IN2014CN02463A - - Google Patents

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Publication number
IN2014CN02463A
IN2014CN02463A IN2463CHN2014A IN2014CN02463A IN 2014CN02463 A IN2014CN02463 A IN 2014CN02463A IN 2463CHN2014 A IN2463CHN2014 A IN 2463CHN2014A IN 2014CN02463 A IN2014CN02463 A IN 2014CN02463A
Authority
IN
India
Prior art keywords
hydrogen atom
pde9
acceptable salt
formula
inhibitory effect
Prior art date
Application number
Inventor
Yoshihiko Norimine
Kunitoshi Takeda
Koji Hagiwara
Yuichi Suzuki
Yuki Ishihara
Nobuaki Sato
Original Assignee
Eisai R&D Man Co Ltd
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 Eisai R&D Man Co Ltd filed Critical Eisai R&D Man Co Ltd
Publication of IN2014CN02463A publication Critical patent/IN2014CN02463A/en

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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
    • C07D471/02Heterocyclic 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
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

123456A compound represented by formula (I) or a pharmacologically acceptable salt thereof which has an inhibitory effect on PDE9 and therefore is expected as being capable of increasing the cGMP level in the brain. Since the inhibitory effect on PDE9 and an increase in the cGMP level contribute to improvement in learning and memory behavior the aforesaid compound or a pharmacologically acceptable salt thereof would be available as a remedy for cognitive dysfunction in Alzheimer s disease. In formula (I): R represents a hydrogen atom; R represents an aromatic ring group etc.; R represents a hydrogen atom etc.; R represents a hydrogen atom; R represents an oxepanyl group etc.; and R represents a hydrogen atom.
IN2463CHN2014 2011-10-07 2012-10-04 IN2014CN02463A (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201161544860P 2011-10-07 2011-10-07
US201161550623P 2011-10-24 2011-10-24
US201161558110P 2011-11-10 2011-11-10
US201161580903P 2011-12-28 2011-12-28
PCT/JP2012/075748 WO2013051639A1 (en) 2011-10-07 2012-10-04 Pyrazoloquinoline derivative

Publications (1)

Publication Number Publication Date
IN2014CN02463A true IN2014CN02463A (en) 2015-06-19

Family

ID=48043792

Family Applications (1)

Application Number Title Priority Date Filing Date
IN2463CHN2014 IN2014CN02463A (en) 2011-10-07 2012-10-04

Country Status (33)

Country Link
US (2) US8563565B2 (en)
EP (1) EP2769980B1 (en)
JP (1) JP5546693B2 (en)
KR (1) KR101943680B1 (en)
CN (1) CN103930423B (en)
AR (1) AR088235A1 (en)
AU (1) AU2012319549B2 (en)
BR (1) BR112014007912B1 (en)
CA (1) CA2861795C (en)
CL (1) CL2014000821A1 (en)
CO (1) CO6910200A2 (en)
CY (1) CY1117427T1 (en)
DK (1) DK2769980T3 (en)
ES (1) ES2568015T3 (en)
HK (1) HK1199018A1 (en)
HR (1) HRP20160273T1 (en)
HU (1) HUE028555T2 (en)
IL (1) IL231650A (en)
IN (1) IN2014CN02463A (en)
JO (1) JO3116B1 (en)
ME (1) ME02394B (en)
MX (1) MX358149B (en)
MY (1) MY167698A (en)
PE (1) PE20141557A1 (en)
PL (1) PL2769980T3 (en)
RS (1) RS54702B1 (en)
RU (1) RU2605096C2 (en)
SG (1) SG11201400717QA (en)
SI (1) SI2769980T1 (en)
SM (1) SMT201600108B (en)
TW (1) TWI562993B (en)
WO (1) WO2013051639A1 (en)
ZA (1) ZA201402439B (en)

