RU2675851C2 - Кристаллические формы свободного основания - Google Patents

Кристаллические формы свободного основания Download PDF

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Publication number
RU2675851C2
RU2675851C2 RU2016101630A RU2016101630A RU2675851C2 RU 2675851 C2 RU2675851 C2 RU 2675851C2 RU 2016101630 A RU2016101630 A RU 2016101630A RU 2016101630 A RU2016101630 A RU 2016101630A RU 2675851 C2 RU2675851 C2 RU 2675851C2
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RU
Russia
Prior art keywords
methyl
crystalline form
free base
crystalline
salt
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Application number
RU2016101630A
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English (en)
Russian (ru)
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RU2016101630A (ru
RU2016101630A3 (enExample
Inventor
Такаси АБЕ
Грэхем БАКТОН
Роберт ДЭВИС
Марк ХУПЕР
Пэн ЛИ
Хидеаки МАРУЯМА
Масахиро ТАКАСУГА
Лоуренс П. УЭННОГЛ
Юхеи ЯМАМОТО
Хиронори ЯМАСИТА
Original Assignee
Интра-Селлулар Терапиз, Инк.
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Publication of RU2016101630A publication Critical patent/RU2016101630A/ru
Publication of RU2016101630A3 publication Critical patent/RU2016101630A3/ru
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic 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
    • C07D487/14—Ortho-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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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)
  • 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)
RU2016101630A 2013-06-21 2014-06-20 Кристаллические формы свободного основания RU2675851C2 (ru)

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 (3)

Publication Number Publication Date
RU2016101630A RU2016101630A (ru) 2017-07-26
RU2016101630A3 RU2016101630A3 (enExample) 2018-03-21
RU2675851C2 true RU2675851C2 (ru) 2018-12-25

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
RU2016101630A RU2675851C2 (ru) 2013-06-21 2014-06-20 Кристаллические формы свободного основания

Country Status (13)

Country Link
US (1) US9630971B2 (enExample)
EP (2) EP3010509B1 (enExample)
JP (2) JP6865036B2 (enExample)
KR (2) KR102430126B1 (enExample)
CN (3) CN105658222A (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 (10)

* Cited by examiner, † Cited by third party
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EP2717877B1 (en) 2011-06-10 2017-11-08 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
US12410175B2 (en) 2019-09-03 2025-09-09 Intra-Cellular Therapies, Inc. Compounds
US12435093B2 (en) 2020-05-06 2025-10-07 Intra-Cellular Therapies, Inc. Free base crystals
WO2022026417A1 (en) * 2020-07-26 2022-02-03 Intra-Cellular Therapies, Inc. Novel uses
JP2024531548A (ja) * 2021-09-03 2024-08-29 イントラ－セルラー・セラピーズ・インコーポレイテッド 共結晶
WO2023147484A1 (en) * 2022-01-27 2023-08-03 Intra-Cellular Therapies, Inc. Novel compositions
WO2023147603A2 (en) * 2022-01-31 2023-08-03 Intra-Cellular Therapies, Inc. Salt crystals
WO2023233410A1 (en) * 2022-06-02 2023-12-07 Biosight Ltd. Crystalline form of aspacytarabine intermediate

Citations (3)

* 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
EA201170770A1 (ru) * 2008-12-06 2012-02-28 Интра-Селлулар Терапиз, Инк. Органические соединения
US20120053190A1 (en) * 2009-05-13 2012-03-01 Fienberg Allen A Organic compounds

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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
ATE496028T1 (de) * 2002-02-08 2011-02-15 Ono Pharmaceutical Co Piperidinderivatverbindungen und arzneimittel, die diese verbindungen als wirkstoff enthalten
EP1613747A1 (en) 2003-03-31 2006-01-11 Pfizer Products Inc. Crystal structure of 3 ,5 -cyclic nucleotide phosphodiesterase 1b (pde1b) and uses thereof
CN100457108C (zh) * 2003-09-02 2009-02-04 默克公司 一种二肽基肽酶iv抑制剂的磷酸盐新晶体
CN101031548B (zh) * 2004-09-27 2011-04-06 阿卡蒂亚药品公司 N-(4-氟苄基)-n-(1-甲基哌啶-4-基)-n'-(4-(2-甲基丙氧基)-苯基甲基)脲的盐及其制备
WO2006133261A2 (en) 2005-06-06 2006-12-14 Intra-Cellular Therapies, Inc. Organic compounds
WO2008063505A1 (en) 2006-11-13 2008-05-29 Intra-Cellular Therapies, Inc. Organic compounds
WO2008070095A1 (en) 2006-12-05 2008-06-12 Intra-Cellular Therapies, Inc. Novel uses
US20120070443A1 (en) 2008-12-02 2012-03-22 University Of Utah Research Foundation Pde1 as a target therapeutic in heart disease
EA201170769A1 (ru) 2008-12-06 2012-02-28 Интра-Селлулар Терапиз, Инк. Органические соединения
AU2009322903A1 (en) 2008-12-06 2010-06-10 Intra-Cellular Therapies, Inc. Organic compounds
WO2010098839A1 (en) 2009-02-25 2010-09-02 Intra-Cellular Therapies, Inc. Pde 1 inhibitors for ophthalmic disorders
US8858911B2 (en) 2009-10-08 2014-10-14 Intra-Cellular Therapies, Inc. Phosphodiesterase 1-targeting tracers and methods
TW201206937A (en) 2010-05-31 2012-02-16 Intra Cellular Therapies Inc Organic compounds
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EP2717877B1 (en) 2011-06-10 2017-11-08 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

Patent Citations (4)

* 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
US20120238589A1 (en) * 2007-12-06 2012-09-20 Peng Li Organic compounds
EA201170770A1 (ru) * 2008-12-06 2012-02-28 Интра-Селлулар Терапиз, Инк. Органические соединения
US20120053190A1 (en) * 2009-05-13 2012-03-01 Fienberg Allen A Organic compounds

Also Published As

Publication number Publication date
CN110498800A (zh) 2019-11-26
EP3010509A2 (en) 2016-04-27
EP3010509A4 (en) 2016-11-23
KR102430126B1 (ko) 2022-08-05
RU2016101630A (ru) 2017-07-26
WO2014205354A3 (en) 2015-05-28
CN105658222A (zh) 2016-06-08
AU2014284224B2 (en) 2019-08-01
BR112015032132A2 (pt) 2017-07-25
KR20160040522A (ko) 2016-04-14
EP3702358A1 (en) 2020-09-02
JP2019189618A (ja) 2019-10-31
JP6865036B2 (ja) 2021-04-28
MX2020001628A (es) 2020-07-13
CA2916393C (en) 2022-03-22
IL267331B2 (en) 2024-12-01
CA2916393A1 (en) 2014-12-24
CN112851683A (zh) 2021-05-28
ES2894770T3 (es) 2022-02-15
US9630971B2 (en) 2017-04-25
WO2014205354A2 (en) 2014-12-24
MX2015017972A (es) 2016-10-28
IL267331B1 (en) 2024-08-01
RU2016101630A3 (enExample) 2018-03-21
IL243269A0 (en) 2016-02-29
AU2014284224A1 (en) 2016-02-11
KR20210122890A (ko) 2021-10-12
IL267331A (en) 2019-08-29
IL243269B (en) 2019-06-30
US20160145261A1 (en) 2016-05-26
HK1223848A1 (zh) 2017-08-11
EP3010509B1 (en) 2021-07-28
BR112015032132B1 (pt) 2022-03-15
JP2016523258A (ja) 2016-08-08

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