08-22 Intra-Cellular Therapies, Inc. Lumateperone and derivatives thereof for modulating the nervous system
WO2025223504A1 (zh) * 2024-04-26 2025-10-30 浙江奥翔药业股份有限公司 卢美哌隆中间体及其制备方法
WO2025240804A1 (en) 2024-05-16 2025-11-20 Intra-Cellular Therapies, Inc. Novel compositions, devices and methods
WO2025257090A1 (en) 2024-06-10 2025-12-18 Interquim, S.A. Process for the preparation of synthesis intermediates of lumateperone and lumateperone analogues
CN119912455B (zh) * 2025-01-22 2025-09-23 成都臻拓医药科技有限公司 一种卢美哌隆中间体化合物的制备方法

Family Cites Families (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US39680A (en) 1863-08-25 Improvement in machines for breaking and cleaning flax
US6713A (en) 1849-09-11 Hobse-poweb
US471A (en) 1837-11-20 Mode of
US38679A (en) 1863-05-26 Improvement in water-elevators
US2490813A (en) 1944-11-29 1949-12-13 Standard Oil Co Continuous process for making aryl amines
US3299078A (en) 1962-10-01 1967-01-17 Smith Kline French Lab Pyrido [3', 4': 4, 5] pyrrolo [3, 2, 1-hi] indoles and-[3, 2, 1-ij] quinolines
US3813392A (en) 1969-06-09 1974-05-28 J Sellstedt Pyrrolo(1,2,3-alpha epsilon)quinoxalin-2(3h)-ones and related compounds
US4238607A (en) 1972-06-19 1980-12-09 Endo Laboratories Inc. Pyridopyrrolo benzheterocycles
US3914421A (en) 1972-06-19 1975-10-21 Endo Lab Pyridopyrrolobenzheterocycles for combatting depression
US4115577A (en) 1972-06-19 1978-09-19 Endo Laboratories, Inc. Pyridopyrrolobenzheterocycles
US4183936A (en) 1972-06-19 1980-01-15 Endo Laboratories, Inc. Pyridopyrrolobenzheterocycles
US4219550A (en) 1978-11-09 1980-08-26 E. I. Du Pont De Nemours And Company Cis- and trans- octahydropyridopyrrolobenzheterocycles
US4522944A (en) 1982-12-23 1985-06-11 Erba Farmitalia Carboxamido-derivatives of 5H-1,3,4-thiadiazolo[3,2-a]pyrimidines, compositions and use
ES2058068T3 (es) 1986-03-19 1994-11-01 Kumiai Chemical Industry Co Derivados de 5h-1,3,4-tiadiazol-(3,2-a)-pirimidin-5-ona y compuestos fungicidas con contenido en dichos derivados.
JP2641443B2 (ja) 1986-04-07 1997-08-13 クミアイ化学工業株式会社 5H−1,3,4−チアジアゾロ〔3,2−a〕ピリミジン−5−オン誘導体及びこれを有効成分とする農園芸用殺菌剤
US5576460A (en) 1994-07-27 1996-11-19 Massachusetts Institute Of Technology Preparation of arylamines
US5648542A (en) 1996-02-29 1997-07-15 Xerox Corporation Arylamine processes
US5648539A (en) 1996-02-29 1997-07-15 Xerox Corporation Low temperature arylamine processes
US5654482A (en) 1996-02-29 1997-08-05 Xerox Corporation Triarylamine processes
US5847166A (en) 1996-10-10 1998-12-08 Massachusetts Institute Of Technology Synthesis of aryl ethers
US5705697A (en) 1997-01-30 1998-01-06 Xerox Corporation Arylamine processes
US5723669A (en) 1997-01-30 1998-03-03 Xerox Corporation Arylamine processes
US5723671A (en) 1997-01-30 1998-03-03 Xerox Corporation Arylamine processes
US6323366B1 (en) 1997-07-29 2001-11-27 Massachusetts Institute Of Technology Arylamine synthesis
GB2328686B (en) 1997-08-25 2001-09-26 Sankio Chemical Co Ltd Method for producing arylamine
WO1999018057A1 (en) 1997-10-06 1999-04-15 Massachusetts Institute Of Technology Preparation of diaryl ether by condensation reactions
US6235936B1 (en) 1998-02-26 2001-05-22 Massachusetts Institute Of Technology Metal-catalyzed arylations of hydrazines, hydrazones, and related substrates
CA2322194C (en) 1998-02-26 2011-04-26 Massachusetts Institute Of Technology Metal-catalyzed arylations and vinylations of hydrazines, hydrazones, hydroxylamines and oximes
US5902901A (en) 1998-05-07 1999-05-11 Xerox Corporation Arylamine processes
ATE360634T1 (de) 1998-07-10 2007-05-15 Massachusetts Inst Technology Ligande für metalle und verbesserte metall- katalysierte verfahren, die darauf basieren
US6395916B1 (en) 1998-07-10 2002-05-28 Massachusetts Institute Of Technology Ligands for metals and improved metal-catalyzed processes based thereon
US7223879B2 (en) 1998-07-10 2007-05-29 Massachusetts Institute Of Technology Ligands for metals and improved metal-catalyzed processes based thereon
