KR102430126B1 - 유리 염기 결정 - Google Patents

유리 염기 결정 Download PDF

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Publication number
KR102430126B1
KR102430126B1 KR1020217030964A KR20217030964A KR102430126B1 KR 102430126 B1 KR102430126 B1 KR 102430126B1 KR 1020217030964 A KR1020217030964 A KR 1020217030964A KR 20217030964 A KR20217030964 A KR 20217030964A KR 102430126 B1 KR102430126 B1 KR 102430126B1
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KR
South Korea
Prior art keywords
methyl
free base
crystals
pyrazolo
imidazo
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KR1020217030964A
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English (en)
Korean (ko)
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KR20210122890A (ko
Inventor
다카시 아베
그라함 북톤
로버트 데이비스
마크 후퍼
펭 리
히데아키 마루야마
마사히로 다카수가
로렌스 피. 웨노글
유헤이 야마모토
히로노리 야마시타
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인트라-셀룰라 써래피스, 인코퍼레이티드.
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Publication of KR20210122890A publication Critical patent/KR20210122890A/ko
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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)
KR1020217030964A 2013-06-21 2014-06-20 유리 염기 결정 Active KR102430126B1 (ko)

Applications Claiming Priority (6)

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
KR1020167001273A KR20160040522A (ko) 2013-06-21 2014-06-20 유리 염기 결정
PCT/US2014/043422 WO2014205354A2 (en) 2013-06-21 2014-06-20 Free base crystals

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
KR1020167001273A Division KR20160040522A (ko) 2013-06-21 2014-06-20 유리 염기 결정

Publications (2)

Publication Number Publication Date
KR20210122890A KR20210122890A (ko) 2021-10-12
KR102430126B1 true KR102430126B1 (ko) 2022-08-05

Family

ID=52105535

Family Applications (2)

Application Number Title Priority Date Filing Date
KR1020217030964A Active KR102430126B1 (ko) 2013-06-21 2014-06-20 유리 염기 결정
KR1020167001273A Ceased KR20160040522A (ko) 2013-06-21 2014-06-20 유리 염기 결정

Family Applications After (1)

Application Number Title Priority Date Filing Date
KR1020167001273A Ceased KR20160040522A (ko) 2013-06-21 2014-06-20 유리 염기 결정

Country Status (13)

Country Link
US (1) US9630971B2 (https=)
EP (2) EP3010509B1 (https=)
JP (2) JP6865036B2 (https=)
KR (2) KR102430126B1 (https=)
CN (3) CN105658222A (https=)
AU (1) AU2014284224B2 (https=)
BR (1) BR112015032132B1 (https=)
CA (1) CA2916393C (https=)
ES (1) ES2894770T3 (https=)
IL (2) IL267331B2 (https=)
MX (2) MX2015017972A (https=)
RU (1) RU2675851C2 (https=)
WO (1) WO2014205354A2 (https=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN105658222A (zh) 2013-06-21 2016-06-08 细胞内治疗公司 游离碱晶体
EP4025202A4 (en) 2019-09-03 2023-08-02 Intra-Cellular Therapies, Inc. NOVEL CONNECTIONS
WO2021226407A1 (en) * 2020-05-06 2021-11-11 Intra-Cellular Therapies, Inc. Free base crystals
EP4188353A4 (en) * 2020-07-26 2024-07-03 Intra-Cellular Therapies, Inc. Novel uses
EP4395767A4 (en) * 2021-09-03 2025-07-23 Intra Cellular Therapies Inc CO-CRYSTALS
EP4469052A4 (en) * 2022-01-27 2026-02-11 Intra Cellular Therapies Inc NEW 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 (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2001504758A (ja) 1996-11-26 2001-04-10 ゼネカ リミテッド 結晶化方法
JP2007504230A (ja) 2003-09-02 2007-03-01 メルク　エンド　カムパニー　インコーポレーテッド ジペプチジルペプチダーゼ−ｉｖ阻害剤のリン酸塩の新規結晶性形態
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

