AU2014284224B2 - Free base crystals - Google Patents

Free base crystals Download PDF

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Publication number
AU2014284224B2
AU2014284224B2 AU2014284224A AU2014284224A AU2014284224B2 AU 2014284224 B2 AU2014284224 B2 AU 2014284224B2 AU 2014284224 A AU2014284224 A AU 2014284224A AU 2014284224 A AU2014284224 A AU 2014284224A AU 2014284224 B2 AU2014284224 B2 AU 2014284224B2
Authority
AU
Australia
Prior art keywords
methyl
crystal
free base
pyrazolo
imidazo
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.)
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Application number
AU2014284224A
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English (en)
Other versions
AU2014284224A1 (en
Inventor
Takashi Abe
Graham Buckton
Robert Davis
Mark Hooper
Peng Li
Hideaki Maruyama
Masahiro TAKASUGA
Lawrence P. Wennogle
Yuhei Yamamoto
Hironori Yamashita
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.)
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Publication date
Application filed by Intra Cellular Therapies Inc filed Critical Intra Cellular Therapies Inc
Publication of AU2014284224A1 publication Critical patent/AU2014284224A1/en
Application granted granted Critical
Publication of AU2014284224B2 publication Critical patent/AU2014284224B2/en
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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14Ortho-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
    • 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2014284224A 2013-06-21 2014-06-20 Free base crystals Active AU2014284224B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361838105P 2013-06-21 2013-06-21
US61/838,105 2013-06-21
US201361919424P 2013-12-20 2013-12-20
US61/919,424 2013-12-20
PCT/US2014/043422 WO2014205354A2 (en) 2013-06-21 2014-06-20 Free base crystals

Publications (2)

Publication Number Publication Date
AU2014284224A1 AU2014284224A1 (en) 2016-02-11
AU2014284224B2 true AU2014284224B2 (en) 2019-08-01

Family

ID=52105535

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2014284224A Active AU2014284224B2 (en) 2013-06-21 2014-06-20 Free base crystals

Country Status (13)

Country Link
US (1) US9630971B2 (enExample)
EP (2) EP3010509B1 (enExample)
JP (2) JP6865036B2 (enExample)
KR (2) KR20160040522A (enExample)
CN (3) CN112851683A (enExample)
AU (1) AU2014284224B2 (enExample)
BR (1) BR112015032132B1 (enExample)
CA (1) CA2916393C (enExample)
ES (1) ES2894770T3 (enExample)
IL (2) IL267331B2 (enExample)
MX (2) MX2015017972A (enExample)
RU (1) RU2675851C2 (enExample)
WO (1) WO2014205354A2 (enExample)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10561656B2 (en) 2011-06-10 2020-02-18 Intra-Cellular Therapies, Inc. Organic compounds
AR091507A1 (es) 2012-06-21 2015-02-11 Intra Cellular Therapies Inc SALES DE (6aR,9aS)-5,6a,7,8,9,9a-HEXAHIDRO-5-METIL-3-(FENILAMINO)-2-((4-(6-FLUOROPIRIDIN-2-IL)FENIL)METIL)-CICLOPENT[4,5]IMIDAZO[1,2-a]PIRAZOLO[4,3-e]PIRIMIDIN-4(2H)-ONA
EP3010509B1 (en) 2013-06-21 2021-07-28 Intra-Cellular Therapies, Inc. Free base crystals
EP4413980A3 (en) 2019-09-03 2024-10-30 Intra-Cellular Therapies, Inc. Novel compounds
US12435093B2 (en) 2020-05-06 2025-10-07 Intra-Cellular Therapies, Inc. Free base crystals
JP2023535224A (ja) * 2020-07-26 2023-08-16 イントラ-セルラー・セラピーズ・インコーポレイテッド 新規使用
EP4395767A4 (en) * 2021-09-03 2025-07-23 Intra Cellular Therapies Inc CO-CRYSTALS
US20250144029A1 (en) * 2022-01-27 2025-05-08 Intra-Cellular Therapies, Inc. Novel compositions
WO2023233410A1 (en) * 2022-06-02 2023-12-07 Biosight Ltd. Crystalline form of aspacytarabine intermediate

Citations (2)

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WO2009075784A1 (en) * 2007-12-06 2009-06-18 Intra-Cellular Therapies, Inc. Organic compounds
WO2013192556A2 (en) * 2012-06-21 2013-12-27 Intra-Cellular Therapies, Inc. Salt crystals