US6307087B1 (en) 1998-07-10 2001-10-23 Massachusetts Institute Of Technology Ligands for metals and improved metal-catalyzed processes based thereon
US20010008942A1 (en) 1998-12-08 2001-07-19 Buchwald Stephen L. Synthesis of aryl ethers
PE20010052A1 (es) 1999-04-23 2001-01-27 Upjohn Co Compuestos de azepinindol tetraciclico como agonistas o antagonistas del receptor de 5-ht
US6407092B1 (en) 1999-04-23 2002-06-18 Pharmacia & Upjohn Company Tetracyclic azepinoindole compounds
AR024378A1 (es) 1999-06-15 2002-10-02 Du Pont Pharm Co Gamma-carbolinas fusionadas heterociclicas sustituidas
US6713471B1 (en) 1999-06-15 2004-03-30 Bristol-Myers Squibb Pharma Company Substituted heterocycle fused gamma-carbolines
US7071186B2 (en) 1999-06-15 2006-07-04 Bristol-Myers Squibb Pharma Co. Substituted heterocycle fused gamma-carbolines
US6541639B2 (en) 2000-07-26 2003-04-01 Bristol-Myers Squibb Pharma Company Efficient ligand-mediated Ullmann coupling of anilines and azoles
US6849619B2 (en) 2000-12-20 2005-02-01 Bristol-Myers Squibb Company Substituted pyridoindoles as serotonin agonists and antagonists
SK7042003A3 (en) 2000-12-20 2004-07-07 Bristol Myers Squibb Co Substituted pyridoindoles as serotonin agonists and antagonists
CA2445159C (en) 2001-04-24 2012-09-11 Massachusetts Institute Of Technology Copper-catalyzed formation of carbon-heteroatom and carbon-carbon bonds
CA2453537A1 (en) * 2001-08-08 2003-02-20 Pharmacia & Upjohn Company Therapeutic 1h-pyrido¬4,3-b|indoles
KR20050032107A (ko) 2002-08-02 2005-04-06 메사추세츠 인스티튜트 오브 테크놀로지 구리를 촉매로 한 탄소-헤테로원자 결합 및 탄소-탄소결합 형성방법
US7223870B2 (en) 2002-11-01 2007-05-29 Pfizer Inc. Methods for preparing N-arylated oxazolidinones via a copper catalyzed cross coupling reaction
EP1581221B1 (en) * 2002-12-19 2011-05-18 Bristol-Myers Squibb Company Substituted tricyclic gamma-carbolines as serotonin receptor agonists and antagonists
JP2005259113A (ja) 2004-02-12 2005-09-22 Ricoh Co Ltd プロセス編集装置、プロセス管理装置、プロセス編集プログラム、プロセス管理プログラム、記録媒体、プロセス編集方法及びプロセス管理方法
US7592454B2 (en) * 2004-04-14 2009-09-22 Bristol-Myers Squibb Company Substituted hexahydro-pyridoindole derivatives as serotonin receptor agonists and antagonists
ES2338139T3 (es) * 2004-12-15 2010-05-04 F. Hoffmann-La Roche Ag Fenil-metanonas bi- y triciclicas sustituidas como inhibidores del transportador de la glicina i (glyt-1) para el tratamiento de la enfermedad de alzheimer.
KR102372149B1 (ko) * 2007-03-12 2022-03-07 인트라-셀룰라 써래피스, 인코퍼레이티드. 치환된 헤테로환 융합 감마-카르볼린 합성
PL2262505T3 (pl) 2008-03-12 2015-04-30 Intra Cellular Therapies Inc Podstawione heterocykliczne skondensowane gamma-karboliny w postaci stałej
US8598119B2 (en) 2008-05-27 2013-12-03 Intra-Cellular Therapies, Inc. Methods and compositions for sleep disorders and other disorders
US8309772B2 (en) 2008-07-31 2012-11-13 Celanese International Corporation Tunable catalyst gas phase hydrogenation of carboxylic acids
US8993572B2 (en) * 2010-04-22 2015-03-31 Intra-Cellular Therapies, Inc. Pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalines derivatives and [1,4]oxazino[2,3,4-hi]pyrido[4,3-b]indole derivatives
WO2013155504A1 (en) 2012-04-14 2013-10-17 Intra-Cellular Therapies, Inc. Novel methods
WO2014145192A1 (en) 2013-03-15 2014-09-18 Intra-Cellular Therapies, Inc. Organic compounds
IL321987A (en) 2013-12-03 2025-09-01 Intra Cellular Therapies Inc A long-acting injectable preparation containing polymeric microspheres of modified compressed gamma-carboline heterocyclic compounds or a sustained-release pharmaceutical preparation containing these compounds for use in the treatment of bipolar I and/or bipolar II disorders
MX388258B (es) 2014-04-04 2025-03-19 Intra Cellular Therapies Inc Gamma-carbolinas fusionadas con heterociclos sustituidas con deuterio.
JP6686168B2 (ja) 2016-03-25 2020-04-22 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
WO2019102240A1 (en) 2017-11-27 2019-05-31 Egis Gyógyszergyár Zrt. Method for the manufacture of lumateperone and its salts