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Publication number Priority date Publication date Assignee Title
CN106905324B (en) 2011-10-10 2018-09-25 H.隆德贝克有限公司 PDE9 inhibitor with Imidazopyrazines ketone skeleton
US9550776B2 (en) * 2013-04-05 2017-01-24 Eisai R&D Management Co., Ltd. Pyridinylpyrazoloquinoline compounds
KR101997955B1 (en) * 2013-04-05 2019-07-08 에자이 알앤드디 매니지먼트 가부시키가이샤 Salt of pyrazoloquinoline derivative, and crystal thereof
GB201406486D0 (en) 2014-04-10 2014-05-28 Redx Pharma Ltd Antibacterial compounds
WO2016021192A1 (en) * 2014-08-08 2016-02-11 Eisai R&D Management Co., Ltd. Process for production of (s)-(tetrahydrofuran-3-yl)hydrazine
DK3303339T3 (en) 2015-07-07 2021-04-12 H Lundbeck As PDE9 INHIBITORS WITH THE IMIDAZOTRIAZINON SKELELINE AND IMIDAZOPYRAZINON SKELELINE FOR THE TREATMENT OF PERIOD DISEASES
WO2017046606A1 (en) * 2015-09-18 2017-03-23 Redx Pharma Plc Antibacterial compounds
CN107056690A (en) * 2017-03-22 2017-08-18 上海康鹏科技有限公司 A kind of preparation method of the formaldehyde of 6 bromopyridine 3
JP7293129B2 (en) * 2017-06-01 2023-06-19 エーザイ・アール・アンド・ディー・マネジメント株式会社 Pharmaceutical compositions containing PDE9 inhibitors
MX2019013383A (en) * 2017-06-01 2020-02-20 Eisai R&D Man Co Ltd Dementia therapeutic agent combining pyrazoloquinoline derivative and memantine.
EP3632439B1 (en) * 2017-06-01 2024-03-27 Eisai R&D Management Co., Ltd. Dementia therapeutic agent combining pyrazoloquinoline derivative and donepezil
CA3061884A1 (en) 2017-06-01 2019-10-29 Eisai R&D Management Co., Ltd. Lewy body disease therapeutic agent containing pyrazoloquinoline derivative
US11591312B2 (en) 2018-01-23 2023-02-28 Basf Se Halogenation of pyridine derivatives
JP2021526134A (en) 2018-05-25 2021-09-30 イマラ インク. 6-[(3S, 4S) -4-methyl-l- (pyrimidine-2-ylmethyl) pyrrolidine-3-yl] -3-tetrahydropyran-4-yl-7H-imidazole [l, 5-A] pyrazine- 8-one monohydrate and crystalline form
BR112021003686A2 (en) * 2018-08-31 2021-05-18 Imara Inc. pde9 inhibitors to treat sickle cell disease
BR112021011084A2 (en) * 2018-12-13 2021-08-31 Intervet International B.V. PROCESS FOR PREPARING 1-[(3R,4S)-4-CYANOTETRAHYDROPYRAN-3-IL]-3-[(2-FLUORO-6-METOXY-4-PYRIDYL)AMINO]PYRAZOLE-4-CARBOXAMIDE
US11883461B2 (en) 2019-05-09 2024-01-30 The Feinstein Institutes For Medical Research HMGB1 antagonist treatment of severe sepsis
EP3965792A4 (en) 2019-05-09 2023-01-18 The Feinstein Institutes for Medical Research Hmgb1 antagonist
WO2020227592A1 (en) 2019-05-09 2020-11-12 The Feinstein Institutes For Medical Research Thiosemicarbazates and uses thereof
AU2020268409A1 (en) * 2019-05-09 2021-11-25 The Feinstein Institutes For Medical Research Compounds for use in synthesis of peptidomimetics
US11530218B2 (en) 2020-01-20 2022-12-20 Incyte Corporation Spiro compounds as inhibitors of KRAS
CR20220584A (en) * 2020-04-16 2023-02-15 Incyte Corp Fused tricyclic kras inhibitors
US11739102B2 (en) 2020-05-13 2023-08-29 Incyte Corporation Fused pyrimidine compounds as KRAS inhibitors
US20230303549A1 (en) 2020-06-30 2023-09-28 Bayer Aktiengesellschaft Substituted heteroaryloxypyridines, the salts thereof and their use as herbicidal agents
WO2022047093A1 (en) 2020-08-28 2022-03-03 Incyte Corporation Vinyl imidazole compounds as inhibitors of kras
US11767320B2 (en) 2020-10-02 2023-09-26 Incyte Corporation Bicyclic dione compounds as inhibitors of KRAS
WO2023064857A1 (en) 2021-10-14 2023-04-20 Incyte Corporation Quinoline compounds as inhibitors of kras

