IL267331B2 - Process For The Preparation Of A Mono-Phosphate Salt Crystal Of (6aR,9aS)-5,6a,7,8,9,9a-Hexahydro-5-Methyl-3-(Phenylamino) -2-((4-(6-Fluoropyridin-2-yl)Phenyl)Methyl)-Cyclopent[4,5]Imidazo[1,2-A] -Pyrazolo[4,3-E]Pyrimidin-4(2H)-One - Google Patents

Process For The Preparation Of A Mono-Phosphate Salt Crystal Of (6aR,9aS)-5,6a,7,8,9,9a-Hexahydro-5-Methyl-3-(Phenylamino) -2-((4-(6-Fluoropyridin-2-yl)Phenyl)Methyl)-Cyclopent[4,5]Imidazo[1,2-A] -Pyrazolo[4,3-E]Pyrimidin-4(2H)-One

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Publication number
IL267331B2
IL267331B2 IL267331A IL26733119A IL267331B2 IL 267331 B2 IL267331 B2 IL 267331B2 IL 267331 A IL267331 A IL 267331A IL 26733119 A IL26733119 A IL 26733119A IL 267331 B2 IL267331 B2 IL 267331B2
Authority
IL
Israel
Prior art keywords
methyl
free base
crystal
pyrazolo
pyrimidin
Prior art date
Application number
IL267331A
Other languages
English (en)
Hebrew (he)
Other versions
IL267331A (en
IL267331B1 (en
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 IL267331A publication Critical patent/IL267331A/en
Publication of IL267331B1 publication Critical patent/IL267331B1/en
Publication of IL267331B2 publication Critical patent/IL267331B2/en

Links

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)
IL267331A 2013-06-21 2014-06-20 Process For The Preparation Of A Mono-Phosphate Salt Crystal Of (6aR,9aS)-5,6a,7,8,9,9a-Hexahydro-5-Methyl-3-(Phenylamino) -2-((4-(6-Fluoropyridin-2-yl)Phenyl)Methyl)-Cyclopent[4,5]Imidazo[1,2-A] -Pyrazolo[4,3-E]Pyrimidin-4(2H)-One IL267331B2 (en)

Applications Claiming Priority (3)

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

Publications (3)

Publication Number Publication Date
IL267331A IL267331A (en) 2019-08-29
IL267331B1 IL267331B1 (en) 2024-08-01
IL267331B2 true IL267331B2 (en) 2024-12-01

Family

ID=52105535

Family Applications (2)

Application Number Title Priority Date Filing Date
IL267331A IL267331B2 (en) 2013-06-21 2014-06-20 Process For The Preparation Of A Mono-Phosphate Salt Crystal Of (6aR,9aS)-5,6a,7,8,9,9a-Hexahydro-5-Methyl-3-(Phenylamino) -2-((4-(6-Fluoropyridin-2-yl)Phenyl)Methyl)-Cyclopent[4,5]Imidazo[1,2-A] -Pyrazolo[4,3-E]Pyrimidin-4(2H)-One
IL243269A IL243269B (en) 2013-06-21 2015-12-21 Crystals of (sa9,ra6)-a9,9,8,7,a6,5-hexahydro-5-methyl-3-(phenylamino)-2- ((4-(6-fluoropyridin-2-yl)phenyl)methyl ) cyclopent[5,4]imidazo[a-2,1]pyrazolo[e-3,4]pyrimidine-4(h2)-one, their salts and a process for preparing the salts.

Family Applications After (1)

Application Number Title Priority Date Filing Date
IL243269A IL243269B (en) 2013-06-21 2015-12-21 Crystals of (sa9,ra6)-a9,9,8,7,a6,5-hexahydro-5-methyl-3-(phenylamino)-2- ((4-(6-fluoropyridin-2-yl)phenyl)methyl ) cyclopent[5,4]imidazo[a-2,1]pyrazolo[e-3,4]pyrimidine-4(h2)-one, their salts and a process for preparing the salts.

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

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GB9412571D0 (en) 1994-06-22 1994-08-10 Celltech Ltd Chemical compounds
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
WO2009075784A1 (en) 2007-12-06 2009-06-18 Intra-Cellular Therapies, Inc. Organic compounds
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
US9468637B2 (en) * 2009-05-13 2016-10-18 Intra-Cellular Therapies, Inc. Organic compounds
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
JP5911854B2 (ja) 2010-05-31 2016-04-27 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
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
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

Also Published As

Publication number Publication date
ES2894770T3 (es) 2022-02-15
EP3010509A4 (en) 2016-11-23
KR20210122890A (ko) 2021-10-12
AU2014284224B2 (en) 2019-08-01
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
JP6865036B2 (ja) 2021-04-28
EP3010509B1 (en) 2021-07-28

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