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016155849A (ja) * 2007-03-12 2016-09-01 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. 置換ヘテロ環縮合ガンマ−カルボリンの合成
JP2018035189A (ja) * 2007-03-12 2018-03-08 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. 置換ヘテロ環縮合ガンマ−カルボリンの合成
JP2019147819A (ja) * 2007-03-12 2019-09-05 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. 置換ヘテロ環縮合ガンマ−カルボリンの合成

Also Published As

Publication number Publication date
KR20100014428A (ko) 2010-02-10
AU2019229334A1 (en) 2019-10-03
MX2009009773A (es) 2009-12-16
IN2009DN05670A (OSRAM) 2015-07-24
KR20150140397A (ko) 2015-12-15
KR102065319B1 (ko) 2020-01-10
AU2008226814C1 (en) 2014-11-20
US20200087305A1 (en) 2020-03-19
MX2022008904A (es) 2022-08-16
US20160194326A1 (en) 2016-07-07
US20140364609A1 (en) 2014-12-11
AU2016234905A1 (en) 2016-10-20
KR20180074802A (ko) 2018-07-03
WO2008112280A1 (en) 2008-09-18
US9315504B2 (en) 2016-04-19
US8779139B2 (en) 2014-07-15
US12139490B2 (en) 2024-11-12
KR20190053975A (ko) 2019-05-20
ES2776889T3 (es) 2020-08-03
JP5918306B2 (ja) 2016-05-18
US20180044337A1 (en) 2018-02-15
US9751883B2 (en) 2017-09-05
EP2134710B1 (en) 2020-02-12
JP2016155849A (ja) 2016-09-01
CN101796051A (zh) 2010-08-04
US20100113781A1 (en) 2010-05-06
KR102107954B1 (ko) 2020-05-07
KR20200047755A (ko) 2020-05-07
US10597395B2 (en) 2020-03-24
EP2134710A1 (en) 2009-12-23
JP2019147819A (ja) 2019-09-05
AU2014203483A1 (en) 2014-07-17
US20130046097A1 (en) 2013-02-21
AU2014203483B2 (en) 2016-06-30
US20220332716A1 (en) 2022-10-20
KR101805914B1 (ko) 2017-12-06
JP6773837B2 (ja) 2020-10-21
US8309722B2 (en) 2012-11-13
CN103626766A (zh) 2014-03-12
AU2018201818A1 (en) 2018-04-05
US20250101022A1 (en) 2025-03-27
JP6231151B2 (ja) 2017-11-15
AU2008226814B2 (en) 2014-03-27
JP2022180440A (ja) 2022-12-06
JP2018035189A (ja) 2018-03-08
DK2134710T3 (da) 2020-05-18
CA2679754C (en) 2018-08-07
US10221176B2 (en) 2019-03-05
JP2021006559A (ja) 2021-01-21
KR20210038731A (ko) 2021-04-07
US11066407B2 (en) 2021-07-20
KR102238390B1 (ko) 2021-04-08
US20190218219A1 (en) 2019-07-18
US11407751B2 (en) 2022-08-09
MX394214B (es) 2025-03-24
EP2134710A4 (en) 2011-09-28
KR101981840B1 (ko) 2019-05-23
KR102372149B1 (ko) 2022-03-07
AU2019229334B2 (en) 2020-09-17
US20200115380A1 (en) 2020-04-16
CN103626766B (zh) 2017-06-09
KR20190083009A (ko) 2019-07-10
US10464938B2 (en) 2019-11-05
KR101999300B1 (ko) 2019-07-12
MX2020001497A (es) 2020-03-12
EP3663294A1 (en) 2020-06-10
AU2018201818B2 (en) 2019-06-20
JP2014208676A (ja) 2014-11-06
US20190292185A1 (en) 2019-09-26
CA2679754A1 (en) 2008-09-18
JP2010521464A (ja) 2010-06-24
AU2008226814A1 (en) 2008-09-18
CN101796051B (zh) 2013-11-06
AU2016234905B2 (en) 2018-03-29
JP6522710B2 (ja) 2019-05-29

Similar Documents

Publication Publication Date Title
JP6231151B2 (ja) 置換ヘテロ環縮合ガンマ−カルボリンの合成
HK1139932B (en) Substituted heterocycle fused gamma-carbolines synthesis
HK1139932A (en) Substituted heterocycle fused gamma-carbolines synthesis

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20110314

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20110314

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20130312

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20130611

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20130618

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20130711

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20130719

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20130809

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20130816

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20130912

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20131008

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20140107

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20140115

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20140207

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20140217

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20140307

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20140314

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20140408

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20140520

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20140619

R150 Certificate of patent or registration of utility model

Ref document number: 5567349

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250