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US5471001A (en) * 1994-12-15 1995-11-28 E. I. Du Pont De Nemours And Company Crystallization of adipic acid
GB9624615D0 (en) 1996-11-26 1997-01-15 Zeneca Ltd Chrystallisation process
TWI265925B (en) 1999-10-11 2006-11-11 Pfizer Pyrazolo[4,3-d]pyrimidin-7-ones useful in inhibiting type 5 cyclic guanosine 3',5'-monophosphate phosphodiesterases(cGMP PDE5), process and intermediates for their preparation, their uses and composition comprising them
WO2003066590A1 (en) 2002-02-08 2003-08-14 Ono Pharmaceutical Co., Ltd. Piperidine derivative compounds and drugs containing the compounds as the active ingredient
EP1613747A1 (en) * 2003-03-31 2006-01-11 Pfizer Products Inc. Crystal structure of 3 ,5 -cyclic nucleotide phosphodiesterase 1b (pde1b) and uses thereof
AU2004268024B2 (en) 2003-09-02 2007-07-12 Merck Sharp & Dohme Llc Novel crystalline forms of a phosphoric acid salt of a dipeptidyl peptidase-IV inhibitor
DK1794126T3 (da) * 2004-09-27 2013-06-24 Acadia Pharm Inc Krystallinsk form af N-(-4-fluorbenzyl)-N-(1-methylpiperidn-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl)carbamid-hemitartrat
CN101248050B (zh) 2005-06-06 2013-07-17 武田药品工业株式会社 有机化合物
WO2008063505A1 (en) 2006-11-13 2008-05-29 Intra-Cellular Therapies, Inc. Organic compounds
US9006258B2 (en) 2006-12-05 2015-04-14 Intra-Cellular Therapies, Inc. Method of treating female sexual dysfunction with a PDE1 inhibitor
US20120070443A1 (en) 2008-12-02 2012-03-22 University Of Utah Research Foundation Pde1 as a target therapeutic in heart disease
EP2367429B1 (en) 2008-12-06 2017-06-07 Intra-Cellular Therapies, Inc. Organic compounds
EP2358204B1 (en) 2008-12-06 2015-08-05 Intra-Cellular Therapies, Inc. 4,5,7,8-tetrahydro-4-oxo-2H-imidazo[1,2-a]pyrrolo[3,4-e]pyrimidine compounds as PDE1 inhibitors.
CN102232077A (zh) 2008-12-06 2011-11-02 细胞内治疗公司 有机化合物
EP2400970A4 (en) 2009-02-25 2012-07-18 Intra Cellular Therapies Inc PDE-1-HEMMER FOR EYE DRESSING
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JP2013507360A (ja) 2009-10-08 2013-03-04 イントラ−セルラー・セラピーズ・インコーポレイテッド ホスホジエステラーゼ1−標的トレーサーおよび方法
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TW201206937A (en) 2010-05-31 2012-02-16 Intra Cellular Therapies Inc Organic compounds
US10561656B2 (en) 2011-06-10 2020-02-18 Intra-Cellular Therapies, Inc. Organic compounds
EP3010509B1 (en) 2013-06-21 2021-07-28 Intra-Cellular Therapies, Inc. Free base crystals

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009075784A1 (en) * 2007-12-06 2009-06-18 Intra-Cellular Therapies, Inc. Organic compounds
WO2013192556A2 (en) * 2012-06-21 2013-12-27 Intra-Cellular Therapies, Inc. Salt crystals

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
BOWKER ET AL, A Procedure for Salt Selection and Optimization, HANDBOOK OF PHARMACEUTICAL SALTS : PROPERTIES, SELECTION, AND USE, ZÜRICH : VERL. HELVETICA CHIMICA ACTA ; PAGE(S) 162 - 173, (2002-01-01), ISBN 978-3-906390-26-0 *
CAIRA, "Crystalline Polymorphism of Organic Compounds", TOPICS IN CURRENT CHEMISTRY, SPRINGER, BERLIN, DE, (1998-01-01), vol. 198, ISSN 0340-1022, pages 163 - 208 *
HILFIKER R (EDITOR) ED - HILFIKER R, Polymorphism in the Pharmaceutical Industry, 2006-01-01, PAGE(S) 1 - 19, (2006-01-01), ISBN 978-3-527-31146-0 *
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Also Published As

Publication number Publication date
ES2894770T3 (es) 2022-02-15
EP3010509A4 (en) 2016-11-23
KR20210122890A (ko) 2021-10-12
MX2015017972A (es) 2016-10-28
CN112851683A (zh) 2021-05-28
AU2014284224A1 (en) 2016-02-11
BR112015032132B1 (pt) 2022-03-15
EP3702358A1 (en) 2020-09-02
IL243269B (en) 2019-06-30
WO2014205354A3 (en) 2015-05-28
RU2675851C2 (ru) 2018-12-25
MX2020001628A (es) 2020-07-13
IL267331A (en) 2019-08-29
KR20160040522A (ko) 2016-04-14
CA2916393C (en) 2022-03-22
EP3010509A2 (en) 2016-04-27
RU2016101630A3 (enExample) 2018-03-21
RU2016101630A (ru) 2017-07-26
JP2016523258A (ja) 2016-08-08
CN110498800A (zh) 2019-11-26
HK1223848A1 (zh) 2017-08-11
US9630971B2 (en) 2017-04-25
JP2019189618A (ja) 2019-10-31
KR102430126B1 (ko) 2022-08-05
BR112015032132A2 (pt) 2017-07-25
CA2916393A1 (en) 2014-12-24
IL243269A0 (en) 2016-02-29
IL267331B1 (en) 2024-08-01
WO2014205354A2 (en) 2014-12-24
US20160145261A1 (en) 2016-05-26
CN105658222A (zh) 2016-06-08
IL267331B2 (en) 2024-12-01
JP6865036B2 (ja) 2021-04-28
EP3010509B1 (en) 2021-07-28

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