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
TWI305530B (en) * 2002-02-08 2009-01-21 Ono Pharmaceutical Co Piperidine derivative compound and pharmaceuticals containing same as 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
CA2580129A1 (en) * 2004-09-27 2006-04-06 Acadia Pharmaceuticals Inc. Salts of n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and their preparation
US8273750B2 (en) 2005-06-06 2012-09-25 Takeda Pharmaceutical Company Limited Organic compounds
JP2010509399A (ja) 2006-11-13 2010-03-25 イントラ−セルラー・セラピーズ・インコーポレイテッド 有機化合物
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
MX2011005936A (es) 2008-12-06 2011-12-16 Intra Cellular Therapies Inc Compuestos organicos.
JP5989993B2 (ja) 2008-12-06 2016-09-07 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
CN102231953A (zh) 2008-12-06 2011-11-02 细胞内治疗公司 有机化合物
JP2012518685A (ja) 2009-02-25 2012-08-16 イントラ−セルラー・セラピーズ・インコーポレイテッド 眼障害のためのｐｄｅ１阻害剤
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
TW201206937A (en) 2010-05-31 2012-02-16 Intra Cellular Therapies Inc Organic compounds
US9763948B2 (en) 2010-05-31 2017-09-19 Intra-Cellular Therapies, Inc. PDE1 inhibitory compounds and methods
EP2717877B1 (en) 2011-06-10 2017-11-08 Intra-Cellular Therapies, Inc. Organic compounds
CN105658222A (zh) 2013-06-21 2016-06-08 细胞内治疗公司 游离碱晶体

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2001504758A (ja) 1996-11-26 2001-04-10 ゼネカ リミテッド 結晶化方法
JP2007504230A (ja) 2003-09-02 2007-03-01 メルク　エンド　カムパニー　インコーポレーテッド ジペプチジルペプチダーゼ−ｉｖ阻害剤のリン酸塩の新規結晶性形態
WO2009075784A1 (en) 2007-12-06 2009-06-18 Intra-Cellular Therapies, Inc. Organic compounds
JP2011506321A (ja) * 2007-12-06 2011-03-03 イントラ−セルラー・セラピーズ・インコーポレイテッド 有機化合物
WO2013192556A2 (en) 2012-06-21 2013-12-27 Intra-Cellular Therapies, Inc. Salt crystals

Also Published As

Publication number Publication date
BR112015032132A2 (pt) 2017-07-25
KR20210122890A (ko) 2021-10-12
IL267331B2 (en) 2024-12-01
IL243269A0 (en) 2016-02-29
HK1223848A1 (zh) 2017-08-11
JP2019189618A (ja) 2019-10-31
MX2015017972A (es) 2016-10-28
US20160145261A1 (en) 2016-05-26
WO2014205354A2 (en) 2014-12-24
KR20160040522A (ko) 2016-04-14
IL267331B1 (en) 2024-08-01
CA2916393C (en) 2022-03-22
MX2020001628A (es) 2020-07-13
WO2014205354A3 (en) 2015-05-28
AU2014284224A1 (en) 2016-02-11
RU2675851C2 (ru) 2018-12-25
AU2014284224B2 (en) 2019-08-01
EP3010509A2 (en) 2016-04-27
CA2916393A1 (en) 2014-12-24
IL243269B (en) 2019-06-30
JP6865036B2 (ja) 2021-04-28
RU2016101630A (ru) 2017-07-26
ES2894770T3 (es) 2022-02-15
IL267331A (en) 2019-08-29
BR112015032132B1 (pt) 2022-03-15
US9630971B2 (en) 2017-04-25
CN110498800A (zh) 2019-11-26
EP3010509B1 (en) 2021-07-28
JP2016523258A (ja) 2016-08-08
CN105658222A (zh) 2016-06-08
CN112851683A (zh) 2021-05-28
EP3702358A1 (en) 2020-09-02
RU2016101630A3 (https=) 2018-03-21
EP3010509A4 (en) 2016-11-23

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