Family Cites Families (12)

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Publication number Priority date Publication date Assignee Title
RU2426734C2 (en) * 2003-10-03 2011-08-20 Зм Инновейтив Пропертиз Компани Pyrazolopyridines and analogues thereof
WO2005118583A1 (en) * 2004-05-28 2005-12-15 Millennium Pharmaceuticals, Inc. 2, 5-dihydro-pyrazolo`4, 3-c!quinolin-4-ones as chk-1 inhibitors
KR20080046728A (en) * 2005-09-15 2008-05-27 아스카 세이야쿠 가부시키가이샤 Heterocyclic compound, and production process and use thereof
JP2009184924A (en) 2006-05-31 2009-08-20 Eisai R & D Management Co Ltd Compound for biological reagent
EP2103613B1 (en) * 2006-12-13 2016-02-17 ASKA Pharmaceutical Co., Ltd. Quinoxaline derivative
ME00954B (en) 2007-05-11 2012-06-20 Pfizer Amino-heterocyclic compounds
UA105362C2 (en) 2008-04-02 2014-05-12 Бьорингер Ингельхайм Интернациональ Гмбх 1-heterocyclyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a modulators
ES2612954T3 (en) * 2009-03-05 2017-05-19 Astellas Pharma Inc. Quinoxaline Compounds
NZ594567A (en) 2009-03-31 2013-12-20 Boehringer Ingelheim Int 1-heterocyclyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a modulators
US8880976B2 (en) 2009-09-25 2014-11-04 Stmicroelectronics, Inc. Method and apparatus for encoding LBA information into the parity of a LDPC system
ES2583528T3 (en) * 2010-09-07 2016-09-21 Astellas Pharma Inc. Pyrazoloquinoline compound
JP6042060B2 (en) * 2011-09-26 2016-12-14 サノフイ Pyrazoloquinolinone derivatives, their preparation and therapeutic use

Also Published As

Publication number Publication date
SG11201400717QA (en) 2014-06-27
HRP20160273T1 (en) 2016-04-08
RU2014112931A (en) 2015-11-20
JO3116B1 (en) 2017-09-20
PL2769980T3 (en) 2016-07-29
PE20141557A1 (en) 2014-11-15
US20130143907A1 (en) 2013-06-06
CL2014000821A1 (en) 2014-07-25
EP2769980A4 (en) 2015-02-25
HK1199018A1 (en) 2015-06-19
US8563565B2 (en) 2013-10-22
NZ622594A (en) 2015-06-26
SMT201600108B (en) 2016-04-29
EP2769980B1 (en) 2016-02-03
CA2861795C (en) 2018-12-04
RS54702B1 (en) 2016-08-31
MX2014003800A (en) 2014-07-28
EP2769980A1 (en) 2014-08-27
HUE028555T2 (en) 2016-12-28
RU2605096C2 (en) 2016-12-20
MY167698A (en) 2018-09-21
TW201321379A (en) 2013-06-01
BR112014007912A2 (en) 2017-04-04
CN103930423B (en) 2015-09-16
SI2769980T1 (en) 2016-08-31
US20130296352A1 (en) 2013-11-07
CA2861795A1 (en) 2013-04-11
AU2012319549A1 (en) 2014-04-24
BR112014007912B1 (en) 2022-06-07
CY1117427T1 (en) 2017-04-26
AR088235A1 (en) 2014-05-21
IL231650A (en) 2016-05-31
JPWO2013051639A1 (en) 2015-03-30
CO6910200A2 (en) 2014-03-31
JP5546693B2 (en) 2014-07-09
ME02394B (en) 2016-09-20
CN103930423A (en) 2014-07-16
TWI562993B (en) 2016-12-21
AU2012319549B2 (en) 2016-07-28
ZA201402439B (en) 2015-03-25
KR20140082684A (en) 2014-07-02
ES2568015T3 (en) 2016-04-27
KR101943680B1 (en) 2019-01-29
WO2013051639A1 (en) 2013-04-11
MX358149B (en) 2018-08-07
DK2769980T3 (en) 2016-04-11
IL231650A0 (en) 2014-05-28

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